HUP0100619A2 - Mikrobicidális és növényimmunizáló hatású tiazol-, izotiazol- és tiadiazolszármazékok, intermedierjeik és alkalmazásuk - Google Patents

Mikrobicidális és növényimmunizáló hatású tiazol-, izotiazol- és tiadiazolszármazékok, intermedierjeik és alkalmazásuk

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Publication number
HUP0100619A2
HUP0100619A2 HU0100619A HUP0100619A HUP0100619A2 HU P0100619 A2 HUP0100619 A2 HU P0100619A2 HU 0100619 A HU0100619 A HU 0100619A HU P0100619 A HUP0100619 A HU P0100619A HU P0100619 A2 HUP0100619 A2 HU P0100619A2
Authority
HU
Hungary
Prior art keywords
amino
alkyl
carbonyl
general formula
atoms
Prior art date
Application number
HU0100619A
Other languages
English (en)
Inventor
Philippe Chemla
Peter Ertl
Thomas Maetzke
Original Assignee
Novartis Ag.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag. filed Critical Novartis Ag.
Publication of HUP0100619A2 publication Critical patent/HUP0100619A2/hu
Publication of HUP0100619A3 publication Critical patent/HUP0100619A3/hu

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D275/00Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/02Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings
    • C07D275/03Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A01N43/74Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,3
    • A01N43/781,3-Thiazoles; Hydrogenated 1,3-thiazoles
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A01N43/80Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,2
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A01N43/82Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with three ring hetero atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/30Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/061,2,3-Thiadiazoles; Hydrogenated 1,2,3-thiadiazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Dentistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

A találmány tárgyát vegyületek és eljárás növények fitopatogénmikroorganizmusok támadása elleni védelmére és immunizálására képezi,ahol az eljárás során egy olyan (I) általános képletű vegyületetalkalmazunk, amelynek általános képletében a) X jelentése CR4általános képletű csoport és Y jelentése nitrogénatom, Z jelentése egyegy szénatomot tartalmazó csoport, amelyben a szénatomhoz 1-3halogénatom vagy 1-3 szubsztituált heteroatom kapcsolódik, amelynél aheteroatomok oxigénatom, kénatom vagy nitrgénatom lehetnek, R1, R2 ésR4 jelentése egymástól függetlenül hidrogén-, halogénatom, hidroxi-,merkapto-, ciano-, karboxi-, nitro-, amino-, adott esetbenszubsztituált alkil-, alkoxi-amino-alkil-, alkanoil-oxi-, aroiloxi-,alkoxi-karbonil-, ariloxi-karbonil-, benziloxi-karbonil-, alkil-karbonil-, aril-karbonil, benzil-karbonil-, amino-karbonil-, alkil-amino-karbonil-, dialkil-amino-karbonil-, alkil-tio-, alkil-szulfinil,alkil-szulfonil-, aril--szulfinil-, aril-szulfonil-, alkenil-,alkinil-, karboxi-alkinil-, alkoxi--karbonil-alkil-, cikloalkil-,alkanoil-alkil-, alkil-, alkil-karbonil-oxi-alkil-, fenil-karbonil-oxi-alkil-, alkil-amino-, dialkil-amino-, alkenil-amino-, alkanoil-amino-, alkoxi-karbonil-amino-, benzil-amino-, benzoil-amino-, benzil-oxi-karbonil-amino-, fenil-, fenoxi-, benzil-, vagy fenetil-csoport,vagy Rl és R2 jelentése adott esetben helyettesített heterociklusoscsoport vagy trialkil-szilil-vagy trialkil-szilil-oxi-csoport. Ó
HU0100619A 1997-12-22 1998-12-18 Thiazole-, isothiazole- and thiadiazole-derivatives having microbicidal and plant immunizing activities, intermediates and use thereof HUP0100619A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9726989.8A GB9726989D0 (en) 1997-12-22 1997-12-22 Organic compounds
PCT/EP1998/008335 WO1999032464A1 (en) 1997-12-22 1998-12-18 Thiazole-, isothiazole- and thiadiazole-derivatives having microbicidal and plant immunizing activities

Publications (2)

Publication Number Publication Date
HUP0100619A2 true HUP0100619A2 (hu) 2001-06-28
HUP0100619A3 HUP0100619A3 (en) 2002-03-28

Family

ID=10823994

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0100619A HUP0100619A3 (en) 1997-12-22 1998-12-18 Thiazole-, isothiazole- and thiadiazole-derivatives having microbicidal and plant immunizing activities, intermediates and use thereof

Country Status (15)

Country Link
EP (1) EP1042306A1 (hu)
JP (1) JP2001526277A (hu)
CN (1) CN1282324A (hu)
AR (1) AR017438A1 (hu)
AU (1) AU2054699A (hu)
BR (1) BR9814394A (hu)
CA (1) CA2309973A1 (hu)
GB (1) GB9726989D0 (hu)
GT (1) GT199800193A (hu)
HU (1) HUP0100619A3 (hu)
IL (1) IL136589A0 (hu)
PL (1) PL341290A1 (hu)
TR (1) TR200001740T2 (hu)
WO (1) WO1999032464A1 (hu)
ZA (1) ZA9811706B (hu)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6310052B1 (en) 1996-06-04 2001-10-30 Queen's University At Kingston Nitrate esters and their use for neurological conditions
WO2001087863A1 (de) * 2000-05-15 2001-11-22 Basf Aktiengesellschaft 3-arylisothiazole und ihre verwendung als herbizide
DE10029077A1 (de) * 2000-06-13 2001-12-20 Bayer Ag Thiazolylsubstituierte Heterocyclen
HUP0303829A3 (en) 2001-04-16 2006-02-28 Tanabe Seiyaku Co Large conductance calcium-acitvated k channel opener compounds, use thereof and pharmaceutical compositions containing them
US6699866B2 (en) 2001-04-17 2004-03-02 Sepracor Inc. Thiazole and other heterocyclic ligands for mammalian dopamine, muscarinic and serotonin receptors and transporters, and methods of use thereof
GB0712653D0 (en) 2007-06-28 2007-08-08 Syngenta Ltd Novel herbicides
GB0717082D0 (en) 2007-09-03 2007-10-10 Syngenta Ltd Novel herbicides
US20110144067A1 (en) * 2009-12-07 2011-06-16 Toscano John P N-Acyloxysulfonamide and N-Hydroxy-N-Acylsulfonamide Derivatives
CN102753519B (zh) 2009-12-07 2015-08-05 约翰斯霍普金斯大学 二酰基化的羟基胺衍生物
CA2800626A1 (en) * 2010-05-27 2011-12-01 Bayer Intellectual Property Gmbh Heterocyclic alkanol derivatives as fungicides
BR112012030208A2 (pt) * 2010-05-27 2015-09-29 Bayer Intelectual Property Gmbh derivados de alcanol heterocíclicos como fungicidas
BR112012030186B1 (pt) 2010-05-27 2017-12-19 Bayer Intellectual Property Gmbh Alcanol heterocyclic derivatives, its uses, a composition and its preparation process, and a process for combating phytopathogenic harmful fungi
EP2508511A1 (en) * 2011-04-07 2012-10-10 Laboratoire Biodim Inhibitors of viral replication, their process of preparation and their therapeutical uses
CN102417505B (zh) * 2011-08-29 2014-07-09 南开大学 含甲基-1,2,3-噻二唑的四氮唑类化合物及其制备方法和用途
CN108752287A (zh) * 2018-05-21 2018-11-06 南开大学 一类杂环叔醇衍生物的制备方法和用途
CN108912108B (zh) * 2018-06-27 2021-09-03 中国科学院上海有机化学研究所 三氟甲基化合物及其制备方法及其在农药中的应用
CN113214241A (zh) * 2021-04-29 2021-08-06 华东理工大学 一种用于检测十字花科蔬菜核盘菌的化合物及其应用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1953861C2 (de) * 1969-10-25 1982-12-23 Fujisawa Pharmaceutical Co., Ltd., Osaka 7-Tetrazolylacetamido-3-thiomethyl-3-cephem-4- carbonsäuren
BE793037A (fr) * 1971-12-23 1973-06-20 Fujisawa Pharmaceutical Co Procede de preparation de derives d'acide 7-acylamino-3-substitue-3-cephem-4-carboxylique et nouveaux produits ainsi obtenus
US4851029A (en) * 1985-08-23 1989-07-25 Ciba-Geigy Corporation Thiazolylalkyl esters of α-imidazolinonenicotinic acids and herbicidal methods of use
US5135927A (en) * 1987-01-30 1992-08-04 Ciba-Geigy Corporation Microbicidal composition
CA2014880A1 (en) * 1989-04-27 1990-10-27 Indu Sawhney Thiazole derivatives
JP3726306B2 (ja) * 1994-04-27 2005-12-14 日産化学工業株式会社 ピラゾールカルボン酸誘導体および植物病害防除剤
WO1996017840A1 (en) * 1994-12-06 1996-06-13 Agrevo Uk Limited Heterocyclyl substituted hydroxyacetamide derivatives as fongicides
MY113237A (en) * 1995-03-31 2001-12-31 Nihon Nohyaku Co Ltd An agricultural and horticultural disease controller and a method for controlling the diseases
DE19545638A1 (de) * 1995-12-07 1997-06-12 Bayer Ag Verwendung von 1,2,3-Thiadiazolcarbonsäure(thio)estern zur Bekämpfung von Schädlingen
WO1998014437A1 (fr) * 1996-09-30 1998-04-09 Nihon Nohyaku Co., Ltd. Derives de 1,2,3-thiadiazole et sels de ces derives, agents en usage dans l'agriculture et l'horticulture pour lutter contre les maladies vegetales, et procede d'utilisation correspondant

Also Published As

Publication number Publication date
CN1282324A (zh) 2001-01-31
GT199800193A (es) 2000-05-25
BR9814394A (pt) 2000-10-10
CA2309973A1 (en) 1999-07-01
TR200001740T2 (tr) 2000-11-21
HUP0100619A3 (en) 2002-03-28
IL136589A0 (en) 2001-06-14
PL341290A1 (en) 2001-04-09
GB9726989D0 (en) 1998-02-18
AR017438A1 (es) 2001-09-05
AU2054699A (en) 1999-07-12
JP2001526277A (ja) 2001-12-18
ZA9811706B (en) 1999-06-22
EP1042306A1 (en) 2000-10-11
WO1999032464A1 (en) 1999-07-01

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