Chalcogen Bonded Directly To Ring Carbon Of Pyridine Or Partially Hydrogenated Pyridine Ring Patents (Class 546/261)
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Publication number: 20110172248Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: September 17, 2010Publication date: July 14, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Charles David Weaver, Alice L. Rodriguez, Andrew S. Felts, Carrie K. Jones, Brittney S. Bates
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Publication number: 20110172247Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions.Type: ApplicationFiled: September 17, 2010Publication date: July 14, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Charles David Weaver, Alice L. Rodriguez, Andrew S. Felts, Carrie K. Jones, Brittney S. Bates
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Publication number: 20110166158Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: September 17, 2010Publication date: July 7, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Charles David Weaver, Alice L. Rodriguez, Andrew S. Felts, Carrie K. Jones, Brittney S. Bates, Brian A. Chauder
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Patent number: 7973059Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: October 17, 2006Date of Patent: July 5, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Scott Wolkenberg, Mark T. Bilodeau, M. Brad Nolt
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Publication number: 20110136871Abstract: The present application relates to novel 2-alkoxy-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: May 22, 2009Publication date: June 9, 2011Applicant: BAYER SCHERING AKTIENGESELLSCHAFTInventors: Walter Hübsch, Daniel Meibom, Alexandros Vakalopoulos, Barbara albrecht-Küpper, Peter Nell, Katja Zimmermann, Frank Süssmeier, Joerg Keldenich
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Publication number: 20110130365Abstract: The present invention provides Formula (1A) XN O R 3 HN R 5 O R 4 R 2 R 1 (1A) 5 compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the glucokinase enzyme, where X, R 1, R 2, R 3, R 4, and R 5 are as described herein.Type: ApplicationFiled: July 15, 2009Publication date: June 2, 2011Inventors: John W. Benbow, Jihong Lou, Jeffrey A. Pferfferkorn, Meihua M. Tu
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Publication number: 20110118248Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: January 13, 2009Publication date: May 19, 2011Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M. K. Pennell, John J. Wright, Antoni Krasinski, Qiang Wang
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Publication number: 20110118470Abstract: Compounds represented by the following general formula: wherein Ag is an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xg is —O—, —S—, etc.; Yg is an optionally substituted C6-14 aryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tg1 is a group represented by the following general formula: (wherein Eg is a single bond or —N(Rg2)—), Rg1 and Rg2 each independently represent a hydrogen atom, an optionally substituted C1-6 alkyl group, etc. and Zg represents a C1-8 alkyl group, a C3-8 alicyclic hydrocarbon group, a C6-14 aryl group, etc.), salts thereof or hydrates of the foregoing.Type: ApplicationFiled: January 7, 2011Publication date: May 19, 2011Inventors: Yasuhiro FUNAHASHI, Akihiko Tsuruoka, Masayuki Matsukura, Toru Haneda, Yoshio Fukuda, Junichi Kamata, Keiko Takahashi, Tomohiro Matsushima, Kazuki Miyazaki, Ken-ichi Nomoto, Tatsuo Watanabe, Hiroshi Obaishi, Atsumi Yamaguchi, Sachi Suzuki, Katsuji Nakamura, Fusayo Mimura, Yuji Yamamoto, Junji Matsui, Kenji Matsui, Takako Yoshiba, Yasuyuki Suzuki, Itaru Arimoto
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Patent number: 7943638Abstract: A carboxamide compound represented by the formula (1): [wherein Q represents a nitrogen-containing 6-membered aromatic heterocyclic group optionally fused with a benzene ring, one of ring constitutional atoms of the heterocyclic group is a nitrogen atom and the heterocyclic group may be substituted with a group selected from the group consisting of a C1-C3 alkyl and the like, R1 represents a C1-C3 alkyl group or the like, R2 represents a hydrogen atom or the like, and R3 represents a hydrogen atom or the like] and a plant disease controlling agent comprising this as an active ingredient.Type: GrantFiled: July 12, 2006Date of Patent: May 17, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Shin-ichiro Souma, Yoshiharu Kinoshita
