JP2024523506A - 上皮成長因子受容体阻害剤の塩及び結晶形態 - Google Patents

上皮成長因子受容体阻害剤の塩及び結晶形態 Download PDF

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JP2024523506A
JP2024523506A JP2023579154A JP2023579154A JP2024523506A JP 2024523506 A JP2024523506 A JP 2024523506A JP 2023579154 A JP2023579154 A JP 2023579154A JP 2023579154 A JP2023579154 A JP 2023579154A JP 2024523506 A JP2024523506 A JP 2024523506A
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Prior art keywords
salt
compound
crystalline
egfr
ray powder
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JP2023579154A
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Japanese (ja)
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JP2024523506A5 (https=
Inventor
バトラー，エリカ
キンキマ，ケイトリン・エヌ
リー，クリストファー
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ブループリント メディシンズ コーポレイション
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Publication of JP2024523506A publication Critical patent/JP2024523506A/ja
Publication of JP2024523506A5 publication Critical patent/JP2024523506A5/ja
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    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/10—Succinic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/12—Glutaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2023579154A 2021-06-23 2022-06-22 上皮成長因子受容体阻害剤の塩及び結晶形態 Pending JP2024523506A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163214089P 2021-06-23 2021-06-23
US63/214,089 2021-06-23
PCT/US2022/034550 WO2022271846A1 (en) 2021-06-23 2022-06-22 Salt and crystal forms of an epidermal growth factor receptor inhibitor

Publications (2)

Publication Number Publication Date
JP2024523506A true JP2024523506A (ja) 2024-06-28
JP2024523506A5 JP2024523506A5 (https=) 2025-06-30

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JP2023579154A Pending JP2024523506A (ja) 2021-06-23 2022-06-22 上皮成長因子受容体阻害剤の塩及び結晶形態

Country Status (9)

Country Link
US (1) US20240293404A1 (https=)
EP (1) EP4359400B1 (https=)
JP (1) JP2024523506A (https=)
CN (1) CN117836287A (https=)
CA (1) CA3223859A1 (https=)
ES (1) ES3042447T3 (https=)
IL (1) IL309469A (https=)
TW (1) TW202317543A (https=)
WO (1) WO2022271846A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202309022A (zh) 2021-04-13 2023-03-01 美商努法倫特公司 用於治療具egfr突變之癌症之胺基取代雜環
EP4358942A1 (en) * 2021-06-23 2024-05-01 Blueprint Medicines Corporation Pharmaceutical compositions of an epidermal growth factor receptor inhibitor
CN116554150B (zh) * 2022-12-30 2025-12-19 苏州浦合医药科技有限公司 第四代egfr抑制剂

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017120429A1 (en) * 2016-01-07 2017-07-13 CS Pharmasciences, Inc. Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
WO2021133809A1 (en) * 2019-12-23 2021-07-01 Blueprint Medicines Corporation Inhibitors of mutant forms of egfr
WO2022061202A1 (en) * 2020-09-21 2022-03-24 The Regents Of The University Of California Compositions and methods for treating cancer
WO2022271801A1 (en) * 2021-06-23 2022-12-29 Blueprint Medicines Corporation Process for preparing egfr inhibitors
WO2022271765A1 (en) * 2021-06-23 2022-12-29 Blueprint Medicines Corporation Pharmaceutical compositions of an epidermal growth factor receptor inhibitor

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017120429A1 (en) * 2016-01-07 2017-07-13 CS Pharmasciences, Inc. Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
WO2021133809A1 (en) * 2019-12-23 2021-07-01 Blueprint Medicines Corporation Inhibitors of mutant forms of egfr
WO2022061202A1 (en) * 2020-09-21 2022-03-24 The Regents Of The University Of California Compositions and methods for treating cancer
WO2022271801A1 (en) * 2021-06-23 2022-12-29 Blueprint Medicines Corporation Process for preparing egfr inhibitors
WO2022271765A1 (en) * 2021-06-23 2022-12-29 Blueprint Medicines Corporation Pharmaceutical compositions of an epidermal growth factor receptor inhibitor

Also Published As

Publication number Publication date
CA3223859A1 (en) 2022-12-29
WO2022271846A1 (en) 2022-12-29
ES3042447T3 (en) 2025-11-20
EP4359400B1 (en) 2025-07-02
EP4359400A1 (en) 2024-05-01
IL309469A (en) 2024-02-01
US20240293404A1 (en) 2024-09-05
TW202317543A (zh) 2023-05-01
CN117836287A (zh) 2024-04-05

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