PATENT CLAIM ANALYSIS

Application Number: 16329336
Application Type: Utility
Filing Date: 2019-02
Publication Date: 2019-07
Patent Classification: ["514", "365000"]

Abstract:
The invention describes an aryl-2,2′-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2′-tandem bisthiazole compound with the structure as shown in general formula I and the preparation method thereof and use thereof as a histone deacetylase inhibitor in the preparation of antitumor drugs.

Claim (Index 6):
A method for the preparation of the compound or an optical isomer thereof, or a pharmaceutically acceptable salt thereof of  claim 1 , wherein, the method is with a route shown in the route I, wherein, R 1 , R 2 , R 3  and R 4  are defined as above, except that R 4  is other than H; comprising steps: (1) condensing methyl 4-acetylbenzoate with tert-butyl sulfenamide to form tert-butyl sulfoximine 1; (2) adding tert-butyl sulfinimide 1 and Grignard reagent to form tert-butyl sulfenamide 2; (3) deprotecting tert-butyl sulfinamide 2 to form amine 3; (4) condensation reacting amine 3 with acid 4 to form methyl ester 5; (5) after hydrolysis reacting methyl ester 5 with alkali, exchanging with a hydroxylamine protected by a protecting group, and finally removing the protecting group to form a compound of the formula II-1; or the method is with a route shown in the route II: wherein, R 1 , R 2 , and R 3  are defined as above; comprising steps: (i) condensation reacting acid 4 with methyl 4-aminomethylbenzoate to form methyl ester 8; (ii) after hydrolysis reacting methyl ester 8 with alkali, reacting with a hydroxylamine protected by a protecting group, and finally removing the protecting group to form a compound of the formula II-2.

Metadata:
- Claim Count in Document: 14.0
- Percentile: 99.0
- Lexical Diversity: 1.65714
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['14391386', '16078054', '12734026', '14361548', '10594483']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7725120572812859
- 35 USC 102 Novelty (BERT): 0.5095671290256824
- Combined Prediction Score: 0.7462175644557255
- Mean Citation Score: 281.938596
- Max Citation Score: 288.99008
- Similarity Product: 212.17269297294607

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

Dataset: test