KR940002210A - 24-시클로프로판 비타민 d 유도체 - Google Patents

24-시클로프로판 비타민 d 유도체 Download PDF

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KR940002210A
KR940002210A KR1019930012709A KR930012709A KR940002210A KR 940002210 A KR940002210 A KR 940002210A KR 1019930012709 A KR1019930012709 A KR 1019930012709A KR 930012709 A KR930012709 A KR 930012709A KR 940002210 A KR940002210 A KR 940002210A
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compound
hydrogen
vitamin
disease
bone
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KR1019930012709A
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KR100273182B1 (ko
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에프. 델루카 헥터
나오시 나까가와
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존 알. 파이크
위스콘신 앨럼나이 리써치파운데이션
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C401/00—Irradiation products of cholesterol or its derivatives; Vitamin D derivatives, 9,10-seco cyclopenta[a]phenanthrene or analogues obtained by chemical preparation without irradiation

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Rheumatology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

본 발명은 lα, 25-디히드록시비타민 D2및 lα-히드록시 비타민 D2의 측쇄의 24번 탄소에 시플로프로판 고리가 도입된 비타민 D2동족체에 관한 것이다. 상기의 화합물은 lα,25-디히드록시비타민 D2와 비교하여 뼈로 부터의 칼슘 이동능은 매우 낮은 반면 현저하게 높은 장내 칼슘 수송능을 나타내는 것으로 특징지워진다. 상기의 화합물은 이러한 바람직한 칼슘 활성이 있으므로 골다공증 등 뼈의 형성이 목적인 질환의 치료에 유용할 것이다.

Description

24-시클로프로판 비타민 D 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (16)

  1. 하기 일반식의 화합물
    상기 식중, R1은 수소 또는 히드록시기일 수 있다.
  2. 24,28-메틸렌-la,25-디히드록시비타민 D2.
  3. 24,28｜메틸렌-lα-디히드록시비타민 D2.
  4. 뼈의 대사성 질환의 있는 환자에게 하기 일반식의 화합물을 투여하는 것으로 이루어지는, 뼈의 질량의 유지 및 상승을 필요로 하는 뼈의 대사성 질환의 치료방법.
    상기 식중, R1은 수소 또는 히드록시기일 수 있다.
  5. 제4항에 있어서, 질환이 골다공증인 치료방법.
  6. 제4항에 있어서, 질환이 골연화증인 치료방법.
  7. 제4항에 있어서, 질환이 신성 골이영양증인 치료방법.
  8. 제4항에 있어서, 화합물이 경구 투여되는 치료방법.
  9. 제4항에 있어서, 화합물이 비경구 투여되는 치료방법.
  10. 제4항에 있어서, 화합물이 경피 투여되는 치료방법.
  11. 제4항에 있어서, 화합물이 1일 0.5㎍내지 50㎍의 용량으로 투여되는 치료방법.
  12. 하기 일반식의 화합물.
    상기식중, R2은 수소 또는 히드록시기일 수 있고, R3은 히드록시기 보호기일 수 있고, R4은 수소 또는 히드록시기일 수일 수 있다.
  13. 제12항에 있어서, R2및 R4가 모두 수소이고, R3가 히드록시 보호기인 화합물.
  14. 제1항에 급한 1종 이상의 화합물을 제약학적으로 허용 가능한 부형제와 함께 함유하는 제약학적 조성물.
  15. 제14항에 있어서, 24,28-메틸렌-lα,25-디히드록시비타민 D2를 약 0.5㎍내지 50㎍의 양으로 함유하는 제약학적 조성물.
  16. 제14항에 있어서, 24,28-디메틸렌-lα-디히드록시비타민 D2를 약 0.5㎍내지 5㎍의 양으로 함유하는 제약학적 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019930012709A 1992-07-08 1993-07-07 24-시클로프로판 비타민 d 유도체 KR100273182B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US7/910,423 1992-07-08
US07/910,423 US5194431A (en) 1992-07-08 1992-07-08 24-cyclopropane vitamin D derivatives

Publications (2)

Publication Number Publication Date
KR940002210A true KR940002210A (ko) 1994-02-16
KR100273182B1 KR100273182B1 (ko) 2000-12-01

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US (1) US5194431A (ko)
EP (1) EP0578494B1 (ko)
JP (1) JP3253425B2 (ko)
KR (1) KR100273182B1 (ko)
AT (1) ATE123767T1 (ko)
AU (1) AU659745B2 (ko)
DE (1) DE69300196T2 (ko)
IL (1) IL106167A (ko)

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DE4220757A1 (de) * 1992-06-24 1994-01-05 Schering Ag Derivate in der Vitamin D-Reihe mit Modifikationen in der 20-Position, Verfahren zu ihrer Herstellung, Zwischenprodukte für dieses Verfahren, diese Derivate enthaltende pharmazeutische Präparate sowie deren Verwendung zur Herstellung von Arzneimitteln
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RU2559084C2 (ru) * 2009-12-22 2015-08-10 Лео Фарма А/С Фармацевтическая композиция, включающая растворяющую смесь и производное или аналог витамина d
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JP3253425B2 (ja) 2002-02-04
IL106167A0 (en) 1993-10-20
ATE123767T1 (de) 1995-06-15
US5194431A (en) 1993-03-16
KR100273182B1 (ko) 2000-12-01
IL106167A (en) 1998-08-16
DE69300196T2 (de) 1995-10-19
AU659745B2 (en) 1995-05-25
JPH0672995A (ja) 1994-03-15
AU4181793A (en) 1994-01-13
EP0578494B1 (en) 1995-06-14
DE69300196D1 (de) 1995-07-20
EP0578494A1 (en) 1994-01-12

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