The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/361)
  • Patent number: 10017476
    Abstract: The present invention relates to the compound having Formula (I) or pharmaceutically acceptable salts or solvates thereof, and its use in treating and/or preventing a Tauopathy.
    Type: Grant
    Filed: March 16, 2016
    Date of Patent: July 10, 2018
    Assignees: INSERM (Institut National de la Sante et de la Recherche Medicale), CENTRE HOSPITALIER REGIONAL ET UNIVERSITAIRE DE LILLE (CHRU), UNIVERSITE DE LILLE 2 DROIT ET SANTE
    Inventors: Nicolas Sergeant, Luc Buee, Patricia Melnyk, Marion Gay, Nicolas Le Fur
  • Patent number: 9540365
    Abstract: In one aspect, the invention provides compounds of Formula I, and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I, Formula II, or Formula III. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease and cancer, using a compound of Formula I, Formula II, or Formula III.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: January 10, 2017
    Assignee: OSTEOQC INC.
    Inventors: Debra Ellies, Jean-Philippe Rey, F. Scott Kimball
  • Patent number: 9458170
    Abstract: The present disclosure relates to a compound of formula I, a pharmaceutical composition thereof and the use thereof as an anti-tumor drug.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: October 4, 2016
    Assignee: YULIANG LI
    Inventor: Yuliang Li
  • Publication number: 20150141419
    Abstract: The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Inventors: Hong Liu, Xuechu Zhen, Haifeng Sun, Liyuan Zhu, Wangke Qian, Leiping Yu, Zeng Li, Shengbin Zhou, Wenxian Cai, Hualiang Jiang, Kaixian Chen
  • Publication number: 20150139905
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 21, 2015
    Inventors: Dinesh Chimmanamada, Weiwen Ying
  • Patent number: 9034869
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: May 19, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Patent number: 9029387
    Abstract: The present invention relates to benzonaphthyridinamines of the formula (I) as autotaxin inhibitors and to the use thereof in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in which the inhibition, regulation and/or modulation of phosphodiesterase or lysophospholipase autotaxin plays a role, in particular of various types of cancer and autoimmune and inflammatory diseases.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: May 12, 2015
    Assignee: Merck Patent GmbH
    Inventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann
  • Publication number: 20150105554
    Abstract: The present invention relates to inhibitors of the oncogenic protein kinase ALK of formula (I) as herein described and pharmaceutical compositions thereof, as well as to key intermediates towards their synthesis. The compounds of formula (I) are useful in the preparation of a medicament, in particular for the treatment of cancer.
    Type: Application
    Filed: May 10, 2013
    Publication date: April 16, 2015
    Inventors: Carlo Gambacorti-Passerini, Luca Mologni, Leonardo Scapozza, William Bisson, Shaheen Ahmed, Peter Goekjian, Sébastien Tardy, Alexandre Orsato, David Gueyrard, Joseph Benoit
  • Patent number: 9006246
    Abstract: An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. The present invention provides a compound represented by the general formula (I): (wherein definition of each group is as defined in the description) having the ENPP2 inhibitory activity, a salt thereof or a solvate thereof or a prodrug thereof, and an agent for preventing or treating urinary excretion disorder and/or improving symptoms thereof, containing them as an active ingredient.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: April 14, 2015
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Akira Ohata, Shingo Nakatani, Tetsuya Sugiyama, Takashi Morimoto
  • Publication number: 20150098905
    Abstract: The present invention relates to targeting agents and methods: of using the targeting agents to detect a fungal cell in a subject.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 9, 2015
    Applicant: Rutgers, The State University of New Jersey
    Inventors: David S. Perlin, Guillermo Garcia-Effron, Arkady Mustaev
  • Patent number: 8999977
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: April 7, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Patent number: 8999978
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: April 7, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sundeep Dugar, Sarvajit Chakravarty
  • Publication number: 20150094302
    Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating cancer mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of cancer in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 2, 2015
    Applicant: Genentech, Inc.
    Inventors: James John Crawford, Wendy B. Young
  • Publication number: 20150080366
    Abstract: Compounds of Formula (I) wherein n, A, R1, R2, R3 and R5 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
    Type: Application
    Filed: April 3, 2013
    Publication date: March 19, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Lee Fader, Pierre Louis Beaulieu, Murray Bailey, Francois Bilodeau, Rebekah J. Carson, André Giroux, Cédrickx Godbout, Oliver Hucke, Marc-André Joly, Mélissa Leblanc, Olivier Lepage, Benoit Moreau, Julie Naud, Martin Poirier, Elisia Villemure
  • Publication number: 20150065499
    Abstract: The present invention relates to compounds according to Formula I: and salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, and Y are as defined herein. Methods for preparing compounds of Formula I are also provided. The present invention further includes methods of treating cellular proliferative disorders, such as cancer, with the compounds of Formula I.
    Type: Application
    Filed: February 26, 2013
    Publication date: March 5, 2015
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
  • Patent number: 8962607
    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 Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: February 24, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J Connolly, Christopher Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark M McDonnell, Philip M Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Publication number: 20150051204
    Abstract: Present invention refers to new compounds of formula I or II, its synthesis and its use in the treatment of metabolic syndrome, particularly for the treatment of type I or type II diabetes and/or metabolic syndrome or metabolic disease or metabolic disorders.
    Type: Application
    Filed: March 28, 2012
    Publication date: February 19, 2015
    Applicant: SJT MOLECULAR RESEARCH, S.L.
    Inventors: Juan Carlos Agreda Navajas, Roberto Mikio Kassuya
  • Publication number: 20150038438
    Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.
    Type: Application
    Filed: August 29, 2012
    Publication date: February 5, 2015
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Guangming Chen, Olya Ginzburg, Song Huang, Jana Narasimhan, Srinivasa Peddi, Sean Wesley Smith, Anthony Allan Turpoff, Matthew G. Woll, Nanjing Zhang, Xiaoyan Zhang
  • Publication number: 20150023990
    Abstract: Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
    Type: Application
    Filed: September 30, 2014
    Publication date: January 22, 2015
    Inventors: Kyle J. Lindstrom, Bryon A. Merrill, Chad A. Haraldson, Michael J. Rice, Tushar A. Kshirsagar, Philip D. Heppner, Joshua R. Wurst, Shri Niwas, Sarah J. Slania
  • Publication number: 20140357647
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel 7-substituted fangchinoline derivatives of formula (I) and a pharmaceutically acceptable adduct, complex and salt thereof, to a process for the preparation of these compounds, pharmaceutical compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Application
    Filed: January 21, 2013
    Publication date: December 4, 2014
    Applicant: HANGZHOU BENSHENG PHARMACEUTICAL CO., LTD.
    Inventors: Frank Rong, Rongzhen Xu, Hongxi Lai, Fuwen Xie
  • Publication number: 20140343047
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel 5-substituted tetrandrine derivatives of formula (I) and a pharmaceutically acceptable adduct, complex and salt thereof, to a process for the preparation of these compounds, pharmaceutical compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Application
    Filed: August 20, 2012
    Publication date: November 20, 2014
    Applicant: HANGZHOU BENSHENG PHARMACEUTICAL CO., LTD.
    Inventors: Rongzhen Xu, Frank Rong, Fuwen Xie, Hongxi Lai
  • Publication number: 20140343015
    Abstract: A morphinan derivative represented by the following general formula (I) (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like, R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like, X represents O or CH2, and Y represents C?O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.
    Type: Application
    Filed: September 7, 2012
    Publication date: November 20, 2014
    Applicants: NIPPON CHEMIPHAR CO., LTD., THE KITASATO INSTITUTE
    Inventors: Hiroshi Nagase, Hideaki Fujii, Eriko Nakata, Yoshikazu Watanabe, Toshihiro Takahashi
  • Publication number: 20140336188
    Abstract: N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 13, 2014
    Applicants: PURDUE RESEARCH FOUNDATION, THE GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETSR
    Inventors: Mark S. CUSHMAN, Andrew E. MORRELL, Muthukaman NAGARAJAN, Yves G. POMMIER, Keli K. AGAMA, Smitha ANTONY
  • Publication number: 20140336178
    Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.
    Type: Application
    Filed: April 29, 2014
    Publication date: November 13, 2014
    Applicants: The General Hospital Corporation, Massachusetts Institute of Technology
    Inventors: Aleksey G. Kazantsev, Anne B. Young, David E. Housman, Steven M. Hersch
  • Publication number: 20140329800
    Abstract: The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.
    Type: Application
    Filed: December 13, 2012
    Publication date: November 6, 2014
    Inventors: Daxin Gao, Heping Yang, Yajun Yu
  • Publication number: 20140315888
    Abstract: The present invention relates to novel heterocyclic compounds useful in preparing drugs for treatment of diseases associated with various functions of the histamine 4 receptor. Especially, the said drugs are useful for treatment of inflammatory diseases, allergy, pain, nasal polyps, rhinitis, chronic sinusitis, nasal congestion, nasal itch, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis, eczema, pruritus, itchy skin, urticaria, idiopathic chronic urticaria, scleroderma, conjunctivitis, keratoconjunctivitis, ocular inflammation, dry eye, cardiac dysfunction, arrhythmia, atherosclerosis, multiple sclerosis, inflammatory bowel disease (including colitis, Crohn's disease, ulcerative colitis), inflammatory pain, neuropathic pain, osteoarthritic pain, autoimmune thyroid disease, immune-mediated (also known as type I) diabetes, lupus, post-operative adhesions, vestibular disorders and cancer.
    Type: Application
    Filed: September 28, 2012
    Publication date: October 23, 2014
    Applicant: C&C RESEARCH LABORATORIES
    Inventors: Pil Su Ho, Dong Oh Yoon, Sun Young Han, Won Il Lee, Jung Sook Kim, Woul Seong Park, Sung Oh Ahn, Hye Jung Kim
  • Patent number: 8865130
    Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: October 21, 2014
    Assignee: Vanderbilt University
    Inventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
  • Publication number: 20140302987
    Abstract: Use of substituted isoquinolinones, isoquinolinediones, isoquinolinetriones and dihydroisoquinolinones of the general formula (I) or their respective salts where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress, for strengthening plant growth and/or for increasing plant yield, and selected processes for preparing the compounds mentioned above.
    Type: Application
    Filed: July 2, 2012
    Publication date: October 9, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiss, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döering, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills
  • Patent number: 8853391
    Abstract: Disclosed are dipyridyl-pyrrole derivative compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.
    Type: Grant
    Filed: December 3, 2009
    Date of Patent: October 7, 2014
    Assignee: Merck Patent GmbH
    Inventors: Bayard R. Huck, Amanda E. Sutton, Benny C. Askew, Jr., Christopher Charles Victor Jones, Garry R. Smith, Nadia Brugger
  • Publication number: 20140288068
    Abstract: In one aspect, the invention provides compounds of Formula I, and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I, Formula II, or Formula III. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease and cancer, using a compound of Formula I, Formula II, or Formula III.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: OssiFi Inc.
    Inventors: Debra Ellies, Jean-Philippe Rey, F. Scott Kimball
  • Patent number: 8822448
    Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: September 2, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
  • Publication number: 20140242121
    Abstract: The present invention relates to a compound of Formula I: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
    Type: Application
    Filed: October 3, 2012
    Publication date: August 28, 2014
    Applicant: JANUS BIOTHERAPEUTICS, INC.
    Inventors: Grayson B. Lipford, Charles M. Zepp
  • Publication number: 20140243311
    Abstract: The present invention provides compounds represented by the general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 is cyano or the like; R2 and R3 are hydrogen or the like; R4 is C1-6 alkyl or the like; R5 is C1-6 alkyl, halo-C1-6 alkyl, cycloalkyl, cycloalkyl-C1-6 alkyl, aralkyl or the like; R6 and R7 are each hydrogen, C1-6 alkyl, halo-C1-6 alkyl, cycloalkyl, C1-6 alkoxy-C1-6 alkyl, R12R13N—C1-6 alkyl or the like, which exhibit potent dopamine D2 receptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
    Type: Application
    Filed: March 12, 2012
    Publication date: August 28, 2014
    Applicant: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Toshihiro Nishimura, Hirotaka Teranshi, Masako Yoshida, Yasunori Ueno, Kiyoshi Kasai
  • Publication number: 20140235616
    Abstract: The invention relates to compounds corresponding to formula (I), in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 21, 2014
    Applicant: SANOFI
    Inventors: Alexandre Benazet, Olivier Duclos, Nathalie Guillo, Gilbert Lassalle, Karim Macary, Valerie Vin
  • Patent number: 8785639
    Abstract: The invention provides a compound of Formula (Ie), pharmaceutically acceptable salts, or stereoisomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: July 22, 2014
    Assignee: AbbVie Inc.
    Inventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Kristine E. Frank, Dawn M. George, Eric R. Goedken, Michael Friedman, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Jeffrey W. Voss, Lu Wang, Eric C. Breinlinger, Kelly D. Mullen, Gagandeep Somal, Michael Z Hoemann
  • Publication number: 20140194414
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 10, 2014
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: MEDIVATION TECHNOLOGIES, INC.
  • Publication number: 20140179671
    Abstract: The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: September 12, 2013
    Publication date: June 26, 2014
    Applicant: Corcept Therapeutics, Inc.
    Inventors: Robin D. Clark, Nicholas C. Ray, Paul M. Blaney, Christopher A. Hurley, Karen Williams
  • Publication number: 20140171407
    Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Application
    Filed: February 17, 2014
    Publication date: June 19, 2014
    Applicant: Genentech, Inc.
    Inventors: Hazel Joan Dyke, Lewis Gazzard, Karen Williams, Huifen Chen, Samuel Kintz, Joy Drobnick, Joseph P. Lyssikatos, Simon Goodacre, Calum Macleod, Charles Ellwood
  • Publication number: 20140163012
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described.
    Type: Application
    Filed: October 31, 2013
    Publication date: June 12, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Matthew D. SURMAN, Emily E. FREEMAN, Peter R. GUZZO, Alan J. HENDERSON, Mark HADDEN
  • Publication number: 20140148451
    Abstract: The present invention relates to compounds of formulas III and V that are useful as pharmaceutical agents, particularly as autophagy inhibitors.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 29, 2014
    Applicants: Translational Genomics Research Institute, Van Andel Research Institute
    Inventors: Jeffrey Paul MacKeigan, Katie Renee Martin, Megan Lynne Goodall, Stephen Gately, Tong Wang
  • Patent number: 8729072
    Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: May 20, 2014
    Assignee: F. Hoffman-La Roche AG
    Inventors: James John Crawford, Wendy B. Young
  • Patent number: 8716274
    Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: May 6, 2014
    Assignee: Genentech, Inc.
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • Publication number: 20140121152
    Abstract: The embodiments provide prodrug compounds of Formulae I-XVII. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XVII that provides controlled release of an active agent. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of an active agent from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
    Type: Application
    Filed: March 8, 2012
    Publication date: May 1, 2014
    Applicant: Signature Therapeutics, Inc.
    Inventors: Thomas E. Jenkins, Craig O. Husfeld
  • Publication number: 20140107129
    Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Application
    Filed: December 11, 2013
    Publication date: April 17, 2014
    Applicant: Galderma Research & Development
    Inventors: Laurence CLARY, Sandrine CHAMBON, Laurent CHANTALAT, Carine ROSIGNOLI, Olivier ROYE, Jean-Claude PASCAL, Marlene SCHUPPLI-NOLLET
  • Patent number: 8697700
    Abstract: The present invention relates to piperazinone-substituted tetrahydrocarboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: April 15, 2014
    Assignee: Albany Molecular Research, Inc.
    Inventors: Matthew D. Surman, Peter R. Guzzo
  • Publication number: 20140093505
    Abstract: The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.
    Type: Application
    Filed: June 4, 2012
    Publication date: April 3, 2014
    Applicant: Xuanzhu Pharma Co., Ltd.
    Inventors: Frank Wu, Yan Zhang
  • Publication number: 20140079636
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to an binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 20, 2014
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Publication number: 20140073058
    Abstract: Methods of using dyes and associated technology are provided. A dye, such as a monomeric dye or a dimeric dye, may be used in a nucleic acid gel staining application and/or a nucleic acid detection application. Such a dye and a salt that comprises an anion that is associated with a strong acid and a cation that is associated with a strong base may be used in such an application. A dimeric dye, such as a dimeric dye capable of forming a hairpin-like structure, may be used to stain and/or detect nucleic acids via a release-on-demand mechanism. A dimeric dye having low background fluorescence in the absence of nucleic acids and high fluorescence in the presence of nucleic acids, upon binding therewith, may be used to stain and/or detect nucleic acids.
    Type: Application
    Filed: August 8, 2013
    Publication date: March 13, 2014
    Applicant: Biotium, Inc.
    Inventors: Fei Mao, Wai-Yee Leung
  • Patent number: 8653127
    Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
    Type: Grant
    Filed: January 14, 2010
    Date of Patent: February 18, 2014
    Assignee: Cara Therapeutics, Inc.
    Inventor: Robert Zhiyong Luo
  • Publication number: 20140031362
    Abstract: The present invention relates to compounds of following general formula (I): and to the pharmaceutically acceptable salts of same, the tautomers of same, the stereoisomers or mixture of stereoisomers in any proportions of same, such as a mixture of enantiomers, notably a racemic mixture, as well as to methods for preparing same and uses of same, notably as an antineoplastic agent.
    Type: Application
    Filed: April 12, 2012
    Publication date: January 30, 2014
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Rémi Rabot, Karim Bedjeguelal, El Bachir Kaloun, Philippe Schmitt, Nicolas Rahier, Patrice Mayer, Emmanuel Fournier