JP7693691B2 - P2x3アンタゴニストの製造 - Google Patents

P2x3アンタゴニストの製造 Download PDF

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Publication number
JP7693691B2
JP7693691B2 JP2022548876A JP2022548876A JP7693691B2 JP 7693691 B2 JP7693691 B2 JP 7693691B2 JP 2022548876 A JP2022548876 A JP 2022548876A JP 2022548876 A JP2022548876 A JP 2022548876A JP 7693691 B2 JP7693691 B2 JP 7693691B2
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Japan
Prior art keywords
compound
methyl
mixture
difluoro
morpholine
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JP2022548876A
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English (en)
Japanese (ja)
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JP2023513738A5 (https=
JP2023513738A (ja
Inventor
ナタリー・ショーレ
ジェレミー・グリーン
デイヴィッド・アール・クロネンタル
カリーヌ・ヴィルヌーヴ
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GlaxoSmithKline Intellectual Property No 3 Ltd
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GlaxoSmithKline Intellectual Property No 3 Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40Esters thereof
    • C07F9/4003Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006Esters of acyclic acids which can have further substituents on alkyl

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2022548876A 2020-02-14 2021-02-12 P2x3アンタゴニストの製造 Active JP7693691B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202062977004P 2020-02-14 2020-02-14
US62/977,004 2020-02-14
US202163144902P 2021-02-02 2021-02-02
US63/144,902 2021-02-02
PCT/IB2021/000130 WO2021161109A1 (en) 2020-02-14 2021-02-12 Preparation of a p2x3 antagonist

Publications (3)

Publication Number Publication Date
JP2023513738A JP2023513738A (ja) 2023-04-03
JP2023513738A5 JP2023513738A5 (https=) 2024-02-20
JP7693691B2 true JP7693691B2 (ja) 2025-06-17

Family

ID=77292130

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2022548876A Active JP7693691B2 (ja) 2020-02-14 2021-02-12 P2x3アンタゴニストの製造

Country Status (11)

Country Link
US (1) US12503470B2 (https=)
EP (1) EP4103572A4 (https=)
JP (1) JP7693691B2 (https=)
KR (1) KR20220140804A (https=)
CN (1) CN115427419B (https=)
AU (1) AU2021219992A1 (https=)
BR (1) BR112022015818A2 (https=)
CA (1) CA3184277A1 (https=)
IL (1) IL295394A (https=)
MX (1) MX2022009765A (https=)
WO (1) WO2021161109A1 (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7578602B2 (ja) 2019-02-25 2024-11-06 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー3)、リミテッド P2x3修飾薬での治療
WO2022156783A1 (zh) * 2021-01-22 2022-07-28 武汉人福创新药物研发中心有限公司 咪唑并吡啶类化合物的制备方法及其中间体
CN114805237B (zh) * 2021-01-22 2026-04-21 武汉人福创新药物研发中心有限公司 杂环类化合物的制备方法及其中间体
WO2022161462A1 (zh) * 2021-01-29 2022-08-04 上海海雁医药科技有限公司 吗啉衍生物及其药物组合物和用途
WO2023021328A1 (en) * 2021-08-17 2023-02-23 Bellus Health Cough Inc. Preparation of a p2x3 antagonist
EP4577528A1 (en) * 2022-08-25 2025-07-02 14245563 Canada Inc. Preparation of a p2x3 antagonist
WO2025125445A1 (en) 2023-12-12 2025-06-19 Glaxosmithkline Intellectual Property (No.3) Limited Process of manufacture of p2x3 antagonists including camlipixant
WO2025191081A1 (en) 2024-03-15 2025-09-18 Glaxosmithkline Intellectual Property (No.3) Limited Crystalline form of camlipixant
WO2026022326A1 (en) 2024-07-25 2026-01-29 Glaxosmithkline Intellectual Property (No.3) Limited P2x3 antagonist formulation

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016506935A (ja) 2013-01-31 2016-03-07 ネオメド・インスティチュート イミダゾピリジン化合物及びその使用
WO2020135771A1 (zh) 2018-12-29 2020-07-02 武汉朗来科技发展有限公司 杂环类化合物、中间体、其制备方法及应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2010229142A1 (en) * 2009-03-23 2011-10-13 Merck Sharp & Dohme Corp. P2X3, receptor antagonists for treatment of pain
CN102358739B (zh) * 2011-04-29 2013-02-20 中国科学院广州生物医药与健康研究院 咪唑[1,2-a]吡啶和咪唑醛类化合物的合成方法
US10111883B1 (en) 2017-09-18 2018-10-30 Bellus Health Cough Inc. Selective P2X3 modulators
EP4103564A4 (en) * 2020-02-14 2024-05-01 GlaxoSmithKline Intellectual Property (No.3) Limited P2X3 MODULATORS
WO2021244634A1 (zh) 2020-06-05 2021-12-09 武汉人福创新药物研发中心有限公司 咪唑并吡啶类化合物及其用途
EP4169921A4 (en) 2020-06-29 2024-06-19 Wuhan LL Science and Technology Development Co., Ltd. Crystalline form of heterocyclic compound, preparation method therefor and application thereof
WO2022156783A1 (zh) 2021-01-22 2022-07-28 武汉人福创新药物研发中心有限公司 咪唑并吡啶类化合物的制备方法及其中间体
CN114805237B (zh) 2021-01-22 2026-04-21 武汉人福创新药物研发中心有限公司 杂环类化合物的制备方法及其中间体

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016506935A (ja) 2013-01-31 2016-03-07 ネオメド・インスティチュート イミダゾピリジン化合物及びその使用
WO2020135771A1 (zh) 2018-12-29 2020-07-02 武汉朗来科技发展有限公司 杂环类化合物、中间体、其制备方法及应用

Also Published As

Publication number Publication date
IL295394A (en) 2022-10-01
BR112022015818A2 (pt) 2022-10-25
MX2022009765A (es) 2022-09-09
US20230101612A1 (en) 2023-03-30
JP2023513738A (ja) 2023-04-03
KR20220140804A (ko) 2022-10-18
CA3184277A1 (en) 2021-08-19
CN115427419A (zh) 2022-12-02
EP4103572A4 (en) 2024-03-06
WO2021161109A1 (en) 2021-08-19
CN115427419B (zh) 2026-04-21
EP4103572A1 (en) 2022-12-21
US12503470B2 (en) 2025-12-23
AU2021219992A1 (en) 2022-09-01

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