フェニルピリ(ミ)ジニラゾール類

Japanese Patent JP2013507334

A

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-(trimethylstannyl)-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-methyl-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]pyrimidin-2-amine, 4-(5-methyl-3-phenyl-1H-pyrazol-4-yl)pyrimidin-2-amine and [4-(2-aminopyrimidin-4-yl)-3-(3-chloro-5-hydroxyphenyl)-1H-pyrazol-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%.

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Sudow, Alexander
S-Side, Marzen
Brown, Christoph Andreas
Musener, Ruth
Servane, Catherine
Bentain, Yoga
Damen, Peter
Portis, Daniela
Wuerhendorf-Neumann, Ulrike
Devold, philip
Vannavi, Samil
Kissarin, Christoph
Levstock, Anne-Sophie
Gross Jean-Cournoyer, Marie-Clair
Hiroyuki Hatano
Novrotsk, thomas
Linorhuy, Philip

JP2012532558A

March 04, 2013

October 04, 2010

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BAYER CROPSCIENCE AG

C07D401/04; A01N43/56; A01P3/00; C07D231/16; C07D403/04; C07D405/06; C07D405/14; C07D409/14; C07D417/14; C07D471/04; C07D473/00; C07D487/04; C07D495/04

JPS6388179A	1988-04-19
JP2007535558A	2007-12-06
JP2009525350A	2009-07-09
JP2002284782A	2002-10-03
JP2007217322A	2007-08-30
JPH10503201A	1998-03-24
JP2002508754A	2002-03-19
JP2009530261A	2009-08-27
JP2004531456A	2004-10-14
JP2009521492A	2009-06-04
JP2006501183A	2006-01-12

WO2009086041A1	2009-07-09
US7074801B1	2006-07-11
US3040047A	1962-06-19
US4957971A	1990-09-18
DE602004000260T2	2006-08-24
US6525059B1	2003-02-25
WO2004029043A1	2004-04-08
WO2003015781A1	2003-02-27
WO2004083814A2	2004-09-30
WO2001030154A2	2001-05-03
WO2003049542A1	2003-06-19

JPN5012017179; ＳＬＩＳＫＯＶＩＣ　Ｄ　Ｒ: 'ＩＮＨＩＢＩＴＯＲＳ　ＯＦ　ＣＨＯＬＥＳＴＥＲＯＬ　ＢＩＯＳＹＮＴＨＥＳＩＳ．６．ＴＲＡＮＳ-６-［２-（（２-Ｎ-ＨＥＴＲＯＡＲＹＬ-３，５-以下備考' ＪＯＵＲＮＡＬ　ＯＦ　ＭＥＤＩＣＩＮＡＬ　ＣＨＥＭＩＳＴＲＹ Ｖ３５　Ｎ１１, 19920501, Ｐ２０９５-２１０３, ＡＭＥＲＩＣＡＮ　ＣＨＥＭＩＣＡＬ　ＳＯＣＩＥＴＹ
JPN5012017178; ＶＥＲＨＯＥＳＴ　Ｐ　Ｒ: 'ＤＩＳＣＯＶＥＲＹ　ＯＦ　Ａ　ＮＯＶＥＬ　ＣＬＡＳＳ　ＯＦ　ＰＨＯＳＰＨＯＤＩＥＳＴＥＲＡＳＥ　１０Ａ　ＩＮＨＩＢＩＴＯＲＳ　ＡＮＤ　ＩＤＥＮＴＩＦＩＣＡＴＩＯＮ　以下備考' ＪＯＵＲＮＡＬ　ＯＦ　ＭＥＤＩＣＩＮＡＬ　ＣＨＥＭＩＳＴＲＹ Ｖ５２　Ｎ１６, 20090827, Ｐ５１８８-５１９６, ＡＭＥＲＩＣＡＮ　ＣＨＥＭＩＣＡＬ　ＳＯＣＩＥＴＹ
JPN5012017177; ＴＡＮＧ　Ｊ: 'ＫＮＯＷＬＥＤＧＥ-ＢＡＳＥＤ　ＤＥＳＩＧＮ　ＯＦ　７-ＡＺＡＩＮＤＯＬＥＳ　ＡＳ　ＳＥＬＥＣＴＩＶＥ　Ｂ-ＲＡＦ　ＩＮＨＩＢＩＴＯＲＳ' ＢＩＯＯＲＧＡＮＩＣ　＆　ＭＥＤＩＣＩＮＡＬ　ＣＨＥＭＩＳＴＲＹ　ＬＥＴＴＥＲＳ Ｖ１８　Ｎ１６, 20080815, Ｐ４６１０-４６１４, ＥＬＳＥＶＩＥＲ　ＳＣＩＥＮＣＥ
JPN6014041975; Ｉｂｒａｈｉｍ　Ｍ．　Ｅｌ-Ｄｅｅｂ，　ｅｔ　ａｌ．: 'Ｄｅｓｉｇｎ，　ｓｙｎｔｈｅｓｉｓ，　ｓｃｒｅｅｎｉｎｇ，　ａｎｄ　ｍｏｌｅｃｕｌａｒ　ｍｏｄｅｌｉｎｇ　ｓｔｕｄｙ　ｏｆ　ａ　ｎｅｗ　ｓｅｒｉｅｓ　ｏｆ　ＲＯＳ１　ｒｅｃｅｐｔｏｒ　ｔｙｒｏｓｉｎｅ' Ｂｉｏｏｒｇａｎｉｃ　＆　Ｍｅｄｉｃｉｎａｌ　Ｃｈｅｍｉｓｔｒｙ　Ｌｅｔｔｅｒｓ Ｖｏｌ．１９，　Ｎｏ．１９, 20090812, ｐｐ．５６２２-５６２６
JPN6014041976; Ｊｅｆｆｒｅｙ　Ｍ．　Ｒａｌｐｈ，　ｅｔ　ａｌ．: 'Ｔｗｏ　ｃｏｎｖｅｎｉｅｎｔ　ｒｅｇｉｏｓｅｌｅｃｔｉｖｅ　ｓｙｎｔｈｅｓｅｓ　ｏｆ　１-Ｎ-ａｌｋｙｌ-３-ａｒｙｌ-４-［ｐｙｒｉｍｉｄｉｎ-４-ｙｌ］-ｐｙｒａｚｏｌｅｓ' Ｔｅｔｒａｈｅｄｒｏｎ　Ｌｅｔｔｅｒｓ　（２００９）， Ｖｏｌ．５０，　Ｎｏ．１３, 20090113, ｐｐ．１３７７-１３８０

Yoshikazu Iwase
Makoto Ono
Kenkyo Kanayama
Mitsuaki Tsubokura
Kazuki Shigemori
Kenji Ando
Yasufumi Shiroyama

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