KR940007010A - 옥사졸리딘 - Google Patents

옥사졸리딘 Download PDF

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Publication number
KR940007010A
KR940007010A KR1019930017111A KR930017111A KR940007010A KR 940007010 A KR940007010 A KR 940007010A KR 1019930017111 A KR1019930017111 A KR 1019930017111A KR 930017111 A KR930017111 A KR 930017111A KR 940007010 A KR940007010 A KR 940007010A
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South Korea
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compound
formula
hydrogen
same time
oxazolidine
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KR1019930017111A
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English (en)
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KR100306652B1 (ko
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살만 알프레트
쉬빈트 한스-페터
프란코테 에릭
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베르너 발데그
시바-가이기 에이지
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Publication of KR100306652B1 publication Critical patent/KR100306652B1/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/04—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/04—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D263/06—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by oxygen atoms, attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

본 발명은 라세미체 및 키랄 형태의 일반식(Ⅰ)의 옥사졸리딘 및 이들의 염, 이들 화합물의 제조방법, 이들을 포함하는 약제 조성물 및 약제로서의 이들의 용도에 관한 것이다.
상기식에서, R1 및 R2는 동시에 수소이거나 둘다가 동일한 저급 알킬 라디칼이거나 함께 4-내지 7-원 저급알킬렌이다.
본 발명의 화합물은 베타-아드레날린 작동성 수용체에 대한 자극 효과를 가지며, 특히, 호흡기의 가역적 폐쇄와 관련된 질환, 대표적으로 천식 및 만성 기관지염의 치료 및 또한 다른기관의 염증에 대해 사용될 수 있다.

Description

옥사졸리딘
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (13)

  1. 라세미체 및 키랄 형태의 일반식(Ⅰ)의 화합물, 또는 이의 염.
    상기식에서, R1및 R2는 동시에 수소이거나 둘다가 동일한 저급 알킬 라디칼이거나 함께 4-내지 7-원 저급알킬렌이다.
  2. 제1항에 있어서, R1 및 R2가 동시에 수소이거나 둘다가 동일한 저급알킬 라디칼이거나 함께 4-내지 5-원저급 알킬레인, 라세미체 및 키랄 형태의 일반식(Ⅰ)의 화합물 또는 이의 염.
  3. 제1항에 있어서, R1 및 R2가 동시에 수소이거나 둘다가 동시에 메틸 또는 에틸인 라세미체 및 키랄 형태의 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용되는 이의 염.
  4. 제1항에 있어서, R1 및 R2가 동시에 수소인 라세미체 또는 키랄 형태의 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용되는 이의 염.
  5. (5R)-5-(3-포르밀아미노-4-하이드록시페닐)-3-[(2R)-1-(4-메톡시페닐)프로프-2-일]옥사졸리딘 및 (5S)-5-(3-포르밀아미노-4-하이드록시페닐)-3-[(2S)-1-(4-메톡시페닐)프로프-2-일]옥사졸리딘의 라세미체, 또는 약제학적으로 허용되는 이의 염.
  6. (5R)-5-(3-포르밀아미노-4-하이드록시페닐)-3-[(2R)-1-(4-메톡시페닐)프로프-2-일]옥사졸리딘 또는 약제학적으로 허용되는 이의 염.
  7. (5R)-5-(3-포르밀아미노-4-하이드록시페닐)-3-[(2S)-1-(4-메톡시페닐)프로프-2-일]옥사졸리딘 또는 약제학적으로 허용되는 이의 염.
  8. 인체 또는 동물체의 치료 방법에 사용하기 위한 제1항 내지 제7항중 어느 한 항에 따른 화합물.
  9. 활성 성분으로서 유리 형태 또는 약제학적으로 허용되는 염 형태의 제1항 내지 제7항중 어느 한 항에 따른 화합물 및 통상의 약제학적 부형제를 포함하는 약제 조성물.
  10. 일반식(Ⅱ)의 화합물을 유리 형태 및 아세탈 또는 케탈 형태의 일반식(Ⅲ)의 화합물과 반응시키고, 필요한 경우, 이성체의 혼합물을 각각의 이성체로 분리시킨 다음, 목적하는 이성체를 분리시키고/시키거나 유리 화합물을 염으로 전환시키거나 염을 유리 화합물이나 또다른 염으로 전환시킴을 특징으로 하여, 일반식(Ⅰ)의 화합물을 제조하는 방법.
    상기식에서, R1 및 R2는 동시에 수소이거나 둘다가 동일한 저급 알킬 라디칼이거나 함께 4-내지 7-원 저급 알킬렌이다.
  11. 제10항에 있어서, 일반식(Ⅰ)의 화합물의 라세미체를 각각의 에난티오머로 분리시킴을 특징으로 하는 방법.
  12. 제10항 또는 제11항에 있어서, 일반식(Ⅰ)의 화합물의 라세미체를 키랄 고정상을 통해 컬럼 크로마토그래피로 분리시킴을 특징으로 하는 방법.
  13. 본원의 실시예중 어느 하나에 따른 제조방법, 이에 사용된 출발물질, 이로부터 수득된 중간체 및 이 제조방법으로 수득된 최종 생성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019930017111A 1992-09-02 1993-08-31 옥사졸리딘,이를포함하는약제학적조성물및이의제조방법 KR100306652B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CH2742/92-9 1992-09-02
CH02742/92-9 1992-09-02
CH274292 1992-09-02

Publications (2)

Publication Number Publication Date
KR940007010A true KR940007010A (ko) 1994-04-26
KR100306652B1 KR100306652B1 (ko) 2001-12-28

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KR1019930017111A KR100306652B1 (ko) 1992-09-02 1993-08-31 옥사졸리딘,이를포함하는약제학적조성물및이의제조방법

Country Status (14)

Country Link
US (1) US5369117A (ko)
EP (1) EP0586344B1 (ko)
JP (1) JP3070812B2 (ko)
KR (1) KR100306652B1 (ko)
AT (1) ATE170848T1 (ko)
AU (1) AU672984B2 (ko)
CA (1) CA2105215C (ko)
DE (1) DE59308970D1 (ko)
DK (1) DK0586344T3 (ko)
ES (1) ES2121071T3 (ko)
IL (1) IL106862A (ko)
NZ (1) NZ248550A (ko)
TW (1) TW223065B (ko)
ZA (1) ZA936393B (ko)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6048857A (en) * 1989-10-17 2000-04-11 Ellinwood, Jr.; Everett H. Dosing method of administering medicaments via inhalation administration
US5503869A (en) * 1994-10-21 1996-04-02 Glaxo Wellcome Inc. Process for forming medicament carrier for dry powder inhalator
CA2163399A1 (en) * 1994-11-24 1996-05-25 Katsuhiro Kawano Triazine derivative, chymase activity inhibitor and nitric oxide production inhibitor

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2366625C2 (ko) * 1972-02-05 1988-06-09 Yamanouchi Pharmaceutical Co., Ltd., Tokio/Tokyo, Jp
US3994974A (en) * 1972-02-05 1976-11-30 Yamanouchi Pharmaceutical Co., Ltd. α-Aminomethylbenzyl alcohol derivatives
US4219655A (en) * 1979-07-16 1980-08-26 Stauffer Chemical Company Process for the production of N-acyl substituted oxazolidines
US4407819A (en) * 1980-08-25 1983-10-04 American Cyanamid Company Phenylethanolamine derivatives and acid addition salts thereof for the depression of fat deposition in warm blooded animals
US4705798A (en) * 1985-09-27 1987-11-10 University Of Iowa Research Foundation Phenylephrine prodrug useful as mydriatic agent
US5066793A (en) * 1987-10-26 1991-11-19 Ciba-Geigy Corporation Finely particulate cellulose esters of aromatic or aromatic-aliphatic carboxylic acids, process for their preparation, and the use thereof

Also Published As

Publication number Publication date
CA2105215C (en) 2004-06-29
CA2105215A1 (en) 1994-03-03
ZA936393B (en) 1994-03-25
ATE170848T1 (de) 1998-09-15
EP0586344B1 (de) 1998-09-09
DE59308970D1 (de) 1998-10-15
ES2121071T3 (es) 1998-11-16
JPH06157487A (ja) 1994-06-03
NZ248550A (en) 1995-09-26
AU672984B2 (en) 1996-10-24
IL106862A (en) 1997-07-13
JP3070812B2 (ja) 2000-07-31
TW223065B (ko) 1994-05-01
EP0586344A1 (de) 1994-03-09
DK0586344T3 (da) 1999-06-07
IL106862A0 (en) 1993-12-28
KR100306652B1 (ko) 2001-12-28
US5369117A (en) 1994-11-29
AU4499393A (en) 1994-03-10

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