KR930000511A - 결정질 옥사티올란 유도체 - Google Patents

결정질 옥사티올란 유도체 Download PDF

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KR930000511A
KR930000511A KR1019920009537A KR920009537A KR930000511A KR 930000511 A KR930000511 A KR 930000511A KR 1019920009537 A KR1019920009537 A KR 1019920009537A KR 920009537 A KR920009537 A KR 920009537A KR 930000511 A KR930000511 A KR 930000511A
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crystalline form
hydroxymethyl
cis
amino
oxathiolan
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KR1019920009537A
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KR100244008B1 (ko
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레이븐스크로프트 폴
고든 로버츠 토니
에반스 폴
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원본미기재
글락소 그룹 리미티드
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Communicable Diseases (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Oncology (AREA)
  • Veterinary Medicine (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
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Abstract

내용 없음

Description

결정질 옥사티올란 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 침상 결정 형태(형태 Ⅰ)의 3TC를 나타내는 도면.
제2도는 양추형 결정 형태(형태Ⅱ)의 3TC를 나타내는 도면.
제3도는 결정 형태 Ⅰ의 적외선 스펙트럼을 나타내는 도면.

Claims (25)

  1. 결정질 형태의 (-)-시스-4-아미노-1-(2-히드록시메틸-1,3-옥사티올란-5일)-(1H)-피리미딘-2-온.
  2. 양추형 결정 형태의 (-)-시스-4-아미노-1-(2-히드록시메틸-1,3-옥사티올란-5일)-(1H)-피리미딘-2-온.
  3. 제1항 또는 제2항에 있어서, 융점이 170℃이상인 결정질 형태.
  4. 제1항 내지 3항중 어느 한 항에 있어서, 융점이 177 내지 178℃인 결정질 형태.
  5. 제1항 내지 4항중 어느 한 항에 있어서, 적외선 스펙트럼의 920및 850파수에서 흡수띠를 갖는 결정질 형태.
  6. 제1항 내지 5항중 어느 한 항에 있어서, 적외선 스펙트럼의 1110파수에서 흡수띠가 없는 결정질 형태.
  7. 제1항 내지 6항중 어느 한 항에 있어서, 시차 주사 열량계 프로파일에서 177 내지 178℃에서 흡열이 개시되는 결정질 형태.
  8. 침상 결정 형태의 (-)-시스-4-아미노-1-(2-히드록시메틸-1,3-옥사티올란-5일)-(1H)-피리미딘-2-온.
  9. 제1항 또는 8항에 있어서, 융점이 약 130℃미만인 결정질 형태.
  10. 제1항, 8항 또는 9항에 있어서, 융점이 124 내지 127℃인 결정질 형태.
  11. 제1항 및 8항 내지 11항중 어느 한 항에 있어서, 시차 주사 열량계 프로파일에서 124 내지 127℃에서 흡열이 개시되는 결정질 형태.
  12. 제1항 및 8항 내지 11항중 어느 한 항에 있어서, 적외선 스펙트럼의 약1110파수에서 흡수띠를 갖는 결정질 형태.
  13. 제1도에 나타낸 결정질 형태의 (-)-시스-4-아미노-1-(2-히드록시메틸-1,3-옥사티올란-5일)-(1H)-피리미딘-2-온.
  14. 제2도에 나타낸 결정질 형태의 (-)-시스-4-아미노-1-(2-히드록시메틸-1,3-옥사티올란-5일)-(1H)-피리미딘-2-온.
  15. 제3도에 나타낸 적외선 스펙트럼을 갖는 결정질 형태의 (-)-시스-4-아미노-1-(2-히드록시메틸-1,3-옥시티올란-5일)-(1H)-피리미딘-2-온.
  16. 제4도에 나타낸 적외선 스펙트럼을 갖는 결정질 형태의 (-)-시스-4-아미노-1-(2-히드록시메틸-1,3-옥사티올란-5일)-(1H)-피리미딘-2-온.
  17. 수용액으로부터 화합물을 결정화시키는 것으로 이루어진, 결정질 형태의 (-)-시스-4-아미노-1-(2-히드록시메틸-1,3-옥사티올란-5일)-(1H)-피리미딘-2-온의 제조방법.
  18. 화합물의 수용액을 프로판-1-올과 함께 공비중류시키는 것으로 이루어진, 결정질 형태의 (-)-시스-4-아미노-1-(2-히드록시메틸-1,3-옥사티올란-5일)-(1H)-피리미딘-2-온의 제조방법.
  19. 비수성 매질로부터 재결정화시키는 것으로 이루어진, 결정질 형태의 (-)-시스-4-아미노-1-(2-히드록시메틸-1,3-옥사티올란-5일)-(1H)-피리미딘-2-온의 제조방법.
  20. 제19항에 있어서, 비수성 매질이 C2-6알콜인 방법.
  21. 제20항 또는 21항에 있어서, 비수성 매질이 에탄올 및 공업용 메틸화 주정으로부터 선택되는 방법.
  22. 침상 결정 형태의 화합물을 에탄올 또는 공업용 메틸화 주정 중에서 승온에서 숙성시키는 것으로 이루어진, 양추형 결정 형태의 (-)-시스-4-아미노-1-(2-히드록시메틸-1,3-옥사티올란-5일)-(1H)-피리미딘-2-온의 제조방법.
  23. 결정질 형태의 (-)-시스-4-아미노-1-(2-히드록시메틸-1,3-옥사티올란-5일)-(1H)-피리미딘-2-온 및 그의 제약상 허용되는 담체로 이루어진 약제.
  24. 제23항에 있어서, 경구 투어용으로 적절한 형태의 약제.
  25. 제23항 또는 24항에 있어서, 정제 또는 캡슐제 형태의 약제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920009537A 1991-06-03 1992-06-02 결정질 옥사티올란 유도체 KR100244008B1 (ko)

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GB9111902.4 1991-06-03
GB919111902A GB9111902D0 (en) 1991-06-03 1991-06-03 Chemical compounds

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KR930000511A true KR930000511A (ko) 1993-01-15
KR100244008B1 KR100244008B1 (ko) 2000-03-02

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US (1) US5905082A (ko)
EP (2) EP1099700A1 (ko)
JP (1) JP2851480B2 (ko)
KR (1) KR100244008B1 (ko)
AP (1) AP300A (ko)
AT (1) ATE212630T1 (ko)
AU (2) AU656379B2 (ko)
BG (1) BG60914B1 (ko)
CA (2) CA2311988C (ko)
CZ (1) CZ284513B6 (ko)
DE (1) DE69232387T2 (ko)
DK (1) DK0517145T3 (ko)
ES (1) ES2171158T3 (ko)
GB (1) GB9111902D0 (ko)
GE (1) GEP19991834B (ko)
HK (1) HK1009599A1 (ko)
IE (2) IE921780A1 (ko)
IL (1) IL102073A (ko)
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AU1881092A (en) 1993-01-08
IS1867B (is) 2003-05-02
AP9200395A0 (en) 1992-07-31
ATE212630T1 (de) 2002-02-15
IL102073A (en) 1996-05-14
US5905082A (en) 1999-05-18
CA2311988C (en) 2005-11-15
EP1099700A1 (en) 2001-05-16
IS3873A (is) 1992-12-04
WO1992021676A1 (en) 1992-12-10
IS4268A (is) 1995-02-27
BG98254A (bg) 1994-07-29
AU656379B2 (en) 1995-02-02
DE69232387D1 (de) 2002-03-14
RU2102393C1 (ru) 1998-01-20
GB9111902D0 (en) 1991-07-24
NO301713B1 (no) 1997-12-01
DK0517145T3 (da) 2002-05-06
SK281249B6 (sk) 2001-01-18
KR100244008B1 (ko) 2000-03-02
AU1736192A (en) 1993-03-11
JPH06211848A (ja) 1994-08-02
IL102073A0 (en) 1993-01-14
CA2311988A1 (en) 1992-12-04
JP2851480B2 (ja) 1999-01-27
EP0517145B1 (en) 2002-01-30
NO922182L (no) 1992-12-04
IE921780A1 (en) 1992-12-16
CA2070230C (en) 2004-08-03
BG60914B1 (bg) 1996-06-28
UA41265C2 (uk) 2001-09-17
CA2070230A1 (en) 1992-12-04
TW254939B (ko) 1995-08-21
OA09913A (en) 1994-09-15
ES2171158T3 (es) 2002-09-01
IE20020782A1 (en) 2003-04-02
SK125793A3 (en) 1994-11-09
GEP19991834B (en) 1999-11-05
NZ242981A (en) 1994-04-27
CZ284513B6 (cs) 1998-12-16
NO922182D0 (no) 1992-06-02
MX9202619A (es) 1992-12-01
AP300A (en) 1994-01-20
CZ261293A3 (en) 1994-04-13
ZA924007B (en) 1993-04-28
DE69232387T2 (de) 2002-09-26
PT517145E (pt) 2002-07-31
SG52455A1 (en) 1998-09-28
HK1009599A1 (en) 1999-06-04

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