Plural Rings Containing Patents (Class 568/325)
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Patent number: 6232476Abstract: This invention provides an improved process for cis-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenoxy]ethyl}pyrrolidine which is an intermediate for the preparation of (-)cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol which is useful for the treatment of osteoporosis.Type: GrantFiled: May 19, 2000Date of Patent: May 15, 2001Assignee: Pfizer Inc.Inventor: Charles K. F. Chiu
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Patent number: 6147216Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula ##STR1## wherein W represents --C(.dbd.O)-- or --CH(OH)--;R.sub.1 represents hydrogen or hydroxy;R.sub.2 represents hydrogen;R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;n is an integer of from 1 to 5;m is an integer 0 or 1;R.sub.3 is --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; andpharmaceutically acceptable salts and individual optical isomers thereof,with the proviso that where R.sub.1 and R.sub.2 are ta to form a second bond between the carbon R.sub.1 and R.sub.2 or where R.sub.1 represented hydroxy integer 0.Type: GrantFiled: June 2, 1995Date of Patent: November 14, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
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Patent number: 6147224Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.Type: GrantFiled: October 1, 1998Date of Patent: November 14, 2000Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
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Patent number: 6075057Abstract: Optically pure enantiomers of avarol are obtained. The enantiomers of avarol are demonstrated to be highly effective inhibitors of .alpha.-glucosidase and .alpha.-mannosidase. Other enzymes assayed were not inhibited by these optically pure compounds. Inhibition of these two enzymes is useful for a variety of assays and probes, and offers particular utility in the treatment of retroviral infection-associated syndromes, such as AIDS.Type: GrantFiled: April 1, 1997Date of Patent: June 13, 2000Assignee: The University of Virginia Patent FoundationInventors: Sidney M. Hecht, Edward Locke
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Patent number: 6051588Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.Type: GrantFiled: April 19, 1995Date of Patent: April 18, 2000Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6005113Abstract: The invention relates to fluorescent dyes that are substituted or unsubstituted derivatives of 1-(isoindolyl)methylene-isoindole that are bound through both isoindole nitrogens to a boron difluoride moiety, forming a fluorescent dibenzopyrrometheneboron difluoride compound ##STR1## that is further substituted by bathochromic substituents that are aryl or heteroaryl moieties further substituted by an additional aryl or heteroaryl, that is itself optionally further substituted by an additional aryl or heteroaryl. These aryl and heteroaryl groups are separated by a covalent bond, or by an ethenyl, butadienyl or hexatrienyl linkage. The dyes of the invention are particularly useful as labels for carriers, particularly polymeric microparticles. The resulting microparticles have a long-wavelength fluorescence emission, and possess utility for tracing flow in biological systems, particularly in tracing blood flow.Type: GrantFiled: May 14, 1997Date of Patent: December 21, 1999Assignee: Molecular Probes, Inc.Inventors: Yexin Wu, Dieter H. Klaubert, Hee Chol Kang, Yu-Zhong Zhang
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Patent number: 5968482Abstract: The invention relates to the use of .alpha.-hydroxyketoalkyl derivatives as light protection filters for cosmetic or pharmaceutical products, the .alpha.-hydroxyketoalkyl group being linked, if appropriate via a spacer, to a chromophoric group which has an absorption maximum in a wavelength range of between 280 and 400 nm and has a conjugated .pi.-electron system of at least 8 .pi.-electrons, and to new .alpha.-hydroxyalkyl derivatives, processes for their preparation and pharmaceutical and cosmetic formulations comprising these derivatives as light protection substances.Type: GrantFiled: September 20, 1996Date of Patent: October 19, 1999Assignee: Merck Patent Gesellschaft MIT Beschrankter HaftungInventors: Roland Martin, Ingeborg Stein, Ulrich Heywang, Michael Schwarz, Thekla Kurz
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Patent number: 5932765Abstract: The present invention relates to the compounds of formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.3, E, A, X, Z, p and n are as defined herein. These compounds are aldose reductase inhibitors.Type: GrantFiled: October 22, 1997Date of Patent: August 3, 1999Assignee: Merck Patent Gesellschaft MitInventors: Claude Lardy, Jaques Barbanton, Herve Dumas, Francois Collonges, Phillippe Durbin
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Patent number: 5861415Abstract: Curcuminoids have been found to have anti-oxidant, anti-inflammatory, antibacterial, antifungal, antiparasitic, anti-mutagen, anticancer and detox properties. The present invention is directed to compositions containing three curcuminoids, i.e. curcumin, demethoxy curcumin and bis demethoxy curcumin, extracted from roots of tumeric. These compositions have been found to have activity in the anti-oxidant mechanisms of prevention and intervention.Type: GrantFiled: October 27, 1997Date of Patent: January 19, 1999Assignee: Sami Chemicals & Extracts, Ltd.Inventors: Muhammed Majeed, Vladimir Badmaev, R. Rajendran
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Patent number: 5840879Abstract: The invention provided methods and compositions for oligonucleotide synthesis and labeling. The subject compounds have either rigid ring or long linear linker structures and provide enhanced coupling efficiencies over prior art labeling reagents because of lack of stereo hindering and/or provide more convenient and cost-effective syntheses. These novel linkers also contain a base labile structure which provides: labeling at 3' end with regular solid supports, cleaving under mild conditions, and achieving higher yield because of the complete cleavage and higher purity because the mild conditions will not bring down the impurities on the solid support. When used in a solid support pre-attached with either a nucleotide for unlabeled oligonucleotide synthesis, or a label for 3' end labeled oligonucleotide synthesis, or an alternate structure to use as an universal support, these linkers provide solid supports requiring only mild cleavage conditions.Type: GrantFiled: December 6, 1996Date of Patent: November 24, 1998Inventor: Edge R. Wang
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Patent number: 5840724Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.Type: GrantFiled: June 24, 1997Date of Patent: November 24, 1998Assignee: Rhone-Poulenc Rorer LimitedInventors: Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Keith Alfred James Stuttle, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher
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Patent number: 5763672Abstract: Catalyst compositions for preparing polyketones comprising(a) a Group VIII metal compound, containing at least one ligand capable of coordinating to the Group VIII metal, and(b) a boron hydrocarbyl compoundare disclosed, in particular catalyst compositions wherein the boron hydrocarbyl compound is a Lewis acid of the formula BXYZ where at least one of X, Y and Z is a monovalent hydrocarbyl group. A preferred catalyst composition comprises a palladium complex and B(C.sub.6 F.sub.5).sub.3.Type: GrantFiled: November 4, 1996Date of Patent: June 9, 1998Assignee: BP Chemical LimitedInventors: Neil Andrew Cooley, Adrian Peter Kirk
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Patent number: 5763673Abstract: A diarylheptanoide derivative of the following formula (1), ##STR1## and a drug composition comprising this compound, such as a 5-lipoxygenase inhibitor, an antiinflammatory agent, and the like. The diarylheptanoide derivative (1) is effective for treating and preventing various inflammatory diseases due to its strong 5-lipoxygenase inhibiting effect.Type: GrantFiled: November 22, 1995Date of Patent: June 9, 1998Assignee: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Takeshi Matsuzaki, Ritsuo Aiyama, Shusuke Hashimoto, Teruo Yokokura
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Patent number: 5760092Abstract: Disclosed are allocolchinones, which are anti-mitotic agents. Allocolchinones bind to tubulin reversibly and are more effective at inhibiting microtubule formation than colchicine. 7-Acetamido-allocolchinone inhibits the growth of a number of tumor cell lines at concentrations about 100 times lower than colchicine. Also disclosed is a method of treating an individual with cancer by administering a composition which comprises a therapeutically effective amount of an allocolchinone which inhibits microtubule assembly. Administering a therapeutically effective amount of a composition which comprises an allocolchinone which inhibits microtubule assembly can also be used for treating inflammatory diseases, multiple sclerosis, primary biliary cirrhosis, Alzheimer's Disease and Behcet's Disease.Type: GrantFiled: March 11, 1996Date of Patent: June 2, 1998Assignee: Brandeis UniversityInventors: Serge M. Timasheff, Marina J. Gorbunoff, Bernardo Perez-Ramirez
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Patent number: 5739374Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: February 14, 1997Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5723621Abstract: A novel process for producing a biaryl compound represented by formula (III), which is useful as a medicine, an agricultural chemical and an electrooptical liquid-crystal display material:Ar--Ar' (III)(wherein Ar and Ar' each independently represents a substituted or unsubstituted aromatic group) which comprises the steps of (i) reacting a trialkoxysilyl-substituted aromatic compound represented by formula (I):Ar--Si(OR).sub.3 (I)(wherein Ar has the same meaning as defined above and R represents an alkyl group having from 1 to 5 carbon atoms) with a fluoride ion source in the presence of a solvent, and then (ii) adding thereto an aromatic compound represented by formula (II):X--Ar' (II)(wherein X represents an eliminating group and Ar' has the same meaning as defined above) and a catalyst comprising a transition metal of tenth group to conduct a further reaction.Type: GrantFiled: May 14, 1996Date of Patent: March 3, 1998Assignee: Chisso CorporationInventors: Koichi Shibata, Shuichi Matsui, Kazutoshi Miyazawa
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Patent number: 5679696Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.Type: GrantFiled: June 7, 1995Date of Patent: October 21, 1997Assignee: Rhone-Poulenc Rorer LimitedInventors: Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Keith Alfred James Stuttle, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher
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Patent number: 5656619Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5610197Abstract: This invention relates to benzyl and naphthalenylmethyl thiophenones and cyclopentenones, some of which are novel, which have oral antihyperglycemic activity in diabetic mice, a genetic animal model of non-insulin dependent diabetes mellitus. These compounds are represented by the formula ##STR1## wherein: R.sup.2 and R.sup.3 are independently selected from hydrogen, C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifluoromethyl or R.sup.2 together with R.sup.3 forms a benzo ring fused to the phenyl ring and optionally substituted with one or two substituents independently selected from C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifluoromethyl;R.sup.1 is selected from hydrogen, C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifluoromethyl; andR.sup.4 is selected from the group consisting of: ##STR2## wherein R.sup.5 is H or C.sub.1-6 alkyl or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 17, 1995Date of Patent: March 11, 1997Inventor: Michael S. Malamas
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Patent number: 5545399Abstract: A composition for topical application to the skin in order to promote the repair of photo-damaged or aged skin and/or to reduce or prevent damaging effects of ultra-violet light on skin and/or to lighten the skin comprising a hydrocalchone of general structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3, which may be the same or different, represent H, --OH, --OR or --COR (where R is a C.sub.1-20 alkyl group);R.sub.4, R.sub.5, R.sub.6 and R.sub.7, which may be the same or different, represent H or --COR (where R is as herein before defined).Optional additional ingredients include sunscreens and other skin lightening skin lightening agents, particularly retinol or derivatives thereof.Type: GrantFiled: October 24, 1994Date of Patent: August 13, 1996Assignee: Chesebrough-Pond's USA Co.Inventors: Caroline M. Lee, Martin R. Green, Giuseppe Prota
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Patent number: 5488180Abstract: This invention relates to complex hydrophobe compounds and to alkoxylation products, i.e., condensation reaction products of alkylene oxides and complex hydrophobe compounds having at least one active hydrogen. This invention also relates to alkoxylation products that have beneficial, narrow molecular weight ranges.Type: GrantFiled: May 29, 1992Date of Patent: January 30, 1996Assignee: Union Carbide Chemicals & Plastics Technology CorporationInventors: Richard D. Jenkins, David R. Bassett, Danny E. Smith, John N. Argyropoulos, James E. Loftus, Gregory D. Shay
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Patent number: 5399291Abstract: Fluorine-containing, chiral and achiral liquid crystal compounds comprise (a) an aliphatic fluorocarbon terminal portion comprising a perfluorinated or partially-fluorinated alkylene group and a terminal hydrocarbon alkyl group, the groups optionally containing at least one catenary ether oxygen atom; (b) an aliphatic hydrocarbon terminal portion; and (c) a central core connecting the terminal portions. The compounds have smectic mesophases or latent smectic mesophases and are useful, for example, in liquid crystal display devices.Type: GrantFiled: September 30, 1993Date of Patent: March 21, 1995Assignee: Minnesota Mining and Manufacturing CompanyInventors: Eugene P. Janulis, Gilbert C. Johnson, Marc D. Radcliffe, Patricia M. Savu, Daniel C. Snustad, Terence D. Spawn
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Patent number: 5380900Abstract: Disclosed herein is an .alpha.-methylene-cyclopentanone derivative represented by the formula [I] below which is useful as an intermediate for pharmaceuticals and insecticides, especially prostaglandins. Also disclosed herein is a process for producing the derivative advantageously on an industrial scale. ##STR1## where X denotes (.alpha.-OZ, .beta.-H) or (.alpha.-H, .beta.-OZ), with Z representing a protecting group for the hydroxyl group; U denotes (.alpha.-H, .beta.-R.sup.1) or (.beta.-R.sup.1, .alpha.-H); R.sup.1 denotes ##STR2## where R.sup.2 denotes a protected hydroxyl group, a substituted or unsubstituted C.sub.1-15 alkyl group, a substituted or unsubstituted C.sub.2-15 alkenyl group, a substituted or unsubstituted C.sub.2-15 alkynyl group, or a substituted or unsubstituted C.sub.6-15 aryl group; Z' denotes a protecting group for the hydroxyl group; and k is 0 or 1).Type: GrantFiled: February 12, 1992Date of Patent: January 10, 1995Assignee: Nissan Chemical Industries, LimitedInventors: Fumie Sato, Kazutaka Arai, Katsuaki Miyaji
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Patent number: 5349105Abstract: Retinoid like activity is exhibited by compounds of the formula ##STR1## where R.sub.1 -R.sub.4 independently are hydrogen, lower alkyl, cycloalkyl or lower alkenyl, A and B independently are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, SR* or OR* where R* is lower alkyl, cycloalkyl or lower alkenyl; Y is lower alkenyl, lower alkynyl, lower cycloalkyl, lower branched chain alkyl or (CH.sub.2).sub.n where n is 0-6; and Z is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR' or a ketal derivative where R' is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons.Type: GrantFiled: March 17, 1993Date of Patent: September 20, 1994Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5326898Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently are hydrogen, lower alkyl of 1 to 6 carbons, halogen or lower alkoxy of 1 to 6 carbons; R.sub.5 and R.sub.5 ' independently are hydrogen or lower alkyl of 1 to 6 carbons; Y is oxygen or sulfur; Z is n-alkyl having 2 to 10 carbons, cyclo or branch-chained alkyl of 3 to 10 carbons, and straight chain alkenyl having 2 to 10 carbons, or cyclo or branched chained alkenyl of 3 to 10 carbons, and the Z-Y substituent is in a 1,2 (ortho) or 1,3 (meta) position on the phenyl ring relative to the ethene moiety; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3 to 6 carbons, cycloalkyl having 3 to 6 carbons, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.Type: GrantFiled: February 11, 1992Date of Patent: July 5, 1994Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5312930Abstract: This invention relates to optical elements capable of second harmonic generation and novel compositions for use in such optical elements comprising polar molecules placed in noncentrosymmetric configuration wherein such optical element has an electron donor moiety linked through a conjugated bonding moiety to an electron acceptor moiety which consists of a selected fluorinated sulfone, fluorinated ketone, fluorinated vinyl sulfone or fluorinated alkyl vinyl sulfone.Type: GrantFiled: December 31, 1992Date of Patent: May 17, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventors: Lap T. Cheng, Andrew E. Feiring, Wilson Tam
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Patent number: 5288742Abstract: The invention concerns .alpha.,.alpha.-dialkylbenzyl derivatives of the formula I ##STR1## wherein Ar.sup.1 is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;the phenylene group may optionally bear one or two substituents R.sup.3 ;each of R.sup.1 and R.sup.2, which may be the same or different, is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, fluoro-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, provided that both of R.sup.1 and R.sup.2 are not methyl or fluoromethyl; andQ is cyano, amino, nitro, formyl, (1-4C)alkoxy, thiazolyl or (2-4C)alkanoyl;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.Type: GrantFiled: March 18, 1992Date of Patent: February 22, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Philip N. Edwards, David Waterson
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Patent number: 5266344Abstract: The present invention relates to a novel compound tetrahydrocurcumin and a substance containing the same, which are produced from curcumin or a substance containing it as a material. This substance has characteristic properties such as strong antioxidative activity and yellowish color generated from reducing the original color of curcumin. The curcumin is being produced from a Zingiberaceae plant classified into Curcuma longa as a tropical product and is used for a spice and a yellow pigment for curry powder and pickles. The present invention further relates to the production method.Type: GrantFiled: November 20, 1990Date of Patent: November 30, 1993Assignee: Kabushiki Kaisha Kobe Seiko ShoInventors: Akio Mimura, Yoshimasa Takahara, Toshihiko Osawa
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Patent number: 5262082Abstract: Fluorine-containing liquid crystal compounds are provided. The compounds comprise a fluorocarbon terminal portion having at least one catenary ether oxygen and a hydrocarbon terminal portion, the terminal portion being connected by a central core, the compounds having smectic mesophases or having latent smectic mesophases.Type: GrantFiled: April 28, 1992Date of Patent: November 16, 1993Assignee: Minnesota Mining and Manufacturing CompanyInventors: Eugene P. Janulis, Gilbert C. Johnson, Patricia M. Savu, Terence D. Spawn
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Patent number: 5254708Abstract: The present invention relates to substituted cyclopentanone and cyclohexanone derivatives and substituted cyclopentenone and cyclohexenone derivatives, which are useful as intermediates for pharmaceutical products and agricultural chemicals and especially useful for the synthesis of prostaglandins, and also to a process for producing the same.Type: GrantFiled: December 14, 1990Date of Patent: October 19, 1993Assignee: Nissan Chemical Industries, Ltd.Inventors: Fumie Sato, Kazutaka Arai, Katsuaki Miyaji
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Patent number: 5231208Abstract: The present invention relates to substituted cyclopentanone and cyclohexanone derivatives and substituted cyclopentenone and cyclohexenone derivatives, which are useful as intermediates for pharmaceutical products and agricultural chemicals and especially useful for the synthesis of prostaglandins, and also to a process for producing the same.Type: GrantFiled: December 14, 1990Date of Patent: July 27, 1993Assignee: Nissan Chemical Industries, Ltd.Inventors: Fumie Sato, Kazutaka Arai, Katsuaki Miyaji
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Patent number: 5216185Abstract: Polymerizable calixarene and oxacalixarene derivates wherein at least one aryl group of the macrocyclic ring has a phenolic side chain of the formula VII: ##STR1## wherein Z is a group containing an acrylate or methacrylate functional group. Linear polymers may be formed from these compounds by free radical polymerization at the (meth)acrylate group. Such compounds and their polymers are capable of sequestering metals.Type: GrantFiled: December 10, 1990Date of Patent: June 1, 1993Assignee: Loctite LimitedInventors: Stephen J. Harris, John Guthrie, Maureen MacManus, Michael A. McKervey
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Patent number: 5208388Abstract: 2,2-Difluorocyclopropyl derivatives of the formula ##STR1## in which R represents alkyl, optionally substituted aryl or optionally substituted aralkyl andX represents hydroxymethyl, 2-hydroxyethyl, isocyanato, amino, amino hydrohalide or a radical of the formula --CO--R.sup.1, whereR.sup.1 represents hydrogen, hydroxyl, alkoxy, alkyl, halogen or amino,are intermediates for fungicides.Type: GrantFiled: September 20, 1991Date of Patent: May 4, 1993Assignee: Bayer AktiengesellschaftInventors: Karl-Rudolf Gassen, Bernd Baasner
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Patent number: 5208353Abstract: This invention relates to a process for preparing epoxy esters, and intermediates prepared by this process, in particular, to a process which produces non-racemic epoxy esters which are of use as intermediates in the preparation of pharmaceutical compounds.Type: GrantFiled: July 15, 1992Date of Patent: May 4, 1993Assignee: SmithKline Beecham Corp.Inventors: Joseph R. Flisak, Paul G. Gassman, Ivan Lantos, Wilford L. Mendelson
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Patent number: 5194636Abstract: In the preparation of benzyl ketones of the formula ##STR1## a benzyl chloride of the formula ##STR2## is reacted with an acid chloride of the formulaR.sup.6 --CO--Cl (III)a) in a first stage with an excess of zinc powder in the presence of a diluent at a temperature between 80.degree. C. and 200.degree. C. under an inert gas atmosphere, and separating off the excess zinc powder, thereby to obtain a benzyl derivative of the formula ##STR3## and b) in a second stage reacting the benzyl derivative of the formula (IV) with an acid chloride of the formula (III) in the presence of a palladium catalyst and in the presence of a diluent at a temperature between 0.degree. C. and 150.degree. C. under an inert gas atmosphere.Type: GrantFiled: March 3, 1992Date of Patent: March 16, 1993Assignee: Bayer AktiengesellschaftInventors: Thomas Himmler, Udo Kraatz, Wolfgang Kramer, Klaus Stroech
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Patent number: 5177259Abstract: The present invention is novel diarylalkanoids having activity as lipoxygenase inhibitors, novel pharmaceutical compositions therefor, and novel methods of use in treating asthma, allergies, cardiovascular diseases, migraines, psoriasis and immunoinflammatory diseases for diarylalkanoids. The compounds of this invention are also useful as cytoprotective agents.Type: GrantFiled: August 27, 1991Date of Patent: January 5, 1993Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn
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Patent number: 5146001Abstract: In the preparation of benzyl ketones of the formula ##STR1## a benzyl chloride of the formula ##STR2## is reacted with an acid chloride of the formulaR.sup.6 --CO--Cl (III)a) in a first stage with an excess of zinc powder in the presence of a diluent at a temperature between 80.degree. C. and 200.degree. C. under an inert gas atmosphere, and separating off the excess zinc powder, thereby to obtain a benzyl derivative of the formula ##STR3## and b) in a second stage reacting the benzyl derivative of the formual (IV) with an acid chloride of the formula (III) in the presence of a palladium catalyst and in the presence of a diluent at a temperature between 0.degree. C. and 150.degree. C. under an inert gas atmosphere.Type: GrantFiled: June 3, 1991Date of Patent: September 8, 1992Assignee: Bayer AktiengesellschaftInventors: Thomas Himmler, Udo Kraatz, Wolfgang Kramer, Klaus Stroech
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Patent number: 5142095Abstract: The present invention is novel diarylalkanoids having activity as lipoxygenase inhibitors, novel pharmaceutical compositions therefor, and novel methods of use in treating asthma, allergies, cardiovascular diseases, migraines, psoriasis and immunoinflammatory diseases for diarylalkanoids. The compounds of this invention are also useful as cytoprotective agents.Type: GrantFiled: August 17, 1989Date of Patent: August 25, 1992Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn
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Patent number: 5128479Abstract: Oxidized diphenylheteroalkanes of the formula I ##STR1## where R.sup.1 to R.sup.6 and A have the meanings specified in the description, and the preparation thereof are described. The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: January 29, 1990Date of Patent: July 7, 1992Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5120876Abstract: This invention relates to optical elements capable of second harmonic generation and novel compositions for use in such optical elements comprising polar molecules placed in noncentrosymmetric configuration wherein such optical element has an electron donor moiety linked through a conjugated bonding moiety to an electron acceptor moiety which consists of a selected fluorinated sulfone, fluorinated ketone, fluorinated vinyl sulfone or fluorinated alkyl vinyl sulfone.Type: GrantFiled: February 28, 1990Date of Patent: June 9, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventors: Lap T. Cheng, Andrew E. Feiring, Wilson Tam
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Patent number: 5117062Abstract: A novel synthesis of aromatic tertiary amines involves reacting an aromatic anil and an aromatic ether in a molar ratio of 1:1; adjusting the ratio to 2:1 produces novel enamines and by employing a two step process for enamine production, various unsymmetrically substituted enamines can be obtained which are readily hydrolyzed to corresponding deoxybenzoins which in turn are readily oxidized to benzils, the aromatic tertiary amines may be used to produce charge transport layers in xerography, while the benzils may be used to produce a variety of desired polymers.Type: GrantFiled: January 22, 1991Date of Patent: May 26, 1992Inventors: Allan S. Hay, Martino Paventi
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Patent number: 5114601Abstract: Non-sulphurized overbased metal salts of sulphur-free calixarenes having a substituent hydroxyl group or groups available for reaction with metal base are claimed. The salts are useful as additives to lubricating oils by reason of their acids neutralization capability, their detergent and their antioxidant properties.Type: GrantFiled: March 22, 1991Date of Patent: May 19, 1992Assignee: BP Chemicals (Additive) LimitedInventors: Stephen J. Cook, Sean P. O'Connor, Andrew Pearce
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Patent number: 5106871Abstract: The present invention relates to an anti-ulcer agent comprising a compound represented by the following general formula I as the effective ingredient, and a novel chalcone derivative included in the compound represented by this general formula I: ##STR1## wherein X and Y independently stand for a hydrogen atom or together form a single bond, R.sub.1 stands for a hydroxyl group, an acetoxy group, a carboxymethoxy group or a methoxycarbonylmethoxy group, R.sub.2 stands for a hydrogen atom, an isoprenyl group, isopentyl group or a propyl group, R.sub.3 stands for hydroxyl group or a methoxy group, R.sub.4 stands for a hydrogen atom, a hydroxyl group or a methoxy group, R.sub.5 stands for a hydrogen atom, a hydroxyl group, a methoxy group or an isopentyl group, R.sub.6 stands for a hydroxyl group, a methoxy group or a carboxymethoxy group, and R.sub.7 stands for a hydrogen atom or a methoxy group.Type: GrantFiled: July 19, 1991Date of Patent: April 21, 1992Assignee: Tsumura & Co.Inventors: Yukio Komazawa, Shigefumi Takeda, Kunio Hosaka, Hiroshi Mitsuhashi, Toshihiko Watanabe
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Patent number: 5095147Abstract: 2,2-Difluorocyclopropyl derivatives of the formula ##STR1## in which R represents alkyl, optionally substituted aryl or optionally substituted aralkyl andX represents hydroxymethyl, 2-hydroxyethyl, isocyanato, amino, amino hydrohalide or a radical of the formula --CO--R.sup.1, whereR.sup.1 represents hydrogen, hydroxyl, alkoxy, alkyl, halogen or amino,are intermediates for fungicides.Type: GrantFiled: April 26, 1991Date of Patent: March 10, 1992Assignee: Bayer AktiengesellschaftInventors: Karl-Rudolf Gassen, Bernd Baasner
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Patent number: 5081283Abstract: Novel intermediates for fungicides, comprising fluorocyclopropyl derivatives of the formula ##STR1## in which R represents alkyl, optionally substituted aryl or optionally substituted aralkyl,X represents hydrogen, chlorine or bromine andR.sup.1 represents hydroxyl, alkoxy, alkyl or halogen.Type: GrantFiled: April 26, 1991Date of Patent: January 14, 1992Assignee: Bayer AktiengesellschaftInventors: Karl-Rudolf Gassen, Bernd Baasner
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Patent number: 5068447Abstract: Aromatic carbonyl compounds, in particular arylene ether ketones, are prepared by reacting an appropriate reagent system in the presence of free Lewis acid and a complex between a Lewis acid, for example, aluminum trichloride, and an inorganic salt controlling agent, for example, lithium chloride, and, optionally, a diluent, such as methylene chloride. The process is particularly advantageous for the preparation of substantially or all para-linked arylene ether ketones as the presence of the Lewis acid/Lewis base complex markedly reduces alkylation and ensures the substantial absence of ortho substitution.Type: GrantFiled: July 6, 1990Date of Patent: November 26, 1991Assignee: Raychem CorporationInventors: Heinrich C. Gors, Patrick J. Horner, Viktors Jansons
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Patent number: 5043415Abstract: The application describes nitrogen-containing an oxacalixarene or calixarene derivative of formula I: ##STR1## wherein m'+m"=0-8n=0-8m'.gtoreq.1/2(m'+M")3.ltoreq.m'+m"+n.ltoreq.8if n=0, m'+m".gtoreq.4R.sup.3 is H, halogen, or hydrocarbyl, aryl, hydrocarbylaryl or a substituted derivative thereof and R.sup.3 may be the same or different on each aryl group;R.sup.1 and R.sup.15 which may be the same or different are H or hydrocarbyl, aryl, hydrocarbylaryl or a substituted derivative thereof;R.sup.2 is selected from:R.sup.4 which is H, or hydrocarbyl, aryl, hydrocarbylaryl or a substituted derivative thereof, ##STR2## wherein R.sup.5 and R.sup.6 which may be the same or different are H, or hydrocarbyl, aryl, hydrocarbylaryl, or a substituted derivative thereof,-OR.sup.1, wherein R.sup.1 is as defined aboveand R.sup.17 which is a residue of a hydrocarbyl, aryl, or hydrocarbylaryl group or of a substituted derivative thereof providing a bond to another oxacalixarene or calixarene derivative of formula I wherein R.Type: GrantFiled: September 23, 1988Date of Patent: August 27, 1991Assignee: Loctite (Ireland) Ltd.Inventors: Stephen J. Harris, Maureen G. MacManus, John Guthrie
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Patent number: 5025036Abstract: The invention relates to catechol carboxylic acid derivatives of the formula ##STR1## wherein, R.sub.1 is ##STR2## acetyl, hydrogen, hydroxy or alkanoyloxy, R.sub.2 is ##STR3## hydroxy, hydrogen or alkanoyloxy, wherein R is hydrogen, lower alkyl or --(CH.sub.2).sub.n --N--(lower alkyl).sub.2,R.sub.3 is hydrogen, lower alkyl or amino,R.sub.4 is hydrogen, lower alkyl, halogen or aminoA is ##STR4## wherein, R.sub.5 is hydrogen or acyl, R.sub.6 is hydrogen, halogen, lower alkyl, aryl or cycloalkyl, and R.sub.7 and R.sub.8, independently, are hydrogen, lower alkyl or halogen, orA is ##STR5## wherein, R.sub.5 is hydrogen or acyl, R.sub.9 is hydrogen, lower alkyl, R.sub.10 is hydrogen, lower alkyl or halogen, R.sub.11 is hydrogen, lower alkyl, cycloalkyl or halogen, m is 0 or 1, n is an integer of 2-10, provided, that no more than one of R.sub.1 or R.sub.2 can be hydroxy, alkanoyloxy or ##STR6## and when R is hydrogen, salts thereof with pharmaceutically acceptable bases or when R is --(CH.sub.2).sub.Type: GrantFiled: May 3, 1989Date of Patent: June 18, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Matthew Carson, Ru-Jen L. Han, Ronald A. LeMahieu
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Patent number: 4967011Abstract: The present invention relates to a process for decomposing an aromatic acylated compound.HF-BF.sub.3 complex in preparing an aromatic acylated compound by decomposing an aromatic acylated compound.HF-BF.sub.3 complex obtained by reacting an aromatic compound with an acylating agent in the presence of HF-BF.sub.3 as a catalyst, which comprises subjecting the aromatic acylated compound.HF-BF.sub.3 complex to thermal decomposition in the presence of at least one aromatic hydrocarbon (A.H.) selected from benzene, toluene and chlorobenzene and at least one saturated aliphatic hydrocarbon (S.H.) selected from pentane, hexane and cyclohexane, as a decomposing agent.Type: GrantFiled: August 11, 1989Date of Patent: October 30, 1990Assignee: Mitsubishi Gas Chemical Co., Inc.Inventors: Nobuyuki Tokura, Tadayoshi Takefumi, Shunichi Matsumoto, Tatsuhiko Yanagawa, Yoshihiro Shiokawa, Ichiyo Ohtsuka
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Patent number: 4959503Abstract: The present invention is novel diarylalkanoids having activity as lipoxygenase inhibitors, novel pharmaceutical compositions therefor, and novel methods of use in treating asthma, allergies, cardiovascular diseases, migraines, psoriasis and immunoinflammatory diseases for diarylalkanoids. The compounds of this invention are also useful as cytoprotective agents.Type: GrantFiled: November 2, 1988Date of Patent: September 25, 1990Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn