Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Attached Directly To The Five- Membered Ring By Nonionic Bonding Patents (Class 546/279.1)
  • Publication number: 20150141624
    Abstract: This invention relates to anti-CD70 antibodies and antibody drug conjugates comprising at least one non-naturally-encoded amino acid. Disclosed herein are ?CD70 antibodies with one or more non-naturally encoded amino acids and further disclosed are antibody drug conjugates wherein the ?CD70 antibodies of the invention are conjugated to one or more toxins. Further disclosed are methods for using such non-natural amino acid antibody drug conjugates, including therapeutic, diagnostic, and other biotechnology uses.
    Type: Application
    Filed: June 19, 2013
    Publication date: May 21, 2015
    Applicant: AMBRX, INC.
    Inventors: Richard S. Barnett, Nick Knudsen, Ying Sun, Sandra Biroc, Timothy Buss, Tsotne Javahishvili, Damien Bresson, Shailaja Srinagesh, Amha Hewet, Jason K. Pinkstaff
  • Publication number: 20150141646
    Abstract: In certain aspects, compounds and uses thereof are provided. In certain aspects, compound-conjugates and uses thereof are provided.
    Type: Application
    Filed: May 14, 2013
    Publication date: May 21, 2015
    Applicant: Concortis Biosystems, Corp., a wholly owned subsidary of Sorrento Therapeutics, Inc,
    Inventors: Zhenwei Miao, Yufeng Hong, Tong Zhu
  • Patent number: 9034864
    Abstract: The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I wherein R is hydrogen or methyl, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: May 19, 2015
    Assignee: Eli Lilly and Company
    Inventors: Danwen Huang, Joshua O Odingo
  • Publication number: 20150133430
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 14, 2015
    Inventors: Qing XU, Zhe LI
  • Patent number: 9029401
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: May 12, 2015
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Patent number: 9029557
    Abstract: Contemplated compositions and methods are employed to bind in vitro and in vivo to an ?4?2 nicotinic acetylcholine receptor in a highly selective manner. Where such compounds are labeled, compositions and methods employing such compounds can be used for PET and SPECT analysis. Alternatively, and/or additionally contemplated compounds can be used as antagonists, partial agonists or agonists in the treatment of diseases or conditions associated with ?4?2 dysfunction.
    Type: Grant
    Filed: February 6, 2013
    Date of Patent: May 12, 2015
    Assignee: The Regents of the University of California
    Inventors: Jogeshwar Mukherjee, Sharon A. Kuruvilla
  • Publication number: 20150105392
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Patent number: 8993523
    Abstract: The present invention provides compounds of formula M-L-M? (where M and M? are each independently a monomeric moiety of Formula (I) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: March 31, 2015
    Assignee: Novartis AG
    Inventors: Zhuoliang Chen, Christopher Sean Straub
  • Publication number: 20150080559
    Abstract: Disclosed herein are non-natural amino acids and dolastatin analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The dolastatin analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid dolastatin analogs and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology uses.
    Type: Application
    Filed: May 24, 2012
    Publication date: March 19, 2015
    Applicant: AMBRX, INC.
    Inventors: Zhenwei Miao, Kyle Atkinson, Sandra Biroc, Timothy Buss, Melissa Neal, Vadim Kraynov, Robin Mardsen, Jason Pinkstaff, Lillian Skidmore, Ying Sun, Agnieszka Szydlik, Ianina Valenta
  • Patent number: 8980276
    Abstract: The present invention relates in part to nicotine-derived hapten-carrier conjugates of the formula (III): wherein m, n, W, -(spacer)-, X* and Y are as defined in the description. In certain embodiments, said nicotine-derived hapten-carrier conjugates can be used to prepare vaccines for the treatment and/or prevention of nicotine addiction.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: March 17, 2015
    Assignee: Pfizer Inc
    Inventors: Alan Daniel Brown, Heather Lynn Davis, David P. Gervais, Lyn Howard Jones, James R. Merson, David Cameron Pryde, David R. Stead, Michael J. McCluskie, Jennifer Marie Thorn, Paul Robert Mehelic, Parag Ashok Kolhe, Keshab Bhattacharya, Jari Ilmari Finneman, Erin Kristen Parsons, Nickolas Anastasiou
  • Publication number: 20150065464
    Abstract: The present disclosure relates to substituted amide compounds that are inhibitors of Fatty Acid Amide Hydrolase (FAAH), their stereoisomers, tautomers, prodrugs, polymorphs, solvates, pharmaceutically acceptable salts, and pharmaceutical compositions containing them.
    Type: Application
    Filed: September 21, 2012
    Publication date: March 5, 2015
    Inventors: Rajendra Kharul, Debnath Bhuniya, Kasim A. Mookhtiar, Umesh Singh, Atul Hazare, Satish Patil, Laxmikant Datrange, Mahesh Thakkar
  • Publication number: 20150057248
    Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.
    Type: Application
    Filed: September 1, 2014
    Publication date: February 26, 2015
    Applicant: The Board of Regents of The University of Texas System
    Inventors: Jia Zhou, Haijun Chen, Kenneth M. Johnson, Cheng Z. Wang
  • Publication number: 20150051253
    Abstract: The present invention is directed to (?)-(2R,3S)-2-amino-3-hydroxy-3-pyridin-4-yl-1-pyrrolidin-1-yl-propan-1-one (L)-(+)tartrate salt, a pharmaceutical composition comprising said salt, a process for making said salt, and the use of said salt in the treatment of pain.
    Type: Application
    Filed: August 14, 2014
    Publication date: February 19, 2015
    Inventors: Gyorgy F. Ambrus, Katherine C. Kurjan, Jacopo Zanon, Giovanna Libralon, Carla De Faveri
  • Patent number: 8921567
    Abstract: The present invention relates to a process for preparing an N-substituted 1H-pyrazole-5-carbonylchloride compound of the formula (I) in which R1 is hydrogen, halogen, cyano, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, C1-C6-fluoroalkoxy, C1-C4-fluoroalkoxy-C1-C4-alkyl, phenyl and the like; each R2 is independently selected from halogen, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, phenyl and the like; r is 0, 1, 2, 3 or 4; comprising the steps of i) deprotonating a compound of the formula (II) in which the variables R1, R2 and r are each as defined above, with a base selected from lithium-organic base having a carbon or nitrogen bound lithium or with a magnesium-organic base having a carbon bound magnesium; and ii) subjecting the product obtained in step (i) to a chlorocarbonylation by reacting it with a reagent selected from the group c
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: December 30, 2014
    Assignee: BASF SE
    Inventors: Karsten Körber, Prashant Deshmukh, Florian Kaiser, Michael Rack, Timo Frassetto, Gemma Veitch, Markus Kordes
  • Publication number: 20140378430
    Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 25, 2014
    Applicant: SPINIFEX PHARMACEUTICALS PTY LTD
    Inventors: Thomas David McCarthy, Alan Naylor
  • Publication number: 20140371195
    Abstract: The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Marc Labelle, Thomas Boesen, Mukund Mehrotra, Qasim Khan, Farman Ullah
  • Publication number: 20140364457
    Abstract: Novel small molecule compounds for reduction of A? 42 production and for treatment of Alzheimer's disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.
    Type: Application
    Filed: August 26, 2014
    Publication date: December 11, 2014
    Inventors: Venkateswarlu Akella, Uday Saxena, Anji Reddy Kallam
  • Publication number: 20140357650
    Abstract: The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 4, 2014
    Applicant: Fox Chase Cancer Center
    Inventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
  • Publication number: 20140357614
    Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xioahu Zhang
  • Publication number: 20140348850
    Abstract: The present invention relates to methods of reducing blood pressure in a subject by administering a plasma kallikrein inhibitor.
    Type: Application
    Filed: August 15, 2014
    Publication date: November 27, 2014
    Inventors: Edward P. Feener, Allen Clermont
  • Publication number: 20140350015
    Abstract: The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.
    Type: Application
    Filed: June 12, 2014
    Publication date: November 27, 2014
    Inventors: Edward McDonald, Julian Blagg, Mark Pichowicz, Simon Ross Crumpler
  • Publication number: 20140343052
    Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent glucose lowering effect. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof: wherein R1 represents a C1-C3 alkyl group, each substituent R2 may be the same or different and may each represent a C1-C3 alkyl group, R3 represents an optionally substituted pyridyl group or the like, R4 and R5, which are the same or different, each represent a C1-C3 alkyl group, R6 and R7, which are the same or different, each represent a C1-C3 alkyl group, and n represents 0 to 3.
    Type: Application
    Filed: May 30, 2014
    Publication date: November 20, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Shigeo YAMANOI, Katsuji KAGECHIKA, Tsuyoshi SONEDA, Yuichi OCHIAI, Hidenori NAMIKI, Fuminao DOI, Madoka HOSHINO, Shoko YOSHIDA
  • Patent number: 8859588
    Abstract: The present disclosure relates to a series of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I). wherein R1, R2, R3, R4, Q1, Q2, Q3, Q4, X, m and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I) and intermediates therefor.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: October 14, 2014
    Assignee: Sanofi
    Inventors: Zhongli Gao, Daniel Hall, David Stefany
  • Publication number: 20140296237
    Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: June 12, 2014
    Publication date: October 2, 2014
    Inventors: Hirohide NOGUCHI, Tadashi INOUE, Mikio MORITA, Yoshimasa ARANO
  • Patent number: 8846721
    Abstract: Novel small molecule compounds for reduction of A? 42 production and for treatment of Alzheimer?s Disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.
    Type: Grant
    Filed: January 22, 2011
    Date of Patent: September 30, 2014
    Assignee: Kareus Therapeutics SA
    Inventors: Venkateswarlu Akella, Uday Saxena, Anji Reddy Kallam
  • Patent number: 8841287
    Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Grant
    Filed: June 11, 2009
    Date of Patent: September 23, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xiaohu Zhang
  • Publication number: 20140275008
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Qing Xu, Zhe Li
  • Publication number: 20140275079
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, and R10 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Inventors: Lisa A. Hasvold, John Pratt, Keith F. McDaniel, George S. Sheppard, Dachun Liu, Steven W. Elmore, Robert D. Hubbard
  • Publication number: 20140256745
    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: October 19, 2012
    Publication date: September 11, 2014
    Applicant: CalciMedica, Inc.
    Inventors: Jianguo Cao, Jeffrey P. Whitten, Zhijun Wang, Evan Rogers, Jonathan Grey
  • Publication number: 20140256728
    Abstract: The present invention relates to the use of predominantly known pyridyl carboxamide derivatives as nematicides, compositions containing such compounds and methods for the control of nematodes.
    Type: Application
    Filed: October 29, 2012
    Publication date: September 11, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jörg Nico Greul, Heiko Rieck, Christian Paulitz, Matthias Riedrich, Ralf Dunkel, Arianna Martelletti, Alexander Sudau, Peter Lösel, Olga Malsam, Arnd Voerste, Hans-Georg Schwarz, Ulrich Görgens, Kerstin Ilg, Michael Maue, Pierre-Yves Coqueron, Philippe Desbordes, Philippe Meresse, Stephanie Gary, Pierre Cristau, David Bernier
  • Patent number: 8822463
    Abstract: A novel methylcyclohexane derivative, and a pharmaceutical composition including the same that is effective for the prevention or treatment of pain.
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: September 2, 2014
    Assignee: Sk Biopharmaceuticals Co., Ltd.
    Inventors: Sung Jin Bae, Han Ju Yi, Sun Gwan Hwang, Mo Ses Jeong, Yeo Jin Yoon, Sang Mi Chae, Joo Young Park, Eun Ju Ryu
  • Patent number: 8815871
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: August 26, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Muneaki Kurimura, Shinichi Taira, Takahiro Tomoyasu, Nobuaki Ito, Kuninori Tai, Noriaki Takemura, Takayuki Matsuzaki, Yasuhiro Menjo, Shin Miyamura, Yohji Sakurai, Akihito Watanabe, Yasuyo Sakata, Takumi Masumoto, Kohei Akazawa, Haruhiko Sugino, Naoki Amada, Satoshi Ohashi, Tomoichi Shinohara, Hirofumi Sasaki, Chisako Morita, Junko Yamashita, Satoko Nakajima
  • Patent number: 8809380
    Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Grant
    Filed: August 4, 2010
    Date of Patent: August 19, 2014
    Assignee: RaQualia Pharma Inc.
    Inventors: Hirohide Noguchi, Tadashi Inoue, Mikio Morita, Yoshimasa Arano
  • Patent number: 8791100
    Abstract: The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: July 29, 2014
    Assignee: Novartis AG
    Inventors: Daniela Angst, Birgit Bollbuck, Philipp Janser, Jean Quancard, Nikolaus Johannes Stiefl
  • Patent number: 8778628
    Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: July 15, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Publication number: 20140179925
    Abstract: Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas 1 and 2 wherein the variables have the meaning disclosed in the specification
    Type: Application
    Filed: December 18, 2013
    Publication date: June 26, 2014
    Applicant: Allergan, Inc.
    Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
  • Publication number: 20140171316
    Abstract: The present invention relates to anthranilamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the anthranilamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: June 19, 2014
    Applicant: BASF SE
    Inventors: Prashant Deshmukh, Karsten Körber, Florian Kaiser, Markus Kordes, Joachim Dickhaut, Arun Narine, Nina Gertrud Bandur, Gemma Veitch, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
  • Publication number: 20140163234
    Abstract: The present invention relates to a process for preparing an N-substituted 1H-pyrazole-5-carbonylchloride compound of the formula (I) in which R1 is hydrogen, halogen, cyano, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, C1-C6-fluoroalkoxy, C1-C4-fluoroalkoxy-C1-C4-alkyl, phenyl and the like; each R2 is independently selected from halogen, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, phenyl and the like; r is 0, 1, 2, 3 or 4; comprising the steps of i) deprotonating a compound of the formula (II) in which the variables R1, R2 and r are each as defined above, with a base selected from lithium-organic base having a carbon or nitrogen bound lithium or with a magnesium-organic base having a carbon bound magnesium; and ii) subjecting the product obtained in step (i) to a chlorocarbonylation by reacting it with a reagent selected from the group c
    Type: Application
    Filed: August 10, 2012
    Publication date: June 12, 2014
    Applicant: BASF SE
    Inventors: Karsten Körber, Prashant Deshmukh, Florian Kaiser, Michael Rack, Timo Frassetto, Gemma Veitch, Markus Kordes
  • Publication number: 20140142074
    Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
    Type: Application
    Filed: January 27, 2014
    Publication date: May 22, 2014
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Elisabetta ARMANI, Gabriele Amari, Carmelida Capaldi, Oriana Esposito, Ilaria Peretto
  • Patent number: 8729063
    Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: May 20, 2014
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taishing Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
  • Patent number: 8722663
    Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: May 13, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida
  • Publication number: 20140128436
    Abstract: The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula:
    Type: Application
    Filed: November 8, 2013
    Publication date: May 8, 2014
    Applicant: ActiveSite Pharmaceuticals, Inc.
    Inventors: Sukanto Sinha, Tamie Jo Chilcote
  • Patent number: 8703938
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: April 22, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
  • Patent number: 8703721
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: April 22, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Patent number: 8685992
    Abstract: The present invention refers to compounds derived from trisubstituted 1H-pyrrole rings and aromatic rings, which have the following formula (I): wherein: R1 and R2 represent, independently, an optionally substituted C6-C10 aryl radical or an optionally substituted heteroaryl radical; A and M represent, independently, a methylene group or a single bond, in which case the adjacent aromatic ring would be attached directly to the amide group; the Y?Z group represents together and indistinctly an oxygen atom, a sulfur atom, a cis-vinylidene group, an imino group, or a methine group with a sp2-hybridized carbon atom; X represents indistinctly a methine group, a cis-vinylidene group or a nitrogen atom; and W represents a hydroxyl group, an optionally substituted C1-C6 alkyl group, an optionally substituted heteroaryl group or an optionally substituted C6-C10 aryl group; or a salt, solvate or prodrug thereof, as well as to the process for their preparation and the use thereof for the treatment of cancer.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: April 1, 2014
    Assignees: Universidad del País Vasco, Ikerschem, S.L.
    Inventors: Fernando Pedro Cossío Mora, Aizpea Zubia Olascoaga, Yosu Vara Salazar, Eider Ion San Sebastián Larzabal, Dorleta Otaegui Ansa, María del Carmen Masdeu Margalef, Eneko Aldaba Arévalo
  • Publication number: 20140088156
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Application
    Filed: February 14, 2012
    Publication date: March 27, 2014
    Applicant: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Publication number: 20140080770
    Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 17, 2013
    Publication date: March 20, 2014
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi MIYAZAKI, Junko OKABE, Kosuke YASUDA, Iwao TAKAMURO, Osamu SAKURAI, Tetsuya YANAGIDA, Yutaka HISADA
  • Publication number: 20140057882
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and the treatment of certain conditions such as COPD.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 27, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Elisabetta ARMANI, GABRIELE AMARI, LAURA CARZANIGA, CARMELIDA CAPALDI, ORIANA ESPOSITO, GINO VILLETTI, RENATO DE FANTI
  • Publication number: 20140038948
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: June 25, 2013
    Publication date: February 6, 2014
    Applicant: Plexxikon Inc.
    Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
  • Publication number: 20140031341
    Abstract: An in vitro method of screening candidate compounds for the preventive or curative treatment of rosacea is described. The method can include determining the capacity of a compound to modulate the expression or activity of the Transient Receptor Potential (TRPs), as well as the use of modulators of the expression or activity of this transcription factor for the treatment of rosacea. The method can also include in vitro diagnosis or prognosis of this pathology.
    Type: Application
    Filed: December 19, 2011
    Publication date: January 30, 2014
    Applicants: UNIVERSITAT MUNSTER, GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Jerome Aubert, Martin Steinhoff