IL274488B2 - 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-sulfonamideInfo
- Publication number
- IL274488B2 IL274488B2 IL274488A IL27448820A IL274488B2 IL 274488 B2 IL274488 B2 IL 274488B2 IL 274488 A IL274488 A IL 274488A IL 27448820 A IL27448820 A IL 27448820A IL 274488 B2 IL274488 B2 IL 274488B2
- Authority
- IL
- Israel
- Prior art keywords
- crystalline form
- composition
- treating
- thalassemia
- angles
- Prior art date
Links
Classifications
-
- 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
-
- 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
- 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
-
- 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)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Biophysics (AREA)
- Molecular Biology (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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762589822P | 2017-11-22 | 2017-11-22 | |
| US201862691709P | 2018-06-29 | 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 (3)
| Publication Number | Publication Date |
|---|---|
| IL274488A IL274488A (en) | 2020-06-30 |
| IL274488B1 IL274488B1 (en) | 2023-09-01 |
| IL274488B2 true IL274488B2 (en) | 2024-01-01 |
Family
ID=64734113
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL305343A IL305343B1 (en) | 2017-11-22 | 2018-11-21 | Crystalline forms of n-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide |
| IL274488A IL274488B2 (en) | 2017-11-22 | 2018-11-21 | Crystalline forms of n-(4-(4-(cyclopropylmethyl) piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide |
| IL322576A IL322576A (en) | 2017-11-22 | 2018-11-21 | Crystalline forms of N-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL305343A IL305343B1 (en) | 2017-11-22 | 2018-11-21 | Crystalline forms of n-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL322576A IL322576A (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 (2) | US11254652B2 (enExample) |
| EP (2) | EP3713919B1 (enExample) |
| JP (2) | JP7275130B2 (enExample) |
| KR (3) | KR20250034202A (enExample) |
| CN (2) | CN117551030A (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 |
|---|---|---|---|---|
| PT2448582T (pt) * | 2009-06-29 | 2017-07-10 | Agios Pharmaceuticals Inc | Compostos e composições terapêuticas |
| US11014927B2 (en) | 2017-03-20 | 2021-05-25 | Forma Therapeutics, Inc. | Pyrrolopyrrole compositions as pyruvate kinase (PKR) activators |
| ES2989438T3 (es) | 2018-09-19 | 2024-11-26 | Novo Nordisk Healthcare Ag | Activación de la piruvato cinasa R |
| US12053458B2 (en) | 2018-09-19 | 2024-08-06 | Novo Nordisk Health Care Ag | Treating sickle cell disease with a pyruvate kinase R activating compound |
| EP3972957A1 (en) * | 2019-05-22 | 2022-03-30 | 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 |
| EP4031132A4 (en) | 2019-09-19 | 2023-09-13 | Forma Therapeutics, Inc. | Activating pyruvate kinase r |
| EP4097085A1 (en) | 2020-01-28 | 2022-12-07 | 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 |
| 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 |
| JP2024518779A (ja) | 2021-04-30 | 2024-05-02 | 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 | ミタピバットを滴定するための方法 |
| 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8785450B2 (en) * | 2009-06-29 | 2014-07-22 | Agios Pharmaceuticals, Inc. | Therapeutic compounds and compositions |
| WO2016201227A1 (en) * | 2015-06-11 | 2016-12-15 | Agios Pharmaceuticals, Inc. | Methods of using pyruvate kinase activators |
Family Cites Families (6)
| 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 |
| CN108451955B (zh) | 2011-05-03 | 2022-02-01 | 安吉奥斯医药品有限公司 | 用于治疗的丙酮酸激酶活化剂 |
| US20140249150A1 (en) | 2011-10-13 | 2014-09-04 | Agios Pharmaceuticals, Inc | 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 |
| IN2015DN01662A (enExample) | 2012-09-18 | 2015-07-03 | Auspex Pharmaceuticals Inc |
-
2018
- 2018-11-21 SM SM20230327T patent/SMT202300327T1/it unknown
- 2018-11-21 WO PCT/US2018/062197 patent/WO2019104134A1/en not_active Ceased
- 2018-11-21 MX MX2020005348A patent/MX2020005348A/es unknown
- 2018-11-21 TW TW112118933A patent/TW202334115A/zh unknown
- 2018-11-21 SI SI201830984T patent/SI3713919T1/sl unknown
- 2018-11-21 IL IL305343A patent/IL305343B1/en unknown
- 2018-11-21 HR HRP20230931TT patent/HRP20230931T1/hr unknown
- 2018-11-21 IL IL274488A patent/IL274488B2/en unknown
- 2018-11-21 AU AU2018373122A patent/AU2018373122B2/en active Active
- 2018-11-21 KR KR1020257007025A patent/KR20250034202A/ko active Pending
- 2018-11-21 CA CA3081945A patent/CA3081945A1/en active Pending
- 2018-11-21 KR KR1020207015018A patent/KR102682430B1/ko active Active
- 2018-11-21 PL PL18821779.8T patent/PL3713919T3/pl unknown
- 2018-11-21 LT LTEPPCT/US2018/062197T patent/LT3713919T/lt unknown
- 2018-11-21 US US16/765,456 patent/US11254652B2/en active Active
- 2018-11-21 UA UAA202003680A patent/UA127502C2/uk unknown
- 2018-11-21 CN CN202311301795.5A patent/CN117551030A/zh active Pending
- 2018-11-21 FI FIEP18821779.8T patent/FI3713919T3/fi active
- 2018-11-21 DK DK18821779.8T patent/DK3713919T3/da active
- 2018-11-21 ES ES18821779T patent/ES2959764T3/es active Active
- 2018-11-21 KR KR1020247022172A patent/KR102777452B1/ko active Active
- 2018-11-21 PT PT188217798T patent/PT3713919T/pt unknown
- 2018-11-21 JP JP2020528129A patent/JP7275130B2/ja active Active
- 2018-11-21 EP EP18821779.8A patent/EP3713919B1/en active Active
- 2018-11-21 SG SG11202004587XA patent/SG11202004587XA/en unknown
- 2018-11-21 MD MDE20200988T patent/MD3713919T2/ro unknown
- 2018-11-21 CN CN201880075099.8A patent/CN111372920B/zh active Active
- 2018-11-21 TW TW107141542A patent/TWI808108B/zh active
- 2018-11-21 HU HUE18821779A patent/HUE063264T2/hu unknown
- 2018-11-21 BR BR112020010185-0A patent/BR112020010185A2/pt unknown
- 2018-11-21 IL IL322576A patent/IL322576A/en unknown
- 2018-11-21 RS RS20230793A patent/RS64592B1/sr unknown
- 2018-11-21 EP EP23186155.0A patent/EP4285904A3/en active Pending
-
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
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8785450B2 (en) * | 2009-06-29 | 2014-07-22 | Agios Pharmaceuticals, Inc. | Therapeutic compounds and compositions |
| WO2016201227A1 (en) * | 2015-06-11 | 2016-12-15 | Agios Pharmaceuticals, Inc. | Methods of using pyruvate kinase activators |
Non-Patent Citations (3)
| Title |
|---|
| BERGE ET AL.,, PHARMACEUTICALS SALTS, 1 January 1977 (1977-01-01) * |
| BYRN ET AL.,, PHARMACEUTICAL SOLIDS: A STRATEGIC APPROACH TO REGULATORY CONSIDERATIONS, 1 January 1995 (1995-01-01) * |
| CAIRA,, CRYSTALLINE POLYMORPHISM OF ORGANIC COMPOUNDS, 1 January 1998 (1998-01-01) * |
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