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} fosfonicoInfo
- 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
Links
- 239000002253 acid Substances 0.000 title 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 6
- 150000003839 salts Chemical class 0.000 abstract 4
- QDZOEBFLNHCSSF-PFFBOGFISA-N (2S)-2-[[(2R)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-1-[(2R)-2-amino-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2R)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide Chemical compound C([C@@H](C(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)NC(=O)[C@@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](N)CCCNC(N)=N)C1=CC=CC=C1 QDZOEBFLNHCSSF-PFFBOGFISA-N 0.000 abstract 1
- 102100024304 Protachykinin-1 Human genes 0.000 abstract 1
- 101800003906 Substance P Proteins 0.000 abstract 1
- 206010047700 Vomiting Diseases 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 238000010531 catalytic reduction reaction Methods 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 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
- C07F9/547—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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (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.
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) | CN103130834A (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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2715781C (en) * | 2008-02-26 | 2016-06-28 | Sandoz Ag | Preparation of morpholine derivatives |
| ES2550003T5 (es) | 2008-07-17 | 2018-08-22 | Glenmark Pharmaceuticals Limited | Producto intermedio de dimeglumina de fosaprepitant, fosaprepitant neutro y dimeglumina de fosaprepitant amorfa, y procesos para sus preparaciones |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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)
| 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 |
| US6569842B2 (en) * | 2000-08-18 | 2003-05-27 | Board Of Trustees Of The University Of Illinois, The | Method of preparing and use of prodrugs of betulinic acid derivatives |
-
2005
- 2005-11-02 AR ARP050104590A patent/AR051475A1/es unknown
- 2005-11-03 BR BRPI0517989-0A patent/BRPI0517989A/pt not_active IP Right Cessation
- 2005-11-03 CN CN2013100964534A patent/CN103130834A/zh active Pending
- 2005-11-03 EP EP05851364A patent/EP1809379B1/en active Active
- 2005-11-03 CA CA002586114A patent/CA2586114A1/en not_active Abandoned
- 2005-11-03 US US11/667,001 patent/US7807829B2/en active Active
- 2005-11-03 AU AU2005310240A patent/AU2005310240B9/en not_active Ceased
- 2005-11-03 WO PCT/US2005/039946 patent/WO2006060110A2/en active Application Filing
- 2005-11-03 JP JP2007539355A patent/JP4917541B2/ja active Active
- 2005-11-03 TW TW094138638A patent/TWI358413B/zh not_active IP Right Cessation
- 2005-11-03 CN CNA2005800380368A patent/CN101056672A/zh active Pending
- 2005-11-03 ES ES05851364T patent/ES2373451T3/es active Active
- 2005-11-03 AT AT05851364T patent/ATE529162T1/de active
-
2010
- 2010-08-25 US US12/862,857 patent/US7915407B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| CA2586114A1 (en) | 2006-06-08 |
| TW200631959A (en) | 2006-09-16 |
| US7915407B2 (en) | 2011-03-29 |
| AU2005310240B2 (en) | 2011-06-09 |
| CN101056672A (zh) | 2007-10-17 |
| AU2005310240A1 (en) | 2006-06-08 |
| US7807829B2 (en) | 2010-10-05 |
| WO2006060110A3 (en) | 2006-08-17 |
| JP4917541B2 (ja) | 2012-04-18 |
| JP2008518970A (ja) | 2008-06-05 |
| US20070265442A1 (en) | 2007-11-15 |
| TWI358413B (en) | 2012-02-21 |
| ATE529162T1 (de) | 2011-11-15 |
| CN103130834A (zh) | 2013-06-05 |
| US20100324287A1 (en) | 2010-12-23 |
| EP1809379A2 (en) | 2007-07-25 |
| AU2005310240B9 (en) | 2011-10-13 |
| EP1809379B1 (en) | 2011-10-19 |
| ES2373451T3 (es) | 2012-02-03 |
| BRPI0517989A (pt) | 2008-10-21 |
| WO2006060110A2 (en) | 2006-06-08 |
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