KR100942382B1 - 피라졸 유도체를 포함하는 골다공증 예방 및 치료용 조성물 - Google Patents
피라졸 유도체를 포함하는 골다공증 예방 및 치료용 조성물 Download PDFInfo
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
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- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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Abstract
Description
이때 R1은 피리딘, R2는 페닐, 메톡시페닐, 니트로페닐, 퓨라닐이다. 따라서 상기 히드라진은 예를 들어 2-히드라지노피리딘이 사용될 수 있다. 또한, 상기 β-케토에스테르는 예를 들어 에틸 벤조일아세테이트, 3-(3-메톡시페닐)-3-옥소-프로피온 산 에틸 에스테르, 3-(4-니트로페닐)-3-옥소-프로피온 산 또는 에틸 3-(3-퓨릴)-3-옥소프로파노에이트가 사용될 수 있다. 반응용매로는 에탄올 또는 초산이 사용되는 것이 바람직하다. 상기 고리화 반응은 100 내지 130℃의 온도에서 2 내지 72시간 동안 수행하는 것이 바람직하다.
R1과 R2가 상기 정의된 바와 같을 경우, 본 발명의 피라졸 유도체는 상기 화학식 1 내지 4와 같으며, 화학식 1 내지 4의 엔올형 화합물에 대응하는 케토형 화합물은 각각 다음의 화학식 1' 내지 4'와 같다. 호변이성질체 관계에 있는 엔올형과 케토형 화합물은 그 성질이 유사한 것으로 알려져 있다.
<화학식 1'>
<화학식 2'>
<화학식 3'>
<화학식 4'>
본 발명의 화합물은 약학적으로 허용가능한 염의 형태로 사용할 수 있으며, 통상의 방법에 의하여 제조되는 모든 염, 수화물 및 용매화물이 포함된다.
Claims (4)
- 제 1항에 있어서, 상기 피라졸 유도체가 NADPH 옥시다아제(nicotinamide adenine dinucleotide phosphate oxidase) 활성을 억제하는 것을 특징으로 하는 조성물.
- 제 1항에 있어서, 상기 피라졸 유도체가 파골세포에서 NF-κB의 수용성 활성인자 리간드(RANKL)를 억제하는 것을 특징으로 하는 조성물.
- 삭제
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KR1020080027414A KR100942382B1 (ko) | 2008-03-25 | 2008-03-25 | 피라졸 유도체를 포함하는 골다공증 예방 및 치료용 조성물 |
PCT/KR2009/001315 WO2009119987A2 (ko) | 2008-03-25 | 2009-03-17 | 피라졸 유도체를 포함하는 골다공증 예방 및 치료용 조성물 |
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Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2012118309A2 (ko) | 2011-02-28 | 2012-09-07 | 이화여자대학교 산학협력단 | 피라졸 유도체, 이의 제조방법 및 이를 포함하는 골다공증 예방 및 치료용 조성물 |
WO2012118308A2 (ko) * | 2011-02-28 | 2012-09-07 | 이화여자대학교 산학협력단 | 피라졸 유도체를 포함하는 심혈관 질환 예방 및 치료용 조성물. |
KR101252520B1 (ko) * | 2010-09-20 | 2013-04-09 | 서울대학교산학협력단 | Rankl-유도 파골세포형성을 억제하는 벤조피라닐 테트라사이클 |
WO2014035070A1 (ko) | 2012-08-27 | 2014-03-06 | 이화여자대학교 산학협력단 | 피라졸 유도체를 포함하는 신장질환 예방 또는 치료용 조성물 |
KR101395658B1 (ko) | 2012-09-20 | 2014-05-16 | 서울대학교산학협력단 | 4-(5-(2-메톡시페닐)-3-(p-톨릴)-4,5-디하이드로-1H-피라졸-1-일)-4-옥소부탄산을 포함하는 골대사성 질환의 예방 및 치료용 조성물 |
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KR101840702B1 (ko) | 2017-11-01 | 2018-03-22 | 압타바이오 주식회사 | 간질환 치료제 |
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- 2008-03-25 KR KR1020080027414A patent/KR100942382B1/ko active IP Right Grant
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- 2009-03-17 WO PCT/KR2009/001315 patent/WO2009119987A2/ko active Application Filing
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EP0469357A1 (de) * | 1990-07-24 | 1992-02-05 | Bayer Ag | 1-[Pyri(mi)dyl-(2)]-5-hydroxy-pyrazol-Mikrobizide |
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Cited By (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101252520B1 (ko) * | 2010-09-20 | 2013-04-09 | 서울대학교산학협력단 | Rankl-유도 파골세포형성을 억제하는 벤조피라닐 테트라사이클 |
WO2012118309A2 (ko) | 2011-02-28 | 2012-09-07 | 이화여자대학교 산학협력단 | 피라졸 유도체, 이의 제조방법 및 이를 포함하는 골다공증 예방 및 치료용 조성물 |
WO2012118308A2 (ko) * | 2011-02-28 | 2012-09-07 | 이화여자대학교 산학협력단 | 피라졸 유도체를 포함하는 심혈관 질환 예방 및 치료용 조성물. |
WO2012118308A3 (ko) * | 2011-02-28 | 2012-12-20 | 이화여자대학교 산학협력단 | 피라졸 유도체를 포함하는 심혈관 질환 예방 및 치료용 조성물. |
WO2014035070A1 (ko) | 2012-08-27 | 2014-03-06 | 이화여자대학교 산학협력단 | 피라졸 유도체를 포함하는 신장질환 예방 또는 치료용 조성물 |
KR101395658B1 (ko) | 2012-09-20 | 2014-05-16 | 서울대학교산학협력단 | 4-(5-(2-메톡시페닐)-3-(p-톨릴)-4,5-디하이드로-1H-피라졸-1-일)-4-옥소부탄산을 포함하는 골대사성 질환의 예방 및 치료용 조성물 |
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