Global Patent Index - EP 1075484 A1

EP 1075484 A1 2001-02-14 - 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 (EN)

Application

EP 99919679 A

Priority

  • KR 9900220 W
  • KR 19980016348 A

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 (main, further and additional classification)

C07H 15/252; A61K 31/70

IPC 8 full level (invention and additional information)

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 (invention and additional information)

C07H 15/252 (2013.01)

Citation (search report)

See references of WO 9957126A1

Designated contracting state (EPC)

DE ES FR GB IT

EPO simple patent family

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

INPADOC legal status


2003-07-30 [18D] DEEMED TO BE WITHDRAWN

- Effective date: 20030121

2002-08-28 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20020710

2001-06-13 [RAP1] TRANSFER OF RIGHTS OF AN EP PUBLISHED APPLICATION

- Owner name: METABOLIC ENGINEERING LABORATORIES CO., LTD.

2001-06-13 [RIN1] INVENTOR (CORRECTION)

- Inventor name: PARK, SANG CHUL

2001-06-13 [RIN1] INVENTOR (CORRECTION)

- Inventor name: KANG, HEUN SOO, 707-101, HWASEONG VILLAGE

2001-06-13 [RIN1] INVENTOR (CORRECTION)

- Inventor name: RHO, YOUNG, S.

2001-02-14 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20001207

2001-02-14 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): DE ES FR GB IT