HRP20240304T1 - Soli valbenazin dihidroklorida i njihovi polimorfi - Google Patents

Soli valbenazin dihidroklorida i njihovi polimorfi Download PDF

Info

Publication number
HRP20240304T1
HRP20240304T1 HRP20240304TT HRP20240304T HRP20240304T1 HR P20240304 T1 HRP20240304 T1 HR P20240304T1 HR P20240304T T HRP20240304T T HR P20240304TT HR P20240304 T HRP20240304 T HR P20240304T HR P20240304 T1 HRP20240304 T1 HR P20240304T1
Authority
HR
Croatia
Prior art keywords
crystalline form
amorphous form
temperature
amorphous
form according
Prior art date
Application number
HRP20240304TT
Other languages
English (en)
Inventor
Kevin MCGEE
Scott Zook
Andrew Carr
Thierry Bonnaud
Original Assignee
Neurocrine Biosciences, Inc.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=57281297&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20240304(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Neurocrine Biosciences, Inc. filed Critical Neurocrine Biosciences, Inc.
Publication of HRP20240304T1 publication Critical patent/HRP20240304T1/hr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D455/00Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/03Heterocyclic 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
    • C07D455/04Heterocyclic 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
    • C07D455/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/4375Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/32Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30Sulfonic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (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 (26)

1. Kristalni oblik, naznačen time, da je od spoja Formule II: [image]
2. Kristalni oblik prema patentnom zahtjevu 1, naznačen time, da posjeduje uzorak rendgenske difrakcije na prahu koji sadrži maksimume na 7,2, 9,2, i 18,0 stupnjeva dva-theta ± 0,2 theta.
3. Kristalni oblik prema patentnom zahtjevu 2, naznačen time, da posjeduje termogram diferencijalne pretražne kalorimetrije koji sadrži endotermičku pojavu s početnom temperaturom od 240°C i s maksimumom na 250°C.
4. Kristalni oblik prema patentnom zahtjevu 2 ili 3, naznačen time, da pokazuje povećanje mase od 14% kada se podvrgava povećanju relativne vlažnosti od 0% do 90% relativne vlage.
5. Kristalni oblik prema patentnom zahtjevu 1, naznačen time, da posjeduje uzorak rendgenske difrakcije na prahu koji sadrži maksimume na 4,8, 13,3, i 24,9 stupnjeva dva-theta ± 0,2 theta.
6. Kristalni oblik prema patentnom zahtjevu 5, naznačen time, da posjeduje termogram diferencijalne pretražne kalorimetrije koji sadrži endotermičku pojavu s početnom temperaturom od 80°C i s maksimumom na 106°C.
7. Kristalni oblik prema patentnom zahtjevu 5 ili 6, naznačen time, da posjeduje shemu toplinske gravimetrijske analize koja sadrži gubitak mase od 10% kada se zagrijava od 25°C do 140°C.
8. Kristalni oblik prema bilo kojem od patentnih zahtjeva 5 do 7, naznačen time, da pokazuje smanjenje mase od 12% kada se podvrgava smanjenju relativne vlažnosti od 75% do 0% relativne vlage.
9. Amorfni oblik, naznačen time, da je od spoja Formule II: [image]
10. Farmaceutski pripravak, naznačen time, da sadrži kristalni oblik prema bilo kojem od patentnih zahtjeva 1 do 8, ili amorfni oblik prema patentnom zahtjevu 9, i farmaceutski prihvatljiv nosač.
11. Farmaceutski pripravak prema patentnom zahtjevu 10, naznačen time, da se pripravak formulira za oralnu primjenu.
12. Farmaceutski pripravak prema patentnom zahtjevu 10 ili 11, naznačen time, da se pripravak formulira kao jednostruki oblik za doziranje.
13. Kristalni oblik prema bilo kojem od patentnih zahtjeva 1 do 8, ili amorfni oblik prema patentnom zahtjevu 9, naznačen time, da je za uporabu u postupku za liječenje, prevenciju, ili poboljšavanje jednog ili više simptoma hiperkinetskog poremećaja.
14. Kristalni oblik ili amorfni oblik za uporabu prema patentnom zahtjevu 13, naznačen time, da hiperkinetski poremećaj je Huntingtonova bolest, tardivna diskinezija, Touretteov sindrom, distonija, hemibalizam, koreja, senilna koreja, ili tikovi.
15. Kristalni oblik ili amorfni oblik za uporabu prema patentnom zahtjevu 13, naznačen time, da hiperkinetski poremećaj je Huntingtonova bolest.
16. Kristalni oblik ili amorfni oblik za uporabu prema patentnom zahtjevu 13, naznačen time, da hiperkinetski poremećaj je tardivna diskinezija.
17. Kristalni oblik ili amorfni oblik za uporabu prema patentnom zahtjevu 13, naznačen time, da hiperkinetski poremećaj je Touretteov sindrom.
18. Kristalni oblik ili amorfni oblik za uporabu prema patentnom zahtjevu 13, naznačen time, da hiperkinetski poremećaj su tikovi.
19. Postupak za proizvodnju kristalnog oblika prema bilo kojem od patentnih zahtjeva 1 do 8, ili amorfnog oblika prema patentnom zahtjevu 9, naznačen time, da obuhvaća sljedeće faze: (a) pripravljanje emulzije od spoja Formule II u otapalu na prvoj temperaturi; i (b) generiranje kristalnog oblika ili amorfnog oblika putem hlađenja otopine na drugu temperaturu.
20. Postupak za proizvodnju kristalnog oblika prema bilo kojem od patentnih zahtjeva 1 do 8, ili amorfnog oblika prema patentnom zahtjevu 9, naznačen time, da obuhvaća sljedeće faze: (a) pripravljanje otopine spoja Formule II u otapalu na prvoj temperaturi; (b) formiranje emulzije putem hlađenja otopine na drugu temperaturu; i (c) generiranje kristalnog oblika ili amorfnog oblika pomoću obrade emulzije s jednim ili više ciklusa zagrijavanja i hlađenja.
21. Postupak prema patentnom zahtjevu 20, naznačen time, da se ciklus zagrijavanja i hlađenja izvodi u temperaturnom rasponu od -50 do 120°C.
22. Postupak prema patentnom zahtjevu 20 ili 21, naznačen time, da prva temperatura iznosi od 20 do 200°C.
23. Postupak prema bilo kojem od patentnih zahtjeva 20 do 22, naznačen time, da druga temperatura iznosi od -100 do 100°C.
24. Postupak prema bilo kojem od patentnih zahtjeva 20 do 23, naznačen time, da nadalje obuhvaća fazu izoliranja kristalnog oblika ili amorfnog oblika.
25. Postupak prema bilo kojem od patentnih zahtjeva 20 do 24, naznačen time, da se otapalo bira od ugljikovodika, kloriranog ugljikovodika, alkohola, etera, ketona, estera, karbonata, amida, nitrila, nitro spoja, heterocikla, vode, i njihovih mješavina.
26. Postupak prema bilo kojem od patentnih zahtjeva 20 do 25, naznačen time, da se otapalo bira od acetonitrila, 1,2-dikloroetana, DMF, 1,4-dioksana, metanola, 2-metoksietanola, MIBK, toluena, heptana, kumena, acetona, 1-butanola, MTBE, etanola, etil acetata, etil formata, izobutil acetata, izopropil acetata, metil acetata, nitrometana, 1-propanola, IPA, MEK, THF, vode, i njihovih mješavina.
HRP20240304TT 2015-10-30 2016-10-28 Soli valbenazin dihidroklorida i njihovi polimorfi HRP20240304T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562249074P 2015-10-30 2015-10-30
EP21153302.1A EP3875459B1 (en) 2015-10-30 2016-10-28 Valbenazine dihydrochloride salts and polymorphs thereof

Publications (1)

Publication Number Publication Date
HRP20240304T1 true HRP20240304T1 (hr) 2024-05-10

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 After (1)

Application Number Title Priority Date Filing Date
HRP20210469TT HRP20210469T1 (hr) 2015-10-30 2021-03-22 Valbenazin ditosilat i njegovi polimorfi

Country Status (31)

Country Link
US (4) US10065952B2 (hr)
EP (3) EP4344742A2 (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) DK3875459T3 (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) LT3368534T (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) RS61645B1 (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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA43116B1 (fr) 2015-10-30 2021-04-30 Neurocrine Biosciences Inc Ditosylate de valbénazine et polymorphes associés
JP6869988B2 (ja) 2015-12-23 2021-05-12 ニューロクライン バイオサイエンシーズ,インコーポレイテッド (S)−(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−2,3,4,6,7,11b−ヘキサヒドロ−1H−ピリド[2,1−a]イソキノリン−2−イル2−アミノ−3−メチルブタノエートジ(4−メチルベンゼンスルホネート)の調製のための合成方法
US11242341B2 (en) 2016-10-06 2022-02-08 Assia Chemical Industries Ltd. Solid state forms of valbenazine
EP3548027A1 (en) * 2016-12-02 2019-10-09 Neurocrine Biosciences, Inc. Use of valbenazine for treating schizophrenia or schizoaffective disorder
WO2018130345A1 (en) * 2017-01-10 2018-07-19 Sandoz Ag Crystalline valbenazine free base
KR20200066662A (ko) 2017-01-27 2020-06-10 뉴로크린 바이오사이언시즈 인코퍼레이티드 특정 vmat2 억제제의 투여 방법
US10954235B2 (en) * 2017-02-27 2021-03-23 Sandoz Ag Crystalline forms of valbenazine salts
US20200179352A1 (en) * 2017-04-26 2020-06-11 Neurocrine Biosciences, Inc. Use of valbenazine for treating levodopa-induced dyskinesia
MX2020002841A (es) 2017-09-21 2020-07-22 Neurocrine Biosciences Inc Formulacion de valbenazina de alta dosis y composiciones, metodos y kits relacionados con la misma.
EA202090932A1 (ru) 2017-10-10 2021-05-20 Нейрокрин Байосайенсиз, Инк Способы введения некоторых vmat2-ингибиторов
US10993941B2 (en) 2017-10-10 2021-05-04 Neurocrine Biosciences, Inc. Methods for the administration of certain VMAT2 inhibitors
WO2019104141A1 (en) 2017-11-22 2019-05-31 Teva Pharmaceuticals Usa, Inc. Solid state form of valbenazine
CA3086611C (en) * 2017-12-26 2023-07-25 Crystal Pharmaceutical (Suzhou) Co., Ltd. A crystalline form of valbenazine ditosylate, processes for preparation 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
CA3104693A1 (en) 2018-08-15 2020-02-20 Neurocrine Biosciences, Inc. Methods for the administration of certain vmat2 inhibitors
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
EP4028397A1 (en) 2019-09-13 2022-07-20 Neurocrine Biosciences, Inc. Processes for the synthesis of valbenazine
KR20230066379A (ko) 2020-09-09 2023-05-15 크리네틱스 파마슈티칼스, 인크. 소마토스타틴 조절제 제형
WO2022232060A1 (en) 2021-04-26 2022-11-03 Neurocrine Biosciences, Inc. Processes for the synthesis of valbenazine
KR20240027780A (ko) 2021-06-30 2024-03-04 뉴로크린 바이오사이언시즈 인코퍼레이티드 조현병의 부가적 치료에 사용하기 위한 발베나진
EP4362942A1 (en) * 2021-06-30 2024-05-08 Neurocrine Biosciences, Inc. Valbenazine for use in the treatment of dyskinesia due to cerebral palsy
IL310907A (en) 2021-08-20 2024-04-01 Neurocrine Biosciences Inc Screening methods for VMAT2 inhibitors

Family Cites Families (99)

* Cited by examiner, † Cited by third party
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
HU196714B (en) 1984-10-04 1989-01-30 Monsanto Co Process for producing non-aqueous composition comprising somatotropin
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
EP0835101B1 (en) 1995-06-27 2004-06-09 Takeda Chemical Industries, Ltd. Method of producing sustained-release preparation
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
EP1007012A4 (en) 1996-10-01 2006-01-18 Cima Labs Inc TASTE-MASKED MICRO-CAPSULE COMPOSITION AND MANUFACTURING PROCESS
CA2217134A1 (en) 1996-10-09 1998-04-09 Sumitomo Pharmaceuticals Co., Ltd. Sustained release formulation
PT839525E (pt) 1996-10-31 2004-10-29 Takeda Chemical Industries Ltd Preparacao de libertacao prolongada
US6131570A (en) 1998-06-30 2000-10-17 Aradigm Corporation Temperature controlling device for aerosol drug delivery
US6197350B1 (en) 1996-12-20 2001-03-06 Takeda Chemical Industries, Ltd. Method of producing a sustained-release preparation
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
WO2000024399A1 (en) 1998-10-23 2000-05-04 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
BR0113626A (pt) 2000-08-30 2003-06-17 Pfizer Prod Inc Formulações de liberação sustentada para secretores de hormÈnio do crescimento
AU2003240818B2 (en) 2002-05-28 2006-05-04 Bette Pollard Cardiac glycosides to treat cystic fibrosis and other IL-8 dependent disorders
AU2003272608A1 (en) 2002-09-19 2004-04-08 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
AR049200A1 (es) 2004-06-04 2006-07-05 Genentech Inc Metodo para tratar esclerosis multiple con una composicion que contiene un anticuerpo cd20
DE602006004009D1 (de) 2005-08-06 2009-01-15 Cambridge Lab Ireland Ltd 3,11b-cis-dihydrotetrabanezin zur behandlung von schizophrenie und anderen psychosen
US20100076087A1 (en) 2005-10-06 2010-03-25 Auspex Pharmaceuticals, Inc. Methods of reduction of interpatient variability
EA018378B1 (ru) 2006-11-08 2013-07-30 Ньюрокрайн Байосайенсиз, Инк. ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 3-ИЗОБУТИЛ-9,10-ДИМЕТОКСИ-1,3,4,6,7,11b-ГЕКСАГИДРО-2Н-ПИРИДО[2,1-a]ИЗОХИНОЛИН-2-ОЛА И СВЯЗАННЫЕ С НИМИ СПОСОБЫ
GB0721669D0 (en) 2007-11-02 2007-12-12 Cambridge Lab Ireland Ltd Pharmaceutical compounds
PE20091438A1 (es) 2008-01-18 2009-09-26 Eisai Randd Man Co Ltd Derivados fusionados de aminodihidrotiazina
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
GB2463451A (en) 2008-09-08 2010-03-17 Cambridge Lab 3, 11b cis-dihydrotetrabenazine compounds for use in the treatment of dementia
GB2463452A (en) 2008-09-08 2010-03-17 Cambridge Lab Desmethyl derivatives of tetrabenazine and pharmaceutical compositions thereof
ES2425623T3 (es) 2008-09-18 2013-10-16 Auspex Pharmaceuticals, Inc. Inhibidores benzoquinolínicos de transportador vesicular de monoaminas 2
US20100096319A1 (en) 2008-10-17 2010-04-22 General Electric Company Separator assembly
JP2013501810A (ja) 2009-08-12 2013-01-17 ヴァリーント インターナショナル(バルバドス)エスアールエル 医薬組成物
EP3351247A1 (en) 2010-06-01 2018-07-25 Auspex Pharmaceutical, Inc. Benzoquinolone inhibitors of vmat2
CN111728971A (zh) 2012-09-18 2020-10-02 奥斯拜客斯制药有限公司 D6-四苯喹嗪固体口服剂型、化合物、及其药物组合物、制备及治疗方法
BR112015014619A2 (pt) 2012-12-18 2017-07-11 Vanda Pharmaceuticals Inc tratamento de transtornos do ritmo circadiano
JP2016506957A (ja) 2013-01-31 2016-03-07 オースペックス・ファーマシューティカルズ・インコーポレイテッドAuspex Pharmaceuticals, Inc. Vmat2のベンゾキノロン阻害剤
WO2015077521A1 (en) 2013-11-22 2015-05-28 Auspex Pharmaceuticals, Inc. Benzoquinoline inhibitors of vesicular monoamine transporter 2
MX2016009817A (es) 2014-01-27 2017-02-28 Auspex Pharmaceuticals Inc Inhibidores de benzoquinolina del transportador vesicular de monoaminas 2.
EP3102239A1 (en) * 2014-02-07 2016-12-14 Neurocrine Biosciences, Inc. Pharmaceutical compositions comprising an antipsychotic drug and a vmat2 inhibitor and uses thereof
KR20160117596A (ko) * 2014-02-07 2016-10-10 오스펙스 파마슈티칼스, 인코포레이티드 신규 제약 제제
CN106456629A (zh) * 2014-05-06 2017-02-22 纽罗克里生物科学有限公司 用于运动机能亢进性运动障碍的治疗的vmat2抑制剂
AU2016215033B2 (en) 2015-02-06 2020-06-25 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
PL3265085T3 (pl) 2015-03-06 2022-11-07 Auspex Pharmaceuticals, Inc. Sposoby leczenia zaburzeń związanych z nieprawidłowymi ruchami mimowolnymi
MX2017017015A (es) * 2015-06-23 2018-02-26 Neurocrine Biosciences Inc Inhibidores de transportador de monoamina vesicular tipo 2 (vmat2) para tratar enfermedades o trastornos neurologicos.
MA43116B1 (fr) 2015-10-30 2021-04-30 Neurocrine Biosciences Inc Ditosylate de valbénazine et polymorphes associés
JP6869988B2 (ja) 2015-12-23 2021-05-12 ニューロクライン バイオサイエンシーズ,インコーポレイテッド (S)−(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−2,3,4,6,7,11b−ヘキサヒドロ−1H−ピリド[2,1−a]イソキノリン−2−イル2−アミノ−3−メチルブタノエートジ(4−メチルベンゼンスルホネート)の調製のための合成方法
EP3548027A1 (en) 2016-12-02 2019-10-09 Neurocrine Biosciences, Inc. Use of valbenazine for treating schizophrenia or schizoaffective disorder
KR20200066662A (ko) 2017-01-27 2020-06-10 뉴로크린 바이오사이언시즈 인코퍼레이티드 특정 vmat2 억제제의 투여 방법
US20200179352A1 (en) 2017-04-26 2020-06-11 Neurocrine Biosciences, Inc. Use of valbenazine for treating levodopa-induced dyskinesia
MX2020002841A (es) 2017-09-21 2020-07-22 Neurocrine Biosciences Inc Formulacion de valbenazina de alta dosis y composiciones, metodos y kits relacionados con la misma.
EA202090932A1 (ru) 2017-10-10 2021-05-20 Нейрокрин Байосайенсиз, Инк Способы введения некоторых vmat2-ингибиторов
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
CA3104693A1 (en) 2018-08-15 2020-02-20 Neurocrine Biosciences, Inc. Methods for the administration of certain vmat2 inhibitors
US10689380B1 (en) * 2019-07-30 2020-06-23 Farmhispania S.A. Crystalline forms of valbenazine ditosylate

Also Published As

Publication number Publication date
RS61645B1 (sr) 2021-04-29
IL284874B1 (en) 2023-06-01
AU2016343633B2 (en) 2021-07-01
US10844058B2 (en) 2020-11-24
EP3368534A1 (en) 2018-09-05
KR20180075591A (ko) 2018-07-04
CN115322188A (zh) 2022-11-11
US20200339574A1 (en) 2020-10-29
US20170145008A1 (en) 2017-05-25
SA518391477B1 (ar) 2022-03-20
CY1124002T1 (el) 2022-05-27
JP2018531963A (ja) 2018-11-01
MA56137B1 (fr) 2024-03-29
MA43116A (fr) 2018-09-05
US20200339575A1 (en) 2020-10-29
DK3368534T3 (da) 2021-02-15
US20200339576A1 (en) 2020-10-29
EP3368534B1 (en) 2021-01-27
HRP20210469T1 (hr) 2021-05-14
EP4344742A2 (en) 2024-04-03
IL258732A (en) 2018-06-28
IL284874B2 (en) 2023-10-01
HUE053872T2 (hu) 2021-07-28
JP2022141821A (ja) 2022-09-29
AU2016343633A1 (en) 2018-05-10
IL284874A (en) 2021-08-31
PH12018500900A1 (en) 2018-11-12
EA201890852A1 (ru) 2018-10-31
CL2018001089A1 (es) 2018-08-17
JP7109360B2 (ja) 2022-07-29
CN115304596A (zh) 2022-11-08
CA3002074A1 (en) 2017-05-04
CN108473489A (zh) 2018-08-31
WO2017075340A1 (en) 2017-05-04
LT3368534T (lt) 2021-04-12
TN2018000121A1 (en) 2019-10-04
US10851104B2 (en) 2020-12-01
MA43116B1 (fr) 2021-04-30
ES2857085T3 (es) 2021-09-28
LT3875459T (lt) 2024-02-26
PT3368534T (pt) 2021-03-09
PL3368534T3 (pl) 2021-07-12
CN108473489B (zh) 2022-09-02
IL258732B (en) 2021-07-29
MX2018005136A (es) 2018-05-07
BR112018008460A2 (pt) 2018-11-06
SI3368534T1 (sl) 2021-04-30
FI3875459T3 (fi) 2024-02-14
EP3875459A1 (en) 2021-09-08
RS65154B1 (sr) 2024-02-29
MA56137A (fr) 2022-04-13
US10065952B2 (en) 2018-09-04
DK3875459T3 (da) 2024-01-29
CO2018004589A2 (es) 2018-07-19
PT3875459T (pt) 2024-02-21
EP3875459B1 (en) 2023-12-13
US10851103B2 (en) 2020-12-01
MY193767A (en) 2022-10-27
SG11201803408PA (en) 2018-05-30

Similar Documents

Publication Publication Date Title
HRP20240304T1 (hr) Soli valbenazin dihidroklorida i njihovi polimorfi
HRP20180970T1 (hr) Policiklični lpa1 antagonist i njegove primjene
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
FI78691B (fi) Foerfarande foer framstaellning av i position 3-substituerade pyridazinderivat, vilka inverkar pao det centrala nervsystemet.
HRP20171696T1 (hr) 3,4-dihidroizokinolin-2(1h)-ilni spojevi
JP2018531963A5 (hr)
CA2787018A1 (en) Inhibitors of histone deacetylase (hdac) enzymes
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
JP2016537346A5 (hr)
JP2016506368A5 (hr)
JP2015512942A5 (hr)
JP2002523369A (ja) 新規イソオキサゾリノン抗菌剤
HRP20201275T1 (hr) Kristalni oblik derivata benzimidazola i postupak njegove proizvodnje
EP3752497A1 (en) P300/cbp hat inhibitors
HRP20210667T1 (hr) Kristalni oblici antagonista androgenog receptora, postupak pripreme i njihova upotreba
CN104926775A (zh) 一种含氟吡喃衍生物的制备方法
JP6411355B2 (ja) 抗菌剤
CN114375293A (zh) 异喹啉类化合物及其制备方法和应用
CN107074878B (zh) 2,3-二氢-噻唑并[3,2-a]吡啶-5-酮衍生物、其中间体及其作为抗细菌剂的用途
RU2721120C2 (ru) Новые гетероциклические соединения как ингибиторы brd4
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
JP2022060192A5 (hr)
RU2020114890A (ru) Кристаллическое промежуточное соединение, используемое для получения линаглиптина, и способ получения линаглиптина
AU2018354780A1 (en) Process for preparing benzothiophen-2yl boronate