Ortho Fused Patents (Class 560/139)
  • Patent number: 5656619
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: August 12, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5612368
    Abstract: 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: Grant
    Filed: October 25, 1995
    Date of Patent: March 18, 1997
    Assignee: Adir et Compagnie
    Inventors: Jean Andrieux, Michel Langlois, Pierre Renard, Philippe Delagrange
  • Patent number: 5563129
    Abstract: 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: Grant
    Filed: April 24, 1995
    Date of Patent: October 8, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirotomo Masuya, Masayoshi Yamaoka
  • Patent number: 5514794
    Abstract: 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: Grant
    Filed: January 22, 1991
    Date of Patent: May 7, 1996
    Assignee: Eli Lilly and Company
    Inventor: Russell L. Barton
  • Patent number: 5491170
    Abstract: .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: Grant
    Filed: December 19, 1994
    Date of Patent: February 13, 1996
    Assignee: Warner-Lambert Company
    Inventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
  • Patent number: 5407956
    Abstract: 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: Grant
    Filed: March 17, 1993
    Date of Patent: April 18, 1995
    Assignee: Zambon Group S.p.A.
    Inventors: Francesco Santangelo, Giorgio Bertolini, Cesare Casagrande, Francesco Marchini, Stefania Montanari, Claudio Semeraro
  • Patent number: 5386017
    Abstract: 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: Grant
    Filed: February 26, 1990
    Date of Patent: January 31, 1995
    Assignee: Board of Governors of Wayne State University
    Inventor: Arthur P. Schaap
  • Patent number: 5347040
    Abstract: 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: Grant
    Filed: December 9, 1992
    Date of Patent: September 13, 1994
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Arnost Reiser, Xiaohua He
  • Patent number: 5334766
    Abstract: 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: Grant
    Filed: April 9, 1992
    Date of Patent: August 2, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Marco Cereghetti, Alain Rageot
  • Patent number: 5319139
    Abstract: 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: Grant
    Filed: March 30, 1993
    Date of Patent: June 7, 1994
    Assignee: 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
  • Patent number: 5314916
    Abstract: 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: Grant
    Filed: April 19, 1993
    Date of Patent: May 24, 1994
    Assignee: Alcon Laboratories, Inc.
    Inventors: Billie M. York, Evan P. Kyba
  • Patent number: 5294731
    Abstract: 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: Grant
    Filed: March 23, 1993
    Date of Patent: March 15, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Joachim Paust, Wolfgang Siegel
  • Patent number: 5292719
    Abstract: The present invention relates to novel formate ester tetralin compounds having fragrant musk-like aroma.
    Type: Grant
    Filed: June 18, 1993
    Date of Patent: March 8, 1994
    Assignee: Union Camp Corporation
    Inventor: Walter C. Frank
  • Patent number: 5292720
    Abstract: The present invention relates to novel formate ester indane compounds having fragrant musk-like aroma.
    Type: Grant
    Filed: June 18, 1993
    Date of Patent: March 8, 1994
    Assignee: Union Camp Corporation
    Inventor: Walter C. Frank
  • Patent number: 5254595
    Abstract: 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: Grant
    Filed: January 9, 1992
    Date of Patent: October 19, 1993
    Assignee: Elf Sanofi
    Inventors: Umberto Guzzi, Marco Baroni, Sergio Boveri, Luciano Manara, Alberto Bianchetti
  • Patent number: 5243088
    Abstract: 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: Grant
    Filed: October 31, 1991
    Date of Patent: September 7, 1993
    Assignee: Potasse et Produits Chimiques
    Inventors: Roland Jacquot, Francoise Truchet
  • Patent number: 5214192
    Abstract: 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: Grant
    Filed: October 2, 1991
    Date of Patent: May 25, 1993
    Assignee: Interox Chemicals Limited
    Inventors: Alexander McKillop, Duncan Kemp
  • Patent number: 5210279
    Abstract: 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: Grant
    Filed: July 12, 1990
    Date of Patent: May 11, 1993
    Assignee: Eastman Kodak Company
    Inventors: Dale E. Van Sickle, Brad W. Overturf
  • Patent number: 5206217
    Abstract: 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: Grant
    Filed: December 20, 1991
    Date of Patent: April 27, 1993
    Assignee: Union Camp Corporation
    Inventor: Walter C. Frank
  • Patent number: 5206418
    Abstract: The invention relates to aminotetrahydronaphthalene derivatives which are intermediates for the preparation of sulfonylaminotetrahydronaphthalenes.
    Type: Grant
    Filed: March 13, 1992
    Date of Patent: April 27, 1993
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Hideo Nakai, Toyoharu Yamashita, Harumichi Kohno, Yasuhiko Sasaki, Akio Odawara
  • Patent number: 5177112
    Abstract: 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: Grant
    Filed: September 10, 1991
    Date of Patent: January 5, 1993
    Assignee: Whitby Research, Inc.
    Inventor: Alan S. Horn
  • Patent number: 5175342
    Abstract: 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: Grant
    Filed: April 18, 1991
    Date of Patent: December 29, 1992
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventor: Arnold Brossi
  • Patent number: 5169978
    Abstract: 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: Grant
    Filed: December 16, 1991
    Date of Patent: December 8, 1992
    Assignee: Societe ATOCHEM
    Inventor: Jean-Philippe Gillet
  • Patent number: 5136084
    Abstract: 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: Grant
    Filed: June 14, 1991
    Date of Patent: August 4, 1992
    Assignee: San Fu Chemical Co., Ltd.
    Inventors: Shu-Chung Lin, Min-Hon Rei
  • Patent number: 5134111
    Abstract: 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: Grant
    Filed: December 15, 1989
    Date of Patent: July 28, 1992
    Assignee: 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
  • Patent number: 5128479
    Abstract: 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: Grant
    Filed: January 29, 1990
    Date of Patent: July 7, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5122537
    Abstract: 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: Grant
    Filed: November 2, 1990
    Date of Patent: June 16, 1992
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Franco Buzzetti, Angelo Crugnola
  • Patent number: 5116994
    Abstract: 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: Grant
    Filed: April 17, 1990
    Date of Patent: May 26, 1992
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Mitsunori Ono
  • Patent number: 5110989
    Abstract: 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: Grant
    Filed: July 17, 1990
    Date of Patent: May 5, 1992
    Assignee: ICI Australia Limited
    Inventors: Alexander Serban, Keith G. Watson, Graham J. Bird, Graeme J. Farquharson, Linsay E. Cross
  • Patent number: 5091558
    Abstract: 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: Grant
    Filed: March 6, 1987
    Date of Patent: February 25, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gordon H. Jones, Michael C. Venuti, John M. Young
  • Patent number: 5089657
    Abstract: 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: Grant
    Filed: March 11, 1987
    Date of Patent: February 18, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Michael C. Venuti
  • Patent number: 5006555
    Abstract: 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: Grant
    Filed: January 17, 1990
    Date of Patent: April 9, 1991
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Douglas G. Batt
  • Patent number: 4996372
    Abstract: 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: Grant
    Filed: February 2, 1990
    Date of Patent: February 26, 1991
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Kenji Saeki, Hiroshi Fukuhara, Tokinori Agoo, Toru Taguchi, Hisaya Miki, Yutaka Haneda, Sadao Yoshimoto
  • Patent number: 4975461
    Abstract: 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: Grant
    Filed: June 19, 1986
    Date of Patent: December 4, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Raj N. Misra
  • Patent number: 4956477
    Abstract: 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: Grant
    Filed: September 22, 1989
    Date of Patent: September 11, 1990
  • Patent number: 4952722
    Abstract: 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: Grant
    Filed: January 26, 1983
    Date of Patent: August 28, 1990
    Assignee: ICI Australia Limited
    Inventors: Alexander Serban, Keith G. Watson, Graham J. Bird, Graeme J. Farquharson, Lindsay E. Cross
  • Patent number: 4946845
    Abstract: 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: Grant
    Filed: November 25, 1988
    Date of Patent: August 7, 1990
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: D. V. Krishna Murthy, Michael C. Venuti, John M. Young
  • Patent number: 4946863
    Abstract: 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: Grant
    Filed: January 18, 1989
    Date of Patent: August 7, 1990
    Assignee: H. Lundbeck A/S
    Inventors: Klaus P. Boegesoe, Jens K. Perregaard
  • Patent number: 4945108
    Abstract: New angucyclinones with a therapeutic action can be prepared with the aid of a strain of the genus Streptomyces.
    Type: Grant
    Filed: April 24, 1989
    Date of Patent: July 31, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Susanne Grabley, Joachim Wink, Carlo Giani, Gerhard Seibert, Wolfgang Raether, Susanne Dobreff, Axel Zeeck
  • Patent number: 4939169
    Abstract: 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: Grant
    Filed: March 13, 1989
    Date of Patent: July 3, 1990
    Assignee: The Upjohn Company
    Inventors: Gordon L. Bundy, Chiu-Hong Lin
  • Patent number: 4935537
    Abstract: 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: Grant
    Filed: October 27, 1988
    Date of Patent: June 19, 1990
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Susumu Naito, Koichi Abe, Hidetaka Kiga, Yuzi Onda
  • Patent number: 4933489
    Abstract: 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: Grant
    Filed: October 24, 1985
    Date of Patent: June 12, 1990
    Assignee: Warner-Lambert Company
    Inventor: Daniel L. Flynn
  • Patent number: 4933475
    Abstract: 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: Grant
    Filed: February 28, 1989
    Date of Patent: June 12, 1990
    Assignee: Pfizer, Inc.
    Inventors: Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4927956
    Abstract: 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: Grant
    Filed: June 2, 1989
    Date of Patent: May 22, 1990
    Assignee: Hoechst Celanese Corporation
    Inventors: Richard Vicari, Mohammad Aslam, Wilson B. Ray, Kenneth G. Davenport, Ralph Dammel, Juergen Lingnau, Karl-Friedrich Doessel
  • Patent number: 4904661
    Abstract: 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: Grant
    Filed: December 16, 1987
    Date of Patent: February 27, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
  • Patent number: 4801737
    Abstract: 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: Grant
    Filed: August 1, 1985
    Date of Patent: January 31, 1989
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Susumu Naito, Koichi Abe, Hidetaka Kiga, Yuzi Onda
  • Patent number: 4792556
    Abstract: 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: Grant
    Filed: April 28, 1986
    Date of Patent: December 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: D. V. K. Murthy, Michael C. Venuti, John M. Young
  • Patent number: 4788341
    Abstract: 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: Grant
    Filed: October 13, 1987
    Date of Patent: November 29, 1988
    Assignee: Eastman Kodak Company
    Inventor: Joseph R. Zoeller
  • Patent number: 4778922
    Abstract: 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: Grant
    Filed: June 17, 1986
    Date of Patent: October 18, 1988
    Assignee: Hoechst Celanese Corporation
    Inventors: Kenneth G. Davenport, Charles B. Hilton
  • Patent number: 4760061
    Abstract: 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: Grant
    Filed: April 24, 1985
    Date of Patent: July 26, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventors: Philip N. Edwards, Brian S. Tait