Benzene Ring Containing Patents (Class 564/139)
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Patent number: 7678879Abstract: The invention is based on the discovery that the compounds and compositions described herein are useful as film-forming adhesives for use in a variety of applications, including, for example, adhesive tapes for the electronic packaging industry. The invention compositions described herein can be cured in a variety of ways with or without a catalyst.Type: GrantFiled: November 1, 2006Date of Patent: March 16, 2010Assignee: Designer Molecules, Inc.Inventor: Stephen M. Dershem
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Publication number: 20100036163Abstract: Process for the industrial synthesis of the compound of formula (I)Type: ApplicationFiled: August 3, 2009Publication date: February 11, 2010Applicant: LES LABORATOIRES SERVIERInventors: Christophe Hardouin, Jean-Pierre Lecouve
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Patent number: 7612236Abstract: It is provided that a method for producing an optically active bisamidoalcohol compound represented by the formula (3): wherein R1 represents a C1-6 alkyl group, an optionally substituted phenyl group, an optionally substituted aralkyl group or a hydrogen atom, or two R1s, which are bonded to the same carbon atom, are bonded to form a ring together with the carbon atom to which they are bonded, R2 represents a C1-6 alkyl group, an optionally substituted phenyl group, a 1-naphthyl group, a 2-naphthyl group or an optionally substituted aralkyl group, R3 and R4 are the same or different, and each represents a hydrogen atom or C1-3 alkyl group, m represents an integer of 0 to 2, and * represents an asymmetric center, which comprises reacting an optically active aminoalcohol compound represented by the formula (1): wherein R1, R2 and * are as defined above, with a diester compound represented by the formula (2): wherein R3, R4 and m are as defined above and R5 represents a C1-3 alkyl group,Type: GrantFiled: December 21, 2004Date of Patent: November 3, 2009Assignee: Sumitomo Chemical Company, LimitedInventor: Makoto Itagaki
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Publication number: 20090253927Abstract: A process for the preparation of a compound of formula (I): which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.Type: ApplicationFiled: March 31, 2009Publication date: October 8, 2009Inventors: Ursula Hoffmann, Michael Jansen, Reinhard Reents, Helmut Stahr
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Patent number: 7586004Abstract: The invention relates to a process for continuously preparing alkylamino(meth)acrylamide by reacting methyl (meth)acrylate, ethyl (meth)acrylate or amines having a high boiling point compared to methanol or ethanol. A special workup technique which includes removing water from the amine before entering the reactor allows product qualities which have hitherto not been attained to be achieved. In addition, very high space-time and overall yields can be achieved.Type: GrantFiled: April 13, 2004Date of Patent: September 8, 2009Assignee: Roehm GmbH & Co. KGInventors: Volker Schleep, Thomas Mertz
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Publication number: 20090221848Abstract: The invention relates to a process for preparing chiral octenoic acid derivatives, which constitute important intermediates in the preparation of medicament active ingredients, and also to novel intermediates which are used in the process for preparing the octenoic acid derivatives mentioned.Type: ApplicationFiled: October 27, 2006Publication date: September 3, 2009Applicant: REUTER CHEMISCHER APPARATEBAU KGInventors: Milan Soukup, Karl Reuter, Florian Stolz, Viktor Meier, Jofzsef Balint, Mark Kantor
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Patent number: 7521579Abstract: The invention concerns a novel process for the preparation of 2-phenyl-2-hydroxy-N-[2-(3-alkoxy-4-hydroxyphenyl)-ethyl]-acetamides of the formula (I), wherein R1 is alkyl, R2 and R3 are each independently hydrogen or alkyl, and R4 is optionally substituted aryl or optionally substituted heteroaryl, which process comprises reacting a 2-(3-alkoxy-4-hydroxyphenyl)-ethylamine of the formula (II), wherein R1 R2 and R3 are as defined above with a ?-hydoxycarboxylic acid ester of the formula (III) or a dioxolanone of the formula (III)a, wherein R4 is as defined above, and R5, R6 and R7 independently of each other are lower alkyl. The compounds of formula (I) are important intermediates for a novel group of fungicides derived from mandelic acid amides.Type: GrantFiled: November 15, 2002Date of Patent: April 21, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: Martin Zeller, Dominik Faber, Thomas Vettiger, Clemens Lamberth
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Patent number: 7510657Abstract: The present invention is a method of preparing affinity ligands, which method comprises to provide a cyclic scaffold comprising a thiol group, a carbonyl group and an amine group; to derivatize the amine group of said scaffold with an electrophile that carries either a functionality capable of affinity interaction or a functionality capable of a second interaction with a target molecule; and to open up the derivatized scaffold and add an amine that carries either a functionality capable of a second interaction or a functionality capable of affinity interaction with a target molecule. The method provides provide affinity ligands, which are capable of affinity interaction as well as a second kind of interaction.Type: GrantFiled: March 5, 2004Date of Patent: March 31, 2009Assignee: GE Healthcare Bio-Sciences ABInventors: Jean-Luc Maloisel, Nicolas Thevenin
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Publication number: 20090069536Abstract: An amide is formed by reacting an ?-ketoacid or salt thereof in a decarboxylative condensation reaction with an amine or salt thereof comprising a nitrogen covalently bound to an atom selected from oxygen, nitrogen, and sulfur. The amide bond is formed between the ?-carbon of the ketoacid and the nitrogen of the amine. The ?-ketoacid can be formed using a novel sulfur reagent.Type: ApplicationFiled: November 10, 2008Publication date: March 12, 2009Inventors: Jeffrey W. Bode, Ryan M. Fox
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Patent number: 7462740Abstract: Disclosed is a process for making the compound of formula I: using the compounds of formulas II, Q, and XI or XII: wherein A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R represents (C1-C10)alkyl. Also disclosed are intermediate compounds that are made in the disclosed process.Type: GrantFiled: May 9, 2006Date of Patent: December 9, 2008Assignee: Schering CorporationInventors: Jianguo Yin, Xiaoyong Fu, Shuyi Zhang, Timothy L. McAllister, Agnes S. Kim-Meade, Jason L. Winters, Anantha Sudhakar, Doris P. Schumacher
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Patent number: 7329780Abstract: Provided is a method of preparing an optically pure compound having formula 1 or its salts. The method includes: reacting (R)-2-(4-methoxy-3-aminosulfonyl-phenyl)-1 -methylethylamine or its salts with a compound selected from the group consisting of chloroacetic acid, bromoacetic acid, fluoroacetic acid, iodoacetic acid, ?-halogenoacetic acid anhydride, and ?-halogenoacetyl halide in the presence of a base or an acylating agent.Type: GrantFiled: December 9, 2004Date of Patent: February 12, 2008Assignee: CJ CorporationInventors: Seong Hwan Cho, Dong Kwon Lim, Kwang Hyeg Lee, Yong Sik Youn, Choong Sil Park
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Patent number: 7291621Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals.Type: GrantFiled: January 3, 2006Date of Patent: November 6, 2007Assignee: Neurogen CorporationInventors: Yang Gao, Andrew Thrukauf, He Zhao
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Patent number: 7291615Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.Type: GrantFiled: April 29, 2004Date of Patent: November 6, 2007Assignee: Bristol-Myers Squibb CompanyInventor: Robert J. Cherney
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Patent number: 7189873Abstract: The invention relates to 4-propargyloxy-benzyl dervatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl or optionally substituted aryl; R2, R3, R5, R6, and R7 are each independently of each other hydrogen or optionally substituted alkyl; R4 is optionally substituted alkyl; X is O or N—R7; and R8 is a group R9 is optionally substituted aryl or optionally substituted heteroaryl; R10 and R11 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl; R12 is optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; R13 is hydrogen or optionally substituted alkyl, alkenyl or alkynyl; and R14 is optionally substituted alkyl or optionally substituted amino.Type: GrantFiled: October 9, 2003Date of Patent: March 13, 2007Assignee: Syngenta Corp Protection, Inc.Inventors: Clemens Lamberth, Martin Zeller
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Patent number: 7148225Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals.Type: GrantFiled: November 19, 2004Date of Patent: December 12, 2006Assignee: Neurogen CorporationInventors: Yang Gao, Alan J. Hutchinson, Wallace C. Pringle, Taeyoung Yoon, He Zhao
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Patent number: 7109371Abstract: A process for the preparation of prostaglandin compounds having the formula (I): wherein A is selected from the group consisting of C1–C6 alkyl groups; C7–C16 aralkyl groups wherein an aryl portion thereof is unsubstituted or substituted with one to three substituents selected from the group consisting of C1–C6 alkyl groups, halo and CF3; and (CH2)nOR? wherein n is an integer from 1 to 3 and R? represents a C6–C10 aryl group which is unsubstituted or substituted with one to three substituents selected from the group consisting of C1–C6 alkyl groups, halo and CF3; B is selected from OR? and NHR? wherein R? is C1–C6 alkyl groups; and represents a double bond or a single bond, is disclosed. Novel intermediates are also disclosed.Type: GrantFiled: January 5, 2004Date of Patent: September 19, 2006Assignee: Johnson Matthey Public Limited CompanyInventors: Derek Wyndham Clissold, Stuart Wilbert Craig, Rajendrakumar Reddy Gadikota, Min He, Jurjus Fayez Jurayj, Shahrokh Kazerani, Erwin Rannala, Pradeep Kumar Sharma
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Patent number: 7045139Abstract: An efficient, simple, high yielding, eco-friendly process for the manufacture of tosylates quaternary ammonium salts of cinnamidoalkylamines and/or benzamidoalkylamines (Formula I) has been described. These compounds are substantive UV-absorbers. They are useful in making fabric care products and personal care products. The scope of this methodology has been demonstrated by converting water soluble organic sunscreen quaternary halides to their corresponding tosylates of Formula VI.Type: GrantFiled: October 8, 2003Date of Patent: May 16, 2006Assignee: Galaxy Surfactants LimitedInventors: Nirmal Madhukar Koshti, Shubhangi Dattaram Naik, Bharat Bhikaji Parab, Tanaji Shamrao Jadhav, Subhash Shivling Nashte
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Patent number: 7045521Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.Type: GrantFiled: November 12, 2003Date of Patent: May 16, 2006Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Robert Cherney
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Patent number: 6921839Abstract: The present invention relates to an improved and industrially advantageous process for the preparation of N,N-dimethyl-3-(4-methyl)benzoyl propionamide of Formula I, which is a key intermediate in the synthesis of zolpidem hemitartrate, a non-benzodiazepine hypnotic agent. The process includes reacting 3-(4-methyl)-benzoyl propionic acid of Formula IV, with alkyl chloroformate or pivaloyl chloride to get a mixed anhydride of Formula V; and reacting the mixed anhydride of Formula V with dimethylamine of Formula VI to get the N,N-dimethyl-3-(4-methyl)benzoyl propionamide of Formula I.Type: GrantFiled: August 28, 2001Date of Patent: July 26, 2005Assignee: Ranbaxy Laboratories LimitedInventors: Yatendra Kumar, Mohan Prasad, Azok Nath
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Patent number: 6908934Abstract: Compounds of Formula I and the pharmaceutically acceptable salts and esters thereof, wherein Z is selected from the group consisting of: (a) Formula Ia ?and (b) Formula Ib are novel LXR agonists and are useful in the treatment of dyslipidemic conditions particularly depressed levels of HDL cholesterol.Type: GrantFiled: May 30, 2002Date of Patent: June 21, 2005Assignee: Merck & Co., Inc.Inventors: Alan D. Adams, Aileen Bouffard, James F. Dropinski, Clare E. Gutteridge, A. Brian Jones, Weiguo Lui, John George Ondeyka, Ali Shiafee, Sheo Bux Singh
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Patent number: 6891049Abstract: The method for producing N-alkoxy-N-alkylamides of general formula (I): wherein R1 represents C1-10-alkyl, cyclo-C5-7-alkyl, cyclo-C5-7-alkenyl, C2-10-alkenyl, aryl, aryl-C1-3-alkyl, heteroaryl, heteroaryl-C1-3-alkyl or heterocyclyl; and R2 represents C1-6 alkyl. In the process, an ester of general formula (II): R1COOR3, wherein R1 has the above-mentioned meaning, and R3 represents C1-6-alkyl, 4-nitrophenyl, 2,4-dinitrophenyl, succinimido or benzotriazole-1-yl, is reacted with hydroxylamine, a hydroxylamine derivative or with a hydroxylammonium salt, and the reaction product is alkylated in the presence of a phase transfer catalyst.Type: GrantFiled: January 24, 2001Date of Patent: May 10, 2005Assignee: Lonza AGInventors: Paul Hanselmann, Stefan Hildbrand, Etienne Sterren
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Patent number: 6878750Abstract: This invention describes the new benzocycloheptenes of general formula I in which R1, R2 and SK have the meanings that are indicated in the description. The new compounds have selective estrogenic activity on bones and are suitable for the production of pharmaceutical agents, especially for prophylaxis and therapy of osteoporosis.Type: GrantFiled: September 11, 2002Date of Patent: April 12, 2005Assignee: Schering AGInventors: Rolf Bohlmann, Jorg Kroll, Hermann Kuenzer, Christa Hegele-Hartung, Monika Lessl, Rosemarie Lichtner, Yukishige Nishino
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Patent number: 6821965Abstract: The invention concerns amide derivatives of the Formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl, (1-6C)alkoxy, halogeno(1-6C)alkyl, hydroxy-(1-6C)alkyl, di-[(1-6C)alklyl]amino-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, (1-6)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, amino-2(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, aryl-(1-6C)alkoxy, heteroaryl, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyl-(1-6C)alkyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseaseType: GrantFiled: February 2, 2001Date of Patent: November 23, 2004Assignee: AsterZeneca ABInventors: Dearg S Brown, George R Brown
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Publication number: 20040220424Abstract: This invention relates to a method for preparing certain acids of formula (I) via a chloroepoxy ester, which are useful as phosphodiesterase 4 inhibitors.Type: ApplicationFiled: June 2, 2004Publication date: November 4, 2004Applicant: SmithKline Beecham CorporationInventors: Ann M. Diederich, Vance J. Novack
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Publication number: 20040171880Abstract: A process for the production of an amide comprising: (a) reacting R1—CX and oxygen to form R1—COOH, wherein the reacting occurs in the liquid or vapor phase and in the presence of a first catalyst, wherein X is a group that leaves upon oxidation, and wherein R1 is phenyl, which is unsubstituted or substituted by one or more identical or different radicals selected from (C1-C12)-alkyl, (C1-C12)-alkoxy, (C1-C12)-alkanoyloxy, (C1-C12)-alkanoyl, amino, hydroxyl, —CH2—O—(C1-C12)-alkyl, —NH—(C1-C12)-alkyl, —NH—CO—(C1-C12)-alkyl, or —S—(C1-C12)-alkyl; (b) separating the R1—COOH from the mixture formed in step (a), wherein the R1—COOH is maintained in a liquid or vapor phase; and (c) reacting the R1—COOH maintained in the liquid or vapor phase from step (b) with an amine to form an amide, wherein the reacting occurs in the vapor phase and in the presence of a second catalyst.Type: ApplicationFiled: October 17, 2001Publication date: September 2, 2004Inventors: Jack S. Warren, David R. Westphal, Steve J. Zoubek
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Patent number: 6706712Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.Type: GrantFiled: December 20, 2001Date of Patent: March 16, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Robert Cherney
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Patent number: 6683211Abstract: The invention relates to phenyl-propargylether derivatives of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7, and R8 are each independently hydrogen or alkyl, R9 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl, R10 is optionally substituted aryl or optionally substituted heteroaryl, and Z is halogen, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted alkenyloxy, optionally substituted alkynyloxy, optionally substituted arylthio, optionally substituted alkylthio, optionally substituted alkenylthio; optionally substituted alkynylthio, optionally substituted alkylsulfinyl, optionally substituted alkenylsulfinyl, optionally substituted alkynylsulfinyl, optionally substituted alkylsulfonType: GrantFiled: November 15, 2002Date of Patent: January 27, 2004Assignee: Syngenta Crop Protection, Inc.Inventors: Clemens Lamberth, Martin Zeller, Walter Kunz, Fredrik Cederbaum
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Patent number: 6613340Abstract: Substantive UV absorbing organic-soluble quaternary salts of cinnamidoalkylamine are described. Hair, skin and fabric care compositions containing the compounds of formula I. wherein R1 is a substituent, selected from H, halo, —OH, —NH2, —NO2, —OCH3, —N(CH3)2, alkyl groups containing from 1 to 6 carbon atoms, alkoxy groups containing from 1 to 6 carbon atoms, alkylamino or N,N-dialkylamino groups containing from 1 to 6 carbon atoms; R2 is selected from hydrogen, alkyl group containing from 1 to 12 carbon atoms; R3 and R4 are independently selected from benzyl, alkyl group containing from 1 to 12 carbon atoms; n is an integer from 1 to 6; R5 is selected from an alkyl group containing from 8 to 22 carbon atoms; alkenyl groups containing from 8 to 22 carbon atoms; R7 is selected from bromo, chloro, nitro, methyl and ethyl groups.Type: GrantFiled: July 31, 2001Date of Patent: September 2, 2003Assignee: Galaxy Surfactants Ltd.Inventors: Nirmal Madhukar Koshti, Arun Harchandra Jawale, Bharat Bhikaji Parab, Shubhangi Dattaram Naik, Manasi Dattatraya Moghe, Tanaji Shamrao Jadhav, Subhash Shivling Nashte
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Patent number: 6603043Abstract: Process for the preparation of a Schiff base of an &agr;-alkyl-&agr;-amino acid amide and an aldehyde, wherein the corresponding &agr;-aminonitrile is contacted with a base and the aldehyde and wherein it is ensured that the reagents are in good contact. The Schiff base obtained may be further hydrolysed to form the &agr;-alkyl-&agr;-amino acid amide and the aldehyde. Preferably a substituted or unsubstituted benzaldehyde is used as the aldehyde. The reaction is preferably carried out in a practically homogeneously mixed phase obtained by using a solvent, for example methanol or ethanol. Preferably NaOH or KOH is used as the base.Type: GrantFiled: July 13, 2001Date of Patent: August 5, 2003Assignee: DSM N.V.Inventors: Dominique Monique Charles Callant, Daniel Mink, Anna Maria Cornelia Francisca Castelijns
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Patent number: 6562963Abstract: The present invention is directed to a process for the preparation of a compound of formula (X-a) or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.Type: GrantFiled: July 31, 2001Date of Patent: May 13, 2003Inventors: Roberta L. Dorow, Silvio Campagna, Pasquale N. Confalone, Fuqiang Jin, Zhe Wang
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Patent number: 6555709Abstract: Aromatic amides, their preparation process and their use as pesticides.Type: GrantFiled: October 7, 1999Date of Patent: April 29, 2003Assignee: Hoechst Schering AgrEvo S.A.Inventors: Agnés Brouillard, Jacques Demassey, Philippe Dutheil, John Weston
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Patent number: 6528230Abstract: The present invention provides a dye precursor for forming color through contact with a base and which is represented by either of the following formulas (1) and (2): wherein Ar represents an aromatic ring or a heterocyclic ring, each of which may have a substituent; Cp represents a coupler residue; L1 represents a protective group which can be eliminated by a base; and L2 represents an elimination group or a protective group which is eliminated after L1 is eliminated. Further, the present invention provides an image forming material and an image forming method, wherein the image forming material has an image forming layer on a support, the image forming layer containing at least one type of each of a photopolymerization initiator, a dye precursor which can form color through contact with a base, a base or a base precursor, and a polymerizable compound.Type: GrantFiled: January 28, 2000Date of Patent: March 4, 2003Assignee: Fuji Photo Film Co., Ltd.Inventors: Masanobu Takashima, Hiroshi Sato, Hirotaka Matsumoto, Yuuichi Fukushige
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Patent number: 6495607Abstract: Benzocycloheptenes of general formula I in which R1, R2 and Y have the meanings indicated herein, have antiestrogenic activity on and are suitable for the production of pharmaceutical agents, especially for prophylaxis and therapy of osteoporosis.Type: GrantFiled: July 19, 1999Date of Patent: December 17, 2002Assignee: Schering AGInventors: Rolf Bohlmann, Jorg Kroll, Hermann Kuenzer, Christa Hegele-Hartung, Monika Lessl, Rosemarie Lichtner, Yukishige Nishino
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Patent number: 6486347Abstract: A process for the preparation of a compound having the formula R3R4P—Ar—CO—X wherein Ar is an aryl group bearing the PR3R4 and COX groups in a 1,2-relationship, and optionally bearing also one or more non-interfering groups, R3 and R4 are each a hydrocarbon group optionally substituted by any non-interfering group, and X is OH or a non-interfering group, comprises (i) the reaction of NaPR3R4 with F—Ar—COX, or (ii) when X is an amine group, the reaction of R3R4P—Ar—COOY, OY being OH or a leaving group, with a solution of the amine obtained in situ by adding a base to a salt thereof. Certain ligands prepared by such a process are in a novel, crystalline form.Type: GrantFiled: March 29, 2001Date of Patent: November 26, 2002Assignee: Chirotech Technology, Ltd.Inventors: Ian Campbell Lennon, Ulrich Berens
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Patent number: 6472435Abstract: The invention concerns anti-tumor agents of formula (I), wherein each of R1, R2 and R3 has the meanings defined in the specification including hydrogen, (1-4C)alkyl, (3-4C)alkynyl and (1-4C)alkoxyl; each of R4 and R5 is (1-4C) alkyl; each of R6 and R7 is hydrogen or (1-4C)alkyl; X is N-(1-4C)alkylimino, N-(3-4C)alkenylimino, or (3-4C)alkynylimino; m is 1 or 2 and each R8 is as defined in the specification; each Y′ and Y2 is halogen, (1-4C)alkanesulphonyloxy, benzensulphonyloxy or phenyl-(1-4C)alkanesulfonyloxy; or a pharmaceutical acceptable salt thereof; provided that at least one of R1, R2 and R3 is other than hydrogen; a process for their preparation, pharmaceutical composition containing them and their use for producing an anti-proliferative effect in a warm-blooded animal.Type: GrantFiled: November 16, 2000Date of Patent: October 29, 2002Assignee: Astrazeneca ABInventor: Francis T Boyle
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Patent number: 6458948Abstract: A method of preparing carboxylic acid derivatives comprising mixing a quaternary ammonium salt having a particular triazine ring in the molecules thereof, a carboxylic acid compound and a compound having a nucleophilic functional group, to condense the carboxylic acid with the compound having the nucleophilic functional group. The invention further provides a condensing agent comprising the quaternary ammonium salt. The condensation is conducted under mild conditions to form carboxylic acid derivatives and, particularly, amide compounds or ester compounds maintaining high yields.Type: GrantFiled: December 11, 2000Date of Patent: October 1, 2002Assignee: Tokuyama CorporationInventors: Fumiaki Iwasaki, Shohei Tani, Munetaka Kunishima, Keiji Terao, Michiko Miharu, Naoki Hirano, Masako Saijyo
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Patent number: 6441235Abstract: A process for preparing 5-amino-N,N′-bis(R)isophthalamides, where A is 2,3-dihydroxypropyl or 1,3-dihydroxyisopropyl, useful as intermediates in preparing iodinated diagnostic agents, which comprises reacting a di-lower-alkyl 5-nitroisophthalate with a compound of the formula RNH2 in the presence of a basic catalyst and without isolating the intermediate 5-nitro-N,N′-bis(R)isophthalamide, catalytically hydrogenating the latter.Type: GrantFiled: May 14, 2001Date of Patent: August 27, 2002Assignee: Amersha, Health ASInventors: Edward David Parady, Karl Olaf Gelotte
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Publication number: 20020068838Abstract: Compounds of formula (I) in which a, b, c, 1Type: ApplicationFiled: December 28, 1999Publication date: June 6, 2002Inventors: JACQUES DEMASSEY, ROBERT PEEK, ANTONIO UGOLINI, JOHN WESTON
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Publication number: 20020068765Abstract: This invention describes the new benzocycloheptenes of general formula I 1Type: ApplicationFiled: July 19, 1999Publication date: June 6, 2002Inventors: ROLF BOHLMANN, JORG KROLL, HERMANN KUENZER, CHRISTA HEGELE-HARTUNG, MONIKA LESSL, ROSEMARIE LICHTNER, YUKISHIGE NISHINO
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Patent number: 6384278Abstract: The present invention provides an inexpensive one-step method for preparing an aromatic carboxamide, such as a phenyl substituted carboxamide) by reacting an aromatic amine (e.g. a phenylamine) and a carboxylic acid (e.g. an alkanoic acid or ester thereof) in the presence of a boron containing compound (e.g. boronic acid or boric acid) and, optionally, a chelating agent (e.g. a 2-pyridinylamine).Type: GrantFiled: February 5, 2001Date of Patent: May 7, 2002Assignee: Emisphere Technologies, Inc.Inventors: Pingwah Tang, Feng Ye
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Patent number: 6319925Abstract: Oxime ethers of formula (I) in which a) X is an N atom and Y is an oxygen atom or NH, or b) X is CH and Y is an oxygen atom, in which furthermore R1 is C1-C4alkyl; R2 is hydrogen, C1-C4alkyl or cyclopropyl; and in which R3 and R4 are as defined herein, are fungicidal, acaricidal and insecticidal active ingredients for agriculture. They can be employed as formulated crop protection compositions.Type: GrantFiled: December 22, 1997Date of Patent: November 20, 2001Assignee: Bayer AktiengesellschaftInventor: Hugo Ziegler
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Patent number: 6265611Abstract: The present invention relates to hydroxymandelic acid amides of phenolic amines which can be used as antioxidants or as free-radical scavengers, particularly in the cosmetic or dermatological field, in foods and in cosmetic and dermatological compositions.Type: GrantFiled: February 10, 2000Date of Patent: July 24, 2001Assignee: Haarmann & Reimer GmbHInventor: Jakob Peter Ley
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Patent number: 6207861Abstract: The present invention provides a method for producing a mass-coded combinatorial library comprising a set of compounds having the general formula X(Y)n, where X is a scaffold, each Y is, independently, a peripheral moiety, and n is an integer greater than 1. The method comprises selecting a peripheral moiety precursor subset from a peripheral moiety precursor set. The subset includes a sufficient number of peripheral moiety precursors that at least about 50 distinct combinations of n peripheral moieties derived from the peripheral moiety precursors in the subset exist. The subset of peripheral moiety precursors is selected so that at least about 90% of all possible combinations of n peripheral moieties derived from the subset have a molecular mass sum which is distinct from the molecular mass sums of all of the other combinations of n peripheral moieties. The method further comprises contacting the peripheral moiety precursor subset with a scaffold precursor which has n reactive groups.Type: GrantFiled: February 17, 1998Date of Patent: March 27, 2001Assignee: NeoGenesis, Inc.Inventors: Huw M. Nash, Seth Birnbaum, Edward A. Wintner, Krishna Kalghatgi, Gerald Shipps, Satish Jindal
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Patent number: 6130312Abstract: A process for producing an aromatic polyamide which comprises:(a) a dicarboxylic acid component which consists of 30-100 mol % of terephthalic acid and optionally 0-70 mol % of at least one dicarboxylic acid other than terephthalic acid, and(b) a diamine component which consists of 50-100 mol % of an aliphatic alkylenediamine of 4-25 carbons and optionally 0-50 mol % of at least one alicyclic diamine of 3-25 carbons, said process comprising a first step of performing melt reaction of said dicarboxylic acid with said diamine, thereby giving a low molecular weight condensate having an intrinsic viscosity [.eta.] of 0.05-0.6 dl/g, a second step of subjecting it to solid phase polymerization, thereby giving an aromatic polyamide precursor having an intrinsic viscosity [.eta.] of 0.5-1.0 dl/g, and a third step of subjecting it to melt polymerization, thereby giving an aromatic polyamide having a desired intrinsic viscosity [.eta.] of 0.8-2.5 dl/g.Type: GrantFiled: November 12, 1997Date of Patent: October 10, 2000Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Hidetatsu Murakami, Satoshi Omori, Kenji Wakatsuru
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Patent number: 6130315Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.Type: GrantFiled: August 24, 1998Date of Patent: October 10, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: H. Michael Kolb, Joseph P. Burkhart, Michael J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin
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Patent number: 6124502Abstract: This invention relates to matrix metalloproteinase (MMP) inhibiting compounds of the formula: ##STR1## where R.sup.1 is C.sub.1 -C.sub.12 alkyl, straight or branched and optionally substituted by halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, carboxamido, nitrile, mono- or di-(C.sub.1 -C.sub.6)alkylamino, thio, C.sub.1 -C.sub.6 alkylthio, aryl, --Oaryl or --OCH.sub.2 aryl where aryl is optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, carboxy, halogen, cyano, nitro, carboxamido, or hydroxy; and C.sub.1 -C.sub.6 alkanesulfonyloxy. R.sup.2 is .alpha.-OH or .beta.-OH and R.sup.6 is H or R.sup.2 and R.sup.6 together are carbonyl; the chemical intermediates; and processes for the preparation of these compounds and the intermediates thereto.Matrix metalloproteinases (MMP) are a family of zinc-containing calcium dependent proteinases, including stromelysins, collagenases, and gelatinases.Type: GrantFiled: October 9, 1998Date of Patent: September 26, 2000Assignee: American Cyanamid CompanyInventor: Jeremy Ian Levin
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Patent number: 6121326Abstract: Compounds which are useful as a tachykinin antagonist are substituted alkyltetraamine derivatives which are represented by the following formula (I) or a pharmaceutically acceptable salt, a complex compound or a solvate thereof. ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each is a phenyl group which may be substituted with one or more hydroxyl, lower alkoxy and/or acyloxy group(s). The compounds are useful as an anti-inflammatory agent, anti-allergic agent, analgesic, antiemetic, agent for irritable colon syndrome, agent for dermal disease, agent for vasospastic disease, agent for cerebral ischemic disease, antidepressant, antianxiety agent, agent for autoimmune disease, antispasmodic, and as a muscle relaxant, etc.Type: GrantFiled: January 5, 2000Date of Patent: September 19, 2000Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Atsushi Yamamoto, Ko Nakamura, Masanori Otsuka
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Patent number: 6117365Abstract: The invention relates to specific phenolic acid amides of hydroxy-substituted benzylamines of the formula I ##STR1## to a process for their preparation and to their use as antioxidants or as free-radical scavengers, in particular in the cosmetic or dermatological field, in foods and cosmetic and dermatological compositions comprising these phenolic acid amides.Type: GrantFiled: August 27, 1998Date of Patent: September 12, 2000Assignee: Haarmann & Reimer GmbHInventor: Jakob Ley
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Patent number: 6107498Abstract: Methods for producing carboxylic amides involves combining near-stoichiometric amounts of carboxylic acid and amine in a reaction vessel and reacting under pressures greater than atmospheric pressure. Alternatively, an excess of amine is reacted with carboxylic acid at atmospheric pressure to produce a carboxylic amide.Type: GrantFiled: April 22, 1997Date of Patent: August 22, 2000Assignee: AKZO Nobel N.V.Inventors: Bernard Maisonneuve, Dale Steichen, Ralph Franklin, Kornelis Overkempe
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Patent number: 6057322Abstract: Compounds of the formula I ##STR1## and the pharmaceutically tolerated salts thereof, are described. A process for their preparation and their use as medicaments in cardiovascular diseases are also described.Type: GrantFiled: July 30, 1997Date of Patent: May 2, 2000Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus