TWI899110B - Raf激酶抑制劑 - Google Patents

Raf激酶抑制劑

Info

Publication number
TWI899110B
TWI899110B TW109136965A TW109136965A TWI899110B TW I899110 B TWI899110 B TW I899110B TW 109136965 A TW109136965 A TW 109136965A TW 109136965 A TW109136965 A TW 109136965A TW I899110 B TWI899110 B TW I899110B
Authority
TW
Taiwan
Prior art keywords
carboxamide
trifluoroethyl
pyrrolidine
methylphenyl
amino
Prior art date
Application number
TW109136965A
Other languages
English (en)
Chinese (zh)
Other versions
TW202128680A (zh
Inventor
史蒂芬 W 卡多爾
托菲克 卡諾尼
約翰 泰納斯
艾瑞克 A 墨菲
Original Assignee
法商皮爾法伯製藥公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 法商皮爾法伯製藥公司 filed Critical 法商皮爾法伯製藥公司
Publication of TW202128680A publication Critical patent/TW202128680A/zh
Application granted granted Critical
Publication of TWI899110B publication Critical patent/TWI899110B/zh

Links

Classifications

    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW109136965A 2019-10-24 2020-10-23 Raf激酶抑制劑 TWI899110B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201962925596P 2019-10-24 2019-10-24
US62/925,596 2019-10-24
US202063044898P 2020-06-26 2020-06-26
US63/044,898 2020-06-26

Publications (2)

Publication Number Publication Date
TW202128680A TW202128680A (zh) 2021-08-01
TWI899110B true TWI899110B (zh) 2025-10-01

Family

ID=75619376

Family Applications (1)

Application Number Title Priority Date Filing Date
TW109136965A TWI899110B (zh) 2019-10-24 2020-10-23 Raf激酶抑制劑

Country Status (16)

Country Link
US (3) US11098031B1 (https=)
EP (1) EP4048259A4 (https=)
JP (1) JP7626910B2 (https=)
KR (1) KR20220104702A (https=)
CN (1) CN114845711B (https=)
AU (1) AU2020371727B2 (https=)
BR (1) BR112022007612A2 (https=)
CA (1) CA3158530A1 (https=)
CL (1) CL2022000998A1 (https=)
CO (1) CO2022006712A2 (https=)
IL (1) IL292424B1 (https=)
MX (1) MX2022004937A (https=)
PH (1) PH12022550976A1 (https=)
TW (1) TWI899110B (https=)
WO (1) WO2021081375A1 (https=)
ZA (1) ZA202204284B (https=)

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* Cited by examiner, † Cited by third party
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TW202106684A (zh) 2019-05-03 2021-02-16 美商奇奈特生物製藥公司 Raf激酶抑制劑
JP7626910B2 (ja) 2019-10-24 2025-02-05 ピエール ファーブル メディカモン Rafキナーゼの阻害剤
JP7214925B2 (ja) * 2019-12-06 2023-01-30 メッドシャイン ディスカバリー インコーポレイテッド Pan-RAFキナーゼ阻害剤としてのビアリール化合物
PH12022551513A1 (en) 2019-12-20 2023-04-24 Mirati Therapeutics Inc Sos1 inhibitors
WO2022060996A1 (en) * 2020-09-18 2022-03-24 Kinnate Biopharma Inc. Inhibitors of raf kinases
WO2022081469A1 (en) 2020-10-12 2022-04-21 Kinnate Biopharma Inc. Inhibitors of raf kinases
BR112023021913A2 (pt) * 2021-04-23 2024-01-16 Kinnate Biopharma Inc Tratamento de câncer com inibidor de raf
EP4326255A4 (en) * 2021-04-23 2025-03-12 Pierre Fabre Medicament Solid state forms of (s)-n-(3-(2-(((r)-1-hydroxypropan-2-yl)amino)-6-morpholinopyridin-4-yl)-4-methylphenyl)-3-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and salts thereof
EP4373806A4 (en) * 2021-07-19 2025-06-18 Pierre Fabre Medicament Preparation method of 3- (2, 2, 2-trifluoroethyl) pyrrolidine hydrochloride
WO2023061492A1 (zh) * 2021-10-14 2023-04-20 华领医药技术(上海)有限公司 2-氧代-3-氮杂双环[3.1.0]己烷衍生物
WO2023070053A1 (en) * 2021-10-21 2023-04-27 Kinnate Biopharma Inc. Inhibitors of raf kinases
CA3240192A1 (en) * 2021-12-09 2023-06-15 Daniel L. Flynn Raf kinase inhibitors and methods of use thereof
CA3240263A1 (en) 2021-12-09 2023-06-15 Daniel L. Flynn Raf kinase inhibitors and methods of use thereof
EP4472968A1 (en) * 2022-02-03 2024-12-11 Pierre Fabre Medicament Inhibitors of raf kinases
EP4486722A4 (en) * 2022-03-02 2026-03-25 Nico Therapeutics Inc COMPOUNDS, COMPOSITIONS AND PROCESSES

Citations (1)

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Publication number Priority date Publication date Assignee Title
TW201443021A (zh) * 2013-03-14 2014-11-16 Novartis Ag 用作激酶抑制劑的二芳基醯胺化合物

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US6334997B1 (en) 1994-03-25 2002-01-01 Isotechnika, Inc. Method of using deuterated calcium channel blockers
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US20070244120A1 (en) 2000-08-18 2007-10-18 Jacques Dumas Inhibition of raf kinase using substituted heterocyclic ureas
GB9823873D0 (en) 1998-10-30 1998-12-30 Pharmacia & Upjohn Spa 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents
WO2003068229A1 (en) 2002-02-11 2003-08-21 Bayer Pharmaceuticals Corporation Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors
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CA2592118C (en) 2004-12-23 2015-11-17 Deciphera Pharmaceuticals, Llc Urea derivatives as enzyme modulators
US8188113B2 (en) 2006-09-14 2012-05-29 Deciphera Pharmaceuticals, Inc. Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
CL2008001933A1 (es) 2007-06-29 2009-09-25 Millennium Pharm Inc Compuestos derivados de pirimidina, inhibidores de la raf quinasa; compuestos intermediarios; procedimiento de preparacion; composicion farmaceutica; y su uso para tratar trastornos proliferativos, cardiacos, neurodegenerativos, inflamatorios, oseos, inmunologicos enfermedad viral, entre otros.
EA018551B1 (ru) 2008-02-22 2013-08-30 Айрм Ллк ГЕТЕРОЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ И СОДЕРЖАЩИЕ ИХ КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗ c-KIT И PDGFR
EP2112150B1 (en) 2008-04-22 2013-10-16 Forma Therapeutics, Inc. Improved raf inhibitors
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CA3026876A1 (en) 2016-06-10 2017-12-14 Novartis Ag Therapeutic uses of a c-raf inhibitor
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WO2020198058A1 (en) * 2019-03-22 2020-10-01 Kinnate Biopharma Inc. Inhibitors of raf kinases
TW202106684A (zh) 2019-05-03 2021-02-16 美商奇奈特生物製藥公司 Raf激酶抑制劑
JP7626910B2 (ja) 2019-10-24 2025-02-05 ピエール ファーブル メディカモン Rafキナーゼの阻害剤
WO2022060996A1 (en) 2020-09-18 2022-03-24 Kinnate Biopharma Inc. Inhibitors of raf kinases
WO2022081469A1 (en) 2020-10-12 2022-04-21 Kinnate Biopharma Inc. Inhibitors of raf kinases
BR112023021913A2 (pt) 2021-04-23 2024-01-16 Kinnate Biopharma Inc Tratamento de câncer com inibidor de raf
EP4326255A4 (en) 2021-04-23 2025-03-12 Pierre Fabre Medicament Solid state forms of (s)-n-(3-(2-(((r)-1-hydroxypropan-2-yl)amino)-6-morpholinopyridin-4-yl)-4-methylphenyl)-3-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and salts thereof

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TW201443021A (zh) * 2013-03-14 2014-11-16 Novartis Ag 用作激酶抑制劑的二芳基醯胺化合物

Also Published As

Publication number Publication date
CN114845711A (zh) 2022-08-02
US20260055084A1 (en) 2026-02-26
US12312336B2 (en) 2025-05-27
AU2020371727A1 (en) 2022-05-26
ZA202204284B (en) 2024-09-25
CL2022000998A1 (es) 2023-02-10
CO2022006712A2 (es) 2022-05-31
KR20220104702A (ko) 2022-07-26
BR112022007612A2 (pt) 2022-09-20
MX2022004937A (es) 2022-07-27
AU2020371727B2 (en) 2026-01-22
US20210300904A1 (en) 2021-09-30
PH12022550976A1 (en) 2023-09-25
JP7626910B2 (ja) 2025-02-05
CA3158530A1 (en) 2021-04-29
EP4048259A1 (en) 2022-08-31
EP4048259A4 (en) 2023-08-02
WO2021081375A1 (en) 2021-04-29
NZ788005A (en) 2024-10-25
TW202128680A (zh) 2021-08-01
IL292424A (en) 2022-06-01
CN114845711B (zh) 2024-10-01
IL292424B1 (en) 2026-02-01
JP2022554169A (ja) 2022-12-28
US11098031B1 (en) 2021-08-24

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