ME02401B - Postupci za proizvodnju farmaceutski aktivnog agensa - Google Patents

Postupci za proizvodnju farmaceutski aktivnog agensa

Info

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
Application number
MEP-2016-105A
Other languages
German (de)
English (en)
French (fr)
Inventor
Frans Therkelsen
Michael Harold Rock
Svend Treppendahl
Original Assignee
H Lundbeck As
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 H Lundbeck As filed Critical H Lundbeck As
Publication of ME02401B publication Critical patent/ME02401B/me

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.
MEP-2016-105A 2009-12-23 2010-12-20 Postupci za proizvodnju farmaceutski aktivnog agensa ME02401B (me)

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) CN103694161B (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)

* Cited by examiner, † Cited by third party
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
MA41148A (fr) * 2014-12-12 2017-10-17 H Lundbeck As Procédé de fabrication d'idalopirdine
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
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
AU2019412747B8 (en) * 2018-12-27 2025-04-24 F. Hoffmann-La Roche Ag Process for the preparation exo-tert-butyl N-(3-azabicyclo[3.2.1]octan-8-yl)carbamate

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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
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TW201139370A (en) 2009-12-23 2011-11-16 Lundbeck & Co As H Processes for the manufacture of a pharmaceutically active agent

Also Published As

Publication number Publication date
HUE028806T2 (en) 2017-01-30
UA111584C2 (uk) 2016-05-25
AU2010335659A1 (en) 2012-07-05
KR101796330B1 (ko) 2017-11-09
EA201290552A1 (ru) 2012-12-28
JP6195605B2 (ja) 2017-09-13
KR101873182B1 (ko) 2018-06-29
US20110152539A1 (en) 2011-06-23
JP2016117734A (ja) 2016-06-30
KR20120112480A (ko) 2012-10-11
SI2516394T1 (sl) 2016-07-29
US8901318B2 (en) 2014-12-02
EP2516394A2 (en) 2012-10-31
US8461353B2 (en) 2013-06-11
MY159251A (en) 2016-12-30
JP2013515683A (ja) 2013-05-09
AU2010335659B2 (en) 2015-05-21
GEP20146078B (en) 2014-04-10
ZA201305936B (en) 2015-09-30
CN102656146A (zh) 2012-09-05
CR20120316A (es) 2012-08-16
IL220329A0 (en) 2012-08-30
IL231141A (en) 2016-03-31
CY1118032T1 (el) 2017-05-17
MX2012007078A (es) 2012-07-20
CN103694161A (zh) 2014-04-02
CL2012001725A1 (es) 2012-11-30
PH12012501258A1 (en) 2013-02-04
DOP2012000170A (es) 2012-08-31
US20130245281A1 (en) 2013-09-19
CA2785440A1 (en) 2011-06-30
SMT201600166B (it) 2016-07-01
HK1174921A1 (en) 2013-06-21
AR079580A1 (es) 2012-02-01
EA021440B1 (ru) 2015-06-30
ES2575666T3 (es) 2016-06-30
BR112012015749A2 (pt) 2015-09-15
JP5864435B2 (ja) 2016-02-17
CN102656146B (zh) 2014-12-17
IL220329A (en) 2016-03-31
RS54820B1 (sr) 2016-10-31
NZ600639A (en) 2014-07-25
PL2516394T3 (pl) 2016-09-30
DK2516394T3 (en) 2016-06-13
TW201139370A (en) 2011-11-16
HRP20160518T1 (hr) 2016-06-03
US20150080584A1 (en) 2015-03-19
CA2785440C (en) 2018-05-01
NZ625798A (en) 2014-10-31
MA33945B1 (fr) 2013-01-02
EP2516394B1 (en) 2016-03-16
WO2011076212A2 (en) 2011-06-30
IL231141A0 (en) 2014-03-31
TN2012000279A1 (en) 2013-12-12
US9382205B2 (en) 2016-07-05
SG181910A1 (en) 2012-08-30
PT2516394E (pt) 2016-06-07
WO2011076212A3 (en) 2011-08-11
KR20170125417A (ko) 2017-11-14
CN103694161B (zh) 2015-09-09
HK1196352A1 (en) 2014-12-12

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