Field
     Health care, Medicine

Keywords
     Dihydronaphthalene Compounds, Proteasomal inhibitor

Advantages
     Proteasomal inhibitors are generally used as therapeutic agents for targeted diseases such as
     multiple myeloma and other cancers. One such example is Onyx Pharmaceuticals, Inc. 
    (Nasdaq: ONXX)'s "carfilzomib" currently underdevelopment. The present patent application
    concerns a novel compound with activity of proteasome inhibitor.

Abstract
Disclosed is a compound represented by the formula (I) below as a dihydronaphthalene compound having a chemical structure which is excellent in production efficiency when compared with lasofoxifene and nafoxidine. This compound is useful as a proteasome inhibitor and/or an antitumor agent. (In the formula, two -(CH2)l-N(R1)(R2) groups represent a same substituent; R1 and R2 each represents a hydrogen atom, or a same or different alkyl group; or alternatively, R1 and R2 may combine together to form a monocyclic heterocyclic ring with a nitrogen atom having them or additionally together with one or more atoms selected from an oxygen atom, a sulfur atom and a nitrogen atom; R3, R4 and R5 each represents one or more substituents selected from a hydrogen atom, an alkyl group, an acyl group, an alicyclic group, an aromatic group, a halogen atom, an acyloxy group, a cyano group and a nitro group; l represents an integer of 2-5; n represents an integer of 1-4; m represents an integer of 1-5; and q represents an integer of 1-3.)

Inventor
     Prof. Isamu Shiina　(Tokyo University of Science)


Patent Publication No
     (APPLICATION NUMBER, FILING DATE)
     WO2008066384（Sep. 11, 2008）, EP08830489.4（Sep. 11, 2008）, US12/675331（Sep. 11, 2008）,
     JP2009-532207 (Sep. 11, 2008）
     (PUBLICATION NUMBER, PUBLICATION DATE)
     WO2009/035020（Mar. 19, 2009）, EP2192108 (Jun. 2, 2010), US2010/02249400 (Sep. 30, 2010),
     JP,2009/035020,A1 (Dec. 24, 2010)

Publication
(1) Cncer Sci. March 2008, vol99,no3,608-614 (2) Biochemical Pharacology 75(2008)1014-1026  (3)Bioorg. Med. Chem. Lett 17 (2007) 2421-2424  (4)Bioorg. Med. Chem.15(2007)7599-7617

Internal file number
     LSP:35
     G2008-009, T2009-070, (T2007-053)

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