Chalcogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/243)
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Patent number: 6605631Abstract: Compounds of the general formula I where the index and the substituents have the following meanings: n is 0 or 1 to 4; X is O or S; Y is a five-membered heteroaromatic ring; R1 is nitro; cyano; halogen; alkyl; haloalkyl; alkoxy; haloalkoxy; alkylthio; phenyl or phenoxy; R2 is hydrogen; alkyl, alkenyl or alkynyl; or a saturatedy,or unsaturated ring which, in addition to carbon atoms, can also contain hetero atoms as ring members are described.Type: GrantFiled: September 30, 1999Date of Patent: August 12, 2003Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Wassilios Grammenos, Herbert Bayer, Reinhard Doetzer, Hartmann Koenig, Klaus Oberdorf, Hubert Sauter, Horst Wingert, Gisela Lorenz, Eberhard Ammermann, Volker Harries
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Publication number: 20030146420Abstract: Organic dye molecular materials prepared by coupling existing organic chromophore molecules to benzene or carbazole derivatives and nonlinear optical polymeric compounds having polyimide repeating units coupled with the organic dye molecular material are provided.Type: ApplicationFiled: February 27, 2002Publication date: August 7, 2003Inventors: Jung Yun Do, Myung Hyun Lee, Seung Koo Park, Jung Jin Ju, Suntak Park
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Patent number: 6599925Abstract: This invention provides compounds which act as inhibitors of plasminogen activator inhibitor-1 (PAI-1) of the formula: wherein: R, R1, R2, and R3 are H, alkyl, cycloalkyl, —CH2-(cycloalkyl), alkanoyl, halo, hydroxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, perfluoroalkyl, alkoxy, amino, —NH(alkyl), —N(alkyl)2, or perfluoroalkoxy; R4 is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl, aryl, —CH2R5, —CH(OH)R5, —C(O)R5, —CH(SH)R5, or —C(S)R5; R5 is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl; R6 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, alkylaryl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl; n is an integer of 0-6; A is COOH, or an acid mimic; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds to treatType: GrantFiled: June 18, 2002Date of Patent: July 29, 2003Assignee: WyethInventors: Hassan Mahmoud Elokdah, Geraldine Ruth McFarlane, Scott Christian Mayer, David LeRoy Crandall
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Publication number: 20030114505Abstract: The present invention relates to novel isoxazole and thiazole compounds having an excellent lysophosphatidic acid (LPA) receptor antagonistic activity represented by general formula [1] or salts thereof: 1Type: ApplicationFiled: August 19, 2002Publication date: June 19, 2003Inventors: Akihiro Ueno, Rika Nagao, Tomoko Watanabe, Hideo Ohta, Mikio Yagi
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Publication number: 20030107027Abstract: A nonlinear optical chromophore having the formula D-&pgr;-A, wherein &pgr; is a &pgr; bridge including a thiophene ring having oxygen atoms bonded directly to the 3 and 4 positions of the thiophene ring, D is a donor, and A is an acceptor.Type: ApplicationFiled: November 22, 2002Publication date: June 12, 2003Inventors: Diyun Huang, Baoquan Chen
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Publication number: 20030100590Abstract: 1 The invention relates to 3-(4,5-dihydroisoxazole-5-yl)benzoylpyrazole of the formula (I), wherein the variables have the following meanings: R1, R1 represent hydrogen, nitro, halogen, cyano, alkyl, halogenalkyl, alkoxy, halogenalkoxy, alkylthio, halogenalkylthio, alkylsulfinyl, halogenalkylsulfinyl, alkylsulfonyl or halogenalkylsulfonyl; hydrogen, R3 represents halogen or alkyl; R4 represents hydrogen or alkyl; R5, R6 represent hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylthio, dialkylamino, phenyl R3 or carbonyl, wherein the latter six groups can be substituted; R7 represents halogen, cyano, hydroxy, alkyl, halogenalkyl, alkoxy, halogenalkoxy, alkylthio, halogenalkylthio, alkylsulfinyl, halogenalkylsulfinyl, alkylsulfonyl, halogenalkylsulfonyl, amino, alkylamino, dialkylamino, dialkoxymethyl, hydroxyiminoalkyl, alkoxyiminoalkyl or optionally substituted carbonyl; R11 represents optionally substituted pyrazole that is bound in the 4 position and that carries a hydroxy group or a derivative theType: ApplicationFiled: June 19, 2002Publication date: May 29, 2003Inventors: Ernst Baumann, Wolfgang von Deyn, Steffen Kudis, Klaus Langemann, Guido Mayer, Ulf Misslitz, Ulf neidlein, Helmut Walter, Karl-Otto Westphalen, Matthias Witschel
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Patent number: 6569888Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt, in vivo hydrolysable ester, or an N—C1-6alkyl or N,N-di-(C1-6alkyl)amide thereof, where X is CH2 or SO2; R1 is an aryl optionally substituted by alkyl, alkenyl, alkynyl, halo, haloalkyl including perhaloalkyl such as trifluoromethyl, mercapto, alkoxy, haloalkoxy, alkenyloxy, alkynyloxy, hydroxyalkoxy, alkoxyalkoxy, alkanoyl, alkanoyloxy, cyano, nitro, amino, mono- or di-alkyl amino, oximino, sulphonamido, carbamoyl, mono or dialkylcarbamoyl or S(O)mR21 where m is defined above and R21 is hydrocarbyl; R4 is a group OR15 or S(O)qR15, where q is 0, 1 or 2 and R15 is a hydrogen-containing alkyl group substituted by at least one functional group as defined below, or an aryl group which is optionally substituted by one or more functional groups as defined below; and R2, R3, R5, R6 and R7 are specified organic groups.Type: GrantFiled: September 12, 2001Date of Patent: May 27, 2003Assignee: AstraZeneca ABInventors: Jason Kettle, Alan W Faull
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Publication number: 20030092740Abstract: The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: 1Type: ApplicationFiled: May 16, 2002Publication date: May 15, 2003Inventors: Robert A. Galemmo, Celia Dominguez, John M. Fevig, Qi Han, Patrick Y. Lam, Donald J.P. Pinto, James R. Pruitt, Mimi L. Quan
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Patent number: 6545154Abstract: The invention relates to a process for preparing N-(5-amino-2-cyano-4-fluoro-phenyl)-sulphonamides in which, in a first step, 2-amino-4,5-difluoro-benzonitrile is reacted with sulphonyl halides in the presence of an acid acceptor and in the presence of a diluent at temperatures between 0° C. and 150° C. and, in a second step, the N-(2-cyano-4,5-difluoro-phenyl)-sulphonamides and/or N-(2-cyano-4,5-difluoro-phenyl)-sulphonimides obtained in the first step are as pure substances or as mixtures with ammonia in the presence of a diluent reacted at a temperature between 100° C. and 200° C. The invention furthermore relates to novel intermediates of the process.Type: GrantFiled: September 5, 2001Date of Patent: April 8, 2003Assignee: Bayer AktiengesellschaftInventors: Achim Hupperts, Mark Wilhelm Drewes, David Erdman, Reinhard Lantzsch
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Publication number: 20030004193Abstract: 1-Heterocycle substituted diarylamines, methods of making and using them, and compositions containing them.Type: ApplicationFiled: July 23, 2002Publication date: January 2, 2003Inventors: Stephen Douglas Barrett, Alexander James Bridges, Haile Tecle, Lu-Yan Zhang
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Publication number: 20020165398Abstract: The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like.Type: ApplicationFiled: April 19, 2002Publication date: November 7, 2002Inventors: Lone Jeppesen, Henrik Sune Andersen, Ole Hvilsted Olsen, Luke Milburn Judge, Daniel Dale Holsworth, Farid Bakir, Frank Urban Axe, Yu Ge
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Publication number: 20020094984Abstract: This invention describes isoxazolinone derivatives which possess antibacterial activity and are useful in the treatment of bacterial diseases.Type: ApplicationFiled: February 13, 2001Publication date: July 18, 2002Inventors: Lawrence B. Snyder, Zhizhen Zheng
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Patent number: 6420349Abstract: This invention describes isoxazolinone compounds which possess antibacterial activity and are useful in the treatment of bacterial diseases.Type: GrantFiled: February 13, 2001Date of Patent: July 16, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Lawrence B. Snyder, Zhizhen Zheng
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Publication number: 20020091270Abstract: Thienylsulfonamides and their pharmaceutically acceptable derivatives, pharmaceutical compositions, articles of manufacture, combinations, lyophilized powders and methods for the treatment of endothelin diseases using these formulations and sulfonamides are provided. A process of preparing an alkali metal salt of a hydrophobic sulfonamide is provided. The process includes the step of dissolving a free sulfonamide in an organic solvent in the presence of a saturated alkali metal salt solution and recovering the formed sulfonamide salt from the organic phase.Type: ApplicationFiled: December 20, 2001Publication date: July 11, 2002Inventors: Chengde Wu, Natalie Blok, Timothy Kogan, Karin Keller, Patricia Woodard
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Patent number: 6395724Abstract: Disclosed are multibinding compounds which inhibit cyclooxygenase-2 (COX-2), an enzyme which catalyzes the first committed step in the biosynthesis of prostaglandins. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to COX-2. The multibinding compounds of this invention are useful in the treatment inflammation, pain, fever and the like.Type: GrantFiled: June 7, 1999Date of Patent: May 28, 2002Assignee: Advanced Medicine, Inc.Inventors: J. Kevin Judice, Deborah L. Higgins, John H. Griffin
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Publication number: 20020055505Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: November 1, 2001Publication date: May 9, 2002Inventors: David John Anderson, Jackson B. Hester
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Patent number: 6384066Abstract: Novel sulphonyltriazole derivatives of the formula in which Hal represents fluorine, chlorine or bromine, R1 represents hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkylaminocarbonyl, optionally substituted phenyl, optionally substituted phenoxy or represents optionally substituted heterocyclyl and R2 represents alkyl or represents optionally substituted heterocyclyl or represents a radical of the formula in which R3 represents halogen, alkyl or phenyl, R4 represents hydrogen or alkyl and R5 represents alkyl or optionally substituted phenyl, or R4 and R5 together with the nitrogen atom to which they are attached form a heterocyclic ring which may be substituted and which may also contain an additional heteroatom, a process for preparing these substances and their use for controlling undesirable microorganisms.Type: GrantFiled: March 20, 2001Date of Patent: May 7, 2002Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Stefan Hillebrand, Klaus Stenzel, Ulrike Wachendorff-Neumann
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Publication number: 20020035137Abstract: Compounds of formula (I) 1Type: ApplicationFiled: July 31, 2001Publication date: March 21, 2002Inventors: Gang Liu, Bruce G. Szczepankiewicz, Zhonghua Pei, Zhili Xin, Thorsten K. Oost, David A. Janowick
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Patent number: 6358983Abstract: The present invention relates to carboxylic acid derivatives of the formula I the substituents having the meanings explained in the description, preparation and use as endothelin receptor antagonists.Type: GrantFiled: April 27, 2000Date of Patent: March 19, 2002Assignee: Abbott LaboratoriesInventors: Wilhelm Amberg, Rolf Jansen, Heinz Hillen, Stefan Hergenröder, Manfred Raschack, Liliane Unger
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Patent number: 6355672Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.Type: GrantFiled: January 30, 2001Date of Patent: March 12, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
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Patent number: 6344471Abstract: The present invention relates to novel 2-aminocarbonyl-5(2H)-isoxazolones as selective ligands of a high-affinity binding site of diisopropyl fluorophosphate (DFP) on brain membranes for the prophylaxis and treatment of disorders of the central nervous system, in particular cognitive disorders, depression, schizophrenia and anxiety.Type: GrantFiled: February 27, 2001Date of Patent: February 5, 2002Assignee: Bayer AktiengesellschaftInventors: Stephan Lensky, Bernd Riedl, Chantal Fürstner, Jens Ergüden, Frank Böss, Bernhard Schmidt, Franz-Josef van der Staay, Werner Schröder, Joachim Schuhmacher, Delf Schmidt
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Publication number: 20020006943Abstract: Compounds of the formula: 1Type: ApplicationFiled: April 12, 2001Publication date: January 17, 2002Inventors: Theodore O. Johnson , Jr., Ye Hua, Hiep T. Luu, Peter S. Dragovich
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Patent number: 6331637Abstract: N-alkyl, N-alkenyl, N-alkynyl, N-aryl and N-fused bicyclo or tricyclo thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, (phenyl) and (phenoxy)thienylsulfonamides, (phenyl) and (phenoxy)furylsulfonamides, and (phenyl) and (phenoxy)pyrrolylsulfonamides and methods of using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.Type: GrantFiled: March 22, 1999Date of Patent: December 18, 2001Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Chengde Wu, Bore Gowda Raju, Timothy Kogan, Adam Kois, Erik Joel Verner, Rosario Silvestre Castillo, Venkatachalapathi Yalamoori, Vitukudi Narayanaiyengar Balaji
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Patent number: 6316474Abstract: Benzimidazoles, substituted in the 2-position by substituted benzyl groups or heteroaryl groups are effective as NMDA NR2B antagonists and are useful for relieving pain.Type: GrantFiled: October 25, 2000Date of Patent: November 13, 2001Assignee: Merck & Co., Inc.Inventors: John A. McCauley, Cory R. Theberge, Nigel J. Liverton, David A. Claremon, Christopher F. Claiborne
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Patent number: 6313312Abstract: Compounds of formula (I), their salts and prodrugs thereof, where the substituents are as defined herein are disclosed as opiate binding agents useful in the treatment of opiate-mediated conditions. Also described are processes for making such substances.Type: GrantFiled: December 20, 1999Date of Patent: November 6, 2001Assignee: Pfizer INCInventors: Bernard Joseph Banks, Robert James Crook, Stephen Paul Gibson, Graham Lunn, Alan John Pettman
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Patent number: 6310206Abstract: The invention relates to a process for preparing N-(5-amino-2-cyano-4-fluoro-phenyl)-sulphonamides in which, in a first step, 2-amino-4,5-difluoro-benzonitrile is reacted with sulphonyl halides in the presence of an acid acceptor and in the presence of a diluent at temperatures between 0° C. and 150° C. and, in a second step, the N-(2-cyano-4,5-difluoro-phenyl)-sulphon-amides and/or N-(2-cyano-4,5-difluoro-phenyl)-sulphonamides obtained in the first step are as pure substances or as mixtures with ammonia in the presence of a diluent reacted at a temperature between 100° C. and 200° C. The invention furthermore relates to novel intermediates of the process.Type: GrantFiled: January 18, 2000Date of Patent: October 30, 2001Assignee: Bayer AktiengesellschaftInventors: Achim Hupperts, Mark Wilhelm Drewes, David Erdman, Reinhard Lantzsch
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Patent number: 6303569Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms.Type: GrantFiled: August 21, 1998Date of Patent: October 16, 2001Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Yun H. Choe, Annapurna Pendri
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Patent number: 6297198Abstract: Compounds defined by the generic formula or an agriculturally acceptable salt thereof, wherein the letter R represents a lower alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, or alkenyl, each of which is optionally substituted, the symbol R1 represents a lower alkyl, haloalkyl or phenyl group, optionally substituted, X and Y are each independently a hydrogen, hydroxyl, halogen, cyano, alkylsulfenyl, alkylsulfinyl, alkylsulfonyl, acyloxy, carbamoyloxy, alkylsulfonyloxy, amino, substituted amino, acylamino, sulfamoyloxy, sulfamyl, or X and Y can be combined to be ═O, —S(CH2)mS— and —O(CH2)mO—, in which m is 2 or 3, the symbol Ar represents an aromatic ring moiety optionally substituted with from one to four groups and wherein two substituents on adjacent positions of the aromatic ring may be taken together with the two atoms to which they are attached, to form a 5- to 7-membered ring optionally substituted, and the letter Z represents —S—, —SO— oType: GrantFiled: April 29, 1997Date of Patent: October 2, 2001Assignee: Syngenta Participations AGInventor: Shy-Fuh Lee
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Patent number: 6291507Abstract: A pharmaceutical composition which comprises a compound of formula (I) or a pharmaceutically acceptable salt, ester or amide thereof, which is an inhibitor of monocyte chemoattractant protein-1, and wherein A and B form an optionally substituted alkylene chain so as to form a ring with the carbon atoms to which they are attached; X is CH2 or SO2, R1 is an optionally substituted aryl or heteroaryl ring; R2 is a specified organic group such as carboxy, and R3 is hydrogen or a specified organic group; in combination with a pharmaceutically acceptable carrier. Certain compounds of formula (I) are novel and are claimed as such.Type: GrantFiled: July 26, 2000Date of Patent: September 18, 2001Assignee: Astrazeneca UK LimitedInventors: Alan W Faull, Andrew J Barker, Jason G Kettle
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Patent number: 6265575Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.Type: GrantFiled: August 5, 1999Date of Patent: July 24, 2001Assignee: Eli Lilly and CompanyInventors: Kenneth Jeff Thrasher, Kenneth Lee Hauser, Alan David Palkowitz
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Patent number: 6255251Abstract: Compounds of formula 1 wherein R1 and R2 are independently C1-C8alkyl, are suitable for use as herbicides.Type: GrantFiled: October 2, 2000Date of Patent: July 3, 2001Assignee: Syngenta Crop Protection, Inc.Inventors: Alain De Mesmaeker, Jürgen Schaetzer, Walter Kunz
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Patent number: 6251921Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.Type: GrantFiled: May 14, 1999Date of Patent: June 26, 2001Assignee: Eli Lilly and CompanyInventors: Jolie Anne Bastian, Nickolay Yuri Chirgadze, Michael Lyle Denney, Matthew Joseph Fisher, Robert James Foglesong, Richard Waltz Harper, Mary George Johnson, Valentine Joseph Klimkowski, Todd Jonathan Kohn, Ho-Shen Lin, Michael Patrick Lynch, Jefferson Ray McCowan, Alan David Palkowitz, Michael Enrico Richett, Daniel Jon Sall, Gerald Floyd Smith, Kumiko Takeuchi, Jennifer Marie Tinsley, Minsheng Zhang
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Patent number: 6239283Abstract: The invention is a process for the preparation of cyclic-sulfur fluorine containing oxazolidinone antibacterial agents which utilizes the important tetrahydrothiopyran-o-fluorinated carbamate of formula (IV)Type: GrantFiled: January 31, 2000Date of Patent: May 29, 2001Assignee: Pharmacia & Upjohn CompanyInventor: James R. Gage
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Patent number: 6232317Abstract: Imino-substituted phenyl compounds of the formula I where the substituents have the following meanings: z is a group A or B where # denotes the bond with the phenyl ring and Ra is halogen, alkyl or alkoxy; y is halogen, alkyl, haloalkyl or alkoxy; n is 0, 1 or 2, it being possible for the radicals Y to be different if n=2; R1 is halogen, haloalkyl or alkoxy; R2 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl; R3 is cyano, alkyl, haloalkyl, alkoxy, cycloalkoxy, alkoxyalkyl; unsubstituted or substituted cycloalkyl, aryl, aryloxy or arylmethylene, heteroaryl, heterocyclyl, C(R3a)═N—OR3b or C(R3a)═CR3cR3d, where R3a, R3b, R3c, R3d independently of one another are hydrogen, alkyl or unsubstituted or substituted phenyl, processes for their preparation, and their use.Type: GrantFiled: January 27, 2000Date of Patent: May 15, 2001Assignee: BASF AktiengesellschaftInventors: Wassilios Grammenos, Herbert Bayer, Hubert Sauter, Thomas Grote, Andreas Gypser, Bernd Müller, Arne Ptock, Franz Röhl, Norbert Götz, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6200999Abstract: (3-Alkoxyisoxazol-4-yl)-substituted 2-amino carboxylic acid derivatives and sulfur analogues thereof having general formula (I) or (II), wherein R1 is hydrogen, alkyl, alkenyl, alkynyl, cycloalk(en)yl, cycloalk(en)yl-alk(en/yn)yl or optionally substituted phenyl-alk(en/yn)yl; A is a bond or a hydrocarbon spacer group; B is a group —CRa(NRbRc)—COOR5 wherein Ra-Rc are independently hydrogen or alkyl, and R5 is defined as R1 or pivaloyloxymethyl, or B is a group of Formula (III), wherein R2, R3 and R4 are independently selected from hydrogen, a non-aromatic hydrocarbon group, phenyl- and thienyl-alkyl, and a hetero aliphatic group, or R3 and R4 are connected, thereby forming an alkylene, alkenylene or alkynylene group, or R4 and R2 are connected in order to form an alkylene, alkenylene or alkynylene group, optionally substituted with hydroxy or methyl, or to form CH2—O—CH2; E is COOR6, where R6 is defined as R5, or E is a tetrazolyl or triazolyl; X is OType: GrantFiled: May 20, 1999Date of Patent: March 13, 2001Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Klaus Peter Bøgesø, Povl Krogsgaard-Larsen, Sibylle Moltzen Lenz
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Patent number: 6194575Abstract: The present invention relates to a process for the preparation of compounds of the formula (I) by reacting compounds of the formula (II) in which Het, R1, R2 and R4 are as defined in the description, with urea.Type: GrantFiled: September 21, 1999Date of Patent: February 27, 2001Assignee: Bayer AktiengesellschaftInventors: Detlef Wollweber, Wolfgang Krämer, Eric Rivadeneira
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Patent number: 6187929Abstract: A dye represented by the following formula (1); Formula (1) wherein A represents an acidic nucleus, L1, L2 and L3 represent a methine group, n represents 0, 1 or 2, Z represents a nonmetalic atom group necessary to form a heterocyclic group by bonding with a nitrogen atom included in the above formula (1), Y represents a substituent represented by the following formula (2) or a heterocyclic group; Formula (2) wherein R1 and R2 represent an alkyl group, and R1 and R2 may form a ring by bonding with each other, R3 represents a hydrogen atom or an electron withdrawing group: said dye represented by the above formula (1) has at least one carboxy group or one alkylsulfonamide group in an aromatic ring portion of its molecular structure.Type: GrantFiled: June 14, 1999Date of Patent: February 13, 2001Assignee: Konica CorporationInventors: Mitsuhiro Fukuda, Motoaki Sugino, Akira Onishi
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Patent number: 6187944Abstract: Acrylonitrile compounds having pesticidal activity of formula (I) and salts thereof. wherein Q is Y is ═C(R4)— or ═N—, R1 is alkyl, haloalkyl, etc., each of R2 and R3 is halogen, alkyl which may be substituted, alkenyl which may be substituted, etc., R4 is hydrogen, halogen, alkyl or haloalkyl, 1 is from 1 to 4, m is from 0 to 5, n is from 0 to 3, q is from 0 to 4, when 1 is 2 or more, a plurality of R2 may be the same or different, when each of m, n and q is 2 or more, a plurality of R3 may be the same or different.Type: GrantFiled: August 16, 1999Date of Patent: February 13, 2001Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Toru Koyanagi, Yuji Nakamura, Masayuki Morita, Koji Sugimoto, Tsuyoshi Ikeda, Munekazu Ogawa
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Patent number: 6159995Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6159673Abstract: An oxonol compound is represented by the following formula (I): ##STR1## in which Z is an atomic group that forms a cyclic amide ring; each of W.sup.1 and W.sup.2 independently is an atomic group that forms an acidic nucleus ring; and M is a cation. Other oxonol compounds, a light-sensitive material containing an oxonol compound and a process for the synthesis of an oxonol compound are also disclosed.Type: GrantFiled: January 20, 1999Date of Patent: December 12, 2000Assignee: Fuji Photo Film Co., Ltd.Inventors: Junji Nishigaki, Yasuaki Deguchi
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Patent number: 6153752Abstract: Process for the preparation of heterocycles by reacting 2-substituted acetals of malondialdehyde with a reactant selected from hydroxylamines and their salts, hydrazines and their salts, formamid, amidines and their salts, guanidines and their salts, aminoguanidines and their salts, nitroguanidine and their salts, O-alkyl-isoureas and their salts, O-cycloalkyl-isoureas and their salts, O-aralkyl-isoureas and their salts, O-aryl-isoureas and their salts, S-alkyl-isothioureas, S-cycloalkyl-isothioureas, S-aralkyl-isothioureas, S-arylisothioureas, S-alkyl-isothiouronium salts, S-cycloalkyl-isothiouronium salts, S-aralkyl-isothiouronium salts, S-aryl-isothiuronium salts, thiourea and urea.Type: GrantFiled: January 28, 2000Date of Patent: November 28, 2000Assignee: Creanova, Inc.Inventors: Frank Bauer, Chitoor Subramaniam
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Patent number: 6150303Abstract: Substituted 3-phenylisoxazolines I, and their salts and enol ethers, are described as herbicides ##STR1## where X.dbd.--O--, --S--, --N(R.sup.9)--;R.sup.1 .dbd.CN, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylsulfonyl;R.sup.2 .dbd.H or unsubstituted or substituted C.sub.1 -C.sub.6 -alkyl, (C.sub.1 -C.sub.6 -alkyl)carbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.2 -C.sub.6 -alkenyl, (C.sub.2 -C.sub.6 -alkenyl)carbonyl, C.sub.2 -C.sub.6 -alkynyl, (C.sub.2 -C.sub.6 -alkynyl)carbonyl;R.sup.3 .dbd.H, halogen;R.sup.4 .dbd.CN, halogen, C.sub.1 -C.sub.3 -haloalkyl;R.sup.5 .dbd.H, CN, halogen, C.sub.1 -C.sub.3 -haloalkyl;R.sup.6 .dbd.H, CN, halogen, C.sub.1 -C.sub.3 -haloalkyl or unsubstituted or substituted C.sub.1 -C.sub.6 -alkoxy;R.sup.7 .dbd.CN, halogen;R.sup.8 in position .alpha., R.sup.7 in this case being in position .beta., or in position .beta., R.sup.7 in this case being in position .alpha., is1) H, OH, SH, CN, NO.sub.2, halogen, C.sub.1 -C.sub.Type: GrantFiled: January 21, 2000Date of Patent: November 21, 2000Assignee: BASF AktiengesellschaftInventors: Olaf Menke, Markus Menges, Gerhard Hamprecht, Robert Reinhard, Peter Schafer, Cyrill Zagar, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
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Patent number: 6130225Abstract: The invention relates to novel substituted p-trifluoromethylphenyluracils of the general formula (I) in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each as defined in the description, to a process for their preparation and to their use as herbicides.Type: GrantFiled: February 2, 1999Date of Patent: October 10, 2000Assignee: Bayer AktiengesellschaftInventors: Mark-Wilhelm Drewes, Roland Andree, Markus Dollinger
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Patent number: 6114328Abstract: This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: November 25, 1997Date of Patent: September 5, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: John Wityak, Chu-Biao Xue, Thais Motria Sielecki-Dzurdz, Richard Eric Olson, William Frank Degrado, Gary Avonn Cain, Douglas Guy Batt, Donald Pinto, Munir Alwan Hussain, Shaker Ahmed Mousa
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Patent number: 6107491Abstract: Diketopyrrolopyrroles of formula I ##STR1## wherein R.sub.1 is a radical of formula II--Y--X--Z--Q (II),whereinY is --CR.sub.3 R.sub.4, --SO.sub.2 --, --CO--, --Si(Hal).sub.2 --, --POHal--, wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen or C.sub.1 -C.sub.4 alkyl, and Hal is halogen,X is an unsubstituted or substituted carbocylic or heterocyclic arylene group,Z is a single bond, uninterrupted linear or branched C.sub.1 -C.sub.30 alkylene, or linear or branched C.sub.2 -C.sub.30 alkylene which is interrupted once or more than once by a hetero atom, --CH.dbd.CH--,--C.tbd.C--, --N.dbd.CH--, --CH.dbd.N-- or --NH--, or is C.sub.5 -C.sub.12 cycloalkylene,Q is a polyreactive functional group, andR.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR2## or R.sub.1, and R.sub.7 is hydrogen or C.sub.1 -C.sub.Type: GrantFiled: January 26, 1999Date of Patent: August 22, 2000Assignee: Ciba Specialty Chemicals CorporationInventor: Sameer Eldin
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Patent number: 6107320Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R.sup.1, R.sup.2 and R.sup.3 are each independently(a) hydrogen, except that R.sup.1 is other than hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g) --C(O)H or --C(O)R.sup.6 ;(h) --CO.sub.2 H or --CO.sub.2 R.sup.6 ;(i) --SH, --S(O).sub.n R.sup.6, --S(O).sub.m --OH, --S(O).sub.m --OR.sup.6, --O--S(O).sub.m --R.sup.6, --O--S(O).sub.m OH or --O--S(O).sub.m --OR.sup.6 ;(j) --Z.sup.4 --NR.sup.7 R.sup.8 ; or(k) --Z.sup.4 --N(R.sup.11)--Z.sup.5 --NR.sup.9 R.sup.10 ;and the remaining symbols are as defined in the specification.Type: GrantFiled: January 11, 1996Date of Patent: August 22, 2000Assignee: Bristol-Myers Squibb Co.Inventors: Natesan Murugesan, John T. Hunt
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Patent number: 6096895Abstract: Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful as fungicides ##STR1## In said formula, E is a ring system selected from certain 5- to 12-membered monocyclic and fused bicyclic aromatic heterocyclic ring systems, or an optionally substituted naphthalene ring as defined in the disclosure;A is O; S; N; NR.sup.5 ; or CR.sup.14 ;G is C or N; provided that when G is C, then A is O, S or NR.sup.5 and the floating double bond is attached to G; and when G is N, then A is N or CR.sup.14 and the floating double bond is attached to A;W is O; S; NH; N(C.sub.1 -C.sub.6 alkyl); or NO(C.sub.1 -C.sub.6 alkyl);X is OR.sup.1 ; S(O).sub.m R.sup.1 ; or halogen;R.sup.1 is C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl; C.sub.2 -C.sub.6 alkenyl; C.sub.2 -C.sub.6 haloalkenyl; C.sub.2 -C.sub.6 alkynyl; C.sub.2 -C.sub.6 haloalkynyl; C.sub.3 -C.sub.6 cycloalkyl; C.sub.2 -C.sub.4 alkylcarbonyl; or C.sub.2 -C.sub.4 alkoxycarbonyl;R.sup.2 is H; C.sub.1 -C.sub.6 alkyl; C.Type: GrantFiled: November 13, 1997Date of Patent: August 1, 2000Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, Dilon Jancey Daniel, Deborah Ann Frasier, Michael Henry Howard, Jr., Gerard Michael Koether, Morris Padgett Rorer
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Patent number: 6080768Abstract: Compounds of the formula: ##STR1## wherein the variables are as defined in the specification. These compounds are useful in the treatment of arterial hypertension and heart failure, of renal insufficiency, of peripheral arteriopathies and of cerebrovascular insufficiencies.Type: GrantFiled: October 17, 1997Date of Patent: June 27, 2000Assignee: Zambon Group S.p.A.Inventors: Stefania Montanari, Paolo Cavalleri, Francesco Santangelo
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Patent number: 6057319Abstract: The invention encompasses the novel compound of formula (I) useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of formula (I).Type: GrantFiled: October 2, 1998Date of Patent: May 2, 2000Assignee: Merck Frosst Canada & Co.Inventors: Cameron Black, Serge Leger, Petpiboon Prasit, Zhaoyin Wang, Pierre Hamel, Yongxin Han, Gregory Hughes
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Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten