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Title:
【発明の名称】ファルネシルタンパク質トランスフェラーゼインヒビターとして有用な三環式ケトアミド誘導体
Document Type and Number:
Japanese Patent JP3269636
Kind Code:
B2
Abstract:
Compounds of the following formula useful for inhibiting Ras function and therefore inhibiting or treating the abnormal growth of cells are disclosed: or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof, wherein: R and R2 are halo; R1 and R3 are H and halo, provided that at least one of R1 and R3 is H; X is N, CH or C, when the double bond is present at the C-11 position; R4 is=O, -NHOH, -N=NHR6, -N=NHSO2R6, -N=NHCOR6, -N=NHCONH2, -N=NHCOCONH2, (H, OH), (H, -OR6), (H, -OCOR6), (H, OSO2R6) or -E-(CH2)n1-G-, wherein n1 is 1 to 5, and E and G are O, S or N, and are joined to the same carbon to form a cyclic structure; R5 is H, lower alkyl, or optionally substituted aryl, heteroaryl, aralkyl, heteroaralkyl or heterocycloalkyl-alkyl; R6 is lower alkyl or optionally substituted aryl, heteroaryl, aralkyl, heteroaralkyl or heterocycloalkyl-alkyl; R7, R8 and R9 are independently selected from the group consisting of H, lower alkyl, aryl, and aralkyl; and n is 0-5.

Inventors:
Doll, Ronald Jay.
Lalwani, Tariq
Albarez, Carmen
Application Number:
JP50449999A
Publication Date:
March 25, 2002
Filing Date:
June 15, 1998
Export Citation:
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Assignee:
Schering Corporation
International Classes:
A61K31/4427; A61K31/4545; A61K31/496; A61P35/00; C07D221/16; C07D401/04; (IPC1-7): C07D401/04; A61K31/4545; A61K31/496; A61P35/00; C07D221/16
Other References:
【文献】国際公開96/31478(WO,A1)
Attorney, Agent or Firm:
Shusaku Yamamoto