ME02407B - Soli i solvati derivata tetrahidroizohinolina - Google Patents
Soli i solvati derivata tetrahidroizohinolinaInfo
- Publication number
- ME02407B ME02407B MEP-2016-98A MEP9816A ME02407B ME 02407 B ME02407 B ME 02407B ME P9816 A MEP9816 A ME P9816A ME 02407 B ME02407 B ME 02407B
- Authority
- ME
- Montenegro
- Prior art keywords
- solvate
- degrees
- sodium salt
- crystalline
- phenylmethoxy
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
- C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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]
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (18)
1. Natrijumova so (S) -2- (difenilacetil) -1,2,3,4-tetrahidro-6-metoksi-5- (fenilmetoksi) -3- izohinolin karboksilne kiseline i njenih solvata, u amorfnom obliku ili u obliku kristalnog solvata.
2. Natrijumova so, prema patentnom zahtevu 1, naznačena time da je solvat etanolni solvat, izo-propanolni solvat ili hidrat koji ima 2 do 5 molekule vode.
3. Natrijumova so, prema patentnom zahtevu 2, naznačena time da je solvat etanolni solvat ili izo-propanolni solvat.
4. Natrijumova so, prema patentnom zahtevu 2, naznačena time da je solvat hidrat koji sadrži 2 molekula vode.
5. Natrijumova so, prema patentnom zahtevu 2, naznačena time da je solvat hidrat koji sadrži 3 do 5 molekula vode.
6. Hidrat natrijumove soli, prema patentnom zahtevu 4, naznačen time da kristalni solvat pokazuje rendgenogram rendgenske difrakcije praha koji sadrži signal/pik na 19. 3 stepeni 2θ ± 0.1 stepeni 2θ i opciono dalje sadrži signal/pik na 18.2 stepeni 2θ ± 0.1 stepeni 2θ, i opciono naznačen time kristalni solvat pokazuje 13C NMR spektar čvrstog stanja koji sadrži signale na 55.7, 128.2 i 151.3 ppm ± 0,2 ppm.
7. Hidrat natrijumove soli, prema patentnom zahtevu 5, naznačen time da kristalni solvat pokazuje rendgenogram difrakcije x-zraka na prahu koji sadrži signal/pik na 15.2 stepena 2θ ± 0.1 stepeni 2θ i opciono dalje sadrži najmanje dva signala/pika iz sledeće grupe koju čine 4.8, 7.3, 12.0, 12.6, 23.5, i 24.5 stepeni 2θ ± 0.1 stepeni 2θ i opciono pri čemu pomenuti kristalni solvat pokazuje 13C NMR spektar čvrstog stanja koji sadrži signale na 53,7, 122,9 i 128,1 ppm ± 0,2 ppm.
8. Etanolni solvat prema patentnom zahtevu 3, naznačen time da kristalni solvat pokazuje rendgenogram rendgenske difrakcije praha koji sadrži pik na 14.3 stepeni 2θ ± 0.1 stepena 2θ ili pokazuje rendgenogram difrakcije iks-zraka na prahu koji sadrži signal/pik na 14,7 stepeni 2θ ± 0.1 stepeni 2θ ili pokazuje rendgenogram koji sadrži najmanje dva signala/pika iz grupe koja sadrži 14.3, 14.7, 26.9, i 29.7 stepeni 2θ ± 0.1 stepen 2θ, i opciono gde navedeni kristalni solvat pokazuje 13C NMR spektar čvrstog stanja koji sadrži signale na 18.4, 139.7 i 141.4 ± 0,2 ppm.
9. Izo-propanolni solvat prema patentnom zahtevu 3, naznačen time da pokazuje rendgenogram difrakcije x-zraka praha koji sadrži najmanje jedan pik izabran iz grupe koja se sastoji od 20.6, 26.6, 27.2, 28.3 i 29.3 stepena 2θ ± 0.1 stepen 2θ i opciono dalje sadrži najmanje dva pika izabrana iz grupe koju čine 25.0, 26.0, 26.6, 27.2, 28.3 i 29.3 stepena 2θ ± 0.1 stepen 2θ ili dalje sadrži najmanje jedan signal izabran iz grupe koju čine signali
10.8, 14.0, 21.1, 21.9, i 22.5 stepeni 2θ ± 0.1 stepen 2θ, i opciono gde pomenuti kristalni solvat pokazuje spektar 13C NMR čvrstog stanja koji sadrži signale na 63.1 i 140.7 ppm ± 0,2 ppm. 10. Farmaceutski preparat koji sadrži natrijumovu so (S)-2-(difenilacetil)-1,2,3,4-tetrahidro-6-metoksi-5-(fenilmetoksi)-3-izohinolin karboksilne kiseline ili solvat natrijumove soli zajedno sa farmaceutski prihvatljivim nosačem, sredstvom za razblaživanje ili ekscipijentom, naznačen time da je natrijumova so (S)-2-(difenilacetil)-1,2,3,4-tetrahidro-6-metoksi-5-(fenilmetoksi)-3-izohinolin karboksilne kiseline u amorfnom obliku ili u obliku kristalnog solvata.
11. Farmaceutski preparat prema patentnom zahtevu 10, naznačen time, što je formulisan za oralnu primenu.
12. Postupak za dobijanje natrijumove soli (S)-2-(difenilacetil)-1,2,3,4-tetrahidro-6-metoksi-5-(fenilmetoksi)-3-izohinolin karboksilne kiseline ili solvata sastoji se iz: (i) tretiranja (S)-2-(difenilacetil)-1,2,3,4-tetrahidro-6-metoksi-5-(fenilmetoksi)-3-izohinolin karbonske kiseline sa natrijum-alkoksidom; (ii) građenja kristalnog alkoholnog solvata proizvedene natrijumove soli nagrađene postupkom (i); i(iii) rekristalizacije solvata.
13. Postupak prema patentnom zahtevu 12 naznačen time da je navedeni kristalni solvat etanolni solvat, izopropanolni solvat, ili hidrat koji sadrži 2 do 5 molekule vode.
14. Postupak prema patentnom zahtevu 12 naznačen time da se molekul alkohola kristalnog alkoholnog solvata formiran u koraku (ii) se menja sa drugim molekulom solvata pre, tokom ili nakon koraka (iii), naročito naznačen time da je formirani solvat hidrat.
15. Postupak prema bilo kojem od patentnih zahteva 12 ili 14 naznačen time da je solvat koji se prekristališe u koraku (iii) izo-propanolni solvat.
16. Postupak prema bilo kojem od patentnih zahteva 12 do 15, koji sadrži dalji korak sušenja solvata.
17. Postupak prema bilo kom od patentnih zahteva 12 do 15 koji dalje sadrži postupak acidifikacije natrijumove soli da bi se formirala (S)-2-(difenilacetil)-1,2,3,4-tetrahidro-6-metoksi-5-(fenilmetoksi)-3-izohinolin karboksilna kiselina u suštinski čistom obliku, naznačen time da suštinski čist oblik ukazuje na proizvod koji ima više od 96% hemijske čistoće i / ili više od 97% ee.
18. Postupak za dobijanje solvata natrijumove soli (S)-2-(difenilacetil)-1,2,3,4-tetrahidro-6-metoksi-5-(fenilmetoksi)-3-izohinolin karboksilne kiseline koji sadrži sledeće korake: (i) acilovanje izohinolinskog atoma azota (S)-1,2,3,4-tetrahidro-6-metoksi-5-(fenilmetoksi)-3-izohinolin karboksilne kiseline sa aktiviranim cikličnim amidom formule: naznačen time prsten A predstavlja 5-člani heterocikl koji sadrži azot; i(ii) tretiranje proizvoda iz faze (i) sa alkoksidnom soli u alkoholnom rastvaraču. 4
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36636710P | 2010-07-21 | 2010-07-21 | |
| PCT/GB2011/001096 WO2012010843A1 (en) | 2010-07-21 | 2011-07-21 | Salt and solvates of a tetrahydroisoquinoline derivative |
| EP11740973.0A EP2595960B1 (en) | 2010-07-21 | 2011-07-21 | Salt and solvates of a tetrahydroisoquinoline derivative |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02407B true ME02407B (me) | 2016-09-20 |
Family
ID=44386640
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2016-98A ME02407B (me) | 2010-07-21 | 2011-07-21 | Soli i solvati derivata tetrahidroizohinolina |
Country Status (20)
| Country | Link |
|---|---|
| US (3) | US8614227B2 (me) |
| EP (2) | EP2595960B1 (me) |
| JP (3) | JP5948326B2 (me) |
| CN (2) | CN105777636A (me) |
| AU (3) | AU2011281381B2 (me) |
| CA (1) | CA2803699C (me) |
| DK (1) | DK2595960T3 (me) |
| ES (1) | ES2570135T3 (me) |
| HK (1) | HK1224290A1 (me) |
| HR (1) | HRP20160540T1 (me) |
| HU (1) | HUE028620T2 (me) |
| ME (1) | ME02407B (me) |
| NZ (2) | NZ605444A (me) |
| PL (1) | PL2595960T3 (me) |
| PT (1) | PT2595960E (me) |
| RS (1) | RS54789B1 (me) |
| SI (1) | SI2595960T1 (me) |
| SM (1) | SMT201600171B (me) |
| WO (1) | WO2012010843A1 (me) |
| ZA (1) | ZA201300169B (me) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2011281381B2 (en) * | 2010-07-21 | 2015-07-16 | Novartis Ag | Salt and solvates of a tetrahydroisoquinoline derivative |
| US9320530B2 (en) * | 2013-03-13 | 2016-04-26 | The Spectranetics Corporation | Assisted cutting balloon |
| ES2883155T3 (es) * | 2013-07-08 | 2021-12-07 | Novartis Ag | Compuestos heterocíclicos y métodos para su uso |
| JP6667551B2 (ja) | 2015-01-13 | 2020-03-18 | ノバルティス アーゲー | アンジオテンシンｉｉ２型拮抗薬としてのピロリジン誘導体 |
| US10308628B2 (en) | 2015-03-12 | 2019-06-04 | Novartis Ag | Heterocyclic compounds and methods for their use |
| CN106478502B (zh) * | 2015-08-29 | 2021-04-27 | 上海翰森生物医药科技有限公司 | 1,2,3,4-四氢异喹啉衍生物、其制备方法和应用 |
| WO2018001997A1 (en) | 2016-06-27 | 2018-01-04 | Ratiopharm Gmbh | Crystalline calcium salt of (s)-2-(diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid |
| JP2019514862A (ja) * | 2017-03-23 | 2019-06-06 | ノバルティス アーゲー | （ｓ）−２−（ジフェニルアセチル）−１，２，３，４−テトラヒドロ−６−メトキシ−５−（フェニルメトキシ）−３−イソキノリンカルボン酸ナトリウムの無水結晶形 |
| PT3620454T (pt) * | 2017-06-09 | 2021-09-10 | Shandong Danhong Pharmaceutical Co Ltd | Derivado de ácido carboxílico como antagonista do recetor at2r |
| JP2021531749A (ja) | 2018-07-12 | 2021-11-25 | コデクシス， インコーポレイテッド | 操作されたフェニルアラニンアンモニアリアーゼポリペプチド |
| WO2020012266A1 (en) | 2018-07-12 | 2020-01-16 | Novartis Ag | Biocatalytic synthesis of olodanrigan (ema401) from 3-(2-(benzyloxy)-3-methoxyphenyl)propenoic acid with phenylalanine ammonia lyase |
| CN111620816B (zh) * | 2020-05-27 | 2023-06-02 | 上海赛默罗生物科技有限公司 | 螺桨烷类衍生物、其制备方法、药物组合物和用途 |
| GB202100352D0 (en) * | 2021-01-12 | 2021-02-24 | Balticgruppen Bio Ab | New methods |
| CN115901740A (zh) * | 2022-11-18 | 2023-04-04 | 南京工业大学 | 基于Pictet-Spengler反应的多巴胺检测试剂及应用、多巴胺的检测方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5246943A (en) * | 1992-05-19 | 1993-09-21 | Warner-Lambert Company | Substituted 1,2,3,4-tetahydroisoquinolines with angiotensin II receptor antagonist properties |
| US5236934A (en) | 1992-08-26 | 1993-08-17 | E. I. Du Pont De Nemours And Company | 1,2,3,4-tetrahydroisoquinolines useful in the treatment of CNS disorders |
| CA2318778A1 (en) * | 1998-02-25 | 1999-09-02 | Merck & Co., Inc. | Method for decreasing qt dispersion or inhibiting the progression of qt dispersion with an angiotensin ii receptor antagonist |
| WO2006066361A1 (en) * | 2004-12-24 | 2006-06-29 | The University Of Queensland | Method of treatment or prophylaxis |
| CA2866540A1 (en) * | 2006-03-20 | 2007-09-27 | Spinifex Pharmaceuticals Pty Ltd. | Method of treatment or prophylaxis of inflammatory pain |
| NZ601383A (en) * | 2010-01-19 | 2014-07-25 | Spinifex Pharm Pty Ltd | Methods and compositions for improved nerve conduction velocity |
| AU2011281381B2 (en) * | 2010-07-21 | 2015-07-16 | Novartis Ag | Salt and solvates of a tetrahydroisoquinoline derivative |
-
2011
- 2011-07-21 AU AU2011281381A patent/AU2011281381B2/en not_active Ceased
- 2011-07-21 SI SI201130804A patent/SI2595960T1/sl unknown
- 2011-07-21 ES ES11740973T patent/ES2570135T3/es active Active
- 2011-07-21 CN CN201610152658.3A patent/CN105777636A/zh active Pending
- 2011-07-21 US US13/187,882 patent/US8614227B2/en not_active Expired - Fee Related
- 2011-07-21 RS RS20160358A patent/RS54789B1/sr unknown
- 2011-07-21 EP EP11740973.0A patent/EP2595960B1/en active Active
- 2011-07-21 PL PL11740973.0T patent/PL2595960T3/pl unknown
- 2011-07-21 WO PCT/GB2011/001096 patent/WO2012010843A1/en not_active Ceased
- 2011-07-21 EP EP15200360.4A patent/EP3081557A1/en not_active Withdrawn
- 2011-07-21 CA CA2803699A patent/CA2803699C/en not_active Expired - Fee Related
- 2011-07-21 DK DK11740973.0T patent/DK2595960T3/en active
- 2011-07-21 NZ NZ605444A patent/NZ605444A/en not_active IP Right Cessation
- 2011-07-21 HU HUE11740973A patent/HUE028620T2/en unknown
- 2011-07-21 HR HRP20160540TT patent/HRP20160540T1/hr unknown
- 2011-07-21 ME MEP-2016-98A patent/ME02407B/me unknown
- 2011-07-21 PT PT117409730T patent/PT2595960E/pt unknown
- 2011-07-21 NZ NZ708529A patent/NZ708529A/en not_active IP Right Cessation
- 2011-07-21 JP JP2013520203A patent/JP5948326B2/ja not_active Expired - Fee Related
- 2011-07-21 CN CN201180035468.9A patent/CN103003244B/zh not_active Expired - Fee Related
-
2013
- 2013-01-08 ZA ZA2013/00169A patent/ZA201300169B/en unknown
- 2013-07-03 HK HK16112556.3A patent/HK1224290A1/en unknown
- 2013-11-18 US US14/083,391 patent/US8927575B2/en not_active Expired - Fee Related
-
2014
- 2014-12-17 US US14/573,774 patent/US9162985B2/en not_active Expired - Fee Related
-
2015
- 2015-10-06 AU AU2015238774A patent/AU2015238774A1/en not_active Abandoned
-
2016
- 2016-04-11 JP JP2016078656A patent/JP2016164178A/ja active Pending
- 2016-06-15 SM SM201600171T patent/SMT201600171B/it unknown
-
2017
- 2017-05-15 AU AU2017203236A patent/AU2017203236A1/en not_active Abandoned
- 2017-08-14 JP JP2017156436A patent/JP2017214415A/ja active Pending
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