Patents Represented by Attorney Prabodh I. Almaula
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Patent number: 4322431Abstract: Benzimidazole 2-derivatives that are acylated in the nucleus and have the formula ##STR1## in which R.sub.1 represents an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclic-aliphatic radical,R.sub.2 represents hydrogen or an aliphatic radical, andPh represents a 1,2-phenylene group containing the radical R.sub.1 --C(.dbd.O)--,have anti-allergic properties, serve as medicaments and can be used as medicinal active substances in pharmaceutical preparations.Type: GrantFiled: January 28, 1980Date of Patent: March 30, 1982Assignee: Ciba-Geigy CorporationInventors: Ernst Habicht, Pier G. Ferrini, Alfred Sallmann
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Patent number: 4320137Abstract: The present invention provides new derivatives of perhydro-aza-heterocycles of the formula ##STR1## in which X is the oxo radical or hydrogen and the radical OR.sub.1, in which R.sub.1 is hydrogen or a substituted or unsubstituted aliphatic hydrocarbon radical, a substituted or unsubstituted araliphatic hydrocarbon radical or a substituted or unsubstituted aromatic hydrocarbon radical or an acyl radical, R.sub.2 is hydrogen or a substituted or unsubstituted aliphatic hydrocarbon radical, Y is oxygen or sulphur, n.sub.1 and n.sub.2 each are values of 1 to 3, n.sub.1 +n.sub.2 being at most four, and Ar is a substituted or unsubstituted aromatic hydrocarbon radical, and the acid addition salts, in particular the pharmaceutically acceptable acid addition salts thereof. These new substances possess valuable pharmacological properties, in particular antidepressant activity, and can be used for the treatment of mental depressions.Type: GrantFiled: September 28, 1980Date of Patent: March 16, 1982Assignee: Ciba-Geigy CorporationInventor: Romeo Paioni
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Patent number: 4320138Abstract: Oxothia compounds, especially 2-oxo-2,3-dihydro-benzo[b]-thiophene compounds of the formula ##STR1## in which Ph represents an optionally substituted 1,2-phenylene radical, X represents oxygen or sulphur, R.sub.1 represents an organic radical bonded via a carbon atom and R.sub.2 denotes hydrogen or an optionally substituted hydrocarbon radical of aliphatic character, and their salts are useful as peripheral analgetics and/or as antiphlogistic uricosuric and/or thrombolytic agents.Type: GrantFiled: December 8, 1980Date of Patent: March 16, 1982Assignee: Ciba-Geigy CorporationInventors: Raymond Bernasconi, Pier G. Ferrini, Richard Goschke, Jacques Gosteli
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Patent number: 4318926Abstract: Method for the treatment of herpes infections by administering a compound of the formula ##STR1## in which alk represents alkylene containing 1 to 4 carbon atoms,R.sub.1 and R.sub.2 independently of each other, represent hydrogen, alkyl containing 1 to 4 carbon atoms or together represent an alkylene radical containing 4 to 6 carbon atoms,R.sub.3 represents hydrogen, methyl or chlorine, andthe rings A and B, independently of each other, are unsubstituted or may be substituted by chlorine,or their pharmaceutically acceptable acid addition salts, and also the pharmaceutical compositions suitable for use in this method.Type: GrantFiled: August 6, 1980Date of Patent: March 9, 1982Assignee: Ciba-Geigy CorporationInventors: Karl H. Schmidt-Ruppin, Bohumir Lukas, Walter Wiesendanger
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Patent number: 4319027Abstract: The invention concerns a process for the manufacture of 7.beta.-amino-3-cephem-3-ol-4-carboxylic acid compounds by ring closure of esters of 2-[4-(substituted-thio)-3-acylamino-2-oxoazetidin-1-yl]-3-substituted-amin o-crotonic acids and solvolysing the enamino group in the resulting 7.beta.-acylamino-3-substituted-amino-cephem-4-carboxylic acid esters.Type: GrantFiled: May 7, 1979Date of Patent: March 9, 1982Assignee: Ciba-Geigy CorporationInventors: Robert B. Woodward, Hans Bickel
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Patent number: 4316890Abstract: The somatostatin-analogous peptides according to the invention of the general formula ##STR1## in which Bmp represents the desaminocysteine radicalX represents Asn or His,trp represents D-Trp that may be substituted in the benzene ring by a halogen atom, andY represents the radical of a secondary .alpha.-amino acid having a maximum of 8 carbon atomsand the corresponding peptide amides and also acid addition salts and complexes thereof are distinguished by strong insulin-antagonistic and glucagon-antagonistic effects and are therefore therapeutically acceptable, preferably in the form of pharmaceutical preparations, in similar indications to those of somatostatin, especially also as antidiabetics. The compounds are manufactured by conventional processes of peptide synthesis, especially by liberation from corresponding protected intermediates and by the formation of the cystine disulphide bridge by means of oxidation.Type: GrantFiled: March 10, 1980Date of Patent: February 23, 1982Assignee: Ciba-Geigy CorporationInventors: Bruno Kamber, Hans Rink, Peter Sieber
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Patent number: 4316850Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## and functional derivatives thereof, are anti-inflammatory agents.Type: GrantFiled: November 16, 1972Date of Patent: February 23, 1982Assignee: Ciba-Geigy CorporationInventors: Richard W. J. Carney, George deStevens
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Patent number: 4313945Abstract: The invention relates to aminothiazolacetamido-3-cephem-4-carboxylic acid compounds of the formula ##STR1## in which the index n represents an integer of 1 to 4,X represents oxygen, sulphur, an --NH-- group or the direct bond,Y represents oxygen or sulphur,A represents methylene or methylene substituted by amino, hydroxy, carboxyl, sulpho, oxo, or the group .dbd.N--O--R.sup.o in which R.sup.o represents hydrogen or optionally substituted lower alkyl,R.sub.1 represents hydrogen, lower alkyl, an esterified or etherified hydroxy or mercapto group, halogen, formyl or a group of the formula --CH.sub.2 --R.sub.2 in which R.sub.2 represents an esterified or etherified hydroxy or mercapto group or a quaternary ammonium group, andR.sub.3 represents hydrogen or methoxy,in which functional groups are optionally present in protected form,salts of such compounds with acidic and/or basic groups, processes for the manufacture of these compounds, pharmaceutical agents containing such substances and their therapeutic use.Type: GrantFiled: November 13, 1979Date of Patent: February 2, 1982Assignee: Ciba-Geigy CorporationInventors: Rene Wiederkehr, Riccardo Scartazzini
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Patent number: 4312870Abstract: 2-Aryl-pyrazolo[4-3-c]quinolin-3-ones, e.g. those of the formula ##STR1## and pharmaceutically acceptable acyl derivatives or salts thereof, are psychoactive agents useful in the treatment of anxiety or depression.Type: GrantFiled: May 16, 1980Date of Patent: January 26, 1982Assignee: Ciba-Geigy CorporationInventor: Naokata Yokoyama
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Patent number: 4310527Abstract: A compound of the formula ##STR1## in which R.sub.1 denotes optionally substituted lower alkyl which is optionally branched at the linking carbon atom, R.sub.2 represents hydrogen or lower alkanoyl and R.sub.3 is a group of the formula --R.sub.3.sup.a --(R.sub.3.sup.b).sub.n -- (Ia), in which R.sub.3.sup.a represents the radical of the formula --N(R.sub.4)-- or --O-- and R.sub.4 represents hydrogen or lower alkyl, R.sub.3.sup.b denotes the radical of the formula --CH.sub.2 -- or, if R.sub.3.sup.a represents --N(R.sub.4)--, denotes the radical of the formula --C(.dbd.O)-- and n represents nought or 1, and a group of the formula Ia, in which n represents 1, can be linked to the carbonyl group of the carbamoyl grouping either via the group R.sub.3.sup.a or the group R.sub.3.sup.b, or acid addition salts thereof, which can be used pharmaceutically can be used as beta-receptor blocking agents for the treatment of disorders in the cardiac rhythm and coronary heart diseases.Type: GrantFiled: March 8, 1979Date of Patent: January 12, 1982Assignee: Ciba-Geigy CorporationInventors: Knut A. Jaeggi, Franz Ostermayer, Herbert Schroter
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Patent number: 4309353Abstract: New benzopyrane derivatives of the general formula ##STR1## in which R is free, esterified or amidated carboxyl, Ph is 1,2-phenylene which contains the group R--CO--NR.sub.3 -- and is otherwise unsubstituted or is substituted, X is a group of the formula --CO--CR.sub.1 .dbd.CR.sub.2 --, in which R.sub.1 and R.sub.2 independently of one another are hydrogen, acyl or a substituted or unsubstituted hydrocarbon radical or a hetero-analogue thereof, or conjointly are 3-membered to 5-membered lower alkylene, and R.sub.2 can also be free or etherified hydroxyl or hydroxyl etherified by an organic carboxylic acid, and R.sub.3 is hydrogen or lower alkyl, are useful as anti-allergic agents.Type: GrantFiled: November 21, 1979Date of Patent: January 5, 1982Assignee: Ciba-Geigy CorporationInventor: Pier G. Ferrini
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Patent number: 4308277Abstract: Compounds of the formula ##STR1## in which R.sub.1 and R.sub.2 independently of one another are substituted or unsubstituted aryl or hetero-aryl groups, R.sub.3 is hydrogen or lower alkyl and R.sub.4 is a substituted or unsubstituted aliphatic hydrocarbon radical, and their pharmaceutically usable salts. These compounds possess immunoregulatory, antithrombotic and antiinflammatory properties and can be used as active ingredients in medicaments. They are prepared, for example, by reacting compounds of the formulae ##STR2## in which one of the radicals X and Y is mercapto, which can be in the form of a salt, and the other is a radical replaceable by etherified mercapto, with one another.Type: GrantFiled: July 30, 1979Date of Patent: December 29, 1981Assignee: Ciba-Geigy CorporationInventors: Pier G. Ferrini, Richard Goschke
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Patent number: 4304912Abstract: Piperidines of the formula ##STR1## in which R.sub.1 is a substituted or unsubstituted heteroaryl radical, alk.sub.1 and alk.sub.2 independently of one another are lower alkylene radicals, each of which separates by 2 carbon atoms the nitrogen atom bonded thereto from the methane group bonded thereto, R.sub.2 is a free or acylated hydroxyl group, Ph is a substituted or unsubstituted o-phenylene radical, n is 0 or 1, R.sub.3 is a hydrogen atom, a lower alkyl radical or a hydroxyl group and R.sub.5 is a lower alkyl radical or a hydrogen atom, or R.sub.3 and R.sub.5 together are a second bond and R.sub.4 and R.sub.6 are each a hydrogen atom, or R.sub.4 together with R.sub.3 is an oxo group, R.sub.5 is a lower alkyl radical or a hydrogen atom and R.sub.6 is a hydrogen atom, or R.sub.6 together with R.sub.5 is an oxo group, R.sub.3 is a hydrogen atom, a lower alkyl radical or a hydroxyl group and R.sub.4 is a hydrogen atom, or salts thereof are antihypertensive and antiarrhythmic agents.Type: GrantFiled: December 10, 1979Date of Patent: December 8, 1981Assignee: Ciba-Geigy CorporationInventors: Herbert Schroter, Kurt Eichenberger, Hans Kuhnis, Christian Egli, Oswald Schier, Franz Ostermayer
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Patent number: 4301279Abstract: Process for the production of 7.beta.-substituted 3-hydroxycepham-4-carboxylic acid compounds of the formula ##STR1## in which R.sub.1.sup.a represents hydrogen or an amino-protecting group R.sub.1.sup.A, andR.sub.1.sup.b represents hydrogen or an acyl radical Ac,or in whichR.sub.1.sup.a and R.sub.1.sup.b together form a bivalent amino-protecting group, andR.sub.2 represents a radical that, together with the carbonyl grouping --C(.dbd.O)--, forms a protected carboxyl group,and 1-oxides thereof as well as salts of such compounds with salt-forming groups, from a 7.beta.-substituted 3-hydroxy-3-cephem-4-carboxylic acid compound of the formula ##STR2## from a 1-oxide or a salt thereof, and a complex borohydride, characterized in that the reduction is carried out in the presence of an organic acid.The reduction in the presence of an organic acid produces higher yields.Type: GrantFiled: February 13, 1980Date of Patent: November 17, 1981Assignee: Ciba-Geigy CorporationInventor: Riccardo Scartazzini
