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WO2008111604A1 - 新規なベンジル(ヘテロサイクリックメチル)アミン構造を有するピリミジン化合物及びこれを含有する医薬 - Google Patents

新規なベンジル(ヘテロサイクリックメチル)アミン構造を有するピリミジン化合物及びこれを含有する医薬 Download PDF

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Publication number
WO2008111604A1
WO2008111604A1 PCT/JP2008/054459 JP2008054459W WO2008111604A1 WO 2008111604 A1 WO2008111604 A1 WO 2008111604A1 JP 2008054459 W JP2008054459 W JP 2008054459W WO 2008111604 A1 WO2008111604 A1 WO 2008111604A1
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl group
lower alkyl
hydrogen atom
heterocyclicmethyl
benzyl
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/JP2008/054459
Other languages
English (en)
French (fr)
Inventor
Tadaaki Ohgiya
Toru Miura
Ayumu Okuda
Toshiharu Arai
Koichi Yamazaki
Taro Aoki
Katsutoshi Miyosawa
Haruki Shibata
Kimiyuki Shibuya
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Kowa Co Ltd
Original Assignee
Kowa Co Ltd
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 Kowa Co Ltd filed Critical Kowa Co Ltd
Priority to CN2008800158234A priority Critical patent/CN101679363B/zh
Priority to JP2009504064A priority patent/JP5204091B2/ja
Priority to EP08721875A priority patent/EP2138489B9/en
Publication of WO2008111604A1 publication Critical patent/WO2008111604A1/ja
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

 コレステロールエステル転送タンパク(CETP)に対し強い阻害活性を示す下記一般式(I)で表される化合物(R1、R2、R3、R4及びR5は水素原子、ハロゲン原子、低級アルキル基などを示し、R6、はアルキル基、シクロアルキル基などを示し、R7及びR8は水素原子、低級アルキル基、低級シクロアルキル低級アルキル基などを示し、R9は、水素原子、ハロゲン原子、低級アルコキシ基などを示し、R10及びR11は水素原子、低級アルキル基、低級アルコキシ基、ハロ低級アルキル基などを示し、Aは6から10原子で構成される複素環を示す)。
PCT/JP2008/054459 2007-03-13 2008-03-12 新規なベンジル(ヘテロサイクリックメチル)アミン構造を有するピリミジン化合物及びこれを含有する医薬 Ceased WO2008111604A1 (ja)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CN2008800158234A CN101679363B (zh) 2007-03-13 2008-03-12 具有苯甲基(杂环甲基)胺结构的嘧啶化合物及含有其的药物
JP2009504064A JP5204091B2 (ja) 2007-03-13 2008-03-12 新規なベンジル(ヘテロサイクリックメチル)アミン構造を有するピリミジン化合物及びこれを含有する医薬
EP08721875A EP2138489B9 (en) 2007-03-13 2008-03-12 Novel pyrimidine compound having benzyl(heterocyclicmethyl)amine structure and pharmaceutical product containing the same

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US89453407P 2007-03-13 2007-03-13
US60/894,534 2007-03-13

Publications (1)

Publication Number Publication Date
WO2008111604A1 true WO2008111604A1 (ja) 2008-09-18

Family

ID=39759538

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/054459 Ceased WO2008111604A1 (ja) 2007-03-13 2008-03-12 新規なベンジル(ヘテロサイクリックメチル)アミン構造を有するピリミジン化合物及びこれを含有する医薬

Country Status (7)

Country Link
US (2) US7790737B2 (ja)
EP (1) EP2138489B9 (ja)
JP (1) JP5204091B2 (ja)
KR (1) KR20090122278A (ja)
CN (1) CN101679363B (ja)
TW (1) TW200902011A (ja)
WO (1) WO2008111604A1 (ja)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009051827A (ja) * 2007-07-30 2009-03-12 Mitsubishi Tanabe Pharma Corp 医薬組成物
WO2011157827A1 (de) 2010-06-18 2011-12-22 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
US20130190540A1 (en) * 2010-07-22 2013-07-25 Kowa Company, Ltd. Method for preparing optically active 1-bromo-1-[3,5-bis(trifluoromethyl)phenyl]ethane
WO2014017569A1 (ja) * 2012-07-26 2014-01-30 興和株式会社 血中ldlを低下させるための医薬
JP2014525929A (ja) * 2011-08-18 2014-10-02 ドクター レディズ ラボラトリーズ リミテッド コレステリルエステル転送タンパク質(cetp)インヒビターとしての置換複素環式アミン化合物
JP2014527997A (ja) * 2011-09-27 2014-10-23 ドクター レディズ ラボラトリーズ リミテッド アテローム性動脈硬化症の処置のために有用なコレステリルエステル転送タンパク質(cetp)インヒビターとしての5−ベンジルアミノメチル−6−アミノピラゾロ[3,4−b]ピリジン誘導体
JP2015054838A (ja) * 2013-09-12 2015-03-23 興和株式会社 血中ldlコレステロールを低下させる医薬
US10653681B2 (en) 2016-03-16 2020-05-19 Recurium Ip Holdings, Llc Analgesic compounds

