ES2550003T3 - Producto intermedio de dimeglumina de fosaprepitant, fosaprepitant neutro y dimeglumina de fosaprepitant amorfa, y procesos para sus preparaciones - Google Patents

Producto intermedio de dimeglumina de fosaprepitant, fosaprepitant neutro y dimeglumina de fosaprepitant amorfa, y procesos para sus preparaciones Download PDF

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Publication number
ES2550003T3
ES2550003T3 ES09806538.6T ES09806538T ES2550003T3 ES 2550003 T3 ES2550003 T3 ES 2550003T3 ES 09806538 T ES09806538 T ES 09806538T ES 2550003 T3 ES2550003 T3 ES 2550003T3
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Spain
Prior art keywords
fosaprepitant
dimeglumine
preparations
neutral
processes
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ES09806538.6T
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English (en)
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ES2550003T5 (es
Inventor
Navin Ganeshbhatt
Nikhil Rasiklaltrivedi
Mahesh Khedekar
Sukumar Sinha
Mubeen Ahmed Khan
Ramjilal Yadav
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Glenmark Generics Ltd
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Glenmark Generics Ltd
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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
    • C07F9/547—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Otolaryngology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hospice & Palliative Care (AREA)
  • Toxicology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Un proceso para la preparación de una forma cristalina de ácido dibencil {3-[2(R)-[(1R)-1-[3,5- bis(trifluorometil)fenil]etoxi]-3(S)-(4-fluorofenil)morfolin-4-il}-5-oxo-4,5-dihidro-[1,2,4]-triazol-1-il}fosfónico de fórmula (II),**Fórmula** y el proceso comprende: (a) proporcionar una solución de ácido dibencil {3-[2(R)-[(1R)-1-[3,5-bis(trifluorometil)fenil]etoxi]-3(S)-(4- fluorofenil)morfolin-4-il}-5-oxo-4,5-dihidro-[1,2,4]-triazolil}fosfónico en un solvente o una mezcla de solventes; (b) adicionar un anti-solvente a la solución del paso (a) para hacer precipitar un sólido; y (c) recuperar la forma cristalina de ácido dibencil{3-[2(R)-[(1R)-1-[3,5-bis(trifluorometil)fenil]etoxi]-3(S)-(4- fluorofenil)morfolin-4-il}-5-oxo-4,5-dihidro-[1,2,4]-triazol-1-il}fosfónico como un precipitado, en cuyo caso la precipitación se lleva a cabo a un rango de temperaturas desde -10 °C a 35 °C.

Description

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Claims (1)

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ES09806538.6T 2008-07-17 2009-07-17 Producto intermedio de dimeglumina de fosaprepitant, fosaprepitant neutro y dimeglumina de fosaprepitant amorfa, y procesos para sus preparaciones Active ES2550003T5 (es)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
IN1510MU2008 2008-07-17
INMU15102008 2008-07-17
INMU21542008 2008-10-08
IN2154MU2008 2008-10-08
IN690MU2009 2009-03-24
INMU06902009 2009-03-24
PCT/IN2009/000408 WO2010018595A2 (en) 2008-07-17 2009-07-17 Fosaprepitant dimeglumine intermediate, neutral fosaprepitant, and amorphous fosaprepitant dimeglumine and processes for their preparations

Publications (2)

Publication Number Publication Date
ES2550003T3 true ES2550003T3 (es) 2015-11-03
ES2550003T5 ES2550003T5 (es) 2018-08-22

Family

ID=41669418

Family Applications (1)

Application Number Title Priority Date Filing Date
ES09806538.6T Active ES2550003T5 (es) 2008-07-17 2009-07-17 Producto intermedio de dimeglumina de fosaprepitant, fosaprepitant neutro y dimeglumina de fosaprepitant amorfa, y procesos para sus preparaciones

Country Status (5)

Country Link
US (1) US8623844B2 (es)
EP (1) EP2303901B2 (es)
CA (1) CA2730681C (es)
ES (1) ES2550003T5 (es)
WO (1) WO2010018595A2 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011045817A2 (en) 2009-10-15 2011-04-21 Sandoz Private Limited Process for the preparation of fosaprepitant, intermediate and pharmaceutical acceptable salt thereof
CN102166199B (zh) * 2011-04-02 2012-11-07 武汉希熙生物科技有限公司 一种注射用福沙吡坦二甲葡胺冻干制剂的制备方法
EP2714701B1 (en) * 2011-06-03 2016-07-13 Hetero Research Foundation Process for fosaprepitant
CN102977142B (zh) * 2011-09-02 2017-03-29 江苏豪森药业集团有限公司 福沙匹坦二甲葡胺的制备方法
CN103183708A (zh) * 2011-12-31 2013-07-03 扬子江药业集团上海海尼药业有限公司 福沙吡坦二甲葡胺的制备方法
WO2013168176A2 (en) * 2012-03-30 2013-11-14 Glenmark Generics Limited Process for preparation of fosaprepitant and salt thereof
CZ304982B6 (cs) * 2012-04-30 2015-03-11 Zentiva, K.S. Způsob přípravy a čištění nových polymorfů intermediátu fosaprepitantu
CN102675369B (zh) * 2012-05-16 2017-07-11 北京华众思康医药技术有限公司 一种制备[3‑[(2r)‑[(1r)‑1‑[3，5‑二(三氟甲基)苯基]乙氧基]‑3(s)‑(4‑氟苯基)吗啉‑4‑基]甲基]‑5‑氧代‑4，5‑二氢‑[1，2，4]‑三唑‑1‑基]膦酸一苄酯的新方法
US9850267B2 (en) * 2015-06-03 2017-12-26 Navinta, Llc Crystalline fosaprepitant dicyclohexylamine salt and its preparation
WO2017021880A1 (en) * 2015-08-03 2017-02-09 Leiutis Pharmaceuticals Pvt Ltd Liquid formulations of fosaprepitant
WO2017093899A1 (en) * 2015-12-01 2017-06-08 Piramal Enterprises Limited A process for preparation of fosaprepitant dimeglumine and an intermediate thereof
CN107353303B (zh) 2016-05-09 2020-09-01 上海奥博生物医药技术有限公司 一种福沙匹坦磷酸酯中间体的制备方法
CN106565783A (zh) * 2016-11-08 2017-04-19 山东裕欣药业有限公司 福沙匹坦双葡甲胺晶体化合物及其制备方法、药物组合物
US11065265B2 (en) 2018-05-18 2021-07-20 Spes Pharmaceuticals Inc. Compositions of fosaprepitant and methods of preparation
CN109608498A (zh) * 2018-12-25 2019-04-12 四川制药制剂有限公司 一种福沙匹坦超临界反应制备方法
US11654154B2 (en) * 2019-01-29 2023-05-23 Navinta Iii Inc Process for preparing injectable Fosaprepitant Dimeglumine compositions having improved storage stability
CA3173697A1 (en) 2020-04-03 2021-10-07 Mike TROWER An nk-1 receptor antagonist for treating a disease selecting from sepsis, septic shock, acute respiratory distress syndrome (ards) or multiple organ dysfunction syndrome (mods)
CA3177477A1 (en) 2020-06-02 2021-12-09 Nerre Therapeutics Limited Neurokinin (nk)-1 receptor antagonists for use in the treatment of pulmonary fibrosis conditions promoted by mechanical injury to the lungs

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL112778A0 (en) 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them
AR051475A1 (es) 2004-11-05 2007-01-17 Merck & Co Inc Procedimiento para acido{3- [2 (r) -[(1r) - 1-[ 3,5- bis( trifluorometil)- fenil] etoxi] -3 (s) - (4- fluorfenil) morfolin -4- il]metil -5-oxo-4,5-dihidro- [1,2,4]-triazol-1-il} fosfonico

Also Published As

Publication number Publication date
WO2010018595A3 (en) 2011-05-26
CA2730681A1 (en) 2010-02-18
CA2730681C (en) 2017-03-07
EP2303901A2 (en) 2011-04-06
EP2303901B1 (en) 2015-09-23
EP2303901A4 (en) 2012-07-18
WO2010018595A2 (en) 2010-02-18
US8623844B2 (en) 2014-01-07
US20110130366A1 (en) 2011-06-02
EP2303901B2 (en) 2018-05-09
EP2303901B8 (en) 2015-12-23
ES2550003T5 (es) 2018-08-22

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