Aziridinyl-epothilone compounds

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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C548S962000

Reissue Patent

active

RE042930

ABSTRACT:
The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having the following Formula:wherein K is —O—, —S—, or —NR7—; A is —(CR8R9)—(CH2)m—Z—wherein Z is —(CHR10)—, —C(═O)—, —C(═O)—C(═O)—, —OC(═O)—, —N(R11)C(═O)—, —O2—, or —N(R11)SO2—; B1is hydroxyl or cyano and R1is hydrogen or B1and R1are taken together to form a double bond; R2, R3, and R5are, independently, hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; or R2and R3may be taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl; R4is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl; R6is hydrogen, alkyl or substituted alkyl; R7, R8, R9, R10, R11and R12are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or substituted heteroaryl; and R13is aryl, substituted aryl, heteroaryl or substituted heteroaryl.

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