KR102546513B1 - 7H-피롤로[2,3-d]피리미딘 유도체의 제조 방법 및 그의 합성 중간체 - Google Patents

7H-피롤로[2,3-d]피리미딘 유도체의 제조 방법 및 그의 합성 중간체 Download PDF

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KR102546513B1
KR102546513B1 KR1020197020824A KR20197020824A KR102546513B1 KR 102546513 B1 KR102546513 B1 KR 102546513B1 KR 1020197020824 A KR1020197020824 A KR 1020197020824A KR 20197020824 A KR20197020824 A KR 20197020824A KR 102546513 B1 KR102546513 B1 KR 102546513B1
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KR20190095408A (ko
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히로무 다키구치
아키노부 히가시
다카시 이나바
다카시 와타나베
츠바사 다케이치
안데르스 클라르스코프 페테르센
페르 베소에
킴 레벡 옌센
얀 보른홀트
소렌 엡드룹
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니뽄 다바코 산교 가부시키가이샤
레오 파마 에이/에스
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
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    • 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)
KR1020197020824A 2016-12-21 2017-12-20 7H-피롤로[2,3-d]피리미딘 유도체의 제조 방법 및 그의 합성 중간체 Active KR102546513B1 (ko)

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JPJP-P-2016-247607 2016-12-21
JP2016247607 2016-12-21
PCT/JP2017/045729 WO2018117152A1 (ja) 2016-12-21 2017-12-20 ７Ｈ－ピロロ［２，３－ｄ］ピリミジン誘導体の製造方法及びその合成中間体

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KR102546513B1 true KR102546513B1 (ko) 2023-06-23

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US (3) US11673900B2 (https=)
EP (1) EP3560932B1 (https=)
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KR (1) KR102546513B1 (https=)
CN (2) CN117865992A (https=)
AU (2) AU2017384317C1 (https=)
BR (1) BR112019012688A2 (https=)
CA (1) CA3047891A1 (https=)
IL (2) IL288080B2 (https=)
MX (2) MX2019007542A (https=)
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WO (1) WO2018117152A1 (https=)

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HK1251223A1 (en) 2015-07-07 2019-01-25 Japan Tobacco, Inc. Method for producing 7h-pyrrolo[2, 3-d]pyrimidine derivative and intermediate thereof
AU2017384317C1 (en) * 2016-12-21 2022-06-30 Japan Tobacco Inc. PROCESS FOR PREPARING 7H-PYRROLO[2,3-d]PYRIMIDINE DERIVATIVES AND SYNTHETIC INTERMEDIATES THEREOF
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
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
WO2024194105A1 (en) 2023-03-17 2024-09-26 Leo Pharma A/S A method for the treatment of chronic hand eczema in patients with moderate to severe chronic hand eczema
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
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WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
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WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
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WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

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JP2016512195A (ja) 2013-03-05 2016-04-25 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ネプリライシン阻害剤

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JP2016512195A (ja) 2013-03-05 2016-04-25 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ネプリライシン阻害剤

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IL288080B2 (en) 2024-03-01
EP3560932B1 (en) 2026-03-11
CN117865992A (zh) 2024-04-12
JPWO2018117152A1 (ja) 2018-12-20
AU2017384317B2 (en) 2022-03-10
US20240140967A1 (en) 2024-05-02
CA3047891A1 (en) 2018-06-28
JP7098496B2 (ja) 2022-07-11
US20250084106A1 (en) 2025-03-13
IL267385A (https=) 2019-07-31
TW202400613A (zh) 2024-01-01
CN110300756B (zh) 2024-01-02
US12195481B2 (en) 2025-01-14
RU2019122691A (ru) 2021-01-25
US11673900B2 (en) 2023-06-13
US20200216470A1 (en) 2020-07-09
EP3560932A1 (en) 2019-10-30
IL288080A (en) 2022-01-01
JP2019048806A (ja) 2019-03-28
CN110300756A (zh) 2019-10-01
AU2017384317A1 (en) 2019-07-11
AU2017384317C1 (en) 2022-06-30
MX2024005335A (es) 2024-05-20
TWI854815B (zh) 2024-09-01
TWI816651B (zh) 2023-10-01
KR20190095408A (ko) 2019-08-14
IL267385B1 (https=) 2023-02-01
RU2019122691A3 (https=) 2021-02-08
EP3560932A4 (en) 2020-10-28
WO2018117152A1 (ja) 2018-06-28
BR112019012688A2 (pt) 2019-11-19
AU2022203506A1 (en) 2022-06-09
IL267385B2 (en) 2023-06-01
IL288080B1 (en) 2023-11-01
JP6434678B2 (ja) 2018-12-05
MX2019007542A (es) 2019-11-18
TW201829422A (zh) 2018-08-16
AU2022203506B2 (en) 2024-02-08

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