PATENT CLAIM ANALYSIS

Application Number: 15771487
Application Type: Utility
Filing Date: 2018-04
Publication Date: 2018-11
Patent Classification: ["514", "217060"]

Abstract:
To provide a compound having an inhibitory activity for an androgen receptor. A fused pyrimidine compound represented by the following formula (I) or a pharmaceutically acceptable thereof (in the formula, X, Y, Z, R 1 , and R 2  are as defined in the specification).

Claim (Index 11):
The compound or pharmaceutically acceptable salt thereof according to  claim 1 , wherein the compound is selected from the group consisting of the following compounds (1) to (48):\n (1) 6-((7-(3-chloro-4-cyanophenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)-N-ethyl-2-fluoronicotinamide; (2) 6-((7-(3-chloro-4-cyanophenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)-2-fluoro-N-methylnicotinamide; (3) 6-((7-(4-cyano-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)-2-fluoro-N-methylnicotinamide; (4) 6-((7-(4-cyano-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)-N-ethyl-2-fluoronicotinamide; (5) 6-((7-(4-cyano-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)-N-ethylnicotinamide; (6) 4-(4-((5-(azepane-1-carbonyl)pyridin-2-yl)amino)-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-2-(trifluoromethyl)benzonitrile; (7) N-(tert-butoxy)-6-((7-(4-cyano-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)nicotinamide; (8) tert-butyl (2-(6-((7-(4-cyano-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)pyridazine-3-carboxamido)ethyl)carbamate; (9) 6-((7-(4-cyano-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)-N-cyclopropylpyridazine-3-carboxamide; (10) 6-((7-(4-cyano-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)-N-ethylpyridazine-3-carboxamide; (11) 6-((7-(4-cyano-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)-N-(prop-2-yn-1-yl)pyridazine-3-carboxamide; (12) N-ethyl-2-fluoro-6-((7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)nicotinamide; (13) 2-(6-((7-(3-chloro-4-nitrophenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)pyridin-3-yl)propan-2-ol; (14) 2-(6-((7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)pyridin-3-yl)propan-2-ol; (15) 2-(6-((7-(3-methoxy-4-nitrophenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)pyridin-3-yl)propan-2-ol; (16) 2-(6-((7-(3-methyl-4-nitrophenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)pyridin-3-yl)propan-2-ol; (17) 2-(6-((7-(3-bromo-4-nitrophenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)pyridin-3-yl)propan-2-ol; (18) 2-(6-((7-(3-chloro-2-fluoro-4-nitrophenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)pyridin-3-yl)propan-2-ol; (19) 2-(6-((7-(3-isopropoxy-4-nitrophenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)pyridin-3-yl)propan-2-ol; (20) 4-(4-((5-(2-hydroxypropan-2-yl)pyridin-2-yl)amino)-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-2-methylbenzonitrile; (21) N-(3-fluoro-4-methoxyphenyl)-7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-amine; (22) 7-(3-chloro-4-nitrophenyl)-N-(3-fluoro-4-methoxyphenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-amine; (23) 4-(4-((5-(2-hydroxypropan-2-yl)pyridin-2-yl)amino)-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-2-methoxybenzonitrile; (24) 6-((7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)-N-(2,2,2-trifluoroethyl)pyridazine-3-carboxamide; (25) N-(6-methoxypyridin-3-yl)-7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-amine; (26) 4-(4-((3,4-dimethoxyphenyl)amino)-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-2-(trifluoromethyl)benzonitrile; (27) 4-(4-((4-(trifluoromethoxy)phenyl)amino)-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-2-(trifluoromethyl)benzonitrile; (28) 4-(4-((4-(2-oxa-6-azaspiro[3.3]heptan-6-yl)phenyl)amino)-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-2-chlorobenzonitrile; (29) tert-butyl 5-((7-(3-chloro-4-cyanophenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)isoindoline-2-carboxylate; (30) tert-butyl 4-(3-(2-chloro-4-((7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)phenoxy)propyl)piperazine-1-carboxylate; (31) N-(3,4-dimethoxyphenyl)-7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-amine; (32) tert-butyl 7-((7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)-3,4-dihydroisoquinoline-2(1H)-carboxylate; (33) N-(3-methyl-4-(2-oxa-6-azaspiro[3.3]heptan-6-yl)phenyl)-7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-amine; (34) N-([1,1\u2032-biphenyl]-3-yl)-7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-amine; (35) 2-chloro-4-(4-((6-fluoro-5-(3-hydroxyoxetan-3-yl)pyridin-2-yl)amino)-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)benzonitrile; (36) tert-butyl 7-((7-(3-chloro-4-cyanophenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)-3,4-dihydroisoquinolin-2(1H)-carboxylate; (37) 2-chloro-4-(4-((1,2,3,4-tetrahydroisoquinolin-7-yl)amino)-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)benzonitrile; (38) 2-chloro-4-(4-((4-(3-(piperazin-1-yl)propoxy)-3-(trifluoromethyl)phenyl)amino)-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)benzonitrile; (39) 1-(4-(3-(2-chloro-4-((7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)phenoxy)propyl)piperazin-1-yl)ethanone; (40) N-(3-chloro-4-(3-(4-(methylsulfonyl)piperazin-1-yl)propoxy)phenyl)-7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-amine; (41) N-(3-chloro-4-(3-(4-methylpiperazin-1-yl)propoxy)phenyl)-7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-amine; (42) 4-(4-((4-(3-(4-acetylpiperazin-1-yl)propoxy)-3-chlorophenyl)amino)-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-2-chlorobenzonitrile; (43) 4-(4-((4-(3-(4-acetylpiperazin-1-yl)propoxy)-3-(trifluoromethyl)phenyl)amino)-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-2-chlorobenzonitrile; (44) 4-(4-((4-(3-(4-acetylpiperazin-1-yl)propoxy)-2-(trifluoromethyl)phenyl)amino)-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-2-(trifluoromethyl)benzonitrile; (45) 1-(4-(3-(4-((7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)-2-(trifluoromethyl)phenoxy)propyl)piperazin-1-yl)ethanone; (46) 1-(4-(3-(4-((7-(4-nitro-3-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)amino)phenoxy)propyl)piperazin-1-yl)ethanone; (47) 7-(4-cyano-3-(trifluoromethyl)phenyl)-4-((4-methoxyphenyl)amino)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine-2-carbonitrile; and (48) 4-(4-((4-methoxyphenyl)amino)-2-methyl-5,6-dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-2-(trifluoromethyl)benzonitrile.

Metadata:
- Claim Count in Document: 38.0
- Percentile: 91.0
- Lexical Diversity: 1.375
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15203059', '15893804', '15023894', '13394525', '13796928']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8571995559102774
- 35 USC 102 Novelty (BERT): 0.5758492408894378
- Combined Prediction Score: 0.8290645244081934
- Mean Citation Score: 457.957174
- Max Citation Score: 524.8892
- Similarity Product: 382.8303004258632

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

Dataset: test