JP7275130B2 - 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 - Google Patents
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 Download PDFInfo
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- JP7275130B2 JP7275130B2 JP2020528129A JP2020528129A JP7275130B2 JP 7275130 B2 JP7275130 B2 JP 7275130B2 JP 2020528129 A JP2020528129 A JP 2020528129A JP 2020528129 A JP2020528129 A JP 2020528129A JP 7275130 B2 JP7275130 B2 JP 7275130B2
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/36—Sulfur atoms
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Quinoline Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2021504338A JP2021504338A (ja) | 2021-02-15 |
| JP2021504338A5 JP2021504338A5 (https=) | 2023-01-30 |
| JP7275130B2 true 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 (https=) |
| EP (2) | EP3713919B1 (https=) |
| JP (2) | JP7275130B2 (https=) |
| KR (3) | KR102777452B1 (https=) |
| CN (2) | CN117551030A (https=) |
| AU (2) | AU2018373122B2 (https=) |
| BR (1) | BR112020010185A2 (https=) |
| CA (1) | CA3081945A1 (https=) |
| DK (1) | DK3713919T3 (https=) |
| ES (1) | ES2959764T3 (https=) |
| FI (1) | FI3713919T3 (https=) |
| HR (1) | HRP20230931T1 (https=) |
| HU (1) | HUE063264T2 (https=) |
| IL (3) | IL274488B2 (https=) |
| LT (1) | LT3713919T (https=) |
| MD (1) | MD3713919T2 (https=) |
| MX (2) | MX2020005348A (https=) |
| PH (1) | PH12020550644A1 (https=) |
| PL (1) | PL3713919T3 (https=) |
| PT (1) | PT3713919T (https=) |
| RS (1) | RS64592B1 (https=) |
| SG (1) | SG11202004587XA (https=) |
| SI (1) | SI3713919T1 (https=) |
| SM (1) | SMT202300327T1 (https=) |
| TW (1) | TWI808108B (https=) |
| UA (1) | UA127502C2 (https=) |
| WO (1) | WO2019104134A1 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI598337B (zh) * | 2009-06-29 | 2017-09-11 | 阿吉歐斯製藥公司 | 治療化合物及組成物 |
| LT3483164T (lt) | 2017-03-20 | 2020-05-11 | Forma Therapeutics, Inc. | Pirolpirolo kompozicijos kaip piruvato kinazės (pkr) aktyvatoriai |
| KR102777452B1 (ko) | 2017-11-22 | 2025-03-10 | 아지오스 파마슈티컬스 아이엔씨. | N-(4-(4-(시클로프로필메틸)피페라진-1-카르보닐)페닐)퀴놀린-8-술폰아미드의결정 형태 |
| EP3852791B1 (en) | 2018-09-19 | 2024-07-03 | Novo Nordisk Health Care AG | Activating pyruvate kinase r |
| EP3853206B1 (en) | 2018-09-19 | 2024-04-10 | Novo Nordisk Health Care AG | Treating sickle cell disease with a pyruvate kinase r activating compound |
| 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 |
| HRP20251148T1 (hr) | 2019-09-19 | 2025-11-21 | Novo Nordisk Health Care Ag | Pripravci koji aktiviraju piruvat-kinazu r (pkr) |
| WO2021154987A1 (en) | 2020-01-28 | 2021-08-05 | Teva Pharmaceuticals International Gmbh | Solid state forms of mitapivat and process for preparation thereof |
| CN116568281A (zh) * | 2020-09-25 | 2023-08-08 | 安吉奥斯医药品有限公司 | 药物制剂 |
| EP4216956A1 (en) * | 2020-09-25 | 2023-08-02 | Agios Pharmaceuticals, Inc. | Pharmaceutical formulation |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
| WO2023154036A1 (en) | 2022-02-08 | 2023-08-17 | Agios Pharmaceuticals, Inc. | Methods for titrating mitapivat |
| WO2022231627A1 (en) | 2021-04-30 | 2022-11-03 | Agios Pharmaceuticals, Inc. | Methods for titrating mitapivat for use in treating thalassemia |
| EP4329758A1 (en) * | 2021-04-30 | 2024-03-06 | 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 |
| IL312679A (en) | 2021-11-16 | 2024-07-01 | Agios Pharmaceuticals Inc | Compounds for the treatment of anemia associated with MDS 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 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003506329A (ja) | 1999-07-30 | 2003-02-18 | ランバクシー ラボラトリーズ リミテッド | セフポドキシメプロキセチルの改良アモルファス形態 |
| JP2005521636A (ja) | 2001-10-18 | 2005-07-21 | シプラ・リミテッド | 薬剤的に許容されるアモルファス形態のアレンドロ酸塩 |
| JP2015528516A (ja) | 2012-09-18 | 2015-09-28 | 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 |
| WO2016201227A1 (en) | 2015-06-11 | 2016-12-15 | Agios Pharmaceuticals, Inc. | Methods of using pyruvate kinase activators |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU722662B2 (en) | 1996-05-20 | 2000-08-10 | Darwin Discovery Limited | Quinoline sulfonamides as TNF inhibitors and as PDE-IV inhibitors |
| US20010041706A1 (en) | 2000-03-24 | 2001-11-15 | Synold Timothy W. | Blockade of taxane metabolism |
| US20020055495A1 (en) | 2000-09-05 | 2002-05-09 | Anthony Jannetta | Two-component anti-emetic composition |
| CN101711164B (zh) | 2007-01-18 | 2014-06-04 | 密苏里-哥伦比亚大学 | 可修复肌纤维膜中的神经元型一氧化氮合酶的合成小/微-抗肌萎缩蛋白基因 |
| TWI598337B (zh) * | 2009-06-29 | 2017-09-11 | 阿吉歐斯製藥公司 | 治療化合物及組成物 |
| AU2011283008A1 (en) | 2010-07-30 | 2013-01-24 | Merck Sharp & Dohme Corp. | Inhibition of CYP3A drug metabolism |
| SMT202400081T1 (it) | 2011-05-03 | 2024-03-13 | Agios Pharmaceuticals Inc | Attivatori della piruvato chinasi per uso in terapia |
| WO2013056153A1 (en) * | 2011-10-13 | 2013-04-18 | Kung Charles | Activators of pyruvate kinase m2 and methods of treating disease |
| US9921221B2 (en) | 2012-07-26 | 2018-03-20 | Joslin Diabetes Center, Inc. | Predicting and treating diabetic complications |
| AU2015225496A1 (en) | 2014-03-03 | 2016-10-13 | Sujata ACHARJEE | Chimeric dystrophin-VSV-G-protein to treat dystrophinopathies |
| KR102777452B1 (ko) | 2017-11-22 | 2025-03-10 | 아지오스 파마슈티컬스 아이엔씨. | N-(4-(4-(시클로프로필메틸)피페라진-1-카르보닐)페닐)퀴놀린-8-술폰아미드의결정 형태 |
| US11878049B1 (en) | 2019-06-14 | 2024-01-23 | Agios Pharmaceuticals, Inc. | Mitapivat therapy and modulators of cytochrome P450 |
-
2018
- 2018-11-21 KR KR1020247022172A patent/KR102777452B1/ko active Active
- 2018-11-21 AU AU2018373122A patent/AU2018373122B2/en active Active
- 2018-11-21 EP EP18821779.8A patent/EP3713919B1/en active Active
- 2018-11-21 JP JP2020528129A patent/JP7275130B2/ja active Active
- 2018-11-21 US US16/765,456 patent/US11254652B2/en active Active
- 2018-11-21 CA CA3081945A patent/CA3081945A1/en active Pending
- 2018-11-21 SG SG11202004587XA patent/SG11202004587XA/en unknown
- 2018-11-21 EP EP23186155.0A patent/EP4285904A3/en active Pending
- 2018-11-21 LT LTEPPCT/US2018/062197T patent/LT3713919T/lt unknown
- 2018-11-21 WO PCT/US2018/062197 patent/WO2019104134A1/en not_active Ceased
- 2018-11-21 IL IL274488A patent/IL274488B2/en unknown
- 2018-11-21 SI SI201830984T patent/SI3713919T1/sl unknown
- 2018-11-21 KR KR1020207015018A patent/KR102682430B1/ko active Active
- 2018-11-21 MD MDE20200988T patent/MD3713919T2/ro unknown
- 2018-11-21 HR HRP20230931TT patent/HRP20230931T1/hr unknown
- 2018-11-21 CN CN202311301795.5A patent/CN117551030A/zh active Pending
- 2018-11-21 PL PL18821779.8T patent/PL3713919T3/pl unknown
- 2018-11-21 KR KR1020257007025A patent/KR20250034202A/ko active Pending
- 2018-11-21 CN CN201880075099.8A patent/CN111372920B/zh active Active
- 2018-11-21 FI FIEP18821779.8T patent/FI3713919T3/fi active
- 2018-11-21 BR BR112020010185-0A patent/BR112020010185A2/pt unknown
- 2018-11-21 PT PT188217798T patent/PT3713919T/pt unknown
- 2018-11-21 HU HUE18821779A patent/HUE063264T2/hu unknown
- 2018-11-21 IL IL305343A patent/IL305343B2/en unknown
- 2018-11-21 UA UAA202003680A patent/UA127502C2/uk unknown
- 2018-11-21 SM SM20230327T patent/SMT202300327T1/it unknown
- 2018-11-21 DK DK18821779.8T patent/DK3713919T3/da active
- 2018-11-21 RS RS20230793A patent/RS64592B1/sr unknown
- 2018-11-21 TW TW107141542A patent/TWI808108B/zh active
- 2018-11-21 IL IL322576A patent/IL322576A/en unknown
- 2018-11-21 ES ES18821779T patent/ES2959764T3/es active Active
- 2018-11-21 MX MX2020005348A patent/MX2020005348A/es unknown
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2020
- 2020-05-15 PH PH12020550644A patent/PH12020550644A1/en unknown
- 2020-07-13 MX MX2022009998A patent/MX2022009998A/es unknown
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2022
- 2022-01-14 US US17/575,898 patent/US12612381B2/en active Active
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2023
- 2023-05-02 JP JP2023076364A patent/JP2023093762A/ja not_active Withdrawn
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2024
- 2024-02-06 AU AU2024200724A patent/AU2024200724B2/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003506329A (ja) | 1999-07-30 | 2003-02-18 | ランバクシー ラボラトリーズ リミテッド | セフポドキシメプロキセチルの改良アモルファス形態 |
| JP2005521636A (ja) | 2001-10-18 | 2005-07-21 | シプラ・リミテッド | 薬剤的に許容されるアモルファス形態のアレンドロ酸塩 |
| JP2015528516A (ja) | 2012-09-18 | 2015-09-28 | 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 |
| WO2016201227A1 (en) | 2015-06-11 | 2016-12-15 | Agios Pharmaceuticals, Inc. | Methods of using pyruvate kinase activators |
Non-Patent Citations (3)
| Title |
|---|
| 平山令明,有機化合物結晶作製ハンドブック,2008年,pp. 17-23,37-40,45-51,57-65 |
| 長瀬博監訳,最新 創薬化学 下巻,株式会社テクノミック,1999年09月25日,pp. 347-365 |
| 高田則幸,創薬段階における原薬Formスクリーニングと選択,PHARM STAGE,Vol. 6, No. 10,2007年01月15日,pp. 20-25 |
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