PATENT CLAIM ANALYSIS

Application Number: 16060146
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2018-09
Patent Classification: ["514", "255050"]

Abstract:
The present invention discloses a five-membered heterocyclic amide WNT pathway inhibitor, which belongs to a compound that regulates the activity of a Wnt signaling pathway, and provides a method for preparing such a compound, and the use of such a compound in preparing a medicament that antagonizes the Wnt signaling pathway. The five-membered heterocyclic amide WNT pathway inhibitor provided by the invention has a remarkable anti-tumor activity based on a target-based rational drug design of, and can be used for the development of a new generation of Wnt pathway inhibitors, and has a great clinical application value and considerable market potential.

Claim (Index 8):
A five-membered heterocyclic amide Wnt pathway inhibitor, selected from the following: N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-1-methyl-3-phenyl-1H-pyrazole-5-carboxamide;\n N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-phenyl-1H-pyrazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-2-phenylthiazole-5-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-phenylthiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-2-phenylthiazole-4-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-4-phenylthiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-phenylisoxazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-phenyl-1,3,4-thiadiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-1-methyl-5-phenyl-1H-pyrazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-4-methyl-5-phenylthiazole-2-carboxamide; 5-(2-chlorophenyl)-N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)thiazole-2-carboxamide; 5-(3-chlorophenyl)-N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)thiazole-2-carboxamide; 5-(4-chlorophenyl)-N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)thiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyridin-2-yl)thiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyrazin-2-yl)thiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyridin-2-yl)-1H-pyrazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(3-fluoropyridin-2-yl)-1H-pyrazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(5-fluoropyridin-3-yl)-1H-pyrazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(6-methylpyridin-2-yl)-1H-pyrazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyrimidin-2-yl)-1H-pyrazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyrazin-2-yl)-1H-pyrazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyrazin-2-yl)-1H-pyrazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-2-(pyridin-2-yl)thiazole-5-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-2-(3-fluoropyridin-2-yl)thiazole-5-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-2-(5-fluoropyridin-3-yl)thiazole-5-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-2-(6-methylpyridin-2-yl)thiazole-5-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-2-(pyrimidin-2-yl)thiazole-5-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-2-(pyrazin-2-yl)thiazole-5-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyridin-2-yl)isoxazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(3-fluoropyridin-2-yl)isoxazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(5-fluoropyridin-3-yl)isoxazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(6-methylpyridin-2-yl)isoxazole-3-carboxamide; N-((2\u2032,3-dimethyl[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyrimidin-2-yl)isoxazole-3-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyrazin-2-yl)isoxazole-3-carboxamide; 5-(4-acetylpiperazin-1-yl)-N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)isoxazole-3-carboxamide; N-((2\u2032,3-dimethyl[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyridin-3-yl)thiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(3-fluoropyridin-2-yl)thiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(5-fluoropyridin-3-yl)thiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(6-methylpyridin-2-yl)thiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyrimidin-2-yl)thiazole-2-carboxamide; N-((2\u2032,3-dimethyl[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyrimidin-5-yl)thiazole-2-carboxamide; 5-(4-acetylpiperazin-1-yl)-N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-1,3,4-thiadiazole-2-carboxamide; 5-(4-acetylpiperazin-1-yl)-N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)thiazole-2-carboxamide; 2-(4-acetylpiperazin-1-yl)-N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)thiazole-5-carboxamide; 5-(3-chlorophenyl)-N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-1,3,4-thiadiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(3-fluorophenyl)-1,3,4-thiadiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyridin-2-yl)-1,3,4-thiadiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(3-fluoropyridin-2-yl)-1,3,4-thiadiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(5-fluoropyridin-3-yl)-1,3,4-thiadiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(6-methylpyridin-2-yl)-1,3,4-thiadiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyrimidin-2-yl)-1,3,4-thiadiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(pyrazin-2-yl)-1,3,4-thiadiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(5-methylpyridin-3-yl)-1,3,4-thiadiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(2-methylpyridin-3-yl)-1,3,4-thiadiazole-2-carboxamide; N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(4-methylpyridin-3-yl)-1,3,4-thiadiazole-2-carboxamide; and N-((2\u2032,3-dimethyl-[2,4\u2032-bipyridin]-5-yl)methyl)-5-(3-methylpyridin-2-yl)-1,3,4-thiadiazole-2-carboxamide.

Metadata:
- Claim Count in Document: 13.0
- Percentile: 94.0
- Lexical Diversity: 1.83051
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15699112', '13948038', '13132294', '12263949', '14214185']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7794739338079801
- 35 USC 102 Novelty (BERT): 0.5346634339297509
- Combined Prediction Score: 0.7549928838201572
- Mean Citation Score: 331.698596
- Max Citation Score: 350.51352
- Similarity Product: 295.51072397696976

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