Glutamate Aggrecanase Inhibitors

Abstract: The present invention relates to compounds of the formula (I), which are modulators of metalloproteinase activity, and pharmaceutically acceptable salts thereof, wherein W is -C(O)-, -OC(O)-, -NHC(O)-, -C(O)O-, Or -C(O)NH-; R1 is phenyl, heteroaryl, biphenyl, bicyciic aryi, tricyclic aryl, bicyclic heteroaryl or tricyclic heteroaryl, each optionally substituted with one or more of R5 or R6, and when R1 is substituted with more than one of R5 or Re, the substituents can be identical or different; R2 is hydrogen, (C1 -C6) alkyl, (C2-C6) alkenyl, (C2-C6)alkynyl, -(CH2)nR11, -OH, or -0-(C1-C6) alkyl; R3 is -CO2H, -CONH2, -CONHOH, -CONHSO2R7, tetrazole, -SO2NHR7, -SO3H, -PO(OH)NH2, -PO(OH)OR7, -CONHR7, -COOR7, an acid mimetic group, or a 5 or 6-membered heterocycloalkyl or heteroaryl containing 1 to 4 heteroatoms selected from O, N, S; R4 is -CO2H, -CONH2, -(CH2)nOR7, or -CONR9R10;

Patent Information

Application #

Filing Date

24 December 2007

Publication Number

19/2008

Publication Type

INA

Invention Field

PHARMACEUTICALS

Status

Email

Parent Application

Applicants

WYETH

FIVE GIRALDA GARMS MADISON, NJ

Inventors

1. SUM PHAIK-ENG

16 CHAMBERLAIN COURT, POMONA, NY 10970

2. HOW DAVID BRIAN

10 HIGH AVENUE, NYACK, NY 10960

3. SABATINI JOSHUA JAMES

12 OLD MAMARONECK ROAD, APT. 7G, WHITE PLAINS, NY 10605

4. XIANG JASON SHAOYUN

3 RIVER STREET, WINCHESTER, MA 01890

5. IPEK MANUS

197 SCHOOL STREET, WATERTOWN, MA 02472

6. FEYFANT ERIC

41 KENDELL ROAD, LEXINGTON, MA 02421

Specification

The present invention relates to compounds of the formula (I), which are modulators of metalloproteinase activity, and pharmaceutically acceptable salts thereof, wherein W is -C(O)-, -OC(O)-, -NHC(O)-, -C(O)O-, Or -C(O)NH-; R1 is phenyl, heteroaryl, biphenyl, bicyciic aryi, tricyclic aryl, bicyclic heteroaryl or tricyclic heteroaryl, each optionally substituted with one or more of R5 or R6, and when R1 is substituted with more than one of R5 or Re, the substituents can be identical or different; R2 is
hydrogen, (C1 -C6) alkyl, (C2-C6) alkenyl, (C2-C6)alkynyl, -(CH2)nR11, -OH, or -0-(C1-C6) alkyl; R3 is -CO2H, -CONH2, -CONHOH,
-CONHSO2R7, tetrazole, -SO2NHR7, -SO3H, -PO(OH)NH2, -PO(OH)OR7, -CONHR7, -COOR7, an acid mimetic group, or a 5 or
6-membered heterocycloalkyl or heteroaryl containing 1 to 4 heteroatoms selected from O, N, S; R4 is -CO2H, -CONH2, -(CH2)nOR7,
or -CONR9R10;

Documents

Application Documents

#	Name	Date
1	4985-KOLNP-2007-EXAMINATION REPORT-1.1.pdf	2018-10-12
1	abstract-04985-kolnp-2007.jpg	2011-10-08
2	4985-kolnp-2007-form 18.pdf	2011-10-08
2	4985-KOLNP-2007-OTHERS-1.pdf	2018-10-12
3	4985-KOLNP-2007-CORRESPONDENCE-1.1.pdf	2011-10-08
3	4985-KOLNP-2007 ABANDONED LETTER.pdf	2017-06-23
4	4985-KOLNP-2007-ANEXURE TO FORM 3.pdf	2011-10-08
4	4985-KOLNP-2007 ASSIGNMENT.pdf	2017-06-23
5	4985-KOLNP-2007 CORRESPONDENCE.pdf	2017-06-23
5	04985-kolnp-2007-pct request form.pdf	2011-10-08
6	4985-KOLNP-2007 DESCRIPTION.pdf	2017-06-23
6	04985-kolnp-2007-pct priority document notification.pdf	2011-10-08
7	4985-KOLNP-2007 FIRST EXAMINATION REPORT.pdf	2017-06-23
7	04985-kolnp-2007-international search report.pdf	2011-10-08
8	4985-KOLNP-2007 INTERNATIONAL PUBLICATION.pdf	2017-06-23
8	04985-kolnp-2007-gpa.pdf	2011-10-08
9	04985-kolnp-2007-form 5.pdf	2011-10-08
9	4985-KOLNP-2007_EXAMREPORT.pdf	2016-06-30
10	04985-kolnp-2007-abstract.pdf	2011-10-08
10	04985-kolnp-2007-form 3.pdf	2011-10-08
11	04985-kolnp-2007-claims.pdf	2011-10-08
11	04985-kolnp-2007-form 1.pdf	2011-10-08
12	04985-kolnp-2007-correspondence others.pdf	2011-10-08
12	04985-kolnp-2007-drawings.pdf	2011-10-08
13	04985-kolnp-2007-correspondence others.pdf	2011-10-08
13	04985-kolnp-2007-drawings.pdf	2011-10-08
14	04985-kolnp-2007-claims.pdf	2011-10-08
14	04985-kolnp-2007-form 1.pdf	2011-10-08
15	04985-kolnp-2007-abstract.pdf	2011-10-08
15	04985-kolnp-2007-form 3.pdf	2011-10-08
16	04985-kolnp-2007-form 5.pdf	2011-10-08
16	4985-KOLNP-2007_EXAMREPORT.pdf	2016-06-30
17	4985-KOLNP-2007 INTERNATIONAL PUBLICATION.pdf	2017-06-23
17	04985-kolnp-2007-gpa.pdf	2011-10-08
18	4985-KOLNP-2007 FIRST EXAMINATION REPORT.pdf	2017-06-23
18	04985-kolnp-2007-international search report.pdf	2011-10-08
19	4985-KOLNP-2007 DESCRIPTION.pdf	2017-06-23
19	04985-kolnp-2007-pct priority document notification.pdf	2011-10-08
20	4985-KOLNP-2007 CORRESPONDENCE.pdf	2017-06-23
20	04985-kolnp-2007-pct request form.pdf	2011-10-08
21	4985-KOLNP-2007-ANEXURE TO FORM 3.pdf	2011-10-08
21	4985-KOLNP-2007 ASSIGNMENT.pdf	2017-06-23
22	4985-KOLNP-2007-CORRESPONDENCE-1.1.pdf	2011-10-08
22	4985-KOLNP-2007 ABANDONED LETTER.pdf	2017-06-23
23	4985-KOLNP-2007-OTHERS-1.pdf	2018-10-12
23	4985-kolnp-2007-form 18.pdf	2011-10-08
24	abstract-04985-kolnp-2007.jpg	2011-10-08
24	4985-KOLNP-2007-EXAMINATION REPORT-1.1.pdf	2018-10-12