TW200519095A - Substituted fused-ring pyrimidin-4(3H)-one derivatives - Google Patents

Substituted fused-ring pyrimidin-4(3H)-one derivatives

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Publication number
TW200519095A
TW200519095A TW093126498A TW93126498A TW200519095A TW 200519095 A TW200519095 A TW 200519095A TW 093126498 A TW093126498 A TW 093126498A TW 93126498 A TW93126498 A TW 93126498A TW 200519095 A TW200519095 A TW 200519095A
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TW
Taiwan
Prior art keywords
group
optionally substituted
alkyl group
equiv
arteriosclerosis
Prior art date
Application number
TW093126498A
Other languages
Chinese (zh)
Inventor
Masami Arai
Satoru Kaneko
Satoshi Shibuya
Tsuyoshi Watanabe
Kozo Oda
Original Assignee
Sankyo Co
X Ceptor Therapeutics Inc
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Publication date
Application filed by Sankyo Co, X Ceptor Therapeutics Inc filed Critical Sankyo Co
Publication of TW200519095A publication Critical patent/TW200519095A/en

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Abstract

The present invention provides a compound of the following formula (I) or the pharmaceutical acceptable salt or ester thereof: [wherein, A: phenyl group,heteroaryl group; R1:R1a [R1a: substituted alkyl group, optionally substituted cycloalkyl group, optionally substituted alkenyl group, optionally substituted aryl group, optionally substituted heterocyclic group], -Z1b-R1b [R1b:substituted alkyl group, optionally substituted cycloalkyl group, optionally substituted alkenyl group, optionally substituted aryl group,optionally substituted heterocyclic group,; Z1b: -NH-, -O-, -S-, -SO-, -SO2-, -CO-, -COO-, -OCO-, -CONH-, -NHCO-], -Z1c-R1c[R1c:the same as defined in R1b, alkyl group; Z1c:-C &equiv C-, -OCH2CO-, -OCOCH2O-, -OCH2CONH-, -OCH2CONMe-], -N(R1b)(R1c), -OCON(Me)2, -C &equiv CH, -C &equiv C-COMe; R2 R3: H, optionally substituted alkyl group, OH, alkoxy group, NH 2,optionally substituted amino group, nitoro group, halogen, alkylenedioxy group ;R4,R5 H, optionally substituted alkyl group, OH, alkoxy group, NH 2, SH, alkylthio group, COOH, alkoxycarbonyl group, CN, halogen;X:OH, alkoxy group; Y: optionally substituted alkyl group, optionally substituted cycloalkyl group, optionally substituted aryl group, optionally substituted arylalkyl group, optionally substituted heterocyclic group, optionally substituted heterocycloalkyl group: provided that, when Y: specific group, and A: phenyl group, then R4, R5:H; -C(CF3)2(X):-C(CF3)2(OH) which is substituted on 3 or 4 position of the phenyl group bond with]. These compounds have the exellent binding activity to LXR, and are useful as medecement, especially for treating and/or preventing arteriosclerosis, athroma arteriosclerosis, the arteriosclerosis caused by diabetes, hyperlipemia,lipid concerning diseases, inflammatory disease, or diabetes, in warm blood animals(especially human).
TW093126498A 2003-09-05 2004-09-02 Substituted fused-ring pyrimidin-4(3H)-one derivatives TW200519095A (en)

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JP2003314817A JP2006193426A (en) 2003-09-05 2003-09-05 Substituted condensed-ring pyrimidin-4(3h)-one compound

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