Global Patent Index - EP 1240148 A1

EP 1240148 A1 2002-09-18 - BENZO¬A PHENAZIN-11-CARBOXAMIDE DERIVATIVES AND THEIR USE AS JOINT INHIBITORS OF TOPOMERASE I AND II

Title (en)

BENZO¬A PHENAZIN-11-CARBOXAMIDE DERIVATIVES AND THEIR USE AS JOINT INHIBITORS OF TOPOMERASE I AND II

Title (de)

BENZO¬A PHENAZIN-11-CARBOXAMID DERIVATE UND IHRE VERWENDUNG ALS GLEICHZEITIGE INHIBITOREN DER TOPOMERASE I AND II

Title (fr)

DERIVES DE BENZO A PHENAZINE-11-CARBOXAMIDE ET LEUR UTILISATION COMME INHIBITEURS COMMUNS DE LA TOPOMERASE I ET II

Publication

EP 1240148 A1 (EN)

Application

EP 00979799 A

Priority

  • GB 0004609 W
  • GB 9928542 A

Abstract (en)

[origin: WO0146157A1] A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R<1> to R<4>, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1-C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1-C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R<10>, CON(R<12>)2, OCON(R<12>), SR<10>, SOR<11>, SO2(R11), SO2N(R<12>)2, N(R<12>)2, NR<10>SO2R<11>, N(SO2R<11>)2NR<10>(CH2)nCN, NR<10>COR<11>, OCOR<11> or COR<10>; each of R<5> to R<7>, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1-C6 alkoxy, C1-C6 alkyl, SR<10> and N(R<12>)2; Q is C1-C6 alkylene which is unsubstituted or substituted by (i) C1-C6 alkyl which is unsubstituted or substituted, (ii) hydroxy, provided that the hydroxy group is not alpha to either of the N atoms adjacent to Q in formula (I), (iii) CO2R<10>, or (iv) CON(R<12>); R<8> and R<9>, which are the same or different, are each hydrogen or C1-C6 alkyl, or R<8> and R<9> together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered N-containing heterocyclic ring which may include one additional heteroatom selected from O, N and S, or one of R<8> and R<9> is an alkylene chain optionally interrupted by O, N or S, which is attached to a carbon atom on the alkylene chain represented by Q to complete a saturated 5- or 6-membered N-containing heterocyclic ring as defined above; or a pharmaceutically acceptable salt thereof; with the proviso that at least one R<1> to R<4> is other than hydrogen. These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR.

IPC 1-7 (main, further and additional classification)

C07D 241/46; A61K 31/498; C07D 403/12

IPC 8 full level (invention and additional information)

A61K 31/498 (2006.01); A61P 31/04 (2006.01); A61P 31/10 (2006.01); A61P 31/12 (2006.01); A61P 35/00 (2006.01); A61P 43/00 (2006.01); C07D 241/46 (2006.01); C07D 403/12 (2006.01)

CPC (invention and additional information)

C07D 403/12 (2013.01); C07D 241/46 (2013.01)

Citation (search report)

See references of WO 0146157A1

Designated contracting state (EPC)

AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR

EPO simple patent family

WO 0146157 A1 20010628; AU 1718401 A 20010703; AU 784397 B2 20060323; BR 0016093 A 20020820; CA 2392873 A1 20010628; CN 1304380 C 20070314; CN 1433406 A 20030730; EP 1240148 A1 20020918; GB 0215275 D0 20020814; GB 2373499 A 20020925; GB 2373499 B 20041117; GB 9928542 D0 20000202; HK 1046133 A1 20050415; HU 0300392 A2 20030728; HU 0300392 A3 20030929; JP 2003518103 A 20030603; MX PA02005476 A 20030922; MY 136029 A 20080731; PL 356482 A1 20040628; TW I280242 B 20070501; ZA 200204296 B 20030529

INPADOC legal status


2009-04-01 [18D] APPLICATION DEEMED TO BE WITHDRAWN

- Effective date: 20081010

2008-07-02 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20080529

2007-11-07 [RTI1] TITLE (CORRECTION)

- Free text: BENZO??A PHENAZIN-11-CARBOXAMIDE DERIVATIVES AND THEIR USE AS JOINT INHIBITORS OF TOPOMERASE I AND II

2002-12-18 [RIN1] INVENTOR CHANGED BEFORE GRANT

- Inventor name: MILTON, JOHN

2002-12-18 [RIN1] INVENTOR CHANGED BEFORE GRANT

- Inventor name: VICKER, NIGEL

2002-12-18 [RIN1] INVENTOR CHANGED BEFORE GRANT

- Inventor name: FOLKES, ADRIAN, JOHN

2002-12-18 [RIN1] INVENTOR CHANGED BEFORE GRANT

- Inventor name: WANG, SHOUMING

2002-12-18 [RIN1] INVENTOR CHANGED BEFORE GRANT

- Inventor name: DENNY, WILLIAM A., AUCKLAND CANCER RESEARCHCENTRE

2002-09-18 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20020702

2002-09-18 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR

2002-09-18 [AX] REQUEST FOR EXTENSION OF THE EUROPEAN PATENT TO:

- Free text: AL;LT;LV;MK;RO;SI