DOROSKI, MATTHEW DAVID,MADERNA, ANDREAS,O&APOSDONNELL, CHRISTOPHER JOHN,SUBRAMANYAM, CHAKRAPANI,VETELINO, BETH COOPER,DUSHIN, RUSSELL GEORGE,STROP, PAVEL,GRAZIANI, EDMUND IDRIS
申请号：
PE0007082014
公开号：
PE17902014A1
申请日:
2012.11.07
申请国别(地区):
PE
年份:
2014
代理人:
摘要：
Relates to compounds of formula (i) where W is the compound (R1) n (R2) - C (R3A) (r3b) - C (o) - N (R1), (R2) - C (R4A) (r4b) - C (R3A) (r3b) - C (o) -, among others, where R1 and R2 are each h, alkyl (C8 (C1) or haloalquilo C1 C8) R3A is H, alkyl, aryl (C1 C8), among others, r3b is alkyl (C8, haloalquilo C1 (C1) - carbociclilo (C8), C3, C8), among others and R4A r4b are each h, alkyl (C8, C1)Carbociclilo (C3, C8), among others R5 is heterociclilo (C1 - C10), carbociclilo (C3 - aryl (C6, C8) 14C), among others X is o or S.Preferred compounds are: N - methyl - l-valyl - N - [(3R, 4S, 5S) - 3 - methoxy - 1 - ((2S) - 2 - [(1R, 2R) - 1 - methoxy - 3 - methyl - 2 - {[(1S) - phenyl - 2 - 1 - (1,3 - thiazol-2-yl) ethyl] amino} - 3 - tioxopropil pyrrolidin-1-yl]} - 5 - methyl - 1 - oxoheptan - 4-yl] - N - methyl - L - valinamide N2 - [(1 - aminociclopentil) carbonyl] - N - [(3R, 4S, 5S) - 3 - methoxy - 1 - ((2S) - 2 - [(1 R, 2R) - 1 - methoxy - 3 - methyl - 2 - {[(1S) - 2 - phenyl - (1, - 13 - thiazol-2-yl) ethyl] amino} - 3 - tioxopropil pyrrolidin-1-yl]} - 5 - methyl - 1 - oxoheptan - 4-yl] - N - methyl - L - valinamide among others. It also relates to a Pharmaceutical composition. These compounds are cytotoxic polypeptides are useful in the treatment of cancerSE REFIERE A COMPUESTOS DE FORMULA (I) DONDE W ES EL COMPUESTO N(R1)(R2)-C(R3A)(R3B)-C(O)-, N(R1)(R2)-C(R4A)(R4B)-C(R3A)(R3B)-C(O)-, ENTRE OTROS, EN DONDE R1 Y R2 SON CADA UNO H, ALQUILO(C1-C8) O HALOALQUILO(C1-C8) R3A ES H, ALQUILO(C1-C8), ARILO, ENTRE OTROS R3B ES ALQUILO(C1-C8), HALOALQUILO(C1-C8), CARBOCICLILO(C3-C8), ENTRE OTROS R4A Y R4B SON CADA UNO H, ALQUILO(C1-C8), CARBOCICLILO(C3-C8), ENTRE OTROS R5 ES HETEROCICLILO(C1-C10), CARBOCICLILO(C3-C8), ARILO(C6-C14), ENTRE OTROS X ES O U S. SON COMPUESTOS PREFERIDOS: N-METIL-L-VALIL-N-[(3R,4S,5S)-3-METOXI-1-{(2S)-2-[(1R,2R)-1-METOXI-2-METIL-3-{[(1S)-2-FENIL-1-(1,3-TIAZOL-2-IL)ETIL]AMINO}-3-TIOXOPROPIL]PIRROLIDIN-1-IL}-5-METIL-1-OXOHEPTAN-4-IL]-N-METIL-L-VALINAM
