HRP20191431T1 - Postupak za pripravu (4s)-4-(4-cijano-2-metoksifenil)-5-etoksi-2,8-dimetil-1,4-dihidro-1-6- naftiridin-3-karboksamida i njegovo pročišćavanje za uporabu kao aktivni farmaceutski pripravak - Google Patents
Postupak za pripravu (4s)-4-(4-cijano-2-metoksifenil)-5-etoksi-2,8-dimetil-1,4-dihidro-1-6- naftiridin-3-karboksamida i njegovo pročišćavanje za uporabu kao aktivni farmaceutski pripravak Download PDFInfo
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- HRP20191431T1 HRP20191431T1 HRP20191431T HRP20191431T1 HR P20191431 T1 HRP20191431 T1 HR P20191431T1 HR P20191431 T HRP20191431 T HR P20191431T HR P20191431 T1 HRP20191431 T1 HR P20191431T1
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- Prior art keywords
- formula
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- 238000000034 method Methods 0.000 title claims 11
- 238000002360 preparation method Methods 0.000 title claims 11
- 239000008186 active pharmaceutical agent Substances 0.000 title 1
- 238000000746 purification Methods 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 43
- 150000002905 orthoesters Chemical class 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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Claims (12)
1. Postupak za pripravu spoja s formulom (I)
naznačen time što se racemski spoj s formulom (XIII) razdvaja na njegove enantiomere, i spoj s formulom (XIII)
se pripravlja reakcijom spoja s formulom (XVIII)
s ortoesterom (XX)
gdje R može biti H ili metil, i spoj s formulom (XVIII)
se pripravlja reakcijom spojeva s formulom (XVI a,b)
sa spojem s formulom (IX)
i
spoj s formulom (XVI a,b) se pripravlja reakcijom spoja s formulom (VI)
sa spojem s formulom (XVII)
2. Postupak za pripravu spoja s formulom (I)
naznačen time što se racemski spoj s formulom (XIII) razdvaja na njegove enantiomere, gdje se spoj s formulom (XIII)
pripravlja reakcijom spoja s formulom (XVIII)
s ortoesterom (XX)
gdje R može biti H ili metil, i
spoj s formulom (XVIII)
se pripravlja reakcijom spojeva s formulom (XVI a,b)
sa spojem s formulom (IX)
3. Postupak za pripravu spoja s formulom (I)
naznačen time što se racemski spoj s formulom (XIII) razdvaja na njegove enantiomere, gdje se spoj s formulom (XIII)
pripravlja reakcijom spoja s formulom (XVIII)
s ortoesterom (XX)
gdje R može biti H ili metil.
4. Postupak za pripravu spoja s formulom (I)
uporabom spoja s formulom (XVIII)
5. Postupak za pripravu spoja s formulom (I)
uporabom spojeva s formulom (XVI a,b)
6. Postupak za pripravu spoja s formulom (I)
uporabom spoja s formulom (XVIII)
i
spojeva s formulom (XVI a,b)
7. Spoj s formulom
i soli, solvati i solvati njihovih soli.
8. Spoj s formulom (XVI, a+b) kao E/Z smjesa
i soli, solvati i solvati njihovih soli.
9. Postupak za pripravu spoja s formulom (XVIII)
naznačen time što spojevi s formulom (XVI a,b)
reagiraju sa spojem s formulom (IX)
10. Postupak za pripravu spojeva s formulom (XVI a,b)
naznačen time što spoj s formulom (VI)
reagira sa spojem s formulom (XVII)
11. Postupak za pripravu spoja (XIII)
naznačen time što spoj s formulom (XVIII)
reagira s ortoesterom (XX)
gdje R može biti H ili metil.
12. Postupak za pripravu spoja s formulom (XIII)
naznačen time što spoj s formulom (XVIII)
reagira s ortoesterom (XX)
gdje R može biti H ili metil, i
naznačen time što se spoj s formulom (XVIII) pripravlja reakcijom spojeva s formulom (XVI a,b)
sa spojem s formulom (IX)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15182043 | 2015-08-21 | ||
| EP16753388.4A EP3337800B1 (de) | 2015-08-21 | 2016-08-18 | Verfahren zur herstellung von (4s)- 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridin-3-carboxamid und dessen aufreinigung für die verwendung als pharmazeutischer wirkstoff |
| PCT/EP2016/069558 WO2017032673A1 (de) | 2015-08-21 | 2016-08-18 | Verfahren zur herstellung von (4s)- 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridin-3-carboxamid und dessen aufreinigung für die verwendung als pharmazeutischer wirkstoff |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20191431T1 true HRP20191431T1 (hr) | 2019-11-01 |
Family
ID=53938271
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20191431 HRP20191431T1 (hr) | 2015-08-21 | 2019-08-07 | Postupak za pripravu (4s)-4-(4-cijano-2-metoksifenil)-5-etoksi-2,8-dimetil-1,4-dihidro-1-6- naftiridin-3-karboksamida i njegovo pročišćavanje za uporabu kao aktivni farmaceutski pripravak |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | USRE49826E1 (hr) |
| EP (1) | EP3337800B1 (hr) |
| JP (1) | JP6824247B2 (hr) |
| KR (1) | KR102669559B1 (hr) |
| CN (1) | CN107849043B (hr) |
| AR (1) | AR105774A1 (hr) |
| AU (1) | AU2016312904C1 (hr) |
| CA (1) | CA2995905A1 (hr) |
| CL (1) | CL2018000427A1 (hr) |
| CO (1) | CO2018001466A2 (hr) |
| DK (1) | DK3337800T3 (hr) |
| ES (1) | ES2739904T3 (hr) |
| HK (1) | HK1251565A1 (hr) |
| HR (1) | HRP20191431T1 (hr) |
| HU (1) | HUE044574T2 (hr) |
| IL (1) | IL257371B (hr) |
| JO (1) | JOP20160186B1 (hr) |
| LT (1) | LT3337800T (hr) |
| MX (1) | MX367960B (hr) |
| MY (1) | MY195226A (hr) |
| PE (1) | PE20180554A1 (hr) |
| PL (1) | PL3337800T3 (hr) |
| PT (1) | PT3337800T (hr) |
| RS (1) | RS59055B1 (hr) |
| RU (1) | RU2743429C2 (hr) |
| SG (1) | SG11201801110TA (hr) |
| SI (1) | SI3337800T1 (hr) |
| TW (1) | TWI725045B (hr) |
| UY (1) | UY36864A (hr) |
| WO (1) | WO2017032673A1 (hr) |
| ZA (1) | ZA201801859B (hr) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110317265B (zh) * | 2018-03-28 | 2023-03-10 | 江苏豪森药业集团有限公司 | 比伐芦定晶型a及其制备方法 |
| EP3560922A1 (de) * | 2018-04-24 | 2019-10-30 | Bayer Aktiengesellschaft | Verfahren zur herstellung von (4s)- 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridin-3-carbox-amid durch racemat-spaltung mittels diastereomerer weinsäureester |
| EP3566704A1 (en) | 2018-05-11 | 2019-11-13 | Bayer Aktiengesellschaft | The use of non-steroidal mineralocorticoid receptor antagonists alone or in combination for the treatment of muscular or neuromuscular diseases |
| CA3157823A1 (en) * | 2019-10-17 | 2021-04-22 | Bayer Aktiengesellschaft | Process for producing acyloxymethyl esters of (4s)-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridin-3-carboxylic acid |
| CN115340539B (zh) | 2022-01-19 | 2024-02-27 | 奥锐特药业股份有限公司 | 制备非奈利酮及其中间体的方法 |
| CN114524812A (zh) * | 2022-03-18 | 2022-05-24 | 湖南凯铂生物药业有限公司 | 1,4-二氢-1,6-萘啶化合物的晶型制备以及合成方法 |
| WO2023205164A1 (en) | 2022-04-18 | 2023-10-26 | Teva Pharmaceuticals International Gmbh | Processes for the preparation of finerenone |
| WO2024075139A1 (en) * | 2022-10-06 | 2024-04-11 | Maithri Drugs Private Limited | A process for preparation of finerenone and intermediates thereof |
| CN116715664A (zh) * | 2023-06-12 | 2023-09-08 | 常州制药厂有限公司 | 一种非奈利酮关键中间体的制备方法 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL75987A (en) * | 1984-08-25 | 1991-07-18 | Goedecke Ag | Tri-and tetrasubstituted-1,4-dihydro-1,6-naphthyridine-3-carboxylic acid derivatives,their preparation and pharmaceutical compositions containing them |
| DE3431303A1 (de) * | 1984-08-25 | 1986-02-27 | Goedecke Ag | 1,6-naphthyridin-derivate, verfahren zu deren herstellung und deren verwendung |
| KR20010033442A (ko) * | 1997-12-22 | 2001-04-25 | 에가시라 구니오 | 신규 디하이드로피리딘 유도체 |
| DE19834044A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | Neue substituierte Pyrazolderivate |
| DE19834047A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | Substituierte Pyrazolderivate |
| DE19943639A1 (de) | 1999-09-13 | 2001-03-15 | Bayer Ag | Dicarbonsäurederivate mit neuartigen pharmazeutischen Eigenschaften |
| DE19943634A1 (de) | 1999-09-13 | 2001-04-12 | Bayer Ag | Neuartige Dicarbonsäurederivate mit pharmazeutischen Eigenschaften |
| DE19943636A1 (de) | 1999-09-13 | 2001-03-15 | Bayer Ag | Neuartige Dicarbonsäurederivate mit pharmazeutischen Eigenschaften |
| DE19943635A1 (de) | 1999-09-13 | 2001-03-15 | Bayer Ag | Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften |
| AR031176A1 (es) | 2000-11-22 | 2003-09-10 | Bayer Ag | Nuevos derivados de pirazolpiridina sustituidos con piridina |
| DE10110749A1 (de) | 2001-03-07 | 2002-09-12 | Bayer Ag | Substituierte Aminodicarbonsäurederivate |
| DE10110750A1 (de) | 2001-03-07 | 2002-09-12 | Bayer Ag | Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften |
| DE10220570A1 (de) | 2002-05-08 | 2003-11-20 | Bayer Ag | Carbamat-substituierte Pyrazolopyridine |
| US20080312209A1 (en) | 2005-07-12 | 2008-12-18 | Glaxo Group Limited | Piperazine Heteroaryl Derivatives as Gpr38 Agonists |
| DE102006026583A1 (de) * | 2006-06-07 | 2007-12-13 | Bayer Healthcare Aktiengesellschaft | Aryl-substituierte hetero-bicyclische Verbindungen und ihre Verwendung |
| DE102007009494A1 (de) | 2007-02-27 | 2008-08-28 | Bayer Healthcare Ag | Substituierte 4-Aryl-1, 4-dihydro-1,6-naphthyridinamide und ihre Verwendung |
| PE20170141A1 (es) | 2014-08-01 | 2017-04-02 | Bayer Pharma AG | Procedimiento para la preparacion de (4s)-4-(4-ciano-2-metoxifenil)-5-etoxi-2,8-dimetil-1,4-dihidro-1,6-naftiridin-3-carbox-amida y su purificacion para su uso como principio activo farmaceutico |
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