Carbon, Also In The Chain, Double Bonded To The Nitrogen Patents (Class 558/391)
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Publication number: 20150025042Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: December 16, 2013Publication date: January 22, 2015Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
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Publication number: 20150018543Abstract: The present invention relates to 4H-pyrido[1,2-a]pyrimidin-4-one compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.Type: ApplicationFiled: April 28, 2014Publication date: January 15, 2015Applicants: Institut Pasteur Korea, INSERM (Institut National de la Sante et de la Recherche Medicale)Inventors: Priscille BRODIN, Thierry CHRISTOPHE, Zaesung NO, Jaeseung KIM, Auguste GENOVESIO, Denis Philippe Cedric FENISTEIN, Heekyoung JEON, Fanny Anne EWANN, Sunhee KANG, Saeyeon LEE, Min Jung SEO, Eunjung PARK, Monica CONTRERAS DOMINGUEZ, Ji Youn NAM, Eun Hye KIM
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Patent number: 8629288Abstract: The present invention relates to a process for the regioselective synthesis of 1-alkyl-3-halo-alkylpyrazole-4-carboxylic acid derivatives by cyclization of 2,3-disubstituted acrylic acid derivatives, and to the hydrazones formed as intermediates in the process.Type: GrantFiled: February 12, 2009Date of Patent: January 14, 2014Assignee: Bayer Intellectual Property GmbHInventors: Sergii Pazenok, Norbert Lui, Jens-Dietmar Heinrich, Thomas Wollner
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Patent number: 8592605Abstract: The present invention relates to a process for the regioselective synthesis of 1-alkyl-3-halo-alkylpyrazole-4-carboxylic acid derivatives by cyclization of 2,3-disubstituted acrylic acid derivatives, and to the hydrazones formed as intermediates in the process.Type: GrantFiled: March 14, 2013Date of Patent: November 26, 2013Assignee: Bayer Intellectual Property GmbHInventors: Sergii Pazenok, Norbert Lui, Jens-Dietmar Heinrich, Thomas Wollner
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Patent number: 7884244Abstract: Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: March 28, 2008Date of Patent: February 8, 2011Assignee: Allergan, Inc.Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil, Michael E. Garst
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Publication number: 20110009642Abstract: The present invention relates to a process for the regioselective synthesis of 1-alkyl-3-halo-alkylpyrazole-4-carboxylic acid derivatives by cyclization of 2,3-disubstituted acrylic acid derivatives, and to the hydrazones formed as intermediates in the process.Type: ApplicationFiled: February 12, 2009Publication date: January 13, 2011Applicant: Bayer Cropscience AGInventor: Sergii Pazenok
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Patent number: 7446219Abstract: The invention relates to compounds of the general formula in which R1, R2, R3, R4, R5, R6, W, X, A1, A2, a, b and c are as defined in the specification, and to any enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are particularly suitable for controlling parasites in warm-blooded animals.Type: GrantFiled: May 21, 2003Date of Patent: November 4, 2008Assignee: Novartis Animal Health US Inc.Inventors: Pierre Ducray, Thomas Goebel, Jacques Bouvier, Corinne Durano
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Publication number: 20080255230Abstract: Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: March 28, 2008Publication date: October 16, 2008Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil, Michael E. Garst
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Patent number: 7371747Abstract: The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by unregulated cysteine protease activity, in particular cathepsin K utilizing these compounds and methods of preparing these compounds are also disclosed.Type: GrantFiled: November 13, 2002Date of Patent: May 13, 2008Assignee: Merck Frosst Canada & Co.Inventors: Cameron Black, Sheldon N. Crane, Dana Davis, Eduardo L. Setti
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Patent number: 7365098Abstract: The present invention relates to novel N?-cyano-N-methylimidamide derivatives of the general formula (I) in which n represents 2, 3, 4 or 5, R represents optionally halogen-substituted C1-C4-alkyl, and X represents halogen, where the substituents X may in each case be identical or different, to processes for their preparation and to their use as pesticides.Type: GrantFiled: May 8, 2003Date of Patent: April 29, 2008Assignee: Bayer CropScience AGInventors: Achim Hense, Rüdiger Fischer, Ernst R. F. Gesing, Stefan Herrmann, Kristian Kather, Angelika Lubos-Erdelen, legal representative, Jörg Konze, Peter Lösel, Christoph Erdelen
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Patent number: 7179913Abstract: The invention discloses a method for preparing the intermediate 2-(2,3-dichlorophenyl)-2-(aminoguanidine)acetonitrile of formula (II), which comprises the reaction of 2,3-dichlorobenzoyl cyanide with aminoguanidine bicarbonate in non-aqueous medium in the presence of methanesulphonic acid, which produces good yields and short reaction times. Said intermediate is useful for preparing 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine of formula (I).Type: GrantFiled: October 27, 2003Date of Patent: February 20, 2007Assignee: Vita Cientifica, S.A.Inventors: Jordi Bessa Bellmunt, Pere Dalmases Barjoan
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Patent number: 7135585Abstract: Compounds of Formula I are disclosed which are useful as fungicides wherein Q is Z is X is —O—, —CH(R11)— or ?C(R11)—; R1 is H or C1–C2 alkyl; R2 is H; C1–C6 alkyl; C3–C6 cycloalkyl; or phenyl optionally substituted with halogen, cyano, C1–C2 alkyl or C1–C2 alkoxy; and R3–R11 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.Type: GrantFiled: March 2, 2001Date of Patent: November 14, 2006Inventors: Gregory Steven Basarab, Douglas Brian Jordan, Thomas Arend Lessen, Stephen L. Hansen
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Patent number: 6812229Abstract: It is to provide a novel fungicide having high controlling effects on plant diseases particularly on wheat powdery mildew and cucumber gray mold, without ill effects on crops. A carbamate derivative represented by the general formula [I] {wherein X is a halogen atom, a C1-C6 alkyl group or the like, n is 0 or an integer of from 1 to 4, R1 is a C1-C6 alkyl group, R2 is a hydrogen atom, a C1-C6 alkyl group or the like, R3 is a hydrogen atom or a C1-C6 alkyl group, G is an oxygen atom, a sulfur atom or the like, Y is a hydrogen atom, a C1-C10 alkyl group, C2-C10 alkenyl group or the like, and Q is a hydrogen atom, a C1-C6 haloalkyl group, a phenyl group or the like} and an agricultural/horticultural fungicide containing the same as the active ingredient.Type: GrantFiled: February 5, 2002Date of Patent: November 2, 2004Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masami Ozaki, Shunichiro Fukumoto, Ryuji Tamai, Kazuhiro Ikegaya, Norihisa Yonekura, Takahiro Kawashima, Junetsu Sakai, Norimichi Muramatsu, Makikazu Takagaki, Kouzou Nagayama
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Patent number: 6646151Abstract: The invention relates to a process for the preparation of compounds of the formula or, if appropriate, a tautomer thereof, in each case in the free form or in salt form, in which A, X, Y, Z, R2, R3, R4, R5, R7, R9 and n are as defined in claim 1 and the C═N double bond marked with E has the E configuration, which comprises a1) reacting either a compound of the formula (II) mentioned above with a compound of the formula (III) mentioned above, in which X1 is a leaving group, or a2) a compound of the formula (IV) mentioned above, if appropriate in the presence of a base, with a compound of the formula (V) mentioned above, or b1) reacting a compound of the formula (VI) mentioned above with a compound of the formula R7—A—X2 (VII), in which X2 is a leaving group, and either further reacting the compound thus obtainable, of the formula (IV), for example according to method a2), or b2) reacting it with hydroxylamine or a salt thereof, if appropriate in the presence of a basic orType: GrantFiled: September 26, 2000Date of Patent: November 11, 2003Assignee: Bayer AktiengesellschaftInventors: Saleem Farooq, Stephan Trah, Hugo Ziegler, René Zurflüh
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Patent number: 6555702Abstract: A compound of the formula I: wherein A and C are independently H, alkyl of 1-6 carbon atoms, hydroxy, or alkoxy of 1-6 carbon atoms; B is hydroxy, alkoxy of 1-6 carbon atoms —CO2Z, —O(CH2)mCO2Z, —SO3Z, —OPO3Z2; and Y is cyano, —C(NR1R2)═C(CN)2; wherein X═O or S, and R1 and R2 are independently H, benzyl, —CH(CH3)C6H6, —(CH2)n C6H6, phenyl; —CO2R; n=2-4; R is lower alkyl of 1-6 carbon atoms; m=1-4 and Z is H, a cation or lower alkyl of 1-6 cabon atoms; is used for treating inflammation, immunological diseases or diabetes.Type: GrantFiled: April 3, 1998Date of Patent: April 29, 2003Assignee: Calyx Therapeutics, Inc.Inventors: Subramaniam Sriram, John Bright, Bishwajit Nag, Somesh D. Sharma
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Publication number: 20020128485Abstract: The present invention relates to processes for the preparation of a compound of the formula 1Type: ApplicationFiled: April 12, 2002Publication date: September 12, 2002Inventor: Jean-Erick Ancel
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Patent number: 6417386Abstract: A composition, which comprises at least one compound of the formula in which A1, A2, R1 and R2 are as defined in claim 1, or, if appropriate, an E/Z isomer, an E/Z isomer mixture and/or a tautomer thereof in each case in free form or in aqrochemically utilizable salt form, as active ingredient and at least one auxiliary, can used for pest control.Type: GrantFiled: February 13, 2001Date of Patent: July 9, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: Friedrich Karrer, Roger Graham Hall
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Patent number: 6403794Abstract: The invention relates to novel substituted 2-amino-4-alkylamino-1,3,5-triazines of the formula (I) in which R1 represents in each case optionally substituted alkyl having 2 to 6 carbon atoms or cycloalkyl having 3 to 6 carbon atoms, R2 represents hydrogen or represents alkyl having 1 to 4 carbon atoms, A represents oxygen or methylene, Ar represents in each case optionally substituted phenyl, naphthyl or heterocyclyl, and Z represents hydrogen, represents halogen or represents in each case optionally substituted alkyl, alkoxy, alkylcarboxyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, alkenyl or alkinyl, to processes and to novel intermediates for their preparation and to their use as herbicides.Type: GrantFiled: April 5, 2001Date of Patent: June 11, 2002Assignee: Bayer AktiengesellschaftInventors: Hans-Jochem Riebel, Stefan Lehr, Uwe Stelzer, Yukiyoshi Watanabe, Markus Dollinger
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Patent number: 6362205Abstract: Described are substituted cyanoenamines of formula I wherein Z, R1, R2 and R3 are defined in the description, compositions thereof and methods for preparing these compounds. These compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinologic system.Type: GrantFiled: March 16, 2001Date of Patent: March 26, 2002Assignee: Novo Nordisk A/SInventors: John Bondo Hansen, Tina Moller Tagmose, John Patrick Mogensen, Florencio Zaragoza Dorwald, Anker Steen Jorgensen
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Patent number: 6313339Abstract: Certain cyclopropyl oxime ethers substituted by aryl and heterocyclic moieties possess broad spectrum fungicidal and insecticidal properties. These compounds are disclosed along with compositions containing these compounds and methods for controlling fungi and insects by the use of a fungitoxic or insecticidal amount of these compounds.Type: GrantFiled: February 17, 2000Date of Patent: November 6, 2001Inventors: Ronald Ross, Jr., Duyan Vuong Nguyen, Steve Howard Shaber
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Patent number: 6306798Abstract: A composition, which comprises at least one compound of the formula in which A1, A2, R1 and R2 are as defined in claim 1, or, if appropriate, an E/Z isomer, an E/Z isomer mixture and/or a tautomer thereof, in each case in free form or in agrochemically utilizable salt form, as active ingredient and at least one auxiliary, can used for pest control.Type: GrantFiled: January 21, 1999Date of Patent: October 23, 2001Assignee: Syngenta Crop Protection, Inc.Inventors: Friedrich Karrer, Roger Graham Hall
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Patent number: 6156923Abstract: The invention relates to a process for the preparation of compounds of the formula ##STR1## or, if appropriate, a tautomer thereof, in each case in the free form or in salt form, in whichA, X, Y, Z, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7, R.sub.9 and n are as defined in claim 1 and the C.dbd.N double bond marked with E has the E configuration, which comprisesa1) reacting either a compound of the formula (II) mentioned above with a compound of the formula (III) mentioned above, in which X.sub.1 is a leaving group, ora2) a compound of the formula (IV) mentioned above, if appropriate in the presence of a base, with a compound of the formula (V) mentioned above, orb1) reacting a compound of the formula (VI) mentioned above with a compound of the formula R.sub.7 --A--X.sub.2 (VII), in which X.sub.Type: GrantFiled: December 6, 1996Date of Patent: December 5, 2000Assignee: Novartis CorporationInventors: Saleem Farooq, Stephan Trah, Hugo Ziegler, Rene Zurfluh
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Patent number: 6077866Abstract: Novel benzophenonehydrazone derivatives represented by the formula (I): ##STR1## wherein, R.sup.1 is halogen; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is cyano, optically substituted C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-4 alkynyl, C.sub.1-4 alkyl-carbonyl or C.sub.1-4 alkoxy-thiocarbonyl; R.sup.4 is hydrogen, phenyl, optionally substituted C.sub.1-6 alkyl, optionally substituted C.sub.2-8 alkenyl, --CO--R.sup.8, --CO--O--R.sup.9 or ##STR2## R.sup.5 is hydrogen, formyl, phenyl, optionally substituted C.sub.1-8 alkyl, optionally substituted C.sub.2-8 alkenyl, optionally substituted C.sub.3-8 alkynyl, optionally substituted C.sub.1-8 alkyl-arbonyl, optionally substituted C.sub.1-6 alkyl-oxalyl, optionally substituted C.sub.1-8 alkoxy-carbonyl, optionally substituted C.sub.1-8 alkoxy-oxalyl, optionally substituted C.sub.3-8 cycloalkyl-carbonyl, optionally substituted C.sub.2-8 alkenyl-carbonyl or optionally substituted benzoyl; R.sup.6 is hydrogen or halogen; R.sup.7 is hydrogen, halogen or C.sub.Type: GrantFiled: May 10, 1996Date of Patent: June 20, 2000Assignee: Nihon Bayer Agrochem K.K.Inventors: Yoshinori Kitagawa, Katsuaki Wada, Yoshiko Kyo, Yuichi Otsu, Yumi Hattori, Toru Obinata, Takahisa Abe, Katsuhiko Shibuya, Wolfram Andersch
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Patent number: 6063813Abstract: Cyanoiminooxime ethers of the formula I ##STR1## wherein X is NOCH.sub.3, CHOCH.sub.3 or CHCH.sub.3 ;Y is O or NZ where Z is hydrogen or alkyl;R.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl;R.sup.2 is cyano, nitro, halogen, alkyl, trifluoromethyl or alkoxy;m is 0, 1 or 2;R.sup.3 is hydrogen, cyano, alkyl, haloalkyl, alkoxy or cycloalkyl;R.sup.4 is hydrogen, orunsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl or hetaryl,or a salt thereof, their preparation, intermediates for their preparation, and their use for controlling harmful fungi and animal pests.Type: GrantFiled: June 25, 1998Date of Patent: May 16, 2000Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Ruth Muller, Hubert Sauter, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Muller, Klaus Oberdorf, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6043282Abstract: Azinooxime ethers of the formula I ##STR1## (X=NOCH.sub.3, CHOCH.sub.3, CHCH.sub.3 ; Y=O, NZ, where Z=H, alkyl; R.sup.1 =H, alkyl; R.sup.2 =cyano, nitro, trifluoromethyl, halogen, alkyl, alkoxy; m=0, 1, 2, it being possible for the radicals R.sup.2 to be different if m=2; R.sup.3 =H, cyano, alkyl, haloalkyl, alkoxy, cycloalkyl; R.sup.4, R.sup.5, R.sup.6 =indepedently of one another H, unsubst. or subst. alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl), and their salts, processes and intermediates for their preparation and their use for controlling harmful fungi and animal pests.Type: GrantFiled: July 29, 1998Date of Patent: March 28, 2000Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Klaus Oberdorf, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Muller, Ruth Muller, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6013606Abstract: Substituted cinnamic oxime derivatives I and cinnamic hydroxamide derivatives II ##STR1## (R.sup.1= halogen, NO.sub.2, CN, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3= H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, hydroxy-C.sub.1 -C.sub.6 -alkyl;R.sup.4= H, halogen, CN, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl orR.sup.3 +R.sup.4 =chemical bond;Y=--O--, --S--, --O--CO--, --O--SO.sub.2 -- or chemical bond;Y'=--O-- or --S--;R.sup.5= unsubst. or subst. C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -haloalkyl; C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, unsubst. or subst. phenyl or phenyl-C.sub.1 -C.sub.6 -alkyl, or, if Y is --O--, --S-- or a chemical bond, is (C.sub.1 -C.sub.6 -alkyl)carbonyl or (C.sub.1 -C.sub.6 -alkoxy)carbonyl; or, if Y is a chemical bond, is hydrogen or halogen;R.sup.5 '=R.sup.5, H or (C.sub.1 -C.sub.6 -haloalkyl)carbonyl;R.sup.6= H, C.sub.1 -C.Type: GrantFiled: June 30, 1997Date of Patent: January 11, 2000Assignee: BASF AkteingesellschaftInventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schafer, Christoph-Sweder von dem Bussche-Hunnefeld, Peter Munster, Reinhard Kirstgen, Albrecht Harreus, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 5994359Abstract: 2-Iminooxyphenylacetic acid derivatives ##STR1## where the substituents and the index have the following meanings: R.sup.1 is C(CO.sub.2 CH.sub.3).dbd.NOCH.sub.3 (Ia), C(CONHCH.sub.3).dbd.NOCH.sub.3 (Ib), C(CONH.sub.2).dbd.NOCH.sub.3 (Ic), C(CO.sub.2 CH.sub.3).dbd.CHOCH.sub.3 (Id) or C(CO.sub.2 CH.sub.3).dbd.CHCH.sub.3 (Ie);R.sup.2 is cyano, nitro, halogen, alkyl, haloalkyl or alkoxy;m is 0, 1 or 2;R.sup.3 is hydrogen, cyano, hydroxyl, halogen,alkyl, haloalkyl, alkoxyalkyl, alkoxy, haloalkoxy, alkylthio, cyclopropyl, alkenyl,unsubstituted or substituted aryloxyalkyl, benzyl or benzyloxy,R.sup.4 is hydrogen, cyano,unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and hetaryl;unsubstituted or substituted alkoxy, alkenyloxy, alkynyloxy, cycloalkoxy, heterocyclyloxy, aryloxy and hetaryloxy;unsubstituted or substituted arylthio and hetarylthio;--Q--C(R.sup.5).dbd.N--Y.sup.1 --R.sup.6 or --Q--O--N.dbd.CR.sup.7 R.sup.8,R.sup.3 and R.sup.Type: GrantFiled: June 25, 1998Date of Patent: November 30, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Grote, Hubert Sauter, Reinhard Kirstgen, Herbert Bayer, Ruth Muller, Bernd Muller, Klaus Oberdorf, Wassilios Grammenos, Norbert Gotz, Michael Rack, Albrecht Harreus, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 5965613Abstract: The present invention relates to aromatic compounds, namely substituted methyl 2-phenyl-3-methoxy-acrylates of the general formula ##STR1## where X represents an aldimino or ketimino group, in particular a group ##STR2## where R.sup.1 and R.sup.2 independently of one another denote hydrogen, C.sub.1-12 -alkyl, C.sub.1-4 -haloalkyl, and C.sub.1-4 -alkoxy-C.sub.1 -C.sub.4 -alcyl.Type: GrantFiled: September 22, 1997Date of Patent: October 12, 1999Assignee: Novartis Finance CorporationInventors: Hans P. Isenring, Stephan Trah, Bettina Drechsel
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Patent number: 5892095Abstract: Disclosed is a novel positive-working or negative-working chemical-sensitization photoresist composition useful in the photolithographic patterning works for the manufacture of electronic devices. The photoresist composition is characterized by a unique acid-generating agent capable of releasing an acid by the pattern-wise exposure of the resist layer to actinic rays so as to increase or decrease the solubility of the resist layer in an aqueous alkaline developer solution. The acid-generating agent proposed is a novel cyano group-containing oxime sulfonate di- or triester compound represented by the general formulaA?C(CN).dbd.N--O--SO.sub.2 --R!.sub.n,in which each R is, independently from the others, an unsubstituted or substituted monovalent hydrocarbon group such as alkyl groups, A is a divalent or tervalent organic group or, preferably, phenylene group and the subscript n is 2, when A is a divalent group, or 3, when A is a tervalent group or, preferably 2.Type: GrantFiled: January 30, 1997Date of Patent: April 6, 1999Assignee: Tokyo Ohka Kogyo Co., Ltd.Inventors: Hideo Hada, Hiroshi Komano, Toshimasa Nakayama
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Patent number: 5847005Abstract: The present invention relates to benzamidoxime derivatives represented by the formula ?I!; ##STR1## wherein R.sup.1 is unsubstituted or substituted C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted C.sub.2 -C.sub.4 alkenyl or unsubstituted or substituted C.sub.2 -C.sub.4 alkynyl, R.sup.2 is phenyl optionally having substituents or heterocycle optionally having substituents, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are each independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylthio or the like, and r.sub.1 and r.sub.2 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl or the like, having excellent fungicidal activity and being useful as a fungicide for agricultural and horticultural use, and methods for preparation thereof.Type: GrantFiled: August 14, 1997Date of Patent: December 8, 1998Assignee: Nippon Soda Co., Ltd.Inventors: Isamu Kasahara, Hirohito Ooka, Shinsuke Sano, Hiroyasu Hosokawa, Homare Yamanaka
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Patent number: 5811456Abstract: Novel monoamine oxidase B inhibitors of formula (I), wherein R.sub.1 .dbd.H, an optionally substituted benzyloxy or phenylethoxy group; p=0-3; R.sub.3 .dbd.H, a CN, OH, CCH group, a C.sub.1 -C.sub.3 alkoxy-carbonyl group, or a C.sub.1 -C.sub.3 alkylated cyanomethyl group; R.sub.2 .dbd.H or a C.sub.1 -C.sub.3 alkyl group; n=0 or 1; if n=0, R.sub.4 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3 alkoxy group, while if n=1, y=1 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group, a C.sub.1 -C.sub.3 alkoxy group or a phenyl group. The invention also concerns processes for the preparation of said novel inhibitors and the therapeutic use thereof.Type: GrantFiled: August 6, 1996Date of Patent: September 22, 1998Assignees: Laboratoires Mayoly Spindler, Michel SemanInventors: Michel Seman, Suzanne Bernard, Rene Milcent, Catherine Paillat
