PATENT CLAIM ANALYSIS

Application Number: 15991150
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2019-05
Patent Classification: ["514", "001300"]

Abstract:
The present invention discloses doxorubicin derivatives for targeted activation by Legumain, its preparation method and use. The doxorubicin derivatives are obtained by condensation between the amino group of compound A and the carboxyl group of compound B and have the following structure: compounds A and B have the following structures, respectively: wherein R 3  in compound B is Leu or absent; R 4  is any one amino acid selected from the group consisting of Ala and Thr; R 5  is any one amino acid selected from the group consisting of Ala, Thr and Asn; R 6  is wherein n=1-20; or wherein R 7  is substituted or unsubstituted, linear or branched, saturated or unsaturated C1-C20 fatty hydrocarbon, or substituted or unsubstituted C6-C20 aromatic hydrocarbon. The doxorubicin derivatives of the present invention are specifically tumor-targeted and have a long in vivo metabolic half-life, as compared with doxorubicin. They exhibit an efficient and safe anti-tumor effect and could be used to prepare an anti-tumor drug.

Claim (Index 1):
A cleavable linker within a conjugate, the conjugate having a first chemical moiety and a second chemical moiety, the first chemical moiety being conjugated by the cleavable linker to the second chemical moiety, the first chemical moiety represented by R 6  and may including a carbonyl group forming an amide bond with the cleavable linker, the second chemical moiety represented by Asn-R4-R5, the cleavable linker comprising a modified peptide sequence corresponding to a bracketed radical within the conjugate selected from the group consisting of:\n Asn-R4-R5-R6 and Leu-Asn-R4-R5-R6, wherein R 4  and R5 are any amino acid; R 6  is wherein n=1-20; or wherein R 7  is a substituted or unsubstituted, linear or branched, saturated or unsaturated C1-C20 fatty hydrocarbon, or substituted or unsubstituted C6-C20 aromatic hydrocarbon.

Metadata:
- Claim Count in Document: 9.0
- Percentile: 93.0
- Lexical Diversity: 1.90426
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14655869', '15505861', '12623859', '11288978', '10659501']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7263717615636455
- 35 USC 102 Novelty (BERT): 0.5946991845198156
- Combined Prediction Score: 0.7132045038592625
- Mean Citation Score: 325.433198
- Max Citation Score: 578.5147
- Similarity Product: 398.4954292198957

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