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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CN
China
Prior art keywords
compound
formula
ester
ether
pharmaceutically acceptable
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
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
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.)
Merck Sharp and Dohme LLC
Original Assignee
Schering Corp
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22622452&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN1064685(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
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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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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P31/10—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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic 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
    • C07F9/65586—Heterocyclic 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Dermatology (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Thermal Transfer Or Thermal Recording In General (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 (2)
JP (1) JP2834889B2 (2)
KR (1) KR0179990B1 (2)
CN (1) CN1064685C (2)
AT (1) ATE204875T1 (2)
AU (1) AU681753B2 (2)
BR (1) BR1100154B1 (2)
CA (1) CA2179396C (2)
CO (1) CO4520281A1 (2)
CZ (1) CZ294823B6 (2)
DE (2) DE122006000004I2 (2)
DK (1) DK0736030T3 (2)
ES (1) ES2159623T3 (2)
FI (1) FI118470B (2)
FR (1) FR06C0009I2 (2)
HU (1) HU225062B1 (2)
IL (1) IL112081A (2)
LU (1) LU91216I2 (2)
MY (1) MY130217A (2)
NL (1) NL300219I2 (2)
NO (2) NO316173B1 (2)
NZ (1) NZ278713A (2)
PL (1) PL181193B1 (2)
PT (1) PT736030E (2)
SK (1) SK283035B6 (2)
TW (1) TW377349B (2)
WO (1) WO1995017407A1 (2)
ZA (1) ZA9410142B (2)

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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SG48386A1 (en) * 1994-01-24 1998-04-17 Janssen Pharmaceutica Nv Watersoluble azole antifungals
HUP9701690A3 (en) * 1995-06-02 1998-04-28 Schering Corp Kenilwort Tetrahydrofuran derivatives as antifungals and pharmaceutical compositions containing the same
IL118668A0 (en) * 1995-06-19 1996-10-16 Schering Corp Tetrahydrofuran antifungals
US5698557A (en) * 1995-06-19 1997-12-16 Schering Corporation Hydroxy-substituted antifungals
KR20000064469A (ko) * 1995-12-20 2000-11-06 둘락 노먼 씨. 하이드라지드의제조방법
CA2255663C (en) * 1996-05-24 2002-08-20 Schering Corporation Antifungal composition with enhanced bioavailability
US5834472A (en) * 1996-05-24 1998-11-10 Schering Corporation Antifungal composition with enhanced bioavailability
US5972381A (en) * 1996-06-28 1999-10-26 Schering Corporation Solid solution of an antifungal agent with enhanced bioavailability
DE69730241T2 (de) * 1996-06-28 2005-08-11 Schering Corp. Feste lösung eines fungizids mit erhöhter bioverfügbarkeit
US5846971A (en) * 1996-06-28 1998-12-08 Schering Corporation Oral antifungal composition
CA2258683C (en) * 1996-06-28 2007-07-31 Schering Corporation Oral composition comprising a triazole antifungal compound
JP2001504121A (ja) * 1996-11-12 2001-03-27 セプラコール，インク． ２ｒ，４ｓ，ｒ，ｓ―および２ｓ，４ｒ，ｒ，ｓ―ヒドロキシイトラコナゾール―およびヒドロキシサパーコナゾール誘導体
WO1998021204A1 (en) 1996-11-12 1998-05-22 Sepracor, Inc. 2r,4s,s,s- and 2s,4r,s,s-hydroxyitraconazole
CN1237174A (zh) * 1996-11-12 1999-12-01 塞普拉科公司 2r,4s,s,r－和2s,4r,s,r－羟基伊曲康唑
AU5251398A (en) * 1996-11-12 1998-06-03 Sepracor, Inc. (2r,4s,r,r-) and (2s,4r,r,r-)hydroxyitraconazole
US5684197A (en) * 1996-12-12 1997-11-04 Schering Corporation Process for preparation of hydrazides
WO1998034934A1 (en) * 1997-02-11 1998-08-13 Janssen Pharmaceutica N.V. Amino acid ester containing azole antifungals
US6043245A (en) * 1997-09-25 2000-03-28 Schering Corporation Tetrahydrofuran antifungal phosphate
PE120799A1 (es) * 1997-09-25 1999-12-01 Schering Corp Fosfato de tetrahidrofurano antifungal
WO1999018111A1 (en) * 1997-10-07 1999-04-15 Schering Corporation Crystalline antifungal glycine ester polymorph
KR100626109B1 (ko) * 1997-10-07 2006-09-20 쉐링 코포레이션 항진균성 결정성 다형체 및 이를 포함하는 약제학적 조성물
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
AU768491B2 (en) 1999-05-04 2003-12-11 Janssen Pharmaceutica N.V. 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
EP1372394A1 (en) 2001-04-03 2004-01-02 Schering Corporation Antifungal composition with enhanced bioavailability
US7446107B2 (en) 2002-02-15 2008-11-04 Transform Pharmaceuticals, Inc. Crystalline forms of conazoles and methods of making and using the same
US7790905B2 (en) 2002-02-15 2010-09-07 Mcneil-Ppc, Inc. Pharmaceutical propylene glycol solvate compositions
WO2004000284A1 (en) 2002-06-21 2003-12-31 Transform Pharmaceuticals, Inc. Pharmaceutical compositions with improved dissolution
US7927613B2 (en) 2002-02-15 2011-04-19 University Of South Florida Pharmaceutical co-crystal compositions
EP2316468A1 (en) 2002-02-22 2011-05-04 Shire LLC Delivery system and methods for protecting and administering dextroamphetamine
CA2477923C (en) 2002-03-01 2021-02-23 University Of 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
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
KR101289115B1 (ko) * 2004-08-13 2013-07-23 엠에스디 인터내셔널 홀딩즈 게엠베하 항생제인 트리아졸 및 코르티코스테로이드를 포함하는약제학적 제형
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
WO2011003992A1 (en) 2009-07-09 2011-01-13 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
JP5955837B2 (ja) 2010-05-19 2016-07-20 サンド・アクチエンゲゼルシヤフト ポサコナゾール及びポサコナゾール中間体の精製
EP2571847B1 (en) * 2010-05-19 2016-09-21 Sandoz AG Process for the preparation of chiral hydrazides
AU2011254657B2 (en) * 2010-05-19 2016-02-04 Sandoz Ag Preparation of posaconazole intermediates
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
HUE056581T2 (hu) 2010-06-29 2022-02-28 Merck Sharp & Dohme Szubsztituált béta-ciklodextrinnel stabilizált pozakonazol intravénás oldat formulációk
CA2838051C (en) 2011-06-16 2019-09-24 Sandoz Ag Process for the preparation of a chiral compound
EP2789610A1 (en) 2013-04-10 2014-10-15 Sandoz Ag Purification of Posaconazole Intermediates
CA2919290A1 (en) * 2013-07-25 2015-01-29 Sandoz Ag Improved process for the preparation of crystalline form iv of posaconazole
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
EP3227277B1 (en) 2014-12-05 2020-02-05 Pulmocide Limited Antimycotic compound
KR102653821B1 (ko) * 2015-05-21 2024-04-02 풀모사이드 리미티드 항진균성 4-(4-(4-(((3r,5r)-5-((1h-1,2,4-트리아졸-1-일)메틸)-5-(2,4-디플루오로페닐)테트라하이드로푸란-3-일)메톡시)-3-메틸페닐)피페라진-1-일)-n-(2-하이드록시사이클로헥실)벤즈아미드 또는 이의 약학적으로 허용가능한 염.
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
AU2016325733B2 (en) * 2015-09-23 2020-04-09 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
US11185548B2 (en) 2016-12-23 2021-11-30 Helmholtz Zentrum Munchen—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

Also Published As

Publication number Publication date
PL181193B1 (pl) 2001-06-29
HUT75879A (en) 1997-05-28
CA2179396A1 (en) 1995-06-29
DE122006000004I1 (de) 2006-04-27
PT736030E (pt) 2002-01-30
JP2834889B2 (ja) 1998-12-14
NO2006002I1 (no) 2006-02-20
FR06C0009I1 (2) 2006-05-19
CZ294823B6 (cs) 2005-03-16
IL112081A0 (en) 1995-03-15
FI962577L (fi) 1996-06-20
LU91216I2 (en) 2006-03-27
HU9601709D0 (en) 1996-08-28
HU225062B1 (en) 2006-05-29
AU1512795A (en) 1995-07-10
WO1995017407A1 (en) 1995-06-29
PL315169A1 (en) 1996-10-14
NZ278713A (en) 1997-12-19
NO962616L (no) 1996-08-07
AU681753B2 (en) 1997-09-04
NL300219I1 (nl) 2006-04-03
SK283035B6 (sk) 2003-02-04
DE69428125T2 (de) 2002-05-02
NO2006002I2 (no) 2011-03-07
BR1100154B1 (pt) 2013-11-26
TW377349B (en) 1999-12-21
DK0736030T3 (da) 2001-10-29
ES2159623T3 (es) 2001-10-16
CA2179396C (en) 2001-04-17
DE122006000004I2 (de) 2007-03-29
CZ180596A3 (en) 1997-01-15
KR0179990B1 (en) 1999-03-20
EP0736030B1 (en) 2001-08-29
EP0736030A1 (en) 1996-10-09
ATE204875T1 (de) 2001-09-15
DE69428125D1 (de) 2001-10-04
HK1008820A1 (en) 1999-05-21
SK82696A3 (en) 1997-03-05
CO4520281A1 (es) 1997-10-15
MY130217A (en) 2007-06-29
NL300219I2 (nl) 2006-05-01
ZA9410142B (en) 1996-05-02
CN1142828A (zh) 1997-02-12
FR06C0009I2 (2) 2006-12-29
FI962577A0 (fi) 1996-06-20
NO316173B1 (no) 2003-12-22
NO962616D0 (no) 1996-06-20
IL112081A (en) 2001-08-26
JPH09500658A (ja) 1997-01-21
FI118470B (fi) 2007-11-30

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