Spiro Patents (Class 540/543)
  • Patent number: 8575148
    Abstract: This invention concerns spiro azepane-ox-azolidinones as voltage gated Kv1.3 potassium channel blockers, pharmaceutical compositions containing these compounds, methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in the treatment of diabetes, psoriasis, obesity, transplant rejection and inflammatory neuropathies, including T-cell mediated autoimmune diseases such as rheumatoid arthritis and multiple sclerosis. The compounds have formula (1): wherein R1, R2, (R3)n, and (R4)m have the meanings given in the specification.
    Type: Grant
    Filed: December 10, 2009
    Date of Patent: November 5, 2013
    Assignee: Abbott Healthcare Products B.V.
    Inventors: Pieter Smid, Michael Mlinaric, Konrad F. Koehler, Sara Nuñez Garcia, Elmar Wegener, Josephus H. M. Lange
  • Patent number: 8563714
    Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: October 22, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Patent number: 8546379
    Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: October 1, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Brian Smith, Jeffrey Smith
  • Publication number: 20130231327
    Abstract: Substituted spiro-amide compounds corresponding to formula I in which R5 through R8, D, X, Y and Z have defined meanings, processes for preparing such spiro-amide compounds, pharmaceutical compositions containing such compounds, and methods of using such spiro-amide compounds for treating and/or inhibiting disorders or disease states mediated at least in part by the bradykinin 1 receptor.
    Type: Application
    Filed: April 15, 2013
    Publication date: September 5, 2013
    Applicant: Gruenenthal GmbH
    Inventor: Gruenenthal GmbH
  • Publication number: 20130225558
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: August 29, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Patent number: 8507669
    Abstract: It is to provide a novel optically active dibenzazepine derivative having a high utility value as an asymmetric phase-transfer catalyst. It is an optically active 6,7-dihydro-5H-dibenzo[c,e]azepine derivative represented by the following formula (1?), (wherein R represents a divalent organic group for cross-linking the 1st position and the 11th position; R1 and R2 are the same or different, and represent a hydrogen atom, halogen atom, or organic group, or R1 and R2 together represent a divalent organic group; R3? and R4? are the same or different and represent a monovalent organic group, or R3? and R4? together form an organic group that forms a cyclic structure comprising an onium nitrogen atom; Ar represents a monovalent organic group; * represents optical activity, i.e., that one axially asymmetric isomer is present in excess of the other axially asymmetric isomer with respect to a bond axis that constitutes the biphenyl structure of the compound; and X? represents a counter anion).
    Type: Grant
    Filed: April 8, 2009
    Date of Patent: August 13, 2013
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Yasushi Kubota, Tsutomu Inoue
  • Patent number: 8481524
    Abstract: The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: July 9, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Lauffer, Pan Li, Nathan Waal, Kira Mcginty, Qing Tang, Steven Ronkin, Luc Farmer, Dean Shannon, Dylan Jacobs
  • Patent number: 8481525
    Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.
    Type: Grant
    Filed: April 6, 2010
    Date of Patent: July 9, 2013
    Assignee: University of Health Network
    Inventors: Peter Brent Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
  • Publication number: 20130172325
    Abstract: The invention relates to compounds of general formula (I) wherein R1, R2, R3, R4, m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immuno-suppression would be desirable for example in organ transplantation.
    Type: Application
    Filed: July 8, 2011
    Publication date: July 4, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Simon Felbdæk Nielsen, Daniel R. Greve, Gunnar Grue-Sorensen, Carsten Ryttersgaard, Søren Christian Schou, Anette Graven Sams
  • Patent number: 8466142
    Abstract: The present invention provides novel cephalotaxus esters, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of using said compounds or compositions in the treatment of proliferative diseases (e.g., benign neoplasm, cancer, inflammatory disease, autoimmune disease, diabetic retinopathy) and infectious disease. The invention further provides methods of using said compounds or compositions in the treatment of multidrug resistant cancer.
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: June 18, 2013
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: David Gin, Jeremy Wilmot, Hakim Djaballah
  • Publication number: 20130131337
    Abstract: An optically active bisbenzyl compound or a racemic bisbenzyl compound represented by formula (2) that has axial chirality. An optically active azepine derivative or a racemic azepine derivative represented by formula (3). Methods of producing an optically active quaternary ammonium salt compound represented by formula (8).
    Type: Application
    Filed: December 5, 2012
    Publication date: May 23, 2013
    Applicant: NIPPON SODA CO., LTD.
    Inventor: NIPPON SODA CO., LTD.
  • 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
  • Patent number: 8431565
    Abstract: The present invention provides substituted imidazoheterocyclic compounds having the structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: April 30, 2013
    Assignee: Cara Therapeutics, Inc.
    Inventors: R. Paul Beckett, Richard Foster, Christelle Henault, Janet L. Ralbovsky, Carla M. Gauss, Gary R. Gustafson, Robert Zhiyong Luo, Ann-Marie Campbell, Tatiana E. Shelekhin, Mary-Margaret E. Zablocki
  • Publication number: 20130102775
    Abstract: The present invention is a photochromic material formed of a biimidazole compound represented by general formula (1-1): (where, R4 and R5 respectively and independently represent a halogen atom or alkyl group, R1 to R3 and R6 to R8 respectively and independently represent a hydrogen atom, halogen atom, alkyl group, fluoroalkyl group, hydroxyl group, alkoxyl group, amino group, alkylamino group, carbonyl group, alkylcarbonyl group, nitro group, cyano group or aryl group, Ar1 to Ar4 respectively and independently represent a substituted or unsubstituted aryl group, R4 may form a condensed, substituted or unsubstituted aryl ring with R3, and R5 may form a condensed, substituted or unsubstituted aryl ring with R6).
    Type: Application
    Filed: July 8, 2011
    Publication date: April 25, 2013
    Applicant: MITSUBISHI GAS CHEMICAL COMPANY, INC.
    Inventors: Takeru Horino, Atsuhiro Tokita, Toyoji Oshima
  • Publication number: 20130079511
    Abstract: The oxidative functionalization of olefins is a common method for the formation of vicinal carbon-heteroatom bonds. However, oxidative methods to transform allenes into synthetic motifs containing three contiguous carbon-heteroatom bonds are much less developed. The use of bicyclic methylene aziridines (MAs), prepared via intramolecular allene aziridination, as scaffolds for functionalization of all three allene carbons, among other reactions, is described herein.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 28, 2013
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Jennifer SCHOMAKER, Luke BORALSKY, John HERSHBERGER, Jared RIGOLI, Christopher S. ADAMS
  • Patent number: 8399453
    Abstract: The invention relates to organic compounds which have interesting pharmaceutical properties. In particular, the compounds are useful in the treatment and/or prevention of infections such as those caused by Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae, Plasmodium ovale, Trypanosoma cruzi and parasites of the Leishmania genus such as, for example. Leishmania donovani. The invention also relates to pharmaceutical compositions containing the compounds, as well as processes for their preparation.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: March 19, 2013
    Assignee: Novartis AG
    Inventors: Shi Hua Ang, Philipp Krastel, Seh Yong Leong, Liying Jocelyn Tan, Wei Lin Josephine Wong, Bryan K. S. Yeung, Bin Zou
  • Publication number: 20130065881
    Abstract: There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description (and which compounds are optionally substituted as indicated in the description), and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease. There is also provided combinations comprising the compounds of formula (I).
    Type: Application
    Filed: December 31, 2010
    Publication date: March 14, 2013
    Applicant: CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS
    Inventors: Joaquin Pastor Fernandez, Francisco Javier Ramos Lima, Ana Isabel Hernandez Higueras, Sonia Martinez Gonzalez, Jose Ignacio Martin Hernando, Carl-Gustave Pierre Saluste, Esther Gonzalez Cantalapiedra, Carmen Blanco Aparicio, Antonio Rodriguez Hergueta, Ana Maria Garcia Collazo, Antonio Salgado Serrano, Beatriz Noya Marino
  • Publication number: 20130065883
    Abstract: There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3, and/or Flt3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
    Type: Application
    Filed: February 18, 2011
    Publication date: March 14, 2013
    Applicant: Centro Nacional de Investigaceiones Oncologicas (CNIO)
    Inventors: Joaquin Pastor Fernández, Julen Oyarzabal Santamarina, Carl-Gustaf Pierre Saluste, Carmen Blanco Aparicio, Rosa Maria Alvarez Escobar, Virginia Rivero Buceta
  • Publication number: 20130046091
    Abstract: The use of a compound of formula I wherein Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; R1, R2, R3, R4, R8 and Ra are specified organic groups and p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2, 3, 4, 5 or 6; provided that when p is 2 then q is not 2; p+q is 1, 2, 3, 4, 5 or 6; or salts or N-oxides thereof or compositions containing them and their using incontrolling insects, acarines, nematodes or molluscs. Novel compounds are also provided.
    Type: Application
    Filed: October 23, 2012
    Publication date: February 21, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventor: Syngenta Crop Protection LLC
  • Patent number: 8367820
    Abstract: Disclosed is an optically active quaternary ammonium salt compound represented by the formula (1) below. Also disclosed are a production intermediate of such an optically active quaternary ammonium salt compound, and a method for producing such an optically active quaternary ammonium salt compound. (1) (In the formula, R1, R2, R21, R3 and R4 respectively represent an alkyl group, an aryl group or the like; R5 and R6 respectively represent an alkyl group, an alkoxy group or the like; and X? represents an anion.
    Type: Grant
    Filed: March 3, 2006
    Date of Patent: February 5, 2013
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Keiji Maruoka, Yasushi Kubota
  • Patent number: 8367657
    Abstract: The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
    Type: Grant
    Filed: June 16, 2004
    Date of Patent: February 5, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Beverly L. Wolgast, Charles A. Gilson, III, Shelley Aytes, Scott A. Estrada, Dipanjan Sengupta, Brian Smith, Ulrich Weigl, Heidedore Jlsabeth Rey-Papina
  • Publication number: 20130012495
    Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Inventors: Brian Smith, Jeffrey Smith
  • Publication number: 20130005962
    Abstract: The present invention relates to a process for the manufacturing of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) and their precursors in high optical purity to the precursors of the synthesis of substituted S-Amino-tetrahydrofuran-5-carboxylic acid amides of general formula (I) in high optical purity, and to the tautomers, enantiomers, diastereomers, mixtures and salts of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) in high optical purity, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Zhengxu HAN, Kai GERLACH, Dhileepkumar KRISHNAMURTHY, Burkhard MATTHES, Herbert NAR, Roland PFAU, Henning PRIEPKE, Annette SCHULER-METZ, Chris H. SENANAYAKE, Peter SIEGER, Wenjun TANG, Wolfgang WIENEN, Yibo XU, Nathan K. YEE
  • Publication number: 20120322788
    Abstract: The present invention relates to spirocyclic amide derivatives of the formula I, pharmaceutically acceptable salts thereof, a process for their preparation, pharmaceutical compositions containing them, and their use in therapy.
    Type: Application
    Filed: April 2, 2012
    Publication date: December 20, 2012
    Inventors: Lilian Alcaraz, Andrew Bailey, Richard James Bull, Timothy Johnson, Nicholas David Kindon, Andrew Stuart Lister, Andrew James Robbins, Michael John Stocks, Barry John Teobald
  • Publication number: 20120302549
    Abstract: The present invention provides spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: May 21, 2012
    Publication date: November 29, 2012
    Inventors: Robert Narquizian, Emmanuel Pinard, Wolfgang Wostl
  • Publication number: 20120302540
    Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.
    Type: Application
    Filed: May 24, 2012
    Publication date: November 29, 2012
    Inventors: Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
  • Publication number: 20120283243
    Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
    Type: Application
    Filed: July 11, 2012
    Publication date: November 8, 2012
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Lewis R. Makings, Miguel Garcia-Guzman Blanco, Dennis J. Hurley, Ioana Drutu, Gabriel Raffai, Daniele M. Bergeron, Akiko Nakatani, Andreas P. Termin, Alina Silina
  • Patent number: 8304407
    Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: November 6, 2012
    Assignee: Array BioPharma Inc.
    Inventors: George A. Doherty, Charles Todd Eary, Robert D. Groneberg, Zachary Jones
  • Patent number: 8304423
    Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: November 6, 2012
    Assignee: Vertex Pharmaceutical Incorporated
    Inventors: Robert J. Davies, Jinwang Xu
  • Publication number: 20120270071
    Abstract: A chromene compound having a skeleton represented by the following formula (1) and exhibiting double peak characteristic: wherein Z is a group represented by any one of the following formulas: n is an integer of 1 to 3, when n is 2 or 3, Z? s may be the same or different, with the proviso that when n is 1, Z cannot be —CH2—, and when n is 2 or 3, Z's cannot be —CH2— at the same time; R1 is an electron absorbing group having a Hammett constant ?p of more than 0, with the proviso that when there are a plurality of R1's, R1's may be the same or different; and X and Y are each independently an oxygen atom or ?NR2, with the proviso that X and Y cannot be oxygen atoms at the same time.
    Type: Application
    Filed: July 21, 2010
    Publication date: October 25, 2012
    Inventors: Toshiaki Takahashi, Junji Takenaka
  • Publication number: 20120270838
    Abstract: The present invention relates to a compound represented by the following formula (1): wherein W, X, Y, R1, R2, R33, R34, m and n are as defined in the claims, or a pharmacologically acceptable salt thereof.
    Type: Application
    Filed: April 27, 2010
    Publication date: October 25, 2012
    Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHA
    Inventors: Toru Esaki, Yoshikazu Nishimura, Yoshiaki Isshiki, Naoki Okamoto, Yoshiyuki Furuta, Akemi Mizutani, Masateru Ohta, Wayne Wen Lai, Tomoya Kotake
  • Publication number: 20120258949
    Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C?R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
    Type: Application
    Filed: April 13, 2012
    Publication date: October 11, 2012
    Applicant: DAC S.r.I.
    Inventors: Mario Varasi, Florian Thaler, Raffaella Amici, Agnese Abate, Maria Carmela Fulco, Saverio Minucci, Ciro Mercurio
  • Publication number: 20120245144
    Abstract: Benzoxazepin Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: March 20, 2012
    Publication date: September 27, 2012
    Applicant: Genentech, Inc.
    Inventors: Timothy Heffron, Brian Safina, Steven Staben, Daniel P. Sutherlin, BinQing Wei, Richard Elliott, Robert Heald, Eileen M. Seward, Emanuela Gancia, Bohdan Waskowycz
  • Publication number: 20120225866
    Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
    Type: Application
    Filed: August 20, 2010
    Publication date: September 6, 2012
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kunio Oshima, Shuuji Matsumura, Hokuto Yamabe, Naohiro Isono, Noriaki Takemura, Shinichi Taira, Takashi Oshiyama, Yasuhiro Menjo, Tsuyoshi Nagase, Masataka Ueda, Yasuo Koga, Sunao Nakayama, Kenji Tsujimae, Toshiyuki Onogawa, Kuninori Tai, Motohiro Itotani
  • Publication number: 20120220567
    Abstract: The present invention relates to certain 4,5-dihydro-3H-spiro[benzo[b]-[1,4]oxazepine compounds of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, m, n, o, and p are as herein described. In addition, the invention relates to compositions comprising at least one such compound, and methods of using the compounds for treating or preventing disorders such as non-insulin dependent (Type 2) diabetes, insulin resistance, hyperglycemia, a lipid disorder, obesity, fatty liver disease, or a skin disorder.
    Type: Application
    Filed: July 21, 2010
    Publication date: August 30, 2012
    Inventors: Gerald W. Shipps, JR., Zhiwei Yang, Yongqi Deng, Robert E. West, JR., Dineshwar P. Sinha
  • Patent number: 8232390
    Abstract: The present invention relates to pentacyclic indole derivatives of formula (I): wherein A, Ar, R1, R2, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
    Type: Grant
    Filed: May 4, 2007
    Date of Patent: July 31, 2012
    Assignee: Istituto di Richerche di Biologia Molecolare P. Angeletti SpA
    Inventors: Elena Capito, Joerg Habermann, Frank Narjes, Maria del Rosario Rico Ferreira, Ian Stansfield
  • Publication number: 20120190844
    Abstract: The invention relates to an ionic liquid composition and a method for preparing the ionic liquid. The ionic liquid comprises a cation containing the Formula I, as herein disclosed, and wherein: n is 2, R1 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R2 may form a heterocyclic ring, and R2 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R1 may form a heterocyclic ring, and R3 is selected from the group consisting of hydrogen and C1-C12 alkyl, and wherein R1 and R2 are not simultaneously selected from hydrogen.
    Type: Application
    Filed: July 20, 2011
    Publication date: July 26, 2012
    Applicant: INVISTA North America S.a r.l.
    Inventors: Stewart Forsyth, Kenneth Richard Seddon, Keith Whiston
  • Publication number: 20120165304
    Abstract: The present invention relates to compounds defined by formula (I), wherein the groups X, Y, W and R1 to R4 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are agonists of the 5-HT2C receptor, and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this receptor, such as metabolic and CNS-related disorders.
    Type: Application
    Filed: November 26, 2009
    Publication date: June 28, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephan-Georg Mueller, Christopher John Brown, Alexander Heifetz, Bernd Nosse, Juergen Prestle, Natacha Prevost, Klaus Rudolf, Stefan Scheuerer, Marcus Schindler, Dirk Stenkamp, Leo Thomas, Heather Tye
  • Publication number: 20120157428
    Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: December 2, 2011
    Publication date: June 21, 2012
    Applicant: CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Brian K. Albrecht, James E. Audia, Alexandre Côté, Victor S. Gehling, Jean-Christophe Harmange, Michael C. Hewitt, Yves LeBlanc, Christopher G. Naveschuk, Alexander M. Taylor, Rishi G. Vaswani
  • Publication number: 20120156219
    Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.
    Type: Application
    Filed: February 22, 2012
    Publication date: June 21, 2012
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
  • Publication number: 20120149686
    Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.
    Type: Application
    Filed: April 6, 2010
    Publication date: June 14, 2012
    Applicant: University Health Networks
    Inventors: Peter B. Sampson, Yong liu, Sze-Wan Le, Brian T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
  • Publication number: 20120129846
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: November 5, 2009
    Publication date: May 24, 2012
    Inventors: Zhaoning Zhu, William J. Greenlee, Mihir Baran Mandal, Duane A. Burnett, Chad E. Bennett, Troy McCracken
  • Patent number: 8163738
    Abstract: Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.
    Type: Grant
    Filed: August 17, 2006
    Date of Patent: April 24, 2012
    Assignee: Array BioPharma Inc.
    Inventors: George A. Doherty, Zachary Jones
  • Patent number: 8153622
    Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.
    Type: Grant
    Filed: August 17, 2006
    Date of Patent: April 10, 2012
    Assignee: Array BioPharma Inc.
    Inventors: George A. Doherty, C. Todd Eary, Robert D. Groneberg, Zachary Jones
  • Patent number: 8148365
    Abstract: This invention relates to a novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivative and its use in the manufacture of pharmaceutical compositions. The compound of the invention is found to be a cholinergic ligand at the nicotinic acetylcholine receptors. Due to its pharmacological profile the compound of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Grant
    Filed: May 29, 2007
    Date of Patent: April 3, 2012
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Daniel B Timmermann, Steven Charles Loechel
  • Publication number: 20120077802
    Abstract: Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: June 9, 2010
    Publication date: March 29, 2012
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
  • Patent number: 8133992
    Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.
    Type: Grant
    Filed: January 29, 2009
    Date of Patent: March 13, 2012
    Assignee: Exelixis, Inc.
    Inventors: Richard Martin, Tie-Lin Wang, Brenton T. Flatt, Xiao-Hui Gu, Ronald Griffith
  • Patent number: 8110567
    Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
    Type: Grant
    Filed: February 4, 2010
    Date of Patent: February 7, 2012
    Assignee: H. Lundbeck A/S
    Inventors: Thomas Ruhland, Garrick Paul Smith, Benny Bang-Andersen, Ejner Knud Moltzen, Kim Andersen, Ask Puschl
  • Publication number: 20120028957
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Application
    Filed: August 1, 2010
    Publication date: February 2, 2012
    Inventors: William F. DeGrado, Jun Wang
  • Publication number: 20120027796
    Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).
    Type: Application
    Filed: November 10, 2009
    Publication date: February 2, 2012
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, David Butler, Jayaprakash K. Narayanannair, Muthusamy Jayaraman, Laxmab Eltepu