David R Borcherding

US Patent:

6413974, Jul 2, 2002

Filed:

Feb 9, 1999

Appl. No.:

09/247052

Inventors:

Jennifer A. Dumont - Flemington NJ
Alan J. Bitonti - Ringoes NJ
David R. Borcherding - Bangor PA
Norton P. Peet - Neshanic Station NJ
Patrick W. Shum - Flemington NJ

Assignee:

Aventis Pharmaceuticals Inc. - Bridgewater NJ

International Classification:

C07D47316

US Classification:

514261, 514266, 544277

Abstract:

The present invention provides novel compounds of the formula (I) wherein R is selected from the group consisting of R2, R2NHâ, or H NâR3â wherein R2 is selected from the group consisting of C -C alkyl and âwherein Z is selected from the group consisting of phenyl, heterocycle and cycloalkyl, each R4 is independently hydrogen or C -C alkyl, and n is an integer 1-8; wherein each C -C alkyl and Z is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of Ha1, OH, and C -C alkyl; R3 is C -C alkylene; and R1 is selected from the group consisting of cyclopentyl and isopropyl, and the pharmaceutically acceptable salts, optical isomers, and hydrates thereof. In addition, the present invention provides a method of inhibiting cell cycle progression. More specifically, the present invention provides a method of inhibiting cyclin dependent kinases, particularly cdk-2.

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:

6479487, Nov 12, 2002

Filed:

Feb 9, 1999

Appl. No.:

09/247053

Inventors:

Jennifer A. Dumont - Flemington NJ
Alan J. Bitonti - Acton MA
David R. Borcherding - Bangor PA
Norton P. Peet - Neshanic Station NJ
Patrick W. Shum - Flemington NJ

Assignee:

Aventis Pharmaceuticals Inc. - Bridgewater NJ

International Classification:

C07D47316

US Classification:

5142342, 514261, 514266, 544118, 544277

Abstract:

The present invention provides novel compounds of the formula (I) wherein R is selected from the group consisting of R2, R2NHâ, or R3R4NâR5- wherein R2 is selected from the group consisting of C -C alkyl, Z is selected from the group consisting of phenyl, heterocycle, cycloalkyl, and naphthanlene; and M is selected from the group consisting of hydrogen, C -C alkyl, and wherein each C -C alkyl or Z is optionally substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting of D, E, wherein each D is independently selected from the group consisting of trifluoromethyl, trifluoromethoxy, and C -C alkoxy; each E is independently selected from the group consisting of Hal, OH, and C -C alkyl; R3 and R4 are selected from the group consisting of hydrogen, C -C alkyl and (CH ) -phenyl, wherein y is an integer 0-8, with the proviso that R3 and R4 not both be hydrogen; R5 is C -C alkylene; and R1 is selected from the group consisting of cyclopentyl, cyclopentenyl and isopropyl, and the pharmaceutically acceptable salts, optical isomers, and hydrates thereof, with the proviso that when R2 is the group wherein n is 1 or greater; R1 is isopropyl or cyclopentyl; R6 is hydrogen, C -C alkyl, or (CH ) -phenyl; and Z is phenyl, heterocycle, or cycloalkyl, that Z is substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting of In addition, the present invention provides a method of inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms.

US Patent:

6541482, Apr 1, 2003

Filed:

Feb 3, 1995

Appl. No.:

08/383339

Inventors:

David R Borcherding - Bangor PA 18013

International Classification:

C07D47334

US Classification:

5142634, 544264, 544277, 546118

Abstract:

The present invention relates to compounds of the formula wherein X is N , NH , NHR, N(R) , CN, SH, SR, or OR ; R is C -C alkyl or (CH ) â ; n is an integer 0, 1, 2, 3 or 4; is a phenyl group unsubstituted or substituted with from 1 to 3 substituents, each substituent is independently selected from the group consisting of C -C alkyl, C -C alkoxy, halogen, CF , OCF , OH, CN, NO or NH ; R is C -C alkyl or (CH ) âNR R ; m is an integer 1, 2, 3 or 4; R and R are each independently C -C fluorinated akyl or cycloalkyl; The X substituent on the cyclopentanyl ring is in the TRANS configuration relative to the bicyclic substituent; Y is nitrogen; Z and Z are each independently hydrogen, halogen or NH ; and represents a singe or double bond; or pharmaceutically acceptable salts thereof, compositions comprising such compounds, and methods of treatment comprising administering of such compounds.

US Patent:

6642231, Nov 4, 2003

Filed:

Jun 24, 2002

Appl. No.:

10/178494

Inventors:

Jennifer A. Dumont - Groton MA
Alan J. Bitonti - Acton MA
David R. Borcherding - Bangor PA
Norton P. Peet - North Andover MA
Patrick W. Shum - Flemington NJ

Assignee:

Aventis Pharmaceuticals Inc. - Bridgewater NJ

International Classification:

C07D47316

US Classification:

5142342, 5142634, 51426321, 51426322, 51426333, 5142632, 544118, 544277

Abstract:

The present invention comprises 6-9-Disubstituted 2-[trans-(4-aminocyclohexyl]aminopurines that are useful in inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms.

US Patent:

6861524, Mar 1, 2005

Filed:

Oct 31, 2001

Appl. No.:

09/998976

Inventors:

David Borcherding - Bangor PA, US
Jennifer A. Dumont - Groton MA, US
Norton P. Peet - North Andover MA, US
Paul S. Wright - New Hope PA, US

Assignee:

Aventis Pharmaceuticals Inc. - Bridgewater NJ

International Classification:

C07D473/16
A61K031/52
A61P035/00
A61P037/06

US Classification:

544277

Abstract:

The present invention is directed to acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4-diaminocyclohexyl)-purines of the formula where Z is selected from the group consisting of —S(O)—, and —C(O)—.

US Patent:

7429595, Sep 30, 2008

Filed:

Oct 2, 2003

Appl. No.:

10/677683

Inventors:

David Borcherding - Bangor PA, US
Jennifer A. Dumont - Groton MA, US
Norton P. Peet - North Andover MA, US
Paul S. Wright - New Hope PA, US

Assignee:

Aventis Pharmaceuticals Inc. - Bridgewater NJ

International Classification:

C07D 473/16
A61K 31/52
A61P 35/00
A61P 35/02

US Classification:

51426322, 544277

Abstract:

The present invention is directed to acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4 -diaminocyclohexyl)-purines of the formula.