Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazole Ring Patents (Class 548/200)
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Patent number: 4889953Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.Type: GrantFiled: July 22, 1987Date of Patent: December 26, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
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Patent number: 4879295Abstract: Compounds of the formula: ##STR1## wherein A is a C.sub.1-6 alkyl group, an aryl group which is unsubstituted or substituted with at least one substituent selected from hydroxy, alkoxy, aryl-(C.sub.1-6)alkoxy, C.sub.1-6 alkylcarbonyloxy, halo-(C.sub.1-6)alkyl, halogen, nitro and amino,or 5- or 6-membered heterocyclic group containing at least one hetero atom selected from oxygen, nitrogen and sulfur, or a condensed heterocyclic group consisting of a heterocycle as defined above and a benzene nucleus,these two heterocyclic groups being unsubstituted or substituted with at least one substituent selected from hydroxy, C.sub.1-6 alkyl and halogen, and R is hydrogen or a C.sub.1-6 alkyl group,or a pharmaceutically acceptable salt thereof are nobel and useful as antiallergic.Type: GrantFiled: September 17, 1987Date of Patent: November 7, 1989Assignee: Sawai Pharmaceutical Co., Ltd.Inventors: Junji Yoshinaga, Takeshi Shoyaki, Takao Kakita, Hiromi Ozeki, Nobuko Sugimoto, Yoshiko Kato
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Patent number: 4877802Abstract: The invention provides thiazole derivatives of general formula I; ##STR1## or an acid-addition salt or metal salt complex thereof, in which R represents an optionally substituted aryl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl or alkynyl group; R.sup.2 represents a hydrogen or halogen atom or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, hydroxyl, cyano, nitro, amino, alkylamino, dialkylamino or morpholine group; X represents an oxygen or sulphur atom, a carbonyl group or a group --CR.sup.4 R.sup.5 -- where R.sup.4 and R.sup.5 independently represent a hydrogen atom or an alkoxy group; Y represents an oxygen or sulphur atom; n represents an integer from 0 to 6; m is 0 or 1; and Z represents a phenyl group; processes for their preparation; compositions containing such compounds and their use as fungicides.Type: GrantFiled: May 27, 1988Date of Patent: October 31, 1989Assignee: Shell Internationale Research Maatschappij B.V.Inventors: John R. H. Wilson, Ernest Haddock
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Patent number: 4877441Abstract: A substituted carboxylic acid derivative which is fungicidally active is provided. The compound has the formula: ##STR1## wherein R.sub.1 stands for a methyl or ethyl group, A stands for ##STR2## R.sub.2 stands for a methyl, ethyl or trifluoromethyl group, R.sub.3 stands for a methyl group or a halogen or hydrogen atom, R.sub.4 stands for a fluorine or hydrogen atom, R.sub.5 stands for a methyl, nitro or trifluoromethyl group or a halogen atom, Z stands for a .dbd.CH-- group or an N atom, R.sub.6 stands for a methyl, ethyl or trifluoromethyl group and R.sub.7 stands for an amino or methyl group or a chlorine atom.Type: GrantFiled: October 18, 1988Date of Patent: October 31, 1989Assignee: Sumitomo Chemical Company Ltd.Inventors: Tatsuya Mori, Tadashi Ohsumi, Shigeo Nakamura, Kiyoto Maeda, Sumio Nishida, Hirotaka Takano
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Patent number: 4877785Abstract: Non-peptidyl compounds characterized generally as .beta.-succinamidoacyl aminodios are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: October 31, 1989Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 4863940Abstract: Certain N-acetonyl-substituted-amides of the formula: ##STR1## wherein A is a heterocycle, a phenylalkyl, a phenylalkoxy, naphthyl, cycloalkyl, alkoxyalkyl, alkyl, haloalkyl or alkenyl group; X, Y and Z are selected from the group consisting of hydrogen, halo, cyano, thiocyano, isothiocyano, methylsulfonyloxy, thio(C.sub.1 -C.sub.2) alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyloxy, thiocarbamoylthio, hydroxy, azide, trifluoromethylcarboxy, (C.sub.1 -C.sub.4)alkylcarbonyloxy, phenylcarbonyloxy, phenoxy, thiophenyl, imidazolyl or triazolyl group as described herein; R.sup.1 and R.sup.2 are each independently a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group; and compositions containing these amides are fungicidally active, particularly against phytopathogenic fungi.Type: GrantFiled: July 26, 1984Date of Patent: September 5, 1989Assignee: Rohm and HaasInventor: Ashok K. Sharma
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Patent number: 4864017Abstract: The present invention provides novel renin-inhibiting peptides of the formula X-A.sub.6 -B.sub.7 -C.sub.8 -D.sub.9 -E.sub.10 -F.sub.11 -G.sub.12 -H.sub.13 - I.sub.14 -Z, wherein the E.sub.10 -F.sub.11 moiety is a dihydroxyethylene isostere, X and Z are terminal groups, and the remaining variables are absent or are amino acid residues. Such inhibitors are useful for the control of hypertension.Type: GrantFiled: August 23, 1988Date of Patent: September 5, 1989Assignee: The Upjohn CompanyInventor: Suvit Thaisrivongs
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Patent number: 4863947Abstract: This invention relates to novel N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: August 11, 1986Date of Patent: September 5, 1989Assignee: Rohm and HaasInventor: Richard M. Jacobson
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Patent number: 4857524Abstract: In one embodiment this invention provides novel thiazolidine compounds, such as 3-[R-(-)-3-benzyloxycarbonylthiazolidine-4-carbonyl]thiazolidine corresponding to the formula: ##STR1## An invention thiazolidine compound exhibits prolyl endopeplidase inhibitory activity, and has utility as a therapeutic agent for the treatment of dementia and amnesia disorders.Type: GrantFiled: August 3, 1988Date of Patent: August 15, 1989Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Sunao Furukawa, Tadashi Yoshimoto, Yukiyoshi Ajisawa, Seiichi Ikeguchi, Yukihiko Kinoshita
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Patent number: 4857643Abstract: 2-Substituted thiazolidines compounds having formula I ##STR1## wherein X is a CH.sub.2, O or S, R is hydroxy or an acyloxy, alkyloxy, alkenyloxy or alkinyloxy group, R.sub.1 is hydrogen or a group of formula ##STR2## R.sub.2 is hydrogen or a free or esterified carboxy group, R.sub.a and R.sub.b are hydrogen or methyl, p is zero or 1, R.sub.3 is hydrogen, a C.sub.1 -C.sub.2 alkylsulphonyl group, a phenyl or p-Cl phenyl, p-methylsulphonyl group or an acyl group; are useful as mucus regulating, antitussive and antibronchospastic agents.Type: GrantFiled: November 3, 1988Date of Patent: August 15, 1989Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Carmelo A. Gandolfi, Silvano Spinelli, Odoardo Tofanetti, Raimondo Russo, Sergio Tognella
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Patent number: 4857537Abstract: A novel thiazolidine derivative of general formula: ##STR1## [wherein R represents a group of general formula:G-E-D-B-A-(wherein A represents single bond, alkylene group of from 1 to 6 carbon atom(s), alkylene group of from 2 to 6 carbon atoms, a group of general formula: ##STR2## or saturated hydrocarbon ring of from 4 to 7 carbon atoms or single heterocyclic ring.Y represents alkylene group of from 1 to 4 carbon atom(s) or alkenylene group of from 2 to 4 carbon atoms.B represents single bond or alkylene group of from 1 to 6 carbon atom(s).D represents single bond, oxygen atom, carbonyl group or a group of general formula: ##STR3## R.sup.1 represents hydrogen atom, alkyl group of from 1 to 4 carbon atom(s), phenyl group or benzyl group.E represents single bond, alkylene group of from 1 to 8 carbon atom(s) or alkylene group of from 1 to 8 carbon atom(s) substituted by phenyl group or benzyl group.Type: GrantFiled: February 23, 1988Date of Patent: August 15, 1989Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
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Patent number: 4851422Abstract: The compound represented by the formula: ##STR1## where R.sup.1 stands for amino or an organic residue bonded through nitrogen; R.sup.2 stands for carboxyl or a group derivable therefrom; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 independently stand for hydrogen or an organic residue, including the case where R.sup.5 or R.sup.6 forms a chemical bond or a ring with R.sup.7 or R.sup.8 ; X stands for hydrogen, methoxy or formylamino; or a salt thereof, produceable by the present method, exhibits excellent antimicrobial activity, and is utilized as antimicrobial agents.Type: GrantFiled: April 30, 1986Date of Patent: July 25, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Yasuhiko Kawano, Akira Morimoto, Kouichi Yoshioka
