发明申请
- 专利标题: IDO INHIBITORS AND THERAPEUTIC USES THEREOF
- 专利标题(中): IDO抑制剂及其治疗用途
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申请号: US12736526申请日: 2009-04-15
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公开(公告)号: US20110112282A1公开(公告)日: 2011-05-12
- 发明人: Ute Roehrig , Loay Awad , Olivier Michelin , Benoit Van Den Eynde , Luc Pilotte , Vincent Stroobant , Pierre Larrieu
- 申请人: Ute Roehrig , Loay Awad , Olivier Michelin , Benoit Van Den Eynde , Luc Pilotte , Vincent Stroobant , Pierre Larrieu
- 优先权: GB0806794.4 20080415
- 国际申请: PCT/EP2009/054482 WO 20090415
- 主分类号: C07H7/04
- IPC分类号: C07H7/04 ; C07D209/48 ; C07C211/58 ; C07C211/63 ; C07D215/38 ; C07C237/20 ; C07D207/16
摘要:
Compounds of formula (I), and pharmaceutically acceptable salts thereof, in which each compound is adapted to occupy the binding site of human IDO, which comprises a large hydrophobic pocket A and a second, proximal hydrophobic pocket B, the compound comprising at least one of the following elements: (i) a large hydrophobic fragment to substantially fill pocket A in the binding site of human IDO; (ii) an atom that can coordinate to the heme iron of human IDO, (iii) a positively charged group that can form a salt-bridge with the heme 7-propionate of the human IDO; (iv) a negatively charged group that can form a salt-bridge with Arg231 of the human IDO; (v) a hydrophobic group that can form van der Waals interactions with pocket B; and (vi) one or more substituents that can hydrogen bond to Ser167 and to Gly262, and as IDO inhibitors and their therapeutic use, eg in the treatment of cancer.
公开/授权文献
- US1626317A Rail-tie support 公开/授权日:1927-04-26
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