JP6189434B2 - ピリミジンピラゾリル誘導体 - Google Patents

ピリミジンピラゾリル誘導体 Download PDF

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JP6189434B2
JP6189434B2 JP2015520844A JP2015520844A JP6189434B2 JP 6189434 B2 JP6189434 B2 JP 6189434B2 JP 2015520844 A JP2015520844 A JP 2015520844A JP 2015520844 A JP2015520844 A JP 2015520844A JP 6189434 B2 JP6189434 B2 JP 6189434B2
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pyrazol
mmol
phenyl
methyl
formula
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JP2015522045A (ja
JP2015522045A5 (enExample
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クロジニャーニ,ステファノ
ジョランド−ルブラン,カトリーヌ
ガーバー,パトリック
ミュゼリー,マティルデ
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アレス トレーディング ソシエテ アノニム
アレス トレーディング ソシエテ アノニム
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