Ring In A Substituent E Patents (Class 564/217)
- A ring or polycyclo ring system in a substituent E is attached indirectly to the carboxamide nitrogen or to an amino nitrogen in substituent E by acyclic nonionic bonding (Class 564/219)
- Plural rings in a substituent E (Class 564/221)
- Hydroxy, bonded directly to carbon, or ether in a substituent E (H of -OH may be replaced by a substituted or unsubstituted ammonium ion or a Group IA or IIA light metal) (Class 564/223)
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Publication number: 20150105587Abstract: An amorphous amide compound of the formula wherein R is selected from the group consisting of an alkyl group, an aryl group, an alkylaryl group, an arylalkyl group, and combinations thereof. An amorphous diamide compound of the formula wherein R1 is selected from the group consisting of an alkylene group, an arylene group, an alkylarylene group, an arylalkylene group, and combinations thereof.Type: ApplicationFiled: October 14, 2013Publication date: April 16, 2015Applicant: Xerox CorporationInventors: Naveen Chopra, Adela Goredema, Kentaro Morimitsu, Barkev Keoshkerian, Jennifer L. Belelie
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Publication number: 20140275245Abstract: Analgesic compounds for treatment of pain or fever, comprising a bicyclopentane moiety linked to an amine, combinations of the compounds with opioid analgesic drugs, and methods for treating pain or fever by administering the compounds.Type: ApplicationFiled: March 6, 2014Publication date: September 18, 2014Applicant: KALYRA PHARMACEUTICALS, INC.Inventor: Kevin Duane Bunker
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Patent number: 8796491Abstract: The present invention pertains to process for the amidation of a substituted 1-bromo-adamantane comprising a step (0) of reacting a substituted adamantane with an excess of bromine to obtain a 1-bromo-adamantane and a step (i) of reacting said substituted 1-bromo-adamantane with an amide, wherein the substituted 1-bromo-adamantane is used in the form of a mixture comprising bromine as obtained in step (0), wherein in step (0) a bromine: substituted adamantane molar ratio of from [2.5:1] to less than [5:1] is employed.Type: GrantFiled: August 7, 2009Date of Patent: August 5, 2014Assignee: Merz Pharma GmbH & Co. KGaAInventors: Markus-Rene Gold, Herbert Koller, Michael Pyerin
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Patent number: 8796468Abstract: Disclosed is an adamantanamine derivative which is useful as a significant intermediate of an 11?HSD-1 inhibitor. Disclosed is a compound represented by the formula (II): wherein R10 is a group represented by the formula: —(CR13R14)m-NR12—R11 or the like.Type: GrantFiled: December 20, 2010Date of Patent: August 5, 2014Assignee: Shionogi & Co., Ltd.Inventors: Tomoyuki Ogawa, Koji Masuda
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Patent number: 8664441Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like. Processes for making the compound of formula (I), as well as related intermediates, are disclosed.Type: GrantFiled: July 3, 2013Date of Patent: March 4, 2014Assignee: Sunovion Pharmaceuticals Inc.Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
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Patent number: 8501994Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like.Type: GrantFiled: August 22, 2008Date of Patent: August 6, 2013Assignee: Sunovion Pharmaceuticals Inc.Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
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Patent number: 8436209Abstract: The present invention relates to a process for manufacturing N-Formyl-1-amino-3,5-dimethyladamantane, an intermediate product in the overall process of producing 1-Amino-3,5-dimethyladamantane hydrochloride (Memantine). Therein, the process comprises the following steps: (a) reacting 1,3-dimethyladamantane with an acid mixture comprising concentrated sulfuric acid and concentrated nitric acid, wherein 1 to 6 volume parts of sulfuric acid (measured in ml) are used per weight part of 1,3-dimethyladamantane (measured in g); (b) reacting the solution from step (a) with an amount of formamide varying from 1 to 5 molar equivalents per mole of deprotonated 1,3-dimethyladamantane from step (a) to obtain N-Formyl-1-amino-3,5-dimethyladamantane. In step (b), the molar ratio of total acid, i.e. the molar amount of sulfuric acid and the molar amount of nitric acid taken together versus the molar amount of formamide is at least 1.5 and that the temperature is at least 50° C.Type: GrantFiled: March 19, 2009Date of Patent: May 7, 2013Assignee: Merz Pharma GmbH & Co. KGaAInventors: Florian Anton Martin Huber, Giorgio Gallo, Carla De Faveri
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Patent number: 8436210Abstract: The present invention provides an amide compound having antibacterial activity, and a bacterial infection control agent for agricultural and horticultural use that contains the amide compound. The novel amide compound of the present invention is represented by General Formula (1): wherein R is a —CH(R1)(R2) or a —CO(R2) group, R1 is a hydrogen atom or a hydroxyl group, and R2 is a C1-12 alkyl group.Type: GrantFiled: November 6, 2008Date of Patent: May 7, 2013Assignees: The University of Tokyo, Otsuka Chemical Co., Ltd.Inventors: Hiroaki Suga, Jun Igarashi
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Patent number: 8314270Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: GrantFiled: September 9, 2010Date of Patent: November 20, 2012Assignee: Abbott LaboratoriesInventors: James T. Link, Qi Shuai, Martin Winn, Hong Yong
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Publication number: 20120270901Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5, and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: December 8, 2011Publication date: October 25, 2012Applicant: Aquinox Pharmaceuticals Inc.Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
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Publication number: 20120259128Abstract: Disclosed is an adamantanamine derivative which is useful as a significant intermediate of an 11?HSD-1 inhibitor. Disclosed is a compound represented by the formula (II): wherein R10 is a group represented by the formula: —(CR13R14)m-NR12—R11 or the like.Type: ApplicationFiled: December 20, 2010Publication date: October 11, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Tomoyuki Ogawa, Koji Masuda
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Patent number: 8138375Abstract: The invention relates to a method for producing 1-formamido-3,5-dimethyladamantane in only two reaction steps by direct formamide formation of 1,3-dimethyladamantane, the 1,3-dimethyladamantane being reacted with formamide in concentrated acids.Type: GrantFiled: February 20, 2007Date of Patent: March 20, 2012Assignee: MERZ PHARMA GmbH & Co. KGaAInventors: Peter R. Schreiner, Andrey A. Fokin, Lukas Wanka, Derek M. Wolfe
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Publication number: 20120040930Abstract: The invention concerns a triterpene alkaloid of general formula (I). The invention also concerns a method for making same and use thereof as medicine.Type: ApplicationFiled: January 13, 2006Publication date: February 16, 2012Inventors: Catherine Guillou, Jean-Yves Lallemand, Thibault Sauvaítre, Jordi Molgo, Denyse Herlem, Daniel Guenard, Françoise Khuong-Huu
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Publication number: 20110263900Abstract: The present invention pertains to process for the amidation of a substituted 1-bromo-adamantane comprising a step (0) of reacting a substituted adamantane with an excess of bromine to obtain a 1-bromo-adamantane and a step (i) of reacting said substituted 1-bromo-adamantane with an amide, wherein the substituted 1-bromo-adamantane is used in the form of a mixture comprising bromine as obtained in step (0), wherein in step (0) a bromine:substituted adamantane molar ratio of from [2.5:1] to less than [5:1] is employed.Type: ApplicationFiled: August 7, 2009Publication date: October 27, 2011Applicant: MERZ PHARMA GmbH & CO. KGaAInventors: Markus-Rene Gold, Herbert Koller, Michael Pyerin
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Publication number: 20110218214Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: ApplicationFiled: September 9, 2010Publication date: September 8, 2011Applicant: ABBOTT LABORATORIESInventors: James T. Link, Qi Shuai, Martin Winn, Hong Yong
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Publication number: 20110200549Abstract: Disclosed are compounds having the ability to modulate, namely to improve, enhance and/or modify fragrance compositions due to their ability to inhibit cytochrome P450 enzymes, e.g. CYP2A, e.g. 2A13 and 2A6, and CYP2B6.Type: ApplicationFiled: September 29, 2009Publication date: August 18, 2011Inventors: Thierry Granier, Boris Schilling
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Publication number: 20110082317Abstract: The present invention relates to a process for manufacturing N-Formyl-1-amino-3,5-dimethyladamantane, an intermediate product in the overall process of producing 1-Amino-3,5-dimethyladamantane hydrochloride (Memantine). Therein, the process comprises the following steps: (a) reacting 1,3-dimethyladamantane with an acid mixture comprising concentrated sulfuric acid and concentrated nitric acid, wherein 1 to 6 volume parts of sulfuric acid (measured in ml) are used per weight part of 1,3-dimethyladamantane (measured in g); (b) reacting the solution from step (a) with an amount of formamide varying from 1 to 5 molar equivalents per mole of deprotonated 1,3-dimethyladamantane from step (a) to obtain N-Formyl-1-amino-3,5-dimethyladamantane. In step (b), the molar ratio of total acid, i.e. the molar amount of sulfuric acid and the molar amount of nitric acid taken together versus the molar amount of formamide is at least 1.5 and that the temperature is at least 50° C.Type: ApplicationFiled: March 19, 2009Publication date: April 7, 2011Inventors: Florian Anton Martin Huber, Giorgio Gallo, Carla De Faveri
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Publication number: 20100261920Abstract: The present invention provides an amide compound having antibacterial activity, and a bacterial infection control agent for agricultural and horticultural use that contains the amide compound. The novel amide compound of the present invention is represented by General Formula (1): wherein R is a —CH(R1)(R2) or a —CO(R2) group, R1 is a hydrogen atom or a hydroxyl group, and R2 is a C1-12 alkyl group.Type: ApplicationFiled: November 6, 2008Publication date: October 14, 2010Applicants: THE UNIVERSITY OF TOKYO, OTSUKA CHEMICAL CO., LTD.Inventors: Hiroaki Suga, Jun Igarashi
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Publication number: 20100120031Abstract: The present invention concerns methods of synthesis of trans-tert-butyl-2-aminocylcopentylcarbamate comprising contacting 6-tosyl-6-azabicyclo[3.1.0]hexane with TMSN3 and TBAF to produce 2-azido-N-tosylcyclopentananiine; reducing the 2-azido-N-tosylcyclopentanamine to produce 2-amino-N-tosylcyclopentanamine; contacting the 2-amino-N-tosylcyclopentanamine with di-tert/-butyl dicarbonate to produce tert-butyl-2-(tosylamino)cyclopentylcarbamate; and detosylation of tert-butyl O(tosylamino) cyclopentylcarbamate to produce trans-tert-butyl-2-aminocyclopentylcarbamate. The invention also concerns PNAs comprising residues of the monomers of the invention in the backbone and uses of such PNAs. The PNAs of the invention can be used to detect DNAs of infectious agents or to suppress expression of protein associated with cancer.Type: ApplicationFiled: September 21, 2007Publication date: May 13, 2010Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPT. OFInventors: Daniel H. Appella, Qun Xu, Ning Zhang
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Publication number: 20100036153Abstract: The invention at hand provides at least dinitroxylated diamantanes. In addition, it provides methods for producing substituted diamantanes with high yields and selectivity. According to the invention, dinitroxylated diamantanes are suitable for being reacted with nucleophiles to form the corresponding disubstituted diamantanes. Surprisingly, it was discovered that at least dinitroxylated or hydroxylated diamantanes are rearranged in the presence of a strong acid, creating at least 4,9-nitroxylated or hydroxylated diamantanes. On the basis of this, 4,9-substituted diamantanes are able to be produced in a targeted manner by reaction with further nucleophiles.Type: ApplicationFiled: December 4, 2006Publication date: February 11, 2010Inventors: Peter R. Schreiner, Andrey A. Fokin
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Publication number: 20090299096Abstract: The invention relates to 1-formamido-adamantane derivatives of formula (I), which carry the substituents R1, R2 or R3 in 3, 5 and/or 7 position, the substituents being defined as follows: hydrogen, a linear or branched alkyl, alkenyl or alkinyl group with up to 6 C atoms, an aliphatic or aromatic, cyclic or heterocyclic hydrocarbon group with up to 10 carbon atoms, and formamides of hydrocarbons from the group of diamondoids, for example diamantane, triamantane, tetramantane and pentamantane, however, with the exception of 1-formamido-3,5-dimethyladamantane. The invention also relates to a method for the direct formation of formamide or acetamide of adamantane, adamantane derivatives with the aforementioned definition of substituents or of a hydrocarbon from the group of diamondoids, characterized by reacting the adamantane, the adamantane derivative or the diamondoid with formamide, acetamide or acetonitrile in concentrated acids, while avoiding SO3 containing sulfuric acid or 100% azotic acid.Type: ApplicationFiled: February 20, 2007Publication date: December 3, 2009Inventors: Peter R. Schreiner, Andrey A. Fokin, Lukas Wanka, Derek M. Wolfe
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Publication number: 20090299097Abstract: The invention relates to a method for producing 1-formamido-3,5-dimethyladamantane in only two reaction steps by direct formamide formation of 1,3-dimethyladamantane, the 1,3-dimethyladamantane being reacted with formamide in concentrated acids.Type: ApplicationFiled: February 20, 2007Publication date: December 3, 2009Applicant: MERZ PHARMA GMBH & CO. KGAAInventors: Peter R. Schreiner, Andrey A. Fokin, Lukas Wanka, Derek M. Wolfe
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Publication number: 20090176886Abstract: The present invention relates to polymorphic forms of (3R,4R,5S)-5-amino-4-acetylamino-3-(1-ethyl-propoxy)-cyclohex-1-ene-carboxylic acid ethyl ester phosphate, which is a potent inhibitor of viral neuraminidase.Type: ApplicationFiled: December 19, 2008Publication date: July 9, 2009Inventors: Andre Bubendorf, Pierre Goldbach, Olaf Grassmann, Michael Henning, Ines Sauer, Rene Trussardi
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Patent number: 7511175Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: GrantFiled: January 5, 2006Date of Patent: March 31, 2009Assignee: Abbott LaboratoriesInventors: Jyoti R. Patel, Qi Shuai, James T. Link, Jeffrey J. Rohde, Jurgen Dinges, Bryan K. Sorensen, Martin Winn, Hong Yong, Peer B. Jacobson, Michael E. Brune
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Publication number: 20080275112Abstract: The present invention describes 1-aminoadamantane derivatives and 3-aminoadamantane-1-carboxylic derivatives in which the 5- or 7-position of the basic adamantane structure can be optionally substituted, methods for the production of the compounds based on the present invention, and methods for the coupling of the monomeric 3-aminoadamantane-1-carboxylic derivatives thus obtained to oligomers. The compounds based on the present invention are suitable for the utilisation as antiviral active ingredients, artificial ion channels, as well as for the therapy, diagnostics and prophylaxis of diseases in which a dysfunction of the GABA system occurs.Type: ApplicationFiled: July 22, 2005Publication date: November 6, 2008Inventors: Peter R. Schreiner, Lukas Wanka
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Patent number: 7405324Abstract: The present invention concerns a new process for synthesising aminoadamantanes of formula I in which R1 and R2 are identical or different and are H or a straight or branched alkyl group comprising from 1 to 6 carbon atoms, and addition salts thereof with inorganic or organic acids, in particular memantine hydrochloride (1-amino-3,5-dimethyladamantane hydrochloride).Type: GrantFiled: May 10, 2006Date of Patent: July 29, 2008Assignee: A.M.S.A. Anonima Materie Sintetiche E. Afini S.p.A.Inventors: Enrico Vigano′, Ernesto Landonio, Simona Lanfranconi, Renato Molteni
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Patent number: 7166744Abstract: The present invention relates to a novel retinoid derivative compound represented by the formula I: wherein X, R1, R2 and R3 are as defined herein or pharmaceutically acceptalbe salts thereof. Also, the present invention relates to processes for producing the compound of the formula I and to an anti-cancer composition comprising the compound of the formula I. The compound of the formula I according to the present invention exerts high anti-cancer effects while not causing undesirable side effects.Type: GrantFiled: May 29, 2002Date of Patent: January 23, 2007Assignee: Chebigen Co., Ltd.Inventors: Hong-Sig Sin, Soo-Jong Um, Young-Soy Rho, Si-Ho Park, Youn-Ja Kwon, Myoung-Soon Park, Hye-Sook Han, So-Mi Kim, Dong-Myoung Kim, Deok-Kun Oh, Jong-Sup Park, Tae-Sung Bae
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Publication number: 20040235836Abstract: The present application describes modulators of MCP-1 of formula (I): 1Type: ApplicationFiled: April 29, 2004Publication date: November 25, 2004Inventor: Robert J. Cherney
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Patent number: 6790992Abstract: The present invention relates to novel scyphostatin analogues, which distinguish themselves by acting as SMase inhibitors so that they are of therapeutic use for a number of diseases such as a HIV infection, neurodegenerative diseases, inflammatory diseases, apoplexy, ischemia, myocardial infarction or in the case of atherosclerosis.Type: GrantFiled: August 22, 2002Date of Patent: September 14, 2004Assignee: Biofrontera Pharmaceuticals GmbHInventor: Hans-Peter Deigner
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Patent number: 6770784Abstract: Gamma-hydroxybutryic acid amides are used in the treatment of drug addiction and especially in the treatment of alcoholism.Type: GrantFiled: December 11, 2001Date of Patent: August 3, 2004Assignee: Laboratorio Farmaceutico C.T. S.r.l.Inventors: Roberto Cacciaglia, Antonella Loche, Vincenzo Perlini, Lorenza Guano
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Patent number: 6767925Abstract: A sprayable analgesic composition containing an analgesic which is absorbed into the bloodstream through the buccal mucosa and a pharmacologically acceptable liquid carrier.Type: GrantFiled: November 1, 1999Date of Patent: July 27, 2004Inventor: Joseph A. Deihl
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Patent number: 6756500Abstract: A process for preparing a cyclic compound comprising subjecting a starting material in the presence of a catalyst component to metathesis reaction in the presence of an ionic liquid, wherein the starting material is a &agr;,&ohgr;-diene bearing a &agr; substituent NRR1 in the &agr; position to a double bond, wherein R is hydrogen or an organic substituent, R1 is tert-butyl, P(R)2, P(R2)2, COR, SO2PhR, COOR or CONRR2, R2is alkyl or phenyl, or R and R1 together form and in which &agr;,&ohgr;-dienes optionally bear at least one further substituent R in any other position with the exception of the &agr; position, wherein R is selected from the group consisting of hydrogen, fused or unfused aryl, alkyl, CN, COOR2 or halogen, and wherein the starting material optionally contains a member selected from the group containing at least one further substituent that is inert in the metathesis reaction and a heteroatom selected from the group consisting of branched alkyl radicals, unbranched alkyl radicalType: GrantFiled: February 25, 2000Date of Patent: June 29, 2004Assignee: Bayer AktiengesellschaftInventors: Christoph Gürtler, Manfred Jautelat
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Patent number: 6706765Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: February 6, 2003Date of Patent: March 16, 2004Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
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Patent number: 6518310Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: March 16, 2001Date of Patent: February 11, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
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Publication number: 20020165264Abstract: Compounds of formula (I) 1Type: ApplicationFiled: January 14, 2002Publication date: November 7, 2002Inventors: Michael E. Kort, Robert J. Gregg, William A. Carroll, Arturo Perez Medrano, Jurgen Dinges, Fatima Z. Basha
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Publication number: 20020147230Abstract: Compounds of formula (I) 1Type: ApplicationFiled: February 7, 2001Publication date: October 10, 2002Inventors: Michael E. Kort, Robert J. Gregg, William A. Carroll, Arturo Perez Medrano, Jurgen Dinges
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Patent number: 6441232Abstract: There is provided a method of selectively replacing a carbon-hydrogen bond at an unactivated saturated sp3 hybridised carbon atom in an organic compound by a carbon-nitrogen bond, the method comprising reacting the compound with a fluorinating agent in a solvent reaction medium comprising a nitrile compound and providing a Lewis acid whereby the carbon-hydrogen bond is replaced by a carbon-nitrogen bond. Advantageously, the reaction may be performed in one stage and/or in one vessel. Advantageously, the method may be carried out at or just below ambient or room temperature.Type: GrantFiled: January 1, 2002Date of Patent: August 27, 2002Assignee: F2 Chemicals Ltd.Inventors: Richard Dickinson Chambers, Mandy Parsons, Graham Sandford
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Patent number: 6326369Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.Type: GrantFiled: July 6, 1999Date of Patent: December 4, 2001Assignee: Takeda Chemicals Industries, Ltd.Inventors: Kaneyoshi Kato, Taiichi Ohra, Masaomi Miyamoto
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Patent number: 6262308Abstract: The invention relates to a process for preparing cis-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine, or racemic sertraline, corresponding to formula (I) in salt form, starting with 4-(3,4-dichlorophenyl)tetralone of formula (II) according to which (a) the 4-(3,4-dichlorophenyl)tetralone of formula (II) is reacted with N-methylformamide in the presence of formic acid, (b) the reaction medium obtained according to (a) is treated with a base, and (c) the racemic sertraline salt is separated out by selective crystallization with an acid. The invention also relates to N-methylformamide-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine and to its use to obtain racemic sertraline.Type: GrantFiled: March 29, 1999Date of Patent: July 17, 2001Assignee: CatalysInventor: Patrick Bigot
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Patent number: 6262295Abstract: A process for the preparation of a racemic or optically active compound of the formula where the group R1 is an unsubstituted or a halogen substituted C1-4-alkyl, a C1-4-alkoxy, an aryl, an arylalkyl, an aryloxy, or arylalkylloxy.Type: GrantFiled: August 13, 1999Date of Patent: July 17, 2001Assignee: Lonza A.G.Inventors: Christine Bernegger, Eva Maria Urban, Olwen Mary Birch, Kurt Burgdorf, Frank Brux, Kay-Sara Etter, Pierre Bossard, Walter Brieden, Laurent Duc, John Gordon, Colm O'Murchu, Yves Guggisberg
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Patent number: 6252112Abstract: A novel process for the preparation of (1S, 4R)- or (1R, 4S)-4-(2-amino-6-chloro-9H-purin-9-yl)-2 -cyclopentene-1-methanol of the formula is described.Type: GrantFiled: August 13, 1999Date of Patent: June 26, 2001Assignee: Lonza A.G.,Inventors: Christine Bernegger, Eva Maria Urban, Olwen Mary Birch, Kurt Burgdorf, Frank Brux, Kay-Sara Etter, Pierre Bossard, Walter Brieden, Laurent Duc, John Gordon, Colm O'Murchu, Yves Guggisberg
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Patent number: 6235925Abstract: Using the process according to the invention, it is possible to provide, with few reaction steps, a novel route to &agr;-substituted ring systems which optionally have further substituents.Type: GrantFiled: August 31, 1999Date of Patent: May 22, 2001Assignee: Bayer AktiengesellschaftInventors: Christoph Gürtler, Manfred Jautelat, Helmut Greiving, Herbert Hugl
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Patent number: 6137007Abstract: A novel process for the preparation of (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9H-purin-9-yl)-2-cyclopentene-1-methanol of the formulae ##STR1## is described. This entails in the first stage (.+-.)-2-azabicyclo[2.2.1]hept-5-en-3-one of the formula ##STR2## being acylated to give a (.+-.)-2-azabicyclo[2.2.1]hept-5-en-3-one derivative of the general formula ##STR3## in which R.sup.1 denotes C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, aryl or aryloxy, the latter being reduced in the second stage to give a cyclopentene derivative of the general formula ##STR4## in which R.sup.Type: GrantFiled: August 13, 1999Date of Patent: October 24, 2000Assignee: Lonza AGInventors: Christine Bernegger, Eva Maria Urban, Olwen Mary Birch, Knut Burgdorf, Frank Brux, Kay-Sara Etter, Pierre Bossard, Walter Brieden, Laurent Duc, John Gordon, Colm O'Murchu, Yves Guggisberg
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Patent number: 5998653Abstract: Compounds of the formula ##STR1## are useful as intermediates to new herbicidal 4-benzoylisoxazoles.Type: GrantFiled: May 19, 1997Date of Patent: December 7, 1999Assignee: Rhone Poulenc Agriculture LimitedInventors: Angela Jacqueline Bailey, Michael Gingell, David William Hawkins
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Patent number: 5939554Abstract: A method for preparing a diarylalanine compound is provided. The method includes reacting a diarylaminopropanediol with a reducing agent to form a diarylaminopropanol compound and/or contacting a serine ester derivative with an aryl metal reagent to form diarylaminopropanediol. A diarylmethyloxazolidinone compound is also provided.Type: GrantFiled: April 17, 1997Date of Patent: August 17, 1999Assignee: NDSU Research FoundationInventors: Mukund P. Sibi, Prasad K. Despande, Anthony J. LaLoggia
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Patent number: 5900507Abstract: The present invention relates to a process for the preparation of 1-amino-1-methyl-3(4)-aminomethyl cyclohexane (AMCA) bya) catalytically hydrogenating 1-formamido-1-methyl-3(4)-cyano cyclohexane (FMC) in a first reaction stage to form 1-formamido-1-methyl-3(4)-aminomethyl cyclohexane (FMA), 1-amino-1-methyl-3(4)-formamidomethyl cyclohexane (AMF), 1-formamido-1-methyl-3(4)-formamidomethyl cyclohexane (FMF) and/or AMCA, andb) reacting FMA, AMF and/or FMF in a second reaction stage with an alkaline compound to from AMCA and a formic acid derivative, andc) separating the reaction mixture obtained in step b) into components by fractional distillation and/or by crystallization and filtration.The present invention is also relates to carrying the hydrogenation reaction of step a) in the presence of a formulating agent to form 1-formamido-1-methyl-3(4)-formamidomethyl cyclohexane (FMF).Type: GrantFiled: March 11, 1998Date of Patent: May 4, 1999Assignee: Bayer AktiengesellschaftInventors: Konrad Fischer, Oswald Wilmes, Dieter Arlt, Carl Casser, Peter Maas, Pierre Woestenborghs, Theo Van Der Knaap, Raf Reintjens
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Patent number: 5856575Abstract: This invention provides a process for the manufacture of N-acetyl amino phenol, which process comprises reacting an appropriate phenol and an amide in the presence of a heteropoly acid or its alkali metal salt catalyst.Type: GrantFiled: January 22, 1997Date of Patent: January 5, 1999Assignee: Council of Scientific Industrial ResearchInventors: Sarada Gopinathan, Changaramponnath Gopinathan, Joseph Kuruvilla, Sanjeevani Amrit Pardhy, Paul Ratnasamy
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Patent number: 5852194Abstract: The present invention relates to new N-substituted cis-N-propenyl-acetamides of the general formula (I) ##STR1## in which R.sup.1 represents in each case optionally substituted alkyl, -C(alkyl).sub.2 -alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aralkyl or hetarylalkyl;a process for their preparation, and their use for the preparation of 2-chloro-5-methyl-pyridine.Type: GrantFiled: June 7, 1996Date of Patent: December 22, 1998Assignee: Bayer AktiengesellschaftInventor: Reinhard Lantzsch
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Patent number: 5753652Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.Type: GrantFiled: April 4, 1995Date of Patent: May 19, 1998Assignee: Novartis CorporationInventors: Alexander Fassler, Guido Bold, Marc Lang, Shripad Bhagwat, Peter Schneider
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Patent number: 5753709Abstract: Certain N-acyl 2-aryl cyclopropylmethylamine derivatives are useful as melatonergic agents.Type: GrantFiled: May 9, 1996Date of Patent: May 19, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Daniel J. Keavy, Michael F. Parker, Ronald J. Mattson, Graham Johnson