Mark J Bock

US Patent:

6376503, Apr 23, 2002

Filed:

Jun 17, 1998

Appl. No.:

09/097947

Inventors:

Michael A. Patane - Harleysville PA
Mark G. Bock - Hatfield PA
Randall C. Newton - West Point PA
Bharat Lagu - Maywood NJ

Assignee:

Merck Co., Inc - Rahway NJ
Synaptic Pharmaceutical Corporation - Paramus NJ

International Classification:

A61K 31513

US Classification:

514274, 544295, 544296, 544283, 544284, 544316, 514252, 514259, 514253

Abstract:

This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

US Patent:

6919343, Jul 19, 2005

Filed:

Jan 30, 2003

Appl. No.:

10/354674

Inventors:

Michael R. Wood - Harleysville PA, US
Neville J. Anthony - Hatfield PA, US
Mark G. Bock - Hatfield PA, US
Dong-Mei Feng - Blue Bell PA, US
Scott D. Kuduk - Harleysville PA, US
Dai-Shi Su - Dresher PA, US
Jenny Miu-chun Wai - Harleysville PA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07C237/24
C07D213/82
A61K031/165

US Classification:

514256, 514335, 514364, 514378, 514381, 514542, 514616, 544333, 544335, 546316, 548131, 548247, 548250, 560 42, 564155

Abstract:

N-Biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

US Patent:

7091380, Aug 15, 2006

Filed:

Feb 4, 2003

Appl. No.:

10/503502

Inventors:

Michael R. Wood - Harleysville PA, US
Neville J. Anthony - Chalfont PA, US
Mark G. Bock - Hatfield PA, US
Dong-Mei Feng - Blue Bell PA, US
Scott D. Kuduk - Harleysville PA, US
Dai-Shi Su - Dresher PA, US
Jenny Miu-chun Wai - Harleysville PA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07C 233/05
C07C 233/65
A61K 31/165

US Classification:

564155, 514531, 514616, 560 45

Abstract:

N-Biphenyl(substituted methyl) aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

US Patent:

7163951, Jan 16, 2007

Filed:

Aug 25, 2003

Appl. No.:

10/523911

Inventors:

Scott D. Kuduk - Harleysville PA, US
Michael R. Wood - Harleysville PA, US
Mark G. Bock - Hatfield PA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31/4427
C07D 401/12

US Classification:

514336, 5462681, 5462687, 546337, 544296, 544333, 514256, 514269, 514340, 514342, 514357

Abstract:

N-Biarylmethylaminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

US Patent:

7790754, Sep 7, 2010

Filed:

Dec 17, 2004

Appl. No.:

10/583675

Inventors:

Michael R. Wood - Harleysville PA, US
Neville J. Anthony - Chalfont PA, US
Mark G. Bock - Hatfield PA, US
Scott D. Kuduk - Harleysville PA, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

A61K 31/4439
C07D 413/10

US Classification:

514338, 5462691

Abstract:

α-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. Ris selected from (1) a group selected from R. (2) (CH)NRC(O)R. (3) (CH)NRSOR. (4) (CH)NRCOR. (5) (CH)-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen. nitro, cyano. OR. SR. Calkyl and Chaloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N. O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or (b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6) (CH)COR.

US Patent:

20040029920, Feb 12, 2004

Filed:

Aug 5, 2003

Appl. No.:

10/634401

Inventors:

Scott Kuduk - Harleysville PA, US
Mark Bock - Hatfield PA, US
Dong-Mei Feng - Blue Bell PA, US
Jenny Wai - Harleysville PA, US

International Classification:

A61K031/444
C 07D 4 1/02
C07D213/54

US Classification:

514/332000, 546/264000, 546/307000, 514/351000

Abstract:

Compounds disclosed herein are bradykinin B1 antagonist compounds useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

US Patent:

20040034064, Feb 19, 2004

Filed:

Aug 5, 2003

Appl. No.:

10/634402

Inventors:

Scott Kuduk - Harleysville PA, US
Mark Bock - Hatfield PA, US
Dong-Mei Feng - Blue Bell PA, US
Jenny Wai - Harleysville PA, US

International Classification:

A61K031/444
C 07D 4 1/02

US Classification:

514/332000, 514/351000, 546/264000, 546/307000

Abstract:

Compounds disclosed herein are bradykinin B1 antagonist compounds useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

US Patent:

20040044041, Mar 4, 2004

Filed:

Aug 5, 2003

Appl. No.:

10/634426

Inventors:

Scott Kuduk - Harleysville PA, US
Mark Bock - Hatfield PA, US
Dong-Mei Feng - Blue Bell PA, US
Dai-Shi Su - Dresher PA, US
Jenny Wai - Harleysville PA, US

International Classification:

A61K031/444
A61K031/44
C 07D 4 1/02

US Classification:

514/332000, 514/351000, 546/264000, 546/307000

Abstract:

Compounds disclosed herein are bradykinin B1 antagonist compounds useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.