[發明專利]肽有效
| 申請號： | 201580060378.3 | 申請日： | 2015-11-25 |
| 公開（公告）號： | CN107001423B | 公開（公告）日： | 2020-10-16 |
| 發明（設計）人： | 佩爾-奧拉·弗雷斯克加德;埃里克·A·基塔斯 | 申請（專利權）人： | 豪夫邁·羅氏有限公司 |
| 主分類號： | C07K7/08 | 分類號： | C07K7/08;A61K38/10;A61P25/28 |
| 代理公司： | 中科專利商標代理有限責任公司 11021 | 代理人： | 張國梁;程金山 |
| 地址： | 瑞士*** | 國省代碼： | 暫無信息 |
| 權利要求書： | 查看更多 | 說明書： | 查看更多 |
| 摘要： | |||
| 搜索關鍵詞： | 肽 | ||
1.一種雙位點BACE1抑制劑，其結合BACE酶的酶活性位點和催化結構域二者，其選自由以下組成的組：
Tyr-Pro-Lys-Phe-Ile-Pro-Leu-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(棕櫚酰)-NH2，
Tyr-Pro-Lys-Phe-Ile-Pro-Leu-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(棕櫚腦酰基)-NH2，
Tyr-Pro-Lys-Phe-Ile-Pro-Leu-Gly-DLys-Gly-G1u-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(油酰基)-NH2，
Tyr-Pro-Lys-Phe-Ile-Pro-Leu-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(反油酰基)-NH2，
Tyr-Pro-Lys-Phe-Ile-Pro-Leu-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(異油酰基)-NH2，
Tyr-Pro-Lys-Phe-Ile-Pro-Leu-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(芥酰基)-NH2，
Tyr-Pro-Lys-Phe-Ile-Pro-Leu-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(肉豆蔻腦酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-DLys-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(棕櫚酰)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-DLys-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(棕櫚腦酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-DLys-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(油酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-DLys-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(反油酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-DLys-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(異油酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-DLys-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(芥酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-DLys-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(肉豆蔻腦酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-(PEG)3-Glu-Val-Asn-MetSta-Val-Ala-Glu-DPhe-Lys(棕櫚酰)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-(PEG)4-Glu-Val-Asn-MetSta-Val-Ala-Glu-DPhe-Lys(棕櫚酰)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Ala-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-DAla-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-DLys-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(棕櫚酰)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-DPro-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Ala-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-DAla-DLys-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-DAla-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(棕櫚酰)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-DPro-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Ala-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-DAla-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-DLys-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(棕櫚酰)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-DPro-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Gly-Gly-Glu-Val-Asn-MetSta-Val-Ala-Glu-DPhe-Lys(棕櫚酰)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Gly-Gly-Gly-Glu-Val-Asn-MetSta-Val-Ala-Glu-DPhe-Lys(棕櫚酰)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Lys-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(棕櫚酰)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Nle-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Pro-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Ser-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Lys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(棕櫚酰)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Nle-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Om-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys(棕櫚酰)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Pro-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Ser-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro—T yr-Phe-lie-Pro-Leu-Lys-Gly-Gly-Glu—Val-Asn-Sta—Val-Ala-Glu—DPro-Lys(棕櫚酰)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Nle-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Pro-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，和
Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Ser-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys(棕櫚酰基)-NH2，
或其藥用鹽。
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