TWI911172B - Kras g12c突變體之小分子抑制劑 - Google Patents

Kras g12c突變體之小分子抑制劑

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Publication number
TWI911172B
TWI911172B TW109137485A TW109137485A TWI911172B TW I911172 B TWI911172 B TW I911172B TW 109137485 A TW109137485 A TW 109137485A TW 109137485 A TW109137485 A TW 109137485A TW I911172 B TWI911172 B TW I911172B
Authority
TW
Taiwan
Prior art keywords
mmol
int
mixture
oxy
compound
Prior art date
Application number
TW109137485A
Other languages
English (en)
Chinese (zh)
Other versions
TW202130645A (zh
Inventor
英朵 巴拉森
西蒙 蓋西亞克
湯瑪士 Ｈ 葛拉翰
永信 韓
堤摩西 韓德森
伊莉莎白 軒尼詩
馬曉申
萊恩 奧特
安南達 帕拉尼
大衛 Ｌ 史隆麥恩
Original Assignee
美商默沙東有限責任公司
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Application filed by 美商默沙東有限責任公司 filed Critical 美商默沙東有限責任公司
Publication of TW202130645A publication Critical patent/TW202130645A/zh
Application granted granted Critical
Publication of TWI911172B publication Critical patent/TWI911172B/zh

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Classifications

    • 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
    • A61K31/495—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • C07D471/22—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 systems contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
TW109137485A 2019-10-28 2020-10-28 Kras g12c突變體之小分子抑制劑 TWI911172B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201962926879P 2019-10-28 2019-10-28
US62/926,879 2019-10-28
US202063030014P 2020-05-26 2020-05-26
US63/030,014 2020-05-26

Publications (2)

Publication Number Publication Date
TW202130645A TW202130645A (zh) 2021-08-16
TWI911172B true TWI911172B (zh) 2026-01-11

Family

ID=73598936

Family Applications (1)

Application Number Title Priority Date Filing Date
TW109137485A TWI911172B (zh) 2019-10-28 2020-10-28 Kras g12c突變體之小分子抑制劑

Country Status (22)

Country Link
US (3) US11697657B2 (https=)
EP (1) EP4051678B1 (https=)
JP (2) JP7340100B2 (https=)
KR (1) KR20220106980A (https=)
CN (1) CN114867726B (https=)
AU (1) AU2020372881A1 (https=)
BR (1) BR112022007783A8 (https=)
CA (1) CA3158793A1 (https=)
CO (1) CO2022006858A2 (https=)
CR (1) CR20220230A (https=)
DO (1) DOP2022000090A (https=)
EC (1) ECSP22033597A (https=)
GE (2) GEP20247710B (https=)
IL (1) IL292438B2 (https=)
JO (1) JOP20220101A1 (https=)
MX (1) MX2022005053A (https=)
PE (1) PE20221253A1 (https=)
PH (1) PH12022551027A1 (https=)
TW (1) TWI911172B (https=)
UA (1) UA129778C2 (https=)
WO (1) WO2021086833A1 (https=)
ZA (1) ZA202205938B (https=)

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