Robert L Larsen

US Patent:

56938128, Dec 2, 1997

Filed:

Jun 3, 1996

Appl. No.:

8/684125

Inventors:

Gerald S. Brenner - Norristown PA
Louis S. Crocker - Belle Mead NJ
Hossain Jahansouz - North Wales PA
Robert D. Larsen - Bridgewater NJ
Chris H. Senanayake - North Brunswick NJ
Andrew S. Thompson - Mountainside NJ
Karen C. Thompson - Lansdale PA
Thomas R. Verhoeven - Cranford NJ

Assignee:

Merck & Co. Inc. - Rahway NJ

International Classification:

C07D49102

US Classification:

546118

Abstract:

Polymorphic forms of the angiotensin II receptor antagonist, 3-�2'-(N-benzoyl)sulfonamidobiphenyl-4-yl!methyl-5,7-dimethyl-2-ethyl-3H-i midazo�4,5-b!pyridine and a method for the preparation of these crystal forms.

US Patent:

6320049, Nov 20, 2001

Filed:

May 2, 2000

Appl. No.:

9/563203

Inventors:

Daniel R. Sidler - Whitehouse Station NJ
Robert D. Larsen - Bridgewater NJ
Wenjie Li - Pittsburgh PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D23922

US Classification:

544316

Abstract:

This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.