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 21):
The compound according to any one of  claims 1 - 20 , wherein R 12  is:\n (i) halo; (ii) \u2014OSO 2 \u2014R 16 ; (iii) \u2014OC(\u2550O)R 16 ; (iv) \u2014OP(\u2550O)(R 16 ) 2 , (v) \u2014OP(\u2550O)(OR 16 ) 2 ; (vi) \u2014OP(\u2550O)(R 16 )(OR 16 ); or (vii) \u2014O\u2014(N-linked heteroaryl); wherein: R 16  is C 1-6 alkyl, C 1-6 haloalkyl, heteroalkyl, C 6-10 aryl, C 7-12 aralkyl, C 3-7 cycloalkyl, heteroaryl 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), or heterocyclyl including from 3-7 ring atoms (wherein from 1-3 of the ring atoms are independently selected from N, NH, N\u2014C 1 -C 6  alkyl, and O), each of which is optionally substituted with from 1-3 R a ; or R 16  is \u2014Y\u2032 p \u2014Z\u2032; wherein: Y\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, \u2014OC(\u2550O)\u2014, \u2014C(\u2550O)O\u2014, \u2014NHC(\u2550O)\u2014, \u2014C(\u2550O)NH\u2014, \u2014C(\u2550O)\u2014, cyclodextrin, human serum albumin, amino acid, amino acid mimetic, or hydrazine; Z\u2032 is conjugate for enhancing solubility, stability, half-life, permeability, volume of distribution, and/or target specificity, which comprises 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): alkylene chain, heteroalkylene chain, polyheteroalkylene chain, alkenylene chain, cyclodextrin, alkylated cyclodextrin, human serum albumin, \u2014OC(\u2550O)\u2014, \u2014C(\u2550O)O\u2014, \u2014NHC(\u2550O)\u2014, \u2014C(\u2550O)NH\u2014, \u2014C(\u2550O)\u2014, monoclonal anti-body, quaternary ammonium ion, NH 2 , docosahexenoic acid, hyaluronic acid, poly(L-glutamic acid), N-(2-hydroxypropyl) methacrylamide copolymer, or dendrimers (e.g., nitro-substituted dendrimers); p is 0 or 1; and R a  at each occurrence is, independently selected from halo, cyano, nitro, hydroxyl, C 1-6  alkoxy, heteroalkyl, C 6-10  aryloxy, C 7-12  aralkoxy, CF 3 , quaternary ammonium ion, sugar, \u2014Y\u2032 p \u2014Z\u2032, C 1-6  alkyl, \u2014C(\u2550)(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), phosphate (or a salt thereof), \u2014C(\u2550O)\u2014Y\u2032 p \u2014Z\u2032, and \u2014SO 2 \u2014Y\u2032 p \u2014Z\u2032.

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): 0.7842195915600136
- 35 USC 102 Novelty (BERT): 0.6693443723183291
- Combined Prediction Score: 0.7727320696358452
- Mean Citation Score: 569.07662
- Max Citation Score: 793.8515
- Similarity Product: 612.3698348932268

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