Nitrogen Or Chalcogen Attached Indirectly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/214)
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Patent number: 5003074Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl or aryl, m and n are 0 or 1, and A is a divalent organic radical which, with (CR.sup.1 R.sup.2).sub.m NF--SO.sub.2 (CR.sup.3 R.sup.4).sub.n groups, forms a 5- to 8-membered ring, are admirably suitable fluorinating agents for fluorinating carbon atoms, especially as stereospecific fluorinating agents, when the compounds contain a chiral carbon atom and are in optically active form. The compounds of formula I are prepared by reacting the corresponding silated sulfonamides, wherein the NF group is replaced by an N-SiR.sup.7 R.sup.8 R.sup.9 group and R.sup.7, R.sup.8 R.sup.9 are each independently C.sub.1 -C.sub.12 alkyl, cyclopentyl, cyclohexyl, benzyl or phenyl, with a fluorinating agent.Type: GrantFiled: September 28, 1988Date of Patent: March 26, 1991Assignee: Ciba-Geigy CorporationInventors: Thomas Allmendinger, Edmond Differding, Robert W. Lang
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Patent number: 5001138Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.Type: GrantFiled: May 4, 1989Date of Patent: March 19, 1991Assignee: Nihon Tokushu Noyaku Seizo, K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
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Patent number: 4992421Abstract: The present invention relates to novel luteinizing hormone releasing hormone antagonists ##STR1## The invention also relates to pharmaceutical compositions containing such compounds and to the use of such compounds for suppressing levels of sex hormones in male or female mammals.Type: GrantFiled: April 19, 1988Date of Patent: February 12, 1991Assignee: Abbott LaboratoriesInventors: Biswanath De, Hwan-Soo Jae, Jacob J. Plattner
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Patent number: 4987146Abstract: N-hetaryl imidazole derivatives of general Formula I ##STR1##are disclosed in whichHet represents an optionally substituted monocyclic or bicyclic heteroaromate,R.sup.3 represents hydrogen, a straight or branched C.sub.1-6 -alkyl group, or a C.sub.1-6 -alkoxy-alkyl group, andR.sup.4 represents --COOR.sup.5 --CONR.sup.6 R.sup.7 --CN, ##STR2##with R.sup.5 meaning hydrogen, a straight or branched C.sub.1-6 -alkyl group, R.sup.6 and R.sup.7 are the same of different and represent hydrogen or a straight, branched, or cyclic alkyl group with up to 7 carbon atoms or, together with the nitrogen atom, form a saturated five or six ring optionally containing another heteroatom and R.sup.8 means hydrogen or a straight, branched or cyclic alkyl group with up to 7 carbon atoms.Type: GrantFiled: July 14, 1989Date of Patent: January 22, 1991Assignee: Schering AktiengesellschaftInventors: Ralph Rohde, Helmut Biere, Ralph Schmiechen, John S. Andrews, David N. Stephens
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Patent number: 4980363Abstract: An amide derivative represented by the following general formula (I) ##STR1## wherein one of X and Y represents a sulfur atom and the other represents a carbon atom, Z represents a nitrile or thioamide group, each of R.sup.1 and R.sup.2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, a halomethyl group or a phenyl group, and R.sup.Type: GrantFiled: October 19, 1988Date of Patent: December 25, 1990Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Hitoshi Shimotori, Yoshiro Kanemoto, Hideo Yamazaki, Tsutomu Ishii, Shuji Ozawa, Yuji Yanase, Toshiaki Kuwatsuka, Yoshinori Tanaka, Takeshi Sekine, Keiko Shinada
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Patent number: 4968681Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical, are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: November 15, 1988Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 4968691Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which X represents a group ##STR2## in which p represents an integer of 2 to 4; r represents an integer of 1 or 2; s represents 0 or 1; and A represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, any amino nitrogen optionally substituted by a C.sub.1-4 alkyl group, and when (p,r,s) is (2,2,0) or (2,2,1) any A comprising 2 heteroatoms is optionally C-substituted by a methyl group, and when (p,r,s) is (2,1,0), (2,1,1) or (3,1,0) any A comprising 2 heteroatoms is optionally C-substituted by C.sub.1-2 alkyl and any A comprising one heteroatom is optionally C-substituted by a methyl group, and wherein compounds of formula (I) having two asymetric centers have the stereo-chemical configuration in which the group X and the (CH.sub.2).sub.Type: GrantFiled: March 7, 1989Date of Patent: November 6, 1990Assignee: Beecham Group P.L.C.Inventors: Barry S. Orlek, Michael S. Hadley, Howard E. Rosenberg, Harry J. Wadsworth
