KR890001554A - 시클로덱스트린을 함유하는 항비루스성 약제 조성물 - Google Patents
시클로덱스트린을 함유하는 항비루스성 약제 조성물 Download PDFInfo
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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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- B—PERFORMING OPERATIONS; TRANSPORTING
- B82—NANOTECHNOLOGY
- B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
- A61K47/6949—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
- A61K47/6951—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes using cyclodextrin
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- 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
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- 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
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Abstract
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Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (11)
- 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.
- 제1항에 있어서, 항바이루스제가 소수성 비펩티드제(hydrophobic nonpetide agent)인 약제 조성물.
- 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.
- 제3항에 있어서, 에테르의 치환기가1-3알킬, 히드록시 C2-4알킬 또는 카르복시 C1-2알킬인 약제 조성물.
- 제3항에 있어서, 치환도(DS)가 0.125 내지 3이고, 몰치환평균(MS)가 0.3 내지 3인 약제 조성물.
- 제1항 또는 제5항의 어느 한 항에 있어서, 시클로텍스트린 : 항비루스제의 몰비가 1:1 내지 5:1 인 약제 조성물.
- 제1항 또는 제6항의 어느 한 항에 있어서, 항비루스가 다음 일반식(I)의 화합물상기 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.
- 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.
- 항비루스 약제 조성물(제1항 또는 제8항의 어느 한 항의 조성물)을 함유하는 분무제.
- 시클로텍스트린과 항비루스성 약제를 균일하게 혼합하고 임의로 약제성분을 조성하여 약제 조성물(제1항 또는 제8항의 어느 한 항의 약제 조성물)을 제조하는 벙법.
- 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.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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US6851287A | 1987-07-01 | 1987-07-01 | |
US068,512 | 1987-07-01 |
Publications (1)
Publication Number | Publication Date |
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KR890001554A true KR890001554A (ko) | 1989-03-27 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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KR1019880007902A KR890001554A (ko) | 1987-07-01 | 1988-06-29 | 시클로덱스트린을 함유하는 항비루스성 약제 조성물 |
Country Status (16)
Country | Link |
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US (1) | US4956351A (ko) |
EP (1) | EP0300526A3 (ko) |
JP (1) | JPS6445319A (ko) |
KR (1) | KR890001554A (ko) |
AU (1) | AU611692B2 (ko) |
CA (1) | CA1322172C (ko) |
DK (1) | DK360988A (ko) |
FI (1) | FI883136A (ko) |
HU (1) | HU204705B (ko) |
IL (1) | IL86910A0 (ko) |
NO (1) | NO882926L (ko) |
NZ (1) | NZ225045A (ko) |
PH (1) | PH26159A (ko) |
PT (1) | PT87880A (ko) |
RU (1) | RU2016567C1 (ko) |
ZA (1) | ZA884747B (ko) |
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Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GR64915B (en) * | 1978-09-14 | 1980-06-09 | Janssen Pharmaceutica Nv | Improved etomidate-containing compositions |
HU194858B (en) * | 1982-12-03 | 1988-03-28 | Chinoin Gyogyszer Es Vegyeszet | Process for producing dibenzo/b,d/pirane derivatives and pharmaceutical compositions containing them |
DE3346123A1 (de) * | 1983-12-21 | 1985-06-27 | Janssen Pharmaceutica, N.V., Beerse | Pharmazeutische praeparate von in wasser schwerloeslichen oder instabilen arzneistoffen und verfahren zu ihrer herstellung |
IT1196033B (it) * | 1984-02-22 | 1988-11-10 | Chiesi Farma Spa | Composto ad attivita' antiinfiammatoria ottenuto per complessazione con beta-ciclodestrina e relative formulazioni farmaceutiche |
US5001125A (en) * | 1984-03-26 | 1991-03-19 | Janssen Pharmaceutica N.V. | Anti-virally active pyridazinamines |
US4727064A (en) * | 1984-04-25 | 1988-02-23 | The United States Of America As Represented By The Department Of Health And Human Services | Pharmaceutical preparations containing cyclodextrin derivatives |
GB8506792D0 (en) * | 1985-03-15 | 1985-04-17 | Janssen Pharmaceutica Nv | Derivatives of y-cyclodextrin |
GB8613688D0 (en) * | 1986-06-05 | 1986-07-09 | Euro Celtique Sa | Pharmaceutical composition |
-
1988
- 1988-06-15 NZ NZ225045A patent/NZ225045A/xx unknown
- 1988-06-22 EP EP88201288A patent/EP0300526A3/en not_active Ceased
- 1988-06-23 US US07/210,677 patent/US4956351A/en not_active Expired - Fee Related
- 1988-06-24 AU AU18352/88A patent/AU611692B2/en not_active Ceased
- 1988-06-29 KR KR1019880007902A patent/KR890001554A/ko not_active Application Discontinuation
- 1988-06-29 IL IL86910A patent/IL86910A0/xx unknown
- 1988-06-30 NO NO88882926A patent/NO882926L/no unknown
- 1988-06-30 RU SU884356120A patent/RU2016567C1/ru active
- 1988-06-30 FI FI883136A patent/FI883136A/fi not_active Application Discontinuation
- 1988-06-30 CA CA000570955A patent/CA1322172C/en not_active Expired - Fee Related
- 1988-06-30 PT PT87880A patent/PT87880A/pt not_active Application Discontinuation
- 1988-06-30 DK DK360988A patent/DK360988A/da not_active Application Discontinuation
- 1988-06-30 HU HU883383A patent/HU204705B/hu not_active IP Right Cessation
- 1988-07-01 ZA ZA884747A patent/ZA884747B/xx unknown
- 1988-07-01 PH PH37160A patent/PH26159A/en unknown
- 1988-07-01 JP JP63162733A patent/JPS6445319A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
HUT47433A (en) | 1989-03-28 |
RU2016567C1 (ru) | 1994-07-30 |
DK360988A (da) | 1989-01-02 |
EP0300526A2 (en) | 1989-01-25 |
FI883136A (fi) | 1989-01-02 |
AU611692B2 (en) | 1991-06-20 |
NZ225045A (en) | 1990-06-26 |
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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