AR016480A1 - Azoles hidrosolubles como antifungicos de amplio espectro, un proceso para su preparacion, un intermediario y una composicion farmaceutica que los comprende y el uso d elos mismos en la elaboracion de un medicamento - Google Patents
Azoles hidrosolubles como antifungicos de amplio espectro, un proceso para su preparacion, un intermediario y una composicion farmaceutica que los comprende y el uso d elos mismos en la elaboracion de un medicamentoInfo
- Publication number
- AR016480A1 AR016480A1 ARP990102270A ARP990102270A AR016480A1 AR 016480 A1 AR016480 A1 AR 016480A1 AR P990102270 A ARP990102270 A AR P990102270A AR P990102270 A ARP990102270 A AR P990102270A AR 016480 A1 AR016480 A1 AR 016480A1
- Authority
- AR
- Argentina
- Prior art keywords
- mono
- alkyl
- amino
- aryl
- alkyloxy
- Prior art date
Links
Classifications
-
- 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
-
- 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
-
- 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
- A61P31/10—Antimycotics
-
- 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
-
- 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
- C07D249/10—1,2,4-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
- C07D249/12—Oxygen 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
Azoles hidrosolubles de la formula (I), una forma de N-oxido, una sales de adicion farmacéuticamente aceptable o una forma estereoquímicamente isoméricaposible del mismo, donde L representa un radical seleccionado de las formulas (a)a la (f), en elc ual Alk representa independientemente un alcanodiilo C1-6optativamente sustituido con hidroxi o alquiloxi C1-4;n es 1,2 o 3; Y es O, S o NR2; R1 representa H, arilo, Het1 o un alquilo C1-6 optativamente sustituidocon 1, 2 o 3 sustituyentes, cadauno de los cuales es independientemente seleccionado entre halo, hidroxi, mercapto, alquiloxi C1-4, alquiltio C1-4, ariloxi,ariltio, arilalquiloxi C1-4, arilalquiltio C1-4, ciano, amino, mono- o di(alquilo C1-4) amino, mono- o diarilamino, mono- odi(ari lalquil)C1-4, amino,alquloxicarbonilamino C1-4, benciloxicarbonilamino, aminocarbonilo, carboxilo, alquiloxicarbonilo C1-4, guanidilo, arilo, o Het2; cada R2 representaindependientemente H, o alquilo C1-6, o en caso de estar unidos R1 y R2 almismo á tomo de nitrogeno, pueden tomarse juntos para formar un radical heterocíclicoseleccionado entre morfolinilo, pirrolidinilo, piperidinilo, homopeperidinilo o piperazinilo; dicho radical heterocíclico puede estar optativamentesustituido conalquilo C1- 4, arilo, Het2, arilalquilo C1-4, Het2alquilo C1-4, hidroxialquilo C1-4, amino, mono- o dialquil C1-4 amino, aminoalquilo C1-4,mono- o dialquil C1-4aminoalquilo, carboxilo, aminocarbonilo, alquiloxicarbonilo C1-4, alquiloxicarbonilaminoC1-4, o mono- o dialquil C1-4 aminocarbonilo, opueden tomarse juntos, para formar un radical azido; cada R3 representa independientemente H, hidroxi o alquiloxi C1-4; arilo representa fenilo,naftalenilo, 1,2,3,4-tetrahidronaftalenilo, indenilo oindanilo; cada un o de dichos grupos arilo pueden estar optativamente sustituidos con uno o mássustituyentes seleccionados entre halo, alquilo C1-4, hidroxi, alquiloxi C1-4, nitro, amino, trifluorometilo, hidroxialquilo C1-4, alquil C1-4oxialquiloC1-4, aminoalquilo C 1-4, mono- o dialquil C1-4 aminoalquilo C1-4; Het1 representa un radical heterocíclico sustituido monocíclico o bicíclico; el radical
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 |
|---|---|
| AR016480A1 true AR016480A1 (es) | 2001-07-04 |
Family
ID=8233724
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP990102276A AR016482A1 (es) | 1998-05-14 | 1999-05-13 | AZOLES HIDROSOLUBLES COMO ANTIFUNGICOS DE AMPLIO ESPECTRO, UN PROCESO PARA SU PREPARACIoN, UNA COMPOSICIoN FARMACEUTICA QUE LOS COMPRENDE Y EL USO DE LOS MISMOS PARA LA ELABORACIoN DE UN MEDICAMENTO. |
| ARP990102270A AR016480A1 (es) | 1998-05-14 | 1999-05-13 | Azoles hidrosolubles como antifungicos de amplio espectro, un proceso para su preparacion, un intermediario y una composicion farmaceutica que los comprende y el uso d elos mismos en la elaboracion de un medicamento |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP990102276A AR016482A1 (es) | 1998-05-14 | 1999-05-13 | AZOLES HIDROSOLUBLES COMO ANTIFUNGICOS DE AMPLIO ESPECTRO, UN PROCESO PARA SU PREPARACIoN, UNA COMPOSICIoN FARMACEUTICA QUE LOS COMPRENDE Y EL USO DE LOS MISMOS PARA LA ELABORACIoN DE UN MEDICAMENTO. |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US6384030B1 (es) |
| EP (3) | EP0957101A1 (es) |
| JP (2) | JP2002514646A (es) |
| KR (2) | KR100575147B1 (es) |
| CN (2) | CN1135229C (es) |
| AR (2) | AR016482A1 (es) |
| AT (2) | ATE238296T1 (es) |
| AU (2) | AU751135B2 (es) |
| BG (2) | BG64388B1 (es) |
| BR (2) | BR9911057A (es) |
| CA (2) | CA2331141C (es) |
| CO (1) | CO5021227A1 (es) |
| CZ (2) | CZ299481B6 (es) |
| DE (2) | DE69907171T2 (es) |
| DK (1) | DK1077976T3 (es) |
| EE (2) | EE04346B1 (es) |
| ES (2) | ES2198915T3 (es) |
| HK (2) | HK1032781A1 (es) |
| HR (2) | HRP20000741B1 (es) |
| HU (2) | HUP0102031A3 (es) |
| IL (2) | IL139647A0 (es) |
| MY (2) | MY120248A (es) |
| NO (2) | NO319851B1 (es) |
| NZ (2) | NZ507965A (es) |
| PL (2) | PL194086B1 (es) |
| PT (1) | PT1077976E (es) |
| SI (1) | SI1077976T1 (es) |
| SK (2) | SK286156B6 (es) |
| TR (2) | TR200003323T2 (es) |
| TW (2) | TWI259835B (es) |
| WO (2) | WO1999058530A1 (es) |
| ZA (2) | ZA200007173B (es) |
Families Citing this family (15)
| 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 |
| CN102906087B (zh) * | 2010-05-19 | 2016-03-23 | 桑多斯股份公司 | 制备手性三唑酮的方法 |
| 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 |
| KR102240329B1 (ko) | 2013-06-07 | 2021-04-14 | 더 스크립스 리서치 인스티튜트 | 섬유증의 소분자 억제제 |
| KR102579848B1 (ko) | 2014-12-05 | 2023-09-18 | 풀모사이드 리미티드 | 항진균 화합물 |
| WO2016094570A1 (en) * | 2014-12-10 | 2016-06-16 | The California Institute For Biomedical Research | Small molecule inhibitors of fibrosis |
| CA2981945C (en) * | 2015-05-21 | 2023-08-29 | Pulmocide Limited | Antifungal 4-(4-(4-(((3r,5r)-5-((1 h-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 |
| US11390613B2 (en) | 2017-08-20 | 2022-07-19 | University Of Connecticut | Azole analogues and methods of use thereof |
| 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)
| 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 |
| ES2158859T3 (es) * | 1992-03-18 | 2001-09-16 | Janssen Pharmaceutica Nv | Estereoisomeros itraconazol y saperconazol. |
| CO4520281A1 (es) * | 1993-12-21 | 1997-10-15 | Schering Corp | Antifungicos de tetrahidrofurano |
| HU227281B1 (en) * | 1994-01-24 | 2011-01-28 | Janssen Pharmaceutica Nv | Watersoluble azole antifungals, process for their preparation intermediates, and pharmaceutical compositions containing the compounds |
| 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. |
| BR9809744A (pt) * | 1997-02-11 | 2000-06-20 | Janssen Pharmaceutica Nv | Antifúngicos de azol contendo éster de aminoácido |
| EP0957101A1 (en) * | 1998-05-14 | 1999-11-17 | Janssen Pharmaceutica N.V. | Water soluble azoles as broad-spectrum antifungals |
-
1998
- 1998-05-14 EP EP98201588A patent/EP0957101A1/en not_active Withdrawn
-
1999
- 1999-05-06 KR KR1020007011624A patent/KR100575147B1/ko not_active IP Right Cessation
- 1999-05-06 DE DE69907171T patent/DE69907171T2/de not_active Expired - Lifetime
- 1999-05-06 ES ES99924942T patent/ES2198915T3/es not_active Expired - Lifetime
- 1999-05-06 CN CNB998060690A patent/CN1135229C/zh not_active Expired - Fee Related
- 1999-05-06 JP JP2000548334A patent/JP2002514646A/ja active Pending
- 1999-05-06 WO PCT/EP1999/003243 patent/WO1999058530A1/en active IP Right Grant
- 1999-05-06 CA CA002331141A patent/CA2331141C/en not_active Expired - Fee Related
- 1999-05-06 CZ CZ20004108A patent/CZ299481B6/cs not_active IP Right Cessation
- 1999-05-06 CN CNB998059560A patent/CN1137118C/zh not_active Expired - Fee Related
- 1999-05-06 SI SI9930131T patent/SI1077976T1/xx unknown
- 1999-05-06 AU AU41417/99A patent/AU751135B2/en not_active Ceased
- 1999-05-06 DE DE69902461T patent/DE69902461T2/de not_active Expired - Lifetime
- 1999-05-06 BR BR9911057-1A patent/BR9911057A/pt not_active Application Discontinuation
- 1999-05-06 IL IL13964799A patent/IL139647A0/xx not_active IP Right Cessation
- 1999-05-06 US US09/700,251 patent/US6384030B1/en not_active Expired - Lifetime
- 1999-05-06 NZ NZ507965A patent/NZ507965A/en not_active IP Right Cessation
- 1999-05-06 SK SK1681-2000A patent/SK286156B6/sk not_active IP Right Cessation
- 1999-05-06 BR BR9910448-2A patent/BR9910448A/pt not_active Application Discontinuation
- 1999-05-06 EP EP99924942A patent/EP1077975B1/en not_active Expired - Lifetime
- 1999-05-06 CA CA002331187A patent/CA2331187C/en not_active Expired - Fee Related
- 1999-05-06 EE EEP200000651A patent/EE04346B1/xx not_active IP Right Cessation
- 1999-05-06 KR KR1020007009640A patent/KR100593395B1/ko active IP Right Grant
- 1999-05-06 NZ NZ507966A patent/NZ507966A/xx not_active IP Right Cessation
- 1999-05-06 AU AU43615/99A patent/AU758876B2/en not_active Ceased
- 1999-05-06 EP EP99926304A patent/EP1077976B1/en not_active Expired - Lifetime
- 1999-05-06 DK DK99926304T patent/DK1077976T3/da active
- 1999-05-06 AT AT99924942T patent/ATE238296T1/de not_active IP Right Cessation
- 1999-05-06 TR TR2000/03323T patent/TR200003323T2/xx unknown
- 1999-05-06 JP JP2000548333A patent/JP2002514645A/ja active Pending
- 1999-05-06 US US09/700,166 patent/US6448244B1/en not_active Expired - Lifetime
- 1999-05-06 HU HU0102031A patent/HUP0102031A3/hu unknown
- 1999-05-06 PL PL99344037A patent/PL194086B1/pl unknown
- 1999-05-06 IL IL13964999A patent/IL139649A/en not_active IP Right Cessation
- 1999-05-06 EE EEP200000657A patent/EE04311B1/xx not_active IP Right Cessation
- 1999-05-06 ES ES99926304T patent/ES2182531T3/es not_active Expired - Lifetime
- 1999-05-06 WO PCT/EP1999/003242 patent/WO1999058529A1/en active IP Right Grant
- 1999-05-06 PT PT99926304T patent/PT1077976E/pt unknown
- 1999-05-06 CZ CZ20004109A patent/CZ298702B6/cs not_active IP Right Cessation
- 1999-05-06 PL PL99344047A patent/PL194085B1/pl unknown
- 1999-05-06 HU HU0103536A patent/HUP0103536A3/hu unknown
- 1999-05-06 TR TR2000/03322T patent/TR200003322T2/xx unknown
- 1999-05-06 SK SK1682-2000A patent/SK285763B6/sk not_active IP Right Cessation
- 1999-05-06 AT AT99926304T patent/ATE221884T1/de active
- 1999-05-10 TW TW088107505A patent/TWI259835B/zh not_active IP Right Cessation
- 1999-05-10 TW TW088107504A patent/TW572899B/zh not_active IP Right Cessation
- 1999-05-11 MY MYPI99001861A patent/MY120248A/en unknown
- 1999-05-11 MY MYPI99001862A patent/MY122147A/en unknown
- 1999-05-13 AR ARP990102276A patent/AR016482A1/es active IP Right Grant
- 1999-05-13 CO CO99029778A patent/CO5021227A1/es unknown
- 1999-05-13 AR ARP990102270A patent/AR016480A1/es active IP Right Grant
-
2000
- 2000-08-28 BG BG104717A patent/BG64388B1/bg unknown
- 2000-11-02 HR HR20000741A patent/HRP20000741B1/xx not_active IP Right Cessation
- 2000-11-02 HR HR20000740A patent/HRP20000740B1/xx not_active IP Right Cessation
- 2000-11-09 BG BG104933A patent/BG64954B1/bg unknown
- 2000-11-13 NO NO20005712A patent/NO319851B1/no not_active IP Right Cessation
- 2000-11-13 NO NO20005713A patent/NO319760B1/no not_active IP Right Cessation
- 2000-12-04 ZA ZA200007173A patent/ZA200007173B/en unknown
- 2000-12-13 ZA ZA200007459A patent/ZA200007459B/xx unknown
-
2001
- 2001-05-19 HK HK01103466A patent/HK1032781A1/xx not_active IP Right Cessation
- 2001-05-19 HK HK01103465A patent/HK1033312A1/xx not_active IP Right Cessation
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