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    • 2. 发明公开
    • 페닐피리(미)디닐아졸
    • PHENYLPYRI(MI)DINYLAZOLES
    • KR1020120101338A
    • 2012-09-13
    • KR1020127008037
    • 2010-10-04
    • 바이엘 크롭사이언스 악티엔게젤샤프트
    • 수다우알렉산더에스-사예드마젠브라운크리스토프안드레아스마이스너루쓰시르방카트린느벤팅위르겐다멘페터포르츠다니엘라바헨도르프-노이만울리케데스보르데스필리프베나비사미르캐서린크리스토퍼레브스톡앤-소피그로장-쿠노에마리-클레르하다노히로유키크노블로흐토마스리놀피필리프
    • C07D403/14C07D401/14C07D487/04A01N43/56
    • A01N43/56A01N43/84A01N43/90A61K31/415A61K31/44A61K31/495C07D231/12C07D401/04C07D401/14C07D403/04C07D403/14C07D405/14C07D471/04C07D487/04C07F5/02C07F7/2212
    • Phenylpyri(mi)dinylpyrazole compounds (A) and their salts, are new. Phenylpyri(mi)dinylpyrazole compounds (A) of formulae (I) and (II), and their salts, are new. In formula (I): X1 : CH or N; R1 : e.g. 1-benzothiophen-4-yl, 1-benzothiophen-7-yl, 1-benzofuran-4-yl, 1-benzofuran-7-yl, 1,3-benzodioxol-4-yl or 1,3-benzodioxol-5-yl (all optionally one or more times substituted); R2 : e.g. CN, nitro, halo, 2-9C-heterocyclyl or H; R3 : e.g. 1-6C-alkyl, 2-6C-alkenyl, 2-6C-alkynyl or 3-6C-cycloalkyl (all optionally one or more times substituted); R4 : e.g. 1-6C-alkyl, 3-8C-cycloalkyl, 2-6C-alkenyl, 6-14C-aryl, 2-9C-heterocyclyl or 2-9C-heteroaryl (all optionally one or more times substituted), H, halo or CN; and R5, R6 : e.g. 1-6C-alkyl, 6-14C-aryl, S-(1-4C-alkyl), S(O)-(1-6C-alkyl) or C(O)-(1-6C-alkyl) (all optionally one or more times substituted), H, F, Cl, Br, CN, nitro, OH or SH. In formula (II): e.g. X1 : CH or N; R1 : e.g. isoquinolin-5-yl, isoquinolin-8-yl, 1-benzothiophen-4-yl, 1-benzofuran-7-yl or 1,3-benzodioxol-5-yl (all optionally one or more times substituted); R2 : e.g. 1-6C-(halo)alkyl, 3-6C-(halo)cycloalkyl, 2-9C-heterocyclyl or H; R301 : e.g. 1-6C-alkyl, 2-6C-alkenyl, 3-6C-allenyl, 2-6C-alkynyl, 3-8C-cycloalkyl, 1-6C-alkoxy, 2-9C-heterocyclyl, 2-9C-oxo-heterocyclyl or heteroaryl (all optionally one or more times substituted); R401 : NR12R13 or C(O)NR12R13; R5, R6 : e.g. 1-6C-alkyl, 3-6C-cycloalkyl, 2-6C-alkenyl, 2-6C-alkynyl, 6-14C-aryl, S(O)-(1-6C-alkyl) or C(O)-(1-6C-alkyl) (all optionally one or more times substituted); R12 : e.g. C(S)R15, C(O)R15 or SO 2R15; R13 : e.g. 1-6C-alkyl, 3-6C-cycloalkyl, 2-6C-alkenyl or 2-9C-heteroaryl (all optionally one or more times substituted) or H; and R15 : e.g. 1-6C-alkyl, 3-6C-cycloalkyl, 2-6C-alkenyl, 2-6C-alkynyl or 2-9C-heteroaryl (all optionally one or more times substituted), H or OH. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are included for: (1) (hetero)aryl-pyrazole compounds (X) of formulae (XA) and (XB) and their salts; (2) (hetero)aryl-pyrazole compounds (XI) of formulae (XIA) and (XIB) and their salts, where (XI) exclude 1-({4-[1-(2,2-difluoroethyl)-3-(t rimethylstannyl)-1H-pyrazol-4-yl]pyrimidin-2-yl}amino)propan-2-ol; and (3) (hetero)arylamine-pyrazole compounds (III) of formulae (IIIA) and (IIIB) and their salts, where (III) exclude 4-[3-(4-fluorophenyl)-5-m ethyl-1H-pyrazol-4-yl]pyridin-2-amine, 4-[3-(4-chlorophenyl)-5-methyl -1H-pyrazol-4-yl]pyridin-2-amine, 4-[3-(4-methoxyphenyl)-5-methyl-1H- pyrazol-4-yl]pyridin-2-amine, 4-[3-(4-fluorophenyl)-1H-pyrazol-4-yl]p yrimidin-2-amine, 4-(5-methyl-3-phenyl-1H-pyrazol-4-yl)pyrimidin-2-a mine and [4-(2-aminopyrimidin-4-yl)-3-(3-chloro-5-hydroxyphenyl)-1H-p yrazol-1-yl]acetonitrile. PG : tetrahydro-2H-pyran-2-yl; M3 : tributylstannyl, 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl; and PG1 : tetrahydro-2H-pyran-2-yl or 2-(trimethylsilyl)ethoxymethyl. [Image] [Image] [Image] - ACTIVITY : Fungicide; Antibacterial. - MECHANISM OF ACTION : None given. The fungicidal activity of (A) against Botrytis cinereawas tested in cucumber plants. The results showed that 4-[3-(4-fluorophenyl)-1-(2-methylpropyl)-1H-pyrazol-4-yl]pyridine (500 ppm) exhibited an activity of 70%.