CN106795150B - 1,3,4-噻二唑化合物及其在治疗癌症中的用途 - Google Patents

1,3,4-噻二唑化合物及其在治疗癌症中的用途 Download PDF

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Publication number
CN106795150B
CN106795150B CN201580041233.9A CN201580041233A CN106795150B CN 106795150 B CN106795150 B CN 106795150B CN 201580041233 A CN201580041233 A CN 201580041233A CN 106795150 B CN106795150 B CN 106795150B
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acetamide
amino
thiadiazol
methoxy
phenyl
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Chinese (zh)
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CN106795150A (zh
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M·R·V·芬利
C·T·埃库卢
M·D·查理斯
P·A·罗博
J·J·G·温特
J·W·M·尼斯克
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Cancer Research Technology Ltd
AstraZeneca AB
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Cancer Research Technology Ltd
AstraZeneca AB
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    • 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
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433Thidiazoles
    • 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201580041233.9A 2014-05-30 2015-05-27 1,3,4-噻二唑化合物及其在治疗癌症中的用途 Active CN106795150B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1409624.2 2014-05-30
GBGB1409624.2A GB201409624D0 (en) 2014-05-30 2014-05-30 1,3,4-thiadiazole compounds and their use in treating cancer
PCT/GB2015/051537 WO2015181539A1 (en) 2014-05-30 2015-05-27 1, 3, 4-thiadiazole compounds and their use in treating cancer

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CN106795150A CN106795150A (zh) 2017-05-31
CN106795150B true CN106795150B (zh) 2019-10-15

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Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201520959D0 (en) 2015-11-27 2016-01-13 Astrazeneca Ab And Cancer Res Technology Ltd Bis-pyridazine compounds and their use in treating cancer
US9938265B2 (en) * 2015-11-30 2018-04-10 Astrazeneca Ab 1,3,4-thiadiazole compounds and their use in treating cancer
US10323028B2 (en) 2015-11-30 2019-06-18 Astrazeneca Ab 1,3,4-thiadiazole compounds and their use in treating cancer
US10040789B2 (en) * 2015-11-30 2018-08-07 Astrazeneca Ab 1,3,4-thiadiazole compounds and their use in treating cancer
JP7275053B2 (ja) * 2017-06-13 2023-05-17 メッドシャイン ディスカバリー インコーポレイテッド Gls1阻害剤としての化合物
JP2019064976A (ja) * 2017-10-03 2019-04-25 国立大学法人 熊本大学 抗がん剤
JP7026852B2 (ja) * 2018-10-16 2022-02-28 メッドシャイン ディスカバリー インコーポレイテッド チアジアゾール誘導体及びgls1阻害剤としてのその使用
CN113508118B (zh) * 2019-03-05 2024-07-19 阿斯利康(瑞典)有限公司 用作抗癌剂的稠合三环化合物
WO2024233839A1 (en) * 2023-05-10 2024-11-14 Leal Therapeutics, Inc. Small molecule inhibitors of glutaminase
CN116854582B (zh) * 2023-07-10 2025-08-29 泰州葛林美克医药科技有限公司 一种对映纯α-甲氧基苯乙酸的制备方法
CN117003745B (zh) * 2023-07-20 2024-06-07 南京市第一医院 Gls1/hdac双靶点抑制剂及其合成方法和应用
WO2025196447A1 (en) 2024-03-22 2025-09-25 Sitryx Therapeutics Limited Thiadiazoles as glutaminase 1 inhibitors
WO2025196446A1 (en) 2024-03-22 2025-09-25 Sitryx Therapeutics Limited Thiadiazoles as glutaminase 1 inhibitors

Citations (2)

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WO2013078123A1 (en) * 2011-11-21 2013-05-30 Calithera Biosciences Inc. Heterocyclic inhibitors of glutaminase
US20140142081A1 (en) * 2012-11-22 2014-05-22 Agios Pharmaceuticals, Inc Compounds and their methods of use

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DE60332475D1 (de) * 2002-10-30 2010-06-17 Vertex Pharma Zusammensetzungen verwendbar für die hemmung von rock und anderen kinasen
WO2012170664A2 (en) 2011-06-10 2012-12-13 President And Fellows Of Harvard College Methods of cancer treatment and prevention through the modulation of sirt4 activity
EP2895623B1 (en) * 2012-09-17 2018-08-22 Agios Pharmaceuticals, Inc. Use of e-cadherin and vimentin for selection of treatment responsive patients
RS62447B1 (sr) 2012-11-16 2021-11-30 Calithera Biosciences Inc Heterociklični inhibitori glutaminaze
EP2922832B1 (en) 2012-11-21 2019-10-09 Agios Pharmaceuticals, Inc. Glutaminase inhibitors and methods of use
WO2014079011A1 (en) 2012-11-22 2014-05-30 Agios Pharmaceuticals, Inc. Heterocyclic compounds for inhibiting glutaminase and their methods of use
CA2892817A1 (en) 2012-12-03 2014-06-12 Calithera Biosciences Inc. Treatment of cancer with heterocyclic inhibitors of glutaminase

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013078123A1 (en) * 2011-11-21 2013-05-30 Calithera Biosciences Inc. Heterocyclic inhibitors of glutaminase
US20140142081A1 (en) * 2012-11-22 2014-05-22 Agios Pharmaceuticals, Inc Compounds and their methods of use

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Small Molecule Glutaminase Inhibitors Block Glutamate Release from Stimulated Microglia;Ajit G. Thomas,等;《Biochem. Biophys. Res. Commun》;20140103;第443卷(第1期);第32–36页 *

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EA201692260A1 (ru) 2017-06-30
CA2949598C (en) 2022-08-09
NI201600176A (es) 2017-08-25
PE20170148A1 (es) 2017-04-05
HUE039879T2 (hu) 2019-02-28
SG11201609880QA (en) 2016-12-29
DK3148994T3 (en) 2018-10-08
SV2016005330A (es) 2017-06-07
AR100694A1 (es) 2016-10-26
KR20170005875A (ko) 2017-01-16
HRP20181490T1 (hr) 2019-01-11
SI3148994T1 (sl) 2018-12-31
PT3148994T (pt) 2018-10-22
PH12016502394A1 (en) 2017-02-20
US10040788B2 (en) 2018-08-07
AU2015265703A1 (en) 2016-12-15
TN2016000511A1 (en) 2018-04-04
US20180305349A1 (en) 2018-10-25
CL2016003074A1 (es) 2017-04-28
CR20160558A (es) 2017-09-01
AP2016009578A0 (en) 2016-11-30
IL249020A0 (en) 2017-01-31
PL3148994T3 (pl) 2019-04-30
EP3148994B1 (en) 2018-07-11
UY36145A (es) 2016-01-08
MY192861A (en) 2022-09-13
CA2949598A1 (en) 2015-12-03
DOP2016000308A (es) 2017-03-15
TW201609720A (zh) 2016-03-16
NZ726790A (en) 2017-11-24
IL249020B (en) 2020-11-30
US10294221B2 (en) 2019-05-21
AU2015265703B2 (en) 2017-12-07
JP2017516859A (ja) 2017-06-22
CN106795150A (zh) 2017-05-31
JP6538830B2 (ja) 2019-07-03
WO2015181539A1 (en) 2015-12-03
BR112016028002B1 (pt) 2022-09-27
EP3148994A1 (en) 2017-04-05
ES2688396T3 (es) 2018-11-02
RS57876B1 (sr) 2018-12-31
US20170197954A1 (en) 2017-07-13
LT3148994T (lt) 2018-11-26
SMT201800516T1 (it) 2018-11-09
TWI693220B (zh) 2020-05-11
CY1120836T1 (el) 2019-12-11
EA030937B1 (ru) 2018-10-31
GB201409624D0 (en) 2014-07-16
MX2016015738A (es) 2017-02-27
GT201600250A (es) 2019-06-10
BR112016028002A2 (enExample) 2017-08-22

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