KR890011882A - Ergoline derivatives - Google Patents

Ergoline derivatives Download PDF

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Publication number
KR890011882A
KR890011882A KR1019890000711A KR890000711A KR890011882A KR 890011882 A KR890011882 A KR 890011882A KR 1019890000711 A KR1019890000711 A KR 1019890000711A KR 890000711 A KR890000711 A KR 890000711A KR 890011882 A KR890011882 A KR 890011882A
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South Korea
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compound
methyl
compound according
treatment
phenyl
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KR1019890000711A
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Korean (ko)
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아키니 로란드
암스튜츠 린
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예안 클라메르·한스 로돌프 하우스
산도즈 리미티드
한스 로돌프 하우스
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Publication of KR890011882A publication Critical patent/KR890011882A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D457/00—Heterocyclic compounds containing indolo [4, 3-f, g] quinoline ring systems, e.g. derivatives of ergoline, of the formula:, e.g. lysergic acid
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • 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
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • 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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • A—HUMAN NECESSITIES
    • 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
    • A61P25/28—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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 없음No content

Description

에르고린 유도체Ergoline derivatives

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (35)

유리염기 혹은 산부가염 형태의 위치 8-미치환 및 위치 에르고린 유도체.Position 8-unsubstituted and position ergoline derivatives in freebase or acid addition salt form. 유리염기 혹은 산부가염 형태의 일반식(Ⅰ)의 화합물.Compound of general formula (I) in free base or acid addition salt form. 상기식에서, R¹은 수소 혹은 (C1-4)알킬이고, R²는 퓨라닐, 페닐 혹은 플로린, 클로린, 브로민, (C1-4)알킬, 트리플로로메틸 혹은 (C1-4)알콕시로 단일 혹은 이중 치환된 페닐이다.Wherein R 1 is hydrogen or (C 1-4 ) alkyl and R 2 is furanyl, phenyl or fluorine, chlorine, bromine, (C 1-4 ) alkyl, trifluoromethyl or (C 1-4 ) alkoxy Is phenyl which is single or double substituted. 제2항에 있어서, R₁이 수소 혹은 (C1-4)알킬이고, R₂가 퓨라닐, 페닐 혹은 플로린, 클로린, 브로민, (C1-4)알킬 혹은 (C1-4)알콕시로 단일 혹은 이중 치환된 페닐인 화합물.The compound of claim 2, wherein R 'is hydrogen or (C 1-4 ) alkyl, and R 2 is single with furanyl, phenyl or fluorine, chlorine, bromine, (C 1-4 ) alkyl or (C 1-4 ) alkoxy. Or double substituted phenyl. 제2항에 있어서, R₁이 메틸이고, R₂가 페닐인 화합물.3. The compound of claim 2, wherein R 'is methyl and R2 is phenyl. 제2항에 있어서, R₁이 메틸이고, R₂가 P-클로로페닐인 화합물.3. The compound of claim 2, wherein R 'is methyl and R2 is P-chlorophenyl. 제2항에 있어서, R₁은 n-프로필이고, R₂는 페닐인 화합물.3. The compound of claim 2, wherein R 'is n-propyl and R2 is phenyl. 제2항에 있어서, R₁은 n-메틸이고, R₂는 퓨라닐인 화합물.3. The compound of claim 2, wherein R 'is n-methyl and R2 is furanyl. 제2항에 있어서, R₁은 메틸이고, R₂는 3,4-다이메톡시페닐인 화합물.3. The compound of claim 2, wherein R 'is methyl and R2 is 3,4-dimethoxyphenyl. 제2항에 있어서, R₁은 수소이고, R₂는 페닐인 화합물.3. The compound of claim 2, wherein R 'is hydrogen and R2 is phenyl. 제2항에 있어서, R₁은 메틸이고, R₂는 P-플로로페닐인 화합물.The compound of claim 2, wherein R ₁ is methyl and R 2 is P-fluorophenyl. 제2항에 있어서, R₁은 메틸이고, R₂는 P-트리플로로 메틸페닐인 화합물.3. A compound according to claim 2, wherein R 'is methyl and R2 is P-trifluoro methylphenyl. 제2항에 있어서, (+)-이성질체 형태중, R₁은 메틸이고, R₂는 페닐인 화합물.The compound of claim 2, wherein in the (+)-isomer form R ′ is methyl and R 2 is phenyl. 제2항에 있어서, (-)-이성질체 형태중, R₁은 메틸이고, R₂는 페닐인 화합물.The compound of claim 2, wherein, in the (-)-isomer form, R 'is methyl and R2 is phenyl. 제2항에 있어서, (+)-이성질체 형태중, R₁은 메틸이고, R₂는 P-프로로페닐인 화합물.The compound of claim 2, wherein in the (+)-isomeric form R ′ is methyl and R 2 is P-proprophenyl. 제2항에 있어서, (-)-이성질체 형태중, R₁은 메틸이고, R₂는 P-플로로페닐인 화합물.The compound of claim 2, wherein, in the (-)-isomer form, R 'is methyl and R2 is P-fluorophenyl. 약제로 사용되는 제1항 내지 15항중 어느 하나에 따른 화합물.A compound according to any one of claims 1 to 15 for use as a medicament. 파킨슨씨 병의 치료에 사용되는 제1항 내지 15항중 어느 하나에 따른 화합물.The compound according to any one of claims 1 to 15 for use in the treatment of Parkinson's disease. 1차 퇴행 치매의 치료에 사용되는 제2항 내지 15항중 어느 하나에 따른 화합물.The compound according to any one of claims 2 to 15, which is used for the treatment of primary dementia. 알츠하이머 형태의 노인성 치매의 치료에 사용되는 제2항 내지 15항중 어느 하나에 따른 화합물.The compound according to any one of claims 2 to 15 used for the treatment of senile dementia in the Alzheimer's form. 억울증의 치료에 사용되는 제2항 내지 15항중 어느 하나에 따른 화합물.The compound according to any one of claims 2 to 15 used for the treatment of depression. 불안증의 치료에 사용되는 제2항 내지 15항중 어느 하나에 따른 화합물.The compound according to any one of claims 2 to 15 used for the treatment of anxiety. 비만증의 치료에 사용되는 제2항 내지 15항중 어느 하나에 따른 화합물.The compound according to any one of claims 2 to 15 used for the treatment of obesity. 고혈압의 치료에 사용되는 제2항 내지 15항중 어느 하나에 따른 화합물.The compound according to any one of claims 2 to 15 used for the treatment of hypertension. 울혈성 순환 심부전증의 치료에 사용되는 제2항 내지 15항중 어느 하나에 따른 화합물.The compound according to any one of claims 2 to 15 used for the treatment of congestive circulatory heart failure. 만성 신부전증의 치료에 사용되는 제2항 내지 15항중 어느 하나에 따른 화합물.The compound according to any one of claims 2 to 15 used for the treatment of chronic renal failure. 정신분열증의 치료에 사용되는 제2항 내지 15항중 어느 하나에 따른 화합물.The compound according to any one of claims 2 to 15 used for the treatment of schizophrenia. 약학적 담체 혹은 희석제와 함께 제1항 내지 15항중 어느 하나에 따른 화합물을 포함하는 약학 조성물.A pharmaceutical composition comprising a compound according to any one of claims 1 to 15 together with a pharmaceutical carrier or diluent. 상응하는 2,3-다이히드로-에르고린을 산화시킨다음 수득된 화합물을 유리 염기 혹은 산부가 형태로 회수하는 단계를 포함하는 유기 염기 혹은 산부가염 형태의 위치 8-미치환 및 위치 9-치환 에르고린 유도체의 제조방법.Oxidizing the corresponding 2,3-dihydro-ergorin and then recovering the obtained compound in free base or acid addition form in position 8-unsubstituted and position 9-substituted ergo in organic base or acid addition salt form. Method for preparing lean derivatives. 제2항에 있어서, 일반식(Ⅱ)의 화합물을 산화시킨 다음 수득된 일반식(Ⅰ)의 화합물을 유리 염기 혹은 산부가염 형태로 회수하는 단계를 포함하는 제조방법.The process according to claim 2, comprising the step of oxidizing the compound of formula (II) and then recovering the compound of formula (I) obtained in the form of a free base or an acid addition salt. 상기식에서, R₁및 R₂는 제2항에서 정의한 바와 같다.Wherein R 'and R2 are as defined in claim 2. 제29항에서 정의된 일반식(Ⅱ)의 화합물.A compound of formula (II) as defined in claim 29. 명세서에 기재된 일반식(Ⅲ)의 화합물.Compound of general formula (III) described in the specification. 명세서에 기재된 일반식(Ⅳ)의 화합물.A compound of formula (IV) as described in the specification. 명세서에 기재된 일반식(Ⅴ)의 화합물.A compound of formula (V) as described in the specification. 명세서에 기재된 일반식(Ⅵ)의 화합물.A compound of formula (VI) as described in the specification. 약제물로서 사용하는 제30항 내지 제34항중 어느 하나의 화합물.35. A compound according to any one of claims 30 to 34 for use as a medicament. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019890000711A 1988-01-26 1989-01-24 Ergoline derivatives KR890011882A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE3802178 1988-01-26
DEP3802178.1 1988-01-26

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KR890011882A true KR890011882A (en) 1989-08-23

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JP (1) JPH01224374A (en)
KR (1) KR890011882A (en)
AU (1) AU2872489A (en)
DK (1) DK32389A (en)
ES (1) ES2011986A6 (en)
FI (1) FI890337A (en)
FR (1) FR2626177B1 (en)
GB (1) GB2214183A (en)
GR (1) GR890100048A (en)
HU (1) HUT51275A (en)
IL (1) IL89063A0 (en)
IT (1) IT1229537B (en)
LU (1) LU87439A1 (en)
NL (1) NL8900185A (en)
PT (1) PT89518B (en)
SE (1) SE8900256L (en)
ZA (1) ZA89640B (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4033496A1 (en) * 1990-10-20 1992-04-23 Sandoz Ag NEW ERGOL DERIVATIVES, THEIR PRODUCTION AND USE
TW224091B (en) * 1992-04-03 1994-05-21 Lilly Co Eli

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PT89518B (en) 1994-02-28
JPH01224374A (en) 1989-09-07
DK32389D0 (en) 1989-01-25
FR2626177B1 (en) 1992-07-31
FI890337A0 (en) 1989-01-24
IT1229537B (en) 1991-09-04
AU2872489A (en) 1989-07-27
IT8947562A0 (en) 1989-01-24
LU87439A1 (en) 1989-08-30
FR2626177A1 (en) 1989-07-28
SE8900256L (en) 1989-07-27
IL89063A0 (en) 1989-08-15
ES2011986A6 (en) 1990-02-16
DK32389A (en) 1989-07-27
FI890337A (en) 1989-07-27
PT89518A (en) 1989-10-04
GR890100048A (en) 1994-03-31
HUT51275A (en) 1990-04-28
GB8901440D0 (en) 1989-03-15
NL8900185A (en) 1989-08-16
GB2214183A (en) 1989-08-31
SE8900256D0 (en) 1989-01-25
ZA89640B (en) 1990-09-26

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