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NOUVEAUX COMPOSÉS ANTAGONISTES DU RÉCEPTEUR DE LA NEUROKININE 1
专利权人:
Leo Pharma A/S
发明人:
申请号:
EP13720801.3
公开号:
EP2817312A1
申请日:
2013.02.20
申请国别(地区):
EP
年份:
2014
代理人:
摘要:
The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(═O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(═O)R7, C(═O)OR7, C(═O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(═O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ═CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically acceptable salt or solvate thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating or ameliorating pruritic dermal diseases or conditions with said compounds, and to the use of said compounds in the manufacture of medicaments.La présente invention concerne un composé selon la formule (A) dans laquelle n vaut 1 ou 2 ; R1 et R2 représentent indépendamment hydrogène, C1-4-alkyle, C1-4-halogénoalkyle, C1-4-alcoxy, CD3 ou halogène ; R3 représente hydrogène, C(=O)OR7 ou C1-4-alkyle éventuellement substitué par hydroxy ou NR8R9 ; R4 représente hydrogène ou oxo ; R5 et R6 représentent indépendamment hydrogène, hydroxy, NR8R9, C(=O)R7, C(=O)OR7, C(=O)NR8R9, C1-4-alkyle, ledit C1-4-alkyle étant éventuellement substitué par hydroxy, NR8R9 ou un cycle hétérocyclique à 5 ou 6 chaînons, ledit cyc
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