Plural Double Bonds Between Ring Members Of The Oxazole Ring Patents (Class 548/247)
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Publication number: 20110028447Abstract: This invention relates to compounds, pharmaceutical compositions and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) wherein R1, R2 and R3 are as defined in this specification.Type: ApplicationFiled: February 26, 2009Publication date: February 3, 2011Inventors: Ingrid Price Buchler, Michael Joseph Hayes, Shridhar Gajanan Hegde, Susan Landis Hockerman, Darin Eugene Jones, Steven Wade Kortum, Joseph Gerace Rico, Ruth Elizabeth TenBrink, Kun Ken Wu
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Publication number: 20110018866Abstract: The present invention provides compositions comprising the ligand binding domain (LBD) of a farnesoid X receptor (FXR) in crystalline form. In alternative embodiments, the LBD of FXR is complexed with a ligand therefor. There are provided high resolution structures of FXR complexed with a novel high affinity agonist fexaramine. The discovered structure of a FXR LBD provides the first three-dimensional view of the structural basis for FXR ligand binding. The present invention further provides a computer for producing a time-dimensional representation of FXR or a complex thereof, and a computer for determining at least a portion of the structure coordinates of FXR or a complex thereof. The present invention further provides methods of using this structural information to predict molecules capable of binding to FXR; to identify compounds with agonist, antagonist or partial agonist activity for FXR; and to determine whether a test compound is capable of binding to the LBD of FXR.Type: ApplicationFiled: January 12, 2010Publication date: January 27, 2011Inventors: Michael R. Downes, Mark A. Verdicia, Joseph P. Noel, Ronald M. Evans, Lindsey J. Bowman, Marianne Bowman
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Patent number: 7875618Abstract: The invention relates to imidazo[1,5-a]quinoxaline derivatives having Formula IIa: to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.Type: GrantFiled: November 25, 2008Date of Patent: January 25, 2011Assignees: Wyeth, elbion GmbHInventors: Michael S. Malamas, Yike Ni, James Joseph Erdei, Norbert Höfgen, Hans Stange, Rudolf Schindler, Ute Egerland, Barbara Langen
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Patent number: 7868031Abstract: The present invention relates to propionamide compounds of formula I for use as antiinflammatory agents: wherein R1, R2 and R3 are as defined herein and pharmaceutically acceptable salts thereof. The invention also relates to methods of using the compounds of formula I and pharmaceutical compositions comprising the compounds of formula I.Type: GrantFiled: December 8, 2006Date of Patent: January 11, 2011Assignee: Roche Palo Alto LLCInventors: Leyi Gong, Counde O'Yang, Yun-chou Tan
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Patent number: 7863302Abstract: Compounds of formula and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.Type: GrantFiled: February 2, 2007Date of Patent: January 4, 2011Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Michael James Genin, Peter Ambrose Lander, Lindsay Scott Stelzer, Robert Anthony Doti, Francisco Javier Agejas-Chicharro, Ana Belen Bueno Melendo, Peter Rudolph Manninen, Jason Matthew Ochoada, Quanrong Shen, Alan M. Warshawsky, Tianwei Ma, Ryan Edward Stites
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Patent number: 7863334Abstract: The present invention relates to compounds having the formula: salts thereof; compositions comprising one or more of the compounds and/or salts thereof; methods of using; and methods of making.Type: GrantFiled: September 17, 2007Date of Patent: January 4, 2011Assignee: Cytokine PharmaSciences, Inc.Inventor: Thais M. Sielecki-Dzurdz
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Patent number: 7863308Abstract: Disclosed herein are substituted pyrimidine-based endothelin modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: April 10, 2008Date of Patent: January 4, 2011Assignee: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. Gant, Sepehr Sarshar
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Patent number: 7851469Abstract: The present invention is concerned isoxazole-imidazole derivatives having affinity and selectivity for GABA A ?5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use for enhancing cognition or for the treatment of cognitive disorders like Alzheimer's disease. In particular, the present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I wherein R1, R2 and R3 are as described in the specification.Type: GrantFiled: June 16, 2008Date of Patent: December 14, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas
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Patent number: 7846950Abstract: The present invention provides novel compounds with histamine-H3 receptor antagonist or inverse agonist activity. In particular, the invention provides a compound of Formula I, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and intermediates and methods for making these compounds. The invention provides methods of using compounds and pharmaceutical compositions to treat obesity, cognitive deficiences, narcolepsy, and other histamine H3 receptor-related diseases.Type: GrantFiled: October 11, 2005Date of Patent: December 7, 2010Assignee: Eli Lilly and CompanyInventors: Cynthia Darshini Jesudason, Freddie Craig Stevens
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Patent number: 7846956Abstract: The present invention provides a malononitrile compound represented by the formula (I): wherein any one of X1, X2, X3 and X4 is CR100, wherein R100 is a group represented by the formula: the other three of X1, X2, X3 and X4 each represent nitrogen or CR5, provided that 1 to 3 of X1, X2, X3 and X4 represent nitrogen, and Z represents oxygen, sulfur or NR6, which has pest-controlling activity.Type: GrantFiled: January 13, 2005Date of Patent: December 7, 2010Assignee: Sumitomo Chemical Company, LimitedInventors: Hiromasa Mitsudera, Ken Otaka, Jun Fujiwara
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Patent number: 7834188Abstract: N-Substituted sulfoximines are effective at controlling insects.Type: GrantFiled: November 11, 2009Date of Patent: November 16, 2010Assignee: Dow AgroSciences LLCInventors: Yuanming Zhu, Richard B. Rogers, Jim X. Huang
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Publication number: 20100286115Abstract: The present invention is concerned with isoxazole-pyrazoles of formula I, having affinity and selectivity for GABA A a5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutics. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: ApplicationFiled: April 28, 2010Publication date: November 11, 2010Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Publication number: 20100286103Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: July 31, 2008Publication date: November 11, 2010Inventor: Shoujun Chen
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Patent number: 7829719Abstract: N-Substituted sulfoximines are effective at controlling insects.Type: GrantFiled: November 11, 2009Date of Patent: November 9, 2010Assignee: Dow AgroSciences LLCInventors: Yuanming Zhu, Richard B. Rogers, Jim X. Huang
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Publication number: 20100280073Abstract: The present invention provides tricyclic compounds according to formula (I): (I) where R1, R2, R3, W, X, Y, Z, m, n, and p are as defined in the description; as well as pharmaceutical compositions comprising the same, methods of use of the compounds and compositions of the invention for the treatment of conditions associated with hydroxysteroid dehydrogenases (e.g., 11-HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.Type: ApplicationFiled: June 11, 2008Publication date: November 4, 2010Applicant: Amgen Inc.Inventors: Jay P. Powers, Daqing Sun, Xuelei Yan, Lisa Julian, Felix Gonzalez Lopez De Turiso
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Publication number: 20100279868Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds of formula (I), which are suitable for use as herbicides.Type: ApplicationFiled: June 26, 2008Publication date: November 4, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Stephane Andre Marie Jeanmart, Christopher John Mathews, Steve Smith, John Benjamin Taylor, Mangala Govenkar
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Patent number: 7825146Abstract: A compound represented by the general formula (I-A): wherein R1 is hydroxy and the like; R2 is optionally substituted lower alkyl and the like; R3 is hydrogen atom and the like; R4 is optionally substituted arylene and the like; R5 is a group represented by the formula: R6 is optionally substituted aryl and the like, its optically active substance, their pharmaceutically acceptable salt, or a solvate thereof; and a metalloproteinase inhibitor containing them.Type: GrantFiled: July 28, 2004Date of Patent: November 2, 2010Assignee: Shionogi & Co., Ltd.Inventors: Fumihiko Watanabe, Naoki Yoshikawa, Yoshinori Tamura
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Patent number: 7825142Abstract: Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.Type: GrantFiled: August 24, 2009Date of Patent: November 2, 2010Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Jeffrey Bagdanoff, Simon D. P. Baugh, Kenneth G. Carson, Theodore C. Jessop, James E. Tarver
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Publication number: 20100272656Abstract: A method of providing a range of flavors to an orally-receivable or ingestible product, the method including adding at least one compound, including salts thereof, of the formula: wherein R1 may be H, OH, O(CH2)2OH, OCH2OCH3 or R2 may be selected from a range of 5- and 6-membered heterocyclic rings, and wherein R3 may be H or OH. The compounds give rise to a wide range of flavors, and some are useful as sweetness enhancers, this allowing sweetener content to be reduced while maintaining sweetness. Also disclosed are orally-receivable or ingestible products including the compounds.Type: ApplicationFiled: June 7, 2010Publication date: October 28, 2010Inventors: Andrew DANIHER, Yili Wang
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Publication number: 20100261772Abstract: The present invention relates to compounds of formula (I) with a variety of therapeutic uses, more particularly the substituted cyclic alkylidene compounds are useful for selective estrogen receptor modulation.Type: ApplicationFiled: May 24, 2010Publication date: October 14, 2010Inventors: Jing Fang, Dennis Heyer, Subba Reddy Katamreddy, Kenneth William Batchelor, Richard Dana Caldwell
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Publication number: 20100254916Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: ApplicationFiled: February 19, 2010Publication date: October 7, 2010Applicant: Senomyx, Inc.Inventors: Donald S. Karanewsky, Joseph Fotsing, Catherine Tachdjian, Melissa Arellano
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Publication number: 20100249179Abstract: The present invention provides novel isoxazole compounds, pharmaceutical compositions, therapeutic uses and processes for preparing the same.Type: ApplicationFiled: June 13, 2008Publication date: September 30, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: David Norman Deaton, Frank Navas, III, Paul Kenneth Spearing
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Publication number: 20100249192Abstract: Heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer; liver steatosis; and non-alcoholic steatohepatitis.Type: ApplicationFiled: December 9, 2008Publication date: September 30, 2010Inventors: Chun Sing Li, Yeeman K. Ramtohul, Jean-Philippe Leclerc
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Publication number: 20100240722Abstract: There is provided a fluorine-containing organosulfur compound having an excellent controlling effect m represents 0 or 1; n represents 0, 1 or 2; A represents an optionally substituted 5-membered aromatic heterocyclic group; R1 and R3 are independently represent an optionally substituted C1-C4 chain hydrocarbon group, —C(=G)R5, cyano, halogen or hydrogen; R2 and R4 independently represent an optionally substituted C1-C4 chain hydrocarbon group, halogen or hydrogen; Q represents a C1-C5 haloalkyl group containing at least one fluorine, or fluorine; G represents oxygen or sulfur; and R5 represents optionally substituted C1-C4 alkyl, hydroxyl, optionally substituted C1-C4 alkoxy, optionally substituted C3-C6 alkenyloxy, optionally substituted C3-C6 alkynyloxy, amino, optionally substituted C1-C4 alkylamino, optionally substituted di(C1-C4 alkyl)amino, C2-C5 cyclic amino or hydrogen.Type: ApplicationFiled: August 28, 2008Publication date: September 23, 2010Applicant: Sumitomoo Chemical Company, LimitedInventors: Koji Kumamoto, Hiroyuki Miyazaki
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Patent number: 7799812Abstract: The present invention relates to polycyclic compounds, processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: January 25, 2007Date of Patent: September 21, 2010Assignee: Novartis AGInventors: Rainer Albert, Frederic Zecri
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Patent number: 7790759Abstract: The present invention relates to the field of a medicine for treating diseases associated with inflammation, immunity or infection, and in particular, to glycyrrhetinic acid-30-amide derivatives of general formula I and their preparation, and a pharmaceutical composition containing the same. Said derivatives and composition exhibit anti-inflammatory, analgesic, anti-allergic, cough-preventing, liver-protecting and anti-viral properties, wherein each group is as defined in the description.Type: GrantFiled: October 16, 2006Date of Patent: September 7, 2010Assignee: Tianjin Institute of Pharmaceutical ResearchInventors: Jianwu Wang, Weiren Xu, Jianping Wong, Lida Tang, Shijun Zhang, Lijun Liu, Yuli Wang, Xiaowen Ren
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Publication number: 20100221215Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 9, 2010Publication date: September 2, 2010Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Patent number: 7786155Abstract: The invention relates to compound of the formula I wherein the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: GrantFiled: October 15, 2008Date of Patent: August 31, 2010Assignee: Novartis AGInventors: Joachim Nozulak, David Orain
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Patent number: 7781469Abstract: A compound of the formula (I): pharmaceutically acceptable salt or solvate thereof, wherein Y is a group of the formula: wherein Ring A is optionally substituted aryl or optionally substituted heteroaryl, X3 is COOR17 or the like Y is not optionally substituted phenyl which is substituted with the formula: —CR9R10X3 at the para position, R1 to R10 are each independently halogen, hydroxy, optionally substituted lower alkyl, optionally substituted aryl or the like, X1 is —O—, —S— or the like.Type: GrantFiled: May 23, 2006Date of Patent: August 24, 2010Assignee: Shionogi & Co., Ltd.Inventor: Yasuhiko Kanda
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Publication number: 20100210680Abstract: The present invention relates to a tricyclic heterocyclic derivative of Formula (I) wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment of serotonin-mediated disorders such as obesity, schizophrenia and cognitive dysfunction.Type: ApplicationFiled: September 15, 2008Publication date: August 19, 2010Inventors: Simon James Anthony Grove, Takao Kiyoi, Ashvinkumar Dhirubhai Mistry, Peter Christopher Ray, Grant Wishart
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Publication number: 20100210524Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, wherein W, X, Y, Z, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15 and R16 are as defined in the specification. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.Type: ApplicationFiled: July 21, 2008Publication date: August 19, 2010Inventors: Theresa Apelqvist, Joakim Löfstedt, Thomas Norin, Mattias Wennerstål, Xiongyu Wu, Lars Hagberg
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Publication number: 20100210632Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.Type: ApplicationFiled: March 28, 2008Publication date: August 19, 2010Inventors: Hiroyuki Kai, Shunji Shinohara, Takayuki Kameyama
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Patent number: 7767670Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein substituted 3-carboxamido isoxazoles compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.Type: GrantFiled: November 15, 2004Date of Patent: August 3, 2010Assignee: Ambit Biosciences CorporationInventors: Shamal A. Mehta, Robert M. Grotzfeld, Zdravko V. Milanov, Andiliy G. Lai, Hitesh K. Patel, David J. Lockhart
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Publication number: 20100184746Abstract: An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R1 represents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while R1 represents aryl or a five- or six-membered monocyclic heterocyclic group; R2 represents a hydrogen atom or C1-6 alkyl; R3 represents C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; R4, R5, and R6 represent a hydrogen atom; R7 represents C1-6 alkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant Streptococcus pneumoniae. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.Type: ApplicationFiled: May 30, 2008Publication date: July 22, 2010Inventors: Eijirou Umemura, Kou Kumura, Satomi Masaki, Kazutaka Ueda, Yoshinari Wakiyama, Yasuo Sato, Mikio Yamamoto, Keiichi Ajito, Takashi Watanabe, Chizuko Kaji
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Patent number: 7759374Abstract: The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).Type: GrantFiled: October 12, 2006Date of Patent: July 20, 2010Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Alexey Rivkin, Fumikiko Yoshimura, Ting-Chao Chou, Ana E. Gabarda, Huajin Dong
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Publication number: 20100179138Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, —SO.sub.Type: ApplicationFiled: February 19, 2010Publication date: July 15, 2010Applicants: Vernalis (Cambridge) Limited, Cancer Research Technology Ltd., The Institute Of Cancer ResearchInventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Publication number: 20100173962Abstract: N-Substituted heteroaryl (substituted)alkyl sulfoximines are effective at controlling insects.Type: ApplicationFiled: March 11, 2010Publication date: July 8, 2010Applicant: DOW AGROSCIENCES LLCInventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Gregory T. Whiteker, Nneka T. Breaux, John F. Daeuble
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Patent number: 7741341Abstract: The present invention relates to compounds of the formula I, wherein R0, R1, R2, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: May 19, 2004Date of Patent: June 22, 2010Assignee: sanofi-aventis Deutschland GmbHInventors: Marc Nazare, Michael Wagner, Volkmar Wehner, Hans Matter, Matthias Urmann, Kurt Ritter
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Publication number: 20100152252Abstract: The present invention relates to heterocyclyl-substituted-ethylamino-phenyl compounds of general formula (I), wherein K-L-M-N, Z and R1, R2, R3, R4 are as described in the claims methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals.Type: ApplicationFiled: December 21, 2007Publication date: June 17, 2010Applicant: LABORATORIOS DEL DR. ESTEVE,S.A.Inventors: Mónica Garcia-López, Antonio Torrens-Jover, Luz Romero-Alonso, Helmut H. Buschmann
