Claims
- 1. A compound selected from those of formula (I): in whichX and Y, which may be identical or different, each independently of the other represents a group selected from hydrogen, halogen, hydroxy, mercapto, cyano, nitro, linear or branched (C1-C6)alkyl, linear or branched (C1-C6)alkoxy, linear or branched (C1-C6)trihaloalkyl, and amino which is optionally substituted by one or two, identical or different, linear or branched (C1-C6)alkyl which are themselves optionally substituted by linear or branched (C1-C6)alkoxy or by —NR7R8 wherein R7 and R8, which may be identical or different, each independently of the other represents hydrogen or linear or branched (C1-C6)alkyl, or X and Y together form methylenedioxy or ethylenedioxy, R1 represents hydrogen or linear or branched (C1-C6)alkyl, R2 represents a group selected from: hydrogen, hydroxy, linear or branched (C1-C6)alkyl, linear or branched (C1-C6)alkoxy which is optionally substituted: by NR′7R′8 wherein R′7 and R′8, which may be identical or different, each independently of the other represent a group selected from hydrogen, linear or branched (C1-C6)alkyl, and linear or branched (C1-C6)hydroxyalkyl, or by a saturated or unsaturated, monocyclic or bicyclic heterocycle having 5 to 7 ring members, and containing one or two hetero atoms selected from oxygen, nitrogen, and sulphur, linear or branched (C1-C6)alkylcarbonyloxy, and amino which is optionally substituted: by one or two, identical or different, linear or branched (C1-C6)alkyl, by linear or branched (C1-C6)alkylcarbonyl which is optionally substituted by —NR′7R′8 wherein R′7 and R′8 are as defined above, by —R9—NR′7R′8 wherein R9 represents linear or branched (C1-C6)alkylene and R′7 and R′8, which may be identical or different, each independently of the other represents a group selected from hydrogen, linear or branched (C1-C6)alkyl, and linear or branched (C1-C6)hydroxyalkyl, by linear or branched (C1-C6)alkylene which is substituted by a saturated or unsaturated, monocyclic or bicyclic heterocycle having 5 to 7 ring members and containing one or two hetero atoms selected from oxygen, nitrogen, and sulphur, or by wherein R9 is as defined above, and R10 represents hydroxy or linear or branched (C1-C6)alkoxy,R3 and R4, which may be identical or different, each independently of the other represents hydrogen or linear or branched (C1-C6)alkyl, A represents —CH═CH—, or ethylene with the formula —CH(R5)—CH(R6) wherein R5 and R6, which may be identical or different, each independently of the other represents: hydrogen, hydroxy, linear or branched (C1-C6)alkoxy, linear or branched (C1-C6)alkylcarbonyloxy, arylcarbonyloxy, amino optionally substituted by one or two, identical or different, linear or branched (C1-C6)alkyl, or linear or branched (C1-C6)acyl, mercapto, linear or branched (C1-C6)alkylthio, or arylthio, or R5 and R6 together form: wherein Z represents oxygen or sulphur,—O—(CH2)n—O— wherein n is 1 to 4 inclusibve, (C1-C6)alkylene or linear (C2-C6)alkylene, or R5 and R6 form, together with the carbons carrying them, oxirane or azirideine, optionally substituted on nitrogen by linear or branched (C1-C6)alkyl, wherein the term “aryl” denotes phenyl or naphthyl, optionally containing one or more, identical or different, substituents selected from hydroxy, halogen, carboxy, nitro, amino, linear or branched (C1-C6)alkylamino, linear or branched di-(C1-C6)alkylamino, linear or branched (C1-C6)alkoxy, linear or branched (C1-C6)acyl, and linear or branched (C1-C6)alkylcarbonyloxy,its optical isomers, diastereomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof.
- 2. A compound of claim 1, wherein R3 and R4, which may be identical or different, represent linear or branched (C1-C6)alkyl.
- 3. A compound of claim 1, wherein that R2 represents linear or branched (C114 C6)alkoxy, or amino which is optionally substituted
- 4. A compound of claim 1, wherein R2 represents amino substituted by —R9—NR7R8 wherein R9 represents linear or branched (C1-C6)alkylene, and R7 and R8, which may be identical or different, represent hydrogen or linear or branched (C1-C6)alkyl, its isomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof.
- 5. A compound of claim 1, wherein A represents —CH═CH—, or —CH(R5)—CH(R6)— wherein R5 and R6 represent hydroxy, linear or branched (C1-6)alkylcarbonyloxy, or R5 and R6 together form
- 6. A compound of claim 1 which is (±)-cis-1,2diacetoxy-&methoxy-3,3,14-trimethyl-2,3,7,14-tetrahydro-1H-benzo[b]pymano[3,2-h]-acridin-7-one.
- 7. A compound of claim 1 which is cis-7-methoxy-4,4,15-trimethyl-3a,8,15,15c-tetrahydro-4H-benzo[b][1,3]dioxolo[4′,5′:4,5]pyrano[3,2-h]acridine-2,8dione.
- 8. A compound of claim 1 which is 6-methoxy-3,3,14-trimethyl-7,14-dihydro-3H-benzo[b]pyrano[3,2-h]acridin-7-one.
- 9. A compound of claim 1 which is 6-(diethylaminopropylamino)-3,3,14-trimethyl-7,14-dihydro-3H-benzo[b]pyrano[3,2-h]acridin-7-one.
- 10. A compound of claim 1 which is (±)-cis-diacetoxy-6-(diethylaminopropylamino)-3,3,14-trimethyl-2,3,7,14-tetrahydro-1H-benzofpyrano[3,2-h]acridin-7-one.
- 11. A method for treating a living body afflicted with a cancer susceptible to treatment with acronycine, comprising the step of administering to the living body in need thereof an amount of a compound of claim 1 which is effective for alleviation of said cancer.
- 12. A pharmaceutical composition comprising compound as claimed in claim 1, together with one or more pharmaceutically-acceptable excipients or vehicles.
Priority Claims (1)
Number |
Date |
Country |
Kind |
97 16131 |
Dec 1997 |
FR |
|
Parent Case Info
The present application is a U.S. National Application filed under 35 USC 371 of PCT/FR98/02785 filed Dec. 18, 1998 based upon French application Serial No. 97.16131 filed Dec. 19, 1997.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
102e Date |
371c Date |
PCT/FR98/02785 |
|
WO |
00 |
6/19/2000 |
6/19/2000 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO99/32491 |
7/1/1999 |
WO |
A |
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
5567707 |
Koch |
Oct 1996 |
|
Non-Patent Literature Citations (2)
Entry |
Elomri A et al. J. Med. Chem. 1996, 39(24), 4762-4764.* |
A. Elomri et al., “Synthesis and Cytotoxic and Antitumor Activity of Esters in the 1,2-Dihydroxy-1,2-Dihydroacronycine Series”, Journal of Medicinal Chemistry, vol. 39, No. 24 (1996) pp. 4762-4764. |