JP2023511105A - ２－［３－［４－アミノ－３－（２－フルオロ－４－フェノキシ－フェニル）－１ｈ－ピラゾロ［３，４－ｄ］ピリミジン－１－イル］ピペリジン－１－カルボニル］－４－メチル－４－［４－（オキセタン－３－イル）ピペラジン－１－イル］ペンタ－２－エンニトリルの結晶形態 - Google Patents

２－［３－［４－アミノ－３－（２－フルオロ－４－フェノキシ－フェニル）－１ｈ－ピラゾロ［３，４－ｄ］ピリミジン－１－イル］ピペリジン－１－カルボニル］－４－メチル－４－［４－（オキセタン－３－イル）ピペラジン－１－イル］ペンタ－２－エンニトリルの結晶形態 Download PDF

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JP2023511105A
JP2023511105A JP2022543667A JP2022543667A JP2023511105A JP 2023511105 A JP2023511105 A JP 2023511105A JP 2022543667 A JP2022543667 A JP 2022543667A JP 2022543667 A JP2022543667 A JP 2022543667A JP 2023511105 A JP2023511105 A JP 2023511105A
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crystalline form
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パシット・フィアシヴォンサ
コルボット・バイ
ジーン・バウム
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プリンシピア バイオファーマ インコーポレイテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
JP2022543667A 2020-01-22 2021-01-21 ２－［３－［４－アミノ－３－（２－フルオロ－４－フェノキシ－フェニル）－１ｈ－ピラゾロ［３，４－ｄ］ピリミジン－１－イル］ピペリジン－１－カルボニル］－４－メチル－４－［４－（オキセタン－３－イル）ピペラジン－１－イル］ペンタ－２－エンニトリルの結晶形態 Pending JP2023511105A (ja)

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JP2025155648A JP2026001041A (ja) 2020-01-22 2025-09-19 ２－［３－［４－アミノ－３－（２－フルオロ－４－フェノキシ－フェニル）－１ｈ－ピラゾロ［３，４－ｄ］ピリミジン－１－イル］ピペリジン－１－カルボニル］－４－メチル－４－［４－（オキセタン－３－イル）ピペラジン－１－イル］ペンタ－２－エンニトリルの結晶形態

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US202062964378P 2020-01-22 2020-01-22
US62/964,378 2020-01-22
PCT/US2021/014371 WO2021150723A1 (en) 2020-01-22 2021-01-21 Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile

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JP2025155648A Division JP2026001041A (ja) 2020-01-22 2025-09-19 ２－［３－［４－アミノ－３－（２－フルオロ－４－フェノキシ－フェニル）－１ｈ－ピラゾロ［３，４－ｄ］ピリミジン－１－イル］ピペリジン－１－カルボニル］－４－メチル－４－［４－（オキセタン－３－イル）ピペラジン－１－イル］ペンタ－２－エンニトリルの結晶形態

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JP2023511105A true JP2023511105A (ja) 2023-03-16
JP2023511105A5 JP2023511105A5 (https=) 2024-01-29

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JP2022543667A Pending JP2023511105A (ja) 2020-01-22 2021-01-21 ２－［３－［４－アミノ－３－（２－フルオロ－４－フェノキシ－フェニル）－１ｈ－ピラゾロ［３，４－ｄ］ピリミジン－１－イル］ピペリジン－１－カルボニル］－４－メチル－４－［４－（オキセタン－３－イル）ピペラジン－１－イル］ペンタ－２－エンニトリルの結晶形態
JP2025155648A Pending JP2026001041A (ja) 2020-01-22 2025-09-19 ２－［３－［４－アミノ－３－（２－フルオロ－４－フェノキシ－フェニル）－１ｈ－ピラゾロ［３，４－ｄ］ピリミジン－１－イル］ピペリジン－１－カルボニル］－４－メチル－４－［４－（オキセタン－３－イル）ピペラジン－１－イル］ペンタ－２－エンニトリルの結晶形態

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JP2025155648A Pending JP2026001041A (ja) 2020-01-22 2025-09-19 ２－［３－［４－アミノ－３－（２－フルオロ－４－フェノキシ－フェニル）－１ｈ－ピラゾロ［３，４－ｄ］ピリミジン－１－イル］ピペリジン－１－カルボニル］－４－メチル－４－［４－（オキセタン－３－イル）ピペラジン－１－イル］ペンタ－２－エンニトリルの結晶形態

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US (3) US11814390B2 (https=)
EP (1) EP4093741A1 (https=)
JP (2) JP2023511105A (https=)
KR (1) KR20220130184A (https=)
CN (1) CN115461341A (https=)
AU (1) AU2021209884A1 (https=)
BR (1) BR112022014149A2 (https=)
CA (1) CA3164698A1 (https=)
CO (1) CO2022009916A2 (https=)
IL (1) IL294785A (https=)
MX (2) MX2022009009A (https=)
PH (1) PH12022551787A1 (https=)
WO (1) WO2021150723A1 (https=)

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CN115054586B (zh) 2016-06-29 2024-08-02 普林斯匹亚生物制药公司 改性的释放制剂
US20210106584A1 (en) 2019-10-14 2021-04-15 Principia Biopharma Inc. Methods for treating immune thrombocytopenia by administering (r)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
US11814390B2 (en) 2020-01-22 2023-11-14 Principia Biopharma Inc. Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1H-pyrazolo[3,4-D]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
KR20250023505A (ko) 2022-06-14 2025-02-18 프린시피아 바이오파마, 인코퍼레이티드 2-[3-[4-아미노-3-(2-플루오로-4-페녹시-페닐)피라졸로[3,4-d]피리미딘-1-일]피페리딘-1-카보닐]-4-메틸-4-[4-(옥세탄-3-일)피페라진-1-일]펜트-2-엔니트릴의결정질 형태
AU2023390489A1 (en) 2022-12-09 2025-07-24 Principia Biopharma Inc. Methods for treating immune thrombocytopenia in subjects with cognitive impairment by administering rilzabrutinib
WO2025006680A1 (en) 2023-06-30 2025-01-02 Principia Biopharma Inc. Methods for treating persistent or chronic immune thrombocytopenia in children, adolescents and adults by administering (r)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy- phenyl)pyrazolo[3,4-d]pyrimidin-l-yl]piperidine-l-carbonyl]-4- methyl-4-[4-(oxetan-3-yl)piperazin-l-yl]pent-2-enenitrile
IL326256A (en) 2023-08-01 2026-03-01 Principia Biopharma Inc Process for the preparation of 2-[(3R)-2-[4-AMINO-3-(2-FLUORO-4-PHENOXY- PHENYL)PYRAZOLO[3,4-D]PYRIMIDIN-1-YL]PIPERIDINE-1-CARBONYL]-4- METHYL-4[4-(OXETAN-3-YL)PIPERAZIN-1-YL]-PENT-2-ENENITRIL and its solvate forms
TW202535404A (zh) 2023-10-25 2025-09-16 美商普林斯匹亞生物製藥公司 使用ｂｔｋ抑制劑２－［（３ｒ）－３－［４－胺基－３－（２－氟－４－苯氧基－苯基）吡唑并［３，４－ｄ］嘧啶－１－基］哌啶－１－羰基］－４－甲基－４－［４－（氧雜環丁烷－３－基）哌𠯤－１－基］戊－２－烯腈治療與異位性皮炎和／或結節性癢疹相關的搔癢
TW202539683A (zh) 2023-12-06 2025-10-16 美商普林斯匹亞生物製藥公司 透過投予（ｒ）－２［３－［４－胺基－３－（２－氟－４－苯氧基－苯基）吡唑並［３，４－ｄ］嘧啶－１－基］哌啶－１－羰基］－４－甲基－４－［４－（氧雜環丁烷－３－基）哌𠯤－１－基］戊－２－烯腈治療中度至重度氣喘
TW202602449A (zh) 2024-03-19 2026-01-16 美商普林斯匹亞生物製藥公司 ２－［（３ｒ）－２－［４－胺基－３－（２－氟－４－苯氧基－苯基）吡唑並［３，４－ｄ］嘧啶－１－基］哌啶－１－羰基］－４－甲基－４［４－（氧雜環丁烷－３－基）哌－１－基］－戊－２－烯腈的調配物
WO2026024765A1 (en) 2024-07-23 2026-01-29 Principia Biopharma Inc. Treatment of venous thrombosis with rilzabrutinib and derivatives thereof
WO2026024885A1 (en) 2024-07-24 2026-01-29 Principia Biopharma Inc. Rilzabrutinib for treating warm antibody autoimmune hemolytic anemia
WO2026035812A1 (en) 2024-08-08 2026-02-12 Principia Biopharma Inc. Methods for treating sickle cell disease by administering a btk inhibitor

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