1,2-oxazoles (including Hydrogenated) Patents (Class 514/378)
Polycyclo ring system having the oxazole ring as one of the cyclos (Class 514/379)
Chalcogen or nitrogen bonded directly to ring carbon of the oxazole ring (Class 514/380)
  • INSECTICIDAL COMPOUNDS
    Publication number: 20130245072
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, A5, G1, R1, R2, R3 and R4 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 them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: May 10, 2013
    Publication date: September 19, 2013
    Applicant: SYNGENTA CORP PROTECTION LLC
    Inventors: Peter Renold, Jerome Yves Cassayre, Jagadish Pabba, Myriem El Qacemi, Thomas Pitterna
  • AGONISTS OF GPR40
    Publication number: 20130237571
    Abstract: The present invention relates to compounds that have the ability to modulate the activity of GPR40 and are therefore useful in the treatment of GPR40 related disorders. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders related to GPR40 activity.
    Type: Application
    Filed: July 20, 2011
    Publication date: September 12, 2013
    Applicant: Conexios Life Sciences PVT. LTD.
    Inventors: Jagannath Madanahalli Ranganath Rao, Nagarajan Arumugam, Mohd Mudabbir Ansari, Chandrasekhas Gudla, Shanmugam Pachiyappan, Manivannan Ramalingam, Jenson George, George Fernanda Arul, Kenchegowda Bommegowda, Y, Sathesh Kumar Angupillai, Ramamoorthy Kottamalai, Pradeep Jidugu, Shivanageshwara Rao, D
  • COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    Publication number: 20130237531
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: April 19, 2013
    Publication date: September 12, 2013
    Inventors: Guoxian Wu, Jiazhong Zhang, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, James Tsai
  • 1, 2-disubstituted amido-anthraquinone derivatives, preparation method and application thereof
    Patent number: 8530465
    Abstract: The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.
    Type: Grant
    Filed: August 1, 2012
    Date of Patent: September 10, 2013
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Chia-Chung Lee
  • Azetidine derivatives
    Patent number: 8530461
    Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 10, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Bernd Nosse, Martin Fleck, Niklas Heine, Gerald Juergen Roth
  • COMPOUNDS, COMPOSITIONS, PROCESSES OF MAKING, AND METHODS OF USE RELATED TO INHIBITING MACROPHAGE MIGRATION INHIBITORY FACTOR
    Publication number: 20130225586
    Abstract: The present invention provides a compound having Formula I or II: wherein B, R, X, Ar, and Y are defined herein, pharmaceutically acceptable salts thereof and pharmaceutically acceptable prodrugs thereof. The present invention also provides methods of making and using the compound.
    Type: Application
    Filed: September 25, 2012
    Publication date: August 29, 2013
    Applicant: CPSI STOCKHOLDER TRUST
    Inventor: CPSI Stockholder Trust
  • Naphthalene Isoxazoline Invertebrate Pest Control Agents
    Publication number: 20130217736
    Abstract: Disclosed are compounds of Formula 1, wherein R1 is halogen, C1-C2 haloalkyl or C1-C2 haloalkoxy; R2 is H, halogen or cyano; R3 is H, halogen or CF3; R4 is H, C2-C7 alkylcarbonyl or C2-C7 alkoxycarbonyl; and R5 is C1-C6 alkyl or C1-C6 haloalkyl, each substituted with one substituent independently selected from hydroxy, C1-C6 alkoxy, C1-C6 alkylthio, C1-C6 alkylsulfinyl, C1-C6 alkylsulfonyl, C2-C7 alkylaminocarbonyl, C3-C9 dialkylaminocarbonyl, C2-C7 haloalkylaminocarbonyl and C3-C9 halodialkylaminocarbonyl. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 22, 2013
    Inventor: E. I. Du Pont de Nemours and Company
  • Use of Malononitrilamides in Neuropathic Pain
    Publication number: 20130217737
    Abstract: Provided herein are compounds and pharmaceutical compositions for use in the treatment of neuropathic pain and the neuropathic pain syndromes.
    Type: Application
    Filed: October 28, 2011
    Publication date: August 22, 2013
    Applicant: AL-GIAX PHARMACEUTICALS GMBH
    Inventors: Birgit Hasse, Guido Koopmans
  • PARASITICIDAL DIHYDROISOXAZOLE COMPOUNDS
    Publication number: 20130217699
    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: May 8, 2012
    Publication date: August 22, 2013
    Applicant: 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
  • PESTICIDAL MIXTURES INCLUDING ISOXAZOLINE DERIVATIVES
    Publication number: 20130210623
    Abstract: The present invention provides pesticidal mixtures comprising a component A and a component B, wherein component A is an enantiomeric mixture of a compound of formula I that is enantiomerically enriched for the S enantiomer (Formula I) wherein the symbol * indicates the chiral centre; wherein A1, A2, R1, R2, R4, R5, R6 and p are as defined in claim 1, and component B is a compound as defined in claim 1. The present invention also relates to methods of using said mixtures for the control of plant pests.
    Type: Application
    Filed: June 8, 2011
    Publication date: August 15, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Jerome Yves Cassayre, Elvira Molitor
  • N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
    Patent number: 8507541
    Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: August 13, 2013
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Brian M. Glass, Richard B. Sparks, Eddy Wai Tsun Yue
  • Isoxazole compounds as inhibitors of heat shock proteins
    Patent number: 8507480
    Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, —SO.sub.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: August 13, 2013
    Assignees: Vernalis (R&D) Limited, Cancer Research Technology Limited, The Institute of Cancer Research
    Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
  • PARASITICIDAL ORAL VETERINARY COMPOSITIONS COMPRISING SYSTEMICALLY-ACTING ACTIVE AGENTS, METHODS AND USES THEREOF
    Publication number: 20130203692
    Abstract: This invention relates to oral veterinary compositions for combating ectoparasites and endoparasites in animals, comprising at least one systemically-acting active agent in combination with a pharmaceutically acceptable carrier. This invention also provides for improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the compositions of the invention to the animal in need thereof.
    Type: Application
    Filed: January 31, 2013
    Publication date: August 8, 2013
    Applicant: MERIAL LIMITED
    Inventors: Mark David Soll, Diane Larsen, Susan Mancini Cady, Peter Cheifetz, Izabela Galeska
  • PESTICIDAL MIXTURES INCLUDING ISOXAZOLINE DERIVATIVES
    Publication number: 20130203591
    Abstract: The present invention provides pesticidal mixtures comprising a component A and a component B, wherein component A is an enantiomeric mixture of a compound of formula (I) that is enantiomerically enriched for the S enantiomer wherein the symbol * indicates the chiral centre; wherein A1, A2, R1, R2, R4, R5, R6 and p are as defined in claim 1, and component B is a fungicide as defined in claim 1. The present invention also relates to methods of using said mixtures for the control of plant pests.
    Type: Application
    Filed: June 8, 2011
    Publication date: August 8, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Jerome Yves Cassayre, Elvira Molitor
  • ACYLSULFONAMIDES AND PROCESSES FOR PRODUCING THE SAME
    Publication number: 20130203709
    Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.
    Type: Application
    Filed: August 9, 2011
    Publication date: August 8, 2013
    Applicants: THE PENN STATE RESEARCH FOUNDATION, UNIVERSITY OF SOUTH FLORIDA
    Inventors: Roman Manetsch, Sameer Kulkarni, Iredia D. Iyamu, Hong-Gang Wang, Kenichiro Doi, Wayne Guida, Daniel Santiago, Courtney du Boulay
  • PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
    Publication number: 20130203593
    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: January 23, 2013
    Publication date: August 8, 2013
    Applicant: Dow AgroSciences LLC
    Inventor: Dow AgroSciences LLC
  • PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
    Publication number: 20130203592
    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: January 22, 2013
    Publication date: August 8, 2013
    Applicant: Dow AgroSciences LLC
    Inventor: Dow AgroSciences LLC
  • Thiazole and oxazole-substituted arylamides as P2Xand P2Xantagonists
    Patent number: 8501933
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.
    Type: Grant
    Filed: July 26, 2010
    Date of Patent: August 6, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament
    Publication number: 20130197011
    Abstract: Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders.
    Type: Application
    Filed: July 27, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Riccardo GIOVANNINI, Barbara BERTANI, Marco FERRARA, Iain LINGARD, Rocco MAZZAFERRO, Holger ROSENBROCK
  • USE OF ISOXAZOLINE COMPOUNDS AND COMPOSITIONS IN BLADDER CANCER
    Publication number: 20130196996
    Abstract: One embodiment provides a method, comprising treating or preventing at least one disease selected from the group consisting of bladder cancer, weight loss accompanying bladder cancer, bone pain accompanying bladder cancer, bladder cancer carcinoma in-situ (CIS), TA stage bladder cancer, T1 stage bladder cancer, T2 stage bladder cancer, T3 stage bladder cancer, T4 stage bladder cancer, lymph node metastasis therefrom, solid organ metastasis therefrom, bony metastasis therefrom, cachexia/anorexia associated with bladder cancer, generalized wasting syndrome associated with bladder cancer, or a combination thereof, by administering to a subject in need thereof one or more compounds described herein, prodrug thereof, salt thereof, or a combination thereof.
    Type: Application
    Filed: January 19, 2011
    Publication date: August 1, 2013
    Applicant: CPSI STOCKHOLDER TRUST
    Inventors: John Arthur Taylor, III, Thais Sielecki-Dzurdz
  • Crystalline pyrimidine nucleoside derivative suspensions in capsules
    Patent number: 8497291
    Abstract: The present invention relates to a pharmaceutical formulation which comprises (i) a capsule, and (ii) a core comprising crystalline 2?-cyano-2?-deoxy-N4-palmitoyl-1-?-D-arabinofuranosylcytosine and a liquid carrier.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: July 30, 2013
    Assignee: Cyclacel Limited
    Inventors: Robert Westwood, Alistair Selkirk
  • Pyrrolinone derivative and pharmaceutical composition comprising the same
    Patent number: 8497263
    Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: July 30, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroyuki Kai, Shunji Shinohara, Takayuki Kameyama
  • DUAL INHIBITORS OF FARNESYLTRANSFERASE AND GERANYLGERANYLTRANSFERASE I
    Publication number: 20130190355
    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: Application
    Filed: March 11, 2013
    Publication date: July 25, 2013
    Applicants: Yale University, H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: H. Lee Moffitt Cancer Center and Research Institute, Inc., Yale University
  • MODIFIED MACROPHAGE MIGRATION INHIBITORY FACTOR INHIBITORS
    Publication number: 20130190369
    Abstract: Provided are various compounds of Formula I (I). Also provided are various compounds of Formula II (II). Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.
    Type: Application
    Filed: January 28, 2013
    Publication date: July 25, 2013
    Applicant: The Feinstein Institute for Medical Research
    Inventor: Yousef Al-Abed
  • BENZYL SULFONAMIDE DERIVATIVES AS RORC MODULATORS
    Publication number: 20130190356
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 25, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genetech, Inc.
  • Compounds as cannabinoid receptor ligands
    Patent number: 8492371
    Abstract: Disclosed herein are compounds of formula (I) wherein Ring A and R1 are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and pharmaceutical compositions are also disclosed.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: July 23, 2013
    Assignee: AbbVie Inc.
    Inventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Steven P. Latshaw, Tongmei Li, Bo Liu, Sridhar Peddi, Xueqing Wang, Teodozyj Kolasa, Derek W. Nelson, Arturo Perez-Medrano
  • 2-aminoimidazole beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 8492387
    Abstract: The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: February 18, 2009
    Date of Patent: July 23, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Ivory D. Hills, Craig A. Coburn, Samuel L. Graham, Keith P. Moore, Philippe G. Nantermet, Hemaka A. Rajapakse, Shawn J. Stachel, Hong Zhu
  • Hepatitis C Virus Inhibitors
    Publication number: 20130183269
    Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
    Type: Application
    Filed: January 7, 2013
    Publication date: July 18, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • N-((3-BENZYL)-2,2-(BIS-PHENYL)-PROPAN-1-AMINE DERIVATIVES AS CETP INHIBITORS FOR THE TREATMENT OF ATHEROSCLEROSIS AND CARDIOVASCULAR DISEASES
    Publication number: 20130184279
    Abstract: Compounds of formula Ia and Ib wherein A, B, C, R1 and R14 are described herein.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 18, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • SULFONYL COMPOUNDS WHICH MODULATE THE CB2 RECEPTOR
    Publication number: 20130184315
    Abstract: Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: July 18, 2011
    Publication date: July 18, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbH
    Inventors: Eugene Richard Hickey, Doris Riether, Monika Ermann
  • ISOXAZOLE TREATMENTS FOR DIABETES
    Publication number: 20130178506
    Abstract: The present invention relates to compounds and methods for inducing synthesis and secretion of insulin from pancreatic beta cells. The methods may take place in vitro, ex vivo such as in isolates from adult mammalian tissue, or in vivo. Compounds and methods described herein may find use in the treatment of diabetes.
    Type: Application
    Filed: November 21, 2012
    Publication date: July 11, 2013
    Applicant: The Board of Regents of the University of Texas System
    Inventor: The Board of Regents of the University of Texas S
  • SULFONAMIDE COMPOUNDS
    Publication number: 20130172339
    Abstract: A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.
    Type: Application
    Filed: September 19, 2011
    Publication date: July 4, 2013
    Applicant: KANCERA AB
    Inventors: Styrbjorn Bystrom, Charles Hedgecock, Evert Homan, Thomas Lundback, Jessica Martinsson, Meral Sari, Katarina Farnegardh, Mattias Jonsson
  • INSECTICIDAL COMPOUNDS
    Publication number: 20130165490
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, G2, R1, R2, R3 and R4 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 them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: February 21, 2013
    Publication date: June 27, 2013
    Applicants: Syngenta Crop Protection LLC
    Inventors: Myriem El Qacemi, Thomas Pitterna, Jerome Yves Cassayre, Peter Renold
  • BIPHENYL AND PHENYL-PYRIDINE AMIDES AS P2X3 AND P2X2/3 ANTAGONISTS
    Publication number: 20130165443
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Application
    Filed: August 23, 2012
    Publication date: June 27, 2013
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • INSECTICIDAL COMPOUNDS
    Publication number: 20130165485
    Abstract: A compound of formula (I): where A, B, C, G, m, n, o, p, R1, R2, R3, R4, R5, R6, X, R7, R8, R9, R10 and R11 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: Application
    Filed: February 20, 2013
    Publication date: June 27, 2013
    Applicant: Syngenta Crop Protection LLC
    Inventors: Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik, Myriem El Qacemi, Anne Jacqueline Dalencon, Werner Zambach, Christopher Richard Godfrey, Thomas Pitterna, Pierre Joseph Jung, Jagadish Pabba
  • Heteroaryl Nitrile Compounds Useful as Inhibitors of Cathepsin-S
    Publication number: 20130158018
    Abstract: Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same.
    Type: Application
    Filed: March 2, 2011
    Publication date: June 20, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Michael J. Burke, Derek Cogan, Donghong Amy Gao, Alexander Heim-Riether, Eugene Richard Hickey, Matthew Russell Netherton, Philip Dean Ramsden, David Charles Thompson, Zhaoming Xiong
  • 6-substituted sulfonyl azabicyclo[3.2.1]octanes useful to inhibit 11?-hydroxysteroid dehydrogenase type-I
    Patent number: 8466149
    Abstract: In its many embodiments, the present invention relates to a novel class of 6-substituted sulfonyl-1,3,3-trialkyl-6-azabicyclo[3.2.1]octane compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: June 18, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Claire M. Lankin
  • Small molecule inhibitors of kynurenine-3-monooxygenase
    Patent number: 8466182
    Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: June 18, 2013
    Assignees: The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone, University of Maryland, Baltimore
    Inventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
  • Compounds and methods for inhibiting the interaction of BCL proteins with binding partners
    Patent number: 8461191
    Abstract: One aspect of the present invention relates to heterocyclic compounds that bind to bcl proteins and inhibit Bcl function. Another aspect of the present invention relates to compositions comprising a heterocyclic compound of the invention. The present invention provides methods for treating and modulating disorders associated with hyperproliferation, such as cancer.
    Type: Grant
    Filed: November 30, 2010
    Date of Patent: June 11, 2013
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Edward B. Holson, Brian T. Hopkins, Nii O. Koney, Daniel A. Snyder, Thomas T. Tibbitts
  • STEM CELL DIFFERENTIATING AGENTS AND USES THEREFOR
    Publication number: 20130143935
    Abstract: The present invention relates to screens for compounds that can induce stem cell differentiation. In addition, isoxazoles and sulfonyl hydrazones are identified as general classes of compounds that can induce differentiation of stem cells into cells of neuronal and cardiac fate, respectively.
    Type: Application
    Filed: November 12, 2012
    Publication date: June 6, 2013
    Applicant: The Board of Regents of the University of Texas System
    Inventor: The Board of Regents of the University of Texas
  • CHEMICAL INDUCERS OF NEUROGENESIS
    Publication number: 20130143885
    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: Application
    Filed: June 4, 2012
    Publication date: June 6, 2013
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Jay Schneider, Jenny Hsieh, Douglas Frantz, Steven L. McKnight, Joseph M. Ready
  • POSITIVE ALLOSTERIC MODULATORS OF MGLUR2
    Publication number: 20130143880
    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: Application
    Filed: August 5, 2011
    Publication date: June 6, 2013
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • 3-hydroxy-5-arylisoxazole derivative
    Patent number: 8455500
    Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is a specific cyclic group; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is —CH2—, O, —S(O)i— (i is 0 to 2), or —NR7—; R1 to R6 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: June 4, 2013
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventors: Akihiro Okano, Munetaka Ohkouchi
  • Inhibitors of aspartyl protease
    Patent number: 8455497
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: June 4, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
  • CRYSTALLINE FORM OF 4- [5 - [3 -CHLORO-5 - (TRIFLUOROMETHYL) PHENYL] -4, 5 - DIHYDRO - 5 - (TRIFLUOROMETHYL) -3 - ISOXAZOLYL] -N- [2-0X0-2- [ ( 2, 2, 2 - TRIFLUOROETHYL) AMINO] ETHYL] -1- NAPH-THALENECARBOXAMIDE
    Publication number: 20130137735
    Abstract: Disclosed is a solid form of 4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-1-naphthalenecarboxamide (Compound 1). Also disclosed are compositions containing a solid form of Compound 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a solid form of Compound 1 or a composition containing a solid form of Compound 1.
    Type: Application
    Filed: May 19, 2011
    Publication date: May 30, 2013
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventor: Martin James Currie
  • Isoxazole compounds as inhibitors of heat shock proteins
    Patent number: 8450310
    Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: May 28, 2013
    Assignees: Vernalis (R&D) Limited, Cancer Research Technology Ltd., The Institute of Cancer Research
    Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
  • PEST CONTROL COMPOSITION
    Publication number: 20130131083
    Abstract: A pest control composition comprising a hydrazide compound shown by formula (1) below (in the formula, G, M, Q1, Q2, Q3, Q4, R2, R4, R5, R6 and m have the same meanings described in the specification) and a pyrazole compound shown by formula (2) below (in the formula, X10, X20 and X30 have the same meanings described in the specification) and a method for controlling pests whereby an effective dose of the hydrazide compound represented by formula (1) and the pyrazole compound represented by formula (II) is applied to a pest or a pest habitat.
    Type: Application
    Filed: July 25, 2011
    Publication date: May 23, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Kaori Ikari
  • PEST CONTROL COMPOSITION
    Publication number: 20130131118
    Abstract: A pest control composition comprising a hydrazide compound shown by formula (1) below (in the formula, G, M, Q1, Q2, Q3, Q4, R2, R4, R5, R6 and m have the same meanings described in the specification) and an ester compound shown by formula (2) below (in the formula, X10, X20 and X30 have the same meanings described in the specification) and a method for controlling pests whereby an effective dose of the hydrazide compound represented by formula (1) and the ester compound represented by formula (II) is applied to a pest or a pest habitat.
    Type: Application
    Filed: July 25, 2011
    Publication date: May 23, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Kaori Ikari
  • Compounds and Methods for Inhibiting the Interaction of BCL Proteins with Binding Partners
    Publication number: 20130131063
    Abstract: The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.
    Type: Application
    Filed: May 15, 2012
    Publication date: May 23, 2013
    Applicant: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Kristopher M. Depew, Michael J. Grogan, Charles W. Johannes, Edward B. Holson, Brian T. Hopkins, Gregg F. Keaney, Nii O. Koney, Tao Liu, David A. Mann, Marta Nevalainen, Stephane Peluso, Lawrence Blas Perez, Daniel A. Snyder, Thomas T. Tibbitts
  • PEST CONTROL COMPOSITION
    Publication number: 20130131117
    Abstract: A pest control composition comprising a hydrazide compound shown by formula (1) below (in the formula, G, M, Q1, Q2, Q3, Q4, R2, R4, R5, R6 and m have the same meanings described in the specification) and dinotefuran, and a method for controlling pests whereby an effective dose of the hydrazide compound represented by formula (1) and dinotefuran is applied to a pest or a pest habitat.
    Type: Application
    Filed: July 25, 2011
    Publication date: May 23, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Kaori Ikari