AU2018373122B2 - 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 PDF

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AU2018373122B2
AU2018373122B2 AU2018373122A AU2018373122A AU2018373122B2 AU 2018373122 B2 AU2018373122 B2 AU 2018373122B2 AU 2018373122 A AU2018373122 A AU 2018373122A AU 2018373122 A AU2018373122 A AU 2018373122A AU 2018373122 B2 AU2018373122 B2 AU 2018373122B2
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crystalline form
crystalline
compound
subject
thalassemia
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AU2018373122A1 (en
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Liting GUO
Mahmoud Mirmehrabi
Jacob P. Sizemore
Yeqing Su
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Agios Pharmaceuticals Inc
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Agios Pharmaceuticals Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/36Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • 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)
AU2018373122A 2017-11-22 2018-11-21 Crystalline forms of N-(4-(4-(cyclopropylmethyl) piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide Active AU2018373122B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2024200724A AU2024200724A1 (en) 2017-11-22 2024-02-06 Crystalline forms of N-(4-(4-(cyclopropylmethyl) piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide

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)

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AU2024200724A Division AU2024200724A1 (en) 2017-11-22 2024-02-06 Crystalline forms of N-(4-(4-(cyclopropylmethyl) piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide

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AU2018373122A1 AU2018373122A1 (en) 2020-05-21
AU2018373122B2 true AU2018373122B2 (en) 2023-11-09

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AU2018373122A Active AU2018373122B2 (en) 2017-11-22 2018-11-21 Crystalline forms of N-(4-(4-(cyclopropylmethyl) piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide
AU2024200724A Pending AU2024200724A1 (en) 2017-11-22 2024-02-06 Crystalline forms of N-(4-(4-(cyclopropylmethyl) piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide

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AU2024200724A Pending AU2024200724A1 (en) 2017-11-22 2024-02-06 Crystalline forms of N-(4-(4-(cyclopropylmethyl) piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide

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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)

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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

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US8785450B2 (en) * 2009-06-29 2014-07-22 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions

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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
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Publication number Publication date
DK3713919T3 (da) 2023-09-25
US11254652B2 (en) 2022-02-22
US20220220093A1 (en) 2022-07-14
CN111372920A (zh) 2020-07-03
CN111372920B (zh) 2023-10-20
FI3713919T3 (fi) 2023-09-29
MX2022009998A (es) 2022-09-19
HUE063264T2 (hu) 2024-01-28
EP3713919B1 (en) 2023-08-02
KR20250034202A (ko) 2025-03-10
ES2959764T3 (es) 2024-02-28
RS64592B1 (sr) 2023-10-31
PL3713919T3 (pl) 2023-12-27
KR102777452B1 (ko) 2025-03-10
HRP20230931T1 (hr) 2023-11-24
CA3081945A1 (en) 2019-05-31
IL274488B1 (en) 2023-09-01
AU2018373122A1 (en) 2020-05-21
SMT202300327T1 (it) 2023-11-13
IL305343B1 (en) 2025-09-01
EP4285904A2 (en) 2023-12-06
JP2023093762A (ja) 2023-07-04
PH12020550644A1 (en) 2021-04-26
IL322576A (en) 2025-10-01
SG11202004587XA (en) 2020-06-29
TWI808108B (zh) 2023-07-11
JP7275130B2 (ja) 2023-05-17
KR102682430B1 (ko) 2024-07-08
IL274488A (en) 2020-06-30
UA127502C2 (uk) 2023-09-13
IL274488B2 (en) 2024-01-01
AU2024200724A1 (en) 2024-02-22
WO2019104134A1 (en) 2019-05-31
EP3713919A1 (en) 2020-09-30
KR20200090787A (ko) 2020-07-29
EP4285904A3 (en) 2023-12-20
PT3713919T (pt) 2023-10-26
SI3713919T1 (sl) 2023-10-30
IL305343A (en) 2023-10-01
TW201930289A (zh) 2019-08-01
LT3713919T (lt) 2023-10-10
KR20240108581A (ko) 2024-07-09
MD3713919T2 (ro) 2024-02-29
TW202334115A (zh) 2023-09-01
JP2021504338A (ja) 2021-02-15
MX2020005348A (es) 2020-08-13
CN117551030A (zh) 2024-02-13
BR112020010185A2 (pt) 2021-01-12
US20200277279A1 (en) 2020-09-03

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