The Diazine Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/116)
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Publication number: 20130178469Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof.Type: ApplicationFiled: July 15, 2011Publication date: July 11, 2013Applicants: SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY (SIOC), AVEXA LIMITEDInventors: David Ian Rhodes, John Joseph Deadman, Giang Thanh Le, Nicholas Andrew Van de Graff, Lu Long, Li Xinming, Feng Xiao, Yu Changjiang
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Publication number: 20130172323Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: May 6, 2011Publication date: July 4, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Grauert, Remko Bakker, Steffen Breitfelder, Frank Buettner, Peter Eickelmann, Thomas Fox, Marc Grundl, Thorsten Lehmann-Lintz, Wolfgang Rist
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Patent number: 8476298Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: GrantFiled: May 24, 2007Date of Patent: July 2, 2013Assignee: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrisson B. Mac, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wie Xu
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Publication number: 20130143871Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.Type: ApplicationFiled: August 12, 2011Publication date: June 6, 2013Inventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
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Publication number: 20130116250Abstract: The invention relates to compounds corresponding to formula (I): in which R2 and R3 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: in which the wavy lines represent the phenyl nucleus to which R2 and R3 are attached. Preparation process and therapeutic use.Type: ApplicationFiled: July 4, 2011Publication date: May 9, 2013Applicant: SANOFIInventors: Chantal Alcouffe, Reinhard Kirsch, Corentin Herbert, Gilbert Lassalle
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Publication number: 20130116233Abstract: The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of 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: ApplicationFiled: October 29, 2012Publication date: May 9, 2013Applicants: AbbVie Inc., Abbott GmbH & Co. KGInventors: Abbott GmbH & Co. KG, AbbVie Inc.
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Publication number: 20130102602Abstract: Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: wherein Ar represents R5, R6, R7, R8, R1?, R2?, R3?, R4?, R5?, R6?, R7?, R8? independently represent H, OH, F, Cl, Br, C1 to C6 alkyl group, C1 to C6 alkoxy group, C2 to C6 alkenyl group, C2 to C6 alkenoxy group, C2 to C6 alkynyl group, C2 to C6 alkynoxy group, amine group, mono- or di-substituted amino group, cyclic C1 to C5 alkylamino group, imidazolyl group, morpholino group, piperazinyl group, optionally substituted with one or more hydroxy or halo; and X represents NH, O or S. The present invention also provides a composition comprising the compound of formula I. The compound and the composition in accordance with the present invention are effective on treating or alleviating a disease or disorder, such as malignant glioma.Type: ApplicationFiled: October 20, 2011Publication date: April 25, 2013Applicant: China Medical UniversityInventors: Mann-Jen Hour, Po-Wu Gean, Sheng-Chu Kuo, Hong-Zin Lee, Jai-Sing Yang, Li-Chen Chou, Tai-Lin Chen
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Publication number: 20130102603Abstract: The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.Type: ApplicationFiled: May 31, 2011Publication date: April 25, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Dieter Dorsch, Alfred Jonczyk, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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Publication number: 20130102576Abstract: Compounds, pyridine N-oxides, and pharmaceutically acceptable salts of formula (I) are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and for preventing and/or treating diseases of the respiratory tract characterized by airway obstruction, such as asthma or COPD.Type: ApplicationFiled: October 19, 2012Publication date: April 25, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Publication number: 20130085142Abstract: The present application relates to: (a) compounds of Formula (I): and salts thereof, wherein Z1, Z2, Z3, Z4, R1, R2, and R3 are as defined in the specification; (b) compositions comprising such compounds and salts; and (c) methods of use of such compounds, salts, and compositions, particularly use as calcium channel inhibitors.Type: ApplicationFiled: September 26, 2012Publication date: April 4, 2013Applicant: ABBVIE INC.Inventor: AbbVie Inc.
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Publication number: 20130085141Abstract: The present application relates to: (a) compounds of Formula (I): and salts thereof, wherein Z?, Z?, L2, G2, R1, and R2 are as defined in the specification; (b) compositions comprising such compounds and salts; and (c) methods of use of such compounds, salts, and compositions, particularly use as calcium channel blockers.Type: ApplicationFiled: September 26, 2012Publication date: April 4, 2013Applicant: ABBVIE INC.Inventor: ABBVie Inc.
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Patent number: 8394801Abstract: The invention provides quinoxalines of the general formula I which are used as medicaments preferably for treating tumour disorders, in particular in cases of drug resistance to other active compounds and in cases of metastasic carcinoma. The possible applications are not limited to tumour disorders.Type: GrantFiled: March 25, 2010Date of Patent: March 12, 2013Assignee: Aeterna Zentaris GmbHInventors: Matthias Gerlach, Irene Seipelt, Eckhard Guenther, Tilmann Schuster, Emmanuel Polymeropoulos, Michael Czech, Eckhard Claus
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Publication number: 20130012489Abstract: The invention relates to compounds of the formulae (I), (II) and (III) in which R1, R2, R3, R4, Y, W1, W2, L, A, Alk, Cyc, Ar, Het1, Het2, Hal and n have the meaning indicated in claim 1, and/or physiologically acceptable salts, tautomers and stereo-isomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of their salts.Type: ApplicationFiled: February 17, 2011Publication date: January 10, 2013Applicant: MERCK PATENT GMBHInventors: Werner Mederski, Thomas Fuchss, Frank Zenke
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Publication number: 20130012506Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.Type: ApplicationFiled: January 13, 2011Publication date: January 10, 2013Inventors: Zaesung No, Jaeseung Kim, Priscille Brodin, Min Jung Seo, Eunjung Park, Jonathan Cechetto, Heekyoung Jeon, EunHye Kim, Jamung Heo, Ji Youn Nam, Denis Philippe Cedric Fenistein, Thierry Christophe, Monica Contreras Dominguez, Auguste Genovesio, Saeyeon Lee, Sunhee Kang, Fanny Anne Ewann
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Patent number: 8338591Abstract: The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions.Type: GrantFiled: May 6, 2005Date of Patent: December 25, 2012Assignee: Novartis International Pharmaceutical Ltd.Inventors: Taeyoung Yoon, Jun Yuan, Kyungae Lee, George D. Maynard, Nian Liu
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Publication number: 20120321967Abstract: Embodiments are related to ionic liquids and more specifically to ionic liquids used in electrochemical metal-air cells in which the ionic liquid includes sulfonate ions as the anion.Type: ApplicationFiled: April 17, 2012Publication date: December 20, 2012Applicant: FLUIDIC, INC.Inventors: Derek WOLFE, Cody A. FRIESEN, Paul Bryan JOHNSON
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Patent number: 8318730Abstract: This invention provides fused heterocyclic compounds, pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12 related disease and disorders.Type: GrantFiled: February 20, 2009Date of Patent: November 27, 2012Assignee: Synta Pharmaceuticals CorporationInventors: Mitsunori Ono, Lijun Sun, Yumiko Wada, Teresa Przewloka, Hao Li, Zachary Demko, Dinesh Chimmanamada
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Patent number: 8318732Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.Type: GrantFiled: July 2, 2009Date of Patent: November 27, 2012Assignee: Avexa LimitedInventors: John Joseph Deadman, Eric Dale Jones, David Ian Rhodes, Nicholas Andrew Van de Graff
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Publication number: 20120263708Abstract: The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.Type: ApplicationFiled: August 24, 2010Publication date: October 18, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Benjamin Bader, Ulf Bömer, Stuart Ince, Marcus Koppitz, Philip Lienau, Tobias Marquardt, Duy Nguyen, Stefan Prechtl, Gerhard Siemeister, Christof Wegscheid-Gerlach
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Publication number: 20120232056Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: ApplicationFiled: March 2, 2012Publication date: September 13, 2012Applicant: BIOENERGENIXInventors: John M. McCall, Donna L. Romero, Robert C. Kelly
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Publication number: 20120225863Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: ApplicationFiled: March 2, 2012Publication date: September 6, 2012Applicant: BIOENERGENIXInventors: John M. McCall, Donna L. Romero
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Publication number: 20120220589Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: ApplicationFiled: January 5, 2012Publication date: August 30, 2012Applicant: BIOENERGENIXInventors: John M. McCall, Donna L. Romero
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Patent number: 8252792Abstract: Thienopyrimidines of formula (Ia) or (Ib): wherein R1-R3 have any of the values described herein, and the pharmaceutically acceptable salt thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase, in particular the p110 delta subtype, such as immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.Type: GrantFiled: April 25, 2007Date of Patent: August 28, 2012Assignee: F. Hoffman-La Roche AGInventors: Stewart James Baker, Paul John Goldsmith, Timothy Colin Hancox, Neil Anthony Pegg, Stephen Price, Stephen Joseph Shuttleworth, Sukhjit Sohal
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Publication number: 20120178915Abstract: This invention relates with the arylheterocycle-fused pyrimidines, derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: A-cycle is of 3-8 saturated or unsaturated arylheterocycles or aliheterocyclic, containing 1-4 heteroatoms, B-cycle 5-8 member saturated or unsaturated heterocycle containing 1-4 heteroatoms; X1, X2, X3, X4 are, independently at each occurrence, C, O, S, Se, N and P elements; R1, R2, R3 is a substituent containing alicyclic group, arylcycle group, heterocyclic group, adamantane alkyl, adamantane heterocycle, adamantane analogs, sugar group, hydroxyl group, amino acid group or a combination of the above substituents. This invention also relates with their preparative methods and applications.Type: ApplicationFiled: December 24, 2009Publication date: July 12, 2012Inventor: Lifeng Xu
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Patent number: 8217037Abstract: Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.Type: GrantFiled: April 5, 2007Date of Patent: July 10, 2012Assignees: Board of Supervisors of Louisiana State University and Agricultural and Mechanical College, B.V. Patel Pharmaceutical Education & Research Development (PERD)Inventors: Anthony Giordano, Kamala K. Vasu, Hardik M. Thakar, Rajan S. Giri, Swapnil G. Yerande, Gajanan S. Inamdar, Vasudevan Sudarsanam
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Patent number: 8211892Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives of Formula (I): as disclosed herein, to their preparation and to their therapeutic application.Type: GrantFiled: July 26, 2010Date of Patent: July 3, 2012Assignee: Sanofi-AventisInventors: Alain Jean Braun, Olivier Crespin, Claudie Namane, Eric Nicolai, Francois Pacquet, Cecile Pascal, Christophe Philippo, Olivier Venier
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Publication number: 20120165318Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: ApplicationFiled: February 29, 2012Publication date: June 28, 2012Applicant: BIOENERGENIXInventors: John M. McCall, John McKearn, Donna L. Romero, Michael Clare
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Patent number: 8193189Abstract: The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R7; R2 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8; R3, R4, R5 and R6 are each independently hydrogen or R9; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases.Type: GrantFiled: June 6, 2008Date of Patent: June 5, 2012Assignee: Novartis AGInventors: Marc Gerspacher, Pascal Furet, Eric Vangrevelinghe, Carole Pissot Sondermann, Christoph Gaul, Philipp Holzer
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Patent number: 8193187Abstract: The compounds represented in general formula (1) or a salt thereof are useful for glucocorticoid receptor modulators. In the formula, R1 represents a lower alkyl group, a lower cycloalkyl group, an aryl group and the like; R2 represents a hydrogen atom, a lower alkyl group and the like; R3 represents a hydrogen atom, a lower alkyl group and the like; R4 and R5 represent a hydrogen atom, a lower alkyl group and the like; R6 represents a hydrogen atom, a lower alkyl group and the like; R7 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group and the like; W represents an oxygen atom, a sulfur atom, NR8 and the like; R8 represents a hydrogen atom, a lower alkyl group and the like; X represents an oxygen atom or a sulfur atom; Y represents a lower alkylene group and the like; Z represents an oxygen atom, a sulfur atom, NR9, OCO or OSO2; R9 represents a hydrogen atom, a lower alkyl group and the like respectively.Type: GrantFiled: May 29, 2008Date of Patent: June 5, 2012Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Mamoru Matsuda, Toshiyuki Mori, Masato Nagatsuka, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
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Publication number: 20120122837Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: September 23, 2011Publication date: May 17, 2012Inventors: CLIFFORD CHENG, GERALD W. SHIPPS, JR., XIAOHUA HUANG, YING HUANG, NING SHAO, ASHWIN RAO, ANANDAN PALANI, PETER ORTH, JOHANNES H. VOIGT, ROBERT J. HERR, LANA MICHELE ROSSITER, QI ZENG, XIANFENG SUN
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Publication number: 20120122863Abstract: Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving Chymase.Type: ApplicationFiled: August 12, 2008Publication date: May 17, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Xin Guo, Ho Yin Lo, Chuk Chui Man, Hidenori Takahashi
