PATENT CLAIM ANALYSIS

Application Number: 16226093
Application Type: Utility
Filing Date: 2018-12
Publication Date: 2019-05
Patent Classification: ["548", "400000"]

Abstract:
Hydrophilic linkers are useful for linking drugs to cell-binding ligands in ligand-drug conjugates, such as antibody-drug conjugates. The ligand-drug conjugate includes a cell-binding ligand capable of binding to a particular cell population, and a drug connected to the ligand by a hydrophilic linker. The hydrophilic linker includes one or more hydrophilic groups that render the linker hydrophilic. The hydrophilic linker may also include functional groups at the two termini for coupling to the drug and the cell-binding ligand respectively.

Claim (Index 1):
A compound of Formula (1):\n U\ue8a0X-V-Y\ue8a0 n W\u2003\u2003(Formula 1) wherein: V represents a polar or charged group selected from the group consisting of wherein R is H or C 1 \u02dcC 8  alkyl; Q is CH or N; Z is NH, NH\u2014(CH 2 ) m , or N(CH 3 )(CH 2 ) m , wherein m is an integer from 1 to 5, and \u201c \u201d is a site of attachment;\n U represents a reactive functional group that enables a covalent linkage of the compound of Formula (1) with a cytotoxic drug and is selected from the group consisting of thiol group, disulfide groups, amino groups, carboxyl groups, aldehyde groups, ketone groups, maleimide groups, haloacetyl groups, alkenyl groups, alkynyl groups, hydrazine groups, and hydroxyl group; \n W represents a reactive functional group that enables a covalent linkage of the compound of Formula (1) with a cell-binding ligand, and is selected from the group consisting of N-hydroxysuccinmide ester group, N-sulfosuccinim idyl ester group, nitrophenyl ester group, dinitrophenyl ester group, pentafluorophenyl ester group, tetrafluorophenyl ester group, acyl chloride group, anhydride groups, sulfonyl chloride group, chloroformate group, isocyanate group, isothiocyanate group, aldehyde groups, ketone groups, disulfide groups, maleimide groups, acyl chloride group, haloacetyl groups, alkenyl pyridine groups, isocyanate group, and isothiocyanate group; \n X represents a component composed of one, two, or three methylene units optionally substituted with an alkyl, halo, hydroxyl, or alkoxy group; \n Y represents a component composed of one, two, or three methylene units optionally substituted with an alkyl, halo, hydroxyl, or alkoxy group; \n n is an integer from 1 to 100, provided that when n>1, values of each V, X, and Y in the repeating brackets of Formula (1) are independent and do not have to be identical.

Metadata:
- Claim Count in Document: 12.0
- Percentile: 98.0
- Lexical Diversity: 1.66667
- Patent Class: 548.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15558917', '14432073', '15118726', '15479903', '12574466']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7913515352306882
- 35 USC 102 Novelty (BERT): 0.5413737251000644
- Combined Prediction Score: 0.766353754217626
- Mean Citation Score: 291.2685800000001
- Max Citation Score: 399.9482
- Similarity Product: 281.03063940103056

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

Dataset: test