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Cianopirrolidinas derived compounds as inhibitors of USP - 30
专利权人:
MISSION THERAPEUTICS LIMITED
发明人:
MADIN, ANDREW,KEMP, MARK IAN,STOCKLEY, MARTIN LEE
申请号:
ARP170102707
公开号:
AR109755A1
申请日:
2017.09.29
申请国别(地区):
AR
年份:
2019
代理人:
摘要:
It describes a class of cianopirrolidinas replaced with desubiquitinación activity as inhibitors of Enzymes, in particularUbiquitin c-terminal hydrolase 30 or 30 ubiquitin specific peptidase (USP30), their uses, processes for their Preparation and compositions containing Said inhibitors.These inhibitors are useful in a variety of Therapeutic areas including Cancer and diseases involving mitochondrial dysfunction.Claim 1: a compound of the formula (1), a tautómero thereof, or a pharmaceutically acceptable Salt of the compound or tautómero, wherein: X is selected from o, N (rʰ)(rⁱ) and C (rʲ); rᵃ is selected from Hydrogen, fluoro,C₁₋₃ optionally substituted alkyl and alkoxy optionally substituted c₁₋₃; or rᵃ is joined to form a rᵇ or rʲ c₃₋₄ optionally substituted cycloalkyl Ring; rᵇ, rᶜ, rᵈ and rᵉ,Are each independently selected from Hydrogen,C₁₋₃ optionally substituted alkyl groups and one or more espirocíclicos where rᵇ is United to rᶜ or rᵈ rᵉ is joined to form a c₃₋₄ optionally substituted cycloalkyl or rᵇ is United to rᵃOr rᵉ is joined to form a rᶠ optionally substituted cycloalkyl c₃₋₄; rᶠ and rᵍ are each independently selected from Hydrogen, cyano, Fluorine,A c₁₋₃ alkoxy optionally substituted alkyl, optionally substituted c₁₋₃,And one or More groups espirocíclicos where rᶠ rᵍ is joined to form a ring c₃₋₄ optionally substituted cycloalkyl,Or rᶠ is United to rᵉ or rᵍ is joined to form a rʲ optionally substituted cycloalkyl c₃₋₄; when X is o or N (rʰ), none of rᵃ, rᶠ or rᵍ,It is c₁₋₃ alkoxy optionally substituted or fluoro; rʰ is selected from Hydrogen, alkyl, optionally substituted c₁₋₃, C (o) R, S (OR) ₂r ', and a heterociclilo heteroaryl ring,,Aryl or cycloalkyl of 3 to 6 members through a Linker alquileno c₀₋₃ alkyl; R 'is selected c₁₋₃ optionally substituted heteroaryl ring, and a heterociclilo,,Aryl or cycloalkyl of 3 to 6 members; and rⁱ rʲ are each independently selected from Hydrogen, cyano, Fluorine, c₁₋₃ alkoxy optionally substituted alkyl, optionall
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