PATENT CLAIM ANALYSIS

Application Number: 15976037
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-09
Patent Classification: ["514", "249000"]

Abstract:
The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.

Claim (Index 25):
A method of treating a neurocognitive disorder comprising administering a compound of Formula (I) to a patient in need thereof. or a stereoisomeric form thereof, wherein R 1  is phenyl or 2-pyridinyl, each optionally substituted with one or more substituents each independently selected from the group consisting of halo, C 1-4 alkyl, monohalo-C 1-4 alkyl, polyhalo-C 1-4 alkyl-OH, \u2014CN, \u2014C 1-4 alkyl-O\u2014C 1-4 alkyl, C 3-7 cycloalkyl, \u2014O\u2014C 1-4 alkyl, monohalo-C 1-4 alkyloxy, polyhalo-C 1-4 alkyloxy, SF 5 , C 1-4 alkylthio, monohalo-C 1-4 alkylthio and polyhalo-C 1-4 alkylthio; R 2  is selected from the group consisting of hydrogen; C 1-4 alkyl; C 3-7 cycloalkyl; Het 1 ; Aryl; \u2014C(O)R 5 ; \u2014C(O)Het 2 ; Het 2 ; and C 1-4 alkyl substituted with one or more substituents each independently selected from the group consisting of halo, C 3-7 cycloalkyl, Aryl, Het 1  and Het 2 ; R 5  is selected from the group consisting of hydrogen, C 1-4 alkyl and C 3-7 cycloalkyl; Aryl is phenyl optionally substituted with one or more substituents each independently selected from the group consisting of halo, C 1-4 alkyl, \u2014C 1-4 alkyl-OH, monohalo-C 1-4 alkyl, polyhalo-C 1-4 alkyl, \u2014CN, \u2014OH, \u2014C 1-4 alkyl-O\u2014C 1-4 alkyl, \u2014NR\u2032R\u2033, \u2014NHC(O)C 1-4 alkyl, \u2014C(O)NR\u2032R\u2033, \u2014C(O)NH[C(O)C 1-4 alkyl], \u2014S(O) 2 NR\u2032R\u2033, \u2014S(O) 2 NH[C(O)C 1-4 alkyl] and \u2014S(O) 2 \u2014C 1-4 alkyl; Het 1  is selected from the group consisting of oxetanyl, tetrahydrofuranyl and tetrahydropyranyl; Het 2  is (a) a 6-membered aromatic heterocyclyl substituent selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl and pyridazinyl, each of which may be optionally substituted with one or more substituents each independently selected from the group consisting of halo, C 1-4 alkyl, \u2014C 1-4 alkyl-OH, monohalo-C 1-4 alkyl, polyhalo-C 1-4 alkyl, \u2014CN, \u2014O\u2014C 1-4 alkyl, \u2014OH, \u2014C 1-4 alkyl-O\u2014C 1-4 alkyl, \u2014NR\u2032R\u2033, \u2014NHC(O)C 1-4 alkyl, \u2014C(O)NR\u2032R\u2033, \u2014C(O)NH[C(O)C 1-4 alkyl], \u2014S(O) 2 NR\u2032R\u2033, \u2014S(O) 2 NH[C(O)C 1-4 alkyl] and \u2014S(O) 2 \u2014C 1-4 alkyl; or (b) a 5-membered aromatic heterocyclyl selected from the group consisting of thiazolyl, oxazolyl, 1H-pyrazolyl and 1H-imidazolyl, each of which may be optionally substituted with one or more substituents each independently selected from the group consisting of halo, C 1-4 alkyl, \u2014C 1-4 alkyl-OH, monohalo-C 1-4 alkyl, polyhalo-C 1-4 alkyl, \u2014CN, \u2014O\u2014C 1-4 alkyl, \u2014OH, \u2014C 1-4 alkyl-O\u2014C 1-4 alkyl, \u2014NR\u2032R\u2033, \u2014NHC(O)C 1-4 alkyl, \u2014C(O)NR\u2032R\u2033, \u2014C(O)NH[C(O)C 1-4 alkyl], \u2014S(O) 2 NR\u2032R\u2033, \u2014S(O) 2 NH[C(O)C 1-4 alkyl] and \u2014S(O) 2 \u2014C 1-4 alkyl; R\u2032 and R\u2033 are each independently selected from the group consisting of hydrogen and C 1-4 alkyl, R 3  is selected from the group consisting of hydrogen and C 1-4 alkyl; and R 4  is selected from the group consisting of hydrogen, C 1-4 alkyl, monohalo-C 1-4 alkyl, polyhalo-C 1-4 alkyl, \u2014C 1-4 alkyl-O\u2014C 1-4 alkyl and \u2014C 1-4 alkyl-OH; or a N-oxide, or a pharmaceutically acceptable salt thereof.

Metadata:
- Claim Count in Document: 26.0
- Percentile: 93.0
- Lexical Diversity: 1.55556
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15976223', '15500319', '15500600', '15500234', '15500205']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.783443607396113
- 35 USC 102 Novelty (BERT): 0.6050630743979606
- Combined Prediction Score: 0.7656055540962977
- Mean Citation Score: 449.709548
- Max Citation Score: 535.078
- Similarity Product: 472.5257409110069

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