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AR051475A1 - 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 - Google Patents

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

Info

Publication number
AR051475A1
AR051475A1 ARP050104590A ARP050104590A AR051475A1 AR 051475 A1 AR051475 A1 AR 051475A1 AR P050104590 A ARP050104590 A AR P050104590A AR P050104590 A ARP050104590 A AR P050104590A AR 051475 A1 AR051475 A1 AR 051475A1
Authority
AR
Argentina
Prior art keywords
compound
fluorfenil
trifluorometil
etoxi
morfolin
Prior art date
Application number
ARP050104590A
Other languages
English (en)
Original Assignee
Merck & Co Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR051475A1 publication Critical patent/AR051475A1/es

Links

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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Rheumatology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pain & Pain Management (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Este compuesto es util como antagonista de receptor de la sustancia P (neuroquinina 1). En particular, el compuesto es util, por ejemplo, en el tratamiento de emesis y enfermedades inflamatorias. Reivindicacion 1: Un procedimiento para preparar un compuesto de formula (1), o una sal farmacéuticamente aceptable del mismo, que comprende: la reduccion catalítica de un compuesto de formula (2), en la que Bn es bencilo; opcionalmente en presencia del contraion de una sal farmacéuticamente aceptable, proporcionando el compuesto de formula (3), o una sal farmacéuticamente aceptable del mismo. Reivindicacion 15: Un compuesto de formula (4), o una sal del mismo.
ARP050104590A 2004-11-05 2005-11-02 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 AR051475A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US62520904P 2004-11-05 2004-11-05

Publications (1)

Publication Number Publication Date
AR051475A1 true AR051475A1 (es) 2007-01-17

Family

ID=36263958

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050104590A AR051475A1 (es) 2004-11-05 2005-11-02 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

Country Status (12)

Country Link
US (2) US7807829B2 (es)
EP (1) EP1809379B1 (es)
JP (1) JP4917541B2 (es)
CN (2) CN101056672A (es)
AR (1) AR051475A1 (es)
AT (1) ATE529162T1 (es)
AU (1) AU2005310240B9 (es)
BR (1) BRPI0517989A (es)
CA (1) CA2586114A1 (es)
ES (1) ES2373451T3 (es)
TW (1) TWI358413B (es)
WO (1) WO2006060110A2 (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101630884B1 (ko) * 2008-02-26 2016-06-15 산도즈 아게 모르폴린 유도체의 제조
WO2010018595A2 (en) * 2008-07-17 2010-02-18 Glenmark Generics Limited Fosaprepitant dimeglumine intermediate, neutral fosaprepitant, and amorphous fosaprepitant dimeglumine and processes for their preparations
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
WO2012146692A1 (en) 2011-04-29 2012-11-01 Sandoz Ag Novel intermediates for the preparation of highly pure aprepitant or fosaprepitant
CN102850398B (zh) * 2011-06-27 2015-06-10 上海医药工业研究院 制备福沙匹坦的方法
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
CN103030668B (zh) * 2011-10-09 2016-06-15 江苏豪森药业集团有限公司 一种制备福沙匹坦二甲葡胺的方法
CN102558232B (zh) * 2011-12-31 2015-04-08 江苏奥赛康药业股份有限公司 一种福沙吡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
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
CN102838634B (zh) * 2012-09-28 2015-05-13 江苏奥赛康药业股份有限公司 一种降低化合物中钯残留的方法及应用这种方法的高纯度福沙匹坦二甲葡胺的制备方法
CN102850399B (zh) * 2012-09-28 2015-03-04 江苏奥赛康药业股份有限公司 一种福沙匹坦二甲葡胺的精制方法
CN103159797A (zh) * 2013-03-29 2013-06-19 山东罗欣药业股份有限公司 福沙吡坦二甲葡胺晶型化合物
CN103204878A (zh) * 2013-03-29 2013-07-17 山东罗欣药业股份有限公司 一种福沙吡坦二甲葡胺的合成方法
CN104098604B (zh) * 2013-04-10 2016-12-28 山东省生物药物研究院 一种制备福沙匹坦二甲葡胺的方法
CN105254668B (zh) * 2013-05-14 2017-10-10 北京百川汇德医药技术开发有限公司 一种福沙匹坦及其可药用盐的制备新方法
IN2013MU03772A (es) * 2013-12-02 2015-07-31 Piramal Entpr Ltd
US9850267B2 (en) 2015-06-03 2017-12-26 Navinta, Llc Crystalline fosaprepitant dicyclohexylamine salt and its preparation
SG10202112588PA (en) * 2015-11-19 2021-12-30 Biohaven Pharm Holding Co Ltd Amine prodrugs of pharmaceutical compounds
EP3383829B1 (en) 2015-12-01 2020-10-21 Piramal Enterprises Limited A process for preparation of fosaprepitant dimeglumine and an intermediate thereof
CN108948080B (zh) * 2017-05-22 2022-03-04 齐鲁制药有限公司 一种福沙匹坦药用盐的制备方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW385308B (en) * 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
EP1309605A1 (en) * 2000-08-18 2003-05-14 The Board Of Trustees Of The University Of Illinois Prodrugs of betulinic acid derivatives for the treatment of cancer and hiv

Also Published As

Publication number Publication date
EP1809379A2 (en) 2007-07-25
EP1809379B1 (en) 2011-10-19
US7807829B2 (en) 2010-10-05
AU2005310240B2 (en) 2011-06-09
WO2006060110A3 (en) 2006-08-17
BRPI0517989A (pt) 2008-10-21
WO2006060110A2 (en) 2006-06-08
TWI358413B (en) 2012-02-21
US20100324287A1 (en) 2010-12-23
US20070265442A1 (en) 2007-11-15
JP4917541B2 (ja) 2012-04-18
CA2586114A1 (en) 2006-06-08
AU2005310240A1 (en) 2006-06-08
JP2008518970A (ja) 2008-06-05
CN103130834A (zh) 2013-06-05
CN101056672A (zh) 2007-10-17
AU2005310240B9 (en) 2011-10-13
ES2373451T3 (es) 2012-02-03
US7915407B2 (en) 2011-03-29
ATE529162T1 (de) 2011-11-15
TW200631959A (en) 2006-09-16

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