Oxygen Bonded Directly To The Carbonyl (e.g., Benzoic Acid Esters, Etc.) Patents (Class 558/416)
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Publication number: 20030236234Abstract: This invention relates to novel fluorinated phenyl thiphenyl (also named diarylsulfide) derivatives and their use in Positron Emission Tomagraphy (PET) imaging of Serotonin Transporters (SERTS). The present invention also provides diagnostic compositions comprising the novel compounds of the present invention, and a pharmaceutically acceptable carrier or diluent. The invention further provides a method of imaging SERTS, comprising introducing into a patient a detectable quantity of a labeled compound of the present invetion, or a pharmaceutically acceptable salt, ester, amide or prodrug thereof.Type: ApplicationFiled: March 14, 2003Publication date: December 25, 2003Inventors: Hank F. Kung, Chyng-Yann Shiue, Shunichi Oya, Seok Rye Choi, Grace G. Shiue, Ping Fang
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Publication number: 20030233008Abstract: Carboxylic benzyl esters can be prepared by reacting benzyl chloride with carboxylic acids in the presence of one or more quaternary ammonium carboxylates as catalyst.Type: ApplicationFiled: June 10, 2003Publication date: December 18, 2003Inventors: Pieter Ooms, Ursula Jansen, Bernd-Ulrich Schenke
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Publication number: 20030220375Abstract: N-Biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.Type: ApplicationFiled: January 30, 2003Publication date: November 27, 2003Inventors: Michael R. Wood, Neville J. Anthony, Mark G. Bock, Dong-Mei Feng, Scott D. Kuduk, Dai-Shi Su, Jenny Miu-chun Wai
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Publication number: 20030208088Abstract: Novel addition products of hydroxyl-protecting groups (such as isocyanates) with oxyalkylene-substituted intermediates, such as poly(oxyalkylenated) aniline compounds, for the eventual production of substituted, and substantially pure, colorants, particularly diazo and triphenylmethane derivatives, through the reaction of such intermediates with certain reactants are provided. These new colorants exhibit improved wax and/or oil solubility and high purity, particularly due to the inability of certain impurities to deleteriously react with the protected hydroxyl groups of either the intermediate or the colorant during and/or after formation thereof. A method for producing such novel colorants through utilization of these novel substantially pure colorant intermediates is also provided.Type: ApplicationFiled: May 1, 2003Publication date: November 6, 2003Inventor: Rajnish Batlaw
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Publication number: 20030203935Abstract: Intermediates represented by the following formula: 1Type: ApplicationFiled: March 24, 2003Publication date: October 30, 2003Applicant: TEIJIN LIMITEDInventors: Tomohisa Nakada, Takayuki Hara, Yasunobu Takano
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Patent number: 6639093Abstract: The invention relates to the preparation of hydroxybenzoic benzyl esters by reacting benzyl chloride with hydroxybenzoic acids in the presence of one or more amides.Type: GrantFiled: April 5, 2002Date of Patent: October 28, 2003Assignee: Bayer AktiengesellschaftInventors: Pieter Ooms, Bernd-Ulrich Schenke
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Publication number: 20030181445Abstract: The invention provides novel compounds of the formula I below: 1Type: ApplicationFiled: January 17, 2003Publication date: September 25, 2003Applicant: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Garrick Paul Smith, Christian Krog-Jensen, Klaus Peter Bogeso
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Patent number: 6620933Abstract: A azomethine yellow dye compound of general formula (I): General formula (I) wherein R1 and R2 each independently represent a hydrogen atom or a substituent; R3 represents a substituent; m indicates an integer from 0 to 3; when m is 2 or greater, R3's may be the same or different and may be mutually bonded to form a condensed ring; R3 may be bonded to R1 or R2 to form a condensed ring; R4 represents an aryl group or a heterocyclic group; R5 and R6 each independently represent a hydrogen atom or a substituent; R7 represents a substituent; n indicates an integer from 0 to 4; when n is 2 or greater, R7's may be the same or different and the may be mutually bonded to form a condensed ring; R7 may be bonded to R5 or R6 to form a condensed ring; and R5 and R6 may be bonded to each other to form a ring.Type: GrantFiled: September 26, 2002Date of Patent: September 16, 2003Assignee: Fuji Photo Film Co., Ltd.Inventors: Kiyoshi Takeuchi, Shigeki Uehira
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Patent number: 6590118Abstract: Disclosed are compounds of formula I wherein A, R1, R2, R3, R4 and R5 are described in the specification, pharmaceutical formulations comprising these compounds, the use of these compounds are medicaments, the use of these medicaments in the treatment of and/or prevention of diabetes, especially non-insulin dependent diabetes (NIDDM or Type 2 diabetes), as well as methods for treating diabetes comprising administration of these compounds.Type: GrantFiled: September 28, 2000Date of Patent: July 8, 2003Assignee: Novo Nordisk A/SInventors: Marit Kristiansen, Palle Jakobsen, Jane Marie Lundbeck
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Publication number: 20030100640Abstract: A yellow colorant comprising a chromophore having at least one poly(oxy-C2-C4-alkylene) chain attached to an aromatic methine backbone having at least one cyanoester moiety attached thereto is provided. The ester portion must include a C1-C8 (such as ethyl, butyl, hexyl, or ethyl-hexyl) pendant group and the poly(oxyalkylene) chain must be at most 10 monomers and at least 3 monomers, with ethylene oxide as the capping group. Such a specific group of coloring agents provides the best overall yellow colorations or effects (either alone or in blends with other coloring agents, particularly at low color loadings) as well as the best overall low extraction levels when present within clear polyester (such as polyethylene terephthalate, for example), when compared to all other known polymeric yellow colorants for the same end-use. Compositions and articles comprising such colorants are provided as well as methods for producing such inventive colorants.Type: ApplicationFiled: November 3, 2001Publication date: May 29, 2003Inventor: Eric B. Stephens
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Publication number: 20030073862Abstract: The present invention relates to 2-(benzoylamino)benzoic acid derivatives of the formula I 1Type: ApplicationFiled: July 3, 2002Publication date: April 17, 2003Inventors: Anna-Lena Gustavsson, Lena Jendeberg, Patrick Roussel, Martin Slater, Markus Thor
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Patent number: 6538137Abstract: Intermediates represented by the following formula: (wherein R1 is a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or the like; X is a carboxyl group, an alkoxycarbonyl group, an aryloxycarbonyl group, an aralkoxycarbonyl group, a formyl group, —CH2—Y, —CHZ1Z2, —CH(OR4)OR5 or the like), in the synthesis of biphenylamidine derivatives to be used as inhibitors for an activated blood coagulation factor X, and a process for preparing the same.Type: GrantFiled: November 7, 2001Date of Patent: March 25, 2003Assignee: Teijin LimitedInventors: Tomohisa Nakada, Takayuki Hara, Yasunobu Takano
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Publication number: 20030053964Abstract: The invention relates to the preparation of hydroxybenzoic benzyl esters by reacting benzyl chloride with hydroxybenzoic acids in the presence of one or more amides.Type: ApplicationFiled: April 5, 2002Publication date: March 20, 2003Inventors: Pieter Ooms, Bernd-Ulrich Schenke
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Publication number: 20020137962Abstract: A ferulic acid derivative represented by the general formula: 1Type: ApplicationFiled: May 23, 2002Publication date: September 26, 2002Applicant: Agency of Industrial Science and TechnologyInventors: Takushi Sugino, Yo Shimizu, Hirosato Monobe
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Patent number: 6433211Abstract: A process for producing a cyanobenzoic acid compound, a cyanobenzamide compound, an alkyl cyanobenzoate compound, and a cyanobenzoyl chloride compound, which are useful intermediates for a variety of chemicals such as pharmaceuticals, agrochemicals, liquid crystals, and monomers for functional polymers. One nitrile group of an easily available phthalonitrile compound is selectively hydrolyzed to thereby produce a cyanobenzamide compound with high selectivity and yield. The cyanobenzamide compound thus-produced is transformed under acidic conditions into a cyanobenzoic acid compound and a cyanobenzoate ester compound without the cyano group of the benzene ring being damaged.Type: GrantFiled: September 24, 1999Date of Patent: August 13, 2002Assignee: Showa Denko Kabushiki KaishaInventors: Hiroshi Yasuda, Haruaki Ito, Takashi Tani, Kimitaka Ohshiro, Makoto Saito, Sumio Soya, Kuniomi Marumo
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Publication number: 20020062041Abstract: A process for preparing phenylacetic acid derivatives of the formula (I) by reacting benzyl chlorides of the formula (II) 1Type: ApplicationFiled: November 9, 2001Publication date: May 23, 2002Applicant: Clariant GmbHInventor: Holger Geissler
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Method for making unsymmetrically substituted fluorenyl compounds for nonlinear optical applications
Patent number: 6379590Abstract: A new method for producing unsymmetrically substituted fluorenyl compounds, one step of which is the preparation of 2,7-disubstituted fluoren-9-one derivatives via the nucleophilic substitution of a compound of the formula D wherein A′ is selected from the group consisting of —Br, —Cl, —F, —NO2, and —CN; A is selected from the group consisting of —NO2, —CN, —CO2R, —C(O)R, —SO2R, —SO2RF, —C(CN)═C(CN)2 and —CH═C(CN)2; RF is —CpF2p+1, p=from about 0 to about 10; R is an straight, branched or cyclic aliphatic alkyl group having about 1 to 10 carbon atoms, or an aromatic group such as phenyl or naphthyl; and is a carbonyl or a protected carbonyl such as a ketal or thio-ketal such as wherein R′ is —CrH2r+1; R″ is —(CH2)r—; and r is independently 2 or 3, with a nucleophilic reagent in the presence of an aprotic solventType: GrantFiled: December 2, 1994Date of Patent: April 30, 2002Assignee: AlliedSignal Inc.Inventors: Chengjiu Wu, Jianhui Shan -
Patent number: 6372693Abstract: The invention relates to 2-(3-alkenylbenzoyl)cyclohexane-1,3-diones of the formula I where the variables have the following meanings: R1, R2 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR6, —OCOR7, —OSO2R7, —SH, —S(O)nR8, —SO2OR6, —SO2NR6R9, —NR9SO2R7 or —NR9COR7; R3 is hydrogen, halogen, alkyl, haloalkyl, alkoxy, alkenyl, alkynyl; R4, R5 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, alkoxy, alkylthio, haloalkoxy, —COR10, —CO2R10, —COSR10, —CONR10R11, —C(R12)═NR13, —PO(OR10)(OR11); unsubstituted or substituted alkyl, heterocyclyl, heterocyclylalkyl, phenyl, phenylalkyl, hetaryl or hetarylalkyl; or R4 and R5 together form an alkanediyl chain which can be substituted and/or can be interrupted by a hetero atom; Q is an unsubstituted or substituted cyclohexane-1,3-dione ring whType: GrantFiled: November 2, 1999Date of Patent: April 16, 2002Assignee: BASF AktiengesellschaftInventors: Ernst Baumann, Wolfgang von Deyn, Stefan Engel, Regina Luise Hill, Uwe Kardorff, Guido Mayer, Martina Otten, Michael Rack, Joachim Rheinheimer, Matthias Witschel, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
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Salicylic acid derivatives, processes for their preparation, compositions comprising them, their use
