Condensed heteroaryl derivatives

A technology of condensing heteroaryl and derivatives, applied in the field of condensing heteroaryl derivatives, can solve problems such as no explanation, no disclosure of PI3K inhibitory effect and anticancer effect, etc.
CN1426398AInactive Publication Date: 2003-06-25ASTELLAS PHARMA INC +2
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
ASTELLAS PHARMA INC
Publication Date
2003-06-25
Estimated Expiration
Not applicable · inactive patent
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Abstract

Medicinal compositions which are useful as phosphatidylinositol 3-kinase (PI3K) inhibitors and anticancer agents; and novel bicyclic or tricyclic condensed heteroaryl derivatives or salts thereof having favorable effects of inhibiting PI3K and suppressing the proliferation of cancer cells.
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Description

technical field

[0001] The present invention relates to fused heteroaryl derivatives useful as pharmaceuticals, especially phosphatidylinositol 3-kinase (PI3K) inhibitors and anticancer agents. Background technique

[0002] Phosphatidylinositol (hereinafter referred to as "PI") is one of cell membrane phospholipids, which is known to play a role in intracellular information transmission. In particular, it is well understood that PI(4,5) diphosphate (PI(4,5)P2) is broken down by phospholipase C into diacylglycerol and inositol (1,4,5) triphosphate, causing Activation of protein kinase C and intracellular calcium mobilization [MJ Berridge et al., Nature, 312, 315, (1984), Y Nishizuka, Science, 225, 1365 (1984)].

[0003] On the other hand, in the second half of the 1980s, PI3K was identified as an enzyme that phosphorylates the 3-position of the PI-inositol ring [D Whitman et al., Nature, 332, 664 (1988)].

[0004] PI3K was once thought to be a single enzyme when it was firs...

Claims

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