The Other Ring Is A Benzene Ring Patents (Class 548/361.1)
  • Patent number: 10266525
    Abstract: The present invention provides novel processes for preparing compounds of formula (IV) and salts thereof novel intermediates, and a novel salt and polymorph thereof.
    Type: Grant
    Filed: May 31, 2016
    Date of Patent: April 23, 2019
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Robert Nicholas Bream, John David Hayler, Alan Geoffrey Ironmonger, Peter Szeto, Michael Robert Webb, Katherine Marie Penelope Wheelhouse, Robert David Willacy
  • Patent number: 10246456
    Abstract: Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, and methods for their use and production.
    Type: Grant
    Filed: July 17, 2015
    Date of Patent: April 2, 2019
    Assignee: BIOGEN MA INC.
    Inventors: Timothy Chan, Kevin Guckian, Tracy Jenkins, Jermaine Thomas, Jeffery Vessels, Gnanasambandam Kumaravel, Robert Meissner, Joseph Lyssikatos, Brian Lucas, Irina Leaf, Jeremy Duffield
  • Patent number: 9993411
    Abstract: The present invention relates to a composition for dyeing keratin fibres, comprising: at least one fatty substance, at least one surfactant; at least one oxidation base, at least one coupler of formula (B3) below and also salts thereof, optical and geometrical isomers and tautomers thereof, and hydrates thereof: (B3) in which; R1, R3, R5 represent a hydrogen; a C1-C8 alkyl or alkenyl, —SR or —OR; a (C1-C4)alkylcarbonyl; hydrocarbonyl; sulphonic or carboxylic acid; R2, R4 represent a hydrogen, a C1-C8 alkyl or alkenyl; —OR?; two groups chosen from R1, R2, R3, R4, R5 and borne by adjacent carbon atoms may form, together with said carbon atoms, a ring or a heterocycle which is optionally substituted, and which is optionally interrupted with one or more carbonyl groups; at least one of the radicals R1, R3, R5 representing a hydrogen; at least one of the radicals R2 or R4 denoting a group —OR? with R? representing a C1-C8 alkyl or alkenyl, it being possible for this radical to form, with the carbon atom bearing it
    Type: Grant
    Filed: June 25, 2014
    Date of Patent: June 12, 2018
    Assignee: L'OREAL
    Inventors: Alain Lagrange, Marie Mignon
  • Patent number: 9802922
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Grant
    Filed: January 20, 2017
    Date of Patent: October 31, 2017
    Assignee: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim
  • Patent number: 9738610
    Abstract: The present invention provides novel compounds (e.g., compounds of Formula (I)), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits comprising the inventive compounds, or compositions thereof, for treating and/or preventing a fungal or protozoan infection, inhibiting the activity of a fungal or protozoan enzyme, killing a fungus or protozoon, or inhibiting the growth of a fungus or protozoon. The fungus may be a Candida species, Aspergillus species, or other pathogenic fungal species. The compounds of the invention may inhibit the activity of fungal or protozoan cytochrome b and/or fungal or protozoan Hsp90. The present invention also provides synthetic methods of the inventive compounds.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: August 22, 2017
    Assignees: Whitehead Institute for Biomedical Research, The Broad Institute, Inc., Massachusetts Institute of Technology
    Inventors: Benjamin Vincent, Luke Whitesell, Susan L. Lindquist, Willmen Youngsaye, Stephen L. Buchwald, Jean-Baptiste Langlois, Partha P. Nag, Amal Ting, Barbara J. Morgan, Benito Munoz, Sivaraman Dandapani, Bruce Tidor, Raja R. Srinivas
  • Patent number: 9669028
    Abstract: Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.
    Type: Grant
    Filed: September 30, 2015
    Date of Patent: June 6, 2017
    Assignee: ARRIEN PHARMACEUTICALS LLC
    Inventors: Hariprasad Vankayalapati, Rajendra P. Appalaneni, Y. Venkata Krishna Reddy
  • Publication number: 20150133677
    Abstract: The present invention is directed to novel synthetic methods for preparing a spiro cyclopropyl indolinone compound represented by Structural Formula (A): or its pharmaceutically acceptable salt thereof. Also included are synthetic intermediates described herein.
