Abstract: The present invention relates to novel 2-substituted indane-2-mercaptoacetylamide derivatives which are useful as inhibitors of enkephalinase and ACE.
Abstract: The present invention relates to compounds of the formula ##STR1## wherein B.sub.1 and B.sub.2 are each independently hydrogen; hydroxy; --OR.sub.2 wherein R.sub.2 is a C.sub.1 -C.sub.4 alkyl or an Ar-Y group wherein Ar is aryl and Y is a hydrogen or C.sub.1 -C.sub.4 alkyl; or, where B.sub.1 and B.sub.2 are attached to adjacent carbon atoms, B.sub.1 and B.sub.2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy;A is a bond, methylene or oxygen, sulfur or NR.sub.4 or NCOR.sub.5 wherein R.sub.4 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar-Y- group and R.sub.5 is --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar-Y- group;R.sub.3 is hydrogen or --CH.sub.2 OC(O)C(CH.sub.3).sub.3 ;R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or --CH.sub.2 OC(O)--C(CH.sub.3).sub.3 ; andn is an integer 1 to 3,which are useful as inhibitors of enkephalinase and ACE.
Abstract: The present invention relates to certain novel mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and of ACE.
Type:
Grant
Filed:
April 5, 1995
Date of Patent:
June 18, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Gary A. Flynn, Philippe Bey, Alan M. Warshawsky, Douglas W. Beight, Shujaath Mehdi, Eugene L. Giroux, Timothy P. Burkholder, Edward D. Daugs, John F. French
Abstract: The present invention relates to certain novel mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and of ACE.
Type:
Grant
Filed:
April 5, 1995
Date of Patent:
February 13, 1996
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Gary A. Flynn, Philippe Bey, Alan M. Warshawsky, Douglas W. Beight, Shujaath Mehdi, Eugene L. Giroux, Timothy P. Burkholder, Edward D. Daugs, John F. French
Abstract: The present invention relates to novel 2-substitited indane-2-mercaptoacetylamide tricyclic derivatives which are useful as inhibitors of Enkephalise.
Abstract: The present invention relates to novel 2-substituted indane-2-mercaptoacetylamide tricyclic derivatives which are useful as inhibitors of Enkephalise.
Abstract: The present invention relates to compounds of the formula ##STR1## wherein B.sub.1 and B.sub.2 are each independently hydrogen; hydroxy; --OR.sub.2 wherein R.sub.2 is a C.sub.1 -C.sub.4 alkyl or an Ar-Y group wherein Ar is aryl and Y is a hydrogen or C.sub.1 -C.sub.4 alkyl; or, where B.sub.1 and B.sub.2 are attached to adjacent carbon atoms, B.sub.1 and B.sub.2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy;A is a bond, methylene or oxygen, sulfur or NR.sub.4 or NCOR.sub.5 wherein R.sub.4 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Y-- group and R.sub.5 is --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Y-- group;R.sub.3 is hydrogen or --CH.sub.2 OC(O)C(CH.sub.3).sub.3 ;R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or --CH.sub.2 OC(O)--C(CH.sub.3).sub.3 ; andn is an integer 1 to 3,which are useful as inhibitors of enkephalinase and ACE.
Abstract: The present invention relates to a novel process for preparing (E)-1-amino-2-(fluoromethylene)-4-(p-fluorophenyl)butane, also known in the art as (E)-(p-fluorophenethyl)-3-fluoroallylamine, novel intermediates thereof, a novel process for the preparing (E)-2-(fluoromethylene)-4-(p-fluorophenyl)butan-1-ol, and a novel process for preparing alkali metal salts of diformylamide.
Type:
Grant
Filed:
September 29, 1994
Date of Patent:
January 30, 1996
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Jonathan C. Evans, Christian T. Goralski, Cynthia L. Rand, Paul C. Vosejpka
Abstract: The present invention relates to novel 2-substituted indane-2-mercaptoacetylamide derivatives which are useful as inhibitors of enkephalinase and ACE.
Abstract: The present invention relates to the use of certain mercaptoacetylamide and benzazapine derivatives in treating patients suffering from hypertriglyceridemia, atherosclerosis and hypercholesterolemia.
Type:
Grant
Filed:
March 24, 1994
Date of Patent:
January 16, 1996
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Gary A. Flynn, John F. French, Richard C. Dage
Abstract: The invention relates to compounds of the formula ##STR1## wherein B.sub.1 and B.sub.2 are each independently hydrogen; hydroxy; --OR.sub.2 wherein R.sub.2 is a C.sub.1 -C.sub.4 alkyl or an Ar--Y group wherein Ar is aryl and Y is a hydrogen or C.sub.1 -C.sub.4 alkyl; or, where B.sub.1 and B.sub.2 are attached to adjacent carbon atoms, B.sub.1 and B.sub.2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy;A is a bond, methylene or oxygen, sulfur, NR.sub.4 or NCOR.sub.5 wherein R.sub.4 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Y-- group and R.sub.5 is --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Y-- group; R.sub.3 is hydrogen or --CH.sub.2 OC(O)C(CH.sub.3).sub.3 ; R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or --CH.sub.2 OC(O)--C(CH.sub.3).sub.3 ; and n is an integer 1 to 3,that are useful as inhibitors of enkephalinase and ACE.
Abstract: The present invention relates to compounds of the formula ##STR1## wherein A is methylene, oxygen, sulfur or N--B wherein B is R.sub.1 or COR.sub.2 wherein R.sub.1 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Z--group wherein Ar is aryl and Z is a C.sub.0 -C.sub.4 alkyl and R.sub.2 is a --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Z group;R is hydrogen or a C.sub.1 -C.sub.4 alkyl; andX and Y are each independently hydrogen, nitro or amino, with the proviso that when X is nitro or amino, Y must be hydrogen, and when Y is nitro or amino, X must be hydrogen; andpharmaceutically acceptable salts thereof, which are inhibitors of Angiotensin Converting Enzyme.
Abstract: The present invention relates to compounds of the formula ##STR1## wherein B.sub.1 and B.sub.2 are each independently hydrogen; hydroxy; --OR.sub.2 wherein R.sub.2 is a C.sub.1 -C.sub.4 alkyl or an Ar--Y group wherein Ar is aryl and Y is a hydrogen or C.sub.1 -C.sub.4 alkyl; or, where B.sub.1 and B.sub.2 are attached to adjacent carbon atoms, B.sub.1 and B.sub.2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy;A is a bond, methylene or oxygen, sulfur or NR.sub.4 or NCOR.sub.5 wherein R.sub.4 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Y-- group and R.sub.5 is --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Y-- group;R.sub.3 is hydrogen or --CH.sub.2 OC(O)C(CH.sub.3).sub.3 ;R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or --CH.sub.2 OC(O)--C(CH.sub.3).sub.3 ; andn is an integer 1 to 3,which are useful as inhibitors of enkephalinase and ACE.
Abstract: The present invention relates to certain novel mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and of ACE.
Type:
Grant
Filed:
November 9, 1993
Date of Patent:
July 4, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Gary A. Flynn, Philippe Bey, Alan M. Warshawsky, Douglas W. Beight, Shujaath Mehdi, Eugene L. Giroux, Timothy P. Burkholder, Edward D. Daugs, John F. French
Abstract: The present invention relates to novel 2-substituted indane-2-mercaptoacetylamide derivatives which are useful as inhibitors of enkephalinase and ACE.
Abstract: The present invention relates to novel 2-substitited indane-2-mercaptoacetylamide tricyclic derivatives which are useful as inhibitors of Enkephalise.