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Patent number: 4298692Abstract: New antibiotically active compounds having the basic structure of rifamycin S, namely 3-hydroxyrifamycin S (formula A: X.dbd.>C.dbd.O; R.sup.1 .dbd.OH; R.sup.2 .dbd.H), 3,31-dihydroxyrifamycin S (formula A: X.dbd.>C.dbd.O; R.sup.1 .dbd.R.sup.2 .dbd.OH) and 1-desoxy-1-oxarifamycin S (formula A: X.dbd.--O--; R.sup.1 .dbd.R.sup.2 .dbd.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: GrantFiled: January 17, 1980Date of Patent: November 3, 1981Assignee: Ciba-Geigy CorporationInventors: Thomas Schupp, Peter Traxler, Jakob Nuesch
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Patent number: 4297358Abstract: New 4,7-phenanthroline derivatives of the formula (I) ##STR1## in which Ch represents an optionally substituted 5,6-quinolinylene radical of which the 6-position is joined to the --N(R.sub.E)-- group, andR represents an optionally esterified or amidated carboxy group,and in which eitherR.sub.A and R.sub.B together represent oxo,R.sub.C and R.sub.D together represent an additional link, andR.sub.E represents a radical R.sub.1 which is hydrogen, or an aliphatic, cycloaliphatic, araliphatic or heterocyclic-aliphatic radical, orR.sub.A represents an optionally etherified hydroxy group andR.sub.B together with R.sub.C and R.sub.D together with R.sub.E in each case represents an additional link,and salts of salt-forming compounds of the formula (I), compounds of the formula (I) or the salts thereof have anti-allergic properties. They can be prepared in accordance with processes known per se and may be used as active substances in pharmaceutical preparations.Type: GrantFiled: January 4, 1980Date of Patent: October 27, 1981Assignee: Ciba-Geigy CorporationInventors: Georges Haas, Knut A. Jaeggi, Alberto Rossi, Alex Sele
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Patent number: 4297365Abstract: The invention relates to 2-carboethoxyamino-5(6)-(2-amino-5-thiazoloyl)-benzimidazole compounds with anthelmintic properties and to processes for their preparation and pharmaceutical preparations containing such compounds.Type: GrantFiled: July 26, 1979Date of Patent: October 27, 1981Assignee: Ciba-Geigy CorporationInventors: Srinivasachari Rajappa, Vasudevan Sudarsanam
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Patent number: 4294966Abstract: The invention relates to a process for inverting the configuration in optically active compounds of the formula ##STR1## in which Ar.sub.1 represents a monocyclic or polycyclic, carbocyclic or heterocyclic radical that has at least one ring of aromatic character and is bonded to the oxygen atom by way of a ring carbon atom, preferably of the ring of aromatic character, andR.sub.1 represents an optionally substituted aliphatic, cycloaliphatic or araliphatic hydrocarbon radical,or the salts thereof, characterised in that an optically active compound of the formula ##STR2## having a R(+) or S(-) configuration, in which R.sub.2 represents a monocyclic or polycyclic, carbocyclic or heterocyclic radical, or an optionally substituted aliphatic, cycloaliphatic or araliphatic hydrocarbon radical,is converted, by treating with a strong oxygen-containing inorganic or organic acid or halides thererof, into an optically active compound of the formula ##STR3## in which X.sup..crclbar.Type: GrantFiled: July 16, 1979Date of Patent: October 13, 1981Assignee: Ciba-Geigy CorporationInventor: Janos Zergenyi
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Patent number: 4293462Abstract: The invention concerns a process for the manufacture of 7.beta.-amino-3-cephem-3-ol-4-carboxylic acid compounds by ring closure of esters of 2-[4-(substituted-thio)-3-acylamino-2-oxoazetidin-1-yl]-3-substituted-amin o-crotonic acids and solvolyzing the enamino group in the resulting 7.beta.-acylamino-3-substituted-amino-cephem-4-carboxylic acid esters.Type: GrantFiled: December 10, 1979Date of Patent: October 6, 1981Assignee: Ciba-Geigy CorporationInventors: Robert B. Woodward, Hans Bickel
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Patent number: 4292429Abstract: The invention relates to urea and amido compounds of the formula ##STR1## which have a powerful action on tumors, and to processes for their preparation and pharmaceutical preparations containing such compounds.Type: GrantFiled: February 23, 1979Date of Patent: September 29, 1981Assignee: Ciba-Geigy CorporationInventor: Adrian Marxer