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Patent number: 4964846Abstract: This invention comprises a process for the production of unsymmetrical olefins from prochiral symmetrical ketones by addition of lithiosulfoximine from n-butyllithium and N-substituted S-methyl-S-phenyl-sulfoximine derivatives and then reaction with n-butyllithium/trimethychlorosilane.Type: GrantFiled: November 21, 1988Date of Patent: October 23, 1990Assignee: Schering AktiengesellschaftInventors: Hans-Joachim Gais, Irene Erdelmeier, Rolf Birk
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Patent number: 4960908Abstract: Novel isoflavone derivatives are provided which have the formula ##STR1## and which exhibit cancerocidal and immunosuppressive activity. The invention also provides pharmaceutical compositions containing the derivatives, methods of use and processes for their preparation.Type: GrantFiled: October 21, 1988Date of Patent: October 2, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Hiroshi Ogawara, Shunichi Watanabe
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Patent number: 4956375Abstract: Disclosed herein is an N-indanyl carboxamide derivative as a novel compound, represented by the following general formula (I): ##STR1## wherein A represents a group of the formula, ##STR2## (wherein X represents a halogen atom, a methyl group, or a trifluoromethyl group, Y represents a hydrogen atom, a halogen atom, a lower alkyl group, an amino group, a mercapto group, or a lower alkylthio group, R.sup.1 represents a methyl group or a trifluoromethyl group, and R.sup.2 and R.sup.3 independently represents a hydrogen atom or a methyl group), R represents a lower alkyl group, and n is an integer in the range of 1 to 6, and an agricultural/horticultural fungicide comprising said N-indanyl carboxamide derivative as an active ingredient.Type: GrantFiled: November 29, 1989Date of Patent: September 11, 1990Assignee: Mitsubishi Chemical Industries LimitedInventors: Masatsugu Oda, Toshiro Sakaki, Naoko Sasaki, Hirofumi Tomita, Nobuyuki Nonaka
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Patent number: 4954518Abstract: This invention relates to a 4H-1-benzopyran-4-one derivative represented by the formula: ##STR1## or a salt thereof, a process for producing the same and a pharmaceutical composition comprising the same as active ingredient.Type: GrantFiled: October 7, 1988Date of Patent: September 4, 1990Assignee: Toyama Chemical Company, Ltd.Inventors: Shuntaro Takano, Chosaku Yoshida, Takihiro Inaba, Keiichi Tanaka, Ryuko Takeno, Hideyoshi Nagaki, Tomoya Shimotori, Shinji Makino
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Patent number: 4952703Abstract: Preparation of 2-oxindole-1-carboxamides by reaction of 2-oxindoles with trichloracetyl isocyanate to produce novel N-trichloroacetyl-2-oxindole-1-carboxamides which are then hydrolyzed to 2-oxindole-1-carboxamides useful as analgesic and anti-inflammatory agents and/or intermediates for such agents.Type: GrantFiled: May 25, 1989Date of Patent: August 28, 1990Assignee: Pfizer Inc.Inventor: Sarah E. Kelly
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Patent number: 4943580Abstract: Novel 1-alkyl substituted benzimidazole derivatives and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.Type: GrantFiled: February 6, 1989Date of Patent: July 24, 1990Assignee: Janssen Pharmaceutica N.V.Inventors: Frans E. Janssens, Gaston S. M. Diels, Joseph L. G. Torremans, Francois M. Sommen
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Patent number: 4937255Abstract: For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, a cation or alkyl, aryl or aralkyl.Type: GrantFiled: March 16, 1989Date of Patent: June 26, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
