KR950702982A - 치환된 티아졸리딘디온 유도체(Substituted Thiazolidinedione Derivatives) - Google Patents

치환된 티아졸리딘디온 유도체(Substituted Thiazolidinedione Derivatives) Download PDF

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KR950702982A
KR950702982A KR1019950700873A KR19950700873A KR950702982A KR 950702982 A KR950702982 A KR 950702982A KR 1019950700873 A KR1019950700873 A KR 1019950700873A KR 19950700873 A KR19950700873 A KR 19950700873A KR 950702982 A KR950702982 A KR 950702982A
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pharmaceutically acceptable
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콜린 리플레이 풀
로빈 셔우드 로만
말콤 데이비드 브라이웰
알랜 윌리암 트렘퍼
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데이비드 로버츠
스미스클라인 비참 피엘씨(SmithKline Beecham plc)
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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

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  • Thiazole And Isothizaole Compounds (AREA)

Abstract

본 발명은 하기 일반식 (I)의 화합물, 또는 그의 토오토머 형태, 및(또는) 그의 제약학상 허용되는 용매화물에 관한 것이다.
상기 식 중에서, R1은 수소 원자, 알킬기, 아실기, 아릴킬기 (여기서, 아릴 잔기는 치환 또는 미치환될 수 있음), 또는 치환 또는 미치환 아릴기를 나타내고, A1은 수소, 또는 알킬, 알콕시, 아릴 및 할로겐으로 이루어지는 군 중에서 선택된 1 내지 4개의 임의 치환기이거나, A1은 이들이 결합하고 있는 탄소 원자와 함께, 치환 또는 미치환 아릴기를 형성하는 인접 탄소 원자 상의 2개의 치환기를 나타내고, A2는 1 내지 3개의 임의 치환기를 갖는 벤젠 고리를 나타내고, M-은 반대 이온을 나타낸다.
또한, 본 발명은 상기 화합물의 제조 방법, 상기 화합물로 이루어지는 제약 조성물, 및 의약으로서의 상기 화합물 및 조성물의 용도에 관한 것이다.

Description

치환된 티아졸리딘디온 유도체(Substituted Thiazolidinedione Derivatives)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (13)

  1. 하기 일반식 (I)의 화합물, 또는 그의 토오토머 형태, 및 (또는) 그의 제약학상 허용되는 용매화물.
    상기 식 중에서, R1은 수소, 알킬기, 아실기, 아랄킬기 (여기서, 아릴 잔기는 치환 또는 미치환될 수 있음), 또는 치환 또는 미치환 아릴기를 나타내고, A1은 수소, 또는 알킬, 알콕시, 아릴 및 할로겐으로 이루어지는 군 중에서 선택된 1 내지 4개의 임의 치환기이거나, A1은 이들이 결합하고 있는 탄소 원자와 함께, 치환 또는 미치환 아릴기를 형성하는, 인접 탄소 원자 상의 2개의 치환기를 나타내고, A2는 1 내지 3개의 임의 치환기를 갖는 벤젠 고리를 나타내고, M-은 반대 이온을 나타낸다.
  2. 제1항에 있어서, M-이 0.1 내지 4.5의 pKa을 갖는 제약학상 허용되는 산에 의해 제공되는 것인 화합물.
  3. 제1항 또는 제2항에 있어서, M-이 1.75 내지 2.5의 pK1을 갖는 제약학상 허용되는 산에 의해 제공되는 것인 화합물.
  4. 제1항 내지 제3항 중 어느 한 항에 잇어서, M-이 말레에이트 이온 HOOCCH=CHCOO-인 화합물.
  5. 제1항에 있어서, 5-[4-[2-(N-메틸-N-(2-피리딜)아미노)에톡시]벤벨]티아졸리딘-2,4-디온, 말레산염인 화합뭍.
  6. 하기 일반식(II)의 화합물을 반대 이온 M-의 공급원과 반응시키고, 이어서, 필요할 경우, 그의 제약학상 허용되는 용매화물을 제조하는 것으로 이루어지는 일반식(I)의 화합물, 또는 그의 토오토머 형태, 및(또는) 그의 제약학상 허용되는 용매화물의 제조 방법.
    상기 식 중에서, R1, A1및 A2은 일반식(I)에서 정의한 바와 같다.
  7. 제6항에 있어서, 반대 이온 M-의 공급원이 1.5 내지 4.5, 또는 1.75 내지 2.5의 pKa을 갖는 제약학상 허용되는 산을 포함하는 것인 방법.
  8. 제6항에 있어서, 반대 이온 M-의 공급원이 말레산인 방법.
  9. 일반식 (I)의 화합물, 또는 그의 토오토머 형태, 또는 그의 제약학상 허용되는 용매화물, 및 이들을 위한 제약학상 허용되는 담체로 이루어지는 제약 조성물.
  10. 활성 치료 물질로서 사용하기 위한 일반식 (I)의 화합물, 또는 그의 토오토머 형태, 및(또는) 그의 제약학상 허용되는 용매화물.
  11. 고혈당증, 고지혈증, 고혈압, 심장 혈관 질환 및 특정 섭취 장애의 치료 및 (또는) 예방에 사용하기 위한 일반식 (I)의 화합물, 또는 그의 토오토머 형태, 및 (또는) 그의 제약학상 허용되는 용매화물.
  12. 고혈당증, 고지혈증, 고혈압, 심장 혈관 질환 및 특정 섭취 장애의 치료 및 (또는) 예방이 필요한 사람 또는 다른 포유 동물에게, 비독성인 유효량의 일반식 (I)의 화합물, 또는 그의 토오토머 형태, 및(또는) 그의 제약학상 허용되는 용매화물을 투여하는 것으로 이루어지는 사람 또는 다른 포유 동물의 고혈당증, 고지혈증, 고혈압, 심장 혈관 및 특정 섭취 장애의 치료 및(또는) 예방 방법.
  13. 고혈당증, 고지혈증, 고혈압, 심장 혈관 질환 및 특정 섭취 장애의 치료 및 (또는) 예방용 의약을 제조하기 위한 일반식 (I)의 화합물, 또는 그의 토오토머 형태, 및 (또는) 그의 제약학상 허용되는 용매화물의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950700873A 1992-09-05 1993-09-01 치환된티아졸리딘디온유도체 KR100371297B1 (ko)

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GB9218830.9 1992-09-05
GB929218830A GB9218830D0 (en) 1992-09-05 1992-09-05 Novel compounds

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KR950702982A true KR950702982A (ko) 1995-08-23
KR100371297B1 KR100371297B1 (ko) 2003-05-09

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KR1020027006870A KR20030097596A (ko) 1992-09-05 1993-09-01 치환된 티아졸리딘디온 유도체
KR1020087020116A KR20080081099A (ko) 1992-09-05 1993-09-01 치환된 티아졸리딘디온 유도체
KR1019950700873A KR100371297B1 (ko) 1992-09-05 1993-09-01 치환된티아졸리딘디온유도체

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KR1020027006870A KR20030097596A (ko) 1992-09-05 1993-09-01 치환된 티아졸리딘디온 유도체
KR1020087020116A KR20080081099A (ko) 1992-09-05 1993-09-01 치환된 티아졸리딘디온 유도체

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US (1) US5910592A (ko)
EP (2) EP0960883A1 (ko)
JP (5) JP2828777B2 (ko)
KR (3) KR20030097596A (ko)
CN (4) CN1040323C (ko)
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ES (1) ES2133410T3 (ko)
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GB (1) GB9218830D0 (ko)
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RU (3) RU2128179C1 (ko)
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UA (1) UA41901C2 (ko)
WO (1) WO1994005659A1 (ko)
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CZ298812B6 (cs) 1996-07-01 2008-02-13 Dr. Reddy's Laboratories Limited Azolidindionové deriváty, způsob jejich přípravy, farmaceutické kompozice s jejich obsahem a jejich použití v léčbě diabetu a příbuzných nemocí
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