Sign In to Follow Application
View All Documents & Correspondence

Benzotriazole Derivative

Abstract: The present invention provides: a compound having a Keap1-inhibitory effect; and a pharmaceutical composition containing the same. Specifically, the present invention provides: a compound represented by general formula (1) [in the formula, symbols have meanings as described in the specification.], or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing the same.

Get Free WhatsApp Updates!
Notices, Deadlines & Correspondence

Patent Information

Application #
Filing Date
09 December 2021
Publication Number
23/2022
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
sna@sna-ip.com
Parent Application
Patent Number
Legal Status
Grant Date
2024-08-20
Renewal Date

Applicants

UBE INDUSTRIES, LTD.
1978-96, Oaza Kogushi, Ube-shi, Yamaguchi 7558633

Inventors

1. KOMORI, Ken-ichi
c/o UBE INDUSTRIES, LTD., 1978-96, Oaza Kogushi, Ube-shi, Yamaguchi 7558633
2. NISHIYAMA, Hayato
c/o UBE INDUSTRIES, LTD., 1978-96, Oaza Kogushi, Ube-shi, Yamaguchi 7558633
3. KINOSHITA, Naoya
c/o UBE INDUSTRIES, LTD., 1978-96, Oaza Kogushi, Ube-shi, Yamaguchi 7558633
4. WADA, Yukinori
c/o UBE INDUSTRIES, LTD., 1978-96, Oaza Kogushi, Ube-shi, Yamaguchi 7558633
5. MORISHITA, Kousuke
c/o UBE INDUSTRIES, LTD., 1978-96, Oaza Kogushi, Ube-shi, Yamaguchi 7558633
6. NINOMIYA, Akishi
c/o UBE INDUSTRIES, LTD., 1978-96, Oaza Kogushi, Ube-shi, Yamaguchi 7558633
7. SHIRAISHI, Yuusuke
c/o UBE INDUSTRIES, LTD., 1978-96, Oaza Kogushi, Ube-shi, Yamaguchi 7558633
8. ONUMA, Kazuhiro
c/o UBE INDUSTRIES, LTD., 1978-96, Oaza Kogushi, Ube-shi, Yamaguchi 7558633
9. OGI, Sayaka
c/o UBE INDUSTRIES, LTD., 1978-96, Oaza Kogushi, Ube-shi, Yamaguchi 7558633
10. KAWADA, Hiroyoshi
c/o UBE INDUSTRIES, LTD., 1978-96, Oaza Kogushi, Ube-shi, Yamaguchi 7558633
11. KIMURA, Tomio
5-10-3209, Konan 3-chome, Minato-ku, Tokyo 1080075

Specification

[0001]The present invention relates to benzotriazole derivatives and pharmaceutical compositions comprising the same, especially benzotriazole derivatives and 10 pharmaceutical compositions comprising the same for the prevention, alleviation, and/or treatment of diseases of which symptoms are improved by the inhibition of Keap1.
BACKGROUND ART 15 [0002]
Nrf2 (NF-E2 related factor 2) is a transcription factor which belongs to the CNC (cap-n-collar) transcription factor group having a basic leucine zipper structure (bZIPstructure). Keap1 (Kelch-like ECH-20 associated protein 1) is an adaptor protein which is associated with Cullin3 (Cul3) in cytoplasm to form a proteasomal degradation E3 enzyme complex, and functions as an inhibitory regulatory factor which ubiquitinates Nrf2 and thereby promotes its degradation under basic 25 conditions. Under oxidative stress conditions caused by
1

PCT/JP2020/021426
electrophile materials, reactive oxygen species, or the like, a Keap1-Cul3 complex is inactivated, and Nrf2 is activated. Activated Nrf2 is transfered to a nucleus, and forms a heterodimer with a small Maf transcription factor 5 to bind to an Antioxidant Response Element (ARE) and
activite the gene expressions of biological defense enzyme group such as NAD(P)H Quinone Dehydrogenase1 (NQO1) (Nonpatent Document 1). Thus, a Keap1 inhibitor which has an inhibitory effect on the binding ofKeap1 and Nrf2 is
10 expected to be useful especially in diseases caused by oxidative stresses. [0003]
The treatment caused by an antioxidant function induction effect mediated by the binding inhibition of
15 Keap1 and Nrf2 is expected to be useful in wide range of diseases. Especially, in chronic renal diseases, it is reported that an irreversible Keap1 inhibitor, bardoxolone methyl (CDDO-Me) improved the kidney functions in human patients (Nonpatent Document 2), and a plurarity of
20 clinical trials are now in progress. Also, dimethyl
fumarate which has an Nrf2 activating effect is approroved in U.S. as a therapeutic agent of relapsing-remitting multiple sclerosis. In reports relating to Keap1 inhibitors in preclinical phases, possibilities as
25 therapeutic agents of various diseases have been suggested
2

PCT/JP2020/021426
such as hepatic fibrogenesis inhibitory effects in a NASH model (Nonpatent Document 3), anti-inflammatory effects in a inflammatory bowel disease model and chronic obstructive pulmonary disease model (Nonpatent Documents 4 and 5), 5 anti-tumor effects in solid cancers such as prostate cancer (Nonpatent Document 6), and clinical score improving effects in a multiple sclerosis model (Nonpatent Document 7). [0004]
10 The reports of genetically modified animals or
oxidative stresses and pathological models relating to Keap1-Nrf2 pathway suggest the relations to even more diseases. Specific examples thereof include chronic lung infection, α1-antitrypsin disease, and cystic fibrosis
15 (Nonpatent Document 8), sepsis-induced acute kidney injury and other acute kidney injuries (Nonpatent Document 9), atherosclerosis, heart failure, acute coronary syndrome, myocardial infarction, myocardial repair, cardiac remodeling, cardiac arrhythmia, heart failure with
20 maintained left ventricular ejection fraction, heart
failure with reduced left ventricular ejection fraction, and various cardiovascular diseases including diabetic cardiomyopathy (Nonpatent Document 10), Parkinson’s disease, Alzheimer’s disease, and Amyotrophic lateral
25 sclerosis (Nonpatent Document 11), Friedreich's ataxia
3

PCT/JP2020/021426
(Nonpatent Document 12), Age-related macular degeneration, Fuchs' endothelial dystrophy, and other inflammatory eye pathologies including uveitis (Nonpatent Document 13), dermatitis caused by radiation or the like (Nonpatent 5 Document 14), immune suppression (Nonpatent Document 15), acute mountain sickness (Nonpatent Document 16), and the others. [0005]
To date, triazole compounds are disclosed in Patent 10 Documents 1 to 17, and Nonpatent Documents 17 and 18 as compounds having Keap1 inhibitory activities, but these compounds have different structures from the Present compound.
15 CITATION LIST
2015/092713 pamphlet 2016/202253 pamphlet 2016/203400 pamphlet 2016/203401 pamphlet 2017/060854 pamphlet 2017/060855 pamphlet 2018/104766 pamphlet 2018/109641 pamphlet
PATENT DOCUMENT [0006]
Patent Document 1: WO
Patent Document 2: WO 20 Patent Document 3: WO
Patent Document 4: WO
Patent Document 5: WO
Patent Document 6: WO
Patent Document 7: WO 25 Patent Document 8: WO
4

PCT/JP2020/021426
Patent Document 9: WO 2018/109642 pamphlet Patent Document 10: WO 2018/109643 pamphlet Patent Document 11: WO 2018/109646 pamphlet Patent Document 12: WO 2018/109647 pamphlet 5 Patent Document 13: WO 2018/109648 pamphlet Patent Document 14: WO 2018/109649 pamphlet Patent Document 15: WO 2018/181345 pamphlet Patent Document 16: WO 2019/224667 pamphlet Patent Document 17: WO 2020/041169 pamphlet 10 NONPATENT DOCUMENT
[0007]
Nonpatent Document 1: BBA Molecular Cell Research,
2018, 1865, 721-733.
Nonpatent Document 2: American Journal of Nephrology, 15 2018, 47, 40-47.
Nonpatent Document 3: Molecular Pharmacology, 2013,
84, 62-70.
Nonpatent Document 4: Scientific Reports, 2016, 6,
26585. 20 Nonpatent Document 5: The Journal of Pharmacology and
Experimantal Therapeutics, 2017, 363, 114-125.
Nonpatent Document 6: Molecular Cancer Therapeutics,
2014, 13, 12, 2968-2977.
Nonpatent Document 7: Proceeding of the National 25 Academy of Sciences of the United States of America, 2016,
5

PCT/JP2020/021426
113, 17, 4777-4782.
Nonpatent Document 8: Plos One, 2008, 3, 10, e3367.
Nonpatent Document 9: Kidney International, 2013, 84, 1090-1095. 5 Nonpatent Document 10: Oxidative Medicine and Cellular Longevity, 2013, 2013, 104308.
Nonpatent Document 11: Brain Research, 2012, 1446, 109-118.
Nonpatent Document 12: Plos One, 4, 1, e4253. 10 Nonpatent Document 13: Investigative Ophthalmology & Visual Science, 2012, 53, 9, 5806-5813.
Nonpatent Document 14: Genes and Development, 2010, 24, 1045-1058.
Nonpatent Document 15: Journal of Clinical 15 Investigation, 2014, 124, 2, 730-741.
Nonpatent Document 16: Free Radical Biology and Medicine, 2013, 63, 264-273.
Nonpatent Document 17: Journal of Medicinal Chemistry, 2016, 59, 3991-4006. 20 Nonpatent Document 18: Journal of Medicinal Chemistry, 2019, 62, 4683-4702.
SUMMARY OF THE INVENTION PROBLEMS TO BE SOLVED BY INVENTION 25 [0008]
6

PCT/JP2020/021426
The present invention provides novel compounds and pharmaceutical compositions comprising the same useful in the prevention, alleviation, and/or treatment of diseases of which symptoms are improved by the inhibition of Keap1. 5
MEANS TO SOLVE PROBLEMS [0009]
The present inventors have earnestly studied compounds having Keap1 inhibitory activities. As a result, they have
10 found that a series of benzotriazole derivatives having intramolecular tricyclic structures or pharmaceutically acceptable salts thereof has excellent Keap1 inhibitory activities, and is useful in the prevention, alleviation, and/or treatment of diseases of which symptoms are improved
15 by the inhibition of Keap1, especially the prevention, alleviation, and/or treatment of renal diseases, and finally completed the present invention. [0010]
The present invention provides the following [1] to
20 [4].
[1] A compound represented by the following general formula (I):
7

PCT/JP2020/021426


•R (I)

