Chalcogen Bonded Directly To A Ring Carbon Of The 1,3-diazole Ring Patents (Class 546/273.7)
  • Patent number: 10370359
    Abstract: The present invention relates to a process for the preparation of anhydrous crystalline 2-(R)-[(3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl)methyl)sulfinyl]-1H-benzimidazole (dexlansoprazole).
    Type: Grant
    Filed: May 2, 2018
    Date of Patent: August 6, 2019
    Assignee: DIPHARMA FRANCIS S.r.L.
    Inventors: Alessandro Restelli, Alessio Bove, Gabriele Razzetti
  • Patent number: 9834540
    Abstract: It discloses Omeprazole Sodium semihydrate and preparation method thereof, wherein every mole of Omeprazole Sodium semihydrate contains 0.5 mole of water, and it has an X-ray diffraction pattern comprising characteristic peaks at diffraction angles 2? of 6.26°±0.1°, 11.10°±0.1°, 12.20°±0.1°, 15.58°±0.1°, 16.02°±0.1°, 17.12°±0.1°, 19.08°±0.1°, 21.00°±0.1°, 22.68°±0.1°, 23.48°±0.1°, 24.08°±0.1°, 26.52°±0.1° and 28.08°±0.1°. A raw material of Omeprazole Sodium hydrate is added into an organic solvent, stirring for 2˜9 hours at constant temperature of 25˜60° C., thereafter Omeprazole Sodium semihydrate is provided after filtrating and drying.
    Type: Grant
    Filed: November 20, 2015
    Date of Patent: December 5, 2017
    Assignees: TIANJIN UNIVERSITY, HAINAN LINGKANG PHARMACEUTICAL CO., LTD
    Inventors: Ying Bao, Linggang Tao, Long Li, Hongxun Hao, Jun Lv, Baohong Hou
  • Patent number: 9688658
    Abstract: An efficient process for increasing the optical purity of the active pharmaceutical ingredient Esomeprazole, by means of a substantially quantitative and selective precipitation and removal of Omeprazole is provided.
    Type: Grant
    Filed: February 23, 2016
    Date of Patent: June 27, 2017
    Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Paolo Stabile, Diego Rasia, Nicola Faccin, Moreno Bertolazzi
  • Patent number: 9428486
    Abstract: Object of the present invention is an improved process for the preparation of Esomeprazole (S)-BINOL complex which is a key intermediate for the synthesis of Esomeprazole and salts thereof.
    Type: Grant
    Filed: June 22, 2015
    Date of Patent: August 30, 2016
    Assignee: F.I.S.—Fabbrica Italiana Sintetici S.p.A.
    Inventors: Paolo Stabile, Moreno Bertolazzi, Nicola Faccin, Diego Rasia
  • Patent number: 9011882
    Abstract: The present disclosure provides DDAH modulators. Thus, the present disclosure provides a method of treating a patient suffering from a disorder characterized by excessive NO production and/or elevated DDAH activity, the method comprising administering to said patient an effective amount of a compound of one of formulae I-X. The present disclosure also provides a pharmaceutical composition comprising a compound of one of formulae I-X.
    Type: Grant
    Filed: February 13, 2013
    Date of Patent: April 21, 2015
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Yohannes T. Ghebremariam, John P. Cooke
  • Patent number: 8993779
    Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • Publication number: 20150080579
    Abstract: The present invention provides dexrabeprazole magnesium hydrate and a process for its preparation. The present invention also provides a magnesium, calcium or potassium salt of dexrabeprazole, optionally in amorphous form, and processes for its preparation.
    Type: Application
    Filed: November 19, 2014
    Publication date: March 19, 2015
    Inventors: Dharmaraj Ramachandra RAO, Rajendra Narayanrao KANKAN, Srinivas Laxminarayan PATHI, Dilip Ramdas BIRARI
  • Publication number: 20150072396
    Abstract: Low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations for modifying biomolecules is provided. Compositions, methods, and kits relating to low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations are also provided.
    Type: Application
    Filed: March 1, 2012
    Publication date: March 12, 2015
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Kyle Gee, Upinder Singh, Scott Grecian, Scott Clarke
  • Patent number: 8962851
    Abstract: The present invention discloses one pot process for enantioselective synthesis of single enantiomers of substituted sulphoxides 2-(2-pyridinylmethylsulphinyl)-1H-benzimidazoles or said compounds in an enantiomerically enriched form.
    Type: Grant
    Filed: December 26, 2012
    Date of Patent: February 24, 2015
    Assignee: Cadila Healthcare Limited
    Inventors: Shriprakash Dhar Dwivedi, Ashok Prasad, Daya Ram Pal
  • Publication number: 20150025115
    Abstract: A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.
    Type: Application
    Filed: October 7, 2014
    Publication date: January 22, 2015
    Inventors: Akira FUJISHIMA, Isao AOKI
  • Patent number: 8912337
    Abstract: The present invention provides dexrabeprazole magnesium hydrate and a process for its preparation. The present invention also provides a magnesium, calcium or potassium salt of dexrabeprazole, optionally in amorphous form, and processes for its preparation.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: December 16, 2014
    Assignee: Cipla Limited
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Srinivas Laxminarayan Pathi, Dilip Ramdas Birari
  • Patent number: 8907100
    Abstract: A process for purifying lansoprazole comprises 1) loading crude lansoprazole material onto a macroporous resin column; 2) concentrating the eluate from the column in a crystallization vessel by vacuum; 3) seeding lansoprazole crystal; 4) crystallizing the lansoprazole; 5) separating the precipitated crystals. The process especially has large processing capacity, can be carried out continuously and therefore suitable for industrial production, improving the quality of formulated products and reducing side effects.
    Type: Grant
    Filed: December 27, 2011
    Date of Patent: December 9, 2014
    Assignee: Hainan Lingkang Pharmaceutical Co., Ltd.
    Inventor: Linggang Tao
  • Publication number: 20140357870
    Abstract: The present invention relates to a process for the preparation of dexlansoprazole.xH2O, wherein x is about 0.0 to about 0.1, using dexlansoprazole.xH2O, wherein x is about 2.6 to about 50.
    Type: Application
    Filed: June 20, 2012
    Publication date: December 4, 2014
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Anmol Kumar Ray, Anu Mittal, Nagaraju Gottumukkala, Mahavir Singh Khanna, Rajesh Kumar Thaper, Mohan Prasad, Sudershan Kumar Arora
  • Publication number: 20140343104
    Abstract: The purpose of the present invention is to provide an osteogenesis promoter that can be administered locally and systemically and that is suitable for clinical application. Provided is an osteogenesis promoter that contains, as an active ingredient, at least one compound selected from the group consisting of phenazopyridine hydrochloride, riluzole hydrochloride, tranilast, rabeprazole, indoprofen, nabumetone, luteolin, leflunomide, lansoprazole, methiazole, thiabendazole, albendazole, tiaprofenic acid, balsalazide sodium salt, and cyclosporin A, or a pharmaceutically acceptable salt thereof. Preferably, rabeprazole or lansoprazole, which are proton pump inhibitors, is used as an active ingredient.
    Type: Application
    Filed: August 23, 2012
    Publication date: November 20, 2014
    Applicant: NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITY
    Inventors: Kinji Ohno, Naoki Ishiguro, Hiroshi Kitoh, Kenichi Mishima
  • Patent number: 8889873
    Abstract: The invention discloses a process for the preparation of compounds having structures typical for proton pump inhibitors in enantiomerically enriched form by using particular metal catalysts in an enantioselective oxidation step. Also disclosed are useful further processes and pure intermediate and subsequently final products.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: November 18, 2014
    Assignee: LEK Pharmaceuticals D.D.
    Inventors: Barbara Mohar, Renata Toplak Casar
  • Publication number: 20140336377
    Abstract: The present invention relates to arylamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: October 18, 2011
    Publication date: November 13, 2014
    Applicant: RAQUALIA PHARMA INC.
    Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Yoshimasa Arano, Mikio Morita
  • Patent number: 8884019
    Abstract: A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: November 11, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Akira Fujishima, Isao Aoki
  • Publication number: 20140329858
    Abstract: The present invention is directed to compounds of formula (I) wherein R1, R2, R3, and A are defined herein. The present invention also provides for pharmaceutical compositions comprising a compound of formula (I) as well as to the use of such compounds as androgen receptor antagonists for the treatment of diseases and conditions mediated by the androgen receptor, such as prostate cancer.
    Type: Application
    Filed: December 3, 2012
    Publication date: November 6, 2014
    Inventors: Mark Gary Bock, Dinesh Chikkanna, Marc Gerspacher, Vinayak Khairnar, Bharat Lagu, Chetan Pandit
  • Patent number: 8853411
    Abstract: The present invention relates to a process for the preparation of crystalline dexlansoprazole.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: October 7, 2014
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Anu Mittal, Anmol Kumar Ray, Mahavir Singh Khanna, Rajesh Kumar Thaper, Mohan Prasad
  • Publication number: 20140275550
    Abstract: A process for purifying lansoprazole comprises 1) loading crude lansoprazole material onto a macroporous resin column; 2) concentrating the eluate from the column in a crystallization vessel by vacuum; 3) seeding lansoprazole crystal; 4) crystallizing the lansoprazole; 5) separating the precipitated crystals. The process especially has large processing capacity, can be carried out continuously and therefore suitable for industrial production, improving the quality of formulated products and reducing side effects.
    Type: Application
    Filed: December 27, 2011
    Publication date: September 18, 2014
    Applicant: HAINAN LINGKANG PHARMACEUTICAL CO., LTD.
    Inventor: Linggang Tao
  • Publication number: 20140275175
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: May 30, 2014
    Publication date: September 18, 2014
    Applicant: NOVARTIS AG
    Inventors: Christopher Michael Adams, Sylvie Chamoin, Qi-Ying Hu, Chun Zhang
  • Patent number: 8822500
    Abstract: The present disclosure relates to the field of tyrosine kinase enzyme inhibition, in particular anaplastic lymphoma kinase (ALK) inhibition using novel small molecules. Provided are compounds capable to modulate ALK activity, compositions that comprise the compounds, and methods of using the compounds for the treatment or prevention of diseases or conditions that are characterized by ALK activity or expression.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: September 2, 2014
    Assignee: Chembridge Corporation
    Inventor: Nelson Levy
  • Publication number: 20140235859
    Abstract: The present invention relates to process for the resolution of omeprazole. The present invention further provides a novel compound of enantiomers of omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a solid of (R)- or (S)-omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a process for the preparation of esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention also provides a process for the preparation of recovery of chiral BINOL.
    Type: Application
    Filed: April 29, 2014
    Publication date: August 21, 2014
    Applicant: HETERO RESEARCH FOUNDATION
    Inventors: Bandi PARTHASARADHI REDDY, Kura RATHNAKAR REDDY, Rapolu RAJI REDDY, Dasari MURALIDHARA REDDY, Bandi VAMSI KRISHNA, Voggu RAMESH REDDY
  • Patent number: 8809542
    Abstract: A sodium salt, magnesium salt, lithium salt, potassium salt, calcium salt or barium salt of (R)-2 -[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2 -pyridinyl]methyl]sulfinyl]-1H-benzimidazole, and a pharmaceutical composition comprising the salt. The novel salt is useful as an excellent antiulcer agent.
    Type: Grant
    Filed: May 29, 2013
    Date of Patent: August 19, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Keiji Kamiyama, Hideo Hashimoto
  • Patent number: 8778975
    Abstract: Disclosed are: a compound which is stable in an acid, has an antibacterial effect against a bacterium Helicobacter pylori, can exert a satisfactory level of an antibacterial effect when used singly, does not affect an enteric bacterium, has an antibacterial effect against a bacterium resistant to an antibacterial agent, and has an inhibitory effect on gastric acid secretion; and a pharmaceutical composition comprising the compound. Specifically disclosed are: a compound represented by the general formula (I) or a salt thereof; and a pharmaceutical composition comprising the compound or the salt thereof: wherein R represents a linear alkyl group having 4 to 8 carbon atoms, preferably 5 to 7 carbon atoms.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: July 15, 2014
    Assignee: Link Geonomics, Inc.
    Inventors: Masaharu Ito, Masaichi Yamamoto
  • Patent number: 8778977
    Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: July 15, 2014
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
  • Publication number: 20140171635
    Abstract: Novel Hydrazone-based Fluorescent and Pro-Fluorescent Reagents and Linkers, including conjugationally extended hydrazine compositions, fluorescent hydrazone compositions, methods of the formation of hydrazones from the reaction of conjugationally extended hydrazines with conjugationally extended carbonyls, and methods of their use in assays systems are described. Use of these conjugationally compositions for direct colorimetric and fluorometric assays wherein a chromophore or the fluorophore is incorporated into the linker that is positioned between a reactive linking moiety and a biotin molecule.
    Type: Application
    Filed: August 14, 2013
    Publication date: June 19, 2014
    Applicant: Solulink Biosciences, Inc.
    Inventors: David A. Schwartz, Leopold Mendoza
  • Patent number: 8748619
    Abstract: The present invention relates to process for the resolution of omeprazole. The present invention further provides a novel compound of enantiomers of omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a solid of (R)- or (S)-omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a process for the preparation of esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention also provides a process for the preparation of recovery of chiral BINOL.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: June 10, 2014
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Bandi Vamsi Krishna, Voggu Ramesh Reddy
  • Publication number: 20140155602
    Abstract: The present invention relates to ethynyl compounds of formula I-C1 wherein R1, R2, R2?, R3, R3?, R6, U, V and W are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof, which are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: November 20, 2013
    Publication date: June 5, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Patent number: 8710082
    Abstract: The various embodiments relate to a compound comprising: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclyl, alkoxy, aryloxy, heteroaryloxy, alkoxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, alkylsulfonyl, arylsulfonyl, aminosulfonyl, alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, acyl, acylamino, amino, alkylamino, dialkylamino, arylamino, carboxylate (—CO2H), cyano, nitro, —CONH2, heteroarylamino, oxime, alkyloxime, aryloxime, amino-oxime or halogen when A, B, C, D, E, F, G, H, I, J, K, L, M, N, O, P, and Q are carbon, and X is O, NR (where R is hydrogen, alkyl, aryl or acyl), S, SO (sulfoxide), SO2 (sulfone), or C(R)2 (where R=H, alkyl, aryl, alkenyl, alkynyl, or acyl); or wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are each independently hydrogen or hydroxyl when A, B, C, D, E, F, G, H, I, J, K, L, M, N, O, P, and Q are each independently nitrogen, and compositions, combination
    Type: Grant
    Filed: February 4, 2012
    Date of Patent: April 29, 2014
    Assignee: Board of Trustees of Michigan State University
    Inventors: Christopher Waters, Karthik Sambanthamoorthy, Matthew Neiditch, Martin Semmelhack
  • Patent number: 8697880
    Abstract: The present invention relates to an improved method for the synthesis of the (S)- or (R)-enantiomer of omeprazole, characterized in that 2-[[(4-X-3,5-dimethylpyridin-2-yl)methyl]thio]-5-methoxy-1H-benzimidazole or 2-[[(4-X-3,5-dimethyl-1-oxidopyridin-2-yl)methyl]thio]-5-methoxy-1H-benzimidazole, wherein X is a leaving group, is oxidized into the corresponding sulphoxide which is obtained as a crystalline compound. Recrystallization of the thus obtained sulphoxide results in a compound of enhanced chemical and optical purity, which is subsequently transformed into the (S)- or (R)-enantiomer of omeprazole.
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: April 15, 2014
    Assignee: AstraZeneca AB
    Inventors: Sverker Von Unge, Christina Fregler
  • Publication number: 20140100370
    Abstract: A method of producing an oxidized compound is disclosed. An electric potential is measured of an oxidation reaction solution for producing an oxidized compound by an oxidation reaction, and an end point is determined of the oxidation reaction on the basis of a predefined decrease of the electric potential. Preferably, after the electric potential of the oxidation reaction solution is reached to a highest electric potential, a point is determined where the amount of an electric potential dropped from the highest electric potential reaches the predefined amount of an electric potential as the end point of the oxidation reaction. The method also may introduce an oxidation reaction terminating agent to the oxidation reaction solution immediately after determining the end point of the oxidation reaction.
    Type: Application
    Filed: October 31, 2013
    Publication date: April 10, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masayoshi Kaneko, Shigeo Yabuno, Kenji Iwaoka, Hidetoshi Nishimura
  • Patent number: 8691995
    Abstract: A one-pot process for the preparation of pantoprazole sodium by reacting 2-chloro methyl 3,4-dimethoxy pyridine hydrochloride with 2-mercapto-5-difluoromethoxy benzimidazole in an organic solvent system in presence of a phase transfer catalyst and further treating with aqueous sodium hypohalite solution comprising sodium hydroxide to obtain pantoprazole sodium in high yield and purity. The process for conversion of pantoprazole sodium to pantoprazole sodium sesquihydrate and also pantoprazole sodium monohydrate are also disclosed herein.
    Type: Grant
    Filed: December 15, 2005
    Date of Patent: April 8, 2014
    Assignee: Cipla Limited
    Inventors: Rajendra Narayanrao Kankan, Srinivas Laxminarayan Pathi
  • Patent number: 8685960
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: April 1, 2014
    Assignee: Elexopharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Patent number: 8680284
    Abstract: A preparation process of esomeprazole sodium substantially free of sulfone impurity including the steps of: a) combining either esomeprazole with a (C3-C8)-ketone or a mixture thereof, a sodium alkoxide, and a (C1-C5)-alcohol, or esomeprazole sodium with a (C3-C8)-ketone or a mixture thereof and a (C1-C5)-alcohol; and b) recovering the esomeprazole sodium formed from the reaction media by filtration.
    Type: Grant
    Filed: February 11, 2011
    Date of Patent: March 25, 2014
    Assignee: Esteve Quimica, S.A.
    Inventors: Marti Bartra Sanmartí, Ramón Berenguer Maimó, Joan Gabriel Solsona Rocabert
  • Publication number: 20140080828
    Abstract: This disclosure relates to antiviral compounds disclosed herein and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising 2-((benzo[d]imidazol-2-yl)thio)-N-phenylpropanamide derivatives, N-phenyl-2-((1-phenyl-benzo[d]imidazol-2-yl)thio)propanamide derivatives, or 2-((benzo[d]imidazol-2-yl)thio)-N-(2-chloro-4-methylphenyl)propanamide derivatives. The derivatives may be substituted with one or more substituents. Typically, the pharmaceutical composition comprises a compound of Formula (I), or salt, prodrug, or ester thereof wherein X, Y, and R1 to R7 are described herein.
    Type: Application
    Filed: March 28, 2012
    Publication date: March 20, 2014
    Applicants: CHILDREN'S HEATLHCARE OF ATLANTA, INC., EMORY UNIVERSITY
    Inventors: Richard K. Plemper, James P. Snyder, Aiming Sun, John M. Ndungu, Jeong-Joong Yoon
  • Patent number: 8658799
    Abstract: The present invention relates to a new process for the preparation of crystal modifications for use in the preparation of esomeprazole sodium salt. Further, the present invention also relates to the use of the new crystal modifications for the treatment of gastrointestinal disorders, pharmaceutical compositions containing them as well as the crystal modifications, as such.
    Type: Grant
    Filed: June 20, 2005
    Date of Patent: February 25, 2014
    Assignee: Astrazeneca AB
    Inventors: Martin Bohlin, Ursula Noreland
  • Publication number: 20140012006
    Abstract: A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.
    Type: Application
    Filed: September 6, 2013
    Publication date: January 9, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Akira FUJISHIMA, Isao AOKI
  • Publication number: 20140005164
    Abstract: The present invention relates to novel compounds of formula (I): as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.
    Type: Application
    Filed: March 23, 2012
    Publication date: January 2, 2014
    Applicant: Siena Biotech S.p.A.
    Inventors: Maurizio Varrone, Massimiliano Travagli, Giacomo Minetto, Lucia Cesari, Simone Galeazzi, Andrea Caricasole, Antonio Chiumiento, Massimiliano Salerno
  • Publication number: 20130345261
    Abstract: The various embodiments relate to a compound comprising: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclyl, alkoxy, aryloxy, heteroaryloxy, alkoxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, alkylsulfonyl, arylsulfonyl, aminosulfonyl, alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, acyl, acylamino, amino, alkylamino, dialkylamino, arylamino, carboxylate (—CO2H), cyano, nitro, —CONH2, heteroarylamino, oxime, alkyloxime, aryloxime, amino-oxime or halogen when A, B, C, D, E, F, G, H, I, J, K, L, M, N, O, P, and Q are carbon, and X is O, NR (where R is hydrogen, alkyl, aryl or acyl), S, SO (sulfoxide), SO2 (sulfone), or C(R)2 (where R?H, alkyl, aryl, alkenyl, alkynyl, or acyl); or wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are each independently hydrogen or hydroxyl when A, B, C, D, E, F, G, H, I, J, K, L, M, N, O, P, and Q are each independently nitrogen, and compositions, combination
    Type: Application
    Filed: February 4, 2012
    Publication date: December 26, 2013
    Inventors: Christopher Waters, Karthik Sambanthamoorthy, Matthew Neiditch, Martin Semmelhack
  • Publication number: 20130345200
    Abstract: Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Application
    Filed: August 7, 2013
    Publication date: December 26, 2013
    Applicant: GlaxoSmithKline LLC
    Inventors: James Brackley, III, Joelle Lorraine Burgess, Seth Grant, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
  • Patent number: 8614331
    Abstract: A process for preparing esomeprazole sodium comprises the steps of providing a solution of esomeprazole sodium in a solvent constituted mainly of methanol or only of methanol; and carrying out precipitation or crystallization of esomeprazole sodium from said solution. Esomeprazole sodium is preferably obtained from pure form of neutral racemate through chiral chromatography using methanol-based mobile phase, and a subsequent reaction with sodium source. Novel crystal and semicrystal forms of esomeprazole sodium can be provided repeatedly and in physically stable and highly pure form.
    Type: Grant
    Filed: July 8, 2009
    Date of Patent: December 24, 2013
    Assignee: Lek Pharmaceuticals D.D.
    Inventor: Dejan Mandic
  • Patent number: 8592600
    Abstract: The invention relates to crystalline forms of racemic ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl) 1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising a crystalline Form of ilaprazole according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: November 26, 2013
    Assignee: Il Yang Pharmaceutical Company, Ltd.
    Inventors: John M. Brackett, David T. Jonaitis, Wei Lai, Jih Hua Liu, Stephan D. Parent, Jinyu Shen
  • Patent number: 8592598
    Abstract: The instant invention describes a method of producing a crystal of an imidazole compound or a salt thereof, which comprises suspending a solvate of the imidazole compound into a solution containing water, alcohol, and a basic substance.
    Type: Grant
    Filed: September 13, 2005
    Date of Patent: November 26, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masayoshi Kaneko, Shigeo Yabuno, Kenji Iwaoka, Hidetoshi Nishimura
  • Patent number: 8592601
    Abstract: A precursor phase of the magnesium tetrahydrate salt of an omeprazole enantiomer, and also processes for preparing it and its use for the preparation of the magnesium tetrahydrate salt are described. Crystals of the magnesium tetrahydrate salt thus obtained, and their uses, especially in the synthesis of the dihydrate form A of the magnesium salt of the enantiomer or as medicament are also disclosed.
    Type: Grant
    Filed: March 31, 2011
    Date of Patent: November 26, 2013
    Assignees: Produits Chimiques Auxiliaires et de Synthese, Universite de Rouen
    Inventors: Snella Chouippe, Jean-Marie Schneider, Guillaume Tauvel, Gerard Coquerel
  • Patent number: 8592599
    Abstract: The invention relates to crystalline forms of racemic ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl)1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising a crystalline Form of ilaprazole according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: November 26, 2013
    Assignee: Il Yang Pharmaceutical Company, Ltd.
    Inventors: John M. Brackett, David T. Jonaitis, Wei Lai, Jih Hua Liu, Stephan D. Parent, Jinyu Shen
  • Patent number: 8586752
    Abstract: Disclosed are a crystalline S-omeprazole strontium hydrate for the prevention or treatment of gastric acid-related diseases, which has high optical purity, theremostability, solubility and nonhygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: November 19, 2013
    Assignee: Hanmi Science Co., Ltd
    Inventors: Tae Hee Ha, Hee Sook Oh, Won Jeoung Kim, Chang Hee Park, Eun Young Kim, Young Hoon Kim, Kwee Hyun Suh, Gwan Sun Lee
  • Publication number: 20130303772
    Abstract: Disclosed are a crystalline S-omeprazole strontium hydrate for the prevention or treatment of gastric acid-related diseases, which has high optical purity, thermostability, solubility and nonhygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.
    Type: Application
    Filed: July 16, 2013
    Publication date: November 14, 2013
    Inventors: Tae Hee HA, Hee Sook OH, Won Jeoung KIM, Chang Hee PARK, Eun Young KIM, Young Hoon KIM, Kwee Hyun SUH, Gwan Sun LEE
  • Publication number: 20130281704
    Abstract: A sodium salt, magnesium salt, lithium salt, potassium salt, calcium salt or barium salt of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole, and a pharmaceutical composition comprising the salt. The novel salt is useful as an excellent antiulcer agent.
    Type: Application
    Filed: May 29, 2013
    Publication date: October 24, 2013
    Inventors: Keiji KAMIYAMA, Hideo HASHIMOTO
  • Patent number: 8563733
    Abstract: A novel process for the preparation of omeprazole and its enantiomers, such as esomeprazole, as well as the preparation of related 2-(2-pyridinylmethyl-sulphinyl)-1H-benzimidazoles, including pantoprazole, lansoprazole and rabeprazole, as recemates or single enantiomers, and their alkali or alkaline salts has been developed. The novel process involves the surprising discovery that protection of the free-base benzimidazole sulfoxide (e.g. omeprazole or esomeprazole), by reaction with an alkyl, aryl or aralkyl chloroformate following oxidation of the corresponding sulfide, eliminates the need for its direct isolation. Subsequent removal of the protecting group with a solution of alkali or alkaline earth alkoxide in a C1-C4 alcohol directly provides the corresponding salt. By eliminating the need to handle the free-base benzimidazole sulfoxide, this advantageous procedure provides increased chemical yields over processes described in the art.
    Type: Grant
    Filed: August 12, 2010
    Date of Patent: October 22, 2013
    Assignee: Apotex Pharmachem Inc
    Inventors: Fan Wang, Laura Kaye Montemayor, Daqing Che, Stephen E. Horne