TWI816651B - 7H-吡咯并[2,3-d]嘧啶衍生物的製造方法及其合成中間體 - Google Patents

7H-吡咯并[2,3-d]嘧啶衍生物的製造方法及其合成中間體 Download PDF

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TWI816651B
TWI816651B TW106144830A TW106144830A TWI816651B TW I816651 B TWI816651 B TW I816651B TW 106144830 A TW106144830 A TW 106144830A TW 106144830 A TW106144830 A TW 106144830A TW I816651 B TWI816651 B TW I816651B
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compound
formula
salt
item
acid
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TW106144830A
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TW201829422A (zh
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滝口大夢
東昭伸
稲葉𨺓之
渡辺
竹市翼
安德斯 卡拉斯考夫 彼得森
佩兒 韋德索
金姆 勒貝克 詹森
詹 伯恩候特
索倫 艾伯杜魯普
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日商日本煙草產業股份有限公司
丹麥商理奧藥品公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/06—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/26—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D307/30—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/32—Oxygen atoms
    • C07D307/33—Oxygen atoms in position 2, the oxygen atom being in its keto or unsubstituted enol form
    • 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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D487/10—Spiro-condensed systems
    • 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
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW106144830A 2016-12-21 2017-12-20 7H-吡咯并[2,3-d]嘧啶衍生物的製造方法及其合成中間體 TWI816651B (zh)

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JP2016247607 2016-12-21
JP2016-247607 2016-12-21

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TW201829422A TW201829422A (zh) 2018-08-16
TWI816651B true TWI816651B (zh) 2023-10-01

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TW112133483A TWI854815B (zh) 2016-12-21 2017-12-20 7H-吡咯并[2,3-d]嘧啶衍生物的製造方法及其合成中間體

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US (3) US11673900B2 (enExample)
EP (1) EP3560932A4 (enExample)
JP (2) JP6434678B2 (enExample)
KR (1) KR102546513B1 (enExample)
CN (2) CN117865992A (enExample)
AU (2) AU2017384317C1 (enExample)
BR (1) BR112019012688A2 (enExample)
CA (1) CA3047891A1 (enExample)
IL (2) IL288080B2 (enExample)
MX (2) MX2019007542A (enExample)
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WO (1) WO2018117152A1 (enExample)

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KR20180025940A (ko) 2015-07-07 2018-03-09 니뽄 다바코 산교 가부시키가이샤 7H-피롤로[2,3-d]피리미딘 유도체의 제조 방법 및 그의 중간체
CN117865992A (zh) 2016-12-21 2024-04-12 日本烟草产业株式会社 7H-吡咯并[2,3-d]嘧啶衍生物的制备方法及其合成中间体
CN111560021B (zh) * 2020-06-30 2023-05-26 上海鲲博玖瑞医药科技发展有限公司 一种德高替尼中间体及其制备方法
CN111606929B (zh) * 2020-06-30 2023-07-07 中瀚(齐河县)生物医药科技有限公司 德高替尼的制备方法
CN111574540B (zh) * 2020-06-30 2023-08-29 云南华派医药科技有限公司 一种德高替尼的制备方法
CN121175050A (zh) 2023-03-17 2025-12-19 利奥药品公司 用于治疗患有中度至重度慢性手部湿疹的患者的慢性手部湿疹的方法
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

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US7662960B2 (en) 2001-04-26 2010-02-16 Choongwae Pharma Corporation Beta-strand mimetics and method relating thereto
NZ543790A (en) * 2003-05-30 2009-09-25 Choongwae Pharma Corp Beta-strand mimetics and methods relating thereto
US7230119B2 (en) 2004-08-25 2007-06-12 Biocryst Pharmaceuticals, Inc. Process for the preparation of substituted pyrrolidine derivatives and intermediates
EP2078022B1 (en) 2006-09-22 2011-11-09 Janssen Pharmaceutica N.V. Spiro benzazepines used as vasopressin antagonists
TWI466885B (zh) 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
BR112013018286A2 (pt) 2011-01-19 2016-11-16 Galapagos Nv derivados d azetidina úteis para o tratamento de doenças metabólicas e inflamatórias
CN103570601B (zh) 2012-07-20 2016-03-30 重庆博腾制药科技股份有限公司 一种光学活性药物中间体的制备方法
WO2014138053A1 (en) * 2013-03-05 2014-09-12 Theravance Biopharma R&D Ip, Llc Neprilysin inhibitors
JP6500634B2 (ja) * 2015-06-24 2019-04-17 株式会社Ihi 溶接装置及び溶接方法
KR20180025940A (ko) * 2015-07-07 2018-03-09 니뽄 다바코 산교 가부시키가이샤 7H-피롤로[2,3-d]피리미딘 유도체의 제조 방법 및 그의 중간체
KR102788829B1 (ko) * 2016-12-21 2025-03-31 니뽄 다바코 산교 가부시키가이샤 야누스 키나제 억제제의 결정질 형태
CN117865992A (zh) * 2016-12-21 2024-04-12 日本烟草产业株式会社 7H-吡咯并[2,3-d]嘧啶衍生物的制备方法及其合成中间体

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TWI854815B (zh) 2024-09-01
IL267385B1 (enExample) 2023-02-01
MX2024005335A (es) 2024-05-20
JP7098496B2 (ja) 2022-07-11
US11673900B2 (en) 2023-06-13
AU2017384317B2 (en) 2022-03-10
KR102546513B1 (ko) 2023-06-23
CN110300756A (zh) 2019-10-01
WO2018117152A1 (ja) 2018-06-28
KR20190095408A (ko) 2019-08-14
RU2019122691A3 (enExample) 2021-02-08
TW201829422A (zh) 2018-08-16
IL288080B2 (en) 2024-03-01
EP3560932A1 (en) 2019-10-30
JP2019048806A (ja) 2019-03-28
AU2017384317C1 (en) 2022-06-30
JPWO2018117152A1 (ja) 2018-12-20
JP6434678B2 (ja) 2018-12-05
IL267385A (enExample) 2019-07-31
EP3560932A4 (en) 2020-10-28
BR112019012688A2 (pt) 2019-11-19
MX2019007542A (es) 2019-11-18
US20240140967A1 (en) 2024-05-02
CN110300756B (zh) 2024-01-02
RU2019122691A (ru) 2021-01-25
CN117865992A (zh) 2024-04-12
US12195481B2 (en) 2025-01-14
US20200216470A1 (en) 2020-07-09
CA3047891A1 (en) 2018-06-28
AU2022203506A1 (en) 2022-06-09
US20250084106A1 (en) 2025-03-13
IL288080B1 (en) 2023-11-01
AU2022203506B2 (en) 2024-02-08
IL288080A (en) 2022-01-01
AU2017384317A1 (en) 2019-07-11
IL267385B2 (en) 2023-06-01
TW202400613A (zh) 2024-01-01

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