Global Patent Index - EP 1075484 A1

EP 1075484 A1 20010214 - NOVEL ANTHRACYCLINE DERIVATIVES AND THEIR PREPARATION

Title (en)

NOVEL ANTHRACYCLINE DERIVATIVES AND THEIR PREPARATION

Title (de)

NEUE ANTHRACYCLINE UND IHRE HERSTELLUNG

Title (fr)

NOUVEAUX DERIVES D'ANTHRACYCLINE ET LEUR PREPARATION

Publication

EP 1075484 A1 20010214 (EN)

Application

EP 99919679 A 19990507

Priority

  • KR 9900220 W 19990507
  • KR 19980016348 A 19980507

Abstract (en)

[origin: WO9957126A1] Disclosed are novel anthracycline derivatives, represented by formula (I), (wherein R1 and R4 which may be the same or different, each is a hydrogen atom, methoxy or hydroxy; R2 is L-aspartate or pyruvate; and R3 is a hydrogen atom or fluorine atom), which have potent antitumor activity against a broad spectrum of tumors with greatly reduced cardiac toxicity, and a preparation method therefor. The compounds can complement the NAD/NADH ratio balance in vivo to control the activity of oxygen radical-producing enzymes. The compounds can be prepared by linking L-aspartate or pyruvate via an ester bond to the position 14 of conventional anthracycline glycosides. By virtue of the potent activity and pharmaceutical safety, the compounds can be used as pharmaceutically effective ingredients for antitumoral agents.

IPC 1-7

C07H 15/252; A61K 31/70

IPC 8 full level

A61K 31/7028 (2006.01); A61K 31/7034 (2006.01); A61K 31/704 (2006.01); A61P 35/00 (2006.01); C07H 15/252 (2006.01)

CPC (source: EP KR)

A61P 35/00 (2017.12 - EP); C07H 1/00 (2013.01 - KR); C07H 15/252 (2013.01 - EP KR)

Citation (search report)

See references of WO 9957126A1

Designated contracting state (EPC)

DE ES FR GB IT

DOCDB simple family (publication)

WO 9957126 A1 19991111; EP 1075484 A1 20010214; JP 2002513797 A 20020514; KR 100398289 B1 20030919; KR 19990084528 A 19991206; KR 20010043400 A 20010525

DOCDB simple family (application)

KR 9900220 W 19990507; EP 99919679 A 19990507; JP 2000547095 A 19990507; KR 19980016348 A 19980507; KR 20007012427 A 20001107