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
Authority
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
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
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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Publication number Priority date Publication date Assignee Title
GB0412769D0 (en) 2004-06-08 2004-07-07 Novartis Ag Organic compounds
US20080255111A1 (en) * 2004-07-02 2008-10-16 Sankyo Company Limited Tissue Factor Production Inhibitor
AR056155A1 (en) * 2005-10-26 2007-09-19 Bristol Myers Squibb Co ANTAGONISTS OF NON-BASIC MELANINE CONCENTRATION HORMONE RECEIVER 1
AU2007323836B2 (en) * 2006-11-13 2013-04-18 Icos Corporation Thienopyrimidinones for treatment of inflammatory disorders and cancers
CN101595096B (en) * 2006-11-30 2012-06-27 兴和株式会社 Substituted carbinol compound
US20080255161A1 (en) * 2007-04-11 2008-10-16 Dmitry Koltun 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS
CN101531638B (en) * 2008-03-13 2011-12-28 中国科学院广州生物医药与健康研究院 Compound used as a regulator of estrogen-related receptor and applications thereof
PE20091928A1 (en) 2008-05-29 2009-12-31 Bristol Myers Squibb Co HAVE HYDROXYSUSTITUTED PYRIMIDINES AS NON-BASIC MELANIN-CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
US8153634B2 (en) 2008-05-29 2012-04-10 Kowa Company, Ltd. Carbinol derivatives having cyclic linker
CA2811145A1 (en) 2010-09-07 2012-03-15 Snu R&Db Foundation Sesterterpene compound and use thereof
HUE040231T2 (en) 2012-03-02 2019-02-28 Ralexar Therapeutics Inc Liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions
ES2804304T3 (en) 2013-09-04 2021-02-05 Ellora Therapeutics Inc Hepatic X receptor (LXR) modulators
CA2923178A1 (en) 2013-09-04 2015-03-12 Alexar Therapeutics, Inc. Liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions
AU2015204572B2 (en) 2014-01-10 2020-07-30 Inspirna, Inc. LXR agonists and uses thereof
CA3008171A1 (en) 2015-12-22 2017-06-29 SHY Therapeutics LLC Compounds for the treatment of cancer and inflammatory disease
EP3402477A4 (en) 2016-01-11 2019-08-21 The Rockefeller University Methods for the treatment of myeloid derived suppressor cells related disorders
IL310023A (en) 2017-06-21 2024-03-01 SHY Therapeutics LLC Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
WO2019104062A1 (en) 2017-11-21 2019-05-31 Rgenix, Inc. Polymorphs and uses thereof
US11174220B2 (en) 2019-12-13 2021-11-16 Inspirna, Inc. Metal salts and uses thereof
JPWO2021157596A1 (en) * 2020-02-07 2021-08-12

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6316503B1 (en) * 1999-03-15 2001-11-13 Tularik Inc. LXR modulators
EP1343505A1 (en) * 2000-12-11 2003-09-17 Tularik Inc. Cxcr3 antagonists
AU2002363429B2 (en) * 2001-11-07 2008-05-08 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2003106435A1 (en) * 2002-06-18 2003-12-24 Sankyo Company, Limited Fused-ring pyrimidin-4(3h)-one derivatives, processes for the preparation and uses thereof

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