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Patent number: 5763618Abstract: A method of manufacturing a sulfide comprises the steps of (a) dissolving a thiol in a solvent to form a solution; (b) oxidizing the thiol to a disulfide in the presence of a first oxidizing agent in the solution; (c) reacting the disulfide with a coupler in the presence of a base and a second oxidizing agent, without isolation of said disulfide from the solution, to form a reaction mixture in which the sulfide is produced; and (d) obtaining said sulfide.Type: GrantFiled: April 29, 1996Date of Patent: June 9, 1998Assignee: Konica CorporationInventors: Ryuzou Watanabe, Shinri Tanaka, Katsuji Ota, Michiko Nagato, Tomio Horiuchi
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Patent number: 5756426Abstract: Described herein are compounds of the formula I ##STR1## and the isomers thereof, in which either a) X is an N atom andY is OR.sub.11 or N(R.sub.12)R.sub.13, orb) X is CH andY is OR.sub.11,and in which furthermore:R.sub.11 is C.sub.1 -C.sub.4 alkyl;R.sub.12 and R.sub.13, independently, are hydrogen or C.sub.1 -C.sub.4 alkyl;A is an O atom or the group NR.sub.4 ; and whereinR.sub.1, R.sub.2 and R.sub.3 are as defined herein, are pesticidal active ingredients. They can be used for pest control, in particular as microbicides, insecticides and acaricides in agriculture, horticulture and in the hygiene sector.Type: GrantFiled: September 11, 1995Date of Patent: May 26, 1998Assignee: Novartis CorporationInventors: Hugo Ziegler, Stephan Trah, Saleem Farooq, Rene Zurfluh
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Patent number: 5721277Abstract: The present invention features compounds and methods for inhibiting hyper-proliferative cell growth. The compounds and method are preferably used to treat patients having a hyper-proliferative cell disorder.Type: GrantFiled: April 21, 1995Date of Patent: February 24, 1998Assignee: Sugen, Inc.Inventor: Peng Cho Tang
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Patent number: 5696161Abstract: Substituted phenoxymethylphenyl derivatives I ##STR1## X is .dbd.CH--OCH.sub.3, .dbd.CH--CH.sub.3 or .dbd.N--OCH.sub.3 ; R.sup.1 is, inter alia,R.sup.2 and R.sup.3 are, inter alia,H, halogen, CN, NO.sub.2, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.2 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.2 -haloalkoxy;R.sup.4 is, inter alia,CN, Cl, Br, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio or C.sub.1 -C.sub.4 -haloalkoxy;R.sup.5 is, inter alia,NO.sub.2, CN, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -haloalkoxy;n is 0-4; Y is --O--, --NH--, --N(CH.sub.3)--; R.sup.6 is H, C.sub.1 -C.sub.4 -alkyl.The compounds are useful for controlling pests and fungi.Type: GrantFiled: May 13, 1996Date of Patent: December 9, 1997Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Klaus Oberdorf, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Harald Rang, Volker Harries, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5629441Abstract: 2-(Arylimino-methyl)-3-dialkylaminoacrylonitriles can be obtained by reaction of .beta.-anilino-acrylonitriles with ortho-formamides. They are suitable as starting substances for the preparation of 4-amino-5-iminiummethylene-2-pyrimidines or 4-amino-5-formyl-2-pyrimidines.Type: GrantFiled: August 11, 1995Date of Patent: May 13, 1997Assignee: Bayer AktiengesellschaftInventors: Helmut Kraus, Horst Behre, Helmut Fiege
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Patent number: 5591833Abstract: Colorants and compositions useful as a fugitive or permanent colorant for a variety of substrates, or as intermediates for their manufacture, and having one or more improved properties of enhanced aqueous washability, compatibility with and non-extractibility from thermoplastic resins, or reactivity with resins having reactive functionality, said composition having the formula C(Z).sub.Type: GrantFiled: August 10, 1993Date of Patent: January 7, 1997Assignee: Milliken Research CorporationInventors: John B. Hines, David J. Moody, Edward W. Kluger
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Patent number: 5545664Abstract: Substituted phenoxymethylphenyl derivatives I ##STR1## X is .dbd.CH--OCH.sub.3, .dbd.C--CH.sub.3 or .dbd.N--OCH.sub.3 ; R.sup.1 is, inter alia,R.sup.2 and R.sup.3 are, inter alia,H, halogen, CN, NO.sub.2, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.2 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 --C.sub.2 -haloalkoxy;R.sup.4 is, inter alia,CN, Cl, Dr, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio or C.sub.1 -C.sub.4 -haloalkoxy;R.sup.5 is, inter alia,NO.sub.2, CN, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -haloalkoxy;n is 0-4; Y is --O--, --NH--, --N(CH.sub.3)--; R.sup.6 is H, C.sub.1 -C.sub.4 -alkyl.The compounds are useful for controlling pests and fungi.Type: GrantFiled: March 23, 1995Date of Patent: August 13, 1996Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Klaus Oberdorf, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Harald Rang, Volker Harries, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5493053Abstract: A new and versatile route to N'-[5-[[4-[[5-(acetylhydroxyamino)pentyl]amino]-1,4-dioxobutyl]hydroxyamin o]pentyl]-N-(5-aminopentyl)-N-hydroxybutanediamide, desferrioxamine B (DFO) is described. N-Benzyloxy-1,5-diaminopentane is selectively protected at the primary amino site. The product is reacted at the benzyloxyamine with an anhydride to produce a carboxylic acid which is, in turn, acylated regio-specifically with a diamine at the primary amine to give a benzyloxyamine. The previous two steps are repeated to afford a DFO reagent. Acetylation of the DFO reagent, followed by hydrogenolysis and tert-butoxycarbonyl group removal, furnishes DFO.Type: GrantFiled: December 21, 1994Date of Patent: February 20, 1996Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 5489605Abstract: Cyanooxime ethers of the formula IR.sup.1 R.sup.2 CH--ON.dbd.C(CN)--R.sup.3 IwhereR.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl;R.sup.2 is an unsubstituted or substituted mononuclear to trinuclear aliphatic or aromatic ring system which, in addition to carbon atoms, may contain from one to four nitrogen atoms or from one to three hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen andR.sup.3 is unsubstituted or substituted alkyl or an unsubstituted or substituted aliphatic ring system which, in addition to carbon atoms, may contain one or two hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen,processes for their preparation, agents containing them and their use.Type: GrantFiled: August 24, 1994Date of Patent: February 6, 1996Assignee: BASF AktiengesellschaftInventors: Klaus Oberdorf, Uwe Kardorff, Hans Theobald, Albrecht Harreus, Hartmann Koenig, Volker Harries
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Patent number: 5476935Abstract: Dye-donor element for use according to thermal dye transfer comprising least one dye corresponding to the general formula (I): ##STR1## wherein Z is --CN, --COOR.sup.1 or --CONR.sup.2 R.sup.3 ; R.sup.1 is --H, (cyclo)alkyl, or aryl; R.sup.2 and R.sup.3 is --H, (cyclo)alkyl, aryl, or R.sup.2 and R.sup.3 together represent the atoms necessary to complete a heterocyclic nucleus; R.sup.4 and R.sup.5 is --H, (cyclo)alkyl, aryl, a heterocyclic ring, SO.sub.2 R.sup.8, COR.sup.8, CSR.sup.8, POR.sup.8 R.sup.9, OR.sup.6, NR.sup.6 R.sup.7, SR.sup.6, or R.sup.4 and R.sup.5 together represent the atoms necessary to complete a aliphatic ring, a heterocyclic ring including a heterocyclic ring carrying a fused-on aliphatic or aromatic ring; R.sup.6 and R.sup.7 is (cyclo)alkyl, aryl, alkenyl, aralkyl, aryl, a heterocyclic group, or R.sup.6 and R.sup.7 together represent the atoms necessary to complete a 5- or 6-membered ring; R.sup.8 and R.sup.Type: GrantFiled: May 18, 1994Date of Patent: December 19, 1995Assignee: Agfa-Gevert, N.V.Inventors: Luc Vanmaele, Hans Junek, Renate Dworczak
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Patent number: 5468870Abstract: Dye-donor element for use according to thermal dye sublimation transfer comprising a support having thereon a dye layer containing a dye corresponding to the following formula ##STR1## wherein Z represents CN, COOR.sup.1 or CONR.sup.2 R.sup.3 ;R.sup.1, R.sup.2 and R.sup.3 each independently represent hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, or R.sup.2 and R.sup.3 together represent the necessary atoms to close a heterocyclic nucleus or substituted heterocyclic nucleus;Y represents OR.sup.4 or NR.sup.5 R.sup.6 or CN;R.sup.4 represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, SO.sub.2 R.sup.7, COR.sup.7, CSR.sup.7, POR.sup.7 R.sup.8 ;R.sup.5 and R.sup.6 each independently has one of the significances given to R.sup.4 or represent substituted or unsubstituted amino, or R.sup.5 and R.sup.Type: GrantFiled: October 20, 1994Date of Patent: November 21, 1995Assignee: AGFA-GAVAERT, N.V.Inventor: Luc J. Vanmaele
