Nitrogen Attached Indirectly To The Six-membered Hetero Ring Through The Directly Attached Nitrogen By Nonionic Bonding Patents (Class 546/162)
  • Patent number: 9029395
    Abstract: Tetrahydroquinoline derivatives, pharmaceutical compositions containing such compounds and to their use in therapy.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: May 12, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Robert J. Watson
  • Publication number: 20150094333
    Abstract: Disclosed are compounds having the formula: wherein R1, R2R3, R4 and R5 are as defined herein, and methods of making and using the same.
    Type: Application
    Filed: September 13, 2013
    Publication date: April 2, 2015
    Inventors: Linda N. Casillas, Michael P. Demartino, Pamela A. Haile, John F. Mehlmann, Joshi M. Ramanjulu, Robert Singhaus, JR.
  • Patent number: 8993554
    Abstract: Tetrahydroquinoline compounds, pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: March 31, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Jonathan Thomas Seal
  • Patent number: 8993767
    Abstract: The present invention relates to multiphoton activable organic compounds responding to the following formula (I). The present invention also relates to a method of synthesizing the compounds of the invention, to an aqueous solution comprising at least one compound of the invention, and to their specific uses. The present invention also concerns a method of liberating organic ligands, said method involving the step of irradiating a compound according to the invention.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: March 31, 2015
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Peter Dalko, Morgane Petit, David Ogden, Francine Acher
  • Patent number: 8980892
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: March 17, 2015
    Assignees: Syngenta Crop Protection LLC, Syngenta Limited
    Inventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
  • Publication number: 20150060787
    Abstract: Provided is a compound represented by Formula 1, Formula 2, or Formula 3:
    Type: Application
    Filed: May 21, 2014
    Publication date: March 5, 2015
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Jun-Ha PARK, Seok-Hwan HWANG, Young-Kook KIM, Hye-Jin JUNG, Eun-Young LEE, Jong-Woo KIM, Jin-O LIM, Sang-Hyun HAN, Eun-Jae JEONG, Soo-Yon KIM
  • Publication number: 20150038714
    Abstract: The present invention relates to novel and concise process for the construction of chiral 3-substituted tetrahyroquinoline derivatives based on proline catalyzed asymmetric ?-functionalization of aldehyde, followed by in situ reductive cyclization of nitro group under catalytic hydrogenation condition with high optical purities. Further the invention relates to conversion of derived chiral 3-substituted tetrahydroquinoline derivatives into therapeutic agents namely (?)-sumanirole (96% ee) and 1-[(S)-3-(di-methylamino)-3,4-dihydro-6,7-dimethoxy-quinolin-1(2H)-yl]propanone[(S)-903] (92% ee).
    Type: Application
    Filed: March 19, 2013
    Publication date: February 5, 2015
    Applicant: Council of Scientific & Industrial Research
    Inventors: Varun Rawat, Senthil Kumar Boopathi, Arumugam Sudalai
  • Patent number: 8946443
    Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a C1 to C6 alkyl group which may be substituted by one to three groups selected from substituent group A, or the like (substituent group A: a hydroxy group, a halogeno group, a cyano group, a nitro group, an amino group, a carboxy group, a C1 to C3 alkyl group, etc.); R2, R3, and R8 each independently represent a hydrogen atom or a C1 to C3 alkyl group; R4, R5, R6, R7, R9, and R10 each independently represent a hydrogen atom or the like; and R11 represents a hydrogen atom or the like, has TAFIa enzyme inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, or the like.
    Type: Grant
    Filed: March 14, 2011
    Date of Patent: February 3, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Tsutomu Nagata, Jun Kobayashi, Yoshiyuki Onishi, Masamichi Kishida, Kengo Noguchi
  • Patent number: 8940724
    Abstract: Substituted bicyclic heteroaryls 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, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: January 27, 2015
    Assignee: Amgen Inc.
    Inventors: Timothy D. Cushing, Paul John Dransfield, Felix Gonzalez Lopez de Turiso, Michael G. Johnson, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
  • Patent number: 8927577
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: January 6, 2015
    Assignee: Pfizer Inc.
    Inventors: Mary Didiuk, Kevin J. Filipski, Angel Guzman-Perez, Esther C. Lee, Jeffrey A. Pfefferkorn, Benjamin Stevens, Meihua Tu
  • Publication number: 20140350048
    Abstract: Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed.
    Type: Application
    Filed: January 14, 2013
    Publication date: November 27, 2014
    Inventors: Michael K. Riscoe, Rolf W. Winter, Sovitj Pou, David J. Hinrichs, Jane Xu Kelly, Yuexin Li, Aaron Nilsen
  • Patent number: 8877741
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Publication number: 20140309257
    Abstract: The invention provides methods of inhibiting the growth or metastasis of cancer in a mammal by inhibiting TopoIIa in the mammal. The invention also provides small molecule inhibitors of TopoIIa useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds and methods of using the same.
    Type: Application
    Filed: November 13, 2012
    Publication date: October 16, 2014
    Inventor: Daniel V. Labarbera
  • Publication number: 20140303206
    Abstract: The invention provides certain 3-pyridyl carboxamide-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: October 1, 2012
    Publication date: October 9, 2014
    Inventors: Michael D. Altman, Kaleen Konrad Childers, Anthony Donofrio, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
  • Patent number: 8846675
    Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.
    Type: Grant
    Filed: May 3, 2012
    Date of Patent: September 30, 2014
    Assignee: Cymabay Therapeutics, Inc.
    Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
  • Publication number: 20140288120
    Abstract: A compound having the following formula or a pharmaceutically acceptable salt thereof: where: R? is a hydrogen atom or a (C1-C4)alkyl group; n? is 1 or 2; n is 1, 2, or 3; R independently represents a hydrogen atom, a halogen atom, or a group selected from a (C1-C3)alkyl group, a —CN group, a hydroxyl group, a —NR1R2 group, a —COOR1 group, a (C1-C3)fluoroalkyl group, a —NO2 group, a (C1-C3)fluoroalkoxy, and a (C1-C4)alkoxy group; R? is a hydrogen atom, a halogen atom, or a group selected from a (C1-C3)alkyl group, a —COOR1 group, a —NO2 group, a —NR1R2 group, a (C1-C4)alkoxy group, and a CN group; R1 and R2 are a hydrogen atom or a (C1-C3)alkyl group; with the proviso that when R and R? are not simultaneously a hydrogen atom: when n is 1, R is not a methyl group in an ortho or para position with respect to N, when R? is a hydrogen atom, R is not a bromine atom or a chlorine atom, and when R is a hydrogen atom, R is not a methyl or ethyl group, a —COOH group, a —COOC2H5 group, or a bromine atom that is
    Type: Application
    Filed: April 18, 2014
    Publication date: September 25, 2014
    Applicants: SOCIETE SPLICOS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE MONTPELLIER 2
    Inventors: Jamal TAZI, Florence MAHUTEAU, Romain NAJMAN, Didier SCHERRER, Noelie CAMPOS, Aude GARCEL
  • Publication number: 20140256949
    Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, R4 and R5 are as defined herein, and methods of making and using the same.
    Type: Application
    Filed: May 21, 2014
    Publication date: September 11, 2014
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Linda N. CASILLAS, Adam Kenneth Charnley, Pamela A. Haile, Terry Vincent Hughes, Robert W. Marquis, JR., John F. Mehlmann, Michael Reilly, Joseph J. Romano, Robert R. Singhaus, JR.
  • Patent number: 8822691
    Abstract: To provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Carboxamides represented by the following Formula (I) and use thereof as pesticides and an animal parasite control agent: wherein each substituent is as defined in the specification.
    Type: Grant
    Filed: July 10, 2010
    Date of Patent: September 2, 2014
    Assignee: Bayer CropScience AG
    Inventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
  • Publication number: 20140243322
    Abstract: Described herein are compounds capable of modulating one or more biomolecules substantially simultaneously, e.g., modulating two or more binding domains (e.g., bromodomains) on a protein or on different proteins.
    Type: Application
    Filed: February 28, 2014
    Publication date: August 28, 2014
    Applicant: Coferon, Inc.
    Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
  • Publication number: 20140243286
    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
    Type: Application
    Filed: February 28, 2014
    Publication date: August 28, 2014
    Applicant: Coferon, Inc.
    Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
  • Publication number: 20140235857
    Abstract: The present invention pertains to a compound represented by a formula (I) and a method for producing thereof (in the formula, Ax is an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, Ay is a hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a cycloalkyl group, an alkenyl group having 2 to 18 carbon atoms, an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, or the like. Ax and Ay optionally bond to each other to form a ring, and Q is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like.).
    Type: Application
    Filed: April 27, 2012
    Publication date: August 21, 2014
    Applicant: ZEON CORPORATION
    Inventors: Kei Sakamoto, Kumi Okuyama, Yasushi Nakano
  • Publication number: 20140235671
    Abstract: Compounds of the invention are of the formula wherein: is a double bond and X is C; or is a single bond and X is N, CH or CQR1; and wherein: n is 1 to 10; R is H or QR1; each R? is independently selected from H and QR1; each Q is independently selected from a bond, CO, NH, S, SO, SO2 or O; each R1 is independently selected from C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl or C1-C10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.
    Type: Application
    Filed: April 30, 2014
    Publication date: August 21, 2014
    Applicant: Karus Therapeutics Limited
    Inventors: Stephen Joseph SHUTTLEWORTH, Cyrille Davy TOMASSI
  • Publication number: 20140200227
    Abstract: The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
    Type: Application
    Filed: January 14, 2014
    Publication date: July 17, 2014
    Applicant: INCYTE CORPORATION
    Inventors: Chu-Biao Xue, Yun-Long Li, Hao Geng, Jun Pan, Anlai Wang, Ke Zhang, Wenqing Yao, Fenglei Zhang, Jincong Zhuo
  • Patent number: 8754053
    Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: June 17, 2014
    Assignee: Syngenta Crop Protection LLC
    Inventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
  • Publication number: 20140142114
    Abstract: The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X2, X3, X4, X5, X6, X7 and X8 are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.
    Type: Application
    Filed: November 19, 2013
    Publication date: May 22, 2014
    Applicant: Merial Limited
    Inventors: Charles Q. Meng, Alan Long, Scot Huber, Srinivas Reddy Gurrala, Douglas Edward Wilkinson, Gregory Pacofsky
  • Publication number: 20140142266
    Abstract: The present invention relates to a polymerizable compound represented by a formula (I). The present invention provides a polymerizable compound, a polymerizable composition, a polymer, and an optically anisotropic article that are capable of obtaining an optical film having a low melting point, having excellent solubility, capable of being manufactured at low cost, and capable of uniform polarized light conversion across a broad wavelength region. [In formula: Y1 to Y6 are independently a chemical single bond, —O—, —O—C(?O)—, —C(?O)—O— etc.; G1 and G2 are independently a divalent C1-C20 aliphatic group etc.; Z1 and Z2 are independently C2-C10 alkenyl group that is substituted with a halogen atom etc.; Ax is a C2-C30 organic group that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring; Ay is a hydrogen atom, a C1-C20 alkyl group, a C2-C20 alkenyl group, a C3-C12 cycloalkyl group etc.; A1 is a trivalent aromatic group etc.
    Type: Application
    Filed: April 27, 2012
    Publication date: May 22, 2014
    Applicant: ZEON CORPORATION
    Inventors: Kei Sakamoto, Kumi Okuyama
  • Publication number: 20140135338
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: July 12, 2012
    Publication date: May 15, 2014
    Applicant: PFIZER INC.
    Inventors: Mary Didiuk, Kevin J. Filipski, Angel Guzman-Perez, Esther C. Lee, Jeffrey A. Pfefferkorn, Benjamin Stevens, Meihua Tu
  • Publication number: 20140134235
    Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.
    Type: Application
    Filed: October 14, 2013
    Publication date: May 15, 2014
    Applicant: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima BARUAH, Dibyendu DE, Ish Kumar KHANNA, Sivaram PILLARISETTI, Santanu MAITRA, Christopher W. ALEXANDER, Jennepalli SREENU, Indu Dagar, Shanavas Alikunju
  • Patent number: 8716289
    Abstract: Compound corresponding to general formula (I): in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or NR8R9 group; n is an integer equal to 1, 2 or 3 and m is an integer equal to 1 or 2; A is a covalent bond or a C1-8-alkylene group; R1 is a phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, naphthyl, quinolinyl, isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl or naphthyridinyl group, this group being optionally substituted; R3 is a hydrogen or fluorine atom, a C1-6-alkyl group or a tritluoromethyl group; R4 is a group selected from furanyl, pyrrolyl, thienyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, imidazole, triazolyl, tetrazolyl, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone and triazolone, this group being optionally substituted; in the form of a base or o
    Type: Grant
    Filed: November 13, 2009
    Date of Patent: May 6, 2014
    Assignee: Sanofi
    Inventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Mourad Saady, Julien Vache, Corinne Veronique, Philippe Yaiche
  • Publication number: 20140113931
    Abstract: Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Application
    Filed: March 15, 2013
    Publication date: April 24, 2014
    Applicant: Portola Pharmaceuticals, Inc.
