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ES2182531T3 - Azoles solubles en agua como antifungicos de amplio espectro. - Google Patents

Azoles solubles en agua como antifungicos de amplio espectro.

Info

Publication number
ES2182531T3
ES2182531T3 ES99926304T ES99926304T ES2182531T3 ES 2182531 T3 ES2182531 T3 ES 2182531T3 ES 99926304 T ES99926304 T ES 99926304T ES 99926304 T ES99926304 T ES 99926304T ES 2182531 T3 ES2182531 T3 ES 2182531T3
Authority
ES
Spain
Prior art keywords
4alkyl
mono
amino
aminoc1
aryl
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES99926304T
Other languages
English (en)
Inventor
Lieven Meerpoel
Leo Jacobus Jozef Backx
Der Veken Louis Jozef Elis Van
Frank Christopher Odds
Jan Heeres
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Janssen Pharmaceutica NV
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
Application granted granted Critical
Publication of ES2182531T3 publication Critical patent/ES2182531T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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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

Un compuesto de fórmula una forma de N¿óxido, una sal de adición farmacéuticamente aceptable o una forma estereoquímicamente isómera de la misma, en la cual L representa un radical de fórmula o en las cuales cada Alk representa independientemente C1¿6¿alcanodiílo opcionalmente sustituido con hidroxi o C1¿4alquiloxi; cada n es independientemente 1, 2 ó 3; Y representa O, S o NR2; cada R1 representa independientemente hidrógeno, arilo, Het1, o C1¿6alquilo opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados independientemente de halo, hidroxi, mercapto, C1¿4¿alquiloxi, C1¿4alquiltio, ariloxi, ariltio, arilC1¿4¿alquiloxi, arilC1¿4alquiltio, ciano, amino, mono¿ o di(C1¿4alquil)¿amino, mono¿ o di(aril)amino, mono¿ o di(arilC1¿4alquil)amino, C1¿4alquiloxicarbonilamino, benciloxicarbonilamino, aminocarbonilo, carboxilo, C1¿4alquiloxicarbonilo, guanidinilo, arilo o Het2; cada R2 representa independientemente hidrógeno o C1¿6¿alquilo; o en el caso en que R1 y R2 están unidos al mismo átomo de nitrógeno, pueden considerarse juntos para formar un radical heterocíclico seleccionado de morfolinilo, pirrolidinilo, piperidinilo, homopiperidinilo o piperazinilo; dicho radical heterocíclico puede estar sustituido opcionalmente con C1¿4alquilo, arilo, Het2, arilC1¿4alquilo, Het2C1¿4alquilo, hidroxiC14alquilo, amino, mono¿ o di(C1¿4alquil)amino, aminoC1¿4alquilo, mono¿ o di(C1¿4alquil)aminoC1¿4¿alquilo, carboxilo, aminocarbonilo, C1¿4¿alquil¿oxicarbonilo, C1¿4alquiloxicarbonilamino o mono¿ o di(C1¿4alquil)aminocarbonilo; o los mismos se pueden considerar juntos para formar un radical azido; cada R3 representa independientemente hidrógeno, hidroxi o C1¿4alquiloxi; arilo representa fenilo, naftalenilo, 1,2,3,4¿tetrahidro¿naftalenilo, indenilo o indanilo; cada uno de dichos grupos arilo puede estar sustituido opcionalmente con uno o más sustituyentes seleccionados de halo, C1¿4alquilo, hidroxi, C1¿4alquiloxi, nitro, amino, trifluorometilo, hidroxiC1¿4alquilo, C1¿4alquiloxiC1¿4alquilo, aminoC1¿4alquilo, mono¿ o di(C1¿4alquil)aminoC1¿4alquilo; Het1 representa un radical heterocíclico monocíclico o bicíclico; seleccionándose dicho radical heterocíclico monocíclico del grupo piridinilo, piperidinilo, homopiperidinilo, pirazinilo, pirimidinilo, piridazinilo, triazinilo, triazolilo, piranilo, tetrahidropiranilo, imidazolilo, imidazolinilo, imidazolidinilo, pirazolilo, pirazolinilo, pirazolidinilo, tiazolilo, tiazolidinilo, isotiazolilo, oxazolilo, oxazolidinilo, isoxazolilo, pirrolilo, pirrolinilo, pirrolidinilo, furanilo, tetrahidrofuranilo, tienilo, tiolanilo, dioxolanilo; seleccionándose dicho radical heterocíclico bicíclico del grupo quinolinilo, 1,2,3,4¿tetrahidro¿quinolinilo, isoquinolinilo, quinoxalinilo, quinazolinilo, ftalazinilo, cinnolinilo, cromanilo, tiocromanilo, 2H¿cromenilo, 1,4¿benzodioxanilo, indolilo, isoindolilo, indolinilo, indazolilo, purinilo, pirrolopiridinilo, furanopiridinilo, tienopiridinilo, benzotiazolilo, benzoxazolilo, bencisotiazolilo, bencisoxazolilo, bencimidazolilo, benzofuranilo, benzotienilo; donde cada uno de dichos heterociclos mono¿ o bicíclicos puede estar sustituido opcionalmente con uno o, en caso de ser posible, más sustituyentes seleccionados de halo, C1¿4alquilo, hidroxi, C1¿4alquiloxi, nitro, amino, trifluorometilo, hidroxi¿C1¿4alquilo, C1¿4¿alquiloxi¿C1¿4alquilo, aminoC1¿4alquilo, mono¿ o di(C1¿4¿alquil)amino¿C1¿4alquilo, arilo o arilC1¿4alquilo; Het2 es igual que Het1 y puede ser también un heterociclo monocíclico seleccionado de piperazinilo, homopiperazinilo,1,4¿dioxanilo, morfolinilo, tiomorfolinilo; donde cada uno de dichos heterociclos monocíclicos sustituido opcionalmente con uno o, en caso de ser posible, más sustituyentes seleccionados de halo, C1¿4alquilo, hidroxi, C1¿4alquiloxi, nitro, amino, trifluorometilo, hidroxi¿C1¿4¿alquilo, C1¿4alquiloxi¿C1¿4alquilo, aminoC1¿4alquilo, mono¿ o di(C1¿4¿alquil)amino¿C1¿4alquilo, arilo o arilC1¿4alquilo; R6 representa hidrógeno o C1¿4alquilo; R7 representa hidrógeno o C1¿4alquilo; o R6 y R7, considerados juntos, forman un radical bivalente de fórmula ¿R6¿R7¿, en cuya fórmula ¿R6¿R7¿ es: ¿N=CH¿ (i), ¿CH=N¿ (ii), ¿CH=CH¿ (iii), ¿CH2¿CH2 (iv), en cuyas fórmulas un átomo de hidrógeno en los radicales (i) y (ii) puede estar reemplazado con un radical C1¿4¿alquilo y uno o más átomos de hidrógeno en los radicales (iii) y (iv) puede estar reemplazado por un radical C1¿4¿alquilo; D representa un radical de fórmula en cuyas fórmulas X es N o CH; R4 es hidrógeno o halo; R5 es halo.
ES99926304T 1998-05-14 1999-05-06 Azoles solubles en agua como antifungicos de amplio espectro. Expired - Lifetime ES2182531T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP98201588A EP0957101A1 (en) 1998-05-14 1998-05-14 Water soluble azoles as broad-spectrum antifungals

Publications (1)

Publication Number Publication Date
ES2182531T3 true ES2182531T3 (es) 2003-03-01

Family

ID=8233724

Family Applications (2)

Application Number Title Priority Date Filing Date
ES99926304T Expired - Lifetime ES2182531T3 (es) 1998-05-14 1999-05-06 Azoles solubles en agua como antifungicos de amplio espectro.
ES99924942T Expired - Lifetime ES2198915T3 (es) 1998-05-14 1999-05-06 Azoles solubles en agua como antifungicos de amplio espectro.

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES99924942T Expired - Lifetime ES2198915T3 (es) 1998-05-14 1999-05-06 Azoles solubles en agua como antifungicos de amplio espectro.

Country Status (31)

Country Link
US (2) US6384030B1 (es)
EP (3) EP0957101A1 (es)
JP (2) JP2002514645A (es)
KR (2) KR100575147B1 (es)
CN (2) CN1137118C (es)
AR (2) AR016480A1 (es)
AT (2) ATE238296T1 (es)
AU (2) AU758876B2 (es)
BG (2) BG64388B1 (es)
BR (2) BR9910448A (es)
CA (2) CA2331141C (es)
CO (1) CO5021227A1 (es)
CZ (2) CZ298702B6 (es)
DE (2) DE69902461T2 (es)
DK (1) DK1077976T3 (es)
EE (2) EE04346B1 (es)
ES (2) ES2182531T3 (es)
HR (2) HRP20000740B1 (es)
HU (2) HUP0103536A3 (es)
IL (2) IL139647A0 (es)
MY (2) MY122147A (es)
NO (2) NO319851B1 (es)
NZ (2) NZ507966A (es)
PL (2) PL194086B1 (es)
PT (1) PT1077976E (es)
SI (1) SI1077976T1 (es)
SK (2) SK285763B6 (es)
TR (2) TR200003323T2 (es)
TW (2) TW572899B (es)
WO (2) WO1999058530A1 (es)
ZA (2) ZA200007173B (es)

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
NZ521241A (en) * 2000-03-07 2004-02-27 Ranbaxy Lab Ltd 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
EP2571871B1 (en) * 2010-05-19 2017-06-21 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
DK3003038T3 (da) 2013-06-07 2019-11-11 Scripps Research Inst 2h-1,2,3-triazolderivater som inhibitorer af fibrose
KR102579848B1 (ko) 2014-12-05 2023-09-18 풀모사이드 리미티드 항진균 화합물
AU2015360583B2 (en) * 2014-12-10 2020-01-23 The Scripps Research Institute Small molecule inhibitors of fibrosis
AU2016263669B2 (en) * 2015-05-21 2020-04-30 Pulmocide Limited Antifungal 4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4- difluorophenyl)tetrahydrofuran-3-yl) methoxy)-3-methylphenyl)piperazin-1-yl)-N- (2-hydroxycyclohexyl) benzamide, or a pharmaceutically acceptable salt thereof
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
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
ATE201408T1 (de) * 1992-03-18 2001-06-15 Janssen Pharmaceutica Nv Itraconazol- und saperconazolstereoisomere
SK283035B6 (sk) * 1993-12-21 2003-02-04 Schering Corporation Tetrahydrofuránová zlúčenina, spôsob jej prípravy, jej farmaceuticky prijateľný ester, soľ a farmaceutický prostriedok
EP0741737B1 (en) * 1994-01-24 1999-11-10 Janssen Pharmaceutica N.V. Watersoluble azole antifungals
FI98688C (fi) * 1994-07-20 1997-07-25 Nokia Telecommunications Oy Menetelmä lyhytsanomalähetyksen käynnistämiseksi solukkoradiojärjestelmässä, solukkoradiojärjestelmä sekä solukkoradiojärjestelmän tilaajarekisteri
MX9701229A (es) * 1995-06-02 1997-05-31 Schering Corp Antifungicos de tetrahidrofurano.
JPH11507668A (ja) * 1995-06-19 1999-07-06 シェーリング コーポレイション テトラヒドロフラン抗真菌剤
WO1998034934A1 (en) * 1997-02-11 1998-08-13 Janssen Pharmaceutica N.V. Amino acid ester containing azole antifungals
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
BR9911057A (pt) 2001-02-06
PL194085B1 (pl) 2007-04-30
WO1999058529A1 (en) 1999-11-18
US6384030B1 (en) 2002-05-07
AU4141799A (en) 1999-11-29
EP1077975B1 (en) 2003-04-23
WO1999058530A1 (en) 1999-11-18
HUP0102031A2 (hu) 2002-05-29
NZ507965A (en) 2002-05-31
ATE238296T1 (de) 2003-05-15
EE04346B1 (et) 2004-08-16
HRP20000741A2 (en) 2001-06-30
HK1033312A1 (en) 2001-08-24
NO319760B1 (no) 2005-09-12
PL344047A1 (en) 2001-09-24
MY122147A (en) 2006-03-31
PT1077976E (pt) 2002-12-31
HK1032781A1 (en) 2001-08-03
HUP0102031A3 (en) 2002-10-28
CZ20004108A3 (en) 2001-05-16
TWI259835B (en) 2006-08-11
SI1077976T1 (en) 2003-02-28
CZ299481B6 (cs) 2008-08-13
NZ507966A (en) 2002-10-25
PL194086B1 (pl) 2007-04-30
CN1300287A (zh) 2001-06-20
US6448244B1 (en) 2002-09-10
DE69902461T2 (de) 2003-04-10
JP2002514646A (ja) 2002-05-21
JP2002514645A (ja) 2002-05-21
KR100593395B1 (ko) 2006-06-28
CN1300288A (zh) 2001-06-20
BG64954B1 (bg) 2006-10-31
CA2331141A1 (en) 1999-11-18
EE04311B1 (et) 2004-06-15
CZ298702B6 (cs) 2007-12-27
TR200003323T2 (tr) 2001-02-21
EE200000651A (et) 2002-04-15
NO20005713D0 (no) 2000-11-13
ZA200007173B (en) 2002-03-04
SK286156B6 (sk) 2008-04-07
IL139649A (en) 2004-09-27
HUP0103536A2 (hu) 2002-07-29
NO20005713L (no) 2001-01-11
DE69902461D1 (de) 2002-09-12
DK1077976T3 (da) 2002-12-02
ES2198915T3 (es) 2004-02-01
EP1077976A1 (en) 2001-02-28
MY120248A (en) 2005-09-30
SK16822000A3 (sk) 2001-07-10
BG104933A (en) 2001-10-31
SK285763B6 (sk) 2007-07-06
DE69907171T2 (de) 2004-02-05
IL139649A0 (en) 2002-02-10
DE69907171D1 (de) 2003-05-28
AR016480A1 (es) 2001-07-04
CO5021227A1 (es) 2001-03-27
CN1137118C (zh) 2004-02-04
BR9910448A (pt) 2001-01-02
EP0957101A1 (en) 1999-11-17
HRP20000740B1 (en) 2003-12-31
TR200003322T2 (tr) 2001-02-21
TW572899B (en) 2004-01-21
CZ20004109A3 (en) 2001-05-16
AU751135B2 (en) 2002-08-08
ZA200007459B (en) 2002-09-13
CA2331187A1 (en) 1999-11-18
AU758876B2 (en) 2003-04-03
NO20005712D0 (no) 2000-11-13
AR016482A1 (es) 2001-07-04
PL344037A1 (en) 2001-09-24
BG104717A (en) 2001-07-31
HRP20000741B1 (hr) 2009-02-28
AU4361599A (en) 1999-11-29
SK16812000A3 (sk) 2001-08-06
EP1077975A1 (en) 2001-02-28
EE200000657A (et) 2002-04-15
EP1077976B1 (en) 2002-08-07
HUP0103536A3 (en) 2002-08-28
NO20005712L (no) 2000-12-07
NO319851B1 (no) 2005-09-19
CA2331187C (en) 2008-11-18
CN1135229C (zh) 2004-01-21
KR100575147B1 (ko) 2006-05-03
ATE221884T1 (de) 2002-08-15
HRP20000740A2 (en) 2001-10-31
CA2331141C (en) 2008-10-28
KR20010042852A (ko) 2001-05-25
KR20010041480A (ko) 2001-05-25
BG64388B1 (bg) 2004-12-30
IL139647A0 (en) 2002-02-10

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