JP2021504338A5 - - Google Patents
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- Publication number
- JP2021504338A5 JP2021504338A5 JP2020528129A JP2020528129A JP2021504338A5 JP 2021504338 A5 JP2021504338 A5 JP 2021504338A5 JP 2020528129 A JP2020528129 A JP 2020528129A JP 2020528129 A JP2020528129 A JP 2020528129A JP 2021504338 A5 JP2021504338 A5 JP 2021504338A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline
- crystalline form
- diffraction peaks
- ray powder
- powder diffraction
- 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.)
- Granted
Links
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 32
- 150000001875 compounds Chemical class 0.000 claims description 19
- 239000012458 free base Substances 0.000 claims description 19
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- 208000002903 Thalassemia Diseases 0.000 claims description 7
- 239000000203 mixture Substances 0.000 claims description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 5
- 208000007056 sickle cell anemia Diseases 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 3
- 208000007475 hemolytic anemia Diseases 0.000 claims description 3
- 238000002441 X-ray diffraction Methods 0.000 claims description 2
- 208000004622 abetalipoproteinemia Diseases 0.000 claims description 2
- 208000005980 beta thalassemia Diseases 0.000 claims description 2
- 230000001419 dependent effect Effects 0.000 claims description 2
- 210000003743 erythrocyte Anatomy 0.000 claims description 2
- 239000012453 solvate Substances 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 206010015150 Erythema Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 230000007812 deficiency Effects 0.000 claims 1
- 231100000321 erythema Toxicity 0.000 claims 1
- 230000000422 nocturnal effect Effects 0.000 claims 1
- 230000001314 paroxysmal effect Effects 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 238000000034 method Methods 0.000 description 22
- 239000013078 crystal Substances 0.000 description 5
- XOHUEYCVLUUEJJ-UHFFFAOYSA-N 2,3-Bisphosphoglyceric acid Chemical compound OP(=O)(O)OC(C(=O)O)COP(O)(O)=O XOHUEYCVLUUEJJ-UHFFFAOYSA-N 0.000 description 3
- 108700014121 Pyruvate Kinase Deficiency of Red Cells Proteins 0.000 description 3
- 239000007916 tablet composition Substances 0.000 description 3
- ZKHQWZAMYRWXGA-KQYNXXCUSA-J ATP(4-) Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP([O-])(=O)OP([O-])(=O)OP([O-])([O-])=O)[C@@H](O)[C@H]1O ZKHQWZAMYRWXGA-KQYNXXCUSA-J 0.000 description 2
- ZKHQWZAMYRWXGA-UHFFFAOYSA-N Adenosine triphosphate Natural products C1=NC=2C(N)=NC=NC=2N1C1OC(COP(O)(=O)OP(O)(=O)OP(O)(O)=O)C(O)C1O ZKHQWZAMYRWXGA-UHFFFAOYSA-N 0.000 description 2
- 0 CCCN(CC*)CC1CC1 Chemical compound CCCN(CC*)CC1CC1 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- 229930195725 Mannitol Natural products 0.000 description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 2
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 2
- 239000008108 microcrystalline cellulose Substances 0.000 description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 description 2
- MHQJUHSHQGQVTM-VHEBQXMUSA-N (e)-4-octadecoxy-4-oxobut-2-enoic acid Chemical compound CCCCCCCCCCCCCCCCCCOC(=O)\C=C\C(O)=O MHQJUHSHQGQVTM-VHEBQXMUSA-N 0.000 description 1
- 229920002785 Croscarmellose sodium Polymers 0.000 description 1
- 206010014490 Elliptocytosis hereditary Diseases 0.000 description 1
- 102000001554 Hemoglobins Human genes 0.000 description 1
- 108010054147 Hemoglobins Proteins 0.000 description 1
- 208000001825 Hereditary elliptocytosis Diseases 0.000 description 1
- 208000000733 Paroxysmal Hemoglobinuria Diseases 0.000 description 1
- 102100036050 Phosphatidylinositol N-acetylglucosaminyltransferase subunit A Human genes 0.000 description 1
- 108020005115 Pyruvate Kinase Proteins 0.000 description 1
- 102000013009 Pyruvate Kinase Human genes 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 229960001681 croscarmellose sodium Drugs 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 description 1
- -1 for example Proteins 0.000 description 1
- 208000009601 hereditary spherocytosis Diseases 0.000 description 1
- 201000003045 paroxysmal nocturnal hemoglobinuria Diseases 0.000 description 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023076364A JP2023093762A (ja) | 2017-11-22 | 2023-05-02 | Ｎ－（４－（４－（シクロプロピルメチル）ピペラジン－１－カルボニル）フェニル）キノリン－８－スルホンアミドの結晶性形態 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762589822P | 2017-11-22 | 2017-11-22 | |
| US62/589,822 | 2017-11-22 | ||
| US201862691709P | 2018-06-29 | 2018-06-29 | |
| US62/691,709 | 2018-06-29 | ||
| PCT/US2018/062197 WO2019104134A1 (en) | 2017-11-22 | 2018-11-21 | Crystalline forms of n-(4-(4-(cyclopropylmethyl) piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023076364A Division JP2023093762A (ja) | 2017-11-22 | 2023-05-02 | Ｎ－（４－（４－（シクロプロピルメチル）ピペラジン－１－カルボニル）フェニル）キノリン－８－スルホンアミドの結晶性形態 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021504338A JP2021504338A (ja) | 2021-02-15 |
| JP2021504338A5 true JP2021504338A5 (enExample) | 2021-12-02 |
| JPWO2019104134A5 JPWO2019104134A5 (enExample) | 2023-01-30 |
| JP7275130B2 JP7275130B2 (ja) | 2023-05-17 |
Family
ID=64734113
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020528129A Active JP7275130B2 (ja) | 2017-11-22 | 2018-11-21 | Ｎ－（４－（４－（シクロプロピルメチル）ピペラジン－１－カルボニル）フェニル）キノリン－８－スルホンアミドの結晶性形態 |
| JP2023076364A Withdrawn JP2023093762A (ja) | 2017-11-22 | 2023-05-02 | Ｎ－（４－（４－（シクロプロピルメチル）ピペラジン－１－カルボニル）フェニル）キノリン－８－スルホンアミドの結晶性形態 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023076364A Withdrawn JP2023093762A (ja) | 2017-11-22 | 2023-05-02 | Ｎ－（４－（４－（シクロプロピルメチル）ピペラジン－１－カルボニル）フェニル）キノリン－８－スルホンアミドの結晶性形態 |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US11254652B2 (enExample) |
| EP (2) | EP4285904A3 (enExample) |
| JP (2) | JP7275130B2 (enExample) |
| KR (3) | KR20250034202A (enExample) |
| CN (2) | CN111372920B (enExample) |
| AU (2) | AU2018373122B2 (enExample) |
| BR (1) | BR112020010185A2 (enExample) |
| CA (1) | CA3081945A1 (enExample) |
| DK (1) | DK3713919T3 (enExample) |
| ES (1) | ES2959764T3 (enExample) |
| FI (1) | FI3713919T3 (enExample) |
| HR (1) | HRP20230931T1 (enExample) |
| HU (1) | HUE063264T2 (enExample) |
| IL (3) | IL305343B1 (enExample) |
| LT (1) | LT3713919T (enExample) |
| MD (1) | MD3713919T2 (enExample) |
| MX (2) | MX2020005348A (enExample) |
| PH (1) | PH12020550644A1 (enExample) |
| PL (1) | PL3713919T3 (enExample) |
| PT (1) | PT3713919T (enExample) |
| RS (1) | RS64592B1 (enExample) |
| SG (1) | SG11202004587XA (enExample) |
| SI (1) | SI3713919T1 (enExample) |
| SM (1) | SMT202300327T1 (enExample) |
| TW (2) | TW202334115A (enExample) |
| UA (1) | UA127502C2 (enExample) |
| WO (1) | WO2019104134A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2944788C (en) * | 2009-06-29 | 2023-08-22 | Agios Pharmaceuticals, Inc. | Compounds, and compositions thereof, which modulate pyruvate kinase m2, and methods of making same |
| DK3448859T3 (da) | 2017-03-20 | 2019-09-23 | Forma Therapeutics Inc | Pyrrolopyrrolsammensætninger som pyruvatkinase- (pkr) aktivatorer |
| WO2020061378A1 (en) | 2018-09-19 | 2020-03-26 | Forma Therapeutics, Inc. | Treating sickle cell disease with a pyruvate kinase r activating compound |
| JP7450610B2 (ja) | 2018-09-19 | 2024-03-15 | ノヴォ・ノルディスク・ヘルス・ケア・アーゲー | ピルビン酸キナーゼｒの活性化 |
| WO2020237047A1 (en) * | 2019-05-22 | 2020-11-26 | Agios Pharmaceuticals, Inc. | Crystalline salt forms of n-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide |
| US11878049B1 (en) | 2019-06-14 | 2024-01-23 | Agios Pharmaceuticals, Inc. | Mitapivat therapy and modulators of cytochrome P450 |
| MX2022003254A (es) | 2019-09-19 | 2022-04-18 | Forma Therapeutics Inc | Composiciones activadoras de piruvato cinasa r (pkr). |
| US12286404B2 (en) * | 2020-01-28 | 2025-04-29 | Teva Pharmaceuticals International Gmbh | Solid state forms of Mitapivat and process for preparation thereof |
| EP4216956A1 (en) | 2020-09-25 | 2023-08-02 | Agios Pharmaceuticals, Inc. | Pharmaceutical formulation |
| CN116568281A (zh) * | 2020-09-25 | 2023-08-08 | 安吉奥斯医药品有限公司 | 药物制剂 |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
| WO2022231627A1 (en) | 2021-04-30 | 2022-11-03 | Agios Pharmaceuticals, Inc. | Methods for titrating mitapivat for use in treating thalassemia |
| KR20240004620A (ko) | 2021-04-30 | 2024-01-11 | 아지오스 파마슈티컬스 아이엔씨. | 미타피바트를 적정하는 방법 |
| WO2023154036A1 (en) | 2022-02-08 | 2023-08-17 | Agios Pharmaceuticals, Inc. | Methods for titrating mitapivat |
| EP4147700A1 (en) * | 2021-09-08 | 2023-03-15 | LQT Therapeutics Inc. | N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides for use in the treatment of sickle cell disease |
| EP4433057A1 (en) | 2021-11-16 | 2024-09-25 | Agios Pharmaceuticals, Inc. | Compounds for treating mds-associated anemias and other conditions |
| WO2024084501A1 (en) | 2022-10-17 | 2024-04-25 | Mylan Laboratories Limited | Crystalline polymorphs of mitapivat and mitapivat hemisulfate |
| ES2975743A1 (es) * | 2022-11-22 | 2024-07-12 | Moehs Iberica Sl | Metodo de preparacion de mitapivat, intermedios de sintesis de mitapivat y metodos de preparacion de los mismos |
| WO2024228131A1 (en) * | 2023-05-02 | 2024-11-07 | Biophore India Pharmaceuticals Pvt. Ltd | Solid forms of 8-quinoline sulfonamide, n-[4-[[4(cyclopropylmethyl)-1-piperazinyl] carbonyl] phenyl]-sulfate and its process for preparation thereof |
| WO2025008787A1 (en) * | 2023-07-05 | 2025-01-09 | Biophore India Pharmaceuticals Pvt. Ltd | Solid forms of mitapivat hemisulfate |
| WO2025083627A1 (en) * | 2023-10-18 | 2025-04-24 | Apitoria Pharma Private Limited | Novel crystalline forms of mitapivat sulfate and processes for preparation |
| WO2025146636A1 (en) * | 2024-01-03 | 2025-07-10 | Tianish Laboratories Private Limited | Novel crystalline polymorphs of mitapivat sulfate salt |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN191496B (enExample) | 1999-07-30 | 2003-12-06 | Ranbaxy Lab Ltd | |
| GB2383042A (en) | 2001-10-18 | 2003-06-18 | Cipla Ltd | Amorphous alendronate sodium |
| CA2944788C (en) | 2009-06-29 | 2023-08-22 | Agios Pharmaceuticals, Inc. | Compounds, and compositions thereof, which modulate pyruvate kinase m2, and methods of making same |
| KR101873543B1 (ko) | 2011-05-03 | 2018-07-02 | 아지오스 파마슈티컬스 아이엔씨. | 치료에 사용하기 위한 피루베이트 키나아제 활성제 |
| WO2013056153A1 (en) * | 2011-10-13 | 2013-04-18 | Kung Charles | Activators of pyruvate kinase m2 and methods of treating disease |
| WO2014018851A1 (en) * | 2012-07-26 | 2014-01-30 | Joslin Diabetes Center, Inc. | Predicting and treating diabetic complications |
| JP6362601B2 (ja) | 2012-09-18 | 2018-07-25 | 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． | 小胞モノアミン輸送体２の重水素化ベンゾキノリン阻害剤の製剤薬物動態 |
| DK3307271T3 (da) | 2015-06-11 | 2023-10-09 | Agios Pharmaceuticals Inc | Fremgangsmåder til anvendelse af pyruvatkinase-aktivatorer |
-
2018
- 2018-11-21 PL PL18821779.8T patent/PL3713919T3/pl unknown
- 2018-11-21 IL IL305343A patent/IL305343B1/en unknown
- 2018-11-21 EP EP23186155.0A patent/EP4285904A3/en active Pending
- 2018-11-21 KR KR1020257007025A patent/KR20250034202A/ko active Pending
- 2018-11-21 MD MDE20200988T patent/MD3713919T2/ro unknown
- 2018-11-21 AU AU2018373122A patent/AU2018373122B2/en active Active
- 2018-11-21 EP EP18821779.8A patent/EP3713919B1/en active Active
- 2018-11-21 KR KR1020207015018A patent/KR102682430B1/ko active Active
- 2018-11-21 JP JP2020528129A patent/JP7275130B2/ja active Active
- 2018-11-21 CA CA3081945A patent/CA3081945A1/en active Pending
- 2018-11-21 ES ES18821779T patent/ES2959764T3/es active Active
- 2018-11-21 TW TW112118933A patent/TW202334115A/zh unknown
- 2018-11-21 KR KR1020247022172A patent/KR102777452B1/ko active Active
- 2018-11-21 RS RS20230793A patent/RS64592B1/sr unknown
- 2018-11-21 CN CN201880075099.8A patent/CN111372920B/zh active Active
- 2018-11-21 IL IL322576A patent/IL322576A/en unknown
- 2018-11-21 HU HUE18821779A patent/HUE063264T2/hu unknown
- 2018-11-21 SM SM20230327T patent/SMT202300327T1/it unknown
- 2018-11-21 MX MX2020005348A patent/MX2020005348A/es unknown
- 2018-11-21 US US16/765,456 patent/US11254652B2/en active Active
- 2018-11-21 IL IL274488A patent/IL274488B2/en unknown
- 2018-11-21 SI SI201830984T patent/SI3713919T1/sl unknown
- 2018-11-21 PT PT188217798T patent/PT3713919T/pt unknown
- 2018-11-21 WO PCT/US2018/062197 patent/WO2019104134A1/en not_active Ceased
- 2018-11-21 HR HRP20230931TT patent/HRP20230931T1/hr unknown
- 2018-11-21 UA UAA202003680A patent/UA127502C2/uk unknown
- 2018-11-21 LT LTEPPCT/US2018/062197T patent/LT3713919T/lt unknown
- 2018-11-21 FI FIEP18821779.8T patent/FI3713919T3/fi active
- 2018-11-21 TW TW107141542A patent/TWI808108B/zh active
- 2018-11-21 CN CN202311301795.5A patent/CN117551030A/zh active Pending
- 2018-11-21 DK DK18821779.8T patent/DK3713919T3/da active
- 2018-11-21 BR BR112020010185-0A patent/BR112020010185A2/pt unknown
- 2018-11-21 SG SG11202004587XA patent/SG11202004587XA/en unknown
-
2020
- 2020-05-15 PH PH12020550644A patent/PH12020550644A1/en unknown
- 2020-07-13 MX MX2022009998A patent/MX2022009998A/es unknown
-
2022
- 2022-01-14 US US17/575,898 patent/US20220220093A1/en active Pending
-
2023
- 2023-05-02 JP JP2023076364A patent/JP2023093762A/ja not_active Withdrawn
-
2024
- 2024-02-06 AU AU2024200724A patent/AU2024200724A1/en active Pending
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