Z-c(=o)-o-y, Wherein Z Contains A Benzene Ring Patents (Class 514/532)
  • Patent number: 4994495
    Abstract: Fungicidal compounds having the formula: ##STR1## and stereoisomers thereof, wherein R.sup.1 is optionally substituted C.sub.2-10 alkenyl, optionally substituted C.sub.5-6 cycloalkenyl, optionally substituted C.sub.2-10 alkynyl, or C.sub.1-10 alkyl substituted with --CN, --NC, --COR.sup.2, --CO.sub.2 R.sup.2, --NO.sub.2 or --SCN; X is O, S(O)n or NR.sup.2 and is attached to the 3- or the 4-position of the phenyl ring; Y and Z, which may be the same or different, are H, halogen, --CH.sub.3, --C.sub.2 H.sub.5, or --OCH.sub.3 ; R.sup.2 is H, C.sub.1-4 alkyl, C.sub.1-4 alkenyl, or, when R.sup.2 is C.sub.1-4 alkyl in the group --COR.sup.2, it joins with the alkyl group to which --COR.sup.2 is attached to form a 5- or 6-membered aliphatic ring; and n is 0, 1 or 2.
    Type: Grant
    Filed: May 11, 1989
    Date of Patent: February 19, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Paul J. de Fraine, Michael G. Hutchings, Ian Ferguson
  • Patent number: 4992468
    Abstract: Compounds of the following formula, useful for treating diseases affected by retinoids, are disclosed herein.
    Type: Grant
    Filed: July 26, 1989
    Date of Patent: February 12, 1991
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 4970234
    Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, or --CH.dbd.CH--;wherein Z is OR.sup.1 or --NR.sup.4 R.sup.5 ;wherein R.sup.1 is hydrogen, lower alkyl, or a pharmaceutically acceptable cation;wherein R.sup.2 is H, --CH.sub.3 or --C.sub.2 H.sub.5 ;wherein R.sup.3 is OH, H or --O;wherein R.sup.4 and R.sup.5 may independently be hydrogen, or lower alkyl having 1-6 carbon atoms, or R.sup.4 and R.sup.5 may act together with N to form a cyclic amide of the formula: ##STR2## wherein n is an integer from 4-5; and m is an integer from 0-4. More particularly, this invention relates to compounds of the above formula which have utility as LTB.sub.4 antagonists.
    Type: Grant
    Filed: August 7, 1989
    Date of Patent: November 13, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Richard A. Haack, Stella S. Yu
  • Patent number: 4968718
    Abstract: A nonsteroidal anti-inflammatory drug which is phenylacetic acid derivative and methods of using the same in topically controlling eye inflammations.
    Type: Grant
    Filed: January 25, 1988
    Date of Patent: November 6, 1990
    Assignee: University of Iowa Research Foundation
    Inventors: Ronald D. Schoenwald, Charles F. Barfknecht
  • Patent number: 4968710
    Abstract: Novel compounds which are 2,6-di-t-butylphenols substituted in the 4 position by an alkoxy or benzyloxy group or a benzylthio group, which alkoxy or benzyloxy group is directly substituted by a tetrazole ring, and which benzylthio group is directly substituted by carboxy or tetrazolyl are useful as inhibitors of leukotriene biosynthesis and as antiallergic agents. Synthetic intermediates for preparing such compounds are also described.
    Type: Grant
    Filed: September 26, 1988
    Date of Patent: November 6, 1990
    Assignee: Riker Laboratories, Inc.
    Inventor: Mark A. Rustad
  • Patent number: 4966915
    Abstract: An L-dopa derivative represented by formula (I) ##STR1## wherein one of R.sup.1 and R.sup.2 denotes a hydrogen atom and the other denotes a group of formula R--CO-- in which R denotes an alkyl, alkenyl, optionally substituted cycloalkyl, optionally substituted phenyl, optionally substituted aralkyl, lower alkoxy or optionally substituted aralkyloxy group,and its acid addition salt. The compounds are useful in the medical field, especially in the treatment of a series of diseases called Parkinson's disease or Parkinsonism.
    Type: Grant
    Filed: September 16, 1988
    Date of Patent: October 30, 1990
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Yoshimi Tsuchiya, Masahiro Hayashi, Hiroshi Takehana, Akihiro Hisaka, Yoshio Sawasaki, Masaki Ihara
  • Patent number: 4965287
    Abstract: In the control of parasitoses in honey bees by applying to the bees, their food or their habitat a parasiticide which is selectively active against such parasitoses but not against said bees, the improvement wherein such parasiticide is a synthetic pyrethroid.
    Type: Grant
    Filed: March 2, 1989
    Date of Patent: October 23, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wilhelm Stendel, Hubert Neuhauser, Nikolaus Koeniger
  • Patent number: 4960793
    Abstract: Novel diethylene glycol monoester of antirheumatically effective acids, e.g., lonazolac and diclofenac and others are disclosed which have inflammation inhibitory properties superior to the corresponding acid base forms. They may be produced through direct esterification without elimination of water and are suitable in the fight against diseases of the rheumatic complex.
    Type: Grant
    Filed: March 31, 1989
    Date of Patent: October 2, 1990
    Assignee: Merckle GmbH
    Inventors: Gunter Metz, Kurt Rauchle, Manfred Erdmann
  • Patent number: 4959383
    Abstract: Phenylsulfone alkenoic acids and derivatives thereof are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, X is COOR wherein R is hydrogen, alkali metal or lower alkyl or X is 5-tetrazolyl or ##STR2## wherein R' is lower alkyl or aryl; n is 2, 3 or 4 and m is 2, 3 or 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasospastic disease.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: September 25, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Steven E. Hall
  • Patent number: 4952580
    Abstract: Polyhaloalkene compounds of the formula: ##STR1## wherein X is sulfur, oxygen, or nitrogen, Y.sup.1 and Y.sup.2 are fluorine, Z is hydrogen or the same as Y.sup.1 and Y.sup.2, and n is 1-4; provided that:(A) when X is sulfur, Z is fluorine and R is thienyl or substituted thienyl, thianaphthyl or substituted thianaphthyl, thiazolinyl or substituted thiazolinyl, oxadiazolyl or substituted oxadiazolyl, 3,4,4-trifluoro-3-butenyloxycarbonylmethyl, thiadiazolyl substituted by halogen or R.sup.2 S, wherein R.sup.2 is 3,4,4-trifluoro-3-butenyl or R.sup.2 is phenylmethyl or phenylthiomethyl each optionally substituted by halogen or nitro; or R is thiadiazolyl substituted by R.sup.3, wherein R.sup.3 is substituted aryl, arylalkyl, aryloxyalkyl, alkylthio, haloalkylthio, haloarylthio, cyanoalkylthio, arylalkylthio, aryloxyalkylthio, arylthioalkylthio, heterocycloalkylthio, alkenylthio, haloalkenylthio, halocycloalkylalkenylthio, wherein said aryl or heterocyclic groups of R.sup.
    Type: Grant
    Filed: November 9, 1988
    Date of Patent: August 28, 1990
    Assignee: FMC Corporation
    Inventors: Anthony J. Martinez, Thomas G. Cullen
  • Patent number: 4952565
    Abstract: A new inclusion complex of ibuproxam with beta-cyclodextrin is described, which is prepared by adding ibuproxam to a boiling aqueous solution of beta-cyclodextrin, stirring the reaction mixture at the boiling temperature, cooling to a temperature of 0.degree. C. to 5.degree. C. and isolating the title complex.The analgesic, antipyretic and antiinflammatory properties of the inclusion complex of ibuproxam with beta-cyclodextrin are equivalent to those of ibuproxam alone, but owing to its better water-solubility the complex can be more easily formulated into pharmaceutical forms.
    Type: Grant
    Filed: November 13, 1987
    Date of Patent: August 28, 1990
    Inventors: Janko Zmitek, Jenny Milovac, Zdravko Kopitar, Mirjan Zorz, Boris Rusjakovski
  • Patent number: 4950669
    Abstract: The growth rate of an animal is stimulated by administering to the animal a growth promoting amount of a compound of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are each selected from the group consisting of hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms and halogen; X is selected from carbonyl and a ketal group of the formula ##STR2## wherein R.sub.6 and R.sub.7, which can be the same or different, are each selected from hydrogen and alkyl having 1 to 3 carbon atoms; A is a linear or branched alkylene having from 1 to 8 carbon atoms; and R.sub.8 and R.sub.9, which can be the same or different, are each selected from the group consisting of hydrogen, alkyl having 1 to 4 carbon atoms, or 2-hydroxy-alkyl wherein the alkyl group has 2 to 4 carbon atoms, or R.sub.8 and R.sub.
    Type: Grant
    Filed: July 19, 1988
    Date of Patent: August 21, 1990
    Assignee: Cometec s.r.l.
    Inventors: Aldo Garzia, Umberto Bucci
  • 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: 4942174
    Abstract: Novel alkyl aryl ether derivatives corresponding to the formula: ##STR1## in which R.sup.1 is a C.sub.8 -C.sub.20 alkyl group with one or more branches, E is a group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH-- and R.sup.2 is a C.sub.1 -C.sub.4 alkyl group, a C.sub.2 -C.sub.4 hydroxyalkyl group, an alkoxyalkyl group containing 1 to 4 C atoms in the alkoxy group and 2 to 4 C atoms in the alkyl group, hydrogen or a salt-forming cation, are highly effective sebosuppressive agents in cosmetic or pharmaceutical preparations for topical application to the hair and to the skin.
    Type: Grant
    Filed: November 10, 1988
    Date of Patent: July 17, 1990
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: Hinrich Moeller, Siegfried Wallat
  • Patent number: 4940696
    Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.
    Type: Grant
    Filed: November 16, 1987
    Date of Patent: July 10, 1990
    Assignee: Centre International de Recherches Dermatologioues (CIRD)
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
  • Patent number: 4935409
    Abstract: Animal growth promoters of the formula ##STR1## The intermediates of the formula ##STR2## are also new.
    Type: Grant
    Filed: April 27, 1988
    Date of Patent: June 19, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hartmund Wollweber, Jurgen Stoltefuss, Friedrich Berschauer
  • Patent number: 4933367
    Abstract: This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.
    Type: Grant
    Filed: March 12, 1987
    Date of Patent: June 12, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuhnle
  • Patent number: 4929641
    Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.
    Type: Grant
    Filed: May 11, 1988
    Date of Patent: May 29, 1990
    Assignee: Schering Corporation
    Inventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 4929642
    Abstract: A method of combating agricultural pest comprising applying a pesticidally effective amount of a substituted 1,4-naphthoquinone on agricultural pests and/or their environment, said 1,4-naphthoquinone being of the formula ##STR1## in which n represents the number zero or a number from 1 to 12,R.sup.1 represents hydrogen, t-butylcarbonyl or acetyl andR.sup.2 represents phenyl which is substituted by bromine, fluorine, chlorine, trifluoromethyl, trifluoromethoxy, trifluoromethylsulphenyl, trifluoromethylsulphonyl or trimethylsilyl or cyclohexyl which is substituted by methyl, trifluoromethyl or trimethylsilyl orR.sup.2 represents C.sub.1 -C.sub.8 -alkyl which is substituted by fluorine, chlorine or bromine.
    Type: Grant
    Filed: June 29, 1988
    Date of Patent: May 29, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Werner Lindner, Benedikt Becker, Robert Steffens, Ulrike Wachendorff-Neumann, Wilhelm Brandes, Wilhelm Stendel, Stefan Dutzmann
  • Patent number: 4914128
    Abstract: Acrylates of the general formula ##STR1## where R.sup.1 and R.sup.2 independently of one another are each C.sub.1 -C.sub.8 -alkyl, X is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen, C.sub.1 -C.sub.4 -alkoxy, haloalkyl, cyano or nitro, W is unsubstituted or alkyl-substituted, saturated or unsaturated C.sub.1 -C.sub.10 -alkylene, Y is hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aralkyl, aryl, aryloxy, halogen, an unsubstituted or substituted C.sub.4 H.sub.4 chain which is fused to the benzene radical, alkoxy, haloalkoxy, alkylthio, thiocyanato, cyano, NO.sub.2, ##STR2## where R' and R" independently of one another are each hydrogen, alkyl, alkoxy, alkylthio or cycloalkyl, or are phenyl which is unsubstituted or substituted by alkyl, halogen or alkoxy, m is 0 or 1, n is from 1 to 4 and Z is oxygen, sulfur, SO or SO.sub.2, and fungicides containing them.
    Type: Grant
    Filed: October 11, 1988
    Date of Patent: April 3, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulrich Schirmer, Stefan Karbach, Ernst-Heinrich Pommer, Eberhard Ammermann, Wolfgang Steglich, Barbara A. M. Schwalge, Timm Anke
  • Patent number: 4913721
    Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: April 3, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey
  • Patent number: 4908388
    Abstract: Derivatives of carbonyl-group containing behavior modifying compounds, in which said carbonyl group has been converted to a photolabile group which regenerates the carbonyl group on exposure to radiation, are of value in various methods for the control of animal, and in particular insect, species.
    Type: Grant
    Filed: January 20, 1988
    Date of Patent: March 13, 1990
    Assignee: National Research Development Corporation
    Inventors: John A. Pickett, Ewen D. M. Macaulay
  • Patent number: 4902717
    Abstract: Compounds having thromboxane antagonist activity are of use in the treatment of hormone-dependent neoplasias for example oestrogen-dependent neoplasias. Thromboxane antagonists of particular value are compounds of formula (I) ##STR1## wherein ##STR2## represents one of the divalent cyclic groups ##STR3## the letters a and b indicating in each case the points of attachment of the substituents R.sup.1 and CV(R.sup.2)--NV'R, respectively; R.sup.
    Type: Grant
    Filed: September 3, 1986
    Date of Patent: February 20, 1990
    Assignee: National Research Development Corporation
    Inventors: Judith Senior, Kay M. Troughton
  • Patent number: 4902709
    Abstract: Novel antihypercholesterolemic compounds of structure (I) or (II), ##STR1## pharmaceutically acceptable salts, thereof and a novel process for preparing compounds of structure I, are disclosed.
    Type: Grant
    Filed: August 12, 1988
    Date of Patent: February 20, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Gerald E. Stokker
  • Patent number: 4898883
    Abstract: The present invention relates to 1-substituted derivatives of 4-methoxy-2,3,6-trimethylbenzene which are useful in cosmetic or pharmaceutical preparations for use in the treamtnet of dermatological complaints connected with a keratinisation disorder, dermatological complaints having an inflammatory and/or immuno-alleric component or ophthalmological complaints.
    Type: Grant
    Filed: July 21, 1987
    Date of Patent: February 6, 1990
    Assignee: L'Oreal
    Inventors: Gerard Lang, Serge Forestier, Alain Lagrange, Braham Shroot
  • Patent number: 4898864
    Abstract: Bicyclic aromatic compound having the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent hydrogen or alkyl, at least two of R.sub.1 -R.sub.4 radicals being other than hydrogen,A represents methylene or dimethylene; when A represents dimethylene, R.sub.1 and R.sub.3 together can form a methylene or dimethylene radical,R.sub.5 and R.sub.6 represent hydrogen, halogen, lower alkyl, lower alkoxy or hydroxy,R' represents hydrogen, hydroxy, alkoxy, C.sub.1 -C.sub.4 cicyloxy or amino,R" represents hydrogen or lower alkoxy, or R' and R" together form an oxo, methano or hydroxyimino radical,B represents cyclohexyl, cyclohexenyl, cyclohexadienyl or phenyl, substituted or not,R represents --CH.sub.2 OH or --COR.sub.7,R.sub.7 represents hydrogen, --OR.sub.8 or ##STR2## R.sub.8 represents hydrogen, C.sub.1 -C.sub.20 alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl, aralkyl or a sugar residue.
    Type: Grant
    Filed: October 27, 1987
    Date of Patent: February 6, 1990
    Assignee: L'Oreal
    Inventors: Jean Maignan, Gerard Lang, Gerard Malle, Philippe Vingler
  • Patent number: 4889847
    Abstract: The present invention is directed to the topical administration of a retinoid-containing pharmaceutical composition for the prevention of glucocorticoid-induced skin atrophy.
    Type: Grant
    Filed: November 3, 1986
    Date of Patent: December 26, 1989
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Albert M. Kligman, James A. Mezick, Robert J. Capetola
  • Patent number: 4889870
    Abstract: There are provided new 2-(2,2-difluorocyclopropyl)alkyl esters of general formula I ##STR1## in which Y, R.sub.1-7 and n have the meanings given in the description and processes for their preparation. The new compounds can be used to combat insects and mites.
    Type: Grant
    Filed: January 29, 1988
    Date of Patent: December 26, 1989
    Assignee: Schering Aktiengesellschaft
    Inventors: Peter Wegner, Hans-Rudolf Kruger, Dietrich Baumert, Hartmut Joppien
  • Patent number: 4886835
    Abstract: Substituted alkadienes of the formula: ##STR1## in which R.sub.1 is hydroxy or acetoxy, R.sub.2 is hydrogen, carboxy, alkoxycarbonyl, phenyl or benzoyl, andR.sub.3 is alkylthio or alkoxy and R.sub.4 is naphthoyl or optionally substituted benzoyl,or R.sub.3 is alkoxycarbonyl, cycloalkyloxycarbonyl or cyano and R.sub.4 is alkyl, naphthyl, optionally substituted phenyl, alkylthio, naphthylmethanethio, optionally substituted benzylthio, optionally substituted phenylthio, naphthylthio, phenethylthio or allylthio,or R.sub.3 and R.sub.4 form, with the carbon atom to which they are attached, a ring-system of formula: ##STR2## in which R.sub.5 is hydrogen or alkoxy and X is methylene or S inhibit 5-lipoxygenase and are useful, for example, as anti-inflammatories.
    Type: Grant
    Filed: September 26, 1988
    Date of Patent: December 12, 1989
    Assignee: Rhone-Poulenc Sante
    Inventors: Jean-Luc Malleron, Gerard Ponsinet, Gerard Roussel
  • Patent number: 4877811
    Abstract: Compounds of the formula: ##STR1## and stereoisomers thereof wherein X and Y, which are the same or different, are hydrogen, halogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted heteroaryloxy, optionally substituted arylalkoxy, optionally substituted heteroarylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6, except that X and Y are not both hydrogen; R.sup.1 and R.sup.2, which are the same or different, are alkyl or fluoroalkyl; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6, which are the same or different, are hydrogen, alkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted aralkyl, or cycloalkylalkyl.
    Type: Grant
    Filed: November 12, 1987
    Date of Patent: October 31, 1989
    Assignee: Imperial Chemical Industries PLC
    Inventors: Vivienne M. Anthony, John M. Clough, Christopher A. Godfrey
  • Patent number: 4877805
    Abstract: Various effects of photoaging or sundamage of skin including impairment of differentiation of epidermal epithelial cells and loss of collagen fibers, abnormal changes in elastic fibers and deterioration of small blood vessels in the dermis of the skin are retarded by applying topically to the epidermis in a maintenance therapy program effective amounts of retinoids including retinoid derivatives and stereoisomers thereof such that epithelial growths are substantially reduced and prevented and the skin substantially regains and maintains its firmness, turgor and elasticity. Moreover, with persistent treatment dermal blood cells and vessels increase and the epidermis and dermis thicken, resulting in improved ability of the skin to sense, resist and recover from irritation or injury. Further, hyperpigmentation, lines and wrinkles due to aging are reduced and prevented. The treatment is particularly useful for human facial skin and preferably applied in amounts insufficient to cause excessive irritation.
    Type: Grant
    Filed: June 3, 1988
    Date of Patent: October 31, 1989
    Inventor: Albert M. Kligman
  • Patent number: 4876280
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl or t-butyl, R.sub.2 is hydrogen or C.sub.1-3 alkyl,R.sub.3 is hydrogen or C.sub.1-3 alkyl,R.sub.4 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl or t-butyl,R.sub.5 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.1-3 alkoxy, n-butoxy, i-butoxy, fluoro, chloro, trifluoromethyl, phenoxy or benzyloxy,R.sub.6 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, fluoro, chloro, trifluoromethyl, phenoxy or benzyloxy, with the provisos that not more than one of R.sub.5 and R.sub.6 is trifluoromethyl, not more than one of R.sub.5 and R.sub.6 is phenoxy, and not more than one of R.sub.5 and R.sub.6 is benzyloxy, orR.sub.5 and R.sub.6 are attached to adjacent carbon atoms and taken together form a radical of the formula --CH.dbd.CH--CH.dbd.CH--,R.sub.6a is hydrogen, C.sub.1-2 alkyl, fluoro or chloro,X is --CH.sub.2 CH.sub.2 -- or ##STR2## wherein R.sub.7 is hydrogen or C.sub.1-3 alkyl, andR.sub.8 is hydrogen, R.
    Type: Grant
    Filed: March 10, 1988
    Date of Patent: October 24, 1989
    Assignee: Sandoz Pharm. Corp.
    Inventor: Robert E. Damon, II
  • Patent number: 4874781
    Abstract: A compound of formula II: ArCHR.sub.1 CO.sub.2 CHDR.sub.2in which formula:Ar represents a phenyl or naphthyl group optionally substituted by one or more halogen, alkoxy, haloalkoxy, methylenedioxy, C.sub.1 -C.sub.6 alkyl or haloalkyl groups;R.sub.1 represents the group --CH(CF.sub.3)CH.sub.3 or --C(CF.sub.3).dbd.CH.sub.2R.sub.2 represents the residue of an alcohol R.sub.2 CHDOH in which D is hydrogen or cyano and of which the [1R, cis]2,2-dimethyl-3-(2,2-dibromovinyl)cyclopropane carboxylic ester is significantly insecticidal.
    Type: Grant
    Filed: January 11, 1988
    Date of Patent: October 17, 1989
    Assignee: National Research Development Corporation
    Inventors: Michael Elliott, Norman F. Janes, Bhupinder P. S. Khambay
  • Patent number: 4867979
    Abstract: Antidiarrheal compositions showing enhanced antidiarrheal activity comprise a non-steroidal anti-inflammatory drug compound and a polymeric hydroabsorptive agent. A patient in need of remedial or preventive treatment of diarrhea symptoms is administered an antidiarrheally effective amount of said antidiarrheal compositions.
    Type: Grant
    Filed: September 30, 1986
    Date of Patent: September 19, 1989
    Assignee: Richardson-Vicks Inc.
    Inventors: Bhogilal B. Sheth, Sheri A. Gilbert, Jane F. Kinsel
  • Patent number: 4867915
    Abstract: Sixteen carbon atom carboxylic acids having 16-phenoxy or 16-phenylthio substituents, and 0, 1, or 4 triple bonds, methods of preparing them, and pharmaceutical preparations containing them. These compounds are useful as lipoxygenase inhibitors.
    Type: Grant
    Filed: May 21, 1986
    Date of Patent: September 19, 1989
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchwoski, Angel Guzman
  • Patent number: 4859697
    Abstract: Substituted acenaphthenes and their use as inhibitors of phospholipase A.sub.2 are provided. The acenaphthenes have the formula ##STR1## wherein R.sup.1 is H or alkyl;R.sup.2 is alkyl, cycloalkyl, or aryl; andR.sup.1 and R.sup.2 taken together are various aryl groups optionally substituted; andA is .dbd.O, .dbd.CH.sub.2 and derivatives thereof, ##STR2## and derivatives thereof, or .dbd.NOH and derivatives thereof.
    Type: Grant
    Filed: October 6, 1988
    Date of Patent: August 22, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: William C. Ripka, William J. Sipio
  • Patent number: 4857551
    Abstract: A method of killing or controlling insect, mite or nematode pests which method comprises applying to the insect or to the locus thereof an effective amount of a compound of the formula (I): ##STR1## wherein R is hydrogen or C.sub.1-4 alkyl; and X, Y and Z are independently selected from hydrogen, halogen, or OR.sup.1 where R.sup.1 is optionally substituted aryl or heteroaryl group. Certain of the compounds are new.
    Type: Grant
    Filed: August 31, 1987
    Date of Patent: August 15, 1989
    Assignee: Imperial Chemical Industries PLC
    Inventors: David J. Tapolczay, Mark A. Spinney
  • Patent number: 4855323
    Abstract: Leukotriene antagonists, a process for the preparation thereof, and the use thereof for the treatment of diseases ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X have the indicated meanings, a process for the preparation of these compounds, the use thereof as pharmaceuticals, and pharmaceutical products based on these compounds, are described.
    Type: Grant
    Filed: July 22, 1988
    Date of Patent: August 8, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gunther Wess, Wilhelm Bartmann, Gerhard Beck, Hiristo Anagnostopulos
  • Patent number: 4855321
    Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.
    Type: Grant
    Filed: July 18, 1988
    Date of Patent: August 8, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Robert L. Smith, Gerald E. Stokker
  • Patent number: 4851440
    Abstract: Leukotriene antagonists, processes for the preparation thereof, the use thereof for the treatment of diseases, and precursors.Compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and X have the indicated meanings, processes for the preparation of these compounds, the use thereof as pharmaceuticals, and pharmaceutical products based on these compounds are described. In addition, precursors for the preparation of compounds of the formula I are described.
    Type: Grant
    Filed: July 22, 1988
    Date of Patent: July 25, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Beck, Peter Below, Andreas Bergmann
  • Patent number: 4849450
    Abstract: Compounds with arthropodicidal activity having the general formula (I); ##STR1## wherein R.sup.1 is a halo group; or a lower alkyl, lower alkoxy or lower alkylthio group, in each of which the alkyl group may be substituted with one or more halo groups; R.sup.2 is hydrogen or a halo or methyl group; or R.sup.1 and R.sup.2 together form a methylenedioxy, or a difluoro-methylenedioxy group or, R.sup.1 and R.sup.2 together with the carbon atoms to which they are attached, form an aromatic ring; R.sup.3 is hydrogen, CN, or C.ident.CH; Y is --CH-- or --N--; Z is H or F; and X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are the same or different and each is hydrogen or a fluoro, bromo or chloro group; with the proviso that Y is --N-- when Z is H.
    Type: Grant
    Filed: May 1, 1987
    Date of Patent: July 18, 1989
    Assignee: Dunlena Pty. Ltd.
    Inventors: George Holan, Reimund A. Walser, Bryan C. Elmes
  • Patent number: 4845119
    Abstract: A compound of the formula ##STR1## wherein X has the formula --CR.sup.5 .dbd.CR.sup.6 --, --C.tbd.C-- or ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl;wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent of each is hydrogen or alkyl, alkoxy or dialkylamino, provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substitutent;wherein R.sup.5 and R.sup.6, each is hydrogen, halogeno or alkyl;wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 has the formula --Y--Q--R.sup.9 wherein Y is straight- or branched-chain alkylene or alkenylene; wherein Q is --O--, --S--, --SO-- or --SO.sub.2 --; andwherein R.sup.9 is alkyl or up to 6 carbon atoms which contains one or more defined substituents, processes for their manufacture and pharmaceutical compositions containing them.
    Type: Grant
    Filed: February 18, 1986
    Date of Patent: July 4, 1989
    Assignee: Imperial Chemical Industries PLC
    Inventors: Leslie R. Hughes, Howard Tucker
  • Patent number: 4835192
    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 4, 1988
    Date of Patent: May 30, 1989
    Assignee: Pfizer Inc.
    Inventors: Michael R. Johnson, Lawrence Melvin, Jr.
  • Patent number: 4808572
    Abstract: Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: a is an integer of from 1 to 7,R.sup.o represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted at the terminal carbon atom by a free or acylated hydroxy group, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C.sub.1-3 -perfluoroalkyl,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene or alternatively, if R.sup.1 represents a halogenated radical and/or B represents phenylene or ethylene, a single bond or vinylene,B represents a single bond, ethynylene or phenylene,R.sup.3 represents hydroxy, C.sub.
    Type: Grant
    Filed: December 1, 1986
    Date of Patent: February 28, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Andreas Beck, Werner Breitenstein, Andreas von Sprecher, Robert W. Lang, Konrad Oertle
  • Patent number: 4804679
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.1-3 alkyl, andZ is ##STR2## wherein R.sub.7 is hydrogen, R.sub.8 or M,whereinR.sub.8 is a physiologically acceptable and hydrolyzable ester group, andM is a pharmaceutically acceptable cation,the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
    Type: Grant
    Filed: August 6, 1987
    Date of Patent: February 14, 1989
    Assignee: Sandoz Pharm. Corp.
    Inventor: Paul L. Anderson
  • Patent number: 4801609
    Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic peptides useful for treating hypertension are disclosed.
    Type: Grant
    Filed: March 27, 1987
    Date of Patent: January 31, 1989
    Assignee: Schering Corporation
    Inventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 4801611
    Abstract: This invention encompasses compounds and methods for inhibiting lipoxygenase and includes a pharmaceutical composition comprising a pharmaceutical carrier and an effective lipoxygenase inhibiting amount of a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different members of the group consisting of tert-alkyl of 4 to 10 carbon atoms; and R.sub.3 is ##STR2## wherein R.sub.4 is hydrogen or lower alkyl; ##STR3## wherein R.sub.6 and R.sub.7 may be the same or different and are alkyl of 1 to 4 carbon atoms; or ##STR4## and the pharmaceuticlaly acceptable salts thereof. The compounds and pharmaceutical formulations of the present invention are 5-lipoxygenase inhibitors and, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
    Type: Grant
    Filed: May 7, 1987
    Date of Patent: January 31, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Leland J. Chinn, Bipinchandra N. Desai, Richard A. Mueller
  • Patent number: 4791133
    Abstract: This invention relates to leukotriene B.sub.4 antagonists having the structure ##STR1## and the pharmaceutically acceptable addition salts thereof; wherein R.sup.1 is lower alkyl having 1-10 carbon atoms; or lower alkenyl or alkynyl having 2-10 carbon atoms; or lower alkadienyl having 3-10 carbon atoms; or lower alkadiynyl or alkenynyl having 4-10 carbon atoms;wherein R.sup.2 and R.sup.3 are the same or different and represent hydrogen or lower alkyl having 1-6 carbon atoms;wherein X is CH.dbd.CH, S, or O;wherein Y is CH.dbd.CH or C.tbd.C;wherein Z is OR.sup.4 or NR.sup.5 R.sup.6, and wherein R.sup.4 represent H, lower alkyl having 1-6 carbon atoms, or a pharmaceutically acceptable cation, and wherein R.sup.5 and R.sup.6 act independently and represent H or lower alkyl having 1-6 carbon atoms, or R.sup.5 and R.sup.
    Type: Grant
    Filed: June 26, 1987
    Date of Patent: December 13, 1988
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
  • Patent number: 4785004
    Abstract: Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: R.sup.0 represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted by one or more halogen atoms having an atomic number of at most 17,R.sup.2 represents an aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene, a single bond or vinylene,B.sup.1 represents C.sub.1-7 -alkylene or phenylene,B.sup.2 represents a single bond, ethylene or phenylene, andM represents an aromatic radical of the partial formula ##STR2## in which the symbols have the following meanings: R.sup.3 represents hydrogen or C.sub.1-4 -alkyl,X represents NH, O, S or if R.sup.4 represents hydrogen, a single bond,one of the symbols R.sup.4 and R.sup.5 represents hydrogen and the other represents the group --CO--R.sup.6, orR.sup.4 and R.sup.5 together represent the radical --CO--C(R.sup.6).dbd.C(R.sup.7)--or--CO--C(R.sup.7).dbd.C(R.sup.6)--orR.sup.4 R.sup.
    Type: Grant
    Filed: December 15, 1986
    Date of Patent: November 15, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Andreas Von Sprecher, Werner Breitenstein, Andreas Beck, Robert W. Lang, Konrad Oertle
  • Patent number: 4766235
    Abstract: Unsaturated camphor derivatives have an activity in the topical and systemic treatment of acne, psoriasis and other dermatological disorders.
    Type: Grant
    Filed: November 5, 1986
    Date of Patent: August 23, 1988
    Assignee: Societe Anonyme dite: L'Oreal
    Inventors: Gerard Lang, Braham Shroot, Serge Forestier, Alain Lagrange