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Publication number: 20110110865Abstract: The present invention relates to chelators, in particular to chelators which are capable of forming complexes, i.e. paramagnetic chelates, with paramagnetic metal ions. The invention also relates to said paramagnetic chelates, said paramagnetic chelates linked to other molecules and their use as contrast agents in magnetic resonance imaging (MRI).Type: ApplicationFiled: August 12, 2008Publication date: May 12, 2011Inventors: Oskar Axelsson, Horry John Wadsworth, Ian Martin Newington, Dennis O'Shea
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Patent number: 7928239Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions in such therapy.Type: GrantFiled: February 7, 2001Date of Patent: April 19, 2011Assignee: Bayer Healthcare LLCInventors: Jacques Dumas, Bernd Riedl, Uday Khire, Jill E. Wood, Robert N. Sibley, Mary-Katherine Monahan, Joel Renick, David E. Gunn, Timothy B. Lowinger, William J. Scott, Roger A. Smith
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Patent number: 7902372Abstract: 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: GrantFiled: April 2, 2008Date of Patent: March 8, 2011Assignee: Eli Lilly and CompanyInventors: Mark Donald Chappell, Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel
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Patent number: 7901559Abstract: It is intended to provide a method for easily detecting a phosphorylated peptide (protein) in a test sample by using SDS-polyacrylamide gel electrophoresis (SDS-PAGE) which has been conventionally employed in analyzing a protein; a polyacrylamide gel for electrophoresis to be used in the method; a method of producing the gel; and a synthesizing intermediate in producing the gel. The polyacrylamide gel for electrophoresis to be used in the method of the invention is characterized in that at least a part of the structure thereof has a structure represented by the following formula (I); wherein M2+represents a transition metal ion; and X represents a linker group.Type: GrantFiled: August 1, 2005Date of Patent: March 8, 2011Assignee: Nard Institute, Ltd.Inventors: Tohru Koike, Akihiko Kawasaki, Tatsuhiro Kobashi
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Publication number: 20110054172Abstract: The present invention provides a novel pyridylaminoacetic acid compound represented by the following formula (1): (wherein R1, R2, R3, Y and Z are as defined in the description and claims), or a pharmacologically acceptable salt thereof. The pyridylaminoacetic acid compound has EP2 agonistic action and is therefore useful as a therapeutic and/or prophylactic agent for respiratory diseases such as asthma or chronic obstructive pulmonary disease.Type: ApplicationFiled: March 12, 2009Publication date: March 3, 2011Inventors: Ryo Iwamura, Masayuki Tanaka, Tetsushi Katsube, Manabu Shigetomi, Eiji Okanari, Yasunori Tokunaga, Hiroshi Fujiwara
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Patent number: 7897621Abstract: The present invention relates to compounds formula I: and pharmaceutically acceptable salts thereof, wherein R1 to R8 are as defined in the description and claims for use as HDL-cholesterol raising agents in the treatment and/or prophylaxis of diseases or disorders that can be treated with such agents such as dyslipidemia.Type: GrantFiled: March 16, 2009Date of Patent: March 1, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Paul Hebeisen, Constantinos G. Panousis, Stephan Roever, Pius Waldmeier, Matthew Wright
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Publication number: 20110046088Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: ApplicationFiled: February 20, 2008Publication date: February 24, 2011Applicants: SYNGENTA CROP PROTECTION, INC., SYNGENTA LIMTIEDInventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
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Patent number: 7893061Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein A1-3, R1 and R3-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: July 13, 2007Date of Patent: February 22, 2011Assignee: Amgen Inc.Inventor: Ryan White
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Publication number: 20110034416Abstract: Disclosed are compounds of Formula (I): and salts thereof. Also, disclosed are methods of using the compounds in the treatment of proliferative diseases, such as cancer, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a pharmaceutically acceptable salt.Type: ApplicationFiled: January 22, 2009Publication date: February 10, 2011Inventors: Robert M. Borzilleri, Zhen-Wei Cai
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Publication number: 20110028509Abstract: The invention relates to compounds of formula I wherein R1, R2, R4, Ra, Rb, Rc, Re, A*, W1, W2 and W3 are as defined in claim 16, for the treatment of CXCR3 related diseases.Type: ApplicationFiled: April 8, 2009Publication date: February 3, 2011Applicant: MERCK SERONO SAInventors: Stefano Crosignani, Christophe Cleva, Christos Tsaklakidis, Lars Burgdorf
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Patent number: 7880004Abstract: The invention is directed to compounds that are useful for the treatment of cancer having the following Formula:Type: GrantFiled: September 14, 2006Date of Patent: February 1, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Zhen-wei Cai, Donna D. Wei, John S. Tokarski
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Patent number: 7879839Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: July 27, 2005Date of Patent: February 1, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman, Douglas C. Beshore, B. Wesley Trotter, Kausik K. Nanda, Richard Isaacs, Linda S. Payne, Lou Anne Neilson, Zhicai Wu, Mark T. Bilodeau, Peter J. Manley, Adrienne E. Balitza
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Publication number: 20110021487Abstract: The present application relates to novel cycloalkoxy-substituted 4-phenyl-3,5-dicyanopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders.Type: ApplicationFiled: January 31, 2009Publication date: January 27, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Walter Hübsch, Peter Nell, Frank Süssmeier, Alexandros Vakalopoulos, Daniel Meibom, Barbara Albrecht-Küpper, Katja Zimmermann
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Patent number: 7875633Abstract: A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents —CH2—O—, —CH?CH— or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.Type: GrantFiled: August 23, 2006Date of Patent: January 25, 2011Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Akira Naya, Toshihiro Sakamoto, Yuji Haga, Norikazu Otake
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Publication number: 20110009407Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.Type: ApplicationFiled: April 27, 2010Publication date: January 13, 2011Inventors: Ying-Zi Xu, Shendong Yuan, David Wone, Andrei Konradi
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Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
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Publication number: 20110009454Abstract: Disclosed is a composition for agricultural use, which is used for controlling or preventing plant diseases caused by plant pathogens. The composition for agricultural use contains a compound represented by formula (1), a salt thereof or a hydrate of the compound or the salt. (1) [In the formula, Z represents an oxygen atom, a sulfur atom or NRZ; and E represents a furyl group, a thienyl group, a pyrrolyl group, a tetrazolyl group, a thiazolyl group, a pyrazolyl group, a phenyl group or the like.Type: ApplicationFiled: February 27, 2009Publication date: January 13, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yuichi Matsuzaki, Takashi Komori, Tohru Inoue
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Publication number: 20110009421Abstract: An object of the present invention is to provide an agent for preventing or treating schizophrenia or the like, wherein the compound of the present invention has GPRS2 agonist activity.Type: ApplicationFiled: February 27, 2009Publication date: January 13, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masaki Setoh, Toshitake Kobayashi, Toshio Tanaka, Atsuo Baba
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Publication number: 20110003826Abstract: This invention relates to new chemical compounds, application of these compounds as anticoagulants, pharmaceutical compositions, and plasma-substituting solutions on their basis, and can be used for treating thromboembolic complications of diseases such as myocardial infarction, stroke, and thrombosis of deep veins or a pulmonary artery; and for preventing hypercoagulation conditions in consequence of injuries, surgeries, sepsis, various obstetric pathologies, in disaster medicine, resuscitation, and so on.Type: ApplicationFiled: June 27, 2008Publication date: January 6, 2011Applicant: Obschestvo S Organichennoi Otvetsttvennoctiyu "BioInventors: Elena Ivanovna Sinauridze, Fazoil Inoyatovich Ataullakhanov, Andrey Alexandrovich Butylin, Vladimir Borisovich Sulimov, Alexey Nickolayevich Romanov, Alexey Alexeevich Bogolyubov, Yury Vladimirovich Kuznetsov, Irina Vladimirovna Gribkova, Alexander Sergeevich Gorbatenko, Olga Anatolievna Kondakova
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Publication number: 20110003858Abstract: The invention provides compounds of formula (I) and formula (IV) (M)-(L)-(M) (I) [(M)-(L4)]t-G (VI) wherein M, L, L4, G and t 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: September 3, 2007Publication date: January 6, 2011Inventors: Lena Bergström, Hans Lönn, Michael Lundkvist, Peter Sjö
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Patent number: 7863280Abstract: This invention relates to compounds of formula (I), wherein R1 and R3 independently represent fluorine, methoxy, —OCF3, C2-C3-alkenyl or C1-C4-alkyl which is optionally substituted by chlorine, methoxy or one, two or three fluorine atoms; R2 represents hydrogen, fluorine, methoxy, —OCF3, C2-C3-alkenyl or C1-C4-alkyl which is optionally substituted by chlorine, methoxy or one, two or three fluorine atoms; X represents O, S, NH or N(C1-C3-alkyl); and Ar represents an unsubstituted or at least monosubstituted aryl or heteroaryl. Said compounds are inhibitors of poly(ADP-ribose) polymerase (PARP), and may be used for the treatment of a variety of disorders.Type: GrantFiled: April 11, 2007Date of Patent: January 4, 2011Assignee: Sanofi-Aventis Deutschland GmbHInventors: Stefan Peukert, Stefan Guessregen, Armin Hofmeister, Herman Schreuder, Uwe Schwahn
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Publication number: 20100324058Abstract: This invention relates to new chemical compounds, application of these compound as thrombin inhibitors, and pharmaceutical compositions based on them, and can be used to treat and prevent thrombin-dependent thromboembolic events, and in research.Type: ApplicationFiled: June 27, 2008Publication date: December 23, 2010Applicant: Obschestvo S Organichennoi Otvetsttvennoctiyou "Bionika"Inventors: Elena Ivanovna Sinauridze, Fazoil Inoyatovich Ataullakhanov, Andrey Alexandrovich Butylin, Vladimir Borisovich Sulimov, Alexey Nickolayevich Romanov, Alexey Alexeevich Bogolyubov, Yury Vladimirovich Kuznetsov, Irina Vladimirovna Gribkova, Alexander Sergeevich Gorbatenko, Olga Anatolievna Kondakova
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Publication number: 20100317851Abstract: There is described novel organo-platinum luminophores comprising a complex of formula (I). The luminophores have application as the emissive component in organic light emitting diodes.Type: ApplicationFiled: September 29, 2008Publication date: December 16, 2010Applicant: UNIVERSITY OF YORKInventors: Duncan W. Bruce, Valey Kozhevnikov
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Patent number: 7851489Abstract: The invention is directed to pyridinone compounds useful for modulating Met kinase, having the following structure: and is further directed to pharmaceutical compositions comprising the compound; and methods for treating proliferative diseases, such as cancer by the administration of this compound.Type: GrantFiled: November 8, 2007Date of Patent: December 14, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Gretchen M. Schroeder, Zhen-Wei Cai
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Publication number: 20100311748Abstract: The present disclosure relates to heterocyclic amide compounds, which are useful for inhibiting the Hedgehog pathway, and their use in treating a disease or medical condition mediated alone or in part by Hedgehog pathway inhibition. Also disclosed are methods for manufacture of these compounds, pharmaceutical compositions including these compounds, and use of these compounds in the manufacture of medicaments for treating such diseases and medical conditions in a subject. Formula (IA) with the provisio that either R2 or R3 is (Z).Type: ApplicationFiled: August 29, 2008Publication date: December 9, 2010Applicant: ASTRAZENECA ABInventors: Leslie Dakin, Benjamin Fauber, Alexander Hird, James Janetka, Daniel John Russell, Qibin Su, Bin Yang, Xiaolan Zheng
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Publication number: 20100305124Abstract: The present invention relates to aminopyridine and aminopyridazine derivatives of the general formula (I) in which R1, X, W and Q have the definitions given in the description, to a number of processes for preparing them, and to their use as insecticides.Type: ApplicationFiled: April 2, 2010Publication date: December 2, 2010Applicant: BAYER CROPSCIENCE AGInventors: Martin FUSSLEIN, Ernst Rudolf Gesing, Markus Heil, Bernd Alig, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Koichi Araki, Norio Sasaki, Sachio Kudo, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
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Publication number: 20100305097Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.Type: ApplicationFiled: July 28, 2010Publication date: December 2, 2010Inventors: Namal Chithranga Warshakoon, Rodney Dean Bush
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Publication number: 20100298271Abstract: Compound of Formula I or a salt thereof for treating cancer, wherein X represents CH or N; R1 represents hydrogen or —CH2COR5; R5 represents hydroxy, optionally hydroxylated alkoxy, amino or alkylamido; R2 represents ZYR6; Z represents a bond, or a C1-3 alkylene or oxoalkylene group optionally substituted by R7; Y represents a bond, an oxygen atom or NR6; R6 is a hydrogen atom, COOR8, an alkyl, alkenyl, cycloalkyl, aryl or aralkyl group optionally substituted by one or more selected from COOR8, CONR82, NR82, OR8, ?NR8, ?O, OP(O)(OR8)R7 and OSO3M; R7 is hydroxy, an optionally hydroxylated, optionally alkoxylated alkyl or aminoalkyl group; R8 is a hydrogen atom or an optionally hydroxylated, optionally alkoxylated alkyl group; M is a hydrogen atom or one equivalent of a physiologically tolerable cation; R3 represents C1-8 alkylene, 1,2-cykloalkylene, or 1,2-arylene, optionally substituted with R7; and R4 represents hydrogen or C1-3 alkyl.Type: ApplicationFiled: December 12, 2008Publication date: November 25, 2010Applicant: PLEDPHARMA ABInventors: Jan Olof G. Karlsson, Tino Kurz, Rolf Andersson
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Publication number: 20100298270Abstract: Described herein are novel HDAC modulators, formulations containing them and methods of using them. In some embodiments, the HDAC modulators possess specific stereo chemistry. In other embodiments, the compounds described herein are used in the treatment or prevention of histone deacetylase mediated disorders.Type: ApplicationFiled: July 23, 2008Publication date: November 25, 2010Applicant: SYNDAX PHARMACEUTICALS, INC.Inventors: John F.W. Keana, Peter Ordentlich, Robert Goodenow
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Patent number: 7838536Abstract: Disclosed herein are novel zinc ionophores, zinc chelators and/or zinc complexes with enhanced aqueous solubility. Methods of treating cancer using at least one zinc ionophore and/or zinc chelator are also disclosed. Also disclosed herein are compositions and methods for treating cancer with combination therapy using at least one texaphyrin metal complex and at least one zinc ionophore or the respective pharmaceutically acceptable derivatives or salts thereof.Type: GrantFiled: March 24, 2009Date of Patent: November 23, 2010Inventors: Darren Magda, Jonathan L. Sessler
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Publication number: 20100286206Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.Type: ApplicationFiled: September 12, 2008Publication date: November 11, 2010Applicants: ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC., ADDEX PHARMA, S.A.Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James Macdonald, Guillaume Albert Jacques Duvey, Robert Johannes Lutjens, Patrick Terry Finn
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Publication number: 20100280036Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100272677Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5a, R5b, R5c and R6 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: April 23, 2010Publication date: October 28, 2010Inventors: Eun Kyung Lee, Ryan Craig Schoenfeld, Francisco Xavier Talamas
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Publication number: 20100266539Abstract: The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.Type: ApplicationFiled: March 25, 2010Publication date: October 21, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Hiroshi Ochiai, Natsuko Tokuda, Shiro Shibayama, Noriki Watanabe, Takaki Komiya, Kazuhiko Takeda
