Carl X Edwards

US Patent:

20020004508, Jan 10, 2002

Filed:

Feb 3, 1995

Appl. No.:

08/383339

Inventors:

CARL K. EDWARDS - WEST CHESTER OH, US
DAVID R. BORCHERDING - LOVELAND OH, US

International Classification:

A61K031/52
C07D473/00

US Classification:

514/261000, 544/264000, 544/277000

Abstract:

The present invention relates to novel carbocyclic nucleoside agents which are useful as selective inhibitors of proinflammatory cytokines.

US Patent:

57234663, Mar 3, 1998

Filed:

Jun 7, 1995

Appl. No.:

8/485263

Inventors:

David R. Borcherding - Loveland OH
Carl K. Edwards - Superior CO
Ronald E. Esser - Berkeley Heights NJ
Douglas L. Cole - San Diego CA

Assignee:

Hoechst Marion Roussel, Inc. - Cincinnati OH

International Classification:

C07D48704
A61K 31505

US Classification:

514258

Abstract:

This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y. sub. 3, Y. sub. 5 and Y. sub. 9 are each nitrogen and Y. sub. 7 and Y. sub. 8 are a CH group, R is a C. sub. 1 -C. sub. 7 alkyl acyl or aryl acyl, Q is NH. sub. 2, halogen or hydrogen, Z is hydrogen, halogen, or NH. sub. 2 ; or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

US Patent:

58176608, Oct 6, 1998

Filed:

Jun 7, 1995

Appl. No.:

8/477342

Inventors:

David R. Borcherding - Loveland OH
Carl K. Edwards - Superior CO
Ronald E. Esser - Berkeley Heights NJ
Douglas L. Cole - San Diego CA

Assignee:

Hoechst Marion Roussel, Inc. - Cincinnati OH

International Classification:

A61K 31505
C07D47316
C07D47332
C07D47334

US Classification:

514258

Abstract:

This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y. sub. 3, Y. sub. 5, Y. sub. 7, Y. sub. 8 and Y. sub. 9 are each nitrogen, R is a hydrogen, a C. sub. 1 -C. sub. 7 alkyl acyl or aryl acyl, Q is NH. sub. 2, halogen or hydrogen, Z is hydrogen, halogen, or NH. sub. 2 ; or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

US Patent:

56312580, May 20, 1997

Filed:

Apr 26, 1995

Appl. No.:

8/427937

Inventors:

David R. Borcherding - Loveland OH
Carl K. Edwards - West Chester OH
Ronald E. Esser - Sharonville OH

Assignee:

Merrell Pharmaceuticals Inc. - Cincinnati OH

International Classification:

A61K 3152
A61K 31505

US Classification:

514261

Abstract:

This invention relates to methods of effecting immunosuppression and inhibiting tumor necrosis factor. alpha. in a patient in need thereof comprising administering to said patient an effective immunosuppressive amount of a compound of the formula ##STR1## wherein the hydroxy substituent on the cyclopentanyl ring is in the CIS configuration relative to the bicyclic substituent, Y. sub. 3 is N, Y. sub. 7, Y. sub. 8 and Y. sub. 9 are each independently nitrogen or a CH group, Q is NH. sub. 2, halogen or hydrogen, and Z is hydrogen, halogen, or NH. sub. 2 ; or a pharmaceutically-acceptable salt thereof. Also presented are pharmaceutical compositions comprising compounds of the same formula.

US Patent:

58176721, Oct 6, 1998

Filed:

Jun 7, 1995

Appl. No.:

8/477344

Inventors:

David R. Borcherding - Loveland OH
Carl K. Edwards - Superior CO
Ronald E. Esser - Berkeley Heights NJ
Douglas L. Cole - San Diego CA

Assignee:

Hoechst Marion Roussel, Inc. - Cincinnati OH

International Classification:

C07D47334
C07D47316
C07D47104
A61K 3144

US Classification:

514303

Abstract:

This invention relates to novel Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y. sub. 3 and Y. sub. 8 are CH, Y. sub. 5, Y. sub. 7 and Y. sub. 9 are each independently nitrogen, R is a hydrogen, a C. sub. 1 -C. sub. 7 alkyl acyl or aryl acyl, Q is NH. sub. 2, halogen or hydrogen, Z is hydrogen, halogen, or NH. sub. 2 ; or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

US Patent:

59290790, Jul 27, 1999

Filed:

Nov 20, 1997

Appl. No.:

8/975088

Inventors:

David R. Borcherding - Loveland OH
Carl K. Edwards - Superior CO
Ronald E. Esser - Berkeley Heights NJ
Douglas L. Cole - San Diego CA

Assignee:

Hoechst Marion Roussel, Inc. - Bridgewater NJ

International Classification:

C07D47316
C07D47334
C07D47332
A61K 31505

US Classification:

514258

Abstract:

This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y. sub. 3, Y. sub. 5, Y. sub. 7, Y. sub. 8 and Y. sub. 9 are each nitrogen, R is a hydrogen, a C. sub. 1 -C. sub. 7 alkyl acyl or aryl acyl, Q is NH. sub. 2, halogen or hydrogen, Z is hydrogen, halogen, or NH. sub. 2 ; or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

US Patent:

55146880, May 7, 1996

Filed:

May 12, 1994

Appl. No.:

8/241814

Inventors:

David R. Borcherding - Loveland OH
Carl K. Edwards - West Chester OH
Ronald E. Esser - Sharonville OH

Assignee:

Merrell Dow Pharmaceuticals Inc. - Cincinnati OH

International Classification:

C07D23500
C07D22100
A61K 3141

US Classification:

514300

Abstract:

This invention relates to carbocyclic adenosine compounds of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentanyl ring is in the CIS configuration relative to the bicyclic substituent, Y. sub. 3, Y. sub. 7, Y. sub. 8 and Y. sub. 9 are each independently nitrogen or a CH group, Q is NH. sub. 2, halogen or hydrogen, and Z is hydrogen, halogen, or NH. sub. 2 ; or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

US Patent:

58176616, Oct 6, 1998

Filed:

Jun 7, 1995

Appl. No.:

8/485745

Inventors:

David R. Borcherding - Loveland OH
Carl K. Edwards - Superior CO
Ronald E. Esser - Berkeley Heights NJ
Douglas L. Cole - San Diego CA

Assignee:

Hoechst Marion Roussel, Inc. - Cincinnati OH

International Classification:

C07D47334
C07D47316
C07D47104
A61K 3152

US Classification:

514261

Abstract:

This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y. sub. 3, Y. sub. 5 Y. sub. 7, Y. sub. 9 are each nitrogen and Y. sub. 8 is a CH group, R is a hydrogen, a C. sub. 1 -C. sub. 7 alkyl acyl or aryl acyl, Q is NH. sub. 2, halogen or hydrogen, Z is hydrogen, halogen, or NH. sub. 2 ; or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.