KR870010015A - 페닐-피페라진 유도체 및 그의 제조방법 - Google Patents
페닐-피페라진 유도체 및 그의 제조방법 Download PDFInfo
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- KR870010015A KR870010015A KR870003727A KR870003727A KR870010015A KR 870010015 A KR870010015 A KR 870010015A KR 870003727 A KR870003727 A KR 870003727A KR 870003727 A KR870003727 A KR 870003727A KR 870010015 A KR870010015 A KR 870010015A
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/88—Nitrogen atoms, e.g. allantoin
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Cardiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (18)
- (i)일반식(Ⅱ)의 화합물을a)일반식 R4SO2C1(여기에서, R4C1-C4알킬 또는 C3-C7사이클로알킬이다)의 설포닐클로라이드 또는 일반식(R4SO2)2O(여기에서, R4는 상기에서 정의한 의미와 같다)의 설폰산 무수물과 반응시켜 R이 R3SO2NH-이며 R3은 R4에 대해 상기 정의한 바와 같은 일반식(Ⅰ)의 화합물을 수득하거나,b)일반식R1R2NSO2C1(여기에서, R1및 R2중 하나 또는 둘다는 C1-C4알킬이다)의 설파모일 클로라이드와 반응시켜 R이 R3SO2NH-이며 R3는 NR1R|2인 일반식(Ⅰ)의 화합물을 수득하거나,c)H2NSO2NH2와 반응시켜 R이 R3SO2NH-이며 R3은NH2인 일반식(Ⅰ)의 화합물을 수득하거나,d)일반식 R4COC1(여기에서 R4는 상기a)에서 정의한 바와 같다)의 아실할라이드 또는 일반식(R4CO)2O(여기에서, R4는 상기 a)에서 정의한 바와 같다)의 무수물과 반응시켜 R이 R3CONH-이며 R3은 R4에대해 정의한 바와 같은 일반식(Ⅰ)의 화합물을 수득하거나,e)C1-C4알킬 이소시아네이트와 반응시켜 R이 R3CONH-이며 R3은 NH(C1-C4알킬)인 일반식(Ⅰ)의 화합물을 수득하거나,f)일반식(C1-C4알킬)2NCOC1의 화합물과 반응시켜 R이 R1R2NCONH-이며R1및 R2는 각각 C1-C4알킬인 일반식(Ⅰ)의 화합물을 수득하거나,g)수성 산성 조건하에서 알칼리 금속 시아네이트와 반응시켜 R이 H2NCONH-인 일반식(Ⅰ)의 화합물을 수득하거나:(ⅱ)일반식(Ⅳ)의 4-헤테로사이클릴-피페라진을 일반식(ⅩⅠ)의 4-치환된-할로벤젠과 반응시키거나;(ⅲ)일반식(ⅩⅢ)의 할로-피리딘과 일반식(ⅩⅡ)의 4-페닐피페라진을 반응시켜 Het가 피리딜 또는 알킬-치환된 피리딜인 일반식(Ⅰ)의 화합물을 수득하거나;(ⅳ)일반식(ⅩⅣ)의 화합물을 환원시켜 Het가 아미노-치환된 피리딜인 일반식(Ⅰ)의 화합물을 수득하거나;(ⅴ)일반식(ⅩⅤ)의 화합물을 온화한 조건하에서 가수분해시켜 R이 H2NCO-인 일반식(Ⅰ)의 화합물을수득하거나, 격렬한 조건하에서 가수분해시켜 4-카복실산을 수득하고, 계속해서 산 클로라이드 또는 이미다졸리드로 전환시킨 다음, 일반식 R1R2NH(여기에서, R1및 R2중 하나 또는 둘다는 C1-C|4알킬이다)의 아민과 반응시켜 R이 R1R2NCO-의 일반식(Ⅰ)의 화합물을 수득하거나;(ⅵ)일반식(ⅩⅥ)의 화합물을 가수분해시켜 Het가 아미노-치환된 피리딜인 일반식(Ⅰ)의 화합물을 수득함을 특징으로 하여, 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용되는 그의 염을 제조하는 방법.상기식에서,R은 R3SO2NH-, R3CONH-, R1R2NSO2-또는 R1R2NCO-이고,R1및 R2는 각각 독립적인 H 또는 C1-C4알킬이고,R3은 C1-C4알킬, C3-C7사이클로알킬 또는 NR1R2이며,Het는 각각 독립적으로 C1-C4알킬 및 NH2로 부터 선택된 하나 또는 그 이상의 치환체에 의해 임의로 치환된 2,3 또는 4-피리딜이거나, 하나 또는 그 이상의 C1-C4알킬 그룹에 의해 임의로 치환된 2-아미다졸릴이고,n은 0 또는 1이며,X는 할로이고,R5는 H 또는 C1-C4알킬이며,R6은 C1-C4알킬이다.
- 제1(ⅰ)(a)항에 있어서, 다음 일반식의 화합물을 메탄설포닐 클로라이드와 반응시켜 R이 CH3SO2NH-인 제1항에서 정의한 일반식(Ⅰ)의 화합물을 수득하는 방법.
- 제2항에 있어서, Het가 4-페리딜인 방법.
- 제2항에 있어서, Het가 2-메틸-4-피리딜인 방법.
- 제1(ⅳ)항에 있어서, R 이 CH3SO2NH-인 방법.
- 제5항에 있어서, N-{4-[4-(4-니트로피리드-2-일)피페라진-1-일]페닐}메탄설폰아미드를 환원시켜 N-{4-[4-(4-아미노피리드-2-일)피페라진-1-일]페닐}메탄설폰아미드를 수득하는 방법.
- 제1(ⅵ)항에 있어서, R이 CH3SO2NH-인 방법.
- 제1항에서 정의한 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용되는 그의 염을 약제학적으로 허용되는 희석제 또는 담체와 혼합시킴을 특징으로 하여, 약제학적 조성물을 제조하는 방법.
- 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용되는 그의 염.상기식에서,R은 R3SO2NH-, R3CONH-, R1R2NSO2-또는 R1R2NCO-이고,R1및 R2는 각각 독립적인 H 또는 C1-C4알킬이고,R3은 C1-C4알킬, C3-C7사이클로알킬 또는 NR|1R2이며,Het는 각각 독립적으로 C1-C4알킬 및 NH2로 부터 선택된 하나 또는 그 이상의 치환체에 의해 임의로 치환된 2,3 또는 4-피리딜이거나, 하나 또는 그 이상의 C1-C4알킬 그룹에 의해 임의로 치환된 2-아미다졸릴이다.
- 제9항에 있어서, R은 CH3SO2NH-인 화합물.
- 제9항 또는 제10항에 있어서, Het가 CH3도는 NH2에 의해 임의로 치환된 2 또는 4-페리딜인 화합물.
- 제9항에 있어서, R이 CH3SO2NH-이며 Het는 4-피리딜인 화합물.
- 제9항에 있어서, R이 CH3SO2NH-이며 Het는 2-메틸-4-피리딜인 화합물.
- 제9항에 있어서, R이 CH3SO2NH-이며 Het는 4-아미노-2-피리딜인 화합물.
- 제9항 내지 13항 중의 어느 한 항에 청구된 일반식(Ⅰ)의 화합물 또는 그의 약제학적으로 허용되는 염과 약제학적으로 허용되는 희석제 또는 담체를 함유하는 약제학적 조성물.
- 약물, 특히 부정맥 치료제로 사용하기 위한 제9항 내지 13항중의 어느 한항에 청구된 일반식(Ⅰ)화합물 또는 약제학적으로 허용되는 그의 염.
- 심부정맥의 예방 또는 치료용 약물의 제조를 위한 제9항 내지 13항 중의 어느 한 항에 청구된 일반식(Ⅰ) 화합물 또는 약제학적으로 허용되는 그의 염의 용도
- 다음 일반식의 화합물.상기식에서, R은 제1항에서 정의한 바와 같으며,Het'은 NO2에 의해 치환된 2,3 또는 4-피리딜, 또는 기의 N-옥사이드이거나, -CONHNH2또는 -NHCO2(C1-C4알킬)에 의해 치의된 2,3 또는 4-피리딜이다.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB868609630A GB8609630D0 (en) | 1986-04-19 | 1986-04-19 | Anti-arrhythmia agents |
GB8609630 | 1986-04-19 |
Publications (1)
Publication Number | Publication Date |
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KR870010015A true KR870010015A (ko) | 1987-11-30 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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KR870003727A KR870010015A (ko) | 1986-04-19 | 1987-04-18 | 페닐-피페라진 유도체 및 그의 제조방법 |
Country Status (18)
Country | Link |
---|---|
US (1) | US4788196A (ko) |
EP (1) | EP0244115A3 (ko) |
JP (1) | JPS62255480A (ko) |
KR (1) | KR870010015A (ko) |
CN (1) | CN87102873A (ko) |
AU (1) | AU577218B2 (ko) |
DD (1) | DD261787A5 (ko) |
DK (1) | DK195587A (ko) |
FI (1) | FI871694A (ko) |
GB (1) | GB8609630D0 (ko) |
HU (1) | HUT44027A (ko) |
IL (1) | IL82221A0 (ko) |
MY (1) | MY101208A (ko) |
NO (1) | NO871594L (ko) |
PL (1) | PL265207A1 (ko) |
PT (1) | PT84695B (ko) |
YU (1) | YU70787A (ko) |
ZA (1) | ZA872744B (ko) |
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BR9711135A (pt) * | 1996-08-14 | 1999-08-17 | Zeneca Ltd | Composto composi-Æo farmac-utica utiliza-Æo de um composto e processos para prepara-Æo de um composto e para inibi-Æo de Äxido-equaleno ciclase num animal de sangue quente requerendo um tal tratamento |
UA56197C2 (uk) | 1996-11-08 | 2003-05-15 | Зенека Лімітед | Гетероциклічні похідні |
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US6083991A (en) | 1997-06-04 | 2000-07-04 | University Of Florida Research Foundation, Inc. | Anti-arrhythmic composition and methods of treatment |
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BE485737A (ko) * | 1947-11-12 | |||
US2606906A (en) * | 1948-10-14 | 1952-08-12 | American Cyanamid Co | 1-(2-pyridyl) piperazine and process of preparing same |
DE942029C (de) * | 1951-06-22 | 1956-04-26 | American Cyanamid Co | Verfahren zur Herstellung von neuen, in 1-Stellung substituierten 4-Aminopiperazinderivaten |
US3306903A (en) * | 1965-10-07 | 1967-02-28 | Council Scient Ind Res | 1-aminopyridyl-4-(phenyl or pyridyl)-piperazines and intermediates |
US4287195A (en) * | 1978-07-14 | 1981-09-01 | Janssen Pharmaceutica, N.V. | Heterocyclic derivatives of [4-(piperazin-1-yl-phenyloxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazoles and 1H-1,2,4-triazoles |
US4255575A (en) * | 1979-05-04 | 1981-03-10 | Richardson-Merrell Inc. | 2-Hydroxy-5-(1-hydroxy-2-piperazinylethyl)-benzoic acid derivatives |
AU2108283A (en) * | 1979-07-13 | 1984-03-29 | Dr. Karl Thomae Gmbh | 2-amino benzoic acid derivatives |
US4613598A (en) * | 1984-03-13 | 1986-09-23 | Mitsubishi Chemical Industries Limited | Piperazine derivatives and their acid addition salts |
US4544654A (en) * | 1984-03-20 | 1985-10-01 | Schering A.G. | Substituted sulfonamidobenzamides, antiarrhythmic agents and compositions thereof |
US4639524A (en) * | 1984-07-09 | 1987-01-27 | G. D. Searle & Co. | Monobasic disobutamide derivatives |
DE3428526A1 (de) * | 1984-08-02 | 1986-02-13 | Boehringer Mannheim Gmbh, 6800 Mannheim | Neue aminoalkohole, verfahren zu deren herstellung sowie diese verbindung enthaltende arzneimittel |
US4596827A (en) * | 1984-10-15 | 1986-06-24 | Eli Lilly And Company | Alkylsulfonamidophenylalkylamine compounds used for treating arrhythmia |
US4569801A (en) * | 1984-10-15 | 1986-02-11 | Eli Lilly And Company | Alkylsulfonamidophenylalkylamines |
GB8603120D0 (en) * | 1986-02-07 | 1986-03-12 | Pfizer Ltd | Anti-dysrhythmia agents |
AU7642187A (en) * | 1986-07-01 | 1988-01-29 | Maude, A.E. | Impregnation process and apparatus with a vacuum pump valve control system |
-
1986
- 1986-04-19 GB GB868609630A patent/GB8609630D0/en active Pending
-
1987
- 1987-04-14 EP EP87303234A patent/EP0244115A3/en not_active Ceased
- 1987-04-15 DK DK195587A patent/DK195587A/da not_active Application Discontinuation
- 1987-04-15 NO NO871594A patent/NO871594L/no unknown
- 1987-04-15 CN CN198787102873A patent/CN87102873A/zh active Pending
- 1987-04-16 FI FI871694A patent/FI871694A/fi not_active Application Discontinuation
- 1987-04-16 PL PL1987265207A patent/PL265207A1/xx unknown
- 1987-04-16 DD DD87301901A patent/DD261787A5/de unknown
- 1987-04-16 AU AU71731/87A patent/AU577218B2/en not_active Expired - Fee Related
- 1987-04-16 PT PT84695A patent/PT84695B/pt unknown
- 1987-04-16 ZA ZA872744A patent/ZA872744B/xx unknown
- 1987-04-16 IL IL82221A patent/IL82221A0/xx unknown
- 1987-04-17 US US07/039,508 patent/US4788196A/en not_active Expired - Lifetime
- 1987-04-17 MY MYPI87000499A patent/MY101208A/en unknown
- 1987-04-17 YU YU00707/87A patent/YU70787A/xx unknown
- 1987-04-17 HU HU871713A patent/HUT44027A/hu unknown
- 1987-04-18 KR KR870003727A patent/KR870010015A/ko not_active Application Discontinuation
- 1987-04-20 JP JP62097245A patent/JPS62255480A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
PT84695B (en) | 1989-05-23 |
DK195587D0 (da) | 1987-04-15 |
AU577218B2 (en) | 1988-09-15 |
HUT44027A (en) | 1988-01-28 |
FI871694A (fi) | 1987-10-20 |
IL82221A0 (en) | 1987-10-30 |
PL265207A1 (en) | 1988-07-21 |
AU7173187A (en) | 1987-11-05 |
DK195587A (da) | 1987-10-20 |
EP0244115A3 (en) | 1988-10-05 |
GB8609630D0 (en) | 1986-05-21 |
YU70787A (en) | 1988-10-31 |
US4788196A (en) | 1988-11-29 |
DD261787A5 (de) | 1988-11-09 |
FI871694A0 (fi) | 1987-04-16 |
MY101208A (en) | 1991-08-17 |
NO871594D0 (no) | 1987-04-15 |
EP0244115A2 (en) | 1987-11-04 |
JPS62255480A (ja) | 1987-11-07 |
NO871594L (no) | 1987-10-20 |
PT84695A (en) | 1987-05-01 |
CN87102873A (zh) | 1987-10-28 |
ZA872744B (en) | 1988-11-30 |
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E902 | Notification of reason for refusal | ||
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