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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crystalline form
compound
crystalline
certain embodiments
thalassemia
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TW107141542A
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Chinese (zh)
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TW201930289A (zh
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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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    • 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
    • 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
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Biophysics (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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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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US (2) US11254652B2 (https=)
EP (2) EP3713919B1 (https=)
JP (2) JP7275130B2 (https=)
KR (3) KR102777452B1 (https=)
CN (2) CN117551030A (https=)
AU (2) AU2018373122B2 (https=)
BR (1) BR112020010185A2 (https=)
CA (1) CA3081945A1 (https=)
DK (1) DK3713919T3 (https=)
ES (1) ES2959764T3 (https=)
FI (1) FI3713919T3 (https=)
HR (1) HRP20230931T1 (https=)
HU (1) HUE063264T2 (https=)
IL (3) IL274488B2 (https=)
LT (1) LT3713919T (https=)
MD (1) MD3713919T2 (https=)
MX (2) MX2020005348A (https=)
PH (1) PH12020550644A1 (https=)
PL (1) PL3713919T3 (https=)
PT (1) PT3713919T (https=)
RS (1) RS64592B1 (https=)
SG (1) SG11202004587XA (https=)
SI (1) SI3713919T1 (https=)
SM (1) SMT202300327T1 (https=)
TW (1) TWI808108B (https=)
UA (1) UA127502C2 (https=)
WO (1) WO2019104134A1 (https=)

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LT3483164T (lt) 2017-03-20 2020-05-11 Forma Therapeutics, Inc. Pirolpirolo kompozicijos kaip piruvato kinazės (pkr) aktyvatoriai
KR102777452B1 (ko) 2017-11-22 2025-03-10 아지오스 파마슈티컬스 아이엔씨. N-(4-(4-(시클로프로필메틸)피페라진-1-카르보닐)페닐)퀴놀린-8-술폰아미드의결정 형태
EP3852791B1 (en) 2018-09-19 2024-07-03 Novo Nordisk Health Care AG Activating pyruvate kinase r
EP3853206B1 (en) 2018-09-19 2024-04-10 Novo Nordisk Health Care AG Treating sickle cell disease with a pyruvate kinase r activating compound
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
HRP20251148T1 (hr) 2019-09-19 2025-11-21 Novo Nordisk Health Care Ag Pripravci koji aktiviraju piruvat-kinazu r (pkr)
WO2021154987A1 (en) 2020-01-28 2021-08-05 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
EP4216956A1 (en) * 2020-09-25 2023-08-02 Agios Pharmaceuticals, Inc. Pharmaceutical formulation
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
EP4329758A1 (en) * 2021-04-30 2024-03-06 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
IL312679A (en) 2021-11-16 2024-07-01 Agios Pharmaceuticals Inc Compounds for the treatment of anemia associated with MDS 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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IL322576A (en) 2025-10-01
IL274488A (en) 2020-06-30
US11254652B2 (en) 2022-02-22
KR20200090787A (ko) 2020-07-29
TW201930289A (zh) 2019-08-01
CN117551030A (zh) 2024-02-13
EP3713919B1 (en) 2023-08-02
IL305343B1 (en) 2025-09-01
AU2018373122B2 (en) 2023-11-09
HRP20230931T1 (hr) 2023-11-24
JP7275130B2 (ja) 2023-05-17
US12612381B2 (en) 2026-04-28
EP3713919A1 (en) 2020-09-30
SI3713919T1 (sl) 2023-10-30
UA127502C2 (uk) 2023-09-13
IL274488B2 (en) 2024-01-01
KR102682430B1 (ko) 2024-07-08
IL305343A (en) 2023-10-01
MX2020005348A (es) 2020-08-13
FI3713919T3 (fi) 2023-09-29
EP4285904A2 (en) 2023-12-06
MD3713919T2 (ro) 2024-02-29
LT3713919T (lt) 2023-10-10
MX2022009998A (es) 2022-09-19
AU2024200724A1 (en) 2024-02-22
TW202334115A (zh) 2023-09-01
PH12020550644A1 (en) 2021-04-26
CN111372920A (zh) 2020-07-03
CA3081945A1 (en) 2019-05-31
PT3713919T (pt) 2023-10-26
IL274488B1 (en) 2023-09-01
KR20250034202A (ko) 2025-03-10
ES2959764T3 (es) 2024-02-28
US20220220093A1 (en) 2022-07-14
HUE063264T2 (hu) 2024-01-28
WO2019104134A1 (en) 2019-05-31
EP4285904A3 (en) 2023-12-20
IL305343B2 (en) 2026-01-01
JP2021504338A (ja) 2021-02-15
BR112020010185A2 (pt) 2021-01-12
AU2018373122A1 (en) 2020-05-21
AU2024200724B2 (en) 2026-02-05
DK3713919T3 (da) 2023-09-25
PL3713919T3 (pl) 2023-12-27
CN111372920B (zh) 2023-10-20
SG11202004587XA (en) 2020-06-29
SMT202300327T1 (it) 2023-11-13
US20200277279A1 (en) 2020-09-03
RS64592B1 (sr) 2023-10-31
KR102777452B1 (ko) 2025-03-10
JP2023093762A (ja) 2023-07-04
KR20240108581A (ko) 2024-07-09

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