Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

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

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

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.