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Spliceostatina analogs and Methods for their Preparation
专利权人:
PFIZER INC.
发明人:
申请号:
ARP130104017
公开号:
AR093339A1
申请日:
2013.11.04
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
This report deals with Cytotoxicology and analogues of derivatives, their antibody pharmacological combinations, and methods for treating medical diseases, including cancer. 1. Claim 1: a formula compound (1),Where: a dotted line represents an optional link; each X1 is selected independently from the following groups:-S-Y-NREach square kilometer is selected independently from a group consisting of:-S-Y-NRR1 was selected from the following groups: R, O, ocor 3,-OCONR¹⁴R¹⁵,-OCON (R) NR (R)=O (double connection with oxygen) y-nr.8308; R1 83099;R² and R³ are independently selected from the group consisting of: hydrogen and C₁₋₆-alkyl;R⁴ and R⁵ are independently selected from the group consisting of: hydrogen, -OR, -NR¹⁴R¹⁵ and oxo; R⁶ and R⁷ are independently selected from the group consisting of: hydrogen, halogen, hydroxyl, and C₁₋₆-alkyl optionally substituted with 1-3 substituents, independently selected from hydroxyl and halogen, R⁶ and R⁷ together form with the carbon atom to which they are attached, a C₂₋₅-alkylidene optionally substituted with 1-3 substituents independently selected from R, R⁶ and R⁷ together are oxo or R⁶ and R⁷ form, together with the carbon atom at that are linked,a 3- to 5-membered heterocycloalkyl moiety comprising 1 or 2 heteroatoms independently selected from the group consisting of oxygen, nitrogen and sulfur, wherein said heterocycloalkyl moiety may optionally be substituted with one to three selected substituents, from R independent mode; R⁸ is hydrogen, C₁₋₆-alkyl or -OR; R⁹ is independently selected from hydrogen, -alkyl C₁₋₆,- (C (R)) -C (O) OR - (C (R)) -C (O) NR R- (C (R)) -NR R- (C (R)) -N (R) COR- (C (R)) -C (O) -SR - (C (R)) -C (O) NR N (R) R- (C (R)) -NR-C (O) -NR R y - (C (R)) -NR N (R) RR3 was selected from the hydrogen group, tar c83215331;carbocyclyl C₃₋₈,C₃₋₈ heterocyclyl,C₁₋₆-alkyl C₆₋₁₄-aryl,C₁₋₆-alkyl-C₅₋₁₄-heteroaryl,Among them, R1 cubic meter is selected by - NRR o-so8322;; NRR; each r8308 and r183099 is selected fro
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