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Patent number: 5426231Abstract: This invention relates to an improved process for the preparation of 3-aminopropanol and a primary amine by reacting a cyanoethyl ketoxime with hydrogen in the presence of a hydrogenation catalyst to generate the primary amine and aminopropanol. The sequence of reactions to form the aminopropanol and primary amine involves the reaction of hydroxylamine with a ketone to generate a ketoxime followed by reaction of acrylonitrile with the ketoxime to generate a cyanoethyl ketoxime followed by complete hydrogenation of the cyanoethyl ketoxime in the presence of a hydrogenation catalyst to generate the primary amine and aminopropanol. The significant advantage associated with this process is the high degree of selectivity to 3-aminopropanol and the primary amine.Type: GrantFiled: January 5, 1994Date of Patent: June 20, 1995Assignee: Air Products and Chemicals, Inc.Inventors: Richard V. C. Carr, Barry J. Koehler
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Patent number: 5395853Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, orPh(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, orR.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, orR.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; ##STR2## Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.Type: GrantFiled: November 24, 1993Date of Patent: March 7, 1995Assignee: Burroughs Wellcome Co.Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
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Patent number: 5387607Abstract: O-Benzyloxime ethers of the formula I ##STR1## where X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: December 13, 1993Date of Patent: February 7, 1995Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5371084Abstract: Compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.Type: GrantFiled: October 28, 1993Date of Patent: December 6, 1994Assignee: Zeneca LimitedInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5367113Abstract: Synthesis of desferrioxamine B and analogs and homologs thereof beginning with O-protected, N-protected hydroxylamine, which is N-alkylated to produce a protected N-4-cyanoalkylhydroxylamine which is acylated with a suitable anhydride. The resulting half-acid amide is subjected to a series of high yield condensations and reductions which vide desferrioxamine B in high overall yield. Alternatively, polyether analogs of desferrioxamine B can be prepared by reacting an activated polyether with the O-protected, N-protected hydroxylamine and subjecting the resulting product to a series of similar steps.Type: GrantFiled: June 23, 1993Date of Patent: November 22, 1994Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 5358968Abstract: Substituted oxime ethers of the general formula I ##STR1## where R.sup.1 is alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, cyanoalkyl, alkoxycarbonylalkyl, arylalkyl, heteroarylalkyl, arylalkenyl or aryloxyalkyl, the aromatic or heteroaromatic ring being substituted or unsubstituted,R.sup.2 and R.sup.3 are hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, halogen, cyano or nitro,R.sup.4 is hydrogen, alkyl, cycloalkyl, haloalkyl or aryl, the aromatic ring being substituted or unsubstituted, andR.sup.5 and R.sup.6 are identical or different and each is hydrogen or alkyl, andX is CH or N, and fungicides and pesticides containing these compounds.Type: GrantFiled: July 15, 1993Date of Patent: October 25, 1994Assignee: BASF AktiengesellschaftInventors: Klaus Oberdorf, Hubert Sauter, Wassilios Grammenos, Reinhard Kirstgen, Volker Harries, Gisela Lorenz, Eberhard Ammermann, Randall E. Gold, Wolfgang Siegel, Albrecht Harreus
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Patent number: 5294616Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: March 25, 1992Date of Patent: March 15, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
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Patent number: RE37839Abstract: O-Benzyloxime ethers of the formula I wherein 5 x is substituted or unsubstituted CH2, NOalkyl Y is O, S, NR5 R1, R2, R5 are H, alkyl Z1, Z2 are H, halogen, methyl, methoxy, cyano R3, R4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl substituted or unsubstituted benzyloxycarbonyl, N(R6)2, where R6 is H, alkyl, substituted or unsubstituted phenyl, —CO—N(R7)2, where R7 is H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aryloxy, substituted or unsubstituted arylthio, substituted or unsubstituted hetaryl, substituted or unsubstituted hetaryloxy, substituted or unsubstituted hetarylthio, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocyclyloxy, R3 and R4 together may form a caType: GrantFiled: April 5, 1996Date of Patent: September 10, 2002Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus