PATENT CLAIM ANALYSIS

Application Number: 16074017
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2019-03
Patent Classification: ["540", "474000"]

Abstract:
A Rapafucin library containing compounds of the general structure, (A) and (E), and a synthesis of these compounds are provided.

Claim (Index 1):
A compound of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein: R is wherein R 1 , R 2 , R 3 , R 4 , and R 5  are each independently selected from hydrogen, hydroxyl, alkoxy, cyano, alkylthio, amino, and alkylamino, and wherein is a resin;\n wherein one, two, three, or four of A 1 , A 2 , A 3 , A 4 , and A 5  is N or P with the remaining being CH; \n wherein one, two, three, or four of B 1 , B 2 , B 3  and B 4  is O, N, or S with the remaining being CH or CH 2  as appropriate; \n wherein   is a single or double bond; \n X 1  is O or NR 6 ; \n Y is \u2014C(O)\u2014 or \n X 2  is (CH 2 ) m , O, OC(O), NR 6 , NR 6 C(O); Z is W is O, CH, CH 2 , CR 9 , or C R 10 R 11 ; L 1  and L 2  are each independently a direct bond, substituted or unsubstituted \u2014(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n O(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n NH(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n S(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n O(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n NH(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n S(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n O(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n NH(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n S(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n O(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n NH(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O) n NH(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n S(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n O(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n NH(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O) n NH(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n S(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n O(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O) n O(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n NH(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n S(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n O(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n NH(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n S(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n O(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n NH(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n S(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n O(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n NH(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n S(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 2 -C 6 )alkynyl-C(O)\u2014, \u2014O\u2014, \u2014NH\u2014, \u2014S\u2014, \u2014S(O)\u2014, \u2014SO 2 \u2014, \u2014Si\u2014, and \u2014B\u2014, wherein each alkyl, alkenyl, and alkynyl group may be optionally substituted with alkyl, alkoxy, amino, hydroxyl, sulfhydryl, halogen, carboxyl, oxo, cyano, nitro, or trifluoromethyl; L 3  is a direct bond, substituted or unsubstituted \u2014(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n O(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O) n O(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n NH(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 )S(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 1 -C 6 )alkyl-, substituted or unsubstituted \u2014(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n O(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n NH(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n S(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 2 -C 6 )alkenyl-, substituted or unsubstituted \u2014(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n O(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n NH(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n S(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 2 -C 6 )alkynyl-, substituted or unsubstituted \u2014(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n O(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O) n O(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n NH(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n S(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 1 -C 6 )alkyl-NR 18 \u2014, substituted or unsubstituted \u2014(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n O(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n NH(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n S(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 2 -C 6 )alkenyl-NR 18 \u2014, substituted or unsubstituted \u2014(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n O(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n NH(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n S(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 2 -C 6 )alkynyl-NR 18 \u2014, substituted or unsubstituted \u2014(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n O(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n NH(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n S(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 1 -C 6 )alkyl-C(O)\u2014, substituted or unsubstituted \u2014(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n O(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n NH(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n S(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 2 -C 6 )alkenyl-C(O)\u2014, substituted or unsubstituted \u2014(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n O(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)O(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n OC(O)(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n NH(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)NH(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n S(C 2 -C 6 )alkynyl-C(O)\u2014, substituted or unsubstituted \u2014(CH 2 ) n C(O)(CH 2 ) n S(C 2 -C 6 )alkynyl-C(O)\u2014, wherein each alkyl, alkenyl and alkynyl group may be optionally substituted with alkyl, alkoxy, amino, hydroxyl, sulfhydryl, halogen, carboxyl, oxo, cyano, nitro, or trifluoromethyl; each m is independently an integer selected from 0, 1, 2, 3, 4, 5, and 6; each n is independently an integer selected from 0, 1, 2, 3, 4, 5, and 6; R 6  is hyrdrogen or alkyl; R 7  and R 8  are each independently selected from hydrogen, hydroxy, alkyl, alkoxy, cyano, alkylthio, amino, and alkylamino, and OPG, wherein OPG is a protecting group; R 9 , R 10 , R 11  and are each independently selected from hydrogen, hydroxy, alkyl, alkoxy, cyano, alkylthio, amino, and alkylamino, and OPG, wherein OPG is a protecting group; wherein the Effector Domain has Formula II: wherein: R 12 , R 14 , R 16 , and R 18  are each independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted perfluoroalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkyl amino, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroalkylaryl, (CH 2 ) n CN, (CH 2 ) n CF 3 , (CH 2 ) n C 2 F 5 . R 13 , R 15 , and R 17  are each independently the sidechains of naturally occurring amino acids and their modified forms including but are not limited to D-amino acid configuration, or hydrogen, halogen, amino, cyano, nitro, trifluoromethyl, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted perfluoroalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkyl amino, substituted or unsubstituted alkylthio, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroalkylaryl, substituted or unsubstituted (CH 2 ) n -aryl, substituted or unsubstituted (CH 2 ) n -heteroaryl, (CH 2 ) n CN, (CH 2 ) n CF 3 , (CH 2 ) n C 2 F 5 , (CH 2 ) n OR 19 , (CH 2 ) n C(O)R 19 , (CH 2 ) n C(O)OR 19 , (CH 2 ) n OC(O)R 19 , (CH 2 ) n NR 20 R 21 , (CH 2 ) n C(O)NR 20 R 21 , (CH 2 ) n NR 22 C(O)R 19 , (CH 2 ) n NR 22 C(O)OR 19 , (CH 2 ) NR 22 C(O)NR 20 R 21 , (CH 2 ) n SR 19 , (CH 2 ) n S(O) j NR 20 R 21 , (CH 2 ) n NR 22 (O) j R 19 , or \u2014(CH 2 ) n NR 22 S(O) j NR 20 R 21 ; R 12  and R 13 , R 14  and R 15 , R 16  and R 17  can be convalently connected to form a substituted or unsubstituted 5-, 6-, or 7-membered heterocycle. each k is independently an integer selected from 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10; each j is independently an integer selected from 0, 1, and 2; R 19 , R 20 , R 21 , and R 22  are each independently hydrogen, halogen, amino, cyano, nitro, trifluoromethyl, alkyl, alkenyl, alkynyl, cycloalkyl, perfluoroalkyl, alkoxy, alkylamino, alkylthio, aryl, alkylaryl, heteroalkyl, heterocycloalkyl, heteroaryl, or heteroalkylaryl, or R 19  and R 22  are as described above, and R 20  and R 21 , together with the N atom to which they are attached, form a substituted or unsubstituted 5-, 6-, or 7-membered heterocycloalkyl or a substituted or unsubstituted 5-membered heteroaryl, wherein each of the above groups listed for R 13 , R 15 , and R 17  may be optionally independently substituted with 1 to 3 groups selected from halogen, amino, cyano, nitro, trifluoromethyl, alkyl, alkenyl, alkynyl, cycloalkyl, perfluoroalkyl, alkoxy, alkylamino, alkylthio, aryl, alkylaryl, heteroalkyl, heterocycloalkyl, heteroaryl, heteroalkylaryl, (CH 2 ) n CN, (CH 2 ) n CF 3 , (CH 2 ) n C 2 F 5 , (CH 2 ) n O 19 , (CH 2 ) n C(O)R 19 , (CH 2 ) n C(O)OR 19 , (CH 2 ) n OC(O)R 19 , (CH 2 ) n NR 20 R 21 , (CH 2 ) n C(O)NR 20 R 21 , (CH 2 ) n NR 22 C(O)R 19 , (CH 2 ) n NR 22 C(O)OR 19 , (CH 2 ) n NR 22 C(O)NR 20 R 21 , (CH 2 ) n SR 19 , (CH 2 ) n S(O) j NR 20 R 21 , (CH 2 ) n NR 22 S(O) j R 19 , or \u2014(CH 2 ) n NR 22 S(O) j NR 20 R 21 ; or wherein the Effector Domain has Formula III: wherein: each k is independently an integer selected from 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10; R 23  is a hydrogen or alkyl; X 3  is substituted or unsubstituted \u2014(C 1 -C 30 )alkyl-, alkenyl-, alkynyl- with each carbon individually assuming one of the following redox states: CH 2 , CH\u2014OH, C(O); or wherein the Effector Domain has Formula IV: wherein: X 4  is substituted or unsubstituted \u2014(C 1 -C 30 )alkyl-, alkenyl-, alkynyl- with each carbon individually assuming one of the following redox states: CH 2 , CH\u2014OH, C(O). Or wherein the Effector Domain has Formula V: wherein: R 24  and R 25  are each a hydrogen or alkyl; X 5  is substituted or unsubstituted \u2014(C 1 -C 30 )alkyl-, alkenyl-, alkynyl- with each carbon individually assuming one of the following redox states: CH 2 , CH\u2014OH, C(O). Or wherein the Effector Domain has Formula VI: wherein: X 6  is substituted or unsubstituted \u2014(C 1 -C 30 )alkyl-, alkenyl-, alkynyl- with each carbon individually assuming one of the following redox states: CH 2 , CH\u2014OH, C(O).

Metadata:
- Claim Count in Document: 26.0
- Percentile: 95.0
- Lexical Diversity: 1.35
- Patent Class: 540.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15728282', '13990396', '14987653', '14793296', '15581749']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.6492252349206563
- 35 USC 102 Novelty (BERT): 0.5050170406364679
- Combined Prediction Score: 0.6348044154922374
- Mean Citation Score: 213.20821
- Max Citation Score: 239.5702
- Similarity Product: 182.0859727903366

Labels:
- Claim Label 101: 1
- Claim Label 102: 0
- Claim Label 103: 0
- Claim Label 112: 0
- Combined Label: 0
- Label 101 Adjusted: 1

Dataset: test