1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds as LRRK2, NUAK1 and/or TYK2 kinase modulators for the treatment of e.g. autoimmune disease

US12384788B2 · kind B2 · utility

Assignee

• Origenis GMBH · DE

Inventors

• Roland Koestler · Martinsried, DE
• Jean Tassel · Augsburg, DE
• Michael Thormann · Martinsried, DE
• Nasser Yehia · Martinsried, DE
• Andreas Treml · Martinsried, DE
• Michael Almstetter · Martinsried, DE

Key dates

• Filing date: Sep 11, 2020
• Grant date: Aug 12, 2025
• Expiry date: Dec 12, 2042

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D487/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to compounds of formula (I) that are capable of modulating, e.g., inhibiting or activating, one or more kinases, especially LRRK2 and/or NUAK1 and/or TYK2 or mutants thereof. The compounds are useful for treating diseases, such as 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. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 40 to 146; examples 1 to 63; compounds 1 to 248; tables 1 to 3). Preferred compounds are e.g. 1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds. An exemplary compound is e.g. 5-(2,6-difluorophenyl)-8-methoxy-1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine (example 49). (Formula (II):