KR960700708A - 3,4-디아릴크로만을 이용한 뼈 손실의 억제방법(methdos for inhibiting bone loss with 3,4-diarylchroman) - Google Patents

3,4-디아릴크로만을 이용한 뼈 손실의 억제방법(methdos for inhibiting bone loss with 3,4-diarylchroman) Download PDF

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KR960700708A
KR960700708A KR1019950703749A KR19950703749A KR960700708A KR 960700708 A KR960700708 A KR 960700708A KR 1019950703749 A KR1019950703749 A KR 1019950703749A KR 19950703749 A KR19950703749 A KR 19950703749A KR 960700708 A KR960700708 A KR 960700708A
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South Korea
Prior art keywords
compound
lower alkoxy
lower alkyl
independently hydrogen
hydrogen
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KR1019950703749A
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KR100263009B1 (ko
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엠. 라브루 비렌더
알. 피고트 제임스
디. 베인 스티븐
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마크 제이. 머레이
자이모제네틱스 인코오퍼레이티드
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Priority claimed from PCT/US1994/000663 external-priority patent/WO1994015704A1/en
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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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • 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
    • 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
    • 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

Abstract

뼈 손실을 감소시키는 방법 및 약학조성물이 개시되어 있다. 3,4-디아릴크로만 및 약학적으로 허용가능한 이들의 염은 골다공증 또는 다른 이상에 기인한 뼈 손실의 치료제로 조제된다. 전형적인 3,4-디아릴크로만은 센트크로만(3,4-트랜스-2,2-디메틸-3-페닐-4-[p-(베타-피롤리디노에톡시)페닐]-7-메톡시-크로만)이다. 조제물은 정제 및 경구투여에 적당한 다른 형태와 서방성 피하이식편을 포함한다.

Description

3,4-디아릴크로만을 이용한 뼈 손실의 억제방법(METHDOS FOR INHIBITING BONE LOSS WITH 3,4-DIARYLCHROMAN)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (25)

  1. 환자의 뼈 손실을 감소시키는 방법에 있어서, 골다공증, 파게트 질환 또는 상피소체 기능항진증에 기인하는 뼈 손실을 앓는 환자에게 약학적으로 허용가능한 담체와 조합하여 뼈 손실을 억제하는 다음 식의 화합물 또는 약학적으로 허용가능한 이들의 염으로 이루어진 조성물의 유효량을 투여하는 것으로 이루어지는 방법 :
    여기에서 R1, R4 및 R5는 독립적으로 수소, 히드록시, 할로, 트리플루오로메틸, 저급알킬, 저급알콕시 또는 3차 아미노 저급알콕시이고; R2 및 R3은 독립적으로 수소 또는 저급알킬이다.
  2. 제1항에 있어서, R1은 저급알콕시, R2와 R3은 저급알킬, R4는 수소, 및 R5는 3차 아미노 저급알콕시인 것을 특징으로 하는 방법.
  3. 제1항에 있어서, R1은 메톡시인 것을 특징으로 하는 방법.
  4. 제1항에 있어서, R2와 R3은 메틸인 것을 특징으로 하는 방법.
  5. 제1항에 있어서, R4는 수소인 것을 특징으로 하는 방법.
  6. 제1항에 있어서, R5는인 것을 특징으로 하는 방법.
  7. 제1항에 있어서, 상기 화합물은 분리된 d- 또는 ℓ-거울상체인 것을 특징으로 하는 방법.
  8. 제1항에 있어서, 상기 화합물은
    인 것을 특징으로 하는 방법.
  9. 제1항에 있어서, 상기 화합물은
    인 것을 특징으로 하는 방법.
  10. 제9항에 있어서, 상기 화합물은 분리된 d- 또는 ℓ-거울상체인 것을 특징으로 하는 방법.
  11. 제1항에 있어서, 상기 환자는 폐경기후 여성인 것을 특징으로 하는 방법.
  12. 제1항에 있어서, 상기 조성물은 경구투여에 적당한 형태인 것을 특징으로 하는 방법.
  13. 제1항에 있어서, 상기 화합물은 0.1-5.0㎎/환자체중 ㎏/day의 투여량으로 투여되는 것을 특징으로 하는 방법.
  14. 제1항에 있어서, 상기 조성물은 매일 내지 매주 간격으로 투여되는 것을 특징으로 하는 방법.
  15. 제1항에 있어서, 상기 조성물은 피하이식편의 형태인 것을 특징으로 하는 방법.
  16. 골다공증을 치료하는 방법에 있어서, 뼈 손실은 억제하는 다음식의 화합물 또는 약학적으로 허용가능한 이들의 염의 분리된 d- 또는 ℓ-거울상체를 뼈 재흡수를 억제하는 충분한 양으로 환자에게 투여하는 것으로 이루어지는 방법.
    여기에서 R1, R4 및 R5는 독립적으로 수소, 히드록시, 할로, 트리플루오로메틸, 저급알킬, 저급알콕시 또는 3차 아미노 저급알콕시이고; R2 및 R3은 독립적으로 수소 또는 저급알킬이다.
  17. 제16항에 있어서, R1은 저급알콕시, R2와 R3은 저급알킬, R4는 수소, 및 R5는 3차 아미노 저급알콕시인 것을 특징으로 하는 방법.
  18. 제16항에 있어서, R1은 메톡시인 것을 특징으로 하는 방법.
  19. 제16항에 있어서, R2와 R3은 메틸인 것을 특징으로 하는 방법.
  20. 제16항에 있어서, R4는 수소인 것을 특징으로 하는 방법.
  21. 제16항에 있어서, R5는인 것을 특징으로 하는 방법.
  22. 제16항에 있어서, 상기 화합물은
    인 것을 특징으로 하는 방법.
  23. 제16항에 있어서, 상기 화합물은
    인 것을 특징으로 하는 방법.
  24. 제16항에 있어서, 상기 환자는 폐경기후 여성인 것을 특징으로 하는 방법.
  25. 골다공증, 파게트 질환 또는 상피소체기능항진증에 기인한 뼈 손실의 치료를 위한 약학조성물의 제조에 있어서, 다음 식 화합물의 이용 :
    여기에서 R1, R4 및 R5는 독립적으로 수소, 히드록시, 할로, 트리플루오로메틸, 저급알킬, 저급알콕시 또는 3차 아미노 알콕시이고; R2 및 R3은 독립적으로 수소 또는 저급알킬이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950703749A 1993-03-11 1994-01-13 3,4-디아릴크로만을 포함하는 뼈 손실 억제에 유용한 조성물 KR100263009B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US08/029,729 1993-03-11
US08/029,729 US5280040A (en) 1993-03-11 1993-03-11 Methods for reducing bone loss using centchroman derivatives
US8/029729 1993-03-11
PCT/US1994/000663 WO1994015704A1 (en) 1993-01-15 1994-01-14 Mixing apparatus

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KR960700708A true KR960700708A (ko) 1996-02-24
KR100263009B1 KR100263009B1 (ko) 2000-08-01

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EP (1) EP0688214B1 (ko)
JP (1) JP2834581B2 (ko)
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AT (1) ATE178488T1 (ko)
AU (2) AU674394B2 (ko)
BR (1) BR9405843A (ko)
CA (1) CA2157879C (ko)
CZ (1) CZ287603B6 (ko)
DE (1) DE69417733T2 (ko)
DK (1) DK0688214T3 (ko)
ES (1) ES2131678T3 (ko)
GR (1) GR3030128T3 (ko)
HU (1) HUT74575A (ko)
NO (1) NO309361B1 (ko)
NZ (1) NZ262569A (ko)
RU (1) RU2166940C2 (ko)
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JP2834581B2 (ja) 1998-12-09
KR100263009B1 (ko) 2000-08-01
EP0688214A1 (en) 1995-12-27
AU674394B2 (en) 1996-12-19
BR9405843A (pt) 1996-01-16
JPH08506346A (ja) 1996-07-09
CZ287603B6 (en) 2001-01-17
NZ262569A (en) 1997-08-22
AU1639497A (en) 1997-05-22
CA2157879C (en) 2000-08-29
DE69417733D1 (de) 1999-05-12
CA2157879A1 (en) 1994-09-12
CZ232095A3 (en) 1996-04-17
GR3030128T3 (en) 1999-07-30
US5464862A (en) 1995-11-07
AU695497B2 (en) 1998-08-13
WO1994020098A1 (en) 1994-09-15
NO953542D0 (no) 1995-09-08
HU9502624D0 (en) 1995-11-28
RU2166940C2 (ru) 2001-05-20
NO309361B1 (no) 2001-01-22
DE69417733T2 (de) 1999-09-16
HUT74575A (en) 1997-01-28
ATE178488T1 (de) 1999-04-15
SG65584A1 (en) 1999-06-22
AU6230294A (en) 1994-09-26
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DK0688214T3 (da) 2000-10-09

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