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Title:
DACOS TYPE NNRTIS AMINO ACID ESTER DERIVATIVE, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION, AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/170051
Kind Code:
A1
Abstract:
Disclosed is a DACOs-type NNRTIs amino acid ester derivative, a preparation method thereof, a pharmaceutical composition, and an application thereof. The structure of the DACOs-type NNRTIs amino acid ester derivative of the present invention is represented by formula (I), in which R1 is H, a C1-C6 branched or linear alkyl, or C3-C6 cycloalkyl, n is an integer between 0-8, R2 is H, a C1-C12 linear or branched alkyl, C3-C6 cycloalkyl, a C1-C12 linear or branched alkyl, -NH2, a C1-C12 linear or branched alkyl, -OH, NH2C(=O)-, a C1-C12 linear or branched alkoxy, a C1-C12 linear or branched alkylthio, a C6-C20 aryl, a C2-C10 heteroaryl, a C6-C20 aryl substituted by one or more R2a, or a C2-C10 heteroaryl substituted by one or more R2b, and R3 is H, or R2, R3 and a structural fragment linked thereto together to form a C2-C6 heterocycloalkyl group. The DACOs-type NNRTIs amino acid ester derivatives of the present invention can be used as HIV-1 inhibitors and for the preparation of a drug for treating and/or preventing immunodeficiency viruses.

Inventors:
HE YANPING (CN)
ZHANG HONGBIN (CN)
ZHENG YONGTANG (CN)
ZHANG YUFANG (CN)
TANG CHENGRUN (CN)
DING WEI (CN)
YANG LIUMENG (CN)
LI YIMING (CN)
Application Number:
PCT/CN2019/076842
Publication Date:
September 12, 2019
Filing Date:
March 04, 2019
Export Citation:
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Assignee:
UNIV YUNNAN (CN)
KUNMING INST ZOOLOGY CAS (CN)
International Classes:
A61K31/513; C07D239/56; A61P31/18; C07D403/12
Foreign References:
CN106866548A2017-06-20
CN102558072A2012-07-11
Other References:
HE, YANPING ET AL.: "Synthesis and Biological Evaluation of Novel Dihydro-aryl/Alkylsulfanyl- Cyclohexylmethyl-Oxopyrimidines (S-DACOs) as High Active Anti-HIV Agents", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 21, no. 2, 31 December 2011 (2011-12-31), pages 694 - 697, XP027593537, ISSN: 0960-894X, doi:10.1016/j.bmcl.2010.12.003
Attorney, Agent or Firm:
SHANGHAI BESHINING LAW OFFICE (CN)
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