Triazoles (including Hydrogenated) Patents (Class 514/93)
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Patent number: 6369165Abstract: A process for preparing polymers of N-vinyl compounds comprises polymerizing the vinyl compounds in the presence of free radicals of the formula I where Q is NR2 or S and T is CR3R4 or S and R1, R2, R3 and R4 can be identical or different and are, independently of one another, hydrogen, C1-C20-alkyl or C6-C18-aryl.Type: GrantFiled: August 16, 2000Date of Patent: April 9, 2002Assignee: BASF Akiengesellschaft & Max-Planck-GesellschaftInventors: Roman Benedikt Raether, Wolfgang Paulus, Frank Braun, Klaus Müllen, Markus Klapper, Marco Steenbock
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Patent number: 6369044Abstract: Novel triazolinethione-phosphoric acid derivatives of the formula in which R1, R2, R3 and Q are each as defined in the description and their metal salt complexes, a process for preparing the novel substances and their use as microbicides in crop protection and in the protection of materials are described.Type: GrantFiled: May 17, 2001Date of Patent: April 9, 2002Assignee: Bayer AktiengesellschaftInventors: Stefan Hillebrand, Bernd-Wieland Krüger, Manfred Jautelat, Klaus Stenzel, Astrid Mauler-Machnik, Stefan Dutzmann
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Patent number: 6362172Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.Type: GrantFiled: January 10, 2001Date of Patent: March 26, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Yasutsugu Ueda, John D. Matiskella, Jerzy Golik, Thomas W. Hudyma, Chung-Pin Chen
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Patent number: 6331531Abstract: Method for controlling harmful organisms in genetically modified cotton plants which contain a gene derived from Bacillus thuringiensis which encodes and expresses an insecticidally active protein, which comprises applying an insecticisally effective amount of one or more compounds from the following groups and a-f, described herein, to the plants, to their seeds or propagation stock and/or to the area in which they are cultivated. The method according to the invention makes it possible to reduce the application rate of crop protection agents which act synergistically with the transgenic plants, and also to increase and widen the efficacy of the transgenic plants, and therefore offers both economical and ecological advantages.Type: GrantFiled: June 3, 1999Date of Patent: December 18, 2001Assignee: Aventis CropScience GmbHInventor: Manfred Kern
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Patent number: 6300356Abstract: Angiotensin II receptor antagonists are useful for decreasing QT dispersion or inhibiting the progression of QT prolongation in patients. Also disclosed is a method for monitoring the reduction in die risk of experiencing an adverse cardiac event, such as sudden cardiac death, myocardial infarction or arrhythmias, using QT dispersion in patients treated with a therapeutically effective amount of an angiotensin II antagonist.Type: GrantFiled: August 10, 2000Date of Patent: October 9, 2001Assignee: Merck & Co., Inc.Inventors: Robert Segal, Paul J. Robinson, Lawrence I. Deckelbaum
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Patent number: 6281201Abstract: Antiviral compounds have the formula wherein m is zero, 1, 2 or 3; n is from 1 to 8, preferably 1, 2 or 3; most preferably 1 or 2; R is independently selected from the group consisting of provided that all R may not be R1 is independently selected from the group consisting of hydroxyl and hydrogen; R2 is independently selected from the group consisting of oxygen and sulfur; or water soluble salts thereof.Type: GrantFiled: December 8, 1999Date of Patent: August 28, 2001Assignee: Temple University- of the Commonwealth System of Higher EducationInventors: Robert J. Suhadolnik, Wolfgang Pfleiderer
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Patent number: 6262039Abstract: Novel triazolinethione-phosphoric acid derivatives of the formula in which R1, R2, R3 and Q are each as defined in the description and their metal salt complexes, a process for preparing the novel substances and their use as microbicides in crop protection and in the protection of materials are described.Type: GrantFiled: January 20, 2000Date of Patent: July 17, 2001Assignee: Bayer AktiengesellschaftInventors: Stefan Hillebrand, Bernd-Wieland Krüger, Manfred Jautelat, Klaus Stenzel, Astrid Mauler-Machnik, Stefan Dutzmann
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Patent number: 6235728Abstract: Water soluble prodrugs of azole antifungal agents are provided by quaternizing a nitrogen atom of the azole ring with a phosphonooxymethyl group.Type: GrantFiled: February 11, 2000Date of Patent: May 22, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Jerzy Golik, John D. Matiskella, Yasutsugu Ueda
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Patent number: 6200961Abstract: A low volatile organic compound co-solvent system is disclosed for preparing emulsion concentrates of low melting organophosphorous insecticides wherein the bioefficacy of the insecticide active is significantly enhanced. The co-solvent system comprises a water-soluble ethoxylated fatty acid/rosin acid-nonionic surfactant composition.Type: GrantFiled: December 16, 1998Date of Patent: March 13, 2001Assignee: Aquatrols Corporation of America, Inc.Inventors: Stanley J. Kostka, Rennan Pan
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Patent number: 6110904Abstract: A method for suppressing plant damage by nematodes which comprises the concurrent administration, to the locus, soil or seeds of plants in need of such treatment, of (a) a metabolite of the fungus Myrothecium verrucaria and (b) a chemical pesticide, as well as synergistic nematocidal compositions useful therein.Type: GrantFiled: August 28, 1997Date of Patent: August 29, 2000Assignee: Valent BioSciences, Inc.Inventors: Prem Warrior, Daniel F. Heiman, Linda A. Rehberger
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Patent number: 5962439Abstract: Fused benzeneoxyacetic acid derivatives of the formula (I): ##STR1## or salts thereof possess an agonistic effect on the PGI.sub.2 receptor and thus are useful for preventing and/or treating thrombosis, arteriosclerosis, ischemic heart diseases, gastric ulcer and hypertension. A, B, D, and R.sup.1 are as defined in the specification.Type: GrantFiled: October 7, 1998Date of Patent: October 5, 1999Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
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Patent number: 5880111Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.Type: GrantFiled: June 7, 1995Date of Patent: March 9, 1999Inventors: Dan Farcasiu, John F. Hartmann, Pal Herczegh, Ferenc J. Sztaricskai
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Patent number: 5741784Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; ....... represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## ,or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.Type: GrantFiled: August 30, 1996Date of Patent: April 21, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Patent number: 5707978Abstract: Therapeutically active, heteroaryl-substituted deoxy glycero-phosphoethanolamines are disclosed having the general Formula I: ##STR1## wherein one of X, Y or Z is a fatty ether substituent, one is a heteroaryl ring substituent with 1-4 nitrogens as the only heteroatoms, one of which is bonded to a carbon of the glyceryl backbone, and one is a phosphoethanolamine substituent substituted at the nitrogen, provided that each of X, Y and Z is a different substituent, and the pharmaceutical compositions comprising the therapeutically active compounds and methods of using the therapetically active compounds to treat cancerous tumors, psoriasis and inflammation are also disclosed.Type: GrantFiled: June 7, 1995Date of Patent: January 13, 1998Assignee: Clarion Pharmaceuticals Inc.Inventors: Friedrich Paltauf, Albin Hermetter, Rudolf Franzmair
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Patent number: 5624916Abstract: 2-Aryl or 2-heterocyclyl-2, 2-disubstituted ethyl-1,2,4-triazoles have been shown to have fungicidal activity.Type: GrantFiled: June 12, 1995Date of Patent: April 29, 1997Assignee: Rohm and Haas CompanyInventors: Steven H. Shaber, Luong T. Nguyen
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Patent number: 5622917Abstract: The invention relates to new 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, X, Y and G have the meanings given in the description, to a plurality of processes for their preparation, and to their use as pesticides.Type: GrantFiled: January 3, 1995Date of Patent: April 22, 1997Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kr uger, Michael Ruther, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger
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Patent number: 5614509Abstract: The use of NMDA receptor antagonists or their physiologically compatible salts for preventing the development of tolerance during the long-term treatment with benzodiazepine-receptor-binding active ingredients as well as the combination of new pharmaceutical agents with benzodiazepine-receptor-binding active ingredients is described.Type: GrantFiled: March 2, 1995Date of Patent: March 25, 1997Assignee: Schering AktiengesellschaftInventors: Lechoslaw Turski, Karin G. Steppuhn, Herbert Schneider, David N. Stephens
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Patent number: 5580863Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.Type: GrantFiled: May 13, 1994Date of Patent: December 3, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Patent number: 5476846Abstract: The present invention concerns new substituted sulfonamides, and the physiologically acceptable salts, complexes, esters and amides thereof, represented by the formula ##STR1## which is defined herein. Said compounds find application as anti-thrombotic and anti-asthmatic medicines.Type: GrantFiled: November 17, 1994Date of Patent: December 19, 1995Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Claude Lardy, Daniel Guerrier, Gilles Chavernac, Francois Collonges
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Patent number: 5462931Abstract: 2-Aryl or 2-heterocyclyl-2, 2-disubstituted ethyl-1,2,4-triazoles have been shown to have fungicidal activity.Type: GrantFiled: June 30, 1994Date of Patent: October 31, 1995Assignee: Rohm and Haas CompanyInventors: Steven H. Shaber, Luong T. Nguyen
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Patent number: 5449785Abstract: Compounds of the formula ##STR1## which have antifungal activity.Type: GrantFiled: July 10, 1992Date of Patent: September 12, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Yuhko Aoki, Hiromichi Kotaki, Kazunao Masubuchi, Toru Okuda, Nobuo Shimma, Takuo Tsukuda, Isao Umeda
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Patent number: 5405841Abstract: The invention relates to new phosphorylated aza compounds, to processes for their preparation and to their use as pesticides, in particular as soil-acting insecticides and nematicide.The new compounds have the general formula (I) ##STR1## in which R.sup.1 -R.sup.5, X and Y are defined as in the specification, with the exception of compound O-ethyl S-propyl 3-(6-chloro-3-pyridinylmethyl)-2-nitroimino-imidazolidine-1-thiophosphate.Type: GrantFiled: November 30, 1993Date of Patent: April 11, 1995Assignee: Bayer AktiengesellschaftInventors: Fritz Maurer, Jurgen Hartwig, Christoph Erdelen
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Patent number: 5358939Abstract: 2-Aryl or 2-heterocyclyl-2,2-disubstituted ethyl-1,2,4,-triazoles have been shown to have fungicidal activity.Type: GrantFiled: June 25, 1992Date of Patent: October 25, 1994Assignee: Rohm and Haas CompanyInventors: Steven H. Shaber, Luong T. Nguyen
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Patent number: 5326776Abstract: Compounds are disclosed having the formula: ##STR1## wherein the substituents are defined herein. The compounds of the invention are angiotensin II receptor antagonists.Type: GrantFiled: February 24, 1993Date of Patent: July 5, 1994Assignee: Abbott LaboratoriesInventors: Martin Winn, Biswanath De, Thomas M. Zydowsky, Daniel J. Kerkman, John F. DeBernardis, Saul H. Rosenberg, Kazumi Shiosaki, Fatima Z. Basha, Kenneth P. Spina, Thomas W. von Geldern, Steven Boyd, Diane M. Yamamoto, Anthony K. L. Fung
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Patent number: 5234917Abstract: Angiotensin II receptor antagonists having the formula: ##STR1## which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma pharmaceutical compositions including these antagonists, and methods of using these compounds to produce angiotensin II receptor antagonism in mammals.Type: GrantFiled: November 30, 1990Date of Patent: August 10, 1993Inventors: Joseph A. Finkelstein, Judith Hempel, Richard M. Keenan, James Samanen, Joseph Weinstock
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Patent number: 5189062Abstract: ULV plant protecting arthropodicidal formulation comprising alkyl aryl polyglycol ether as further additives in addition to the active ingredient(s) dissolved in the mixture of alphatic hydrocarbons and sunflower oil. The formulation according to the invention has an initial contact angle on the plant surface of >13.degree., after 20 minutes of >6.degree. and it is often 120 minutes still at least 2.degree..Type: GrantFiled: January 28, 1992Date of Patent: February 23, 1993Assignee: Chinoin Gyogyszer -ES Vegyeszeti Termekek Gyara R.T.Inventors: Andras Szego, Laszlo Pap, Lajos Nagy, Eva Somfai, Gyorgy Szucsany, Istvan Szekely, Aniko D. nee Molnar, Agnes Hegedus
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Patent number: 5164381Abstract: 1,5-Diaryl-3-substituted pyrazoles, a method of their preparation, compositions containing the same and methods of their use are disclosed. The pyrazoles are useful in alleviating inflammatory and cardiovascular disorders in mammals.Type: GrantFiled: July 12, 1991Date of Patent: November 17, 1992Assignee: Ortho Pharmaceutical CorporationInventors: Michael P. Wachter, Michael P. Ferro
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Patent number: 5147865Abstract: The invention relates to new phosphonopyrrolidine- and piperidine-containing pseudopeptides, to a process for their preparation and to their use as medicaments, in particular as antiviral agents in human and veterinary medicine.Type: GrantFiled: August 15, 1991Date of Patent: September 15, 1992Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Jutta Hansen, Arnold Paessens
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Patent number: 5057505Abstract: Heteroarylaminomethanediphosphonic acids of the formula ##STR1## in which R.sub.1 represents an optionally benzo- or cyclohexeno-fused 5-membered heteroaryl radical that contains, as hetero atom(s), either from 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O-atom or S-atom and that is unsubstituted or is substituted by lower alkyl; by phenyl that is unsubstituted or is substituted by lower alkyl, lower alkoxy and/or by halogen; by lower alkoxy; by hydroxy; by di-lower alkylamino; by lower alkylthio and/or by halogen; and R.sub.2 represents hydrogen or lower alkyl, and their salts, have a regulatory action on the calcium metabolism and can be used as active ingredients in medicaments for the treatment of illnesses that can be attributed to disorders of the calcium metabolism. They are manufactured, for example, as follows: in a compound of the formula ##STR2## in which X.sub.1 represents a functionally modified phosphono group X and X.sub.Type: GrantFiled: May 19, 1989Date of Patent: October 15, 1991Assignee: Ciba-Geigy CorporationInventors: Leo Widler, Knut Jaeggi
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Patent number: 5055471Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.Type: GrantFiled: November 15, 1989Date of Patent: October 8, 1991Assignee: Imperial Chemical Industries PLCInventors: Paul J. de Fraine, Anne Martin
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Patent number: 4988681Abstract: A phosphinic acid derivative represented by the general formula [I], or a pharmaceutically acceptable salt thereof, ##STR1## wherein R.sup.1 represents an alkyl, cycloalkyl or aralkyl group which may be substituted; R.sup.2 and R.sup.5 may be identical or different, and each represents a hydrogen atom, or an ester residue capable of forming a non-toxic ester hydrolyzable in vivo; and A represents a group of the formula ##STR2## wherein R.sup.3 represents an alkyl group, a group of the formula ##STR3## wherein R.sup.30 represents a halogen atom, a carboxyl group, a hydroxyl group, a cycloalkyl group which may be substituted, an aryl group which may be substituted, an arylthio group, a heteroarylthio group which may be substituted, an alkylthio group which may be substituted, an amino group which may be substituted, or a lower alkoxycarbonyl group; R.sup.Type: GrantFiled: June 22, 1989Date of Patent: January 29, 1991Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Kiyofumi Ishikawa, Takehiro Fukami, Hiroshi Naganuma, Kyoko Nakamichi
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Patent number: 4939130Abstract: Alkanediphosphonic acids, in particular heteroarylalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is a 5-membered heteroaryl radical which may be fused with benzene or cyclohexene nuclei and which contains, as hetero atoms, 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O- or S-atom, and which is unsubstituted or C-substituted by lower alkyl, phenyl or phenyl which is substituted by lower alkyl, lower alkoxy and/or halogen, or by lower alkoxy, hydroxy, di-lower alkylamino, lower alkylthio and/or halogen, and/or is N-substituted at a N-atom which is capable of substitution by lower alkyl, lower alkoxy and/or halogen, and R.sub.2 is hydrogen, hydroxy, amino, lower alkylthio or halogen, and salts thereof, have regulatory action on calcium metabolism and can be used as medicaments for the treatment of diseases associated with impairment of calcium metabolism. The compounds are obtained for example by converting, in a compound of formula ##STR2## wherein X.sub.Type: GrantFiled: February 27, 1989Date of Patent: July 3, 1990Assignee: Ciba-Geigy CorporationInventors: Knut A. Jaeggi, Leo Widler
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Patent number: 4938797Abstract: The invention relates to a process for the preparation of microcapsules having a capsule wall of polyurea and encapsulating a water-immiscible pesticide. The process comprises first dispersing a solution of a polyisocyanate in the sparingly water-soluble pesticide, in the presence of an anionic dispersant and at least one nonionic protective colloid and/or a nonionic surfactant, and subsequently reacting the dispersion with a polyamine, to give a stable aqueous suspension of microcapsules which can be used either direct or after dilution with water as pesticidal composition.Type: GrantFiled: June 7, 1988Date of Patent: July 3, 1990Assignee: Ciba-Geigy CorporationInventors: Hans W. Hasslin, Michael J. Hopkinson
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Patent number: 4885283Abstract: The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.Type: GrantFiled: December 1, 1987Date of Patent: December 5, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Balraj K. Handa, William H. Johnson, Geoffrey Lawton, Peter J. Machin
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Patent number: 4870103Abstract: The invention relates to plant protection agents based on aqueous microemulsions which contain, as emulsifiers, ethoxylated and phosphorylated, styryl-substituted phenols or salts thereof in combination with one or more non-phosphorylated emulsifiers belonging to the group comprising salts of (C.sub.10 -C.sub.16)-alkyl-monoglycol to -hexaglycol ether-sulfates, salts of .alpha.-(C.sub.14 -C.sub.19)-alkenol sulfates, salts of optionally chlorinated (C.sub.13 -C.sub.18)-alkanesulfonic acids, salts of dodecylphenylsulfonic acid, amine oxethylates or .alpha.(C.sub.9 -C.sub.20)-alkyl-.omega.-hydroxypolyoxyethylenes containing 2 to 22 moles of ethylene oxide.Type: GrantFiled: July 21, 1987Date of Patent: September 26, 1989Assignee: Hoechst AktiengesellschaftInventors: Hans Rochling, Konrad Albrecht
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Patent number: 4870065Abstract: The present invention relates to novel compounds of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and stand for alkyl having 1 to 4 carbon atoms optionally substituted by one or more halogen atoms, alkenyl having 2 to 6 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, phenyl or lower alkoxy-alkyl group,R.sub.3 stands for alkyl having 1 to 6 carbon atoms or alkenyl having 2 to 6 carbon atoms,R.sub.4 and R.sub.5 are the same or different and represent hydrogen, alkyl having 1 to 6 carbon atoms, alkenyl having 2 to 6 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, phenyl, benzyl, phenyl substituted by one or more alkyl having 1 to 3 carbon atoms and/or by one or more halogen atoms, lower alkoxy-alkyl, a group of the formula --(CH.sub.2).sub.n --R.sub.6, wherein n is an integer between 0 to 3 and R.sub.Type: GrantFiled: September 26, 1985Date of Patent: September 26, 1989Assignee: Eszakmagyarorszagi VegyimuvekInventors: Karoly Balogh, Zsolt Dombay, Karoly Fodor, Gregna nee ToErzsebet, Erno Lorik, Magdolna Magyar nee Tomorkenyi, Jozsef Nagy, Karoly Pasztor, Pal Santha, Gyula Tarpai, Istvan Toth, Eszter Urszin nee Simon
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Patent number: 4784993Abstract: The present invention provides diphosphonates of the general formula: ##STR1## wherein Het is 1,2,3-triazole, or 1,2,4-triazole radical, which is optionally substituted by alkyl, alkoxy, halogen, hydroxyl, carboxyl, an amino group optionally substituted by alkyl or acyl radicals or is a benzyl radical optionally substituted by alkyl, nitro, amino or aminoalkyl, A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 carbon atoms, X is a hydrogen atom, optionally substituted by acyl, or an amino group optionally substituted by alkyl or acyl radicals and R is a hydrogen atom or an alkyl radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these diphosphonates and pharmaceutical compositions containing them.Type: GrantFiled: July 23, 1987Date of Patent: November 15, 1988Assignee: Boehringer Mannheim GmbHInventors: Elmar Bosies, Rudi Gall
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Patent number: 4777163Abstract: The present invention produces alkyldiphosphonic acid derivative of the general formula: ##STR1## wherein Het is a heteroaromatic five-membered ring containing to 3 heteroatoms which can be partly hydrogenated and optionally substituted one or more times by alkyl, alkoxy, phenyl, cyclohexyl, cyclohexylmethyl, halogen or amino, and two adjacent alkyl substituents can together also form a ring, Y is a hydrogen atom or a lower alkyl radical, X is a hydrogen atom, a hydroxyl group or an amino group optionally substituted by lower alkyl and R is a hydrogen atom or a lower alkyl radical, with the proviso that Het is not a pyrazole ring; as well as the pharmacologically acceptable salts thereof.Type: GrantFiled: July 24, 1987Date of Patent: October 11, 1988Assignee: Boehringer Mannheim GmbHInventors: Elmar Bosies, Rudi Gall
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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: 4687767Abstract: The present invention provides diphosphonates of the general formula: ##STR1## wherein Het is an imidazole, oxazole, isoxazole, thiazole, pyridine, 1,2,3-triazole, 1,2,4-triazole or benzimidazole radical, which is optionally substituted by alkyl, alkoxy, halogen, hydroxyl, carboxyl, an amino group optionally substituted by alkyl or alkanoyl radicals or a benzyl radical optionally substituted by alkyl, nitro, amino or aminoalkyl, A is a straight-chained or branched, saturated or unsaturated hydrocarbon chain containing 2 to 8 carbon atoms, X is a hydrogen atom, optionally substituted by alkanoyl, or an amino group optionally substituted by alkyl or alkanoyl radicals and R is a hydrogen atom or an alkyl radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these diphosphonates and pharmaceutical compositions containing them.Type: GrantFiled: July 26, 1985Date of Patent: August 18, 1987Assignee: Boehringer Mannheim GmbHInventors: Elmar Bosies, Rudi Gall
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Patent number: 4643993Abstract: Compounds of the formula ##STR1## wherein Het is a heterocycle containing 2 to 3 nitrogen atoms;R is hydrogen, lower alkyl, alkoxy of 1 to 3 carbon atoms or halogen;Y is --SO.sub.3 H or ##STR2## R" is alkyl of 1 to 3 carbon atoms; and R' is straight or branched alkyl which may contain a heteroatom such as sulfur, oxygen or nitrogen; straight or branched alkenyl; cycloalkyl; alkyl-cycloalkyl; aryl; or aralkyl optionally substituted by lower alkyl, alkoxy of 1 to 3 carbon atoms or halogen; tautomers thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics and gastric acid secretion inhibitors.Type: GrantFiled: May 18, 1983Date of Patent: February 17, 1987Assignee: Istituto de Angeli S.p.A.Inventors: Enzo Cereda, Arturo Donetti, Antonio Giachetti, Piero del Soldato
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Patent number: 4619918Abstract: Insecticidally and nematicidally active novel triazol-3-yl thionophosphates of the formula ##STR1## in which R represents i-propyl or sec.-butyl,R.sup.1 represents alkyl or aryl andR.sup.2 represents halogen.Type: GrantFiled: November 4, 1985Date of Patent: October 28, 1986Assignee: Bayer AktiengesellschaftInventors: Fritz Maurer, Bernhard Homeyer
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Patent number: 4602929Abstract: Compounds having the general formula (I): ##STR1## and stereoisomers thereof, wherein R.sup.1 and R.sup.2 are each hydrogen, a cation, alkyl, cycloalkyl, aryl or aralkyl optionally substituted with halogen, nitro, alkyl, haloalkyl, alkoxy, haloalkoxy, phenyl, phenoxy, halophenyl or halophenoxy, or together form a ring; R.sup.3 and R.sup.4 are each hydrogen, alkyl, cycloalkyl, heterocyclyl, aryl or aralkyl optionally substituted with halogen, nitro, alkyl, haloalkyl, alkoxy, haloalkoxy, phenyl, phenoxy, halophenyl or halophenoxy; W is N or CH; X is oxygen or sulphur; ester and ether derivatives of the alcohol; and its acid addition salts and metal complexes. The compounds are useful as fungicides and for plant growth regulation.Type: GrantFiled: March 2, 1984Date of Patent: July 29, 1986Assignee: Imperial Chemical Industries PLCInventors: John Dalziel, Paul A. Worthington, Balasubramanyan Sugavanam
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Patent number: 4562185Abstract: The present invention relates to combating pests with five-membered nitrogen-containing heterocyclic compounds of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given in the description. Many of the compounds are new.Type: GrantFiled: March 15, 1984Date of Patent: December 31, 1985Assignee: Bayer AktiengesellschaftInventors: Gerhard Jager, Rudolf Fauss, Kurt Findeisen, Benedikt Becker, Bernhard Homeyer
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Patent number: 4535074Abstract: Fungicidally active novel phosphorylated azolyl derivatives of the formula ##STR1## in which A represents a nitrogen atom or the CH group,R represents optionally substituted phenyl or the grouping ##STR2## wherein X and Y are identical or different and represent hydrogen or halogen,R.sup.1 represents hydrogen andR.sup.2 represents hydrogen, optionally substituted phenoxy or optionally substituted benzyl, orR.sup.1 and R.sup.2 together represent the grouping .dbd.CH--Z, wherein Z represents optionally substituted cycloalkyl or optionally substituted phenyl,R.sup.3 represents alkyl, optionally substituted phenyl or optionally substituted benzyl,R.sup.4 represents hydrogen or alkyl andR.sup.5 represents hydrogen or alkyl,or salts or addition products thereof with metal salts.Type: GrantFiled: March 26, 1984Date of Patent: August 13, 1985Assignee: Bayer AktiengesellschaftInventors: Reinhard Preuss, Hermann Perrey, Helmut Ritter, Paul Reinecke, Wilhelm Brandes
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Patent number: 4528284Abstract: Phosphoric acid esters of the formula ##STR1## wherein X is CH or N,Ar is optionally substituted phenyl, diphenyl or naphthyl,R is cyano, carboxylic acid ester, carboxylic acid thioester or carboxylic acid amide.R.sub.10 is alkyl,R.sub.11 alkyl, alkoxy, alkylthio or phenyl, andY is sulfur.For R: the ester groups are alkenyl, alkynyl, cycloalkyl, optionally substituted phenyl, alkyl interrupted by oxygen or sulfur and optionally substituted by halogen, phenyl, carboxylic acid ester, alkylcarbonyl, optionally substituted phenyl carbonyl, or a C.sub.5 or C.sub.6 heterocycle; the thioester groups are alkyl or optionally substituted phenyl or benzyl; the amide is optionally mono- or di-substituted by alkyl, cycloalkyl, optionally substituted phenyl or benzyl, or may form a C.sub.5 or C.sub.6 heterocyclic ring. The compounds are useful in controlling phytopathogenic fungi.Type: GrantFiled: October 5, 1983Date of Patent: July 9, 1985Assignee: Ciba-Geigy CorporationInventors: Wolfgang Eckhardt, Walter Kunz