Patent ID: 9493510
Filing Date: 2016-11-15
CPC Classification: A61K,A61P,C07K,G16B,Y02A

Claim Text:
1. A compound of Formula (I): wherein each A, B, C, and E is independently a natural or non-natural amino acid; D is a natural, or non-natural amino acid, amino acid analog, [—NH-L1-CO—], [—NH-L2-SO 2 —] or [—NH-L3-]; W is a natural or non-natural amino acid or amino acid analog where the amino acid side chain contains a warhead; u and z are independently integers from 0-100; v, w, and y are independently integers from 0-10; t is 1, s is 0 or 1, x is 0 or 1, wherein provided s is 0, x is 1, or provided x is 0, s is 1; n is an integer from 1-5; R R L is a macrocycle-forming linker of the formula -L1-L2-L3-; L1, L2 and L3 are independently a bond, alkylene, alkenylene, alkynylene, heteroalkylene, cycloalkylene, heterocycloalkylene, cycloarylene, heterocycloarylene, or [—R4-K—R4-] R3 is hydrogen, alkyl, alkenyl, alkynyl, arylalkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, cycloalkylalkyl, cycloaryl or heterocycloaryl, optionally substituted with R5; each K is independently O, S, SO, SO each R4 is independently alkylene, alkenylene, alkynylene, heteroalkylene, cycloalkylene, heterocycloalkylene, arylene, or heteroarylene; each R5 is independently halogen, alkyl, —OR6, —N(R6) each R6 is independently —H, alkyl, alkenyl, alkynyl, arylalkyl, cycloalkylalkyl, heterocycloalkyl, a fluorescent moiety, a radioisotope or a therapeutic agent; R7 is —H, alkyl, alkenyl, alkynyl, arylalkyl, cycloalkyl, heteroalkyl, cycloalkylalkyl, heterocyeloalkyl, cycloaryl, or heterocycloaryl, optionally substituted with R4, or part of a cyclic structure with an A residue; R8 is —H, alkyl, alkenyl, alkynyl, arylalkyl, cycloalkyl, heteroalkyl, cycloalkylalkyl, heterocycloalkyl, cycloaryl, or heterocycloaryl, optionally substituted with R4, or part of a cyclic structure with an E residue; warhead is one of the moieties 2a, 2b, 2c, 2d, 2e, 2f, 2g, 2h, 2i, 2j, 2k, 2m, 2n, 2o or 2p shown as follows, wherein; X is C, NH, NR8, O or S; n′ is an integer from 0-3; R9 is hydrogen, CN, or (CO)CH R10 is hydrogen, or a bivalent C1-4 saturated or unsaturated, straight or branched, hydrocarbon chain, or an electron-withdrawing group; R11 and R12 are each independently hydrogen, a bivalent C1-4 saturated or unsaturated, straight or branched, hydrocarbon chain, —N(R6) R13 is hydrogen, a bivalent C1-4 saturated or unsaturated, straight or branched, hydrocarbon chain; R14 is an electron-withdrawing group chosen from NO or SO 2 F; R15 is a halogen, a C2 alkynyl side chain optionally substituted with oxo, halogen, NO