Chalcogen Bonded Directly At The 2-position Of The Oxazole Ring Patents (Class 548/221)
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Patent number: 5223517Abstract: Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or amidation, or by reaction of heterocyclically substituted hydrazines with cycloalkanones or by subsequent introduction of the heterocyclic group into appropriate indole derivatives. The heterocyclically substituted cycloalkano[b]-indolesulphonamides can be employed for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, asthma, allergies and for the prophylaxis of myocardial infarcts.Type: GrantFiled: August 23, 1991Date of Patent: June 29, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich E. Muller, Ulrich Niewohner, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
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Patent number: 5223616Abstract: A heterocyclic compound which is useful for dyeing or printing hydrophobic fiber materials and which has the following formula (I), ##STR1##wherein A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are each hydrogen, halogen, alkyl, alkoxy or alkenyl, X.sub.1 is --O-- or the like, R.sub.1 is a methylene or the like, X.sub.2 is a direct linkage or a divalent group of --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## in which R.sub.3 is a hydrogen atom or a C.sub.1-4 alkyl group, ##STR3## in which R.sub.3 is as defined above, T and u are each independently hydrogen or a C.sub.1-4 alkyl, l is O or an integer of 1 to 3, Q is an unsubstituted or substituted 5-, 6- or 7-membered saturated or unsaturated heterocyclic residue, Y is hydrogen, C.sub.1-4 alkyl, a C.sub.1-4 alkoxy group or the like.Type: GrantFiled: November 4, 1991Date of Patent: June 29, 1993Assignee: Sumitomo Chemical Company, Ltd.Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
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Patent number: 5223614Abstract: Compounds of formula ##STR1## wherein the substituents are defined hereinbelow, useful in the treatment of bronchospasm are described.Type: GrantFiled: October 25, 1990Date of Patent: June 29, 1993Assignee: Boehringer Ingelheim GmbHInventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Gojko Mualcevic, Werner Traunecker
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Patent number: 5214169Abstract: The present invention as directed to a new class of N-(2,3-epoxycyclopentyl) carbamate derivatives as described by Formula V below, that are useful as chemical intermediates in the production of a new class of anti-hypertensives: ##STR1##Type: GrantFiled: April 30, 1992Date of Patent: May 25, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Theophilus F. Leapheart
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Patent number: 5213605Abstract: N-aryltetrahydrophthalimide compounds of the general formula I ##STR1## where n, R.sup.1, Y, R.sup.2 and R.sup.3 have the meanings stated in the claims and description, and a method for controlling undesirable plant growth.Type: GrantFiled: September 17, 1991Date of Patent: May 25, 1993Assignee: BASF AktiengesellschaftInventors: Lothar Rueb, Karl Eicken, Peter Plath, Barbara Schwalge, Karl-Otto Westphalen, Bruno Wuerzer, Norbert Meyer
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Patent number: 5196434Abstract: Compound of general formula (I): ##STR1## where R.sub.1, R.sub.2, R.sub.3, n, X and A are defined in the description.Medicinal products.Type: GrantFiled: September 26, 1991Date of Patent: March 23, 1993Assignee: Adir et CompagnieInventors: Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
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Patent number: 5182278Abstract: Compounds of general formula (I): ##STR1## in which: R.sub.1 denotes a hydrogen atom or a lower alkyl optionally substituted with a hydroxyl group,R.sub.2 and R.sub.3 :a- identical or different, denote a hydrogen atom, a lower alkyl, a lower alkenyl, a substituted or unsubstituted aryl, a substituted or unsubstituted (lower alkyl)aryl,b- are such that they form, with the nitrogen which carries them, a saturated or unsaturated, mono- or bicyclic heterocyclic system containing at most 3 hetero atoms per ring, substituted or unsubstituted, with the exception of 1-arylpiperazine systems,X denotes a hydrogen atom,Y denotes a hydrogen atom or a hydroxyl,or alternatively X and Y denote an oxygen atom, provided thatR.sub.1 is then other than a methyl group,Z denotes a hydrogen atom or forms a .pi.Type: GrantFiled: July 29, 1991Date of Patent: January 26, 1993Assignee: Adir et CompagnieInventors: Daniel Lesieur, Charles Lespagnol, Jacqueline Bonnet
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Patent number: 5180419Abstract: There are provided o-carboxy-(5-oxo-2-imidazolin-2-yl)benzo-(5-membered)-heterocyclic compounds and derivatives thereof and a method for the use therewith to control monocotyledenous and dicotyledenous plant species.Type: GrantFiled: November 22, 1991Date of Patent: January 19, 1993Assignee: American Cyanamid CompanyInventors: David M. Gange, Michael A. Guaciaro, Robert F. Doehner, Jr.
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Patent number: 5180825Abstract: Disclosed in a mitomycin derivative represented by the formula (I): ##STR1## wherein W is a heterocyclic group.Type: GrantFiled: November 13, 1991Date of Patent: January 19, 1993Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hitoshi Arai, Motomichi Kono, Masaji Kasai, Katsushige Gomi, Tadashi Ashizawa
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Patent number: 5180417Abstract: Disclosed herein are derivatives of 4-((aryloxy)phenoxy)fluoroalkanoic acid and their use as active herbicides for the pre- and postemergent control of grassy weeds, especially in the presence of broadleaf crops.Type: GrantFiled: April 12, 1991Date of Patent: January 19, 1993Assignee: DowElancoInventor: James A. Turner
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Patent number: 5156667Abstract: Derivatives of 4-((aryloxy)phenoxy)alkenols, their preparation and use as active herbicides for the postemergent control of grassy weeds and especially the control of said weeds in the presence of corn plants are disclosed.Type: GrantFiled: April 12, 1991Date of Patent: October 20, 1992Assignee: DowElancoInventors: James A. Turner, Paul S. Zorner, Wendy S. Jacks
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Patent number: 5152929Abstract: Compounds of the formula I ##STR1## in which X is --S--, --O-- or --NH--, R is H or a monovalent substituent, n is 0 or 1 and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl, alkyl which is substituted by OH, halogen, COOH or alkoxy, unsubstituted or substituted aryl or aralkyl, or carboxyl, or R.sup.1 and R.sup.2 or R.sup.1 and R.sup.3 together are alkylene or R.sup.1 and R.sup.2 are a direct bond, at least two of the groups R.sup.1, R.sup.2, R.sup.3 and R.sup.4 being carboxyl or carboxyalkyl groups, and base addition salts thereof are effective corrosion inhibitors. The preparation of these novel polycarboxylic acids can be effected by various processes.Type: GrantFiled: October 10, 1990Date of Patent: October 6, 1992Assignee: Ciba-Geigy CorporationInventors: Robert L. Bentley, Michael P. Savage, Kenneth W. Shelton
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Patent number: 5147883Abstract: Compounds of general formula (I): ##STR1## in which: R.sub.1 represents a hydrogen atom or a lower alkyl group,A represents a hydrogen atom, and in this case B represents a group CO-G, G being:either a heteroaryl group selected from furan, indole, pyrrole, pyridine, quinoline, isoquinoline and benzofuran, optionally substituted with one or more lower alkyl or lower alkoxy groups or a halogen atoms,or a linear or branched lower alkyl group substituted with a carboxyl group,or a linear or branched lower alkenyl group substituted with a carboxyl group,or a phenyl or naphthyl group substituted with a carboxyl group,or alternatively A forms with B a group CO(CH.sub.2).sub.n CH(CH.sub.Type: GrantFiled: May 31, 1991Date of Patent: September 15, 1992Assignee: Adir et CompagnieInventors: Hocine Aichaioui, Daniel Lesieur, Charles Lespagnol, Michelle Devissaguet, Beatrice Guardiola
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Patent number: 5147878Abstract: Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S, --SO--, or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen such as chlorine, bromine or iodine, A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical in which the hydroxy is optionally substituted by a lower alkyl radical, Ar represents a group ##STR2## R.sub.4 denotes hydrogen or an alkyl radical and Cy represents a cyclic group.Type: GrantFiled: April 19, 1990Date of Patent: September 15, 1992Assignee: SanofiInventors: Jean Gubin, Pierre Chatelain
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Patent number: 5136043Abstract: A process for the preparation of aromatic sulfonyl chlorides of the formula I ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 are identical or different and are hydrogen, fluorine, chlorine, bromine or iodine atoms, alkyl(C.sub.1 -C.sub.4), acetamido, nitro or carboxyl groups, or R.sub.1 and R.sub.2 together form an aromatic or heteroaromatic ring having 5 or 6 ring members, which can be substituted by fluorine, chlorine, bromine or iodine atoms, alkyl(C.sub.1 -C.sub.4), acetamido, nitro or carboxyl groups, by reaction of aromatic compounds of the formula II ##STR2## in which R.sub.1, R.sub.2 and R.sub.3 have the abovementioned meanings, with chlorosulfonic acid in excess or with chlorosulfonic acid or oleum and thionyl chloride, by reacting in the presence of sulfamic acid as a catalyst.Type: GrantFiled: August 16, 1991Date of Patent: August 4, 1992Assignee: Hoechst AktiengesellschaftInventors: Michael Meier, Wolfgang Tronich
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Patent number: 5132305Abstract: Compounds of general formula (I): ##STR1## in which: R.sub.1 denotes a hydrogen atom or a lower alkyl optionally substituted with a hydroxyl group,R.sub.2 and R.sub.3 :a--identical or different, denote a hydrogen atom, a lower alkyl, a lower alkenyl, a substituted or unsubstituted aryl, a substituted or unsubstituted (lower alkyl)aryl,b--are such that they form, with the nitrogen which carries them, a saturated or unsaturated, mono- or bicyclic heterocyclic system containing at most 3 hetero atoms per ring, substituted or unsubstituted, with the exception of 1-arylpiperazine systems,X denotes a hydrogen atom,Y denotes a hydrogen atom or a hydroxyl,or alternatively X and Y denote an oxygen atom, provided that R.sub.1 is then other than a methyl group,Z denotes a hydrogen atom or forms a .pi. bond with Y, andT denotes a hydrogen atom or a lower alkyl, their stereoisomers and their quaternary ammonium salts, as well as their addition salts with a pharmaceutically acceptable acid.Type: GrantFiled: February 26, 1990Date of Patent: July 21, 1992Assignee: Adir et CompagnieInventors: Daniel Lesieur, Charles Lespagnol, Jacqueline Bonnet
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Patent number: 5114952Abstract: A series of novel alkanesulphonamidophenyl-N-alkyl-N-(heterocyclic-alkyl)alkylamine derivatives have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in therapy as anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrhythmias. Said sulfonamide compounds are of the formula: ##STR1## wherein R and R.sup.1 are each C.sub.1 -C.sub.4 alkyl; X is --CH.sub.2 --, --CO-- or --CH(OH)--; n is two, three or four; and "Het" is a nitrogen-containing heterocyclic group wherein said heterocyclic group is preferably 2H-3,4-dihydroisoquinol-1-on-2-yl or 2H-isoquinol-1-on-2-yl, each optionally substituted with halogen or C.sub.1 -C.sub.4 alkyl.Type: GrantFiled: November 21, 1990Date of Patent: May 19, 1992Assignee: Pfizer Inc.Inventors: John E. Arrowsmith, Peter E. Cross, Geoffrey N. Thomas
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Patent number: 5110823Abstract: Pyrrolidine derivatives of formula (I) are disclosed. ##STR1## wherein the ring A represents the following heterocyclic ring ##STR2## The compounds of formula (I) are useful as nootropic agents.Type: GrantFiled: February 26, 1991Date of Patent: May 5, 1992Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Fumiko Hamaguchi, Tatsuo Nagasaka, Rie Hakamada, Einosuke Sakurai
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Patent number: 5105009Abstract: Intermediates of Formula ##STR1## where R is a methylthio, methylsulfoxy, methylsulfonyl or a nitro group; andX1 is hydrogen, 1-6 C alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl, phenyl or phenylalkyl(1-6C), where the phenyl ring may be substituted by one or two halogen, 1-3 C alkyl, 1-3 C alkoxy or nitro; orX1 together with X2 is an oxygen atom or an alkylene having from two to five Carbon atoms; orX1 together with X2 and R4 is a chain of formula ##STR2## where p is 3 or 4 and q is 1 or 2; and X2 is hydrogen, 1-6 C alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl or phenyl which may be substituted by one or two halogen, 1-3 C alkyl, 1-3 C alkoxy or nitro; orX2 together with R4 is ##STR3## where n is 1 or 2; m is 0 or 1; X is hydrogen, halogen, 1-3 C alkyl, 1-3 C alkoxy or nitro; andX3 is hydrogen or --CO--R4 where R4 is hydrogen, 1-6 alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl, phenylalkyl(1-6C) or phenyl where the phenyl ring may be substituted by one or two halogen, 1-3 alkyl, 1-3 alkoxy or nitro; andX4 is --OH, fluorine,Type: GrantFiled: February 29, 1988Date of Patent: April 14, 1992Assignee: Zambon S.p.A.Inventors: Giancarlo Jommi, Dario Chiarino
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Patent number: 5103007Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.Type: GrantFiled: October 27, 1989Date of Patent: April 7, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
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Patent number: 5102898Abstract: Novel compounds of the formula ##STR1## wherein X is I or Br; andY is independently selected from the group consisting of H, halogen, NO.sub.2, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, CN, OCO (C.sub.1 -C.sub.4) alkyl, OCOPh or halo (C.sub.1 -C.sub.4) alkyl, are disclosed as having microbicidal activity.Type: GrantFiled: May 8, 1991Date of Patent: April 7, 1992Assignee: Rohm and Haas CompanyInventor: Adam C. Hsu
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Patent number: 5101034Abstract: A process for the preparation of a heteroaryloxyacetamide of the formula ##STR1## in which R is a 5 membered heterocycle which may be benzo-fused, andR.sup.1 and R.sup.2 each independently is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, halogenoalkyl, alkoxyalkyl, alkoxy, aralkyl or aryl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, form a heterocycle,which comprises reacting a sulphonylated heteroaromatic of the formulaR--SO.sub.2 --R'in whichR' is lower alkyl or benzyl,with an .alpha.-oxyacetamide of the formula ##STR2## in which R" is hydrogen or acyl,in the presence of an inorganic base as an acid acceptor and of solvent as a diluent at a temperature of about -50.degree. C. to +150.degree. C. The products are known herbicides.Type: GrantFiled: March 7, 1991Date of Patent: March 31, 1992Assignee: Bayer AktiengesellschaftInventors: Thomas Schmidt, Hans-Joachim Diehr
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Patent number: 5099021Abstract: Process for the preparation of pure, unsymmetrically disubstituted ureas of the general formula ##STR1## in which R denotes a phenyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy, aryloxy or trifluoromethyl groups, an oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, benzoxazolyl or benzothiazolyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy or trifluoromethyl groups and R.sub.1 and R.sub.2 independently of one another denote a hydrogen atom or an alkyl group, where R.sub.1 and R.sub.2 are not simultaneously hydrogen or R.sub.1 and R.sub.2 together denote a butylene or pentylene group, by reaction of an N-alkyl- or N,N-dialkylurea with an unsubstituted or substituted arylamine or a heterocyclic amine in the presence of that amine which is already present in the starting material, the respective N-alkyl- or N,N-dialkylurea.Type: GrantFiled: October 30, 1990Date of Patent: March 24, 1992Assignee: Agrolinz Agrarchemikalien Gesellschaft m.b.H.Inventors: Rudolf H. Worther, Horst Korntner, Egmont Auer, Kurt Thonhofer
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Patent number: 5097034Abstract: Color formers of the formula ##STR1## in which X.sup.1 denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy or acyloxy,R.sup.1 denotes hydrogen, halogen, alkyl or alkoxy,R.sup.2 denotes hydrogen, alkoxy, aralkoxy, aryloxy or a radical of the formula ##STR2## Y.sup.1 and Y.sup.2, independently of one another, denote alkyl, cycloalkyl or aralkyl,R.sup.2 can form a heterocyclic ring with A in the o-position, in which a benzene ring can be additionally fused onto ring A in the o-/m-position with respect to R.sup.2,R.sup.3 denotes hydrogen, alkyl, alkenyl, aralkyl, cycloalkyl or aryl, or R.sup.3 is linked to ring B in the o-position with respect to the nitrogen,Z.sup.1 stands for the remaining members of a partially hydrogenated or completely hydrogenated ring, with the proviso that Z.sup.Type: GrantFiled: May 14, 1991Date of Patent: March 17, 1992Assignee: Bayer AktiengesellschaftInventor: Udo Eckstein
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Patent number: 5091533Abstract: Compounds of the formula: ##STR1## where R.sup.2 contains certain aryls or heteroaryls are effective leukotriene inhibitors.Type: GrantFiled: March 12, 1990Date of Patent: February 25, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Patrice C. Belanger, Claude Dufresne, Brian Fitzsimmons, deceased, Maryann Fitzsimmons, Heir, Yvan Guindon, Cheuk K. Lau, Joshua Rokach, John Schiegetz, Michel Therien, Robert N. Young
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Patent number: 5086062Abstract: This invention relates to certain benzoxazolinones which inhibit lipoxygenase and/or cyclooxygenase enzymes. Such compounds are useful in inhibiting such enzymes, per se, and are useful in treating allergic and inflammatory conditions in a mammal. This invention also relates to methods of inhibiting lipoxygenase and/or cyclooxygenase in a mammal with such benzoxazolinones; methods of treating an allergic condition in a mammal with such compounds; methods of treating an inflammatory condition in a mammal with such compounds; and pharmaceutical compositions comprising the benzoxazolinones hereof.Type: GrantFiled: May 29, 1990Date of Patent: February 4, 1992Assignee: Pfizer Inc.Inventors: Kazuo Ando, Nobuko Asai, Fumitaka Ito, Takashi Mano, Masami Nakane, Kunio Satake, Kaoru Shimada
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Patent number: 5081245Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.Type: GrantFiled: August 18, 1989Date of Patent: January 14, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
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Patent number: 5077401Abstract: Herbicidal benzo-fused cyclic compounds of the formula ##STR1## wherein Q is ##STR2## Y is O or S, W is ##STR3## T is O, S, --NH-- or ##STR4## and R.sup.4 may represent, together with T, chlorine,Z is O or S,X is hydrogen or halogen,n is 0 or 1 andR is C.sub.3-6 cycloalkyl, and optionally substituted 5-membered heterocyclic group or an optionally substituted 6-membered heteroaromatic group which contains one to three nitrogen atoms,and salts thereof.Type: GrantFiled: October 6, 1989Date of Patent: December 31, 1991Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Shigeki Yagi, Hiroshi Miyauchi, Katsuhiko Shibuya
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Patent number: 5077309Abstract: Novel compounds have the formula (I) ##STR1## where ##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.1 is a group --(CH.sub.2).sub.b --(A).sub.a --(CH.sub.2).sub.c --B--CH.sub.2 --CO.sub.2 R' in which A and B are each separately oxygen or sulphur, a is 0, b is 0 and c is an integer from 3 to 10, or a is 1, b is 0 or an integer from 1 to 7 and c is an integer from 2 to 9 with the sum of b and c being from 2 to 9, and CO.sub.2 R' is a carboxy group or an amide, ester or salt derivative thereof; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a group --OR.sup.3, --OR.sup.4, --D--R.sup.3, --N.dbd. R.sup.5 or --NW.G.Type: GrantFiled: March 28, 1990Date of Patent: December 31, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5071863Abstract: Certain 6-aryl- or 6-heteroaryl- alkylaminobenzoxazolones, and their pharmaceutically-acceptable salts, are dual inhibitors of lipoxygenase and cyclooxygenase enzymes, and so are useful as antiallergy and antiinflammatory agents.Type: GrantFiled: July 18, 1990Date of Patent: December 10, 1991Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Takashi Mano, Masami Nakane
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Patent number: 5055582Abstract: 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: GrantFiled: December 13, 1988Date of Patent: October 8, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 5037841Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n denotes a number from 1 to 19, andB denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.Type: GrantFiled: April 12, 1989Date of Patent: August 6, 1991Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Peter-Rudolf Seidel, Jorg Traber, Thomas Glaser
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Patent number: 5036088Abstract: Compounds of the formula ##STR1## where Y is alkyl, aryl or heterocyclic, n is 1-7, R is hydrogen, alkyl, aralkyl or carboxymethyl, R.sub.1 is acetoxy, thiophenoxy, hydrogen, halo, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen, alkyl or alkanoyl and X is C.dbd.O, CH.sub.2, NH, O or S as antiallergy and antiinflammatory agents.Type: GrantFiled: December 3, 1990Date of Patent: July 30, 1991Assignee: Pfizer Inc.Inventors: Yoshihiko Kitaura, Fumitaka Ito, Rodney W. Stevens, Nobuko Asai
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Patent number: 5034050Abstract: Derivatives of 4-((aryloxy)phenoxy)alkenols, their preparation and use as active herbicides for the postemergent control of grassy weeds and especially the control of said weeds in the presence of corn plants are disclosed.Type: GrantFiled: June 16, 1989Date of Patent: July 23, 1991Assignee: DowElancoInventors: James A. Turner, Paul S. Zorner, Wendy S. Jacks
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Patent number: 5032590Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical,are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: March 8, 1990Date of Patent: July 16, 1991Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 5026848Abstract: A heteroaryloxyalkylheterocyclic derivative of the Formula I:R--(CH.sub.2).sub.n --O--R.sup.1 Iis provided wherein:R is a non-fused azole moiety;n is 5, 6, 7 or 8; andR.sup.1 is a non-fused or fused substituted azole, azine, furyl or polycyclic hydrocarbon.Type: GrantFiled: March 27, 1989Date of Patent: June 25, 1991Assignee: Synphar Laboratories IncorporatedInventors: Mohsen Daneshtalab, Dai Q. Nguyen, Chan M. Ha, Hiep T. Luu, Laurence M. Tempest, Ronald G. Micetich
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Patent number: 5021438Abstract: Novel compounds having an affinity for 5-hydroxytryptamine receptors of the formula ##STR1## in which R.sup.1 stands for H, alkyl, aralkyl or heteroarylalkyl,X stands for H, OCH.sub.3, OH, SCH.sub.3, halogen, CN or CONH.sub.2,Y stands for a straight-chain or branched, saturated or unsaturated alkylene chain having up to 6 carbon atomsandZ stands for a group of the formula ##STR2## --OR.sup.4, --SO.sub.m R.sup.5, --COOR.sup.6 or CONR.sup.7 R.sup.8 or salts thereof.Type: GrantFiled: March 15, 1989Date of Patent: June 4, 1991Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber
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Patent number: 5007952Abstract: Herbicidally active pyrroles of the formula ##STR1## wherein R.sup.1 represents C.sub.1-4 alkyl, or one R.sup.1 together with the other R.sup.1 forms tetramethylene or butenylene,X represents hydrogen or halogen,Y represents O or S,n represents 0 or 1,R.sup.2 represents hydrogen or an organic radical.Type: GrantFiled: November 9, 1989Date of Patent: April 16, 1991Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Hiroshi Miyauchi, Tadao Asami
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Patent number: 4996218Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, which have .beta..sub.2 -adrenoreceptor stimulant activity. They may be used in the treatment of diseases associated with reversible airways obstruction, such as asthma and chronic bronchitis.In preferred embodiments, Q represents a chlorine atom or a trifluoromethyl group, X represents a C.sub.3-4 alkylene chain, Y a C.sub.1-5 alkylene chain, R, R.sup.1 and R.sup.2 are each preferably a hydrogen atom or a methyl group and Het represents a pyrimidinyl pyrazinyl, triazinyl, thiazolyl, quinolinyl, benzimidazolyl, benzothiazolyl, benzoxazolyl or pyridyl group.Type: GrantFiled: August 10, 1988Date of Patent: February 26, 1991Assignee: Glaxo Group LimitedInventor: Lawrence H. C. Lunts
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Patent number: 4992563Abstract: This invention relates to several intermediates useful in preparing 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.-methano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: February 12, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 4988718Abstract: Fungicidal substituted 4-heterocyclyloximinopyrazolin-5-ones of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another in each case represent hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl or dialkylaminocarbonylalkyl, or represent in each case unsubstituted or in each case substituted oxiranylalkyl, aralkyl, heterocyclyl or aryl andHet represents an unsubstituted or substituted heterocycle.Type: GrantFiled: August 9, 1990Date of Patent: January 29, 1991Assignee: Bayer AktiengesellschaftInventors: Kurt Findeisen, Klaus Jelich, Gerd Hanssler
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Patent number: 4968844Abstract: Retinal is prepared by condensing a C.sub.15 sulphide of formula: ##STR1## in which R.sub.1 denotes aryl, aralkyl, pyridyl, 2-thiazolyl, 2-benzothiazolyl, 2-benzimidazolyl or 2-benzoxazolyl, with a haloacetal of formula: ##STR2## in which X denotes a halogen atom and R denotes an alkyl radical containing 1 to 4 carbon atoms, to give a C.sub.20 sulphide acetal of formula: ##STR3## in which R.sub.1 and R are defined as above, hydrolysing the said sulphide acetal to give a C.sub.20 sulphide aldehyde of formula: ##STR4## in which R.sub.1 is defined as above, desulphurizing the said sulphide aldehyde to give retinal, and isolating the retinal obtained.Type: GrantFiled: October 27, 1988Date of Patent: November 6, 1990Assignee: Centre National de la Recherche Scientifique (C. N. R. S.)Inventor: Marc Julia
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Patent number: 4968681Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical, are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: November 15, 1988Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 4963576Abstract: The invention relates to dithioacetal compounds having 5-lipoxygenase-inhibiting activity, of the formula: ##STR1## wherein R.sup.1 is lower alkyl, di-(lower)alkylamino, aryl, or heterocyclic group which may have one or more substituents selected from halogen, lower alkyl, lower alkoxy and phenyl,R.sup.2 and R.sup.3 are each lower alkyl, aryl or ar-(lower)alkyl, or R.sup.2 and R.sup.3 are together to form 1,3-dithian ring,R.sup.4 is hydrogen or lower alkoxy, andn is O or an integer 1 to 4 and pharmaceutically acceptable salts thereof.Type: GrantFiled: May 6, 1988Date of Patent: October 16, 1990Assignee: Fujisawa Pharmaceutical Company, Ltd.Inventors: Teruo Oku, Yoshio Kawai, Hiroshi Kayakiri, Kazuyoshi Kuratani, Masashi Hashimoto
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Patent number: 4952599Abstract: Novel substituted phenylthioureas, phenylisothioureas and phenylcarbodiimides of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl, unsubstituted or substituted by one or more halogen atoms and/or C.sub.1 -C.sub.6 alkoxy groups; C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl which is substituted by one or more halogen atoms and/or C.sub.1 -C.sub.4 alkyl groups; C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl, di(C.sub.3 -C.sub.8)cycloalkyl-C.sub.1 -C.sub.4 alkyl; C.sub.1 -C.sub.4 phenylalkyl or C.sub.1 -C.sub.4 phenylalkyl which is substituted in the phenyl nucleus by one or more members selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and/or C.sub.1 -C.sub.4 haloalkyl; or is C.sub.5 -C.sub.6 cycloalkenyl,R.sub.2 is hydrogen, C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkenyl,R.sub.3 is C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen or C.sub.1 -C.sub.3 alkyl,R.sub.Type: GrantFiled: July 20, 1988Date of Patent: August 28, 1990Assignee: Ciba-Geigy CorporationInventors: Josef Ehrenfreund, Manfred Boger, Jozef Drabek
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Patent number: 4937255Abstract: For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, a cation or alkyl, aryl or aralkyl.Type: GrantFiled: March 16, 1989Date of Patent: June 26, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
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Patent number: 4935522Abstract: A method for producing ethyl 2-[4'-(6"-chloro-2"-benzoxazolyloxy)phenoxy]propanoate by reacting a hydroxyaromatic ketone derivative with a 2-substituted propanoic ester under basic conditions and thereafter oxidizing the intermediate with subsequent hydrolysis and reaction with 2,6-dichlorobenzoxazole.Type: GrantFiled: March 21, 1988Date of Patent: June 19, 1990Assignee: Hoechst Celanese CorporationInventors: Varadaraj Elongo, Kenneth G. Davenport
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Patent number: 4935423Abstract: A substituted, 1,2,4-triazinedione of the formula ##STR1## in which R.sup.1 stands for an unsubstituted or substituted heteroaromatic radicals bonded via carbon,X stands for one or more, identical or different radicals selected from the group consisting of hydrogen, halogen, nitro, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy and halogenoalkylthio.R.sup.3 stands for hydrogen, unsubstituted or substituted alkyl, alkenyl, alkinyl or aralkyl. The substituted 1,2,4-triazinedione is useful to combat parasitic protozoa in warmblooded animals.Type: GrantFiled: February 14, 1989Date of Patent: June 19, 1990Assignee: Bayer AktiengesellschaftInventors: Werner Lindner, Axel Haberkorn
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Patent number: 4911754Abstract: This invention relates to aryloxy dihydrobenzofuran, oxoindole or benzofuranone derivatives having herbicidal activity and to the use of such compounds to control the growth of noxious plants, i.e., weeds.Type: GrantFiled: July 16, 1987Date of Patent: March 27, 1990Assignee: American Cyanamid CompanyInventors: David A. Hunt, James A. Schwindeman
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Patent number: 4910309Abstract: The optical purity of an optically active 2-(4-aryloxyphenoxy)propionic acid is enriched by formation of the hydrate of the enantiomer in excess and its removal from solution.Type: GrantFiled: July 8, 1988Date of Patent: March 20, 1990Assignee: The Dow Chemical CompanyInventors: Larry D. Kershner, Jimmy J. Tai