Publication number: 20020032178Abstract: Salicylic acid derivatives of the formula I, 1Type: ApplicationFiled: July 2, 2001Publication date: March 14, 2002Inventors: Andreas Gypser, Thomas Grote, Joachim Rheimheimer, Ingo Rose, Oliver Cullmann, Markus Gewehr, Wassilios Grammenos, Jordi Tormo i Blasco, Bernd Muller, Hubert Sauter, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl -
Patent number: 6355490Abstract: The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or raman spectroscopy when directly attached to the support.Type: GrantFiled: September 4, 1997Date of Patent: March 12, 2002Inventors: Jill Edie Hochlowski, Thomas J. Sowin, Daniel W. Norbeck, Anne-Laure Marie Grillot, Rolf E. Swenson
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Patent number: 6278013Abstract: Intermediates useful in the preparation of 8-cyano-1-cyclopropyl-7-(2,8-diazabicyclo[4.3.0]nonan-8-yl-6-fluorol,4-dihydro-4-oxo-3-quinolinecarboxylic acids of the following structures are claimed.Type: GrantFiled: November 21, 2000Date of Patent: August 21, 2001Assignee: Bayer AktiengesellschaftInventors: Stefan Bartel, Thomas Jaetsch, Thomas Himmler, Hans-Georg Rast, Werner Hallenbach, Ernst Heinen, Franz Pirro, Martin Scheer, Michael Stegemann, Hans-Peter Stupp, Heinz-Georg Wetzstein
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Patent number: 6265606Abstract: 1-Alkyl-4-benzoyl-5-hydroxypyrazole compounds in which the benzoyl moiety is substituted in the 2-position with a halo, alkyl, or alkoxy group, in the 4-position with an alkylsulfonyl group, and in the 3-position with an optionally substituted phenyl group, for example, 1-(1,1-dimethylethyl)-4-(2-methyl-4-methyl-sulfonyl-3-(4-methoxyphenyl)benzoyl-5-hydroxypyrazole, were prepared and found to be useful for the control of a variety of broadleaf and grassy weeds. The compounds can be applied either preemergently or postemergently and can be used to control undesirable vegetation selectively in small grain crops and turf or non-selectively.Type: GrantFiled: May 10, 1999Date of Patent: July 24, 2001Assignee: Dow AgroSciences LLCInventors: Thomas L. Siddall, Zoltan L. Benko, Gail M. Garvin, Johnny L. Jackson, Jeffrey M. McQuiston, David G. Ouse, Thomas D. Thibault, James A. Turner, John C. Van Heertum
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Patent number: 6262292Abstract: The invention relates to (1) a process for producing a cyanobenzaldehyde compound by converting the aminomethyl group in a cyanobenzylamine compound into an aldehyde group using an oxidizing agent without impairing the cyano group, to (2) a process for producing a cyanobenzoyl halide compound by converting the aldehyde group in a cyanobenzaldehyde compound into an acid halide group without impairing the cyano group, and to (3) a process for producing a cyanobenzoic acid compound by reacting a cyanobenzaldehyde compound with a hypohalogenous compound. According to the present invention, cyanophenyl derivatives that are useful as an intermediate of medical preparations, agricultural chemicals, liquid crystals, functional high molecular monomers and the like can be produced efficiently from raw materials that are obtained without difficulty.Type: GrantFiled: June 30, 1999Date of Patent: July 17, 2001Assignee: Showa Denko K.K.Inventors: Hiroshi Yasuda, Kimitaka Ohshiro, Kaneo Nozawa, Kohei Morikawa
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Patent number: 6194454Abstract: The present invention provides novel compounds of the Formula and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1-R8 and X are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.Type: GrantFiled: February 28, 2000Date of Patent: February 27, 2001Assignee: Pfizer Inc.Inventor: Robert L. Dow
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Patent number: 6187945Abstract: An industrially advantageous process for producing cyanobenzyl compounds under mild conditions from relatively easily available cyanobenzylamine having a cyano group on the benzene ring or a compound thereof which is ring-substituted with a chlorine atom, a fluorine atom, etc. The process for producing a cyanobenzyl compound includes transforming an aminomethyl group of a cyanobenzylamine compound into a hydroxymethyl group, a halogenomethyl group, or an acyloxymethyl group without causing damage to a cyano group on the benzene ring. The transformation may be carried out by use of nitrosonium ions.Type: GrantFiled: November 24, 1999Date of Patent: February 13, 2001Assignee: Showa Denko K.K.Inventors: Hiroshi Yasuda, Masatoshi Murakami
