WO2008129951A1 - 新規なジベンジ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

新規なジベンジ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
WO2008129951A1
WO2008129951A1 PCT/JP2008/057058 JP2008057058W WO2008129951A1 WO 2008129951 A1 WO2008129951 A1 WO 2008129951A1 JP 2008057058 W JP2008057058 W JP 2008057058W WO 2008129951 A1 WO2008129951 A1 WO 2008129951A1
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Prior art keywords
alkyl group
compound
lower alkyl
hydrogen atom
medicine
Prior art date
Application number
PCT/JP2008/057058
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English (en)
French (fr)
Inventor
Tadaaki Ohgiya
Toru Miura
Ayumu Okuda
Toshiharu Arai
Koichi Yamazaki
Taro Aoki
Katsutoshi Miyosawa
Haruki Shibata
Kimiyuki Shibuya
Original Assignee
Kowa Company, 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
Priority to MX2009010962A priority Critical patent/MX2009010962A/es
Priority to EA200970943A priority patent/EA017321B1/ru
Application filed by Kowa Company, Ltd. filed Critical Kowa Company, Ltd.
Priority to BRPI0810880A priority patent/BRPI0810880A2/pt
Priority to NZ580777A priority patent/NZ580777A/en
Priority to AU2008241904A priority patent/AU2008241904B2/en
Priority to KR1020097023309A priority patent/KR101501299B1/ko
Priority to ES08740159.2T priority patent/ES2533910T3/es
Priority to CA2683534A priority patent/CA2683534C/en
Priority to DK08740159.2T priority patent/DK2149563T3/en
Priority to PL08740159T priority patent/PL2149563T3/pl
Priority to JP2009510828A priority patent/JP5244095B2/ja
Priority to EP20080740159 priority patent/EP2149563B9/en
Priority to CN2008800199910A priority patent/CN101679309B/zh
Publication of WO2008129951A1 publication Critical patent/WO2008129951A1/ja
Priority to IL201402A priority patent/IL201402A/en
Priority to HK10104447.9A priority patent/HK1138274A1/xx

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (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、ハロ低級アルキル基、シアノ基等を示し、R6はアルキル基、シクロアルキル基等を示し、R7、R8、R9、及びR10は水素原子、ハロゲン原子、低級アルキル基、ハロ低級アルキル基等を示し、R11及びR12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等を示し、R13は、水素原子、ハロゲン原子、低級アルコキシ基等を示す）。
PCT/JP2008/057058 2007-04-13 2008-04-10 新規なジベンジ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 WO2008129951A1 (ja)

Priority Applications (15)

Application Number Priority Date Filing Date Title
DK08740159.2T DK2149563T3 (en) 2007-04-13 2008-04-10 Novel pyrimidine compound with dibenzylaminstruktur, and medicine comprising the compound
CA2683534A CA2683534C (en) 2007-04-13 2008-04-10 Novel pyrimidine compound having dibenzylamine structure and medicament comprising the same
BRPI0810880A BRPI0810880A2 (pt) 2007-04-13 2008-04-10 novo composto de pirimidina com a estrutura de dibenzilamina e medicamento à base do mesmo
EA200970943A EA017321B1 (ru) 2007-04-13 2008-04-10 Производные n,n-дибензил-2-аминопиримидина и лекарственные средства, их содержащие
AU2008241904A AU2008241904B2 (en) 2007-04-13 2008-04-10 Novel pyrimidine compound having dibenzylamine structure and medicament comprising the same
KR1020097023309A KR101501299B1 (ko) 2007-04-13 2008-04-10 신규한 디벤질아민 구조를 갖는 피리미딘 화합물 및 이것을 함유하는 의약
PL08740159T PL2149563T3 (pl) 2007-04-13 2008-04-10 Nowy związek pirymidynowy mający strukturę dibenzyloaminy i lek zawierający ten związek
MX2009010962A MX2009010962A (es) 2007-04-13 2008-04-10 Compuesto pirimidina novedoso que tiene estructura de dibencilamina y medicamento que comprende el mismo.
NZ580777A NZ580777A (en) 2007-04-13 2008-04-10 Novel pyrimidine compound having dibenzylamine structure, and medicine comprising the compound
ES08740159.2T ES2533910T3 (es) 2007-04-13 2008-04-10 Compuesto novedoso de pirimidina que tiene estructura de dibencilamina y medicamento que comprende el compuesto
JP2009510828A JP5244095B2 (ja) 2007-04-13 2008-04-10 新規なジベンジ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
EP20080740159 EP2149563B9 (en) 2007-04-13 2008-04-10 Novel pyrimidine compound having dibenzylamine structure, and medicine comprising the compound
CN2008800199910A CN101679309B (zh) 2007-04-13 2008-04-10 具有二苄胺结构的新型嘧啶化合物和含有该化合物的药物
IL201402A IL201402A (en) 2007-04-13 2009-10-11 A pyrimidine compound with a dibenzylamine formulation and a drug containing it
HK10104447.9A HK1138274A1 (en) 2007-04-13 2010-05-06 Novel pyrimidine compound having dibenzylamine structure, and medicine comprising the compound

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US91162007P 2007-04-13 2007-04-13
US60/911,620 2007-04-13

Publications (1)

Publication Number Publication Date
WO2008129951A1 true WO2008129951A1 (ja) 2008-10-30

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/057058 WO2008129951A1 (ja) 2007-04-13 2008-04-10 新規なジベンジ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 (20)

Country Link
US (1) US7659271B2 (ja)
EP (1) EP2149563B9 (ja)
JP (2) JP5244095B2 (ja)
KR (1) KR101501299B1 (ja)
CN (1) CN101679309B (ja)
AU (1) AU2008241904B2 (ja)
BR (1) BRPI0810880A2 (ja)
CA (1) CA2683534C (ja)
DK (1) DK2149563T3 (ja)
EA (1) EA017321B1 (ja)
ES (1) ES2533910T3 (ja)
HK (1) HK1138274A1 (ja)
HU (1) HUE024898T2 (ja)
IL (1) IL201402A (ja)
MX (1) MX2009010962A (ja)
NZ (1) NZ580777A (ja)
PL (1) PL2149563T3 (ja)
PT (1) PT2149563E (ja)
TW (1) TWI439453B (ja)
WO (1) WO2008129951A1 (ja)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010061621A1 (ja) 2008-11-28 2010-06-03 興和株式会社 ｔｒａｎｓ－｛４－［（アルキルアミノ）メチル］シクロヘキシル｝酢酸エステルの製造方法
WO2011152508A1 (ja) 2010-06-04 2011-12-08 興和株式会社 光学活性ジベンジルアミン誘導体及びその製造方法
WO2012011516A1 (ja) 2010-07-22 2012-01-26 興和株式会社 光学活性１－ブロモ－１－［３，５－ビス（トリフルオロメチル）フェニル］エタンの製造方法
WO2012046681A1 (ja) 2010-10-04 2012-04-12 興和株式会社 脂質代謝関連ｍＲＮＡの発現抑制剤
WO2013081087A1 (ja) * 2011-12-02 2013-06-06 興和株式会社 光学活性化合物の製造方法
WO2013080999A1 (ja) 2011-11-29 2013-06-06 興和株式会社 ＮＰＣ１Ｌ１及び／又はＬＩＰＧ ｍＲＮＡの発現抑制剤並びに肥満症の予防及び／又は治療剤
JP2013136572A (ja) * 2011-12-02 2013-07-11 Kowa Co 光学活性ジベンジルアミン誘導体及びその製造方法
WO2013137371A1 (ja) * 2012-03-15 2013-09-19 興和株式会社 新規ピリミジン化合物及びそれらを含有する医薬
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
JP2014520795A (ja) * 2011-07-08 2014-08-25 ノバルティス アーゲー 高トリグリセリド対象においてアテローム性動脈硬化症を治療する方法
WO2014192903A1 (ja) 2013-05-31 2014-12-04 興和株式会社 ジベンジルアミン構造を有するピリミジン化合物の新規形態
WO2017209158A1 (ja) * 2016-05-31 2017-12-07 興和株式会社 医薬組成物

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP5319457B2 (ja) * 2008-08-25 2013-10-16 興和株式会社 新規なジベンジ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
WO2010029756A1 (ja) * 2008-09-12 2010-03-18 興和株式会社 ５－[２－（メチルチオ）エトキシ]ピリミジン－２－アミンの製造方法
CN104628584B (zh) * 2013-11-08 2017-03-08 广州朗圣药业有限公司 一种适合工业化的高纯度达泊西汀的制备方法
EP3225240A4 (en) * 2014-11-28 2018-06-06 Kowa Company, Ltd. Medicine

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