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Patent number: 4935543Abstract: A novel compound of the formula (I): ##STR1## wherein R.sub.1 is optionally esterified or amidated carboxyl; R.sub.2, R.sub.3 and R.sub.4 are the same or different and are hydrogen or halogen or alkyl; A is formyl, hydroxyiminomethyl or carboxyl; and A is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active compound the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R.sub.1 is carboxyl, R.sub.2, R.sub.3 and R.sub.4 are hydrogen and X is formyl are also disclosed.Type: GrantFiled: May 18, 1989Date of Patent: June 19, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Kanamaru, Tsuneaki Hida, Masayuki Muroi
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Patent number: 4924002Abstract: The present invention is a process in which isoxazoles are treated with Mo(CO).sub.6 and then hydrazine to obtain corresponding pyrazoles.Type: GrantFiled: February 13, 1989Date of Patent: May 8, 1990Assignee: Warner-Lambert CompanyInventor: Catherine R. Kostlan
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Patent number: 4922020Abstract: A compound of the formula: ##STR1## wherein A is ##STR2## B is a group of the formula: ##STR3## when B is of Formula III, X is of Formula III;when B is of Formula IV,X is selected from H, phenyl, substituted phenyl, naphthyl, substituted naphthyl, thienyl, substituted thienyl, thiazol-5-yl and substituted thiazol-5-yl in which the substituents are selected from NR.sup.7 R.sup.8, NO.sub.2, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.2-4 -alkenyl, halogen, cyano and phenyl;each Q is independently selected from H, C.sub.1-4 -alkyl, phenyl and benzyl;and wherein each benzene ring in Formulae II, III and IV has no further substituents or carries 1 or 2 further substituents selected from halogen, C.sub.1-4 -alkyl and C.sub.1-4 -alkoxy.The compound is suitable for use as a charge transport material in organic photoconductors, as a charge control agent in electroreprographic toners and as a color former in pressure sensitive recording materials.Type: GrantFiled: March 17, 1988Date of Patent: May 1, 1990Assignee: Imperial Chemical Industries PLCInventors: Peter Gregory, Nigel Hughes
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Patent number: 4920231Abstract: A process for the preparation of trifluoromethylvinyl compounds in all their possible streoisomeric forms and mixtures thereof comprising reacting a salt of trifluoroacetic acid with a halovinyl compound in the presence of a cuprous salt to obtain the same stereo-specific compound and all possible stereo-isomeric forms and mixtures thereof of 1R, trans compounds of the formula ##STR1## wherein R is an alcohol residue used in pyrethrinoid series, or an alcohol residue capable of blocking the acid function, and Z is aryl or haloaryl and the double bond has Z geometry having pesticide activity.Type: GrantFiled: March 30, 1989Date of Patent: April 24, 1990Assignee: Roussel UclafInventors: Werner Bonin, Jean-Pierre Demoute, Jean Tessier
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Patent number: 4914097Abstract: Disclosed herein is an N-indanyl carboxamide derivative as a novel compound, represented by the following general formula (I): ##STR1## wherein A represents a group of the formula, ##STR2## (wherein X represents a halogen atom, a methyl group, or a trifluoromethyl group, Y represents a hydrogen atom, a halogen atom, a lower alkyl group, an amino group, a mercapto group, or a lower alkylthio group, R.sup.1 represents a methyl group or a trifluoromethyl group, and R.sup.2 and R.sup.3 independently represents a hydrogen atom or a methyl group), R represents a lower alkyl group, and n is an integer in the range of 1 to 6, and an agricultural/horticultural fungicide comprising said N-indanyl carboxamide derivative as an active ingredient.Type: GrantFiled: February 23, 1988Date of Patent: April 3, 1990Assignee: Mitsubishi Kasei CorporationInventors: Masatsugu Oda, Toshiro Sakaki, Naoko Sasaki, Hirofumi Tomita, Nobuyuki Nonaka
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Patent number: 4906280Abstract: T-butylhydrazides of carboxylic acid anhydrides and carboxylic acid chlorides useful as plant growth regulants in the free acid form or their equivalent salts.Type: GrantFiled: October 14, 1987Date of Patent: March 6, 1990Assignee: Pennwalt CorporationInventors: Stanley R. Sandler, Shyam B. Advani
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Patent number: 4904661Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.Type: GrantFiled: December 16, 1987Date of Patent: February 27, 1990Assignee: Imperial Chemical Industries PLCInventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
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Patent number: 4904660Abstract: Novel compounds of the following formula (I) and their salts: A compound of the formula (I) ##STR1## These compounds are expected to be useful for renin inhibitors. Thus, the compounds are useful medical agents, in particular, anti-hypertensive agents.Type: GrantFiled: February 25, 1988Date of Patent: February 27, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kohji Nakano, Takashi Fujikura, Ryuichiro Hara, Masato Ichihara, Yukiko Fukunaga, Masayuki Shibasaki
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Patent number: 4900825Abstract: 4-Nitro-5-imidazolyl ethers and thioethers of the formula I ##STR1## where R.sup.1 is alkyl, alkoxyalkyl, cycloalkyl, aryl, aralkyl or alkylaryl, R.sup.2 is hydrogen, alkyl, cycloalkyl, aryl, aralkyl or alkylaryl, R.sup.3 is alkyl, cycloalkyl, aryl, aralkyl, alkylaryl or a heterocyclic or heteroaromatic radical or a counter-ion of the corresponding alcoholate or thiolate or, where X is sulfur, R.sup.3 is hydrogen, and X is oxygen or sulfur, and the stated organic radicals may furthermore carry substituents which are inert under the reaction conditions, are prepared by reacting a dinitroimidazole of the formula II ##STR2## with an alcohol or thiol of the formula IIIR.sup.3 --XH (III)in a solvent or diluent at a pH of the from 4 to 16.Type: GrantFiled: June 1, 1988Date of Patent: February 13, 1990Assignee: BASF AktiengsellschaftInventors: Hermann Koehler, Toni Dockner
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Patent number: 4889953Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.Type: GrantFiled: July 22, 1987Date of Patent: December 26, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
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Patent number: 4882342Abstract: The present invention concerns new 5-alkylbenzimidazoles of the formula: ##STR1## wherein R.sub.1 is a phenyl ring of the formula: ##STR2## or R.sub.1 is naphthyl, heterocycle or a bicyclic heterocycle and R.sub.1 -R.sub.7 are described in claim 1.These compounds are useful for prophylaxis or treatment of heart and circulatory disease especially to increase contractility of the heart, lower blood pressure and/or influence the thrombocyte function and improve the microcirculation.Type: GrantFiled: October 6, 1987Date of Patent: November 21, 1989Assignee: Boehringer Mannheim GmbHInventors: Wolfgang von der Saal, Jens-Peter Holck, Alfred Mertens, Bernd Muller-Beckmann, Lothar Kling
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Patent number: 4880802Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine or a group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,d denotes a number 2 or 3, andX denotes oxygen, sulphur, or NR.sup.5,and their salts.Type: GrantFiled: December 8, 1987Date of Patent: November 14, 1989Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4876263Abstract: Nitro-subsliluted heterocyclic compounds of the formula (I) ##STR1## wherein R is hydrogen or alkyl, Z is an optionally substituted aryl or optionally subtituted heterocyclic groun containing at least one atom selected from N, O and S,A is optionally substituted ethylene or optionally substituted trimethylene, andB stands for 2 or 3 members of a heterocyclic ring which is formed, together with the adjacent C-atom and N-aom and at least one of said members may represent a hetero atom and may be optionally substituted, provided that when B stands for 3 members, two of which are carbon atoms and the other one is a nitrogen atom which is located in the middle of the three members, then at least one of said two carbon atoms must be substituted by a keto group. Such compounds being useful as insecticides.Type: GrantFiled: June 17, 1988Date of Patent: October 24, 1989Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shoko Sasaki, Koichi Moriya, Yumi Hattori, Katsuhiko Shibuya
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Patent number: 4863947Abstract: This invention relates to novel N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: August 11, 1986Date of Patent: September 5, 1989Assignee: Rohm and HaasInventor: Richard M. Jacobson
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Patent number: 4864029Abstract: Microbicidal substituted pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkyllaminocarbonylalkyl or dialkylaminocarbonylalkyl, or represent in each case optionally substituted oxiranylalkyl, aralkyl, heterocyclyl or aryl andHet represents an optionally substituted heterocyclic radical.Intermediates therefor of the formula ##STR2## in which R is alkyl, are also new.Type: GrantFiled: May 11, 1988Date of Patent: September 5, 1989Assignee: Bayer AktiengesellschaftInventors: Klaus Jelich, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
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Patent number: 4863940Abstract: Certain N-acetonyl-substituted-amides of the formula: ##STR1## wherein A is a heterocycle, a phenylalkyl, a phenylalkoxy, naphthyl, cycloalkyl, alkoxyalkyl, alkyl, haloalkyl or alkenyl group; X, Y and Z are selected from the group consisting of hydrogen, halo, cyano, thiocyano, isothiocyano, methylsulfonyloxy, thio(C.sub.1 -C.sub.2) alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyloxy, thiocarbamoylthio, hydroxy, azide, trifluoromethylcarboxy, (C.sub.1 -C.sub.4)alkylcarbonyloxy, phenylcarbonyloxy, phenoxy, thiophenyl, imidazolyl or triazolyl group as described herein; R.sup.1 and R.sup.2 are each independently a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group; and compositions containing these amides are fungicidally active, particularly against phytopathogenic fungi.Type: GrantFiled: July 26, 1984Date of Patent: September 5, 1989Assignee: Rohm and HaasInventor: Ashok K. Sharma
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Patent number: 4857522Abstract: Derivatives of pravastatin are provided which are useful in inhibiting cholesterol biosynthesis and in preparing radiolabeled compounds useful in the radioimmunoassay (RIA) of pravastatin and derivatives thereof. The pravastatin derivatives have the structure ##STR1## wherein R is hydroxy, lower alkylamine, arylamine, arylalkylamine or heterocyclic alkylamine such as histamine, tyramine, O-benzyltyramine, methyl tyrosinate as well as iodinated derivatives thereof.Type: GrantFiled: March 21, 1988Date of Patent: August 15, 1989Assignee: E. R. Squibb & Sons, Inc.Inventors: Richard A. DiPietro, Jan-I Tu, Noor Z. Turabi
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Patent number: 4853470Abstract: Novel 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles, intermediates and processes for the preparation thereof, and methods for treating psychoses, treating depression, alleviating pain, treating convulsions and treating hypertension utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: December 23, 1988Date of Patent: August 1, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventor: Joseph T. Strupczewski
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Patent number: 4851406Abstract: The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.Type: GrantFiled: September 4, 1986Date of Patent: July 25, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Wolfgang von der Saal, Walter-Gunar Friebe, Bernd Muller-Beckmann, Gisbert Sponer
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Patent number: 4851422Abstract: The compound represented by the formula: ##STR1## where R.sup.1 stands for amino or an organic residue bonded through nitrogen; R.sup.2 stands for carboxyl or a group derivable therefrom; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 independently stand for hydrogen or an organic residue, including the case where R.sup.5 or R.sup.6 forms a chemical bond or a ring with R.sup.7 or R.sup.8 ; X stands for hydrogen, methoxy or formylamino; or a salt thereof, produceable by the present method, exhibits excellent antimicrobial activity, and is utilized as antimicrobial agents.Type: GrantFiled: April 30, 1986Date of Patent: July 25, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Yasuhiko Kawano, Akira Morimoto, Kouichi Yoshioka
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Patent number: 4849432Abstract: Novel heterocyclic compounds of the formula ##STR1## wherein, R.sup.1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group ##STR2## in which R.sup.2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R.sup.3 represents a hydrogen atom or an alkyl group, and Z represents an optionally sibstituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group.The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: February 24, 1987Date of Patent: July 18, 1989Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hattori
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Patent number: 4841063Abstract: This disclosure relates to a novel class of 2-alkyl-3-haloisothiazolium salts. These salts have been found to be useful in controlling the growth of bacteria and fungi. They have also been found to be useful intermediates in the preparation of novel and known antibacterial and antifungal compounds.Type: GrantFiled: January 31, 1984Date of Patent: June 20, 1989Assignee: Givaudan CorporationInventors: Joseph A. Virgilio, Milton Manowitz, Emanuel Heilweil
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Patent number: 4837225Abstract: 2,5-Dimethylpyrrole derivatives of the formula I ##STR1## in which R denotes alkyl which is substituted by --NH.sub.2, acylamino of the formula--NH--CX--R.sup.1or by an optionally substituted heterocycle having 1 hetero member; or denotes an optionally substituted heterocycle having 1 member, and X and R.sup.1 have the meanings givenand their pharmacologically acceptable acid addition salts, their preparation by reaction of amines of the formula IIR--NH.sub.2 (II)with acetonylacetone or by acylating N-aminoalkyl-2,5-dimethylpyrroles, and their use as pharmaceutical active compounds.Type: GrantFiled: July 17, 1986Date of Patent: June 6, 1989Assignee: Cassell AktiengesellschaftInventors: Gerhard Zoller, Rudi Beyerle, Ursula Schindler, Rolf-Eberhard Nitz, Piero Martorana
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Patent number: 4835280Abstract: The present invention provides Indolines of the formula: ##STR1## ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.Type: GrantFiled: July 14, 1987Date of Patent: May 30, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Martens, Jens-Peter Holck, Herbert Berger, Bernd Muller-Beckman, Klaus Strein, Egon Roesch
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Patent number: 4833252Abstract: Substituted N-phenylsulfonyl-N'-pyrimidinylureas and N-phenylsulfonyl-N'-triazinylureas of the general formula ##STR1## and the salts thereof with amines, alkali metal bases or alkaline earth metal bases, or with quaternary ammonium bases, have good pre- and postemergence selective herbicidal and growth regulating properties.In the above formula the symbols have the following meanings:R.sup.1 is hydrogen, halogen, nitro, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkylsulfinyl, --CO--R.sup.8, --NR.sup.9 R.sup.10, --CO--NR.sup.11 R.sup.12 or --SO.sub.2 --NR.sup.13 R.sup.14,R.sup.2 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl or C.sub.1 -C.sub.4 alkylsulfonyl,R.sup.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl or cyano,R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl,R.sup.5 is hydrogen, C.sub.Type: GrantFiled: September 28, 1988Date of Patent: May 23, 1989Assignee: Ciba-Geigy CorporationInventors: Werner Topfl, Georg Pissiotas
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Patent number: 4831032Abstract: The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.Type: GrantFiled: July 3, 1986Date of Patent: May 16, 1989Assignee: Boehringer Mannheim GmbHInventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
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Patent number: 4831161Abstract: Prepare N-(amidoalkyl)imides by contacting an imide with a 2-oxazoline under reaction conditions, optionally in the presence of a solvent.Type: GrantFiled: June 24, 1987Date of Patent: May 16, 1989Assignee: The Dow Chemical CompanyInventors: Pen-Chung Wang, Steven P. Crain
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Patent number: 4812471Abstract: Hypoglycemic 5-chromanyl, 2,3-dihydro-5-benzo[b]-furanyl, 5-pyridyl, 5-quinolyl, 5-pyrrolyl, 5-indolyl, 5-thiazolyl, 5-oxazolyl, 5-isothiazolyl and 5-isoxazolyl oxazolidine-2.4-diones and the pharmacetically-acceptable salts thereof; certain 3-acylated derivatives thereof; a method of treating hyperglycemic animals therewith; and intermediates useful in the preparation of said compounds.Type: GrantFiled: February 8, 1988Date of Patent: March 14, 1989Assignee: Pfizer Inc.Inventor: Rodney C. Schnur
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Patent number: 4810282Abstract: This invention relates to ortho-(isoxazolyl, isothiazolyl, pyrazolyl, thiadiazolyl, oxadiazolyl, and triazolyl)benzenesulfonamides and their use as herbicides.Type: GrantFiled: June 10, 1987Date of Patent: March 7, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Morris P. Rorer
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Patent number: 4810716Abstract: The present invention is novel diarylalkanoids having activity as lipoxygenase inhibitors, novel pharmaceutical compositions therefor, and novel methods of use in treating asthma, allergies, cardiovascular diseases, migraines, psoriasis and immunoinflammatory diseases for diarylalkanoids. The compounds of this invention are also useful as cytoprotective agents.Type: GrantFiled: March 3, 1987Date of Patent: March 7, 1989Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn
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Patent number: 4792606Abstract: A process for the preparation of a dimeric aromatic acyl cyanide of the formula ##STR1## in which Ar is optionally substituted phenyl, naphthyl or hetaryl,comprising reaction an acyl halide of the formulaAr--CO--Halin whichHal is fluorine, chlorine or bromine, with an alkali metal cyanide in a two-phase system comprising water and a water-immiscible or only sparingly water-miscible aliphatic ketone, and in the presence of a phase-transfer catalyst. The products are known intermediates for pesticides.Type: GrantFiled: July 16, 1987Date of Patent: December 20, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Hermann-Dieter Krall
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Patent number: 4791131Abstract: Certain new 2-oxindole-3-carboxamide compounds having an acyl substituent at the 1-position are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and anti-inflammatory agents in mammalian subjects. In particular, the compounds of the invention are useful for acute administration for ameliorating or eliminating pain in human subjects recovering from surgery or trauma, and also for chronic administration for alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects.Type: GrantFiled: December 31, 1987Date of Patent: December 13, 1988Assignee: Pfizer Inc.Inventor: Saul B. Kadin
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Patent number: 4785116Abstract: Novel compounds of the general formula I ##STR1## where X and Y independently of one another are each carboxyl, a carboxylic ester group, cyano or an unsubstituted or substituted carbamyl or carboxylic hydrazide group and X and Y together form a radical of the formula ##STR2## where R.sup.1 is hydrogen or a radical of a primary amine and R.sup.2 and R.sup.3 are each hydrogen or unsubstituted or substituted alkyl, cycloalkyl or aryl, are very useful as diazo components.Type: GrantFiled: January 18, 1985Date of Patent: November 15, 1988Assignee: BASF AktiengesellschaftInventors: Heinz Eilingsfeld, Karl-Heinz Etzbach
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Patent number: 4772714Abstract: Disclosed is a process for the preparation of alpha-aryl and alpha-heteroaryl ketones useful as intermediates in the synthesis of various pharmaceutical and agricultural chemicals, which process operates according to the following reaction scheme: ##STR1##Type: GrantFiled: July 7, 1986Date of Patent: September 20, 1988Assignee: Agency of Industrial Science & TechnologyInventors: Masato Tanaka, Toshiyasu Sakakura
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Patent number: 4772309Abstract: A 5-Acylamino-pyrazole derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,R.sup.3 represents hydrogen or alkyl,R.sup.4 represents hydrogen or alkyl,X represents oxygen or sulphur,n represents the integer 0, 1 or 2,Ar represents in each case optionally substituted phenyl or pyridyl andHet represents an optionally substituted 5- or 6- membered heterocyclic radical linked via a carbon atom,which exhibit herbicidal and plant growth regulating activity.Type: GrantFiled: March 19, 1987Date of Patent: September 20, 1988Assignee: Bayer AktiengesellschaftInventors: Jorg Stetter, Reinhold Gehring, Otto Schallner, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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Patent number: 4772683Abstract: Disclosed herein is a novel process using novel silyl enol ether intermediates of the formula ##STR1## to generate novel azetidione thiolester intermediates of the formula ##STR2## which can be used to form 1-.beta.-alkyl carbapenem antibiotics. It has now been discovered that if the R.sup.4 group is selected from a small group of moieties having the formula: ##STR3## an increased .beta.-yield of up to approximately 100% can be obtained.Type: GrantFiled: February 24, 1986Date of Patent: September 20, 1988Assignee: Bristol-Myers CompanyInventors: Alain Martel, Jean-Paul Daris, Jacques Corbeil