KR850005417A - 화학적 화합물 - Google Patents

화학적 화합물 Download PDF

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KR850005417A
KR850005417A KR1019850000179A KR850000179A KR850005417A KR 850005417 A KR850005417 A KR 850005417A KR 1019850000179 A KR1019850000179 A KR 1019850000179A KR 850000179 A KR850000179 A KR 850000179A KR 850005417 A KR850005417 A KR 850005417A
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methyl
formula
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dihydro
phenyl
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앤토니 슬래터 로버트
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데비드 마틴 워터스
스미스 클라인 앤드 프랜취 라보라토리스 리미티드
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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
    • C07D237/22Nitrogen and oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/28Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to cyano groups, e.g. cyanoguanidines, dicyandiamides
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/04Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having less than three double bonds between ring members or between ring members and non-ring members

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Abstract

내용 없음

Description

화학적 화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (19)

  1. R1이 수소 또는 메틸이고 R2가 수소 또는 C1-4알킬로서 다음 공정을 포함하는 다음 일반식(Ⅰ)화합물 또는 그 약학적으러 허용 가능한 염을 제조하는 방법.
    (가) R1이 앞서 정의한 바와 같은 다음 일반식(Ⅲ)화합물을,
    L1이 이탈그룹이고 R은 R2가 앞서 정의한 바와 같은 NHR2그룹이거나 R이 이탈그룹 L2인 일반식(Ⅳ)화합물과 반응시키고 ;
    그 후에 R이 이탈그룹 L2면 R2가 앞서 정의한 바와 같은 아민 NH2R2와 반응시키거나 또는 (나)일반식 (Ⅴ)화합물을,
    L2, R1및 RR가 앞서 정의한 바와 같은 아민 NH2R2와 반응시키거나; 또는 (다) R1과 R2가 앞서 정의한 바와 같고 X는 치환 가능한 그룹인 일반식(Ⅵ)화합물을,
    하이드라진 또는 그 화학적 균등률과 반응시키거나; 또는 (라) R1과 R2가 앞서 정의한 바와 같고, A는 치환가능 그룹인 일반식(Ⅶ)화합물을,
    시안아마이드 또는 그것들의 중금속염과 반응시키거나; (마) R2가 수소인 일반식(Ⅰ) 화합물을 얻기 위해, 앞서 정의한 일반식(Ⅲ) 화합물을 디시안아마이드염과 반응시키고; 그 후 약학적으로 허용가능한 이들의 염을 임의로 형성시키는 것으로 구성되는 상기 제조방법.
  2. 청구범위 1에서 일반식(Ⅳ) 화합물의 L1과 L2가 독립적으로 벤질티오, C1-6알킬리오, C1-6알콜시, 페녹시 또는 벤젤톡시인 공정.
  3. 청구범위 1에서 일반식(Ⅴ) 화합물의 L2벤젤티오, C1-6알킬리오, C1-6알콕시, 페녹시 또는 벤질톡시인 공정.
  4. 청구범위 1에서 일반식(Ⅵ) 화합물의 X가 하이드록시, C1-6알콕시, 아미노 또는 C1-6알킬아미노인 공정.
  5. 청구범위 1에서 일반식(Ⅶ) 화합물의 A가 메르캅토, C1-4알킬티오, C1-4알콕시, 페녹시 또는 벤질톡시인 공정.
  6. 청구범위 1내지 5중에서 R1이 메틸인 화합물을 제조하기 위한 공정.
  7. 청구범위 1내지 6중에서 R2가 C1-4알킬인 화합물의 제조를 위한 공정.
  8. 청구범위 7에서 R2가 메틸 또는 에틸인 화합물의 제조를 위한 공정.
  9. 청구범위 1에서 다음 화합물의 제조를 위한 공정 :
    6-[4-(N3-메틸-N2-시아노구아니디노)페닐]-5-메틸-4,5-디하이드로-3(2H)-피리다진온,
    6-[4-(N3-에틸-N2-시아노구아니디노)페닐]-5-메틸-4,5-디하이드로-3(2H)-피리다진온,
    6-[4-(N3-이소프로필-N2-시아노구아니디노)페닐]-5-메틸-4,5-디하이드로-3(2H)-피리다진온,
    6-[4-(N3-부틸-N2-시아노구아니디노)페닐]-5-메틸-4,5-디하이드로-3(2H)-피리다진온,
    6-[4-(N3-시아노구아니디노)페닐]-5-메틸-4,5-디하이드로-3(2H)-피리다진온, 또는 6-[4-(N3-메틸-N2-시아노구아니디노)페닐]-4,5-디하이드로-3(2H)-피리다진.
  10. 6-[4-(N-시아노S-메틸이소티오우레이도)페닐)-5-메틸-4,5-디하이드로-3(2H)-피리다진온과 메틸아민과의 반응을 포함하는 6-[4-(N3-메틸-N2-시아노구아니디노)페닐]-5-메틸-4,5-디하이드로-3(2H)-피리다진온을 제조하는 공정.
  11. 6-(4-[N2-시아노)페녹시포름아미디노)]페닐)-5-메틸-4,5-디하이드로-3(2H)-피리다진온과 메틸아민과의 반응을 포함하는 6-[4-(N3-메틸-N2-시아노구아니디노)페닐]-5-메틸-4,5-디하이드로-3(2H)-피리다진온을 제조하는 공정.
  12. 일반식(Ⅰ) 화합물 또는 약학적으로 바람직한 그 염과 약학적으로 바람직한 전달체를 결합시키는 공정을 포함하는 약학적인 성형을 제조하는 공정.
  13. 청구범위 12에서 일반식(Ⅰ)화합물이 6-[4-(N3-메틸-N2-시아노구아니디노)페닐]-5-메틸-4,5-디하이드로-3(2H)-피리다진온 공정.
  14. R1과 L2가 청구범위 1에서 정의한 바와 같은 다음 일반식(Ⅴ) 화합물을 제조하는 공정 :
    (가)R1이 앞서 정의한 바와 같은 다음 구조식(Ⅲ) 화합물을,
    L1과 L2가 청구범위 1에서 정의한 바와 같은 다음 구조식으 화합물과 반응시킴, 또는
    (나) L2,X 및 R1이 청구범위 1에서 정의한 바와 같은 다음 구조식의 화합물을,
    하이드라진 또는 그 화학적 동질물과 반응시킴.
  15. 청구범위 14에서 R1이 메틸이고, L2가 페녹시, C1-6알콕시 또는 C1-6알칼티오인 화합물의 제조를 위한 공정.
  16. 청구범위 15에서 L2가 메틸티오인 화합물의 제조를 위한 공정.
  17. 청구범위 15에서 에톡시인 화합물의 제조를 위한 공정
  18. R1과 L2가 청구범위 1에서 정의한 바와 같은 다음 일반식(Ⅴ) 화합물,
  19. R1과 R2및 X가 청구범위 1에서 정의한 바와 같은 다음구조식(Ⅵ) 화합물 :
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019850000179A 1984-01-13 1985-01-12 디하이드로 피리다진온 유도체를 제조하는 방법 KR920006781B1 (ko)

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GB8400863 1984-01-13
GB848400863A GB8400863D0 (en) 1984-01-13 1984-01-13 Chemical compounds

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PH22136A (en) 1988-06-01
JPS60158181A (ja) 1985-08-19
EP0150937B1 (en) 1988-09-14
DK9185D0 (da) 1985-01-08
AU3761185A (en) 1985-07-18
IL74031A (en) 1988-07-31
ES8706645A1 (es) 1987-07-01
NO850129L (no) 1985-07-15
WO1985003076A1 (en) 1985-07-18
ES549629A0 (es) 1987-03-01
MY100124A (en) 1989-12-18
DK162519C (da) 1992-03-30
GR850068B (ko) 1985-05-03
ZW385A1 (en) 1985-08-07
HU193591B (en) 1987-11-30
CA1260471C (ko) 1989-09-26
ZA85251B (en) 1986-08-27
JPS63313776A (ja) 1988-12-21
RO92607A (ro) 1987-11-30
AU572252B2 (en) 1988-05-05
ES8607949A1 (es) 1986-06-01
EP0150937A3 (en) 1985-08-21
EP0150937A2 (en) 1985-08-07
SU1396963A3 (ru) 1988-05-15
IE57969B1 (en) 1993-06-02
IE850069L (en) 1985-07-13
DD231350A5 (de) 1985-12-24
NZ210816A (en) 1987-06-30
CA1260471A (en) 1989-09-26
FI850140A0 (fi) 1985-01-11
FI850140L (fi) 1985-07-14
PT79819B (en) 1987-01-07
JPS63313775A (ja) 1988-12-21
PT79819A (en) 1985-02-01
US4654342A (en) 1987-03-31
JO1351B1 (en) 1986-11-30
CN85101722A (zh) 1987-01-31
ES539446A0 (es) 1986-06-01
CS248731B2 (en) 1987-02-12
IL74031A0 (en) 1985-04-30
HUT37128A (en) 1985-11-28
PL251516A1 (en) 1985-12-17
ES8703846A1 (es) 1987-03-01
GB8400863D0 (en) 1984-02-15
DK162519B (da) 1991-11-11
PL147123B1 (en) 1989-04-29
KR920006781B1 (ko) 1992-08-17
DK9185A (da) 1985-07-14
ES554965A0 (es) 1987-07-01
DE3564941D1 (en) 1988-10-20
ATE37179T1 (de) 1988-09-15
CA1251209A (en) 1989-03-14

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