BR9910448A - Azóis solúveis em água como antifúngicos de amplo aspectro - Google Patents
Azóis solúveis em água como antifúngicos de amplo aspectroInfo
- 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
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
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.
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 (32)
| Country | Link |
|---|---|
| US (2) | US6448244B1 (pt) |
| EP (3) | EP0957101A1 (pt) |
| JP (2) | JP2002514646A (pt) |
| KR (2) | KR100575147B1 (pt) |
| CN (2) | CN1137118C (pt) |
| AR (2) | AR016480A1 (pt) |
| AT (2) | ATE238296T1 (pt) |
| AU (2) | AU758876B2 (pt) |
| BG (2) | BG64388B1 (pt) |
| BR (2) | BR9911057A (pt) |
| CA (2) | CA2331187C (pt) |
| CO (1) | CO5021227A1 (pt) |
| CZ (2) | CZ298702B6 (pt) |
| DE (2) | DE69907171T2 (pt) |
| DK (1) | DK1077976T3 (pt) |
| EE (2) | EE04346B1 (pt) |
| ES (2) | ES2182531T3 (pt) |
| HK (2) | HK1032781A1 (pt) |
| HR (2) | HRP20000741B1 (pt) |
| HU (2) | HUP0102031A3 (pt) |
| IL (2) | IL139647A0 (pt) |
| MY (2) | MY122147A (pt) |
| NO (2) | NO319760B1 (pt) |
| NZ (2) | NZ507965A (pt) |
| PL (2) | PL194086B1 (pt) |
| PT (1) | PT1077976E (pt) |
| SI (1) | SI1077976T1 (pt) |
| SK (2) | SK286156B6 (pt) |
| TR (2) | TR200003323T2 (pt) |
| TW (2) | TWI259835B (pt) |
| WO (2) | WO1999058530A1 (pt) |
| ZA (2) | ZA200007173B (pt) |
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 |
| CA2402345A1 (en) * | 2000-03-07 | 2001-09-13 | Sudershan K. Arora | 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 |
| WO2011144653A1 (en) * | 2010-05-19 | 2011-11-24 | Sandoz Ag | Process for the preparation of chiral triazolones |
| US11028078B2 (en) * | 2011-09-07 | 2021-06-08 | The Johns Hopkins University | Itraconazole analogs and use thereof |
| WO2013036866A1 (en) * | 2011-09-07 | 2013-03-14 | The Johns Hopkins University | Itraconazole analogs and use thereof |
| PT3003038T (pt) | 2013-06-07 | 2019-11-19 | Scripps Research Inst | Derivados 2h-1,2,3-triazólicos como inibidores de fibrose |
| CA2963625C (en) | 2014-12-05 | 2023-08-22 | Pulmocide Limited | 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-(4-fluorophenyl)benzamide or salts thereof, and use to treat mycoses |
| 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 |
| EA032454B1 (ru) * | 2015-05-21 | 2019-05-31 | Палмосайд Лимитед | Противогрибковый 4-(4-(4-(((3r,5r)-5-((1h-1,2,4-триазол-1-ил)метил)-5-(2,4-дифторфенил)тетрагидрофуран-3-ил)метокси)-3-метилфенил)пиперазин-1-ил)-n-(2-гидроксициклогексил)бензамид или его фармацевтически приемлемая соль |
| 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 |
| WO2019040363A1 (en) * | 2017-08-20 | 2019-02-28 | University Of Connecticut | AZOLE-TYPE COMPOUND ANALOGUES AND METHODS OF USE |
| 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 |
|---|---|---|---|---|
| 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 |
| ES2158859T3 (es) * | 1992-03-18 | 2001-09-16 | Janssen Pharmaceutica Nv | Estereoisomeros itraconazol y saperconazol. |
| CA2179396C (en) * | 1993-12-21 | 2001-04-17 | Anil K. Saksena | Tetrahydrofuran antifungals |
| PT741737E (pt) * | 1994-01-24 | 2000-04-28 | Janssen Pharmaceutica Nv | Antifungicos do tipo azole soluveis em agua |
| FI98688C (fi) * | 1994-07-20 | 1997-07-25 | Nokia Telecommunications Oy | Menetelmä lyhytsanomalähetyksen käynnistämiseksi solukkoradiojärjestelmässä, solukkoradiojärjestelmä sekä solukkoradiojärjestelmän tilaajarekisteri |
| DE69628117T2 (de) * | 1995-06-02 | 2004-04-01 | Schering Corp. | Antifungale tetrahydrofurane |
| 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 |
| ES2224364T3 (es) * | 1997-02-11 | 2005-03-01 | Janssen Pharmaceutica N.V. | Azoles antifungicos que contienen esteres de aminoacidos. |
| 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 DE DE69907171T patent/DE69907171T2/de not_active Expired - Lifetime
- 1999-05-06 PL PL99344037A patent/PL194086B1/pl unknown
- 1999-05-06 CA CA002331187A patent/CA2331187C/en not_active Expired - Fee Related
- 1999-05-06 EP EP99926304A patent/EP1077976B1/en not_active Expired - Lifetime
- 1999-05-06 AT AT99924942T patent/ATE238296T1/de not_active IP Right Cessation
- 1999-05-06 AU AU43615/99A patent/AU758876B2/en not_active Ceased
- 1999-05-06 CN CNB998059560A patent/CN1137118C/zh not_active Expired - Fee Related
- 1999-05-06 CZ CZ20004109A patent/CZ298702B6/cs not_active IP Right Cessation
- 1999-05-06 CN CNB998060690A patent/CN1135229C/zh not_active Expired - Fee Related
- 1999-05-06 EE EEP200000651A patent/EE04346B1/xx not_active IP Right Cessation
- 1999-05-06 SI SI9930131T patent/SI1077976T1/xx unknown
- 1999-05-06 EE EEP200000657A patent/EE04311B1/xx not_active IP Right Cessation
- 1999-05-06 TR TR2000/03323T patent/TR200003323T2/xx unknown
- 1999-05-06 SK SK1681-2000A patent/SK286156B6/sk not_active IP Right Cessation
- 1999-05-06 PL PL99344047A patent/PL194085B1/pl unknown
- 1999-05-06 JP JP2000548334A patent/JP2002514646A/ja active Pending
- 1999-05-06 CA CA002331141A patent/CA2331141C/en not_active Expired - Fee Related
- 1999-05-06 AU AU41417/99A patent/AU751135B2/en not_active Ceased
- 1999-05-06 WO PCT/EP1999/003243 patent/WO1999058530A1/en active IP Right Grant
- 1999-05-06 KR KR1020007011624A patent/KR100575147B1/ko not_active IP Right Cessation
- 1999-05-06 NZ NZ507965A patent/NZ507965A/en not_active IP Right Cessation
- 1999-05-06 BR BR9911057-1A patent/BR9911057A/pt not_active Application Discontinuation
- 1999-05-06 CZ CZ20004108A patent/CZ299481B6/cs not_active IP Right Cessation
- 1999-05-06 BR BR9910448-2A patent/BR9910448A/pt not_active Application Discontinuation
- 1999-05-06 HU HU0102031A patent/HUP0102031A3/hu unknown
- 1999-05-06 IL IL13964799A patent/IL139647A0/xx not_active IP Right Cessation
- 1999-05-06 US US09/700,166 patent/US6448244B1/en not_active Expired - Lifetime
- 1999-05-06 KR KR1020007009640A patent/KR100593395B1/ko active IP Right Grant
- 1999-05-06 US US09/700,251 patent/US6384030B1/en not_active Expired - Lifetime
- 1999-05-06 NZ NZ507966A patent/NZ507966A/xx not_active IP Right Cessation
- 1999-05-06 PT PT99926304T patent/PT1077976E/pt unknown
- 1999-05-06 ES ES99926304T patent/ES2182531T3/es not_active Expired - Lifetime
- 1999-05-06 TR TR2000/03322T patent/TR200003322T2/xx unknown
- 1999-05-06 HU HU0103536A patent/HUP0103536A3/hu unknown
- 1999-05-06 EP EP99924942A patent/EP1077975B1/en not_active Expired - Lifetime
- 1999-05-06 ES ES99924942T patent/ES2198915T3/es not_active Expired - Lifetime
- 1999-05-06 JP JP2000548333A patent/JP2002514645A/ja active Pending
- 1999-05-06 DK DK99926304T patent/DK1077976T3/da active
- 1999-05-06 AT AT99926304T patent/ATE221884T1/de active
- 1999-05-06 DE DE69902461T patent/DE69902461T2/de not_active Expired - Lifetime
- 1999-05-06 IL IL13964999A patent/IL139649A/en not_active IP Right Cessation
- 1999-05-06 SK SK1682-2000A patent/SK285763B6/sk not_active IP Right Cessation
- 1999-05-06 WO PCT/EP1999/003242 patent/WO1999058529A1/en active IP Right Grant
- 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 MYPI99001862A patent/MY122147A/en unknown
- 1999-05-11 MY MYPI99001861A patent/MY120248A/en unknown
- 1999-05-13 CO CO99029778A patent/CO5021227A1/es unknown
- 1999-05-13 AR ARP990102270A patent/AR016480A1/es active IP Right Grant
- 1999-05-13 AR ARP990102276A patent/AR016482A1/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 NO20005713A patent/NO319760B1/no not_active IP Right Cessation
- 2000-11-13 NO NO20005712A patent/NO319851B1/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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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B09B | Patent application refused [chapter 9.2 patent gazette] |
Free format text: INDEFERIMENTO DO PRESENTE PEDIDO, UMA VEZ QUE NAO ATENDE AO REQUISITO DE ATIVIDADE INVENTIVA ( ART. 8O COMBINADO COM ART. 13 DA LPI ); NAO APRESENTA SUFICIENCIA DESCRITIVA ( ART. 24 DA LPI ) AS REIVINDICACOES ESTAO INDEFINIDAS E/OU ESTAO FUNDAMENTADAS NO RELATORIO DESCRITIVO ( ART. 25 DA LPI ) |
|
| B09B | Patent application refused [chapter 9.2 patent gazette] |
Free format text: MANTIDO O INDEFERIMENTO UMA VEZ QUE NAO FOI APRESENTADO RECURSO DENTRO DO PRAZO LEGAL. |