AU2010266213B2 - Synthesis of N4- (2, 2-dimethyl-4- [ (dihydrogen phosphonoxy ] -3-oxo-5-pyrido [1, 4] oxazin-6-yl)-5-fluoro-N2- (3, 4, 5,-trimethoxyphenyl) -2, 4- pyrimidinediamine disodium salt - Google Patents

Synthesis of N4- (2, 2-dimethyl-4- [ (dihydrogen phosphonoxy ] -3-oxo-5-pyrido [1, 4] oxazin-6-yl)-5-fluoro-N2- (3, 4, 5,-trimethoxyphenyl) -2, 4- pyrimidinediamine disodium salt Download PDF

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AU2010266213B2
AU2010266213B2 AU2010266213A AU2010266213A AU2010266213B2 AU 2010266213 B2 AU2010266213 B2 AU 2010266213B2 AU 2010266213 A AU2010266213 A AU 2010266213A AU 2010266213 A AU2010266213 A AU 2010266213A AU 2010266213 B2 AU2010266213 B2 AU 2010266213B2
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compound
formula
amide
solvate
conditions suitable
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AU2010266213A1 (en
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Ulfried Felfer
Karl-Heinz Giselbrecht
Michael Wolberg
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Rigel Pharmaceuticals Inc
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Rigel Pharmaceuticals Inc
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    • 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
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • 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
    • C07F9/091—Esters of phosphoric acids with hydroxyalkyl compounds with further substituents on alkyl

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  • 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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
AU2010266213A 2009-07-02 2010-07-01 Synthesis of N4- (2, 2-dimethyl-4- [ (dihydrogen phosphonoxy ] -3-oxo-5-pyrido [1, 4] oxazin-6-yl)-5-fluoro-N2- (3, 4, 5,-trimethoxyphenyl) -2, 4- pyrimidinediamine disodium salt Active AU2010266213B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US27007309P 2009-07-02 2009-07-02
US61/270,073 2009-07-02
PCT/US2010/040792 WO2011002999A1 (en) 2009-07-02 2010-07-01 Synthesis of n4- (2, 2-dimethyl-4- [ (dihydrogen phosphonoxy ] -3-oxo-5-pyrido [1, 4] oxazin-6-yl)-5-fluoro-n2- (3, 4, 5,-trimethoxyphenyl) -2, 4- pyrimidinediamine disodium salt

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AU2010266213A1 AU2010266213A1 (en) 2012-02-02
AU2010266213B2 true AU2010266213B2 (en) 2015-06-18

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AU2010266213A Active AU2010266213B2 (en) 2009-07-02 2010-07-01 Synthesis of N4- (2, 2-dimethyl-4- [ (dihydrogen phosphonoxy ] -3-oxo-5-pyrido [1, 4] oxazin-6-yl)-5-fluoro-N2- (3, 4, 5,-trimethoxyphenyl) -2, 4- pyrimidinediamine disodium salt

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US (3) US8299242B2 (enExample)
EP (1) EP2448950B1 (enExample)
JP (1) JP5739882B2 (enExample)
CN (1) CN102482305B (enExample)
AU (1) AU2010266213B2 (enExample)
BR (1) BRPI1011888A2 (enExample)
CA (1) CA2766801C (enExample)
CY (1) CY1117489T1 (enExample)
DK (1) DK2448950T3 (enExample)
EA (1) EA021657B1 (enExample)
ES (1) ES2565985T3 (enExample)
HR (1) HRP20160319T1 (enExample)
HU (1) HUE027212T2 (enExample)
ME (1) ME02388B (enExample)
PL (1) PL2448950T3 (enExample)
RS (1) RS54679B1 (enExample)
SG (1) SG176799A1 (enExample)
SI (1) SI2448950T1 (enExample)
SM (1) SMT201600084B (enExample)
UA (1) UA108077C2 (enExample)
WO (1) WO2011002999A1 (enExample)

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JP5468899B2 (ja) 2006-07-20 2014-04-09 アフィニウム ファーマシューティカルズ， インク． Ｆａｂｉインヒビターとしてのアクリルアミド誘導体
UA108077C2 (xx) 2009-07-02 2015-03-25 Синтез динатрієвої солі n4-(2,2-диметил-4-$(дигідрофосфонокси)метил]-3-оксо-5-піридо$1,4]оксазин-6-іл)-5-фтор-n2-(3,4,5-триметоксифеніл)-2,4-піримідиндіаміну
US20110206661A1 (en) * 2010-02-24 2011-08-25 Auspex Pharmaceuticals, Inc. Trimethoxyphenyl inhibitors of tyrosine kinase
EP2736487B2 (en) * 2011-07-28 2024-08-28 Rigel Pharmaceuticals, Inc. New (trimethoxyphenylamino)pyrimidinyl formulations
TWI526437B (zh) * 2011-09-09 2016-03-21 台灣神隆股份有限公司 卡巴他賽之結晶型
US8426450B1 (en) * 2011-11-29 2013-04-23 Helsinn Healthcare Sa Substituted 4-phenyl pyridines having anti-emetic effect
MY170437A (en) 2012-06-19 2019-07-31 Debiopharm Int Sa Prodrug derivatives of (e)-n-methyl-n-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
CN102746337B (zh) * 2012-06-21 2014-12-17 成都苑东药业有限公司 一种2，4-嘧啶二胺类化合物及其制备方法
TW201410657A (zh) 2012-08-02 2014-03-16 Endo Pharmaceuticals Inc 經取代胺基－嘧啶衍生物
LT3083648T (lt) * 2013-12-20 2019-01-25 Rigel Pharmaceuticals, Inc. Farmacinis būdas ir tarpiniai junginiai
PL3419628T3 (pl) 2016-02-26 2021-05-31 Debiopharm International Sa Lek do leczenia zakażeń stopy cukrzycowej
EP3509578B1 (en) 2016-09-08 2022-12-21 Glykon Technologies Group, LLC Monomeric bimetal hydroxycitric acid compounds and methods of making and using the same
JP2020536100A (ja) * 2017-10-04 2020-12-10 セルジーン コーポレイション シス−４−［２−｛［（３ｓ，４ｒ）−３−フルオロキサン−４−イル］アミノ｝−８−（２，４，６−トリクロロアニリノ）−９ｈ−プリン−９−イル］−１−メチルシクロヘキサン−１−カルボキサミドの製造プロセス
HRP20230437T1 (hr) 2019-02-14 2023-07-07 Debiopharm International S.A. Formulacija afabicina, postupak izrade iste
CN113939306B (zh) 2019-06-14 2024-07-19 德彪药业国际股份公司 用于治疗涉及生物膜的细菌感染的药物及其用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006078846A1 (en) * 2005-01-19 2006-07-27 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
WO2008064274A1 (en) * 2006-11-21 2008-05-29 Rigel Pharmaceuticals, Inc. Prodrug salts of 2, 4-pyrimidinediamine compounds and their uses

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US303022A (en) 1884-08-05 Egg-beater
US324087A (en) 1885-08-11 Abel combs
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US20040024716A1 (en) 2002-04-12 2004-02-05 James Malatesta Mail sorting processes and systems
CN103169708B (zh) 2002-07-29 2018-02-02 里格尔药品股份有限公司 用2,4‑嘧啶二胺化合物治疗或者预防自体免疫性疾病的方法
US7122542B2 (en) 2003-07-30 2006-10-17 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
US20060047135A1 (en) 2004-08-30 2006-03-02 Chadwick Scott T Process for preparing chloromethyl di-tert-butylphosphate
US20090114877A1 (en) * 2005-09-13 2009-05-07 Eisai R&D Management Co., Ltd. Composition Containing Stability-Improved Chloromethyl Phosphate Derivatve and Process for Producing Same
UA108077C2 (xx) 2009-07-02 2015-03-25 Синтез динатрієвої солі n4-(2,2-диметил-4-$(дигідрофосфонокси)метил]-3-оксо-5-піридо$1,4]оксазин-6-іл)-5-фтор-n2-(3,4,5-триметоксифеніл)-2,4-піримідиндіаміну

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006078846A1 (en) * 2005-01-19 2006-07-27 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
WO2008064274A1 (en) * 2006-11-21 2008-05-29 Rigel Pharmaceuticals, Inc. Prodrug salts of 2, 4-pyrimidinediamine compounds and their uses

Also Published As

Publication number Publication date
CN102482305B (zh) 2016-07-13
CA2766801C (en) 2018-03-13
US20110003986A1 (en) 2011-01-06
CN102482305A (zh) 2012-05-30
BRPI1011888A2 (pt) 2016-04-12
US20130274499A1 (en) 2013-10-17
HRP20160319T1 (hr) 2016-04-22
AU2010266213A1 (en) 2012-02-02
SI2448950T1 (sl) 2016-05-31
JP5739882B2 (ja) 2015-06-24
HUE027212T2 (en) 2016-10-28
RS54679B1 (sr) 2016-08-31
WO2011002999A1 (en) 2011-01-06
EP2448950A1 (en) 2012-05-09
CY1117489T1 (el) 2017-04-26
EP2448950B1 (en) 2016-01-13
DK2448950T3 (en) 2016-04-04
US8691798B2 (en) 2014-04-08
SMT201600084B (it) 2016-04-29
EA021657B1 (ru) 2015-08-31
US8481724B2 (en) 2013-07-09
CA2766801A1 (en) 2011-01-06
US8299242B2 (en) 2012-10-30
EA201270114A1 (ru) 2012-05-30
ME02388B (me) 2016-09-20
PL2448950T3 (pl) 2016-06-30
SG176799A1 (en) 2012-01-30
US20130018185A1 (en) 2013-01-17
UA108077C2 (xx) 2015-03-25
HK1169996A1 (zh) 2013-02-15
ES2565985T3 (es) 2016-04-08
JP2012532143A (ja) 2012-12-13

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