PATENT CLAIM ANALYSIS

Application Number: 16309999
Application Type: Utility
Filing Date: 2018-12
Publication Date: 2019-06
Patent Classification: ["514", "233200"]

Abstract:
The present invention relates to bicyclic pyridine, pyrazine, and pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kβ inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Claim (Index 1):
A compound of Formula (I) a tautomer or a stereoisomeric form thereof, wherein X 1  represents CH or N; X 2  represents CR 1  or N; provided that maximum one of X 1  and X 2  represents N; R 1  represents hydrogen, \u2014C(\u2550O)OH, \u2014C(\u2550O)NH 2 , \u2014NH 2 , \u2014CH 2 OH, Y represents \u2014CH 2 \u2014 or \u2014NH\u2014; R 2  represents R 3  represents C 1-4 alkyl; \u2014C(\u2550O)\u2014O\u2014C 1-4 alkyl; \u2014C(\u2550O)\u2014Het 1 ; \u2014CH(OH)\u2014CH 2 \u2014R q ; C 1-4 alkyl substituted on the same carbon atom with one \u2014OH and with one Het 1 ; or C 1-4 alkyl substituted with one substituent selected from the group consisting of halo, \u2014OH, \u2014NH 2 , \u2014O\u2014(C\u2550O)\u2014C 1-4 alkyl, \u2014(C\u2550O)\u2014O\u2014C 1-4 alkyl, \u2014NH\u2014(C\u2550O)\u2014C 1-4 alkyl, \u2014NH\u2014(SO 2 )\u2014C 1-4 alkyl, \u2014N(CH 3 )\u2014C 1-4 alkyl-SO 2 \u2014CH 3 , \u2014NH\u2014C 1-4 alkyl-SO 2 \u2014CH 3 , \u2014N(CH 3 )\u2014C 1-4 alkyl-OH, \u2014N(C\u2550O\u2014C 1-4 alkyl)-C 1-4 alkyl-OH, \u2014(C\u2550O)\u2014NH\u2014C 1-4 alkyl-OH, \u2014O\u2014(C\u2550O)\u2014CH(NH 2 )\u2014C 1-4 alkyl, \u2014O\u2014(C\u2550O)\u2014CH(NH 2 )\u2014C 1-4 alkyl-Ar, \u2014NH\u2014C 1-4 alkyl-OH, Het 1 , \u2014O\u2014C(\u2550O)\u2014C 1-4 alkyl-Het 1 , \u2014C(\u2550O)\u2014Het 1 , and \u2014NH\u2014C(\u2550O)\u2014Het 1 ;\n R q  represents Het 1 , halo, \u2014OH, \u2014NH 2 , \u2014O\u2014(C\u2550O)\u2014C 1-4 alkyl, \u2014NH\u2014(C\u2550O)\u2014C 1-4 alkyl, \u2014NH\u2014(SO 2 )\u2014C 1-4 alkyl, \u2014N(CH 3 )\u2014C 1-4 alkyl-SO 2 \u2014CH 3 , \u2014NH\u2014C 1-4 alkyl-SO 2 \u2014CH 3 , \u2014N(CH 3 )\u2014C 1-4 alkyl-OH, \u2014O\u2014(C\u2550O)\u2014CH(NH 2 )\u2014C 1-4 alkyl, \u2014O\u2014(C\u2550O)\u2014CH(NH 2 )\u2014C 1-4 alkyl-Ar, \n or \u2014NH\u2014C 1-4 alkyl-OH;\n Ar represents phenyl optionally substituted with one hydroxy; \n R 4a  represents hydrogen, C 1-4 alkyl, Het a , or C 1-4 alkyl substituted with one or more substituents each independently selected from the group consisting of \u2014OH, \u2014NR 5 R 6  and Het a ; \n R 4b  represents hydrogen, halo, C 1-4 alkyl, or C 1-4 alkyl substituted with one or more halo substituents; \n or R 4a  and R 4b  are taken together to form together with the phenyl ring to which they are attached a structure of Formula (a-1), (a-2), (a-3), (a-4) or (a-5): \n X represents \u2014NH\u2014, \u2014O\u2014, \u2014N(C 1-3 alkyl)-, or \u2014N(hydroxyC 1-3 alkyl)-; both R 7  substituents are the same and are selected from the group consisting of hydrogen, fluoro and methyl; or both R 7  substituents are taken together to form together with the common carbon atom to which they are attached a cyclopropyl, cyclobutyl or oxetanyl; both R 8  substituents are the same and are selected from the group consisting of hydrogen and methyl; or both R 