1154870-59-3Relevant articles and documents
Potent MCH-1 receptor antagonists from cis-1,4-diaminocyclohexane-derived indane analogs
Qian, Yimin,Conde-Knape, Karin,Erickson, Shawn D.,Falcioni, Fiorenza,Gillespie, Paul,Hakimi, Irina,Mennona, Francis,Ren, Yonglin,Salari, Hamid,So, Sung-Sau,Tilley, Jefferson W.
, p. 4216 - 4220 (2013)
Benzimidazole and indane are the two key fragments in our potent and selective MCH-1 receptor (MCHR1) antagonists. To identify novel linkers connecting the two fragments, we investigated diamino-cycloalkane-derived analogs and discovered highly potent antagonists with cis-1,4-diaminocyclohexane as a unique spacer in this chemical class. Structural overlay suggested that cis-1-substituted-4-aminocyclohexane functions as a bioisostere of 4-substituted-piperidine and that the active conformation adopts a U-shaped orientation.
KRAS G12C Inhibitor compound and application thereof
-
Paragraph 0141-0145, (2021/05/12)
The invention provides a KRAS G12C inhibitor compound and an application thereof, and particularly provides a compound as shown in a formula (I), and an optical isomer, a hydrate, a solvate or pharmaceutically acceptable salt thereof. The compound can be used as a KRAS G12C inhibitor and is used for treating diseases related to the activity or expression quantity of KRAS G12C.
Intermediate for preparing bictegravir and preparation method thereof
-
Paragraph 0102; 0103; 0104; 0105, (2019/01/08)
The invention relates to the technical field of a drug, and concretely relates to an intermediate for preparing bictegravir and a preparation method thereof. The present invention provides two novel types of compounds and three routes for preparation of a compound (VI). Through substrate induction, chiral catalysis or synergistic effect of substrate induction and chiral catalysis, the stereoselectivity of a Diels-Alder reaction can be greatly improved, and a high chiral purity of a common intermediate (III) can be obtained; cut-out of N-O bond and reduction the double bond use catalytic hydrogenation, which can be environmentally friendly; the reaction conditions are mild, the yield is higher than the existing preparation method, the method is economic and effective, and is adapted to large-scale industrial production.