The 1,3-diazole Ring Is Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/274.1)
  • Patent number: 11541052
    Abstract: The invention provides compounds of formula (I): Said compounds being modulators of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Grant
    Filed: September 23, 2020
    Date of Patent: January 3, 2023
    Assignee: Autifony Therapeutics Limited
    Inventors: Giuseppe Alvaro, Agostino Marasco
  • Patent number: 11465987
    Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.
    Type: Grant
    Filed: September 20, 2016
    Date of Patent: October 11, 2022
    Assignees: ONCTERNAL THERAPEUTICS, INC., UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
    Inventors: Wei Li, Min Xiao, James Dalton, Sunjoo Ahn, Duane D Miller, Jin Wang
  • Patent number: 11352340
    Abstract: The present disclosure provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that modulate the activity of phosphoinositide 3-kinases-gamma (PI3K?) and are useful in the treatment of diseases related to the activity of PI3K? including, for example, autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
    Type: Grant
    Filed: March 29, 2019
    Date of Patent: June 7, 2022
    Assignee: Incyte Corporation
    Inventors: Richard B. Sparks, Stacey Shepard, Andrew P. Combs, Andrew W. Buesking, Lixin Shao, Haisheng Wang, Nikoo Falahatpisheh
  • Patent number: 11149017
    Abstract: Disclosed are solid state forms of Apalutamide and salts thereof, processes for preparation thereof and pharmaceutical compositions thereof.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: October 19, 2021
    Assignee: WATSON LABORATORIES INC.
    Inventors: Anantha Rajmohan Muthusamy, Sundara Lakshmi Kanniah, Nitin Dnyaneshwar Arote, Omkar Vilas Bhagwat, Jitendra Kamalakar Sonar, Vitthal Baburao Poundkar, Yogesh Dhananjay Wagh
  • Patent number: 11149007
    Abstract: Provided herein are piperidine dione compounds having the following structure: wherein RN, R1, R2, R3, R4, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
    Type: Grant
    Filed: December 18, 2019
    Date of Patent: October 19, 2021
    Assignee: Celgene Corporation
    Inventors: Massimo Ammirante, Sogole Bahmanyar, Matthew D. Correa, Virginia Heather Sharron Grant, Joshua Hansen, Evan J. Horn, Timothy S. Kercher, Christopher Mayne, Mark A. Nagy, Rama Krishna Narla, Surendra Nayak, Stephen Norris, Patrick Papa, Veronique Plantevin-Krenitsky, John J. Sapienza, Brandon W. Whitefield, Shuichan Xu
  • Patent number: 10835534
    Abstract: The invention provides compounds of formula (I): Said compounds being modulators of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Grant
    Filed: December 23, 2019
    Date of Patent: November 17, 2020
    Assignee: Autifony Therapeutics Limited
    Inventors: Giuseppe Alvaro, Agostino Marasco
  • Patent number: 10273222
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: June 7, 2017
    Date of Patent: April 30, 2019
    Assignee: CELGENE QUANTSCEL RESEARCH, INC.
    Inventors: Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 9975880
    Abstract: Imidazolidine-2,4-dione derivatives of formula (I): These compounds have anti-proliferative activity and are useful for treating pathological states and diseases linked to an abnormal cell proliferation, such as cancer.
    Type: Grant
    Filed: December 31, 2013
    Date of Patent: May 22, 2018
    Assignee: IPSEN PHARMA S.A.S.
    Inventors: Serge Auvin, Christophe Lanco, Oliver Dutruel, Qi Chao, Kaichun Gu
  • Patent number: 9637469
    Abstract: Provided is a pyridine derivative represented by formula (I), a prodrug thereof, a pharmaceutically acceptable salt of the pyridine derivative or the prodrug, or a solvate of the pyridine derivative, the prodrug or the pharmaceutically acceptable salt, which is useful for treatment or prophylaxis of diseases associated with URAT1 such as gout, hyperuricemia, hypertension, kidney diseases such as interstitial nephritis, diabetes, arteriosclerosis and Lesch-Nyhan syndrome.
    Type: Grant
    Filed: November 13, 2013
    Date of Patent: May 2, 2017
    Assignee: Teijin Pharma Limited
    Inventors: Akinobu Maruyama, Hirofumi Kamada, Mika Fujinuma, Susumu Takeuchi, Hiroshi Saitoh, Yoshimasa Takahashi
  • Patent number: 9278977
    Abstract: A process for manufacturing 5-chloromethyl-2,3-pyridine dicarboxylic acid anhydrides (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; comprising the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with a chlorinating agent, optionally in the presence of a radical initiator in a solvent selected from halogenated hydrocarbons, and (ii) crystallizing the compound (I) formed in step (i) from a solvent selected from chlorobenzene, 1,2-dichlorobenzene, 1,3-dichlorobenzene, 1,4-dichlorobenzene, dichloroethane, trichloromethane, dichloromethane, toluene, xylenes, ethyl acetate, methyl tert.-butyl ether, and mixtures thereof. Compounds (I) are useful intermediates in the synthesis of herbicidal imidazolinones.
    Type: Grant
    Filed: March 20, 2014
    Date of Patent: March 8, 2016
    Assignee: BASF SE
    Inventors: Frederik Menges, Joachim Gebhardt, Michael Rack, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schroeder
  • Patent number: 9133166
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: September 15, 2015
    Assignee: QUANTICEL PHARMACEUTICALS, INC.
    Inventors: Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • Publication number: 20150111096
    Abstract: The invention relates to the salts of bicyclic imidazole compounds (IV) having general structural formulae in which A represents a monovalent cation, X represents independently a carbon atom, an oxygen atom, a sulphur atom or a nitrogen atom. The invention also relates to the associated production method and to the use thereof, in particular as an electrolyte component for batteries.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 23, 2015
    Inventor: Grégory Schmidt
  • Publication number: 20150105354
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicants: MERCK SHARP & DOHME CORP., PHARMACOPEIA, LLC
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, JR., John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • Publication number: 20150104870
    Abstract: The present invention provides an agent for promoting neuronal differentiation of neural stem cells, which contains a p38 inhibitor. In addition, the present invention provides a method of promoting neuronal differentiation of neural stem cells, which includes cultivating neural stem cells in the presence of a p38 inhibitor. Neural stem cells are gliogenic or neurogenic. The p38 inhibitor is a nucleic acid which hybridizes to DNA or mRNA encoding p38 under physiological conditions, thereby inhibiting the transcription and/or translation thereof, an expression vector of the nucleic acid, a low molecular p38 inhibitor and the like.
    Type: Application
    Filed: April 26, 2013
    Publication date: April 16, 2015
    Inventors: Hayato Kaneda, Hideyuki Okano, Takuya Shimazaki
  • Publication number: 20150099748
    Abstract: Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).
    Type: Application
    Filed: September 29, 2014
    Publication date: April 9, 2015
    Inventors: Gregory W. Endres, Pil Heui Lee, Kirk Lang Olson, James Bernard Kramer, Fred Lawrence Ciske, Stephen Douglas Barrett
  • Patent number: 8975411
    Abstract: An object of the present invention is to provide a pharmaceutical agent useful for treating and preventing neurological disease, having satisfactory solubility and oxidative stress-mediated cell death suppressive activity as well as capable of exhibiting excellent blood-brain barrier permeability. The present invention is directed to an acylaminoimidazole derivative represented by general formula (I) or a salt thereof, and a pharmaceutical and a therapeutic or preventive agent for neurological disease containing the same, as an active ingredient.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: March 10, 2015
    Assignees: Neugen Pharma Inc., Wakunaga Pharmaceutical Co., Ltd.
    Inventors: Joh-E Ikeda, Noriaki Hirayama, Satoshi Inoue, Kazunori Tanaka, Takuya Kanno
  • Patent number: 8969338
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, Y, R1, R2, R2?, R3, R3? and R8 are described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: March 3, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20150057218
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: November 3, 2014
    Publication date: February 26, 2015
    Inventors: Min ZHONG, Leping LI
  • Publication number: 20150057282
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 26, 2015
    Applicant: SAREUM LIMITED
    Inventors: John Charles READER, John Mark ELLARD, Helen BOFFEY, Susanne TAYLOR, Andrew David CARR, Michael CHERRY, Michelle WILSON, Richard Boakye OWOARE
  • Publication number: 20150051225
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: February 19, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Ishtiyaque Ahmad, Rajagopal Bakthavatchalam, Sivaramakrishna Battula, Henricus Jacobus, Maria Gijsen, Mark Wall
  • Publication number: 20150045394
    Abstract: The present invention relates to novel carboxamide compounds and their use as a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds. The carboxamide compounds are compounds of the general formula I in which W—R2 is selected from and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Application
    Filed: October 23, 2014
    Publication date: February 12, 2015
    Inventors: Andreas Kling, Helmut Mack, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Patent number: 8952018
    Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. cancer.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: February 10, 2015
    Assignee: GlaxosmithKline LLC
    Inventors: Melissa Dumble, Rakesh Kumar, Sylvie Laquerre, Peter Lebowitz
  • Patent number: 8946443
    Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a C1 to C6 alkyl group which may be substituted by one to three groups selected from substituent group A, or the like (substituent group A: a hydroxy group, a halogeno group, a cyano group, a nitro group, an amino group, a carboxy group, a C1 to C3 alkyl group, etc.); R2, R3, and R8 each independently represent a hydrogen atom or a C1 to C3 alkyl group; R4, R5, R6, R7, R9, and R10 each independently represent a hydrogen atom or the like; and R11 represents a hydrogen atom or the like, has TAFIa enzyme inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, or the like.
    Type: Grant
    Filed: March 14, 2011
    Date of Patent: February 3, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Tsutomu Nagata, Jun Kobayashi, Yoshiyuki Onishi, Masamichi Kishida, Kengo Noguchi
  • Patent number: 8937184
    Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CB2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB2 receptors are involved. The compounds have the general formula (I) wherein R1-R4 have the meanings given in the specification.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: January 20, 2015
    Assignee: Abbvie B.V.
    Inventors: Josephus H. M. Lange, Herman H. Van Stuivenberg, Bernard J. Van Vliet
  • Patent number: 8901314
    Abstract: The present invention relates to compounds of Formula (I), wherein X1, X2, X3, X4, R1, R2, R3, and Q are as defined herein, useful as N-type calcium channel blockers.
    Type: Grant
    Filed: August 16, 2013
    Date of Patent: December 2, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Mark Wall, Nalin Subasinghe, Zhihua Sui, Christopher Flores
  • Patent number: 8889874
    Abstract: The present invention provides Chalcone linked Imidazolone compounds of formula A as anti cancer agent against fifty three human cancer cell lines.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: November 18, 2014
    Assignee: Council of Scientific and Industrial Research
    Inventors: Kamal Ahmed, Ramakrishna Gadupudi, Balakishan Gorre, Raju Paidakula, Viswanath Arutla, Balakrishna Moku
  • Publication number: 20140323508
    Abstract: The invention provides compounds of formula (I): Said compounds being modulators of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Application
    Filed: December 6, 2012
    Publication date: October 30, 2014
    Inventors: Giuseppe Alvaro, Agostino Marasco
  • Publication number: 20140323729
    Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Application
    Filed: May 15, 2014
    Publication date: October 30, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • Publication number: 20140315957
    Abstract: The present invention relates to novel substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss, muscle loss, acne and hirsutism.
    Type: Application
    Filed: June 3, 2014
    Publication date: October 23, 2014
    Inventor: Youzhi TONG
  • Publication number: 20140309237
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: June 26, 2014
    Publication date: October 16, 2014
    Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
  • Publication number: 20140309262
    Abstract: Described herein, inter alia, are compounds useful for the prevention or treatment of hyperproliferative diseases or disorders.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 16, 2014
    Inventors: Michael E. Jung, Charles L. Sawyers, Samedy Ouk, Chris Tran, John Wongvipat
  • Publication number: 20140296068
    Abstract: This document discloses molecules having the following formula (Formula One) and processes related thereto.
    Type: Application
    Filed: October 24, 2012
    Publication date: October 2, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Negar Garizi, Tony K. Trullinger, Ricky Hunter, Yu Zhang, Noormohamed M. Niyaz, Daniel Knueppel, Christian T. Lowe, Ann M. Buysse
  • Publication number: 20140275084
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Quanticel Pharmaceuticals, Inc.
    Inventors: Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 8835450
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: September 16, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Melissa Dumble, Tona Gilmer, Rakesh Kumar, Peter F. Lebowitz, Shannon Renae Morris, Sylvie Laquerre
  • Publication number: 20140228386
    Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.
    Type: Application
    Filed: April 27, 2012
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Saumitra Sengupta
  • Patent number: 8796298
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: August 5, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Melissa Dumble, Tona Gilmer, Rakesh Kumar, Peter F. Lebowitz, Shannon Renae Morris, Sylvie Laquerre
  • Publication number: 20140206873
    Abstract: A process for manufacturing 5-chloromethyl-2,3-pyridine dicarboxylic acid anhydrides (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; comprising the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with a chlorinating agent, optionally in the presence of a radical initiator in a solvent selected from halogenated hydrocarbons, and (ii) crystallizing the compound (I) formed in step (i) from a solvent selected from chlorobenzene, 1,2-dichlorobenzene, 1,3-dichlorobenzene, 1,4-dichlorobenzene, dichloroethane, trichloromethane, dichloromethane, toluene, xylenes, ethyl acetate, methyl tert.-butyl ether, and mixtures thereof. Compounds (I) are useful intermediates in the synthesis of herbicidal imidazolinones.
    Type: Application
    Filed: March 20, 2014
    Publication date: July 24, 2014
    Applicant: BASF SE
    Inventors: Frederik MENGES, Joachim GEBHARDT, Michael RACK, Michael KEIL, Rodney F. KLIMA, David CORTES, Robert LEICHT, Helmut ZECH, Jochen SCHROEDER
  • Publication number: 20140194473
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2 and R3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: December 10, 2013
    Publication date: July 10, 2014
    Applicant: E I Du Pont De Nemours And Company
    Inventor: THOMAS FRANCIS PAHUTSKI, JR.
  • Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • Publication number: 20140163075
    Abstract: The invention relates to the field of 26S proteasome inhibition, activation and modulation and to identify compounds which activate 26S proteasome in live cells and a method of treating autoimmune diseases, cancer, inflammation and neurogenerative disorders by inhibition, activation and modulation of the 26S proteasome.
    Type: Application
    Filed: June 1, 2012
    Publication date: June 12, 2014
    Applicant: NETHERLAND CANCER INSTITUTE
    Inventors: Huib Ovaa, Celia R. Berkers, Yves Leestemaker, Karianne Shuurman, Annemieke De Jong
  • Publication number: 20140155602
    Abstract: The present invention relates to ethynyl compounds of formula I-C1 wherein R1, R2, R2?, R3, R3?, R6, U, V and W are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof, which are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: November 20, 2013
    Publication date: June 5, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Patent number: 8742119
    Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: June 3, 2014
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • Patent number: 8729101
    Abstract: The present invention relates to a group of novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CB1 receptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I), wherein R and R1-R4 have the meanings given in the specification.
    Type: Grant
    Filed: September 2, 2008
    Date of Patent: May 20, 2014
    Assignee: Solvay Pharmaceuticals, B.V.
    Inventors: Cornelis G. Kruse, Josephus H. M. Lange, Arnoldus H. J. Herremans, Herman H. Van Stuivenberg
  • Patent number: 8722893
    Abstract: A process for manufacturing 5-chloromethyl-2,3-pyridine dicarboxylic acid anhydrides (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; comprising the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with a chlorinating agent, optionally in the presence of a radical initiator in a solvent selected from halogenated hydrocarbons, and (ii) crystallizing the compound (I) formed in step (i) from a solvent selected from chlorobenzene, 1,2-dichlorobenzene, 1,3-dichlorobenzene, 1,4-dichlorobenzene, dichloroethane, trichloromethane, dichloromethane, toluene, xylenes, ethyl acetate, methyl tert.-butyl ether, and mixtures thereof. Compounds (I) are useful intermediates in the synthesis of herbicidal imidazolinones.
    Type: Grant
    Filed: November 3, 2009
    Date of Patent: May 13, 2014
    Assignee: BASF SE
    Inventors: Frederik Menges, Joachim Gebhardt, Michael Rack, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schroeder
  • Patent number: 8722695
    Abstract: The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy.
    Type: Grant
    Filed: December 6, 2010
    Date of Patent: May 13, 2014
    Assignee: Autifony Therapeutics Limited
    Inventors: Giuseppe Alvaro, Anne Décor, Stefano Fontana, Dieter Hamprecht, Charles Large, Agostino Marasco
  • Patent number: 8703781
    Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophen-}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. cancer.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: April 22, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Melissa Dumble, Rakesh Kumar, Sylvie Laquerre, Peter Lebowitz
  • Patent number: 8697673
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: March 29, 2012
    Date of Patent: April 15, 2014
    Assignee: Pfizer Inc.
    Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Benjamin Adam Fish, Michael Eric Green, Patrick Bradley Mullins, Cory Michael Stiff, Tuan Phong Tran, Thayalan Navaratnam
  • Patent number: 8691816
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: April 8, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20140088152
    Abstract: The present invention provides a composition comprising a pyrazole derivative compound and a pharmaceutically acceptable salt thereof. The composition is remarkably effective for preventing and treating cardiovascular diseases.
    Type: Application
    Filed: February 27, 2012
    Publication date: March 27, 2014
    Applicant: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION
    Inventors: Yun Soo Bae, Kee In Lee, Jee Hyun Lee, Han Joong Jo, Jinoh Kim
  • Publication number: 20140081025
    Abstract: The compound represented by formula (IA) or a pharmaceutically acceptable salt thereof is based on orexin (OX) receptor antagonist activity, is useful in the treatment and prevention of illnesses including sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependency, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, pain, gastrointestinal disease, epilepsy, inflammation, immunological disease, endocrinological related disease, and hypertension.
    Type: Application
    Filed: May 8, 2012
    Publication date: March 20, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Ryo Suzuki, Aya Futamura, Masahito Abe, Shuhei Kashiwa, Nobutaka Hattori, Dai Nozawa, Hiroshi Ohta, Yuko Araki