Patents Represented by Attorney, Agent or Law Firm Irving N. Feit
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Patent number: 4517184Abstract: The invention relates to novel benzodioxole derivatives of the formula I ##STR1## in which R.sub.1 represents an unsubstituted or substituted, aromatic or heteroaromatic radical, alk represents an alkylene or alkylidene radical having a maximum of 5 carbon atoms, n represents O or 1, R.sub.2 and R.sub.3 each represents, independently of the other, hydrogen, lower alkyl, lower alkoxy or halogen, and A represents the radical O-R.sub.4, wherein R.sub.4 represents hydrogen or an unsubstituted or substituted, aliphatic or araliphatic hydrocarbon radical, or A represents the radical ##STR2## in which either R.sub.5 and R.sub.6 each represents, independently of the other, hydrogen or lower alkyl, or R.sub.5 and R.sub.6 are bonded to one another and, together with the adjacent nitrogen atom, represent unsubstituted or lower alkyl-substituted tetra- or hexa-methyleneimino or 4-morpholinyl, to salts of compounds of the formula I in which A represents OR.sub.4 wherein R.sub.Type: GrantFiled: August 8, 1983Date of Patent: May 14, 1985Assignee: Ciba-Geigy CorporationInventors: Ernst Habicht, Paul Zbinden
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Patent number: 4515717Abstract: 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: September 24, 1982Date of Patent: May 7, 1985Assignee: Ciba Geigy CorporationInventors: Jacques Gosteli, Ivan Ernest, Robert B. Woodward
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Patent number: 4511567Abstract: The invention relates to a process for the manufacture of novel benzazole derivatives of the formula I ##STR1## in which R.sub.1 represents an optionally 4-substituted piperazino group or a group of the formula R.sub.2 --alk--X.sub.2 --,R.sub.2 represents optionally esterified carboxy or represents hydroxymethyl,alk represents lower alkylene or lower alkylidene,X.sub.1 and X.sub.2, independently of one another, each represents oxygen or sulphur,Ph represents 1,2-phenylene optionally substituted as well as by the group R.sub.1 --C(.dbd.X.sub.1)--NH--,X.sub.3 represents oxygen, sulphur or optionally substituted imino, andR.sub.3 represents optionally fluorine-substituted lower alkyl or cycloalkyl,and their salts.The compounds of the formula I, which have proved to be excellent micro- and macrofilaricides and schistosomacides, are manufactured according to methods known per se.Type: GrantFiled: September 16, 1982Date of Patent: April 16, 1985Assignee: Ciba-Geigy CorporationInventors: Jean J. Gallay, Ernst Schweizer
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Patent number: 4508723Abstract: 6-Amino-penam compounds, having an antimicrobial action, of the formula ##STR1## in which R.sub.1 is an azaoligocycloalkyl radical which is bonded via the ring nitrogen atom and contains at least one endo-bridge atom and a total of 7 to 12 ring atoms and can contain a double bond and/or, if desired, as a further ring hetero-atom, an oxygen atom, or a nitrogen atom which can link the radical X.sub.1, where X.sub.1 is hydrogen or lower alkyl, and/or, if desired, free, esterified or etherified hydroxyl which is bonded to a ring carbon atom, and in which R.sub.Type: GrantFiled: June 4, 1982Date of Patent: April 2, 1985Assignee: Ciba Geigy CorporationInventors: Karl Schaffner, Riccardo Scartazzini
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Patent number: 4505913Abstract: Substituted anthranilamides of the formula ##STR1## in which R.sub.1 is hydrogen or an aliphatic, cycloaliphatic or cycloaliphatic-aliphatic hydrocarbon radical, R.sub.2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, R.sub.3 is hydrogen or an aliphatic or substituted or unsubstituted araliphatic or heteroaryl-aliphatic hydrocarbon radical and alk and alk' are identical or different lower alkylene radicals which separate the nitrogen atoms by 2 or 3 carbon atoms, and salts thereof, possess analgesic, anti-inflammatory and anti-allergic properties and may be used as active ingredients of analgesic, anti-inflammatory and anti-allergic pharmaceuticals. They are prepared, for example, by reacting an acid of the formula ##STR2## or a reactive functional derivative thereof, with an amine of the formula ##STR3## or a reactive derivative or salt thereof.Type: GrantFiled: September 30, 1982Date of Patent: March 19, 1985Assignee: Ciba-Geigy CorporationInventors: Pier G. Ferrini, Alberto Rossi, Georges Haas
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Patent number: 4500457Abstract: 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: March 1, 1982Date of Patent: February 19, 1985Assignee: Ciba-Geigy CorporationInventors: Jacques Gosteli, Ivan Ernest, Robert B. Woodward
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Patent number: 4500542Abstract: The invention relates to novel dioxaheterocyclic compounds of the formula I ##STR1## in which R.sub.1 represents an unsubstituted or substituted aromatic or heteroaromatic radical or an unsubstituted or lower alkylated, mono- or bi-cyclic cycloaliphatic hydrocarbon radical or an .alpha.-branched aliphatic hydrocarbon radical, each of R.sub.2 and R.sub.3, independently of the other, represents hydrogen or lower alkyl, and each of R.sub.4 and R.sub.5, independently of the other, represents hydrogen, lower alkyl or halogen, and A represents the radical --O--R.sub.6, wherein R.sub.6 represents hydrogen or an unsubstituted or substituted aliphatic or araliphatic hydrocarbon radical or A represents the radical ##STR2## in which each of R.sub.7 and R.sub.8, independently of the other, represents hydrogen or lower alkyl, or R.sub.7 and R.sub.Type: GrantFiled: November 8, 1983Date of Patent: February 19, 1985Assignee: Ciba-Geigy CorporationInventors: Ernst Habicht, Paul Zbinden
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Patent number: 4497808Abstract: The present invention relates to novel N-oxide compounds that have cardiovascular properties, especially antihypertensive activity, and that correspond to the formula ##STR1## in which Py represents an unsubstituted or substituted N-oxidopyridyl radical, R.sub.1 represents hydrogen or unsubstituted or substituted lower alkyl, one of the radicals R.sub.2 and R.sub.3 represents lower alkyl and the other represents hydrogen; lower alkyl; lower alkyl containing free, etherified or esterified hydroxy, oxo, functionally modified carboxy or free or substituted amino or imino; functionally modified carboxy; or free or substituted amino, it being possible for an amino group R.sub.2 or R.sub.3 to be bonded to a lower alkyl radical R.sub.1 or, if R.sub.2 or R.sub.3 represents, for example, hydroxy-lower alkyl, for this hydroxy-lower alkyl, together with the adjacent acyl radical Ac.sub.1 or Ac.sub.Type: GrantFiled: December 27, 1982Date of Patent: February 5, 1985Assignee: Ciba-Geigy CorporationInventors: Markus Zimmermann, Hans Kuhnis
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Patent number: 4492691Abstract: Azatetracyclic carbonitriles of the formula ##STR1## in which R represents hydrogen, lower alkyl, cycloalkyl-lower alkyl having up to 10 carbon atoms, lower alkenyl, lower alkynyl or free, etherified or esterified hydroxy-lower alkyl, and acid addition salts thereof, processes for their manufacture, pharmaceutical compositions that contain such compounds and their use. They are distinguished especially by their central nervous system-depressant, agitation-inhibitory (amphetamine-antagonistic) action. They can therefore be used as tranquillizing, anti-psychotic, agitation-inhibitory compounds for the treatment of agitated states having various causes.Type: GrantFiled: July 1, 1982Date of Patent: January 8, 1985Assignee: Ciba-Geigy CorporationInventors: Hans Blattner, Angelo Storni
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Patent number: 4476132Abstract: Quinolinone derivatives of the formula (I) ##STR1## in which X represents oxy or a direct bond, R.sub.1 represents an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclic-aliphatic radical or hydrogen, Ph represents an optionally additionally substituted 1,2-phenylene radical containing the group R.sub.1 --X--C(O)--, and one of the radicals R.sub.2 and R.sub.3 represents an optionally esterified or amidated carboxy group R.sub.4 and the other represents hydrogen or an aliphatic radical or, in the case of a radical R.sub.3, hydroxy, and in which either R.sub.A and R.sub.B together represent oxo, R.sub.C and R.sub.D together represent an additional bond, or, when R.sub.2 represents a radical R.sub.4, R.sub.C is hydrogen and R.sub.3 and R.sub.D together represent oxo, and R.sub.E represents a radical R.sub.5 which represents hydrogen or an aliphatic, cycloaliphatic, araliphatic heterocyclic-aliphatic radical, or R.sub.A represents an optionally etherified hydroxy group and R.sub.Type: GrantFiled: March 19, 1982Date of Patent: October 9, 1984Assignee: Ciba-Geigy CorporationInventors: Richard Goschke, Pier G. Ferrini, Alfred Sallmann
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Patent number: 4468229Abstract: Contact lenses comprising polymeric lens materials in which reactive dyestuffs have been covalently bonded to monomer units of the polymer backbone, said reactive dyestuffs being reactive dyes capable of forming ether linkages with cellulose and reactive with hydroxyl, amino, amido or mercapto groups present in a hydrogel polymer to form the covalent bond therewith. The invention is of particular interest in the area of so-called hydrophilic or "soft" contact lenses, commonly referred to as hydrogel lenses.Type: GrantFiled: June 1, 1982Date of Patent: August 28, 1984Assignee: Ciba-Geigy CorporationInventor: Kai C. Su
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Patent number: 4465666Abstract: The invention relates to new pharmaceutical preparations for the topical treatment of infections caused by herpes viruses, especially those which have been caused by herpes virus hominis, for example of herpes genitalis and herpes dermatitis. The preparations contain as antiviral agent a synergistic combination of an acid sulphated polysaccharide or acid sulphated polymer, in particular heparin, and zinc ions, and may further contain polyoxyethylene sorbitan monolaurate and/or -monooleate. They are usual types of preparations for topical administration such as tinctures, solutions, creams, ointments and, especially, gels.Type: GrantFiled: October 30, 1981Date of Patent: August 14, 1984Assignee: Ciba-Geigy CorporationInventors: Bohumir Lukas, Walter Wiesendanger, Karl H. Schmidt-Ruppin
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Patent number: 4461770Abstract: Novel substituted 2-mercaptoimidazoles of the formula ##STR1## in which at least one of the radicals R.sub.1 and R.sub.2 is a substituted or unsubstituted heteroaryl group and the other is a substituted or unsubstituted aryl group, R.sub.3 is hydrogen or lower alkyl, n is 0, 1 or 2 and R.sub.4 is a substituted or unsubstituted aliphatic hydrocarbon radical and their pharmaceutically usable salts exhibit anti-inflammatory, anti-nociceptive and/or antithrombotic activity.Type: GrantFiled: November 16, 1981Date of Patent: July 24, 1984Assignee: Ciba-Geigy CorporationInventors: Pier G. Ferrini, Richard Goschke
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Patent number: 4460580Abstract: The invention relates to novel N-alkylated aminoalcohols of the formula ##STR1## in which Ar is a radical of aromatic character which is unsubstituted or substituted by hydroxyl, n has the values nought or 1 and Alk is an alkylene radical having 2 to 5 carbon atoms and the nitrogen atom and the oxygen atom or, if n is nought, the salicylamide radical are separated from one another by at least two carbon atoms in the straight-chain, and their salts. The main action of the novel compounds consists in a stimulation of cardiac .beta.-receptors; the compounds also effect a blockage of adrenergic .alpha.-receptors and a lowering in the blood pressure. They can therefore be used as .beta.-stimulators, especially as agents having a positively inotropic action for the treatment of cardiac insufficiency.Type: GrantFiled: June 24, 1982Date of Patent: July 17, 1984Assignee: Ciba-Geigy CorporationInventors: Franz Ostermayer, Markus Zimmermann
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Patent number: 4458069Abstract: The invention concerns the decarbonylation of the formyl group in 7-amino-3-formyl-ceph-2-em-4-carboxylic acid compounds and 7-amino-3-formyl-ceph-3-em-4-carboxylic acid compounds by treatment with a platinum metal complex capable of taking up carbon monoxide. Also included are the 7-amino-ceph-2-em-4-carboxylic acid compounds and the 1-oxides of 7-amino-ceph-3-em-4-carboxylic acid compounds; these compounds are used as intermediates.Type: GrantFiled: January 14, 1981Date of Patent: July 3, 1984Assignee: Ciba-Geigy CorporationInventors: Heinrich Peter, Hans Bickel
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Patent number: 4452901Abstract: Solid supports for proteins consisting of nitrocellulose sheets containing a replica of an electropherogram of proteins as obtained by electrophoretic separation in a gel. Faithful replica of such electropherograms on the nitrocellulose support can be obtained by contacting the gel with a nitrocellulose sheet and applying an electric field perpendicular to the plane of the gel causing an electrophoretic migration of the proteins toward the nitrocellulose sheet where the proteins are adsorbed. Various analytical problems and especially immuno-assays, for enzyme immuno-assays or such involving radioactively labeled indicators, can be made with the new solid supports.Type: GrantFiled: April 20, 1981Date of Patent: June 5, 1984Assignee: Ciba-Geigy CorporationInventors: Julian Gordon, Theophil Staehelin, Harry Towbin
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Patent number: 4452738Abstract: The invention relates to a process for the manufacture of the known 5-carbamoyl-10-oxo-10,11-dihydro-5H-dibenz[b,f]azepine of the formula III which is characterized in that, for example, 5-cyano-5H-dibenz[b,f]azepine of the formula I is nitrated to form 5-cyano-10-nitro-5H-dibenz[b,f]azepine of the formula II, this is subjected to hydrolysis, then reduction, then the reduction product contained in the reaction mixture is subjected to hydrolysis and the end product of the formula III is isolated in pure form.The process is illustrated by the following reaction scheme: ##STR1## The invention relates also to new intermediates produced in these reactions.Type: GrantFiled: May 26, 1983Date of Patent: June 5, 1984Assignee: Ciba-Geigy CorporationInventor: Ernst Aufderhaar
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Patent number: 4451471Abstract: 2,4,5-Trisubstituted thiazoles of the formula ##STR1## in which each of R.sub.1 and R.sub.2, independently of the other, represents an aryl or optionally N-oxidized heteroaryl radical each of which is unsubstituted or substituted by aliphatic hydrocarbon radicals, free, etherified or esterified hydroxy, etherified optionally S-oxidized mercapto, aliphatically substituted amino and/or trifluoromethyl,X represents thio,n represents 0, 1, or 2, andR.sub.3 represents an aliphatic hydrocarbon radical that is unsubstituted or substituted by etherified or esterified hydroxy, etherified optionally S-oxidized mercapto and/or, in a position higher than the .alpha.-position, by oxo and/or hydroxy and optionally contains, in addition to terminally bonded hydroxy, sulpho that is present in salt form, or represents an araliphatic hydrocarbon radical that is unsubstituted or substituted in the aryl moiety as indicated for R.sub.1 and R.sub.Type: GrantFiled: March 8, 1982Date of Patent: May 29, 1984Assignee: Ciba-Geigy CorporationInventors: Pier G. Ferrini, Richard Goschke
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Patent number: 4446128Abstract: The invention relates to novel antigen derivatives comprising an antigen and at least one muramyl-peptide covalently bonded thereto, if appropriate via a spacer, to pharmaceutical preparations which contain such compounds and to their use as a vaccine.The novel antigen derivatives produce a pronounced increase in the immuno-response to the antigen, and in particular also a cell-medicated immunity under clinically acceptable conditions of administration.Type: GrantFiled: May 18, 1982Date of Patent: May 1, 1984Assignee: Ciba-Geigy CorporationInventors: Gerhard Baschang, Felix M. Dietrich, Roland Gisler, Albert Hartmann, Jaroslav Stanek, Lajos Tarcsay
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Patent number: 4444768Abstract: Novel amidines, especially N,N'-bridged carboxylic acid amidines of the general formula ##STR1## in which R.sub.1 represents an aromatic radical, R.sub.2 represents optionally esterified or amidated 1-carboxy-lower alkyl, Ph represents optionally substituted 1,2-phenylene and alk represents an aliphatic hydrocarbon radical separating the imino group from the methine group by from 1 to 3 carbon atoms, and their salts, have, inter alia, anti-inflammatory activity and can be used as active medicament substances in pharmaceutical preparations. They are produced according to methods known per se.Type: GrantFiled: July 1, 1982Date of Patent: April 24, 1984Assignee: Ciba-Geigy CorporationInventors: Ulrich Renner, Knut A. Jaeggi