[wherein:
R represents a hydrogen atom or an alkyl group optionally substituted with 1 to 5 substituent(s) 5 independently selected from Group E;
R1 and R2 each independently represent a hydrogen atom, an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an alkenyl group optionally substituted with 1 to 5 10 substituent(s) independently selected from Group E, or an alkynyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
or R1 and R2 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle 15 optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
R3, R4, and R6 each independently represent a hydrogen atom, a halogen atom, an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from 20 Group E, an alkenyl group optionally substituted with 1 to
8

PCT/JP2020/021426
5 substituent(s) independently selected from Group E, an alkynyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an alkoxy group optionally substituted with 1 to 5 5 substituent(s) independently selected from Group E, a cycloalkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, a nonaromatic heterocyclyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E,
10 an aryl group optionally substituted with 1 to 5
substituent(s) independently selected from Group E, a heteroaryl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, or a cyano group;
15 R5 represents (i) a hydrogen atom, or (ii) an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a halogen atom, a hydroxy group, a cycloalkyl group optionally substituted with 1 to 5 substituent(s)
20 independently selected from Group E, a phenyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, and an alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
25 A has a structure represented by the following formula
9

PCT/JP2020/021426 (II)

;
R7 and R8 each independently represent a hydrogen atom, an alkyl group optionally substituted with 1 to 5 5 substituent(s) independently selected from Group E, an alkenyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, or an alkynyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
10 or R7 and R8 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
ring B represents a bicyclic ring optionally
15 substituted with 1 to 5 substituent(s) independently
selected from the group consisting of a halogen atom, an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an alkenyl group optionally substituted with 1 to 5
20 substituent(s) independently selected from Group E, an alkynyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an
10

PCT/JP2020/021426
alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, a cycloalkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, a 5 nonaromatic heterocyclyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an aryl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, a heteroaryl group optionally substituted with 1 to 5 10 substituent(s) independently selected from Group E, and a cyano group;
the symbol
represents the point of attachment to the rest of molecule; 15 and
Group E represents a group consisting of a halogen
atom, a hydroxy group, and an alkoxy group optionally
substituted with 1 to 5 halogen atom(s)]
(hereinafter also referred to as "Compound (I)") or a 20 pharmaceutically acceptable salt thereof.
[2] A pharmaceutical composition comprising the compound
according to [1] or a pharmaceutically acceptable salt
thereof.
[3] The pharmaceutical composition according to [2] for 25 the prevention, alleviation, and/or treatment of a disease
11

PCT/JP2020/021426
which is improved by the inhibition of Keap1.
[4] The pharmaceutical composition according to [3],
wherein the disease which is improved by the inhibition of
Keap1 is a renal disease. 5 [0011]
The present invention also provides the following [5]
to [20].
[5] The compound according to [1] or a pharmaceutically
acceptable salt thereof, wherein 10 R represents a hydrogen atom or an alkyl group
optionally substituted with 1 to 5 substituent(s)
independently selected from Group E;
R1 and R2 each independently represent a hydrogen atom
or an alkyl group optionally substituted with 1 to 5 15 substituent(s) independently selected from Group E;
or R1 and R2 are combined with the carbon atom to
which they are attached to form a monocyclic carbocycle
optionally substituted with 1 to 5 substituent(s)
independently selected from Group E; 20 R3, R4, and R6 each independently represent a hydrogen
atom, a halogen atom, an alkyl group optionally substituted
with 1 to 5 substituent(s) independently selected from
Group E, or an alkoxy group optionally substituted with 1
to 5 substituent(s) independently selected from Group E; 25 R5 represents (i) a hydrogen atom, or (ii) an alkyl
12

PCT/JP2020/021426
group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a halogen atom, a hydroxy group, a phenyl group optionally substituted with 1 to 5 substituent(s) independently 5 selected from Group E, and an alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
R7 and R8 each independently represent a hydrogen atom or an alkyl group optionally substituted with 1 to 5
10 substituent(s) independently selected from Group E;
or R7 and R8 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle optionally substituted with 1 to 5 substituent(s) independently selected from Group E; and
15 ring B represents a bicyclic ring optionally
substituted with 1 to 5 substituent(s) independently selected from the group consisting of a halogen atom, an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an
20 alkoxy group optionally substituted with 1 to 5
substituent(s) independently selected from Group E, and a
cyano group.
[0012]
[6] The compound according to [1] or a pharmaceutically
25 acceptable salt thereof, wherein
13

PCT/JP2020/021426
R represents a hydrogen atom or an alkyl group;
R1 and R2 each independently represent a hydrogen atom or an alkyl group;
or R1 and R2 are combined with the carbon atom to 5 which they are attached to form a monocyclic carbocycle;
R3, R4, and R6 each independently represent a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group;
R5 represents (i) a hydrogen atom, or (ii) an alkyl group optionally substituted with 1 to 5 substituent(s) 10 independently selected from the group consisting of a halogen atom, a hydroxy group, a phenyl group, and an alkoxy group;
R7 and R8 each independently represent a hydrogen atom or an alkyl group; 15 or R7 and R8 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle optionally substituted with 1 to 5 substituent(s) independently selected from Group E; and
ring B represents a bicyclic ring optionally 20 substituted with 1 to 5 substituent(s) independently
selected from the group consisting of a halogen atom, an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an alkoxy group optionally substituted with 1 to 5 25 substituent(s) independently selected from Group E, and a
14

PCT/JP2020/021426
cyano group. [0013]
[7] The compound according to any one of [1] or [5] to [6], wherein 5 The compound has a structure represented by the following general formula (I-1):

R (1-1)
; R represents a hydrogen atom or an alkyl group;
R1 and R2 each independently represent a hydrogen atom
10 or an alkyl group;
or R1 and R2 are combined with the carbon atom to
which they are attached to form a monocyclic carbocycle;
R3 represents a hydrogen atom, a halogen atom, an
alkyl group, or an alkoxy group;
15 R4 and R6 each independently represent a hydrogen
atom, an alkyl group, or an alkoxy group; and
R5 represents a hydrogen atom or an alkyl group
(hereinafter also referred to as "Compound (I-1)") or a
pharmaceutically acceptable salt thereof.
20 [0014]
15

PCT/JP2020/021426
[8] The compound according to any one of [1] or [5] to [7] or a pharmaceutically acceptable salt thereof, wherein
R represents a hydrogen atom;
R1 and R2 each independently represent a hydrogen atom 5 or an alkyl group;
or R1 and R2 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle;
R3 represents an alkyl group;
R4 represents an alkyl group; 10 R5 represents an alkyl group; and
R6 represents a hydrogen atom. [0015]
[8-1] The compound according to [8] or a pharmaceutically acceptable salt thereof, wherein R1 and R2 15 each independently represent a hydrogen atom or an alkyl group. [0016]
[9] The compound according to any one of [1] or [5] to [8-1], wherein 20 A has a structure represented by any one of the following formulae (II-1) to (II-3):
16

PCT/JP2020/021426

R8
R7
O N-
O N-
N-
X2

X1
X1^
D (II-2)

X2
D
X1
(II-3)
(II-1) [wherein:
R7 and R8 each independently represent a hydrogen atom or an alkyl group; 5 or R7 and R8 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
X1 and X2 each independently represent CR9 or a 10 nitrogen atom;
1 an
R9 each independently represents a hydrogen atom, a halogen atom, an alkyl group optionally substituted with to 5 substituent(s) independently selected from Group E, alkoxy group optionally substituted with 1 to 5 15 substituent(s) independently selected from Group E, or a cyano group; and
5
ring D represents a 5 to 6 membered carbocycle or a to 6 membered heterocycle, each of which is optionally substituted with 1 to 5 substituent(s) independently 20 selected from the group consisting of a halogen atom, an
17

PCT/JP2020/021426
alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, and a 5 cyano group]
(hereinafter also referred to as "Compound (II-1) to (II-3)") or a pharmaceutically acceptable salt thereof. [0017]
[10] The compound according to any one of [1] or [5] to 10 [8], wherein
A has a structure represented by any one of the following formulae (II-1-1) to (II-3-4):
18

PCT/JP2020/021426




N-
X2
X2
X2
X1
X1
X1
Y4
Q2
Y2
Z
w
N—

Y 2 Y1 Y (II-1-1)
N—R 7 R8 O'

Y1Z
(II-1-2) R 7 R8
O
N-
A

R8
R7
X2

X1
O
(II-1-3)
R 7 R8
O

XQ3-Q1
(II-1-4) R 7 R8
O
N-




X2
X1
X2
X1
Q1 Q2~Q3
(II-2-4)
;Y1
Z-Y2 (II-2-3)
R8
R8
R7
R7
Q2
X2' Q 1
Z
X1 Y2
X2"' Y 1
"X1
X2 (II-3-4)
(II-3-3)

X2
X1
Y3
Y2;

X2
Y1
(II-2-1) R 7 R8
X1
Y3 Y2
Z Y2=Y1
(II-2-2)
O
N
R 7 R8
O
Y4
Y2-
Y1-X2 X1 Y1
(II-3-2)
(II-3-1)

N-|

[wherein:
R7 and R8 each independently represent a hydrogen atom or an alkyl group; 5 or R7 and R8 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
19

PCT/JP2020/021426
X1 and X2 each independently represent CR9 or a nitrogen atom;
Y1, Y2, Y3, and Y4 each independently represent CR10 or a nitrogen atom; 5 R9 and R10 each independently represent a hydrogen
atom, a halogen atom, an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, or a 10 cyano group;
Q1 and Q2 each independently represent CR11R12, NR13, an oxygen atom, a sulfur atom, SO, or SO2;
R11 and R12 each independently represent a hydrogen atom, a halogen atom, or an alkyl group; 15 R13 each independently represents a hydrogen atom or an alkyl group;
Z represents NR14, an oxygen atom, or a sulfur atom;
R14 represents a hydrogen atom or an alkyl group;
Q3 represents (CU1U2)n; 20 U1 and U2 each independently represent a hydrogen atom, a halogen atom, or an alkyl group; and
n represents 1, 2, or 3] (hereinafter also referred to as "Compound (II-1-1) to (II-3-4)") or a pharmaceutically acceptable salt thereof. 25 [0018]
20

PCT/JP2020/021426
[10-1] The compound according to [10] or a pharmaceutically acceptable salt thereof, wherein Q1 and Q2 each independently represent CR11R12, NR13, or an oxygen atom. 5 [0019]
[10-2] The compound according to [10] or [10-1] or a pharmaceutically acceptable salt thereof, wherein n represents 1 or 2. [0020] 10 [11] The compound according to any one of [10] to [10-2] or a pharmaceutically acceptable salt thereof, wherein
A has a structure represented by any one of the following formula (II-1-1) or (II-3-1):

(11-1-1) (11-3-1)
15 [0021]
[12] The compound according to any one of [1] or [5] to [11] or a pharmaceutically acceptable salt thereof, wherein A has a structure represented by the following formula (II-1-1):
21

PCT/JP2020/021426
YlY2 Y1
(11-1-1)
[wherein:
R7 and R8 each independently represent a hydrogen atom
or an alkyl group;
5 or R7 and R8 are combined with the carbon atom to
which they are attached to form a monocyclic carbocycle; X1 and X2 each independently represent CR9; any one of Y1, Y2, Y3, and Y4 represents a nitrogen atom, and the other three each independently represent 10 CR10;
R9 each represents a hydrogen atom; and R10 each independently represents a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group]. [0022] 15 [12-1] The compound according to [12] or a
pharmaceutically acceptable salt thereof, wherein
R7 and R8 each independently represent a hydrogen atom or an alkyl group; and
R10 each independently represents a hydrogen atom, a 20 halogen atom, or an alkyl group.
22

PCT/JP2020/021426
[0023]
[13] The compound according to any one of [1] or [5] to [11] or a pharmaceutically acceptable salt thereof, wherein A has a structure represented by the following formula 5 (II-3-1):

Y2AX2-X1
(II-3-1)
[wherein:
R7 and R8 each independently represent a hydrogen atom
or an alkyl group;
10 any one of X1 and X2 represents a nitrogen atom, and
the other one represents CR9;
Y1, Y2, Y3, and Y4 each independently represent CR10;
R9 each represents a hydrogen atom; and
R10 each independently represents a hydrogen atom, a 15 halogen atom, or an alkyl group]. [0024]
[14] The compound according to [1] represented by the following general formula (I-1-1):
23

PCT/JP2020/021426


*R


[wherein:
R represents a hydrogen atom or an alkyl group;
R1 and R2 each independently represent a hydrogen atom 5 or an alkyl group;
or R1 and R2 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle;
R3, R4, and R6 each independently represent a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group; 10 R5 represents (i) a hydrogen atom, or (ii) an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a halogen atom, a hydroxy group, a phenyl group, and an alkoxy group; 15 R7 and R8 each independently represent a hydrogen atom or an alkyl group;
or R7 and R8 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle
24

PCT/JP2020/021426
optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
R10 represents a hydrogen atom, a halogen atom, an alkyl group optionally substituted with 1 to 5 5 substituent(s) independently selected from Group E, an alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, or a cyano group; and
Group E represents a group consisting of a halogen 10 atom, a hydroxy group, and an alkoxy group optionally substituted with 1 to 5 halogen atom(s)]
(hereinafter also referred to as "Compound (I-1-1)") or a pharmaceutically acceptable salt thereof. [0025] 15 [15] The compound according to [14] or a pharmaceutically acceptable salt thereof, wherein
R represents a hydrogen atom or an alkyl group;
R1 and R2 each independently represent a hydrogen atom or an alkyl group; 20 or R1 and R2 are combined with the carbon atom to
which they are attached to form a monocyclic carbocycle;
R3 represents a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group;
R4 represents a hydrogen atom or an alkyl group; 25 R5 represents an alkyl group;
25

PCT/JP2020/021426
R6 represents a hydrogen atom;
R7 and R8 each independently represent a hydrogen atom or an alkyl group;
or R7 and R8 are combined with the carbon atom to 5 which they are attached to form a monocyclic carbocycle; and
R10 represents a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group. [0026] 10 [16] The compound according to [1] selected from the group consisting of
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2,2-difluoro-6,7-dihydro-[1,3]dioxolo[4’,5’:4,5]benzo[1,2-f][1,4]oxazepin-8(9H)-15 yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 1-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2,2-difluoro-6,7-dihydro-[1,3]dioxolo[4’,5’:4,5]benzo[1,2-f][1,4]oxazepin-8(9H)-20 yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid
(Example 1-(b), Example 29 (Diastereomer 1), and Example 30 (Diastereomer 2));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-9-ethyl-2,2-difluoro-8,9-dihydro-25 [1,3]dioxolo[4’,5’:3,4]benzo[1,2-f][1,4]oxazepin-7(6H)-26

PCT/JP2020/021426
yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 2-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-9-ethyl-2,2-difluoro-8,9-dihydro-5 [1,3]dioxolo[4’,5’:3,4]benzo[1,2-f][1,4]oxazepin-7(6H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 2-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,5,7,8,9-hexahydro-4H-indeno[5,6-10 f][1,4]oxazepin-4-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 3-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,5,7,8,9-hexahydro-4H-indeno[5,6-f][1,4]oxazepin-4-yl)methyl)-4-methylphenyl)-2,2-15 dimethylpropanoic acid (Example 3-(b), Example 31
(Diastereomer 1), and Example 32 (Diastereomer 2));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,7,8,9,10-hexahydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-20 dimethylpropanoate (Example 4-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,7,8,9,10-hexahydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 4-(b), Example 33 25 (Diastereomer 1), and Example 34 (Diastereomer 2));
27

PCT/JP2020/021426
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4,8,9,10,11-hexahydronaphtho[1,2-f][1,4]oxazepin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 5-(a)); 5 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4,8,9,10,11-hexahydronaphtho[1,2-f][1,4]oxazepin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 5-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-10 yl)-3-(3-(((R)-2-ethyl-2,3,5,8,9,10-hexahydro-4H-indeno[5,4-f][1,4]oxazepin-4-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 6-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,5,8,9,10-hexahydro-4H-indeno[5,4-15 f][1,4]oxazepin-4-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 6-(b), Example 35 (Diastereomer 1), and Example 36 (Diastereomer 2));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,8,9,10,11-hexahydronaphtho[2,1-20 f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 7-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,8,9,10,11-hexahydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-25 dimethylpropanoic acid (Example 7-(b));
28

PCT/JP2020/021426
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 8-(a)); 5 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 8-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-10 yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 9-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-15 4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 9-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-20 dimethylpropanoate (Example 10-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 10-(b), Example 37 (Diastereomer 1), and Example 25 38 (Diastereomer 2));
29

PCT/JP2020/021426
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 11-(a)); 5 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 11-(b), Example 39 (Diastereomer 1), and Example 40 (Diastereomer 2)); 10 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 12-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-15 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 12-(b), Example 41 (Diastereomer 1), and Example 42 (Diastereomer 2));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-20 yl)-3-(3-(((R)-2-ethyl-10-methyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 13-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methyl-2,3-dihydro-[1,4]oxazepino[7,6-25 b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-30

PCT/JP2020/021426
dimethylpropanoic acid (Example 13-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-8-methyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-4(5H)-yl)methyl)-4-5 methylphenyl)-2,2-dimethylpropanoate (Example 14-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-8-methyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 14-(b)); 10 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-1,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 15-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-15 (((R)-8-ethyl-1,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 15-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4-dihydronaphtho[1,2-20 f][1,4]oxazepin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 16-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4-dihydronaphtho[1,2-f][1,4]oxazepin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid 25 (Example 16-(b));
31

PCT/JP2020/021426
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-8,9-dihydro-[1,4]oxazepino[7,6-h]quinolin-10(11H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 17-(a)); 5 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-8,9-dihydro-[1,4]oxazepino[7,6-h]quinolin-10(11H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 17-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-10 yl)-3-(3-(((R)-4-ethyl-3,4-dihydro-[1,4]oxazepino[6,7-f]quinolin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 18-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4-dihydro-[1,4]oxazepino[6,7-f]quinolin-15 2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 18-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4-dihydro-[1,4]oxazepino[7,6-c]quinolin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-20 dimethylpropanoate (Example 19-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4-dihydro-[1,4]oxazepino[7,6-c]quinolin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 19-(b)); 25 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-32

PCT/JP2020/021426
yl)-3-(3-(((R)-7-ethyl-1,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 20-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-5 (((R)-7-ethyl-1,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 20-(b), Example 43 (Diastereomer 1), and Example 44 (Diastereomer 2));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-10 yl)-3-(3-(((R)-7-ethyl-1-methyl-1,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 21-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-7-ethyl-1-methyl-1,7,8,10-tetrahydro-9H-15 [1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 21-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-7-ethyl-2-methyl-2,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-20 2,2-dimethylpropanoate (Example 22-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-7-ethyl-2-methyl-2,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 22-(b)); 25 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-33

PCT/JP2020/021426
(((R)-4-ethyl-1,3,4,9,10,11-hexahydro-2H-pyrimido[1’,2’:1,6]pyrido[2,3-f][1,4]oxazepin-2-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 23); methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-5 yl)-3-(3-(((R)-2-ethyl-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 24-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-10 yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 24-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-15 dimethylpropanoate (Example 25-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 25-(b), Example 45 (Diastereomer 1), and Example 20 46 (Diastereomer 2));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 26-(a)); 25 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-34

PCT/JP2020/021426
(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 26-(b), Example 47 (Diastereomer 1), and Example 48 (Diastereomer 2)); 5 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-h]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 27-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-10 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-h]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 27-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-15 f]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 28-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-f]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid 20 (Example 28-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-7-fluoro-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 49-(a)); 25 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-35

PCT/JP2020/021426
(((R)-2-ethyl-7-fluoro-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 49-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-5 yl)-3-(3-(((R)-8-ethyl-1-methyl-1,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 50-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-1-methyl-1,5,7,8-tetrahydro-6H-10 [1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 50-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-2-methyl-2,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-15 2,2-dimethylpropanoate (Example 51-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-2-methyl-2,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 51-(b)); 20 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-g]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 52-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-25 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-g]isoquinolin-36

PCT/JP2020/021426
4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 52-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]isoquinolin-5 4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 53);
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-7-fluoro-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-10 dimethylpropanoate (Example 54-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-7-fluoro-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 54-(b)); 15 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-f]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 55-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-20 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-f]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid ditrifluoroacetate (Example 55-(b));
ethyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-25 g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)propanoate
37

PCT/JP2020/021426
(Example 56-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)propanoic acid (Example 56-5 (b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((S)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 57-(a)); 10 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((S)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 57-(b), Example 57-(c) (Diastereomer 1), and Example 58 (Diastereomer 2)); 15 methyl 3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoate (Example 59-(a)); 20 3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid (Example 59-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-25 yl)-3-(3-((2,2-dimethyl-2,3-dihydro-[1,4]oxazepino[7,6-38

PCT/JP2020/021426
g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 60-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-((2,2-dimethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-5 4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 60-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2,2-dimethyl-6,7-dihydro-[1,3]dioxolo[4’,5’:4,5]benzo[1,2-f][1,4]oxazepin-8(9H)-10 yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 61-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2,2-dimethyl-6,7-dihydro-[1,3]dioxolo[4’,5’:4,5]benzo[1,2-f][1,4]oxazepin-8(9H)-15 yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 61-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-h]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid 20 (Example 62);
methyl 3-(3-((2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoate (Example 63-(a)); 25 3-(3-((2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-39

PCT/JP2020/021426
4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid (Example 63-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-5 yl)-3-(3-(((R)-6-ethyl-1,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 64-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-1,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-10 f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 64-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-1-methyl-1,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-15 2,2-dimethylpropanoate (Example 65-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-1-methyl-1,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 65-(b)); 20 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2-methyl-2,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 66-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-25 (((R)-6-ethyl-2-methyl-2,6,7,9-tetrahydro-8H-40

PCT/JP2020/021426
[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 66-(b)); methyl 3-(3-(((R)-7-chloro-2-ethyl-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-5 methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoate (Example 67-(a));
3-(3-(((R)-7-chloro-2-ethyl-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-10 dimethylpropanoic acid (Example 67-(b));
methyl 3-(3-(((R)-7-chloro-2-ethyl-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoate (Example 68-(a)); 15 3-(3-(((R)-7-chloro-2-ethyl-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid (Example 68-(b));
3-(3-(((R)-10-chloro-2-ethyl-2,3-dihydro-20 [1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid (Example 69);
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methoxy-2,3-dihydro-25 [1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-41

PCT/JP2020/021426
methylphenyl)-2,2-dimethylpropanoate (Example 70-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methoxy-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-5 dimethylpropanoic acid (Example 70-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 71-(a)); 10 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 71-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-15 yl)-3-(3-(((R)-2-ethyl-2,3-dihydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 72-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-20 (((R)-2-ethyl-2,3-dihydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 72-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,7,8-25 tetrahydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-42

PCT/JP2020/021426
yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 73-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,7,8-tetrahydrothieno[2’,3’:4,5]benzo[1,2-5 f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 73-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-9,9-dioxide-2,3,7,8-tetrahydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-10 yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 74-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-9,9-dioxide-2,3,7,8-tetrahydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-15 yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 74-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethyl-3-(4-methyl-3-(((R)-2-methyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-20 yl)methyl)phenyl)propanoate (Example 75-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethyl-3-(4-methyl-3-(((R)-2-methyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)propanoic acid (Example 75-(b)); 25 methyl 3-(3-((3’H-spiro[cyclopropane-1,2’-43

PCT/JP2020/021426
[1,4]oxazepino[7,6-g]quinoline]-4’(5’H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoate (Example 76-(a));
3-(3-((3’H-spiro[cyclopropane-1,2’-[1,4]oxazepino[7,6-5 g]quinoline]-4’(5’H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid (Example 76-(b), Example 85 (Diastereomer 1), and Example 86 (Diastereomer 2));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-10 yl)-2,2-dimethyl-3-(4-methyl-3-((2-propyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)propanoate (Example 77-(a) and Example 78-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-15 dimethyl-3-(4-methyl-3-((2-propyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)propanoic acid (Example 77-(b) and Example 78-(b));
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-20 yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)-2,2-dimethylpropanoate (Example 79-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-25 4(5H)-yl)methyl)phenyl)-2,2-dimethylpropanoic acid (Example
44

PCT/JP2020/021426
79-(b));
methyl 3-(4-chloro-3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-5 dimethylpropanoate (Example 80-(a));
3-(4-chloro-3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid (Example 80-(b)); 10 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methoxyphenyl)-2,2-dimethylpropanoate (Example 81-(a));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-15 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methoxyphenyl)-2,2-dimethylpropanoic acid (Example 81-(b));
methyl 3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-20 methylphenyl)-2,2-dimethyl-3-(1-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoate (Example 82-(a));
3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethyl-3-(1-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid 25 (Example 82-(b));
45

PCT/JP2020/021426
methyl 1-((1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)methyl)cyclopentane-1-carboxylate (Example 83-5 (a));
1-((1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)methyl)cyclopentane-1-carboxylic acid (Example 83-(b)); 10 methyl 1-((1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)methyl)cyclobutane-1-carboxylate (Example 84-(a)); 15 1-((1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)methyl)cyclobutane-1-carboxylic acid (Example 84-(b), Example 87 (Diastereomer 1), and Example 88 (Diastereomer 2)); 20 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((S)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate (Example 89-(a)); and
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-25 (((S)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]isoquinolin-46

PCT/JP2020/021426
4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 89-(b) (Diastereomer 1) and Example 90 (Diastereomer 2))
or a pharmaceutically acceptable salt thereof. 5 [0027]
[17] The compound according to [1] selected from the group consisting of
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2,2-difluoro-6,7-dihydro-10 [1,3]dioxolo[4’,5’:4,5]benzo[1,2-f][1,4]oxazepin-8(9H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 1-(b), Example 29 (Diastereomer 1), and Example 30 (Diastereomer 2));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-15 (((R)-9-ethyl-2,2-difluoro-8,9-dihydro-[1,3]dioxolo[4’,5’:3,4]benzo[1,2-f][1,4]oxazepin-7(6H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 2-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-20 (((R)-2-ethyl-2,3,5,7,8,9-hexahydro-4H-indeno[5,6-f][1,4]oxazepin-4-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 3-(b), Example 31 (Diastereomer 1), and Example 32 (Diastereomer 2));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-25 (((R)-2-ethyl-2,3,7,8,9,10-hexahydronaphtho[2,3-47

PCT/JP2020/021426
f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 4-(b), Example 33 (Diastereomer 1), and Example 34 (Diastereomer 2));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-5 (((R)-4-ethyl-3,4,8,9,10,11-hexahydronaphtho[1,2-f][1,4]oxazepin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 5-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,5,8,9,10-hexahydro-4H-indeno[5,4-10 f][1,4]oxazepin-4-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 6-(b), Example 35 (Diastereomer 1), and Example 36 (Diastereomer 2));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,8,9,10,11-hexahydronaphtho[2,1-15 f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 7-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid 20 (Example 8-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 9-(b)); 25 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-48

PCT/JP2020/021426
(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 10-(b), Example 37 (Diastereomer 1), and Example 38 (Diastereomer 2)); 5 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 11-(b), Example 39 (Diastereomer 1), and Example 40 (Diastereomer 2)); 10 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 12-(b), Example 41 (Diastereomer 1), and Example 42 (Diastereomer 2)); 15 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 13-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-20 (((R)-2-ethyl-8-methyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 14-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-1,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-25 f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-49

PCT/JP2020/021426
dimethylpropanoic acid (Example 15-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4-dihydronaphtho[1,2-f][1,4]oxazepin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid 5 (Example 16-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-8,9-dihydro-[1,4]oxazepino[7,6-h]quinolin-10(11H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 17-(b)); 10 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4-dihydro-[1,4]oxazepino[6,7-f]quinolin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 18-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-15 (((R)-4-ethyl-3,4-dihydro-[1,4]oxazepino[7,6-c]quinolin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 19-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-7-ethyl-1,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-20 g]indazol-9-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 20-(b), Example 43 (Diastereomer 1), and Example 44 (Diastereomer 2));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-7-ethyl-1-methyl-1,7,8,10-tetrahydro-9H-25 [1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-50

PCT/JP2020/021426
2,2-dimethylpropanoic acid (Example 21-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-7-ethyl-2-methyl-2,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-5 2,2-dimethylpropanoic acid (Example 22-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-1,3,4,9,10,11-hexahydro-2H-pyrimido[1’,2’:1,6]pyrido[2,3-f][1,4]oxazepin-2-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 23); 10 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 24-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-15 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 25-(b), Example 45 (Diastereomer 1), and Example 46 (Diastereomer 2));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-20 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 26-(b), Example 47 (Diastereomer 1), and Example 48 (Diastereomer 2));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-25 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-h]quinolin-51

PCT/JP2020/021426
4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 27-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-f]quinolin-5 4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 28-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-7-fluoro-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-10 dimethylpropanoic acid (Example 49-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-1-methyl-1,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 50-(b)); 15 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-2-methyl-2,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 51-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-20 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-g]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 52-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]isoquinolin-25 4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid
52

PCT/JP2020/021426
(Example 53);
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-7-fluoro-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-5 dimethylpropanoic acid (Example 54-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-f]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid ditrifluoroacetate (Example 55-(b)); 10 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)propanoic acid (Example 56-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-15 (((S)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 57-(b), Example 57-(c) (Diastereomer 1), and Example 58 (Diastereomer 2));
3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-20 g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid (Example 59-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-((2,2-dimethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-25 4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid
53

PCT/JP2020/021426
(Example 60-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2,2-dimethyl-6,7-dihydro-[1,3]dioxolo[4’,5’:4,5]benzo[1,2-f][1,4]oxazepin-8(9H)-5 yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 61-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-h]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid 10 (Example 62);
3-(3-((2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid (Example 63-(b)); 15 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-1,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 64-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-20 (((R)-6-ethyl-1-methyl-1,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 65-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2-methyl-2,6,7,9-tetrahydro-8H-25 [1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-54

PCT/JP2020/021426
2,2-dimethylpropanoic acid (Example 66-(b));
3-(3-(((R)-7-chloro-2-ethyl-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-5 dimethylpropanoic acid (Example 67-(b));
3-(3-(((R)-7-chloro-2-ethyl-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid (Example 68-(b)); 10 3-(3-(((R)-10-chloro-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid (Example 69);
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-15 (((R)-2-ethyl-10-methoxy-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 70-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methyl-2,3-dihydro-[1,4]oxazepino[7,6-20 g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 71-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-25 dimethylpropanoic acid (Example 72-(b));
55

PCT/JP2020/021426
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,7,8-tetrahydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 73-(b)); 5 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-9,9-dioxide-2,3,7,8-tetrahydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid (Example 74-(b)); 10 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethyl-3-(4-methyl-3-(((R)-2-methyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)propanoic acid (Example 75-(b));
3-(3-((3’H-spiro[cyclopropane-1,2’-[1,4]oxazepino[7,6-15 g]quinoline]-4’(5’H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid (Example 76-(b), Example 85 (Diastereomer 1), and Example 86 (Diastereomer 2));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-20 dimethyl-3-(4-methyl-3-((2-propyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)propanoic acid (Example 77-(b) and Example 78-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-25 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-56

PCT/JP2020/021426
4(5H)-yl)methyl)phenyl)-2,2-dimethylpropanoic acid (Example 79-(b));
3-(4-chloro-3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)-3-5 (1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid (Example 80-(b));
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methoxyphenyl)-2,2-dimethylpropanoic 10 acid (Example 81-(b));
3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethyl-3-(1-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid (Example 82-(b)); 15 1-((1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)methyl)cyclopentane-1-carboxylic acid (Example 83-(b));
1-((1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)(3-20 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)methyl)cyclobutane-1-carboxylic acid (Example 84-(b), Example 87 (Diastereomer 1), and Example 88 (Diastereomer 2)); and
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-25 (((S)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]isoquinolin-57

PCT/JP2020/021426
4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid
(Example 89-(b) (Diastereomer 1) and Example 90
(Diastereomer 2))
or a pharmaceutically acceptable salt thereof. 5 [0028]
[18] A pharmaceutical composition comprising the compound
according to any one of [5] to [17] or a pharmaceutically
acceptable salt thereof.
[0029] 10 [19] The pharmaceutical composition according to [18] for
the prevention, alleviation, and/or treatment of a disease
which is improved by the inhibition of Keap1.
[0030]
[20] The pharmaceutical composition according to [19], 15 wherein the disease which is improved by the inhibition of
Keap1 is a renal disease.
EFFECT OF INVENTION [0031]
20 The compounds represented by general formula (I) or pharmaceutically acceptable salts thereof of the present invention have activities for inhibiting Keap1. Accordingly, the compounds represented by general formula (I) or pharmaceutically acceptable salts thereof are useful
25 as agents for the prevention, alleviation, and/or treatment
58

PCT/JP2020/021426
of various diseases of which symptoms are improved by the inhibition of Keap1 such as renal diseases.
MODE FOR CARRYING OUT THE INVENTION 5 [0032]
Embodiments of the present invention are described below. In the present description, "compound represented by general formula (I)" and the like are also conveniently referred to as "Compound (I)" and the like, respectively.
10 Also, the Compound (I) and compounds encompassed by the
Compound (I) such as Compound (I-1), the Compounds (II-1) to (II-3), the Compounds (II-1-1) to (II-3-4), the Compound (I-1-1), and Example compounds are also collectivelly referred to as "Present compound" or "compound of the
15 present invention". Various substituents defined or
illustrated below may be optionally selected and combined with each other. Further, embodiments created by optionally selecting and combining each embodiment defined below are also encompassed by the present invention.
20 [0033]
The definition of each term used in the present description is as follows. [0034]
The term "halogen atom" as described herein refers to
25 a fluorine atom, a chlorine atom, a bromine atom, or an
59

PCT/JP2020/021426
iodine atom. [0035]
The term "alkyl group" as described herein refers to a straight or branched saturated hydrocarbon group having 1 5 to 6 carbon atom(s) (C1-C6) such as 1 to 4 carbon atom(s) (C1-C4), and examples thereof include a methyl group, an ethyl group, a propyl group, an isopropyl group, a n-butyl group, a tert-butyl group, an isobutyl group, a n-pentyl group, a n-hexyl group, and various branched isomers 10 thereof. [0036]
The term "alkenyl group" as described herein refers to a straight or branched unsaturated hydrocarbon group having one carbon-carbon double bond and 2 to 6 carbon atoms (C2 15 to C6) such as 2 to 4 carbon atoms (C2 to C4), and examples thereof include a vinyl group, a propenyl group, an isopropenyl group, a butenyl group, and various branched isomers thereof. [0037] 20 The term "alkynyl group" as described herein refers to a straight or branched unsaturated hydrocarbon group having one carbon-carbon triple bond and 2 to 6 carbon atoms (C2 to C6) such as 2 to 4 carbon atoms (C2 to C4), and examples thereof include an ethynyl group, a 1-propynyl group, a 2-25 butynyl group, a 4-pentynyl group, a 5-hexynyl group, and
60

PCT/JP2020/021426
various branched isomers thereof. [0038]
The term "alkoxy group" as described herein refers to a group in which an oxygen atom is bound to the above 5 straight or branched alkyl group, and examples thereof
include a methoxy group, an ethoxy group, a propoxy group, an isopropoxy group, a butoxy group, a tert-butoxy group, an isobutoxy group, and various branched isomers thereof. [0039]
10 The term "cycloalkyl group" as described herein refers to a monocyclic alicyclic saturated hydrocarbon group having 3 to 8 ring-constituting carbon atoms (C3 to C8) such as 3 to 6 ring-constituting carbon atoms (C3 to C6), and examples thereof include a cyclopropyl group, a
15 cyclobutyl group, a cyclopentyl group, a cyclohexyl group, a cycloheptyl group, and a cyclooctyl group. [0040]
The term "nonaromatic heterocyclyl group" as described herein refers to a 4 to 8 membered monocyclic nonaromatic
20 heterocyclic group or a 6 to 12 membered bicyclic nonaromatic heterocyclic group comprising 1 to 4 heteroatom(s) selected from an oxygen atom, a sulfur atom, and a nitrogen atom other than carbon atom(s), and examples thereof include an azetidinyl group, an oxetanyl group, a
25 thietanyl group, a pyrrolidinyl group, a piperidinyl group,
61

PCT/JP2020/021426
a piperidino group, a tetrahydrofuryl group, a tetrahydropyranyl group, a tetrahydrothienyl group (i.e., a thiolanyl group), a piperazinyl group, a morpholinyl group, a morpholino group, a perhydroazepinyl group, a 5 perhydroazocinyl group, 6 to 12 membered azabicycloalkyl groups (for example, an azabicyclohexyl group, an azabicycloheptyl group, an azabicyclooctyl group, an azabicyclononyl group, an azabicyclodecyl group, an azabicycloundecyl group, or an azabicyclododecyl group), 6
10 to 12 membered azabicycloalkenyl groups (for example, an azabicyclohexenyl group, an azabicycloheptenyl group, an azabicyclooctenyl group, an azabicyclononenyl group, an azabicyclodecenyl group, an azabicycloundecenyl group, or an azabicyclododecenyl group), and 6 to 12 membered
15 azaspiroalkyl groups (for example, an azaspirohexyl group, an azaspiroheptyl group, an azaspirooctyl group, an azaspirononyl group, an azaspirodecyl group, an azaspiroundecyl group, or an azaspirododecyl group). [0041]
20 The term "aryl group" as described herein refers to a monocyclic or bicyclic aromatic hydrocarbon group having 6 to 11 ring-constituting carbon atoms (C6 to C11), and examples thereof include monocyclic aryl groups such as a phenyl group; and optionally partially saturated bicyclic
25 aryl groups hsving 9 to 11 ring-constituting carbon atoms
62

PCT/JP2020/021426
(C9 to C11) such as a naphthyl group, a tetrahydronaphthyl
group, an indenyl group, and indanyl group.
[0042]
The term "heteroaryl group" as described herein refers 5 to a 5 to 11 membered monocyclic or bicyclic aromatic
heterocyclic group comprising 1 to 4 heteroatom(s) selected from an oxygen atom, a sulfur atom, and a nitrogen atom other than carbon atom(s), and examples thereof include 5 to 6 membered monocyclic heteroaryl groups comprising 1 to
10 4 heteroatom(s) selected from an oxygen atom, a sulfur
atom, and a nitrogen atom other than carbon atom(s) such as a pyrrolyl group, a furyl group, a thienyl group, a pyrazolyl group, an imidazolyl group, an oxazolyl group, an isoxazolyl group, a thiazolyl group, an isothiazolyl group,
15 a thiadiazolyl group, a pyridyl group, a pyrazinyl group, a pyrimidinyl group, a pyridazinyl group, and a triazinyl group; and 8 to 11 membered bicyclic heteroaryl groups comprising 1 to 4 heteroatom(s) selected from an oxygen atom, a sulfur atom, and a nitrogen atom other than carbon
20 atom(s) such as an indolyl group, an indolinyl group, an isoindolinyl group, an indazolyl group, a tetrahydroindazolyl group, a benzofuranyl group, a dihydrobenzofuranyl group, a dihydroisobenzofuranyl group, a benzothiophenyl group, a dihydrobenzothiophenyl group, a
25 dihydroisobenzothiophenyl group, a benzoxazolyl group, a
63

PCT/JP2020/021426
dihydrobenzoxazolyl group, a benzothiazolyl group, a dihydrobenzothiazolyl group, a quinolyl group, a tetrahydroquinolyl group, an isoquinolyl group, a tetrahydroisoquinolyl group, a naphthyridinyl group, a 5 tetrahydronaphthyridinyl group, a quinoxalinyl group, a tetrahydroquinoxalinyl group, and a quinazolinyl group. [0043]
The term "monocyclic carbocycle" as described herein refers to a saturated or unsaturated monocyclic hydrocarbon
10 ring such as one formed by combining R1 and R2 or R7 and R8 with the carbon atom to which they are attached in a group represented by >CR1R2 or >CR7R8 (wherein R1, R2, R7, and R8 have the same meanings as those described above). The number of ring-constituting carbon atoms is 3 to 8 (C3-C8)
15 such as 3 to 6 (C3-C6). [0044]
The term "bicyclic ring" as described herein refers to a saturated or unsaturated 6 to 12 membered, for example 9 to 10 membered bicyclic ring optionally comprising 1 to 4
20 heteroatom(s) selected from an oxygen atom, a sulfur atom, and a nitrogen atom other than carbon atom(s), and examples thereof include the following rings formed by ring C and ring D.
64

PCT/JP2020/021426

When the bicyclic ring in ring B of the Compound (I) is the above ring formed by ring C and ring D, the ring B is attached to the oxazepine ring at the ring C moiety. 5 [0045]
The term "5 to 6 membered carbocycle" as described herein refers to a 5 or 6 membered monocyclic carbocycle, and examples thereof include a ring D in the above "bicyclic ring" which does not comprise a heteroatom. 10 [0046]
The term "5 to 6 membered heterocycle" as described herein refers to a 5 or 6 membered monocyclic heterocycle comprising 1 to 4 heteroatom(s) selected from an oxygen atom, a sulfur atom, and a nitrogen atom other than carbon 15 atom(s), and examples thereof include a ring D in the above "bicyclic ring" which comprises heteroatom(s). [0047]
Hereinafter, embodiments of each substituent of the Compound (I) are described. Further, embodiments created 20 by optionally selecting and combining each embodiment of
the following each substituent are also encompassed by the
65

PCT/JP2020/021426
present invention. [0048]
(Embodiment 1) The compound according to any one of the Present compounds or a pharmaceutically acceptable salt 5 thereof, wherein R represents a hydrogen atom or an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E.
(Embodiment 2) The compound according to any one of the Present compounds or a pharmaceutically acceptable salt
10 thereof, wherein R represents a hydrogen atom or an alkyl group optionally substituted with 1 to 5 halogen atom(s). (Embodiment 3) The compound according to any one of the Present compounds or a pharmaceutically acceptable salt thereof, wherein R represents a hydrogen atom or an alkyl
15 group.

WE CLAIMS

A compound represented by the following general formula (I):

R5

R6

N/N"lfn R1 R2 XNN^k^YX^O^R (I)
O

5
R3
[wherein:
R represents a hydrogen atom or an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
10 R1 and R2 each independently represent a hydrogen atom, an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an alkenyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, or an
15 alkynyl group optionally substituted with 1 to 5
substituent(s) independently selected from Group E;
or R1 and R2 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle optionally substituted with 1 to 5 substituent(s)
20 independently selected from Group E;
699

PCT/JP2020/021426
R3, R4, and R6 each independently represent a hydrogen atom, a halogen atom, an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an alkenyl group optionally substituted with 1 to 5 5 substituent(s) independently selected from Group E, an alkynyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, a
10 cycloalkyl group optionally substituted with 1 to 5
substituent(s) independently selected from Group E, a nonaromatic heterocyclyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an aryl group optionally substituted with 1 to 5
15 substituent(s) independently selected from Group E, a heteroaryl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, or a cyano group;
R5 represents (i) a hydrogen atom, or (ii) an alkyl
20 group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a halogen atom, a hydroxy group, a cycloalkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, a phenyl group
25 optionally substituted with 1 to 5 substituent(s)
700

PCT/JP2020/021426
independently selected from Group E, and an alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
A has a structure represented by the following formula 5 (II)

R7

R8

%
O N-\ (II)
BJ
R7 and R8 each independently represent a hydrogen atom, an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an
10 alkenyl group optionally substituted with 1 to 5
substituent(s) independently selected from Group E, or an alkynyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
or R7 and R8 are combined with the carbon atom to
15 which they are attached to form a monocyclic carbocycle optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
ring B represents a bicyclic ring optionally substituted with 1 to 5 substituent(s) independently
20 selected from the group consisting of a halogen atom, an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an
701

PCT/JP2020/021426
alkenyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an alkynyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an 5 alkoxy group optionally substituted with 1 to 5
substituent(s) independently selected from Group E, a cycloalkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, a nonaromatic heterocyclyl group optionally substituted with
10 1 to 5 substituent(s) independently selected from Group E, an aryl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, a heteroaryl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, and a
15 cyano group;
the symbol
SXAAAAA/t
represents the point of attachment to the rest of molecule;
and
20 Group E represents a group consisting of a halogen
atom, a hydroxy group, and an alkoxy group optionally substituted with 1 to 5 halogen atom(s)] or a pharmaceutically acceptable salt thereof.
25 2. The compound according to claim 1 or a
702

PCT/JP2020/021426
pharmaceutically acceptable salt thereof, wherein
R represents a hydrogen atom or an alkyl group
optionally substituted with 1 to 5 substituent(s)
independently selected from Group E; 5 R1 and R2 each independently represent a hydrogen atom
or an alkyl group optionally substituted with 1 to 5
substituent(s) independently selected from Group E;
or R1 and R2 are combined with the carbon atom to
which they are attached to form a monocyclic carbocycle 10 optionally substituted with 1 to 5 substituent(s)
independently selected from Group E;
R3, R4, and R6 each independently represent a hydrogen
atom, a halogen atom, an alkyl group optionally substituted
with 1 to 5 substituent(s) independently selected from 15 Group E, or an alkoxy group optionally substituted with 1
to 5 substituent(s) independently selected from Group E; R5 represents (i) a hydrogen atom, or (ii) an alkyl
group optionally substituted with 1 to 5 substituent(s)
independently selected from the group consisting of a 20 halogen atom, a hydroxy group, a phenyl group optionally
substituted with 1 to 5 substituent(s) independently
selected from Group E, and an alkoxy group optionally
substituted with 1 to 5 substituent(s) independently
selected from Group E; 25 R7 and R8 each independently represent a hydrogen atom
703

PCT/JP2020/021426
or an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
or R7 and R8 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle 5 optionally substituted with 1 to 5 substituent(s) independently selected from Group E; and
ring B represents a bicyclic ring optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a halogen atom, an 10 alkyl group optionally substituted with 1 to 5
substituent(s) independently selected from Group E, an alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, and a cyano group. 15
3. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein
R represents a hydrogen atom or an alkyl group;
R1 and R2 each independently represent a hydrogen atom 20 or an alkyl group;
or R1 and R2 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle;
R3, R4, and R6 each independently represent a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group; 25 R5 represents (i) a hydrogen atom, or (ii) an alkyl
704

PCT/JP2020/021426
group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a halogen atom, a hydroxy group, a phenyl group, and an alkoxy group; 5 R7 and R8 each independently represent a hydrogen atom or an alkyl group;
or R7 and R8 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle optionally substituted with 1 to 5 substituent(s)
10 independently selected from Group E; and
ring B represents a bicyclic ring optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a halogen atom, an alkyl group optionally substituted with 1 to 5
15 substituent(s) independently selected from Group E, an alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, and a cyano group.
20 4. The compound according to any one of claims 1 to 3 or a pharmaceutically acceptable salt thereof, wherein
The compound has a structure represented by the following general formula (I-1):
705

PCT/JP2020/021426

R (1-1)
; R represents a hydrogen atom or an alkyl group;
R1 and R2 each independently represent a hydrogen atom
or an alkyl group;
5 or R1 and R2 are combined with the carbon atom to
which they are attached to form a monocyclic carbocycle;
R3 represents a hydrogen atom, a halogen atom, an
alkyl group, or an alkoxy group;
R4 and R6 each independently represent a hydrogen
10 atom, an alkyl group, or an alkoxy group; and
R5 represents a hydrogen atom or an alkyl group.
5. The compound according to any one of claims 1 to 4 or a pharmaceutically acceptable salt thereof, wherein 15 R represents a hydrogen atom;
R1 and R2 each independently represent a hydrogen atom or an alkyl group;
or R1 and R2 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle; 20 R3 represents an alkyl group;
706

PCT/JP2020/021426

5

R4 represents an alkyl group;
R5 represents an alkyl group; and
R6 represents a hydrogen atom.
6. The compound according to any one of claims 1 to 5 or a pharmaceutically acceptable salt thereof, wherein
A has a structure represented by any one of the following formulae (II-1) to (II-3):


O
O'
10
15
20

N-
N-

X2
N-
'-X1
D (II-2)

X2
D
X1
(II-3)
(II-1) [wherein:
R7 and R8 each independently represent a hydrogen atom or an alkyl group;
or R7 and R8 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
X1 and X2 each independently represent CR9 or a nitrogen atom;
R9 each independently represents a hydrogen atom, a halogen atom, an alkyl group optionally substituted with 1

707

PCT/JP2020/021426
to 5 substituent(s) independently selected from Group E, an alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, or a cyano group; and 5 ring D represents a 5 to 6 membered carbocycle or a 5 to 6 membered heterocycle, each of which is optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a halogen atom, an alkyl group optionally substituted with 1 to 5 10 substituent(s) independently selected from Group E, an alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, and a cyano group].
15 7. The compound according to any one of claims 1 to 5 or a pharmaceutically acceptable salt thereof, wherein
A has a structure represented by any one of the following formulae (II-1-1) to (II-3-4):
708

PCT/JP2020/021426


X2
X2
X
X1
X1
Y4
Z
Y2

Y (II-1-1)

Y1 Z
(II-1-2)

R 7 R8 O
X1
(II-1-3)

N—
R>R
X2
Q2 X1
Q3-Q1
(II-1-4)


R 7 R8 O'

N—
O

N-

A

O

N-A

R 7 R8
O

N—


X2
X1
Z
(II-2-2)
R 7 R8
R8
N-l
1 Y Y
,X1
-X2
(II-3-2)

X2
X1
Y3
Y2,

Y1
Y4 Y3 Y2
!Y
(II-2-1) R 7 R8
O
Y4
X1
Y1^X2' (II-3-1)

N-

Y2
X2 X1
Y1
Z

X2
•Q1 Q2-Q3
(II-2-4)
X1
Y1 Z-Y'2
(II-2-3)
R7>
R 7 R8
O
Q2
~X2'X
(II-3-3) (II-3-4)

N-f

[wherein:
R7 and R8 each independently represent a hydrogen atom or an alkyl group; 5 or R7 and R8 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
709

PCT/JP2020/021426
X1 and X2 each independently represent CR9 or a nitrogen atom;
Y1, Y2, Y3, and Y4 each independently represent CR10 or a nitrogen atom; 5 R9 and R10 each independently represent a hydrogen
atom, a halogen atom, an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, an alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, or a 10 cyano group;
Q1 and Q2 each independently represent CR11R12, NR13, an oxygen atom, a sulfur atom, SO, or SO2;
R11 and R12 each independently represent a hydrogen atom, a halogen atom, or an alkyl group; 15 R13 each independently represents a hydrogen atom or an alkyl group;
Z represents NR14, an oxygen atom, or a sulfur atom;
R14 represents a hydrogen atom or an alkyl group;
Q3 represents (CU1U2)n; 20 U1 and U2 each independently represent a hydrogen atom, a halogen atom, or an alkyl group; and
n represents 1, 2, or 3].
8. The compound according to any one of claims 1 to 7 or 25 a pharmaceutically acceptable salt thereof, wherein
710

PCT/JP2020/021426
A has a structure represented by the following formula (II-1-1):



X2
X1
Y4
Y (11-1-1)
[wherein:
5 R7 and R8 each independently represent a hydrogen atom
or an alkyl group;
or R7 and R8 are combined with the carbon atom to
which they are attached to form a monocyclic carbocycle;
X1 and X2 each independently represent CR9;
10 any one of Y1, Y2, Y3, and Y4 represents a nitrogen
atom, and the other three each independently represent
CR10;
R9 each represents a hydrogen atom; and R10 each independently represents a hydrogen atom, a 15 halogen atom, an alkyl group, or an alkoxy group].
9. The compound according to claim 1 represented by the following general formula (I-1-1):
711


PCT/JP2020/021426
7 R8

[wherein:
R represents a hydrogen atom or an alkyl group;
R1 and R2 each independently represent a hydrogen atom 5 or an alkyl group;
or R1 and R2 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle;
R3, R4, and R6 each independently represent a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group; 10 R5 represents (i) a hydrogen atom, or (ii) an alkyl group optionally substituted with 1 to 5 substituent(s) independently selected from the group consisting of a halogen atom, a hydroxy group, a phenyl group, and an alkoxy group; 15 R7 and R8 each independently represent a hydrogen atom or an alkyl group;
or R7 and R8 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle
712

PCT/JP2020/021426
optionally substituted with 1 to 5 substituent(s) independently selected from Group E;
R10 represents a hydrogen atom, a halogen atom, an alkyl group optionally substituted with 1 to 5 5 substituent(s) independently selected from Group E, an alkoxy group optionally substituted with 1 to 5 substituent(s) independently selected from Group E, or a cyano group; and
Group E represents a group consisting of a halogen 10 atom, a hydroxy group, and an alkoxy group optionally substituted with 1 to 5 halogen atom(s)] or a pharmaceutically acceptable salt thereof.
10. The compound according to claim 9 or a 15 pharmaceutically acceptable salt thereof, wherein
R represents a hydrogen atom or an alkyl group; R1 and R2 each independently represent a hydrogen atom or an alkyl group;
or R1 and R2 are combined with the carbon atom to 20 which they are attached to form a monocyclic carbocycle; R3 represents a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group;
R4 represents a hydrogen atom or an alkyl group; R5 represents an alkyl group; 25 R6 represents a hydrogen atom;
713

PCT/JP2020/021426
R7 and R8 each independently represent a hydrogen atom or an alkyl group;
or R7 and R8 are combined with the carbon atom to which they are attached to form a monocyclic carbocycle; 5 and
R10 represents a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group.
11. The compound according to claim 1 selected from the 10 group consisting of
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2,2-difluoro-6,7-dihydro-[1,3]dioxolo[4’,5’:4,5]benzo[1,2-f][1,4]oxazepin-8(9H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate; 15 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2,2-difluoro-6,7-dihydro-[1,3]dioxolo[4’,5’:4,5]benzo[1,2-f][1,4]oxazepin-8(9H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-20 yl)-3-(3-(((R)-9-ethyl-2,2-difluoro-8,9-dihydro-[1,3]dioxolo[4’,5’:3,4]benzo[1,2-f][1,4]oxazepin-7(6H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-9-ethyl-2,2-difluoro-8,9-dihydro-25 [1,3]dioxolo[4’,5’:3,4]benzo[1,2-f][1,4]oxazepin-7(6H)-714

PCT/JP2020/021426
yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,5,7,8,9-hexahydro-4H-indeno[5,6-f][1,4]oxazepin-4-yl)methyl)-4-methylphenyl)-2,2-5 dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,5,7,8,9-hexahydro-4H-indeno[5,6-f][1,4]oxazepin-4-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 10 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,7,8,9,10-hexahydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-15 (((R)-2-ethyl-2,3,7,8,9,10-hexahydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4,8,9,10,11-hexahydronaphtho[1,2-20 f][1,4]oxazepin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4,8,9,10,11-hexahydronaphtho[1,2-f][1,4]oxazepin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-25 dimethylpropanoic acid;
715

PCT/JP2020/021426
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,5,8,9,10-hexahydro-4H-indeno[5,4-f][1,4]oxazepin-4-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate; 5 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,5,8,9,10-hexahydro-4H-indeno[5,4-f][1,4]oxazepin-4-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-10 yl)-3-(3-(((R)-2-ethyl-2,3,8,9,10,11-hexahydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,8,9,10,11-hexahydronaphtho[2,1-15 f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-20 dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-25 yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-716

PCT/JP2020/021426
b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-5 4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-10 dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 15 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-20 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-25 g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-717

PCT/JP2020/021426
dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic 5 acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate; 10 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-15 yl)-3-(3-(((R)-2-ethyl-8-methyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-8-methyl-2,3-dihydro-[1,4]oxazepino[7,6-20 b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-1,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-25 2,2-dimethylpropanoate;
718

PCT/JP2020/021426
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-1,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 5 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4-dihydronaphtho[1,2-f][1,4]oxazepin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-10 (((R)-4-ethyl-3,4-dihydronaphtho[1,2-f][1,4]oxazepin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-8,9-dihydro-[1,4]oxazepino[7,6-h]quinolin-10(11H)-yl)methyl)-4-methylphenyl)-2,2-15 dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-8,9-dihydro-[1,4]oxazepino[7,6-h]quinolin-10(11H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 20 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4-dihydro-[1,4]oxazepino[6,7-f]quinolin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-25 (((R)-4-ethyl-3,4-dihydro-[1,4]oxazepino[6,7-f]quinolin-719

PCT/JP2020/021426
2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4-dihydro-[1,4]oxazepino[7,6-5 c]quinolin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4-dihydro-[1,4]oxazepino[7,6-c]quinolin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic 10 acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-7-ethyl-1,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate; 15 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-7-ethyl-1,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-20 yl)-3-(3-(((R)-7-ethyl-1-methyl-1,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-7-ethyl-1-methyl-1,7,8,10-tetrahydro-9H-25 [1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-720

PCT/JP2020/021426
2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-7-ethyl-2-methyl-2,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-5 2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-7-ethyl-2-methyl-2,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 10 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-1,3,4,9,10,11-hexahydro-2H-pyrimido[1’,2’:1,6]pyrido[2,3-f][1,4]oxazepin-2-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-15 yl)-3-(3-(((R)-2-ethyl-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-20 yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate; 25 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-721

PCT/JP2020/021426
(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-5 yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]quinolin-10 4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-h]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-15 dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-h]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 20 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-f]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-25 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-f]quinolin-722

PCT/JP2020/021426
4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-7-fluoro-2,3-dihydronaphtho[2,1-5 f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-7-fluoro-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-10 dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-1-methyl-1,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate; 15 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-1-methyl-1,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-20 yl)-3-(3-(((R)-8-ethyl-2-methyl-2,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-2-methyl-2,5,7,8-tetrahydro-6H-25 [1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-723

PCT/JP2020/021426
2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-g]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-5 dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-g]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 10 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-15 yl)-3-(3-(((R)-2-ethyl-7-fluoro-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-7-fluoro-2,3-dihydronaphtho[2,3-20 f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-f]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-25 dimethylpropanoate;
724

PCT/JP2020/021426
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-f]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid ditrifluoroacetate; 5 ethyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)propanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-10 4(5H)-yl)methyl)-4-methylphenyl)propanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((S)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate; 15 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((S)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(3-(((R)-2-ethyl-2,3-dihydro-20 [1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoate;
3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-25 methyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-725

PCT/JP2020/021426
dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-((2,2-dimethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-5 dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-((2,2-dimethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 10 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2,2-dimethyl-6,7-dihydro-[1,3]dioxolo[4’,5’:4,5]benzo[1,2-f][1,4]oxazepin-8(9H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-15 (((R)-6-ethyl-2,2-dimethyl-6,7-dihydro-[1,3]dioxolo[4’,5’:4,5]benzo[1,2-f][1,4]oxazepin-8(9H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-h]isoquinolin-20 4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(3-((2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-25 dimethylpropanoate;
726

PCT/JP2020/021426
3-(3-((2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid; methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-5 yl)-3-(3-(((R)-6-ethyl-1,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-1,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-10 f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-1-methyl-1,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-15 2,2-dimethylpropanoate);
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-1-methyl-1,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 20 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2-methyl-2,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-25 (((R)-6-ethyl-2-methyl-2,6,7,9-tetrahydro-8H-727

PCT/JP2020/021426
[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(3-(((R)-7-chloro-2-ethyl-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-5 methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoate;
3-(3-(((R)-7-chloro-2-ethyl-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-10 dimethylpropanoic acid;
methyl 3-(3-(((R)-7-chloro-2-ethyl-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoate; 15 3-(3-(((R)-7-chloro-2-ethyl-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid;
3-(3-(((R)-10-chloro-2-ethyl-2,3-dihydro-20 [1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methoxy-2,3-dihydro-25 [1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-728

PCT/JP2020/021426
methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methoxy-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-5 dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate; 10 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-15 yl)-3-(3-(((R)-2-ethyl-2,3-dihydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydrothieno[2’,3’:4,5]benzo[1,2-20 f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,7,8-tetrahydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-25 yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
729

PCT/JP2020/021426
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,7,8-tetrahydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 5 methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-9,9-dioxide-2,3,7,8-tetrahydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-10 (((R)-2-ethyl-9,9-dioxide-2,3,7,8-tetrahydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethyl-3-(4-methyl-3-(((R)-2-methyl-2,3-dihydro-15 [1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)propanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethyl-3-(4-methyl-3-(((R)-2-methyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-20 yl)methyl)phenyl)propanoic acid;
methyl 3-(3-((3’H-spiro[cyclopropane-1,2’-[1,4]oxazepino[7,6-g]quinoline]-4’(5’H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoate; 25 3-(3-((3’H-spiro[cyclopropane-1,2’-[1,4]oxazepino[7,6-730

PCT/JP2020/021426
g]quinoline]-4’(5’H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-5 yl)-2,2-dimethyl-3-(4-methyl-3-((2-propyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)propanoate;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethyl-3-(4-methyl-3-((2-propyl-2,3-dihydro-10 [1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)propanoic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)-2,2-dimethylpropanoate; 15 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)-2,2-dimethylpropanoic acid;
methyl 3-(4-chloro-3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)-3-20 (1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoate;
3-(4-chloro-3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-25 dimethylpropanoic acid;
731

PCT/JP2020/021426
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methoxyphenyl)-2,2-dimethylpropanoate; 5 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methoxyphenyl)-2,2-dimethylpropanoic acid;
methyl 3-(3-(((R)-2-ethyl-2,3-dihydro-10 [1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethyl-3-(1-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoate;
3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethyl-3-15 (1-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid; methyl 1-((1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)methyl)cyclopentane-1-carboxylate; 20 1-((1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)methyl)cyclopentane-1-carboxylic acid;
methyl 1-((1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-25 yl)(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-732

PCT/JP2020/021426
g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)methyl)cyclobutane-1-carboxylate;
1-((1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-5 4(5H)-yl)methyl)-4-methylphenyl)methyl)cyclobutane-1-carboxylic acid;
methyl 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((S)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-10 dimethylpropanoate; and
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((S)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid or a pharmaceutically acceptable salt thereof. 15
12. The compound according to claim 1 selected from the group consisting of
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2,2-difluoro-6,7-dihydro-20 [1,3]dioxolo[4’,5’:4,5]benzo[1,2-f][1,4]oxazepin-8(9H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-9-ethyl-2,2-difluoro-8,9-dihydro-[1,3]dioxolo[4’,5’:3,4]benzo[1,2-f][1,4]oxazepin-7(6H)-25 yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
733

PCT/JP2020/021426
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-
(((R)-2-ethyl-2,3,5,7,8,9-hexahydro-4H-indeno[5,6-
f][1,4]oxazepin-4-yl)methyl)-4-methylphenyl)-2,2-
dimethylpropanoic acid;
5 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-
(((R)-2-ethyl-2,3,7,8,9,10-hexahydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-10 (((R)-4-ethyl-3,4,8,9,10,11-hexahydronaphtho[1,2-
f][1,4]oxazepin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,5,8,9,10-hexahydro-4H-indeno[5,4-15 f][1,4]oxazepin-4-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,8,9,10,11-hexahydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-20 dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-25 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-
734

PCT/JP2020/021426
4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-b]quinolin-5 4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic 10 acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 15 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-20 (((R)-2-ethyl-8-methyl-2,3-dihydro-[1,4]oxazepino[7,6-b]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-1,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-25 f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-735

PCT/JP2020/021426
dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4-dihydronaphtho[1,2-f][1,4]oxazepin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 5 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-8,9-dihydro-[1,4]oxazepino[7,6-h]quinolin-10(11H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-10 (((R)-4-ethyl-3,4-dihydro-[1,4]oxazepino[6,7-f]quinolin-2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-4-ethyl-3,4-dihydro-[1,4]oxazepino[7,6-c]quinolin-15 2(1H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-7-ethyl-1,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-2,2-20 dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-7-ethyl-1-methyl-1,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 25 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-736

PCT/JP2020/021426
(((R)-7-ethyl-2-methyl-2,7,8,10-tetrahydro-9H-[1,4]oxazepino[7,6-g]indazol-9-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-5 (((R)-4-ethyl-1,3,4,9,10,11-hexahydro-2H-pyrimido[1’,2’:1,6]pyrido[2,3-f][1,4]oxazepin-2-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-10 yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 15 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-20 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-h]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-f]quinolin-25 4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic
737

PCT/JP2020/021426
acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-7-fluoro-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-5 dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-1-methyl-1,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 10 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-8-ethyl-2-methyl-2,5,7,8-tetrahydro-6H-[1,4]oxazepino[6,7-f]indazol-6-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-15 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-g]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]isoquinolin-20 4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-7-fluoro-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-25 dimethylpropanoic acid;
738

PCT/JP2020/021426
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-f]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid ditrifluoroacetate; 5 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)propanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((S)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-10 4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-15 dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-((2,2-dimethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 20 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-2,2-dimethyl-6,7-dihydro-[1,3]dioxolo[4’,5’:4,5]benzo[1,2-f][1,4]oxazepin-8(9H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-25 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-h]isoquinolin-739

PCT/JP2020/021426
4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(3-((2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-5 benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-1,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 10 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-6-ethyl-1-methyl-1,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-15 (((R)-6-ethyl-2-methyl-2,6,7,9-tetrahydro-8H-[1,4]oxazepino[7,6-f]indazol-8-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(3-(((R)-7-chloro-2-ethyl-2,3-dihydronaphtho[2,1-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-20 dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid;
3-(3-(((R)-7-chloro-2-ethyl-2,3-dihydronaphtho[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-25 dimethylpropanoic acid;
740

PCT/JP2020/021426
3-(3-(((R)-10-chloro-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid; 5 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-10-methoxy-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-10 (((R)-2-ethyl-10-methyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydrothieno[2’,3’:4,5]benzo[1,2-15 f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3,7,8-tetrahydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-20 dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-9,9-dioxide-2,3,7,8-tetrahydrothieno[2’,3’:4,5]benzo[1,2-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid; 25 3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-741

PCT/JP2020/021426
dimethyl-3-(4-methyl-3-(((R)-2-methyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)propanoic acid;
3-(3-((3’H-spiro[cyclopropane-1,2’-[1,4]oxazepino[7,6-5 g]quinoline]-4’(5’H)-yl)methyl)-4-methylphenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethyl-3-(4-methyl-3-((2-propyl-2,3-dihydro-10 [1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)propanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)-2,2-dimethylpropanoic acid; 15 3-(4-chloro-3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)phenyl)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-2,2-dimethylpropanoic acid;
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-20 (((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methoxyphenyl)-2,2-dimethylpropanoic acid;
3-(3-(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethyl-3-25 (1-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid;
742

PCT/JP2020/021426
1-((1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)(3-
(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-
4(5H)-yl)methyl)-4-methylphenyl)methyl)cyclopentane-1-
carboxylic acid;
5 1-((1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)(3-
(((R)-2-ethyl-2,3-dihydro-[1,4]oxazepino[7,6-g]quinolin-4(5H)-yl)methyl)-4-methylphenyl)methyl)cyclobutane-1-carboxylic acid; and
3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-10 (((S)-2-ethyl-2,3-dihydro-[1,4]oxazepino[6,7-c]isoquinolin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpropanoic acid or a pharmaceutically acceptable salt thereof.
13. A pharmaceutical composition comprising the compound
15 according to any one of claims 1 to 12 or a
pharmaceutically acceptable salt thereof.
14. The pharmaceutical composition according to claim 13
for the prevention, alleviation, and/or treatment of a
20 disease which is improved by the inhibition of Keap1.
15. The pharmaceutical composition according to claim 14
wherein the disease which is improved by the inhibition of
Keap1 is a renal disease.

Documents

Application Documents

# Name Date
1 202117057337.pdf 2021-12-09
2 202117057337-TRANSLATIOIN OF PRIOIRTY DOCUMENTS ETC. [09-12-2021(online)].pdf 2021-12-09
3 202117057337-STATEMENT OF UNDERTAKING (FORM 3) [09-12-2021(online)].pdf 2021-12-09
4 202117057337-PRIORITY DOCUMENTS [09-12-2021(online)].pdf 2021-12-09
5 202117057337-FORM 1 [09-12-2021(online)].pdf 2021-12-09
6 202117057337-FIGURE OF ABSTRACT [09-12-2021(online)].pdf 2021-12-09
7 202117057337-DECLARATION OF INVENTORSHIP (FORM 5) [09-12-2021(online)].pdf 2021-12-09
8 202117057337-COMPLETE SPECIFICATION [09-12-2021(online)].pdf 2021-12-09
9 202117057337-Proof of Right [10-03-2022(online)].pdf 2022-03-10
10 202117057337-FORM-26 [10-03-2022(online)].pdf 2022-03-10
11 202117057337-FORM 3 [10-03-2022(online)].pdf 2022-03-10
12 202117057337-Others-150322.pdf 2022-03-17
13 202117057337-GPA-150322.pdf 2022-03-17
14 202117057337-Correspondence-150322.pdf 2022-03-17
15 202117057337-RELEVANT DOCUMENTS [18-11-2022(online)].pdf 2022-11-18
16 202117057337-MARKED COPIES OF AMENDEMENTS [18-11-2022(online)].pdf 2022-11-18
17 202117057337-FORM 13 [18-11-2022(online)].pdf 2022-11-18
18 202117057337-AMENDED DOCUMENTS [18-11-2022(online)].pdf 2022-11-18
19 202117057337-FORM-26 [22-11-2022(online)].pdf 2022-11-22
20 202117057337-Response to office action [28-11-2022(online)].pdf 2022-11-28
21 202117057337-Others-251122.pdf 2022-12-08
22 202117057337-Correspondence-251122.pdf 2022-12-08
23 202117057337-RELEVANT DOCUMENTS [24-05-2023(online)].pdf 2023-05-24
24 202117057337-MARKED COPIES OF AMENDEMENTS [24-05-2023(online)].pdf 2023-05-24
25 202117057337-FORM 13 [24-05-2023(online)].pdf 2023-05-24
26 202117057337-AMMENDED DOCUMENTS [24-05-2023(online)].pdf 2023-05-24
27 202117057337-FORM 18 [25-05-2023(online)].pdf 2023-05-25
28 202117057337-FER.pdf 2024-01-09
29 202117057337-Verified English translation [05-04-2024(online)].pdf 2024-04-05
30 202117057337-FORM 3 [08-04-2024(online)].pdf 2024-04-08
31 202117057337-Information under section 8(2) [03-07-2024(online)].pdf 2024-07-03
32 202117057337-FORM 3 [03-07-2024(online)].pdf 2024-07-03
33 202117057337-FER_SER_REPLY [03-07-2024(online)].pdf 2024-07-03
34 202117057337-COMPLETE SPECIFICATION [03-07-2024(online)].pdf 2024-07-03
35 202117057337-CLAIMS [03-07-2024(online)].pdf 2024-07-03
36 202117057337-ABSTRACT [03-07-2024(online)].pdf 2024-07-03
37 202117057337-US(14)-HearingNotice-(HearingDate-16-08-2024).pdf 2024-08-05
38 202117057337-Correspondence to notify the Controller [12-08-2024(online)].pdf 2024-08-12
39 202117057337-Information under section 8(2) [14-08-2024(online)].pdf 2024-08-14
40 202117057337-FORM 3 [14-08-2024(online)].pdf 2024-08-14
41 202117057337-RELEVANT DOCUMENTS [19-08-2024(online)].pdf 2024-08-19
42 202117057337-MARKED COPIES OF AMENDEMENTS [19-08-2024(online)].pdf 2024-08-19
43 202117057337-FORM 13 [19-08-2024(online)].pdf 2024-08-19
44 202117057337-AMMENDED DOCUMENTS [19-08-2024(online)].pdf 2024-08-19
45 202117057337-PatentCertificate20-08-2024.pdf 2024-08-20
46 202117057337-IntimationOfGrant20-08-2024.pdf 2024-08-20

Search Strategy

1 SearchstratogyE_08-01-2024.pdf

ERegister / Renewals

3rd: 14 Oct 2024

From 29/05/2022 - To 29/05/2023

4th: 14 Oct 2024

From 29/05/2023 - To 29/05/2024

5th: 14 Oct 2024

From 29/05/2024 - To 29/05/2025

6th: 17 Mar 2025

From 29/05/2025 - To 29/05/2026