KR900018082A - 페닐알카노산의 에스테르 - Google Patents
페닐알카노산의 에스테르 Download PDFInfo
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- KR900018082A KR900018082A KR1019900006517A KR900006517A KR900018082A KR 900018082 A KR900018082 A KR 900018082A KR 1019900006517 A KR1019900006517 A KR 1019900006517A KR 900006517 A KR900006517 A KR 900006517A KR 900018082 A KR900018082 A KR 900018082A
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- phenyl
- methyl
- propionate
- hydroxy
- aminopropoxy
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- 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
- C07D405/12—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 chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
- C07D317/72—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 spiro-condensed with carbocyclic 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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- 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
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- 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
- A61P9/06—Antiarrhythmics
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- 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
- A61P9/08—Vasodilators for multiple indications
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
- C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
- C07D317/14—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D317/18—Radicals substituted by singly bound oxygen or sulfur atoms
- C07D317/24—Radicals substituted by singly bound oxygen or sulfur atoms esterified
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- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
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- 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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Description
Claims (13)
- 일반식(Ⅰ)의 페닐알카노산의 에스테르 및 이의 약제학적으로 허용되는 산 부가염.상기식에서, R1은 헤테로 원자로서(ⅰ) 1 또는 2개의 질소, (ⅱ)총 2 또는 3개의 질소 황, 또는 (ⅲ) 1 또는 2개의 황을 함유하는 4내지 10원, 포화 또는 불포화, 모노-또는 비-사이클릭 헤테로 환이고;R2는 수소이거나;R1및 R2는 이들이 결합된 질소와 함께, 헤테로 원자로서 (ⅰ) 1 또는 2개의 질소, (ⅱ)총 2 또는 3개의 질소 및 산소를 포함하는 4내지 7원, 포화 또는 불포화, 모노-사이클릭 헤테로 환(여기서, R1으로 표기된 또는 R1및 R2가 이들이 결합된 질소와 함께 형성한 헤테로 환은 C1-4알킬 및 C2-5아실중에서 선택된 1개의 치환체로 치환될 수 있다)을 형성하며;R3는 각각 독립적으로 수소 또는 C1-4알킬이고;R4는 수소, 할로겐, 트리할로메틸, C1-4알킬, C1-4알콕시, C2-5아실, 시아노, 니트로 또는 니트록시이며;R|5는 각각 독립적으로 수소, C1-4알킬 또는 페닐 이거나;2개의 R5는 이들이 결합된 탄소와 함께 사이틀로펜탄 또는 사이클로헥산을 형성한다.
- 제1항에 있어서, R1및 R2가 이들이 결합된 질소와 함께, 헤테로 원자로서 총 2 또는 3개의 질소 및 산소를 함유하는 4내지 7원, 포화 또는 불포화, 모노-사이클릭 헤테로 환을 형성하는 에스테르.
- 제1항에 있어서, R1및 R2가 이들이 결합된 질소와 함께 모노폴리노 그룹을 나타내는 에스테르.
- 제3항에 있어서, (2,2-디메틸-1,3-디옥솔란-4-일)메틸 3-[4-[2-하이드록시-3-(2-모르폴리노카보닐아미노에틸)아미노프로폭시]페닐]프로피오네이트,(2,2-디메틸-1,3-디옥솔란-4-일)메틸 3-[4-[2-하이드록시-3-(1,1-디메틸-2-모르폴리노카보닐아미노에틸)아미노프로폭시]페닐]프로피오네이트,(2-메틸-2-페닐-1,3-디옥솔란-4-일)메틸 3-[4-[2-하이드록시-3-(2-모르폴리노카보닐아미노에틸)아미노프로폭시]페닐]프로피오네이트,(1,4-디옥사스피로[4,4]노난-2-일)메틸 3-[4-[2-하이드록시-3-(2-모르폴리노카보닐아미노에틸)아미노프로폭시]페닐]프로피오네이트,(2,2-디메틸-1,3-디옥솔란-4-일)메틸 3-[3-플루오로-4-[2-하이드록시-3-(2-모르폴리노카보닐아미노에틸)아미노프로폭시]페닐]프로피오네이트,(2,2-디메틸-1,3-디옥솔란-4-일)메틸 3-[3-메틸-4-[2-하이드록시-3-(2-모르폴리노카보닐아미노에틸)아미노프로폭시]페닐]프로피오네이트,(2,2-디메틸-1,3-디옥솔란-4-일)메틸 3-[3-메톡시-4-[2-하이드록시-3-(2-모르폴리노카보닐아미노에틸)아미노프로폭시]페닐]프로피오네이트,(2,2-디메틸-1,3-디옥솔란-4-알)메틸 3-[3-아세틸-4-[2-하이드록시-3-(2-모르폴리노카보닐아미노에틸)아미노프로폭시]페닐]프로피오네이트,(2,2-디메틸-1,3-디옥솔란-4-일)메틸 3-[3-시아노-4-[2-하이드록시-3-(2-모르폴리노카보닐아미노에틸)아미노프로폭시]페닐]프로피오네이트 또는 (2,2-디메틸-1,3-디옥솔란-4-알)메틸 3-[3-니트로-4-[2-하이드록시-3-(2-모르폴리노카보닐아미노에틸)아미노프로폭시]페닐]프로피오네이트인 에스테르.
- 제1항에 있어서, R1및 R2가 이들이 결합된 질소와 함께, 헤테로 원자 1 또는 2개의 질소를 함유하는 4내지 7원, 포화 또는 불포화, 모노-사이클릭 헤테로 환을 형성하는 에스테르.
- 제1항에 있어서, R1및 R2가 이들이 결합된 질소와 함께 피페라지닐을 나타내는 에스테르.
- 제6항에 있어서, (2,2-디메틸-1,3-디옥솔란-4-일)메틸 3-[4-[2-하이드록시-3-[2-(4-메틸피페라진-1-일)카보닐아미노에틸)아미노프로폭시]페닐]프로피오네이트인 에스테르.
- 제1항에 있어서, R1이 헤테로 원자로서 1 또는 2개의 질소을 함유하는 4 내지 10원, 포화 또는 불포화, 모노-또는 비-사이클릭 헤테로 환이고, R2가 수소인 에스테르.
- 제1항에 있어서, R1이 피리딜 그룹이고 R2가 수소인 에스테르.
- 제9항에 있어서, (2,2-디메틸-1,3-디옥솔란-4-일)메틸 3-[4-[2-하이드록시-3-[2-(4-피리딜)아미노 카보닐아미노에틸)아미노프로폭시]페닐]프로피오네이트인 에스테르.
- (ⅰ) 일반식(Ⅱ)의 화합물을 일반식(Ⅲ)의 화합물과 에톡사이드-절단 반응시키고, (ⅱ) 일반식(Ⅰ)의 페닐 알카노산의 에스테르를 필요한 경우 공지된 방법으로 상응하는 산 부가염으로 전환시킴을 특징으로 하여, 일반식(Ⅰ)의 페닐알카노산의 에스테르 및 이의 약제학적으로 허용되는 산 부가염을 제조하는 방법.상기식에서, R1은, 헤테로 원자로서 (ⅰ) 1 또는 2개의 질소, (ⅱ)총 2 또는 3개의 질소 황, 또는 (ⅲ) 1 또는 2개의 황을 함유하는 4내지 10원, 포화 또는 불포화, 모노-또는 비-사이클릭 헤테로 환이고;R2는 수소이거나;R1및 R2는 이들이 결합된 질소와 함께, 헤테로 원자로서 (ⅰ) 1 또는 2개의 질소, 또는 (ⅱ)총 2 또는 3개의 질소 및 산소를 함유하는 4내지 7원, 포화 또는 불포화, 모노-사이클릭 헤테 환(여기서, R1으로 표기된 또는 R1및 R2가 이들이 결합된 질소와 함께 형성한 헤테로 환은 C1-4알킬 및 C2-5아실중에서 선택된 1개의 치환체로 치환될 수 있다)을 형성하며;R3는 각각 독립적으로 수소 또는 C1-4알킬이고;R4는 수소, 할로겐, 트리할로메틸, C1-4알킬, C1-4알콕시, C2-5아실, 시아노, 니트로 또는 니트록시이며;R|5는 각각 독립적으로 수소, C1-4알킬 또는 페닐 이거나;2개의 R5는 이들이 결합된 탄소와 함께 사이틀로펜탄 또는 사이클로헥산이다.
- 활성성분으로서 제1항에 따른 일반식(Ⅰ)의 페닐알카노산의 에스테르 또는 이의 약제학적으로 허용되는 산 부가염을 약제학적 담체 또는 피복물과 함께 함유하는 약제학적 조성물.
- 제1항에 따른 일반식(Ⅰ)의 페닐알카노산의 에스테르 또는 이의 약제학적으로 허용되는 산 부가염의 유효량을 투여함을 특징으로 하여, 협심증, 심근 결색증, 울혈성심부전증, 고혈압, 부정맥과 같은 심장혈관 질병을 예방하고 치료하는 방법.※ 참고사항 : 최초출원내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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JP1-119873 | 1989-05-12 | ||
JP11987389 | 1989-05-12 |
Publications (2)
Publication Number | Publication Date |
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KR900018082A true KR900018082A (ko) | 1990-12-20 |
KR970003457B1 KR970003457B1 (ko) | 1997-03-18 |
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Application Number | Title | Priority Date | Filing Date |
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KR1019900006517A KR970003457B1 (ko) | 1989-05-12 | 1990-05-09 | 페닐알킨산의 에스테르 |
Country Status (9)
Country | Link |
---|---|
US (1) | US5013734A (ko) |
EP (1) | EP0397031B1 (ko) |
JP (2) | JPH0730068B2 (ko) |
KR (1) | KR970003457B1 (ko) |
AT (1) | ATE108788T1 (ko) |
CA (1) | CA2015730C (ko) |
DE (1) | DE69010757T2 (ko) |
DK (1) | DK0397031T3 (ko) |
ES (1) | ES2060853T3 (ko) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
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WO1997013744A1 (en) * | 1995-10-10 | 1997-04-17 | The University Of Melbourne | 3-amino-propoxyphenyl derivatives (i) |
US20060286037A1 (en) * | 2003-08-08 | 2006-12-21 | Ono Pharmaceutical Co., Ltd. | Heart-slowing drug containing short-acting ß blocker as the active ingredient |
ITMI20110343A1 (it) * | 2011-03-04 | 2012-09-05 | Procos Spa | Processo per la sintesi enantioselettiva di landiolol |
ES2532851T3 (es) | 2012-07-20 | 2015-04-01 | Procos S.P.A. | Proceso para la síntesis enantioselectiva de landiolol |
CN104003973B (zh) * | 2014-06-05 | 2016-02-24 | 重庆植恩药业有限公司 | 一种兰地洛尔草酸盐的制备方法 |
CN106608863A (zh) * | 2015-10-23 | 2017-05-03 | 北京创立科创医药技术开发有限公司 | 一种盐酸兰地洛尔的制备方法 |
CN106248825B (zh) * | 2016-07-21 | 2017-10-10 | 山东省分析测试中心 | 盐酸兰地洛尔原料药物中起始物料a的检测方法 |
CN118754867A (zh) * | 2024-09-05 | 2024-10-11 | 伊诺药物研究(南京)有限公司 | 一种盐酸兰地洛尔的合成方法 |
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SE8004087L (sv) * | 1980-06-02 | 1981-12-03 | Haessle Ab | Nya parasubstituerade 3-fenoxi-1-alkylaminopropanol-2-er med betareceptorblockerande egenskaper, samt forfarande for deras framstellning, farmaceutiska beredningar innehallande desamma, och metod att behandla akut ... |
ZA827646B (en) * | 1981-11-12 | 1983-08-31 | American Hospital Supply Corp | Esters of aryloxypropanolamine derivatives |
US4548941A (en) * | 1984-07-30 | 1985-10-22 | Merck & Co., Inc. | 1,5-Methano-1H-4-benzazonine dicarboxylates, process for preparing and use as calcium blockers |
GB2169892B (en) * | 1985-01-23 | 1988-02-03 | Ferrer Int | Piperazine derivatives |
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1990
- 1990-04-30 CA CA002015730A patent/CA2015730C/en not_active Expired - Fee Related
- 1990-05-03 ES ES90108375T patent/ES2060853T3/es not_active Expired - Lifetime
- 1990-05-03 DK DK90108375.8T patent/DK0397031T3/da active
- 1990-05-03 DE DE69010757T patent/DE69010757T2/de not_active Expired - Fee Related
- 1990-05-03 AT AT90108375T patent/ATE108788T1/de not_active IP Right Cessation
- 1990-05-03 EP EP90108375A patent/EP0397031B1/en not_active Expired - Lifetime
- 1990-05-08 JP JP2116947A patent/JPH0730068B2/ja not_active Expired - Lifetime
- 1990-05-09 KR KR1019900006517A patent/KR970003457B1/ko not_active IP Right Cessation
- 1990-05-11 US US07/521,962 patent/US5013734A/en not_active Expired - Lifetime
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1993
- 1993-04-07 JP JP5104985A patent/JP2539734B2/ja not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
ES2060853T3 (es) | 1994-12-01 |
JPH0673044A (ja) | 1994-03-15 |
JPH0372475A (ja) | 1991-03-27 |
US5013734A (en) | 1991-05-07 |
CA2015730A1 (en) | 1990-11-12 |
ATE108788T1 (de) | 1994-08-15 |
JP2539734B2 (ja) | 1996-10-02 |
JPH0730068B2 (ja) | 1995-04-05 |
DK0397031T3 (da) | 1994-10-31 |
CA2015730C (en) | 1997-10-07 |
EP0397031A1 (en) | 1990-11-14 |
EP0397031B1 (en) | 1994-07-20 |
KR970003457B1 (ko) | 1997-03-18 |
DE69010757T2 (de) | 1994-12-15 |
DE69010757D1 (de) | 1994-08-25 |
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