The Shared Ring Nitrogen Is Bonded Directly To A Ring Nitrogen Of The Second Ring Of The Bicyclo Ring System (e.g., Pyrazolo[1,5-a]pyrimidine, Etc.) Patents (Class 514/259.3)
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Patent number: 8633199Abstract: The problem to be solved by the present invention is to provide a medicine which is excellent in the treatment of type 2 diabetes, diabetic complications or impaired glucose tolerance. The present invention provides a medicine characterized in that a compound represented by the following general formula (I), a salt thereof, or a solvate thereof, and at least one kind of other diabetic medicine: (wherein R1, R2, R3 and R4 are each a hydrogen atom, a trifluoromethyl group or a C1-3 alkyl group).Type: GrantFiled: May 12, 2009Date of Patent: January 21, 2014Assignee: Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Moritaka Goto, Satoko Yamashita, Keizo Nakaya, Tetsushi Tomoguri, Tsutomu Ishida, Masahiro Fuchigami
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Publication number: 20140011805Abstract: The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.Type: ApplicationFiled: July 12, 2013Publication date: January 9, 2014Inventors: Paul B. Yu, Gregory D. Cuny, Kenneth D. Bloch, Randall T. Peterson, Charles C. Hong
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Publication number: 20140005182Abstract: The present invention is directed to benzoquinazilinone 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: August 29, 2013Publication date: January 2, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Douglas C. Beshore, Christina Ng Di Marco, Thomas J. Greshock
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Patent number: 8618114Abstract: The invention relates to the novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, serotonin 5-HT6 receptor antagonists and pharmaceutical compositions, and also to method for prophylaxis and treatment of various diseases of central nervous system at humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HT6 receptors, in particular, Alzheimer's disease, Parkinson's disease, Huntington's disease, schizophrenia, and other neurodegenerative diseases, cognitive disorders and obesity.Type: GrantFiled: October 6, 2009Date of Patent: December 31, 2013Inventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko, Yan Lavrovsky, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
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Patent number: 8614218Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.Type: GrantFiled: March 25, 2010Date of Patent: December 24, 2013Assignee: Bayer Intellectual Property GmbHInventors: Swen Hölder, Matthias Vennemann, Gerrit Beneke, Armin Zülch, Volker Gekeler, Thomas Beckers, Astrid Zimmermann, Hemant Joshi
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Patent number: 8609669Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein R1, R2, R3, R4, and R5 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: GrantFiled: November 2, 2011Date of Patent: December 17, 2013Assignee: AbbVie Inc.Inventors: Xiangdong Xu, Jennifer Van Camp, Marc J. Scanio, William H. Bunnelle, Lei Shi, Augustine T. Osuma, David DeGoey, Arturo Perez-Medrano, Sridhar Peddi, Jyoti R. Patel
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Patent number: 8609668Abstract: A pharmaceutical composition comprising an effective amount of a compound of formulas (I-III) and a pharmaceutically acceptable carrier. Methods for treating a hepatitis virus in a patient comprising administering an effective amount of the compound of formulas (I-III) are also presented.Type: GrantFiled: May 4, 2007Date of Patent: December 17, 2013Assignees: Philadelphia Health & Education Corporation, Institute For Hepatitis and Virus ResearchInventors: Andrea Cuconati, Timothy M. Block, Xiaodong Xu
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Publication number: 20130331401Abstract: The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R1, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.Type: ApplicationFiled: August 13, 2013Publication date: December 12, 2013Applicant: Ferrer Internactional, S.A.Inventors: Luis Anglada, Albert Palomer, Antonio Guglietta
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Publication number: 20130324547Abstract: Embodiments of the disclosure relate to tetrahydropyrazolopyrimidine compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritisType: ApplicationFiled: May 31, 2013Publication date: December 5, 2013Inventors: Roch Boivin, Eric Carlson, Atsushi Endo, Hans Hansen, Lynn D. Hawkins, Sally Ishizaka, Matthew Mackey, Sridhar Narayan, Takashi Satoh, Shawn Schiller
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Publication number: 20130324525Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: August 6, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
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Publication number: 20130317002Abstract: Compounds of formula (I) or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6, R7, m and n have the meanings as given in the description and the claims, which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.Type: ApplicationFiled: February 2, 2010Publication date: November 28, 2013Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventor: Barbara Beckers
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Publication number: 20130317021Abstract: The present invention relates to a compound having the general formula (C), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: May 23, 2013Publication date: November 28, 2013Inventors: Andrea WOLKERSTORFER, Oliver Szolar, Norbert Handler, Stephen Cusack, Thibault Sauvaitre, Céline Simon, Christophe Morice, Bruno Giethlen, Thierry Langer, Mark Smith, Sung-Sau So, Dirk Classen-Houben, Helmut Buschmann
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Publication number: 20130317022Abstract: The present invention relates to a compound having the general formula (A), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: May 23, 2013Publication date: November 28, 2013Applicants: European Molecular Biology Laboratory, F. Hoffmann-La Roche AGInventors: Andrea WOLKERSTORFER, Oliver SZOLAR, Norbert HANDLER, Stephen CUSACK, Thibault SAUVAITRE, Céline SIMON, Christophe MORICE, Bruno GIETHLEN, Thierry LANGER, Mark SMITH, Sung-Sau SO, Dirk CLASSEN-HOUBEN, Helmut BUSCHMANN
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Patent number: 8591943Abstract: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.Type: GrantFiled: April 8, 2010Date of Patent: November 26, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Yongqi Deng, Binyuan Sun, Hongbo Zeng, Matthew Richards, Gerald W. Shipps, Jr., Cliff C. Cheng, Yinyan Zhao, Andrew McRiner, Zhaoyang Meng, Yang Nan, Mehul F. Patel, Iwona E. Wrona, Panduranga Adulla Reddy, Brian M. Eklov, Shuyi Tang, Duan Liu, Amit K. Mandal, Lianyun Zhao, M. Arshad Siddiqui
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Patent number: 8586576Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: February 23, 2007Date of Patent: November 19, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Marc Labroli, Kartik M. Keertikar
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Patent number: 8586594Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.Type: GrantFiled: May 31, 2012Date of Patent: November 19, 2013Assignee: AbbVie Inc.Inventors: Andrew J. Souers, Ju Gao, Todd M. Hansen, Rajesh R. Iyengar, Philip R. Kym, Bo Liu, Zhonghua Pei, Vince S. Yeh, Gang Zhao, Zhili Xin
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Patent number: 8586581Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or 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) and they are therefore useful for the treatment of diseases related to this receptor.Type: GrantFiled: December 10, 2010Date of Patent: November 19, 2013Assignee: Hoffmann-La Roche IncInventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 8580782Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or compositions.Type: GrantFiled: April 20, 2007Date of Patent: November 12, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Marc A. Labroli, Kartik M. Keertikar
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Publication number: 20130296319Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: ApplicationFiled: July 11, 2013Publication date: November 7, 2013Inventors: Scott William Bagley, David Andrew Griffith, Daniel Wei-Shung Kung
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Patent number: 8575177Abstract: The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds.Type: GrantFiled: November 15, 2010Date of Patent: November 5, 2013Assignee: Senhwa Biosciences, Inc.Inventors: Mustapha Haddach, Joe A. Tran, Fabrice Pierre, Collin F. Regan, Nicholas B. Raffaele, Suchitra Ravula, David M. Ryckman
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Patent number: 8552005Abstract: The present invention relates to novel substituted 3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1 pharmaceutically acceptable salts and/or hydrates, to novel serotonin 5-HT6 receptor antagonists, to novel drug substances, pharmaceutical compositions, medicaments and methods for their preparation and use for treatment and prophylaxis of pathological states and diseases of CNS, pathogenesis of which is associated with disturbance of serotonin 5-HT6 receptor activation. In compounds of general formula 1 Ar represents optionally substituted aryl or heterocyclyl; R1, R2 and R3 independently of each other represent hydrogen, C1-C3 alkyl or phenyl; R4 represents hydrogen, optionally substituted C1-C5 alkyl, substituted hydroxyl group or substituted sulfanyl group.Type: GrantFiled: January 23, 2009Date of Patent: October 8, 2013Assignee: Avincuro Pharmaceuticals, Inc.Inventors: Andrey Alexandrovich Ivashchenko, Alexander Vasilievich Ivashchenko, Nikolay Filippovich Savchuk
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Patent number: 8552006Abstract: The present invention relates to compounds of formula IVA, formula IVB, or formula IVC, useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.Type: GrantFiled: June 11, 2010Date of Patent: October 8, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Peter D. J. Grootenhuis, Albert Pierce, Lev T. D. Fanning
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Patent number: 8546406Abstract: Compounds of the formula I, in which D, X, Y, Z, R and R1 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumors.Type: GrantFiled: December 22, 2009Date of Patent: October 1, 2013Assignee: Merck Patent GmbHInventors: Timo Heinrich, Frank Zenke, Mireille Krier, Kai Schiemann
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Publication number: 20130252951Abstract: The compounds of formula (I) are antagonists of the CCR2 receptor Wherein R1-7 and A are as defined in the claims.Type: ApplicationFiled: September 26, 2011Publication date: September 26, 2013Applicant: Proximagen LimitedInventors: Joe William Boyd, Paul Meo, Michael Higginbottom, Iain Simpson, David Mountford, Edward Daniel Savory
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Publication number: 20130237499Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: ApplicationFiled: March 1, 2013Publication date: September 12, 2013Applicant: Bristol-Myers Squibb CompanyInventors: Zhizhen Barbara Zheng, Stanley D'Andrea, David R. Langley, B. Narasimhulu Naidu
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Patent number: 8530482Abstract: The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R1, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.Type: GrantFiled: June 15, 2006Date of Patent: September 10, 2013Assignee: Ferrer Internacional, S.A.Inventors: Luis Anglada, Albert Palomer, Antonio Guglietta
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Publication number: 20130231331Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: ApplicationFiled: March 1, 2013Publication date: September 5, 2013Inventors: Annapurna Pendri, David R. Langley, Samuel Gerritz, Guo Li, Weixu Zhai, Stanley D'Andrea, Manoj Patel, B. Narasimhulu Naidu, Kevin Peese, Zhongyu Wang
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Publication number: 20130231337Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 13, 2013Publication date: September 5, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
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Patent number: 8518944Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: October 25, 2010Date of Patent: August 27, 2013Assignee: Pfizer Inc.Inventors: Chakrapani Subramanyam, Travis T. Wager
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Patent number: 8518943Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: April 6, 2012Date of Patent: August 27, 2013Assignee: UCB Pharma, S.A.Inventors: Benoit Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joel Mercier
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Patent number: 8513276Abstract: The invention relates to new bicyclic heterocyclic derivative compounds of Formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. The compounds of Formula (I) are inhibitors of FGFR, VEGFR or PDGFR.Type: GrantFiled: December 21, 2007Date of Patent: August 20, 2013Assignee: Astex Therapeutics LimitedInventors: Valerio Berdini, Gilbert Ebai Besong, Owen Callaghan, Maria Grazia Carr, Miles Stuart Congreve, Adrian Liam Gill, Charlotte Mary Griffiths-Jones, Andrew Madin, Christopher William Murray, Rajdeep Kaur Nijjar, Michael Alistair O'Brien, Andrew Pike, Gordon Saxty, Richard David Taylor, Emma Vickerstaffe
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Patent number: 8513263Abstract: Compounds of Formula (I) in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.Type: GrantFiled: October 21, 2009Date of Patent: August 20, 2013Assignee: Array BioPharma Inc.Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
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Publication number: 20130210839Abstract: The present invention provides, for example, the following compound: wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, X1—X2?X3 is CR5—CR6?CR7, N—CR6?CR7, CR5—N?CR7 or CR5—CR6?N, R1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2a and R2b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R4a, R4b, R5, R6 and R7 are each independently hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid ? production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid ? proteins.Type: ApplicationFiled: October 27, 2011Publication date: August 15, 2013Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Genta Tadano
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Publication number: 20130210838Abstract: The invention encompasses pyrazolo[1,5-a]pyrimidine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: January 11, 2011Publication date: August 15, 2013Inventors: Jongwon Lim, Brandon M. Taoka, Sandra Lee, Alan Northrup, Michael D. Altman, David L. Sloman, Matthew G. Stanton, Njamkou Noucti
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Patent number: 8507501Abstract: The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.Type: GrantFiled: March 13, 2009Date of Patent: August 13, 2013Assignees: The Brigham and Women's Hospital, Inc., The General Hospital CorporationInventors: Paul B. Yu, Gregory D. Cuny, Kenneth D. Bloch, Randall T. Peterson, Charles C. Hong
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Publication number: 20130203748Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: ApplicationFiled: August 9, 2012Publication date: August 8, 2013Inventors: B. Narasimhulu Naidu, Manoj Patel
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Publication number: 20130203731Abstract: 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.Type: ApplicationFiled: March 28, 2013Publication date: August 8, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventor: TAKEDA PHARMACEUTICAL COMPANY LIMITE LIMITED
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Publication number: 20130203777Abstract: Disclosed herein are compounds and compositions thereof which find use in increasing stability of TTR tetramers reducing its tendency to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of TTR and therby decreasing aggegate formation by TTR. Also disclosed herein are methods to screen for candidate compounds that increase stability of TTR. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.Type: ApplicationFiled: May 5, 2011Publication date: August 8, 2013Inventors: Isabella A. Graef, Mamoun Alhamadsheh
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Publication number: 20130178460Abstract: The present invention relates to the use of novel compounds of Formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: January 10, 2013Publication date: July 11, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130164280Abstract: The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.Type: ApplicationFiled: December 20, 2012Publication date: June 27, 2013Applicant: GILEAD SCIENCES, INC.Inventor: Gilead Sciences, Inc.
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Publication number: 20130150362Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.Type: ApplicationFiled: August 22, 2011Publication date: June 13, 2013Applicant: MERCK SHARP & DOHME CORP.Inventors: Lianyun Zhao, Duan Liu, Shuyi Tang, Amit K. Mandal, Umar Faruk Mansoor, Lalanthi Dilrukshi Vitharana, Panduranga Adulla P. Reddy, M. Arshad Siddiqui
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Patent number: 8461163Abstract: 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, to methods and intermediates useful for making the compounds, and to methods of using the compounds.Type: GrantFiled: March 30, 2009Date of Patent: June 11, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Edcon Chang, Tracy Duong, Takehiro Hirano, Matthew H. McNiell, Yoshito Terao, Angie Vassar
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Patent number: 8461162Abstract: Compounds of the following formula (I) are inhibitors of microtubule affinity regulating kinase, and hence find use in the treatment of neurodegenerative diseases associated with hyperphosphorylation of tau.Type: GrantFiled: July 16, 2008Date of Patent: June 11, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Matthew G. Stanton, Njamkou Noucti, David L. Sloman, Jongwon Lim, Benito Munoz
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Publication number: 20130137707Abstract: The present invention is directed to pyrazolopyrimidine 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: ApplicationFiled: September 26, 2011Publication date: May 30, 2013Inventors: Christopher D. Cox, Izzat T. Raheem, John D. Schreier
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Patent number: 8431582Abstract: The present disclosure describes inhibitors of fatty acid uptake and methods of using such inhibitors. Specifically, the present disclosure describes inhibitors with specificity for FATP2.Type: GrantFiled: August 10, 2012Date of Patent: April 30, 2013Assignee: NUtech VenturesInventors: Concetta DiRusso, Paul Black
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Publication number: 20130102620Abstract: The invention provides a pyrazolopyrimidine derivative of formula (I), wherein, for example, R1 represents —NR1aR1b (wherein R1a and R1b are the same or different and each is a hydrogen atom or aralkyl), R2 represents formula (Ya) [wherein k and m each represents an integer of 0-2, n represents an integer of 0-4, L represents a single bond, R5 represents halogen, R6 represents aryl, X represents —CR8 (wherein R8 represents a hydrogen atom), and R7 represents a hydrogen], R3 represents —SO2R13a [wherein R13a represents lower alkoxy, —NR13dC(?O)R13e (wherein R13d represents a hydrogen atom, and R13e represents lower alkyl)], and R4 represents a hydrogen atom, or a pharmaceutically acceptable salt thereof. The invention also provides a medicament containing the pyrazolopyrimidine derivative, as well as a method of using the pyrazolopyrimidine derivative to prevent and/or treat skin diseases.Type: ApplicationFiled: March 4, 2011Publication date: April 25, 2013Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Keisuke Yamamoto, Seiji Aratake, Kazuki Hemmi
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Publication number: 20130089512Abstract: New heteroaryl imidazolone derivatives having the chemical structure of formula (I) are disclosed, as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: June 14, 2011Publication date: April 11, 2013Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Elena Gomez Castillo, Jordi Bach Taña
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Patent number: 8410118Abstract: The present disclosure describes inhibitors of fatty acid uptake and methods of using such inhibitors. Specifically, the present disclosure describes inhibitors with specificity for FATP2.Type: GrantFiled: August 10, 2012Date of Patent: April 2, 2013Assignee: NUtech VenturesInventors: Concetta DiRusso, Paul Black
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Publication number: 20130079350Abstract: The present invention relates to novel substituted 2-amino-3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, to medicaments, methods for preparation thereof, and to methods for prophylaxis and treatment of various CNS diseases, pathogenesis of which is associated with disturbance of monoaminergic signaling pathways, more specifically over- or hypo-activation of serotonin 5-HT6 receptors.Type: ApplicationFiled: October 9, 2012Publication date: March 28, 2013Inventors: Alexander Vasilievich Ivashtchenko, Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk
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Publication number: 20130078304Abstract: The invention relates to a controlled-release formulation for preventing and/or treating sleep disorders comprising Zaleplon or a pharmaceutically acceptable salt thereof in immediate release form and Zolpidem or a pharmaceutically acceptable salt thereof in sustained release form, wherein Zaleplon or a pharmaceutically acceptable salt thereof and Zolpidem or a pharmaceutically acceptable salt thereof are released in two phases where the first phase is a immediate release phase of Zaleplon or a pharmaceutically acceptable salt thereof and the second phase is a sustained release phase of Zolpidem or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 28, 2011Publication date: March 28, 2013Applicant: TAIWAN BIOTECH CO., LTD.Inventors: HSIEN-JEN HSIEH, KUO-HUA YANG, CHIH-SHENG YANG, YU-CHENG WEI, CHUNG-HSUAN LU