HRP20211666T1 - Oblici soli lumateperon ditozilata u krutom stanju - Google Patents
Oblici soli lumateperon ditozilata u krutom stanju Download PDFInfo
- Publication number
- HRP20211666T1 HRP20211666T1 HRP20211666TT HRP20211666T HRP20211666T1 HR P20211666 T1 HRP20211666 T1 HR P20211666T1 HR P20211666T T HRP20211666T T HR P20211666TT HR P20211666 T HRP20211666 T HR P20211666T HR P20211666 T1 HRP20211666 T1 HR P20211666T1
- Authority
- HR
- Croatia
- Prior art keywords
- lumateperone
- theta
- degrees
- ditosylate
- less
- Prior art date
Links
- HOIIHACBCFLJET-SFTDATJTSA-N 4-((6br,10as)-3-methyl-2,3,6b,9,10,10a-hexahydro-1h-pyrido-[3',4':4,5]-pyrrolo[1,2,3-de]quinoxalin-8-(7h)-yl)-1-(4-fluorophenyl)-1-butanone Chemical compound C([C@@H]1N2CCN(C=3C=CC=C(C2=3)[C@@H]1C1)C)CN1CCCC(=O)C1=CC=C(F)C=C1 HOIIHACBCFLJET-SFTDATJTSA-N 0.000 title claims 30
- 229950003467 lumateperone Drugs 0.000 title claims 30
- 239000007787 solid Substances 0.000 title claims 12
- 150000003839 salts Chemical class 0.000 title 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 20
- 239000000203 mixture Substances 0.000 claims 14
- 238000000034 method Methods 0.000 claims 6
- 239000002904 solvent Substances 0.000 claims 6
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 claims 6
- LHAPOGAFBLSJJQ-GUTACTQSSA-N iti007 Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1.C([C@@H]1N2CCN(C=3C=CC=C(C2=3)[C@@H]1C1)C)CN1CCCC(=O)C1=CC=C(F)C=C1 LHAPOGAFBLSJJQ-GUTACTQSSA-N 0.000 claims 5
- 239000000825 pharmaceutical preparation Substances 0.000 claims 5
- 238000000634 powder X-ray diffraction Methods 0.000 claims 5
- 238000003756 stirring Methods 0.000 claims 5
- 239000012296 anti-solvent Substances 0.000 claims 4
- 238000001460 carbon-13 nuclear magnetic resonance spectrum Methods 0.000 claims 4
- 239000013078 crystal Substances 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 150000001335 aliphatic alkanes Chemical class 0.000 claims 2
- 150000001924 cycloalkanes Chemical class 0.000 claims 2
- 150000002170 ethers Chemical class 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 238000001157 Fourier transform infrared spectrum Methods 0.000 claims 1
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 1
- 238000010521 absorption reaction Methods 0.000 claims 1
- -1 aliphatic ethers Chemical class 0.000 claims 1
- 230000003542 behavioural effect Effects 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 238000002955 isolation Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000002156 mixing Methods 0.000 claims 1
- 150000004682 monohydrates Chemical class 0.000 claims 1
- 239000003960 organic solvent Substances 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 239000011877 solvent mixture Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 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
- C07D471/12—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 three hetero rings
- C07D471/16—Peri-condensed systems
-
- 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
- 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
- C07D471/06—Peri-condensed systems
-
- 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)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Saccharide Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (15)
1. Oblik lumateperon ditozilata u krutom stanju, odabran od:
(A) kristalnog oblika lumateperon ditozilata označenog kao oblik F1, naznačen time što ima podatke odabrane između jednog ili više od sljedećeg:
(i) XRPD uzorak koji ima vrhove na: 4.2, 6.3, 10.4, 14.6 i 18.7 stupnjeva dva theta ± 0.2 stupnjeva dva theta; i također odsutnost jednog, dva, tri ili četiri vrha odabrana od: 11.4, 13.4,17.5 i 23.5 stupnjeva dva theta ± 0.2 stupnjeva dva theta, po izboru uglavnom kao što je prikazano na slici 2, ili Figure 8 ili Figure 9;
(ii) XRPD uzorak koji ima vrhove na: 4.2, 6.3, 10.4, 14.6 i 18.7 stupnjeva dva theta ± 0.2 stupnjeva dva theta; i također odsutnost vrha na 5.7 stupnjeva dva theta ± 0.2 stupnjeva dva theta, po izboru uglavnom kao što je prikazano na slici 2, ili slici 8 ili slici 9:
[image]
[image]
(iii) spektar 13C NMR u krutom stanju koji ima vrhove pri 142.6, 141.0, 133.8, 129.5 i 123.2 ppm ± 0.2 ppm i također odsutnost jednog, dva, tri ili četiri vrha odabrana od: 194.5, 110.2, 62.2 i 35.7 ppm ± 0.2 ppm, po izboru uglavnom kao što je prikazano na slici 4, 5 ili 6:
[image]
[image]
ili
(B) kristalnog oblika lumateperon ditozilata označenog kao oblik F1, pri čemu oblik F1 sadrži: 20% ili manje, 10% ili manje, 5% ili manje, 2% ili manje, ili 1% (m/m) ili manje bilo kojeg drugog krutog oblika lumateperon tozilata ili lumateperon ditozilata,
koji je naznačen time što ima podatke odabrane između jednog ili više od sljedećeg:
(i) uzorak difrakcije rendgenskih zraka na prahu koji ima vrhove na: 4.2, 6.3, 10.4, 14.6 i 18.7 stupnjeva dva theta ± 0.2 stupnjeva dva theta;
(ii) XRPD uzorak koji ima vrhove na: 4.2, 6.3, 10.4, 14.6 i 18.7 stupnjeva dva theta ± 0.2 stupnjeva dva theta i također ima jedan, dva, tri, četiri ili pet vrhova odabranih od: 15.4, 20.4, 21.3, 24.0 i 25.1 stupnjeva dva theta ± 0.2 stupnjeva dva theta;
(iii) spektar 13C NMR u krutom stanju koji ima vrhove pri 142.6, 141.0, 133.8, 129.5 i 123.2 ppm ± 0.2 ppm; i
(iv) spektar 13C NMR u krutom stanju koji ima sljedeće apsolutne razlike kemijskog pomaka u odnosu na referentni vrh pri 64.0 ppm ± 2 ppm od 78.6, 77.0, 69.8, 65.5 i 59.2 ppm ± 0.1 ppm.
2. Kristalni oblik F1 lumateperon ditozilata prema patentnom zahtjevu 1(A) nadalje naznačen time što ima jedno ili više od slijedećih:
(i) uzorak difrakcije rendgenskih zraka na prahu koji ima vrhove na: 4.2, 6.3, 10.4, 14.6 i 18.7 stupnjeva dva theta ± 0.2 stupnjeva dva theta i također ima jedan, dva, tri, četiri ili pet vrhova odabranih od: 15.4, 20.4, 21.3, 24.0 i 25.1 stupnjeva dva theta ± 0.2 stupnjeva dva theta;
(ii) spektar 13C NMR u krutom stanju koji ima sljedeće apsolutne razlike kemijskog pomaka u odnosu na referentni vrh pri 64.0 ppm ± 2 ppm od 78.6, 77.0, 69.8, 65.5 i 59.2 ppm ± 0.1 ppm.
3. Kristalni oblik F1 lumateperon ditozilata prema patentnom zahtjevu 1 ili zahtjevu 2 nadalje naznačen time što ima FT-IR spektar s apsorpcijom na 2617, 1632, 1480, 1280, 1210, 1163, 1104, 1004, 824, 750 cm-1 ± 2 cm-1.
4. Kristalni oblik F1 prema bilo kojem od patentnih zahtjeva 1(A), 2 ili 3 naznačen time što kristalni oblik F1 sadrži: 20% ili manje, 10% ili manje, 5% ili manje, 2% ili manje, ili 1% (m/m) ili manje bilo kojeg drugog čvrstog oblika lumateperon tozilata ili lumateperon ditozilata, poželjno pri čemu je kristalni oblik uglavnom slobodan oblik A lumateperon tozilata, pri čemu oblik A ima karakteristične vrhove na: 5.7, 11.4 i/ili 13.4 stupnjeva dva theta ± 0.2 stupnjeva dva theta.
5. Kristalni oblik F1 prema bilo kojem od patentnih zahtjeva 1-4 naznačen time što je kristalni oblik izoliran.
6. Upotreba oblika u krutom stanju lumateperon ditozilata prema bilo kojem od patentnih zahtjeva 1-5 za pripremu farmaceutskog pripravka koji sadrži lumateperon ditozilat.
7. Postupak za pripremu kristalnog oblika F1 lumateperon ditozilata kako je definiran u bilo kojem od zahtjeva 1-5, poželjno pri čemu oblik F1 sadrži: 20% ili manje, 10% ili manje, 5% ili manje, 2% ili manje, ili 1% (m/m) ili manje bilo kojeg drugog oblika u krutom stanju lumateperon tozilata/ditozilata, ili pri čemu oblik F1 sadrži: manje od 20 mas.%, manje od 10 mas.%, manje od 5 mas.%, manje od 2 mas.%, ili manje od 1 mas.% oblika A lumateperon tozilata, pri čemu oblik A ima karakteristične vrhove na: 5.7, 11.4 i/ili 13.4 stupnjeva dva theta ± 0.2 stupnjeva dva theta, koji sadrži:
a) osiguravanje:
i) smjese lumateperona i najmanje 2 ekvivalenta p-toluen sulfonske kiseline; ili
ii) smjese lumateperon monotozilata i najmanje 1 ekvivalent p-toluen sulfonske kiseline;
pri čemu je smjesa (i) ili (ii) predviđena u sustavu otapala koji po izboru sadrži vodu, poželjno pri čemu je smjesa u koraku (a) otopina
i provođenje jednog ili više od sljedećih koraka (b)-(f) pri čemu se koraci (b), (c), (d) i (e) mogu izvesti bilo kojim redoslijedom:
b) miješanje
c) hlađenje
d) koncentriranje i/ili
e) dodavanje anti-otapala, i
f) po izboru izoliranje lumateperon ditozilata oblika F1;
pri čemu sustav otapala u koraku (a) sadrži jedan ili više od metanola, etanola, THF, 1,4-dioksan, ili metil etil keton.
8. Postupak prema patentnom zahtjevu 7 naznačen time što se anti-otapalo u koraku (e) bira iz skupine koju čine eteri, poželjno alifatski eteri, poželjnije C4-C8 eteri, alkani, poželjno C3-C8 alkani, i cikloalkani, poželjno C5-C10 cikloalkani, pri čemu je poželjnije anti-otapalo MTBE ili heptan.
9. Postupak prema patentnom zahtjevu 7, naznačen time što sadrži jedan od (A) do (D):
(A) osiguravanje smjese lumateperon monotozilata i najmanje 1 ekvivalenta p-toluen sulfonske kiseline u smjesi otapala koja sadrži dva organska otapala, miješanje smjese tijekom odgovarajućeg vremenskog perioda, i izoliranje kristalnog oblika F1 lumateperon ditozilata;
(B) osiguravanje smjese lumateperona i najmanje 2 ekvivalenta p-toluensulfonske kiseline, u najmanje jednom otapalu tako da nastane otopine, miješanje smjese tijekom odgovarajućeg vremenskog perioda, koncentriranje, po izboru trituriranje s odgovarajućim otapalom, i izoliranje kristalnog oblika F1 lumateperon ditozilata;
(C) osiguravanje smjese lumateperon monotozilata i najmanje 1 ekvivalent p-toluen sulfonske kiseline u otapalu, po izboru zagrijavanje, miješanje smjese tijekom odgovarajućeg vremenskog perioda, i izoliranje kristalnog oblika F1 lumateperon ditozilata; ili
(D) osiguravanje smjese lumateperon monotozilata i najmanje 1 ekvivalent p-toluen sulfonske kiseline u otapalu, dodavanje anti-otapala, miješanje smjese tijekom odgovarajućeg vremenskog perioda, i izoliranje kristalnog oblika F1 lumateperon ditozilata.
10. Postupak prema bilo kojem od patentnih zahtjeva 7-9 naznačen time što se p-toluensulfonska kiselina koristi u obliku monohidrata.
11. Postupak prema bilo kojem od patentnih zahtjeva 7-10, naznačen time što se smjesa lumateperona i najmanje 2 ekvivalenta p-toluensulfonske kiseline ili smjesa lumateperon monotozilata i najmanje 1 ekvivalenta p-toluen sulfonske kiseline priprema u obrocima ili kap po kap dodavanjem p-toluensulfonske kiseline u lumateperon ili lumateperon monotozilat, poželjno uz miješanje.
12. Postupak prema bilo kojem od patentnih zahtjeva 7-11, naznačen time što nadalje sadrži kombiniranje kristalnog oblika F1 lumateperon ditozilata s najmanje jednom farmaceutski prihvatljivom pomoćnom tvari da se dobije farmaceutski pripravak.
13. Farmaceutski pripravak naznačen time što sadrži oblike u čvrstom stanju lumateperon ditozilata prema bilo kojem od patentnih zahtjeva 1-5.
14. Postupak za pripremu farmaceutskog pripravka prema patentnom zahtjevu 13 naznačen time što sadrži kombiniranje krutih oblika lumateperon ditozilata prema bilo kojem od patentnih zahtjeva 1-5 s najmanje jednom farmaceutski prihvatljivom pomoćnom tvari.
15. Kristalni oblik lumateperon ditozilata prema bilo kojem od patentnih zahtjeva 1-5 ili farmaceutski pripravak prema patentnom zahtjevu 13 za upotrebu u terapiji, poželjno za upotrebu u liječenju poremećaja središnjeg živčanog sustava, poželjno pri čemu je poremećaj odabran od jednog ili više od: shizofrenije, bipolarnog poremećaja, depresije, spavanja i poremećaja ponašanja kod demencije, autizma i drugih neuropsihijatrijskih poremećaja.
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662372553P | 2016-08-09 | 2016-08-09 | |
| US201662382479P | 2016-09-01 | 2016-09-01 | |
| US201662382977P | 2016-09-02 | 2016-09-02 | |
| US201662400358P | 2016-09-27 | 2016-09-27 | |
| US201762486554P | 2017-04-18 | 2017-04-18 | |
| EP17754571.2A EP3497104B1 (en) | 2016-08-09 | 2017-08-08 | Solid state forms of lumateperone ditosylate salt |
| PCT/US2017/045877 WO2018031535A1 (en) | 2016-08-09 | 2017-08-08 | Solid state forms of lumateperone ditosylate salt |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20211666T1 true HRP20211666T1 (hr) | 2022-02-18 |
Family
ID=59656224
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20211666TT HRP20211666T1 (hr) | 2016-08-09 | 2017-08-08 | Oblici soli lumateperon ditozilata u krutom stanju |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US11332469B2 (hr) |
| EP (2) | EP4001281A1 (hr) |
| ES (1) | ES2901375T3 (hr) |
| HR (1) | HRP20211666T1 (hr) |
| HU (1) | HUE057055T2 (hr) |
| IL (1) | IL264521A (hr) |
| PL (1) | PL3497104T3 (hr) |
| SI (1) | SI3497104T1 (hr) |
| WO (1) | WO2018031535A1 (hr) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE057055T2 (hu) * | 2016-08-09 | 2022-04-28 | Teva Pharmaceuticals Int Gmbh | Lumateperon-ditozilátsó szilárd halmazállapotú formái |
| EP3525763A4 (en) | 2016-10-12 | 2020-06-17 | Intra-Cellular Therapies, Inc. | AMORPHE FIXED DISPERSIONS |
| CN116327770A (zh) | 2017-03-24 | 2023-06-27 | 细胞内治疗公司 | 新组合物和方法 |
| JP2020513023A (ja) | 2017-04-10 | 2020-04-30 | ドクター・レディーズ・ラボラトリーズ・リミテッド | ルマテペロンｐ−トシラートの非晶質形態および固体分散体 |
| US11440911B2 (en) | 2017-09-26 | 2022-09-13 | Intra-Cellular Therapies, Inc. | Salts and crystals |
| WO2019102240A1 (en) * | 2017-11-27 | 2019-05-31 | Egis Gyógyszergyár Zrt. | Method for the manufacture of lumateperone and its salts |
| WO2019178484A1 (en) * | 2018-03-16 | 2019-09-19 | Intra-Cellular Therapies, Inc. | Novel methods |
| CA3102848A1 (en) * | 2018-06-06 | 2019-12-12 | Intra-Cellular Therapies, Inc. | Novel salts and crystals |
| WO2019241278A1 (en) * | 2018-06-11 | 2019-12-19 | Intra-Cellular Therapies, Inc. | Substituted heterocycle fused gamma-carbolines synthesis |
| EP3843739A4 (en) * | 2018-08-31 | 2022-06-01 | Intra-Cellular Therapies, Inc. | NEW METHODS |
| BR112021003655A2 (pt) * | 2018-08-31 | 2021-05-18 | Intra-Cellular Therapies, Inc. | métodos novos |
| WO2020112941A2 (en) | 2018-11-27 | 2020-06-04 | Teva Czech Industries S.R.O | Solid state forms of lumateperone salts and processes for preparation of lumateperone and salts thereof |
| CN113473988A (zh) * | 2018-12-14 | 2021-10-01 | 细胞内治疗公司 | 无定形固体分散体 |
| EP4134101A1 (en) * | 2019-07-07 | 2023-02-15 | Intra-Cellular Therapies, Inc. | Deuterated lumateperone for the treatment of the bipolar ii disorder |
| WO2022195500A1 (en) * | 2021-03-16 | 2022-09-22 | Ami Organics Ltd. | A process for the preparation of lumateperone tosylate intermediate |
| WO2024030835A2 (en) * | 2022-07-30 | 2024-02-08 | Intra-Cellular Therapies, Inc. | Novel salts and crystals |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008112280A1 (en) | 2007-03-12 | 2008-09-18 | Intra-Cellular Therapies, Inc. | Substituted heterocycle fused gamma-carbolines synthesis |
| CN105237536A (zh) | 2008-03-12 | 2016-01-13 | 细胞内治疗公司 | 取代的杂环稠合的γ-咔啉固体 |
| WO2012071425A1 (en) | 2010-11-22 | 2012-05-31 | Teva Pharmaceutical Industries Ltd. | Solid state forms of sorafenib besylate, and processes for preparations thereof |
| US10654854B2 (en) | 2016-03-28 | 2020-05-19 | Intra-Cellular Therapies, Inc. | Salts and crystals of ITI-007 |
| US11014925B2 (en) | 2016-03-28 | 2021-05-25 | Intra-Cellular Therapies, Inc. | Co-crystals of 1-(4-fluoro-phenyl)-4-((6bR,1OaS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H- pyrido[3′,4′:4,51_pyrrolo [1,2,3-delqcuinoxalin-8-yl)-butan-1-one with nicotinamide or isonicotinamide |
| HUE057055T2 (hu) * | 2016-08-09 | 2022-04-28 | Teva Pharmaceuticals Int Gmbh | Lumateperon-ditozilátsó szilárd halmazállapotú formái |
| CN116327770A (zh) | 2017-03-24 | 2023-06-27 | 细胞内治疗公司 | 新组合物和方法 |
| WO2019102240A1 (en) | 2017-11-27 | 2019-05-31 | Egis Gyógyszergyár Zrt. | Method for the manufacture of lumateperone and its salts |
| CA3102848A1 (en) | 2018-06-06 | 2019-12-12 | Intra-Cellular Therapies, Inc. | Novel salts and crystals |
| WO2019241278A1 (en) | 2018-06-11 | 2019-12-19 | Intra-Cellular Therapies, Inc. | Substituted heterocycle fused gamma-carbolines synthesis |
| EP3843729A4 (en) | 2018-08-29 | 2022-06-01 | Intra-Cellular Therapies, Inc. | NEW COMPOSITIONS AND METHODS |
| BR112021003655A2 (pt) | 2018-08-31 | 2021-05-18 | Intra-Cellular Therapies, Inc. | métodos novos |
| EP3843739A4 (en) | 2018-08-31 | 2022-06-01 | Intra-Cellular Therapies, Inc. | NEW METHODS |
| WO2020112941A2 (en) | 2018-11-27 | 2020-06-04 | Teva Czech Industries S.R.O | Solid state forms of lumateperone salts and processes for preparation of lumateperone and salts thereof |
-
2017
- 2017-08-08 HU HUE17754571A patent/HUE057055T2/hu unknown
- 2017-08-08 US US16/323,939 patent/US11332469B2/en active Active
- 2017-08-08 WO PCT/US2017/045877 patent/WO2018031535A1/en unknown
- 2017-08-08 SI SI201730962T patent/SI3497104T1/sl unknown
- 2017-08-08 ES ES17754571T patent/ES2901375T3/es active Active
- 2017-08-08 HR HRP20211666TT patent/HRP20211666T1/hr unknown
- 2017-08-08 PL PL17754571T patent/PL3497104T3/pl unknown
- 2017-08-08 EP EP21200789.2A patent/EP4001281A1/en active Pending
- 2017-08-08 EP EP17754571.2A patent/EP3497104B1/en active Active
-
2019
- 2019-01-29 IL IL264521A patent/IL264521A/en unknown
-
2022
- 2022-01-07 US US17/570,502 patent/US11760757B2/en active Active
-
2023
- 2023-08-14 US US18/233,390 patent/US20230382914A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US11760757B2 (en) | 2023-09-19 |
| SI3497104T1 (sl) | 2021-12-31 |
| US11332469B2 (en) | 2022-05-17 |
| EP3497104A1 (en) | 2019-06-19 |
| PL3497104T3 (pl) | 2022-02-21 |
| US20190211015A1 (en) | 2019-07-11 |
| HUE057055T2 (hu) | 2022-04-28 |
| EP3497104B1 (en) | 2021-10-06 |
| IL264521A (en) | 2019-05-30 |
| US20230382914A1 (en) | 2023-11-30 |
| ES2901375T3 (es) | 2022-03-22 |
| US20220127268A1 (en) | 2022-04-28 |
| EP4001281A1 (en) | 2022-05-25 |
| WO2018031535A1 (en) | 2018-02-15 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20211666T1 (hr) | Oblici soli lumateperon ditozilata u krutom stanju | |
| AU2021286276B2 (en) | Compositions and methods for phosphoramidite and oligonucleotide synthesis | |
| ES2965746T3 (es) | Procesos para producir brivaracetam | |
| HRP20210675T1 (hr) | Mono- ili di-supstituirani derivati indola kao inhibitori replikacije denga virusa | |
| ES2585396T3 (es) | Alquilamidas como inhibidores de la unión del VIH | |
| CN107849037A (zh) | 用于治疗和预防乙型肝炎病毒感染的新的三环4‑吡啶酮‑3‑甲酸衍生物 | |
| GB2542881A8 (en) | Crystal forms of ß-nicotinamide mononucleotide | |
| CA2995997A1 (en) | Compounds and compositions useful for treating disorders related to ntrk | |
| JP2018520205A5 (hr) | ||
| JP2016510758A5 (hr) | ||
| HRP20210667T1 (hr) | Kristalni oblici antagonista androgenog receptora, postupak pripreme i njihova upotreba | |
| JP2016027050A5 (hr) | ||
| CN106470975A (zh) | 多环氨基甲酰基吡啶酮化合物的合成 | |
| AR078475A1 (es) | Procedimiento para preparar una forma cristalina | |
| HRP20210551T1 (hr) | Postupak kristalizacije derivata aripiprazola u formulacijama sa produženim oslobađanjem za liječenje shizofrenije | |
| CL2008003577A1 (es) | Compuestos derivados de imidazo[1,5-a] pirido[3,2-e]pirazina, 2, 6, 7, 9 tetrasustituidos; inhibidores de fosfodiesterasa 10; procedimiento de preparación; composición farmacéutica que comprende a dichos compuestos; y su uso para tratar enfermedades relacionadas con el sistema nervioso central, obesidad y trastornos del metabolismo. | |
| ECSP13012891A (es) | Derivados de heteroarilo como moduladores de nachr alfa 7 | |
| CN107556244A (zh) | 并环化合物、其药物组合物及应用 | |
| HRP20201470T1 (hr) | Oblici soli nilotiniba u krutom stanju | |
| HRP20210503T1 (hr) | Kristalni oblici soli tapentadola i postupci za njihovu pripremu | |
| JP2017537095A (ja) | シス及びトランスリッチなｍｄａｃｈ（２，４−及び／又は２，６−ジアミノ−１−メチルシクロヘキサン）を製造する方法 | |
| WO2015198232A1 (en) | Fused triterpene compounds and uses thereof | |
| CN104119297B (zh) | 一种精制哌嗪的方法 | |
| JP2016525529A5 (hr) | ||
| Torres-Gómez et al. | Design, synthesis and receptor affinity of novel conformationally restricted σ ligands based on the [4.3. 3] propellane scaffold |