Plural Rings In Alcohol Moiety Patents (Class 560/255)
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Patent number: 6162445Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (I): in which X is one of the radicals: ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: October 6, 1997Date of Patent: December 19, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6159988Abstract: Compounds of formula I, ##STR1## and the physiologically tolerable salts thereof, wherein the substituents R.sub.1 -R.sub.4 have the meanings given in the specifications and show an activity against inflammatory conditions.Type: GrantFiled: June 29, 1998Date of Patent: December 12, 2000Assignee: Hoeschst AktiengesellschaftInventors: Ramachandra Ganapati Naik, Vilas Narayan Mumbaikar, Ravishankar Vasumathy, Aftab Dawoodbhai Lakdawala, Mandakini Bipin Alreja, Bansi Lal, Jurgen Blumbach, Klaus Ulrich Weithmann, Robert Ryder Bartlett, Kalpana Sanjay Joshi, Swati Bal-Tembe, Sadagopan Raghavan
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Patent number: 6143922Abstract: The present invention relates to a novel composition of diols, said composition of diols comprisingHO--(H.sub.3 C)R.sup.4 C--Q--CR.sup.5 (CH.sub.3)--OHwherein Q is a diaryl group comprising two aryl groups linked together directly (as in biphenyl) or bridged by an oxygen atom, sulfur atom or methyl group,R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen and lower alkyl groups (e.g., methyl, ethyl, propyl and butyl, most preferably methyl). The diols will usually be provided as compositions which comprise either:a solution of the diols, with the diols comprising more than 99% by weight solids of the solution, and whichdiol has less than 1% by weight of impurity selected from the group consisting essentially of monoaryl hydroxy compounds, especially monoaryl monohydroxy compounds, and monoaryl dihydroxy compounds where only one hydroxy group is attached directly to the aryl ring.Type: GrantFiled: October 7, 1998Date of Patent: November 7, 2000Inventor: Boris A. Zaitsev
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Patent number: 6083986Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.Type: GrantFiled: July 15, 1997Date of Patent: July 4, 2000Assignees: ICAgen, Inc., Eli Lilly & CompanyInventors: Neil Alexander Castle, Sean Patrick Hollinshead, Philip Floyd Hughes, Jose Serafin Mendoza, Joseph Wendell Wilson, George Salvatore Amato, Serge Beaudoin, Michael Gross, Grant McNaughton-Smith
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Patent number: 6080739Abstract: The present invention relates to colchicine and thiocolchicine derivatives which can be obtained from these molecules by functionalization of the C-7 to ketone or functionalization of the amino group. Said compounds have a marked antiblastic activity both on the normal cancer cells and on the chemoresistant phenotype. The compounds of the invention can be administered both by injection and orally.Type: GrantFiled: November 24, 1998Date of Patent: June 27, 2000Assignee: Indena S.p.A.Inventor: Ezio Bombardelli
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Patent number: 6046354Abstract: A novel glycerol derivative, a process for preparing the same, and a process for preparing a triazole derivative. An optically active 2-arylglycerol derivative which is novel and useful as a synthetic intermediate of medicament is provided, and furthermore, (R)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazole-1-yl)-propane-1,2-diol, which is useful as an antifungal agent, is prepared.Type: GrantFiled: August 31, 1998Date of Patent: April 4, 2000Assignee: Kanegafuchi Kagaku Kogyo Kabushiki KaishaInventors: Yoshihiko Yasohara, Kenji Miyamoto, Noriyuki Kizaki, Shigeru Kawano, Junzo Hasegawa
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Patent number: 6040470Abstract: There is provided a developer composition including at least one of sulfonyl compounds represented by formula (1) and at least one of sulfonyl compounds represented by formula 2: ##STR1## wherein X is H or lower alkyl, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 which may be the same or different, present H, halogen or lower alkyl and Y represents alkyl, benzenesulfonyl, benzoyl et al, A thermalsensitive recording medium having the above developer is of high sensitivity, less surface-blushing with lapse of time and is excellent in storage stability of a recorded image, particularly in heat resistance, humidity resistance and anti-plasticizer.Type: GrantFiled: September 10, 1998Date of Patent: March 21, 2000Assignee: Sanko Kaihatsu Kagaku KenkyushoInventors: Shigeru Oda, Eiji Kawabata
