BRPI0517989A - processo para preparar um composto ou um sal farmaceuticamente aceitável do mesmo, e, composto ou um sal do mesmo - Google Patents
processo para preparar um composto ou um sal farmaceuticamente aceitável do mesmo, e, composto ou um sal do mesmoInfo
- Publication number
- BRPI0517989A BRPI0517989A BRPI0517989-0A BRPI0517989A BRPI0517989A BR PI0517989 A BRPI0517989 A BR PI0517989A BR PI0517989 A BRPI0517989 A BR PI0517989A BR PI0517989 A BRPI0517989 A BR PI0517989A
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- salt
- pharmaceutically acceptable
- preparing
- acceptable salt
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 150000003839 salts Chemical class 0.000 title abstract 5
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 102100024304 Protachykinin-1 Human genes 0.000 abstract 2
- 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
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 abstract 1
- 101000831616 Homo sapiens Protachykinin-1 Proteins 0.000 abstract 1
- 101800003906 Substance P Proteins 0.000 abstract 1
- 206010047700 Vomiting Diseases 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
- ADNPLDHMAVUMIW-CUZNLEPHSA-N substance P Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CCCN=C(N)N)C1=CC=CC=C1 ADNPLDHMAVUMIW-CUZNLEPHSA-N 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 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)
- 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
PROCESSO PARA PREPARAR UM COMPOSTO OU UM SAL FARMACEUTICAMENTE ACEITáVEL DO MESMO, E, COMPOSTO OU UM SAL DO MESMO. A presente invenção refere-se a um processo para a preparação do composto ácido {3 - ¢2(R)-Li R)- 1- ¢3,5-bis (trifluorometil) fenil!etóxi!-3 (5)-(4-fluorofenil)morfolin-4-il ¢metil! -5 -oxo-4,5 -diidro- ¢1,2,4! -triazol- 1- il}fosfónico e sais farmaceuticamente aceitáveis do mesmo. Este composto é útil como um antagonista do receptor da substância P (neurocinina- 1). Em particular, o composto é útil, por exemplo, no tratamento de êmese e doenças inflamatórias.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US62520904P | 2004-11-05 | 2004-11-05 | |
| PCT/US2005/039946 WO2006060110A2 (en) | 2004-11-05 | 2005-11-03 | Process for preparing {3-[2(r)-[(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(s)-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0517989A true BRPI0517989A (pt) | 2008-10-21 |
Family
ID=36263958
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0517989-0A BRPI0517989A (pt) | 2004-11-05 | 2005-11-03 | processo para preparar um composto ou um sal farmaceuticamente aceitável do mesmo, e, composto ou um sal do mesmo |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US7807829B2 (pt) |
| EP (1) | EP1809379B1 (pt) |
| JP (1) | JP4917541B2 (pt) |
| CN (2) | CN103130834A (pt) |
| AR (1) | AR051475A1 (pt) |
| AT (1) | ATE529162T1 (pt) |
| AU (1) | AU2005310240B9 (pt) |
| BR (1) | BRPI0517989A (pt) |
| CA (1) | CA2586114A1 (pt) |
| ES (1) | ES2373451T3 (pt) |
| TW (1) | TWI358413B (pt) |
| WO (1) | WO2006060110A2 (pt) |
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 |
| EP2303901B2 (en) | 2008-07-17 | 2018-05-09 | Glenmark Pharmaceuticals 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 |
| 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 |
| 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 |
| WO2015083033A1 (en) * | 2013-12-02 | 2015-06-11 | Piramal Enterprises Limited | An improved process for the preparation of fosaprepitant having improved purity |
| US9850267B2 (en) | 2015-06-03 | 2017-12-26 | Navinta, Llc | Crystalline fosaprepitant dicyclohexylamine salt and its preparation |
| SG11201803645PA (en) * | 2015-11-19 | 2018-06-28 | 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 |
| 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 |
-
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 CA CA002586114A patent/CA2586114A1/en not_active Abandoned
- 2005-11-03 AU AU2005310240A patent/AU2005310240B9/en not_active Ceased
- 2005-11-03 JP JP2007539355A patent/JP4917541B2/ja not_active Expired - Lifetime
- 2005-11-03 AT AT05851364T patent/ATE529162T1/de active
- 2005-11-03 WO PCT/US2005/039946 patent/WO2006060110A2/en not_active Ceased
- 2005-11-03 CN CNA2005800380368A patent/CN101056672A/zh active Pending
- 2005-11-03 TW TW094138638A patent/TWI358413B/zh not_active IP Right Cessation
- 2005-11-03 ES ES05851364T patent/ES2373451T3/es not_active Expired - Lifetime
- 2005-11-03 EP EP05851364A patent/EP1809379B1/en not_active Expired - Lifetime
- 2005-11-03 US US11/667,001 patent/US7807829B2/en active Active
-
2010
- 2010-08-25 US US12/862,857 patent/US7915407B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| US7915407B2 (en) | 2011-03-29 |
| JP2008518970A (ja) | 2008-06-05 |
| AU2005310240B9 (en) | 2011-10-13 |
| CA2586114A1 (en) | 2006-06-08 |
| TWI358413B (en) | 2012-02-21 |
| AU2005310240A1 (en) | 2006-06-08 |
| AR051475A1 (es) | 2007-01-17 |
| ATE529162T1 (de) | 2011-11-15 |
| CN103130834A (zh) | 2013-06-05 |
| CN101056672A (zh) | 2007-10-17 |
| WO2006060110A2 (en) | 2006-06-08 |
| TW200631959A (en) | 2006-09-16 |
| US20070265442A1 (en) | 2007-11-15 |
| WO2006060110A3 (en) | 2006-08-17 |
| EP1809379B1 (en) | 2011-10-19 |
| US7807829B2 (en) | 2010-10-05 |
| EP1809379A2 (en) | 2007-07-25 |
| AU2005310240B2 (en) | 2011-06-09 |
| JP4917541B2 (ja) | 2012-04-18 |
| US20100324287A1 (en) | 2010-12-23 |
| ES2373451T3 (es) | 2012-02-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B25D | Requested change of name of applicant approved |
Owner name: MERCK SHARP AND DOHME CORP. (US) Free format text: NOME ALTERADO DE: MERCK AND CO., INC. |
|
| B25A | Requested transfer of rights approved |
Owner name: SCHERING CORPORATION, (US) |
|
| B25D | Requested change of name of applicant approved |
Owner name: MERCK SHARP AND DOHME CORP. (US) |
|
| B25G | Requested change of headquarter approved |
Owner name: MERCK SHARP AND DOHME CORP. (US) |
|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] | ||
| B15K | Others concerning applications: alteration of classification |
Ipc: A61K 31/675 (2006.01), A61P 29/00 (2006.01), C07F |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |