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Triazole compounds as blockers of the T-type calcium channels
专利权人:
Idorsia Pharmaceuticals Ltd
发明人:
BEZENCON, Olivier,GATFIELD, John,HEIDMANN, Bibia,SIEGRIST, Romain,STAMM, Simon,BEZENCON OLIVIER,GATFIELD JOHN,HEIDMANN BIBIA,SIEGRIST ROMAIN,STAMM SIMON
申请号:
ES15763321
公开号:
ES2693052T3
申请日:
2015.09.14
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound of formula (I) ** Formula ** in which X represents a ring carbon atom or a ring nitrogen atom; - R1 represents - (C2-6) alkyl; - (C2-4) alkyl mono-substituted with cyano, or (C1-3) alkoxy; - fluoroalkyl (C1-4); - fluoroalkoxy (C1-3); - pentafluoro sulfanyl; - (C3-6) -L1- cycloalkyl in which - said (C3-6) cycloalkyl optionally contains a ring oxygen atom; wherein said (C3-6) cycloalkyl is not substituted; or is mono-substituted with fluorine, (C1-3) alkyl, (C1-3) alkoxy, hydroxy, cyano, or (C1-3) fluoroalkyl; or is di-substituted with fluorine, or tri-substituted with two fluorine substituents and a (C 1-3) alkyl substituent; and - the L1 linker represents a direct bond, (C1-2) alkylene, oxygen, or (C1-2) -oxy alkylene; - 5- or 6-membered heteroaryl, independently and optionally mono-substituted with (C1-3) alkyl; - -NR11R12, in which - R11 and R12 independently represent hydrogen, (C1-3) alkyl, fluoroalkyl (C2-3), cycloalkyl (C3-6), cycloalkyl (C3-6) mono- or di-substituted by fluorine , (C3-6) cycloalkyl (C1-3) alkyl, (C1-3) alkoxy-(C2-3) alkyl; - or R11 and R12, together with the nitrogen atom to which they are attached, form a 4- to 6-membered ring which is optionally mono- or di-substituted with fluorine; a 2-oxo-pyrrolidinyl group; or a morpholinyl group; and (R4) n represents one or two optional substituents independently selected from (C1-4) alkyl, (C1-4) alkoxy, fluoroalkyl (C1-3), fluoroalkoxy (C1-3), halogen, and cyano; - or R1 together with (R4) n forms a 5 or 6 membered non-aromatic ring that is fused to the phenyl / pyridine ring; wherein said 5 or 6 member ring optionally contains one or two heteroatoms independently selected from oxygen and nitrogen; wherein said non-aromatic ring of 5 or 6 members independently is optionally and additionally mono-substituted with oxo; or di-, tri-, or tetra-substituted with one of the substituents is oxo and the rest are (C1-3) alkyl; - or R1 together with (R4) n forms a 5 or 6 membered aromatic ring that
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