FIELD OF THE INVENTION
The present invention relates to novel triterpene derivatives and related compounds,
compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated
diseases.
BACKGROUND OF THE INVENTION
The Human Immunodeficiency Virus (HIV) has now been established as the
causative agent of the Acquired Immunodeficiency Syndrome (AIDS) for over 20 years
(Science 1983, 220, 868-871; N.Eng.J.Med.1984, 311, 1292-1297). AIDS is characterized by
the destruction of the immune system, particularly of CD4+ T -cells. HIV is a retrovirus, and
the HIV life cycle encompasses several crucial steps, starting from the attachment of the virus
15 to the host cell membrane and finishing with the release of progeny virons from the cell.
The natural compound betulinic acid, isolated from Syzygium clavifolium and several
other plant species was found to possess anti-HIV activity. Chemical modifications were
undertaken by several research groups in an attempt to identify potent anti-HIV agents by
making semi-synthetic analogs of betulinic acid, leading to the discovery of bevirimat as a
20 compound with a novel mechanism of action (J. Nat. Prod. 1994, 57(2): 243-7; J. Med.
Chern. 1996, 39(5), 1016). Further studies shown that bevirimat acts by disrupting Gag
processing (Proc. Natl. Acad. Sci. USA 2003, 100(23):13555-60; Antimicrob. Agents.
Chemother. 2001, 45(4), 1225-30; J. Viral. 2004, 78(2): 922-9; J. Bioi. Chern. 2005,
280(51):42149-55; J. Viral. 2006, 80(12): 5716-22) and to be a first-in-class maturation
25 inhibitor with a potent activity against HIV -1. Bevirimat went up to phase 2 clinical trials, in
clinic despite optimal plasma concentrations, not all patients given bevirimat have a robust
viral load reduction. It was reported that non-respondant patients had more frequent base line
Gag polymorphisms near the capsid SP-1 cleavage site than responders. (HIV gag
polymorphism determines treatment response to bevirimat. XVII international HIV drug
30 resistance work shop June 10-14, 2008, Sitges, Spain).
Encouraged by these developments, medicinal chemists started exploring betulinic
acid derivatives and related compounds intensively for their therapeutic activities. For
example, W02017/149518 disclosed C-3 novel triterpene with C-17 amine derivatives as hiv
3
inhibitors; W02014/105926 disclosed novel betulinic acid proline derivatives as HIV
inhibitors; W02014/130810 describes preparation of C3 alkyl and alkenyl modified betulinic
acid derivatives useful in the treatment of HIV; W02014/123889 describes preparation of
triterpenoid derivatives for use as HIV maturation inhibitors; W02013/160810 disclosed
5 novel betulinic acid derivatives as HIV inhibitors; W02013/169578 describes C-17 bicyclic
amines of triterpenoids with HIV maturation inhibitory activity and their preparation; WO
20131123019 describes C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory
activity; W02013/043778 describes novel betulinic acid derivatives with antiviral activity;
W02013/035943 describes betulinic acid and derivatives thereof having anti-aging activity;
10 W02012/106190 describes preparation of C17 and C3 modified triterpenoids with HIV
maturation inhibitory activity; CN102399254 describes novel pentacyclic triterpenoid
derivatives, their preparation method and application for preventing and treating diabetes,
cardiovascular disease, cerebrovascular disease and tumor; W02011/007230 describes
preparation of lupeol-type triterpene derivatives as antiviral agents; W02010/032123
15 describes preparation of triterpenoid compounds for pharmaceutical use; Journal of Medicinal
Chemistry (20 1 0), 53( 1 ), 178-190 describes structure-activity relationship study of betulinic
acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in
diabetes; WO 20091100532 describes preparation of 17~-lupane derivatives for the treatment
of HIV infection; CN 101367861 describes preparation method and application of 2-hydroxy-
20 3-deoxy-pentacyclic triterpene compounds and derivatives; W02008/138200 describes
preparation of lupane derivatives as NMDA and MC receptor antagonists exhibiting
neuroprotective and memory enhancing activities; W02008/127364 describes preparation of
betulinic acid derivatives for use in antiviral and anticancer pharmaceutical compositions.
Some additional references disclose betulinic acid related compounds. For example,
25 W02006/053255 describes preparation of betulin derivatives for use in pharmaceutical
compositions which inhibit the transmission of viral infection; W02004/089357 describes
anti-fungal formulation of triterpene and essential oil; Bioorganic & Medicinal Chemistry
Letters (2003), 13(20), 3549-3552 describes lupane triterpenes and derivatives with antiviral
activity; Russian Journal of Bioorganic Chemistry (2003), 29(6), 594-600 describes synthesis
30 and antiviral activity of ureides and carbamates of betulinic acid and its derivatives; Journal
of Medicinal Chemistry (1996), 39(5), 1056-68 describes betulinic acid derivatives: a new
class of human immunodeficiency virus type 1 specific inhibitors with a new mode of action;
4
Oxidation Communications (1987), 10(3-4), 305-12 describes oxidative decarboxylations. II.
oxidative decarboxylation of acetyl betulinic acid.
Given the fact of the world wide epidemic level of AIDS, there is a strong continued
need for new effective drugs for treatment of HIV infected patients, disease conditions and/or
5 disorders mediated by HIV by discovering new compounds with novel structures and/or
mechanism of action(s).
SUMMARY OF THE INVENTION
The present invention relates to the compound of the formula (I):
Formula (I)
10 wherein,
15
20
25
~V'V't ~ykx 0~
R1 is selected from g I" , o , oH
HO~·
'
H01fX!-
' '
::n-..~0
~bH
'
or
R2 is selected from C1-C6 alkyl, optionally substituted C2-C6 alkenyl, or optionally
substituted C3-C8 cycloalkyl; wherein the optional substituent is C1-C6 alkyl;
R3 is hydrogen, or C1-C6 alkyl;
~ is selected from optionally substituted C1-C6 alkyl, or -C(O)ORa; wherein the
optional substituent is selected from halo, hydroxy, alkoxy, -OC(O)CH2alkoxy, -0Si(Ra)3, -
N(Ra)(Rb), -S(Ra), or -O-CH2-P(O)(ORah;
t (~)
: : () o~t
n. ng /.'t._. ... N... : . "" ~ ,, Ra ~-- IS o , or o
Ra is hydrogen, or C1-C6 alkyl;
Rb is selected from hydrogen, alkyl, -C(O)alkoxy, or -S(Ohalkyl, and
'n' is an integer selected from 1-2; or
pharmaceutically acceptable salts, pharmaceutically acceptable stereoisomers,
prodrugs, or combination thereof.
According to one embodiment, there is provided a compound of formula (I), wherein
5
5
Rl is Ho~!-.
According to another embodiment, there is provided a compound of formula (1),
wherein
According to yet another embodiment, there is provided a compound of formula (1),
wherein R2 is isopropylene.
According to yet another embodiment, there is provided a compound of formula (1),
wherein R2 is methylcyclopropyl.
According to yet another embodiment, there is provided a compound of formula (1),
10 wherein R3 is hydrogen.
15
According to yet another embodiment, there is provided a compound of formula (1),
wherein 'n' is 1 or 2.
According to yet another embodiment, there is provided a compound of formula (1),
+ N : : C)
wherein ring /\N,~_.: is c5' ~
Accordingly, another aspect of the present invention provides compound of formula
(lA):
'' '' '' ''
Formula (IA)
I '
wherein R1, R2, R3, ~, and ring /\N,~_) are same as defined in formula (I); or
pharmaceutically acceptable salts, pharmaceutically acceptable stereoisomers,
20 prodrugs, or combination thereof.
25
According to one embodiment, there IS provided a compound of formula (lA),
wherein R2 is isopropylene.
According to another embodiment, there is provided a compound of formula (lA),
wherein R2 is methylcyclopropyl.
According to yet another embodiment there is provided a compound of formula (lA),
wherein R3 is hydrogen.
6
5
10
15
According to yet another embodiment there is provided a compound of formula (lA),
wherein R3 is methyl.
According to yet another embodiment, there is provided a compound of formula (1),
wherein 'n' is 2.
According to yet another embodiment, there is provided a compound of formula (lA),
+ N :' ': c)
wherein ring ,..\:N'~--: is cl'>o
Accordingly, another aspect of the present invention provides compound of formula
(IB):
·,
' '
N"'"XN'~-)
H R3 ~
Formula (IB)
' '
wherein R2, R3, ~'and ring XN-~ _ _:' are same as defined in formula (I); or
pharmaceutically acceptable salts, pharmaceutically acceptable stereoisomers,
prodrugs, or combination thereof.
According to one embodiment, there IS provided a compound of formula (lA),
wherein R2 is isopropylene.
According to another embodiment, there is provided a compound of formula (lA),
wherein R2 is methylcyclopropyl.
According to yet another embodiment there is provided a compound of formula (lA),
wherein R3 is hydrogen.
According to yet another embodiment there is provided a compound of formula (lA),
20 wherein R3 is methyl.
According to yet another embodiment, there is provided a compound of formula (1),
wherein 'n' is 2.
According to yet another embodiment, there is provided a compound of formula (lA),
+ N
: : ()
wherein ring ,..\:N'~--: is c/'b
7
Below are the representative compounds, which are illustrative in nature only and are
not intended to limit to the scope of the invention (Nomenclature has been generated from
ChemBioDraw Ultra 13.0 version):
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1, Is
dioxidothiomorpholino )-3-methoxy-3-oxopropyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(lmethylcyclopropyl)
icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2
dimethylcyclobutane-1-carboxylic acid,
5-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,l3aR,l3bR)-3a-(((2R,3R)-2-(l,ldioxidothiomorpholino
)-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
10 yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5 -oxopentanoic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,l3aR,l3bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
15 (1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,l3aR,l3bR)-3a-(((2R,3S)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2S,3R)-2-( 1,1-
20 dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3S)-2-( 1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
25 methylcyclopropyl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbony 1)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2S,3R)-2-( 1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
30 dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
8
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2S,3S)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
5 (1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2R,3S)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2S,3R)-2-(1, 1-
10 dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
15 yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
20 carboxylic acid,
(1S,3R)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3S)-2-( 1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
25 (1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2S,3R)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
30 dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
9
me thy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )carbon y 1)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1S,3R)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((2R,3S)-2-( 1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
5 methylcyclopropyl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbony 1)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1S,3R)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2S,3R)-2-( 1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
10 dimethylcyclobutane-1-carboxylic acid,
(1S,3R)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
15 (1S,3R)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2S,3S)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1S,3R)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2R,3S)-2-(1, 1-
20 dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1S,3R)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2S,3R)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11a-
25 pentamethylicosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
30 carboxylic acid,
(1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxylic acid,
10
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8,11a-pentamethy1-1-(prop-1-en-2-
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxy1ic acid,
5 (1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8,11a-pentamethy1-1-(prop-1-en-2-
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxy1ic acid,
(1S,3R)-3-(2-(((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(((2R,3R)-2-
10 (1,1-dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8, 11a-pentamethy1-1-(prop-1-
en-2-y1)icosahydro-1H-cyclopenta[a]chrysen-9-y1)oxy)-2-oxoethy1)-2,2-
dimethylcyclopropane-1-carboxy1ic acid,
(1S,3R)-3-(2-( (( 1R,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-(( (2S,3S)-2-(1, 1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8,11a-pentamethy1-1-(prop-1-en-2-
15 y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy)-2-oxoeth y 1 )-2,2-dimeth y lcyclopropane-1-
carboxy1ic acid,
2-( (1R,3S)-3-( (( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-2-
(1,1-dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8, 11a-pentamethy1-1-(prop-1-
en-2-y1)icosahydro-1H-cyclopenta[a]chrysen-9-y1)oxy)carbony1)-2,2-
20 dimethylcyclopropy1)acetic acid,
2-((1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(((2S,3S)-2-
(1,1-dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8, 11a-pentamethy1-1-(prop-1-
en-2-y1)icosahydro-1H-cyclopenta[a]chrysen-9-y1)oxy)carbony1)-2,2-
dimethylcyclopropy1)acetic acid,
25 2-((1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(((2R,3R)-2-
(1,1-dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8, 11a-pentamethy1-1-(1-
methylcyclopropy1)icosahydro-1H-cyclopenta[a]chrysen-9-y1)oxy)carbony1)-2,2-
dimethylcyclopropy1)acetic acid,
2-( (1R,3S)-3-( (( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2S,3S)-2-
30 (1,1-dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8, 11a-pentamethy1-1-(1-
methylcyclopropy1)icosahydro-1H-cyclopenta[a]chrysen-9-y1)oxy)carbony1)-2,2-
dimethylcyclopropy1)acetic acid,
2-( (1R,3S)-3-( (( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-2-
(1,1-dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-1-isopropy1-5a,5b,8,8, 11a11
pentamethylicosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropyl)acetic acid,
2-( (1R,3S)-3-( (( (lS,3aS,5aR,5bR,7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((2S,3S)-2-
(l,l-dioxidothiomorpholino )-3-hydroxybutyl)amino )-l-isopropyl-5a,5b,8,8, lia-
S pentamethylicosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropyl)acetic acid,
4-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,l3aR,l3bR)-3a-(((2R,3R)-2-(l,ldioxidothiomorpholino
)-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-2,2-dimethyl-4-oxobutanoic acid,
10 4-(((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,l3aR,l3bR)-3a-(((2S,3S)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-2,2-dimethyl-4-oxobutanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
15 methylcyclopropyl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-2,2-dimethyl-4-
oxobutanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,l3aR,l3bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-
20 oxobutanoic acid,
4-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,l3aR, 13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentameth
ylicosah ydro-1 H -cyclopenta[ a] chrysen -9-y l)ox y)-2,2-dimeth y 1-4-oxobutanoic
acid,
25 4-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,l3aR, 13bR)-3a-(((2S,3S)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentameth
ylicosah ydro-1 H -cyclopenta[ a] chrysen -9-y l)ox y)-2,2-dimeth y 1-4-oxobutanoic
acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,l3aR,l3bR)-3a-(((2R,3R)-2-(1,1-
30 dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5 -oxopentanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,l3aR,l3bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5 -oxopentanoic acid,
12
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-
oxopentanoic acid,
5 5-(((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(((2S,3S)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )-3,3 -dimeth y 1-5-
oxopentanoic acid,
5-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((2R,3R)-2-(1, 1-
10 dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-oxopentanoic
acid,
5-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((2S,3S)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11a-
15 pentamethylicosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-oxopentanoic
acid,
4-( (( 1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-
20 4-oxobutanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8, 11 a-pentamethyl-1-
(prop-1-en-2-yl)icosahydro-1H -cyclopenta[ a ]chrysen -9-yl)oxy )-2,2-dimethyl-4-oxobutanoic
acid,
25 (1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
30 dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-
(prop-1-en-2-yl)icosahydro-1H -cyclopenta[ a ]chrysen -9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11a13
pentameth yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,13aR,13bR)-3a-(((2R,3R)-2-(l, 1-
dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8, 11 a-pentamethyl-1-
5 ( 1-methylcyclopropyl)icosahydro-IH -cyclopenta[ a ]chrysen -9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lS,3aS,5aR,5bR,7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-l-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
10 dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((2R,3R)-2-(l,ldioxidothiomorpholino
)-3 -(phosphonomethox y) buty 1 )amino )-1-isopropy 1-5 a,5b, 8,8, 11 apentamethylicosahydro-
IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
15 5-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,13aR,13bR)-3a-(((2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, llapentamethyl-
1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-
5-oxopentanoic acid,
5-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,13aR,13bR)-3a-(((2R,3R)-2-(l,l-
20 dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8,lla-pentamethyl-l(
prop-l-en-2-yl)icosahydro-IH -cyclopenta[ a ]chrysen -9-yl)oxy )-3 ,3-dimethyl-5-oxopentanoic
acid,
5-( (( lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, lla-
25 pentamethyl-1-(1-methylcyclopropyl)icosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)-3,3-
dimethyl-5-oxopentanoic acid,
5-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,13aR,13bR)-3a-(((2R,3R)-2-(l, 1-
dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8, 11 a-pentamethyl-1-
( 1-methylcyclopropyl)icosahydro-IH -cyclopenta[ a ]chrysen -9-yl)oxy )-3 ,3-dimethyl-5-
30 oxopentanoic acid,
5-( (( lS,3aS,5aR,5bR,7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-l-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5-
oxopentanoic acid,
14
5-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3 -(phosphonomethox y) buty 1 )amino )-1-isopropy 1-5 a,5b, 8,8, 11 apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-oxopentanoic
acid,
5 2-((1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR, 13aR, 13bR)-3a-(((2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropyl)acetic acid,
2-( (1R,3S)-3-( (( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-2-
10 (1,1-dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8,11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropyl)acetic acid,
2-( (1R,3S)-3-( (( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11a-
15 pentameth yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclopropyl)acetic acid,
2-( (1R,3S)-3-( (( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-2-
( 1, 1-dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8, 11apentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
20 yl)oxy)carbonyl)-2,2-dimethylcyclopropyl)acetic acid,
2-( (1R,3S)-3-( (( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-1-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclopropyl)acetic acid,
25 2-( (1R,3S)-3-( (( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-2-
(1,1-dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropyl)acetic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((12R,13R)-13-(1,1-
30 dioxidothiomorpholino )-12-methyl-2,5,8, 11-tetraoxatetradecan-14-yl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-
4-oxobutanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((12R,13R)-13-(1,1-
dioxidothiomorpholino )-12-methyl-2,5,8, 11-tetraoxatetradecan-14-yl)amino )-5a,5b,8,8, 11a15
pentamethyl-1-(1-methylcyclopropyl)icosahydro-IH-cyclopenta[ a]chrysen-9-yl)oxy)-2,2-
dimethyl-4-oxobutanoic acid,
4-(((lS,3aS,5aR,5bR,7aR,9S,llaR,llbR,13aR, 13bR)-3a-(((12R, 13R)-13-(l,ldioxidothiomorpholino
)-12-methyl-2,5,8, 11-tetraoxatetradecan-14-yl)amino )-1-isopropyl-
5 5a,5b,8,8, 11 a-pentamethylicosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )-2,2-dimethyl-4-
oxobutanoic acid,
5-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,13aR,13bR)-3a-(((12R,13R)-13-(l,ldioxidothiomorpholino
)-12-methyl-2,5,8, 11-tetraoxatetradecan-14-yl)amino )-5a,5b,8,8, llapentamethyl-
1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-
10 5-oxopentanoic acid,
5-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,13aR,13bR)-3a-(((12R,13R)-13-(l,ldioxidothiomorpholino
)-12-methyl-2,5,8, 11-tetraoxatetradecan-14-yl)amino )-5a,5b,8,8, llapentamethyl-
1-(1-methylcyclopropyl)icosahydro-IH-cyclopenta[ a]chrysen-9-yl)oxy)-3,3-
dimethyl-5-oxopentanoic acid,
15 5-(((lS,3aS,5aR,5bR,7aR,9S,llaR,llbR,13aR, 13bR)-3a-(((12R, 13R)-13-(l,ldioxidothiomorpholino
)-12-methyl-2,5,8, 11-tetraoxatetradecan-14-yl)amino )-l-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5-
oxopentanoic acid,
4-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,13aR,13bR)-3a-(((15R,l6R)-16-(l,l-
20 dioxidothiomorpholino )-15-methyl-13-oxo-2,5,8, 11, 14-pentaoxaheptadecan-17-yl)amino )-
5a,5b,8,8, lla-pentamethyl-1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[a]chrysen-9-
yl)oxy)-2,2-dimethyl-4-oxobutanoic acid,
4-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,13aR, 13bR)-3a-(((15R,l6R)-16-(l,ldioxidothiomorpholino
)-15-methyl-13-oxo-2,5,8, 11, 14-pentaoxaheptadecan-17-yl)amino )-
25 5 a,5b, 8,8, 11 a-pentamethy 1-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)-2,2-dimethyl-4-oxobutanoic acid,
4-(((lS,3aS,5aR,5bR,7aR,9S,llaR,llbR, 13aR, 13bR)-3a-(((15R, 16R)-16-(l,ldioxidothiomorpholino
)-15-methyl-13-oxo-2,5,8, 11, 14-pentaoxaheptadecan-17-yl)amino )-!isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )-2,2-
30 dimethyl-4-oxobutanoic acid,
5-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,13aR,13bR)-3a-(((15R,l6R)-16-(l,ldioxidothiomorpholino
)-15-methyl-13-oxo-2,5,8, 11, 14-pentaoxaheptadecan-17-yl)amino )-
5a,5b,8,8, lla-pentamethyl-1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[a]chrysen-9-
yl)oxy)-3,3-dimethyl-5-oxopentanoic acid,
16
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((15R,16R)-16-(1,1-
dioxidothiomorpholino )-15-methyl-13-oxo-2,5,8, 11, 14-pentaoxaheptadecan-17-yl)amino )-
5a,5b,8,8, 11a-pentamethyl-1-( 1-methylcyclopropyl)icosahydro-1H -cyclopenta[ a]chrysen-9-
yl)oxy)-3,3-dimethyl-5-oxopentanoic acid,
5 5-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((15R, 16R)-16-(1,1-
dioxidothiomorpholino )-15-methyl-13-oxo-2,5,8, 11, 14-pentaoxaheptadecan-17-yl)amino )-1-
isopropyl-5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3,3-
dimethyl-5-oxopentanoic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((S)-3-amino-2-
10 (1,1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((S)-3-amino-2-
(1,1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
15 me thy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )carbon y 1)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (S)-3-amino-2-
(1,1-dioxidothiomorpholino )propyl)amino )-1-isopropyl-5a,5b,8,8, 11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
20 dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-
amino-2-(1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-
2-yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
25 (1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-
amino-2-(1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )carbon y 1)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
30 amino-2-(1, 1-dioxidothiomorpholino )butyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-( (tertbutoxycarbonyl)
amino )-2-( 1, 1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8, 11a17
pentamethyl-1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-( (tertbutoxycarbonyl)
amino )-2-( 1, 1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8, lia-
S pentameth yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lS,3aS,5aR,5bR,7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ( (R)-3-( (tertbutoxycarbonyl)
amino )-2-( 1, 1-dioxidothiomorpholino )propyl)amino )-l-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
10 dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-((tertbutoxycarbonyl)
amino )-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, llapentamethyl-
1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
15 (1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-((tertbutoxycarbonyl)
amino )-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, llapentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lS,3aS,5aR,5bR,7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-( (tert-
20 butoxycarbonyl)amino )-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-l-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )propyl)amino )-5a,5b,8,8, lla-
25 pentamethyl-1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )propyl)amino )-5a,5b,8,8, llapentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
30 yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((R)-2-(l, 1-
dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )propyl)amino )-l-isopropyl-5a,5b,8,8, llapentamethylicosahydro-
IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
18
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )butyl)amino )-5a,5b,8,8, 11a-pentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[ a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
5 (1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )butyl) amino )-5a,5b,8,8, 11a-pentamethyl-
1-( 1-methylcyclopropyl)icosahydro-1 H -cyclopenta[ a ]chrysen -9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2R,3R)-2-(1,1-
10 dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )butyl) amino )-1-isopropyl-5a,5b,8,8, 11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR, 13aR, 13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-3-( (isopropoxycarbonyl)amino )propyl)amino )-5a,5b,8,8, 11a-
15 pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-3-( (isopropoxycarbonyl)amino )propyl)amino )-5a,5b,8,8, 11apentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
20 yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((R)-2-(1, 1-
dioxidothiomorpholino )-3-( (isopropoxycarbonyl)amino )propyl)amino )-1-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
25 (1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-( (isopropoxycarbonyl)amino )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
30 dioxidothiomorpholino )-3-( (isopropoxycarbonyl)amino )butyl)amino )-5a,5b,8,8, 11apentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-( (isopropoxycarbonyl)amino )butyl)amino )-1-isopropyl19
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino)-3-(((2-methoxyethoxy)carbonyl)amino)propyl)amino)-
5 5a,5b,8,8, 11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-3-( ( (2-methoxyethoxy )carbonyl)amino )propyl)amino )-
5a,5b,8,8, 11a-pentamethyl-1-( 1-methylcyclopropyl)icosahydro-1H -cyclopenta[ a]chrysen-9-
10 yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((R)-2-(1, 1-
dioxidothiomorpholino )-3-( ((2-methoxyethoxy)carbonyl)amino )propyl)amino )-1-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
15 (1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-( ((2-methoxyethoxy)carbonyl)amino )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR, 13aR, 13bR)-3a-(((2R,3R)-2-(1, 1-
20 dioxidothiomorpholino )-3-( ((2-methoxyethoxy)carbonyl)amino )butyl)amino )-5a,5b,8,8, 11apentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-( ((2-methoxyethoxy)carbonyl)amino )butyl)amino )-1-isopropyl-
25 5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((R)-12-(1,1-
dioxidothiomorpholino )-9-oxo-2,5,8-trioxa-1 0-azatridecan-13-yl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
30 dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((R)-12-(1,1-
dioxidothiomorpholino )-9-oxo-2,5,8-trioxa-1 0-azatridecan-13-yl)amino )-5a,5b,8,8, 11apentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
20
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((R)-12-(1, 1-
dioxidothiomorpholino )-9-oxo-2,5,8-trioxa-10-azatridecan-13-yl)amino )-1-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
5 (1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(((11R,12R)-12-
(1,1-dioxidothiomorpholino )-11-methyl-9-oxo-2,5,8-trioxa-10-azatridecan-13-yl)amino )-
5a,5b,8,8, 11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((11R, 12R)-12-
10 ( 1, 1-dioxidothiomorpholino )-11-methyl-9-oxo-2,5 ,8-trioxa-1 0-azatridecan-13-yl)amino )-
5a,5b,8,8, 11a-pentamethyl-1-( 1-methylcyclopropyl)icosahydro-1H -cyclopenta[ a]chrysen-9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR,13aR,13bR)-3a-(((11R,12R)-12-
( 1, 1-dioxidothiomorpholino )-11-methyl-9-oxo-2,5 ,8-trioxa-1 0-azatridecan-13-yl)amino )-1-
15 isopropyl-5a,5b,8,8,11a-pentamethylicosahydro-1H-cyclopenta[a]chrysen-9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )propyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
20 dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )propyl)amino )-5a,5b,8,8, 11apentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
25 (1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((R)-2-(1, 1-
dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )propyl)amino )-1-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
30 dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )butyl)amino )-5a,5b,8,8, 11a21
pentameth yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((2R,3R)-2-(l,ldioxidothiomorpholino
)-3-( (1-methylethyl)sulfonamido )butyl)amino )-1-isopropyl-
5 5a,5b,8,8, lla-pentamethylicosahydro-IH-cyclopenta[ a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-3-(methylthio )propyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-len-
2-yl)icosahydro-IH -cyclopenta[ a ]chrysen -9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
10 carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-3-(methylthio )propyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(lmethylcyclopropyl)
icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
15 (lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,l3aR,l3bR)-3a-(((S)-2-(l, 1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-len-
2-yl)icosahydro-IH -cyclopenta[ a ]chrysen -9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((S)-2-(l,l-
20 dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(lmethylcyclopropyl)
icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
4-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,l3aR, 13bR)-3a-(((S)-3-amino-2-(l, 1-
dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-l-en-2-
25 yl)icosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )-2,2-dimethyl-4-oxobutanoic acid,
5-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,l3aR,l3bR)-3a-(((S)-3-amino-2-(l, 1-
dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-l-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5 -oxopentanoic acid,
4-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,l3aR,l3bR)-3a-(((2R,3R)-3-amino-2-(l, 1-
30 dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-l-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-2,2-dimethyl-4-oxobutanoic acid,
5-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,l3aR,l3bR)-3a-(((2R,3R)-3-amino-2-(l, 1-
dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-l-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5 -oxopentanoic acid,
22
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )propyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-
4-oxobutanoic acid,

WE CLAIM:
69
5
10
15
20
1. A compound of the formula (I):
Formula (I)
wherein,
HO~t HOyk"( 0~
R1 is selected from g I' , o , oH
HO~·
'
H0'1()(!-
' '
"J-t-..~0
/Z..._ OH
'
or
R2 is selected from C1-C6 alkyl, optionally substituted C2-C6 alkenyl, or optionally
substituted C3-C8 cycloalkyl; wherein the optional substituent is C1-C6 alkyl;
R3 is hydrogen, or C1-C6 alkyl;
~ is selected from optionally substituted C1-C6 alkyl, or -C(O)ORa; wherein the
optional substituent is selected from halo, hydroxy, alkoxy, -OC(O)CH2alkoxy, -0Si(Ra)3, -
N(Ra)(Rb), -S(Ra), or -O-CH2-P(O)(ORah;
t (~)
N
: : () o~t
ring /\. -~---' is cf ->a, or C! R.
Ra is hydrogen, or C1-C6 alkyl;
Rb is selected from hydrogen, alkyl, -C(O)alkoxy, or -S(Ohalkyl, and
'n' is an integer selected from 1-2; or
pharmaceutically acceptable salts, pharmaceutically acceptable stereoisomers,
prodrugs, or combination thereof.
2. The compound according to claim 1, which is a compound of the formula (lA):
'' '' ' . ' '
Formula (lA)
wherein,
70
5
10
15
20
Ho~t Hoyk-..;: 0~
R1 is selected from g I" , o , oH
HO~·
'
HO'()Z'-
' '
'A.~ a
~bH
'
or
R2 is selected from C1-C6 alkyl, optionally substituted C2-C6 alkenyl, or optionally
substituted C3-Cs cycloalkyl; wherein the optional substituent is C1-C6 alkyl;
R3 is hydrogen, or C1-C6 alkyl;
~ is selected from optionally substituted C1-C6 alkyl, or -C(O)ORa; wherein the
optional substituent is selected from halo, hydroxy, alkoxy, -OC(O)CH2alkoxy, -0Si(Ra)3, -
N(Ra)(Rb), -S(Ra), or -O-CH2-P(O)(ORah;
t (~)
: : C) o~t . 'l._,N.. , . ,, "o , Ra nng .... ,_ ~-- IS o , or o
Ra is hydrogen, or C 1-C6 alkyl; and
Rb is selected from hydrogen, alkyl, -C(O)alkoxy, or -S(Ohalkyl, or
pharmaceutically acceptable salts, pharmaceutically acceptable stereoisomers,
prodrugs, or combination thereof.
3. The compound according to claim 1, which is a compound of the formula (IB):
·,
' '
N~N-~_)
H R3 ~
Formula (IB)
wherein,
R2 is selected from C1-C6 alkyl, optionally substituted C2-C6 alkenyl, or optionally
substituted C3-C8 cycloalkyl; wherein the optional substituent is C1-C6 alkyl;
R3 is hydrogen, or C1-C6 alkyl;
~ is selected from optionally substituted C1-C6 alkyl, or -C(O)ORa; wherein the
optional substituent is selected from halo, hydroxy, alkoxy, -OC(O)CH2alkoxy, -0Si(Ra)3, -
N(Ra)(Rb), -S(Ra), or -O-CH2-P(O)(ORah;
' ' t (~) : : C) o~t
n.n g ...'.l ,.__ ,N.. , . "" "o " Ra ~-- IS o , or o
Ra is hydrogen, or C1-C6 alkyl; and
71
5
10
15
20
Rb is selected from hydrogen, alkyl, -C(O)alkoxy, or -S(Ohalkyl, or
pharmaceutically acceptable salts, pharmaceutically acceptable stereoisomers,
prodrugs, or combination thereof.
4. The compound according to claim 1, which is a compound of the formula (IC):
Formula (IC)
wherein,
R2 is selected from C1-C6 alkyl, optionally substituted C2-C6 alkenyl, or optionally
substituted C3-Cs cycloalkyl; wherein the optional substituent is C1-C6 alkyl;
R3 is hydrogen, or C1-C6 alkyl;
~ is selected from optionally substituted C1-C6 alkyl, or -C(O)ORa; wherein the
optional substituent is selected from halo, hydroxy, alkoxy, -OC(O)CH2alkoxy, -0Si(Ra)3, -
N(Ra)(Rb), -S(Ra), or -O-CH2-P(O)(ORah;
Ra is hydrogen, or C 1-C6 alkyl; and
Rb is selected from hydrogen, alkyl, -C(O)alkoxy, or -S(Ohalkyl, or
pharmaceutically acceptable salts, pharmaceutically acceptable stereoisomers,
prodrugs, or combination thereof.
5. The compound according to claim 1, which is a compound of the formula (ID):
Formula (ID)
wherein,
~~t~ykxo~
R1 is selected from g I" , o , oH
HO'()ZI-
' '
HQLOt-.
'
:n-..~0
/Z-... bH
'
or
R2 is selected from C1-C6 alkyl, optionally substituted C2-C6 alkenyl, or optionally
substituted C3-Cs cycloalkyl; wherein the optional substituent is C1-C6 alkyl;
R3 is hydrogen, or C1-C6 alkyl;
72
~ is selected from optionally substituted C1-C6 alkyl, or -C(O)ORa; wherein the
optional substituent is selected from halo, hydroxy, alkoxy, -OC(O)CH2alkoxy, -0Si(Ra)3, -
N(Ra)(Rb), -S(Ra), or -O-CH2-P(O)(ORah;
Ra is hydrogen, or C 1-C6 alkyl; and
5 Rb is selected from hydrogen, alkyl, -C(O)alkoxy, or -S(Ohalkyl, or
pharmaceutically acceptable salts, pharmaceutically acceptable stereoisomers,
prodrugs, or combination thereof.
6. A compound selected from the group consisting of:
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
10 dioxidothiomorpholino )-3-methoxy-3-oxopropyl)amino )-5a,5b,8,8,lla-penta methyl-1-(1-
methylcyclopropyl)icosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2
dimethylcyclobutane-1-carboxylic acid,
5-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,13aR,13bR)-3a-(((2R,3R)-2-(l,ldioxidothiomorpholino
)-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
15 yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5 -oxopentanoic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
20 (1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3S)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2S,3R)-2-( 1,1-
25 dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3S)-2-( 1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
30 methylcyclopropyl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbony 1)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2S,3R)-2-( 1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
73
me thy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )carbon y 1 )-2,2-
dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((2R,3R)-2-(l,ldioxidothiomorpholino
)-3-hydroxybutyl)amino )-l-isopropyl-5a,5b,8,8,lla-
5 pentamethylicosahydro-lH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((2S,3S)-2-(l,ldioxidothiomorpholino
)-3-hydroxybutyl)amino )-l-isopropyl-5a,5b,8,8,llapentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
10 dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((2R,3S)-2-(l, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-l-isopropyl-5a,5b,8,8,llapentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
15 (lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((2S,3R)-2-(l, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-l-isopropyl-5a,5b,8,8,llapentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(lS,3R)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,l3aR,l3bR)-3a-(((2R,3R)-2-(l, 1-
20 dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,l3aR,l3bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
25 yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1S,3R)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3S)-2-( 1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
30 carboxylic acid,
(1S,3R)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2S,3R)-2-( 1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
74
(1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8,11a-pentamethy1-1-(1-
methy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )carbon y 1 )-2,2-
dimethylcyclobutane-1-carboxy1ic acid,
5 (1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8,11a-pentamethy1-1-(1-
methylcyclopropy1)icosahydro-1H-cyclopenta[a]chrysen-9-y1)oxy)carbony1)-2,2-
dimethylcyclobutane-1-carboxy1ic acid,
(1S,3R)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3S)-2-( 1,1-
10 dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8,11a-pentamethy1-1-(1-
methylcyclopropy1)icosahydro-1H-cyclopenta[a]chrysen-9-y1)oxy)carbony1)-2,2-
dimethylcyclobutane-1-carboxy1ic acid,
(1S,3R)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2S,3R)-2-( 1,1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8,11a-pentamethy1-1-(1-
15 me thy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )carbon y 1)-2,2-
dimethylcyclobutane-1-carboxy1ic acid,
(1S,3R)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-1-isopropy1-5a,5b,8,8,11apentamethy1icosahydro-
1H-cyclopenta[a]chrysen-9-y1)oxy)carbony1)-2,2-
20 dimethylcyclobutane-1-carboxy1ic acid,
(1S,3R)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2S,3S)-2-(1,1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-1-isopropy1-5a,5b,8,8,11apentamethy1icosahydro-
1H-cyclopenta[a]chrysen-9-y1)oxy)carbony1)-2,2-
dimethylcyclobutane-1-carboxy1ic acid,
25 (1S,3R)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2R,3S)-2-(1, 1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-1-isopropy1-5a,5b,8,8,11apentamethy1icosahydro-
1H-cyclopenta[a]chrysen-9-y1)oxy)carbony1)-2,2-
dimethylcyclobutane-1-carboxy1ic acid,
(1S,3R)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2S,3R)-2-(1, 1-
30 dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-1-isopropy1-5a,5b,8,8,11apentamethy1icosahydro-
1H-cyclopenta[a]chrysen-9-y1)oxy)carbony1)-2,2-
dimethylcyclobutane-1-carboxy1ic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8,11a-pentamethy1-1-(prop-1-en-2-
75
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxylic acid,
(lS,3R)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,13aR,13bR)-3a-(((2R,3R)-2-(l, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
5 y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
10 carboxylic acid,
(1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclopropane-1-
carboxylic acid,
15 (1S,3R)-3-(2-(((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(((2R,3R)-2-
(1,1-dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8, 11a-pentamethyl-1-(prop-1-
en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2-oxoethyl)-2,2-
dimethylcyclopropane-1-carboxylic acid,
(1S,3R)-3-(2-( (( 1R,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2S,3S)-2-(1, 1-
20 dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-2-oxoeth yl)-2,2-dimethylcyclopropane-1-
carboxylic acid,
2-( (1R,3S)-3-( (( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-2-
(1,1-dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8, 11a-pentamethyl-1-(prop-1-
25 en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropyl)acetic acid,
2-( (1R,3S)-3-( (( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2S,3S)-2-
(1,1-dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8, 11a-pentamethyl-1-(prop-1-
en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
30 dimethylcyclopropyl)acetic acid,
2-( (1R,3S)-3-( (( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-2-
(1,1-dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8, 11a-pentamethyl-1-(1-
methy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )carbon y 1)-2,2-
dimethylcyclopropyl)acetic acid,
76
2-( (1R,3S)-3-( (( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2S,3S)-2-
(1,1-dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8, 11a-pentamethy1-1-(1-
methy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )carbon y 1)-2,2-
dimethylcyclopropy1)acetic acid,
s 2-( (1R,3S)-3-( (( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-2-
(1,1-dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-1-isopropy1-5a,5b,8,8, 11apentamethy1icosahydro-
1H-cyclopenta[a]chrysen-9-y1)oxy)carbony1)-2,2-
dimethylcyclopropy1)acetic acid,
2-( (1R,3S)-3-( (( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2S,3S)-2-
10 (1,1-dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-1-isopropy1-5a,5b,8,8, 11apentamethy1icosahydro-
1H-cyclopenta[a]chrysen-9-y1)oxy)carbony1)-2,2-
dimethylcyclopropy1)acetic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8,11a-pentamethy1-1-(prop-1-en-2-
15 y1)icosahydro-1H -cyclopenta[ a ]chrysen-9-y1)oxy )-2,2-dimethy1-4-oxobutanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8,11a-pentamethy1-1-(prop-1-en-2-
y1)icosahydro-1H -cyclopenta[ a ]chrysen-9-y1)oxy )-2,2-dimethy1-4-oxobutanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1,1-
20 dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8,11a-pentamethy1-1-(1-
methylcyclopropy1)icosahydro-1H-cyclopenta[a]chrysen-9-y1)oxy)-2,2-dimethy1-4-
oxobutanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-5a,5b,8,8,11a-pentamethy1-1-(1-
25 methylcyclopropy1)icosahydro-1H -cyclopenta[ a ]chrysen-9-y1)oxy )-2,2-dimethy1-4-
oxobutanoic acid,
4-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-1-isopropy1-5a,5b,8,8,11apentameth
y1icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1)ox y)-2,2-dimeth y 1-4-oxobutanoic
30 acid,
4-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((2S,3S)-2-(1,1-
dioxidothiomorpho1ino )-3-hydroxybuty1)amino )-1-isopropy1-5a,5b,8,8,11apentameth
y1icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1)ox y)-2,2-dimeth y 1-4-oxobutanoic
acid,
77
5-(((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR, 13aR, 13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5 -oxopentanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR, 13bR)-3a-(((2S,3S)-2-(1, 1-
5 dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5 -oxopentanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-
10 oxopentanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2S,3S)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-
oxopentanoic acid,
15 5-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-oxopentanoic
acid,
5-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((2S,3S)-2-(1,1-
20 dioxidothiomorpholino )-3-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-oxopentanoic
acid,
4-( (( 1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11a-
25 pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-
4-oxobutanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8, 11 a-pentamethyl-1-
(prop-1-en-2-yl)icosahydro-1H -cyclopenta[ a ]chrysen -9-yl)oxy )-2,2-dimethyl-4-oxobutanoic
30 acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl) amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
78
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8, 11 a-pentamethyl-1-
(prop-1-en-2-yl)icosahydro-1H -cyclopenta[ a ]chrysen -9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
5 (1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11apentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
10 dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-
( 1-methylcyclopropyl)icosahydro-1H -cyclopenta[ a ]chrysen -9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-1-isopropyl-
15 5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3 -(phosphonomethox y) buty 1 )amino )-1-isopropy 1-5 a,5b, 8,8, 11 apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
20 dimethylcyclobutane-1-carboxylic acid,
5-( (( 1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-
5-oxopentanoic acid,
25 5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8, 11 a-pentamethyl-1-
(prop-1-en-2-yl)icosahydro-1H -cyclopenta[ a ]chrysen -9-yl)oxy )-3 ,3-dimethyl-5-oxopentanoic
acid,
5-( (( 1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
30 ( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(1-methylcyclopropyl)icosahydro-1H-cyclopenta[ a]chrysen-9-yl)oxy)-3,3-
dimethyl-5-oxopentanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8, 11 a-pentamethyl-1-
79
( 1-methylcyclopropyl)icosahydro-1H -cyclopenta[ a ]chrysen -9-yl)oxy )-3 ,3-dimethyl-5-
oxopentanoic acid,
5-( (( 1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-1-isopropyl-
5 5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5-
oxopentanoic acid,
5-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3 -(phosphonomethox y) buty 1 )amino )-1-isopropy 1-5 a,5b, 8,8, 11 apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-oxopentanoic
10 acid,
2-( (1R,3S)-3-( (( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropyl)acetic acid,
15 2-((1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR, 13aR, 13bR)-3a-(((2R,3R)-2-
( 1, 1-dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropyl)acetic acid,
2-( (1R,3S)-3-( (( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
20 ( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11apentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclopropyl)acetic acid,
2-( (1R,3S)-3-( (( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-2-
( 1, 1-dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-5a,5b,8,8, 11a-
25 pentameth yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclopropyl)acetic acid,
2-( (1R,3S)-3-( (( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-
( ( dimethoxyphosphoryl)methoxy)-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-1-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
30 dimethylcyclopropyl)acetic acid,
2-( (1R,3S)-3-( (( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-2-
(1,1-dioxidothiomorpholino )-3-(phosphonomethoxy)butyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropyl)acetic acid,
80
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR, 13bR)-3a-(((12R,13R)-13-(1,1-
dioxidothiomorpholino )-12-methyl-2,5,8, 11-tetraoxatetradecan-14-yl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-
4-oxobutanoic acid,
5 4-(((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(((12R,13R)-13-(1,1-
dioxidothiomorpholino )-12-methyl-2,5,8, 11-tetraoxatetradecan-14-yl)amino )-5a,5b,8,8, 11apentamethyl-
1-(1-methylcyclopropyl)icosahydro-1H-cyclopenta[ a]chrysen-9-yl)oxy)-2,2-
dimethyl-4-oxobutanoic acid,
4-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR, 13aR, 13bR)-3a-(((12R, 13R)-13-(1,1-
10 dioxidothiomorpholino )-12-methyl-2,5,8, 11-tetraoxatetradecan-14-yl)amino )-1-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-2,2-dimethyl-4-
oxobutanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((12R,13R)-13-(1,1-
dioxidothiomorpholino )-12-methyl-2,5,8, 11-tetraoxatetradecan-14-yl)amino )-5a,5b,8,8, 11a-
15 pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-
5-oxopentanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((12R,13R)-13-(1,1-
dioxidothiomorpholino )-12-methyl-2,5,8, 11-tetraoxatetradecan-14-yl)amino )-5a,5b,8,8, 11apentamethyl-
1-(1-methylcyclopropyl)icosahydro-1H-cyclopenta[ a]chrysen-9-yl)oxy)-3,3-
20 dimethyl-5-oxopentanoic acid,
5-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((12R, 13R)-13-(1,1-
dioxidothiomorpholino )-12-methyl-2,5,8, 11-tetraoxatetradecan-14-yl)amino )-1-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5-
oxopentanoic acid,
25 4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((15R,16R)-16-(1,1-
dioxidothiomorpholino )-15-methyl-13-oxo-2,5,8, 11, 14-pentaoxaheptadecan-17-yl)amino )-
5a,5b,8,8, 11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-
yl)oxy)-2,2-dimethyl-4-oxobutanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((15R,16R)-16-(1,1-
30 dioxidothiomorpholino )-15-methyl-13-oxo-2,5,8, 11, 14-pentaoxaheptadecan-17-yl)amino )-
5a,5b,8,8, 11a-pentamethyl-1-( 1-methylcyclopropyl)icosahydro-1H -cyclopenta[ a]chrysen-9-
yl)oxy)-2,2-dimethyl-4-oxobutanoic acid,
4-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((15R, 16R)-16-(1,1-
dioxidothiomorpholino )-15-methyl-13-oxo-2,5,8, 11, 14-pentaoxaheptadecan-17-yl)amino )-1-
81
isopropyl-5a,5b,8,8, 11 a-pentamethylicosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )-2,2-
dimethyl-4-oxobutanoic acid,
5-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,13aR,13bR)-3a-(((15R,l6R)-16-(l,ldioxidothiomorpholino
)-15-methyl-13-oxo-2,5,8, 11, 14-pentaoxaheptadecan-17-yl)amino )-
5 5a,5b,8,8, lla-pentamethyl-1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[a]chrysen-9-
yl)oxy)-3,3-dimethyl-5-oxopentanoic acid,
5-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,13aR,13bR)-3a-(((15R,l6R)-16-(l,ldioxidothiomorpholino
)-15-methyl-13-oxo-2,5,8, 11, 14-pentaoxaheptadecan-17-yl)amino )-
5a,5b,8,8, lla-pentamethyl-1-( 1-methylcyclopropyl)icosahydro-IH -cyclopenta[ a]chrysen-9-
10 yl)oxy)-3,3-dimethyl-5-oxopentanoic acid,
5-(((lS,3aS,5aR,5bR,7aR,9S,llaR,llbR,13aR, 13bR)-3a-(((15R, 16R)-16-(l,ldioxidothiomorpholino
)-15-methyl-13-oxo-2,5,8, 11, 14-pentaoxaheptadecan-17-yl)amino )-!isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )-3,3-
dimethyl-5-oxopentanoic acid,
15 (1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((S)-3-amino-2-
(1,1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-l-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((S)-3-amino-2-
20 (1,1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(lmethylcyclopropyl)
icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lS,3aS,5aR,5bR,7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ( (S)-3-amino-2-
(1,1-dioxidothiomorpholino )propyl)amino )-l-isopropyl-5a,5b,8,8, lla-
25 pentamethylicosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-
amino-2-(l, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-l-en-
2-yl)icosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
30 carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-
amino-2-(l, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(lmethylcyclopropyl)
icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
82
(1R,3S)-3-(( ( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-
amino-2-(1, 1-dioxidothiomorpholino )butyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
5 (1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-( (tertbutoxycarbonyl)
amino )-2-( 1, 1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-( (tert-
10 butoxycarbonyl)amino )-2-( 1, 1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8, 11apentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (R)-3-( (tertbutoxycarbonyl)
amino )-2-( 1, 1-dioxidothiomorpholino )propyl)amino )-1-isopropyl-
15 5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-((tertbutoxycarbonyl)
amino )-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
20 dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-((tertbutoxycarbonyl)
amino )-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11apentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
25 (1R,3S)-3-(( ( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (2R,3R)-3-( (tertbutoxycarbonyl)
amino )-2-( 1, 1-dioxidothiomorpholino )butyl)amino )-1-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
30 dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )propyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR, 13aR, 13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )propyl)amino )-5a,5b,8,8, 11a83
pentameth yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, liaR, llbR, 13aR, 13bR)-3a-(((R)-2-(l, 1-
dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )propyl)amino )-l-isopropyl-5a,5b,8,8, lia-
S pentamethylicosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,l3aR,l3bR)-3a-(((2R,3R)-2-(l, 1-
dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )butyl) amino )-5a,5b,8,8, lla-pentamethyl-
1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[ a]chrysen-9-yl)oxy)carbonyl)-2,2-
10 dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,l3aR,l3bR)-3a-(((2R,3R)-2-(l, 1-
dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )butyl) amino )-5a,5b,8,8, lla-pentamethyl-
1-( 1-methylcyclopropyl)icosahydro-1 H -cyclopenta[ a ]chrysen -9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
15 (lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((2R,3R)-2-(l,ldioxidothiomorpholino
)-3-( ( ethoxycarbonyl)amino )butyl) amino )-l-isopropyl-5a,5b,8,8, llapentamethylicosahydro-
IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
20 dioxidothiomorpholino )-3-( (isopropoxycarbonyl)amino )propyl)amino )-5a,5b,8,8, llapentamethyl-
1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-3-( (isopropoxycarbonyl)amino )propyl)amino )-5a,5b,8,8, lla-
25 pentameth yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((R)-2-(l, 1-
dioxidothiomorpholino )-3-( (isopropoxycarbonyl)amino )propyl)amino )-l-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
30 dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,l3aR,l3bR)-3a-(((2R,3R)-2-(l, 1-
dioxidothiomorpholino )-3-( (isopropoxycarbonyl)amino )butyl)amino )-5a,5b,8,8, llapentamethyl-
1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
84
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-( (isopropoxycarbonyl)amino )butyl)amino )-5a,5b,8,8, 11apentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
5 (1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR,13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-( (isopropoxycarbonyl)amino )butyl)amino )-1-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR, 13aR, 13bR)-3a-(((R)-2-(1,1-
10 dioxidothiomorpholino )-3-( ((2-methoxyethoxy)carbonyl)amino )propyl)amino )-
5a,5b,8,8, 11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino)-3-(((2-methoxyethoxy)carbonyl)amino)propyl)amino)-
15 5 a,5b, 8,8, 11 a-pentamethy 1-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((R)-2-(1, 1-
dioxidothiomorpholino )-3-( ((2-methoxyethoxy)carbonyl)amino )propyl)amino )-1-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
20 dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-( ((2-methoxyethoxy)carbonyl)amino )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
25 (1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-( ((2-methoxyethoxy)carbonyl)amino )butyl)amino )-5a,5b,8,8, 11apentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2R,3R)-2-(1,1-
30 dioxidothiomorpholino )-3-( ((2-methoxyethoxy)carbonyl)amino )butyl)amino )-1-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((R)-12-(1,1-
dioxidothiomorpholino )-9-oxo-2,5,8-trioxa-1 0-azatridecan-13-yl)amino )-5a,5b,8,8, 11a85
pentamethyl-1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,13aR,13bR)-3a-(((R)-12-(l,ldioxidothiomorpholino
)-9-oxo-2,5,8-trioxa-1 0-azatridecan-13-yl)amino )-5a,5b,8,8, lia-
S pentameth yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((R)-12-(l, 1-
dioxidothiomorpholino )-9-oxo-2,5,8-trioxa-10-azatridecan-13-yl)amino )-l-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
10 dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,13aR,13bR)-3a-(((llR, 12R)-12-
( 1, 1-dioxidothiomorpholino )-11-methyl-9-oxo-2,5 ,8-trioxa-1 0-azatridecan-13-yl)amino )-
5a,5b,8,8, lla-pentamethyl-1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[a]chrysen-9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
15 (lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR,llbR,13aR,13bR)-3a-(((llR,l2R)-l2-
( 1, 1-dioxidothiomorpholino )-11-methyl-9-oxo-2,5 ,8-trioxa-1 0-azatridecan-13-yl)amino )-
5a,5b,8,8, lla-pentamethyl-1-( 1-methylcyclopropyl)icosahydro-IH -cyclopenta[ a]chrysen-9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((llR,l2R)-12-
20 ( 1, 1-dioxidothiomorpholino )-11-methyl-9-oxo-2,5 ,8-trioxa-1 0-azatridecan-13-yl)amino )-lisopropyl-
5a,5b,8,8,lla-pentamethylicosahydro-1H-cyclopenta[a]chrysen-9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )propyl)amino )-5a,5b,8,8, lla-
25 pentamethyl-1-(prop-1-en-2-yl)icosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )propyl)amino )-5a,5b,8,8, llapentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
30 yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((R)-2-(l, 1-
dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )propyl)amino )-l-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
86
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
5 (1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1, 1-
dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )butyl)amino )-5a,5b,8,8, 11apentameth
yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((2R,3R)-2-(1,1-
10 dioxidothiomorpholino )-3-((1-methylethyl)sulfonamido )butyl)amino )-1-isopropyl-
5a,5b,8,8, 11 a-pentamethylicosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR, 13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-3-(methylthio )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
15 en-2-yl)icosahydro-1H -cyclopenta[ a]chrysen-9-yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR, 13aR, 13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-3-(methylthio )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
20 dimethylcyclobutane-1-carboxylic acid,
25
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR, 13aR, 13bR)-3a-(((S)-2-(1, 1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
en-2-yl)icosahydro-1H -cyclopenta[ a ]chrysen -9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((S)-2-(1,1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((S)-3-amino-2-(1, 1-
30 dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-2,2-dimethyl-4-oxobutanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR, 13aR, 13bR)-3a-(((S)-3-amino-2-(1, 1-
dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5 -oxopentanoic acid,
87
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-3-amino-2-(1, 1-
dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-2,2-dimethyl-4-oxobutanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-3-amino-2-(1, 1-
5 dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5 -oxopentanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )propyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-
10 4-oxobutanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )propyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-
5-oxopentanoic acid,
15 4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )butyl) amino )-5a,5b,8,8, 11a-pentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[ a]chrysen-9-yl)oxy)-2,2-dimethyl-4-
oxobutanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1,1-
20 dioxidothiomorpholino )-3-( ( ethoxycarbonyl)amino )butyl) amino )-5a,5b,8,8, 11a-pentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[ a]chrysen-9-yl)oxy)-3,3-dimethyl-5-
oxopentanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )propyl)amino )-5a,5b,8,8, 11a-
25 pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-
4-oxobutanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )propyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-
30 5-oxopentanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-
4-oxobutanoic acid,
88
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((2R,3R)-2-(1,1-
dioxidothiomorpholino )-3-( (1-methylethyl)sulfonamido )butyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-
5-oxopentanoic acid,
5 4-(((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-3-(methylthio )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-oxobutanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR, 13aR,13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-3-(methylthio )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
10 en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-oxopentanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((S)-2-(1, 1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-oxobutanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((S)-2-(1, 1-
15 dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-oxopentanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((S)-2-(1, 1-
dioxidothiomorpholino )-3-(methylthio )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-oxobutanoic acid,
20 4-(((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(((S)-2-(1,1-
dioxidothiomorpholino )-3-(methylthio )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-
oxobutanoic acid,
4-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((S)-2-(1,1-
25 dioxidothiomorpholino )-3-(methylthio )propyl)amino )-1-isopropyl-5a,5b,8,8, 11apentameth
ylicosah ydro-1 H -cyclopenta[ a] chrysen -9-y l)ox y)-2,2-dimeth y 1-4-oxobutanoic
acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
30 en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-oxobutanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-
oxobutanoic acid,
89
4-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((R)-2-(1, 1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-1-isopropyl-5a,5b,8,8, 11apentameth
ylicosah ydro-1 H -cyclopenta[ a] chrysen -9-y l)ox y)-2,2-dimeth y 1-4-oxobutanoic
acid,
5 5-(((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-oxopentanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
10 methylcyclopropyl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5-
oxopentanoic acid,
5-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((R)-2-(1, 1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-1-isopropyl-5a,5b,8,8, 11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-oxopentanoic
15 acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
en-2-yl)icosahydro-1H -cyclopenta[ a ]chrysen -9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
20 (1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
en-2-yl)icosahydro-1H -cyclopenta[ a ]chrysen -9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
2-((1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR, 13aR, 13bR)-3a-(((R)-2-(1,1-
25 dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropyl)acetic acid,
2-((1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR, 13aR, 13bR)-3a-(((S)-2-(1, 1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
30 en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropyl)acetic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-3-hydroxypropyl)amino )-5a,5b,8,8, 11a-pentamethyl-1-(prop-1-en-2-
90
yl)icosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclopropane-1-
carboxylic acid,
(lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,13aR,13bR)-3a-(((S)-2-(l, 1-
dioxidothiomorpholino )-3-hydroxypropyl)amino )-5a,5b,8,8, lla-pentamethyl-1-(prop-1-en-2-
5 y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((2R,3S)-2-( 1,1-
dioxidothiomorpholino )-3-fluorobutyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-l-en-2-
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
10 carboxylic acid,
(1S,3R)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((2R,3S)-2-( 1,1-
dioxidothiomorpholino )-3-fluorobutyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-l-en-2-
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxylic acid,
15 (lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,13aR,13bR)-3a-(((R)-2-(l,ldioxidothiomorpholino
)-3-fluoropropyl)amino )-5a,5b,8,8, lla-pentamethyl-1-(prop-1-en-2-
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxylic acid,
(lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,13aR,13bR)-3a-(((S)-2-(l, 1-
20 dioxidothiomorpholino )-3-fluoropropyl)amino )-5a,5b,8,8, lla-pentamethyl-1-(prop-1-en-2-
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((S)-3-amino-2-
(1,1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-l-en-2-
25 y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-amino-2-
(1,1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-l-en-2-
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
30 carboxylic acid,
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-
amino-2-(l, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-l-en-
2-yl)icosahydro-IH -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclopropane-1-
carboxylic acid,
91
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2S,3S)-3-
amino-2-(1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-
2-yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclopropane-1-
carboxylic acid,
5 (1S,3R)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2R,3R)-3-
amino-2-(1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-
2-yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclopropane-1-
carboxylic acid,
(1S,3R)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((2S,3S)-3-
10 amino-2-(1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-
2-yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclopropane-1-
carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
dioxidothiomorpholino )-3-(methylthio )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
15 en-2-y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbonyl)-2,2-dimeth y lcyclopropane-
1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((S)-2-(1, 1-
dioxidothiomorpholino )-3-(methylthio )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
en-2-y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbonyl)-2,2-dimeth y lcyclopropane-
20 1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((S)-2-(1, 1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
en-2-y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )ox y )carbonyl)-2,2-dimeth y lcyclopropane-
1-carboxylic acid,
25 (1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((R)-2-(1,1-
dioxidothiomorpholino )-4-(methylthio )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-
en-2-y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbonyl)-2,2-dimeth y lcyclopropane-
1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-( 1,1-
30 dioxidothiomorpholino )-3-methylbutyl)amino )-5a,5b,8,8, 11a-pentamethyl-1-(prop-1-en-2-
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxylic acid, and
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((S)-2-(1, 1-
dioxidothiomorpholino )-3-methylbutyl)amino )-5a,5b,8,8, 11a-pentamethyl-1-(prop-1-en-2-
92
5
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxylic acid, or
pharmaceutically acceptable salts, pharmaceutically acceptable stereoisomers,
prodrugs, or combination thereof.
7. A compound selected from the group consisting of:
5-(((lR,3aS,5aR,5bR,7aR,9S, liaR, llbR,l3aR,l3bR)-3a-((3-(l, 1-
dioxidothiomorpholino )-4-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
10 yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5 -oxopentanoic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((3S,4R)-2-( 1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
15 (1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,l3aR,l3bR)-3a-(((12S,l3S)-13-
(1,1-dioxidothiomorpholino )-12-methyl-10-oxo-2,5,8,11-tetraoxapentadecan-15-yl)amino )-
5a,5b,8,8, 11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((3R,4S)-3-( 1,1-
20 dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((3S,4S)-3-(1,1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-1-isopropyl-5a,5b,8,8, 11 a-
25 pentamethylicosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((3R,4S)-3-(1, 1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-1-isopropyl-5a,5b,8,8, 11 apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
30 dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,l3aR,l3bR)-3a-(((3S,4S)-3-(1, 1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
93
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((3R,4S)-3-( 1,1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
5 (1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((3R,4R)-3-(1, 1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1S,3R)-3-((((1S,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((3R,4R)-3-(1, 1-
10 dioxidothiomorpholino )-4-hydroxypentyl)amino )-1-isopropyl-5a,5b,8,8, 11 apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1S,3R)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((3R,4R)-3-(1, 1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
15 me thy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )carbon y 1 )-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((3R,4R)-3-(1, 1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbony 1)-2,2-dimeth ylcyclopropane-1-
20 carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((3R,4R)-3-(1,1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-1-isopropyl-5a,5b,8,8, 11 apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropane-1-carboxylic acid,
25 (1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((3R,4R)-3-(1, 1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-( 1,1-
30 dioxidothiomorpholino )-4-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-4-amino-3-
(1,1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
94
y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxylic acid,
(lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((R)-3-(l, 1-
dioxidothiomorpholino )-4-hydroxybutyl)amino )-l-isopropyl-5a,5b,8,8,lla-
5 pentamethylicosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropane-1-carboxylic acid,
(1R,3S)-3-(( ( (lS,3aS,5aR,5bR,7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ( (R)-4-amino-3-
(1,1-dioxidothiomorpholino )butyl)amino )-l-isopropyl-5a,5b,8,8,lla-pentamethylicosahydrol
H -cyclopenta[ a] chrysen -9-y 1 )ox y )carbon y 1 )-2,2-dimethy lcyclopropane-1-carbox y lie acid,
10 (lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,l3aR,l3bR)-3a-(((R)-3-(l,ldioxidothiomorpholino
)-4-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-4-amino-3-
15 (1,1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-( 1,1-
dioxidothiomorpholino )-4-fluorobutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
20 y 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-y 1 )oxy )carbon y 1)-2,2-dimeth ylcyclopropane-1-
carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((R)-3-(1, 1-
dioxidothiomorpholino )-4-fluorobutyl)amino )-1-isopropyl-5a,5b,8,8, 11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
25 dimethylcyclopropane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-( 1,1-
dioxidothiomorpholino )-4-fluorobutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )carbon y 1)-2,2-
dimethylcyclopropane-1-carboxylic acid,
30 (1S,3R)-3-(2-(((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,l3aR,l3bR)-3a-(((3R,4R)-3-
(1,1-dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8, 11a-pentamethyl-1-(prop-1-
en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2-oxoethyl)-2,2-
dimethylcyclopropane-1-carboxylic acid,
95
2-( (1R,3S)-3-( (( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (3R,4R)-3-
(1,1-dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8, 11a-pentamethyl-1-(prop-1-
en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclopropyl)acetic acid,
5 4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((3R,4R)-3-(1,1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-2,2-dimethyl-4-oxobutanoic acid,
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((3R,4R)-3-(1,1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-1-(prop-1-
10 en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-oxobutanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((3S,4R)-2-(1,1-
dioxidothiomorpholino )-3-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-2,2-dimethyl-4-oxobutanoic acid,
4-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((3R,4R)-3-(1, 1-
15 dioxidothiomorpholino )-4-hydroxypentyl)amino )-1-isopropyl-5a,5b,8,8, 11 apentameth
ylicosah ydro-1 H -cyclopenta[ a] chrysen -9-y l)ox y)-2,2-dimeth y 1-4-oxobutanoic
acid,
4-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((3R,4S)-3-(1, 1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-1-isopropyl-5a,5b,8,8, 11 a-
20 pentamethylicosahydro-1 H -cyclopenta[ a ]chrysen -9-yl)oxy )-2,2-dimethyl-4-oxobutanoic
acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((3R,4R)-3-(1,1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-
25 oxobutanoic acid,
4-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR, 13aR, 13bR)-3a-(((3R,4S)-3-(1,1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-
oxobutanoic acid,
30 5-(((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(((3R,4R)-3-(1,1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5 -oxopentanoic acid,
96
5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((3R,4S)-3-(1,1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )-3 ,3-dimethyl-5 -oxopentanoic acid,
5-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((3R,4R)-3-(1, 1-
5 dioxidothiomorpholino )-4-hydroxypentyl)amino )-1-isopropyl-5a,5b,8,8, 11 apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-oxopentanoic
acid,
5-(((1S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR, 13bR)-3a-(((3R,4S)-3-(1, 1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-1-isopropyl-5a,5b,8,8, 11 a-
10 pentamethylicosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-oxopentanoic
acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((R)-3-(1, 1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-
oxopentanoic acid,
15 5-(((1R,3aS,5aR,5bR,7aR,9S, 11aR, 11bR,13aR,13bR)-3a-(((3R,4S)-3-(1,1-
dioxidothiomorpholino )-4-hydroxypentyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)-3,3-dimethyl-5-
oxopentanoic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-( 1,1-
20 dioxidothiomorpholino )-4-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-4-
( ( dimethoxyphosphoryl)oxy)-3-( 1, 1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8, 11a-
25 pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((R)-13-(1,1-
dioxidothiomorpholino )-10-oxo-2,5,8, 11-tetraoxapentadecan-15-yl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
30 dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((S)-3-(1,1-
dioxidothiomorpholino )-4-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
97
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((R)-3-(1, 1-
dioxidothiomorpholino )-4-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
5 (1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((S)-3-(1,1-
dioxidothiomorpholino )-4-hydroxybutyl)amino )-1-isopropyl-5a,5b,8,8,11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((S)-3-(1,1-
10 dioxidothiomorpholino )-4-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbony 1)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((R)-13-(1,1-
dioxidothiomorpholino )-10-oxo-2,5,8, 11-tetraoxapentadecan-15-yl)amino )-5a,5b,8,8, 11a-
15 pentameth yl-1-( 1-meth y lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((S)-3-(1, 1-
dioxidothiomorpholino )-4-hydroxybutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
20 dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-4-amino-3-
(1,1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
25 (1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((R)-3-(1,1-
dioxidothiomorpholino )-4-( ( ethoxycarbonyl)amino )butyl)amino )-5a,5b,8,8, 11a-pentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[ a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((S)-4-amino-3-
30 (1,1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
98
(1R,3S)-3-(( ( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (R)-4-amino-3-
(1,1-dioxidothiomorpholino )butyl)amino )-1-isopropyl-5a,5b,8,8,11a-pentamethylicosahydro-
1H -cyclopenta[ a ]chrysen -9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (S)-4-amino-3-
5 (1,1-dioxidothiomorpholino )butyl)amino )-1-isopropyl-5a,5b,8,8,11a-pentamethylicosahydro-
1H -cyclopenta[ a ]chrysen -9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
( 1R,3S)-3-( (( ( 1R,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (R)-4-amino-3-
(1,1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
10 dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((S)-4-amino-3-
(1,1-dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methylcyclopropyl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
15 (1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-amino-3-
(1,1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-( 1,1-
20 dioxidothiomorpholino )-2-( ( ethoxycarbonyl)amino )propyl)amino )-5a,5b,8,8, 11apentamethyl-
1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-( 1,1-
dioxidothiomorpholino)-2-(((2-methoxyethoxy)carbonyl)amino)propyl)amino)-
25 5a,5b,8,8, 11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-
yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((S)-2-amino-3-
(1,1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
30 carboxylic acid,
(1R,3S)-3-(( ( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (R)-2-amino-3-
(1,1-dioxidothiomorpholino )propyl)amino )-1-isopropyl-5a,5b,8,8, 11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
99
(1R,3S)-3-(( ( (1S,3aS,5aR,5bR,7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ( (S)-2-amino-3-
(1,1-dioxidothiomorpholino )propyl)amino )-1-isopropyl-5a,5b,8,8, 11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
5 (1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-2-amino-3-
(1,1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )carbon y 1 )-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((S)-2-amino-3-
10 (1,1-dioxidothiomorpholino )propyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )carbon y 1 )-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-( 1,1-
dioxidothiomorpholino )-4-fluorobutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
15 yl)icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((S)-3-(1, 1-
dioxidothiomorpholino )-4-fluorobutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
20 carboxylic acid,
(1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((R)-3-(1, 1-
dioxidothiomorpholino )-4-fluorobutyl)amino )-1-isopropyl-5a,5b,8,8, 11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
25 (1R,3S)-3-((((1S,3aS,5aR,5bR,7aR,9S, 11aR,11bR, 13aR, 13bR)-3a-(((S)-3-(1,1-
dioxidothiomorpholino )-4-fluorobutyl)amino )-1-isopropyl-5a,5b,8,8, 11apentamethylicosahydro-
1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-(( ( (1R,3aS,5aR,5bR, 7 aR,9S, 11aR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-( 1,1-
30 dioxidothiomorpholino )-4-fluorobutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
methy lcyclopropy 1 )icosah ydro-1 H -cyclopenta[ a] chrysen -9- y 1 )ox y )carbon y 1 )-2,2-
dimethylcyclobutane-1-carboxylic acid,
(1R,3S)-3-((((1R,3aS,5aR,5bR,7aR,9S,11aR, 11bR,13aR,13bR)-3a-(((S)-3-(1, 1-
dioxidothiomorpholino )-4-fluorobutyl)amino )-5a,5b,8,8,11a-pentamethyl-1-(1-
100
methylcyclopropyl)icosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid,
(lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,13aR,13bR)-3a-(((S)-3-(l, 1-
dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-l-en-2-
5 yl)icosahydro-IH-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid,
(lR,3S)-3-((((lS,3aS,5aR,5bR,7aR,9S, llaR,llbR, 13aR, 13bR)-3a-(((S)-3-(l,ldioxidothiomorpholino
)butyl)amino )-l-isopropyl-5a,5b,8,8, lla-pentamethylicosahydro-IHcyclopenta[
a ]chrysen -9-y l)oxy )carbonyl)-2,2-dimethylcyclobutane-1-carboxylic acid,
10 (lR,3S)-3-((((lR,3aS,5aR,5bR,7aR,9S,llaR, llbR,13aR,13bR)-3a-(((S)-3-(l, 1-
dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(lmethylcyclopropyl)
icosahydro-1H-cyclopenta[a]chrysen-9-yl)oxy)carbonyl)-2,2-
dimethylcyclobutane-1-carboxylic acid, and
(1R,3S)-3-(( ( (lR,3aS,5aR,5bR, 7 aR,9S, liaR, 11 bR, 13aR, 13bR)-3a-( ((R)-3-( 1,1-
15 dioxidothiomorpholino )butyl)amino )-5a,5b,8,8,lla-pentamethyl-l-(prop-l-en-2-
yl)icosahydro-1H -cyclopenta[ a ]chrysen-9-yl)oxy )carbonyl)-2,2-dimethylcyclobutane-1-
carboxylic acid, or
pharmaceutically acceptable salts, pharmaceutically acceptable stereoisomers, prodrugs, or
combination thereof.
20 8. A pharmaceutical composition comprising a compound according to any one of
claims 1-7 and at least one pharmaceutically acceptable excipient.
9. The pharmaceutical composition according to claim 8, wherein the
pharmaceutically acceptable excipient is a carrier or diluent.
10. A method for preventing, ameliorating or treating a viral mediated disease,
25 disorder or syndrome in a subject in need thereof comprising administering to the subject a
therapeutically effective amount o fa compound according to any one of claims 1-7.
11. The method according to claim 10, wherein the viral mediated disease, disorder or
syndrome is HIV infection, HBV infection, HCV infection , a retroviral infection genetically
related to AIDS, respiratory disorders (including adult respiratory distress syndrome
30 (ARDS)), inflammatory disease, or a combination thereof.
12. A method of treating HIV in a subject in need thereof comprising administering to
the subject a therapeutically effective amount o fa compound according to any one of claims
1-7.
Dated this 04th day of August, 2022
Manisha Singh
Agent for the Applicant [IN/PA-740]
LEXORBIS
101
13. A method for preventing, ameliorating or treating a viral mediated disease,
disorder or syndrome in a subject in need thereof comprising administering to the subject the
pharmaceutical composition according to claims 8-9, comprising a therapeutically effective
amount of the compound.
5 14. The method according to claim 13, wherein the viral mediated disease, disorder or
10
15
20
syndrome is HIV infection, HBV infection, HCV infection, a retroviral infection genetically
related to AIDS, respiratory disorders (including adult respiratory distress syndrome
(ARDS)), inflammatory disease, or a combination thereof.