KR920019787A - 피라졸로피리딘 화합물 및 이의 제조 방법 - Google Patents

피라졸로피리딘 화합물 및 이의 제조 방법 Download PDF

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KR920019787A
KR920019787A KR1019920005893A KR920005893A KR920019787A KR 920019787 A KR920019787 A KR 920019787A KR 1019920005893 A KR1019920005893 A KR 1019920005893A KR 920005893 A KR920005893 A KR 920005893A KR 920019787 A KR920019787 A KR 920019787A
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alkyl
compound
carboxy
salt
formula
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요우이치 시오카와
아쯔시 아카하네
히로히토 카타야마
타가후미 미쯔나가
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후지사와 토모키치로
후지사와 야꾸힝 코교 가부시키가이샤
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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • 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
    • A61K31/435—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/24—Antidepressants
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    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
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    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • 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

Abstract

내용 없음

Description

피라졸로피리딘 화합물 및 이의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 하기 일반식(I)의 피라졸로피리딘 화합물 및 이의 약학적 허용가능함 염;
    (상기식에서, R1은 아릴이고, R2는 아실(저급)알킬이고, A는 저급 알케닐렌이다.)
  2. 제1항에 있어서, R1이 페닐이고, R2가 저급 알카노일(저급)알킬, 카르복시(저급)알킬 또는 보호된 카르복시(저급)알킬인 화합물.
  3. 제2항에 있어서, R2가 저급 알카노일(저급)알킬, 카르복시(저급)알킬, 에스테르화 카르복시(저급)알킬 또는 아미드화 카르복시(저급)알킬인 화합물,
  4. 제3항에 있어서, R2가 저급 알카노일(저급)알킬, 카르복시(저급)알킬, 저급 알콕시카르보닐(저급)알킬, 카르바모일(저급)알킬, N-저급 알킬카르바모일(저급)알킬 또는 N,N-디(저급) 알킬카르바모일(저급)알킬인 화합물.
  5. 제4항에 있어서, R2가 카르복시(저급)알킬인 화합물.
  6. 제5항에 있어서, 1-[3-(2-페닐피라졸로[1,5-a]피리딘-3-일)아크릴로일]-2-(카르복시메틸)피페리딘 화합물.
  7. 제6항에 있어서, (2R)-1-[3-(2-페닐피라졸로[1,5-a]피리딘-3-일)아크릴로일]-2-(카르복시메틸)피페리딘 (트랜스 이성질체)인 화합물.
  8. ⅰ) 하기 일반식(II)의 화합물 또는 이의 카르복시기에서의 반응성 유도체 또는 이의 염을 하기 일반식(III)의 화합물 또는 이의 아미노기에서의 반응성 유도체 또는 이의 염과 반응시키거나,
    ii) 하기 일반식(Ia)의 화합물 또는 이의 염의 카르복시 보호기의 제거반응을 수행시켜, 하기 일반식(Ib)의 화합물 또는 이의 염을 생성시키거나,
    iii) 하기 일반식(Ⅳ)의 화합물 또는 이의 염의 산화반응을 수행시켜, 하기 일반식(Ic)의 화합물 또는 이의 염을 생성시키거나,
    iv) 하기 일반식(Ib)의 화합물 또는 이의 카르복시기에서의 반응성 유도체 또는 이의 염의 아미드화 반응을 수행시켜, 하기 일반식(Id)의 화합물 또는 이의 염을 생성시키는 것을 포함하는, 하기 일반식(I)의 피라졸로피리딘 화합물 또는 이의 염을 제조하는 방법:
    (상기식에서, R1은 아릴이고, R2는 아실(저급)알킬이고, Ra2는 보호된 카르복시(저급)알킬이고, Rb2는 카르복시(저급)알킬이고, Rc2는 포르밀(저급)알킬 또는 카르복시(저급)알킬이고, Rd2는 아미드화 카르복시(저급)알킬이고, R3는 히드록시(저급)알킬이고, A는 저급 알케닐렌이다.)
  9. 활성성분으로서 약학적 허용 가능한 담체 또는 부형제와의 혼합물상태의 제1항의 화합물 또는 이의 약학적 허용 가능한 염을 포함하는 약학적 조성물.
  10. 약제를 제조하는데 제1항의 화합물 또는 이의 약학적 허용 가능한 염을 사용하는 방법.
  11. 약제로서 사용하기 위한 제1항과 화합물 또는 이의 약학적 허용 가능한 염.
  12. 사람 또는 동물에게 제1항의 화합물 또는 이의 약학적 허용 가능한 염을 투여하는 것을 포함하는 , 울증, 심부전, 고혈압, 신기능 부전증, 신장독소, 신증, 신장염, 부종, 비만증, 기관지 천식, 통풍, 요산과다뇨, 영아급사 증후군, 면역억제, 당뇨병, 심근경색, 혈전증, 폐색증, 폐색성 동맥경화증, 혈전성 정맥염, 대뇌 경색중, 일과성 허혈성 발작, 협심증의 치료 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920005893A 1991-04-10 1992-04-09 피라졸로피리딘 화합물 및 이의 제조 방법 KR100248700B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB919107513A GB9107513D0 (en) 1991-04-10 1991-04-10 Pyrazolopyridine compound and processes for preparation thereof
GB9107513.5 1991-04-10

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KR920019787A true KR920019787A (ko) 1992-11-20
KR100248700B1 KR100248700B1 (ko) 2000-08-01

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US (1) US5234930A (ko)
EP (1) EP0516941B1 (ko)
JP (2) JP2546470B2 (ko)
KR (1) KR100248700B1 (ko)
CN (2) CN100508975C (ko)
AT (1) ATE146473T1 (ko)
AU (1) AU653007B2 (ko)
CA (1) CA2065644C (ko)
DE (1) DE69215965T2 (ko)
DK (1) DK0516941T3 (ko)
ES (1) ES2095976T3 (ko)
FI (1) FI100969B (ko)
GB (1) GB9107513D0 (ko)
GR (1) GR3022113T3 (ko)
HU (2) HU214871B (ko)
IE (1) IE921086A1 (ko)
IL (1) IL101544A (ko)
MX (1) MX9201672A (ko)
NO (1) NO300271B1 (ko)
RU (1) RU2069662C1 (ko)
SG (1) SG43917A1 (ko)
TW (1) TW205550B (ko)
UA (1) UA27252C2 (ko)

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CN1067427A (zh) 1992-12-30
CN100508975C (zh) 2009-07-08
CA2065644C (en) 2002-12-03
FI921522A (fi) 1992-10-11
US5234930A (en) 1993-08-10
NO300271B1 (no) 1997-05-05
MX9201672A (es) 1992-10-01
DE69215965T2 (de) 1997-04-10
HU9201213D0 (en) 1992-07-28
RU2069662C1 (ru) 1996-11-27
SG43917A1 (en) 1997-11-14
CN1205205A (zh) 1999-01-20
JPH05112566A (ja) 1993-05-07
ATE146473T1 (de) 1997-01-15
AU1398892A (en) 1992-10-15
IL101544A (en) 1996-06-18
TW205550B (ko) 1993-05-11
JP2903040B2 (ja) 1999-06-07
GR3022113T3 (en) 1997-03-31
JP2546470B2 (ja) 1996-10-23
FI100969B (fi) 1998-03-31
DK0516941T3 (da) 1997-01-06
IE921086A1 (en) 1992-10-21
UA27252C2 (uk) 2000-08-15
DE69215965D1 (de) 1997-01-30
EP0516941B1 (en) 1996-12-18
KR100248700B1 (ko) 2000-08-01
GB9107513D0 (en) 1991-05-29
HUT61300A (en) 1992-12-28
JPH08208650A (ja) 1996-08-13
FI921522A0 (fi) 1992-04-07
AU653007B2 (en) 1994-09-15
NO921413D0 (no) 1992-04-09
NO921413L (no) 1992-10-12
CA2065644A1 (en) 1992-10-11
HU214871B (hu) 1998-07-28
ES2095976T3 (es) 1997-03-01
CN1041203C (zh) 1998-12-16
EP0516941A1 (en) 1992-12-09
HU211680A9 (en) 1995-12-28
IL101544A0 (en) 1992-12-30

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