EA030646B1 - Соединения и способы их применения - Google Patents

Соединения и способы их применения Download PDF

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Publication number
EA030646B1
EA030646B1 EA201590987A EA201590987A EA030646B1 EA 030646 B1 EA030646 B1 EA 030646B1 EA 201590987 A EA201590987 A EA 201590987A EA 201590987 A EA201590987 A EA 201590987A EA 030646 B1 EA030646 B1 EA 030646B1
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EA
Eurasian Patent Office
Prior art keywords
compound
bis
diyl
pharmaceutically acceptable
acceptable salt
Prior art date
Application number
EA201590987A
Other languages
English (en)
Russian (ru)
Other versions
EA201590987A1 (ru
Inventor
Рене М. Лемье
Джанета Поповичи-Мюллер
Франческо Г. Салитуро
Джеффри О. Сондерз
Джереми М. Трэвинс
Юншэн Чэнь
Original Assignee
Аджиос Фармасьютикалз, Инк.
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Application filed by Аджиос Фармасьютикалз, Инк. filed Critical Аджиос Фармасьютикалз, Инк.
Publication of EA201590987A1 publication Critical patent/EA201590987A1/ru
Publication of EA030646B1 publication Critical patent/EA030646B1/ru

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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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/121,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/1251,3,4-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
    • C07D285/135Nitrogen atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
EA201590987A 2012-11-22 2013-11-21 Соединения и способы их применения EA030646B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/CN2012/085023 WO2014079011A1 (en) 2012-11-22 2012-11-22 Heterocyclic compounds for inhibiting glutaminase and their methods of use
PCT/CN2013/000294 WO2014079136A1 (en) 2012-11-22 2013-03-15 Compounds, pharmaceutical compositions and uses as glutaminase inhibitors for treating cancers thereof
PCT/CN2013/001428 WO2014079150A1 (en) 2012-11-22 2013-11-21 Compounds and their methods of use

Publications (2)

Publication Number Publication Date
EA201590987A1 EA201590987A1 (ru) 2015-12-30
EA030646B1 true EA030646B1 (ru) 2018-09-28

Family

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Family Applications (2)

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EA201590987A EA030646B1 (ru) 2012-11-22 2013-11-21 Соединения и способы их применения
EA201890754A EA201890754A1 (ru) 2012-11-22 2013-11-21 Соединения и способы их применения

Family Applications After (1)

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EA201890754A EA201890754A1 (ru) 2012-11-22 2013-11-21 Соединения и способы их применения

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EP (2) EP3456719A1 (enExample)
JP (2) JP6333277B2 (enExample)
KR (1) KR20150085079A (enExample)
CN (2) CN104936954B (enExample)
AR (1) AR093598A1 (enExample)
AU (2) AU2013347771B2 (enExample)
BR (1) BR112015011830A2 (enExample)
CA (1) CA2893510C (enExample)
CL (1) CL2015001392A1 (enExample)
CR (1) CR20150316A (enExample)
CY (1) CY1120581T1 (enExample)
DK (1) DK2922850T3 (enExample)
EA (2) EA030646B1 (enExample)
EC (1) ECSP15026557A (enExample)
ES (1) ES2690390T3 (enExample)
HR (1) HRP20181628T1 (enExample)
HU (1) HUE040111T2 (enExample)
IL (1) IL238958B (enExample)
LT (1) LT2922850T (enExample)
MX (1) MX367389B (enExample)
MY (1) MY177344A (enExample)
NZ (1) NZ708382A (enExample)
PE (1) PE20151072A1 (enExample)
PH (2) PH12015501150B1 (enExample)
PL (1) PL2922850T3 (enExample)
PT (1) PT2922850T (enExample)
RS (1) RS57859B1 (enExample)
SA (1) SA515360469B1 (enExample)
SG (2) SG11201504049VA (enExample)
SI (1) SI2922850T1 (enExample)
SM (1) SMT201800504T1 (enExample)
TR (1) TR201812360T4 (enExample)
TW (2) TW201906825A (enExample)
UA (1) UA117360C2 (enExample)
WO (3) WO2014079011A1 (enExample)

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EA029531B1 (ru) 2012-11-21 2018-04-30 Аджиос Фармасьютикалз, Инк. Соединения, ингибирующие глутаминазу, и содержащие эти соединения фармацевтические композиции и их применение
WO2014079011A1 (en) 2012-11-22 2014-05-30 Agios Pharmaceuticals, Inc. Heterocyclic compounds for inhibiting glutaminase and their methods of use
MX2015006939A (es) * 2012-12-03 2015-09-08 Calithera Biosciences Inc Tratamiento de cancer con inhibidores heterociclicos de glutaminasa.
EP2943485B1 (en) 2013-01-14 2017-09-20 Incyte Holdings Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
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CN111393431A (zh) 2014-01-06 2020-07-10 理森制药股份公司 谷氨酰胺酶抑制剂
CN106231900B (zh) * 2014-03-21 2019-05-28 阿吉奥斯制药公司 化合物及其使用方法
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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
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US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
WO2016014890A1 (en) * 2014-07-24 2016-01-28 Calithera Biosciences, Inc. Treatment of multiple myeloma with heterocyclic inhibitors of glutaminase
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US10245254B2 (en) 2014-10-03 2019-04-02 University of Pittsburgh—of the Commonwealth System of Higher Education Glutaminase inhibitors
CA2981762A1 (en) 2015-04-06 2016-10-13 Calithera Biosciences, Inc. Treatment of lung cancer with inhibitors of glutaminase
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
EP3316887B1 (en) * 2015-06-30 2020-04-08 Board of Regents, The University of Texas System Gls1 inhibitors for treating disease
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
US9920032B2 (en) 2015-10-02 2018-03-20 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
US10258619B2 (en) 2015-10-05 2019-04-16 Calithera Biosciences, Inc. Combination therapy with glutaminase inhibitors and immuno-oncology agents
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
CN106890184B (zh) * 2015-12-18 2019-06-25 诺言医药科技(上海)有限公司 抗肿瘤的谷氨酰胺酶抑制剂和肿瘤血管生成抑制剂药物组合物及其应用
JP6976248B2 (ja) 2015-12-22 2021-12-08 ボード オブ リージェンツ、ザ ユニバーシテイ オブ テキサス システム (r)−1−(4−(6−(2−(4−(3,3−ジフルオロシクロブトキシ)−6−メチルピリジン−2−イル)アセトアミド)ピリダジン−3−イル)−2−フルオロブチル)−n−メチル−1h−1,2,3−トリアゾール−4−カルボキサミドの塩形態および多形体
WO2018039441A1 (en) 2016-08-25 2018-03-01 Calithera Biosciences, Inc. Combination therapy with glutaminase inhibitors
KR20190040302A (ko) * 2016-08-25 2019-04-17 칼리테라 바이오사이언시즈, 인코포레이티드 글루타미나제 억제제와의 병용 요법
EP3697764B1 (en) 2017-10-18 2025-06-11 Board Of Regents, The University Of Texas System Gls-1 inhibitors for use in the treatment of cancer
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
CA3102279A1 (en) 2018-06-01 2019-12-05 Cornell University Combination therapy for pi3k-associated disease or disorder
WO2020096916A2 (en) 2018-11-08 2020-05-14 Merck Sharp & Dohme Corp. Inhibitors of histone deacetylase useful for the treatment or prevention of hiv infection
WO2020191356A1 (en) * 2019-03-21 2020-09-24 Goncalves Marcus Anti-fructose therapy for colorectal and small intestine cancers
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
CN112898200A (zh) * 2021-01-20 2021-06-04 都创(上海)医药科技股份有限公司 5-溴-6-甲氧基吡啶-2-羧酸酯的合成方法

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MX367389B (es) 2019-08-19
CA2893510A1 (en) 2014-05-30
US20190084976A1 (en) 2019-03-21
RS57859B1 (sr) 2018-12-31
EP2922850A1 (en) 2015-09-30
KR20150085079A (ko) 2015-07-22
MX2015006493A (es) 2015-08-05
CN104936954A (zh) 2015-09-23
AU2013347771B2 (en) 2018-02-01
ECSP15026557A (es) 2016-01-29
UA117360C2 (uk) 2018-07-25
CR20150316A (es) 2015-08-28
US10087172B2 (en) 2018-10-02
CL2015001392A1 (es) 2016-04-22
CY1120581T1 (el) 2019-07-10
HRP20181628T1 (hr) 2018-12-14
IL238958B (en) 2019-09-26
EA201890754A1 (ru) 2018-08-31
WO2014079150A1 (en) 2014-05-30
DK2922850T3 (en) 2018-10-08
ES2690390T3 (es) 2018-11-20
CN108727307A (zh) 2018-11-02
SI2922850T1 (sl) 2018-10-30
AR093598A1 (es) 2015-06-10
EP2922850B1 (en) 2018-07-18
TR201812360T4 (tr) 2018-09-21
IL238958A0 (en) 2015-07-30
TWI629268B (zh) 2018-07-11
TW201906825A (zh) 2019-02-16
PL2922850T3 (pl) 2018-12-31
US20150291576A1 (en) 2015-10-15
JP2016500082A (ja) 2016-01-07
WO2014079136A1 (en) 2014-05-30
PH12015501150A1 (en) 2015-08-17
NZ708382A (en) 2020-04-24
CN104936954B (zh) 2018-08-14
US10689375B2 (en) 2020-06-23
SG11201504049VA (en) 2015-07-30
EP3456719A1 (en) 2019-03-20
PH12015501150B1 (en) 2018-05-04
HK1214593A1 (en) 2016-07-29
PE20151072A1 (es) 2015-08-26
SMT201800504T1 (it) 2018-11-09
AU2018202954A1 (en) 2018-05-17
PT2922850T (pt) 2018-10-15
AU2013347771A1 (en) 2015-06-11
HUE040111T2 (hu) 2019-02-28
PH12017502141A1 (en) 2019-02-27
CA2893510C (en) 2021-01-19
LT2922850T (lt) 2018-09-10
TW201427963A (zh) 2014-07-16
JP2018150316A (ja) 2018-09-27
MY177344A (en) 2020-09-13
SA515360469B1 (ar) 2017-07-11
BR112015011830A2 (pt) 2017-07-11
EA201590987A1 (ru) 2015-12-30
SG10201609940RA (en) 2016-12-29
EP2922850A4 (en) 2016-05-18
WO2014079011A1 (en) 2014-05-30
JP6333277B2 (ja) 2018-05-30

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