Polycyclo Ring System Having One Of The Two Rings Which Form The Spiro As One Of The Cyclos Patents (Class 546/17)
  • Patent number: 11479561
    Abstract: Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.
    Type: Grant
    Filed: May 11, 2020
    Date of Patent: October 25, 2022
    Assignee: Cytokinetics, Incorporated
    Inventors: Ippei Sato, Takashi Kamikubo, Masanori Miura, Yuji Matsushima, Hiroaki Tanaka, Yasuhiro Shiina, Susumu Yamaki, Tomoyuki Saito, Hiroshi Kiyohara, Munemichi Ohe, Kayoko Mihara, Bradley Paul Morgan, Fady Malik, Scott Emile Collibee, Luke Ashcraft, Pu-Ping Lu, Jeffrey Michael Warrington, Marc Garard
  • Patent number: 10479797
    Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the beta-3 adrenergic receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a beta-3 adrenergic receptor-mediated disorder, such as, heart failure; cardiac performance in heart failure; mortality, reinfarction, and/or hospitalization in connection with heart failure; acute heart failure; acute decompensated heart failure; congestive heart failure; severe congestive heart failure; organ damage associated with heart failure (e.g.
    Type: Grant
    Filed: June 4, 2019
    Date of Patent: November 19, 2019
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Quyen-Quyen Do, Brett Ullman, Anthony C. Blackburn, Maiko Nagura
  • Patent number: 10196403
    Abstract: Disclosed are compounds of formula (I): and pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disease and disorders in a subject in need are also disclosed.
    Type: Grant
    Filed: July 28, 2017
    Date of Patent: February 5, 2019
    Assignees: Sunovion Pharmaceuticals Inc., PGI Drug Discovery LLC
    Inventors: Taleen G. Hanania, Michele L. R. Heffernan, Philip Glyn Jones, Linghong Xie
  • Patent number: 10179791
    Abstract: The present invention relates to spiro-cyclic amine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms, monocyclic heterocycle optionally independently substituted with halogen, (1-6C)a
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: January 15, 2019
    Assignees: AbbVie B.V., AbbVie, Inc.
    Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Maria J. P. van Dongen, Nicolas J.-L. D. Leflemme, Adrian Hobson
  • Patent number: 9492435
    Abstract: The invention provides derivatives of cyclopamine having the following formula:
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: November 15, 2016
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Brian Austad, Mark L. Behnke, Alfredo C. Castro, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Andre B. Charette, Martin R. Tremblay
  • Patent number: 9238672
    Abstract: The invention is directed to a method to reduce a C—C double bond of an enone of a steroidal compound to produce a mixture of ? ketone product and ? ketone product, comprising treating a solution or suspension of the steroidal compound in a solvent with hydrogen gas in the presence of a catalyst and a substituted pyridine.
    Type: Grant
    Filed: May 2, 2014
    Date of Patent: January 19, 2016
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Brian C. Austad, Andre Lescarbeau, Lin-Chen Yu
  • Patent number: 9181252
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: November 10, 2015
    Assignee: Pfizer Inc.
    Inventors: David A. Griffith, Robert L. Dow, Scott W. Bagley, Aaron Smith
  • Publication number: 20150141403
    Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
    Type: Application
    Filed: December 1, 2014
    Publication date: May 21, 2015
    Inventors: Jose Maria CID-NUNEZ, Daniel OEHLRICH, Andres Avelino TRABANCO-SUAREZ, Gary John TRESADERN, Juan Antonio VEGA RAMIRO, Gregor James MACDONALD
  • Publication number: 20150112068
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 areas described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Application
    Filed: January 9, 2015
    Publication date: April 23, 2015
    Applicant: PFIZER INC.
    Inventors: Robert Lee Dow, David James Edmonds, David Andrew Griffith, James Alfred Southers, JR.
  • Patent number: 8993586
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: March 31, 2015
    Assignee: Pfizer Inc.
    Inventors: David A. Griffith, Robert L. Dow, Scott W. Bagley, Aaron Smith
  • Patent number: 8980877
    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: Grant
    Filed: April 13, 2012
    Date of Patent: March 17, 2015
    Assignee: DAC S.R.L.
    Inventors: Mario Varasi, Florian Thaler, Raffaella Amici, Agnese Abate, Maria Carmela Fulco, Saverio Minucci, Ciro Mercurio
  • Publication number: 20150057302
    Abstract: This invention relates to spiroindoline compounds for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: October 14, 2014
    Publication date: February 26, 2015
    Inventors: Jürgen LUTZ, Sandra KOCH, Manfred UPHOFF, Anja Regina HECKEROTH, Britta von OEPEN, Ulrich SONDERN, Christophe Pierre Alain CHASSAING
  • Publication number: 20150038490
    Abstract: The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kun Liu, Shawn J. Stachel, Craig A. Coburn, Thomas G. Steele, Richard Soll, Hao Wu, Xuanjin Peng, Yaxian Cai, Xiaoxiang Du, Jian Li
  • Publication number: 20150031678
    Abstract: The present invention relates to new substituted pyrazolo[1,5-a]pyridine having a great affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 29, 2015
    Applicant: LABORATORIES DEL DR. ESTEVE S.A.
    Inventors: José Luis Diaz Fernández, Ma Rosa Cuberes Altisent
  • Publication number: 20150018339
    Abstract: Compounds having the general formula II, III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.
    Type: Application
    Filed: February 21, 2014
    Publication date: January 15, 2015
    Inventors: Christopher R. MCCURDY, Christophe Mesangeau, Bonnie Ann Avery, Ahmed Hassan Amin Abdelazeem, Frederick T. Chin, Jacques Henri Poupaert
  • Publication number: 20150017673
    Abstract: The disclosure provides rifamycin and rifamycin derivative compositions, including rifabutin and rifabutin derivative compositions able to cause drug-sensitization in a cancer cell or inhibition of a cancer cell. The disclosure also provides methods of administering such compositions to cancer cells to sensitize them to drugs, such as chemotherapeutics, or directly inhibit them. The disclosure also provides methods of administering such compositions to increase reactive oxygen species (ROS), particularly superoxides, in cancer cells. The disclosure further provides methods of determining whether a cancer will respond to chemotherapeutics and whether to administer rifamycin or a rifamycin derivative based on ROS levels in cancer cells of a patient.
    Type: Application
    Filed: August 29, 2013
    Publication date: January 15, 2015
    Inventors: James Sacchettini, Nian Zhou, Dwight Baker, Steven A. Maxwell, Deeann Wallis
  • Publication number: 20150011470
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Application
    Filed: September 19, 2014
    Publication date: January 8, 2015
    Applicant: PFIZER INC.
    Inventors: Mary Theresa Didiuk, Robert Lee Dow, David Andrew Griffith
  • Patent number: 8927503
    Abstract: The present invention provides novel compounds of the Formula (1), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for modulating Protease Activated Receptor-2 (PAR2) and for treating a subject at risk of—or susceptible to—a disease or disorder, or having a disease or disorder associated with undesirable PAR2 activity.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: January 6, 2015
    Assignee: The University of Queensland
    Inventors: David Paul Fairlie, Ligong Liu, Mei Kwan Yau, Jacky Yung Suen, Robert Reid
  • Patent number: 8927715
    Abstract: This invention relates to novel compounds of the Formula (I*), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
    Type: Grant
    Filed: August 24, 2007
    Date of Patent: January 6, 2015
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Salvacion Cacatian, Wei He, Robert Simpson, Zhenrong Xu, Wei Zhao
  • Patent number: 8921551
    Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: December 30, 2014
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Nobuyuki Ae, Yuji Fujiwara
  • Publication number: 20140378473
    Abstract: This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: COGNITION THERAPEUTICS, INC.
    Inventors: Susan M. Catalano, Gilbert Rishton, Nicholas J. Izzo
  • Patent number: 8901085
    Abstract: The present invention provides novel compounds of the Formula (1), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for modulating Protease Activated Receptor-2 (PAR2) and for treating a subject at risk of—or susceptible to—a disease or disorder, or having a disease or disorder associated with undesirable PAR2 activity.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: December 2, 2014
    Assignee: The University of Queensland
    Inventors: David Paul Fairlie, Ligong Liu, Mei Kwan Yau, Jacky Yung Suen, Robert Reid
  • Patent number: 8883816
    Abstract: The invention relates to fused and spirocycle compounds of Formula I: or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1, R2, Q1-Q3, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: July 29, 2013
    Date of Patent: November 11, 2014
    Assignee: Purdue Pharma L.P.
    Inventors: Laykea Tafesse, Khondaker Islam
  • Publication number: 20140323730
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: Robert Lee Dow, David James Edmonds, David Andrew Griffith, James Alfred Southers, JR.
  • Publication number: 20140309220
    Abstract: The invention relates to benzoxazines useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: November 2, 2012
    Publication date: October 16, 2014
    Inventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Corey Anderson, Joseph Pontillo, Edward Adam Kallel, Mehdi Michael Djamel Numa, Bryan A. Frieman, Jason McCartney, Jennings Franklin Worley, III, Vijayalaksmi Arumugam, Johnny Uy, Nicole Hilgraf, Brian Richard Bear
  • Patent number: 8859773
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Grant
    Filed: October 27, 2011
    Date of Patent: October 14, 2014
    Assignee: Pfizer Inc.
    Inventors: David A. Griffith, Robert L. Dow, Scott W. Bagley, Aaron Smith
  • Patent number: 8859577
    Abstract: The invention provides a compound of Formula (I) Z N N O N O A1R2 R1 R3R 3 L A2 (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3,Z, A1, L and A 5 2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: October 14, 2014
    Assignee: Pfizer Inc.
    Inventors: Mary Theresa Didiuk, Robert Lee Dow, David Andrew Griffith
  • Publication number: 20140296524
    Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
    Type: Application
    Filed: May 5, 2014
    Publication date: October 2, 2014
    Applicant: Nanoquantum Sciences, Inc.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Patent number: 8846907
    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: Grant
    Filed: October 23, 2012
    Date of Patent: September 30, 2014
    Assignee: Syngenta Crop Protection LLC
    Inventors: Jerome Yves Cassayre, Louis-Pierre Molleyres, Peter Maienfisch, Fredrik Emil Malcolm Cederbaum
  • Publication number: 20140288111
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 25, 2014
    Applicant: Pfizer Inc.
    Inventors: Scott William Bagley, David Andrew Griffith, Daniel Wei-Shung Kung
  • Publication number: 20140288109
    Abstract: The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventors: Tjeerd Andries BARF, Arthur OUBRIE, Carsten SCHULTZ-FADERMRECHT, Eduard Willem ZWART, Niels HOOGENBOOM, Sander Martijn DE WILDE, Allard KAPTEIN
  • Publication number: 20140275017
    Abstract: Compounds of Formula I: (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
  • Publication number: 20140256712
    Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 11, 2014
    Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.
    Inventors: Liming SHAO, John Emmerson CAMPBELL, Michael Charles HEWITT, Una CAMPBELL, Taleen G. HANANIA
  • Publication number: 20140249308
    Abstract: The present invention relates to electronic devices, in particular organic electroluminescent devices, comprising compounds of the formula (1), to the corresponding compounds, and to a process for the preparation of these compounds.
    Type: Application
    Filed: October 11, 2012
    Publication date: September 4, 2014
    Applicant: Merck Patent GmbH
    Inventors: Amir Hossain Parham, Christof Pflumm, Anja Jatsch, Thomas Eberle, Philipp Stoessel
  • Patent number: 8822448
    Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: September 2, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
  • Patent number: 8822486
    Abstract: A compound of the formula: or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition, and a method for treating diabetes.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: September 2, 2014
    Assignee: Eli Lilly and Company
    Inventors: Chafiq Hamdouchi, Jayana Pankaj Lineswala, Pranab Maiti
  • Patent number: 8809381
    Abstract: A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: August 19, 2014
    Assignees: The University of Mississippi, L'Universite Catholique de Louvain
    Inventors: Christopher R. McCurdy, Christophe Mesangeau, Sanju Narayanan, Rae Reiko Matsumoto, Jacques Henri Poupaert
  • Patent number: 8802688
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Grant
    Filed: April 21, 2012
    Date of Patent: August 12, 2014
    Assignee: Pfizer Inc.
    Inventors: Robert Lee Dow, David James Edmonds, David Andrew Griffith, James Alfred Southers, Jr.
  • Patent number: 8785634
    Abstract: Compounds of structural formula (I) are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: July 22, 2014
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Fa-Xiang Ding, JinLong Jiang, Dong-Ming Shen, Hong Shen, Zhi-Cai Shi
  • Patent number: 8772288
    Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: July 8, 2014
    Assignee: Almirall, S.A.
    Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
  • Patent number: 8765744
    Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, R7, A, Z and m are as defined herein. The compounds of formula (I) are inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 (11beta-HSD1) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Grant
    Filed: June 23, 2011
    Date of Patent: July 1, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Frank Himmelsbach
  • Patent number: 8765752
    Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: July 1, 2014
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventor: Munetaka Ohkouchi
  • Publication number: 20140171427
    Abstract: The invention relates to heterocyclic chromene-spirocyclic piperidine amides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: November 25, 2013
    Publication date: June 19, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina HADIDA-RUAH, Edward Adam KALLEL, Mark Thomas MILLER, Joseph PONTILLO, Vijayalaksmi ARUMUGAM, Nicole HILGRAF, Jason McCARTNEY, Peter Diederik Jan GROOTENHUIS, Corey ANDERSON, Mehdi NUMA, Bryan A. Frieman, Brian Richard BEAR, Jason Philip JOHNSON, JR.
  • Patent number: 8754107
    Abstract: The present invention is directed to novel aminopyrrolidines of formula I pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compounds of formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: June 17, 2014
    Assignee: AbbVie Inc.
    Inventors: Dawn M. George, Richard W. Dixon, Michael Friedman, Adrian D. Hobson, Biqin Li, Lu Wang, Xiaoyun Wu, Neil Wishart
  • Patent number: 8754097
    Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumors.
    Type: Grant
    Filed: August 22, 2012
    Date of Patent: June 17, 2014
    Assignee: Merck Patent GmbH
    Inventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober
  • Publication number: 20140163056
    Abstract: This invention relates to novel spiroindoline compounds of formula (I) that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of said compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: August 3, 2012
    Publication date: June 12, 2014
    Inventors: Christophe Pierre Alain Chassaing, Sandra Koch, Jürgen LUTZ
  • Publication number: 20140161729
    Abstract: The present invention is directed to method of using a collection of monomers capable of forming multimers as a fluorescence reporter in different applications such as ligand detection/screening, disease diagnosis, drug discovery or screening, fluorescent labeling and imaging, or other fluorescent methodologies. Each monomer in the collection includes one or more ligand elements useful for binding to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the ligand elements directly or indirectly through a connector. Association of linker elements of different combinations of monomers, with their ligand elements bound to the target molecule to form a multimer, will generate a unique fluorescent signature different from that produced by those monomers either alone or in association with each other in the absence of the target molecule, when subjected to electromagnetic excitement.
    Type: Application
    Filed: April 9, 2012
    Publication date: June 12, 2014
    Applicant: CORNELL UNIVERSITY
    Inventors: Francis Barany, Maneesh Pingle, Donald E. Bergstrom, Sarah F. Giardina, Lee Daniel Arnold
  • Patent number: 8748446
    Abstract: Halo-organic heterocyclic compounds are described, which have the formulas Ring A is an aromatic ring bound to at least two halogen atoms, at least one of which is iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
    Type: Grant
    Filed: March 3, 2012
    Date of Patent: June 10, 2014
    Assignee: Nanoquantum Sciences, Inc.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Publication number: 20140147412
    Abstract: Disclosed are spiro compounds of formula (I), or stereomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof. The compounds can be used to treat hepatitis C virus (HCV) infection or hepatitis C disease. Furthermore disclosed are pharmaceutical compositions containing the compounds and the method of using the compounds or pharmaceutical compositions in the treatment of HCV infection or hepatitis C disease.
    Type: Application
    Filed: July 9, 2012
    Publication date: May 29, 2014
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Jiancun Zhang, Yingjun Zhang, Hongming Xie, Qingyun Ren, Huichao Luo, Tianzhu Yu, Yumei Tan
  • Patent number: 8716479
    Abstract: The invention is directed to a method to reduce a C—C double bond of an enone of a steroidal compound to produce a mixture of ? ketone product and ? ketone product, comprising treating a solution or suspension of the steroidal compound in a solvent with hydrogen gas in the presence of a catalyst and a substituted pyridine.
    Type: Grant
    Filed: December 24, 2008
    Date of Patent: May 6, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Brian C. Austad, Andre Lescarbeau, Lin-Chen Yu