Oxy In Acid Moiety Patents (Class 560/45)
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Patent number: 5461045Abstract: A fused benzeneoxyacetic acid derivative of the formula: ##STR1## wherein ##STR2## is (i) ##STR3## (ii) ##STR4## (iii) ##STR5## or (iv) ##STR6## A is (i) ##STR7## or (ii) ##STR8## R.sup.1 is hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl or phenyl;R.sup.3 is(i) C.sub.1-15 alkyl,(ii) C.sub.1-8 alkyl substituted by one or two of benzene, C.sub.4-7 cycloalkane or 4-7 ring-membered monocyclic ring which contains one nitrogen atom or(iii) C.sub.10-15 condensed tricyclic ring;e is 3-5;f is 1-3;p is 0-4;q is 0-2;s is 0-3With the proviso that, ring(s) in R.sup.3 may be substituted by one to three of C.sub.1-4 alkyl, .sub.1-4 alkoxy, halogen atom, nitro or trihalomethyl. And, when D--B is the formula (iii) or (iv), --(CH2)p- or .dbd.CH--(CH2)s- is attached at the position of a or b on the ring.Type: GrantFiled: July 14, 1992Date of Patent: October 24, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
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Patent number: 5459275Abstract: An electrophotographic photoconductor comprises an electroconductive substrate and a photoconductive layer formed thereon comprising as an effective component at least one pyrenylamine derivative of formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W, j, k, l, m and n are specifically defined in the specification. Furthermore, a novel pyrenylamine derivative for use in the above electrophotographic photoconductor, an aldehyde compound, which is an intermediate for producing the pyrenylamine derivative, and methods of preparing the pyrenylamine derivative and the aldehyde compound are disclosed.Type: GrantFiled: June 15, 1994Date of Patent: October 17, 1995Assignee: Ricoh Company, Ltd.Inventors: Chiaki Tanaka, Masaomi Sasaki, Tamotsu Aruga, Tomoyuki Shimida, Hiroshi Adachi
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Patent number: 5459134Abstract: A novel (fused) benz(thio)amide of the general formula: ##STR1## or a non-toxic salt thereof, wherein R.sup.4 represents:(i) when B represents a closed ring, a group of the general formula: ##STR2## wherein U represents an oxygen atom or a sulfur atom; or (ii) when B represents a divalent group, a group of the general formula: ##STR3## wherein R.sup.5, R.sup.6, R.sup.7, R.sup.8, n, m, p and q are as defined in the specification, and exclusing certain compounds as defined in the specification, depending on whether A represents a single bond or a group. The compounds are useful for the prevention and/or treatment of diseases induced by leukotrienes, 5.alpha.-reductase, phospholipase and aldose reductase in mammals, especially human beings.Type: GrantFiled: October 21, 1994Date of Patent: October 17, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Tsumoru Miyamoto, Yoshinobu Arai
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Patent number: 5457232Abstract: A pyrenylamine derivative having an unsaturated bond of formula (I), which can be employed as an organic photoconductive material for use in electrophotography: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W, l, m, n, j and k are specifically defined in the specification, an aldehyde compound of formula (II), which is an intermediate for preparing the pyrenylamine derivative: ##STR2## and methods of producing the pyrenylamine derivative and the aldehyde compound are disclosed.Type: GrantFiled: September 9, 1994Date of Patent: October 10, 1995Assignee: Ricoh Company, Ltd.Inventors: Chiaki Tanaka, Masaomi Sasaki, Tamotsu Aruga, Tomoyuki Shimada, Hiroshi Adachi
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Patent number: 5446158Abstract: A process is described for the total synthesis of the macrolide immunosuppressant, FK-506, and important tricarbonyl process intermediates thereof. The tricarbonyl intermediates can be produced by the mild oxidation of 2,3-dihydroxy carboxylate compounds containing olefin moieties.Type: GrantFiled: October 12, 1990Date of Patent: August 29, 1995Assignee: Merck & Co., Inc.Inventors: Todd K. Jones, Sander G. Mills, David Askin, Robert A. Reamer, Richard Desmond, David M. Tschaen, Ralph P. Volante, Ichiro Shinkai
