Patents Represented by Attorney Prabodh I. Almaula
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Patent number: 4447360Abstract: 2-Penem-3-carboxylic acid compounds of the formula ##STR1## in which R.sub.1 represents hydrogen, an organic radical bonded by a carbon atom to the ring carbon atom or an etherified mercapto group andR.sub.2 represents hydroxy or a radical R.sub.2.sup.A forming together with the carbonyl grouping --C(.dbd.O)-- a protected carboxyl group,1-oxides thereof, as well as salts of such compounds having salt-forming groups, in racemic and optically active form, processes for their preparation, pharmaceutical compositions containing such compounds, and their use as antibiotics, and intermediates and their processes which are useful in the production of the compounds of the formula I.Type: GrantFiled: December 8, 1980Date of Patent: May 8, 1984Assignee: Ciba-Geigy CorporationInventors: Jacques Gosteli, Ivan Ernest, Robert B. Woodward
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Patent number: 4386097Abstract: 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 29, 1981Date of Patent: May 31, 1983Assignee: Ciba-Geigy CorporationInventors: Srinivasachari Rajappa, Vasudevan Sudarsanam
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Patent number: 4376166Abstract: 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: GrantFiled: June 3, 1981Date of Patent: March 8, 1983Assignee: Ciba-Geigy CorporationInventors: Thomas Schupp, Peter Traxler, Jakob Nuesch
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Patent number: 4374129Abstract: N-acylated 11-amino derivatives of papulacandin A or B of the formula I ##STR1## in which Pap is the remainder of papulacandin A or B, R represents methyl or hydrogen and Ac represents the acyl radical of an organic acid, including salts of compounds with salt-forming properties, are distinguished by their antibiotic, especially antimycotic, action and can be used for combating infections of that type, especially those caused by Candida albicans. The compounds are produced according to conventional processes from corresponding 11-unsubstituted papulacandin derivatives.Type: GrantFiled: December 14, 1981Date of Patent: February 15, 1983Assignee: Ciba-Geigy CorporationInventor: Peter Traxler
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Patent number: 4369179Abstract: Acylpeptides derived from somatostatin or from a derivative thereof having analogous action, in which the amino acids sequence is modified by omitting individual amino acids and/or by exchanging them for other amino acids, and in which the .epsilon.-amino group of the lysine residue in the 9-position, and optionally also the .epsilon.-amino group of the lysine residue in the 4-position and/or the N-terminal .alpha.-amino group carries the acyl radical of an optionally substituted alkanecarboxylic acid, and salts and complexes thereof can be used as antidiabetics and/or for combating gastrointestinal bleeding. They are manufactured by conventional methods of peptide chemistry.Type: GrantFiled: December 5, 1980Date of Patent: January 18, 1983Assignee: Ciba-Geigy CorporationInventors: Hans Rink, Peter Sieber, Bruno Kamber
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Patent number: 4364865Abstract: The invention relates to 6-amino-2-penem-3-carboxylic acid compounds of the formula ##STR1## in which R.sub.1.sup.a denotes hydrogen or an amino protective group R.sub.1.sup.A and R.sub.1.sup.b represents hydrogen or an acyl radical Ac, or in which R.sub.1.sup.a and R.sub.1.sup.b conjointly form a bivalent amino protective group, R.sub.2 denotes hydroxyl or a radical R.sub.2.sup.A which, together with the carbonyl grouping --C(.dbd.O)--, forms a protected carboxyl group, and R.sub.3 represents hydrogen or an organic radical which is linked via a carbon atom to the ring carbon atom, and 1-oxides thereof, as well as salts of such compounds having salt-forming groups, which compounds possess antibiotic properties, processes for the manufacture of such compounds, and also pharmaceutical formulations containing compounds of the formula I with pharmacological properties, and the use thereof, either as antibiotics, preferably in the form of pharmaceutical formulations, or as intermediate products.Type: GrantFiled: June 11, 1980Date of Patent: December 21, 1982Assignee: Ciba-Geigy CorporationInventors: Ivan Ernest, Jacques Gosteli, Robert B. Woodward
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Patent number: 4361558Abstract: Novel halogenated steroids of the formula ##STR1## in which X represents a halogen atom having a maximum atomic number of 17,Y represents a hydrogen atom or hydroxyl, andR represents an alkyl radical having a maximum of 6 carbon atoms,and their 1,2-dehydro derivatives and the processes for the production thereof.Type: GrantFiled: April 21, 1981Date of Patent: November 30, 1982Assignee: Ciba-Geigy CorporationInventor: Peter Wieland
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Patent number: 4359555Abstract: Salts of formamidines with polymers containing sulfonic acid groups; processes for producing these salts; and the use thereof in combating pests.Type: GrantFiled: June 18, 1980Date of Patent: November 16, 1982Assignee: Ciba-Geigy CorporationInventors: Christian d'Hondt, Dieter Lohmann, Ernst Neuenschwander
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Patent number: 4358439Abstract: Cyclic peptides of the formula ##STR1## in which trp represents L-Trp, D-Trp, or an analogous radical which carries a halogen atom in the indole nucleus, Ac.sub.A represents hydrogen, or an acyl radical Ac of a carboxylic acid present at the .epsilon.-amino group, A represents L-Phe, D-Phe, L-Phg or D-Phg, or a corresponding radical having a substituted or saturated phenyl ring, and B represents the residue of a .gamma.- or .delta.-amino-lower alkanecarboxylic acid which may carry an optionally substituted cyclic hydrocarbyl radical Ar, and also pharmacologically tolerable salts and therapeutically acceptable complexes thereof can be used as an antidiabetic in an analogous manner to somatostatin. They can be obtained by conventional processes of peptide chemistry, especially by cyclisation of corresponding linear peptides.Type: GrantFiled: December 15, 1980Date of Patent: November 9, 1982Assignee: Ciba-Geigy CorporationInventors: Peter Sieber, Bruno Kamber, Hans Rink
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Patent number: 4353918Abstract: The invention relates to the dextrorotatory enantiomer of trans-5,6-di-p-methoxyphenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole and its pharmaceutically acceptable salts and to pharmaceutical preparations containing them.The new compounds have valuable pharmacological properties, especially anti-inflammatory and anti-rheumatic effects.Type: GrantFiled: December 22, 1980Date of Patent: October 12, 1982Assignee: Ciba-Geigy CorporationInventors: Richard Goschke, Pier G. Ferrini
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Patent number: 4353887Abstract: Divisible tablet having controlled and delayed release of the active substance and consisting of a compact that is optionally provided with a coating and is formed by at least one active substance in an adjunct composition that effects a delayed and controlled release of the active substance and optionally one or more additional adjunct compositions that optionally contain active substances and are arranged in longitudinal layers, the compact being of an oblong shape in which the ratio of length to width to depth is approximately 2.5 to 5: approximately 0.Type: GrantFiled: August 11, 1980Date of Patent: October 12, 1982Assignee: Ciba-Geigy CorporationInventors: Hans Hess, Carlo Voellmy
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Patent number: 4353826Abstract: Antibiotically active compounds derived from rifamycin S or from the corresponding hydroquinone, rifamycin SV, or from derivatives at least partially hydrogenated in positions 16, 17; 18, 19; 28, 29, such as the 16, 17; 18, 19--tetrahydro- or the 16, 17; 18, 19; 28, 29--hexahydro derivatives, which contain in position 3 a free or an aliphatically substituted amino group. The hydrocarbon radicals of the aliphatically substituted amino group can also be interrupted in their carbon chain by heteroatoms and/or be substituted by functional groups.A special group of these new compounds is represented by 3-amino derivatives as defined above, in which the amino group is a particular type of N-aza-cyclo-aliphatic radical unsubstituted by functional groups, and which has, in addition to the antibiotic action against sensitive microorganisms also an antibacterial activity against certain types of resistant microorganisms.Type: GrantFiled: September 30, 1980Date of Patent: October 12, 1982Assignee: Ciba-Geigy CorporationInventors: Hans Bickel, Wilhelm Kump
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Patent number: 4344957Abstract: New heterocyclylcarboxylic acid derivatives which are acylated in the nucleus, especially benz-acyl-benzimidazole-2-carboxylic acid derivatives of the formula ##STR1## in which R is a free, esterified or amidated carboxyl group or a free, etherified or esterified hydroxymethyl group, R.sub.1 is an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclic-aliphatic radical, R.sub.2 is hydrogen or an aliphatic radical and Ph is a 1,2-phenylene group containing the radical R.sub.1 --C(.dbd.O)--, with the proviso that R.sub.1 contains at least 2 carbon atoms if Ph is otherwise unsubstituted, R.sub.2 is ethyl and R is acetoxymethyl, and salts of such compounds having salt-forming properties, are useful as anti-allergic agents.Type: GrantFiled: December 28, 1979Date of Patent: August 17, 1982Assignee: Ciba-Geigy CorporationInventors: Ernst Habicht, Pier G. Ferrini, Alfred Sallmann
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Patent number: 4331676Abstract: 2-Penem-3-carboxylic acid compounds of the formula ##STR1## in which R.sub.1 represents hydrogen, an organic radical bonded by a carbon atom to the ring carbon atom or an etherified mercapto group andR.sub.2 represents hydroxy or a radical R.sub.2.sup.A forming together with the carbonyl grouping --C(.dbd.O)-- a protected carboxyl group, 1-oxides thereof, as well as salts of such compounds having salt-forming groups, in racemic and optically active form, processes for their preparation, pharmaceutical compositions containing such compounds, and their use as antibiotics, and intermediates and their processes which are useful in the production of the compounds of the formula I.Type: GrantFiled: May 4, 1978Date of Patent: May 25, 1982Assignee: Ciba-Geigy CorporationInventors: Jacques Gosteli, Ivan Ernest, Robert B. Woodward
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Patent number: 4329348Abstract: N-Oxacyclic-alkylpiperidyl-diazacompounds, e.g., those of the formula ##STR1## and salts thereof are antidepressants and psychostimulants.Type: GrantFiled: September 12, 1980Date of Patent: May 11, 1982Assignee: Ciba-Geigy CorporationInventor: Charles F. Huebner
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Patent number: 4328214Abstract: The somatostatin-analogous cyclic octapeptides according to the invention of the general formula ##STR1## in which trp represents L-Trp or D-Trp, in which the benzene ring may be substituted by a halogen atom, andGaba(Ar) represents the residue of a .gamma.-aminobutyric acid substituted by a cyclic hydrocarbyl radical,and their acid addition salts and complexes are distinguished by a strong inhibition of the insulin and glucagon secretion of the pancreas and are therefore therapeutically acceptable, preferably in the form of pharmaceutical preparations, in similar indications to those of somatostatin, especially as anti-diabetics. The compounds are manufactured by conventional processes of peptide synthesis, especially by liberation from corresponding protected intermediates after intramolecular cyclization of a corresponding linear octapeptide.Type: GrantFiled: June 25, 1980Date of Patent: May 4, 1982Assignee: Ciba-Geigy CorporationInventors: Hans Rink, Peter Sieber, Bruno Kamber
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Patent number: 4327091Abstract: 3,4-Dihydro-2H-1,2-benzothiazine 1,1-dioxides of the formula ##STR1## wherein Ph represents a substituted or unsubstituted 1,2-phenylene radical, R represents a substituted or unsubstituted benzopyrone radical, and R.sub.1 represents hydrogen or a substituted or unsubstituted hydrocarbon radical of aliphatic character, and their salts, possess antiinflammatory properties and are useful as medicaments.Type: GrantFiled: January 28, 1980Date of Patent: April 27, 1982Assignee: Ciba-Geigy CorporationInventors: Alex Sele, Pier G. Ferrini, Georges Haas, Knut A. Jaeggi, Alberto Rossi
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Patent number: 4323688Abstract: Novel substituted heterocyclyl compounds of the formula ##STR1## in which R is a free, esterified or amidated carboxyl group or a free, etherified or esterified hydroxymethyl group, R.sub.1 is an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclic-aliphatic radical, R.sub.2 is hydrogen or an aliphatic radical and Ph is a 1,2-phenylene group containing the radical R.sub.1 -X, and X is lower alkylidene or a direct bond, and pharmaceutically usable salts of compounds of the formula I with salt-forming properties as medicaments, pharmaceutical preparations containing these, their use as medicaments and also novel compounds of the formula I and salts of compounds of the formula I with salt-forming properties, with the proviso that R.sub.1 -X-Ph differs from 1,2-phenylene substituted by methyl in the 4- and/or 5-position when R is carboxyl, carbamyl or hydroxymethyl and R.sub.2 is hydrogen, and pharmaceutically acceptable salts thereof are useful as anti-allergic agents.Type: GrantFiled: July 27, 1978Date of Patent: April 6, 1982Assignee: Ciba-Geigy CorporationInventors: Ernst Habicht, Pier G. Ferrini, Alfred Sallmann
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Patent number: 4323560Abstract: Phosphorylmuramyl peptides of the formula ##STR1## are immuno-potentiating. In the formula, R.sub.1 represents optionally substituted alkyl or aryl, R.sub.2, R.sub.4, R.sub.6 and R.sub.7 represent, for example, hydrogen, R.sub.3 represents hydrogen or lower alkyl, R.sub.5 represents, for example, hydrogen, lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl or aralkyl, or nitrogen-containing heterocyclyl or heterocyclyl-lower alkyl, and one of the radicals A.sub.1 and A.sub.2 represents a radical of the formula (II) ##STR2## In the formula (II), T represents NH or O, Y represents an optionally substituted alkylene group, which may also be interrupted by one or two oxycarbonyl and/or iminocarbonyl groups, and W represents an aliphatic radical or a cycloalkyl or cycloalkenyl radical having more than 6 carbon atoms. The other of the radicals A.sub.1 and A.sub.2 represents free or etherified hydroxy, amino, lower alkylamino or aminocarbonyl-lower alkylamino.Type: GrantFiled: October 6, 1980Date of Patent: April 6, 1982Assignee: Ciba-Geigy CorporationInventors: Gerhard Baschang, Lajos Tarcsay, Albert Hartmann, Jaroslav Stanek
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Patent number: 4322419Abstract: Derivatives of 5-norbicyclomycin of the formula ##STR1## wherein R represents an unsubstituted or substituted monovalent hydrocarbon radical in which one, two or more carbon atoms can be replaced by heteroatoms, and X represents a bivalent group of the formula --O-- or --N(R')--, wherein R' has one of the meanings assigned to R, whilst R and R', if both have a meaning which is different from hydrogen, can also be linked to each other through a C--C bond or an oxygen, sulphur or nitrogen atom, and corresponding compounds, in which at least one hydroxyl group is protected, and salts of said compounds, provided they contain salt-forming groups, are useful as antibiotics, especially against Enterobacteriaceae, or as intermediates for the production of such antibiotics. They are obtained by condensing a corresponding 5-norbicyclomycin-5-one with a compound of the formula R--X--NH.sub.2 in which X and R have the above meaning.Type: GrantFiled: January 8, 1979Date of Patent: March 30, 1982Assignee: Ciba-Geigy CorporationInventors: Beat Muller, Wilhelm Kump, Oskar Wacker