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新穎的神經激肽1受體拮抗劑化合物
专利权人:
LEO PHARMA A/S
发明人:
SORENSEN, MORTEN DAHL,索伦森 摩坦 戴尔,索倫森 摩坦 戴爾,FABIO, ROMANO DI,法比欧 罗曼诺 迪,法比歐 羅曼諾 迪,POZZAN, ALFONSO,宝禅 雅风硕,寶禪 雅風碩,CATALANI, MARIA PIA,卡特李妮 玛丽亚 别亚,卡特李妮 瑪麗亞 別亞,BLADH, HAAKON,布拉德 哈肯,FELDING, JAKOB,费汀 雅,索伦森 摩坦 戴尔,索倫森 摩坦 戴爾,法比欧 罗曼诺 迪,法比歐 羅曼諾 迪,宝禅 雅风硕,寶禪 雅風碩,卡特李妮 玛丽亚 别亚,卡特李妮 瑪麗亞 別亞,布拉德 哈肯,费汀 雅
申请号:
TW102106062
公开号:
TW201339161A
申请日:
2013.02.21
申请国别(地区):
TW
年份:
2013
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.本發明係關於一種式A化合物其中n為1或2;R1及R2獨立地為氫、C1-4烷基、C1-4鹵烷基、C1-4烷氧基、CD3或鹵素;R3為氫、C(=O)OR7或視情況經羥基或NR8R9取代之C1-4烷基;R4為氫或側氧基;R5及R6獨立地為氫、羥基、NR8R9、C(=O)R7、C(=O)OR7、C(=O)NR8R9、C1-4烷基,其中該C1-4烷基視情況經羥基、NR8R9或5員或6員雜環取代,其中該5員或6員雜環視情況經C1-4烷基或C(=O)R7取代;或R5及R6與其所連接之碳原子一起形成=CH2或5員或6員雜環烷基,其中該雜環烷基視情況經C1-4烷基取代;R7為氫或C1-4烷基;R8及R9獨立地為氫或C1-4烷基,或R8及R9與其所連接之氮原子一起形成5員或6員雜環,或其醫藥學上可接受之鹽或溶劑合物。本發明進一步係關於用於製備該等化合物之中間體,用於治療之該等化合物,包含該等化合物之醫藥組合物,用該等化合物治療或改善瘙癢性皮膚疾病或病狀之方法及該等化合物在藥物之製造中之用途。
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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