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Patent number: 4849437Abstract: Thiazolidines of formula I ##STR1## wherein R is H, C.sub.1 -C.sub.4 -alkyl, allyl or propargyl;X is O, CH.sub.2, S;R.sub.1 is C.sub.1 -C.sub.6 -linear or branched alkyl, phenyl, benzyl, or a group of formula CH.sub.2 --CH.sub.2 --O--(CH.sub.2 --CH.sub.2 --O).sub.n --Ra wherein n is zero or an integer from 1 to 3 and Ra is H, benzyl or C.sub.1 -C.sub.6 -linear or branched alkyl.Compounds I are endowed with favourable therapeutical properties for pathologies of the respiratory system.Type: GrantFiled: April 14, 1988Date of Patent: July 18, 1989Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Roberto Di Domenico, Daniele Castoldi, Silvano Spinelli, Odoardo Tofanetti, Sergio Tognella, Carmelo A. Gandolfi
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Patent number: 4840936Abstract: Compounds of formula ##STR1## in which R, R.sub.1 and Y have the meanings shown in the description, their preparation by condensing an aldehyde or a ketone with cysteine or a derivative thereof and their use in the pharmaceutical field.The compounds of formula I possess antipyretic, anti-inflammatory, mucolytic and analgesic activity together with a low capacity to cause gastric injuries.The compounds of formula I, furthermore, are particularly useful in the treatment of ischemia and reperfusion syndromes.Type: GrantFiled: July 13, 1987Date of Patent: June 20, 1989Assignee: Zambon S.p.A.Inventors: Davide Della Bella, Angelo Carenzi, Dario Chiarino, Franco Pellacini
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Patent number: 4837242Abstract: Heterocyclic derivatives represented by the following formula have excellent preventive, curative and systemic controlliing effects on various plant microbes. ##STR1## wherein R.sup.1 represents a hydrogen atom or a methyl group, A represents ##STR2## wherein R.sup.2 represents a methyl group, an ethyl group or a trifluoromethyl group, Y.sup.1 represents an amino group, a methyl group or a chlorine atom, R.sup.3 represents a methyl group or a trifluoromethyl group and Z represents a hydrogen atom, a halogen atom or a methyl group and when A represents the formula: ##STR3## X represents an oxygen atom or sulfur atom and when A represents the formula: ##STR4## X represents a sulfur atom.Type: GrantFiled: December 30, 1987Date of Patent: June 6, 1989Assignee: Sumitomo Chemical Company, LimitedInventors: Tadashi Ohsumi, Kazunori Tsushima, Sumio Nishida, Kiyoto Maeda, Tadashi Ooishi, Noritada Matsuo
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Patent number: 4835280Abstract: The present invention provides Indolines of the formula: ##STR1## ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.Type: GrantFiled: July 14, 1987Date of Patent: May 30, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Martens, Jens-Peter Holck, Herbert Berger, Bernd Muller-Beckman, Klaus Strein, Egon Roesch
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Patent number: 4826990Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## Y is ##STR3## Z is ##STR4## R.sup.1 is ##STR5## n is 0-5; R.sup.2 is hydrogen, loweralkyl, loweralkoxy, lower alkoxycarbonyl, trifluoromethyl, nitro, cyano or halo;R.sup.3 is ##STR6## W represents a bond or ##STR7## m is 1-15; R.sup.4 is hydrogen or loweralkyl;R.sup.5 is lower alkyl, monofluoroloweralkyl, difluoroloweralkyl, polyfluoroloweralkyl, perfluoroloweralkyl or ##STR8## R.sup.6 is hydrogen, lower alkyl, ##STR9## and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and as antiinflammatory agents.Type: GrantFiled: September 30, 1987Date of Patent: May 2, 1989Assignee: American Home Products CorporationInventors: John H. Musser, Reinhold H. W. Bender, Anthony F. Kreft, III
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Patent number: 4820691Abstract: Compounds of the formula ##STR1## are disclosed. These compounds interevene in the conversion of angiotensin to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.Type: GrantFiled: June 24, 1987Date of Patent: April 11, 1989Assignee: E. R. Squibb & Sons, Inc.Inventor: Dinesh V. Patel
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Patent number: 4820823Abstract: In accordance with a process of the present invention, .alpha.-keto acids of the general formula RCOCOOH wherein R is aryl, alkenyl or heterocyclic group, can be obtained through one-step carbonylation reaction of an organic halogenide of the general formula RX wherein R is the same as above and X is a halogen atom, with carbon monoxide and water in the presence of a basic compound and a palladium containing catalyst.Type: GrantFiled: February 21, 1986Date of Patent: April 11, 1989Assignee: Director-General of Agency of Industrial Science and TechnologyInventors: Masato Tanaka, Toshiaki Kobayashi, Toshiyasu Sakakura
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Patent number: 4798898Abstract: 2-Substituted thiazolidines compounds having formula I ##STR1## wherein X is a CH.sub.2, O or S, R is hydroxy or an acyloxy, alkyloxy, alkenyloxy or alkinyloxy group, R.sub.1 is hydrogen or a group of formula ##STR2## R.sub.2 is hydrogen or a free or esterified carboxy group, R.sub.a and R.sub.b are hydrogen or methyl, p is zero or 1, R.sub.3 is a C.sub.1 -C.sub.2 alkylsulphonyl group, a phenyl or p-Cl phenyl, p-methylsulphonyl group or an acyl group; are useful as mucus regulating, antitussive and antibronchospastic agents.Type: GrantFiled: July 17, 1985Date of Patent: January 17, 1989Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Carmelo A. Gandolfi, Silvano Spinelli, Odoardo Tofanetti, Raimondo Russo, Sergio Tognella
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Patent number: 4782083Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: one of R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 -polymethylene;either R.sub.3 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy and R.sub.4 is hydrogen or R.sub.3 and R.sub.4 together are a bond;R.sub.5 is hydrogen C.sub.1-6 alkyl optionally substituted by halogen hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, carboxy or amino optionally substituted by one or two independent C.sub.1-6 alkyl groups, or C.sub.2-6 alkenyl, amino optionally substituted by a C.sub.1-6 alkyl or C.sub.1-6 alkenyl group or by a C.sub.1-6 alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen, or aryl or hetroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C.sub.1-6 alkyl, C.sub.Type: GrantFiled: August 29, 1986Date of Patent: November 1, 1988Assignee: Beecham Group P.L.C.Inventors: Frederick Cassidy, Geoffrey Stemp, John M. Evans
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Patent number: 4775676Abstract: Compounds of formula I ##STR1## wherein A represents: a saturated or unsaturated acyclic residue;a saturated cyclic or heterocyclic residue;a saturated or unsaturated bicyclic residue; and R represents OH, a C.sub.1 -C.sub.4 alkoxy group or a straight or heterocycle aminoresidue; R.sub.1 represents hydrogen, an alkyl group or an aromatic or heteroaromatic residue.Compounds I are endowed with valuable therapeutic characteristics.Type: GrantFiled: November 12, 1986Date of Patent: October 4, 1988Assignee: Chiesi Farmaceutici S.p.A.Inventors: Paolo Chiesi, Vittorino Servadio
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Patent number: 4767757Abstract: Novel fungicidally active acyloxythiophene-carboxamides of the formula ##STR1##Type: GrantFiled: March 19, 1987Date of Patent: August 30, 1988Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler
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Patent number: 4766120Abstract: Tetrazole derivatives of the formula: ##STR1## wherein R.sup.1 is an optional defined substituent; A is sulfur or a lower alkylene-thio, l is 0 or 1; B is a lower alkylene; R.sup.2 is hydroxy, a lower alkoxy, or a group: ##STR2## wherein R.sup.3 and R.sup.4 are optional defined substituents, or the R.sup.3 or R.sup.4 may combine together with the nitrogen atom to which they are joined to form a defined heterocyclic group, and a pharmaceutically acceptable salt thereof, which have prophylactic or therapeutic activities against peptic and/or duodenal ulcers and also anti-inflammatory activity and are useful as an anti-ulcer or anti-inflammatory drug; processes for the preparation of the tetrazole derivatives; and pharmaceutical compositon containing said tetrazole derivatives.Type: GrantFiled: May 30, 1986Date of Patent: August 23, 1988Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Minoru Uchida, Takao Nishi, Kazuyuki Nakagawa
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Patent number: 4764522Abstract: Compounds of the formula ##STR1## wherein R is an aromatic, 5- or 6-membered heterocyclic residue, as described herein, and their pharmaceutically usable acid addition salts are described. These compounds have interesting monoamine oxidase inhibiting properties with low toxicity and can accordingly be used for the treatment of depressive states and parkinsonism.Type: GrantFiled: August 16, 1985Date of Patent: August 16, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Rene Imhof, Emilio Kyburz
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Patent number: 4761399Abstract: The compounds of formula ##STR1## wherein the group ##STR2## represents the residue of a natural amino acid selected from the group consisting of glycine, alanine, beta-alanine, phenylalanine, isoleucine, methionine, proline, aspartic acid and arginine; R represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl; and their acid-addition salts with pharmaceutically acceptable organic or inorganic acids; are useful in the preventive and curative treatment of pathologic syndromes due to the lowering of glutathione (GSH) levels.Type: GrantFiled: August 11, 1986Date of Patent: August 2, 1988Assignee: Zambon S.p.A.Inventors: Alberto Pilotto, Mario Portelli, Angelo Carenzi, Davide Della Bella
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Patent number: 4752607Abstract: Alkoxycarbonyl-substituted hydroxythiophenecarboxamides of the formula ##STR1## in which R.sup.1 represents alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl or alkinyl or represents cycloalkyl,R.sup.2 represents alkyl or optionally substituted phenyl,R.sup.3 represents alkyl, alkoxyalkyl, alkylthioalkyl, cyanoalkyl, fluoroalkyl, alkenyl, alkinyl, cycloalkyl or alkoxy andR.sup.4 represents hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl, alkinyl or cycloalkyl, orR.sup.3 and R.sup.4, together with the nitrogen atom, represent a heterocyclic radical which is optionally substituted by alkyl and can be further substituted in the alkylene chain by oxygen, sulphur or nitrogen,are useful as fungicides and intermediates.Type: GrantFiled: June 17, 1986Date of Patent: June 21, 1988Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler
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Patent number: 4742060Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.Type: GrantFiled: January 21, 1986Date of Patent: May 3, 1988Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
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Patent number: 4737494Abstract: A 1,3-dithiole derivative having the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 is a substituted or unsubstituted alkyl, cycloalkyl, lower alkenyl, lower alkynyl, aryl or aralkyl group or R.sup.1 and R.sup.2 together form a substituted or unsubstituted alkylene or alkenylene group having from 3 to 6 carbon atoms, which may contain a cycloalkylene group, an o-phenylene group or a hetero atom selected from the group consisting of an oxygen atom, a sulfur atom and a nitrogen atom which may have a substituent, and Q is an acid residue useful for the treatment of liver diseases.Type: GrantFiled: December 26, 1985Date of Patent: April 12, 1988Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Mitsuo Yano, Yoshimi Tsuchiya, Yukio Hirayama, Kyoko Nakamichi, Junji Yoshizawa
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Patent number: 4736058Abstract: A novel prostacyclins expressed by the following formula (1) ##STR1## wherein a symbol between the 2-position and 3-position indicates single bond or double bond; G indicates --CO.sub.2 R.sup.5 or --CONR.sup.6 R.sup.7 in which R.sup.5 is a hydrogen atom, C.sub.1 -C.sub.10 alkyl group, substituted or unsubstituted alicyclic group, substituted or unsubstituted phenyl (C.sub.1 -C.sub.2) alkyl group, tri (C.sub.1 -C.sub.7) hydrocarbon-silyl group, or one equivalent cation, R.sup.6 and R.sup.7 are identical or different and each representing a hydrogen atom, or C.sub.1 -C.sub.10 alkyl group, or R.sup.6 and R.sup.7 are substituted or unsubstituted five to six-membered ring which may join together with a nitrogen atom to which they are linked and further contain a hetero atom; R.sup.1 indicates a hydrogen atom, or methyl group; R.sup.2 indicates an unsubstituted C.sub.3 -C.sub.8 alkyl group substituted or unsubstituted alicyclic group, or substituted C.sub.1 -C.sub.Type: GrantFiled: September 27, 1984Date of Patent: April 5, 1988Assignee: Teijin LimitedInventors: Shiro Ikegami, Seizi Kurozumi
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Patent number: 4735957Abstract: New thiazole derivatives of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, a drivative of carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl, hydroxyiminomethyl or alkenyl which may be substituted with lower alkoxycarbonyl, pyridyl or cyano,R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkylN-acylamino, guanidino optionally substituted with dimethylaminomethylene, or ar(lower)alkylamino optionally substituted with lower alkoxy,R.sup.3 is lower alkyl, halo(lower)alkyl or N-containing unsaturated heterocyclic group which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, a derivative of carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkyl-N-acylamino, guanidino, N-oxide or ar(lower)alkylamino optionally substituted with lower alkoxy,Q is --CO--, andn is an integer of 0 or 1,provided that when both of R.sup.1 and R.sup.Type: GrantFiled: November 18, 1986Date of Patent: April 5, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Hisashi Takasugi