    Type: Application
    Filed: December 23, 2014
    Publication date: May 14, 2015
    Applicant: University Health Network
    Inventors: Graham Cumming, Narendra Kumar B. Patel, Bryan T. Forrest, Yong Liu, Sze-Wan Li, Peter Brent Sampson, Louise G. Edwards, Heinz W. Pauls
  • Publication number: 20150119439
    Abstract: The invention provides saturated acyl guanidine compounds that inhibit F1F0-ATPase, and methods of using saturated acyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: April 30, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood, Chad A. Van Huis
  • Patent number: 9018382
    Abstract: Herein are disclosed indazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Grant
    Filed: August 13, 2014
    Date of Patent: April 28, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Celine Duquenne, Neil Johnson, Steven D. Knight, Louis LaFrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
  • Publication number: 20150111890
    Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof,that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: April 19, 2013
    Publication date: April 23, 2015
    Inventors: Lisa A. Hasvold, Dachun Liu, Chang Hoon Park, John K. Pratt, George S. Sheppard, Le Wang
  • Patent number: 9012039
    Abstract: A compound for an organic photoelectric device and an organic photoelectric device including the same, the compound being represented by the following Chemical Formula 1:
    Type: Grant
    Filed: December 28, 2010
    Date of Patent: April 21, 2015
    Assignee: Cheil Industries, Inc.
    Inventors: Nam-Soo Kim, Myeong-Soon Kang, Sung-Hyun Jung, Ho-Kuk Jung, Kyu-Yeol In, Dong-Min Kang, Eui-Su Kang, Nam-Heon Lee, Seung-Gyoung Lee, Young-Sung Park, Hyon-Gyu Lee, Eun-Sun Yu, Mi-Young Chae
  • Publication number: 20150105403
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 16, 2015
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Karensa L. Douglas, Celine Bonnefous, Andiliy G. Lai
  • Publication number: 20150087829
    Abstract: The present invention relates to compounds of formula I wherein RS denotes F or CF3, Ra denotes H or C1-4-alkyl and Z denotes a leaving group or an optionally substituted or protected hydroxyl group, suitable as intermediates in the synthesis of indanyloxydihydrobenzofuranylacetic acids, which are GPR40 agonists, to a process for preparing these intermediates and to the process for preparing the GPR40 agonists making use of an asymmetric catalytic hydrogenation reaction in the presence of a transition metal catalyst and a chiral auxiliary.
    Type: Application
    Filed: September 24, 2014
    Publication date: March 26, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Georg DAHMANN, Holger WAGNER, Matthias ECKHARDT, Markus FRANK, Marco SANTAGOSTINO, Juergen SCHNAUBELT, Uwe STERTZ, Thorsten PACHUR
  • Patent number: 8987473
    Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: March 24, 2015
    Assignee: Sato Pharmaceutical Co., Ltd.
    Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
  • Publication number: 20150080397
    Abstract: Provided herein are pharmaceutically acceptable salts of 3,5-diaminopyrazoles, for example, pharmaceutically acceptable salts of compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: September 17, 2014
    Publication date: March 19, 2015
    Inventors: Tai Wei LY, Erik Dean RAAUM
  • Publication number: 20150080434
    Abstract: A compound of formula Ia: The present invention relates to novel indazolyl derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments
    Type: Application
    Filed: November 19, 2014
    Publication date: March 19, 2015
    Inventors: Markus Berger, Hartmut Rehwinkel, Jan Dahmen, Anders Eriksson, Thomas Hansson, Nafizal Hossain, Per Thomas Klingstedt, Matti Lepistö, Stinabritt Nilsson, Martin Hemmerling, Karl Edman
  • Patent number: 8980934
    Abstract: The present teachings provide a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: March 17, 2015
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Radoslaw Laufer, Sze-Wan Li, Grace Ng
  • Patent number: 8962835
    Abstract: Certain imidazopyrazines of Formula (I): or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: February 24, 2015
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford
  • Patent number: 8962156
    Abstract: An organic EL device includes an organic EL emitter that emits blue light and a blue color filter through which the light emitted from the organic EL emitter passes. The blue color filter contains a coloring material selected from the group consisting of a triarylmethane dye, a lake pigment, a copper-phthalocyanine pigment, and a mixture of a copper-phthalocyanine pigment and a dioxazine pigment. The chromaticity of the light that has passed through the blue color filter after being emitted from the organic EL emitter, is in the range defined by lines connecting three chromaticity coordinates (0.150, 0.060), (0.143, 0.031), and (0.130, 0.049) on the CIE chromaticity diagram.
    Type: Grant
    Filed: November 28, 2008
    Date of Patent: February 24, 2015
    Assignee: Dai Nippon Printing Co., Ltd.
    Inventor: Norihisa Moriya
  • Publication number: 20150045398
    Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
    Type: Application
    Filed: October 7, 2014
    Publication date: February 12, 2015
    Applicant: NOVARTIS AG
    Inventors: Claus EHRHARDT, Leslie Wighton MCQUIRE, Pascal RIGOLLIER, Olivier ROGEL, Michael David SHULTZ, Ruben Alberto TOMMASI
  • Publication number: 20150031681
    Abstract: A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and the like, which comprises a compound of Formula (I): wherein A is CR1E or a nitrogen atom, X—Y—Z is N—CO—NR3AR3B and the like, R1A to R1E are each independently a hydrogen atom and the like, R2A to R2D are each independently a hydrogen atom and the like, R3A and R3B are each independently an optionally-substituted C3-10 cycloalkyl and the like, and n is 1 or 2 or a pharmaceutically acceptable salt thereof, which exhibits potent modulatory-effects on the activity of ?7 nicotinic acetylcholine receptor (?7 nAChR).
    Type: Application
    Filed: April 9, 2013
    Publication date: January 29, 2015
    Inventors: Shinya Usui, Hiroki Yamaguchi, Yoko Nakai
  • Publication number: 20150018337
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: July 29, 2014
    Publication date: January 15, 2015
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Publication number: 20150005232
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 1, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Zacharia Cheruvallath, Philip Erickson, Jun Feng, Mallareddy Komandla, John David Lawson, Christopher McBride, Joanne Miura, Sean Murphy, Mingnam Tang, Huong-Thu Ton-Nu
  • Publication number: 20150005279
    Abstract: The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: June 26, 2014
    Publication date: January 1, 2015
    Applicant: ABBVIE INC.
    Inventors: Dominique Bonafoux, Heather M. Davis, Kristine E. Frank, Michael M. Friedman, J. Martin Herold, Michael Z. Hoemann, Raymond Huntley, Augustine Osuma, George Sheppard, Gagandeep K. Somal, Jennifer Van Camp, Stacy A. Van Epps, Anil Vasudevan, Grier A. Wallace, Lu Wang, Lu Wang, Zhi Wang, Noel S. Wilson, Xiangdong Xu
  • Patent number: 8921545
    Abstract: The present invention is directed to novel synthetic methods for preparing a spiro cyclopropyl indolinone compound represented by Structural Formula (A): (A) or its pharmaceutically acceptable salt thereof. Also included are synthetic intermediates described herein.
    Type: Grant
    Filed: April 6, 2011
    Date of Patent: December 30, 2014
    Assignee: University Health Network
    Inventors: Graham Cumming, Narendra Kumar B. Patel, Bryan T. Forrest, Yong Liu, Sze-Wan Li, Peter Brent Sampson, Louise G. Edwards, Heinz W. Pauls
  • Patent number: 8916555
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: December 23, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
  • Publication number: 20140371202
    Abstract: The present teaching provide indazole compounds represented by Structural Formulae (I) or (I?) or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as TTK protein kinase, polo-like kinase 4 (PLK4) and Aurora kinases having anticancer activity against breast cancer cells, colon cancer cells, and ovarian cancer cells.
