KR950000691A - 피페리딘 및 피페라진 - Google Patents

피페리딘 및 피페라진 Download PDF

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KR950000691A
KR950000691A KR1019940014712A KR19940014712A KR950000691A KR 950000691 A KR950000691 A KR 950000691A KR 1019940014712 A KR1019940014712 A KR 1019940014712A KR 19940014712 A KR19940014712 A KR 19940014712A KR 950000691 A KR950000691 A KR 950000691A
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formula
piperidine
compound
dimethoxyphenyl
ethyl
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KR1019940014712A
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바움가르트 만프레드
루에스 잉게
밍크 클라우스-옷토
바이어 노베르트
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위르겐 호르만, 라인하르트 슈틀러
메르크 파텐트 게젤샤프트 미트 베쉬랭크터 하프퉁
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Publication of KR950000691A publication Critical patent/KR950000691A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/06—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 carbon chain containing only aliphatic carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Quinoline Compounds (AREA)
  • Furan Compounds (AREA)
  • Pyrane Compounds (AREA)

Abstract

하기 일반식(Ⅰ)의 피페리딘 및 피페라진 유도체 및 그의 생리학적으로 허용가능한 염은 항부정맥 효과를 나타낸다 :
상기식에서, R1및 R2는 H 또는 A이고, R3,R4및 R5는 각각의 경우 서로 독립적으로 H,Hal,OH,OA,OAc,NO2,NH2,NHAc,NHSO2A 또는 CN이거나, 또는 R3및 R4는 함께 또한 －O－(CH2)m－O－이고, n은 0,1 또는 2이고, X는 만약 n이 0 또는 2이면, O 또는 CH2이거나, 또는 만약 n이 1이면, CH2,NH,NA 또는 NAc이고, Y는 CH 또는 N이고, m은 1 또는 2이고, Hal은 F,Cl,Br 또는 I이고, A는 탄소수 1 내지 6의 알킬이며, Ac는 탄소수 14 내지 8의 알카노일, 탄소수 1 내지 10의 아르알카노일 또는 탄소수 7 내지 11의 아로일이다.

Description

피페리딘 및 피페라진
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (8)

  1. 하기 일반식(Ⅰ)의 피페리딘 및 피페라진 유도체 및 그의 약학적으로 허용가능한 염 :
    상기식에서, R1및 R2는 H 또는 A이고, R3,R4및 R5는 각각의 경우 서로 독립적으로 H,Hal,OH,OA,OAc,NO2,NH2,NHAc,NHSO2A 또는 CN이거나, 또는 R3및 R4는 함께 또한 －O－(CH2)m－O－이고, n은 0,1 또는 2이고, X는 만약 n이 0 또는 2이면, O 또는 CH2이거나, 또는 만약 n이 1이면, CH2,NH,NA 또는 NAc이고, Y는 CH 또는 N이고, m은 1 또는 2이고, Hal은 F,Cl,Br 또는 I이고, A는 탄소수 1 내지 6의 알킬이며, Ac는 탄소수 14 내지 8의 알카노일, 탄소수 1 내지 10의 아르알카노일 또는 탄소수 7 내지 11의 아로일이다.
  2. 제 1 항에 따라는 일반식(Ⅰ) 화합물의 거울상이성체.
  3. (a) 1－[2－(6,7,8,9－테트라하이드로－5H－벤조사이클로헵텐－5－일)에틸]－4－(3,4－디메톡시페닐)피페리딘; (b) 5－[2－(4－(3,4－디메톡시페닐)－1－피페리디닐)－에틸]－2,3,4,5－테트라하이드로－1－벤조옥세핀; (c) 3－[2－(4－(3,4－디메톡시페닐)－1－피페리디닐)－에틸]－2,3－디하이드로벤조푸란; (d) 1－[2－(테트랄린－1－일)－에틸]－4,(3,4－디메톡시페닐)피페리딘; (e) 1－[2－(인단－1－일)－에틸]－4－(3,4－디메톡시페닐)피페리딘 ; (f) 1－[2－(1,2,3,4－테트라하이드로퀴놀린－4－일)에틸]－4－(3,4－디메톡시페닐)피페리딘 및 그의 염.
  4. 하기 일반식(Ⅱ)의 화합물을 하기 일반식(Ⅲ)의 화합물과 반응시키거나, 또는 하나 이상의 CH2그룹 대신에 하나 이상의 환원성 그룹을 가짐을 제외하고는, 그 자체로 일반식(Ⅰ)에 상응하는 화합물을 환원에 의해 일반식(Ⅰ)의 화합물로 전환시키고/시키거나, 일반식(Ⅰ)의 화합물에서 각각 하나 이상의 라디칼 R3, R4및/또는 R5또는 X(X＝NH일 경우)를 각각 다른 라디칼 R3, R4및/또는 R5또는 X로 전환시키고/시키거나, 일반식(Ⅰ)의 염기성 화합물을 산 처리에 의해 그의 생리학적으로 허용가능한 산 부가 염중의 하나로 전환시킴을 특징으로 하는, 제 1 항에 따르는 일반식(Ⅰ)의 피페리딘 및 피페라진 유도체의 제조방법;
    상기식에서, Z는 Cl,Br,OH 또는 반응식으로, 작용기가 변형된 OH 그룹이고, R1,R2,R3,R4,R5,X,Y 및 n은 제 1 항에 언급된 정의와 동일하다.
  5. 일반식(Ⅰ)의 화합물 및/또는 그의 생리학적으로 허용가능한 염중의 하나를 하나 이상의 고체, 액체 또는 반고체 부형제 또는 보조제와 함께 적합한 투여형으로 제공함을 특징으로 하는, 약학 제제의 제조방법.
  6. 하나 이상의 일반식(Ⅰ)의 화합물 및/또는 그의 생리학적으로 허용가능한 염중의 하나를 함유함을 특징으로 하는, 약학 제제.
  7. 약물을 제조하기 위한, 제 1 항에 따르는 일반식(Ⅰ)의 화합물 또는 그의 생리학적으로 허용가능한 염의 용도.
  8. 질병 치료에 있어서의 제 1 항에 따르는 일반식(Ⅰ)의 화합물 또는 그의 생리학적으로 허용가능한 염의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940014712A 1993-06-26 1994-06-25 피페리딘 및 피페라진 KR950000691A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE4321366A DE4321366A1 (de) 1993-06-26 1993-06-26 Piperidine und Piperazine
DEP4321366.9 1993-06-26

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KR950000691A true KR950000691A (ko) 1995-01-03

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US (1) US5495022A (ko)
EP (1) EP0634398A1 (ko)
JP (1) JPH0725851A (ko)
KR (1) KR950000691A (ko)
CN (1) CN1102649A (ko)
AU (1) AU6487294A (ko)
CA (1) CA2126719A1 (ko)
CZ (1) CZ155994A3 (ko)
DE (1) DE4321366A1 (ko)
HU (1) HUT70834A (ko)
NO (1) NO942411L (ko)
PL (1) PL303978A1 (ko)
RU (1) RU94022271A (ko)
SK (1) SK77494A3 (ko)
TW (1) TW293818B (ko)
ZA (1) ZA944573B (ko)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU694212B2 (en) * 1994-04-28 1998-07-16 Merck Sharp & Dohme Limited Benzofuran derivatives as d4 receptor antagonists
FR2734819B1 (fr) * 1995-05-31 1997-07-04 Adir Nouveaux composes de la piperazine, de la piperidine et de la 1,2,5,6-tetrahydropyridine, leur procede de preparation et les compositions pharmaceutiques les contenant
WO1997013512A1 (en) * 1995-10-10 1997-04-17 Eli Lilly And Company N-[2-substituted-3-(2-aminoethyl)-1h-indol-5-yl]-amides: new 5-ht1f agonists
GB9521347D0 (en) * 1995-10-18 1995-12-20 Merck Sharp & Dohme Therapeutic agents
GB9912410D0 (en) * 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
JP6498672B2 (ja) * 2013-12-20 2019-04-10 エステベ ファーマシューティカルズ，ソシエダッド アノニマＥｓｔｅｖｅ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｓ．Ａ． 疼痛に対して多重モードの活性を有するピペリジン化合物

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4302589A (en) * 1980-05-08 1981-11-24 American Cyanamid Company Cis-mono and disubstituted-2-methyl-3-[(piperazinyl) and (piperidino)ethyl]indolines, intermediates for their preparation and methods of preparation
FR2618437B1 (fr) * 1987-07-23 1989-11-17 Rhone Poulenc Sante Nouveaux derives du benzopyranne, leur preparation et les medicaments qui les contiennent
FR2670491B1 (fr) * 1990-12-14 1993-02-05 Adir Nouvelles piperazines 1,4-disubstituees, leur procede de preparation et les compositions pharmaceutiques les renfermant.

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PL303978A1 (en) 1995-01-09
ZA944573B (en) 1995-02-14
US5495022A (en) 1996-02-27
DE4321366A1 (de) 1995-01-05
CN1102649A (zh) 1995-05-17
HU9401914D0 (en) 1994-09-28
EP0634398A1 (de) 1995-01-18
JPH0725851A (ja) 1995-01-27
HUT70834A (en) 1995-11-28
NO942411L (no) 1994-12-27
TW293818B (ko) 1996-12-21
CA2126719A1 (en) 1994-12-27
SK77494A3 (en) 1995-07-11
RU94022271A (ru) 1996-04-20
CZ155994A3 (en) 1995-10-18
AU6487294A (en) 1995-01-05
NO942411D0 (ko) 1994-06-24

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