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KR930016402A - 항-hiv 활성을 갖는 이미다졸 유도체 - Google Patents

항-hiv 활성을 갖는 이미다졸 유도체 Download PDF

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KR930016402A
KR930016402A KR1019930000496A KR930000496A KR930016402A KR 930016402 A KR930016402 A KR 930016402A KR 1019930000496 A KR1019930000496 A KR 1019930000496A KR 930000496 A KR930000496 A KR 930000496A KR 930016402 A KR930016402 A KR 930016402A
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히로히꼬 스기모또
마사루 오가따
히로시 마쯔모또
겐-이찌 스기따
아끼히꼬 사또
다미오 후지와라
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시오노 요시히꼬
시오노기 세이야꾸 가부시끼가이샤
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    • C—CHEMISTRY; METALLURGY
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C07D233/62—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with triarylmethyl radicals attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
    • C07D233/72—Two oxygen atoms, e.g. hydantoin
    • C07D233/80—Two oxygen atoms, e.g. hydantoin with hetero atoms or acyl radicals directly attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
    • C07D233/84—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
    • C07D233/86—Oxygen and sulfur atoms, e.g. thiohydantoin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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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
    • C07D417/06—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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Abstract

본 발명은 하기 일반식(Ⅰ)의 신규 이미다졸 유도체 및 그의 약학적으로 허용 가능한 염에 관한 것이다:
상기식에서, R1은 수소, 알킬, 할로겐 또는 선택적으로 치환된 아릴이고; R2는 알킬, 선택적으로 치환된 아릴, 선택적으로 치환된 아르알킬 또는 선택적으로 치환된 이종환 그룹이고; R3은 수소, 알킬, 선택적으로 치환된 이종환 그룹이고; R3은 수소, 알킬, 선택적으로 치환된 아릴, 선택적으로 치환된 아르알킬 또는 선택적으로 치환된 하이드록시 알킬이고; R4는 수소, 알킬, 할로겐, 아실, 선택적으로 치환된 하이드록시 알킬, 선택적으로 에스테르화되거나 아미드화된 카복실 그룹, 하이드록시 그룹, 아릴 또는 아릴티오이고; X는 S, SO, SO2, CH2또는 Se이고, n은 1 내지 3의 정수이고, 상기 신규 이미다졸 유도체는 항-HIV 활성이 있으며 HIV 감염증을 치료하는데 유용하다.

Description

항-HIV 활성을 갖는 이미다졸 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (4)

  1. 하기 일반식(Ⅰ)의 화합물 또는 그의 약학적으로 허용가능한 염;
    상기식에서, R1은 수소, 알킬 할로겐 또는 선택적으로 치환된 아릴이고; R2는 알킬 선택적으로 치환된 아릴, 선택적으로 치환된 아르알킬 또는 선택적으로 치환된 이종환 그룹이고; R3은 수소, 알킬, 선택적으로 치환된 아릴, 선택적으로 치환된 아르알킬 또는 선택적으로 치환된 하이드록시 알킬이고; R4는 수소, 알킬, 할로겐, 아실, 선택적으로 치환된 하이드록시 알킬, 선택적으로 에스테르화되거나 아미드화된 카복실 그룹, 하이드록시 그룹, 아릴 또는 아릴티오이고; X는 S, SO, SO2, CH2또는 Se이고, n은 1 내지 3의 정수이다.
  2. 제1항에 있어서, R1이 수소, 저급 알킬, 할로겐 또는 페닐이고; R2가 저급 알킬, 저급 알킬 또는 할로겐으로 선택적으로 치환된 페닐, 또는 필리딜이고; R3이 저급 알킬, 벤질 또는 하이드록시알킬이고; R4가 수소, 저급 알킬, 할로겐, 포르밀, 선택적으로 치환된 하이드록시메틸, 선택적으로 에스테르화되거나 아미드화된 카복실 그룹, 하이드록시 그룹 또는 페닐티오 그룹이고; X가 S 또는 CH2이고, n이 1의 정수인 화합물.
  3. 효과량의 제1항의 화합물을 약학적으로 허용 가능하고 실질적으로 무독성인 담체 또는 부형제와 함께 포함하는 약학적으로 조성물.
  4. 효과량의 제1항의 화합물을 약학적으로 허용 가능한 담체와 함께 포함하는 항바이러스제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019930000496A 1992-01-16 1993-01-15 항-hiv 활성을 갖는 이미다졸 유도체 KR100259309B1 (ko)

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JP92-5577 1992-01-16
JP557792 1992-01-16

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KR930016402A true KR930016402A (ko) 1993-08-26
KR100259309B1 KR100259309B1 (ko) 2000-08-01

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US (2) US5326780A (ko)
EP (2) EP0552060B1 (ko)
JP (1) JP3464498B2 (ko)
KR (1) KR100259309B1 (ko)
AT (2) ATE200082T1 (ko)
AU (1) AU649906B2 (ko)
CA (1) CA2087112A1 (ko)
DE (2) DE69322106T2 (ko)
DK (2) DK0552060T3 (ko)
ES (2) ES2157291T3 (ko)
GR (1) GR3035646T3 (ko)
HU (1) HU219917B (ko)
NZ (1) NZ245674A (ko)
PT (1) PT700911E (ko)
TW (1) TW235963B (ko)
ZA (1) ZA93217B (ko)

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US5300519A (en) * 1988-07-06 1994-04-05 The University Of Sheffield Immunosuppressive agents
US5514781A (en) * 1994-04-11 1996-05-07 Bayer Corporation Use of azoles as virucidal agents in solutions of biologically active proteins
US5922751A (en) * 1994-06-24 1999-07-13 Euro-Celtique, S.A. Aryl pyrazole compound for inhibiting phosphodiesterase IV and methods of using same
EP0786455B1 (en) * 1994-09-26 2003-12-03 Shionogi & Co., Ltd. Imidazole derivative
ATE286884T1 (de) * 1996-03-28 2005-01-15 Shionogi & Co Durch lymphe absorbierbare imidazolderivate
WO1997036881A1 (en) * 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5891889A (en) * 1996-04-03 1999-04-06 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997037657A1 (fr) * 1996-04-04 1997-10-16 Shionogi & Co., Ltd. Composition anti-vih contenant un derive d'imidazole
US6544193B2 (en) * 1996-09-04 2003-04-08 Marcio Marc Abreu Noninvasive measurement of chemical substances
ES2245005T3 (es) * 1996-12-26 2005-12-16 SHIONOGI & CO., LTD. Procedimiento de produccion de derivados de imidazol.
TWI232214B (en) * 1998-04-16 2005-05-11 Shionogi & Co Preparation of aryl sulfenyl halide
US6184241B1 (en) 1998-08-24 2001-02-06 Kansas State University Research Foundation Aspartic protease inhibitors
ATE375332T1 (de) 1998-12-24 2007-10-15 Astellas Pharma Inc Imidazol verbindungen und ihre medizinische verwendung
GB0028484D0 (en) 2000-11-22 2001-01-10 Hoffmann La Roche Imidazolone derivatives for the treatment of viral diseases
CA2439053A1 (en) * 2001-02-23 2002-09-06 K.U. Leuven Research & Development Hiv inhibiting n-aminoimidazole derivatives
AU2013403917A1 (en) 2013-11-04 2016-04-28 Covidien Lp Surgical fastener applying apparatus

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JPS63150266A (ja) * 1986-12-12 1988-06-22 Mitsui Petrochem Ind Ltd ベンジルイミダゾ−ル誘導体
US5668136A (en) * 1990-09-25 1997-09-16 Eisai Co., Ltd. Trisubstituted benzene derivatives, composition and methods of treatment

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AU649906B2 (en) 1994-06-02
EP0552060A1 (en) 1993-07-21
EP0700911B1 (en) 2001-03-28
DE69330072D1 (de) 2001-05-03
DE69322106D1 (de) 1998-12-24
HU9300107D0 (en) 1993-04-28
KR100259309B1 (ko) 2000-08-01
EP0552060B1 (en) 1998-11-18
CA2087112A1 (en) 1993-07-17
GR3035646T3 (en) 2001-06-29
ES2125301T3 (es) 1999-03-01
US5326780A (en) 1994-07-05
JPH05255270A (ja) 1993-10-05
PT700911E (pt) 2001-07-31
ATE200082T1 (de) 2001-04-15
ZA93217B (en) 1993-08-18
NZ245674A (en) 1995-06-27
DE69330072T2 (de) 2001-08-23
DE69322106T2 (de) 1999-04-29
US5472965A (en) 1995-12-05
ES2157291T3 (es) 2001-08-16
AU3182793A (en) 1993-07-22
TW235963B (ko) 1994-12-11
HUT63615A (en) 1993-09-28
ATE173470T1 (de) 1998-12-15
DK0700911T3 (da) 2001-05-07
DK0552060T3 (da) 1999-08-02
JP3464498B2 (ja) 2003-11-10
HU219917B (hu) 2001-09-28
EP0700911A1 (en) 1996-03-13

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