CN108349966B - 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
CN108349966B
CN108349966B CN201680067245.3A CN201680067245A CN108349966B CN 108349966 B CN108349966 B CN 108349966B CN 201680067245 A CN201680067245 A CN 201680067245A CN 108349966 B CN108349966 B CN 108349966B
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Prior art keywords
methoxy
phenyl
thiadiazol
acetamide
pyridazin
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CN201680067245.3A
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English (en)
Chinese (zh)
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CN108349966A (zh
Inventor
M.R.V.芬莱
J.W.M.尼辛克
M.D.查尔斯
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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
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201680067245.3A 2015-11-30 2016-11-30 1,3,4-噻二唑化合物及其在治疗癌症中的用途 Active CN108349966B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562260789P 2015-11-30 2015-11-30
US62/260789 2015-11-30
PCT/EP2016/079250 WO2017093299A1 (en) 2015-11-30 2016-11-30 1,3,4-thiadiazole compounds and their use in treating cancer

Publications (2)

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CN108349966A CN108349966A (zh) 2018-07-31
CN108349966B true CN108349966B (zh) 2022-02-15

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US (3) US10323028B2 (enExample)
EP (1) EP3383873B1 (enExample)
JP (1) JP6999550B2 (enExample)
KR (1) KR20180083942A (enExample)
CN (1) CN108349966B (enExample)
AR (1) AR106874A1 (enExample)
AU (1) AU2016363718B2 (enExample)
BR (1) BR112018010806A2 (enExample)
CA (1) CA3005495C (enExample)
CL (1) CL2018001407A1 (enExample)
CO (1) CO2018006928A2 (enExample)
EA (1) EA201891241A1 (enExample)
ES (1) ES2914333T3 (enExample)
IL (1) IL259510A (enExample)
MX (1) MX2018006532A (enExample)
NI (1) NI201800064A (enExample)
PH (1) PH12018501131A1 (enExample)
RU (1) RU2018123714A (enExample)
SG (1) SG11201803810XA (enExample)
SV (1) SV2018005702A (enExample)
TN (1) TN2018000127A1 (enExample)
TW (1) TW201733587A (enExample)
WO (1) WO2017093299A1 (enExample)

Families Citing this family (7)

* 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
TW201733587A (zh) 2015-11-30 2017-10-01 阿斯特捷利康公司 1,3,4-噻二唑化合物及其在治療癌症中之用途
TW201731511A (zh) * 2015-11-30 2017-09-16 阿斯特捷利康公司 1,3,4-噻二唑化合物及其在治療癌症中之用途
US9938265B2 (en) 2015-11-30 2018-04-10 Astrazeneca Ab 1,3,4-thiadiazole compounds and their use in treating cancer
ES2903182T3 (es) * 2017-06-13 2022-03-31 Medshine Discovery Inc Compuesto como inhibidor GLS1
WO2020078350A1 (zh) * 2018-10-16 2020-04-23 南京明德新药研发有限公司 噻二唑衍生物及其作为gls1抑制剂的应用
WO2025196446A1 (en) * 2024-03-22 2025-09-25 Sitryx Therapeutics Limited Thiadiazoles as glutaminase 1 inhibitors

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020115698A1 (en) * 2000-08-10 2002-08-22 Newcomb Robert W. Selective inhibition of glutaminase by bis-thiadiazoles
WO2015138902A1 (en) * 2014-03-14 2015-09-17 Calithera Biosciences, Inc. Combination therapy with glutaminase inhibitors
CN105051041A (zh) * 2012-11-16 2015-11-11 卡利泰拉生物科技公司 杂环谷氨酰胺酶抑制剂
WO2015181539A1 (en) * 2014-05-30 2015-12-03 Astrazeneca Ab 1, 3, 4-thiadiazole compounds and their use in treating cancer

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2761866T3 (es) * 2011-11-21 2020-05-21 Calithera Biosciences Inc Inhibidores heterocíclicos de glutaminasa
US9029531B2 (en) 2012-11-22 2015-05-12 Agios Pharmaceuticals, Inc. Compounds and their methods of use
CN111892589A (zh) 2014-01-06 2020-11-06 理森制药股份公司 谷氨酰胺酶抑制剂
GB201520959D0 (en) 2015-11-27 2016-01-13 Astrazeneca Ab And Cancer Res Technology Ltd Bis-pyridazine compounds and their use in treating cancer
TW201733587A (zh) 2015-11-30 2017-10-01 阿斯特捷利康公司 1,3,4-噻二唑化合物及其在治療癌症中之用途
TW201731511A (zh) 2015-11-30 2017-09-16 阿斯特捷利康公司 1,3,4-噻二唑化合物及其在治療癌症中之用途
US9938265B2 (en) * 2015-11-30 2018-04-10 Astrazeneca Ab 1,3,4-thiadiazole compounds and their use in treating cancer

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020115698A1 (en) * 2000-08-10 2002-08-22 Newcomb Robert W. Selective inhibition of glutaminase by bis-thiadiazoles
CN105051041A (zh) * 2012-11-16 2015-11-11 卡利泰拉生物科技公司 杂环谷氨酰胺酶抑制剂
WO2015138902A1 (en) * 2014-03-14 2015-09-17 Calithera Biosciences, Inc. Combination therapy with glutaminase inhibitors
WO2015181539A1 (en) * 2014-05-30 2015-12-03 Astrazeneca Ab 1, 3, 4-thiadiazole compounds and their use in treating cancer

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Design, Synthesis, and Pharmacological Evaluation of Bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl Sulfide 3 (BPTES) Analogs as Glutaminase Inhibitors;Krupa Shukla et al.;《Journal of Medicinal Chemistry》;20121114;第55卷;第10551-10563页 *

Also Published As

Publication number Publication date
PH12018501131A1 (en) 2019-01-21
CN108349966A (zh) 2018-07-31
EP3383873B1 (en) 2022-03-09
JP6999550B2 (ja) 2022-02-10
CA3005495A1 (en) 2017-06-08
AR106874A1 (es) 2018-02-28
CO2018006928A2 (es) 2018-10-10
ES2914333T3 (es) 2022-06-09
US20210246131A1 (en) 2021-08-12
CA3005495C (en) 2023-12-12
TN2018000127A1 (en) 2019-10-04
IL259510A (en) 2018-07-31
JP2018535986A (ja) 2018-12-06
US10323028B2 (en) 2019-06-18
CL2018001407A1 (es) 2018-10-12
EP3383873A1 (en) 2018-10-10
SG11201803810XA (en) 2018-06-28
AU2016363718B2 (en) 2019-11-14
US20190389853A1 (en) 2019-12-26
RU2018123714A (ru) 2020-01-09
US11753405B2 (en) 2023-09-12
US10981904B2 (en) 2021-04-20
SV2018005702A (es) 2018-11-27
MX2018006532A (es) 2019-05-15
US20170152255A1 (en) 2017-06-01
AU2016363718A1 (en) 2018-07-12
EA201891241A1 (ru) 2019-01-31
TW201733587A (zh) 2017-10-01
NI201800064A (es) 2018-10-18
BR112018010806A2 (pt) 2018-11-27
WO2017093299A1 (en) 2017-06-08
KR20180083942A (ko) 2018-07-23

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