CA2981762A1 - Treatment of lung cancer with inhibitors of glutaminase - Google Patents
Treatment of lung cancer with inhibitors of glutaminase Download PDFInfo
- Publication number
- CA2981762A1 CA2981762A1 CA2981762A CA2981762A CA2981762A1 CA 2981762 A1 CA2981762 A1 CA 2981762A1 CA 2981762 A CA2981762 A CA 2981762A CA 2981762 A CA2981762 A CA 2981762A CA 2981762 A1 CA2981762 A1 CA 2981762A1
- Authority
- CA
- Canada
- Prior art keywords
- substituted
- arylalkyl
- unsubstituted
- heteroaryl
- alkyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Abandoned
Links
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- 206010058467 Lung neoplasm malignant Diseases 0.000 title claims abstract description 49
- 201000005202 lung cancer Diseases 0.000 title claims abstract description 49
- 238000011282 treatment Methods 0.000 title claims description 38
- 239000003112 inhibitor Substances 0.000 title abstract description 28
- 102000009127 Glutaminase Human genes 0.000 title abstract description 21
- 108010073324 Glutaminase Proteins 0.000 title abstract description 21
- 238000000034 method Methods 0.000 claims abstract description 128
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- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims abstract 11
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- VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 VJJPUSNTGOMMGY-MRVIYFEKSA-N 0.000 claims description 37
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- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 13
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- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 12
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- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims description 6
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- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 5
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- 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
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
- C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
- C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
- C12Q1/6886—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
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- C12Q2600/00—Oligonucleotides characterized by their use
- C12Q2600/106—Pharmacogenomics, i.e. genetic variability in individual responses to drugs and drug metabolism
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- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q2600/00—Oligonucleotides characterized by their use
- C12Q2600/156—Polymorphic or mutational markers
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q2600/00—Oligonucleotides characterized by their use
- C12Q2600/158—Expression markers
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- Medicinal Chemistry (AREA)
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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
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| US201562143494P | 2015-04-06 | 2015-04-06 | |
| US62/143,494 | 2015-04-06 | ||
| US201562149489P | 2015-04-17 | 2015-04-17 | |
| US62/149,489 | 2015-04-17 | ||
| PCT/US2016/026127 WO2016164401A1 (en) | 2015-04-06 | 2016-04-06 | Treatment of lung cancer with inhibitors of glutaminase |
Publications (1)
| Publication Number | Publication Date |
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| CA2981762A1 true CA2981762A1 (en) | 2016-10-13 |
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| CA2981762A Abandoned CA2981762A1 (en) | 2015-04-06 | 2016-04-06 | Treatment of lung cancer with inhibitors of glutaminase |
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| EP (1) | EP3280415A4 (enExample) |
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| US8604016B2 (en) | 2011-11-21 | 2013-12-10 | Calithera Biosciences Inc. | Heterocyclic inhibitors of glutaminase |
| EP3954686A1 (en) | 2012-11-16 | 2022-02-16 | Calithera Biosciences, Inc. | Heterocyclic glutaminase inhibitors |
| EA033919B1 (ru) | 2014-04-30 | 2019-12-10 | Пфайзер Инк. | Соединённые циклоалкилом дигетероциклические производные |
| CA2957225A1 (en) | 2014-08-07 | 2016-02-11 | Calithera Biosciences, Inc. | Crystal forms of glutaminase 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 |
| BR112019003533A2 (pt) | 2016-08-25 | 2019-05-21 | Calithera Biosciences Inc. | terapia de combinação com inibidores de glutaminase |
| WO2018039441A1 (en) | 2016-08-25 | 2018-03-01 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
| EP3592354A4 (en) * | 2017-03-10 | 2021-04-07 | Calithera Biosciences, Inc. | COMBINATION THERAPY WITH GLUTAMINASE INHIBITORS |
| JP7188936B2 (ja) * | 2018-08-21 | 2022-12-13 | 国立大学法人富山大学 | 抗炎症剤 |
| JP7156856B2 (ja) * | 2018-08-21 | 2022-10-19 | 国立大学法人富山大学 | 抗肥満剤 |
| US20250275964A1 (en) * | 2019-10-15 | 2025-09-04 | Cornell University | Methods of inhibiting liver-type glutaminase, gls2 |
| US20240082158A1 (en) * | 2020-05-21 | 2024-03-14 | University Of Pittsburgh-Of The Commonwealth System Of Higher Education | Compositions and methods for administering a yap1/wwrt1 inhibiting composition and a gls1 inhibiting composition |
| CN111514460B (zh) * | 2020-05-22 | 2021-12-14 | 西安交通大学 | 大气压冷等离子体在抑制谷氨酰胺酶活性方面的用途及酶抑制剂 |
| CN113956233B (zh) * | 2021-10-22 | 2023-06-06 | 南方医科大学 | 一种酰胺类化合物或其药学上可接受的盐及其制备方法和应用 |
| WO2023212718A2 (en) * | 2022-04-29 | 2023-11-02 | Cornell University | Methods of treating a virus infection and methods of inhibiting viral replication |
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| US1019519A (en) | 1911-07-11 | 1912-03-05 | Oscar Martin Polin | Apparatus for making backing for teeth. |
| US6451828B1 (en) | 2000-08-10 | 2002-09-17 | Elan Pharmaceuticals, Inc. | Selective inhibition of glutaminase by bis-thiadiazoles |
| AU2002305926A1 (en) | 2001-02-05 | 2002-10-08 | Exegenics Inc. | Cysteine protease inhibitors |
| ES2367311T3 (es) | 2004-04-15 | 2011-11-02 | University Of Florida Research Foundation, Inc. | Productos de degradación proteolítica de map-2 como biomarcadores de diagnóstico para las lesiones neurales. |
| CN101951930A (zh) | 2008-02-19 | 2011-01-19 | 阿奈斯特药品株式会社 | 对身体功能的恢复有用的口服或经肠组合物 |
| 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 |
| MX2013005434A (es) | 2010-11-18 | 2013-09-26 | Deuteria Pharmaceuticals Inc | 3´ - deutero - polidomida. |
| CN103030597B (zh) * | 2011-09-30 | 2014-10-01 | 南昌滨西科技有限公司 | 肾脏型谷氨酰胺酶抑制剂及其制备方法和用途 |
| EA026656B1 (ru) | 2011-11-21 | 2017-05-31 | Калитера Байосайенсиз Инк. | Гетероциклические ингибиторы глютаминазы |
| US8604016B2 (en) * | 2011-11-21 | 2013-12-10 | Calithera Biosciences Inc. | Heterocyclic inhibitors of glutaminase |
| EP2855698A4 (en) * | 2012-05-24 | 2016-03-30 | Dana Farber Cancer Inst Inc | OBTAINING TO THE GLUTAMINE-TO-PYRUVAT SIGNAL PATH FOR THE TREATMENT OF CANCER ASSOCIATED WITH THE KRAS ONKOGEN |
| US9694015B2 (en) | 2012-09-10 | 2017-07-04 | Celgene Corporation | Methods for the treatment of locally advanced breast cancer |
| WO2014043633A1 (en) | 2012-09-17 | 2014-03-20 | Agios Pharmaceuticals, Inc. | Use of e-cadherin and vimentin for selection of treatment responsive patients |
| EP3954686A1 (en) * | 2012-11-16 | 2022-02-16 | Calithera Biosciences, Inc. | Heterocyclic glutaminase inhibitors |
| HK1213889A1 (zh) | 2012-11-21 | 2016-07-15 | 安吉奥斯医药品有限公司 | 殼氨醯胺酶抑制劑及使用方法 |
| 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 |
| KR20150091389A (ko) | 2012-12-03 | 2015-08-10 | 칼리테라 바이오사이언시즈 인코포레이티드 | 글루타미나제의 헤테로사이클릭 억제제에 의한 암 치료 |
| WO2015061432A1 (en) | 2013-10-25 | 2015-04-30 | Calithera Biosciences, Inc. | Treatment of viral infections with inhibitors of glutaminase |
| US20150258082A1 (en) | 2014-03-14 | 2015-09-17 | Francesco Parlati | Combination therapy with glutaminase inhibitors |
| US10221459B2 (en) | 2014-05-13 | 2019-03-05 | Case Western Reserve University | Compositions and methods of treating cancer harboring PIKC3A mutations |
| BR112016029041A8 (pt) | 2014-06-13 | 2021-07-20 | Calithera Biosciences Inc | uso de um inibidor de glutaminase, composição farmacêutica e kit farmacêutico |
| WO2016004418A1 (en) | 2014-07-03 | 2016-01-07 | Board Of Regents, University Of Texas System | Glutaminase inhibitor therapy |
| WO2016014890A1 (en) | 2014-07-24 | 2016-01-28 | Calithera Biosciences, Inc. | Treatment of multiple myeloma with heterocyclic inhibitors of glutaminase |
| CA2957225A1 (en) | 2014-08-07 | 2016-02-11 | Calithera Biosciences, Inc. | Crystal forms of glutaminase inhibitors |
| WO2016054388A1 (en) | 2014-10-03 | 2016-04-07 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Glutaminase inhibitors |
| WO2016077632A2 (en) | 2014-11-13 | 2016-05-19 | Buck Institute For Research On Aging | Inhibition of proline catabolism for the treatment of cancer and other therapeutic applications |
| EP3277276B1 (en) * | 2015-03-30 | 2020-11-04 | Calithera Biosciences, Inc. | Methods of administering glutaminase inhibitors |
| WO2018039442A1 (en) | 2016-08-25 | 2018-03-01 | Calithera Biosciences, Inc. | Treatment of cancer with inhibitors of glutaminase |
| WO2018039441A1 (en) | 2016-08-25 | 2018-03-01 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
| BR112019003533A2 (pt) | 2016-08-25 | 2019-05-21 | Calithera Biosciences Inc. | terapia de combinação com inibidores de glutaminase |
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2016
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- 2016-04-06 BR BR112017021312A patent/BR112017021312A2/pt not_active IP Right Cessation
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Also Published As
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| CN107949387B (zh) | 2021-08-13 |
| CN107949387A (zh) | 2018-04-20 |
| JP2021102662A (ja) | 2021-07-15 |
| EA035354B1 (ru) | 2020-06-01 |
| EP3280415A4 (en) | 2018-12-26 |
| KR20170132333A (ko) | 2017-12-01 |
| IL254876A0 (en) | 2017-12-31 |
| WO2016164401A8 (en) | 2017-11-23 |
| HK1254349A1 (zh) | 2019-07-19 |
| BR112017021312A2 (pt) | 2018-06-26 |
| AU2016246521B2 (en) | 2020-07-09 |
| EP3280415A1 (en) | 2018-02-14 |
| US10441587B2 (en) | 2019-10-15 |
| JP6944377B2 (ja) | 2021-10-06 |
| JP2018510884A (ja) | 2018-04-19 |
| EA201792227A1 (ru) | 2018-11-30 |
| WO2016164401A1 (en) | 2016-10-13 |
| AU2016246521A8 (en) | 2019-08-15 |
| AU2016246521A1 (en) | 2017-11-02 |
| MX2017012824A (es) | 2018-05-15 |
| SG11201708153XA (en) | 2017-11-29 |
| US20160287585A1 (en) | 2016-10-06 |
| MX383034B (es) | 2025-03-13 |
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