Richard C Ransom

US Patent:

57189129, Feb 17, 1998

Filed:

Oct 28, 1996

Appl. No.:

8/736705

Inventors:

Wayne J. Thomspon - Lansdale PA
Pierre Mallorga - Lansdale PA
Richard W. Ransom - New Britain PA
Ian M. Bell - Harleysville PA
Michael F. Sugrue - Blue Bell PA
Peter M. Munson - Harleysville PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61F 200
A01N 4340
A61K 31445

US Classification:

424427

Abstract:

This invention is concerned with novel 1-�cycloalkylpioeridin-4-yl!-2H benzimidazolones, their compositions and method of use. The novel compounds are selective muscarinic agonists of the m2 subtype with low activity at the m3 subtype. The compounds are effective for the treatment of glaucoma with fewer side effects than the pilocarpine therapy.

US Patent:

52887251, Feb 22, 1994

Filed:

Oct 15, 1992

Appl. No.:

7/961589

Inventors:

Keith M. Witherup - Lansdale PA
Richard W. Ransom - New Britain PA
Sandor L. Varga - Harleysville PA
Steven M. Pitzenberger - Lansdale PA
Victor J. Lotti - Harleysville PA
William J. Lumma - Pennsburg PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D47104
A61K 3144

US Classification:

514292

Abstract:

A pyrroloquinoline compound of the following formula is disclosed: ##STR1## wherein H, C. sub. 1-6 alkyl, R. sup. 1 is: ##STR2## wherein R is H, C. sub. 1-10 alkyl, or C. sub. 1-6 alkyloxycarbonyl; R. sup. 2 is: H, C. sub. 1-6 alkyl, ##STR3## wherein R. sup. 5 is C. sub. 1-10 alkyl, aryl, or aryl C. sub. 1-10 alkyl; R. sup. 3 is: (CH. sub. 2). sub. n NHR wherein R is H, C. sub. 1-6 alkyl, or C. sub. 1-6 alkyloxycarbonyl; ##STR4## R. sup. 4 is: H, C. sub. 1-6 alkyl, C. sub. 1-6 alkyloxycarbonyl, RCH. sub. 2 --, wherein R is H, C. sub. 1-6 alkyl or aryl, or ##STR5## X is O, or NR. sup. 6 wherein R. sup. 6 is equal to H or C. sub. 1-6 alkyl and n is an integer from 1-3. The compounds of the invention exhibit bradykinin antagonist activity as well as activity with. alpha.

US Patent:

57565082, May 26, 1998

Filed:

Oct 28, 1996

Appl. No.:

8/736704

Inventors:

Wayne J. Thompson - Lansdale PA
Richard W. Ransom - New Britain PA
Pierre Mallorga - Lansdale PA
Michael F. Sugrue - Blue Bell PA

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D21114
C07D23526
C07D23926
A61K 31415

US Classification:

514256

Abstract:

This invention is concerned with novel 1,3-dihydro-1-�1-(1-heteroarylpiperidin-4-yl)piperidin-4-yl!-2H-benzimidaz olones, derivatives thereof, their preparation, method of use and pharmaceutical compositions. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).