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Patent number: 6037059Abstract: Novel dibenzoylresorcinol compositions capable of absorbing ultraviolet light having the formula ##STR1## where Ar.sub.1 and Ar.sub.2 are independently substituted or unsubstituted monocyclic or polycyclic aryl groups, R is hydrogen, an aryl group, or a linear or branched alkyl chain having less than about 10 carbons, and Ar.sub.3 is an aryl group bearing at least one hydroxyl group. Methods of making the compositions are provided. The novel dibenzoylresorcinol compositions are methylene-bridged dibenzoylresorcinol derivatives having a phenol group on the bridging methylene and are compatible in coating compositions to improve the weatherability of thermoplastic substrates.Type: GrantFiled: October 23, 1998Date of Patent: March 14, 2000Assignee: General Electric CompanyInventors: James Edward Pickett, Amy Kathleen Simonian
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Patent number: 6025328Abstract: The present invention provides illudin analogs of the general formula I: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.Type: GrantFiled: February 20, 1998Date of Patent: February 15, 2000Assignee: The Regents of the University of CaliforniaInventors: Trevor C. McMorris, Michael J. Kelner
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Patent number: 5942290Abstract: Molecular complex compounds comprising a mono-, bis- or trisacylphosphine oxide compound with an .alpha.-hydroxy ketone compound are suitable as photoinitiators for the photopolymerization of free-radically polymerizable compounds.Type: GrantFiled: August 21, 1997Date of Patent: August 24, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: David George Leppard, Thomas Lloyd James, Nils Hock, Manfred Kohler, Ronald Salathe
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Patent number: 5883235Abstract: Calix?4!arene compounds are disclosed that can be used as active components in a calcium sensitive sensor. The compounds exhibit strong calcium ion binding selectivity over sodium and potassium ions and they are stable during sterilization.Type: GrantFiled: October 14, 1997Date of Patent: March 16, 1999Assignee: Radiometer Medical A/SInventors: Allan Milton Byrnard, Rocco Ungaro, Andrea Pochini
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Patent number: 5874611Abstract: A hydroquinone derivative (I) represented by the following formula: ##STR1## wherein R.sup.1 is a hydrogen atom, acetyl group or benzoyl group, such hydroquinone derivative being useful as an intermediate for chroman derivatives useful as a blood sugar-lowering agent.Type: GrantFiled: July 1, 1996Date of Patent: February 23, 1999Assignee: Eisai Chemical Co., Ltd.Inventors: Kimio Hamamura, Chiaki Seki, Masayuki Konishi
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Patent number: 5856490Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: September 4, 1997Date of Patent: January 5, 1999Assignee: AllerganInventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 5808137Abstract: The present invention relates to the use of some natural or synthetic chalcones and the esters thereof with straight or branched aliphatic acids, saturated and unsaturated, containing up to 22 carbon atoms in the therapy and prevention of the uterus, ovary and breast tumors, as well as the formulations containing them. Chalcones such as isocordoin, cordoin, 2-hydroxyderricin, 2',4'-dihydroxychalcone, 4,2',4'-trihydroxychalcone have a marked affinity to the estrogen receptors of type II and an antiproliferative activity on uterus, ovary and breast tumor cell lines. These molecules proved to be useful both in therapy and in the prevention of such tumors.Type: GrantFiled: June 12, 1997Date of Patent: September 15, 1998Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Salvatore Mancuso, Franco Delle Monache
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Patent number: 5789413Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: January 21, 1997Date of Patent: August 4, 1998Assignee: Merck Frosst Canada, Inc.Inventors: Cameron Black, Erich Grimm, Serge Leger, Greg Hughes, Petpiboon Prasit, Zhaoyin Wang
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Patent number: 5763719Abstract: A fullerene derivative of the formula I ##STR1## where the symbols and indices have the following meanings: F is a fullerene radical of the formula (C.sub.20+2m), where m is a number from 1 to 50R.sup.1 to R.sup.8 are identical or different and are each H, CO.sub.2 R.sup.9, CN, COR.sup.10, Cl, Br, I, F, OR.sup.11, C.sub.1 -C.sub.20 -alkyl, phenyl or H, R.sup.1 -R.sup.4 and/or R.sup.5, R.sup.7 can also be part of a cycloalipathic, cycloaromatic or cycloheteroaromatic system which in turn is substituted by C.sub.1 -C.sub.20 -alkyl, aryl, carboxyl, carbonyl, alkoxy, aryloxy, halogen, nitro, alcohol or amine, or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, R.sup.3 and R.sup.4 can together be ##STR2## where R.sup.15 -R.sup.18 are each H, C.sub.1 -C.sub.20 -alkyl, F, Cl, Br, I or phenyl, andAR is the radical of a fused cyclo-aromatic system, and n is from 1 to 20 and a process for its preparation.Type: GrantFiled: September 15, 1995Date of Patent: June 9, 1998Assignee: Hoechst AGInventors: Andreas Gugel, Pavel Belik, Klaus Mullen
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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: 5705659Abstract: Intermediate compounds represented as formula (I) useful for the synthesis of 16-phenoxy-prostatrienoic acid derivatives and a preparing method thereof are disclosed. ##STR1## wherein R is tetrahydropyranyl, tetrahydrofuranyl, 2-ethoxyethyl, t-butyldimethylsilyl, triisopropylsilyl or triethylsilyl group; R.sup.1 and R.sup.2 are independently hydrogen or ester-forming group; P is hydrogen, trimethylsilyl or tri-n-butyltin; and wavy line means epi-stereoisomeric mixture.Type: GrantFiled: June 20, 1996Date of Patent: January 6, 1998Assignee: Korea Institute of Science and TechnologyInventors: Hokoon Park, Sun Ho Jung, Yong Sup Lee, Ki Hong Nam
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Patent number: 5693251Abstract: An optically active phenol useful in the preparation of liquid crystalline compounds which is represented by the formula (V): ##STR1## wherein R.sub.2 represents an alkyl or alkoxyalkyl group having 1 to 20 carbon atoms optionally substituted by halogen atoms; Z' represents ##STR2## wherein q represents a number of 1 to 5 and * indicates asymmetric carbon atom; l represents a number of 2; t represents a number of 1 to 5; s represents a number of 0 or 1.Type: GrantFiled: November 23, 1994Date of Patent: December 2, 1997Assignee: Sumitomo Chemical Company, LimitedInventors: Takayuki Higashii, Isao Kurimoto, Shoji Toda, Masayoshi Minai, Takeshi Tani, Chizu Kawakami, Koichi Fujisawa
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Patent number: 5684198Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof,which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.Type: GrantFiled: August 23, 1996Date of Patent: November 4, 1997Assignee: Imperial Chemical Industries, PLCInventors: Keith Russell, Cyrus John Ohnmacht, Keith Hopkinson Gibson
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Patent number: 5665773Abstract: Disclosed is the use of cloprostenol and fluprostenol analogues for the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic compositions comprising said compounds.Type: GrantFiled: December 18, 1996Date of Patent: September 9, 1997Assignee: Alcon Laboratories, Inc.Inventors: Peter G. Klimko, John E. Bishop, Verney L. Sallee, Paul W. Zinke
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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: 5574036Abstract: Novel pharmaceutically/cosmetically-active adamantyl-substituted polycyclic acetylene compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(f): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: April 26, 1995Date of Patent: November 12, 1996Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, Bruno Charpenter
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Patent number: 5563176Abstract: Antineoplastic illudin analogs are provided of the formula: wherein R.sub.4, R.sub.5 and R.sub.6 are (C.sub.1 -C.sub.4)alkyl, Y is H, (C.sub.1 -C.sub.3)alkyl, (R.sub.4)R.sub.5)(R.sub.6)Si or alkanoyl ((C.sub.1 -C.sub.4)alkylC(O)) and R is CH.sub.2 OH, halo, benzyl optionally substituted with OY, or alkanoylmethyl (CH.sub.2 OC(O)R.sub.7), wherein R.sub.7 is (C.sub.1 -C.sub.4)alkyl, (C.sub.6 -C.sub.2)aryl or N(X).sub.2, wherein each X is H or (C.sub.1 -C.sub.4)alkyl, and the pharmaceutically-acceptable salts thereof.Type: GrantFiled: July 15, 1994Date of Patent: October 8, 1996Assignee: The Regents of the University of CaliforniaInventors: Michael J. Kelner, Trevor C. McMorris, Raymond Taetle
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Patent number: 5563292Abstract: Novel compounds of Formula 1 ##STR1## or a pharmaceutically acceptable salt or solvate thereof are disclosed. Also disclosed are pharmaceutical compositions containing compounds of Formula 1. Methods of treating allergy, inflammation and hyperproliferative skin diseases with compounds of Formula 1 are also disclosed.Type: GrantFiled: April 2, 1992Date of Patent: October 8, 1996Assignee: Schering CorporationInventors: Neng-Yang Shih, Pietro Mangiaracina
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Patent number: 5514825Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 10 carbons; R.sub.2 and R.sub.3 are hydrogen, or alkyl of 1 to 6 carbons and the substituted ethynyl group occupies either the 2 or the 3 position of the tetrahydronaphthalene nucleus; m is an integer having the value of 0-3; o is an integer having the value 0-4; Y is a phenyl group, or heteroaryl selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.2 groups; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, 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.13 O, --COR.sub.7, CR.sub.Type: GrantFiled: December 29, 1994Date of Patent: May 7, 1996Assignee: Allergan, Inc.Inventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Tien T. Duong, Yuan Lin, Roshantha A. Chandraratna
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Patent number: 5434295Abstract: The present invention provides certain novel 4-phenylpinene derivatives, and teaches how to use said novel derivatives and related compounds in pharmaceutical compositions that have utility in treating various pathological conditions associated with damage to the central nervous system. The active ingredient of the pharmaceutical compositions according to the present invention is a compound of the formula: ##STR1## wherein A - - - B designates an optional double bond, R.sub.1 designates a variety of organic moieties, G designates alkyl, halogen, or various oxy groups, and R.sub.3 designates various alkyl groups, ether groups, or combinations thereof.Type: GrantFiled: February 7, 1994Date of Patent: July 18, 1995Assignees: Yissum Research Development Company, Pharmos Corp.Inventors: Raphael Mechoulam, Aviva Breuer, Anat Biegon
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Patent number: 5405948Abstract: A compound of formula (I): selected from 1,5-diyne-3-cyclodecene and undecene compounds. ##STR1## in which: R represents a hydrogen atom, a straight-chain or branched (C.sub.1 -C.sub.6) acyl radical or a glycoside radical,R' represents a hydrogen atom ##STR2## n is 1 or 2, and R.sub.1 and R.sub.2 simultaneously represent two hydrogen atoms or, together with the two carbon atoms and the double bond to which they are attached, form a phenyl ring.Type: GrantFiled: September 30, 1992Date of Patent: April 11, 1995Assignee: Adir et CompagnieInventors: Jean-Marie Beau, Christophe Crevisy, Ghanem Atassi, Alain Pierre
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Patent number: 5382598Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolyzable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.Type: GrantFiled: September 24, 1993Date of Patent: January 17, 1995Assignees: Imperial Chemical Industries PLC, Imperial Chemical HouseInventors: Russell Keith, Cyrus J. Ohnmacht, Keith H. Gibson
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Patent number: 5326902Abstract: Oxyalkyne compounds corresponding to the formula I ##STR1## in which the substituent Y in the meta- or para-position is R.sup.1 represents CH.sub.3 or NH.sub.2, R.sup.2 represents H or CH.sub.3, R.sup.3 represents H, C.sub.1-3 -alkyl or COCH.sub.3, and Ar represents an aromatic residue selected from the group ##STR2## with the proviso that the substituents R.sup.4, R.sup.5 and R.sup.6 are the same or different and each substituent represents H, F, Cl, Br, C.sub.1-6 -alkyl, CF.sub.3 or C.sub.1-6 -alkoxy, and R.sup.7 represents H, F, Cl, Br, C.sub.1-3 -alkyl or CF.sub.3,in the form of their racemates or mixtures of diastereoisomers or in optically active form, which are suitable active ingredients in pharmaceutical compositions.Type: GrantFiled: March 24, 1993Date of Patent: July 5, 1994Assignee: Gruenenthal GmbHInventors: Ulrich Seipp, Werner Vollenberg, Werner Englberger, Cornelia Geist, Michael Haurand
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Patent number: 5321044Abstract: 15,16-Seco-19-nor progestins are provided which display elevated progestational activity with a minimum of ancillary hormonal activity. Processes for the preparation of the novel progestins are provided as are methods of use. A preferred method of use is in the suppression of ovulation in the human female.Type: GrantFiled: May 4, 1992Date of Patent: June 14, 1994Assignee: SRI InternationalInventors: Richard H. Peters, Masato Tanabe
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Patent number: 5286750Abstract: Unsaturated phenylacetic acid derivatives of the general formula ##STR1## where U is .dbd.O, .dbd.CH--OCH.sub.3, .dbd.N--OCH.sub.3, .dbd.N--NH--CH.sub.3, .dbd.CH.sub.2, .dbd.CH--CH.sub.3, .dbd.CH--CH.sub.2 --CH.sub.3 or .dbd.CH--S--CH.sub.3 andZ.sup.1 and Z.sup.2 are hydrogen, halogen, trifluoromethyl, cyanide, NO.sub.2 or unsubstituted or substituted alkyl, alkenyl, aryl, alkynyl, alkoxy, aryloxy, arylalkoxy, acyloxy, hetaryl, --CO.sub.2 R.sup.1, --CONR.sup.2 R.sup.3, COR.sup.4 or NR.sup.5 R.sup.6, and Z.sup.1 and Z.sup.2 may also form a ring,A is meta or para and is (CH.sub.2).sub.n, CH.dbd.CH, O--(CH.sub.2).sub.n, O--(CH.sub.2).sub.n --CO, CH.sub.2 --O--CO--(CH.sub.2).sub.n, CO--O--(CH.sub.2).sub.n, O--CO--(CH.sub.2).sub.n, O--(CH.sub.2).sub.n --CO--O, O--(CH.sub.2).sub.n+2 --O, CH.sub.2 O--(CH.sub.2).sub.n, CH.sub.2 --S--(CH.sub.2).sub.n CH.sub.2 --NR.sup.7 --(CH.sub.2).sub.n, CH(CN)--O--CO--(CH.sub.2).sub.n, CH.dbd.N--(CH.sub.2).sub.n or CH.dbd.N--O--(CH.sub.2).sub.n.Type: GrantFiled: March 15, 1993Date of Patent: February 15, 1994Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz, Franz Roehl
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Patent number: 5266235Abstract: A phenylbicyclohexanol ester derivative which is a nematic liquid crystal compound having a weakly positive dielectric anisotropy is disclosed. This compound has a high N-I point and yet a low .DELTA.n value. When mixed with other nematic liquid crystal compound(s), it can give a liquid crystal display cell material having excellent visual properties and high-temperature driving properties.Type: GrantFiled: March 18, 1992Date of Patent: November 30, 1993Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Haruyoshi Takatsu, Kiyofumi Takeuchi, Yuji Tamura
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Patent number: 5208333Abstract: (2R)-1-(Aryloxy)-3-(butyryloxy)-2-propanols of the general formula (I), ##STR1## where Ar is a monocyclic or polycyclic aromatic or heteroaromatic radical, and a process for their preparation by the reaction of (2R)-glycidyl butyrate with an aromatic hydroxy compound Ar--OH in the presence of a quaternary ammonium halide.Type: GrantFiled: December 9, 1988Date of Patent: May 4, 1993Assignee: BASF AktiengesellschaftInventors: Axel Paul, Wolfgang Ladner, Hardo Siegel
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Patent number: 5192817Abstract: Novel phenanthrene derivatives represented by the general formula (1), ##STR1## wherein the group of the formula ##STR2## is a group of the formula ##STR3## (wherein R.sup.1 is a hydrogen atom or a lower alkyl group), a group of the formula ##STR4## (wherein R.sup.2 is a hydrogen atom or a lower alkanoyl group) or a group of the formula ##STR5## (wherein R.sup.2 is the same as defined above), and salts thereof, and other compounds derived therefrom and salts thereof; processes for preparing the same; and interleukin-1 (IL-1) inhibitors containing the abovementioned novel phenanthrene derivatives as to the active ingredient(s).Type: GrantFiled: November 5, 1991Date of Patent: March 9, 1993Assignees: Otsuka Pharmaceutical Co., Ltd., Otsuka Pharmaceutical Factory, Inc.Inventors: Yoshihisa Takaishi, Kiyoto Goto, Takuji Uesako, Toshiko Kuwahara, Masaaki Takai, Yukihisa Ono, Yoshihiro Taniguchi, Sachiko Manabe, Takahiro Asakuni
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Patent number: 5164515Abstract: A novel class of protecting compounds, particularly for amino acids, is based on 2,2 di nitrophenyl ethan- groups, particularly the groups wherein the nitro is in the para position. The ethyl group may be substituted, e.g. by an alkyl group, in the l- position. Preferred compounds include the alcohol or halide which are suitable for protecting acid functional groups, and esters, including activated and substituted esters, particularly the succinimidyl ester, for protecting amine groups. The invention includes methods of manufacture and use, together with protected amino acids.Type: GrantFiled: February 20, 1990Date of Patent: November 17, 1992Assignee: Wendstone Chemicals PLCInventor: Robert Ramage
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Patent number: 5152920Abstract: A phenylbicyclohexanol ester derivatives which is a nematic liquid crystal compound having a weakly positive dielectric anisotropy is disclosed. This compound has a high N-I point and yet a low .DELTA.n value. When mixed with other nematic liquid crystal compound(s), it can give a liquid crystal display cell material having excellent visual properties and high-temperature driving properties.Type: GrantFiled: July 19, 1989Date of Patent: October 6, 1992Assignee: Dainippon Ink & Chemicals, Inc.Inventors: Haruyoshi Takatsu, Kiyofumi Takeuchi, Yuji Tamura
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Patent number: 5151548Abstract: Benzene derivatives of the general formula ##STR1## where Hal is halogen, R.sup.1 is a hydrocarbon radical of 1 to 18 carbon atoms, R.sup.2 is hydrogen or alkyl of 1 to 6 carbon atoms and X is hydrogen or halogen, are prepared by a process in which a toluene derivative of the general formula ##STR2## is electrochemically oxidized in the presence of an acid of the formula R.sup.2 --COOH (III). Novel benzene derivatives of the general formula ##STR3## where R.sup.3 is hydrogen or an R.sup.2 --CO-- radical but R.sup.1 cannot be methyl if X is hydrogen, and of the general formula ##STR4## where R.sup.4 is a branched or cyclic alkyl radical of 3 to 12 carbon atoms, but R.sup.4 cannot be isopropyl if X is hydrogen. The compounds of formulas IV and VI are intermediates for crop protecting agents, e.g. pyrethroids.Type: GrantFiled: June 12, 1989Date of Patent: September 29, 1992Assignee: BASF AktiengesellschaftInventors: Dieter Hermeling, Dieter Degner, Albrecht Harreus, Norbert Goetz, Jochen Wild, Hans Theobald, Bernd Wolf
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Patent number: 5149711Abstract: A 2-cyclopentenone derivative represented by the following formula ##STR1## wherein R.sup.1 represents an alkyl group having 1 to 10 carbon atoms which may be substituted by a substituted or unsubstituted phenyl or phenoxy group, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and each represents a hydrogen atom or a lower alkanoyl group, and the wavy line shows that the bonded state of the double bond is E or Z.This compound is useful for treating, for instance, malignant tumors.Type: GrantFiled: March 7, 1989Date of Patent: September 22, 1992Assignee: Teijin LimitedInventors: Atsuo Hazato, Seizi Kurozumi
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Patent number: 5130306Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by structural formulae (I) or (II): ##STR1## wherein position 5 of the polyhydronaphthyl ring is singly or doubly bonded to oxygen or incorporated into a C.sub.3-7 carbocyclic ring.Type: GrantFiled: June 6, 1990Date of Patent: July 14, 1992Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman
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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: 5126371Abstract: Novel diarylacetylenes of the formula I ##STR1## where A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meanings stated in the description, are useful for the treatment of disorders.Type: GrantFiled: August 20, 1990Date of Patent: June 30, 1992Assignee: BASF AkteingesellschaftInventors: Hans-Heiner Wuest, Fritz-Frieder Frickel, Axel Nuerrenbach
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Patent number: 5116869Abstract: 2-Substituted-2-cyclopentenones represented by the formula (I): ##STR1## wherein A is a hydroxyl group or ##STR2## and B is a hydrogen atom or A and B are bonded together to form one bonding arm;R.sup.1 represents a substituted or unsubstituted hydrocarbon group having 1 to 10 carbon atoms;R.sup.2 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms;R.sup.3 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms; wherein,when R.sup.3 is a single bond bonded to the cyclopentene skeleton, X represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; andwhen R.sup.3 is a double bond bonded to the pentene skeleton, X represents a bonding arm constituting a part of said double bond; andm and n independently represent 0, 1 or 2.Type: GrantFiled: September 3, 1991Date of Patent: May 26, 1992Assignee: Teijin LimitedInventors: Satoshi Sugiura, Atsuo Hazato, Toru Minoshima, Yoshinori Kato, Yasuko Koshihara, Seizi Kurozumi
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Patent number: 5105020Abstract: The invention concerns a cycloalkane derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl;A.sup.1 is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;Ar.sup.2 is optionally substituted phenylene, or a 6 membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted banzoyl; andR.sup.2 and R.sup.3 together form a (3-6C)alkylene group which defines an optionally substituted ring having 4 to 7 ring atoms; or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: December 22, 1989Date of Patent: April 14, 1992Assignees: Imperial Chemistries Industries PLC, ICI PharmaInventor: Jean-Marc M. M. Girodeau
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Patent number: 5091565Abstract: New poly-dicarboxylic acid anhydrides, which are suitable as bio-degradable matrix materials for the controlled release of medicinal agents in humans.Type: GrantFiled: August 21, 1990Date of Patent: February 25, 1992Assignee: Sandoz Ltd.Inventor: Gerd Ziegast
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Patent number: 5089635Abstract: 13-alkyl-11.beta.-phenyl-gonanes of general formula I ##STR1## wherein A and B together stand for an oxygen atom, a CH.sub.2 group or a second bond between carbon atoms 9 and 10,X is an oxygen atom or the hydroxyimino grouping N.about.OH,R.sub.1 is a straight-chained or branched, saturated or unsaturated alkyl radical with up to 8 carbon atoms, which contains the grouping ##STR2## with X as described above, R.sub.2 is a methyl or ethyl radical in the .alpha. or .beta. position,R.sub.9, R.sub.10, R.sub.11 and R.sub.12 each stand for a hydrogen atom, a hydroxy, alkyl, alkoxy or acyloxy group with 1 to 4 carbon atoms respectively or a halogen atom and R.sub.3 and R.sub.4 have a variety of meanings, have antigestagenic and antiglucocorticoid effects.Type: GrantFiled: February 7, 1986Date of Patent: February 18, 1992Assignee: Schering AktiengesellschaftInventors: Gunter Neef, Sybille Beier, Walter Elger, David Henderson, Eckard Otto, Ralph Rohde
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Patent number: 5079245Abstract: The compounds 2-trifluoromethyl-7-substituted-6,7,8,9-tetrahydro-[5H]-benzocycloheptenes are disclosed and disclosed to be useful in the treatment of metabolic illnesses such as diabetes, obesity, and their complications. A perferred compound is 2-trifluoromethyl-7-amino-6,7,8,9-tetrahydro-[5H-benzocycloheptane.Type: GrantFiled: July 5, 1989Date of Patent: January 7, 1992Assignee: Adir et CompagnieInventors: Michel Wierzbicki, Pierre Hugon, Jacques Duhault, Francoise Lacour
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Patent number: 5072034Abstract: 4-alkoxy-2-hydroxybenzophenone-5-sulfonic acids of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.20 -alkyl which is unsubstituted or substituted by halogen, cyanao, hydroxyl, C.sub.1 -C.sub.20 -alkoxy, C.sub.2 -C.sub.20 -alkoxycarbonyl, acyloxy and/or phenyl which is unsubstituted or substituted by C.sub.1 -c.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy and/or halogen, R.sup.2 and R.sup.3 independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.12 -alkyl, C.sub.1 -C.sub.12 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.4 -C.sub.12 -cycloalkylalkyl, cyano, hydroxyl or hydroxyethyl or are each phenoxy, C.sub.7 -C.sub.10 -phenalkyl or phenyl which is unsubstituted or substituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy and/or halogen, and R.sup.4 is hydrogen or sulfo, are prepared by reacting a 4-alkoxy-2-hydroxybenzophenone of the general formula II ##STR2## with chlorosulfonic acid at from -20.degree. to +100.degree. C.Type: GrantFiled: December 13, 1990Date of Patent: December 10, 1991Assignee: BASF AktiengesellschaftInventors: Peter Neumann, Heinz Eilingsfeld, Alexander Aumueller
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Patent number: 5053547Abstract: A compound of formula (I) ##STR1## its isomers and its salts in which --R.sub.1, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, halogen, C.sub.1 -C.sub.8 -acyloxy or hydroxyl;--R' is hydrogen or C.sub.1 -C.sub.6 -alkyl;--R" is either a polyene chain or a benzene ring are useful in cosmetics and in the treatment of various dermatological and other complaints.Type: GrantFiled: November 14, 1989Date of Patent: October 1, 1991Assignee: L'OrealInventors: Gerard Lang, Jean Maignan, Serge Restle, Braham Shroot
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Patent number: RE34805Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.Type: GrantFiled: July 10, 1992Date of Patent: December 6, 1994Assignee: Centre International de Recherches Dermatologiques (CIRD)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon