1,2-diazole (including Hydrogenated) Patents (Class 546/211)
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Patent number: 5624941Abstract: The present invention relates to compounds of the formula: ##STR1## These compounds are useful in pharmaceuticals in which cannabis is known to be involved.Type: GrantFiled: November 29, 1994Date of Patent: April 29, 1997Assignee: SanofiInventors: Francis Barth, Pierre Casellas, Christian Congy, Serge Martinez, Murielle Rinaldi, Gilles Anne-Archard
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Patent number: 5610305Abstract: Novel pyrazole-containing compounds useful as light-stabilizers for polymers, their Ni, Zn, Cu, and Co metal complexes, and methods for the synthesis of such complexes are provided. The compounds include a hindered amine light stabilizer (HALS) such as a substituted piperidine, thereby incorporate the properties of UV absorbers and redical scavengers. The compounds are of the formulas I and II, ##STR1## where R.sub.1 is phenyl, R.sub.2 is methyl, X is oxygen or sulphur, Z is oxygen or N-aryl, and R.sub.3 is hydrogen, alkyl, a derivative of carboxyacryloyl or carboxybenzoyl or a derivative of pyrazole. The compounds and their metal complexes are highly compatible with various polymers, thermostable, and retain their photostability under conditions of continuous and intensive irradiation. Methods for the synthesis of metal complexes include the reaction of: (a) a compound with metal acetate; or (b) a metal complex with anhydride or a pyrazole derivative.Type: GrantFiled: November 22, 1995Date of Patent: March 11, 1997Assignee: UV Stab Ltd.Inventors: Idel Y. Kvitko, Jack Azran
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Patent number: 5591764Abstract: N-sulfenylated and N-acylated pyrazoline arthropodicides, compositions containing them and methods for controlling arthropods by applying compounds of the invention to them or to their environment. The pyrazolines are selected from those of Formulae I to III wherein R.sub.1, R.sub.2, R.sub.Type: GrantFiled: June 6, 1995Date of Patent: January 7, 1997Assignee: E. I. Du Pont de Nemours and CompanyInventors: Mohamed A. H. Fahmy, deceased, Charles R. Harrison, George P. Lahm, Thomas M. Stevenson
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Patent number: 5583146Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.Type: GrantFiled: January 17, 1995Date of Patent: December 10, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Spencer D. Kimball, Jagabandhu Das, Wan F. Lau, Steven E. Hall, Wen-Ching Han
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Patent number: 5580985Abstract: A class of pyrazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, alkenyl, aralkyl, alkynyl, cyanoalkyl, carboxyalkyl, aminocarbonylalkyl, arylaminocarbonylalkyl, heterocyciicalkyl, and alkoxycarbonylalkyl; wherein R.sup.3 is aryl substituted at a substitutable position with halo; wherein R.sup.4 is selected from hydrido and haloalkyl; and wherein R.sup.5 is selected from alkyl and amino; or a pharmaceutically-acceptable salt or prodrug thereof.Type: GrantFiled: September 28, 1995Date of Patent: December 3, 1996Assignee: G. D. Searle & Co.Inventors: Len F. Lee, Thomas D. Penning, Steven W. Kramer
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Patent number: 5561146Abstract: Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; andR.sup.1 is cyano, hydroxyl, alkoxy, amino, aminoalkyl or nitro.Type: GrantFiled: October 14, 1994Date of Patent: October 1, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Kyoung S. Kim, Spencer D. Kimball, Jagabandhu Das, Edwin J. Iwanowicz, Wen-Ching Han
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Patent number: 5556987Abstract: A process for producing a pyrazolecarboxamide derivative represented by formula (C) which comprises reacting a pyrazolecarboxylic ester compound represented by formula (A) with an amine compound represented by formula (B) in the presence of a Lewis acid: ##STR1## wherein R.sup.1 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group; R.sup.2 represents a substituted or unsubstituted alkyl group; and R.sup.3 and R.sup.4 each represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, provided that R.sup.3 and R.sup.4 may be bonded to each other to form a ring.Type: GrantFiled: October 25, 1995Date of Patent: September 17, 1996Assignee: Fuji Photo Film Co., Ltd.Inventors: Mario Aoki, Akira Ogawa
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Patent number: 5543529Abstract: Pyrazole compounds represented by formulae (A), (B), and (C): ##STR1## wherein R.sub.1 represents an unsubstituted alkyl group, an ester group, a carboxyl group, an amino group or an aryl group; R.sub.2 and R.sub.3 each represents an alkyl group or an aryl group, and the alkyl groups represented by R.sub.2 and R.sub.3 may bond each other to form a saturated 5- or 6-membered ring; R.sub.4 represents an alkoxy group or a carbonamido group; R.sub.5 and R.sub.6 each represents a hydrogen atom, an alkyl group or an aryl group, and the alkyl groups represented by R.sub.5 and R.sub.6 may bond each other to form a saturated 5- or 6-membered ring; R.sub.7 represents an aryl group, an ester group or a carboxyl group; and M represents a hydrogen atom or a monovalent cation.Type: GrantFiled: January 26, 1995Date of Patent: August 6, 1996Assignee: Fuji Photo Film Co., Ltd.Inventors: Koji Wariishi, Mario Aoki
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Patent number: 5475017Abstract: Compounds of formula I ##STR1## and compounds of formula Ia ##STR2## and their physiologically tolerated salts, processes for their preparation and drugs and cosmetics prepared therefrom.Type: GrantFiled: May 13, 1994Date of Patent: December 12, 1995Assignee: BASF AktiengesellschaftInventors: Hans-Heiner Wuest, Bernd Janssen, William V. Murray, Michael P. Wachter, Stanley Bell
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Patent number: 5405829Type: GrantFiled: June 13, 1994Date of Patent: April 11, 1995Assignee: Schering AktiengesellschaftInventors: Uwe Hartfiel, Gabriele Dorfmeister, Helga Franke, Jens Geisler, Gerhard Johann, Richard Rees
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Patent number: 5380744Abstract: Disclosed are a phenoxyalkylamine compound represented by the formula (I): ##STR1## wherein R.sup.1 is C.sub.1-8 alkyl group, C.sub.3-8 cycloalkyl group, a hydrogen atom, a phenyl group, or C.sub.1-4 haloalkyl group; R.sup.2 is a halogen atom, a hydrogen atom, C.sub.1-4 alkyl group, C.sub.1-4 alkoxy group or a nitro group; R.sup.1 and R.sup.2 may be linked with each other and condensed to a pyrazole ring to form a saturated 4- to 8-membered ring; R.sup.3 is C.sub.1-15 alkyl group, C.sub.3-8 cycloalkyl group, a phenyl group, C.sub.1-4 haloalkyl group, C.sub.2-8 alkoxyalkyl group, C.sub.3-6 alkenyl group, a pyridyl group, a benzyl group, C.sub.3-8 alkoxycarbonylalkyl group, a pyrazole group, or C.sub.1-4 alkoxy group; R.sup.4 is C.sub.1-4 alkyl group, a hydrogen atom or a halogen atom; R.sup.5 is C.sub.1-20 alkyl group, a hydrogen atom, C.sub.3-6 alkenyl group, a benzyl group, a phenoxy group, a halogen atom, a cyanomethyl group or --A--O--R.sup.7 where A is C.sub.1-4 alkylene group and R.sup.7 is C.sub.Type: GrantFiled: April 1, 1994Date of Patent: January 10, 1995Assignee: Ube Industries, Ltd.Inventors: Tokio Obata, Akira Ooka, Katsutoshi Fujii, Shin Suizu
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Patent number: 5371091Abstract: Sulfonamide thrombin inhibitors are provided which have the structure ##STR1## including all stereoisomers thereof, wherein n is 1, 2 or 3; m is 0, 1 or 2; R.sup.1 and R.sup.2 are independently H, lower alkyl, cycloalkyl, aryl, heteroaryl or heteroaryl-alkyl, or R.sup.1 and R.sup.2 can be taken together with the N atom to which they are attached to form a 4- to 8-membered ring; R.sup.3 is monocyclic heteroaryl; and R.sup.4 is alkyl, cycloalkyl, aryl, heteroaryl, quinolinyl or tetrahydroquinolinyl, and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 14, 1993Date of Patent: December 6, 1994Assignee: Bristol-Myers Squibb CompanyInventors: Raj N. Misra, Steven E. Hall
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Patent number: 5328916Abstract: New heterocyclic compounds of the formulaX--W--CR.sup.1 R.sup.2 --CO--Y--NR.sup.3 --CHR.sup.4 --CR.sup.5 --CH.sub.2 --(CR.sup.6 R.sup.7).sub.r --Z--Het Iin which R.sup.1 to R.sup.7, W, X, Y, Z, r and Het have the meanings defined herein, and the salts thereof, inhibit the activity of human plasma renin.Type: GrantFiled: May 2, 1991Date of Patent: July 12, 1994Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Peter Raddatz, Claus J. Schmitges, Klaus-Otto Minck
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Patent number: 5290796Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein R.sup.1 is lower-alkyl, or phenyl-lower-alkyl;R.sup.2, R.sup.3 and R.sup.4 are the same or different lower-alkyl;n is zero or one;R.sup.5 is hydrogen, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, lower-alkoxy, phenyl, phenyl-lower-alkyl, phenyl-lower-alkyl in which the phenyl ring is substituted in the 2, 3, or 4-position by one to two, the same or different, halogen substituents, or R.sup.5 is a 5-membered aromatic monocyclic heterocycle selected from the group consisting of thienyl, furanyl and isoxazolyl;R.sup.6 is hydrogen or lower-alkyl; or when n is zero, R.sup.5 and R.sup.6 together are --(CH.sub.2).sub.m -- wherein m is an integer from four to six; with the proviso that when R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are methyl, n is zero and R.sup.6 is hydrogen or methyl, R.sup.5 cannot be hydrogen; further provided that when n is zero, R.sup.Type: GrantFiled: November 20, 1992Date of Patent: March 1, 1994Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
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Patent number: 5286733Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein: R.sup.1 is hydrogen, lower-alkyl, phenyl-lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl-lower-alkyl, or hydroxy-C.sub.3 -C.sub.7 -monocycliccycloalkyl-lower-alkyl;R.sup.2 is lower-alkyl;R.sup.3 is hydrogen or lower-alkyl;R.sup.4 is lower-alkyl;n is an integer from zero to three; andR.sup.5 is hydroxy, lower-alkoxy, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, phenyl, or a 5-membered heterocycle selected from furanyl, thienyl and isoxazolyl;with the proviso that when n is zero, R.sup.5 is other than hydroxy or a pharmaceutically acceptable acid-addition salt thereof.Type: GrantFiled: November 20, 1992Date of Patent: February 15, 1994Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
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Patent number: 5250532Abstract: 3,4,N-triaryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds having an aryl moiety in the 4-position that is an optionally substituted pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or quinolinyl moiety and aryl moieties in the 3-position and the N-position that are optionally substituted phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or quinolinyl moieties, such as N-(4-chlorophenyl)-4,5- -dihydro-3-(4-fluorophenyl)-4-(5-trifluoromethyl-2- -pyridinyl)-1H-pyrazole-1-carboxamide, were prepared and found to possess insecticidal utility. 1,2-Diarylethanone compounds were converted to 1,2-diaryl-2-propen-1-one compounds by treatment with bis(dimethylamino)methane, the 1,2-diaryl-2-propen-1-one compounds were converted to 3,4-diaryl-4,5-dihydro-1H-pyrazole compounds by treatment with hydrazine, and the 3,4-diaryl-4,5-dihydro-1H-pyrazole compounds were converted to the insecticidal subject compounds by treatment with an aryl isocyanate.Type: GrantFiled: February 27, 1992Date of Patent: October 5, 1993Assignee: DowElancoInventors: Kevin L. McLaren, Mark B. Hertlein, James T. Pechacek, Michael J. Ricks, Yulan C. Tong, Laura L. Karr
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Patent number: 5235058Abstract: There is disclosed a 3(5)-hydrazinopyrazole compound represented by the following formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an aryl group, a heterocyclic group, a hydroxyl group, an alkoxy group, or an aryloxy group, R.sub.2 represents a hydrogen atom or an acyl group, X represents an aryloxy group, an alkoxy group, a heterocyclic oxy group, or an azolyl group, M represents a hydrogen ion or a metal ion, Y represents an acid radical, and n is 0 or a positive number.Type: GrantFiled: September 17, 1991Date of Patent: August 10, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Tadahisa Sato, Keizo Kumura
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Patent number: 5225548Abstract: Indophenol dyes of the formula ##STR1## where X is nitrogen or the radical CH,Q is a five-membered heterocyclic radical, andK is a radical of an aniline, aminonaphthalene, aminoquinoline or aminothiazole derivative, andthe radical A can be benzofused,are useful for thermal transfer processes.Type: GrantFiled: September 20, 1991Date of Patent: July 6, 1993Assignee: BASF AktiengesellschaftInventors: Volker Bach, Karl-Heinz Etzbach, Ruediger Sens
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Patent number: 5206259Abstract: The present invention relates to certain novel amide compound represented by the formula of ##STR1## wherein A, X, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and l are the same as defined in the present specification, an insecticidal and/or acaricidal composition containing it as an active ingredient, and a method for exterminating insects and/or acarids which comprises applying it as an active ingredient.Type: GrantFiled: October 16, 1991Date of Patent: April 27, 1993Assignee: Sumitomo Chemical Company, LimitedInventors: Akira Shuto, Hirosi Kisida, Naoto Meki, Tomotoshi Imahase, Hiroaki Fujimoto, Kimitoshi Umeda
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Patent number: 5204359Abstract: Insecticidally active nitro compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, cyano or alkyl,R.sup.2 is hydrogen or an organic radical,R.sup.3 is ##STR2## R.sup.4 is an organic radical, R.sup.5 and R.sup.6 are hydrogen or organic radicals,Y is CH or N, andZ is an optionally substituted 5- or 6-membered heterocyclic group,with certain conditions and exceptions.Type: GrantFiled: September 11, 1991Date of Patent: April 20, 1993Assignee: Nihon Bayer Agrochem K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Koichi Moriya, Yumi Hattori, Ikuro Honda, Katsuhiko Shibuya
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Patent number: 5194606Abstract: Novel aminoketones useful as central muscle relaxants and their preparation processes are disclosed. The disclosed processes are novel processes which do not use any heavy metal in view of the facts that their products are will be used as drugs and which require no complex purification step such as liberation of the aminoketones from their hydrochlorides or the like.Type: GrantFiled: July 23, 1991Date of Patent: March 16, 1993Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Akira Matsubara, Kazuya Sakai, Hideki Tanada, Hironori Komatsu
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Patent number: 5169856Abstract: The present invention relates to unsaturated carboxylic acid amide derivatives of the formula ##STR1## wherein ring A stands for an optionally substituted aromatic ring; R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon residue or forms an optionally substituted carbocyclic ring with the adjacent group --CH.dbd.C-- together with two carbon atoms constituting the ring A; R.sup.2 stands for a hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group; R.sup.3 stands for an optionally substituted hydrocarbon residue; and n denotes an integer ranging from 2 to 6, and salts thereof, as well as the production thereof.The compounds of the present invention act on the central nervous system of mammals and has a strong anti-cholinesterase activity, which can be used for the prophylaxis and therapy of, for example, senile dementia, Alzheimer's diseases, Huntington's chorea, et., and are useful as medicines.Type: GrantFiled: February 6, 1989Date of Patent: December 8, 1992Assignee: Takeda Chemical Industries, Inc.Inventors: Giichi Goto, Akinobu Nagaoka
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Patent number: 5162528Abstract: The invention relates to the use of partly known substituted pyrazolin-5-one derivatives of the formula (I) ##STR1## as herbicides and fungicides, new substituted pyrazolin-5-one derivatives and processes for their preparation.Type: GrantFiled: February 4, 1991Date of Patent: November 10, 1992Assignee: Bayer AktiengesellschaftInventors: Reinhold Gehring, Markus Lindig, Heinz-Jurgen Wroblowsky, Hans-Joachim Santel, Robert R. Schmidt, Wilhelm Brandes, Robert H. Strang
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Patent number: 5152824Abstract: A sulfamidosulfonamide derivative of the formula (1) and an agriculturally suitable salt thereof: ##STR1## wherein Q is ##STR2## X is an oxygen atom or a sulfur atom; and G is ##STR3## which are useful as herbicide.Type: GrantFiled: March 6, 1991Date of Patent: October 6, 1992Assignee: Nissan Chemical Industries Ltd.Inventors: Kenzi Makino, Katsushi Morimoto, Shigeaki Akiyama, Hideaki Suzuki, Takeshi Nagaoka, Koichi Suzuki, Tsutomu Nawamaki, Shigeomi Watanabe
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Patent number: 5145967Abstract: The present invention is directed to a method for preparing a 4-alkoxyalkyl-4-phenylaminopiperidine compound which comprises the steps of (a) reacting an N-substituted-4-piperidone compound with an aniline compound to form a Schiff base compound, (b) reacting the Schiff base compound with an anionic reagent having an anion stabilizing group to form an amine compound, and (c) reducing the amine compound in step (b) with a reducing agent to displace the anion stabilizing group.The anionic reagent in step (b) above has the general formula:X--CYM--Zwherein X is an anion stabilizing group, Y is hydrogen or lower-alkyl, Z is lower-alkoxy or phenylmethoxy, M is an alkali or alkaline earth metal, and C is a carbon atom.Type: GrantFiled: November 2, 1990Date of Patent: September 8, 1992Assignee: Anaquest, Inc.Inventors: Bor-Sheng Lin, H. Kenneth Spencer, Joseph W. Scheblein
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Patent number: 5118685Abstract: Aminopropanol derivatives of the formula: ##STR1## where R.sup.1 and R.sup.2 are identical or different and are each hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl or hydroxyalkyl, each of not more than 6 carbon atoms, alkoxyalkyl, alkylthioalkyl or dialkylaminoalkyl, each of not more than 9 carbon atoms in total, or phenylalkyl or phenoxyalkyl where the alkyl radical is of not more than 6 carbon atoms and the phenyl radical is unsubstituted or substituted by alkyl or alkoxy, each of not more than 3 carbon atoms, or R.sup.1 and R.sup.2, together with the nitrogen atom which links them, form a 5-membered to 7-membered saturated heterocyclic ring which can be substituted by one or two phenyl and/or hydroxyl radicals and can contain an oxygen or nitrogen atom, as a further heteroatom in the ring, and such an additional nitrogen atom can be substituted by alkyl of 1 to 3 carbon atoms or by phenyl, and -- .circle.Type: GrantFiled: December 3, 1984Date of Patent: June 2, 1992Assignee: BASF AktiengesellschaftInventors: Albrecht Franke, Wolfgang Spiegler, Hardo Siegel, Claus D. Mueller, Gerda von Philipsborn, Dieter Lenke, Josef Gries
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Patent number: 5116835Abstract: Enzyme-inhibiting urea derivatives of dipeptides, a process for the preparation thereof, agents containing these, and the use thereof.The present invention relates to compounds of the formula I ##STR1## in which A and B denote, indpendently of one another, an amino acid,X as desired can be absent or represents --O--, --S--, --CF.sub.2 --, --CO-- or --CHR.sup.8,p and q denote, independently of one another, 0, 1, 2, 3 or 4, andR.sup.1 to R.sup.4 are defined in the description, as well as the salts thereof.The invention furthermore relates to a process for the preparation of the compounds of the formula I and to the use thereof as medicines.Type: GrantFiled: December 7, 1989Date of Patent: May 26, 1992Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Ruger, Hansjorg Urbach, Dieter Ruppert, Bernward Scholkens
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Patent number: 5110585Abstract: The invention relates primarily to quaternized polycyclic compounds having the formula ##STR1## wherein m is an integer having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; R.sub.2 together with the quaternary nitrogen, forms a 5 to 14 membered heterocyclic ring, said ring containing at least 2 hetero atoms selected from the group of nitrogen, sulfur and oxygen; R.sub.1 forms a double bond in the heterocyclic ring of the quaternized nitrogen or is alkyl, alkyleneoxyalkyl, alkylhydroxy, aryl, aralkyl, aralkenyl, alkaryl, alkylamidoalkyl and X.sup.- is an anion. The invention also relates to the preparation and use of said quaternized polycyclic compounds.Type: GrantFiled: March 1, 1989Date of Patent: May 5, 1992Assignee: ISP Investments Inc.Inventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login, Michael W. Helioff
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Patent number: 5091405Abstract: Pyrazolines and their intermediates, including all geometric and stereoisomers of the pyrazolines and intermediates, agricultural compositions containing the pyrazolines, and methods for use as insecticides.Type: GrantFiled: May 12, 1989Date of Patent: February 25, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thomas M. Stevenson
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Patent number: 5078780Abstract: 1,5-diphenylpyrazole-3-carboxylic acid derivatives of the formula ##STR1## are capable of antagonising specifically the phytotoxic action of phenoxypropionic acid ester herbicides of the formula II ##STR2## in which G represents ##STR3## Compositions, containing those compositions, as selective herbicides and the use of those two active ingredients for controlling weeds in crops of useful plants are described, as are also novel 1,5-diphenylpyrazole-3-carboxylic acid derivatives corresponding to the formula I and the preparation thereof.Type: GrantFiled: October 16, 1987Date of Patent: January 7, 1992Assignee: Ciba-Geigy CorporationInventors: Hans Moser, Beat Bohner, Werner Fory
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Patent number: 5055482Abstract: An N-phenylpyrazol-4-yl ether derivative of the formula: ##STR1## wherein R.sup.1 represents halogen, alkyl or alkoxy unsubstituted or substituted by halogen, alkylthio or alkylsulphinyl substituted by one or more halogen atoms, nitro, cyano, or alkylsulphonyl unsubstituted or substituted by halogen and n is 1 to 5, R.sup.3 represents hydrogen, halogen, cyano, nitro or alkyl group R.sup.2 which may be unsubstituted or substituted by halogen, R.sup.4 represents alkyl, alkenyl or alkynyl which is substituted by halogen, R.sup.5 represents hydrogen or an amino group NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 represent hydrogen, alkyl, formyl or alkanoyl (or R.sup.6 and R.sup.7 together form a 5 or 6 membered cyclic imide) which may be unsubstituted or substituted by halogen, or alkoxycarbonyl unsubstituted or substituted by halogen, or R.sup.Type: GrantFiled: July 6, 1989Date of Patent: October 8, 1991Assignee: May & Baker Ltd.Inventors: Leslie R. Hatton, David W. Hawkins, Richard G. Pennicard, David A. Roberts
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Patent number: 5055466Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are inhibitors of renin and therefore useful as cardiovascular agents.Type: GrantFiled: December 14, 1989Date of Patent: October 8, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Harold N. Weller, III, Denis E. Ryono
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Patent number: 5055475Abstract: P-hydroxy phenone derivatives of the formula 1 ##STR1## where X is ##STR2## where R.sup.1 =F, Cl, Br or trifluoromethyl or a heteroaryl of the structure ##STR3## with R.sup.2 =C.sub.1 -C.sub.4 - alkyl,Y is a bridging member of the formula --CH.dbd.CH--, --CH.sub.2 CH.sub.2 -- or --CH.sub.2 --,n is one of the numbers 2, 3 or 4 andZ is an amino group of the formula --NR.sup.2 R.sup.3 or N--pyrrolidyl or N-piperidyl, where R.sup.2 and R.sup.3 are, independently of one another, C.sub.1 -C.sub.4 -alkyl, as well as the physiologically tolerated salts thereof, are used for preparing antiarrhythmic drugs.Type: GrantFiled: July 6, 1990Date of Patent: October 8, 1991Assignee: BASF AktiengesellschaftInventors: Wilfried Lubisch, Gerda Von Philipsborn
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Patent number: 5032165Abstract: There are disclosed a (3-substituted phenyl)pyrazole derivative represented by the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X are various substituents and a salt thereof, and its production process. Said pyrazole derivative or its salt is useful as a herbicide for controlling various injurious weeds.Type: GrantFiled: August 30, 1989Date of Patent: July 16, 1991Assignee: Nihon Nohyaku Company, Ltd.Inventors: Yuzo Miura, Tsutomu Mabuchi, Mitsuru Kajioka, Isao Yanai
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Patent number: 5017214Abstract: Tetrazole-substituted benzenesulfonamides are useful as agricultural chemicals and, in particular, as growth regulants and herbicides.Type: GrantFiled: November 15, 1989Date of Patent: May 21, 1991Inventor: George Levitt
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Patent number: 5015656Abstract: A pharmaceutical compound of the formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen, hydroxy, halo, nitro, amino, C.sub.2-5 acylamino, C.sub.1-4 alkyl, --CHO, --CH.sub.2 OH, --CH.sub.2 OC.sub.1-4 alkyl, --COOH, --COC.sub.1-3 alkyl, --CH(OH)C.sub.1-3 alkyl, C.sub.1-4 alkoxy, C.sub.2-4 alkenyloxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphinyl, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene bridge; provided that at least one of R.sup.2 and R.sup.3 is C.sub.1-4 alkoxy or C.sub.2-4 alkenyloxy; and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.Type: GrantFiled: September 26, 1989Date of Patent: May 14, 1991Assignees: Lilly S.A., Lilly Industries LimitedInventors: Maria I. F. Fernandez, Terrence M. Hotten, David E. Tupper
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Patent number: 5006524Abstract: Triphenylpyrazoline compounds, including all of their geometric isomers, stereoisomers and agriculturally suitable salts; agricultural compositions containing them; and use of such compounds as insecticides.Type: GrantFiled: January 2, 1990Date of Patent: April 9, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventor: George P. Lahm
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Patent number: 4988725Abstract: N-[(alkylamino)alkyl]-3,4(or 4,5)-diaryl-1H-pyrazole-1-(branched)alkanamides and pyrazole-1-alkanamines useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic acid with an appropriate diamine followed by reduction or by reacting the anion of a lower-alkyl ester of a pyrazole-1-acetic acid with an alkylating agent followed by displacement of the ester by an appropriate amine.Type: GrantFiled: December 28, 1989Date of Patent: January 29, 1991Assignee: Sterling Drug Inc.Inventors: Denis M. Bailey, Ronald G. Powles
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Patent number: 4986845Abstract: A pyrazole derivative of the formula I ##STR1## wherein A is C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 alkynyl; B is hydrogen, C.sub.1 -C.sub.3 alkyl, halogen, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio, C.sub.2 -C.sub.4 alkoxyalkyl, C.sub.2 -C.sub.4 alkylthioalkyl or C.sub.2 -C.sub.4 alkoxycarbonyl; X is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen, nitro, cyano, etc.; Y is --OR.sup.1 (wherein R.sup.1 is C.sub.3 -C.sub.8 cycloalkyl, etc), --O--L--O--R.sup.1 (wherein L is C.sub.1 -C.sub.6 alkylene which may be substituted by C.sub.1 -C.sub.3 alkyl), --O--L--OH, --O--L--O--L--O--R.sup.2 (wherein R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl group, etc.), --O--L--R.sup.3 (wherein R.sup.3 is phenyl which may be substituted by C.sub.1 -C.sub.3 alkyl, etc.), --O--M (wherein M is a 3- to 6-membered alicyclic group), --O--L--M, --O--L--NR.sup.4 R.sup.5 (wherein each of R.sup.4 and R.sup.5 is hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.Type: GrantFiled: June 21, 1989Date of Patent: January 22, 1991Assignee: Nissan Chemical Industries Ltd.Inventors: Eiichi Oya, Junichi Watanabe, Yasuo Kondo, Takuya Kakuta, Koichi Suzuki, Tsutomu Nawamaki, Shigeomi Watanabe
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Patent number: 4987146Abstract: N-hetaryl imidazole derivatives of general Formula I ##STR1##are disclosed in whichHet represents an optionally substituted monocyclic or bicyclic heteroaromate,R.sup.3 represents hydrogen, a straight or branched C.sub.1-6 -alkyl group, or a C.sub.1-6 -alkoxy-alkyl group, andR.sup.4 represents --COOR.sup.5 --CONR.sup.6 R.sup.7 --CN, ##STR2##with R.sup.5 meaning hydrogen, a straight or branched C.sub.1-6 -alkyl group, R.sup.6 and R.sup.7 are the same of different and represent hydrogen or a straight, branched, or cyclic alkyl group with up to 7 carbon atoms or, together with the nitrogen atom, form a saturated five or six ring optionally containing another heteroatom and R.sup.8 means hydrogen or a straight, branched or cyclic alkyl group with up to 7 carbon atoms.Type: GrantFiled: July 14, 1989Date of Patent: January 22, 1991Assignee: Schering AktiengesellschaftInventors: Ralph Rohde, Helmut Biere, Ralph Schmiechen, John S. Andrews, David N. Stephens
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Patent number: 4983737Abstract: Ethylenically unsaturated compounds containing 1-hydroxycarbyloxy-2,2,6,6-tetramethylpiperidine moieties represent reactable stabilizers which may be homopolymerized or copolymerized with other ethylenically saturated monomers to form non-migrating, light stabilizers which are very effective in stabilizing polyolefins and other polymer substrates against the deleterious effects of actinic light.Type: GrantFiled: February 14, 1990Date of Patent: January 8, 1991Assignee: Ciba-Geigy CorporationInventors: Ramanathan Ravichandran, Peter J. Schirmann, Andrew Mar
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Patent number: 4968714Abstract: Fungicidal substituted 3-amino-2-pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 represents unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl or alkinyl, or unsubstituted or substituted cycloalkyl or cycloalkenyl,R.sup.2 represents hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl or alkinyl, unsubstituted or substituted cycloalky or cycloalkenyl, unsubstituted or substituted aryl or unsubstituted or substituted heterocyclyl, or represents one of the radicals --CX--YR.sup.3, --CXNR.sup.4 R.sup.5, ##STR2## --SO.sub.2 NR.sup.4 R.sup.5 or --SO.sub.2 R.sup.7, R.sup.3 represents unsubstituted or substituted alkyl or unsubstituted or substituted alkenyl or alkinyl,R.sup.4 and R.sup.Type: GrantFiled: February 16, 1990Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Winfried Lunkenheimer, Gerd Hanssler
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Patent number: 4957929Abstract: Compounds are disclosed of the formula ##STR1## where R.sup.2 is unsubstituted or substituted phenyl, R.sup.3 is lower alkyl, lower cycloalkyl or lower alkoxy lower alkyl, and L is selected from a wide variety of groups. This new class of compounds exhibit improved analgesic and anesthetic properties.Type: GrantFiled: November 22, 1988Date of Patent: September 18, 1990Assignee: BOC, Inc.Inventors: Linas V. Kudzma, H. Kenneth Spencer, Sherry A. Severnak
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Patent number: 4950754Abstract: Chromogenic dicyanomethylenepyrazolinone for thermographic recording processes and the corresponding cyanomethylene dyes of the formula ##STR1## in which R is hydrogen, hydroxyl, amino, alkyl, cycloalkyl, aryl, aralkyl or a heterocylic radical, T.sub.1 and T.sub.2, independently of one another, are each hydrogen, unsubstituted or halogen-, hydroxyl-, cyano- or lower alkoxy-substituted alkyl having a maximum of 12 carbon atoms, cycloalkyl having 5 to 10 carbon atoms or unsubstituted or halogen-, cyano-, lower alkyl- or lower alkoxy-(ring)substituted phenalkyl or phenyl, or T.sub.1 and T.sub.2 together with the nitrogen linking them are a five- or six-membered heterocyclic radical, and rings A and B, independently of one another, are unsubstituted or substituted by halogen, cyano, nitro, lower alkyl, lower alkoxy, (lower alkyl)carbonyl or (lower alkoxy)carbonyl.Type: GrantFiled: January 19, 1990Date of Patent: August 21, 1990Assignee: Ciba-Geigy CorporationInventors: Hans Junek, Manfred Klade
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Patent number: 4950668Abstract: A novel pyrazole derivative and an insecticidal or miticidal composition containing the derivative as the effective ingredient are disclosed.The pyrazole derivative of the present invention has an excellent controlling effect also against harmful insects and mites exhibiting resistance to conventional insecticides and does not disturb the ecosystem since it is less toxic and less residual.Type: GrantFiled: April 14, 1988Date of Patent: August 21, 1990Assignee: Mitsubishi Kasei CorporationInventors: Itaru Okada, Shuko Okui, Yoji Takahashi, Toshiki Fukuchi
