Patents Represented by Attorney Prabodh I. Almaula
  • Patent number: 4447360
    Abstract: 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: Grant
    Filed: December 8, 1980
    Date of Patent: May 8, 1984
    Assignee: Ciba-Geigy Corporation
    Inventors: Jacques Gosteli, Ivan Ernest, Robert B. Woodward
  • Patent number: 4386097
    Abstract: 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: Grant
    Filed: July 29, 1981
    Date of Patent: May 31, 1983
    Assignee: Ciba-Geigy Corporation
    Inventors: Srinivasachari Rajappa, Vasudevan Sudarsanam
  • Patent number: 4376166
    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
  • Patent number: 4374129
    Abstract: 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: Grant
    Filed: December 14, 1981
    Date of Patent: February 15, 1983
    Assignee: Ciba-Geigy Corporation
    Inventor: Peter Traxler
  • Patent number: 4369179
    Abstract: 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: Grant
    Filed: December 5, 1980
    Date of Patent: January 18, 1983
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Rink, Peter Sieber, Bruno Kamber
  • Patent number: 4364865
    Abstract: 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: Grant
    Filed: June 11, 1980
    Date of Patent: December 21, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Ivan Ernest, Jacques Gosteli, Robert B. Woodward
  • Patent number: 4361558
    Abstract: 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: Grant
    Filed: April 21, 1981
    Date of Patent: November 30, 1982
    Assignee: Ciba-Geigy Corporation
    Inventor: Peter Wieland
  • Patent number: 4359555
    Abstract: Salts of formamidines with polymers containing sulfonic acid groups; processes for producing these salts; and the use thereof in combating pests.
    Type: Grant
    Filed: June 18, 1980
    Date of Patent: November 16, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Christian d'Hondt, Dieter Lohmann, Ernst Neuenschwander
  • Patent number: 4358439
    Abstract: 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: Grant
    Filed: December 15, 1980
    Date of Patent: November 9, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Sieber, Bruno Kamber, Hans Rink
  • Patent number: 4353918
    Abstract: 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: Grant
    Filed: December 22, 1980
    Date of Patent: October 12, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Richard Goschke, Pier G. Ferrini
  • Patent number: 4353887
    Abstract: 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: Grant
    Filed: August 11, 1980
    Date of Patent: October 12, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Hess, Carlo Voellmy
  • Patent number: 4353826
    Abstract: 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: Grant
    Filed: September 30, 1980
    Date of Patent: October 12, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Bickel, Wilhelm Kump
  • Patent number: 4344957
    Abstract: 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: Grant
    Filed: December 28, 1979
    Date of Patent: August 17, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Ernst Habicht, Pier G. Ferrini, Alfred Sallmann
  • Patent number: 4331676
    Abstract: 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: Grant
    Filed: May 4, 1978
    Date of Patent: May 25, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Jacques Gosteli, Ivan Ernest, Robert B. Woodward
  • Patent number: 4329348
    Abstract: N-Oxacyclic-alkylpiperidyl-diazacompounds, e.g., those of the formula ##STR1## and salts thereof are antidepressants and psychostimulants.
    Type: Grant
    Filed: September 12, 1980
    Date of Patent: May 11, 1982
    Assignee: Ciba-Geigy Corporation
    Inventor: Charles F. Huebner
  • Patent number: 4328214
    Abstract: 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: Grant
    Filed: June 25, 1980
    Date of Patent: May 4, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Rink, Peter Sieber, Bruno Kamber
  • Patent number: 4327091
    Abstract: 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: Grant
    Filed: January 28, 1980
    Date of Patent: April 27, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Alex Sele, Pier G. Ferrini, Georges Haas, Knut A. Jaeggi, Alberto Rossi
  • Patent number: 4323688
    Abstract: 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: Grant
    Filed: July 27, 1978
    Date of Patent: April 6, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Ernst Habicht, Pier G. Ferrini, Alfred Sallmann
  • Patent number: 4323560
    Abstract: 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: Grant
    Filed: October 6, 1980
    Date of Patent: April 6, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Gerhard Baschang, Lajos Tarcsay, Albert Hartmann, Jaroslav Stanek
  • Patent number: 4322419
    Abstract: 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: Grant
    Filed: January 8, 1979
    Date of Patent: March 30, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Beat Muller, Wilhelm Kump, Oskar Wacker