    Inventor: Portola Pharmaceuticals, Inc.
  • Publication number: 20140114069
    Abstract: The present invention relates to electroluminescent compounds of formula 1 where A and/or B represent fluorene, carbazole, dibenzo[b,d]thiophene or dibenzo[b,d]furan derivatives and L1, X1, Ar1, Ar2, R5, R6 and R7 are as defined herein, and organic electroluminescent devices comprising the same. The compounds according to the present invention have an advantage in manufacturing an organic electroluminescent device which has a high luminous efficiency and a long operational lifetime.
    Type: Application
    Filed: March 23, 2012
    Publication date: April 24, 2014
    Applicant: Ronm and Haas Electronic Materials Korea Ltd.
    Inventors: Hee-Sook Kim, Seok-Keun Yoon, Kyung-Joo Lee, Hong-Yoep Na, Nam-Kyun Kim, Young-Jun Cho, Hyuck-Joo Kwon, Bong-Ok Kim
  • Publication number: 20140066459
    Abstract: Tetrahydroquinoline compounds pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Application
    Filed: May 2, 2012
    Publication date: March 6, 2014
    Applicant: GlaxoSmithkline LLC
    Inventors: Dominique Amans, Emmanuel Hubert Demont, Katherine Louise Jones, Jonathan Thomas Seal, Ann Louise Walker
  • Patent number: 8648195
    Abstract: An objective of the present invention is to provide a crystal of 2-ethyl-3,7-dimethyl-6-(4-(trifluoromethoxy)phenoxy)quinoline-4-yl methyl carbonate having stable physicochemical properties. The objective is attained by a crystal of 2-ethyl-3,7-dimethyl-6-(4-(trifluoromethoxy)phenoxy)quinoline-4-yl methyl carbonate that exhibits a diffraction peak pattern shown in FIG. 1 as determined by powder X-ray diffractometry.
    Type: Grant
    Filed: February 22, 2011
    Date of Patent: February 11, 2014
    Assignees: Nippon Kayaku Co., Ltd., Meiji Seika Pharma Co., Ltd.
    Inventors: Kouki Tanigakiuchi, Mikio Sekiguchi, Hiroki Hotta, Shizuo Shimano, Akinori Morikawa, Kazumi Yamamoto, Nozomu Nakanishi, Nobuto Minowa, Takashi Watanabe
  • Publication number: 20140039006
    Abstract: Tetrahydroquinoline derivatives, pharmaceutical compositions containing such compounds and to their use in therapy.
    Type: Application
    Filed: April 19, 2012
    Publication date: February 6, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Robert J. Watson
  • Publication number: 20140031336
    Abstract: Tetrahydroquinoline compounds, pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Application
    Filed: April 19, 2012
    Publication date: January 30, 2014
    Applicant: Glaxosmithkline LLC
    Inventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Jonathan Thomas Seal
  • Publication number: 20140012002
    Abstract: The present invention relates to compounds of general formula I wherein R100 and R200 are each independently hydrogen, C1-C10-alkyl which in case of C2-alkyl may be interrupted by one and in case of C3-C10-alkyl by one or two nonadjacent oxygen atoms, C5-C7-cycloalkyl, aryl, aryl-C1-C10-alkyl or aryloxy-C1-C10-alkyl, D is an m-valent (m=1, 2 or 3) donor moiety which comprises at least one carbon-carbon or carbon-heteroatom double bond and/or at least one unfused or fused carbo- or heterocyclic ring, A is an acceptor moiety which comprises at least one carbon-carbon or carbon-heteroatom double bond and/or at least one unfused or fused carbo- or heterocyclic ring, and the donor moiety D and the acceptor moiety A are ?-conjugated to one another. Furthermore, the present invention relates to the use of compounds of formula I for producing dye-sensitized solar cells and to dye-sensitized solar cells comprising compounds of formula I.
