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: 9505763Abstract: Methods for regulating cancer cell growth and survival, inhibiting cancer cell growth, promoting cancer cell death, and/or treating a cancer make use of antagonists of a type I BMP receptor. In some embodiments the cancer is a lung cancer and the cancer cell is a lung cancer cell.Type: GrantFiled: July 25, 2012Date of Patent: November 29, 2016Assignees: Vanderbilt University, Rutgers, The State University of new JerseyInventors: Charles C. Hong, John Langenfeld
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Patent number: 9493476Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.Type: GrantFiled: December 18, 2014Date of Patent: November 15, 2016Assignee: Array BioPharma, Inc.Inventors: Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, Hong-Woon Yang, Qian Zhao
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Patent number: 9487519Abstract: 5,6-Dialkyl-7-aminotriazolopyrimidines of the formula I in which the substituents are as defined below: R1 is alkyl or alkoxyalkyl, where the aliphatic groups may be substituted as defined in the description; R2 is CHR3CH3, cyclopropyl, CH?CH2 or CH2CH?CH2; R3 is hydrogen, CH3 or CH2CH3; processes for preparing these compounds, compositions comprising them and their use for controlling phytopathogenic harmful fungi.Type: GrantFiled: March 8, 2005Date of Patent: November 8, 2016Assignee: BASF SEInventors: Jordi Tormo i Blasco, Carsten Blettner, Bernd Müller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Joachim Rheinheimer, Peter Schäfer, Frank Schieweck, Anja Schwögler, Oliver Wagner, Matthias Niedenbrück, Maria Scherer, Siegfried Strathmann, Ulrich Schöfl, Reinhard Stierl
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Patent number: 9447104Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.Type: GrantFiled: September 18, 2014Date of Patent: September 20, 2016Assignee: Array BioPharma, Inc.Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
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Patent number: 9447106Abstract: The invention is substituted 4,5-dihydro- and 4,5,6,7-tetrahydro-pyrazolo[1,5-?]pyrimidine compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor, such as inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.Type: GrantFiled: May 27, 2015Date of Patent: September 20, 2016Assignee: BeiGene, Ltd.Inventors: Zhiwei Wang, Yunhang Guo
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Patent number: 9353063Abstract: Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.Type: GrantFiled: November 27, 2012Date of Patent: May 31, 2016Assignee: Bikam Pharmaceuticals, Inc.Inventors: David S. Garvey, Jeremy R. Greenwood, Leah L. Frye
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Patent number: 9278971Abstract: 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: GrantFiled: June 4, 2014Date of Patent: March 8, 2016Assignee: 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: 9255071Abstract: A pharmaceutically acceptable salt, prodrug or derivative compound of the formula I, wherein R1 is selected from H, a (C1-C5) alkyl group and a COR4 group; R2 is selected from H, a (C1-C5) alkyl group and a COR5 group; R3 is selected from H, a (C1-C5) alkyl group, a (C1-C5)-O-alkyl group, a cycloalkyl of (C5-C6) carbon atoms, an aryl group, and an aryl (C1-C5) alkyl group wherein the aryl group can be an unsubstituted aryl or substituted with one or more R6 groups and an NHCOR5 group, or the R2 and R3 groups together with N may form a piperidine, morpholine or piperazine group; R4 is selected from H and a (C1-C5)alkyl group; R5 is selected from an aryl group unsubstituted or substituted with one or more R6, linear or branched(C1-C5) alkyl or pyridyne groups and a pyridine group; R6 is selected from (C1-C5)alkyl groups, halogen and nitro.Type: GrantFiled: January 10, 2013Date of Patent: February 9, 2016Assignees: Consejo Nacional de Investigaciones Cientificas y Técnicas (CONICET), Laboratorios Richmond Sociedad Anónima Comercial Industrial y FinancieraInventors: Gerardo Burton, Fernando Javier Duran, Mario David Martinez, Elvira Zini, Veronica Mora Munoz, Lucila Bertoncello
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Patent number: 9255103Abstract: In one aspect, the invention relates to substituted pyrazolo[1,5-a]pyrazines analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: March 27, 2014Date of Patent: February 9, 2016Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor Macdonald, Han Min Tong, Carrie K. Jones
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Patent number: 9096605Abstract: PI3K? selective compounds having the structureType: GrantFiled: June 29, 2012Date of Patent: August 4, 2015Assignee: GlaxoSmithKline LLCInventors: Hong Lin, Juan Ignacio Luengo, Michael Lee Moore, Junya Qu, Ralph A. Rivero, Rosanna Tedesco, Hongyi Yu
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Patent number: 9045484Abstract: The present invention provides pyridinyl-substituted pyrazolyl pyrimidine small molecule inhibitors of bone morphogenetic protein (BMP) signaling having the structure of formula (I), wherein variables A, B, E, F, X, Y, Z, Ar, L1, R4 and R15 are as defined in the specification. The compounds of the invention are useful in modulating cell growth, differentiation, proliferation, and apoptosis, and thus are 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: July 12, 2013Date of Patent: June 2, 2015Assignees: 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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Patent number: 9034882Abstract: 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: GrantFiled: March 1, 2013Date of Patent: May 19, 2015Assignee: Bristol-Myers Squibb CompanyInventors: 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: 20150126506Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: January 8, 2015Publication date: May 7, 2015Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
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Publication number: 20150126531Abstract: A pharmaceutical composition is provided which includes a pharmaceutically acceptable excipient and a pharmaceutically and physically acceptable amount of a compound selected from the group consisting of Chemical Formulas I-IV as described herein, or a pharmaceutically acceptable salt thereof. Also provided are methods of increasing a level of a defined neurotrophic peptide in an organism or tissue comprising the administration of a pharmaceutically and physically acceptable amount of one or more of the compositions described above, and a method for treating a neurodegenerative disease in a subject in need thereof, the method comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 1.Type: ApplicationFiled: May 3, 2013Publication date: May 7, 2015Applicant: Saint Louis College of PharmacyInventor: John M. Beale
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Patent number: 9023844Abstract: Heterocyclylpyri(mi)dinylpyrazole of the formula (I) in which R1 to R5, X1, U, Q, W, Y, n, a, b have the meanings given in the description, and agrochemically active salts, to their use and to methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants and for reducing mycotoxins in plants and parts of the plants, to processes for preparing such compounds and compositions and treated seed and also to their use for controlling phytopathogenic harmful fungi in agriculture, horticulture, forestry, in animal husbandry, in the protection of materials, in the domestic and hygiene field and for the reduction of mycotoxins in plants and parts of the plants.Type: GrantFiled: October 4, 2012Date of Patent: May 5, 2015Assignee: Bayer Intellectual Property GmbHInventors: Stefan Hillebrand, Amos Mattes, Alexander Sudau, Pierre Wasnaire, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann, Haruko Sawada, Philippe Desbordes, Anne-Sophie Rebstock, Stéphane Brunet, Hélène Lachaise, Philippe Rinolfi
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Patent number: 9018219Abstract: 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: GrantFiled: October 27, 2011Date of Patent: April 28, 2015Assignee: Shionogi & Co., Ltd.Inventors: Moriyasu Masui, Genta Tadano
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Publication number: 20150111874Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: October 3, 2014Publication date: April 23, 2015Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Martin R. TREMBLAY
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Publication number: 20150105377Abstract: The invention discloses methods and compositions for treating or preventing RAF kinase mediated diseases or conditions by administering a compound of Formula 1: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.Type: ApplicationFiled: March 12, 2013Publication date: April 16, 2015Inventors: Joseph M. Gozgit, Victor M. Rivera, William C. Shakespeare, Xiaotian Zhu, David C. Dalgarno
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Patent number: 9006235Abstract: 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: GrantFiled: March 1, 2013Date of Patent: April 14, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Zhizhen Barbara Zheng, Stanley D'Andrea, David R. Langley, B. Narasimhulu Naidu
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Patent number: 8999998Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.Type: GrantFiled: July 2, 2010Date of Patent: April 7, 2015Assignee: Genentech, Inc.Inventors: Paul Gibbons, Emily Hanan, Wendy Liu, Joseph P. Lyssikatos, Steven R. Magnuson, Rohan Mendonca, Richard Pastor, Thomas E. Rawson, Michael Siu, Mark Zak, Aihe Zhou, Bing-Yan Zhu
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Publication number: 20150094310Abstract: The present invention relates to a corticotropin releasing hormone receptor type 1 (CRHR1) antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in a novel group of patients, i.e. patients having corticotropin releasing hormone (CRH) overactivity.Type: ApplicationFiled: April 23, 2013Publication date: April 2, 2015Inventor: Florian Holsboer
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Publication number: 20150073036Abstract: Novel NTRK1 fusion molecules, detection reagents, and uses and kits for evaluating, identifying, assessing and/or treating a subject having a cancer are disclosed.Type: ApplicationFiled: August 29, 2014Publication date: March 12, 2015Inventors: Matthew J. Hawryluk, Doron Lipson, Vincent A. Miller, Philip James Stephens
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Patent number: 8975264Abstract: Disclosed is a novel compound acting as a cannabinoid receptor 1 inhibitor, the compound being a pyrazolo[1,5-a]pyrimidine derivative, a prodrug thereof, an isomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof. The novel compound or the like is useful for preventing or treating diseases mediated by the cannabinoid receptor-1.Type: GrantFiled: August 31, 2011Date of Patent: March 10, 2015Assignee: Amorepacific CorporationInventors: Song Seok Shin, Yong Deog Hong, Kyoung Hee Byoun, Mi Young Park, Jin Kyu Choi, Yang Hui Park, Il Hong Bae, Yung Hyup Joo, Kyung Min Lim, Young Ho Park
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Patent number: 8975254Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.Type: GrantFiled: October 27, 2010Date of Patent: March 10, 2015Assignee: Orion CorporationInventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
