KR880006229A - 항궤양 활성을 갖는 피리딘 유도체 - Google Patents

항궤양 활성을 갖는 피리딘 유도체 Download PDF

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KR880006229A
KR880006229A KR870012813A KR870012813A KR880006229A KR 880006229 A KR880006229 A KR 880006229A KR 870012813 A KR870012813 A KR 870012813A KR 870012813 A KR870012813 A KR 870012813A KR 880006229 A KR880006229 A KR 880006229A
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lower alkyl
alkyl group
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시게루 소우다
노리히로 우에다
슈헤이 미야자와
가쯔야 다가미
세이이찌로오 노모또
마꼬도 오끼다
나오유끼 시모무라
도시히꼬 가네꼬
마사또시 후지모도
마나부 무라까미
기요시 오께다니
히데아끼 후지사끼
히사시 시비따
쯔네오 와까바야시
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나이또오 유우지
에자이 가부시끼가이샤
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    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D417/14—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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

내용 없음

Description

항궤양 활성을 갖는 피리딘 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (17)

  1. 다음 일반식으로 표시되는 것을 특징으로 하는 피리딘 유도체 및 그의 약학적으로 허용가능한 염.
    식중 R1및 R2는 상호 동일하거나 상이하며, 각각은 수소원자, 저급 알킬기, 저급 알콕시기, 할로겐화 저급 알킬기, 저급 알콕시카보닐기 또는 카르복실기 또는 할로겐원자를 나타내며: X는 다음 일반식으로 표시되는 기 -O-, -S- 또는(식중 R3는 수소원자 또는 저급 알킬기, 페닐기, 벤질기 또는 저급 알콕시카르보닐기를 나타낸다)를 나타내며; Z는 ① 다음 일반식으로 표시되는 기: -O(CH2)p-O-R4(식중 p는 1내지 3의 정수를 나타내며, R4는 수소원자 또는 저급 알킬기, 알킬기 또는 아르알킬기를 나타낸다), ② 다음의 일반식으로 표시되는 기: -O(CH2)q-O-R5(식중 q는 1내지 3의 정수를 나타내며, R5는 할로겐원자 또는 알콕시카르보닐기, 아릴기 또는 헤테로아릴기를 나타낸다), ③ 다음의 일반식으로 표시되는 기:-O(CH2)q-O-(CH2)s-O-R6(식중 r및 s는 각각 1 내지 5의 정수를 나타내며, R6는 수소원자 또는 저급 알킬기를 나타낸다),
    ④ 다음 식으로 표시되는 기:⑤ 다음 식으로 표시되는 기:
    ⑥ 다음 식으로 표시되는 기:⑦ 다음 식으로 표시되는 기:
    (식중 t는 0내지 2의 정수를 나타내며, A는 다음 일반식으로 표시되는 기
    (식중 B는 일반식 -NH-, -O-또는 -S-로 표시되는 기를 나타낸다), 저급 알킬기, 알콕시카르보닐메틸기, 피리딜기 또는 푸릴기 또는 다음 일반식으로 표시되는 기
    (식중 R7은 수소원자, 저급 알킬기 또는 저급 알콕시기 또는 할로겐원자를 나타내며, W는 0또는 1의 정수를 나타낸다)를 나타낸다.)
    ⑧ 다음의 일반식으로 표시되는기:
    (식중 R8은 아세톡시기 또는 저급 알킬기를 나타낸다), 또는
    ⑨ 다음 식으로 표시되는 기: -OR9
    (식중 R9는 수소원자 또는 저급 알킬기 또는 아릴기를 나타낸다), n은 0내지 2의 정수를 나타내며; m은 2내지 10의 정수를 나타내며, 및 J 및 K는 상호 동일하거나 상이하며 각각은 수소원자 또는 저급 알킬기를 나타내며, 단 Z가 상기 ⑨(식중 R9는 저급 알킬기이다)에서 표시되는 기라면, m은 3내지 10의 정수를 나타낸다.
  2. 제1항에서 정의한 식을 갖는 피리딘 유도체 또는 그의 약리적으로 허용가능한 염의 약리적 유효량 및 약리적으로 허용가능한 담체로 구성되는 것을 특징으로 하는 약학조성물.
  3. 제1항에 있어서, Z가 기①,②,③,④,⑤ 또는 ⑨인 것을 특징으로 하는 화합물.
  4. 제3항에 있어서, Z가 기①,② 또는 ⑨인 것을 특징으로 하는 화합물.
  5. 제4항에 있어서, Z는 ⑨이고 R1은 수소 또는 저급 알킬기 및 R2가 수소인 것을 특징으로 하는 화합물.
  6. 제1항에 있어서, X는 질소, K는 수소, n은 1및 z는 -OR9이고, R1및 R2는 둘다 수소이거나 R1은 5-저급 알킬기, 5-할로겐화 저급 알킬기 또는 5-저급 알콕시기이고 R2는 수소, J는 수소 또는 메틸기 및 m은 3내지 10이며, R9가 저급 알킬기인 것을 특징으로 하는 화합물.
  7. 제6항에 있어서, R1및 R2는 둘다 수소이고, J는 수소, m은 3및 R9가 메틸기인 것을 특징으로 하는 화합물.
  8. 제6항에 있어서, R1및 R2는 둘다 수소이고, J는 수소, m은 3및 R9가 메틸기인 것을 특징으로 하는 화합물.
  9. 제6항에 있어서, R1및 R2는 둘다 수소이고, J는 수소, m은 2및. R9가 벤질기인 것을 특징으로 하는 화합물.
  10. 제1항에 있어서, X는 질소, n은 1 및 Z는 -O(CH2)p-OR4이고, R1및 R2는 둘다 수소이거나 R1이 5-저급 알킬기, 5-할로겐화 저급 알킬기 또는 5-저급 알콕시기이고 R2가 수소, m이 2 또는 3, p가 2또는 3이며 R4가 메틸기 또는 벤질기 및 K가 수소인 것을 특징으로 하는 화합물.
  11. 제10항에 있어서, R1은 메톡시기, R2는 수소, J는 메틸기, m은 2, p는 2이고 R4가 메틸기인 것을 특징으로 하는 화합물.
  12. 제2항에 있어서, 화합물이 화합물 19인 것을 특징으로 하는 약학조성물.
  13. 제2항에 있어서, 약학조성물이 1회 복용시 화합물 0.1내지 100그램으로 구성되는 것을 특징으로 하는 약학조성물.
  14. 사람에게 소화성 궤양완화 또는 예방량의 제12항 조성물을 투여하는 것으로 되어 있는 것을 특징으로 하는 그와 같은 것을 필료로 하는 사람의 소화성 궤양을 치료 또는 예방하는 방법.
  15. 제14항에 있어서, 0.1내지 200㎎/kg/day를 투여하는 것을 특징으로 하는 방법.
  16. 제15항에 있어서, 0.05내지 5㎎/kg/day를 투여하는 것을 특징으로 하는 방법.
  17. 제16항에 있어서, 0.1내지 10㎎/kg/day를 투여하는 것을 특징으로 하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019870012813A 1986-11-13 1987-11-13 항궤양 활성을 갖는 피리딘 유도체 KR910003330B1 (ko)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
JP27053686 1986-11-13
JP61-270536 1986-11-13
JP62-21989 1987-02-02
JP2198987 1987-02-02
JP7778487 1987-03-31
JP62-77784 1987-03-31

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KR880006229A true KR880006229A (ko) 1988-07-22
KR910003330B1 KR910003330B1 (ko) 1991-05-27

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US (3) US5045552A (ko)
EP (3) EP0268956B2 (ko)
JP (1) JP2544567B2 (ko)
KR (1) KR910003330B1 (ko)
CN (1) CN1018923B (ko)
AT (2) ATE168111T1 (ko)
AU (1) AU594836B2 (ko)
CA (1) CA1265138A (ko)
DE (4) DE19975035I2 (ko)
DK (2) DK171024B1 (ko)
ES (3) ES2061471T5 (ko)
FI (1) FI90544C (ko)
HK (1) HK194296A (ko)
HU (1) HU198475B (ko)
LU (1) LU90396I2 (ko)
NL (1) NL990015I2 (ko)
NO (2) NO170932C (ko)
NZ (1) NZ222488A (ko)

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ATE163011T1 (de) 1998-02-15
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