KR950031068A - 골다공증의 복합 치료 - Google Patents

골다공증의 복합 치료 Download PDF

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KR950031068A
KR950031068A KR1019950001289A KR19950001289A KR950031068A KR 950031068 A KR950031068 A KR 950031068A KR 1019950001289 A KR1019950001289 A KR 1019950001289A KR 19950001289 A KR19950001289 A KR 19950001289A KR 950031068 A KR950031068 A KR 950031068A
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compound
alkoxy
formula
pharmaceutically acceptable
substituted
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KR1019950001289A
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존 블랙 래리
조셉 쿨리난 죠지
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피터 지. 스트링거
일라이 릴리 앤드 캄파니
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Publication of KR950031068A publication Critical patent/KR950031068A/ko

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/4025Heterocyclic 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

본 발명은 1) 하기 일반식(Ⅰ)의 화합물 또는 그의 약학적으로 허용가능한 염 또는 용매화물을; 2) 메드록시 프로게스테론, 노르에틴드론 또는 노르에티노드렐 중에서 선택된 프로게스틴 또는 그의 약학적으로 허용가능한 염과 함께; 상기 복합물을 유지시키거나 또는 골 밀도를 증가시키는 양으로 투여함을 포함하는 신규한 골다공증의 치료방번을 제공한다:
상기 식에서 R 및 R1은 독립적으로 수소, 하이드록실, C1-C6알콕시, C1-C6아실옥시, C1-C6알콕시-C2-C6아실옥시, R2-치환된 아릴옥시, R2-치환된 아로일옥시, R3-치환된 카보닐 옥시 또는 할로이고; R2는 C1-C6알킬, C1-C6알콕시, 수소 또는 할로이고; R3는 C1-C6알콕시 또는 아릴옥시이고; n은 2, 3 또는 4이고, p는 4, 5 또는 6이다.
본 발명은 또한 1) 일반식 (Ⅰ)의 화합물 또는 그의 약학적으로 허용가능한 염 또는 용해화물; 및 2) 메드록시 프로게스테론, 노르에틴드론 또는 노르에티노드렐중에서 선택된 프로게스틴 또는 그의 약학적으로 허용가능한 염을; 하나이상의 약학적으로 허용가능한 담체와 함께 상기 복합물이 골 손실을 억제시키는 양으로 포함하는, 골 손실 억제를 위한 약학 조성물을 제공한다.

Description

골다공증의 복합 치료
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (6)

  1. 골 밀도의 유지 또는 증가, 또는 골 손실의 억제를 위해 복합적으로 사용하기 위한, 하기 일반식(Ⅰ)의 화합물 또는 그의 약학적으로 허용가능한 염 또는 용매화물, 및 메드록시프로게스테론, 노르에틴드론 또는 노르에티노드렐중에서 선택된 프로게스틴 또는 그의 약학적으로 허용가능한 염:
    상기 식에서 R 및 R1은 독립적으로 수소, 하이드록실, C1-C6알콕시,C1-C6아실옥시, C1-C6알콕시-C2-C6아실옥시, R2-치환된 아릴옥시, R2-치환된 아로일옥시, R3-치환된 카보닐옥시 또는 할로이고; R2는 C1-C6알킬, C1-C6알콕시, 수소 또는 할로이고; R3는 C1-C6알콕시 또는 아릴옥시이고; n은 2, 3 또는 4이고, p는 4, 5 또는 6이다.
  2. 제1항에 있어서, 일반식(Ⅰ) 화합물이, R 및 R1이 하이드록실, C1-C6아릴옥시, C1-C6알콕시-C2-C6아릴옥시, R2-치환된 아로일옥시, 또는 R3-치환된 카보닐옥시인 화합물이고; 선택된 프로게스틴이 노르에틴드론 또는 노르에티노드렐인 화합물.
  3. 제2항에 있어서, 일반식 (Ⅰ)화합물이, R 및 R1이 하이드록실이고, n이2고, p가 4 또는 5인 화합물이고; 선택된 프로게스틴이 노르에틴드론인 화합물.
  4. 제3항에 있어서, 일반식( I )화합물이, p가 5인 화합물인 화합물.
  5. 제2항에 있어서, 일반식( I )화합물이, R 및 R1이 하이드록실이고, n이 2이고, p가 5인 화합물이고; 선택된 프로게스틴이 노르에티노드렐인 화합물.
  6. 제1항에 있어서, 상기 일반식( I )화합물의 투여량이 0.1 내지 약 1000mg/체중kg이고, 상기 선택된 프로게스틴의 투여량이 약 0.01 내지 약 500mg/체중kg인 화합물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950001289A 1994-01-28 1995-01-25 골다공증의 복합 치료 KR950031068A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/189,399 1994-01-28
US08/189,399 US5591753A (en) 1994-01-28 1994-01-28 Combination treatment for osteoporosis

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US (2) US5591753A (ko)
EP (1) EP0665015A3 (ko)
JP (1) JPH07267858A (ko)
KR (1) KR950031068A (ko)
CN (1) CN1084617C (ko)
AU (1) AU692811B2 (ko)
CA (1) CA2140952A1 (ko)
CZ (1) CZ290045B6 (ko)
HU (1) HUT72633A (ko)
IL (1) IL112455A (ko)
NO (1) NO950275L (ko)
NZ (1) NZ270386A (ko)
PH (1) PH31553A (ko)
RU (1) RU2181048C2 (ko)
TW (1) TW401296B (ko)
UA (1) UA29451C2 (ko)
ZA (1) ZA95556B (ko)

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NO950275L (no) 1995-07-31
CN1084617C (zh) 2002-05-15
IL112455A0 (en) 1995-03-30
US5591753A (en) 1997-01-07
RU2181048C2 (ru) 2002-04-10
ZA95556B (en) 1996-07-24
EP0665015A2 (en) 1995-08-02
PH31553A (en) 1998-11-03
IL112455A (en) 1999-12-31
TW401296B (en) 2000-08-11
CN1111511A (zh) 1995-11-15
US5646137A (en) 1997-07-08
CZ17695A3 (en) 1995-10-18
NO950275D0 (no) 1995-01-25
AU1139095A (en) 1995-08-10
EP0665015A3 (en) 1998-04-08
AU692811B2 (en) 1998-06-18
CZ290045B6 (cs) 2002-05-15
CA2140952A1 (en) 1995-07-29
NZ270386A (en) 1996-09-25
HUT72633A (en) 1996-05-28
UA29451C2 (uk) 2000-11-15
JPH07267858A (ja) 1995-10-17
HU9500229D0 (en) 1995-03-28

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