KR900016175A - 피페리딘 화합물, 이의 제조방법 및 용도 - Google Patents
피페리딘 화합물, 이의 제조방법 및 용도 Download PDFInfo
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- KR900016175A KR900016175A KR1019890005606A KR890005606A KR900016175A KR 900016175 A KR900016175 A KR 900016175A KR 1019890005606 A KR1019890005606 A KR 1019890005606A KR 890005606 A KR890005606 A KR 890005606A KR 900016175 A KR900016175 A KR 900016175A
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Abstract
내용 없음.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (20)
- 일반식(I)의 피페리딘 화합물 및 이의 약학적으로 허용되는 산과의 염.상기식에서, R3는 하나 이상의 할로겐, C1-6-알콕시, 임의로 치환된 아릴옥시 또는 아릴-C1-6-알콕시, 시아노, 모노 또는 폴리할로겐화 C1-6-알킬, C1-6-알케닐, C1-6-알킬, C3-5-알킬렌 또는 트리플루오로메틸 그룹으로 임의로 치환된 3,4-메틸렌디옥시페닐, 아릴 또는 헤테로 아릴이고, R1은 하나 이상의 시아노, 에스테르, 디알킬아미노, 하이드록시, 아미도, 할로게노, 치환되거나 비치환된 피페리디노, 모르폴리노, 티오 모르폴리노, 디옥솔라닐, 테트라하이드로푸라닐, C1-8-알콕시 또는 C3-8-사이클로알킬 그룹에 의해 치환되거나 비치환된 직쇄 또는 측쇄 C1-8-알킬이며,X는 수소, 할로겐, 트리플루오로메틸, 하이드로시, 시아노 또는 C1-8-알콕시이고, Y는 산소 또는 황원자이며, 단, R3가 하나 이상의 C1-6-알킬, C1-6-알콕시, C3-5-알킬렌, C3-8-사이클로알킬 또는 아르알콕시에 의해 임의로 치환된 3,4-메틸렌 디옥시페닐, 아릴 또는 헤테로아릴이고, 이와 동시에 X가 수소 또는 할로겐인 경우, R1은 비치환된 C1-6-알킬이 아니다.
- 제1항에 있어서, R3가 할로겐 또는 C1-6-알콕시로 임의로 치환된 3,4-메틸렌디옥시페닐이거나 C3-5-알킬렌으로 치환된 페닐인 화합물.
- 제1항에 있어서, R1이 직쇄 또는 측쇄 C1-8-알킬인 화합물.
- 제1항에 있어서, X가 수소, 할로겐, 트리플루오로메틸 또는 C1-6-알콕시인 화합물.
- 제1항에 있어서, R3가 할로겐 또는 C1-6알콕시로 임의로 치환된 3,4-메틸렌 디옥시페닐이거나, C3-5-알킬렌으로 치환된 페닐이고, R1이 직쇄 또는 측쇄 C1-8-알킬이며, X가 수소, 할로겐 트리플루오로메틸 또는 C1-6-알콕시인 화합물.
- 제1항에 있어서, (-)-트랜스-3-(2-브로모-4,5-메틸렌디옥시펜옥시메틸)-1-부틸-4-(4-플루오로 페닐)-피페리딘 염산염인 화합물.
- 제1항에 있어서, (-)-트랜스-4-(4-메톡시 페닐)-3-(3,4-메틸렌디옥시펜옥시메틸)-1-펜틸-피페리딘 옥살레이트인 화합물.
- 제1항에 있어서, (+)-트랜스-4-(4-메톡시 페닐)-3-(3,4-메틸렌디옥시펜옥시메틸)-1-펜틸-피페리딘 옥살레이트인 화합물.
- 제1항에 있어서, (-)-트랜스-4-(4-플루오로 페닐)-3-(3,4-메틸렌디옥시펜옥시메틸)-1-(3-티아모르폴리닐프로필)-피페리딘 이염산염인 화합물.
- a) 일반식(II) 화합물을 일반식(IV) 화합물과 반응시키거나, b) 일반식(III) 화합물을 일반식(V) 화합물과 반응시키거나, c) 일반식(III) 화합물을 브롬과 반응시킨후, 임의로 약학적으로 허용되는 산과의 염을 형성시키는 단계를 포함함을 특징으로 하여, 제1항에 따른 화합물을 제조하는 방법.상기식에서, R1, R3, X, 및 Y는 상기에서 정의한 바와 같고, Z는 할로겐과 같은 이탈그룹이며, Y는 산소 또는 항원자이다.
- 제1항에 따른 화합물을 약학적으로 허용되는 담체 또는 희석제와 함께 함유하는 약학적 조성물.
- 제11항에 있어서, 활성 화합물 1 내지 100mg을 함유하는 경구투여 단위용량형인 약학적 조성물.
- 칼슘과다 차단량의 일반식(I)의 피페리딘 화합물을 뇌세포의 칼슘과다증과 관련된 질환의 치료를 필요로 하는 대상에 투여함을 특징으로 하여, 사람을 포함하는 포유동물 뇌세포의 칼슘과다증과 관련된 질환을 치료하는 방법.상기식에서, R3는 하나 이상의 할로겐, C1-6-알콕시, 임의로 치환된 아릴옥시 또는 아릴-C1-6-알콕시, 시아노, 모노 또는 폴리할로겐화 C1-6-알킬, C1-6-알케닐, C1-6-알킬, C3-5-알킬렌 또는 트리플루오로메틸 그룹으로 임의로 치환된 3,4-메틸렌디옥시페닐, 아릴 또는 헤테로 아릴이고, R1은 하나 이상의 시아노, 에스테르, 디알킬아미노, 하이드록시, 아미도, 할로게노, 치환되거나 비치환된 피페리디노, 모르폴리노, 티오 모르폴리노, 디옥솔라닐, 테트라하이드로푸라닐, C1-8-알콕시 또는 C3-8-사이클로알킬 그룹에 의해 치환되거나 비치환된 직쇄 또는 측쇄 C1-8알킬이며, X는 수소, 할로겐, 트리플루오로메틸, 하이드록시, 시아노 또는 CSB>1-8-알콕시이고, Y는 산소 또는 황원자이며, 단, R3가 하나 이상의 C1-6-알킬, C1-6-알콕시, C3-5-알킬렌, C3-8-사이클로알킬 또는 아르알콕시에 의해 임로 치환된 3,4-메틸렌 디옥시페닐, 아릴 또는 헤테로아릴이고, 이와 동시에 X가 수소 또는 할로겐인 경우, R1은 비치환된 C1-8-알킬, C1-6-알콕시-C1-8-알킬 또는 C3-8-사이클로알킬-C1-8-알킬이 아니다.
- 제13항에 있어서, 허혈증 또는 두부(head) 손상의 치료에 직접적으로 사용되는 치료방법.
- 포유동물 뇌세포의 칼슘과다증을 치료하기 위한 제1항에 따른 화합물의 용도.
- 허혈증 또는 두부손상을 치료하는데 유용한 약제를 제조하기 위한 일반식(I)의 화합물 또는 이의 약학적으로 허용되는 산과의 염의 용도.상기식에서, R3는 하나 이상의 할로겐, C1-6-알콕시, 임의로 치환된 아릴옥시 또는 아릴-C1-6-알콕시, 시아노, 모노 또는 폴리할로겐화 3C1-6-알킬, C1-6-알케닐, C1-6-알킬, C3-5-알킬렌 또는 트리플루오로메틸 그룹으로 임의로 치환된 3,4-메틸렌디옥시페닐, 아릴 또는 헤테로 아릴이고, R1은 하나 이상의 시아노, 에스테르, 디알킬아미노, 하이드록시, 아미도, 할로게노, 치환되거나 비치환된 피페리디노, 모르폴리노, 티오모르폴리노, 디옥솔라닐, 테트라하이드로푸라닐, C1-8-알콕시 또는 C3-8-사이클로알킬 그룹에 의해 치환되거나 비치환된 직쇄 또는 측쇄 C1-8알킬이며, X는 수소, 할로겐, 트리플루오로메틸, 하이드록시, 시아노 또는 C1-8-알콕시이고, Y는 산소 또는 황원자이며, 단, R3가 하나 이상의 C1-6-알킬, C1-6-알콕시, C3-5-알킬렌, C3-8-사이클로알킬 또는 아르알콕시에 의해 임의로 치환된 3,4-메틸렌 디옥시페닐, 아릴 또는 헤테로아릴이고, 이와 동시에 X가 수소 또는 할로겐인 경우, R1은 비치환된 C1-8-알킬이 아니다.
- 제1항에 있어서, (+-)-트랜스-3-(3,4-메틸렌디옥시펜옥시메틸)-1-펜틸-4-(3-트리플루오로메틸페닐)-1-펜틸피페리딘 염산염인 화합물.
- 제1항에 있어서, (+)-트랜스-3-(2-브로모-4,5-메틸렌디옥시펜옥시메틸)-4-(4-플루오로페닐)-1-펜틸피페리딘 염산염인 화합물.
- 제1항에 있어서, (+-)-트랜스-3-(3,4-메틸렌디옥시펜옥시메틸)-1-펜틸-4-(4-펜틸옥시페닐)-피페리딘 염산염인 화합물.
- 제1항에 있어서, (+-)-트랜스-3-(4-알릴-2-메톡시펜옥시메틸)-1-부틸-4-페닐피페리딘옥살레이트인 화합물.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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DK2310/88 | 1988-04-28 | ||
DK231088A DK231088D0 (da) | 1988-04-28 | 1988-04-28 | Piperidinforbindelser, deres fremstilling og anvendelse |
Publications (1)
Publication Number | Publication Date |
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KR900016175A true KR900016175A (ko) | 1990-11-12 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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KR1019890005606A KR900016175A (ko) | 1988-04-28 | 1989-04-28 | 피페리딘 화합물, 이의 제조방법 및 용도 |
Country Status (17)
Country | Link |
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EP (1) | EP0339579B1 (ko) |
JP (1) | JP2857414B2 (ko) |
KR (1) | KR900016175A (ko) |
CN (1) | CN1037332A (ko) |
AT (1) | ATE168375T1 (ko) |
AU (1) | AU631121B2 (ko) |
DE (1) | DE68928735T2 (ko) |
DK (1) | DK231088D0 (ko) |
ES (1) | ES2118708T3 (ko) |
FI (1) | FI92822C (ko) |
HU (1) | HUT55387A (ko) |
IL (1) | IL89903A0 (ko) |
NO (1) | NO173826C (ko) |
NZ (1) | NZ228895A (ko) |
PT (1) | PT90412B (ko) |
ZA (1) | ZA893003B (ko) |
ZW (1) | ZW4889A1 (ko) |
Families Citing this family (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DK640289D0 (da) * | 1989-12-18 | 1989-12-18 | Ferrosan As | Ny heterocyklisk kemi |
IL98757A (en) * | 1990-07-18 | 1997-01-10 | Novo Nordisk As | Piperidine derivatives their preparation and pharmaceutical compositions containing them |
GB9226111D0 (en) * | 1992-12-15 | 1993-02-10 | Smithkline Beecham Plc | Madicaments |
US6319914B1 (en) | 1993-11-05 | 2001-11-20 | Apollo Biopharmaceuticals, Inc. | Cytoprotective effect of polycyclic phenolic compounds |
US6197833B1 (en) | 1995-07-24 | 2001-03-06 | Apollo Biopharmaceutics, Inc. | Neuroprotective effects of polycyclic phenolic compounds |
US5859001A (en) * | 1996-01-11 | 1999-01-12 | University Of Florida Research Foundation, Inc. | Neuroprotective effects of polycyclic phenolic compounds |
ES2102295B1 (es) * | 1994-03-18 | 1998-04-01 | Ferrer Int | Nuevos compuestos derivados de la n-benzoilmetil-piperidina. |
JP3935502B2 (ja) * | 1995-02-28 | 2007-06-27 | 第一アスビオファーマ株式会社 | アリールピペリジン及びアリールピペラジン誘導体並びにそれらを含む医薬 |
WO1997003661A1 (en) * | 1995-07-24 | 1997-02-06 | University Of Florida Research Foundation, Incorporated | Use of non-estrogen polycyclic phenol compounds for the manufacture of a medicament for conferring neuroprotection to cells |
ES2117557B1 (es) * | 1996-02-29 | 1999-07-01 | Ferrer Int | Nuevo procedimiento de obtencion de (-)-trans -n-p-fluorobenzoilmetil-4-(p-fluorofenil)-3- ((3,4-(metilendioxi)fenoxi ) metil)-piperidina. |
WO1998003172A1 (fr) * | 1996-07-22 | 1998-01-29 | Suntory Limited | Derives arylpiperidinol et arylpiperidine et medicaments les contenant |
AU710594B2 (en) | 1996-07-22 | 1999-09-23 | Asubio Pharma Co., Ltd. | Arylpiperidinol and arylpiperidine derivatives and pharmaceuticals containing the same |
ATE433959T1 (de) | 1997-04-07 | 2009-07-15 | Univ Georgetown | Analoge von kokain |
US6376672B1 (en) * | 1999-04-27 | 2002-04-23 | Hoffmann-La Roche Inc. | Naphthalenylmethoxypiperidines as renin inhibitors |
WO2001032178A1 (en) * | 1999-10-29 | 2001-05-10 | Novo Nordisk A/S | Use of 3,4-substituted piperidines |
WO2004043921A1 (en) * | 2002-11-11 | 2004-05-27 | Natco Pharma Limited | Novel process for the preparation of 4-aryl-3-hydroxymethyl-1-methylpiperidines. |
US20070142389A1 (en) * | 2005-12-20 | 2007-06-21 | Pfizer Inc. | Piperidine derivatives |
KR20180041751A (ko) * | 2015-09-02 | 2018-04-24 | 트레베나, 인코포레이티드. | 6-원 아자-헤테로고리(6-membered aza-heterocyclic) 함유 델타-오피오이드 수용체 조절 화합물, 그 사용 및 제조 방법 |
EP3582779B1 (en) | 2017-02-17 | 2024-04-17 | Trevena, Inc. | 5-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same |
WO2018152286A1 (en) | 2017-02-17 | 2018-08-23 | Trevena, Inc. | 7-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1422263A (en) * | 1973-01-30 | 1976-01-21 | Ferrosan As | 4-phenyl-piperidine compounds |
EP0190496A3 (en) * | 1984-12-13 | 1987-05-27 | Beecham Group Plc | Piperidine derivatives having a gastro-intestinal activity |
ES2058061T3 (es) * | 1985-10-25 | 1994-11-01 | Beecham Group Plc | Derivado de piperidina, su preparacion y su uso como medicamento. |
IE66332B1 (en) * | 1986-11-03 | 1995-12-27 | Novo Nordisk As | Piperidine compounds and their preparation and use |
-
1988
- 1988-04-28 DK DK231088A patent/DK231088D0/da not_active Application Discontinuation
-
1989
- 1989-04-10 IL IL89903A patent/IL89903A0/xx not_active IP Right Cessation
- 1989-04-12 ZW ZW48/89A patent/ZW4889A1/xx unknown
- 1989-04-24 ZA ZA893003A patent/ZA893003B/xx unknown
- 1989-04-24 AU AU33366/89A patent/AU631121B2/en not_active Ceased
- 1989-04-25 EP EP89107481A patent/EP0339579B1/en not_active Expired - Lifetime
- 1989-04-25 ES ES89107481T patent/ES2118708T3/es not_active Expired - Lifetime
- 1989-04-25 AT AT89107481T patent/ATE168375T1/de active
- 1989-04-25 DE DE68928735T patent/DE68928735T2/de not_active Expired - Fee Related
- 1989-04-26 NZ NZ228895A patent/NZ228895A/en unknown
- 1989-04-27 FI FI892012A patent/FI92822C/fi not_active IP Right Cessation
- 1989-04-27 NO NO891762A patent/NO173826C/no unknown
- 1989-04-27 HU HU892019A patent/HUT55387A/hu unknown
- 1989-04-28 JP JP1107889A patent/JP2857414B2/ja not_active Expired - Lifetime
- 1989-04-28 PT PT90412A patent/PT90412B/pt not_active IP Right Cessation
- 1989-04-28 KR KR1019890005606A patent/KR900016175A/ko not_active Application Discontinuation
- 1989-04-28 CN CN89102923A patent/CN1037332A/zh active Pending
Also Published As
Publication number | Publication date |
---|---|
JPH01313461A (ja) | 1989-12-18 |
AU3336689A (en) | 1989-11-02 |
JP2857414B2 (ja) | 1999-02-17 |
NO173826B (no) | 1993-11-01 |
AU631121B2 (en) | 1992-11-19 |
NO891762L (no) | 1989-10-30 |
PT90412B (pt) | 1994-09-30 |
NZ228895A (en) | 1992-05-26 |
FI892012A (fi) | 1989-10-29 |
EP0339579A3 (en) | 1991-12-18 |
ES2118708T3 (es) | 1998-10-01 |
ZW4889A1 (en) | 1989-08-09 |
EP0339579B1 (en) | 1998-07-15 |
PT90412A (pt) | 1989-11-10 |
DE68928735D1 (de) | 1998-08-20 |
DK231088D0 (da) | 1988-04-28 |
FI92822C (fi) | 1995-01-10 |
FI892012A0 (fi) | 1989-04-27 |
NO173826C (no) | 1994-02-09 |
EP0339579A2 (en) | 1989-11-02 |
NO891762D0 (no) | 1989-04-27 |
ATE168375T1 (de) | 1998-08-15 |
FI92822B (fi) | 1994-09-30 |
IL89903A0 (en) | 1989-12-15 |
ZA893003B (en) | 1989-12-27 |
DE68928735T2 (de) | 1998-11-19 |
HUT55387A (en) | 1991-05-28 |
CN1037332A (zh) | 1989-11-22 |
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