KR880001643A - Ischemic vascular disease treatment method - Google Patents

Ischemic vascular disease treatment method Download PDF

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Publication number
KR880001643A
KR880001643A KR1019870006952A KR870006952A KR880001643A KR 880001643 A KR880001643 A KR 880001643A KR 1019870006952 A KR1019870006952 A KR 1019870006952A KR 870006952 A KR870006952 A KR 870006952A KR 880001643 A KR880001643 A KR 880001643A
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South Korea
Prior art keywords
carbon atoms
alkoxy
alkyl
compound
cycloalkyl
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KR1019870006952A
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Korean (ko)
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노르트 프랑크
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제랄드 디. 샤르킨
산도즈 파마슈티칼스 코오포레이숀
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Publication of KR880001643A publication Critical patent/KR880001643A/en

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    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61P9/08—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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

내용 없음No content

Description

허혈성 혈관 질병 치료방법Ischemic vascular disease treatment method

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음As this is a public information case, the full text was not included.

제1도는 KP 3와 플루나리진 농도의 로그의 용혈억제의 백분율과의 상관관계를 나타낸 그래프.1 is a graph showing the correlation between KP 3 and the percentage of hemolytic inhibition of log of flunarizine concentration.

제2도는 칼슘이온이 부가된 적혈구의 엑타사이토메트리 변형지수에 대한 KP 3의 영향을 나타낸 그래프.2 is a graph showing the effect of KP 3 on the ectocytometry modification index of red blood cells added with calcium ion.

Claims (7)

하기식(I)의 출혈성 활성화합물 또는 그의 약학적으로 허용 가능한 산부가염의 치료적으로 효과적인양을 투여하는 것으로 구성된 허혈성 맥관 질병의 숙주의 치료에 사용하는 치료학적 방법.A therapeutic method for use in the treatment of a host of ischemic vascular disease, comprising administering a therapeutically effective amount of a hemorrhagic active compound of formula (I) or a pharmaceutically acceptable acid addition salt thereof. 상기식에서, R1은 수소, 1-6 탄소원자의 알킬, 3-6 탄소원자의 알케닐 또는 알키닐, 3-7 탄소원자의 시클로알킬, 4-8 탄소원자의 시클로알킬 알킬, 7-9 탄소원자의 페닐 알킬 또는 9-12 탄소원자의 페닐 알케닐, 할로겐, 히드록시 또는 1-4 탄소원자의 알콕시 또는 알킬로 독자적으로 모노-, 디- 또는 트리치환 된 또는 비치환 된 페닐환, R2와 R5는 독자적으로 수소 또는 1-6 탄소원자의 알킬, R3과 R4는 독자적으로 1-6 탄소원자의 알킬, 3-6 탄소원자의 알키닐 또는 알케닐, 3-7 탄소원자의 시클로알킬, 4-8 탄소원자의 시클로알킬 알킬, 1-6 탄소원자의 알콕시, 2-6 탄소원자의 히드록시 알콕시, 3-6 탄소원자의 알콕시 알콕시, 4-8 탄소원자의 히드록시 알콕시 알콕시, 3-6 탄소원자의 알키닐옥시 또는 알케닐옥시, 3-7 탄소원자의 시클로알킬 알콕시 또는 4-8 탄소원자의 시클로알킬 알콕시, R6는 수소, 할로겐 또는 각각 1-4 탄소원자의 알킬술포닐 또는 알킬티오 또는 알콕시 또는 알킬, 트리플루오로메틸, 니트로 또는 히드록시, X는 산소 또는 황.Wherein R 1 is hydrogen, alkyl of 1-6 carbon atoms, alkenyl or alkynyl of 3-6 carbon atoms, cycloalkyl of 3-7 carbon atoms, cycloalkyl alkyl of 4-8 carbon atoms, phenyl alkyl of 7-9 carbon atoms Or mono-, di- or trisubstituted or unsubstituted phenyl rings independently of phenyl alkenyl, halogen, hydroxy of 1-12 carbon atoms or alkoxy or alkyl of 1-4 carbon atoms, R 2 and R 5 are independently Hydrogen or alkyl of 1-6 carbon atoms, R 3 and R 4 are independently alkyl of 1-6 carbon atoms, alkynyl or alkenyl of 3-6 carbon atoms, cycloalkyl of 3-7 carbon atoms, cycloalkyl of 4-8 carbon atoms Alkyl, alkoxy of 1-6 carbon atoms, hydroxy alkoxy of 2-6 carbon atoms, alkoxy alkoxy of 3-6 carbon atoms, hydroxy alkoxy alkoxy of 4-8 carbon atoms, alkynyloxy or alkenyloxy of 3-6 carbon atoms, 3 -7 carbon atoms of cycloalkyl alkoxy or 4-8 carbon atoms Cycloalkyl alkoxy, R 6 is hydrogen, halogen or alkylsulfonyl or alkylthio or alkoxy or alkyl, trifluoromethyl, nitro or hydroxy of 1-4 carbon atoms, respectively, X is oxygen or sulfur. 특허청구범위 제 1항의 식(I)의 화합물의 치료에 효과적인 양만큼 투여하는 것으로 구성된 적혈구 변형 칼슘-조절된 손실에 의한 허혈성 맥관 질병의 치료에 사용하는 치료학적 방법.A therapeutic method for use in the treatment of ischemic vascular disease caused by red blood cell modified calcium-controlled loss consisting of administering an amount effective to treat a compound of formula (I) of claim 1. 제 1항 또는 제 2항에 있어서, 상기 화합물 또는 그의 약학적으로 허용가능한 산부가염 4-(2,1,3-벤즈옥시디아졸-4-일)-1,4-디히드로-2,6-디메틸-피리딘-3,5-디카르복실산디에틸 에스테르, 4--(2,1,3-벤즈옥시디아졸-4-일)-1,4-디히드로-2,6-디메틸-3-메톡시카르보닐-피리딘-5-카르복실산 이소프로필 에스테르 또는 4-(2,1,3-벤즈옥시디아졸-4-일)-2,6-디메틸-1,4-디히드로-피리딘-3,5-디카르복실산디메틸 에스테르에서 선택되는 방법.The compound according to claim 1 or 2, wherein the compound or a pharmaceutically acceptable acid addition salt thereof 4- (2,1,3-benzoxydiazol-4-yl) -1,4-dihydro-2,6 -Dimethyl-pyridine-3,5-dicarboxylic acid diethyl ester, 4-(2,1,3-benzoxydiazol-4-yl) -1,4-dihydro-2,6-dimethyl-3 -Methoxycarbonyl-pyridine-5-carboxylic acid isopropyl ester or 4- (2,1,3-benzoxydiazol-4-yl) -2,6-dimethyl-1,4-dihydro-pyridine -3,5-dicarboxylic acid dimethyl ester. 제 1항, 제 2항 또는 제 3항에 있어서, 식(I)의 화합물 또는 그의 약학적으로 허용가능한 그의 산부가염의 일일용량이 10내지 300mg인 방법.The method according to claim 1, 2 or 3, wherein the daily dose of the compound of formula (I) or a pharmaceutically acceptable acid addition salt thereof is 10 to 300 mg. 제 1항 내지 제 4항의 어느 한항에 있어서, 식(I)의 화합물 또는 그의 약학적으로 허용가능한 그의 산부가염을 2.5내지 300mg 함유하는 단위용량형으로 투여하는 방법.The method according to any one of claims 1 to 4, wherein the compound of formula (I) or a pharmaceutically acceptable acid addition salt thereof is administered in unit dosage form containing 2.5 to 300 mg. 실시예중 어느 하나에 의한 특허청구의 범위 제 1항 또는 제 2항의 방법.The method of claim 1 or claim 2 according to any one of the embodiments. 허혈성 맥관 질병의 치료에 있어서, 치료적 사용에 유용한 특허청구의 범위 제 1항의 식(I)의 화합물 또는 그의 약학적으로 허용가능한 그의 산부가염 및 약학적 담체 또는 희석제로 구성된 약학적 조성물.A pharmaceutical composition comprising the compound of formula (I) of claim 1, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutical carrier or diluent thereof, in the treatment of ischemic vascular disease. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019870006952A 1986-07-01 1987-07-01 Ischemic vascular disease treatment method KR880001643A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB868616047A GB8616047D0 (en) 1986-07-01 1986-07-01 A 1 4-dihydropyridine derivatives
GB8616047 1986-07-01

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KR880001643A true KR880001643A (en) 1988-04-25

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KR1019870006952A KR880001643A (en) 1986-07-01 1987-07-01 Ischemic vascular disease treatment method

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JP (1) JPS6322519A (en)
KR (1) KR880001643A (en)
AU (1) AU7491487A (en)
DE (1) DE3720509A1 (en)
DK (1) DK333587A (en)
FR (1) FR2601012A1 (en)
GB (2) GB8616047D0 (en)
IT (1) IT1216830B (en)
SE (1) SE8702697L (en)
ZA (1) ZA874768B (en)

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* Cited by examiner, † Cited by third party
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DE4011695A1 (en) * 1990-04-11 1991-10-17 Bayer Ag USE OF N-ALKYLATED 1,4-DIHYDROPYRIDE INDICARBOXIC ACID ESTERS AS DRUGS, NEW COMPOUNDS AND METHOD FOR THEIR PREPARATION

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* Cited by examiner, † Cited by third party
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FI64938C (en) * 1977-06-20 1984-02-10 Sandoz Ag PROCEDURE FOR THE FRAMEWORK OF THERAPEUTIC THERAPEUTIC BENSOX A- AND OX BENZOTIADIAZOLYL-1,4-DIHYDROPYRID DERIVATIVES

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DE3720509A1 (en) 1988-01-28
AU7491487A (en) 1988-01-07
JPS6322519A (en) 1988-01-30
IT1216830B (en) 1990-03-14
DK333587D0 (en) 1987-06-29
IT8748101A0 (en) 1987-06-25
ZA874768B (en) 1989-02-22
DK333587A (en) 1988-01-02
GB8616047D0 (en) 1986-08-06
GB2192132A (en) 1988-01-06
SE8702697L (en) 1988-01-02
GB8715219D0 (en) 1987-08-05
FR2601012A1 (en) 1988-01-08
SE8702697D0 (en) 1987-06-30

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