Aralkyl Bonded Directly To Urea Nitrogen Patents (Class 564/56)
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Patent number: 6723875Abstract: The present invention relates to the preparation of alkyl-ureas, starting from O,S-dimethyl dithiocarbonate, which provides the following steps: A) causing the O,S-dimethyl dithiocarbonate to react with a primary amine of general formula R1NH2 in order to obtain an O-methyl thiocarbamate; B) isomerising the O-methyl thiocarbamate in order to obtain an S-methyl thiocarbamate; C) causing the S-methyl thiocarbamate with a compound of general formula R′R″NH, wherein R′ and R″ may be equal or different one in respect of the other and of R1 and may be H, R2 or R3, in order to obtain one of the alkyl-ureas of formula (4), (5) or (6).Type: GrantFiled: February 6, 2003Date of Patent: April 20, 2004Assignee: Oxon Italia S.p.A.Inventors: Edoardo Pallucca, Jacopo Degani, Anna Maria Serri, Rita Fochi, Sonia Gazzetto, Claudia Fenoglio, Claudio Ornati, Mara Migliaccio, Silvano Cadamuro, Gianni Carvoli
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Patent number: 6683200Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.Type: GrantFiled: October 4, 2001Date of Patent: January 27, 2004Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Hiroshi Suhara
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Patent number: 6635650Abstract: The invention relates to compounds of formula (I): A-G1-Cy-G2-Cy-G3-B (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: August 8, 2001Date of Patent: October 21, 2003Assignee: Les Laboratoires ServierInventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
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Patent number: 6620961Abstract: Biarylalkylenecarbamic acid derivative represented by general formula (I): [wherein Q is a phenyl group which may be substituted or the like, X is a halogen atom, a (C1-C6) alkyl group or the like, n is 0 or an integer of from 1 to 4, R1 is a (C1-C6) alkyl group or the like, R2 is a hydrogen atom, a (C1-C6) alkyl group or the like, A is a (C1-C7) alkylene group which may be branched, and G is an oxygen atom, a sulfur atom or a group —NR— (wherein R3 is a hydrogen atom or a (C1-C4) alkyl group)] and agricultural and horticultural fungicides. The agricultural and horticultural fungicides of the present invention are useful as agricultural and horticultural fungicides because they have high preventive effects on cucumber downy mildew, apple scab, wheat powdery mildew, rice blast, cucumber gray mold and rice sheath blight without damaging crops, and are excellent in residual effectiveness and rain-resistance.Type: GrantFiled: February 25, 2000Date of Patent: September 16, 2003Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co. Ltd.Inventors: Kazuhiro Ikegaya, Masami Ozaki, Takahiro Kawashima, Ichiro Miura, Norimichi Muramatsu
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Patent number: 6528543Abstract: Glucokinase activating compounds of the formula wherein R1 and R2 are independently hydrogen, halo, amino, nitro, cyano, sulfonamido, lower alkyl, perfluoro-lower alkyl, lower alkyl thio, perfluoro-lower alkyl thio, lower alkyl sulfonyl, or perfluoro-lower alkyl sulfonyl; R3 is cycloalkyl having from 3 to 7 carbon atoms or lower alkyl having from 2 to 4 carbon atoms; R4 is hydrogen, lower alkyl, lower alkenyl, hydroxy lower alkyl, halo lower alkyl, R5 and R6 are hydrogen or lower alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereofType: GrantFiled: March 21, 2000Date of Patent: March 4, 2003Assignee: Hoffman-La Roche Inc.Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Antonio Focella, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Patent number: 6423870Abstract: The invention concerns compounds of formula (I) in which: A forms a tricyclic system of formula A1, A2, A3 or A4; R1 represents a hydrogen atom, an alkyl, hydroxy, alkoxy or oxo group; (R2)m and (R3)m′ are such as defined in the description; n represents an integer such that 0≦n≦3; p represents an integer such as defined in the description; B represents a group (a) or (b). The invention is useful for preparing medicines.Type: GrantFiled: July 14, 2000Date of Patent: July 23, 2002Assignee: Les Laboratoires ServierInventors: Michel Langlois, Monique Mathe-Allainmat, Carole Jellimann, Jean Andrieux, Caroline Bennejean, Pierre Renard, Philippe Delagrange
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Patent number: 6329529Abstract: Disclosed are a fluorinating agent represented by the general formula (1): wherein R1 to R4 are a substituted or unsubstituted, saturated or unsaturated alkyl group or a substituted or unsubstituted aryl group, and can be the same or different; R1 and R2 or R3 and R4 can bond to form a ring including a nitrogen atom or a nitrogen atom and other hetero atoms; or R1 and R3 can bond to form a ring including a nitrogen atom or a nitrogen atom and other hetero atoms, for example: a preparation process of the fluorinating agent and a process for preparing fluorine compounds by reacting various compounds with the fluorinating agent. The invention has also disclosed that the fluorinating agent is very effective for fluorinating oxygen containing functional compounds.Type: GrantFiled: July 31, 1998Date of Patent: December 11, 2001Assignee: Mitsui Chemicals, Inc.Inventors: Hiroshi Sonoda, Kazunari Okada, Akira Takahashi, Kouki Fukumura, Hidetoshi Hayashi, Teruyuki Nagata, Yasuhiro Takano
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Patent number: 6319930Abstract: The invention relates to compounds of formula (I): A—G1—Cy—G2—Cy—G3—B (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure and G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: March 24, 2000Date of Patent: November 20, 2001Assignee: Adir et CompagnieInventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
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Patent number: 6316616Abstract: The present invention provides methods and compositions, i.e. synthetic libraries of candidate compounds, useful in the discovery and optimization of compounds which catalyze at least one chemical transformation. In certain instances, the subject compounds catalyze a chemoselective, regioselective, stereoselective or enantioselective transformation.Type: GrantFiled: April 22, 1998Date of Patent: November 13, 2001Assignee: President and Fellows of Harvard CollegeInventors: Eric N. Jacobsen, Matthew S. Sigman
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Patent number: 6313071Abstract: A phenylacetylene derivative represented by the formula [I]: {wherein X is a halogen atom, a C1-C6 alkyl group, a C2-C6 alkoxy group, a C2-C6 haloalkyl group, etc., n is 0 or an integer of from 1 to 4, R1 is a C1-C6 alkyl group, R2 is a hydrogen atom, a C1-C6 alkyl group, a C2-C6 alkynyl group, a C2-C6 alkynyl group, a C1-C6 alkoxy group, etc., A is a C1-C6 alkylene group which may be branched, G is an oxygen atom, a sulfur atom or a —NR3— group; R3 is a hydrogen atom or a C1-C6 alkyl group, and Y is a hydrogen atom, a C1-C10 alkyl group, said group may be substituted by a halogen atom, a hydroxyl group or a C1-C6 alkoxy group], a C2-C6 alkenyl group, etc.; and an agricultural/horticultural fungicide containing the same as the active ingredient.Type: GrantFiled: December 4, 2000Date of Patent: November 6, 2001Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Kazuhiro Ikegaya, Shunichiro Fukumoto, Masami Ozaki, Takahiro Kawashima, Haruchika Sekido, Norimichi Muramatsu
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Patent number: 6310074Abstract: The invention relates to compound of formula (I): A—G1—Cy—G2—Cy′—G3—B (I) wherein: A represents a grouping NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents a grouping NR1C(Q)R2, NR1C(Q)NR2R3, C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy and Cy′, which are different, represent a ring structure or G2 represents a chain and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: May 18, 2000Date of Patent: October 30, 2001Assignee: Adir et CompagnieInventors: Patrick Depreux, Said Yous, Gwenael Cheve, Gérald Guillaumet, Marie-Claude Viaud, Carlos Larraya, Caroline Bennejean, Philippe Delagrange, Pierre Renard, Carole Descamps-Francois
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Patent number: 6235789Abstract: A compound of the formula wherein R1 and R2 are H, a hydrocarbon group or a heterocyclic group, or R1 and R2 are combinedly a spiro ring; R3 is a hydrocarbon group, a substituted amino group, a substituted hydroxyl group or a heterocyclic group; R4 is H or alkyl; ring A is a substituted benzene ring; m and n denote 1 to 4; {overscore (.........)} means a single or double bond or a salt, a process of producing thereof and a composition having a binding affinity for melatonin receptor.Type: GrantFiled: May 28, 1997Date of Patent: May 22, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Osamu Uchikawa, Masaomi Miyamoto
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Patent number: 6184410Abstract: Carbodiimides based on 1,3-bis(1-methyl-1-isocyanatoethyl)benzene contain from 12 to 40% by weight of ethylene oxide units [—CH2—CH2—O—], based on the weight of the carbodiimides.Type: GrantFiled: April 22, 1999Date of Patent: February 6, 2001Assignee: BASF AktiengesellschaftInventors: Heinz Bollmann, Karl Häberle, Nicolas Kokel, Raina Thärigen
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Patent number: 6152968Abstract: The use of water-soluble quinacridones of the formula I ##STR1## where M.sup..sym. is a lithium, sodium, potassium or ammonium cation,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently are hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, sulfamoyl, mono- or di-(C.sub.1 -C.sub.4)-alkylsulfamoyl, carbamoyl, mono- or di-(C.sub.1 -C.sub.4)-alkylcarbamoyl, unsubstituted or substituted mono- or diphenylsulfamoyl, unsubstituted or substituted mono- or diphenylcarbamoyl, halogen, nitro or cyano,n is 0, 1 or 2 andm is 0, 1 or 2 and the sum n+m is at least 1,for dyeing and printing natural and synthetic fiber material.Type: GrantFiled: September 17, 1999Date of Patent: November 28, 2000Assignee: BASF AktiengesellschaftInventors: Karl-Heinz Etzbach, Carolin Kranz, Rudiger Sens
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Patent number: 6140531Abstract: Describes a method of producing N-1-alkenyl carbonylamino compounds represented by the following general formula I, ##STR1## wherein R.sub.1 is the residue of an active hydrogen functional material, n is a number from 1 to a number equal to the number of active hydrogen groups of said active hydrogen functional material, X is selected from O, S and N(R.sub.5), R.sub.5 being hydrogen, hydrocarbyl, or R.sub.5 and R.sub.1 may together form a cyclic ring, R.sub.2, R.sub.3 and R.sub.4 are each independently selected from hydrogen, C.sub.1 -C.sub.4 alkyl and C.sub.2 -C.sub.4 alkenyl.Type: GrantFiled: March 29, 1999Date of Patent: October 31, 2000Assignee: PPG Industries Ohio, Inc.Inventors: Cheruthur Govindan, John M. Pascone
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Patent number: 6140368Abstract: The present invention relates to a novel class of compounds that are potent inhibitors of HIV reverse transcriptase and HIV integrase. In addition to being multienzyme inhibitors, the inventive compounds of the present invention are remarkable in at least two other respects. First, they do not appear to be toxic to cells at typical therapeutic concentrations. Second, they appear to be equally effective against mutant strains of HIV reverse transcriptase commonly found in patients who have developed resistance to current reverse transcriptase inhibitors. Because the inventive compounds show promise in combatting viral resistance and are potent inhibitors of both HIV reverse transcriptase and integrase, they are ideal candidates for use in combination with existing therapies or alone in treating AIDS or HIV infection.Type: GrantFiled: May 4, 1998Date of Patent: October 31, 2000Assignees: The Regents of the University of California, Rutgers, The University of New JerseyInventors: George L. Kenyon, Margaret Stauber, Karl Maurer, Dolan Eargle, Angelika Muscate, Andrew Leavitt, Diana C. Roe, Todd J. A. Ewing, Allan G. Skillman, Jr., Edward Arnold, Irwin D. Kuntz, Malin Young
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Patent number: 6127414Abstract: There is provided pharmaceutically useful compounds of formula I, ##STR1## wherein Ar.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have meanings given in the description, which are useful as antagonists of neuropeptide Y and in particular in the treatment of cardiovascular diseases, for example vasoconstriction.Type: GrantFiled: October 26, 1998Date of Patent: October 3, 2000Assignee: Astra AktiebolagInventors: Nils-.ANG.ke Bergman, Thomas D'Ambra, Garry M Pilling
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Patent number: 6114390Abstract: NPY-antagonistic compounds of the formula ##STR1## Exemplary are: (A) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -bis(4-hydroxyphenyl)acetyl]-argininamide-trifluoracetate;(B) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -[bis(4-chlorphenyl)acetyl]-argininamide-trifluoracetate;(C) (R)-N-[[4-Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -(diphenylacetyl)-argininamide-trifluoracetate;(D) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethoxycarbonylmethylamino-carbonylaminomethyl)phe nyl]methyl]-argininamide-trifluoroacetate;(E) (R,S)-N.sup.5 -(Aminoiminomethyl)-N.sup.2 -(diphenylacetyl)-N-[(4-hy-droxyphenyl)methyl]-N.sup.5 -methyl-ornithinamide-hydrochloride;(F) (R)-N-[[4-(Aminocarbonylmethyl)phenyl]methyl]-N.sup.2 -(diphenyl-acetyl)-argininamide-diacetate;(G) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethylaminocarbonylamino-methyl)-phenyl]methyl]-ar gininamide-bis-(trifluoroacetate); and,(H) (R)-N.sup.Type: GrantFiled: October 14, 1997Date of Patent: September 5, 2000Assignee: Karl Thomae GmbHInventors: Wolfhard Engel, Wolfgang Eberlein, Klaus Rudolf, Henri Doods, Heike-Andrea Wieland, Klaus-Dieter Willim, Michael Entzeroth, Wolfgang Wienen
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Patent number: 6080874Abstract: The present invention provides a simple, 1-step process for preparing a N-(aryl or heteroaryl)-hydroxyurea comprising reacting the corresponding alcohol, ester or ether with hydroxyurea and acid. This reaction is particularly useful for preparing a benzo[b]thienyl substituted N-hydroxyurea of formula: ##STR1## from compound 1: ##STR2## by reacting compound 1 with hydroxyurea and acid. R.sup.1 is selected from the group consisting of hydrogen, 1-6 carbon alkyl, 1-6 carbon alkoxy, and halogen; R.sup.2 is an 1-4 carbon alkyl; and R.sup.3 is selected from the group consisting of hydrogen, acyl, methyl, ethyl and mixtures thereof. Additional steps to isolate the pure bulk product follow.Type: GrantFiled: September 25, 1998Date of Patent: June 27, 2000Assignee: Abbott LaboratoriesInventors: John E. Hengeveld, Elise H. Leese, Brian S. Moon, Dennis M. Abad, Kimberly A. Allen, Philip E. Bauer, David B. Murphey, Brian T. Fohey, Richard R. Copp, Jr., Greg S. Lannoye, Rodney M. Mittag
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Patent number: 6022899Abstract: There are described compounds of the formula I ##STR1## in which the substituents R(1) to R(7) and X have the meanings shown in the claims, and their pharmaceutically tolerable salts. These are effective inhibitors of the cellular sodium proton antiporter (Na.sup.+ /H.sup.+ exchanger). They are therefore outstandingly suitable for the treatment of all diseases which can be attributed to increased Na.sup.+ /H.sup.+ exchange.Type: GrantFiled: January 9, 1998Date of Patent: February 8, 2000Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans-Jochen Lang, Udo Albus, Wolfgang Scholz
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Patent number: 5962530Abstract: The invention relates to new amino acid derivatives of general formula ##STR1## wherein R, U, V, Y, n, m and R.sup.1 to R.sup.3 are defined as in claim 1, their tautomers, diastereomers, enantiomers, mixtures thereof and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly selective NPY-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.Type: GrantFiled: May 29, 1998Date of Patent: October 5, 1999Assignee: Dr. Karl Thomae GmbHInventors: Wolfhard Engel, Wolfgang Eberlein, Klaus Rudolf, Henri Doods, Heike-Andrea Wieland, Klaus-Dieter Willim
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Patent number: 5932595Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.Type: GrantFiled: December 18, 1996Date of Patent: August 3, 1999Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.Inventors: Steven Lee Bender, Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Lawrence Emerson Fisher, Robert Than Hendricks, Keshab Sarma
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Patent number: 5925762Type: GrantFiled: September 15, 1997Date of Patent: July 20, 1999Assignee: Boehringer Ingelheim (Canada) Ltd.Inventor: Bounkham Thavonekham
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Patent number: 5922771Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.Type: GrantFiled: August 19, 1996Date of Patent: July 13, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
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Patent number: 5892100Abstract: The present invention provides a method for producing N-acyl carbamate in high yield. The method of the present invention comprises the step of reacting an unsaturated acid halide with a carbamate in the presence of a hindered amine. Another method of the present invention comprises the step of reacting a N,N-diacyl carbamate with an active hydrogen compound.Type: GrantFiled: September 9, 1997Date of Patent: April 6, 1999Assignee: Nippon Paint Co., Ltd.Inventors: Eiji Yamanaka, Masami Yabuta, Satoshi Urano
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Patent number: 5849732Abstract: Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R.sup.0 represents H, alkyl or alkyloxy; R.sup.1 represents alkyl; R.sup.2 represents alkyl or alkyloxy; OR.sup.3 represents OH; R.sup.4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR.sup.7 ; where R.sup.7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): ##STR2## represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.Type: GrantFiled: February 14, 1997Date of Patent: December 15, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Toshikazu Suzuki, Hiroshi Ohmizu, Yoshimasa Hashimura, Hitoshi Kubota, Keiko Tanaka
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Patent number: 5811456Abstract: Novel monoamine oxidase B inhibitors of formula (I), wherein R.sub.1 .dbd.H, an optionally substituted benzyloxy or phenylethoxy group; p=0-3; R.sub.3 .dbd.H, a CN, OH, CCH group, a C.sub.1 -C.sub.3 alkoxy-carbonyl group, or a C.sub.1 -C.sub.3 alkylated cyanomethyl group; R.sub.2 .dbd.H or a C.sub.1 -C.sub.3 alkyl group; n=0 or 1; if n=0, R.sub.4 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3 alkoxy group, while if n=1, y=1 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group, a C.sub.1 -C.sub.3 alkoxy group or a phenyl group. The invention also concerns processes for the preparation of said novel inhibitors and the therapeutic use thereof.Type: GrantFiled: August 6, 1996Date of Patent: September 22, 1998Assignees: Laboratoires Mayoly Spindler, Michel SemanInventors: Michel Seman, Suzanne Bernard, Rene Milcent, Catherine Paillat
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Patent number: 5807875Abstract: Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R,S)-N.sup.2 -(diphenylacetyl)-N-?(4-hydroxyphenyl)methyl!-N.sup.5 -(1H-imidazol-2-yl)-ornithinamide.Type: GrantFiled: December 11, 1996Date of Patent: September 15, 1998Assignee: Dr. Karl Thomae GmbHInventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Henri Doods, Heike Andrea Wieland, Klaus-Dieter Willim, Jurgen Krause, Horst Dollinger, Franz Esser, Gerd Schnorrenberg, Michael Entzeroth, Wolfgang Wienen
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Patent number: 5780512Abstract: The invention relates to a compounds selected from these of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and A are as defined in the description, and a medicinal product containing the same useful for treating a melatoninergic disorder.Type: GrantFiled: March 26, 1997Date of Patent: July 14, 1998Assignee: Adir et CompagnieInventors: Daniel Lesieur, Eric Fourmaintraux, Patrick Depreux, Philippe Delagrange, Pierre Renard, Beatrice Guardiola-Lemaitre
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Patent number: 5760071Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, R.sub.1, R'.sub.1, R.sub.2, R.sub.3 and n are as defined in the description, and medicinal product containing the same useful for treating a mammal afflicted with a disorder of the melatoninergic system.Type: GrantFiled: March 10, 1997Date of Patent: June 2, 1998Assignee: Adir et CompagnieInventors: Daniel Lesieur, Veronique Leclerc, Patrick Depreux, Philippe Delagrange, Pierre Renard
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Patent number: 5714633Abstract: The present invention provides a process for the preparation of a compound of formula ##STR1## wherein R is a straight or branched alkyl group of from one to twelve carbon atoms; M represents hydrogen or a pharmaceutically acceptable cation; and A is selected from optionally substituted carbocyclic phenyl.Type: GrantFiled: August 16, 1996Date of Patent: February 3, 1998Assignee: Abbott LaboratoriesInventors: Sanjay R. Chemburkar, Hemantkumar H. Patel, David P. Sawick, Albert V. Thomas
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Patent number: 5712312Abstract: The invention relates to a compound selected from these of formula (I): ##STR1## in which R.sub.7, R.sub.8, Y, n and A are as defined in the description, and medicinal product containing the same useful for treating a disorder of the melatoninergic system.Type: GrantFiled: April 12, 1996Date of Patent: January 27, 1998Assignee: Adir et CompagnieInventors: Michel Langlois, Monique Mathe-Allainmat, Philippe Delagrange, Pierre Renard, Beatrice Guardiola
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Patent number: 5703076Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: December 30, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, Ko-Chung Lin, Gary A. DeCrescenzo, Donald J. Rogier, Jr., John N. Freskos
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Patent number: 5688875Abstract: A hydrophilic tetramethylxylylenecarbodiimide represented by the following formula (1): ##STR1## wherein n is an average polymerization degree and is an integer of 1 to 30; R.sub.1 is a residue of an organic compound having a hydrophilic segment and at least one functional group reactive with an isocyanate group; and X is a group formed by the reaction of the functional group with the isocyanate group. The carbodiimide is free from the problems of the prior art, has good storage stability and accordingly is usable as an easy-to-handle crosslinking agent for hydrophilic resin.Type: GrantFiled: May 31, 1995Date of Patent: November 18, 1997Assignee: Nisshinbo Industries, Inc.Inventors: Eiji Sasaki, Yasuo Imashiro, Ikuo Takahashi, Naofumi Horie
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Patent number: 5681858Abstract: The present invention provides a novel N-hydroxyurea compound of chemical formula (I) wherein R.sup.1 and R.sup.2 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl; Ar is phenyl or mono-, di- or trisubstituted phenyl; A is a valence bond or a C.sub.1 -C.sub.6 alkylene chain, optionally having one double bond or one triple bond in the chain, and optionally having one or more C.sub.1 -C.sub.4 alkyl groups attached to the chain: X is oxygen or sulfur, n is an integer of 3 to 6; M is hydrogen, pharmaceutically acceptable cation or a metabolically cleavable group: and X and A may be attached at any available position on the ring. These compounds are useful for treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.Type: GrantFiled: October 3, 1995Date of Patent: October 28, 1997Assignee: Pfizer Inc.Inventors: Rodney William Stevens, Takashi Mano, Yoshiyuki Okumura, Masami Nakane
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Patent number: 5668180Abstract: A compound selected from those of formula (I): ##STR1## in which A, R, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined in the description,and a medicinal product containing the same useful for treating a disorder of the melatoninergic system.Type: GrantFiled: May 30, 1996Date of Patent: September 16, 1997Assignee: Adir Et CompagnieInventors: Daniel Lesieur, Patrick Depreux, Veronique Leclerc, Philippe Delagrange, Pierre Renard
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Patent number: 5661186Abstract: Certain tetralinyl- and indanyl-ethylamides are useful central nervous system agents.Type: GrantFiled: December 21, 1995Date of Patent: August 26, 1997Assignee: Bristol-Myers Squibb Co.Inventors: Katherine S. Takaki, Brett T. Watson, Graham S. Poindexter, James R. Epperson
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Patent number: 5661185Abstract: New melatonergic agents are phenyl alkanyl or phenyl alkyl substituted carboxamides and ureas of Formula I: ##STR1## wherein: R.sub.1 =C.sub.1-3 alkyl, allyl, C.sub.3-6 cycloalkyl substituted C.sub.1-4 alkyl;R.sub.2 =hydrogen, halogen or C.sub.1-4 alkoxy;R.sub.3 =hydrogen or C.sub.1-4 alkyl;R.sub.4 =C.sub.1-4 alkyl, C.sub.1-4 alkyl substituted amino, carboxylic acid substitutedC.sub.1-4 alkyl or C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl, or straight or branched chainC.sub.2-4 alkenyl;A=a linear C.sub.2-4 alkanediyl or alkenediyl chain, provided that A not be --CH.sub.2 CH.sub.2 -- when X is a bond; andX=a covalent bond or oxygen.Type: GrantFiled: December 14, 1995Date of Patent: August 26, 1997Assignee: Bristol-Myers Squibb Co.Inventors: Katherine S. Takaki, George N. Karageorge, Daniel J. Keavy, Michael F. Parker, Brett T. Watson
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Patent number: 5637769Abstract: The present invention provides: a urea-modified carbodiimide represented by the following general formula ##STR1## (wherein each R is a C.sub.1 -C.sub.12 alkyl group or a C.sub.3 -C.sub.10 cycloalkyl group; each Z is a C.sub.1 -C.sub.12 alkylene group, a C.sub.3 -C.sub.10 cycloalkylene group, a C.sub.4 -C.sub.16 alkylene group having a cyclic or non-cyclic structure, or a C.sub.8 -C.sub.16 alkylene group having an aromatic ring; n is an integer of 1-50; and each m is an integer of 1 or 2), and a process for producing the above urea-modified carbodiimide, which comprises (1) reacting an organic aliphatic diisocyanate represented by the following general formulaO.dbd.C.dbd.N--Z--N.dbd.C.dbd.Type: GrantFiled: June 27, 1995Date of Patent: June 10, 1997Assignee: Nisshinbo Industries, Inc.Inventors: Yasuo Imashiro, Ikuo Takahashi, Naofumi Horie, Takeshi Yamane
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Patent number: 5620977Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: April 15, 1997Assignee: G.D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
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Patent number: 5616620Abstract: Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R)-N2-(diphenylacetyl)-N-[(4-hydroxyphenyl) methyl]-argininamide-acetate.Type: GrantFiled: June 1, 1995Date of Patent: April 1, 1997Assignee: Karl Thomae GmbHInventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Henri Doods, Heike A. Wieland, Klaus-Dieter Willim, Jurgen Krause, Horst Dollinger, Franz Esser, Gerd Schnorrenberg, Michael Entzeroth, Wolfgang Wienen
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Patent number: 5614522Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: July 24, 1995Date of Patent: March 25, 1997Assignee: G.D. Searle & Co.Inventors: John J. Talley, Kathryn L. Reed
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Patent number: 5610190Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV Protease.Type: GrantFiled: June 7, 1995Date of Patent: March 11, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Ko-Chung Lin, Michael L. Vazquez, Richard A. Mueller, Kathryn L. Reed, Robert M. Heintz, Michael Clare, John N. Freskos, Eric T. Sun
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Patent number: 5606096Abstract: The present invention provides a process for producing a variety of unsaturated carbamic acid derivatives from corresponding unsaturated carbamates by substitution reaction. The present invention provides a process for producing unsaturated carbamic acid derivatives, comprising reacting an unsaturated carbamate represented by ##STR1## wherein R represents a hydrogen atom or an alkyl group having 1 to 8 carbon atoms, R.sup.1 represents a residue of an alcohol from which an OH group is removed,with an alcohol, a primary or secondary amine or an oxime at a temperature of 80.degree. to 150.degree. C. to substitute the --OR.sup.1 group in the formula (A).Type: GrantFiled: April 3, 1995Date of Patent: February 25, 1997Assignee: Nippon Paint Co., Ltd.Inventors: Eiji Yamanaka, Noriyuki Tsuboniwa, Takao Morimoto, Masamichi Furukawa, Satoshi Urano
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Patent number: 5597942Abstract: Novel carbodiimides and/or oligomeric polycarbodiimides containing terminal isocyanate, urethane and/or urea groups are obtainable, for example, by condensation of 1,3-bis(1-methyl-1-isocyanatoethyl)benzene with elimination of carbon dioxide followed, if desired, by reaction of all or some of the free isocyanate groups of the resultant (poly)carbodiimides with aliphatic, cycloaliphatic or araliphatic amines, alcohols and/or alkoxypolyoxyalkylene alcohols, and are used as stabilizers against hydrolytic degradation of polyaddition and polycondensation products containing ester groups.Type: GrantFiled: January 30, 1996Date of Patent: January 28, 1997Assignee: BASF AktiengesellschaftInventors: Siegmund Pohl, Friedhelm Lehrich, Manfred Genz, Bernd Bruchmann, Helmut Tesch, Roland Minges, Joachim Streu
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Patent number: 5545640Abstract: Disclosed herein are compounds which inhibit human immunodeficiency virus (HIV) protease activity and inhibit HIV replication in human cells. Thus, the compounds are indicated for the treatment of HIV infections. The compounds can be represented by the formula ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an arylalkyl carbamoyl; A is absent or an amino acid or a derived amino acid; either R.sup.1 or R.sup.2 is hydrogen while the other is alkyl or R.sup.1 and R.sup.2 are joined to form a cyclohexane; Q is hydrogen, hydroxy, halo or lower alkoxy; and Y is a terminal group, for example, an alkylamino, alkoxy or an optionally substituted anilino.Type: GrantFiled: April 4, 1995Date of Patent: August 13, 1996Assignee: Bio-Mega/Boehringer Ingeleheim Research Inc.Inventors: Pierre L. Beaulieu, Ingrid Guse
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Patent number: 5541228Abstract: New melatonergic agents are phenyl alkanyl or phenyl alkyl substituted carboxamides and ureas of Formula I: ##STR1## wherein: R.sub.1 =C.sub.1-3 alkyl, allyl, C.sub.3-6 cycloalkyl substituted C.sub.1-4 alkyl;R.sub.2 =hydrogen, halogen or C.sub.1-4 alkoxy;R.sub.3 =hydrogen or C.sub.1-4 alkyl;R.sub.4 =C.sub.1-4 alkyl, C.sub.1-4 alkyl substituted amino, carboxylic acid substitutedC.sub.1-4 alkyl or C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl, or straight or branched chain C.sub.2-4 alkenyl;A=a linear C.sub.2-4 alkanediyl or alkenediyl chain, provided that A not be --CH.sub.2 CH.sub.2 -- when X is a bond; andX=a covalent bond or oxygen.Type: GrantFiled: March 8, 1995Date of Patent: July 30, 1996Assignee: Bristol-Myers Squibb Co.Inventors: Katherine S, Takaki, George N. Karageorge, Daniel J. Keavy, Michael F. Parker, Brett T. Watson
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Patent number: 5516789Abstract: Compounds having the structure ##STR1## or a pharmaceutically acceptable salt thereof have activity as inhibitors of cylooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4 and cylooxygenase products such as prostaglandins and thromboxane and are useful in the treatment of inflammatory and allergic disease states. The compounds have the structure indicated above wherein A is selected from (a) optinally substituted carbocyclic aryl, (b) optinally substituted furyl, (c) optinally substituted benzo[b]furyl, (d) optinally substituted thienyl, (e) optinally substituted pyridyloxy, (f) optinally substituted pyridylalkyl, (g) optinally substituted benzo[b]thienyl, (h) optinally substituted pyridyl, (i) optinally substituted quinolyl, and (j) optinally substituted indolyl; X is selected from (a) optionally substituted alkyl, (b) optinally substituted alkenyl, and (c) optinally substituted alkynyl; R.sup.1 and R.sup.Type: GrantFiled: April 12, 1995Date of Patent: May 14, 1996Assignee: Abbott LaboratoriesInventors: Clint D. W. Brooks, Andrew O. Stewart, Anwer Basha, Randy L. Bell
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Patent number: 5510349Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: April 23, 1996Assignee: G.D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Ko-Chung Lin, Michael L. Vazquez, Richard A. Mueller, Kathryn L. Reed, Robert M. Heintz, Michael Clare, John N. Freskos, Eric T. Sun
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Patent number: 5504241Abstract: There is now provided a carbodiimide or polycarbodiimide of the formula: ##STR1## where the R radicals are identical or different and are selected from the group consisting of --NHCONHR.sup.1 --, --NHCONR.sup.1 R.sup.2 --, and --NHCOOR.sup.3 --, where R.sup.1 and R.sup.2 may be identical or different and are alkyl, cycloalkyl, or aralkyl, and R.sup.3 is identical to R.sup.1 or is alkoxypolyoxyalkylene, and n is an integer from 0 to 10.There is also provided an ester containing plastic which contains this carbodiimide as an anti-hydrolysis agent. The plastics may be a polyurethane cellular or non-cellular elastomer or thermoplastic.Type: GrantFiled: March 7, 1995Date of Patent: April 2, 1996Assignee: BASF AktiengesellschaftInventors: Siegmund Pohl, Friedhelm Lehrich, Manfred Genz, Bernd Bruchmann, Helmut Tesch, Roland Minges, Joachim Streu