公开(公告)号：EP3315495A1

公开(公告)日：2018-05-02

申请号：EP16195622.2

申请日：2016-10-25

申请人： Universität Innsbruck ,  Friedrich-Schiller-Universität Jena ,  Institute of Experimental Botany, Academy of Sciences of the Czech Republic

发明人： Schuster, Daniela ,  Temml, Veronika ,  Kutil, Zsofia ,  Matuszczak, Barbara ,  Werz, Oliver ,  Garscha, Ulrike ,  Waltenberger, Birgit ,  Stuppner, Hermann

IPC分类号： C07D263/56 ,  C07D235/12 ,  C07D235/14 ,  C07D277/64 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/427 ,  A61P29/00

CPC分类号： C07D235/12 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/427 ,  C07D235/14 ,  C07D263/56 ,  C07D277/64

摘要： A compound according to formula I

wherein L is CH 2 -O, CH 2 -S, CH 2 -CH 2 , or CH=CH; R 1 and R 2 are independently selected out of H, halogen, C1 to C3 alkyl, halogenated C1 to C3 alkyl, C1 to C3 alkyloxy, or halogenated C1 to C3 alkyloxy; Ar is an aryl moiety, preferably phenyl or naphthyl, or a moncyclic- or bicyclic heteroaryl moiety, wherein optionally the aryl or heteroaryl moiety is further substituted; X is O, S, or NR 3 , wherein R 3 is H, C1 to C3 alkyl, halogenated C1 to C3 alkyl, or tert -butyloxycarbonyl; Y is O, S, NR 4 or N(R 4 )R 5 , wherein R 4 and R 5 are independently selected out of H or C1 to C3 alkyl; and wherein if Y is O, S, or NR 4 , then both A are NH, and the punctuated bonds represent a double bond to Y and single bonds to each A; or wherein if Y is N(R 4 )R 5 , then one A is N, the other A is NH, and the punctuated bonds represent a double bond to the A being N, a single bond to the A being NH and a single bond to Y; and use of such a compound in treatment or prevention of an inflammatory disease or an inflammation-related disorder.

摘要翻译： 根据式I的化合物，其中L是CH 2 -O，CH 2 -S，CH 2 -CH 2或CH = CH; R1和R2独立地选自H，卤素，C1至C3烷基，卤代C1至C3烷基，C1至C3烷氧基或卤代C1至C3烷氧基; Ar是芳基部分，优选苯基或萘基，或者单环 - 或双环杂芳基部分，其中任选地芳基或杂芳基部分被进一步取代; X为O，S或NR 3，其中R 3为H，C 1至C 3烷基，卤代C 1至C 3烷基或叔丁氧基羰基; Y是O，S，NR 4或N（R 4）R 5，其中R 4和R 5独立地选自H或C 1 -C 3烷基; 并且其中如果Y是O，S或NR 4，则两个A都是NH，并且中断的键代表与Y的双键和与每个A的单键; 或其中如果Y是N（R 4）R 5，则一个A是N，另一个A是NH，并且中断的键代表与A的双键为N，与A的单键为NH和与 Ÿ; 以及使用这样的化合物治疗或预防炎性疾病或炎症相关病症。