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Patent number: 4716237Abstract: 3-oxonitriles are produced by reaction of carboxylic acid esters with carboxylic acid nitriles in the presence of 70 to 80% suspension of sodium hydride in white oil. The oxonitrile are intermediate products for the production of 3-oxocarboxylic acid amides or esters and pesticides.Type: GrantFiled: March 15, 1983Date of Patent: December 29, 1987Assignee: Degussa AktiengesellschaftInventors: Karlheinz Drauz, Axel Kleemann, Elisabeth Wolf-Heuss
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Patent number: 4704157Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: A, B and D are selected from CH and N;E is selected from oxygen and sulfur;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkenyloxy, alkynyl, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, alkanoyloxy, benzyloxy, substituted benzyloxy, phenyl, substituted phenyl, amino, substituted amino, and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof;R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorglanic or organic cation;R.sup.2 is selected from alkyl substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl;R.sup.Type: GrantFiled: May 8, 1986Date of Patent: November 3, 1987Assignee: CI Australia Ltd.Inventors: Richard J. Conway, Keith G. Watson, Graeme J. Farquharson
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Patent number: 4686295Abstract: This invention relates to new compounds of the formula ##STR1## wherein A is a hydroxy, lower alkoxy, lower alkenoxy, diloweralkylamino lower alkoxy, acylamino lower alkoxy, acyloxy, lower alkoxy, aryloxy, arloweralkyloxy, amino, loweralkylamino, diloweralkylamino, aryloweralkylamino, hydroxyamino, or substituted aryloxy, or substituted arloweralkoxy wherein the substituent is methyl, halo or methoxy;R.sub.1, R.sub.2, and R.sub.Type: GrantFiled: March 7, 1983Date of Patent: August 11, 1987Assignee: USV Pharmaceutical CorporationInventors: Raymond D. Youssefyeh, Jerry W. Skiles, John T. Suh, Howard Jones
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Patent number: 4675330Abstract: A compound of formula I ##STR1## wherein R.sub.1 represents ethyl or vinyl andR.sub.2 represents a five membered saturated heterocycle or aminoalkyl unsubstituted or substituted in its alkyl moiety by hydroxy,in free or in the form of an acid addition or quaternary salt, which compounds are indicated for use as chemotherapeutic agents e.g. as anti-bacterially active antibiotics and as veterinary agents e.g. in combatting microorganism infections and promoting growth in domestic animals.Type: GrantFiled: May 6, 1986Date of Patent: June 23, 1987Assignee: Sandoz Ltd.Inventors: Heinz Berner, Hermann Vyplel
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Patent number: 4663341Abstract: This invention relates to N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: January 11, 1985Date of Patent: May 5, 1987Assignee: Rohm and Haas CompanyInventor: Richard M. Jacobson
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Patent number: 4649146Abstract: The invention relates to novel pharmaceutical compounds for treatment for ulcer of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl or hydroxyiminomethyl,R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino or guanidino optionally substituted with dimethylaminomethylene,R.sup.3 is dihydroisoquinolyl which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino or guanidino,Q is --CO--, andn is an integer of 0 or 1, andpharmaceutically acceptable salts thereof.Type: GrantFiled: January 27, 1984Date of Patent: March 10, 1987Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Hisashi Takasugi
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Patent number: 4639442Abstract: A class of benzocyclobutene aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: November 1, 1985Date of Patent: January 27, 1987Assignee: William H. Rorer, Inc.Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
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Patent number: 4638001Abstract: A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: April 27, 1984Date of Patent: January 20, 1987Assignee: William H. Rorer, Inc.Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
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Patent number: 4634715Abstract: There are disclosed aza analogs of carboxyalkyl dipeptide derivatives and related compounds which are useful as converting enzyme inhibitors and as antihypertensives said compounds being represented by the general formula: ##STR1## wherein A and B can be joined together to form various ring structures.Type: GrantFiled: July 27, 1983Date of Patent: January 6, 1987Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, Eugene D. Thorsett
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Patent number: 4634773Abstract: This invention relates to 2-(thiazolidin-2'-yl) ethylchlorocarbonates useful as intermediates in the synthesis of photographic image dye-providing materials and to their preparation by the reaction of the appropriate 2-(2'-hydroxyethyl)-thiazolidine with phosgene under certain conditions.Type: GrantFiled: June 10, 1985Date of Patent: January 6, 1987Assignee: Polaroid CorporationInventor: William J. Cumming
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Patent number: 4631344Abstract: Photographic products and processes for the imagewise generation of a dye from a color shifted dye precursor of a preformed image dye, said precursor having at least one ##STR1## group, wherein R is hydrogen, alkyl, provided that the .alpha.-carbon does not have a hydrogen atom attached thereto, aryl such as phenyl or substituted phenyl, e.g. p-nitrophenyl, or heterocyclic such as pyridine; R.sub.1 -R.sub.6 are hydrogen, alkyl, preferably having from 1 to 6 carbon atoms, or aryl; n is 0 or 1; and T is a moiety containing a thiazolidin-2-yl group which upon silver-assisted cleavage of said thiazolidin-2-yl group results in the formation of a ##STR2## group, which may be protonated under the reaction conditions, followed by cleavage of said ##STR3## which cleavage is anchimerically assisted or accelerated by said ##STR4## to provide after protonation, an ##STR5## group in a dye chromophore. In a preferred embodiment the precursor is a substantially colorless compound.Type: GrantFiled: April 29, 1985Date of Patent: December 23, 1986Assignee: Polaroid CorporationInventors: Myron S. Simon, David P. Waller
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Patent number: 4628101Abstract: Compounds having antidote activity and belonging to the class of the derivatives of 1,3-thiazolidine useful for protecting cultivations of agrarian interest from the toxic action of nonselective herbicides are herein described. The invention relates, also, to a method for protecting cultivations of agrarian interest from the toxic action of nonselective herbicides consisting in the use, as antidotes, of the above mentioned compounds and the compositions for agrarian use containing said compounds.Type: GrantFiled: February 28, 1986Date of Patent: December 9, 1986Assignee: Montedison S.p.A.Inventors: Giovanni Camaggi, Franco Gozzo, Ernesto Signorini, Ottorino Palla
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Patent number: 4612309Abstract: A class of bicyclic benzo-oxy heterocyclic ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastro-intestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: October 23, 1984Date of Patent: September 16, 1986Assignee: William H. Rorer, Inc.Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Kent W. Neuenschwander
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Patent number: 4600774Abstract: Cyclic sulfoperfluoroaliphaticcarboxylic acid anhydrides, amide derivatives thereof, a process for making the same, curable compositions containing cyclic sulfoperfluoroaliphaticcarboxylic acid anhydrides or amide derivatives thereof and cationically-sensitive monomers, and a process for using cyclic sulfoperfluoroaliphaticcarboxylic acid anhydrides or amide derivatives thereof as catalysts for the cure of cationically-sensitive monomers.Type: GrantFiled: June 13, 1985Date of Patent: July 15, 1986Assignee: Minnesota Mining and Manufacturing CompanyInventor: Robert J. Koshar
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Patent number: 4595764Abstract: This invention relates to photographic processes and products for forming an image in dye from a colorless precursor of a preformed image dye which is substituted with a moiety containing a thiazolidinyl group, said thiazolidinyl group (a) being capable of undergoing cleavage imagewise in the presence of an imagewise distribution of silver ion and/or soluble silver complex and (b) possessing a substituent on the carbon atom in the 2-position that undergoes a .beta.-elimination reaction upon said imagewise cleavage, which moiety maintains the precursor in its colorless form at least until said thiazolidinyl group undergoes said cleavage. In a further embodiment, an imagewise distribution of a photographically useful reagent, which reagent may be, for example, a photographically active reagent, is released as a carbamic acid by a .beta.-elimination reaction following the cleavage of a thiazolidinyl group whereby said reagent is provided with a solubilizing group at least during the initial stages of processing.Type: GrantFiled: July 23, 1984Date of Patent: June 17, 1986Assignee: Polaroid CorporationInventors: Roberta R. Arbree, James W. Foley, Frank A. Meneghini
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Patent number: 4591646Abstract: This invention relates to photographic processes and products for forming an image in dye from a colorless precursor of a preformed image dye which is substituted with a moiety containing a thiazolidinyl group, said thiazolidinyl group (a) being capable of undergoing cleavage imagewise in the presence of an imagewise distribution of silver ion and/or soluble silver complex and (b) possessing a substituent on the carbon atom in the 2-position which upon cleavage of said thiazolidinyl group, undergoes a .beta.-elimination reaction followed by an intramolecularly accelerated nucleophilic displacement reaction, which moiety maintains the precursor in its colorless form at least until said thiazolidinyl group undergoes said cleavage. In a further embodiment, this sequence of reactions is used to release an imagewise distribution of a photographically useful reagent which reagent may be, for example, a photographically active reagent.Type: GrantFiled: July 23, 1984Date of Patent: May 27, 1986Assignee: Polaroid CorporationInventors: Frank A. Meneghini, Paul S. Palumbo
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Patent number: 4591628Abstract: This invention relates to photographic processes and products for forming an image in dye from a colorless precursor of a preformed image dye which is substituted with a moiety comprising a 1,3-sulfur-nitrogen group, said 1,3-sulfur-nitrogen group (a) being capable of undergoing cleavage in the presence of silver ion and/or soluble silver complex, and (b) possessing an amide substituent on the carbon atom in the 2-position that undergoes an intramolecularly accelerated cleavage reaction following the cleavage of said 1,3-sulfur-nitrogen group, which moiety maintains said precursor in its colorless form at least until the 1,3-sulfur-nitrogen group undergoes said cleavage. In a further embodiment, the cleavage of the amide substituent following the cleavage of the 1,3-sulfur-nitrogen group is used to provide an imagewise distribution of a photographically useful reagent, which reagent may be, for example, a photographically active reagent.Type: GrantFiled: July 23, 1984Date of Patent: May 27, 1986Assignee: Polaroid CorporationInventor: James W. Foley
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Patent number: 4568684Abstract: N-substituted 2-methylnaphthylamides of the general formula I ##STR1## where R is an unsubstituted or substituted furyl, isoxazolyl, oxazolyl, isothiazolyl, thiazolyl, 1,2,4-oxadiazol-3-yl, 1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazol-5-yl, 1,2,5-thiadiazol-3-yl, 1,3,4-thiadiazol-2-yl or C.sub.1 -C.sub.5 -alkyl radical, or the group --CH.sub.2 --Y--R.sup.1, where Y is oxygen or sulfur and R.sup.1 is C.sub.1 -C.sub.6 -alkoxyethyl or C.sub.1 -C.sub.6 -alkoxyethoxyethyl, or R is C.sub.2 -C.sub.5 -alkenyl, C.sub.2 -C.sub.5 -alkynyl, C.sub.1 -C.sub.5 -alkoxy, C.sub.1 -C.sub.5 -alkoxycarbonyl or C.sub.3 -C.sub.7 -cycloalkyl, and fungicides containing these compounds.Type: GrantFiled: December 17, 1984Date of Patent: February 4, 1986Assignee: BASF AktiengesellschaftInventors: Costin Rentzea, Karl Eicken, Hans Theobald, Bernd Zeeh, Ernst-Heinrich Pommer, Eberhard Ammermann
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Patent number: 4562201Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S-- where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.Type: GrantFiled: July 26, 1982Date of Patent: December 31, 1985Assignee: American Hospital Supply CorporationInventors: David M. Stout, William L. Matier