Abstract: A process for the preparation of substituted benzenes or benzenesulfonic acid and its derivatives comprising diazotisation of an aminobenzene or ortho-amino-benzenesulfonic acid derivative followed by homogeneous palladium-catalyzed coupling with an olefine and heterogeneous palladium-catalyzed hydrogenation of the olefinic substituent, wherein the homogeneous catalyst is reduced and precipitated as metal after the coupling in the reaction mixture and used as a heterogeneous palladium catalyst for the hydrogenation step. The process is particular suitable for the preparation N-benzenesulfon-N'-triazinyl-urea herbicides.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
June 10, 1997
Assignee:
Ciba-Geigy Corporation
Inventors:
Peter Baumeister, Gottfried Seifert, Heinz Steiner
Abstract: Compounds of formula I ##STR1## wherein Z, R, R.sub.1, R.sub.2 and X are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
June 10, 1997
Assignee:
Ciba Geigy Corporation
Inventors:
Marc Lang, Edmond Differding, Jaroslav Stanek
Abstract: The invention relates to novel substituted oxazolidines of formula (I) wherein R.sub.1 and R.sub.2 are simultaneously hydrogen or both together are the identical lower alkyl radical, and to the salts thereof in racemic and chiral form, to a process for the preparation of said compounds, to pharmaceutical compositions containing them, and to the use thereof as medicaments. The compounds have a stimulating effect on beta-adrenergic receptors and can be used, inter alia, for the treatment of diseases associated with reversible obstruction of the respiratory tract, typically asthma and chronic bronchitis, and also for inflammation of different origin.
Type:
Grant
Filed:
June 10, 1996
Date of Patent:
June 3, 1997
Assignee:
Ciba-Geigy Corporation
Inventors:
Alfred Sallmann, Hans-Peter Gschwind, Eric Francotte
Abstract: The present invention relates to novel substituted thiosemicarbazonic acid esters of formula I ##STR1## wherein R.sub.1 is lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, or aryl-lower alkyl, R.sub.2 is hydrogen, lower alkyl, aryl, aryl-lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, unsaturated or saturated heterocyclyl-lower alkyl, lower alkoxycarbonyl-lower alkyl or the group --C(.dbd.O)-R.sub.3, wherein R.sub.3 is lower alkyl, aryl, aryl-lower alkyl, aryl-lower alkenyl, heteroaryl (hetaryl), aryloxy, aryl-lower alkoxy or lower alk-2-en-1-yloxy, and R.sub.4 is lower alkyl, lower alkoxy, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, aryl-lower alkyl, aryl-lower alkenyl, or also lower alkoxycarbonyl-lower alkyl, and the salts thereof, to a process for the preparation of said compounds, to pharmaceutical compositions containing them, and to the use thereof as medicaments.
Abstract: 3-Heteroaliphatyl- and 3-hetero(aryl)aliphatyl-2(1H)quinolone derivatives of formula I ##STR1## wherein the radicals R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently of the others hydrogen, an aliphatic hydrocarbon radical, free or etherified hydroxy, mercapto or etherified and/or oxidised mercapto, unsubstituted or aliphaticaliy substituted amino, nitro, free or esterified or amidated carboxy, cyano, free or amidated sulfamoyl, halogen or trifluoromethyl, X is oxy or optionally oxidised thio, A is a divalent aliphatic radical and R.sub.
Abstract: The present invention relates to novel substituted thiosemicarbazonethiones containing 6-ring members of formula I ##STR1## wherein R.sub.1 is lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, or aryl-lower alkyl, R.sub.2 is hydrogen, lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, aryl, aryl-lower alkyl, unsaturated or saturated heterocyclyl-lower alkyl, lower alkoxycarbonyl-lower alkyl or a group --C(.dbd.O)-R.sub.3 or --C(.dbd.S)-R.sub.3, wherein R.sub.3 is lower alkyl, aryl, aryl-lower alkyl, aryl-lower alkenyl, heteroaryl (hetaryl), aryloxy, aryl-lower alkoxy or lower alk-2-en-1-yloxy, and the salts thereof, to a process for the preparation of said compounds, to pharmaceutical compositions containing them, and to the use thereof as medicaments.
Abstract: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.
Type:
Grant
Filed:
July 25, 1996
Date of Patent:
May 6, 1997
Assignee:
Ciba Geigy Corporation
Inventors:
Richard G oschke, J urgen K. Maibaum, Walter Schilling, Stefan Stutz, Pascal Rigollier, Yasuchika Yamaguchi, Nissim C. Cohen, Peter Herold
Abstract: The invention relates to compounds of the following general formula I ##STR1## especially the compound of formula Ia referred to as thiangazole ##STR2## their pharmaceutically acceptable acid addition salts, processes for their preparation and therapeutic compositions and compositions that can be used in crop-protection.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
April 22, 1997
Assignees:
Ciba-Geigy Corporation, Gesellschaft fur Biotechnologische Forschung mbH
Inventors:
Gerhard H ofle, Norbert Bedorf, Edgar Forche, Klaus Gerth, Herbert Irschik, Rolf Jansen, Brigitte Kunze, Hans Reichenbach, Florenz Sasse, Heinrich Steinmetz, Wolfram Trowitzsch-Kienast, Johannes P. Pachlatko
Abstract: A selective herbicidal composition for controlling grasses and weeds in crops of cultivated plants, comprising, in addition to inert carriers and adjuvants, as active component a mixture ofa) a herbicidally effective mount of a N-phenylsulfonyl-N'-triazinylurea of formula I ##STR1## wherein the substituents are as defined in claim 1, and b) to antagonise the herbicide, an antidotally effective mount of a quinoline derivative of formula IIa ##STR2## wherein R.sub.10 is hydrogen, C.sub.1 -C.sub.8 alkyl or C.sub.1 -C.sub.8 alkyl which is substituted by C.sub.1 -C.sub.6 alkoxy or C.sub.3 -C.sub.6 alkenyloxy; andX.sub.2 is hydrogen or chloro; or of a 1-phenylazole-3-carboxylic acid derivative of formula IIb ##STR3## wherein E is nitrogen or methine;R.sub.11 is --CCl.sub.3, phenyl or halogen-substituted phenyl;R.sub.12 and R.sub.13 are each independently of the other hydrogen or halogen; and R.sub.14 is C.sub.1 -C.sub.4 alkyl.
Type:
Grant
Filed:
December 21, 1995
Date of Patent:
April 8, 1997
Assignee:
Ciba-Geigy Corporation
Inventors:
Jutta Glock, Manfred Hudetz, Elmar Kerber
Abstract: N-phenyl-2-pyrimidineamine derivatives of formula (I) wherein the substituents are as defined in claim 1 are described. Those compounds can be used for example, in the treatment of tumour diseases.
Abstract: Compounds of the formula XI, wherein R, R.sub.4, R.sub.8 and R.sub.38 are as defined in claim 1, are useful as intermediates in the preparation of compounds of formula I. Mixtures of a herbicidally effective amount of a pyridylsulfonylurea of formula I, ##STR1## wherein R, R.sub.1, R.sub.2 and A are as defined in the specification and of a herbicide-antagonistically effective amount of a sulfamoylphenylurea of formula II, ##STR2## wherein R.sub.7 to R.sub.11 and A.sub.2 are as defined in the specification are very suitable for controlling weeds in crops of useful plants, especially maize and sugar cane.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
March 18, 1997
Assignee:
Ciba Geigy Corporation
Inventors:
Werner F ory, Elmar Kerber, Manfred Hudetz
Abstract: The invention relates to compounds of the following general formula I ##STR1## especially the compound of formula Ia referred to as thiangazole ##STR2## their pharmaceutically acceptable acid addition salts, processes for their preparation and therapeutic compositions and compositions that can be used in crop-protection.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
March 11, 1997
Assignees:
Ciba-Geigy Corporation, Gesellschaft fur Biotechnologische Forschung mbH
Inventors:
Gerhard Hofle, Norbert Bedorf, Edgar Forche, Klaus Gerth, Herbert Irschik, Rolf Jansen, Brigitte Kunze, Hans Reichenbach, Florenz Sasse, Heinrich Steinmetz, Wolfram Trowitzsch-Kienast, Johannes P. Pachlatko
Abstract: The invention relates to substituted 3-amino-1-arylalkyl-benzazepin-2-ones of the general formula ##STR1## wherein Ar is aryl;X is --O-- or --S(O).sub.n -- and n is 0, 1 or 2;X.sub.1 is C.sub.1 -C.sub.2 alkylene or a direct bond;R.sub.1 is hydrogen, lower alkyl, aryl-lower alkyl or acyl;R.sub.2 is lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkoxy-lower alkyl, aryl-lower alkyl or C.sub.3 -C.sub.7 cycloalkyl-lower alkyl;R.sub.3 is carboxy; lower alkoxycarbonyl; lower alkoxy-lower alkoxycarbonyl; aryl-lower alkoxycarbonyl; aryloxycarbonyl; carbamoyl; carbamoyl that (i) is monosubstituted by hydroxy, lower alkanesulfonyl, halo-lower alkanesulfonyl or by arylsulfonyl, (ii) is monosubstituted or disubstituted, the substituents being independent of one another, by lower alkyl, lower alkenyl, lower alkynyl or by phenyl-lower alkyl or (iii) is disubstituted by lower alkylene or by lower alkylene-Z.sub.1 -lower alkylene, Z.sub.1 being O, S or NH; 5-tetrazolyl; PO.sub.2 H.sub.2 ; PO.sub.3 H.
Abstract: The invention relates to novel aromatic acids, especially to compounds of formula ##STR1## wherein R.sub.1 is lower alkyl, R.sub.2 is lower alkyl, R.sub.3 is hydrogen, carboxy or sulfo, R.sub.4 is carboxy or sulfo, G is an unsubstituted or substituted 1,4-phenylene group or an unsubstituted or substituted 1,4-naphthylene group, and wherein either R.sub.5 and R.sub.6 together are an additional bond and L is an oxygen or sulfur atom or wherein R.sub.5 is hydrogen, R.sub.6 is halomethyl and L is an oxygen atom, and salts thereof, to the use of compounds I and their salts, to a process for the preparation of compounds I and their salts, to starting materials used in that preparation process, and salts thereof, to a process for the preparation of those starting materials and their salts, to a device in which the compounds I and their salts are used, and to a process in which that device is used.
Abstract: A process for the preparation of 6-alkyl-4-(pyridin-3-yl-methyleneamino)-4,5-dihydro-1,2,4-triazin-3(2H)-on e by the reaction of 4-amino-6-alkyl-3-oxo-2,3,4,5-tetrahydro-1,2,4-triazine with 3-cyanopyridine wherein the reaction is carried out under catalytic hydrogenation conditions in the presence of a Raney-nickel catalyst in an aqueous alcoholic medium, at a temperature between 0.degree. and 70.degree. C., at a pH of between 2 and 7, and in the presence of and a C.sub.1 -C.sub.6 -carboxylic acid or a C.sub.1 -C.sub.6 -carboxylic acid alkali metal salt or both, whereby the hydrogen pressure is between 0.1 and 10 bar.
Type:
Grant
Filed:
February 9, 1994
Date of Patent:
February 25, 1997
Assignee:
Ciba-Geigy Corporation
Inventors:
Thomas Pitterna, Urs Siegrist, Henry Szczepanski
Abstract: Compounds of formula I ##STR1## wherein rings A and B are as defined in the specification, have valuable pharmacological properties and are particularly effective as NK1 antagonists and substance P antagonists. Said compounds are prepared in a manner known per se.
Type:
Grant
Filed:
April 16, 1996
Date of Patent:
February 18, 1997
Assignee:
Ciba-Geigy Corporation
Inventors:
Andreas Von Sprecher, Marc Gerspacher, Robert Mah, Silvio Roggo, Walter Schilling, Silvio Ofner, Siem J. Veenstra
Abstract: The invention relates to compounds of the following general formula I ##STR1## especially the compound of formula Ia referred to as thiangazole ##STR2## their pharmaceutically acceptable acid addition salts, processes for their preparation and therapeutic compositions and compositions that can be used in crop-protection.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
February 18, 1997
Assignees:
Ciba-Geigy Corporation, Gesellschaft fur Biotechnologische Forschung mbH
Inventors:
Gerhard H ofle, Norbert Bedorf, Edgar Forche, Klaus Gerth, Herbert Irschik, Rolf Jansen, Brigitte Kunze, Hans Reichenbach, Florenz Sasse, Heinrich Steinmetz, Wolfram Trowitzsch-Kienast, Johannes P. Pachlatko
Abstract: A microbicidal composition comprising metalaxyl and copper hydroxide exerts a synergistically potentiated activity against plant diseases, especially against metalaxyl-resistant pathogens. The active components may be applied in succession in any order or simultaneously.
Abstract: A method of achieving a relaxing, invigorating, tingling bath in the substantial absence of a menthol aroma, comprising incorporating into said bath a bath product formulation comprising menthyl lactate in an amount of about 0.5% to about 15% by weight of said formulation together with a bath product suitable carrier therefor.
Type:
Grant
Filed:
November 14, 1994
Date of Patent:
February 11, 1997
Assignee:
Ciba-Geigy Corporation
Inventors:
Robert Caroselli, Theodore Clemente, Jr., Sandra E. Sandbeck
Abstract: A miniaturized detector cell (4) having a measuring chamber volume of 25 fl-1 .mu.l is described. In spite of its miniaturized construction, the detector cell has an optical path length of about 0.1-100 mm. The incident measuring light (R) is repeatedly reflected at the inner walls (23, 25, 26) of the interaction region (21 ) before it leaves the detector cell (4) again. In a preferred manner, the detector cell (4) is manufactured from silicon or quartz by photolithographic means.