Nitrogen Or Chalcogen Attached Indirectly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/214)
  • Patent number: 5003074
    Abstract: 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: Grant
    Filed: September 28, 1988
    Date of Patent: March 26, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Thomas Allmendinger, Edmond Differding, Robert W. Lang
  • Patent number: 5001138
    Abstract: 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: Grant
    Filed: May 4, 1989
    Date of Patent: March 19, 1991
    Assignee: Nihon Tokushu Noyaku Seizo, K.K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
  • Patent number: 4992421
    Abstract: 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: Grant
    Filed: April 19, 1988
    Date of Patent: February 12, 1991
    Assignee: Abbott Laboratories
    Inventors: Biswanath De, Hwan-Soo Jae, Jacob J. Plattner
  • Patent number: 4987146
    Abstract: 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: Grant
    Filed: July 14, 1989
    Date of Patent: January 22, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Ralph Rohde, Helmut Biere, Ralph Schmiechen, John S. Andrews, David N. Stephens
  • Patent number: 4980363
    Abstract: 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: Grant
    Filed: October 19, 1988
    Date of Patent: December 25, 1990
    Assignee: 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
  • Patent number: 4968681
    Abstract: 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: Grant
    Filed: November 15, 1988
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
  • Patent number: 4968691
    Abstract: 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: Grant
    Filed: March 7, 1989
    Date of Patent: November 6, 1990
    Assignee: Beecham Group P.L.C.
    Inventors: Barry S. Orlek, Michael S. Hadley, Howard E. Rosenberg, Harry J. Wadsworth
  • Patent number: 4964846
    Abstract: 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: Grant
    Filed: November 21, 1988
    Date of Patent: October 23, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Hans-Joachim Gais, Irene Erdelmeier, Rolf Birk
  • Patent number: 4960908
    Abstract: 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: Grant
    Filed: October 21, 1988
    Date of Patent: October 2, 1990
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Noriki Ito, Hiroshi Ogawara, Shunichi Watanabe
  • Patent number: 4956375
    Abstract: 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: Grant
    Filed: November 29, 1989
    Date of Patent: September 11, 1990
    Assignee: Mitsubishi Chemical Industries Limited
    Inventors: Masatsugu Oda, Toshiro Sakaki, Naoko Sasaki, Hirofumi Tomita, Nobuyuki Nonaka
  • Patent number: 4954518
    Abstract: 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: Grant
    Filed: October 7, 1988
    Date of Patent: September 4, 1990
    Assignee: Toyama Chemical Company, Ltd.
    Inventors: Shuntaro Takano, Chosaku Yoshida, Takihiro Inaba, Keiichi Tanaka, Ryuko Takeno, Hideyoshi Nagaki, Tomoya Shimotori, Shinji Makino
  • Patent number: 4952703
    Abstract: 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: Grant
    Filed: May 25, 1989
    Date of Patent: August 28, 1990
    Assignee: Pfizer Inc.
    Inventor: Sarah E. Kelly
  • Patent number: 4943580
    Abstract: 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: Grant
    Filed: February 6, 1989
    Date of Patent: July 24, 1990
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Gaston S. M. Diels, Joseph L. G. Torremans, Francois M. Sommen
  • Patent number: 4937255
    Abstract: 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: Grant
    Filed: March 16, 1989
    Date of Patent: June 26, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
  • Patent number: 4935543
    Abstract: 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: Grant
    Filed: May 18, 1989
    Date of Patent: June 19, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tsuneo Kanamaru, Tsuneaki Hida, Masayuki Muroi
  • Patent number: 4924002
    Abstract: The present invention is a process in which isoxazoles are treated with Mo(CO).sub.6 and then hydrazine to obtain corresponding pyrazoles.
    Type: Grant
    Filed: February 13, 1989
    Date of Patent: May 8, 1990
    Assignee: Warner-Lambert Company
    Inventor: Catherine R. Kostlan
  • Patent number: 4922020
    Abstract: 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: Grant
    Filed: March 17, 1988
    Date of Patent: May 1, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: Peter Gregory, Nigel Hughes
  • Patent number: 4920231
    Abstract: 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: Grant
    Filed: March 30, 1989
    Date of Patent: April 24, 1990
    Assignee: Roussel Uclaf
    Inventors: Werner Bonin, Jean-Pierre Demoute, Jean Tessier
  • Patent number: 4914097
    Abstract: 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: Grant
    Filed: February 23, 1988
    Date of Patent: April 3, 1990
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Masatsugu Oda, Toshiro Sakaki, Naoko Sasaki, Hirofumi Tomita, Nobuyuki Nonaka
  • Patent number: 4906280
    Abstract: 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: Grant
    Filed: October 14, 1987
    Date of Patent: March 6, 1990
    Assignee: Pennwalt Corporation
    Inventors: Stanley R. Sandler, Shyam B. Advani
  • Patent number: 4904661
    Abstract: 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: Grant
    Filed: December 16, 1987
    Date of Patent: February 27, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
  • Patent number: 4904660
    Abstract: 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: Grant
    Filed: February 25, 1988
    Date of Patent: February 27, 1990
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kohji Nakano, Takashi Fujikura, Ryuichiro Hara, Masato Ichihara, Yukiko Fukunaga, Masayuki Shibasaki
  • Patent number: 4900825
    Abstract: 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: Grant
    Filed: June 1, 1988
    Date of Patent: February 13, 1990
    Assignee: BASF Aktiengsellschaft
    Inventors: Hermann Koehler, Toni Dockner
  • Patent number: 4889953
    Abstract: 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: Grant
    Filed: July 22, 1987
    Date of Patent: December 26, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
  • Patent number: 4882342
    Abstract: 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: Grant
    Filed: October 6, 1987
    Date of Patent: November 21, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang von der Saal, Jens-Peter Holck, Alfred Mertens, Bernd Muller-Beckmann, Lothar Kling
  • Patent number: 4880802
    Abstract: 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: Grant
    Filed: December 8, 1987
    Date of Patent: November 14, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4876263
    Abstract: 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: Grant
    Filed: June 17, 1988
    Date of Patent: October 24, 1989
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shoko Sasaki, Koichi Moriya, Yumi Hattori, Katsuhiko Shibuya
  • Patent number: 4863947
    Abstract: 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: Grant
    Filed: August 11, 1986
    Date of Patent: September 5, 1989
    Assignee: Rohm and Haas
    Inventor: Richard M. Jacobson
  • Patent number: 4864029
    Abstract: 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: Grant
    Filed: May 11, 1988
    Date of Patent: September 5, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Jelich, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
  • Patent number: 4863940
    Abstract: 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: Grant
    Filed: July 26, 1984
    Date of Patent: September 5, 1989
    Assignee: Rohm and Haas
    Inventor: Ashok K. Sharma
  • Patent number: 4857522
    Abstract: 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: Grant
    Filed: March 21, 1988
    Date of Patent: August 15, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard A. DiPietro, Jan-I Tu, Noor Z. Turabi
  • Patent number: 4853470
    Abstract: 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: Grant
    Filed: December 23, 1988
    Date of Patent: August 1, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventor: Joseph T. Strupczewski
  • Patent number: 4851406
    Abstract: 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: Grant
    Filed: September 4, 1986
    Date of Patent: July 25, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Alfred Mertens, Wolfgang von der Saal, Walter-Gunar Friebe, Bernd Muller-Beckmann, Gisbert Sponer
  • Patent number: 4851422
    Abstract: 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: Grant
    Filed: April 30, 1986
    Date of Patent: July 25, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideaki Natsugari, Yasuhiko Kawano, Akira Morimoto, Kouichi Yoshioka
  • Patent number: 4849432
    Abstract: 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: Grant
    Filed: February 24, 1987
    Date of Patent: July 18, 1989
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hattori
  • Patent number: 4841063
    Abstract: 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: Grant
    Filed: January 31, 1984
    Date of Patent: June 20, 1989
    Assignee: Givaudan Corporation
    Inventors: Joseph A. Virgilio, Milton Manowitz, Emanuel Heilweil
  • Patent number: 4837225
    Abstract: 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: Grant
    Filed: July 17, 1986
    Date of Patent: June 6, 1989
    Assignee: Cassell Aktiengesellschaft
    Inventors: Gerhard Zoller, Rudi Beyerle, Ursula Schindler, Rolf-Eberhard Nitz, Piero Martorana
  • Patent number: 4835280
    Abstract: 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: Grant
    Filed: July 14, 1987
    Date of Patent: May 30, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Alfred Martens, Jens-Peter Holck, Herbert Berger, Bernd Muller-Beckman, Klaus Strein, Egon Roesch
  • Patent number: 4833252
    Abstract: 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: Grant
    Filed: September 28, 1988
    Date of Patent: May 23, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Werner Topfl, Georg Pissiotas
  • Patent number: 4831032
    Abstract: 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: Grant
    Filed: July 3, 1986
    Date of Patent: May 16, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
  • Patent number: 4831161
    Abstract: Prepare N-(amidoalkyl)imides by contacting an imide with a 2-oxazoline under reaction conditions, optionally in the presence of a solvent.
    Type: Grant
    Filed: June 24, 1987
    Date of Patent: May 16, 1989
    Assignee: The Dow Chemical Company
    Inventors: Pen-Chung Wang, Steven P. Crain
  • Patent number: 4812471
    Abstract: 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: Grant
    Filed: February 8, 1988
    Date of Patent: March 14, 1989
    Assignee: Pfizer Inc.
    Inventor: Rodney C. Schnur
  • Patent number: 4810282
    Abstract: This invention relates to ortho-(isoxazolyl, isothiazolyl, pyrazolyl, thiadiazolyl, oxadiazolyl, and triazolyl)benzenesulfonamides and their use as herbicides.
    Type: Grant
    Filed: June 10, 1987
    Date of Patent: March 7, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Morris P. Rorer
  • Patent number: 4810716
    Abstract: 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: Grant
    Filed: March 3, 1987
    Date of Patent: March 7, 1989
    Assignee: Warner-Lambert Company
    Inventors: David T. Connor, Daniel L. Flynn
  • Patent number: 4792606
    Abstract: 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: Grant
    Filed: July 16, 1987
    Date of Patent: December 20, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhard Lantzsch, Hermann-Dieter Krall
  • Patent number: 4791131
    Abstract: 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: Grant
    Filed: December 31, 1987
    Date of Patent: December 13, 1988
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4785116
    Abstract: 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: Grant
    Filed: January 18, 1985
    Date of Patent: November 15, 1988
    Assignee: BASF Aktiengesellschaft
    Inventors: Heinz Eilingsfeld, Karl-Heinz Etzbach
  • Patent number: 4772714
    Abstract: 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: Grant
    Filed: July 7, 1986
    Date of Patent: September 20, 1988
    Assignee: Agency of Industrial Science & Technology
    Inventors: Masato Tanaka, Toshiyasu Sakakura
  • Patent number: 4772309
    Abstract: 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: Grant
    Filed: March 19, 1987
    Date of Patent: September 20, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jorg Stetter, Reinhold Gehring, Otto Schallner, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
  • Patent number: 4772683
    Abstract: 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: Grant
    Filed: February 24, 1986
    Date of Patent: September 20, 1988
    Assignee: Bristol-Myers Company
    Inventors: Alain Martel, Jean-Paul Daris, Jacques Corbeil