IP Library Granted Patent US 11,472,815
Granted Patent B2
US 11,472,815 · App. 17/043,646 · Granted Oct 18, 2022

1,4-diphenyl-1H-imidazole and 2,4-diphenylthiazole derivatives and preparation method therefor and use thereof

Inventors: Kui Cheng (Guangzhou, CN); Shuwen Liu (Guangzhou, CN); Gengzhen Zhu (Guangzhou, CN)
Assignee: SOUTHERN MEDICAL UNIVERSITY
C07D495/04C07D233/64C07D277/28
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Quick Facts
Patent No.
US 11,472,815
App. No.
17/043,646
Granted
Oct 18, 2022
Kind
B2
Abstract

Provided are 1,4-diphenyl-1H-imidazole and 2,4-diphenylthiazole derivatives having a structure represented by Formula I, a preparation method therefor and uses thereof: wherein R 1 is any one of H, OH, and OCH 3 , R 2 is any one of H, NO 2 , CH 3 , CF 3 , SO 2 CH 3 , COOCH 3 , or CONHCH 3 , R 3 is any one of H, NO 2 , OCH 3 , or CF 3 , R 4 is selected from H, CF 3 , or Cl, R 5 is any one of H, Cl, CF 3 , or NHCH 3 , and R 6 is any one of OCF 3 , CF 3 , or CN; V is either C or N, W is either CH or N, X is a C atom, Y is either CH or N, and Z is either CH or S. This compound can be used in preparation of anti-inflammatory adjuvants, TLR1 or TLR2 agonists, and anti-tumor agents and for regulating the activity activation level of TLR1 and TLR2 alkaline phosphatases in vitro and in vivo.

Claims (18)

1. A compound, or a pharmaceutically acceptable salt thereof, wherein the compound has a structural formula below: Compound 23

2. A preparation method of the compound according to claim 1 , comprising the following steps:

1) allowing compound A1

to react as catalyzed by inethyllithium to obtain compound A2

allowing the compound A2

to react in a presence of tetrabutylammonium tribromide to obtain compound A3

2) allowing compound B1

to react in methylamine to give an amino-substituted compound B2

reducing the amino-substituted compound B2 to obtain compound B3

or aminomethylating compound B5

to obtain the compound B 3 ;

3) reacting compound B3 with triethyl orthofomiate to form a ring to obtain compound B4

4) reacting the compound 134 with the compound A3 to obtain compound B6

5) refluxing the compound B 6 under acidic conditions to obtain the compound according to claim 1 ;

wherein R 1 , R 2 and R 6 in the compounds A3, B1, B2, B3, B4 and B5 for preparing the compound according to claim 1 are as follows:

R 1 ═OH, R 6 ═CF 3 , R 2 ═SO 2 CH 3 .

3. A pharmaceutical composition, comprising the compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or an excipient.

4. A method for regulating an activity activation level of URI and TLR2 alkaline phosphatases in vivo, comprising administering the compound according to claim 1 to a subject.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 9, 2020
From: CHENG, KUI; LIU, SHUWEN; ZHU, GENGZHEN
To: SOUTHERN MEDICAL UNIVERSITY
Reel/Frame 054045/0342 →
Continuity (1)
Related Publication 20210017189A1 · Jan 21, 2021