Polycyclo Ring System Which Contains The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/211.09)
  • Publication number: 20140378436
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: November 23, 2011
    Publication date: December 25, 2014
    Applicant: Exelixis, Inc.
    Inventor: Kenneth D. Rice
  • Publication number: 20140377332
    Abstract: Nano-constructs comprising nanoshells and methods of using the nano-constructs for treating or ameliorating a medical condition are provided.
    Type: Application
    Filed: November 21, 2013
    Publication date: December 25, 2014
    Inventors: Florian N. Ludwig, Stephen D. Pacetti, Syed F.A. Hossainy, Dariush Davalian
  • Publication number: 20140371202
    Abstract: The present teaching provide indazole compounds represented by Structural Formulae (I) or (I?) or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as TTK protein kinase, polo-like kinase 4 (PLK4) and Aurora kinases having anticancer activity against breast cancer cells, colon cancer cells, and ovarian cancer cells.
    Type: Application
    Filed: October 12, 2012
    Publication date: December 18, 2014
    Applicant: University Health Network
    Inventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter Brent Sampson, Miklos Feher, Donald E. Awrey
  • Patent number: 8906904
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: December 9, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jehrod Burnett Brenneman, John Ginn, Michael D. Lowe, Christopher Ronald Sarko, Edward S. Tasber, Zhonghua Zhang
  • Publication number: 20140349998
    Abstract: The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 27, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Sean P Ahearn, Matthew Christopher, Christopher Dinsmore, Joon Jung, Qinglin Pu, Alexey Rivkin, Mark E. Scott, David J. Witter, Hyun Chong Woo, Brandon Cash
  • Publication number: 20140336169
    Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: May 9, 2014
    Publication date: November 13, 2014
    Applicant: GILEAD CONNECTICUT, INC.
    Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD, James P. HARDING, Antonio J. M. BARBOSA, JR., Zhongdong ZHAO, David M. ARMISTEAD, Soumya MITRA
  • Patent number: 8877742
    Abstract: The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase enzymes.
    Type: Grant
    Filed: June 8, 2012
    Date of Patent: November 4, 2014
    Assignee: GlaxoSmithKline Intellectual Property Limited
    Inventors: Deborah W. Chen, Sarah Duncan, Nigel Paul King, Kiew Ching Lee, Sing Yeung Mak, Dean Andrew Rivers
  • Publication number: 20140323412
    Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 30, 2014
    Inventors: Bronislava Gedulin, Michael Grey, Niall O'Donnell
  • Patent number: 8871756
    Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R10, A, Q, X and Y are as defined in the specification and claims, and their use as a pharmaceutical for the treatment or prophylaxis of respiratory syncytial virus disease.
    Type: Grant
    Filed: July 30, 2012
    Date of Patent: October 28, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Lichun Feng, Song Feng, Lu Gao, Tao Guo, Mengwei Huang, Chungen Liang, Yongfu Liu, Lisha Wang, Jason Christopher Wong, Jim Zhen Wu, Xihan Wu, Hongying Yun, Xiufang Zheng
  • Publication number: 20140315881
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: October 23, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir GHOSH, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Publication number: 20140309184
    Abstract: Embodiments of the present disclosure relate to methods and compositions for treating a subject with ovarian cancer. Some embodiments include treating a subject with a particular combination of chemotherapeutic agents.
    Type: Application
    Filed: July 20, 2012
    Publication date: October 16, 2014
    Applicant: UNIVERSITY OF SOUTH ALABAMA
    Inventors: Rodney P. Rocconi, Lalita Samant
  • Patent number: 8853198
    Abstract: The present invention relates to 1,4-benzothiazepine derivatives and their use to treat conditions, disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel functioning in cells. The invention also discloses pharmaceutical compositions comprising the compounds and uses thereof to treat diseases and conditions associated with RyRs, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders.
    Type: Grant
    Filed: November 11, 2013
    Date of Patent: October 7, 2014
    Assignees: Les Laboratoires Servier, ARMGO Pharma, Inc.
    Inventors: Jiaming Yan, Sandro Belvedere, Yael Webb, Marc Bertrand, Nicole Villeneuve
  • Patent number: 8840923
    Abstract: Slow-release excipients which comprise an association of at least one glycogen and at least one alginate with an alkaline-earth metal salt are useful for the preparation of slow-release pharmaceutical formulations.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: September 23, 2014
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Vincenzo Russo, Elisa Liberati, Nicola Cazzolla, Leonardo Marchitto, Lorella Ragni
  • Publication number: 20140275017
    Abstract: Compounds of Formula I: (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
  • Publication number: 20140243281
    Abstract: Provided herein are pediatric dosage forms for use in the treatment of a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of the pediatric dosage form comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are said pediatric dosage form for use in the treatment of a pediatric liver disease, for use in decreasing the levels of serum bile acids or hepatic bile acids, for use in the treatment of pruritis, for use in reducing liver enzymes or bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: August 28, 2014
    Applicant: Lumena Pharmaceuticals, Inc.
    Inventors: Bronislava Gedulin, Michael Grey, Niall O'Donnell
  • Publication number: 20140221298
    Abstract: The present invention provides an agricultural and horticultural fungicidal composition including a compound A which is at least one selected from a nitrogen-containing heterocyclic compound having a specific structure including a compound represented by the formula (1), and a salt thereof, and a compound B which is at least one selected from the group of specific pesticidally active compounds: in the formula (1), X each independently represents a halogeno group or a C1 to 6 alkyl group; n represents the number of X(s) and is an integer of 0 to 6; and X? represents a halogeno group; and R1, R2 and R3 each independently represent a C1 to 6 alkyl group or a hydroxyl group.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 7, 2014
    Inventor: Raito Kuwahara
  • Publication number: 20140213571
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 20, 2012
    Publication date: July 31, 2014
    Inventors: Nigel J. Liverton, Casey Cameron McComas, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Shuwen He, Xing Dai, Hong Liu, Zhong Lai, Clare London, Dong Xiao, Nicolas Zorn, Ravi Nargund
  • Publication number: 20140200208
    Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
    Type: Application
    Filed: March 17, 2014
    Publication date: July 17, 2014
    Applicants: ADDEX PHARMA, S.A., JANSSEN PHARMACEUTICALS, INC.
    Inventors: JOSE MARIA CID-NUNEZ, ANA ISABEL DE LUCAS OLIVARES, ANDRES AVELINO TRABANCO-SUAREZ, GREGOR JAMES MACDONALD
  • Publication number: 20140187536
    Abstract: Methods for reducing toxicity or side effects caused by administration of a rycal compound for repairing ryanodine receptor channel leaks when treating a disorder in a subject caused by such leaks. These methods are based upon the selection for administration of those rycal compounds having properties including an EC50 value of 102 nM when assayed for its ability to facilitate the rebinding of FKBP12.6 to PKA-phosphorylated RyR2 or less and less than 50% inhibition of the hERG K+ channel (IKr) when administered at 10 ?M to reduce compound toxicity or side effects after administration compared to other rycal compounds not having those properties.
    Type: Application
    Filed: February 14, 2014
    Publication date: July 3, 2014
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Andrew Robert Marks, Donald W. Landry, Shixian Deng
  • Publication number: 20140179676
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: ABBVIE INC.
    Inventors: Kevin P. Cusack, Thomas D. Gordon, Michael Z. Hoemann, David C. Ihle, Bin Li, Gloria Y. Lo Schiavo, Gagandeep K. Somal, Michael Friedman, Martin E. Hayes, Wouter Iwema Bakker
  • Patent number: 8759337
    Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Theodros Asberom, Xianhai Huang, Zhaoning Zhu, John W. Clader, Dmitri A. Pissarnitski, Hubert B. Josien, Hongmei Li
  • Publication number: 20140170111
    Abstract: The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A?, B, G, R1, U, V, W, W?, X, X?, Y and Y? are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: September 28, 2011
    Publication date: June 19, 2014
    Applicant: Merck Sharp & Dohmn Corp.
    Inventors: Craig A. Coburn, Brian J. Lavey, Michael P. Dwyer, Joseph A. Kozlowski, Stuart B. Rosenblum
  • Publication number: 20140163009
    Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.
    Type: Application
    Filed: January 23, 2012
    Publication date: June 12, 2014
    Applicant: CHDI Foundation
    Inventors: Christopher A Luckhurst, Alen F Haughan, Perla Breccia, Andrew J Stott, Roland W Burli, Samantha J Hughes, Ignacio Munoz-Sanjuan, Celia Dominguez
  • Publication number: 20140155375
    Abstract: The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase enzymes.
    Type: Application
    Filed: June 8, 2012
    Publication date: June 5, 2014
    Applicant: GlaxoSmithKline Interllectual Property Limited
    Inventors: Deborah W. Chen, Sarah Duncan, Nigel Paul King, Kiew Ching Lee, Sing Yeung Mak, Dean Andrew Rivers
  • Publication number: 20140155381
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: June 5, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Publication number: 20140135313
    Abstract: Provided are novel compound that is useful as a treatment agent or a prophylactic agent for cardiac failure, cardiac failure due to dystelectasis, left ventricular diastolic impairment, angina or cardiac infarct, hypertension, ischemic cardiac disease, and myocardial relaxation impairment recognized in cardiac failure, atrial fibrillation or ventricular arrhythmia, and a pharmaceutical composition containing the same. The invention pertains to a 1,4-benzothiazepine-1-oxide derivative represented by general formula [I] (In the formula, R represents a hydrogen atom or a hydroxyl group.) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same [I].
