Abstract: Pharmaceutical compositions of specific substituted pyrimidines and methods of treatment of certain cardiovascular disorders are disclosed. Also disclosed are novel substituted acrylated pyrimidines which are useful as calcium channel blockers.
Type:
Grant
Filed:
February 7, 1986
Date of Patent:
June 23, 1987
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Steven M. Pitzenberger, David E. McClure
Abstract: Substituted lactams and related compounds and methods for their preparation are disclosed. These compounds are useful as angiotensin converting enzyme inhibitors and as antihypertensives.
Abstract: Substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit pharmacological activity which includes antihypertensive activity and .beta.-adrenergic blocking activity.
Abstract: Compounds of the formula: ##STR1## where R.sup.3 is ##STR2## where n is 1-3 and the R.sup.a 's and R.sup.b 's are independently hydrogen or loweralkyl; and pharmaceutically acceptable salts thereof; are inhibitors or angiotensin I converting enzyme useful as antihypertensive agents.
Abstract: There are disclosed aza analogs of carboxyalkyl dipeptide derivatives and related compounds which are useful as converting enzyme inhibitors and as antihypertensives said compounds being represented by the general formula: ##STR1## wherein A and B can be joined together to form various ring structures.
Type:
Grant
Filed:
July 27, 1983
Date of Patent:
January 6, 1987
Assignee:
Merck & Co., Inc.
Inventors:
William J. Greenlee, Eugene D. Thorsett
Abstract: The invention in its broad aspects relates to caprolactam derivatives which are useful as angiotensin converting enxyme inhibitors and as antihypertensives.
Type:
Grant
Filed:
July 2, 1982
Date of Patent:
December 16, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Elbert E. Harris, Arthur A. Patchett, Eugene D. Thorsett
Abstract: Pharmaceutical compositions comprising 4-(5H-dibenzo[a,d]cyclohepten-5-yl)piperidine compounds and the use of 4-(5H-dibenzo[a,d]cyclohepten-5-yl)piperidine compounds for treatment of certain cardiovascular disorders are disclosed.
Abstract: There are disclosed novel O-sulfate derivatives of avermectin and milbemycin. The avermectin and milbemycin O-sulfate derivatives have improved water solubility compared to the parent avermectin and milbemycin compounds and have utility as anti-parasitic agents and as potent insecticides against agricultural pests.
Abstract: Sulfoxide and sulfone derivatives of bicyclic lactams are disclosed which are useful as converting enzyme inhibitors and as antihypertensives.
Type:
Grant
Filed:
June 22, 1983
Date of Patent:
October 14, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Arthur A. Patchett, Matthew J. Wyvratt, Jr.
Abstract: Novel substituted and bridged pyrimidine compounds useful as calcium channel blockers, pharmaceutical compositions thereof, and methods of treatment are disclosed.
Type:
Grant
Filed:
February 21, 1985
Date of Patent:
September 2, 1986
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, David A. Claremon, David E. McClure
Abstract: Compounds of the formula: ##STR1## wherein R.sup.2 is --(CH.sub.2).sub.k --X--(CH.sub.2).sub.j --NHR.sup.3 ; wherein k is 0 to 3, j is 1 or 2; X is F or OH; and, R.sup.3 is hydrogen; loweralkyl or loweraralkyl which may be substituted by hydroxy, carboxy, carbamoyl, or carbalkoxy; or, acyl; and, a pharmaceutically acceptable salt thereof; are inhibitors of angiotensin I converting enzyme useful as antihypertensive agents.
Abstract: Novel substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit cardioselective .beta.-adrenergic blocking activity, and are useful as antihypertensive agents, cardioprotective agents, antiarrythmic agents, antianginal agents with reduced side effects; e.g., they are devoid of intrinsic sympathomimetic activity.
Type:
Grant
Filed:
February 8, 1984
Date of Patent:
July 22, 1986
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
Abstract: The novel compounds of this invention and their pharmaceutically acceptable salts exhibit cardioselective .beta.-adrenergic blocking activity, with a direct relaxing effect on the .beta..sub.2 -adrenergic receptors and are useful as antihypertensive, cardioprotective, antiarrhythmic and, antianginal agents.
Abstract: There are disclosed perhydro-1,4-thiazepin-5-one and perhydro-1,4-thiazocin-5-one derivatives and related compounds which are useful as angiotensin converting enzyme inhibitors and as antihypertensives.
Type:
Grant
Filed:
April 29, 1985
Date of Patent:
June 10, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Yak-Fa Cheung, Eugene D. Thorsett, Arthur A. Patchett
Abstract: Novel substituted and bridged pyridine compounds useful as calcium channel blockers and analgesics, pharmaceutical compositions thereof, and methods of treatment are disclosed.
Abstract: The invention in its broad aspects relates to caprylolactam derivatives which are useful as angiotensin converting enzyme inhibitors and as antihypertensives.
Type:
Grant
Filed:
July 9, 1982
Date of Patent:
May 6, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Elbert E. Harris, Arthur A. Patchett, Eugene D. Thorsett
Abstract: The invention in its broad aspects relates to enantholactam derivatives which are useful as angiotensin converting enzyme inhibitors and antihypertensives.
Type:
Grant
Filed:
February 11, 1985
Date of Patent:
May 6, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Elbert E. Harris, Eugene D. Thorsett, Arthur A. Patchett