Substituted pyrazolo{4,3-D}pyrimidines as kinase inhibitors
AssigneeOrigenis GmbH
InventorsMichael Thormann, Andreas Treml, Michael Almstetter, Nadine Traube
Life of this patent
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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.
Claims26
A compound of formula (I)
- wherein
- A is NH, O, S, C═O, NR4 or CR5R6;
- R1 is an optionally substituted alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl group;
- R2 is an optionally substituted alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl group, wherein R2 is bound to the pyrimidine ring of formula (I) via a carbon-carbon bond;
- R3 is a hydrogen atom, F, Cl, CH3, CF3, NO2, cyclopropyl, CN, N3, OH, SH, OMe, SMe, NHMe, NMe2 or NH2 group;
- R4 is an alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl group;
- R5 is a hydrogen atom, NO2, N3, OH, SH, NH2 or an alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl group;
- and
- R6 is a hydrogen atom, NO2, N3, OH, SH, NH2 or an alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl group;
- or a pharmaceutically acceptable salt, ester, solvate or hydrate thereof.
Dependencies are inferred from the claim text.