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Publication number: 20100261902Abstract: Chelating monomers and fluoride-releasing compositions are disclosed that may be incorporated into dental composite restorative materials, dental bonding agents or other dental materials, to produce materials with high fluoride release rates, and high fluoride recharge capability. Such dental restorative materials may help reduce the level of dental caries in patients, particularly the level of caries occurring on the margins of the restorative materials.Type: ApplicationFiled: February 12, 2008Publication date: October 14, 2010Applicant: BOARD OF SUPERVISORS OF LOUISIANA STATE UNIVERSITYInventors: Xiaoming Xu, Shailaja Jayaramachandran, Liang Chen
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Publication number: 20100249077Abstract: The present invention relates to novel pyridylmethyl-sulfonamide compounds of formula (I) where: n is 0 to 4; m is 0 to 4; R1 is halogen, CN, NO2, OH, SH, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, etc.; and/or two radicals R1 together form a fused ring; R2 is H, C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C2-C4-alkynyl, C3-C8-cycloalkyl, C1-C4-alkyl-C3-C8-cycloalkyl or benzyl; R3 is halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy; Y is —O—, C1-C4-alkanediyl, —O—CH2—, —CH2—O—, —C(NORn)—, —S—, —S(?O)—, —S(?O)2— or —N(Rn)—; and the N-oxides, and salts thereof and their use for combating phytopathogenic harmful fungi, and also to compositions and seed comprising at least one such compound.Type: ApplicationFiled: November 21, 2008Publication date: September 30, 2010Applicant: BASF SEInventors: Wassilios Grammenos, Jan Klaas Lohmann, Thomas Grote, Jochen Dietz, Bernd Mueller, Michael Puhl, Jens Renner, Sarah Ulmschneider, Marianna Vrettou, Joachim Rheinheimer
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Publication number: 20100233190Abstract: The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.Type: ApplicationFiled: March 12, 2009Publication date: September 16, 2010Applicant: ENZON PHARMACEUTICALS, INC.Inventors: Hong ZHAO, Maria Belen RUBIO, Pasanna Reddy
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Publication number: 20100234429Abstract: The invention relates to substituted nicotinamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.Type: ApplicationFiled: March 10, 2010Publication date: September 16, 2010Applicant: GRÜNENTHAL GMBHInventors: Sven Kühnert, Beatrix Merla, Gregor Bahrenberg, Wolfgang Schröder
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Publication number: 20100234428Abstract: The invention relates to substituted 2-mercapto-3-aminopyridines, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.Type: ApplicationFiled: March 10, 2010Publication date: September 16, 2010Applicant: GRUNENTHAL GMBHInventors: Sven Kühnert, Beatrix Merla, Achim Kless, Gregor Bahrenberg, Wolfgang Schröder
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Patent number: 7786130Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: August 28, 2006Date of Patent: August 31, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Sharn Ramaya, Steven Durrant, Juan-Miguel Jimenez, Guy Brenchley, Ronald Knegtel, Michael Mortimore
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Publication number: 20100216758Abstract: An active ingredient is a compound represented by the general formula [I]: [wherein R1 and R2 represent a lower alkyl group, a C3-6 cycloalkyl group or the like, X1 and X2 represent methine, an Ar—Y1—Y2—Y3-substituted methine or the like, however either of them is an Ar—Y1—Y2—Y3-substituted methine, X3 to X8 represent methine, —N— or the like, Y1 and Y3 represent a single bond, —O— or the like, Y2 represent a single bond, a lower alkylene group or the like, W represent —(O)—(CH2)n-(O)— or the like, n represents an integer of 1 to 4, L and Z2 represent a single bond or a methylene group, Z1 represents a single bond, a C1-4 alkylene group or the like, and Ar represents an aromatic carbocyclic group or the like]. The compound acts as a melanin-concentrating hormone receptor antagonist and useful as a therapeutic agent for obesity or the like.Type: ApplicationFiled: August 3, 2006Publication date: August 26, 2010Inventors: Makoto Ando, Etsuko Sekino, Yuji Haga, Norikazu Otake, Minoru Moriya