Title:
【発明の名称】抗増殖性医薬の燐脂質プロドラッグ
Document Type and Number:
Japanese Patent JP2003514770
Kind Code:
A
Abstract:
The invention discloses prodrugs comprising anti-proliferative drugs covalently linked, via bridging group, to a phospholipid moiety such that the active species is preferentially released, preferably by enzymatic cleavage, at the required site of action. The invention further discloses pharmaceutical compositions said prodrugs and the uses thereof for the treatment of diseases and disorders related to inflammatory, to degenerative or atrophic conditions, and to uncontrolled cell growth. FIG. 1 depicts a graph of animal survival during the course of an experiment wherein mice were i.p. transplanted with 11210 mouse leukemia cells and then treated with vehicle only (squares), MTX (triangles) or molar equivalent dose of DP-MTX071 (circles) according to the regiment described example in Example 11.
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Inventors:
Kozak, Alexander
Shapiro, Israel
Vinnikova, Marina
Archob, Leonide
Sendelicin, Alexander
Ayaron, Oran
Shapiro, Israel
Vinnikova, Marina
Archob, Leonide
Sendelicin, Alexander
Ayaron, Oran
Application Number:
JP2001522958A
Publication Date:
April 22, 2003
Filing Date:
September 13, 2000
Export Citation:
Assignee:
D-Farm Limited
International Classes:
A61K9/02; A61K9/06; A61K9/08; A61K9/10; A61K9/12; A61K9/20; A61K9/48; A61K9/72; A61K31/56; A61K31/661; A61K45/00; A61P1/04; A61P9/10; A61P11/06; A61P17/06; A61P19/02; A61P21/00; A61P25/00; A61P25/02; A61P25/06; A61P25/14; A61P25/16; A61P25/28; A61P27/02; A61P29/00; A61P35/00; A61P35/02; A61P37/00; A61P37/02; A61P43/00; A61K47/48; C07F9/6512; C07F9/6524; A61K; C07F; (IPC1-7): A61K47/48; A61K9/02; A61K9/06; A61K9/08; A61K9/10; A61K9/12; A61K9/20; A61K9/48; A61K9/72; A61K45/00; A61P1/04; A61P9/10; A61P11/06; A61P17/06; A61P19/02; A61P21/00; A61P25/00; A61P25/02; A61P25/06; A61P25/14; A61P25/16; A61P25/28; A61P27/02; A61P29/00; A61P35/00; A61P35/02; A61P37/00; A61P37/02; A61P43/00
Domestic Patent References:
| JPS61152694A | 1986-07-11 | |||
| JPS6383093A | 1988-04-13 |
Foreign References:
| WO1996039831A1 | 1996-12-19 | |||
| WO1999042830A1 | 1999-08-26 | |||
| WO1998005349A1 | 1998-02-12 |
Attorney, Agent or Firm:
Akira Asamura (3 outside)