CN110545817B - Gsk-3抑制剂 - Google Patents

Gsk-3抑制剂 Download PDF

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Publication number
CN110545817B
CN110545817B CN201780084344.7A CN201780084344A CN110545817B CN 110545817 B CN110545817 B CN 110545817B CN 201780084344 A CN201780084344 A CN 201780084344A CN 110545817 B CN110545817 B CN 110545817B
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Prior art keywords
pyrimidine
yield
esi
nmr
retention time
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CN201780084344.7A
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Chinese (zh)
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CN110545817A (zh
Inventor
R·A·哈尔茨
V·T·阿呼佳
罗光林
L·陈
P·西瓦拉卡萨姆
G·M·杜博奇克
S·E·雅库廷门
J·E·马科尔
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201780084344.7A 2016-11-28 2017-11-27 Gsk-3抑制剂 Active CN110545817B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662426631P 2016-11-28 2016-11-28
US62/426,631 2016-11-28
PCT/US2017/063231 WO2018098412A1 (en) 2016-11-28 2017-11-27 Gsk-3 inhibitors

Publications (2)

Publication Number Publication Date
CN110545817A CN110545817A (zh) 2019-12-06
CN110545817B true CN110545817B (zh) 2022-11-15

Family

ID=60655130

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780084344.7A Active CN110545817B (zh) 2016-11-28 2017-11-27 Gsk-3抑制剂

Country Status (8)

Country Link
US (1) US10752609B2 (cg-RX-API-DMAC10.html)
EP (1) EP3544613B1 (cg-RX-API-DMAC10.html)
JP (1) JP7114591B2 (cg-RX-API-DMAC10.html)
KR (1) KR102575990B1 (cg-RX-API-DMAC10.html)
CN (1) CN110545817B (cg-RX-API-DMAC10.html)
ES (1) ES2878078T3 (cg-RX-API-DMAC10.html)
MA (1) MA46889A (cg-RX-API-DMAC10.html)
WO (1) WO2018098412A1 (cg-RX-API-DMAC10.html)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110198934B (zh) * 2016-11-28 2022-07-22 百时美施贵宝公司 作为gsk-3抑制剂的嘧啶甲酰胺
MA54550A (fr) 2018-12-20 2022-03-30 Amgen Inc Inhibiteurs de kif18a
AU2019401495B2 (en) 2018-12-20 2025-06-26 Amgen Inc. Heteroaryl amides useful as KIF18A inhibitors
AU2019404576B2 (en) * 2018-12-20 2025-07-17 Amgen Inc. Heteroaryl amides useful as KIF18A inhibitors
AU2020325115B2 (en) 2019-08-02 2026-03-12 Amgen Inc. Pyridine derivatives as KIF18A inhibitors
JP7699100B2 (ja) 2019-08-02 2025-06-26 アムジエン・インコーポレーテツド Kif18a阻害剤
CN116178281B (zh) * 2023-04-27 2023-07-21 中国药科大学 一种双功能免疫抑制剂及其制备方法和应用
CN121666382A (zh) * 2023-05-10 2026-03-13 缆图药品公司 GSK3α抑制剂和其使用方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101801958A (zh) * 2007-07-19 2010-08-11 先灵公司 作为蛋白质激酶抑制剂的杂环酰胺化合物
WO2012024179A1 (en) * 2010-08-18 2012-02-23 Merck Sharp & Dohme Corp. Substituted amide derivatives as dgat-1 inhibitors
CN105849098A (zh) * 2013-11-06 2016-08-10 百时美施贵宝公司 Gsk-3抑制剂
WO2016144792A1 (en) * 2015-03-06 2016-09-15 Alpharmagen, Llc Alpha 7 nicotinic acetylcholine receptor allosteric modulators, their derivatives and uses thereof

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0102438D0 (sv) * 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
JP2017500287A (ja) * 2013-11-06 2017-01-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Gsk−3阻害剤として有用な置換ピリジン誘導体
CN110198934B (zh) * 2016-11-28 2022-07-22 百时美施贵宝公司 作为gsk-3抑制剂的嘧啶甲酰胺

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101801958A (zh) * 2007-07-19 2010-08-11 先灵公司 作为蛋白质激酶抑制剂的杂环酰胺化合物
WO2012024179A1 (en) * 2010-08-18 2012-02-23 Merck Sharp & Dohme Corp. Substituted amide derivatives as dgat-1 inhibitors
CN105849098A (zh) * 2013-11-06 2016-08-10 百时美施贵宝公司 Gsk-3抑制剂
WO2016144792A1 (en) * 2015-03-06 2016-09-15 Alpharmagen, Llc Alpha 7 nicotinic acetylcholine receptor allosteric modulators, their derivatives and uses thereof

Also Published As

Publication number Publication date
MA46889A (fr) 2019-10-02
US20190315714A1 (en) 2019-10-17
US10752609B2 (en) 2020-08-25
ES2878078T3 (es) 2021-11-18
KR20190085114A (ko) 2019-07-17
JP7114591B2 (ja) 2022-08-08
JP2019535788A (ja) 2019-12-12
KR102575990B1 (ko) 2023-09-08
EP3544613A1 (en) 2019-10-02
CN110545817A (zh) 2019-12-06
EP3544613B1 (en) 2021-06-09
WO2018098412A1 (en) 2018-05-31

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