Cyclohexyl Ring Containing Patents (Class 564/462)
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Patent number: 7642381Abstract: The process of the present invention can be briefly summarized as depicted in the following scheme: R1 is C1-Calkyl, R2 is C1-C6alkyl and Hal is a halogen atom.Type: GrantFiled: January 18, 2007Date of Patent: January 5, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Jinhua J. Song, Jinghua Xu
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Publication number: 20090203910Abstract: Organic compounds having nitrogen atoms protected with t-butoxycarbonyl are effectively deprotected by heating in a fluorinated alcohol solution.Type: ApplicationFiled: December 11, 2008Publication date: August 13, 2009Inventors: Jason Chi-Chung Choy, Saul Jaime-Figueroa, Joseph M. Muchowski, Paul J. Wagner
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Publication number: 20090169495Abstract: Disclosed are merocyanine derivatives of formula (1), wherein R1 and R2 independently from each other are branched C4-C22alkyl; or branched C4-C12 alkenyl; R3 and R4 independently from each other are cyano; COR7, COOR7; CONR7R8; SO2(C6-C12)aryl; C2-C12alk-1-enyl; C3-C12cycloalk-1-enyl; C2-C12alk-1-inyl; C2-C12heteroalkyl; C3-C5heterocycloalkyl; C6-C10aryl; or C1-C9heteroaryl; wherein at least one of R3 and R4 is cyano; R5 and R6 independently from each other are hydrogen; C1-C6alkyl; C5-C8cycloalkyl which may be substituted by one or more than one C1-C4alkyl; and R7 and R8 independently from each other are hydrogen; C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; —(CH2)tCOOH; C7-C12aralkyl; C1-C12heteroalkyl; C2-C11heteroaralkyl; C6-C10aryl; C1-C9heteroaryl. The compounds are useful as UV absorbers for protecting human hair and skin against the damaging effect of UV radiation.Type: ApplicationFiled: December 11, 2006Publication date: July 2, 2009Inventors: Barbara Wagner, Astrid Walther, Bernd Herzog
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Publication number: 20090124785Abstract: An isocyanate has been widely used as a starting material for the production of a polyurethane material, a polyisocyanurate material or the like which is suitably applicable to the field of optical materials. Disclosed is a process for producing an isocyanate which includes a step for producing the isocyanate in the form of a hydrochloride with improved productivity. A process for producing a linear or cyclic aliphatic isocyanate comprising the step of reacting a linear or cyclic aliphatic amine with hydrogen chloride to yield a hydrochloride of the linear or cyclic aliphatic amine, the step being performed under a pressure higher by 0.01 MPa or more than the atmospheric pressure.Type: ApplicationFiled: July 20, 2006Publication date: May 14, 2009Applicant: Mitsui Chemicals, Inc.Inventors: Chitoshi Shimakawa, Hiroyuki Morijiri, Hidetoshi Hayashi, Norihiko Fukatsu, Seiichi Kobayashi, Homare Yumoto, Junichi Ishiyama, Shinya Tsuchiyama
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Patent number: 7485755Abstract: An acid addition salt of a carba-sugar amine derivative represented by the following formula (1): wherein R1 and R2 each independently represents a hydrogen atom, or an alkyl group, an alkenyl group, an alkynyl group, an acyl group, an aryl group or an aralkyl group which may have one or at least two of the following substituent (I) or (II), or R1 and R2 are taken together to represent a substituent (III) (R8 to R12 each independently represents an alkyl group, an alkenyl group, an alkynyl group, an acyl group, an aryl group or an aralkyl group), with the proviso that both R1 and R2 are not a hydrogen atom at the same time; R3, R4 and R7 each independently represents a hydroxyl group or a hydroxyl group having a substituent; and R5 and R6 each independently represents a hydrogen atom, or a hydroxyl group or a hydroxyl group having a substituent, with the proviso that when one of R5 and R6 is a hydrogen atom, the other is a hydroxyl group or a hydroxyl group having a substituent.Type: GrantFiled: May 19, 2004Date of Patent: February 3, 2009Assignee: Seikagaku CorporationInventors: Kiyoshi Suzuki, Masami Iida, Yuji Kaneda, Naoko Kajimoto, Miwa Sawa
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Publication number: 20090023876Abstract: Crosslink agents used to copolymerize at least one hydrophilic monomer with at least one lens monomer typically used to prepare polymeric materials for ophthalmic lenses. The crosslink agents have a relatively high selectivity for the hydrophilic monomer and limited reactivity with the crosslink agent used to polymerize the lens monomer. Accordingly, the invention is also directed to a hydrophilic crosslinked polymer that comprises at least two monomeric units and at least two different crosslink units. The use of the dual crosslink system provides an improved means to control the final chemical, physical and structural characteristics of the resulting polymer.Type: ApplicationFiled: July 8, 2008Publication date: January 22, 2009Inventors: Ivan M. Nunez, Joseph A. McGee, David E. Seelye
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Publication number: 20080312470Abstract: The present invention is directed to novel compounds which are derivatives of minocycline or doxycycline, pharmaceutical compositions containing same and use thereof in lowering excess IgE levels in a mammal suffering from a disease where IgE is pathogenic.Type: ApplicationFiled: August 25, 2008Publication date: December 18, 2008Applicant: The Research Foundation of State University of New YorkInventors: Helen G. Durkin, Martin H. Bluth, Tamar A. Smith-Norowitz, Rauno Joks, Alexander Kiselyov
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Patent number: 7432399Abstract: A polyol monomer comprising the formula: R1 and R3 are —H, aliphatic, aromatic, or ether; R2 is aliphatic, aromatic, ester, ether, or acrylic, and R1 contains a hydroxyl group, R3 contains a hydroxyl group, R2 contains —O—CH2—CH(OH)—, or any combination thereof. The polyol monomer may be made by reacting an epoxy and an amine. Either the epoxy contains more than one epoxide groups, the amine contains a hydroxyl group, or both. A thermoset made by reacting the polyol monomer with a polyisocyanate.Type: GrantFiled: November 2, 2004Date of Patent: October 7, 2008Assignee: The United States of America as represented by the Secretary of the NavyInventors: Jozef Verborgt, Arthur Anthony Webb
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Publication number: 20080242861Abstract: This invention relates to methods of preparing the compounds of formula (V): Each variable in this formula is defined in the specification.Type: ApplicationFiled: April 2, 2007Publication date: October 2, 2008Inventors: Chi-Feng Yen, Chang-Pin Huang, Cheng-Kung Hu, Ming-Chen Chou, Chi-Hsin Richard King
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Publication number: 20080234319Abstract: The invention provides compounds of formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, wherein R1, R2, R3 and n are as defined in the specificationType: ApplicationFiled: March 21, 2008Publication date: September 25, 2008Inventors: Simon David Guile, Mark Ebden
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Patent number: 7419981Abstract: The instant invention relates to a combination of an alpha-2-delta ligand and a PDEV inhibitor for use in therapy, particularly in the treatment of pain, particularly neuropathic pain. Particularly preferred alpha-2-delta ligands are gabapentin and pregabalin. A particularly preferred PDEV inhibitors is sildenafil.Type: GrantFiled: February 3, 2004Date of Patent: September 2, 2008Assignee: Pfizer Inc.Inventors: Mark John Field, Richard Griffith Williams
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Publication number: 20080167499Abstract: Aldehyde or ketone compounds having more than one carbonyl group are reductively aminated to form a product amine compound having more than one primary amino group. The aldehyde or ketone compound is reacted with the product amine compound in the presence of an alcohol solvent, to form a reaction mixture that contains one or more intermediates. The intermediate is then reductively aminated to form the desired product. This process may produce the desired product in very high yields with low levels of secondary amine impurities.Type: ApplicationFiled: December 14, 2007Publication date: July 10, 2008Applicant: DOW GLOBAL TECHNOLOGIES INC.Inventors: Erich J. Molitor, Todd W. Toyzan
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Publication number: 20080124285Abstract: Described are merocyanine derivatives of formula (1a) or (1b) wherein n and o are integers from 2 to 4 and aminocyclohexenone intermediates. They are used in protecting human and animal hair and skin from UV radiation.Type: ApplicationFiled: December 8, 2004Publication date: May 29, 2008Inventors: Barbara Wagner, Thomas Ehlis, Stefan Muller
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Patent number: 7365192Abstract: The present invention provides a preparation method of valienamine from acarbose or acarbose derivatives using organic acid TFA (trifluoroacetic acid). By using the method of the present invention, valienamine, the core precursor of voglibose which is a strong retardant of ?-glucosidase and which is used for the cure of diabetes, can be produced in large quantities by using selective hydrolysis from acarbose or acarbose derivatives using TFA.Type: GrantFiled: November 23, 2002Date of Patent: April 29, 2008Assignee: B T Gin, Inc.Inventors: Youl Her, Jin-Hwan Oh
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Publication number: 20080045738Abstract: The invention relates to a one-stage or multistage process for preparing mono-, di- and/or polyamines from compounds having carbodiimide groups and optionally also other groups of isocyanate chemistry by hydrolysis with water.Type: ApplicationFiled: January 27, 2005Publication date: February 21, 2008Applicant: DEGUSSA AGInventors: Matthias Orschel, Rainer Lomolder, Stephan Kohlstruk
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Patent number: 7276631Abstract: The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment of the disclosure relates to compounds of Formula (I); or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.Type: GrantFiled: July 18, 2005Date of Patent: October 2, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Huan He
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Patent number: 7232847Abstract: The invention relates to 4-hydroxymethyl-1-aryl-cyclohexylamine compounds, methods for their production, pharmaceutical formulations containing such compounds and the use of 4-hydroxymethyl-1-aryl-cyclohexylamine derivatives for producing medicines which are useful, for example for treating pain. Related methods of treatment are also provided.Type: GrantFiled: May 11, 2005Date of Patent: June 19, 2007Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Hans Schick, Claudia Hinze
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Patent number: 7196226Abstract: The present invention relates to fluorination reagents comprising 1-fluoro-1-aminoolefins and also processes for preparing fluorination reagents comprising 1-fluoro-1-aminoolefins.Type: GrantFiled: December 16, 2004Date of Patent: March 27, 2007Assignee: Lanxess Deutschland GmbHInventors: Wolfgang Ebenbeck, Albrecht Marhold
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Patent number: 7084303Abstract: The present invention provides ester group-containing tertiary amine compounds of the formula (R1OCH2CH2)nN(CH2CH2CO2R2)3-n which, when used as additives in chemical amplification photolithography, can yield photoresists having a high resolution and an excellent focus margin. The present invention also provides a process comprising the step of subjecting a primary or secondary amine compound to Michael addition to an acrylic ester compound; a process comprising the steps of subjecting monoethanolamine or diethanolamine to Michael addition to an acrylic ester compound so as to form an ester group-containing amine compound and introducing a R1 group to the resultant ester group-containing amine compound; and a process comprising the step of effecting the ester exchange reaction of an ester group-containing tertiary amine with R2OH.Type: GrantFiled: April 22, 2002Date of Patent: August 1, 2006Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Takeru Watanabe, Koji Hasegawa, Takeshi Kinsho, Jun Hatakeyama
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Patent number: 7038087Abstract: An object of the present invention is to provide a process for the production of an optically active amino alcohol, particularly an optically active amino alcohol of a trans-form, being excellent in economy and efficiency, and suitable for industry using easily available and less expensive materials. The present invention relates to a process for the production of an optically active amino alcohol comprising the steps that an optically active hydroxy ester in a trans-form obtained by an asymmetric hydrogenation of an easily available ?-keto ester is reacted with hydrazine, the resulting optically active hydrazinocarbonyl alcohol is subjected to a Curtius rearrangement in the presence of alcohol and protective group of amino group of the resulting optically active alkoxycarbonylamino alcohol is deprotected. As a result of the process for the production in accordance with the present invention, the objected substance is able to be prepared in a high optical purity and in a high yield.Type: GrantFiled: September 4, 2003Date of Patent: May 2, 2006Assignee: Takasago International CorporationInventors: Takahiro Fujiwara, Hideki Nara, Tsukasa Sotoguchi
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Patent number: 7026514Abstract: N,N?-bis(3-aminopropyl)cyclohexane-1,4-diamine, of formula (I), is a new compound that is prepared by hydrogenation with Raney nickel catalyst of N,N?-bis(2-cyanoethyl)-cyclohexane-1,4-diamine, the latter being prepared by reaction between 1,4-cyclohexanediamine and acrylonitrile. The oral administration to genetically alcoholic rats (from the strain UChB of the University of Chile) of the tetrametanesulfonate monohydrate of (I) causes a significant reduction in the alcohol consumption. The activity lasts for some time after the treatment period. Besides, there is a virtually null disulfiram-like adverse effect, what constitutes an advantage over the unpleasant use of some anti-alcoholism agents, such as calcium cyanamide or disulfiram itself.Type: GrantFiled: July 1, 2002Date of Patent: April 11, 2006Assignee: Garbil Pharma Investigacion Chile Ltda.Inventors: Norberto Bilbeny Lojo, Hernan Garcia Madrid, Maria Belen Font Arellano
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Patent number: 6962964Abstract: This invention relates to improved polyepoxide resins cured with a mixture of methylene bridged poly(cycloaliphatic-aromatic)amines and a process for preparing such polyepoxide resins as well as to the methylene bridged poly(cycloaliphatic-aromatic)amine compositions and a method of making them. The improvement resides in using a curative (herein referred to as “Heavy MPCA”) comprised of the partially hydrogenated condensation product of formaldehyde and aniline or methyl substituted aniline containing a substantial amount (from 35 to 85% by weight, preferably 40 to 60% by weight) of oligomers in the form of 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 and 15 aniline or methyl substituted aniline derivatives.Type: GrantFiled: February 6, 2003Date of Patent: November 8, 2005Assignee: Air Products and Chemicals, Inc.Inventors: Michael Ulman, Gamini Ananda Vedage, David Alan Dubowik, Stephen Michael Boyce
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Patent number: 6951958Abstract: Described is method for preparing tertiary amines comprising sequential, exhaustive alkylation of a hydroxylamine derivative and cleavage of the O—N bond using the following steps: a) reacting the hydroxylamine derivative with an alkylating agent or with a carbonyl compound to form an oxime intermediate. b) reacting the oxime intermediate with a reducing agent to produce an alkylated derivative c) reacting the alkylated derivative with an alkylating agent or a carbonyl compound in the presence of a reducing agent to produce a dialkylated derivative d) reacting the dialkylated derivative with an alkylating agent to produce a quaternized derivative e) reacting the quaternized derivative with a reagent causing cleavage of the O—N bond to produce a tertiary amine.Type: GrantFiled: August 3, 2000Date of Patent: October 4, 2005Assignee: Acadia Pharmaceuticals Inc.Inventors: Carl-Magnus A. Andersson, Magnus Gustafsson, Kent R. I. Olsson
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Patent number: 6828462Abstract: Unsaturated 1-Amino-alkylcyclohexane compounds which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.Type: GrantFiled: November 6, 2002Date of Patent: December 7, 2004Assignee: Merz Pharma GmbH & Co. KGAAInventors: Markus Henrich, Wojciech Danysz, Christopher Graham Raphael Parsons, Ivars Kalvinsh, Valerjans Kauss, Aigars Jirgensons, Markus Gold
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Publication number: 20040225015Abstract: A carba-sugar amine derivative represented by the following formula (1) or (2) is used as the active ingredient of a &bgr;-galactosidase inhibitor or a glycolipid metabolic disorder treating agent.Type: ApplicationFiled: March 8, 2004Publication date: November 11, 2004Applicant: Seikagaku CorporationInventors: Seiichiro Ogawa, Yoshiyuki Suzuki, Eiji Nanba, Junichiro Matsuda, Kousaku Ohno
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Patent number: 6765104Abstract: The present invention provides transition metal complexes of N,N′,N″-trialkyl-cis,cis-1,3,5-triaminocyclohexane and related compositions and methods of synthesis and use in vitro and in vivo, such as a therapeutic agent or a delivery/imaging agent.Type: GrantFiled: June 18, 2002Date of Patent: July 20, 2004Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Martin Brechbiel, Roy P. Planalp, Kim Deal
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Patent number: 6747149Abstract: N-Substituted glucamine compounds of formula I are effective in treatment of hepatitis infections, including hepatitis B and hepatitis C. In treating hepatitis infections the compounds of formular I may be used alone, or in combinatioin with another antiviral agent selected from among nucleosides, nucleotides, immunomodulators, immunostimulants or various combination of such other agents.Type: GrantFiled: December 17, 2002Date of Patent: June 8, 2004Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Martin L. Bryant, Richard A. Partis
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Patent number: 6723879Abstract: Disclosed is a process for the enantioselective production of an optically active amino compound by the amination of the C—H bond of an organic compound. The amino compound is produced by converting the C—H bond at the allyl position of an alkene or the C—H bond at the benzyl position of an alkylarene to the corresponding C—N bond, using a salen-manganese complex as the catalyst and N-substituted iminoaryliodinane as the amination agent. Both the catalytic activity and the enantioselectivity are very high when there is used a catalyst in which the 3- and 5-positions of the salicylaldehyde moiety of the salen ligand are substituted with an electron-withdrawing group, particularly with a halogen atom.Type: GrantFiled: November 7, 2002Date of Patent: April 20, 2004Assignee: Japan Science and Technology CorporationInventors: Tsutomu Katsuki, Yoshinori Kohmura
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Publication number: 20040054184Abstract: Tertiary perfluorocycloamines (TPFCAs) of general formula (1) 1Type: ApplicationFiled: October 7, 2003Publication date: March 18, 2004Inventors: Lev Lvovich Gervits, Kirill Nikolaevich Makarov, Ilich Maevsky Evgeny
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Patent number: 6632635Abstract: Methods are disclosed for refolding proteins of the TGF-&bgr; family of proteins. The methods employ as refolding agents one or more compounds which are acid substituted aminocyclohexanes.Type: GrantFiled: May 22, 2000Date of Patent: October 14, 2003Assignee: Genetics InstituteInventor: Steven M. Vicik
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Patent number: 6583246Abstract: The invention provides modifiers for the anionic polymerization of conjugated dienes or of conjugated dienes with vinylaromatic compounds, wherein the modifiers are specific aminoethers.Type: GrantFiled: November 6, 2001Date of Patent: June 24, 2003Assignee: Bayer AktiengesellschaftInventors: Michael Grün, Thomas Knauf, Wilfried Braubach
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Patent number: 6562934Abstract: An amino compound obtained by addition reaction of diamine represented by the following formula (1) and an alkenyl compound and a process for producing the same. H2N—H2C—A—CH2—NH2 (1) wherein A is a phenylene group or a cyclohexylene group.Type: GrantFiled: September 10, 2001Date of Patent: May 13, 2003Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Shinichi Yonehama, Tetsushi Ichikawa
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Patent number: 6448445Abstract: The invention relates to a method for disubstituting carboxylic acid amides on the geminal carbonyl-C-atom using at least one grignard reagent in the presence of a metal alcoholate compound used as a catalyst and in the presence of another organometallic compound used as a co-catalyst.Type: GrantFiled: February 23, 2001Date of Patent: September 10, 2002Assignee: Merck Patent Gesellschaft mit beschraenkter HaftungInventors: Herwig Buchholz, Urs Welz-biermann, Armin Meijere
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Publication number: 20020072632Abstract: New ligands having a backbone comprised of NCCX can be combined with a metal or metal precursor compound or formed into a metal-ligand complex to catalyze a number of different chemical transformations, including polymerization.Type: ApplicationFiled: February 1, 2002Publication date: June 13, 2002Applicant: Symyx TechnologiesInventors: Anil S. Guram, Anne Marie LaPointe, Howard W. Turner, Tetsuo Uno
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Patent number: 6369274Abstract: 1,n-cyclohexanediamines (n=2, 3, 4) of general formula (I), wherein one of the radicals R1 to R3 is an amino group and the two others mean hydrogen, are produced from the corresponding cyclohexanediols and ammonia in the presence of a catalyst containing cobalt, at 100° to 350° C. and 50 to 300 bar. The compounds that can be produced according to the invention are structural elements for polymers, especially polyamides, polyimides, polyurea or polyurethanes, and ligands for cytostatically effective transition metal complexes.Type: GrantFiled: July 20, 2001Date of Patent: April 9, 2002Assignee: Lonza AGInventors: Alfons Baiker, Tamas Mallat, Achim Fischer
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Patent number: 6242641Abstract: The present invention relates to compounds selected from formula I wherein R1, R2, R3 and R4 are the same or different and represent hydrogen, C1, to C6-alkyl, C5 to C6-cycloalkyl, phenyl and halogen, m and n are the same or different and represent the 2, 3, 4 or 5, X, A and B represent carbon and Y1, Y2, Z1 and Z2 are the same or different and represent hydrogen, hydroxyl (OH), amino (NH2), isocyanato (NCO) or 4-hydroxyphenyl.Type: GrantFiled: March 22, 1999Date of Patent: June 5, 2001Assignee: Bayer AktiengesellschaftInventors: Manfred Jautelat, Carl Casser, Hanns-Peter Müller, Manfred Hajek
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Patent number: 6232501Abstract: This invention relates to a process for the cis-selective preparation of cyclic amines of the sertraline type by reductive alkylation of cyclic immines or of their precursors and for the catalytic hydrogenation in the presence of copper-containing catalysts.Type: GrantFiled: September 14, 2000Date of Patent: May 15, 2001Assignee: Ciba Specialty Chemicals CorporationInventors: Heinz Steiner, Markus Benz, Hans-Peter Jalett, Marc Thommen
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Patent number: 6172116Abstract: wherein R1, R2, R3 and R4 are selected independently from each other from —NR5R6, —NR5R6R7+, hydrogen, aryl or heteroaryl with up to 7 ring members, C1-C20-alkyl, C1-C20-alkenyl and C1-C20-alkinyl, wherein the alkyl, alkenyl and alkinyl residues can be branched, unbranched or cyclized and optionally substituted with halogen, aryl or heteroaryl with up to 7 ring members, with the proviso that at least one of the residues R1, R2, R3 and R4 are represented by —NR5R6 or —NR5R6R7; and R5, R6 and R7 are selected independently from each other from hydrogen, aryl or heteroaryl with up to 7 ring members, C1-C20-alkyl, C1-C20-alkenyl, C1-C20-alkinyl, wherein the alkyl, alkenyl and alkinyl residues can be branched, unbranched or cyclized and optionally substituted with halogen, aryl or heteroaryl with up to 7 ring members, or R5 and R6, together with the nitrogen atom, form a heterocyclic group with up to 7 ring members; for the regulation of the activity of already activType: GrantFiled: July 31, 1998Date of Patent: January 9, 2001Assignee: Merz + Co. GmbH & Co.Inventor: Erich F. Elstner
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Patent number: 6111140Abstract: Catalysts containing ruthenium and palladium for the hydrogenation of aromatic amines to cycloaliphatic amines. Methods for making and using the catalysts.Type: GrantFiled: April 5, 1999Date of Patent: August 29, 2000Assignee: Bayer AktiengesellschaftInventors: Hans-Josef Buysch, Gerhard Darsow, Otto Immel, Reinhard Langer
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Patent number: 6069176Abstract: The present invention relates to phenylethanolamine compounds represented by general formula [I]: ##STR1## (where R.sub.1 represents hydrogen or halogen; R.sub.2 represents hydrogen, hydroxy, lower alkoxy, lower alkoxy substituted with one or two lower alkoxycarbonyl or carboxy groups, lower alkoxy substituted with lower alkylaminocarbonyl which may be substituted with lower alkoxy, lower alkoxy substituted with cyclic aminocarbonyl of 4 to 6 carbon atoms, lower alkoxycarbonyl or carboxy; R.sub.3 represents hydrogen, hydroxy, lower alkoxy or lower alkoxy substituted with one or two lower alkoxycarbonyl or carboxy groups; R.sub.2 and R.sub.3 may be bonded to each other to form methylenedioxy substituted with carboxy or lower alkoxycarbonyl; and m and n are 0 or 1), and their pharmacologically acceptable salts, which have a potent .beta.3 adrenergic stimulating effect and high .beta.3 adrenergic receptor selectivity, as well as to processes for their production and intermediates in their production.Type: GrantFiled: April 24, 1998Date of Patent: May 30, 2000Assignee: Mitsubishi-Tokyo Pharmaceuticals, Inc.Inventors: Susumu Tsuchiya, Nobuyuki Yasuda, Toshifumi Matsumoto, Kozo Hiratsuka, Hiroyuki Iizuka, Atsusi Hukuzaki, Kouichi Matsunaga
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Patent number: 6034134Abstract: Certain 1-aminoalkylcyclohexanes are systemically-active uncompetitive NMDA receptor antagonists having rapid blocking/unblocking kinetics and strong voltage-dependency and are therefore useful in the alleviation of conditions resulting from disturbances of glutamatergic transmission giving them a wide range of utility in the treatment of CNS disorders involving the same, as well as in non-NMDA indications, due to their immunomodulatory, antimalarial, anti-Borna virus, and anti-Hepatitis C activities and utilities. Pharmaceutical compositions thereof and a method-of-treating conditions which are alleviated by the employment of an NMDA receptor antagonist, as well as the aforementioned non-NMDA indications, and a method for the preparation of the active 1-aminoalkylcyclohexane compounds involved.Type: GrantFiled: August 27, 1998Date of Patent: March 7, 2000Assignee: Merz + Co. GmbH & Co.Inventors: Markus Gold, Wojciech Danysz, Christopher Graham Raphael Parsons, Ivars Kalvinsh, Valerjans Kauss, Aigars Jirgensons
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Patent number: 6013838Abstract: Novel trifluoromethylated intermediates are provided which are useful in synthesizing trifluoromethylated organic compounds. Specifically, compounds of the formula CF.sub.3 CR are provided, wherein R is (Cl).dbd.CHCH.sub.2 SO.sub.2 Ph, (Cl).dbd.CHCH.sub.2 CH.sub.2 C(.dbd.O)CH.sub.3, (Cl).dbd.CHCH.sub.2 CH(COCH.sub.3).sub.2, (Cl).dbd.CHCH.sub.2 NR'R" or H.dbd.CHCH.dbd.NR'; R' and R" are the same or different and are selected from the group consisting of hydrogen, unsubstituted or substituted C.sub.1 to C.sub.6 straight chain or branched alkyl, unsubstituted or substituted C.sub.3 to C.sub.7 cycloalkyl, unsubstituted or substituted C.sub.2 to C.sub.12 alkenyl, a benzyl group unsubstituted or substituted with R'", or a phenyl group unsubstituted or substituted with R'"; or R' and R" taken together form a five- or six-membered ring; and R'" is an unsubstituted or substituted C.sub.1 to C.sub.6 straight chain or branched alkyl, an unsubstituted or substituted C.sub.1 to C.sub.Type: GrantFiled: January 26, 1999Date of Patent: January 11, 2000Assignee: Alliedsignal Inc.Inventor: Michael Van Der Puy
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Patent number: 5923044Abstract: A process for producing nornally liquid hydrocarbon solutions of lithium dialkylamides and lithium alkylenecycloimides, essentially free of ethers and by-product gaseous alkanes derived from C1-C4 alkyllithium compounds, comprising reacting lithium metal with a C.sub.5 to C.sub.12 secondary amine and an electron carrier compound containing at least five carbon atoms in a normally liquid hydrocarbon solvent.Type: GrantFiled: May 15, 1997Date of Patent: July 13, 1999Assignee: FMC CorporationInventors: Randy W. Hall, James A. Schwindeman, Conrad W. Kamienski, John F. Engel
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Patent number: 5814616Abstract: The present invention is directed to methods of reducing the degree of inflammation arising from a secondary immune response in a mammal due to antigen exposure (challenge) by the administration of valienamine-related disaccharide compounds and the pharmaceutical compositions employed in the method.Type: GrantFiled: November 5, 1996Date of Patent: September 29, 1998Assignee: Alberta Research CouncilInventors: Om P. Srivastava, Roman Szweda, Richard H. Smith, Robert M. Ippolito, Ulrike Spohr
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Patent number: 5801202Abstract: Disclosed is an amine derivative represented by the following formula (1) or an acid addition salt thereof: ##STR1## wherein R.sup.1 represents a group ##STR2## a cyclopentyl group, cyclohexyl group, or a cycloheptyl group, R.sup.2 is a hydrogen atom or C1-C3 alkyl group which may be substituted by one or more hydroxyl groups, m is an integer falling in the range from 3 to 5 inclusive, and n is an integer falling in the range from 9 to 11 inclusive. Also, intermediates useful in the manufacture of the amine derivative (1), compositions for external application to the skin containing the amine derivative, and keratinization improvers containing the amine derivative as an active component are described. The compound (1) has excellent keratinization improving action, pigmentation preventing action, etc.Type: GrantFiled: May 30, 1997Date of Patent: September 1, 1998Assignee: Kao CoprorationInventors: Taketoshi Fujimori, Hiroshi Kusuoku, Akira Yamamuro, Yukihiro Yada, Kazuhiko Higuchi, Genji Imokawa, Naoki Kondo, Yoshinori Masukawa, Hajime Tokuda, Hisashi Tsujimura
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Patent number: 5773617Abstract: The present invention relates to a reagent and to a process which are useful, when carrying out an organic synthesis, for cleaving an allylic group from a function which is protected with the latter.This reagent is defined in that it contains:a) a solvent system;b) a catalyst containing at least one element from column VIII of the Periodic Table of the Elements, the said element from column VIII of the Periodic Table being coordinated with at least one coordination agent which is soluble in the said solvent system;c) a compound which is at least partially soluble in the said solvent system and which contains at least one nucleophilic function.Application to organic synthesis.Type: GrantFiled: February 22, 1996Date of Patent: June 30, 1998Assignee: Rhone-Poulenc ChimieInventors: Jean-Marie Bernard, Errol Blart, Jean-Pierre Genet, Sandrine Lemaire-Audoire, Monique Savignac
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Patent number: 5741928Abstract: Disclosed is a process for producing bis(aminomethyl)cyclohexane, which comprises hydrogenating a xylylenediamine in the presence of a catalyst and at least one solvent selected from the group consisting alkylamines and alkylenediamines.Type: GrantFiled: September 19, 1995Date of Patent: April 21, 1998Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Shoichi Kobayashi, Susumu Naito
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Patent number: 5739405Abstract: A process for the preparation of amines of the general formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 denote hydrogen, C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.20 alkenyl, C.sub.2 -C.sub.20 alkynyl, C.sub.3 -C.sub.20 cycloalkyl, C.sub.4 -C.sub.20 alkylcycloalkyl, C.sub.4 -C.sub.20 cycloalkylalkyl, aryl, C.sub.7 -C.sub.20 alkylaryl, or C.sub.7 -C.sub.20 aralkyl,R.sup.1 and R.sup.2 together denote a saturated or unsaturated C.sub.3 -C.sub.9 alkylene dichain andR.sup.3 or R.sup.5 denotes C.sub.21 -C.sub.200 alkyl, C.sub.21 -C.sub.200 alkenyl or they together form a C.sub.2 -C.sub.12 alkylene dichain,by the reaction of olefins of the general formula II ##STR2## in which R.sup.3, R.sup.4, R.sup.5, and R.sup.6 have the above meanings, with ammonia or primary or secondary amines of the general formula III ##STR3## in which R.sup.1 and R.sup.2 have the above meanings, at temperatures ranging from 200.degree. to 350.degree. C.Type: GrantFiled: December 4, 1996Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Karsten Eller, Rudolf Kummer, Peter Stops
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Patent number: 5726308Abstract: A process for preparing high purity solutions of highly substituted lithium amide bases by direct reaction of lithium metal with highly substituted amine bases alone or in an ether solvent, a hydrocarbon solvent or in a mixed ether/hydrocarbon solvent mixture, optionally in the presence of a catalyst selected from tin salts and transition metal salts of Groups 4B, 5B, 6B, 7B, and 8 of the Periodic Table.Type: GrantFiled: March 22, 1996Date of Patent: March 10, 1998Assignee: FMC CorporationInventors: Randy W. Hall, Robert S. Wedinger, Terry L. Rathman, James A. Schwindeman
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Patent number: 5719280Abstract: The present invention relates to novel benzocycloalkylazolethione compounds which are dopamine .beta.-hydroxylase inhibitors in which the benzocycloalkyl portion of the compound is selected from indanyl, 1,2,3,4-tetrahydronaphthalenyl and 6,7,8,9-tetrahydro-5H-benzocycloheptenyl (in which the benzo is optionally substituted with one to three substituents) and the azolethione portion of the compound is selected from 2-thioxo-2,3-dihydro-1H-imidazol-3-yl, 5-thioxo-4,5-dihydro-1H-?1,2,4!triazol-4-yl and 5-thioxo-4,5-dihydro-1H-?1,2,4!triazol-1-yl (each optionally substituted with one to three substituents); and the prodrugs, pharmaceutically acceptable salts, individual isomers and mixtures of isomers and the methods of using and preparing such benzocycloalkylazolethione compounds.Type: GrantFiled: April 7, 1997Date of Patent: February 17, 1998Assignee: Syntex (U.S.A.) Inc.Inventors: Gregory Ricardo Martinez, Owen Will Gooding, David Bruce Repke, Philip Jay Teitelbaum, Keith Adrian Murray Walker, Roger Lewis Whiting