Nitrogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/491)
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Patent number: 5112382Abstract: Compounds of the formula ##STR1## wherein A is selected from the group consisting of (1) phenyl, (2) naphthyl, (3) phenyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4) alkyl, nitro, (C.sub.1 -C.sub.4)haloalkyl, and (C.sub.1 -C.sub.4)thioalkyl, (4) naphthyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4)alkyl,nitro,(C.sub.1 -C.sub.4), and (C.sub.1 -C.sub.4) thioalkyl, (5) thiophene, (6) furan, (7) thiophene substituted with one or more substituents selected from halo and nitro, and (8) furan substituted with one or more substituents selected from halo and nitro;R disclose as microbicidally and fungicidally active.Type: GrantFiled: May 24, 1990Date of Patent: May 12, 1992Assignee: Rohm and Haas CompanyInventor: Adam C. Hsu
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Patent number: 5110831Abstract: The present invention relates to vinylogous hydroxamic acids, processes for their manufacture, pharmaceutical preparations containing them, and their use in the treatment of various disorders.Type: GrantFiled: November 30, 1990Date of Patent: May 5, 1992Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Ronald L. Magolda, Stephen W. Wright
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Patent number: 5103019Abstract: A novel process for obtaining an .alpha.-amino-nitrile of the formula ##STR1## by reacting a nitrile with a metallic reducing agent to form a metallic imine of the formula ##STR2## and reacting the latter with a cyaniding agent to obtain the corresponding .alpha.-amino-nitrile.Type: GrantFiled: May 2, 1990Date of Patent: April 7, 1992Assignee: Albert Rolland S.A.Inventors: Gerard Moinet, Thierry Imbert
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Patent number: 5089639Abstract: N-Cycloalkylalkylamines of formula I: ##STR1## in which: R1 is phenyl which is optionally mono-, di- or trisubstituted by halogens or lower alkyl, haloalkyl or lower alkoxy radicals, or is an aromatic heterocyclic radical having 5 to 7 chain members, in which the hetero atom is nitrogen, oxygen or sulphur,R2 is lower alkyl,R3 is hydrogen or lower alkyl,m has the value of 1 or 2,R4 is cycloalkyl --CH(CH2)n, in which a carbon atom may carry a radical Rx, which is lower alkyl or phenyl; and in which n has the values from 2 to 5,R5 is phenyl, which can be mono-, di- or trisubstituted by halogens or by lower alkoxy radicals, andQ represents an ethylene-1,2-diyl group --CH.dbd.Type: GrantFiled: January 24, 1991Date of Patent: February 18, 1992Assignee: Jouveinal S.A.Inventors: Gilbert G. Aubard, Alain P. Calvet, Jean-Pierre Defaux, Claude J. Gouret, Agnes M. Grouhel, Henry L. Jacobelli, Jean-Louis Junien, Xavier B. Pascaud, Francois F. Roman, James P. Hudspeth, Yuan Lin
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Patent number: 5086074Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sup.2 is selected from hydroxy and lower alkoxy, R.sup.5 is lower alkyl, and R.sup.11 and R.sup.12 are independently selected from hydrogen, halo, hydroxy, methoxy, and lower alkyl, are selective .alpha..sub.2 adrenergic receptor antagonists useful in the treatment of glaucoma.Type: GrantFiled: March 26, 1990Date of Patent: February 4, 1992Assignee: Abbott LaboratoriesInventors: John F. DeBernardis, Robert E. Zelle, Fatima Z. Basha
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Patent number: 5081246Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: December 20, 1989Date of Patent: January 14, 1992Assignees: Hiroyoshi Hidaka, Tobishi Yakuhin Kogyo Kabushiki KaishaInventors: Horoyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
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Patent number: 5077411Abstract: The present invention is novel diarylalkanoids having activity as lipoxygenase inhibitors, novel pharmaceutical compositions therefor, and novel methods of use in treating asthma, allergies, cardiovascular diseases, migrains, psoriasis and immunoinflammatory diseases for diarylalkanoids. The compounds of this invention are also useful as cytoprotective agents.Type: GrantFiled: June 21, 1990Date of Patent: December 31, 1991Assignee: Warner-Lambert Co.Inventors: David T. Connor, Daniel L. Flynn
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Patent number: 5055471Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.Type: GrantFiled: November 15, 1989Date of Patent: October 8, 1991Assignee: Imperial Chemical Industries PLCInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5045566Abstract: A series of novel imidate insecticides distinguished by the general formula ##STR1## in which R.sub.1 is an optionally substituted aryl group in which the substituents are halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkylthio, C.sub.3 -C.sub.6 cycloalkyl, nitro, C.sub.1 -C.sub.4 haloalkyl, C.sub.2 -C.sub.5 carboalkoxy, C.sub.1 -C.sub.4 alkylthio, cyano, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.2 -C.sub.4 haloalkylsulfonyl; C.sub.2 -C.sub.5 alkylcarbonyl, C.sub.2 -C.sub.4 alkyleneoxy, C.sub.1 -C.sub.2 perhaloalkyleneoxy; C.sub.1 -C.sub.4 alkylendioxy, C.sub.1 -C.sub.3 halo-substituted alkylenedioxy, phenyl, mono-substituted phenyl, pyridyloxy, C.sub.2 -C.sub.4 alkylene, C.sub.2 -C.sub.4 alkenyl, C.sub.3 -haloalkenoxy; and/or amido;R.sub.2 is C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.6 haloalkyl, cyclopropyl, cyclobutyl, mono- or poly- halo- or methyl-substituted cyclopropyl, cyano, C.sub.2 -C.sub.4 alkoxyalkyl, C.sub.2 -C.sub.6 haloalkenyl or C.sub.2 -C.Type: GrantFiled: April 27, 1989Date of Patent: September 3, 1991Assignee: ICI Americas Inc.Inventors: Michael D. Broadhurst, Thomas H. Cromartie, Karl J. Fisher, William G. Haag
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Patent number: 5041663Abstract: The invention relates to novel oxime ethers of the formula I ##STR1## wherein R.sub.1 is hydrogen, halogen, lower alkyl, lower haloalkyl, lower alkoxy, lower haloalkoxy, lower alkylthio, lower haloalkylthio, lower alkylsulfinyl, lower alkylsulfonyl, lower haloalkylsulfinyl, lower haloalkylsulfonyl or nitro, each of R.sub.2 and R.sub.3 is hydrogen, halogen, lower alkyl, lower alkoxy or lower haloalkoxy, and Q is an unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl or cycloalkyl group, a lower alkanoyl radical, an aliphatic, cycloaliphatic, aromatic or heterocyclic acyl radical which may be substituted or unsubstituted, a carbonyl or thiocarbonyl radical, an aryl or aralkyl radical, an acylimidomethyl radical, a phthalimidomethyl radical or a heterocyclic radical.These compounds are able to act as antidotes or safeners for protecting cultivated plants from the phytotoxic action of aggressive herbicides.Type: GrantFiled: December 11, 1990Date of Patent: August 20, 1991Assignee: Ciba-Geigy CorporationInventors: Henry Martin, Urs Fricker
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Patent number: 5034419Abstract: N-Cycloalkylalkylamines of formula I: ##STR1## in which: R1 is phenyl which is optionally mono-, di- or trisubstituted by halogens or lower alkyl, haloalkyl or lower alkoxy radicals, or is an aromatic heterocyclic radical having 5 to 7 chain members, in which the hetero atom is nitrogen, oxygen or sulphur,R2 is lower alkyl,R3 is hydrogen or lower alkyl,m has the value of 1 or 2,R4 is cycloalkyl --CH(CH2)n, in which a carbon atom may carry a radical Rx, which is lower alkyl or phenyl; and in which n has the values from 2 to 5,R5 is phenyl, which can be mono-, di- or trisubstituted by halogens or by lower alkoxy radicals, andQ represents an ethylene-1,2-diyl group --CH.dbd.Type: GrantFiled: February 26, 1990Date of Patent: July 23, 1991Assignee: L'OrealInventors: Gilbert G. Aubard, Alain P. Calvet, Jean-Pierre DeFaux, Claude J. Gouret, Agnes M. Grouhel, Henry L. Jacobelli, Jean-Louis Junien, Xavier Pascaud, Francois F. Roman, James P. Hudspeth, Yuan Lin
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Patent number: 5034537Abstract: This invention relates to (R)-.alpha.-methyl-4-halobenzenemethanamine salts of epimers of acids of the formula ##STR1## and the use of these salts to separate these epimers. These acids are leukotriene antagonists.Type: GrantFiled: February 8, 1990Date of Patent: July 23, 1991Assignee: SmithKline Beecham CorporationInventor: James S. Frazee
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Patent number: 5034047Abstract: Cyclohexenone derivatives of the general formula I ##STR1## where the substituents have the following meanings: R.sup.1 : substituted or unsubstituted C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -alkenyl or C.sub.3 -C.sub.6 -alkynyl, phenyl, benzyl or thenyl;R.sup.2 : substituted or unsubstituted C.sub.1 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl or phenyl;R.sup.3 : hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.10 -alkylcarbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.4 -trialkylsilyl, C.sub.1 -C.sub.4 -dialkylphosphonyl, C.sub.1 -C.sub.4 -dialkylthiophosphonyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkenylcarbonyl, C.sub.3 -C.sub.6 -alkynyl or substituted or unsubstituted benzoyl- or phenylsulfonyl;R.sup.4 : hydrogen, cyano, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxycarbonyl;A: a substituted or unsubstituted C.sub.1 -C.sub.Type: GrantFiled: August 24, 1990Date of Patent: July 23, 1991Assignee: BASF AktiengesellschaftInventors: Dieter Kolassa, Juergen Kast, Thomas Kuekenhoehner, Norbert Meyer, Karl-Otto Westphalen, Bruno Wuerzer
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Patent number: 5023269Abstract: The present invention provides 3-aryloxy-3-substituted propanamines capable of inhibiting the uptake of serotonin and norepinephrine.Type: GrantFiled: March 27, 1990Date of Patent: June 11, 1991Assignee: Eli Lilly and CompanyInventors: David W. Robertson, David T. Wong, Joseph H. Krushinski, Jr.
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Patent number: 5022914Abstract: Cyclohexenone oxime ethers of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl,A is substituted or unsubstituted C.sub.4 -alkylene or C.sub.4 -alkenylene,X is nitro, cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl and/or phenyl,n is from 0 to 3 or from 1 to 5 when X is halogen,R.sup.2 is C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl or C.sub.5 -C.sub.Type: GrantFiled: October 31, 1989Date of Patent: June 11, 1991Assignee: BASF AktiengesellschaftInventors: Juergen Kast, Dieter Kolassa, Norbert Meyer, Ulrich Schirmer, Albrecht Harreus, Jochen Wild, Karl-Otto Westphalen, Bruno Wuerzer
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Patent number: 5021413Abstract: Analgesic compounds are of the general formula (I): ##STR1## in which, R.sup.1 and R.sup.2 each represents hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocycle; E represents methylene, sulfur, oxygen or imino group optionally substituted with C.sub.1 -C.sub.6 alkyl or aralkyl; ring A is aryl or heteroaryl ring, optionally substituted; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen or R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(.dbd.Y)-- (IV)(wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen, up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygen); provided that when E represents a methylene group, then R.sup.3 is a C.sub.1 -C.sub.6 alkyl group or R.sup.3 and R.sup.4 together represent a group of the formula (IV).Type: GrantFiled: August 22, 1989Date of Patent: June 4, 1991Assignee: Sankyo Company LimitedInventors: Atsusuke Terada, Yoshio Iizuka, Kazuyuki Wachi, Kenji Fujibayashi
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Patent number: 5021458Abstract: Amine derivatives having the general formula (I): ##STR1## wherein X is selected from the group consisting of ##STR2## wherein Q is oxygen, sulfur or nitrogen atom, and ##STR3## wherein Q is as above; Y is selected from the group consisting of ##STR4## R.sup.1 is hydrogen atom or an alkyl group; R.sup.2 is hydrogen atom or an alkyl group; R.sup.3 is hydrogen atom, a halogen atom or an alkyl group; R.sup.4 is hydrogen atom, an alkyl group, a cycloalkyl group, a halogenated alkyl group or a halogen atom; R.sup.5 is hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, nitro group or hydroxy group; R.sup.5 is attached to an arbitrary position of X, and R.sup.3 or R.sup.4 is attached to an arbitrary position of Y.The amine derivatives (I) are useful as fungicides.Type: GrantFiled: December 7, 1988Date of Patent: June 4, 1991Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Tetsuya Maeda, Toshiyuki Yamamoto, Mituo Takase, Kazuya Sasaki, Tadashi Arika, Mamoru Yokoo, Rieko Hashimoto, Kouji Amemiya, Sakae Koshikawa
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Patent number: 4990630Abstract: The present invention relates to a 2,3-diaminoacrylonitrile derivative or salts thereof, having the formula ##STR1## wherein R represents an alkyl group (which may be substituted by unsubstituted or substituted phenyl groups, halogen atoms, C.sub.1-6 alkoxycarbonyl groups, carboxy groups, C.sub.1-6 alkoxycarbonyl C.sub.1-6 alkylthio groups, hydroxy groups, mercapto groups, cycloalkyl groups or heterocyclic groups containing oxygen atoms); an alkenyl group; a cycloalkyl group; an aryl group (which may be substituted by halogen atoms, C.sub.1-6 alkyl groups, nitro-groups, unsubstituted or substituted phenyl or phenoxy groups or heterocyclic groups containing oxygen atoms or sulfur atoms).The 2,3-diaminoacrylonitrile derivative can be used as starting materials for the production of pharmaceutical and/or agricultural intermediates such as cyanoimidazoles, cyanopyrazines or other cyano-substituted heterocycles.Type: GrantFiled: August 28, 1989Date of Patent: February 5, 1991Assignee: Nippon Soda Co., Ltd.Inventors: Katsunori Mikuma, Nobuhiro Umeda, Tomio Yagihara, Isami Hamamoto
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Patent number: 4990668Abstract: Described is a process for preparing a racemic or chiral aryloxypropanolamine (1) or arylethanolamine (2) of the formula ##STR1## wherein Ar is aryl, substituted aryl, heteroaryl, or aralkyl and R is alkyl, substituted alkyl, aralkyl, or WB wherein W is a straight or branched chain alkylene of from 1 to about 6 carbon atoms and wherein B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, where R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.sub.5 are not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.3 or --NR.sub.3 COOR.sub.5, or R.sub.3 and R.sub.4 may together with N form a 5- to 7-membered heterocyclic group.The process can be used to prepare beta-blocking agents, useful in the treatment of cardiac conditions.Type: GrantFiled: December 4, 1985Date of Patent: February 5, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventors: Khuong H. X. Mai, Ghanshyam Patil, William L. Matier
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Patent number: 4977146Abstract: The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group, Y is an alkyl or substituted alkyl group, R.sup.6 is an alkyl or a substituted alkyl group and the substituents at positions 3, 4 or 5 are acyclic.Type: GrantFiled: April 11, 1990Date of Patent: December 11, 1990Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Mitree M. Ponpipom, Nirindar N. Girotra
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Patent number: 4973715Abstract: This invention relates to novel furan polyols, which are characterized in that they are the product of reaction of a strain selected from the group or consisting of a polyalcohol, a monoamine or polyamine, said polyalcohol or said amine possibly containing a furan cycle and mixtures thereof with a chain extension agent constituted by an organic epoxide, with the proviso that this organic epoxide is a furannic oxiran when this polyalcohol does not contain a furan cycle with the exclusion of 2,5(bis-hydroxy)furan as sole strain, when the chain extension agent does not contain any furan cycle. These furan polyols are used for the preparation of polyurethane foams having improved properties.Type: GrantFiled: August 22, 1988Date of Patent: November 27, 1990Assignee: Centre Scientifique et Technique du BattmentInventors: Gabriel Roux, Janine Rivero, Alessandro Gandini
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Patent number: 4965377Abstract: 2-(2-bromo-2-nitroethenyl)-furan can be used as an antimicrobial in broad spectrum of uses. A novel process for preparing 2-(2-bromo-2-nitroethenyl)-furan has been found in which furfural is reacted with bromonitromethane using a primary amine or primary amine salt as a catalytic agent to produce an intermediate product which is dehydrated in the presence of acid to the desired product. An antimicrobial composition comprising 2-(2-bromo-2-nitroethenyl)-furan and a carrier is also disclosed.Type: GrantFiled: September 13, 1989Date of Patent: October 23, 1990Assignee: Great Lakes Chemical CorporationInventors: William F. McCoy, Scott Thornburgh
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Patent number: 4964846Abstract: This invention comprises a process for the production of unsymmetrical olefins from prochiral symmetrical ketones by addition of lithiosulfoximine from n-butyllithium and N-substituted S-methyl-S-phenyl-sulfoximine derivatives and then reaction with n-butyllithium/trimethychlorosilane.Type: GrantFiled: November 21, 1988Date of Patent: October 23, 1990Assignee: Schering AktiengesellschaftInventors: Hans-Joachim Gais, Irene Erdelmeier, Rolf Birk
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Patent number: 4962212Abstract: The invention disclosed herein relates to a process for producing heterocyclic ethanolamines, especially 2-(2-furyl)ethanolamine.Type: GrantFiled: December 26, 1989Date of Patent: October 9, 1990Assignee: Monsanto CompanyInventor: Lowell R. Smith
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Patent number: 4945111Abstract: Fungicidal N,N'-diacylaminals of the formula ##STR1## in which R.sup.1 is optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl or cycloalkenyl,R.sup.2 and R.sup.3 are hydrogen or various organic radicals, andX is oxygen or sulphur.Type: GrantFiled: August 11, 1988Date of Patent: July 31, 1990Assignee: Bayer AktiengesellschaftInventors: Winfried Lunkenheimer, Dieter Berg, Wilhelm Brandes
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Patent number: 4923882Abstract: This invention relates to amine derivatives and salts thereof. These compounds have an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such compound, a process for the preparation thereof and an anti-ulcer agent containing the same.Type: GrantFiled: October 16, 1986Date of Patent: May 8, 1990Assignee: Toyama Chemical Co., Ltd.Inventors: Shiro Hirai, Hiroshi Hirano, Hirotoshi Arai, Yasuo Kiba, Hisanari Shibata, Yoshikazu Kusayanag, Minako Yotsuji, Kazuhiko Hashiba, Kikuko Tanada
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Patent number: 4917826Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.Type: GrantFiled: June 16, 1987Date of Patent: April 17, 1990Assignee: The Upjohn CompanyInventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased
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Patent number: 4888338Abstract: This invention relates to new tetrahydrofurans and tetrahydrothiophenes of the general formula: ##STR1## wherein X stands for O or S, m is an integer from 1 to 12 and A is a pyridinium or an ammonium salt, to a preparation process of said compounds and to therapeutic compositions of matter containing the same.Type: GrantFiled: May 27, 1988Date of Patent: December 19, 1989Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Jean-Jacques Godfroid, Pierre Braquet
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Patent number: 4882354Abstract: The present invention involves certain N-hydroxy-5-phenyl-2-furancarboximidamides, pharmaceutical compositions containing such compounds, and methods for increasing the contractile force of cardiac muscle of a mammal which comprises systemically administering such compounds to a mammal.Type: GrantFiled: December 16, 1987Date of Patent: November 21, 1989Assignee: Norwich Eaton Pharmaceuticals, Inc.Inventors: Chau-Ting Huang, Stanford S. Pelosi, Jr., Allan V. Bayless
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Patent number: 4870100Abstract: 2-benzylfuryl compounds of the general formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are identical or different substituents and are each hydrogen, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, haloalkylthio, alkenyl or haloalkenyl, each of not more than 6 carbon atoms, n being 1, 2 or 3 where R.sup.3 is not hydrogen, and R.sup.4 and R.sup.5 are each hydrogen or alkyl of not more than 6 carbon atoms, R is --CHO or CHR.sup.6 OA, R.sup.6 is hydrogen, cyano, alkyl, alkenyl, haloalkenyl or alkynyl, each of not more than 6 carbon atoms, or carboxamide, and A is either hydrogen or a radical of an acid typical for pyrethroids, with the proviso that R.sup.2 is not hydrogen, chlorine, bromine, methyl or methoxy when R.sup.1 is hydrogen or methyl and R.sup.3 and A are each hydrogen, and furthermore with the proviso that R.sup.1 and R.sup.2 are not methyl when A is a radical of tetramethylcyclopropanecarboxylic acid, and finally with the proviso that R.sup.2 is not methyl, chlorine, bromine or methoxy and R.Type: GrantFiled: December 11, 1986Date of Patent: September 26, 1989Assignee: BASF AktiengesellschaftInventors: Bernd Wolf, Hans Theobald, Rainer Becker, Norbert Goetz, Walter Himmele, Rudolf Kropp
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Patent number: 4859784Abstract: Optically active cyanohydrins are produced by the reaction of an aldehyde with hydrocyanic acid in the presence of D-oxynitrilase (E.C.4.1.2.10). The reaction takes place in an organic solvent which is not miscible with water, but which is saturated with water or an aqueous buffer solution.Type: GrantFiled: January 19, 1988Date of Patent: August 22, 1989Assignee: Degussa AktiengesellschaftInventors: Franz Effenberger, Thomas Ziegler, Siegfried Foerster
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Patent number: 4857070Abstract: The invention relates to new 2,4-diaminophenyl tetrahydrofurfuryl ethers of the general formula VIII and to their salts with inorganic or organic acids ##STR1## in which R.sub.1, R.sub.2, R.sub.3 and R.sub.4, independently of one another, each represent a hydrogen atom, a (C.sub.1 -C.sub.4)alkyl group, hydroxy(C.sub.2 -C.sub.4)alkyl group, dihydroxy(C.sub.3 -C.sub.4)alkyl group, halogeno(C.sub.2 -C.sub.4)alkyl group, amino(C.sub.2 -C.sub.4)alkyl group or an amino(C.sub.2 -C.sub.4)alkyl group which is substituted once or twice by methyl, ethyl or hydroxyethyl radicals on the nitrogen, the carbon chain having a straight or branched arrangement, and it being a proviso that at least one of R.sub.1, R.sub.2, R.sub.3 and R.sub.Type: GrantFiled: February 8, 1988Date of Patent: August 15, 1989Inventors: Winfried Seidel, Horst Tappe
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Patent number: 4849530Abstract: The invention relates to novel crystalline salts of aryloxypropanolamines with diphenylacetic acid, a process for their preparation and the use of these salts for the preparation of chemically pure aryloxy-propanolamines or pharmaceutically acceptable salts thereof.Type: GrantFiled: June 6, 1988Date of Patent: July 18, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Gerhard Zol, Gerhard Pfarrhofer
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Patent number: 4827019Abstract: Photographic coupler solvents comprising aromatic carboxylic esters such as phthalates and isophthalates having bulky or branched ester substituents are described for incorporation in photographic emulsions and elements. The solvents are preferably employed in the cyan layer to protect the cyan dye against ferrous ion reduction. The solvents also provide improvements in yellow dye stability to light, cyan dye stability in the dark and magenta dye stability to heat and light.Type: GrantFiled: January 12, 1987Date of Patent: May 2, 1989Assignee: Eastman Kodak CompanyInventor: Sundaram Krishnamurthy
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Patent number: 4820858Abstract: The invention relates to a process for the preparation of 2-(hydroxyalkyl)acrylic compounds having the formula ##STR1## wherein X represents a --CN group, a --COOR.sub.3 group, a --COR.sub.4 group or a --CONR.sub.4 R.sub.5 group wherein R.sub.3 is an alkyl group containing 1-4 C atoms and R.sub.4 and R.sub.5 independently represent an H atom or R.sub.3, andwherein R.sub.1 and R.sub.2 independently represent an H atom or an alkyl group with 1-4 C atoms or an (hetero) aryl group, or R.sub.1 and R.sub.2 together represent a cyclic compound with 5-12 C atomsby contacting an acrylic compound H.sub.2 C.dbd.CH--X with a carbonyl compound of the formula ##STR2## wherein X, R.sub.1 and R.sub.2 denote the same as in the above, this being effected in the liquid phase in the presence of a tertiary amine, characterized in that the reaction is carried out at a pressure in excess of 500 bar in excess of 500 bar, advantageously 1,500-18,000 bar.Type: GrantFiled: March 18, 1988Date of Patent: April 11, 1989Assignee: Stamicarbon B.V.Inventors: Neil S. Isaacs, Jonathan Hill
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Patent number: 4786646Abstract: The invention relates to compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het or aryl, *E is ##STR2## or --(CH.sub.2).sub.k -- wherein k is an integer from 0 to 4, R.sub.3, R.sub.4 and R.sub.8 are independently hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently are hydrogen or lower alkyl, R.sub.Type: GrantFiled: July 10, 1987Date of Patent: November 22, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
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Patent number: 4783473Abstract: Geminally-substituted cyclic ether carboxylic acids or derivatives thereof are provided which have the structure ##STR1## wherein Z is aryl, which may be optionally substituted with one or more of the following groups: halo, lower alkyl, lower alkoxy, hydroxy, lower alkylamino, phenyl or carbo-lower alkoxy ##STR2## R is COOH, COO alkali metal, coo lower alkyl, ##STR3## R.sup.1 is lower alkyl or aryl; n is 1 or 2;p is 2 to 5; andq is 1 to 4.These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic disease.Type: GrantFiled: September 2, 1987Date of Patent: November 8, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: Steven E. Hall, Philip M. Sher
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Patent number: 4778818Abstract: Substituted cinnamyl-2,3-dihydrobenzofurans and analogs were prepared from the nucleophlic substitution of a cinnamylhalide with a 2,3-dihydrobenzofuran anion or an analog thereof. These compounds were found to be potent topical anti-inflammatory agents.Type: GrantFiled: April 17, 1987Date of Patent: October 18, 1988Assignee: Merck & Co., Inc.Inventors: Michael N. Chang, Norman P. Jensen, Milton L. Hammond, Robert A. Zambias, John McDonald, Kathleen M. Rupprecht
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Patent number: 4772714Abstract: Disclosed is a process for the preparation of alpha-aryl and alpha-heteroaryl ketones useful as intermediates in the synthesis of various pharmaceutical and agricultural chemicals, which process operates according to the following reaction scheme: ##STR1##Type: GrantFiled: July 7, 1986Date of Patent: September 20, 1988Assignee: Agency of Industrial Science & TechnologyInventors: Masato Tanaka, Toshiyasu Sakakura
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Patent number: 4744812Abstract: Substituted diphenyl ethers of the formula ##STR1## where Z.sub.1, Z.sub.2 and Z.sub.3 are hydrogen, halogen, nitro, cyano, carboxyl, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylmercapto, haloalkylmercapto, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl or haloalkylsulfonyl, Z.sub.4 is hydrogen, cyano, alkyl, alkoxy, acetoxy or alkylmercapto, Y is hydrogen, halogen, cyano or nitro, X is oxygen, sulfur, sulfinyl or sulfonyl, and A is hydrogen, unsubstituted or substituted alkyl ##STR2## and can also be sulfonyl ##STR3## when X is oxygen, and, when Z.sub.4 is alkoxy or alkylmercapto, can also be a methylene chain --(CH.sub.2).sub.m -- by which the radicals Z.sub.4 --CH--X-- are bonded to form a ring, R.sub.1 is hydrogen, methyl, ethyl or n-propyl, R.sub.2 is cyano, methoxy, ethoxy or ##STR4## where B is OH, ONa, O--alkyl, unsubstituted or substituted phenoxy, --NH.sub.2, --NH--alkyl or --N(alkyl).sub.2, n is 1, 2 or 3, R.sub.3 and R.sub.Type: GrantFiled: March 4, 1985Date of Patent: May 17, 1988Assignee: BASF AktiengesellschaftInventors: Adolf Parg, Bruno Wuerzer, Gerhard Hamprecht
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Patent number: 4743617Abstract: This invention relates to novel heterocyclyl-2-propyn-1-amines which are useful as dopamine beta hydroxylase inhibitors in the treatment of hypertension.Type: GrantFiled: August 31, 1987Date of Patent: May 10, 1988Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Thomas M. Bargar, Lawrence C. Creemer, James R. McCarthy
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Patent number: 4743602Abstract: According to the invention there are provided compounds useful for combatting fungi having the general formula (I): ##STR1## and stereoisomers thereof, wherein one of X and Y, but not both, is a group of the formula (II): ##STR2## and the other of X and Y is a hydrogen atom, a halogen atom, or an alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, aralkyl, alkoxy, aryloxy or haloalkyl group or a ##STR3## group wherein R.sup.9, R.sup.10 and R.sup.11 can be alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or aryl, Z is an oxygen atom, a sulphur atom or an --NH-group, A and B have the same significance as X or Y excluding a group of formula (II), R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each represent a hydrogen atom, a halogen atom or an alkyl group containing from 1 to 4 carbon atoms, R.sup.5 and R.sup.6 each represent a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, and R.sup.7 and R.sup.8 each represent an alkyl group containing from 1 to 4 carbon atoms or R.sup.7 and R.sup.Type: GrantFiled: June 30, 1987Date of Patent: May 10, 1988Assignee: Imperial Chemical Industries PLCInventors: Paul A. Worthington, Vivienne M. Anthony
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Patent number: 4739068Abstract: N-Phenylsulfonyl-N'-pyrimidinylureas and --N'-triazinylureas of the general formula ##STR1## and the salts of these compounds with amines, alkali metal bases and alkaline earth metal bases or with quaternary ammonium bases, have good selective herbicidal and plant growth regulating properties when applied pre- and postemergence.In the formulaR.sub.1 is hydrogen, halogen, nitro, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.5 alkenyl or C.sub.1 -C.sub.4 alkoxycarbonyl,R.sub.2 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy, each unsubstituted or substituted by 1 to 3 halogen atoms,R.sub.3 is halogen, hydrogen, --NR.sub.4 R.sub.5, C.sub.1 -C.sub.3 alkyl, unsubstituted or substituted by 1 to 3 halogen atoms or C.sub.1 -C.sub.4 alkoxy, or is C.sub.1 -C.sub.3 alkoxy, unsubstituted or substituted by methoxy, ethoxy, or 1 to 3 halogen atoms,R.sub.4 is hydrogen or methyl,R.sub.5 is hydrogen, C.sub.1 -C.sub.2 alkyl or methoxy,A is C.sub.1 -C.sub.4 alkylene or C.sub.Type: GrantFiled: July 21, 1986Date of Patent: April 19, 1988Assignee: Ciba-Geigy CorporationInventors: Karl Gass, Werner Fory, Willy Meyer, Werner Topfl
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Patent number: 4736055Abstract: Oxime sulfonates of formula I ##STR1## wherein Y is a polymerizable unsaturated group or epoxide group or an --OH, --NHR.sup.5, --COOH, COOR.sup.6, --COCl, --CH.sub.2 Hal, --SO.sub.2 Cl or --NCO group, Z is an (x+y)-valent connecting member, R.sup.1 and R.sup.2 are monovalent organic radicals, m is 0 or 1, x is 1 or 2 and y is 1 or 2, can be converted into polymers which can be thermally or photochemically dissociated to form free sulfonic acid groups. Said polymers can therefore be used as photoresists which can be developed with aqueous alkalis.Type: GrantFiled: April 11, 1986Date of Patent: April 5, 1988Assignee: Ciba-Geigy CorporationInventors: Kurt Dietliker, Werner Rutsch, Godwin Berner, Max Hunziker, Christopher G. Demmer
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Patent number: 4728666Abstract: Heterocyclic acetylenes of the formula (I): ##STR1## wherein Y and R.sup.1 are substituents such as hydrogen, alkyl, alkoxy, chloro or fluoro, m is 0-2, R.sup.2 is branched alkyl and Het is an aromatic heterocycle. The acetylenes are useful in treating hypertension and/or angina.Type: GrantFiled: November 24, 1986Date of Patent: March 1, 1988Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4725602Abstract: Acetylenes of the following formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, R.sup.3, n and R.sup.4 are defined herein and R.sup.5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and antihypertensives.Type: GrantFiled: October 24, 1985Date of Patent: February 16, 1988Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4703058Abstract: This invention relates to novel .beta.-methylenefuranethanamines which are mechanism-based inhibitors of dopamine beta-hydroxylase useful as antihypertensive agents.Type: GrantFiled: June 6, 1986Date of Patent: October 27, 1987Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Thomas M. Bargar, Robert Broersma, Jr., James R. McCarthy
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Patent number: 4695634Abstract: Hypoglycemic 5-furyl and 5-thienyl derivatives of oxazolidine-2,4-dione and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; and intermediates useful in the preparation of said compounds.Type: GrantFiled: August 6, 1986Date of Patent: September 22, 1987Assignee: Pfizer Inc.Inventor: Rodney C. Schnur
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Patent number: 4695656Abstract: 2,4-Dinitrophenyl ethers are prepared by reacting a 2,4-dinitrochlorobenzene or 2,4-dinitrobromobenzene with an alkali metal alcoholate in a non-polar, inert solvent, at a temperature from -25.degree. C. to 50.degree. C.Type: GrantFiled: March 31, 1986Date of Patent: September 22, 1987Assignee: Cassella AktiengesellschaftInventors: Kuno Reh, Friedrich Schophoff
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Patent number: 4692513Abstract: Alpha-L-Aspartyl-D-heteroaromatic-substituted glycine esters and amides are disclosed to be useful as high intensity sweeteners. These compounds can be used to sweeten a variety of foods, beverages and other oral products.Type: GrantFiled: December 20, 1985Date of Patent: September 8, 1987Assignee: The Procter & Gamble CompanyInventors: Robert B. Blum, John M. Gardlik, John M. Janusz, George P. Rizzi