TWI808108B - N-(4-(4-(環丙基甲基)哌嗪-1-羰基)苯基)喹啉-8-磺醯胺之結晶型 - Google Patents

N-(4-(4-(環丙基甲基)哌嗪-1-羰基)苯基)喹啉-8-磺醯胺之結晶型 Download PDF

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Publication number
TWI808108B
TWI808108B TW107141542A TW107141542A TWI808108B TW I808108 B TWI808108 B TW I808108B TW 107141542 A TW107141542 A TW 107141542A TW 107141542 A TW107141542 A TW 107141542A TW I808108 B TWI808108 B TW I808108B
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Taiwan
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crystalline form
compound
crystalline
certain embodiments
thalassemia
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TW107141542A
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English (en)
Chinese (zh)
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TW201930289A (zh
Inventor
賈寇柏 Ｐ 賽斯摩爾
郭麗婷
馬默德 密爾迷拉畢
蘇葉清
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美商阿吉歐斯製藥公司
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    • 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

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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)
TW107141542A 2017-11-22 2018-11-21 N-(4-(4-(環丙基甲基)哌嗪-1-羰基)苯基)喹啉-8-磺醯胺之結晶型 TWI808108B (zh)

Applications Claiming Priority (4)

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

Publications (2)

Publication Number Publication Date
TW201930289A TW201930289A (zh) 2019-08-01
TWI808108B true TWI808108B (zh) 2023-07-11

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TW112118933A TW202334115A (zh) 2017-11-22 2018-11-21 N-(4-(4-(環丙基甲基)哌嗪-1-羰基)苯基)喹啉-8-磺醯胺之結晶型
TW107141542A TWI808108B (zh) 2017-11-22 2018-11-21 N-(4-(4-(環丙基甲基)哌嗪-1-羰基)苯基)喹啉-8-磺醯胺之結晶型

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TW112118933A TW202334115A (zh) 2017-11-22 2018-11-21 N-(4-(4-(環丙基甲基)哌嗪-1-羰基)苯基)喹啉-8-磺醯胺之結晶型

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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)

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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)

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TW201103913A (en) * 2009-06-29 2011-02-01 Agios Pharmaceuticals Inc Therapeutic compounds and compositions
WO2016201227A1 (en) * 2015-06-11 2016-12-15 Agios Pharmaceuticals, Inc. Methods of using pyruvate kinase activators

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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

Patent Citations (2)

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TW201103913A (en) * 2009-06-29 2011-02-01 Agios Pharmaceuticals Inc Therapeutic compounds and compositions
WO2016201227A1 (en) * 2015-06-11 2016-12-15 Agios Pharmaceuticals, Inc. Methods of using pyruvate kinase activators

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UA127502C2 (uk) 2023-09-13
AU2024200724A1 (en) 2024-02-22
IL274488A (en) 2020-06-30
CN111372920A (zh) 2020-07-03
SMT202300327T1 (it) 2023-11-13
ES2959764T3 (es) 2024-02-28
MX2022009998A (es) 2022-09-19
JP2021504338A (ja) 2021-02-15
MX2020005348A (es) 2020-08-13
EP4285904A3 (en) 2023-12-20
JP2023093762A (ja) 2023-07-04
EP3713919A1 (en) 2020-09-30
KR20250034202A (ko) 2025-03-10
IL274488B2 (en) 2024-01-01
CN111372920B (zh) 2023-10-20
IL274488B1 (en) 2023-09-01
EP3713919B1 (en) 2023-08-02
BR112020010185A2 (pt) 2021-01-12
KR20240108581A (ko) 2024-07-09
PT3713919T (pt) 2023-10-26
IL305343A (en) 2023-10-01
HUE063264T2 (hu) 2024-01-28
KR102682430B1 (ko) 2024-07-08
JP7275130B2 (ja) 2023-05-17
SG11202004587XA (en) 2020-06-29
PH12020550644A1 (en) 2021-04-26
MD3713919T2 (ro) 2024-02-29
AU2018373122B2 (en) 2023-11-09
TW202334115A (zh) 2023-09-01
IL322576A (en) 2025-10-01
RS64592B1 (sr) 2023-10-31
KR102777452B1 (ko) 2025-03-10
DK3713919T3 (da) 2023-09-25
PL3713919T3 (pl) 2023-12-27
KR20200090787A (ko) 2020-07-29
CA3081945A1 (en) 2019-05-31
EP4285904A2 (en) 2023-12-06
AU2018373122A1 (en) 2020-05-21
US20220220093A1 (en) 2022-07-14
SI3713919T1 (sl) 2023-10-30
TW201930289A (zh) 2019-08-01
FI3713919T3 (fi) 2023-09-29
WO2019104134A1 (en) 2019-05-31
CN117551030A (zh) 2024-02-13
HRP20230931T1 (hr) 2023-11-24
LT3713919T (lt) 2023-10-10
US20200277279A1 (en) 2020-09-03
US11254652B2 (en) 2022-02-22
IL305343B1 (en) 2025-09-01

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