PATENT CLAIM ANALYSIS

Application Number: 15752923
Application Type: Utility
Filing Date: 2018-02
Publication Date: 2018-08
Patent Classification: ["546", "080000"]

Abstract:
Provided is a pharmaceutical preparation including a polymerized camptothecin derivative that is obtained by bonding a camptothecin derivative having nanoparticle-forming properties by associating in an aqueous solution, to a polymer carrier, the pharmaceutical preparation composition having enhanced preparation stability. Particularly, a pharmaceutical preparation maintaining nanoparticle-forming properties and camptothecin derivative bonding stability, which are important factors, and having excellent storage stability is provided. Disclosed is a pharmaceutical preparation including a block copolymer in which a polyethylene glycol segment is linked to a polyglutamic acid segment including a glutamic acid unit having a camptothecin derivative bonded thereto; and a saccharide. The pharmaceutical preparation forms associates in an aqueous solution, and the ratio of change in the scattered light intensity of the associates of the pharmaceutical preparation obtained after the pharmaceutical preparation is stored for 4 weeks at 40° C. under light-shielded conditions, is 20% or less.

Claim (Index 1):
A pharmaceutical preparation comprising a block copolymer of a polyethylene glycol segment and a polyglutamic acid segment linked together, the polyglutamic acid segment comprising a glutamic acid unit having a camptothecin derivative bonded thereto; and a saccharide,\n wherein the block copolymer is a block copolymer represented by General Formula (1): wherein R 1  represents hydrogen atom or a (C1-C6) alkyl group optionally substituted with a substituent; A represents a (C1-C6) alkylene group; R 2  represents any one selected from the group consisting of a hydrogen atom, a (C1-C6) acyl group optionally substituted with a substituent, and a (C1-C6) alkoxycarbonyl group optionally substituted with a substituent; R 3  represents a hydroxyl group and/or \u2014N(R 6 )CONH(R 7 ); R 6  and R 7  may be identical with or different from each other, each representing a (C1-C8) alkyl group optionally substituted with a tertiary amino group; R 4  represents any one selected from the group consisting of a hydrogen atom, a (C1-C6) alkyl group optionally substituted with a substituent, and a silyl group optionally substituted with a substituent; R 5  represents a hydrogen atom or a (C1-C6) alkyl group optionally substituted with a substituent; t represents an integer from 45 to 450; d and e each represent an integer, (d+e) represents an integer from 6 to 60, the proportion of d with respect to (d+e) is 1% to 100%, the proportion of e is 0% to 99%; and the polyglutamic acid segment has a polyglutamic acid segment structure having a glutamic acid unit with a camptothecin derivative bonded thereto and a glutamic acid unit with a R 3  group bonded thereto, with the glutamic acid units being each independently arranged randomly, wherein the pharmaceutical preparation has a physical property of forming associates based on a plurality of the block copolymer molecules in an aqueous solution, and wherein the ratio of change in the scattered light intensity of the associates of the pharmaceutical preparation obtained after the pharmaceutical preparation has been stored for 4 weeks at 40\u00b0 C. under light-shielded conditions, is 20% or less.

Metadata:
- Claim Count in Document: 15.0
- Percentile: 88.0
- Lexical Diversity: 1.98734
- Patent Class: 546.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15515295', '15822817', '15548259', '13319175', '10532670']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.74419990463695
- 35 USC 102 Novelty (BERT): 0.5621310671083366
- Combined Prediction Score: 0.7259930208840887
- Mean Citation Score: 322.4260700000001
- Max Citation Score: 425.98413
- Similarity Product: 404.6383266107797

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