Nitrogen In Alcohol Moiety Other Than As Nitro, Nitroso Or Isocyanate Patents (Class 560/250)
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Publication number: 20090118368Abstract: The present invention discloses compounds of formula (I), their optical isomers or pharmaceutically acceptable salts thereof, their preparation and uses thereof, wherein the definitions of R1, R2, R3 and R4 are shown in the description. These compounds are optical isomers or racemic mixtures. After these compounds are uptaken, they are metabolically transformated in vivo into 1-[2-dimethylamino-1-(4-hydroxyphenyl)-ethyl]-cyclohexanol that has neuropharmacological activity, by interrupting reuptake of 5-hydroxytryptamine (5-HT) and/or norepinephrine (NA), which is used for treating diseases associated with central nerve system, such as depression, etc.Type: ApplicationFiled: June 16, 2006Publication date: May 7, 2009Applicants: SHANDONG LUYE PHARMACEUTICAL CO. LTD.Inventor: Luping Zhang
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Patent number: 7402698Abstract: The present invention is directed to secondary amino- and cycloamino-cycloalkanol derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: October 12, 2004Date of Patent: July 22, 2008Assignee: WyethInventors: Paige Erin Mahaney, Michael Byron Webb, Lori Krim Gavrin, Eugene John Trybulski
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Patent number: 7329775Abstract: Ketoamine compounds and related methods for reactivation of tumor suppressor protein p53.Type: GrantFiled: November 1, 2004Date of Patent: February 12, 2008Assignee: Northwestern UniversityInventors: Daniel H. Appella, Michael C. Myers
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Patent number: 7273952Abstract: Substituted C-cyclohexylmethylamine derivatives, methods for the production thereof, pharmaceuticals containing said compounds, the use of substituted C-cyclohexylmethylamine derivatives for producing pharmaceuticals, and method of pain treatment using the pharmaceuticals.Type: GrantFiled: March 31, 2003Date of Patent: September 25, 2007Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Corinna Maul, Helmut Buschmann, Michael Finkam, Babette-Yvonne Koegel
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Patent number: 7253210Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.Type: GrantFiled: October 14, 2003Date of Patent: August 7, 2007Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Igor Rakov
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 7022870Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.Type: GrantFiled: June 17, 2003Date of Patent: April 4, 2006Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Craig A. Marhefka, Wenqing Gao
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Patent number: 6858650Abstract: The present invention concerns highly pure, crystalline, stable compounds of novel derivatives of 3,3-diphenylpropylamines in the form of their salts, a method for the manufacture and highly pure, stable intermediate products. The method is in particular characterized by regio- and chemoselectivity and high yield. Salts of phenolic monoesters of 3,3-diphenylpropylamines are provided, that are particularly well-suited for use in pharmaceutical formulations. Preferred compounds are R-(+)-2-(3-diisopropylamino-1-phenyl-propyl)-4-hydroxymethylphenylisobutyrate ester hydrogen fumarate and R-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenylisobutyrate ester hydrochloride hydrate. Furthermore, stable, crystalline intermediate products that are essential for obtaining the abovementioned salts are provided. A preferred intermediate product is R-(?)-3-(3-diisopropylamino-phenyl-propyl)-4-hydroxy-benzoic acid methyl ester.Type: GrantFiled: November 15, 2000Date of Patent: February 22, 2005Assignee: Schwarz Pharma AGInventor: Claus Meese
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Publication number: 20040192775Abstract: Novel stable and pharmacologically acceptable salts of L-carnitine and lower alkanoyl L-carnitines with alpha-ketoglutaric acid are disclosed as well as the compositions useful as dietary and dietetic supplements, nutraceuticals or drugs containing same.Type: ApplicationFiled: April 7, 2004Publication date: September 30, 2004Inventor: Pietro Pola
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Publication number: 20040147601Abstract: This invention provides O-&agr;-acyloxyalkyl ethers of the venlafaxine metabolite 4-[2-(Dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenol, represented by Formula (I): 1Type: ApplicationFiled: October 24, 2003Publication date: July 29, 2004Applicant: WyethInventors: John P. Yardley, Magid A. Abou-Gharbia, John W. Ullrich
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Publication number: 20040147775Abstract: The present invention relates to a process for the synthesis of 3,3a,6,6a-tetrahydo-2H-cyclopentan[b]furan-2-one.Type: ApplicationFiled: December 12, 2003Publication date: July 29, 2004Inventors: Kevin Edward Henegar, Mateusz Cebula
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Patent number: 6767923Abstract: Benzhydryl derivatives of the formula I, where the index and the variables are as defined below: X is oxygen or sulfur; R1, R3 are halogen, cyano, nitro, hydroxyl, mercapto, amino, alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylcarbonyloxy, formyloxy, alkylthio, alkenylthio, alkynylthio, alkylamino, dialkylamino, alkylcarbonyl or formyl, where the carbon atoms in the radicals mentioned may be partially or fully halogenated; R2 is halogen, cyano, nitro, hydroxyl, mercapto, amino, alkyl, alkoxy, haloalkyl or haloalkoxy, where the groups R2 may be different if n=2; R4 is alkyl, alkenyl or alkynyl, where the carbon atoms in these radicals may be unsubstituted or partially or fully halogenated; R5, R6 are hydroxyl, alkyl, alkenyl, haloalkyl, haloalkenyl, alkoxy, alkenyloxy, haloalkoxy, haloalkenyloxy, cycloalkyl, cycloalkylalkyl, cycloalkoxy or cycloalkylalkoxy; n is 0, 1 or 2; processes for preparing the compounds I, compositions comprising them and their use for conType: GrantFiled: October 29, 2002Date of Patent: July 27, 2004Assignee: BASF AktiengesellschaftInventors: Ingo Rose, Jordi Tormo i Blasco, Markus Gewehr, Wassilios Grammenos, Bernd Müller, Joachim Rheinheimer, Peter Schäfer, Frank Schieweck, Thomas Grote, Andreas Gypser, Eberhard Ammermann, Gisela Lorenz, Reinhard Stierl, Siegfried Strathmann, Paul Carter, Jürgen Curtze
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Publication number: 20040127564Abstract: The present invention provides a series of compounds having structural formulas 1Type: ApplicationFiled: December 12, 2003Publication date: July 1, 2004Applicant: The University of Arkansas for Medical SciencesInventors: Kathleen Gilbert, E. Kim Fifer
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Patent number: 6667341Abstract: Amidomethyl esters, carbonylmercaptomethyl esters, keto-containing esters, amidomethyl thioesters, amidomethyl amides, and methylene dithioesters are disclosed. The novel compounds have two carbonyl groups connected by a linking moiety having an oxygen, sulfur or nitrogen attached to a methylene group, to which is further attached a sulfur, nitrogen or CH2 group. Methods of treating illnesses and conditions, such as cancer, hemological disorders, inherited metabolic disorders and others, using these compounds are also disclosed.Type: GrantFiled: May 17, 2001Date of Patent: December 23, 2003Assignee: Beacon Laboratories, Inc.Inventors: Hsuan-Yin Lan-Hargest, Norbert L. Wiech
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Publication number: 20030166721Abstract: Choline derivatives useful in the treatment of the diseases related with central cholinergic deficitType: ApplicationFiled: March 24, 2003Publication date: September 4, 2003Inventors: Vincenzo Carelli, Felice Liberatore, Luigi Scipione, Mario Cardellini, Domenicantonio Rotiroti, Vincenzo Rispoli
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Patent number: 6593492Abstract: A methods of preparing a substantially pure enantiomer of an acylanilide such as Casodex® (bicalutamide) and/or its derivatives includes resolving an intermediate compound having the structure of Formula I: wherein R1 is alkyl or haloalkyl having up to 4 carbons; R2 is alkyl having up to 6 carbon atoms; R3 is a direct link or alkyl having up to 6 carbon atoms; R4 is alkyl, alkenyl, hydroxyalkyl or cycloalkyl each of up to 6 carbons; or R4 is phenyl which bears one, two or three substituents independently selected from hydrogen, halogen, nitro, carboxy, carbamoyl and cyano, and alkyl, alkoxy, alkanoyl, alkylthio, alkylsulphinyl, alkylsulphonyl, perfluoroalkyl, perfluoroalkylthio, perfluoroalkylsulphinyl, perfluoroalkylsulphonyl, alkoxycarbonyl and N-alkylcarbamoyl each of up to 4 carbon atoms, and phenyl, phenylthio, phenylsulphinyl and phenylsulphonyl; or R4 is naphthyl; or R4 is a 5- or 6-membered saturated or unsaturated heterocyclic which contains one, two or three heteroatoms selType: GrantFiled: October 25, 2000Date of Patent: July 15, 2003Assignee: Nobex CorporationInventors: Nnochiri Nkem Ekwuribe, Kenneth D. James
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Publication number: 20030130539Abstract: An improved process is described for the industrial preparation of L-carnitine or alkanoyl L-carnitine mucate, which allows operations in a homogeneous phase in conditions of greater dilution, in a normal chemical reactor with stirring, in a batch process.Type: ApplicationFiled: October 28, 2002Publication date: July 10, 2003Inventors: Carlo Alberto Bagolini, Angelo De Luca
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Publication number: 20030119904Abstract: A novel solid, crystalline and non-hygroscopic substance consisting of acetyl L-carnitine acid fumarate and a process for preparing same are disclosed.Type: ApplicationFiled: July 31, 2002Publication date: June 26, 2003Inventor: Aldo Fassi
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Publication number: 20030050507Abstract: The invention concerns a method for preparing alkoxyamines in a biphasic medium. Said method consists in mixing an ionic liquid, an organic solvent, a metal salt, a metal ligand, a halogeno-carbonaceous ZX compound and a nitroxide, maintaining the reaction medium under agitation at a temperature between 20° C. and 90° C., until the nitroxide is eliminated, decanting, recuperating the organic phase, optionally washing it with water and then in isolating the alkoxyamine by evaporating the organic solvent under reduced pressure.Type: ApplicationFiled: August 8, 2002Publication date: March 13, 2003Inventors: Jean-Luc Couturier, Olivier Guerret
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Patent number: 6472555Abstract: The present invention relates to a process for the preparation of esters from alcohols using acetic acid as acetylating agent and clays as catalysts, which comprises the preparation of esters in a single step from the reaction of aliphatic, acyclic, cyclic, heterocyclic, &agr;,&bgr;-unsaturated and aromatic alcohols with carbon atoms in the range of C1 to C10 with acetic acid in a molar ratio of 1:3 to 11 using reusable natural montmorillonite/metal ion-exchanged clay catalysts in the solvent medium of aliphatic, aromatic, or chlorinated hydrocarbons at 30-140° C. for a period in the range of 0.02 to 3.0 hrs, and recovering the corresponding esters by simple work-up procedure.Type: GrantFiled: February 12, 1999Date of Patent: October 29, 2002Assignee: Council of Scientific and Industrial ResearchInventors: Boyapati Manoranjan Choudary, Veldurthy Bhaskar, Mannepalli Lakshmi Kantam, Kottapalli Koteswara Rao, Kondapuram Vijaya Raghavan
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Publication number: 20020143056Abstract: The present invention provides a series of compounds having structural formulas 1Type: ApplicationFiled: April 12, 2002Publication date: October 3, 2002Applicant: The University of Arkansas for Medical SciencesInventors: Kathleen Gilbert, E. Kim Fifer
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Patent number: 6444702Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.Type: GrantFiled: February 22, 2000Date of Patent: September 3, 2002Assignee: NeuroMolecular, Inc.Inventors: Yuqiang Wang, Wenqing Ye, James W. Larrick, Jonathan S. Stemler, Stuart A. Lipton
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Publication number: 20020099238Abstract: This invention provides an environmentally clean process for the selective esterfication of a tertiary alcohol (I) by an acid anhydride (II) to produce corresponding tertiary ester (III) and carboxylic acid (V), using a reusable solid catalyst (IV) comprising one or more halides of indium, gallium, zinc and iron. The process comprises: (i) contacting a mixture of (I) and (II) in the absence or presence of a non aqueous solvent with the fine particles of (IV) in a stirred hatch reactor provided with a reflux water condenser at atmospheric pressure at the reaction conditions, such that the mole ratio of (II) to (I) is in the range from about 0.1 to about 10.0; the weight ratio of (IV) to (I+II) is in the range from about 0.005 to about 0.5; the reaction temperate is below about 80° C.; and the reaction period is in the range from about 0.Type: ApplicationFiled: November 29, 2000Publication date: July 25, 2002Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Vasant Ramchandra Choudhary, Kshudiram Mantri, Suman Kumar Jana
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Patent number: 6414170Abstract: The present invention relates to a method for preparing a cationic surfactant in which physical chemical characteristics such as softness, antistatic properties, etc. as well as biodegradability are quite excellent due to having an ester group and a hydrophilic hydroxyl group in its molecules. A cationic surfactant of the present invention is prepared by reacting tertiary amine drivatives, fatty acid, and epihalohydrin, and prepared simply by reacting esterification and quaternary reactions in one step with a high yield. The above cationic surfactant is a high grade alkyl quaternary ammonium compound as represented in General Formula (1), wherein R1 is a C1-C4 alkyl group; R2 is a C7-C21 linear or branched alkyl or alkenyl group; A is OCOR3, NHCOR3 or OH; R3 is a C7-C21 linear or branched alkyl or alkenyl group; X is a halogen atom; and n is an integral number from 2 to 6.Type: GrantFiled: January 23, 2001Date of Patent: July 2, 2002Assignee: LG Chemical Ltd.Inventors: Dong-Il Kim, Jeong-Wook Ha, Tae-Seong Kim, Moon-Jeong Rang
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Patent number: 6383633Abstract: A fluorochemical composition is described comprising a polymer derived from a fluorochemical urethane (meth)acrylate monomer. The fluorochemical composition is useful for imparting stain release properties to a substrate.Type: GrantFiled: September 24, 1999Date of Patent: May 7, 2002Assignee: 3M Innovative Properties CompanyInventors: Kathy E. M. L. A. Allewaert, Pierre J. Vander Elst
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Patent number: 6365626Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: December 7, 2000Date of Patent: April 2, 2002Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Publication number: 20020037922Abstract: This invention provides O-&agr;-acyloxyalkyl ethers of the venlafaxine metabolite 4-[2-(Dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenol, represented by Formula (I): 1Type: ApplicationFiled: November 21, 2001Publication date: March 28, 2002Applicant: American Home Products CorporationInventors: John P. Yardley, Magid A. Abou-Gharbia, John W. Ullrich
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Patent number: 6359147Abstract: Reactions of ring systems, such as aziridines, oxetanes and oxiranes with carboxylic acids, anhydrides, imides, lactones and carbonate esters are catalyzed by C3-C60, substituted or unsubstituted, straight or branched-chained, alkyl, aryl, or aralkyl carboxylate Cr+3 salts, preferably chromium +3 octoate. The catalysts also accelerate the reaction of hydroxy compounds with anhydrides, and of thiiranes with anhydrides. The catalysts selectively enhance the conversion of ring systems to form monomers, prepolymers, copolymers, functional end-group monomers, functional end-group prepolymers, and functional end-group polymers rather than forming homopolymers. By varying the catalyst concentration, molar ratios, and reaction temperatures, the reaction time required to form the desired product can be controlled.Type: GrantFiled: April 3, 2000Date of Patent: March 19, 2002Assignee: Dimension Technology Chemical Systems, Inc.Inventors: Renato R. Rindone, W. Kenneth Musker
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Patent number: 6348615Abstract: A process for producing (2R, 3S)-3-amino-4-phenylbutane-1,2-epoxide compounds which comprises treating a (2S, 3S)-3-amino-1-halo-2-hydroxy-4-phenylbutane compound or a (2S, 3S)-3-amino-4-phenylbutane-1,2-epoxide with a carboxylic acid quaternary ammonium salt or a carboxylic acid metal salt a quaternary ammonium salt and a quaternary ammonium salt, to give a (2S, 3S)-1-acyloxy-3-amino-2-hydroxy-4-phenylbutane compound, further treating the same with a sulfonic acid halide in the presence of an organic base to give a (2S, 3S)-1-acyloxy-3-amino-2-sulfonyloxy-4-phenylbutane compound, furthermore treating said compound with an inorganic base. An intermediate for the production of an HIV protease inhibitor can be produced from L-phenylalanine.Type: GrantFiled: May 11, 2001Date of Patent: February 19, 2002Assignee: Kaneka CorporationInventors: Kazumi Okuro, Kenji Inoue
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Patent number: 6344558Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.Type: GrantFiled: April 20, 2001Date of Patent: February 5, 2002Assignee: Gruenthal GmbHInventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
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Patent number: 6303652Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: March 19, 1999Date of Patent: October 16, 2001Assignee: Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6294575Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: October 16, 2000Date of Patent: September 25, 2001Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Publication number: 20010016666Abstract: The present invention relates to a process for the preparation of esters from alcohols using acetic acid as acetylating agent and clays as catalysts, which comprises the preparation of esters in a single step from the reaction of aliphatic, acyclic, cyclic, heterocyclic, &agr;,&bgr;-unsaturated and aromatic alcohols with carbon atoms in the range of C1 to C10 with acetic acid in a molar ratio of 1:3 to 11 using reusable natural montmorillonite/metal ion-exchanged clay catalysts in the solvent medium of aliphatic, aromatic, or chlorinated hydrocarbons at 30-140° C. for a period in the range of 0.02 to 3.0 hrs, and recovering the corresponding esters by simple work-up procedure.Type: ApplicationFiled: February 12, 1999Publication date: August 23, 2001Inventors: BOYAPATI MANORANJAN CHOUDARY, VELDURTHY BHASKAR, MANNEPALLI LAKSHMI KANTAM, KOTTAPALLI KOTESWARA RAO, KONDAPURAM RAGHAVAN
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Publication number: 20010009923Abstract: Non-hygrocopic salts of L-carnitine and of the lower alkanoyl L-carnitines with pamoic acid are described, which are used to prepare solid compositions suitable for oral administration. Solid compositions containing such salts are also described.Type: ApplicationFiled: December 21, 2000Publication date: July 26, 2001Inventors: Mose Santaniello, Nazareno Scafetta, Maria Ornella Tinti
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Patent number: 6248737Abstract: 1-phenyl-3 -dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.Type: GrantFiled: June 6, 1995Date of Patent: June 19, 2001Assignee: Gruenenthal GmbHInventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
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Patent number: 6225499Abstract: This invention provides a process for preparing aminoarylacetylenes comprising reacting a N-arylmethylidene aminoarylhalide with a terminal acetylene in the presence of a base and a catalyst system comprising a palladium catalyst and a cuprous salt to produce a novel N-arylmethylidene aminoarylacetylene, and hydrolyzing the N-arylmethylidene aminoarylacetylene to the aminoarylacetylene. In one embodiment, the invention provides a process for preparing aminophenylacetylenes comprising reacting a N-benzylidene aminophenylhalide with a terminal acetylene in the presence of a base and the catalyst system to produce a novel N-benzylidene aminophenylacetylene, and hydrolyzing the N-benzylidene aminophenylacetylene to the aminophenylacetylene.Type: GrantFiled: July 14, 1997Date of Patent: May 1, 2001Assignee: Catalytica Pharmaceuticals, Inc.Inventor: John M. Gruber
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Patent number: 6218536Abstract: 1,2-Bis-adducts of stable hindered nitroxide compounds with substituted ethylenes are prepared by reacting two equivalents of nitroxyl compound with an ethylenically unsaturated compound such as styrene or an acrylate ester. These adducts are very effective inhibitors to prevent the premature polymerization of ethylenically unsaturated monomers when such monomers are distilled, processed or stored.Type: GrantFiled: October 7, 1998Date of Patent: April 17, 2001Assignee: Ciba Specialty Chemcials CorporationInventors: Glen Thomas Cunkle, Thomas F. Thompson, Volker H. von Ahn, Roland A. E. Winter
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2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same
Patent number: 6214873Abstract: The present invention relates to a compound of the general formula wherein R1, R2, R3 and R4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.Type: GrantFiled: January 5, 2000Date of Patent: April 10, 2001Assignee: Welfide CorporationInventors: Kunitomo Adachi, Yoshiyuki Aoki, Tokushi Hanano, Koji Teshima, Yukio Hoshino, Tetsuro Fujita -
Patent number: 6160010Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: July 22, 1999Date of Patent: December 12, 2000Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6124270Abstract: A cationic amphipathic compound of formula (I), ##STR1## wherein A is a single bond, an NH--R' grouping or (a), wherein --R'-- is a straight or branched, optionally substituted, saturated or unsaturated C.sub.1-22 aliphatic chain optionally interrupted by one or more O, S or N heteroatoms and one or more saturated, unsaturated or aromatic carbocyclic or heterocyclic radicals; each of R.sub.1, R.sub.2 and R.sub.3, which are the same or different, is a higher acyl or alkyl grouping; each of R.sub.7, R.sub.8 and R.sub.9, which are the same or different, is a (CH.sub.2).sub.n alkylene radical where 1.ltoreq.N.ltoreq.6; each of R.sub.4, R.sub.5 and R.sub.6, which are the same or different, is a hydrogen atom or an optionally substituted C.sub.1-22 alkyl, alkenyl, alkynyl or acyl radical optionally interrupted by one or more heteroatoms selected from), S and N, or one or more saturated, unsaturated or aromatic carbocyclic or heterocyclic radicals, or else at least two of the groupings R.sub.4, R.sub.5 and R.sub.Type: GrantFiled: March 3, 1997Date of Patent: September 26, 2000Assignee: Pasteur Merieux Serums et VaccinsInventor: Jean Haensler
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Patent number: 6100425Abstract: A process for the preparation of the compound L-5-(2-acetoxypropionylamino)-2,4,6-triiodoisophthaloyl dichloride by reacting 5-amino-2,4,6-triiodoisophthaloyl dichloride with L-2-acetoxypropionyl chloride in N,N-dimethylacetamide as a solvent, characterized in that a catalytic amount of a lower alcohol is added to the reaction mixture.Type: GrantFiled: December 19, 1997Date of Patent: August 8, 2000Assignee: Bracco International, B.V.Inventors: Marco Villa, Maurizio Paiocchi
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Patent number: 6069247Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.Type: GrantFiled: October 5, 1998Date of Patent: May 30, 2000Assignee: Eli Lilly and CompanyInventors: Lynne Ann Hay, David Mitchell
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Patent number: 5929272Abstract: Epoxide-amine adducts having a proportion by mass of at least 20% of aliphatic epoxide or amine units which comprise at least one tertiary or quaternary carbon atom are disclosed. The adducts are employed as binders for coatings of relatively high environment-friendliness, if desired, for example, in a mixture with other hydroxy-functional binders, and as reactive component in corresponding adhesive compositions and sealing compounds.Type: GrantFiled: May 2, 1996Date of Patent: July 27, 1999Assignee: Vianova Resins GmbHInventors: Ulrich Epple, Manfred Marten, Uwe Kubillus, Harald Oswald
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Patent number: 5917038Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.Type: GrantFiled: April 11, 1997Date of Patent: June 29, 1999Assignee: Eli Lilly and CompanyInventors: Lynne Ann Hay, David Mitchell
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Patent number: 5892061Abstract: A preparation process of isoimide comprising reacting a compound having one or more carboxyl group and one or more amide bond in the same molecule in the presence of a haloiminium salt and basic substance, and a preparation process of isoimide comprising reacting a compound having one or more carboxyl group with a compound having one or more amide bond in the presence of a haloiminium salt and basic substance are disclosed.Type: GrantFiled: November 21, 1997Date of Patent: April 6, 1999Assignee: Mitsui Chemicals, Inc.Inventors: Kan Ikeda, Wataru Yamashita, Shoji Tamai
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Patent number: 5753707Abstract: An amide derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents a C.sub.1-40 hydrocarbon; R.sup.2 represents a C.sub.1-6 alkylene; R.sup.3 represents H, OH or alkoxyl; R.sup.4 represents a C.sub.1-39 hydrocarbon; R.sup.5 represents ##STR2## with the proviso that when R.sup.5 represents ##STR3## R.sup.3 does not represent OH; and a composition of the amide derivative for topical application to human skin. The composition improves the barrier function of the stratum corneum, providing improvement and prevention of dermatitis, skin roughness, or similar disorders.Type: GrantFiled: September 6, 1996Date of Patent: May 19, 1998Assignee: Kao CorporationInventors: Masahide Hoshino, Hiroshi Kusuoku, Tadashi Hase, Atsuko Otsuka, Ichiro Tokimitsu, Akira Yamamuro, Yoshiya Sugai, Koji Yoshino, Youichi Arai, Shinichi Meguro
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Patent number: 5710279Abstract: The invention provides novel N-acyloxyalkyl-carboxamides of the general formula (I): ##STR1## in which R.sup.1 is alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, arylalkyl or heteroarylalkyl, each of which is optionally substituted,R.sup.2 is optionally substituted alkyl andR.sup.3 is hydrogen, halogen or optionally substituted alkyl,in the isolated and pure form, and a process for their preparation.Type: GrantFiled: September 5, 1996Date of Patent: January 20, 1998Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Werner Lindner
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Patent number: 5705680Abstract: The present invention relates to a process for the preparation of O-acylglycolanilides of the formula (1) ##STR1## in which R.sup.1 and R.sup.2 are identical or different and are hydrogen, halogen, a nitro group, a cyano group, a straight-chain or branched alkyl, alkenyl, alkynyl or alkoxy group having from 1 to 12 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms, a cycloalkyl group having from 6 to 12 carbon atoms or an aryl group having from 6 to 12 carbon atoms,. R.sup.3 is hydrogen or a straight-chain or branched alkyl group having from 1 to 12 carbon atoms, and R.sup.4 is an alkyl group having from 1 to 6 carbon atoms or is a substituted or unsubstituted phenyl radical, in which an aniline of the formula (2) ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 have the same meaning as in formula (1), and an O-acylglycolic acid of the general formula (3) ##STR3## in which R.sup.Type: GrantFiled: August 3, 1995Date of Patent: January 6, 1998Assignee: Hoechst AktiengesellschaftInventors: Andreas Dierdorf, Theodor Papenfuhs
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2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same
Patent number: RE39072Abstract: The present invention relates to a compound of the general formula wherein R1, R2, R3 and R4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.Type: GrantFiled: April 3, 1998Date of Patent: April 18, 2006Assignee: Mitsubishi Pharma CorporationInventors: Kunitomo Adachi, Yoshiyuki Aoki, Tokushi Hanano, Koji Teshima, Yukio Hoshino, Tetsuro Fujita -
Patent number: RE39593Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.Type: GrantFiled: June 17, 2003Date of Patent: April 24, 2007Assignee: Gruenenthal GmbHInventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs