Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/312)
  • Patent number: 9701639
    Abstract: The present disclosure relates to co-crystals comprising N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and a co-former and methods for their preparation. The present disclosure further relates to pharmaceutical compositions comprising the co-crystal forms, as well as methods of treatment therewith and kits.
    Type: Grant
    Filed: October 7, 2015
    Date of Patent: July 11, 2017
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Mark Strohmeier, John Caesar, Jr., Patrick Raymond Connelly, Majed Fawaz, Eduard Luss-Lusis, Brian McClain, Ales Medek, Hai Miao, Kwame Wiredu Nti-Addae, Ping Yin, Yuegang Zhang
  • Patent number: 9694004
    Abstract: A novel crystalline form of a compound is disclosed.
    Type: Grant
    Filed: September 1, 2016
    Date of Patent: July 4, 2017
    Assignee: Glaxo Group Limited
    Inventor: Mei-yin Lee
  • Patent number: 9687490
    Abstract: A compound of formula (I) for use in the treatment of a condition or disorder associated with nicotinamide adenine dinucleotide phosphate oxidase.
    Type: Grant
    Filed: October 22, 2013
    Date of Patent: June 27, 2017
    Assignee: GLUCOX BIOTECH AB
    Inventors: Mona Wilcke, Erik Walum, Per Wikstrom
  • Patent number: 9682967
    Abstract: The present invention is directed to N-substituted-5-substituted phthalamic acids which of formula (A). The compounds are considered useful for the treatment of diseases treatment of a neurodegenerative disease, psychiatric disease, motorneuron disease, peripheral neuropathies, pain, neuroinflammation or atherosclerosis such as Alzheimer's disease and Parkinson's disease.
    Type: Grant
    Filed: January 27, 2014
    Date of Patent: June 20, 2017
    Assignee: H. Lundbeck A/S
    Inventors: Philip James Maltas, Stephen Watson, Morten Langg{hacek over (a)}rd, Laurent David
  • Patent number: 9675606
    Abstract: The invention relates to the compounds of general formula (I): Preparation process and therapeutic use.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: June 13, 2017
    Assignee: SANOFI
    Inventors: Alain Braun, Olivier Duclos, Gilbert Lassalle, Franz Lorge, Valerie Martin, Olaf Ritzeler, Aurelie Strub
  • Patent number: 9676724
    Abstract: Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2, R3 and R4 are each as defined in the present application.
    Type: Grant
    Filed: October 12, 2015
    Date of Patent: June 13, 2017
    Assignee: Tianjin Hemay Oncology Pharmaceutical Co., Ltd.
    Inventors: Hesheng Zhang, Yingwei Chen, Qingchao He
  • Patent number: 9676765
    Abstract: A compound of the formula: (I) or a pharmaceutically acceptable salt thereof, wherein: L is a 5-membered nitrogen-containing heteroaryl which is optionally fused to a benzene; Y is a 5, 6 or 7-membered nitrogen-containing heteroaryl, which is optionally fused to a benzene; and W is a zinc-binding group. The compounds are HDAC inhibitors and therefore have potential utility in therapy.
    Type: Grant
    Filed: November 6, 2013
    Date of Patent: June 13, 2017
    Assignee: Karus Therapeutics Limited
    Inventors: Stephen J. Shuttleworth, Cyrille D. Tomassi, Alexander R. Cecil, Somhairle Maccormick, William J. Nodes, Franck A. Silva
  • Patent number: 9662327
    Abstract: Provided are compounds of formula (I), wherein X, Y, Z, W, V, R2, R3 and m are defined as in the description. Their pharmaceutical compositions and their uses for treating cancers are also provided.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: May 30, 2017
    Assignee: AGIOS PHARMACEUTICALS, INC
    Inventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
  • Patent number: 9662322
    Abstract: This invention provides a method for treating or for reducing ambulatory deterioration in a human patient diagnosed to be afflicted with relapsing-remitting multiple sclerosis (RRMS) and having a high baseline disability score according to the Kurtzke Expanded Disability Status Scale (EDSS), comprising periodically administering to only the patient diagnosed with RRMS and having a high baseline disability score an amount of laquinimod effective to treat the patient or to reduce ambulatory deterioration. This invention further provides pharmaceutical compositions and packages comprising an effective amount of laquinimod for treating a human patient diagnosed to be afflicted with RRMS and having a high baseline disability score according to the EDSS.
    Type: Grant
    Filed: November 19, 2015
    Date of Patent: May 30, 2017
    Assignee: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventor: Volker Knappertz
  • Patent number: 9636375
    Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Grant
    Filed: November 9, 2015
    Date of Patent: May 2, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alan Xiangdong Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
  • Patent number: 9624235
    Abstract: A method for treating a neoplasm in a subject, comprising co-administering to the subject a therapeutically effective amount of an anticancer agent and a substituted 6,7-methylenedioxy-4-amino-quinoline, or a pharmaceutically acceptable salt or ester thereof.
    Type: Grant
    Filed: January 29, 2013
    Date of Patent: April 18, 2017
    Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
    Inventors: Barry I. Gold, Xiangqun Xie, Ajay Srinivasan, LiRong Wang
  • Patent number: 9617217
    Abstract: The present application provides novel compounds having anti-cancer or anti-Helicobacter pylori activity, pharmaceutical compositions and method for producing and using the novel compound.
    Type: Grant
    Filed: February 24, 2014
    Date of Patent: April 11, 2017
    Assignee: MICROBIAL CHEMISTRY RESEARCH FOUNDATION
    Inventors: Manabu Kawada, Hikaru Abe, Takumi Watanabe, Hiroyuki Inoue, Shun-ichi Ohba, Chigusa Hayashi, Masayuki Igarashi
  • Patent number: 9603804
    Abstract: [Problem] To provide a solid pharmaceutical composition which contains a compound represented by general formula (1) or a salt thereof and suppresses decomposition of said compound or salt thereof, and a production method of said solid pharmaceutical composition. [Solution] This solid pharmaceutical composition contains a compound represented by general formula (1) or a salt thereof, a cellulosic excipient, and an acidic substance of pH 4.0 or less.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: March 28, 2017
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi Uchida, Masataka Hanada
  • Patent number: 9592186
    Abstract: Embodiments of the invention are generally directed to compositions useful for reducing pigmentation in the skin. The composition may further include other depigmenting agents such as nicotinamide and its melanasome transfer-inhibiting derivatives, 3,3?-thiodipropanoic acid and its tyrosinase-inhibiting derivatives, or resorcinol and its tyrosinase-inhibiting derivatives, in a topically acceptable vehicle.
    Type: Grant
    Filed: September 30, 2014
    Date of Patent: March 14, 2017
    Assignee: Avon Products, Inc.
    Inventors: Hong Hu, Sunghan Yim, Uma Santhanam, John W. Lyga
  • Patent number: 9585878
    Abstract: This application provides for a method of increasing brain-derived neurotrophic factor (BDNF) serum level in a human subject comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to increase BDNF serum level in the human subject. The method can further comprise periodically administering to the subject an amount of a second BDNF-increasing agent. This application also provides for a method for treating a human subject suffering from a BDNF-related disease comprising periodically administering laquinimod or a pharmaceutically acceptable salt thereof in an amount effective to treat the human subject. This application additionally provides for use of laquinimod in the manufacture of a medicament for increasing BDNF serum level in a human subject. This application further provides for a pharmaceutical composition comprising an amount of laquinimod effective for use in increasing BDNF serum level in a human subject.
    Type: Grant
    Filed: August 9, 2010
    Date of Patent: March 7, 2017
    Assignee: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventor: Liat Hayardeny
  • Patent number: 9580409
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., ?-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: November 7, 2012
    Date of Patent: February 28, 2017
    Assignee: SUNOVION PHARMACEUTICALS, INC.
    Inventors: Scott Malcolm, Carrie Bowen, Laurence Melnick, Linghong Xie
  • Patent number: 9540389
    Abstract: Novel compounds are disclosed having the structure of Formula I: wherein, n is an integer from 1 to 5; X is —CN, —F, —Cl, —Br, —I, —NO2; W is S, SO, SO2, O, NH, or NR5; R5 is alkyl, aralkyl, alkenyl, or alkynyl; Y is O, S; Z is NR1R2 or heterocycloalkyl; R1, R2 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups; R3 and R4 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups, and may together form a cyclic structure; and Ar is mono-, di-, or tri-substituted phenyl or heteroaryl, a pharmaceutically acceptable salts thereof. The compounds are potent bacterial efflux pump inhibitors (EPIs).
    Type: Grant
    Filed: May 3, 2014
    Date of Patent: January 10, 2017
    Assignee: Microbiotix, Inc.
    Inventors: Timothy J. Opperman, Son T. Nguyen, Steven M. Kwasny, Xiaoyuan Ding
  • Patent number: 9499552
    Abstract: The present invention relates to a pyrazolo[1,5-a]pyrimidine derivative of general formula 1 and a pharmaceutically acceptable salt thereof. The present invention also relates to use of compounds of formula 1 in the preparation of an anti-tumor medicament.
    Type: Grant
    Filed: May 22, 2015
    Date of Patent: November 22, 2016
    Assignees: Yanti University, Wuhan University
    Inventors: Hongbo Wang, Xuechuan Hong, Xi Zhu, Mingmin Ding, Guangyao Lv, Jianqiao Zhang, Meng Wen, Chunrong Qu, Jinmei Zhu, Xianming Hu
  • Patent number: 9475772
    Abstract: The invention relates to new and improved processes for the preparation of Indacaterol and pharmaceutically acceptable salts thereof as well as intermediates for the preparation of Indacaterol. The new process avoids the use of the epoxide compound known in the art and the impurities associated therewith and results in a higher yield.
    Type: Grant
    Filed: September 9, 2013
    Date of Patent: October 25, 2016
    Assignee: Crystal Pharma S.A.U.
    Inventors: Antonio Lorente Bonde-Larsen, Yolanda Fernández Sainz, Jesús Iglesias Retuerto, Javier Gallo Nieto
  • Patent number: 9468693
    Abstract: Imaging agents are described that comprise labeled substrates capable of being introduced into cells via the cystine/glutamate antiporter. The substrates may be used for imaging or detecting oxidative stress in cells by introducing the labeled agents into cells via the cystine/glutamate antiporter and subsequent detection.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: October 18, 2016
    Assignee: General Electric Company
    Inventors: Bruce Allan Hay, Jack Mathew Webster
  • Patent number: 9463194
    Abstract: The disclosure describes methods for treatment of patients co-infected with HIV and tuberculosis, wherein the patient receives effective amounts of elvitegravir, an antimycobacterial agent and a CYP inhibitor.
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: October 11, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Rebecca Restituto Begley, Joseph Marcello Custodio, Brian P. Kearney
  • Patent number: 9464058
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3 and R4 n are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: February 13, 2013
    Date of Patent: October 11, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan
  • Patent number: 9408829
    Abstract: The present invention relates to compounds acting as selective inhibitors of CD40-TRAF6 interaction, their use as medicaments and their use in the treatment of (chronic) inflammatory diseases. The present invention also relates to pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: August 9, 2016
    Assignees: LUDWIG-MAXIMILIANS-UNIVERSITÄT MÜNCHEN, MAASTRICHT UNIVERSITY, ACADEMISCH ZIEKENHUIS MAASTRICHT
    Inventors: Esther Lutgens, Christian Weber, Gerry Nicolaes
  • Patent number: 9403816
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Grant
    Filed: October 15, 2013
    Date of Patent: August 2, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Maxwell D. Cummings
  • Patent number: 9394303
    Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having pyrazolopyridine structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Grant
    Filed: April 3, 2015
    Date of Patent: July 19, 2016
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Zaneta Nikolovska-Coleska, Fardokht Abulwerdi, Hollis Showalter, Lei Miao, Jeanne Stuckey, Ahmed Mady
  • Patent number: 9382232
    Abstract: The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: July 5, 2016
    Assignees: Shenyang Pharmaceutical University, Shenyang Pharmaceutical University (Benxi) Pharmaceutical Science and Technology Co., Ltd.
    Inventors: Ping Gong, Yanfang Zhao, Yajing Liu, Xin Zhai, Sai Li, Wufu Zhu, Mingze Qin
  • Patent number: 9371295
    Abstract: The present invention relates to compounds of formula (I) and (IV), and pharmaceutically acceptable salts, tautomers, stereoisomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are for use in the treatment of disorders that are ameliorated by inhibition of HDAC such as cancer and hemoglobinopathies like ?-thalassemia or sickle cell anemia.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: June 21, 2016
    Assignees: IRBM-SCIENCE PARK S.P.A., C.N.C.C.S. SCARL COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING
    Inventors: Sergio Altamura, Alberto Bresciani, Giulia Breveglieri, Danilo Fabbrini, Roberto Gambari, Steven Harper, Ralph Laufer, Edith Monteagudo, Emanuela Nizi, Paola Pace, Vincenzo Summa
  • Patent number: 9359363
    Abstract: Herein, methods of modulating inclusion formation and stress granules in cells are described. The methods comprise contacting a cell with an inclusion inhibitor. Methods for screening for modulators of TDP-43 aggregation are also described.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: June 7, 2016
    Assignees: AQUINNAH PHARMACEUTICALS, INC., THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
    Inventors: Benjamin Wolozin, Marcie Glicksman, Gregory D. Cuny, Justin Boyd
  • Patent number: 9340503
    Abstract: Compounds of the invention are of the formula wherein: is a double bond and X is C; or is a single bond and X is N, CH or CQR1; and wherein: n is 1 to 10; R is H or QR1; each R? is independently selected from H and QR1; each Q is independently selected from a bond, CO, NH, S, SO, SO2 or O; each R1 is independently selected from C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl or C1-C10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.
    Type: Grant
    Filed: April 30, 2014
    Date of Patent: May 17, 2016
    Assignee: Karus Therapeutics, Limited
    Inventors: Stephen Joseph Shuttleworth, Cyrille Davy Tomassi
  • Patent number: 9315464
    Abstract: Compositions, compounds, and methods with significant antiviral effect against RNA viruses and especially orthomyxoviruses are contemplated, and target the viral promoter that is formed by the 5? and 3?-UTR sequences of the viral genome.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: April 19, 2016
    Assignee: Nant Holdings IP, LLC
    Inventors: Kayvan Niazi, Shahrooz Rabizadeh, Anne-Laure Le Ny, Oleksandr Buzko, Justin Golovato, Patrick Soon-Shiong
  • Patent number: 9309222
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Grant
    Filed: October 15, 2013
    Date of Patent: April 12, 2016
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Taraneh Mirzadegan, Kelly Ganamet
  • Patent number: 9303015
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Grant
    Filed: October 15, 2013
    Date of Patent: April 5, 2016
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue
  • Patent number: 9301949
    Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: April 5, 2016
    Assignee: Siga Technologies, Inc.
    Inventors: Chelsea M. Byrd, Dongcheng Dai, Robert Jordan, Dennis E. Hruby
  • Patent number: 9290476
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Grant
    Filed: October 15, 2013
    Date of Patent: March 22, 2016
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Joan Pierce, Steven Goldberg, Anne Fourie, Xiaohua Xue
  • Patent number: 9284308
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Grant
    Filed: October 15, 2013
    Date of Patent: March 15, 2016
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings, William Moore Jones, Steven Goldberg
  • Patent number: 9265784
    Abstract: A combination of a 4-anilino-3-cyanoquinoline compound (e.g. HKI-272, SKI-606, EKB-569) and a capecitabine compound in the treatment of a neoplasm is provided. Regimens, kits, and methods for treatment of neoplasm, including breast cancer including metastatic breast cancer, and lung cancer, using this combination, optionally in combination with other anti-neoplastic agents, or immune modulators are also described.
    Type: Grant
    Filed: January 30, 2014
    Date of Patent: February 23, 2016
    Assignee: WYETH LLC
    Inventors: Charles Michael Zacharchuk, Susan Elizabeth Quinn, Kenneth Kuan-Yuen Wang, Florence Marie Helene Binlich
  • Patent number: 9227940
    Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Grant
    Filed: September 4, 2014
    Date of Patent: January 5, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alan Xiangdong Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
  • Patent number: 9221804
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Grant
    Filed: October 15, 2013
    Date of Patent: December 29, 2015
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
  • Patent number: 9216954
    Abstract: A novel serine racemase inhibitor exhibits sufficient activity and specificity. The serine racemase inhibitor includes one or more compounds selected from compounds respectively represented by the following general formulas [MM_1], [DR_1], [DR?_1], [LW_1], and [ED_1] as an active ingredient.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: December 22, 2015
    Assignee: NATIONAL UNIVERSITY CORPORATION UNIVERSITY OF TOYAMA
    Inventors: Hisashi Mori, Naoki Toyooka, Mineyuki Mizuguchi, Takayuki Obita, Syuichi Hirono, Hiroaki Goda
  • Patent number: 9216956
    Abstract: Deuterium-enriched 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[(4-trifluoromethyl) -phenyl]-1,2-dihydroquinoline-3-carboxamide, having a deuterium enrichment in the amide-N methyl group of at least 70%; or a salt thereof with a pharmaceutically acceptable organic or inorganic cation; and a method of preparing said compounds. The compounds are useful in therapy, e.g. for the treatment of a malignant hyperproliferative disorder or an autoimmune disease.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: December 22, 2015
    Assignee: ACTIVE BIOTECH AB
    Inventor: Leif Svensson
  • Patent number: 9206154
    Abstract: TSHR inverse agonists and neutral antagonists that are useful for treating Graves' orbitopathy, Graves' hyperthyroidism and/or thyroid cancer.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: December 8, 2015
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Marvin Gershengorn, Susanne Neumann, Wenwei Huang, Craig J. Thomas
  • Patent number: 9206191
    Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: January 9, 2015
    Date of Patent: December 8, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Song Feng, Lu Gao, Di Hong, Lisha Wang, Hongying Yun, Shu-Hai Zhao
  • Patent number: 9173910
    Abstract: Methods and compositions are provided for treating weight related conditions and metabolic disorders by altering microbiota in a subject. One aspect provides methods and compositions to alter microbiota in a subject by administering to the subject a composition that includes a substantially purified microbiota from phyla such as Bacteroidetes, Proteobacteria, Firmicutes and Verrucomicrobia or orders such as Bacteroidales, Verrucomicrobiales, Clostridiales and Enterobacteriales or genera such as Alistipes, Clostridium, Escherichia, and Akkermansia. Another aspect includes a pharmaceutical composition for altering microbiota that includes a therapeutically effective amount of substantially purified microbiota and a pharmaceutically acceptable carrier. Yet another aspect includes methods for treating a disorder, such as obesity, in a subject in need of such treatment by changing relative abundance of microbiota in a gastrointestinal tract of the subject without or in addition to a surgical procedure.
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: November 3, 2015
    Assignees: The General Hospital Corporation, Ethicon Endo-Surgery, Inc., President and Fellows of Harvard College
    Inventors: Lee M. Kaplan, Alice P. Liou, Peter J. Turnbaugh, Jason L. Harris
  • Patent number: 9156828
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: (F) wherein A is selected from the group consisting of: (F) and; (F) and wherein Z is: (F) are useful as HIV attachment inhibitors.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: October 13, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
  • Patent number: 9149471
    Abstract: To provide an agent for treating osteoporosis, comprising an acyl thiourea compound represented by the following formula (I) or a salt thereof as an active ingredient: wherein, R1 represents an optionally substituted C1-6 alkyl group; R2 represents a fluorine atom or a chlorine atom; and R3 represents a hydrogen atom, a fluorine atom, or a chlorine atom.
    Type: Grant
    Filed: September 30, 2013
    Date of Patent: October 6, 2015
    Assignees: NATIONAL UNIVERSITY CORPORATION TOKYO UNIVERSITY OF AGRICULTURE AND TECHNOLOGY, TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Chisato Miyaura, Masaki Inada, Hidenori Fujita
  • Patent number: 9139593
    Abstract: Provided are compounds of Formula I, R1-L1-A-L2-R2??(I), and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein A, L1, L2, R1 and R2 are defined herein. The present invention also provides a pharmaceutical composition and methods of using such compounds. The compounds are useful for therapy and/or prophylaxis in a patient, and in particular to inhibitors of Soluble Epoxide Hydrolase (sEH).
    Type: Grant
    Filed: July 10, 2014
    Date of Patent: September 22, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Simona M. Ceccarelli, Carine Guerot, Henner Knust
  • Patent number: 9102591
    Abstract: The present invention is directed to benzamide containing compounds which inhibit the P2X7 Receptor.
    Type: Grant
    Filed: October 10, 2013
    Date of Patent: August 11, 2015
    Assignee: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang, Allen T. Hopper
  • Patent number: 9102674
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: August 11, 2015
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Jillian Basinger, Graeme Freestone, Varsha Gupta, Alan Kaplan, Chi-Ching Mak, Benjamin Pratt, Vincent Santora, Dipanjan Sengupta, Lino Valdez
  • Patent number: 9102620
    Abstract: The subject invention provides deuterated N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, its salts and uses.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: August 11, 2015
    Assignee: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventors: Victor Piryatinsky, Avital Laxer
  • Patent number: 9096569
    Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
    Type: Grant
    Filed: May 9, 2014
    Date of Patent: August 4, 2015
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty