Jie Li

US Patent:

6869958, Mar 22, 2005

Filed:

Aug 5, 2003

Appl. No.:

10/634181

Inventors:

Jie Jack Li - Ann Arbor MI, US

Assignee:

Warner-Lambert Company - Morris Plains NJ

International Classification:

A61K031/519
C07D471/04

US Classification:

514258, 544279

Abstract:

This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof,.

US Patent:

20030004172, Jan 2, 2003

Filed:

Feb 13, 2002

Appl. No.:

10/075073

Inventors:

William Harter - Chelsea MI, US
Jie Li - Ann Arbor MI, US
Daniel Ortwine - Saline MI, US
Kevon Shuler - Chelsea MI, US
Wen-Song Yue - Ypsilanti MI, US

International Classification:

A61K031/522
A61K031/519
C07D491/02
C07D473/02

US Classification:

514/260100, 514/263340, 514/263330, 514/265100, 544/256000, 544/267000, 544/271000, 544/280000

Abstract:

Selective MMP-13 inhibitors are fused pyrimidinones of the formula or a pharmaceutically acceptable salt thereof, wherein: W, together with the carbon atoms to which it is attached, form a 5-membered ring diradical X is O, S, SO, SO, NR, or CH; B is O or NR; or A and B are taken together to form —C≡C—; R, R, and Rare hydrogen, alkyl, alkenyl, alkynyl, (CH)aryl, (CH)cycloalkyl, C-Calkanoyl, or (CH)heteroaryl; Rand Rare hydrogen, alkyl, alkenyl, alkynyl CN, NO, NRR, (CH)cycloalkyl, (CH)aryl, or (CH)heteroaryl; Rmay further be halo; n is an integer of from 0 to 5; and Rand Rwhen taken together with a nitrogen to which they are both attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing O, S, or N, and substituted or unsubstituted; with the proviso that Rand Rare not both selected from hydrogen and C-Calkyl.

US Patent:

20030220355, Nov 27, 2003

Filed:

Apr 16, 2003

Appl. No.:

10/417073

Inventors:

Bernard Gaudilliere - Nanterre, FR
Henry Jacobelli - Paray Vieille Poste, FR
Catherine Kostlan - Saline MI, US
Jie Li - Ann Arbor MI, US
Wen-Song Yue - Ann Arbor MI, US

International Classification:

A61K031/517
C 07D 4 3/02
C07D239/72

US Classification:

514/266200, 514/266300, 544/284000, 544/286000

Abstract:

A compound selected from those of formula (I): wherein: X, X, and X, represent N or —CRin which Ris as described in the description, Grepresents a group selected from those of formulae (i/a) and (i/b): in which R, R, and Rare as defined in the description, Grepresents a group selected from carbon-carbon triple bond, —CH C CH—, C O, C S, S(O)in which n1 represents an integer from 0 to 2 inclusive, or a group of formula (i/c): in which Yrepresents O, S, —NH or —Nalkyl, and Yrepresents O, S, —NH or —Nalkyl, n is an integer from 0 to 6 inclusive, and m is an integer from 0 to 7 inclusive, Zrepresents —CRRwherein Rand Rare as defined in the description, A represents a ring system, Rrepresents a group selected from H, alkyl, alkenyl, alkynyl, optionally substituted and the group of formula (i/d): in which p, Z, B, q and Gare as defined in the description and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix mettaloprotease.

US Patent:

20040043983, Mar 4, 2004

Filed:

Aug 5, 2003

Appl. No.:

10/634182

Inventors:

Jie Li - Ann Arbor MI, US

International Classification:

C07D471/02
C07D487/02
A61K031/53
A61K031/519
A61K031/4745

US Classification:

514/210210, 544/184000, 514/243000, 514/249000, 514/248000, 514/264100, 514/300000, 544/236000, 544/279000, 544/350000, 546/122000

Abstract:

This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R, Q, Y, Y, U, U, U, R, and Rare as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency, inflammatory bowel disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active component as described in the specification.

US Patent:

20060040957, Feb 23, 2006

Filed:

Feb 8, 2002

Appl. No.:

10/071032

Inventors:

Richard Dyer - Ann Arbor MI, US
William Harter - Chelsea MI, US
James Hicks - Chelsea MI, US
Adam Johnson - Ann Arbor MI, US
Jie Li - Ann Arbor MI, US
William Roark - Ann Arbor MI, US
Kevon Shuler - Chelsea MI, US

International Classification:

A61K 31/519
C07D 498/04

US Classification:

514259200, 544278000

Abstract:

Selective MMP-13 inhibitors are bicyclic pyrimidines of the Formula I or a pharmaceutically acceptable salt thereof, wherein Ris hydrogen or alkyl; R, R, and Rinclude hydrogen, halo, alkyl, C≡C(CH)aryl, COalkyl, CO(CH)aryl, COHN alkyl, and CONH(CH)aryl; and X is O, S, SO, SO, CH, C═O, CHOH, NH, or NR. A compound of Formula I, or a pharmaceutically acceptable salt thereof, is useful for treating cancer or arthritis.