    Type: Application
    Filed: October 12, 2012
    Publication date: December 18, 2014
    Applicant: University Health Network
    Inventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter Brent Sampson, Miklos Feher, Donald E. Awrey
  • Patent number: 8912188
    Abstract: Disclosed herein are substituted quinoxaline carboxylic acids of Formula (I): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: December 16, 2014
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero, Robert C. Kelly
  • 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
  • Publication number: 20140364398
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: PFIZER INC.
    Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
  • Publication number: 20140336440
    Abstract: Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.
    Type: Application
    Filed: January 24, 2013
    Publication date: November 13, 2014
    Inventors: Ernst Schonbrunn, Rongshi Li, Said M. Sebti
  • Publication number: 20140336224
    Abstract: Compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases are disclosed. Processes for preparing compounds of the Formula (I), use of the compounds for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and pharmaceutical compositions which comprise compounds of the Formula (I) are disclosed.
    Type: Application
    Filed: October 18, 2012
    Publication date: November 13, 2014
    Inventors: Ping Lan, Kun Liu, Anthony Ogawa, Hong Shen, Christine Yang, Yuguang Wang, Richard Beresis, Changhe Qi
  • Publication number: 20140323518
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 to R9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.
    Type: Application
    Filed: August 2, 2012
    Publication date: October 30, 2014
    Inventors: Aiping Cheng, Neeraj Garg, Lars Krüger, Joakim Löfstedt, Eva Koch, Konrad Koehler, Lars Hagberg, Daniel Nöteberg
  • Patent number: 8871946
    Abstract: The present invention relates to the benzimidazole-4-carboxamide derivatives, their preparation methods, pharmaceutical compositions and their uses; wherein X represents monosubstituted or bissubstituted or polysubstitued C1-C14 alkoxy, monosubstituted or bisubstituted or polysubstitued C1-C14 alkyl, monosubstituted or bisubstituted or polysubstitued C2-C14 alkenyl, monosubstituted or bisubstituted or polysubstitued C6-C14 aryl, or monosubstituted or bisubstituted or polysubstitued 5 to 6 membered heterocyclic group, or monosubstituted or bisubstituted or polysubstitued fused ring group containing nitrogen heteroatom; Y represents hydrogen, monosubstituted or bisubstituted or polysubstitued C1-C16 alkyl, monosubstituted or bisubstituted or polysubstitued C6-C12 aryl, or monosubstituted or bisubstituted or polysubstitued 5 to 6 membered heterocyclic group, or monosubstituted or bisubstituted or polysubstitued fused ring group containing nitrogen heteroatom.
    Type: Grant
    Filed: January 6, 2010
    Date of Patent: October 28, 2014
    Assignee: Zhejiang Medicine Co., Ltd. Xinchang Pharmaceutical Factory
    Inventors: Xianjin Luo, Fei Xue, Zhonglv Zhang, Naiyun Xiu
  • Patent number: 8871760
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, and R3 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: October 28, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Christine E. Brotherton-Pleiss, Ralph New Harris, III, Bradley E. Loe, Francisco Javier Lopez-Tapia, Pankaj D. Rege, David Bruce Repke, Russell Stephen Stabler, Keith Adrian Murray Walker
  • Publication number: 20140315945
    Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: EPIZYME, INC.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • Patent number: 8846745
    Abstract: A method of treating insulin resistance, obesity and metabolic syndrome by administering an indazolemethoxyalkanoic acid as described herein.
    Type: Grant
    Filed: May 8, 2012
    Date of Patent: September 30, 2014
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Angelo Guglielmotti, Giuseppe Biondi
  • Patent number: 8846935
    Abstract: Herein are disclosed indazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Grant
    Filed: May 5, 2011
    Date of Patent: September 30, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Celine Duquenne, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
  • Publication number: 20140288084
    Abstract: In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: October 28, 2012
    Publication date: September 25, 2014
    Applicant: VANDERBILT UNIVERSITY
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Woods, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney, Darren W. Engers
  • Publication number: 20140288105
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: EPIZYME, INC.
    Inventors: RICHARD CHESWORTH, LORNA HELEN MITCHELL, GIDEON SHAPIRO, OSCAR MIGUEL MORADEI
  • Patent number: 8841462
    Abstract: The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: September 23, 2014
    Inventors: Robert A. Heald, Philip Jackson, Joseph P. Lyssikatos, Stephen Price, Pascal Pierre Alexandre Savy
  • Patent number: 8841455
    Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R1, R2, R3, R4 and R5 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases and pain.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: September 23, 2014
    Assignee: Array BioPharma Inc.
    Inventors: Mark Laurence Boys, Michael F. Bradley, Robert Kirk DeLisle, D. David Hennings, April L. Kennedy, Fredrik P. Marmsater, Matthew David Medina, Mark C. Munson, Bryson Rast, James P. Rizzi, Martha E. Rodriguez, George T. Topalov, Qian Zhao
  • Publication number: 20140275074
    Abstract: The present invention is related to a compound represented by formula (I), wherein X1, X2, X3, X4, X5, R5, R6, R7, R8, n, p, q, ring A and ring B are as described in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 24, 2012
    Publication date: September 18, 2014
    Inventors: Kayoko Hata, Manami Masuda, Hiromi Nakai, Daisuke Taniyama, Hiroyuki Tobinaga, Yoshio Hato, Motohiro Fujiu
  • Publication number: 20140243310
    Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: October 23, 2012
    Publication date: August 28, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tohru Yamashita, Takuya Fujimoto, Ryo Mizojiri, Kazuko Yonemori, Hideki Hirose, Zenichi Ikeda, Ikuo Fujimori, Kyoko Toyofuku, Tsuneo Yasuma, Nobuyuki Matsunaga
  • Publication number: 20140243366
    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: May 1, 2014
    Publication date: August 28, 2014
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20140220050
    Abstract: The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SA
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Prashant Kashinath Bhavar, Srikant Viswanadha, Swaroop Kumar V.S. Vakkalanka, Gayatri Swaroop Merikapudi
  • Publication number: 20140221339
    Abstract: The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are the same or different aromatic rings, etc., and ring A is a heterocyclic ring. The compound of the invention or a pharmaceutically acceptable salt thereof has potent mPGES-1 inhibiting activity and is useful as an agent for the treatment or prevention of a disease, such as rheumatoid arthritis, osteoarthritis, temporomandibular joint disorders, low back pain, endometriosis, dysmenorrhea, overactive bladder, malignant tumors or neurodegenerative disease.
    Type: Application
    Filed: August 17, 2012
    Publication date: August 7, 2014
    Applicant: NIPPON SHINYAKU CO., LTD.
    Inventor: Hironori Otsu
  • Patent number: 8796270
    Abstract: An imidazopyridine having the structure or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: August 5, 2014
    Assignee: Gilead Connecticut, Inc.
    Inventor: Scott A. Mitchell
  • Publication number: 20140194471
    Abstract: In one aspect, the invention relates to substituted 1-benzylindolin-2-one analog compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: January 6, 2013
    Publication date: July 10, 2014
    Applicant: Vanderbilt University
    Inventors: Craig W. Lindlsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney
  • Patent number: 8772327
    Abstract: A compound represented by the following general formula (1) or a salt thereof, which has superior inhibitory activity against type 4 PLA2, and thus has prostaglandin and/or leucotriene production suppressing action [X represents a halogen atom, an alkyl group which may be substituted, or the like, Y represents hydrogen atom or an alkyl group which may be substituted, and Z represents hydrogen atom or an alkyl group which may be substituted].
    Type: Grant
    Filed: October 17, 2012
    Date of Patent: July 8, 2014
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Kohei Morita, Hiroshi Kuriyama, Kosuke Tanaka