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US 2013/0172349 A1Published application
Inhibitors of phosphatidylinositol 3-kinase
AssigneeNovartis AG
InventorsIan BRUCE, Bernard CUENOUD, Thomas Hugo KELLER, Gaynor Elizabeth WOODWARD, Nicola PRESS, Darren Mark LE GRAND, Cathy RITCHIE, Barbara VALADE, Judy Fox HAYLER, Emma BUDD
Life of this patent
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Abstract
Compounds of formula I in free or salt form, wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
Claims10
A compound of formula I
- in free or salt form, wherein
- R1 is —CO—NRxRy, where Rx and Ry together with the nitrogen to which they are attached form a substituted or unsubstituted 5- to 12-membered N-heterocyclic ring optionally including one or more ring hetero atoms selected from the group consisting of oxygen, nitrogen and sulphur;
- wherein the optional substituent is selected from hydroxy, —SO2—CH3 or aminocarbonyl;
- R2 is C1-C3-alkyl;
- Y is carbon;
- and
- R3 and R4 are each independently hydrogen, halo, hydroxy, cyano, amino, carboxy, C1-C8-alkylsulfanyl, C1-C8-alkylsulfinyl, C1-C8-alkylsulfonyl, —SO2NH2, C1-C8-alkyl, C1-C8-haloalkyl, amino-C1-C8-alkyl, amino-C1-C8-alkoxy, C1-C8-alkylaminocarbonyl, di(C1-C8-alkyl)aminocarbonyl, di(C1-C8-alkyl)amino-C1-C8-alkyl, di(C1-C8-alkyl)amino-C1-C8-alkoxy, C1-C8-acylamino, aminocarbonyl, C1-C8-alkoxycarbonyl, carboxy-C1-C8-alkyl, carboxy-C1-C8-alkoxy, a C3-C15-carbocycle, a 5- or 6-membered heterocyclic ring having one or more ring hetero atoms selected from the group consisting of oxygen, nitrogen and sulphur, C1-C8-alkylamino or di(C1-C8-alkyl)amino each being optionally substituted by amino, hydroxy, di(C1-C8-alkyl)amino or a 5- or 6-membered heterocyclic ring having one or more ring hetero atoms selected from the group consisting of oxygen, nitrogen and sulphur, or C1-C8-alkoxy optionally substituted by a 5- or 6-membered heterocyclic ring having one or more ring hetero atoms selected from the group consisting of oxygen, nitrogen and sulphur.
4 more elements
A compound of formula XXI
- where R1, Y, Ra and Rb are as shown in the following table:
- R1
- Y
- Ra
- Rb
- C
- H
- H
- C
- Cl
- H
- C
- H
- C
- H
- C
- H
- C
- H
- C
- Cl
- H
- C
- Cl
- H
- C
- Cl
- H
- C
- H
- C
- H
- C
- H
- C
- H
- C
- H
- C
- H
- C
- H
- H
- C
- H
- H
- C
- H
- H
- C
- —CH3
- —CH3
- C
- —CH3
- —CH3
- C
- H
- H
- C
- H
- H
- C
- H
- H
- C
- H
- H
- C
- —CH3
- —CH3
- C
- —CH3
- —CH3
- C
- Cl
- H
- C
- Cl
- H
- C
- Cl
- H
- C
- Cl
- H
- C
- Cl
- H
85 more elements
Dependencies are inferred from the claim text.