ME02401B - Postupci za proizvodnju farmaceutski aktivnog agensa - Google Patents
Postupci za proizvodnju farmaceutski aktivnog agensaInfo
- Publication number
- ME02401B ME02401B MEP-2016-105A MEP10516A ME02401B ME 02401 B ME02401 B ME 02401B ME P10516 A MEP10516 A ME P10516A ME 02401 B ME02401 B ME 02401B
- Authority
- ME
- Montenegro
- Prior art keywords
- process according
- formula
- compound
- alcoholic solvent
- rani
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
- C07D209/16—Tryptamines
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Indole Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Cephalosporin Compounds (AREA)
Claims (14)
1.Postupak za pripremanje jedinjenja formule IV, koji obuhvata sledeće faze: (a)mešanje (6-fluoro-lH-indol-3-il)acetonitrila, NH3 u vodi i katalizatora na bazi prelaznog metala u alkoholnom rastvaraču; i (b)hidrogenovanje smeše sa H2.
2.Postupak prema zahtevu 1,u kojem je katalizator na bazi prelaznog metala RaNi.
3.Postupak prema zahtevu 1,u kojem je alkoholni rastvarač metanol.
4.Postupak prema bilo kom od zahteva 1-3, u kojem se hidrogenovanje izvodi pod pritiskom od 250000 Paskala (2,5 bara) tokom 16 sati.
5.Postupak prema bilo kom od zahteva 1-4, u kojem se hidrogenovanje izvodi na temperaturi od 55°C do 65°C.
6.Postupak prema zahtevu 2, u kojem je korišćeni RaNi sunđerasti katalizator na bazi metala.
7. Postupak prema zahtevu 2 ili 6, u kojem nominalni sadržaj aluminijuma u RaNi iznosi 5%, a srednja veličina čestica za RaNi je 33 mikrona.
8.Postupak prema bilo kom od zahteva 1-7, u kojem je NH3 prisutan u vodenom rastvoru u koncentraciji od 25%.
9.Postupak prema bilo kom od prethodnih zahteva, koji dalje obuhvata prečišćavanje jedinjenja formule IV, gde prečišćavanje obuhvata: (a)rastvaranje jedinjenja formule IV u alkoholnom rastvaraču; (b)dodavanje rastvora L(+)-vinske kiseline; i (c)hvatanje soli vinske kiseline kao talog.
10.Postupak prema zahtevu 9, u kojem je alkoholni rastvarač metanol.
11.Postupak prema zahtevu 9 ili 10, u kome se etil acetat koristi sa alkoholnim rastvaračem.
12.Postupak prema bilo kom od prethodnih zahteva, koji dalje obuhvata reakciju jedinjenja formule IV kako bi se nagradilo jedinjenje formule I, kuplovanjem amina sa 3-(2,2,3,3-tetrafluoropropoksijbenzaldehidom u prisustvu rastvarača, praćeno redukcijom imino veze redukcionim agensom
13.Postupak prema zahtevu 12, u kojem je redukcioni agens natrijum borhidrid.
