BR112013010075A2 - compostos intermediários e processo para a preparação de fingolimod - Google Patents
compostos intermediários e processo para a preparação de fingolimodInfo
- Publication number
- BR112013010075A2 BR112013010075A2 BR112013010075A BR112013010075A BR112013010075A2 BR 112013010075 A2 BR112013010075 A2 BR 112013010075A2 BR 112013010075 A BR112013010075 A BR 112013010075A BR 112013010075 A BR112013010075 A BR 112013010075A BR 112013010075 A2 BR112013010075 A2 BR 112013010075A2
- Authority
- BR
- Brazil
- Prior art keywords
- fingolimod
- preparation
- intermediate compounds
- compounds
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title 1
- KKGQTZUTZRNORY-UHFFFAOYSA-N fingolimod Chemical compound CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 KKGQTZUTZRNORY-UHFFFAOYSA-N 0.000 title 1
- 229960000556 fingolimod Drugs 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
- C07C213/02—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C201/00—Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
- C07C201/06—Preparation of nitro compounds
- C07C201/12—Preparation of nitro compounds by reactions not involving the formation of nitro groups
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C205/00—Compounds containing nitro groups bound to a carbon skeleton
- C07C205/01—Compounds containing nitro groups bound to a carbon skeleton having nitro groups bound to acyclic carbon atoms
- C07C205/02—Compounds containing nitro groups bound to a carbon skeleton having nitro groups bound to acyclic carbon atoms of a saturated carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C205/00—Compounds containing nitro groups bound to a carbon skeleton
- C07C205/27—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups
- C07C205/28—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups having nitro groups and etherified hydroxy groups bound to acyclic carbon atoms of the carbon skeleton
- C07C205/31—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups having nitro groups and etherified hydroxy groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C205/00—Compounds containing nitro groups bound to a carbon skeleton
- C07C205/39—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by esterified hydroxy groups
- C07C205/40—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by esterified hydroxy groups having nitro groups and esterified hydroxy groups bound to acyclic carbon atoms of the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C205/00—Compounds containing nitro groups bound to a carbon skeleton
- C07C205/45—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by at least one doubly—bound oxygen atom, not being part of a —CHO group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/02—Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D319/04—1,3-Dioxanes; Hydrogenated 1,3-dioxanes
- C07D319/06—1,3-Dioxanes; Hydrogenated 1,3-dioxanes not condensed with other 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
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/40—Esters thereof
- C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
- C07F9/4021—Esters of aromatic acids (P-C aromatic linkage)
-
- 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
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/40—Esters thereof
- C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
- C07F9/4056—Esters of arylalkanephosphonic 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
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/54—Quaternary phosphonium compounds
- C07F9/5442—Aromatic phosphonium compounds (P-C aromatic linkage)
-
- 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
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/54—Quaternary phosphonium compounds
- C07F9/5456—Arylalkanephosphonium compounds
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40748310P | 2010-10-28 | 2010-10-28 | |
| PCT/IL2011/000838 WO2012056458A2 (en) | 2010-10-28 | 2011-10-27 | Intermediate compounds and process for the preparation of fingolimod |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112013010075A2 true BR112013010075A2 (pt) | 2017-10-24 |
Family
ID=45994490
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112013010075A BR112013010075A2 (pt) | 2010-10-28 | 2011-10-27 | compostos intermediários e processo para a preparação de fingolimod |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8735627B2 (pt) |
| EP (1) | EP2632889B1 (pt) |
| JP (1) | JP2014503478A (pt) |
| CN (1) | CN103313964A (pt) |
| AU (1) | AU2011322115A1 (pt) |
| BR (1) | BR112013010075A2 (pt) |
| CA (1) | CA2815634A1 (pt) |
| ES (1) | ES2697605T3 (pt) |
| MX (1) | MX2013004649A (pt) |
| PL (1) | PL2632889T3 (pt) |
| WO (1) | WO2012056458A2 (pt) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ2012406A3 (cs) * | 2012-06-15 | 2013-12-27 | Zentiva, K.S. | Způsob výroby fingolimodu založený na otevírání aziridinového kruhu |
| CN103539683A (zh) * | 2012-07-17 | 2014-01-29 | 广东东阳光药业有限公司 | 治疗硬化病的药物的新晶型及其制备方法 |
| CN103804123B (zh) * | 2012-11-14 | 2016-12-07 | 成都弘达药业有限公司 | 一种盐酸芬戈莫德的合成方法及其中间体 |
| EP2945927A4 (en) | 2013-01-17 | 2017-01-18 | Shilpa Medicare Limited | Process for preparation of fingolimod and its salts |
| CN103145689B (zh) * | 2013-01-24 | 2014-07-16 | 华东师范大学 | 合成芬戈莫德中间体的方法 |
| CN103724215A (zh) * | 2013-11-28 | 2014-04-16 | 镇江圣安医药有限公司 | 2-氨基-2-[2-(4-辛基苯基)乙基]-1,3-丙二醇的新型衍生物及其应用 |
| EP3092222B1 (en) | 2014-01-07 | 2018-02-14 | Emcure Pharmaceuticals Limited | Improved fingolimod process |
| US9925138B2 (en) | 2015-01-20 | 2018-03-27 | Handa Pharmaceuticals, Llc | Stable solid fingolimod dosage forms |
| JP2017008044A (ja) * | 2015-06-22 | 2017-01-12 | 学校法人 久留米大学 | ドーパミンシグナル伝達の抑制剤 |
| CN105924327A (zh) * | 2016-05-05 | 2016-09-07 | 成都百裕制药股份有限公司 | 一种芬戈莫德中间体及其类似物的制备方法 |
| WO2020165672A1 (en) | 2019-02-15 | 2020-08-20 | Shivalik Rasayan Limited | Process for preparation of highly pure fingolimod hydrochloride |
| WO2021158848A1 (en) * | 2020-02-07 | 2021-08-12 | Argentum Pharmaceuticals Llc | Dosage regimen of an s1p receptor agonist |
| US11135197B2 (en) | 2020-02-07 | 2021-10-05 | Argentum Pharmaceuticals Llc | Dosage regimen of an S1P receptor modulator |
| CN112679299B (zh) * | 2020-12-29 | 2022-03-18 | 湖南科技大学 | 一种二芳基甲烷及其衍生物的制备方法 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2946824A (en) | 1958-10-15 | 1960-07-26 | Gen Aniline & Film Corp | Alkylbenzyltriphenylphosphonium chlorides |
| US4086341A (en) * | 1974-08-22 | 1978-04-25 | Bayer Aktiengesellschaft | Cephalosporin derivatives |
| FI864901A (fi) | 1985-12-06 | 1987-06-07 | Ciba Geigy Ag | Hydroxitioetrar. |
| US4857659A (en) * | 1986-04-28 | 1989-08-15 | Merck Frosst Canada, Inc. | Stereoselective synthesis of leukotriene antagonists |
| US4978793A (en) * | 1988-06-23 | 1990-12-18 | W. R. Grace & Co.-Conn. | Novel process for the preparation of serinol |
| JP2579602B2 (ja) | 1992-10-21 | 1997-02-05 | 吉富製薬株式会社 | ２−アミノ−１，３−プロパンジオール化合物および免疫抑制剤 |
| DE19711762A1 (de) | 1997-03-21 | 1998-09-24 | Huels Chemische Werke Ag | Verfahren zur Herstellung von Bishydroxymethylverbindungen |
| WO1999001420A1 (fr) | 1997-07-03 | 1999-01-14 | Taito Co., Ltd. | Procede de preparation de derives d'acide 2-aminomalonique, et intermediaires utilises dans ce procede |
| JP4079505B2 (ja) | 1998-04-28 | 2008-04-23 | 田辺三菱製薬株式会社 | ２−アミノ−２−［２−（４−オクチルフェニル）エチル］プロパン−１，３−ジオールの新規な製造法 |
| DK1129066T3 (da) | 1998-11-11 | 2005-03-29 | Novartis Ag | Fremstilling af 2-amino-2-[2-(C2-20alkylphenyl)ethyl]propan-1,3-dioler |
| CN1144779C (zh) | 1999-03-11 | 2004-04-07 | 杭州中美华东制药有限公司 | 制备2-[2-(4-烷基苯基)-乙基]-2-氨基-丙二醇的方法以及其中制得的中间产物 |
| CN1241903C (zh) | 2003-10-14 | 2006-02-15 | 马启明 | 制备2－对辛基苯乙基－2－氨基丙二醇的方法 |
| WO2005041899A2 (en) | 2003-11-03 | 2005-05-12 | University Of Virginia Patent Foundation | Orally available sphingosine 1-phosphate receptor agonists and antagonists |
| DE10355169A1 (de) | 2003-11-26 | 2005-06-23 | Studiengesellschaft Kohle Mbh | Verfahren zur Herstellung von substituierten Arylverbindungen |
| JP2006199652A (ja) * | 2005-01-21 | 2006-08-03 | Ajinomoto Co Inc | ２’−デオキシグアノシン化合物の製造方法 |
| CN1310869C (zh) | 2005-11-22 | 2007-04-18 | 江苏吴中苏药医药开发有限责任公司 | 2－氨基－2－[2－(4－烷基苯基)乙基]－1,3－丙二醇的制备方法 |
| US20090082471A1 (en) | 2007-09-26 | 2009-03-26 | Protia, Llc | Deuterium-enriched fingolimod |
| EP2217561A2 (en) | 2007-11-02 | 2010-08-18 | Concert Pharmaceuticals, Inc. | Deuterated fingolimod |
| TW201004965A (en) | 2008-04-28 | 2010-02-01 | Basf Se | New borane-amine complexes and their application in Suzuki-type cross-coupling reactions |
| MX2011004924A (es) | 2008-11-11 | 2011-05-30 | Novartis Ag | Sales de fingolimod. |
| MX2011004962A (es) | 2008-11-11 | 2011-05-30 | Novartis Ag | Formas cristalinas de hcl de fingolimod. |
| WO2011159870A1 (en) * | 2010-06-17 | 2011-12-22 | Bracco Imaging S.P.A. | Methods and compounds for the preparation of fluorine-labeled deoxy-fty720 |
-
2011
- 2011-10-27 US US13/881,961 patent/US8735627B2/en active Active
- 2011-10-27 BR BR112013010075A patent/BR112013010075A2/pt not_active IP Right Cessation
- 2011-10-27 AU AU2011322115A patent/AU2011322115A1/en not_active Abandoned
- 2011-10-27 JP JP2013535590A patent/JP2014503478A/ja active Pending
- 2011-10-27 MX MX2013004649A patent/MX2013004649A/es not_active Application Discontinuation
- 2011-10-27 CA CA2815634A patent/CA2815634A1/en not_active Abandoned
- 2011-10-27 WO PCT/IL2011/000838 patent/WO2012056458A2/en active Application Filing
- 2011-10-27 CN CN2011800632167A patent/CN103313964A/zh active Pending
- 2011-10-27 EP EP11835740.9A patent/EP2632889B1/en active Active
- 2011-10-27 ES ES11835740T patent/ES2697605T3/es active Active
- 2011-10-27 PL PL11835740T patent/PL2632889T3/pl unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN103313964A (zh) | 2013-09-18 |
| EP2632889A2 (en) | 2013-09-04 |
| US8735627B2 (en) | 2014-05-27 |
| US20130217899A1 (en) | 2013-08-22 |
| PL2632889T3 (pl) | 2019-04-30 |
| WO2012056458A2 (en) | 2012-05-03 |
| WO2012056458A3 (en) | 2013-07-18 |
| EP2632889B1 (en) | 2018-08-29 |
| JP2014503478A (ja) | 2014-02-13 |
| MX2013004649A (es) | 2013-06-05 |
| EP2632889A4 (en) | 2015-01-07 |
| CA2815634A1 (en) | 2012-05-03 |
| AU2011322115A1 (en) | 2013-05-30 |
| ES2697605T3 (es) | 2019-01-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B15I | Others concerning applications: loss of priority | ||
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] | ||
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |