The Ring Oxygens Are In The 1,2- Or 1,3-positions Of The Hetero Ring Patents (Class 549/365)
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Patent number: 4730008Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein Ar, R.sup.1, R.sup.2, X, Y and Q are defined in the specification and physiologically acceptable salts and solvates thereof.The compounds have a selective stimulant action at .beta..sub.2 -adrenoreceptors and may be used, inter alia, in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: January 10, 1986Date of Patent: March 8, 1988Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Harry Finch, Alan Naylor, Lawrence H. C. Lunts, Ian B. Campbell
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Patent number: 4686233Abstract: Pesticidal water-soluble aminoacid sulfenylated carbamates useful as broad spectrum insecticides and miticides, particularly useful as systemic insecticides.Type: GrantFiled: May 1, 1986Date of Patent: August 11, 1987Assignee: Union Carbide CorporationInventors: Chennupati K. Rao, Themistocles D. D'Silva
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Patent number: 4686232Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly strains thereof which are resistant to benzimidazole or thiophanate fungicides and/or cyclic imide fungicides.Type: GrantFiled: February 6, 1984Date of Patent: August 11, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Mitsuru Sasaki, Hiroshi Noguchi, Toshiro Kato
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Patent number: 4684664Abstract: Disclosed herein are derivatives of .beta.-(4-isocyano-1,2,3,4-diepoxycyclopentyl)acrylic acid, the derivatives showing an antibacterial activity, an antifungal activity and an antimycoplasmal activity.Type: GrantFiled: January 16, 1985Date of Patent: August 4, 1987Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Katsuhisa Osugi, Isao Ichinose, Eisaku Takahashi, Masato Arahira
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Patent number: 4681889Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently --H or lower alkoxy;R.sub.3 and R.sub.4 are each independently lower alkyl; andR.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--and pharmaceutically acceptable acid addition salts thereof are calcium channel blockers useful for treating cardiovascular disorders including angina, hypertension and congestive heart failure.Type: GrantFiled: June 27, 1986Date of Patent: July 21, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Robin Clark, Joseph M. Muchowski, Fang-Ting Chiu, John O. Gardner, Jacob Berger
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Patent number: 4678811Abstract: New substituted benzyl-type ethers of formula I ##STR1## in which R.sub.1 is aryl or aryl substituted by C.sub.1-4 -alkyl, halo-C.sub.1-4 -alkyl, phenyl-C.sub.1-4 -alkyl, C.sub.2-4 -alkenyl, halo-C.sub.2-4 -alkenyl, phenyl-C.sub.2-4 -alkenyl, C.sub.2-4 -alkynyl, halo-C.sub.2-4 -alkynyl, phenyl-C.sub.2-4 -alkynyl, C.sub.1-4 -alkoxy, halo-C.sub.1-4 -alkoxy, phenyl-C.sub.1-4 -alkoxy, C.sub.2-4 -alkenyloxy, halo-C.sub.2-4 -alkenyloxy, phenyl-C.sub.2-4 -alkenyloxy, C.sub.2-4 -alkynyloxy, halo-C.sub.2-4 -alkynyloxy, phenyl-C.sub.2-4 -alkynyloxy, alkylsulfonyloxy, haloalkylsulfonyloxy, arylsulfonyloxy, halo, cyano, nitro, aryloxy, haloaryloxy, C.sub.1-4 -alkyl-aryloxy, or nitroaryloxy,R.sub.2 is hydrogen or C.sub.1-4 alkyl,R.sub.3 is hydrogen, cyano or ethynyl,R.sub.4 is phenyl or pyridyl or one of these groups substituted by one or more of C.sub.1-6 -alkyl, halo-C.sub.1-6 -alkyl, phenyl-C.sub.1-6 -alkyl, C.sub.1-6 -alkyl interrupted by an O--, N-- or S-- atom, C.sub.2-4 -alkenyl, halo-C.sub.2-4 -alkenyl, phenyl-C.Type: GrantFiled: October 17, 1985Date of Patent: July 7, 1987Assignee: Schering AktiengesellschaftInventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien
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Patent number: 4667038Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 and each independently --H or lower alkoxy; R.sub.3 and R.sub.4 are each independently lower alkyl; and R.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--, and pharmaceutically acceptable acid addition salts thereof are prepared by cyclizing, deoxygenating, coupling, or hydrogenating the intermediates disclosed herein.Type: GrantFiled: September 22, 1986Date of Patent: May 19, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Robin Clark, Joseph M. Muchowski, Fang-Ting Chiu, John O. Gardner, Jacob Berger
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Patent number: 4634701Abstract: Compounds of formula (I): ##STR1## wherein: A represents a CH-NO.sub.2 group or a N-CN group;B represents CH.sub.2, O, S or a direct bond;R represents a bicyclic or polycyclic residue, variously substituted and functionalized;R.sup.1 and R.sup.2, which may be the same or different, are hydrogen or C.sub.1 -C.sub.4 alkyl groups; andn and m, which may be the same or different, are 0, 1, 2, 3 or 4;are valuable pharmacological agents.Type: GrantFiled: May 28, 1985Date of Patent: January 6, 1987Assignee: Ausonia Farmaceutici s.r.l.Inventor: Leonardo De Vincentiis
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Patent number: 4616035Abstract: Combating pests such as insects, arachnids and nematodes with novel N-oxalyl-N-methylcarbamic acid esters of the formula ##STR1## in which R represents alkyl, alkenyl, alkinyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenalkylthio, halogen, nitro, dialkylamino, alkylsulphinyl, alkylsulphonyl, cycloalkyl or a saturated, optionally substituted heterocyclic radical with one or more hetero-atoms from the group comprising O, S and N, or forms a ring which is fused onto the phenyl radical, optionally contains one or more hetero-atoms from the group comprising O, S and N and is optionally substituted.Type: GrantFiled: October 15, 1984Date of Patent: October 7, 1986Assignee: Bayer AktiengesellschaftInventors: Gerhard Heywang, Engelbert Kuhle, Bernhard Homeyer
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Patent number: 4613606Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently --H or lower alkoxy;R.sub.3 and R.sub.4 are each independently lower alkyl; andR.sub.5 and R.sub.6 are each --OCH.sub.3, or together form --OCH.sub.2 O-- or --OCH.sub.2 CH.sub.2 O--and pharmaceutically acceptable acid addition salts thereof are calcium channel blockers useful for treating cardiovascular disorders including angina, hypertension and congestive heart failure.Type: GrantFiled: December 2, 1985Date of Patent: September 23, 1986Assignee: Syntex (U.S.A.) Inc.Inventors: Robin Clark, Joseph M. Muchowski, Fang-Ting Chiu, John O. Gardner, Jacob Berger
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Patent number: 4605667Abstract: Pesticidal water-soluble aminoacid sulfenylated carbamates useful as broad spectrum insecticides and miticides, particularly useful as systemic insecticides.Type: GrantFiled: March 29, 1985Date of Patent: August 12, 1986Assignee: Union Carbide CorporationInventors: Chennupati K. Rao, Themistocles D. D'Silva
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Patent number: 4567053Abstract: The sweetness of an ingestible product containing a sweetening sugar or sugar alcohol in large quantities can be reduced by incorporating therein a sweetness-reducing amount of at least one compound of the general formula: ##STR1## in which m represents 0 or 1, and when m represents 0, n represents 1, 2 or 3, and p represents 1, 2, 3 or 4, and when m represents 1, n represents 1 or 2 and p represents 0, 1, 2, 3 or 4; the substituents R, which may be the same or different, each represent a lower alkoxy group, e.g. with 1 to 5 carbon atoms, phenoxy group or a lower alkyl or trifluoromethyl group; and/or two substituents R together represent an aliphatic chain linked to the phenyl ring at two positions, either directly or via an oxa-group, e.g. an alkylenedioxy, alkenylenedioxy, alkylenoxy or alkenylenoxy group; and/or one substituent R represents a hydroxy group while at least one other substituent R represents an alkoxy group; and X.sup.+ represents a physiologically acceptable cation.Type: GrantFiled: April 11, 1984Date of Patent: January 28, 1986Assignee: Tate & Lyle Public Limited CompanyInventor: Michael G. Lindley
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Patent number: 4558129Abstract: Novel compounds of the general formula: ##STR1## and the pharmaceutically acceptable esters and acid addition salts thereof, wherein:R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are each independently hydrogen, lower alkyl, lower alkoxy, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl, lower alkyl sulfonyl; orR.sup.2 and R.sup.3 together form --OCH.sub.2 O--; andR.sup.10 and R.sup.11 are each independently hydrogen or lower alkyl.These compounds combine .beta.-blockade and calcium entry blockade properties in the same compound and therefore are useful in therapy in the treatment of cardiovascular diseases, including hypertension, arrhythmias and variant and exercise induced angina.Type: GrantFiled: May 18, 1983Date of Patent: December 10, 1985Assignee: Syntex (U.S.A.) Inc.Inventors: Arthur F. Kluge, Robin D. Clark, Arthur M. Strosberg
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Patent number: 4533676Abstract: A 2,5-dihalogenobenzoyl-(thio)urea of the formula ##STR1## in which X represents sulphur or oxygen,X.sup.1 and X.sup.2 are identical or different and represent fluorine, chlorine, bromine or iodine,R.sup.1 represents hydrogen, halogen, or optionally substituted radicals from the series comprising alkyl, alkoxy and alkylthio,R.sup.2 represents hydrogen, halogen, cyano, nitro or optionally substituted radicals from the series comprising alkyl, alkylthio, alkylsulphonyl, alkoxy, aryloxy, alkylcarbonyl, alkoxycarbonyl, alkoxycarbonylalkyl and alkoxycarbonylalkylthio,R.sup.1 and R.sup.2 together represent an optionally substituted alkylenedioxy radical or represent --CF.sub.2 --O--CF.sub.2 --O--,R.sup.3 represents hydrogen, halogen, or an optionally substituted alkyl, alkoxy or aryloxy radical, andR.sup.4 represents hydrogen, halogen, or optionally substituted radicals from the series comprising alkyl, alkylthio and alkoxy, with the exception of those cases in which X represents oxygen, X.sup.1 and X.sup.Type: GrantFiled: April 22, 1983Date of Patent: August 6, 1985Assignee: Bayer AktiengesellschaftInventors: Wilhelm Sirrenberg, Erich Klauke, Ingeborg Hammann
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Patent number: 4521539Abstract: Tetrahydrofuranyl substituted ethers are provided having the structural formula ##STR1## wherein A is (CH.sub.2).sub.2, CH.dbd.CH or a single bond, m is 1 to 5, B is a single bond or CH.dbd.CH, n is 1 to 4, X is O or ##STR2## wherein n' is 0, 1 or 2, R is H, lower alkyl or alkali metal and R.sup.1 is lower alkyl, arylalkyl, aryl, cycloalkyl, cycloalkylalkyl or lower alkenyl and including all stereoisomers thereof.The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease and as antiinflammatory agents and analgesics.Type: GrantFiled: May 10, 1984Date of Patent: June 4, 1985Assignee: E. R. Squibb & Sons, Inc.Inventor: Jagabandhu Das
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Patent number: 4503062Abstract: This invention relates to novel alicyclic alcohol compounds of the formula ##STR1## wherein Az is imidazole or 1,2,4-triazole, R.sup.6 is optionally substituted phenyl and A is an alicyclic ring optionally benzo-fused, which compounds possess pharmaceutical, veterinary, agricultural and horticultural antifungal properties; together with a process for their manufacture, compositions containing them, and a method of combatting plant fungal diseases.Type: GrantFiled: March 28, 1983Date of Patent: March 5, 1985Assignee: Imperial Chemical Industries PLCInventor: Michael B. Gravestock
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Patent number: 4497740Abstract: New 2-acylaminomethyl-1H-2,3-dihydro-1,4-benzodiazepine compounds are described having the general formula I ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl or alkenyl radical or the cyclopropylmethyl radical, R.sub.2 is a hydrogen atom, or a lower alkyl or alkenyl radical, n is 0, 1 or 2, R.sub.3 is an optionally substituted furyl, thienyl, pyrrolyl, pyridyl or phenyl radical, R.sub.4 is an optionally substituted furyl, thienyl, pyrrolyl or pyridyl radical, R.sub.5 is a hydrogen or halogen atom, or a lower alkyl, lower alkoxy, hydroxyl, lower alkylthio, nitro, trifluoromethyl, cyano, amino, lower mono- or dialkylamino, lower monoalkanoylamino, lower N-alkyl-N-alkanoylamino or lower alkanoyloxy radical, and R.sub.6 is a hydrogen atom, or a lower alkyl or lower alkoxy radical or R.sub.5 and R.sub.6 together denote a methylenedioxy or ethylenedioxy radical. The compounds have pharmacological, for example, analgesic, properties.Type: GrantFiled: June 8, 1982Date of Patent: February 5, 1985Assignee: Kali-Chemie Pharma GmbHInventors: Horst Zeugner, Dietmar Romer, Hans Liepmann, Wolfgang Milkowski
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Patent number: 4486447Abstract: Bis-sulfenylated bis-carbamate compounds exhibit activity against insect and mite pests.Type: GrantFiled: June 24, 1983Date of Patent: December 4, 1984Assignee: Union Carbide CorporationInventor: Themistocles D. J. D'Silva
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Patent number: 4459304Abstract: 2-Anilino-3,5-dinitro-benzotrifluorides of the formula ##STR1## in which X is O, S, SO or SO.sub.2,n is 1, 2, 3 or 4,R.sup.1 is haloalkyl, haloalkoxyalkyl, phenyl, halophenyl, haloalkylphenyl, haloalkoxyphenyl, haloalkylmercaptophenyl or haloalkylsulphonyl, andR.sup.2 each independently is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl or haloalkoxyalkyl, orXR.sup.1 and R.sup.2, when in the ortho-position relative to one another, together with the two adjacent carbon atoms of the phenyl nucleus, form an optionally halogen-substituted dioxanyl ring, orprovided X represents S, SO or SO.sub.2, R.sup.1 can represent unsubstituted alkyl in addition to the aforementioned radicals,which possess arthropodicidal, nematicidal, fungicidal and bactericidal properties.Type: GrantFiled: March 28, 1979Date of Patent: July 10, 1984Assignee: Bayer AktiengesellschaftInventors: Alfons Hartmann, Erich Klauke, Ingeborg Hammann, Peter Roessler, Volker Paul
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.OMEGA.-Cyano-1, .OMEGA.-diphenyl-azaalkane derivatives, their preparation and drugs containing them
Patent number: 4438131Abstract: .omega.-Cyano-1,.omega.-diphenyl-azaalkane derivatives of the formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, m and n have the meanings given in the description, and salts thereof with physiologically tolerated acids, are useful in treating cardiovascular disorders.Type: GrantFiled: March 30, 1982Date of Patent: March 20, 1984Assignee: BASF AktiengesellschaftInventors: Oskar Ehrmann, Manfred Raschack, Josef Gries, Rolf Kretzschmar, Hans D. Lehmann, Ludwig Friedrich, Dirk Wuppermann, Frank Zimmermann, Werner Seitz, Hans J. Treiber, Ferdinand Dengel, Wolfram Frank, Hans-Georg Kurbjuweit, Claus D. Mueller -
Patent number: 4435394Abstract: 3-Sulfonamido-benzophenonimine derivatives useful for prophylactically or therapeutically treating patients suffering from viral infections are provided from 3-sulfonamido-benzophenones.Type: GrantFiled: December 17, 1981Date of Patent: March 6, 1984Assignee: Shionogi & Co., Ltd.Inventors: Masaru Ogata, Kosaburo Sato
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Patent number: 4432784Abstract: N-Heterocyclylmethyl amides of formula (I): ##STR1## wherein R.sup.1 is optionally substituted alkyl, alkenyl, aryl, or heterocyclyl; R.sup.2 is hydrogen, C.sub.1-4 alkyl, or C.sub.3-4 alkenyl. E is CN, CSNH.sub.2, alkoxycarbonyl, or --CONR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are H or optionally substituted alkyl or alkenyl; X is oxygen or sulphur; and R.sup.3 is H, or one or more Me or Cl. The compounds are useful as herbicides and fungicides.Type: GrantFiled: March 10, 1982Date of Patent: February 21, 1984Assignee: Imperial Chemical Industries PLCInventors: Ian T. Kay, Robert A. Noon
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Patent number: 4426385Abstract: Novel bicyclooxyphenyl ureas, such as 1-(bicyclooxyphenyl)-benzoyl ureas, are provided which exhibit pesticidal activity. The compositions are conveniently prepared by reacting an isocyanate with either an amide or a bicyclooxyaniline.Type: GrantFiled: September 28, 1981Date of Patent: January 17, 1984Assignee: Union Carbide CorporationInventor: Paul A. Cain
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Patent number: 4397864Abstract: The present invention relates to 2-arylpropyl ether or thioether derivatives represented by the following general formula [I]: ##STR1## wherein Ar stands for an aryl group, R stands for a methyl or ethyl group, Y stands for an oxygen or sulfur atom, and B stands for a group represented by the following formula [II]: ##STR2## or the following general formula [III]: ##STR3## wherein Z stands for an oxygen or sulfur atom or a carbonyl or methylene group, R.sup.1 stands for a hydrogen or halogen atom or a lower alkyl group or a lower alkoxy group, and n is an integer of from 1 to 5 with the proviso that when n is 2 or more, the groups R.sup.1 may be the same or different, and also to processes for the preparation or these ethers of thioethers and a use of these ethers or thioethers.These compounds of the present invention have excellent insecticidal and acaricidal activities while the toxicity of these compounds are very low.Type: GrantFiled: April 14, 1981Date of Patent: August 9, 1983Assignee: Mitsuitoatsu Chemicals Inc.Inventors: Kiyoshi Nakatani, Satoshi Numata, Tsuneo Inoue, Kenji Kodaka, Tsutomu Ishii, Teruhiko Toyama, Hajime Tachibana, Takatoshi Udagawa, Masatoshi Gohbara