Title:
SMALL-MOLECULE COMPOUND SPAM1 FOR UP-REGULATING NEUROPEPTIDE PACAP AND RECEPTOR PAC1-R THEREOF, AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/226814
Kind Code:
A1
Abstract:
Disclosed are a small-molecule compound SPAM1 for up-regulating a neuropeptide PACAP and a receptor PAC1-R thereof, and a preparation method therefor and an application thereof. The structure of the SPAM1 is as shown in formula (I), wherein R=none or H 2O or HCl; the SPAM1 is small in molecular weight, and can efficiently pass through biological barriers comprising a blood brain barrier, a blood testis barrier, and the like; the SPAM1 up-regulates, by positive feedback, expression of a neurotransmitter/neuromodulator PACAP secreted by the hypothalamus-pituitary gland and a specific receptor PAC1-R of the PACAP and acts on downstream glands of the gonadal axis and the adrenal axis, and thus, the regulation and control effects for the PACAP are comprehensive; the SPAM1 specifically targets PAC1-R1, only acts on cells and tissues naturally expressing PAC1-R in an nervous system and an endocrine system, and has relatively small side effects. Therefore, the SPAM1 will become a novel small-molecule compound drug for effectively treating and preventing functional aging and disorder, closely related to the neuropeptide PACAP, of the nervous system, the endocrine system, and the immune system.
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Inventors:
YU RONGJIE (CN)
Application Number:
PCT/CN2020/089716
Publication Date:
November 18, 2021
Filing Date:
May 12, 2020
Export Citation:
Assignee:
YU RONGJIE (CN)
CHEN JIANHUAN (CN)
CHEN JIANHUAN (CN)
International Classes:
C07D239/90; A61P25/16; A61P25/28; A61P27/02
Foreign References:
| CN109293584A | 2019-02-01 |
Other References:
C O USIFOH: "3-Propynyl-2substituted Carboxylic Acid Derivatives of Quinazolinone", SCIENTIA PHARMAZEUTICA, vol. 68, no. 3, 1 August 2000 (2000-08-01), pages 275 - 279, XP055867003, DOI: 10.3797/scipharm.aut-00-25
HUANG XIAOLING; LI JUNFENG; SONG SUQIN; WANG LIKE; LIN ZHUOCHAO; OUYANG ZEHUA; YU RONGJIE: "Hormesis effect of hydrogen peroxide on the promoter activity of neuropeptide receptor PAC1‐R", JOURNAL OF FOOD BIOCHEMISTRY, vol. 43, no. 7, 4 July 2019 (2019-07-04), US, pages 1 - 7, XP055867009, ISSN: 0145-8884, DOI: 10.1111/jfbc.12877
See also references of EP 4155295A4
HUANG XIAOLING; LI JUNFENG; SONG SUQIN; WANG LIKE; LIN ZHUOCHAO; OUYANG ZEHUA; YU RONGJIE: "Hormesis effect of hydrogen peroxide on the promoter activity of neuropeptide receptor PAC1‐R", JOURNAL OF FOOD BIOCHEMISTRY, vol. 43, no. 7, 4 July 2019 (2019-07-04), US, pages 1 - 7, XP055867009, ISSN: 0145-8884, DOI: 10.1111/jfbc.12877
See also references of EP 4155295A4
Attorney, Agent or Firm:
GUANGZHOU SHENYAN PATENT AGENT OFFICE (GENERAL PARTNERSHIP) (CN)
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