CN104557928A - 一种含二环酰胺结构凝血因子Xa抑制剂、其制备方法及其用途 - Google Patents
一种含二环酰胺结构凝血因子Xa抑制剂、其制备方法及其用途 Download PDFInfo
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- CN104557928A CN104557928A CN201510083185.1A CN201510083185A CN104557928A CN 104557928 A CN104557928 A CN 104557928A CN 201510083185 A CN201510083185 A CN 201510083185A CN 104557928 A CN104557928 A CN 104557928A
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- PGOHTUIFYSHAQG-LJSDBVFPSA-N (2S)-6-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylsulfanylbutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-3-sulfanylpropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-carboxybutanoyl]amino]-5-oxopentanoyl]amino]hexanoic acid Chemical compound CSCC[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(O)=O PGOHTUIFYSHAQG-LJSDBVFPSA-N 0.000 title 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
化合物 | IC50(nM) |
Edoxaban | 3.9 |
参比化合物D-1 | 6.5 |
本发明化合物I | 3.7 |
Claims (3)
Priority Applications (1)
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CN201510083185.1A CN104557928B (zh) | 2015-02-14 | 2015-02-14 | 一种含二环酰胺结构凝血因子Xa抑制剂、其制备方法及其用途 |
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CN201510083185.1A CN104557928B (zh) | 2015-02-14 | 2015-02-14 | 一种含二环酰胺结构凝血因子Xa抑制剂、其制备方法及其用途 |
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CN104557928A true CN104557928A (zh) | 2015-04-29 |
CN104557928B CN104557928B (zh) | 2016-08-24 |
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Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1420882A (zh) * | 1999-07-28 | 2003-05-28 | 阿温蒂斯药物公司 | 取代的氧代氮杂杂环基化合物 |
CN101309919A (zh) * | 2005-11-16 | 2008-11-19 | 弗·哈夫曼-拉罗切有限公司 | 作为凝血因子xa抑制剂的新的吡咯烷衍生物 |
CN102015675A (zh) * | 2008-02-21 | 2011-04-13 | 赛诺菲-安万特 | 作为凝血因子Xa和凝血酶的抑制剂的氯噻吩-酰胺 |
US20120270879A1 (en) * | 2009-10-27 | 2012-10-25 | Boehringer Ingelheim International Gmbh | Heterocyclic Compounds As CCR1 Receptor Antagonists |
CN103242310A (zh) * | 2012-02-10 | 2013-08-14 | 苏州迈泰生物技术有限公司 | 吡唑并吡啶酮类化合物及其在制备抗凝血药物中的用途 |
CN103626749A (zh) * | 2012-08-21 | 2014-03-12 | 苏州泽璟生物制药有限公司 | 取代的噁唑烷酮化合物和包含该化合物的药物组合物及其用途 |
CN104136030A (zh) * | 2011-12-21 | 2014-11-05 | 赛诺菲 | 磺酰基氨基吡咯烷酮衍生物,及其制备及治疗应用 |
-
2015
- 2015-02-14 CN CN201510083185.1A patent/CN104557928B/zh active Active
Patent Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1420882A (zh) * | 1999-07-28 | 2003-05-28 | 阿温蒂斯药物公司 | 取代的氧代氮杂杂环基化合物 |
CN101309919A (zh) * | 2005-11-16 | 2008-11-19 | 弗·哈夫曼-拉罗切有限公司 | 作为凝血因子xa抑制剂的新的吡咯烷衍生物 |
CN102015675A (zh) * | 2008-02-21 | 2011-04-13 | 赛诺菲-安万特 | 作为凝血因子Xa和凝血酶的抑制剂的氯噻吩-酰胺 |
US20120270879A1 (en) * | 2009-10-27 | 2012-10-25 | Boehringer Ingelheim International Gmbh | Heterocyclic Compounds As CCR1 Receptor Antagonists |
CN104136030A (zh) * | 2011-12-21 | 2014-11-05 | 赛诺菲 | 磺酰基氨基吡咯烷酮衍生物,及其制备及治疗应用 |
CN103242310A (zh) * | 2012-02-10 | 2013-08-14 | 苏州迈泰生物技术有限公司 | 吡唑并吡啶酮类化合物及其在制备抗凝血药物中的用途 |
CN103626749A (zh) * | 2012-08-21 | 2014-03-12 | 苏州泽璟生物制药有限公司 | 取代的噁唑烷酮化合物和包含该化合物的药物组合物及其用途 |
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