KR930010047A - 아미노알칸포스핀산 및 이의 염 - Google Patents

아미노알칸포스핀산 및 이의 염 Download PDF

Info

Publication number
KR930010047A
KR930010047A KR1019920021950A KR920021950A KR930010047A KR 930010047 A KR930010047 A KR 930010047A KR 1019920021950 A KR1019920021950 A KR 1019920021950A KR 920021950 A KR920021950 A KR 920021950A KR 930010047 A KR930010047 A KR 930010047A
Authority
KR
South Korea
Prior art keywords
ethyl
hydroxy
propyl
phosphinic acid
amino
Prior art date
Application number
KR1019920021950A
Other languages
English (en)
Inventor
죤 미켈 스튜어트
Original Assignee
베르너 발데크
시바-가이기 에이지
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 베르너 발데크, 시바-가이기 에이지 filed Critical 베르너 발데크
Publication of KR930010047A publication Critical patent/KR930010047A/ko

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/655Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
    • C07F9/65515Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring
    • C07F9/65517Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring condensed with carbocyclic rings or carbocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/30Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/301Acyclic saturated acids which can have further substituents on alkyl
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/58Pyridine rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/60Quinoline or hydrogenated quinoline ring systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Air Bags (AREA)

Abstract

하기 일반식(I)의 화합물 및 이의 염은 GABAB-길항 특성을 지니며 GABAB-길항제에 응하는 질병의 치료에 사용할 수 있다.
상기식에서 R, R1, 내지 R3는 본 명세서에서 정의한 바와 동일하다.

Description

아미노알칸포스핀산 및 이의 염
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (16)

  1. 일반식(I)의 화합물 또는 이의 염.
    상기식에서, a)R은 부틸이고, R1은 수소이고, R2는 3,4-디클로로벤질, 1-(4-클로로페닐)에틸 또는 1-(3,4-디클로로페닐)에틸이고, R3은 수소이거나, b)R은 디에톡시메틸이고, R1은 수소이고, R2는 2,6-또는 3,5-디클로로벤질, 피리드-3-일메틸, 1-(4-메톡시페닐)에틸, 1-(4-클로로-3-요오드-페닐)에틸 또는 1-(3-클로로-4-요오드-페닐)에틸이고, R3은 수소이거나, 또는 R은 디에톡시메틸이고, R1은 하이드록시이고, R2는 3,4-디클로로벤질, 1-(3-클로로-4-요오드-페닐)에틸, 1-(4-클로로-3-요오드-페닐)에틸 또는 1-(3,4-디클로로벤질)에틸이고, R3은 수소이거나, c)R은 사이클로헥실메틸이고, R1은 수소이고, R2는 3,5-디클로로벤질, 퀴놀린-4-일-메틸, 1-(3-클로로페닐)에틸 또는 1-(3,4,5-트리메톡시페닐)에틸이고, R3은 수소이거나, R은 사이클로헥실메틸이고, R1은 하이드록시이고, R2는 3,4-디메틸벤질, 3,4-메틸렌디옥시벤질, 1-(3-클로로페닐)에틸, 1-(3,4-디클로로페닐)에틸, 1-(3-클로로-4-요오드-페닐)에틸, 1-(4-클로로-3-요오드-페닐)에틸, 1-(2,4-디메톡시페닐)에틸, 1-(2,5-디메톡시페닐)에틸, 1-(2,6-디메톡시페닐)에틸, 1-(3,4-디메톡시페닐)에틸, 1-(3,4-메틸렌디옥시페닐)에틸, 1-(3,5-디메톡시-페닐)에틸, 1-(3,4,5-트리메톡시페닐)에틸, 3-페닐프로프-2-일, 2-(3,4-디클로로페닐)프로필, 2-(3,4-디클로로페닐)프로필, 3-(,4-디클로로페닐)프로프-2-일 또는 3-페닐-3-하이드록시-프로프-2-일이고, R3는 수소이거나, 또는 R은 사이클로헥실메틸이고, R1은 수소이고, R2는 4-클로로벤질이고, R3은 메틸이거나, d)R은 사이클로헥스-3-에닐메틸이고, R1은 (S)-하이드록시이고, R2는 1(S)-(3,4-디클로로페닐)에틸이고, R3는 수소이거나, e)R은 벤질이고, R1은 하이드록시이고, R2는 α-사이클로프로필-3,4-디클로로-벤질, 3,4,5-트리메톡시벤질, 1-(3,5-디메톡시페닐)에틸, 1-(3,4-디클로로페닐)에틸, 2-(3,4-디클로로페닐)에틸, 1-(3-클로로-4-요오드-페닐)에틸, 1-(3,4-디클로로페닐)-2-하이드록시-에틸, 2-(,3,4-디클로로페닐)-2-하이드록시-에틸, 1-(2,4-디메톡시페닐)에틸, 1-(2,5-디메톡시페닐)에틸, 1-(2,6-디메톡시페닐)에틸, 1-(3,4-디메톡시페닐)에틸, 1-(3,4-메틸렌디옥시페닐)에틸, 1-(3,4,5-트리메톡시페닐)에틸, 3-페닐프로프-2-일, 3-페닐-3-하이드록시-프로프-2-일, 1-,2-, 또는 3-(3,4-디클로로페닐)프로필, 3-(3,4-디클로로페닐)프로프-2-일, 3-(3,4-디클로로페닐)-3-하이드록시-프로프-2-일 또는 4-(3,4-디클로로페닐)부틸이고, R3는 수소이거나, 또는 f)R은 4-클로로벤질, 4-메틸벤질, 4-메톡시벤질 또는 사이클로헥스-3-에틸메틸이고, R1, R2, 및 R3은 수소이다.
  2. 제1항에 있어서, R이 사이클로헥실메틸 또는 벤질이고, R1이 하이드록시이고, R2가 1-(2,4-메톡시페닐)에틸, 1-(2,5-디메톡시페닐)에틸, 1-(2,6-디메톡시페닐)에틸, 1-(3,4-디메톡시페닐)에틸, 1-(3,4-메틸렌디옥시페닐)에틸, 1-(3,5-디메톡시페닐)에틸 또는 1-(3,4,5-트리메톡시)펜에틸이고, R3이 수소인 일반식(I)의 화합물 또는 이의 염.
  3. 제1항에 있어서, R이 사이클로헥실메틸 또는 벤질이고, R1이 하이드록시이고, R2가 1-(3,4,5-트리메톡시페닐)에틸이고, R3이 수소인 일반식(I)의 화합물 또는 이의 염.
  4. 제1항 내지 제3항 중의 어느 한 항에 있어서, R1이 하이드록시이고, 1-(3,4-디클로로-, 3-클로로-4-요오드-, 4-클로로-3-요오드-, 2,4-디메톡시-, 2,5-디메톡시-, 2,4-디메톡시-, 3,4-디메톡시-, 3,5-디메톡시, 3,4,5-트리메톡시- 및 3,4-메틸렌디옥시페닐)에틸, α-사이클로프로필-4,4-디클로로-벤질 및 1-(3,4-디클로로페닐)프로필의 하이드록시 그룹 함유 탄소원자 및, 존재하는 경우, α-탄소원자가 (S)-배위를 갖고, R, R2및 R3은 각각의 경우에 위에서 정의한 바와 동일한 일반식(I)의 화합물 또는 이의 염.
  5. 3-{N-[1-(3,4,5-트리메톡시페닐)에틸]아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산 또는 이의 염.
  6. 3-{N-[1(S)-(3,4,5-트리메톡시페닐)에틸]아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산 또는 이의 염.
  7. 3-{N-[1-(3,4-메틸렌디옥시페닐)에틸]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산 또는 이의 염.
  8. 3-{N-[1-(3,4-디메톡시페닐)에틸]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산 또는 이의 염.
  9. 3-{N-[1-(3,4-디메톡시페닐)에틸]아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산 또는 이의 염.
  10. 3-{N-[1-(3,4-메틸렌디옥시페닐)에틸]아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산 또는 이의 염.
  11. 3-{N-[1-(3,4-메틸렌디옥시페닐)아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산 또는 이의 염.
  12. 3-{N-[1(S)-(3,4,5-트리메톡시페닐)에틸]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산 또는 이의 염.
  13. 3-(3,5-디클로로벤질아미노)프로필(디에톡시메틸)포스핀산, 3-{N-1-(3,4-디클로로페닐)에틸]아미노}-2(S)-하이드록시-프로필(사이클로헥실메틸)포스핀산, 3-{N-(2,6-디클로로벤질)아미노]프로필-(디에톡시메틸)-포스핀산 또는 이의 염, 3-[N-(피리드-3-일메틸)아미노]프로필-(디에톡시메틸)-포스핀산, 3-{N-[1-(4-메톡시페닐)에틸]아미노)프로필-(디에톡시메틸)-포스핀산, 3-[N-(3,4,5-트리메톡시벤질)아미노]-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[-1-(3,4-디클로로페닐)에틸]아미노}-2(S)-하이드록시-프로필(벤질)-포스핀산, 3-{N-[-1-(3,4-디클로로페닐)에틸]아미노}-2(S)-하이드록시-프로필-(사이클로헥스-3-에닐메틸)-포스핀산, 3-[(3,5-디클로로벤질)아미노]-프로필-(사이클로헥실메틸)-포스핀산, 3-[N-퀴놀린-4-일)메틸아미노]-프로필-(사이클로헥실메틸)-포스핀산, 3-[N-(4-클로로벤질)-N-메틸-아미노]-프로필-(사이클로헥실메틸)-포스핀산, 3-[N-(3,4-클로로벤질)아미노]-프로필-(부틸)-포스핀산, 3-{N-[1-(4-클로로페닐)에틸아미노}-프로필-(부틸)-포스핀산 또는 이의 염, 3-{N-[1-(3,4-디클로로페닐)에틸아미노}-프로필-(부틸)-포스핀산 또는 이의 염, 3-{N-[1-(3-클로로-4-요오드-페닐)에틸]아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[1-4-클로로-3-요오드-페닐)에틸]아미노)-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[1-(4-클로로-3-요오드-페닐)에틸]아미노)프로필-(디에톡시메틸)-포스핀산, 3-{N-[1(S)-(3,4-디클로로페닐)에틸]아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[1(S)-(3,4-디클로로페닐)에틸]아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-[N-[1(S)-(3,4-디클로로페닐)에틸]아미노}-2(R)-하이드록시-프로필(사이콜로헥실메틸)-포스핀산, 3-[N-(3,4-디메틸벤질)아미노]-2(S)-하이드록시-프로판-(사이클로헥실메틸)-포스핀산, 3-{N-[1(R)-(3,4-디클로로페닐)에틸]아미노}-2(R)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[1(R)-(3,4-디클로로페닐)에틸]아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[1-(3-클로로-4-요오드-페닐)에틸]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[1-(3-클로로-4-요오드-페닐)에틸]아미노}프로필-(디에톡시메틸)-포스핀산, 3-{N-[1-(3,4,5-트리메톡시페닐)에틸]아미노}프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[1-(3,4-디클로로페닐)에틸]아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산,3-{N-[1(3,4-디클로로페닐)에틸]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산,3-[N-[1(S)-(3,4,5-트리메톡시페닐)에틸]아미노}프로필-(사이콜로헥실메틸)-포스핀산,3-[N-(3,4-디클로로-α-사이클로프로필-벤질)아미노]-2(S)-하이드록시-프로필-(벤질)-포스핀산) 3-{N-[1-(2,5-디메톡시페닐)에틸]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[1(3,4-메틸렌디옥시페닐)에틸]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[1-(3,4-디메톡시페닐)에틸]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[1-(2,5-디메톡시페닐)에틸아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[1-(2,6-디메톡시페닐)에틸아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[1-(3,4-디메톡시페닐)에틸아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[1-(2,4-디메톡시페닐)에틸아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산,3-{N-[1-(3,4-디메톡시페닐)에틸아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산,3-{N-[1-(3,4-디메톡시페닐)에틸아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[1(S)-(3,4,5-트리메톡시페닐)에틸]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산,3-[N-(3,4-디클로로벤질)아미노}-2(S)-하이드록시-프로필-(디에톡시메틸)-포스핀산, 3-아미노-2(S)-하이드록시-프로필-(4-메톡시벤질)-포스핀산 또는 이들의 염.
  14. 3-{N-[1-(3,5-디메톡시페닐)에틸])아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[1(R)-(3,4-디클로로로페닐)에틸])아미노}-2(S)-하이드록시-프로필-(사이클로헥스-3-에닐메틸)-포스핀산, 3-{N-[1(S)-(3,4-디클로로페닐)에틸])아미노}-2(R)-하이드록시-프로필-(사이클로헥스-3-에닐메틸)-포스핀산
    3-{N-[1(R)-(3,4-디클로로페닐)에틸])아미노}-2(S)-하이드록시-프로필-(사이클로헥스-3-에닐메틸)-포스핀산, 3-{N-[1(R)-(3,4-클로로페닐)에틸])아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[1(S)-(3,4-디클로로페닐)에틸])아미노}-2(R)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[1(R)-(3,4-디클로로페닐)에틸])아미노}-2(S)-하이드록시-프로필-(디에톡시메닐)-포스핀산, 3-{N-[1(S)-(3,4-디클로로페닐)에틸])아미노}-2(S)-하이드록시-프로필-(디에톡시메닐)-포스핀산, 3-{N-[1(R)-(3,4-디클로로페닐)에틸])아미노}-2(S)-하이드록시-프로필-(디에톡시메닐)-포스핀산, 3-{N-[3-(3,4-디클로로페닐)에틸])아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[3(R)-(페닐)프로프-2(R)-일]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[3(R)-(페닐)프고로프-2(R)-일]아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[3(R)-(페닐)-3-하이드록시-프로프-2(R)-일]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[3(R)-(페닐)-3-하이드록시-프로프-2(R)-일]아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[3-(3,4-디클로로페닐)-3-하이드록시-프로프-2-일]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[2-3,4-디클로로페닐)프로필)아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 3-{N-[2-3,4-디클로로페닐)프로필)아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[3-(3,4-디클로로페닐)프로프)-2-일]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[4-(3,4-디클로로페닐)부트)-3-일]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[1-(3,4-디클로로페닐)-2-하이드록시-에틸]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[2-(3,4-디클로로페닐)-2-하이드록시-에틸]아미노}-2(S)-하이드록시-프로필-(벤질)-포스핀산, 3-{N-[1(S)-(3-클로로페닐)에틸]아미노}프로필-(사이클로헥실메틸)포스핀산 또는 3-{N-[1(S)-(3-클로로페닐)에틸]아미노}-2(S)-하이드록시-프로필-(사이클로헥실메틸)-포스핀산, 또는 이들의 염.
  15. 제1항 내지 14항 중의 어느 한 항에 따른 화합물을 통상적인 약제학적 부형제 및 담체와 함께 포함하는 약제학적 조성물.
  16. 일반식(Ⅱ)의 화합물 또는 이의 염에서, 하이드록시-보호 그룹 R6을 수소로 치환시켜 하이드록시 그룹을 유리시키고, 경우에 따라서 이모노-보호 그룹 R8로부터 하이드록시 그룹 R1을 유리시키고, 경우에 따라서 생성된 화합물을 일반식 (I)의 상이한 화합물로 전환시키고, 본 방법에 따라서 수득 가능한 이서아체 혼합물을 단일 성분으로 분리하고, 바람직한 이성체를 분리하고/분리하거나, 본 방법에 따라 수득 가능한 유리 화합물을 염으로 전환시키거나, 또는 본 방법에 따라 수득 가능한 염을 상응하는 유리 화합물로 전환시킴을 특징으로 하여 일반식(I)의 화합물 또는 이의 염을 제조하는 방법.
    상기식에서, R 및 R1내지 R3은 제1항에서 정의한 바와 동일하고, R5는 수소 또는 보호된 하이드록시이고, R6은 하이드록시 -보호 그룹이고, R8는 그룹 R3또는 아미노-보호 그룹니다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920021950A 1991-11-21 1992-11-21 아미노알칸포스핀산 및 이의 염 KR930010047A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH340491 1991-11-21
CH03404/91-9 1991-11-21

Publications (1)

Publication Number Publication Date
KR930010047A true KR930010047A (ko) 1993-06-21

Family

ID=4255259

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019920021950A KR930010047A (ko) 1991-11-21 1992-11-21 아미노알칸포스핀산 및 이의 염

Country Status (14)

Country Link
US (2) US5376684A (ko)
EP (2) EP0543780A3 (ko)
JP (1) JPH05247069A (ko)
KR (1) KR930010047A (ko)
AU (2) AU662938B2 (ko)
CA (1) CA2083307A1 (ko)
FI (1) FI925243A (ko)
IL (1) IL103808A0 (ko)
MX (1) MX9206702A (ko)
NO (4) NO924479L (ko)
NZ (1) NZ245185A (ko)
PH (1) PH30097A (ko)
TW (1) TW213466B (ko)
ZA (1) ZA928979B (ko)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL114631A (en) * 1990-06-22 1998-12-06 Novartis Ag Anti-epileptic preparations containing antagonists of BABAG
EP0543780A3 (en) * 1991-11-21 1993-09-01 Ciba-Geigy Ag Novel aminoalkanephosphinic acids and their salts
AU662404B2 (en) * 1992-05-08 1995-08-31 Novartis Ag Novel N-aralkyl- and N-heteroaralkyl-aminoalkanephosphinic acids
AU7130196A (en) * 1995-09-28 1997-04-17 Novartis Ag Novel hydroxylated and alkoxylated N- and/or P-aralkylphosphinic acid derivatives
ATE282625T1 (de) * 1997-06-23 2004-12-15 Polychip Pharmaceuticals Pty Gaba-c-rezeptor-antagonisten zur stimulation des erinnerungsvermögens
DE10014127A1 (de) * 2000-03-22 2001-10-18 Hassan Jomaa Verwendung von phosphororganischen Verbindungen zur Behandlung von Infektionen
US6462084B1 (en) 2001-05-14 2002-10-08 Brookhaven Science Associates, Llc Treatment for obsessive-compulsive disorder (OCD) and OCD-related disorders using GVG
AR045794A1 (es) * 2003-09-23 2005-11-16 Aventis Pharma Inc Procedimiento para preparar derivados de acido 3- amino-2- hidroxipropilfosfinico
GB0327186D0 (en) 2003-11-21 2003-12-24 Novartis Ag Organic compounds
WO2006050472A2 (en) * 2004-11-03 2006-05-11 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous and -phosphinic acids
WO2006050471A2 (en) * 2004-11-03 2006-05-11 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs of sulfinic acids, methods of synthesis, and use
AU2006213663A1 (en) * 2005-02-11 2006-08-17 Aventis Pharmaceuticals Inc. Substituted propane phosphinic acid esters
WO2008033572A1 (en) * 2006-09-15 2008-03-20 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs, methods of synthesis and use

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2440239A1 (de) * 1974-08-22 1976-03-04 Hoechst Ag Innere ammoniumsalze von phosphinsaeuren
DE3362581D1 (en) * 1982-04-23 1986-04-24 Ciba Geigy Ag Herbicide and plant-growth regulator product
US4536355A (en) * 1982-10-08 1985-08-20 Zoecon Corporation Phenoxyphenylaminoalkylphosphinates useful in weed control
US5243062A (en) * 1984-10-12 1993-09-07 Ciba-Geigy Corporation Substituted propane-phosphonous acid compounds
GB8425872D0 (en) * 1984-10-12 1984-11-21 Ciba Geigy Ag Chemical compounds
DK704488D0 (da) * 1988-12-19 1988-12-19 Novo Industri As Nye n-substituerede azaheterocykliske carboxylsyrer
US5190933A (en) * 1987-12-04 1993-03-02 Ciba-Geigy Corporation Substituted propane-phosphinic acid compounds
US5300679A (en) * 1987-12-04 1994-04-05 Ciba-Geigy Corporation Substituted propane-phosphinic acid compounds
GB8728483D0 (en) * 1987-12-04 1988-01-13 Ciba Geigy Ag Chemical compounds
DK270488D0 (da) * 1988-05-18 1988-05-18 Novo Industri As Hidtil ukendte o-substituerede ketoximer
GB8820266D0 (en) * 1988-08-26 1988-09-28 Smith Kline French Lab Compounds
US5281747A (en) * 1989-05-13 1994-01-25 Ciba-Geigy Corporation Substituted aminoalkylphosphinic acids
GB8911017D0 (en) * 1989-05-13 1989-06-28 Ciba Geigy Ag Substituted aminoalkylphosphinic acids
US5190934A (en) * 1989-06-03 1993-03-02 Ciba-Geigy Corporation P-subsituted propane-phosphinic acid compounds
GB8912814D0 (en) * 1989-06-03 1989-07-19 Ciba Geigy Ag P-substituted propane-phospinic acid compounds
IL114631A (en) * 1990-06-22 1998-12-06 Novartis Ag Anti-epileptic preparations containing antagonists of BABAG
EP0543780A3 (en) * 1991-11-21 1993-09-01 Ciba-Geigy Ag Novel aminoalkanephosphinic acids and their salts
AU662404B2 (en) * 1992-05-08 1995-08-31 Novartis Ag Novel N-aralkyl- and N-heteroaralkyl-aminoalkanephosphinic acids

Also Published As

Publication number Publication date
AU662938B2 (en) 1995-09-21
NO924479D0 (no) 1992-11-20
NO974116D0 (no) 1997-09-08
NZ245185A (en) 1995-04-27
AU4045695A (en) 1996-04-26
NO924479L (no) 1993-05-24
FI925243A0 (fi) 1992-11-18
CA2083307A1 (en) 1993-05-22
NO974117L (no) 1993-05-24
MX9206702A (es) 1994-06-30
NO974116L (no) 1993-05-24
NO974115L (no) 1993-05-24
IL103808A0 (en) 1993-04-04
PH30097A (en) 1996-12-27
NO974115D0 (no) 1997-09-08
TW213466B (ko) 1993-09-21
US5500418A (en) 1996-03-19
EP0767174A1 (de) 1997-04-09
EP0543780A2 (de) 1993-05-26
ZA928979B (en) 1994-04-15
FI925243A (fi) 1993-05-22
AU2850492A (en) 1993-05-27
NO974117D0 (no) 1997-09-08
US5376684A (en) 1994-12-27
EP0543780A3 (en) 1993-09-01
JPH05247069A (ja) 1993-09-24

Similar Documents

Publication Publication Date Title
KR930010047A (ko) 아미노알칸포스핀산 및 이의 염
ES545885A0 (es) Un metodo para preparar 4-(4-(dimetilamino)-1-(4'-fluoro- fenil)-1-hidroxibutil)-3-(hidroximetil)-benzonitrilo
AR247558A1 (es) COMPUESTO HERBICIDA3-°/O-CICLOPROPILCARBONIL)-FENIL/SULFAMOIL)ç-3-(4, 6-DIMETOXI-2-PIRIMID INIL)-UREA, SU PREPARACION Y APLICACION COMPOSICION QUE LO COMPRENDE E INTERMEDIARIO PARA PREPARARLO
SE8302464D0 (sv) Aromatiskt alkanderivat samt sett for framstellning derav
BR9206552A (pt) Composto, processo para a preparação do mesmo, composição inseticida ou acaricida e processo de combater pregas de insetos ou acarinas
RU93005057A (ru) Фармацевтические соединения, производные тиенобензодиазепина, способ их получения, фармкомпозиция и их использование
RU99122603A (ru) Новые производные пиримидина и способы их получения
RU94004997A (ru) Производные полизамещенных 2-амидо-4-фенилтиазолов, способ их получения, промежуточные соединения синтеза и фармацевтическая композиция на их основе
RU2002133458A (ru) Соединения пиперазина и пиперидина
ATE202079T1 (de) Krampflösende, enantiomere aminosäure-derivate
ES2166972T3 (es) Procedimiento para preparar alfa-hidroxiacidos libres a partir de sus sales amonicas.
ATE74598T1 (de) Optisch aktive salze aus einem substituierten thiazolidin-4-carboxylat und 3-chlor-2hydroxypropyltrimethylammonium, deren herstellung und verwendung.
EA199800019A1 (ru) Способ повышения плотности кальциевых каналов
BR9204827A (pt) Composto de haloalquiltio,-sulfinil e-sulfonil arilpirrol,processo para controlar insetos e acaros,e,composicao para controlar insetos e acaros
ATE56716T1 (de) 2,4-diphenyl-1,3-dioxane.
ATE183995T1 (de) Herstellung von mit enantiomer angereicherten ortho-substituierten alpha, alpha-diaromatischen methanolen
ATE1997T1 (de) Verfahren zur gewinnung der enantiomeren formen von 4-cyan-1-(n-methyl-n-(2'-((3'',4''dimethoxyphenyl))-ethyl)-amino)-5-methyl-4(3',4',5'-trimethoxyphenyl)-hexan und dessen salzen.
FI853685A0 (fi) Nya n-alk(en)yl-n-(o,o-disubstituerade -tiofosforyl)-n'n'-disubstituerade glycinamider, foerfarande foer framstaellning av dessa samt kvalstergifter, insektgifter och svampgifter vilka innehaoller dessa som aktiv bestaondsdel.
DE3587252T2 (de) Keten-s,s,-acetalderivate, verfahren zu ihrer herstellung und methode zur heilung von mykose unter verwendung dieser derivate.
BR0101630A (pt) Processo para a preparação do trihidrato do salmesilato de1-(4-hidroxifenil)-2(4-hidróxi-4fenilpiperidin-1-il)-1-propanol
EP0382506A3 (en) Optically active diastereomer salts of tetrahydro-2-furoic acid
ATE304535T1 (de) Verfahren zu herstellung von 3(2h)pyridazinon-4- substituierte amino-5-chloro derivate
KR900001696A (ko) 궤양치료 활성을 갖는 1.4-디아제핀 유도체
MX9200286A (es) Compuesto de piridino sulfon amida sustituida, o ssal; proceso para prepararlo y herbicida que lo contiene.
ES2110974T3 (es) Procedimiento para la preparacion de (s)-vinil y de (s)-alenil-gaba.

Legal Events

Date Code Title Description
N231 Notification of change of applicant
A201 Request for examination
E902 Notification of reason for refusal
E601 Decision to refuse application