PATENT CLAIM ANALYSIS

Application Number: 16231177
Application Type: Utility
Filing Date: 2018-12
Publication Date: 2019-08
Patent Classification: ["514", "265100"]

Abstract:
The present invention relates to compounds of formula I, wherein R 1  is phenyl, lower alkyl, C 3-6 -cycloalkyl, —CH 2 —C 3-6 -cycloalkyl, or bridged C 3-5 -cycloalkyl, optionally substituted by one, two or three substituents, selected from halogen, lower alkyl or lower alkyl substituted by halogen; R 2  is hydrogen, halogen, lower alkoxy, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; R 3  is a five membered heteroaryl group, selected from wherein R 6  is hydrogen or lower alkyl; R 7  is halogen or lower alkyl; R 8  is hydrogen or lower alkyl; R 9  is hydrogen or lower alkyl; R 4  is lower alkyl or lower alkyl substituted by hydroxy; R 5 /R 5′  is independently from each other hydrogen or lower alkyl; ( ) n - is —CH 2 — or —CH 2 CH 2 — for n being 1 or 2; X is CH or N;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):
The compound of  claim 2 , selected from the group consisting of:\n N2-(4-(4-Chloro-1H-imidazol-1-yl)-3-methoxyphenyl)-7-(4-fluorophenyl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; N2-(6-(4-Chloro-1H-imidazol-1-yl)-5-methoxypyridin-3-yl)-7-(4-fluorophenyl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; 7-(4-Fluorophenyl)-N2-(5-methoxy-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; N2-(4-(2,4-Dimethyl-1H-imidazol-1-yl)-3-fluorophenyl)-7-(4-fluorophenyl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; 7-(4-Fluorophenyl)-N4,5,5-trimethyl-N2-(4-(4-methyl-1H-imidazol-1-yl)phenyl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; N2-(6-(4-Chloro-1H-imidazol-1-yl)-5-methoxypyridin-3-yl)-7-(3,4-difluorophenyl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; 7-(3,4-Difluorophenyl)-N2-(5-methoxy-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; 7-(3,3-Difluorocyclobutyl)-N2-(5-methoxy-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; 7-(2,4-Difluorophenyl)-N2-(5-methoxy-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; N2-(5-Methoxy-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl)-N4,5,5-trimethyl-7-(3-(trifluoromethyl)bicyclo[1.1.1]pentan-1-yl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; N2-(6-(4-Chloro-1H-imidazol-1-yl)-5-methoxypyridin-3-yl)-7-(2,4-difluorophenyl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; N2-(5-Fluoro-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl)-7-(4-fluorophenyl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; 7-(2,4-Difluorophenyl)-N2-(5-fluoro-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; 2-((7-(4-Fluorophenyl)-2-((5-methoxy-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl)amino)-5,5-dimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)ethanol; 2-((2-((6-(4-Chloro-1H-imidazol-1-yl)-5-methoxypyridin-3-yl)amino)-7-(4-fluorophenyl)-5,5-dimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)ethanol; 7-(4-Fluorophenyl)-N2-(5-methoxy-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl)-N4-methyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; N2-(3-Fluoro-4-(4-methyl-1H-imidazol-1-yl)phenyl)-7-(4-fluorophenyl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; N2-(5-Fluoro-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl)-8-(4-fluorophenyl)-N4,5,5-trimethyl-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2,4-diamine; N2-(3-Fluoro-4-(4-methyl-1H-imidazol-1-yl)phenyl)-8-(4-fluorophenyl)-N4,5,5-trimethyl-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2,4-diamine; N2-(3-Fluoro-4-(4-methyl-1H-imidazol-1-yl)phenyl)-7-(4-fluorophenyl)-N4-methyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; 7-(4-Fluorophenyl)-N2-(5-methoxy-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl)-N4,5-dimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; 7-(2,3-Difluorophenyl)-N2-(5-fluoro-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; 7-(2,3-Difluorophenyl)-N2-(3-fluoro-4-(4-methyl-1H-imidazol-1-yl)phenyl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; 7-(2,3-Difluorophenyl)-N2-(5-methoxy-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; 7-(2-Chloro-4-fluorophenyl)-N2-(3-fluoro-4-(4-methyl-1H-imidazol-1-yl)phenyl)-N4,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; (S)\u2014N2-(3-Fluoro-4-(4-methyl-1H-imidazol-1-yl)phenyl)-7-(4-fluorophenyl)-N4,5-dimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine; and (R)\u2014N2-(3-Fluoro-4-(4-methyl-1H-imidazol-1-yl)phenyl)-7-(4-fluorophenyl)-N4,5-dimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-2,4-diamine.

Metadata:
- Claim Count in Document: 26.0
- Percentile: 98.0
- Lexical Diversity: 2.26667
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['16339345', '12845045', '14645033', '13013373', '10480958']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8129245272269738
- 35 USC 102 Novelty (BERT): 0.5491970369381364
- Combined Prediction Score: 0.7865517781980901
- Mean Citation Score: 378.725678
- Max Citation Score: 395.26392
- Similarity Product: 353.7784464629173

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