PATENT CLAIM ANALYSIS

Application Number: 15975423
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-12
Patent Classification: ["424", "179100"]

Abstract:
The present disclosure relates to compounds of formula (I): RCG1-L-P  (I) wherein RCG1 represents a reactive chemical group being reactive towards a chemical group present on a polypeptide such as an antibody; P represents H, OH or an activated O; and L represents a specific linker. The disclosure also relates to cryptophycin payloads, as well as to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The disclosure also relates to the process for preparing these conjugates.

Claim (Index 14):
A Cryptophycin payload of formula (IV): wherein:\n R 1  represents a (C 1 -C 6 )alkyl group; \n R 2  and R 3  represent, independently of each other, a hydrogen atom or a (C 1 -C 6 )alkyl group; \n or alternatively R 2  and R 3  form together with the carbon atom to which they are attached, a (C 3 -C 6 )cycloalkyl or a (C 3 -C 6 )heterocycloalkyl group; \n R 4  and R 5  represent, independently of each other, a hydrogen atom, a (C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkyl-NH(R 12 ) group, a (C 1 -C 6 )alkyl-OH group, a (C 1 -C 6 )alkyl-SH group, or a (C 1 -C 6 )alkyl-CO 2 H group; \n or alternatively R 4  and R 5  form together with the carbon atom to which they are attached a (C 3 -C 6 )cycloalkyl or a (C 3 -C 6 )heterocycloalkyl group; \n X represents O or N(R 6 ); \n R 6  represents a hydrogen atom or a (C 1 -C 6 )alkyl group; \n R 7  and R 5  represent, independently of each other, a hydrogen atom, a (C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkyl-CO 2 H group or a (C 1 -C 6 )alkyl-N(C 1 -C 6 )alkyl 2  group; \n or alternatively R 7  and R 8  form together with the carbon atom to which they are attached a (C 3 -C 6 )cycloalkyl group or a (C 3 -C 6 )heterocycloalkyl group; \n R 9  represents at least one substituent of the phenyl nucleus chosen, each independently of each other, a hydrogen atom, \u2014OH, (C 1 -C 4 )alkoxy, a halogen atom, \u2014NH 2 , \u2014NH(C 1 -C 6 )alkyl or \u2014N(C 1 -C 6 )alkyl 2  or \u2014NH(C 1 -C 6 )cycloalkyl or (C 3 -C 6 )heterocycloalkyl group; \n R 10  represents at least one substituent of the phenyl nucleus chosen from a hydrogen atom and a (C 1 -C 4 )alkyl group; \n Y represents NR 11 \u2014(C 1 -C 6 )alkyl-, \u2014O\u2014(C 1 -C 6 )alkyl-, or \u2014S\u2014(C 1 -C 6 )alkyl-; \n R 11  and R 12  represent, independently of each other, a hydrogen atom or (C 1 -C 6 )alkyl; \n n represents an integer ranging from 1 to 6; \n L is defined as in formula (I) according to  claim 1  and represents a linker of formula (II) as defined in  claim 1 ; and \n RCG1 represents a reactive chemical group present at the end of the linker L, RCG1 being reactive towards a chemical group present on a polypeptide such as an antibody.

Metadata:
- Claim Count in Document: 55.0
- Percentile: 93.0
- Lexical Diversity: 1.61667
- Patent Class: 424.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['14069057', '15581749', '15280563', '14843520', '14818455']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.769139118137051
- 35 USC 102 Novelty (BERT): 0.5180660387593136
- Combined Prediction Score: 0.7440318101992773
- Mean Citation Score: 309.744996
- Max Citation Score: 313.26495
- Similarity Product: 229.43803154473903

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