Hydroxy, Bonded Directly To Carbon, Or Ether In Substituent Q (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/167)
  • Patent number: 5434188
    Abstract: 1-Ether and 1-thioether-naphthalene-2-carboxamides are described, methods of manufacture therefor and their use as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases, and their utility in inhibiting the activation of human immunodeficiency virus (HIV), latent in infected humans.
    Type: Grant
    Filed: March 7, 1994
    Date of Patent: July 18, 1995
    Assignee: Warner-Lambert Company
    Inventors: Diane H. Boschelli, David T. Connor, Sony S. Khatana, James B. Kramer, Paul C. Unangst
  • Patent number: 5430060
    Abstract: The invention concerns novel N-phenylacetyl and related acyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.
    Type: Grant
    Filed: September 15, 1993
    Date of Patent: July 4, 1995
    Assignee: Zeneca Limited
    Inventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Slater
  • Patent number: 5426229
    Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: June 20, 1995
    Assignee: Eli Lilly and Company
    Inventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus
  • Patent number: 5416118
    Abstract: Novel bicyclic amides of the formula ##STR1## wherein Ar.sup.1 and Ar.sup.2 are phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl, wherein R.sup.2 is 1 to 3 substituents independently selected from the group consisting of halogeno, hydroxy, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino and lower dialkylamino;X, Y and Z are --CH.sub.2 --, --CH(alkyl)--, --C(alkyl).sub.2 --, --NH--, --N(alkyl)--, --O-- or --SO.sub.r, wherein r is 0, 1 or 2, and m, n and p are 0 or 1;R.sup.1 is an alkyl chain of 1 to 25 carbon atoms; an alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain --O--, --SO.sub.r, phenylene, R.sup.2 -substituted phenylene, heteroarylene or R.sup.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: May 16, 1995
    Assignee: Schering Corporation
    Inventors: John W. Clader, Thomas Fevig, Wayne Vaccaro, Joel G. Berger
  • Patent number: 5414122
    Abstract: There is disclosed an efficient process for producing .alpha.-ketoacetamide of the formula: ##STR1## which is useful as an intermediate for the production of various alkoxyiminoacetamide compounds to be used for agricultural fungicides. In this process, a corresponding acid halide is condensed with isocyanide to produce the .alpha.-ketoacetamide.
    Type: Grant
    Filed: August 17, 1993
    Date of Patent: May 9, 1995
    Assignee: Shionogi & Co., Ltd.
    Inventors: Akira Murabayashi, Hideyuki Takenaka, Hiroyuki Kai
  • Patent number: 5407902
    Abstract: A methoxyiminoacetic acid derivative represented by the following formula (I): ##STR1## wherein X represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms; A represents a methoxy group or a methylamino group; when A is a methoxy group, B represents --O--CO-- or --N=C(R.sup.1)-- and when A is a methylamino group, B represents --O--CR.sup.1 R.sup.2 --, wherein R.sup.1 and R.sup.2 independently represent a hydrogen atom, an alkyl group having 1 to 4 carbon atoms or a trifluoromethyl group; and Ar represents an optionally substituted aryl group or an optionally substituted heteroaryl group, and an agricultural/horticultural fungicide containing the same as an active ingredient.
    Type: Grant
    Filed: October 1, 1993
    Date of Patent: April 18, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Masatsugu Oda, Manabu Katsurada, Hirofumi Tomita
  • Patent number: 5399673
    Abstract: Compounds containing at least one alkenyl group, at least one maleimide group and at least one rodlike mesogenic moiety are prepared by reacting one or more aminophenols containing one or more rodlike mesogenic moieties with a stoichiometric quantity of a maleic anhydride per amine group of said aminophenol and then alkenylating the resulting phenolic functional maleimide.
    Type: Grant
    Filed: February 9, 1993
    Date of Patent: March 21, 1995
    Assignee: The Dow Chemical Company
    Inventor: Robert E. Hefner, Jr.
  • Patent number: 5395854
    Abstract: Ortho-substituted phenyl-acetamides I ##STR1## (R.sup.1 =H, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkynyl, alkoxyalkyl, alkoxycarbonyl, phenyl, phenylalkyl, phenylalkenyl or phenoxyalkyl, 5- or 6-membered heterocycle with 1-3 hetero atoms to which a benzene ring or a 5- or 6-membered heterocycle can be fused; R.sup.2 and R.sup.3 =H, CN, halogen, alkyl, alkoxy; R.sub.4 and R.sup.5 =H, alkyl and R.sup.4 or R.sup.5 =alkoxy; Y=O, S, SO, SO.sub.2, N=N, O--CO, CO--O, CO--O--CH.sub.2, alkylene or haloalkylene, alkenylene, alkynylene, oxy- alkylene, thio-alkylene, alkyleneoxy, carbonylalkylene or alkylenecarbonyl, W=alkoxyimino, alkoxymethylene or alkylthiomethylene), excepting compounds where R.sup.1 is hydrogen, phenyl or 2,2-dimethyl-3-(2,2-dichlorovinyl)cyclopropyl, R.sup.2 to R.sup.5 are each hydrogen, Y is carbonyloxymethylene and W is methoxymethylene or methylthiomethylene, are suitable as fungicides and for controlling pests.
    Type: Grant
    Filed: September 22, 1993
    Date of Patent: March 7, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Siegbert Brand, Eberhard Ammermann, Gisela Lorenz, Hubert Sauter, Klaus Oberdorf, Uwe Kardorff, Christoph Kuenast
  • Patent number: 5393776
    Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.
    Type: Grant
    Filed: May 13, 1994
    Date of Patent: February 28, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventor: Bradley C. Pearce
  • Patent number: 5354891
    Abstract: Disclosed is a method for producing aromatic amine derivatives in a high yield at a low price, which comprises inducing an aromatic hydroxamic acid derivative to undergo a rearrangement reaction under a mild condition in the presence of a base and a nitrile or a nitrile equivalent.
    Type: Grant
    Filed: March 4, 1993
    Date of Patent: October 11, 1994
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Tatsuhiko Obayashi
  • Patent number: 5354779
    Abstract: New oxime ether amides of the formula (I) ##STR1## in which R has the meaning given in the description, and a plurality of processes for their preparation were described.The new oxime ether amides are used as pesticides.
    Type: Grant
    Filed: November 30, 1992
    Date of Patent: October 11, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Kramer, Dieter Berg, Heinz-Wilhelm Dehne, Stefan Dutzmann, Christoph Erdelen
  • Patent number: 5302739
    Abstract: Compounds of the formula ##STR1## as intermediates for the preparation of pyrimidine or triazine herbicides.
    Type: Grant
    Filed: October 29, 1992
    Date of Patent: April 12, 1994
    Assignees: Kumiai Chemical Industry Co., Ihara Chemical Industry Co., Ltd.
    Inventors: Masatoshi Tamaru, Norihiro Kawamura, Masahiro Sato, Fumiaki Takabe, Shigehiko Tachikawa, Ryo Yoshida
  • Patent number: 5298647
    Abstract: Aromatic compounds absorbing UVB and/or UVA, substituted with an amide function, selected from the group consisting of ##STR1## whose variable substituents are as defined in the specification, e.g. ##STR2## are useful as photoprotective agents or tanning accelerators.
    Type: Grant
    Filed: December 14, 1987
    Date of Patent: March 29, 1994
    Inventors: Dominique Robert, Louis Jung
  • Patent number: 5280045
    Abstract: The subject invention involves compositions comprising 4-(3,5-bis(1,1-dimethylethyl-4-hydroxyphenyl)-4-oxobutanamide, or 4-(3,5-bis-(1,1-dimethylethyl)-4-hydroxyphenyl)-4-oxobutanoic acid and pharmaceutically-acceptable salts thereof, and a pharmaceutically-acceptable carrier. The subject invention also involves methods for treating diseases characterized by inflammation and/or pain, such as rheumatoid arthritis and osteoarthritis, in humans or lower animals by administration of a safe and effective amount of this compound to the human or lower animal in need of such treatment.
    Type: Grant
    Filed: October 1, 1992
    Date of Patent: January 18, 1994
    Assignee: The Procter & Gamble Company
    Inventors: Roy L. M. Dobson, Kenneth R. Wehmeyer, Steven P. Sirko, Benjamin F. Floyd
  • Patent number: 5270342
    Abstract: The invention concerns novel N-phenylacetyl and related acyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.
    Type: Grant
    Filed: July 31, 1991
    Date of Patent: December 14, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Salter
  • Patent number: 5258551
    Abstract: There is disclosed an efficient process for producing .alpha.-ketoacetamide of the formula: ##STR1## which is useful as an intermediate for the production of various alkoxyiminoacetamide compounds to be used for agricultural fungicides. In this process, a corresponding acid halide is condensed with isocyanide to produced the .alpha.-ketoacetamide.
    Type: Grant
    Filed: December 3, 1992
    Date of Patent: November 2, 1993
    Assignee: Shionogi & Co., Ltd.
    Inventors: Akira Murabayashi, Hideyuki Takenaka, Hiroyuki Kai
  • Patent number: 5248823
    Abstract: 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: December 4, 1992
    Date of Patent: September 28, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5241102
    Abstract: A Schiff base compound of formula (I): ##STR1## wherein Ar represents an aromatic group, which may have a substituent; n is 0 or 1; and Z represents ##STR2## in which m is an integer of 0 or 1, or ##STR3## provided that when Z is ##STR4## and Ar is a phenyl group and the substituent thereof is an alkoxyl group represented by C.sub.p H.sub.2p+1 O, p is an integer of 1 to 4.In addition, a nonlinear optical material using the above Schiff base compound of formula (I) is disclosed.
    Type: Grant
    Filed: March 20, 1992
    Date of Patent: August 31, 1993
    Assignee: Ricoh Company, Ltd.
    Inventors: Masayuki Syoshi, Miwa Syutou
  • Patent number: 5236957
    Abstract: N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.
    Type: Grant
    Filed: January 25, 1991
    Date of Patent: August 17, 1993
    Assignee: Farmitalia Carlo Erba Srl
    Inventors: Philippe Dostert, Paolo Pevarello, Franco Heidempergher, Mario Varasi, Alberto Bonsignori, Romeo Roncucci
  • Patent number: 5221691
    Abstract: Fungicidal compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted aryloxyalkyl, optionally substituted heterocyclyloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heterocyclyl, optionally substituted aryloxy, optionally substituted heterocyclyloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.sup.3).sub.
    Type: Grant
    Filed: January 29, 1992
    Date of Patent: June 22, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Paul J. de Fraine, Ian R. Matthews
  • Patent number: 5217982
    Abstract: This invention relates to compounds which are derivatives of cyclopentane which are useful as antihypertensive agents, to pharmaceutical compositions including such compounds, and to their use in treating hypertension.
    Type: Grant
    Filed: November 15, 1990
    Date of Patent: June 8, 1993
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Cynthia A. Fink, Alfred P. Spada
  • Patent number: 5196454
    Abstract: The invention relates to novel 2,5-diaminotetralines of the formula: ##STR1## wherein R1, R2, R3 and R4 are defined herein, processes for preparing them and their use in pharmaceutical compositions. The novel 2,5-diaminotetralines are useful in treating diseases caused by disorders of the dopaminergic systems.
    Type: Grant
    Filed: June 15, 1990
    Date of Patent: March 23, 1993
    Assignee: Boehringer Ingelheim KG
    Inventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
  • Patent number: 5166402
    Abstract: Herbicidal .alpha.-(5-aryloxy-naphthalen-1-yl-oxy)propionic acid derivatives of the formula ##STR1## in which R.sup.1 stands for hydrogen, halogen, cyano or trifluoromethyl,R.sup.2 stands for hydrogen or halogen,R.sup.3 stands for halogen, cyano, trifluoromethyl or trifluoromethoxy,R.sup.4 stands for hydrogen or halogen,R.sup.5 stands for hydrogen or halogen andZ stands for halogen, hydroxyl, amino, alkylamino, alkenylamino, alkinylamino, arylamino, aralkylamino, alkoxycarbonylalkylamino, cyanamino, dialkylamino, dialkenylamino, alkylsulphonylamino, arylsulphonylamino, hydroxylamino, alkoxyamino, hydrazino, alkylsulphonylhydrazino, arylsulphonylhydrazino, alkylthio, arylthio, aralkylthio, alkoxycarbonylalkylthio or for the --O--R.sup.6 group,wherein R.sup.6 can be various organic radicals.The starting material naphthol of the formula ##STR2## is also new.
    Type: Grant
    Filed: November 1, 1990
    Date of Patent: November 24, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Haug, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
  • Patent number: 5166434
    Abstract: A process is disclosed for preparing aromatic-substituted unsaturated amides. The process comprises treating a compound of the formula ##STR1## where Ar is C.sub.6 to C.sub.10 aryl unsubstituted or substituted with at least one halo, amino, nitro, hydroxy, C.sub.1 to C.sub.12 linear or branched alkyl, C.sub.1 to C.sub.12 linear or branched alkoxy or haloalkyl, the alkyl moiety being C.sub.1 to C.sub.6 linear or branched or the group ##STR2## where Ar' is C.sub.6 to C.sub.10 aryl unsubstituted or substituted with at least one halo, amino, nitro, hydroxy, C.sub.1 to C.sub.12 linear or branched alkyl, C.sub.1 to C.sub.12 alkoxy or haloalkyl, the alkyl moiety being C.sub.1 to C.sub.6 linear or branched; and R and R' are the same or different and are hydrogen or C.sub.1 to C.sub.12 linear or branched alkyl and can also be phenyl unsubstituted or substituted with at least one halo, amino, nitro, hydroxy, C.sub.1 to C.sub.12 linear or branched alkyl, C.sub.1 to C.sub.
    Type: Grant
    Filed: April 1, 1991
    Date of Patent: November 24, 1992
    Assignee: Ethyl Corporation
    Inventor: Kathleen S. Laurenzo
  • Patent number: 5155271
    Abstract: The invention relates to a process for the preparation of compounds of the formula ##STR1## in which Q is substituted or unsubstituted C.sub.1 -C.sub.6 alkyl, A is a direct bond or a bridging member, s is the number 1 or 2, Z is a radical of the formula --CH.sub.2 CH.sub.2 OH, --CH.dbd.CH.sub.2 or --CH.sub.2 CH.sub.2 --Y, and Y is a leaving group, and the benzene or napthalene nucleus I can be further substituted, which comprises reacting compounds of the formula ##STR2## with compounds of the formulaQ--OH (3)in which A, s, Z and Q are as defined under formula (1), in the presence of hydrogenation catalysts, and then carrying out further conversion reactions where appropriate.The compounds obtained by the process according to the invention are suitable as intermediates for the preparation of reactive dyes.
    Type: Grant
    Filed: June 25, 1990
    Date of Patent: October 13, 1992
    Assignee: Ciba-Geigy Corporation
    Inventor: Peter Aeschlimann
  • Patent number: 5153226
    Abstract: The present invention are novel amino acid amide compounds of the following general formula which inhibit the enzyme acylcoenzyme A:cholesterol acyltransferase: ##STR1## wherein R is phenyl or 1- or 2-naphthyl which are unsubstituted or may be substituted; R.sub.1 is hydrogen or a straight or branched alkyl group having from 1 to 6 carbon atoms; R.sub.2 is hydrogen, an aliphatic group, an aromatic group, an aralkyl or diarylalkyl group or R.sub.1 and R.sub.2 form a carbocyclic group; R.sub.3 is hydrogen, an aliphatic group, an aralkyl group wherein the alkyl moiety may contain a carbocyclic entity; R.sub.4 is hydrogen, an aliphatic group, SO.sub.2 R.sub.14, --C(.dbd.S)NHR.sub.15, --CO.sub.2 R.sub.15, --COR.sub.18, or --C(.dbd.O)NHR.sub.15 wherein R.sub.14 is morpholino, phenyl or substituted phenyl; R.sub.15 is an alkyl group, phenyl or phenylalkyl wherein the phenyl group may be substituted; and R.sub.18 is the same is R.sub.15 or is halo-substituted alkyl, 9-fluoroenylmethylene or pyrrolidino.
    Type: Grant
    Filed: July 30, 1990
    Date of Patent: October 6, 1992
    Assignee: Warner-Lambert Company
    Inventors: Alexander W. Chucholowski, Mark W. Creswell, William H. Roark, Ila Sircar
  • Patent number: 5141960
    Abstract: A class of tricyclic glycinamide derivatives is described having use in treatment of CNS dysfunctions such as epilepsy and convulsive disorders. Compounds of most interest are those of the formula ##STR1## wherein each of X and Y is hydrido; wherein Z is selected from methylene, ethylene, ethenylene, thiomethylene and thioethylene; and wherein each of R.sup.1, R.sup.2 and R.sup.3 is hydrido; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: June 25, 1991
    Date of Patent: August 25, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Alexis A. Cordi, Claude L. Gillet
  • Patent number: 5136082
    Abstract: Disclosed is a process for the preparation of organic esters and amides by reacting (a) a 5 to 60 mole % excess of an ester of (substituted-4-hydroxyphenyl) alkanoic acid with (b) (i) a C.sub.4 -C.sub.20 aliphatic alcohol or thioether alcohol having one or more hydroxyl groups or (ii) an amine of the formula, (R"').sub.2 N(CH.sub.2).sub.n R"" wherein R"' is hydrogen, C.sub.1-7 alkyl, C.sub.5-12 cycloalkyl, or C.sub.6-12 aryl, provided that one R"' is hydrogen, and R"" is hydrogen or N(R"').sub.2 wherein R"' is a defined above, in the presence of a catalyst system comprising a basic inorganic compound and a polar aprotic organic compound. The process provides higher yields of the desired product, shorter reaction times, and reduces the production of undesirable side-products.
    Type: Grant
    Filed: August 3, 1990
    Date of Patent: August 4, 1992
    Assignee: Himont Incorporated
    Inventors: Vu A. Dang, Gleason O. Cookson, Krishna Raman
  • Patent number: 5136081
    Abstract: The invention provides a process for the preparation of fungicidally active cyclopentene derivatives of the general formula ##STR1## cyclopentane derivatives of the general formula ##STR2## and cyclohexane derivatives of the general formula ##STR3## in which n, R, R.sup.1, R.sup.2, R.sup.5, X and Y are as herein defined. Compounds of formula II and III are also provided which are useful as intermediates in the preparation of certain fungicidally active cyclopentane derivatives.
    Type: Grant
    Filed: September 11, 1989
    Date of Patent: August 4, 1992
    Assignee: Shell Internationale Research Maatschappij B.V.
    Inventor: Paul H. Briner
  • Patent number: 5118697
    Abstract: Novel cyclic beta-ketoamides which contain an aryl moiety having utility as blood cholesterol lowering agents rendering them useful in the treatment of atherosclerosis.
    Type: Grant
    Filed: March 6, 1991
    Date of Patent: June 2, 1992
    Assignee: Warner-Lambert Company
    Inventors: Corinne E. Augelli-Szafran, Bharat K. Trivedi
  • Patent number: 5112868
    Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.
    Type: Grant
    Filed: May 2, 1990
    Date of Patent: May 12, 1992
    Assignee: Warner-Lambert Company
    Inventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
  • Patent number: 5110983
    Abstract: Compounds of the formula I ##STR1## can be prepared by various process steps from 2-(4-methylphenyl)-2-hexafluoroisopropanol.Hexafluoroisopropyl-containing monomers are important starting compounds in the preparation of linear polycarboxamides and polycarboximides.
    Type: Grant
    Filed: March 22, 1990
    Date of Patent: May 5, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jurgen Lau, Gunter Siegemund, Freimund Rohrscheid
  • Patent number: 5087743
    Abstract: 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: January 23, 1990
    Date of Patent: February 11, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5079263
    Abstract: R.sup.2 is H or OH;R.sup.3 is H, OH, OCH.sub.3, CH.sub.3 or NH.sub.2 ;Rhu 4 is H, OH, OCH.sub.3, NH.sub.2 or ##STR2## The compounds of the formula I are prepared by fermentation of the strain Streptomyces parvulus DSM 40722 in the presence of substituted benzoic acids of the general formula II ##STR3## where R.sup.1 is H or OH;R.sup.2 is H or OH;R.sup.3 is H, OH, OCH.sub.3, CH.sub.3 or NH.sub.2 ;R.sup.4 is H, OH, OCH.sub.3 or NH.sub.2,and they inhibit Leukocyte elastase and can be used as pharmaceuticals.
    Type: Grant
    Filed: December 2, 1988
    Date of Patent: January 7, 1992
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Axel Zeeck, Ralf Thiericke, Hans Zahner, Gerhard Dickneite, Hans H. Sedlacek
  • Patent number: 5068392
    Abstract: 2-Chloro and 2,6-dichloroanilines, optionally substituted in the 3-, 5-, and/or 6-position are prepared from the corresponding anilides by selective bromination, chlorination, reduction and hydrolysis. The selectivity of the process for introducing chlorines ortho to the amino group is very high.
    Type: Grant
    Filed: January 24, 1991
    Date of Patent: November 26, 1991
    Assignee: DowElanco
    Inventors: Lennon H. McKendry, Mark W. Zettler
  • Patent number: 5055582
    Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.
    Type: Grant
    Filed: December 13, 1988
    Date of Patent: October 8, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert B. Garland, Masateru Miyano
  • Patent number: 5047420
    Abstract: Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.
    Type: Grant
    Filed: August 21, 1989
    Date of Patent: September 10, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Donald W. Graham, Tesfaye Biftu, John C. Chabala, Michael N. Chang, Yuan-Ching P. Chiang, Kathryn L. Thompson, Shu S. Yang
  • Patent number: 5047410
    Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.
    Type: Grant
    Filed: July 12, 1989
    Date of Patent: September 10, 1991
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Arturo Donetti, Marco Turconi, Massimo Nicola, Rosamaria Micheletti
  • Patent number: 5028732
    Abstract: Compounds having the formula ##STR1## wherein Q is substituted phenyl or substituted pyridyl; Y is nitro, cyano, or halogen; R is a group of the formula --(CHR.sup.1).sub.m --A--(CH.sup.2)--.sub.n --R.sup.3 wherein R.sup.1 and R.sup.2, independently of each other and in each (CHR.sup.1) and (CHR.sup.2) group, are hydrogen, unsubstituted or substituted alkyl, alkoxy, or alkylthio; A is --N(R.sup.1)--, --N(O)--, --O--, --S--, --S(O)--, --S(O).sub.2 --, --C(O)--, --C(O)B--, or --N(H)S(O).sub.2 --; B is alkylene, --O--, --S--, or --N(R.sup.4)--; R.sup.3 is cyano, halogen, or C(O)Z; R.sup.4 is hydrogen or unsubstituted or substituted alkyl; Z is hydrogen, unsubstituted or substituted alkyl, --N(R.sup.4).sub.2, --OR.sup.5, --SR.sup.5, or --N(R.sup.4)SO.sub.2 R.sup.6 ; R.sup.5 is hydrogen, unsubstituted or substituted alkyl, or an agronomically-acceptable cation; R.sup.
    Type: Grant
    Filed: March 13, 1986
    Date of Patent: July 2, 1991
    Assignee: Rohm and Haas Company
    Inventors: Ann H. Beaulieu, Roy Y. Yih
  • Patent number: 5013757
    Abstract: A novel compound of the formula (I): ##STR1## wherein R.sub.1 is optionally esterified or amidated carboxyl; R.sub.2, R.sub.3 and R.sub.4 are the same or different and are hydrogen or alkyl; A is formyl, hydroxyiminomethyl or carboxyl; and X is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active component the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R.sub.1 is carboxyl, R.sub.2, R.sub.3 and R.sub.4 are hydrogen and X is formyl are also disclosed.
    Type: Grant
    Filed: April 13, 1990
    Date of Patent: May 7, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tsuneo Kanamaru, Tsuneaki Hida, Masayuki Muroi
  • Patent number: 5011992
    Abstract: Novel substituted benzamides of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A are as defined herein are useful in the treatment of emesis, and particularly chemotherapy-induced emesis in cancer patients. Some of the compounds are also useful in disorders relating to impaired gastric motility.
    Type: Grant
    Filed: August 22, 1989
    Date of Patent: April 30, 1991
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ivo Monkovic, David Willner
  • Patent number: 5011628
    Abstract: Substituted benzamidines and their hydrochloride salts are useful as ultraviolet light absorbers, the benzamidines having the formula ##STR1## wherein: A.sup.1 and A.sup.2 may be the same or different and represent --COOR.sup.1, --CONR.sup.1 R.sup.2, --C.tbd.N or --C.sub.6 H.sub.5 ;A.sup.3 represents --H, --OH, --OR, --Cl, --NO.sub.2, --C.tbd.N, --C.sub.6 H.sub.5, or an alkyl group of one to five carbon atoms;R.sup.1 and R.sup.2 may be the same or different and represent hydrogen or an alkyl group of one to ten carbon atoms; and,R represents an alkyl group of one to ten carbon atoms.
    Type: Grant
    Filed: April 11, 1989
    Date of Patent: April 30, 1991
    Assignee: Givaudan Corporation
    Inventors: Isaac D. Cohen, Joseph A. Virgilio
  • Patent number: 5002605
    Abstract: Compounds having the formula ##STR1## wherein R is C.sub.1 -C.sub.6 lower alkoxy; C.sub.1 -C.sub.6 lower alkylthio; 3- to 6-membered heterocycle or substituted heterocycle; phenyl or substituted phenyl; R.sub.1 is hydrogen or C.sub.1 -C.sub.3 lower alkyl; R.sub.2 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.3 lower alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.3 lower alkylalkoxy or combinations thereof; R.sub.3 and R.sub.4 are independently selected from the group consisting of hydrogen; C.sub.1 -C.sub.6 lower alkyl; C.sub.2 -C.sub.6 lower alkenyl; C.sub.2 -C.sub.6 lower alkynyl; 3- to 6-membered heterocyle or substituted heterocycle; alkyl heterocycle or substituted alkyl heterocycle; phenyl or substituted phenyl; and where R.sub.3 l or R.sub.4 is a basic heterocyle, herbicidally acceptable organic or inorganic salts thereof are herbicidally active.
    Type: Grant
    Filed: December 21, 1988
    Date of Patent: March 26, 1991
    Assignee: ICI Americas Inc.
    Inventors: Francis H. Walker, Don R. Baker
  • Patent number: 5001159
    Abstract: A compound of formula (I) ##STR1## in which: X denotes hydrogen, a halogen, a trifluoromethyl group, a C.sub.1 -C.sub.4 alkyl group or a C.sub.1 -C.sub.4 alkoxy group;R.sub.1 denotes a linear or branched C.sub.2 -C.sub.8 alkyl group, a C.sub.3 -C.sub.5 cycloalkyl group or a cycloalkylmethyl group in which the cycloalkyl moiety has from 3 to 5 carbon atoms;R.sub.2 denotes hydrogen or a C.sub.1 -C.sub.4 alkyl group;R.sub.3 denotes hydrogen, a C.sub.1 -C.sub.4 alkyl group, an optionally substituted phenylalkyl group or a pyridylalkyl group;or R.sub.2 and R.sub.3 denote, together with the nitrogen to which they are attached, a pyrrolidinyl, piperidyl, morpholinyl, perhydrothiazinyl, piperazinyl or 4-methylpiperazinyl ring; andAr denotes a phenyl group, optionally having from one to three substituents, each of which is, independently, a halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.
    Type: Grant
    Filed: May 2, 1990
    Date of Patent: March 19, 1991
    Assignee: Synthelabo
    Inventors: Christian Hoornaert, Jean-Claude Muller, Nigel Beeley
  • Patent number: 4999186
    Abstract: The present invention relates to novel sunscreen agents which have the ability to absorb both UVA and UVB wavelength radiation. The sunscreen agents comprise a specific type of UVA-absorbing chromophore covalently bonded to a specific type of UVB-absorbing chromophore. The chromophore moieties are covalently bonded together such that the electron systems of these moieties are not directly coupled.The present invention further relates to sunscreen compositions containing the hereinbefore described type of sunscreen agents. Furthermore, the present invention relates to methods for protecting the skin of humans or lower animals from the effects of UVA and UVB wavelength radiation. This method comprises topically applying to the skin an effective coating of a sunscreen composition of the present invention.
    Type: Grant
    Filed: June 2, 1987
    Date of Patent: March 12, 1991
    Assignee: The Procter & Gamble Company
    Inventors: Anthony D. Sabatelli, Josephine A. Spirnak
  • Patent number: 4943310
    Abstract: The invention relates to new 4-benzoyl-3-hydroxy-5-oxo-3-cyclohexenecarboxylic acid derivatives of general formula I ##STR1## in which A, B, R.sup.1, R.sup.2, R.sup.2 and R.sup.3 have the meanings given in the description, and their use as plant growth regulants.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: July 24, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Alfred Angermann, Helga Franke, Gerhard Johann
  • Patent number: 4939133
    Abstract: The present invention relates to novel N-substituted 2-hydroxybenzamide and N-substituted 2-hydroxy-.alpha.-oxo-benezene acetamide compounds pharmaceutical compositions, and methods of use for therefore for the treatment of diseases in which products having lipoxygenase enzyme activity contribute to the pathological condition. Selected novel intermediates are also the present invention.
    Type: Grant
    Filed: October 1, 1985
    Date of Patent: July 3, 1990
    Assignee: Warner-Lambert Company
    Inventors: David T. Connor, Daniel L. Flynn, Wiaczeslaw A. Cetenko, Jagadish C. Sircar, Charles F. Schwender, Elizabeth A. Johnson, Roderick J. Sorenson, Paul C. Unangst
  • Patent number: 4935543
    Abstract: A novel compound of the formula (I): ##STR1## wherein R.sub.1 is optionally esterified or amidated carboxyl; R.sub.2, R.sub.3 and R.sub.4 are the same or different and are hydrogen or halogen or alkyl; A is formyl, hydroxyiminomethyl or carboxyl; and A is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active compound the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R.sub.1 is carboxyl, R.sub.2, R.sub.3 and R.sub.4 are hydrogen and X is formyl are also disclosed.
    Type: Grant
    Filed: May 18, 1989
    Date of Patent: June 19, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tsuneo Kanamaru, Tsuneaki Hida, Masayuki Muroi
  • Patent number: 4921998
    Abstract: Antithrombotic, antiatherosclerotic and antiischaemic compounds of the formula ##STR1## in which R.sup.1 is ##STR2## or SO.sub.2 R.sup.4, R.sup.3 is aryl, substituted aryl, heteroaryl, aralkyl or the group ##STR3## R.sup.4 is aryl or substrituted aryl, R.sup.2 is OH, alkoxy, phenoxy, benzoxy or NR.sup.5 R.sup.6, andR.sup.5 and R.sup.6 each independently is hydrogen or alkyl, orone of the radicals R.sup.5 or R.sup.6 is benzyl, and physiologically acceptable salts thereof with mono- and divalent cations.
    Type: Grant
    Filed: May 15, 1989
    Date of Patent: May 1, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Niewohner, Franz-Peter Hoever, Bodo Junge, Elisabeth Perzborn, Friedel Seuter, Volker-Bernd Fiedler
  • Patent number: 4915727
    Abstract: A plant male sterilant, which comprises as an active ingredient a compound having the formula (I): ##STR1## in which X is --OH, --O.sup.- M.sup.+, --OR.sup.1 or ##STR2## wherein M.sup.+ is an alkali metal cation, an alkaline earth metal cation or ##STR3## in which R.sup.4, R.sup.5 and R.sup.6 are the same or different and each is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.4 alkenyl group, C.sub.3 -C.sub.4 alkynyl, C.sub.3 -C.sub.8 cycloslkyl, benzyl or phenyl group;R.sup.1 is a C.sub.1 -C.sub.9 alkyl, a C.sub.3 -C.sub.6 alkenyl, a C.sub.3 -C.sub.4 alkynyl, C.sub.1 -C.sub.3 alkoxy (C.sub.1 -C.sub.4)-alkyl, C.sub.3 -C.sub.8 cycloalkyl, benzyl or phenyl; andR.sup.2 and R.sup.3 are the same or different and each is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, a benzyl group in which at most two hydrogen atoms at the .alpha.-position thereof may be substituted by methyl, C.sub.2 -C.sub.
    Type: Grant
    Filed: December 24, 1987
    Date of Patent: April 10, 1990
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masato Mizutani, Masao Shiroshita, Nobuaki Mito, Hiroki Okuda, Masaharu Sakaki