[go: up one dir, main page]
More Web Proxy on the site http://driver.im/

EA201692166A1 - Гетероциклические ингибиторы глютаминазы - Google Patents

Гетероциклические ингибиторы глютаминазы

Info

Publication number
EA201692166A1
EA201692166A1 EA201692166A EA201692166A EA201692166A1 EA 201692166 A1 EA201692166 A1 EA 201692166A1 EA 201692166 A EA201692166 A EA 201692166A EA 201692166 A EA201692166 A EA 201692166A EA 201692166 A1 EA201692166 A1 EA 201692166A1
Authority
EA
Eurasian Patent Office
Prior art keywords
gletaminase
heterocyclic inhibitors
relates
heterocyclic
compounds
Prior art date
Application number
EA201692166A
Other languages
English (en)
Inventor
Джим Ли
Лицзин Чэнь
Бинду Гоял
Гай Лайдиг
Тимоти Френд Стэнтон
Эрик Брайан Сьегрен
Original Assignee
Калитера Байосайенсиз Инк.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Калитера Байосайенсиз Инк. filed Critical Калитера Байосайенсиз Инк.
Publication of EA201692166A1 publication Critical patent/EA201692166A1/ru

Links

Classifications

    • 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
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C07D271/113—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)

Abstract

Изобретение относится к новым гетероциклическим соединениям формулы (I), определенной в настоящей заявке, и к фармацевтическим препаратам таких соединений. Изобретение также относится к способам лечения рака, иммунологических и неврологических заболеваний с использованием гетероциклических соединений по настоящему изобретению.
EA201692166A 2011-11-21 2012-11-19 Гетероциклические ингибиторы глютаминазы EA201692166A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161562266P 2011-11-21 2011-11-21
US201261665370P 2012-06-28 2012-06-28
US201261727195P 2012-11-16 2012-11-16

Publications (1)

Publication Number Publication Date
EA201692166A1 true EA201692166A1 (ru) 2017-07-31

Family

ID=48470227

Family Applications (2)

Application Number Title Priority Date Filing Date
EA201491012A EA026656B1 (ru) 2011-11-21 2012-11-19 Гетероциклические ингибиторы глютаминазы
EA201692166A EA201692166A1 (ru) 2011-11-21 2012-11-19 Гетероциклические ингибиторы глютаминазы

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EA201491012A EA026656B1 (ru) 2011-11-21 2012-11-19 Гетероциклические ингибиторы глютаминазы

Country Status (27)

Country Link
EP (2) EP2782570B1 (ru)
JP (3) JP6031527B2 (ru)
KR (2) KR20190127971A (ru)
CN (2) CN108785305B (ru)
AR (1) AR090398A1 (ru)
AU (1) AU2012340866B2 (ru)
BR (1) BR112014012129A8 (ru)
CA (1) CA2856386C (ru)
CY (1) CY1122707T1 (ru)
DK (1) DK2782570T3 (ru)
EA (2) EA026656B1 (ru)
ES (1) ES2761866T3 (ru)
HK (1) HK1204768A1 (ru)
HR (1) HRP20192144T1 (ru)
HU (1) HUE047642T2 (ru)
IL (2) IL232665A0 (ru)
LT (1) LT2782570T (ru)
MX (1) MX362550B (ru)
PL (1) PL2782570T3 (ru)
PT (1) PT2782570T (ru)
RS (1) RS59705B1 (ru)
SG (2) SG11201402305WA (ru)
SI (1) SI2782570T1 (ru)
SM (1) SMT201900738T1 (ru)
TW (1) TWI585084B (ru)
WO (1) WO2013078123A1 (ru)
ZA (2) ZA201404518B (ru)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8604016B2 (en) 2011-11-21 2013-12-10 Calithera Biosciences Inc. Heterocyclic inhibitors of glutaminase
ES2690829T3 (es) 2012-09-17 2018-11-22 Agios Pharmaceuticals, Inc. Uso de e-cadherina y vimentina para la selección de pacientes que responden al tratamiento
CN105051041B (zh) * 2012-11-16 2018-03-30 卡利泰拉生物科技公司 杂环谷氨酰胺酶抑制剂
US10011574B2 (en) * 2012-11-21 2018-07-03 Agios Pharmaceuticals, Inc. Glutaminase 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
SG11201504184PA (en) * 2012-12-03 2015-06-29 Calithera Biosciences Inc Treatment of cancer with heterocyclic inhibitors of glutaminase
US9457016B2 (en) 2013-08-29 2016-10-04 New York University Methods for treating polycystic kidney disease
WO2015061432A1 (en) * 2013-10-25 2015-04-30 Calithera Biosciences, Inc. Treatment of viral infections with inhibitors of glutaminase
EP3092235A2 (en) * 2014-01-06 2016-11-16 Rhizen Pharmaceuticals S.A. Novel inhibitors of glutaminase
CN103880777B (zh) * 2014-03-06 2015-12-30 陕西科技大学 一种制备双噻二唑二胺的方法
EP3116872A4 (en) * 2014-03-14 2017-08-30 Calithera Biosciences, Inc. Combination therapy with glutaminase inhibitors
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
CR20160497A (es) 2014-04-30 2016-12-20 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
EP3164394B1 (en) 2014-07-03 2020-04-01 Board of Regents, The University of Texas System Gls1 inhibitors for treating diseases
WO2016007647A1 (en) 2014-07-09 2016-01-14 The Johns Hopkins University Glutaminase inhibitor discovery and nanoparticle-enhanced delivery for cancer therapy
WO2016022969A1 (en) * 2014-08-07 2016-02-11 Calithera Biosciences, Inc. Crystal forms of glutaminase inhibitors
US10245254B2 (en) 2014-10-03 2019-04-02 University of Pittsburgh—of the Commonwealth System of Higher Education Glutaminase inhibitors
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
AU2016246521B2 (en) 2015-04-06 2020-07-09 Calithera Biosciences, Inc. Treatment of lung cancer with inhibitors of glutaminase
CA2990457A1 (en) 2015-06-30 2017-01-05 Board Of Regents, University Of Texas System Pyrrolidinyl and piperidinyl derivatives and pharmaceutical compositions thereof useful as gls1 inhibitors
CN108601767A (zh) * 2015-10-05 2018-09-28 卡利泰拉生物科技公司 用谷氨酰胺酶抑制剂和免疫肿瘤学药剂的组合疗法
GB201520959D0 (en) * 2015-11-27 2016-01-13 Astrazeneca Ab And Cancer Res Technology Ltd Bis-pyridazine compounds and their use in treating cancer
US10040789B2 (en) 2015-11-30 2018-08-07 Astrazeneca Ab 1,3,4-thiadiazole 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
TW201730188A (zh) 2015-11-30 2017-09-01 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
RU2018124266A (ru) 2015-12-22 2020-01-23 Боард Оф Реджентс, Де Юниверсити Оф Техас Систем Солевые формы и полиморфы (R)-1-(4-(6-(2-(4-(3,3-дифторциклобутокси)-6-метилпиридин-2-ил)ацетамидо)пиридазин-3-ил)-2- фторбутил) -N-метил-1Н-1,2,3-триазол-4-карбоксамид
MX2019002108A (es) 2016-08-25 2019-07-08 Calithera Biosciences Inc Terapia de combinacion con inhibidores de glutaminasa.
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
WO2018145109A1 (en) 2017-02-06 2018-08-09 Massachusetts Institute Of Technology Methods and products related to glutaminase inhibitors
CN107137401A (zh) * 2017-03-28 2017-09-08 刘纪君 一种治疗产后抑郁症的药物组合物
CN106860460B (zh) * 2017-03-29 2019-04-23 上海市第一人民医院 谷氨酰胺酶抑制剂cb-839在制备治疗雌激素敏感型子宫内膜癌的药物中的应用
CN110741003B (zh) * 2017-06-13 2021-07-23 南京明德新药研发有限公司 作为gls1抑制剂的化合物
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
KR102379226B1 (ko) * 2018-10-16 2022-03-25 메드샤인 디스커버리 아이엔씨. 티아디아졸 유도체 및 이의 gls1억제제로서의 용도
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
KR102649592B1 (ko) * 2021-08-18 2024-03-20 한국화학연구원 신규한 마크로사이클 화합물, 이의 제조방법, 이를 유효성분으로 포함하는 암 또는 자가면역질환의 예방 또는 치료용 약학적 조성물
CN116023375A (zh) * 2021-10-25 2023-04-28 成都苑东生物制药股份有限公司 一种杂环类衍生物、其制备方法及用途

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4172896A (en) 1978-06-05 1979-10-30 Dainippon Pharmaceutical Co., Ltd. Methane-sulfonamide derivatives, the preparation thereof and composition comprising the same
GB9217295D0 (en) 1992-08-14 1992-09-30 Wellcome Found Controlled released tablets
US5358970A (en) 1993-08-12 1994-10-25 Burroughs Wellcome Co. Pharmaceutical composition containing bupropion hydrochloride and a stabilizer
US5541231A (en) 1993-07-30 1996-07-30 Glaxo Wellcome Inc. Stabilized Pharmaceutical
GB9315856D0 (en) 1993-07-30 1993-09-15 Wellcome Found Stabilized pharmaceutical
DK1348427T3 (da) 1997-07-29 2008-06-30 Alcon Lab Inc Oftalmiske sammensætninger indeholdende galactomannanpolymerer og borater
US6310093B1 (en) 1997-08-29 2001-10-30 Elan Pharmaceuticals, Inc. Method of preventing neuronal death
EP1051167A1 (en) 1998-01-29 2000-11-15 Sepracor, Inc. Pharmaceutical uses of optically pure (-) -bupropion
US8889112B2 (en) 1999-09-16 2014-11-18 Ocularis Pharma, Llc Ophthalmic formulations including selective alpha 1 antagonists
US6451828B1 (en) * 2000-08-10 2002-09-17 Elan Pharmaceuticals, Inc. Selective inhibition of glutaminase by bis-thiadiazoles
US6933289B2 (en) 2003-07-01 2005-08-23 Allergan, Inc. Inhibition of irritating side effects associated with use of a topical ophthalmic medication
ATE444732T1 (de) 2003-08-07 2009-10-15 Allergan Inc Zusammensetzungen zur abgabe von therapeutika in die augen und verfahren zu ihrer herstellung und verwendung
US20050059744A1 (en) 2003-09-12 2005-03-17 Allergan, Inc. Methods and compositions for the treatment of pain and other alpha 2 adrenergic-mediated conditions
US7928140B2 (en) * 2007-08-02 2011-04-19 Amgen Inc. Benzothiazole PI3 kinase modulators for cancer treatment
WO2009118174A1 (de) 2008-03-27 2009-10-01 Grünenthal GmbH Substituierte cyclohexyldiamine
WO2011143160A2 (en) * 2010-05-10 2011-11-17 The Johns Hopkins University Metabolic inhibitor against tumors having an idh mutation
US10064885B2 (en) * 2010-07-09 2018-09-04 Massachusetts Institute Of Technology Metabolic gene, enzyme, and flux targets for cancer therapy

Also Published As

Publication number Publication date
PT2782570T (pt) 2019-12-17
EA026656B1 (ru) 2017-05-31
CA2856386C (en) 2022-05-31
JP2016210810A (ja) 2016-12-15
JP2014533699A (ja) 2014-12-15
EP2782570A1 (en) 2014-10-01
IL259958B (en) 2021-06-30
DK2782570T3 (da) 2019-12-09
PL2782570T3 (pl) 2020-04-30
JP6577623B2 (ja) 2019-09-18
BR112014012129A8 (pt) 2017-06-20
RS59705B1 (sr) 2020-01-31
MX362550B (es) 2019-01-24
SMT201900738T1 (it) 2020-01-14
SG11201402305WA (en) 2014-06-27
WO2013078123A1 (en) 2013-05-30
MX2014005928A (es) 2014-08-27
AR090398A1 (es) 2014-11-12
CN104220070B (zh) 2020-01-21
CN104220070A (zh) 2014-12-17
JP6031527B2 (ja) 2016-11-24
EP2782570B1 (en) 2019-09-18
CN108785305A (zh) 2018-11-13
IL259958A (en) 2018-07-31
NZ625913A (en) 2015-12-24
JP2018111729A (ja) 2018-07-19
CN108785305B (zh) 2021-10-29
IL232665A0 (en) 2014-07-31
LT2782570T (lt) 2020-01-10
EP3620162A1 (en) 2020-03-11
AU2012340866B2 (en) 2017-03-16
ES2761866T3 (es) 2020-05-21
HK1204768A1 (en) 2015-12-04
CY1122707T1 (el) 2021-03-12
ZA201404518B (en) 2017-04-26
HRP20192144T1 (hr) 2020-02-21
ZA201601655B (en) 2017-06-28
TW201329071A (zh) 2013-07-16
SI2782570T1 (sl) 2020-02-28
AU2012340866A1 (en) 2014-06-26
HUE047642T2 (hu) 2020-05-28
TWI585084B (zh) 2017-06-01
KR20150000866A (ko) 2015-01-05
KR102042290B1 (ko) 2019-11-07
BR112014012129A2 (pt) 2017-06-13
EP2782570A4 (en) 2015-05-27
CA2856386A1 (en) 2013-05-30
JP6329226B2 (ja) 2018-05-23
KR20190127971A (ko) 2019-11-13
SG10201607685SA (en) 2016-11-29
EA201491012A1 (ru) 2014-12-30

Similar Documents

Publication Publication Date Title
EA201692166A1 (ru) Гетероциклические ингибиторы глютаминазы
EA201400412A1 (ru) ЗАМЕЩЕННЫЕ БЕНЗИЛИНДАЗОЛЫ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Bub1 КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ ГИПЕРПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ
EA201290980A1 (ru) Производные 1-амино-2-циклопропилэтилбороновой кислоты
EA201591753A1 (ru) 3-пиримидин-4-илоксазолидин-2-оны в качестве ингибиторов мутантного idh
EA201591745A1 (ru) 3-пиримидин-4-ил-оксазолидин-2-оны в качестве ингибиторов мутантого idh
EA201291143A1 (ru) Пиразолилхиназолиновые ингибиторы киназы
EA201101650A1 (ru) Новые производные пиримидина и их применение в лечении злокачественных новообразований и последующих заболеваний
EA201491824A1 (ru) Производные бензамида для ингибирования активности abl1, abl2 и bcr-abl1
EA201591591A1 (ru) Соединения карбазола, применяемые в качестве ингибиторов бромодомена
EA201391106A1 (ru) Новые гетероциклические производные
EA201400333A1 (ru) Бензонитрильные производные в качестве ингибиторов киназ
JO3438B1 (ar) مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
EA201490888A1 (ru) Новые производные пурина и их применение для лечения заболевания
EA201491579A1 (ru) Соединения оксазолидин-2-она и их применения в качестве ингибиторов pi3k
EA201891553A1 (ru) Ингибиторы syk
EA201690316A1 (ru) Соединения для применения в качестве иммуномодуляторов
EA201391682A1 (ru) Замещенные производные индазола, активные в качестве ингибиторов киназы
EA201590281A1 (ru) Новые гетероарильные и гетероциклические соединения, их композиции и способы
EA201492216A1 (ru) Ингибиторы бромодомена и их применение
EA201391290A1 (ru) Гетероциклические модуляторы синтеза липидов
EA201400735A1 (ru) Производные альфа-амино бороновой кислоты, селективные ингибиторы иммунопротеасомы
EA201391285A1 (ru) Производные тетрагидрохинолина, полезные в качестве ингибиторов бромодомена
EA201490696A1 (ru) 3-пиримидин-4-ил-оксазолидин-2-оны в качестве ингибиторов мутантной idh
EA201301019A1 (ru) Бензодиоксановые ингибиторы продуцирования лейкотриена
IN2014KN02601A (ru)