发明申请
US20130281657A1 MACROCYCLES AND MACROCYCLE STABILIZED PEPTIDES
有权
MACROCYCLES和MACROCYCLE STABILIZED PEPTIDES
- 专利标题: MACROCYCLES AND MACROCYCLE STABILIZED PEPTIDES
- 专利标题(中): MACROCYCLES和MACROCYCLE STABILIZED PEPTIDES
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申请号: US13879513申请日: 2011-10-13
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公开(公告)号: US20130281657A1公开(公告)日: 2013-10-24
- 发明人: Mark G. Saulnier , Dolatrai M. Vyas , David R. Langley , David B. Frennesson
- 申请人: Mark G. Saulnier , Dolatrai M. Vyas , David R. Langley , David B. Frennesson
- 申请人地址: US NJ Princeton
- 专利权人: Bristol-Myers Squibb Company
- 当前专利权人: Bristol-Myers Squibb Company
- 当前专利权人地址: US NJ Princeton
- 国际申请: PCT/US11/56124 WO 20111013
- 主分类号: C07K7/64
- IPC分类号: C07K7/64 ; C07K5/12
摘要:
The invention provides methods of preparing macrocycles including macrocycle stabilized peptides (MSPs). Macrocycles and MSPs are prepared according to nucleophilic capture of an iminoquinomethide type intermediate generated from a suitably substituted 2-amino-thiazol-5-yl carbinol. The preferred nucleophile may be selected from an electron rich aromatic moiety in the case of macrocycles and, in the case of MSPs, at least one amino acid comprises an electron rich aromatic moiety. In addition, the concept can be extended to other related 5-membered heterocyclic systems in place of the thiazole, such as imidazole or oxazole. The conditions for the generation of the corresponding iminoquinomethide type intermediates may be similar or different than the conditions used for the 2-amino-thiazol-5-yl carbinol.
公开/授权文献
- US09169295B2 Macrocycles and macrocycle stabilized peptides 公开/授权日:2015-10-27