CN112789040A - 转谷氨酰胺酶2(tg2)抑制剂 - Google Patents

转谷氨酰胺酶2(tg2)抑制剂 Download PDF

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Publication number
CN112789040A
CN112789040A CN201980065467.5A CN201980065467A CN112789040A CN 112789040 A CN112789040 A CN 112789040A CN 201980065467 A CN201980065467 A CN 201980065467A CN 112789040 A CN112789040 A CN 112789040A
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methyl
oxo
amino
dimethylamino
dihydropyridin
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CN201980065467.5A
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Chinese (zh)
Inventor
D.坎普贝尔
J.查普曼
M.H.张
T.R.迪莱蒙多
S.G.杜伦
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Starley Pharmaceutical Co
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Starley Pharmaceutical Co
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    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
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    • 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
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • C07D417/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
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    • C07D473/28—Oxygen atom
    • C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
    • C—CHEMISTRY; METALLURGY
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    • C07D473/00—Heterocyclic compounds containing purine ring systems
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    • C07D473/32—Nitrogen atom
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    • 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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    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
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    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic

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  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
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CN201980065467.5A 2018-08-10 2019-08-09 转谷氨酰胺酶2(tg2)抑制剂 Pending CN112789040A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862717697P 2018-08-10 2018-08-10
US62/717,697 2018-08-10
US201962845229P 2019-05-08 2019-05-08
US62/845,229 2019-05-08
PCT/US2019/045827 WO2020033784A1 (en) 2018-08-10 2019-08-09 Transglutaminase 2 (tg2) inhibitors

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CN112789040A true CN112789040A (zh) 2021-05-11

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CN115611760A (zh) * 2022-10-13 2023-01-17 天津药明康德新药开发有限公司 一种适合规模化生产(s)-2-氨基-5-炔基己酸的化学合成方法
CN116891413A (zh) * 2023-06-06 2023-10-17 山东东岳高分子材料有限公司 一种连续化制备2,4,5-三氟苯胺的方法
CN117561240A (zh) * 2021-06-30 2024-02-13 策迪拉有限公司 转谷氨酰胺酶的抑制剂
WO2024153137A1 (zh) * 2023-01-17 2024-07-25 西藏海思科制药有限公司 一种手性氨基醇医药中间体的制备方法

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WO2017210134A1 (en) 2016-05-31 2017-12-07 Board Of Regents, University Of Texas System Heterocyclic inhibitors of ptpn11
KR102611661B1 (ko) 2018-05-02 2023-12-08 나비레 파르마, 인코퍼레이티드 Ptpn11의 치환된 헤테로사이클릭 억제제
US12157746B2 (en) 2018-06-05 2024-12-03 Hoffmann-La Roche Inc. Tetrahydro-1H-pyrazino[2,1-a]isoindolylquinoline compounds for the treatment of autoimmune disease
PL3833670T3 (pl) 2018-08-10 2024-08-19 Navire Pharma, Inc. Pochodne 6-(4-amino-3-metylo-2-oksa-8-azaspiro[4.5]dekan-8-ylo)-3-(2,3-dichlorofenylo)-2-metylopirymidyn-4(3h)-onu oraz powiązane związki jako inhibitory ptpn11 (shp2) do leczenia raka
TWI825144B (zh) * 2018-08-10 2023-12-11 美商思達利醫藥公司 第二型轉麩醯胺酸酶(tg2)抑制劑
WO2020227549A1 (en) 2019-05-08 2020-11-12 Aligos Therapeutics, Inc. MODULATORS OF THR-β AND METHODS OF USE THEREOF
IL309476A (en) * 2021-06-30 2024-02-01 Zedira Gmbh Transglutaminase inhibitors
WO2023090479A1 (ko) * 2021-11-18 2023-05-25 주식회사 엠디바이오팜 신규한 트랜스글루타미나제 2 억제제 및 이의 용도
CN117024254B (zh) * 2023-08-10 2025-09-09 浙江大学衢州研究院 一种多氟苯酚的合成方法
WO2025153465A1 (en) 2024-01-15 2025-07-24 UCB Biopharma SRL Method for the treatment of fibrotic-related disorder associated to ibd

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TWI825144B (zh) * 2018-08-10 2023-12-11 美商思達利醫藥公司 第二型轉麩醯胺酸酶(tg2)抑制劑

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WO2007025247A2 (en) * 2005-08-26 2007-03-01 The Board Of Trustees Of The Leland Stanford Junior University Transglutaminase inhibitors and methods of use thereof
WO2012078519A2 (en) * 2010-12-06 2012-06-14 Numerate, Inc. 3-acylidene-2-oxoindole derivatives for inhibition of transglutaminase 2
US20120302539A1 (en) * 2011-05-10 2012-11-29 Michael Prime Transglutaminase tg2 inhibitors, pharmaceutical compositions, and methods of use thereof
CN104603109A (zh) * 2012-07-17 2015-05-06 策迪拉有限公司 作为组织转谷氨酰胺酶的抑制剂的吡啶酮衍生物
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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117561240A (zh) * 2021-06-30 2024-02-13 策迪拉有限公司 转谷氨酰胺酶的抑制剂
CN115611760A (zh) * 2022-10-13 2023-01-17 天津药明康德新药开发有限公司 一种适合规模化生产(s)-2-氨基-5-炔基己酸的化学合成方法
WO2024153137A1 (zh) * 2023-01-17 2024-07-25 西藏海思科制药有限公司 一种手性氨基醇医药中间体的制备方法
CN116891413A (zh) * 2023-06-06 2023-10-17 山东东岳高分子材料有限公司 一种连续化制备2,4,5-三氟苯胺的方法

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