The Chalcogen Is In An -oh Or -om Group (m Is Group Ia Or Group Iia Light Metal) Patents (Class 546/240)
  • Publication number: 20150057443
    Abstract: Cycloalkyl amine compounds of Formula (I), wherein ring A is C3-C6 cycloalkyl, optionally substituted with one or more C1-C3 alkyl, and R5 is ORS2, in which RS2 is H or C1-C6 alkyl, or R5 and R6, together with the carbon atom to which they are attached, form C?O, for use in treating CNS disorders, including movement disorders, depressive disorders, sleep disorders, cognitive dysfunctions, obesity, sexual dysfunction and substance abuse.
    Type: Application
    Filed: August 21, 2014
    Publication date: February 26, 2015
    Inventors: Philip Huxley, Jonathan R. Heal, Richard S. Todd
  • Publication number: 20140378473
    Abstract: This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: COGNITION THERAPEUTICS, INC.
    Inventors: Susan M. Catalano, Gilbert Rishton, Nicholas J. Izzo
  • Publication number: 20140200244
    Abstract: Described herein are enhanced N-methyl-D-aspartate (NMDA) receptor antagonists, pharmaceutical compositions thereof, and their methods of use and treatment, e.g., of Formula (I): wherein one or more of R1, R2, R3, R4, R5, or the ring formed by the joining of R1 and R2, is a hydrophobic moiety which confers enhanced antagonist activity as compared to existing NMDA receptor antagonists, e.g., ifenprodil. Compounds described herein are designed based on the discovery that ifenprodil binds within the allosteric domain of the GluN1/GluN2B NMDA receptor, particularly at the interface between GluN1 and GluN2B subunits. In silico methods are further described herein.
    Type: Application
    Filed: January 2, 2014
    Publication date: July 17, 2014
    Applicant: Cold Spring Harbor Laboratory
    Inventors: Hiro Furukawa, Erkan Karakas
  • Publication number: 20140135360
    Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 15, 2014
    Applicant: Jacobus Pharmaceutical Company, Inc
    Inventors: Gavin David Heffernan, David Penman Jacobus, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
  • Patent number: 8648198
    Abstract: Described herein are enhanced N-methyl-D-aspartate (NMDA) receptor antagonists, pharmaceutical compositions thereof, and their methods of use and treatment, e.g., of Formula (I): wherein one or more of R1, R2, R3, R4, R5, or the ring formed by the joining of R1 and R2, is a hydrophobic moiety which confers enhanced antagonist activity as compared to existing NMDA receptor antagonists, e.g., ifenprodil. Compounds described herein are designed based on the discovery that ifenprodil binds within the allosteric domain of the GluN1/GluN2B NMDA receptor, particularly at the interface between GluN1 and GluN2B subunits. In silico methods are further described herein.
    Type: Grant
    Filed: January 19, 2012
    Date of Patent: February 11, 2014
    Assignee: Cold Spring Harbor Laboratory
    Inventors: Hiro Furukawa, Erkan Karakas
  • Patent number: 8598358
    Abstract: An object of the present invention is to provide a method for producing an oxazole compound in a high yield.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: December 3, 2013
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Akihiro Yamamoto, Koichi Shinhama, Nobuhisa Fujita, Shinji Aki, Shin Ogasawara, Naoto Utsumi
  • Publication number: 20130211080
    Abstract: The present invention is directed to a process for the manufacture of 2,3,5-trimethyl-hydro-p-benzoquinone comprising the following steps: a) hydrogenating 2,6-dimethyl-p-benzoquinone with hydrogen in the presence of a hydrogenation catalyst in an organic solvent to obtain 2,6-dimethyl-hydro-p-benzoquinone; b) reacting 2,6-dimethyl-hydro-p-benzoquinone with a secondary amine and formal-dehyde in an organic solvent to obtain 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone; c) reacting 2,6-dimethyl-3-(N,N-disubstituted aminomethyl)-hydro-p-benzoquinone with hydrogen in the presence of a hydrogenolysis catalyst in an organic solvent to obtain 2,3,5-trimethylhydro-p-benzoquinone; wherein the organic solvent in all steps a), b) and c) is independently selected from the group consisting of methyl tert.-butyl ether, ethyl tert.-butyl ether, tert.-amyl ether, methoxycyclopentane and any mixtures thereof. Preferably the organic solvent used in all steps a), b) and c) is the same.
    Type: Application
    Filed: August 25, 2011
    Publication date: August 15, 2013
    Applicant: DSM IP ASSETS B.V.
    Inventors: Werner Bonrath, Thomas Netscher, Jan Schütz, Bettina Wüstenberg
  • Patent number: 8501778
    Abstract: The present invention relates to aralkyl piperidine derivatives, compositions containing the same, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are a free base of the compound represented by the following formula or a salt thereof. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: August 6, 2013
    Assignees: NHWA Pharma. Corporation, Shanhai Institute of Pharmaceutical Industry
    Inventors: Jianqi Li, Guan Wang, Guisen Zhang, Yanqin Ma, Wenhua Ji, Yuan Zhang, Lin Guo
  • Patent number: 8476445
    Abstract: The present invention relates to a process for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents, The process comprises providing a regiosomer of the following formula: wherein Z is —CG1G2G3, m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group co
    Type: Grant
    Filed: January 13, 2010
    Date of Patent: July 2, 2013
    Assignee: Albany Molecular Research, Inc.
    Inventors: Thomas E. D'Ambra, Garry M. Pilling
  • Publication number: 20130045165
    Abstract: 4-Fluoro-4-phenylpiperidin-1-yl ? antagonists of general structure as well as pharmaceutical compositions comprising compounds of formula I, are disclosed. These compounds and compositions are useful as treatments of conditions or diseases associated with binding opioid receptors including pain, obesity, hyperalgesia, inflammation, osteoarthritis, drug addiction, and cancer. These compounds and compositions are also useful as treatments for tardive dyskinesia.
    Type: Application
    Filed: April 29, 2011
    Publication date: February 21, 2013
    Applicant: KINENTIA BIOSCIENCES, LLC
    Inventor: David J. Fairfax
  • Publication number: 20120323012
    Abstract: 4-(azacycloalkyl)-benzene-1,3-diol compounds with the following general formula (I): Also described, are compositions that include these compounds and processes for their preparation and use in pharmaceutical or cosmetic compositions for treating pigmentary disorders.
    Type: Application
    Filed: December 8, 2010
    Publication date: December 20, 2012
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Jean-Guy Boiteau, Anne-Pascale Luzy
  • Publication number: 20120302757
    Abstract: An object of the present invention is to provide a method for producing an oxazole compound in a high yield.
    Type: Application
    Filed: January 28, 2011
    Publication date: November 29, 2012
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Yamamoto, Koichi Shinhama, Nobuhisa Fujita, Shinji Aki, Shin Ogasawara, Naoto Utsumi
  • Publication number: 20120294804
    Abstract: Described herein are enhanced N-methyl-D-aspartate (NMDA) receptor antagonists, pharmaceutical compositions thereof, and their methods of use and treatment, e.g., of Formula (I): wherein one or more of R1, R2, R3, R4, R5, or the ring formed by the joining of R1 and R2, is a hydrophobic moiety which confers enhanced antagonist activity as compared to existing NMDA receptor antagonists, e.g., ifenprodil. Compounds described herein are designed based on the discovery that ifenprodil binds within the allosteric domain of the GluN1/GluN2B NMDA receptor, particularly at the interface between GluN1 and GluN2B subunits. In silico methods are further described herein.
    Type: Application
    Filed: January 19, 2012
    Publication date: November 22, 2012
    Applicant: Cold Spring Harbor Laboratory
    Inventors: Hiro Furukawa, Erkan Karakas
  • Publication number: 20120259122
    Abstract: Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.
    Type: Application
    Filed: June 20, 2012
    Publication date: October 11, 2012
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Tomohiro TOYODA, Hidefumi YOSHINAGA
  • Patent number: 8258305
    Abstract: The invention provides a class of dopamine transporter inhibitors of formula (I) (DAT inhibitors), packaged pharmaceuticals comprising such inhibitors, and their uses in treating, or manufacturing medicaments for treating disease conditions including Parkinson's disease, when assessed by one or more of Hoehn and Yahr Staging of Parkinson's Disease, Unified Parkinson Disease Rating Scale (UPDRS), and Schwab and England Activities of Daily Living Scale. Related business methods such as marketing the inhibitors to healthcare providers are also provided.
    Type: Grant
    Filed: February 21, 2006
    Date of Patent: September 4, 2012
    Assignee: Prexa Pharmaceuticals, Inc.
    Inventor: James R. Hauske
  • Patent number: 8247434
    Abstract: Anhydrous crystalline fexofenadine hydrochloride Form C, crystalline fexofenadine acetate monohydrate Form D, crystalline fexofenadine acetate dihydrate Form E and crystalline fexofenadine free base monohydrate Form F, processes of preparing the same, pharmaceutical compositions thereof, therapeutic uses thereof and methods of treatment therewith.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: August 21, 2012
    Assignee: Cipla Limited
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Manish Gopaldas Gangrade, Dilip Ramdas Birari
  • Patent number: 8236961
    Abstract: A process for the preparation of 4-[1-oxo-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-?,?-dimethylbenzeneacetic acid, useful as an intermediate for the preparation of fexofenadine, is provided.
    Type: Grant
    Filed: May 15, 2008
    Date of Patent: August 7, 2012
    Assignee: Dipharma Francis s.r.l.
    Inventors: Tiziano Scubla, Pietro Allegrini, Eliana Rocchini, Caterina Napoletano
  • Patent number: 8173678
    Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.
    Type: Grant
    Filed: October 25, 2010
    Date of Patent: May 8, 2012
    Assignee: Research Triangle Institute
    Inventors: Frank Ivy Carroll, Hernan A. Navarro, Lawrence E. Brieaddy, Scott P. Runyon, James B. Thomas
  • Patent number: 8153657
    Abstract: One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aforementioned compounds in a method of treating a disorder of the central nervous system in a mammal.
    Type: Grant
    Filed: October 22, 2004
    Date of Patent: April 10, 2012
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Jia Zhou
  • Publication number: 20110124685
    Abstract: The invention provides novel phenolic ester local anesthetic compounds. The invention also provides pharmaceutical compositions that include such compounds as well as methods for making such compounds and compositions and methods for using such compounds and compositions to induce and/or maintain anesthesia and/or analgesia.
    Type: Application
    Filed: January 13, 2009
    Publication date: May 26, 2011
    Inventor: Thomas E. Jenkins
  • Publication number: 20110065743
    Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.
    Type: Application
    Filed: October 25, 2010
    Publication date: March 17, 2011
    Applicant: Research Triangle Institute
    Inventors: Frank Ivy CARROLL, Hernan A. Navarro, Lawrence E. Brieaddy, Scott P. Runyon, James B. Thomas
  • Publication number: 20110046179
    Abstract: This invention relates to novel piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: August 29, 2007
    Publication date: February 24, 2011
    Inventors: Birgitte L. Eriksen, Dan Peters, Bjarne H. Dahl, Elsebet Østergaard Nielsen, John Paul Redrobe
  • Publication number: 20100279997
    Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.
    Type: Application
    Filed: October 28, 2009
    Publication date: November 4, 2010
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Patent number: 7816375
    Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
    Type: Grant
    Filed: March 12, 2009
    Date of Patent: October 19, 2010
    Assignee: Sepracor Inc.
    Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike Radeke, Fengjiang Wang, Liming Shao
  • Patent number: 7700779
    Abstract: The present invention is related to novel polymorph of Fexofenadine and Fexofenadine hydrochloride of formula 1 and process of preparation thereof. The present invention is also directed to provide pure novel polymorphs of Fexofenadine and its hydrochloride by a simple process which is cost effective, commercially viable and environment friendly.
    Type: Grant
    Filed: July 31, 2001
    Date of Patent: April 20, 2010
    Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.
    Inventors: M. Satyanarayana Reddy, S. Thirumalai Rajan, U. V. Bhaskara Rao
  • Patent number: 7691615
    Abstract: The present invention relates to the production of a product compound having a structure according to Formulae IA and/or IB: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, and alkoxy. This process involves incubating a starting compound having a structure according to Formulae IIA and/or IIB: wherein R3 is —CH3 and R1, R2, A, B, and D are defined above in the presence of a microorganism under conditions effective to produce the product compound.
    Type: Grant
    Filed: January 17, 2007
    Date of Patent: April 6, 2010
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter C. Michels, Eric L. Zirbes
  • Patent number: 7678915
    Abstract: The present invention relates to a process for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents, The process comprises providing a regiosomer of the following formula: m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety,
    Type: Grant
    Filed: September 15, 2006
    Date of Patent: March 16, 2010
    Assignee: Albany Molecular Research, Inc.
    Inventors: Thomas D'Ambra, Garry Pilling
  • Patent number: 7671071
    Abstract: Provided is a crystalline (polymorphic) form of fexofenadine hydrochloride, denominated fexofenadine hydrochloride Form XVI.
    Type: Grant
    Filed: October 3, 2005
    Date of Patent: March 2, 2010
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Barnaba Krochmal, Dov Diller, Ben-Zion Dolitzky, Judith Aronhime, Shlomit Wizel, Boaz Gome, Igor Lifshitz
  • Publication number: 20090163461
    Abstract: The present invention provides a novel compound represented by the formula (I): wherein R1 and R2 are as defined in the specification, or a salt thereof, which is useful as a reagent (radiotracer) for VAChT mapping and the like, and can be used for positron emission tomography (PET), and a production method of the compound. Moreover, the present invention provides a diagnostic reagent for diagnosing cholinergic neurodegenerative disorders (e.g., Alzheimer's disease, memory disorder, learning disorder, schizophrenia, cognitive dysfunction, hyperactivity disorder, anxiety neurosis, depression, analgia, Parkinson's disease and the like) and the like, which contains the aforementioned compound.
    Type: Application
    Filed: March 31, 2006
    Publication date: June 25, 2009
    Inventors: Kazuhiro Shiba, Kiichi Ishiwata, Hideo Tsukada, Shingo Nishiyama
  • Patent number: 7517892
    Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
    Type: Grant
    Filed: September 12, 2001
    Date of Patent: April 14, 2009
    Assignee: Sepracor Inc.
    Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike Radeke, Fengjiang Wang, Liming Shao
  • Publication number: 20080255089
    Abstract: Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.
    Type: Application
    Filed: November 22, 2006
    Publication date: October 16, 2008
    Inventor: Subba Reddy Katamreddy
  • Publication number: 20080227983
    Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings, each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.
    Type: Application
    Filed: May 29, 2008
    Publication date: September 18, 2008
    Applicant: AMR TECHNOLOGY, INC.
    Inventor: Thomas E. D'Ambra
  • Patent number: 7390904
    Abstract: Sterically hindered N-hydrocarbyloxyamines are prepared from hindered amine N-oxyl compounds by a process which uses hydrogen peroxide or a hydrogen peroxide equivalent, a catalytic amount of a peroxide decomposing transition metal salt, metal oxide, or metal-ligand complex, a hydrocarbon solvent containing no activated hydrogen atoms, and a relatively inert cosolvent. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.
    Type: Grant
    Filed: July 12, 2004
    Date of Patent: June 24, 2008
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: James P. Galbo, Robert E. Detlefsen
  • Patent number: 7390906
    Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.
    Type: Grant
    Filed: June 19, 2006
    Date of Patent: June 24, 2008
    Assignee: AMR Technology, Inc.
    Inventor: Thomas E. D'Ambra
  • Patent number: 7294637
    Abstract: One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substituted piperidine. In a preferred embodiment, the method of the present invention treats cocaine addiction or methamphetamine addiction.
    Type: Grant
    Filed: February 4, 2004
    Date of Patent: November 13, 2007
    Assignee: Sepracor, Inc.
    Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike S. Radeke, Fengjiang Wang, Liming Shao
  • Patent number: 7238834
    Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: July 3, 2007
    Assignee: AMR Technology, Inc.
    Inventor: Thomas E. D'Ambra
  • Patent number: 7232908
    Abstract: The present invention relates to a process for the production of piperidine derivatives with microorganisms. This is carried out by incubating starting compounds in the presence of a microorganism under conditions effective to produce piperidine derivative products. Suitable microorganisms can be from any one of the genus of Stemphylium, Gliocladium, Bacillus, Botrytis, Cyathus, Rhizopus, Pycniodosphora, Pseudomonas, Helicostylum, Mucor, Gelasinospora, Rhodotorula, Candida, Mycobacterium, and Penicillium. In another aspect of the invention, starting compounds are incubated in the presence of Cunninghamella bainieria under conditions effective to produce piperidine derivative products.
    Type: Grant
    Filed: August 11, 2003
    Date of Patent: June 19, 2007
    Assignee: AMR Technology, Inc.
    Inventors: Peter C. Michels, Eric L. Zirbes
  • Patent number: 7176318
    Abstract: An improved process for the manufacture of fexofenadine is described in which a compound of formula (F): wherein R2 represents COOH, COO—C1-6 alkyl or CN; and R3 represents hydrogen, mesylate, triflate, tosylate or carboxy-C1-6-alkyl, or a salt thereof is prepared by: (I) reacting a compound of formula (B): wherein R1 represents hydrogen or carboxy-C1-6-alkyl; and R2 is a hereinbefore defined, with a copper and/or silver compound in the presence of palladium or a compound thereof to yield a compound of formula (C): wherein R1, and R2 are as hereinbefore defined; (II) converting said compound of formula (C) into a compound of formula (E): wherein R2 and R3 are as hereinbefore defined and R4 represents a halogen atom, and (III) reacting said compound of formula (E) with azacyclonol.
    Type: Grant
    Filed: July 19, 2001
    Date of Patent: February 13, 2007
    Assignee: Texcontor Establissement
    Inventors: Federico Junquera Milla, William Paul Jackson
  • Patent number: 7164025
    Abstract: The present invention pertains to a process for obtaining a single enantiomer, d or l, of threo-methylphenidate, comprising resolution of a mixture of the enantiomers; racemisation of the unwanted enantiomer, to give a mixture of all four stereoisomers; and separation of the erythro stereoisomers, to leave the same mixture of enantiomers for resolution.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: January 16, 2007
    Assignee: Celltech Pharma Europe Limited
    Inventors: Marianne Langston, Hooshang Shahriari Zavareh
  • Patent number: 6992090
    Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
    Type: Grant
    Filed: June 16, 2003
    Date of Patent: January 31, 2006
    Assignee: Adolor Corporation
    Inventors: Bertrand Le Bourdonnec, Roland E. Dolle
  • Patent number: 6974872
    Abstract: The present invention discloses processes for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: December 13, 2005
    Assignee: AMR Technology, Inc.
    Inventors: Thomas E. D'Ambra, Garry M. Pilling
  • Patent number: 6949650
    Abstract: A process for the racemization of enantiomerically enriched 1-benzyl-4-(4-fluorophenyl)-3-hydroxymethyl-1,2,3,6-tetrahydropyridine which is a useful intermediate in the preparation of paroxetine. Formula (A) means that the compound (I) has an enantiomeric excess of one enantiomer over the other enantiomer. R1 and R2 are defined as in claim 1.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: September 27, 2005
    Assignee: Aesica Pharmaceuticals Ltd.
    Inventors: Jayne Froggett, Dean Riley, Andrew Turner
  • Patent number: 6930197
    Abstract: This invention relates to a process for the preparation of compounds of the formula: wherein R1 is C1-C6alkyl and the C1-C6alkyl moiety is straight or branched.
    Type: Grant
    Filed: March 22, 2002
    Date of Patent: August 16, 2005
    Assignee: Aventis Pharmaceuticals Inc.
    Inventor: Timothy A. Ayers
  • Patent number: 6930186
    Abstract: The present invention is directed to methods for preparing intermediates useful in the synthesis of paroxetine wherein the intermediates are substantially free of alkoxy impurities as well as to methods for preparing paroxetine and pharmaceutically acceptable salts thereof substantially free of alkoxy impurities. The alkoxy impurity is reacted with an ether cleaving agent to generate the corresponding phenol, which is separated, yielding the desired product substantially free of alkoxy impurities. Paroxetine intermediates such as PMA, paroxetine, and pharmaceutically acceptable salts thereof substantially free of alkoxy impurities also form part of the present invention.
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: August 16, 2005
    Assignee: Teva Pharmacetical Industries Ltd.
    Inventors: Valerie Niddam, Ilya Avrutov
  • Patent number: 6919458
    Abstract: The present invention relates to a process for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents, The process comprises providing a regiosomer of the following formula: wherein Z is —CG1G2G3, m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydr
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: July 19, 2005
    Assignee: AMR Technology, Inc.
    Inventors: Thomas E. D'Ambra, Garry M. Pilling
  • Patent number: 6894191
    Abstract: The present invention provides a process for the preparation of arylamines comprises reacting aryl halide and aryl amine/heterocyclic amine. The said process is carried out in the presence of a solvent, catalyst and a base.
    Type: Grant
    Filed: December 10, 2003
    Date of Patent: May 17, 2005
    Assignee: Council of Scientific and Industrial Research
    Inventors: Ashutosh Anant Kelkar, Nandkumar Manikrao Patil, Raghunath Vitthal Chaudhari
  • Patent number: 6890920
    Abstract: Novel quaternary ammonium compounds of the formula and any stereoisomers thereof, wherein R1, R2 and R3 independently represent C1-C6 alkyl, optionally substituted with phenyl or hydroxyl, or both, and wherein any two of R1, R2 and R3 may form a ring together with the quaternary ammonium nitrogen; R4 represents —H, —CH3, or —CO—R4-1, wherein R4-1 represents —(C1-C4 alkyl), —(C1-C4 alkoxy), or —NR4-2R4-3, wherein R4-2 and R4-3 independently represent —H or —(C1-C4 alkyl); R5, R6 and R7 independently represent —H, —OCH3, —OH, —CONH2, —SO2NH2, —F, —Cl, —Br, —I, —CF3, or —(C1-C4 alkyl), optionally substituted with one or two —OH, —(C1-C4 alkoxy), —COOH, or —CO—O—(C1-C3 alkyl); and X? represents an anion of a pharmaceutically acceptable acid, the compounds for use as medicaments, use of the compounds for the manufacture of specific medicaments, and pharmaceutical compositions comprising the compounds. The present invention also concerns a method of treatment involving administration of the compounds.
    Type: Grant
    Filed: October 25, 2002
    Date of Patent: May 10, 2005
    Assignee: Pharmacia & Upjohn Company
    Inventors: Ivan Richards, Sue K. Cammarata, Craig D. Wegner, Michael Hawley, Mark Peter Warchol, Mark Kontny, Walter Morozowich, Karen Patrice Kolbasa, Malcolm Wilson Moon, Dominique Bonafoux, Sergey Gregory Wolfson, Patrick James Lennon
  • Patent number: 6875775
    Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula: wherein R1 and R2, which are the same or different are a) H, halogen, OCH3, OH; or where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, —CH2C?CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or c) —Y—(CH2)nCH2—O—R6 where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and ?R3 is H, halogen, OH or —OCH3; stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.
    Type: Grant
    Filed: April 8, 2003
    Date of Patent: April 5, 2005
    Assignee: Hormos Medical Oy LTD
    Inventors: Marja-Liisa Södervall, Arja Kalapudas, Lauri Kangas, Risto Lammintausta, Pirkko Härkönen, Kalervo Väänänen, Arto Karjalainen
  • Patent number: 6864254
    Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: March 8, 2005
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
  • Patent number: RE39667
    Abstract: The invention relates to 3,3-diphenylpropylamines of formula (I), wherein R1 signifies hydrogen or methyl, R2 and R3 independently signify hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of formula (II), wherein R4 and R5 signify non-aromatic hydrocarbyl groups, which may be the same or different and which together contain at least three carbon atoms, and wherein R4 and R5 may form a ring together with the amine nitrogen, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers.
    Type: Grant
    Filed: November 5, 1993
    Date of Patent: May 29, 2007
    Assignee: Pfizer Health AB
    Inventors: Rolf A. Johansson, Pinchas Moses, Lisbeth Nilvebrant, Bengt A. Sparf