AU2019318543B2 - Transglutaminase 2 (TG2) inhibitors - Google Patents

Transglutaminase 2 (TG2) inhibitors Download PDF

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Publication number
AU2019318543B2
AU2019318543B2 AU2019318543A AU2019318543A AU2019318543B2 AU 2019318543 B2 AU2019318543 B2 AU 2019318543B2 AU 2019318543 A AU2019318543 A AU 2019318543A AU 2019318543 A AU2019318543 A AU 2019318543A AU 2019318543 B2 AU2019318543 B2 AU 2019318543B2
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methyl
oxo
amino
dimethylamino
dihydropyridin
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AU2019318543A1 (en
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David Campbell
Justin Chapman
Mui H. Cheung
Thoams R. DIRAIMONDO
Sergio G. Duron
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Sitari Pharma Inc
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Sitari Pharma Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • C07D401/06—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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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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    • C07D417/02—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
    • 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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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D473/00—Heterocyclic compounds containing purine ring systems
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    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • 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
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D487/04—Ortho-condensed systems
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    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • 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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    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic

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  • Chemical & Material Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Proteomics, Peptides & Aminoacids (AREA)
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  • Neurology (AREA)
  • Neurosurgery (AREA)
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  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Analysing Materials By The Use Of Radiation (AREA)
AU2019318543A 2018-08-10 2019-08-09 Transglutaminase 2 (TG2) inhibitors Active AU2019318543B2 (en)

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

Publications (2)

Publication Number Publication Date
AU2019318543A1 AU2019318543A1 (en) 2021-03-11
AU2019318543B2 true AU2019318543B2 (en) 2022-12-22

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AU2019318543A Active AU2019318543B2 (en) 2018-08-10 2019-08-09 Transglutaminase 2 (TG2) inhibitors

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US (3) US12152026B2 (https=)
EP (2) EP4219460B1 (https=)
JP (1) JP7433315B2 (https=)
KR (1) KR102904276B1 (https=)
CN (1) CN112789040A (https=)
AU (1) AU2019318543B2 (https=)
BR (1) BR112021002532A2 (https=)
CL (1) CL2021000328A1 (https=)
CO (1) CO2021001472A2 (https=)
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KR102611661B1 (ko) 2018-05-02 2023-12-08 나비레 파르마, 인코퍼레이티드 Ptpn11의 치환된 헤테로사이클릭 억제제
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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
LT3833670T (lt) 2018-08-10 2024-06-25 Navire Pharma, Inc. 6-(4-amino-3-metil-2-oksa-8-azaspiro[4.5]dekan-8-il)-3-(2,3-dichlorfenil)-2-metilpirimidin-4(3h)-ono dariniai ir susiję junginiai kaip ptpn11 (shp2) inhibitoriai, skirti vėžiui gydyti
GEP20247637B (en) 2019-05-08 2024-06-25 Aligos Therapeutics Inc Modulators of thr-b and methods of use thereof
AU2022301517A1 (en) * 2021-06-30 2023-12-14 Zedira Gmbh Inhibitors of transglutaminases
KR20240028466A (ko) * 2021-06-30 2024-03-05 제디라 게엠베하 트랜스글루타미나아제 억제제
US20240300902A1 (en) * 2021-11-18 2024-09-12 Md Biolab Co., Ltd. Novel transglutaminase 2 inhibitor and use thereof
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
EP4653420A1 (en) * 2023-01-17 2025-11-26 Shenyang Haisco Pharmaceutical Co., Ltd. Method for preparing chiral amino alcohol pharmaceutical intermediates
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
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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JP6676058B2 (ja) 2015-01-14 2020-04-08 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ヘテロアリーレン架橋したベンゾジアゼピン二量体、そのコンジュゲート、ならびに製造および使用方法
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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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MY205622A (en) 2024-10-31
EP3833348B1 (en) 2023-05-31
LT3833348T (lt) 2023-07-10
ES2947438T3 (es) 2023-08-09
SG11202100736PA (en) 2021-02-25
CN112789040A (zh) 2021-05-11
DK3833348T3 (da) 2023-06-26
CA3109195A1 (en) 2020-02-13
PT3833348T (pt) 2023-06-29
UY38333A (es) 2020-05-29
AU2019318543A1 (en) 2021-03-11
EP4219460A1 (en) 2023-08-02
CL2021000328A1 (es) 2021-08-27
JP7433315B2 (ja) 2024-02-19
EP3833348A4 (en) 2021-06-30
BR112021002532A2 (pt) 2021-05-04
IL280719B1 (en) 2023-07-01
CO2021001472A2 (es) 2021-03-08
KR102904276B1 (ko) 2025-12-30
ES3017786T3 (en) 2025-05-13
JP2021534240A (ja) 2021-12-09
EP3833348A1 (en) 2021-06-16
SMT202300186T1 (it) 2023-07-20
HUE062140T2 (hu) 2023-09-28
US11548892B1 (en) 2023-01-10
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IL280719A (en) 2021-03-25
PL3833348T3 (pl) 2023-10-09
TWI825144B (zh) 2023-12-11
US20250011324A1 (en) 2025-01-09
SI3833348T1 (sl) 2023-08-31
IL280719B2 (en) 2023-11-01
TW202023553A (zh) 2020-07-01
US20210163480A1 (en) 2021-06-03
PH12021500008A1 (en) 2021-09-13
MX2021001550A (es) 2021-07-15
KR20210044248A (ko) 2021-04-22
US12152026B2 (en) 2024-11-26

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