TWI874443B - KRas G12D抑制劑 - Google Patents

KRas G12D抑制劑 Download PDF

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Publication number
TWI874443B
TWI874443B TW109129561A TW109129561A TWI874443B TW I874443 B TWI874443 B TW I874443B TW 109129561 A TW109129561 A TW 109129561A TW 109129561 A TW109129561 A TW 109129561A TW I874443 B TWI874443 B TW I874443B
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Taiwan
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group
compound
pharmaceutically acceptable
acceptable salt
alkyl
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TW109129561A
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English (en)
Chinese (zh)
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TW202122396A (zh
Inventor
小稜 王
馬修 阿諾德 馬克思
詹姆士 蓋兒 克里斯騰森
亞倫 克雷格 伯恩斯
克里斯托弗 羅納德 史密斯
約翰 麥可 凱瑟姆
托尼 Ｐ 湯
杰伊 布拉德福德 費爾
詹姆士 F 布萊克
瑪莎 Ｅ 羅德里格斯
瑪瑟多尼奧 Ｊ 梅加
帕維爾 薩維琴科夫
馬克 約瑟夫 奇卡雷利
峰 阮
蓋伊 Ｐ Ａ 威格士
東樺 戴
雪莉 艾倫
約書亞 達爾克
斯賓瑟 帕杰克
布拉德 紐豪斯
雅各布 Ｍ 奧萊里
千 趙
約翰 大衛 勞森
約翰 彼得 費希爾
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美商米拉蒂醫療公司
美商陣列生化製藥公司
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Publication of TW202122396A publication Critical patent/TW202122396A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • 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
    • 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
    • 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
    • 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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • C07D498/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW109129561A 2019-08-29 2020-08-28 KRas G12D抑制劑 TWI874443B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201962893604P 2019-08-29 2019-08-29
US62/893,604 2019-08-29
US202063052840P 2020-07-16 2020-07-16
US63/052,840 2020-07-16
US202063058188P 2020-07-29 2020-07-29
US63/058,188 2020-07-29

Publications (2)

Publication Number Publication Date
TW202122396A TW202122396A (zh) 2021-06-16
TWI874443B true TWI874443B (zh) 2025-03-01

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Application Number Title Priority Date Filing Date
TW109129561A TWI874443B (zh) 2019-08-29 2020-08-28 KRas G12D抑制劑
TW114103629A TW202523663A (zh) 2019-08-29 2020-08-28 KRas G12D抑制劑

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW114103629A TW202523663A (zh) 2019-08-29 2020-08-28 KRas G12D抑制劑

Country Status (16)

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US (3) US11453683B1 (enExample)
EP (1) EP4021444A4 (enExample)
JP (2) JP7622043B2 (enExample)
KR (1) KR20220071193A (enExample)
CN (1) CN114615981B (enExample)
AU (1) AU2020337938B2 (enExample)
BR (1) BR112022003543A2 (enExample)
CA (1) CA3148745A1 (enExample)
CL (1) CL2022000447A1 (enExample)
CO (1) CO2022003782A2 (enExample)
IL (1) IL290845A (enExample)
MX (1) MX2022002465A (enExample)
PH (1) PH12022550469A1 (enExample)
TW (2) TWI874443B (enExample)
WO (1) WO2021041671A1 (enExample)
ZA (1) ZA202202362B (enExample)

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* Cited by examiner, † Cited by third party
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