PATENT CLAIM ANALYSIS

Application Number: 15998791
Application Type: Utility
Filing Date: 2018-08
Publication Date: 2019-02
Patent Classification: ["546", "212000"]

Abstract:
The present invention relates to a novel 2,3,5-substituted thiophene compound having inhibitory activity against kinases, an anticancer agent including the compound as an active ingredient, and a method for preparing the compound.

Claim (Index 4):
The compound of  claim 1 , wherein the compound is selected from the group consisting of:\n 1) ethyl (S)-4-((5-(piperidin-3-ylcarbamoyl)-4-ureidothiophen-2-yl) ethynyl)benzoate; 2) (S)-5-(phenylethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 3) (S)\u2014N-(piperidin-3-yl)-5-(pyridin-3-ylethynyl)-3-ureidothiophene-2-carboxamide; 4) (S)\u2014N-(piperidin-3-yl)-5-(pyridin-4-ylethynyl)-3-ureidothiophene-2-carboxamide; 5) (S)-5-((3-nitrophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 6) (S)-5-((3-cyanophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 7) (S)-5-((4-nitrophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 8) (S)-5-((4-chlorophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 9) (S)-5-((4-fluorophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 10) (S)\u2014N-(piperidin-3-yl)-5-(pyridin-2-ylethynyl)-3-ureidothiophene-2-carboxamide; 11) (S)-5-((4-cyanophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 12) (S)-5-((1H-indazol-3-yl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 13) (S)-5-((6-fluoropyridin-3-yl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 14) (S)-5-((3,4-difluorophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 15) (S)-5-((1-methyl-1H-pyrazol-4-yl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 16) (S)\u2014N-(piperidin-3-yl)-5-((4-(trifluoromethyl)phenyl)ethynyl)-3-ureidothiophene-2-carboxamide; 17) (S)\u2014N-(piperidin-3-yl)-5-((6-(trifluoromethyl)pyridin-3-yl)ethynyl)-3-ureidothiophene-2-carboxamide; 18) methyl (S)-4-((5-(piperidin-3-ylcarbamoyl)-4-ureidothiophen-2-yl)ethynyl)benzoate; 19) (S)-5-((6-chloropyridin-3-yl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 20) (S)-5-((5-fluoropyridin-3-yl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 21) (S)-5-((2-fluoropyridin-4-yl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 22) (S)-5-((3-fluorophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 23) (S)-5-((1-(1-(methylsulfonyl)piperidin-4-yl)-1H-pyrazol-4-yl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 24) (S)\u2014N-(piperidin-3-yl)-5-(p-tolylethynyl)-3-ureidothiophene-2-carboxamide; 25) (S)-5-((3-bromo-4-cyanophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 26) (S)-5-((4-cyano-3-fluorophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 27) (S)-5-((3-fluoro-4-(trifluoromethyl)phenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 28) (S)-5-((4-chloro-3-cyanophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 29) (S)-5-((2-chloropyrimidin-5-yl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 30) (S)\u2014N-(piperidin-3-yl)-5-(pyrazin-2-ylethynyl)-3-ureidothiophene-2-carboxamide; 31) (S)-5-((4-chloro-3-fluorophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 32) (S)-5-((3,5-difluorophenyl)ethynyl)-N-(piperidin-3-yl) 3-ureidothiophene-2-carboxamide; 33) (S)-5-((2-fluorophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 34) (S)-5-((2,3-difluorophenyl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 35) (S)-5-((6-methylpyridin-3-yl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 36) (S)\u2014N-(piperidin-3-yl)-5-((6-(pyrrolidin-1-yl)pyridin-3-yl)ethynyl)-3-ureidothiophene-2-carboxamide; 37) (S)-5-((6-(piperidin-1-yl)pyridin-3-yl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 38) (S)-5-((6-morpholinopyridin-3-yl)ethynyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 39) 5-((1-methyl-1H-pyrazol-4-yl)ethynyl)-N-(pyrrolidin-3-yl)-3-ureidothiophene-2-carboxamide; 40) 5-((3-fluorophenyl)ethynyl)-N-(pyrrolidin-3-yl)-3-ureidothiophene-2-carboxamide; 41) (S)\u2014N-(azepan-3-yl)-5-((1-methyl-1H-pyrazol-4-yl)ethynyl)-3-ureidothiophene-2-carboxamide; 42) (S)-5-((1H-pyrazol-4-yl)ethynyl)-N-(azepan-3-yl)-3-ureidothiophene-2-carboxamide; 43) (S)\u2014N-(azepan-3-yl)-5-((1-ethyl-1H-pyrazol-4-yl)ethynyl)-3-ureidothiophene-2-carboxamide; 44) (S)\u2014N-(azepan-3-yl)-5-((1-isopropyl-1H-pyrazol-4-yl)ethynyl)-3-ureidothiophene-2-carboxamide; 45) (S)\u2014N-(azepan-3-yl)-5-((1-(2-methoxyethyl)-1H-pyrazol-4 yl)ethynyl)-3-ureidothiophene-2-carboxamide; 46) (S)\u2014N-(azepan-3-yl)-5-((1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)ethynyl)-3-ureidothiophene-2-carboxamide; 47) (S)\u2014N-(azepan-3-yl)-5-((1-(1-methylsulfonyl)piperidin-4-yl)-1H-pyrazol-4-yl)ethynyl)-3-ureidothiophene-2-carboxamide; 48) (S)\u2014N-(azepan-3-yl)-5-(thiophen-3-ylethynyl)-3-ureidothiophene-2-carboxamide; 49) (S)-5-((1-(1-(acetylpiperidin-4-yl)-1H-pyrazol-4-yl)ethynyl)-N-(azepan-3-yl)-3-ureidothiophene-2-carboxamide; 50) (S)\u2014N-(azepan-3-yl)-5-((3-fluorophenyl)ethynyl)-3-ureidothiophene-2-carboxamide; 51) 5-(2-((1-methyl-1H-pyrazol-4-yl)ethyl)-N-(pyrrolidin-3-yl)-3-ureidothiophene-2-carboxamide; 52) (S)\u2014N-(azepan-3-yl)-5-(2-(1-methyl-1H-pyrazol-4-yl)ethyl)-3-ureidothiophene-2-carboxamide; 53) (S)-5-(3-fluoro phenethyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide; 54) (S)\u2014N-(azepan-3-yl)-5-(3-fluorophenethyl)-3-ureidothiophene-2-carboxamide; and 55) 5-(3-fluorophenethyl)-N-(pyrrolidin-3-yl)-3-ureidothiophene-2-carboxamide.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 96.0
- Lexical Diversity: 1.2069
- Patent Class: 546.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15370631', '14153891', '13834316', '13980182', '13080762']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8205120979804568
- 35 USC 102 Novelty (BERT): 0.4936312331137773
- Combined Prediction Score: 0.7878240114937888
- Mean Citation Score: 258.022286
- Max Citation Score: 262.91245
- Similarity Product: 205.9780400512696

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

Dataset: test