PATENT CLAIM ANALYSIS

Application Number: 16033395
Application Type: Utility
Filing Date: 2018-07
Publication Date: 2019-04
Patent Classification: ["546", "119000"]

Abstract:
The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

Claim (Index 1):
A compound according to formula (I): or a pharmaceutically acceptable salt thereof; wherein:\n L is selected from the group consisting of NH, CH 2 , S and O; \n R1 is selected from the group consisting of hydrogen, linear or branched C 1 -C 5  alkyl, C 1 -C 5  fluoroalkyl and saturated monocyclic C 3 -C 5  cycloalkyl; \n R2 is selected from the group consisting of linear or branched C 1 -C 8  alkyl, saturated monocyclic C 3 -C 8  cycloalkyl, oxetanyl, tetrahydrofuranyl, and tetrahydropyranyl; all of which can be optionally substituted one or more times with one or more substituents selected from the group consisting of methyl, fluorine, hydroxy, cyano and methoxy; \n R3 is methyl substituted with phenyl, pyridonyl, pyridinyl, pyrimidinyl or pyrazinyl all of which can be optionally substituted one or more times with one or more substituents selected from the group consisting of halogen, cyano, C 1 -C 3  alkyl, C 1 -C 3  fluoroalkyl, C 1 -C 3  fluoroalkoxy and C 1 -C 3  alkoxy; or \n R3 is methyl substituted with a 5-membered heteroaryl which is optionally substituted with one or more substituents selected from halogen, cyano, C 1 -C 3  alkyl, C 1 -C 3  fluoroalkyl, C 1 -C 3  fluoroalkoxy and C 1 -C 3  alkoxy; or \n R3 is ethyl substituted with phenyl, pyridonyl, pyridinyl, pyrimidinyl or pyrazinyl all of which can be optionally substituted one or more times with one or more substituents selected from the group consisting of halogen, cyano, C 1 -C 3  alkyl, C 1 -C 3  fluoroalkyl, C 1 -C 3  fluoroalkoxy and C 1 -C 3  alkoxy; or \n R3 is ethyl substituted with a 5-membered heteroaryl which is optionally substituted with one or more substituents selected from halogen, cyano, C 1 -C 3  alkyl, C 1 -C 3  fluoroalkyl, C 1 -C 3  fluoroalkoxy and C 1 -C 3  alkoxy; or \n L is CH 2  and R3 is NH which is substituted with phenyl, pyridonyl, pyridinyl, pyrimidinyl or pyrazinyl all of which can be optionally substituted one or more times with one or more substituents selected from the group consisting of halogen, cyano, C 1 -C 3  alkyl, C 1 -C 3  fluoroalkyl, C 1 -C 3  fluoroalkoxy and C 1 -C 3  alkoxy; or \n L is CH 2  and R3 is NH which is substituted with a 5-membered heteroaryl which is optionally substituted with one or more substituents selected from halogen, cyano, C 1 -C 3  alkyl, C 1 -C 3  fluoroalkyl, C 1 -C 3  fluoroalkoxy and C 1 -C 3  alkoxy; and \n R4 is phenyl, pyridinyl or pyridonyl all of which can be optionally substituted one or more times with one or more substituents selected from the group consisting of halogen, cyano, C 1 -C 4  alkyl, C 1 -C 4  fluoroalkyl, C 1 -C 4  deutereoalkyl, C 1 -C 3  fluoroalkoxy, cyclopropyloxy, C 1 -C 3  alkoxy, C 1 -C 3  deutereoalkoxy and N-R5R6 wherein R5 and R6 are each independently selected from H, C 1 -C 3  alkyl and C 1 -C 3  deutereoalkyl; or \n R4 is a 5-membered heteroaryl which is optionally substituted with one or more substituents selected from halogen, cyano, C 1 -C 4  alkyl, C 1 -C 4  fluoroalkyl, C 1 -C 4  deutereoalkyl, C 1 -C 3  fluoroalkoxy, cyclopropyloxy, C 1 -C 3  alkoxy, C 1 -C 3  deutereoalkoxy and N-R5R6 wherein R5 and R6 are each independently selected from H, C 1 -C 3  alkyl and C 1 -C 3  deutereoalkyl; or \n R4 is a 4, 5 or 6 membered saturated heterocycle all of which can be optionally substituted with one or more substituents selected from oxo, C 1 -C 4  alkyl and C 1 -C 4  fluoroalkyl.

Metadata:
- Claim Count in Document: 5.0
- Percentile: 95.0
- Lexical Diversity: 1.125
- Patent Class: 546.0
- Transitional Phrase Type: closed
- Component Type: 1
- Foreign Priority: True
- Related Applications: ['15637920', '15849798', '16340429', '12303618', '14671531']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.8440949483502062
- 35 USC 102 Novelty (BERT): 0.6269584448578853
- Combined Prediction Score: 0.8223812980009741
- Mean Citation Score: 413.943516
- Max Citation Score: 574.4137
- Similarity Product: 563.2283038673758

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