Patent Number: 6,169,086

Title: Pyrazole derivatives

Abstract: The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): ##STR1## wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: ##STR2## These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)-1 piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-prope ne hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.

Inventors: Ejima; Akio (Tokyo, JP), Ohsuki; Satoru (Tokyo, JP), Ohki; Hitoshi (Tokyo, JP), Naito; Hiroyuki (Tokyo, JP)

Assignee: Daiichi Pharmaceutical Co., Ltd.

International Classification: C07D 403/14 (20060101); C07D 403/04 (20060101); C07D 471/00 (20060101); C07D 417/00 (20060101); C07D 231/00 (20060101); C07D 231/12 (20060101); C07D 417/04 (20060101); C07D 401/00 (20060101); C07D 403/00 (20060101); C07D 401/04 (20060101); C07D 471/04 (20060101); C07D 487/00 (20060101); C07D 487/04 (20060101); C07D 498/00 (20060101); C07D 498/04 (20060101); C07D 231/12 (); C07D 401/04 (); C07D 417/04 (); A61K 031/495 (); A61K 031/505 ()

Expiration Date: 01/02/2018