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US 6,617,346 B1Granted
Cis-imidazolines
AssigneeHoffmann-La Roche Inc.
InventorsNorman Kong, Emily Aijun Liu, Binh Thanh Vu
Life of this patent
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Abstract
The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity
Claims11
A compound of formula I
- and the pharmaceutically acceptable salts and esters thereof, wherein
- Z1, Z2 and Z3 are each independently selected from lower alkoxy, —CH2OCH3, and —CH2OCH2CH3,
- or one of Z1, Z2 or Z3 is —H and the other two are each independently selected from lower alkyl, lower alkoxy, —Cl, —Br, —F, —CF3, —CH2OCH3, —CH2OCH2CH3, —OCH2CH2R1, —CH2-morpholino, —OR2, —CH2R2, —OCH2CF3, —OCH(CH3)CH2OH and —COOQ,
- wherein Q is selected from —H and lower alkyl,
- or one of Z1, Z2 or Z3 is —H and the other two taken together with the two carbon atoms and the bonds between them from the benzene ring to which they are substituted form a ring selected from 5- and 6-membered unsaturated rings, and 5- and 6-membered saturated rings that contain at least one hetero atom selected from S, N, and O,
- wherein R1 is selected from —F, —OCH3, —N(CH3)2, and unsaturated 5-membered rings containing at least one hetero atom wherein the hetero atom is selected from S, N and O,
- wherein R2 is a 3- to 6-membered saturated ring, and
- Y1 and Y2 are each independently selected from —Cl, —Br, —NO2, —C≡N and —C≡CH.
5 more elements
A compound of formula II
- and the pharmaceutically acceptable salts and esters thereof, wherein
- Z4 is selected from C1-C2 alkyl, lower alkoxy, —OH, —SCH3, —CF3, —NO2, —COOQ2, —N(CH3)2, —OCH2-phenyl, —Cl, —Br, —F, —OCH2C═OOQ1, saturated 5- and 6-membered rings containing at least one hetero atom wherein the hetero atom is selected from S, N and O,
- wherein Q1 is selected from —H, —NH2, and lower alkyl,
- wherein Q2 is selected from —H and lower alkyl,
- Y1 and Y2 are independently selected from —Cl, —Br, —NO2, —C≡N and —C≡CH,
- with the proviso that where Y1 and Y2 are both —Cl, Z4 is not —Cl, and
- with the proviso that where Y1 and Y2 are both —NO2, Z4 is not —NO2, and
- with the proviso that where Y1 and Y2 are both —CN, Z4 is not —CN.
5 more elements
Dependencies are inferred from the claim text.