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Title:
PHENOXYACETIC ACID AND PHENOXYMETHYLITETRAZOLE DERIVATIVE EACH HAVING ANTITUMOR ACTIVITY
Document Type and Number:
Japanese Patent JP2000063340
Kind Code:
A
Abstract:

To obtain the subject new phenoxyacetic acid and phenoxymethyltetrazole derivative each functioning as an antagonist in the interaction between MDM2 and p 53, inducing the growth of an active p 53 in cells, and enabling a p 53 protein to accelerate an apoptosis in cancerous cells.

This compound is of formula I [A is e.g. -COOH, -COO-, CN or an 1-4C alkyl; (p) is 0, 1 or 2; R1 and R2 are each e.g. H or an 1-8C alkyl; R4 is e.g. Cl, Br, I, F, an 1-8C alkyl or a hydroxy; (n) is an integer of 1 to 4; (m) is 0 or 1; and B is e.g. an 1-10C alkyl or -CO-C(R3)=CH-R (R is e.g. H; and R3 is H or 1-8C alkyl)], e.g. a compound of formula II. A compound of formula I wherein (m) is 0 and B is e.g. an 1-10C alkyl or -COCH3 can be prepared by beginning with the use of an intermediary of formula III [B' is e.g. an 1-10C alkyl, -COCH3 or -CO-C(R3)-CH-R] and subsequently using an appropriate acid ester or nitrile.


Inventors:
DI DOMENICO ROBERTO
SILKE HANSEN
BRIGITTE CALZA
MENTA ERNESTO
RALF SCHUMACHER
Application Number:
JP8793299A
Publication Date:
February 29, 2000
Filing Date:
March 30, 1999
Export Citation:
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Assignee:
HOFFMANN LA ROCHE
International Classes:
A61K31/00; A61K31/19; A61K31/192; A61K31/24; A61K31/41; A61P35/00; A61P43/00; C07C45/62; C07C45/74; C07C49/83; C07C49/835; C07C59/90; C07C69/712; C07C235/76; C07D257/04; (IPC1-7): C07C235/76; A61P35/00; A61P43/00; A61K31/192; A61K31/24; A61K31/41; C07D257/04
Attorney, Agent or Firm:
Hajime Tsukuni (2 outside)