KR900001678A - 아미디노 및 구아니디노 유도체 - Google Patents

아미디노 및 구아니디노 유도체 Download PDF

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KR900001678A
KR900001678A KR1019890009896A KR890009896A KR900001678A KR 900001678 A KR900001678 A KR 900001678A KR 1019890009896 A KR1019890009896 A KR 1019890009896A KR 890009896 A KR890009896 A KR 890009896A KR 900001678 A KR900001678 A KR 900001678A
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도네티 알튜로
터코니 마르코
니콜라 마시모
미첼레티 로사마리아
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에스.벤비그나티, 엠.게타니
이스티튜토 드 안젤리 에스.피.에이.
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Abstract

내용 없음

Description

아미디노 및 구아니디노 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (19)

  1. 일반식(I)화합ㅁ루, 이의 토우토머, 광학이성체 및 이의 산부가염.
    상기식에서,
    A는 치환된 벤젠(a) (여기에서, R2는 H; C1-6알킬; 할로겐, 하이드록시, 아세틸로 임의로 치환된 C1-6알콕시, 또는 R2는 C1-6알케닐옥시, C1-6알케닐옥시, 할로겐, 아미노,C1-6알킬 아미노, 니트로, 설포닐아미노이고, n은 0 내지 4이다);
    (여기에서, R3는 H, 할로겐, C1-6알콕시이고, R4는 H,C1-6알킬이다)중에서 선택된 모노-또는 비사이클릭 헤테로사이클이고, X는 -O- 또는 -NH-이고,
    (여기에서 m은 1,2이고 P는 0,1,2이고, g는 0,1,2,3이고, R5는 H,C1-6알킬이다)중에서 선택된 그룹이고, R은 H, 할로겐으로 임의로 치환된 C1-6알킬, NR6R7(여기에서, R6은 H, C1-6알킬, NO2, CN이고, R7은 H,C1-6알킬이다)이고, R1은 H; 할로겐, CN으로 임의로 치환된 C1-6알킬이다.
  2. 제 1 항에 있어서, A가 2-메톡시-4-아미노-5-클로로페닐이고, B는 그룹(a)이고, X는 NH이고, R 및R75제 1 항에서 정의된 바와 같은 일반식(I)화합물.
  3. 제 1 항에 있어서, A가 3-결합된 1H-인돌, 3-결합된 1-메틸인다졸, 3,5-디메틸-페닐 또는 3ㅡ5-디클로페닐이고, B는 그룹(b)이고, X,R 및 R1은 제 1 항에서 정의된 바와 같은 일반식(I)의 화합물.
  4. 제 1 항에 있어서, A는 2-메톡시-4-아미노-5-클로로페닐이고, X는 NH이고, B는 그룹(c)이고, R및 R1은 제 1 항에서 정의된 바와 같은 일반식(I)의 화합물.
  5. [엔도-8-이미노메틸-8-아자비사이클로[3,2,1]옥트-3-일]-3,5-디클로로벤조에이트, 하이드로클로라이드.
  6. [엔도-8-이미노메틸-8-아자비사이클로[3,2,1]옥트-3-일]-1H-인돌-3-카복실레이트, 하이드로클로라이드.
  7. [엔도-8-구아닐-8-아자비사이클로[3,2,1]옥트-3-일]-3,5-디크로로벤조에이트, 하이드로클로라이드.
  8. 제 1 항에 내지 7항에 따라 화합물의 생리학적으로 허용되는 산부가염.
  9. 제 8 항에 있어서, 생리학적으로 허용되는 산이 염산, 황산, 브롬산, 아세트산, 시트로산 또는 타르타르산 임을 특징으로 하는 염.
  10. 일반식(II)의 화합물 또는 이의 산부가염형태인 일반식(II)의 화합물을 비양성자성 용매중에서 0 내지 130℃에서 일반식(III)의 반응성 화합물과 반응시킴을 특징으로 하여, 제 1 항에 따른 일반식(I)의 화합물을 제조하는 방법.
    상기식에서, X,B,R,R1및 A는 제 1 항에서 정의된 바와 같고, Y는 이탈그룹이다.
  11. 제 10항에 있어서, 이탈그룹을 염소, 이미다졸릴, OCOCH3, OCOC2H5, OCOCF3,OH중에서 선택함을 특징으로 하는 방법.
  12. 일반식(V)의 반응성 화합물을 극성용매, 물 또는 이의 혼합물중에서 10 내지 120℃에서 일반식(XIII)의 화합물과 반응시킴을 특징으로 하여, 제 1 항에 따른 일반식(I)의 화합물을 제조하는 방법.
    상기식에서, R,R1,A,X 및 B는 제 1 항에서 정의된 바와 같고, Z는 아탈그룹이다.
  13. 제 12항에 있어서, 이탈그룹을 C1-4알콕시, C1-4알킬티오, 할로겐, 페녹시중에서 선택함을 특징으로 하는 방법.
  14. 일반식(VII)의 아미을 불활성 용매중에서 또는 용매부재하에 -10 내지 80℃에서 일반식(XV)화합물과 반응시킴을 특징으로 하여, R이 H인 제 1 항에 따른 일반식(I)의 화합물을 제조하는 방법.
    상기식에서, R1,A,X 및 B는 제 1 항에서 정의된 바와 같고, ALK는 메틸 또는 에틸그룹니다.
  15. 일반식(XI)의 아민을 극성용매중에서 0 내지 100℃의 온도에서 일반식(XVII)의 화합물과 반응시킴을 특징으로하여, R이 NR6R7인 제 1 항에 따른 일반식(I)의 화합물을 제조하는 방법.
    상기식에서, R6및R7,A,X,B 및 R1은 제 1 항에서 정의된 바와같고, ALK는 제14항에 정의된 바와같다.
  16. 활성성분으로 제 1 항에 따른 일반식(I)의 화합물, 토우토머 또는 생리학적으로 허용되는 산 부가염 하나 이상과 약제학적 담체 또는 부형체를 함유하는 약제학적 조성물.
  17. 제16항에 있어서, 5-HT3약제로서의 약제학적 조성물.
  18. 제16항에 있어서, 화학요법 및 구역질 및 구토를 야기하는 방사선으로 고생하는 환자 또는 지연된 위의 배출시간, 위장운동 불규칙 및 특히 소화불량, 고창, 식도 역튜, 자극성 장 증세 및 이포키네아사(ipokinesia)로 고생하는 환자를 치료하는데 사용하기 위한 약제학적 조성물.
  19. 제16항에 있어서, 운동병, 편두통, 집락 두통, 불안 및 정신병으로 고생하는 환자치료에 사용하기 위한 약제학적 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890009896A 1988-07-12 1989-07-12 아미디노 및 구아니디노 유도체 KR900001678A (ko)

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IT8821330A IT1226389B (it) 1988-07-12 1988-07-12 Nuovi derivati ammidinici e guanidinici

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GB8928837D0 (en) * 1989-12-21 1990-02-28 Beecham Group Plc Pharmaceuticals
AU671071B2 (en) * 1990-08-30 1996-08-15 State of Oregon, acting by and through The Oregon State Board of Higher Education, acting for and on behalf of The Oregon Health Sciences University, Portland, Oregon, and The University of Oregon, Eugene, Oregon, Johnson Hall, Substituted amidines having high binding to the sigma receptor and the use thereof
GB9214184D0 (en) * 1992-07-03 1992-08-12 Smithkline Beecham Plc Pharmaceuticals
TW200533348A (en) * 2004-02-18 2005-10-16 Theravance Inc Indazole-carboxamide compounds as 5-ht4 receptor agonists
US8309575B2 (en) 2004-04-07 2012-11-13 Theravance, Inc. Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
US7728006B2 (en) * 2004-04-07 2010-06-01 Theravance, Inc. Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
TWI351282B (en) 2004-04-07 2011-11-01 Theravance Inc Quinolinone-carboxamide compounds as 5-ht4 recepto
WO2006052640A1 (en) * 2004-11-05 2006-05-18 Theravance, Inc. 5-ht4 receptor agonist compounds
ES2327142T3 (es) * 2004-11-05 2009-10-26 Theravance, Inc. Compuestos de quinolinona-carboxamida.
NZ555180A (en) * 2004-12-22 2010-09-30 Theravance Inc Indazole-carboxamide compounds useful as 5-HT4 receptor agonists
JP2008530225A (ja) * 2005-02-17 2008-08-07 セラヴァンス， インコーポレーテッド インダゾール−カルボキサミド化合物の結晶型
NZ560828A (en) * 2005-03-02 2011-01-28 Theravance Inc Quinolinone compounds as 5-HT4 receptor agonists
JOP20130213B1 (ar) 2012-07-17 2021-08-17 Takeda Pharmaceuticals Co معارضات لمستقبلht3-5
WO2014049471A1 (en) * 2012-09-29 2014-04-03 Mahesh Kandula Compositions and methods for the treatment of ventricular arrhythmias and cardiovascular diseases
PL3201203T3 (pl) * 2014-09-29 2021-11-22 Takeda Pharmaceutical Company Limited Krystaliczna postać 1-(1-metylo-1h-pirazol-4-ilo)-n-((1r,5s,7s)-9-metylo-3-oksa-9-azabicyklo[3.3.1]nonan-7-ylo)-1h-indolo-3-karboksyamidu

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IT1231238B (it) * 1987-09-21 1991-11-26 Angeli Inst Spa Derivati ammidinici
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HUT52041A (en) 1990-06-28
CZ424289A3 (en) 1994-12-15
AU622918B2 (en) 1992-04-30
IT8821330A0 (it) 1988-07-12
FI892993A (fi) 1990-01-13
NO892820L (no) 1990-01-15
IT1226389B (it) 1991-01-15
EP0351385A3 (en) 1991-11-06
DD284013A5 (de) 1990-10-31
NZ229889A (en) 1991-07-26
RU1776255C (ru) 1992-11-15
DK341589A (da) 1990-01-13
AU3803889A (en) 1990-01-25
IL90911A (en) 1994-05-30
PL160812B1 (pl) 1993-04-30
EP0351385A2 (en) 1990-01-17
MX16754A (es) 1993-10-01
US5047410A (en) 1991-09-10
NO173093B (no) 1993-07-19
PT91122A (pt) 1990-02-08
FI892993A0 (fi) 1989-06-19
DK341589D0 (da) 1989-07-11
IL90911A0 (en) 1990-02-09
NO173093C (no) 1993-10-27
JPH0285253A (ja) 1990-03-26
PT91122B (pt) 1995-01-31
PL161071B1 (pl) 1993-05-31
ZA895217B (en) 1991-03-27
YU138889A (en) 1991-10-31

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