Abstract: .alpha.-(Cyclic tert. aminophenoxy)-alkanoic acids, e.g., those of the formula ##EQU1## AND FUNCTIONAL DERIVATIVES THEREOF ARE ANTI-INFLAMMATORY AND HYPOLIPIDEMIC AGENTS.
Abstract: wherein Ph denotes a 1,2-phenylene radical which carries cycloaliphatic radical, R.sub.x denotes a free or etherified hydroxyl group or a free or substituted amino group, R.sub.o denotes an alkyl radical, a free hydroxyl group or a hydroxyl group etherified by lower alkyl or, above all, a hydrogen atom and R.sub.1 denotes an aliphatic or cycloaliphatic hydrocarbon radical which is optionally substituted by hydroxyl, an araliphatic radical or a hydrogen atom, and their salts, which possess valuable analgesic, anti-inflammatory, anti-microbial and histamine liberation inhibiting properties.
Type:
Grant
Filed:
May 6, 1974
Date of Patent:
June 1, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Pier Giorgio Ferrini, Georges Haas, Alberto Rossi
Abstract: Piperidines of the formula ##SPC1##In which R.sub.1 stands for optionally substituted aryl, R.sub.2 for hydrogen, lower alkyl, lower alkenyl, acyl or .alpha.-aryl-lower alkyl, R.sub.3 for a free or substituted hydroxyl group, alk for lower alkylene which separates the two nitrogen atoms by 2 or 3 carbon atoms, R.sub.4 represents hydrogen or lower alkyl and n represents an integer from 1 to 4, and their salts as well as processes for their manufacture and pharmaceutical compositions comprising such compounds, and a process for lowering the blood pressure wherein such compositions are administered to a warm-blooded host.
Type:
Grant
Filed:
June 27, 1974
Date of Patent:
May 11, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Max Wilhelm, Kurt Eichenberger, Herbert Schroter, Franz Ostermayer
Abstract: Synthetic hypocalcaemic dotriacontapeptide of the formulaH-Cys-Ser-Asn-Leu-Ser--Thr-Cys-Val-Leu-Ser-Ala-Tyr-Try-Arg-Asn-Leu-Asn-Asn- Phe-His-Arg-Phe-Ser-Gly-Met-Gly-Phe-Gly-Pro-Glu-Thr-Pro-OH Iand analogues and derivatives, salts and complexes thereof and process for their manufacture.
Type:
Grant
Filed:
December 10, 1971
Date of Patent:
May 11, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Max Brugger, Friedrich Werner Kahnt, Bruno Kamber, Robert Neher, Bernhard Riniker, Werner Rittel, Peter Sieber, Herbert Zuber, Hendrik Marie Greven
Abstract: 6-Acylamino-penam-3-carboxylic acids and 7-acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula ##EQU1## in which R.sub.1 is hydrogen, R.sub.2 is optionally substituted phenyl, thienyl or furyl, or R.sub.1 and R.sub.2 together are optionally substituted cycloalkyl, and B is a radical which is bonded via a sulphur atom or is bonded to oxygen or sulphur with the interposition of an optionally substituted CH.sub.2 -group.
Type:
Grant
Filed:
March 22, 1973
Date of Patent:
May 4, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Karoly Kocsis, Bruno Fechtig, Hans Bickel
Abstract: The present invention relates to condensed pyrrole mercapto compounds, especially to optionally substituted indole or aza-indole mercapto derivatives, which compounds have ophthalmological and hypotensive properties, in particular vasoconstrictor, especially decongestant properties. It further relates to pharmaceutical compositions containing these compounds. An illustrative example is 3-(2-imidazolin-2-ylthio)-indole hydrochloride or hydroiodide.
Abstract: .alpha.-Halogen-nitrones of the formula ##EQU1## wherein Hal is a bromine or preferably a chlorine atom, R.sub.1 represents a cycloalkyl or an alkyl radical and R.sub.2 is hydrogen or an organic radical.
Abstract: Compounds of the formula ##SPC1##Wherein Z.sub.4 and Z.sub.5 each independently represent free, etherified or esterified hydroxy groups, are produced by diazotisation of 2-exo-amino-3,4-endo-dihydroxy-8-Z.sub.4 -7-oxabicyclo [4,3,0]nonane followed by ring contraction, they are intermediates in the synthesis of prostaglandins.
Abstract: 4-Arylcarbamoyl-2,3,4,5-tetrahydro-1-benzazepine-2,5-diones, e.g. those of the fromula ##SPC1##R = h, alkyl or aralkylAr = iso- or heterocyclic arylR',r" = h, alkyl, alkanoyl, alkoxy, halogen or CF.sub.3alkali metal or acid addition salts thereof are antiinflammatory agents.
Abstract: Compounds of the class of substituted or unsubstituted 4-amino-3-(5-nitro-2-furyl)-1H-pyrazolo[3,4-d]pyrimidine and their 5-N oxides have antimicrobial properties and are active ingredients in pharmaceutical compositions and animal feedstuff compositions, an illustrative example is 4-amino-1-methyl-3-(5-nitro-2-furyl)-1H-pyrazolo[3,4-d]pyrimidine.
Abstract: Compounds of the class of 6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxamides, their 5-oxides and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties and are active ingredients for therapeutic compositions. In particular, these new compounds have an anti-convulsive and anti-aggressive action and potentiate the action of anaesthetics. Specific embodiments are N,N-dimethyl-6-phenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-c arboxamide, 6-phenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxamide, N,N-dimethyl-6-(o-chlorophenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiaz epine-1-carboxamide and 6-(o-chlorophenyl)-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carb oxamide.
Abstract: Peptides of the calcitonin type when obtained by synthesis can be purified in a simple manner by forming inner salts, which precipitate from aqueous solutions of salts of the peptides with acids or bases when these solutions are adjusted to the isoelectric range. Impurities remain in solution, while the inner salts separate practically quantitatively. The precipitation is completed after several hours. The peptides can then be recuperated by treatment with an acid, especially a therapeutically suitable acid. The process affords products which are superior to those obtained by purification methods hitherto known and gives higher yields. Other long-chain peptides such as ACTH, insulin or glucagon cannot be purified in this manner.
Type:
Grant
Filed:
December 3, 1974
Date of Patent:
April 6, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Werner Rittel, Max Brugger, Bernhard Riniker
Abstract: 6-Aryl-1 or 2H,4H-pyrazolo[4,3-d](2)-benzazepines, e.g. those of the formula ##SPC1##R = h or alkylR.sup.o = H, alkyl, (HO, alkoxy, amino)-alkyl, aralkyl or arylR' = h, oh or alkylR" = h, alkyl, alkoxy, halo or CF.sub.35,6-dihydro- or 5-alkyl-5,6-dihydro-derivatives, N-oxides, acyl derivatives or therapeutically useful acid addition salts thereof exhibit antianxiety and antidepressant effects.
Abstract: Cpmpounds of the class of 5-substituted and 5,6-disubstituted 2-amino-4-(hydroxyamino) and 2,4-bis-(hydroxyamino)pyrimidines and their pharmaceutically acceptable acid addition salts possess valuable biological properties, in particular antibacterial and antimalarial activity and potentiate the action of antibacterial sulphanilamide derivatives. Specific embodiments are 2-amino-4-(hydroxyamino)-5-(3,4,5-trimethoxybenzyl)-pyrimidine, and 2-amino-4-(hydroxyamino)-5-(p-chlorophenyl)-6-ethyl pyrimidine and its hydrochloride.
Type:
Grant
Filed:
August 20, 1974
Date of Patent:
March 30, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Ernst Schweizer, Jorg Frei, Atso Ilvespaa
Abstract: Compounds of the class of acetals of 6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxaldehyde and the 5-oxides and pharmaceutically acceptable acid addition salts thereof have valuable pharmacological properties, in particular anticonvulsant effectiveness. Further, they show central depressant and muscle-relaxing activity and are active ingredients for therapeutic preparations. Specific embodiments are 6-phenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carboxaldehyde -diethylacetal, 6-(o-chlorophenyl)-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carb oxaldehyde-diethylacetal and 6-(o-fluorophenyl-8-chloro-4H-s-triazolo[4,3-a][1,4]benzodiazepine-1-carbo xaldehyde-diethylacetal.
Abstract: Dextrorotatory .alpha.-(4-aminophenyl)-.alpha.-lower alkylglutarimides or salts thereof normalize the secretion of malfunctioning adrenal glands.
Abstract: Temporary protection of amino groups by the group of the formula I ##EQU1## in which R.sub.1 represents lower alkyl, R.sub.2 lower alkyl or phenyl and R.sub.3 phenyl, and wherein the phenyl radicals are unsubstituted or substituted by lower alkyl, phenyl or lower alkylphenyl groups.
Abstract: Compounds of the formula ##EQU1## in which X represents a free carboxyl group or in the second place an esterified or amidated carboxyl group; R represents a 1-cycloalkenyl residue; Ph represents an ortho-phenylene residue or especially a para-phenylene residue; and R.sub.1 and R.sub.2 each represents a hydrogen atom or a monovalent or together a divalent aliphatic or araliphatic hydrocarbon residue, e.g. the .alpha.-[p-(1-cyclohexenyl)-phenyl]-propionic acid, are useful as analgetic and antiinflammatoric agents.
Abstract: Compounds of the class of 6-phenyl-4H-v-triazolo[1,5-a][1,4] benzodiazepines, which in the 3-position are unsubstituted or substituted, particularly by a carbamoyl group or a substituted carbamoyl group, their 5-oxides and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties and are active ingredients for therapeutic compositions. In particular, these new compounds have an anticonvulsive and anti-aggressive action. Specific embodiments are N,N-dimethyl-6-phenyl-8-chloro-4H-v-triazolo [1,5-a][1,4]benzodiazepine-3-carboxamide and N,N-dimethyl-6-(o-fluorophenyl)-8-chloro-4H-v-triazolo [1,5-a][1,4]benzodiazepine-3-carboxamide.
Type:
Grant
Filed:
December 20, 1973
Date of Patent:
March 9, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Andre Gagneux, Roland Heckendorn, Rene Meier