PYRAZOLYL DERIVATIVE AND ITS PRODUCTION

Japanese Patent JP2848375

B2

PROBLEM TO BE SOLVED: To obtain the subject derivative, an 1,3,5-triphenylpyrazolyl derivative, having arachidonic acid metabolic route-inhibitory activity, and useful as e.g. an agent for mitigating inflammation, asthma, anaphylaxis, myocardial ischemia, dermatitis, gastroenteritis, etc.
SOLUTION: This new pyrazolyl derivative is shown by formula I [R1 to R4 are each H, a lower alkyl, lower alkoxy, amino, acetamide, phenyl, halo or OH, R1 and R2 or R3 and R4 are combined together with a phenyl group to be bound to them into a (substituted) naphthyl, etc.; X is a lower alkoxy; R5 to R8 are each H; R9 is OH or OR10 (R10 is a lower alkyl, etc.)], having arachidonic acid metabolic route-inhibitory activity and being useful as e.g. a nonsteroidal antiinflammatory agent. This compound of formula I is obtained by the following process: dihydroxyacetophenone of formula II is alkylated and then reacted with phenylhydrazone to form a hydrazone of formula III (R is a lower alkyl), which is, in turn, reacted with a benzoic ester to form a pyrazole compound of formula IV, which is then converted to the corresponding alcohol derivative, which is then oxidized.

UIRIAMU BUI MAREI
MAIKERU PII WAKUTAA

JP6172497A

January 20, 1999

March 03, 1997

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ORUSO PHARM CORP

A61K31/415; A61K31/44; A61K31/4427; A61K31/443; A61K31/4433; A61P11/00; A61P17/00; A61P29/00; C07C45/59; C07C49/82; C07C51/00; C07C59/76; C07C59/88; C07C62/22; C07C62/38; C07C65/32; C07C65/34; C07C67/00; C07C201/00; C07C205/56; C07C227/00; C07C227/02; C07C229/42; C07C229/54; C07C229/64; C07C231/00; C07C231/12; C07C233/54; C07C313/00; C07C317/44; C07C317/46; C07C317/48; C07C317/50; C07C323/62; C07D231/12; C07D401/06; C07D405/06; C07D409/06; C07D409/10; (IPC1-7): C07D231/12

Heiyoshi Odashima

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