PATENT CLAIM ANALYSIS

Application Number: 16005488
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2018-10
Patent Classification: ["514", "230500"]

Abstract:
The present invention provides compounds represented by formula (I), pharmaceutically acceptable salts thereof, N-oxides thereof, solvates thereof or prodrugs thereof (wherein the characters are as defined in the description). The compounds represented by formula (I) have affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 (GABA A  α5) and act as GABA A  α5 negative allosteric modulators (GABA A  α5 NAM), so that they are useful in the prevention and/or treatment of diseases which are related to the GABA A  α5 such as Alzheimer's disease.

Claim (Index 1):
A compound represented by formula (I): wherein A represents CR 4  or N; B represents CR 5  or N; D represents CR 6  or N; with the proviso that when A represents N, B must also represent N,\n Cyc 1  represents a (1) 5- to 15-membered mono-, bi- or tri-cyclic aromatic carbocyclic ring which may be partially saturated or (2) 5- to 15-membered mono-, bi- or tri-cyclic aromatic heterocyclic ring having 1 to 5 heteroatoms independently selected from nitrogen, oxygen and sulfur, which may be partially saturated; \n R 1  represents (1) 3- to 5-membered cycloalkyl wherein one carbon atom may be replaced by oxygen, which may be substituted with one or more groups independently selected from halogen and C1-4 alkyl which may be substituted with halogen or (2) C1-4 alkyl which may be substituted with halogen; \n R 2  represents hydrogen or C1-4 alkyl; \n R 3  represents (1) oxo, (2) halogen, (3) cyano, (4) hydroxy, (5) C1-6 alkyl which may be substituted with R 7 , (6) C1-6 alkoxy which may be substituted with R 7 , (7) 3- to 5-membered cycloalkyl wherein one carbon atom may be replaced by oxygen, which may be substituted with R 8 , (8) 5- to 12-membered mono- or bi-cyclic aromatic carbocyclic ring which may be partially or fully saturated and may be substituted with R 8  or (9) 5- to 12-membered mono- or bi-cyclic aromatic heterocyclic ring having 1 to 5 heteroatoms independently selected from nitrogen, oxygen and sulfur, which may be partially or fully saturated and may be substituted with R 8 ; \n R 4  represents hydrogen or halogen; \n R 5  represents (1) hydrogen, (2) halogen, (3) hydroxy, (4) cyano, (5) C1-6 alkyl which may be substituted with R 9 , (6) C2-6 alkenyl which may be substituted with R 9 , (7) C1-6 alkoxy which may be substituted with R 9 , (8) C1-6 alkyl-carbonyl which may be substituted with R 9  or (9) 3- to 5-membered cycloalkyl wherein one carbon atom may be replaced by oxygen, which may be substituted with R 9 ; \n R 6  represents hydrogen, halogen or C1-4 alkyl which may be substituted with halogen;\n R 7  represents (1) halogen, (2) hydroxy, (3) C1-4 alkoxy or (4)3- to 5-membered cycloalkyl wherein one carbon atom may be replaced by oxygen, which may be substituted with one or more groups independently selected from halogen and hydroxy; \n R 8  represents (1) oxo, (2) halogen, (3) cyano, (4) hydroxy, (5) C1-6 alkyl which may be substituted with one or more groups independently selected from halogen and hydroxy or (6) 3- to 5-membered cycloalkyl which may be substituted with one or more groups independently selected from halogen and hydroxy; \n R 9  represents halogen or hydroxy; \n n represents an integer of 0 to 2; and \n m represents an integer of 0 to 7, wherein when m represents an integer of 2 to 7, each R 3  may be same or different; \n with the proviso that when A is CH, B is N, D is CH, n is 1, R 1  is cyclopropyl and R 2  is hydrogen, then Cyc 1  is not benzene, pyridine, pyrazole or benzodioxole; \n with the proviso that (a) the compound represented by formula (I), wherein D is CH, and (1) R 1  is C1-4 alkyl which may be substituted with halogen or (2) n is 0 and R 1  is cycloalkyl, (b) (9-isopropyl-6-methyl-9H-purin-2-yl)-(5-piperazin-1-yl-pyridin-2-yl)-amine, (c) 9-butyl-6-chloro-N-(6-ethoxypyridin-3-yl)-9H-purin-2-amine, (d) 4-[(6-chloro-9-methyl-9H-purin-2-yl)amino]benzonitrile, (e) 6-chloro-9-(oxiran-2-ylmethyl)-N-phenyl-9H-purin-2-amine and (f) 6-chloro-9-(propan-2-yl)-N-(pyridin-4-yl)-9H-purin-2-amine are excluded, \n or a pharmaceutically acceptable salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof.

Metadata:
- Claim Count in Document: 27.0
- Percentile: 94.0
- Lexical Diversity: 1.64062
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['15112647', '14208067', '14376307', '10149852', '11942480']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8141787221089455
- 35 USC 102 Novelty (BERT): 0.5902445116357544
- Combined Prediction Score: 0.7917853010616264
- Mean Citation Score: 380.78577
- Max Citation Score: 515.1568
- Similarity Product: 438.9188125928878

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

Dataset: test