FELDING, JAKOB,雅各 费汀,雅各 費汀,NIELSEN, SIMON FELDBAEK,赛蒙 费德贝克 尼尔森,賽蒙 費德貝克 尼爾森
申请号：
TW097122455
公开号：
TWI429433B
申请日:
2008.06.16
申请国别(地区):
TW
年份:
2014
代理人:
摘要：
The present invention relates to a compound according to formula Iwherein X1, X2, X3, X4and X5independently of each other represent -CH- or N or X3, X4and X5independently of each other represent -CH- or N, and X1and X2independently of each other represent C and form part of an additional 6-membered aromatic ring R1represents hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, hydroxyalkyl, or alkylcarbonyl, all of which are optionally substituted R2and R3independently represent hydrogen, -CH2-C(O)NR-R, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, haloalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, alkylalkoxycarbonyl, alkylcarbonyloxy, or alkoxyalkyl, all of which are optionally substituted R11represents hydrogen, halogen, cyano, amino, alkoxy or alkylamino, X1-X5represent -CH- or N, including N-oxides, enantiomers and diastereomers and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to processes for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.本發明係關於根據式I之化合物其中X1, X2, X3, X4及X5互相獨立地表示-CH-或N;或X3, X4及X5互相獨立地表示-CH-或N,且X1與X2互相獨立地表示C,及形成另一個6-員芳族環之一部份;R1表示氫、烷基、烯基、炔基、鹵烷基、羥烷基或烷羰基,其全部均視情況經取代;R2與R3係獨立表示氫、-CH2-C(O)NR-R、烷基、環烷基、烯基、環烯基、炔基、鹵烷基、羥烷基、雜環烯基、烷基芳基、烷基烷氧羰基、烷羰基氧基或烷氧烷基,其全部均視情況經取代;R11表示氫、鹵素、氰基、胺基、烷氧基或烷胺基,X1-X5表示-CH-或N,包括N-氧化物、對掌異構物及非對映異構物;及其藥學上可接受之鹽、水合物或溶劑合物。本發明係進一步關於製備該化合物之方法,該化合物供使用於治療上,包含該化合物之醫藥組合物,以該化合物治療疾病例如皮膚疾病之方法,及該化合物在藥劑製造上之用途。
