Patents Represented by Attorney, Agent or Law Firm David M. Stemerick
  • Farnesyl:protein transferase inhibitors as anticancer agents
    Patent number: 5665715
    Abstract: The present invention relates to certain inhibitors of farnesyl:protein transferase which are useful as antineoplastic agents.
    Type: Grant
    Filed: July 28, 1995
    Date of Patent: September 9, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventor: David M. Stemerick
  • Substituted pyrrolidin-3-yl-alkyl-piperidines
    Patent number: 5661160
    Abstract: The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 26, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Timothy P. Burkholder, Tieu-Binh Le, Elizabeth M. Kudlacz, George D. Maynard
  • Processes for preparing (S)-4-amino-hepta-5,6-dienoic acid and intemediates thereof
    Patent number: 5654477
    Abstract: The present invention relates to a novel enantiospecific processes for preparing (S)-4-amino-hepta-5,6-dienoic acid and pharmaceutically acceptable salts thereof, which is useful as an irreversible inhibitor of GABA-T, to novel intermediates thereof, and a process for preparing an intermediate thereof.
    Type: Grant
    Filed: March 6, 1995
    Date of Patent: August 5, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventor: H. Michael Kolb
  • Polyamine derivatives as antineoplastic agents
    Patent number: 5654484
    Abstract: The present invention relates to a method for the treatment of patients suffering from certain neoplastic disease states which comprises administering a therapeutically effective amount of a compound of the formula: ##STR1## wherein m is an integer 6 to 9, Z is a saturated (C.sub.2 -C.sub.6) alkylene moiety, each R group independently is hydrogen, methyl, ethyl, or n-propyl except that both R groups cannot be hydrogen when Z is a straight chain; or a pharmaceutically acceptable acid addition salt thereof. Said treatment can optionally comprise conjunctive therapy with a polyamine oxidase inhibitor. The invention also relates to certain novel polyamine derivatives.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: August 5, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Nellikunja J. Prakash, David M. Stemerick, Michael L. Edwards
  • Substituted pyrrolidin-3-yl-alkyl-piperidines
    Patent number: 5648366
    Abstract: The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 15, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Timothy P. Burkholder, Tieu-Binh Le, Elizabeth M. Kudlacz, George D. Maynard
  • Processes for preparing intermediates of inhibitors of enkephalinase and angiotensin converting enzyme and intermediates thereof
    Patent number: 5641880
    Abstract: The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme.
    Type: Grant
    Filed: October 24, 1995
    Date of Patent: June 24, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Gary A. Flynn, Thomas D. Bannister
  • Substituted pyrrolidin-3-yl-alkyl-piperidines
    Patent number: 5635510
    Abstract: The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their pharmacological activities such as tachykinin antagonism, especially substance P and neurokinin A antagonism, and the like. Compounds having the property of tachykinin antagonism are indicated for conditions associated with neurogenic inflammation and other diseases described herein.
    Type: Grant
    Filed: October 31, 1994
    Date of Patent: June 3, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Timothy P. Burkholder, Elizabeth M. Kudlacz, George D. Maynard
  • 2-substituted indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and ACE
    Patent number: 5629309
    Abstract: The present invention relates to certain novel 2-substituted indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and of ACE.
    Type: Grant
    Filed: December 14, 1995
    Date of Patent: May 13, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Gary A. Flynn, Douglas W. Beight, Alan M. Warshawsky, Shujaath Mehdi, John F. French, John H. Kehne
  • Indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase
    Patent number: 5604221
    Abstract: The present invention relates to certain novel indane-2-mercaptoacetylamide disulfide derivatives of the formula ##STR1## useful as inhibitors of enkephalinase.
    Type: Grant
    Filed: December 12, 1995
    Date of Patent: February 18, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Gary A. Flynn, Douglas W. Beight, Alan M. Warshawsky, Shujaath Mehdi, John H. Kehne
  • Process for the preparation of alkali metal salts of diformylamide
    Patent number: 5599986
    Abstract: The present invention relates to a novel process for preparing alkali metal salts of diformylamide and a novel crystalline form of sodium diformylamide.
    Type: Grant
    Filed: August 31, 1995
    Date of Patent: February 4, 1997
    Assignee: Hoechst Marion Roussel Inc.
    Inventors: Jonathan C. Evans, Christian T. Goralski, Cynthia L. Rand, Paul C. Vosejpka
  • Substituted alkyldiamine derivatives
    Patent number: 5597845
    Abstract: The present invention relates to novel substituted alkyldiamine derivatives and pharmaceutically acceptable salts thereof which are useful tachykinin antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions including asthma, cough, and bronchitis.
    Type: Grant
    Filed: June 20, 1994
    Date of Patent: January 28, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Timothy P. Burkholder, Elizabeth M. Kudlacz, Tieu-Binh Le
  • 2-substituted indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and ACE
    Patent number: 5567814
    Abstract: The present invention relates to certain novel 2-substituted indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and of ACE.
    Type: Grant
    Filed: March 2, 1995
    Date of Patent: October 22, 1996
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Gary A. Flynn, Douglas W. Beight, Alan M. Warshawsky, Shujaath Mehdi, John F. French, John H. Kehne
  • Triaryl-ethylene derivatives
    Patent number: 5525633
    Abstract: The present invention relates to novel triaryl-ethylene derivatives that are useful as anti-neoplastic agents, antiatherosclerotic agents, and hypocholesterolemic agents.
    Type: Grant
    Filed: June 15, 1994
    Date of Patent: June 11, 1996
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Donald P. Matthews, Alan J. Bitonti, William A. Van Sickle, Donald A. Kaplan
  • Process for preparing (S)-1-[2(S)-(1,3-dihyrdro-1,3-dioxo-isoindo-2-yl)-1-oxo-3-phenylpropyl]- 1,2,3,4,-tetrahydro-2-pyridine-carboxylic acid methyl ester
    Patent number: 5508411
    Abstract: The present invention relates to a novel enantiospecific process for preparing (S)-1-[2(S)-(1,3-dihydro-1,3-dioxo-isoindo-2-yl)-1-oxo-3-phenylpropyl ]-1,2,3,4-tetrahydro-2-pyridine-carboxylic acid methyl ester which is a useful intermediate in the preparation of [4S-[4.alpha., 7.alpha.(R*), 12b.beta.]]-7-[(1-oxo-2(S)-thio-3-phenylpropyl) amino]-1,2,3,4,6,7,8,12b-octahydro-6-oxo-pyrido[2,1-a][2]benzazepine-4-car boxylic acid and [4S-[4.alpha., 7.alpha.(R*), 12b.beta.]]-7-[(1-oxo-2(S)-acetylthio-3-phenylpropyl)amino]-1,2,3,4,6,7,8, 12b-octahydro-6-oxo-pyrido[2,1-a][2]benzazepine-4-carboxylic acid and pharmaceutically acceptable salts thereof which is useful as an inhibitor of enkephali nase and angiotensin converting enzyme and to novel intermediates thereof.
    Type: Grant
    Filed: March 30, 1996
    Date of Patent: April 16, 1996
    Assignee: Merrell Pharmaceuticals Inc.
    Inventor: Gary A. Flynn
  • Cyclohex-2-enyl acetamides
    Patent number: 5502253
    Abstract: The present invention relates to a novel enantiospecific process for preparing (S)-1- 2(S)-(1,3-dihydro-1,3-dioxo-isoindo-2-yl)-1-oxo-3-phenylpropyl!-1,2 ,3,4-tetrahydro-2-pyridine-carboxylic acid methyl ester which is a useful intermediate in the preparation of 4S- 4.alpha., 7.alpha.(R*), 12b.beta.!!-7- (1-oxo-2(S)-thio-3-phenylpropyl)amino!-1,2,3,4,6,7,8,12b-oc tahydro-6-oxo-pyrido 2,1-a! 2!benzazepine-4-carboxylic acid and 4S- 4.alpha., 7.alpha.(R*), 12b.beta.!!-7- (1-oxo-2(S)-acetylthio-3-phenylpropyl)amino!-1,2,3,4,6,7,8, 12b-octahydro-6-oxo-pyrido 2,1-a! 2!benzazepine-4-carboxylic acid and pharmaceutically acceptable salts thereof which is useful as an inhibitor of enkephalinase and angiotensin converting enzyme and to novel intermediates thereof.
    Type: Grant
    Filed: March 30, 1995
    Date of Patent: March 26, 1996
    Assignee: Merrell Pharmaceuticals Inc.
    Inventor: Gary A. Flynn