HRP20230931T1 - Kristalični oblici n-(4-(4-(ciklopropilmetil)piperazin-1-karbonil)fenil)kinolin-8-sulfonamida - Google Patents

Kristalični oblici n-(4-(4-(ciklopropilmetil)piperazin-1-karbonil)fenil)kinolin-8-sulfonamida Download PDF

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HRP20230931T1
HRP20230931T1 HRP20230931TT HRP20230931T HRP20230931T1 HR P20230931 T1 HRP20230931 T1 HR P20230931T1 HR P20230931T T HRP20230931T T HR P20230931TT HR P20230931 T HRP20230931 T HR P20230931T HR P20230931 T1 HRP20230931 T1 HR P20230931T1
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crystalline form
preparation
tablet
individual
pharmaceutical preparation
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HRP20230931TT
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Jacob P. Sizemore
Liting GUO
Mahmoud Mirmehrabi
Yeqing Su
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Agios Pharmaceuticals, Inc.
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Publication of HRP20230931T1 publication Critical patent/HRP20230931T1/hr

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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
    • 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
    • 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)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (13)

1. Kristalični oblik od spoja koji je predstavljen sljedećom formulom: [image] gdje spoj je seskvihidrat; i pritom kristalični oblik je kristalični Oblik A, naznačen time, da ima maksimume rendgenske difrakcije na prahu pod 2Θ kutovima (± 0,2°) 9,9°, 15,8°, i 22,6°.
2. Kristalični oblik prema patentnom zahtjevu 1, pri čemu kristalični oblik je kristalični Oblik A, naznačen time, da ima maksimume rendgenske difrakcije na prahu pod 2Θ kutovima (± 0,2°) 9,9°, 15,8°, i 22,6°, i najmanje jedan, najmanje dva, ili najmanje tri dodatna maksimuma rendgenske difrakcije na prahu pod 2Θ kutovima (± 0,2°) odabrana od 15,0°, 17,1°, 21,3°, i 21,9°.
3. Kristalični oblik prema patentnom zahtjevu 2, pri čemu kristalični oblik je kristalični Oblik A, naznačen time, da ima maksimume rendgenske difrakcije na prahu pod 2Θ kutovima (± 0,2°) 9,9°, 11,4°, 15,0°, 15,3°, 15,8°, 17,1°, 17,7°, 21,3°, 21,9°, 22,6°, i 23,5°.
4. Kristalični oblik prema patentnom zahtjevu 3, pri čemu kristalični oblik je kristalični Oblik A, naznačen time, da ima maksimume rendgenske difrakcije na prahu pod 2Θ kutovima (± 0,2°) 4,9°, 9,9°, 11,0°, 11,4°, 11,7°, 12,3°, 12,8°, 13,6°, 13,9°, 14,2°, 15,0°, 15,3°, 15,8°, 17,1°, 17,4°, 17,7°, 18,8°, 19,1°, 19,8°, 21,3°, 21,9°, 22,6°, 23,0°, 23,2°, 23,5°, 23,8°, 24,1°, 24,5°, 25,3°, 25,6°, 26,1°, 27,1°, 28,1°, i 29,8°.
5. Farmaceutski pripravak, naznačen time, da sadrži kristalični oblik prema bilo kojem od patentnih zahtjeva 1 do 4, i farmaceutski prihvatljiv nosač.
6. Pripravak u tableti, naznačen time, da sadrži kristalični oblik prema bilo kojem od patentnih zahtjeva 1 do 4, i farmaceutski prihvatljiv nosač.
7. Farmaceutski pripravak prema patentnom zahtjevu 5 ili pripravak u tableti prema patentnom zahtjevu 6, naznačen time, da se nosač bira od jednog ili više od mikrokristalične celuloze, manitola, kroskarmeloze natrij, i natrijevog stearil fumarata.
8. Pripravak u tableti prema patentnom zahtjevu 6 ili zahtjevu 7, naznačen time, da pripravak sadrži 5,7 do 5,9 mg, 23,4 do 23,6 mg, ili 58,7 do 58,9 mg kristaličnog Oblika A; 62% masa/masa (± 2%) mikrokristalične celuloze; 23% masa/masa (± 2%) manitola; 3% masa/masa (± 2%) kroskarmeloze natrij; i 2% masa/masa (± 2%) stearil fumarata.
9. Kristalični oblik prema bilo kojem od patentnih zahtjeva 1 do 4, ili farmaceutski pripravak ili pripravak u tableti prema bilo kojem od patentnih zahtjeva 5 do 8, naznačen time, da je za uporabu u postupku liječenja nedostatka piruvat kinaze (PKD) kod pojedinca kojemu je to potrebno, pri čemu postupak obuhvaća davanje pojedincu učinkovite količine navedenog kristaličnog Oblika A, ili navedenog farmaceutskog pripravka ili pripravka u tableti.
10. Kristalični oblik prema bilo kojem od patentnih zahtjeva 1 do 4, ili farmaceutski pripravak ili pripravak u tableti prema bilo kojem od patentnih zahtjeva 5 do 8, naznačen time, da je za uporabu u postupku liječenja bolesti srpastih stanica (SCD) kod pojedinca kojemu je to potrebno, pri čemu postupak obuhvaća davanje pojedincu učinkovite količine navedenog kristaličnog Oblika A, ili navedenog farmaceutskog pripravka ili pripravka u tableti.
11. Kristalični oblik prema bilo kojem od patentnih zahtjeva 1 do 4, ili farmaceutski pripravak ili pripravak u tableti prema bilo kojem od patentnih zahtjeva 5 do 8, naznačen time, da je za uporabu u postupku liječenja talasemije, kao što su alfa-talasemija, beta-talasemija, talasemija neovisna o transfuziji, i talasemija ovisna o transfuziji, kod pojedinca kojemu je to potrebno, pri čemu postupak obuhvaća davanje pojedincu učinkovite količine navedenog kristaličnog Oblika A, ili navedenog farmaceutskog pripravka ili pripravka u tableti.
12. Kristalični oblik prema bilo kojem od patentnih zahtjeva 1 do 4, ili farmaceutski pripravak ili pripravak u tableti prema bilo kojem od patentnih zahtjeva 5 do 8, naznačen time, da je za uporabu u postupku liječenja hemolitičke anemije kod pojedinca kojemu je to potrebno, pri čemu postupak obuhvaća davanje pojedincu učinkovite količine navedenog kristaličnog Oblika A, ili navedenog farmaceutskog pripravka ili pripravka u tableti.
13. Kristalični oblik prema bilo kojem od patentnih zahtjeva 1 do 4, ili farmaceutski pripravak ili pripravak u tableti prema bilo kojem od patentnih zahtjeva 5 do 8, naznačen time, da je za uporabu u postupku liječenja bolesti koja se bira od nasljedne sferocitoze, nasljedne eliptocitoze, abetalipoproteinemije, sindroma Bassen-Kornzweig, i paroksizmalne noćne hemoglobinurije, kod pojedinca kojemu je to potrebno, pri čemu postupak obuhvaća davanje pojedincu učinkovite količine navedenog kristaličnog Oblika A, ili navedenog farmaceutskog pripravka ili pripravka u tableti.
HRP20230931TT 2017-11-22 2018-11-21 Kristalični oblici n-(4-(4-(ciklopropilmetil)piperazin-1-karbonil)fenil)kinolin-8-sulfonamida HRP20230931T1 (hr)

Applications Claiming Priority (4)

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
EP18821779.8A EP3713919B1 (en) 2017-11-22 2018-11-21 Crystalline forms of n-(4-(4-(cyclopropylmethyl) piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide

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HRP20230931T1 true HRP20230931T1 (hr) 2023-11-24

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US (2) US11254652B2 (hr)
EP (2) EP4285904A3 (hr)
JP (2) JP7275130B2 (hr)
KR (1) KR20200090787A (hr)
CN (2) CN111372920B (hr)
AU (2) AU2018373122B2 (hr)
BR (1) BR112020010185A2 (hr)
CA (1) CA3081945A1 (hr)
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HR (1) HRP20230931T1 (hr)
HU (1) HUE063264T2 (hr)
IL (2) IL305343A (hr)
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MD (1) MD3713919T2 (hr)
MX (2) MX2020005348A (hr)
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PL (1) PL3713919T3 (hr)
PT (1) PT3713919T (hr)
RS (1) RS64592B1 (hr)
SG (1) SG11202004587XA (hr)
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SG177434A1 (en) * 2009-06-29 2012-02-28 Agios Pharmaceuticals Inc Therapeutic compounds and compositions
MD3448859T2 (ro) 2017-03-20 2020-03-31 Forma Therapeutics Inc Compoziții de pirolopirol în calitate de activatori ai piruvatkinazei (PKR)
BR112021005188A2 (pt) 2018-09-19 2021-06-08 Forma Therapeutics, Inc. tratamento de anemia falciforme com um composto de ativação de piruvato cinase r
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
MX2021014228A (es) * 2019-05-22 2022-02-21 Agios Pharmaceuticals Inc Formas cristalinas de sal de n-(4-(4 (ciclopropilmetil)piperazin 1- carbonil)fenil)quinolin-8-sulfonamida.
US11878049B1 (en) * 2019-06-14 2024-01-23 Agios Pharmaceuticals, Inc. Mitapivat therapy and modulators of cytochrome P450
WO2021154987A1 (en) 2020-01-28 2021-08-05 Teva Pharmaceuticals International Gmbh Solid state forms of mitapivat and process for preparation thereof
AU2021347349A1 (en) * 2020-09-25 2023-06-08 Agios Pharmaceuticals, Inc. Pharmaceutical formulation
WO2022231627A1 (en) 2021-04-30 2022-11-03 Agios Pharmaceuticals, Inc. Methods for titrating mitapivat for use in treating thalassemia
WO2023154036A1 (en) 2022-02-08 2023-08-17 Agios Pharmaceuticals, Inc. Methods for titrating mitapivat
KR20240004620A (ko) 2021-04-30 2024-01-11 아지오스 파마슈티컬스 아이엔씨. 미타피바트를 적정하는 방법
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
CA3236880A1 (en) 2021-11-16 2023-05-25 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

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IN191496B (hr) * 1999-07-30 2003-12-06 Ranbaxy Lab Ltd
GB2383042A (en) * 2001-10-18 2003-06-18 Cipla Ltd Amorphous alendronate sodium
SG177434A1 (en) 2009-06-29 2012-02-28 Agios Pharmaceuticals Inc Therapeutic compounds and compositions
CN111728971A (zh) * 2012-09-18 2020-10-02 奥斯拜客斯制药有限公司 D6-四苯喹嗪固体口服剂型、化合物、及其药物组合物、制备及治疗方法
WO2016201227A1 (en) * 2015-06-11 2016-12-15 Agios Pharmaceuticals, Inc. Methods of using pyruvate kinase activators

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IL305343A (en) 2023-10-01
JP2021504338A (ja) 2021-02-15
TW202334115A (zh) 2023-09-01
SG11202004587XA (en) 2020-06-29
TWI808108B (zh) 2023-07-11
AU2018373122B2 (en) 2023-11-09
FI3713919T3 (fi) 2023-09-29
UA127502C2 (uk) 2023-09-13
EP4285904A2 (en) 2023-12-06
US11254652B2 (en) 2022-02-22
KR20200090787A (ko) 2020-07-29
EP4285904A3 (en) 2023-12-20
EP3713919A1 (en) 2020-09-30
ES2959764T3 (es) 2024-02-28
WO2019104134A1 (en) 2019-05-31
IL274488B2 (en) 2024-01-01
RS64592B1 (sr) 2023-10-31
DK3713919T3 (da) 2023-09-25
BR112020010185A2 (pt) 2021-01-12
CN111372920B (zh) 2023-10-20
CA3081945A1 (en) 2019-05-31
TW201930289A (zh) 2019-08-01
SI3713919T1 (sl) 2023-10-30
JP2023093762A (ja) 2023-07-04
AU2018373122A1 (en) 2020-05-21
CN111372920A (zh) 2020-07-03
PH12020550644A1 (en) 2021-04-26
LT3713919T (lt) 2023-10-10
HUE063264T2 (hu) 2024-01-28
CN117551030A (zh) 2024-02-13
US20200277279A1 (en) 2020-09-03
MD3713919T2 (ro) 2024-02-29
EP3713919B1 (en) 2023-08-02
MX2020005348A (es) 2020-08-13
IL274488A (en) 2020-06-30
MX2022009998A (es) 2022-09-19
US20220220093A1 (en) 2022-07-14
PT3713919T (pt) 2023-10-26
IL274488B1 (en) 2023-09-01
JP7275130B2 (ja) 2023-05-17
PL3713919T3 (pl) 2023-12-27
AU2024200724A1 (en) 2024-02-22

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