Ring Nitrogen In The Additional Hetero Ring (e.g., Oxazole, Etc.) Patents (Class 514/340)
  • Patent number: 8796467
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: August 5, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer, Bernd Wellenzohn
  • 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: 20140213589
    Abstract: The invention relates to hydroxyphenyl derivatives of formula (I); and uses thereof as anti-bacterial and/or anti-parasitic agents.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 31, 2014
    Applicant: FAB PHARMA S.A.S.
    Inventors: Alexis DENIS, Vincent Gerusz, Yannick Bonvin
  • Publication number: 20140213616
    Abstract: The invention relates to pyridone amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium 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, including pain.
    Type: Application
    Filed: January 29, 2014
    Publication date: July 31, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
  • Publication number: 20140213594
    Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: April 1, 2014
    Publication date: July 31, 2014
    Applicant: NOVARTIS AG
    Inventors: Urs BAETTIG, Anne-Marie D'SOUZA, Peter HUNT, Neil John PRESS, Simon James WATSON
  • Patent number: 8791142
    Abstract: The present invention provides oxadiazole pyridine derivatives of Formula (I), their use as medicaments and their use for treating multiple sclerosis and other diseases.
    Type: Grant
    Filed: March 2, 2010
    Date of Patent: July 29, 2014
    Assignee: Merck Serono S.A.
    Inventors: Anna Quattropani, Patrick Gerber, Jerome Dorbais
  • Patent number: 8791091
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: July 29, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Huji Turdi, Jon J. Hangeland, R. Michael Lawrence, Saleem Ahmad, Wei Meng, Robert Paul Brigance, Pratik Devasthale, Guohua Zhao
  • Patent number: 8791100
    Abstract: The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: July 29, 2014
    Assignee: Novartis AG
    Inventors: Daniela Angst, Birgit Bollbuck, Philipp Janser, Jean Quancard, Nikolaus Johannes Stiefl
  • Publication number: 20140206726
    Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.
    Type: Application
    Filed: August 21, 2012
    Publication date: July 24, 2014
    Inventors: Juergen Benting, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Ulrike Wachendorff-Neumann
  • Publication number: 20140206647
    Abstract: There is disclosed pyridine- and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine- and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.
    Type: Application
    Filed: March 26, 2014
    Publication date: July 24, 2014
    Applicant: SYNTRIX BIOSYSTEMS, INC.
    Inventors: Dean Y. Maeda, John A. Zebala
  • Publication number: 20140206701
    Abstract: The invention provides well-defined heterocyclic compounds that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptor.
    Type: Application
    Filed: March 20, 2014
    Publication date: July 24, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, KEN CHOW, TODD M. HEIDELBAUGH, SANTOSH C. SINHA, PHONG X. NGUYEN, SMITA S. BHAT, WENKUI K. FANG
  • Publication number: 20140206606
    Abstract: The present invention provides compounds of formula (I), wherein G1 is oxygen; R1 is hydrogen; R2 is group P (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y1 is C—R6, CH or nitrogen; Y2 and Y3 are independently CH or nitrogen; wherein no more than two of Y1, Y2 and Y3 are nitrogen and wherein Y2 and Y3 are not both nitrogen; R5 is hydrogen, halogen, cyano, nitro, NH2, C1-C2alkyl, C1-C2haloalkyl, C3-C5cycloalkyl, C3-C5halocycloalkyl, C1-C2alkoxy, C1-C2haloalkoxy; R6 together with R5 forms a —CH?CH—CH?CH— bridge; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl.
    Type: Application
    Filed: August 24, 2012
    Publication date: July 24, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Publication number: 20140206690
    Abstract: The present invention relates to compound (I) wherein R1 and R2 independently represent a hydrogen atom, a (C1-C4)alkoxy group, a fluoro(C1-C4)alkoxy group, a hydroxyl group, a benzyloxy group, a di(C1-C4)alkylamino group, a pyridyl-vinyl group, a pyrimidinyl-vinyl group, a styryl group, or a —NHCOphenyl group; R3, R4 and R5 independently represent a hydrogen atom, a (C1-C4)alkyl group, a CONHR6 group, a —CONR7R8 group, a —SO2NHR6 group, or a heteroaryl group optionally substituted by a halogen atom, a —(CH2)nNR7R8 group or a hydroxy(C1-C4)alkyl group; R6 represents a hydrogen atom, a —(CHR9)m(CH2)nNR7R8 group or a (C1-C6)alkyl group optionally substituted by a hydroxyl group; or anyone of its pharmaceutically acceptable salt, for use in a method for preventing, inhibiting or treating a disease in a patient suffering thereof, said disease involving a deregulated p53. Some of said compounds are new and also form part of the invention.
    Type: Application
    Filed: April 2, 2012
    Publication date: July 24, 2014
    Applicants: SOCIETE SPLICOS, UNIVERSITE DE MONTPELLIER 2, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Didier Scherrer, Jamal Tazi, Romain Najman, Florence Mahuteau, Pierre Roux
  • Patent number: 8785440
    Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: July 22, 2014
    Assignees: Biogen Idec MA, Inc., Sunesis Pharmaceuticals, Inc.
    Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
  • Patent number: 8785442
    Abstract: The present invention relates to a compound as antagonist of LPA receptor, and a pharmaceutical composition comprising the same. The present invention also relates to the use of the compound and the composition, and a method of using the compound to treat, prevent or diagnose diseases, disorders or conditions associated with one or more of the LPA receptors.
    Type: Grant
    Filed: January 30, 2011
    Date of Patent: July 22, 2014
    Assignee: Curegenix, Inc.
    Inventors: Songzhu An, Chufang Li, Guisheng Zhou, Chen Huang
  • Publication number: 20140200134
    Abstract: The present invention relates to anthranilamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the anthranilamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: July 17, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Prashant Deshmukh, Karsten Koerber, Wolfgang Von Deyn, Markus Kordes, Joachim Dickhaut, Arun Narine, Nina Gertrud Bandur, Gemma Veitch, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
  • Patent number: 8778974
    Abstract: The present invention relates to 1-aryl-3-aniline-5-alkyl-1,2,4-triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to potent positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: July 15, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gregor James MacDonald, Johannes Wilhelmus John F. Thuring, Pauline Carol Stanislawski, Wei Zhuang, Yves Emiel Maria Van Roosbroeck, Frans Alfons Maria Van Den Keybus
  • Patent number: 8778940
    Abstract: The present invention relates to compounds and methods for inducing neuronal differentiation in normal neural stem cells and brain cancer stem cells. The methods may take place in vitro, such as in isolates from the adult mammalian brain, or in vivo. Compounds and methods described herein may find use in the treatment of neurodegenerative and psychiatric diseases, the repair and regeneration of the nervous system, and in treatment of neurologic malignancy.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: July 15, 2014
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Jay Schneider, Jenny Hsieh, Douglas Frantz, Steven L. McKnight, Joseph M. Ready
  • Publication number: 20140194426
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: October 24, 2013
    Publication date: July 10, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Paul R. Fatheree, Ryan Hudson, Robert Murray McKinnell
  • Publication number: 20140194376
    Abstract: The present invention provides compounds of formula (I) wherein G1 is oxygen; R1 is hydrogen; R2 is group (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—; R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y2 and Y3 are independently CH or nitrogen, wherein Y2 and Y3 are not both nitrogen; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl. The invention also provides intermediates useful for the preparation of compounds of formula (I), as well as methods of controlling insects, acarines, nematodes or molluscs using the compounds of formula (I).
    Type: Application
    Filed: August 24, 2012
    Publication date: July 10, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Publication number: 20140194436
    Abstract: The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Application
    Filed: February 24, 2014
    Publication date: July 10, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
  • Patent number: 8771665
    Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: July 8, 2014
    Assignee: Cocrystal Discovery, Inc.
    Inventors: Sam S K Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
  • Publication number: 20140187586
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, X1, X2, Z, R3, R4, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 3, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Zhiqiang Xia, Junyi Zhang, Gary Bohnert, Shoujun Chen, Yu Xie
  • Publication number: 20140187527
    Abstract: The present disclosure provides a novel class of macrocyclic compounds and their metal complexes formed with transition metal ion, lanthanide metal ions and other metal ions (e.g., Al, Ga, Y, In, Sn, Tl, Pb and Bi) and their applications in the fields of contrast agents, artificial nucleases, fluorescence probes, nuclear medicines and other biomedical applications in the therapeutics or diagnostics.
    Type: Application
    Filed: December 31, 2012
    Publication date: July 3, 2014
    Applicant: NATIONAL YANG MING UNIVERSITY
    Inventors: Cheng Allen Chang, Ren-Shyan Liu, Bhalchandra Vishnu Bhagwat
  • Patent number: 8765739
    Abstract: Compounds of formula [I]: wherein each symbol is as defined in the description, or a pharmaceutically acceptable salts or solvates thereof.
    Type: Grant
    Filed: May 14, 2010
    Date of Patent: July 1, 2014
    Assignee: Japan Tobacco Inc.
    Inventors: Kazutaka Ikegashira, Taku Ikenogami, Naoki Ogawa, Tatsuya Matsumoto, Takahiro Oka, Takuya Matsuo, Takayuki Yamasaki
  • Publication number: 20140179648
    Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 26, 2014
    Applicant: RVX Therapeutics Inc.
    Inventors: Shuang Liu, Bryan Cordell Duffy, John Frederick Quinn, May Xiaowu Jiang, Ruifang Wang, Gregory Scott Martin, He Zhao, Bruce Francis Molino, Peter Ronald Young
  • Publication number: 20140179699
    Abstract: The present invention relates to compounds useful as inhibitors of indoleamine 2,3-dioxygenase (IDO). 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. The compounds of this invention have formula I-A: wherein the variables are as defined herein.
    Type: Application
    Filed: November 19, 2013
    Publication date: June 26, 2014
    Inventors: Dean Boyall, Christopher Davis, James Dodd, Simon Everitt, Andrew Miller, Peter Weber, James Westcott, Stephen Young
  • Publication number: 20140171437
    Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 19, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Harry Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo
  • Publication number: 20140171315
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Patent number: 8754053
    Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 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 17, 2011
    Date of Patent: June 17, 2014
    Assignee: Syngenta Crop Protection LLC
    Inventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
  • Patent number: 8754227
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: July 30, 2012
    Date of Patent: June 17, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
  • Publication number: 20140162981
    Abstract: The present application relates to novel substituted aryloxazole derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders.
    Type: Application
    Filed: May 14, 2013
    Publication date: June 12, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Peter NELL, Walter HÜBSCH, Barbara ALBRECHT-KÜPPER, Jorg KELDENICH, Alexandros VAKALOPOULOS, Frank SÜSSMEIER, Katja ZIMMERMANN, Dieter LANG, Daniel MEIBOM
  • Patent number: 8748470
    Abstract: The present invention concerns methods and compositions for the inhibition or reduction of the primary tumor and metastasis by inhibition of fatty acid binding proteins.
    Type: Grant
    Filed: March 16, 2012
    Date of Patent: June 10, 2014
    Assignee: The University of Chicago
    Inventors: Ernst Lengyel, Kristin Nieman, Hilary Kenny
  • Patent number: 8748461
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: June 10, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger, Gary D. Gustafson
  • Patent number: 8748340
    Abstract: This document discloses pesticidal compostions comprising molecules having the following formulas: and processes related thereto.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: June 10, 2014
    Assignee: Dow AgroSciecnes LLC.
    Inventors: Gary D. Crouse, William Thomas Lambert, Thomas C. Sparks, Vidyadhar B. Hegde
  • Patent number: 8748412
    Abstract: Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.
    Type: Grant
    Filed: February 2, 2011
    Date of Patent: June 10, 2014
    Assignee: Argusina Bioscience Inc.
    Inventors: Jiayu Liao, Yufeng Hong, Yong Wang, Thomas W. Von Geldern, Kanyin E. Zhang
  • 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
  • Publication number: 20140155370
    Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).
    Type: Application
    Filed: June 28, 2013
    Publication date: June 5, 2014
    Inventors: Sharon Shacham, Michael Kauffman, Vincent P. Sandanayaka, Sharon Shechter
  • Publication number: 20140155436
    Abstract: The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.
    Type: Application
    Filed: November 4, 2013
    Publication date: June 5, 2014
    Applicants: CENTRE NATIONAL DE RECHERCHE SCIENTIFIQUE, UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUES, INSTITUT CURIE
    Inventors: Jamal TAZI, David GRIERSON, Florence MAHUTEAU-BETZER, Pierre ROUX
  • Patent number: 8742118
    Abstract: Methods for the synthesis of 2-alkoxy-5-(pyridin-2-yl)pyridine of formula I or salts thereof are provided.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: June 3, 2014
    Assignee: F.I.S.—Fabbrica Italiana Sintetici S.p.A.
    Inventors: Francesco Fontana, Paolo Stabile
  • Patent number: 8742119
    Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: June 3, 2014
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • Publication number: 20140148340
    Abstract: Pesticidal compositions and their uses are disclosed.
    Type: Application
    Filed: January 31, 2014
    Publication date: May 29, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: Annette V. Brown, Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, Emily M. Rigsbee, William T. Lambert, Noormohamed M. Niyaz
  • Publication number: 20140148453
    Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: July 25, 2011
    Publication date: May 29, 2014
    Inventors: Joel Francis Austin, Lisa S. Sharma, James Aaron Balog, Audris Huang, Upender Velaparthi, Chetan Padmakar Darne, Mark George Saulnier
  • Patent number: 8735432
    Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Y and W are as defined herein. The invention also concerns a method for preparing said compounds and their therapeutic use.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventors: Laurent Dubois, Yannick Evanno, Andre Malanda
  • Patent number: 8735398
    Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.
    Type: Grant
    Filed: November 7, 2012
    Date of Patent: May 27, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
  • Patent number: 8735399
    Abstract: The invention provides oxazolidine and thiazolidine derivatives that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.
    Type: Grant
    Filed: January 14, 2009
    Date of Patent: May 27, 2014
    Assignee: Allergan, Inc.
    Inventors: Todd M. Heidelbaugh, Ken Chow, Santosh C. Sinha, Phong X. Nguyen, Wenkui K. Fang, Ling Li, Janet A. Takeuchi, Smita S. Bhat
  • Patent number: 8735362
    Abstract: The present invention relates to compounds of formula (I): Wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: May 27, 2014
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Publication number: 20140142085
    Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: July 5, 2012
    Publication date: May 22, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-hung Chou, Randall L. Halcomb, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • Publication number: 20140142143
    Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: October 24, 2013
    Publication date: May 22, 2014
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
  • Publication number: 20140142074
    Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
    Type: Application
    Filed: January 27, 2014
    Publication date: May 22, 2014
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Elisabetta ARMANI, Gabriele Amari, Carmelida Capaldi, Oriana Esposito, Ilaria Peretto