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Patent number: 5446058Abstract: A novel (fused) benz(thio)amide of the general formula: ##STR1## or a non-toxic salt thereof, wherein A represents a single bond or a group as defined in the specification;B represents(i) a substituted or unsubstituted carbocyclic ring of 4 to 8 members being unreplaced or optionally having one, two or three carbon atom(s) replaced by oxygen, nitrogen and/or sulfur atom(s); or(ii) a divalent group of formula: ##STR2## T represents oxygen or sulfur; R.sup.1 represents a group of general formula: ##STR3## or (iv) a straight or branched alkyl, alkenyl or alkynyl group of from 1 to 20 carbon atom(s);R.sup.2 represents hydrogen or a straight or branched alkyl group of from 1 to 6 carbon atom(s);R.sup.' represents hydrogen, a halogen atom, a hydroxy group, a nitro group or a group --COOR.sup.7 ;R.sup.Type: GrantFiled: November 29, 1991Date of Patent: August 29, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Tumoru Miyamoto, Yoshinobu Arai
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Patent number: 5424474Abstract: The present invention relates to fluorinated carboxylic acid esters of phosphono- and phosphinocarboxylic acids containing hydroxyl and/or mercapto groups, their use as waterproofing and/or oil-repellency agents, and a method for their preparation.Type: GrantFiled: December 23, 1993Date of Patent: June 13, 1995Assignee: Bayer AGInventors: Klaus Pohmer, Rainer Weber, Hans-Dieter Block, Hans-Heinrich Moretto
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Patent number: 5420160Abstract: There are described new 1-alkoxyhexatriene-2-carboxylates of the formula (I) ##STR1## in which R represents substituted phenyl,and a plurality of processes for their preparation.The new 1-alkoxyhexytriene-2-carboxylates are used as pesticides.Type: GrantFiled: January 21, 1994Date of Patent: May 30, 1995Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Peter Gerdes, Heinz-Wilhelm Dehne, Stefan Dutzmann
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Patent number: 5414102Abstract: The present invention relates to fluorinated carboxylic acid esters of phosphonocarboxylic acids containing acrylate and/or methacrylate groups, their use as waterproofing or oil-repellency agents, and a method for their preparation.Type: GrantFiled: December 27, 1993Date of Patent: May 9, 1995Assignee: Bayer AktiengesellschaftInventors: Klaus Pohmer, Rainer Weber, Hans-Dieter Block, Hans-Heinrich Moretto
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Patent number: 5401882Abstract: The present invention is directed to a process for the preparation of deactivated anilines, which comprises the step of reacting a compound of formula (I) ##STR1## with a dialkylamide in the presence of a base at elevated temperature, in which:R.sub.1 is chosen from groups whose anions (R.sub.1.sup.-) constitute leaving groups;R.sub.2 and R.sub.4, which may be the same or different, are chosen from hydrogen, hydrocarbon chains, halogens and groups which are electron-attracting (EAG);R.sub.3 is chosen from hydrocarbon chains, halogens and groups which are electron-attracting, preferably through an inductive effect rather than a mesomeric effect; with the proviso that at least one of the groups R.sub.2, R.sub.3, and R.sub.4 is electron-attracting through an inductive effect.A second embodiment of the present invention is directed to a process for the dealkylation of deactivated anilines which comprises the steps of free radical halogenation of the benzyl carbon followed by hydrogenation.Type: GrantFiled: November 24, 1993Date of Patent: March 28, 1995Assignee: Rhone-Poulenc ChimieInventor: Jean-Marc Ricca
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Patent number: 5389619Abstract: Compounds of the formula I ##STR1## where n, W, X, Y, Z, R.sup.1, R.sup.2, and R.sup.3 are as defined herein exhibit fungicidal, insecticidal, and acaracidal activity.Type: GrantFiled: March 29, 1993Date of Patent: February 14, 1995Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Horst Wingert, Reinhard Kirstgen, Albrecht Harreus, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5385917Abstract: Carboxylic acid derivatives of the formula: ##STR1## are provided, which are useful for treatment of androgen dependent diseases.Type: GrantFiled: July 16, 1993Date of Patent: January 31, 1995Assignee: Mitsubishi Kasei CorporationInventors: Hiroaki Ueno, Masahiko Morioka, Fumiko Hatanaka
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Patent number: 5384399Abstract: Process for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: ##STR1## wherein R.sub.1 is aryl, heteroaryl, alkyl, alkenyl, alkynyl or OR.sub.7 wherein R.sub.7 is alkyl, alkenyl, alkynyl, aryl or heteroaryl; R.sub.2 and R.sub.5 are independently selected from hydrogen, alkyl alkenyl, alkynyl, aryl, heteroaryl, and OR.sub.8 wherein R.sub.8 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or hydroxyl protecting group; and R.sub.3 and R.sub.6 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl and heteroaryl.Type: GrantFiled: June 15, 1992Date of Patent: January 24, 1995Assignee: Florida State UniversityInventor: Robert A. Holton
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Patent number: 5384107Abstract: Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid; n is an integer from 0 to 6;R.sup.1 and R.sup.2 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy or aryloxy;R.sup.3 and R.sup.4 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, halogen, hydroxy or acylamino;Q represents the atoms necessary to complete a carbocyclic or heterocyclic unsaturated mono- or bicyclic aromatic ring; andR.sup.5 is H, alkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, halogen, hydroxy, amino, acylamino, alkoxyalkyl, fluoroalkyl, acetamidoalkyl, COO-alkyl, cyano, carboxamido, sulfonate, sulfonamido, ureido, or carbamyl are useful as contrast agents in x-ray imaging compositions and methods.Type: GrantFiled: August 3, 1994Date of Patent: January 24, 1995Assignee: Sterling Winthrop Inc.Inventors: Baldev Singh, Edward R. Bacon, Carl R. Illig
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Patent number: 5380883Abstract: A compound of the formula ##STR1##Type: GrantFiled: April 12, 1993Date of Patent: January 10, 1995Assignee: Roussel-UclafInventors: Marc Benoit, Sylvain Laugraud, Jean-Louis Brayer
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Patent number: 5374623Abstract: A method of treating medical conditions with proteinase inhibitors of the formula: ##STR1## wherein B is H or an amino acid blocking group for the N-terminal amino acid nitrogen;R.sub.1 is an optionally protected .alpha.-amino acid side chain such that P.sub.2 is the residue of an .alpha.-amino acid selected from the group consisting of phenylalanine (Phe), leucine (Leu), tyrosine (Tyr) and valine (Val), and substituted analogs thereof, particularly including Tyr(OMe);R.sub.2 is an optionally protected .alpha.-amino acid side chain such that P.sub.1 is the residue of an .alpha.Type: GrantFiled: August 20, 1992Date of Patent: December 20, 1994Assignee: Prototek, Inc.Inventors: Mary P. Zimmerman, Eugene R. Bissell, Robert E. Smith
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Patent number: 5374769Abstract: Novel polycyanate compositions containing one or more mesogenic moieties as lateral substituents are disclosed which provide improved processability relative to polycyanates containing one or more mesogenic moieties in the main chain of the molecule. Molecular level ordering of the resulting thermosets is maintained much similar to that found thermosets of polycyanates which have one or more mesogenic moieties in the main chain.Type: GrantFiled: December 24, 1992Date of Patent: December 20, 1994Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5357032Abstract: A diamine compound of the general formula ##STR1## wherein the arrows denote isomerism, R.sub.1 is a divalent aromatic group selected from the group consisting of ##STR2## R.sub.2 is a tetravalent aromatic group selected from the group consisting of ##STR3## and R.sub.4 is a monovalent aliphatic group selected from the group consisting of ethyl and isopropyl; and, a process for preparing same.Type: GrantFiled: August 17, 1992Date of Patent: October 18, 1994Assignee: Korea Research Institute of Chemical TechnologyInventors: Suh Bong Rhee, Ji Y. Chang, Bong S. Moon, Ji-Woong Park
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Patent number: 5356935Abstract: A series of dihydrophenanthreneones and tetrahydrophenanthreneones are useful as inhibitors of 5.alpha.-reductase, and a series of hexahydrophenanthreneones are useful as intermediates for preparing such pharmaceuticals.Type: GrantFiled: December 13, 1993Date of Patent: October 18, 1994Assignee: Eli Lilly and CompanyInventors: James E. Audia, Thomas C. Britton, Patrick G. Spinazze
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Patent number: 5354885Abstract: A composition which comprises a pharmaceutically acceptable carrier and an active ingredient, such active ingredient comprising L-DOPA ethyl ester in an amount which is at least 97%, by weight, of the active ingredient, and L-DOPA in an amount which is less than 1% by weight of such active ingredient is provided by this invention. This invention also provides a process for preparing such a composition. Further, this invention provides a method of treating a patient suffering from Parkinson's disease which comprises administering to a patient a pharmaceutical composition comprising a therapeutically effective amount of L-DOPA ethyl ester and a pharmaceutically acceptable carrier.Type: GrantFiled: December 24, 1992Date of Patent: October 11, 1994Assignees: Yissum Research Development Company of the Hebrew University of Jerusalem, Teva Pharmaceutical Industries Ltd.Inventors: Isaac Milman, Alexander Veinberg, Daphne Atlas, Eldad Melamed
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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: 5347036Abstract: Novel compounds which are 2,6-di-t-butylphenols substituted on the 4 position by an anilino group, which anilino group is substituted by a carboxyl substituent, a tetrazolyl substituent or an N-methyltetrazolyl substituent, are useful antiallergic agents. Pharmaceutical compositions containing and pharmacological methods of using such compounds are also disclosed, as are synthetic intermediates for preparing such compounds. Certain of the synthetic intermediates also exhibit useful antiallergic activity.Type: GrantFiled: May 26, 1993Date of Patent: September 13, 1994Assignee: Riker Laboratories, Inc.Inventor: Robert A. Scherrer
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Patent number: 5347037Abstract: A process for the preparation of a compound of formula (I) ##STR1## which is a (RR) and (RS) stereoisomer of N-(7-ethoxycarbonylmethoxy-1,2,3,4,-tetrahydronaphth-2-yl)-2-(3-chlorophen yl)-2-hydroxyethanamine and their pharmaceutically acceptable salts.Type: GrantFiled: September 1, 1993Date of Patent: September 13, 1994Assignee: SanofiInventors: Robert Boigegrain, Roberto Cecchi, Sergio Boveri
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Patent number: 5334748Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2 CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.tbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1 S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.Type: GrantFiled: September 9, 1988Date of Patent: August 2, 1994Assignee: Imperial Chemical Industries PLCInventors: Alan J. Buckley, Michael G. Huchings, Ian Ferguson, Kevin Beautement, John M. Clough, Patrick J. Crowley, Christopher R. A. Godfrey, Paul J. deFraine, Vivienne M. Anthony, Stephen P. Heaney
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Patent number: 5324747Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, n, m, o, p and q are as hereinafter set forth, and, when R.sub.2 is hydrogen, pharmaceutically acceptable salts thereof with bases, are described. The compounds of formula 1 are potent inhibitors of phospholipases A.sub.2 (PLA.sub.2 's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.Type: GrantFiled: July 15, 1992Date of Patent: June 28, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Mathew Carson, Ru-Jen L. Han, Ronald A. LeMahieu, Vincent S. Madison
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Patent number: 5312961Abstract: The invention relates to 2-amino-7-hydroxytetralin carboxyalkyl ethers of formula ##STR1## wherein Alk represents a straight or branched (C.sub.3 -C.sub.5)alkylene group, and R is hydrogen or (C.sub.1 -C.sub.4)alkyl, useful as starting materials in the synthesis of 7-substituted phenylethanolaminotetralins of formula (XII) ##STR2## wherein X represents hydrogen, halogen, (C.sub.1 -C.sub.4)alkyl, or trifluoromethyl which are useful as spasmolytics and anti-glaucoma agents.The new 7-substituted phenylethanolaminotetralins (XII) as well as the intermediates in the preparation of the compounds (I), the N-protected 2-amino-7-hydroxytetralin carboxyalkyl ethers, are also claimed.Type: GrantFiled: June 29, 1992Date of Patent: May 17, 1994Assignee: Elf SanofiInventors: Umberto Guzzi, Roberto Cecchi, Luciano Manara
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Patent number: 5310760Abstract: Certain 3,4-disubstituted anilines and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --NH.sub.2 or --NHCH.sub.3 ;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.Type: GrantFiled: July 9, 1993Date of Patent: May 10, 1994Assignee: Sterling Winthrop Inc.Inventors: William N. Washburn, Lee H. Latimer, Barbara B. Lussier, Carl R. Illig, Alexander L. Weis
