Synthetic antineoplastic agents derived from dolastatin 15...

Details Synthetic antineoplastic agents derived from dolastatin 15... Synthetic antineoplastic agents derived from dolastatin 15...

C - Chemistry, Metallurgy

07

K

C07K 11/00 (2006.01) A61K 38/04 (2006.01) A61K 38/15 (2006.01) A61P 35/00 (2006.01) C07K 7/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2298639

A composition of matter, denominated herein as 12a-r, having structural formula (12a-r) wherein R is selected from the group consisting of: a) R = NHPh; (CH3O)2Ph; b) R = NHCH2Ph; c) R = NH(CH2)2Ph; d) R = NH(CH2)2-4-F Ph; e) R = NH(CH2)2-4-Cl-Ph; f) R = NH(CH2)2-3-Cl-Ph; g) R = NH(CH2)2-2-Cl-Ph; h) R = NH(CH2)2-4-Br Ph; i) R = NH(CH2)2-4-NO2-Ph; j) R = NH(CH2)2-3,4-; k) R = NH(CH2)2-pyridine; 1) R = NH(CH2)3Ph; m) R = L-Phe-OCH3; n) R = L-Met- OCH3; o) R = L-Pro-OCH3; p) R = NH-2-thiazolyl; q) R = NH-2-benzothiazolyle; r) R = NH-3-quinolyl; and methods of making these compounds 12a-r.

L'invention concerne une composition de matière, appelée ici 12a-r, de formule structurale (12a-r), dans laquelle R est choisi dans le groupe formé de: a) R = NHPh; (CH3O)2Ph; b) R = NHCH2Ph; c) R = NH(CH2)2Ph;d) R = NH(CH2)2-4-F-Ph; e) R = NH(CH2)2-4-Cl-Ph; f) R=NH(CH2)2-3-Cl-Ph; g) R = NH(CH2)2-2-Cl-Ph; h) R = NH(CH2)2-4-Br-Ph;i) R = NH(CH2)2-4-NO2-Ph; j) R = NH(CH2)2-3-4-; k) R = NH(CH2)2-2-pyridine; l) R = NH(CH2)3Ph; m) R = L-Phe-OCH3; n) R = L-Met-OCH3; o) R = L-Pro-OCH3: p) R = NH-2-thiazolyle; q) R = NH-2-benzothiazolyle; r) R = NH-3-quinolyle. L'invention porte aussi sur des procédés de fabrication desdits composés 12a-r.

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