KR910016336A - 용액 제제 - Google Patents

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KR910016336A
KR910016336A KR1019910003135A KR910003135A KR910016336A KR 910016336 A KR910016336 A KR 910016336A KR 1019910003135 A KR1019910003135 A KR 1019910003135A KR 910003135 A KR910003135 A KR 910003135A KR 910016336 A KR910016336 A KR 910016336A
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시게오 나까니시
이와오 야마나까
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후지사와 도모기찌로
후지사와 야꾸힝 고교 가부시끼가이샤
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    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
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    • 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
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection

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  • Health & Medical Sciences (AREA)
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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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Abstract

내용 없음

Description

용액 제제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (6)

  1. 하기 일반식(Ⅰ)의 화합물 또는 이의 약학적으로 허용되는 염. 약학적으로 허용되는 계면 활성제 및 약학적으로 허용되는 비수용매를 함유하는 용액제제.
    상기식에서, 치환기[R1및 R2],[R3및 R4]및 [R5및 R6]의 각각의 근접 쌍은 독립적으로 a) 두개의 근접 수소원자를 나타내거나 b) 이들이 부착되어 있는 근접 탄소원자간에 제2결합을 형성하고; 상기 의미외에, R2는 알킬 그룹을 나타낼 수 있으며; R7은 H, OH, 보호된 하이드록시 또는 O-알킬을 나타내거나 R1과 함께 =O를 나타낼 수 있으며; R8및 R9는 독립적으로 H 또는 OH를 나타내고; R10은 H, 알킬, 하나이상의 하이드록실 그룹으로 치환된 알킬, 알케닐, 하나이상의 히이드록실 그룹으로 치환된 알케닐 또는 =O로 치환된 알킬이고; X는 0, (H, 0H),(H,H)또는 -CH2O-이고; Y는 O, (H, OH)(H, H) 또는 N-NR11R12또는 N-OR13을 나타내고; R11및 R12는 독립적으로 H, 알킬, 아릴 또는 토실을 나타내고; R13,R14,R15,R16,R17,R18,R19,R22,및 R23은 독립적으로 H 또는 알킬이고; R20및 R21은 독립적으로 0을 나타내거나 (R20a, H) 및 (R21a, H)를 각각 나타낼 수 있으며; R20a및 R21a는 독립적으로 OH, O- 알킬 또는 OCH2OCH2COH2OCH3를 나타내거나 R21a는보호된 하이드록시이고 ; 또한 R20a 및 R21a는 함께 에폭시드 고리내의 산소원자를 나타낼 수 있으며; n은 1,2 또는 3이고; 상기 의미외에, Y,R10및R23은 이들이 부착되어 있는 탄소원자와 함께 5원 또는 6원 N-, S- 또는 O-함유 복소환식 고리를 나타낼 수 있으며, 이들은 포화 또는 불포화될 수 있고, 알킬, 하이드록시, 하나이상의 하이드록실 그룹으로 치환된 알킬, O-알킬, 벤질 및 -CH2Se(C6H5)중에서 선택된 하나이상의 그룹으로 치환될 수 있다.
  2. 제 1 항에 있어서, 화합물(Ⅰ) 또는 이의 약학적으로 허용되는 염과 약학적으로 허용되는 계면 활성제가 1:1 내지 1:100 중량비 범위인 용액 제제.
  3. 제2항에 있어서, 약학적으로 허용되는 계면 활성제가 피마자유-계면 활성제인 용액 제제.
  4. 제3항에 있어서, 약학적으로 허용되는 비수용매가 에틸알코올인 용액제제.
  5. 제4항에 있어서, 화합물(Ⅰ)이 17-알릴-1, 14-디히드록시-12-[2-(4-하이드록시-3-메톡시시클로헥실)-1-메틸비닐]-23,25-디메톡시-13,19,21,27-테트라메틸-11,28-디옥사-4-아자트리시클로-[22.3.1.04.9]옥타코스-18-엔-2,3,10,16-테트라온인 용액 제제.
  6. 하기 일반식(Ⅰ)의 화합물 또는 이의 약학적으로 허용되는 염 및 약학적으로 허용되는 계면 활성제를 약학적으로 허용되는 비수용매중에 용해시킴을 특징으로 하여 용액 제제를 제조하는 방법;
    상기식에서, 치환기[R1및 R2],[R3및 R4]및[R5및 R6]의 각각의 근접 쌍은 독립적으로 a)두개의 근접 수소원자를 나타내거나 b)이들이 부착되어 있는 근접 탄소원자간에 제2결합을 형성하고; 상기 의미외에. R2는 알킬 그룹을 나타낼 수 있으며; R7은 H,OH, 보호된 하이드록시 또는 O-알킬을 나타내거나 R1과 함께 =O를 나타낼 수 있으며; R3및 R4는 독립적으로 H또는 OH를 나타내고; R10은 H, 알킬 하나이상의 하이드록실 그룹으로 치환된 알킬, 알케닐, 하나이상의 하이드록실 그룹으로 치환된 알케닐 또는 =O로 치환된 알킬이고; X는 O, (H,OH)(H,H) 또는 -CH2O-이고; Y는 O, (H,OH),(H,H)또는 N-NR11R12또는 N-OR13을 나타내고; R11및 R12는 독립적으로 H, 알킬, 아릴 또는 토실을 나타내고; R13,R14,R15,R16,R17,R18,R19,R22,및 R23은 독립적으로 H 또는 알킬이고; R20및 R21은 독립적으로 O를 나타내거나 (R20a,H)및(R21a,H)를 각각 나타낼 수 있으며; R20a및 R21a는 독립적으로 OH, O-알킬 또는 OCH2OCH2OCH2OH3를 나타내거나 R21a는 보호된 하이드록시이고; 또한 R20a및 R21a는 함께 에폭시드 고리내의 산소 원자를 나타낼 수 있으며; n은 1,2 또는 3이고; 상기 의미외에, Y,R10및R23은 이들이 부착되어 있는 탄소원자와 함께 5원 또는 6원 N-, S- 또는 O-함유 복소환식 고리를 나타낼 수 있으며, 이들은 포화 또는 불포화될 수 있고, 알킬, 하이드록시, 하나이상의 하이드록실 그룹으로 치환된 알킬 O-알킬, 벤질 및-CH2Se(C6H5)중에서 선택된 하나이상의 그룹으로 치환될 수 있다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910003135A 1990-03-01 1991-02-27 면역억제 활성을 갖는 트리사이클릭 화합물 함유 용액 제제 KR0177158B1 (ko)

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JP2-51110 1990-03-01
JP5111090 1990-03-01

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KR910016336A true KR910016336A (ko) 1991-11-05
KR0177158B1 KR0177158B1 (ko) 1999-03-20

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EP (1) EP0444659B1 (ko)
JP (1) JP2522121B2 (ko)
KR (1) KR0177158B1 (ko)
CN (1) CN1028961C (ko)
AT (1) ATE143598T1 (ko)
AU (1) AU642707B2 (ko)
CA (1) CA2037408C (ko)
DE (1) DE69122418T2 (ko)
DK (1) DK0444659T3 (ko)
ES (1) ES2093650T3 (ko)
GR (1) GR3021777T3 (ko)
HK (1) HK62797A (ko)
HU (2) HU209436B (ko)
IE (1) IE75221B1 (ko)
MX (1) MX9203032A (ko)
PT (1) PT96916B (ko)
RU (1) RU2028142C1 (ko)
SG (1) SG47986A1 (ko)
UA (1) UA51608C2 (ko)
ZA (1) ZA911502B (ko)

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MX9203032A (es) 1992-07-31
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PT96916B (pt) 1998-07-31
GR3021777T3 (en) 1997-02-28
HK62797A (en) 1997-05-16
CN1028961C (zh) 1995-06-21
AU7194991A (en) 1991-10-31
EP0444659A2 (en) 1991-09-04
ES2093650T3 (es) 1997-01-01
SG47986A1 (en) 1998-04-17
HU211502A9 (en) 1995-11-28
DE69122418D1 (de) 1996-11-07
ZA911502B (en) 1991-12-24
EP0444659A3 (en) 1991-12-18
JP2522121B2 (ja) 1996-08-07
CN1055110A (zh) 1991-10-09
PT96916A (pt) 1991-11-29
JPH04211012A (ja) 1992-08-03
RU2028142C1 (ru) 1995-02-09
IE910679A1 (en) 1991-09-11
CA2037408C (en) 2002-12-17
CA2037408A1 (en) 1991-09-02
KR0177158B1 (ko) 1999-03-20
HU209436B (en) 1994-06-28
DK0444659T3 (da) 1996-11-18
DE69122418T2 (de) 1997-03-06
UA51608C2 (uk) 2002-12-16
IE75221B1 (en) 1997-08-27
EP0444659B1 (en) 1996-10-02
ATE143598T1 (de) 1996-10-15
HUT57043A (en) 1991-11-28

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