KR880001598A - 사이클로알킬-치환 4- 피리딜 유도체 및 이의 제조방법 - Google Patents

사이클로알킬-치환 4- 피리딜 유도체 및 이의 제조방법 Download PDF

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KR880001598A
KR880001598A KR1019870007741A KR870007741A KR880001598A KR 880001598 A KR880001598 A KR 880001598A KR 1019870007741 A KR1019870007741 A KR 1019870007741A KR 870007741 A KR870007741 A KR 870007741A KR 880001598 A KR880001598 A KR 880001598A
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cyclohexyl
dimethylpyrid
methylpyrid
ethyl
formula
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KR1019870007741A
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크루그놀라 안젤로
디 살레 엔리코
롬바르디 파올로
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비토리노 페라리오
파미탈리아 카를로 에르바 에스.피.에이.
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Priority claimed from GB868617596A external-priority patent/GB8617596D0/en
Priority claimed from GB868628029A external-priority patent/GB8628029D0/en
Application filed by 비토리노 페라리오, 파미탈리아 카를로 에르바 에스.피.에이. filed Critical 비토리노 페라리오
Publication of KR880001598A publication Critical patent/KR880001598A/ko

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Abstract

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Description

사이클로알킬-치환 4-피리딜 유도체 및 이의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 하기 일반식(Ⅰ)의 사이클로알킬-치환4-피리딜 유도체 및 약제학적으로 허용되는 이의 염.
    상기식에서,
    R은 C1-C4알킬이고 ;
    R1및 R2는 각기 독립적으로 수소또는 C1-C4알킬이며 ;
    n은 1내지 5의 정수이고 ;
    (a)A는이고 B는 -0-, -NH- 또는 -CH2- 이거나;
    (b)A는 -CH2-이고 B는 -0-, -NH-, -CH2- 또는 C=0이거나 ;
    (c)A는 -0- 이고 B는또는 -CH2- 이거나 ;
    (d)A는 -NH-이고 B는또는 -CH2- DLEK.
  2. 제 1항에 있어서, R의 C1-C4알킬이며;
    R1및 R2가 각기 독립적으로, 수소 또는 C1-C4알킬이며:
    n이 1내지 5의 정수이며 : A 가또는 -CH2- 이고, B가 독립적으로 -0-, -NH- 또는 -CH2- 인 일반식(Ⅰ)의 사이클로 알킬 치환된 4-피리딜 유도체 및 약제학적으로 허용되는 이의 염.
  3. 제 1항 또는 2항에 있어서, 일반식(Ⅰ)의 유도체가 일반식(Ia)의 에난티오머의 화합물.
    상기식에서,
    R, R1, R2, n, A 및 B는 제 1항 또는 2항에 정의한 바와 같다.
  4. 제 1항 내지 3항중 어느 한 항에 있어서, R1및 R2가 둘다 수소 또는 둘다 메틸이거나, 이중 하나가 수소이고 나머지가 메틸이며, n이 3 또는 4인 화합물.
  5. 사이클로 헥실(2-(4'-피리딜)프로피오네이트;
    사이클로 헥실(2-(2'-메틸피리드-4'-일)프로피오네이트;
    사이클로 헥실(2-(3'-메틸피리드-4'-일)프로피오네이트;
    사이클로 헥실(2-(2',6'-티메틸피리드-4'-일)프로피오네이트;
    사이클로 헥실(2-(2',5'-티메틸피리드-4'-일)프로피오네이트;
    사이클로 헥실(2-(2',3'-티메틸피리드-4'-일)프로피오네이트;
    사이클로 헥실(2-(2',5'-티메틸피리드-4'-일)프로피오네이트;
    N-사이클로헥실-2-(4'-피리딜)프로판아미드 ;
    N-사이클로헥실-2-(2'-메틸피리드-4'-일)프로판아미드 ;
    N-사이클로헥실-2-(3'-메틸피리드-4'-일)프로판아미드 ;
    N-사이클로헥실-2-(2',6'-디메틸피리드-4'-일)프로판아미드 ;
    N-사이클로헥실-2-(2',5'-디메틸피리드-4'-일)프로판아미드 ;
    N-사이클로헥실-2-(2',3'-디메틸피리드-4'-일)프로판아미드 ;
    N-사이클로헥실-2-(2',5'-디메틸피리드-4'-일)프로판아미드 ;
    2-(4'-피리딜)프로필사이클로헥실에테르 ;
    2-(2'-메틸피리드-4'-일)프로필사이클로헥실 에테르 ;
    2-(3'-메틸피리드-4'-일)프로필사이클로헥실 에테르 ;
    2-(2',6'-디메틸피리드-4'-일)프로필사이클로헥실 에테르 ;
    2-(2',5'-디메틸피리드-4'-일)프로필사이클로헥실 에테르 ;
    2-(2',3'-디메틸피리드-4'-일)프로필사이클로헥실 에테르 ;
    2-(2',3'-디메틸피리드-4'-일)프로필사이클로헥실 에테르 ;
    2-(2',5'-디메틸피리드-4'-일)프로필사이클로헥실 에테르 ;
    N-사이클로헥실-2-(4'-피리딜)프로필아민 ;
    N-사이클로헥실-2-(2'-메틸피리드-4'-일)프로필아민 ;
    N-사이클로헥실-2-(3'-메틸피리드-4'-일)프로필아민 ;
    N-사이클로헥실-2-(2',6'-디메틸피리드-4'-일)프로필아민 ;
    N-사이클로헥실-2-(2',5'-디메틸피리드-4'-일)프로필아민 ;
    N-사이클로헥실-2-(2',3'-디메틸피리드-4'-일)프로필아민 ;
    N-사이클로헥실-2-(2',5'-디메틸피리드-4'-일)프로필아민 ;
    1-사이클로헥실-3-(4'-피리딜)-2-부탄온 ;
    1-사이클로헥실-3-(2'-메틸피리드-4'-일)-2-부탄온 ;
    1-사이클로헥실-3-(3'-메틸피리드-4'-일)-2-부탄온 ;
    1-사이클로헥실-3-(2',6'-디메틸피리드-4'-일)-2-부탄온 ;
    1-사이클로헥실-3-(2',5'-디메틸피리드-4'-일)-2-부탄온 ;
    1-사이클로헥실-3-(2',3'-디메틸피리드-4'-일)-2-부탄온 ;
    1-사이클로헥실-3-(3',5'-디메틸피리드-4'-일)-2-부탄온 ;
    1-사이클로헥실-3-(4'-피리딜)부탄 ;
    1-사이클로헥실-3-(2',-메틸피리드-4'-일)부탄 ;
    1-사이클로헥실-3-(3',-메틸피리드-4'-일)부탄 ;
    1-사이클로헥실-3-(2',6'-디메틸피리드-4'-일)부탄 ;
    1-사이클로헥실-3-(2',5'-디메틸피리드-4'-일)부탄 ;
    1-사이클로헥실-3-(2',3'-디메틸피리드-4'-일)부탄 ;
    1-사이클로헥실-3-(3',5'-디메틸피리드-4'-일)부탄 ;
    1-(4'-피리딜)에틸 사이클로헥산카복실레이트 ;
    1-(2'-메틸피리드-4'-일)에틸 사이클로헥산카복실레이트 ;
    1-(3'-메틸피리드-4'-일)에틸 사이클로헥산카복실레이트 ;
    1-(2',6'-디메틸피리드-4'-일)에틸 사이클로헥산카복실레이트 ;
    1-(2',5'-디메틸피리드-4'-일)에틸 사이클로헥산카복실레이트 ;
    1-(2',3'-디메틸피리드-4'-일)에틸 사이클로헥산카복실레이트 ;
    1-(3',5'-디메틸피리드-4'-일)에틸 사이클로헥산카복실레이트 ;
    1-(4'-피리딜)에틸 사이클로헥실메틸에테르 ;
    1-(2'메틸피리드-4'-일)에틸 사이클로헥실메틸 에테르 ;
    1-(3'메틸피리드-4'-일)에틸 사이클로헥실메틸 에테르 ;
    1-(2',6'-디메틸피리드-4'-일)에틸 사이클로헥실메틸 에테르 ;
    1-(2',5'-디메틸피리드-4'-일)에틸 사이클로헥실메틸 에테르 ;
    1-(2',3'-디메틸피리드-4'-일)에틸 사이클로헥실메틸 에테르 ;
    1-(3',4'-디메틸피리드-4'-일)에틸 사이클로헥실메틸 에테르 ;
    N-[1-4'-피리딜)에틸]사이클로헥산카복시아미드 ;
    N-[1-(2'-메틸피리드-4'-일)에틸]사이클로헥산카복시아미드 ;
    N-[1-(3'-메틸피리드-4'-일)에틸]사이클로헥산카복시아미드 ;
    N-[1-(2',6'-디메틸피리드-4'-일)에틸]사이클로헥산카복시아미드 ;
    N-[1-(2',5'-디메틸피리드-4'-일)에틸]사이클로헥산카복시아미드 ;
    N-[1-(2',3'-디메틸피리드-4'-일)에틸]사이클로헥산카복시아미드 ;
    N-[1-(3',5'-디메틸피리드-4'-일)에틸]사이클로헥산카복시아미드 ;
    N-[1-(4'-피리딜)에틸]사이클로헥실메틸아민 ;
    N-[1-(2'-메틸피리드-4'-일)에틸]사이클로헥실메틸아민 ;
    N-[1-(3'-메틸피리드-4'-일)에틸]사이클로헥실메틸아민 ;
    N-[1-(2',6'-디메틸피리드-4'-일)에틸]사이클로헥실메틸아민 ;
    N-[1-(2',5'-디메틸피리드-4'-일)에틸]사이클로헥실메틸아민 ;
    N-[1-(2',3'-디메틸피리드-4'-일)에틸]사이클로헥실메틸아민 ;
    N-[1-(3',5'-디메틸피리드-4'-일)에틸]사이클로헥실메틸아민 ;
    2-(4'-피리딜)프로필사이클로헥실케톤 ;
    2-(2'-메틸피리드-4'-일)프로필사이클로헥실케톤 ;
    2-(3'-메틸피리드-4'-일)프로필사이클로헥실케톤 ;
    2-(2',6'-디메틸피리드-4'-일)프로필사이클로헥실케톤 ;
    2-(2',5'-디메틸피리드-4'-일)프로필사이클로헥실케톤 ;
    2-(2',3'-디메틸피리드-4'-일)프로필사이클로헥실케톤 ;
    2-(3',5'-디메틸피리드-4'-일)프로필사이클로헥실케톤 ;
    중에서 선택된 단일 에난티오머로서 또는 라세미 혼합물서의 화합물 및 약제학적으로 허용되는 이의 염.
  6. 사이클로헥실2-(4'-피리딜)프로피오네이트 ;
    사이클로헥실2-(2'-메틸피리드-4'-일)프로피오네이트 ;
    사이클로헥실2-(3'-메틸피리드-4'-일)프로피오네이트 ;
    사이클로헥실2-(2',6'-디메틸피리드-4'-일)프로피오네이트 ;
    사이클로헥실2-(2',5'-디메틸피리드-4'-일)프로피오네이트 ;
    사이클로헥실2-(2',3'-디메틸피리드-4'-일)프로피오네이트 ;
    사이클로헥실2-(2',5'-디메틸피리드-4'-일)프로피오네이트 ;
    N-사이클로헥실-2-(4'-프리딜)프로판아미드 ;
    N-사이클로헥실-2-(2'-메틸피리드-4'-일)프로판아미드 ;
    N-사이클로헥실-2-(3'-메틸피리드-4'-일)프로판아미드 ;
    N-사이클로헥실-2-(2',6'-디메틸피리드-4'-일)프로판아미드 ;
    N-사이클로헥실-2-(2',5'-디메틸피리드-4'-일)프로판아미드 ;
    N-사이클로헥실-2-(2',3'-디메틸피리드-4'-일)프로판아미드 ;
    N-사이클로헥실-2-(3',5'-디메틸피리드-4'-일)프로판아미드 ;
    2-(4'-피리딜)프로필사이클로헥실 에테르 ;
    2-(2'-메틸피리드-4'-일)프로필사이클로헥실 에테르 ;
    2-(3'-메틸피리드-4'-일)프로필사이클로헥실 에테르 ;
    2-(2',6'-디메틸피리드-45-)프로필사이클로헥실 에테르 ;
    2-(2',5'-디메틸피리드-45-)프로필사이클로헥실 에테르 ;
    2-(2',3'-디메틸피리드-45-)프로필사이클로헥실 에테르 ;
    2-(2',5'-디메틸피리드-45-)프로필사이클로헥실 에테르 ;
    N-사이클로헥실-2-(4'-피리딜)프로필아민 ;
    N-사이클로헥실-2-(2'-메틸피리드-4'-일)프로필아민 ;
    N-사이클로헥실-2-(3'-메틸피리드-4'-일)프로필아민 ;
    N-사이클로헥실-2-(2',6'-디메틸피리드-4'-일)프로필아민 ;
    N-사이클로헥실-2-(2',5'-디메틸피리드-4'-일)프로필아민 ;
    N-사이클로헥실-2-(2',3'-디메틸피리드-4'-일)프로필아민 ;
    N-사이클로헥실-2-(3',5'-디메틸피리드-4'-일)프로필아민 ;
    1-사이클로헥실-3-(4'-피리딜)-2-부탄온 ;
    1-사이클로헥실-3-(2'-메틸피리드-4'-일)-2-부탄온 ;
    1-사이클로헥실-3-(3'-메틸피리드-4'-일)-2-부탄온 ;
    1-사이클로헥실-3-(2',6'-디메틸피리드-4'-일)-2-부탄온 ;
    1-사이클로헥실-3-(2',5'-디메틸피리드-4'-일)-2-부탄온 ;
    1-사이클로헥실-3-(2',3'-디메틸피리드-4'-일)-2-부탄온 ;
    1-사이클로헥실-3-(3',5'-디메틸피리드-4'-일)-2-부탄온 ;
    1-사이클로헥실-3-(4'-피리딜)부탄 ;
    1-사이클로헥실-3-(2'-메틸피리드-4'-일)부탄 ;
    1-사이클로헥실-3-(3'-메틸피리드-4'-일)부탄 ;
    1-사이클로헥실-3-(2',6'-디메틸피리드-4'-일)부탄 ;
    1-사이클로헥실-3-(3',5'-디메틸피리드-4'-일)부탄 ;
    1-사이클로헥실-3-(2',3'-디메틸피리드-4'-일)부탄 ; 및
    1-사이클로헥실-3-(2',5'-디메틸피리드-4'-일)부탄 ;
    중에서 선택된 단일 에난티오머로서 또는 라세미 혼합물로서의 화합물 및 약제학적으로 허용되는 이의 염.
  7. 제 5항 또는 6항에 있어서, 염이 하이드로클로라이드인 화합물의 염.
  8. (1)알킬화 반응에 의해 그룹 R을 일반식(Ⅱ)의 화합물에 도입시켜 일반식(Ⅰ)의 화합물[여기에서, R, R1,R2, 및 n은 제 1항에 정의한 바와 같고, A는이며 B는 -0-, -NH- 또는 -CH2- 이다] 을 수득하거나 ;
    (2)일반식 (Ⅲ)의 화합물 또는 이의 반응성 유도체를 일반식(Ⅳ)의 화합물과 반응시켜 일반식(Ⅰ)의화합물 [여기에서, R,R1,R2, 및 n 은 제 1항에서 정의한 바와 같고, A는 -0-, -NH- 또는 -CH2- 이며, B는 O=이다]을 수득하거나 ;
    (3)일반식(Ⅰ)의 화합물[여기에서, R, R1, R2및 n은 제1항에서 정의한 바와 같고 (i)A는 C=O이고 B는-0- 또는 NH이거나 (ⅱ) A는 -0- 또는 -NH- 이고 B는이다]을 환원시켜 상응하는 일반식(Ⅰ)의화합물[여기에서, (ⅰ')A는 -CH2-이고 B는 -0- 또는 -NH- 이거나 (ⅱ') A는 -0- 또는 NH 이고 B는 -CH2- 이다]을 수득하거나 ;
    (4) 일반식(Ⅰ)의 화합물 [여기에서, R, R1, R2, 및 n은 제1항에서 정의한 바와 같고, A는이고 B는 -CH2-이거나 A는 -CH2-이고 B는이다]을 수득하고: 필요한 경우, 일반식(I)의 화합물을 염화(Salifying)시키거나 이의 염으로 부터 일반식(I)의 유리 화합물을 수득하고/하거나, 필요한 경우, 일반식(I)의 이성체 혼합물을 단독 이성체로 분리시킴을 특징으로 하여 제1항에 따른 필요한 일반식(I)의 화합물 또는 이의 염을 제조하는 방법.
    상기식에서, B는 -0-, NH- 또는 -CH2-이고, Y는 -OH-, NH2또는 그룹 -CH2-M-X(여기에서, M은 금속이고 X는 할로겐이다)이며, R, R1, R2및 n 은 제1항에서 정의한 바와 같다.
  9. 불활성 담체 및/ 또는 희석제 및 , 활성물질로서 제 1항에 따른 일반식(Ⅰ)의 화합물, 또는 약제학적으로 허용되는 이의 염을 함유하는 약제학적 조성물.
  10. 제1항에 있어서, 아로마타제 억제제로서, 및 홀몬-의존 종양 및 전립선 중생(hyperplasia)의 치료에 사용하기 위한 일반식(Ⅰ)의 화합물 또는 이의 염.
  11. 제 9항에 있어서, 아로마타제 억제제로서, 및 홀몬-의존 종양 및 전립선 증생의 치료에 사용하기 위한 약제학적 조성물.
  12. 아로마타제 억제, 및 홀몬-의존 종양 및 전립선 중생의 치료에 활성을 갖는 제9항에 따른 약제학적 조성물의 제조에 있어서, 제1항에 따른 일반식 (Ⅰ)의 화합물 및 이의 염의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019870007741A 1986-07-18 1987-07-16 사이클로알킬-치환 4- 피리딜 유도체 및 이의 제조방법 KR880001598A (ko)

Applications Claiming Priority (4)

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GB868617596A GB8617596D0 (en) 1986-07-18 1986-07-18 Cycloalkyl-substituted 4-pyridyl derivatives
GB8617596 1986-07-18
GB868628029A GB8628029D0 (en) 1986-11-24 1986-11-24 Cycloalkyl-substituted 4-pyridyl derivatives
GB8628029 1986-11-24

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CA (1) CA1294624C (ko)
DK (1) DK375987A (ko)
FI (1) FI873144A (ko)
HU (1) HU201013B (ko)
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GB8701080D0 (en) * 1987-01-19 1987-02-18 Erba Farmitalia Cycloalkyl-substituted 4-aminophenyl halo derivatives
NZ242054A (en) * 1991-03-22 1993-11-25 British Tech Group Pyridine derivatives having a bridged alicyclic group; medicaments
US6011068A (en) * 1991-08-23 2000-01-04 Nps Pharmaceuticals, Inc. Calcium receptor-active molecules
US6001884A (en) * 1991-08-23 1999-12-14 Nps Pharmaceuticals, Inc. Calcium receptor-active molecules
US6031003A (en) * 1991-08-23 2000-02-29 Nps Pharmaceuticals, Inc. Calcium receptor-active molecules
US6313146B1 (en) 1991-08-23 2001-11-06 Nps Pharmaceuticals, Inc. Calcium receptor-active molecules
KR100235976B1 (ko) * 1992-05-15 1999-12-15 말콤 카터, 리차드 케이쓰 퍼시 치환된 피리딘 화합물,이것들의 제조방법 및 약제학적 사용방법
JP3298883B2 (ja) * 1992-06-30 2002-07-08 ポハン アイアン アンド スチール カンパニー リミテッド 強力なpaf拮抗剤としての新規な環式脂質誘導体
ATE287390T1 (de) 1994-10-21 2005-02-15 Nps Pharma Inc Kalzium-rezeptor aktive verbindungen
ATE430123T1 (de) 1996-05-01 2009-05-15 Nps Pharma Inc Inorganische am ionen-rezeptor aktive verbindungen
JP5383191B2 (ja) * 2005-08-15 2014-01-08 ジボダン エス エー 清涼化合物
CN108530347A (zh) * 2018-05-29 2018-09-14 湖南华腾制药有限公司 一种2-取代-4-吡啶乙酸盐酸盐的化合物及其制备方法

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GB842996A (en) * 1956-06-22 1960-08-04 Irwin Neisler & Co Pyridine derivatives
JPS5071646A (ko) * 1973-11-05 1975-06-13
GB2080808B (en) * 1980-01-25 1984-01-04 Reanal Finomvegyszergyar Process for the preparation of n-aryl-n-(mono- or disubstituted)-urea derivatives
US4617307A (en) * 1984-06-20 1986-10-14 Ciba-Geigy Corporation Substituted imidazo[1,5-A]pyridine derivatives as aromatase inhibitors
MA20552A1 (fr) * 1985-10-11 1986-07-01 Pan Medica Sa Alkylacarboxamides de pyridylalkylamines,leurs preparations et leurs utilisations

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DK375987D0 (da) 1987-07-17
IL83163A (en) 1991-06-10
CA1294624C (en) 1992-01-21
FI873144A (fi) 1988-01-19
IL83163A0 (en) 1987-12-31
EP0253681A3 (en) 1989-08-02
HU201013B (en) 1990-09-28
PT85337A (en) 1987-08-01
NZ221059A (en) 1989-10-27
EP0253681A2 (en) 1988-01-20
DK375987A (da) 1988-01-19
HUT44506A (en) 1988-03-28
AU597691B2 (en) 1990-06-07
FI873144A0 (fi) 1987-07-16
SU1639428A3 (ru) 1991-03-30
PT85337B (pt) 1990-04-30
AU7569087A (en) 1988-01-21

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