公开(公告)号：EP2070940A1

公开(公告)日：2009-06-17

申请号：EP09075145.4

申请日：2004-04-23

申请人： GlaxoSmithKline istrazivacki centar Zagreb d.o.o.

发明人： Mercep, Mladen ,  Mesic, Milan ,  Tomaskovic, Linda ,  Markovic, Stribor ,  Hrvacic, Boska ,  Makaruha, Oresta ,  Poljak, Vionja

IPC分类号： C07J1/00 ,  C07D413/12 ,  C07D273/00

CPC分类号： C07D273/00 ,  C07D413/12 ,  C07D473/04 ,  C07H17/08 ,  C07J1/00

摘要： The present invention relates to new compounds represented by Formula I:

wherein M represents a macrolide subunit of the substructure II:

L represents the chain of the substructure III:

         -X 1 -(CH 2 ) m -Q-(CH 2 ) n -X 2 -      III

D represents the steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity;
The present invention relates also to pharmaceutically acceptable salts and solvates of such prepared compounds, to processe and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals.

摘要翻译： 本发明涉及由式I表示的新化合物：其中M表示亚结构II的大环内酯亚单位：L表示亚结构III的链：-X1-（CH2）mQ-（CH2）n-X2-III D表示 来自具有抗炎活性的类固醇或非甾体（NSAID）药物的类固醇或非甾体亚单位; 本发明还涉及这样制备的化合物的药学上可接受的盐和溶剂化物，用于其制备的加工和中间体，以及改善的治疗作用和用于治疗人类和动物中的炎性疾病和病症的用途。

公开(公告)号：EP1509528B1

公开(公告)日：2008-09-24

申请号：EP03755236.1

申请日：2003-05-20

申请人： GlaxoSmithKline istrazivacki centar Zagreb d.o.o.

发明人： Mercep, Mladen ,  Mesic,Milan ,  Rupcic, Renata ,  Pesic, Dijana

IPC分类号： C07D491/04 ,  C07D495/04 ,  C07D487/04 ,  C07D235/02 ,  A61K31/55 ,  A61P29/00

CPC分类号： C07D491/04 ,  C07D495/04

摘要： The present invention relates to 1,3-diaza-dibenzoazulene derivatives of formula (I), to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-α (TNF-α) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

公开(公告)号：EP2070940A3

公开(公告)日：2009-11-25

申请号：EP09075145.4

申请日：2004-04-23

申请人： GlaxoSmithKline istrazivacki centar Zagreb d.o.o.

发明人： Mercep, Mladen ,  Mesic, Milan ,  Tomaskovic, Linda ,  Markovic, Stribor ,  Hrvacic, Boska ,  Makaruha, Oresta ,  Poljak, Vionja

IPC分类号： C07J1/00 ,  C07D413/12 ,  C07D273/00

CPC分类号： C07D273/00 ,  C07D413/12 ,  C07D473/04 ,  C07H17/08 ,  C07J1/00

摘要： The present invention relates to new compounds represented by Formula I:

wherein M represents a macrolide subunit of the substructure II:

L represents the chain of the substructure III:

         -X 1 -(CH 2 ) m -Q-(CH 2 ) n -X 2 -      III

D represents the steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity;
The present invention relates also to pharmaceutically acceptable salts and solvates of such prepared compounds, to processe and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals.

公开(公告)号：EP2196469A1

公开(公告)日：2010-06-16

申请号：EP09075144.7

申请日：2005-10-27

申请人： GlaxoSmithKline istrazivacki centar Zagreb d.o.o.

发明人： Mercep, Mladen ,  Mesic, Milan ,  Tomaskovic, Linda ,  Markovic, Stribor ,  Poljak, Visnja ,  Sijan, Gordana ,  Selmani, Selvira

IPC分类号： C07J43/00 ,  C07D413/12 ,  C07D267/00 ,  A61K31/58 ,  A61P29/00

CPC分类号： C07J43/003 ,  C07D267/00 ,  C07D413/12

摘要： The present invention relates to new compounds represented by Formula I:

wherein M represents a macrolide subunit of the substructure VIII:

L represents the chain of the substructure IX or XIII:

         -X 1 -(CH 2 ) m -Q-(CH 2 ) n -X 2 -     IX

         -X 1 -(CH 2 ) m -V-(CH 2 ) p -Q-(CH 2 ) n -X 1 -     XIII

Z represents the steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity;
The present invention relates also to pharmaceutically acceptable salts and solvates of such prepared compounds, to processe and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals.

摘要翻译： 本发明涉及由式I表示的新化合物：其中M表示下结构VIII的大环内酯亚单位：L代表下结构IX或XIII的链：€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ -X 1 - （CH 2）m -Q-（CH 2）n -X 2 - €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ-X 1 - （CH 2）m -V-（CH 2）p -Q-（CH 2）n -X 1 - €ƒ€ƒ€ƒXIII Z代表衍生自类固醇或非甾体类固醇（NSAID）的类固醇或非甾体亚基 ）具有抗炎活性的药物; 本发明还涉及这些制备的化合物的药学上可接受的盐和溶剂化物，其制备方法和中间体，以及改进的治疗作用以及在治疗人和动物中的炎性疾病和病症中的用途。