KR910004582A - 티아졸 유도체, 이의 제조방법 및 이를 함유하는 약학조성물 - Google Patents

티아졸 유도체, 이의 제조방법 및 이를 함유하는 약학조성물 Download PDF

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KR910004582A
KR910004582A KR1019900012081A KR900012081A KR910004582A KR 910004582 A KR910004582 A KR 910004582A KR 1019900012081 A KR1019900012081 A KR 1019900012081A KR 900012081 A KR900012081 A KR 900012081A KR 910004582 A KR910004582 A KR 910004582A
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compound
salt
general formula
following general
halogen
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KR1019900012081A
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마사키 마츠오
다카시 오기노
노리히로 이가리
하치로 세노
교이치 시모무라
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후지사와 도모키치로
후지사와 야쿠힌 코교 가부시기가이샤
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Priority claimed from GB898918045A external-priority patent/GB8918045D0/en
Priority claimed from GB909003930A external-priority patent/GB9003930D0/en
Application filed by 후지사와 도모키치로, 후지사와 야쿠힌 코교 가부시기가이샤 filed Critical 후지사와 도모키치로
Publication of KR910004582A publication Critical patent/KR910004582A/ko

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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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/38—Nitrogen atoms
    • C07D277/40—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/54—Nitrogen and either oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

Abstract

내용 없음.

Description

티아졸 유도체, 이의 제조방법 및 이를 함유하는 약학조성물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기 일반식(I)의 화합물 또는 이의 약학적 허용염 :
    상기식중, R1은 수소 또는 할로겐에 의해 치환가능한 아실, R2는 수소, 저급알킬, 히드록시(저급)알킬, 할로겐 또는 카르복시, A는 -CH2-, -CO-, -C(=NOR4)-(여기에서, R4는 저급알킬이다),또는(여기에서, m은 0,1 또는 2이다), R3는 할로겐, 히드록시, 저급알콕시, 니트로, 아미노 또는 아실아미노; 또는 저급알킬, 아미노, 히드록시 또는 할로 (저급) 알킬에 의해 치환가능한 N-함유불포화헤테로시클릭기이다.
  2. 제1항에 있어서, R1은 수소, 저급알카노일, 저급알칸설포닐 또는 할로겐에 의해 치환가능한 벤조일이고, R3은 할로겐, 히드록시, 저급알콕시, 니트로, 아미노, 저급알카노일아미노 또는 저급알칸설포닐아미노에 의해 치환가능한 페닐; 또는 각각 저급알킬, 아미노, 히드록시 또는 할로(저급)알킬에 의해 치환가능한 피리딜, 피리미디닐, 이미다졸릴, 테트라졸릴 또는 티아디아졸릴인 화합물.
  3. 제2항에 있어서, R1이 수소인 화합물.
  4. 제3항에 있어서, R2가 수소인 화합물.
  5. 제4항에 있어서, A가(여기에서, m은 0, 1 또는 2이다)인 화합물.
  6. 제5항에 있어서, R3가 피리딜, 피리미디닐, 이미다졸릴, 테트라졸릴 또는 티아디아졸릴인 화합물.
  7. (1) 하기 일반식(Ia)화합물 또는 그 염을 탈아실화시켜서 하기 일반식(Ib)화합물 또는 그 염을 제조하거나, (2) 하기 일반식(II)화합물 또는 그 염을 하기 일반식(III)화합물 또는 그 염과 반응시켜서 하기 일반식(Ic) 또는 그 염을 제조하거나, (3) 하기 일반식(Id) 화합물 또는 그 염을 환원시켜서 하기 일반식(Ie)화합물 또는 그 염을 제조하거나, (4) 하기 일반식(If)화합물 또는 그 염을 산화시켜서 하기 일반식(Ig)화합물 또는 그 염을 제조하거나, (5) 하기 일반식(Ih)화합물 또는 그 염을 산화시켜서 하기 일반식(Ii) 화합물 또는 그 염을 제조하거나, (6) 하기 일반식(Ij) 화합물 또는 그 염을 할로겐화시켜서 하기 일반식(Ik)화합물 또는 그 염을 제조하거나, (7) 하기 일반식(Ib) 화합물 또는 그 염을 아실화시켜서 하기 일반식(Ia) 화합물 또는 그 염을 제조하거나, (8) 하기 일반식(Ie)화합물 또는 그 염을 아실화시켜서 하기 일반식(I1)화합물 또는 그 염을 제조하거나, (9) 하기 일반식(IV) 화합물 또는 그 염을 하기 일반식(V) 화합물 또는 그염과 반응시켜서 하기 일반식(Im)화합물 또는 그 염을 제조하거나, (10) 하기 일반식(VI)화합물 또는 그 염을 하기일반식(V)화합물 또는 그염과 반응시켜서 하기 일반식(In)화합물 또는 그 염을 제조하거나, (11) 하기 일반식(Io) 화합물 또는 그 염을 하기 일반식(VII) 화합물 또는 그염과 반응시켜서 하기 일반식(Ip)화합물 또는 그 염을 제조하는 것으로 구성되는 하기 일반식(I)화합물 또는 그염의 제조방법 :
    상기식중, R1은 수소 또는 할로겐에 의해 치환가능한 아실, R2는 수소, 저급알킬, 히드록시(저급)알킬, 할로겐 또는 카르복시, A는 -CH2-, -CO-, -C(=NOR4)-(여기에서, R4는 저급알킬이다),또는(여기에서, m은 0,1 또는 2이다), R3는 할로겐, 히드록시, 저급알콕시, 니트로, 아미노 또는 아실아미노; 또는 저급알킬, 아미노, 히드록시 또는 할로(저급)알킬에 의해 치환가능한 N-함유불포화헤테로시클릭기, R5는 할로겐에 의해 치환가능한 아실, R6은 아실아미노, X는 할로겐, 1은 0 또는 1, n은 0 또는 1, q는 1 또는 2(여기에서 n이 1이면, q는 2이다)이다.
  8. 활성 성분인 제1항의 화합물 또는 이의 약학적으로 허용되는 염과함께 약학적으로 허용되는 담체를 포함하는 약학조성물.
  9. 제1항의 화합물 또는 이의 약학적으로 허용되는 염을 인체 또는 동물에 투여하는 것으로 구성되는 류머티즘, 신장염, 혈전증, 종양 및 항종양제의 부작용을 치료하는 방법.
  10. 제1항의 화합물 또는 이의 약학적으로 허용되는 염을 의약으로서 사용하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900012081A 1989-08-07 1990-08-06 티아졸 유도체, 이의 제조방법 및 이를 함유하는 약학조성물 KR910004582A (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB898918045A GB8918045D0 (en) 1989-08-07 1989-08-07 Thiazole derivatives,processes for production thereof and pharmaceutical compositions comprising the same
GB89180459 1989-08-07
GB90039306 1990-02-21
GB909003930A GB9003930D0 (en) 1990-02-21 1990-02-21 Thiazole derivatives,processes for production thereof and pharmaceutical compositions comprising the same

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KR910004582A true KR910004582A (ko) 1991-03-29

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EP (1) EP0412404B1 (ko)
JP (1) JPH0368567A (ko)
KR (1) KR910004582A (ko)
CN (1) CN1027370C (ko)
AT (1) ATE133667T1 (ko)
AU (1) AU635758B2 (ko)
CA (1) CA2022731A1 (ko)
DE (1) DE69025104T2 (ko)
DK (1) DK0412404T3 (ko)
ES (1) ES2082805T3 (ko)
FI (1) FI96857C (ko)
GR (1) GR3019009T3 (ko)
HK (1) HK151596A (ko)
HU (2) HUT57752A (ko)
IE (1) IE902679A1 (ko)
IL (1) IL95281A (ko)
NO (1) NO179638C (ko)
PH (1) PH26766A (ko)
PT (1) PT94925B (ko)
RU (2) RU2010026C1 (ko)
TW (1) TW205041B (ko)

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IL95281A0 (en) 1991-06-30
DE69025104D1 (de) 1996-03-14
IE902679A1 (en) 1991-02-27
RU2048468C1 (ru) 1995-11-20
AU635758B2 (en) 1993-04-01
DK0412404T3 (da) 1996-02-26
TW205041B (ko) 1993-05-01
NO903438L (no) 1991-02-08
HU904912D0 (en) 1991-01-28
CA2022731A1 (en) 1991-02-08
NO903438D0 (no) 1990-08-06
PT94925B (pt) 1997-04-30
ATE133667T1 (de) 1996-02-15
ES2082805T3 (es) 1996-04-01
DE69025104T2 (de) 1996-07-04
HU211557A9 (en) 1995-12-28
NO179638C (no) 1996-11-20
GR3019009T3 (en) 1996-05-31
HK151596A (en) 1996-08-16
PH26766A (en) 1992-09-28
EP0412404B1 (en) 1996-01-31
FI96857B (fi) 1996-05-31
IL95281A (en) 1996-06-18
JPH0368567A (ja) 1991-03-25
RU2010026C1 (ru) 1994-03-30
CN1027370C (zh) 1995-01-11
CN1049337A (zh) 1991-02-20
FI903879A0 (fi) 1990-08-06
AU6004590A (en) 1991-02-07
EP0412404A3 (en) 1991-06-12
HUT57752A (en) 1991-12-30
NO179638B (no) 1996-08-12
EP0412404A2 (en) 1991-02-13
FI96857C (fi) 1996-09-10
PT94925A (pt) 1991-04-18

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