Substituted tetrazolo[1,5-a]pyrazines as ROR-gamma inhibitors

US9688684B2 · kind B2 · utility

Assignee

• Merck Patent GmbH · DE

Inventors

• Dirk Finsinger · Darmstadt, DE
• Margarita Wucherer-Plietker · Messel, DE
• Beatrix Blume · Bodenwerder, DE

Key dates

• Filing date: Nov 26, 2014
• Grant date: Jun 27, 2017
• Expiry date: Nov 26, 2034

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to tetrahydro-tetrazolo[1,5-a]pyrazine compounds of formula (I), wherein R1 denotes —R3, —CH2—R3 or —CO—R3; R2 denotes Ar2, Hetar2 or C3-7-cycloalkyl; and R3 denotes Ar3, Hetar3 or C3-7-cycloalkyl. These compounds are useful for inhibiting the retinoid-related orphan receptor γ (ROR γ, ROR-gamma) and for the prevention and/or treatment of medical conditions affected by ROR γ activity such as rheumatoid arthritis, multiple sclerosis, psoriasis, ulcerative colitis, asthma, autoimmune hepatitis or type 1 and type 2 diabetes.