JPWO2022051770A5 - - Google Patents
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- Publication number
- JPWO2022051770A5 JPWO2022051770A5 JP2023514771A JP2023514771A JPWO2022051770A5 JP WO2022051770 A5 JPWO2022051770 A5 JP WO2022051770A5 JP 2023514771 A JP2023514771 A JP 2023514771A JP 2023514771 A JP2023514771 A JP 2023514771A JP WO2022051770 A5 JPWO2022051770 A5 JP WO2022051770A5
- Authority
- JP
- Japan
- Prior art keywords
- salt
- crystal
- lumateperone
- free base
- lysine
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
- 150000003839 salts Chemical class 0.000 claims description 48
- 239000013078 crystal Substances 0.000 claims description 40
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims description 31
- 229950003467 lumateperone Drugs 0.000 claims description 30
- 239000012458 free base Substances 0.000 claims description 24
- 239000004472 Lysine Substances 0.000 claims description 21
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 12
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 12
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims description 11
- 235000018977 lysine Nutrition 0.000 claims description 11
- 235000019766 L-Lysine Nutrition 0.000 claims description 10
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 claims description 10
- VFQXVTODMYMSMJ-UHFFFAOYSA-N isonicotinamide Chemical compound NC(=O)C1=CC=NC=C1 VFQXVTODMYMSMJ-UHFFFAOYSA-N 0.000 claims description 9
- 238000000034 method Methods 0.000 claims description 7
- LBLYYCQCTBFVLH-UHFFFAOYSA-N 2-Methylbenzenesulfonic acid Chemical compound CC1=CC=CC=C1S(O)(=O)=O LBLYYCQCTBFVLH-UHFFFAOYSA-N 0.000 claims description 5
- 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 claims description 5
- 239000002253 acid Substances 0.000 claims description 4
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 239000003960 organic solvent Substances 0.000 claims description 4
- 102000019208 Serotonin Plasma Membrane Transport Proteins Human genes 0.000 claims description 3
- 108010012996 Serotonin Plasma Membrane Transport Proteins Proteins 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims description 2
- 230000002159 abnormal effect Effects 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 229960003638 dopamine Drugs 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims description 2
- 108020003175 receptors Proteins 0.000 claims description 2
- 102000005962 receptors Human genes 0.000 claims description 2
- 230000019491 signal transduction Effects 0.000 claims description 2
- PXHVJJICTQNCMI-UHFFFAOYSA-N Nickel Chemical compound [Ni] PXHVJJICTQNCMI-UHFFFAOYSA-N 0.000 claims 4
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims 2
- 229910052802 copper Inorganic materials 0.000 claims 2
- 239000010949 copper Substances 0.000 claims 2
- 229910052759 nickel Inorganic materials 0.000 claims 2
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 claims 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 claims 1
- 108010078791 Carrier Proteins Proteins 0.000 claims 1
- 102100029503 E3 ubiquitin-protein ligase TRIM32 Human genes 0.000 claims 1
- 101000634982 Homo sapiens E3 ubiquitin-protein ligase TRIM32 Proteins 0.000 claims 1
- 238000002441 X-ray diffraction Methods 0.000 description 5
- 238000004458 analytical method Methods 0.000 description 2
- 238000005160 1H NMR spectroscopy Methods 0.000 description 1
- 102100036321 5-hydroxytryptamine receptor 2A Human genes 0.000 description 1
- 101710138091 5-hydroxytryptamine receptor 2A Proteins 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 238000000113 differential scanning calorimetry Methods 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 238000002411 thermogravimetry Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063075019P | 2020-09-04 | 2020-09-04 | |
| US63/075,019 | 2020-09-04 | ||
| PCT/US2021/071366 WO2022051770A2 (en) | 2020-09-04 | 2021-09-03 | Novel salts, crystals, and co-crystals |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023540506A JP2023540506A (ja) | 2023-09-25 |
| JPWO2022051770A5 true JPWO2022051770A5 (https=) | 2024-09-11 |
| JP2023540506A5 JP2023540506A5 (https=) | 2024-09-11 |
Family
ID=80492079
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023514771A Pending JP2023540506A (ja) | 2020-09-04 | 2021-09-03 | 新規の塩、結晶および共結晶 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20230312573A1 (https=) |
| EP (1) | EP4208434A4 (https=) |
| JP (1) | JP2023540506A (https=) |
| KR (1) | KR20230104121A (https=) |
| CN (1) | CN116113622A (https=) |
| AU (1) | AU2021338439A1 (https=) |
| CA (1) | CA3186537A1 (https=) |
| IL (1) | IL300886A (https=) |
| MX (1) | MX2023002468A (https=) |
| WO (1) | WO2022051770A2 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL268970B2 (en) | 2017-03-24 | 2023-12-01 | Intra Cellular Therapies Inc | Oral transmucosal formulations of substituted heterocycle fused gamma carbolines |
| WO2019178484A1 (en) | 2018-03-16 | 2019-09-19 | Intra-Cellular Therapies, Inc. | Novel methods |
| US12414948B2 (en) | 2022-05-18 | 2025-09-16 | Intra-Cellular Therapies, Inc. | Methods |
| WO2025240804A1 (en) | 2024-05-16 | 2025-11-20 | Intra-Cellular Therapies, Inc. | Novel compositions, devices and methods |
| CN118566395B (zh) * | 2024-08-02 | 2024-10-25 | 则正(济南)生物科技有限公司 | 测定甲苯磺酸卢美哌隆口崩片中杂质含量的方法、应用和系统 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3407889T3 (pl) * | 2016-03-25 | 2021-11-22 | Intra-Cellular Therapies, Inc. | Związki organiczne i ich zastosowanie w leczeniu lub zapobieganiu zaburzeniom ośrodkowego układu nerwowego |
| 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 |
| IL268970B2 (en) * | 2017-03-24 | 2023-12-01 | Intra Cellular Therapies Inc | Oral transmucosal formulations of substituted heterocycle fused gamma carbolines |
| 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 |
| CN111107847A (zh) * | 2017-09-26 | 2020-05-05 | 细胞内治疗公司 | 新的盐和晶体 |
| IL321985A (en) * | 2018-06-06 | 2025-09-01 | Intra Cellular Therapies Inc | New salts and crystals |
| CA3106447A1 (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. | NOVEL COMPOSITIONS AND PROCESSES |
| US20220024924A1 (en) * | 2018-11-27 | 2022-01-27 | Teva Czech Industries S.R.O | Solid state forms of lumateperone salts and processes for preparation of lumateperone and salts thereof |
| JP7673040B2 (ja) * | 2019-07-07 | 2025-05-08 | イントラ－セルラー・セラピーズ・インコーポレイテッド | 新規方法 |
| EP4034119A4 (en) * | 2019-09-25 | 2023-10-18 | Intra-Cellular Therapies, Inc. | NOVEL METHODS |
-
2021
- 2021-09-03 WO PCT/US2021/071366 patent/WO2022051770A2/en not_active Ceased
- 2021-09-03 IL IL300886A patent/IL300886A/en unknown
- 2021-09-03 CA CA3186537A patent/CA3186537A1/en active Pending
- 2021-09-03 JP JP2023514771A patent/JP2023540506A/ja active Pending
- 2021-09-03 US US18/043,959 patent/US20230312573A1/en active Pending
- 2021-09-03 MX MX2023002468A patent/MX2023002468A/es unknown
- 2021-09-03 CN CN202180054461.5A patent/CN116113622A/zh active Pending
- 2021-09-03 KR KR1020237010822A patent/KR20230104121A/ko active Pending
- 2021-09-03 EP EP21865304.6A patent/EP4208434A4/en active Pending
- 2021-09-03 AU AU2021338439A patent/AU2021338439A1/en active Pending
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