KR100215609B1 - Pharmaceutical compositions of quinoziline derivatives as orexigenics - Google Patents

Pharmaceutical compositions of quinoziline derivatives as orexigenics Download PDF

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Publication number
KR100215609B1
KR100215609B1 KR1019940700357A KR19940700357A KR100215609B1 KR 100215609 B1 KR100215609 B1 KR 100215609B1 KR 1019940700357 A KR1019940700357 A KR 1019940700357A KR 19940700357 A KR19940700357 A KR 19940700357A KR 100215609 B1 KR100215609 B1 KR 100215609B1
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South Korea
Prior art keywords
alkyl
hydrogen
endo
alkoxy
halogen
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KR1019940700357A
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Korean (ko)
Inventor
존티.버크
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슈테펜엘.네스비트
메렐 다우 파마슈티칼스 인크
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Application filed by 슈테펜엘.네스비트, 메렐 다우 파마슈티칼스 인크 filed Critical 슈테펜엘.네스비트
Priority claimed from PCT/US1992/005809 external-priority patent/WO1993002678A1/en
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Publication of KR100215609B1 publication Critical patent/KR100215609B1/en

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Classifications

    • AHUMAN NECESSITIES
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

본 발명은 식요증진 효과를 내는 약제를 제조하기 위한 헥사하이드로-8-하이드록시-2,6-메타노-2H-퀴놀리진-3(4H)-은 및 헥사하이드로-8-하이드록시-2,6-메타노-2H-퀴놀리진의 에스테르의 용도에 관한 것이다.The present invention provides hexahydro-8-hydroxy-2,6-methano-2H-quinolizine-3 (4H) -silver and hexahydro-8-hydroxy-2 for the preparation of a drug having a dietary boosting effect. And the use of esters of, 6-methano-2H-quinolizine.

Description

퀴노질린 유도체를 포함하는 식욕증진제로서 유용한 약제학적 조성물Pharmaceutical composition useful as an appetite enhancer comprising a quinoziline derivative

본 발명은 신규한 부류의 식욕증진제에 관한 것이다.The present invention relates to a novel class of appetite enhancers.

본 발명에 따라 하기 일반식(I)의 신규한 부류의 식욕 증진제 및 이의 약제학적으로 허용되는 산 부가염 및 4급 암모늄염이 발견되었다.According to the present invention a novel class of appetite enhancers of the general formula (I) and pharmaceutically acceptable acid addition salts and quaternary ammonium salts thereof have been found.

22 22 22 33 22 33 44 22 33 44 2-42-4 22 22 22 22 99 55 66 88 1-31-3 1-31-3 77 1-41-4 1-41-4 22 99 1-41-4 1-21-2 1010 1-41-4 1-41-4 22 1111 1-41-4 1-41-4 1-41-4 22 22 33

Claims (3)

활성 성분으로서 하기 일반식(I)의 화합물 및 이의 약제학적으로 허용되는 산 부가염 및 4급 암모늄염을 포함하는, 식욕증진제로서 유용한 약제학적조성물.A pharmaceutical composition useful as an appetite enhancer, comprising as an active ingredient a compound of the general formula (I) and pharmaceutically acceptable acid addition salts and quaternary ammonium salts thereof. 상기식에서, A는 H2, O, (H)(OH),(OH)2또는 N-OH이고: B는 H2,(H)(CH3),(H)(CH2NR3R4) 또는 CH2이며; L 및 R4는 C2-4알킬이거나 함께 테트라메틸렌, 펜타메틸렌 또는-CH2CH2-O-CH2CH2-를 형성하고;Wherein A is H 2 , O, (H) (OH), (OH) 2 or N-OH: B is H 2 , (H) (CH 3 ), (H) (CH 2 NR 3 R 4 ) Or CH 2 ; L and R 4 are C 2-4 alkyl or together form tetramethylene, pentamethylene or —CH 2 CH 2 —O—CH 2 CH 2 —; Z는 NR9, O 또는 S이고; R5, R6및 R8는 각각 수소, 할로겐, C1-3알킬 또는 C1-3알콕시이며; R7은 수소, 아미노,(C1-4알킬)아미노,(C1-4알킬)2 아미노, 알콕시 또는 니트로이고; R9는 수소, C1-4알킬 또는 페닐(C1-2알킬)이며; R10은 수소, 할로겐, C1-4알킬, C1-4알콕시, 하이드록시, 시아노 또는 -CONH2이고; R11은 수소, 할로겐, C1-4알킬 또는 페닐이며; 파선(∼)은 환의 산소 치환체의 배위가 엔도 또는 엑소일 수 있음을 나타낸다.Z is NR 9 , O or S; R 5 , R 6 and R 8 are each hydrogen, halogen, C 1-3 alkyl or C 1-3 alkoxy; R 7 is hydrogen, amino, (C 1-4 alkyl) amino, (C 1-4 alkyl) 2 amino, alkoxy or nitro; R 9 is hydrogen, C 1-4 alkyl or phenyl (C 1-2 alkyl); R 10 is hydrogen, halogen, C 1-4 alkyl, C 1-4 alkoxy, hydroxy, cyano or —CONH 2 ; R 11 is hydrogen, halogen, C 1-4 alkyl or phenyl; Dashed lines (-) indicate that the coordination of the oxygen substituents of the ring may be endo or exo. 제 1 항에 있어서, 화합물이 엔도-헥사하이드로-8-(3-인돌릴카보닐옥시)-2,6-메타노-2H-퀴놀리진-3(4H)-온인 약제학적 조성물.The pharmaceutical composition of claim 1, wherein the compound is endo-hexahydro-8- (3-indolylcarbonyloxy) -2,6-methano-2H-quinolizine-3 (4H) -one. 제 1 항에 있어서, 화합물이 엔도-8-(3-인돌릴카보닐옥시)-2,6-메타노옥타하이드로-2H-퀴놀리진-3-을인 약제학적 조성물.The pharmaceutical composition of claim 1, wherein the compound is endo-8- (3-indolylcarbonyloxy) -2,6-methanooctahydro-2H-quinolizine-3-.
KR1019940700357A 1991-08-09 1992-07-09 Pharmaceutical compositions of quinoziline derivatives as orexigenics KR100215609B1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US74295191A 1991-08-09 1991-08-09
US7/.742.951 1991-08-09
PCT/US1992/005809 WO1993002678A1 (en) 1991-08-09 1992-07-09 Use of quinozilinederivatives as orexigenics

Publications (1)

Publication Number Publication Date
KR100215609B1 true KR100215609B1 (en) 1999-08-16

Family

ID=26784875

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019940700357A KR100215609B1 (en) 1991-08-09 1992-07-09 Pharmaceutical compositions of quinoziline derivatives as orexigenics

Country Status (3)

Country Link
KR (1) KR100215609B1 (en)
CA (1) CA2113623C (en)
NO (1) NO940417D0 (en)

Also Published As

Publication number Publication date
CA2113623A1 (en) 1993-02-18
NO940417L (en) 1994-02-08
CA2113623C (en) 2006-10-10
NO940417D0 (en) 1994-02-08

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