TWI776882B - 胺吡啶衍生化合物之鹽類、其結晶形及其製備方法 - Google Patents

胺吡啶衍生化合物之鹽類、其結晶形及其製備方法 Download PDF

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TWI776882B
TWI776882B TW107113234A TW107113234A TWI776882B TW I776882 B TWI776882 B TW I776882B TW 107113234 A TW107113234 A TW 107113234A TW 107113234 A TW107113234 A TW 107113234A TW I776882 B TWI776882 B TW I776882B
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crystalline form
mesylate
mesylate salt
organic solvent
formula
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TW107113234A
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Chinese (zh)
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TW201841910A (zh
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吳相昊
金鍾均
吳世雄
韓兌東
鄭水龍
李性蘭
金京培
李永成
申優燮
朱賢
姜正基
朴秀民
金東均
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南韓商柳韓洋行股份有限公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/02—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof
    • C07C303/22—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of sulfonic acids or halides thereof from sulfonic acids, by reactions not involving the formation of sulfo or halosulfonyl groups; from sulfonic halides by reactions not involving the formation of halosulfonyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
TW107113234A 2017-04-21 2018-04-18 胺吡啶衍生化合物之鹽類、其結晶形及其製備方法 TWI776882B (zh)

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KR20170051687 2017-04-21
KR10-2017-0051687 2017-04-21
??10-2017-0051687 2017-04-21

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TW201841910A TW201841910A (zh) 2018-12-01
TWI776882B true TWI776882B (zh) 2022-09-11

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US (3) US11453656B2 (enExample)
EP (1) EP3612529A4 (enExample)
JP (2) JP7126514B2 (enExample)
KR (3) KR102629654B1 (enExample)
CN (1) CN110869367B (enExample)
AR (1) AR111469A1 (enExample)
AU (2) AU2018256227B2 (enExample)
CA (1) CA3059543A1 (enExample)
CO (1) CO2019011578A2 (enExample)
EA (1) EA201992501A1 (enExample)
IL (2) IL294666B2 (enExample)
MA (1) MA49696A (enExample)
MX (2) MX392634B (enExample)
MY (1) MY201919A (enExample)
NZ (1) NZ758443A (enExample)
PH (1) PH12019502370A1 (enExample)
SA (1) SA519410342B1 (enExample)
SG (1) SG11201909615YA (enExample)
TW (1) TWI776882B (enExample)
UA (1) UA124364C2 (enExample)
WO (1) WO2018194356A1 (enExample)
ZA (1) ZA201907687B (enExample)

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AR111469A1 (es) * 2017-04-21 2019-07-17 Yuhan Corp Sal de un compuesto del derivado de aminopiridina, una forma cristalina de la misma, y un proceso para preparar la misma
ES2962961T3 (es) 2017-07-28 2024-03-22 Yuhan Corp Procedimiento de preparación de n-(5-((4-(4-(dimetilamino)metil)-3-fenil-1h-pirazol-1-il)pirimidin-2-il)amino)-4-metoxi-2-morfolinofenil)acrilamida haciendo reaccionar la amina correspondiente con un cloruro de 3-halo-propionilo
KR20200043618A (ko) * 2018-10-18 2020-04-28 주식회사유한양행 아미노피리미딘 유도체 또는 이의 염을 포함하는 경구투여용 약학 조성물
KR101973074B1 (ko) * 2018-11-30 2019-04-26 주식회사 티움바이오 퓨로피리미딘 화합물의 염 및 결정형, 및 이를 포함하는 약학적 조성물
CN111349084B (zh) * 2018-12-21 2022-11-25 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白激酶活性的氨基嘧啶类化合物
MX2021010265A (es) 2019-02-26 2021-09-23 Janssen Biotech Inc Terapias de combinacion y estratificacion de pacientes con anticuerpos anti-egfr/c-met biespecificos.
MY208668A (en) 2019-05-14 2025-05-23 Janssen Biotech Inc Combination therapies with bispecific anti-egfr/c-met antibodies and 3rd generation egfr tyrosine kinase inhibitors
BR112021022828A2 (pt) * 2019-05-14 2022-04-12 Janssen Biotech Inc Terapias combinadas com anticorpos biespecíficos anti-egfr/c-met e inibidores de egfr tirosina-quinase de terceira geração
US11850248B2 (en) 2019-05-14 2023-12-26 Yuhan Corporation Therapies with 3rd generation EGFR tyrosine kinase inhibitors
BR112022015140A2 (pt) 2020-02-12 2022-10-11 Janssen Biotech Inc Tratamento de pacientes que têm mutações de salto do éxon 14 de c-met
TWI923583B (zh) * 2020-04-14 2026-05-01 美商健生生物科技公司 包含胺基嘧啶衍生物或其醫藥上可接受之鹽之用於經口投予之醫藥組成物
EP4349835A4 (en) * 2021-06-01 2025-06-25 Hangzhou Solipharma Co., Ltd. Hydrated crystal form of lazertinib methanesulfonate, process for its preparation and use thereof
CA3228195A1 (en) 2023-05-23 2025-06-30 Janssen Biotech, Inc. Methods for treatment of non-small cell lung cancer (nsclc)
IL326946A (en) 2023-09-05 2026-05-01 Janssen Biotech Inc Methods of treating non-small cell lung cancer
WO2026042017A1 (en) 2024-08-19 2026-02-26 Janssen Biotech, Inc. Amivantamab in combination with lazertinib for the treatment of non-small cell lung cancer (nsclc)

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US20160102076A1 (en) * 2014-10-13 2016-04-14 Yuhan Corporation Compounds and compositions for modulating egfr mutant kinase activities

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PL1720853T3 (pl) 2004-02-11 2016-06-30 Natco Pharma Ltd Nowa odmiana polimorficzna metanosulfonianu imatynibu i sposób jej otrzymywania
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AR111469A1 (es) 2017-04-21 2019-07-17 Yuhan Corp Sal de un compuesto del derivado de aminopiridina, una forma cristalina de la misma, y un proceso para preparar la misma
KR20200043618A (ko) 2018-10-18 2020-04-28 주식회사유한양행 아미노피리미딘 유도체 또는 이의 염을 포함하는 경구투여용 약학 조성물

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US20230021395A1 (en) 2023-01-26
KR20230175161A (ko) 2023-12-29
KR20180118535A (ko) 2018-10-31
US12428401B2 (en) 2025-09-30
TW201841910A (zh) 2018-12-01
SA519410342B1 (ar) 2023-02-09
US20240279203A1 (en) 2024-08-22
AU2022203486A1 (en) 2022-06-09
US20210139461A1 (en) 2021-05-13
MX392634B (es) 2025-03-24
IL294666B1 (en) 2024-01-01
CN110869367B (zh) 2023-09-15
MX2022006357A (es) 2022-06-23
AU2018256227A1 (en) 2019-10-31
CN110869367A (zh) 2020-03-06
IL270018A (enExample) 2019-12-31
AU2022203486B2 (en) 2024-06-06
PH12019502370A1 (en) 2020-07-13
MA49696A (fr) 2020-06-03
US11453656B2 (en) 2022-09-27
US11981659B2 (en) 2024-05-14
JP2022166179A (ja) 2022-11-01
MY201919A (en) 2024-03-23
NZ758443A (en) 2023-03-31
CO2019011578A2 (es) 2020-02-28
IL270018B (en) 2022-08-01
SG11201909615YA (en) 2019-11-28
UA124364C2 (uk) 2021-09-01
CA3059543A1 (en) 2018-10-25
EP3612529A4 (en) 2020-11-18
EA201992501A1 (ru) 2020-02-18
JP2020517611A (ja) 2020-06-18
JP7390444B2 (ja) 2023-12-01
IL294666A (en) 2022-09-01
KR102629654B1 (ko) 2024-01-29
KR102835717B1 (ko) 2025-07-18
IL294666B2 (en) 2024-05-01
ZA201907687B (en) 2023-04-26
AU2018256227B2 (en) 2022-03-03
EP3612529A1 (en) 2020-02-26
JP7126514B2 (ja) 2022-08-26
BR112019021868A2 (pt) 2020-05-26
KR20250111074A (ko) 2025-07-22
AR111469A1 (es) 2019-07-17
WO2018194356A1 (en) 2018-10-25

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