JP2016500082A5 - - Google Patents
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- Publication number
- JP2016500082A5 JP2016500082A5 JP2015543242A JP2015543242A JP2016500082A5 JP 2016500082 A5 JP2016500082 A5 JP 2016500082A5 JP 2015543242 A JP2015543242 A JP 2015543242A JP 2015543242 A JP2015543242 A JP 2015543242A JP 2016500082 A5 JP2016500082 A5 JP 2016500082A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- alkyl
- formula
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims description 82
- 125000000217 alkyl group Chemical group 0.000 claims description 30
- 150000003839 salts Chemical class 0.000 claims description 29
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 239000001257 hydrogen Substances 0.000 claims description 10
- 125000000623 heterocyclic group Chemical group 0.000 claims description 9
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 8
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 7
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 5
- 102000000905 Cadherin Human genes 0.000 claims description 4
- 108050007957 Cadherin Proteins 0.000 claims description 4
- 108010053763 Pyruvate Carboxylase Proteins 0.000 claims description 4
- 102100039895 Pyruvate carboxylase, mitochondrial Human genes 0.000 claims description 4
- 102000013127 Vimentin Human genes 0.000 claims description 4
- 108010065472 Vimentin Proteins 0.000 claims description 4
- 125000001188 haloalkyl group Chemical group 0.000 claims description 4
- 125000005843 halogen group Chemical group 0.000 claims description 4
- 150000002431 hydrogen Chemical class 0.000 claims description 4
- 125000005309 thioalkoxy group Chemical group 0.000 claims description 4
- 210000005048 vimentin Anatomy 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 125000004043 oxo group Chemical group O=* 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000012830 cancer therapeutic Substances 0.000 claims 5
- 229940124597 therapeutic agent Drugs 0.000 claims 5
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010024612 Lipoma Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2012/085023 | 2012-11-22 | ||
| 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 |
| CNPCT/CN2013/000294 | 2013-03-15 | ||
| PCT/CN2013/001428 WO2014079150A1 (en) | 2012-11-22 | 2013-11-21 | Compounds and their methods of use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018082754A Division JP2018150316A (ja) | 2012-11-22 | 2018-04-24 | 化合物およびその使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016500082A JP2016500082A (ja) | 2016-01-07 |
| JP2016500082A5 true JP2016500082A5 (enExample) | 2016-12-28 |
| JP6333277B2 JP6333277B2 (ja) | 2018-05-30 |
Family
ID=50775393
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015543242A Expired - Fee Related JP6333277B2 (ja) | 2012-11-22 | 2013-11-21 | 化合物およびその使用方法 |
| JP2018082754A Pending JP2018150316A (ja) | 2012-11-22 | 2018-04-24 | 化合物およびその使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018082754A Pending JP2018150316A (ja) | 2012-11-22 | 2018-04-24 | 化合物およびその使用方法 |
Country Status (36)
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8604016B2 (en) | 2011-11-21 | 2013-12-10 | Calithera Biosciences Inc. | Heterocyclic inhibitors of glutaminase |
| WO2014078645A1 (en) | 2012-11-16 | 2014-05-22 | Calithera Biosciences, Inc. | Heterocyclic glutaminase inhibitors |
| MX369691B (es) | 2012-11-21 | 2019-11-19 | Agios Pharmaceuticals Inc | Inhibidores de glutaminasa y métodos de empleo. |
| WO2014079011A1 (en) | 2012-11-22 | 2014-05-30 | Agios Pharmaceuticals, Inc. | Heterocyclic compounds for inhibiting glutaminase and their methods of use |
| CA2892817A1 (en) * | 2012-12-03 | 2014-06-12 | Calithera Biosciences Inc. | Treatment of cancer with heterocyclic inhibitors of glutaminase |
| EP2943485B1 (en) | 2013-01-14 | 2017-09-20 | Incyte Holdings Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
| HUE050215T2 (hu) | 2013-01-15 | 2020-11-30 | Incyte Holdings Corp | Pim kináz inhibitorokként hasznos tiazolkarboxamid és piridinkarboxamid vegyületek |
| TW201605866A (zh) | 2013-08-23 | 2016-02-16 | 英塞特公司 | 可用作ｐｉｍ激酶抑制劑之呋喃并－及噻吩并－吡啶甲醯胺化合物 |
| CN105960405B (zh) * | 2014-01-06 | 2021-02-19 | 理森制药股份公司 | 谷氨酰胺酶抑制剂 |
| WO2015143340A1 (en) | 2014-03-21 | 2015-09-24 | Agios Pharmaceuticals, Inc. | Compounds and their methods of use |
| US20170050958A1 (en) * | 2014-04-30 | 2017-02-23 | Pfizer Inc. | Cycloalkyl-Linked Diheterocycle Derivatives |
| GB201409624D0 (en) | 2014-05-30 | 2014-07-16 | Astrazeneca Ab | 1,3,4-thiadiazole compounds and their use in treating cancer |
| US9809588B2 (en) | 2014-07-03 | 2017-11-07 | Board Of Regents, The University Of Texas System | GLS1 inhibitors for treating disease |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| 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 |
| KR20170082494A (ko) | 2014-08-07 | 2017-07-14 | 칼리테라 바이오사이언시즈, 인코포레이티드 | 결정 형태의 글루타미나아제 억제제 |
| WO2016054388A1 (en) * | 2014-10-03 | 2016-04-07 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Glutaminase inhibitors |
| AU2016246521B2 (en) | 2015-04-06 | 2020-07-09 | Calithera Biosciences, Inc. | Treatment of lung cancer with inhibitors of glutaminase |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| CN107921044B (zh) * | 2015-06-30 | 2022-01-21 | 德州大学系统董事会 | 用于治疗疾病的gls1抑制剂 |
| TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Ｐｉｍ激酶抑制劑之鹽 |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase 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 |
| 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 |
| MX384732B (es) | 2015-12-22 | 2025-03-14 | Univ Texas | Formas de sales y polimorfos de (r)-1-(4-(6-(2-(4-(3,3-difluorociclobutoxi)-6-metilpiridin-2-il)acetamido)piridazin-3-il)-2-fluorobutil)-n-metil-1h-1,2,3-triazol-4-carboxamida. |
| KR20190040302A (ko) * | 2016-08-25 | 2019-04-17 | 칼리테라 바이오사이언시즈, 인코포레이티드 | 글루타미나제 억제제와의 병용 요법 |
| JP2019524852A (ja) | 2016-08-25 | 2019-09-05 | 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用いる併用療法 |
| 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 |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| JP7768505B2 (ja) | 2018-06-01 | 2025-11-12 | コーネル・ユニバーシティー | Ｐｉ３ｋに関連する疾患または障害に対する併用療法 |
| 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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| DE2037257A1 (en) | 1970-07-28 | 1972-02-03 | Farbwerke Hoechst AG, vorm. Meister Lucius & Brüning, 6000 Frankfurt | Poly-(5-amino-1,3,4-thiadiazol-2-yl) derivs prepn - intermediates for drug and polymer prodn |
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| EP2399129B1 (en) | 2009-02-20 | 2015-11-25 | Michael P. Lisanti | A method of diagnosis or prognosis of a neoplasm comprising determining the level of expression of a protein in stromal cells adjacent to the neoplasm |
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| CN102827073A (zh) | 2011-06-17 | 2012-12-19 | 安吉奥斯医药品有限公司 | 治疗活性组合物和它们的使用方法 |
| AU2012340866B2 (en) * | 2011-11-21 | 2017-03-16 | Calithera Biosciences Inc. | Heterocyclic inhibitors of glutaminase |
| CN104519899A (zh) | 2012-03-15 | 2015-04-15 | 纽约州立大学研究基金会 | 包含e-钙粘蛋白的细胞外结构域的抑制剂的组合疗法 |
| MX369691B (es) | 2012-11-21 | 2019-11-19 | Agios Pharmaceuticals Inc | Inhibidores de glutaminasa y métodos de empleo. |
| US9029531B2 (en) | 2012-11-22 | 2015-05-12 | Agios Pharmaceuticals, Inc. | Compounds and their methods of use |
| WO2014079011A1 (en) | 2012-11-22 | 2014-05-30 | Agios Pharmaceuticals, Inc. | Heterocyclic compounds for inhibiting glutaminase and their methods of use |
| US20160008380A1 (en) | 2013-03-06 | 2016-01-14 | The Johns Hopkins University | Targeting glutamine metabolism in brain tumors |
| CN105960405B (zh) | 2014-01-06 | 2021-02-19 | 理森制药股份公司 | 谷氨酰胺酶抑制剂 |
| WO2015143340A1 (en) | 2014-03-21 | 2015-09-24 | Agios Pharmaceuticals, Inc. | Compounds and their methods of use |
-
2012
- 2012-11-22 WO PCT/CN2012/085023 patent/WO2014079011A1/en not_active Ceased
-
2013
- 2013-03-15 WO PCT/CN2013/000294 patent/WO2014079136A1/en not_active Ceased
- 2013-11-21 HR HRP20181628TT patent/HRP20181628T1/hr unknown
- 2013-11-21 LT LTEP13857585.7T patent/LT2922850T/lt unknown
- 2013-11-21 EA EA201890754A patent/EA201890754A1/ru unknown
- 2013-11-21 PT PT13857585T patent/PT2922850T/pt unknown
- 2013-11-21 UA UAA201506066A patent/UA117360C2/uk unknown
- 2013-11-21 PE PE2015000674A patent/PE20151072A1/es unknown
- 2013-11-21 CN CN201810824418.2A patent/CN108727307A/zh active Pending
- 2013-11-21 PL PL13857585T patent/PL2922850T3/pl unknown
- 2013-11-21 ES ES13857585.7T patent/ES2690390T3/es active Active
- 2013-11-21 EP EP13857585.7A patent/EP2922850B1/en active Active
- 2013-11-21 SM SM20180504T patent/SMT201800504T1/it unknown
- 2013-11-21 NZ NZ708382A patent/NZ708382A/en unknown
- 2013-11-21 EP EP18183580.2A patent/EP3456719A1/en not_active Withdrawn
- 2013-11-21 MY MYPI2015001355A patent/MY177344A/en unknown
- 2013-11-21 HU HUE13857585A patent/HUE040111T2/hu unknown
- 2013-11-21 DK DK13857585.7T patent/DK2922850T3/en active
- 2013-11-21 SG SG10201609940RA patent/SG10201609940RA/en unknown
- 2013-11-21 KR KR1020157016414A patent/KR20150085079A/ko not_active Ceased
- 2013-11-21 SI SI201331140T patent/SI2922850T1/sl unknown
- 2013-11-21 SG SG11201504049VA patent/SG11201504049VA/en unknown
- 2013-11-21 CN CN201380070365.5A patent/CN104936954B/zh not_active Expired - Fee Related
- 2013-11-21 RS RS20181133A patent/RS57859B1/sr unknown
- 2013-11-21 MX MX2015006493A patent/MX367389B/es active IP Right Grant
- 2013-11-21 JP JP2015543242A patent/JP6333277B2/ja not_active Expired - Fee Related
- 2013-11-21 BR BR112015011830A patent/BR112015011830A2/pt not_active Application Discontinuation
- 2013-11-21 TR TR2018/12360T patent/TR201812360T4/tr unknown
- 2013-11-21 WO PCT/CN2013/001428 patent/WO2014079150A1/en not_active Ceased
- 2013-11-21 CA CA2893510A patent/CA2893510C/en active Active
- 2013-11-21 AU AU2013347771A patent/AU2013347771B2/en not_active Ceased
- 2013-11-21 US US14/646,634 patent/US10087172B2/en active Active
- 2013-11-21 EA EA201590987A patent/EA030646B1/ru not_active IP Right Cessation
- 2013-11-22 AR ARP130104322A patent/AR093598A1/es unknown
- 2013-11-22 TW TW102142566A patent/TWI629268B/zh not_active IP Right Cessation
- 2013-11-22 TW TW107111990A patent/TW201906825A/zh unknown
-
2015
- 2015-05-21 IL IL238958A patent/IL238958B/en not_active IP Right Cessation
- 2015-05-22 SA SA515360469A patent/SA515360469B1/ar unknown
- 2015-05-22 PH PH12015501150A patent/PH12015501150B1/en unknown
- 2015-05-22 CL CL2015001392A patent/CL2015001392A1/es unknown
- 2015-06-15 CR CR20150316A patent/CR20150316A/es unknown
- 2015-06-22 EC ECIEPI201526557A patent/ECSP15026557A/es unknown
-
2017
- 2017-11-24 PH PH12017502141A patent/PH12017502141A1/en unknown
-
2018
- 2018-04-24 JP JP2018082754A patent/JP2018150316A/ja active Pending
- 2018-04-30 AU AU2018202954A patent/AU2018202954A1/en not_active Abandoned
- 2018-08-17 CY CY20181100864T patent/CY1120581T1/el unknown
- 2018-08-21 US US16/107,220 patent/US10689375B2/en not_active Expired - Fee Related
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