Q Is Monocyclic Patents (Class 514/604)
  • Patent number: 5455258
    Abstract: Particularly the invention relates to the compounds of formula I ##STR1## (a) wherein Ar is carbocyclic or heterocyclic aryl;R is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, amino, mono- or di-lower alkylamino)-lower alkyl, acylamino-lower alkyl, (N-lower alkyl-piperazino or N-aryl-lower alkylpiperazino)-lower alkyl, or (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl or N-lower alkylpiperidyl)-lower alkyl;R.sub.1 is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.
    Type: Grant
    Filed: January 6, 1993
    Date of Patent: October 3, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence J. MacPherson, David T. Parker
  • Patent number: 5455273
    Abstract: The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: October 3, 1995
    Assignee: Karl Thomae GmbH
    Inventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
  • Patent number: 5446065
    Abstract: Compounds of the formula I ##STR1## in which R.sub.1 signifies an aryl, aralkyl or an aralkenyl group, the aryl radical of which can, in each case, be substituted one or more times by halogen, cyano, alkyl, trifluoromethyl, alkoxy, alkylthio, trifluoromethoxy, hydroxyl or carboxyl, m a whole number from 1 to 3, n a whole number from 1 to 5, R.sub.2 hydrogen, an alkyl, aralkyl or acyl group, Q a bond or an oxygen atom, R.sub.3 hydrogen or a lower alkyl radical which is possibly terminally substituted by carboxyl or by a hydroxyl group and R.sub.4 hydrogen, a lower alkyl group with 1-4 C-atoms, which is possibly terminally substituted by carboxyl or hydroxyl, a possibly substituted phenyl, heteroaryl, cycloalkyl or acyl group or a group ##STR2## in which R.sub.
    Type: Grant
    Filed: June 21, 1993
    Date of Patent: August 29, 1995
    Assignee: Boehringer Mannheim GmbH
    Inventors: Ernst-Christian Witte, Hansjorg Beckh, Karlheinz Stegmeier, Liesel Doerge
  • Patent number: 5434186
    Abstract: Compounds of the formula ##STR1## wherein X is O or CH.sub.2 ; Y is O, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, or --OCH.sub.2 C.sub.6 H.sub.4 --;Z is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; and A is B or --O--B, wherein B is a mono-, di- or tricyclic aromatic or heteroaromatic moiety substituted by the group --COR.sup.2, --(O).sub.t --(W).sub.s --COR.sup.2 or --(CH.dbd.CH).sub.p COR.sup.2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl, --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, provided that no more than one of said substituents is --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, and wherein E is COR.sup.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: July 18, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Ferdinand K. Lee, Keith A. Yagaloff
  • Patent number: 5418254
    Abstract: A class of 2,3-substituted cyclopenta-2,4-dienyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, lower alkyl, lower hydroxyalkyl, halo, lower haloalkyl, lower alkoxycarbonyl and carboxyl; and wherein each of R.sup.3 through R.sup.12 is independently selected from hydrido, halo, lower alkyl, lower alkylthio, cyano, hydroxyl, mercapto, lower haloalkyl, lower haloalkoxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl, lower alkylsulfonyl, lower haloalkylsulfonyl and sulfamyl; provided R.sup.5 and R.sup.10 are not both hydrido or methoxy; or a pharmaceutically suitable salt or prodrug thereof.
    Type: Grant
    Filed: May 4, 1994
    Date of Patent: May 23, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Horng-Chih Huang, David R. Reitz
  • Patent number: 5416117
    Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: February 28, 1994
    Date of Patent: May 16, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
  • Patent number: 5409956
    Abstract: The present invention relates to indan derivatives represented by the formula (1) or pharmaceutically acceptable salts thereof: ##STR1## [wherein R.sup.1 represents C1 to C12 alkyl, benzyl, styryl, naphthyl, optionally substituted phenyl or optionally substituted thienyl; R.sup.2 represents carboxyl, C1 to C4 alkoxycarbonyl, ##STR2## Y represents --(CH.sub.2).sub.p -- (wherein p represents an integer of 0 to 5), --CO--(CH.sub.2).sub.q .about., --CH(OH)--(CH.sub.2).sub.q .about., (wherein q represents an integer of 1 to 4, and the symbol .about. represents a linkage to R.sup.2), oxymethylene or ethylene; and n represents an integer of 1 to 4]. The compounds according to the present invention potently antagonize the action of thromboxane A.sub.2, and therefore useful for the treatment and prevention of diseases caused by thromboxane A.sub.2 such as angiosis, vasospasm, asthma and the like.
    Type: Grant
    Filed: August 30, 1993
    Date of Patent: April 25, 1995
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Yoshida, Yoshiaki Yamaji, Tadashi Kurimoto, Ryuichi Sato, Motoki Torizuka
  • Patent number: 5403853
    Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl;A is a substituted phenyl group containing one or two substituents selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfone, perfluoroalkylsulfone, arylsulfone, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: April 4, 1995
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane
  • Patent number: 5393790
    Abstract: A class of substituted spiro compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein n is a number selected from 0, 1 and 2; wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein R.sup.8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: February 10, 1994
    Date of Patent: February 28, 1995
    Assignee: G.D. Searle & Co.
    Inventors: David B. Reitz, Robert E. Manning, Horng-Chi Huang, Jinglin Li
  • Patent number: 5387608
    Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.
    Type: Grant
    Filed: August 17, 1993
    Date of Patent: February 7, 1995
    Assignee: Allergan, Inc.
    Inventor: Steven W. Andrews
  • Patent number: 5328909
    Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: July 12, 1994
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
  • Patent number: 5318770
    Abstract: Methods and compositions are disclosed for enhancing .sup.19 F magnetic resonance imaging which utilize trifluorometyl derivatives of iodinated X-ray contrast media. Typical magnetic resonance contrast media within the scope of the present invention include bis(trifluoromethyl)benzene derivatives, tris(trifluoromethyl)benzene derivatives, tetrakis(trifluoromethyl)benzene derivatives, and other related trifluoromethylated benzene derivatives.
    Type: Grant
    Filed: October 25, 1991
    Date of Patent: June 7, 1994
    Assignee: Mallinckrodt Medical, Inc.
    Inventors: David H. White, Steven R. Woulfe, Youlin Lin, Mills T. Kneller
  • Patent number: 5292755
    Abstract: Benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is equal to R(6)--S(O).sub.n -- or R(7)R(8)N--O.sub.2 S--and the other substituent R(1) or R(2) is in each case equal to H, F, Cl, Br, I, alkyl, alkoxy or phenoxy, R(6)--S(O).sub.n or R(7)R(8)N--and R(6) is equal to alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl,R(7) and R(8) are equal to alkyl or phenylalkyl or phenyl,and in which R(7) and R(8) may also together be a C.sub.4 --C.sub.7 chain, and in which R(7) and R(8), together with the nitrogen atom to which they are bonded, may be a dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system,and where R(3), R(4) and R(5) are equal to hydrogen or alkyl, or R(3) and R(4) are together an alkylene chain or R(4) and R(4) are together an alkylene chain,and where n is equal to zero, 1 or 2and their pharmaceutically tolerable salts are outstanding antiarrhythmics.
    Type: Grant
    Filed: January 31, 1992
    Date of Patent: March 8, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich C. Englert, Hans-Jochen Lang, Wolfgang Linz, Bernward Scholkens, Wolfgang Scholz
  • Patent number: 5280043
    Abstract: Phenylalkanoic acids containing a sulphonamido group, and their use in a method of treatment of thromboxane-A.sub.2 mediated diseases are disclosed. A compound of the invention is 4-[4-(phenyl-sulphonamido)phenyl]butyric acid.
    Type: Grant
    Filed: April 2, 1992
    Date of Patent: January 18, 1994
    Assignee: Smith Kline & French Laboratories Ltd.
    Inventors: David G. Cooper, Andrew D. Gribble
  • Patent number: 5266597
    Abstract: A method of controlling fungus is provided which comprises contacting said fungus with a fungicidally effective amount of a compound having the following structure: ##STR1## wherein R is a halogen atom, andR.sup.1 is selected from the group consisting of substituted or unsubstituted, straight or branched alkyl having from about 1 to 6 carbon atoms,alkoxy having from about 1 to 6 carbon atoms,halo, provided that when any R.sup.1 is chloro, n is 2 and at least one R.sup.1 is meta-chloro,substituted or unsubstituted sulfamoyl, andsubstituted or unsubstituted carbamoyl,where n is 1 or 2.
    Type: Grant
    Filed: June 16, 1992
    Date of Patent: November 30, 1993
    Assignee: Eastman Kodak Company
    Inventors: Thomas R. Welter, John J. Delany, III
  • Patent number: 5266589
    Abstract: The invention relates to a method of improving the growth and the feed efficiency and of increasing the muscle/fat ratio of agricultural domestic animals, in particular bovine animals and sheep, by administering to the animals a composition which comprises as an active substance a compound of the general formula ##STR1## wherein: R.sub.1 is a phenylalkyl group the alkyl group of which comprises 1-3 carbon atoms and the phenyl group of which may be substituted with one or more substituents selected from the group consisting of hydroxy, methoxy, fluoro and methylsulphonylamino, or whereinR.sub.1 is a thienyl alkyl group or a tetrahydrofurylalkyl group the alkyl group of which comprises 1-3 carbon atoms; or whereinR.sub.1 is an optionally branched alkyl group having 1-8 carbon atoms which optionally is substituted with a C.sub.1 -C.sub.4 alkoxy group, a hydroxy group, a C.sub.1 -C.sub.4 alkoxycarbonyl group or a carboxy group; and whereinR.sub.2 and R.sub.
    Type: Grant
    Filed: November 21, 1991
    Date of Patent: November 30, 1993
    Assignee: Duphar International Research B.V.
    Inventors: Johan K. Van Dasler, Jan Van Dijk
  • Patent number: 5264458
    Abstract: Iso- and heterocyclic phenylsulphonamides can be prepared by reaction of corresponding iso- and heterocyclic amines with phenylsulphonic acid derivatives. The iso- and heterocyclic phenylsulphonamides have thrombocyte aggregation-inhibiting and thromboxane A.sub.2 antagonist action and can be used in medicaments.
    Type: Grant
    Filed: July 14, 1992
    Date of Patent: November 23, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Niewohner, Franz-Peter Hoever, Elisabeth Perzborn, Volker-Bernd Fiedler, Peter Norman, Hilary P. Francis, Marie G. McKenniff
  • Patent number: 5246965
    Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(.dbd.NH)--NHR group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which:R is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid;R.sub.1 is a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical and a cycloaliphatic hydrocarbon radical;X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); andX.sub.
    Type: Grant
    Filed: September 17, 1992
    Date of Patent: September 21, 1993
    Assignee: Ciba-Geigy
    Inventor: Alan J. Main
  • Patent number: 5238959
    Abstract: The present invention provides 3-(4-substitutedphenoxy)-3-phenyl propanamines capable of inhibiting the uptake of serotonin. These compounds are useful for treating many pharmacological disorders, including depression and obesity. These compounds can also be used to reduce the desire to smoke and consume alcohol.
    Type: Grant
    Filed: April 20, 1992
    Date of Patent: August 24, 1993
    Assignee: Eli Lilly and Company
    Inventors: David W. Robertson, David T. Wong
  • Patent number: 5168101
    Abstract: A sulfonamide derivative of the general formula:Tx--R.sup.1 (I)wherein, R.sup.1 represents(i) COOR.sup.11,(ii) CH.sub.2 OR.sup.12 or(iii) CONR.sup.13 R.sup.14,Tx--represents ##STR1## X.sub.b represents(i) bond,(ii) alkylene group of from 1 to 4 carbon atoms or(iii) alkenylene group of from 2 to 4 carbon atoms (with the proviso that --CH.dbd.CHCH.sub.2 -- and --CH.sub.2 CH.dbd.CHCH.sub.2 -- are excluded),R.sup.2b represents(i) hydrogen atom,(ii) halogen atom or(iii) alkyl group of from 1 to 4 carbon atom(s), posses an antagonistic activity on TXA.sub.2.
    Type: Grant
    Filed: October 13, 1988
    Date of Patent: December 1, 1992
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Yoshinobu Arai, Nobuyuki Hamanaka, Tohru Miyazaki
  • Patent number: 5155136
    Abstract: A method of controlling fungus is provided which comprises contacting said fungus with a fungicidally effective amount of a compound having the following structure: ##STR1## wherein R is a halogen ateom, andR.sup.1 is selected from the group consisting of substituted or unsubstituted, straight or branched alkyl having from about 1 to 6 carbon atoms, alkoxy having from about 1 to 6 carbon atoms, halo, provided that when any R.sup.1 is chloro, n is 2 and at least one R.sup.1 is meta-chloro, substituted or unsubstituted sulfamoyl, and substituted or unsubstituted carbamoyl,where n is 1 or 2.
    Type: Grant
    Filed: November 23, 1990
    Date of Patent: October 13, 1992
    Assignee: Eastman Kodak Company
    Inventors: Thomas R. Welter, John J. Delany, III
  • Patent number: 5153227
    Abstract: The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.
    Type: Grant
    Filed: February 6, 1989
    Date of Patent: October 6, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston
  • Patent number: 5143937
    Abstract: Compounds of the formula I ##STR1## where R.sup.1 to R.sup.5 have the meaning indicated, a process for their preparation and their use as medicaments are described. They are effective lipid-lowering agents with antioxidative properties from the benzenesulfonamide series. They do not have hypotensive and diuretic properties.
    Type: Grant
    Filed: February 16, 1990
    Date of Patent: September 1, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Jochen Lang, Ernold Granzer, Bela Kerekjarto
  • Patent number: 5124348
    Abstract: A compound of Formula (I):R.sup.1 (CA.dbd.CA.sup.1).sub.x --C(.dbd.X)NR.sup.2 R.sup.3 (I)where R.sup.1 is alkyl optionally substituted by a group selected from alkoxy, alkenyl, alkynyl, alkenyloxy, alkynyloxy, aryl, aryloxy, arylalkoxy and cycloalkyl fused to an aryl ring; x=1 or 2; X=O or S; each A and A.sup.1 is independently hydrogen, alkyl or haloalkyl; R.sup.2 is alkyl, alkenyl or cycloalkyl any of which may be substituted by halo, alkenyl, alkyl, cycloalkyl, alkynyl, dioxalanylalkyl or alkoxy; and R.sup.3 is selected from groups (A) to (D):(A) --Y.dbd.X.sup.1 --(R.sup.4).sub.a where X.sup.1 is O or S, Y is phosphorus or carbon, R.sup.4 is hydrogen, alkyl, alkoxy, acyl or CO.sub.2 R.sup.5 where R.sup.5 is alkyl or aryl, and a is 1 or 2(B) --S(R.sup.6)(O).sub.b where R.sup.6 is alkyl, aryl, aryloxy, alkoxy, thioalkoxy, thioaryl, alkythio, alkoxythio or arylthio and b is 0, 1 or 2(C) --S(O).sub.c NR.sup.7 R.sup.8 where c is 0, 1 or 2, R.sup.7 is --COR.sup.9 or --CO.sub.2 R.sup.9 where R.sup.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: June 23, 1992
    Assignee: Burroughs Wellcome Co.
    Inventors: Malcolm H. Black, Robert J. Blade, Robert J. Peek
  • Patent number: 5095026
    Abstract: Prodrugs are prepared of the carbonic anhydrase inhibitors 2-benzothiazolesulfonamide, hydroxymethazolamide, and dichlorphenamide. The prodrugs link a water soluble compound to the pharmacologically active carbonic anhydrase inhibitor through an enzymatically or hydrolytically degradable bond.
    Type: Grant
    Filed: September 22, 1989
    Date of Patent: March 10, 1992
    Assignee: University of Iowa Research Foundation
    Inventors: Ronald D. Schoenwald, Charles F. Barfknecht
  • Patent number: 5095038
    Abstract: This invention comprises novel carbocyclic compounds of formula I (wherein A, Z, R.sup.11 and R.sup.12 are defined in the specification) derived from acylsulfonamide derivatives of .alpha.-carbocyclyltoluic acids wherein said compounds of formula I antagonize the actions of one or more of the arachidonic acid metabolites known as leukotrienes. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.
    Type: Grant
    Filed: April 12, 1989
    Date of Patent: March 10, 1992
    Assignee: ICI Americas Inc.
    Inventors: Frederick J. Brown, Thomas P. Maduskuie, Jr., Victor G. Matassa, Ying K. Yee
  • Patent number: 5086067
    Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CH.dbd.CH-- or --CH.dbd.N--; wherein R.sub.1 is alkyl, alkenyl or alkynyl of about 1 to 20 carbon atoms; wherein R is --CO.sub.2 R.sup.2, tetrazole, methylsulfonamide or benzenesulfonamide, wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbon atoms or a pharmaceutically acceptable cation and R.sup.3 is hydroxyl or halogen, having utility as LTB.sub.4 synthesis inhibitors.
    Type: Grant
    Filed: December 18, 1989
    Date of Patent: February 4, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
  • Patent number: 5086073
    Abstract: The invention concerns compounds having formula: ##STR1## or a salt thereof, wherein E represents hydrogen, lower alkyl or a group Ar.sup.1 --A.sup.1 ; Ar and Ar.sup.1 are the same or different aryl groups (including heteroaryl) which are optionally substituted, e.g. by one or more substituents commonly used in pharmaceutical chemistry; A and A.sup.1 are the same or different alkylene groups having one or two carbon atoms linking Ar or Ar.sup.1 to N and optionally substituted by lower alkyl and/or optionally substituted aryl, B is an alkylene group of 3 or 4 carbon atoms, which may be substituted by lower alkyl; D.sup.1 represents halogen, CH.sub.3, CR.sup.1 R.sup.2 NH.sub.2, SO.sub.3 H or SO.sub.2 NR.sup.6 R.sup.7 where R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl and R.sup.6 and R.sup.7 are each hydrogen, lower alkyl or aralkyl of 7 to 12 carbon atoms or R.sup.6 and R.sup.
    Type: Grant
    Filed: May 30, 1990
    Date of Patent: February 4, 1992
    Assignee: John Wyeth & Brother Limited
    Inventors: John F. White, Michael C. Warren, Christine Ennis
  • Patent number: 5070099
    Abstract: Arylthioalkylphenylcarboxylic acids 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 where R is hydrogen, alkali metal, or lower alkyl, or X is 5-tetrazolyl or ##STR2## wherein R.sup.1 is lower alkyl or aryl, p is 1 to 5, and m is 1 to 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasospastic diseases.
    Type: Grant
    Filed: February 4, 1991
    Date of Patent: December 3, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Steven E. Hall, Philip D. Stein
  • Patent number: 5053430
    Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.
    Type: Grant
    Filed: September 22, 1989
    Date of Patent: October 1, 1991
    Assignee: Boehringer Ingelheim KG
    Inventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
  • Patent number: 5026690
    Abstract: The present invention relates to the use of sulphonamide derivatives for the treatment of diseases caused by viruses, especially caused by enclosed viruses such as, e.g., herpes simplex, as well as to an antiviral agent having a content of these sulphonamide derivatives as active substance, optionally together with pharmaceutically acceptable carriers and/or auxiliaries.
    Type: Grant
    Filed: December 28, 1988
    Date of Patent: June 25, 1991
    Assignee: Chemische Fabrik Stockhausen GmbH
    Inventors: Joachim Kresken, Bernd Komp, Dolf Stockhausen
  • Patent number: 5021448
    Abstract: A method of reducing serum uric acid and/or increasing renal clearance of uric acid in a mammal in need thereof comprising administering to such mammal a uricosuric effective amount of a thromboxane synthetase inhibitor, a thromboxane receptor antagonist, or both in a combined uricosuric effective amount is disclosed. Compositions having one or more of the foregoing in combination with one or more known uricosurics are also set forth.
    Type: Grant
    Filed: February 22, 1990
    Date of Patent: June 4, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Anthony J. Piraino, Steven D. Saris
  • Patent number: 5010104
    Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: April 23, 1991
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 5006542
    Abstract: Arylthioalkylphenylcarboxylic acids 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 where R is hydrogen, alkali metal, or lower alkyl, or X is 5-tetrazolyl or ##STR2## where R.sup.1 is lower alkyl or aryl, p is 1 to 5, and m is 1 to 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasopastic diseases.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: April 9, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Steven E. Hall, Philip D. Stein
  • Patent number: 5006523
    Abstract: Novel compounds of the formula ##STR1## and tautomers thereof are disclosed. These compounds possess potassium channel blocking activity and, as such, are useful as antiarrhythmic agents.
    Type: Grant
    Filed: October 26, 1989
    Date of Patent: April 9, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 5002972
    Abstract: Pharmaceutical compounds and compositions for injectable use in the treatment of thromboxane A.sub.2 mediating diseases, comprising a pharmaceutical carrier and a pharmacologically effective amount of a compound of the formula: ##STR1## wherein R.sup.1 is carboxyl or 5-tetrazolyl; R.sup.2 is hydrogen, methyl, hydroxy, chloro, or bromo; or a pharmaceutically acceptable ester or salt thereof, together with one or more non-toxic pharmaceutically acceptable carriers; and methods for treating thromboxane A.sub.2 mediating diseases.
    Type: Grant
    Filed: February 7, 1990
    Date of Patent: March 26, 1991
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masayuki Narisada, Mitsuaki Ohtani, Fumihiko Watanabe, Takaharu Matsuura
  • Patent number: 4999345
    Abstract: Sulfonamide derivatives of the formula I ##STR1## where R.sup.1 is a C.sub.1 -C.sub.4 -alkyl or phenyl group which may be substituted by halogen, trifluoromethyl or C.sub.1 -C.sub.4 -alkyl, R.sup.2 is hydrogen or C.sub.1 -C.sub.4 -alkyl, A is a group CHOR.sup.3 C.dbd.O, C.dbd.S or C.dbd.N--OR.sup.4, R.sup.3 is hydrogen, C.sub.1 -C.sub.4 -alkyl phenyl, benzyl or C.sub.1 -C.sub.4 -acyl, R.sup.4 is hydrogen or methyl, B may be methylene or ethylene in the m or p position or, of A is not carbonyl, may be methyleneoxy, the oxygen atom being bonded to the aromatic, and E is a carboxyl, phosphonic acid or sulfo radical, their physiologically acceptable salts, esters with C.sub.1 -C.sub.4 -alcohols or amides or the tetrazol-5-yl radical, their preparation and their use as drugs.
    Type: Grant
    Filed: May 26, 1989
    Date of Patent: March 12, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernhard Schmied, Hand D. Lehmann, Verena Baldinger, Klaus Ruebsamen
  • Patent number: 4980366
    Abstract: Novel 4'-hydroxybenzylamine derivatives of the formula ##STR1## pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, succh as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.
    Type: Grant
    Filed: March 16, 1989
    Date of Patent: December 25, 1990
    Assignee: Warner-Lambert Co.
    Inventors: Graham Johnson, Michael F. Rafferty
  • Patent number: 4965279
    Abstract: Novel cyclopropyl aza prostaglandin analogs are disclosed having the formula ##STR1## wherein A can be carbonyl, sulfonyl or a single bond. These compounds are useful, for example, as thromboxane antagonists.
    Type: Grant
    Filed: November 18, 1988
    Date of Patent: October 23, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Raj N. Misra, David M. Floyd, Steven E. Hall
  • Patent number: 4954513
    Abstract: This invention relates to alkanoic acid compounds having phenyl and heteroarylthio substituents which are useful as leukotriene antagonists, pharmaceutical compositions containing such compounds, and methods of treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: September 4, 1990
    Assignee: SmithKline Beecham Corporation
    Inventors: John G. Gleason, Ralph F. Hall, Joanne Smallheer
  • Patent number: 4948810
    Abstract: Novel phenoxyacetic acid derivative of the formula: ##STR1## wherein R is a substituted or unsubstituted phenyl group, naphthyl group or a sulfur-containing 5-membered hetero-monocyclic group, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group or phenyl group, R.sup.5 is hydrogen atom or a lower alkyl group, R.sup.6 is carboxyl group, a protected carboxyl group, hydroxy group or a di(lower alkyl)-amino group, Ring A is a substituted or unsubstituted phenylene group, m is 0 or 1 and n is an integer 0 to 5, provided that, when m is 0,(1) at least either one of R.sup.1 to R.sup.4 is or/are a phenyl-lower alkyl group or phenyl group,(2) at least either one of R.sup.1 to R.sup.4 is or/are a lower alkyl group, and R.sup.6 is hydroxy group, or(3) all of R.sup.1 to R.sup.4 are hydrogen atom, and Ring A is a substituted phenylene group,or a pharmaceutically acceptable salt thereof are disclosed.
    Type: Grant
    Filed: February 6, 1989
    Date of Patent: August 14, 1990
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Takeo Iwakuma, Takayuki Kawaguchi, Toyoharu Yamashita, Yasuhiko Sasaki, Tamotu Shimazaki
  • Patent number: 4918106
    Abstract: Disclosed herein are N-(2-chloro-4-nitrophenyl)-3-trifluoromethyl-benzenesulfonamide derivatives represented by the following general formula (I): ##STR1## wherein X and Y individually mean a hydrogen or chlorine atom and agricultural fungicides containing said derivatives.
    Type: Grant
    Filed: February 9, 1988
    Date of Patent: April 17, 1990
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Takeo Yoshimoto, Mitsumasa Umemoto, Keiichi Igarashi, Yutaka Kubota, Hideo Yamazaki, Yuji Enomoto, Hirohisa Yanagita
  • Patent number: 4871756
    Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4, E.sub.4 and the slow reacting substance of anaphylaxis.As such, these compounds will be useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Grant
    Filed: February 17, 1987
    Date of Patent: October 3, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: John Gillard, Joshua Rokach, Patrice C. Belanger
  • Patent number: 4870107
    Abstract: Disclosed herein are N-(2-chloro-4-nitrophenyl)-benzenesulfonamide derivatives represented by the following general formula (I): ##STR1## wherein X and Y individually mean a hydrogen or chlorine atom and Z denotes a chlorine atom or trifluoromethyl group, and agricultural fungicides containing said derivatives.
    Type: Grant
    Filed: October 7, 1987
    Date of Patent: September 26, 1989
    Assignee: Mitsui Toatsu Chemicals, Incorporated
    Inventors: Takeo Yoshimoto, Mitsumasa Umemoto, Keiichi Igarashi, Yutaka Kubota, Hideo Yamazaki, Yuji Enomoto, Hirohisa Yanagita
  • Patent number: 4855289
    Abstract: The invention concerns the use of a compound with diuretic properties and of a magnesium supplementation in the form of magnesium monoaspartate hydrochloride, magnesium oxide, magnesium hydroxide or magnesium carbonate, and optionally of a potassium supplementation, and pharmaceutical preparations comprising a compound with diuretic properties and a magnesium supplementation in the form of magnesium monoasparate hydrochloride, magnesium oxide, magnesium hydroxide, or magnesium carbonate and optionally a potassium supplementation.
    Type: Grant
    Filed: July 30, 1987
    Date of Patent: August 8, 1989
    Inventors: Per O. Wester, Thomas R. Dyckner
  • Patent number: 4851445
    Abstract: Disclosed herein are N-(2-chloro-4-nitrophenyl)benzenesulfonamide derivatives represented by the following general formula (I): ##STR1## wherein X and Y individually mean a hydrogen or chlorine atom and Z denotes a chlorine atom or trifluoromethyl group, and agricultural fungicides containing said derivatives.
    Type: Grant
    Filed: June 28, 1988
    Date of Patent: July 25, 1989
    Assignee: Mitsui Toatsu Chemicals, Incorporated
    Inventors: Takeo Yoshimoto, Mitsumasa Umemoto, Keiichi Igarashi, Yutaka Kubota, Hideo Yamazaki, Yuji Enomoto, Hirohisa Yanagita
  • Patent number: 4849563
    Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 s an alkyl of 1-6 carbon atoms, benzyl, phenyl, or phenyl substituted by halogen, alkoxy of 1 to 4 carbon atoms, alkyl of 1 to 4 carbon atoms, amino, or carbonyl substituents, or --RN(R').sub.2 wherein R and R' are each independently an alkyl of 1 to 4 carbon atoms; R.sub.2 is an aromatic substituent selected from the group consisting of phenyl, benzyl, and naphthyl, and A is an aromatic substitution selected from the group consisting of hydrogen, alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, halogen, --NO.sub.2, --NH.sub.2, --COOH, and --NHCOCH.sub.3. The compounds have been found to be alkylating agents having antineoplastic activity for use in inhibiting the growth of tumors.
    Type: Grant
    Filed: December 28, 1987
    Date of Patent: July 18, 1989
    Assignee: Yale University
    Inventors: Alan C. Sartorelli, Krishnamurthy Shyam, Robert T. Hrubiec
  • Patent number: 4843062
    Abstract: Disclosed herein are N-acyl-N-napthoylglycines and methods of their preparation. The N-acyl-N-napthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
    Type: Grant
    Filed: December 23, 1987
    Date of Patent: June 27, 1989
    Assignee: American Home Products Corporation
    Inventors: Kazimir Sestanj, Jay E. Wrobel, Joseph M. Kelly
  • Patent number: 4752615
    Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole, thiophanate and/or cyclic imide fungicides.
    Type: Grant
    Filed: November 13, 1986
    Date of Patent: June 21, 1988
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
  • Patent number: 4737522
    Abstract: Fungicidally active novel N-sulphenylated benzene sulphonic acid amides of the formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 independently of one another represent hydrogen, halogen, nitro, alkyl or halogenoalkyl andR.sup.4 represents alkyl, alkenyl, halogenoalkinyl, cycloalkyl which is optionally substituted by alkyl, alkoxyalkyl or alkylthioalkyl, excluding the compounds in which (a) R.sup.4 represents methyl and (i) R.sup.1, R.sup.2 and R.sup.3 represents hydrogen, or (ii) R.sup.1 represents chlorine or nitro, R.sup.2 represents chlorine and R.sup.3 represents hydrogen, or (iii) R.sup.1 represents nitro and R.sup.2 and R.sup.3 represent hydrogen, or (iv) R.sup.1 and R.sup.3 represent chlorine and R.sup.2 represents hdyrogen and (b) R.sup.4 represents n-butyl, R.sup.1 and R.sup.3 represent hydrogen and R.sup.2 represents chlorine.
    Type: Grant
    Filed: August 21, 1986
    Date of Patent: April 12, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Engelbert Kuhle, Hans-Georg Schmitt, Wilhelm Brandes, Paul Reinecke