BR9910448A - Azóis solúveis em água como antifúngicos de amplo aspectro - Google Patents

Azóis solúveis em água como antifúngicos de amplo aspectro

Info

Publication number
BR9910448A
BR9910448A BR9910448-2A BR9910448A BR9910448A BR 9910448 A BR9910448 A BR 9910448A BR 9910448 A BR9910448 A BR 9910448A BR 9910448 A BR9910448 A BR 9910448A
Authority
BR
Brazil
Prior art keywords
radical
alkyl
substituted
hydrogen
het1
Prior art date
Application number
BR9910448-2A
Other languages
English (en)
Inventor
Lieven Meerpoel
Leo Jacobus Jozef Backx
Louis Jozef Elisabeth Va Veken
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of BR9910448A publication Critical patent/BR9910448A/pt

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/56Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D249/12Oxygen or sulfur atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

Patente de Invenção: <B>"AZóIS SOLúVEIS EM áGUA COMO ANTIFúNGICOS DE AMPLO ESPECTRO"<D> A presente invenção refere-se a novos compostos de fórmula (I), às formas N-óxido, aos sais de adição farmaceuticamente aceitáveis e às formas estereoquimicamente isoméricas dos compostos, onde L representa um radical de fórmulas (a), (b), (c), (d), (e) ou (f); onde cada Alk independentemente representa uma C~ 1-6~alcanodiíla opcionalmente substituída; n é 1, 2 ou 3; Y é O, S ou NR²; R¹ representa arila, Het¹ ou uma C~ 1-6~alquila opcionalmente substituída; R² representa hidrogênio; ou no caso que que R¹ e R² são ligados ao mesmo átomo de nitrogênio, eles poderão ser tomados juntamente para formar um radical heterocíclico; ou eles poderão ser tomados juntamente para formar um radical azido; cada R³ independentemente representa hidrogênio, hidróxi ou C~ 1-4~alquilóxi; arila representa fenila, naftalenila, 1,2,3,4-tetraidronaftalenila, indenila ou indanila; cada um desses grupos arila poderá opcionalmente ser substituído; Het¹ representa um radical heterocíclico monocíclico ou bicíclico opcionalmente substituído; Het² é o mesmo que Het¹ e poderá também ser piperazinila, homopiperazinila, 1,4-dioxanila, morfolinila, tiomorfolinila; R^ 6^ representa hidrogênio ou C~ 1-4~alquila; R^ 7^ representa hidrogênio ou C~ 1-4~alquila; ou R^ 6^ e R^ 7^ tomados juntamente formam um radical bivalente de fórmula -N=CH- (i), -CH=N- (ii), -CH=CH-(iii), -CH~ 2~-CH~ 2~ (iv), onde um átomo de hidrogênio nos radicais (i) e (ii) poderá ser substituído por um radical C~ 1-4~alquila e um ou mais átomos de hidrogênio em radicais (iii) e (iv) poderão ser substituídos por um radical C~ 1-4~alquila; D representa um derivado de tetraidrofurano trissubstituído; como antifúngicos; a seus processos para preparação, a composições que contêm os compostos e a seu uso como medicamento.
BR9910448-2A 1998-05-14 1999-05-06 Azóis solúveis em água como antifúngicos de amplo aspectro BR9910448A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP98201588A EP0957101A1 (en) 1998-05-14 1998-05-14 Water soluble azoles as broad-spectrum antifungals
PCT/EP1999/003242 WO1999058529A1 (en) 1998-05-14 1999-05-06 Water soluble azoles as broad-spectrum antifungals

Publications (1)

Publication Number Publication Date
BR9910448A true BR9910448A (pt) 2001-01-02

Family

ID=8233724

Family Applications (2)

Application Number Title Priority Date Filing Date
BR9911057-1A BR9911057A (pt) 1998-05-14 1999-05-06 Azóis solúveis em água como antifúngicos de amplo espectro
BR9910448-2A BR9910448A (pt) 1998-05-14 1999-05-06 Azóis solúveis em água como antifúngicos de amplo aspectro

Family Applications Before (1)

Application Number Title Priority Date Filing Date
BR9911057-1A BR9911057A (pt) 1998-05-14 1999-05-06 Azóis solúveis em água como antifúngicos de amplo espectro

Country Status (31)

Country Link
US (2) US6384030B1 (pt)
EP (3) EP0957101A1 (pt)
JP (2) JP2002514645A (pt)
KR (2) KR100593395B1 (pt)
CN (2) CN1137118C (pt)
AR (2) AR016482A1 (pt)
AT (2) ATE238296T1 (pt)
AU (2) AU751135B2 (pt)
BG (2) BG64388B1 (pt)
BR (2) BR9911057A (pt)
CA (2) CA2331141C (pt)
CO (1) CO5021227A1 (pt)
CZ (2) CZ298702B6 (pt)
DE (2) DE69907171T2 (pt)
DK (1) DK1077976T3 (pt)
EE (2) EE04311B1 (pt)
ES (2) ES2182531T3 (pt)
HR (2) HRP20000740B1 (pt)
HU (2) HUP0103536A3 (pt)
IL (2) IL139649A (pt)
MY (2) MY122147A (pt)
NO (2) NO319760B1 (pt)
NZ (2) NZ507965A (pt)
PL (2) PL194085B1 (pt)
PT (1) PT1077976E (pt)
SI (1) SI1077976T1 (pt)
SK (2) SK286156B6 (pt)
TR (2) TR200003322T2 (pt)
TW (2) TWI259835B (pt)
WO (2) WO1999058529A1 (pt)
ZA (2) ZA200007173B (pt)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0957101A1 (en) * 1998-05-14 1999-11-17 Janssen Pharmaceutica N.V. Water soluble azoles as broad-spectrum antifungals
PL365072A1 (en) * 2000-03-07 2004-12-27 Ranbaxy Laboratories Limited Azole compounds as therapeutic agents for fungal infections
EP1413301A1 (fr) * 2002-10-24 2004-04-28 Bayer CropScience SA Médicaments antifongiques à base de dérivés d'arylamidine
ITMI20032020A1 (it) * 2003-10-17 2005-04-18 Italfarmaco Spa Nuovi agenti antifungini azolici con diminuita interazione con i citocromi metabolici
AR052342A1 (es) * 2004-12-21 2007-03-14 Janssen Pharmaceutica Nv Derivados sustituidos de triazolona,tetrazolona e imidazolona con actividad selectiva antagonista de alfa2c-adenoreceptores
US9040539B2 (en) * 2010-05-19 2015-05-26 Sandoz Ag Process for the preparation of chiral triazolones
WO2013036866A1 (en) * 2011-09-07 2013-03-14 The Johns Hopkins University Itraconazole analogs and use thereof
US11028078B2 (en) * 2011-09-07 2021-06-08 The Johns Hopkins University Itraconazole analogs and use thereof
HK1221606A1 (zh) 2013-06-07 2017-06-09 加州生物医学研究所 纤维化的小分子抑制剂
ES2790875T3 (es) 2014-12-05 2020-10-29 Pulmocide Ltd Compuesto antimicótico
JP6706023B2 (ja) * 2014-12-10 2020-06-03 ザ・スクリップス・リサーチ・インスティテュート 線維症の小分子阻害剤
KR102653821B1 (ko) 2015-05-21 2024-04-02 풀모사이드 리미티드 항진균성 4-(4-(4-(((3r,5r)-5-((1h-1,2,4-트리아졸-1-일)메틸)-5-(2,4-디플루오로페닐)테트라하이드로푸란-3-일)메톡시)-3-메틸페닐)피페라진-1-일)-n-(2-하이드록시사이클로헥실)벤즈아미드 또는 이의 약학적으로 허용가능한 염.
CN105237392B (zh) * 2015-11-24 2017-12-12 辽宁渤大化工有限公司 芳烷基水杨酸及其衍生物的制备方法
CA3073228A1 (en) * 2017-08-20 2019-02-28 University Of Connecticut Azole analogues and methods of use thereof
US12435067B2 (en) 2019-08-09 2025-10-07 University Of Connecticut Truncated itraconazole analogues and methods of use thereof
GB201917867D0 (en) 2019-12-06 2020-01-22 Pulmocide Ltd Polymorphs
CN111138421A (zh) * 2019-12-26 2020-05-12 上海英诺富成生物科技有限公司 抗真菌水溶性化合物及其制备方法与应用

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4218458A (en) * 1978-06-23 1980-08-19 Janssen Pharmaceutica, N.V. Heterocyclic derivatives of (4-aryloxy-methyl-1,3-dioxolan-2-yl)methyl-1H-imidazoles and 1H-1,2,4-triazoles
RU2127733C1 (ru) * 1992-03-18 1999-03-20 Жансен Фармасетика Н.В. Стереоизомеры итраконазола или саперконазола, способ их получения, их комплексы и фармацевтическая композиция на их основе
IL112081A (en) * 1993-12-21 2001-08-26 Schering Plough Corp Tetrahydrofuran derivatives, their preparation and antifungal pharmaceutical compositions containing them
ES2141329T3 (es) * 1994-01-24 2000-03-16 Janssen Pharmaceutica Nv Antifungicos azolicos solubles en agua.
FI98688C (fi) * 1994-07-20 1997-07-25 Nokia Telecommunications Oy Menetelmä lyhytsanomalähetyksen käynnistämiseksi solukkoradiojärjestelmässä, solukkoradiojärjestelmä sekä solukkoradiojärjestelmän tilaajarekisteri
IL118464A (en) * 1995-06-02 2000-08-13 Schering Corp (2R-cis)-4-¬4-¬4-¬4¬¬-5-(2',4 dihalophenyl)-tetrahydro-5-(1-H-1,2,4,triazol-1-yl-methyl)furan-3-yl(methoxy¾phenyl¾-1-piperazinyl¬phenyl2,4,dihydro2¬(5)-1-ethyl-2-(5)hydroxy propyl¾-3H-1,2,4-triazol-3-one and pharmaceutical compositions comprising them
MX9710270A (es) * 1995-06-19 1998-08-30 Schering Corp Fungicidas de tetrahidrofurano.
ID21755A (id) * 1997-02-11 1999-07-22 Janssen Pharmaceutica Nv Antijamur azol yang mengandung ester asam amino
EP0957101A1 (en) * 1998-05-14 1999-11-17 Janssen Pharmaceutica N.V. Water soluble azoles as broad-spectrum antifungals

Also Published As

Publication number Publication date
NO319760B1 (no) 2005-09-12
IL139647A0 (en) 2002-02-10
WO1999058529A1 (en) 1999-11-18
ZA200007173B (en) 2002-03-04
AU4141799A (en) 1999-11-29
CO5021227A1 (es) 2001-03-27
CN1300288A (zh) 2001-06-20
CN1300287A (zh) 2001-06-20
PL194086B1 (pl) 2007-04-30
CA2331187C (en) 2008-11-18
KR20010042852A (ko) 2001-05-25
AR016480A1 (es) 2001-07-04
DE69907171T2 (de) 2004-02-05
ES2182531T3 (es) 2003-03-01
MY120248A (en) 2005-09-30
SK16822000A3 (sk) 2001-07-10
CN1135229C (zh) 2004-01-21
BG64954B1 (bg) 2006-10-31
NZ507966A (en) 2002-10-25
HRP20000740B1 (en) 2003-12-31
DK1077976T3 (da) 2002-12-02
BR9911057A (pt) 2001-02-06
WO1999058530A1 (en) 1999-11-18
DE69902461T2 (de) 2003-04-10
SK286156B6 (sk) 2008-04-07
CZ20004108A3 (en) 2001-05-16
ATE238296T1 (de) 2003-05-15
PL344037A1 (en) 2001-09-24
HUP0102031A2 (hu) 2002-05-29
ATE221884T1 (de) 2002-08-15
CN1137118C (zh) 2004-02-04
AR016482A1 (es) 2001-07-04
HK1032781A1 (en) 2001-08-03
DE69902461D1 (de) 2002-09-12
CZ20004109A3 (en) 2001-05-16
HUP0103536A3 (en) 2002-08-28
BG64388B1 (bg) 2004-12-30
ZA200007459B (en) 2002-09-13
TR200003322T2 (tr) 2001-02-21
EP1077975A1 (en) 2001-02-28
CA2331141A1 (en) 1999-11-18
AU4361599A (en) 1999-11-29
NZ507965A (en) 2002-05-31
CZ299481B6 (cs) 2008-08-13
EP1077976B1 (en) 2002-08-07
SK16812000A3 (sk) 2001-08-06
IL139649A (en) 2004-09-27
AU758876B2 (en) 2003-04-03
EE200000651A (et) 2002-04-15
SI1077976T1 (en) 2003-02-28
CA2331187A1 (en) 1999-11-18
EE200000657A (et) 2002-04-15
JP2002514645A (ja) 2002-05-21
EE04311B1 (et) 2004-06-15
US6448244B1 (en) 2002-09-10
EE04346B1 (et) 2004-08-16
NO20005713D0 (no) 2000-11-13
JP2002514646A (ja) 2002-05-21
CA2331141C (en) 2008-10-28
HK1033312A1 (en) 2001-08-24
NO20005712L (no) 2000-12-07
NO319851B1 (no) 2005-09-19
SK285763B6 (sk) 2007-07-06
PL194085B1 (pl) 2007-04-30
NO20005713L (no) 2001-01-11
AU751135B2 (en) 2002-08-08
TWI259835B (en) 2006-08-11
KR100575147B1 (ko) 2006-05-03
HRP20000741A2 (en) 2001-06-30
EP1077976A1 (en) 2001-02-28
NO20005712D0 (no) 2000-11-13
MY122147A (en) 2006-03-31
PT1077976E (pt) 2002-12-31
KR100593395B1 (ko) 2006-06-28
HUP0103536A2 (hu) 2002-07-29
HRP20000740A2 (en) 2001-10-31
IL139649A0 (en) 2002-02-10
TW572899B (en) 2004-01-21
HRP20000741B1 (hr) 2009-02-28
EP0957101A1 (en) 1999-11-17
BG104933A (en) 2001-10-31
ES2198915T3 (es) 2004-02-01
DE69907171D1 (de) 2003-05-28
TR200003323T2 (tr) 2001-02-21
US6384030B1 (en) 2002-05-07
PL344047A1 (en) 2001-09-24
KR20010041480A (ko) 2001-05-25
HUP0102031A3 (en) 2002-10-28
EP1077975B1 (en) 2003-04-23
BG104717A (en) 2001-07-31
CZ298702B6 (cs) 2007-12-27

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B09B Patent application refused [chapter 9.2 patent gazette]

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