Plural Double Bonds Between Ring Members Of The Oxazole Ring Patents (Class 548/247)
  • Patent number: 10412986
    Abstract: The present invention relates to processes and intermediates for the preparation of compounds of formula (I): or a salt or oxide thereof wherein Alk, M1, M2, R1, R2, R3, R4, R5, R6, R7, and n are as described herein. The present invention also relates to compounds of formula (I) and composition comprising a compound of formula (I). Also disclosed is a method of altering or improving the taste of a composition that includes adding to the composition at least one compound of formula (I), in an amount effective to obtain a modified composition having altered or improved taste relative to an otherwise identical composition lacking said compound.
    Type: Grant
    Filed: April 9, 2018
    Date of Patent: September 17, 2019
    Assignee: SENOMYX, INC.
    Inventor: Joseph R. Fotsing
  • Patent number: 10246428
    Abstract: A method and compound includes mixing dichloroglyoxime with an alcohol containing an alkyne functional group in methanol to create a mixture; adding a salt compound and water to the mixture to create bis-isoxazole diol; and nitrating the bis-isoxazole diol to create 3,3?-bis-isoxazole-5,5?-bis-methylene dinitrate, which has the structural formula: The alcohol containing an alkyne functional group may include propargyl alcohol. The salt compound may include sodium bicarbonate. The method may include nitrating the bis-isoxazole diol with nitric acid. The nitric acid may include at least a concentration of 90% nitric acid in water. Alternatively, the method may include nitrating the bis-isoxazole diol with 100% nitric acid and acetic anhydride. The salt compound and the water may be added to the mixture over at least a six-hour period. The method may include mixing the mixture after adding the salt compound and the water for at least ten hours.
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: April 2, 2019
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: Jesse J. Sabatini, Gregory W. Drake, Leah A. Wingard, Eric C. Johnson
  • Patent number: 9845291
    Abstract: Described herein are compounds that are estrogen receptor modulators of Formula (I): and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein SERMF is a selective estrogen receptor modulator fragment and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: December 19, 2017
    Assignee: Genentech, Inc.
    Inventors: Jun Liang, Daniel Fred Ortwine, Xiaojing Wang, Steven P. Govek, Mehmet Kahraman, Johnny Y. Nagasawa, Nicholas D. Smith, Simon Charles Goodacre, Nicholas Charles Ray
  • Patent number: 9102684
    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: Grant
    Filed: March 26, 2014
    Date of Patent: August 11, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Harald Engelhardt, Davide Gianni, Andreas Mantoulidis, Christian Smethurst
  • Patent number: 9040534
    Abstract: The present invention is directed to a compound of Formula (I) and to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 26, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Jason C. Rech, Brad M. Savall
  • Publication number: 20150133400
    Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
    Type: Application
    Filed: September 15, 2014
    Publication date: May 14, 2015
    Inventors: Jiazhong Zhang, John Buell, Katrina Chan, Prabha N. Ibrahim, Jack Lin, Phuongly Pham, Songyuan Shi, Wayne Spevak, Guoxian Wu, Jeffrey Wu
  • Publication number: 20150105252
    Abstract: Disclosed is a method for controlling the growth of undesired vegetation comprising contacting the vegetation or its environment with a herbicidally effective amount of a compound of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein A, R1, Q and J are as defined in the disclosure. Also disclosed is a method wherein the compound of Formula 1 (i.e. in a herbicidally effective amount) is comprised in a herbicidal composition further comprising at least one component selected from the group consisting of surfactants, solid diluents and liquid diluents. Also disclosed are compound of Formula 1 (including all stereoisomers), including N-oxides and salts thereof, their use as herbicides wherein A, R1, Q and J are as defined in the disclosure.
    Type: Application
    Filed: October 15, 2014
    Publication date: April 16, 2015
    Inventor: THOMAS MARTIN STEVENSON
  • Publication number: 20150099696
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed to compounds suitable for the treatment of Disease conditions such as hyperlipidemia.
    Type: Application
    Filed: June 26, 2012
    Publication date: April 9, 2015
    Applicant: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pandya, Sairam V.V.M. Kalapatapu
  • Patent number: 8993779
    Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • Publication number: 20150087519
    Abstract: N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of formula I and their use as herbicides, The invention relates to N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of formula I and their use as herbicides. In said formula I, B represents N or CH, whereas R, R1, R2, R3, R4 and R5 represent groups such as hydrogen, halogen or organic groups such as alkyl or phenyl.
    Type: Application
    Filed: April 16, 2013
    Publication date: March 26, 2015
    Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Klaus Kreuz, Johannes Hutzler, Maciej Pasternak, Jens Lerchl, Richard Roger Evans
  • Patent number: 8969552
    Abstract: The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, —CH?N—, —CH?CH— or —N?CH—; A is CH2, O or S; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the physiologically tolerated acid addition salts
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: March 3, 2015
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry
  • Publication number: 20150051257
    Abstract: Sulphonamide derivatives of benzylamine of formula (I), wherein A represents phenyl unsubstituted or substituted; or 9- or 10-membered bicyclic group, linked to —(O)x—(CH2)y— through one of its aromatic carbon atoms, consisting of benzene ring fused with -membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein such bicyclic group is unsubstituted or substituted or with 5- or 6-membered non-aromatic heterocyclic ring having 1 or 2 O atoms, wherein heterocyclic ring is unsubstituted or substituted with one or more C1-C3-alkyls; D represents a group selected from: phenyl unsubstituted or substituted; naphthyl unsubstituted or substituted; thiophene unsubstituted or substituted; bicyclic group consisting of imidazolering fused with 5-membered non-aromatic carbocyclic ring; bicyclic group consisting of benzene ring fused with 5-membered heteroaromatic ring, having 1 or 2 heteroatoms independently selected from the group consisting of N, O and
    Type: Application
    Filed: March 20, 2013
    Publication date: February 19, 2015
    Applicant: ADAMED SP. ZO.O
    Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Tomasz Lysakowski, Maciej Pawlowski
  • 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
  • Publication number: 20150018399
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: August 5, 2014
    Publication date: January 15, 2015
    Inventors: SONGNIAN LIN, Fengqi Zhang, Emma R. Parmee, Sunita V. Dewnani
  • Patent number: 8927709
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: January 6, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • 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: 20140364398
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: PFIZER INC.
    Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
  • Publication number: 20140357628
    Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof, with the proviso that the compound is no Tranilast.
    Type: Application
    Filed: June 27, 2014
    Publication date: December 4, 2014
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
  • Patent number: 8901295
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Grant
    Filed: February 21, 2014
    Date of Patent: December 2, 2014
    Assignees: Institut National de la Sante et de la Recherche Medicale (INSERM), Universite Montpellier 1, Universite Paris-EST Creteil val de Marne, Assistance Publique-Hopitaux de Paris, Centre National de la Recherche Scientifique
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
  • Publication number: 20140342906
    Abstract: Tetrazol-5-yl- and triazol-5-yl-aryl compounds of the general formula (I) as herbicides are described. In this formula (I), X, Z, W and R are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. A and B are N and CY. Q is cyanoalkylcarbonyl or isoxazolyl.
    Type: Application
    Filed: January 10, 2013
    Publication date: November 20, 2014
    Inventors: Ralf Braun, Lothar Willms, Ines Heinemann, Isolde Haeuser-Hahn, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger
  • Publication number: 20140329989
    Abstract: The present invention relates to the preparation of compounds, in particular to the preparation of compounds of formula (I), which may be used with a compound of formula (VI), or a salt thereof as intermediates for the preparation of antifungal agents, preferably micafungin (MICA) or a salt thereof.
    Type: Application
    Filed: September 7, 2012
    Publication date: November 6, 2014
    Applicant: SANDOZ AG
    Inventors: Roland Barth, Kerstin Knepper, Hubert Sturm
  • Patent number: 8877759
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: September 4, 2012
    Date of Patent: November 4, 2014
    Assignee: Vertex Pharnaceuticals Incorporated
    Inventors: Jean-Damien Charrier, David Kay, Somhairle MacCormick, Pierre-Henri Storck, Joanne Pinder, Michael Edward O'Donnell, Ronald Marcellus Alphonsus Knegtel, Stephen Clinton Young, Philip Michael Reaper, Steven John Durrant, Heather Clare Twin, Christopher John Davis
  • Publication number: 20140323518
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 to R9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.
    Type: Application
    Filed: August 2, 2012
    Publication date: October 30, 2014
    Inventors: Aiping Cheng, Neeraj Garg, Lars Krüger, Joakim Löfstedt, Eva Koch, Konrad Koehler, Lars Hagberg, Daniel Nöteberg
  • Publication number: 20140315961
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
  • Publication number: 20140315881
    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: October 23, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir GHOSH, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Patent number: 8865744
    Abstract: Disclosed are (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.
    Type: Grant
    Filed: May 15, 2014
    Date of Patent: October 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Doris Riether, Florian Paul Christian Binder, Henri Doods, Stephan Georg Mueller, Janet Rachel Nicholson, Achim Sauer
  • Publication number: 20140309210
    Abstract: A compound of formula I: stereoisomers or a pharmaceutically acceptable salt thereof, wherein X, X1, X2, X3, R1, R2, R3, R4, R5 and R6 are described herein, compositions including the compounds and methods of making and using the compounds for the treatment of diseases.
    Type: Application
    Filed: February 12, 2014
    Publication date: October 16, 2014
    Applicant: Genentech, Inc.
    Inventors: Jason Burch, Richard A. Goldsmith, Daniel Fred Ortwine, Richard Pastor, Zhonghua Pei
  • Publication number: 20140308317
    Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.
    Type: Application
    Filed: December 9, 2013
    Publication date: October 16, 2014
    Applicant: CELLCEUTIX CORPORATION
    Inventors: Xiaodong Fan, Yongjiang Xu, Dahui Liu, Michael J. Costanzo
  • Publication number: 20140303121
    Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 9, 2014
    Inventors: Jiazhong Zhang, Wayne Spevak
  • 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
  • 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
  • Patent number: 8841308
    Abstract: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: September 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael O'Donnell, Joanne Pinder, Philip Michael Reaper
  • Publication number: 20140275539
    Abstract: Provided herein are stabilized radioiodinated and astatinated compounds, and to methods for their preparation.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Ground Fluor Pharmaceuticals, Inc.
    Inventor: Stephen G. DiMagno
  • 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: 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
  • Patent number: 8828992
    Abstract: Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.
    Type: Grant
    Filed: February 25, 2010
    Date of Patent: September 9, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Cheol-Hyoung Park, Hye-Kyung Min, Mi-Jung Lim, Ji-Won Lee, Jin-Yong Chung, Choon-Ho Ryu, Yeo-Jin Yoon, Mi-Kyung Ji, Joo-Young Park
  • Publication number: 20140243322
    Abstract: Described herein are compounds capable of modulating one or more biomolecules substantially simultaneously, e.g., modulating two or more binding domains (e.g., bromodomains) on a protein or on different proteins.
    Type: Application
    Filed: February 28, 2014
    Publication date: August 28, 2014
    Applicant: Coferon, Inc.
    Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
  • Publication number: 20140243362
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR? wherein R1 to R7 are as defined in claim 35.
    Type: Application
    Filed: September 25, 2012
    Publication date: August 28, 2014
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le
  • Publication number: 20140235446
    Abstract: The compounds of the formula (I) in which L represents a radical of the formula and A1, B1 and A2 and B2 are as defined in Claim 1, are suitable as herbicides for the control of harmful plants or as plant growth regulators. The compounds can be prepared by the process of Claim 12.
    Type: Application
    Filed: July 11, 2012
    Publication date: August 21, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Marc Mosrin, Harald Jakobi, Alfred Angermann, Elmar Gatzweiler, Isolde Häuser-Hahn, Ines Heinemann, Christopher Hugh Rosinger, Stefan Lehr, Stefan Schnatterer
  • Patent number: 8796271
    Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: August 5, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20140206651
    Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.
    Type: Application
    Filed: March 24, 2014
    Publication date: July 24, 2014
    Applicant: Pfizer Inc.
    Inventors: Matthew Frank Brown, Charles Francis Donovan, Edmund Lee Ellsworth, Denton Wade Hoyer, Timothy Allan Johnson, Manjinder Singh Lall, Chris Limberakis, Sean Timothy Murphy, Debra Ann Sherry, Clarke Bentley Taylor, Joseph Scott Warmus
  • Publication number: 20140206668
    Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.
    Type: Application
    Filed: March 25, 2014
    Publication date: July 24, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: Gary D. Crouse, Thomas C. Sparks, William H. Dent, III, CaSandra L. McLeod, Lawrence C. Creemer, David A. Demeter, Amanda E. Fritz, Lindsey G. Fischer, Erich W. Baum
  • Patent number: 8785489
    Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: July 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Bennett Farmer, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
  • Patent number: 8778983
    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: Grant
    Filed: September 29, 2010
    Date of Patent: July 15, 2014
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: Ryan Clark, Brian Andrew Stearns, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie M. Arruda, David Nathan Zalatan
  • Patent number: 8772296
    Abstract: Benzamide derivatives of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, and n are as defined herein.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: July 8, 2014
    Assignee: Amgen Inc.
    Inventors: Jay P. Powers, Michael Degraffenreid, Lisa Julian, Jacob Kaizerman, Dustin McMinn, Yosup Rew, Daqing Sun, Xuelei Yan, Zhulun Wang, Felix Gonzalez Lopez De Turiso
  • Publication number: 20140187592
    Abstract: The present invention provides a compound having excellent regulating action on blood lipid level. The present invention provides a compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, etc., wherein A represents a 5-membered nitrogen-containing aromatic heterocyclyl group; R1 represents COOH or the like; each R2 represents an alkyl or the like; each R3 represents an optionally substituted phenyl, an optionally substituted phenylalkyl, or the like; m represents 0, 1, 2, or 3; n represents 0 or 1; each of R4, R5, R6, and R7 represents H, an alkyl, or the like; and B represents an optionally substituted naphthyl, an optionally substituted aromatic heterocyclyl, or a group represented by the following formula (II) wherein each of B1 and B2 represents an optionally substituted phenyl or an optionally substituted aromatic heterocyclyl.
    Type: Application
    Filed: February 10, 2014
    Publication date: July 3, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Keiko Suzuki, Takahiro Yamaguchi, Akihiro Tamura, Tomohiro Nishizawa, Mitsuhiro Yamaguchi
  • Patent number: 8765812
    Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof; with the proviso that the compound is not Tranilast.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: July 1, 2014
    Assignee: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Willams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
  • Publication number: 20140179687
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Application
    Filed: February 21, 2014
    Publication date: June 26, 2014
    Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michael Pawlotsky
  • Patent number: 8748431
    Abstract: Compounds of the formula I Formula (I) wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.
    Type: Grant
    Filed: November 25, 2011
    Date of Patent: June 10, 2014
    Assignee: Syngenta Participations AG
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta, Fredrik Cederbaum, Guillaume Berthon
  • Patent number: 8748627
    Abstract: The present invention relates to compounds of formula (I), which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
    Type: Grant
    Filed: February 15, 2007
    Date of Patent: June 10, 2014
    Assignee: AbbVie Inc.
    Inventors: Yu Gui Gu, Moshe Weitzberg, Xiangdong Xu, Richard F. Clark, Tianyuan Zhang, Qun Li, Todd M. Hansen, Hing Sham, Bruce A. Beutel, Heidi S. Camp, Xiaojun Wang