PATENT CLAIM ANALYSIS

Application Number: 16224507
Application Type: Utility
Filing Date: 2018-12
Publication Date: 2019-06
Patent Classification: ["548", "262400"]

Abstract:
The present invention relates to compounds of formula wherein HetAr is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R 1  is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R 2  is lower alkyl substituted by halogen; R 3  is hydrogen, lower alkyl substituted by halogen, lower alkyl or lower alkyl substituted by hydroxy; Y is R 4  is lower alkoxy, lower alkoxy substituted by halogen or CN; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.

Claim (Index 3):
A compound of formula IA according to  claim 2 , wherein the compound is selected from the group consisting of:\n 5-(2,2,2-Trifluoroethoxy)-N-((8 endo)-3-(2-(trifluoromethyl)pyridin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; N-((8 endo)-3-(3-methylisothiazol-5-yl)-3-azabicyclo[3.2.1]octan-8-yl)-5-(2,2,2-trifluoroethoxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; 8-methyl-5-(2,2,2-trifluoroethoxy)-N-((8 endo)-3-(2-(trifluoromethyl)pyridin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; 8-methyl-N-((8 endo)-3-(6-methylpyrimidin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-5-(2,2,2-trifluoroethoxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; N-((8 endo)-3-(2-chloropyridin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-8-methyl-5-(2,2,2-trifluoroethoxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; N-((8 endo)-3-(2-methoxypyridin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-8-methyl-5-(2,2,2-trifluoroethoxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; N-((8 endo)-3-(6-chloropyridazin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-8-methyl-5-(2,2,2-trifluoroethoxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; 2-(5-(2,2,2-trifluoroethoxy)-2-(((8 endo)-3-(2-(trifluoromethyl)pyridin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)amino)-[1,2,4]triazolo[1,5-a]pyridin-8-yl)propan-2-ol; 2-(2-(((8 endo)-3-(6-methylpyrimidin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)amino)-5-(2,2,2-trifluoroethoxy)-[1,2,4]triazolo[1,5-a]pyridin-8-yl)propan-2-ol; 8-isopropyl-5-(2,2,2-trifluoroethoxy)-N-((8 endo)-3-(2-(trifluoromethyl)pyridin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; 8-isopropyl-N-((8 endo)-3-(6-methylpyrimidin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-5-(2,2,2-trifluoroethoxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; N-((8 endo)-3-(2-chloropyridin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-8-isopropyl-5-(2,2,2-trifluoroethoxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; 8-Isopropyl-N-((8 endo)-3-(2-methoxypyridin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-5-(2,2,2-trifluoroethoxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; N-((8 endo)-3-(6-chloropyridazin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-8-isopropyl-5-(2,2,2-trifluoroethoxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; 8-isopropyl-N-((8 endo)-3-(6-methoxypyridazin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-5-(2,2,2-trifluoroethoxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; 8-Isopropyl-N-((8 endo)-3-(3-methyl-1,2,4-oxadiazol-5-yl)-3-azabicyclo[3.2.1]octan-8-yl)-5-(2,2,2-trifluoroethoxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; 2-[2-[[(8 endo)-3-(6-methylpyrimidin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl]amino]-5-[(1S)-2,2,2-trifluoro-1-methyl-ethoxy]-[1,2,4]triazolo[1,5-a]pyridin-8-yl]propan-2-ol; 2-[2-[[(8 endo)-3-(6-chloropyridazin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl]amino]-5-[(1S)-2,2,2-trifluoro-1-methyl-ethoxy]-[1,2,4]triazolo[1,5-a]pyridin-8-yl]propan-2-ol; 8-isopropyl-N-((8 endo)-3-(2-methoxypyridin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-5-(((S)-1,1,1-trifluoropropan-2-yl)oxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; 8-isopropyl-N-((8 endo)-3-(6-methoxypyridazin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-5-(((S)-1,1,1-trifluoropropan-2-yl)oxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine . ; .  N-((8 endo)-3-(6-chloropyridazin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl)-8-isopropyl-5-(((S)-1,1,1-trifluoropropan-2-yl)oxy)-[1,2,4]triazolo[1,5-a]pyridin-2-amine; 8-isopropyl-N-[(8 endo)-3-(3-methyl-1,2,4-oxadiazol-5-yl)-3-azabicyclo[3.2.1]octan-8-yl]-5-[(1S)-2,2,2-trifluoro-1-methyl-ethoxy]-[1,2,4]triazolo[1,5-a]pyridin-2-amine; and 8-isopropyl-N-[(8 endo)-3-(5-methyl-1,3,4-oxadiazol-2-yl)-3-azabicyclo[3.2.1]octan-8-yl]-5-[(1S)-2,2,2-trifluoro-1-methyl-ethoxy]-[1,2,4]triazolo[1,5-a]pyridin-2-amine; or a pharmaceutically active acid addition salt thereof, a racemic mixture or its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof.

Metadata:
- Claim Count in Document: 16.0
- Percentile: 98.0
- Lexical Diversity: 1.86047
- Patent Class: 548.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['16004145', '15913087', '12843702', '16473507', '13215914']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8264559457272137
- 35 USC 102 Novelty (BERT): 0.6946527102718588
- Combined Prediction Score: 0.8132756221816783
- Mean Citation Score: 515.214988
- Max Citation Score: 771.7488400000003
- Similarity Product: 709.6259972162105

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