PATENT CLAIM ANALYSIS

Application Number: 16327854
Application Type: Utility
Filing Date: 2019-02
Publication Date: 2019-06
Patent Classification: ["546", "269700"]

Abstract:
The present invention relates to novel substituted phenoxy- and benzyloxy-piperidine compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.

Claim (Index 5):
A compound of formula (I) according to  claim 1 , or a pharmaceutically acceptable salt thereof including any stereochemically isomeric form thereof, selected from the group: 1 2-chloro-6-fluoro-N-(2-{4-[(4-fluorophenyl)methoxy]piperidin-1-yl}-2-(4-methyl-1,3- thiazol-5-yl)ethyl)benzamide 2 2-chloro-N-(2-{4-[(4-chlorophenyl)methoxy]piperidin-1-yl}-2-(4-methyl-1,3-thiazol-5-yl) ethyl)-6-fluorobenzamide 3 2-chloro-6-fluoro-N-(2-{4-[(3-fluorophenyl)methoxy]piperidin-1-yl}-2-(4-methyl-1,3- thiazol-5-yl)ethyl)benzamide 4 2-chloro-6-fluoro-N-(2-{4-[(2-fluorophenyl)methoxy]piperidin-1-yl}-2-(4-methyl-1,3- thiazol-5-yl)ethyl)benzamide 5 2-chloro-N-(2-{4-[(3,5-difluorophenyl)methoxy]piperidin-1-yl}-2-(4-methyl-1,3-thiazol-5- yl)ethyl)-6-fluorobenzamide 6 2-chloro-N-(2-{4-[(3,4-difluorophenyl)methoxy]piperidin-1-yl}-2-(4-methyl-1,3-thiazol-5- yl)ethyl)-6-fluorobenzamide 7 2-chloro-6-fluoro-N-{2-[4-(4-fluorophenoxy)piperidin-1-yl]-2-(4-methyl-1,3-thiazol-5-yl) ethyl}benzamide 8 2-chloro-N-{2-[4-(4-chlorophenoxy)piperidin-1-yl]-2-(4-methyl-1,3-thiazol-5-yl)ethyl}-6- fluorobenzamide 9 2-chloro-6-fluoro-N-{2-[4-(3-fluorophenoxy)piperidin-1-yl]-2-(4-methyl-1,3-thiazol-5-yl) ethyl}benzamide 10 2-chloro-6-fluoro-N-{2-[4-(2-fluorophenoxy)piperidin-1-yl]-2-(4-methyl-1,3-thiazol-5-yl) ethyl}benzamide 11 2-chloro-N-{2-[4-(3,5-difluorophenoxy)piperidin-1-yl]-2-(4-methyl-1,3-thiazol-5-yl) ethyl}-6-fluorobenzamide 12 2-chloro-N-{2-[4-(3,4-difluorophenoxy)piperidin-1-yl]-2-(4-methyl-1,3-thiazol-5-yl) ethyl}-6-fluorobenzamide 13 N-(2-{4-[(4-fluorophenyl)methoxy]piperidin-1-yl}-2-(4-methyl-1,3-thiazol-5-yl)ethyl) quinoline-5-carboxamide 14 N-(2-{4-[(4-chlorophenyl)methoxy]piperidin-1-yl}-2-(4-methyl-1,3-thiazol-5-yl)ethyl) quinoline-5-carboxamide 15 N-(2-{4-[(3-fluorophenyl)methoxy]piperidin-1-yl}-2-(4-methyl-1,3-thiazol-5-yl)ethyl) quinoline-5-carboxamide 16 N-(2-{4-[(2-fluorophenyl)methoxy]piperidin-1-yl}-2-(4-methyl-1,3-thiazol-5-yl)ethyl) quinoline-5-carboxamide 17 N-(2-{4-[(3,5-difluorophenyl)methoxy]piperidin-1-yl}-2-(4-methyl-1,3-thiazol-5-yl)ethyl) quinoline-5-carboxamide 18 N-(2-{4-[(3,4-difluorophenyl)methoxy]piperidin-1-yl}-2-(4-methyl-1,3-thiazol-5-yl)ethyl) quinoline-5-carboxamide 19 N-{2-[4-(4-fluorophenoxy)piperidin-1-yl]-2-(4-methyl-1,3-thiazol-5-yl)ethyl}quinoline-5- carboxamide 20 N-{2-[4-(4-chlorophenoxy)piperidin-1-yl]-2-(4-methyl-1,3-thiazol-5-yl)ethyl}quinoline-5- carboxamide 21 N-{2-[4-(3-fluorophenoxy)piperidin-1-yl]-2-(4-methyl-1,3-thiazol-5-yl)ethyl}quinoline-5- carboxamide 22 N-{2-[4-(2-fluorophenoxy)piperidin-1-yl]-2-(4-methyl-1,3-thiazol-5-yl)ethyl}quinoline-5- carboxamide 23 N-{2-[4-(3,5-difluorophenoxy)piperidin-1-yl]-2-(4-methyl-1,3-thiazol-5-yl)ethyl}quinoline- 5-carboxamide 24 N-{2-[4-(3,4-difluorophenoxy)piperidin-1-yl]-2-(4-methyl-1,3-thiazol-5-yl)ethyl}quinoline- 5-carboxamide 25 2-chloro-N-{2-[4-(difluoromethyl)-1,3-thiazol-5-yl]-2-{4-[(2-fluorophenyl)methoxy] piperidin-1-yl}ethyl}-6-fluorobenzamide 26 2-chloro-N-{2-[4-(difluoromethyl)-1,3-thiazol-5-yl]-2-{4-[(3,5-difluorophenyl)methoxy] piperidin-1-yl}ethyl}-6-fluorobenzamide 27 2-chloro-N-{2-[4-(difluoromethyl)-1,3-thiazol-5-yl]-2-{4-[(3,4-difluorophenyl)methoxy] piperidin-1-yl}ethyl}-6-fluorobenzamide 28 2-chloro-N-{2-[4-(4-chlorophenoxy)piperidin-1-yl]-2-[4-(difluoromethyl)-1,3-thiazol-5-yl] ethyl}-6-fluorobenzamide 29 2-chloro-N-{2-[4-(difluoromethyl)-1,3-thiazol-5-yl]-2-[4-(3-fluorophenoxy)piperidin-1-yl] ethyl}-6-fluorobenzamide 30 2-chloro-N-{2-[4-(difluoromethyl)-1,3-thiazol-5-yl]-2-[4-(2-fluorophenoxy)piperidin-1-yl] ethyl}-6-fluorobenzamide 31 2-chloro-N-{2-[4-(difluoromethyl)-1,3-thiazol-5-yl]-2-[4-(3,5-difluorophenoxy)piperidin- 1-yl]ethyl}-6-fluorobenzamide 32 N-{2-[4-(difluoromethyl)-1,3-thiazol-5-yl]-2-{4-[(2-fluorophenyl)methoxy]piperidin-1-yl} ethyl}quinoline-5-carboxamide 33 N-{2-[4-(difluoromethyl)-1,3-thiazol-5-yl]-2-{4-[(3,4-difluorophenyl)methoxy]piperidin- 1-yl}ethyl}quinoline-5-carboxamide 34 N-{2-[4-(difluoromethyl)-1,3-thiazol-5-yl]-2-[4-(4-fluorophenoxy)piperidin-1-yl]ethyl} quinoline-5-carboxamide 35 N-{2-[4-(4-chlorophenoxy)piperidin-1-yl]-2-[4-(difluoromethyl)-1,3-thiazol-5-yl]ethyl} quinoline-5-carboxamide 36 N-{2-[4-(difluoromethyl)-1,3-thiazol-5-yl]-2-[4-(3-fluorophenoxy)piperidin-1-yl]ethyl} quinoline-5-carboxamide 37 N-{2-[4-(difluoromethyl)-1,3-thiazol-5-yl]-2-[4-(2-fluorophenoxy)piperidin-1-yl]ethyl} quinoline-5-carboxamide 38 N-{2-[4-(difluoromethyl)-1,3-thiazol-5-yl]-2-[4-(3,5-difluorophenoxy)piperidin-1-yl]ethyl} quinoline-5-carboxamide

Metadata:
- Claim Count in Document: 4.0
- Percentile: 99.0
- Lexical Diversity: 1.31111
- Patent Class: 546.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15115963', '14747485', '15763281', '15176597', '13057510']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7966493783816068
- 35 USC 102 Novelty (BERT): 0.5207302321116999
- Combined Prediction Score: 0.7690574637546161
- Mean Citation Score: 282.820674
- Max Citation Score: 340.03296
- Similarity Product: 290.48209876888274

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

Dataset: test