Warner-lambert Company

Schering Corporation

Shering Corporation

John G Topliss

Rudolph O Neri

Om Prakash Goel

Vladimir Genukh Beylin

Huai G Chen

Mark E Marlatt

Donald E Butler

John C Hodges

Ila Sircar

Adriano Afonso

Annette M Doherty

Wayne Livingston Cody

Michael H Cain

Novel antagonists of endothelin are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, metabolic, endocrinological, neurological disorders especially cerebral vasospasm, stroke, and head injury, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease, restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, and diabetes.

Endothelin Antagonists II

Novel cyclic amino acids which are useful in preparing biologically active peptides as well as a process for the preparation of D and L enantiomers of the cyclic amino acids are described where an N-protected derivative of the racemic cyclic amino acid is treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.

Cyclic amino acids and derivatives thereof

Novel substituted 4-(1-H-pyrrol-1-yl)imidazoles are disclosed as well as methods of preparing them, pharmaceutical compositions containing them, and methods of using them. Novel 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, glaucoma, vascular smooth muscle proliferation associated with atherosclerosis, and with postsurgical vascular restenosis.

4-(1H-pyrrol-1-yl)imidazoles with angiotensin II antagonist activity

4-(1H-pyrrol-1-yl) imidazoles with angiotension II antagonist activity

A process for the preparation of D(-) and L(+)-3,3-diphenylalanine and D(-) and L(+)-substituted 3,3-diphenylalanines is described where N-protected DL-3,3-diphenylalanine or N-protected-DL-substituted 3,3-diphenylalanine are treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.

Process for the preparation of D(-) and L(+)-3,3-diphenylalanine and

A unique series of saturated cycloalkyl[b]pyrrol-1(2H)-acetic acid amides are useful as agents for the reversal of amnesia. Intermediates for preparing the compounds, pharmaceutical composition containing the compounds, and method for using the pharmaceutical compositions for treating senility and for the reversal of amnesia are described. pg,

Saturated cycloalkyl (B) pyrrol-1 (2H)- acetic acid amides and

A unique series of saturated cycloalkyl[c]-pyrrol-2(1H)-acetic acid amides are useful as agents for the reversal of amnesia. Intermediates for preparing the compounds, pharmaceutical composition containing the compounds, and methods for using the pharmaceutical compositions for treating senility and for the reversal of amnesia are described.

Saturated cycloalkyl[c] pyrrole-2(1H)-acetic acid amides and derivatives

Cardiotonic and antihypertensive imidazole or triazole substituted phenyl-4H-1,3,4-oxadiazin-5(6H)-ones are described including pharmaceutical compositions and methods of administering the active ingredients. The subject compounds may be manufactured by ring closing appropriate derivatives of benzoic acid-2-(haloacetyl)hydrazides with sodium hydride.

Cardiotonic and antihypertensive oxadiazinone compounds

A pharmaceutical preparation comprising flutamide, useful in the treatment of prostatic carcinoma, is disclosed.

Pharmaceutical preparations comprising flutamide

This application relates to treatment of prostatic carcinoma with 4'-nitro-3'-trifluoromethylisobutyranilide.

Antiandrogenic agents and methods for the treatment of androgen

Disclosed herein are di-O-(aminoglycosyl)-1,3-diaminocyclitol antibacterial agents having on the 1-N-position of the 1,3-diaminocyclitol moiety a dipeptidyl or a tripeptidyl substituent. The compounds are useful antibacterial agents, as are their non-toxic pharmaceutically acceptable acid addition salts. Also disclosed are methods for preparing such agents from di-O-(aminoglycosyl)-1,3-diaminocyclitol antibacterial agents which are unsubstituted at the 1-N-position.

1-Peptidyl derivatives of di-O-aminoglycosyl-1,3-diaminocyclitol

This application relates to certain 4'-substituted and to 3',4'-disubstituted anilides, to methods for their preparation and to methods for their use as antiandrogens. These substituted anilides are useful in the treatment of androgen dependent disease states, such as benign prostatic hypertrophy, hirsutism, acne and the like.

This application relates to certain 4'-substituted and to 3',4'-disubstituted anilides, to methods for their preparation and to methods for their use as anti-androgens.

Growing community of inventors

Ann Arbor, MI, United States of America

John G Topliss