Abstract: The present invention relates to novel coumarin derivatives and related compounds which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The coumarin derivatives are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized coumarins and of related structures.
Type:
Grant
Filed:
November 19, 1993
Date of Patent:
April 23, 1996
Assignee:
Warner-Lambert Company
Inventors:
John M. Domagala, Susan E. Hagen, Elizabeth Lunney, Bradley D. Tait
Abstract: The present invention relates to novel substituted tricyclic pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The tricyclic pyrone derivatives are useful in the development of therapies for the treatment of vital infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized tricyclic pyrones and of related structures.
Abstract: The present invention is directed to compounds useful for the regulation of cholesterol of Formula I, methods for using them and pharmaceutical compositions thereof, ##STR1## wherein X and Y are oxygen, sulfur, or (CR'R").sub.n wherein n is 1 to 4; R is hydrogen, alkyl, or benzyl; R.sub.1 and R.sub.2 are phenyl, substituted phenyl, naphthyl, substituted naphthyl, an aralkyl group, an alkyl chain, adamantyl, or a cycloalkyl group.
Type:
Grant
Filed:
April 13, 1994
Date of Patent:
February 13, 1996
Assignee:
Warner-Lambert Company
Inventors:
Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic, Wendell Wierenga
Abstract: The instant invention is a method of using known compounds, such as (-)-5.alpha.,7.alpha.,-8.beta.-N-methyl-N-[7-(1-pyrrolidinyl)-1-oxaspiro[4 .5]dec-8-yl]-4-benzofuranacetamide, as agents for treating benign prostatic hyperplasia.
Type:
Grant
Filed:
February 16, 1995
Date of Patent:
February 6, 1996
Assignee:
Warner-Lambert Company
Inventors:
Michael A. Breider, Cynthia L. Courtney, Felix A. De La Iglesia, Alexander W. Gough, Alan L. Metz
Abstract: The present invention provides indolocarbazole derivatives of the formula ##STR1## as well as the regioisomeric mixtures thereof, pharmacologically acceptable salts thereof, processes for the preparation thereof, and pharmaceutical compositions containing them for the treatment and/or prophylaxis of heart and blood vessel diseases, such as thromboses, arterioscleroses, hypertonias, of bronchopulmonary diseases, inflammatory processes, allergies, cancers and degenerative damage of the central nervous system, and for the treatment of viral diseases.
Type:
Grant
Filed:
February 2, 1995
Date of Patent:
February 6, 1996
Assignee:
Goedecke Aktiengesellschaft
Inventors:
Jurgen Kleinschroth, Johannes Hartenstein, Christoph Schachtele, Claus Rudolph
Abstract: Novel naphthyl-substituted .alpha.-amino acid derivatives, pharmaceutical compositions containing the same and a method of using the same, for the blockade of aspartate and glutamate receptors, are described. Novel intermediates of the napthyl-substituted .alpha.-amino acid derivatives are disclosed.
Abstract: This invention relates to novel substituted 1,2,3,4-tetrahydroisoquinolines which are useful in the treatment of vascular restenosis, various disorders of the central nervous system, in the regulation of female reproductive functions, in cognitive enhancement, in atherosclerosis and in treating excessive AVP secretory disorders. Novel intermediates useful in the preparation of the compounds are also disclosed. Methods of using the compounds and pharmaceutical compositions containing them are disclosed.
Type:
Grant
Filed:
April 28, 1994
Date of Patent:
February 6, 1996
Assignee:
Warner-Lambert Company
Inventors:
Clifton J. Blankley, John C. Hodges, Sylvester Klutchko
Abstract: A method of treating cognitive deficiencies is described by administering a quinazoline derivative of the general formula ##STR1## wherein A represents ##STR2## in which n is 1-10, P is a bond or (CH.sub.2).sub.m in which m is 0-10, and M is .dbd.O, .dbd.S, .dbd.NR, .dbd.CRR', ##STR3## novel compounds of the above are also described as well as methods of manufacture and pharmaceutical compositions.
Abstract: Novel indole and indoline nonpeptide antagonists of endothelin I are described, as well as novel intermediates used in their preparation, methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure and subarachnoid hemorrhage.
Type:
Grant
Filed:
November 14, 1994
Date of Patent:
January 9, 1996
Assignee:
Warner-Lambert Company
Inventors:
Kent A. Berryman, Amy M. Bunker, Annette M. Doherty, Jeremy J. Edmunds
Abstract: The invention concerns novel renin-inhibitory compounds which contain an amino-substituted heterocycle at the P.sub.2 position. These are useful for treating renin-associated hypertension, congestive heart failure, glaucoma, hyperaldosteronism, and diseases caused by retroviruses including HTLV-I and -III. Processes for preparing the compounds, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, or hyperaldosteronism.
Type:
Grant
Filed:
March 26, 1993
Date of Patent:
September 26, 1995
Assignee:
Warner-Lambert Company
Inventors:
Cleo Connolly, Annette M. Doherty, Harriet W. Hamilton, William C. Patt, Ila Sircar
Abstract: Unnatural dipeptoids of .alpha.-substituted Try-Phe derivatives are useful as agents in the treatment of panic disorders. These dipeptoids are CCK.sub.B antagonists having utility in the prevention of panic attacks in patients prone to these attacks.
Abstract: New indolocarbazoles of formula: ##STR1## or a pharmaceutically acceptable salt thereof, processes for their preparation, compositions containing, and methods for using the composition for the inhibition of protein kinases, such as protein kinase C, for the prevention and/or treatment of heart and blood vessel diseases such as thromboses, arterioscleroses, hypertension, or for inflammatory processes, allergies, cancers, viral diseases, and certain degenerative damages of the central nervous system are disclosed.
Type:
Grant
Filed:
January 21, 1994
Date of Patent:
August 1, 1995
Assignee:
Godecke Aktiengesellschaft
Inventors:
Jurgen Kleinschroth, Johannes Hartenstein, Hubert Barth, Christoph Schachtele, Claus Rudolph, Gunter Weinheimer, Hartmut Osswald
Abstract: Substituted 1-benzylimidazole-5-methylidene hydantoins are disclosed as well as methods of preparing them, pharmaceutical compositions containing them, and methods of using them. Intermediates useful in the preparation of the compounds of the invention are also disclosed and synthetic methods for preparing the novel intermediates. The compounds are useful as antagonists of angiotensin II and thus are useful in the control of hypertension, hyperaldosteronism, congestive heart failure, surgically induced vascular smooth muscle proliferation, and glaucoma.
Abstract: The invention concerns 2-aminocarboxylic acids and derivatives of formula ##STR1## processes for their preparation, as well as medicaments containing them for the inhibition of protein kinase C and thus for the prevention and/or treatment of heart and blood vessel diseases, such as thromboses, arterioscleroses, hypertension, of inflammatory processes, allergies, cancers, and certain degenerative damages of the central nervous system.
Type:
Grant
Filed:
April 22, 1991
Date of Patent:
March 28, 1995
Assignee:
Godecke Aktiengesellschaft
Inventors:
Uwe Trostmann, Johannes Hartenstein, Claus Rudolph, Christoph Schachtele, Hartmut Osswald, Gunter Weinheimer
Abstract: Novel .alpha.-substituted Trp dipeptoid derivatives cyclized at the C-terminal useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the compounds are antianxiety agents and antiulcer agents. They are agents useful for preventing the response to the withdrawal from chronic treatment with or use of nicotine, diazepam, alcohol, cocaine, caffeine, or opioids. The compounds of the invention are also useful in treating and/or preventing panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the compounds as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the compounds in diagnostic compositions.
Type:
Grant
Filed:
April 20, 1993
Date of Patent:
March 14, 1995
Assignee:
Warner-Lambert Company
Inventors:
David C. Horwell, Martyn C. Pritchard, Edward Roberts, Reginald S. Richardson
Abstract: This invention concerns novel dihydro- and tetrahydronaphthyridines useful for enhancing the lethal effects on tumor cells to treatment causing DNA-damaging activity as with ionizing radiation or with a chemotherapeutic agent.
Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.
Abstract: This invention relates to novel substituted imidazole and triazole derivatives which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of hypertension, heart failure, glaucoma, and hyperaldosteronism. Methods of making the compounds, novel intermediates useful in the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of using them are also covered.
Abstract: The present invention provides bis-(1H-indol-3-yl)maleinimide derivatives and the pharmacologically acceptable salts thereof, processes for the preparation of these compounds, and pharmaceutical compositions containing them for the treatment of heart and blood vessel diseases, such as thromboses, arteriosclerosis, hypertension, of inflammatory processes, allergies, cancer, and certain degenerative damages of the central nervous system, as well as of diseases of the immune system and viral diseases.
Type:
Grant
Filed:
March 9, 1993
Date of Patent:
January 10, 1995
Assignee:
Goedecke Aktiengesellschaft
Inventors:
Hubert Barth, Johannes Hartenstein, Claus Rudolph, Christoph Schachtele, Hans-Jurgen Betche, Reinhard Reck, Hartmut Osswald