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US 2010/0137584 A1Published application
Fused heteroaryl derivatives
AssigneesAstellas Pharma Inc., Ludwig Institute for Cancer Research, Imperial Cancer Research Technology, Ltd.
InventorsMasahiko HAYAKAWA, Hiroyuki Kaizawa, Hiroyuki Moritomo, Ken-Ichi Kawaguchi, Tomonobu Koizumi, Mayumi Yamano, Koyo Matsuda, Minoru Okada, Mitsuaki Ohta
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Abstract
The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.
Claims5
1-21. (canceled)
A fused heteroaryl compound of the formula:
- wherein:
- R1 is independently selected from C1-C10 alkyl, C6-C14 aryl, or 5- or 6-membered monocyclic heteroaryl;
- where C1-C10 alkyl, C6-C14 aryl, and 5- or 6-membered monocyclic heteroaryl are optionally and independently substituted with one or more substituents selected from C1-C10 alkyl, C1-C10 alkenyl, C1-C10 alkynyl, halogen, halogenated C1-C10 alkyl, (C1-C10 alkylene)-OR, NO2, CN, ═O, OR, O-(halogenated C1-C10 alkyl), O—(C1-C10 alkylene)-NRR′, O—(C1-C10 alkylene)-OR, O—(C1-C10 alkylene)-(C6-C14 aryl), SR, SO2—(C1-C10 alkyl), SO—(C1-C10 alkyl), COOR, COO—(C1-C10 alkylene)-(C6-C14 aryl), SO—(C1-C10 alkyl), COR, CO—(C6-C14 aryl), C6-C14 aryl, CONRR′, SO2NRR′, NRR′, NR″—(C1-C10 alkylene)-NRR′, NR′—(C1-C10 alkylene)-OR, NR—(C1-C10 alkylene)-(C6-C14aryl), NRCO—(C1-C10 alkyl), NRSO2—(C1-C10 alkyl), C3-C8 cycloalkyl, and C3-C8 cycloalkenyl;
- R4b is C6-C14 aryl, 5- or 6-membered monocyclic heteroaryl, or bicyclic heteroaryl;
- where C6-C14 aryl, 5- or 6-membered monocyclic heteroaryl, and bicyclic heteroaryl are optionally and independently substituted with one or more substituents selected from C1-C10 alkyl, C1-C10 alkenyl, C1-C10 alkynyl, halogen, halogenated C1-C10 alkyl, (C1-C10 alkylene)-OR, NO2, CN, ═O, OR, O-(halogenated C1-C10 alkyl), O—(C1-C10 alkylene)-NRR′, O—(C1-C10 alkylene)-OR, O—(C1-C10 alkylene)-(C6-C14 aryl), SR, SO2—(C1-C10 alkyl), SO—(C1-C10 alkyl), COOR, COO—(C1-C10 alkylene)-(C6-C14 aryl), SO—(C1-C10 alkyl), COR, CO—(C6-C14 aryl), C6-C14 aryl, CONRR′, SO2NRR′, NRR′, NR″—(C1-C10 alkylene)-NRR′, NR′—(C1-C10 alkylene)-OR, NR—(C1-C10 alkylene)-(C6-C14 aryl), NRCO—(C1-C10 alkyl), NRSO2—(C1-C10 alkyl), C3-C8 cycloalkyl, and C3-C8 cycloalkenyl;
- R, R′, and R″ are independently selected from H and C1-C10 alkyl;
- and
- n is 1 or 2.
5 more elements
Dependencies are inferred from the claim text.