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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China
Prior art keywords
pyrimidine
yield
esi
nmr
retention time
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CN201780084344.7A
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English (en)
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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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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 (https=)
EP (1) EP3544613B1 (https=)
JP (1) JP7114591B2 (https=)
KR (1) KR102575990B1 (https=)
CN (1) CN110545817B (https=)
ES (1) ES2878078T3 (https=)
MA (1) MA46889A (https=)
WO (1) WO2018098412A1 (https=)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2850773T3 (es) * 2016-11-28 2021-08-31 Bristol Myers Squibb Co Piridincarboxamidas como inhibidores de GSK-3
WO2020132651A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
EP3898616B1 (en) * 2018-12-20 2024-10-02 Amgen Inc. Heteroaryl amides useful as kif18a inhibitors
JP7676308B2 (ja) 2018-12-20 2025-05-14 アムジエン・インコーポレーテツド Kif18a阻害剤として有用なヘテロアリールアミド
US12540129B2 (en) 2019-08-02 2026-02-03 Amgen Inc. KIF18A inhibitors
WO2021026099A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
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
EP4709712A1 (en) * 2023-05-10 2026-03-18 Blueprint Medicines Corporation Gsk3a inhibitors and methods of use thereof

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
CN105849097A (zh) 2013-11-06 2016-08-10 百时美施贵宝公司 取代的吡啶衍生物用作gsk-3抑制剂
ES2850773T3 (es) 2016-11-28 2021-08-31 Bristol Myers Squibb Co Piridincarboxamidas como inhibidores de GSK-3

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

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