Oxy, Bonded Directly To A Ring, In Same Side Chain As Ester Function Patents (Class 560/61)
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Process for the preparation and uses of derivatives of esters of &agr;-methylene-&bgr;-hydroxy acids
Patent number: 6310237Abstract: A process for the preparation of derivatives of halo-but-2-enoic acids and esters high in 2-ene content, several of which are novel. The esters and their derivatives are useful as promoters for the polymerization of ethylene or the copolymerization of ethylene with &agr;-olefins and, optionally, nonconjugated polyenes. The promoters can also be combined with transition metal compounds, e.g., vanadium, to form combination promoter-catalyst compounds.Type: GrantFiled: July 18, 2000Date of Patent: October 30, 2001Assignee: Uniroyal Chemical Company, Inc.Inventors: Xu Wu Feng, Walter Nudenberg -
Patent number: 6303648Abstract: Methods and compositions for the treatment of lung disease, such as emphysema and/or bronchopulmonary dysplasia, in a mammal. Also disclosed are methods promoting the formation of alveolar septa and increasing the gas-exchange surface area of a mammalian lung, and for the prevention and/or treatment of alveolar destruction.Type: GrantFiled: April 13, 2000Date of Patent: October 16, 2001Assignee: Allergan Sales, Inc.Inventors: Gloria DeCarlo Massaro, Donald Massaro, Roshantha A. Chandraratna
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Patent number: 6297395Abstract: Disclosed are “acid-amide” calixarenes of formula (I) wherein: L is [—CH2—] or [—O—CH2—O—] and may be the same or different between each aryl group; R5 is H, halogen, or C1-C10 aliphatic hydrocarbyl group, C6-C20 aryl group, C6-C10 hydrocarbyaryl group, any of which may optionally be substituted by one or more halo or oxo groups or interrupted by one or more oxo groups, and R5 may be the same or different on each aryl group; R1 comprises an optionally protected carboxy group; two groups out of R2, R3, and R4 are H; the one group out of R2, R3, and R4 not being H comprises an amide group. The amide group may be linked to a second calixarene to form a dimer. Also disclosed are methods of use of such calixarenes for the purposes of metal sequestration, especially of lanthanides and actinides. Also disclosed are calixarene dimer derivatives of the calixarenes of the invention. Also disclosed are processes for preparing the calixarenes and dimers.Type: GrantFiled: December 13, 1999Date of Patent: October 2, 2001Assignee: The Secretary of State for Defence in Her Brittanic Majesty's Government of the United Kingdom of Great Britain and Northern IrelandInventors: Graeme P. Nicholson, Mark J. Kan, Gareth Williams, Michael G. Drew, Paul D. Beer
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Patent number: 6294580Abstract: A compound having formula (I), wherein A is selected from the group consisting of: (i) phenyl, wherein said phenyl is optionally substituted by one or more halogen atoms, C1-6alkyl, C1-3alkoxy, C1-3fluoroalkoxy, nitrile, or —NR7R8 where R7 and R8 are independently hydrogen or C1-3alkyl; (ii) a 5- or 6-membered hetrocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur; and (iii) a fused bicyclic ring (a), wherein ring C represents a heterocyclic group as defined in point (ii) above, which bicyclic ring is attached to group B via a ring atom of ring C; B is selected from the group consisting of: (iv) C1-6alkylene; (v) —MC1-6alkylene or C1-6alkyleneMC1-6alkylene, wherein M is O, S, or —NR2 wherein R2 represents hydrogen or C1-3alkyl; (vi) a 5- or 6-membered heterocyclic group containing at least one nitrogen heteroatom and optionally at least one further heteroatom selected from oxygen, nitrogen and sulfur and optionally substituted by C1-3alkyl; and (vii) HType: GrantFiled: August 25, 1998Date of Patent: September 25, 2001Assignee: Glaxo Wellcome Inc.Inventors: Timothy Mark Willson, Robert Anthony Mook, Istvan Kaldor, Brad Richard Henke, David Norman Deaton, Jon Loren Collins, Jeffrey Edmond Cobb, Marcus Brackeen, Matthew Jude Sharp, John Mark O'Callaghan, Greg Alan Erickson, Grady Evan Boswell
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Patent number: 6258974Abstract: There are disclosed amphoteric nano-sized metal oxide particles functionalized with silyl esters of a phosphonate and composites thereof with an acrylate-based monomer, including liquid crystal monomers photopolymerizable at ambient temperature. Also disclosed are the method making such functionalized particular by reacting a metal oxide with a silyl ester of a phosphonate in the presence of a non-aqueous solvent and in an inert atmosphere and the method of making the composites wherein the functionalized particles are admixed with an acrylate-based matrix monomer, including liquid crystal monomers photopolymerizable at ambient temperature. Further disclosed is the method of dental repair wherein the composites are applied to a tooth and photopolymerized.Type: GrantFiled: June 23, 1998Date of Patent: July 10, 2001Assignee: Southwest Research InstituteInventors: Stephen T. Wellinghoff, Hong Dixon, Henry R. Rawls, Barry K. Norling
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Patent number: 6255342Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups in which A, B, D, G, X and Z are each as defined in the description, to a plurality of processes and intermediates for their preparation, and to their use as pesticides.Type: GrantFiled: April 12, 2000Date of Patent: July 3, 2001Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Reiner Fischer, Thomas Bretschneider, Michael Ruther, Alan Graff, Udo Schneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wolfram Andersch, Andreas Turberg
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Patent number: 6248899Abstract: A description is given of a process for the transesterification of carboxylic esters, characterized in that the catalyst used is a tin(IV) compound comprising a radical of the formula bound to an inorganic support, where L is an at least divalent radical and at least one of the free valences of the Si in formula (I) is bound to the inorganic support, novel tin(IV) compounds and their preparation.Type: GrantFiled: August 9, 1999Date of Patent: June 19, 2001Assignee: Ciba Specialty Chemicals CorporationInventors: Benoît Pugin, Benoît Dubuis, Adrian Müller
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Patent number: 6207853Abstract: A process for the preparation of an enantiomerically enriched 2-substituted succinic acid derivative of formula 2, which comprises asymmetric hydrogenation of the dehydro precursor of formula 7 or 8, or a mixture thereof wherein R1 and R2 are independently H, a salt-forming cation, or an organic group of up to 30 C atoms, and R3 and R4 are independently H or an organic group of up to 30 C atoms, provided that R3 and R4 are not both H, in the presence of a transition metal complex of a chiral phosphine ligand having the partial formula 10 wherein n is 0 to 6 and R represents at least one non-hydrogen organic group of up to 30 C atoms.Type: GrantFiled: December 17, 1998Date of Patent: March 27, 2001Assignee: Chirotech Technology, Inc.Inventors: Mark Joseph Burk, Frank Bienewald, Martin Edward Fox, Antonio Zanotti-Gerosa
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Patent number: 6177154Abstract: Disclosed are (a) liquid crystalline compounds which are essential as component of the liquid crystal compositions, are excellent in miscibility with other liquid crystal compositions, particularly in the miscibility at low temperatures, and expressed by the general formula (1) wherein R0 and R1 independently represent an alkyl group having 1 to 10 carbon atoms; ring A0, ring A1, ring A2, and ring A3 represent 1,4-cyclohexylene group, 1,3-dioxane-2,5-diyl group, 1,4-phenylene group in which one or more hydrogen atoms on the ring may be represented by a halogen atom or R2O group, pyridine-2,5-diyl group, or pyrimidine-2,5-diyl group; Z0, Z1, Z2, and Z3 represent —CH2CH2—, —CH═CH—, —C≡C—, —CH2O—, —OCH2—, —CF2O—, —OCF2—, —COO—, —OCO—, —(CH2)4—, or single bond; Q1 and Q2 represent hydrogen atom or a halogen atom; Q3 represents hydrogen atom, a halogen atom, or R2O gType: GrantFiled: March 16, 1999Date of Patent: January 23, 2001Assignee: Chisso CorporationInventors: Shuichi Matsui, Tugumiti Andou, Kazutoshi Miyazawa, Hiroyuki Takeuchi, Yasusuke Hisatsune, Fusayuki Takeshita, Etsuo Nakagawa
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Patent number: 6172239Abstract: The invention relates to compounds of the formula The compounds have agreat affinity for the neurotensin receptors.Type: GrantFiled: August 16, 1999Date of Patent: January 9, 2001Assignee: SanofiInventors: Bernard Labeeuw, Danielle Gully, Francis JeanJean, Jean-Charles Molimard, Robert Boigegrain
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Patent number: 6153787Abstract: The invention encompasses a process for making compounds of Formula I or Ia useful in the treatment of cyclooxygenase-2 mediated diseases.Type: GrantFiled: December 4, 1998Date of Patent: November 28, 2000Assignee: Merck & Co., Inc.Inventors: Kai Rossen, Guo-Jie Ho, Ralph P. Volante, Roger N. Farr, David J. Mathre
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Patent number: 6147251Abstract: A process for the preparation of derivatives of halo-but-2-enoic acids and esters high in 2-ene content, several of which are novel. The esters and their derivatives are useful as promoters for the polymerization of ethylene or the copolymerization of ethylene with .alpha.-olefins and, optionally, nonconjugated polyenes. The promoters can also be combined with transition metal compounds, e.g., vanadium, to form combination promoter-catalyst compounds.Type: GrantFiled: November 6, 1998Date of Patent: November 14, 2000Assignee: Uniroyal Chemical Company, Inc.Inventors: Xu Wu Feng, Walter Nudenberg
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Patent number: 6136852Abstract: The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives represented by the general formula: ##STR1## [wherein Q represents a vinylene group or a group represented by the general formula:-A-(CH.sub.2).sub.m --(wherein A represents an oxygen atom or a methylene group; and m is an integer of from 1 to 6); R represents a hydrogen atom or a lower alkyl group; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration] and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and promoting stone removal in urolithiasis.Type: GrantFiled: March 8, 1999Date of Patent: October 24, 2000Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Makio Kitazawa, Kosuke Okazaki, Tetsuro Tamai, Masaru Saito, Nobuyuki Tanaka, Hiroaki Kobayashi, Ken Kikuchi, Hideyuki Muranaka
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Patent number: 6118019Abstract: A 3-alkoxypropionic ester derivative, an olefin polymerization solid catalyst component using the same, an olefin polymerization catalyst using the same, and a process for the preparation of a polyolefin using the same. The 3-alkoxypropionic ester derivative is represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrocarbon group having from 1 to 10 carbon atoms; R.sup.2 represents a hydrocarbon group having from 1 to 20 carbon atoms; R.sup.3 represents a hydrocarbon group having from 1 to 20 carbon atoms; and R.sup.4 represents a branched hydrocarbon group having 3 or more carbon atoms.Type: GrantFiled: December 29, 1998Date of Patent: September 12, 2000Assignee: Showa Denko K.K.Inventors: Masaki Fushimi, Shintaro Inazawa
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Patent number: 6107517Abstract: Thyroid hormone analogues are disclosed. Methods of using such analogues and pharmaceutical compositions containing them are also disclosed, as are novel procedures for their preparation.Type: GrantFiled: June 30, 1999Date of Patent: August 22, 2000Assignee: The Regents of the University of CaliforniaInventors: Thomas S. Scanlan, Hikari A.I. Yoshihara, Grazia Chiellini, Timothy J. Mitchison
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Patent number: 6048895Abstract: The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, and Z are as defined. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof.The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.Type: GrantFiled: September 4, 1998Date of Patent: April 11, 2000Assignee: The Procter & Gamble CompanyInventors: John August Wos, Mitchell Anthony deLong, Jack S. Amburgey, Jr., Haiyan George Dai, Biswanath De, David Lindsey Soper
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Patent number: 6030993Abstract: This invention relates to a novel 2-hydroxypropionic acid derivative and its manufacturing method. Based on its mechanism to inhibit the CPT I, 2-hydroxypropionic acid derivative of this invention has blood glucose lowering effects so that the derivative may be effectively used as an antidiabetic agent having remarkable antidiabetic activity and fewer side effects.Type: GrantFiled: May 4, 1999Date of Patent: February 29, 2000Assignees: Sang Sup JEW, Kwang Ho KO, Bak Kwang KIMInventors: Sang Sup Jew, Suk Ku Kang, Deuk Joon Kim, Won Ki Kim, Hwa Jung Kim, Chang Kiu Moon, Jeong Hill Park, Young Ger Suh, Bong Jin Lee, Jee Woo Lee, Ki Hwa Jung, Moon Woo Chun, Hoon Huh, Eung Seok Lee, Hyung Ook Kim, Eun Kyung Kim, Sung Jin Kim, Jae Hoon Cheong, Kwang Ho Ko, Bak Kwang Kim
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Patent number: 5935986Abstract: There are described compounds of the general formula I ##STR1## in which the index and the substituents have the following meanings: n is 0, 1, 2, 3 or 4;R is nitro, cyano, halogen,unsubstituted or substituted alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy orin the event that n is greater than 1 additionally an unsubstituted or substituted bridge which is bonded to two adjacent ring atoms;R.sup.1, R.sup.2 are alkyl;R.sup.3 is a substituted pyrazole ?sic! or triazole ?sic! radical of the formulae A.1 to A.3 ##STR2## where the bond marked .circle-solid. is the bond to the oxygen, processes for their preparation, and their use.Type: GrantFiled: November 20, 1997Date of Patent: August 10, 1999Assignee: BASF AktiengesellschaftInventors: Bernd Muller, Reinhard Kirstgen, Hartmann Konig, Michael Rack, Klaus Oberdorf, Franz Rohl, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
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Patent number: 5929117Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: GrantFiled: August 11, 1997Date of Patent: July 27, 1999Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 5917015Abstract: A support material for solid phase synthesis is provided having an amine-containing organic group attached to it through a linker.Type: GrantFiled: June 18, 1996Date of Patent: June 29, 1999Assignee: Regents of the University of MinnesotaInventors: Knud J. Jensen, George Barany, Micheal F. Songster, Fernando Albericio, Jordi Alsina, Josef Vagner
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Patent number: 5910508Abstract: Novel pharmaceutically/cosmetically-active polycyclic polyenic compounds have the structural formula (I): ##STR1## and are useful for modulating cellular hormone receptors.Type: GrantFiled: September 2, 1997Date of Patent: June 8, 1999Assignee: Centre International De Recherches Dermatologiques GaldermaInventors: Etienne Thoreau, Braham Shroot
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Patent number: 5886209Abstract: A multi-stage catalytic process for preparing a 2-(4-hydroxyphenoxy)-propionate, especially methyl 2-(4-hydroxyphenoxy)-propionate, with a purity greater than 99% by esterifying the corresponding 2-(4-hydroxyphenoxy)-propionic acid with an excess amount of alcohol, e.g. methyl alcohol, in a series of at least 2 up to 10 sequential stages at temperatures of 20.degree. to 150.degree. C. and pressures of 0.05 to 5 bar in the presence of a distillable acid catalyst such as hydrochloric acid or hydrogen chloride. In a first esterification stage, unreacted alcohol is removed from the ester product in vacuo at temperatures of 30.degree. to 100.degree. C. together with other volatile components, including the acid catalyst. Without a separate purification of the resulting ester as the bottoms product of the first stage, the esterification step is repeated in at least one additional stage. The final ester product of this multi-stage process is characterized by a water content of less than 0.Type: GrantFiled: September 6, 1996Date of Patent: March 23, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Wettling, Manfred Dimmler, Bernd Hupfeld, Jochem Henklemann
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Patent number: 5883294Abstract: Selective thyroid hormone agonists are disclosed that are highly selective for the TR.beta. subtype with high binding affinity. Methods of using such agonists and pharmaceutical compositions containing them are also disclosed, as are novel procedures for their preparation.Type: GrantFiled: June 18, 1997Date of Patent: March 16, 1999Assignee: The Regeants of the University of CaliforniaInventors: Thomas S. Scanlan, Grazia Chiellini, Hikari Yoshihara, James Apriletti, John D. Baxter, Ralff C. J. Ribeiro
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Patent number: 5877334Abstract: A solid phase synthesis method and intermediates useful in the process are disclosed for the preparation of diamino diol and diamino alcohol inhibitors of HIV protease.Type: GrantFiled: July 23, 1996Date of Patent: March 2, 1999Assignee: Abbott LaboratoriesInventor: Gary T. Wang
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Patent number: 5869735Abstract: Process for the preparation of alkyl aryl ethers containing carboxyl groups which are suitable for the preparation of colour film couplers, or derivatives thereof, by reaction of aromatic alcohols with alkyl halides containing carboxyl groups or derivatives thereof and basic alkali metal or alkaline earth metal compounds, characterized in that the reaction is carried out in the melt of the aromatic alcohol.Type: GrantFiled: October 11, 1996Date of Patent: February 9, 1999Assignee: Bayer AktiengesellschaftInventors: Stefan Antons, Erich Hammerschmidt, Heinz Ulrich Blank, Helmut Fiege, Heinz-Gerd Hartges
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Patent number: 5855629Abstract: This invention provides alkoxy acetic acid derivatives of general formula I: ##STR1## wherein R is the residue of an amine, an aminoalcohol or a polyol linked to the or each --CHR'--CO-- moiety via an amide or ester linkage;R' is hydrogen or a C.sub.1-4 alkyl group;R.sup.1 is an optionally substituted hydrocarbyl group of 1 to 300 carbon atoms;one of R.sup.2 and R.sup.3 is independently selected from hydrogen and optionally substituted hydrocarbyl of 1 to 10 carbon atoms, the other of R.sup.2 and R.sup.3 being independently selected from optionally substituted hydrocarbyl of 1 to 10 carbon atoms;m is from 3 to 200;n is from 0 to 20, provided that m/n is at least 1; andp is from 1 to 5; a process for their preparation; and their incorporation in additive concentrates and fuel compositions for internal combustion engines.Type: GrantFiled: April 25, 1997Date of Patent: January 5, 1999Assignee: Shell Oil CompanyInventors: Michael John Grundy, David Roy Kendall, Thomas Webster Naisby, Andrew Czeslaw Sutkowski
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Patent number: 5777151Abstract: Mono- or polycarboxylic acid esters are prepared by reacting a salt of such carboxylic acid with an organic halocompound, e.g., a (cyclo)alkyl, (cyclo)alkenyl, aryl or aralkyl halide, in an aqueous reaction medium, in the presence of a catalytically effective amount of a phase transfer catalyst, for example an onium salt.Type: GrantFiled: September 24, 1992Date of Patent: July 7, 1998Assignee: Rhone-Poulenc ChimieInventor: Michel Crochemore
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Patent number: 5773625Abstract: The present invention relates to a process for the preparation of cabonate compounds useful for the preparation of compounds which are human immunodeficiency virus (HIV) protease inhibitors.The compounds have formula I: ##STR1## wherein R.sup.9 is hydrogen or lower alkyl, and the thiazolyl ring can be unsubituted or substituted with a lower alkyl group.Type: GrantFiled: October 2, 1997Date of Patent: June 30, 1998Assignee: Abbott LaboratoriesInventor: Denton C. Langridge
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Patent number: 5755994Abstract: A novel liquid crystalline compound having a large dielectric anisotropy value, a small change in the threshold voltage depending upon temperatures, and an improved solubility in other liquid crystal materials at low temperatures, and a liquid crystal composition containing the compound are provided,which liquid crystalline compound is expressed by the formula (1) ##STR1## wherein R is H or an alkyl group of 1 to 10C; l is an integer of 1 to 9; m, n and o are each independently 0 or 1; A.sub.1, A.sub.2 and A.sub.3 are each independently trans-1,4-cyclohexylene group, 1,4-phenylene group, one or more H atoms on the ring of which group may be replaced by F, or the like group; Z.sub.1, Z.sub.2 and Z.sub.3 are each independently --COO--, etc., but at least one of them is --COO--; X is CF.sub.3, etc.; and Y.sub.1, and Y.sub.2 are each independently H or F.Type: GrantFiled: February 22, 1996Date of Patent: May 26, 1998Assignee: Chisso CorporationInventors: Tomoyuki Kondo, Shuichi Matsui, Yasuyuki Koizumi, Koichi Shibata, Yasuhiro Haseba, Norihisa Hachiya, Etsuo Nakagawa, Kazutoshi Miyazawa
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Method of treating malignant tumors with thyroxine analogues having no significant hormonal activity
Patent number: 5736576Abstract: The present invention provides methods for treating cancer, particularly malignant tumors, with thyroxine analogues having no significant hormonal activity. A thyroxine analogue is administered to an afflicted mammal in an amount effective to cause depression or regression of malignant tumor growth or to treat cancer.Type: GrantFiled: June 4, 1996Date of Patent: April 7, 1998Assignee: Octamer, Inc.Inventors: Ernest Kun, Jerome Mendeleyev -
Patent number: 5734077Abstract: New substituted 2,2-dimethyl-.omega.-phenoxyalkanoic acids and esters of formula: ##STR1## wherein: X, A, B, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and Z are as defined in the specification,The corresponding enantiomers and diastereoisomers, and the physiologically tolerable salts thereof with appropriate bases.The products of the invention may be used therapeutically.Type: GrantFiled: September 13, 1996Date of Patent: March 31, 1998Assignee: Adir ET CompagnieInventors: Gilbert Regnier, Claude Guillonneau, Jean-Paul Vilaine, Florence Mahlberg, Christine Breugnot
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Patent number: 5728864Abstract: A liquid crystal compound of the formula (1) ##STR1## wherein R is a linear alkyl group having 6 to 12 carbon atoms,both X and Y are hydrogen atoms or one of X and Y is a fluorine atom and the other is a hydrogen atom,A is --CF.sub.3 or --C.sub.2 F.sub.5,m is an integer of 2 to 4,n is an integer of 2 to 4, andC* is an asymmetric carbon,having a ferrielectric phase in its phase sequence, or a ferrielectric liquid crystal composition containing the liquid crystal compound of the formula (1) having a ferrielectric phase, may be injected between substrates provided with nonlinear active elements, such as thin film transistors or diodes formed on each pixel, to form an active matrix liquid crystal display device.Type: GrantFiled: April 12, 1996Date of Patent: March 17, 1998Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Yuki Motoyama, Tomoyuki Yui, Masahiro Johno, Maki Ito, Takahiro Matsumoto, Hiroshi Mineta
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Patent number: 5726205Abstract: This document describes O-acyl-4-phenyl-cycloalkanols of general formula I ##STR1## wherein n denotes the number 0 or 1, m denotes the number 1 or 2, p denotes the number 0 or 1, R.sup.1 and R.sup.2 each denote hydrogen, lower alkyl, alkenyl or alkynyl, which may optionally also be substituted, or together with the nitrogen atom between them denote 5- to 7-membered saturated, monocyclic, heterocyclic rings which may optionally also be interrupted by an oxygen or sulphur atom or by an imino group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 denote hydrogen or lower alkyl, R.sup.5 additionally denotes lower alkoxy, R.sup.7 denotes hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A denotes a chemical bond or alkyl, alkenyl or alkynyl having up to 17 carbon atoms, and also processes for preparing them, pharmaceutical compositions containing these compounds and the use of these pharmaceutical compositions which intervene in cholesterol biosynthesis.Type: GrantFiled: January 17, 1997Date of Patent: March 10, 1998Assignee: Karl Thomae GmbHInventors: Eberhard Woitun, Roland Maier, Peter Muller, Rudolf Hurnaus, Michael Mark, Bernard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
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Patent number: 5707544Abstract: The present invention is concerned with chromophore-containing photo cross-linkable liquid crystalline compounds having the formula ##STR1## wherein A.sup.1 and A.sup.2 each represent a cross-linkable, mesogenic group; andA.sup.3 represents a dichroic group.as well as liquid crystalline mixtures which contain such compounds and their use in the cross-linked state as optical components.Type: GrantFiled: May 20, 1996Date of Patent: January 13, 1998Assignee: Rolic AGInventor: Stephen Kelly
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Patent number: 5703130Abstract: New retinoid compounds, as chalcone retinoids and compositions thereof, are provided which exhibit therapeutic and/or biological activity on cancer or precancer cells, as well as to methods of use of same.Type: GrantFiled: June 7, 1996Date of Patent: December 30, 1997Assignee: Institute of Materia Medica, an Institute of the Chinese Academy of Medical SciencesInventors: Rui Han, Zong-Ru Guo
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Patent number: 5686633Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.Type: GrantFiled: December 31, 1991Date of Patent: November 11, 1997Assignee: Ciba Specialty Chemicals CorporationInventors: Eric Vieira, Hugh Stephen Laver
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Patent number: 5658944Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein Ar is a mono- or bicyclic aromatic group optionally containing one or two heteroatoms independently selected from nitrogen, oxygen and sulphur, said group being optionally substituted by one or more atoms or groups independently selected from halogen, nitro, amino, --NRR.sup.1 where R and R.sup.1 are independently selected from hydrogen, C.sub.1-8 alkyl and C.sub.1-8 alkanoyl, cyano, carboxyalkoxy, alkoxycarbonylalkoxy, C.sub.1-8 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.1-8 alkoxy (including cycloalkoxy and cycloalkylalkoxy), C.sub.Type: GrantFiled: April 14, 1995Date of Patent: August 19, 1997Assignee: The University of South CarolinaInventors: James Mood Chapman, Jr., Roy Lee Hawke, Karl Witold Franzmann, Kevin Julian O'Connor
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Patent number: 5654338Abstract: Optically active .alpha.-(hydroxyphenoxy)-alkanecarboxylic acids or derivatives thereof, for example D-2-(4-hydroxyphenoxy)propionic acid or lower alkyl ester thereof, are prepared by (a) saponifying an alkyl ester of an optically active .alpha.-halogeno-alkanecarboxylic acid, in an alcoholic solvent medium, by reacting same with an aqueous solution of an alkali metal hydroxide, thereby providing a solution of an alkali metal salt of an optically active .alpha.-halogeno-alkanecarboxylic acid, (b) next reacting the step (a) solution thus provided with a dihydroxybenzene or salt thereof, in the presence of an alkali metal hydroxide and in an alcoholic solvent medium, and thence (c) recovering the optically active .alpha.-(hydroxyphenoxy)-alkanecarboxylic acid or derivative thereof from the medium of reaction.Type: GrantFiled: April 25, 1995Date of Patent: August 5, 1997Assignee: Rhone-Poulenc ChimieInventor: Pascal Metivier
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Patent number: 5650533Abstract: The invention relates to 4-substituted isoxazole derivatives of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, Q and n have the meaning defined in the description which possess valuable herbicidal properties.Type: GrantFiled: June 2, 1995Date of Patent: July 22, 1997Assignee: Rhone-Poulenc Agriculture Ltd.Inventors: David Alan Roberts, Susan Mary Cramp, Derek Ian Wallis, Jean-Paul Bulot
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Patent number: 5646184Abstract: Disclosed is a preparation for external application to the skin characterized by containing at least one of benzoic acid derivatives represented by formula (I) or pharmacologically acceptable salts thereof as an active ingredient, the preparation having sufficient sebaceous secretion inhibitory activity with no substantial side effect and high safety for human body. ##STR1## wherein R.sup.1 represents --OH, --OR.sup.3 or --NHR.sup.3 ; R.sup.2 represents a hydrogen atom, a lower alkyl group or a lower acyl group; R represents --O--R.sup.4 or ##STR2## R.sup.3 represents an alkyl group, an alkenyl group or a hydroxyalkyl group; R.sup.4 represents a straight-chain or branched, saturated or mono-unsaturated alkyl group or cycloalkylalkyl group having from 4 to 10 carbon atoms; X represents --O-- or --NH--; and n represents 1 or 2.Type: GrantFiled: November 9, 1994Date of Patent: July 8, 1997Assignee: Kao CorporationInventors: Akira Sakaguchi, Takashi Kitahara, Keiko Koizumi, Noriko Sato, Kimihiko Hori, Hiroyuki Shinta
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Patent number: 5622532Abstract: Polylactone aromatic esters having the formula: ##STR1## wherein R.sub.1 is a hydrocarbyl group having a sufficient number of carbon atoms to render the compound soluble in hydrocarbons boiling in the gasoline or diesel fuel range;R.sub.2 is an alkylene group of about 2 to 5 carbon atoms;R.sub.3 and R.sub.4 are each independently hydrogen, hydroxy, nitro, amino, N-alkylamino having 1 to 6 carbon atoms in the alkyl group, or N,N-dialkylamino having 1 to 6 carbon atoms in each alkyl group, provided that R.sub.3 and R.sub.4 may not both be hydrogen;and x is an integer from 1 to 25.The polylactone aromatic esters of formula I are useful as fuel additives for the prevention and control of engine deposits.Type: GrantFiled: June 20, 1996Date of Patent: April 22, 1997Assignee: Chevron Chemical CompanyInventor: Richard E. Cherpeck
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Patent number: 5621133Abstract: Novel compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, whereinA is --O--, --S-- or --CR.sup.2 R.sup.8 --;R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, X and Y are specifically defined; andup to one combination of (a) R.sup.2 and R.sup.5, (b) R.sup.5 and R.sup.6, (c) R.sup.5 and R.sup.7, (d) R.sup.6 and R.sup.7, and (e) R.sup.7 and Y, taken together with the atoms to which they are attached, may form a ring, the compounds being useful for treating dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of cognitive impairment, attention deficit disorder, and substance abuse and other addictive behavior disorders.Also disclosed are intermediates and processes useful in the preparation of the above compounds.Type: GrantFiled: June 5, 1995Date of Patent: April 15, 1997Inventors: Michael P. DeNinno, Richard J. Perner
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Patent number: 5618320Abstract: Aromatic esters of polyalkylphenoxyalkanols having the formula: ##STR1## or a fuel soluble salt thereof, wherein R is hydroxy, nitro or --(CH.sub.2).sub.x --NR.sub.5 R.sub.6, wherein R.sub.5 and R.sub.6 are independently hydrogen or lower alkyl having 1 to 6 carbon atoms and x is 0 or 1;R.sub.1 is hydrogen, hydroxy, nitro or --NR.sub.7 R.sub.8, wherein R.sub.7 and R.sub.8 are independently hydrogen or lower alkyl having 1 to 6 carbon atoms;R.sub.2 and R.sub.3 are independently hydrogen or lower alkyl having 1 to 6 carbon atoms; andR.sub.4 is a polyalkyl group having an average molecular weight in the range of about 450 to 5,000.The compounds of formula I are useful as fuel additives for the prevention and control of engine deposits.Type: GrantFiled: May 14, 1996Date of Patent: April 8, 1997Assignee: Chevron Chemical CompanyInventor: Richard E. Cherpeck
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Patent number: 5602196Abstract: Stabilisers of formula I ##STR1## wherein R.sub.1 and R.sub.2 may be C.sub.1 -C.sub.5 alkyl, the substituents R.sub.3 to R.sub.8 may be hydrogen, the variable n may be 1 or 2, and, when n is 1, A may be an alkoxy radical, and, when n is 2, A may be a diamine radical.Type: GrantFiled: November 27, 1995Date of Patent: February 11, 1997Assignee: Ciba-Geigy CorporationInventors: Bernard Gilg, Rita Pitteloud
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Patent number: 5599966Abstract: Compounds of the formula (I): Ar.sub.1 --CH(OH)--CH.sub.2 --NH--CH.sub.2 --X--CH.sub.2 --E--(CH.sub.2).sub.n --Y--Ar.sub.2, in which the substituents and symbols have the meanings given in the description, are novel active compounds having, in particular, a broncholytic action.Type: GrantFiled: April 17, 1995Date of Patent: February 4, 1997Assignee: BYK Nederland BVInventors: Jan Bron, Geert J. Sterk, Hendrik Timmerman, Meta E. J. Veerman, Jan F. Van Der Werf
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Patent number: 5596124Abstract: There is provided a method for safening herbicides in cereal crop plants by using 5-aryloxy-1,2 -(disubstituted)benzene compounds of formula I ##STR1## Further provided are compositions comprising a 5-aryloxy-1,2-(disubstituted)benzene compound of formula I.Type: GrantFiled: December 9, 1994Date of Patent: January 21, 1997Assignee: American Cyanamid CompanyInventors: Gail E. Cary, Peter J. Wepplo, Barbara A. Bench
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Patent number: 5593617Abstract: The present invention is related to photochemically polymerizable liquid crystals of the general formula ##STR1## wherein A.sup.1, A.sup.2 and A.sup.3 are, independently, photochemically polymerizable mesogenic residues. The present invention also provides liquid crystalline mixtures which contain these compounds, as well as use of these compounds in the cross-linked state as optical or electronic components.Type: GrantFiled: August 21, 1995Date of Patent: January 14, 1997Assignee: Hoffmann-LaRoche Inc.Inventors: Stephen Kelly, Teodor Luk ac
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Patent number: 5591884Abstract: Novel compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, whereinA is --O--, --S-- or --CR.sup.2 R.sup.8 --;R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, X and Y are specifically defined; andup to one combination of (a) R.sup.2 and R.sup.5, (b) R.sup.5 and R.sup.6, (c) R.sup.5 and R.sup.7, (d) R.sup.6 and R.sup.7, and (e) R.sup.7 and Y, taken together with the atoms to which they are attached, may form a ring, the compounds being useful for treating dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of cognitive impairment, attention deficit disorder, and substance abuse and other addictive behavior disorders.Also disclosed are intermediates and processes useful in the preparation of the above compounds.Type: GrantFiled: June 5, 1995Date of Patent: January 7, 1997Assignee: Abbott LaboratoriesInventors: Michael P. DeNinno, Richard J. Perner
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Patent number: 5565606Abstract: The invention relates to compounds of the formula I ##STR1## in which A denotes hydrogen or an amino protective group, B denotes one or more amino acids, X denotes alkylene or aralkylene, Y.sup.1, Y.sup.2, Y.sup.3 and Y.sup.4 are identical or different and denote hydrogen, methyl, methoxy or nitro, V denotes hydrogen or a carboxyl protective group, W denotes --[CH.sub.2 ].sub.n -- or --O--[CH.sub.2 ].sub.n --, m denotes 0 or 1, n denotes 0 to 6, and p denotes 0 to 5, to a process for their preparation. The compounds of formula I are useful as linkage agents or anchor groups in the solid-phase synthesis of peptide aminoalkylamides and peptide hydrazides.Type: GrantFiled: June 8, 1994Date of Patent: October 15, 1996Assignee: Hoechst AktiengesellschaftInventors: Gerhard Breiphol, Jochen Knolle
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Patent number: 5554641Abstract: The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK.sub.3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.Type: GrantFiled: March 20, 1995Date of Patent: September 10, 1996Inventors: David C. Horwell, Martyn C. Pritchard, Jennifer Raphy