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Publication number: 20100152166Abstract: Compounds of formula (I): formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and diseases related to dyslipidemia.Type: ApplicationFiled: July 11, 2008Publication date: June 17, 2010Applicant: ELI LILLY AND COMPANYInventors: Michael James Genin, Francisco Javier Agejas-Chicharro, Ana Belen Bueno Melendo, Peter Rudolph Manninen, Alan M. Warshawsky
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Patent number: 7732453Abstract: The present invention discloses pyrido[2,3-B]pyrazin-3(4h)-ones for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.Type: GrantFiled: October 5, 2007Date of Patent: June 8, 2010Assignee: Gilead Palo Alto, Inc.Inventors: Dmitry Koltun, Jeff Zablocki, Eric Parkhill, Andrey Glushkov, Natalya Vasilevich, Timur Zilbershtein, Alexey Ivanov
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Publication number: 20100137599Abstract: The present invention relates to a process for the preparation of 1,4-butanediol mononitrate as intermediate for large scale preparation of high purity nitrooxybutyl ester of pharmaceutically active compounds.Type: ApplicationFiled: June 18, 2008Publication date: June 3, 2010Applicant: NICOX S.A.Inventors: Achim Hack, Gunter Weingarner, Matthias Kramer
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Publication number: 20100130497Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof; with the proviso that the compound is not Tranilast.Type: ApplicationFiled: July 5, 2007Publication date: May 27, 2010Applicants: Fibrotech Therapeutics Pty Ltd, The University of MelbourneInventors: Spencer John Williams, David Stapleton, Steven Zammit, Darren James, Richard Ernest, Henry Krum
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NOVEL ORGANOMETALLIC COMPLEXES WHICH EMIT IN THE RED TO GREEN SPECTRAL REGION AND THEIR USE IN OLEDS
Publication number: 20100127215Abstract: Organometallic complexes which bear at least one ligand which has a unit having a triplet energy of at least 22 000 cm?1, a process for preparing the organometallic complexes, a mixture comprising at least one inventive organometallic complex, the use of the organometallic complexes or of the mixture in organic light-emitting diodes, the organometallic complexes preferably being used as emitter materials, and specific nitrogen- or phosphorus-substituted triphenylene derivatives and a process for their preparation.Type: ApplicationFiled: April 4, 2008Publication date: May 27, 2010Applicant: BASF SEInventors: Herbert Friedrich Boerner, Hans-Peter Loebl, Josef Salbeck, Elena Popova -
Patent number: 7723372Abstract: There are provided compounds of the general formulas wherein W, X, Y, R1, R2, R3, and R4 are as described herein. The compounds exhibit anticancer activity.Type: GrantFiled: February 18, 2009Date of Patent: May 25, 2010Assignee: Hoffman-La Roche Inc.Inventor: Jin-Jun Liu
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Patent number: 7723356Abstract: Compounds of Formula (I); in salt or zwitterionic form wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: GrantFiled: October 31, 2005Date of Patent: May 25, 2010Assignee: Novartis AGInventors: Neil John Press, Stephen Paul Collingwood, Urs Baettig, Brian Cox, Sudhakar Devidasrao Garad, Hyungchul Kim, Dimitris Papoutsakis, Simon James Watson
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Patent number: 7714008Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: GrantFiled: September 6, 2007Date of Patent: May 11, 2010Assignee: Amgen Inc.Inventors: Hilary Beck, Paul Dransfield, Zice Fu, Jonathan B. Houze, XianYun Jiao, Todd J. Kohn, SuJen Lai, Jinqian Liu, Jiwen Liu, Zhihua Ma, Julio C. Medina, Michael J. Schmitt, Rajiv Sharma, Wang Shen, Marc Vimolratana, Yingcai Wang, Zhongyu Wang
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Publication number: 20100113423Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: ApplicationFiled: October 19, 2009Publication date: May 6, 2010Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Publication number: 20100113536Abstract: The present invention relates to novel compounds of formula [I], wherein R1 represents heteroaryl, at least one substituent among R5, R6 and R7 represent —SR12, —S(O)R12 or —S(O)2R12 and the remaining substituents are as defined in the claims, that act as chemical uncouplers. Compounds of the invention are useful inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases associated therewith.Type: ApplicationFiled: November 15, 2007Publication date: May 6, 2010Inventors: Anders Klarskov Petersen, Preben Houlberg Olesen, Lise Brown Christiansen, Flemming Elmelund Nielsen
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Publication number: 20100105894Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: ApplicationFiled: June 9, 2009Publication date: April 29, 2010Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafuml Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro