Double Bonded Divalent Chalcogen Containing Patents (Class 544/52)
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Patent number: 6448246Abstract: Disclosed are 4H-1,4-Benzothiazine-2-carboxamides. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, depression, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.Type: GrantFiled: May 25, 2000Date of Patent: September 10, 2002Assignee: Neurogen CorporationInventors: Guolin Cai, Gang Liu, Pamela A. Albaugh
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Publication number: 20020115853Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: 1Type: ApplicationFiled: February 12, 2002Publication date: August 22, 2002Inventors: Puwen Zhang, Reinhold H. W. Bender, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6410484Abstract: A 5,6-dihydrouracil compound given by the formula [I]: wherein, R1 represents C1-C2 haloalkyl group and Q represents Q1 of the formula below, etc.: wherein, R3 is hydrogen atom or halogen atom, R15 is C3-C6 alkynyl group, etc., Z is oxygen atom, sulfur atom or NH group, and T is direct bond or methylene group, has an excellent herbicidal efficacy.Type: GrantFiled: October 30, 2000Date of Patent: June 25, 2002Assignee: Sumitomo Chemical Company, LimitedInventors: Minoru Takano, Hirofumi Mishima
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Patent number: 6339155Abstract: The uracil compounds represented by the formula [V]: wherein R1 represents C1-C5 perfluoroalkyl group and Q represents an aromatic group, can be produced by making the amide compounds represented by the formula [II]: wherein R1 and Q have the same meanings defined above, or its hydrate react with a cyanate salt in the presence of a protonic acid.Type: GrantFiled: November 13, 2000Date of Patent: January 15, 2002Assignee: Sumitomo Chemical Company, LimitedInventors: Minoru Takano, Hirofumi Mishima
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Patent number: 6339084Abstract: A process of forming the cis- or the trans-isomers of thiazine-indigo compounds comprising the step of reacting o-aminomercapto-carbocyclic or -heterocyclic compounds with a maleic acid or fumaric acid derivative in the presence of an aqueous system. The invention further relates to a process of converting cis-isomers of thiazine-indigo compounds into the trans-isomers being pigments. The invention also relates to the cis-isomers of thiazine-indigo compounds of formula I as defined in claim 14 which are new compounds.Type: GrantFiled: July 19, 2000Date of Patent: January 15, 2002Assignee: Clariant Finance (BVI) LimitedInventors: Bansi Lal Kaul, Bruno Piastra
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Publication number: 20020004596Abstract: A process for preparing symmetrical or asymmetrical trans-thiazineindigo pigments of the formula (1) 1Type: ApplicationFiled: June 21, 2001Publication date: January 10, 2002Applicant: Clariant GmbHInventors: Petra Maria Rothe, Leonhard Unverdorben, Bruno Piastra
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Patent number: 6333413Abstract: Carboxylic acids of formula (1): wherein R2 and R3 are independently hydrogen or C1-C3 alkyl, and Q is optionally substituted phenyl, can be easily converted by ring closing into pyridazin-3-one derivatives of formula (7): The carboxylic acids of formula (1) can be produced by reacting hydrazone compounds of formula (5): wherein R3 and Q are as defined above, with malonic acid derivatives of formula (6): R2CH(COOH)2 wherein R2 is as defined above, in the presence of a base.Type: GrantFiled: July 17, 2000Date of Patent: December 25, 2001Assignee: Sumitomo Chemical Company, LimitedInventor: Takashi Furukawa
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Patent number: 6303542Abstract: This invention relates to 3-substituted-phenyl-1,2,3-benzotriazin-4-ones which have activity as herbicides, to compositions which contain these compounds and to methods of use of these compounds.Type: GrantFiled: August 18, 2000Date of Patent: October 16, 2001Assignee: Rohm and Haas CompanyInventors: Bin Li, Adam Chi-Tung Hsu
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Patent number: 6300342Abstract: Antithrombotic phenylalkyl derivatives of the formula Exemplary compounds are: (a) 1-[3-(4-amidino-phenyl)propionyl]-6-(4-fluoro-phenylsulphonamido)-1,2,3,4-tetrahydro-quinoline, (b) 1-[3-(4-amidino-phenyl)propionyl]-6-butylsulphonamido-1,2,3,4-tetrahydro-quinoline, (c) 1-[3-(4-amidino-phenyl)propionyl]-5-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, (d) 1-[3-(4-amidino-phenyl)propionyl]-3-methyl-6-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, and, (e) 1-[3-(4-amidino-phenyl)propionyl]-6-(5-chloro-thien-2-ylsulphonamido)-1,2,3,4-tetrahydro-quinoline.Type: GrantFiled: December 9, 1999Date of Patent: October 9, 2001Assignee: Boehringer Ingelheim Pharm KGInventors: Armin Heckel, Rainer Soyka, Wolfgang Grell, Eric Haaksma, Klaus Binder, Rainer Zimmerman
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Patent number: 6265401Abstract: Compounds of formula (I) its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates can be used to prevent or treat diabetes caused by insulin resistance or impaired glucose tolerance or complications of diabetes caused by insulin resistance or impaired glucose tolerance. The compounds can also be used to reduce cholesterol, body weight, blood glucose, triglycerides and free fatty acids in the blood.Type: GrantFiled: May 27, 1998Date of Patent: July 24, 2001Assignees: Reddy-Cheminor, Inc., Dr. Reddy's Research FoundationInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Patent number: 6232310Abstract: The present invention relates to fused 1,4-thiazine-2-carbonitrile derivatives, compositions thereof and methods for preparing the compounds. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system.Type: GrantFiled: March 8, 2000Date of Patent: May 15, 2001Assignee: Novo Nordisk A/SInventors: Holger Claus Hansen, Tina Møller Tagmose, John Bondo Hansen
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Patent number: 6204380Abstract: Carboxylic acid ester derivatives of formula (1): wherein R is C1-C6 alkyl, R2 and R3 are independently hydrogen or C1-C3 alkyl, and Q is optionally substituted phenyl, can be easily converted by ring closing into pyridazin-3-one derivatives of formula (7): The carboxylic acids of formula (1) can be produced by reacting hydrazone compounds of formula (5): wherein R3 and Q are as defined above, with malonic acid monoester derivatives of formula (6): wherein R and R2 are as defined above, in the presence of a base.Type: GrantFiled: April 21, 1999Date of Patent: March 20, 2001Assignee: Sumitomo Chemical Company, LimitedInventor: Takashi Furukawa
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Patent number: 6200971Abstract: The bicyclic heterocyclic compounds are prepared by reaction of correspondingly substituted carboxylic acids with amines, in particular with phenylglycinolamine. The bicyclic heterocyclic compounds according to the invention are suitable as active compounds in medicaments, in particular in medicaments having an antiatherosclerotic action.Type: GrantFiled: October 18, 1999Date of Patent: March 13, 2001Assignee: Bayer AktiengesellschaftInventors: Richard Connell, Siegfried Goldmann, Ulrich Müller, Stefan Lohmer, Hilmar Bischoff, Dirk Denzer, Rudi Gr{umlaut over (u )}tzmann, Stefan Wohlfeil
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Patent number: 6191127Abstract: Compounds of Formula I wherein X and R1-6, are as defined herein, tautomeric forms thereof, and isomeric forms thereof, and salts thereof, are suitable for treating diseases that are induced by the action of nitrogen monooxide at pathological concentration. Such diseases include neurodegenerative diseases, inflammatory diseases, auto-immune diseases, and cardiovascular diseases.Type: GrantFiled: November 1, 1999Date of Patent: February 20, 2001Assignee: Schering AktiengesellschaftInventors: Peter Holscher, Hartmut Rehwinkel, Detlev Suelzle, Gerardine Burton, Margrit Hillmann, Iris Pribilla, David Daniel Davey
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N-((phenyl, benzodioxinyl or N-heteroarylpiperazinyl)alkyl)-N-(N-heteroaryl)substituted carboxamides
Patent number: 6127357Abstract: Piperazine derivatives of formula I ##STR1## and their pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents, particularly 5-HT.sub.1A antagonists and may be used, for example, as anxiolytics. In the formula A is C.sub.2-4 alkylene chain optionally substituted by lower alkyl, Z is oxygen or sulphur, R is hydrogen or lower alkyl, R.sup.1 is a mono or bicyclic aryl or heteroaryl radical, R.sup.2 is a mono or bicyclic heteroaryl radical and R.sup.3 is hydrogen or a specified radical such as lower alkyl, cycloalkyl, aryl, heteroaryl or optionally substituted amino.Type: GrantFiled: May 11, 1995Date of Patent: October 3, 2000Assignee: John Wyeth & Brother, Ltd.Inventors: Ian Anthony Cliffe, Howard Langham Mansell -
Patent number: 6071860Abstract: Compounds of the formula (I) and salts thereof ##STR1## where R.sup.1 to R.sup.5, A, Z, X, X', n and m are as defined in claim 1 are suitable as herbicides and plant growth regulators.Type: GrantFiled: February 6, 1997Date of Patent: June 6, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Wolfgang Giencke, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6069114Abstract: Compounds of the formula (I) and their salts ##STR1## in which R.sup.1 to R.sup.6, Y.sup.1, to Y.sup.2, Y.sup.3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepared analogously to known processes using intermediates of the formula (V) (cf. claim 6).Type: GrantFiled: February 25, 1997Date of Patent: May 30, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Klaus Lorenz, Klemens Minn, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6015774Abstract: Novel pyrazin-2-one derivatives of formula [1] are provided, ##STR1## which are useful as active ingredients of herbicides, wherein R.sup.1 is hydrogen or alkyl; R.sup.2 is haloalkyl; R.sup.3 is optionally substituted alkyl; alkenyl, or alkynyl; and Q is optionally substituted phenyl. Also provided are their use and intermediates for their production.Type: GrantFiled: March 20, 1998Date of Patent: January 18, 2000Assignee: Sumitomo Chemical Company, LimitedInventors: Akira Shuto, Hisayuki Hoshi, Yuzuru Sanemitsu
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Patent number: 6011031Abstract: Novel antidiabetic compounds, their tautomeric forms, their derivatives, their analogues, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them; methods for preparing the antidiabetic compounds and their uses.Type: GrantFiled: December 2, 1997Date of Patent: January 4, 2000Assignees: Dr. Reddy's Research Foundation, Reddy-Cheminor, Inc.Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Chennaveerappa Bajji, Shivaramayya Kalchar, Sekar Reddy Alla, Rajagopalan Ramanujam, Reeba Kannimel Vikramadithyan
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Patent number: 6011033Abstract: This invention relates to a phenylene derivative represented by the following formula (1) or a salt thereof and also to a medicine containing it as an effective ingredient. ##STR1## wherein R.sup.1 represents H or halogen; A represents --CH.dbd.CH--, --CH.dbd.N--, --N(R.sup.2)--, --O-- or --S--; W represents --CH.dbd.CH-- or --CH.sub.2 O--; X represents --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 N(R.sup.3)--, --CH.dbd.N--, --COO-- or --CONH--; Y represents ##STR2## B.sup.1 represents --C(R.sup.7)(R.sup.8)(CH.sub.2).sub.l --, --S(O).sub.m (CH.sub.2).sub.n -- or --CH.dbd.C(R.sup.9)--; B.sup.2 represents --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --; Z.sup.1 and Z.sup.2 each represents O or S; etc. The phenylene derivative or salt thereof has antileukotrienic action and antihistaminic action and is useful as a medicine such as an asthma preventive or curative.Type: GrantFiled: November 13, 1998Date of Patent: January 4, 2000Assignee: Kowa Co., Ltd.Inventors: Henk Timmerman, Mingqiang Zhang, Kazuhiro Onogi, Masahiro Tamura, Tsutomu Toma, Yasushi Wada
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Patent number: 6008218Abstract: This invention relates to An N-phenyl carbamate compound which is represented by the following formula (1): wherein R.sup.1 represents a hydrogen atom, an alkoxyalkyl group having 2 to 5 carbon atoms, an alkynyl group having 2 to 5 carbon atoms, an alkyl group having 1 to 4 carbon atoms, an alkenyl group having 2 to 5 carbon atoms, CO.sub.2 R.sup.6 or an alkoxy group having 1 to 4 carbon atoms;where R.sup.6 represents an alkyl group having 1 to 4 carbon atoms;R.sup.2 represents an alkyl group having 1 to 4 carbon atoms;R.sup.3 and R.sup.4 each independently represent a hydrogen atom or an alkyl group having 1 to 4 carbon atoms;R.sup.Type: GrantFiled: June 8, 1998Date of Patent: December 28, 1999Assignee: Ube Industries, Ltd.Inventors: Masanori Watanabe, Toshinobu Tanaka, Shin Suizu, Tadashi Murakami, Takehiko Asahara
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Patent number: 5981436Abstract: The invention relates to new substituted diazacyclohexanedi(thi)ones of the general formula (I) ##STR1## in which Q.sup.1, Q.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings given in the description,a process for their preparation, new intermediate products and their use as herbicides.Type: GrantFiled: April 29, 1998Date of Patent: November 9, 1999Assignee: Bayer AktiengesellschaftInventors: Mark-Wilhelm Drewes, Roland Andree, Otto Schallner, Hans-Joachim Santel, Markus Dollinger
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Patent number: 5919784Abstract: A compound of general formula (I): ##STR1## where A, X, R.sub.1, Y, n and Ar are defined in the description. Medicinal products containing the same are useful as D.sub.4 receptor Ligands.Type: GrantFiled: November 7, 1997Date of Patent: July 6, 1999Assignee: Adir Et CompagnieInventors: Daniel Lesieur, Pascal Carato, Jean-Paul Bonte, Patrick Depreux, Daniel-Henri Caignard, Mark Millan, Adrian Newman-Tancredi, Pierre Renard, Marie-Claire Rettori
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Patent number: 5885987Abstract: This invention relates to a phenylene derivative represented by the following formula (1) or a salt thereof and also to a medicine containing it as an effective ingredient. ##STR1## wherein R.sup.1 represents H or halogen; A represents --CH.dbd.CH--, --CH.dbd.N--, --N(R.sup.2)--, --O-- or --S--; W represents --CH.dbd.CH-- or --CH.sub.2 O--; X represents --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 N(R.sup.3)--, --CH.dbd.N--, --COO-- or --CONH--; Y represents ##STR2## B.sup.1 represents --C(R.sup.7)(R.sup.8)(CH.sub.2).sub.l, --S(O).sub.m (CH.sub.2).sub.n -- or --CH.dbd.C(R.sup.9)--; B.sup.2 represents --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --; Z.sup.1 and Z.sup.2 each represents O or S; etc. The phenylene derivative or salt thereof has antileukotrienic action and antihistaminic action and is useful as a medicine such as an asthma preventive or curative.Type: GrantFiled: November 18, 1997Date of Patent: March 23, 1999Assignee: Kowa Co., Ltd.Inventors: Henk Timmerman, Mingqiang Zhang, Kazuhiro Onogi, Masahiro Tamura, Tsutomu Toma, Yasushi Wada
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Patent number: 5883049Abstract: This invention provides with novel hydantoin derivatives, processes for preparing them, and herbicides containing said derivatives as active ingredient.Type: GrantFiled: August 18, 1997Date of Patent: March 16, 1999Assignees: Sagami Chemical Research Center, Kaken Pharmaceutical Co., Ltd.Inventors: Kenji Hirai, Tomoyuki Yano, Natsuko Okano, Sadayuki Ugai, Osamu Yamada
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Patent number: 5863924Abstract: The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT.sub.2B -antagonists. The invention is also directed to formulations and methods for treatment.Type: GrantFiled: May 20, 1997Date of Patent: January 26, 1999Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Lee Allen Flippin, Robert Greenhouse, Saul Jaime-Figueroa, Yanzhou Liu, Aubry Kern Miller, David George Putman, Klaus Kurt Weinhardt, Shu-Hai Zhao
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Patent number: 5830890Abstract: Compounds, useful as plant fungicides, having the formula (I): ##STR1## or a stereoisomer thereof, wherein A is CH or N, B is OCH.sub.3 or NHCH.sub.3, X is CH.sub.2, CH.sub.2 O, O or S, Y is R.sup.1 --C.dbd.C--R.sup.2 or R.sup.1 --CH--CH--R.sup.2 wherein R.sup.1 and R.sup.2 are independently H, halo, hydroxy, alkyl, haloalkyl, alkoxy, haloalkoxy, cyano, nitro, amino, mono- or dialkylamino, alkanoylamino, carboxy, alkoxycarbonyl, aminocarbonyl, mono- or di-alkylaminocarbonyl, alkylcarbonyloxy, optionally substituted aryl, optionally substituted aralkyl or optionally substituted aryloxy or R.sup.1 and R.sup.2 join to form with the carbon atoms to which they are attached an optionally substituted benzene ring, and Z is CH.sub.2, CHCH.sub.3, C(CH.sub.3).sub.2 or C.dbd.O.Type: GrantFiled: September 30, 1996Date of Patent: November 3, 1998Assignee: Zeneca LimitedInventors: Ian Richard Matthews, Paul John deFraine, Patrick Jelf Crowley, John Williams
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Patent number: 5750706Abstract: The compounds of formula I ##STR1## wherein R.sup.1 -R.sup.9, R.sup.15, A, X, Y, Z and n have the meaning given in the specification are active as protein kinase inhibitors and can be used as medicaments, particularly for the treatment of inflammatory skin disorders and alopecia.Type: GrantFiled: September 3, 1996Date of Patent: May 12, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Pierre Barbier, Isabelle Huber, Fernand Schneider, Josef Stadlwieser, Sven Taylor
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Patent number: 5739130Abstract: Heterotricyclic derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino,R.sup.2 is hydroxy, protected hydroxy, halogen, amino or protected amino,R.sup.3 is hydrogen or an organic group,R.sup.4 is hydrogen or lower alkyl,R.sup.8 is hydrogen or lower alkyl, and--Z-- is --O-- or a group of the formula: ##STR2## (in which n is 0, 1 or 2), and pharmaceutically acceptable salts thereof which are useful as a medicament.Type: GrantFiled: September 4, 1996Date of Patent: April 14, 1998Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Kiyoshi Tsuji, Katsuya Nakamura, Glen W. Spears
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Patent number: 5728692Abstract: A compound represented by the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, each represents a hydrogen atom or a lower alkyl group having from 1 to 4 carbon atoms and a salt thereof, and an antirheumatic agent containing, as an active ingredient, at least one of these compounds.Type: GrantFiled: June 15, 1995Date of Patent: March 17, 1998Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Nobuhiro Ohi, Hiroshi Suzuki
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Patent number: 5726307Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: December 15, 1994Date of Patent: March 10, 1998Assignee: Merck & Co., Inc.Inventors: William R. Schoen, Matthew J. Wyvratt
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Patent number: 5719141Abstract: Compounds of the formula I ##STR1## in which R.sub.1 is arylamino, N-aryl-N-(lower alkoxy-lower alkyl)-amino, N-aryl-N-aryl-lower alkyl-amino or heterocyclyl bonded via a ring carbon atom, X is a carbonyl or methylene group, R.sub.2 and R.sub.3 independently of one another are hydrogen or lower alkyl or, together with the carbon atom with which they are bonded, are a cycloalkylidene radical, R.sub.4 is hydrogen, lower alkyl, lower alkanoyl or lower alkoxycarbonyl, R.sub.5 is hydroxyl, lower alkanoyloxy or lower alkoxycarbonyloxy, R.sub.6 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cycloalkyl-lower alkyl, aryl-lower alkyl or heteroaryl-lower alkyl having 5 to 7 ring atoms in the heteroaryl ring and R.sub.7 is hydrogen or lower alkyl, or R.sub.6 and R.sub.7, together with the carbon atom with which they are bonded, are a cydoalkylidene radical and R.sub.Type: GrantFiled: September 8, 1995Date of Patent: February 17, 1998Assignee: Novartis CorporationInventors: Vittorio Rasetti, Heinrich Rueger, Jurgen Klaus Maibaum, Robert Mah, Markus Grutter, Nissim Claude Cohen
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Patent number: 5712225Abstract: The present invention relates to oxa(di)azabicyclic and thia(di)azabicyclic compounds, a method for their preparation and their use as herbicides.Type: GrantFiled: February 28, 1996Date of Patent: January 27, 1998Assignees: E. I. du Pont de Nemours and Company, Degussa AktiengesellschaftInventors: Wonpyo Hong, Matthias Schafer, Thomas Martin Stevenson
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Patent number: 5661107Abstract: Compounds of the formula ##STR1## wherein m represents 1 or 2, X represents O, S, CH.sub.2 or substituted CH.sub.2, R.sub.1 -R.sub.4 represent hydrogen or substituted or unsubstituted hydrocarbon groups, and Q represents a substituted phenyl group. These compounds are useful as herbicides and are active in small doses with high selectivity between useful plants and weeds.Type: GrantFiled: April 13, 1995Date of Patent: August 26, 1997Assignee: Degussa AktiengesellschaftInventors: Matthias Schafer, Karlheinz Drauz
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Patent number: 5643932Abstract: A superoxide radical inhibitor containing, as an effective ingredient, an azole derivative represented by the general formula (1), ##STR1## [wherein R.sup.1 represents a phenyl group which may have 1-3 lower alkoxy groups as substituent(s) on the phenyl ring, a phenyl group having a lower alkylenedioxy group, or the like; R.sup.2 represents a hydrogen atom, a phenyl group, a halogen atom, a lower alkoxycarbonyl group, a lower alkyl group, an amino-lower alkyl group which may have a lower alkyl group as a substituent, a dihydrocarbostyril group, or the like; R.sup.3 represents a group of the formula, ##STR2## (R.sup.4B represents a hydroxyl group, a carboxy group, a lower alkenyl group or a lower alkyl group. m represents 0, 1 or 2); X represents a sulfur atom or an oxygen atom] or a salt thereof.Type: GrantFiled: May 19, 1995Date of Patent: July 1, 1997Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Masatoshi Chihiro, Hajime Komatsu, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5599815Abstract: Compounds represented by the formula (I) and pharmacologically acceptable salts thereof: ##STR1## These compounds have little extrapyramidal effect and thus are effective as an anti-psychotic agent having few side effects.Type: GrantFiled: December 20, 1994Date of Patent: February 4, 1997Assignee: Meiji Seika Kabushiki KaishaInventors: Yoshimasa Fukuda, Toshiro Sasaki, Yuuko Nakatani, Yasuyuki Ichimaru, Taiichiro Imanishi
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Patent number: 5597819Abstract: New benzothiazine derivatives corresponding to the general formula I: ##STR1## in which: X represents halogen,n represents 0, 1, or 2,B represents the following formula: ##STR2## in which: R.sub.1 & R.sub.2 together with the carbons to which they are attached form a 6-carbon-atom aromatic ring which is optionally substituted by a group X' representing halogen, andY represents the radical --(SO.sub.2).sub.x --Alk--Z, x, Alk, and Z are as defined in the specification;as well as their possible stereoisomers, epimers, N-oxides and pharmaceutically-acceptable acid or base addition salts; and medicinal products containing the same, useful in the treatment of inflammatory disorders requiring an inhibitor of cytokines.Type: GrantFiled: February 13, 1995Date of Patent: January 28, 1997Assignee: Adir Et CompagnieInventors: Jean-Daniel Brion, Anne-Marie Chollet, Luc Demuynck, Lucy De Montarby, Yves Rolland, Jacqueline Bonnet, Pietro Ghezzi, Armel Fradin
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Patent number: 5583135Abstract: wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino,R.sup.2 is hydroxy, protected hydroxy, halogen, amino or protected amino,R.sup.3 is hydrogen or an organic group,R.sup.4 R is hydrogen or lower alkyl,R.sup.8 is hydrogen or lower alkyl, and--Z-- is --O-- or a group of the formula: ##STR2## (in which n is 0, 1 or 2), and pharmaceutically acceptable salts thereof which are useful as a medicament.Type: GrantFiled: July 26, 1994Date of Patent: December 10, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Kiyoshi Tsuji, Katsuya Nakamura, Glen W. Spears
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Patent number: 5547952Abstract: This invention relates to the compounds of the formula [I] which are useful for the treatment of cataracts, and the synthetic intermediates of the formula [II], ##STR1## wherein R.sup.1 is hydroxy which can be protected by a protective group;R.sup.2 is lower alkyl;R.sup.3 is hydrogen, lower alkyl, hydroxy, which can be protected by a protective group, or lower alkoxy, and the said lower alkyl can be substituted by hydroxy, which can be protected by a protective group, amino or lower alkylamino;R.sup.4 is tetrazolyl, phosphonol or lower alkyl ester thereof, or sulfonyl or lower alkyl ester thereof, andA is alkylene.Type: GrantFiled: November 30, 1994Date of Patent: August 20, 1996Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Yoichi Kawashima, Atsutoshi Ota, Yuko Morikawa, Hiroyuki Mibu
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Patent number: 5530126Abstract: The disclosure herein relates to a process for the preparation of compounds according to Formula N ##STR1## which comprises using a compound of Formula M ##STR2## as starting material for alkylation to said compounds of Formula N in an inert solvent at temperatures within the range of 0.degree.-200.degree. C. whereinR.sub.1 is C.sub.1-5 alkyl;R.sub.2 is C.sub.1-5 haloalkyl;R.sub.3 is halogen;R.sub.5 is hydrogen or halogen;q is 0-2;R.sub.28 and R.sub.30 are independently an alkyl, alkenyl or alkynyl radical having up to 5 carbon atoms or said radicals substituted with a ##STR3## radical; X is O, S(O).sub.m, NR.sub.19 or CR.sub.20 R.sub.21 ;Y is O, S(O).sub.m or NR.sub.22 ;m is 0-2 andR.sub.13 and R.sub.19 -R.sub.22 are hydrogen or an R.sub.28 member.The above compounds are useful as herbicides.Type: GrantFiled: January 31, 1994Date of Patent: June 25, 1996Assignee: Monsanto CompanyInventors: Scott S. Woodard, Bruce C. Hamper, Kurt Moedritzer, Michael D. Rogers, Deborah A. Mischke, Gerard A. Dutra
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Patent number: 5521145Abstract: There is disclosed an iminothiazoline derivative of the general formula: ##STR1## wherein R.sub.1 is (halo)alkyl, (halo)alkenyl, (halo)alkynyl or the like; R.sub.2 is (halo)alkyl, optionally substituted aryl, formyl, cyano or the like; R.sub.3 is hydrogen, (halo)alkyl or the like; and Q is a group of the particular general formula. Also disclosed are a herbicide containing a herbicidally effective amount of the iminothiazoline derivative and a method for controlling unfavorable weeds, which includes applying a herbicidally effective amount of the iminothiazoline derivative to an area where the unfavorable weeds grow or will grow.Type: GrantFiled: April 3, 1995Date of Patent: May 28, 1996Assignee: Sumitomo Chemical Company, Ltd.Inventors: Minoru Takano, Masayuki Enomoto, Kazuo Saito, Satoru Kizawa
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Patent number: 5496817Abstract: This invention offers the compounds of the formula [I]which are useful for treatment of cataract. ##STR1## wherein R.sup.1 is hydroxy which can be protected by a protective group;R.sup.2 is lower alkyl;R.sup.3 is hydrogen, lower alkyl, hydroxy, which can be protected by a protective group, or lower alkoxy, and the said lower alkyl can be substituted by hydroxy, which can be protected by a protective group, amino or lower alkylamino;R.sup.4 is carboxy which can be converted to ester or amide, andA is alkylene.Type: GrantFiled: April 22, 1994Date of Patent: March 5, 1996Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Yoichi Kawashima, Atsutoshi Ota, Hiroyuki Mibu
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Patent number: 5496815Abstract: Thiazine derivatives of the formula [I]: ##STR1## wherein R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are each hydrogen atom; R.sup.3 is hydrogen atom or a halogen atom; X is sulfur atom; R.sup.6 is naphthyl, a sulfur-containing monoheterocyclic group or a substituted phenyl; Z.sup.1 is two hydrogen atoms; Z.sup.2 is oxygen atom; A is a lower alkylene; R.sup.7 and R.sup.8 are the same or different and are each i) hydrogen atom, ii) a lower alkyl, iii) a lower alkenyl, iv) a lower alkynyl, or v) a lower alkyl which is substituted by a substituted phenyl, or both form together with the adjacent nitrogen atom a nitrogen-containing monoheterocyclic group; except for the compound [I] wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each hydrogen atom, X is sulfur atom, R.sup.6 is a halogenophenyl, Z.sup.1 is two hydrogen atoms, Z.sup.2 is oxygen atom, A is a lower alkylene, R.sup.7 and R.sup.Type: GrantFiled: October 28, 1993Date of Patent: March 5, 1996Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Masakatsu Ozeki, Shin-ichi Kodato, Kousuke Yasuda, Yukitsuka Kudo, Kayoko Maeda
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Patent number: 5440035Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: October 25, 1994Date of Patent: August 8, 1995Assignee: Zeneca Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
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Patent number: 5416084Abstract: Compounds characterized generally as benzo-fused thiomorpholinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a benzo-fused thiomorpholinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sub.q --C.ident.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: February 22, 1994Date of Patent: May 16, 1995Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, Robert E. Manning
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Patent number: 5416065Abstract: Thiadiazabicyclooctanes of formula I ##STR1## wherein Z is oxygen or sulfur;R.sub.53 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.54 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.6 alkenyloxy, C3-C6alkynyioxy, hydroxy or C.sub.1 -C.sub.6 haloalkoxy; orR.sub.53 and R.sub.54, together with the carbon atom to which they are bonded, form an unsubstituted 3-, 4-, 5- or 6-membered saturated ring;W is a group of formulae W.sub.1 to W.sub.Type: GrantFiled: November 18, 1993Date of Patent: May 16, 1995Assignee: Ciba-Geigy CorporationInventors: Hans-Georg Brunner, Hans Moser, Georg Pissiotas
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Patent number: 5411958Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a benzothiomorpholinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: February 22, 1994Date of Patent: May 2, 1995Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5401745Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebal and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.Type: GrantFiled: March 19, 1993Date of Patent: March 28, 1995Assignee: Merck & Co., Inc.Inventors: Scott W. Bagley, Prasun K. Chakravarty, Anna Chen, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Elizabeth M. Naylor, James R. Tata, Thomas F. Walsh, David L. Williams, Jr.
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Patent number: RE37555Abstract: The invention relates to a method of producing a mixture of a quaternary ammonium compound, fatty acid, fatty acid ester and tertiary amine salt in situ which is a highly functional mixture that is manufactured in a single step reaction whereby quaternization is completed without the aid of solvents, especially flammable solvents. The single step reaction process eliminates separate blending of individual components. The compositions obtained can be used as fabric softeners, in modified clays, as hair treating compounds and as disinfectants.Type: GrantFiled: June 11, 1999Date of Patent: February 19, 2002Assignee: Goldschmidt Chemical CompanyInventors: Jeannene A. Ackerman, Michael Miller, David E. Whittlinger
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Patent number: RE37556Abstract: A superoxide radical inhibitor containing, as an effective ingredient, an azole derivative represented by the general formula (1), [wherein R1 represents a phenyl group which may have 1-3 lower alkoxy groups as substituent(s) on the phenyl ring, a phenyl group having a lower alkylenedioxy group, or the like; R2 represents a hydrogen atom, a phenyl group, a halogen atom, a lower alkoxycarbonyl group, a lower alkyl group, an amino-lower alkyl group which may have a lower alkyl group as a substituent, a dihydrocarbostyril group, or the like; R3 represents a group of the formula, (R4B represents a hydroxyl group, a carboxy group, a lower alkenyl group or a lower alkyl group, m represents 0, 1 or 2); X represents a sulfur atom or an oxygen atom] or a salt thereof.Type: GrantFiled: February 8, 1999Date of Patent: February 19, 2002Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Masatoshi Chihiro, Hajime Komatsu, Michiaki Tominaga, Yoichi Yabuuchi