Double Bonded Divalent Chalcogen Containing Patents (Class 544/131)
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Patent number: 8518972Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: GrantFiled: February 10, 2011Date of Patent: August 27, 2013Assignee: Celgene CorporationInventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
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Publication number: 20130217650Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: November 15, 2012Publication date: August 22, 2013Applicant: Allergan, Inc.Inventor: Allergan, Inc.
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Publication number: 20130217686Abstract: A novel methylcyclohexane derivative, and a pharmaceutical composition including the same that is effective for the prevention or treatment of pain.Type: ApplicationFiled: September 28, 2011Publication date: August 22, 2013Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Sung Jin Bae, Han Ju Yi, Sun Gwan Hwang, Mo Ses Jeong, Yeo Jin Yoon, Sang Mi Chae, Joo Young Park, Eun Ju Ryu
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Publication number: 20130217660Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.Type: ApplicationFiled: May 12, 2011Publication date: August 22, 2013Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
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Patent number: 8513257Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: December 30, 2011Date of Patent: August 20, 2013Assignee: Cytokinetics, IncorporatedInventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, Jr.
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Publication number: 20130210822Abstract: The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning calorimetry profile, as well as a unique crystalline structure.Type: ApplicationFiled: September 13, 2012Publication date: August 15, 2013Applicant: Kinex Pharmaceuticals, LLCInventors: David G. Hangauer, JR., Debasis Patra, Jeremy A. Cody, Grant J. Palmer, Paul K. Isbester, Jonathon Salsbury
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Publication number: 20130210721Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: MOCHIDA PHARMACEUTICAL CO., LTD.
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Publication number: 20130210773Abstract: In one aspect, the invention relates to indole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 21, 2011Publication date: August 15, 2013Inventor: Craig W. Lindsley
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Publication number: 20130211075Abstract: The present invention relates to a novel amide derivative. More specifically, the present invention provides a medicinal agent useful as a prophylactic or therapeutic agent for diseases, which relies on the production of cytokines from T cells, and which comprises an amide derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or the pharmacologically acceptable salt as an active ingredient. Provided is an amide derivative represented by general formula (I) [wherein each symbol is as defined in the description] or a pharmacologically acceptable salt thereof, or a solvate of the derivative or the pharmacologically acceptable salt.Type: ApplicationFiled: October 13, 2011Publication date: August 15, 2013Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Hiroyuki Ushio, Maiko Hamada, Masayuki Watanabe, Atsushi Numata, Naoto Fujie, Tooru Takashima, Hiroyuki Furukawa, Junki Ando
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Publication number: 20130203757Abstract: The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed.Type: ApplicationFiled: November 16, 2012Publication date: August 8, 2013Applicants: THE GENERAL HOSPITAL CORPORATION, CANTHERA THERAPEUTICS INC.Inventors: Canthera Therapeutics Inc., The General Hospital Corporation
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Patent number: 8501943Abstract: The present disclosure is directed to the sodium salt of 5-cyclopropyl-2-{[2-(2,6-difluorophenyl)pyrimidin-5-yl]amino}benzoic acid, pharmaceutically acceptable solvates thereof, pharmaceutical combinations thereof, and methods of treatment.Type: GrantFiled: March 11, 2010Date of Patent: August 6, 2013Assignee: Almirall, S.A.Inventors: Nuria Garcia Gonzalez, Francesc Carrera Carrera, Monserrat Julia Jane, Laurent Debethune, Xavier Serra Masia
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Publication number: 20130196960Abstract: The present disclosure relates to compounds useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders either alone or in combination therapy.Type: ApplicationFiled: February 9, 2011Publication date: August 1, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Jason Rohde, Charles Kim, Takashi Nakai, Galen John Carey
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Publication number: 20130196975Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4, m and n are defined as in the specification, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: March 12, 2013Publication date: August 1, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Tobias WUNBERG, Siegfried SCHNEIDER, Lars VAN DER VEEN
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Publication number: 20130196984Abstract: The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.Type: ApplicationFiled: March 13, 2013Publication date: August 1, 2013Applicants: Siena Biotech S.p.A., Hoffmann-La Roche Inc.Inventors: Hoffmann-La Roche Inc., Siena Biotech S.p.A.
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Publication number: 20130190286Abstract: The present invention encompasses compounds of general formula (1) where in the groups R0to R3 and L are defined as in claim 1, which are suitable for the 5 treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: ApplicationFiled: March 25, 2011Publication date: July 25, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Publication number: 20130190312Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Such compounds disrupt Nek2/Hec1 binding and may be useful as chemotherapeutic agents for neoplastic diseases.Type: ApplicationFiled: November 29, 2012Publication date: July 25, 2013Inventors: Jiann-Jyh HUANG, Shih-Hsien CHUANG, Ying-Shuan Eda LEE, Yu-Ling HUANG, Johnson LAU
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Publication number: 20130190290Abstract: The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: January 23, 2013Publication date: July 25, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventor: BAYER INTELLECTUAL PROPERTY GmbH
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Publication number: 20130190488Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.Type: ApplicationFiled: December 12, 2012Publication date: July 25, 2013Applicant: Abbott LaboratoriesInventor: Abbott Laboratories
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Publication number: 20130184259Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.Type: ApplicationFiled: November 16, 2012Publication date: July 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: VERTEX PHARMACEUTICALS INCORPORATED
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Patent number: 8481750Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: May 28, 2010Date of Patent: July 9, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Jennifer A. Kowalski, Matt Aaron Tschantz
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Patent number: 8476269Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: GrantFiled: July 9, 2012Date of Patent: July 2, 2013Assignee: Novartis AGInventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Legrand, Katrin Spiegel
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Patent number: 8476278Abstract: The present invention relates to novel Thiazole Derivatives, compositions comprising the Thiazole Derivatives, and methods for using the Thiazole Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.Type: GrantFiled: October 27, 2008Date of Patent: July 2, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Panduranga Adulla P. Reddy, Tzu T. Wong, Lianyun Zhao, Shuyi Tang, Marc A. Labroli, Timothy J. Guzi, M. Arshad Siddiqui
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Patent number: 8476257Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: GrantFiled: December 3, 2008Date of Patent: July 2, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
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Publication number: 20130165441Abstract: The present invention is directed to novel polymorphs and salts of a compound which is an inhibitor of kinase activity.Type: ApplicationFiled: September 6, 2011Publication date: June 27, 2013Applicant: GlaxoSmithKline Intellectual Property Development LimitedInventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Charlotte Jane Mitchell, Nigel James Parr, Robert David Willacy
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Publication number: 20130165412Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.Type: ApplicationFiled: September 14, 2012Publication date: June 27, 2013Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
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Patent number: 8470819Abstract: This invention provides compounds of Formula I which are PAFR antagonists: I and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.Type: GrantFiled: October 26, 2009Date of Patent: June 25, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Lin Chu, Anthony Ogawa, Hyun O. Ok, Feroze Ujjainwalla
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Publication number: 20130158002Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.Type: ApplicationFiled: February 28, 2011Publication date: June 20, 2013Inventors: Mark E. Layton, Michael J. Kelly, Timothy J. Hartingh
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Publication number: 20130158020Abstract: The present invention provides a compound of the Formula I: Formula I or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, R4, X, m and n are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.Type: ApplicationFiled: August 29, 2011Publication date: June 20, 2013Inventors: Yongqi Deng, Gerald W. Shipps, JR., Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Kiran Muppalla
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Publication number: 20130158034Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: June 21, 2012Publication date: June 20, 2013Applicant: Amgen Inc.Inventors: James BROWN, Jian J. CHEN, Vijay Keshav GORE, Scott HARRIED, Daniel B. Horne, Matthew R. KALLER, Qingyian LIU, Holger MONENSCHEIN, Thomas T. NGUYEN, Nobuko NISHIMURA, Wenge ZHONG
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Publication number: 20130143880Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. 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 metabotropic glutamate receptors are involved, such as schizophrenia.Type: ApplicationFiled: August 5, 2011Publication date: June 6, 2013Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
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Publication number: 20130137648Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: January 23, 2013Publication date: May 30, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Patent number: 8449936Abstract: A method of providing a range of flavors to an orally-receivable or ingestible product, the method including adding at least one compound, including salts thereof, of the formula: wherein R1 may be H, OH, O(CH2)2OH, OCH2OCH3 or R2 may be selected from a range of 5- and 6-membered heterocyclic rings, and wherein R3 may be H or OH. The compounds give rise to a wide range of flavors, and some are useful as sweetness enhancers, this allowing sweetener content to be reduced while maintaining sweetness. Also disclosed are orally-receivable or ingestible products including the compounds.Type: GrantFiled: February 20, 2009Date of Patent: May 28, 2013Assignee: Givaudan SAInventors: Andrew Daniher, Yili Wang
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Patent number: 8450314Abstract: A compound formula (IA) or (IB), or a pharmaceutically acceptable thereof; wherein the substituents are defined as in the claims, and their use as P38 MAP kinase.Type: GrantFiled: February 16, 2010Date of Patent: May 28, 2013Assignee: Chiesi Farmaceutici S.p.A.Inventors: Amanda Beswick, Bohdan Waszkowycz
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Patent number: 8450316Abstract: Disclosed are 6-(morpholinoalkyl)-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications.Type: GrantFiled: June 24, 2011Date of Patent: May 28, 2013Assignees: Trustees of Tufts College, Arisaph Pharmaceuticals, Inc.Inventors: William W. Bachovchin, Hung-sen Lai, Daniel Philip O'Connell, Wengen Wu, Christopher P. Kiritsy
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Publication number: 20130131056Abstract: The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4?, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.Type: ApplicationFiled: January 15, 2013Publication date: May 23, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130123260Abstract: The disclosure relates to compounds of formula (I) for use in the treatment or prophylaxis of rhinovirus infection, methods of treating or preventing rhinovirus infection employing said compounds or pharmaceutical composition comprising the same. The disclosure also relates to compounds of formula (I) for use in the treatment or prophylaxis of exacerbation of respiratory disorders (such as asthma, COPD, bronchitis and/or cystic fibrosis) by rhinovirus infection.Type: ApplicationFiled: June 17, 2011Publication date: May 16, 2013Applicant: RESPIVERT LIMITEDInventors: Catherine Elisabeth Charron, Kazuhiro Ito, William Garth Rapeport
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Publication number: 20130123259Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: December 20, 2012Publication date: May 16, 2013Applicant: Allergan, Inc.Inventor: Allergan, Inc.
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Publication number: 20130123234Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: December 20, 2012Publication date: May 16, 2013Applicants: EISAI R&D MANAGEMENT CO., LTD., EPIZYME, INC.Inventors: EPIZYME, INC., EISAI R&D MANAGEMENT CO., LTD.
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Publication number: 20130116230Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: December 20, 2012Publication date: May 9, 2013Applicant: INCYTE CORPORATIONInventor: Incyte Corporation
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Publication number: 20130116214Abstract: The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. The present invention provides a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof.Type: ApplicationFiled: July 14, 2011Publication date: May 9, 2013Inventors: Osamu Ujikawa, Kazuaki Takami, Nobuyuki Takakura, Nozomu Sakai
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Publication number: 20130116216Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.Type: ApplicationFiled: November 12, 2010Publication date: May 9, 2013Inventors: Celia Dominguez, John Wityak, Michael Prime, Stephen Martin Courtney, Christopher Yarnold, Frederick Brookfield, Richard Marston, Douglas Macdonald
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Publication number: 20130116430Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.Type: ApplicationFiled: December 28, 2012Publication date: May 9, 2013Applicant: FUJIFILM CORPORATIONInventors: Hideyasu FUJIWARA, Kimihiko SATO, Shinsuke MIZUMOTO, Yuichiro SATO, Hideki KURIHARA, Yohei KUBO, Hiyoku NAKATA, Yasutaka BABA, Takashi TAMURA, Hidenobu KUNIYOSHI, Shinji HAGIWARA, Mari YAMAMOTO
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Publication number: 20130109652Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.Type: ApplicationFiled: December 20, 2012Publication date: May 2, 2013Applicants: Addex Pharmaceuticals S.A., Janssen Pharmaceuticals, Inc.Inventors: Janssen Pharmaceuticals, Inc., Addex Pharmaceuticals S.A.
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Publication number: 20130109686Abstract: The present invention is directed to isoindolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: June 27, 2011Publication date: May 2, 2013Inventors: Douglas C. Beshore, Scott D. Kuduk, Youheng Shu, Zhi-Qiang Yang
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Publication number: 20130102600Abstract: The present invention relates to a compound having the general formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicants: F. HOFFMANN-LA ROCHE LTD, EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL), SAVIRA PHARMACEUTICALS GMBHInventors: F. HOFFMANN-LA ROCHE LTD, SAVIRA PHARMACEUTICALS GMBH, EUROPEAN MOLECULAR BIOLOGY LABORAT
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Publication number: 20130102592Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted en by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: December 5, 2012Publication date: April 25, 2013Applicant: SAREUM LIMITEDInventor: Sareum Limited
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Publication number: 20130102607Abstract: Medicinal use The disclosure relates to compounds of formula (I) for use in the treatment or prophylaxis of respiratory syncitial virus (RSV) infection in particular viral exacerbation of a respiratory disorder such as bronchitis, asthma, COPD and/or cystic fibrosis, methods of treating or preventing RSV infection employing said compounds or pharmaceutical composition comprising the same.Type: ApplicationFiled: June 17, 2011Publication date: April 25, 2013Applicant: Respivert LimitedInventors: Lindsey Cass, Kazuhiro Ito, William Garth Rapeport, Peter Strong
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Publication number: 20130102778Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 and R2 are as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.Type: ApplicationFiled: October 12, 2012Publication date: April 25, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8426407Abstract: A 1-(substituted aryl)-5-trifluoromethyl-2-(1H)pyridone compounds and pharmaceutical acceptable salts, preparation methods and uses for preparing the drugs for treating fibrosis thereof.Type: GrantFiled: May 24, 2010Date of Patent: April 23, 2013Assignee: Central South UniversityInventors: Gaoyun Hu, Lijian Tao, Jun Chen
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Publication number: 20130096117Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): And salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: October 2, 2012Publication date: April 18, 2013Inventors: Julie Nicole HAMBLIN, Paul Spencer JONES, Suzanne Elaine KEELING, Joelle LE, Nigel James PARR