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Patent number: 5310682Abstract: Compounds containing .alpha.-discarbonyl groups are rendered capable of fluorescent emission by conjugation with carboxylic acid-terminated ortho-diaminoaryl reagents. The carboxylic acid groups serve as ionizable moieties which facilitate the conjugation reaction, and are retained in the conjugation product to enable, or enhance the ability of, the conjugated compounds to be separated in chromatographic and electromigration separation processes, notably electrophoresis. Ortho-dinitro derivatives of the reagents are also disclosed, these derivatives offering the advantage of stability as well as the ability to be used directly in the reaction in the presence of a reducing agent.Type: GrantFiled: June 17, 1992Date of Patent: May 10, 1994Assignee: Indiana University FoundationInventors: Milos V. Novotny, Osamu Shirota, Donald Wiesler
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Patent number: 5298647Abstract: Aromatic compounds absorbing UVB and/or UVA, substituted with an amide function, selected from the group consisting of ##STR1## whose variable substituents are as defined in the specification, e.g. ##STR2## are useful as photoprotective agents or tanning accelerators.Type: GrantFiled: December 14, 1987Date of Patent: March 29, 1994Inventors: Dominique Robert, Louis Jung
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Patent number: 5294643Abstract: Novel cinnamamide derivatives and the salts thereof are provided. An antihyperlipidemic composition is also provided. The composition comprises an active ingredient which is at least one selected from the group consisting of the above-mentioned cinnamamide derivative and the pharmaceutically acceptable salt thereof.Type: GrantFiled: July 5, 1990Date of Patent: March 15, 1994Assignee: Kanegafuchi Kagaku Kogyo KabushikiInventors: Yoshihide Fuse, Kenji Fujii, Keiji Kameyama, Taizo Kawabe, Toshiaki Miwa, Ikuo Katsumi
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Patent number: 5292922Abstract: The invention provides N-acyl-N-phenyltetrahydrophthalamic acid derivatives represented by the general formula [I], methods of producing the same, and herbicides containing the same as the effective components, ##STR1## wherein X and Y each individually represent hydrogen atoms or halogen atoms, R.sup.1 represents a hydrogen atom, a halogen atom, a lower alkoxy group, a lower alkenyloxy group, a lower alkynyloxy group, a lower alkoxyalkoxy group or a lower alkoxycarbonylalkoxy group, R.sup.2 represents a lower alkyl group, a halogenated lower alkyl group, or a substituted or unsubstituted phenyl group, and R.sup.3 represents a lower alkoxy group, a lower alkenyloxy group, a lower alkynyloxy group, a lower alkoxyalkoxy group, a benzyloxy group or a lower alkoxycarbonylalkoxy group. The herbicides which are very useful can be widely applied to upland, paddy field, orchard, turf, forest, non-crop land, etc, and are not harmful to crops.Type: GrantFiled: April 22, 1992Date of Patent: March 8, 1994Assignee: Central Glass Company, LimitedInventors: Tetsuo Takematsu, Takashi Kume, Takeo Komata, Kiyoshi Suzuki, Matsue Minezaki, Yumiko Shirakawa, Kaoru Mori
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Patent number: 5254595Abstract: Aryloxypropanolaminotetralins with beta-antagonist activity of the formula ##STR1## wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group, in optically active or inactive form as well as their acid addition salts are described.A process for their preparation and pharmaceutical compositions containing the compounds of formula (i) or their pharmaceutically acceptable acid addition salts, are also described.Type: GrantFiled: January 9, 1992Date of Patent: October 19, 1993Assignee: Elf SanofiInventors: Umberto Guzzi, Marco Baroni, Sergio Boveri, Luciano Manara, Alberto Bianchetti
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Patent number: 5248817Abstract: A novel procedure for bromination of aromatic moieties utilizes N-bromosuccinimide or dibromodimethylhydantoin in an aqueous alkali medium. The bromination procedure is employed for the preparation of an intermediate used in the preparation of remoxipride, an antipsychotic compound.Type: GrantFiled: July 8, 1992Date of Patent: September 28, 1993Assignee: Merck & Co., Inc.Inventors: Joseph Auerbach, Steven A. Weissman
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Patent number: 5235090Abstract: A method for synthesizing 2-(4-amidophenoxy)alkanoic acids and esters and 2-(4-aminophenoxy)alkanoic acids and esters by reacting a hydroxyaromatic ketone derivative with a 2-substituted alkanoic acid or ester under basic conditions and thereafter reacting with a hydroxylamine derivative and conducting a Beckmann Rearrangement with subsequent solvolysis.Type: GrantFiled: November 19, 1992Date of Patent: August 10, 1993Assignee: Hoechst Celanese Corp.Inventor: Varadaraj Elango
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Patent number: 5235103Abstract: A process for the preparation of phenylethanolaminotetralins of formula ##STR1## wherein X is hydrogen, a halogen, a trifluoromethyl or a lower alkyl group and R.sup.o is hydrogen or a methyl group substituted by a carboxy or a lower carbalkoxy group, which comprises treating a mandelic acid with a 2-amino-7-hydroxytetralin, optionally alkylating with a lower alkyl haloacetate and reducing the amido group of the mandelamide into a methyleneamino group. The mandelamides intermediates are novel.Type: GrantFiled: December 15, 1992Date of Patent: August 10, 1993Assignee: SanofiInventors: Robert Boigegrain, Roberto Cecchi, Sergio Boveri
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Patent number: 5229107Abstract: The present invention relates to novel sunscreen agents which have the ability to absorb both UVA and UVB wavelength radiation. The sunscreen agents comprise a specific type of UVA-absorbing chromophore covalently bonded to a specific type of UVB-absorbing chromophore. The chromophore moieties are covalently bonded together such that the electron systems of these moieties are not directly coupled.The present invention further relates to sunscreen compositions containing the hereinbefore described type of sunscreen agents. Furthermore, the present invention relates to methods for protecting the skin of humans or lower animals from the effects of UVA and UVB wavelength radiation. This method comprises topically applying to the skin an effective coating of a sunscreen composition of the present invention.Type: GrantFiled: August 5, 1992Date of Patent: July 20, 1993Assignee: The Procter & Gamble CompanyInventors: Anthony D. Sabatelli, Josephine A. Spirnak
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Patent number: 5229106Abstract: The present invention relates to novel sunscreen agents which have the ability to absorb both UVA and UVB wavelength radiation. The sunscreen agents comprise a specific type of UVA-absorbing chromophore covalently bonded to a specific type of UVB-absorbing chromophore. The chromophore moieties are covalently bonded together such that the electron systems of these moieties are not directly coupled.The present invention further relates to sunscreen compositions containing the hereinbefore described type of sunscreen agents. Furthermore, the present invention relates to methods for protecting the skin of humans or lower animals from the effects of UVA and UVB wavelength radiation. This method comprises topically applying to the skin an effective coating of a sunscreen composition of the present invention.Type: GrantFiled: August 5, 1992Date of Patent: July 20, 1993Assignee: The Procter & Gamble CompanyInventors: Anthony D. Sabatelli, Josephine A. Spirnak
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Patent number: 5223639Abstract: A process for producing N-(3',4'-dimethoxycinnamoyl)-anthranilic acid, which comprises (i) allowing 3',4'-dimethoxycinnamic acid to react with anthranilic acid in an aprotic polar solvent in the presence of a particular inorganic salt and an iminium salt--which could be prepared quantitatively from dimethylformamide and an inexpensive acid halide--or (ii) allowing 3',4'-dimethoxycinnamic acid to react with an iminium salt and then with an anthranilic acid-inorganic salt complex, a novel complex not described in the literature. According to the process of this invention, the desired compound can be produced in a high yield with no substantial formation of hardly separable by-products.Type: GrantFiled: June 7, 1991Date of Patent: June 29, 1993Assignee: Kohjin Co., Ltd.Inventor: Masashi Satou
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Patent number: 5214191Abstract: 2-Phenylalkanoate esters which are useful as inhibitors of human leukocyte elastase.Type: GrantFiled: May 22, 1990Date of Patent: May 25, 1993Assignee: Cortech, Inc.Inventors: Gary P. Kirschenheuter, Lyle W. Spruce, John C. Cheronis
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Patent number: 5210276Abstract: Phenylethanolamino- and phenylethanolaminomethyltetralines of formula (I) ##STR1## wherein X represents a hydrogen atom, a halogen atom, a (C.sub.1 -C.sub.4)alkyl group or a trifluoromethyl group,A represents a bond between the --COOR group and the tetraline ring, a (C.sub.1 -C.sub.4)alkylene or a (C.sub.2 -C.sub.4)alkenylene group,R is hydrogen or a (C.sub.1 -C.sub.4)alkyl group, andn is 0 or 1and their salts, are typically prepared by reaction of an epoxide of formula (IIa) ##STR2## with a tetraline derivative of formula (III) ##STR3## wherein A and n are as defined above and R' is a (C.sub.1 -C.sub.4)alkyl group, optionally followed by basic hydrolysis to obtain the compounds (I) wherein R is hydrogen.The new compounds show very interesting properties as antidepressant and intestinal spasmolytic agents.The new intermediates of formula (III) are also claimed.Type: GrantFiled: February 18, 1992Date of Patent: May 11, 1993Assignee: Elf SanofiInventors: Domenico Badone, Umberto Guzzi, Roberto Cecchi
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Patent number: 5202466Abstract: 2-amino-7-hydroxytetraline ethers of formula ##STR1## wherein R' represents methyl substituted by a carboxy group or lower carbalkoxy group or a salt thereof; a process for their preparation starting from the 2-amino-7-hydroxytetraline, N-protection, O-alkylation and N-deprotection; N-protected intermediates; and use of the compounds I for the preparation of the corresponding phenylethanolaminotetralines.Type: GrantFiled: July 31, 1992Date of Patent: April 13, 1993Assignee: SanofiInventors: Robert Boigegrain, Roberto Cecchi, Sergio Boveri
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Patent number: 5198586Abstract: A process for the preparation of phenylethanolaminotetralins of formula ##STR1## wherein X is hydrogen, a halogen, a trifluoromethyl or a lower alkyl group and R.degree. is hydrogen or a methyl group substituted by a carboxy or a lower carbalkoxy group, which comprises treating a mandelic acid with a 2-amino-7-hydroxytetralin, optionally alkylating with a lower alkyl haloacetate and reducing the amido group of the mandelamide into a methyleneamino group. The mandelamides intermediates are novel.Type: GrantFiled: October 25, 1990Date of Patent: March 30, 1993Assignee: SanofiInventors: Robert Boigegrain, Roberto Cecchi, Sergio Boveri
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Patent number: 5191113Abstract: A cinnamoylamide derivative of general formula: ##STR1## [wherein, (i) in case that R.sup.2 represents a methyl group and R.sup.3 represents a hydrogen atom,(R.sup.1).sub.n represents a group selected out of3-pentyl group,4-pentyl group,4-neopentyl group,4-(2-ethylbutyl) group,4-(2-methylpentyl) group,2-fluoro-4-pentyloxy group,4-butylthio group,4-cyclobutylmethyl group,4-cyclohexylmethyl group,4-(4-phenylbutyl) group and4-phenoxy group, and(ii) in case that R.sup.2 represents a hydrogen atom and R.sup.3 represents a methyl group,(R.sup.1).sub.n represents a group selected out of3-pentyl group and4-phenethyl group.]or non-toxic salts thereof possess an inhibitory activity on 5.alpha.-reductase, and therefore be useful for treating and/or preventing agent for alopecia, acnes or prostatic hypertrophy.Type: GrantFiled: December 5, 1991Date of Patent: March 2, 1993Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Hiroshi Terashima, Yoshinobu Arai
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Patent number: 5189063Abstract: Pesticidal substituted acrylic esters of the formula ##STR1## in which R.sup.1 represents alkyl, or represents unsubstituted or substituted aralkyl,R.sup.2 represents dialkylamino, or represents a radical --Z--R.sup.3,R.sup.3 represents alkyl, or represents unsubstituted or substituted aralkyl,Z represents oxygen or sulphur,A represents ##STR2## where n represents a number from 0 to 6,R.sup.4 and R.sup.5 in each case independently of one another represent alkyl, or together represent an alkylene chain having 2 to 7 carbon atoms, andR.sup.6 represents alkyl, or represents a radical ##STR3## where R.sup.7 represents alkyl, alkoxy or dialkylamino,B represents the group CH--R.sup.8 or, whereR.sup.9 represents unsubstituted or substituted alkyl, alkenyl, alkynyl, aralkyl, aryl or hetaryl, andR and Q independently of one another represent hydrogen, alkyl, halogenoalkyl or alkoxy.Type: GrantFiled: August 17, 1990Date of Patent: February 23, 1993Assignee: Bayer AktiengesellschaftInventors: Alexander Klausener, Herbert Gayer, Wolfgang Kramer, Dieter Berg, Wilhelm Brandes, Gerd Hanssler, Ulrike Wachendorff-Neumann
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Patent number: 5183924Abstract: Derivatives of benzocycloalkenyldihydroxyalkanoic acids, inhibitors of HMG CoA reductase, antagonists of thromboxane A.sub.2 receptors and antifungals, denoted by the formula I ##STR1## in which X=CH.sub.2, O or S; R.sub.1 and R.sub.2, identical or different, =H, C.sub.1-3 alkyl or together form a --(CH.sub.2).sub.n -- chain (n=4,5) optionally substituted symmetrically by one or two C.sub.1-3 alkyl radicals.R.sub.3 and R.sub.4, identical or different, =H, CF.sub.3, halogen (Cl, F, Br), C.sub.1-5 N,N-dialkylamino, C.sub.1-4 alkyl, C.sub.1-5 -alkoxy, C.sub.1-3 alkylthio, or phenyl optionally substituted by at most substituents which may be identical or different and may denote C.sub.1-3 alkyl or C.sub.1-3 alkoxy radicals or halogens (F, Cl), it being understood that when one of R.sub.3 and R.sub.4 denotes the radicals: CF.sub.3, N,N-dialkylamino, C.sub.6 H.sub.5 or substituted phenyl, it is present at the vertices 3', R' or 5' according to formula 1 and the other denotes a hydrogen atom.R.sub.5 and R.sub.Type: GrantFiled: October 24, 1991Date of Patent: February 2, 1993Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Didier Festal, Jean-Yves Nioche, Denis Descours, Robert Bellemin, Jacques Decerprit
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Patent number: 5177222Abstract: 1,1-Dialkoxy-2-oxo-6-aryl-3,5-alkadienes of the general formula I ##STR1## where Ar is a phenyl, biphenyl or naphthyl radical which may be substituted by one, two or three C.sub.1 -C.sub.4 -alkyl groups, C.sub.1 -C.sub.4 -alkoxy groups, hydroxyl groups, phenoxy groups, amino groups which may be mono- or di-C.sub.1 -C.sub.4 -alkyl-substituted, halogen atoms or a methylenedioxy group, the substituents being identical or different,R.sup.1 is hydrogen or C.sub.1 -C.sub.8 -alkyl,R.sup.2 is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.10 -alkoxycarbonyl or C.sub.1 -C.sub.10 -acyl,the radicals R.sup.3 are C.sub.1 -C.sub.8 -alkyl groups which may be bonded to one another with formation of a five-membered or six-membered ring andR.sup.4 is hydrogen or C.sub.1 -C.sub.4 -alkyl, are used as sunscreen agents in cosmetic preparations.Type: GrantFiled: November 5, 1990Date of Patent: January 5, 1993Assignee: BASF AktiengesellschaftInventors: Helmut Guembel, Joachim Paust, Karin Sperling-Vietmeier, Rainer Becker
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Patent number: 5175170Abstract: Non-peptidyl compounds characterized generally as cycloalkyl/cycloalkylkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest of the formula ##STR1## wherein R.sub.1 is selected from cycloalkyl and cycloakylalkyl groups, wherein said cycloalkyl group contains three to about eight carbon atoms and the acyclic alkyl portion of said cycloakylalkyl group contains one to about eight carbon atoms; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; and wherein R.sub.7 is isobutyl or ethyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: July 29, 1991Date of Patent: December 29, 1992Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran, Dave Weissing, Mark Russell
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Patent number: 5164388Abstract: A renin inhibiting compound of the formula ##STR1## wherein X is N, O or CH; R.sub.1 is absent or a functional group; A and L are independently selected from absent, C.dbd.O, SO.sub.2 and CH.sub.2 ; D is C.dbd.O, SO.sub.2 or CH.sub.2 ; Y is N or CH; R.sub.2 is hydrogen, loweralkyl or substituted alkyl; Z is a functional group; R.sub.3 is loweralkyl or substituted alkyl; n is 0 or 1; and T is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.Type: GrantFiled: April 18, 1991Date of Patent: November 17, 1992Assignee: Abbott LaboratoriesInventors: Biswanath De, Thomas N. Zydowsky, William R. Baker, Joseph F. Dellaria, Saul H. Rosenberg, Hwan S. Jae
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Patent number: 5162571Abstract: Novel phenol derivatives of the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, Y and n are as defined in the specification, which have therapeutic and prophylactic activities against cerebral, cardiac, renal and pulmonary circulatory system diseases, respiratory diseases, allergy, anaphylactic shock, endotoxin shock, inflammation and the like as well as inhibiting activities against vascularization by oncocytes.Type: GrantFiled: June 8, 1988Date of Patent: November 10, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Kohei Mishikawa
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Patent number: 5159103Abstract: 2-amino-7-hydroxytetraline ethers of formula ##STR1## wherein R' represents methyl substituted by a carboxy group or lower carbalkoxy group or a salt thereof; a process for their preparation starting from the 2-amino-7-hydroxytetraline, N-protection, O-alkylation and N-deprotection; N-protected intermediates; and use of the compounds I for the preparation of the corresponding phenylethanolaminotetralines.Type: GrantFiled: January 28, 1992Date of Patent: October 27, 1992Assignee: SanofiInventors: Robert Boigegrain, Roberto Cecchi, Sergio Boveri