The Additional Hetero Ring Contains Chalcogen As The Only Ring Hetero Atom Patents (Class 548/365.7)
  • Publication number: 20140162997
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, ring A, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: June 12, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Mark Wall, Nalin Subasinghe, Zhihua Sui, Christopher Flores
  • Publication number: 20140163031
    Abstract: The present invention relates to compounds of Formula (I), wherein X1, X2, X3, X4, R1, R2, R3, and Q are as defined herein, useful as N-type calcium channel blockers.
    Type: Application
    Filed: August 16, 2013
    Publication date: June 12, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Mark Wall, Nalin Subasinghe, Zhihua Sui
  • Patent number: 8735600
    Abstract: The present invention relates to improvements in processes towards the production 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid, which is a useful intermediate in fungicide production. In particular, the invention relates to a process for treating a compound of formula III, wherein R1 is C1-C6 alkyl and R2 is CF3, CF2H or CFH2, comprising the steps of a) contacting a compound of formula III with base, and b) separating the compound of formula III and the base.
    Type: Grant
    Filed: April 20, 2010
    Date of Patent: May 27, 2014
    Assignee: Syngenta Limited
    Inventors: Graham McDougald, James Peter Muxworthy, Beverley Ann Wilde
  • 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: 20140135322
    Abstract: The present invention relates to novel chemical compounds formula (I) (C)n—B-(A)m-B—(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five- and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group (—CO—), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1. The compounds are useful in therapy, especially therapy of a mammal suffering from a disease involving misfolded or aggregated forms of proteins.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 15, 2014
    Inventors: Peter Asberg, Kristin Hammer, Johan Olsson, Martin Henriksson
  • Patent number: 8716485
    Abstract: The invention describes a novel process for synthesizing pyrazoles by means of oxidative conversion of enamines with suitable N-containing carboxylic acid derivatives.
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: May 6, 2014
    Assignee: Westfälishe Wilhelms-Universität Münster
    Inventors: Julia Neumann, Mamta Suri, Frank Glorius
  • Patent number: 8703805
    Abstract: Compounds of the invention, such as compounds of Formulae Ia, Ib, Ic, or Id and pharmaceutically acceptable salts, isomers, and prodrugs thereof, which are useful as modulators of the activity of liver X receptors, where R1, R2, R21, R3, and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: April 22, 2014
    Assignee: Exelixis Patent Company LLC
    Inventors: Brett B. Busch, Brenton T. Flatt, Xiao Hui Gu, Shao Po Lu, Richard Martin, Raju Mohan, Michael Charles Nyman, Edwin Schweiger, William C. Stevens, Jr., Tie Lin Wang, Yinong Xie
  • Publication number: 20140107340
    Abstract: The present invention is directed to benzamide containing compounds which inhibit the P2X7 receptor
    Type: Application
    Filed: October 10, 2013
    Publication date: April 17, 2014
    Applicant: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang, Allen T. Hopper
  • Patent number: 8685975
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: April 1, 2014
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Patent number: 8680292
    Abstract: The invention demonstrates the synthesis of a new pyrazole-containing monomer by means of an easily implemented two-step process. This monomer can be electropolymerized to yield a stable n-doping polymer that may easily be electrochemically characterized. It is demonstrated that the electrochemical behavior of the polymer films produced is dependent upon the conditions applied during electrodeposition. Films deposited by cycling only at relatively positive potentials (0 to 2000 mV) show less intense n-doping responses than those films obtained by scanning the applied potential throughout a wider range (?2000 mV to 2000 mV).
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: March 25, 2014
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: David J. Irvin, David L. Witker, John D. Stenger-Smith, Jennifer A. Irvin
  • Patent number: 8680119
    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: March 25, 2014
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Dennis Chapman, Marc Decaire, Peter I. Dosa, Konrad Feichtinger, Honnappa Jayakumar, Thuy-Anh Tran, Sonja Strah-Pleynet, Jingdong Xu
  • Publication number: 20140073679
    Abstract: An improved AKT inhibiting compound, crystalline N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride.
    Type: Application
    Filed: November 19, 2013
    Publication date: March 13, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Pingyun Y. CHEN, Jeffrey Gauling
  • Publication number: 20140073783
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have 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: July 8, 2013
    Publication date: March 13, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Roland Gendron, Adam D. Hughes
  • Patent number: 8664257
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 26, 2011
    Date of Patent: March 4, 2014
    Assignee: Sanofi
    Inventors: Sven Ruf, Josef Pernerstorfer, Thorsten Sadowski, Georg Horstick, Herman Schreuder, Christian Buning, Thomas Olpp, Bodo Scheiper, Klaus Wirth
  • Patent number: 8664258
    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: March 4, 2014
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Dennis Chapman, Juyi Choi, Konrad Feichtinger, Sangdon Han, Honnappa Jayakumar, Thuy-Anh Tran, Jay Xu, Ning Zou
  • Publication number: 20140051682
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
  • Patent number: 8653112
    Abstract: The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R4, R5, R6 and R7 are as defined in the specification; or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: February 18, 2014
    Assignee: Karo Bio AB
    Inventors: Joakim Löfstedt, Xiongyu Wu, Lars Krüger
  • Patent number: 8642637
    Abstract: The pharmaceutically acceptable salts of bicyclo-substituted pyrazolon azo derivatives represented by the general formula (I), their preparation methods, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor. The definitions of substituents in the general formula (I) are the same as the description.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: February 4, 2014
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Peng Cho Tang, Hejun Lü, Hongbo Fei, Yiqian Chen
  • Publication number: 20140031406
    Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.
    Type: Application
    Filed: September 30, 2013
    Publication date: January 30, 2014
    Applicant: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Izumi SASAKI, Tomohiro TOYODA, Hidefumi YOSHINAGA, Itaru NATSUTANI, Yoko TAKAHASHI
  • Patent number: 8629286
    Abstract: The present invention relates to heterocycles which have microbiocidal activity, in particular, fungicidal activity. The invention also relates to preparation of these heterocycles, to heterocyclic derivatives used as intermediates in the preparation of these heterocycles, to preparation of these intermediates, to agrochemical compositions which comprise at least one of the heterocycles, to preparation of these compositions and to use of the heterocycles or compositions in agriculture or horticulture.
    Type: Grant
    Filed: November 25, 2010
    Date of Patent: January 14, 2014
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Sarah Sulzer, Clemens Lamberth
  • Publication number: 20140005389
    Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.
    Type: Application
    Filed: August 30, 2013
    Publication date: January 2, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Christopher John MATHEWS, James Nicholas SCUTT, Michel MUEHLEBACH
  • Publication number: 20130345267
    Abstract: The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.
    Type: Application
    Filed: May 30, 2013
    Publication date: December 26, 2013
    Inventors: Ronen Marmorstein, Xin Liu, Philip A. Cole, Ling Wang, Erin M. Bowers, David J. Meyers, Chandrani Mukherjee
  • Patent number: 8614243
    Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
    Type: Grant
    Filed: June 8, 2010
    Date of Patent: December 24, 2013
    Assignee: Dendreon Corporation
    Inventors: Ofir Moreno, Sateesh Natarajan, David F. Duncan
  • Patent number: 8609711
    Abstract: An improved AKT inhibiting compound, crystalline N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride.
    Type: Grant
    Filed: January 28, 2010
    Date of Patent: December 17, 2013
    Assignee: GlaxoSmithKline LLC
    Inventors: Pingyun Y. Chen, Jeffrey Gaulding
  • Publication number: 20130330366
    Abstract: In one aspect, the invention relates to compounds having the formula XII: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20130330365
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20130324557
    Abstract: The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.
    Type: Application
    Filed: November 4, 2011
    Publication date: December 5, 2013
    Applicant: SENOMYX, INC.
    Inventors: Chad Priest, Alain Noncovich, Andrew Patron, Jane Ung
  • Publication number: 20130323283
    Abstract: Methods for treating or preventing a Foxp3+ T regulatory cell (Treg) related disease in a subject in need thereof comprise administering to the subject an effective amount of a pharmaceutical composition comprising an inhibitor of a histone/protein acetyltransferase (HAT). Methods for identifying an agent useful for treating or preventing a Foxp3+ T regulatory cell (Treg) related disease comprise (a) contacting a candidate agent with a test sample comprising Foxp3+ T regulatory cells (Tregs), and (b) comparing a function of the Foxp3+ Tregs in the test sample with that in a control sample, wherein inhibition of the function of the Foxp3+ Tregs in the test sample when compared with the control sample indicates that the candidate agent is an agent useful for treating or preventing a Foxp3+ Treg related disease.
    Type: Application
    Filed: December 1, 2011
    Publication date: December 5, 2013
    Applicants: THE CHILDREN'S HOSPITAL OF PHILADELPHIA, THE JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE, THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Wayne W. Hancock, Steven M. Albelda, Philip A. Cole
  • Publication number: 20130324536
    Abstract: The invention provides pyrazolyl guanidine compounds that inhibit F1Fo-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: December 8, 2011
    Publication date: December 5, 2013
    Applicant: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Clarke B. Taylor, Chad A. Van Huis
  • Patent number: 8598078
    Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: December 3, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
  • Patent number: 8592475
    Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
    Type: Grant
    Filed: October 14, 2009
    Date of Patent: November 26, 2013
    Assignee: GlaxoSmithKline LLC
    Inventors: Meagan B. Rouse, Mark Andrew Seefeld
  • Publication number: 20130303492
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: March 14, 2013
    Publication date: November 14, 2013
    Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
  • Patent number: 8580834
    Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1, R2 and B are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases in which HGF/SF or the activities thereof, or agonists or antagonists thereof have a therapeutically useful role.
    Type: Grant
    Filed: August 13, 2007
    Date of Patent: November 12, 2013
    Assignee: Angion Biomedica Corp.
    Inventors: David E. Zembower, David A. Eiznhamer
  • Publication number: 20130281455
    Abstract: Phenylpyri(mi)dinylazoles of the formula [I-a] and [I-b], wherein the symbols have the meanings stated in the description, and agrochemically active salts thereof and the use thereof for the control of undesired microorganisms in the protection of plants and materials and for the reduction of mycotoxins in plants and plant parts and methods for the production of compounds of the formula [I-a] and [I-b].
    Type: Application
    Filed: March 15, 2013
    Publication date: October 24, 2013
    Inventors: Alexander SUDAU, Mazen ES-SAYED, Christoph Andreas BRAUN, Ruth MEISSNER, Catherine SIRVEN, Jürgen BENTING, Peter DAHMEN, Daniela PORTZ, Ulrike WACHENDORFF-NEUMANN, Philippe DESBORDES, Samir BENNABI, Christophe CATHERIN, Anne-Sophie REBSTOCK, Marie-Claire GROSJEAN-COURNOYER, Hiroyuki HADANO, Thomas KNOBLOCH, Philippe RINOLFI
  • Publication number: 20130281366
    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 towards compounds which can be used to treat diseases such as Hyperlipidemia and also have a beneficial effect on cholesterol.
    Type: Application
    Filed: December 26, 2011
    Publication date: October 24, 2013
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pankaj, Sairam Kalapatapu, V.V.M., Mukul R. JAIN
  • Patent number: 8563747
    Abstract: The invention provides a process for the preparation of a compound of formula (I) in particular, wherein a compound of formula (II) is reacted with a dialkylsulphate. R1 is C1-C4haloalkyl; R2 is optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; and R3 is methyl or ethyl.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: October 22, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Linhua Wang, Jefferson Thomas Ebert
  • Publication number: 20130274227
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: March 14, 2013
    Publication date: October 17, 2013
    Applicant: Axikin Pharmaceuticals, Inc.
    Inventors: Erik Dean RAAUM, Garrett Thomas Potter, Tai Wei Ly
  • Publication number: 20130274481
    Abstract: The present invention provides a process for the preparation of a compound of formula (I) wherein R1 is C1-C4 haloalkyl; R2 is optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; and R3 is methyl or ethyl; comprising reacting a compound of formula (IV) wherein R1, R2 and R3 are as defined for the compound of formula I; with an alkylating agent in the presence of an amide.
    Type: Application
    Filed: August 3, 2011
    Publication date: October 17, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Linhua Wang, Ritesh Bharat Sheth
  • Publication number: 20130269064
    Abstract: Novel heteroaromatic compounds of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Application
    Filed: November 18, 2011
    Publication date: October 10, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Pierre Joseph Marcel Jung, Ottmar Franz Hueter, Peter Renold
  • Publication number: 20130267543
    Abstract: The present invention relates to HSF activating compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof. In particular, the present invention provides compounds capable of facilitating HSF1 homotrimerization, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with irregular HSF1 activity.
    Type: Application
    Filed: November 8, 2011
    Publication date: October 10, 2013
    Applicants: CHAPERONE THERAPEUTICS, INC., DUKE UNIVERSITY
    Inventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
  • Patent number: 8551426
    Abstract: Provided are an RNase activity inhibitory compound to effectively control the activity of the RNase promoting degradation of extracted RNAs and, in addition, a sample storage container including the same. The RNase activity inhibitory compound and the sample storage container according to the present invention may be effectively used to store RNAs during RNA extraction or the extracted RNAs.
    Type: Grant
    Filed: June 12, 2009
    Date of Patent: October 8, 2013
    Assignee: Bioneer Corporation
    Inventors: Jong Hoon Kim, Hwangseo Park, Han Oh Park
  • Publication number: 20130237500
    Abstract: The present invention relates to novel (thio)carboxamides, 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.
    Type: Application
    Filed: November 14, 2011
    Publication date: September 12, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Juergen Benting, Philippe Desbordes, Stephanie Gary, Joerg Greul, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann
  • Publication number: 20130231344
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: January 4, 2013
    Publication date: September 5, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20130231378
    Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
    Type: Application
    Filed: February 22, 2013
    Publication date: September 5, 2013
    Applicant: GlaxoSmithKline LLC
    Inventors: Mark A. SEEFELD, Meagan B. Rouse, Dirk A. Heerding, Dennis S. Yamashita, Kenneth C. McMulty
  • Publication number: 20130231303
    Abstract: The present invention relates to novel 5-halogenopyrazole(thio)carboxamides, 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.
    Type: Application
    Filed: November 14, 2011
    Publication date: September 5, 2013
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Juergen Benting, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Joerg Greul, Hiroyuki Hadano, Jan Peter Schmidt, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann, Lars Rodefeld
  • Publication number: 20130225606
    Abstract: The present invention relates to N-Hetarylmethyl pyrazolylcarboxamides derivatives or their thiocarboxamides derivatives, their process of preparation, their use as fungicide, particularly in the form of compositions. Formula (I), and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Application
    Filed: November 2, 2011
    Publication date: August 29, 2013
    Inventors: Jurgen Benting, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Jan-Peter Schmidt, Ulrike Wachendorff-Neumann
  • Patent number: 8519188
    Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: August 27, 2013
    Assignee: Marc-Henry Pitty
    Inventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
  • Publication number: 20130217727
    Abstract: The present invention relates to fungicidal 1-(heterocyclic carbonyl)-2-substituted pyrrolidines and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.
    Type: Application
    Filed: October 20, 2011
    Publication date: August 22, 2013
    Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Hiroyuki Hadano, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
  • Patent number: 8513244
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have 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: Grant
    Filed: May 18, 2012
    Date of Patent: August 20, 2013
    Assignee: Theravance, Inc.
    Inventors: Roland Gendron, Adam D. Hughes
  • Publication number: 20130203818
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: April 27, 2011
    Publication date: August 8, 2013
    Applicant: CALCIMEDICA, INC.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey