Chalcogen Bonded Directly To Ring Carbon Of The Quinuclidine Ring System Patents (Class 546/137)
  • Patent number: 10570127
    Abstract: Provided herein is a bulk composition comprising the trihydrate form of (3S, 4R, 3?R)-6-[4-(4-amino-5-chloro-2-methoxy-benzoylamino)-3-methoxy-piperidin-1-yl]-hexanoic acid 1-azabicyclo[2.2.2]oct-3?-yl ester di-hydrochloride salt. Provided are also pharmaceutical compositions and dosage forms comprising the trihydrate form, and methods and uses for treating a gastrointestinal disorder in a subject with the trihydrate form. In some embodiments, the gastrointestinal disorder is gastroesophageal reflux disease (GERD), dyspepsia (such as functional dyspepsia or functional motility disorder), gastroparesis, paralytic ileus, post-operative ileus, emesis, nausea, heartburn, intestinal pseudo-obstruction, irritable bowel syndrome (IBS), constipation, enteral feeding intolerance (EFI), or esophagitis. In some embodiments, the gastrointestinal disorder is post-operative ileus, chronic grass sickness, constipation, megacolon, gastritis, gastrointestinal stasis, or abomasal emptying defect.
    Type: Grant
    Filed: November 5, 2018
    Date of Patent: February 25, 2020
    Assignee: Renexxion, LLC
    Inventors: Pascal Jean Druzgala, Jien Heh Tien
  • Patent number: 9199980
    Abstract: Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.
    Type: Grant
    Filed: December 5, 2013
    Date of Patent: December 1, 2015
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Elisabetta Armani, Gabriele Amari, Mauro Riccaboni, Andrea Rizzi, Charles Baker-Glenn, Wesley Blackaby, Herve′ Van de Poel, Ben Whittaker
  • Patent number: 9139580
    Abstract: The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
    Type: Grant
    Filed: September 18, 2013
    Date of Patent: September 22, 2015
    Assignee: Genzyme Corporation
    Inventors: Elyse Bourque, Bradford Hirth, Renato Sklerj, Elina Makino, Fazeela Morshed, Lingyun Li, Paul Mason, John P. Leonard, James Lillie, Hanlan Liu, Mary A. Cromwell, Bing Wang, Thomas O'Shea
  • Patent number: 9126993
    Abstract: The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: September 8, 2015
    Assignee: Genzyme Corporation
    Inventors: Elyse Bourque, Bradford Hirth, Renato Sklerj, Elina Makino, Fazeela Morshed, Lingyun Li, Paul Mason, John P. Leonard, James Lillie, Hanlan Liu, Mary A. Cromwell, Bing Wang, Thomas O'Shea
  • Patent number: 9114390
    Abstract: An organocatalyst for oxidizing alcohols in which a primary alcohol is selectively oxidized in a polyol substrate having a plurality of alcohols under environmentally-friendly conditions. The organic oxidation catalyst has an oxygen atom bonded to a nitrogen atom of an azanoradamantane skeleton and at least one alkyl group at positions 1 and 5. The oxidation catalyst has higher activity than TEMPO, which is an existing oxidation catalyst, in the selective oxidation reaction of primary alcohols, and better selectivity than AZADO and 1-Me-AZADO. This DMN-AZADO can be applied to the selective oxidation reaction of primary alcohols that contributes to shortening the synthesizing process for pharmaceuticals, pharmaceutical raw materials, agricultural chemicals, cosmetics, organic materials, and other such high value-added organic compounds.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: August 25, 2015
    Assignee: TOHOKU UNIVERSITY
    Inventors: Yoshiharu Iwabuchi, Masatoshi Shibuya, Ryusuke Doi
  • Patent number: 9035058
    Abstract: A method of synthesizing a crystalline molecular sieve having an MSE framework type comprises crystallizing a reaction mixture comprising a source of water, a source of an oxide of a tetravalent element, Y, selected from at least one of silicon, tin, titanium, vanadium, and germanium, optionally a source of a trivalent element, X, a source of an alkali or alkaline earth metal, M, and a source of organic dications, Q, such as 3-hydroxy-1-(4-(1-methylpiperidin-1-ium-1-yl)butyl)quinuclidin-1-ium, 3-hydroxy-1-(5-(1-methylpiperidin-1-ium-1-yl)pentyl)quinuclidin-1-ium, 1,1?-(butane-1,4-diyl)bis(1-methylpiperidin-1-ium), 1,1?-(pentane-1,5-diyl)bis(1-methylpiperidin-1-ium), 1,1?-(hexane-1,6-diyl)bis(1-methylpiperidin-1-ium), and 1,1?-((3as,6as)-octahydropentalene-2,5-diyl)bis(1-methylpiperidin-1-ium).
    Type: Grant
    Filed: November 14, 2014
    Date of Patent: May 19, 2015
    Assignee: EXXONMOBIL RESEARCH AND ENGINEERING COMPANY
    Inventors: Simon C. Weston, Karl G. Strohmaier, Hilda B. Vroman
  • Patent number: 9018379
    Abstract: Disclosed herein is a method of preparing solifenacin or a salt thereof, including the steps of: (a) reacting (R)-quinuclidinol with bis(pentafluorophenyl)carbonate in an organic solvent to prepare a solifenacin intermediate, (3R)-1-azabicyclo[2,2,2]oct-3-yl pentafluorophenylcarbonate, and (b) reacting the solifenacin intermediate with (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline in an organic solvent to prepare solifenacin. The method is advantageous in that high-purity solifenacin or a salt thereof can be simply and efficiently prepared with high yield using a novel intermediate.
    Type: Grant
    Filed: March 21, 2013
    Date of Patent: April 28, 2015
    Assignee: Kyung Dong Pharm. Co., Ltd.
    Inventors: Byoung Suk Lee, Sang Hoon Shin, Ki Young Lee
  • Publication number: 20150112072
    Abstract: Disclosed herein is a method of preparing solifenacin or a salt thereof, including the steps of: (a) reacting (R)-quinuclidinol with bis(pentafluorophenyl)carbonate in an organic solvent to prepare a solifenacin intermediate, (3R)-1-azabicyclo[2,2,2]oct-3-yl pentafluorophenylcarbonate, and (b) reacting the solifenacin intermediate with (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline in an organic solvent to prepare solifenacin. The method is advantageous in that high-purity solifenacin or a salt thereof can be simply and efficiently prepared with high yield using a novel intermediate.
    Type: Application
    Filed: March 21, 2013
    Publication date: April 23, 2015
    Applicant: Kyung Dong Pharm. Co., Ltd.
    Inventors: Byoung Suk Lee, Sang Hoon Shin, Ki Young Lee
  • Patent number: 9000212
    Abstract: Provided by the present invention is a method for efficient oxidation of alcohols by using, as a catalyst for dehydrogenation oxidation, a ruthenium complex which can be easily produced and easily handled and is obtainable at a relatively low cost. The invention relates to a method of producing a compound having a carbonyl group by dehydrogenation oxidation of alcohols by using as a catalyst the ruthenium carbonyl complex represented by the following general formula (1) RuXY(CO)(L) (1) (in the general formula (1), X and Y may be the same or different from each other and represent an anionic ligand, and L represents a tridentate aminodiphosphine ligand).
    Type: Grant
    Filed: April 18, 2012
    Date of Patent: April 7, 2015
    Assignee: Takasago International Corporation
    Inventors: Taichiro Touge, Kunimori Aoki, Hideki Nara, Wataru Kuriyama
  • Publication number: 20150087841
    Abstract: A method of synthesizing a crystalline molecular sieve having an MSE framework type comprises crystallizing a reaction mixture comprising a source of water, a source of an oxide of a tetravalent element, Y, selected from at least one of silicon, tin, titanium, vanadium, and germanium, optionally a source of a trivalent element, X, a source of an alkali or alkaline earth metal, M, and a source of organic dications, Q, such as 3-hydroxy-1-(4-(1-methylpiperidin-1-ium-1-yl)butyl)quinuclidin-1-ium, 3-hydroxy-1-(5-(1-methylpiperidin-1-ium-1-yl)pentyl)quinuclidin-1-ium, 1,1?-(butane-1,4-diyl)bis(1-methylpiperidin-1-ium), 1,1?-(pentane-1,5-diyl)bis(1-methylpiperidin-1-ium), 1,1?-(hexane-1,6-diyl)bis(1-methylpiperidin-1-ium), and 1,1?-((3as,6as)-octahydropentalene-2,5-diyl)bis(1-methylpiperidin-1-ium).
    Type: Application
    Filed: November 14, 2014
    Publication date: March 26, 2015
    Applicant: ExxonMobil Research and Engineering Company
    Inventors: Simon C. Weston, Karl G. Strohmaier, Hilda B. Vroman
  • Publication number: 20150065511
    Abstract: The invention provides compositions and methods for the treatment of presbyopia. The compositions preferably use aceclidine separate or together with a cycloplegic agent and/or with a nonionic surfactant and viscosity enhancer, and or with low concentrations of a selective ?-2 adrenergic receptor agonist.
    Type: Application
    Filed: March 24, 2014
    Publication date: March 5, 2015
    Applicant: Presbyopia Therapies, LLC
    Inventors: Gerald Horn, Lee Nordan
  • Publication number: 20150065443
    Abstract: A composition having a structure of: X-L-Y wherein X comprises at least one embelin moiety; L comprises a linker; and Y comprises a hydrophilic moiety. Also disclosed is a micelle that includes: a core that includes at least one hydrophobic active agent and at least one embelin moiety; and a hydrophilic zone surrounding the core and comprising at least one hydrophilic moiety.
    Type: Application
    Filed: April 4, 2013
    Publication date: March 5, 2015
    Applicant: University of Pittsburgh - of the Commonwealth System of Higher Educatioon
    Inventors: Song Li, Xiang Gao, Yixian Huang, Jianqin Lu
  • Patent number: 8952165
    Abstract: A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: February 10, 2015
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Cheol Young Maeng, Young Koo Jang, Su Bong Cha, Hye Won Shin, Chan Mi Joung, Eun Jung Yi
  • Patent number: 8940763
    Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release solifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release solifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 9, 2012
    Date of Patent: January 27, 2015
    Assignee: TheraVida, Inc.
    Inventors: Mehdi Paborji, Wendy Jade Limayo Hernandez, Kenneth L. Duchin, Roger S. Flugel
  • Publication number: 20140371460
    Abstract: The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Elyse BOURQUE, Cassandra CELATKA, Bradford HIRTH, Markus METZ, Zhong ZHAO, Renato SKLERJ, Yibin XIANG, Katherine JANCSICS, John MARSHALL, Seng CHENG, Ronald SCHEULE, Mario CABRERA-SALAZAR, Andrew GOOD
  • Publication number: 20140364451
    Abstract: In various embodiments, compositions and methods are provided for treatment and/or prevention of amyloidogenic diseases. In certain embodiments, the methods entail administering an effective amount of a tropinol ester to a subject in need thereof for prophylactic or therapeutic effect. The methods are particularly useful for prophylactic and therapeutic treatment of Alzheimer's disease. In certain embodiments, methods of reducing the risk, lessening the severity, or delaying the progression or onset of a disease characterized by beta-amyloid deposits in the brain of a mammal are also provided. In certain embodiments, methods of directly or indirectly inhibiting the C-terminal cleavage of APP resulting in the formation of APP-C31 peptide and APPneo (AP-P664) in a mammal are provided.
    Type: Application
    Filed: August 1, 2012
    Publication date: December 11, 2014
    Applicant: BUCK INSTITUTE FOR RESEARCH ON AGING
    Inventors: Varghese John, Dale E. Bredesen
  • Publication number: 20140303126
    Abstract: A compound according to formula (I) wherein z© is a phenyl ring, a C4 to C9 heteroaromatic compound containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl group; R1, R2 and R3 each independently represent a hydrogen or halogen atom, or a hydroxy group, or a phenyl, —OR4, —SR4, —NR4R5, —NHCOR4, —CONR4R5, —CN, —NO2, —COOR4 or —CF3 group, or a straight or branched lower alkyl group which may optionally be substituted, for example, with a hydroxy or alcoxy group, wherein R4 and R5 each independently represent a hydrogen atom, straight or branched lower alkyl group, or together form an alicyclic ring; or R1 and R2 together form an aromatic, alicyclic or heterocyclic ring; n is an integer from 0 to 4; A represents a —CH2—, —CH?CR6, —CR6?CH—, —CR6R7—, —CO—, —O—, —S—, —S(O)—, SO2 or NR6— group, wherein R6 and R7 each independently represent a hydrogen atom, straight or branched lower alkyl group, or R6 and R7 together form an alicyclic ring; in is an integer from 0 to 8; pro
    Type: Application
    Filed: June 20, 2014
    Publication date: October 9, 2014
    Inventors: Maria Dolors FERNANDEZ FORNER, Maria PRAT QUINONES, Maria Antonia BUIL ALBERO
  • Publication number: 20140303231
    Abstract: The invention features therapeutic compositions comprising agents useful for the treatment or prevention of pruritis, and methods useful for identifying such agents.
    Type: Application
    Filed: January 24, 2014
    Publication date: October 9, 2014
    Applicant: The Johns Hopkins University
    Inventors: Xinzhong Dong, Qin Liu, David J. Anderson
  • Publication number: 20140303374
    Abstract: Provided by the present invention is a method for efficient oxidation of alcohols by using, as a catalyst for dehydrogenation oxidation, a ruthenium complex which can be easily produced and easily handled and is obtainable at a relatively low cost. The invention relates to a method of producing a compound having a carbonyl group by dehydrogenation oxidation of alcohols by using as a catalyst the ruthenium carbonyl complex represented by the following general formula (1) RuXY(CO)(L) (1) (in the general formula (1), X and Y may be the same or different from each other and represent an anionic ligand, and L represents a tridentate aminodiphosphine ligand).
    Type: Application
    Filed: April 18, 2012
    Publication date: October 9, 2014
    Applicant: TAKASAGO INTERNATIONAL CORPORATION
    Inventors: Taichiro Touge, Kunimori Aoki, Hideki Nara, Wataru Kuriyama
  • Patent number: 8835638
    Abstract: This invention relates to 1,3-oxathiolane derivatives (I), processes for the preparation of 1,3-oxathiolane derivatives and intermediate compounds thereof.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: September 16, 2014
    Assignee: Apotex Pharmachem Inc.
    Inventors: Craig Stewart, Michael B. Johansen, Probal Kanti Datta, Yajun Zhao
  • Publication number: 20140255381
    Abstract: The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
    Type: Application
    Filed: September 18, 2013
    Publication date: September 11, 2014
    Applicant: GENZYME CORPORATION
    Inventors: Elyse BOURQUE, Cassandra CELATKA, Bradford HIRTH, Markus METZ, Zhong ZHAO, Renato SKLERJ, Yibin XIANG, Katherine JANCSICS, John MARSHALL, Seng CHENG, Ronald SCHEULE, Mario CABRERA-SALAZAR, Andrew GOOD
  • Publication number: 20140256730
    Abstract: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
    Type: Application
    Filed: January 13, 2014
    Publication date: September 11, 2014
    Applicant: Corsair Pharma, Inc.
    Inventors: Cyrus K. BECKER, Jürg R. PFISTER, Gwenaella RESCOURIO, Meenakshi S. VENKATRAMAN, Xiaoming ZHANG
  • Publication number: 20140228575
    Abstract: The invention provides a new process for the preparation of solifenacin or a pharmaceutically acceptable acid addition salt thereof, comprising reacting (R)-quinuclidin-3-yl phenethylcarbamate with benzaldehyde in the presence of an acid to obtain a diasteroisomeric mixture (S,R)—((R)-quinuclidin-3-yl) 1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate of formula (IV) which can be resolved and the solifenacin or a pharmaceutically acceptable acid addition salt thereof recovered. The invention also provides the new key intermediate (R)-quinuclidin-3-yl phenethylcarbamate involved in the process. Further the invention provides a method for the transformation of (R)—((R)-quinuclidin-3-yl) 1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate into a diasteroisomeric mixture (S,R)—((R)-quinuclidin-3-yl) 1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate.
    Type: Application
    Filed: June 22, 2011
    Publication date: August 14, 2014
    Applicant: ISOCHEM
    Inventors: Jordi Bessa Bellunt, Marina Corbella Morato
  • Publication number: 20140220125
    Abstract: The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.
    Type: Application
    Filed: July 12, 2012
    Publication date: August 7, 2014
    Applicant: NOVARTIS AG
    Inventors: Wolfgang Marterer, Mahavir Prashad, Edwin Bernard Villhauer, Liladhar Murlidhar Waykole, James Anthony Vivelo, Bertrand Sutter, Jean-Claude Bianchi, Raeann Wu, Denis Har, Piotr H. Karpinski, Massimo Pignone, Doris Stingelin, Eckart Buerger
  • Patent number: 8772491
    Abstract: The present invention relates to a process for the preparation of Solifenacin succinate by condensing a compound of formula (IVb) with (RS)-3-quinuclidinol, wherein, R represents methyl, ethyl, isopropyl; to produce a diastereomeric mixture of (1S)-3,4-dihydro-1-phenyl-2(1H)-isoquinolinecarboxylic acid (3RS)-1-azabicyclo[2.2.2]oct-3-yl ester, which is treated with succinic acid in a solvent or mixture of solvents to produce optically pure Solifenacin succinate, Formula (X).
    Type: Grant
    Filed: June 20, 2011
    Date of Patent: July 8, 2014
    Assignee: Aurobindo Pharma Ltd
    Inventors: Anand Gopalkrishna Kamat, Joseph Prabahar Koilpillai, Naga Trinadhachari Ganala, Venkata Lakshmi Upputuri, Venkata Balalji Boddu, Sivakumaran Meenakshisunderam
  • Patent number: 8772314
    Abstract: Alkaloid aminoester derivatives according to formula (I) and (VI) act as muscarinic receptor antagonists.
    Type: Grant
    Filed: November 23, 2011
    Date of Patent: July 8, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Mauro Riccaboni, Marco Farina
  • Patent number: 8765785
    Abstract: The invention concerns fumarate salts of solifenacin, as well as pharmaceutical compositions comprising fumarate salts of solifenacin. The invention furthermore concerns a process for preparing solifenacin and salts thereof. The fumarate salt provides improved properties over the known solifenacin salts, especially in terms of its stability. The novel process for its preparation is furthermore improved over known processes for preparing solifenacin in that it provides a higher yield and recovers a greater amount of starting material.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: July 1, 2014
    Assignee: Crystal Pharma, S.A.U.
    Inventors: Gerardo Gutiérrez Fuentes, Antonio Lorente Bonde-Larsen, Jaime del Campo López-Bachiller, Celso Sandoval Rodríguez, Yolanda Fernández Sainz
  • Patent number: 8759524
    Abstract: A process is provided for efficiently producing an optically active 3-quinuclidinol derivative of high optical purity using a readily available ruthenium compound as an asymmetric reduction catalyst. This process is a process for producing an optically active 3-quinuclidinol derivative represented by the following formula (III) comprising asymmetrically hydrogenating a 3-quinuclidinone derivative represented by the following formula (I) in the presence of a ruthenium compound (II) represented by formula (II): Ru(X)(Y)(Px)n[R1R2C*(NR3R4)-A-R5R6C*(NR7R8)] (in the formulas, R represents a hydrogen atom or C7 to C18 aralkyl group and the like, X and Y represent hydrogen atoms or halogen atoms and the like, Px represents a phosphine ligand, n represents 1 or 2, R1 to R8 represent hydrogen atoms or C1 to C20 alkyl groups and the like, * represents an optically active carbon atom and A represents an ethylene group and the like).
    Type: Grant
    Filed: April 8, 2013
    Date of Patent: June 24, 2014
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Takeshi Ohkuma, Noriyoshi Arai, Masaya Akashi, Hirohito Oooka, Tsutomu Inoue
  • Patent number: 8748613
    Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: June 10, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Cristina Pesenti, Stefano Bossolo
  • Publication number: 20140155373
    Abstract: Compounds of formula (I) described herein are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.
    Type: Application
    Filed: December 5, 2013
    Publication date: June 5, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Elisabetta Armani, Gabriele Amari, Mauro Riccaboni, Charles Baker-Glenn
  • Publication number: 20140155428
    Abstract: Compounds of formula (I) defined herein are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of a disease of the respiratory tract characterized by airway obstruction.
    Type: Application
    Filed: December 5, 2013
    Publication date: June 5, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A
    Inventors: Elisabetta ARMANI, Gabriele Amari, Mauro Riccaboni, Charles Baker-Glenn
  • Publication number: 20140155427
    Abstract: Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.
    Type: Application
    Filed: December 5, 2013
    Publication date: June 5, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Elisabetta Armani, Gabriele Amari, Mauro Riccaboni, Andrea Rizzi, Charles Baker-Glenn, Wesley Blackaby, Herve' Van de Poel, Ben Whittaker
  • Patent number: 8716309
    Abstract: A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: May 6, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Cheol Young Maeng, Young Koo Jang, Su Bong Cha, Hye Won Shin, Chan Mi Joung, Hwa Ryun Cha, Eun Jung Yi
  • Publication number: 20140057921
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula (I) wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals in the prevention and treatment of psychotic and neurodegenerative disorders. The claimed compounds act as nicotinic acetylcholine receptors (NACHR) ligands.
    Type: Application
    Filed: October 31, 2013
    Publication date: February 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Dominik FEUERBACH, Mathias FREDERIKSEN, Konstanze HURTH, Bernard Lucien ROY
  • Patent number: 8629160
    Abstract: The present invention relates to alkaloid aminoester compounds which act as muscarinic receptor antagonists, processes for their preparation, compositions comprising them, and therapeutic uses thereof.
    Type: Grant
    Filed: June 22, 2011
    Date of Patent: January 14, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Mauro Riccaboni, Antonio Caligiuri
  • Publication number: 20130317059
    Abstract: A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.
    Type: Application
    Filed: January 30, 2012
    Publication date: November 28, 2013
    Applicant: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Cheol Young Maeng, Young Koo Jang, Su Bong Cha, Hye Won Shin, Chan Mi Joung, Hwa Ryun Cha, Eun Jung Yi
  • Publication number: 20130310357
    Abstract: Provided herein are azolyl urea compounds for treatment of CSF-1R kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Application
    Filed: May 26, 2011
    Publication date: November 21, 2013
    Applicant: AMBIT BIOSCIENCES CORPORATION
    Inventor: Gang Liu
  • Publication number: 20130296340
    Abstract: A pyridone derivative compound and a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof, and a preventive or therapeutic pharmaceutical composition for cognitive disorders that includes the pyridone derivative compound or a pharmaceutically acceptable salt, isomer, solvate or hydrate thereof.
    Type: Application
    Filed: January 30, 2012
    Publication date: November 7, 2013
    Inventors: Cheol Young Maeng, Young Koo Jang, Su Bong Cha, Hye Won Shin, Chan Mi Joung, Eun Jung Yi
  • Patent number: 8563577
    Abstract: The present invention relates to alkaloid aminoester compounds which act as muscarinic receptor antagonists, processes for the preparation of such a compound, compositions which contain such a compound, and therapeutic uses of such a compound.
    Type: Grant
    Filed: June 22, 2011
    Date of Patent: October 22, 2013
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Mauro Riccaboni
  • Publication number: 20130274474
    Abstract: This invention relates to 1,3-oxathiolane derivatives (I), processes for the preparation of 1,3-oxathiolane derivatives and intermediate compounds thereof.
    Type: Application
    Filed: April 12, 2013
    Publication date: October 17, 2013
    Applicant: APOTEX PHARMACHEM INC.
    Inventors: Craig Stewart, Michael B. Johansen, Probal Kanti Datta, Yajun Zhao
  • Patent number: 8524736
    Abstract: The subject invention provides stereoisomeric compounds of formula (X): wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited to, gastroparesis, gastroesophageal reflux and related conditions. The compounds of the subject invention are also useful in treating a variety of conditions involving the central nervous system.
    Type: Grant
    Filed: February 10, 2012
    Date of Patent: September 3, 2013
    Assignee: Armetheon, Inc.
    Inventors: Ian Irwin, Monica Palme, Cyrus Becker, Pascal J. Druzgala
  • Publication number: 20130225824
    Abstract: A process is provided for efficiently producing an optically active 3-quinuclidinol derivative of high optical purity using a readily available ruthenium compound as an asymmetric reduction catalyst. This process is a process for producing an optically active 3-quinuclidinol derivative represented by the following formula (III) comprising asymmetrically hydrogenating a 3-quinuclidinone derivative represented by the following formula (I) in the presence of a ruthenium compound (II) represented by formula (II): Ru(X)(Y)(Px)n[R1R2C*(NR3R4)-A-R5R6C*(NR7R8)] (in the formulas, R represents a hydrogen atom or C7 to C18 aralkyl group and the like, X and Y represent hydrogen atoms or halogen atoms and the like, Px represents a phosphine ligand, n represents 1 or 2, R1 to R8 represent hydrogen atoms or C1 to C20 alkyl groups and the like, * represents an optically active carbon atom and A represents an ethylene group and the like).
    Type: Application
    Filed: April 8, 2013
    Publication date: August 29, 2013
    Applicant: NIPPON SODA CO., LTD.
    Inventors: Takeshi OHKUMA, Noriyoshi ARAI, Masaya AKASHI, Hirohito OOOKA, Tsutomu INOUE
  • Publication number: 20130203804
    Abstract: The invention concerns fumarate salts of solifenacin, as well as pharmaceutical compositions comprising fumarate salts of solifenacin. The invention furthermore concerns a process for preparing solifenacin and salts thereof. The fumarate salt provides improved properties over the known solifenacin salts, especially in terms of its stability. The novel process for its preparation is furthermore improved over known processes for preparing solifenacin in that it provides a higher yield and recovers a greater amount of starting material.
    Type: Application
    Filed: July 5, 2011
    Publication date: August 8, 2013
    Applicant: CRYSTAL PHARMA, S.A.U.
    Inventors: Gerardo Gutiérrez Fuentes, Antonio Lorente Bonde-Larsen, Jaime del Campo López-Bachiller, Celso Sandoval Rodríguez, Yolanda Fernández Sainz
  • Publication number: 20130196978
    Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.
    Type: Application
    Filed: March 14, 2013
    Publication date: August 1, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Patent number: 8492402
    Abstract: The present invention refers to a stable crystalline salt of (R)-3-fluorophenyl-3,4,5-trifluorobenzylcarbamic acid 1-azabicyclo[2.2.2]oct-3-yl ester and its use as medicament, in particular for the treatment of urinary incontinence or other diseases involving genitourinary disorders.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: July 23, 2013
    Assignee: Laboratorios Salvat, S.A.
    Inventors: Juan Lorenzo Catena Ruiz, José Hidalgo Rodriguez, María del Carmen Serra Comas, Isabel Masip Masip
  • Publication number: 20130172302
    Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.
    Type: Application
    Filed: December 28, 2012
    Publication date: July 4, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Patent number: 8455646
    Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: June 4, 2013
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Antonio Caligiuri, Mauro Riccaboni, Gabriele Amari
  • Publication number: 20130123502
    Abstract: The present invention relates to a process for the preparation of Solifenacin succinate by condensing a compound of formula (IVb) with (RS)-3-quinuclidinol, wherein, R represents methyl, ethyl, isopropyl; to produce a diastereomeric mixture of (1S)-3,4-dihydro-1-phenyl-2(1H)-isoquinolinecarboxylic acid (3RS)-1-azabicyclo[2.2.2]oct-3-yl ester, which is treated with succinic acid in a solvent or mixture of solvents to produce optically pure Solifenacin succinate, Formula (X).
    Type: Application
    Filed: June 20, 2011
    Publication date: May 16, 2013
    Inventors: Anand Gopalkrishna Kamat, Joseph Prabahar Koilpillai, Naga Trinadhachari Ganala, Venkata Lakshmi Upputuri, Venkata Balalji Boddu, Sivakumaran Meenakshisunderam
  • Publication number: 20130115163
    Abstract: A method of synthesizing a crystalline molecular sieve having an MSE framework type comprises crystallizing a reaction mixture comprising a source of water, a source of an oxide of a tetravalent element, Y, selected from at least one of silicon, tin, titanium, vanadium, and germanium, optionally a source of a trivalent element, X, a source of an alkali or alkaline earth metal, M, and a source of organic dications, Q, such as 3-hydroxy-1-(4-(1-methylpiperidin-1-ium-1 yl)butyl)quinuclidin-1-ium, 3-hydroxy-1-(5-(1-methylpiperidin-1-ium-1-yl)pentyl)quinuclidin-1-ium, 1,1?-(butane-1,4-diyl)bis(1-methylpiperidin-1-ium), 1,1?-(pentane-1,5-diyl)bis(1-methylpiperidin-1-ium), 1,1?-(hexane-1,6-diyl)bis(1-methylpiperidin-1-ium), and 1,1?-((3as,6as)-octahydropentalene-2,5-diyl)bis(1-methylpiperidin-1-ium).
    Type: Application
    Filed: October 11, 2012
    Publication date: May 9, 2013
    Applicant: EXXONMOBIL RESEARCH AND ENGINEERING COMPANY
    Inventors: SIMON C. WESTON, KARL G. STROHMAIER, HILDA B. VROMAN
  • Patent number: 8436181
    Abstract: A process is provided for efficiently producing an optically active 3-quinuclidinol derivative of high optical purity using a readily available ruthenium compound as an asymmetric reduction catalyst. This process is a process for producing an optically active 3-quinuclidinol derivative represented by the following formula (III) comprising asymmetrically hydrogenating a 3-quinuclidinone derivative represented by the following formula (I) in the presence of a ruthenium compound (II) represented by formula (II): Ru(X)(Y)(Px)n[R1R2C*(NR3R4)-A-R5R6C*(NR7R8)] (in the formulas, R represents a hydrogen atom or C7 to C18 aralkyl group and the like, X and Y represent hydrogen atoms or halogen atoms and the like, Px represents a phosphine ligand, n represents 1 or 2, R1 to R8 represent hydrogen atoms or C1 to C20 alkyl groups and the like, * represents an optically active carbon atom and A represents an ethylene group and the like).
    Type: Grant
    Filed: September 2, 2008
    Date of Patent: May 7, 2013
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Takeshi Ohkuma, Noriyoshi Arai, Masaya Akashi, Hirohito Oooka, Tsutomu Inoue