KR102220175B1 - 헤테로사이클릭 글루타미나아제 억제제 - Google Patents

헤테로사이클릭 글루타미나아제 억제제 Download PDF

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KR102220175B1
KR102220175B1 KR1020157015874A KR20157015874A KR102220175B1 KR 102220175 B1 KR102220175 B1 KR 102220175B1 KR 1020157015874 A KR1020157015874 A KR 1020157015874A KR 20157015874 A KR20157015874 A KR 20157015874A KR 102220175 B1 KR102220175 B1 KR 102220175B1
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cancer
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KR20150085053A (ko
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짐 리
리징 첸
빈두 고얄
가이 라이딕
티모시 프랜드 스탠톤
에릭 브라이언 쇼그렌
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칼리테라 바이오사이언시즈, 인코포레이티드
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    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles 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
    • A61K31/495—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135—Nitrogen atoms
    • 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
    • C07D417/02—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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020157015874A 2012-11-16 2013-11-15 헤테로사이클릭 글루타미나아제 억제제 Active KR102220175B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261727195P 2012-11-16 2012-11-16
US61/727,195 2012-11-16
US201361824434P 2013-05-17 2013-05-17
US61/824,434 2013-05-17
PCT/US2013/070277 WO2014078645A1 (en) 2012-11-16 2013-11-15 Heterocyclic glutaminase inhibitors

Publications (2)

Publication Number Publication Date
KR20150085053A KR20150085053A (ko) 2015-07-22
KR102220175B1 true KR102220175B1 (ko) 2021-02-24

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US (2) US10793535B2 (enExample)
EP (2) EP3954686A1 (enExample)
JP (1) JP6275153B2 (enExample)
KR (1) KR102220175B1 (enExample)
CN (1) CN105051041B (enExample)
AU (1) AU2013344560B2 (enExample)
BR (1) BR112015010955A2 (enExample)
CA (1) CA2891667A1 (enExample)
CY (1) CY1125279T1 (enExample)
DK (1) DK2920168T3 (enExample)
EA (1) EA029707B1 (enExample)
ES (1) ES2899461T3 (enExample)
HR (1) HRP20211610T1 (enExample)
HU (1) HUE056078T2 (enExample)
IL (1) IL238787A0 (enExample)
LT (1) LT2920168T (enExample)
MX (1) MX381260B (enExample)
PL (1) PL2920168T3 (enExample)
PT (1) PT2920168T (enExample)
RS (1) RS62447B1 (enExample)
SG (1) SG11201503720SA (enExample)
SI (1) SI2920168T1 (enExample)
SM (1) SMT202100589T1 (enExample)
WO (1) WO2014078645A1 (enExample)
ZA (2) ZA201504294B (enExample)

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EP3092235A2 (en) 2014-01-06 2016-11-16 Rhizen Pharmaceuticals S.A. Novel inhibitors of glutaminase
MX2016014143A (es) * 2014-04-30 2017-02-15 Pfizer Derivados de diheterociclo enlazado a cicloalquilo.
GB201409624D0 (en) 2014-05-30 2014-07-16 Astrazeneca Ab 1,3,4-thiadiazole compounds and their use in treating cancer
AU2015274361B2 (en) * 2014-06-13 2020-11-05 Calithera Biosciences, Inc. Combination therapy with glutaminase inhibitors
WO2016004413A2 (en) * 2014-07-03 2016-01-07 Board Of Regents, University Of Texas System Gls1 inhibitors for treating disease
ES2921989T3 (es) * 2014-07-03 2022-09-05 Univ Texas Terapia con inhibidores de glutaminasa
CN107074805B (zh) 2014-07-03 2021-02-26 德州大学系统董事会 用于治疗疾病的gls1抑制剂
WO2016007647A1 (en) * 2014-07-09 2016-01-14 The Johns Hopkins University Glutaminase inhibitor discovery and nanoparticle-enhanced delivery for cancer therapy
EA037738B1 (ru) * 2014-08-07 2021-05-17 Калитера Байосайенсиз, Инк. Кристаллические формы ингибиторов глутаминазы
JP6768693B2 (ja) * 2015-03-30 2020-10-14 キャリセラ バイオサイエンシーズ， インコーポレイテッド グルタミナーゼ阻害剤を投与する方法
US10441587B2 (en) * 2015-04-06 2019-10-15 Calithera Biosciences, Inc. Treatment of lung cancer with inhibitors of glutaminase
EP3316887B1 (en) 2015-06-30 2020-04-08 Board of Regents, The University of Texas System Gls1 inhibitors for treating disease
WO2017062354A1 (en) 2015-10-05 2017-04-13 Calithera Biosciences, Inc. Combination therapy with glutaminase inhibitors and immuno-oncology agents
US10323028B2 (en) * 2015-11-30 2019-06-18 Astrazeneca Ab 1,3,4-thiadiazole 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
US10150753B2 (en) 2015-12-22 2018-12-11 Board Of Regents, The University Of Texas System Salt forms and polymorphs of (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyrdin-2-yl)acetamido) pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide
CN109982703A (zh) 2016-08-25 2019-07-05 卡利泰拉生物科技公司 用谷氨酰胺酶抑制剂的组合疗法
WO2018039544A1 (en) * 2016-08-25 2018-03-01 Calithera Biosciences, Inc. Combination therapy with glutaminase inhibitors
US20180055825A1 (en) * 2016-08-25 2018-03-01 Yu Liang Treatment of cancer with inhibitors of glutaminase
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
JP7361687B2 (ja) 2017-10-18 2023-10-16 ボード オブ レジェンツ，ザ ユニバーシティ オブ テキサス システム グルタミナーゼ阻害薬療法
CN110746416A (zh) * 2019-09-05 2020-02-04 中国药科大学 含有三氮唑结构的谷氨酰胺酶gls1抑制剂或其可药用的盐、其制备方法及用途
CN114805346A (zh) * 2021-07-08 2022-07-29 成都硕德药业有限公司 杂环类衍生物、其制备方法及用途

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EA037738B1 (ru) 2014-08-07 2021-05-17 Калитера Байосайенсиз, Инк. Кристаллические формы ингибиторов глутаминазы
JP6768693B2 (ja) 2015-03-30 2020-10-14 キャリセラ バイオサイエンシーズ， インコーポレイテッド グルタミナーゼ阻害剤を投与する方法
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WO2017062354A1 (en) 2015-10-05 2017-04-13 Calithera Biosciences, Inc. Combination therapy with glutaminase inhibitors and immuno-oncology agents
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Patent Citations (3)

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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
WO2011143160A2 (en) 2010-05-10 2011-11-17 The Johns Hopkins University Metabolic inhibitor against tumors having an idh mutation
KR102042290B1 (ko) * 2011-11-21 2019-11-07 칼리테라 바이오사이언시즈, 인코포레이티드 글루타미나제의 헤테로사이클릭 억제제

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CA2891667A1 (en) 2014-05-22
US20140194421A1 (en) 2014-07-10
CN105051041A (zh) 2015-11-11
ZA201504294B (en) 2018-12-19
SI2920168T1 (sl) 2022-01-31
HK1215023A1 (zh) 2016-08-12
SG11201503720SA (en) 2015-06-29
RS62447B1 (sr) 2021-11-30
JP6275153B2 (ja) 2018-02-07
CY1125279T1 (el) 2023-03-24
LT2920168T (lt) 2021-10-25
IL238787A0 (en) 2015-06-30
HUE056078T2 (hu) 2022-01-28
PT2920168T (pt) 2021-10-18
CN105051041B (zh) 2018-03-30
EP3954686A1 (en) 2022-02-16
ZA201606590B (en) 2019-04-24
HRP20211610T1 (hr) 2022-02-04
JP2016505526A (ja) 2016-02-25
EP2920168A4 (en) 2016-04-20
BR112015010955A2 (pt) 2017-07-11
SMT202100589T1 (it) 2021-11-12
MX381260B (es) 2025-03-12
KR20150085053A (ko) 2015-07-22
AU2013344560B2 (en) 2017-09-14
EA029707B1 (ru) 2018-05-31
US10793535B2 (en) 2020-10-06
WO2014078645A1 (en) 2014-05-22
EA201590941A1 (ru) 2016-02-29
PL2920168T3 (pl) 2022-01-03
EP2920168A1 (en) 2015-09-23
EP2920168B1 (en) 2021-07-21
US20210292289A1 (en) 2021-09-23
DK2920168T3 (da) 2021-10-18
MX2015005963A (es) 2015-09-16
ES2899461T3 (es) 2022-03-11

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