KR890001554A - 시클로덱스트린을 함유하는 항비루스성 약제 조성물 - Google Patents

시클로덱스트린을 함유하는 항비루스성 약제 조성물 Download PDF

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KR890001554A
KR890001554A KR1019880007902A KR880007902A KR890001554A KR 890001554 A KR890001554 A KR 890001554A KR 1019880007902 A KR1019880007902 A KR 1019880007902A KR 880007902 A KR880007902 A KR 880007902A KR 890001554 A KR890001554 A KR 890001554A
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pharmaceutical composition
hydrogen
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엘. 메센스 제인
제이. 엘. 엠. 인드리에스 코엔라아드
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폴 아드리안 쟌 쟈안센
쟈안센 파아마슈우티카 엔.부이.
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses

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Abstract

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Description

시클로텍스트린을 함유하는 항비루스성 약제 조성물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (11)

  1. 시클로텍스트린과 일반식(I)의 항비루스성 화합물, 그 산부가염, 그 입체화학 이성체 또는 그 호변 이성체로 이루어진 항비루스성 전염병 치료제인 약제 조성물. 단, 시클로텍스트린이 γ-시클로텍스트린 에테르 또는 혼합에테르이고, 에테르 치환제가 C1-6알킬, 히드록시, C1-6알킬, 카르복시 C1-6알킬 또는 (C|1-6알킬 옥시카르보닐) C1-6알킬인 경우 일반식(I)의 화합물인 약제가 아니다.
    상기 일반식(I)에서, R1은 수소, 할로, 1H-이미다졸-1-일. C1-6알킬옥시, 아릴옥시, 아릴C1-6알킬옥시, C1-6알킬티오, 아릴티오, 히드록시, 메르캅토, 아미노 C1-6알킬술포닐, 시아노, C1-6알킬옥시카르보닐, C1-6알킬카르보닐 또는 C1-6알킬이고, R2와 R3는 각각 수소 또는 C1-6알킬이거나, R2와 R3가 결합하여 식 -CH=CH-CH=CH-의 2가 기를 형성할 수 있고, A는
    -CH=N-CH=CH- (a)
    -CmH2m-N(R4-CnH2n- (b)
    -CmH2m-C(R5R6-CnH2n- (c), 또는
    -Cm-1H2(m-1)-C(R7)=C(R8)-CnH2n- (d)의 기이고, 상기 CnH2n, Cn-1H2(m-1) 또는 CmH2m기 내의 수소원자 1개는 C1-6알킬 또는 아릴과 치환될 수 있고, m은 n은 각각 1 내지 4의 정수이고, m과 n의 합은 3,4 또는 5이고, R4는 수소, C1-6알킬, 아릴, 티리아졸릴, 피리미디닐, 퀴노리닐, C1-6알킬카르보닐, C1-6알킬옥시카그보닐, 아릴 C1-6알킬, 디아릴 C1-6알킬, 아릴카르보닐로 치환된 페닐 : 피리디닐 : 시아노 또는 C1-6알킬로 치환된 피리디닐 : 시클로헥실, 시클로헥세닐이거나, 시아노 및 아릴 중에서 선택 치환되는 시클로헥실 또는 시클로헥시닐이고, R5는 수소, C1-6알킬, 아릴 히드록시, C1-6알킬옥시, 아릴옥시 : 모르폴린, 피롤리딘 또는 피페리딘으로 치환된 C1-6알킬옥시 : 아미노(C1-6알킬 옥시카르보닐) 아미노, 아릴아미노, (아릴)(C1-6알킬)아미노, (아릴 C1-6알킬) 아미노, (아릴-C1-6알케닐) 아미노, (아릴-C1-2알케닐)아미노, (아릴 C1-2알케닐)(C1-6알킬) 아미노, 아릴카르보닐옥시이고, R6는 수소, 아릴, C1-6알킬, (C1-6알킬카르보닐아미노)-C1-6알킬, 아릴 C1-6알킬, 아릴카르보닐 C1-6알킬, 아미노카르보닐, 아릴카르보닐, 아릴아미노카르보닐, (아릴 C1-6알킬)카르보닐, C1-6알킬옥시카르보닐, 인들릴, 피리디닐이고, R7과 R8는 각각 수소, C1-6알킬, 아릴, 아릴C1-6알킬, 피리디닐이며, 상기 아릴은 페닐인데, 이는 할로, C1-6알킬, 트리플루오로메틸, 니트로, 아미노, C1-6알킬옥시, 히드록시, C1-6알킬옥시카르보닐, 티에닐 및 나프탈레닐 중에서 선택한 3개 이하의 치환기로 치환될 수 있다.
  2. 제1항에 있어서, 항바이루스제가 소수성 비펩티드제(hydrophobic nonpetide agent)인 약제 조성물.
  3. 제2항에 있어서, 시클로텍스트린이 β 또는 γ-시클로텍스트린에테르 또는 혼합에테르이고, 에테르의 치환기는 C1-6알킬, 히드록시, C1-6알킬, 카르복시, C1-6알킬 또는 (C1-6알킬옥시카르보닐) C1-6알킬인 약제 조성물.
  4. 제3항에 있어서, 에테르의 치환기가1-3알킬, 히드록시 C2-4알킬 또는 카르복시 C1-2알킬인 약제 조성물.
  5. 제3항에 있어서, 치환도(DS)가 0.125 내지 3이고, 몰치환평균(MS)가 0.3 내지 3인 약제 조성물.
  6. 제1항 또는 제5항의 어느 한 항에 있어서, 시클로텍스트린 : 항비루스제의 몰비가 1:1 내지 5:1 인 약제 조성물.
  7. 제1항 또는 제6항의 어느 한 항에 있어서, 항비루스가 다음 일반식(I)의 화합물
    상기 일반식(I)에서, R1은 수소, 할로, 1H-이미다졸-1-일, C1-6알킬옥시, 아릴옥시, 아릴C1-6알킬옥시, C1-6알킬티오, 아릴티오, 히드록시, 메르캅토, 아미노 C1-6알킬술포닐, C1-6알킬술포닐, 시아노, C1-6알킬옥시카르보닐, C1-6알킬카르보닐 또는 C1-6알킬이고, R2와 R3는 각각 수소 또는 C1-6알킬이거나, R2와 R3가 결합하여 식 -CH=CH-CH=CH-의 2가기를 형성할 수 있고, A는
    -CmH2m-N(R4-CnH2n- (b)
    -CmH2m-C(R5R6-CnH2n- (c), 또는
    -Cm-1H2(m-1)-C(R7)=C(R8)-CnH2n- (d)의 기이고, C1-6알킬, 아릴, C1-6알킬, 아미노카르보닐, 아릴카르보닐, 아릴아미노카르보닐, (아릴 C1-6알킬)카르보닐, C1-6알킬옥시 카르보닐, 인돌릴, 피리디닐이고, R7과 R8은 각각 수소, C1-6알킬, 아릴, 아릴 C1-6알킬, 피리디닐이며, 상기 아릴은 페닐인데, 이는 할로, C1-6알킬, 트리플루오로메틸, 니트로, 아미노, C1-6알킬옥시, 히드록시, C1-6알킬옥시카르보닐, 티에닐 및 나프탈레닐중에서 선택한 3개 이하의 치환기로 치환될 수 있다.
  8. 제7항에 있어서, 항비루스제가 3-클로로-6-[3,6-디히듣로-4-(3-메틸페닐)-1(2H)-피리디닐]피리디진 : 3-클로로-6-[3-[3-(트리플로오로메틸)페닐]-1-피톨리디닐]피리다진 :3-메틸-6-[3-[3-(트리플루오로메틸)페닐]-1-피톨리디닐]피리다진 :3-요도-6-[3-[3-(트리플루오로메틸)페닐]-1-피톨리디닐]피리다진 : 3-브로모-6-[3-[3-(트리풀루오로메틸)페닐]-1-피톨리디닐]피리다진 : 3-[3,6-디히드로-4-(3-메틸페닐)-1(2H)-피리디닐]-6-메톡시피리다진 : 3-메톡시-6-[4-[3-(메톡시페닐)페닐]-1-피페라지닐]피리다진 :3-보로모-6-[4-[3-(메틸페닐)-1-피페라지닐]피리다진인 약제 조성물.
  9. 항비루스 약제 조성물(제1항 또는 제8항의 어느 한 항의 조성물)을 함유하는 분무제.
  10. 시클로텍스트린과 항비루스성 약제를 균일하게 혼합하고 임의로 약제성분을 조성하여 약제 조성물(제1항 또는 제8항의 어느 한 항의 약제 조성물)을 제조하는 벙법.
  11. 시클로텍스트린을 물에 용해시키고 항비루스성 화합물을 가한 후 임의로 용액을 건조시켜 약제 조성물(제1항 또는 제8항의 어느 한 항의 약제 조성물)을 제조하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880007902A 1987-07-01 1988-06-29 시클로덱스트린을 함유하는 항비루스성 약제 조성물 KR890001554A (ko)

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AU611692B2 (en) 1991-06-20
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EP0300526A3 (en) 1989-04-12
PT87880A (pt) 1989-06-30
DK360988D0 (da) 1988-06-30
HU204705B (en) 1992-02-28
AU1835288A (en) 1989-01-05
CA1322172C (en) 1993-09-14
PH26159A (en) 1992-03-18
NO882926D0 (no) 1988-06-30
ZA884747B (en) 1990-03-28
IL86910A0 (en) 1988-11-30
JPS6445319A (en) 1989-02-17
NO882926L (no) 1989-01-02
US4956351A (en) 1990-09-11
FI883136A0 (fi) 1988-06-30

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