    Type: Application
    Filed: July 1, 2013
    Publication date: January 9, 2014
    Inventors: Ingmar BRUDER, Robert Send, Simona Urnikaite, Tadas Malinauskas, Maryte Daskeviciene, Vytautas Getautis
  • 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
  • Publication number: 20130317218
    Abstract: The present invention relates to novel bicyclic thiazole compounds that inhibit Traf2- and Nck-interacting kinase (TNIK), and as such are useful as TNIK inhibitors administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. The bicyclic thiazole compounds are showed by a next formula (I). (wherein R1, R2, R3 and Q are as defined in the specification), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 24, 2012
    Publication date: November 28, 2013
    Inventors: Masaaki Sawa, Hideki Moriyama, Tesshi Yamada, Miki Shitashige, Yusuke Kawase, Yuko Uno
  • Publication number: 20130310348
    Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).
    Type: Application
    Filed: July 25, 2013
    Publication date: November 21, 2013
    Applicants: State University
    Inventors: David H. Peyton, Steven Burgess
  • Publication number: 20130310393
    Abstract: Disclosed are heteroaryl compounds of Formula (I), (I), or pharmaceutically acceptable salts thereof, wherein Z is CH or N; W is CR3 or N; and R1, R2, and R3 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: September 23, 2011
    Publication date: November 21, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Audris Huang
  • Publication number: 20130296363
    Abstract: Provided herein are compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Application
    Filed: August 31, 2011
    Publication date: November 7, 2013
    Applicant: AMBIT BIOSCIENCES CORPORATION
    Inventors: Raffaella Faraoni, Michael J. Hadd, Mark W. Holladay, Martin W. Rowbottom, Eduardo Setti
  • Publication number: 20130274278
    Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.
    Type: Application
    Filed: June 6, 2013
    Publication date: October 17, 2013
    Inventors: Stephen M. CONDON, Yijun DENG, Matthew D. ALEXANDER, Matthew G. LAPORTE
  • Publication number: 20130253186
    Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Application
    Filed: May 10, 2013
    Publication date: September 26, 2013
    Applicant: Amgen Inc.
    Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
  • Publication number: 20130237531
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: April 19, 2013
    Publication date: September 12, 2013
    Inventors: Guoxian Wu, Jiazhong Zhang, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, James Tsai
  • Publication number: 20130225579
    Abstract: Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2, R3 and R4 are each as defined in the present application.
    Type: Application
    Filed: June 8, 2011
    Publication date: August 29, 2013
    Applicant: Tianjin Hemay Bio-Tech Co., Ltd.
    Inventors: Hesheng Zhang, Yingwei Chen, Qingchao He
  • Publication number: 20130225580
    Abstract: Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.
    Type: Application
    Filed: February 28, 2013
    Publication date: August 29, 2013
    Applicant: CHEMOCENTRYX, INC.
    Inventor: ChemoCentryx, Inc.
  • Publication number: 20130224735
    Abstract: Chemical compounds having a high selectivity for double stranded DNA over RNA and single stranded DNA are disclosed. The chemical compounds are stains that become fluorescent upon illumination and interaction with double stranded DNA, but exhibit reduced or no fluorescence in the absence of double stranded DNA. The compounds can be used in a variety of biological applications to qualitatively or quantitatively assay DNA, even in the presence of RNA.
    Type: Application
    Filed: April 11, 2013
    Publication date: August 29, 2013
    Applicant: Life Technologies Corporation
    Inventor: Life Technologies Corporation
  • Publication number: 20130217709
    Abstract: The invention provides novel cyclic amine azaheterocyclic carboxamide according to Formula (I), Formula (II) and Formula (III) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: July 28, 2011
    Publication date: August 22, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Bayard R. Huck, Xiaoling Chen, Constantin Neagu, Reinaldo Jones, Yufang Xiao, Igor Mochalkin
  • Publication number: 20130217671
    Abstract: The present invention directs a compound represented by formula (I).
    Type: Application
    Filed: July 28, 2011
    Publication date: August 22, 2013
    Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Raymond Huntley, Joel R. Walker, Helene Decomez
  • Patent number: 8507682
    Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity, wherein these compounds selected from the group consisting of wherein A, B, C, D, X, Y, Z and R3 are defined in the specification. Said compounds are useful for treating a disease or condition of a mammal selected from the group consisting of ocular diseases; systemic vascular barrier related diseases; allergies and other inflammatory diseases; cardiac diseases or conditions; fibrosis; pain and wounds.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: August 13, 2013
    Assignee: Allergan, Inc.
    Inventors: Wenkiu K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im