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Patent number: 8178532Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: GrantFiled: May 24, 2007Date of Patent: May 15, 2012Assignee: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Timothy Patrick Forsyth, Richard George Khoury, James William Leahy, Morrisson B. Mac, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Yong Wang, Wie Xu
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Publication number: 20120108564Abstract: [Problem] Provided is a novel 1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, or a solvate thereof, which is useful as an anti-HIV agent. [Solving Means] The present invention provides a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof.Type: ApplicationFiled: February 25, 2011Publication date: May 3, 2012Inventors: Susumu MIYAZAKI, Yuki BESSHO, Kaoru ADACHI, Seiji KAWASHITA, Hirotaka ISOSHIMA, Kengo OSHITA, Shunichi FUKUDA
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Patent number: 8158628Abstract: Sulfonylated tetrahydroazolopyrazine compounds corresponding to the formula I wherein R1, R2a, R2b, R3a, R3b, R4, R8, R9a, R9b, R10, R11, A, B, W1, W2 and W3 have the meanings defined herein, pharmaceutical compositions containing such compounds, a method for the preparation of such compounds, and the use of such compounds for treating or inhibiting various types of pain and/or other conditions mediated at least in part by the bradykinin 1 receptor (B1R).Type: GrantFiled: March 4, 2010Date of Patent: April 17, 2012Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Stefan Oberboersch, Melanie Reich, Stefan Schunk, Ruth Jostock, Sabine Hees, Michael Engels, Tieno Germann, Edward Bijsterveld
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Publication number: 20120058987Abstract: The subject matter of the present invention is the use of compounds of formula (I) in the form of a base, a hydrate or a solvate, or of mixtures thereof, as a medicament or for preparing a medicament intended for the treatment and/or prevention of disorders associated with the central nervous system (abbreviated to CNS) and/or associated with the peripheral nervous system (abbreviated to PNS).Type: ApplicationFiled: March 25, 2010Publication date: March 8, 2012Applicant: SANOFIInventors: Gilbert Marciniak, Jean-Francois Nave, Fabrice Viviani
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Publication number: 20120059002Abstract: Disclosed are methods of regulating interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1) and methods of treating and/or preventing cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s) by administering a naturally occurring or synthetic quinazolone derivative. The invention provides novel synthetic quinazolone compounds, as well as pharmaceutical compositions comprising those compounds.Type: ApplicationFiled: April 21, 2010Publication date: March 8, 2012Inventors: Henrik C. Hansen, Gregory S. Wagner, Sarah C. Attwell, Kevin G. McLure, Ewelina B. Kulikowski
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Publication number: 20120040983Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A4, L, R1, R2, R3, R5 and m are as defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, ankylosing spondylitis, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: October 7, 2009Publication date: February 16, 2012Applicant: Amgen Inc.Inventors: Andrew Tasker, James R. Falsey, Robert M. Rzasa, Bradley J. Herberich, Dawei Zhang
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Publication number: 20120040980Abstract: The present invention relates to quinazolinone compounds, processes for their preparation and their use as pharmaceutical agents for the treatment of Parkinson's disease (PD). The quinazolinone compounds are of general formula (I).Type: ApplicationFiled: December 23, 2009Publication date: February 16, 2012Applicant: PRANA BIOTECHNOLOGY LIMITEDInventors: Penelope Jane Huggins, Jack Gordon Parsons
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Patent number: 8101612Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of p38 kinase mediated diseases and related inflammatory conditions. The compounds have a general Formula II wherein L1, L2, R1a, R1b, R1c, R2, R3, R3a, R4, R5 and p are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: September 4, 2007Date of Patent: January 24, 2012Assignee: Amgen Inc.Inventors: Andrew Tasker, Dawei Zhang, Liping H. Pettus, Rob M. Rzasa, Kelvin K. C. Sham, Shimin Xu, Partha Chakrabarti
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Publication number: 20110319380Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: December 17, 2010Publication date: December 29, 2011Applicant: Sunovion Pharmaceuticals Inc.Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
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Publication number: 20110294807Abstract: Disclosed are novel compounds that are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis. Also disclosed are pharmaceutical compositions comprising the novel compounds.Type: ApplicationFiled: January 8, 2010Publication date: December 1, 2011Inventor: Henrik C. Hansen
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Patent number: 8053431Abstract: The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: GrantFiled: November 1, 2006Date of Patent: November 8, 2011Assignee: High Point Pharmaceuticals, LLCInventors: John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
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Publication number: 20110263532Abstract: The present invention provides novel analogs and derivatives of halofuginone. The invention also provides pharmaceutical and cosmetic compositions thereof and methods for using halofuginone analogs in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, ischemic damage, transplant and implant rejection, neurodegenerative diseases, and cosmetic applications.Type: ApplicationFiled: August 11, 2009Publication date: October 27, 2011Applicant: President and Fellows of Harvard CollegeInventors: Tracy Keller, Ralph Mazitschek, Malcolm Whitman, Jinbo Lee
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Patent number: 8044041Abstract: The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives of formula (III) that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: November 14, 2007Date of Patent: October 25, 2011Assignee: Forest Laboratories Holdings LimitedInventors: Gian-Luca Araldi, Matthew Ronsheim, Melanie Ronsheim
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Publication number: 20110251179Abstract: Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: ApplicationFiled: September 17, 2009Publication date: October 13, 2011Applicant: NERVIANO MEDICAL SCIENCES S.r.lInventors: Danilo Mirizzi, Giovanni Cervi, Matteo D'Anello, Gianluca Mariano Enrico Papeo, Ron Ferguson, Francesco Casuscelli
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Patent number: 8034814Abstract: The invention relates to new phthalazine derivatives of formula I, and to processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof alone or in combination with one or more other pharmaceutically active compounds for the treatment especially of a disease that responds to the inhibition of especially the vascular endothelial growth factor receptor kinase, preferably the treatment of a proliferative disease, or the treatment of inflammatory rheumatic or rheumatoid arthritis and/or pain; and the use of such a compound alone or in combination with one or more other pharmaceutically active compounds for the manufacture of a pharmaceutical preparation for the treatment of said diseases in an animal.Type: GrantFiled: November 24, 2010Date of Patent: October 11, 2011Assignee: Novartis AGInventors: Guido Bold, Paul William Manley
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Publication number: 20110230465Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: ApplicationFiled: September 16, 2010Publication date: September 22, 2011Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBHInventors: Timothy STAMMERS, Xavier BARBEAU, Pierre BEAULIEU, Megan BERTRAND-LAPERLE, Christian BROCHU, Paul J. EDWARDS, Pasquale FORGIONE, Cédrickx GODBOUT, Oliver HUCKE, Marc-André JOLY, Serge LANDRY, Olivier LEPAGE, Julie NAUD, Marc PESANT, Martin POIRIER, Maude POIRIER, Bounkham THAVONEKHAM
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Publication number: 20110218196Abstract: The compounds according to formula (VIII), their pharmaceutically acceptable acid or base addition salts, and the uses thereof. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for preparing medicaments for modulating estrogen related receptors (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity. The substituents of the formula are defined in the description.Type: ApplicationFiled: March 6, 2009Publication date: September 8, 2011Inventors: Ke Ding, Chiwai Wong, Lijie Peng, Zhanfang Kang, Xi Zhou
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Patent number: 7998958Abstract: Disclosed are novel gamma secretase inhibitors of the formula: Also disclosed are methods for inhibiting gamma secretase, for treating one or more neurodegenerative diseases, for inhibiting the deposition of beta amyloid protein, and for treating Alzheimer's disease using the compounds of formula (I).Type: GrantFiled: December 8, 2009Date of Patent: August 16, 2011Assignee: Schering CorporationInventors: Hubert B. Josien, John W. Clader, Thomas A. Bara, Ruo Xu, Hongmei Li, Dmitri A. Pissarnitski, Zhiqiang Zhao
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Publication number: 20110195965Abstract: The present invention relates to the use of tetrahydro- and dihydroquinazolinones of formula (I) as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases, their use for the manufacture of a pharmaceutical composition and new tetrahydro- and dihydroquinazolinones.Type: ApplicationFiled: April 12, 2011Publication date: August 11, 2011Inventors: Dirk FINSINGER, Armin De Meijere