KR880011147A - 트리아졸론 유도체 - Google Patents

트리아졸론 유도체 Download PDF

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Publication number
KR880011147A
KR880011147A KR1019880002863A KR880002863A KR880011147A KR 880011147 A KR880011147 A KR 880011147A KR 1019880002863 A KR1019880002863 A KR 1019880002863A KR 880002863 A KR880002863 A KR 880002863A KR 880011147 A KR880011147 A KR 880011147A
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South Korea
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alkyl
formula
compound
aryl
hydrogen
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KR1019880002863A
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KR960012370B1 (ko
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히레스 쟌
야곱스 죠제프 박스 레오
죠제프 에리사베스 반 데르 베켄 루이스
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폴 아드리안 쟌 쟈안센
쟈안센 파아마슈우티카 엔. 부이.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Communicable Diseases (AREA)
  • Animal Behavior & Ethology (AREA)
  • Oncology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Auxiliary Devices For And Details Of Packaging Control (AREA)

Abstract

내용 없음

Description

트리아졸론 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 일반식(I)의 화합물, 그 산부염 또는 그 입체화학이성체
    위의 일반식에서, Q는 N 또는 CH이고, R은 수소, C1-6알킬 또는 아릴 C1-6알킬이고, R1은 수소, C1-6알킬 또는 아릴 C1-6알킬이고, 아릴은 페닐이거나, 할로, C1-6알킬, C1-6알킬옥시 및 트리플루오로메틸로 이루어진 그룹으로부터 선택한 3이하의 치환기로 치환된 페닐이다.
  2. 제1항에 있어서, R 및 R1이 각각 수소 또는 C1-6알킬인 화합물.
  3. 제2항에 있어서, R1이 수소이고, R이 C1-6알킬인 화합물.
  4. 제3항에 있어서, 디옥솔란 부위의 치환기가 씨스배열을 이룬 화합물.
  5. 제1항에 있어서, Q가 질소인 화합물.
  6. 유효성분으로 일반식(I)의 화합물, 그 산부염 또는 그 입체화학 이성체를 항균, 항박테리아 작용의 유효량 함유하고 1이상의 불활성 담체로 조성된 약제 조성물.
    위의 일반식에서, Q는 N 또는 CH이고, R은 수소, C1-6알킬 또는 아릴 C1-6알킬이고, R1은 수소, C1-6알킬 또는 아릴 C1-6알킬이고, 아릴은 페닐이거나, 할로, C1-6알킬, C1-6알킬옥시, 및 트리플루오로메틸로 이루어진 그룹으로부터 선택한 3이하의 치환기로 치환된 페닐이다.
  7. 제6항에 있어서, R1이 수소이고, R이 C1-6알킬인 약제조성물.
  8. 일반식(I)의 화합물, 그 산부가염 또는 그 입체화학 이성체의 항균, 항박테리아 작용의 유효량을 온혈동물에 계통 또는 국부투여하여 균 및/또는 박테리아 감열 질환을 저지 및/또는 치료하는 방법.
    위의 일반식이고, Q는 N 또는 CH이고, R은 수소, C1-6알킬 또는 아릴 C1-6알킬이고, R1은 수소, C1-6알킬 또는 아릴 C1-6알킬이고, 아릴은 페닐이거나, 할로, C1-6알킬, C1-6알킬옥시, 및 트리플루오로메틸로 이루어진 그룹으로부터 선택한 3이하의 치환기로 치환된 페닐이다.
  9. 제8항에 있어서, R1이 수소이고, R이 C1-6알킬인 약제조성물.
  10. a) 일반식 (III)의 페놀유도체를 염기존재하에 불활성 용매중에서 일반식(II)의 디옥솔란유도체와 반응시키거나, b) 일반식(IV)의 케톤유도체를 산존재하에 불활성 용매중에서 일반식(V)의 디올유도체와 반응시키고 물을 제거시키거나, c) 일반식(VI)의 아졸유도체 또는 그 금속염을 불활성 용매 중에서 일반식(IX) 또는 (X)의 화합물로 N-알킬화 반응시키거나, d) 일반식(VIII) 또는 (XI)의 화합물을 불활성 극성용매 중에서 일반식(IX) 또는 (X)의 화합물과 각각 반응시키거나, e) 일반식(XII) 또는 (XV)의 피페라진 유도체를 불황성 용매중에서 일반식(XIII) 또는 (XIV)의 화합물과 각각 반응시키거나, f) 일반식 (XIV)의 벤젠아민 유도체 또는 일반식(XVIII)의 히드라진 카르복스아미드 유도체를 불활성용매 중에서 일반식(XVII) 또는 (XIX)의 화합물로 각각 폐환 반응시켜, 일반식(I-a)의 화합물과 생성시키거나, 일반식(I-a)의 화합물을 불활성 용매중에서 일반식(XX)의 화합물로 N-알킬화하여, 일반식(I-b)의 화합물을 생성시킴을 특징으로 하는 일반식(I-a)의 화합물, 그 산부가염 또는 그 입체화학 이성체를 제조하는 방법.
    위의 일반식에서, Q는 N 또는 CH이고, R은 수소, C1-6 알킬 또는 아릴 C1-6 알킬이고, R1은 수소, C1-6 알킬 또는 아릴 C1-6 알킬이고, 아릴은 페닐이거나, 할로, C1-6 알킬, C1-6 알킬옥시, 및 트리플루오로메틸로 이루어진 그룹으로부터 선택한 3이하의 치환기로 치환된 페닐이고, W,W1,L1및 L2은 각기 반응성 이탈기를 나타내고, R2는 C1-6알킬 또는 (아릴) C1-6알킬이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880002863A 1987-03-25 1988-03-18 4-[4-[4-[4-[[2-(2,4-디플루오로페닐)-2-(1h-아졸릴메틸)-1,3-디옥솔란-4-일]메톡시]페닐]-1-피페라지닐]페닐]트리아졸론 KR960012370B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US3020787A 1987-03-25 1987-03-25
US30,207 1987-03-25
US30207 1987-03-25

Publications (2)

Publication Number Publication Date
KR880011147A true KR880011147A (ko) 1988-10-26
KR960012370B1 KR960012370B1 (ko) 1996-09-20

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KR1019880002863A KR960012370B1 (ko) 1987-03-25 1988-03-18 4-[4-[4-[4-[[2-(2,4-디플루오로페닐)-2-(1h-아졸릴메틸)-1,3-디옥솔란-4-일]메톡시]페닐]-1-피페라지닐]페닐]트리아졸론

Country Status (25)

Country Link
EP (1) EP0283992B1 (ko)
JP (1) JPH0667929B2 (ko)
KR (1) KR960012370B1 (ko)
CN (1) CN1038588C (ko)
AT (1) ATE80626T1 (ko)
AU (1) AU600107B2 (ko)
CA (1) CA1313875C (ko)
CY (1) CY1837A (ko)
DE (1) DE3874576T2 (ko)
DK (1) DK168336B1 (ko)
ES (1) ES2044991T3 (ko)
FI (1) FI89798C (ko)
GR (1) GR3006420T3 (ko)
HK (1) HK50395A (ko)
HU (1) HU204819B (ko)
IE (1) IE61802B1 (ko)
IL (1) IL85823A (ko)
MA (1) MA21227A1 (ko)
NO (1) NO168476C (ko)
NZ (1) NZ223799A (ko)
PH (1) PH25023A (ko)
PT (1) PT87073B (ko)
SU (1) SU1635900A3 (ko)
TN (1) TNSN88025A1 (ko)
ZA (1) ZA882118B (ko)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1331757C (en) * 1988-02-29 1994-08-30 Janssen Pharmaceutica Naamloze Vennootschap 5-lipoxygenase inhibiting 4-(4-phenyl-1-piperazinyl)phenols
NZ233502A (en) * 1989-06-09 1991-11-26 Janssen Pharmaceutica Nv 4-(1,2,4-triazole- or imidazole-phenyl-substituted) -1-(1,3-dioxolan-4-ylmethoxyphenyl) piperazine derivatives; preparatory processes: fungicidal and antiviral compositions
US5075309A (en) * 1989-06-09 1991-12-24 Janssen Pharmaceutica N.V. Antifungal 4-[4-[4-[4-[[2-(2,4-difluorophenyl)-2-(1H-azolylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]triazolones and imidazolones
WO1993007847A1 (en) * 1991-10-15 1993-04-29 Kenneth Vincent Mason Anti-seborrhoeic formulation
IL103558A0 (en) * 1991-10-30 1993-03-15 Schering Corp Tri-substituted tetrahydrofuran antifungals
TW218017B (ko) * 1992-04-28 1993-12-21 Takeda Pharm Industry Co Ltd
PH30929A (en) * 1992-09-03 1997-12-23 Janssen Pharmaceutica Nv Beads having a core coated with an antifungal and a polymer.
WO1995019983A1 (en) * 1994-01-24 1995-07-27 Janssen Pharmaceutica N.V. Watersoluble azole antifungals
SK281908B6 (sk) * 1994-10-27 2001-09-11 Janssen Pharmaceutica N. V. Heteroarylsubstituované deriváty 1,3-dioxolan-4-ylmetoxyfenyl-1- piperazinylfenyl-2,4-dihydro-2-alkyl-3h-1,2,4-triazol-3-ónu, spôsob a medziprodukty na ich výrobu a farmaceutické prostriedky
US5625064A (en) * 1995-04-19 1997-04-29 Schering Corporation Process for the preparation of triazolones
TW457240B (en) 1995-04-20 2001-10-01 Janssen Pharmaceutica Nv Novel triazolones as apolipoprotein-B synthesis inhibitors
US7790905B2 (en) 2002-02-15 2010-09-07 Mcneil-Ppc, Inc. Pharmaceutical propylene glycol solvate compositions
US7446107B2 (en) 2002-02-15 2008-11-04 Transform Pharmaceuticals, Inc. Crystalline forms of conazoles and methods of making and using the same
US7927613B2 (en) 2002-02-15 2011-04-19 University Of South Florida Pharmaceutical co-crystal compositions
JP4906233B2 (ja) 2002-03-01 2012-03-28 ユニバーシティー オブ サウス フロリダ 少なくとも１種の有効薬剤成分を含有する多構成要素固相
AU2003243354A1 (en) 2002-05-31 2003-12-19 Transform Pharmaceuticals, Inc. Novel conazole crystalline forms and related processes, pharmaceutical compositions and methods
MXPA05000232A (es) 2002-06-21 2005-06-17 Transform Pharmaceuticals Inc Composiciones farmaceuticas con disolucion mejorada.
US8183290B2 (en) 2002-12-30 2012-05-22 Mcneil-Ppc, Inc. Pharmaceutically acceptable propylene glycol solvate of naproxen
US20070293674A1 (en) * 2004-04-22 2007-12-20 Transform Pharmaceuticals, Inc. Novel Saperconazole Crystalline Forms and Related Processes, Pharmaceutical Compositions and Methods
RU2585760C2 (ru) * 2010-05-19 2016-06-10 Сандоз Аг Способ получения хиральных триазолонов

