JP6434678B2 - 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 - Google Patents

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 Download PDF

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JP6434678B2
JP6434678B2 JP2018518551A JP2018518551A JP6434678B2 JP 6434678 B2 JP6434678 B2 JP 6434678B2 JP 2018518551 A JP2018518551 A JP 2018518551A JP 2018518551 A JP2018518551 A JP 2018518551A JP 6434678 B2 JP6434678 B2 JP 6434678B2
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compound
formula
salt
acid
added
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JPWO2018117152A1 (ja
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大夢 滝口
大夢 滝口
昭伸 東
昭伸 東
隆之 稲葉
隆之 稲葉
渡辺　隆
隆 渡辺
翼 竹市
翼 竹市
アナス・クラースコウ・ピーターセン
ペア・ヴェズセ
キム・レベク・イェンセン
ヤン・ボルンホルト
セレン・エプドルプ
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Leo Pharma AS
Japan Tobacco Inc
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Leo Pharma AS
Japan Tobacco Inc
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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
    • 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
    • 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
    • C07B2200/07—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)
JP2018518551A 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 Active JP6434678B2 (ja)

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JP2016247607 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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JP2018185491A Active JP7098496B2 (ja) 2016-12-21 2018-09-28 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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US (3) US11673900B2 (OSRAM)
EP (1) EP3560932A4 (OSRAM)
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KR (1) KR102546513B1 (OSRAM)
CN (2) CN110300756B (OSRAM)
AU (2) AU2017384317C1 (OSRAM)
BR (1) BR112019012688A2 (OSRAM)
CA (1) CA3047891A1 (OSRAM)
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MX (2) MX2019007542A (OSRAM)
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019048806A (ja) * 2016-12-21 2019-03-28 日本たばこ産業株式会社 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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HK1251223A1 (en) 2015-07-07 2019-01-25 Japan Tobacco, Inc. Method for producing 7h-pyrrolo[2, 3-d]pyrimidine derivative and intermediate thereof
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
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
KR20250159260A (ko) 2023-03-17 2025-11-10 레오 파마 에이/에스 중등도 내지 중증의 만성 손 습진 환자의 만성 손 습진 치료 방법
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
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
JP4546923B2 (ja) * 2003-05-30 2010-09-22 チョンウェ ファーマ コーポレーション ベータストランドミメティックスおよびこれに関連した方法
US7230119B2 (en) 2004-08-25 2007-06-12 Biocryst Pharmaceuticals, Inc. Process for the preparation of substituted pyrrolidine derivatives and intermediates
DK2078022T3 (da) 2006-09-22 2012-02-13 Janssen Pharmaceutica Nv Spirobenzazepiner anvendt som vasopressinantagonister
TWI466885B (zh) * 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
PH12013501437A1 (en) 2011-01-19 2013-09-16 Galapagos Nv Azetidine derivatives useful for the treatment of metabolic and inflammatory diseases
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
DK2964616T3 (en) 2013-03-05 2017-08-28 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
HK1251223A1 (en) 2015-07-07 2019-01-25 Japan Tobacco, Inc. Method for producing 7h-pyrrolo[2, 3-d]pyrimidine derivative and intermediate thereof
JP2020502224A (ja) * 2016-12-21 2020-01-23 日本たばこ産業株式会社 ヤヌスキナーゼ阻害剤の結晶形
CN110300756B (zh) * 2016-12-21 2024-01-02 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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019048806A (ja) * 2016-12-21 2019-03-28 日本たばこ産業株式会社 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
JP7098496B2 (ja) 2016-12-21 2022-07-11 日本たばこ産業株式会社 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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TW201829422A (zh) 2018-08-16
BR112019012688A2 (pt) 2019-11-19
AU2017384317C1 (en) 2022-06-30
IL288080B2 (en) 2024-03-01
TW202400613A (zh) 2024-01-01
IL267385B2 (en) 2023-06-01
AU2022203506B2 (en) 2024-02-08
IL267385A (OSRAM) 2019-07-31
EP3560932A4 (en) 2020-10-28
CN110300756A (zh) 2019-10-01
KR102546513B1 (ko) 2023-06-23
US12195481B2 (en) 2025-01-14
MX2024005335A (es) 2024-05-20
TWI854815B (zh) 2024-09-01
JPWO2018117152A1 (ja) 2018-12-20
US20200216470A1 (en) 2020-07-09
KR20190095408A (ko) 2019-08-14
CN117865992A (zh) 2024-04-12
AU2017384317B2 (en) 2022-03-10
JP2019048806A (ja) 2019-03-28
US20240140967A1 (en) 2024-05-02
AU2017384317A1 (en) 2019-07-11
US20250084106A1 (en) 2025-03-13
IL267385B1 (OSRAM) 2023-02-01
JP7098496B2 (ja) 2022-07-11
RU2019122691A3 (OSRAM) 2021-02-08
WO2018117152A1 (ja) 2018-06-28
CN110300756B (zh) 2024-01-02
MX2019007542A (es) 2019-11-18
IL288080A (en) 2022-01-01
RU2019122691A (ru) 2021-01-25
TWI816651B (zh) 2023-10-01
US11673900B2 (en) 2023-06-13
CA3047891A1 (en) 2018-06-28
EP3560932A1 (en) 2019-10-30
AU2022203506A1 (en) 2022-06-09
IL288080B1 (en) 2023-11-01

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