Hetero Ring Is Four-membered Containing Nitrogen And Having Chalcogen Double Bonded Directly To A Ring Carbon Which Is Adjacent To The Ring Nitrogen Patents (Class 540/200)
  • Patent number: 9994520
    Abstract: The present invention provides an enzymatic process for the preparation of (S)-5-(4-Fluoro-phenyl)-5-hydroxy-Imorpholin-4-yl-pentan-1-one by the reduction of 1-(4-Fluoro-phenyl)-5-morpholin-4-yl-pentane-1,5-dione by using a suitable enzyme or by the resolution of (R, S)-5-(4-Fluoro-phenyl)-5-hydroxy-1 morpholin-4-yl-pentan-1-one by using an enzyme. The present invention also provides process for the preparation of Ezetimibe comprising the steps of a) protecting the compound (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1 morpholin-4-yl-pentan-1-one with hydroxy protecting group b) hydrolyzing the obtained compound c) condensing with a chiral auxiliary d) reacting with an protected imine compound e) converting to alkyl ester f) cyclizing and g) deprotecting to obtain Ezetimibe.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: June 12, 2018
    Assignee: Mylan Laboratories Limited
    Inventors: Mofazzal Husain, Srikanth G. S. C., Swapna Thorpunuri, Debashish Datta
  • Patent number: 9878997
    Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and Ring C are as defined herein, and wherein the Y—B moiety and the NH—C(?X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: January 30, 2018
    Assignee: Array BioPharma Inc.
    Inventors: Shelley Allen, Steven W. Andrews, James F. Blake, Kevin R. Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Gabrielle R. Kolakowski, Jeongbeob Seo
  • Patent number: 9862680
    Abstract: The invention provides monobactams that can be used as antibacterial agents or intermediates for the preparation of other useful compounds such as antibacterial agents.
    Type: Grant
    Filed: June 13, 2016
    Date of Patent: January 9, 2018
    Assignee: University of Notre Dame du Lac
    Inventors: Marvin Miller, Serena Carosso
  • Patent number: 9748487
    Abstract: The present invention relates to polymers comprising one or more (repeating) unit(s) of the formula (I), and compounds of formula (III), wherein Y, Y15, Y16 and Y17 are independently of each other a group of formula and their use as IR absorber, organic semiconductor in organic devices, especially in organic photovoltaics and photodiodes, or in a device containing a diode and/or an organic field effect transistor. The polymers and compounds according to the invention can have excellent solubility in organic solvents and excellent film-forming properties. In addition, high efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when the polymers and compounds according to the invention are used in organic field effect transistors, organic photovoltaics and photodiodes.
    Type: Grant
    Filed: November 5, 2013
    Date of Patent: August 29, 2017
    Assignee: BASF SE
    Inventors: Pascal Hayoz, Bernd Tieke, Haichang Zhang
  • Patent number: 9469610
    Abstract: Novel methods for the production of enantiomerically pure (EP) ?-lactams by decomposition of ?-diazo-?-ketoamides.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: October 18, 2016
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Yvette S. Vaske, Maximillian E. Mahoney, Joseph P. Konopelski
  • Patent number: 9212175
    Abstract: The present invention relates to novel azetidinone-containing compounds having a novel side-chain which is attached to the aryl ring at C4 via a C—C bond and comprises a 3,3-disubstituted oxetane ring and a polar group A, and which are useful in the treatment and prevention of atherosclerosis and for the reduction of cholesterol levels.
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: December 15, 2015
    Assignee: Lipideon Biotechnology AG
    Inventors: Thomas Fessard, Dong-Bo Li, Damien Barbaras, Susanne Wolfrum, Erick Carreira
  • Publication number: 20150148533
    Abstract: The present invention relates to a process for preparing ?-aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-?]pyrazin-7-yl compounds.
    Type: Application
    Filed: June 13, 2013
    Publication date: May 28, 2015
    Applicant: Lek Pharmaceuticals d.d.
    Inventors: Stefan Starcevic, Peter Mrak, Gregor Kopitar
  • Patent number: 9040688
    Abstract: The process of the present invention relates to a method for the synthesis of a 1,4-diphenylazetidinone of formula (VIII) by using novel oxime intermediates.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: May 26, 2015
    Assignee: LUPIN LIMITED
    Inventors: Dhananjai Srivastava, Rajiv Kumar Shakya, Namrata Anil Chaudhari, Inamus Saqlain Ansari, Girij Pal Singh
  • Patent number: 8946408
    Abstract: Novel methods for the production of enantiomerically pure (EP) ?-lactams by decomposition of ?-diazo-?-ketoamides using fluorescent light.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: February 3, 2015
    Inventors: Yvette S. Vaske, Maximillian E. Mahoney, Joseph P. Konopelski
  • Patent number: 8927533
    Abstract: The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds.
    Type: Grant
    Filed: September 17, 2012
    Date of Patent: January 6, 2015
    Assignee: SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Giuseppe Giannini, Walter Cabri, Gianfranco Battistuzzi, Davide Vignola, Nicola Fanto', Claudio Pisano, Loredana Vesci
  • Patent number: 8921568
    Abstract: Iminosugar compounds are described that have inbuilt delivery features by virtue of covalent incorporation of a tocopherol moiety, or alternative moieties that are analogs of tocopherol or select analogs of cholesterol, or its antagonist “Ezitimibe”; and are likely to have broad spectrum antiviral activity. The compounds differ from previous iminosugar compounds, even lipophillic ones, being more hydrophobic and resembling fats and oils in their partition behavior in vivo into lipid phases of lipoproteins, cellular lipid droplet organelles and biological membranes. These features confer a number of unique delivery attributes in vivo, favorable to the therapy of virus infections involving cells of the lymphoid system and the liver, in particular, but these features are also favorable in general for the treatment of virus infections of man and animals.
    Type: Grant
    Filed: June 5, 2013
    Date of Patent: December 30, 2014
    Assignees: Unither Virology, LLC, The Chancellor, Masters and Scholars of The University of Oxford
    Inventors: J. L. Kiappes, Peter Laing, Raymond Dwek, Nicole Zitzmann, Stephanie Pollock
  • Patent number: 8859183
    Abstract: Provided are N-acyl-?-lactam derivatives represented by the following general formula, from which a photoresist composition capable of controlling an acid diffusion length to be short is obtained; a polymer obtained by polymerizing the N-acyl-?-lactam derivative represented by the following general formula as one of starting materials; and a photoresist composition containing the polymer, where the structural variables are as defined herein.
    Type: Grant
    Filed: August 2, 2013
    Date of Patent: October 14, 2014
    Assignee: Kuraray Co., Ltd.
    Inventors: Takashi Fukumoto, Shuji Matsunaga, Miki Tsuruta
  • Publication number: 20140275004
    Abstract: Disclosed are compound of Formula (Ia), wherein R1, R2, and R3 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions, comprising one or more compounds of Formula (Ia).
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Alan S. Florjancic, Yunsong Tong, Thomas D. Penning, Andrew J. Souers, Rajeev Goswami
  • Publication number: 20140221333
    Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
    Type: Application
    Filed: July 19, 2012
    Publication date: August 7, 2014
    Inventors: Adrianus Petrus Antonius De Man, Jan-Gerard Sterrenburg, Han C.A. Raaijmakers, Allard Kaptein, Arthura A. Oubrie, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Jacobus C.H.M. Wijkamans, Tjeerd A. Barf, Alan B. Cooper, Ronald M. Kim, Sobhana Babu Boga, Hugh Y. Zhu, Xiaolei Gao, Xin Yao, Rajan Anand, Hao Wu, Shilan Liu, Chundao Yang, Abdul-Basit Alhassan, James Wang, Younong Yu, Jian Liu, Henry M. Vaccaro
  • Patent number: 8753794
    Abstract: Disclosed are an N-acyl-?-lactam derivative represented by the following general formula, from which a photoresist composition capable of controlling an acid diffusion length to be short is obtained; a polymer obtained by polymerizing the N-acyl-?-lactam derivative represented by the following general formula as one of starting materials; and a photoresist composition containing the polymer.
    Type: Grant
    Filed: August 27, 2010
    Date of Patent: June 17, 2014
    Assignee: Kuraray Co., Ltd.
    Inventors: Takashi Fukumoto, Shuji Matsunaga, Miki Tsuruta
  • Patent number: 8741261
    Abstract: Methods and reagents for transition metal-promoted carbonylation via isocyanate using carbon-isotope labeled carbon monoxide are provided. The resultant carbon-isotope labeled compounds are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.
    Type: Grant
    Filed: March 22, 2005
    Date of Patent: June 3, 2014
    Assignee: GE Healthcare Limited
    Inventors: Bengt Langstrom, Julien Barletta, Hisashi Doi, Masaaki Suzuki, Ryoji Noyori, Yasuyoshi Watanabe, Farhad Karimi
  • Patent number: 8729079
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: May 20, 2014
    Assignee: Endo Pharmaceuticals Inc.
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Patent number: 8673891
    Abstract: The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutical acceptable salt of the compound. (I) X is CH or N; R1 is a halogen atom, and R2 is H, a halogen atom, CN, [2], [3], [8], [9], an —O-alkyl, an —O-(saturated ring), etc. [2]: —C(RC)(RD)(RE) (RC to RE each are H, an alkyl, etc.) [3]: —N(RF)(RG) (RF and RG each are H, OH, amino, a (hetero)aryl, etc.) [8]: —C(?O)RL (RL is an alkyl, OH, an alkoxy, amino, etc.) [9]: a (substituted)phenyl; (II) X is >C—C(—O)RB (RB is a (substituted)amino, an alkoxy, OH, etc.); R1 is a halogen atom; R2 is H; R3 is H or OH; and R3 and R4 each are H or an alkyl.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: March 18, 2014
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Hidetaka Fujihara, Tetsuo Asaki, Katsutoshi Hori, Haruna Naito
  • Publication number: 20140011795
    Abstract: Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
    Type: Application
    Filed: March 16, 2012
    Publication date: January 9, 2014
    Inventors: Stephen T. Wrobleski, Gregory D. Brown, Lidia M. Doweyko, Jingwu Duan, Junqing Guo, John Hynes, Bin Jiang, James Kempson, Shuqun Lin, Zhonghui Lu, Steven H. Spergel, John S. Tokarski, Hong Wu, Bingwei Vera Yang
  • Patent number: 8623855
    Abstract: Preparation of azetidinone compounds and medical use thereof are provided by the present invention. More particularly, azetidionne compounds, shown as formula (I), wherein R1, R2, R3, R4, R5 and R6 are defined in description, and preparation methods thereof are provided by the present invention. The compounds of the present invention can reduce the levels of total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) in plasma, and can be used as medicaments for reducing cholesterol in blood. Therefore the compounds of the present invention can be used to treat or prevent diseases of atherosclerosis, cacergasia of blood vessel, cardiac failure, coronary artery disease, angiocardiopathy, myocardial, angina, hyperlipoidemia and hypercholesteremia and the like. Preparation method of compounds of formula (I) and intermediate compounds are also provided by the present invention.
    Type: Grant
    Filed: August 9, 2010
    Date of Patent: January 7, 2014
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Hua Bai, Xuyang Zhao, Xiaojie Xu, Xiaoyu Liu, Yuncai Zhang, Ying Chen, Xiaohe Zheng, Maojian Gu, Qifeng Zhu, Yong Zhang, Hairong Luo
  • Publication number: 20140005146
    Abstract: Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
    Type: Application
    Filed: March 16, 2012
    Publication date: January 2, 2014
    Inventors: Stephen T. Wrobleski, Jagabandhu Das, Lidia M. Doweyko, Junqing Guo, John Hynes, Bin Jiang, James Kempson, Shuqun Lin, Steven H. Spergel, John S. Tokarski, Hong Wu, Bingwei Vera Yang
  • Publication number: 20130331369
    Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.
    Type: Application
    Filed: August 8, 2013
    Publication date: December 12, 2013
    Applicant: Novartis AG
    Inventors: Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
  • Publication number: 20130331578
    Abstract: Iminosugar compounds are described that have inbuilt delivery features by virtue of covalent incorporation of a tocopherol moiety, or alternative moieties that are analogues of tocopherol or select analogues of cholesterol, or its antagonist “Ezitimibe”; and are likely to have broad spectrum antiviral activity. The compounds differ from previous iminosugar compounds, even lipophillic ones, being more hydrophobic and resembling fats and oils in their partition behavior in vivo into lipid phases of lipoproteins, cellular lipid droplet organelles and biological membranes. These features confer a number of unique delivery attributes in vivo, favorable to the therapy of virus infections involving cells of the lymphoid system and the liver, in particular, but these features are also favorable in general for the treatment of virus infections of man and animals.
    Type: Application
    Filed: June 5, 2013
    Publication date: December 12, 2013
    Inventors: J. L. Kiappes, Peter Laing, Raymond Dwek, Nicole Zitzmann, Stephanie Pollock
  • Publication number: 20130289013
    Abstract: Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed.
    Type: Application
    Filed: June 24, 2013
    Publication date: October 31, 2013
    Inventors: Qun Kevin FANG, Frank Xinhe Wu, Paul T. Grover, Seth C. Hopkins, Una Campbell, Milan Chytil, Kerry L. Spear
  • Publication number: 20130231322
    Abstract: A compound having a structure is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Application
    Filed: April 16, 2013
    Publication date: September 5, 2013
    Applicant: Allergan, Inc.
    Inventor: David W. Old
  • Publication number: 20130190487
    Abstract: The present invention relates to the method of preparing of ezetimibe and in particular to novel intermediates for its synthesis and an improved process for preparing such intermediates. Said intermediates may be obtained in high yields and purity in a fast and cost efficient manner. The present invention relates to a novel crystalline form of ezetimibe as well.
    Type: Application
    Filed: January 24, 2008
    Publication date: July 25, 2013
    Applicant: KRKA
    Inventors: Anton Stimac, Barbara Mohar, Michel Stephan, Mojca Bevc, Rok Zupet, Andrej Gartner, Vesna Kroselj, Matej Smrkolj, Davor Kidemet, Gregor Sedmak, PRIMOZ BENKIC, ALEN KLJAJIC, MIHA PLEVNIK
  • Patent number: 8492340
    Abstract: The invention relates to methods for treating depression, anxiety, and other related diseases by administering a peptide NMDAR partial agonist.
    Type: Grant
    Filed: September 10, 2012
    Date of Patent: July 23, 2013
    Assignee: Northwestern University
    Inventor: Joseph Moskal
  • Patent number: 8492499
    Abstract: The invention relates to addition compounds which are obtainable by reacting a) one or more polyisocyanates containing uretdione groups with b) one or more compounds of the formula (I) Y—(XH)n??(I) with the proviso that at least 50% of the free isocyanate groups of component a) are reacted with the compounds of the formula (I) to give an intermediate which contains uretdione groups, and subsequently the intermediate is reacted with c) one or more compounds of the general formula (II) Z—NHRm??(II) with the proviso that all free NCO groups optionally still present and at least 20% of uretdione groups originally used are reacted with Z—(NHR)m. The invention further relates to the use of the addition compounds as dispersants and dispersion stabilizers, and to a process for preparing them.
    Type: Grant
    Filed: March 20, 2007
    Date of Patent: July 23, 2013
    Assignee: BYK-Chemie GmbH
    Inventors: Karlheinz Haubennestel, Stefan Moessmer, Wolfgang Pritschins, Thomas Launag
  • Publication number: 20130184249
    Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: February 28, 2013
    Publication date: July 18, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8445622
    Abstract: The present invention relates to a process for preparing polyisocyanates by oligomerization of isocyanates.
    Type: Grant
    Filed: November 30, 2007
    Date of Patent: May 21, 2013
    Assignee: BASF SE
    Inventors: Horst Binder, Hubert Graf
  • Patent number: 8444877
    Abstract: Provided are liquid crystal compounds and mixtures incorporating the same. The liquid crystal compounds of the invention generally comprise a terminal cyclopentene group, along with at least two other ring groups.
    Type: Grant
    Filed: January 15, 2009
    Date of Patent: May 21, 2013
    Assignee: VVI Bright China Ltd.
    Inventors: Xinhua Chen, R. Amaranatha Reddy
  • Patent number: 8440819
    Abstract: A compound having a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof; wherein a dashed line represents the presence or absence of a bond; Y has from 0 to 14 carbon atoms and is: an organic acid functional group, or an amide or ester thereof; hydroxymethyl or an ether thereof; or a tetrazolyl functional group; A is —(CH2)6—, cis-CH2CH?CH—(CH2)3—, or —CH2C?C—(CH2)3—, wherein 1 or 2 carbon atoms may be replaced by S or O; or A is —(CH2)m—Ar—(CH2)o— wherein Ar is interarylene or heterointerarylene, the sum of m and o is 1, 2, 3, or 4, and wherein 1 -CH2— may be replaced by S or O, and 1 -CH2—CH2— may be replaced by —CH?CH— or —C?C—; J is hydrogen, OH, O, SH, S, C1-6 alkyl, —O—(C1-6 alkyl), —S—(C1-6 alkyl), F, Cl, Br, I, CN, or CF3; and B is aryl or heteroaryl, is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: February 17, 2009
    Date of Patent: May 14, 2013
    Assignee: Allergan, Inc.
    Inventor: David W. Old
  • Patent number: 8420628
    Abstract: Disclosed herein is a compound comprising or a pharmaceutically acceptable salt or a prodrug or a metabolite thereof; wherein Y is an organic acid functional group, or an amide or ester thereof comprising up to 12 carbon atoms; or Y is hydroxymethyl or an ether thereof comprising up to 12 carbon atoms; or Y is a tetrazolyl functional group; A is —(CH2)6—, cis —CH2CH?CH—(CH2)3—, or —CH2C?C—(CH2)3—, wherein 1 or 2 carbon atoms may be substituted with S or O; or A is —(CH2)m—Ar—(CH2)o— wherein Ar is interarylene or heterointerarylene, the sum of m and o is from 1 to 4, and wherein one CH2 may be substituted with S or O; and D is aryl or heteroaryl.
    Type: Grant
    Filed: May 2, 2006
    Date of Patent: April 16, 2013
    Assignee: Allergan, Inc.
    Inventor: David W. Old
  • Patent number: 8415295
    Abstract: Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CH2; S; O; CF2 or C(CH3)2; Z is H; halogen; hydroxyl; (C1-6)alkoxy; (C1-12)alkyl; (C3-12)cycloalkyl; phenyl; or heteroaryl; where the phenyl and heteroaryl groups are optionally mono- or independently plurisubstituted with R7; optionally, X together with an adjacent ring carbon and Z form a fused cyclopropyl; and optionally, one of the bonds in the ring containing X is a double bond; and CriRii, R1, R1, R3, R4 and R5 are as described herein. Methods for preparing these compounds, and methods for treating diabetes, especially Type II diabetes, and other related diseases are described using the compounds of formula I in pharmaceutical compositions which contain these compounds. Pharmaceutical compositions which contain combinations of these compounds with other antidiabetic agents are also described herein.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: April 9, 2013
    Assignee: Phenomix Corporation
    Inventors: David Alan Campbell, David T. Winn, Juan Manuel Betancort
  • Publication number: 20130053325
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorders such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain.
    Type: Application
    Filed: February 11, 2011
    Publication date: February 28, 2013
    Inventors: Joseph Moskal, M. Amin Khan
  • Publication number: 20130053346
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Application
    Filed: August 23, 2012
    Publication date: February 28, 2013
    Applicant: Endo Pharmaceuticals Inc
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Patent number: 8383810
    Abstract: A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a ?-(substituted-amino)amide, a ?-(substituted-amino)acid ester, or a ?-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.
    Type: Grant
    Filed: December 12, 2011
    Date of Patent: February 26, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tiruvettipuram K. Thiruvengadam, John S. Chiu, Xiaoyong Fu, Timothy L. McAllister
  • Publication number: 20120322761
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Application
    Filed: August 29, 2012
    Publication date: December 20, 2012
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Publication number: 20120309734
    Abstract: Cancer is one of the major causes of death worldwide. Although many advances have been made in the treatment and management of the disease, the existence of chemotherapy-resistance means there is still a great need to develop new strategies and drugs for its treatment. Provided herein are synthetic derivatives of combretastatin A-4, in particular those in which the aromatic rings are locked into a non-isomerisable active conformation, thus resulting in improved, stable compounds. The novel compounds are structurally related to combretastatin A-4 (CA-4) and lock the rings into the known active conformation by means of a four membered nitrogen containing heterocyclic ring, such as a beta-lactam ring, incorporated into the standard CA-4 structure. The compounds exhibit potent anti-cancer activity.
    Type: Application
    Filed: December 14, 2010
    Publication date: December 6, 2012
    Inventors: Mary J. Meegan, Daniela Zisterer, Miriam Carr, Thomas Greene, Niamh O'Boyle, Lisa Greene
  • Publication number: 20120302540
    Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.
    Type: Application
    Filed: May 24, 2012
    Publication date: November 29, 2012
    Inventors: Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
  • Patent number: 8314087
    Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: November 20, 2012
    Assignee: Amgen Inc.
    Inventors: Brian K. Albrecht, Steven Bellon, Shon Booker, Alan C. Cheng, Derin D'Amico, Noel D'Angelo, Jean-Christophe Harmange, Tae-Seong Kim, Longbin Liu, Mark H. Norman, Aaron C. Siegmund, Markian Stec, Ning Xi, Kevin Yang
  • Patent number: 8304403
    Abstract: Compounds of formula Ia and Ib and wherein A, B, C and R1 are described herein.
    Type: Grant
    Filed: June 10, 2010
    Date of Patent: November 6, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Publication number: 20120208994
    Abstract: Preparation of azetidinone compounds and medical use thereof are provided by the present invention. More particularly, azetidionne compounds, shown as formula (I), wherein R1, R2, R3, R4, R5 and R6 are defined in description, and preparation methods thereof are provided by the present invention. The compounds of the present invention can reduce the levels of total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) in plasma, and can be used as medicaments for reducing cholesterol in blood. Therefore the compounds of the present invention can be used to treat or prevent diseases of atherosclerosis, cacergasia of blood vessel, cardiac failure, coronary artery disease, angiocardiopathy, myocardial, angina, hyperlipoidemia and hypercholesteremia and the like. Preparation method of compounds of formula (I) and intermediate compounds are also provided by the present invention.
    Type: Application
    Filed: August 9, 2010
    Publication date: August 16, 2012
    Applicant: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.
    Inventors: Hua Bai, Xuyang Zhao, Xiaojie Xu, Xiaoyu Liu, Yuncai Zhang, Ying Chen, Xiaohe Zheng, Maojian Gu, Qifeng Zhu, Yong Zhang, Hairong Luo
  • Patent number: 8236789
    Abstract: It is to provide a novel compound useful for preventing and/or treating diseases that involves 11?-hydroxysteroid dehydrogenase 1, particularly diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome. It is an 1-adamantyl azetidin-2-one derivative represented by the following general formula (1) or salt thereof, or their solvate.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: August 7, 2012
    Assignee: Kowa Company, Ltd.
    Inventors: Hisashi Nakashima, Takahiro Mori, Ryoko Mori, legal representative, Takaaki Araki, Takahisa Ogamino, Kazutoyo Abe, Tadaaki Ohgiya
  • Publication number: 20120196740
    Abstract: Bi-functional cobalt-containing catalysts useful for making stereo specific compounds and compositions, along with methods of making, and uses thereof in the syntheses of optically pure ?-lactones from aldehydes and ketene are described. Precursors, intermediates, compositions, and particular features of the use if the compositions, such as high enantiomeric selectivity, high yield and low mole percent of catalyst useful are provided.
    Type: Application
    Filed: June 7, 2010
    Publication date: August 2, 2012
    Applicant: UNIVERSITY OF TOLEDO
    Inventor: Yun-Ming Lin
  • Patent number: 8232389
    Abstract: The present invention relates to a method for crystallization of (2R)-2-{(3S,4S)-3-[(1R)-1-(tert-butyldimethylsilyloxy)ethyl]-2-oxoazetidin-4-yl}propionic acid, and is characterized in that crystallization is carried out by mixing a solution containing the compound with a substituted aromatic hydrocarbon solvent and/or a halogenated hydrocarbon solvent. The method can provide a crystal of the compound with a high purity and a high yield while the content of 2S isomer is kept at a low level.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: July 31, 2012
    Assignee: Kaneka Corporation
    Inventors: Keita Nishino, Teruyoshi Koga, Masafumi Fukae, Yasuyoshi Ueda
  • Publication number: 20120184731
    Abstract: Novel methods for the production of enantiomerically pure (EP) ?-lactams by decomposition of ?-diazo-?-ketoamides using fluorescent light.
    Type: Application
    Filed: March 15, 2010
    Publication date: July 19, 2012
    Inventors: Yvette S. Vaske, Maximillian E. Mahoney, Joseph P. Konopelski
  • Patent number: 8202855
    Abstract: Disclosed herein is a compound comprising a formula or a pharmaceutically acceptable salt or a prodrug or a metabolite thereof; Y is A is —(CH2)6—, cis —CH2CH?CH—(CH2)3—, or —CH2C?C—(CH2)3—, wherein 1 or 2 carbon atoms may be substituted with S or O; or A is —(CH2)m—Ar—(CH2)o— wherein Ar is interarylene or heterointerarylene, the sum of m and o is from 1 to 4, and wherein one CH2 may be substituted with S or O; and D is aryl or heteroaryl. Methods of use are also disclosed.
    Type: Grant
    Filed: March 2, 2009
    Date of Patent: June 19, 2012
    Assignee: Allergan, Inc
    Inventor: David W. Old
  • Patent number: 8178665
    Abstract: A process for the production of 1-(4-3(R)-[3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) according to the following reaction scheme: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI) where the substances of the general Formulas II, IV, VI, VIII, IX, X and XI are new, Formula III is a non-isolated intermediate, R1, R2 and R3 are represented by the compounds of Formulas Va-Vd, (Va), (Vb), (Vc), (Vd) and R4 is a silyl, e.g., tert-butyl-dimethyl-silyl, tert-butyl-diphenyl-silyl group.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: May 15, 2012
    Assignee: Richter Gedeon Nyrt.
    Inventors: József Bódi, János Éles, Katalin Szöke, Krisztina Vukics, Tamás Gáti, Krisztina Temesvári, Dorottya Kiss-Bartos
  • Publication number: 20120083601
    Abstract: A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a ?-(substituted-amino)amide, a ?-(substituted-amino)acid ester, or a ?-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.
    Type: Application
    Filed: December 12, 2011
    Publication date: April 5, 2012
    Applicant: Schering-Plough Corporation
    Inventors: TIRUVETTIPURAM K. THIRUVENGADAM, John S. Chiu, Xiaoyong Fu, Timothy L. McAllister