AKT-PROTEIN KINASE INHIBITOR HYDROXYLATED AND METHOXYLATED CYCLOPENTA [D] PYRIMIDINE

PROBLEM TO BE SOLVED: To provide a novel compound that inhibits AKT protein kinase.SOLUTION: Provided is a compound, including its resolved enantiomer, resolved diastereomer, solvate and pharmaceutically acceptable salt thereof, that comprises the formula I. Also provided is a method of using the co...

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Hauptverfasser: SCHLACHTER STEPHEN T, XIAO DENGMING, SAFINA BRIAN, BENCSIK JOSEF R, LIANG JUN, BANKA ANNA L, BLAKE JAMES F, MITCHELL IAN S, CHABOT CHRISTINE, ZHANG BIRONG, DO STEVEN, SPENCER KEITH LEE, RUI XU, WALLACE ELI W, KALLEN NICHOLAS C
Format: Patent
Sprache:eng ; jpn
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Zusammenfassung:PROBLEM TO BE SOLVED: To provide a novel compound that inhibits AKT protein kinase.SOLUTION: Provided is a compound, including its resolved enantiomer, resolved diastereomer, solvate and pharmaceutically acceptable salt thereof, that comprises the formula I. Also provided is a method of using the compound as AKT protein kinase inhibitor for the treatment of hyperproliferative diseases such as cancer. In one aspect, a method of inhibiting the production of AKT protein kinase in mammals is provided and the method includes a step of administering a compound of the formula I or its enantiomer, solvate, metabolite or pharmaceutically acceptable salt thereof, or prodrug, in an effective amount for inhibiting the production of AKT protein kinase to the mammals. 【課題】AKTプロテインキナーゼを阻害する新規化合物を提供すること。【解決手段】本発明は、式Iを含む、分割された鏡像異性体、分割されたジアステレオマー、溶媒和物および薬学的に許容されるその塩を含む化合物を提供する。AKTプロテインキナーゼ阻害剤として、癌等の過剰増殖性疾患の治療のためにこの発明の化合物を使用する方法も提供される。一つの態様において、本発明は、哺乳動物におけるAKTプロテインキナーゼの産生を阻害する方法であって、式Iの化合物、または鏡像異性体、溶媒和物、代謝産物、または薬学的に許容されるその塩もしくはプロドラッグを、AKTプロテインキナーゼの産生を阻害するために有効な量でこの哺乳動物に投与するステップを含む方法を提供する。【選択図】なし