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US 9,428,542 B2Granted
Lupane triterpenoid derivatives and pharmaceutical use thereof
AssigneesJiangxi Qingfeng Pharmaceutical Inc., Qiaodi Feng, Feng Lu
InventorFeng Lu
Life of this patent
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Abstract
The present invention relates to a lupane triterpenoid derivatives and pharmaceutical use thereof, specifically relates to a lupane triterpenoid derivatives of formula (I)˜(III), a pharmaceutical composition and a combination preparation comprising a lupane triterpenoid derivatives or a pharmaceutically acceptable salt thereof in a therapeutically-effective dose, particularly relates to the use in preparation of a medicament for the treatment of HIV-1/AIDS.
Claims19
A compound of formula (I), or a pharmaceutically acceptable salt thereof,
- wherein:
- R1 is independently H,
- X is independently methylene, or carbonyl;
- L is independently a direct bond, —NR4—, —(CH2)r-,
- Y is independently a direct bond, —NR4—, —NR4CH2—,
- —CH2—, —C(═O)—, —CH(CH3)—, or —C(CH3)2—;
- Ar1is independently substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- when substituted, the substituents are one, two or three groups independently selected from the group consisting of:
- halo, alkyl, alkoxy, haloalkyl, haloalkoxy, amino, aminoalkyl, hydroxyalkyl, thioalkyl, —NHC(O)NH2, —NHC(O)NH(R3), —OH, —NO2, —SH, —CN, —C(O)OH, —R3C(O)OH, HOOC—R3—C(O)—, —C(O)O—R3, —C(O)NH2, —C(O)NH(R3), —C(O)N(R3)2, —(CH2)rCONH2, —(CH2)rCONHR3, and —(CH2)rCON(R3)2;
- Ar2 is independently substituted or unsubstituted heteroaryl;
- when substituted, the substituents are one, two or three groups independently selected from the group consisting of:
- halo, haloalkyl, haloalkoxy, amino, —OH, —NO2, —SH, —(CH2)rS(═O)CH3, —(CH2)rS(═O)2CH3, —CN, —C(O)OH, —C(O)O—R3, —C(O)NH2, —C(O)NH(R3), —C(O)N(R3)2, —(CH2)rCONH2, —(CH2)rCONHR3, —(CH2)rCON(R3)2, aminoalkyl, hydroxyalkyl, alkyl, alkynyl, alkoxy, cycloalkylalkyl, and heterocycloalkylalkyl;
- R3 is independently alkyl, or two R3 groups together with the nitrogen atom to which they are attached, form a 3- to 7-membered heterocycloalkyl ring;
- R4 is independently hydrogen, alkyl, cycloalkylalkyl, heterocycloalkylalkyl, aminoalkyl, hydroxyalkyl, —(CH2)rS(═O)CH3, —(CH2)rS(═O)2CH3, —C(O)O—R3, —C(O)NH2, —C(O)NH(R3), —C(O)N(R3)2, —(CH2)rCONH2, —(CH2)rCONHR3, or —(CH2)rCON(R3)2;
- and
- r is an integer from 1 to 8.
13 more elements
Dependencies are inferred from the claim text.