KR930019213A - 간염치료에 유용한 1,3-옥사티올란류 - Google Patents

간염치료에 유용한 1,3-옥사티올란류 Download PDF

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KR930019213A
KR930019213A KR1019920008402A KR920008402A KR930019213A KR 930019213 A KR930019213 A KR 930019213A KR 1019920008402 A KR1019920008402 A KR 1019920008402A KR 920008402 A KR920008402 A KR 920008402A KR 930019213 A KR930019213 A KR 930019213A
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cis
cytosine
oxathiolane
compound
hydrogen
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벨류 베르나드
누옌-바 네
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로우렌스 알. 윌슨
바이오켐 파르마 인코오포레이티드
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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Abstract

본 발명은 비루스감염을 치료하는데 뉴클레오시드 동족체를 사용하는 방법에 관한 것이다. 구체적으로 간염, 특히 B형 간염을 치료하는데 1,3-옥사티올란 뉴클레오시드 동족체를 사용하는 방법에 관한 것이다.

Description

간염치료에 유용한 1, 3-옥사티올란류
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (29)

  1. B형간염치료용 약물을 제조하는데 하기일반식(I)의 화합물 또는 그 약학적 허용 유도체를 사용하는 방법:
  3. 상기식중, R1은 수소 또는 아실이고; R2는 푸린 또는 피리미딘 염기 또는 그것의 동족체 또는 동족체이며; Z는, S, S=O, 또는 SO2인데; 단, 일반식(I)의 화합물이 시스배열이고, R1이 수소이며 Z가 S인 경우에는 R2는 시토신이 아니다.
  4. 제1항에 있어서, 상기 에스테르가 R-CP-O-(여기에서, R은 수소, 직쇄 또는 측쇄형 알킬, 알콕시알킬, 아르알킬, 아릴옥시알킬, 아릴 및 치환디히드로피리디닐에서 선택된다); 설포네이트 에스테르; 설페이트 에스테르; 아미노산 에스테르; 모노-, 디-또는 트리-포스페이트 에스테르; 다가산의 에스테르; 및 인산 에스테르로 이루어지는 군에서 선택되는 방법.
  5. 제1항에 있어서, Z가 S인 방법.
  6. 제1항에 있어서, 일반식(I)의 R2가 하기의 기들로 이루어지는 군에서 선택되는 방법;
  8. 상기식중, R3는 수소 및 비치환되거나 헤테로원자로 치환된 C1-6알킬로 이루어지는 군에서 선택되고; R4및 R5는 각각 수소, C1-6알킬, 염소, 불소 및 요오드로 이루어지는 군에서 선택되며; R6은 수소, CN, 카르복시, 에톡시카르보닐, 카바모일 및 티오카바 모일로 이루어지는 군에서 선택되고; X 및 Y는 각각 브롬, 염소, 불수, 요오드, 아미노 및 히드록시기로 이루어지는 군에서 선택된다.
  9. 제 4항에 있어서, R2가 하기의 기인 방법:
  11. 상기식중, R3수소 및 비치환되거나 헤테로원자로 치환된 C1-6알킬로 이루어지는 군에서 선택되고; R4는 수소, C1-6알킬 및 브롬, 염소, 불소 및 요오드로 이루어지는 군에서 선택되다.
  12. 제4항에 있어서, R3및 R4가 수소 또는 C1-6알킬인 방법.
  13. 제4항에 있어서, R5가 CH3또는 F인 방법.
  14. 제4항에 있어서, X 및 Y가 모두 NH2인 방법.
  15. 제1항에 있어서, 상기 화합물이 라셈혼합물 또는 단일 거울상이성질체 형태의 하기의 화합물들로 이루어지는 군에서 선택되는 방법 : 트랜스-2-히드록시멜틸-5-(시토신-1′-일)-1,3-옥사티올란; 시스-2-벤조일옥시메틸-5-(시토신-1′-일)-1,3-옥사티올란, 및 이들의 혼합물; 시스-2-히드록시메틸-5-(N4′-아셀틸-시토신-1′-일)-1,3-옥사티올란, 트랜스-2-히드록시멜틸-5-(N4′-아세틸-시토신-1′-일)-1,3-옥사티올란, 및 이들의 혼합물;시스-2-벤조일옥시메틸-5-(N4′-아세틸시토신-1′-일)-1,3-옥사티올란, 트랜스-2-벤조일옥시메틸-5-(N4′-아세틸시토신-1′-일)-1,3-옥사티올란 및 이들의 혼합물; 시스-2-벤조일옥시메틸-5-(N4′-아세틸-5-플로오로시토신 -1′-일)-1,3-옥사티올란,트랜스-2-벤조일옥시메틸-5-(N4′-아세틸-5-플루오로-시토신-1′-일)-1,3-옥사티올란, 및 이들의 혼합물; 시스-2-히드록시메틸-5-(5′-플루오로시토신-1′-일)-1,3-옥사티올란, 트랜스-2-히드록시메틸-5-(5-′플루오로시토신-1′-일)-1,3-옥사티올란 및 이들의 혼합물; 시스-2-히드록시메틸-5-(시토신-1′-일)-3-옥사티올란; 시스-2-히드록시메틸-5-(티민-N-1′-일)-1,3-옥사티올란; 시스-2-히드록시메틸-5-(N,N-디메틸아미노메틸렌 시토신-1′-일)-1,3-옥사티올란; 또는 이들의 약학적허용유도체.
  16. 제1항 내지 제9항중 어느 한항에 있어서, 상기 일반식(I)의 화합물이 단일 거울상이성질체 또는 라셈혼합물 형태인 방법.
  17. 제10항에 있어서, 상기 일반식(I)의 화합물이 그것의 (-)거울상이성질체 형태인 방법.
  18. 제10항에 있어서, 상기 일반식(I)의 화합물이 그것의 (+)거울상이성질체 형태인 방법.
  19. 제1항 내지 제9항중 어느 한항에 있어서, 상기 화합물이 그것의 시스 또는 트랜스배열 또는 이들의 혼합물형태인 방법.
  20. 제13항에 있어서 상기 일반식(I)의 화합물이 그것의 시스배열 형태인 방법.
  21. B형간염치료용 약물을 제조하는데 시스-2-히드록시메틸-5-(5′-플루오로시토신-1′-일)-1,3-옥사티올란을 사용하는 방법.
  22. B형간염치료용 약물을 제조하는데 시스-히드록시메틸-5-(N,N-디메틸아미노메틸렌시토신-1′-일)-1,3-옥사티올란을 사용하는 방법.
  23. 제1항 내지 제9항중 어느 한항에 있어서, 상기 약물이 경구, 비경구, 직장, 비강, 질내 또는 국소투여용인 방법.
  24. 제17항에 있어서, 상기 약물이 1일에 약 0.1내지 750mg/kg(체중)의 용량으로 투여되는 방법.
  25. 제17항에 있어서, 상기 약물이 단위투약형태의 약물인 방법.
  26. 제19항에 있어서, 상기 단위 투약형태가 약 10 내지 1500mg의 일반식(I)의 화합물을 함유하는 방법.
  27. 제1항 내지 제9항중 어느 한항에 있어서, 상기 약물이 약학적허용 부형제와 함께 투여되는 방법.
  28. 제1항 내지 제7항중 어느 한항에 있어서, 상기 약물이 항비루스제, 항박테리아제, 항균제 및 면역조절제로 이루어지는 군에서 선택된 치료활성제와 함께 투여되는 방법.
  29. ※ 참고사항 : 최초출원 내용에 의하여 공개되는 것임.
KR1019920008402A 1991-05-20 1992-05-19 1,3-옥사티올란을 포함하는 간염 치료용 약학적 조성물 KR100219958B1 (ko)

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DK0515144T3 (da) 2006-10-09
ATE329598T1 (de) 2006-07-15
AU1635192A (en) 1992-11-26
JP3167788B2 (ja) 2001-05-21
CA2068943A1 (en) 1992-11-21
GB9110874D0 (en) 1991-07-10
JPH11322608A (ja) 1999-11-24
JP2001226268A (ja) 2001-08-21
ES2270413T3 (es) 2007-04-01
HK1005542A1 (en) 1999-01-15
JPH05202045A (ja) 1993-08-10
DE69233631T2 (de) 2007-05-24
EP0515144B1 (en) 2006-06-14
DE69233631D1 (de) 2006-07-27
MX9202374A (es) 1994-06-30
US5486520A (en) 1996-01-23
EP0515144A1 (en) 1992-11-25
SG47418A1 (en) 1998-04-17
CA2068943C (en) 2000-11-28
AU656961B2 (en) 1995-02-23
IL101836A (en) 1997-03-18
ZA923477B (en) 1993-01-27
IE921601A1 (en) 1992-12-02
IL101836A0 (en) 1992-12-30

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