The Additional Hetero Ring Is A Cyclo In A Polycyclo Ring System (e.g., Benzofuranyl-benzimidazole, Etc.) Patents (Class 548/305.1)
  • Patent number: 8143421
    Abstract: 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: Grant
    Filed: April 27, 2009
    Date of Patent: March 27, 2012
    Assignee: 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
  • Patent number: 8110578
    Abstract: 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: Grant
    Filed: October 26, 2009
    Date of Patent: February 7, 2012
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: 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
  • Publication number: 20120028959
    Abstract: 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: Application
    Filed: March 26, 2010
    Publication date: February 2, 2012
    Applicant: 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
  • Publication number: 20120015998
    Abstract: 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: Application
    Filed: July 11, 2011
    Publication date: January 19, 2012
    Applicant: Nitto Denko Corporation
    Inventors: Amane Mochizuki, Sazzadur Rahman Khan, Sheng Li, Shijun Zheng, Jensen Cayas, Keisaku Okada, Brett T. Harding
  • Publication number: 20120010241
    Abstract: 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: Application
    Filed: March 18, 2010
    Publication date: January 12, 2012
    Applicant: SANOFI
    Inventors: Luc Bertin, Jean-Christophe Carry, Patrick Mailliet, Herve Minoux, Fabienne Pilorge, Jean-Marie Ruxer
  • Publication number: 20110312996
    Abstract: 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: Application
    Filed: May 16, 2011
    Publication date: December 22, 2011
    Applicant: InterMune, Inc.
    Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
  • Publication number: 20110312949
    Abstract: 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: Application
    Filed: August 30, 2011
    Publication date: December 22, 2011
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventors: John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
  • Publication number: 20110312935
    Abstract: 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: Application
    Filed: September 25, 2009
    Publication date: December 22, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer, Juergen Mack, Henning Priepke, Dirk Stenkamp
  • Publication number: 20110312969
    Abstract: 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: Application
    Filed: December 8, 2009
    Publication date: December 22, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephen Peter East, Mark Whittaker, Osamu Ichihara, Adrian Kotei Kotei, Smantha Jayne Bamford
  • Publication number: 20110309348
    Abstract: 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: Application
    Filed: June 20, 2011
    Publication date: December 22, 2011
    Applicant: Samsung Mobile Display Co., Ltd.
    Inventors: Yoon-Hyun KWAK, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jong-Hyuk Lee, Hee-Joo Ko
  • Patent number: 8067613
    Abstract: 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: Grant
    Filed: July 15, 2008
    Date of Patent: November 29, 2011
    Assignee: Abbott Laboratories
    Inventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D Penning, Gui-Dong Zhu
  • Publication number: 20110288139
    Abstract: 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: Application
    Filed: January 21, 2009
    Publication date: November 24, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Klaus Fuchs, Cornelia Dorner-Ciossek, Sandra Handschuh, Niklas Heine, Stefan Hoerer, Klaus Klinder
  • Patent number: 8063053
    Abstract: 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: Grant
    Filed: November 11, 2009
    Date of Patent: November 22, 2011
    Assignee: Wyeth LLC
    Inventors: Simon Nicolas Haydar, Patrick Michael Andrae, Heedong Yun, Albert Jean Robichaud
  • Publication number: 20110275630
    Abstract: 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: Application
    Filed: November 3, 2010
    Publication date: November 10, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Mark Matulenko, Tammie Jinkerson, Brian S. Brown, Wilfried Braje, Michael Curtin, Howard Robin Heyman, Victoria Scott, Karen Kage, Steven Cassar, Anil Vasudevan
  • Publication number: 20110262388
    Abstract: 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: Application
    Filed: April 21, 2011
    Publication date: October 27, 2011
    Applicant: PROBIODRUG AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Torsten Hoffmann, Livia Boehme
  • Publication number: 20110251401
    Abstract: 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: Application
    Filed: June 22, 2011
    Publication date: October 13, 2011
    Applicant: Nitto Denko Corporation
    Inventors: Shijun Zheng, Rebecca Bottger
  • Publication number: 20110240978
    Abstract: 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: Application
    Filed: April 1, 2011
    Publication date: October 6, 2011
    Applicant: SAMSUNG MOBILE DISPLAY CO., LTD
    Inventors: Jin-O LIM, Seok-Hwan HWANG, Young-Kook KIM, Yoon-Hyun KWAK, Hye-Jin JUNG, Jong-Hyuk LEE
  • Publication number: 20110240977
    Abstract: 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: Application
    Filed: March 31, 2011
    Publication date: October 6, 2011
    Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.
    Inventors: Hye-Jin JUNG, Seok-Hwan HWANG, Young-Kook KIM, Yoon-Hyun KWAK, Jin-O LIM, Jong-Hyuk LEE
  • Publication number: 20110243850
    Abstract: 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: Application
    Filed: December 24, 2009
    Publication date: October 6, 2011
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Taichi Shintou, Takeshi Miyazaki, Masashi Hirose, Taketoshi Okubo, Kohei Watanabe, Tsuyoshi Nomoto, Toshio Tanaka, Yuhei Nishimura, Yasuhito Shimada, Norihiro Nishimura
  • Publication number: 20110220513
    Abstract: 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: Application
    Filed: March 15, 2010
    Publication date: September 15, 2011
    Applicant: Rohm and Haas Electronic Materials LLC
    Inventors: Zukhra I. Niazimbetova, Maria Anna Rzeznik
  • Publication number: 20110210318
    Abstract: 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: Application
    Filed: August 21, 2009
    Publication date: September 1, 2011
    Applicant: 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
  • Publication number: 20110207767
    Abstract: 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: Application
    Filed: November 3, 2009
    Publication date: August 25, 2011
    Inventors: 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
  • Publication number: 20110195964
    Abstract: 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: Application
    Filed: October 19, 2009
    Publication date: August 11, 2011
    Inventors: 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
  • Publication number: 20110193074
    Abstract: 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: Application
    Filed: October 8, 2009
    Publication date: August 11, 2011
    Inventors: Dae-Woong Lee, Sung-Kil Hong, Tae-Yoon Park, Yeon-Hwan Kim, Seong-So Kim
  • Publication number: 20110190262
    Abstract: 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: Application
    Filed: November 14, 2008
    Publication date: August 4, 2011
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
  • Publication number: 20110166169
    Abstract: 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: Application
    Filed: September 14, 2010
    Publication date: July 7, 2011
    Applicant: sanofi-aventis
    Inventors: Jean-Marie RUXER, Victor CERTAL, Marcel ALASIA, Luc BERTIN, Herve MINOUX, Patrick MAILLIET, Frank HALLEY, Maria MENDEZ-PEREZ
  • Publication number: 20110166102
    Abstract: 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: Application
    Filed: March 17, 2011
    Publication date: July 7, 2011
    Inventors: Vernon C. ALFORD, JR., James C. LANTER, Raymond A. NG
  • Publication number: 20110166159
    Abstract: 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: Application
    Filed: March 17, 2011
    Publication date: July 7, 2011
    Applicant: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20110147792
    Abstract: 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: Application
    Filed: December 20, 2010
    Publication date: June 23, 2011
    Inventors: Yuko Kawata, Hiroshi Kadoma, Harue Osaka, Nobuharu Ohsawa, Satoshi Seo
  • Publication number: 20110152260
    Abstract: 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: Application
    Filed: September 7, 2007
    Publication date: June 23, 2011
    Applicant: Biogen Idec Ma Inc.
    Inventors: Kevin Guckian, Charles Jewell, Patrick Conlon, Edward Yin Shiang Lin, Timothy Chan
  • Publication number: 20110136859
    Abstract: 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: Application
    Filed: June 4, 2010
    Publication date: June 9, 2011
    Applicant: Xention Ltd.
    Inventors: Richard John HAMLYN, David MADGE, Mushtaq MULLA
  • Publication number: 20110118259
    Abstract: 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: Application
    Filed: January 20, 2011
    Publication date: May 19, 2011
    Inventors: Janus S. Larsen, Lene Teuber, Philip K. Ahring, Elsebet Ostergaard Nielsen, Naheed Mirza
  • Publication number: 20110118257
    Abstract: 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: Application
    Filed: November 3, 2010
    Publication date: May 19, 2011
    Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant VISWANADHA, Govindarajulu BABU, Swaroop Kumar V.S. VAKKALANKA
  • Publication number: 20110105573
    Abstract: 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: Application
    Filed: June 8, 2010
    Publication date: May 5, 2011
    Inventors: Youssef L. Bennani, Lawrence Nathan Tumey, Elizabeth Ann Gleason, Michael Joseph Robarge
  • Publication number: 20110098236
    Abstract: 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: Application
    Filed: February 23, 2009
    Publication date: April 28, 2011
    Applicant: Sequoia Pharmaceuticals, Inc.
    Inventors: Michael Eissenstat, Dehui Duan
  • Patent number: 7928105
    Abstract: 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: Grant
    Filed: January 21, 2010
    Date of Patent: April 19, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
  • Publication number: 20110082143
    Abstract: 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: Application
    Filed: October 1, 2010
    Publication date: April 7, 2011
    Applicant: National Taiwan University
    Inventors: Chung-Ming Sun, Min-Liang Kuo
  • Publication number: 20110071150
    Abstract: 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: Application
    Filed: September 23, 2010
    Publication date: March 24, 2011
    Inventors: Muzaffar Alam, Daisy Joe Du Bois, Ronald Charles Hawley, Joshua Kennedy-Smith, Ana Elena Minatti, Wylie Solang Palmer, Tania Silva, Robert Stephen Wilhelm
  • Publication number: 20110071156
    Abstract: 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: Application
    Filed: July 20, 2010
    Publication date: March 24, 2011
    Applicant: Abbott GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Hornberger, Herve Geneste, Daryl Richard Sauer, Wolfgang Wernet, Andrea Hager-Wernet, Liliane Unger, Wilfried Lubisch
  • Publication number: 20110065713
    Abstract: 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: Application
    Filed: November 19, 2010
    Publication date: March 17, 2011
    Applicant: High Point Pharmaceuticals, LLC
    Inventors: Adnan M.M. Mjalli, David Jones, Devi Reddy Gohimmukkula, Guoxiang Huang, Jeff Zhu, Mohan Rao, Robert C. Andrews, Tan Ren
  • Publication number: 20110065702
    Abstract: 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: Application
    Filed: December 19, 2008
    Publication date: March 17, 2011
    Inventors: Heinz W. Pauls, Bryan T. Forrest, Radoslaw Laufer, Miklos Feher, Peter Brent Sampson, Guohua Pan, Sze-Wan Li, Yong Liu
  • Publication number: 20110062386
    Abstract: 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: Application
    Filed: September 15, 2010
    Publication date: March 17, 2011
    Applicant: NITTO DENKO CORPORATION
    Inventors: Shijun Zheng, David T. Sisk, Brett T. Harding, Jensen Cayas, Sheng Li, Amane Mochizuki, Hyunsik Chae, Sazzadur Rahman Khan, Liping Ma, Rebecca Bottger
  • Publication number: 20110052562
    Abstract: 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: Application
    Filed: December 18, 2008
    Publication date: March 3, 2011
    Applicant: The Scripps Research Institute
    Inventors: 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
  • Publication number: 20110046133
    Abstract: 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: Application
    Filed: October 17, 2007
    Publication date: February 24, 2011
    Inventors: Moo Je Sung, Gary Mark Coppola, Taeyoung Yoon, Thomas A. Gilmore
  • Patent number: 7879851
    Abstract: 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: Grant
    Filed: February 17, 2009
    Date of Patent: February 1, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Youla S. Tsantrizos, Catherine Chabot, Pierre Beaulieu, Christian Brochu, Martin Poirier, Timothy A. Stammers, Bounkham Thavonekham, Jean Rancourt
  • Publication number: 20110009459
    Abstract: Epothilone derivatives of Formula (I) and their use as a pharmaceutical.
    Type: Application
    Filed: September 21, 2010
    Publication date: January 13, 2011
    Applicant: NOVARTIS AG
    Inventor: Karl-Heinz ALTMANN
  • Publication number: 20110009385
    Abstract: 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: Application
    Filed: August 9, 2010
    Publication date: January 13, 2011
    Applicant: Amura Therapeutics Limited
    Inventors: MARTIN QUIBELL, John P. Watts, Nicholas S. Flinn
  • Publication number: 20100331346
    Abstract: 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: Application
    Filed: December 23, 2008
    Publication date: December 30, 2010
    Applicant: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Stefan Bender, Lars Thore Burgdorf, Ulrich Emde, Norbert Beier, Johannes Gleitz, Christine Charon
  • Publication number: 20100331543
    Abstract: 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: Application
    Filed: August 30, 2010
    Publication date: December 30, 2010
    Inventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang
  • Publication number: 20100326526
    Abstract: 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: Application
    Filed: June 29, 2010
    Publication date: December 30, 2010
    Applicant: NITTO DENKO CORPORATION
    Inventors: SHIJUN ZHENG, JENSEN CAYAS, SHENG LI, AMANE MOCHIZUKI, HYUNSIK CHAE, BRETT T. HARDING