IL118464A - (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 - Google Patents

(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

Info

Publication number: IL118464A
Authority: IL; Israel
Prior art keywords: triazol; dihydro2; phenyl2; dihalophenyl; piperazinyl
Prior art date: 1995-06-02

Application number

IL11846496A

Other languages

English (en)

Other versions

IL118464A0 (en

Original Assignee

Schering Corp

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.)

1995-06-02

Filing date

1996-05-30

Publication date

2000-08-13

1995-06-02 Priority claimed from US08/459,145 external-priority patent/US5693626A/en

1995-06-02 Priority claimed from US08/459,225 external-priority patent/US5710154A/en

1995-06-02 Priority claimed from US08/458,543 external-priority patent/US5714490A/en

1996-05-30 Application filed by Schering Corp filed Critical Schering Corp

1996-09-12 Publication of IL118464A0 publication Critical patent/IL118464A0/xx

2000-08-13 Publication of IL118464A publication Critical patent/IL118464A/xx

Links

125000003682 3-furyl group Chemical group O1C([H])=C([*])C([H])=C1[H] 0.000 title 1
125000002887 hydroxy group Chemical group [H]O* 0.000 title 1
239000008194 pharmaceutical composition Substances 0.000 title 1

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
- A61P31/10—Antimycotics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic 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

Landscapes

Organic Chemistry (AREA)
Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Pharmacology & Pharmacy (AREA)
Public Health (AREA)
General Chemical & Material Sciences (AREA)
General Health & Medical Sciences (AREA)
Tropical Medicine & Parasitology (AREA)
Communicable Diseases (AREA)
Oncology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Saccharide Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Peptides Or Proteins (AREA)

IL11846496A 1995-06-02 1996-05-30 (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 IL118464A (en)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US08/459,145 US5693626A (en)	1993-12-21	1995-06-02	Tetrahydrofuran antifungals
US08/459,225 US5710154A (en)	1993-12-21	1995-06-02	Tetrahydrofuran antifungals
US08/458,543 US5714490A (en)	1993-12-21	1995-06-02	Tetrahydrofuran antifungals

Publications (2)

Publication Number	Publication Date
IL118464A0 IL118464A0 (en)	1996-09-12
IL118464A true IL118464A (en)	2000-08-13

Family

ID=27412736

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
IL11846496A IL118464A (en)	1995-06-02	1996-05-30	(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

Country Status (18)

Country	Link
EP (1)	EP0773941B1 (fr)
CN (1)	CN1073109C (fr)
AR (1)	AR002751A1 (fr)
AT (1)	ATE240319T1 (fr)
AU (1)	AU5928096A (fr)
CA (1)	CA2197672C (fr)
CZ (1)	CZ59497A3 (fr)
DE (1)	DE69628117T2 (fr)
ES (1)	ES2199291T3 (fr)
HU (1)	HUP9701690A3 (fr)
IL (1)	IL118464A (fr)
MX (1)	MX9701229A (fr)
NO (1)	NO971218D0 (fr)
NZ (1)	NZ309281A (fr)
PL (1)	PL319635A1 (fr)
SK (1)	SK27097A3 (fr)
TW (1)	TW357146B (fr)
WO (1)	WO1996038443A1 (fr)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CN1238353C (zh) *	1997-02-11	2006-01-25	詹森药业有限公司	含氨基酸酯之唑类抗真菌剂
JP2001519346A (ja) *	1997-10-07	2001-10-23	シェーリングコーポレイション	抗真菌性結晶性多形物
WO1999018111A1 (fr) *	1997-10-07	1999-04-15	Schering Corporation	Polymorphe antifongique cristallin d'ester de glycine
US6713481B1 (en) *	1997-10-17	2004-03-30	David R. Andrews	Crystalline antifungal polymorph
US5883097A (en) *	1998-04-16	1999-03-16	Schering Corporation	Soluble azole antifungal salt
EP0957101A1 (fr) *	1998-05-14	1999-11-17	Janssen Pharmaceutica N.V.	Azoles solubles dans l'eau, antifongiques à large spectre
WO2000030655A1 (fr)	1998-11-20	2000-06-02	Bristol-Myers Squibb Company	Promedicaments solubles a l'eau comprenant des composes de type azole
BR0010279A (pt) *	1999-05-04	2002-05-14	Janssen Phamaceutica N V	éteres antifúngicos
US6362172B2 (en)	2000-01-20	2002-03-26	Bristol-Myers Squibb Company	Water soluble prodrugs of azole compounds
US6448401B1 (en)	2000-11-20	2002-09-10	Bristol-Myers Squibb Company	Process for water soluble azole compounds
EP2130540A1 (fr)	2008-06-02	2009-12-09	Sandoz AG	Compositions pharmaceutiques contenant une forme cristalline du posaconazole
EP2141159A1 (fr)	2008-07-03	2010-01-06	Sandoz AG	Formule cristalline de posaconazole
CA2767489A1 (fr)	2009-07-09	2011-01-13	Sandoz Ag	Forme cristalline du posaconazole
CN102234267A (zh) *	2010-04-21	2011-11-09	中国科学院上海药物研究所	新型三氮唑类抗真菌化合物、其药物组合物及其制备方法和用途
CN102892763B (zh) *	2010-05-19	2016-03-09	桑多斯股份公司	泊沙康唑及泊沙康唑中间体的纯化
EP2571847B1 (fr)	2010-05-19	2016-09-21	Sandoz AG	Procédé de préparation de hydrazides chiraux
AU2011254654B2 (en)	2010-05-19	2016-01-07	Sandoz Ag	Process for the preparation of chiral triazolones
US9073904B2 (en)	2010-05-19	2015-07-07	Sandoz Ag	Preparation of posaconazole intermediates
CN103635465A (zh)	2011-06-16	2014-03-12	桑多斯股份公司	制备手性化合物的方法
WO2015011224A1 (fr)	2013-07-25	2015-01-29	Sandoz Ag	Procédé amélioré pour la préparation de la forme cristalline iv du posaconazole
ITMI20132114A1 (it)	2013-12-18	2015-06-19	Djada Pharmaceutical Sa	Una forma cristallina di posaconazolo
CN104370894A (zh) *	2014-10-21	2015-02-25	江苏恒盛药业有限公司	无定型泊沙康唑的制备工艺
CN105622591B (zh) *	2014-11-06	2018-09-21	博瑞生物医药（苏州）股份有限公司	一种新型三唑类抗真菌药物的制备方法
WO2016087880A1 (fr)	2014-12-05	2016-06-09	Pulmocide Limited	Composé antimycotique
ES2790723T3 (es)	2015-05-21	2020-10-29	Pulmocide Ltd	Antifúngico 4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-il)metil)-5-(2,4-difluorofenil)tetrahidrofurano-3-il)metoxi)-3-metilfenil)piperazina-1-il)-N -(2-hidroxiciclohexil)benzamida, o una sal farmacéuticamente aceptable del mismo
CN106432338A (zh) *	2015-08-08	2017-02-22	陕西合成药业股份有限公司	泊沙康唑衍生物、合成和在长效制剂中的用途
CN105606736A (zh) *	2016-01-27	2016-05-25	重庆华邦制药有限公司	分离测定泊沙康唑中间体z1及其有关物质的方法
US10517867B2 (en)	2016-02-04	2019-12-31	Wuhan Ll Science And Technology Development Co., Ltd.	Posaconazole derivative, pharmaceutical composition and use thereof
CN105949278B (zh) *	2016-03-30	2019-12-06	南京曼杰生物科技有限公司	一种取代的四氢呋喃水溶性衍生物及其应用
CN106866459A (zh) *	2017-03-30	2017-06-20	成都绿林科技有限公司	一种抗真菌药物中间体的制备方法
CN106986787A (zh) *	2017-03-30	2017-07-28	成都绿林科技有限公司	一种泊沙康唑中间体的合成方法
CN110938093B (zh) *	2018-09-21	2022-08-19	华创合成制药股份有限公司	一种泊沙康唑磷酸酯单胆碱盐及其制备方法和用途
GB201917867D0 (en)	2019-12-06	2020-01-22	Pulmocide Ltd	Polymorphs
CN113666915B (zh) *	2021-08-27	2022-08-16	江苏海洋大学	一种泊沙康唑中间体的制备方法
CN114315811B (zh) *	2021-11-19	2024-04-30	江苏恒盛药业有限公司	一种三氮唑类似物化合物及其制备方法和应用
CN118164968A (zh) *	2024-01-26	2024-06-11	四川大学	一种三唑类抗真菌药伏立康唑的合成方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
IL103558A0 (en) *	1991-10-30	1993-03-15	Schering Corp	Tri-substituted tetrahydrofuran antifungals
DK0736030T3 (da) *	1993-12-21	2001-10-29	Schering Corp	Fungicide tetrahydrofuraner
SG48386A1 (en) *	1994-01-24	1998-04-17	Janssen Pharmaceutica Nv	Watersoluble azole antifungals

