CN108349967B - 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
CN108349967B
CN108349967B CN201680067261.2A CN201680067261A CN108349967B CN 108349967 B CN108349967 B CN 108349967B CN 201680067261 A CN201680067261 A CN 201680067261A CN 108349967 B CN108349967 B CN 108349967B
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China
Prior art keywords
methoxy
pyrrolidin
acetamide
methylpyridazin
thiadiazol
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CN201680067261.2A
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Chinese (zh)
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CN108349967A (zh
Inventor
M.R.V.芬莱
J.W.M.尼辛克
M.D.查尔斯
M.J.伍德
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Cancer Research Technology Ltd
AstraZeneca AB
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Cancer Research Technology Ltd
AstraZeneca AB
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/53—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
CN201680067261.2A 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 CN108349967B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562260787P 2015-11-30 2015-11-30
US62/260787 2015-11-30
PCT/EP2016/079251 WO2017093300A1 (en) 2015-11-30 2016-11-30 1,3,4-thiadiazole compounds and their use in treating cancer

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CN108349967A CN108349967A (zh) 2018-07-31
CN108349967B true CN108349967B (zh) 2022-02-15

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US (1) US9938265B2 (enExample)
EP (1) EP3383871B1 (enExample)
JP (1) JP6873132B2 (enExample)
KR (1) KR20180083412A (enExample)
CN (1) CN108349967B (enExample)
AR (1) AR106876A1 (enExample)
AU (1) AU2016363719B2 (enExample)
BR (1) BR112018010812A2 (enExample)
CA (1) CA3005516C (enExample)
CL (1) CL2018001408A1 (enExample)
CO (1) CO2018006929A2 (enExample)
DK (1) DK3383871T3 (enExample)
DO (1) DOP2018000134A (enExample)
EA (1) EA201891240A1 (enExample)
ES (1) ES2759940T3 (enExample)
IL (1) IL258644A (enExample)
MX (1) MX2018006528A (enExample)
NI (1) NI201800065A (enExample)
PE (1) PE20181450A1 (enExample)
PH (1) PH12018501132A1 (enExample)
SG (1) SG11201803813UA (enExample)
SV (1) SV2018005701A (enExample)
TN (1) TN2018000126A1 (enExample)
TW (1) TW201730188A (enExample)
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Families Citing this family (5)

* 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
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 (9)

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JP2003514910A (ja) * 1999-11-24 2003-04-22 メルク エンド カムパニー インコーポレーテッド Ｈｉｖプロテアーゼ阻害剤としてのガンマ−ヒドロキシ−２−（フルオロアルキルアミノカルボニル）−１−ピペラジンペンタンアミド類
AR044688A1 (es) * 2003-06-12 2005-09-21 Euro Celtique Sa Agentes terapeuticos utiles para el tratamiento del dolor
EP1828144A2 (en) * 2004-11-12 2007-09-05 OSI Pharmaceuticals, Inc. Integrin antagonists useful as anticancer agents
CA2758210C (en) * 2009-04-20 2017-08-29 F. Hoffmann-La Roche Ag Proline derivatives as cathepsin inhibitors
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
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
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

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 *

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Publication number Publication date
BR112018010812A2 (pt) 2018-11-27
ES2759940T3 (es) 2020-05-12
IL258644A (en) 2018-06-28
SV2018005701A (es) 2018-11-27
JP2019501134A (ja) 2019-01-17
EA201891240A1 (ru) 2018-11-30
SG11201803813UA (en) 2018-06-28
DK3383871T3 (da) 2019-12-16
CN108349967A (zh) 2018-07-31
CA3005516C (en) 2024-04-16
MX2018006528A (es) 2019-05-15
NI201800065A (es) 2018-10-18
CL2018001408A1 (es) 2018-10-12
US9938265B2 (en) 2018-04-10
WO2017093300A1 (en) 2017-06-08
KR20180083412A (ko) 2018-07-20
ES2759940T8 (es) 2020-05-20
CA3005516A1 (en) 2017-06-08
EP3383871A1 (en) 2018-10-10
AU2016363719A8 (en) 2018-07-12
AU2016363719A1 (en) 2018-07-05
PH12018501132A1 (en) 2019-01-21
EP3383871B1 (en) 2019-09-11
CO2018006929A2 (es) 2018-10-10
TN2018000126A1 (en) 2019-10-04
DOP2018000134A (es) 2018-06-30
PE20181450A1 (es) 2018-09-12
AR106876A1 (es) 2018-02-28
TW201730188A (zh) 2017-09-01
AU2016363719B2 (en) 2019-11-14
US20170152254A1 (en) 2017-06-01
JP6873132B2 (ja) 2021-05-19

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