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Patent number: 6140528Abstract: The invention relates to intermediates to herbicidal compounds of formulae (Ia), (Ib) or (Ic): ##STR1##Type: GrantFiled: November 22, 1999Date of Patent: October 31, 2000Assignee: Rhone-Poulenc Agriculture LtdInventor: David William Hawkins
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Patent number: 6037472Abstract: Compounds of formula (I) ##STR1## and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as stromelysin, gelatinase, matrilysin and collagenase, and are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.Type: GrantFiled: November 22, 1994Date of Patent: March 14, 2000Assignee: Syntex (U.S.A.) Inc.Inventors: Arlindo Lucas Castelhano, Steven Lee Bender, Judith Gail Deal, Stephen Horne, Teng J. Liak, Zhengyu Yuan
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Patent number: 5976408Abstract: An acrylonitrile derivative expressed by the following general formula I, a composition comprising the derivative and having an improved viscosity and optical anisotropy, and a liquid crystal display device: ##STR1## wherein rings A.sup.1 to A.sup.3 represent phenylene, cyclohexylene, dioxane, or pyrimidine, R.sup.Type: GrantFiled: December 19, 1997Date of Patent: November 2, 1999Assignee: Chisso CorporationInventors: Atsuko Fujita, Shuichi Matsui, Koichi Shibata, Kazutoshi Miyazawa, Yasuko Sekiguchi, Etsuo Nakagawa
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Patent number: 5945450Abstract: Naphthalene derivatives represented by formula ?I!: ##STR1## (wherein A is a hydrogen atom, a hydroxy group, a C.sub.7 -C.sub.11 aralkyloxy group, or an alkoxy group composed of an oxy group and a C.sub.1 -C.sub.12 aliphatic or alicyclic, saturated or unsaturated hydrocarbon group where the allyl may be substituted with a C.sub.6 -C.sub.10 allyloxy group; Q represents O, S, CH.sub.2, O--CH.sub.2, S--CH.sub.2, CO, or CHOR.sup.1 ; L represents CO, CR.sup.2 R.sup.3 CO, CH.sub.2 CH.sub.2 CO, or CH.dbd.CHCO; D represents a hydrogen atom, NO.sub.2, NH.sub.2, CO.sub.2 R.sup.4, or a group having the following formula ?II!: ##STR2## (wherein G represents. a hydrogen atom, OH, SO.sub.2 NH.sub.2, CO.sub.2 R.sup.6, CN, or a tetrazol-5-yl group); E represents a hydrogen atom, OH, SO.sub.2 NH.sub.2, CO.sub.2 R.sup.5, CN, or a tetrazol-5-yl group; M represents a hydrogen atom, a C.sub.1 -C.sub.4 lower alkyl group, a nitro group, or a halogen atom; and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.Type: GrantFiled: November 22, 1996Date of Patent: August 31, 1999Assignee: Teijin LimitedInventors: Kazuya Takenouchi, Katsushi Takahashi, Masaichi Hasegawa, Takahiro Takeuchi, Keiji Komoriya
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Patent number: 5935563Abstract: A compound of the formula I ##STR1## where R.sup.1 is i-propyl, i-butyl or t-butyl,R.sup.2 is alkyl with 6-14 carbon atoms, ##STR2## with R.sup.3 =H or C.sub.1 -C.sub.4 -alkyl and m, n=0 or 1.Type: GrantFiled: April 15, 1998Date of Patent: August 10, 1999Assignee: BASF AktiengesellschaftInventor: Beate Trentmann
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Patent number: 5925651Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: April 1, 1997Date of Patent: July 20, 1999Assignee: Merck & Co., Inc.Inventor: John H. Hutchinson
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Patent number: 5856578Abstract: The present invention relates to a process for the preparation of aromatic amino compounds which are substituted by a least one group comprising at least one unsaturated carbon-carbon bond, by catalytic hydrogenation of corresponding aromatic nitro compounds in the presence of a modified noble metal catalyst, wherein the noble metal catalyst used is platinum modified with a metal selected from the group consisting of lead, mercury, bismuth, germanium, cadmium, arsenic, antimony, silver and gold, and to novel noble metal catalysts for use in this process.Type: GrantFiled: November 25, 1996Date of Patent: January 5, 1999Assignee: Norvartis CorporationInventors: Urs Siegrist, Peter Baumeister
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Patent number: 5705703Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein. the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: January 21, 1997Date of Patent: January 6, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
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Patent number: 5688945Abstract: The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and selected from H and alkyl; X is selected from alkylthio, arylthio, aryloxy, halogen and cyano; R.sup.3, R.sup.4 are the same or different and selected from halogen, methyl, fluoroalkyl, cyano and Z--R.sup.5 wherein Z is selected from CH.sub.n, NH.sub.m, O, S, SO.sub.2 and CO wherein n=1 or 2; m=0 or 1 and R.sup.5 is selected from alkyl, aryl and fluoroalkyl; or R.sup.3 and R.sup.4 together form a saturated or unsaturated ring system Y--V--Z wherein Y and Z, independently of each other, are as defined for Z above and V is selected from C.sub.1 -C.sub.3 alkylene or alkenylene, --N.dbd., --N.dbd.N-- and ##STR2## wherein R.sub.Type: GrantFiled: December 20, 1996Date of Patent: November 18, 1997Assignees: Astra Aktiebolag, The University of Maryland at BaltimoreInventors: Susanna Karin Maria Bjork, Birgitta Kristina Gotthammar, Mats Torbjorn Linderberg, Johan Per Luthman, Kerstin Margareta Irma Persson, Robert Schwarcz
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Patent number: 5616799Abstract: A process for the preparation of glycoloylanilide of the formula (G) ##STR1## is recited that involves reacting a nitrobenzene with hydrogen and, if desired, with a carbonyl compound, in the presence of a noble metal catalyst and a solvent, reacting the compound produced with chloroacetyl chloride, reacting the resulting product with a benzyl alcohol and with a base, or reacting the resulting compound with an O-benzylglycoloyl chloride, and debenzylating the resulting benzylglycoloylanilide product by reacting with hydrogen in the presence of a noble metal catalyst. The invention also relates to a process for the preparation of O-benzylglycoloylanilide.Type: GrantFiled: April 17, 1995Date of Patent: April 1, 1997Assignee: Hoechst AktiengesellschaftInventors: Siegfried Planker, Theodor Papenfuhs
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Patent number: 5612373Abstract: The invention concerns acid derivatives of formula IR.sup.1 --CON(R.sup.2)--N(R.sup.3)CO--X.sup.1 --Q--X.sup.2 --GIand pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention also concerns processes for the preparation of the acid derivatives of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.Type: GrantFiled: June 27, 1994Date of Patent: March 18, 1997Assignee: Zeneca LimitedInventors: Andrew G. Brewster, Peter W. R. Caulkett, Alan W. Faull, Robert J. Pearce, Richard E. Shute
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Patent number: 5602174Abstract: A method of treatment or prophylaxis of angina in mammals, such as humans, which comprises the administration to the sufferer of an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, or a solvate of any of the foregoing: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, A and B are herein defined.Type: GrantFiled: June 1, 1995Date of Patent: February 11, 1997Assignee: Beecham Wuefling GmbH & Co.Inventor: Harald Maschler
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Patent number: 5597825Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: May 16, 1994Date of Patent: January 28, 1997Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, G unter Linz, Thomas M uller, Wolfgang Eisert, Johannes Weisenberger
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Patent number: 5574064Abstract: The present invention provides an agricultural or horticultural fungicide including an effective amount of an amino-acid derivative represented by the formula: ##STR1## wherein R.sup.1 represents a lower alkyl group (optionally having at least one same or different substituent of a halogen atom, an alkoxy group, and a cyano group), R.sup.2 represents an ethyl group, or an n-propyl group, R.sup.3 represents a hydrogen atom or a lower alkyl group, R.sup.4 represents a hydrogen atom, R.sup.5, R.sup.6, and R.sup.7 independently represent a hydrogen atom or a lower alkyl group, R.sup.8 represents a hydrogen atom, or a lower alkyl group, Z.sup.1 and Z.sup.2 independently represent an oxygen atom or a sulfur atom, Z.sup.3 represents an oxygen atom, or a sulfur atom, Q represents a phenyl group, m represents an integer from 0 to 2, and n represents 0 or 1.Type: GrantFiled: December 28, 1994Date of Patent: November 12, 1996Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masaru Shibata, Kazuhiko Sugiyama, Norihisa Yonekura, Junetsu Sakai, Yoshiyuki Kojima, Shigeru Hayashi
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Patent number: 5565191Abstract: Stilbene derivatives of formula (I) ##STR1## wherein A, R.sub.1 and R.sub.2 are as defined in the following, are useful for the protection against UV radiation.Type: GrantFiled: December 13, 1994Date of Patent: October 15, 1996Assignee: 3V Inc.Inventor: Giuseppe Raspanti
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Patent number: 5538521Abstract: A fuel additive having the formula: ##STR1## wherein A.sub.1 is a thioether, a sulfoxide, a sulfone, a sulfonic acid, a sulfonamide, a nitrile, a carboxylic acid or ester, or a carboxamide; R.sub.1 and R.sub.2 are independently hydrogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl; n is an integer from 0 to 100; and when n is 0 to 10, R.sub.5 is polyalkyl having an average molecular weight of 450 to 5,000; and when n is 5 to 100, R.sub.5 is hydrogen, alkyl, phenyl, aralkyl, alkaryl or an acyl group having the formula: ##STR2## wherein R.sub.6 is alkyl, phenyl, aralkyl or alkaryl; R.sub.7 and R.sub.8 are independently hydrogen, hydroxy, lower alkyl or lower alkoxy; A.sub.2 is a thioether, a sulfoxide, a sulfone, a sulfonic acid, a sulfonamide, a nitrile, a carboxylic acid or ester, or a carboxamide; and x and y are independently integers from 0 to 10; with the proviso that when n and x are both 0, then A.sub.Type: GrantFiled: December 23, 1993Date of Patent: July 23, 1996Assignee: Chevron Chemical CompanyInventor: Richard E. Cherpeck
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Patent number: 5478835Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.Type: GrantFiled: May 2, 1994Date of Patent: December 26, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
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Patent number: 5412079Abstract: Disclosed is a liquid crystal monomer compound represented by formula (1): ##STR1## wherein n is an integer of from 2 to 18, X is direct bond, --(C.dbd.O)--O--, --(C.dbd.O)--NH-- or --N.dbd.N--, R.sup.1 is hydrogen or a lower alkyl group, and R.sup.2 is hydrogen, a cyano group or a methoxy group, as well as a liquid crystal polymer derived therefrom.Type: GrantFiled: March 25, 1994Date of Patent: May 2, 1995Assignee: Nippon Paint Co., Ltd.Inventors: Junji Furukawa, Hiroshi Okamoto, Yoshio Onouchi, Takushi Andoh, Satoshi Urano
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Patent number: 5393774Abstract: The invention relates to phenylethanolamines of general formula ##STR1## wherein R.sub.1 and R.sub.2 are defined as in claim 1, the enantiomers and the acid addition salts thereof, which have valuable pharmacological properties, not only analgesic, antiphlogistic, broncholytic, uterus-spasmolytic, lipolytic effects and an antispastic effect on the cross-striped muscle, but also .beta..sub.2 -mimetic and/or .beta..sub.1 -blocking effects, the use thereof as pharmaceuticals and as performance enhancers and processes for preparing them.Type: GrantFiled: January 27, 1994Date of Patent: February 28, 1995Inventors: Helmut Pieper, Gunther Engelhardt
