CA3081945A1 - Crystalline forms of n-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide - Google Patents
Crystalline forms of n-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide Download PDFInfo
- Publication number
- CA3081945A1 CA3081945A1 CA3081945A CA3081945A CA3081945A1 CA 3081945 A1 CA3081945 A1 CA 3081945A1 CA 3081945 A CA3081945 A CA 3081945A CA 3081945 A CA3081945 A CA 3081945A CA 3081945 A1 CA3081945 A1 CA 3081945A1
- Authority
- CA
- Canada
- Prior art keywords
- crystalline form
- crystalline
- compound
- subject
- amorphous
- 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
Classifications
-
- 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)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
- Quinoline Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3081945A1 true CA3081945A1 (en) | 2019-05-31 |
Family
ID=64734113
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3081945A Pending CA3081945A1 (en) | 2017-11-22 | 2018-11-21 | Crystalline forms of n-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide |
Country Status (27)
| Country | Link |
|---|---|
| US (3) | US11254652B2 (enExample) |
| EP (2) | EP4285904A3 (enExample) |
| JP (2) | JP7275130B2 (enExample) |
| KR (3) | KR102682430B1 (enExample) |
| CN (2) | CN117551030A (enExample) |
| AU (3) | 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) | IL274488B2 (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) | TWI922809B (enExample) |
| UA (1) | UA127502C2 (enExample) |
| WO (1) | WO2019104134A1 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20120693A1 (es) * | 2009-06-29 | 2012-07-04 | Agios Pharmaceuticals Inc | Compuestos heterociclos como moduladores de la piruvato cinasa m2 (pkm2) |
| AR111295A1 (es) | 2017-03-20 | 2019-06-26 | Forma Therapeutics Inc | Composiciones de pirrolopirrol como activadores de piruvato quinasa (pkr) |
| KR102682430B1 (ko) | 2017-11-22 | 2024-07-08 | 아지오스 파마슈티컬스 아이엔씨. | N-(4-(4-(시클로프로필메틸)피페라진-1-카르보닐)페닐)퀴놀린-8-술폰아미드의 결정 형태 |
| US20200129485A1 (en) | 2018-09-19 | 2020-04-30 | Forma Therapeutics, Inc. | Treating sickle cell disease with a pyruvate kinase r activating compound |
| WO2020061255A1 (en) | 2018-09-19 | 2020-03-26 | Forma Therapeutics, Inc. | Activating pyruvate kinase r |
| JP2022533227A (ja) * | 2019-05-22 | 2022-07-21 | アジオス ファーマシューティカルズ， インコーポレイテッド | 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塩形態 |
| US11878049B1 (en) | 2019-06-14 | 2024-01-23 | Agios Pharmaceuticals, Inc. | Mitapivat therapy and modulators of cytochrome P450 |
| MX2022003025A (es) | 2019-09-19 | 2022-04-07 | Forma Therapeutics Inc | Activacion de la piruvato cinasa r. |
| US12286404B2 (en) * | 2020-01-28 | 2025-04-29 | 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 |
| CA3196829A1 (en) * | 2020-09-25 | 2022-03-31 | Agios Pharmaceuticals, Inc. | Pharmaceutical formulation |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
| EP4329758A1 (en) | 2021-04-30 | 2024-03-06 | Agios Pharmaceuticals, Inc. | Methods for titrating mitapivat |
| 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 |
| 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 |
| KR20240107326A (ko) | 2021-11-16 | 2024-07-09 | 아지오스 파마슈티컬스 아이엔씨. | Mds 관련 빈혈 및 기타 상태를 치료하기 위한 화합물 |
| US20260146025A1 (en) | 2022-10-17 | 2026-05-28 | Tianish Laboratories Private 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 (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000510866A (ja) | 1996-05-20 | 2000-08-22 | ダーウィン・ディスカバリー・リミテッド | Ｔｎｆとｐｄｅ―ｉｖのインヒビターとしてのキノリンスルホンアミド |
| IN191496B (enExample) | 1999-07-30 | 2003-12-06 | Ranbaxy Lab Ltd | |
| US20010041706A1 (en) | 2000-03-24 | 2001-11-15 | Synold Timothy W. | Blockade of taxane metabolism |
| AU2001288690A1 (en) | 2000-09-05 | 2002-03-22 | Odyssey Pharmaceuticals Llc | Two-component anti-emetic composition comprising dexamethasone and metoclopramide |
| GB2383042A (en) * | 2001-10-18 | 2003-06-18 | Cipla Ltd | Amorphous alendronate sodium |
| WO2008088895A2 (en) | 2007-01-18 | 2008-07-24 | University Of Missouri-Columbia | Synthetic mini/micro-dystrophin genes to restore nnos to the sarcolemma |
| PE20120693A1 (es) * | 2009-06-29 | 2012-07-04 | Agios Pharmaceuticals Inc | Compuestos heterociclos como moduladores de la piruvato cinasa m2 (pkm2) |
| US20140162942A1 (en) | 2010-07-30 | 2014-06-12 | Anima Ghosal | Inhibition of cyp3a drug metabolism |
| PT3406251T (pt) | 2011-05-03 | 2024-01-24 | Agios Pharmaceuticals Inc | Ativadores da piruvato-cinase para utilização em terapia |
| US20140249150A1 (en) * | 2011-10-13 | 2014-09-04 | Agios Pharmaceuticals, Inc | Activators of pyruvate kinase m2 and methods of treating disease |
| EP2877214B1 (en) * | 2012-07-26 | 2019-04-24 | Joslin Diabetes Center, Inc. | Predicting 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 |
| JP2017513921A (ja) | 2014-03-03 | 2017-06-01 | アーチャルジー、スジャータ | ジストロフィン異常症を治療するためのキメラジストロフィン−ｖｓｖ−ｇタンパク質 |
| MX384883B (es) * | 2015-06-11 | 2025-03-14 | Agios Pharmaceuticals Inc | Métodos para usar activadores de piruvato cinasa. |
| KR102682430B1 (ko) | 2017-11-22 | 2024-07-08 | 아지오스 파마슈티컬스 아이엔씨. | N-(4-(4-(시클로프로필메틸)피페라진-1-카르보닐)페닐)퀴놀린-8-술폰아미드의 결정 형태 |
| US11878049B1 (en) | 2019-06-14 | 2024-01-23 | Agios Pharmaceuticals, Inc. | Mitapivat therapy and modulators of cytochrome P450 |
-
2018
- 2018-11-21 KR KR1020207015018A patent/KR102682430B1/ko active Active
- 2018-11-21 PT PT188217798T patent/PT3713919T/pt unknown
- 2018-11-21 FI FIEP18821779.8T patent/FI3713919T3/fi active
- 2018-11-21 MD MDE20200988T patent/MD3713919T2/ro unknown
- 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 SI SI201830984T patent/SI3713919T1/sl unknown
- 2018-11-21 CN CN202311301795.5A patent/CN117551030A/zh active Pending
- 2018-11-21 SG SG11202004587XA patent/SG11202004587XA/en unknown
- 2018-11-21 IL IL274488A patent/IL274488B2/en unknown
- 2018-11-21 CN CN201880075099.8A patent/CN111372920B/zh active Active
- 2018-11-21 WO PCT/US2018/062197 patent/WO2019104134A1/en not_active Ceased
- 2018-11-21 IL IL305343A patent/IL305343B2/en unknown
- 2018-11-21 EP EP23186155.0A patent/EP4285904A3/en active Pending
- 2018-11-21 AU AU2018373122A patent/AU2018373122B2/en active Active
- 2018-11-21 UA UAA202003680A patent/UA127502C2/uk unknown
- 2018-11-21 JP JP2020528129A patent/JP7275130B2/ja active Active
- 2018-11-21 LT LTEPPCT/US2018/062197T patent/LT3713919T/lt unknown
- 2018-11-21 SM SM20230327T patent/SMT202300327T1/it unknown
- 2018-11-21 RS RS20230793A patent/RS64592B1/sr unknown
- 2018-11-21 MX MX2020005348A patent/MX2020005348A/es unknown
- 2018-11-21 DK DK18821779.8T patent/DK3713919T3/da active
- 2018-11-21 TW TW112118933A patent/TWI922809B/zh active
- 2018-11-21 TW TW107141542A patent/TWI808108B/zh active
- 2018-11-21 HU HUE18821779A patent/HUE063264T2/hu unknown
- 2018-11-21 KR KR1020247022172A patent/KR102777452B1/ko active Active
- 2018-11-21 IL IL322576A patent/IL322576A/en unknown
- 2018-11-21 KR KR1020257007025A patent/KR20250034202A/ko active Pending
- 2018-11-21 PL PL18821779.8T patent/PL3713919T3/pl unknown
- 2018-11-21 BR BR112020010185-0A patent/BR112020010185A2/pt unknown
- 2018-11-21 HR HRP20230931TT patent/HRP20230931T1/hr unknown
- 2018-11-21 ES ES18821779T patent/ES2959764T3/es active Active
- 2018-11-21 EP EP18821779.8A patent/EP3713919B1/en active Active
-
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/US12612381B2/en active Active
-
2023
- 2023-05-02 JP JP2023076364A patent/JP2023093762A/ja not_active Withdrawn
-
2024
- 2024-02-06 AU AU2024200724A patent/AU2024200724B2/en active Active
-
2026
- 2026-03-26 US US19/629,456 patent/US20260217676A1/en active Pending
- 2026-04-29 AU AU2026203244A patent/AU2026203244A1/en active Pending
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