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申请/专利权人：豪夫迈·罗氏有限公司

申请日：2015-11-25

公开（公告）日：2020-10-16

公开（公告）号：CN107001423B

专利技术分类：..含有12~20个氨基酸[2006.01]

专利摘要：本发明涉及双位点BACE1抑制剂，它们的制备，含有它们的药物组合物和它们作为治疗活性物质的用途。本发明的活性化合物可用于治疗性和或预防性处理例如阿尔茨海默病。

专利权项：1.一种双位点BACE1抑制剂，其结合BACE酶的酶活性位点和催化结构域二者，其选自由以下组成的组：Tyr-Pro-Lys-Phe-Ile-Pro-Leu-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys棕榈酰-NH2，Tyr-Pro-Lys-Phe-Ile-Pro-Leu-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys棕榈脑酰基-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异油酰基-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肉豆蔻脑酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-DLys-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys棕榈酰-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-DLys-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys棕榈脑酰基-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异油酰基-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肉豆蔻脑酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-PEG3-Glu-Val-Asn-MetSta-Val-Ala-Glu-DPhe-Lys棕榈酰-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-PEG4-Glu-Val-Asn-MetSta-Val-Ala-Glu-DPhe-Lys棕榈酰-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Ala-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-DAla-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-DLys-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys棕榈酰-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-DPro-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Ala-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-DAla-DLys-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-DAla-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-DLys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys棕榈酰-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-DPro-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Ala-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-DAla-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-DLys-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys棕榈酰-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-DPro-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Gly-Gly-Glu-Val-Asn-MetSta-Val-Ala-Glu-DPhe-Lys棕榈酰-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Gly-Gly-Gly-Glu-Val-Asn-MetSta-Val-Ala-Glu-DPhe-Lys棕榈酰-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Lys-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys棕榈酰-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Nle-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Pro-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Gly-Ser-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Lys-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys棕榈酰-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Nle-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Om-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-DPro-Lys棕榈酰-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Pro-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Gly-Ser-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro—Tyr-Phe-lie-Pro-Leu-Lys-Gly-Gly-Glu—Val-Asn-Sta—Val-Ala-Glu—DPro-Lys棕榈酰-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Nle-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Pro-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，和Tyr-Pro-Tyr-Phe-Ile-Pro-Leu-Ser-Gly-Gly-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe-Lys棕榈酰基-NH2，或其药用盐。

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