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Patent number: 4948887Abstract: A pyrazole derivative having the formula: ##STR1## wherein A is alkyl, alkenyl or alkynyl; B is hydrogen, alkyl, halogen, haloalkyl, alkoxy, alkylthio, alkoxyalkyl, alkylthioalkyl or alkoxycarbonyl; X is alkyl, alkoxy, halogen, nitro, cyano, haloalkyl, alkoxyalkyl, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl substituted by hydrogen or alkyl, haloalkoxy, alkylthio or alkylthioalkyl; Y is --COOR1 (wherein R1 is hydrogen, alkyl, etc.), --COO--L--OR1 (wherein L is alkylene which may be substituted), --COO--L--R2 (wherein R2 is phenyl group which may be substituted), --COO--M (wherein M is 3 to 6-membered alicyclic residue containing not more than 2 sulfur or oxygen atoms), --COO--L--M, --COO--L--O--L--R2, --COO--L--S(O).sub.n --CON (R3) (R4) (wherein each of R3 and R4 is hydrogen, alkyl, etc.), a --CON--(CH.sub.2).sub.n, ##STR2## wherein R5 is alkyl), ##STR3## --CONHSO.sub.2 CH.sub.3, --CONHSO.sub.2 CF.sub.3, --COO--L--N(R3) (R4), --COO--L--CO--R1, --COO--L--CO--O--R1, --COO--L--CN, --Coo--L--NO.sub.Type: GrantFiled: March 14, 1988Date of Patent: August 14, 1990Assignee: Nissan Chemical Industries Ltd.Inventors: Masatoshi Baba, Takuya Kakuta, Norio Tanaka, Eiichi Oya, Takashi Ikai, Tsutomu Nawamaki, Shigeomi Watanabe
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Patent number: 4944790Abstract: 1,5-diphenylpyrazole-3-carboxylic acid derivatives of the formula ##STR1## in which each of R.sub.a and R.sub.b, independently of the other represents halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -haloalkyl, C.sub.2 -C.sub.5 -alkenyl, C.sub.2 -C.sub.5 -alkynyl or cyano, n represents zero or an integer from 1 to 3, and OR.sub.1 represents hydroxy, a plant-physiologically tolerable salt radical or any desired ester radical, are capable of antagonizing specifically the phytotoxic action of phenoxypropionic acid ester herbicides of the formula II ##STR2## in which G represents ##STR3## in which Hal.sub.1 represents fluorine, chlorine, bromine, iodine or trifluoromethyl, Hal.sub.2 represents hydrogen, fluorine, chlorine, bromine or trifluoromethyl, Z represents nitrogen or methine (--CH.dbd.), X represents an oxygen or sulphur atom, R.sub.1 ' represents halogen, trifluoromethyl, nitro, cyano, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.Type: GrantFiled: March 20, 1989Date of Patent: July 31, 1990Assignee: Ciba-Geigy CorporationInventors: Hans Moser, Beat Bohner, Werner Fory
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Patent number: 4939161Abstract: This invention pertains to novel substituted N-aryl-N-[1-substituted 3,5-dimethyl-4-piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, cis/trans isomeric forms and the pharmaceutically acceptable acid addition salts thereof, wherein:R.sub.1 is an alkyl group selected from the group consisting of lower-alkyl, and lower-alkoxy lower-alkyl, each alkyl group having from 1 to 6 carbon atoms; andR.sub.2 is a member selected from the group consisting of phenyl lower-alkyl, pyridinyl, lower-alkyl, thienyl lower-alkyl, pyrazolyl lower-alkyl, tetrazolyl lower-alkyl, 4,5-dihydro-5-oxo-1H-tetrazolyl lower-alkyl, 1,3-dihydro-1,3-dioxo-2H-isoindolyl (N-phthalimidyl) lower-alkyl, and 2,3-dihydro-2-oxo-1H-benzimidazolyl lower-alkyl.Type: GrantFiled: May 12, 1989Date of Patent: July 3, 1990Assignee: BOC, Inc.Inventors: Nhora L. Lalinde, John Moliterni, H. Kenneth Spencer
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Patent number: RE33495Abstract: The present invention is directed to an improved stereoselective tandem substitution and reduction of an imine precursor to the cis form of .[.3-substituted-4-(phenylamino)piperidine.]. .Iadd.3-substituted-4-anilino piperidine .Iaddend.compounds or their substituted derivatives.Type: GrantFiled: September 27, 1989Date of Patent: December 18, 1990Assignee: BOC, Inc.Inventors: Linas V. Kudzma, H. Kenneth Spencer, Sherry A. Savernak
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Patent number: RE34779Abstract: A pyrazole derivative of the formula I ##STR1## wherein A is C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 alkynyl; B is hydrogen, C.sub.1 -C.sub.3 alkyl, halogen, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio, C.sub.2 -C.sub.4 alkoxyalkyl, C.sub.2 -C.sub.4 alkylthioalkyl or C.sub.2 -C.sub.4 alkoxycarbonyl; X is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen, nitro, cyano, etc.; Y is --OR.sup.1 (wherein R.sup.1 is C.sub.3 -C.sub.8 cycloalkyl, etc), --O--L--O--R.sup.1 (wherein L is C.sub.1 -C.sub.6 alkylene which may be substituted by C.sub.1 -C.sub.3 alkyl), --O--L--OH, --O--L--O--L--O--R.sup.2 (wherein R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl group, etc.), --O--L--R.sup.3 (wherein R.sup.3 is phenyl which may be substituted by C.sub.1 -C.sub.3 alkyl, etc.), --O--M (wherein M is a 3- to 6-membered alicyclic group), --O--L--M, --O--L--NR.sup.4 R.sup.5 (wherein each of R.sup.4 and R.sup.5 is hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.Type: GrantFiled: September 18, 1992Date of Patent: November 8, 1994Assignee: Nissan Chemical Industries Ltd.Inventors: Eiichi Oya, Junichi Watanabe, Yasuo Kondo, Takuya Kakuta, Koichi Suzuki, Tsutomu Nawamaki, Shigeomi Watanabe