Water-soluble shps as novel alkylating agents

Details Water-soluble shps as novel alkylating agents Water-soluble shps as novel alkylating agents

A - Human Necessities

61

K

A61K 38/16 (2006.01) A61K 38/04 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) A61K 38/08 (2006.01) C07C 323/39 (2006.01) C07F 9/38 (2006.01) C07K 5/04 (2006.01) C07K 5/06 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) C07K 14/00 (2006.01)

Patent

CA 2525091

The present invention relates to compounds according to the structure (I): Where R is -CH3 or -CH2CH2CI; R' is C1-C7alkyl or -CH2CH2C1; R2 or R4 is OPO3H2, NO2, OCO(Glu-OH), NHCO(Glu-OH), NHR7 and unassigned groups of R2, R3, R4, R5 and R6 are, independently, H, F, Cl, Br, I, OH, OPO3H2, OCH3, CF3, OCF3, NO2, CN, SO2CH3, SO2CF3, COCH3, COOCH3, SCH3, SF5, NH2, NHR7, N(CH3)2, OP03H2, or a C1-C7 alkyl group with the proviso that when any two of unassigned groups of R2, R3, R4, R5 or R6 are other than H, the other two of unassigned groups of R2, R3, R4, R5 or R6 are H. R7 is H or polyglutamyl as described. Phosphoric acid and glutamic acid can be a free acid or pharmaceutically acceptable salt thereof.

La présente invention concerne des composés représentés par la structure (I). Dans cette formule, R est -CH¿3? ou -CH¿2?CH¿2?CI; R' est C¿1?-C¿7? alkyle ou -CH¿2?CH¿2?C1; R¿2? ou R¿4? est OPO¿3?H¿2?, NO¿2?, OCO(Glu-OH), NHCO(Glu-OH), NHR¿7?, le groupes non assignés parmi R¿2?, R¿3?, R¿4?,¿ ?R¿5? et R¿6 ?étant indépendamment H, F, Cl, Br, I, OH, OPO¿3?H¿2?, OCH¿3?, CF¿3?, OCF¿3?, NO¿2?, CN, SO¿2?CH¿3?, SO¿2?CF¿3?, COCH¿3?, COOCH¿3?, SCH3, SF¿5?, NH¿2?, NHR¿7?, N(CH¿3?)¿2?, OP0¿3?H¿2?, ou un groupe C¿1?-C¿7? alkyle, mais avec cette réserve que, lorsque deux au moins des groupes non assignés parmi R¿2?, R¿3?, R¿4?, R¿5? ou R¿6? sont différents de H, les deux autres groupes non assignés parmi R¿2?, R¿3?, R¿4?, R¿5? ou R¿6? doivent être H. R¿7? est H ou polyglutamyle conformément à la description. L'acide phosphorique et l'acide glutamique peuvent être des acides libres ou l'un de leurs sels pharmaceutiquement admis.

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