Ortho Fused Patents (Class 560/139)
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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: 5612368Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which Ar, X, R.sub.1 and R.sub.2 are as defined in the description and a medicinal product containing the same in order to treat a disorder of the melatoninergic system.Type: GrantFiled: October 25, 1995Date of Patent: March 18, 1997Assignee: Adir et CompagnieInventors: Jean Andrieux, Michel Langlois, Pierre Renard, Philippe Delagrange
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Patent number: 5563129Abstract: There are disclosed novel hydroquinone derivatives of the formula: ##STR1## The derivatives of the formula (I) have various pharmacological activities such as antioxidation in living bodies and are useful as medicaments.Type: GrantFiled: April 24, 1995Date of Patent: October 8, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirotomo Masuya, Masayoshi Yamaoka
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Patent number: 5514794Abstract: Derivatized drugs are prepared with a linker consisting of a malonate, wherein the drug is linked through a methylene to the 2-position carbon of the malonate.Type: GrantFiled: January 22, 1991Date of Patent: May 7, 1996Assignee: Eli Lilly and CompanyInventor: Russell L. Barton
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Patent number: 5491170Abstract: .beta.-Carboxy sulfonyl compounds of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 is hydrogen or alkyl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is --O--, --S--, or --NR.sub.2 --, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.Type: GrantFiled: December 19, 1994Date of Patent: February 13, 1996Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5407956Abstract: Derivatives of 2-amino-1,2,3,4-tetrahydronaphthalene and their use in therapeutic field are described.The compounds are particularly useful in the treatment of arterial hypertension, cardiac decompensation and renal failure, in the treatment of peripheral arteriopathies and in cerebrovascular insufficiency.Type: GrantFiled: March 17, 1993Date of Patent: April 18, 1995Assignee: Zambon Group S.p.A.Inventors: Francesco Santangelo, Giorgio Bertolini, Cesare Casagrande, Francesco Marchini, Stefania Montanari, Claudio Semeraro
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Patent number: 5386017Abstract: Novel alkenes leading to light producing 1,2-dioxetanes of the formula ##STR1## wherein ArOX is an aryl ring substituted with an X oxy group and A are passive organic groups which allow the 1,2-dioxetane to produce light when triggered by removing X. X is a chemically labile group which is removed by an activating agent. The 1,2-dioxetane compounds can be triggered to produce light at room temperatures.Type: GrantFiled: February 26, 1990Date of Patent: January 31, 1995Assignee: Board of Governors of Wayne State UniversityInventor: Arthur P. Schaap
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Patent number: 5347040Abstract: Onium salt capable of generating acid upon exposure to actinic radiation having the following structure:(R.sub.1).sub.a (R.sub.2).sub.b (R.sub.3).sub.c Q.sup.+ --A--M.sup.+ X.sup.- --B--X'.sup.-where:Q is S;R.sub.1, R.sub.2 and R.sub.3 are independently substituted or unsubstituted aromatic, aliphatic, or aralkyl groups having 7-18 carbon atoms;M.sup.+ is a cationic organic radical;A is a divalent radical selected from the group of hindered alkylene groups, substituted or unsubstituted aromatic or aralkyl groups;B is a divalent aromatic sensitizer which absorbs radiation having a wavelength longer than 300 nm and is capable of transferring an electron to Q,x.sup.- and X'.sup.- are anionic groups; and wherein A provides a spatial separation between Q and M, and B provides a spatial separation between X and X', such that the spatial separation provided by A between Q and M is substantially the same as the spatial separation provided by B between X and X'.Type: GrantFiled: December 9, 1992Date of Patent: September 13, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventors: Arnost Reiser, Xiaohua He
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Patent number: 5334766Abstract: A process for the resolution of racemic diphosphine oxides into the optically active antipodes by reacting the racemate with a resolving agent comprising using a carbamate or thiocarbamate of an optically active .alpha.-hydroxycarboxylic acid or .alpha.-aminocarboxylic acid as the resolving agent.Type: GrantFiled: April 9, 1992Date of Patent: August 2, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Marco Cereghetti, Alain Rageot
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Patent number: 5319139Abstract: Compounds of the formula: ##STR1## where R.sup.1 is a hydrogen atom or a lower alkyl group;R.sub.2 is a lower alkoxy group;R.sub.3 is a group ##STR2## Z is represented by the formula: ##STR3## where R.sub.2 and R.sub.3 may be the same or different from each other and each stands for a hydrogen atom or a lower alkyl;Y is represented by the formula: --(CH.sub.2).sub.n -- where n is 0 or an integer of 1 to 2 or a group represented by the formula: ##STR4## where R.sup.2 and R.sup.3 may be the same or different from each other and each stands for a lower alkyl group; andR.sup.4 represents a group of the formula: ##STR5## where p is 0 or an integer of 1 to 3 and R.sup.12 is hydrogen, a halogen atom, a lower alkyl or a lower alkoxy group a hydrogen atom, R.sup.2 is a methoxy group, R.sup.3 is a hydroxy group and R.sup.4 is a benzyl group having anti-inflammatory activity.Type: GrantFiled: March 30, 1993Date of Patent: June 7, 1994Assignee: Eisai Co. Ltd.Inventors: Hiroyuki Yoshimura, Shinya Abe, Tetsuya Kawahara, Naoyuki Shimomura, Kazuo Okano, Richard S. J. Clark, Takashi Mori, Shuhei Miyazawa, Ryoichi Hashida, Kenzo Muramoto, Koukichi Harada, Takashi Inoue, Hirsohi Shirota, Kenichi Chiba, Kenichi Kusube, Toru Horie, Takeshi Suzuki, Isao Yamatsu
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Patent number: 5314916Abstract: Compounds having beta-2 adrenergic agonist activity and the use of these compounds in controlling intraocular pressure are disclosed. The compounds are believed to be useful in controlling intraocular pressure by increasing the outflow of aqueous humor. The compounds are considered to be less likely to cause cardiovascular side effects and various other side effects associated with stimulation of beta-1 receptors, relative to epinephrine.Type: GrantFiled: April 19, 1993Date of Patent: May 24, 1994Assignee: Alcon Laboratories, Inc.Inventors: Billie M. York, Evan P. Kyba
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Patent number: 5294731Abstract: A process for the preparation of .beta.-hydroxycarboxylates of the general formula I ##STR1## in which R.sup.1 and R.sup.2 individually denoteC.sub.1 -C.sub.20 alkyl optionally substituted by C.sub.1 -C.sub.8 alkoxy and/or halogen, C.sub.3 -C.sub.20 alkoxycarbonylalkyl, C.sub.2 -C.sub.20 alkenyl, C.sub.5 -C.sub.30 acetalalkenyl, aryl optionally mono- to penta-substituted by C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, and/or halogen, C.sub.7 -C.sub.20 aralkyl, C.sub.7 -C.sub.20 aralkenyl, hetaryl, C.sub.3 -C.sub.20 cycloalkyl, or C.sub.4 -C.sub.20 cycloalkylalkyl,or together denote a C.sub.2 -C.sub.8 alkylene chainand one or other of R.sup.1 and R.sup.2 denotes hydrogen, andR.sup.3 denotes hydrogen, C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.20 alkenyl, aryl optionally mono- to penta-substituted by C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, and/or halogen, C.sub.7 -C.sub.20 aralkyl, C.sub.3 -C.sub.20 cycloalkyl, or C.sub.4 -C.sub.20 cycloalkylalkyl, andR.sup.4 denotes C.sub.1 -C.sub.20 alkyl, C.sub.Type: GrantFiled: March 23, 1993Date of Patent: March 15, 1994Assignee: BASF AktiengesellschaftInventors: Joachim Paust, Wolfgang Siegel
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Patent number: 5292719Abstract: The present invention relates to novel formate ester tetralin compounds having fragrant musk-like aroma.Type: GrantFiled: June 18, 1993Date of Patent: March 8, 1994Assignee: Union Camp CorporationInventor: Walter C. Frank
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Patent number: 5292720Abstract: The present invention relates to novel formate ester indane compounds having fragrant musk-like aroma.Type: GrantFiled: June 18, 1993Date of Patent: March 8, 1994Assignee: Union Camp CorporationInventor: Walter C. Frank
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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: 5243088Abstract: Dibromonaphthalene compounds having the formula (1): ##STR1## are 1-monodebrominated by reacting same, neat or in an acid organic solvent, with molecular hydrogen or a compound that generates nascent hydrogen, in situ, in the medium of reaction, in the presence of a catalytically effective amount of a hydrodebromination catalyst.Type: GrantFiled: October 31, 1991Date of Patent: September 7, 1993Assignee: Potasse et Produits ChimiquesInventors: Roland Jacquot, Francoise Truchet
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Patent number: 5214192Abstract: Diacetoxyatene compounds are obtained by reacting a perborate such as sodium perborate monohydrate or tetrahydrate and acetic acid with an iodoarene compound under mild conditions, such as 40 to 50.degree. C. The iodoarene can be further substituted by a wide range of substituents, such as halo, nitro, alkyl, alkoxy or carbosylic acid, in any position around the nucleus, except that electron withdrawing substituents occupy meta positions only. The invention process thus enables a wide range of substituted diacetoxyarene compounds to be produced using widely available and easily handled materials under mild operating conditions.Type: GrantFiled: October 2, 1991Date of Patent: May 25, 1993Assignee: Interox Chemicals LimitedInventors: Alexander McKillop, Duncan Kemp
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Patent number: 5210279Abstract: A continuous process for the production of diacetate derivatives of aromatic compounds, comprising feeding at any convenient temperature an oxygen-containing gas and feedstock comprising a diisopropyl ring substituted aromatic compound and the recycled monoisopropyl-monoacetate derivative thereof, to an oxidizer operated, for example, at from about 10.degree. C. to about 150.degree. C. and oxygen partial pressures of from about 0.05 to 10 atmospheres to form an oxidizer product comprising the mono- and dihydroperoxides of the feedstock, feeding the oxidizer product to a rearrangement-esterification zone containing acetic anhydride at from about 0.degree. C. to 150.degree. C. to form an ester product comprising the diacetate and monoisopropyl-monoacetate derivatives of the feedstock, distilling the ester product to separate the diacetate and monoisopropyl-monoacetate derivatives, and recycling the monoisopropyl-monoacetate derivative back to the oxidizer.Type: GrantFiled: July 12, 1990Date of Patent: May 11, 1993Assignee: Eastman Kodak CompanyInventors: Dale E. Van Sickle, Brad W. Overturf
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Patent number: 5206217Abstract: The present invention relates to novel indane compounds, such as, for example, 5-formyl-1,1,2,3,3,4,6-heptamethylindane, a compound of the formula ##STR1## and to compositions including the same, as well as to methods for their preparation. Compounds and compositions of the invention possess a fragrant musk-like aroma and have utility in the perfumery and/or other industries.Type: GrantFiled: December 20, 1991Date of Patent: April 27, 1993Assignee: Union Camp CorporationInventor: Walter C. Frank
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Patent number: 5206418Abstract: The invention relates to aminotetrahydronaphthalene derivatives which are intermediates for the preparation of sulfonylaminotetrahydronaphthalenes.Type: GrantFiled: March 13, 1992Date of Patent: April 27, 1993Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Hideo Nakai, Toyoharu Yamashita, Harumichi Kohno, Yasuhiko Sasaki, Akio Odawara
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Patent number: 5177112Abstract: Certain novel compounds having the structural formula ##STR1## wherein R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H and OA; A is H or is selected from the group consisting of hydrocarbyl radicals, e.g. lower alkyl radicals, i.e. methyl, ethyl, propyl, etc., or ##STR2## wherein R.sub.5 is selected from the group consisting of hydrocarbyl radicals, e.g. alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of organic radicals having fused aromatic rings, that is, radicals comprising at least two rings that share a pair of carbon atoms or share a carbon and nitrogen atom are useful for inducing a dopaminergic response and reducing the intraocular pressure in a mammal.Type: GrantFiled: September 10, 1991Date of Patent: January 5, 1993Assignee: Whitby Research, Inc.Inventor: Alan S. Horn
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Patent number: 5175342Abstract: The present invention relates to esters of 3-demethylthiocolchicine and N-acyl analogs thereof having the following formula: ##STR1## wherein R is O-CO-alkyl, O-CO-CH.sub.2 Oalkyl, O-CO-Phenyl, O-COOalkyl; the alkyl group having from 1 to 4 carbon atoms and the Ac group representing acetyl and its higher homologs, benzoyl, alkoxyacetyl, or haloacetyl.The invention further relates to processes for preparing these ester compounds, pharmaceutical compositions thereof and methods for treating diseases such as gout, Mediterranean fever and liver disorders.Type: GrantFiled: April 18, 1991Date of Patent: December 29, 1992Assignee: The United States of America as represented by the Department of Health and Human ServicesInventor: Arnold Brossi
