Isoquinolines (including Hydrogenated) Patents (Class 546/139)
  • Patent number: 10273241
    Abstract: Provided herein are compounds of Formula (A), (B), (C), (D) and (E), pharmaceutically acceptable salts, quaternary amine salts, and N-oxides thereof, and pharmaceutical compositions thereof. Compounds of Formula (A), (B), (C), (D), and (E) are contemplated useful as therapeutics for treating a wide variety of conditions, e.g., including but not limited to, conditions associated with angiogenesis and with CDK8 and/or CDK19 kinase activity. Further provided are methods of inhibiting CDK8 and/or CDK19 kinase activity, methods of modulating the -catenin pathway, methods of modulating STAT1 activity, methods of modulating the TGF?/BMP pathway, methods of modulating HIF-1-alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using a compound of Formula (A), (B), (C), (D), or (E). Further provided are CDK8 and CDK19 point mutants and methods of use thereof.
    Type: Grant
    Filed: May 16, 2018
    Date of Patent: April 30, 2019
    Assignee: President and Fellows of Harvard College
    Inventors: Matthew D. Shair, Juergen Ramharter, Henry Efrem Pelish, Brian Bor-Jen Liau, Jae Young Ahn
  • Patent number: 10166249
    Abstract: Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Grant
    Filed: July 12, 2017
    Date of Patent: January 1, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, T. G. Murali Dhar, Hai-Yun Xiao, John L. Gilmore, Michael G. Yang, Zili Xiao, David Marcoux
  • Patent number: 9956214
    Abstract: The present disclosure is generally directed to compositions and methods for treating apicomplexan protozoan related disease, such as toxoplasmosis and cryptosporidiosis.
    Type: Grant
    Filed: November 15, 2016
    Date of Patent: May 1, 2018
    Assignee: University of Washington Through its Center for Commercialization
    Inventors: Erkang Fan, Wesley C. Van Voorhis, Zhongsheng Zhang, Wenlin Huang, Kayode K. Ojo
  • Patent number: 9931327
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and the treatment of certain conditions such as COPD.
    Type: Grant
    Filed: September 24, 2015
    Date of Patent: April 3, 2018
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Elisabetta Armani, Gabriele Amari, Laura Carzaniga, Carmelida Capaldi, Oriana Esposito, Gino Villetti, Renato De Fanti
  • Patent number: 9770459
    Abstract: Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Grant
    Filed: October 28, 2016
    Date of Patent: September 26, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, T.G. Murali Dhar, Hai-Yun Xiao, John L. Gilmore, Michael G. Yang, Zili Xiao, David Marcoux
  • Patent number: 9688689
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds, and methods of using such compounds for treatment of joint damage or joint injury in a mammal, and for inducing differentiation of mesenchymal stem cells into chondrocytes.
    Type: Grant
    Filed: May 12, 2015
    Date of Patent: June 27, 2017
    Assignee: Novartis AG
    Inventors: Ha-Soon Choi, James Paul Lajiness, Srinivasa Reddy Natala, Bao Nguyen, Hank Michael James Petrassi, Zhicheng Wang
  • Patent number: 9040512
    Abstract: The present invention relates, inter alia, to metal complexes having improved solubility, to processes for the preparaion of the metal complexes, to devices comprising these metal complexes and to the use of the metal complexes.
    Type: Grant
    Filed: September 1, 2011
    Date of Patent: May 26, 2015
    Assignee: Merck Patent GmbH
    Inventors: Rémi Manouk Anémian, Burkhard Koenig, Claire de Nonancourt
  • Patent number: 9034899
    Abstract: Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: May 19, 2015
    Assignee: Albany Molecular Research, Inc.
    Inventors: Shuang Liu, Bruce F. Molino, Kassoum Nacro
  • Patent number: 9035059
    Abstract: There are provided compounds represented by the following general formula (I) or pharmaceutically acceptable salts of thereof, which have a superior monoacylglycerol acyltransferase 2 inhibitory action: wherein Ring A represents a partially saturated heteroaryl group, an aryl group or a heteroaryl group, RB represents a C4-18 alkyl group, a C3-8 cycloalkyl group, a partially saturated aryl group, an aryl group, or the following formula (II): wherein V represents the formula —CR11R12—, —CO—, —CO—O—, or —CO—NH—, W represents a single bond or a C1-3 alkylene group, and Ring B represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a partially saturated heteroaryl group, a saturated heterocyclyl group, an aryl group, or a heteroaryl group, Y represents a nitrogen atom or the formula N+(RF), RF represents a C1-4 alkyl group, and m and n, which may be the same or different, each represent an integer of 0 or 1.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: May 19, 2015
    Assignee: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Tsuyoshi Busujima, Takahiro Oi, Hiroaki Tanaka, Yoshihisa Shirasaki, Kanako Iwakiri, Nagaaki Sato, Shigeru Tokita
  • Patent number: 9029531
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: May 12, 2015
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
  • Publication number: 20150126548
    Abstract: There is provided compounds for treating bone loss diseases and for preventing bone loss. Specifically the present invention relates to compounds, preferable isoquinolene derivatives.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Inventors: Abbas Jafari, Li Chen, Moustapha Kassem, Basem Abdallah
  • Patent number: 9024027
    Abstract: Compounds, pyridine N-oxides, and pharmaceutically acceptable salts of formula (I) are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and for preventing and/or treating diseases of the respiratory tract characterized by airway obstruction, such as asthma or COPD.
    Type: Grant
    Filed: October 19, 2012
    Date of Patent: May 5, 2015
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Elisabetta Armani, Gabriele Amari, Carmelida Capaldi, Laura Carzaniga, Elena La Porta, Matilde Guala
  • Patent number: 9012632
    Abstract: Provided is a method whereby a heteroaromatic ring aryl can be very rapidly methylated at a high yield. In an N-alkyl-2-pyrrolidinone, a heteroaromatic ring aryltrialkylstannan is cross-coupled with methyl iodide in the presence of a palladium complex, a phosphine ligand, a cuprous halide, a carbonic acid salt and/or an alkali metal fluoride to thereby rapidly methylate the heteroaromatic ring aryl. (Formula shows a case wherein the heteroaromatic ring aryl is a pyridyl group.
    Type: Grant
    Filed: December 25, 2009
    Date of Patent: April 21, 2015
    Assignee: Riken
    Inventors: Masaaki Suzuki, Hisashi Doi, Hiroko Koyama
  • Patent number: 9006442
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: April 14, 2015
    Assignee: Lupin Limited
    Inventors: Sanjeev Anant Kulkarni, Sachin Madan, Nirmal Kumar Jana, Prashant Vitthalrao Tale, Narasimha Murthy Cheemala, Sachin Jaysing Mahangare, Prashant Popatrao Vidhate, Chaitanya Prabhakar Kulkarni, Sapana Suresh Patel, Amolsing Dattu Patil, Seema Prabhakar Zade, Rohan Mahadev Shinde, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150083223
    Abstract: A fullerene derivative represented by the following formula (1): wherein “FLN” represents a fullerene core, R1 represents an optionally substituted C1-C24 alkyl group or an optionally substituted C7-C24 aralkyl group, R2 and R3 independently represent a hydrogen atom or an optionally substituted C1-C24 hydrocarbon group but excluding a case where both of R2 and R3 are hydrogen atoms, and R2 and R3 may combine together to form a ring.
    Type: Application
    Filed: September 25, 2013
    Publication date: March 26, 2015
    Applicants: Tohoku University, Showa Denko K.K.
    Inventors: Tienan JIN, Weili Si, Yoshinori Yamamoto, Takeshi Igarashi
  • Patent number: 8912186
    Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: December 16, 2014
    Assignee: Universitaet des Saarlandes
    Inventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
  • Patent number: 8883792
    Abstract: The present invention provides a novel isoquinoline-6-sulfonamide derivative that is useful as a medicine. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt, wherein R1 and R2 each independently represent a hydrogen atom, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like; R5 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted cycloalkyl group, an optionally substituted alkanoyl group, or the like; and A represents a linear or branched alkylene group having 2 to 6 carbon atoms.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: November 11, 2014
    Assignee: D. Western Therapeutics Institute, Inc.
    Inventors: Hiroyoshi Hidaka, Kengo Sumi, Kouichi Takahashi, Yoshihiro Inoue
  • Patent number: 8877741
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Patent number: 8865709
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: October 21, 2014
    Assignee: Neosome Life Sciences, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Patent number: 8859814
    Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: October 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Derek Cogan, Alexander Heim-Riether, Wang Mao, Craig Andrew Miller, Philip Dean Ramsden, Lana Louise Smith Keenan, Roger John Snow, Jiang-Ping Wu, Yu Yang
  • Publication number: 20140288309
    Abstract: This invention relates to a process of producing compounds, which are useful as bleach boosters, as well as to the compounds, which are obtainable using said process, and to their use.
    Type: Application
    Filed: June 9, 2014
    Publication date: September 25, 2014
    Applicant: BASF SE
    Inventors: Karin Schein, Arno Kochner, Ludwig Völkel, Christian Bittner, Ingo Münster, Frank Dietsche, Wolfgang Schrof, Hansgeorg Ernst, Karl Beck, Andrea Misske, Martin Scholtissek
  • Patent number: 8815898
    Abstract: The present invention relates compounds of general formula (I) and stereoisomers and pharmaceutically acceptable salts and prodrugs thereof; wherein R? and R1-R5 are as defined in the claims. The invention also relates to said compounds for use as a medicament and particularly in the treatment of drug addiction and CNS related diseases.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: August 26, 2014
    Assignee: Montisera Ltd
    Inventors: Ville Takio, Matti Ekholm
  • Publication number: 20140221655
    Abstract: The invention provides methods for substituting polyaromatic hydrocarbons or polyheterocyclic compounds with perfluoroalkyl groups. The methods can include heating a polyaromatic hydrocarbon substrate or a polyheterocyclic compound substrate in the presence of a perfluoroalkyl iodide, typically in a closed system, wherein the heating is sufficient to bring both the polyaromatic hydrocarbons or polyheterocyclic compound, and the perfluoroalkyl iodide, into the gas phase, thereby allowing the substrate to react with the perfluoroalkyl iodide in the gas phase to form polyaromatic hydrocarbons or polyheterocyclic compounds having one or more perfluoroalkyl substituents. The methods allow for the creation of versatile libraries of novel perfluoroalkyl-containing derivatives that can serve as important building blocks and active components in biomedical, electronic, and materials applications.
    Type: Application
    Filed: February 6, 2014
    Publication date: August 7, 2014
    Applicant: Colorado State University Research Foundation
    Inventors: Steven S. Strauss, Olga V. Boltalina, Igor V. Kuvychko
  • Patent number: 8779144
    Abstract: Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
    Type: Grant
    Filed: March 16, 2007
    Date of Patent: July 15, 2014
    Assignee: Evotec (US) Inc.
    Inventors: Michael G. Kelly, John Kincaid, Yeyu Cao, Carl Kaub, Sumithra Gowlugari, Jianhua He
  • Patent number: 8772492
    Abstract: The invention relates to 6-substituted isoquinoline and isoquinoline derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
    Type: Grant
    Filed: June 18, 2009
    Date of Patent: July 8, 2014
    Assignee: Sanofi
    Inventors: Oliver Plettenburg, Katrin Lorenz, Jochen Goerlitzer, Matthias Lohn
  • Publication number: 20140171455
    Abstract: Methods for deterring microglia-mediated neurotoxicity in a human or non-human animal subjects comprising the step of inhibiting or blocking the intermediate-conductance calcium-activated potassium channel Kv1.3 in microglia, such as in subjects how suffer from neurodegenerative diseases (e.g., Alzheimer's Disease) or ischemic/anoxic/hypoxic conditions. The inhibition or blocking of the KCa1.3 channels may be accomplished by administering a substance that inhibits Kv1.3 in microglia. Examples of Kv1.3 inhibiting substances include certain 5-phenoxyalkoxypsoralens, such as (4-Phenoxybutoxy)psoralen (PAP-1) as well as certain 4-phenoxybutoxy-substituted heterocyclic compounds.
    Type: Application
    Filed: June 8, 2012
    Publication date: June 19, 2014
    Applicant: The Regents of the University of California
    Inventors: Heike Wulff, Lee-Way Jin, Izumi Meezawa
  • Patent number: 8748614
    Abstract: The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
    Type: Grant
    Filed: June 18, 2009
    Date of Patent: June 10, 2014
    Assignee: Sanofi
    Inventors: Oliver Plettenburg, Armin Hofmeister, Jochen Goerlitzer, Matthias Löhn
  • Patent number: 8741924
    Abstract: Small molecule compounds are provided for treating lupus as are methods of treating lupus using these compounds.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: June 3, 2014
    Assignee: The Feinstein Institute for Medical Research
    Inventors: Yousef Al-Abed, Betty A. Diamond
  • Patent number: 8741901
    Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle opt
    Type: Grant
    Filed: July 2, 2012
    Date of Patent: June 3, 2014
    Assignees: Albany Molecular Research, Inc., Bristol-Myers Squibb Company
    Inventors: Bruce F. Molino, Shuang Liu, Peter R. Guzzo, James P. Beck
  • Patent number: 8722671
    Abstract: The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: May 13, 2014
    Assignee: Sanofi
    Inventors: Oliver Plettenburg, Armin Hofmeister, Dieter Kadereit, Stefan Peukert, Sven Ruf, Kurt Ritter, Matthias Loehn, Yuri Ivashchenko, Peter Monecke, Matthias Dreyer, Aimo Kannt
  • Patent number: 8716527
    Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2- substituted-p-quinone derivatives as disclosed herein.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: May 6, 2014
    Assignee: Edison Pharmaceuticals, Inc.
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell
  • Patent number: 8710077
    Abstract: The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
    Type: Grant
    Filed: June 18, 2009
    Date of Patent: April 29, 2014
    Assignee: Sanofi
    Inventors: Oliver Plettenburg, Katrin Lorenz, Jochen Goerlitzer, Matthias Löhn, Sandrine Biscarrat, Fréderic Jeannot, Olivier Duclos
  • Patent number: 8710076
    Abstract: 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: Grant
    Filed: October 15, 2009
    Date of Patent: April 29, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, Anthony J. Roecker, John D. Schreier
  • Patent number: 8710228
    Abstract: The invention relates to 6-substituted isoquinoline derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
    Type: Grant
    Filed: June 18, 2009
    Date of Patent: April 29, 2014
    Assignee: Sanofi
    Inventors: Oliver Plettenburg, Armin Hofmeister, Dieter Kadereit, Stefan Peukert, Sven Ruf, Matthias Löhn, Peter Monecke, Alexander Schiffer, Aimo Kannt, Markus Kohlmann
  • Publication number: 20140107073
    Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
    Type: Application
    Filed: October 4, 2013
    Publication date: April 17, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
  • Patent number: 8664243
    Abstract: (S)-1-(4-Chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine monohydrochloride and a crystal thereof, and a crystal of the aforementioned monohydrochloride having a major peak or peaks at one or more positions selected from the group consisting of positions where 2?s are about 13.9°, 21.5°, 21.7°, 22.4°, 22.8°, 24.5° and 35.0° in a powder X-ray diffraction spectrum, which have excellent properties as active ingredient of a medicament for prophylactic and/or therapeutic treatment of glaucoma and the like.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: March 4, 2014
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Hitoshi Kida, Koki Matsubara, Shunsuke Kaneko
  • Patent number: 8664245
    Abstract: The disclosure relates to fumarate salts of 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, to pharmaceutical compositions thereof, processes for making the same, and methods of use thereof.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: March 4, 2014
    Assignee: Sanofi
    Inventors: Beverly C. Langevin, Robert Allan Farr, Dinubhai H. Shah, Daniel Sherer
  • Patent number: 8658646
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: August 31, 2012
    Date of Patent: February 25, 2014
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Shaoqing Chen, Javier de Vicente Fidalgo, Matthew Michael Hamilton, Johannes Cornelius Hermann, Joshua Kennedy-Smith, Hongju Li, Allen John Lovey, Matthew C. Lucas, Kin-Chun Thomas Luk, Stephen M. Lynch, Counde O'yang, Fernando Padilla, Ryan Craig Schoenfeld, Achyutharao Sidduri, Michael Soth, Ce Wang, Peter Michael Wovkulich, Xiaohu Zhang
  • Publication number: 20140051694
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: NEOSOME LIFE SCIENCES, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • Patent number: 8653100
