HRP20210469T1 - Valbenazin ditosilat i njegovi polimorfi - Google Patents
Valbenazin ditosilat i njegovi polimorfi Download PDFInfo
- Publication number
- HRP20210469T1 HRP20210469T1 HRP20210469TT HRP20210469T HRP20210469T1 HR P20210469 T1 HRP20210469 T1 HR P20210469T1 HR P20210469T T HRP20210469T T HR P20210469TT HR P20210469 T HRP20210469 T HR P20210469T HR P20210469 T1 HRP20210469 T1 HR P20210469T1
- Authority
- HR
- Croatia
- Prior art keywords
- crystalline form
- form according
- relative humidity
- amorphous
- increase
- Prior art date
Links
- GEJDGVNQKABXKG-CFKGEZKQSA-N [(2r,3r,11br)-9,10-dimethoxy-3-(2-methylpropyl)-2,3,4,6,7,11b-hexahydro-1h-benzo[a]quinolizin-2-yl] (2s)-2-amino-3-methylbutanoate Chemical class C1CN2C[C@@H](CC(C)C)[C@H](OC(=O)[C@@H](N)C(C)C)C[C@@H]2C2=C1C=C(OC)C(OC)=C2 GEJDGVNQKABXKG-CFKGEZKQSA-N 0.000 title 1
- 238000000034 method Methods 0.000 claims 9
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 6
- 238000010586 diagram Methods 0.000 claims 6
- 238000000113 differential scanning calorimetry Methods 0.000 claims 6
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- 238000002411 thermogravimetry Methods 0.000 claims 6
- 238000001757 thermogravimetry curve Methods 0.000 claims 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 238000001816 cooling Methods 0.000 claims 4
- 239000002904 solvent Substances 0.000 claims 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims 3
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims 3
- 239000002002 slurry Substances 0.000 claims 3
- 206010008748 Chorea Diseases 0.000 claims 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims 2
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims 2
- 206010043118 Tardive Dyskinesia Diseases 0.000 claims 2
- 208000000323 Tourette Syndrome Diseases 0.000 claims 2
- 208000016620 Tourette disease Diseases 0.000 claims 2
- RWGFKTVRMDUZSP-UHFFFAOYSA-N cumene Chemical compound CC(C)C1=CC=CC=C1 RWGFKTVRMDUZSP-UHFFFAOYSA-N 0.000 claims 2
- 238000010438 heat treatment Methods 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- WSLDOOZREJYCGB-UHFFFAOYSA-N 1,2-Dichloroethane Chemical compound ClCCCl WSLDOOZREJYCGB-UHFFFAOYSA-N 0.000 claims 1
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims 1
- XNWFRZJHXBZDAG-UHFFFAOYSA-N 2-METHOXYETHANOL Chemical compound COCCO XNWFRZJHXBZDAG-UHFFFAOYSA-N 0.000 claims 1
- 206010058504 Ballismus Diseases 0.000 claims 1
- 239000004215 Carbon black (E152) Substances 0.000 claims 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims 1
- 208000012661 Dyskinesia Diseases 0.000 claims 1
- 208000014094 Dystonic disease Diseases 0.000 claims 1
- NTIZESTWPVYFNL-UHFFFAOYSA-N Methyl isobutyl ketone Chemical compound CC(C)CC(C)=O NTIZESTWPVYFNL-UHFFFAOYSA-N 0.000 claims 1
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 1
- 108010029485 Protein Isoforms Proteins 0.000 claims 1
- 102000001708 Protein Isoforms Human genes 0.000 claims 1
- 102000009659 Vesicular Monoamine Transport Proteins Human genes 0.000 claims 1
- 108010020033 Vesicular Monoamine Transport Proteins Proteins 0.000 claims 1
- KXKVLQRXCPHEJC-UHFFFAOYSA-N acetic acid trimethyl ester Natural products COC(C)=O KXKVLQRXCPHEJC-UHFFFAOYSA-N 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 150000008280 chlorinated hydrocarbons Chemical class 0.000 claims 1
- 208000012601 choreatic disease Diseases 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000010118 dystonia Diseases 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- WBJINCZRORDGAQ-UHFFFAOYSA-N formic acid ethyl ester Natural products CCOC=O WBJINCZRORDGAQ-UHFFFAOYSA-N 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 229930195733 hydrocarbon Natural products 0.000 claims 1
- 150000002430 hydrocarbons Chemical class 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- GJRQTCIYDGXPES-UHFFFAOYSA-N iso-butyl acetate Natural products CC(C)COC(C)=O GJRQTCIYDGXPES-UHFFFAOYSA-N 0.000 claims 1
- FGKJLKRYENPLQH-UHFFFAOYSA-M isocaproate Chemical compound CC(C)CCC([O-])=O FGKJLKRYENPLQH-UHFFFAOYSA-M 0.000 claims 1
- JMMWKPVZQRWMSS-UHFFFAOYSA-N isopropanol acetate Natural products CC(C)OC(C)=O JMMWKPVZQRWMSS-UHFFFAOYSA-N 0.000 claims 1
- 229940011051 isopropyl acetate Drugs 0.000 claims 1
- GWYFCOCPABKNJV-UHFFFAOYSA-N isovaleric acid Chemical compound CC(C)CC(O)=O GWYFCOCPABKNJV-UHFFFAOYSA-N 0.000 claims 1
- OQAGVSWESNCJJT-UHFFFAOYSA-N isovaleric acid methyl ester Natural products COC(=O)CC(C)C OQAGVSWESNCJJT-UHFFFAOYSA-N 0.000 claims 1
- 150000002576 ketones Chemical class 0.000 claims 1
- 230000000116 mitigating effect Effects 0.000 claims 1
- 150000002825 nitriles Chemical class 0.000 claims 1
- 150000002828 nitro derivatives Chemical class 0.000 claims 1
- LYGJENNIWJXYER-UHFFFAOYSA-N nitromethane Chemical compound C[N+]([O-])=O LYGJENNIWJXYER-UHFFFAOYSA-N 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
Classifications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
- C07D455/03—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
- C07D455/04—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine
- C07D455/06—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
-
- 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
- A61K31/4353—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
-
- 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
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
- C07C303/32—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
- C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (44)
1. Kristalni oblik, naznačen time, da je od spoja Formule I:
[image]
2. Kristalni oblik prema patentnom zahtjevu 1, naznačen time, da ima uzorak rendgenske difrakcije na prahu koji sadrži maksimume na 6,3, 17,9 i 19,7 stupnjeva 2θ ± 0,2θ.
3. Kristalni oblik prema patentnom zahtjevu 2, naznačen time, da ima termogram diferencijalne pretražne kalorimetrije koji sadrži endotermički slučaj s početnom temperaturom od 240°C i maksimum na 243°C.
4. Kristalni oblik prema patentnom zahtjevu 2 ili 3, naznačen time, da ima dijagram termalne gravimetrijske analize koji sadrži gubitak mase manji od 0,4% kada se zagrijava od 25°C do 140°C.
5. Kristalni oblik prema bilo kojem od patentnih zahtjeva 2 do 4, naznačen time, da je stabilan nakon izlaganja na 25°C i 60% relativnoj vlažnosti za vrijeme od 3 mjeseca.
6. Kristalni oblik prema bilo kojem od patentnih zahtjeva 2 do 5, naznačen time, da pokazuje povećanje mase od 1% kada se podvrgne porastu u relativnoj vlažnosti od 0% do 95% relativne vlažnosti.
7. Kristalni oblik prema patentnom zahtjevu 1, naznačen time, da ima uzorak rendgenske difrakcije na prahu koji sadrži maksimume na 5,7, 15,3 i 22,5 stupnjeva 2θ ± 0,2θ.
8. Kristalni oblik prema patentnom zahtjevu 7, naznačen time, da ima termogram diferencijalne pretražne kalorimetrije koji sadrži endotermički slučaj s početnom temperaturom od 143°C i maksimum na 155°C i; i jedan drugi endotermički slučaj s početnom temperaturom od 232°C i maksimum na 235°C.
9. Kristalni oblik prema patentnom zahtjevu 7 ili 8, naznačen time, da ima dijagram termalne gravimetrijske analize koji sadrži gubitak mase od 2,2% kada se zagrijava od 25°C do 140°C.
10. Kristalni oblik prema bilo kojem od patentnih zahtjeva 7 do 9, naznačen time, da pokazuje povećanje mase od 0,5% kada se podvrgne porastu u relativnoj vlažnosti od 0% do 95% relativne vlažnosti.
11. Kristalni oblik prema patentnom zahtjevu 1, naznačen time, da ima uzorak rendgenske difrakcije na prahu koji sadrži maksimume na 6,3, 18,3, 18,9, 19,8 i 20,4 stupnjeva 2θ ± 0,2θ.
12. Kristalni oblik prema patentnom zahtjevu 11, naznačen time, da ima termogram diferencijalne pretražne kalorimetrije koji sadrži endotermičke slučajeve s temperaturama od 93°C, 158°C i 230°C.
13. Kristalni oblik prema patentnom zahtjevu 11 ili 12, naznačen time, da ima dijagram termalne gravimetrijske analize koji sadrži dva gubitka mase od 2,7% i 8,86% kada se zagrijava od 25°C do 140°C.
14. Kristalni oblik prema patentnom zahtjevu 1, naznačen time, da ima uzorak rendgenske difrakcije na prahu koji sadrži maksimume na 6,2, 10,4, 17,9, 19,2, 19,9 i 20,2 stupnjeva 2θ ± 0,2θ.
15. Kristalni oblik prema patentnom zahtjevu 14, naznačen time, da ima termogram diferencijalne pretražne kalorimetrije koji sadrži endotermičke slučajeve s temperaturama od 128°C, 159°C i 237°C.
16. Kristalni oblik prema patentnom zahtjevu 14 ili 15, naznačen time, da ima dijagram termalne gravimetrijske analize koji sadrži gubitak mase od 3,3% kada se zagrijava od 25°C do 140°C.
17. Kristalni oblik prema bilo kojem od patentnih zahtjeva 14 do 16, naznačen time, da pokazuje povećanje mase od 3,4% kada se podvrgne porastu u relativnoj vlažnosti od 0% do 95% relativne vlažnosti.
18. Kristalni oblik prema patentnom zahtjevu 1, naznačen time, da ima uzorak rendgenske difrakcije na prahu koji sadrži maksimume na 6,7, 7,9, 10,7, 12,8, 17,1 i 23,7 stupnjeva 2θ ± 0,2θ.
19. Kristalni oblik prema patentnom zahtjevu 18, naznačen time, da ima termogram diferencijalne pretražne kalorimetrije koji sadrži endotermičke slučajeve s temperaturama od 113°C i 181°C.
20. Kristalni oblik prema patentnom zahtjevu 18 ili 19, naznačen time, da ima dijagram termalne gravimetrijske analize koji sadrži gubitak mase od 4,1% kada se zagrijava od 25°C do 140°C.
21. Kristalni oblik prema bilo kojem od patentnih zahtjeva 18 do 20, naznačen time, da pokazuje povećanje mase od 1% kada se podvrgne porastu u relativnoj vlažnosti od 0% do 95% relativne vlažnosti.
22. Kristalni oblik prema patentnom zahtjevu 1, naznačen time, da ima uzorak rendgenske difrakcije na prahu koji sadrži maksimume na 6,8, 8,0, 16,3 i 17,5 stupnjeva 2θ ± 0,2θ.
23. Kristalni oblik prema patentnom zahtjevu 22, naznačen time, da ima termogram diferencijalne pretražne kalorimetrije koji sadrži endotermičke slučajeve s temperaturama od 175°C i 238°C.
24. Kristalni oblik prema patentnom zahtjevu 22 ili 23, naznačen time, da ima dijagram termalne gravimetrijske analize koji sadrži gubitak mase od 1% kada se zagrijava od 25°C do 140°C.
25. Kristalni oblik prema bilo kojem od patentnih zahtjeva 22 do 24, naznačen time, da pokazuje povećanje mase od 0,5% kada se podvrgne porastu u relativnoj vlažnosti od 40% do 80% relativne vlažnosti.
26. Amorfni oblik, naznačen time, da je od spoja Formule I:
[image]
27. Farmaceutski pripravak, naznačen time, da sadrži kristalni oblik prema bilo kojem od patentnih zahtjeva 1 do 25 ili amorfni oblik prema patentnom zahtjevu 26, i farmaceutski prihvatljiv nosač.
28. Farmaceutski pripravak prema patentnom zahtjevu 27, naznačen time, da se pripravak formulira za oralnu primjenu.
29. Farmaceutski pripravak prema patentnom zahtjevu 27 ili 28, naznačen time, da se pripravak formulira kao jednostruki oblik za doziranje.
30. Kristalni oblik prema bilo kojem od patentnih zahtjeva 1 do 25 ili amorfni oblik prema patentnom zahtjevu 26, naznačen time, da je za uporabu u postupku inhibicije izooblika 2 vezikularnog monoaminskog transportera kod pojedinca.
31. Kristalni oblik prema bilo kojem od patentnih zahtjeva 1 do 25 ili amorfni oblik prema patentnom zahtjevu 26, naznačen time, da je za uporabu u postupku liječenja, prevencije, ili ublažavanja jednog ili više simptoma hiperkinetičkog poremećaja.
32. Kristalni oblik ili amorfni oblik za uporabu prema patentnom zahtjevu 31, naznačen time, da se kod hiperkinetičkog poremećaja radi o Huntingtonovoj bolesti, tardivnoj diskineziji, Touretteovom sindromu, distoniji, hemibalizmu, koreji, senilnoj koreji ili tikovima.
33. Kristalni oblik ili amorfni oblik za uporabu prema patentnom zahtjevu 31, naznačen time, da hiperkinetički poremećaj jest Huntingtonova bolest.
34. Kristalni oblik ili amorfni oblik za uporabu prema patentnom zahtjevu 31, naznačen time, da hiperkinetički poremećaj jest tardivna diskinezija.
35. Kristalni oblik ili amorfni oblik za uporabu prema patentnom zahtjevu 31, naznačen time, da hiperkinetički poremećaj jest Touretteov sindrom.
36. Kristalni oblik ili amorfni oblik za uporabu prema patentnom zahtjevu 31, naznačen time, da hiperkinetički poremećaj jesu tikovi.
37. Postupak za proizvodnju kristalnog oblika prema bilo kojem od patentnih zahtjeva 1 do 25 ili amorfnog oblika prema patentnom zahtjevu 26, naznačen time, da obuhvaća sljedeće korake:
(a) pripravljanje kašaste smjese spoja Formule I u otapalu na prvoj temperaturi; i
(b) generiranje kristalnog oblika ili amorfnog oblika pomoću hlađenja otopine na drugu temperaturu.
38. Postupak za proizvodnju kristalnog oblika prema bilo kojem od patentnih zahtjeva 1 do 25 ili amorfnog oblika prema patentnom zahtjevu 26, naznačen time, da obuhvaća sljedeće korake:
(a) pripravljanje otopine spoja Formule I u otapalu na prvoj temperaturi;
(b) formiranje kašaste smjese pomoću hlađenja otopine na drugu temperaturu; i
(c) generiranje kristalnog oblika ili amorfnog oblika putem obrade kašaste smjese kroz jedan ili više ciklusa zagrijavanja i hlađenja.
39. Postupak prema patentnom zahtjevu 38, naznačen time, da se ciklus zagrijavanja i hlađenja izvodi na temperaturi u rasponu od -50 do 120°C.
40. Postupak prema bilo kojem od patentnih zahtjeva 37 do 39, naznačen time, da prva temperatura iznosi od 20 do 200°C.
41. Postupak prema bilo kojem od patentnih zahtjeva 37 do 40, naznačen time, da druga temperatura iznosi od -100 do 100°C.
42. Postupak prema bilo kojem od patentnih zahtjeva 37 do 41, naznačen time, da nadalje obuhvaća korak izolacije kristalnog oblika ili amorfnog oblika.
43. Postupak prema bilo kojem od patentnih zahtjeva 37 do 42, naznačen time, da se otapalo odabire od: ugljikovodika, kloriranog ugljikovodika, alkohola, etera, ketona, estera, karbonata, amida, nitrila, nitro spoja, heterocikla, vode, i njihovih mješavina.
44. Postupak prema bilo kojem od patentnih zahtjeva 37 do 42, naznačen time, da se otapalo odabire od: acetonitrila, 1,2-dikloroetana, DMF, 1,4-dioksana, metanola, 2-metoksietanola, MIBK, toluena, heptana, kumena, acetona, 1-butanola, MTBE, etanola, etil acetata, etil formijata, izobutil acetata, izopropil acetata, metil acetata, nitrometana, 1-propanola, IPA, MEK, THF, vode, i njihovih mješavina.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562249074P | 2015-10-30 | 2015-10-30 | |
PCT/US2016/059306 WO2017075340A1 (en) | 2015-10-30 | 2016-10-28 | Valbenazine salts and polymorphs thereof |
EP16794479.2A EP3368534B1 (en) | 2015-10-30 | 2016-10-28 | Valbenazine ditosylate and polymorphs thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20210469T1 true HRP20210469T1 (hr) | 2021-05-14 |
Family
ID=57281297
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20240304TT HRP20240304T1 (hr) | 2015-10-30 | 2016-10-28 | Soli valbenazin dihidroklorida i njihovi polimorfi |
HRP20210469TT HRP20210469T1 (hr) | 2015-10-30 | 2021-03-22 | Valbenazin ditosilat i njegovi polimorfi |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20240304TT HRP20240304T1 (hr) | 2015-10-30 | 2016-10-28 | Soli valbenazin dihidroklorida i njihovi polimorfi |
Country Status (31)
Country | Link |
---|---|
US (4) | US10065952B2 (hr) |
EP (3) | EP3368534B1 (hr) |
JP (2) | JP7109360B2 (hr) |
KR (1) | KR20180075591A (hr) |
CN (3) | CN108473489B (hr) |
AU (1) | AU2016343633B2 (hr) |
BR (1) | BR112018008460A2 (hr) |
CA (1) | CA3002074A1 (hr) |
CL (1) | CL2018001089A1 (hr) |
CO (1) | CO2018004589A2 (hr) |
CY (1) | CY1124002T1 (hr) |
DK (2) | DK3368534T3 (hr) |
EA (1) | EA201890852A1 (hr) |
ES (1) | ES2857085T3 (hr) |
FI (1) | FI3875459T3 (hr) |
HR (2) | HRP20240304T1 (hr) |
HU (1) | HUE053872T2 (hr) |
IL (2) | IL284874B2 (hr) |
LT (2) | LT3875459T (hr) |
MA (2) | MA43116B1 (hr) |
MX (1) | MX2018005136A (hr) |
MY (1) | MY193767A (hr) |
PH (1) | PH12018500900A1 (hr) |
PL (1) | PL3368534T3 (hr) |
PT (2) | PT3368534T (hr) |
RS (2) | RS65154B1 (hr) |
SA (1) | SA518391477B1 (hr) |
SG (1) | SG11201803408PA (hr) |
SI (1) | SI3368534T1 (hr) |
TN (1) | TN2018000121A1 (hr) |
WO (1) | WO2017075340A1 (hr) |
Families Citing this family (25)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
BR112018008460A2 (pt) | 2015-10-30 | 2018-11-06 | Neurocrine Biosciences Inc | sais de valbenazina e seus polimorfos |
RS63170B1 (sr) * | 2015-12-23 | 2022-05-31 | Neurocrine Biosciences Inc | Sintetički postupak za pripremanje (s)-(2r,3r,11br)-3-izobutil-9,10-dimetoksi-2,3,4,6,7,11b-heksahidro-1h-pirido[2,1,-a]izohinolin-2-il 2-amino-3-metilbutanoat di(4-metilbenzensulfonata) |
KR20190062460A (ko) | 2016-10-06 | 2019-06-05 | 아시아 케미컬 인더스트리스 리미티드 | 발베나진의 고체상 형태 |
WO2018102673A1 (en) * | 2016-12-02 | 2018-06-07 | Neurocrine Biosciences, Inc. | Use of valbenazine for treating schizophrenia or schizoaffective disorder |
EP3568394A1 (en) | 2017-01-10 | 2019-11-20 | Sandoz AG | Crystalline valbenazine free base |
MX2019008855A (es) | 2017-01-27 | 2019-09-11 | Neurocrine Biosciences Inc | Metodos para la administracion de ciertos inhibidores del transportador de monamina vesicular 2 (vmat2). |
WO2018153632A1 (en) * | 2017-02-27 | 2018-08-30 | Sandoz Ag | Crystalline forms of valbenazine salts |
WO2018200605A1 (en) * | 2017-04-26 | 2018-11-01 | Neurocrine Biosciences, Inc. | Use of valbenazine for treating levodopa-induced dyskinesia |
EP3684333A2 (en) | 2017-09-21 | 2020-07-29 | Neurocrine Biosciences, Inc. | High dosage valbenazine formulation and compositions, methods, and kits related thereto |
MX2020003421A (es) | 2017-10-10 | 2020-07-20 | Neurocrine Biosciences Inc | Metodos para la administracion de ciertos inhibidores del transportador vesicular de monoamina 2 (vmat2). |
US10993941B2 (en) | 2017-10-10 | 2021-05-04 | Neurocrine Biosciences, Inc. | Methods for the administration of certain VMAT2 inhibitors |
KR20200108828A (ko) | 2017-11-22 | 2020-09-21 | 아시아 케미컬 인더스트리스 리미티드 | 발베나진의 고상 형태 |
EP3733666B1 (en) * | 2017-12-26 | 2022-09-21 | Crystal Pharmaceutical (Suzhou) Co., Ltd. | Crystal form of valbenazine di-p-toluenesulfonate, preparation method thereof and use thereof |
CN110818705A (zh) * | 2018-08-14 | 2020-02-21 | 苏州鹏旭医药科技有限公司 | 缬苯那嗪的盐型和相应晶型与其制备方法 |
BR112021000019A2 (pt) | 2018-08-15 | 2021-04-06 | Neurocrine Biosciences Inc. | Métodos para administração de certos inibidores de vmat2 |
CA3065236A1 (en) | 2018-12-27 | 2020-06-27 | Apotex Inc. | Novel crystalline form of valbenazine dibesylate |
WO2020213014A1 (en) | 2019-04-19 | 2020-10-22 | Mylan Laboratories Limited | An improved process for the preparation of valbenazine and its salts |
US10689380B1 (en) * | 2019-07-30 | 2020-06-23 | Farmhispania S.A. | Crystalline forms of valbenazine ditosylate |
US10940141B1 (en) | 2019-08-23 | 2021-03-09 | Neurocrine Biosciences, Inc. | Methods for the administration of certain VMAT2 inhibitors |
CN117736203A (zh) | 2019-09-13 | 2024-03-22 | 纽罗克里生物科学有限公司 | 用于合成缬苯那嗪的方法 |
MX2023002761A (es) | 2020-09-09 | 2023-04-03 | Crinetics Pharmaceuticals Inc | Formulaciones de un modulador de somatostatina. |
CA3215792A1 (en) | 2021-04-26 | 2022-11-03 | John Lloyd Tucker | Processes for the synthesis of valbenazine |
CA3220946A1 (en) | 2021-06-30 | 2023-01-05 | Angel S. Angelov | Valbenazine for use in the add-on treatment of schizophrenia |
CA3221728A1 (en) * | 2021-06-30 | 2023-01-05 | Grace S. LIANG | Valbenazine for use in the treatment of dyskinesia due to cerebral palsy |
TW202322816A (zh) | 2021-08-20 | 2023-06-16 | 美商紐羅克里生物科學有限公司 | 篩選 vmat2 抑制劑之方法 |
Family Cites Families (99)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3536809A (en) | 1969-02-17 | 1970-10-27 | Alza Corp | Medication method |
US3598123A (en) | 1969-04-01 | 1971-08-10 | Alza Corp | Bandage for administering drugs |
US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
US3916899A (en) | 1973-04-25 | 1975-11-04 | Alza Corp | Osmotic dispensing device with maximum and minimum sizes for the passageway |
US4008719A (en) | 1976-02-02 | 1977-02-22 | Alza Corporation | Osmotic system having laminar arrangement for programming delivery of active agent |
JPS5777697A (en) | 1980-11-04 | 1982-05-15 | Nippon Zoki Pharmaceut Co Ltd | Physiologically active substance nsq |
US4328245A (en) | 1981-02-13 | 1982-05-04 | Syntex (U.S.A.) Inc. | Carbonate diester solutions of PGE-type compounds |
US4410545A (en) | 1981-02-13 | 1983-10-18 | Syntex (U.S.A.) Inc. | Carbonate diester solutions of PGE-type compounds |
JPS57209225A (en) | 1981-06-18 | 1982-12-22 | Yamasa Shoyu Co Ltd | Antitumor activity intensifier |
US4409239A (en) | 1982-01-21 | 1983-10-11 | Syntex (U.S.A.) Inc. | Propylene glycol diester solutions of PGE-type compounds |
KR890002631B1 (ko) | 1984-10-04 | 1989-07-21 | 몬산토 캄파니 | 생물학적으로 활성인 소마토트로핀을 지속적으로 유리하는 조성물 |
IE58110B1 (en) | 1984-10-30 | 1993-07-14 | Elan Corp Plc | Controlled release powder and process for its preparation |
US5073543A (en) | 1988-07-21 | 1991-12-17 | G. D. Searle & Co. | Controlled release formulations of trophic factors in ganglioside-lipsome vehicle |
US5612059A (en) | 1988-08-30 | 1997-03-18 | Pfizer Inc. | Use of asymmetric membranes in delivery devices |
IT1229203B (it) | 1989-03-22 | 1991-07-25 | Bioresearch Spa | Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative. |
PH30995A (en) | 1989-07-07 | 1997-12-23 | Novartis Inc | Sustained release formulations of water soluble peptides. |
US5120548A (en) | 1989-11-07 | 1992-06-09 | Merck & Co., Inc. | Swelling modulated polymeric drug delivery device |
US5585112A (en) | 1989-12-22 | 1996-12-17 | Imarx Pharmaceutical Corp. | Method of preparing gas and gaseous precursor-filled microspheres |
IT1246382B (it) | 1990-04-17 | 1994-11-18 | Eurand Int | Metodo per la cessione mirata e controllata di farmaci nell'intestino e particolarmente nel colon |
US5733566A (en) | 1990-05-15 | 1998-03-31 | Alkermes Controlled Therapeutics Inc. Ii | Controlled release of antiparasitic agents in animals |
US5204329A (en) | 1990-06-11 | 1993-04-20 | Du Pont Merck Pharmaceutical Company | Treatment of organ transplantation rejection |
US5543390A (en) | 1990-11-01 | 1996-08-06 | State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University | Covalent microparticle-drug conjugates for biological targeting |
US5580578A (en) | 1992-01-27 | 1996-12-03 | Euro-Celtique, S.A. | Controlled release formulations coated with aqueous dispersions of acrylic polymers |
TW333456B (en) | 1992-12-07 | 1998-06-11 | Takeda Pharm Ind Co Ltd | A pharmaceutical composition of sustained-release preparation the invention relates to a pharmaceutical composition of sustained-release preparation which comprises a physiologically active peptide. |
US5591767A (en) | 1993-01-25 | 1997-01-07 | Pharmetrix Corporation | Liquid reservoir transdermal patch for the administration of ketorolac |
US6274552B1 (en) | 1993-03-18 | 2001-08-14 | Cytimmune Sciences, Inc. | Composition and method for delivery of biologically-active factors |
US5523092A (en) | 1993-04-14 | 1996-06-04 | Emory University | Device for local drug delivery and methods for using the same |
US5985307A (en) | 1993-04-14 | 1999-11-16 | Emory University | Device and method for non-occlusive localized drug delivery |
US6087324A (en) | 1993-06-24 | 2000-07-11 | Takeda Chemical Industries, Ltd. | Sustained-release preparation |
US6004534A (en) | 1993-07-23 | 1999-12-21 | Massachusetts Institute Of Technology | Targeted polymerized liposomes for improved drug delivery |
IT1270594B (it) | 1994-07-07 | 1997-05-07 | Recordati Chem Pharm | Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida |
US5759542A (en) | 1994-08-05 | 1998-06-02 | New England Deaconess Hospital Corporation | Compositions and methods for the delivery of drugs by platelets for the treatment of cardiovascular and other diseases |
US5660854A (en) | 1994-11-28 | 1997-08-26 | Haynes; Duncan H | Drug releasing surgical implant or dressing material |
US6316652B1 (en) | 1995-06-06 | 2001-11-13 | Kosta Steliou | Drug mitochondrial targeting agents |
US5798119A (en) | 1995-06-13 | 1998-08-25 | S. C. Johnson & Son, Inc. | Osmotic-delivery devices having vapor-permeable coatings |
ATE268591T1 (de) | 1995-06-27 | 2004-06-15 | Takeda Chemical Industries Ltd | Verfahren zur herstellung von zubereitungen mit verzögerter freisetzung |
TW448055B (en) | 1995-09-04 | 2001-08-01 | Takeda Chemical Industries Ltd | Method of production of sustained-release preparation |
JP2909418B2 (ja) | 1995-09-18 | 1999-06-23 | 株式会社資生堂 | 薬物の遅延放出型マイクロスフイア |
US6039975A (en) | 1995-10-17 | 2000-03-21 | Hoffman-La Roche Inc. | Colon targeted delivery system |
US5980945A (en) | 1996-01-16 | 1999-11-09 | Societe De Conseils De Recherches Et D'applications Scientifique S.A. | Sustained release drug formulations |
TW345603B (en) | 1996-05-29 | 1998-11-21 | Gmundner Fertigteile Gmbh | A noise control device for tracks |
US6264970B1 (en) | 1996-06-26 | 2001-07-24 | Takeda Chemical Industries, Ltd. | Sustained-release preparation |
US6419961B1 (en) | 1996-08-29 | 2002-07-16 | Takeda Chemical Industries, Ltd. | Sustained release microcapsules of a bioactive substance and a biodegradable polymer |
ZA977967B (en) | 1996-09-23 | 1999-03-04 | Lilly Co Eli | Combination therapy for treatment of psychoses |
CN1233954A (zh) | 1996-10-01 | 1999-11-03 | 西马实验室股份有限公司 | 掩盖味道的微胶囊组合物及其制备方法 |
CA2217134A1 (en) | 1996-10-09 | 1998-04-09 | Sumitomo Pharmaceuticals Co., Ltd. | Sustained release formulation |
EP0839525B1 (en) | 1996-10-31 | 2004-08-04 | Takeda Chemical Industries, Ltd. | Sustained-release preparation |
US6131570A (en) | 1998-06-30 | 2000-10-17 | Aradigm Corporation | Temperature controlling device for aerosol drug delivery |
ATE233088T1 (de) | 1996-12-20 | 2003-03-15 | Takeda Chemical Industries Ltd | Verfahren zur herstellung einer zusammensetzung mit verzoegerter abgabe |
US5891474A (en) | 1997-01-29 | 1999-04-06 | Poli Industria Chimica, S.P.A. | Time-specific controlled release dosage formulations and method of preparing same |
US6120751A (en) | 1997-03-21 | 2000-09-19 | Imarx Pharmaceutical Corp. | Charged lipids and uses for the same |
US6060082A (en) | 1997-04-18 | 2000-05-09 | Massachusetts Institute Of Technology | Polymerized liposomes targeted to M cells and useful for oral or mucosal drug delivery |
US6350458B1 (en) | 1998-02-10 | 2002-02-26 | Generex Pharmaceuticals Incorporated | Mixed micellar drug deliver system and method of preparation |
US6613358B2 (en) | 1998-03-18 | 2003-09-02 | Theodore W. Randolph | Sustained-release composition including amorphous polymer |
US6048736A (en) | 1998-04-29 | 2000-04-11 | Kosak; Kenneth M. | Cyclodextrin polymers for carrying and releasing drugs |
KR19990085365A (ko) | 1998-05-16 | 1999-12-06 | 허영섭 | 지속적으로 약물 조절방출이 가능한 생분해성 고분자 미립구 및그 제조방법 |
AU1321900A (en) | 1998-10-23 | 2000-05-15 | Sepracor, Inc. | Compositions and methods employing r(-) fluoxetine and other active ingredients |
US6248363B1 (en) | 1999-11-23 | 2001-06-19 | Lipocine, Inc. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
US6271359B1 (en) | 1999-04-14 | 2001-08-07 | Musc Foundation For Research Development | Tissue-specific and pathogen-specific toxic agents and ribozymes |
AU2001276608A1 (en) | 2000-08-30 | 2002-03-13 | Pfizer Products Inc. | Sustained release formulations for growth hormone secretagogues |
WO2003099011A1 (en) | 2002-05-28 | 2003-12-04 | Henry M. Jackson Foundation For The Advancement Of Military Medicine, Inc. | Cardiac glycosides to treat cystic fibrosis and other il-8 dependent disorders |
CA2499601A1 (en) | 2002-09-19 | 2004-04-01 | University Of Utah Research Foundation | Modulating vesicular monoamine transporter trafficking and function: a novel approach for the treatment of parkinson's disease |
GB2410947B (en) | 2004-02-11 | 2008-09-17 | Cambridge Lab Ltd | Pharmaceutical compounds |
CN106075435A (zh) | 2004-06-04 | 2016-11-09 | 健泰科生物技术公司 | 用于治疗多发性硬化的方法 |
PT1855677E (pt) | 2005-08-06 | 2009-01-13 | Cambridge Lab Ireland Ltd | 3-11b-cis-di-hidrotetrabenazina para o tratamento da esquizofrenia e de outras psicoses |
US20100076087A1 (en) | 2005-10-06 | 2010-03-25 | Auspex Pharmaceuticals, Inc. | Methods of reduction of interpatient variability |
BRPI0718247B1 (pt) * | 2006-11-08 | 2021-09-21 | Neurocrine Biosciences, Inc. | Composto usado como inibidor do transportador de monoamina vesicular 2, composição farmacêutica compreendendo o dito composto e uso da dita composição farmacêutica no tratamento de transtornos hipercinéticos |
GB0721669D0 (en) | 2007-11-02 | 2007-12-12 | Cambridge Lab Ireland Ltd | Pharmaceutical compounds |
UA101352C2 (uk) | 2008-01-18 | 2013-03-25 | Ейсей Р Енд Д Менеджмент Ко., Лтд. | Конденсоване похідне амінодигідротіазину |
GB2462611A (en) | 2008-08-12 | 2010-02-17 | Cambridge Lab | Pharmaceutical composition comprising tetrabenazine |
US20110053866A1 (en) | 2008-08-12 | 2011-03-03 | Biovail Laboratories International (Barbados) S.R.L. | Pharmaceutical compositions |
GB2463452A (en) | 2008-09-08 | 2010-03-17 | Cambridge Lab | Desmethyl derivatives of tetrabenazine and pharmaceutical compositions thereof |
GB2463451A (en) | 2008-09-08 | 2010-03-17 | Cambridge Lab | 3, 11b cis-dihydrotetrabenazine compounds for use in the treatment of dementia |
CN102186848B (zh) | 2008-09-18 | 2014-11-12 | 奥斯拜客斯制药有限公司 | 囊泡单胺转运体2的苯并喹啉抑制剂 |
US20100096319A1 (en) | 2008-10-17 | 2010-04-22 | General Electric Company | Separator assembly |
CA2771539A1 (en) | 2009-08-12 | 2011-02-17 | Valeant International (Barbados) Srl | Pharmaceutical compositions with tetrabenzine |
EP2576552A4 (en) | 2010-06-01 | 2013-11-13 | Aupex Pharmaceutical Inc | BENZOQUINOLONE INHIBITORS OF VMAT2 |
AU2013318182C1 (en) | 2012-09-18 | 2022-01-20 | Auspex Pharmaceuticals, Inc. | Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2 |
CN110200958A (zh) | 2012-12-18 | 2019-09-06 | 万达制药公司 | 昼夜节律紊乱的治疗 |
EP3421469A1 (en) | 2013-01-31 | 2019-01-02 | Auspex Pharmaceuticals, Inc. | Benzoquinolone inhibitors of vmat2 |
WO2015077521A1 (en) | 2013-11-22 | 2015-05-28 | Auspex Pharmaceuticals, Inc. | Benzoquinoline inhibitors of vesicular monoamine transporter 2 |
AU2015209330A1 (en) | 2014-01-27 | 2016-07-28 | Auspex Pharmaceuticals, Inc. | Benzoquinoline inhibitors of vesicular monoamine transporter 2 |
KR20160117596A (ko) * | 2014-02-07 | 2016-10-10 | 오스펙스 파마슈티칼스, 인코포레이티드 | 신규 제약 제제 |
EP4049681A1 (en) | 2014-02-07 | 2022-08-31 | Neurocrine Biosciences, Inc. | Pharmaceutical compositions comprising an antipsychotic drug and a vmat2 inhibitor and uses thereof |
AU2015256012B2 (en) | 2014-05-06 | 2020-07-23 | Neurocrine Biosciences, Inc. | VMAT2 inhibitors for the treatment of hyperkinetic movement disorders |
WO2016127133A1 (en) | 2015-02-06 | 2016-08-11 | Neurocrine Biosciences, Inc. | [9,10-dimethoxy-3-(2-methylpropyl)-1h,2h,3h,4h,6h,7h,11bh-pyrido-[2,1-a]isoquinolin-2-yl]methanol and compounds, compositions and methods relating thereto |
KR20230003264A (ko) | 2015-03-06 | 2023-01-05 | 오스펙스 파마슈티칼스, 인코포레이티드 | 비정상적 불수의 운동 장애의 치료 방법 |
EA036837B1 (ru) | 2015-06-23 | 2020-12-25 | Нейрокрин Байосайенсиз, Инк. | Ингибиторы vmat2 для лечения неврологических заболеваний или расстройств |
BR112018008460A2 (pt) | 2015-10-30 | 2018-11-06 | Neurocrine Biosciences Inc | sais de valbenazina e seus polimorfos |
RS63170B1 (sr) | 2015-12-23 | 2022-05-31 | Neurocrine Biosciences Inc | Sintetički postupak za pripremanje (s)-(2r,3r,11br)-3-izobutil-9,10-dimetoksi-2,3,4,6,7,11b-heksahidro-1h-pirido[2,1,-a]izohinolin-2-il 2-amino-3-metilbutanoat di(4-metilbenzensulfonata) |
WO2018102673A1 (en) | 2016-12-02 | 2018-06-07 | Neurocrine Biosciences, Inc. | Use of valbenazine for treating schizophrenia or schizoaffective disorder |
MX2019008855A (es) | 2017-01-27 | 2019-09-11 | Neurocrine Biosciences Inc | Metodos para la administracion de ciertos inhibidores del transportador de monamina vesicular 2 (vmat2). |
WO2018200605A1 (en) | 2017-04-26 | 2018-11-01 | Neurocrine Biosciences, Inc. | Use of valbenazine for treating levodopa-induced dyskinesia |
EP3684333A2 (en) | 2017-09-21 | 2020-07-29 | Neurocrine Biosciences, Inc. | High dosage valbenazine formulation and compositions, methods, and kits related thereto |
MX2020003421A (es) | 2017-10-10 | 2020-07-20 | Neurocrine Biosciences Inc | Metodos para la administracion de ciertos inhibidores del transportador vesicular de monoamina 2 (vmat2). |
US10993941B2 (en) | 2017-10-10 | 2021-05-04 | Neurocrine Biosciences, Inc. | Methods for the administration of certain VMAT2 inhibitors |
MA52896A (fr) | 2018-06-14 | 2021-04-21 | Neurocrine Biosciences Inc | Composés inhibiteurs de vmat2, compositions et méthodes associées |
BR112021000019A2 (pt) | 2018-08-15 | 2021-04-06 | Neurocrine Biosciences Inc. | Métodos para administração de certos inibidores de vmat2 |
US10689380B1 (en) * | 2019-07-30 | 2020-06-23 | Farmhispania S.A. | Crystalline forms of valbenazine ditosylate |
-
2016
- 2016-10-28 BR BR112018008460A patent/BR112018008460A2/pt active Search and Examination
- 2016-10-28 ES ES16794479T patent/ES2857085T3/es active Active
- 2016-10-28 KR KR1020187014815A patent/KR20180075591A/ko not_active Application Discontinuation
- 2016-10-28 AU AU2016343633A patent/AU2016343633B2/en active Active
- 2016-10-28 RS RS20240144A patent/RS65154B1/sr unknown
- 2016-10-28 SI SI201631106T patent/SI3368534T1/sl unknown
- 2016-10-28 TN TNP/2018/000121A patent/TN2018000121A1/en unknown
- 2016-10-28 MX MX2018005136A patent/MX2018005136A/es unknown
- 2016-10-28 EA EA201890852A patent/EA201890852A1/ru unknown
- 2016-10-28 EP EP16794479.2A patent/EP3368534B1/en active Active
- 2016-10-28 LT LTEP21153302.1T patent/LT3875459T/lt unknown
- 2016-10-28 SG SG11201803408PA patent/SG11201803408PA/en unknown
- 2016-10-28 MA MA43116A patent/MA43116B1/fr unknown
- 2016-10-28 RS RS20210402A patent/RS61645B1/sr unknown
- 2016-10-28 PT PT167944792T patent/PT3368534T/pt unknown
- 2016-10-28 CA CA3002074A patent/CA3002074A1/en active Pending
- 2016-10-28 PL PL16794479T patent/PL3368534T3/pl unknown
- 2016-10-28 HU HUE16794479A patent/HUE053872T2/hu unknown
- 2016-10-28 US US15/338,214 patent/US10065952B2/en active Active
- 2016-10-28 EP EP21153302.1A patent/EP3875459B1/en active Active
- 2016-10-28 EP EP23214069.9A patent/EP4344742A2/en active Pending
- 2016-10-28 CN CN201680072826.6A patent/CN108473489B/zh active Active
- 2016-10-28 CN CN202210983938.4A patent/CN115322188A/zh active Pending
- 2016-10-28 JP JP2018521548A patent/JP7109360B2/ja active Active
- 2016-10-28 HR HRP20240304TT patent/HRP20240304T1/hr unknown
- 2016-10-28 MA MA56137A patent/MA56137B1/fr unknown
- 2016-10-28 DK DK16794479.2T patent/DK3368534T3/da active
- 2016-10-28 FI FIEP21153302.1T patent/FI3875459T3/fi active
- 2016-10-28 MY MYPI2018000569A patent/MY193767A/en unknown
- 2016-10-28 CN CN202210983939.9A patent/CN115304596A/zh active Pending
- 2016-10-28 IL IL284874A patent/IL284874B2/en unknown
- 2016-10-28 LT LTEP16794479.2T patent/LT3368534T/lt unknown
- 2016-10-28 PT PT211533021T patent/PT3875459T/pt unknown
- 2016-10-28 DK DK21153302.1T patent/DK3875459T3/da active
- 2016-10-28 WO PCT/US2016/059306 patent/WO2017075340A1/en active Application Filing
-
2018
- 2018-04-16 IL IL258732A patent/IL258732B/en unknown
- 2018-04-24 CL CL2018001089A patent/CL2018001089A1/es unknown
- 2018-04-26 PH PH12018500900A patent/PH12018500900A1/en unknown
- 2018-04-27 CO CONC2018/0004589A patent/CO2018004589A2/es unknown
- 2018-04-30 SA SA518391477A patent/SA518391477B1/ar unknown
-
2020
- 2020-06-12 US US16/899,645 patent/US10851103B2/en active Active
- 2020-06-12 US US16/899,641 patent/US10844058B2/en active Active
- 2020-06-12 US US16/899,654 patent/US10851104B2/en active Active
-
2021
- 2021-03-22 HR HRP20210469TT patent/HRP20210469T1/hr unknown
- 2021-03-31 CY CY20211100278T patent/CY1124002T1/el unknown
-
2022
- 2022-07-19 JP JP2022114755A patent/JP2022141821A/ja active Pending
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20210469T1 (hr) | Valbenazin ditosilat i njegovi polimorfi | |
HRP20160208T4 (hr) | Polimorfi dasatiniba i postupak za njihovu pripremu | |
HRP20201644T1 (hr) | Kristalni oblik 2-butoksi-7-(4-(pirolidin-1-ilmetil)benzil)-5h-pirolo [3,2-d]pirimidin-4-amina kao agonist tlr7, postupak njegove proizvodnje i njegova uporaba | |
HRP20180970T1 (hr) | Policiklični lpa1 antagonist i njegove primjene | |
ES2621664T3 (es) | Cristal de ácido 7-{(3S,4S)-3-[(ciclopropilamino)metil]-4-fluoropirrolidin-1-il}-6-fluoro-1-(2-fluoroetil)-8-metoxi-4-oxo-1,4-dihidroquinolin-3-carboxílico | |
HRP20210675T1 (hr) | Mono- ili di-supstituirani derivati indola kao inhibitori replikacije denga virusa | |
IL258052A (en) | Solid configurations of isoquinolinone derivatives, process for their preparation, compositions containing them and methods of use | |
JP5286087B2 (ja) | 新規グリチルレチン酸−30−アミド誘導体及びその用途 | |
HRP20170295T1 (hr) | Oblik soli inhibitora ljudske histonske metiltransferaze ezh2 | |
HRP20141137T1 (hr) | Polimorfni oblici macrocikliäśkog inhibitora hcv | |
JP2018531963A5 (hr) | ||
JP2016537346A5 (hr) | ||
HRP20160168T1 (hr) | Kristalne forme makrolida i njihova uporaba | |
CN102367253B (zh) | 一种制备他达拉非晶型a的方法 | |
HRP20201275T1 (hr) | Kristalni oblik derivata benzimidazola i postupak njegove proizvodnje | |
HRP20210667T1 (hr) | Kristalni oblici antagonista androgenog receptora, postupak pripreme i njihova upotreba | |
EP2523560A1 (en) | Compounds and methods | |
JP6411355B2 (ja) | 抗菌剤 | |
HRP20191596T1 (hr) | Postupak za pripravu 2-{4-[2-({[2-(4-klorofenil)-1,3-tiazol-4-il]metil}sulfanil)-3,5-dicijan-6- (pirolidin-1-il)piridin-4-il]fenoksi}etil-l-alanil-l-alaninat hidroklorida | |
Marcos et al. | Synthesis of (+)-agelasine C. A structural revision | |
CA2966960A1 (en) | 2,3-dihydro-thiazolo[3,2-a]pyridin-5-one derivatives, intermediates thereof, and their use as antibacterial agents | |
AR087344A1 (es) | Formas polimorficas del acido 5-(3,3-dimetil-but-1-inil)-3-[(trans-4-hidroxi-ciclohexil)-(trans-4-metil-ciclohexancarbonil)-amino]-tiofen-2-carboxilico y su uso en el tratamiento de la hepatitis c | |
HRP20220234T1 (hr) | Kristalni oblici | |
CN104829575A (zh) | 一种6-氟吡喃衍生物的制备方法 | |
CN104860910A (zh) | 一种8-氟吡喃衍生物的制备方法 |