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
Abstract: The present invention provides a compound of formula I; 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.
Abstract: Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed.
Type:
Application
Filed:
November 16, 2010
Publication date:
February 7, 2013
Applicant:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Inventors:
John William Taunton, JR., Rebecca Maglathlin, Iana Serafimova, Michael S. Cohen, Rand Miller, Ville Paavilainen, Jesse McFarland, Shyam Krishnan
Abstract: Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.
Type:
Grant
Filed:
April 28, 2010
Date of Patent:
February 5, 2013
Assignee:
Plexxikon Inc.
Inventors:
James Arnold, Dean R. Artis, Clarence R. Hurt, Prabha N. Ibrahim, Heike Krupka, Jack Lin, Michael V. Milburn, Weiru Wang, Chao Zhang
Abstract: A method for making the compound of Formula I: is set forth using alkylation, amidation, chlorination and phosphate installation procedures.
Type:
Application
Filed:
January 27, 2012
Publication date:
January 31, 2013
Inventors:
Jonathan Clive Tripp, Dayne Dustan Fanfair, Mitchell J. Schultz, Saravanababu Murugesan, Richard J. Fox, Chung-Pin H. Chen, Sabrina E. Ivy, Joseph Francis Payack, Wendel W. Doubleday
Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclopenta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
Type:
Application
Filed:
July 11, 2012
Publication date:
January 31, 2013
Inventors:
Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
Type:
Application
Filed:
July 25, 2012
Publication date:
January 31, 2013
Applicant:
Gruenenthal GmbH
Inventors:
Robert FRANK, Thomas CHRISTOPH, Bernhard LESCH, Jeewoo LEE
Abstract: The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8 X, Y and have the meaning cited in the specification. Also disclosed are the pharmaceutical compositions containing the foregoing compounds, methods for the preparation and pharmaceutical use thereof, particularly as protein kinase inhibitors. Formula (I).
Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.
Type:
Grant
Filed:
December 21, 2010
Date of Patent:
January 29, 2013
Assignee:
Bristol-Myers Squibb Company
Inventors:
Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
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
Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
Type:
Application
Filed:
July 11, 2012
Publication date:
January 17, 2013
Inventors:
Joseph A. Bilotta, Adrian Wai-Hing Cheung, Fariborz Firooznia, Kevin Richard Guertin, Stuart Hayden, Nancy-Ellen Haynes, Christine M. Lukacs-Lesburg, Nicholas Marcopulos, Eric Mertz, Lida Qi, Yimin Qian, Sung-Sau So, Jenny Tan, Kshitij C. Thakkar
Abstract: The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Type:
Application
Filed:
June 19, 2012
Publication date:
January 17, 2013
Applicant:
INCYTE CORPORATION
Inventors:
Wenqing Yao, David M. Burns, Jincong Zhuo
Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).
Type:
Application
Filed:
July 12, 2012
Publication date:
January 17, 2013
Applicant:
GLAXOSMITHKLINE LLC
Inventors:
Martha Alicia De La Rosa, Brian Alvin Johns, Emile Johann Velthuisen, Jason Weatherhead, Vicente Samano
Abstract: The disclosure relates to compounds of formula (I): wherein X1, X2, X3, X4, Z1, Z2, Z3, Z4, Ra, Rb, n, Y, and W are as defined in the disclosure, or a salt thereof, or a hydrate or solvate thereof, and to processes for the preparation of these compounds and the therapeutic use thereof.
Type:
Grant
Filed:
July 21, 2010
Date of Patent:
January 15, 2013
Assignee:
Sanofi
Inventors:
Laurent Dubois, Yannick Evanno, David Machnik, André Malanda
Abstract: The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
Type:
Grant
Filed:
October 26, 2010
Date of Patent:
January 8, 2013
Assignee:
Merck Sharp & Dohme
Inventors:
Michael J. Breslin, Christopher D. Cox, Izzat T. Raheem
Abstract: The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
Type:
Application
Filed:
June 27, 2012
Publication date:
January 3, 2013
Applicants:
Abbott Laboratories, Abbott GmbH & Co. KG
Inventors:
Hervé Geneste, Michael Ochse, Karla Drescher, Berthold Behl, Loic Laplanche, Jürgen Dinges, Clarissa Jakob
Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
Type:
Grant
Filed:
June 8, 2009
Date of Patent:
January 1, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michelle Machacek, Gabriela de Almeida, Jonathan B. Grimm, Rachel N. MacCoss, Eric Romeo, Tony Siu, Catherine White, Kevin Wilson
Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
Type:
Application
Filed:
August 3, 2009
Publication date:
December 27, 2012
Inventors:
John Wityak, Leticia M. Toledo-Sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Application
Filed:
June 4, 2012
Publication date:
December 27, 2012
Inventors:
Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
Abstract: This invention relates to bicyclic ring system substituted amide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.
Type:
Application
Filed:
December 13, 2011
Publication date:
December 27, 2012
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Riccardo GIOVANNINI, Dieter HAMPRECHT, Barbara KISTLER, Iain LINGARD
Abstract: Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by RON and/or MET.
Type:
Application
Filed:
March 3, 2011
Publication date:
December 27, 2012
Inventors:
An-Hu Li, Ramesh C. Gupta, Mark J. Mulvihill, Anand Narain Rai, Jing Wang
Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
Type:
Grant
Filed:
February 27, 2009
Date of Patent:
December 25, 2012
Assignees:
Array BioPharma Inc., Genentech, Inc.
Inventors:
Kateri A. Ahrendt, Alexandre J. Buckmelter, Jonas Grina, Joshua D. Hansen, Ellen R. Laird, David Moreno, Brad Newhouse, Li Ren, Steven M. Wenglowsky, Bainian Feng, Janet Gunzner, Kim Malesky, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Wendy B. Young
Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, R1a, R1b, R2, R3, R4a and R4b are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Type:
Application
Filed:
December 14, 2011
Publication date:
December 20, 2012
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Angela BERRY, Zhidong CHEN, Stephane DE LOMBAERT, Michel Jose EMMANUEL, Pui Leng LOKE, Chuk Chui MAN, Tina Marie MORWICK, Hidenori TAKAHASHI
Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:
Abstract: The invention relates to annelated pyrrolidin sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
Type:
Grant
Filed:
May 22, 2009
Date of Patent:
December 11, 2012
Assignee:
Sanofi
Inventors:
Stefanie Keil, Matthias Urmann, Wolfgang Wendler, Ulrike Wendler, Maike Glien, Hans Matter, Eugen Falk
Abstract: Pyrazine compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein m, n, p, R1, R2, R3, R4, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, Y and Z are defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
Type:
Grant
Filed:
March 7, 2011
Date of Patent:
December 11, 2012
Assignee:
Amgen Inc.
Inventors:
Jennifer R. Allen, Matthew Paul Bourbeau, Ning Chen, Essa Hu, Roxanne Kunz, Shannon Rumfelt
Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as novel synthesis routes for key intermediates used in those processes.
Type:
Grant
Filed:
July 27, 2010
Date of Patent:
December 11, 2012
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Stefan Hildbrand, Hans-Juergen Mair, Roumen Nikolaev Radinov, Yi Ren, James Anderson Wright
Abstract: Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.
Type:
Application
Filed:
July 11, 2012
Publication date:
December 6, 2012
Inventors:
Jiazhong Zhang, Prabha N. Ibrahim, Dean R. Artis, Ryan Bremer, Guoxian Wu, Hongyao Zhu, Marika Nespi, Chao Zhang
Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
Type:
Application
Filed:
December 3, 2010
Publication date:
December 6, 2012
Applicant:
Targacept, Inc.
Inventors:
Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Ronald Joseph Heemstra, Srinivasa V. Murthy, Jon-Paul Strachan, Yunde Xiao
Abstract: The subject matter of the present invention are compounds corresponding to formula (I): in which: X is an unsubstituted or substituted divalent (C1-C5)alkylene radical; RI is an —NR8R9 group; or an unsubstituted or substituted piperidin-3-yl or piperidin-4-yl radical; R2 is a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R3 is a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R4 is a hydrogen atom, a halogen atom, an Alk group, a hydroxyl or an OAlk group; and R5 is a hydrogen atom, a halogen atom, an Alk group, a hydroxyl or an OAlk group.
Abstract: The present invention relates to compounds of formula: in which A, Cy, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the description. The compounds of the invention are modulators of the NURR-1 nuclear receptors.
Abstract: Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula I: wherein A, B, D, E, R1 to R3 and n are described herein. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.
Type:
Application
Filed:
March 1, 2012
Publication date:
November 29, 2012
Applicant:
NPS Pharmaceuticals, Inc.
Inventors:
Louise Edwards, Abdelmalik Slassi, Ashok Tehim, Tao Xin
Abstract: The present application is directed to novel P2X7R antagonists that are indol-3-carboxamide or azaindole-3-carboxamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.
Abstract: Compounds of Formula (I), wherein substituents R1, R2 and R5 are as defined, and Ar represents substituted phenyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, furanyl, imidazolyl and thiophenyl substituted by a hydroxyalkyl substituent and an optional other substituent; compositions containing them, their use in therapy, including their use as antibacterials, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
Type:
Grant
Filed:
January 15, 2010
Date of Patent:
November 27, 2012
Assignee:
Glaxo Group Limited
Inventors:
Carlos Alemparte-Gallardo, David Barros-Aguirre, Monica Cacho-Izquierdo, Jose Maria Fiandor Roman, Jose Luis Lavandera Diaz, Modesto Jesús Remuiñan-Blanco
Abstract: Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
Type:
Application
Filed:
July 6, 2012
Publication date:
November 22, 2012
Applicant:
Pharmacyclics, Inc.
Inventors:
Lee Honigberg, Erik J. Verner, Joseph J. Buggy, David J. Loury, Wei Chen
Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, A, E, G and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used for the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease or non-alcoholic steatohepatitis.
Type:
Application
Filed:
May 4, 2012
Publication date:
November 22, 2012
Inventors:
Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch
Abstract: Compounds of formula I in free or salt or solvate form, wherein X, T1, T3 and T4 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
Type:
Grant
Filed:
January 9, 2009
Date of Patent:
November 20, 2012
Assignee:
Novartis AG
Inventors:
Catherine Leblanc, Robert Alexander Pulz, Nikolaus Johannes Stiefl
Abstract: This invention encompasses to obtain non-convertible solid pharmaceutical formulations of moxifloxacin anhydrous by using of wet granulation with an organic solvent or mixtures of organic solvents.
Type:
Grant
Filed:
October 9, 2008
Date of Patent:
November 20, 2012
Assignee:
Abdi Ibrahim Ilac Sanayi Ve Ticaret Anonim Sirketi
Inventors:
Farhad Farshi, Recep Avci, Fikret Koc, Serdar Soylemez
Abstract: The present invention relates to imidazolone derivatives of formula (I) to methods of preparing such derivatives, intermediates thereto, pharmaceutical compositions comprising such derivatives, and methods of inhibiting protein kinase, and methods of treatment comprising administration of such derivatives.
Type:
Grant
Filed:
March 31, 2009
Date of Patent:
November 20, 2012
Assignee:
Sanofi
Inventors:
Vincent Leroy, Eric Bacque, Emmanuel Conseiller, Anke Steinmetz, Baptiste Ronan, Jean-Philippe Letallec
Abstract: Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.
Type:
Application
Filed:
July 6, 2012
Publication date:
November 15, 2012
Applicant:
NEOPHARM CO., LTD.
Inventors:
Tae-Seong KIM, Eunkyung LEE, Doyoung KIM, Bu-mahn PARK, Jiyeon PARK, JungJe JOO
Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.
Type:
Application
Filed:
July 24, 2012
Publication date:
November 15, 2012
Applicant:
LIFE TECHNOLOGIES CORPORATION
Inventors:
Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
Abstract: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
Type:
Application
Filed:
July 26, 2012
Publication date:
November 15, 2012
Inventors:
Nicholas D. Cosford, Thomas J. Seiders, Joseph E. Payne, Jeffrey R. Roppe, Dehua Huang, Nicholas D. Smith, Steve F. Poon, Chris King, Brian W. Eastman, Bowei Wang, Jeannie M. Arruda, Jean-Michel Vernier, Xiumin Zhao
Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
Type:
Grant
Filed:
June 3, 2009
Date of Patent:
November 6, 2012
Assignee:
Intermune, Inc.
Inventors:
Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
Abstract: The present invention provides a compound which indicates a histamine H4 receptor modulating activity. A compound represented by a formula (I): wherein A ring is a ring represented by the following formula: wherein R1 is substituted or unsubstituted alkyl, etc., W is —O—, etc., n is an integer of 0 to 6; X is —N(R7)— or —O—; R7 is hydrogen, substituted or unsubstituted alkyl, etc.; Y is —C(R8)? or —N?; R8 is hydrogen, substituted or unsubstituted alkyl, etc.; Z is ?O, ?S, etc.; B ring is a ring represented by the following formula: wherein R10 is each independently substituted or unsubstituted alkyl, halogen, hydroxy, substituted or unsubstituted alkyloxy, substituted or unsubstituted amino; R11, R12a and R12b are each independently hydrogen or substituted or unsubstituted alkyl, etc.; p is an integer of 0 to 4, or its pharmaceutically acceptable salt, or a solvate thereof.
Abstract: Two novel crystalline forms, designated form A and form B of the antibacterial agent 1-cyclopropyl-7-([S,S])-2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride of formula, the preparation thereof, and their pharmaceutical compositions are described. These crystalline forms, which are characterized by greater stability and ease of preparation and of formulation, can be produced by industrially applicable methods which comprise the steps of: a) suspending 1-cyclopropyl-7-([S,S])-2,8-diazabicyclo-[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride in a solvent selected from an alcohol and a polyalcohol, b) heating the mixture under reflux, c) cooling, d) isolating the product which is separated, (form A) and, additionally, e) reslurrying the solid at reflux in a solvent selected from alcohols and polyols or mixtures thereof, in which the resulting mixture has an overall water content of between 2.
Type:
Application
Filed:
June 29, 2012
Publication date:
November 1, 2012
Applicant:
CHEMI S.P.A.
Inventors:
Stefano TURCHETTA, Pietro MASSARDO, Valentina AROMATARIO
Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Type:
Application
Filed:
July 22, 2010
Publication date:
November 1, 2012
Inventors:
Amanda E. Sutton, Nadia Brugger, Thomas E. Richardson, Harold George Vandeveer, Bayard R. Huck, Ruoxi Lan, Justin Potnick