The Additional Hetero Ring Is A Cyclo In A Polycyclo Ring System (e.g., Benzofuranyl-benzimidazole, Etc.) Patents (Class 548/305.1)
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Patent number: 8143421Abstract: The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(?O)—, —O—C(?O)—, —NR8—C(?O)—, —O—C1-6alkanediyl-C(?O)—, —NR8—C1-6alkanediyl-C(?O)—, —S(?O)2—, —O—S(?O)2—, —NR8—S(?O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(?O), carboxyl, aminoC(?O), mono- or di(C1-4alkyl)aminoC(?O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(?O)—, —C(?S)—, —S(?O)2—, C1-6alkanediyl-C(?O)—, C1-6alkanediyl-C(?S)— or C1-6alkanediyl-S(?O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted amino-C1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-Type: GrantFiled: April 27, 2009Date of Patent: March 27, 2012Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Dominique Louis Nestor Ghislain Surleraux, Piet Tom Bert Paul Wigerinck, Marieke Christiane Johanna Diepenbeek Voets, Sandrine Marie Helene Vendeville, Herman Augustinus De Kock, Bernhard Joanna Bernard Vergouwen
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Patent number: 8110578Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: GrantFiled: October 26, 2009Date of Patent: February 7, 2012Assignee: Signal Pharmaceuticals, LLCInventors: Sophie Perrin-Ninkovic, Roy L. Harris, John Sapienza, Graziella Shevlin, Patrick Papa, Branden Lee, Garrick Packard, Lida Tehrani, Jingjing Zhao, Jennifer Riggs, Jason Parnes, Deborah Mortensen, Weiming Xu, Loui Madakamutil, Kimberly Fultz, Rama K. Narla, Sabita Sankar, Jan Elsner
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Publication number: 20120028959Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.Type: ApplicationFiled: March 26, 2010Publication date: February 2, 2012Applicant: MERCK SERONO S.A.Inventors: Siva Sanjeeva Rao Thunuguntla, Hosahalli Subramanya, Satish Reddy Kunnam, Sekhar Reddy Sanivaru Vijay, Chakrapani Bingi, Raviraj Kusanur, Matthias Schwarz, Michael Arlt
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Publication number: 20120015998Abstract: Disclosed herein are compounds represented by a formula: R1—Ar1—X—Ar2—Ar3-Het, wherein R1, Ar1, X, Ar2, Ar3, and Het are described herein. Compositions and light-emitting devices related thereto are also disclosed.Type: ApplicationFiled: July 11, 2011Publication date: January 19, 2012Applicant: Nitto Denko CorporationInventors: Amane Mochizuki, Sazzadur Rahman Khan, Sheng Li, Shijun Zheng, Jensen Cayas, Keisaku Okada, Brett T. Harding
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Publication number: 20120010241Abstract: The invention relates to novel products having formula (I), wherein: R4 represents H, CH3, CH2CH3, CF3, F, Cl, Br, I; Het represents a heterocycle optionally substituted by one or more R1 or R?1 radicals selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalkoxy, alkylthio, carboxy that is free or sterified with an alkyl radical, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, S(O2)-N(alkyl)2, all of the alkyl, alkoxy and alkylthio radicals being optionally substituted; R being selected from the group comprising (A?), (B), (C), (D) and (F), wherein W1, W2, W3 represent independently CH or N, X represents O, S, NR2, C(O), S(O) or S(O)2; V represents H, Hal, —O—R2 or —NH—R2 with R2 representing H, alkyl, cycloalkyl or heterocycloalkyl, optionally substituted; said products being in all isomer forms, as well as the salts and intended for use as drugs.Type: ApplicationFiled: March 18, 2010Publication date: January 12, 2012Applicant: SANOFIInventors: Luc Bertin, Jean-Christophe Carry, Patrick Mailliet, Herve Minoux, Fabienne Pilorge, Jean-Marie Ruxer
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Publication number: 20110312996Abstract: The embodiments provide compounds of the general Formulae VI, VII, VIII, IX, X, XI, XII, XIII, XIV, and XV as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: May 16, 2011Publication date: December 22, 2011Applicant: InterMune, Inc.Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
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Publication number: 20110312949Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: ApplicationFiled: August 30, 2011Publication date: December 22, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
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Publication number: 20110312935Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.Type: ApplicationFiled: September 25, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer, Juergen Mack, Henning Priepke, Dirk Stenkamp
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Publication number: 20110312969Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.Type: ApplicationFiled: December 8, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephen Peter East, Mark Whittaker, Osamu Ichihara, Adrian Kotei Kotei, Smantha Jayne Bamford
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Publication number: 20110309348Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound: wherein R1 through R9 are defined as in the specification.Type: ApplicationFiled: June 20, 2011Publication date: December 22, 2011Applicant: Samsung Mobile Display Co., Ltd.Inventors: Yoon-Hyun KWAK, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jong-Hyuk Lee, Hee-Joo Ko
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Patent number: 8067613Abstract: Compounds which inhibit the activity of poly(ADP-ribose)polymerase (PARP), compositions containing the compounds and methods of treating diseases using them are disclosed.Type: GrantFiled: July 15, 2008Date of Patent: November 29, 2011Assignee: Abbott LaboratoriesInventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D Penning, Gui-Dong Zhu
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Publication number: 20110288139Abstract: The present invention relates to substituted amino-benzimidazoles of general formula (1) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: January 21, 2009Publication date: November 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Klaus Fuchs, Cornelia Dorner-Ciossek, Sandra Handschuh, Niklas Heine, Stefan Hoerer, Klaus Klinder
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Patent number: 8063053Abstract: The invention relates to 1-(arylsulfonyl)-4-(piperazin-1-yl)-1H-benzimidazole compounds of the Formula I: or a tautomer, stereoisomer, or pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.Type: GrantFiled: November 11, 2009Date of Patent: November 22, 2011Assignee: Wyeth LLCInventors: Simon Nicolas Haydar, Patrick Michael Andrae, Heedong Yun, Albert Jean Robichaud
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Publication number: 20110275630Abstract: Compounds having the formula: are useful for inhibiting protein kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: November 3, 2010Publication date: November 10, 2011Applicant: ABBOTT LABORATORIESInventors: Mark Matulenko, Tammie Jinkerson, Brian S. Brown, Wilfried Braje, Michael Curtin, Howard Robin Heyman, Victoria Scott, Karen Kage, Steven Cassar, Anil Vasudevan
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Publication number: 20110262388Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: April 21, 2011Publication date: October 27, 2011Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck, Torsten Hoffmann, Livia Boehme
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Publication number: 20110251401Abstract: Polyphenylene compounds such as compounds represented by Formula I may be used in electronic devices such as organic light-emitting devices. For example, the compounds may be used as host materials in a light-emitting layer.Type: ApplicationFiled: June 22, 2011Publication date: October 13, 2011Applicant: Nitto Denko CorporationInventors: Shijun Zheng, Rebecca Bottger
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Publication number: 20110240978Abstract: A heterocyclic compound of formula 1 and an organic light-emitting device including an organic layer containing the heterocyclic compound. The heterocyclic compound of Formula 1 may be suitable as a material for an emission layer, an electron transport layer or an electron injection layer of an organic light-emitting device. Due to the inclusion of the heterocylic group in its molecular structure, the heterocyclic compound of Formula 1 may have a high glass transition temperature (Tg) or a high melting point, and may prevent crystallization. An organic light-emitting device manufactured using the heterocyclic compound of Formula 1, in which a chrysene group and an indole group are fused, has excellent durability when stored or operated.Type: ApplicationFiled: April 1, 2011Publication date: October 6, 2011Applicant: SAMSUNG MOBILE DISPLAY CO., LTDInventors: Jin-O LIM, Seok-Hwan HWANG, Young-Kook KIM, Yoon-Hyun KWAK, Hye-Jin JUNG, Jong-Hyuk LEE
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Publication number: 20110240977Abstract: A heterocyclic compound of formula 1 and an organic light-emitting device including an organic layer containing the heterocyclic compound. The heterocyclic compound of Formula 1 may be suitable as a material for an emission layer, an electron transport layer or an electron injection layer of an organic light-emitting device. Due to the inclusion of the heterocylic group in its molecular structure, the heterocyclic compound of Formula 1 may have a high glass transition temperature (Tg) or a high melting point, and may prevent crystallization. An organic light-emitting device manufactured using the heterocyclic compound of Formula 1, which has a symmetrical structure in which a chrysene group and an indole group are fused, has excellent durability when stored or operated.Type: ApplicationFiled: March 31, 2011Publication date: October 6, 2011Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.Inventors: Hye-Jin JUNG, Seok-Hwan HWANG, Young-Kook KIM, Yoon-Hyun KWAK, Jin-O LIM, Jong-Hyuk LEE
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Publication number: 20110243850Abstract: Provided is a novel probe for a biological specimen for labelling by itself and clearly visualizing one of a specific cell and a specific cell organ in a living body, the probe having excellent spectral characteristics and exhibiting excellent storage stability. The probe for a biological specimen contains, as an active agent, at least one kind of compound represented by a general formula (I).Type: ApplicationFiled: December 24, 2009Publication date: October 6, 2011Applicant: CANON KABUSHIKI KAISHAInventors: Taichi Shintou, Takeshi Miyazaki, Masashi Hirose, Taketoshi Okubo, Kohei Watanabe, Tsuyoshi Nomoto, Toshio Tanaka, Yuhei Nishimura, Yasuhito Shimada, Norihiro Nishimura
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Publication number: 20110220513Abstract: Copper plating baths containing a leveling agent that is a reaction product of a certain benzimidazole with a certain epoxide-containing compound that deposit copper on the surface of a conductive layer are provided. Such plating baths deposit a copper layer that is substantially planar on a substrate surface across a range of electrolyte concentrations. Methods of depositing copper layers using such copper plating baths are also disclosed.Type: ApplicationFiled: March 15, 2010Publication date: September 15, 2011Applicant: Rohm and Haas Electronic Materials LLCInventors: Zukhra I. Niazimbetova, Maria Anna Rzeznik
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Publication number: 20110210318Abstract: The present invention provides a novel compound that is capable of largely improving a life time, efficiency, electrochemical stability, and thermal stability of an organic electronic device, and an organic electronic device that comprises an organic material layer comprising the compound.Type: ApplicationFiled: August 21, 2009Publication date: September 1, 2011Applicant: LG CHEM, LTD.Inventors: Jae-Soon Bae, Ji-Eun Kim, Hye-Young Jang, Jeung-Gon Kim, Jun-Gi Jang, Sung-Kil Hong, Tae-Yoon Park, Dae-Woong Lee
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Publication number: 20110207767Abstract: This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.Type: ApplicationFiled: November 3, 2009Publication date: August 25, 2011Inventors: Patrick Henry Beusker, Rudy Gerardus Elisabeth Coumans, Ronald Christiaan Elgrtsma, Wiro Michaël Petrus Bernardus Menge, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker, Franciscus Marinus Hendrikus De Groot
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Publication number: 20110195964Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: October 19, 2009Publication date: August 11, 2011Inventors: Qun Dang, De Michael Chung, Tony S. Gibson, Daniel K. Cashion, HongJian Jiang, Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka
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Publication number: 20110193074Abstract: The present invention relates to a novel compound and an organic light emitting device using the compound, and the compound according to the present invention may largely improve a life span, efficiency, electrochemical stability and thermal stability of the organic light emitting device.Type: ApplicationFiled: October 8, 2009Publication date: August 11, 2011Inventors: Dae-Woong Lee, Sung-Kil Hong, Tae-Yoon Park, Yeon-Hwan Kim, Seong-So Kim
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Publication number: 20110190262Abstract: The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.Type: ApplicationFiled: November 14, 2008Publication date: August 4, 2011Applicant: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
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Publication number: 20110166169Abstract: The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R?1; R is selected from the group comprising Formula (A?), (B), (C), (D), or (E), with R1 and/or R?1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkylhio, or carboxy that is free or esterified by an alkyl, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—S02-alkyl, S(0)2-NHalkyl, or S(02)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is 0, S, NR2, C(O), S(O), or S(0)2; Z is optionally substituted H, Hal, -0-R2 or —NH—R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.Type: ApplicationFiled: September 14, 2010Publication date: July 7, 2011Applicant: sanofi-aventisInventors: Jean-Marie RUXER, Victor CERTAL, Marcel ALASIA, Luc BERTIN, Herve MINOUX, Patrick MAILLIET, Frank HALLEY, Maria MENDEZ-PEREZ
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Publication number: 20110166102Abstract: The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: ApplicationFiled: March 17, 2011Publication date: July 7, 2011Inventors: Vernon C. ALFORD, JR., James C. LANTER, Raymond A. NG
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Publication number: 20110166159Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: March 17, 2011Publication date: July 7, 2011Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20110147792Abstract: Objects of the present invention are to provide the following: a novel heterocyclic compound which can be used as a material in which a light-emitting substance of a light-emitting layer in a light-emitting element is dispersed; a novel heterocyclic compound having a high electron-transport property; a light-emitting element having high current efficiency; and a light-emitting device, an electronic device and a lighting device each having reduced power consumption. Provided are a heterocyclic compound represented by General Formula (G1-1) or (G1-2) below, and a light-emitting element, a light-emitting device, an electronic device and a lighting device each including the heterocyclic compound. Such use of the heterocyclic compound represented by General Formula (G1-1) or (G1-2) makes it possible to provide a light-emitting element having high current efficiency, and a light-emitting device, an electronic device and a lighting device each having reduced power consumption.Type: ApplicationFiled: December 20, 2010Publication date: June 23, 2011Inventors: Yuko Kawata, Hiroshi Kadoma, Harue Osaka, Nobuharu Ohsawa, Satoshi Seo
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Publication number: 20110152260Abstract: The present invention relates to modulators of IRAK kinases of formula (I) and provides compositions comprising such modulators, as well as methods therewith for treating IRAK-mediated or IRAK-associated conditions or diseases.Type: ApplicationFiled: September 7, 2007Publication date: June 23, 2011Applicant: Biogen Idec Ma Inc.Inventors: Kevin Guckian, Charles Jewell, Patrick Conlon, Edward Yin Shiang Lin, Timothy Chan
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Publication number: 20110136859Abstract: A compound of formula (I) Or its salts or pharmaceutically acceptable derivatives thereof wherein; A represents a chemical moiety with the general formula (II): X is selected from a group consisting of CH2, C(?O), CH(R5), C(R5)(R6) or C(R5)(R6)CH2; R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R2 is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl or NR7R8; R3 R4 R5 R6 R7 and R8 are as defined herein; and n=1 or 2 is provided. Pharmaceutical compositions comprising the compounds are also provided. The compounds are useful in treating various conditions including arrhythmia.Type: ApplicationFiled: June 4, 2010Publication date: June 9, 2011Applicant: Xention Ltd.Inventors: Richard John HAMLYN, David MADGE, Mushtaq MULLA
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Publication number: 20110118259Abstract: This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.Type: ApplicationFiled: January 20, 2011Publication date: May 19, 2011Inventors: Janus S. Larsen, Lene Teuber, Philip K. Ahring, Elsebet Ostergaard Nielsen, Naheed Mirza
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Publication number: 20110118257Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: ApplicationFiled: November 3, 2010Publication date: May 19, 2011Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant VISWANADHA, Govindarajulu BABU, Swaroop Kumar V.S. VAKKALANKA
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Publication number: 20110105573Abstract: The invention relates to benzimidazole acetic acid compounds which function as antagonists of the Chemoattractant Receptor-homologous molecule expressed on T-Helper type 2 cells (CRTH2) receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.Type: ApplicationFiled: June 8, 2010Publication date: May 5, 2011Inventors: Youssef L. Bennani, Lawrence Nathan Tumey, Elizabeth Ann Gleason, Michael Joseph Robarge
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Publication number: 20110098236Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: February 23, 2009Publication date: April 28, 2011Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan
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Patent number: 7928105Abstract: Disclosed are compounds of the following formula: in which R1, R2, R5, R6, R7, R31, u, and X are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: GrantFiled: January 21, 2010Date of Patent: April 19, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20110082143Abstract: Bicyclic heteroaryl compounds of formula (I) shown below are disclosed. Each variable in formula (I) is defined in the specification. Also disclosed is treatment of cancer with these compounds.Type: ApplicationFiled: October 1, 2010Publication date: April 7, 2011Applicant: National Taiwan UniversityInventors: Chung-Ming Sun, Min-Liang Kuo
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Publication number: 20110071150Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with calcium release-activated calcium channels (CRAC).Type: ApplicationFiled: September 23, 2010Publication date: March 24, 2011Inventors: Muzaffar Alam, Daisy Joe Du Bois, Ronald Charles Hawley, Joshua Kennedy-Smith, Ana Elena Minatti, Wylie Solang Palmer, Tania Silva, Robert Stephen Wilhelm
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Publication number: 20110071156Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6, and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.Type: ApplicationFiled: July 20, 2010Publication date: March 24, 2011Applicant: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Hornberger, Herve Geneste, Daryl Richard Sauer, Wolfgang Wernet, Andrea Hager-Wernet, Liliane Unger, Wilfried Lubisch
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Publication number: 20110065713Abstract: The present invention is directed to benzazole compounds that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. 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 BACE is involved.Type: ApplicationFiled: November 19, 2010Publication date: March 17, 2011Applicant: High Point Pharmaceuticals, LLCInventors: Adnan M.M. Mjalli, David Jones, Devi Reddy Gohimmukkula, Guoxiang Huang, Jeff Zhu, Mohan Rao, Robert C. Andrews, Tan Ren
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Publication number: 20110065702Abstract: The present invention is directed to a compound is represented by Structural Formula (A):or a pharmaceutically acceptable salt therof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 19, 2008Publication date: March 17, 2011Inventors: Heinz W. Pauls, Bryan T. Forrest, Radoslaw Laufer, Miklos Feher, Peter Brent Sampson, Guohua Pan, Sze-Wan Li, Yong Liu
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Publication number: 20110062386Abstract: Disclosed herein are compounds represented by a formula: Wherein Ar1, Cb, Ph1, Het1, and A are described herein. Compositions and light-emitting devices related thereto are also disclosed.Type: ApplicationFiled: September 15, 2010Publication date: March 17, 2011Applicant: NITTO DENKO CORPORATIONInventors: Shijun Zheng, David T. Sisk, Brett T. Harding, Jensen Cayas, Sheng Li, Amane Mochizuki, Hyunsik Chae, Sazzadur Rahman Khan, Liping Ma, Rebecca Bottger
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Publication number: 20110052562Abstract: Compounds useful as Rho kinase inhibitors according to formula IA or IB: wherein A, B, D, E, R1, R2 and Ar1 are as defined herein, and any tautomer, salt, stereoisomer, hydrate, solvent, or prodrug thereof, pharmaceutical compositions, methods of treatment, and synthetic methods are provided.Type: ApplicationFiled: December 18, 2008Publication date: March 3, 2011Applicant: The Scripps Research InstituteInventors: Yangbo Feng, Philip LoGrasso, Thomas Bannister, Thomas Schroeter, Hampton Sessions, Lei Yao, Bo Wang, Michael P. Smolinski, Yen Ting Chen, Yan Yin, Bozena Frackowiak-Wojtasek, Sarwat Chowdhury
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Publication number: 20110046133Abstract: The present invention provides compounds of the following structure; A-L1-B-C-D that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: October 17, 2007Publication date: February 24, 2011Inventors: Moo Je Sung, Gary Mark Coppola, Taeyoung Yoon, Thomas A. Gilmore
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Patent number: 7879851Abstract: An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof, as an inhibitor of HCV NS5B polymerase.Type: GrantFiled: February 17, 2009Date of Patent: February 1, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Youla S. Tsantrizos, Catherine Chabot, Pierre Beaulieu, Christian Brochu, Martin Poirier, Timothy A. Stammers, Bounkham Thavonekham, Jean Rancourt
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Publication number: 20110009459Abstract: Epothilone derivatives of Formula (I) and their use as a pharmaceutical.Type: ApplicationFiled: September 21, 2010Publication date: January 13, 2011Applicant: NOVARTIS AGInventor: Karl-Heinz ALTMANN
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Publication number: 20110009385Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: R3 is selected from cyclopentyl and cyclohexyl; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.Type: ApplicationFiled: August 9, 2010Publication date: January 13, 2011Applicant: Amura Therapeutics LimitedInventors: MARTIN QUIBELL, John P. Watts, Nicholas S. Flinn
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Publication number: 20100331346Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R2?, R2?, R3, R4, R5, R6, R7 and R8 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.Type: ApplicationFiled: December 23, 2008Publication date: December 30, 2010Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Stefan Bender, Lars Thore Burgdorf, Ulrich Emde, Norbert Beier, Johannes Gleitz, Christine Charon
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Publication number: 20100331543Abstract: The quenching compounds of the invention are weakly luminescent cyanines that are substituted by one or more heteroaromatic quenching moieties. The quenching compounds of the invention exhibit little or no observable luminescence and efficiently quench a broad spectrum of luminescent compounds. The chemically reactive quenching compounds possess utility for labeling a wide variety of substances, including biomolecules. These labeled substances are highly useful for a variety of energy-transfer assays and applications.Type: ApplicationFiled: August 30, 2010Publication date: December 30, 2010Inventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang
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Publication number: 20100326526Abstract: Disclosed herein are compounds represented by Formula 1, wherein R1, Ar1, X, Ar2, Ara, and Het are described herein. Compositions and light-emitting devices related thereto are also disclosed.Type: ApplicationFiled: June 29, 2010Publication date: December 30, 2010Applicant: NITTO DENKO CORPORATIONInventors: SHIJUN ZHENG, JENSEN CAYAS, SHENG LI, AMANE MOCHIZUKI, HYUNSIK CHAE, BRETT T. HARDING