    Abstract: The present invention relates to tetrahydroisoquinoline of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GlyT1 inhibitors.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: February 18, 2014
    Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: Michael Ochse, Udo Lange, Wilfried Braje, Berthold Behl, Wilfried Hornberger, Mario Mezler, Wilhelm Amberg, Charles W. Hutchins
  • Patent number: 8642766
    Abstract: An in vitro synthesis of (+) cortistatin A from readily available precursors is disclosed, as are the syntheses of related 17-aryl substituted compounds, the 17-aryl substituted compounds themselves and novel compounds useful in their preparation.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: February 4, 2014
    Inventors: Ryan A. Shenvi, Carlos A. Guerrero, Jun Shi, Chuang-Chuang Li, Phil S. Baran
  • Patent number: 8624032
    Abstract: A method for producing libraries of structurally and stereochemically diverse molecules that can be screened for biological or chemical activity. A library of 91 heterocyclic compounds composed of 16 distinct scaffolds was synthesized through a sequence of phosphine-catalyzed ring-forming reactions, Tebbe reactions, Diels-Alder reactions, and, in some cases, hydrolysis to illustrate the methods. Three compounds inhibiting migration of human breast cancer cells are identified from the library.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: January 7, 2014
    Assignees: The Regents of the University of California, The University of Connecticut
    Inventors: Ohyun Kwon, Gabriel Fenteany
  • Patent number: 8623889
    Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O?, and one of X2, X3 and X4 is N or N+—O? and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: January 7, 2014
    Assignee: Genentech, Inc.
    Inventors: Joseph P. Lyssikatos, Lewis J. Gazzard, Emily Hanan, Samuel Kintz, Hans Edward Purkey
  • Patent number: 8618295
    Abstract: Synthetic processes for preparing luminescent iridium complexes and precursors thereof are provided. The method employs water as the reaction solvent to prepare luminescent iridium complexes in two different ways. In the first way, a precursor [Ir2(C11NR8)4I2] (Formula I) is prepared from one of IrCl3, M3IrCl6 (M=Li, Na, K) and [Ir2(C11NR8)4Cl2], and then the precursor [Ir2(C11NR8)4I2] is converted into one of the two luminescent iridium isomeric complexes [Ir(C11NR8)2(C11NR?8)] (Formula II). In the second way, a metal complex IrCl3 or M3IrCl6 (M=Li, Na, K), HC11NR8 and a base are converted selectively into one of the two iridium isomeric complexes [Ir(C11NR8)3] (Formula VIII). Herein, R and R? are defined the same as the specification.
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: December 31, 2013
    Assignee: National Chen Kung University
    Inventors: Kom-Bei Shiu, Wu-Sian Sie
  • Patent number: 8592467
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: November 26, 2013
    Assignee: Abbvie Inc.
    Inventors: Marlon D. Cowart, Minghua Sun, Chen Zhao, Guo Zhu Zheng
  • Patent number: 8592608
    Abstract: Provided herein are bicyclic compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders. Compounds provided herein inhibit uptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations containing the compounds are also provided.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: November 26, 2013
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Liming Shao, Fengjiang Wang, Scott C. Malcolm, Michael C. Hewitt
  • Patent number: 8586570
    Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: November 19, 2013
    Assignee: Massachusetts Institute of Technology
    Inventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
  • Patent number: 8569505
    Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to ?-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: October 29, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Ellen Codd, Scott L. Dax, Michele Jetter, Mark McDonnell, James J. McNally, Mark Youngman
  • Publication number: 20130274269
    Abstract: The present invention provides a novel isoquinoline-6-sulfonamide derivative that is useful as a medicine. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt, wherein R1 and R2 each independently represent a hydrogen atom, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like; R5 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted cycloalkyl group, an optionally substituted alkanoyl group, or the like; and A represents a linear or branched alkylene group having 2 to 6 carbon atoms.
    Type: Application
    Filed: December 21, 2011
    Publication date: October 17, 2013
    Applicant: D. Western Therapeutics Institute, Inc.
    Inventors: Hiroyoshi Hidaka, Kengo Sumi, Kouichi Takahashi, Yoshihiro Inoue