Title:
COMPOUND AND USE THEREOF IN PREPARATION OF DRUG FOR TARGETED INHIBITION OF PTL AND/OR NPC1L1
Document Type and Number:
WIPO Patent Application WO/2022/063071
Kind Code:
A1
Abstract:
Provided in the present invention are a novel inhibitor simultaneously targeting PTL and NPC1L1 and the use thereof. Namely, provided are a compound having a structure as represented by formula (I) and the use thereof in the preparation of a drug for inhibiting PTL and/or NPC1L1. The drug inhibits the intestinal absorption of triglycerides and cholesterol by means of simultaneously inhibiting PTL and NPC1L1. The drug is used for treating and/or preventing obesity, hypercholesterolemia, and related cardiovascular and cerebrovascular diseases. The novel compound prepared by the present invention exhibits a good activity in terms of simultaneously inhibiting PTL and NPC1L1, and has application value in the preparation of a drug for treating and/or preventing obesity, hypercholesterolemia, and related cardiovascular and cerebrovascular diseases.
Inventors:
XING DONGMING (CN)
ZHANG RENSHUAI (CN)
SONG ZHENGMING (CN)
ZHANG RENSHUAI (CN)
SONG ZHENGMING (CN)
Application Number:
PCT/CN2021/119276
Publication Date:
March 31, 2022
Filing Date:
September 18, 2021
Export Citation:
Assignee:
UNIV QINGDAO (CN)
AFFILIATED HOSPITAL QINGDAO UNIV (CN)
AFFILIATED HOSPITAL QINGDAO UNIV (CN)
International Classes:
A61K31/365; C07D305/12; A61P3/04; A61P3/06; A61P9/00
Domestic Patent References:
| WO2009059046A1 | 2009-05-07 |
Foreign References:
| CN112159373A | 2021-01-01 | |||
| CN109851592A | 2019-06-07 | |||
| US5260310A | 1993-11-09 |
Other References:
ZHANG RENSHUAI, ZHENGMING SONG, XUETING WANG, JIAO XUE, DONGMING XING : "One-step modiļ¬cation to identify dual-inhibitors targeting both pancreatic triglyceride lipase and Niemann-Pick C1-like 1", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 216, 9 March 2021 (2021-03-09), XP055913555, DOI: 10.1016/j.ejmech.2021.113358
WEST NICHOLAS P. ET AL.: "Inhibitors of an essential mycobacterial cell wall lipase (Rv3802c) as tuberculosis drug leads", EUROPEAN JOURNAL OF PHARMACOLOGY, vol. 47, no. 18, 14 May 2011 (2011-05-14), XP055859949, DOI: 10.1039/c0cc05635a
ORTAR GIORGIO ET AL.: "Tetrahydrolipstatin Analogues as Modulators of Endocannabinoid 2-Arachidonoylglycerol Metabolism", J. MED. CHEM., vol. 51, no. 21, 10 March 2008 (2008-03-10), XP007913016, ISSN: 0022-2623
ALQAHTANI SAEED ET AL.: "Orlistat limits cholesterol intestinal absorption by Niemann-pick C1-like 1 (NPC1L1) inhibition", EUROPEAN JOURNAL OF PHARMACOLOGY, vol. 762, 3 June 2015 (2015-06-03), XP029258906, DOI: 10.1016/j.ejphar.2015.05.060
WEST NICHOLAS P. ET AL.: "Inhibitors of an essential mycobacterial cell wall lipase (Rv3802c) as tuberculosis drug leads", EUROPEAN JOURNAL OF PHARMACOLOGY, vol. 47, no. 18, 14 May 2011 (2011-05-14), XP055859949, DOI: 10.1039/c0cc05635a
ORTAR GIORGIO ET AL.: "Tetrahydrolipstatin Analogues as Modulators of Endocannabinoid 2-Arachidonoylglycerol Metabolism", J. MED. CHEM., vol. 51, no. 21, 10 March 2008 (2008-03-10), XP007913016, ISSN: 0022-2623
ALQAHTANI SAEED ET AL.: "Orlistat limits cholesterol intestinal absorption by Niemann-pick C1-like 1 (NPC1L1) inhibition", EUROPEAN JOURNAL OF PHARMACOLOGY, vol. 762, 3 June 2015 (2015-06-03), XP029258906, DOI: 10.1016/j.ejphar.2015.05.060
Attorney, Agent or Firm:
SHENYANG PATENT & TRADEMARK AGENCY ACADEMIA SINICA (CN)
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