1,2-oxazoles (including Hydrogenated) Patents (Class 546/272.1)
  • Patent number: 10329286
    Abstract: The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
    Type: Grant
    Filed: June 12, 2017
    Date of Patent: June 25, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Peter A. Blomgren, Kevin S. Currie, Julie Farand, Christian Gege, Jeffrey E. Kropf, Jianjun Xu
  • Patent number: 9913471
    Abstract: The present invention provides compounds of formula (I): wherein A1, A2, A3 and A4 are independently of one another C—H, C—R5, or nitrogen; B1—B2—B3—B4 is —CH2—C?N—CH2—, —CH2—N—CH2—CH2—, —CH2—C?CH—O— or —CH?C—CH2—O—; G1 is oxygen or sulfur; L is a single bond or C1-C8alkylene; R1 is hydrogen, C1-C8alkyl, C1-C8alkylcarbonyl-, C1-C8alkoxy, C2-C8alkenyl, C2-C8alkynyl, C1-C8alkoxy-C1-C8alkyl, aryl or aryl substituted by one to three R6, or R1 is heterocyclyl or heterocyclyl substituted by one to three R6 or C1-C8alkoxycarbonyl-; R2 is hydrogen, C1-C8haloalkyl or C1-C8alkyl; R3 is C1-C8haloalkyl; R4 is aryl or aryl substituted by one to three R6, or R4 is heterocyclyl or heterocyclyl substituted by one to three R6; Y1 is CR7R8, C?O or C?S; Y2, Y3 and Y4 are independently CR7R8, C?O, C?S, N—R9, O, S, SO or SO2; wherein at least two adjacent ring atoms in the ring formed by Y1, Y2, Y3 and Y4 are heteroatoms; each R7 and R8 is independently hydrogen, halogen, C1-C8alkyl, or C1-C8haloalkyl; and R5, R6, R7, R8 and
    Type: Grant
    Filed: November 28, 2016
    Date of Patent: March 13, 2018
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Patent number: 9458092
    Abstract: The present invention is to provide a novel ?-substituted glycinamide derivative, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof. The present invention provides a compound represented by the general formula (I), which has TRPM8 inhibitory effects: [wherein A1 represents a C6-10 aryl and the like, A2 represents a C6-10 aryl and the like, X represents CH and the like, Y represents —CR1R2— and the like, R1 and R2 independently represent a hydrogen atom and the like, R3 and R4 independently represent a halogen atom and the like, n is 1 or 2], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing diseases or symptoms caused by hyperexcitability or disorder of afferent neurons.
    Type: Grant
    Filed: May 7, 2014
    Date of Patent: October 4, 2016
    Assignee: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Hideaki Hirasawa, Naohiro Kawamura, Junichi Kobayashi
  • Publication number: 20150148373
    Abstract: The invention provides heterocyclic guanidine compounds that inhibit F1F0-ATPase, and methods of using heterocyclic guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 28, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood
  • Patent number: 9040563
    Abstract: Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase IC50 value of 25 nM and a whole cell H-Ras processing IC50 value of 90 nM. Several of the inhibitors proved highly selective for hFTase over the related prenyltransferase enzyme geranylgeranyltransferase-I (GGTase-I).
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: May 26, 2015
    Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc., Yale University
    Inventors: Said M. Sebti, Andrew Hamilton
  • Publication number: 20150133495
    Abstract: Disclosed herein is a compound of Formula I or a pharmaceutically acceptable salt thereof, in which A, G, R1 and R2 are as defined herein. The compounds and pharmaceutical compositions of the compounds are suitable for the treatment of HCV infection in mammals and are also useful to modulate or inhibit NS3/4 dimerization.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 14, 2015
    Inventor: Daniel Lamarre
  • Patent number: 9029400
    Abstract: The present invention relates to 5-oxoisoxazole derivatives of the formula I, the pharmaceutically usable salts thereof and the use thereof as medicinal substances.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: May 12, 2015
    Assignee: Sanofi
    Inventors: Stefan Petry, Manfred Seidel, Gerhard Zoller, Gunter Müller, Karl-Heinz Baringhaus, Hubert Heuer
  • Publication number: 20150126485
    Abstract: The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Publication number: 20150119576
    Abstract: There is provided a novel intermediate for producing pesticides. A method for producing the compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method may comprise dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C1-C6 alcohol and an aprotic polar solvent in the presence of a base and water.
    Type: Application
    Filed: December 29, 2014
    Publication date: April 30, 2015
    Inventors: Manabu YAOSAKA, Tomohisa UTSUNOMIYA, Yuji MORIYAMA, Tomohiro MATSUMOTO, Kazutaka MATOBA
  • Publication number: 20150111879
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 24, 2014
    Publication date: April 23, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel P. SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Publication number: 20150111900
    Abstract: The present invention relates to compounds described herein Formula (I) and pharmaceutical acceptable salts thereof, which modulate the activity of calcium release-activated calcium (CRAC) channel. The invention also describes the compounds of Formula (I) and pharmaceutical compositions containing such compounds thereof for treating, managing, and/or lessening the severity of diseases, disorders, syndromes or conditions associated with the modulation of calcium release-activated calcium (CRAC) channel.
    Type: Application
    Filed: May 1, 2013
    Publication date: April 23, 2015
    Inventors: Nageswara Rao Irlapati, Zubair Abdul Wajid Shaikh, Vijay Pandurang Karche, Gokul Keruji Deshmukh, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150111925
    Abstract: The present invention relates to compounds described herein Formula (I) and pharmaceutical acceptable salts thereof, which modulate the activity of calcium release-activated calcium (CRAC) channel. The invention also describes the compounds of Formula (I) and pharmaceutical compositions containing such compounds thereof for treating, managing, and/or lessening the severity of diseases, disorders, syndromes or conditions associated with the modulation of calcium release-activated calcium (CRAC) channel.
    Type: Application
    Filed: May 1, 2013
    Publication date: April 23, 2015
    Inventors: Nageswara Rao Irlapati, Gokul Keruji Deshmukh, Nilesh Raghunath Khedkar, Kiran Chandrashekhar Kulkarni, Zubair Abdul Wajid Shaikh, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150111747
    Abstract: 6-Pyridone-2-carbamoylazoles of the general formula (I) are described as herbicides. In this formula (I), W, X and Z represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q represents a 5-membered radical such as oxadiazyl.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ralf Braun, Stefan Lehr, Arnim Koehn, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
  • Publication number: 20150105550
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Patent number: 9006447
    Abstract: The present invention relates to a method for preparing 4-chloro-, 4-bromo- or 4-iodobenzaldehyde oximes and phenyl-substituted isoxazoline compounds prepared from these oximes.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: April 14, 2015
    Assignee: BASF SE
    Inventors: Karsten Koerber, Markus Kordes, Michael Rack, Wolfgang Von Deyn, Florian Kaiser
  • Publication number: 20150098928
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A is a 6-membered aromatic ring containing carbon atoms and 0-3 nitrogen atoms as ring members, said ring optionally substituted with 1-5 substituents independently selected from R2; R1 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl or C4-C7 cycloalkylalkyl, each optionally substituted with one or more substituents independently selected from R21; R21 is independently H, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, CN or NO2; and Q is as defined in the disclosure.
    Type: Application
    Filed: January 6, 2014
    Publication date: April 9, 2015
    Applicant: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Ty Wagerle, Ming Xu
  • Publication number: 20150099762
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Application
    Filed: December 9, 2014
    Publication date: April 9, 2015
    Inventors: Hilary Schenck EIDAM, Kaushik RAHA, Zhen GONG, Huiping Amy GUAN, Chengde WU, Haiying YANG, Haiyu YU, Zhiliu ZHANG, Mui CHEUNG
  • Patent number: 8980892
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: March 17, 2015
    Assignees: Syngenta Crop Protection LLC, Syngenta Limited
    Inventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
  • Patent number: 8980916
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: March 17, 2015
    Assignees: Merck Sharp & Dohme Corp., Mochida Pharmaceutical Co., Ltd.
    Inventors: Matthew Voss, Hiroki Sone, Samuel Chackalamannil, Munetaka Ohkouchi
  • Publication number: 20150072993
    Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.
    Type: Application
    Filed: November 18, 2014
    Publication date: March 12, 2015
    Inventors: Zengyun AN, Liang CHEN, Shuhui CHEN, Jean Marie DEFAUW, Scott Dale HOLMSTROM, Ping HU, Chongzhi TANG, William Hunter WHITE, Wentao WU, Yang ZHANG
  • Patent number: 8975261
    Abstract: The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: March 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo
  • Publication number: 20150065507
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 5, 2015
    Applicant: Glaxo Group Limited
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Patent number: 8969383
    Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Grant
    Filed: June 12, 2014
    Date of Patent: March 3, 2015
    Assignee: RaQualia Pharma Inc.
    Inventors: Hirohide Noguchi, Tadashi Inoue, Mikio Morita, Yoshimasa Arano
  • Patent number: 8957063
    Abstract: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: February 17, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Monika Ermann, Innocent Mushi
  • Patent number: 8952042
    Abstract: The present invention relates to compounds of formula (1): where R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: February 10, 2015
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Claus Kremoser, Ulrich Abel, Christoph Steeneck, Olaf Kinzel
  • Patent number: 8952176
    Abstract: Disclosed is a compound useful as a type I 11?hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkenyl or the like, One of R2 and R3 is a group of the formula: —C(?O)—Y—R4, wherein Y is —NR9— or the like, R4 is optionally substituted cycloalkyl or the like, R9 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, The other is a group of the formula: —V—R5, wherein V is a bond, —O— or the like, R6 is hydrogen or optionally substituted alkyl, R5 is hydrogen, optionally substituted alkyl or the like, X is a bond, —S—, —SO— or the like, U is a bond or optionally substituted alkylene, R7 is hydrogen or optionally substituted alkyl, Z is —S—, —O— or —NR8—, R8 is hydrogen, optionally substituted alkyl or the like.
    Type: Grant
    Filed: June 6, 2006
    Date of Patent: February 10, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tomoyuki Ogawa, Noriyuki Kurose, Satoru Tanaka, Koichi Nishi
  • Patent number: 8946236
    Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: February 3, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Bernd Alig, Ruediger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Goergens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
  • Publication number: 20150018353
    Abstract: Compound of Table I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Application
    Filed: December 26, 2012
    Publication date: January 15, 2015
    Applicant: IRONWOOD PHARMACEUTICALS, INC.
    Inventors: Charles Kim, Takashi Nakai, Joel Moore, Nicholas Robert Perl, G-yoon Jamie Im, Timothy Claude Barden, Rajesh R. Iyengar, Daniel P. Zimmer, Angelika Fretzen, Paul Allan Renhowe
  • Publication number: 20150005165
    Abstract: The invention relates to a carboxylic acid derivatives of benzoheterocyclyl pyridines and benzoheterocyclyl pyrimidines of general formula (I) and to the use thereof as herbicides.
    Type: Application
    Filed: July 24, 2012
    Publication date: January 1, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Michael Gerhard Hoffmann, Marco Bruenjes, Uwe Doeller, Hans-Joerg Dietrich, Isolde Haeuser-Hahn, Christopher Hugh Rosinger, Elmar Gatzweiler, Ines Heinemann
  • Patent number: 8921399
    Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
    Type: Grant
    Filed: April 16, 2012
    Date of Patent: December 30, 2014
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
  • Publication number: 20140356322
    Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.
    Type: Application
    Filed: January 11, 2013
    Publication date: December 4, 2014
    Inventors: Craig M. Crews, Dennis Buckley, Alessio Ciulli, William Jorgensen, Peter C. Gareiss, Inge Van Molle, Jeffrey Gustafson, Hyun-Seop Tae, Julien Michel, Dentin Wade Hoyer, Anke G. Roth, John David Harling, Ian Edward David Smith, Afjal Hussain Miah, Sebastien Andre Campos, Joelle Le
  • Patent number: 8889710
    Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: November 18, 2014
    Assignee: Eli Lilly and Company
    Inventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
  • Publication number: 20140336190
    Abstract: This application relates to chemical compounds which may act as inhibitors of; or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2, R2b, R3, R4a, R4b, and R5 are described herein.
    Type: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Rick Lee, Ruben Martinez, Samuel E. Metobo, Michael Mish, Manuel Munoz, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
  • Patent number: 8877783
    Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: November 4, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
  • Patent number: 8877782
    Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: November 4, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
  • Publication number: 20140322195
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Application
    Filed: October 24, 2012
    Publication date: October 30, 2014
    Inventors: Matthew Voss, Hiroki Sone, Samuel Chackalamannil, Munetaka Ohkouchi
  • Publication number: 20140309225
    Abstract: The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, wherein R1 is a substituent represented by the following formula (II-1), (III-1), or (IV-1) (wherein R3, R4, R5, n, and X1 have the same definitions as those described in the specification), and R2 is a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 16, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Hideyasu FUJIWARA, Shinsuke MIZUMOTO, Yohei KUBO, Hiyoku NAKATA, Shinji HAGIWARA, Yasutaka BABA, Takashi TAMURA, Hidenobu KUNIYOSHI, Tomoyuki MASHIKO, Mari YAMAMOTO
  • Patent number: 8859588
    Abstract: The present disclosure relates to a series of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I). wherein R1, R2, R3, R4, Q1, Q2, Q3, Q4, X, m and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I) and intermediates therefor.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: October 14, 2014
    Assignee: Sanofi
    Inventors: Zhongli Gao, Daniel Hall, David Stefany
  • Patent number: 8853410
    Abstract: The present invention relates to a new method of preparing halogenated styrene compounds of formula (VIII) which are precursors in the process of synthesis of substituted isoxazoline compounds of formula (I) wherein R1 to R5, R8 and R9 are described as in the description. The present invention relates further to the synthesis of compounds of formula (I) starting from acetophenones. The desired styrenes of formula are prepared from the appropriate substituted acetophenone. Asides bromo anilines react with formoxime. Obtained oximes undergo a cycloaddition with the styrenes and give isoxazolines. Compounds of formula (I) can then be prepared in a palladium catalyzed carbonylative amination reaction of the isoxazolines.
    Type: Grant
    Filed: April 29, 2010
    Date of Patent: October 7, 2014
    Assignee: BASF SE
    Inventors: Michael Rack, Karsten Koerber, Florian Kaiser
  • Publication number: 20140296237
    Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: June 12, 2014
    Publication date: October 2, 2014
    Inventors: Hirohide NOGUCHI, Tadashi INOUE, Mikio MORITA, Yoshimasa ARANO
  • Publication number: 20140296246
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2a, R2b, R3, and X are described herein.
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Ruben Martinez, Samuel E. Metobo, Michael R. Mish, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
  • Publication number: 20140296229
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4, A1 and A2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Application
    Filed: March 26, 2014
    Publication date: October 2, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Harald ENGELHARDT, Davide GIANNI, Andreas MANTOULIDIS, Christian SMETHURST
  • Patent number: 8846719
    Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: September 30, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
  • Publication number: 20140275111
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Hilary Schenck EIDAM, Kaushik Raha, Zhen Gong, Huiping Guan, Chengde Wu, Haiying Yang, Haiyu Yu, Zhiliu Zhang, Mui CHEUNG
  • Publication number: 20140275531
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Patent number: 8835461
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: September 16, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
  • Publication number: 20140256744
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: May 21, 2014
    Publication date: September 11, 2014
    Inventors: Ryan Clark, Brian Andrew Stearns, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie M. Arruda
  • Publication number: 20140256740
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: September 11, 2014
    Applicant: Tempero Pharmaceuticals, Inc.
    Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt
  • Publication number: 20140256745
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 11, 2014
    Applicant: CalciMedica, Inc.
    Inventors: Jianguo Cao, Jeffrey P. Whitten, Zhijun Wang, Evan Rogers, Jonathan Grey
  • Publication number: 20140256728
    Abstract: The present invention relates to the use of predominantly known pyridyl carboxamide derivatives as nematicides, compositions containing such compounds and methods for the control of nematodes.
    Type: Application
    Filed: October 29, 2012
    Publication date: September 11, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jörg Nico Greul, Heiko Rieck, Christian Paulitz, Matthias Riedrich, Ralf Dunkel, Arianna Martelletti, Alexander Sudau, Peter Lösel, Olga Malsam, Arnd Voerste, Hans-Georg Schwarz, Ulrich Görgens, Kerstin Ilg, Michael Maue, Pierre-Yves Coqueron, Philippe Desbordes, Philippe Meresse, Stephanie Gary, Pierre Cristau, David Bernier