Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/91)
  • Patent number: 11629154
    Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ßproduction, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ßproteins. A compound of Formula (I) wherein R3 is each independently alkyl optionally substituted with halogen, cyano, alkyloxy, haloalkyloxy or non-aromatic carbocyclyl, or the like; t is integer from 0 to 3; R5 is a hydrogen atom or halogen; R6 is selected from the group consisting of a hydrogen atom, halogen, and substituted or unsubstituted alkyl; ring B is a substituted or unsubstituted pyrazine or the like; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 25, 2019
    Date of Patent: April 18, 2023
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Genta Tadano, Shinji Suzuki, Ken-ichi Kusakabe
  • Patent number: 11279672
    Abstract: The present invention relates to an improved asymmetric synthesis of alpha-branched amines (hereafter referred to as the compound) and relative chiral amines (1?) or its pharmaceutically acceptable salt and derivatives. The process comprises an unusual substrate specific regioselective ortho lithiation of substituted arene compounds, followed by its highly diastereoselective addition to N-tert-butanesulfinylimines resulting in the selective formation of alpha-branched sulfinyl amine and chiral amine; which on subsequently removing the sulfinyl group provides corresponding alpha-branched amines or relative chiral amines (1?).
    Type: Grant
    Filed: April 17, 2019
    Date of Patent: March 22, 2022
    Assignee: PIRAMAL PHARMA LIMITED
    Inventors: Rajender Reddy Leleti, Sharadsrikar Kotturi, Yogesh Waman, Chirag Patel, Aditya Patwa, Rajesh Shenoy
  • Patent number: 11279668
    Abstract: The present invention relates to an improved asymmetric synthesis of alpha-(diarylmethyl) alkyl amines (hereafter referred to as the compound (1)) or its pharmaceutically acceptable salt and derivatives. The process comprises an unusual substrate specific regioselective lithiation of alpha-diarylmethanes. followed by its highly diastereoselective addition to N-tert-butanesulfinylimines resulting in the selective formation of chiral alpha-(diarylmethyl) alkyl amines 4 and chiral amine 5; which on subsequently removing the sulfinyl group provides corresponding alpha-(diarylmethyl) alkyl amines (1) or relative chiral amines (1?).
    Type: Grant
    Filed: March 20, 2019
    Date of Patent: March 22, 2022
    Assignee: PIRAMAL PHARMA LIMITED
    Inventors: Rajender Reddy Leleti, Sharadsrikar Kotturi, Yogesh Waman, Chirag Patel, Rajesh Shenoy
  • Patent number: 10334852
    Abstract: This disclosure relates to pyrido-1,3-oxazine-2,4-diones of Formula I and their use as fungicides.
    Type: Grant
    Filed: August 30, 2017
    Date of Patent: July 2, 2019
    Assignee: Dow AgroSciences LLC
    Inventors: Brannon Sam, Kevin G. Meyer, Chenglin Yao, Brian A. Loy, Jared W. Rigoli, Nicholas R. Babij
  • Patent number: 9079914
    Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: July 21, 2010
    Date of Patent: July 14, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: John Mark Ellard, Christopher Neil Farthing, Adrian Hall
  • Patent number: 9051333
    Abstract: The present invention provides a novel 6,7-dihydroimidazo[2,1-b][1,3]oxazine compound that has excellent bactericidal action against tubercle bacilli, multidrug-resistant tubercle bacilli, and atypical acid-fast bacilli. Specifically, the present invention provides a compound represented by Formula (1): or a salt thereof, wherein R1 represents tetrahydroisoquinolyl, tetrahydroquinolyl, tetrahydrobenzoazepinyl, benzoxazolyl, benzothiazolyl, indolyl, isoindolinyl, naphthyl, quinolyl, phenyl, biphenylyl, or pyridyl, these groups being optionally substituted, the phenyl, biphenylyl, and pyridyl represented by R1 each being substituted directly or via a linker with at least one group selected from the group consisting of tetrahydropyridyl, diazepanyl, diazabicycloheptanyl, tetrahydrotriazolopyrazinyl, tetrahydroimidazopyrazinyl, azabicyclooctanyl, oxazolyl, piperazinyl, piperidyl, thiazolyl, and the like, each of these groups being optionally substituted; and R2 represents hydrogen or lower alkyl.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: June 9, 2015
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Yoshikazu Kawano, Yoshikazu Haraguchi, Hirofumi Sasaki, Yukitaka Uematsu, Hidetsugu Tsubouchi, Hiromi Yata, Hiroshi Shimizu, Kazuho Kohashi, Motohiro Itotani, Kuninori Tai, Isao Takemura, Mikayo Hayashi, Hiroyuki Hashizume, Miki Matsuba, Izuru Nakamura, Xiuhao Chen, Makoto Matsumoto
  • Patent number: 9029368
    Abstract: The invention relates to antibacterial compounds of formula I wherein G and K are as defined in the description; and salts of such compounds.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: May 12, 2015
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Patent number: 9029367
    Abstract: The present invention provides a compound of Formula III: Formula III wherein A is: and Z, R1, R2, R3, and R4 are as defined herein, or a pharmaceutically acceptable salt thereof, which is useful for treating Alzheimer's disease.
    Type: Grant
    Filed: June 11, 2014
    Date of Patent: May 12, 2015
    Assignee: Eli Lilly and Company
    Inventors: Steven James Green, Erik James Hembre, Dustin James Mergott, Yuan Shi, Brian Morgan Watson, Leonard Larry Winneroski, Jr.
  • Patent number: 9023844
    Abstract: Heterocyclylpyri(mi)dinylpyrazole of the formula (I) in which R1 to R5, X1, U, Q, W, Y, n, a, b have the meanings given in the description, and agrochemically active salts, to their use and to methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants and for reducing mycotoxins in plants and parts of the plants, to processes for preparing such compounds and compositions and treated seed and also to their use for controlling phytopathogenic harmful fungi in agriculture, horticulture, forestry, in animal husbandry, in the protection of materials, in the domestic and hygiene field and for the reduction of mycotoxins in plants and parts of the plants.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: May 5, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Stefan Hillebrand, Amos Mattes, Alexander Sudau, Pierre Wasnaire, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann, Haruko Sawada, Philippe Desbordes, Anne-Sophie Rebstock, Stéphane Brunet, Hélène Lachaise, Philippe Rinolfi
  • Patent number: 9012443
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: April 21, 2015
    Assignee: Amgen Inc.
    Inventors: Christiane Boezio, Howard Bregman, James R. Coats, Erin F. Dimauro, Thomas Dineen, Bingfan Du, Russell Graceffa, Charles Kreiman, Daniel La, Isaac E. Marx, Nagasree Chakka, Hanh Nho Nguyen, Emily Anne Peterson, Matthew Weiss, Katrina W. Copeland, Holly L. Deak, Alessandro Boezio
  • Publication number: 20150087641
    Abstract: The present invention is directed to heterocyclic compounds which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Application
    Filed: May 3, 2013
    Publication date: March 26, 2015
    Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair
  • Publication number: 20150045355
    Abstract: Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.
    Type: Application
    Filed: December 31, 2011
    Publication date: February 12, 2015
    Inventors: Changyou Zhou, Shaohui Wang, Guoliang Zhang
  • Publication number: 20150031668
    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: July 15, 2014
    Publication date: January 29, 2015
    Inventors: Kaustav Biswas, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Vu Van Ma, Kelvin Sham, James Brown, Wenge Zhong, Thomas T. Nguyen
  • Publication number: 20140371212
    Abstract: The present invention provides a compound of Formula III: wherein A is: and Z, R1, R2, R3, and R4 are as defined herein, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 11, 2014
    Publication date: December 18, 2014
    Inventors: Steven James GREEN, Erik James HEMBRE, Dustin James MERGOTT, Yuan SHI, Brian Morgan WATSON, Leonard Larry WINNEROSKI, JR.
  • Publication number: 20140309218
    Abstract: The invention relates to antibacterial compounds of formula I wherein G and K are as defined in the description; and salts of such compounds.
    Type: Application
    Filed: November 29, 2012
    Publication date: October 16, 2014
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Publication number: 20140275092
    Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylses. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Constellation Pharmaceuticals, Inc.
    Inventors: Brian K. Albrecht, Steven F. Bellon, Victor S. Gehling, Jean-Christophe Harmange
  • Publication number: 20140256677
    Abstract: Heterocyclylpyri(mi)dinylpyrazole of the formula (I) in which R1 to R5, X1, U, Q, W, Y, n, a, b have the meanings given in the description, and agrochemically active salts, to their use and to methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants and for reducing mycotoxins in plants and parts of the plants, to processes for preparing such compounds and compositions and treated seed and also to their use for controlling phytopathogenic harmful fungi in agriculture, horticulture, forestry, in animal husbandry, in the protection of materials, in the domestic and hygiene field and for the reduction of mycotoxins in plants and parts of the plants
    Type: Application
    Filed: October 4, 2012
    Publication date: September 11, 2014
    Inventors: Stefan Hillebrand, Amos Mattes, Alexander Sudau, Pierre Wasnaire, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann, Haruko Sawada, Philippe Desbordes, Anne-Sophie Rebstock, Stéphane Brunet, Hélène Lachaise, Philippe Rinolfi
  • Publication number: 20140199263
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 17, 2014
    Inventors: Casey Cameron McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Zhong Lai, Qun Dang, Nicolas Zorn
  • Publication number: 20140171639
    Abstract: Compounds of Formula I are useful as antagonists 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: February 24, 2014
    Publication date: June 19, 2014
    Applicant: AMGEN INC.
    Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
  • Patent number: 8710043
    Abstract: Compounds of Formula I are useful as antagonists 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: Grant
    Filed: June 21, 2012
    Date of Patent: April 29, 2014
    Assignee: Amgen Inc.
    Inventors: Jian J. Chen, Daniel B. Horne, Matthew R. Kaller, Vu Van Ma
  • Publication number: 20140005163
    Abstract: The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone derivatives; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone derivatives.
    Type: Application
    Filed: May 24, 2013
    Publication date: January 2, 2014
    Applicant: NOVARTIS AG
    Inventors: Pascal Furet, Frank Stephan Kalthoff, Robert Mah, Christian Ragot, Frederic Stauffer
  • Publication number: 20130338151
    Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
    Type: Application
    Filed: October 21, 2010
    Publication date: December 19, 2013
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Patent number: 8563547
    Abstract: (6,7-Dihydro-2-nitro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)amide compounds of formula (I), and their pharmaceutically acceptable salts, preparation methods and pharmaceutical compositions thereof are disclosed, wherein m and R are defined as in the description. The uses of the compounds in preparing medicaments for treating infectious diseases caused by Mycobacterium tuberculosis, especially infectious diseases caused by multi-drug resistance Mycobacterium tuberculosi are also disclosed.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: October 22, 2013
    Assignee: Shanghai Sun-Sail Pharmaceutical Science & Technology Co., Ltd.
    Inventors: Tiancai Wang, Ting Xin, Houxing Fan, Yilang Chen
  • Publication number: 20130157996
    Abstract: Compounds of Formula I are useful as antagonists 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: June 21, 2012
    Publication date: June 20, 2013
    Applicant: Amgen Inc.
    Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
  • Publication number: 20130150339
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: December 6, 2012
    Publication date: June 13, 2013
    Applicant: Amgen Inc.
    Inventor: Amgen Inc.
  • Publication number: 20130143864
    Abstract: (6,7-Dihydro-2-nitro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)amide compounds of formula (I), and their pharmaceutically acceptable salts, preparation methods and pharmaceutical compositions thereof are disclosed, wherein m and R are defined as in the description. The uses of the compounds in preparing medicaments for treating infectious diseases caused by Mycobacterium tuberculosis, especially infectious diseases caused by multi-drug resistance Mycobacterium tuberculosi are also disclosed.
    Type: Application
    Filed: October 26, 2012
    Publication date: June 6, 2013
    Inventors: Tiancai Wang, Ting Xin, Houxing Fan, Yilang Chen
  • Patent number: 8404680
    Abstract: The present invention relates to N-[3-(5-Amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: February 2, 2012
    Date of Patent: March 26, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Roland Humm
  • Publication number: 20130045973
    Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
    Type: Application
    Filed: April 20, 2012
    Publication date: February 21, 2013
    Inventors: Matthew Duncton, Donogh John Roger O'Mahony, Matthew Cox, Maria De Los Angeles Estiarte-Martinez
  • Publication number: 20120295181
    Abstract: A benzoxazine-based monomer, a polymer thereof, an electrode for a fuel cell including the same, an electrolyte membrane for a fuel cell including the same, and a fuel cell using the same. The aromatic ring may contain up to 2 nitrogens within the ring. Single ring and fused ring substituents are attached to the pendent nitrogen. The ring substituents may be heterocyclic.
    Type: Application
    Filed: July 27, 2012
    Publication date: November 22, 2012
    Applicant: SAMSUNG ELECTRONICS, CO., LTD.
    Inventors: Seongwoo Choi, Jungock Park, Wonmok Lee
  • Patent number: 8314094
    Abstract: [PROBLEMS] To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases. [MEANS FOR SOLVING PROBLEMS] The compound, which is for use as an active ingredient, is represented by the formula (I): [wherein R1 represents optionally halogenated C1-6 alkyl, etc.; R2 represents, e.g., a group represented by the formula (II-1) or (II-4) (wherein W represents C1-6 alkylene, etc. and R represents C1-6 alkyl, etc.); R3 represents hydrogen, C1-6 alkyl, etc.; X represents —O—, —NH—, etc.; and Y1, Y2, Y3, and Y4 each independently represents —CH—, —N—, etc.].
    Type: Grant
    Filed: October 2, 2008
    Date of Patent: November 20, 2012
    Assignee: MSD K.K
    Inventors: Shiho Ishikawa, Takashi Mizutani, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi
  • Publication number: 20120270863
    Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
    Type: Application
    Filed: October 21, 2010
    Publication date: October 25, 2012
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Patent number: 8293734
    Abstract: The current invention pertains to nitroimidazooxazine and nitroimidazooxazole analogues, their methods of preparation, and uses of the compounds as treatment for Mycobacterium tuberculosis, for use as anti-tubercular drugs, for use as anti-protozoal agents with unexpectedly high potency against Trypanosoma cruzi or Leishmania donovani, and for the treatment of other microbial infections.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: October 23, 2012
    Assignee: Global Alliance for TB Drug Development
    Inventors: Andrew Mark Thompson, William Alexander Denny, Adrian Blaser, Zhenkun Ma
  • Patent number: 8288375
    Abstract: Disclosed are compounds of Formulae 1 and 1a, N-oxides, and salts thereof, wherein R1, R1a, Y, and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Further disclosed is a method for preparing compounds of Formula 1 from compounds of Formula 1a.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: October 16, 2012
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: Andrew Edmund Taggi, Thomas Martin Stevenson
  • Publication number: 20120251920
    Abstract: A benzoxazine-based monomer includes a halogen atom-containing functional group and a nitrogen-containing heterocyclic group. A polymer formed from the benzoxazine-based monomer may be used in an electrode for a fuel cell and electrolyte membrane for a fuel cell.
    Type: Application
    Filed: May 4, 2012
    Publication date: October 4, 2012
    Applicant: Samsung Electronics Co., Ltd.
    Inventors: Seongwoo Choi, Jungock Park
  • Publication number: 20120245155
    Abstract: The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-?proteins. A compound of the formula (I): wherein R1, R2a, R2b, R3, R4, R5a, R5b, R6a, R6b, X, Y, Z, ring A and the dashed lines are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 9, 2010
    Publication date: September 27, 2012
    Applicant: Shionogi & Co., Ltd.
    Inventors: Syuhei Yoshida, Issei Kato, Kouki Fuchino, Yuuji Kooriyama, Yoshiyasu Baba, Norihiko Tanimoto
  • Publication number: 20120245157
    Abstract: The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-? proteins. A compound of the formula (I): wherein R1, R2a, R2b, R3, R4a, R4b, ring A and the dashed lines are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 10, 2010
    Publication date: September 27, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Moriyasu Masui, Akihiro Hori
  • Patent number: 8252890
    Abstract: A benzoxazine-based monomer, a polymer thereof, an electrode for a fuel cell including the same, an electrolyte membrane for a fuel cell including the same, and a fuel cell using the same. The aromatic ring may contain up to 2 nitrogens within the ring. Single ring and fused ring substituents are attached to the pendent nitrogen. The ring substituents may be heterocyclic.
    Type: Grant
    Filed: September 11, 2008
    Date of Patent: August 28, 2012
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Seongwoo Choi, Jungook Park, Wonmok Lee
  • Publication number: 20120202804
    Abstract: A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Application
    Filed: July 21, 2010
    Publication date: August 9, 2012
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: John Mark Ellard, Christopher Neil Farthing, Adrian Hall
  • Publication number: 20120202803
    Abstract: The present invention relates to N-[3-(5-Amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: February 2, 2012
    Publication date: August 9, 2012
    Inventors: Hans Hilpert, Roland Humm
  • Publication number: 20120184516
    Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Application
    Filed: June 30, 2011
    Publication date: July 19, 2012
    Inventors: Charles Kim, Takashi Nakai, Thomas Wai-Ho Lee, Joel Moore, Nicholas Robert Perl, Jason Rohde, Rajesh R. Iyengar, Ara Mermerian
  • Publication number: 20120107273
    Abstract: The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof and an anti-HCV agent and an HCV polymerase inhibitor containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
    Type: Application
    Filed: April 25, 2011
    Publication date: May 3, 2012
    Applicant: Japan Tobacco Inc.
    Inventors: Hiroyuki Abe, Masahiro Tanaka, Kazuyuki Sugimoto, Akira Suma, Masahiro Yokota, Makoto Shiozaki, Kiyosei Ilo, Kazuhito Ueyama, Dai Motoda, Toru Noguchi, Tsuyoshi Adachi, Junichiro Tsuruha, Satoki Doi
  • Patent number: 8163901
    Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: April 24, 2012
    Assignee: Evotec AG
    Inventors: Matthew Duncton, Donogh John Roger O'Mahony, Matthew Cox, Maria De Los Angeles Estiarte-Martinez
  • Publication number: 20120028973
    Abstract: The present invention relates to novel nitroimidazooxazines, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.
    Type: Application
    Filed: July 30, 2010
    Publication date: February 2, 2012
    Applicant: Global Alliance for TB Drug Development
    Inventors: William Alexander Denny, Andrew Mark Thompson, Adrian Blaser, Brian Desmond Palmer, Zhenkun Ma, Hamish Scott Sutherland, Iveta Kmentova
  • Publication number: 20110263845
    Abstract: It is an object of the present invention to provide an efficient method for manufacturing heterocycle-substituted pyridine derivatives. The present invention provides a method for manufacturing a compound represented by the following formula (I): the method including reacting a compound represented by the following formula (III): and a compound represented by the following formula (II): in a solvent and in the presence of a palladium catalyst and a base, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group that may be protected with a protective group, etc.; one of X and Y represents a nitrogen atom and the other represents a nitrogen atom or an oxygen atom; Q represents a leaving group; the ring A represents a 5- or 6-member heteroaryl ring or a benzene ring, which may have one or two halogen atoms or C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, etc.
    Type: Application
    Filed: December 25, 2008
    Publication date: October 27, 2011
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Jun Niijima, Kazuhiro Yoshizawa, Yuki Kosaka, Shinya Abe
  • Publication number: 20110201605
    Abstract: The invention relates to compounds of formula where hetaryl I, hetaryl II, R1, R2, R3, R4, m, n, and o are as defined in the specification or to pharmaceutically active acid addition salts thereof. The compounds of formula I are modulators for amyloid beta and thus may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
    Type: Application
    Filed: February 9, 2011
    Publication date: August 18, 2011
    Inventors: Karlheinz Baumann, Alexander Flohr, Erwin Goetschi, Luke Green, Synese Jolidon, Henner Knust, Anja Limberg, Thomas Luebbers, Andrew Thomas
  • Publication number: 20110190283
    Abstract: Compounds of the Formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.
    Type: Application
    Filed: July 6, 2010
    Publication date: August 4, 2011
    Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. DeWolf, JR., Dalia R. Jakas
  • Publication number: 20110172191
    Abstract: A series of thieno[2,3-b]pyridine derivatives, attached at the 2-position to a substituted anilino moiety, which are substituted in the 3-position by a carbonyl group linked to a pyrrolidin-1-yl ring which in turn forms part of a heteroatom-containing fused bicyclic ring system, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.
    Type: Application
    Filed: December 17, 2010
    Publication date: July 14, 2011
    Applicant: UCB Pharma S.A.
    Inventors: James Andrew Johnson, Daniel Christopher Brookings, Barry John Langham, Judi Charlotte Neuss, Joanna Rachel Thorne
  • Publication number: 20110144098
    Abstract: This invention relates to 5,6-dihydro-4H-[1,3]oxazin-2-ylamine compounds of the formula wherein R1 to R5 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.
    Type: Application
    Filed: December 2, 2010
    Publication date: June 16, 2011
    Inventors: David Banner, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Mark Rogers-Evans
  • Patent number: 7910583
    Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.
    Type: Grant
    Filed: April 30, 2008
    Date of Patent: March 22, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: John M. Fevig, Dean A. Wacker
  • Publication number: 20110053910
    Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
    Type: Application
    Filed: July 3, 2006
    Publication date: March 3, 2011
    Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring