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好中球優位の炎症性疾患の治療のための9-デオキソ-9A-メチル-9A-アザ-9A-ホモエリスロマイシンA誘導体
专利权人:
グラクソ グループ リミテッド
发明人:
スレイマン、アリホジク,アントゥン、ヒュティネク,サンヤ、コストルン,マヤ、マタノビク、スクゴル,イバナ、パレイ、ジャコポビク
申请号:
JP2011546834
公开号:
JP2012516305A
申请日:
2010.01.28
申请国别(地区):
JP
年份:
2012
代理人:
摘要:
In the treatment of inflammatory diseases of the predominance of neutrophils, the present invention is in the treatment of diseases associated with cells altered function of neutrophils and / or inflammatory diseases of the predominance of neutrophils due to neutrophil infiltration, particularly useful formula (I) [Formula 1] In the formula, R 6 is, Substituted at the terminal carbon atom of (i) unsubstituted, or by a group selected -C 1-3 alkoxy and hydroxy -C from (O) OC 1-3 alkyl, or, - C 1-8 alkyl branched If you may be substituted by a hydroxyl group at each terminal carbon atom of the two, -C 1-8 alkyl, Heteroatoms selected from N (ii) O, and S, may be interposed in some cases, -CH (NH 2) C 1-4 alkyl,(R 7) (R 8), however, R 8 and R 7 does not represent H at the same time both CH 2 N represents a C 1-3 alkyl or H R 8 and (iii) R 7 are each independently , It contains two heteroatoms up independently chosen from N (iv) O, and S, substituted of unsubstituted or substituted by 1-3 alkyl -C, four - heterocyclic ring of six-membered , (V) a non-substituted, 1 to 3 groups selected independently or halo, hydroxyl, -C 1-3 alkyl, -C 1-3 alkoxy, -CF 3, and -NH 2 -OCF 3 six-membered heteroaromatic ring, - five substituted by (Vi) the aryl group is unsubstituted, and may be substituted by 1 or 2 substituents selected independently or hydroxyl -C 1-3 alkyl, 1-3 alkoxy -C, CH (NH 2) CH 2 - aryl, Or (vii) -C 3-7 cycloalkyl, and (viii) unsubstituted or halo, hydroxyl, -C 1-3 alkyl, -C 1-3 alkoxy, -CF 3, and -NH 2 -OCF 3 a phenyl which is substituted by one or two groups are independently selected. ] Or salts thereof 15-membered macrolides aza ride or 14-membered 2-O- substitution, methods of their preparation, their use as therapeutic agents, and to salts thereof.本発明は、好中球優位の炎症性疾患の治療において、特に好中球浸潤に起因する好中球優位の炎症性疾患および/または好中球の変化した細胞機能に関連した疾患の治療において有用な式(I)【化1】[式中、R6は、(i)無置換の、またはヒドロキシ-C1-3アルコキシおよび-C(O)OC1-3 アルキルから選択される基によって末端炭素原子において置換された、または、- C1-8アルキルが分岐している場合、2個の各末端炭素原子においてヒ
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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