Pyrazole derivatives
US6169086A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jul 23, 1999 |
| Grant date | Jan 2, 2001 |
| Priority date | — |
| Expiry date | Jul 23, 2019 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D487/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.