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WO2013015535A3 - 신규 피리미딘 유도체 및 이를 활성성분으로 포함하는 약학 조성물 - Google Patents

신규 피리미딘 유도체 및 이를 활성성분으로 포함하는 약학 조성물 Download PDF

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Publication number
WO2013015535A3
WO2013015535A3 PCT/KR2012/005193 KR2012005193W WO2013015535A3 WO 2013015535 A3 WO2013015535 A3 WO 2013015535A3 KR 2012005193 W KR2012005193 W KR 2012005193W WO 2013015535 A3 WO2013015535 A3 WO 2013015535A3
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WIPO (PCT)
Prior art keywords
pharmaceutical composition
active ingredient
composition including
including same
pyrimidine derivative
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PCT/KR2012/005193
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English (en)
French (fr)
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WO2013015535A2 (ko
Inventor
박철현
김원정
정영희
김남두
장영길
김맹섭
Original Assignee
한국보건산업진흥원
한미약품 주식회사
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Priority to CN201280041923.0A priority Critical patent/CN103764661A/zh
Priority to US14/232,667 priority patent/US20140163226A1/en
Priority to JP2014522734A priority patent/JP2014521638A/ja
Priority to EP12817633.6A priority patent/EP2738174A4/en
Publication of WO2013015535A2 publication Critical patent/WO2013015535A2/ko
Publication of WO2013015535A3 publication Critical patent/WO2013015535A3/ko

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    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Child & Adolescent Psychology (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Reproductive Health (AREA)
  • Nutrition Science (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

본 발명은 디아실글리세롤 0-아실전이효소 1형의 활성을 억제하는 하기 화학식 1의 화합물, 및 이의 약학적으로 허용 가능한 염으로 이루어진 군으로부터 선택된 화합물 및 이를 유효성분으로 함유하는 약학 조성물에 관한 것으로, 본 발명의 화합물은 DGAT1의 활성에 의해 유발되는 비만, 제2형 당뇨병, 이상지질혈증, 대사증후군 등의 질환에 대한 부작용 없이 효과적인 치료제로서 활용될 수 있다. 상기 [화학식 1]에서, A, B, X 및 R5~7은 본원 명세서에서 정의한 바와 같다.
PCT/KR2012/005193 2011-07-27 2012-06-29 신규 피리미딘 유도체 및 이를 활성성분으로 포함하는 약학 조성물 WO2013015535A2 (ko)

Priority Applications (4)

Application Number Priority Date Filing Date Title
CN201280041923.0A CN103764661A (zh) 2011-07-27 2012-06-29 新嘧啶衍生物和包含其作为活性成分的药物组合物
US14/232,667 US20140163226A1 (en) 2011-07-27 2012-06-29 Novel pyrimidine derivative and pharmaceutical composition including same as an active ingredient
JP2014522734A JP2014521638A (ja) 2011-07-27 2012-06-29 新規ピリミジン誘導体およびこれを活性成分として含む薬学的組成物
EP12817633.6A EP2738174A4 (en) 2011-07-27 2012-06-29 NOVEL PYRIMIDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME AS ACTIVE INGREDIENT

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020110074706A KR20130013199A (ko) 2011-07-27 2011-07-27 신규 피리미딘 유도체 및 이를 활성성분으로 포함하는 약학 조성물
KR10-2011-0074706 2011-07-27

Publications (2)

Publication Number Publication Date
WO2013015535A2 WO2013015535A2 (ko) 2013-01-31
WO2013015535A3 true WO2013015535A3 (ko) 2013-04-11

Family

ID=47601603

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2012/005193 WO2013015535A2 (ko) 2011-07-27 2012-06-29 신규 피리미딘 유도체 및 이를 활성성분으로 포함하는 약학 조성물

Country Status (6)

Country Link
US (1) US20140163226A1 (ko)
EP (1) EP2738174A4 (ko)
JP (1) JP2014521638A (ko)
KR (1) KR20130013199A (ko)
CN (1) CN103764661A (ko)
WO (1) WO2013015535A2 (ko)

Citations (4)

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Publication number Priority date Publication date Assignee Title
US20050038068A1 (en) * 2003-05-16 2005-02-17 Iyengar Rajesh R. Thienopyridones as AMPK activators for the treatment of diabetes and obesity
KR20060100412A (ko) * 2003-10-23 2006-09-20 글락소 그룹 리미티드 비만, 당뇨, 우울증 및 불안증을 치료하기 위한 ｍｃｈｒ１ 길항제로서의 3-(4-아미노페닐)티에노피리미드-4-온유도체
KR20110044053A (ko) * 2009-10-22 2011-04-28 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노[3,2-ｄ]피리미딘 화합물
KR20110055202A (ko) * 2009-11-19 2011-05-25 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노[3,2-ｄ]피리미딘 화합물

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MXPA01012317A (es) 2000-12-28 2002-07-22 Warner Lambert Co Prueba de aciltransferasa del diacilglicerol (dgat).
WO2004004755A1 (en) 2002-07-09 2004-01-15 Endocrine Health I Göteborg Ab Treatment of osteoporosis
JP4164645B2 (ja) 2002-08-09 2008-10-15 株式会社大塚製薬工場 Ｄｇａｔ阻害剤
CA2497901A1 (en) 2002-09-06 2004-03-18 Takeda Pharmaceutical Company Limited Furan or thiophene derivative and medicinal use thereof
RU2342388C2 (ru) 2002-11-22 2008-12-27 Джапан Тобакко Инк. Конденсированные бициклические азотсодержащие гетероциклы, обладающие dgat ингибирующим действием
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050038068A1 (en) * 2003-05-16 2005-02-17 Iyengar Rajesh R. Thienopyridones as AMPK activators for the treatment of diabetes and obesity
US20060287356A1 (en) * 2003-05-16 2006-12-21 Iyengar Rajesh R Thienopyridones as AMPK activators for the treatment of diabetes and obesity
KR20060100412A (ko) * 2003-10-23 2006-09-20 글락소 그룹 리미티드 비만, 당뇨, 우울증 및 불안증을 치료하기 위한 ｍｃｈｒ１ 길항제로서의 3-(4-아미노페닐)티에노피리미드-4-온유도체
KR20110044053A (ko) * 2009-10-22 2011-04-28 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노[3,2-ｄ]피리미딘 화합물
KR20110055202A (ko) * 2009-11-19 2011-05-25 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노[3,2-ｄ]피리미딘 화합물

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP2738174A4 *

Also Published As

Publication number Publication date
WO2013015535A2 (ko) 2013-01-31
CN103764661A (zh) 2014-04-30
KR20130013199A (ko) 2013-02-06
EP2738174A2 (en) 2014-06-04
JP2014521638A (ja) 2014-08-28
US20140163226A1 (en) 2014-06-12
EP2738174A4 (en) 2014-12-17

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