Double Bonded Divalent Chalcogen Containing Patents (Class 544/52)
  • Patent number: 6448246
    Abstract: 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: Grant
    Filed: May 25, 2000
    Date of Patent: September 10, 2002
    Assignee: Neurogen Corporation
    Inventors: Guolin Cai, Gang Liu, Pamela A. Albaugh
  • Publication number: 20020115853
    Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: 1
    Type: Application
    Filed: February 12, 2002
    Publication date: August 22, 2002
    Inventors: Puwen Zhang, Reinhold H. W. Bender, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
  • Patent number: 6410484
    Abstract: 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: Grant
    Filed: October 30, 2000
    Date of Patent: June 25, 2002
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Minoru Takano, Hirofumi Mishima
  • Patent number: 6339155
    Abstract: 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: Grant
    Filed: November 13, 2000
    Date of Patent: January 15, 2002
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Minoru Takano, Hirofumi Mishima
  • Patent number: 6339084
    Abstract: 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: Grant
    Filed: July 19, 2000
    Date of Patent: January 15, 2002
    Assignee: Clariant Finance (BVI) Limited
    Inventors: Bansi Lal Kaul, Bruno Piastra
  • Publication number: 20020004596
    Abstract: A process for preparing symmetrical or asymmetrical trans-thiazineindigo pigments of the formula (1) 1
    Type: Application
    Filed: June 21, 2001
    Publication date: January 10, 2002
    Applicant: Clariant GmbH
    Inventors: Petra Maria Rothe, Leonhard Unverdorben, Bruno Piastra
  • Patent number: 6333413
    Abstract: 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: Grant
    Filed: July 17, 2000
    Date of Patent: December 25, 2001
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Takashi Furukawa
  • Patent number: 6303542
    Abstract: 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: Grant
    Filed: August 18, 2000
    Date of Patent: October 16, 2001
    Assignee: Rohm and Haas Company
    Inventors: Bin Li, Adam Chi-Tung Hsu
  • Patent number: 6300342
    Abstract: 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: Grant
    Filed: December 9, 1999
    Date of Patent: October 9, 2001
    Assignee: Boehringer Ingelheim Pharm KG
    Inventors: Armin Heckel, Rainer Soyka, Wolfgang Grell, Eric Haaksma, Klaus Binder, Rainer Zimmerman
  • Patent number: 6265401
    Abstract: 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: Grant
    Filed: May 27, 1998
    Date of Patent: July 24, 2001
    Assignees: Reddy-Cheminor, Inc., Dr. Reddy's Research Foundation
    Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rajagopalan Ramanujam, Ranjan Chakrabarti
  • Patent number: 6232310
    Abstract: 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: Grant
    Filed: March 8, 2000
    Date of Patent: May 15, 2001
    Assignee: Novo Nordisk A/S
    Inventors: Holger Claus Hansen, Tina Møller Tagmose, John Bondo Hansen
  • Patent number: 6204380
    Abstract: 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: Grant
    Filed: April 21, 1999
    Date of Patent: March 20, 2001
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Takashi Furukawa
  • Patent number: 6200971
    Abstract: 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: Grant
    Filed: October 18, 1999
    Date of Patent: March 13, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Richard Connell, Siegfried Goldmann, Ulrich Müller, Stefan Lohmer, Hilmar Bischoff, Dirk Denzer, Rudi Gr{umlaut over (u )}tzmann, Stefan Wohlfeil
  • Patent number: 6191127
    Abstract: 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: Grant
    Filed: November 1, 1999
    Date of Patent: February 20, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: Peter Holscher, Hartmut Rehwinkel, Detlev Suelzle, Gerardine Burton, Margrit Hillmann, Iris Pribilla, David Daniel Davey
  • Patent number: 6127357
    Abstract: 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: Grant
    Filed: May 11, 1995
    Date of Patent: October 3, 2000
    Assignee: John Wyeth & Brother, Ltd.
    Inventors: Ian Anthony Cliffe, Howard Langham Mansell
  • Patent number: 6071860
    Abstract: 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: Grant
    Filed: February 6, 1997
    Date of Patent: June 6, 2000
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Wolfgang Giencke, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 6069114
    Abstract: 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: Grant
    Filed: February 25, 1997
    Date of Patent: May 30, 2000
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Klaus Lorenz, Klemens Minn, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 6015774
    Abstract: 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: Grant
    Filed: March 20, 1998
    Date of Patent: January 18, 2000
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Akira Shuto, Hisayuki Hoshi, Yuzuru Sanemitsu
  • Patent number: 6011031
    Abstract: 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: Grant
    Filed: December 2, 1997
    Date of Patent: January 4, 2000
    Assignees: 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
  • Patent number: 6011033
    Abstract: 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: Grant
    Filed: November 13, 1998
    Date of Patent: January 4, 2000
    Assignee: Kowa Co., Ltd.
    Inventors: Henk Timmerman, Mingqiang Zhang, Kazuhiro Onogi, Masahiro Tamura, Tsutomu Toma, Yasushi Wada
  • Patent number: 6008218
    Abstract: 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: Grant
    Filed: June 8, 1998
    Date of Patent: December 28, 1999
    Assignee: Ube Industries, Ltd.
    Inventors: Masanori Watanabe, Toshinobu Tanaka, Shin Suizu, Tadashi Murakami, Takehiko Asahara
  • Patent number: 5981436
    Abstract: 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: Grant
    Filed: April 29, 1998
    Date of Patent: November 9, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Mark-Wilhelm Drewes, Roland Andree, Otto Schallner, Hans-Joachim Santel, Markus Dollinger
  • Patent number: 5919784
    Abstract: 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: Grant
    Filed: November 7, 1997
    Date of Patent: July 6, 1999
    Assignee: Adir Et Compagnie
    Inventors: Daniel Lesieur, Pascal Carato, Jean-Paul Bonte, Patrick Depreux, Daniel-Henri Caignard, Mark Millan, Adrian Newman-Tancredi, Pierre Renard, Marie-Claire Rettori
  • Patent number: 5885987
    Abstract: 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: Grant
    Filed: November 18, 1997
    Date of Patent: March 23, 1999
    Assignee: Kowa Co., Ltd.
    Inventors: Henk Timmerman, Mingqiang Zhang, Kazuhiro Onogi, Masahiro Tamura, Tsutomu Toma, Yasushi Wada
  • Patent number: 5883049
    Abstract: This invention provides with novel hydantoin derivatives, processes for preparing them, and herbicides containing said derivatives as active ingredient.
    Type: Grant
    Filed: August 18, 1997
    Date of Patent: March 16, 1999
    Assignees: Sagami Chemical Research Center, Kaken Pharmaceutical Co., Ltd.
    Inventors: Kenji Hirai, Tomoyuki Yano, Natsuko Okano, Sadayuki Ugai, Osamu Yamada
  • Patent number: 5863924
    Abstract: 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: Grant
    Filed: May 20, 1997
    Date of Patent: January 26, 1999
    Assignee: 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
  • Patent number: 5830890
    Abstract: 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: Grant
    Filed: September 30, 1996
    Date of Patent: November 3, 1998
    Assignee: Zeneca Limited
    Inventors: Ian Richard Matthews, Paul John deFraine, Patrick Jelf Crowley, John Williams
  • Patent number: 5750706
    Abstract: 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: Grant
    Filed: September 3, 1996
    Date of Patent: May 12, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Pierre Barbier, Isabelle Huber, Fernand Schneider, Josef Stadlwieser, Sven Taylor
  • Patent number: 5739130
    Abstract: 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: Grant
    Filed: September 4, 1996
    Date of Patent: April 14, 1998
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masaaki Matsuo, Kiyoshi Tsuji, Katsuya Nakamura, Glen W. Spears
  • Patent number: 5728692
    Abstract: 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: Grant
    Filed: June 15, 1995
    Date of Patent: March 17, 1998
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Nobuhiro Ohi, Hiroshi Suzuki
  • Patent number: 5726307
    Abstract: 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: Grant
    Filed: December 15, 1994
    Date of Patent: March 10, 1998
    Assignee: Merck & Co., Inc.
    Inventors: William R. Schoen, Matthew J. Wyvratt
  • Patent number: 5719141
    Abstract: 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: Grant
    Filed: September 8, 1995
    Date of Patent: February 17, 1998
    Assignee: Novartis Corporation
    Inventors: Vittorio Rasetti, Heinrich Rueger, Jurgen Klaus Maibaum, Robert Mah, Markus Grutter, Nissim Claude Cohen
  • Patent number: 5712225
    Abstract: The present invention relates to oxa(di)azabicyclic and thia(di)azabicyclic compounds, a method for their preparation and their use as herbicides.
    Type: Grant
    Filed: February 28, 1996
    Date of Patent: January 27, 1998
    Assignees: E. I. du Pont de Nemours and Company, Degussa Aktiengesellschaft
    Inventors: Wonpyo Hong, Matthias Schafer, Thomas Martin Stevenson
  • Patent number: 5661107
    Abstract: 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: Grant
    Filed: April 13, 1995
    Date of Patent: August 26, 1997
    Assignee: Degussa Aktiengesellschaft
    Inventors: Matthias Schafer, Karlheinz Drauz
  • Patent number: 5643932
    Abstract: 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: Grant
    Filed: May 19, 1995
    Date of Patent: July 1, 1997
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Masatoshi Chihiro, Hajime Komatsu, Michiaki Tominaga, Yoichi Yabuuchi
  • Patent number: 5599815
    Abstract: 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: Grant
    Filed: December 20, 1994
    Date of Patent: February 4, 1997
    Assignee: Meiji Seika Kabushiki Kaisha
    Inventors: Yoshimasa Fukuda, Toshiro Sasaki, Yuuko Nakatani, Yasuyuki Ichimaru, Taiichiro Imanishi
  • Patent number: 5597819
    Abstract: 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: Grant
    Filed: February 13, 1995
    Date of Patent: January 28, 1997
    Assignee: Adir Et Compagnie
    Inventors: Jean-Daniel Brion, Anne-Marie Chollet, Luc Demuynck, Lucy De Montarby, Yves Rolland, Jacqueline Bonnet, Pietro Ghezzi, Armel Fradin
  • Patent number: 5583135
    Abstract: 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: Grant
    Filed: July 26, 1994
    Date of Patent: December 10, 1996
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masaaki Matsuo, Kiyoshi Tsuji, Katsuya Nakamura, Glen W. Spears
  • Patent number: 5547952
    Abstract: 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: Grant
    Filed: November 30, 1994
    Date of Patent: August 20, 1996
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Yoichi Kawashima, Atsutoshi Ota, Yuko Morikawa, Hiroyuki Mibu
  • Patent number: 5530126
    Abstract: 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: Grant
    Filed: January 31, 1994
    Date of Patent: June 25, 1996
    Assignee: Monsanto Company
    Inventors: Scott S. Woodard, Bruce C. Hamper, Kurt Moedritzer, Michael D. Rogers, Deborah A. Mischke, Gerard A. Dutra
  • Patent number: 5521145
    Abstract: 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: Grant
    Filed: April 3, 1995
    Date of Patent: May 28, 1996
    Assignee: Sumitomo Chemical Company, Ltd.
    Inventors: Minoru Takano, Masayuki Enomoto, Kazuo Saito, Satoru Kizawa
  • Patent number: 5496817
    Abstract: 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: Grant
    Filed: April 22, 1994
    Date of Patent: March 5, 1996
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Yoichi Kawashima, Atsutoshi Ota, Hiroyuki Mibu
  • Patent number: 5496815
    Abstract: 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: Grant
    Filed: October 28, 1993
    Date of Patent: March 5, 1996
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Masakatsu Ozeki, Shin-ichi Kodato, Kousuke Yasuda, Yukitsuka Kudo, Kayoko Maeda
  • Patent number: 5440035
    Abstract: 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: Grant
    Filed: October 25, 1994
    Date of Patent: August 8, 1995
    Assignee: Zeneca Inc.
    Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
  • Patent number: 5416084
    Abstract: 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: Grant
    Filed: February 22, 1994
    Date of Patent: May 16, 1995
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5416065
    Abstract: 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: Grant
    Filed: November 18, 1993
    Date of Patent: May 16, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans-Georg Brunner, Hans Moser, Georg Pissiotas
  • Patent number: 5411958
    Abstract: 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: Grant
    Filed: February 22, 1994
    Date of Patent: May 2, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5401745
    Abstract: 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: Grant
    Filed: March 19, 1993
    Date of Patent: March 28, 1995
    Assignee: 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.
  • Patent number: RE37555
    Abstract: 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: Grant
    Filed: June 11, 1999
    Date of Patent: February 19, 2002
    Assignee: Goldschmidt Chemical Company
    Inventors: Jeannene A. Ackerman, Michael Miller, David E. Whittlinger
  • Patent number: RE37556
    Abstract: 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: Grant
    Filed: February 8, 1999
    Date of Patent: February 19, 2002
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Masatoshi Chihiro, Hajime Komatsu, Michiaki Tominaga, Yoichi Yabuuchi