Polycarboxylic Acid Patents (Class 560/44)
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Publication number: 20090017307Abstract: The present invention relates to advantageous processes for the manufacture of organic pigments and their precursors. The invention particularly relates to reactions carried out in an “All In One Reactor”® (Draiswerke GmbH, Germany), a kneader like the TurbuKneader® of the same company, a paddle dryer like the Turbudry® of the same company or a related system and thereby submitting the reaction mixtures to enhanced driving power as expressed by a Froude number >1, the reaction mixture being caused to react in high concentrations at elevated temperature.Type: ApplicationFiled: May 16, 2008Publication date: January 15, 2009Applicant: MCA TECHNOLOGIES, GMBHInventor: Bansi Lal KAUL
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Publication number: 20080293888Abstract: A diamine compound of formula (I) is proposed as well as polymers, copolymers, polyamic acids, polyamic acid esters, or polyimides based on such compound.Type: ApplicationFiled: December 19, 2006Publication date: November 27, 2008Applicant: ROLIC AGInventors: Thomas Bachels, Zoubair Mohammed Cherkaoui, Guy Marck, Olivier Muller, Joachim Reichardt, Andreas Schuster, Hubert Seiberle, Peggy Studer, Thomas Peglow, Jean-Francois Eckert
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Patent number: 7449573Abstract: A compound which generates a sulfonic acid having one or more —SO3H groups and one or more —SO2— bonds upon irradiation with an actinic ray or a radiation; a photosensitive composition containing the compound; and a method of pattern formation with the photosensitive composition.Type: GrantFiled: February 14, 2005Date of Patent: November 11, 2008Assignee: FUJIFILM CorporationInventors: Kunihiko Kodama, Kenji Wada, Kaoru Iwato
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Patent number: 7238830Abstract: The present invention provides N-alkylaspartyl dipeptideester compounds and salts thereof, such as N-[N-[3-(3-hydroxy-4-methoxyphenyl)-3-methylbutyl]-L-?-aspartyl]-L-phenylalanine 1-methyl ester, which provide high degrees of sweetness in comparison to conventional products, compositions and products containing the novel aspartyl dipeptide ester compounds and method of producing the novel aspartyl dipeptide ester compounds.Type: GrantFiled: March 16, 2001Date of Patent: July 3, 2007Assignee: Ajinomoto Co., Inc.Inventors: Yusuke Amino, Kazuko Yuzawa, Tadashi Takemoto, Ryoichiro Nakamura
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Patent number: 7196214Abstract: 4-aminobiphenyl derivative arylamine compounds are formed by providing an iodinated organic compound; substituting the iodinated organic compound at carboxylic acid groups thereof to provide ester protecting groups; conducting an Ullman condensation reaction to convert the product of step (ii) into an arylamine compound; and conducting a Suzuki coupling reaction to add an additional phenyl group to the arylamine compound in the 4-position relative to the nitrogen.Type: GrantFiled: November 22, 2004Date of Patent: March 27, 2007Assignee: Xerox CorporationInventors: H. Bruce Goodbrand, Timothy P. Bender, Jennifer A. Coggan, Nan-Xing Hu
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Patent number: 7125991Abstract: The invention relates to novel compounds of formula (I) wherein R1 represents a polymer, aryl or alkyl group, R2 represents a hydrogen atom, a halogen atom, a radical CN, CF3, OH, OCF3, COOH, R7, OR7 or OCOR7, R3 represents an represents an alkyl radical. The invention also relates to a cosmetic composition comprising said compounds and to the use thereof to reduce and/or curb hair loss i.e.Type: GrantFiled: December 13, 2004Date of Patent: October 24, 2006Assignee: L'Oreal S.A.Inventors: Jean-Baptiste Galey, Maria Dalko, Lionel Breton
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Patent number: 7087778Abstract: Processes for producing antibacterial agents and intermediates useful in producing antibacterial agents are provided and include producing compound (VI-a) in accordance with the following reaction schema, as well as production intermediates thereofType: GrantFiled: August 23, 2004Date of Patent: August 8, 2006Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Kouji Sato, Yoshihiro Takayanagi, Katsuhiko Okano, Keiji Nakayama, Akihiro Imura, Mikihiro Itoh, Tsutomu Yagi, Yukinari Kobayashi, Tomoyuki Nagai
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Patent number: 6861391Abstract: Trifluoromethyl-substituted spirocyclic ketoenols of the formula (I) are provided wherein Het represents one of the groups and G, V, W, X, Y, and Z are as defined in the specification. Also provides are processes for the preparation of the compounds. The compounds of formula (I) find use as pesticides.Type: GrantFiled: September 19, 2000Date of Patent: March 1, 2005Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht
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Patent number: 6844003Abstract: The invention relates to novel compounds of formula (I) wherein R1 represents a polymer, aryl or alkyl group, R2 presents a hydrogen atom, a halogen atom, a radical CN, CF3, OH, OCF3, COOH, R7, OR7 or OCOR7, R3 represents an aryl or alkyl halogen, R4 represents an alkyl radical. The invention also relates to a cosmetic composition comprising said compounds and to the use thereof to reduce and/or curb hair loss i.e.Type: GrantFiled: April 4, 2003Date of Patent: January 18, 2005Assignee: L'OrealInventors: Jean-Baptiste Galey, Maria Dalko, Lionel Breton
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Patent number: 6664291Abstract: The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula I, which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss. The present invention also provides methods, pharmaceutical compositions and kits for treating such diseases and disorders.Type: GrantFiled: March 28, 2001Date of Patent: December 16, 2003Assignee: Pfizer, Inc.Inventors: Yuan-Ching P. Chiang, Gary E. Aspnes, Kimberly G. Estep
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Patent number: 6583180Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are novel glucocorticoid receptor modulators and are useful for treating type II diabetes in a mammal.Type: GrantFiled: February 8, 2002Date of Patent: June 24, 2003Assignee: Abbott LaboratoriesInventors: James T. Link, Bryan K. Sorensen, Jyoti R. Patel, David L. Arendsen, Gaoquan Li
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Patent number: 6576791Abstract: Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+ channel to modulate the biological processes/functions thereof.Type: GrantFiled: October 3, 2000Date of Patent: June 10, 2003Assignee: Theravance, Inc.Inventors: Sabine M. Axt, Timothy J. Church, Witold N. Hruzewicz, John R. Jacobsen, Thomas E. Jenkins, Yu-Hua Ji, J. Kevin Judice
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Patent number: 6525093Abstract: Compounds are provided that lower blood glucose concentrations, lower serum triglyceride concentrations, lower systolic blood pressure, and increase glucose uptake by adipose tissue, but do not affect the expression of PPAR-&ggr; by adipose tissue.Type: GrantFiled: November 8, 1999Date of Patent: February 25, 2003Assignee: Calyx Therapeutics Inc.Inventors: Partha Neogi, Bishwajit Nag, Frederick J. Lakner, Debendranath Dey, Satyanarayana Medicherla
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Patent number: 6369260Abstract: Process for the preparation of a pharmacologically active chemical combination constituted by the association, through chemical bonds, of units equal to one another, having each an own pharmacological activity, and with the general formula (I): M—A—X—B—M, where M indicates said unit having an own pharmacological activity, X indicates a “bidentate” structure suitable to interconnect the M units, A and B indicate functional groups either equal to or different from one another which allow the interconnection between M and X.Type: GrantFiled: May 16, 1997Date of Patent: April 9, 2002Assignees: Laboratori Alchemica S.r.l., Nicox SAInventors: Francesco Sannicolo′, Tiziana Benincori, Piero Del Soldato
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Patent number: 6316658Abstract: N-Cyclopropyl-2-difluoromethoxy-3-halogenoanilines which serve as important intermediates in the preparation of quinolonecarboxylic acids useful as synthetic antimicrobial agents from industrially inexpensive and easily available raw materials; and intermediates for the preparation thereof. Specifically, compounds represented by the general formula (1), (2) and (3), wherein X is halogeno; and Y is nitro or amino, (2) wherein X is halogeno; and R1 is lower alkyl, (3) wherein X is halogeno; and R is hydrogen or —CH═C(CO2R2)2, R2 being lower alkyl.Type: GrantFiled: April 11, 2000Date of Patent: November 13, 2001Assignee: Ihara Chemical Industry Co., Ltd.Inventors: Yasuo Yoshida, Hiroaki Takeuchi
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Publication number: 20010039357Abstract: The present invention provides N-alkylaspartyl dipeptideester compounds and salts thereof, such as N-[N-[3-(3-hydroxy-4-methoxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester, which provide high degrees of sweetness in comparison to conventional products, compositions and products containing the novel aspartyl dipeptide ester compounds and method of producing the novel aspartyl dipeptide ester compounds.Type: ApplicationFiled: March 16, 2001Publication date: November 8, 2001Applicant: AJINOMOTO CO., INC.Inventors: Yusuke Amino, Kazuko Yuzawa, Tadashi Takemoto, Ryoichiro Nakamura
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Publication number: 20010016592Abstract: The subject-matter of the present invention is novel compounds of the type of esters derived from alkylenediaminediacetic acid or alkylenediaminetriacetic acid and their-process of preparation. The invention also relates to the use of these compounds in cosmetic and pharmaceutical compositions, in particular for protecting the body against oxidative stress.Type: ApplicationFiled: February 9, 2001Publication date: August 23, 2001Applicant: L'Oreal S.A.Inventors: Jean-Baptiste Galey, Jacqueline Dumats
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Patent number: 6187910Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.Type: GrantFiled: May 12, 1999Date of Patent: February 13, 2001Assignee: NeoRx CorporationInventor: Sudhakar Kasina
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Patent number: 6162944Abstract: Process for production of, from inexpensive raw materials of high commercial availability, N-cyclopropylanilines which are an important intermediate in producing a quinolonecarboxylic acid having a cyclopropyl group at the 1-position, a fluorine atom at the 6-position, and an alkyl group, an alkoxy group or a fluorine-substituted methoxy group at the 8-position (this quinolonecarboxylic acid is a useful synthetic antibacterial agent); and intermediates therefor. For example, a process for producing an N-cyclopropyl-3,4-difluoroaniline represented by the formula (4): ##STR1## includes reacting, in the presence of an acid in an alcohol type solvent, a 3,4-difluoro-2-substituted-aniline with a 1-alkoxy-1-trialkylsilyloxycyclopropane to produce an N-alkoxycyclopropylaniline represented by the general formula (3): ##STR2## and then reducing the N-alkoxycyclopropylaniline.Type: GrantFiled: November 22, 1999Date of Patent: December 19, 2000Assignee: Ihara Chemical Industry Co., Ltd.Inventors: Yasuo Yoshida, Kazuto Umezu, Yusuke Hamada, Fumiya Tabuchi
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Patent number: 6111115Abstract: A process for preparation of 2-(10,11-dihydro-10-oxodibenzo[b,f]thiepin-2-yl)propionic acid (i.e., Zaltoprofen) is performed by subjecting 2-(4-amino-3-carboxy-methylphenyl)propionic acid or its salt to diazotization and subsequent reaction with thiophenol to produce 2-(3-carboxymethyl-4-phenylthiophenyl)propionic acid or its salt, and subjecting the product to cyclization reaction. Other related processes and related compounds are also disclosed.Type: GrantFiled: February 17, 1999Date of Patent: August 29, 2000Assignees: Nippon Chemiphar Co., Ltd., Ube Industries, Ltd.Inventors: Masao Yamamoto, Kunio Kobayashi, Katsumasa Harada, Shigeyoshi Nishino, Hiroshi Sasaki
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Patent number: 6069170Abstract: The invention relates to a cosmetic light-screening composition for protecting human skin or human hair against ultraviolett radiation containing at least one compound of formula I ##STR1## wherein R.sup.1 represents a C.sub.1-8 straight or branched alkyl chain, andR.sup.2 and R.sup.3 each independently represent a C.sub.1-8 straight or branched alkyl chain.Type: GrantFiled: July 24, 1998Date of Patent: May 30, 2000Assignee: Roche Vitamins Inc.Inventors: Alain Bringhen, Hans Ulrich Gonzenbach, Magali Pochon, Dominique Sidrac
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Patent number: 5990318Abstract: Novel soluble polyester-supported chiral phosphines have been prepared and have been used in the preparation of rhodium and ruthenium catalysts. Such polymer-supported catalysts show high catalytic activities and enantioselectivities. In the case of Ru(BINAP) catalyst supported on soluble polyester, the resulting catalysts were found to be more active than those of the corresponding homogeneous Ru(BINAP) catalysts in the asymmetric hydrogenation of 2-arylpropenoic acids. These soluble polyester-supported catalysts can be easily separated from the reaction mixture and then be reused without loss of activity and selectivity.Type: GrantFiled: March 6, 1998Date of Patent: November 23, 1999Assignee: The Hong Kong Polytechnic UniversityInventors: Albert Sun-Chi Chan, Qing-Hua Fan
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Patent number: 5945556Abstract: A process for preparing N-carboxymethylene-4-chloroanthranilic acid, and its dialkyl esters. The invention relates to a process for preparing N-carboxymethylene-4-chloroanthranilic acid and its dialkyl esters, which comprises reacting 2,4-dichlorobenzoic acid in the presence of a base, of a solvent and of a catalyst with glycine to give N-carboxymethylene-4-chloroanthranilic acid and, where appropriate, reacting the latter in the presence of a base and of a solvent with a dialkyl sulfate, dialkyl carbonate or alkyl halide to give the dialkyl ester.Type: GrantFiled: April 14, 1998Date of Patent: August 31, 1999Assignee: Clariant GmbHInventors: Theodor Papenfuhs, Ralf Pfirmann, Stefan Krause, Doris Neumann-Grimm
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Patent number: 5811572Abstract: Process for the preparation of N-carboxymethyleneanthranilic acid esters of the formula (3) ##STR1## by reacting a compound of the formula (1) ##STR2## in which R' is hydrogen or a straight-chain or branched alkyl radical having 1 to 4 carbon atoms and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different and independently of one another are hydrogen, halogen, NO.sub.2, a straight-chain or branched alkyl, alkoxy or halogenated alkyl radical having in each case 1 to 6 carbon atoms, with a glyoxylic acid ester of the formula (2)OHC--COOR (2)in which R is a straight-chain or branched alkyl radical having 1 to 20 carbon atoms, phenyl radical or benzyl radical, which are unsubstituted or mono- or polysubstituted by halogen or an alkyl or alkoxy group having in each case 1 to 4 carbon atoms, in the presence of a solvent at 0.degree. to 200.degree. C.Type: GrantFiled: February 7, 1997Date of Patent: September 22, 1998Assignee: Hoechst AktiengesellschaftInventors: Theodor Papenfuhs, Andreas Dierdorf, Stefan Krause, Doris Neumann-Grimm
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Patent number: 5789618Abstract: A method for synthesizing a halogen-containing condensation product, the method comprising the step of:reacting a compound represented by Formula (I) with a compound represented by Formula (II) or (III) in the presence of a halogenating agent whereby dehydration condensation and halogenation are carried out, ##STR1##Type: GrantFiled: June 27, 1996Date of Patent: August 4, 1998Assignee: Konica CorporationInventors: Eisaku Katoh, Osamu Ishige
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Patent number: 5750711Abstract: The dicarboxylic acid derivatives according to the invention have the following structure ##STR1## wherein X denotes O, S, (CF.sub.2).sub.m, C(CF.sub.3).sub.2 or CF.sub.2 --CF(CF.sub.3) (m=1 to 10), and R stems from the following compounds: fluoro- or trifluoromethyl- and nitro- or cyanophenols, thiophenols or -aminobenzenes, 4-hydroxy-, 4-mercapto- or 4-aminocoumarins, N-hydroxysuccinimides or N-hydroxymaleimides, 2-hydroxy- or 2-mercaptobenzoxazoles or -benzothiazoles and 1-hydroxy- or 1-mercaptobenzotriazoles.Type: GrantFiled: August 28, 1996Date of Patent: May 12, 1998Assignee: Siemens AktiengesellschaftInventors: Racai Sezi, Hellmut Ahne, Eberhard Kuehn
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Patent number: 5731440Abstract: An industrially advantageous process for producing 5,7-dichloro-4-hydroxyquinoline (DCHQ) useful as an intermediate for agrohorticultural bactericides. The process comprises (i) hydrolyzing 3-cyano- or 3-ethoxycarbonyl-5,7-dichloro-4-hydroxyquinoline into 5,7-dichloro-3-carboxy-4-hydroxyquinoline (DCQA) in the presence of hydrochloric, sulfuric or phosphoric acid and (ii) decarboxylating the formed DCQA into DCHQ in the presence of sulfuric or phosphoric acid. In particular, this process comprises continuously conducting the hydrolysis of 5,7-dichloro-3-ethoxycarbonyl-4-hydroxyquinoline and the decarboxylation of the hydrolyzate in the presence of sulfuric acid having a specified concentration. The invention also relates to a process for producing DCQA by hydrolyzing 3-cyano- or 3-ethoxycarbonyl-5,7-dichloro-4-hydroxyquinoline in the presence of hydrochloric, sulfuric or phosphoric acid and a process for producing DCHQ by decarboxylating DCQA in the presence of sulfuric or phosphoric acid.Type: GrantFiled: September 3, 1996Date of Patent: March 24, 1998Assignees: Ishihara Sangyo Kaisha Ltd., Chemipro Kasei Kaisha, Ltd.Inventors: Hiroshi Yoshizawa, Motohiko Hamaguchi, Tomizo Fujino
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Patent number: 5714632Abstract: A compound of the formula ##STR1## wherein Q is an organic group of at least two carbon atoms having at least m substituents,m is 1, 2, 3, 4, 5 or 6, andn is 0 or 1.R.sup.3 is H or methyl,R.sup.8 and R.sup.9 are independently hydrogen, alkyl group or aryl,R.sup.12 and R.sup.13 are independently selected from the group consisting of an alkyl group or a cation, andR.sup.10 is independently selected from the group consisting of hydrogen, an alkyl group, aryl group, and highly-fluorinated alkyl group,R.sup.4 may be hydrogen or alkyl group, andR.sup.7 may be hydrogen or lower alkyl group, provides excellent stability to dispersions.Type: GrantFiled: November 13, 1995Date of Patent: February 3, 1998Assignee: Minnesota Mining And Manufacturing CompanyInventors: Prabhakara S. Rao, Larry R. Krepski, Terrance P. Smith
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Patent number: 5637701Abstract: A novel asymmetric synthesis is provided for preparing optically active amides of formula (A) and their salts. ##STR1## In the formula, X represent --N-- or --CH--, R represents a mono or bicyclic aryl or heteroaryl group, R.sup.1 is an aryl or heteroaryl radical, and R.sup.2 and R.sup.3 have specified meanings. The products are useful as 5-HT.sub.1A antagonists.Novel diesters of formula D useful as intermediates in the process are also disclosed.Type: GrantFiled: April 11, 1995Date of Patent: June 10, 1997Assignee: John Wyeth & Brother, LimitedInventor: Mark A. Ashwell
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Patent number: 5466860Abstract: A process for the preparation of blocked isocyanates by reaction of free isocyanates under water-free conditions with blocking agents containing acid hydrogen in the presence of basic catalysts, these being one or more alkali hydroxides, particularly lithium hydroxide. The process leads to yellowing-free products with a low alkali content which may be used as cross-linking agents for polyols, particularly in the lacquer sector.Type: GrantFiled: February 8, 1995Date of Patent: November 14, 1995Assignee: Herberts Gesellschaft mit beschrankter HaftungInventors: Carmen Flosbach, Dieter Philipp, Walter Schubert
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Patent number: 5453517Abstract: The invention relates to fluorescent and/or reactive derivatives of 1,2-bis-(2-aminophenoxyethane)-N,N,N',N'-tetraacetic acid (BAPTA) according to the formula: ##STR1## where at least one of W and X is a functional group, with or without a spacer, that terminates in an alcohol or phenol, a thiol, a haloacetamide, an alkyl halide, an amine or aniline, a carboxylic acid, an anhydride, an isocyanate, an isothiocyanate, a maleimide, or an activated ester. The BAPTA-like molecule may be further substituted, one or more times, by additional functional groups with or without spacers or by CH.sub.3, NO.sub.2, CF.sub.3, F, Cl, Br, I, or carboxylic acid derivatives or pharmaceutically acceptable salts thereof, or by indolyl or benzofuran fluorophores. The functional groups allow for subsequent covalent attachment of one or more oxygen heterocycle fluorophores (e.g. fluorescein, coumarin, rhodamine); or polymolecular assemblies (e.g.Type: GrantFiled: February 25, 1992Date of Patent: September 26, 1995Assignee: Molecular Probes, Inc.Inventors: Michael A. Kuhn, Richard P. Haugland
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Patent number: 5446189Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, n, m, o, p, and q are as hereinafter set forth,and, when R.sub.2 is hydrogen, pharmaceutically acceptable salts thereof with bases, are described. The compounds of formula 1 are potent inhibitors of phospholipases A.sub.2 (PLA.sub.2 's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.Type: GrantFiled: March 22, 1994Date of Patent: August 29, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Mathew Carson, Ru-Jen L. Han, Ronald A. LeMahieu, Vincent S. Madison
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Patent number: 5420339Abstract: Pharmaceutically useful compounds having acylcoenzyme A: cholesterol acyltransferase inhibitory activity having the general formula ##STR1## wherein Ar is di- or trisubstituted aryl or heteroaryl; R.sub.14 and R.sub.15 are each independently aryl, heteroaryl, hydrogen, fluorine, or alkyl, with the proviso that R.sub.14 and R.sub.15 are not both hydrogen, fluorine, or a straight or branched chain alkyl or a combination thereof; and R.sub.16 is a straight or branched hydrocarbon chain having 1 to 20 carbon atoms and is saturated or unsaturated and has 1 to 3 double bonds, the double bonds being adjacent or nonadjacent.Type: GrantFiled: November 22, 1993Date of Patent: May 30, 1995Assignee: Warner-Lambert CompanyInventors: Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5367095Abstract: Polyoxyalkylene polyamine or aromatic diamines or xylylenediamines are modified by them to the Michael reaction with an ethylenically unsaturated monomer having an electron-withdrawing group to convert the primary amino groups at least in part to a secondary amino group of the formula:--NH--CH.sub.2 --CH(R)--Ywherein R is a hydrogen atom or methyl, and Y is an electron-withdrawing group. The modified amines find use in the manufacture of plastics such as polyurea elastomers or polyurea RIM.Type: GrantFiled: September 4, 1992Date of Patent: November 22, 1994Assignee: Nippon Paint Company, Ltd.Inventors: Toshiyuki Ohshima, Hideo Ishibashi, Rie Tamura, Satoshi Yamamoto, Takaharu Izumo
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Patent number: 5359120Abstract: The invention provides compounds of the formula XX: M-Ar-CONH-R, where Ar represents an aromatic ring system, R-NH is the residue of an .alpha.-amino acid R-NH.sub.2 or oligopeptide R-NH.sub.2 and contains at least one carboxylic acid group in the form of a tertiary butyl ester and M represents a nitrogen mustard group of formula (a), where Y and L, which may be the same or different in a molecule, are leaving groups. The compounds are useful intermediates for the production of nitrogen mustard prodrugs.Type: GrantFiled: May 6, 1991Date of Patent: October 25, 1994Assignee: Cancer Research Campaign Technology LimitedInventor: Caroline J. Springer
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Patent number: 5346648Abstract: An antiferroelectric liquid crystal compound represented by the following general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are each independently selected from the group consisting of alkyl groups having from 3 to 18 carbon atoms, Rf is a lower alkyl group or a fluorinated lower alkyl group, (A) and (B) are each independently selected from the group consisting of 1,4-phenylene, 4,4'-biphenylene, and 2,6-naphthalene which may be substituted at least with a halogen atom, and * shows an asymmetric carbon atom.Type: GrantFiled: September 29, 1993Date of Patent: September 13, 1994Assignee: Showa Shell Sekiyu Kabushiki KaishaInventors: Yasuhiro Koide, Hiroyuki Mogamiya, Yoshiichi Suzuki
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Patent number: 5324747Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, n, m, o, p and q are as hereinafter set forth, and, when R.sub.2 is hydrogen, pharmaceutically acceptable salts thereof with bases, are described. The compounds of formula 1 are potent inhibitors of phospholipases A.sub.2 (PLA.sub.2 's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.Type: GrantFiled: July 15, 1992Date of Patent: June 28, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Mathew Carson, Ru-Jen L. Han, Ronald A. LeMahieu, Vincent S. Madison
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Patent number: 5312999Abstract: Propoxybenzene derivatives represented by the following formula ##STR1## wherein Ra represents a nitro group, an amino group which may have a protecting group or an --NHCH.dbd.C(COO--C.sub.1-6 -Alkyl).sub.2 group, Rb represents a hydrogen atom, a protecting group for the hydroxyl group or a substituted sulfonyl group and Xa and Xb, which may be the same or different, each represents a halogen atom, and processes for preparation thereof are disclosed. These derivatives are useful in preparing antibacterial agents.Type: GrantFiled: March 2, 1992Date of Patent: May 17, 1994Assignee: Daiichi Seiyaku Co., Ltd.Inventors: Toshihiro Fujiwara, Tutomu Ebata
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Patent number: 5298647Abstract: Aromatic compounds absorbing UVB and/or UVA, substituted with an amide function, selected from the group consisting of ##STR1## whose variable substituents are as defined in the specification, e.g. ##STR2## are useful as photoprotective agents or tanning accelerators.Type: GrantFiled: December 14, 1987Date of Patent: March 29, 1994Inventors: Dominique Robert, Louis Jung
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Patent number: 5248813Abstract: A process for obtaining a substantially pure enantiomer of an aryl-substituted aliphatic carboxylic acid is described. The process utilizes first an enantiomerically enriched mixture the of aryl-substituted aliphatic carboxylic acid obtained from kinetic resolution, diastereomeric crystallization or asymmetric synthesis processes. This enriched mixture is reacted with a base producing a salt that has the following properties:(1) has at least one eutectic point;(2) a composition that is not at the eutectic point; and(3) a eutectic composition that is closer to the racemic composition than is the eutectic composition of said aryl-substituted carboxylic acid.Substantially pure, enantiomeric salt is separated, leaving a mother liquor comprising the solvent and aryl-substituted aliphatic carboxylic acid enriched in the other enantiomer.Type: GrantFiled: October 14, 1992Date of Patent: September 28, 1993Assignee: Ethyl CorporationInventors: Thanikavelu Manimaran, G. Patrick Stahly, R. Carl Herndon, Jr.
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Patent number: 5231217Abstract: The present invention is directed to a novel solvent-free process for preparing amine terminated compounds by reacting a polyfunctional acetoacetic acid ester with either ammonia or an organic compound which contains one or more primary amino groups in the presence of an acidic catalyst selected from the group consisting of (i) boron trifluoride etherate and (ii) organic acids having pKa values of from 0.1 to 0.8.Type: GrantFiled: March 20, 1991Date of Patent: July 27, 1993Assignee: Miles Inc.Inventors: Robert P. Yeater, Robson Mafoti, Josef Sanders
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Patent number: 5231113Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where the R groups are independently hydrogen, or lower alkyl; A is --C(O)O--, --OC(O)--, --C(O)S--, or --SC(O)--; n is 0-5; and Z is H, --COB where B is --OH or a pharmaceutically acceptable salt, or B is --OR.sub.1 where R.sub.1 is an ester-forming group, or B is --N(R).sub.2 where R is hydrogen or lower alkyl, or Z is --OE where E is hydrogen or an ether-forming group or --COR.sub.2 where R.sub.2 is hydrogen, lower alkyl, phenyl or lower alkyl phenyl, or Z is --CHO or an acetal derivative thereof, or Z is --COR.sub.3 where R.sub.3 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4 and the sum of n and m does not exceed 4.Type: GrantFiled: June 4, 1992Date of Patent: July 27, 1993Assignee: Allergan, Inc.Inventors: Roshantha A. S. Chandraratna, Robert J. Weinkam
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Patent number: 5196576Abstract: A chelating compound of the formula:(R-NHOC-CH.sub.2).sub.n --A--(CH.sub.2 COOH).sub.m (I)wherein R is an aromatic ring-containing organic group, A is a residue of an aminopolyacetic acid excluding acetic acid groups (--CH.sub.2 COOH) therefrom, m is an integer of at least two and n is an integer of 1 or 2, or its salt, which has a specificity to a hepatobiliary system so that a complex formed between said chelating compound and a metallic element through a covalent bond is useful as a diagnostic or therapeutic agent for hepatobiliary organs and tissues.Type: GrantFiled: April 9, 1991Date of Patent: March 23, 1993Assignee: Nihon Medi-Physics Co., Ltd.Inventors: Shigemi Seri, Hirohiko Yamauchi, Makoto Azuma, Yoji Arata
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Patent number: 5136081Abstract: The invention provides a process for the preparation of fungicidally active cyclopentene derivatives of the general formula ##STR1## cyclopentane derivatives of the general formula ##STR2## and cyclohexane derivatives of the general formula ##STR3## in which n, R, R.sup.1, R.sup.2, R.sup.5, X and Y are as herein defined. Compounds of formula II and III are also provided which are useful as intermediates in the preparation of certain fungicidally active cyclopentane derivatives.Type: GrantFiled: September 11, 1989Date of Patent: August 4, 1992Assignee: Shell Internationale Research Maatschappij B.V.Inventor: Paul H. Briner
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Patent number: 5130469Abstract: The present invention concerns N-acyl or N-alkyl derivatives of N,N-bis(2,2-dimethyl-2-carboxyethyl)amine ##STR1## in which R and R" are similar or different C.sub.1 -C.sub.10 -alkyl or aryl groups, R" is a C.sub.3 -C.sub.12 -alkyl or aralkyl group which may contain an ester group in the carbon chain. Said derivatives are prepared by condensing ammonium halide or ammonium sulphate, formaldehyde and isobutyraldehyde, by oxidizing the condensation product thus obtained into acid form, by esterifying, and finally, by N-acylating or N-alkylating. The obtained compounds can be used for plasticizing, stabilizing, lubricating and anticorrosive agents, and for metal complexing agent for polymers, in particular polymers and polymer mixtures of vinyl chloride.Type: GrantFiled: August 15, 1990Date of Patent: July 14, 1992Assignee: Neste OyInventors: Leila Lahtinen, Oili Riutta, Pirkko Vohlonen, Ulf Nummelin, Kjell Ankner, Eija Valtonen, Soile Himanen
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Patent number: 5120869Abstract: A herbicidal compound of formula (I): ##STR1## wherein X is O, S(O).sub.n or NR.sup.a where R.sup.a is H or alkyl and n is 0, 1 or 2;R.sup.1 is H or halo;R.sup.2 is N or CR.sup.3 where R.sup.3 is halo or NO.sub.2 ;R.sup.4 is H, halo, NO.sub.2, alkyl, haloalkyl, CN, CO.sub.2 alkyl, cycloalkyl, phenyl, COalkyl, COphenyl, CHO,OH, NH.sub.2, NHCOalkyl or alkoxyR.sup.5 is H, halo or optionally substituted alkyl;R.sup.6 is H, halo or optionally substituted alkyl; provided that at least one of R.sup.5 and R.sup.6 is halo;R.sup.7 is CN, CHO, COOR.sup.8, CONR.sup.8 R.sup.9, where R.sup.8 is H, optionally substituted alkyl, alkenyl, alkynyl or aryl and R.sup.9 is a group R.sup.8, SO.sub.2 alkyl, NR.sup.10 R.sup.11 or N.sup.+ R.sup.10 R.sup.11 R.sup.12 Z.sup.- where Z is an agriculturally acceptable anion e.g. chloride and R.sup.10, R.sup.11 and R.sup.12 are independently selected from hydrogen and alkyl. Processes for the preparation of these compounds and compositions containing them are also described.Type: GrantFiled: November 7, 1989Date of Patent: June 9, 1992Assignee: Imperial Chemical Industries plcInventor: David Cartwright
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Patent number: 5118681Abstract: S-beta-dicarbonyl substituted beta-thioacrylamide compounds have been discovered to be useful as biocides and fungicides. Compositions comprising the compound and isothiazolin-3-ones and/or carries, methods of preparation of the compounds and methods of using the compounds and compositions are also disclosed.Type: GrantFiled: July 28, 1989Date of Patent: June 2, 1992Assignee: Rohm and Haas CompanyInventors: David R. Amick, Katherine E. Flynn, Cherylann Schieber
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Patent number: 5106997Abstract: A novel squarylium derivative represented by general formula (I) and a process for preparing the same are described: ##STR1## wherein X and Z are defined in the specification. This squarylium derivative exhibits high nonlinearity and is excellent in thermal resistance, light resistance, storage stability and processability, so that it can be used for preparation of nonlinear optical elements.Type: GrantFiled: September 24, 1990Date of Patent: April 21, 1992Assignee: Fuji Xerox Co., Ltd.Inventor: Lyong S. Pu
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Patent number: 5103040Abstract: This invention relates to novel 1,7-disubstituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acid derivatives and certain esters and cation salts thereof. This invention further relates to preparation of the compounds, antibacterial compositions containing the compounds and methods of using the compounds.This invention also relates to a novel process for preparing novel N-cyclopropyl intermediates useful for preparing certain of the 1,7-disubstituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acid derivatives of this invention which contain a cyclopropyl substituent at the 1 position as well as other 1,4-dihydroquinol-4-one-3-carboxylic acid derivatives so substituted with cyclopropyl.Type: GrantFiled: May 29, 1991Date of Patent: April 7, 1992Assignee: Pfizer Inc.Inventor: Paul R. McGuirk
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Patent number: 5103021Abstract: Carbonyl derivatives of acetaminophen are provided for use in homogeneous enzyme immunoassays for acetaminophen. The derivatives are conjugated to antigenic substances for the preparation of antisera specific to acetaminophen, and to enzymes for the preparation of enzyme conjugates which compete with acetaminophen for antibody binding sites in a typical assay.Type: GrantFiled: July 30, 1987Date of Patent: April 7, 1992Assignee: Syntex (U.S.A.) Inc.Inventor: Pyare Khanna