PATENT CLAIM ANALYSIS

Application Number: 15983423
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-10
Patent Classification: ["514", "212070"]

Abstract:
The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

Claim (Index 16):
A compound selected from the group consisting of: 8-methoxy-N-(4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)-2H-pyrazolo[3,4-c]quinolin-4-amine; N-(4-fluoro-3-(methylsulfonyl)phenyl)-8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-amine; N-(3-((dimethylamino)methyl)phenyl)-8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-amine; (4-((8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl) (4-(4-methylpiperazin-1-yl)piperidin-1-yl)methanone; (3-((8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl) (morpholino)methanone; N-(3-(tert-butyl)phenyl)-8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-amine; 9-fluoro-N-(4-morpholinophenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(4-(4-cyclopropylpiperazin-1-yl)phenyl)-9-fluoro-3H-pyrazolo[3,4-c]quinolin-4-amine; 9-fluoro-N-(6-morpholinopyridin-3-yl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 6-((8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-yl)amino)-2,3-dihydrobenzo[b]thiophene 1,1-dioxide; 6-((8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-yl)amino)benzo[b]thiophene 1,1-dioxide; (4-((9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl) (morpholino)methanone; 9-methoxy-N-(4-(morpholinomethyl)phenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 9-methoxy-N-(3-methoxy-4-morpholinophenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 9-methoxy-N-(6-morpholinopyridin-3-yl)-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(1,3-dihydroisobenzofuran-5-yl)-9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-amine; 6-((9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)-2,3-dihydrobenzo[b]thiophene 1,1-dioxide; 6-((9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)benzo[b]thiophene 1,1-dioxide; 9-methoxy-N-(4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(4-((4-(4-methylpiperazin-1-yl)piperidin-1-yl)methyl)phenyl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(3-(morpholinomethyl)phenyl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 2-(3-((8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)-2-methylpropanenitrile; 3-(4-((8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)oxazolidin-2-one; N-(5-cyclopropyl-1H-pyrazol-3-yl)-9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(3-fluoro-4-morpholinophenyl)-9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(3-((dimethylamino)methyl)phenyl)-9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-amine; (4-((9-fluoro-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl) (morpholino)methanone; 9-fluoro-N-(4-(morpholinomethyl)phenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 9-fluoro-N-(3-methoxy-4-morpholinophenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(4-fluoro-3-(methylsulfonyl)phenyl)-9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-amine; 2-(3-((9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)-2-methylpropanenitrile; (2-fluoro-4-((8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)(morpholino)methanone; (4-((8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-yl)amino)-2-nitrophenyl) (morpholino)methanone; 8-methoxy-N-(4-(oxazol-2-yl)phenyl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(4-(oxazol-5-yl)phenyl)-2H-pyrazolo[3,4-c]quinolin-4-amine; N-(4-(4-(tert-butyl)piperazin-1-yl)phenyl)-9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-amine; (4-((9-methoxy- 3 H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl) (4-(4-methylpiperazin-1-yl)piperidin-1-yl)methanone; 3-(4-((9-methoxy-2H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)oxazolidin-2-one; 8-methoxy-N-(pyridazin-4-yl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(3-(methylsulfonyl)-4-nitrophenyl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 8-(methylthio)-N-(4-morpholinophenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(3-(methylsulfonyl)phenyl)-8-(methylthio)-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(3,4-dimethoxyphenyl)-8-(methylthio)-3H-pyrazolo[3,4-c]quinolin-4-amine; 1-(4-(4-((8-(methylthio)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)piperazin-1-yl)ethan-1-one; 7-((8-(methylthio)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)-3,4-dihydroquinolin-2(1H)-one; N-(4-((dimethylamino)methyl)phenyl)-8-(methylthio)-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(2-methylisoindolin-5-yl)-8-(methylthio)-3H-pyrazolo[3,4-c]quinolin-4-amine; 6-fluoro-N-(4-morpholinophenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 6-fluoro-N-(3-(methylsulfonyl)phenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(3,4-dimethoxyphenyl)-6-fluoro-3H-pyrazolo[3,4-c]quinolin-4-amine; 1-(4-(4-((6-fluoro-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)piperazin-1-yl)ethan-1-one; 7-((6-fluoro-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)-3,4-dihydroquinolin-2(1H)-one; 8-(methylsulfonyl)-N-(4-morpholinophenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(2-(methylthio)-1H-benzo[d]imidazol-5-yl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 9-methoxy-N-(4-(oxazol-5-yl)phenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 9-methoxy-N-(4-(oxazol-2-yl)phenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 9-methoxy-N-(4-(4-(methylsulfonyl)piperazin-1-yl)phenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 4-(4-((9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)morpholin-3-one; (4-((9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl) (pyrrolidin-1-yl)methanone; 1-(4-(4-((8-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)piperazin-1-yl)ethan-1-one; N-(3,4-dimethoxyphenyl)-8-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; (4-((8-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl) (morpholino)methanone; (4-methylpiperazin-1-yl) (4-((8-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)methanone; 4-((8-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)benzamide; N-(4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)-8-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 1-(4-((9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)pyrrolidin-2-one; (4-((9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl) (4-methylpiperazin-1-yl)methanone; 8-cyclopropyl-N-(3,4-dimethoxyphenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 5-((9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)-2-morpholinobenzonitrile; N-(3,4-dimethoxyphenyl)-8-methyl-3H-pyrazolo[3,4-c]quinolin-4-amine; 1-(4-(4-((8-methyl-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)piperazin-1-yl)ethan-1-one; 8-methyl-N-(4-morpholinophenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 8-methyl-N-(3-(methylsulfonyl)phenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 3-(4-((8-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)oxazolidin-2-one; 8-((8-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)-4,5-dihydro-1H-benzo[b]azepin-2(3H)-one; 8-(methylsulfonyl)-N-(3-(methylsulfonyl)phenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 9-methoxy-N-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(4-(4-(tert-butyl)piperazin-1-yl)phenyl)-8-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-8-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; N-cyclopropyl-8-methoxy-3H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(1-methyl-1H-pyrazol-4-yl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 5-(4-((8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)-1,3,4-oxadiazole-2-thiol; 8-methoxy-N-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(4-(4-morpholinopiperidin-1-yl)phenyl)-2H-pyrazolo[3,4-c]quinolin-4-amine; N5-(8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-yl)-N2,N2-dimethylpyridine-2,5-diamine; 9-methyl-N-(3-(methylsulfonyl)phenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 9-methyl-N-(4-morpholinophenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(3-(methylsulfonyl)-4-morpholinophenyl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 1-(4-(5-((8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-yl)amino)pyridin-2-yl)piperazin-1-yl)ethan-1-one; 9-(methylsulfonyl)-N-(4-morpholinophenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 1-(4-(4-((9-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)piperazin-1-yl)ethan-1-one; (4-((9-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl) (morpholino)methanone; N-(4-(4-(tert-butyl)piperazin-1-yl)phenyl)-9-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(6-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)pyridin-3-yl)-2H-pyrazolo[3,4-c]quinolin-4-amine; N-(4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)-9-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 8-((9-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)-4,5-dihydro-1H-benzo[b]azepin-2(3H)-one; N-(3,4-dimethoxyphenyl)-9-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-9-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 7-(methylsulfonyl)-N-(4-morpholinophenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 9-methoxy-N-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 8-(methylsulfonyl)-N-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(1,5-dimethyl-1H-pyrazol-4-yl)-8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-amine; N-(1,3-dimethyl-1H-pyrazol-4-yl)-8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-amine; 2-((4-((9-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)phenyl)amino)ethan-1-ol; 9-(methylsulfonyl)-N-(3-(methylsulfonyl)phenyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 9-(methylsulfonyl)-N-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(1-(2-methoxyethyl)-1H-pyrazol-4-yl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(1-(methylsulfonyl)-1H-pyrazol-4-yl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(1-(1-methylpiperidin-4-yl)-1H-pyrazol-4-yl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 1-(4-(4-((8-methoxy-2H-pyrazolo[3,4-c]quinolin-4-yl)amino)-1H-pyrazol-1-yl)piperidin-1-yl)ethan-1-one; N-(1-(2-methoxyethyl)-1H-pyrazol-4-yl)-8-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; N-(1-(1-methylpiperidin-4-yl)-1H-pyrazol-4-yl)-8-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 1-(4-(4-((8-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)-1H-pyrazol-1-yl)piperidin-1-yl)ethan-1-one; 9-methoxy-N-(1-(2-methoxyethyl)-1H-pyrazol-4-yl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 1-(4-(4-((9-methoxy-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)-1H-pyrazol-1-yl)piperidin-1-yl)ethan-1-one; 9-methoxy-N-(1-(1-methylpiperidin-4-yl)-1H-pyrazol-4-yl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 8-((7-(methylsulfonyl)-3H-pyrazolo[3,4-c]quinolin-4-yl)amino)-4,5-dihydro-1H-benzo[b]azepin-2(3H)-one; 7-(methylsulfonyl)-N-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)-3H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(1-methyl-1H-1,2,3-triazol-4-yl)-2H-pyrazolo[3,4-c]quinolin-4-amine; 8-methoxy-N-(2-methyl-2H-1,2,3-triazol-4-yl)-2H-pyrazolo[3,4-c]quinolin-4-amine; and 8-methoxy-N-(1-methyl-1H-pyrazol-3-yl)-2H-pyrazolo[3,4-c]quinolin-4-amine; or a pharmaceutically acceptable salt, ester, solvate or hydrate or a pharmaceutically acceptable formulation thereof.

Metadata:
- Claim Count in Document: 11.0
- Percentile: 93.0
- Lexical Diversity: 1.6087
- Patent Class: 514.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['14436152', '14436145', '13506509', '13506510', '13509442']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8710019054257945
- 35 USC 102 Novelty (BERT): 0.6620991337623586
- Combined Prediction Score: 0.8501116282594509
- Mean Citation Score: 565.8482339999998
- Max Citation Score: 663.3793
- Similarity Product: 637.9739041155577

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