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Patent number: 5169978Abstract: Novel (naphthyloxy)benzoic/naphthoic acid compounds, polymerizable into thermotropic polymers have the formulae: ##STR1## in which R is hydrogen, a straight or branched chain aliphatic or cycloaliphatic hydrocarbon radical having from 1 to 4 carbon atoms or a radical ##STR2## wherein R' is a methyl or ethyl radical, or salt thereof.Type: GrantFiled: December 16, 1991Date of Patent: December 8, 1992Assignee: Societe ATOCHEMInventor: Jean-Philippe Gillet
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Patent number: 5136084Abstract: A novel process for the acetylation of a mono-substituted phenol or a mono-substituted naphthol is disclosed which comprises reacting the said mono-substituted phenol or the said mono-substituted naphthol respectively with vinyl acetate at a temperature of not more than 160.degree. C.Type: GrantFiled: June 14, 1991Date of Patent: August 4, 1992Assignee: San Fu Chemical Co., Ltd.Inventors: Shu-Chung Lin, Min-Hon Rei
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Patent number: 5134111Abstract: A naphthalene derivative having the formula is new and useful for medicine. ##STR1## [wherein R.sup.1 represents a hydrogen atom, a lower alkyl group or an acyl group;R.sup.2 independently represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, a cycloalkyl group, a cycloalkylalkyl group, a hydroxyl group, an aryl group which may be substituted, an arylalkyl group whose aryl group may be substituted, a heteroaryl group, or a heteroarylalkyl group;R.sup.3 and R.sup.4 are the same or different and represent a hydrogen atom, a lower alkyl group, a lower alkenyl group, an aryl group which may have a substituent, an arylalkyl group whose aryl group may be substituted, an arylalkenyl group whose aryl group may be substituted, a cycloalkyl group, an alkoxyalkyl group, a heteroaryl group, a heteroarylalkyl group, a carboxy group, a carboxyalkyl group, an aminoalkyl group, or a cyano group;R.sup.5 represents a group of the formula, --OR.sup.7, (wherein R.sup.Type: GrantFiled: December 15, 1989Date of Patent: July 28, 1992Assignee: Eisai Co., Ltd.Inventors: Makoto Okita, Hiroshi Shirota, Masayuki Tanaka, Toshihiko Kaneko, Katsuya Tagami, Shigeki Hibi, Yasushi Okamoto, Seiichiro Nomoto, Takeshi Suzuki, Kenichi Chiba, Masaki Goto, Ryoichi Hashida, Hideki Ono, Hideto Ohhara, Hideki Sakurai, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
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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: 5122537Abstract: The invention relates to new arylvinylamide derivatives of formula ##STR1## wherein Y is a bicyclic ring system chosen from (A), (B), (C), (D), and (E); ##STR2## in which m is zero, 1 or 2; R is hydrogen, a C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl group;R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen, cyano or C.sub.1 -C.sub.6 alkyl; andn is an integer of 1 to 3; and wherein each of the substituents --CH.dbd.CHNHCOR.sub.1, OR and R.sub.2 may be independently on either of the aryl and heteroaryl moieties of the bicyclic ring system (A), (C), (D) and (E); whereas only the benzene ring may be substituted in the bicyclic ring system (B),which are useful as tyrosine kinase inhibitors.Type: GrantFiled: November 2, 1990Date of Patent: June 16, 1992Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Angelo Crugnola
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Patent number: 5116994Abstract: Deacylating agent represented by the formula (I): ##STR1## wherein R represents an insoluble polymer substituent, and R' and R" each represents an alkyl group, and a deacylation method using the above deacylating agent.Type: GrantFiled: April 17, 1990Date of Patent: May 26, 1992Assignee: Fuji Photo Film Co., Ltd.Inventor: Mitsunori Ono
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Patent number: 5110989Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: W are selected from alkyl, alkenyl and alkynyl;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkynyl, alkenyloxy, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, amino, substituted amino, and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof, and an alkylene group which bridges two adjacent carbon atoms of the benzene ring;R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.Type: GrantFiled: July 17, 1990Date of Patent: May 5, 1992Assignee: ICI Australia LimitedInventors: Alexander Serban, Keith G. Watson, Graham J. Bird, Graeme J. Farquharson, Linsay E. Cross
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Patent number: 5091558Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is alkoxy, alkylthio, optionally substituted phenoxy or optionally substituted phenylthio;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl;R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2, or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(0).sub.Type: GrantFiled: March 6, 1987Date of Patent: February 25, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Gordon H. Jones, Michael C. Venuti, John M. Young
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Patent number: 5089657Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein:R.sup.1 is lower alkoxy or optionally substituted phenoxy;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenyl-lower-alkyl;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;X and Y are different and are selected from the group consisting of hydrogen, R.sup.4 and -C(O)W, whereinW is alkyl of one to seven carbon atoms, optionally substituted phenyl or optionally substituted benzyl; andR.sup.4 is lower alkyl or optionally substituted phenyl-lower-alkyl.Type: GrantFiled: March 11, 1987Date of Patent: February 18, 1992Assignee: Syntex (U.S.A.) Inc.Inventor: Michael C. Venuti
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Patent number: 5006555Abstract: There are provided novel esters of 2-arylmethyl-1-naphthol derivatives useful as anti-inflammatory agents. Also provided are pharmaceutical compositions containing these compounds and methods of using the compounds to treat inflammatory diseases in man.Type: GrantFiled: January 17, 1990Date of Patent: April 9, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventor: Douglas G. Batt
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Patent number: 4996372Abstract: In a process for producing 2,6-dihydroxynaphthalene from 2,6-diisopropylnaphthalene, 2,6-diisopropylnaphthalene is oxidized in the presence of a specific proportion of a basic compound to hydroxylate or hydroperoxylate 2,6-diisopropylnaphthalene in a high conversion, and the resulting intermediate is then subjected to acid cleavage in the presence of hydrogen peroxide to produce 2,6-dihydroxynaphthalene in a high yield. The yield of 2,6-dihydroxynaphthalene increases by subjecting the reaction mixture containing the above intermediate to a purifying operation or dehydrating operation or adding acetone to it before it is submitted to the acid cleavage. 2,6-Dihydroxynaphthalene may be reacted with acetic anhydride to obtain 2,6-diacetoxynaphthalene.Type: GrantFiled: February 2, 1990Date of Patent: February 26, 1991Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Kenji Saeki, Hiroshi Fukuhara, Tokinori Agoo, Toru Taguchi, Hisaya Miki, Yutaka Haneda, Sadao Yoshimoto
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Patent number: 4975461Abstract: p-Aminophenols are provided having the structure ##STR1## wherein m is 0, 1 or 2; n is 0, 1, 2 or 3; R.sup.1 and R.sup.2 may be the same or different and are H, hydroxy or alkoxy; R.sup.3 is H, lower alkyl, alkanoyl or aroyl and R.sup.4 is H, lower alkyl or alkanoyl, and including acid-addition salts thereof.These compounds are useful as inhibitors of leukotriene production and as such are useful as antiallergy, anti-inflammatory and anti-psoriatic agents.Type: GrantFiled: June 19, 1986Date of Patent: December 4, 1990Assignee: E. R. Squibb & Sons, Inc.Inventor: Raj N. Misra
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Patent number: 4956477Abstract: Compounds having the formula: ##STR1## wherein T is a polycycloalkylidene group (e.g., adamant-2-ylidene); R is a C.sub.1-20 alkyl, aralkyl or cycloalkyl group; and Y is a fluorescent chromophore (e.g., m-phenylene), produced by reacting a compound having the formula: ##STR2## with an R-ylating agent (e.g., R.sub.2 SO.sub.4) in the presence of an alkali metal alkoxide in a polar aprotic solvent. Also, compounds having the formula: ##STR3## are produced by reacting a compound having the formula: ##STR4## wherein X is an electronegative leaving group (e.g., a halogen anion such as chloride ion) in the presence of a Lewis base (e.g., a trialkyl-amine) dissolved in an aprotic organic solvent (e.g., benzene or toluene). Also, compounds having the formula ##STR5## are produced by reacting a compound of the formula ##STR6## with a tetra-O-acylated-O-hexopyranoside halide, then hydrolyzing off the protective acyl groups.Type: GrantFiled: September 22, 1989Date of Patent: September 11, 1990