14.Postupak prema zahtevu 12 ili 13, koji dalje obuhvata prevođenje jedinjenja formule I u so HCI dodavanjem HCI, opciono praćeno prečišćavanjem rezultujuće soli.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28953009P | 2009-12-23 | 2009-12-23 | |
| EP10803222.8A EP2516394B1 (en) | 2009-12-23 | 2010-12-20 | Processes for the manufacture of a pharmaceutically active agent |
| PCT/DK2010/050348 WO2011076212A2 (en) | 2009-12-23 | 2010-12-20 | Processes for the manufacture of a pharmaceutically active agent |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02401B true ME02401B (me) | 2016-09-20 |
Family
ID=43567689
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2016-105A ME02401B (me) | 2009-12-23 | 2010-12-20 | Postupci za proizvodnju farmaceutski aktivnog agensa |
Country Status (37)
| Country | Link |
|---|---|
| US (3) | US8461353B2 (me) |
| EP (1) | EP2516394B1 (me) |
| JP (2) | JP5864435B2 (me) |
| KR (2) | KR101796330B1 (me) |
| CN (2) | CN102656146B (me) |
| AR (1) | AR079580A1 (me) |
| AU (1) | AU2010335659B2 (me) |
| BR (1) | BR112012015749A2 (me) |
| CA (1) | CA2785440C (me) |
| CL (1) | CL2012001725A1 (me) |
| CR (1) | CR20120316A (me) |
| CY (1) | CY1118032T1 (me) |
| DK (1) | DK2516394T3 (me) |
| DO (1) | DOP2012000170A (me) |
| EA (1) | EA021440B1 (me) |
| ES (1) | ES2575666T3 (me) |
| GE (1) | GEP20146078B (me) |
| HR (1) | HRP20160518T1 (me) |
| HU (1) | HUE028806T2 (me) |
| IL (2) | IL220329A (me) |
| MA (1) | MA33945B1 (me) |
| ME (1) | ME02401B (me) |
| MX (1) | MX2012007078A (me) |
| MY (1) | MY159251A (me) |
| NZ (2) | NZ625798A (me) |
| PH (1) | PH12012501258A1 (me) |
| PL (1) | PL2516394T3 (me) |
| PT (1) | PT2516394E (me) |
| RS (1) | RS54820B1 (me) |
| SG (1) | SG181910A1 (me) |
| SI (1) | SI2516394T1 (me) |
| SM (1) | SMT201600166B (me) |
| TN (1) | TN2012000279A1 (me) |
| TW (1) | TW201139370A (me) |
| UA (1) | UA111584C2 (me) |
| WO (1) | WO2011076212A2 (me) |
| ZA (1) | ZA201305936B (me) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201139370A (en) | 2009-12-23 | 2011-11-16 | Lundbeck & Co As H | Processes for the manufacture of a pharmaceutically active agent |
| JO3459B1 (ar) | 2012-09-09 | 2020-07-05 | H Lundbeck As | تركيبات صيدلانية لعلاج مرض الزهايمر |
| JO3639B1 (ar) * | 2014-07-04 | 2020-08-27 | H Lundbeck As | صورة متعددة الشكل جديدة لـ n-[2-(6-فلورو-1h-إندول-3-يل)إيثيل]-3-(2،2،3،3-تترا فلورو بروبوكسي)بنزيل أمين هيدروكلوريد |
| CN104130174A (zh) * | 2014-07-30 | 2014-11-05 | 天津市斯芬克司药物研发有限公司 | 一种吲唑衍生物及其制备方法 |
| CN105175307A (zh) * | 2014-11-18 | 2015-12-23 | 苏州晶云药物科技有限公司 | Lu AE58054的盐酸盐晶型A及其制备方法和用途 |
| TW201630881A (zh) | 2014-12-12 | 2016-09-01 | Ｈ 朗德貝克公司 | 用於生產艾達魯吡啶之方法 |
| MA41148A (fr) * | 2014-12-12 | 2017-10-17 | H Lundbeck As | Procédé de fabrication d'idalopirdine |
| CN104529865B (zh) * | 2014-12-12 | 2017-02-01 | 广东东阳光药业有限公司 | 苄胺类衍生物及其在药物上的应用 |
| CN108271369A (zh) * | 2015-10-23 | 2018-07-10 | 法尔玛赞公司 | 用于制备色胺及其衍生物的新工艺 |
| EP3440055B1 (en) * | 2016-04-08 | 2020-03-11 | H. Lundbeck A/S | A process for the manufacture of idalopirdine via hydrogenation of an imine |
| EP3333154A1 (en) | 2016-12-07 | 2018-06-13 | Sandoz Ag | Crystalline form of a selective 5-ht6 receptor antagonist |
| US12275709B2 (en) | 2018-12-27 | 2025-04-15 | Hoffmann-La Roche Inc. | Process for the preparation of exo-tert-butyl N-(3-azabicyclo[3.2.1]octan-8-yl)carbamate |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3042685A (en) | 1962-07-03 | Process of making g-fluoro tryptamine | ||
| GB846675A (en) * | 1958-04-18 | 1960-08-31 | Lab Francais Chimiotherapie | Process for the production of a tryptamine derivative |
| US4803218A (en) * | 1982-09-29 | 1989-02-07 | Mcneilab, Inc. | 3-aminoalkyl-1H-indole-5-urea and amide derivatives |
| JP2851439B2 (ja) | 1993-12-28 | 1999-01-27 | ローヌープーラン シミ | ニトリルを水素化してアミンにするための触媒の調製方法及びこの触媒の水素化における用途 |
| CN1075806C (zh) | 1993-12-28 | 2001-12-05 | 罗纳布朗克化学公司 | 在掺杂阮内镍型催化剂存在下腈催化加氢生成胺的方法 |
| US5869653A (en) | 1997-10-30 | 1999-02-09 | Air Products And Chemicals, Inc. | Hydrogenation of nitriles to produce amines |
| DE69815062T2 (de) | 1997-10-31 | 2004-02-26 | Koninklijke Philips Electronics N.V. | Verfahren und gerät zur audiorepräsentation von nach dem lpc prinzip kodierter sprache durch hinzufügen von rauschsignalen |
| US6156694A (en) | 1998-11-05 | 2000-12-05 | E. I. Dupont De Nemours & Company | Raney cobalt catalyst and a process for hydrogenating organic compounds using said catalyst |
| IL157651A0 (en) * | 2001-03-29 | 2004-03-28 | Lilly Co Eli | N-(2-arylethyl) benzylamines as antagonists of the 5-ht6 receptor |
| US7084154B2 (en) * | 2003-02-11 | 2006-08-01 | Pharmacopeia Drug Disclovery, Inc. | 2-(aminomethyl) arylamide analgesics |
| FR2866335B1 (fr) | 2004-02-13 | 2006-05-26 | Servier Lab | Nouveau procede de synthese de l'agomelatine |
| JP2006169113A (ja) * | 2004-12-10 | 2006-06-29 | Dainippon Sumitomo Pharma Co Ltd | インドール類の合成方法および合成中間体 |
| JP5420908B2 (ja) | 2005-12-15 | 2014-02-19 | エグゼリクシス， インコーポレイテッド | 医薬的薬剤としてのアゼピノインドール誘導体 |
| EP2002834A1 (de) * | 2007-06-13 | 2008-12-17 | Bayer Schering Pharma Aktiengesellschaft | Aryl/Hetarylamide als Modulatoren des EP2-Rezeptors |
| JO2704B1 (en) * | 2007-09-21 | 2013-03-03 | جانسين فارماسوتيكا ان في | Interference inhibition factors between MD2 and B53 |
| AU2008345225A1 (en) | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| WO2010036362A1 (en) * | 2008-09-26 | 2010-04-01 | Wyeth | 1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate nuclear receptor inhibitors |
| CN101531624A (zh) * | 2009-04-08 | 2009-09-16 | 大连凯飞精细化工有限公司 | 6-氟吲哚-3-乙腈的合成方法 |
| TW201139370A (en) | 2009-12-23 | 2011-11-16 | Lundbeck & Co As H | Processes for the manufacture of a pharmaceutically active agent |
-
2010
- 2010-12-16 TW TW099144129A patent/TW201139370A/zh unknown
- 2010-12-20 PT PT108032228T patent/PT2516394E/pt unknown
- 2010-12-20 KR KR1020127016217A patent/KR101796330B1/ko not_active Expired - Fee Related
- 2010-12-20 EP EP10803222.8A patent/EP2516394B1/en active Active
- 2010-12-20 HU HUE10803222A patent/HUE028806T2/en unknown
- 2010-12-20 EA EA201290552A patent/EA021440B1/ru not_active IP Right Cessation
- 2010-12-20 MY MYPI2012002675A patent/MY159251A/en unknown
- 2010-12-20 KR KR1020177031907A patent/KR101873182B1/ko not_active Expired - Fee Related
- 2010-12-20 JP JP2012545093A patent/JP5864435B2/ja not_active Expired - Fee Related
- 2010-12-20 ME MEP-2016-105A patent/ME02401B/me unknown
- 2010-12-20 MA MA35092A patent/MA33945B1/fr unknown
- 2010-12-20 HR HRP20160518TT patent/HRP20160518T1/hr unknown
- 2010-12-20 SI SI201031191A patent/SI2516394T1/sl unknown
- 2010-12-20 DK DK10803222.8T patent/DK2516394T3/en active
- 2010-12-20 NZ NZ625798A patent/NZ625798A/en not_active IP Right Cessation
- 2010-12-20 CN CN201080058864.9A patent/CN102656146B/zh not_active Expired - Fee Related
- 2010-12-20 GE GEAP201012807A patent/GEP20146078B/en unknown
- 2010-12-20 CN CN201410004542.6A patent/CN103694161B/zh not_active Expired - Fee Related
- 2010-12-20 AU AU2010335659A patent/AU2010335659B2/en not_active Ceased
- 2010-12-20 UA UAA201207977A patent/UA111584C2/uk unknown
- 2010-12-20 MX MX2012007078A patent/MX2012007078A/es active IP Right Grant
- 2010-12-20 ES ES10803222.8T patent/ES2575666T3/es active Active
- 2010-12-20 PH PH1/2012/501258A patent/PH12012501258A1/en unknown
- 2010-12-20 RS RS20160382A patent/RS54820B1/sr unknown
- 2010-12-20 US US12/972,559 patent/US8461353B2/en not_active Expired - Fee Related
- 2010-12-20 CA CA2785440A patent/CA2785440C/en not_active Expired - Fee Related
- 2010-12-20 WO PCT/DK2010/050348 patent/WO2011076212A2/en not_active Ceased
- 2010-12-20 NZ NZ600639A patent/NZ600639A/en not_active IP Right Cessation
- 2010-12-20 SG SG2012046793A patent/SG181910A1/en unknown
- 2010-12-20 PL PL10803222.8T patent/PL2516394T3/pl unknown
- 2010-12-20 BR BR112012015749A patent/BR112012015749A2/pt active Search and Examination
- 2010-12-21 AR ARP100104826A patent/AR079580A1/es active IP Right Grant
-
2012
- 2012-05-31 TN TNP2012000279A patent/TN2012000279A1/en unknown
- 2012-06-12 IL IL220329A patent/IL220329A/en not_active IP Right Cessation
- 2012-06-12 CR CR20120316A patent/CR20120316A/es unknown
- 2012-06-18 DO DO2012000170A patent/DOP2012000170A/es unknown
- 2012-06-22 CL CL2012001725A patent/CL2012001725A1/es unknown
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2013
- 2013-05-02 US US13/875,623 patent/US8901318B2/en not_active Expired - Fee Related
- 2013-08-07 ZA ZA2013/05936A patent/ZA201305936B/en unknown
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2014
- 2014-02-25 IL IL231141A patent/IL231141A/en not_active IP Right Cessation
- 2014-11-25 US US14/553,029 patent/US9382205B2/en not_active Expired - Fee Related
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2015
- 2015-12-24 JP JP2015251874A patent/JP6195605B2/ja not_active Expired - Fee Related
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2016
- 2016-06-02 CY CY20161100488T patent/CY1118032T1/el unknown
- 2016-06-10 SM SM201600166T patent/SMT201600166B/it unknown
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