PATENT CLAIM ANALYSIS

Application Number: 16245004
Application Type: Utility
Filing Date: 2019-01
Publication Date: 2019-05
Patent Classification: ["514", "253040"]

Abstract:
Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X 1 , X 2 , X 3  and X 4  have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.

Claim (Index 1):
A method of treating a RET-associated cancer in a subject in need thereof, wherein the cancer has a RET mutation selected from the group consisting of: S32L, D34S, L40P, P64L, R67H, R114H, V145G, V292M, R330Q, R360W, F393L, A510V, E511K, G513D, C515W, G533S, G550E, V591I, G593E, I602V, K603Q, C609W, C618W, F619F, C620L, E623K, D624N, C630R, C630Y, C630A, D631N, D631A, D631G, D631V, D631E, E632K, E632G, C634A, C634L, C634T, R635G, T636M, A640G, A641S, A641T, V648I, A664D, H665Q, K666M, K666N, S686N, R694Q, M700L, V706M, V706A, E713K, G736R, G748C, A750P, S765P, P766M, E768Q, L769L, R770Q, D771N, N777S, Q781R, E805K, Y806E, Y806F, Y806G, E818K, S819I, G823E, Y826M, Y826S, P841L, P841P, E843D, R844W, M848T, I852M, R873W, A876V, L881V, A883F, A883S, A883T, E884K, R886W, R897Q, D898V, E901K, S904F, K907E, K907M, R908K, G911D, R912Q, M918V, M918L, A919V, E921K, S922Y, F961L, R972G, R982C, M1009V, D1017N, V1041G, M1064T, G321R, C515S, G533C, R600Q, K603E, Y606C, C609S, C609G, C609R, C609F, C609W, C609C, C611S, C611F, C611R, C611G, C611W, C618Y, C618R, C618F, C618G, C620S, C620G, C620F, C620Y, C620W, C630F, C630S, D631Y, T636P, S649L, K666E, G691S, P766S, E768D, V778I, L790F, Y791F, R833C, R844L, R844Q, A866W, S904C, R912P, S922P, and T930M, the method comprising administering to the subject a compound selected from the group consisting of:\n ((S)-4-(6-(4-(2-hydroxy-3-phenylpropanoyl)piperazin-1-yl)pyridin-3-yl)-6-(l-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile; 6-(1-methyl-1H-pyrazol-4-yl)-4-(6-(4-(2-(pyridin-2-yl)acetyl)piperazin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile; 4-(6-(4-(2,6-difluorobenzoyl)piperazin-1-yl)pyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile 2,2,2-trifluoroacetate; 4-(5-(3-cyano-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-4-yl)pyridin-2-yl)-N,N-diethylpiperazine-1-carboxamide; 1-(5-(3-cyano-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-4-yl)pyridin-2-yl)-N-(2-methoxy-3-methylbutyl)piperidine-4-carboxamide; 4-(6-(4-(2-(5-fluoropyridin-2-yl)acetyl)piperazin-1-yl)pyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile bis(2,2,2-trifluoroacetate); 4-(6-(4-(2,6-difluorobenzyl)piperazin-1-yl)pyridine-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile; 4-(6-(4-(2-methoxybenzyl)piperazin-1-yl)pyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile; 6-(1-methyl-1H-pyrazol-4-yl)-4-(6-(4-(pyridine-2-ylmethyl)piperazin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile; 4-(6-(4-((6-methoxypyridin-3-yl)methyl)piperazin-1-yl)pyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile; BLU667 ((1s,4R)\u2014N\u2014((S)-1-(6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1H-pyrazol-3-yl)amino)pyrimidin-2-yl)cyclohexane-1-carboxamide); and RXDX-105 (1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea); or a pharmaceutically acceptable salt thereof.

Metadata:
- Claim Count in Document: 10.0
- Percentile: 99.0
- Lexical Diversity: 1.63462
- Patent Class: 514.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15858240', '15860852', '15860808', '15858929', '15860894']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8150644179595085
- 35 USC 102 Novelty (BERT): 0.558648203208559
- Combined Prediction Score: 0.7894227964844136
- Mean Citation Score: 448.1852
- Max Citation Score: 467.79102
- Similarity Product: 335.3197848695111

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