8  substituents are taken together to form together with the common carbon atom to which they are attached a cyclopropyl, cyclobutyl or oxetanyl; R 5  represents hydrogen, C 1-6 alkyl, or C 1-6 alkyl substituted with one \u2014OH; R 6  represents hydrogen, C 1-6 alkyl, or C 1-6 alkyl substituted with one \u2014OH; Het 1  represents a 4-, 5- or 6-membered saturated heterocyclyl containing at least one heteroatom each independently selected from O, S, S(\u2550O) p  and N; said 4-, 5- or 6-membered saturated heterocyclyl is optionally substituted with one or two substituents each independently selected from the group consisting of halo, \u2014NH 2 , C 1-4 alkyl, \u2014S(\u2550O) 2 \u2014C 1-6 alkyl, \u2014C 1-4 alkyl-S(\u2550O) 2 \u2014C 1-6 alkyl, hydroxyl, C 1-4 alkyloxy, fluoro, cyano and C 1-4 alkyl substituted with one hydroxy; or two substituents on the same carbon atom of said 4-, 5- or 6-membered saturated heterocyclyl are taken together to form together with the common carbon atom to which they are attached Ring A; Ring A represents cyclobutyl, cyclopentyl, cyclohexyl or a 4-, 5- or 6-membered saturated heterocyclyl containing at least one heteroatom each independently selected from O, S, S(\u2550O) p  and N; said cyclobutyl, cyclopentyl, cyclohexyl or 4-, 5- or 6-membered saturated heterocyclyl is optionally substituted with one or two C 1-4 alkyl substituents, with one C 1-4 alkyl and one hydroxy substituent, or with one hydroxy substituent; each Het a  independently represents a 4-, 5- or 6-membered saturated heterocyclyl containing at least one heteroatom each independently selected from O, S, S(\u2550O) p  and N; said 4-, 5- or 6-membered saturated heterocyclyl is optionally substituted with one or two substituents each independently selected from the group consisting of C 1-4 alkyl, \u2014S(\u2550O) 2 \u2014C 1-6 alkyl, hydroxy, \u2014C 1-4 alkyl-S(\u2550O) 2 \u2014C 1-6 alkyl, and C 1-4 alkyl substituted with one hydroxy; or two substituents on the same carbon atom of said 4-, 5- or 6-membered saturated heterocyclyl are taken together to form together with the common carbon atom to which they are attached Ring B; Ring B represents cyclobutyl, cyclopentyl, cyclohexyl or a 4-, 5- or 6-membered saturated heterocyclyl containing at least one heteroatom each independently selected from O, S, S(\u2550O) p  and N; said cyclobutyl, cyclopentyl, cyclohexyl or 4-, 5- or 6-membered saturated heterocyclyl is optionally substituted with one or two C 1-4 alkyl substituents, with one C 1-4 alkyl and one hydroxy substituent, or with one hydroxy substituent; p represents 1 or 2; or a N-oxide, a pharmaceutically acceptable addition salt or a solvate thereof.

Metadata:
- Claim Count in Document: 32.0
- Percentile: 98.0
- Lexical Diversity: 1.51111
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15537619', '15537551', '15766887', '15604258', '14872527']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8410082304484001
- 35 USC 102 Novelty (BERT): 0.5762189183569291
- Combined Prediction Score: 0.814529299239253
- Mean Citation Score: 407.055672
- Max Citation Score: 474.54
- Similarity Product: 433.057869143486

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