Abstract: The novel 1-(2,3-dihydro-1,4-benzodioxin-2S-yl)-5-(2,3-dihydro-1,4-benzodioxin-2R-yl )-3-azapentane-1R,5S-diol, and pharmaceutically acceptable acid addition salts thereof, are efficacious antihypertensive and bradycardic agents. Pharmaceutical compositions, methods of preparation and novel intermediates are described.
Abstract: Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-benzazocin-2-one and benzazonin-2-one derivatives are disclosed as angiotensin converting enzyme inhibitors and antihypertensive agents. Synthesis of, pharmaceutical compositions and methods of treatment utilizing such compounds are included.
Abstract: 5-Diazacycloalkylimidazo[1,2-c][1,3]benzodiazepines, for example compounds of the formula ##STR1## in which e.g., R.sub.1, R.sub.2 and R.sub.4 are hydrogen, R.sub.3 is methyl and C.sub.n H.sub.2n is CH.sub.2 CH.sub.2, have neurcleptic and/or antihistaminic activity. The synthesis, pharmaceutical compositions and methods of treatment utilizing such compounds are described.
Abstract: Various 1-carboxylic acid substituted-2-pyridylindoles and functional derivatives thereof are highly specific thromboxane synthetase inhibitors. Synthesis of, pharmaceutical compositions thereof, and methods of treatment utilizing such compounds are included.
Abstract: 5-Diazacycloalkylimidazo[1,2-c][1,3]benzodiazepines, for example compounds of the formula ##STR1## in which e.g., R.sub.1, R.sub.2 and R.sub.4 are hydrogen, R.sub.3 is methyl and C.sub.n H.sub.2n is CH.sub.2 CH.sub.2, have neuroleptic and/or antihistaminic activity. The synthesis, pharmaceutical compositions and methods of treatment utilizing such compounds are described.
Abstract: 5-Diazacycloalkylimidazo[1,2-c][1,3]benzodiazepines, for example compounds of the formula ##STR1## in which e.g., R.sub.1, R.sub.2 and R.sub.4 are hydrogen, R.sub.3 is methyl and C.sub.n H.sub.2n is CH.sub.2 CH.sub.2, have neuroleptic and/or antihistaminic activity. The synthesis, pharmaceutical compositions and methods of treatment utilizing such compounds are described.
Abstract: Certain pyrazolo[4,3-c]quinolin-3-ones, e.g. those of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl or alkoxy with up to 4 carbon atoms each, hydroxy, fluoro, chloro, bromo or trifluoromethyl; and R is phenyl, fluorophenyl or pyridyl; or pharmaceutically acceptable salts thereof; and pharmaceutical compositions comprising above compounds are useful for suppressing appetite in mammals.
Abstract: 5-Diazacycloalkyl-imidazo[2,1-b][1,3,5]benzothiadiazepines, e.g. those of the formula ##STR1## the N-oxides and salts thereof are neuroleptic agents, lacking extrapyramidal side-effects.
Abstract: Disclosed are e.g. novel 5-(carboxyalkyl)imidazo[1,5-a]pyridines, their derivatives and methods of synthesis. Said compounds are useful as selective thromboxane synthetase inhibitors for the treatment of diseases such as cerebral ischaemia, shock, thrombosis and ischaemic heart disease.
Abstract: Various 1-carboxylic acid substituted-2-(1-imidazolyl)indoles and functional derivatives thereof are highly specific thromboxane synthetase inhibitors. Synthesis of, pharmaceutical compositions thereof, and methods of treatment utilizing such compounds are included.
Abstract: .beta.-Oxo-.alpha.-(heterocyclic substituted carbamoyl)-.beta.-pyrrolyl-propionitriles are antiinflammatory and/or antiarthritic agents with immunomodulating properties. Their synthesis, pharmaceutical compositions thereof, and methods of treatment utilizing such compounds are included.
Abstract: 7-Aryl-5H-dibenz[c,e]azepines, e.g., those of the formula ##STR1## wheren: Ar'=phenyl, furyl, thienyl, pyridyl or phenyl subst. by alkyl, OH, alkoxy, halo or CF.sub.3 ;R'=halo or CF.sub.3N-oxides or salts thereof are anxiolytic, tranquilizing and anti-convulsant agents.
Abstract: Certain 1,3,4,14b-tetrahydro-2H,10H-pyrazino?1,2-a!pyrrolo-?2,1-c!?1,4!benzodiazep ines e.g. those of the formula ##STR1## wherein R.sub.1 is lower alkyl or hydroxy(lower)alkyl; R.sub.2 is hydrogen, chloro or trifluoromethyl; pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising said compounds, are useful for the treatment of anxiety in mammals.
Abstract: Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzazepin -2-ones and functional derivatives are angiotension converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.
Abstract: 1-Carboxy-(alkanoyl or aralkanoyl)-1,2,3,4-tetrahydroquinoline-2-carboxylic acids, e.g., those of the formula ##STR1## R=H, alkyl, alkoxy, halogeno or CF.sub.3 ; R'=H or R-phenyl;m=0 or 1;p,q=0 to 2;and functional derivatives thereof, are antihypertensive and cardioactive agents.
Abstract: 5-Diazacycloalkyl-imidazo[2,1-b][1,3,5]benzothiadiazepines, e.g. those of the formula ##STR1## the N-oxides and salts thereof are neuroleptic agents, lacking extrapyramidal side-effects.
Abstract: 1-(Carboxy-azaalkanoyl or azaaralkanoyl)-1,2,3,4-tetrahydroquinoline-2-carboxylic acids, e.g., those of the formula ##STR1## and functional derivatives thereof, are antihypertensive and cardioactive agents.
Abstract: The novel 1-(2,3-dihydro-1,4-benzodioxin-2S-yl)-5-(2,3-dihydro-1,4-benzodioxin-2R-yl )-3-azapentane-1R,5S-diol, and pharmaceutically acceptable acid addition salts thereof, are efficacious antihypertensive and bradycardic agents. Pharmaceutical compositions, methods of preparation and novel intermediates are described.
Abstract: 2,3-Dihydro-1-benzothiepin-4-carboxamides, e.g those of the formula ##STR1## or their salts with therapeutically useful bases, exhibit anti-inflammatory effects.
Abstract: New antibiotically active compounds having the basic structure of rifamycin S, namely 3-hydroxyrifamycin S (formula A: X=<C.dbd.O; R.sup.1 =OH; R.sup.2 =H), 3,31-dihydroxyrifamycin S (formula A: X=<C.dbd.O; R.sup.1 =R.sup.2 =OH) and 1-desoxy-1-oxarifamycin S (formula A: X=--O--; R.sup.1 =R.sup.2 =H) ##STR1## are formed by cultivating, under aerobic conditions, a strain of Nocardia mediterranei which is derived from Streptomyces mediterranei ATCC 13 685 as the parent strain and is characterized by the ability to produce at least one of the mentioned compounds. The recombinant strain Nocardia mediterranei DSM 1415 has proved suitable. The mentioned rifamycin S analogues have analogous antibiotic properties to this but have a wider range of action, especially against gram-negative bacteria.
Type:
Grant
Filed:
June 3, 1981
Date of Patent:
March 8, 1983
Assignee:
Ciba-Geigy Corporation
Inventors:
Thomas Schupp, Peter Traxler, Jakob Nuesch