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 PDF

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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
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CA
Canada
Prior art keywords
crystalline form
crystalline
compound
subject
amorphous
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Pending
Application number
CA3081945A
Other languages
English (en)
French (fr)
Inventor
Jacob P. Sizemore
Liting GUO
Mahmoud Mirmehrabi
Yeqing Su
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Agios Pharmaceuticals Inc
Original Assignee
Agios Pharmaceuticals Inc
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=64734113&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA3081945(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Agios Pharmaceuticals Inc filed Critical Agios Pharmaceuticals Inc
Publication of CA3081945A1 publication Critical patent/CA3081945A1/en
Pending legal-status Critical Current

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Classifications

    • 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)
CA3081945A 2017-11-22 2018-11-21 Crystalline forms of n-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide Pending CA3081945A1 (en)

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 (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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Also Published As

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
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
AU2018373122B2 (en) 2023-11-09
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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