1996
- 1996-05-30 ES ES96916574T patent/ES2199291T3/es not_active Expired - Lifetime
- 1996-05-30 AR ARP960102806A patent/AR002751A1/es not_active Application Discontinuation
- 1996-05-30 HU HU9701690A patent/HUP9701690A3/hu unknown
- 1996-05-30 TW TW085106412A patent/TW357146B/zh active
- 1996-05-30 AT AT96916574T patent/ATE240319T1/de active
- 1996-05-30 EP EP96916574A patent/EP0773941B1/fr not_active Expired - Lifetime
- 1996-05-30 IL IL11846496A patent/IL118464A/xx not_active IP Right Cessation
- 1996-05-30 PL PL96319635A patent/PL319635A1/xx unknown
- 1996-05-30 DE DE69628117T patent/DE69628117T2/de not_active Expired - Lifetime
- 1996-05-30 CZ CZ97594A patent/CZ59497A3/cs unknown
- 1996-05-30 NZ NZ309281A patent/NZ309281A/en unknown
- 1996-05-30 MX MX9701229A patent/MX9701229A/es unknown
- 1996-05-30 CN CN96190848A patent/CN1073109C/zh not_active Expired - Fee Related
- 1996-05-30 SK SK270-97A patent/SK27097A3/sk unknown
- 1996-05-30 WO PCT/US1996/007547 patent/WO1996038443A1/fr not_active Ceased
- 1996-05-30 AU AU59280/96A patent/AU5928096A/en not_active Abandoned
- 1996-05-30 CA CA2197672A patent/CA2197672C/fr not_active Expired - Fee Related
1997
- 1997-03-17 NO NO971218A patent/NO971218D0/no not_active Application Discontinuation

Also Published As

Publication number	Publication date
CA2197672A1 (fr)	1996-12-05
AU5928096A (en)	1996-12-18
CN1073109C (zh)	2001-10-17
CZ59497A3 (en)	1997-08-13
DE69628117D1 (de)	2003-06-18
NO971218L (no)	1997-03-17
ES2199291T3 (es)	2004-02-16
HUP9701690A2 (hu)	1998-03-02
IL118464A0 (en)	1996-09-12
ATE240319T1 (de)	2003-05-15
MX9701229A (es)	1997-05-31
SK27097A3 (en)	1997-09-10
NO971218D0 (no)	1997-03-17
NZ309281A (en)	1998-07-28
HK1008821A1 (en)	1999-05-21
PL319635A1 (en)	1997-08-18
EP0773941A1 (fr)	1997-05-21
TW357146B (en)	1999-05-01
HUP9701690A3 (en)	1998-04-28
AR002751A1 (es)	1998-04-29
CN1161038A (zh)	1997-10-01
EP0773941B1 (fr)	2003-05-14
DE69628117T2 (de)	2004-04-01
WO1996038443A1 (fr)	1996-12-05
CA2197672C (fr)	2011-05-17

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Legal Events

Date	Code	Title
2000-12-06	FF	Patent granted
2001-06-14	KB	Patent renewed
2003-02-12	MM9K	Patent not in force due to non-payment of renewal fees