基本信息:
- 专利标题： ＮＦ-κＢ 억제제 및 그 용도
- 专利标题（英）：Nf-kb inhibitors and uses thereof
- 专利标题（中）：NF-KB抑制剂及其用途
- 申请号：KR1020047018676 申请日：2003-12-03
- 公开(公告)号：KR1020050044764A 公开(公告)日：2005-05-12
- 发明人： 테페,젯츠제이. , 페디브호틀라,새티야마헤쉬워
- 申请人： 미시간 스테이트 유니버시티
- 申请人地址： 미국, 미시간 *****, 이스트 란싱, 어드미니스트레이션 빌딩 ***
- 专利权人： 미시간 스테이트 유니버시티
- 当前专利权人： 미시간 스테이트 유니버시티
- 当前专利权人地址： 미국, 미시간 *****, 이스트 란싱, 어드미니스트레이션 빌딩 ***
- 代理人： 강석용; 강명구
- 优先权： US10/347,323 2003-01-17; US10/449,662 2003-05-30
- 国际申请： PCT/US2003/038261 2003-12-03
- 国际公布： WO2004066996 2004-08-12
- 主分类号： C07D233/28
- IPC分类号： C07D233/28 ; C07D233/26
摘要：
A new class of imidazolines as 4-position esters with very potent anti- inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma, etc.), antibacterial agents, and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-KB as well as potent activity against the Gram (+) bacterium. The compositions are also useful for treating autoimmune diseases and for inhibiting rejection of organ and tissue transplants.
摘要（中）：
描述了一类新的具有非常有效的抗炎和抗微生物活性的4-位酯的咪唑啉。 这些咪唑啉的合成包括适用于组合合成方法的多组分反应。 这两个关键特征的组合在治疗脓毒性休克以及许多其他炎症（关节炎和哮喘）和感染性疾病方面提供了有效的治疗药物。 描述了使用这种新型非甾体药物作为抗炎剂（用于治疗哮喘等），抗菌剂和防腐剂。 这些化合物也可用于治疗肿瘤（如癌症）。 咪唑啉是转录因子NF-κB的有效抑制剂以及对革兰氏阴性菌（+）细菌的有效活性。 所述组合物还可用于治疗自身免疫疾病和抑制器官和组织移植排斥反应。
公开/授权文献:
- KR100647386B1 ＮＦ-κＢ 억제제 및 그 용도 公开/授权日：2006-11-23
信息查询:
EspacenetIPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D233/00 | 杂环化合物，含1,3-二唑或氢化1,3-二唑环、不与其他环稠合 |
| --------C07D233/04 | .环原子间或环原子与非环原子间有1个双键 |
| ----------C07D233/28 | ..有杂原子或有以3个键连杂原子、其中最多以1个键连卤素的碳原子，例如，酯基或腈基，直接连在环碳原子上 |