HUP0301917A2 - Javított eljárás vízoldható azolvegyületek elżállítására - Google Patents
Javított eljárás vízoldható azolvegyületek elżállításáraInfo
- Publication number
- HUP0301917A2 HUP0301917A2 HU0301917A HUP0301917A HUP0301917A2 HU P0301917 A2 HUP0301917 A2 HU P0301917A2 HU 0301917 A HU0301917 A HU 0301917A HU P0301917 A HUP0301917 A HU P0301917A HU P0301917 A2 HUP0301917 A2 HU P0301917A2
- Authority
- HU
- Hungary
- Prior art keywords
- general formula
- compound
- hydroxy
- water soluble
- defined above
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 150000003851 azoles Chemical class 0.000 title 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 238000007796 conventional method Methods 0.000 abstract 2
- 230000000855 fungicidal effect Effects 0.000 abstract 2
- 125000006239 protecting group Chemical group 0.000 abstract 2
- 150000003852 triazoles Chemical class 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-M iodide Chemical compound [I-] XMBWDFGMSWQBCA-UHFFFAOYSA-M 0.000 abstract 1
- 229940006461 iodide ion Drugs 0.000 abstract 1
- 239000003960 organic solvent Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/08—Esters of oxyacids of phosphorus
- C07F9/09—Esters of phosphoric acids
-
- 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
- C07F9/65583—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 each of the hetero rings containing nitrogen as ring hetero atom
-
- 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
- C07F9/6515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having three nitrogen atoms as the only ring hetero atoms
- C07F9/6518—Five-membered rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Preventing Corrosion Or Incrustation Of Metals (AREA)
- Plural Heterocyclic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
A találmány tárgya javított eljárás az általános képletű - ahol A egyszekunder vagy tercier hidroxicsoportot tartalmazó triazol fungicidvegyület nem hidroxi része, R és R1 egymástól függetlenül hidrogénatomvagy 1-6 szénatomos alkilcsoport - triazol fungicid vegyületekvízoldható prodrugjainak előállítására, melynek során az egy A-OHképletű vegyületet - egy általános képletű vegyülettel - amelyben R ésR1 jelentése a fentiekben meghatározott, és Pr jelentése jodid-ionforrással rendelkező hidroxi-védőcsoport - reagáltatnak egy inertszerves oldószerben és egy bázis jelenlétében körülbelül 25°C-tól50°C-ig terjedő hőmérsékleten egy általános képletű - amelyben Pr, A,R és R1 jelentése a fentiekben meghatározott - intermedierré, és (b) aPr védőcsoportot a (IV) intermedierből hagyományos módszerekkeleltávolítva egy (I) általános képletű vegyületet kapnak, amelyetkívánt esetben hagyományos módszerekkel, egy gyógyszerészetilegelfogadható sóvá alakítanak. Ó
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US25200100P | 2000-11-20 | 2000-11-20 | |
PCT/US2001/032382 WO2002042283A1 (en) | 2000-11-20 | 2001-10-18 | Improved process for water soluble azole compounds |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP0301917A2 true HUP0301917A2 (hu) | 2003-09-29 |
HUP0301917A3 HUP0301917A3 (en) | 2005-11-28 |
Family
ID=22954236
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0301917A HUP0301917A3 (en) | 2000-11-20 | 2001-10-18 | Proved process for water soluble azole compounds |
Country Status (18)
Country | Link |
---|---|
US (1) | US6448401B1 (hu) |
EP (1) | EP1345915B1 (hu) |
JP (1) | JP4579496B2 (hu) |
KR (1) | KR100734456B1 (hu) |
CN (1) | CN1279033C (hu) |
AT (1) | ATE353079T1 (hu) |
AU (2) | AU1331702A (hu) |
BR (1) | BR0115448A (hu) |
CA (1) | CA2429378C (hu) |
CZ (1) | CZ20031388A3 (hu) |
DE (1) | DE60126425T2 (hu) |
ES (1) | ES2280405T3 (hu) |
HU (1) | HUP0301917A3 (hu) |
IL (2) | IL155612A0 (hu) |
MX (1) | MXPA03004332A (hu) |
NO (1) | NO20032241D0 (hu) |
PL (1) | PL361003A1 (hu) |
WO (1) | WO2002042283A1 (hu) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6362172B2 (en) * | 2000-01-20 | 2002-03-26 | Bristol-Myers Squibb Company | Water soluble prodrugs of azole compounds |
TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
KR20120062863A (ko) | 2003-07-30 | 2012-06-14 | 리겔 파마슈티칼스, 인크. | 자가면역 질환의 치료 또는 예방에 사용하기 위한 2,4-피리미딘디아민 화합물 |
US20060047135A1 (en) * | 2004-08-30 | 2006-03-02 | Chadwick Scott T | Process for preparing chloromethyl di-tert-butylphosphate |
EP2161275A1 (en) | 2005-01-19 | 2010-03-10 | Rigel Pharmaceuticals, Inc. | Prodrugs of 2,4-pyrimidinediamine compounds and their uses |
JO2691B1 (en) * | 2005-05-03 | 2013-03-03 | ايساي آر آند دي مانجمنت كو.، ليمتد | Monolysine salts for azole compounds |
WO2007032263A1 (ja) * | 2005-09-13 | 2007-03-22 | Eisai R & D Management Co., Ltd. | 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物およびその製造方法 |
CA2632842C (en) * | 2005-12-20 | 2013-06-25 | Eisai R & D Management Co., Ltd. | Process for preparation of water-soluble azole prodrugs |
CN101389333A (zh) | 2006-02-22 | 2009-03-18 | 卫材R&D管理有限公司 | 稳定化药物组合物 |
WO2008108384A1 (ja) | 2007-03-06 | 2008-09-12 | Eisai R & D Management Co., Ltd. | 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物及びその製造方法 |
FI20070574A0 (fi) * | 2007-07-30 | 2007-07-30 | Kuopion Yliopisto | Vesiliukoinen propofolin etylideenifosfaatti-aihiolääke |
BR112013033239A2 (pt) | 2011-06-22 | 2016-09-06 | Vyome Biosciences | pró-farmácos de conjugado baseado em atifungicos e antibacterianos |
CA3039485A1 (en) * | 2016-10-14 | 2018-04-19 | Pulmatrix Operating Company, Inc. | Antifungal dry powders |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2111527C (en) | 1992-12-24 | 2000-07-18 | Jerzy Golik | Phosphonooxymethyl ethers of taxane derivatives |
CA2129288C (en) | 1993-08-17 | 2000-05-16 | Jerzy Golik | Phosphonooxymethyl esters of taxane derivatives |
CZ294823B6 (cs) | 1993-12-21 | 2005-03-16 | Schering Corporation | Fungicidní tetrahydrofurany |
SI0741737T1 (en) * | 1994-01-24 | 2000-02-29 | Janssen Pharmaceutica N.V. | Watersoluble azole antifungals |
NZ270418A (en) * | 1994-02-07 | 1997-09-22 | Eisai Co Ltd | Polycyclic triazole & imidazole derivatives, antifungal compositions |
AR002751A1 (es) | 1995-06-02 | 1998-04-29 | Schering Corp | Antifungicos de tetrahidrofurano, composiciones farmaceuticas que los contienen y el uso de los compuestos para preparar composiciones farmaceuticas utiles para el tratamiento de infecciones fungicas |
GB9602080D0 (en) * | 1996-02-02 | 1996-04-03 | Pfizer Ltd | Pharmaceutical compounds |
EP0829478A3 (en) | 1996-09-09 | 1998-03-25 | F. Hoffmann-La Roche Ag | N-Benzylimidazolium and N-benzyltriazolium derivatives, their preparation and their use as antifungal and antimycotic agents |
ATE252590T1 (de) | 1998-01-29 | 2003-11-15 | Bristol Myers Squibb Co | Phosphorylierte derivate des diaryl 1,3,4 oxadiazolon |
US5883097A (en) | 1998-04-16 | 1999-03-16 | Schering Corporation | Soluble azole antifungal salt |
US6265584B1 (en) | 1998-05-22 | 2001-07-24 | Bristol-Myers Squibb Company | Water soluble prodrugs of azole compounds |
US6204257B1 (en) * | 1998-08-07 | 2001-03-20 | Universtiy Of Kansas | Water soluble prodrugs of hindered alcohols |
WO2000030655A1 (en) * | 1998-11-20 | 2000-06-02 | Bristol-Myers Squibb Company | Water soluble prodrugs of azole compounds |
US6362172B2 (en) * | 2000-01-20 | 2002-03-26 | Bristol-Myers Squibb Company | Water soluble prodrugs of azole compounds |
-
2001
- 2001-10-16 US US09/982,199 patent/US6448401B1/en not_active Expired - Lifetime
- 2001-10-18 PL PL01361003A patent/PL361003A1/xx not_active Application Discontinuation
- 2001-10-18 WO PCT/US2001/032382 patent/WO2002042283A1/en active IP Right Grant
- 2001-10-18 AU AU1331702A patent/AU1331702A/xx active Pending
- 2001-10-18 MX MXPA03004332A patent/MXPA03004332A/es unknown
- 2001-10-18 JP JP2002544418A patent/JP4579496B2/ja not_active Expired - Lifetime
- 2001-10-18 BR BR0115448-6A patent/BR0115448A/pt not_active IP Right Cessation
- 2001-10-18 HU HU0301917A patent/HUP0301917A3/hu unknown
- 2001-10-18 KR KR1020037006747A patent/KR100734456B1/ko active IP Right Grant
- 2001-10-18 EP EP01981688A patent/EP1345915B1/en not_active Expired - Lifetime
- 2001-10-18 AT AT01981688T patent/ATE353079T1/de not_active IP Right Cessation
- 2001-10-18 IL IL15561201A patent/IL155612A0/xx unknown
- 2001-10-18 CA CA002429378A patent/CA2429378C/en not_active Expired - Lifetime
- 2001-10-18 DE DE60126425T patent/DE60126425T2/de not_active Expired - Lifetime
- 2001-10-18 ES ES01981688T patent/ES2280405T3/es not_active Expired - Lifetime
- 2001-10-18 CZ CZ20031388A patent/CZ20031388A3/cs unknown
- 2001-10-18 AU AU2002213317A patent/AU2002213317B2/en not_active Ceased
- 2001-10-18 CN CNB018191665A patent/CN1279033C/zh not_active Expired - Fee Related
-
2003
- 2003-04-28 IL IL155612A patent/IL155612A/en not_active IP Right Cessation
- 2003-05-19 NO NO20032241A patent/NO20032241D0/no unknown
Also Published As
Publication number | Publication date |
---|---|
ES2280405T3 (es) | 2007-09-16 |
KR20040020865A (ko) | 2004-03-09 |
HUP0301917A3 (en) | 2005-11-28 |
IL155612A (en) | 2010-05-31 |
BR0115448A (pt) | 2004-02-17 |
IL155612A0 (en) | 2003-11-23 |
NO20032241D0 (no) | 2003-05-19 |
AU1331702A (en) | 2002-06-03 |
EP1345915A4 (en) | 2005-08-03 |
DE60126425T2 (de) | 2007-10-18 |
EP1345915B1 (en) | 2007-01-31 |
CA2429378A1 (en) | 2002-05-30 |
MXPA03004332A (es) | 2004-05-04 |
KR100734456B1 (ko) | 2007-07-03 |
US20020062028A1 (en) | 2002-05-23 |
WO2002042283A1 (en) | 2002-05-30 |
JP2004518640A (ja) | 2004-06-24 |
PL361003A1 (en) | 2004-09-20 |
CN1279033C (zh) | 2006-10-11 |
CA2429378C (en) | 2008-03-18 |
JP4579496B2 (ja) | 2010-11-10 |
ATE353079T1 (de) | 2007-02-15 |
DE60126425D1 (de) | 2007-03-22 |
CN1474817A (zh) | 2004-02-11 |
AU2002213317B2 (en) | 2007-03-15 |
US6448401B1 (en) | 2002-09-10 |
EP1345915A1 (en) | 2003-09-24 |
CZ20031388A3 (cs) | 2003-08-13 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FA9A | Lapse of provisional patent protection due to relinquishment or protection considered relinquished |