Chalcogen Bonded Directly To Ring Carbon Of The Oxadiazole Ring Patents (Class 548/144)
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Publication number: 20100267710Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 28, 2010Publication date: October 21, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Publication number: 20100261717Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 28, 2010Publication date: October 14, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Patent number: 7812341Abstract: The present invention relates to a compound having an oxadiazole ring structure having a substituted pyridyl group connected thereto, represented by the following general formula (1). According to the present invention, it becomes possible to provide an organic compound having excellent characteristic of high stability in a thin film state, and the emission efficiency and durability of conventional organic EL devices can be remarkably improved.Type: GrantFiled: March 25, 2005Date of Patent: October 12, 2010Assignee: Hodogaya Chemical Co., Ltd.Inventors: Tetsuzo Miki, Makoto Nagaoka, Shuichi Hayashi, Yoshio Taniguchi, Musubu Ichikawa
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Publication number: 20100197696Abstract: The invention relates to compounds of formula wherein Het, A1, A2, A3, A4, D, W, T, Q, Y, X1, X2, R1, R2, R3, R4, k and m are as defined hereinabove, and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, to a process for the preparation of and to the use of those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, to pesticidal compositions in which the active ingredient has been selected from those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in agrochemically usable salt form, to a process for the preparation of and to the use of those compositions, to plant propagation material treated with those compositions, to a method of controlling pests, to intermediates and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, for the preparation of those compounds, E/Z isomers, mType: ApplicationFiled: April 8, 2010Publication date: August 5, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Roger Graham Hall, Stephan Trah, Werner Zambach, Juraj Tuleja
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Publication number: 20100168110Abstract: The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.Type: ApplicationFiled: June 2, 2008Publication date: July 1, 2010Applicant: TORRENT PHARMACEUTICALS LTD.Inventors: Laxmikant Chhipa, Shitalkumar Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, C. Dutt, Vijay Chauthaiwale
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Patent number: 7723362Abstract: The invention relates to compounds of formula wherein Het, A1, A2, A3, A4, D, W, T, Q, Y, X1, X2, R1, R2, R3, R4, k and m are as defined hereinabove, and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, to a process for the preparation of and to the use of those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, to pesticidal compositions in which the active ingredient has been selected from those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in agrochemically usable salt form, to a process for the preparation of and to the use of those compositions, to plant propagation material treated with those compositions, to a method of controlling pests, to intermediates and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, for the preparation of those compounds, E/Z isomers, mType: GrantFiled: January 7, 2005Date of Patent: May 25, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: Roger Graham Hall, Stephan Trah, Werner Zambach, Juraj Tuleja
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Publication number: 20100069381Abstract: For the purpose of providing a GSK-3? inhibitor containing an oxadiazole compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3?-related pathology or disease, the present invention provides a GSK-3? inhibitor containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.Type: ApplicationFiled: August 2, 2007Publication date: March 18, 2010Inventor: Fumio Itoh
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Patent number: 7638539Abstract: The present invention is directed to 1,3,4-oxadiazalones, i.e., the compounds of formula I and their pharmaceutically acceptable salts, stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. The compounds of this invention are modulators of PPARdelta and therefore useful as pharmaceutical agents, especially for the treatment of demyelinating diseases and disorders of fatty acid metabolism and glucose utilization such as multiple scleroses.Type: GrantFiled: September 27, 2006Date of Patent: December 29, 2009Assignees: Aventis Pharmaceuticals Inc., Sanofi-Aventis Deutschland GmbHInventors: Daniel G. McGarry, Jochen Goerlitzer, Stefanie Keil, Karen Chandross, Jean Merrill, Wolfgang Wendler
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Publication number: 20090275621Abstract: The present invention is directed to 1,3,4-oxadiazalones, compounds of formula I and their pharmaceutically acceptable salts stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. The compounds of this invention are modulators of PPARdelta and therefore useful as pharmaceutical agents, especially for the treatment of demyelinating diseases and disorders of fatty acid metabolism and glucose utilization.Type: ApplicationFiled: July 20, 2009Publication date: November 5, 2009Applicants: AVENTIS PHARMACEUTICALS INC., SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Daniel G. MCGARRY, Jochen GOERLITZER, Stefanie KEIL, Karen CHANDROSS, Jean MERRILL, Wolfgang WENDLER
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Publication number: 20090247591Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain or other conditions.Type: ApplicationFiled: March 25, 2009Publication date: October 1, 2009Applicant: Grunenthal GmbHInventors: Saskia Zemolka, Bert Nolte, Klaus Linz, Derek John Saunders, Wolfgang Schroder, Wemer Englberger, Fritz Theil, Hans Schick, Jens Kaufmann, Julian Gebauer, Helmut Sonnenschein
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Patent number: 7576109Abstract: The present invention is directed to 1,3,4-oxadiazolones, compounds of formula I and their pharmaceutically acceptable salts stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. The compounds of this invention are modulators of PPARdelta and therefore useful as pharmaceutical agents, especially for the treatment of demyelinating diseases and disorders of fatty acid metabolism and glucose utilization.Type: GrantFiled: September 26, 2006Date of Patent: August 18, 2009Assignees: Aventis Pharmaceuticals Inc., Sanofi-Aventis Deutschland GmbHInventors: Daniel G. McGarry, Karen Chandross, Jean Merrill, Jochen Goerlitzer, Stefanie Keil, Wolfgang Wendler, Patrick Bernardelli
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Publication number: 20090124669Abstract: Novel compounds for the prevention and treatment of dermatological disorders with an immunoallergic, hyperproliferative and inflammatory component, and a method of producing such compounds. The compounds are bioisosteres of substances with avenanthramide structures.Type: ApplicationFiled: February 21, 2006Publication date: May 14, 2009Inventor: Carlo Ghisalberti
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Publication number: 20090091234Abstract: A salt molten at room temperature that does not contain any organic solvent, excelling in stability; and a display device that is improved in the durability in high-temperature environment by virtue of the use thereof. There is provided a salt molten at room temperature characterized by being composed of a silver salt and any of compounds of the following general formula (I) or general formula (II).Type: ApplicationFiled: April 6, 2006Publication date: April 9, 2009Applicant: KONICA MINOLTA HOLDINGS, INC.Inventor: Noriyuki Kokeguchi
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Patent number: 7511149Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.Type: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Publication number: 20080306125Abstract: Compounds of formula. wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.Type: ApplicationFiled: February 2, 2007Publication date: December 11, 2008Inventors: Michael Gregory Bell, Michael James Genin, Peter Ambrose Lander, Lindsay Scott Stelzer, Robert Anthony Doti, Francisco Javier Agejas-Chicharro, Ana Belen Bueno Melendo, Peter Rudolph Manninen, Jason Matthew Ochoada, Quanrong Shen, Alan M. Warshawsky, Tianwei Ma, Ryan Edward Stites
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Patent number: 7439242Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.Type: GrantFiled: April 15, 2002Date of Patent: October 21, 2008Assignee: Amgen Inc.Inventors: Jonathan B. Houze, Lawrence R. McGee, Steven Marc Rubenstein
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Publication number: 20080242860Abstract: The present invention relates to a silver halide color photographic light-sensitive material wherein at least one of light-sensitive silver halide emulsion layers includes a silver halide emulsion having a silver chloride content of at least 95 mol % and a silver iodide content of 0.05 mol % to 0.75 mol % and/or a silver bromide content of 0.05 mol % to 4.00 mol % and further at least one compound represented by the following formula (I): X-(L)n-Y ??Formula (I) wherein X represents a group adsorptive to a silver halide, L represents a divalent connecting group comprising one of an atom and an atomic group including at least one of a carbon atom, a nitrogen atom, a sulfur atom and an oxygen atom, Y denotes a reducible group and n denotes an integer of 0 or 1.Type: ApplicationFiled: June 3, 2008Publication date: October 2, 2008Applicant: FUJIFILM CORPORATIONInventors: Atsushi Matsunaga, Tadashi Inaba, Shinichi Ichikawa
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Publication number: 20080214620Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl; carbocyclyl which may optionally be substituted by alkyl; alkenyl; alkynyl, provided a triple bond is not adjacent to X; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl in which heterocyclyl may optionally be substituted by alkyl; -alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; aryl; heteroaryl; or H; X represents S or NR3; R3 represents H or C1-4 alkyl.Type: ApplicationFiled: November 28, 2007Publication date: September 4, 2008Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck, Mirko Buchholz, Andre J. Niestroj
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Patent number: 7390804Abstract: An N-containing five-membered ring compound of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of inflammatory diseases, diseases induced by apoptosis, diseases induced by disorders of immune responses, autoimmune diseases, diseases induced by decomposition of proteins which compose organism, shock, circulatory system disorders, blood coagulation systems disorders, malignant tumors, acquired immune deficiency syndrome (AIDS) and AIDS-related complex (ARC), parasitic diseases, nerve degeneration diseases, pulmonary disorders, bone resorption diseases, endocrinesthenia, etc.Type: GrantFiled: December 22, 2004Date of Patent: June 24, 2008Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Iori Itagaki
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Patent number: 7217832Abstract: The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.Type: GrantFiled: February 23, 2006Date of Patent: May 15, 2007Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kosuke Okazaki, Masahiko Uchida, Harunobu Mukaiyama, Hiroaki Kobayashi, Yuichiro Kai, Hideki Takeuchi, Kenji Yokoyama, Yoshihiro Terao, Yuji Hoyano, Hiroaki Shiohara, Norihiko Kikuchi
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Patent number: 7211668Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is sulfur or oxygen; J is nitrogen or C—R?; R1, R? is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy or a functional group having one of following general formulae: wherein A1, A2, A3, A4, A5, is independently selected from H, halogen such as F, Cl, Br or I, CF3, alkyl, preferably C1–C4 alkyl, nitro, nitrile, alkoxy, preferably C1–C4 alkoxy, halogenated (such as F, Cl, Br and I) alkyl, preferably halogenated C1–C4 alkyl, halogenated (such as F, Cl, Br and I) alkoxy, preferably halogenated C1–C4 alkoxy, phenyl, and halogenated (such as F, Cl, Br and I phenyl; R2 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucType: GrantFiled: April 6, 2004Date of Patent: May 1, 2007Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Sung Hee Lee
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Patent number: 7208509Abstract: This invention relates to novel heterocyclic compounds of formula I wherein R1—R4, X1 and X2 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I, pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient and processes to prepare compounds of formula I.Type: GrantFiled: March 23, 2004Date of Patent: April 24, 2007Assignee: Roche Palo Alto LLCInventors: James Patrick Dunn, Steven Swallow, Zachary Kevin Sweeney
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Patent number: 7205321Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is selected from the group consisting of hydrogen, substituted or unsubstituted group selected from C1–C8 alkyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, and C3–C6 cycloalkylaryl-C0-2-alkyl; W is O or S; X is an optionally substituted C1–C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S; Y is C, O, S, NH or a single bond; E is C(R3)(R4)A or AType: GrantFiled: November 13, 2002Date of Patent: April 17, 2007Assignee: Eli Lilly and CompanyInventors: Richard Duane Johnston, Nathan Bryan Mantlo, Richard Craig Thompson
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Patent number: 7196199Abstract: The present invention relates to a phenoxypropylamine compound of the formula (I) wherein each symbol is as defined in the specification, an optically active compound thereof or a pharmaceutically acceptable salt thereof and hydrates thereof, which simultaneously show selective affinity for and antagonistic activity against 5-HT1A receptor, as well as 5-HT reuptake inhibitory activity, and can be used as antidepressants quick in expressing an anti-depressive effect.Type: GrantFiled: December 22, 2003Date of Patent: March 27, 2007Assignee: Mitsubishi Pharma CorporationInventors: Akira Nishiyama, Masahiro Bougauchi, Takanobu Kuroita, Masanori Minoguchi
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Patent number: 7166624Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: December 18, 2003Date of Patent: January 23, 2007Assignee: SmithKline Beecham CorporationInventors: Jack Dale Leber, Mei Li, Jinhwa Lee, Kelly M. Aubart, Siegfried B. Christensen, IV
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Patent number: 7144901Abstract: An oxadiazole derivative of formula (I) and a non-toxic salt thereof, wherein R is hydrogen, alkyl, CycA, etc.; AA1 is a single bond, amino acid residue, etc.; AA2 is a single bond, amino acid residue, etc.; R7 and R8 are hydrogen, alkyl, etc.; R9 is hydrogen, alkyl, etc. R10 is hydrogen, alkyl, etc.).Type: GrantFiled: December 1, 2000Date of Patent: December 5, 2006Assignee: ONO Pharmaceutical Co.,Ltd.Inventors: Kazuyuki Ohmoto, Iori Itagaki
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Patent number: 7115639Abstract: The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation.Type: GrantFiled: June 14, 2002Date of Patent: October 3, 2006Assignee: Applied Research Systems ARS Holding N.V.Inventors: Matthias Schwarz, Anna Quattropani, Patrick Page, Russell J. Thomas, Vincent Pomel
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Patent number: 6919331Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.Type: GrantFiled: December 4, 2002Date of Patent: July 19, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Kuo-Long Yu, Xiangdong Wang, Yaxiong Sun, Christopher Cianci, Jan Willem Thuring, Keith Combrink, Nicholas Meanwell, Yi Zhang, Rita L. Civiello
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Patent number: 6908937Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which X represents hydrogen, halogen or alkyl, m represents integers from 3 to 10, n represents 0, 1 or 2, Het represents the groups where R1 represents hydrogen; mercapto; optionally halogen-substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl or alkenyl; optionally substituted aryl; or optionally substituted heterocyclyl, Y represents oxygen or sulphur, and R2 represents hydrogen, alkyl or optionally substituted aryl, and to processes for their preparation and to their use as pesticides.Type: GrantFiled: July 2, 2001Date of Patent: June 21, 2005Assignee: Bayer Cropscience AGInventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
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Patent number: 6900233Abstract: A substituted 3-phenyl-5-alkoxy-3H-(1,3,4)-oxadiazol-2-one, compound of formula 1, wherein R1, R2, R3, R4 and R5 are as defined herein, pharmaceutical composition comprising the compound and use of the compound for inhibiting pancreatic lipase, or the prophylaxis or treatment of obesity are described.Type: GrantFiled: February 27, 2003Date of Patent: May 31, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Karl Schoenafinger, Stefan Petry, Günter Müller, Armin Bauer, Hubert Otto Heuer
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Patent number: 6852716Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.Type: GrantFiled: February 10, 2003Date of Patent: February 8, 2005Assignee: Pfizer IncInventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Jason K. Myers, Vincent E. Groppi, Jr.
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Patent number: 6838415Abstract: The invention relates to novel substituted benzoylisoxazoles of the general formula (I), in which n represents the number 0, 1, 2 or 3, A represents a single bond or represents alkanediyl (alkylene), R1 represents hydrogen or represents in each case optionally substituted alkyl, alkenyl or cycloalkyl, R2 represents hydrogen, cyano, carbamoyl, halogen, or represents in each case optionally substituted alkyl, alkylcarbonyl, alkoxy, alkoxycarbonyl or alkylthio, alkylsulphinyl or alkylsulphonyl, R3 represents hydrogen, nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino or dialkylaminosulphonyl, R4 represents nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino or dialkylaminosulphonyl, and Z represents an optionally substituted 4-Type: GrantFiled: April 20, 2000Date of Patent: January 4, 2005Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Müller, Stefan Lehr, Otto Schallner, Hans-Georg Schwarz, Heinz-Jürgen Wroblowsky, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky
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Publication number: 20040235912Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is selected from the group consisting of hydrogen, substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, and C3-C6 cycloalkylaryl-C0-2-alkyl; W is O or S; X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom the linker may be replaced with O, NH or S; Y is C, O, S, NH or a single bond; E is C(R3)(R4)A or A.Type: ApplicationFiled: May 10, 2004Publication date: November 25, 2004Inventors: Richard Duane Johnston, Nathan Bryan Mantlo, Richard Craig Thompson
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Publication number: 20040220241Abstract: The invention relates to compounds of the formula I 1Type: ApplicationFiled: January 14, 2003Publication date: November 4, 2004Inventors: Horst Juraszyk, Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Christopher Barnes, Johannes Gleitz
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Patent number: 6797720Abstract: A 1,3,4-oxadiazoline derivative of formula (I) wherein W is oxygen, sulfer; R is hydrogen, alkyl, CycA, etc.; AA1 is a single bond, amino acid residue, etc.; AA2 is a single bond, amino acid residue, etc.; R7 and R8 are hydrogen, alkyl, etc.; R9 is hydrogen, alkyl, etc., and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of inflammatory diseases, diseases induced by apoptosis, diseases induced by disorders of immune responses, autoimmune diseases, diseases induced by decomposition of proteins which compose organism, shock, circulatory system disorders, blood coagulation systems disorders, malignant tumors, acquired immune deficiency syndrome (AIDS) and AIDS-related complex (ARC), parasitic diseases, nerve degeneration diseases, pulmonary disorders, bone resorption diseases, endocrinesthenia, etc.Type: GrantFiled: August 28, 2002Date of Patent: September 28, 2004Assignee: ONO Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Iori Itagaki
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Patent number: 6696475Abstract: The present invention discloses compounds having the formula wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.Type: GrantFiled: August 8, 2001Date of Patent: February 24, 2004Assignee: NeuroSearch A/SInventors: Bjarne H. Dahl, Palle Christophersen
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Publication number: 20040010011Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: 1Type: ApplicationFiled: February 20, 2003Publication date: January 15, 2004Inventors: Jean-Louis Assens, Claude Bernhart, Frederique Cabanel-Haudricourt, Dino Nisato
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Publication number: 20040006050Abstract: Compounds of Formula I, 1Type: ApplicationFiled: June 9, 2003Publication date: January 8, 2004Applicants: Wyeth, ArQule Inc.Inventors: Anthony Frank Kreft, Derek Cecil Cole, Kevin Roger Woller, Joseph Raymond Stock, Kristina Martha Kutterer, Dennis Martin Kubrak, Charles William Mann, William Jay Moore, David Scott Casebier
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Publication number: 20040002525Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.Type: ApplicationFiled: October 28, 2002Publication date: January 1, 2004Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, Jun Li
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Patent number: 6670481Abstract: The invention relates to novel arylalkyl- or aryloxyalkyl-substituted oxiranecarboxylic acids of the general formula I: in which Ar, R3, Y and n are as defined in the description, and also to medicaments comprising them and to their use for the treatment and prophylaxis of the disorders mentioned in claim 4 which are caused by disturbances of glucose and/or lipid metabolism, such as, for example, diabetes type 2 and other insulin-resistant conditions.Type: GrantFiled: June 18, 2002Date of Patent: December 30, 2003Assignee: Medicone AG Gesellschaft fur Molekularbiologische KardiologieInventor: Horst P. O. Wolf
