The Additional Ring Is A Hetero Ring Patents (Class 514/326)
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Patent number: 8754095Abstract: The present disclosure relates to a series of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I). wherein R, R1, R2, R3, R4, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I) and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: June 17, 2014Assignee: SanofiInventor: Zhongli Gao
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Patent number: 8754107Abstract: The present invention is directed to novel aminopyrrolidines of formula I pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compounds of formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: GrantFiled: November 16, 2007Date of Patent: June 17, 2014Assignee: AbbVie Inc.Inventors: Dawn M. George, Richard W. Dixon, Michael Friedman, Adrian D. Hobson, Biqin Li, Lu Wang, Xiaoyun Wu, Neil Wishart
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Publication number: 20140162998Abstract: A Pim kinase inhibitor compound having the structure represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit Pim kinase activity and can be used to prepare drugs for treating Pim kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I.Type: ApplicationFiled: February 10, 2014Publication date: June 12, 2014Applicant: Jikai Biosciences, Inc.Inventor: Yu GE
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Publication number: 20140162997Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, ring A, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: June 12, 2014Applicant: Janssen Pharmaceutica NVInventors: Mark Wall, Nalin Subasinghe, Zhihua Sui, Christopher Flores
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Publication number: 20140163001Abstract: Provided is a heterocyclic compound having an ROR?t inhibitory activity.Type: ApplicationFiled: July 27, 2012Publication date: June 12, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Satoshi Yamamoto, Junya Shirai, Atsuko Ochida, Yoshiyuki Fukase, Yoshihide Tomata, Ayumu Sato, Shotaro Miura, Kazuko Yonemori, Ryokichi Koyama
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Publication number: 20140163032Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: February 18, 2014Publication date: June 12, 2014Applicant: ARENA PHARMACEUTICALS, INC.Inventors: BRADLEY TEEGARDEN, Dennis Chapman, Marc Decaire, Peter I. Dosa, Konrad Feichtinger, HONNAPPA JAYAKUMAR, THUY-ANH Tran, Sonja Strah-Pleynet, Jay Xu
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Patent number: 8748431Abstract: Compounds of the formula I Formula (I) wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.Type: GrantFiled: November 25, 2011Date of Patent: June 10, 2014Assignee: Syngenta Participations AGInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta, Fredrik Cederbaum, Guillaume Berthon
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Patent number: 8748412Abstract: Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.Type: GrantFiled: February 2, 2011Date of Patent: June 10, 2014Assignee: Argusina Bioscience Inc.Inventors: Jiayu Liao, Yufeng Hong, Yong Wang, Thomas W. Von Geldern, Kanyin E. Zhang
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Patent number: 8748432Abstract: The present invention provides compounds of formula (I): wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.Type: GrantFiled: February 8, 2012Date of Patent: June 10, 2014Assignee: Syngenta Participations AGInventors: Clemens Lamberth, Sarah Sulzer-Mosse, Fredrik Cederbaum, Guillaume Berthon
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Publication number: 20140155433Abstract: Disclosed is a compound of formula (I): wherein ‘D’, ‘E’, ‘m’, ‘n’ and R1-R4 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.Type: ApplicationFiled: July 2, 2012Publication date: June 5, 2014Applicant: LUPIN LIMITEDInventors: Neelima Sinha, Navnath Popat Karche, Girish Dhanraj Hatnapure, Anil Kashiram Hajare, Venkata P. Palle, Rajender Kumar Kamboj
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Patent number: 8741894Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: GrantFiled: March 17, 2011Date of Patent: June 3, 2014Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Garrett Thomas Potter, Jared Andrew Forrester
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Publication number: 20140148338Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) a thiazolylisoxazoline of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.Type: ApplicationFiled: June 4, 2012Publication date: May 29, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Sebastian Hoffmann, Pierre Wasnaire, Ulrike Wachendorff-Neumann
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Publication number: 20140148383Abstract: Obesity is inhibited by administering to a person in need thereof an effective amount of entacapone ((2E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide), or a pharmaceutically-acceptable salt thereof, particularly in conjunction with a second, different anti-obesity medicament. Pharmaceutical compositions comprise entacapone copackaged or coformulated with a second, different anti-obesity medicament.Type: ApplicationFiled: January 4, 2014Publication date: May 29, 2014Applicant: NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJINGInventors: Niu Huang, Gang Zhi, Jijie Chai, Shiming Peng, Nannan Hou
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Publication number: 20140148443Abstract: Disclosed are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, R1, R2 and R3 are as described in this application, and methods of using the compounds in the treatment of cancer.Type: ApplicationFiled: November 20, 2013Publication date: May 29, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
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Patent number: 8735429Abstract: The invention concerns benzamide compounds of formula (I): compound of formula (I): wherein R1 is a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from C1-4alkyl, C3-4cycloalkyl, C1-4alkoxy and C3-4cycloalkoxy; or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumors or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC).Type: GrantFiled: May 15, 2012Date of Patent: May 27, 2014Assignee: AstraZeneca ABInventors: David Michael Andrews, Elaine Sophie Elizabeth Stokes, Andrew Turner, Michael James Waring
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Patent number: 8735398Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: GrantFiled: November 7, 2012Date of Patent: May 27, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
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Patent number: 8735430Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: September 26, 2012Date of Patent: May 27, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell, Nigel James Blumire, Monika Ermann, Edward Thomas Glenn, Someina Khor, Przemyslaw Zawadzki
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Publication number: 20140140997Abstract: Provided are methods for treating or reducing the likelihood of developing a retroviral infection in a feline, decreasing retroviral virion entry into a feline cell, decreasing retroviral virion budding from a feline cell, or decreasing syncytium transmission in a feline. These methods require the administration of at least one agent that specifically binds to CD11a and/or CD18, or ICAM-1, and/or decreases or prevents the binding of LFA-1 (CD11a/CD18 heterodimer) to ICAM-1. Also provided are veterinary compositions and methods of identifying candidate agents useful for treating or reducing retroviral infection in a feline, decreasing retroviral virion entry into a feline cell, decreasing retroviral virion budding from a feline cell, or decreasing syncytium transmission in a feline.Type: ApplicationFiled: June 15, 2012Publication date: May 22, 2014Applicant: CytoDyn Inc.Inventor: Richard Trauger
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Publication number: 20140142105Abstract: The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, (I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or metabolic syndrome via inhibition of HDAC4.Type: ApplicationFiled: July 6, 2012Publication date: May 22, 2014Applicant: NOVARTIS AGInventors: Christina Hebach, Emilie Joly, Joerg Kallen, James Gilbert Ternois, Marina Tintelnot-Blomley
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Publication number: 20140142139Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.Type: ApplicationFiled: November 15, 2013Publication date: May 22, 2014Inventors: Bruce A. Ellsworth, Jun Shi, William R. Ewing, Elizabeth A. Jurica, Andres S. Hernandez, Ximao Wu
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Patent number: 8729081Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.Type: GrantFiled: October 12, 2009Date of Patent: May 20, 2014Assignee: VM Discovery Inc.Inventor: Jay Jie-Qiang Wu
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Patent number: 8729101Abstract: The present invention relates to a group of novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CB1 receptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I), wherein R and R1-R4 have the meanings given in the specification.Type: GrantFiled: September 2, 2008Date of Patent: May 20, 2014Assignee: Solvay Pharmaceuticals, B.V.Inventors: Cornelis G. Kruse, Josephus H. M. Lange, Arnoldus H. J. Herremans, Herman H. Van Stuivenberg
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Patent number: 8729069Abstract: The invention relates to compounds of structural formula (Ia): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, X4, X6, X10, R1, Y, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: September 28, 2010Date of Patent: May 20, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Gary Bohnert, Shoujun Chen, Yu Xie
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Patent number: 8729269Abstract: The present invention provides agents having antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel substituted piperidino phenyloxazolidinone derivatives, processes for making compounds as well as antimicrobial compositions containing said derivatives as active ingredients and methods of treating bacterial infections with the said derivatives.Type: GrantFiled: February 12, 2010Date of Patent: May 20, 2014Assignee: Wockhardt LimitedInventors: Prasad Keshav Deshpande, Milind Dattatraya Sindkhedkar, Mahesh Shriram Phansalkar, Ravindra Dattatraya Yeole, Shrikant Vinayak Gupte, Yati Chugh, Nitin Shetty, Sachin Subhash Bhagwat, Milind Chintaman Shukla, Noel John De Souza, Mahesh Vithalbhai Patel
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Publication number: 20140135304Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors.Type: ApplicationFiled: June 7, 2011Publication date: May 15, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Ramasastri Kambhampati, Amol Dinakar Deshpande, Adi Reddy Dwarampudi, Narasimhareddy Gangadasari, Sangram Keshari Saraf, Vishwottam Nagaraj Kandikere, Pradeep Jayarajan, Ishtiyaque Ahmad, Mohmadsadik Abdulhamid Mulla, Venkateswarlu Jasti
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Publication number: 20140135314Abstract: Piperidine compounds and pharmaceutically useful salts thereof, a pharmaceutical composition including an effective amount of the racemic or enantiomerically enriched piperidine compounds to treat gastrointestinal diseases, and a method of treating gastrointestinal diseases in a mammal are provided.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Coo-Min CHUNG, Hyung-Jin JUN, Jin-Sung KIM, Hui-Ho KIM, Hye-Kyung MIN, Yong-Gil KIM, Jong-Gil CHOI, Hongwook KIM
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Patent number: 8722681Abstract: This invention provides thiazolylpiperazine derivatives, and N-sulfonyl heterocyclic derivatives including phenyl- and benzyl-thiazolylpiperidine derivatives, and pharmaceutically acceptable salts thereof, which are useful active ingredients for administration in a method for the treatment of an ?-synucleopathy such as Parkinson's disease, diffuse Lewy body disease, traumatic brain injury, amyotrophic lateral sclerosis, Niemann-Pick disease, Hallervorden-Spatz syndrome, Down syndrome, neuroaxonal dystrophy, multiple system atrophy and Alzheimer's disease. This invention also provides methods for making such derivatives, and pharmaceutical compositions including such derivatives together with pharmaceutically acceptable excipients.Type: GrantFiled: February 5, 2010Date of Patent: May 13, 2014Assignee: NV reMYNDInventors: Gerard Griffioen, Veronica Rojas De La Parra, Annick Lauwers
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Patent number: 8722678Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G, W2 and Z are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Also disclosed are compounds of Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G and Z1 are as defined in the disclosure. Also disclosed is the use of the compounds of Formula 1A as intermediates for preparing compounds of Formula 1.Type: GrantFiled: April 15, 2011Date of Patent: May 13, 2014Assignee: E I du Pont de Nemours and CompanyInventors: Mary Ann Hanagan, Eric Allen Marshall
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Publication number: 20140128368Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: June 11, 2012Publication date: May 8, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
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Publication number: 20140127322Abstract: Disclosed are solid forms of 1-[4-[4-[5-(2,6-difluorophenyl)-4,5-dihydro-3-isoxazolyl]-2-thiazolyl]-1-piperidinyl]-2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]ethanone (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are fungicidal compositions comprising a fungicidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other fungicide or insecticide are also disclosed. Also disclosed are methods for controlling plant diseases caused by fungal plant pathogens comprising applying to a plant or portion thereof, or to a plant seed, a fungicidally effective amount of a solid form of Compound 1.Type: ApplicationFiled: January 13, 2014Publication date: May 8, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: MATTHEW RICHARD OBERHOLZER, ROBERT JAMES PASTERIS
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Publication number: 20140128376Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: January 13, 2014Publication date: May 8, 2014Applicant: Genentech, Inc.Inventor: Xiaojing Wang
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Publication number: 20140128406Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or x-N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.Type: ApplicationFiled: June 27, 2012Publication date: May 8, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Fredrik Emil Malcolm Cederbaum
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Publication number: 20140121217Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein A, Y, L, R1, W1 and W2 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: January 2, 2014Publication date: May 1, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Lijun Sun, Jun Jiang, Yu Xie
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Patent number: 8710031Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.Type: GrantFiled: March 7, 2011Date of Patent: April 29, 2014Assignee: PTC Therapeutics, Inc.Inventors: Jeffrey A. Campbell, Atiyya Kahn, James Takasugi, Ellen Welch
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Patent number: 8710083Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, X1, X2, Z, R3, R4, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: March 29, 2010Date of Patent: April 29, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Zhi-Qiang Xia, Junyi Zhang, Gary Bohnert, Shoujun Chen, Yu Xie
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Patent number: 8710088Abstract: The present invention relates to pharmaceutical and diagnostic compositions as well as to the use of the active substances contained therein for preparing a pharmaceutical or a diagnostic composition for the treatment or diagnosis of neurodegenerative disorders or amyloid diseases.Type: GrantFiled: February 11, 2005Date of Patent: April 29, 2014Assignee: Max-Delbruck-Centrum fur Molekulare MedizinInventors: Erich Wanker, Sabine Engemann, Susanne Rautenberg, Annett Boeddrich, Phoebe Markovic, Dagmar Ehrnhöfer, Martin Herbst, Jacqueline Walther
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Patent number: 8710049Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.Type: GrantFiled: July 16, 2012Date of Patent: April 29, 2014Assignee: Bristol-Myers Squibb CompanyInventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu
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Patent number: 8710076Abstract: The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin 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 orexin receptors are involved.Type: GrantFiled: October 15, 2009Date of Patent: April 29, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, Anthony J. Roecker, John D. Schreier
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Publication number: 20140113890Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.Type: ApplicationFiled: December 23, 2013Publication date: April 24, 2014Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shuoming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
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Patent number: 8703807Abstract: The invention provides novel compounds having the general formula (I) wherein R1 and R2 are as described herein, compositions including the compounds, their pharmaceutically acceptable salts and esters and methods of using the compounds.Type: GrantFiled: March 8, 2012Date of Patent: April 22, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Daniel Hunziker, Werner Neidhart
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Patent number: 8703165Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as pesticides.Type: GrantFiled: November 30, 2010Date of Patent: April 22, 2014Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
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Publication number: 20140107111Abstract: The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat type-2 diabetes-associated pain and related symptoms.Type: ApplicationFiled: May 18, 2012Publication date: April 17, 2014Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jose Miguel Vela Hernandez, Maria Isabel Martin Fontelles
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Publication number: 20140107158Abstract: Disclosed herein are methods of treating a patient suffering a cognitive disorder.Type: ApplicationFiled: December 18, 2013Publication date: April 17, 2014Applicant: ALLERGAN, INC.Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
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Publication number: 20140107123Abstract: The invention relates to the treatment and prevention of type I diabetes. More specifically, the invention relates to compounds that treat or prevent the body's immune system from destroying ?-cells (i.e., insulin-producing cells in the pancreatic islets of Langerhans) by inhibition of JNK2, selective inhibition of JNK2, or inhibition of the expression of the MAPK9 gene or gene product. In one embodiment, the present invention contemplates the diagnosis, identification, production, and use of compounds which modulate MAPK9 gene expression or the activity of the MAPK9 gene product including but not limited to, JNK2, the nucleic acid encoding MAPK9 and homologues, analogues, and deletions thereof, as well as antisense, ribozyme, triple helix, antibody, and polypeptide molecules as well as small inorganic molecules. The present invention contemplates a variety of pharmaceutical formulations and routes of administration for such compounds.Type: ApplicationFiled: August 5, 2013Publication date: April 17, 2014Applicant: University of MassachusettsInventors: Roger J. Davis, Anja Jaeschke
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Publication number: 20140107157Abstract: The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation.Type: ApplicationFiled: June 15, 2012Publication date: April 17, 2014Applicant: Research Triangle InstituteInventors: Alan Bradley Fulp, Rangan Maitra, Yanan Zhang, Herbert H. Seltzman
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Patent number: 8697870Abstract: The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Z 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 modulators 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: GrantFiled: November 19, 2008Date of Patent: April 15, 2014Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Amy Qi Han, Darius J. Robinson, Changsheng Zheng, Anlai Wang, Yingxin Zhang
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Publication number: 20140099316Abstract: The present invention relates to novel compounds acting as agonists at S1P (sphingosine-1-phosphate) receptors, compositions containing these compounds, use of these compounds in medicine and their process of preparation.Type: ApplicationFiled: April 10, 2012Publication date: April 10, 2014Applicants: SUN PHARMA ADVANCED RESEARCH COMPANY LTD., BIOPROJETInventors: Marc Capet, Isabelle Berrebi-Bertrand, Philippe Robert, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Rajamannar Thennati, Ranjan Kumar Pal, Biswajit Samanta, Muthukumaran Natarajan Pillai, Japan Nitinkumar Desai, Dijixa Chandubhai Rana, Kaushik Dhanjubhai Prajapati, Sandeep Pankajbhai Pathak, Bhavesh M. Panchal, Jayraj D. Aradhye
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Patent number: 8691806Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.Type: GrantFiled: June 28, 2012Date of Patent: April 8, 2014Assignees: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology LimitedInventors: Valerio Berdini, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hannah Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
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Patent number: 8691848Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1? converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-? inducing factor-(IGIF), or interferon-?-(“IFN-?”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-? production and methods for treating interleukin-1, apoptosis-, and interferon-?-mediated diseases using the compounds and compositions of this invention.Type: GrantFiled: January 22, 2008Date of Patent: April 8, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
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Publication number: 20140094462Abstract: Sonic Hedgehog modulators and methods of use thereof are provided for.Type: ApplicationFiled: February 28, 2013Publication date: April 3, 2014Inventors: Sara Buhrlage, Chris Dockendorff, Mike Foley, Han-Je Kim, Andrew Germain, Lawrence MacPherson, Partha Nag, Stuart Schreiber, Amal Ting, Michel Weiwer, Willmen Youngsaye