Cyclic ureas
AssigneeSironax Ltd.
InventorsZhiyuan Zhang, Yaning Su, Jianguang Han, Hanying Ruan, Ying Li, Guozheng Wang, Wendong Liu, Chong Zhang, Leiming Liang
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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, hydrates 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
A compound of structure:
- wherein:
- R1 is substituted or unsubstituted phenyl or substituted or unsubstituted 2-, 3- or 4-pyridine;
- R2 is dihydro-pyrazole or isoxazolidine;
- and
- R3 and R4 are linked to form a 4-6 membered N-containing, heterocycloalkyl ring, wherein the 4-6 membered N-containing, heterocycloalkyl ring is fused to phenyl or wherein the 4-6 membered N-containing, heterocycloalkyl ring is linked to R5 through an optional linker selected from —CH2—, —O— and ═CH—, wherein R5 is substituted or unsubstituted C3-C9 cycloalkyl with 0-3 heteroatoms, C3-C9 cycloalkenyl with 0-3 heteroatoms, or C3-C9 cycloalkynyl with 0-3 heteroatoms, or substituted or unsubstituted C5-C14 aryl with 0-3 heteroatoms;
- or a pharmaceutically acceptable salt, or a hydrate of the compound.
A compound comprising a structure of any one of the following structures:
- or a pharmaceutically acceptable salt, or a hydrate of the compound.
A compound of structure:
- or a pharmaceutically acceptable salt, or a hydrate thereof, wherein:
- R1 is substituted or unsubstituted phenyl or substituted or unsubstituted 2-, 3- or 4-pyridyl, wherein the substitute(s) of R1 are selected from halogen and CN;
- R2 is dihydro-pyrazole or isoxazolidine;
- and
- R3 and R4, together with the nitrogen atom to which they are bound, are linked to form a 4-6 membered N-containing, heterocycloalkyl ring,
- wherein the formed 4-6 membered N-containing, heterocycloalkyl ring is fused to phenyl, or wherein the 4-6 membered N-containing, heterocycloalkyl ring is linked through a linker to R5;
- wherein the linker is —CH2—, —O—, or ═CH—;
- and
- R5 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 heteroatoms cyclohexyl, cyclopentyl, wherein the heteroatoms are selected from N, O, and S;
- or
- (e) substituted or unsubstituted 0-3 heteroatoms cyclopentene or cyclopentadiene,
- wherein the heteroatoms are independently selected from N, O, and S;
- and
- wherein the substituent(s) of R5 are selected from halogen, —R′, —OR′, ═O, —NR′R″, —CO2R′, —CONR′R″, —NR″C(O)R′, and —CN, wherein R′ and R″ are each independently selected from hydrogen, unsubstituted (C1-C8)alkyl, and unsubstituted (C1-C8) heteroalkyl, wherein the (C1-C8) heteroalkyl has at least one heteroatom selected from N, O, and S.
Dependencies are inferred from the claim text.