WO2008133288A1 - 三環性アリール化合物 - Google Patents

三環性アリール化合物 Download PDF

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Publication number
WO2008133288A1
WO2008133288A1 PCT/JP2008/057886 JP2008057886W WO2008133288A1 WO 2008133288 A1 WO2008133288 A1 WO 2008133288A1 JP 2008057886 W JP2008057886 W JP 2008057886W WO 2008133288 A1 WO2008133288 A1 WO 2008133288A1
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Prior art keywords
halogeno
hydrogen
same
carboxy
different
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Ceased
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PCT/JP2008/057886
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English (en)
French (fr)
Inventor
Kazuyuki Sugita
Masao Itoh
Masanori Ichikawa
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Daiichi Sankyo Co Ltd
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Daiichi Sankyo Co Ltd
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Priority to JP2009511895A priority Critical patent/JPWO2008133288A1/ja
Publication of WO2008133288A1 publication Critical patent/WO2008133288A1/ja
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
    • C07C69/734—Ethers
    • C07C69/736—Ethers the hydroxy group of the ester being etherified with a hydroxy compound having the hydroxy group bound to a carbon atom of a six-membered aromatic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/16—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D313/00—Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
    • C07D313/02—Seven-membered rings
    • C07D313/06—Seven-membered rings condensed with carbocyclic rings or ring systems
    • C07D313/10—Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D337/00—Heterocyclic compounds containing rings of more than six members having one sulfur atom as the only ring hetero atom
    • C07D337/02—Seven-membered rings
    • C07D337/06—Seven-membered rings condensed with carbocyclic rings or ring systems
    • C07D337/10—Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

　本発明は、下記の一般式（１） （式中、Ｒ１はハロゲノ基、Ｃ１～Ｃ６アルコキシ基等の置換基を有していてもよいフェニル基等；Ｒ２ａ及びＲ２ｂは、同一又は異なって、水素原子、ハロゲノ基等；環Ａはベンゼン環又は芳香族複素環；Ｒ３ａ及びＲ３ｂは、同一又は異なって、水素原子、ハロゲノ基等；Ｘは、ＣＨ２、Ｏ、Ｓ等；Ｒ４ａは、水素原子等；Ｒ４ｂは、カルボキシ基、カルボキシＣ１～Ｃ６アルキル基等を示す。）で表される化合物又はその薬理上許容される塩、及びこれらを有効成分として含有するスクアレン合成酵素阻害剤に関する。本発明の化合物は、スクアレン合成酵素阻害作用、コレステロール合成阻害作用を示すので、ヒトを含む哺乳動物のための高コレステロール血症、高トリグリセライド血症、低ＨＤＬ血症等の高脂血症および／または動脈硬化症の予防および／または治療薬等の医薬として有用である。
PCT/JP2008/057886 2007-04-25 2008-04-24 三環性アリール化合物 Ceased WO2008133288A1 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2009511895A JPWO2008133288A1 (ja) 2007-04-25 2008-04-24 三環性アリール化合物

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-115747 2007-04-25
JP2007115747 2007-04-25

Publications (1)

Publication Number Publication Date
WO2008133288A1 true WO2008133288A1 (ja) 2008-11-06

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JP (1) JPWO2008133288A1 (ja)
TW (1) TW200904403A (ja)
WO (1) WO2008133288A1 (ja)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2567959A1 (en) 2011-09-12 2013-03-13 Sanofi 6-(4-Hydroxy-phenyl)-3-styryl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
JP2015508119A (ja) * 2012-02-22 2015-03-16 メルク パテント ゲーエムベーハー ジベンゾシクロヘプタン構造単位を含むポリマー
WO2016157221A1 (en) 2015-03-30 2016-10-06 Jubilant Biosys Limited Tricyclic fused derivatives of 1-(cyclo)alkyl pyridin-2-one useful for the treatment of cancer
WO2017042834A1 (en) 2015-09-09 2017-03-16 Jubilant Biosys Limited Tricyclic fused pyridin-2-one derivatives and their use as brd4 inhibitors

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH1059953A (ja) * 1996-06-20 1998-03-03 Pfizer Inc スクアレンシンセターゼ阻害剤
JPH11228576A (ja) * 1997-12-10 1999-08-24 Japan Tobacco Inc アポトーシス抑制剤
JP2006517921A (ja) * 2003-02-19 2006-08-03 ファイザー・インク 治療に有用なトリアゾール化合物

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH1059953A (ja) * 1996-06-20 1998-03-03 Pfizer Inc スクアレンシンセターゼ阻害剤
JPH11228576A (ja) * 1997-12-10 1999-08-24 Japan Tobacco Inc アポトーシス抑制剤
JP2006517921A (ja) * 2003-02-19 2006-08-03 ファイザー・インク 治療に有用なトリアゾール化合物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
WEITZBERG M. ET AL.: "Syntheses and chemistry of some dibenz(c,e)azepines", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 52, no. 4, 1987, pages 529 - 536, XP002150438 *

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2567959A1 (en) 2011-09-12 2013-03-13 Sanofi 6-(4-Hydroxy-phenyl)-3-styryl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
JP2015508119A (ja) * 2012-02-22 2015-03-16 メルク パテント ゲーエムベーハー ジベンゾシクロヘプタン構造単位を含むポリマー
WO2016157221A1 (en) 2015-03-30 2016-10-06 Jubilant Biosys Limited Tricyclic fused derivatives of 1-(cyclo)alkyl pyridin-2-one useful for the treatment of cancer
US10689390B2 (en) 2015-03-30 2020-06-23 Jubilant Biosys Limited Tricyclic fused derivatives of 1-(cyclo)alkyl pyridin-2-one useful for the treatment of cancer
US11319326B2 (en) 2015-03-30 2022-05-03 Jubilant Biosys Limited Tricyclic fused derivatives of 1-(cyclo)alkyl pyrtdin-2-one useful for the treatment of cancer
WO2017042834A1 (en) 2015-09-09 2017-03-16 Jubilant Biosys Limited Tricyclic fused pyridin-2-one derivatives and their use as brd4 inhibitors
CN108137588A (zh) * 2015-09-09 2018-06-08 朱比兰特生物系统有限公司 三环稠合吡啶-2-酮衍生物及其作为brd4抑制剂的用途
US10689395B2 (en) 2015-09-09 2020-06-23 Jubilant Biosys Limited Tricyclic fused pyridin-2-one derivatives and their use as BRD4 inhibitors
RU2734959C2 (ru) * 2015-09-09 2020-10-26 Джубилант Байосис Лимитед Трициклические конденсированные производные пиридин-2-она и их применение в качестве ингибиторов brd4
CN108137588B (zh) * 2015-09-09 2021-06-18 朱比兰特生物系统有限公司 三环稠合吡啶-2-酮衍生物及其作为brd4抑制剂的用途
US11267820B2 (en) 2015-09-09 2022-03-08 Jubilant Biosys Limited Tricyclic fused pyridin-2-one derivatives and their use as BRD4 inhibitors

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JPWO2008133288A1 (ja) 2010-07-29

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