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Publication number: 20150065522Abstract: The present invention relates to compounds formula (I): and to salts thereof, wherein R1-R4 and A have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of histone demethylases, such as KDM5. Also included are pharmaceutically acceptable compositions comprising the compounds of the present invention and methods of using said compositions in the treatment of various disorders.Type: ApplicationFiled: September 4, 2014Publication date: March 5, 2015Inventors: Brian K. Albrecht, Steven F. Bellon, Victor S. Gehling, Jean-Christophe Harmange, Yves LeBlanc, Jun Liang, Steven Magnuson, Vicki Tsui, Birong Zhang
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Patent number: 8969341Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: GrantFiled: November 28, 2012Date of Patent: March 3, 2015Assignee: Novartis AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Publication number: 20150051227Abstract: The present invention provides a predictive biomarker whose expression level is useful for identifying patients responsive to a therapeutically effective dose of a CDK inhibitor. In one embodiment of the invention, the predictive biomarker is the ratio of MCL-1 to BCL-xL (MCL-1:BCL-xL ratio) and the CDK inhibitor is SCH 927965 (Dinaciclib).Type: ApplicationFiled: March 27, 2013Publication date: February 19, 2015Applicant: Merck Sharp & Dohme Corp.Inventors: Robert Nolan Booher, Heather A. Hirsch, Leigh Scott Zawel, Stephen Eric Fawell
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Publication number: 20150050355Abstract: A particulate SAE-CD composition is provided. The SAE-CD composition has an advantageous combination of physical properties not found in known solid forms of SAECD. In particular, the SAE-CD composition possesses an advantageous physicochemical and morphological property profile such that it can be tailored to particular uses. The SAE-CD composition of the invention has improved flow and dissolution performance as compared to known compositions of SAE-CD.Type: ApplicationFiled: September 17, 2014Publication date: February 19, 2015Inventors: James D. Pipkin, Gerold L. Mosher, Douglas B. Hecker
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Patent number: 8957077Abstract: 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: GrantFiled: September 26, 2011Date of Patent: February 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher D. Cox, Izzat T. Raheem, John D. Schreier
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Patent number: 8957078Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.Type: GrantFiled: December 6, 2013Date of Patent: February 17, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy Brenchley, Jean-Damien Charrier, Chris Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
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Patent number: 8957064Abstract: 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: GrantFiled: February 2, 2010Date of Patent: February 17, 2015Assignee: Bayer Intellectual Property GmbHInventors: Matthias Vennemann, Thomas Bär, Thomas Maier, Swen Hölder, Gerrit Beneke, Florian Dehmel, Armin Zülch, Andreas Strub, Stuart Ince, Hartmut Rehwinkel, Ningshu Liu, Ulf Bömer, Barbara Beckers
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Publication number: 20150044141Abstract: The present invention provides analog compounds of DPA-713 which specifically bind the translocator protein (TSPO), which is upregulated in activated leukocytes, some malignant tumors and tissues involved in steroid biogenesis. These compounds are linked via a linking moiety to a variety of imaging agents, including, for example, near infra-red dyes. The compounds of the present invention are useful for both pre-clinical near-IR fluorescence imaging (NIRF) and use in optically-guided interventions including NIRF endoscopy. Methods of use in diagnosis and treatment of TSPO related disease are also provided.Type: ApplicationFiled: March 14, 2013Publication date: February 12, 2015Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Martin Gilbert Pomper, Haofan Wang, Catherine Anne Foss
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Patent number: 8946237Abstract: 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: GrantFiled: January 11, 2011Date of Patent: February 3, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: 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: 8946238Abstract: 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: GrantFiled: December 20, 2012Date of Patent: February 3, 2015Assignee: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Hon Chung Hui, Petr Jansa, Richard L. Mackman, Jay P. Parrish, Michael Sangi, Dustin Siegel, David Sperandio, Hai Yang
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Publication number: 20150031667Abstract: Compounds of Formula I: and salts thereof 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 such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.Type: ApplicationFiled: July 1, 2014Publication date: January 29, 2015Inventors: Shelley Allen, Steven Wade Andrews, Kevin Ronald Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Krecher, Jeongbeob Seo
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Publication number: 20150031672Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: October 10, 2014Publication date: January 29, 2015Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
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Patent number: 8940742Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: GrantFiled: March 15, 2013Date of Patent: January 27, 2015Assignee: Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. Castro, Katrina Chan, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Liansheng Li, Tao Liu, Yi Liu, Pingda Ren, Daniel A. Snyder, Martin R. Tremblay
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Patent number: 8937064Abstract: The present invention relates to compounds of formula (I) useful as selective inhibitors of JAK2 kinase. The invention also provides pharmaceutical acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various diseases, conditions or disorders. The invention also provides processes for preparing the compounds of the invention.Type: GrantFiled: June 17, 2010Date of Patent: January 20, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark Ledeboer, Valerie Marone, Michelle Stewart, David Messersmith, John Duffy, Gabriel Martinez Botella, Jon Come, Huai Gao, Albert Pierce, Francesco Salituro
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Publication number: 20150018371Abstract: Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator.Type: ApplicationFiled: March 6, 2013Publication date: January 15, 2015Inventors: Roger D. Cone, Julien A. Sebag, Jacques Pantel, Savannah Y. Williams, David C. Weaver, Gary A. Sulikowski, Craig W. Lindsley, Padma S. Portonova, Chao Zhang
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Patent number: 8921358Abstract: 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: GrantFiled: March 28, 2013Date of Patent: December 30, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Edcon Chang, Matthew H. McNeill, Tracy Duong, Angie Vassar, Takehiro Hirano, Yoshito Terao
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Patent number: 8921380Abstract: Pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of formula [I]: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group, etc., R0 is hydrogen, an alkyl group, etc., E is —C(?O)— or —SO2—, R is a group of formula [i], [ii] or [iii], etc: Ring A is a C3-8 cycloalkyl group optionally fused to a benzene ring or a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom, etc., R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group, etc., one of RA and RB is an alkyl group, etc., and the other is hydrogen, an alkyl group, etc., or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 13, 2012Date of Patent: December 30, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Koichi Tanimoto, Mariko Oi, Yasunori Tsuboi, Yasunori Moritani
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Patent number: 8921379Abstract: Provided is a novel compound represented by the following formula Wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor ? agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.Type: GrantFiled: August 9, 2011Date of Patent: December 30, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuyoshi Maekawa, Hideyuki Igawa
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Publication number: 20140350010Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: November 28, 2012Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Publication number: 20140349993Abstract: Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: October 19, 2012Publication date: November 27, 2014Inventors: Rebecca L. Casaubon, Radha Narayan, Christopher Oalmann, Chi B. Vu
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Publication number: 20140343071Abstract: The instant invention provides a method of treating a cancer, selected from the group consisting of breast cancer, melanoma, colorectal cancer, non-small cell lung cancer and ovarian cancer, by administering a combination of a WEE1 inhibitor and a CHK1 inhibitor, wherein the WEE1 inhibitor is MK-1775 or a pharmaceutically acceptable salt thereof, or MK-3652 or a pharmaceutically acceptable salt thereof, and the CHK1 inhibitor is MK-8776 or a pharmaceutically acceptable salt thereof, or SCH900444 or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 11, 2012Publication date: November 20, 2014Inventors: Stuart Denham Shumway, Carlo Toniatti, Brian Scott Roberts, Melissa M. Martin
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Patent number: 8883801Abstract: 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: GrantFiled: August 22, 2011Date of Patent: November 11, 2014Assignee: 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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Publication number: 20140329807Abstract: The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.Type: ApplicationFiled: July 20, 2012Publication date: November 6, 2014Applicant: TOLERO PHARMACEUTICALS, INC.Inventors: Yong Xu, Benjamin Gary Brenning, Steven G. Kultgen, Xiaohui Liu, Michael Saunders, Koc-Kan Ho
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Publication number: 20140322165Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: ApplicationFiled: July 8, 2014Publication date: October 30, 2014Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
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Publication number: 20140315928Abstract: The present invention is directed at substituted amide compounds, pharmaceutical compositions containing such compounds and the use of such compounds to reduce plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.Type: ApplicationFiled: April 15, 2014Publication date: October 23, 2014Applicant: Pfizer Inc.Inventors: Etzer Darout, Robert Dullea, Julie Jia Li Hawkins, Allyn T. Londregan, Paula M. Loria, Bruce Maguire, Kim F. McClure, Donna N. Petersen, David W. Piotrowski
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Patent number: 8865726Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R2a, R3, n, X and ring B have the meanings given in the specification, are inhibitors of mTOR and are useful in the treatment of diseases which are sensitive to inhibition of mTOR, such as cancers.Type: GrantFiled: September 3, 2010Date of Patent: October 21, 2014Assignee: Array BioPharma Inc.Inventors: Steven W. Andrews, Kevin Ronald Condroski, Lisa A. De Meese, Jay Bradford Fell, John P. Fischer, John A. Josey, Kevin Koch, Yvan Le Huerou, Gregory F. Miknis, Martha E. Rodriguez, George T. Topalov, Eli M. Wallace, Rui Xu