1,3,4-oxadiazoles (including Hydrogenated) Patents (Class 548/143)
  • Publication number: 20130140544
    Abstract: This invention relates to deuterated indolocarbazole compounds that are useful in electronic applications. It also relates to electronic devices in which the active layer includes such a deuterated compound.
    Type: Application
    Filed: January 24, 2013
    Publication date: June 6, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventor: E I DU PONT DE NEMOURS AND COMPANY
  • Patent number: 8455658
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R?1, X, X?, L and Y are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: January 25, 2007
    Date of Patent: June 4, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Nha Huu Vo, Shoujun Chen, Qinglin Che, Yu Xie
  • Patent number: 8455657
    Abstract: A process is described for the preparation of 3-alkylsulfinylbenzoyl derivatives of the formula (IIIa) by reaction of 3-alkylsulfinylbenzoic acids of the formula (Ib) with compounds of the formula (II) in the presence of a chlorinating agent and a base. In the formulae specified above, Y is a radical such as pyrazolyl and cyclohexanedionyl. R1, R2 and R3 are radicals such as halogen, nitro, cyano and alkyl.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: June 4, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Mark James Ford, Jan Peter Schmidt, Helmut Kohlhepp
  • Patent number: 8455525
    Abstract: This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, and or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, Ie, and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, and intermediates useful in the preparation of same.
    Type: Grant
    Filed: August 17, 2010
    Date of Patent: June 4, 2013
    Assignee: Radius Health, Inc.
    Inventor: Chris P. Miller
  • Publication number: 20130136794
    Abstract: Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.
    Type: Application
    Filed: April 21, 2011
    Publication date: May 30, 2013
    Applicant: PEKING UNIVERSITY
    Inventors: Runtao Li, Zemei Ge, Jingrong Cui, Xingyl Sun, Zhongqing Wang, Xu Yan
  • Publication number: 20130137865
    Abstract: A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.
    Type: Application
    Filed: August 11, 2011
    Publication date: May 30, 2013
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto, Hideaki Amada, Hiroki Urabe, Rie Nishikawa, Shuhei Kashiwa ASHIWA
  • Patent number: 8450494
    Abstract: The invention relates to disubstituted benzamide derivatives of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating type II diabetes using the compounds of the invention.
    Type: Grant
    Filed: June 21, 2010
    Date of Patent: May 28, 2013
    Assignee: Cadila Healthcare Limited
    Inventor: Rajendra Kharul
  • Publication number: 20130131321
    Abstract: The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR1—C(O)—, and wherein either NR1 is attached to Ar1 and —C(O)— is attached to Ar2, or —C(O)— is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; a
    Type: Application
    Filed: August 3, 2011
    Publication date: May 23, 2013
    Applicant: GRAFFINITY PHARMACEUTICALS GMBH
    Inventors: Holger Bittermann, Klaus Burkert, Marc Arnold, Oliver Keil, Thomas Neumann, Inge Ott, Kristina Schmidt, Daniel Schwizer, Renate Sekul
  • Patent number: 8440820
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: May 14, 2013
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
  • Publication number: 20130113367
    Abstract: A heterocyclic compound represented by Formula 1A and an organic light-emitting device including the heterocyclic compound: at least one of R1 to R13 is a group represented by Formula 1B below: wherein R1 to R15, Ar1, Ar2, A, B, a, and b are defined as in the specification. The organic light-emitting device may include an organic layer containing the heterocyclic compound, and thus may have a low driving voltage, a high-emission efficiency, and long lifespan characteristics.
    Type: Application
    Filed: April 12, 2012
    Publication date: May 9, 2013
    Applicant: Samsung Mobile Display Co., Ltd.
    Inventors: Hye-Jin Jung, Seok-Hwan Hwang, Young-Kook Kim, Jin-O Lim, Sang-Hyun Han, Soo-Yon Kim, Dae-Yup Shin
  • Publication number: 20130116227
    Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.
    Type: Application
    Filed: July 12, 2011
    Publication date: May 9, 2013
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
  • Publication number: 20130116288
    Abstract: This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, If or Ig and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig and intermediates useful in the preparation of same.
    Type: Application
    Filed: August 9, 2012
    Publication date: May 9, 2013
    Applicant: Radius Health, Inc.
    Inventor: Chris P. Miller
  • Publication number: 20130109649
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: October 25, 2012
    Publication date: May 2, 2013
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
  • Patent number: 8420675
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, W, X, R1—R5 and n are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Grant
    Filed: January 2, 2012
    Date of Patent: April 16, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun, Zhenshan Zhang
  • Patent number: 8415353
    Abstract: Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(?NOH)NH2, —CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: April 9, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
  • Publication number: 20130085138
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Application
    Filed: September 26, 2012
    Publication date: April 4, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130072490
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: September 29, 2010
    Publication date: March 21, 2013
    Applicant: Amira Pharmaceuticals INC.
    Inventors: Ryan Clark, Brian Andrew Stearns, Jill Melissa Scott, Heather Renee Coate, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie Arruda, Nicholas Simon Stock, Yen Pham Truong, David Nathan Zalatan
  • Patent number: 8399666
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.
    Type: Grant
    Filed: October 30, 2006
    Date of Patent: March 19, 2013
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John H. Hutchinson, Petpiboon Peppi Prasit, Mark Moran, Jillian F. Evans, Brian Andrew Stearns, Jeffrey Roger Roppe, Yiwei Li, Jasmine Eleanor Zunic, Jeannie M. Arruda, Nicholas Simon Stock, Mustapha Haddach
  • Patent number: 8394293
    Abstract: The present invention relates to thiophene derivatives, to processes and intermediates for the preparation thereof, to the use thereof for optical, electro-optical and electronic purposes, in particular in liquid-crystal (LC) media and LC displays, and to LC media and LC displays comprising same.
    Type: Grant
    Filed: March 30, 2009
    Date of Patent: March 12, 2013
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Axel Jansen, Detlef Pauluth, Harald Hirschmann, Markus Czanta
  • Publication number: 20130060025
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 12, 2012
    Publication date: March 7, 2013
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Patent number: 8389735
    Abstract: An oxadiazole derivative represented by the following general formula (G1) is synthesized and applied to the light emitting element, wherein Am is a substituent represented by a general formula (Am1), (Am2), or (Am3); each of ?, ?1, and ?2 represents an arylene group having 6 to 25 carbon atoms; each of Ar1 to Ar6 represents an aryl group having 6 to 25 carbon atoms; each of R1 to R3 represents hydrogen, an alkyl group having 1 to 4 carbon atoms, or an aryl group having 6 to 25 carbon atoms; and R4 represents an alkyl group having 1 to 4 carbon atoms or an aryl group having 6 to 25 carbon atoms.
    Type: Grant
    Filed: December 27, 2006
    Date of Patent: March 5, 2013
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroko Murata, Harue Nakashima, Sachiko Kawakami, Nobuharu Ohsawa, Ryoji Nomura, Satoshi Seo
  • Publication number: 20130053386
    Abstract: The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: October 5, 2010
    Publication date: February 28, 2013
    Inventors: William Colby Brown, Richard W. Heidebrecht, Jason Brubaker, Christian Fischer, John T. Hendrix, Elizabeth H. Kelley, Rachel N. MacCoss, Joey L. Methot, Thomas Miller, Karin M. Otte, Phieng Siliphaivanh, Thomas Reger, Peter D. Williams, Catherine M. Wiscount
  • Patent number: 8383622
    Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is a group represented by the formula: Ring B is optionally substituted heteroaryl, provided that optionally substituted isoxazole is excluded, or optionally substituted heterocycle, R1 is hydrogen or optionally substituted alkyl, R2 is —OR5, —SR5, halogen, halogenated alkyl or the like, R3 is optionally substituted alkyl or the like, R4 is optionally substituted alkyl or the like, R5 is optionally substituted alkyl or the like, R6 is hydrogen or the like, R7 and R8 are each independently hydrogen or the like, R10 and R11 are each independently hydrogen or the like, R12 is optionally substituted alkyl or the like, m and p are each independently integer of 1 to 3.
    Type: Grant
    Filed: May 7, 2008
    Date of Patent: February 26, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Koji Masuda, Tomoyuki Ogawa, Takuji Nakatani
  • Patent number: 8383660
    Abstract: Dibenzyl amine compounds and derivatives of Formula I, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
    Type: Grant
    Filed: January 3, 2007
    Date of Patent: February 26, 2013
    Assignee: Pfizer Inc.
    Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry
  • Patent number: 8377975
    Abstract: Novel oxadiazole derivatives of the formula (I), in which R, R?, Y, X1, X2 and X3 have the meanings indicated in claim 1, are kinase inhibitors and can be used for the treatment of diseases and conditions such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, in general in all types of fibroses, inflammatory processes, tumours and tumour diseases.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: February 19, 2013
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Markus Klein, Norbert Beier, Florian Lang
  • Publication number: 20130032787
    Abstract: A heterocyclic compound represented by Formula 1 or Formula 2 below, and an organic light-emitting device including the heterocyclic compound. The organic light-emitting device may include an organic layer containing the heterocyclic compound, and thus may have a low driving voltage, a high-emission efficiency, and long lifespan characteristics. wherein R1 to R12, Ar1, Ar2, A, B, a, and b are defined as in the specification.
    Type: Application
    Filed: November 25, 2011
    Publication date: February 7, 2013
    Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.
    Inventors: Young-Kook Kim, Seok-Hwan Hwang, Hye-Jin Jung, Jin-O Lim, Sang-Hyun Han, Se-Jin Cho, Jong-Hyuk Lee
  • Publication number: 20130030022
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: September 26, 2012
    Publication date: January 31, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Boehringer Ingelheim International GmbH
  • Publication number: 20130018048
    Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Application
    Filed: April 4, 2011
    Publication date: January 17, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: ZhiQiang Yang, Philippe G. Nantermet, Constantine Kreatsoulas, Keith P. Moore, Evan Foster Shalen
  • Patent number: 8354436
    Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: January 15, 2013
    Assignee: 4SC Discovery GmbH
    Inventors: Johann Leban, Stefan Tasler, Wael Saeb, Carine Chevrier
  • Patent number: 8343639
    Abstract: Disclosed is a novel organic semiconductor material which has a twisted quaterphenylene skeleton as a central unit and simultaneously possesses a skeleton having an electron-transporting property and a skeleton having a hole-transporting property at the terminals of the quaterphenylene skeleton. Specifically, the organic semiconductor material has a [1,1?:2?,1?:2?,1??]quaterphenyl-4-4??-diyl group, and one of the terminals of the [1,1?:2?,1?:2?,1??]quaterphenyl-4-4??-diyl group is bonded to a skeleton having an electron-transporting property such as a benzoxazole group or an oxadiazole group. A skeleton having a hole-transporting property such as diarylamino group is introduced at the other terminal. This structure allows the formation of a compound having a bipolar property, a high molecular weight, an excellent thermal stability, a large band gap, and high triplet excitation energy.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: January 1, 2013
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Satoshi Seo, Sachiko Kawakami, Hiroko Nomura, Nobuharu Ohsawa
  • Patent number: 8343970
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: January 1, 2013
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Publication number: 20120329649
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Inventors: James E. Hunter, William C. Lo, Gerald B. Watson, Akshay Patny, Gary D. Gustafson, Dan Pernich, William K. Brewster, Debra L. Camper, Beth Lorsbach, Michael R. Loso, Thomas C. Sparks, Hemant Joshi, Adiraj Mandaleswaran, Ramadevi Sanam, Rambabu Gundla, Pravin S. Iyer
  • Publication number: 20120302524
    Abstract: Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).
    Type: Application
    Filed: December 28, 2010
    Publication date: November 29, 2012
    Applicants: GENERAL INCORPORATED ASSOCIATION PHARMA VALLEY PROJECT SUPPORTING ORGANIZATION, PHARMA DESIGN, INC., KABUSHIKI KAISHA YAKULT HONSHA, KUMAMOTO HEALTH SCIENCE UNIVERSITY, SHIZUOKA PREFECTURE
    Inventors: Akira Asai, Kenji Matsuno, Naohisa Ogo, Osamu Takahashi, Yoshiaki Masuda, Ayumu Muroya, Yasuto Akiyama, Tadashi Ashizawa, Tadashi Okawara
  • Publication number: 20120289698
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 13, 2012
    Publication date: November 15, 2012
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Publication number: 20120289505
    Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.
    Type: Application
    Filed: December 30, 2010
    Publication date: November 15, 2012
    Inventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
  • Patent number: 8299104
    Abstract: The invention relates to substituted aryl-substituted heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to process for their preparation and to their use as medicaments. Compounds of the formula I in which the radicals have the stated meanings, the N-oxides thereof, and the physiologically tolerated salts thereof, and process for the preparation thereof are described. The compounds bring about for example a weight reduction in mammals and are suitable for example for the prevention and treatment of obesity and diabetes.
    Type: Grant
    Filed: November 28, 2007
    Date of Patent: October 30, 2012
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Lothar Schwink, Siegfried Stengelin, Thomas Boehme, Matthias Gossel, Gerhard Hessler, Petra Stahl
  • Patent number: 8288371
    Abstract: Compounds of the formula are disclosed. The compounds are CCR1 antagonists which are useful for the treatment and prevention of inflammatory and autoimmune diseases. Other embodiments are also disclosed.
    Type: Grant
    Filed: October 3, 2008
    Date of Patent: October 16, 2012
    Assignee: Pharmacopeia, LLC
    Inventors: Vidyadhar M. Paradkar, Marc Brescia, Ray James, Jinqi Liu, Ruiyan Liu, James Robert Merritt, Michelle Morris, Michael J. Ohlmeyer, Chongwu Zhang, Rui Zhang
  • Publication number: 20120258986
    Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).
    Type: Application
    Filed: January 16, 2012
    Publication date: October 11, 2012
    Applicant: KARYOPHARM THERAPEUTICS, INC.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Sharon Shechter, Dilara McCauley
  • Publication number: 20120252770
    Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments
    Type: Application
    Filed: March 23, 2012
    Publication date: October 4, 2012
    Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrencher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
  • Publication number: 20120253040
    Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.
    Type: Application
    Filed: December 14, 2010
    Publication date: October 4, 2012
    Applicant: Shionogi & Co., Ltd.
    Inventors: Koji Masuda, Shiro Kida, Naoki Yoshikawa, Manabu Katou, Terukazu Kato, Mado Nakajima, Eiichi Kojima, Mitsuhiro Yonehara
  • Publication number: 20120252853
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: March 30, 2012
    Publication date: October 4, 2012
    Applicant: H. Lundbeck A/S
    Inventors: Anette Graven Sams, Jørgen Eskildsen, Jesper Frank Bastlund
  • Patent number: 8273898
    Abstract: Provided is a bipolar substance having high excitation energy, in particular, high triplet-excitation energy. An oxadiazole derivative represented by General Formula (G1) below is provided In the formula, Ar represents a substituted or unsubstituted aryl group having 6 to 10 carbon atoms in a ring. R1 represents an alkyl group having 1 to 4 carbon atoms or a substituted or unsubstituted aryl group having 6 to 10 carbon atoms in a ring. R2 represents hydrogen, an alkyl group having 1 to 4 carbon atoms, or a substituted or unsubstituted aryl group having 6 to 10 carbon atoms in a ring.
    Type: Grant
    Filed: March 24, 2010
    Date of Patent: September 25, 2012
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
  • Patent number: 8263629
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: September 11, 2012
    Assignee: Novartis AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Patent number: 8247575
    Abstract: Disclosed is a carbazole derivative and a light-emitting element, a light-emitting device, and an electronic device using thereof. The carbazole derivative possesses an oxadiazole moiety or a quinoxaline moiety as a heteroaromatic ring having an electron-transporting property and a carbazole moiety having a hole-transporting property. The ability of the carbazole derivative to transport both electrons and holes and its large excitation energy larger than a triplet excitation energy of a phosphorescent compound allow the formation of a phosphorescent light-emitting element having well-controlled carrier balance, which contributes to the formation of light-emitting devices and electronic devices that are capable of being driven at a low voltage, have a long lifetime, and consume low power. The detailed structure of the carbazole derivative is defined in the specification.
    Type: Grant
    Filed: March 17, 2010
    Date of Patent: August 21, 2012
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
  • Patent number: 8247401
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: October 29, 2008
    Date of Patent: August 21, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Diem Nguyen, Zhengwu Deng, Daniel V. Paone, Craig M. Potteiger, Joseph P. Vacca
  • Publication number: 20120208852
    Abstract: The present application relates to new, heterocyclyl-substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: August 24, 2010
    Publication date: August 16, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Chantal Fürstner, Joerg Keldenich, Armin Kern, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
  • Publication number: 20120202856
    Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.
    Type: Application
    Filed: February 2, 2012
    Publication date: August 9, 2012
    Inventors: Mark R. PLAYER, Raul CALVO, Jinsheng CHEN, Carl ILLIG, Sanath MEEGALLA, Daniel PARKS, William PARSONS
  • Patent number: 8236822
    Abstract: Cannabinoid receptor ligands of formula (I) wherein Ring A and R1 are as defined in the specification. Compositions including such compounds, and methods of treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: August 7, 2012
    Assignee: Abbott Laboratories
    Inventors: Xueqing Wang, Michael J. Dart, Bo Liu
  • Patent number: 8236829
    Abstract: Bicyclic derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: August 7, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Timothy Donald Neubert, Aarti Sameer Kawatkar, Esther Ann Martinborough, Andreas P. Termin, Nicole Hilgraf
  • Publication number: 20120196884
    Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).
    Type: Application
    Filed: June 14, 2010
    Publication date: August 2, 2012
    Applicant: BIOTIE THERAPIES CORPORATION
    Inventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen