David H Borcherding

US Patent:

6420373, Jul 16, 2002

Filed:

Jan 13, 1995

Appl. No.:

08/372712

Inventors:

David R. Borcherding - Loveland OH
H. Randall Munson - Loveland OH

Assignee:

Merrell Pharmaceuticals Inc. - Bridgewater NJ

International Classification:

C07D47334

US Classification:

514261, 514266, 544264, 544277, 546118

Abstract:

The present invention relates to novel 9-N-bicyclic nucleoside agents which are useful as selective inhibitors of proinflammatory cytokines.

US Patent:

6436947, Aug 20, 2002

Filed:

Nov 20, 1997

Appl. No.:

08/975212

Inventors:

David R. Borcherding - Loveland OH
Ronald E. Esser - Berkeley Heights NJ
Douglas L. Cole - San Diego CA

Assignee:

Aventis Pharmaceuticals Inc. - Bridgewater NJ

International Classification:

C07D47316

US Classification:

5142634, 544277

Abstract:

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

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:

54261015, Jun 20, 1995

Filed:

Sep 15, 1994

Appl. No.:

8/306847

Inventors:

Norton P. Peet - Cincinnati OH
David R. Borcherding - Loveland OH
Nelsen L. Lentz - West Chester OH
Philip M. Weintraub - Cincinnati OH
Philip R. Kastner - Loveland OH

Assignee:

Merrell Dow Pharmaceuticals Inc. - Cincinnati OH

International Classification:

C07H 19167
A61K 3170

US Classification:

514 46

Abstract:

The compound (R)-2-[(phenylisopropyl)amino]adenosine whose structure is given below: ##STR1## (R)-2-[(phenylisopropyl)amino]adenosine is about two orders of magnitude greater in its selectivity between the A-1 and A-2 adenosine receptors than its diastereoisomer. This compound is useful for lowering blood pressure.

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.