At Least Three Ring Hetero Atoms In The Two Rings Which Form The Spiro Patents (Class 546/19)
  • Patent number: 11370791
    Abstract: The preparation and properties of crystalline polymorphs and solvates of 1-benzyl-8-methyl-1,4,8-triazaspiro-[4.5]-decan-2-one free base and of the mono- and dihydrochloride salts and solvates thereof are disclosed, as is an amorphous polymorph of the dihydrochloride. A pharmaceutical composition containing one or more polymorphs and a method of using that composition are also disclosed.
    Type: Grant
    Filed: February 21, 2020
    Date of Patent: June 28, 2022
    Assignee: CASSAVA SCIENCES, INC.
    Inventors: Michael Zamloot, Lindsay Burns Barbier, Shawn Anthony Kucera
  • Patent number: 11286260
    Abstract: Disclosed herein are p38? mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and therapeutic methods of using the p38? mitogen-activated protein kinase inhibitors.
    Type: Grant
    Filed: May 14, 2021
    Date of Patent: March 29, 2022
    Assignee: GEN1E LIFESCIENCES INC.
    Inventors: Adam Galan, Wendy Luo, Ritu Lal
  • Patent number: 9102792
    Abstract: A polymer composition that contains at least one high performance polymer and at least one aromatic amide oligomer is provided. The oligomer can serve as a flow aid that lowers the overall viscosity of the polymer matrix under shear.
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: August 11, 2015
    Assignee: Ticona LLC
    Inventors: Kamlesh P. Nair, Joseph J. Grenci, Xinyu Zhao
  • Patent number: 9034891
    Abstract: There are provided certain bicyclic heterocyclic compounds that act as M1 muscarinic receptor modulators. Compositions containing these compounds and their use are also disclosed.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: May 19, 2015
    Assignee: ISRAEL INSTITUTE FOR BIOLOGICAL RESEARCH
    Inventors: Abraham Fisher, Nira Bar-Ner, Victoria Nachum
  • Publication number: 20150099738
    Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
    Type: Application
    Filed: June 30, 2014
    Publication date: April 9, 2015
    Inventors: Mark L. BEHNKE, Alfredo C. CASTRO, Lawrence K. CHAN, Catherine A. EVANS, Louis GRENIER, Michael J. GROGAN, Yves LEBLANC, Tao LIU, Stephane PELUSO, Daniel A. SNYDER, Thomas T. TIBBITTS
  • Patent number: 8993567
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: March 31, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
  • Publication number: 20150065715
    Abstract: The present invention relates to novel amidopyridine derivatives. More specifically, the present invention provides a medicinal agent which is useful as a prophylactic or therapeutic agent for diseases based on the production of cytokines from T cells, comprising as the active ingredient an amidopyridine derivative or a pharmacologically acceptable salt thereof. Provided are an amidopyridine derivative of the following general formula (I): wherein each symbol has the same meaning as defined in the description, or a pharmacologically acceptable salt thereof.
    Type: Application
    Filed: April 12, 2013
    Publication date: March 5, 2015
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventors: Masayuki Watanabe, Hiroyuki Furukawa, Maiko Hamada, Naoto Fujie, Hiroyuki Ushio, Tooru Takashima
  • Patent number: 8957070
    Abstract: The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof. According to the present invention, a glucokinase activator useful as a pharmaceutical agent such as agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like can be provided.
    Type: Grant
    Filed: April 20, 2006
    Date of Patent: February 17, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuneo Yasuma, Osamu Ujikawa
  • Patent number: 8940743
    Abstract: The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: January 27, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Marcel Frans Leopold De Bruyn, Gregor James MacDonald, Ludo Edmond Josephine Kennis, Xavier Jean Michel Langlois, Frans Alfons Maria Van Den Keybus, Yves Emiel Maria Van Roosbroeck
  • Patent number: 8927117
    Abstract: The present invention relates to a compound of the formula (1) and (2) The invention further relates to a process to produce the compound. The invention additionally relates and an electronic device containing the compound of the formula (1) or (2). The electronic device can be an organic electroluminescence devices, particularly a blue emitting device, in which compounds are used as host materials or dopants in the emitting layer and/or as hole transport materials and/or as electron transport materials.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: January 6, 2015
    Assignee: Merck Patent GmbH
    Inventors: Arne Buesing, Holger Heil, Philipp Stoessel
  • Patent number: 8841296
    Abstract: This invention provides novel substituted 1,4-dioxa-8-azaspiro[4,5]decane compounds of the general formula (1), wherein R1 is selected from phenethyl, 4,6-dimethoxypyrimidin-2-yl and (2-chloro-5-thiazolyl)methyl and R2 is selected from the group consisting of hydroxy, 4-bromo-2-chlorophenoxy, morpholin-4-yl, (2-chloro-5-thiazolyl)methyloxy, benzyloxy, phenylsulfanyl, benzotriazol and 5-chloro-2-fluoroanilino. The present invention also relates to a process for the preparation of novel substituted 1,4-dioxa-8-azaspiro[4,5]decanes of general formula (1). The novel substituted 1,4-dioxa-8-azaspiro[4,5]decane of general formula (1) has fungicidal activity.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: September 23, 2014
    Assignee: Council of Scientific and Industrial Research, Anusandhan Bhawan, Rafi Marg
    Inventors: Mukund Vinayak Deshpande, Sunita Ranjan Deshpande, Fazal Shirazi, Preeti Madhukar Chaudhary, Nelavelli Malleswara Rao, Baidyanath Mohanty, Nageshwar Nath Sharma, Anand Kumar Bachhawat, Ganesan Kaliannan, Sanjoy Paul, Raj Kumar, Bommena Vittal Rao, Bhimrao Bodhanrao Gawali, Vaddu Venkata Narayana Reddy, Jhillu Singh Yadav
  • Publication number: 20140275048
    Abstract: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Alkermes Pharma Ireland Limited
    Inventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
  • Publication number: 20140206691
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 24, 2014
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M.P. Doweyko, Joel C. Barrish, John Wityak
  • Patent number: 8765735
    Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: July 1, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Publication number: 20140155387
    Abstract: The present invention refers to: a compound having the general formula (I), wherein n is 0, 1, 2 or; m is 0, 1, 2 or 3; o is 0, 1, 2 or 3; W, X, Y and Z are independently selected from CH, N or N-oxide; A is NR4, C?O, C?S, OP(O)(O), P?O, CH2, or a heteroarly selected from the group consisting of (a), (b), (c), (d), (e), (f), (g); V is C?O, O, S, CH2, or NR5; as well as its use in treating inflammatory diseases such as asthma, COPD, inflammation post infection, arthritis, atherosclerosis, pain and dermatitis.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 5, 2014
    Applicants: QURIENT, CO. LTD., INSTITUT PASTEUR KOREA
    Inventors: Zaesung No, Jaeseung Kim, Sung-Jun Han, Jung Hwan Kim, Young Sam Park, Sangchul Lee, Kiyean Nam, Jeongjun Kim, Jinhwa Lee, Sunhee Kang, Min Jung Seo, Saeyeon Lee, Gahee Choi
  • Patent number: 8729077
    Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: May 20, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Don Roberts, Wieslaw Kazmierski, Richard Grimes
  • Publication number: 20140113895
    Abstract: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.
    Type: Application
    Filed: December 20, 2013
    Publication date: April 24, 2014
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Publication number: 20140113890
    Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.
    Type: Application
    Filed: December 23, 2013
    Publication date: April 24, 2014
    Applicant: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shuoming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
  • Patent number: 8673931
    Abstract: There are disclosed bicyclic heterocyclic spiro compounds; pharmaceutical compositions comprising these compounds; and methods for the treatment in a mammal of diseases and conditions which are susceptible to modulation of the M1 muscarinic receptor, including Alzheimer's disease, insulin resistance syndrome and type 2 diabetes. Other embodiments are also disclosed.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: March 18, 2014
    Inventors: Abraham Fisher, Nira Bar-Ner, Victoria Nachum
  • Publication number: 20140038955
    Abstract: Heteroaryl amide analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: October 2, 2013
    Publication date: February 6, 2014
    Applicant: H. Lundbeck A/S
    Inventors: David C. IHLE, Qin GUO, Kevin HODGETTS, Jun YUAN
  • Patent number: 8614324
    Abstract: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.
    Type: Grant
    Filed: March 8, 2010
    Date of Patent: December 24, 2013
    Assignee: Pain Therapeutics, Inc.
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Patent number: 8592444
    Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C?R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
    Type: Grant
    Filed: April 14, 2009
    Date of Patent: November 26, 2013
    Assignee: DAC S.R.L.
    Inventors: Mario Varasi, Florian Thaler, Agnese Abate, Giacomo Carenzi, Ciro Mercurio, Saverio Minucci
  • Patent number: 8586200
    Abstract: Disclosed is an organic compound represented by the following Chemical Formula 1 that easily dissolves in an organic solvent, and that is applicable as a host material of an emission layer of an organic photoelectric device since it emits fluorescence and phosphorescence at a red wavelength through a blue wavelength.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: November 19, 2013
    Assignee: Cheil Industries, Inc.
    Inventors: Sung-Hyun Jung, Hyung-Sun Kim, Ho-Jae Lee, Eun-Sun Yu, Mi-Young Chae
  • Publication number: 20130302728
    Abstract: The present invention relates to a radically polymerizable composition comprising a hydroxylamine ester used to manufacture color filters. The invention further relates to novel hydroxylamine esters. The invention further relates to the use of hydroxylamine esters in all liquid crystal display components requiring post-baking.
    Type: Application
    Filed: July 11, 2013
    Publication date: November 14, 2013
    Applicant: BASF SE
    Inventors: Hisatoshi Kura, Kaori Sameshima, Kazuhiko Kunimoto, Peter Nesvadba, Masaki Ohwa
  • Publication number: 20130281443
    Abstract: The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.
    Type: Application
    Filed: June 19, 2013
    Publication date: October 24, 2013
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Congxin Liang, Marcel Koenig, Yuanjun He, Par Holmberg
  • Patent number: 8557796
    Abstract: Substituted 1-oxa-2,8-diaza-spiro[4,5]dec-2-ene compounds and processes for their production, the use thereof for producing pharmaceutical compositions, pharmaceutical compositions containing these compounds and methods of treatment using these compounds.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: October 15, 2013
    Assignee: Gruenenthal GmbH
    Inventors: Heinrich Helmut Buschmann, Guenter Werner Englberger, Tieno Germann, Hagen-Henrich Hennies, Corinna Maul, Bernd Sundermann, Joerg Holenz
  • Patent number: 8541595
    Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.
    Type: Grant
    Filed: November 3, 2009
    Date of Patent: September 24, 2013
    Assignee: Merch Sharp & Dohme Corp.
    Inventors: Peter J. Manley, Kausik K Nanda, B. Wesley Trotter
  • Patent number: 8536196
    Abstract: Specifically useful stereoisomers of 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections as well as their use in the treatment of a disease related to TP, such as cardiovascular diseases.
    Type: Grant
    Filed: January 18, 2008
    Date of Patent: September 17, 2013
    Assignee: Evolva SA
    Inventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Prathama S. Mainkar, Melya Hughes Crameri, Thierry Bonnaud, Joanne Kelleher, David Pearson
  • Patent number: 8530469
    Abstract: The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I inhibitors; antimetabolites; tubulin targeting agents; DNA binder and topoisomerase II inhibitors; alkylating agents; monoclonal antibodies; anti-hormones; signal transduction inhibitors; proteasome inhibitors; DNA methyl transferases; cytokines; retinoids and HDAC or HAT modulators.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: September 10, 2013
    Assignee: Astex Therapeutics Ltd.
    Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford, Maria Grazia Carr, Robert Downham, Michael Alistair O'Brien, Theresa Rachel Phillips, Andrew James Woodhead
  • Patent number: 8530465
    Abstract: The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.
    Type: Grant
    Filed: August 1, 2012
    Date of Patent: September 10, 2013
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Chia-Chung Lee
  • Publication number: 20130225624
    Abstract: There are provided certain bicyclic heterocyclic compounds that act as M1 muscarinic receptor modulators. Compositions containing these compounds and their use are also disclosed.
    Type: Application
    Filed: March 14, 2013
    Publication date: August 29, 2013
    Inventors: Abraham FISHER, Nira BAR-NER, Victoria NACHUM
  • Publication number: 20130210800
    Abstract: The present application relates to compounds of Formula (I), and Formula (II), or pharmaceutically acceptable salt thereof, wherein A, X, Y, Z, e, f, R1, R2, R3, R4, R5, R5b, R6, R7, R8, R9, R10, R11, R20, R21, R22 and R23 are defined herein. These novel pyridine derivatives that are useful in therapy, in particular for treating diseases or conditions mediated by Smo, including the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to methods of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: October 19, 2011
    Publication date: August 15, 2013
    Applicant: PFIZER INC.
    Inventors: Sajiv Krishnan Nair, Simon Paul Planken
  • Patent number: 8487099
    Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
    Type: Grant
    Filed: November 3, 2008
    Date of Patent: July 16, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William J. Greenlee, Zhaoning Zhu, Theodros Asberom, Xianhai Huang, Hubert B. Josien
  • Patent number: 8481555
    Abstract: The disclosure generally relates to compounds of the following formula, including their salts, as well as compositions and methods of using the compounds. The compounds are prodrugs for ligands, agonists, and partial agonists for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
    Type: Grant
    Filed: April 29, 2011
    Date of Patent: July 9, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kimberley A. Lentz, Rex Denton, James H. Cook, II, Ivar M. McDonald, Dalton King, Richard E. Olson, Nenghui Wang, Robert A. Mate, Christiana I. Iwuagwu, F. Christopher Zusi, John E. Macor, Matthew D. Hill, Haiquan Fang
  • Publication number: 20130172549
    Abstract: Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: January 29, 2013
    Publication date: July 4, 2013
    Applicant: H. Lundbeck A/S
    Inventor: H. Lundbeck A/S
  • Publication number: 20130165450
    Abstract: This invention relates to certain thiazole carboxamide derivatives of Formula (I) as inhibitors of 3-phosphoinositide-dependent protein kinase (PDK-1). The compounds can be useful in inhibiting the proliferation of cancer cells, and other aberrant conditions where the PDK-1 signaling pathway is overstimulated.
    Type: Application
    Filed: September 9, 2011
    Publication date: June 27, 2013
    Inventors: Hon-Chung Tsui, Sunil Paliwal, Thierry Oliver Fischmann
  • Publication number: 20130158002
    Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: February 28, 2011
    Publication date: June 20, 2013
    Inventors: Mark E. Layton, Michael J. Kelly, Timothy J. Hartingh
  • Publication number: 20130150376
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Application
    Filed: March 31, 2011
    Publication date: June 13, 2013
    Applicant: PFIZER INC.
    Inventors: Michael Aaron Brodney, Ivan Viktorovich Efremov, Christopher John Helal, Brian Thomas O'Neill
  • Publication number: 20130131042
    Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
    Type: Application
    Filed: August 12, 2011
    Publication date: May 23, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joseph L. Duffy, Jianming Bao, Debra L. Ondeyka, Sriram Tyagarajan, Patrick Shao, Feng Ye, Revathi Katipally, Aaron Zwicker, Edward C. Sherer, Michael A. Plotkin, Remond Moningka, Zahid Hussain, Harold B. Wood, Feroze Ujjainwalla, F. Anthony Romero, Paul E. Finke, Yi Zang, Weiguo Liu
  • Publication number: 20130102600
    Abstract: The present invention relates to a compound having the general formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
    Type: Application
    Filed: October 18, 2012
    Publication date: April 25, 2013
    Applicants: F. HOFFMANN-LA ROCHE LTD, EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL), SAVIRA PHARMACEUTICALS GMBH
    Inventors: F. HOFFMANN-LA ROCHE LTD, SAVIRA PHARMACEUTICALS GMBH, EUROPEAN MOLECULAR BIOLOGY LABORAT
  • Patent number: 8415333
    Abstract: The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: April 9, 2013
    Assignee: Respiratorious AB
    Inventors: Martin Johansson, Viveca Thornqvist Otlner, Jorgen Toftered, David Wensbo, Maria Dalence
  • Publication number: 20130079320
    Abstract: The invention relates to amine substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: September 25, 2012
    Publication date: March 28, 2013
    Applicant: Gruenenthal GmbH
    Inventor: Gruenenthal GmbH
  • Patent number: 8404702
    Abstract: Pharmaceutical formulations containing salts of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl]-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: March 26, 2013
    Assignee: Opko Health, Inc.
    Inventors: Zhihui Qiu, Larisa Reyderman
  • Patent number: 8399449
    Abstract: The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula (I) wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR1 (R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R2 is carbamoyl optionally having substituent(s); and R3 is hydroxy optionally having substituent(s), or a salt thereof.
    Type: Grant
    Filed: February 25, 2009
    Date of Patent: March 19, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Nobuhiro Fujii, Yuya Oguro, Satoshi Sasaki, Shigeru Kondo
  • Publication number: 20130060026
    Abstract: This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Application
    Filed: September 6, 2012
    Publication date: March 7, 2013
    Applicant: INCYTE CORPORATION
    Inventors: Jiacheng Zhou, Yongzhong Wu, Pingli Liu, Ganfeng Cao
  • Publication number: 20130053386
    Abstract: The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: October 5, 2010
    Publication date: February 28, 2013
    Inventors: William Colby Brown, Richard W. Heidebrecht, Jason Brubaker, Christian Fischer, John T. Hendrix, Elizabeth H. Kelley, Rachel N. MacCoss, Joey L. Methot, Thomas Miller, Karin M. Otte, Phieng Siliphaivanh, Thomas Reger, Peter D. Williams, Catherine M. Wiscount
  • Publication number: 20130040978
    Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
    Type: Application
    Filed: May 13, 2011
    Publication date: February 14, 2013
    Inventors: Joseph L. Duffy, Jianming Bao, Debra L. Ondeyka, Sriram Tyagarajan, Patrick Shao, Feng Ye, Revathi Katipally, Paul E. Finke, Yi Zang, Michael A. Plotkin, F. Anthony Romero, Remond Moningka, Zahid Hussain
  • Patent number: 8361500
    Abstract: Pharmaceutical formulations containing a salt of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, which are suitable for forming into a tablet dosage form, as well as tablet dosage forms are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: January 29, 2013
    Assignee: Opko Health, Inc.
    Inventors: Zhihui Qiu, Wing-Kee Philip Cho, Na Zhao, Victor Ming-she Wong
  • Publication number: 20130023611
    Abstract: Hindered amines represented by the general formula (I): (wherein R is an alkyl or hydroxyalkyl group having 1 to 30 carbon atoms or alkenyl having 2 to 30 carbon atoms; n is an integer of 1 to 4; when n is 1, R1 is alkyl having 1 to 22 carbon atoms, alkenyl having 2 to 22 carbon atoms, or a group represented by the general formula (III): (R is as defined above), while when n is 2 to 4, R1 is an n-valent organic group having 2 to 20 carbon atoms). When added to synthetic resins or coating materials, the amines can impart long-period stabilizing effect to the resins or the materials and exhibit excellent resistance to extraction with acid rain or chemicals.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 24, 2013
    Applicant: ADEKA CORPORATION
    Inventors: Yoshinori NEGISHI, Takashi AYABE, Etsuo TOBITA
  • Patent number: 8338431
    Abstract: The present invention relates to a compound according to formula I, wherein X, A, G, E, R1, R2, R3 are as shown herein; and pharmaceutically acceptable salts, hydrates, N-oxides or solvates hereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
    Type: Grant
    Filed: February 26, 2008
    Date of Patent: December 25, 2012
    Assignee: Leo Pharma A/S
    Inventors: Ravindra Babu Bollu, Jakob Felding, Simon Feldbæk Nielsen, Jens Christian Højland Larsen