KR970010742A - 프로스타글란딘 유도체 - Google Patents

프로스타글란딘 유도체 Download PDF

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KR970010742A
KR970010742A KR1019960033503A KR19960033503A KR970010742A KR 970010742 A KR970010742 A KR 970010742A KR 1019960033503 A KR1019960033503 A KR 1019960033503A KR 19960033503 A KR19960033503 A KR 19960033503A KR 970010742 A KR970010742 A KR 970010742A
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compound
formula
prostaglandin
derivative
liposome
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KR1019960033503A
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KR100225689B1 (ko
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아키오 니시우라
타쿠야 세코
라이오지 마쯔모토
신이치 하마노
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우에노 도시오
오노 야쿠힝 고교 가부시키가이샤
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    • 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
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Liposomes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C405/00—Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins ; Analogues or derivatives thereof
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    • C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C08B37/0006—Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid
    • C08B37/0009—Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid alpha-D-Glucans, e.g. polydextrose, alternan, glycogen; (alpha-1,4)(alpha-1,6)-D-Glucans; (alpha-1,3)(alpha-1,4)-D-Glucans, e.g. isolichenan or nigeran; (alpha-1,4)-D-Glucans; (alpha-1,3)-D-Glucans, e.g. pseudonigeran; Derivatives thereof
    • C08B37/0012—Cyclodextrin [CD], e.g. cycle with 6 units (alpha), with 7 units (beta) and with 8 units (gamma), large-ring cyclodextrin or cycloamylose with 9 units or more; Derivatives thereof
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    • C08B37/0009—Homoglycans, i.e. polysaccharides having a main chain consisting of one single sugar, e.g. colominic acid alpha-D-Glucans, e.g. polydextrose, alternan, glycogen; (alpha-1,4)(alpha-1,6)-D-Glucans; (alpha-1,3)(alpha-1,4)-D-Glucans, e.g. isolichenan or nigeran; (alpha-1,4)-D-Glucans; (alpha-1,3)-D-Glucans, e.g. pseudonigeran; Derivatives thereof
    • C08B37/0012—Cyclodextrin [CD], e.g. cycle with 6 units (alpha), with 7 units (beta) and with 8 units (gamma), large-ring cyclodextrin or cycloamylose with 9 units or more; Derivatives thereof
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Abstract

본 발명은 하기 화학식 (1)의 프로스타글란딘 E1에스테르 유도체 및 이의 시클로덱스트린 포접 화합물, 그들을 포함하는 리포좀 제제, 그들 제제의 제조방법 및 그들을 활성성분으로 포함하는 약학 조성물에 관한 것이다 :
상기 식에서, R은 (ⅰ) -CH2CH2-O-CO-R1또는 (ⅱ) -CH2CH2-O-CO-CH2-O-R2이고, R1및 R2는 각각 개별적으로 C10-20알킬이다.
상기 화학식 (1)의 화합물은 혈류 증가 효과를 보유하며, 말초 순환 장애, 욕창 또는 피부 궤양의 예방 및/또는 치료, 또는 혈류(blood flow) 유지에 유용하다.

Description

프로스타글란딘 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 하기 화학식 (1)의 프로스타글란딘 E1에스테르 유도체 및 이의 시클로덱스트린 포접 화합물 :
    상기 식에서, R은 (ⅰ) -CH2CH2-O-CO-R1또는 (ⅱ) -CH2CH2-O-CO-CH2-O-R2이고, R1및 R2는 각각 개별적으로 C10-20알킬이다.
  2. 제1항에 있어서, R이 (ⅰ) -CH2CH2-O-CO-R1이고, R1이 C10-12알킬인 화합물.
  3. 제1항에 있어서, R이 (ⅱ) -CH2CH2-O-CO-CH2-O-R2이고, R2가 C11-17 알킬인 화합물.
  4. 제2항에 있어서, 상기 화합물이 PGE12-(도데카노일옥시)에틸 에스테르인 화합물.
  5. 제3항에 있어서, 상기 화합물이 PGE12-(도데실옥시아세톡시)에틸 에스테르 또는 PGE12-(헥사데실옥시아세톡시)에틸 에스테르인 화합물.
  6. 제1항 내지 제5항 중 어느 한 항에서 정의한 바와 같은 화학식 (1)의 프로스타글란딘 E1유도체와 리포좀막 재료를 1 : 1 내지 1 : 400의 비로 함유하는 리포좀 제제.
  7. 제6항에 있어서, 상기 리포좀 막 재료가 디미리스토일포스파티딜콜린을 함유하는 리포좀 제제.
  8. 제6항에 있어서, 상기 리포좀 막 재료가 에그 레시틴을 함유하는 리포좀 제제.
  9. 제6항 내지 제8항 중 어느 한 항에 있어서, 동결 건조에 의해 수득할 수 있는 리포좀 제제.
  10. 하기 화학식 (2)의 화합물이 R3기를 제거하여 하기 화학식 (1)의 화합물을 제조하고, 필요에 따라 이렇게 수득한 화학식 (1)의 화합물을 이의 포접 화합물로 전환시키는 단계를 포함하는 하기 화학식 (1)의 화합물 또는 이의 포접 화합물의 제조방법 :
    상기 식에서, R은 제1항에서 정의한 바와 동일하다.
    상기 식에서, R은 상기 정의한 바와 동일하며, R3은 산성 조건하에서 제거될 수 있는 히드록실-보호기이다.
  11. 활성성분으로 제1항 내지 제5항 중 어느 한 항에서 정의한 바와 같은 화학식 (1)의 프로스타글란딘 E1유도체 또는 이의 시클로덱스트린 포접 화합물과 약학적으로 허용가능한 담체를 함유하는 말초 순환 장애, 욕창 또는 피부 궤양을 예방 및/또는 치료하기 위한 약학 조성물.
  12. 활성성분으로 제1항 내지 제5항 중 어느 한 항에서 정의한 바와 같은 화학식 (1)의 프로스타글란딘 E1유도체 또는 이의 시클로덱스트린 포접 화합물과 약학적으로 허용가능한 담체를 함유하는 혈관 복원 수술후 혈류 유지를 위한 약학 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960033503A 1995-08-16 1996-08-13 프로스타글란딘 유도체(prostaglandin derivatives) KR100225689B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP95-230763 1995-08-16
JP23076395 1995-08-16

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KR970010742A true KR970010742A (ko) 1997-03-27
KR100225689B1 KR100225689B1 (ko) 1999-10-15

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US (1) US5690957A (ko)
EP (1) EP0758645B1 (ko)
KR (1) KR100225689B1 (ko)
CN (1) CN1058706C (ko)
AT (1) ATE185559T1 (ko)
AU (1) AU708905B2 (ko)
CA (1) CA2183486C (ko)
DE (1) DE69604631T2 (ko)
DK (1) DK0758645T3 (ko)
ES (1) ES2140032T3 (ko)
GR (1) GR3032274T3 (ko)
HU (1) HUP9602262A3 (ko)
MX (1) MX9603452A (ko)
NO (1) NO309086B1 (ko)
TW (1) TW367324B (ko)
ZA (1) ZA966934B (ko)

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Publication number Priority date Publication date Assignee Title
DE112006000921T5 (de) * 2005-04-13 2008-05-08 Elan Pharma International Ltd., Athlone Nanopartikuläre Zusammensetzungen zur kontrollierten Freisetzung, die Prostaglandin-Derivate umfassen
CN1813679A (zh) * 2005-11-30 2006-08-09 上海医药(集团)有限公司 一种紫杉烷脂质体冻干组合物及其制备方法
JP5131971B2 (ja) * 2005-12-26 2013-01-30 株式会社Ｌｔｔバイオファーマ 水溶性非ペプチド性低分子薬物含有ナノ粒子
CN101379051B (zh) * 2006-02-07 2014-05-28 株式会社·R-技术上野 用于制备前列腺素衍生物的方法
EP2156848A4 (en) * 2007-05-14 2012-11-28 Ltt Bio Pharma Co Ltd NANOPARTICLE CONTAINING A LOW MOLECULAR WEIGHT DRUG HAVING A NEGATIVELY PROLONGED RELEASE GROUP
ITCA20080017A1 (it) * 2008-07-31 2010-02-01 Giuseppe Brotzu Farmaco a base di liposomi di fosfatidilcolina trasportanti una prostaglandina e1 legata alla alfa-ciclodestrina per il trattamento delle microngiopatie diabetiche e altre patologie vascolari.
US20110262548A1 (en) * 2008-11-18 2011-10-27 Ltt Bio-Pharma Co., Ltd. Novel prostaglandin e1 derivative and nanoparticle having the same encapsulated therein
JP2012528077A (ja) * 2009-05-27 2012-11-12 スキャンポ・アーゲー クローディン媒介機能の調節および皮膚疾患の処置に使用するための、プロスタグランジン誘導体を含む医薬組成物
US8569279B2 (en) 2009-05-27 2013-10-29 Sucampo Ag Method for modulating claudin mediated functions
CN102028696B (zh) * 2009-09-24 2013-02-13 上海天伟生物制药有限公司 一种前列腺素类化合物的用途
CN101912363A (zh) * 2010-07-29 2010-12-15 蔡海德 溶解超滤-喷雾干燥-分子分散包衣-水化制粒-冷冻干燥生产脂质体组合药物

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4054736A (en) * 1970-06-10 1977-10-18 Ono Pharmaceutical Co., Ltd. Clathrate compounds of prostaglandins or their analogues with cyclodextrin
JPS59206349A (ja) * 1983-05-10 1984-11-22 Green Cross Corp:The プロスタグランジンｅ↓１誘導体

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Publication number Publication date
EP0758645B1 (en) 1999-10-13
NO963408D0 (no) 1996-08-15
KR100225689B1 (ko) 1999-10-15
CN1151398A (zh) 1997-06-11
AU708905B2 (en) 1999-08-12
HU9602262D0 (en) 1996-10-28
DE69604631T2 (de) 2000-02-17
AU6210596A (en) 1997-02-20
ATE185559T1 (de) 1999-10-15
NO963408L (no) 1997-02-17
NO309086B1 (no) 2000-12-11
CA2183486A1 (en) 1997-02-17
GR3032274T3 (en) 2000-04-27
DK0758645T3 (da) 1999-12-27
HUP9602262A3 (en) 1997-08-28
CA2183486C (en) 2002-03-26
HUP9602262A2 (en) 1997-05-28
TW367324B (en) 1999-08-21
MX9603452A (es) 1997-03-29
DE69604631D1 (de) 1999-11-18
ES2140032T3 (es) 2000-02-16
US5690957A (en) 1997-11-25
CN1058706C (zh) 2000-11-22
EP0758645A1 (en) 1997-02-19
ZA966934B (en) 1997-02-19

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