PATENT CLAIM ANALYSIS

Application Number: 15881919
Application Type: Utility
Filing Date: 2018-01
Publication Date: 2018-05
Patent Classification: ["514", "001300"]

Abstract:
This disclosure features compounds that are useful as pro-drugs of epoxy ketone protease inhibitors.

Claim (Index 63):
The compound of  claim 51 , wherein the compound has Formula (VI): wherein R 14  is \u2014R 14\u2032 \u2014R 20 \u2014, in which R 20  is connected to PEG, and R 14\u2032  is a divalent spacer comprising one or more of the following moieties (e.g., comprise 1, 2, 3, 4, or 5 of the following moieties; e.g., comprise 1, 2, or 3 of the following moieties; e.g., consist of 1, 2, 3, 4, or 5 of the following moieties; e.g., consist of 1, 2, or 3 of the following moieties): heteroatom (e.g., N, O, or S), alkylene chain, heteroalkylene chain, polyheteroalkylene chain, alkenylene chain, arylene including 6-10 ring atoms, heteroarylene including from 5-10 ring atoms (wherein from 1-3 of the ring atoms are independently selected from N, NH, N\u2014C 1 -C 6  alkyl, O, and S), heterocycloalkylene including 3-9 ring atoms (wherein from 1-3 of the ring atoms are independently selected from N, NH, N\u2014C 1 -C 6  alkyl, O, and S), \u2014OC(\u2550O)\u2014, \u2014C(\u2550O)O\u2014, \u2014NHC(\u2550O)\u2014, \u2014C(\u2550O)NH\u2014, \u2014N(C 1-6  alkyl)C(\u2550O), \u2014C(\u2550O)N(C 1-6  alkyl)-, \u2014C(\u2550O)\u2014, \u2014NHC(\u2550O)NH\u2014, cyclodextrin, human serum albumin, amino acid, amino acid mimetic, or hydrazine, wherein arylene including 6-10 ring atoms, heteroarylene including from 5-10 ring atoms, and heterocycloalkylene including 3-9 ring atoms are each optionally substituted with 1, 2, or 3 substituents each independently selected from the group consisting of halo, cyano, nitro, hydroxyl, C 1-6  alkoxy, heteroalkyl, C 6-10  aryloxy, C 7-12  aralkoxy, CF 3 , quaternary ammonium ion, sugar, C 1-6  alkyl, \u2014C(\u2550O)(C 1-6  alkyl), \u2014SO 2 (C 1-6  alkyl), \u2014C(\u2550O)O(C 1-6  alkyl), \u2014C(\u2550O)O(heteroalkyl), \u2014C(\u2550O)NH(C 1-6  alkyl), \u2014C(\u2550O)NH(heteroalkyl), \u2014C(\u2550O)(phenyl), \u2014SO 2 (phenyl), and phosphate (or a salt thereof); R 20  is absent or R S5  is H, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxyC 1-6 alkyl, C 6-10 aryl, or C 7-12 aralkyl, each of which is optionally substituted with a group selected from amide, amine, carboxylic acid or a pharmaceutically acceptable salt thereof, carboxyl ester, thiol, and thioether; R 1  is defined according to (A) or (B) below: (A) R 1  has formula (II): wherein Het is heterocyclyl that includes from 5-6 ring atoms, wherein at least one ring atom is a nitrogen atom selected from \u2014N(H)\u2014, \u2014N(M)-, or \u2014N(C 1 -C 3  alkyl)-, wherein said ring nitrogen atom is further optionally substituted with a group R 11 , thereby forming a quaternary nitrogen atom and wherein the positive charge associated with the quaternary nitrogen atom is balanced by a pharmaceutically acceptable anion; and M is C 1 -C 12  alkyl; or\n (B) R 1  is heteroaryl that includes from 5-6 ring atoms, wherein at least one ring atom is a nitrogen atom selected from \u2550N\u2014 and \u2014N(C 1 -C 3  alkyl)-, wherein said ring nitrogen atom is further optionally substituted with a group R 11 , thereby forming a quaternary nitrogen atom and wherein the positive charge associated with the quaternary nitrogen atom is balanced by a pharmaceutically acceptable anion; \n R 2  and R 3 , together with the carbon atoms to which each is attached, form an epoxide ring; or \n R 2  is R 12 , and R 3  is hydroxyl or activated hydroxyl; \n R 4  and R 5 , together with the carbon atom to which both are attached, form a carbonyl group; or \n R 4  and R 5 , together with the carbon atom to which both are attached, form R 13 , \n R S1 , R S2 , R S3 , and R S4  are each independently selected from C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxyC 1-6 alkyl, C 6-10 aryl, and C 7-12 aralkyl, each of which is optionally substituted with a group selected from amide, amine, carboxylic acid or a pharmaceutically acceptable salt thereof, carboxyl ester, thiol, and thioether, \n R N1 , R N2 , R N3 , and R N4  are each independently selected from H and R 14 , provided at least one of (e.g., one of) R N1 , R N2 , R N3 , and R N4  is R 14 ; \n R 11  is a moiety that is removable at a pH>7 or in the presence of an esterase; \n R 12  is a leaving group; \n R 13  is a masked carbonyl group that is removable at a pH<6.5 or in the presence of an enzyme selected from esterase, amidase, phosphodiesterase or phosphoamidase and CYP P450, or any combination thereof; and \n each R 14  is, independently, a moiety that is removable at a pH>7 or in the presence of an esterase.

Metadata:
- Claim Count in Document: 3.0
- Percentile: 86.0
- Lexical Diversity: 1.0
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['13938160', '14041953', '15065347', '15602823', '15651687']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7888130592693323
- 35 USC 102 Novelty (BERT): 0.6520479999436942
- Combined Prediction Score: 0.7751365533367686
- Mean Citation Score: 569.07662
- Max Citation Score: 793.8515
- Similarity Product: 565.6503568820657

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

Dataset: test