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Publication number: 20030225083Abstract: Compounds of formula I: 1Type: ApplicationFiled: March 17, 2003Publication date: December 4, 2003Inventors: Stephen A. Fakhoury, Helen Lee, Robert Schaum, Karen Sexton
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Publication number: 20030166574Abstract: A 1,3,4-oxadiazoline derivative of formula (I) 1Type: ApplicationFiled: August 28, 2002Publication date: September 4, 2003Inventors: Kazuyuki Ohmoto, Iori Itagaki
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Publication number: 20030162814Abstract: The novel compounds of formula (I), wherein R1, R2, R2′, R2″, R3, R4, R5, R5′, R5″, R5′″, R″″, X, Y, U, V and W have the meanings given in patent claim no. 1, are inhibitors of the coagulation factors Xa and VIIa and can be used for treating thromboses, myocardial infarction, arteriosclerosis, inflammations, apoplexy, angina pectoris, restenosis following angioplasty, intermittent claudication, tumours, tumour diseases and/or tumour metastases.Type: ApplicationFiled: January 23, 2003Publication date: August 28, 2003Inventors: Horst Juraszyk, Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Christopher Barnes, Johannes Gleitz
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Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones, their preparation and their use in medicaments
Patent number: 6596742Abstract: Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones of the formula 1 in any optically isomeric form, and their physiologically acceptable salts, where R1 is C1-C6-alkyl, C3-C9-cycloalkyl, both of which may be unsubstituted or substituted, and R2 and R3 independently of one another are hydrogen, C6-C10-aryl, C3-C8-cycloalkyl, C6-C10-aryloxymethyl, O-benzyl, O—C6-C10-aryl, O—C3-C8-cycloalkyl, O—C1-C6-alkyl, SO2—NH—C1-C6-alkyl, SO2—NH-(2,2,6,6-tetramethylpiperidin-4-yl), SO2—NH—C3-C8-cycloalkyl, SO2—N(C1-C6-alkyl)2 or COX, where X is O—C1-C6-alkyl, NH—C1-C6-alkyl, NH—C3-C8-cycloalkyl or N(C1-C6-alkyl)2, with the proviso that the substitutents R2 and R3 may in some instances be unsubstituted or substituted and are not both simultaneously hydrogen. A process for their preparation, and their inhibitory effect on the hormone-sensitive lipase, HSL.Type: GrantFiled: September 5, 2000Date of Patent: July 22, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Stefan Petry, Karl Schoenafinger, Guenter Mueller, Karl-Heinz Baringhaus -
Publication number: 20030087831Abstract: 1Type: ApplicationFiled: May 31, 2002Publication date: May 8, 2003Inventors: Kazuyuki Ohmoto, Motohiro Okuma, Tomohiko Sekioka
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Patent number: 6545030Abstract: 1-Heterocycle substituted diarylamines, methods of making and using them, and compositions containing them.Type: GrantFiled: January 17, 2002Date of Patent: April 8, 2003Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Haile Tecle, Lu-Yan Zhang
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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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Patent number: 6472414Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X, are as defined herein.Type: GrantFiled: May 18, 1999Date of Patent: October 29, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
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Patent number: 6413996Abstract: The invention relates to compounds having the formula (I) or a pharmaceutically acceptable salt thereof. In the formula (I), X represents a group having the structural formula (II), and Y represents O or S. The compounds of the invention can be used a chloride channel blockers.Type: GrantFiled: March 8, 2001Date of Patent: July 2, 2002Assignee: Neurosearch A/SInventors: Bjarne H. Dahl, Palle Christophersen
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Patent number: 6388070Abstract: The present invention provides novel thioester derivatives of thiazolyl acetic acid of the general formula (I), wherein, R1 represents H, trityl, CH3, or CRaRbCOOR3, in which Ra and Rb, independently of one another, represents hydrogen or methyl and R3 represents H or C1-C7 alkyl; and R2 represents C1-C4 alkyl or phenyl.Type: GrantFiled: January 5, 2001Date of Patent: May 14, 2002Assignee: Orchid Chemicals & Pharmaceuticals Ltd.Inventors: Pandurang Balwant Deshpande, Parven Kumar Luthra