The Six-membered Hetero Ring Consists Of Two Nitrogens And Four Carbons (e.g., 1,2-diazines, Etc.) Patents (Class 544/224)
  • Patent number: 10246393
    Abstract: In a cross coupling reaction, in a case where a halogen atom is selected as the leaving group of the raw material compound, a harmful halogen waste forms as a by-product after the reaction, and disposal of the waste liquid is complicated and environmental burden is high. In a carbon-hydrogen activation cross coupling reaction which requires no halogen atom as the leaving group, although no halogen waste forms as a by-product, the reaction substrate is considerably restricted, and the reaction remains a limited molecular construction method. A method for producing an aromatic compound, which comprises subjecting an aromatic nitro compound and a boronic acid compound to a cross coupling reaction in the presence of a metal catalyst.
    Type: Grant
    Filed: October 30, 2017
    Date of Patent: April 2, 2019
    Assignees: TOSOH CORPORATION, KYOTO UNIVERSITY
    Inventors: Hisao Eguchi, Takanori Miyazaki, Yoshiaki Nakao
  • Patent number: 9371329
    Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: May 9, 2014
    Date of Patent: June 21, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
  • Patent number: 9096544
    Abstract: The invention provides compounds of formula I or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for inducing apoptosis or treating cancer using compounds of formula I.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: August 4, 2015
    Assignees: Wayne State University, Department of Veterans Affairs, Sanford-Burnham Medical Research Institute
    Inventors: Joseph A. Fontana, Marcia Dawson, Zebin Xia
  • Patent number: 9023850
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: May 5, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
  • Publication number: 20150119397
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: January 8, 2015
    Publication date: April 30, 2015
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Publication number: 20150112061
    Abstract: Hydrazinopyridazines, fused hydrazinopyridazines, phenylethylhydrazines, or combinations thereof, compositions comprising hydrazinopyridazines, fused hydrazinopyridazines, phenyl ethylhydrazines, or combinations thereof, and methods for using them for the treatment of pain are described.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventor: Riyi Shi
  • Patent number: 9012632
    Abstract: Provided is a method whereby a heteroaromatic ring aryl can be very rapidly methylated at a high yield. In an N-alkyl-2-pyrrolidinone, a heteroaromatic ring aryltrialkylstannan is cross-coupled with methyl iodide in the presence of a palladium complex, a phosphine ligand, a cuprous halide, a carbonic acid salt and/or an alkali metal fluoride to thereby rapidly methylate the heteroaromatic ring aryl. (Formula shows a case wherein the heteroaromatic ring aryl is a pyridyl group.
    Type: Grant
    Filed: December 25, 2009
    Date of Patent: April 21, 2015
    Assignee: Riken
    Inventors: Masaaki Suzuki, Hisashi Doi, Hiroko Koyama
  • Patent number: 8993753
    Abstract: The present invention relates to a process for the stereoselective preparation of compounds of formulae (1A) and (1B) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.
    Type: Grant
    Filed: January 14, 2014
    Date of Patent: March 31, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Markus Ostermeier, Juergen Daeubler, Guenther Huchler, Stephan Kling, Marco Santagostino
  • Patent number: 8980935
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: March 17, 2015
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh
  • Publication number: 20150065517
    Abstract: The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Application
    Filed: November 10, 2014
    Publication date: March 5, 2015
    Applicant: NOVARTIS AG
    Inventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming LIU
  • Patent number: 8969346
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 22, 2011
    Date of Patent: March 3, 2015
    Assignee: Cytokinetics, Inc.
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Scott Collibee, Chihyuan Chuang, Jeff Gardina, Bradley P. Morgan, Alex R. Muci, Xiangping Qian, Jeffrey M Warrington, Zhe Yang, Pu-Ping Lu, Antonio Romero
  • Patent number: 8952207
    Abstract: The present invention is a one-step method for efficiently converting carbon-hydrogen bonds into carbon-carbon bonds using a combination of aryl halides, a substrate, and a copper salt as catalyst. This method allows faster introduction of complex molecular entities, a process that would otherwise require many more steps. This invention is particularly relevant for the organic synthesis of complex molecules such as, but not limited to, pharmacophores and explosives.
    Type: Grant
    Filed: September 10, 2008
    Date of Patent: February 10, 2015
    Assignee: The University of Houston System
    Inventors: Olafs Daugulis, Hien-Quang Do
  • Patent number: 8952151
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: February 10, 2015
    Assignee: Quanticel Pharmaceuticals, Inc.
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Patent number: 8946442
    Abstract: Foams of ionic compounds are described. Methods of making the foams are also provided. The foams are ionic and can be used for catalysis, separations, gas storage, biosensors, electronics, and electrochemical applications.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: February 3, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: Mark Brandon Shiflett, Akimichi Yokozeki
  • Patent number: 8946225
    Abstract: The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: —R1 represents one or more groups such as: trifluoromethyl, halogen such as F, Cl, —when n=m=1, W represents CH then Y represents oxygen, —U represents: •either —(C?O)CH2NH— and is branched at position 4 of pyridazinone, then R2 represents H, •or —(C?O)NH— and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, —R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enzyme inhibitors for the treatment of obesity, type-2 diabetes and lipid disorders.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: February 3, 2015
    Assignee: Pierre Fabre Medicament
    Inventors: Elisabeth Dupont-Passelaigue, Samuel Mialhe, Jean-Pierre Rieu, Didier Junquero, Karine Valeille
  • Patent number: 8946220
    Abstract: Hydrazinopyridazines, fused hydrazinopyridazines, phenylethylhydrazines, or combinations thereof, compositions comprising hydrazinopyridazines, fused hydrazinopyridazines, phenylethylhydrazines, or combinations thereof, and methods for using them for the treatment of pain are described.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: February 3, 2015
    Assignee: Purdue Research Foundation
    Inventor: Riyi Shi
  • Patent number: 8940741
    Abstract: This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y4, are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: January 27, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Steven Joseph Berthel, Roland Joseph Billedeau, Christine E. Brotherton-Pleiss, Fariborz Firooznia, Stephen Deems Gabriel, Xiaochun Han, Ramona Hilgenkamp, Saul Jaime-Figueroa, Buelent Kocer, Francisco Javier Lopez-Tapia, Yan Lou, Lucja Orzechowski, Timothy D. Owens, Jenny Tan, Peter Michael Wovkulich
  • Publication number: 20150025235
    Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.
    Type: Application
    Filed: May 30, 2014
    Publication date: January 22, 2015
    Inventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar, Aleksey G. Kazantsev
  • Patent number: 8937072
    Abstract: Disclosed is a substituted cyanoaniline compound or a salt thereof, wherein the compound has a structure represented by General Formula I. The compound of General Formula I has broad-spectrum fungicidal activity in the field of agriculture and effectively prevents against a variety of pathogens such as cucumber downy mildew, wheat powdery mildew, maize rust disease, rice blast and cucumber gray mold. In particular, even at a low dose, the compound effectively prevents and treats rice blast, cucumber gray mold, maize rust disease and cucumber downy mildew. Moreover, the raw materials for preparing the compounds are widely available and the synthesis method therefor is simple and convenient.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: January 20, 2015
    Assignees: Sinochem Corporation, Shenyang Research Institute of Chemical Industry Co., Ltd.
    Inventors: Changling Liu, Guang Huang, Jie Lan, Shulin Hao, Zhinian Li, Huichao Li, Aiying Guan, Airu Jiang, Ying Xu
  • Patent number: 8933076
    Abstract: The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of making and using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for, research, drug screening, and therapeutic applications.
    Type: Grant
    Filed: June 8, 2012
    Date of Patent: January 13, 2015
    Assignees: Centre National de la Recherche Scientifique (CNRS), Northwestern University, Universite de Strasbourg
    Inventors: D. Martin Watterson, Linda Van Eldik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Velentza, Wenhui Hu, Magdalena Zasadzki
  • Patent number: 8927531
    Abstract: Compounds of general formula I wherein the group R1 is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: February 3, 2014
    Date of Patent: January 6, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Matthias Eckhardt
  • Publication number: 20150005495
    Abstract: A composition for controlling plant diseases, containing a pyridazine compound represented by Formula (I) and fipronil, exhibits an excellent control effect against plant diseases. The present invention provides a composition for controlling plant diseases, containing the pyridazine compound represented by Formula (I) and fipronil, and a method for controlling plant diseases, including a step of applying an effective amount of the pyridazine compound represented by Formula (I) and fipronil to a plant or soil for cultivating a plant. [In the formula, R1 represents a chlorine atom, a bromine atom, a cyano group, or a methyl group, and R2 represents a hydrogen atom or a fluorine atom.
    Type: Application
    Filed: January 8, 2013
    Publication date: January 1, 2015
    Inventor: Yuichi Matsuzaki
  • Publication number: 20140378461
    Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides.
    Type: Application
    Filed: February 14, 2013
    Publication date: December 25, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Anthony Cornelius O'Sullivan, Olivier Loiseleur, Daniel Stierli, Torsten Luksch, Thomas Pitterna
  • Publication number: 20140371073
    Abstract: The present invention relates to novel non-steroidal brassinosteroid mimetic derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.
    Type: Application
    Filed: September 11, 2012
    Publication date: December 18, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Pierre Joseph Marcel Jung, Joerg Leipner, Mathilde Denise Lachia, Alain De Mesmaeker
  • Patent number: 8912186
    Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: December 16, 2014
    Assignee: Universitaet des Saarlandes
    Inventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
  • Patent number: 8906921
    Abstract: The present invention relates to (1-benzyl-piperidin-4-yl)-(4-alkoxy-pyridazin-3-y1)-amines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: December 9, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gregor James MacDonald, José Manuel Bartolomé-Nebreda
  • Publication number: 20140357614
    Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xioahu Zhang
  • Patent number: 8895556
    Abstract: The invention relates to a compound of Formula I: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof, wherein the remaining substituents are described herein; and a composition comprising the thiosemicarbazone and/or the semicarbazone. The invention also relates to a method of administration of a thiocarbazone and/or a semicarbazone; and use thereof to treat a cancer.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: November 25, 2014
    Assignee: Critical Outcome Technologies Inc.
    Inventors: Wayne R. Danter, Cheuk Kun Lau
  • Patent number: 8895734
    Abstract: The present invention provides a novel class of peptide nucleic acid derivatives, which show good cell penetration and strong binding affinity for nucleic acid.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: November 25, 2014
    Assignee: OliPass Corporation
    Inventors: Shin Chung, Heui-Yeon Kim, Hyun-Jin Park, Mi-Ran Kim, Jong-Ook Lee
  • Publication number: 20140336198
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Application
    Filed: May 16, 2012
    Publication date: November 13, 2014
    Applicants: MERCK PATENT GMBH, BIONOMICS LIMITED
    Inventors: Andrew Harvey, Agnes Bombrun, Rachel Cooke, Isabelle Jeanclaude-Etter, Nathan Kuchel, Jerome Molette, Jorgen Mould, Dharam Paul, Rajinder Singh, Cristina Donini, Veronique Colovray, Thomas Avery, Julia Crossman, Justin Ripper
  • Patent number: 8883800
    Abstract: The present invention relates to substituted quinazolines of formula (I): wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: November 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Markus Frank, Thomas Klein
  • Patent number: 8884008
    Abstract: The present invention provides a novel class of peptide nucleic acid derivatives, which show good cell penetration and strong binding affinity for nucleic acid.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: November 11, 2014
    Assignee: OliPass Corporation
    Inventors: Shin Chung, Heui-Yeon Kim, Hyun-Jin Park, Mi-Ran Kim, Jong-Ook Lee
  • Patent number: 8877754
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Heike Neubauer, Bernd Nosse
  • Publication number: 20140315878
    Abstract: The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or a pharmaceutically acceptable salt thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes, and to methods of treatment, wherein R1, R2, R3, R4, R5 and R6 are as defined in the description.
    Type: Application
    Filed: April 17, 2014
    Publication date: October 23, 2014
    Applicant: PFIZER LIMITED
    Inventors: Robert Ian Storer, Nigel Alan Swain, Robert McKenzie Owen
  • Patent number: 8859766
    Abstract: The present invention provides a novel class of peptide nucleic acid derivatives, which show good cell penetration and strong binding affinity for nucleic acid.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: October 14, 2014
    Assignee: OliPass Corporation
    Inventors: Shin Chung, Heui-Yeon Kim, Hyun-Jin Park, Mi-Ran Kim, Jong-Ook Lee
  • Patent number: 8859549
    Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, R1, and R2 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: Grant
    Filed: May 8, 2012
    Date of Patent: October 14, 2014
    Assignee: AbbVie, Inc.
    Inventors: Brian S. Brown, Tongmei Li, Sridhar Peddi, Arturo Perez-Medrano, David DeGoey
  • Patent number: 8853390
    Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: October 7, 2014
    Assignee: AbbVie Inc.
    Inventors: Yi-Yin Ku, Timothy A. Grieme, Jeffrey M. Kallemeyn, Mathew M. Mulhern
  • Patent number: 8846918
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: September 30, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, David Kay
  • Patent number: 8846917
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: September 30, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, David Matthew Shaw
  • Publication number: 20140287916
    Abstract: A compound of formula (I), wherein R1 to R4 are, for example, each hydrogen, R5 is, for example, an unsubstituted aromatic 6-membered heterocycle; R6 is, for example, hydrogen; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.
    Type: Application
    Filed: October 31, 2012
    Publication date: September 25, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Olivier Loiseleur, Thomas Pitterna, Anthony Cornelius O'Sullivan, Torsten Luksch
  • Patent number: 8841450
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: September 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Michael Edward O'Donnell, Simon Robert Everitt
  • Patent number: 8841449
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: September 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, Ronald Knegtel
  • Patent number: 8841287
    Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Grant
    Filed: June 11, 2009
    Date of Patent: September 23, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xiaohu Zhang
  • Patent number: 8841337
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: September 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Pierre-Henri Storck, Joanne Pinder, John R. Studley
  • Publication number: 20140275539
    Abstract: Provided herein are stabilized radioiodinated and astatinated compounds, and to methods for their preparation.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Ground Fluor Pharmaceuticals, Inc.
    Inventor: Stephen G. DiMagno
  • Publication number: 20140274692
    Abstract: A compound of formula (I) wherein R1 to R4 are, for example, each hydrogen, R5 is, for example, a substituted phenol; R6 is, for example, hydrogen; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 is, for example, A1 is N or C—X, A3 is C—X, and A2, A4 and A5 are C—H, where X, is, for example, halogen; and its use as a pesticidal agent.
    Type: Application
    Filed: October 31, 2012
    Publication date: September 18, 2014
    Applicant: Syngenta Participations AG
    Inventors: Olivier Loiseleur, Thomas Pitterna, Anthony Cornelius O'Sullivan, Torsten Luksch, Anna Kickova
  • Publication number: 20140275100
    Abstract: The invention provides compounds of formula I, (I) wherein: R represents a cyclic group selected from phenyl, heteroaryl, heterocyclyl and C 3-6 cycloalkyl; 10 wherein each cyclic group is optionally substituted with from 1 to 3 substituents selected from halo, C -6 alkyl optionally substituted with 1-3 halogen atoms, phenyl, C -6 alkoxy optionally substituted with 1-3 halogen atoms, cyano, heteroaryl 1a and heterocyclyl 1a; and wherein each cyclic group is optionally fused to a benzene ring or a 5- or 16-membered heteroaromatic or heterocyclic ring each containing from 1 to 3 heteroatoms (selected from N, O and S); and when the group is substituted the substitution may occur anywhere on the optionally fused ring system as a whole; and wherein heterocyclyl and heterocyclyl 1a may additionally be substituted with ?O; 20 X represents a bond or C -6 alkylene (which may be straight or branched); R 2 represents H or C -6 alkyl; R 3 represents H or C -6 alkyl; Y represents a bond or C -6 alkylene (which may be stra
    Type: Application
    Filed: October 26, 2012
    Publication date: September 18, 2014
    Inventors: Karl Richard Gibson, Dafydd Rhys Owen
  • Patent number: 8822683
    Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: September 2, 2014
    Assignee: G1 Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay C. Strum
  • Patent number: 8815926
    Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: August 26, 2014
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Lv Liao, Robert Mah, Liang Mao, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Publication number: 20140234939
    Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.
    Type: Application
    Filed: December 23, 2013
    Publication date: August 21, 2014
    Applicant: Northwestern University
    Inventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar