Chalcogen Bonded Directly To Diazine Ring Carbon Patents (Class 544/354)
  • Patent number: 10487062
    Abstract: A regioselective one-step process for the synthesis of 2-hydroxyquinoxaline of Formula (1) or tautomers thereof: comprising reacting 1,2-phenylenediamine of Formula (2): with an excess amount of glyoxylic acid, glyoxylic acid monohydrate, or a 2,2-dialkoxyacetic acid of Formula (3): at a low temperature; wherein R1 and R2 are as defined in the specification.
    Type: Grant
    Filed: August 1, 2019
    Date of Patent: November 26, 2019
    Assignee: DEVELOPMENT CENTER FOR BIOTECHNOLOGY
    Inventors: Shao-Zheng Peng, Yuan-Ting Cho, Pao-Chiung Hong
  • Patent number: 9598356
    Abstract: Cyhalofop is prepared by coupling 2-(4-hydroxyphenoxy)propionic acid and 3,4-difluorobenzonitrile with base in a polar aprotic solvent in the presence of a phase-transfer catalyst.
    Type: Grant
    Filed: February 24, 2011
    Date of Patent: March 21, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Ronald B. Leng, Eric W. Otterbacher, Herbert N. Praay
  • Patent number: 9233937
    Abstract: Arylpyrazinone derivatives of formula (I), as insulin secretion stimulators, the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.
    Type: Grant
    Filed: July 22, 2014
    Date of Patent: January 12, 2016
    Assignee: MERCK PATENT GMBH
    Inventors: Gerard Botton, Eric Valeur, Christine Charon, Micheline Kergoat, Samer Elbawab
  • Publication number: 20150148342
    Abstract: The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
    Type: Application
    Filed: November 26, 2014
    Publication date: May 28, 2015
    Applicant: INCYTE CORPORATION
    Inventors: Eddy W. Yue, Andrew P. Combs, Brent Douty
  • Publication number: 20150148344
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
  • Patent number: 9040533
    Abstract: The present disclosure relates to Oxime-Substituted Quinoxaline-Type Piperidine Compounds, such as those of Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R20, R21, Q, Y1, Z, A, B, and a are as defined herein; compositions comprising an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: May 26, 2015
    Assignees: Purdue Pharma L.P., Shionogi & Co., Ltd.
    Inventors: Jeffrey Michael Marra, Naoki Tsuno, Tatsuhiko Ueno, Xiaoming Zhou
  • Publication number: 20150141643
    Abstract: The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.
    Type: Application
    Filed: July 14, 2014
    Publication date: May 21, 2015
    Inventors: Kouki FUCHINO, R. Richard GOEHRING, Akira MATSUMURA, Bin SHAO, Yoshiyuki TAODA, Naoki TSUNO, John William Frank WHITEHEAD, Jiangchao YAO
  • Patent number: 8993779
    Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • Publication number: 20150087513
    Abstract: The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein A1, A2, A3, A4, A5, X, R1, R2 and R6 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), and to their use for controlling weeds, in particular in crops of useful plants.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 26, 2015
    Applicant: SYNGENTA LIMITED
    Inventors: Glynn Mitchell, Olivia Anabelle Sageot
  • Publication number: 20150087644
    Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 26, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
  • Publication number: 20150080373
    Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
  • Publication number: 20150031685
    Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
    Type: Application
    Filed: March 5, 2013
    Publication date: January 29, 2015
    Applicant: Dr. Reeddy's Laboratories Ltd.
    Inventors: Pradip Kumar Sasmal, Chintakunta Vamseekrishna, Vijay Potluri, Ashok Tehim, Yonghua Gai, Hang Zhang
  • Publication number: 20150011529
    Abstract: The disclosure relates to Azetidine-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein the R1, R2, R3, Q, Y1, Z, A, B, a, and b are as defined herein, compositions comprising an effective amount of an Azetidine-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an Azetidine-Substituted Quinoxaline-Type Piperidine Compound.
    Type: Application
    Filed: November 30, 2012
    Publication date: January 8, 2015
    Inventors: Laykea Tafesse, Naoki Tsuno, Xiaoming Zhou
  • Publication number: 20140378305
    Abstract: Compounds of formula wherein the substituents are as defined in claim 1, and related compositions, methods of use and processes of preparation.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Applicant: SYNGENTA LIMITED
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Publication number: 20140371201
    Abstract: The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: June 11, 2014
    Publication date: December 18, 2014
    Inventors: Matthew WEISS, Alessandro BOEZIO, Christiane BOEZIO, John R. BUTLER, Margaret Yuhua CHU-MOYER, Erin F. DIMAURO, Thomas DINEEN, Russell GRACEFFA, Angel GUZMAN-PEREZ, Hongbing HUANG, Charles KREIMAN, Daniel LA, Isaac E. MARX, Benjamin Charles MILGRIM, Hanh Nho NGUYEN, Emily PETERSON, Karina ROMERO, Brian SPARLING
  • Patent number: 8912190
    Abstract: The present invention relates to compounds that are late 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 R1, R2, R3, and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: December 16, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Dmitry Koltun, Eric Parkhill, Jeff Zablocki
  • Publication number: 20140364429
    Abstract: Provided are compounds antiviral compounds represented by formula Ia and Ib: that are highly potent as HCV NS5A inhibitors, where the structural variables are as defined herein. These compounds are useful in, for example, inhibiting Hepatitis C virus and treating Hepatitis C virus infections.
    Type: Application
    Filed: June 6, 2014
    Publication date: December 11, 2014
    Applicant: AB PHARMA LTD.
    Inventor: Zheng-Yun James ZHAN
  • Publication number: 20140359951
    Abstract: An agent for oxidative coloring of keratin-containing fibers, in particular human hair, includes as oxidation dye precursor of the developer type at least one compound of formula (I).
    Type: Application
    Filed: August 22, 2014
    Publication date: December 11, 2014
    Inventors: Antje Gebert, Annika Koenen
  • Patent number: 8865623
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Grant
    Filed: January 6, 2010
    Date of Patent: October 21, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Publication number: 20140309231
    Abstract: A nitrogen-containing heterocyclic compound represented by formula (I-A): (wherein R1A represents lower alkyl which may be substituted with lower alkoxy, R3A represents lower alkyl substituted with fluorine atom(s), and R4A represents an optionally substituted aromatic heterocyclic group) or the like, or a pharmaceutically acceptable salt thereof; and the like, are provided.
    Type: Application
    Filed: November 9, 2012
    Publication date: October 16, 2014
    Applicant: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Toshimi Kanai, Kenji Uchida, Masakazu Honma, Yuichi Fukuda
  • Patent number: 8859552
    Abstract: The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.
    Type: Grant
    Filed: June 10, 2013
    Date of Patent: October 14, 2014
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey
  • Publication number: 20140303150
    Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
    Type: Application
    Filed: December 22, 2011
    Publication date: October 9, 2014
    Applicant: LEO Laboratories Limited
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
  • Publication number: 20140275065
    Abstract: The present invention is directed to compounds of Formula I: wherein ring A is phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl, or indazolyl; R1 is H, alkyl, alkoxy, hydroxyalkylene, OH, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl, or dialkylamino; R2 is H, alkyl, alkoxy, hydroxyalkylene, or halo; Z is NH, N-alkyl, or O; R5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, alkoxy, or halo; and n is 0 or 1. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Inventors: Heather R. Coate, Curt A. Dvorak, Terry P. Lebold, Cathy Preville, Brock T. Shireman
  • Publication number: 20140256549
    Abstract: The present invention relates to esters of carboxylic acid agrochemicals comprising a labile protecting group and having formula (I). Certain of the esters of carboxylic acid agrochemicals do not undergo hydrolysis to a significant degree in the dark, but are cleaved to regenerate the parent carboxylic acid agrochemical when exposed to light. Others of the esters of carboxylic acid agrochemicals undergo hydrolysis under both light and dark conditions. The present invention further relates to methods for the controlled release of a carboxylic acid agrochemicals, and to methods of controlling unwanted plants comprising applying to the unwanted plants an ester of a carboxylic acid agrochemical.
    Type: Application
    Filed: October 11, 2012
    Publication date: September 11, 2014
    Applicant: MONSANTO TECHNOLOGY LLC
    Inventor: David A. Morgenstern
  • Publication number: 20140243519
    Abstract: The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity.
    Type: Application
    Filed: August 16, 2012
    Publication date: August 28, 2014
    Inventors: Nobuyoshi Yasuda, Jeffrey T. Kuethe, Guy Humphrey, Gregory L. Beutner, Yong-Li Zhong, Edward Cleator, Carl Baxter
  • Publication number: 20140243302
    Abstract: Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 28, 2014
    Applicants: MERCK SHARP & DOHME CORPORATION, KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Yasumichi Fukuda, David E. Kaelin, JR., Sheo B. Singh
  • Publication number: 20140228371
    Abstract: The invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.
    Type: Application
    Filed: January 29, 2014
    Publication date: August 14, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
  • Publication number: 20140221348
    Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.
    Type: Application
    Filed: March 17, 2014
    Publication date: August 7, 2014
    Applicant: Basilea Pharmaceutica AG
    Inventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
  • Publication number: 20140221345
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: August 7, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • Publication number: 20140200343
    Abstract: The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams from the intermediates. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 17, 2014
    Inventors: Feng Xu, Guy Humphrey, Tao Pei, Zhiguo Jake Song, Tao Wang, Laura Artino
  • Publication number: 20140194422
    Abstract: The disclosure relates to piperazine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidase.
    Type: Application
    Filed: June 12, 2012
    Publication date: July 10, 2014
    Applicant: EMORY UNIVERSITY
    Inventors: Thota Ganesh, Aiming Sun, Susane M. Smith, John David Lambeth
  • Publication number: 20140194433
    Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 10, 2014
    Applicant: BASF SE
    Inventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
  • Publication number: 20140187544
    Abstract: The present disclosure relates to Oxime-Substituted Quinoxaline-Type Piperidine Compounds, such as those of Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R20, R21, Q, Y1, Z, A, B, and a are as defined herein; compositions comprising an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound.
    Type: Application
    Filed: December 23, 2013
    Publication date: July 3, 2014
    Applicants: Shionogi & Co., Ltd., Purdue Pharma L.P.
    Inventors: Jeffrey Michael MARRA, Naoki Tsuno, Tatsuhiko Ueno, Xiaoming Zhou
  • Patent number: 8753550
    Abstract: Pigment compositions containing organic pigments with an outstanding migration-free property and an excellent rheology at high concentration, and derivatives thereof containing heterocyclic substituents. The pigment compositions contains (a) carbon black or an organic pigment containing a chromophore Q1 of the following formula, wherein Z1 and Z2 are O or N—, C· is a carbon atom with an electron in a p orbital, and n is an integer from 1 to 4; and (b) a compound containing a chromophore of the following formula (II), wherein Q2 is an m-valent residue of carbon black or of the chromophore Q1; G1 is preferably and R1, R2, R3, R4, R5, R6, and R8 are preferably all H; m is an integer from 1 to 4. The pigment compositions can be used as rheology modifiers, preferably for pigmented coating compositions.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: June 17, 2014
    Assignee: BASF SE
    Inventors: Céline Vairon, Marc Maurer, Ulrich Veith, Sascha Gysin
  • Patent number: 8729081
    Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.
    Type: Grant
    Filed: October 12, 2009
    Date of Patent: May 20, 2014
    Assignee: VM Discovery Inc.
    Inventor: Jay Jie-Qiang Wu
  • Publication number: 20140135494
    Abstract: The present invention provides oxazine compounds, method of using and method of making oxazine compounds and its pharmaceutical use.
    Type: Application
    Filed: January 20, 2014
    Publication date: May 15, 2014
    Applicant: SOUTHERN METHODIST UNIVERSITY
    Inventors: Edward R. Biehl, Haribabu Ankati, Sukanta Kamila
  • Patent number: 8722670
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: May 13, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Dalton King, Richard E. Olson, John E. Macor, Imadul Islam, Srinivasan Thangathirupathy, Jayakumar Sankara Warrier
  • Patent number: 8697407
    Abstract: The present invention relates to agents that find use in the treatment, management, and/or study of cancer. In particular, the present invention relates to agents (e.g., small molecules, nucleic acids) that affect MMSET expression or activity.
    Type: Grant
    Filed: February 11, 2011
    Date of Patent: April 15, 2014
    Assignee: The Regents of The University of Michigan
    Inventors: Arul M. Chinnaiyan, Sooryanaryana Lnu, Qi Cao, Irfan Asangani
  • Patent number: 8691820
    Abstract: The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer.
    Type: Grant
    Filed: June 23, 2011
    Date of Patent: April 8, 2014
    Assignee: Curis, Inc.
    Inventors: Changgeng Qian, Xiong Cai, Haixiao Zhai
  • Patent number: 8685959
    Abstract: Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: April 1, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jay Powers, Ju Yang
  • Patent number: 8674097
    Abstract: The present invention relates to compounds of formula (I) wherein X, Y, Z, R1, R2, R3 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diabetes, metabolic syndrome, obesity, cancer, inflammation.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: March 18, 2014
    Assignee: Merck Patent GmbH
    Inventors: Daniel Cravo, Sophie Hallakou-Bozec, Franck Lepifre
  • Publication number: 20140073792
    Abstract: An agricultural or horticultural fungicide contains as an active ingredient thereof at least one compound selected from the group consisting of nitrogenated heterocyclic compounds represented by formula (I) (wherein, R represents a group represented by CR1R2R3 or a cyano group, R1 to R3 represent hydrogen atoms, alkyl groups or hydroxyl groups, or the like, X1 represents a halogeno group or the like, m represents an integer of 0 to 5, X2 represents a halogeno group or the like, n represents an integer of 0 to 3, B represents a carbon atom or a nitrogen atom, D represents a 5- to 7-membered hydrocarbon ring, and A1 to A4 represent carbon atoms or nitrogen atoms, provided that A1 to A4 do not all represent carbon atoms when B represents a carbon atom) and salts thereof.
    Type: Application
    Filed: May 17, 2012
    Publication date: March 13, 2014
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Kotaro Shibayama, Raito Kuwahara, Motoaki Sato, Satoshi Nishimura, Yasuyuki Shiinoki, Masahiro Yokoyama, Juri Kitamura
  • Patent number: 8669363
    Abstract: The present invention provides oxazine compounds, method of using and method of making oxazine compounds and its pharmaceutical use.
    Type: Grant
    Filed: March 23, 2012
    Date of Patent: March 11, 2014
    Assignee: Southern Methodist University
    Inventors: Edward R. Biehl, Haribabu Ankati, Sukanta Kamila
  • Patent number: 8664221
    Abstract: The object aims to find a novel pharmacological activity of a novel 1,2,3,4-tetrahydroquinoxaline derivative which contains, as a substituent, a phenyl group having a sulfonic acid ester structure introduced therein. A compound represented by general formula (1) or a salt thereof is useful as a glucocorticoid receptor agonist, particularly as a therapeutic agent for diseases against which a glucocorticoid receptor agonist (e.g., a steroid) is believed to be effective, such as inflammatory bone/joint diseases, inflammatory ophthalmic diseases (inflammatory ophthalmic diseases in the anterior or posterior segment of an eye).
    Type: Grant
    Filed: September 11, 2009
    Date of Patent: March 4, 2014
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Masatomo Kato, Miwa Takai, Takahiro Matsuyama, Tatsuji Kurose, Yumi Hagiwara, Kenji Oki, Mamoru Matsuda, Toshiyuki Mori
  • Publication number: 20140045830
    Abstract: The disclosure relates to Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein R1, R2, Qa, Y1, Z, A, B, Qx, E, G, J, M, U, W, and a are as defined herein, compositions comprising an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compound.
    Type: Application
    Filed: July 26, 2013
    Publication date: February 13, 2014
    Applicants: Shionogi & Co., Ltd., Purdue Pharma L.P.
    Inventors: Naoki TSUNO, Tatsuhiko Ueno, Xiaoming Zhou
  • Publication number: 20140045855
    Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: August 2, 2013
    Publication date: February 13, 2014
    Applicant: AMGEN INC.
    Inventors: Kaustav BISWAS, Jian J. CHEN, Vijay Keshav GORE, Scott HARRIED, Daniel B. HORNE, Matthew R. KALLER, Vu Van MA, Kelvin SHAM, Wenge ZHONG
  • Patent number: 8604040
    Abstract: Pyridinylcarboxylic acid derivatives of the formula (I) in which the symbols A, X, Y1, Y2, Y3, L1, L2, RG, and R1 are each as defined in the description, and also salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer CropScience AG
    Inventors: Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Nicola Rahn, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Ulrike Wachendorff-Neumann
  • Patent number: 8586739
    Abstract: Substituted bicyclic heteroaryls having the general structure: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: November 19, 2013
    Assignee: Amgen Inc.
    Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian S. Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer L. Seganish, Youngsook Shin, Dawei Zhang
  • Publication number: 20130303537
    Abstract: A 1,2,3,4-tetrahydroquinoxaline compound represented by the following formula: In the formula (1), R1 represents substituents such as a halogen, an alkyl, a cycloalkyl, an aryl or a heterocyclic group; p represents 0 to 5; R2 represents substituents such as a halogen, an alkyl, a hydroxyl or an alkoxy group; q represents 0 to 2; R3 represents substituents such as hydrogen, an alkyl, an alkenyl, an alkylcarbonyl or an arylcarbonyl group; R4 and R5 independently represent substituents such as hydrogen, a halogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; R6 represents substituents such as hydrogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; A represents an alkylene; R7 represents OR8, NR8R9, SR8, S(O)R8, S(O)2R8; R8 and R9 independently represent substituents such as hydrogen, an alkyl or an alkenyl; and X represents O or S.
    Type: Application
    Filed: July 9, 2013
    Publication date: November 14, 2013
    Inventors: Mamoru MATSUDA, Toshiyuki MORI, Kenji KAWASHIMA, Minoru YAMAMOTO, Masatomo KATO, Miwa TAKAI, Masato NAGATSUKA, Sachiko KOBAYASHI
  • Publication number: 20130274265
    Abstract: Compounds of Formula (I): where R1, R2, R5, a, and b are disclosed herein, and pharmaceutically acceptable derivatives thereof (a “Substituted-Quinoxaline-Type Bridged-Piperidine Compound”), compositions comprising an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound.
    Type: Application
    Filed: June 11, 2013
    Publication date: October 17, 2013
    Inventors: Kouki FUCHINO, Naoki TSUNO, John W.F. WHITEHEAD, Jiangchao YAO