Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/298)
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Publication number: 20090170850Abstract: The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula I wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R2R5N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups.Type: ApplicationFiled: May 9, 2008Publication date: July 2, 2009Inventors: Tim Fat Tam, Michael Spino, Wanren Li, Yingsheng Wang, Yanqing Zhao, Birenkumar Hasmukhbhai Shah
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Publication number: 20090131486Abstract: The invention provides compounds of formula wherein R1, R3, R4, R5, R6, R14, X and W are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.Type: ApplicationFiled: May 7, 2007Publication date: May 21, 2009Inventors: Peter Hansen, Karolina Lawitz, Matti Lepisto, Hans Lonn, Asim Ray
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Patent number: 7528255Abstract: The invention relates to the use of a group of aryl ureas in treating raf mediated diseases and pharmaceutical compositions for use in such therapy of the formula wherein, Y is NHR Hal is chlorine or bromine, R is H, CH3 or CH2OH, and X1 to X7 are each, independently, H, OH or —OC(O)C1-C4 alkyl, or a salt purified stereoisomer thereof, wherein at least one of X1 to X7 is OH or —OC(O)C1-C4 alkyl.Type: GrantFiled: February 11, 2002Date of Patent: May 5, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy Lowinger, William Scott, Roger Smith, Jill Wood
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Publication number: 20090099184Abstract: Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same.Type: ApplicationFiled: February 15, 2007Publication date: April 16, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephane Delombaert, Anne Bettina Eldrup, Neil Alexander Farrow, Jennifer A. Kowalski, Ingo Andreas Mugge, Fariba Soleymanzadeh, Alan David Swinamer, Steve John Taylor
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Publication number: 20090093638Abstract: The present invention relates to compositions and methods for achieving the efficient allylic oxidation of organic molecules, especially olefins and steroids, under aqueous conditions. The invention concerns the use of dirhodium (II,II) “paddlewheel complexes, and in particular, dirhodium carboximate and tert-butyl hydroperoxide as catalysts for the reaction. The use of aqueous conditions is particularly advantageous in the allylic oxidation of 7-keto steroids, which could not be effectively oxidized using anhydrous methods, and in extending allylic oxidation to enamides and enol ethers.Type: ApplicationFiled: October 6, 2008Publication date: April 9, 2009Applicant: UNIVERSITY OF MARYLAND, COLLEGE PARKInventors: Michael P. Doyle, Arthur J. Catino, Hojae Choi, Jason M. Nichols
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Publication number: 20090075819Abstract: The present invention relates to Indanyl- and Tetrahydronaphtyl-amino-thiourea compounds of formula I wherein the variables R1 to R4 are as in the description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection.Type: ApplicationFiled: November 15, 2006Publication date: March 19, 2009Applicant: BASF SEInventors: Markus Kordes, Christopher Koradin, Deborah L. Culbertson
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Publication number: 20090069388Abstract: The present application describes deuterium-enriched sorafenib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 21, 2008Publication date: March 12, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090054656Abstract: To provide a method for producing a specific nicotinic acid derivative or a salt thereof. A method for producing a nicotinic acid derivative represented by the formula (I): wherein each of X1 and X2 which are independent of each other, is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a haloalkyl group or a haloalkoxy group; R is an alkyl group; and Hal is a chlorine atom or a bromine atom; or a salt thereof, is provided which comprises reacting a compound represented by the formula (II): is wherein X1, X2 and R are as defined above, or a salt thereof, with a halogenating agent.Type: ApplicationFiled: April 20, 2006Publication date: February 26, 2009Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Shigeyuki Nishimura, Fumio Kanamori, Masashi Hisamoto
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Publication number: 20090053641Abstract: [PROBLEMS] Providing a charge control agent that has a negative charge providing property at a practical level, is colorless to light-colored and usable in color toners, produces static charges stable to environmental changes by electrifying the resin powder of a toner and the like, is excellent in storage stability and durability, and is highly safe, as well as a method of controlling the charge of resin powder using the charge control agent, and a toner. [MEANS OF SOLVING THE PROBLEMS] A charge control agent having a compound represented by the formula shown below as the active ingredient, as well as a method of controlling the charge of resin powder using the charge control agent, and a toner.Type: ApplicationFiled: March 22, 2006Publication date: February 26, 2009Inventors: Kazuyoshi Kuroda, Masashi Yasumatsu
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Publication number: 20090012091Abstract: The present invention relates to a compound represented as the following Formula (I) and a pharmaceutical composition thereof wherein all substituents are as defined in the specification; and also relates to a method for treating or lessening the severity of a disease or a condition, comprising administering said compound or said pharmaceutical composition.Type: ApplicationFiled: June 23, 2008Publication date: January 8, 2009Applicant: KinaGen, Inc.Inventor: Chang Jun Yu
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Publication number: 20080280957Abstract: Disclosed are MEK inhibitors useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: May 17, 2006Publication date: November 13, 2008Applicants: ARRAY BIOPHARMA, INC., ASTRAZENECA ABInventors: Allison L. Marlow, Eli M. Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hoog Woon Yang, James Blake, Richard Anthony Storey, Rebecca Jane Booth, John David Pittam, John Leonard, Mark Richard Fielding
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Publication number: 20080266647Abstract: A colorant molecule is provided that includes at least one switch unit. The switch unit comprises ring-based tautomers, of which there may be more than one per chromophore, and may include donor and/or acceptor moieties.Type: ApplicationFiled: April 26, 2007Publication date: October 30, 2008Inventors: Kent D. Vincent, Xian-An Zhang, Zhou-Lin Zhou
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Publication number: 20080269059Abstract: Compounds of the formula (I), or salts thereof, in which R1 to R4 are as defined in formula (I) of claim 1 are suitable as useful-plant-protecting agents for reducing or preventing harmful effects of agrochemicals on the useful plants and their method of preparation are described.Type: ApplicationFiled: April 29, 2008Publication date: October 30, 2008Inventors: Frank Ziemer, Lothar Willms, Christopher Rosinger, Thomas Auler, Erwin Hacker, Udo Bickers
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Publication number: 20080262236Abstract: The present invention relates to a process for preparing 4-{4-[({[4-chloro-3-(trifluoro-methyl)phenyl]amino}carbonyl)amino]phenoxy}-N-methylpyridine-2-carboxamide and its tosylate salt.Type: ApplicationFiled: September 20, 2005Publication date: October 23, 2008Applicant: Bayer HealthCare AGInventors: Michael Logers, Reinhold Gehring, Oliver Kuhn, Mike Matthaus, Klaus Mohrs, Matthias Muller-Gliemann, Jurgen Stiehl, Mathias Berwe, Jana Lenz, Werner Heilmann
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Publication number: 20080262237Abstract: The present invention provides a black pigment consisting of an oxonol compound having a mean particle diameter ranging from 0.01 to 10.0 micrometers, and a black pigment dispersion and a black resin composition comprising the black pigment.Type: ApplicationFiled: November 13, 2007Publication date: October 23, 2008Applicant: FUJIFILM CorporationInventors: Keizo Kimura, Osamu Uchida, Katsuyoshi Yamakawa
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Publication number: 20080249313Abstract: The invention relates to a process for the preparation of pyridylcarboxylic amides and esters I, Formula (I) wherein Hal, X and R1 have the meanings given in claim 1, which comprises the following steps: (a) heating a mixture consisting essentially of trichloromethylpyridine II, Formula (II), wherein Hal has the meaning given, and 1.0 to 1.5 equivalents of concentrated sulfuric acid, characterized in that the trichloromethylpyridine II in a liquid form is added to the concentrated sulfuric acid at a temperature from 110° C. to 160° C.; and (b) reacting the intermediate product obtained in step (a) with an amine or alcohol III, HXR1, wherein X and R1 have the meaning given, optionally in the presence of a solvent and/or a base.Type: ApplicationFiled: October 26, 2006Publication date: October 9, 2008Applicant: BASF SEInventors: Monika Brink, Marcus Knell, Jan Hendrik Wevers
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Publication number: 20080234332Abstract: The present invention relates to Raf kinase inhibitors containing zinc-binding and their use in the treatment of Raf related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.Type: ApplicationFiled: September 10, 2007Publication date: September 25, 2008Inventors: Xiong Cai, Changgeng Qian, Stephen Gould, Haixiao Zhai
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Publication number: 20080214815Abstract: A process for preparing a compound represented by the formula (I): comprising reacting a compound represented by the formula (II) or salt thereof: with a compound represented by the formula (III): in the presence of a condensation reagent, wherein R1 represents 1) optionally substituted azetidin-1-yl, 2) optionally substituted pyrrolidin-1-yl, 3) optionally substituted piperidin-1-yl, etc.; R2, R3, R4 and R5 may be the same or different and each represents hydrogen or fluorine; and R6 represents hydrogen or fluorine.Type: ApplicationFiled: August 27, 2007Publication date: September 4, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Mitsuo Nagai, Tomohiro Matsushima, Atsushi Kamada, Kazunori Wakasugi, Shuji Shirotori, Shinya Abe, Kazumasa Nara, Takahisa Sakaguchi
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Publication number: 20080207701Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.Type: ApplicationFiled: April 2, 2008Publication date: August 28, 2008Inventors: Mark Donald Chappell, Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel
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Publication number: 20080200521Abstract: Novel hydroxamic acid containing amino acid derivatives are provided that are useful for treatment of inflammation, inflammatory and immunological diseases; lowering blood glucose, serum insulin, free fatty acids, cholesterol and triglyceride levels; and for treatment or prophylaxis of metabolic disorders.Type: ApplicationFiled: January 3, 2008Publication date: August 21, 2008Inventors: Partha Neogi, Debendranath Dey, Abjiheet Nag, Sujata Neogi, Bishwajit Nag
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Publication number: 20080200513Abstract: The present invention relates to pyridinone derivatives of formula (I): wherein Z represents C2-6 alkynyl, aryl or heteroaryl, any of which groups may be optionally substituted, and R1 represents hydrogen, C1-6 alkyl, C3-7 heterocycloalkyl(C1-6)alkyl, di(C1-6)alkylamino(C1-6)alkyl, C2-6 alkylcarbonyloxy(C1-6)alkyl or C3-7 cycloalkoxycarbonyloxy(C1-6)alkyl, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C virus infections.Type: ApplicationFiled: June 1, 2004Publication date: August 21, 2008Applicant: ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPAInventors: Stafania Colarusso, Frank Narjes
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Publication number: 20080194521Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: ApplicationFiled: August 13, 2007Publication date: August 14, 2008Inventors: Robert Eugene Hormann, Colin M. Tice, Orestes Chortyk, Howard Smith, Thomas Meteyer
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Publication number: 20080188528Abstract: Provided are compounds that are modulators of C3a receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, the compounds are pyridones. In certain embodiments, provided are methods for treatment or amelioration of diseases associated with modulation of C3a receptor activity.Type: ApplicationFiled: December 21, 2007Publication date: August 7, 2008Inventors: Ronald J. Biediger, Huong M. Bui, Jie Chen, Kevin M. Henry, Thomas Thrash
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Publication number: 20080171741Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: October 25, 2007Publication date: July 17, 2008Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
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Patent number: 7399774Abstract: A compound of the formula (I) or a pharmaceutically acceptable salt, enantiomer, racemate, diastereomers or mixtures thereof, or a solvate thereof, formulations and methods of use thereof, as opioid receptor antagonists are disclosed wherein the variables are as described herein.Type: GrantFiled: February 25, 2004Date of Patent: July 15, 2008Assignee: Eli Lilly and CompanyInventors: Miles Goodman Siegel, Russell Dean Stucky, Kumiko Takeuchi
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Patent number: 7393873Abstract: N-aryl arylsulfonamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.Type: GrantFiled: June 30, 2004Date of Patent: July 1, 2008Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, John Jin Lim, Dai-shi Su, Michael R. Wood
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Publication number: 20080132507Abstract: A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.Type: ApplicationFiled: October 13, 2005Publication date: June 5, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Richard Clark, Shinsuke Hirota, Hiroshi Azuma, Kazunobu Kira, Nobuhisa Watanabe, Tadashi Nagakura, Tatsuo Horizoe
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Patent number: 7354941Abstract: Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease, of Formula (1.0.0): wherein R5 and R6 are taken together to form a moiety of partial Formulas (1.1.1) through (1.1.5): or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 30, 2001Date of Patent: April 8, 2008Assignee: Pfizer Products Inc.Inventors: Anthony Marfat, Robert James Chambers
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Publication number: 20080064872Abstract: A novel compound having agonist activity at the S1P3 receptor which is represented by the formula I wherein X is selected from the group consisting of CR3, N and NO; Y is selected from the group consisting of CR3, N and NO; Z is selected from the group consisting of CR3, N and NO; and at least one of X, Y and Z is N or NO; V is O or NOR4 R1 is an aryl group; R2 is an aryl group; R3 is selected from the group consisting of H and alkyl; and 2 of said R3 groups may together form a cyclic alkyl ring having from 3 to 6 carbon atoms; R4 is selected from the group consisting of H and alkyl; a is 0 or an integer of from 1 to 6; b is 0 or 1; c is 0 or 1; f is 0 or an integer of 1 or 2; x is 0 or 1; y is 0 or an integer of from 1 to 3; and z is 0 or an integer of from 1 to 3.Type: ApplicationFiled: September 6, 2007Publication date: March 13, 2008Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Xiaoxia Liu
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Patent number: 7342115Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: November 7, 2003Date of Patent: March 11, 2008Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
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Publication number: 20080020010Abstract: A new class of diketo acids constructed on pyridinone scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other integrase-based anti-HIV agents). Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.Type: ApplicationFiled: July 13, 2007Publication date: January 24, 2008Applicant: THE UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.Inventors: Vasu Nair, Byung I. Seo, Vinod R. Uchil
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Patent number: 7276612Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: GrantFiled: April 6, 2004Date of Patent: October 2, 2007Assignee: Pharmacyclics, Inc.Inventors: Eric J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Patent number: 7262252Abstract: There is provided a fluorine-containing resin composition which is used for nonlinear optical material and comprises (I) a fluorine-containing prepolymer and (II) an organic compound exhibiting a second- or higher-order nonlinear optical effect, in which the fluorine-containing prepolymer (I): (1) is a non-crystalline polymer having a fluorine content of not less than 25% and (2) has a carbon-carbon double bond in a polymer side chain or at an end of a polymer trunk chain and also there is provided a nonlinear optical waveguide device produced from the fluorine-containing resin composition. A suitable nonlinear optical material having a stable structure with a nonlinear substance is produced, and an excellent nonlinear optical waveguide device is produced by relatively simple steps while maintaining transparency in a near infrared region.Type: GrantFiled: November 12, 2003Date of Patent: August 28, 2007Assignee: Daikin Industries, Ltd.Inventors: Takayuki Araki, Yoshito Tanaka, Mihoko Ohashi, Yuzo Komatsu
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Patent number: 7230017Abstract: The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: GrantFiled: August 18, 2003Date of Patent: June 12, 2007Assignee: Bayer Healthcare AGInventors: Heike Gielen-Haertwig, Volkhart Min-Jian Li, Ulrich Rosentreter, Karl-Heinz Schlemmer, Swen Allerheiligen, Leila Telan, Lars Bärfacker, Jörg Keldenich, Mary F. Fitzgerald, Kevin Nash, Barbara Albrecht, Dirk Meurer
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Patent number: 7223774Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are also useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: April 21, 2004Date of Patent: May 29, 2007Assignee: Elan Pharmaceuticals, Inc.Inventors: Jose Aquino, Varghese John, John Tucker, Roy Hom, Shon Pulley, Ruth Tenbrink
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Patent number: 7183278Abstract: Disclosed are novel compounds useful for the control of harmful organisms, harmful organism control agents using the same, and processes for producing the novel compounds. The useful novel compounds according to the present invention include compounds represented by formula (1).Type: GrantFiled: November 4, 1999Date of Patent: February 27, 2007Assignee: Meiji Seika Kaisha, Ltd.Inventors: Keiichi Imamura, Kouichi Mitomo, Natsuko Yamada, Kazumi Yamamoto, Takashi Teraoka, Osamu Sakanaka, Hiroshi Kurihara, Makoto Taniguchi
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Patent number: 7153870Abstract: This invention relates to nicotinamide derivatives of general formula (I): in which R1, R2 and R3 have the meanings defined herein, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of such derivatives.Type: GrantFiled: July 20, 2004Date of Patent: December 26, 2006Assignee: Pfizer Inc.Inventor: John Paul Mathias
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Patent number: 7151112Abstract: This invention is directed to methods of using a compound of the formula and pharmaceutically acceptable salts thereof, wherein n, X, R1 and R2 are disclosed herein, for treating inflammatory events in an animal subject.Type: GrantFiled: December 23, 2003Date of Patent: December 19, 2006Assignee: UCB SAInventors: Neil S Cutshall, Scott C Jeffrey
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Patent number: 7141586Abstract: This invention relates to nicotinamide derivatives of formula (I) and to processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions containing, and the uses of such derivatives: wherein each substituent is defined herein.Type: GrantFiled: July 20, 2004Date of Patent: November 28, 2006Assignee: Pfizer Inc.Inventors: Simon Bailey, Christopher Gordon Barber, Paul Alan Glossop, Donald Stuart Middleton
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Patent number: 7138525Abstract: A compound of the formula (I): (wherein Ar1 and Ar2 are independently aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of cyano, halogen, nitro, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl, lower alkenyl, lower alkylamino, di-lower alkylamino, lower alkanoylamino, lower alkylsulfonylamino, arylsulfonylamino, hydroxy, lower alkoxy, halo-lower alkoxy, aryloxy, heteroaryloxy, lower alkylthio, carboxyl, formyl, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, di-lower alkylcarbamoyl, lower alkylsulfonyl, arylsulfonyl, aryl and heteroaryl; R1 and R2 are independently lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl or lower alkoxy, any of which is optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkyType: GrantFiled: July 27, 2004Date of Patent: November 21, 2006Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Nagaaki Sato, Makoto Ando, Shiho Ishikawa, Tsuyoshi Nagase, Keita Nagai, Akio Kanatani
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Patent number: 7129360Abstract: Substituted alkylmetal reagents such as (trimethylsilylmethyl)lithium are reacted with azaaromatic compounds and/or nitrogen heterocycle compounds to produce functionalized azaaromatic compounds and functionalized nitrogen heterocycle compounds.Type: GrantFiled: April 6, 2004Date of Patent: October 31, 2006Assignee: FMC CorporationInventors: Christopher J. Woltermann, Douglas E. Sutton
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Patent number: 7125871Abstract: Compounds of the formula (I) in which R1, R2 and X1 have the meanings given in the specification, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous systemType: GrantFiled: May 24, 2001Date of Patent: October 24, 2006Assignee: Eli Lilly and CompanyInventors: Ivan Collado Cano, Jesus Ezquerra-Carrera, Alicia Marcos Liorente, Luisa Maria Martin-Cabrejas, James Allen Monn
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Patent number: 7074813Abstract: The present invention is directed to substituted N?-(arylcarbonyl)-benzhydrazides, N?-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II: wherein Ar1, Ar2, and R1–R2 are defined herein. The present invention also relates to the discovery that compounds having Formulae I and II are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: April 5, 2004Date of Patent: July 11, 2006Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Shailaja Kasibhatla, John Drewe, P. Sanjeeva Reddy, Han-Zhong Zhang
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Patent number: 7060717Abstract: The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.Type: GrantFiled: June 9, 2004Date of Patent: June 13, 2006Assignee: Pfizer IncInventors: Simon Bailey, Elisabeth C. L. Gautier, Alan J. Henderson, Thomas V. Magee, Anthony Marfat, John P. Mathias, Dale G. McLeod, Sandra M. Monaghan, Blanda L. C. Stammen
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Patent number: 7056932Abstract: The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.Type: GrantFiled: December 10, 2004Date of Patent: June 6, 2006Assignee: Hoffman-La Roche Inc.Inventors: Luca Claudio Gobbi, Katrin Groebke Zbinden, Peter Mohr, Ulrike Obst
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Patent number: 7056934Abstract: This invention relates to nicotinamide derivatives of general formula (I): in which R1, R2 and R3 have the meanings defined herein, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of such derivatives.Type: GrantFiled: July 20, 2004Date of Patent: June 6, 2006Assignee: Pfizer IncInventors: Mark Edward Bunnage, John Paul Mathias
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Patent number: 6992094Abstract: The invention concerns novel diarylselenide compounds corresponding to the general formula (I) and the use thereof in pharmaceutical compositions in human or veterinary medicine (in the treatment of dermatological, rheumatic, cardiovascular and ophthalmologic pathologies in particular), or in cosmetic compositions.Type: GrantFiled: June 11, 1999Date of Patent: January 31, 2006Assignee: Galderma Research & Development, S.N.C.Inventors: Jean-Michael Bernardon, Philippe Diaz
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Patent number: 6969768Abstract: A process for preparing 4-haloalkylnicotinic esters of the formula (I), where RF is (C1-C4)-haloalkyl and R is (C1-C6)-alkyl; which comprises a) reacting an aminoketone of the formula (II), RF—C(O)—CH?CH—NH2 ??(II) ?in a condensation reaction under reduced pressure with a compound of the formulae (III) to (V), (R1Z)CH?CH—COOR??(III), (R1Z)2CH—CH2—COOR??(IV), HC?C—COOR??(V), where R1 is (C1-C6)-alkyl and Z is O, S, NR1 or C(O)O, ?to give a compound of the formulae (VI) and/or (VII), RF—C(O)—CH?CH—NH—CH?CH—COOR??(VI) RF—C(O)—CH?CH—NH—CH(ZR1)—CH2—COOR??(VII) b) and subjecting the reaction product to a ring closure reaction.Type: GrantFiled: September 9, 2002Date of Patent: November 29, 2005Assignee: Bayer CropScience GmbHInventor: Sergiy Pazenok
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Patent number: 6949539Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: June 1, 2001Date of Patent: September 27, 2005Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber
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Patent number: 6949556Abstract: The present invention relates to compounds of general formula (I), wherein R1-R4 have the meanings given in the specification, A is CH2, CHOH or CH—(C1-C3-alkyl), B and C are independently CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group optionally substituted by the substituents listed in the specification.Type: GrantFiled: February 13, 2002Date of Patent: September 27, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart