Donald M Harper

US Patent:

6437177, Aug 20, 2002

Filed:

Nov 20, 1998

Appl. No.:

09/196190

Inventors:

Martha A. Warpehoski - Portage MI 49024
Mark Allen Mitchell - Kalamazoo MI 49008
Donald E. Harper - Plainwell MI 49080
Linda Louise Maggiora - Kalamazoo MI 49008

International Classification:

C07C31704

US Classification:

562426, 562470, 562496, 562508, 562581, 562605

Abstract:

The present invention provides a compound of formula I or pharmaceutical acceptable salts thereof wherein R is C alkyl, C alkenyl, C alkynyl, â(CH ) âC cycloalkyl, substituted and unsubstituted â(CH ) -aryl, substituted and unsubstituted â(CH ) -het, R is substituted and unsubstituted C alkyl, substituted and unsubstituted C alkenyl, substituted and unsubstituted C alkynyl, substituted and unsubstituted â(CH ) âC cycloalkyl, substituted and unsubstituted â(CH ) âC cycloalkenyl, substituted and unsubstituted â(CH ) -aryl, substituted and unsubstituted â(CH ) -heterocyclic ring, substituted and unsubstituted â(CH ) âXâR (X is âOâ, âS( O) â, âNR â, âS( O) NR â, or âC( O)â), and â(CH ) CHR R. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation.

US Patent:

20030166687, Sep 4, 2003

Filed:

May 18, 2000

Appl. No.:

09/530965

Inventors:

MARTHA WARPEHOSKI - PORTAGE MI, US
MARK MITCHELL - KALAMAZOO MI, US
DONALD HARPER - PLAINWELL MI, US
LINDA MAGGIORA - KALAMAZZO MI, US

International Classification:

A61K031/4439
A61K031/44
A61K031/4166
A61K031/165
C 07D 4 3/02

US Classification:

514/341000, 514/357000, 514/575000, 514/389000, 546/274400, 546/336000, 548/318500, 562/621000

Abstract:

The present invention provides a compound of formula (1), or pharmaceutical acceptable salts thereof wherein R1 is C4-12 alkyl, C4-12 alkenyl, C4-12 alkynyl, —(CH2)h-C3-8 cycloalkyl, substituted and unsubstituted —(CH2)h-aryl, substituted and unsubstituted-(CH2)h-het, R2 is substituted and unsubstituted C1-12 alkyl, substituted and unsubstituted C2-12 alkenyl, substituted and unsubstituted C2-12 alkynyl, substituted and unsubstituted-(CH2)h-C3-8 cycloakyl, substituted and unsubstituted —(CH2)h-C3-8 unsubstituted-(CH2)h-C3-8 cycloakyl, substituted and unsubstituted —(CH2)h-C3-8 cycloalkenyl, substituted and unsubstituted-(CH2)h-aryl, substituted and unsubstituted-(CH2)h-heterocyclic ring, substituted and unsubstituted —(CH2)i-X—R4 (X is —O—, —S( O)j-, —NR7-, —S( O)2NR8-, or —C( O)—), and —(CH2)iCHR5R6. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation

US Patent:

58471480, Dec 8, 1998

Filed:

Apr 10, 1997

Appl. No.:

8/835599

Inventors:

Eric J. Jacobsen - Plainwell MI
Mark A. Mitchell - Kalamazoo MI
Heinrich J. Schostarez - Portage MI
Donald E. Harper - Plainwell MI

Assignee:

Pharmacia & Upjohn Company - Kalamazoo MI

International Classification:

C07D285125
C07D20908
C07D24104
A01N 4382

US Classification:

548140

Abstract:

The present invention provides novel thiadiazole derivatives represented by formula I: ##STR1## or pharmaceutical acceptable salts thereof wherein the compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, predominantly stromelysins, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthritis, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis (invasion and growth), periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, and other diseases related to connective tissue degradation.

US Patent:

62359282, May 22, 2001

Filed:

Jul 26, 1999

Appl. No.:

9/269185

Inventors:

Martha A. Warpehoski - Portage MI
Donald E. Harper - Plainwell MI

Assignee:

Pharmacia & Upjohn Company - Kalamazoo MI

International Classification:

C07C31704
C07C31722

US Classification:

562429

Abstract:

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof. Such compounds may be incorporated into pharmaceutical compositions which can inhibit various enzymes from the matrix metalloproteinase family. ##STR1##.

US Patent:

58471537, Dec 8, 1998

Filed:

Sep 19, 1997

Appl. No.:

8/934408

Inventors:

Martha A. Warpehoski - Portage MI
Donald E. Harper - Plainwell MI

Assignee:

Pharmacia & Upjohn Company - Kalamazoo MI

International Classification:

C07D23340

US Classification:

5483195

Abstract:

The present invention provides a compound of formula I ##STR1## or pharmaceutical acceptable salts thereof wherein R. sub. 1 is C. sub. 4-12 alkyl, C. sub. 4-12 alkenyl, C. sub. 4-12 alkynyl, --(CH. sub. 2). sub. h -C. sub. 3-8 cycloalkyl, --(CH. sub. 2). sub. h -aryl, or --(CH. sub. 2). sub. h -het; R. sub. 2 is C. sub. 1-12 alkyl, C. sub. 2-12 alkenyl, C. sub. 2-12 alkynyl, --(CH. sub. 2). sub. h -C. sub. 3-8 cycloalkyl, --(CH. sub. 2). sub. h -C. sub. 3-8 cycloalkenyl, --(CH. sub. 2). sub. h -aryl, --(CH. sub. 2). sub. h -het, --(CH. sub. 2). sub. h -Q, --(CH. sub. 2). sub. i -X-R. sub. 4, or --(CH. sub. 2). sub. i CHR. sub. 5 R. sub. 6. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation.