KR930019669A - 신놀린-3-카르복실산 유도체 - Google Patents

신놀린-3-카르복실산 유도체 Download PDF

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KR930019669A
KR930019669A KR1019930003561A KR930003561A KR930019669A KR 930019669 A KR930019669 A KR 930019669A KR 1019930003561 A KR1019930003561 A KR 1019930003561A KR 930003561 A KR930003561 A KR 930003561A KR 930019669 A KR930019669 A KR 930019669A
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hydrogen atom
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aralkyl
alkyl group
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KR1019930003561A
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아끼라 마루야마
시게루 오가와
사또시 야마자끼
아끼히로 도베
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에도오 다께도시
미쓰비시 가세이 가부시기가이샤
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Publication of KR930019669A publication Critical patent/KR930019669A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • 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
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Anesthesiology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

아래의 일반식(I)으로 나타내어지는 신놀린 유도체, 그 약학적으로 허용되는 염, N-옥사이드 유도체 또는 그 용매화물
본 발명의 화합물은 5-HT3수용체 길항작용을 가지고 있어서 중추 신경계의 장해, 소화기계의 여러가지 질환, 두통, 신경통, 부정맥등의 예방, 치료에 유용하다.

Description

신놀린-3-카르복실산 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. 아래의 일반식(I)으로 나타내어지는 신놀린 유도체, 그 제약학적으로 허용되는 염, N-옥사이드 유도체 또는 그 용매화물
    위의 식(I)에서, x는-O-또는--(여기서 R4는 수소 원자 또는 C1~C5의 알칼기를 나타냄)을 나타내고, A는 아래의 일반식(Ⅱ),(Ⅲ) 또는 (Ⅳ)을 나타내며
    (위의 식에서 n은 1~5의 정수를 나타내고, R5는 수 소원자, C1~C5의 알킬기, C3~C8의 시클로알킬기 또는 C7~C15의 아랄킬기를 나타냄), R|1은 수소원자, C1~C5의 알킬기, C2~C5의 알케닐기, C2~C4의 알키닐기, C3~C|8의 시클로알킬기, C4~C9의 시클로알킬알킬기, C2~C10의 알콕시알킬기 또는 C7~C15의 아랄킬기를 나타내고, R2와R3는 각각 독립하여 수소 원자, 할로겐 원자, 트리플루오로메틸기, 히드록실기, C1~C5의 알콕시기, 시아노기, 니트로기, 아미노기, C1~C5의 알킬아미노기, C2~C10의 디알킬아미노기, C1~C5의 알킬티오기, C1~C5의 알킬기, C3~C8의 시클로알킬기, C7~C15의 아랄킬기 또는 C2~C10의 아실기를 나타낸다.
  2. 제1항에 있어서 X가 -O- 또는 -R4- (여기서 R4는 수소 원자를 나타냄)을 나타내고 A가 아래의 일반식(Ⅱ),(Ⅲ) 또는 (Ⅳ)을 나타내며
    (위의 식에서 n은 2-4의 정수를 나타내고, R5는 수소 원자, C1~C5의 알킬기, C7~C15의 아랄킬기를 나타냄), R1이 수소 원자, C1~C5의 알킬기, C2~C5의 알케닐기, C3~C8의 시클로알킬기, C4~C8의 시클로알킬알킬기, C2~C|10의 알콕시알킬기 또는 C7~C15의 아랄킬기를 나타내고, R2와 R3은 각각 독립하여 수소 원자, 할로겐 원자, 트리플루오로메틸기, 히드록실기, C1~C5의 알콕시기, 시아노기, 니트로기, 아미노기, C1~C15의 알킬티오기, C1~C5의 알킬기, C7~C15의 아랄킬기 또는 C2~C10의 아실기를 나타냄을 특징으로 하는 화합물.
  3. 제2항에 있어서, A가 아래의 일반식(Ⅱ) 또는 (Ⅲ)을 나타내고
    (위의 식에 n은 2 또는 3의 정수를 나타내고 R5는 C1~C5의 알킬기, 또는 C7~C15의 아랄킬기를 나타냄), R1이 수소 원자 C1~C5알칼기, C2~C5의 알케닐기 또는 C7~C15의 아랄킬기를 나타내고, R2와 R3이 각각 독립하여 수소 원자, 할로겐 원자, C1~C5의 알콕시기 또는 C1~C5의 알킬기를 나타냄을 특징으로 하는 화합물.
  4. 제3항에 있어서 X가 -R4- (여기서 R4는 수소 원자를 나타냄)을 나타내고, A가 아래의 일반식(Ⅱ)을 나타내며
    (위의 식에 n은 2 또는 3의 정수를 나타내고, R5는 C1~C5의 알킬기를 나타내고),
    R1이 C1~C5의 알킬기를 나타내고, R2와 R3은 각각 독립하여 수소 원자 또는 할로겐 원자를 나타냄을 특징으로 하는 화합물.
  5. 제1항 기재의 화합물 및 약학상 허용되는 담체를 함유하여서 됨을 특징으로 하는 의약 조성물.
  6. 제1항 기재의 화합을 유효성분으로 하는 위장운동 장해에 의한 질병의 예방, 치료약.
  7. 제1항 기재의 화합물을 유효성분으로 하는 진통약.
  8. 제1항 기재의 화합물을 유효성분으로 하는 토기(吐氣) 및/또는 구토의 예방, 치료약.
  9. 제1항 기재의 화합물을 유효성분으로 하는 불안 및/또는 신경병의 예방, 치료약.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019930003561A 1992-03-12 1993-03-10 신놀린-3-카르복실산 유도체 KR930019669A (ko)

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JP (1) JPH05310732A (ko)
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AT (1) ATE148466T1 (ko)
CA (1) CA2091375A1 (ko)
DE (1) DE69307749T2 (ko)
DK (1) DK0560604T3 (ko)
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DK0560604T3 (da) 1997-04-14
EP0560604A1 (en) 1993-09-15
JPH05310732A (ja) 1993-11-22
DE69307749T2 (de) 1997-05-15
DE69307749D1 (de) 1997-03-13
ATE148466T1 (de) 1997-02-15
US5391549A (en) 1995-02-21
CA2091375A1 (en) 1993-09-13
ES2099904T3 (es) 1997-06-01
EP0560604B1 (en) 1997-01-29
US5556851A (en) 1996-09-17

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