Necrosis Inhibitors
AssigneeNational Institute of Biological Sciences, Beijing
InventorsZhiyuan Zhang, Xiaodong Wang, Yaning Su, Hanying Ruan, Yan Ren
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Abstract
The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
Claims20
An amide compound that is an inhibitor of cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), of formula:
- wherein:
- R1 is
- (a) substituted or unsubstituted phenyl;
- (b) substituted or unsubstituted 2-, 3- or 4-pyridine;
- (c) substituted or unsubstituted naphthyl or 3-azanaphthyl;
- (d) substituted or unsubstituted 0-3 heteroatom cyclohexyl, cyclopentyl;
- or
- (e) substituted or unsubstituted 0-3 heteroatom cyclopentene or cyclopentadiene;
- R2 is substituted or unsubstituted aziridine, azetidine, pyrrolidine, piperidine, oxazridine, oxazetidine, oxazolidine, oxazinane, thiaziridine, thiazetidine, thiazolidine, thiazinane, diaziridine, diazetidine, diazolidine (pyrazolidine), diazinane;
- or
- R2 is substituted or unsubstituted pyrrole, dihydropyrrole, pyridine, dihydropyridine, tetrahydropyridine, azole, pyrimidine, oxazine, thiazine, triazine, ozadiazine, thiadiazine;
- and
- R3 is substituted or unsubstituted, 0-3 heteroatom C1-C9 alkyl, alkenyl, or alkynyl;
- or
- a corresponding sulfonamide of the amide compound, or
- a pharmaceutically acceptable salt, hydride or stereoisomer the compound or corresponding sulfonamide.
Dependencies are inferred from the claim text.