    Type: Application
    Filed: December 24, 2013
    Publication date: May 15, 2014
    Inventor: Noburo KANEKO
  • Publication number: 20140128349
    Abstract: Methods and compositions useful for the treatment and/or prevention of muscle weakness in cancer patients. In certain embodiments, the methods of the present invention include administering to a cancer patient a therapeutically or prophylactically effective amount of one or more inhibitors of TGFbeta signaling in combination with one or more benzothiazepine derivatives.
    Type: Application
    Filed: March 15, 2013
    Publication date: May 8, 2014
    Applicants: Indiana University School of Medicine, The Trustees of Columbia University in the City of New York
    Inventors: The Trustees of Columbia University in the City of New York, Indiana University School of Medicine
  • Patent number: 8710045
    Abstract: The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: April 29, 2014
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Andrew Robert Marks, Donald W. Landry, Shixian Deng
  • Publication number: 20140107100
    Abstract: The invention is directed 10 Compound's of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: November 23, 2011
    Publication date: April 17, 2014
    Applicant: EXELIXIS, INC.
    Inventors: Kenneth Rice, Paul Foster
  • Publication number: 20140088171
    Abstract: The present invention relates to 1,4-benzothiazepine derivatives and their use to treat conditions, disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel functioning in cells. The invention also discloses pharmaceutical compositions comprising the compounds and uses thereof to treat diseases and conditions associated with RyRs, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders.
    Type: Application
    Filed: November 11, 2013
    Publication date: March 27, 2014
    Applicants: ARMGO PHARMA, INC., LES LABORATOIRES SERVIER
    Inventors: JIAMING YAN, SANDRO BELVEDERE, YAEL WEBB, MARK BERTRAND, NICOLE VILLENEUVE
  • Publication number: 20140080810
    Abstract: The invention is directed to Compounds of Formula I: (I) and pharmaceutically acceptable salts or solvates thereof, as well as methods of treating using the compounds, methods for screening for inhibitor compounds and methods for identifying treatment regimens.
    Type: Application
    Filed: November 15, 2011
    Publication date: March 20, 2014
    Applicant: Exelixis, Inc.
    Inventors: Kenneth D. Rice, David Markby
  • Publication number: 20140080788
    Abstract: Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R3, R4, R4a, R5a, R5b, R5c, R5d, R5e, R6a, R6b, and R6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
    Type: Application
    Filed: April 27, 2012
    Publication date: March 20, 2014
    Inventors: Jeffrey A. Robl, Jun Li, Lawrence J. Kennedy, Steven J. Walker, Haixia Wang, William N. Washburn, Saleem Ahmad, Khehyong Ngu
  • Patent number: 8673894
    Abstract: This invention relates to compounds of the formula wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: March 18, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Banner, Wolfgang Guba, Hans Hilpert, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Rogers-Evans, Didier Rombach, Thomas Woltering, Wolfgang Wostl
  • Publication number: 20140073629
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: September 3, 2013
    Publication date: March 13, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Jehrod Burnett BRENNEMAN, John GINN, Michael D. LOWE, Christopher Ronald SARKO, Edward S. TASBER, Zhonghua ZHANG
  • Publication number: 20140073628
    Abstract: The invention is directed to inhibitors of mTOR and pharmaceutically acceptable salts or solvates thereof, as well as methods of using them. The inhibitors are generally of structural formula I and pharmaceutically acceptable salts thereof, wherein the variables are as defined herein.
    Type: Application
    Filed: November 23, 2011
    Publication date: March 13, 2014
    Inventor: Kenneth D. Rice
  • Publication number: 20140066431
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of treating using the compounds, methods for screening for inhibitor compounds and methods for identifying treatment regimens.
    Type: Application
    Filed: November 15, 2011
    Publication date: March 6, 2014
    Applicant: Exelixis, Inc.
    Inventors: Kenneth D. Rice, David Markby
  • Publication number: 20140051679
    Abstract: The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
    Type: Application
    Filed: October 12, 2012
    Publication date: February 20, 2014
    Applicant: UNIVERISTY HEALTH NETWORKS
    Inventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter B. Sampson, Miklos Feher, Donald E. Awrey
  • Publication number: 20140045822
    Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.
    Type: Application
    Filed: July 3, 2013
    Publication date: February 13, 2014
    Applicant: UNIVERSITY HEALTH NETWORK
    Inventors: Peter Brent Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
  • Publication number: 20140045820
    Abstract: This invention relates to compounds of the formula wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.
    Type: Application
    Filed: October 22, 2013
    Publication date: February 13, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: David Banner, Wolfgang Guba, Hans Hilpert, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Rogers-Evans, Didier Rombach, Thomas Woltering, Wolfgang Wostl
  • Patent number: 8648066
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: February 11, 2014
    Assignee: Exelixis, Inc.
    Inventors: Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Chris Allen Buhr, Joerg Bussenius, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Jason R. Harris, Eileen E. Jackson-Ugueto, Anagha Joshi, Angie Inyoung Kim, Amy Lew Tsuhako, Sunghoon Ma, Jean-Claire Limun Manalo, Stephanie Ng, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang, Cristiana A. Zaharia
  • Patent number: 8642586
    Abstract: Provided are novel compound that is useful as a treatment agent or a prophylactic agent for cardiac failure, cardiac failure due to dystelectasis, left ventricular diastolic impairment, angina or cardiac infarct, hypertension, ischemic cardiac disease, and myocardial relaxation impairment recognized in cardiac failure, atrial fibrillation or ventricular arrhythmia, and a pharmaceutical composition containing the same. The invention pertains to a 1,4-benzothiazepine-1-oxide derivative represented by general formula [I] (In the formula, R represents a hydrogen atom or a hydroxyl group.) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same [I].
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: February 4, 2014
    Inventors: Noboru Kaneko, Mitsuru Takahashi
  • Patent number: 8637493
    Abstract: Described are methods for treating cancers, e.g., glioblastoma, including administering an inhibitor of Notch signalling, e.g., a gamma secretase inhibitor, in combination with a chemotherapeutic agent.
    Type: Grant
    Filed: November 10, 2010
    Date of Patent: January 28, 2014
    Assignee: University of Massachusetts
    Inventors: Alonzo H. Ross, Candace Gilbert, Richard Moser
  • Patent number: 8637499
    Abstract: The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides methods of making the compound methods of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: May 25, 2010
    Date of Patent: January 28, 2014
    Assignee: Exelixis, Inc.
    Inventors: Naing Aay, Arlyn Arcalas, Joerg Bussenius, Steven Charles DeFina, Larisa Dubenko, Jason R. Harris, Eileen E. Jackson-Ugueto, Angie Inyoung Kim, Jean-Claire Limun Manalo, Michael Pack, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang, Owen Joseph Bowles, Jeffry Kimo Curtis
  • Publication number: 20140024637
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: November 23, 2011
    Publication date: January 23, 2014
    Applicant: Exelixis, Inc.
    Inventor: Kenneth D. Rice
  • Publication number: 20140018347
    Abstract: The invention is directed to inhibitors of mTOR and pharmaceutically acceptable salts or solvates thereof, as well as methods of using them. The inhibitors are generally of structural Formula (I) wherein the variables are as defined herein.
    Type: Application
    Filed: November 23, 2011
    Publication date: January 16, 2014
    Applicant: Exelixis, Inc.
    Inventor: Kenneth Rice
  • Patent number: 8623861
    Abstract: The present invention relates to a method of treating demyelination diseases, such as multiple sclerosis, comprising administration of an atypical antipsychotic drug, such as quetiapine or an analog thereof, to a subject in need thereof.
    Type: Grant
    Filed: November 5, 2007
    Date of Patent: January 7, 2014
    Inventor: Xin-Min Li
  • Publication number: 20140005172
    Abstract: The invention is directed to inhibitors of PI3K and mTOR and pharmaceutically acceptable salts or solvates thereof as well as methods of using them, wherein the inhibitors are of structural Formula I and pharmaceutically acceptable salts thereof wherein the variables are as defined herein.
    Type: Application
    Filed: November 23, 2011
    Publication date: January 2, 2014
    Applicant: ELELIXIS, INC.
    Inventor: Kenneth D. Rice
  • Publication number: 20130338093
    Abstract: Provided herein are methods of treating or ameliorating a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a pediatric liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 19, 2013
    Publication date: December 19, 2013
    Applicant: Lumena Pharmaceuticals, Inc.
    Inventor: Lumena Pharmaceuticals, Inc.
  • Publication number: 20130338142
    Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or disorder are provided.
    Type: Application
    Filed: June 14, 2013
    Publication date: December 19, 2013
    Inventors: Peter A. BLOMGREN, Kevin S. CURRIE, Randall HALCOMB, Jeffrey E. KROPF, Seung H. LEE, Jiayao LI, Jennifer R. LO, Scott A. MITCHELL, Aaron SCHMITT, Qiaoyin WU, Jin-Min XIONG, Jianjun XU, Zhongdong ZHAO, Jayaraman CHANDRASEKHAR, Eric LANSDON
  • Patent number: 8604018
    Abstract: The invention provides ?-helix mimetic structures and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of diseases including fibrosis, such as pulmonary fibrosis.
    Type: Grant
    Filed: March 28, 2011
    Date of Patent: December 10, 2013
    Assignee: Institute for Chemical Genomics
    Inventors: Michael Kahn, Masakatsu Eguchi