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
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
Abstract: Synthetic pulmonary surfactants having antioxidant properties consisting of a complex of a polypeptide of 3-4 amino acid residues, with an antioxidant moiety, and a lipid consisting of one or more of the lipids associated with natural pulmonary surfactant were prepared. These surfactants are useful in the treatment of respiratory distress syndrome.
Abstract: This invention relates to 1-aryl-3-pyridinyl-2-propene-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.
Type:
Grant
Filed:
November 17, 1993
Date of Patent:
March 19, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Robert J. Dinerstein, Michael L. Edwards, David M. Stemerick, Keith A. Diekema
Abstract: A method for the inhibition of tumor metastases is described herein. The method makes use of the administration of an antimetastatic factor isolated from the leech Haementeria ghilianii.
Abstract: This invention relates to 1-phenyl-3-phenyl-2-propyne-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.
Type:
Grant
Filed:
September 16, 1994
Date of Patent:
August 29, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Robert J. Dinerstein, Jeffrey S. Sabol, Keith A. Diekema
Abstract: Agonists and Antagonist of bombesin are derivatives of naturally occurring bombesin possessing a methyl sulfide or a methyl amide bond connecting the two amino acids on the carboxy terminal end. Agonist and antagonist activities are confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions. Use of these peptides include stimulating or antagonizing growth of tissues, especially lung, and a means for effecting treatment for digestional disorders. Treatment comprises administering to a patient in need thereof, an effective amount of a bombesin analog.
Abstract: Disclosed are Agonists and Antagonists of bombesin which are derivatives of naturally occurring bombesin possessing modified derivatives of phenylalanine. Agonist and antagonist activities are confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions.Use of these peptides may be useful for stimulating or antagonising growth of tissues, especially lung, and of digestion. Treatment comprises administering to a patient in need thereof, an effective amount of a bombesin analog.
Abstract: This invention relates to 1-phenyl-3-aryl-2-propyne-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.
Type:
Grant
Filed:
March 5, 1993
Date of Patent:
April 25, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Robert J. Dinerstein, Jeffrey S. Sabol, Keith A. Diekema
Abstract: The present invention is directed to a new class of arylalkoxyphenoxy-imidazoline compounds and their use for the treatment of depression, anxiety, hypertension, and migraine headaches.
Type:
Grant
Filed:
February 9, 1994
Date of Patent:
April 18, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Jules Freedman, Bruce M. Baron, Mark W. Dudley
Abstract: Agonists of NPY which are derivatives of naturally occurring NPY. The agonism is confirmed using conventional competitive binding and biochemical assays and the use of these derivatives in a variety of conditions in which neuropeptide Y is implicated is also described.
Abstract: Certain Castanospermine ester derivatives of the formula: ##STR1## wherein R, R.sub.1 and R.sub.2 are each independently hydrogen, C.sub.1-14 alkanoyl, C.sub.1-14 alkenoyl, cyclohexanecarbonyl, C.sub.1-8 alkoxyacetyl, ##STR2## naphthalenecarbonyl optionally substituted by methyl or halogen; phenyl (C.sub.2-6 alkanoyl) wherein the phenyl is optionally substituted by methyl or halogen; cinnamoyl; pyridinecarbonyl optionally substituted by methyl or halogen; dihydropyridine carbonyl optionally substituted by C.sub.1 -C.sub.10 alkyl; thiophenecarbonyl optionally substituted by methyl or halogen; or furancarbonyl optionally substituted by methyl or halogen; Y is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, trifluoromethyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylmercapto, cyano or dimethylamino; Y' is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or it is combined with Y to give 3,4-methylenedioxy; Y" is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or halogen; with R, R.sub.1 and R.sub.
Type:
Grant
Filed:
April 1, 1993
Date of Patent:
January 31, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Sai P. Sunkara, Paul S. Liu, A. Stanley Tyms, Debra L. Taylor
Abstract: Various peptides having affinity for sulfated polysaccharides such as heparin, dextran sulfate and Pentosan polysulfate are bound to resins and used in affinity chromatography to prepare anti-HIV sulfated polysaccharides.
Abstract: This invention relates to 1-phenyl-3-phenyl-2-propyne-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.
Type:
Grant
Filed:
June 1, 1992
Date of Patent:
September 28, 1993
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Robert J. Dinerstein, Jeffrey S. Sabol, Keith A. Diekema
Abstract: This invention relates to 1-phenyl-3-aryl-2-propyne-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.
Type:
Grant
Filed:
June 1, 1992
Date of Patent:
June 29, 1993
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Robert J. Dinerstein, Jeffrey S. Sabol, Keith A. Diekema
Abstract: The present invention is directed to a new class of arylalkoxyphenoxy-imidazoline compounds and their use for the treatment of depression, anxiety, hypertension, and migraine headaches.
Type:
Grant
Filed:
February 6, 1992
Date of Patent:
June 1, 1993
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Jules Freedman, Bruce M. Baron, Mark W. Dudley