KR960700261A - 2, 6-디아미노푸린 유도체(2,6-Diaminopurine Derivatives) - Google Patents

2, 6-디아미노푸린 유도체(2,6-Diaminopurine Derivatives)

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KR960700261A
KR960700261A KR1019950702963A KR19950702963A KR960700261A KR 960700261 A KR960700261 A KR 960700261A KR 1019950702963 A KR1019950702963 A KR 1019950702963A KR 19950702963 A KR19950702963 A KR 19950702963A KR 960700261 A KR960700261 A KR 960700261A
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amino
compound
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ribofuranuronamide
ethyl
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마이클 그레그썬
배리 에드워드 에이러스
조지 블랜치 에완
프랭크 엘리스
죤 나이트
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앨렌 헤스케쓰
글락소 그룹 리미티드
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Abstract

본 발명은 하기 일반식(Ⅰ)의 2,6-디아미노푸린-β-D-리보푸란우론아미드 유도체, 및 그의 염 및 용매화물을 제공한다.
상기 식 중, R1은 수소 또는 C3-8-시클로알킬 또는 C1-6-알킬이고, R2는 C3-8-시클로알킬, C3-8-시클로알킬C1-6-알킬, Alk1Y, -(CHR5)m(Alk2)nZ, 또는 적당히 치환된 C3-8-시클로알킬, C3-8시클로알킬C1-6-알킬, 피롤리딘-3-일, 2-옥소피롤리딘-4-일, 2-옥소피롤리딘-5-일, 피페리딘-3-일 또는 피페리딘-4-일이고, Q는 산소 또는 황이다.
일반식(Ⅰ)의 화합물 및 그의 염 및 용매화물을 소염제로서, 특히 백혈구에 의해 조직이 손상받기 쉬운 염증성 질환이 있는 환자를 치료하는데 유용한다.

Description

2,6-디아미노푸린 유도체(2,6-Diaminopurine Derivatives)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (28)

  1. 하기 일반식(Ⅰ)의 화합물, 및 그의 염 및 용매화물.
  3. 상기 식 중, R1은 수소 원자 또는 C3-8-시클로알킬 또는 C1-6-알킬기이고, R2는 (ⅰ)C3-8-시클로알킬, (ⅱ)C2-7-아실아미노, 구아니디노, 카르복실, 옥소 및 (CH2)R3(여기서, p는 0 또는 1이고, R3은 히드록시, NH2, C1-6-알킬아미노 또는 디-C1-6-알킬아미노임)로부터 선택되는 동일 또는 상이한 1개 이상의 기(예컨대 1개, 2개 또는 3개의 기)로 치환된 C3-8-시클로알킬, (ⅲ)고리 질소 원자가 수소, C1-6-알킬 또는 아릴-C1-6-알킬(예:벤질)에 의해 치환된 피롤리딘-3-일, 2-옥소피롤리딘-4-일, 2-옥소피롤리딘-5-일, 피페리딘-3-일 또는 피페리딘-4-일, (ⅳ)고리 질소 원자가 수소, C1-6-알킬 또는 아릴-C1-6-알킬(예:벤질)에 의해 치환되고 고리 탄소 원자 중 1개 이상(예:고리 탄소 원자 1개, 2개 또는 3개)이 C2-7-아실아미노, 구아니디노, 옥소 및 (CH2)pR3(식 중, p 및 R3은 상기에서 정의한 바와 같음)로부터 선택된 동일 또는 상이한 기에 의해 치환된 피롤리딘-3-일, 피페리딘-3-일 또는 피페리딘-4-일, (ⅴ)C3-8-알킬 (ⅵ)고리 탄소 원자 중 1개 이상(예:고리 탄소 원자 1개, 2개 또는 3개)이 C2-7-아실아미노, 구아니디노, 카르복실, 옥소 및 (CH2)pR3(식 중, p 및 R3은 상기에서 정의한 바와 같음)로부터 선택된 동일 또는 상이한 기에 의해 치환된 C3-8-시클로알킬-C1-6-알킬, (ⅶ)-Alk1Y(식중, Alk1은 C2-6-알킬아미노 또는
  5. -[여기서, X는 결합, O, CH2또는 NR4(여기서, R4는 수소, C1-6-알킬 또는 아릴-C1-6-알킬임)임]로부터 선택되는 기임), 및 (ⅷ)-(CHR5)m(Alk2)nZ｛식 중, m 및 n은 각각 독립적으로 0 또는 1이지만, 단 m이 1일 때 n은 1이어야 하고; R5는 수소 원자 또는 카르복시기 또는 CH2R6기(여기서, R6은 6;2-7-아실아미노, 구아니디노, 히드록시, 메톡시, NH2, C1-6-알킬아미노, 또는 디-C1-6-알킬아미노임)이고; Alk2는 C1-6- 알킬리덴기이고; Z는 수소 원자, 또는 고리가 C1-6-알킬, C2-7-아실아미노, 구아니디노, 카르복시에틸, 히드록시, NH2, C1-6-알킬아미노 또는 디-C1-6-알킬아미노로부터 선택돈 동일 또는 상이한 1개 이상의 기(예:1,2 또는 3개의 기)로 임의 치환된 페닐, 피리딜, 피리미디닐, 이미다졸릴, 트리아졸릴, 테트라졸릴 및 벤즈이미다졸릴로부터 선택되는 임의 치환된 방향족 고리임｝로부터 선택된 기이고, Q는 산소 또는 황 원자이고, Rh는 페닐이다.
  6. 제1항에 있어서, R1이 C1-3-알킬인 화합물.
  7. 제1항 또는 제2항에 있어서, Q가 산소 원자인 화합물.
  8. 제1항에 있어서, R1NHC(=1)-가 에틸아미노카르보닐인 화합물.
  9. 상기 전 항 중 어느 하나의 항에 있어서, R2가 C2-7-아실아미노, 구아니디노, 카르복실, 옥소 및 (CH2)pR3로부터 선택된 1 또는 2개의 기로 치환된 시클로펜틸 또는 시클로헥실인 화합물.
  10. 제5항에 있어서, R2가 히드록시, NH2, 메틸아미노, 디메틸아미노, 아세트아미도 또는 트리플루오로사에 트아미도로부터 선택되는 1 또는 2개의 기로 치환된 시클로펜틸 또는 시클로헥실인 화합물.
  11. 제1항 내지 4항 중 어느 하나의 항에 있어서, R2가 각각의 고리가 독립적으로 수소, C1-3-알킬 또는 벤질로 치환될 수 있는 피롤리딘-3-일 또는 피페리딘-3-일인 화합물.
  12. 제1항 내지 4항 중 어느 하나의 하에 있어서, R2가 -(CHR5)m(Alk2)nZ(여기서, Z는 임의 치환된 이미다졸릴기임)인 화합물.
  13. 제8항에 있어서, -(CHR5)m(Alk2)n-가 -CH2CH2-인 화합물.
  14. (1S-트랜스)-1-데옥시-1-[6-[(2,2-디페닐에틸)아미노]-2-[(3-히드록시시클로펜틸)아미노]-9H-푸린-9-일]-N-에틸-β-D-리보푸란우론아미드; [1S-(1α,2β,3β)]-1-데옥시-[2-[(2,3-디히드록시시클로펜틸)아미노]-6-[(2,2-디페닐에틸)아미노]-9H-푸린-9-일]-N-에틸-β-D-리보푸란우론아미드; (1S-트랜스)-1-데옥시-1-[2-[(3-N,N-디메틸아미노)시클로펜틸아미노]-6-[(2,2-디페닐에틸)아미노]-9H-푸린-9-일]-N-에틸-β-D-리보푸란우론아미드; [(3S)-1-데옥시-1-[6-[(2,2-디페닐에틸)아미노]-2-[(3-피롤리디닐)아미노]-9H-푸린-9-일]-N-에틸-β-D-리보푸란우론아미드; (트랜스)-1-[2-[(4-아미노시클로헥실)아미노]-6-[(2,2-디펜닐에틸)아미노]-9H-푸린-9-일]-1-데옥시-N-에틸-β-D-리보푸란우론아미드;1-데옥시-1-[6-[(2,2-디페닐에틸)아미노]-2-[[2-(1-메틸-1H-이미다졸-4-일)에틸]아미노]-N-에틸-9H-푸린-9-일]-β-D-리보푸란우론아미드; (트랜스)-1-데옥시-1-[2-[(4,N,N-디메틸아미노시클로헥실)아미노]-6-[(2,2-디페닐에틸)아미노]-9H-푸린-9-일]-N-에틸-β-D-리보푸란우론아미드; 1-데옥시-1-[6-[(2,2-디페닐에틸)아미노]-2-[[2-(-메틸-1H-이미다졸-4-일)에틸]아미노]-9H-푸린-9-일]-N-에틸-β-D-리보푸란우론아미드; 및 그의 생리학적으로 허용되는 염 및 용매화물.
  15. (트랜스)-1-[2-[(4-아미노시클로헥실)아미노]-6-[(2,2-디페닐에틸]-9H-푸란-9-일]-데옥시-N-에틸-β-D-리보푸란우론아미드 및 그의 생리학적으로 허용되는 염 및 용매화물.
  16. (트랜스)-1-[2-[(4-아미노시클로헥실)아미노]-6-[(2,2-디페닐에틸)아미노]-9H-푸린-9-일]-1-데옥시-N-에틸-β-D-리보푸란우론아미드의 염산염.
  17. Z가 임의 치환된 트리아졸릴 또는 테트라졸릴일 수 없는 제1항에 정의된 일반식(Ⅰ)의 화합물.
  18. 의약 또는 수의약에 사용하기 위한 상기 전 항 중 어느 한 항에 정의된 일반식(Ⅰ)의 화합물.
  19. 백혈구에 의해 조직이 손방받기 쉬운 염증성 질환이 있는 환자 치료용 의약을 제조하기 위한 상기 전항 중 어느 한 항에 정의된 일반식(Ⅰ)의 화합물의 용도.
  20. 상기 전 항 중 어느 한 항에 정의된 일반식(Ⅰ)의 화합물을 필요에 따라 1종 이상의 생리학적으로 허용되는 담체 또는 부형제와 함께 포함하는 제약 조성물.
  21. (A)하기 일반식(Ⅱ)의 화합물을 아민 Rba -6.2aNH2(식 중 Rba -6.2aNH2는 R2기 또는 그의 보호기임)으로 처리하고, 있어서 필요에 따라 보호기를 제거하거나,
  23. (식 중, Ra및 Rb는 각각 수소 원자이거나, 또는 Ra및 Rb는 함께 알킬리덴기를 형성함), 또는 (B)일반식(Ⅰ)의 화합물의 보호된 유도체를 탈보호시키고, 필요에 따라 (ⅰ)염을 형성하거나, 또는 (ⅱ)일반식(Ⅰ)의 한 화합물을 일반식(Ⅰ)의 다른 화합물로 전환시키거나, 또는 (ⅲ)일반식(Ⅰ)의 화합물의 각 이성질체를 제조하는 것을 포함하는 제1항에 정의된 일반식(Ⅰ)의 화합물의 제조 방법.
  24. 백혈구에 의해 조직이 손상되기 쉬운 염증성 질환이 있는 사람 또는 동물에게 유효량의 일반식(Ⅰ)의 화합물 또는 그의 생리학적으로 허용되는 염 또는 용매화물을 투여하는 것을 포함하는 염증성 질환이 있는 사람 또는 동물에 치료 방법.
  25. 실질적으로 본 명세서에 기재된 제1항 내지 12항 중 어느 한 항의 화합물.
  26. 실질적으로 본 명세서에 기재된 제16항의 조성물.
  27. 실질적으로 본 명세서에 기재되고 예시된 제1항에 정의된 화합물의 제조 방법.
  28. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950702963A 1993-01-20 1994-01-18 2, 6-디아미노푸린 유도체(2,6-Diaminopurine Derivatives) KR960700261A (ko)

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IL108372A (en) 1998-06-15
SI9400021A (en) 1994-09-30
HU211914A9 (en) 1996-01-29
ATE164849T1 (de) 1998-04-15
SK91895A3 (en) 1996-04-03
EP0680488A1 (en) 1995-11-08
CZ187995A3 (en) 1996-01-17
TW267168B (ko) 1996-01-01
ECSP941104A (es) 1994-12-15
JPH08505864A (ja) 1996-06-25
ES2117249T3 (es) 1998-08-01
FI953489A0 (fi) 1995-07-19
NZ259880A (en) 1996-11-26
JP3768232B2 (ja) 2006-04-19
CA2153688A1 (en) 1994-08-04
CN1119440A (zh) 1996-03-27
ZA94335B (en) 1994-10-24
EP0680488B1 (en) 1998-04-08
SK281229B6 (sk) 2001-01-18
FI953489A (fi) 1995-09-13
RU2129561C1 (ru) 1999-04-27
WO1994017090A1 (en) 1994-08-04
DE69409503D1 (de) 1998-05-14
NO305603B1 (no) 1999-06-28
US5925624A (en) 1999-07-20
AP9400613A0 (en) 1994-01-31
AU679714B2 (en) 1997-07-10
DE69409503T2 (de) 1998-08-06
PE54194A1 (es) 1995-01-06
IS4121A (is) 1994-07-21
AU5885194A (en) 1994-08-15
NO952872L (no) 1995-09-13
CN1043997C (zh) 1999-07-07
AP457A (en) 1996-02-01
NO952872D0 (no) 1995-07-19
GB9301000D0 (en) 1993-03-10
DK0680488T3 (da) 1999-01-25
PL309975A1 (en) 1995-11-13
US5889178A (en) 1999-03-30
IL108372A0 (en) 1994-04-12

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