The Carbonyl Is Bonded Directly To Nitrogen Of Morpholine Ring Patents (Class 544/176)
  • Patent number: 9682918
    Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogs thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogs thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
    Type: Grant
    Filed: August 25, 2014
    Date of Patent: June 20, 2017
    Assignee: ANHUI NEW STAR PHARMACEUTICAL DEVLOPMENT CO., LTD.
    Inventors: Ziao Xu, Yuanhai Zhao, Degang Li, Xiaoxiang Li
  • Publication number: 20150119572
    Abstract: The present invention relates to a process for manufacturing aryloxyacetamides of formula (I), by reacting haloacetamides of formula (II) with a phenol of formula (III); wherein the variables are defined according to the description, and aryloxyacetamides of formula (I).
    Type: Application
    Filed: December 20, 2012
    Publication date: April 30, 2015
    Applicant: BASF SE
    Inventors: Maximilian Dochnahl, Michael Rack, Michael Keil, Bernd Wolf, Uwe Josef Vogelbacher, Joachim Gebhardt, Timo Frassetto, Volker Maywald
  • Patent number: 9000222
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Grant
    Filed: June 18, 2013
    Date of Patent: April 7, 2015
    Assignee: Androscience Corporation
    Inventors: Charles Shih, Qian Shi, Hui-Kang Wang
  • Publication number: 20150087823
    Abstract: The present invention relates to a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical agent containing the compound as an active ingredient. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt, which is the compound of the present invention, is specifically represented by the general formula (I): wherein X is a substituent such as a 1-pyrrolidyl, a 3-thiazolizyl, or a piperidino, and the compound is highly useful as a pharmaceutical agent, such as a prophylactic or therapeutic agent for a peripheral nerve disorder induced by administration of an anticancer agent, a prophylactic or therapeutic agent for neurodegenerative diseases or mental diseases such as dementia, Alzheimer's disease, Parkinson's disease, diabetic neuropathy, depression, glaucoma, or autistic disorder spectrum, a therapeutic or repairing agent for spinal cord injury, analgesics against various pain diseases, or the like.
    Type: Application
    Filed: April 26, 2013
    Publication date: March 26, 2015
    Inventors: Munekazu Iinuma, Shoei Furukawa, Mitsuru Naiki, Tomonori Matsumoto, Kunihiko Higashiura
  • Publication number: 20150004545
    Abstract: A photoresist composition containing (A) a polymer having a structural unit (I) that includes an acid-labile group, and (I) a compound represented by the following formula (1). In the following formula (1), R1, R2, R3 and R represent a hydrogen atom or a monovalent organic group having 1 to 20 carbon atoms. X represents a single bond, an oxygen atom or —NRa—. Ra represents a hydrogen atom, a hydroxy group or a monovalent organic group having 1 to 20 carbon atoms, and optionally taken together represents a ring structure by binding with R each other. A? represents —SO3? or —CO2?. M+ represents a monovalent onium cation.
    Type: Application
    Filed: September 19, 2014
    Publication date: January 1, 2015
    Applicant: JSR CORPORATION
    Inventors: Hayato NAMAI, Norihiko IKEDA, Takanori KAWAKAMI
  • Patent number: 8853393
    Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: October 7, 2014
    Assignee: Anhui New Star Pharmaceutical Development Co., Ltd.
    Inventors: Ziao Xu, Yuanhai Zhao, Degang Li, Xiaoxiang Li
  • Patent number: 8853392
    Abstract: In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N1-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: June 3, 2008
    Date of Patent: October 7, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
  • Patent number: 8853390
    Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: October 7, 2014
    Assignee: AbbVie Inc.
    Inventors: Yi-Yin Ku, Timothy A. Grieme, Jeffrey M. Kallemeyn, Mathew M. Mulhern
  • Publication number: 20140288077
    Abstract: In one aspect, the invention relates to substituted 4-phenoxyphenol analogs, derivatives thereof, and related compounds, which are useful as inhibitors of proliferating cell nuclear antigen (PCNA); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating hyperproliferative disorders associated with PCNA using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: July 5, 2012
    Publication date: September 25, 2014
    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL
    Inventors: Naoaki Fujii, Marcelo Actis, Chandanamali Punchihewa, Michele Connelly, Sean Wu
  • Publication number: 20140275008
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Qing Xu, Zhe Li
  • Publication number: 20140231729
    Abstract: A negative-type photosensitive resin composition capable of forming a pattern having favorable adhesiveness at a low light exposure; a pattern forming method using the resin composition; a cured film, an insulating film, a color filter formed using resin composition; and a display device provided with the cured film, insulating film, or color filter. The resin composition contains a compound represented by the following formula (1). In the formula, R1 and R2 each independently indicate a hydrogen atom or an organic group, but at least one indicates an organic group. R1 and R2 may be bonded to form a ring structure and may contain a hetero atom bond. R3 indicates a single bond or an organic group. R4 to R9 each independently indicate a hydrogen atom, an organic group, etc., but R6 and R7 are never hydroxyl groups. R10 indicates a hydrogen atom or an organic group.
    Type: Application
    Filed: June 15, 2012
    Publication date: August 21, 2014
    Applicant: TOKYO OHKA KOGYO CO., LTD.
    Inventors: Dai Shiota, Mayumi Kuroko, Kunihiro Noda, Yoshinori Tadokoro
  • Publication number: 20140206537
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: March 25, 2014
    Publication date: July 24, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: James E. Hunter, William C. Lo, Gerald B. Watson, Akshay Patny, Gary D. Gustafson, Dan Pernich, William K. Brewster, Debra L. Camper, Beth Lorsbach, Michael R. Loso, Thomas C. Sparks, Hemant Joshi, Adiraj Mandaleswaran, Ramadevi Sanam, Rambabu Gundla, Pravin S. Iyer
  • Publication number: 20140171314
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171313
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171308
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171309
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171311
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171315
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171312
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Patent number: 8710272
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: April 29, 2014
    Assignee: Androscience Corporation
    Inventors: Charles C. Y. Shih, Qian Shi, Hui-Kang Wang, Ching-Yuan Su
  • Publication number: 20140094464
    Abstract: The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating Ape1 mediated diseases.
    Type: Application
    Filed: May 25, 2012
    Publication date: April 3, 2014
    Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: Mark R. Kelley, James H. Wikel
  • Patent number: 8686154
    Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: April 1, 2014
    Assignee: Emisphere Technologies, Inc.
    Inventors: Donald J. Sarubbi, Eugene N. Barantsevitch
  • Publication number: 20140088074
    Abstract: Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
    Type: Application
    Filed: May 29, 2012
    Publication date: March 27, 2014
    Applicant: NEWRON PHARMACEUTICALS S.P.A.
    Inventor: Paolo Pevarello
  • Publication number: 20140080832
    Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
    Type: Application
    Filed: November 13, 2013
    Publication date: March 20, 2014
    Applicant: MANNKIND CORPORATION
    Inventors: John Bruce PATTERSON, David Gregory LONERGAN, Gary A. FLYNN, Qingping ZENG, Peter V. PALLAI
  • Publication number: 20130324539
    Abstract: Improved methods of treating multiple sclerosis and/or psoriasis using prodrugs of methyl hydrogen fumarate are disclosed. The methods comprise administering certain prodrugs of methyl hydrogen fumarate. The methods are able to achieve high blood plasma concentrations of the active metabolite, methyl hydrogen fumarate, without causing significant gastrointestinal irritation. New prodrugs of methyl hydrogen fumarate are also disclosed.
    Type: Application
    Filed: May 30, 2013
    Publication date: December 5, 2013
    Inventors: Peter A. Virsik, David J. Wustrow, Thamil Annamalai
  • Publication number: 20130316906
    Abstract: The invention relates to novel compounds of the formula (I) in which R1, R2, R3, R4, R5, Y, Q and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as herbicides and/or pesticides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as pesticides and/or for preventing unwanted plant growth.
    Type: Application
    Filed: October 28, 2011
    Publication date: November 28, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alfred Angermann, Stefan Lehr, Guido Bojack, Reiner Fischer, Isolde Häuser-hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Arnd Voerste, Dieter Feucht
  • Publication number: 20130281664
    Abstract: The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e.
    Type: Application
    Filed: October 11, 2011
    Publication date: October 24, 2013
    Inventors: David Milstein, Ekambaram Balaraman, Chidambaram Gunanathan, Boopathy Gnanaprakasam, Jing Zhang
  • Publication number: 20130261121
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Application
    Filed: June 18, 2012
    Publication date: October 3, 2013
    Inventors: Charles C.Y. SHIH, Qian Shi, Hui-Kang Wang, Ching-Yuan Su
  • Patent number: 8546374
    Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: October 1, 2013
    Assignee: Abbvie Inc.
    Inventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biquin C. Li
  • Publication number: 20130231478
    Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
    Type: Application
    Filed: July 29, 2011
    Publication date: September 5, 2013
    Inventors: Ziao Xu, Yuanhai Zhao, Degang Li, Xiaoxiang Li
  • Publication number: 20130059853
    Abstract: Novel biaryl compounds with phosphodiesterase inhibitory activity of the general formula (I), wherein R1, R2, R3, X, Y, Z1, Z2, Z3, and Z4 have the meanings defined herein, as well as their use as therapeutic agents in the treatment of inflammatory diseases and conditions.
    Type: Application
    Filed: April 28, 2011
    Publication date: March 7, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Simon Feldbaek Nielsen, Anne Marie Horneman, Jesper Lau, Jens Christian Hojland Larsen
  • Publication number: 20120220577
    Abstract: The invention relates to naphthalene derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.
    Type: Application
    Filed: June 4, 2010
    Publication date: August 30, 2012
    Inventors: Markus Henrich, Angela Hansen, Jens Nagel, Valerjans Kauss, Jevgenijs Rozhkovs, Ginta Grunsteine, Dina Trifanova
  • Publication number: 20120220768
    Abstract: A process is provided for the synthesis of an amide. A primary or secondary amine and a primary alcohol, with the amine and the alcohol being either moieties of different reactants or moieties of the same molecule, are contacted in the presence of a Ruthenium (II) catalyst. The Ruthenium (II) catalyst is free of a phosphine ligand. The process is also carried out in the absence of a phosphine. Providing the Ruthenium (II) catalyst includes providing an N-heterocyclic carbene.
    Type: Application
    Filed: September 20, 2010
    Publication date: August 30, 2012
    Applicant: NANYANG TECHNOLOGICAL UNIVERSITY
    Inventors: Soon Hyeok Hong, Subhash Chandra Ghosh, Yao Zhang, Senthilkumar Muthaiah, Cheng Chen, Xiangya Xu
  • Publication number: 20120214782
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: August 17, 2011
    Publication date: August 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Gerald Juergen ROTH, Martin FLECK, Heike NEUBAUER, Bernd NOSSE
  • Publication number: 20120184438
    Abstract: This invention relates to agrochemical compositions comprising a benzamide compound of formula (I) where R1 is fluoro, methoxy or C1-4 alkyl; R2 and R3 are each independently optionally substituted C1-6 alkyl or optionally substituted C2-6 alkenyl; or R3 is hydrogen and R3 is optionally substituted C5-8 alkyl or optionally substituted C4-6 alkenyl or optionally substituted benzyl; or R2 and R3 and the nitrogen atom to which they are both attached together form an optionally substituted 5-, 6- or 7-membered ring, which ring optionally contains at least one further heteroatom selected from O, N and S; to the use of those benzamide compounds as solvents; to certain novel compounds of formula (I); and to a process for preparing those novel compounds.
    Type: Application
    Filed: July 15, 2010
    Publication date: July 19, 2012
    Applicant: SYNGENTA CROP PROTECTION, LLC
    Inventors: Gordon Alistair Bell, David Stock, Jeffrey Steven Wailes
  • Publication number: 20120178732
    Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: December 6, 2011
    Publication date: July 12, 2012
    Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
  • Patent number: 8212049
    Abstract: Disclosed is a new class of chiral bidentate ligands capable of performing asymmetric hydrogenation. Also disclosed are processes of performing asymmetric hydrogenation the chiral bidentate ligands.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: July 3, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Carl Alan Busacca, Jon Charles Lorenz
  • Publication number: 20120107902
    Abstract: The disclosure relates to methods for producing amide bonds and reagents related thereto. In some embodiments, the disclosure relates to methods of producing an amide comprising mixing an O-silylated thionoester and an amine under conditions such that an amide is formed. In another embodiment, the disclosure relates to mixing a thiolacid, a silylating agent, and an amine under conditions such that an amide is formed.
    Type: Application
    Filed: October 25, 2011
    Publication date: May 3, 2012
    Applicant: EMORY UNIVERSITY
    Inventors: Lanny S. Liebeskind, Wenting Wu, Zhihui Zhang, Hao Li, Angus A. Lamar
  • Publication number: 20120101080
    Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.
    Type: Application
    Filed: June 25, 2010
    Publication date: April 26, 2012
    Applicant: BioVersys AG
    Inventors: Ronald Schoenmakers, Wilfried Weber, Marc Gitzinger, Martin Fussenegger, Marcel Tigges, Peter Schneider
  • Publication number: 20120077959
    Abstract: Cobalt(II) complexes of the D2-symmetric chiral porphyrins are effective catalysts for asymmetric cyclopropanation reactions with succinimidyl diazoacetate. The Co-catalyzed reaction is suitable for various olefins, providing the corresponding cyclopropane succinimidyl esters in high yields and excellent diastereo- and enantio-selectivity.
    Type: Application
    Filed: February 16, 2010
    Publication date: March 29, 2012
    Inventors: X. Peter Zhang, Joshua V. Ruppel
  • Publication number: 20120071651
    Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.
    Type: Application
    Filed: September 14, 2011
    Publication date: March 22, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Yi-Yin Ku, Timothy A. Grieme, Jeffrey M. Kallemeyn, Mathew M. Mulhern
  • Publication number: 20120046293
    Abstract: The present invention relates to renin inhibitor compounds having the structure and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: October 10, 2011
    Publication date: February 23, 2012
    Applicant: Merck Frosst Canada Ltd.
    Inventors: CHRISTOPHER I. BAYLY, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
  • Publication number: 20110003784
    Abstract: Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.
    Type: Application
    Filed: June 16, 2010
    Publication date: January 6, 2011
    Inventors: David S. Garvey, Gregory J. LaRosa, Jeremy R. Greenwood, Mark L. Brewer, Tan Quach, Jamie B. Côté, Judd Berman
  • Publication number: 20100280034
    Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;
    Type: Application
    Filed: December 28, 2007
    Publication date: November 4, 2010
    Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
  • Publication number: 20100160285
    Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: December 18, 2009
    Publication date: June 24, 2010
    Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
  • Patent number: 7714131
    Abstract: The present invention provides a compounds the formula (IV): and methods for producing an ?-(phenoxy)phenylacetic acid compound of the formula: wherein R1 is a member selected from the group consisting of: each R2 is a member independently selected from the group consisting of (C1-C4)alkyl, halo, (C1-C4)haloalkyl, amino, (C1-C4)aminoalkyl, amido, (C1-C4)amidoalkyl, (C1-C4)sulfonylalkyl, (C1-C4)sulfamylalkyl, (C1-C4)alkoxy, (C1-C4)heteroalkyl, carboxy and nitro; the subscript n is 1 when R1 has the formula (a) or (b) and 2 when R1 has the formula (c) or (d); the subscript m is an integer of from 0 to 3; * indicates a carbon which is enriched in one stereoisomeric configuration; and the wavy line indicates the point of attachment of R1; and compounds.
    Type: Grant
    Filed: September 20, 2006
    Date of Patent: May 11, 2010
    Assignee: Metabolex, Inc.
    Inventors: Yan Zhu, Peng Cheng, Xin Chen, Jingyuan Ma, Zuchun Zhao
  • Patent number: 7671052
    Abstract: Novel phenyl compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, genitourinary disorders, inflammation, glaucoma, auto-immune diseases, ischemic conditions, immune-related disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, and as an appetite stimulant.
    Type: Grant
    Filed: October 3, 2005
    Date of Patent: March 2, 2010
    Assignee: Adolor Corporation
    Inventors: Roland E. Dolle, Karin Worm, Q. Jean Zhou
  • Patent number: 7666866
    Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: November 15, 2005
    Date of Patent: February 23, 2010
    Assignee: Eli Lilly and Company
    Inventors: Jeffry Bernard Franciskovich, David Kent Herron, Valentine Joseph Klimkowski, Angela Lynn Marquart, John Joseph Masters, David Mendel, Andrew Michael Ratz, Gerald Floyd Smith, Michael Robert Wiley, Ying Kwong Yee
  • Publication number: 20090324540
    Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Application
    Filed: June 10, 2009
    Publication date: December 31, 2009
    Applicant: Emisphere Technologies, Inc.
    Inventors: Donald J. Sarubbi, Eugene N. Barantsevitch
  • Publication number: 20090281085
    Abstract: Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Application
    Filed: February 3, 2009
    Publication date: November 12, 2009
    Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Rong Yang, Cédric Chauvignac