KR960022486A - 신규 티아졸리딘-4-온 유도체 - Google Patents

신규 티아졸리딘-4-온 유도체 Download PDF

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KR960022486A
KR960022486A KR1019950061220A KR19950061220A KR960022486A KR 960022486 A KR960022486 A KR 960022486A KR 1019950061220 A KR1019950061220 A KR 1019950061220A KR 19950061220 A KR19950061220 A KR 19950061220A KR 960022486 A KR960022486 A KR 960022486A
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structural formula
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alkyl group
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박병욱
표성수
이기승
감종식
성진흥
박정수
박돈수
류근호
박정호
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김준웅
주식회사 선경인더스트리
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    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A61P5/12—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH for decreasing, blocking or antagonising the activity of the posterior pituitary hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/08—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D277/12—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
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    • 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems

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Abstract

본 발명은 혈소판 활성화인자(Platelet Activationg Factor; PAF)수용체 길항제, 5-리포옥시게나제 저해제 또는 혈소판 활성화인자 수용체 길항제와 5-리포옥시게나제 저해제의 이중적 장용에 의한 염증질환 및 알레르기질환의 예방과 치료에 유용한 다음 구조식(Ⅰ)로 표시되는 신규 티아졸리딘-4-온 유도체에 관한 것이다.
상기식에서, n, T, Q, R1, R2, R3, R4, R5,R6, R7및 R8은 각각 발명의 상세한 설명에서 정의한 바와 같다.

Description

신규 티아졸리딘-4-온 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (8)

  1. 다음 구조식(Ⅰ)로 표시되는 신규 티아졸리딘-4-온 유도체와 이의 산부기염.
    상기식에서, n은 0,1,2, 또는 3이고, Q는 C1∼C10의 알킬기, 치환되거나 치환되지 않은 페닐기로서 치환기로는 메톡시기 또는 니트로기, 또는 치환되거나 치환되지 않은 피리딜기로서 치환기로는 메틸기이고, R1,R2및 R3은 각각 서로 같거나 또는 다른 것으로서 수소원자, C1∼C10의 알킬기, C3∼C6의 시크로알킬기, 치환되거나 치환되지 않은 페닐기로서 치환기로는 메톡시기이고, R4, R5,R6,R7및 R8은 각각 서로 같거나 다른 것으로서 수소원자, 하이드록실기, 할로겐 원자, C1∼C10의 알킬기, C1∼C10의 알콕시기, 니트로기, 치환되거나 치환되지 않은 아미노기로서 치환기로는 C1∼C10의 알킬기 또는 C3-C6의 시클로알킬기, 치환되거나 치완되지 않은 페닐기로서 치환기로는 메톡시기 또는 니트로기, C1∼C10의 할로아릴기, 이고(이때, R15는 C1∼C10의 알킬기를 나타내고; m은 1,2,3, 또는 4를 나타냄), T는 수소원자, 하이드록시기, C1∼C10의 알킬기, 이다.
    이때, m은 1,2,3, 또는 4이고; R9는 수소원자, 치환되거나 치환되지 않은 페닐기로서 치환기로는 C1∼C6의 알킬기 또는 C1∼C6의 알콕시기, 또는 피리딜기이고; R10은 수소원자, C1-C10의 알킬기 또는 C1~C4의 알카노일기이고; R11은 C1~C10의 알킬기, C1~C10의 알콕시기, 또는 치환된 아미노기로서 치환기로는 C1∼C10의 알킬기 또는 C3∼C6의 시클로알킬이고; R12는 C1∼C10의 알킬기, 또는 페닐기이고; R13은 수소원자, C1∼C10의 알킬기 또는 C1∼C10의 알카노일기이고; R14는 수소원자, C1∼C10의 알킬기, 또는 R13과 R14가 서로 연결된 4∼7각형의 치환되거나 치환되지 않은 시클로아미노기 또는 또다른 헤테로원자를 선택적으로 포함하는 시클로아미노기로서 이때 치환기로는 C1∼C10의 알킬기 또는 C3∼C6의 시클로알킬기이고; R16은 수소원자 또는 C1∼C10의 알킬기이다.
  2. 다음 구조식(Ⅰ)로 표시되는 신규 티아졸리딘-4-온 유도체 또는 이의 산부가염을 유효성분으로 함유하는 약제조성물.
    상기식에서, n, T, Q, R1, R2, R3, R4, R5,R6, R7및 R8은 상기 제1항에서 정의한 바와같다.
  3. PAF로 인해서 유발되는 절환, 류코트리엔에 의해서 유발되는 질환 또는 PAF 및 류코트리엔에 의해서 유발되는 질환의 예방과 치료제로서의 다음 구조식(Ⅰ)로 표시되는 신규 티아졸리딘-4-온 유도체 또는 이의 산부가염의 용도.
    상기식에서, n, T, Q, R1, R2, R3, R4, R5,R6, R7및 R8은 상기 제1항에서 정의한 바와같다.
  4. 제3항에 있어서, 상기 PAF, 류코트리엔, 또는 PAF와 류코트리엔에 의해서 유발되는 질환으로는 관절염, 신장염, 쇼크, 혈전질환, 조직이식 거부반응질환, 뇌빈혈, 천식 또는 건선임.
  5. 다음 구조식(Ⅱ)로 표시되는 화합물과 다음 구조식(Ⅲ)으로 표시되는 화합물을 반응시켜 다음 구조식(Ⅰ)로 표시되는 티아졸리딘-4-온 유도체와 이의 산부가염을 제조하는 방법.
    상기식에서, n, T, Q, R1, R2, R3, R4, R5,R6, R7및 R8은 상기 제1항에서 정의한 바와같다.
  6. 다음 구조식(Ⅱ-Ⅰ)로 표시되는 화합물과 다음 구조식(Ⅲ)으로 표시되는 화합물을 반응시켜 다음 구조식(Ⅰ-1)로 표시되는 화합물을 제조한 후, 이를 산 또는 알카리 처리하여 다음 구조식(Ⅰ)로 표시되는 티아졸리딘-4-온 유도체와 이의 산부가염을 제조하는 방법.
    상기식에서, X는 할로겐원자를 나타내며, n, T, Q, R1, R2, R3, R4, R5,R6, R7및 R8은 상기 제1항에서 정의한 바와같다.
  7. 제6항에 있어서, 상기 구조식(Ⅱ-Ⅰ)로 표시되는 화합물과 다음 구조식(Ⅱ)로 표시되는 화합물로부터 제조된 것임.
    상기식에서, T, Q는 상기 제1항에서 정의한 바와 같다.
  8. 제7항에 있어서, 상기 구조식(Ⅱ)로 표시되는 화합물은 구조식(Ⅳ), (Ⅴ) 및 (Ⅶ)로 표시되는 화합물로부터 제조된 것임.
    상기식에서, T, Q는 상기 제1항에서 정의한 바와 같다.
    ※ 참고사항:최초출원 내용에 의하여 공개하는 것임.
KR1019950061220A 1994-12-29 1995-12-28 신규 티아졸리딘-4-온 유도체 KR960022486A (ko)

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EP (1) EP0748317A1 (ko)
JP (1) JPH09503792A (ko)
KR (1) KR960022486A (ko)
CN (1) CN1142227A (ko)
AU (1) AU4317396A (ko)
CA (1) CA2184174A1 (ko)
HU (1) HU9602263D0 (ko)
WO (1) WO1996020936A1 (ko)

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KR970032857A (ko) * 1995-12-29 1997-07-22 김준웅 약제 조성물

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EP1082315A1 (en) * 1998-06-05 2001-03-14 Icagen, Inc. Potassium channel inhibitors
US6174908B1 (en) 1999-05-10 2001-01-16 Icagen, Inc. Potassium channel inhibitors
AU4249700A (en) * 1999-04-19 2000-11-02 Sumitomo Pharmaceuticals Company, Limited Hydroxamic acid derivative
US6506751B1 (en) 1999-11-12 2003-01-14 Millennium Pharmaceuticals, Inc. Thiazolidinone compounds useful as chemokine inhibitors
US6713477B1 (en) 2000-04-19 2004-03-30 Sumitomo Pharmaceuticals Company, Limited Hydroxamic acid derivatives
AU2001284876A1 (en) * 2000-08-15 2002-02-25 South Alabama Medical Science Foundation Treating sickle cell disease
WO2002040021A2 (en) 2000-11-17 2002-05-23 Idenix (Cayman) Limited Methods for inhibiting the transmission of hiv using topically applied substituted 6-benzyl-4-oxopyrimidines
AU2002319677B8 (en) 2001-07-23 2009-04-30 Atwater Management Llc Cytoprotective compounds, pharmaceutical and cosmetic formulations, and methods
CN1596240A (zh) 2001-12-19 2005-03-16 阿特罗吉尼克斯公司 查耳酮衍生物及其治疗疾病的用途
WO2004108094A2 (en) 2003-06-06 2004-12-16 Atherogenics, Inc. Sulfonamide-substituted chalcone derivatives and their use to treat diseases
PL1689726T3 (pl) 2003-11-21 2011-05-31 Actelion Pharmaceuticals Ltd Pochodne 5-(benz-(z)-ylideno)tiazolidyn-4-onu jako środki immunosupresyjne
USRE43833E1 (en) 2003-11-21 2012-11-27 Actelion Pharmaceuticals Ltd. Thiazolidin-4-one derivatives
US7598240B2 (en) 2004-03-02 2009-10-06 Dainippon Sumitomo Pharma Co., Ltd. Benzothiazin-3-one compound and intermediate therefor
CN101541772B (zh) 2006-11-23 2013-04-17 埃科特莱茵药品有限公司 一种制备2-亚氨基-四氢噻唑-4-酮衍生物的新方法
US8912340B2 (en) 2006-11-23 2014-12-16 Actelion Pharmaceuticals Ltd. Process for the preparation of 2-imino-thiazolidin-4-one derivatives
CN104540800B (zh) 2012-08-17 2017-05-10 埃科特莱茵药品有限公司 制备(2z,5z)‑5‑(3‑氯‑4‑((r)‑2,3‑二羟基丙氧基)苯亚甲基)‑2‑(丙亚氨基)‑3‑(邻甲苯基)噻唑烷‑4‑酮的方法及在该方法中所用的中间产物
JP7412546B2 (ja) * 2019-10-02 2024-01-12 克洛索科学公司 抗老化遺伝子ｋｌｏｔｈｏの発現を誘導する化合物およびその用途

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ATE81123T1 (de) * 1987-11-20 1992-10-15 Hoechst Roussel Pharma 3-(4(1-substituierte-4-piperazinyl)butyl>-4thiazolidinone, verfahren zu deren herstellung und ihre anwendung als arzneimittel.
JPH01190679A (ja) * 1988-01-22 1989-07-31 Sumitomo Pharmaceut Co Ltd 光学活性な新規チアゾリジン−４−オン　誘導体およびその酸付加塩

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR970032857A (ko) * 1995-12-29 1997-07-22 김준웅 약제 조성물

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HU9602263D0 (en) 1996-10-28
CN1142227A (zh) 1997-02-05
WO1996020936A1 (en) 1996-07-11
JPH09503792A (ja) 1997-04-15
AU4317396A (en) 1996-07-24
EP0748317A1 (en) 1996-12-18

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