Patents Represented by Attorney John J. Maitner
  • Patent number: 4147864
    Abstract: 7.beta.-amino-3-cephem-3-ol-4-carboxylic acid compounds of the formula ##STR1## wherein R.sub.1.sup.a represents hydrogen or an amino protective group R.sub.1.sup.A and R.sub.1.sup.B represents hydrogen or an acyl group Ac, or R.sub.1.sup.a and R.sub.1.sup.b together represent a bivalent amino protective group, R.sub.2 represents 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, lower alkyl or a hydroxyl protective group, and 1-oxides or 3-cephem compounds of the formula IA, and the corresponding 2-cephem compounds are prepared in that a compound of the formula ##STR2## wherein R.sub.1.sup.a, R.sub.1.sup.b and R.sub.2.sup.A have the meanings mentioned under formula IA, R.sub.3.sup.o represents lower alkyl or a hydroxyl protective group and Y represents a group which is removed, is treated with a base; also comprised are intermediate products.
    Type: Grant
    Filed: December 2, 1976
    Date of Patent: April 3, 1979
    Assignee: Ciba-Geigy Corporation
    Inventors: Robert B. Woodward, Hans Bickel
  • Patent number: 4144344
    Abstract: A process known per se for the manufacture of oxygenated N-aryl-diazacyclic compounds of the formula ##STR1## wherein EACH OF R.sub.1 and R.sub.2 represents a substituted or unsubstituted aryl group and alk represents a lower alkylene group which separates both nitrogen atoms from each other by 2 or 3 carbon atoms, or salts thereof.The novel compounds can be used as antihypertensives, antitachycardiac agents and .alpha.-receptor blockers.
    Type: Grant
    Filed: January 21, 1977
    Date of Patent: March 13, 1979
    Assignee: Ciba-Geigy Corporation
    Inventors: Kurt Eichenberger, Hans Kuhnis, Franz Ostermayer, Herbert Schroter
  • Patent number: 4141982
    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: August 18, 1977
    Date of Patent: February 27, 1979
    Assignee: Ciba-Geigy Corporation
    Inventors: Ernst Habicht, Pier G. Ferrini, Alfred Sallmann
  • Patent number: 4140789
    Abstract: A compound of the formula ##STR1## in which R.sub.1 denotes optionally substituted lower akyl 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.1 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: Grant
    Filed: December 16, 1976
    Date of Patent: February 20, 1979
    Assignee: Ciba-Geigy Corporation
    Inventors: Knut A. Jaeggi, Franz Ostermayer, Herbert Schroter
  • Patent number: 4139633
    Abstract: The present invention relates to new pharmaceutical preparations comprising a .beta.-receptor blocking agent and a diuretic, processes for their preparation and the use of said preparations for the treatment of hypertonia.
    Type: Grant
    Filed: February 27, 1976
    Date of Patent: February 13, 1979
    Assignee: Ciba-Geigy Corporation
    Inventor: Hellmut Brunner
  • Patent number: 4139623
    Abstract: Compounds of the formula ##STR1## WHEREIN Ar.sub.1 and Ar.sub.2 denote an optionally substituted aromatic hydrocarbon radical or a monocyclic, monoazacyclic or diazacyclic radical of aromatic character and Alk represents lower alkylene, or salts thereof, exhibit .beta.-receptor-blocking, blood pressure-lowering and vasodilatory effects and are useful for example in the treatment of arrythmias and angina pectoris, and as blood pressure-lowering agents.
    Type: Grant
    Filed: March 14, 1977
    Date of Patent: February 13, 1979
    Assignee: C-G Corp.
    Inventors: Knut A. Jaeggi, Franz Ostermayer, Herbert Schroter
  • Patent number: 4138451
    Abstract: Thioformamidophosphono-acetates are prepared by reacting an isocyano compound of the formula C.dbd.N--CH.sub.2 --X.sub.1 in the presence of a base with a compound of the formula R.sub.o --X.sub.2, in which compounds one of the groups X.sub.1 and X.sub.2 represents a protected carboxyl group of the formula --C(.dbd.O)--OR.sub.1 and the other a disubstituted phosphono group of the formula --P(.fwdarw.O) (OR).sub.2, and wherein R.sub.o represents a reactive etherified or esterified hydroxyl group, and adding hydrogen sulphide on to the isocyano group of the phosphono-isocyano-acetate formed as an intermediate.
    Type: Grant
    Filed: April 28, 1977
    Date of Patent: February 6, 1979
    Assignee: Ciba-Geigy Corporation
    Inventor: Jacques Gosteli
  • Patent number: 4130652
    Abstract: The present invention provides new imino compounds having the formula I ##STR1## wherein R.sub.1 represents an aliphatic or cycloaliphatic hydrocarbon radical, unsubstituted or substituted phenyl, or phenyl-lower alkyl or diphenyl-lower alkyl, which radicals are unsubstituted or substituted in the phenyl ring(s),R.sub.2 represents unsubstituted or substituted phenyl, unsubstituted or substituted monocyclic heteroaryl or lower alkyl,R.sub.3 represents hydrogen, lower alkyl, a carbonyl group linked with R.sub.2 to form a five-membered ring, or the group R.sub.6 --CO wherein R.sub.6 represents lower alkyl or unsubstituted or substituted phenyl,R.sub.4 represents, if present, hydrogen or lower alkyl which is independent or is linked with R.sub.1 to form a five- to seven-membered ring which can contain as ring members two aromatic ring carbon atoms of an unsubstituted or substituted phenyl or phenyl-lower-alkyl radical R.sub.
    Type: Grant
    Filed: February 23, 1977
    Date of Patent: December 19, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Atso Ilvespaa, Walter Fuhrer
  • Patent number: 4120978
    Abstract: Compounds selected from the group consisting of amines of the formula I ##STR1## in which R.sub.1 and R.sub.2 stand for a member selected from lower alkyl, lower alkenyl, cycloalkyl having 4 to 7 ring members, phenyl-lower alkyl, phenyl-lower alkyl substituted in the phenyl residue by a member selected from lower alkyl, lower alkoxy, halogen and trifluoromethyl, lower alkylene, oxa-lower alkylene, aza-lower alkylene and thia-lower alkylene, and one of R.sub.1 and R.sub.2 stands for hydrogen and the other has the above meanings, Ph stands for a member selected from meta- and para-phenylene and meta- and para-phenylene substituted by a member selected from lower alkyl, lower alkenyl, lower alkinyl, mercapto-lower alkyl, hydroxy-lower alkyl, phenyl, cyano, hydrogen, halogen, lower alkoxy, lower alkenyloxy, lower alkinyloxy, mono-, di and trihalogeno-lower alkyl, cycloalkyl having 5 to 7 ring members and phenoxy, and R.sub.
    Type: Grant
    Filed: April 4, 1977
    Date of Patent: October 17, 1978
    Assignee: Ciba-Geigy Corporation
    Inventor: Max Wilhelm
  • Patent number: 4117156
    Abstract: The present invention relates to anthelmintic preparations containing 4-(4-nitroanilino)-phenylisothiocyanate having a median of particle size of at most 10 .mu.m, particularly at most 5 .mu.m, and to the treatment of infections by parasitic helminthes, especially to the treatment of warm-blooded animals affected by shistosomiasis, hookworm infestation of filariasis, by administration of the preparations named above. Specific embodiments are suspensions of the active substance in triglycerides of medium saturated fatty acids, and mixtures of the active substance with a starch, particularly with maize starch.
    Type: Grant
    Filed: February 15, 1977
    Date of Patent: September 26, 1978
    Assignee: Ciba-Geigy AG
    Inventors: Werner Loewe, Heini Paul Striebel
  • Patent number: 4115575
    Abstract: Heterocyclic compounds of the formula ##STR1## wherein Het denotes optionally substituted pyridazinyl, pyrimidinyl, pyrazinyl or substituted pyridyl, R.sub.1 is hydrogen or methyl and R.sub.2 is lower alkyl, optionally substituted phenyl-lower alkyl, carboxy-lower alkyl or functionally modified carboxy-lower alkyl, their condensation products with aldehydes, ketones or carbonic acid and their N-oxides, which are valuable (cardioselective) .beta.-rezeptor blocking agents, and/or (cardioselective) .beta.-rezeptor-stimulants.
    Type: Grant
    Filed: January 7, 1977
    Date of Patent: September 19, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Jorg Frei, Knut A. Jaeggi, Franz Ostermayer, Herbert Schroter
  • Patent number: 4115566
    Abstract: 6-Acylamino-penam-3-carboxylic acids and 7-acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula ##STR1## 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: December 19, 1975
    Date of Patent: September 19, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Karoly Kocsis, Bruno Fechtig, Hans Bickel
  • Patent number: 4112075
    Abstract: The invention relates to furanose-O-pyridylcarboxylic acid esters, such as the ethyl-2-O-methyl-3,5,6-tri-O-nicotinoyl-D-glucofuranoside, which have anti-inflammatory activity and are fibrinolysis activators. They can be used for the treatment of rheumatic and neuralgic complaints, and especially for the topical percutaneous treatment of localized inflammatory processes.
    Type: Grant
    Filed: September 9, 1976
    Date of Patent: September 5, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Gerhard Baschang, Alex Sele, Jaroslav Stanek, Alberto Rossi
  • Patent number: 4111950
    Abstract: Compounds of the class of 6-phenyl-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-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 inhibit somatic reflexes. Specific embodiments are N,N-dimethyl-6-phenyl-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-c arboxamide, 6-(o-fluorophenyl)-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodiazepine-2-carb oxamide, N,N-dimethyl-6-(o-fluorophenyl)-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodia zepine-2-carboxamide and N,N-dimethyl-6-(o-chlorophenyl)-8-chloro-4H-s-triazolo[1,5-a][1,4]benzodia zepine-2-carboxamide.
    Type: Grant
    Filed: February 4, 1977
    Date of Patent: September 5, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Andre Gagneux, Roland Heckendorn, Rene Meier
  • Patent number: 4112099
    Abstract: New pyridine compounds of the general formula I ##STR1## wherein R denotes an optionally substituted cycloaliphatic hydrocarbon radical, Ph denotes an ortho-phenylene radical or especially a para-phenylene radical, A denotes a lower alkylene radical or a direct bond, X denotes an optionally functionally modified oxo group and Py denotes a pyridine radical, are useful as fibrinolytics, thrombolytics, antiphlogistics and as mild analgesics.
    Type: Grant
    Filed: April 28, 1976
    Date of Patent: September 5, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Georges Haas, Alberto Rossi
  • Patent number: 4112110
    Abstract: 5-Oxygenated azatetracyclic compounds of the formula ##STR1## wherein X represents oxygen or sulphur, R represents a hydroxy group optionally esterified by an alkanecarboxylic acid, and R.sub.1 stands for a lower alkyl, lower alkenyl or allyl, or salts thereof, such compounds having a central-depressant and agitation-inhibiting action connected with cataleptic effects to a very low extent only these properties rendering the new compounds suitable as tranquillizing, antipsychotic and agitation-inhibiting substances.
    Type: Grant
    Filed: November 3, 1976
    Date of Patent: September 5, 1978
    Assignee: Ciba-Geigy Corporation
    Inventor: Hans Blattner
  • Patent number: 4110533
    Abstract: 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: Grant
    Filed: February 10, 1976
    Date of Patent: August 29, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Robert B. Woodward, Hans Bickel
  • Patent number: 4089960
    Abstract: The present invention provides new basically substituted pyridinecarboxamides having the formula I ##STR1## wherein R.sub.1 represents lower alkyl and --OR.sub.1 is in the adjacent position to the carboxamide group,R.sub.2 represents lower alkyl or an ethylene radical which is attached to one of the trivalent radicals designated as A and the nitrogen atom located between it to form a 6-membered ring,A represents a divalent saturated hydrocarbon radical which encompasses at most a single ring with 5 or 6 ring members and contains not more than 7 carbon atoms and whose two linkage positions are separated by (3-m) to 4 carbon atoms, or, if R.sub.2 is an ethylene radical, represents the 1-propanyl-3-ylidene radical, if m s 1, or the 1,2,4-butane-triyl radical, if m is 0,And one of the factors m and n is 0 and the other is 1, and, if desired, the ring B is further substituted, and the acid addition salts of the compounds of the formula I.
    Type: Grant
    Filed: September 14, 1976
    Date of Patent: May 16, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Jacques Gosteli, Angelo Storni, Armin Zust
  • Patent number: 4089955
    Abstract: 7.beta.-[D-2-Amino-2-(1,4-cyclohexadienyl)-acetylamino]-3-Hal-3-cephem-4-ca rboxylic acids, wherein Hal denotes halogen with an atomic number of up to 35, and pharmaceutically acceptable salts thereof are prepared, which compounds have antibiotic activity.
    Type: Grant
    Filed: July 14, 1976
    Date of Patent: May 16, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Schneider, Hans Bickel
  • Patent number: 4076812
    Abstract: The present invention relates to new derivatives of 5H-dibenz[b,f]azepine having the formula I ##STR1## wherein Hal represents halogen with an atomic number up to 35 and R represents hydrogen or halogen with an atomic number up to 35. These new compounds possess useful pharmacological properties, in particular a prolonged anticonvulsive action, and can be used for the treatment of states of convulsion, especially of epilepsy. A specific embodiment of the invention is 10-chloro-5H-dibenz[b,f]azepine-5-carboxamide.
    Type: Grant
    Filed: September 22, 1975
    Date of Patent: February 28, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Allgeier, Erich Schmid