Family Cites Families (3)

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US4267179A (en) * 1978-06-23 1981-05-12 Janssen Pharmaceutica, N.V. Heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidazoles and 1H-1,2,4-triazoles
US4619931A (en) * 1983-02-28 1986-10-28 Janssen Pharmaceutica, N.V. [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H-imidazoles and 1H-1,2,4-triazoles
CA1292472C (en) * 1985-12-03 1991-11-26 Alfonsus Guilielmus Knaeps Derivatives of ¬¬4-¬4-(4-phenyl-1-piperazinyl)- phenoxymethyl|-1,3-dioxolan-2-yl|methyl|-1h-imidazoles and 1h-1,2,4-triazoles

Also Published As

Publication number Publication date
JPS63277674A (ja) 1988-11-15
NO881306L (no) 1988-09-26
DE3874576T2 (de) 1993-02-18
TNSN88025A1 (fr) 1990-07-10
CN1038588C (zh) 1998-06-03
FI881404A0 (fi) 1988-03-24
EP0283992A3 (en) 1989-06-14
CY1837A (en) 1995-12-01
AU600107B2 (en) 1990-08-02
CA1313875C (en) 1993-02-23
FI881404A (fi) 1988-09-26
SU1635900A3 (ru) 1991-03-15
IL85823A0 (en) 1988-09-30
FI89798B (fi) 1993-08-13
IE61802B1 (en) 1994-11-30
IL85823A (en) 1993-05-13
DK163288A (da) 1988-09-26
FI89798C (fi) 1993-11-25
NO168476C (no) 1992-02-26
DK168336B1 (da) 1994-03-14
NO168476B (no) 1991-11-18
PT87073A (pt) 1988-04-01
NO881306D0 (no) 1988-03-24
DE3874576D1 (de) 1992-10-22
HUT50333A (en) 1990-01-29
EP0283992A2 (en) 1988-09-28
DK163288D0 (da) 1988-03-24
HK50395A (en) 1995-04-13
ZA882118B (en) 1989-11-29
HU204819B (en) 1992-02-28
ES2044991T3 (es) 1994-01-16
PH25023A (en) 1991-01-28
PT87073B (pt) 1992-07-31
KR960012370B1 (ko) 1996-09-20
ATE80626T1 (de) 1992-10-15
GR3006420T3 (ko) 1993-06-21
EP0283992B1 (en) 1992-09-16
IE880893L (en) 1988-09-25
JPH0667929B2 (ja) 1994-08-31
NZ223799A (en) 1989-12-21
MA21227A1 (fr) 1988-10-01
AU1358588A (en) 1988-09-29
CN88101660A (zh) 1988-11-09

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