Tropanes (including Nor And Dehydro Forms) Patents (Class 546/124)
  • Patent number: 10377751
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: August 16, 2018
    Date of Patent: August 13, 2019
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Daniel D. Long, John R. Jacobsen, Lan Jiang, Daisuke Roland Saito, Ioanna Stergiades
  • Patent number: 10118927
    Abstract: The disclosure relates to Substituted Piperidin-4-amino-Type Compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof wherein R1, R2, R3, Q1, Q2, E1, E2, A, B, D, W, Z, a, b, n, and x are as defined herein, compositions comprising an effective amount of a Substituted Piperidin-4-amino-Type Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted Piperidin-4-amino-Type Compound.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: November 6, 2018
    Assignee: Purdue Pharma L.P.
    Inventors: Kevin Brown, Dawit Tadesse, Nobuyuki Tanaka, Naoki Tsuno, Xiaoming Zhou
  • Patent number: 9963458
    Abstract: The disclosure relates to indole-type piperidine compounds, indoline-type piperidine compounds and related piperidine-type bicyclic compounds containing a five-membered nitrogen-containing ring (e.g., pyrrole or dihydropyrrole) fused to a heteroaryl ring, compositions comprising an effective amount of such compounds, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an indole-type piperidine compound, indoline-type piperidine compound or related piperidine-type bicyclic compound containing a five-membered nitrogen-containing ring (e.g., pyrrole or dihydropyrrole) fused to a heteroaryl ring.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: May 8, 2018
    Assignee: Purdue Pharma L.P.
    Inventor: Laykea Tafesse
  • Patent number: 9428497
    Abstract: The invention relates to a compound of formula Ia or Ib wherein R1 represents —CO2R3, —COR4 or —R5, wherein R3 represents unsubstituted or substituted C1-C6 alkyl, R4 represents hydrogen, unsubstituted or substituted C1-C6 alkyl, and R5 represents hydrogen, unsubstituted or substituted C1-C6 alkyl, R2 represents —N+(R6)(R7)(R8)X? or a nitro group, wherein R6, R7, R8 independently of each other represent unsubstituted or substituted C1-C6 alkyl or unsubstituted or substituted —(CH2)n- with n=1 to 12 provided that at least two of the substituents R6R7R8 are C1-C6 alkyl, and X? represents a halide, sulphonate, unsubstituted or substituted acetate, sulphate, hydrogen sulphate, nitrate, perchlorate, or oxalate.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: August 30, 2016
    Assignees: ABX ADVANCED BIOCHEMICAL COMPOUNDS GMBH, HELMHOLTZ-ZENTRUM DRESDEN-ROSSENDORF E.V., UNIVERSITAET LEIPZIG
    Inventors: René Smits, Alexander Hoepping, Steffen Fischer, Achim Hiller, Winnie Deuther-Conrad, Peter Brust, Jörg Steinbach, Marianne Patt, Jörg Thomas Patt, Osama Sabri
  • Patent number: 9206172
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: November 6, 2014
    Date of Patent: December 8, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Daniel D. Long, John R. Jacobsen, Lan Jiang, Daisuke Roland Saito, Ioanna Stergiades
  • Patent number: 8993592
    Abstract: Provided is a cyclic amine compound, represented by the following formula (I) that has superior acaricidal activity, has superior properties and safety, and which can be synthesized industrially advantageously, a salt thereof and an acaricide: (wherein, Cy1 and Cy2 respectively and independently represent, for example, an aryl group, R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b and R5a respectively and independently represent, for example, a hydrogen atom, R1a and R2a or R3a and R4a may together form, for example, an ethylene group, R10, R11, R20 and R21 respectively and independently represent, for example, an alkyl group, R10 or R11 may respectively or mutually, or together with an atom that bonds on Cy1, form a ring, R20 or R21 on Cy2 may respectively or mutually, or with an atom that bonds on Cy2, form a ring, m represents an integer of 0 to 5, n represents an integer of 0 to 5, p represents an integer of 0 to 5, and r represents an integer of 0 to 5).
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: March 31, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isami Hamamoto, Keiji Koizumi, Makio Yano, Masahiro Kawaguchi, Hazumi Nomura, Tetsuya Haruyama
  • Patent number: 8980912
    Abstract: The present invention provides a cyclic amine compound represented by formula (I) (in formula (I), Cy1 and Cy2 independently represent a C6-10 aryl group or a heterocyclyl group; R1a to R5a independently represent a hydrogen atom or an unsubstituted or substituted C1-6 alkyl group; R10, R11, R20 and R21 independently represent an unsubstituted or substituted C1-6 alkyl group, an unsubstituted or substituted C1-6 alkoxy group, a halogen atom or the like; m, n, p, and r each represent an integer of 0 to 5; and Y represents an oxygen atom or the like) or salt thereof, and an acaricide including the same.
    Type: Grant
    Filed: February 24, 2011
    Date of Patent: March 17, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isami Hamamoto, Keiji Koizumi, Masahiro Kawaguchi, Hisashi Tanigawa, Takehiko Nakamura, Tomomi Kobayashi
  • Publication number: 20150073014
    Abstract: The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.
    Type: Application
    Filed: July 16, 2014
    Publication date: March 12, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Sean M. Dalziel, Leticia M. Preza, Miroslav Rapta, Pierre-Jean Colson
  • Patent number: 8962653
    Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: October 1, 2013
    Date of Patent: February 24, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-Ki Choi, Adam A. Goldblum, Daniel Genov
  • Patent number: 8940762
    Abstract: The present invention is directed to methods of treating pain by administering a therapeutically effective amount of an ?7 nAChR ligand or a pharmaceutically acceptable salt thereof, to a mammal in need of treatment thereof and to pharmaceutical compositions comprising such a compound or salt.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: January 27, 2015
    Assignee: AbbVie Inc.
    Inventors: Chih-Hung Lee, Michael R. Schrimpf, Timothy A. Esbenshade, Chang Z. Zhu
  • Publication number: 20150025054
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: January 22, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estirate Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Lar
  • Patent number: 8933236
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: May 21, 2013
    Date of Patent: January 13, 2015
    Assignees: Xenon Pharmaceuticals Inc., Genentech, Inc.
    Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
  • Patent number: 8933229
    Abstract: Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof (In the formula, A represents a group that is represented by formula (A-1); R1a and R1b may be the same or different and each independently represents a C1-6 alkyl group which may be substituted by one to three halogen atoms; m and n each independently represents an integer of 0-5; X1 represents a hydroxyl group or an aminocarbonyl group; Z1 represents a single bond or the like; and R2 represents an optionally substituted C1-6 alkyl group, an optionally substituted C6-10 aryl group or the like).
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: January 13, 2015
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Yoshihiro Horiuchi, Kiyoto Sawamura, Hiroaki Fujiwara
  • Publication number: 20140336198
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Application
    Filed: May 16, 2012
    Publication date: November 13, 2014
    Applicants: MERCK PATENT GMBH, BIONOMICS LIMITED
    Inventors: Andrew Harvey, Agnes Bombrun, Rachel Cooke, Isabelle Jeanclaude-Etter, Nathan Kuchel, Jerome Molette, Jorgen Mould, Dharam Paul, Rajinder Singh, Cristina Donini, Veronique Colovray, Thomas Avery, Julia Crossman, Justin Ripper
  • Patent number: 8846655
    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 R1, R2, R3, Ra, and Y are defined herein.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: September 30, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
  • Patent number: 8835456
    Abstract: The invention provides compounds of Formula I and the pharmaceutically salts thereof. These compounds may be generally described as bridged-bicyclo indole-containing compounds. The variables shown in Formula I are defined herein. Certain compounds of Formula I are useful as antiviral agents. Compounds as 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 compounds of Formula I and at least one pharmaceutically acceptable carrier. Such pharmaceutical compositions may contain a compound of Formula I as the only active agent or may contain a combination of a compound of Formula I and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in patients.
    Type: Grant
    Filed: March 19, 2012
    Date of Patent: September 16, 2014
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Venkat Gadhachanada, Avinash Phadke, Milind Deshpande, Dawei Chen
  • Patent number: 8802698
    Abstract: The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: June 10, 2013
    Date of Patent: August 12, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Daisuke Roland Saito, Daniel D. Long, Lan Jiang, Bryan Frieman
  • Publication number: 20140221420
    Abstract: Compounds that modulate the CCR5 chemokine receptor, pharmaceutical compositions containing them, and uses therefor in the treatment of HIV and related diseases are described.
    Type: Application
    Filed: March 18, 2011
    Publication date: August 7, 2014
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventors: Arun K. Ghosh, Hiroaki Mitsuya, Venkateswararao Kalapala, Jianfeng Li
  • Publication number: 20140080855
    Abstract: The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: June 10, 2013
    Publication date: March 20, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Daisuke Roland Saito, Daniel D. Long, Lan Jiang, Bryan Frieman
  • Patent number: 8664242
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: March 4, 2014
    Assignee: Theravance, Inc.
    Inventors: Daniel D. Long, John R. Jacobsen, Lan Jiang
  • Publication number: 20130317000
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 28, 2013
    Applicants: XENON PHARMACEUTICALS INC., GENENTECH, INC
    Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
  • Publication number: 20130310379
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Application
    Filed: November 21, 2011
    Publication date: November 21, 2013
    Applicant: CONSTELLATION PHARMACEUTICALS
    Inventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Naveschuk
  • Patent number: 8476440
    Abstract: The invention provides an efficient method for preparing 3-endo-(8-azabicyclo[3.2.1]oct-3-yl)benzamide by hydrogenation, under controlled conditions, of an amino-protected 3-(8-azabicyclo[3.2.1]oct-2-en-3-yl)benzamide intermediate in which the amino-protecting group is removable by catalytic hydrogenation.
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: July 2, 2013
    Assignee: Theravance, Inc.
    Inventors: Pierre-Jean Colson, Ying Yu, Daniel D. Long, Ioanna Stergiades
  • Publication number: 20130158060
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: June 20, 2012
    Publication date: June 20, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Daniel D. Long, John R. Jacobsen, Lan Jiang
  • Publication number: 20130123243
    Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
    Type: Application
    Filed: October 18, 2012
    Publication date: May 16, 2013
    Inventor: Celtaxsys, Inc.
  • Publication number: 20130079514
    Abstract: (R)-2-Arylpropionamide compounds of formula (I), pharmaceutical preparations of the compounds and a process for making the compounds are described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonuclear leukocytes and monocytes at inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use as inhibitors of chemotaxis of neutrophils and monocytes induced by the C5a fraction of complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of polymorphonuclear leukocytes.
    Type: Application
    Filed: October 15, 2012
    Publication date: March 28, 2013
    Applicant: Dompé S.p.A.
    Inventor: Dompé S.p.A.
  • Patent number: 8329909
    Abstract: To provide a novel method for producing a 2-azaadamantane compound from a bicyclocarbamate compound. In accordance with the following scheme: a bicyclocarbamate compound represented by the formula (1) is reacted with a halogenating agent to produce a 2-azaadamantane carbamate compound represented by the formula (2), and the 2-azaadamantane carbamate compound is subjected to hydrogenolysis to produce a 2-azaadamantane compound represented by the formula (3) (in the formulae, R1 is hydrogen or the like, each of R2 and R3 which are independent of each other, is a hydrogen atom or a C1-6 alkyl group, Ar is an aryl group which may be substituted by Ra, Ra is halogen or the like, X is a halogen atom, and Y is X or a hydrogen atom).
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: December 11, 2012
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Masami Kozawa, Yuki Endo
  • Publication number: 20120302541
    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 R1, R2, R3, Ra, and Y are defined herein.
    Type: Application
    Filed: October 28, 2010
    Publication date: November 29, 2012
    Inventors: Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
  • Patent number: 8293910
    Abstract: The invention relates to a one-pot reaction for the production of 3,7-diaza-bicyclo[3.3.1]nonane compounds, wherein in a first step a dicarboxylic acid ester is reacted with a pyridine aldehyde and a primary amine. The piperidone created in this manner is reacted with formaldehyde and a further primary amine in a second step. It is essential to the invention that both reaction steps are carried out in a one-pot variation in a C1-C4 alcohol as the solvent, and that the reaction water created is removed by means of distillation.
    Type: Grant
    Filed: August 17, 2009
    Date of Patent: October 23, 2012
    Assignee: Clariant Finance (BVI) Limited
    Inventors: Melanie Sajitz, Steve Laborda, Peter Naumann, Michael Wessling
  • Patent number: 8247559
    Abstract: The invention provides an efficient method for preparing 3-endo-(8-azabicyclo[3.2.1]oct-3-yl)benzamide by hydrogenation, under controlled conditions, of an amino-protected 3-(8-azabicyclo[3.2.1]oct-2-en-3-yl)benzamide intermediate in which the amino-protecting group is removable by catalytic hydrogenation.
    Type: Grant
    Filed: March 14, 2011
    Date of Patent: August 21, 2012
    Assignee: Theravance, Inc.
    Inventors: Pierre-Jean Colson, Ying Yu, Daniel D. Long, Ioanna Stergiades
  • Publication number: 20120203004
    Abstract: An improved process for the synthesis of intermediates like Alkyl/Aralkyl (2S)-2-(tert-butoxycarbonyl)-amino-2-[-8-azabicyclo[3.2.1]oct-3-yl]-exo-acetate and analogs thereof which are useful in the synthesis of Dipeptidyl peptidase-IV (DP-PIV) inhibitors.
    Type: Application
    Filed: April 28, 2010
    Publication date: August 9, 2012
    Applicant: LUPIN LIMITED
    Inventors: Bhairab Nath Roy, Rajender Kumar Kamboj, Shaji K. Goerge, Spinvin C. Venugopal, Muthu Kumaran Shanmugvadivelu, Neelima Sinha
  • Publication number: 20120202796
    Abstract: This invention relates to a method for combating adverse effects arising from antipsychotic treatment. The invention furthermore relates to novel pharmaceutical compositions comprising a therapeutically effective combination of a compound of formula I and an antipsychotic drug.
    Type: Application
    Filed: September 2, 2009
    Publication date: August 9, 2012
    Applicant: NEUROSEARCH A/S
    Inventors: Jørgen Scheel-Krüger, Henrik Björk Hansen
  • Patent number: 8207191
    Abstract: The present invention provides a novel process for preparing pleuromutilin derivatives, novel salts of mutilin 14-(exo-8-methyl-8-azabicyclo[3.2.1]oct-3-ylsulfanyl)-acetate or solvates thereof, novel pharmaceutical compositions or formulations for topical administration comprising mutilin 14-(exo-8-methyl-8-azabicyclo[3.2.1]oct-3-ylsulfanyl)-acetate or a pharmaceutically acceptable salt or solvate thereof and their use in medical therapy, particularly antibacterial therapy.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: June 26, 2012
    Assignee: Glaxo Group Limited
    Inventors: Michael Anthony Forth, Susan ShuMei Hu Kopelman, Francis Xavier Muller, Francis Dominic Sanderson
  • Patent number: 8153653
    Abstract: The present invention relates to a compound of formula I wherein R1, R2 and R3 are each independently hydrogen, lower alkyl, lower alkoxy, cycloalkyl, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, racemic mixture, or corresponding enantiomer and/or optical isomer thereof. The compounds of formula I are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. The compounds can be used in the treatment of neurological and neuropsychiatric disorders.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: April 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Publication number: 20120041022
    Abstract: There is provided a process for the preparation of a single enantiomer of anhydroecgonine (of formula I): or a salt thereof, in which R1 is as defined in the description. Such single enantiomers may, for example, be useful intermediates in the synthesis of pharmaceuticals, in which the enantioselectivity is important.
    Type: Application
    Filed: January 29, 2010
    Publication date: February 16, 2012
    Applicant: CAMBREX KARLSKOGA
    Inventors: Lars O. Hansson, Anders Bergh
  • Publication number: 20110312993
    Abstract: The present invention relates to a compound of formula I wherein R1, R2 and R3 are each independently hydrogen, lower alkyl, lower alkoxy, cycloalkyl, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, racemic mixture, or corresponding enantiomer and/or optical isomer thereof. The compounds of formula I are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. The compounds can be used in the treatment of neurological and neuropsychiatric disorders.
    Type: Application
    Filed: June 15, 2011
    Publication date: December 22, 2011
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Publication number: 20110251192
    Abstract: The present invention pertains to the field of pharmaceutical chemistry and discloses 8-(3-aminopropyl)-3-exo-8-azabicyclo[3.2.1]octane-3-amino amide compounds represented by formula I, the pharmaceutical compositions, the preparation method and the use thereof. Such compounds or pharmaceutically acceptable salts thereof can be used as an antagonist of CCR5 in preparing medicaments for treating diseases mediated by CCR5, particularly HIV infection, asthma, rheumatoid arthritis, autoimmune diseases and chronic obstructive pulmonary diseases (COPD).
    Type: Application
    Filed: September 18, 2009
    Publication date: October 13, 2011
    Applicants: SHANGHAI TARGETDRUG CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Yaqiu Long, Xing Fan, Dongzhi Feng, Li Chen, Renhai Chen
  • Patent number: 8012956
    Abstract: A compound according to Formula I or II: wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: September 6, 2011
    Assignee: Exelixis, Inc.
    Inventors: Kenneth D. Rice, Naing Aay, Neel Kumar Anand, Arlyn Arcalas, Tae-Gon Baik, Charles M. Blazey, Owen Joseph Bowles, Chris A. Buhr, Joerg Bussenius, Simona Costanzo, Jeffrey Kimo Curtis, Steven Charles Defina, Larisa Dubenko, Abigail R. Kennedy, Angie Inyoung Kim, Katherine Lara, Sunghoon Ma, Jean-Claire Limun Manalo, Csaba J. Peto, Tsze H. Tsang, Longcheng Wang
  • Publication number: 20110190503
    Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
    Type: Application
    Filed: March 2, 2011
    Publication date: August 4, 2011
    Inventors: Genesis M. BACANI, Diego BROGGINI, Eugene Y. CHEUNG, Christa C. CHROVIAN, Xiaohu DENG, Anne M. FOURIE, Laurent GOMEZ, Cheryl A. GRICE, Aaron M. KEARNEY, Adrienne M. LANDRY-BAYLE, Alice LEE-DUTRA, Jimmy T. LIANG, Susanne LOCHNER, Neelakandha S. MANI, Alejandro SANTILLÁN, JR., Kathleen SAPPEY, Kia SEPASSI, Virginia M. TANIS, Alvah T. WICKBOLDT, John J. M. WIENER, Hartmut ZINSER
  • Patent number: 7989470
    Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: August 2, 2011
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Bjarne H. Dahl, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Jorgen Scheel-Kruger, John Paul Redrobe
  • Publication number: 20110166355
    Abstract: The invention provides an efficient method for preparing 3-endo-(8-azabicyclo[3.2.1]oct-3-yl)benzamide by hydrogenation, under controlled conditions, of an amino-protected 3-(8-azabicyclo[3.2.1]oct-2-en-3-yl)benzamide intermediate in which the amino-protecting group is removable by catalytic hydrogenation.
    Type: Application
    Filed: March 14, 2011
    Publication date: July 7, 2011
    Applicant: THERAVANCE, INC.
    Inventors: Pierre-Jean Colson, Ying Yu, Daniel D. Long, Ioanna Stergiades
  • Publication number: 20110152290
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: November 4, 2010
    Publication date: June 23, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK
  • Publication number: 20110124676
    Abstract: The invention relates to biaryl substituted azabicyclic alkane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Application
    Filed: January 27, 2011
    Publication date: May 26, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Jianguo Ji, Tao Li, Kevin B. Sippy, Chih-Hung Lee, Murali Gopalakrishnan
  • Patent number: 7947710
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: August 26, 2008
    Date of Patent: May 24, 2011
    Assignee: Theravance, Inc.
    Inventors: Daisuke Roland Saito, Daniel D. Long, John R. Jacobsen
  • Publication number: 20110118305
    Abstract: Heterocyclic amides useful as inhibitors of dipeptylpeptidase-IV (DPP-IV) enzyme, process for the preparation thereof and intermediates therefore.
    Type: Application
    Filed: July 7, 2010
    Publication date: May 19, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Péter ARÁNYI, László BALÁZS, Imre BATA, Sándor BÁTORI, Éva BORONKAY, Zoltán KAPUI, Edit SUSÁN, Tibor SZABÓ, Lajos T. NAGY, Katalin URBÁN-SZABÓ, Márton Varga
  • Publication number: 20110059929
    Abstract: In its many embodiments, the present invention relates to a novel class of substituted bicyclic piperidinyl- and piperazinylsulfonamide compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: August 12, 2008
    Publication date: March 10, 2011
    Inventors: Unmesh Shah, Craig D. Boyle, Samuel Chackalamannil
  • Publication number: 20110059937
    Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Application
    Filed: November 12, 2010
    Publication date: March 10, 2011
    Inventor: Jakob Busch-Petersen
  • Patent number: 7902220
    Abstract: The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically -acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: August 26, 2008
    Date of Patent: March 8, 2011
    Assignee: Theravance, Inc,
    Inventors: Daisuke Roland Saito, Daniel D. Long, Priscilla Van Dyke, Timothy J. Church, Lan Jiang, Bryan Frieman
  • Patent number: 7902221
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, and a are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: August 26, 2008
    Date of Patent: March 8, 2011
    Assignee: Theravance, Inc.
    Inventors: Daniel D. Long, Daisuke Roland Saito, Priscilla Van Dyke, Lan Jiang, Tmothy J. Church, John R. Jacobsen
  • Patent number: RE43390
    Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.
    Type: Grant
    Filed: October 27, 1998
    Date of Patent: May 15, 2012
    Assignees: GlaxoSmithKline LLC, SmithKline Beecham Limited
    Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt