TWI862146B - Fgfr3抑制劑之共晶型式 - Google Patents

Fgfr3抑制劑之共晶型式 Download PDF

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Publication number
TWI862146B
TWI862146B TW112133993A TW112133993A TWI862146B TW I862146 B TWI862146 B TW I862146B TW 112133993 A TW112133993 A TW 112133993A TW 112133993 A TW112133993 A TW 112133993A TW I862146 B TWI862146 B TW I862146B
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TW
Taiwan
Prior art keywords
cancer
bladder cancer
fgfr3
crystal form
urothelial
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TW112133993A
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English (en)
Chinese (zh)
Other versions
TW202428260A (zh
Inventor
大衛 安德魯 寇特
洛瑞 拉奎爾 希爾登
吉斯萊恩 庫米內克
傑佛瑞 Ａ 彼得森
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美商美國禮來大藥廠
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Publication of TW202428260A publication Critical patent/TW202428260A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
    • C07C65/03—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring
    • C07C65/05—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring o-Hydroxy carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
TW112133993A 2022-09-07 2023-09-07 Fgfr3抑制劑之共晶型式 TWI862146B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202263404232P 2022-09-07 2022-09-07
US63/404,232 2022-09-07

Publications (2)

Publication Number Publication Date
TW202428260A TW202428260A (zh) 2024-07-16
TWI862146B true TWI862146B (zh) 2024-11-11

Family

ID=88204177

Family Applications (1)

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TW112133993A TWI862146B (zh) 2022-09-07 2023-09-07 Fgfr3抑制劑之共晶型式

Country Status (16)

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US (1) US20240116932A1 (enExample)
EP (1) EP4584270A1 (enExample)
JP (2) JP7541606B2 (enExample)
KR (1) KR20250057022A (enExample)
CN (1) CN120187720A (enExample)
AR (1) AR130417A1 (enExample)
AU (1) AU2023338199A1 (enExample)
CA (1) CA3266872A1 (enExample)
CL (1) CL2025000596A1 (enExample)
CO (1) CO2025002467A2 (enExample)
CR (1) CR20250077A (enExample)
DO (1) DOP2025000054A (enExample)
IL (1) IL319342A (enExample)
PE (1) PE20251400A1 (enExample)
TW (1) TWI862146B (enExample)
WO (1) WO2024054814A1 (enExample)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025259519A1 (en) 2024-06-13 2025-12-18 Eli Lilly And Company Activation of egfr/her2/3 in cancer after treatment with an inhibitor of fibroblast growth factor receptor 3 (fgfr3)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020131627A1 (en) * 2018-12-19 2020-06-25 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007067727A2 (en) 2005-12-08 2007-06-14 Ssci, Inc. Metronidazole cocrystals and imipramine cocrystals
PH12012000132A1 (en) 2011-06-09 2014-10-20 Servier Lab New co-crystals of agomelatine, a process for their preparation and pharmaceutical compositions containing them
CN102964384B (zh) 2012-11-09 2015-06-24 中山大学 阿德福韦酯没食子酸共晶及其制备方法和组合物
JP2021523876A (ja) 2018-02-13 2021-09-09 トランスジェネックス ナノバイオテック、インコーポレイテッド 癌治療のためのタミバロテンの新規の結晶形態
CN111574359A (zh) 2019-02-19 2020-08-25 愈磐生物科技（苏州）有限公司 乐伐替尼-没食子酸共晶晶型及其应用
CN113943284B (zh) 2020-07-15 2023-12-19 中国医学科学院药物研究所 盐酸吡格列酮没食子酸共晶及制备方法和其组合物与用途
TW202402754A (zh) 2021-03-04 2024-01-16 美商美國禮來大藥廠 Fgfr3抑制劑化合物

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020131627A1 (en) * 2018-12-19 2020-06-25 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases

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Publication number Publication date
DOP2025000054A (es) 2025-03-31
CR20250077A (es) 2025-04-02
TW202428260A (zh) 2024-07-16
CN120187720A (zh) 2025-06-20
CL2025000596A1 (es) 2025-04-25
CO2025002467A2 (es) 2025-03-17
PE20251400A1 (es) 2025-05-22
JP2024037713A (ja) 2024-03-19
JP2024153948A (ja) 2024-10-29
JP7541606B2 (ja) 2024-08-28
WO2024054814A1 (en) 2024-03-14
AR130417A1 (es) 2024-12-04
KR20250057022A (ko) 2025-04-28
US20240116932A1 (en) 2024-04-11
IL319342A (en) 2025-05-01
AU2023338199A1 (en) 2025-03-20
EP4584270A1 (en) 2025-07-16
CA3266872A1 (en) 2024-03-14

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