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2 277 534

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IPC

C07D401/14(2006-01-01)

A61K31/506(2006-01-01)

A61P29/00(2006-01-01)

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Application

2004108857/04, 2002-09-25

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Start date

2002-09-25

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Actual filing date

2002-09-25

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Published

2006-06-10

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Inventor

Allen Kimberli K.Anderson Dennis K.Boldus Dzhon E.Klark Dzherri D.D'Juksherer Dehn R.Idni Albert D.Lau Patrik Kh.Mao Majkl K.Makdermott Liza L.Mo Dzhodi L.M'Judipalli Parta S.Naing VinShilke Tobin S.Selness Shaun R.Sejmur Kristin B.Visvanat ShekkharUolker Dzhon K.Jalamanchili Gopi

(73)

Holder

Farmatsija Korporejshn

METHOD FOR PREPARING SUBSTITUTED PYRAZOLES Russian patent published in 2006 - IPC C07D401/14 A61K31/506 A61P29/00 

Abstract RU 2277534 C2

FIELD: organic chemistry, chemical technology, biochemistry.

SUBSTANCE: invention relates to a method for preparing substituted pyrazoles of the formula (I) , tautomers of substituted pyrazoles and salts of substituted pyrazoles and tautomers wherein R3A, R3B, R3C, Y1, Y2, Y3, Y4 and Y5 are determined in the invention description. Prepared pyrazoles show ability to inhibit activity of kinase p38, activity of TNF and/or cyclooxygenase. Method involves formation of mixture by addition of hydrazone of the formula (II) and optionally substituted benzoyl halide of the formula (III) into reactor and heating the mixture to temperature above 50°C and the following formation of the composite wherein above 30 wt.-% of the composite consists of the protected intermediate pyrazole compound of the formula (IV) and unsubstituted intermediate piperidinyl compound of the formula (V) , and interaction of glycolic acid ester with unsubstituted piperidinyl intermediate compound. Invention provides enhancing quality of synthesized pyrazoles.

EFFECT: improved preparing method.

34 cl, 6 tbl, 2 ex

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RU 2 277 534 C2

Authors

Allen Kimberli K.

Anderson Dennis K.

Boldus Dzhon E.

Klark Dzherri D.

D'Juksherer Dehn R.

Idni Albert D.

Lau Patrik Kh.

Mao Majkl K.

Makdermott Liza L.

Mo Dzhodi L.

M'Judipalli Parta S.

Naing Vin

Shilke Tobin S.

Selness Shaun R.

Sejmur Kristin B.

Visvanat Shekkhar

Uolker Dzhon K.

Jalamanchili Gopi

Dates

2006-06-10—Published

2002-09-25—Filed

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