Carbonyl Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/329)
  • PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER
    Publication number: 20140011796
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: AMGEN INC.
    Inventors: Michael David BARTBERGER, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason Duquette, John Eksterwicz, Benjamin Fisher, Brian Matthew Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael William Gribble, Dann James Gustin, Julie Anne Heath, Xin Huang, Xianyun Jiao, Michael Johnson, Frank Kayser, David John Kopecky, Sujen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan Dante Low, Brian Stuart Lucas, Zhihua Ma, Lawrence R. McGee, Joel McIntosh, Dustin McMinn, Julio Cesar Medina, Jeffrey Thomas Mihalic, Steven Howard Olson, Yosup Rew, Philip Marley Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
  • PEPTIDE DEFORMYLASE INHIBITORS
    Publication number: 20130345120
    Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
    Type: Application
    Filed: March 9, 2012
    Publication date: December 26, 2013
    Applicant: Glaxosmithkline LLC
    Inventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
  • HETEROCYCLIC TYROSINE KINASE INHIBITORS
    Publication number: 20130345192
    Abstract: The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.
    Type: Application
    Filed: October 28, 2011
    Publication date: December 26, 2013
    Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.
    Inventors: Brian T. Hopkins, Daniel Scott, Patrick Conlon, Tracy J. Jenkins, Noel Powell, Bing Guan, Julio H. Cuervo, Deping Wang, Art Taveras
  • 2-(substituted phenyl)-6-amino-5-alkoxy, thioalkoxy and aminoalkyl-4-pyrimidinecarboxylates and their use as herbicides
    Patent number: 8609592
    Abstract: 2-(Substituted phenyl)-6-amino-5-alkoxy, thioalkoxy and aminoalkyl-4-pyrimidinecarboxylic acid and its derivatives are potent herbicides demonstrating broad spectrum of weed control.
    Type: Grant
    Filed: December 5, 2012
    Date of Patent: December 17, 2013
    Assignee: Dow AgroSciences, LLC.
    Inventors: Katherine A. Guenthenspberger, Thomas L. Siddall
  • Bi-aryl meta-pyrimidine inhibitors of kinases
    Patent number: 8604042
    Abstract: The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non-receptor kinases.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: December 10, 2013
    Assignee: TargeGen, Inc.
    Inventors: Glenn Noronha, Chi Ching Mak, Jianguo Cao, Joel Renick, Andrew McPherson, Binqi Zeng, Ved P. Pathak, Daniel L. Lohse, John D. Hood, Richard M. Soll
  • N-ALKOXYAMIDES OF 6-(SUBSTITUTED PHENYL)-4-AMINOPICOLINATES AND 2-(SUBSTITUTED PHENYL)-6-AMINO-4-PYRIMIDINECARBOXYLATES AND THEIR USE AS SELECTIVE HERBICIDES FOR CROPS
    Publication number: 20130324412
    Abstract: N-Alkoxyamides of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are selective herbicides for corn, canola and sugar beet.
    Type: Application
    Filed: August 8, 2013
    Publication date: December 5, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Joseph D. Eckelbarger, Paul R. Schmitzer, Carla N. Yerkes, Timothy A. Boebel, Norbert M. Satchivi, Gregory T. Whiteker
  • CYCLIC PYRIMIDIN-4-CARBOXAMIDES AS CCR2 RECEPTOR ANTAGONISTS FOR TREATMENT OF INFLAMMATION, ASTHMA AND COPD
    Publication number: 20130324517
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
    Type: Application
    Filed: July 24, 2013
    Publication date: December 5, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner EBEL, Sara FRATTINI, Riccardo GIOVANNINI, Christoph HOENKE, Thomas TRIESELMANN, Patrick TIELMANN, Stefan SCHEUERER, Silke HOBBIE, Frank BUETTNER
  • 2-(2-fluoro-substituted phenyl)-6-amino-5-chloro-4-pyrimidinecarboxylates and their use as herbicides
    Patent number: 8598085
    Abstract: 2-(2-Fluoro-substituted phenyl)-6-amino-5-chloro-4-pyrimidine carboxylic acid and its derivatives are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: December 3, 2013
    Assignee: Dow AgroSciences, LLC.
    Inventors: Jeffrey B. Epp, William C. Lo, Paul R. Schmitzer, Carla N. Yerkes
  • Fatty Amine Salts Of Herbicidal Pyrimidines
    Publication number: 20130303369
    Abstract: This invention is directed to (1) a soluble intermediate prepared from reaction of the acid form of one or more of the compounds disclosed by Formula I given below with at least one long-chain fatty amine; (2) a process for solubilizing one or more of the compounds disclosed by Formula I given below by reacting said compounds with at least one long-chain fatty amine to form a fatty-amine salt of Formula I compound; and (3) a finished pesticide product comprising at least one of the soluble intermediates, that is, fatty-amine salt of Formula I compound.
    Type: Application
    Filed: December 27, 2012
    Publication date: November 14, 2013
    Applicant: E. I. du Pont de Nemours and Company
    Inventor: E. I. du Pont de Nemours and Company
  • CHEMOKINE RECEPTOR ANTAGONISTS
    Publication number: 20130261129
    Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Application
    Filed: March 29, 2013
    Publication date: October 3, 2013
    Applicant: AbbVie Inc.
    Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Wei, Lijuan Jane Wang
  • SMAC peptidometics useful as IAP inhibitors
    Patent number: 8546336
    Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: October 1, 2013
    Assignee: Novartis AG
    Inventors: Zhuoliang Chen, Mark G. Charest, Christine Hiu-Tung Chen, Miao Dai, Feng He, Huangshu Lei, Ly Luu Pham, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming David Wang, Fan Yang, Leigh Zawel
  • Isotopically enriched pyrimidin-5-yl acetic acid derivatives as CRTH2 antagonists
    Patent number: 8541419
    Abstract: Provided herein are 2H- and 13C-enriched compounds of formula (I) or (II); wherein R is as defined herein, and wherein at least one hydrogen atom, in certain embodiments, three or more hydrogen atoms, are deuterium atoms or at least one carbon atom is a carbon-13 atom. Also provided are pharmaceutical compositions and methods using the 2H- and 13C-enriched compounds, useful for treating CRTH2-related diseases or disorders such as, for example, asthma, allergic rhinitis, atopic dermatitis, allergic conjuvatitis, Churg-Strauss syndrome, sinusitis, basophilic leukemia, chronic urticaria or basophilic leukocytosis.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: September 24, 2013
    Assignee: Actimis Pharmaceuticals, Inc.
    Inventor: Tai Wei Ly
  • PROCESS FOR THE PREPARATION OF PYRIMIDINE DERIVATIVES
    Publication number: 20130245263
    Abstract: A process for the preparation of 5-substituted 4-amino-2-methylpyrimidines of the formula wherein R is CONH2 or CN, and of acid addition salts thereof, characterized in that a compound of formula H2N—CH?C(R) CN (II) is reacted with acetimidic acid methyl ester or an acid addition salt thereof and that, if desired, a compound of formula I is transferred into an acid addition salt, and the transformation of a compound of formula II wherein R is CONH2 into a compound of formula II wherein R is CN by treatment with POCl3.
    Type: Application
    Filed: May 13, 2013
    Publication date: September 19, 2013
    Applicant: DSM IP ASSETS B.V.
    Inventors: Reinhard KARGE, Jan SCHULTZ
  • CARBAMATE AND UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1
    Publication number: 20130244994
    Abstract: This invention relates to novel compounds of the Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Application
    Filed: February 15, 2013
    Publication date: September 19, 2013
    Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice
  • N-alkoxyamides of 6-(trisubstituted phenyl)-4-aminopicolinates and their use as selective herbicides for crops
    Patent number: 8536331
    Abstract: N-Alkoxyamides of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are selective herbicides for corn, canola and sugar beet.
    Type: Grant
    Filed: February 25, 2010
    Date of Patent: September 17, 2013
    Assignee: Dow AgroSciences, LLC.
    Inventors: Joseph D. Eckelbarger, Paul R. Schmitzer, Carla N. Yerkes, Timothy A. Boebel, Norbert M. Satchivi
  • 2-(POLY-SUBSTITUTED ARYL)-6-AMINO-5-HALO-4-PYRIMIDINECARBOXYLIC ACIDS AND THEIR USE AS HERBICIDES
    Publication number: 20130237422
    Abstract: 6-Amino-5-halo-4-pyrimidinecarboxylic acids having poly-substituted aryl substituents in the 2-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Application
    Filed: April 24, 2013
    Publication date: September 12, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Jeffrey B. Epp, Paul R. Schmitzer, James M. Ruiz, Terry W. Balko, Thomas L. Siddall, Carla N. Yerkes
  • ARYLCYCLOPROPYLAMINE BASED DEMETHYLASE INHIBITORS OF LSD1 AND THEIR MEDICAL USE
    Publication number: 20130231342
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
    Type: Application
    Filed: July 27, 2011
    Publication date: September 5, 2013
    Applicant: Oryzon Fenomics S.A.
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez de la Cuesta, Maria de los Ángeles Estirate-Martinez
  • Heterocyclic peptide ketoamides
    Patent number: 8518885
    Abstract: A novel class of peptide ?-ketoamides useful for selectively inhibiting calpains, selectively inhibiting cysteine proteases, and generally inhibiting all cysteine proteases, having the formula M-AA2-AA1-CO—NH—(CH2)n—R3. Processes for the synthesis of peptidyl ?-ketoamide derivatives. Compositions and methods for inhibiting cysteine proteases, inhibiting calpains, and treating disease caused by cysteine proteases and calpains are provided.
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: August 27, 2013
    Assignees: Georgia Tech Research Corporation, Emory University
    Inventors: James C. Powers, Jonathan D. Glass, Asli Ovat, Zhaozhao Li
  • 2-amido pyrazines for inflammation and immune related uses
    Patent number: 8518950
    Abstract: The invention relates to compounds of structural formula (I) and structural formula (VI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R, R1, R2, Z, L, 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: Grant
    Filed: January 25, 2006
    Date of Patent: August 27, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Shoujun Chen, Jun Jiang, Yu Xie, Chih-Yi Yu
  • HETEROARYL COMPOUNDS AND USES THEREOF
    Publication number: 20130217688
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: May 2, 2013
    Publication date: August 22, 2013
    Applicant: Celgene Avilomics Research, Inc.
    Inventor: Celgene Avilomics Research, Inc.
  • 2-SUBSTITUTED-6-AMINO-5-ALKYL, ALKENYL OR ALKYNYL-4-PYRIMIDINECARBOXYLIC ACIDS AND 6-SUBSTITUTED-4-AMINO-3-ALKYL, ALKENYL OR ALKYNYL PICOLINIC ACIDS AND THEIR USE AS HERBICIDES
    Publication number: 20130210631
    Abstract: 6-Amino-4-pyrimidinecarboxylic acids having alkyl, alkenyl or alkynyl substituents in the 5-position and 4-aminopicolinic acids having alkyl, alkenyl or alkynyl substituents in the 3-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Application
    Filed: August 16, 2012
    Publication date: August 15, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Jeffrey B. Epp, Paul R. Schmitzer, Terry W. Balko, Carla N. Yerkes
  • N-HETEROARYL COMPOUNDS
    Publication number: 20130196993
    Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to novel N-heteroaryl compounds and the preparation of said compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: September 28, 2011
    Publication date: August 1, 2013
    Inventors: Michael Berger, Christopher Kern, Marko Eck
  • 3-AMINOCYCLOPENTANECARBOXAMIDES AS CHEMOKINE RECEPTOR AGONISTS
    Publication number: 20130197008
    Abstract: There is provided a compound of Formula I(a) or I(b): or a pharmaceutically acceptable salt thereof, wherein the various substitutents are defined herein.
    Type: Application
    Filed: September 14, 2012
    Publication date: August 1, 2013
    Applicant: Pfizer Inc.
    Inventors: Robert O. HUGHES, Rajesh V. Devraj, Donald J. Rogier, John I. Trujillo, Steve R. Turner, Wei Huang
  • THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE
    Publication number: 20130190249
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: January 18, 2013
    Publication date: July 25, 2013
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventor: Agios Pharmaceuticals, Inc.
  • PYRROLIDINE DERIVATIVES
    Publication number: 20130184249
    Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: February 28, 2013
    Publication date: July 18, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • HEXAFLUOROISOPROPYL CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
    Publication number: 20130165422
    Abstract: The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): in which: R, Z, A, m, and n are as defined in the disclosure; in the form of the base or of an addition salt with an acid, and to the preparation process and therapeutic application thereof.
    Type: Application
    Filed: November 29, 2012
    Publication date: June 27, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Azetidine Derivatives
    Publication number: 20130158004
    Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Application
    Filed: December 14, 2012
    Publication date: June 20, 2013
    Inventors: Martin FLECK, Bernd NOSSE, Niklas HEINE, Gerald Juergen ROTH
  • NEW SELECTIVE CCR2 ANTAGONISTS
    Publication number: 20130150354
    Abstract: The present invention relates to novel and selective antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD as well as pain.
    Type: Application
    Filed: June 14, 2012
    Publication date: June 13, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner EBEL, Sara FRATTINI, Riccardo GIOVANNINI, Stefan SCHEUERER
  • TRYPTOPHAN HYDROXYLASE INHIBITORS FOR THE TREATMENT OF METASTATIC BONE DISEASE
    Publication number: 20130137635
    Abstract: This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of metastatic bone disease.
    Type: Application
    Filed: February 9, 2011
    Publication date: May 30, 2013
    Applicant: LEXICON PHARMACEUTICALS, INC.
    Inventor: Arthur Thomas Sands
  • NOVEL CCR2 RECEPTOR ANTAGONISTS, METHOD FOR PRODUCING THE SAME, AND USE THEREOF AS MEDICAMENTS
    Publication number: 20130123241
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.
    Type: Application
    Filed: May 10, 2011
    Publication date: May 16, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
  • 2-(2-FLUORO-SUBSTITUTED PHENYL)-6-AMINO-5-CHLORO-4-PYRIMIDINECARBOXYLATES AND THEIR USE AS HERBICIDES
    Publication number: 20130109573
    Abstract: 2-(2-Fluoro-substituted phenyl)-6-amino-5-chloro-4-pyrimidine carboxylic acid and its derivatives are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Application
    Filed: December 14, 2012
    Publication date: May 2, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventor: DOW AGROSCIENCES LLC
  • 6-amino-pyrimidine-4-carboxamide derivatives and related compounds which bind to the sphingosine 1-phosphate (S1P) receptor for the treatment of multiple sclerosis
    Patent number: 8399448
    Abstract: The invention relates to compounds of formula (I): wherein X, W, Q, R, R1 and R2 have the meanings given in claim 1. The compounds are useful, for example, in the treatment of autoimmune disorders, such as multiple sclerosis.
    Type: Grant
    Filed: July 29, 2008
    Date of Patent: March 19, 2013
    Assignee: Merck Serono SA
    Inventors: Agnes Bombrun, Matthias Schwarz, Stefano Crosignani, David Covini, Delphine Marin
  • 2,4 (4,6) pyrimidine derivatives
    Patent number: 8394955
    Abstract: The present invention is drawn to intermediates relating to 2,4 (4,6) pyrimidine derived macrocycles, pharmaceutical compositions thereof, and methods of making said compounds. The compounds disclosed herein are inhibitors of EGF receptor tyrosine kinases and are useful for treating cell proliferative disorders, including atherosclerosis, restenosis, and cancer.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: March 12, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Eddy Jean Edgard Freyne, Marc Willems, Werner Constant Johan Embrechts, Kristof Van Emelen, Sven Franciscus Anna Van Brandt, Frederik Jan Rita Rombouts
  • PEPTIDE DEFORMYLASE INHIBITORS
    Publication number: 20130045962
    Abstract: The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives. Specifically, the invention is directed to compounds of formula (I): wherein R1, R2 and R3 are defined below and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.
    Type: Application
    Filed: November 6, 2008
    Publication date: February 21, 2013
    Inventors: Donghui Qin, Beth Norton, Xiangmin Liao, Andrew Nicholson Knox, Jinhwa Lee, Yuhong Fang, Jason Christopher Dreabit, Siegfried Benjamin Christensen, IV, Andrew B. Benowitz, Kelly M. Aubart
  • 2-(2-fluoro-substituted phenyl)-6-amino-5-chloro-4-pyrimidinecarboxylates and their use as herbicides
    Patent number: 8357633
    Abstract: 2-(2-Fluoro-substituted phenyl)-6-amino-5-chloro-4-pyrimidine carboxylic acid and its derivatives are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: January 15, 2010
    Date of Patent: January 22, 2013
    Assignee: Dow AgroSciences, LLC
    Inventors: Jeffrey B. Epp, William C. Lo, Paul R. Schmitzer, Carla N. Yerkes
  • SMAC PEPTIDOMETICS USEFUL AS IAP INHIBITORS
    Publication number: 20130005663
    Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.
    Type: Application
    Filed: September 7, 2012
    Publication date: January 3, 2013
    Applicant: NOVARTIS AG
    Inventors: Mark G. CHAREST, Christine Hiu-Tung CHEN, Zhuoliang CHEN, Miao DAI, Feng HE, Huangshu LEI, Ly Luu PHAM, Sushil Kumar SHARMA, Christopher Sean STRAUB, Run-Ming David WANG, Fan YANG, Leigh ZAWEL
  • 2-(POLY-SUBSTITUTED ARYL)-6-AMINO-5-HALO-4-PYRIMIDINECARBOXYLIC ACIDS AND THEIR USE AS HERBICIDES
    Publication number: 20130005577
    Abstract: 6-Amino-5-halo-4-pyrimidinecarboxylic acids having poly-substituted aryl substituents in the 2-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 3, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Jeffrey B. Epp, Paul R. Schmitzer, James M. Ruiz, Terry W. Balko, Thomas L. Siddall, Carla N. Yerkes
  • IMIDAZOLO-, OXAZOLO-, AND THIAZOLOPYRIMIDINE MODULATORS OF TRPV1
    Publication number: 20130005687
    Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 3, 2013
    Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
  • HETEROCYCLIC AMIDES AS ROCK INHIBITORS
    Publication number: 20120322801
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
    Type: Application
    Filed: March 4, 2011
    Publication date: December 20, 2012
    Applicant: Amakem NV
    Inventors: Dirk Leysen, Olivier Defert, Nadzeya Kaval, Petra Blom, Sandro Boland
  • 2-ARYL-PROPIONAMIDE DERIVATIVES USEFUL AS BRADYKININ RECEPTOR ANTAGONISTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    Publication number: 20120316169
    Abstract: (R,S) 2-aryl-propionamide derivatives, or their single enantiomers (R) and (S) are disclosed useful in the treatment or prevention of symptoms and disorders such as pain and inflammation associated with the bradykinin B1 pathway.
    Type: Application
    Filed: October 28, 2010
    Publication date: December 13, 2012
    Applicant: DOMPÉ S.P.A.
    Inventors: Andrea Beccari, Andrea Aramini, Gianluca Bianchini, Alessio Moriconi
  • Tryptophan Hydroxylase Inhibitors for the Treatment of Cancer
    Publication number: 20120316171
    Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.
    Type: Application
    Filed: November 4, 2010
    Publication date: December 13, 2012
    Inventor: Tamas Oravecz
  • NOVEL SALTS FORMS OF PYRIMIDIN-5-YL ACETIC ACID DERIVATIVE
    Publication number: 20120302584
    Abstract: Provided are crystalline N-methyl-glucamine and sodium salts of [4,6-bis(dimethylamino)-2-(4-{[4-(trifluoromethyl)benzoyl]amino}benzyl)pyrimidin-5-yl] acetic acid, processes for their preparation, pharmaceutical compositions comprising the salts, and methods of their use for treating, preventing, or ameliorating one or more symptoms of a CRTH2-mediated disorder or disease.
    Type: Application
    Filed: November 17, 2010
    Publication date: November 29, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Bing-Shiou Yang
  • Hydrazone derivative
    Patent number: 8314247
    Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.
    Type: Grant
    Filed: January 9, 2008
    Date of Patent: November 20, 2012
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
  • 2-(poly-substituted aryl)-6-amino-5-halo-4-pyrimidinecarboxylic acids and their use as herbicides
    Patent number: 8288318
    Abstract: 6-Amino-5-halo-4-pyrimidinecarboxylic acids having poly-substituted aryl substituents in the 2-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: January 4, 2011
    Date of Patent: October 16, 2012
    Assignee: Dow AgroSciences, LLC.
    Inventors: Jeffrey B. Epp, Paul R. Schmitzer, James M. Ruiz, Terry W. Balko, Thomas L. Siddall, Carla N. Yerkes
  • Substituted Aminobutyric Derivatives as Neprilysin Inhibitors
    Publication number: 20120252830
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 7, 2012
    Publication date: October 4, 2012
    Applicant: NOVARTIS AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • INHIBITORS OF SPHINGOSINE KINASE
    Publication number: 20120252789
    Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, M4, Y1, Y2, V, W, n, m and o have the meanings given in Claim 1, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.
    Type: Application
    Filed: November 22, 2010
    Publication date: October 4, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Frank Stieber, Dirk Wienke
  • Amine salts of a CRTH2 antagonist
    Patent number: 8278310
    Abstract: Provided are amine salts of {4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)benzyl)pyrimidin-5-yl}-acetic acid, processes for their preparation, pharmaceutical compositions containing them, and their use for treating, preventing, or ameliorating one or more symptoms of a CRTH2-mediated disorder or disease.
    Type: Grant
    Filed: June 18, 2008
    Date of Patent: October 2, 2012
    Assignee: Actimis Pharmaceuticals, Inc.
    Inventor: Tai Wei Ly
  • Triazolo pyrimidine compounds
    Patent number: 8273879
    Abstract: The present invention relates to a pyrimidine compound (I) useful as a pharmaceutical intermediate, to a process for preparing said pyrimidine compound, to intermediates used in said process, and to the use of said pyrimidine compound in the preparation of pharmaceuticals.
    Type: Grant
    Filed: March 24, 2011
    Date of Patent: September 25, 2012
    Assignee: AstraZeneca AB
    Inventors: Ulf Larsson, Mattias Magnusson, Tibor Musil, Andreas Palmgren
  • ANTIPROLIFERATIVE PYRIMIDYL, FUSED PYRIMIDYL AND PYRIMIDYL HYDRAZONES
    Publication number: 20120238575
    Abstract: The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease.
    Type: Application
    Filed: May 31, 2012
    Publication date: September 20, 2012
    Applicant: MERCK SERONO SA
    Inventors: BRIAN HEALEY, Zhong Zhao, Amanda Sutton, Matthias Schwarz
  • (1, 1, 1,3,3,3 -HEXAFLUORO-2 HYDROXYPROPAN- 2 -YL) PHENYL DERIVATIVE, PHARMACEUTICAL COMPOSITIONS THEREOF AND THEIR USE FOR THE TREATMENT OF ATHEROSCLEROSIS
    Publication number: 20120238574
    Abstract: The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis.
    Type: Application
    Filed: October 26, 2010
    Publication date: September 20, 2012
    Applicant: N.V. ORGANON
    Inventors: Andrew John Cooke, Emma Louise Carswell, David Jonathan Bennett