HRP20161135T1 - Oblici u krutom stanju n-((s)-2,3-dihidroksi-propil)-3-(2-fluoro-4-jodo-fenilamino)-izonikotinamida - Google Patents
Oblici u krutom stanju n-((s)-2,3-dihidroksi-propil)-3-(2-fluoro-4-jodo-fenilamino)-izonikotinamida Download PDFInfo
- Publication number
- HRP20161135T1 HRP20161135T1 HRP20161135TT HRP20161135T HRP20161135T1 HR P20161135 T1 HRP20161135 T1 HR P20161135T1 HR P20161135T T HRP20161135T T HR P20161135TT HR P20161135 T HRP20161135 T HR P20161135T HR P20161135 T1 HRP20161135 T1 HR P20161135T1
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- Prior art keywords
- solid state
- degrees
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- solid
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- 239000007787 solid Substances 0.000 title claims 19
- 150000003839 salts Chemical class 0.000 claims 3
- VIUAUNHCRHHYNE-JTQLQIEISA-N N-[(2S)-2,3-dihydroxypropyl]-3-(2-fluoro-4-iodoanilino)-4-pyridinecarboxamide Chemical compound OC[C@@H](O)CNC(=O)C1=CC=NC=C1NC1=CC=C(I)C=C1F VIUAUNHCRHHYNE-JTQLQIEISA-N 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Detergent Compositions (AREA)
Claims (17)
1. Oblik u krutom stanju N-((S)-2,3-dihidroksi-propil)-3-(2-fluoro-4-jodo-fenilamino)-izonikotinamida ili njegove farmaceutski prihvatljive soli.
2. Oblik u krutom stanju prema zahtjevu 1, naznačen time da oblik u krutom stanju ili njegova farmaceutski prihvatljiva sol je u kristalnom obliku.
3. Oblik u krutom stanju prema zahtjevu 2, naznačen time da farmaceutski prihvatljiva sol je mono hidroklorid.
4. Oblik u krutom stanju prema zahtjevu 2, naznačen time da je slobodna baza od N-((S)-2,3-dihidroksi-propil)-3-(2-fluoro-4-jodo-fenilamino)-izonikotinamida.
5. Oblik u krutom stanju A1 prema zahtjevu 3, naznačen time da ima karakteristične Cu-Kα1 maksimume X-zraka kod 2θ kutova koji odgovaraju to 5.5 ± 0.2, 16.8 ± 0.2,18.5 ± 0.2, 19.1 ± 0.2, 22.6 ± 0.2, 23.0 ± 0.2, 24.9 ± 0.2, 25.2 ± 0.2, 28.4 ± 0.2, 29.2 ± 0.2 stupnjeva.
6. Oblik u krutom stanju A1 prema zahtjevu 3, naznačen time da ima karakteristične Cu-Kα1 X maksimume X-zraka kod 2θ kutova koji odgovaraju jednom ili više od slijedećih popisa maksimuma:
a) 5.5 ± 0.2, 16.8 ± 0.2, 19.5 ± 0.2, 23.0 ± 0.2 stupnjeva;
b) 5.5 ± 0.2,18.5 ± 0.2, 19.1 ± 0.2, 28.4 ± 0.2, 29.6 ± 0.2 stupnjeva;
c) 15.9 ± 0.2, 19.1 ± 0.2, 24.9 ± 0.2 stupnjeva.
7. Oblik u krutom stanju A1 prema zahtjevu 3, naznačen time da ima prostornu skupinu P21 s parametrima rešetke a = 9.6 ±0.1 Å, b= 11.2 ± 0.1 Å, c = 16.6 ±0.1 Å, i β = 104.4 ± 0.5 ° (α = γ = 90°) kada se mjeri kod 301 K.
8. Oblik u krutom stanju A2 prema zahtjevu 3, naznačen time da ima karakteristične Cu-Kα1 maksimume X-zraka kod 2θ kutova koji odgovaraju to 5.4 ± 0.2, 9.6 ± 0.2, 18.4 ± 0.2, 18.6 ± 0.2, 20.9 ± 0.2, 21.6 ± 0.2, 23.9 ± 0.2, 24.4 ± 0.2, 25.0 ± 0.2, 26.0 ± 0.2 stupnjeva.
9. Oblik u krutom stanju A2 prema zahtjevu 3, naznačen time da ima karakteristične Cu-Kα1 maksimume X-zraka kod 2θ kutova koji odgovaraju jednom ili više od slijedećih popisa maksimuma:
a) 18.4 ± 0.2, 18.6 ± 0.2, 19.2 ± 0.2, 20.2 ± 0.2,21.6 ± 0.2 stupnjeva;
b) 9.6 ± 0.2, 11.3 ± 0.2, 17.8 ± 0.2, 23.9 ± 0.2, 25.0 ± 0.2 stupnjeva.
10. Oblik u krutom stanju A2 prema zahtjevu 3, naznačen time da ima prostornu skupinu P21212 s parametrima rešetke a = 32.3 ± 0.1 A, b = 11.2 ± 0.1 Å, c = 4.8 ± 0.1 Å, uz α = β = γ = 90°, kada se mjeri kod 301 K.
11. Oblik u krutom stanju B1 prema zahtjevu 4, naznačen time da ima karakteristične Cu-Kα1 maksimume X-zraka kod 2θ kutova koji odgovaraju 7.0 ± 0.2, 14.0 ± 0.2, 18.3 ± 0.2, 19.0 ± 0.2, 20.6 ± 0.2, 21.2 ± 0.2, 24.2 ± 0.2, 25.1 ± 0.2, 25.4 ± 0.2, 27.9 ± 0.2 stupnjeva.
12. Oblik u krutom stanju B1 prema zahtjevu 4, naznačen time da ima prostornu skupinu P212121 s parametrima rešetke a = 20.8 ± 0.1 Å, b = 15.7 ± 0.1 Å, c = 5.0 ± 0.1 Å (α = β = γ = 90°) kada se mjeri kod 301 K.
13. Oblik u krutom stanju B2 prema zahtjevu 4, naznačen time da ima karakteristične Cu-Kα1 maksimume X-zraka kod 2θ kutova koji odgovaraju 8.7 ± 0.2, 15.9 ± 0.2, 17.4 ± 0.2, 18.2 ± 0.2, 18.8 ± 0.2, 19.2 ± 0.2, 21.3 ± 0.2, 22.3 ± 0.2, 23.3 ± 0.2, 26.0 ± 0.2 stupnjeva.
14. Oblik u krutom stanju B2 prema zahtjevu 4, naznačen time da ima prostornu skupinu P1 s parametrima rešetke a = 11.7 ±0.1 A, b = 15.7 ± 0.1 A, c = 4.8 ±0.1 Å, α = 92.2 ± 0.5 °, β = 101.3 ± 0.5 °, y = 102.9 ± 0.5 ° kada se mjeri kod 301 K.
15. Oblik u krutom stanju prema jednom ili više od zahtjeva 1 do 14, naznačen time da je lijek.
16. Oblik u krutom stanju prema jednom ili više od zahtjeva 1 do 14, naznačen time da je za uporabu za liječenje raka.
17. Farmaceutski pripravak naznačen time da kao aktivnu tvar sadrži oblik u krutom stanju prema jednom ili više od zahtjeva 1 do 14, zajedno s barem jednim farmaceutski prihvatljivim nosačem.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261653037P | 2012-05-30 | 2012-05-30 | |
| EP13725913.1A EP2855434B1 (en) | 2012-05-30 | 2013-05-07 | Solid state forms of n-((s)-2,3-dihydroxy-propyl)-3-(2-fluoro-4-iodo-phenylamino)-isonicotinamide |
| PCT/EP2013/001352 WO2013178320A1 (en) | 2012-05-30 | 2013-05-07 | Solid state forms of n-((s)-2,3-dihydroxy-propyl)-3-(2-fluoro-4-iodo-phenylamino)-isonicotinamide |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20161135T1 true HRP20161135T1 (hr) | 2016-11-04 |
Family
ID=48537929
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20161135TT HRP20161135T1 (hr) | 2012-05-30 | 2016-09-05 | Oblici u krutom stanju n-((s)-2,3-dihidroksi-propil)-3-(2-fluoro-4-jodo-fenilamino)-izonikotinamida |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US9260393B2 (hr) |
| EP (1) | EP2855434B1 (hr) |
| JP (1) | JP6280543B2 (hr) |
| KR (1) | KR20150022923A (hr) |
| CN (1) | CN104334530A (hr) |
| AR (1) | AR091186A1 (hr) |
| AU (1) | AU2013269994B2 (hr) |
| BR (1) | BR112014029838A2 (hr) |
| CA (1) | CA2875145C (hr) |
| CL (1) | CL2014003285A1 (hr) |
| DK (1) | DK2855434T3 (hr) |
| EA (1) | EA028059B1 (hr) |
| ES (1) | ES2592860T3 (hr) |
| HK (1) | HK1206733A1 (hr) |
| HR (1) | HRP20161135T1 (hr) |
| HU (1) | HUE028850T2 (hr) |
| IL (1) | IL235947A (hr) |
| LT (1) | LT2855434T (hr) |
| MX (1) | MX350295B (hr) |
| MY (1) | MY169266A (hr) |
| NZ (1) | NZ701103A (hr) |
| PL (1) | PL2855434T3 (hr) |
| PT (1) | PT2855434T (hr) |
| RS (1) | RS55167B1 (hr) |
| SG (1) | SG11201407842TA (hr) |
| SI (1) | SI2855434T1 (hr) |
| TW (1) | TWI570108B (hr) |
| UA (1) | UA112899C2 (hr) |
| WO (1) | WO2013178320A1 (hr) |
| ZA (1) | ZA201409426B (hr) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015127234A1 (en) * | 2014-02-20 | 2015-08-27 | Board Of Regents, The University Of Texas System | Use of ibrutinib to treat egfr mutant cancer |
| KR20160138756A (ko) * | 2015-05-26 | 2016-12-06 | 연세대학교 산학협력단 | 신경줄기세포로부터 도파민 신경세포로의 분화 유도용 조성물 및 이를 이용하여 신경줄기세포로부터 도파민 신경세포로 분화시키는 방법 |
| US10179132B2 (en) | 2015-05-26 | 2019-01-15 | Industry-Academic Cooperation Foundation, Yonsei University | Composition for inducing differentiation of multipotent neural stem cells into dopaminergic neurons and method for inducing differentiation of multipotent neural stem cells into dopaminergic neurons by using the same |
| JP6663509B2 (ja) | 2016-11-25 | 2020-03-11 | ジェヌーヴ インク． | 神経幹細胞の分化促進用及び保護用の組成物、並びにそれを利用して神経再生を誘導する方法 |
| KR101833412B1 (ko) | 2017-07-24 | 2018-02-28 | 연세대학교 산학협력단 | 신경줄기세포로부터 도파민 신경세포로의 분화 유도용 조성물 및 이를 이용하여 신경줄기세포로부터 도파민 신경세포로 분화시키는 방법 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2274572T3 (es) * | 1997-07-01 | 2007-05-16 | Warner-Lambert Company Llc | Derivados de acido 2-(4-bromo- o 4-yodo-fenilamino) benzoico y su uso como inhibidor de mek. |
| HUP0105092A3 (en) * | 1999-01-13 | 2003-12-29 | Warner Lambert Co | 1-heterocycle substituted diarylamines and medicaments containing them |
| CA2482345A1 (en) * | 2002-05-31 | 2003-12-11 | Bayer Pharmaceuticals Corporation | Compounds and compositions for the treatment of diabetes and diabetes-related disorders |
| PT1802579E (pt) * | 2004-10-20 | 2014-02-17 | Merck Serono Sa | Derivados da 3-arilaminopiridina |
| CN102134218A (zh) * | 2009-06-15 | 2011-07-27 | 凯美隆(北京)药业技术有限公司 | 6-芳氨基吡啶酮磺酰胺和6-芳氨基吡嗪酮磺酰胺mek抑制剂 |
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2013
- 2013-05-07 BR BR112014029838A patent/BR112014029838A2/pt not_active Application Discontinuation
- 2013-05-07 CA CA2875145A patent/CA2875145C/en active Active
- 2013-05-07 NZ NZ701103A patent/NZ701103A/en not_active IP Right Cessation
- 2013-05-07 KR KR20147036740A patent/KR20150022923A/ko not_active Application Discontinuation
- 2013-05-07 MY MYPI2014703509A patent/MY169266A/en unknown
- 2013-05-07 CN CN201380028114.0A patent/CN104334530A/zh active Pending
- 2013-05-07 AU AU2013269994A patent/AU2013269994B2/en active Active
- 2013-05-07 SG SG11201407842TA patent/SG11201407842TA/en unknown
- 2013-05-07 HU HUE13725913A patent/HUE028850T2/en unknown
- 2013-05-07 EA EA201401341A patent/EA028059B1/ru not_active IP Right Cessation
- 2013-05-07 ES ES13725913.1T patent/ES2592860T3/es active Active
- 2013-05-07 EP EP13725913.1A patent/EP2855434B1/en active Active
- 2013-05-07 US US14/404,060 patent/US9260393B2/en active Active
- 2013-05-07 WO PCT/EP2013/001352 patent/WO2013178320A1/en active Application Filing
- 2013-05-07 PL PL13725913.1T patent/PL2855434T3/pl unknown
- 2013-05-07 RS RS20160795A patent/RS55167B1/sr unknown
- 2013-05-07 DK DK13725913.1T patent/DK2855434T3/en active
- 2013-05-07 LT LTEP13725913.1T patent/LT2855434T/lt unknown
- 2013-05-07 SI SI201330301A patent/SI2855434T1/sl unknown
- 2013-05-07 PT PT137259131T patent/PT2855434T/pt unknown
- 2013-05-07 MX MX2014014520A patent/MX350295B/es active IP Right Grant
- 2013-05-07 JP JP2015514374A patent/JP6280543B2/ja active Active
- 2013-05-29 TW TW102119003A patent/TWI570108B/zh active
- 2013-05-29 AR ARP130101864 patent/AR091186A1/es unknown
- 2013-07-05 UA UAA201413849A patent/UA112899C2/uk unknown
-
2014
- 2014-11-27 IL IL235947A patent/IL235947A/en not_active IP Right Cessation
- 2014-11-28 CL CL2014003285A patent/CL2014003285A1/es unknown
- 2014-12-19 ZA ZA2014/09426A patent/ZA201409426B/en unknown
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2015
- 2015-07-30 HK HK15107274.5A patent/HK1206733A1/xx unknown
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2016
- 2016-09-05 HR HRP20161135TT patent/HRP20161135T1/hr unknown
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