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Patent number: 5354511Abstract: Compounds having non-linear optical activity of the general formula ##STR1## wherein D and A are electron donor and acceptor groups, respectively, R.sup.1 and R.sup.2 are aromatic bridging groups, X and Y are preferably groups capable of partaking in polymerization reactions are suitable for use in polymer-based light modulator devices.Type: GrantFiled: November 27, 1992Date of Patent: October 11, 1994Assignee: AlliedSignal Inc.Inventors: Chengjiu Wu, Jianhui Shan, Ajay Nahata
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Patent number: 5344638Abstract: Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract whereinwhereinZ=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R=C.sub.1 -C.sub.25 alkyl, cycloalkyl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently lower-alkyl, optionally substituted with halo;x is 1-3y is 1-4;n is 1-5;m is 1-15;p is 1-10; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkylin an aqueous, pharmaceutically acceptable carrier.Type: GrantFiled: March 11, 1993Date of Patent: September 6, 1994Assignee: Sterling Winthrop Inc.Inventors: Carl R. Illig, Brent D. Douty
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Patent number: 5321046Abstract: Disclosed herein are novel unsymmetrical dithiol ketals which are useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.Type: GrantFiled: October 27, 1992Date of Patent: June 14, 1994Assignee: Bristol-Myers Squibb CompanyInventors: Sing-Yuen Sit, John J. Wright, Jeff A. Field
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Patent number: 5304573Abstract: The present invention relates to a hydrazone derivative represented by the general formula (I) shown below: ##STR1## wherein the substituents are as defined in the specification, processes for preparing the derivative, and uses of the derivative as an insecticide.The hydrazone derivative has a marked insecticidal effect on insect pests, especially against LEPIDOPTERA and COLEOPTERA.Type: GrantFiled: November 13, 1991Date of Patent: April 19, 1994Assignee: Nihon Nohyaku Co., Ltd.Inventors: Tomokazu Hino, Nobuharu Andoh, Hiroshi Hamaguchi, Atsushi Kanaoka
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Patent number: 5304531Abstract: Compounds of the formula: ##STR1## wherein X is hydrogen, halo, trihalomethyl, alkyl, nitro, or cyano; X.sup.1 is hydrogen, halo, or trihalomethyl; X.sup.2 is trihalomethyl or halo; Y is O, S, NH or NR.sup.1 ; R.sup.1 and R.sup.2 are the same or different radicals selected from hydrogen, alkyl, or mononuclear aralkyl; n is 1 to 5, and Z is carboxy, amino, mono- and dialkyl amino and when Z is carboxy; the agronomically acceptable salts, esters, thioesters and amides thereof, and compositions containing these compounds exhibit herbicidal activity.Type: GrantFiled: December 19, 1984Date of Patent: April 19, 1994Inventor: Wayne O. Johnson
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Patent number: 5304672Abstract: A method for the preparation of compounds of the formula ##STR1## wherein X represents a group of the formula OR.sub.1 or NR.sub.1 R.sub.2, wherein R.sub.1 and R.sub.2 independently represent H or an organic group that forms a stable covalent bond with the N or 0 of said X; Y is H or an organic group that forms a stable ester with the adjacent COO group; R is an alkyl or aryl group optionally substituted with one or more stable organic substituents; each R.sub.3 independently represents a stable organic group; and n is an integer from 0 to 3;the method using new intermediates of the formula ##STR2## wherein R.sub.3 and Y have the foregoing meanings;W is either F or Cl; andR.sub.9 is a hydrocarbon such as a C.sub.1 -C.sub.4 alkyl or alkenyl group.Type: GrantFiled: November 9, 1992Date of Patent: April 19, 1994Assignees: Orsan, OrsemInventors: Jeffrey Labovitz, William J. Guilford, Lawrence Fang, Yi Liang