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1848430T3 (da) * 2004-12-31 2017-11-06 Dr Reddys Laboratories Ltd Nye benzylamin-derivativer som cetp-inhibitors
US8604055B2 (en) 2004-12-31 2013-12-10 Dr. Reddy's Laboratories Ltd. Substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors
US7750019B2 (en) * 2006-08-11 2010-07-06 Kowa Company, Ltd. Pyrimidine compound having benzyl(pyridylmethyl)amine structure and medicament comprising the same
US7790737B2 (en) * 2007-03-13 2010-09-07 Kowa Company, Ltd. Substituted pyrimidine compounds and their utility as CETP inhibitors
PL2149563T3 (pl) * 2007-04-13 2015-06-30 Kowa Co Nowy związek pirymidynowy mający strukturę dibenzyloaminy i lek zawierający ten związek
EP2332923A4 (en) * 2008-09-12 2012-08-01 Kowa Co PROCESS FOR PREPARING 5- [2- (METHYLTHIO) ETHOXY] PYRIMIDIN-2-AMINE

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WO1997019078A1 (fr) 1995-11-21 1997-05-29 Yamanouchi Pharmaceutical Co., Ltd. DERIVES DE PYRIDO[2,3-d] PYRIMIDINE ET LEURS COMPOSES A USAGE MEDICAL
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WO2007073934A1 (en) * 2005-12-29 2007-07-05 Novartis Ag Pyridinyl amine derivatives as inhibitors of cholesteryl ester transfer protein (cetp)
WO2008018529A1 (en) * 2006-08-11 2008-02-14 Kowa Company, Ltd. Novel pyrimidine compound having benzyl(pyridylmethyl)amine structure and pharmaceutical comprising the compound

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EP1981342B1 (en) 2005-12-28 2016-11-30 Dr. Reddy's Laboratories Ltd. Selective benzylamine derivatives and their utility as cholesterol ester-transfer protein inhibitors
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* Cited by examiner, † Cited by third party
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WO1997019078A1 (fr) 1995-11-21 1997-05-29 Yamanouchi Pharmaceutical Co., Ltd. DERIVES DE PYRIDO[2,3-d] PYRIMIDINE ET LEURS COMPOSES A USAGE MEDICAL
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WO2006056854A1 (en) 2004-11-23 2006-06-01 Pfizer Products Inc. Dibenzyl amine compounds and derivatives
WO2006073973A2 (en) 2004-12-31 2006-07-13 Reddy Us Therapeutics, Inc. Novel benzylamine derivatives as cetp inhibitors
WO2006098394A1 (ja) 2005-03-14 2006-09-21 Japan Tobacco Inc. 脂質吸収抑制方法および脂質吸収抑制剤
WO2007041494A2 (en) * 2005-09-30 2007-04-12 Merck & Co., Inc. Cholesteryl ester transfer protein inhibitors
WO2007073934A1 (en) * 2005-12-29 2007-07-05 Novartis Ag Pyridinyl amine derivatives as inhibitors of cholesteryl ester transfer protein (cetp)
WO2008018529A1 (en) * 2006-08-11 2008-02-14 Kowa Company, Ltd. Novel pyrimidine compound having benzyl(pyridylmethyl)amine structure and pharmaceutical comprising the compound

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Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009051827A (ja) * 2007-07-30 2009-03-12 Mitsubishi Tanabe Pharma Corp 医薬組成物
WO2011157827A1 (de) 2010-06-18 2011-12-22 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
US20130190540A1 (en) * 2010-07-22 2013-07-25 Kowa Company, Ltd. Method for preparing optically active 1-bromo-1-[3,5-bis(trifluoromethyl)phenyl]ethane
US9272966B2 (en) * 2010-07-22 2016-03-01 Kowa Company, Ltd. Method for preparing optically active 1-bromo-1[3,5-bis(trifluoromethyl)phenyl]ethane
JP2014525929A (ja) * 2011-08-18 2014-10-02 ドクター レディズ ラボラトリーズ リミテッド コレステリルエステル転送タンパク質(cetp)インヒビターとしての置換複素環式アミン化合物
US9351969B2 (en) 2011-08-18 2016-05-31 Dr. Reddy's Laboratories Ltd. Substituted heterocyclic amine compounds as cholesteryl ester-transfer protein (CETP) inhibitors
JP2014527997A (ja) * 2011-09-27 2014-10-23 ドクター レディズ ラボラトリーズ リミテッド アテローム性動脈硬化症の処置のために有用なコレステリルエステル転送タンパク質(cetp)インヒビターとしての5−ベンジルアミノメチル−6−アミノピラゾロ[3,4−b]ピリジン誘導体
WO2014017569A1 (ja) * 2012-07-26 2014-01-30 興和株式会社 血中ldlを低下させるための医薬
JP2015054838A (ja) * 2013-09-12 2015-03-23 興和株式会社 血中ldlコレステロールを低下させる医薬
US10653681B2 (en) 2016-03-16 2020-05-19 Recurium Ip Holdings, Llc Analgesic compounds

Also Published As

Publication number Publication date
US20100249148A1 (en) 2010-09-30
JP5204091B2 (ja) 2013-06-05
CN101679363A (zh) 2010-03-24
EP2138489A1 (en) 2009-12-30
EP2138489A4 (en) 2011-07-06
EP2138489B9 (en) 2012-10-24
EP2138489B1 (en) 2012-07-11
CN101679363B (zh) 2013-06-05
US20090062306A1 (en) 2009-03-05
JPWO2008111604A1 (ja) 2010-06-24
TW200902011A (en) 2009-01-16
KR20090122278A (ko) 2009-11-26
US8012989B2 (en) 2011-09-06
US7790737B2 (en) 2010-09-07

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