Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Pyridine Or Partially Hydrogenated Pyridine Ring Patents (Class 546/262)
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Patent number: 8455654Abstract: A nanoscale pigment particle composition includes an organic benzimidazolone pigment, and a sterically bulky stabilizer compound, wherein the benzimidazolone pigment associates non-covalently with the sterically bulky stabilizer compound that is a substituted pyridine derivative; and the presence of the associated stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.Type: GrantFiled: July 18, 2011Date of Patent: June 4, 2013Assignees: Xerox Corporation, National Research Council of CanadaInventors: Rina Carlini, Darren Andrew Makeiff
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Publication number: 20130137660Abstract: The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFR?, PDGFR? or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: January 22, 2013Publication date: May 30, 2013Applicant: YM Biosciences Australia Pty LtdInventor: YM Biosciences Australia Pty Ltd
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Publication number: 20130116430Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.Type: ApplicationFiled: December 28, 2012Publication date: May 9, 2013Applicant: FUJIFILM CORPORATIONInventors: Hideyasu FUJIWARA, Kimihiko SATO, Shinsuke MIZUMOTO, Yuichiro SATO, Hideki KURIHARA, Yohei KUBO, Hiyoku NAKATA, Yasutaka BABA, Takashi TAMURA, Hidenobu KUNIYOSHI, Shinji HAGIWARA, Mari YAMAMOTO
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Publication number: 20130065911Abstract: The present invention relates to compounds of the formula wherein R1 to R3 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 10, 2012Publication date: March 14, 2013Inventors: Uwe Grether, Stephan Roever
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Publication number: 20130053417Abstract: The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity, the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.Type: ApplicationFiled: March 21, 2012Publication date: February 28, 2013Applicant: JAPAN TOBACCO INC.Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
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Publication number: 20130035339Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).Type: ApplicationFiled: September 13, 2012Publication date: February 7, 2013Applicant: Gilead Sciences, IncInventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, JR., Gregory Notte
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Publication number: 20120316147Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: June 1, 2012Publication date: December 13, 2012Inventors: Caterina Bissantz, Uwe Grether, Paul Hebeisen, Atsushi Kimbara, Qingping Liu, Matthias Nettekoven, Marco Prunotto, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch, Christoph Ullmer, Zhiwei Wang, Wulun Yang
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Patent number: 8329732Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: GrantFiled: August 31, 2009Date of Patent: December 11, 2012Assignee: Novartis AGInventors: Matthew T. Burger, Wooseok Han, Jiong Lan, Gisele Nishiguchi
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Publication number: 20120295889Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: May 16, 2012Publication date: November 22, 2012Applicant: Merck Serono S.A.Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
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Publication number: 20120295902Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: December 17, 2010Publication date: November 22, 2012Applicant: MERCK PATENT GMBHInventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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Publication number: 20120270885Abstract: The use of a compound of formula I Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; the ring is a 6 membered aromatic ring or is a 5 or 6 membered heteroaromatic ring; Z and Z? are provided that both are not N; R1, R2, R3, R3a, R4, R8 and Ra are specified organic groups and n and p are independently 0, 1, 2, 3 or 4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.Type: ApplicationFiled: February 10, 2012Publication date: October 25, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Peter Maienfisch, Louis-Pierre Molleyres, Jérôme Cassayre, Fredrik Cederbaum, Camilla Corsi, Thomas Pitterna
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Publication number: 20120270852Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; R3 is hydrogen, methyl, halogen or nitrile; R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy; R2/R2? are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2? together with the N-atom to which they are attached form a morpholine ring, a piperidine ring or an azetidine ring, each of which is unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy and methyl; R4/R4? are each independently hydrogen or lower alkyl, or R4 and R4? together form a C3-5 cycloalkyl-, tetrahydrofuran- or an oxetane-ring; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.Type: ApplicationFiled: April 11, 2012Publication date: October 25, 2012Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20120230978Abstract: The present invention relates to a modulator of glucocorticoid biosynthesis, degradation and/or receptor activation for use in preventing or treating symptoms and/or diseases associated with jet lag. The compositions of the invention may be used as a lead compound for developing a drug for preventing or treating symptoms and/or diseases associated with jet lag. The invention relates to the discovery that administration of the modulator(s) to a subject results in a directional change of the time point of maximum amounts of glucocorticoids in the subject as compared to the time point of maximum amounts of glucocorticoids in a subject not treated with the modulator(s).Type: ApplicationFiled: March 7, 2012Publication date: September 13, 2012Applicant: Max-Planck-Gesellschaft-zur-Forderung der Wissenschaften e.V.Inventors: Gregor Eichele, Henrik Oster, Silke Kiessling
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Publication number: 20120225062Abstract: The present invention provides compounds of Formula I: and related compounds as further described herein, and pharmaceutical compositions comprising these compounds. The invention further provides methods to use these compounds and compositions for treating disorders associated with undesired levels of Pim kinase activity, including cancers and autoimmune disorders.Type: ApplicationFiled: March 2, 2012Publication date: September 6, 2012Inventors: Matthew Burger, Gisele Nishiguchi, Timothy D. Machajewski, Alice Rico, Robert Lowell Simmons, Aaron R. Smith, Victoriano Tamez, JR., Huw Tanner, Lifeng Wan
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Publication number: 20120225061Abstract: The present invention provides a compound of formula (I): as further described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: March 1, 2012Publication date: September 6, 2012Inventors: Matthew Burger, Yu Ding, Wooseok Han, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Aaron R. Smith, Victoriano Tamez, JR., Huw Tanner, Lifeng Wan
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Publication number: 20120214799Abstract: 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: ApplicationFiled: April 9, 2012Publication date: August 23, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Guy Bemis, Francois Maltais, Tiansheng Wang, Ronald Knegtel, Chris Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Mortimore
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Patent number: 8247404Abstract: The present invention relates to derivatives of 4-{2-[phenyl-3,6-dihydropyridin-1-yl]-2-oxoalkyl}-1-piperazin-2-one and 4-{2-[phenyl-2,5-dihydropyrrol-1-yl]-2-oxoalkyl}-1-piperazin-2-one having general formula (I): in which A, B, m, R3 and n are as defined herein. The invention also relates to the preparation thereof and to the therapeutic use thereof.Type: GrantFiled: December 13, 2010Date of Patent: August 21, 2012Assignee: SanofiInventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart
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Patent number: 8242140Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: GrantFiled: July 31, 2008Date of Patent: August 14, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Pierre L. Beaulieu, Paul J. Edwards, Martin Poirier, Jean Rancourt, Timothy A. Stammers
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Publication number: 20120190686Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: ApplicationFiled: December 22, 2011Publication date: July 26, 2012Applicant: H. LUNDBECK A/SInventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
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Patent number: 8212025Abstract: An improved process for preparing 11-cyclopropyl-5,11-dihydro-4-methyl-6H-dipyrido[3,2-b:2?,3?-e][1,4]diazepin-6-one of Formula (I).Type: GrantFiled: May 14, 2008Date of Patent: July 3, 2012Assignee: Aurobindo Pharma Ltd.Inventors: Jagan Mohan Reddy Sanapureddy, Ramesh Dandala, Sivakumaran Meenakshisunderam
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Publication number: 20120165343Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: December 22, 2011Publication date: June 28, 2012Applicant: Pfizer Inc.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20120134987Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: December 15, 2011Publication date: May 31, 2012Inventors: Matthew T. Burger, Wooseok Han, Jiong Lan, Gisele Nishiguchi
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Publication number: 20120094980Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: ApplicationFiled: October 14, 2011Publication date: April 19, 2012Inventors: Janet L. Gunzner, Daniel P. Sutherlin, Mark S. Stanley, Liang Bao, Georgette Castanedo, Rebecca Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina, Michael F.T. Koehler
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Publication number: 20120094986Abstract: The invention relates to nicotinamide derivatives which can be used as anticancer drugs.Type: ApplicationFiled: March 22, 2010Publication date: April 19, 2012Applicant: SANOFI-AVENTISInventors: Jérôme Arigon, Claude Bernhart, Monsif Bouaboula, Romain Combet, Sandrine Hilairet, Samir Jegham
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Patent number: 8143406Abstract: The invention provides a process for the manufacture of HI 6 dimethanesulfonate comprising contacting an O-protected pyridine aidoxime compound with bis(methylsulphonoxymethyl)ether in a suitable solvent to form an intermediate compound, contacting said intermediate compound with isonicotinamide to form an O-protected HI 6 product precursor, and de-protecting the precursor to form HI 6 dimethanesulfonate.Type: GrantFiled: August 22, 2007Date of Patent: March 27, 2012Assignee: Phoenix Chemicals LimitedInventors: Jonathan Eddolls, Peter McCormack, Anne Hodgson
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Publication number: 20120053209Abstract: The invention relates to nicotinamide derivatives that can be used as anticancer drugs.Type: ApplicationFiled: March 18, 2010Publication date: March 1, 2012Applicant: SANOFIInventors: Jerome Arigon, Claude Bernhart, Monsif Bouaboula, Romain Combet, Samir Jegham, Sandrine Hilairet
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Publication number: 20120053170Abstract: The present invention relates to nicotinamide derivatives of formula (I), to compositions containing same, and to the therapeutic use thereof, in particular as anticancer drugs. The invention also relates to the method for preparing said compounds, as well as to some of the intermediate products.Type: ApplicationFiled: March 22, 2010Publication date: March 1, 2012Applicant: SANOFIInventors: Jérome Arigon, Claude Bernhart, Monsif Bouaboula, Romain Combet, Sandrine Hilairet, Samir Jegham
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Publication number: 20120015961Abstract: The present invention provides, for example, a compound of the following formula (I): wherein R1 is substituted amino and the like, R2 is halogen and the like, R3 is substituted or unsubstituted lower alkyl and the like, RA and RB are each independently hydrogen, substituted or unsubstituted lower alkyl and the like, RC and RD are each independently hydrogen, substituted or unsubstituted lower alkyl, or RC and RD together with the carbon atom to which they are attached may form a substituted or unsubstituted carbocycle, and ring A is a carbocycle or a heterocycle, its pharmaceutically acceptable salt, or a solvate thereof as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-?proteins.Type: ApplicationFiled: March 29, 2010Publication date: January 19, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Yuusuke Tamura, Shinji Suzuki, Sae Matsumoto, Akihiro Hori, Yuuji Kooriyama
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Publication number: 20110315933Abstract: The present invention relates to metal complexes of the general formulae I to V, in particular as emitter molecules in organic electronic devices, to ligands of the general formulae Ia to Va, and to the use thereof for the preparation of metal complexes, to a layer and an electronic device which comprise the compounds according to the invention, and to a process for the preparation of the compounds according to the invention.Type: ApplicationFiled: February 15, 2010Publication date: December 29, 2011Applicant: MERCK PATENT GMBHInventors: Philipp Stoessel, Holger Heil, Dominik Joosten, Christof Pflumm, Anja Gerhard
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Publication number: 20110319616Abstract: An object is to provide a thiazole derivative produced from easily available raw materials by a simplified production process. Provided are a process for producing a novel thiazole derivative represented by the general formula (I), which is characterized by adding a strong base to a thioamide represented by the general formula (II) and reacting the mixture with a thioformamide represented by the general formula (III), and a novel thiazole derivative.Type: ApplicationFiled: March 8, 2010Publication date: December 29, 2011Applicant: GIFU UNIVERSITYInventor: Toshiaki Murai
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Publication number: 20110313000Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: August 30, 2011Publication date: December 22, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Publication number: 20110306597Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the treatment of allergic and respiratory conditions.Type: ApplicationFiled: June 12, 2009Publication date: December 15, 2011Inventors: James Michael Crawforth, Paul Alan Glossop, Bruce Cameron Hamper, Wei Huang, Bradley Elwood Neal, Simon John Mantell, Kirk Olson, Atli Thorarensen, Steve Ronald Turner
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Publication number: 20110288129Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, and R3, are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: July 8, 2011Publication date: November 24, 2011Applicant: ABBOTT LABORATORIESInventors: Anil Vasudevan, Brian S. Brown, Jerome F. Daanen, Arthur R. Gomtsyan, Tammie K. Jinkerson, Ryan G. Keddy, Michael E. Kort, Philip R. Kym, Mark A. Matulenko
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Patent number: 8063036Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 7, 2010Date of Patent: November 22, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Publication number: 20110275797Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.Type: ApplicationFiled: January 29, 2010Publication date: November 10, 2011Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
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Patent number: 8053212Abstract: This invention relates to nucleoside, nucleotide, and oligonucleotide analogs that incorporate non-standard nucleobase analogs, defined to be those that present a pattern of hydrogen bonds to a paired nucleobase analog in a complementary strand that is different from the pattern presented by adenine, guanine, cytosine, and thymine. The invention is specifically concerned with compositions of matter that present the donor-donor-acceptor, donor-acceptor-donor, and acceptor-donor-donor non-standard hydrogen bonding patterns on pyrimidine analogs, where nucleoside analogs bearing these pyrimidine analogs do not epimerize as easily as those known in the art. The heterocycles on these nucleoside analogs are diaminopyridines and aminopyridones that have electron withdrawing groups attached to the position analogous to the 5-position of the ring in standard pyrimidines, including nitro, cyano, and carboxylic acid derivatives.Type: GrantFiled: March 9, 2006Date of Patent: November 8, 2011Inventor: Steven Albert Benner
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Publication number: 20110263564Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: October 29, 2009Publication date: October 27, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Radha Narayan, Jeremy S. Disch, Robert B. Perni, Chi B. Vu
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Publication number: 20110237576Abstract: The present invention provides a compound which has an effect of inhibiting amyloid-? production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-? proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein A is optionally substituted carbocyclic diyl or optionally substituted heterocyclic diyl; B is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is a group such as optionally substituted lower alkyl; R2 is a group such as hydrogen; and R3a and R3b are each independently a group such as hydrogen, provided that the following compound is excluded.Type: ApplicationFiled: October 22, 2009Publication date: September 29, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Shuji Yonezawa, Yuusuke Tamura, Yuuji Kooriyama, Gaku Sakaguchi
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Publication number: 20110224204Abstract: Di-substituted phenyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. The disclosure also relates to methods for treating neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 25, 2009Publication date: September 15, 2011Inventors: Richard Chesworth, Gideon Shapiro, Amy Ripka
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Publication number: 20110224124Abstract: The invention is to pH tuneable amido-gellant that are suitable for use in consumer product compositions.Type: ApplicationFiled: March 11, 2011Publication date: September 15, 2011Inventors: Susana FERNANDEZ PRIETO, Johan Smets, Beatriu Escuder Gil, Juan Felipe Miravet Celades, Vincent Josep Nebot Carda
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Publication number: 20110206783Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: ApplicationFiled: October 21, 2009Publication date: August 25, 2011Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw
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Patent number: 8003797Abstract: The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: GrantFiled: August 7, 2008Date of Patent: August 23, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Jeffrey M. Bergman, Paul J. Coleman, Mark E. Fraley, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker, Justin T. Steen
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Publication number: 20110201591Abstract: The present invention is directed to isonicotinamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: October 26, 2009Publication date: August 18, 2011Inventors: Jeffrey M. Bergman, Paul J. Coleman, Mamio Christa Mattern, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker
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Publication number: 20110195999Abstract: The present invention provides an antifungal agent represented by the formula: wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula —NH—C(?O)—, a group represented by the formula —C(?O)—NH—, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents.Type: ApplicationFiled: March 14, 2011Publication date: August 11, 2011Inventors: Kazutaka NAKAMOTO, Itaru Tsukada, Keigo Tanaka, Masayuki Matsukura, Toru Haneda, Satoshi Inoue, Norihiro Ueda, Shinya Abe, Katsura Hata, Naoaki Watanabe
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Publication number: 20110184023Abstract: The present invention relates to the salts of N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl) amino-3-pyridine carboxamide, especially hydrochloride and mesylate thereof, and the use of said salts in the preparation of an antineoplastic medicament.Type: ApplicationFiled: June 11, 2009Publication date: July 28, 2011Applicant: Jiangsu Hengrui Medicine Co., Ltd.Inventors: Kaihong Yuan, Piaoyang Sun, Yunshu Zhou, Yongjiang Chen
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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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Patent number: 7947680Abstract: The present invention provides adamantyl-diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: GrantFiled: July 17, 2009Date of Patent: May 24, 2011Assignee: H. Lundbeck A/SInventors: Hermogenes N. Jimenez, Guiying Li, Dario Doller, Michel Grenon, Andrew D. White, Gil Ma, Maojun Guo
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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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Patent number: 7939548Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: GrantFiled: July 31, 2007Date of Patent: May 10, 2011Assignee: Cytokinetics, Inc.Inventors: Pu-Ping Lu, Xiangping Qian, Chihyuan (Grace) Chuang, Bradley P. Morgan, David J. Morgans, Jr.
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Publication number: 20110098476Abstract: Disclosed herein are methods of preparing a bis(thio-hydrazide amides) compounds of the following structural formula: wherein R1, R2, R3, R4, R5, R6 and R13 are defined herein.Type: ApplicationFiled: March 31, 2009Publication date: April 28, 2011Inventors: Shoujun Chen, Jun Jiang, Lijun Sun, Keizo Koya