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Patent number: 4952722Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: W are selected from alkyl, alkenyl and alkynyl;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkynyl, alkenyloxy, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, amino, substituted amino, and the groups formyl and alkanoyl and the oxime and imine derivatives thereof, and an alkylene group which bridges two adjacent carbon atoms of the benzene ring;R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl;p is zero or an integer selected form 1 to 4;n is zero or an integer selected from 1 to 3; andm is zero or an integer selected from 1 to 3.Type: GrantFiled: January 26, 1983Date of Patent: August 28, 1990Assignee: ICI Australia LimitedInventors: Alexander Serban, Keith G. Watson, Graham J. Bird, Graeme J. Farquharson, Lindsay E. Cross
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Patent number: 4946845Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.Type: GrantFiled: November 25, 1988Date of Patent: August 7, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: D. V. Krishna Murthy, Michael C. Venuti, John M. Young
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Patent number: 4946863Abstract: The present invention relates to 3-aminomethyl derivatives of indane, dihydrobenzofurane, dihydrobenzothiophene, and indoline, acid addition salts thereof, isomers thereof, methods of preparation, pharmaceutical compositions and method of treating CNS-disorders such as schizophrenia, Parkinson's disease, depression, anxiety, migraine and senile dementia, or in the cure of cardiovascular diseases, by administering such a derivative.Type: GrantFiled: January 18, 1989Date of Patent: August 7, 1990Assignee: H. Lundbeck A/SInventors: Klaus P. Boegesoe, Jens K. Perregaard
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Patent number: 4945108Abstract: New angucyclinones with a therapeutic action can be prepared with the aid of a strain of the genus Streptomyces.Type: GrantFiled: April 24, 1989Date of Patent: July 31, 1990Assignee: Hoechst AktiengesellschaftInventors: Susanne Grabley, Joachim Wink, Carlo Giani, Gerhard Seibert, Wolfgang Raether, Susanne Dobreff, Axel Zeeck
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Patent number: 4939169Abstract: Novel 1,4-naphthalenediol and 1,4-hydroquinone derivatives of formula I, II, III and IV and their therapeutic uses as 5-lipoxygenase inhibitors, leukotriene inhibitors, antiinflammatory and/or inhibitors of mucus secretion agents are described. Also provided are novel intermediates useful for the preparation of said derivatives.Type: GrantFiled: March 13, 1989Date of Patent: July 3, 1990Assignee: The Upjohn CompanyInventors: Gordon L. Bundy, Chiu-Hong Lin
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Patent number: 4935537Abstract: A process for producing an acyloxynaphthoic acid represented by the general formula ##STR1## wherein R.sub.1 represents a hydrogen atom or an alkyl group, which comprises(a) oxidizing an acylalkylnaphthalene represented by the general formula ##STR2## wherein R.sub.1 is as defined, and R.sub.2 represents a lower alkyl group, with a peroxide, and(b) oxidizing the resulting acyloxyalkylnaphthalene represented by the general formula ##STR3## wherein R.sub.1 and R.sub.2 are as defined above, with molecular oxygen in an organic solvent in the presence of a catalyst comprising a bromine compound and a cobalt compound.Type: GrantFiled: October 27, 1988Date of Patent: June 19, 1990Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Susumu Naito, Koichi Abe, Hidetaka Kiga, Yuzi Onda
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Patent number: 4933489Abstract: An improved process for the manufacture of the antipsoriatic agent, 6-chloro-1,4-diacetoxy-2,3-dimethoxynaphthalene, is herein described which involves in situ Diels-Alder coupling of 2,3-dimethoxybenzo-1,4-quinone with a 3-chloro-1-alkoxy-1,3-butadiene; 1,4-elimination of the alcohol with aromatization of the chlorine-bearing ring, and acetylation.Type: GrantFiled: October 24, 1985Date of Patent: June 12, 1990Assignee: Warner-Lambert CompanyInventor: Daniel L. Flynn
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Patent number: 4933475Abstract: Compounds having the formula ##STR1## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.Type: GrantFiled: February 28, 1989Date of Patent: June 12, 1990Assignee: Pfizer, Inc.Inventors: Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4927956Abstract: 3-substituted-4-hydroxy- and 4-acetoxystyrene compounds, especially 3,5-di(methyl, bromo or chloro)-4-acetoxystyrene as well as a process for its preparation. 2,6-dimethylphenol is acylated with acetic anhydride and HF catalyzed to produce 3,5-dimethyl-4-hydroxy-acetophenone. After subsequent esterification with acetic anhydride and catalyzed hydrogenation to form 1-(3',5'-dimethyl-4'-acetoxyphenyl)ethanol, this intermediate is then dehydrated with an acid and a polymerization inhibitor to produce 3,5-dimethyl-4-acetoxystyrene.Type: GrantFiled: June 2, 1989Date of Patent: May 22, 1990Assignee: Hoechst Celanese CorporationInventors: Richard Vicari, Mohammad Aslam, Wilson B. Ray, Kenneth G. Davenport, Ralph Dammel, Juergen Lingnau, Karl-Friedrich Doessel
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Patent number: 4904661Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.Type: GrantFiled: December 16, 1987Date of Patent: February 27, 1990Assignee: Imperial Chemical Industries PLCInventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
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Patent number: 4801737Abstract: A process for producing an acyloxynaphthoic acid represented by the general formula ##STR1## wherein R.sub.1 represents a hydrogen atom or an alkyl group, which comprises(a) oxidizing an acylalkylnaphthalene represented by the general formula ##STR2## wherein R.sub.1 is as defined, and R.sub.2 represents a lower alkyl group, with a peroxide, and(b) oxidizing the resulting acyloxyalkylnaphthalene represented by the general formula ##STR3## wherein R.sub.1 and R.sub.2 are as defined above, with molecular oxygen in an organic solvent in the presence of a catalyst comprising a bromine compound and a cobalt compound.Type: GrantFiled: August 1, 1985Date of Patent: January 31, 1989Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Susumu Naito, Koichi Abe, Hidetaka Kiga, Yuzi Onda
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Patent number: 4792556Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.Type: GrantFiled: April 28, 1986Date of Patent: December 20, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: D. V. K. Murthy, Michael C. Venuti, John M. Young
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Patent number: 4788341Abstract: 2-Acetonaphthones are prepared by heating a compound selected from the group consisting of ketals and enol ethers of acetyl-substituted benzalacetone at a temperature effective to cyclize the compound and form said 2-acetonaphthones.Type: GrantFiled: October 13, 1987Date of Patent: November 29, 1988Assignee: Eastman Kodak CompanyInventor: Joseph R. Zoeller
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Patent number: 4778922Abstract: N,O-diacetyl-6-amino-2-naphthol is produced by subjecting 2-naphthyl acetate to a Fries rearrangement or 2-naphthol and an acetylating agent to a Friedel-Crafts acetylation to form 6-hydroxy-2-acetonaphthone which is then reacted as is or as its acetate ester with hydroxylamine or a hydroxylamine salt to form 6-hydroxy-2-acetonaphthone oxime. The oxime is then subjected to a Beckmann rearrangement and accompanying acetylation with acetic anhydride to form the N,O-diacetyl-6-amino-2-naphthol.Type: GrantFiled: June 17, 1986Date of Patent: October 18, 1988Assignee: Hoechst Celanese CorporationInventors: Kenneth G. Davenport, Charles B. Hilton
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Patent number: 4760061Abstract: Mono- or bis-complex esters or ethers of a phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined mono- or bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus; whereinA is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, whereinR.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, whereinR.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; whereinR.sup.12 is hydrogen or alkyl, and whereinR.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.Type: GrantFiled: April 24, 1985Date of Patent: July 26, 1988Assignee: Imperial Chemical Industries PLCInventors: Philip N. Edwards, Brian S. Tait