PATENT CLAIM ANALYSIS

Application Number: 16181867
Application Type: Utility
Filing Date: 2018-11
Publication Date: 2019-03
Patent Classification: ["514", "220000"]

Abstract:
The present disclosure relates generally to derivatives of pyrrolobenzodiazepines and antibody-drug conjugates thereof and to methods of using these conjugates as therapeutics and/or diagnostics.

Claim (Index 1):
A compound of Formula (I), or a tautomer thereof, or a pharmaceutically acceptable salt or solvate of the compound or the tautomer, wherein: D is D2: T is C 1-10  alkylene linker; A is wherein the \u2014NH group of A is connected to the \u2014C(O)-T- moiety of Formula (I) and the C\u2550O moiety of A is connected to E; and each independently is E is \u2014OH, \u2014NH\u2014(C 1-6  alkylene)-R 13a , E1, E2, E3, or E4: wherein the dotted line in E1 or E4 indicates the presence of a single or double bond;\n R 4 , R 5  and R 7  are each independently \u2014H, \u2014R 2 , \u2014OH, \u2014OR 2 , \u2014SH, \u2014SR 2 , \u2014NH 2 , \u2014NHR 2 , \u2014NR 2 R 3 , \u2014NO 2 , \u2014SnMe 3 , halo or a polyethylene glycol unit \u2014(OCH 2 CH 2 ) r \u2014OR a ; or R 4  and R 7  together form bis-oxy-C 1-3  alkylene; \n each occurrence of R 2  and R 3  independently is an optionally substituted C 1-8  alkyl, optionally substituted C 2-8  alkenyl, optionally substituted C 2-8  alkynyl, optionally substituted C 3-8  cycloalkyl, optionally substituted 3- to 20-membered heterocycloalkyl, optionally substituted C 6-20  aryl or optionally substituted 5- to 20-membered heteroaryl, and, optionally in relation to the group NR 2 R 3 , R 2  and R 3  together with the nitrogen atom to which they are attached form an optionally substituted 4-, 5-, 6- or 7-membered heterocycloalkyl or an optionally substituted 5- or 6-membered heteroaryl; \n each R 8  independently is \u2014OH, halo, \u2014NO 2 , \u2014CN, \u2014N 3 , \u2014OR 2 , \u2014COOH, \u2014COOR 2 , \u2014COR 2 , \u2014OCONR 13 R 14 , \u2014CONR 13 R 14 , C 1-10  alkyl, \u2014CO\u2014NH\u2014(C 1-6  alkylene)-R 13a , C 3-10  cycloalkyl, C 2-10  alkenyl, C 2-10  alkynyl, a polyethylene glycol unit \u2014(OCH 2 CH 2 ) r \u2014OR a , 3- to 14-membered heterocycloalkyl, 5- to 12-membered heteroaryl, \u2014S(\u2550O) 2 R 12 , \u2014S(\u2550O) 2 NR 13 R 14 , \u2014SR 12 , \u2014SO x M, \u2014OSO x M, \u2014NR 9 COR 19 , \u2014NH(C\u2550NH)NH 2  or \u2014R 20 \u2014R 21 \u2014NR 13 R 14 ; \n each R 9  independently is C 1-10  alkyl, C 3-10  cycloalkyl, C 2-10  alkenyl or C 2-10  alkynyl; \n R 10  is \u2014H or a nitrogen protecting group; \n R 11  is -QR Q  or \u2014SO x M; \n or R 10  and R 11  taken together with the nitrogen atom and carbon atom to which they are respectively attached, form a N\u2550C double bond; \n each R 12  independently is C 1-7  alkyl, 3- to 20-membered heterocycloalkyl, 5- to 20-membered heteroaryl, or C 6-20  aryl; \n each occurrence of R 13  and R 14  are each independently H, C 1-10  alkyl, 3- to 20-membered heterocycloalkyl, 5- to 20-membered heteroaryl, or C 6-20  aryl; \n each R 13a  independently is \u2014OH or \u2014NR 13 R 14 ; \n R 15 , R 16 , R 17  and R 18  are each independently \u2014H, \u2014OH, halo, \u2014NO 2 , \u2014CN, \u2014N 3 , \u2014OR 2 , \u2014COOH, \u2014COOR 2 , \u2014COR 2 , \u2014OCONR 13 R 14 , C 1-10  alkyl, C 3-10  cycloalkyl, C 2-10  alkenyl, C 2-10  alkynyl, a polyethylene glycol unit \u2014(OCH 2 CH 2 ) r \u2014OR a , 3-14 membered heterocycloalkyl, 5- to 12-membered heteroaryl, \u2014NR 13 R 14 , \u2014S(\u2550O) 2 R 12 , \u2014S(\u2550O) 2 NR 13 R 14 , \u2014SR 12 , \u2014SO x M, \u2014OSO x M, \u2014NR 9 COR 19  or \u2014NH(C\u2550NH)NH 2 ; \n each R 19  independently is C 1-10  alkyl, C 3-10  cycloalkyl, C 2-10  alkenyl or C 2-10  alkynyl; \n each R 20  independently is a bond, C 6-10  arylene, 3-14 membered heterocycloalkylene or 5- to 12-membered heteroarylene; \n each R 21  independently is a bond or C 1-10  alkylene; \n each X 1  independently is CR b , or N; \n each Y 1  independently is NR a , O or S; \n each Z 1  independently is NR a , O or S; \n each R a  independently is H or C 1-4  alkyl; \n each R b  independently is H, OH, C 1-4  alkyl, or C 1-4  alkoxyl; \n X 2  is CH, CH 2  or N; \n X 3  is CH or N; \n X 4  is NH, O or S; \n Q is O, S or NH; \n when Q is S or NH, then R Q  is \u2014H or optionally substituted C 1-7  alkyl; or \n when Q is O, then R Q  is \u2014H or optionally substituted C 1-7  alkyl, or \u2014SO x M; \n each M independently is H or a monovalent pharmaceutically acceptable cation; \n each r independently is an integer from 1 to 200; \n s is 1, 2, 3, 4, 5 or 6; \n t is 0, 1, or 2; and \n each x independently is 2 or 3, and \n when E is E4, the dotted line indicates the presence of a double bond, X 3  is CH, and X 4  is O or S, then s is 2, 3, 4, 5 or 6.

Metadata:
- Claim Count in Document: 65.0
- Percentile: 98.0
- Lexical Diversity: 1.19048
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: False
- Related Applications: ['15630068', '15597453', '14305643', '16061295', '15182444']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7808954025574752
- 35 USC 102 Novelty (BERT): 0.5623401475608822
- Combined Prediction Score: 0.759039877057816
- Mean Citation Score: 360.17923
- Max Citation Score: 448.83072
- Similarity Product: 306.4125494538116

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

Dataset: test