CN1064685C - 四氢呋喃抗真菌剂 - Google Patents

四氢呋喃抗真菌剂 Download PDF

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Publication number
CN1064685C
CN1064685C CN94195025A CN94195025A CN1064685C CN 1064685 C CN1064685 C CN 1064685C CN 94195025 A CN94195025 A CN 94195025A CN 94195025 A CN94195025 A CN 94195025A CN 1064685 C CN1064685 C CN 1064685C
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China
Prior art keywords
compound
formula
ester
ether
pharmaceutically acceptable
Prior art date
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Expired - Lifetime
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CN94195025A
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English (en)
Chinese (zh)
Other versions
CN1142828A (zh
Inventor
A·K·莎森纳
V·M·吉力扎瓦拉汉
R·G·罗韦
R·E·派克
H·Y·王
Y·T·刘
A·K·甘古利
F·本内特
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Merck Sharp and Dohme LLC
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Schering Corp
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Application filed by Schering Corp filed Critical Schering Corp
Publication of CN1142828A publication Critical patent/CN1142828A/zh
Application granted granted Critical
Publication of CN1064685C publication Critical patent/CN1064685C/zh
Anticipated expiration legal-status Critical
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    • 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
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P31/10Antimycotics
    • 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
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Biochemistry (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Dental Preparations (AREA)
  • Lubricants (AREA)
  • Thermal Transfer Or Thermal Recording In General (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
CN94195025A 1993-12-21 1994-12-20 四氢呋喃抗真菌剂 Expired - Lifetime CN1064685C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US17108393A 1993-12-21 1993-12-21
US08/171,083 1993-12-21

Publications (2)

Publication Number Publication Date
CN1142828A CN1142828A (zh) 1997-02-12
CN1064685C true CN1064685C (zh) 2001-04-18

Family

ID=22622452

Family Applications (1)

Application Number Title Priority Date Filing Date
CN94195025A Expired - Lifetime CN1064685C (zh) 1993-12-21 1994-12-20 四氢呋喃抗真菌剂

Country Status (28)

Country Link
EP (1) EP0736030B1 (enExample)
JP (1) JP2834889B2 (enExample)
KR (1) KR0179990B1 (enExample)
CN (1) CN1064685C (enExample)
AT (1) ATE204875T1 (enExample)
AU (1) AU681753B2 (enExample)
BR (1) BR1100154B1 (enExample)
CA (1) CA2179396C (enExample)
CO (1) CO4520281A1 (enExample)
CZ (1) CZ294823B6 (enExample)
DE (2) DE122006000004I2 (enExample)
DK (1) DK0736030T3 (enExample)
ES (1) ES2159623T3 (enExample)
FI (1) FI118470B (enExample)
FR (1) FR06C0009I2 (enExample)
HU (1) HU225062B1 (enExample)
IL (1) IL112081A (enExample)
LU (1) LU91216I2 (enExample)
MY (1) MY130217A (enExample)
NL (1) NL300219I2 (enExample)
NO (2) NO316173B1 (enExample)
NZ (1) NZ278713A (enExample)
PL (1) PL181193B1 (enExample)
PT (1) PT736030E (enExample)
SK (1) SK283035B6 (enExample)
TW (1) TW377349B (enExample)
WO (1) WO1995017407A1 (enExample)
ZA (1) ZA9410142B (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
CN106883221A (zh) * 2017-04-17 2017-06-23 兰州大学 一种无定形泊沙康唑及其制备方法

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WO1995019983A1 (en) * 1994-01-24 1995-07-27 Janssen Pharmaceutica N.V. Watersoluble azole antifungals
MX9701229A (es) * 1995-06-02 1997-05-31 Schering Corp Antifungicos de tetrahidrofurano.
WO1997000255A1 (en) * 1995-06-19 1997-01-03 Schering Corporation Tetrahydrofuran antifungals
US5698557A (en) * 1995-06-19 1997-12-16 Schering Corporation Hydroxy-substituted antifungals
BR9612046A (pt) * 1995-12-20 1999-02-09 Schering Corp Processo para a preparação de hidrazidas
PL188401B1 (pl) 1996-05-24 2005-01-31 Schering Corp Kompozycje przeciwgrzybicze o zwiększonej dostępności biologicznej
US5834472A (en) * 1996-05-24 1998-11-10 Schering Corporation Antifungal composition with enhanced bioavailability
JP2000514057A (ja) * 1996-06-28 2000-10-24 シェーリング コーポレイション 増強されたバイオアベイラビリティを有する抗真菌剤の固溶体
US5972381A (en) * 1996-06-28 1999-10-26 Schering Corporation Solid solution of an antifungal agent with enhanced bioavailability
CA2258683C (en) * 1996-06-28 2007-07-31 Schering Corporation Oral composition comprising a triazole antifungal compound
US5846971A (en) * 1996-06-28 1998-12-08 Schering Corporation Oral antifungal composition
EP0937071A1 (en) * 1996-11-12 1999-08-25 Sepracor, Inc. 2r,4s,s,s- and 2s,4r,s,s-hydroxyitraconazole
EP0938487A2 (en) * 1996-11-12 1999-09-01 Sepracor, Inc. 2$i(R),4$i(S),$i(R),$i(S)- AND 2$i(S),4$i(R),$i(R),$i(S)-HYDROXYITRACONAZOLE- AND HYDROXYSAPERCONAZOLE DERIVATIVES
CA2269616A1 (en) * 1996-11-12 1998-05-22 Gerald J. Tanoury 2r,4s,s,r- and 2s,4r,s,r-hydroxyitraconazole
CN1237173A (zh) * 1996-11-12 1999-12-01 塞普拉科公司 2r,4s,r,r-和2s,4r,r,r-羟基伊曲康唑
US5684197A (en) * 1996-12-12 1997-11-04 Schering Corporation Process for preparation of hydrazides
HU227744B1 (en) 1997-02-11 2012-02-28 Janssen Pharmaceutica Nv Amino acid ester containing azole antifungals, process for their preparation, pharmaceuticals containing the same and intermediates
JP3473949B2 (ja) * 1997-09-25 2003-12-08 シェーリング コーポレイション 対応する抗真菌剤のためのプロドラッグとしてのテトラヒドロフランリン酸エステルおよびヒドロキシエステル
US6043245A (en) * 1997-09-25 2000-03-28 Schering Corporation Tetrahydrofuran antifungal phosphate
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
AU9592998A (en) * 1997-10-07 1999-04-27 Schering Corporation Crystalline antifungal glycine ester polymorph
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 (en) * 1998-05-14 1999-11-17 Janssen Pharmaceutica N.V. Water soluble azoles as broad-spectrum antifungals
US6147077A (en) * 1999-04-29 2000-11-14 Sepracor Inc. 2R,4S-hydroxyitraconazole isomers
PL351749A1 (en) 1999-05-04 2003-06-16 Janssen Pharmaceutica Nv Antifungal ethers
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
BR0208626A (pt) * 2001-04-03 2004-03-09 Schering Corp Composição antifúngica com biodisponibilidade intensificada
US7927613B2 (en) 2002-02-15 2011-04-19 University Of South Florida Pharmaceutical co-crystal compositions
US7790905B2 (en) 2002-02-15 2010-09-07 Mcneil-Ppc, Inc. Pharmaceutical propylene glycol solvate compositions
US7446107B2 (en) 2002-02-15 2008-11-04 Transform Pharmaceuticals, Inc. Crystalline forms of conazoles and methods of making and using the same
IL163666A0 (en) 2002-02-22 2005-12-18 New River Pharmaceuticals Inc Active agent delivery systems and methods for protecting and administering active agents
IL163846A0 (en) 2002-03-01 2005-12-18 Univ South Florida Multiple-component solid phases containing at least one active pharmaceutical ingredient
EP1511490A4 (en) 2002-05-31 2009-03-11 Transform Pharmaceuticals Inc NOVEL CONAZOLE CRYSTALLINE FORMS AND RELATED METHODS, PHARMACEUTICAL COMPOSITIONS AND METHODS
CN100360117C (zh) 2002-06-21 2008-01-09 转化医药公司 具有提高的溶出度的药物组合物
US8183290B2 (en) 2002-12-30 2012-05-22 Mcneil-Ppc, Inc. Pharmaceutically acceptable propylene glycol solvate of naproxen
ITMI20032020A1 (it) * 2003-10-17 2005-04-18 Italfarmaco Spa Nuovi agenti antifungini azolici con diminuita interazione con i citocromi metabolici
CN101039668A (zh) * 2004-08-13 2007-09-19 先灵-普劳有限公司 包含抗菌素、三唑和皮质类固醇的药物制剂
JO2691B1 (en) * 2005-05-03 2013-03-03 ايساي آر آند دي مانجمنت كو.، ليمتد Monolysine salts for azole compounds
EP2130540A1 (en) 2008-06-02 2009-12-09 Sandoz AG Pharmaceutical compositions containing a crystalline form of posaconazole
EP2141159A1 (en) * 2008-07-03 2010-01-06 Sandoz AG A Crystalline form of posaconazole
EP2451805A1 (en) 2009-07-09 2012-05-16 Sandoz AG A crystalline form of posaconazole
WO2011158248A2 (en) * 2010-05-12 2011-12-22 Glenmark Generics Limited Process for preparation of posaconazole and crystalline polymorphic form v of posaconazole
BR112012029225B1 (pt) * 2010-05-19 2020-10-27 Sandoz Ag processo para a preparação de um composto quiral, composto quiral e uso de um composto quiral
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
US9073904B2 (en) 2010-05-19 2015-07-07 Sandoz Ag Preparation of posaconazole intermediates
US9206146B2 (en) 2010-05-19 2015-12-08 Sandoz Ag Purification of posaconazole and of posaconazole intermediates
KR101834024B1 (ko) 2010-06-29 2018-03-02 머크 샤프 앤드 돔 코포레이션 치환된 베타―시클로덱스트린에 의해 안정화된 포사코나졸 정맥내 용액 제제
WO2012172015A1 (en) 2011-06-16 2012-12-20 Sandoz Ag Process for the preparation of a chiral compound
EP2789610A1 (en) 2013-04-10 2014-10-15 Sandoz Ag Purification of Posaconazole Intermediates
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ITMI20132114A1 (it) 2013-12-18 2015-06-19 Djada Pharmaceutical Sa Una forma cristallina di posaconazolo
CN105287403A (zh) * 2014-08-02 2016-02-03 陕西合成药业股份有限公司 一种泊沙康唑前体药物的冻干组合物及其制备方法和用途
CN107001343B (zh) 2014-12-05 2020-12-11 普尔莫赛德有限公司 抗真菌的化合物
WO2016185225A1 (en) 2015-05-21 2016-11-24 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-h yd roxycyc lo h exyl) b e nzam i d e, or a pharmaceutically acceptable salt thereof.
CN106317032A (zh) * 2015-06-15 2017-01-11 重庆圣华曦药业股份有限公司 一种制备高纯度的泊沙康唑的方法
US10457668B2 (en) * 2015-09-23 2019-10-29 Biocon Limited Crystalline forms of posaconazole intermediate and process for the preparation of amorphous posaconazole
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
KR20180115329A (ko) * 2016-03-04 2018-10-22 저장 아우선 파마슈티칼 씨오., 엘티디. 포사코나졸, 조성물, 중간체, 제조방법 및 그의 용도
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
WO2017032908A1 (en) 2016-07-08 2017-03-02 Synthon B.V. Pharmaceutical composition comprising amorphous posaconazole
WO2018115319A2 (en) 2016-12-23 2018-06-28 Helmholtz Zentrum München - Deutsches Forschungszentrum für Gesundheit und Umwelt (GmbH) Inhibitors of cytochrome p450 family 7 subfamily b member 1 (cyp7b1) for use in treating diseases
TR201620462A2 (tr) 2016-12-31 2018-07-23 Abdi Ibrahim Ilac Sanayi Ve Ticaret Anonim Sirketi POSAKONAZOL İÇEREN FARMASÖTİK BİLEŞİMLER ve ÜRETİM YÖNTEMİ
CN106967054A (zh) * 2017-03-30 2017-07-21 成都绿林科技有限公司 一种泊沙康唑的制备方法
CN108341754A (zh) * 2018-03-12 2018-07-31 扬子江药业集团有限公司 泊沙康唑杂质及其制备方法和用途
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
CN112778369B (zh) * 2019-11-05 2024-01-26 华创合成制药股份有限公司 一种三唑类衍生物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
CN120794964A (zh) * 2025-07-03 2025-10-17 广州绿十字制药股份有限公司 泊沙康唑脂肪酸酯、泊沙康唑脂肪酸酯脂肪乳及其制备方法

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
CN106883221A (zh) * 2017-04-17 2017-06-23 兰州大学 一种无定形泊沙康唑及其制备方法

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FR06C0009I1 (enExample) 2006-05-19
EP0736030A1 (en) 1996-10-09
DK0736030T3 (da) 2001-10-29
HK1008820A1 (en) 1999-05-21
CN1142828A (zh) 1997-02-12
AU681753B2 (en) 1997-09-04
EP0736030B1 (en) 2001-08-29
JPH09500658A (ja) 1997-01-21
CZ294823B6 (cs) 2005-03-16
BR1100154B1 (pt) 2013-11-26
CZ180596A3 (en) 1997-01-15
DE122006000004I2 (de) 2007-03-29
NO316173B1 (no) 2003-12-22
WO1995017407A1 (en) 1995-06-29
HU225062B1 (en) 2006-05-29
NZ278713A (en) 1997-12-19
NO2006002I2 (no) 2011-03-07
HU9601709D0 (en) 1996-08-28
TW377349B (en) 1999-12-21
HUT75879A (en) 1997-05-28
NO962616L (no) 1996-08-07
DE69428125D1 (de) 2001-10-04
LU91216I2 (en) 2006-03-27
ATE204875T1 (de) 2001-09-15
FI962577L (fi) 1996-06-20
PL315169A1 (en) 1996-10-14
KR0179990B1 (en) 1999-03-20
MY130217A (en) 2007-06-29
DE122006000004I1 (de) 2006-04-27
SK82696A3 (en) 1997-03-05
AU1512795A (en) 1995-07-10
PL181193B1 (pl) 2001-06-29
CO4520281A1 (es) 1997-10-15
CA2179396C (en) 2001-04-17
IL112081A (en) 2001-08-26
ZA9410142B (en) 1996-05-02
NO962616D0 (no) 1996-06-20
FI962577A0 (fi) 1996-06-20
PT736030E (pt) 2002-01-30
NO2006002I1 (no) 2006-02-20
SK283035B6 (sk) 2003-02-04
CA2179396A1 (en) 1995-06-29
IL112081A0 (en) 1995-03-15
NL300219I1 (nl) 2006-04-03
FR06C0009I2 (enExample) 2006-12-29
JP2834889B2 (ja) 1998-12-14
ES2159623T3 (es) 2001-10-16
NL300219I2 (nl) 2006-05-01
FI118470B (fi) 2007-11-30
DE69428125T2 (de) 2002-05-02

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