CN111225903B - 谷氨酰胺酶抑制剂疗法 - Google Patents

谷氨酰胺酶抑制剂疗法 Download PDF

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CN111225903B
CN111225903B CN201880067288.0A CN201880067288A CN111225903B CN 111225903 B CN111225903 B CN 111225903B CN 201880067288 A CN201880067288 A CN 201880067288A CN 111225903 B CN111225903 B CN 111225903B
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haloalkyl
cancer
heteroaryl
cycloalkyl
alkyl
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CN111225903A (zh
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T·赫弗南
J·科瓦奇
N·斯彭斯
C·A·里斯托
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University of Texas System
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/28Compounds containing heavy metals
    • A61K31/282Platinum compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/41961,2,4-Triazoles
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/24Heavy metals; Compounds thereof
    • A61K33/243Platinum; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57545Immunoassay; Biospecific binding assay; Materials therefor for cancer of the ovaries
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/0404Lipids, e.g. triglycerides; Polycationic carriers
    • A61K51/0408Phospholipids

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Inorganic Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Microbiology (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Food Science & Technology (AREA)
  • Cell Biology (AREA)
  • Biotechnology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201880067288.0A 2017-10-18 2018-10-18 谷氨酰胺酶抑制剂疗法 Active CN111225903B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762573906P 2017-10-18 2017-10-18
US62/573,906 2017-10-18
PCT/US2018/056567 WO2019079632A1 (en) 2017-10-18 2018-10-18 GLUTAMINASE INHIBITOR THERAPY

Publications (2)

Publication Number Publication Date
CN111225903A CN111225903A (zh) 2020-06-02
CN111225903B true CN111225903B (zh) 2024-08-16

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US (4) US10722487B2 (https=)
EP (1) EP3697764B1 (https=)
JP (1) JP7361687B2 (https=)
CN (1) CN111225903B (https=)
ES (1) ES3040089T3 (https=)
RU (1) RU2020112558A (https=)
WO (1) WO2019079632A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016004404A2 (en) 2014-07-03 2016-01-07 Board Of Regents, University Of Texas System Gls1 inhibitors for treating disease
WO2017004359A1 (en) 2015-06-30 2017-01-05 Board Of Regents, University Of Texas System Gls1 inhibitors for treating disease
SG11201804664XA (en) 2015-12-22 2018-07-30 Univ Texas Salt forms and polymorphs of (r)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl) acetamido) pyridazin-3-yl)-2-fluorobutyl)-n-methyl-1h-1,2,3-triazole-4-carboxamide
RU2020112558A (ru) 2017-10-18 2021-11-18 Боард Оф Регентс, Зе Юниверсити Оф Тексас Систем Терапия на основе ингибитора глутаминазы
WO2021076814A1 (en) * 2019-10-15 2021-04-22 Cornell University Methods of inhibiting liver-type glutaminase, gls2
CN112791087B (zh) * 2020-06-05 2023-06-30 厦门大学附属中山医院 Bptes在制备预防或治疗炭疽病的药物中的用途
WO2022122044A1 (zh) * 2020-12-11 2022-06-16 杭州紫晶医药科技有限公司 作为gls1抑制剂的杂环化合物
JP2025078888A (ja) * 2022-01-28 2025-05-21 国立大学法人富山大学 グルタミナーゼ阻害剤
WO2024054074A1 (ko) * 2022-09-07 2024-03-14 재단법인 아산사회복지재단 고형암 환자의 화학요법 내성 억제용 약학 조성물 및 이의 용도
CN119326875A (zh) * 2024-12-23 2025-01-21 中国人民解放军总医院第三医学中心 L-ASNase在制备治疗膀胱癌药物中的应用及试剂盒

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016004418A1 (en) * 2014-07-03 2016-01-07 Board Of Regents, University Of Texas System Glutaminase inhibitor therapy
CN107074805A (zh) * 2014-07-03 2017-08-18 德州大学系统董事会 用于治疗疾病的gls1抑制剂

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES498337A0 (es) 1980-01-07 1982-06-01 Nyegaard & Co As Un procedimiento para la preparacion de 5-halo-pirimidin-2- onas
EP0218753B1 (en) 1985-10-10 1989-08-09 Agfa-Gevaert N.V. Image-recieving element for the silver salt diffusion transfer reversal process
WO1991009848A1 (en) 1989-12-22 1991-07-11 The Upjohn Company Pyridinones useful as antiatherosclerotic agents
IL118325A0 (en) 1995-05-25 1996-10-31 Pont Merck And Pharmaceutical Integrin receptor antagonists and pharmaceutical compositions containing them
CA2575902C (en) 1995-07-21 2010-06-08 Tactical Therapeutics Inc Treatment and prevention of neoplasms with salts of aminoimidazole carboxamide
WO1998043962A1 (en) 1997-03-28 1998-10-08 Du Pont Pharmaceuticals Company Heterocyclic integrin inhibitor prodrugs
EP1049693A1 (en) 1997-11-26 2000-11-08 Du Pont Pharmaceuticals Company 1,3,4-THIADIAZOLES AND 1,3,4-OXADIAZOLES AS $g(a) v?$g(b) 3? ANTAGONISTS
US6451828B1 (en) 2000-08-10 2002-09-17 Elan Pharmaceuticals, Inc. Selective inhibition of glutaminase by bis-thiadiazoles
NZ532635A (en) * 2001-11-13 2007-05-31 Univ Pennsylvania A method of identifying unknown adeno-associated virus (AAV) sequences and a kit for the method
SE0400208D0 (sv) 2004-02-02 2004-02-02 Astrazeneca Ab Chemical compounds
US7985548B2 (en) 2006-03-03 2011-07-26 The United States Of America As Represented By The Department Of Health And Human Services Materials and methods directed to asparagine synthetase and asparaginase therapies
US7638541B2 (en) 2006-12-28 2009-12-29 Metabolex Inc. 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
CA2686933A1 (en) 2007-04-06 2008-10-16 The Johns Hopkins University Methods and compositions for the treatment of cancer
JP5368485B2 (ja) 2008-02-25 2013-12-18 エフ.ホフマン−ラ ロシュ アーゲー ピロロピラジンキナーゼインヒビター
PT2300013T (pt) 2008-05-21 2017-10-31 Ariad Pharma Inc Derivados de fósforo como inibidores de cinases
JP2011231015A (ja) 2008-08-29 2011-11-17 Taiho Yakuhin Kogyo Kk 含窒素複素環を有する新規ウラシル化合物又はその塩
KR101411889B1 (ko) 2009-02-27 2014-06-27 이난타 파마슈티칼스, 인코포레이티드 C형 간염 바이러스 억제제
US10532034B2 (en) 2009-03-25 2020-01-14 Cornell University Inhibition of glutaminase C
JP5725475B2 (ja) 2010-01-21 2015-05-27 公立大学法人名古屋市立大学 ヒドロキサム酸誘導体及びそれを用いたhdac8阻害剤
US20130109643A1 (en) 2010-05-10 2013-05-02 The Johns Hopkins University Metabolic inhibitor against tumors having an idh mutation
ES2761866T3 (es) 2011-11-21 2020-05-21 Calithera Biosciences Inc Inhibidores heterocíclicos de glutaminasa
US8604016B2 (en) 2011-11-21 2013-12-10 Calithera Biosciences Inc. Heterocyclic inhibitors of glutaminase
BR112015010955A2 (pt) 2012-11-16 2017-07-11 Calithera Biosciences Inc inibidores de glutaminase heterocíclica
SG11201504022RA (en) 2012-11-21 2015-06-29 Agios Pharmaceuticals Inc Glutamase inhibitors and method of use
WO2014079011A1 (en) 2012-11-22 2014-05-30 Agios Pharmaceuticals, Inc. Heterocyclic compounds for inhibiting glutaminase and their methods of use
US9029531B2 (en) 2012-11-22 2015-05-12 Agios Pharmaceuticals, Inc. Compounds and their methods of use
BR112015012536A2 (pt) 2012-12-03 2017-07-11 Calithera Biosciences Inc tratamento de câncer com inibidores heterocíclicos da glutaminase
BR112015016310B1 (pt) 2013-01-30 2020-12-22 Sumitomo Chemical Company, Limited composto de amida, agente de controle e método para controlar peste artrópode
TW201500356A (zh) 2013-04-12 2015-01-01 Lilly Co Eli 二氫吡啶并嘧啶化合物
CA2934700A1 (en) 2014-01-06 2015-07-09 Rhizen Pharmaceuticals Sa Glutaminase inhibitors
US20160002204A1 (en) 2014-07-03 2016-01-07 Board Of Regents, The University Of Texas System Gls1 inhibitors for treating disease
WO2016004413A2 (en) 2014-07-03 2016-01-07 Board Of Regents, University Of Texas System Gls1 inhibitors for treating disease
US20160058759A1 (en) 2014-07-03 2016-03-03 Board Of Regents, The University Of Texas System Glutaminase inhibitor therapy
WO2017004359A1 (en) 2015-06-30 2017-01-05 Board Of Regents, University Of Texas System Gls1 inhibitors for treating disease
SG11201804664XA (en) 2015-12-22 2018-07-30 Univ Texas Salt forms and polymorphs of (r)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl) acetamido) pyridazin-3-yl)-2-fluorobutyl)-n-methyl-1h-1,2,3-triazole-4-carboxamide
RU2020112558A (ru) * 2017-10-18 2021-11-18 Боард Оф Регентс, Зе Юниверсити Оф Тексас Систем Терапия на основе ингибитора глутаминазы

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016004418A1 (en) * 2014-07-03 2016-01-07 Board Of Regents, University Of Texas System Glutaminase inhibitor therapy
CN107074805A (zh) * 2014-07-03 2017-08-18 德州大学系统董事会 用于治疗疾病的gls1抑制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Deficiency in asparagine synthetase expression in rectal cancers receiving concurrent chemoradiotherapy: negative prognostic impact and therapeutic relevance;Ching-Yih Lin et al.;《Tumor Biol.》;摘要 *

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ES3040089T3 (en) 2025-10-28
EP3697764A4 (en) 2021-07-21
US20220016069A1 (en) 2022-01-20
JP7361687B2 (ja) 2023-10-16
JP2021500335A (ja) 2021-01-07
US20240165070A1 (en) 2024-05-23
US11045443B2 (en) 2021-06-29
US20190274993A1 (en) 2019-09-12
WO2019079632A1 (en) 2019-04-25
RU2020112558A (ru) 2021-11-18
EP3697764B1 (en) 2025-06-11
RU2020112558A3 (https=) 2022-03-21
US11786500B2 (en) 2023-10-17
US20200368196A1 (en) 2020-11-26
CN111225903A (zh) 2020-06-02
US12336976B2 (en) 2025-06-24
US10722487B2 (en) 2020-07-28
EP3697764A1 (en) 2020-08-26

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