JP2017509703A5 - - Google Patents
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- Publication number
- JP2017509703A5 JP2017509703A5 JP2017501134A JP2017501134A JP2017509703A5 JP 2017509703 A5 JP2017509703 A5 JP 2017509703A5 JP 2017501134 A JP2017501134 A JP 2017501134A JP 2017501134 A JP2017501134 A JP 2017501134A JP 2017509703 A5 JP2017509703 A5 JP 2017509703A5
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims description 63
- 125000000217 alkyl group Chemical group 0.000 claims description 30
- 150000003839 salts Chemical class 0.000 claims description 24
- 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
- 239000000203 mixture Substances 0.000 claims description 10
- 206010028980 Neoplasm Diseases 0.000 claims description 9
- 125000000623 heterocyclic group Chemical group 0.000 claims description 9
- 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
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- 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
- 102000009127 Glutaminase Human genes 0.000 claims description 5
- 108010073324 Glutaminase Proteins 0.000 claims description 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 4
- 125000000753 cycloalkyl 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
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 102000000905 Cadherin Human genes 0.000 claims description 2
- 108050007957 Cadherin Proteins 0.000 claims description 2
- 108010053763 Pyruvate Carboxylase Proteins 0.000 claims description 2
- 102100039895 Pyruvate carboxylase, mitochondrial Human genes 0.000 claims description 2
- 102000013127 Vimentin Human genes 0.000 claims description 2
- 108010065472 Vimentin Proteins 0.000 claims description 2
- 230000007488 abnormal function Effects 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
- 230000000694 effects Effects 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
- 210000005048 vimentin Anatomy 0.000 claims description 2
- 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
- 206010058467 Lung neoplasm malignant 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
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 0 C(*CC1=CCC=NN1)C1NNCC=C1 Chemical compound C(*CC1=CCC=NN1)C1NNCC=C1 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 201000010099 disease Diseases 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2014073812 | 2014-03-21 | ||
| CNPCT/CN2014/073812 | 2014-03-21 | ||
| PCT/US2015/021781 WO2015143340A1 (en) | 2014-03-21 | 2015-03-20 | Compounds and their methods of use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019184947A Division JP2020019807A (ja) | 2014-03-21 | 2019-10-08 | 化合物及びそれらの使用の方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017509703A JP2017509703A (ja) | 2017-04-06 |
| JP2017509703A5 true JP2017509703A5 (https=) | 2018-04-05 |
| JP6602364B2 JP6602364B2 (ja) | 2019-11-06 |
Family
ID=54145391
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017501134A Expired - Fee Related JP6602364B2 (ja) | 2014-03-21 | 2015-03-20 | 化合物及びそれらの使用の方法 |
| JP2019184947A Withdrawn JP2020019807A (ja) | 2014-03-21 | 2019-10-08 | 化合物及びそれらの使用の方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019184947A Withdrawn JP2020019807A (ja) | 2014-03-21 | 2019-10-08 | 化合物及びそれらの使用の方法 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US10000479B2 (https=) |
| EP (1) | EP3119199B1 (https=) |
| JP (2) | JP6602364B2 (https=) |
| KR (1) | KR20160127149A (https=) |
| CN (1) | CN106231900B (https=) |
| AU (1) | AU2015231053B2 (https=) |
| BR (1) | BR112016021620A2 (https=) |
| CA (1) | CA2943339A1 (https=) |
| EA (1) | EA201691896A1 (https=) |
| IL (1) | IL247921A0 (https=) |
| MX (1) | MX2016012244A (https=) |
| PH (1) | PH12016501838A1 (https=) |
| WO (1) | WO2015143340A1 (https=) |
| ZA (1) | ZA201606450B (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CR20160497A (es) | 2014-04-30 | 2016-12-20 | Pfizer | Derivados de diheterociclo enlazado a cicloalquilo |
| 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 |
| 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 (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US4070400A (en) | 1975-10-16 | 1978-01-24 | Merck & Co., Inc. | Diphenyl polyamides having a cyclohexylene moiety |
| US4376110A (en) | 1980-08-04 | 1983-03-08 | Hybritech, Incorporated | Immunometric assays using monoclonal antibodies |
| US4366241A (en) | 1980-08-07 | 1982-12-28 | Syva Company | Concentrating zone method in heterogeneous immunoassays |
| US4517288A (en) | 1981-01-23 | 1985-05-14 | American Hospital Supply Corp. | Solid phase system for ligand assay |
| CA1291031C (en) | 1985-12-23 | 1991-10-22 | Nikolaas C.J. De Jaeger | Method for the detection of specific binding agents and their correspondingbindable substances |
| US4843155A (en) | 1987-11-19 | 1989-06-27 | Piotr Chomczynski | Product and process for isolating RNA |
| WO1994022842A1 (en) | 1993-03-29 | 1994-10-13 | Basf Aktiengesellschaft | 1-amino-3-phenoxy propane derivatives as modulators of multi-drug resistance |
| US5895748A (en) | 1996-11-27 | 1999-04-20 | Johnson; Keith R. | Panel of antibodies for detecting cadherins and catenins in tissues and method of using the panel of antibodies |
| EP1087951B9 (en) | 1998-06-18 | 2006-09-13 | Bristol-Myers Squibb Company | Carbon substituted aminothiazole inhibitors of cyclin dependent kinases |
| WO2000052204A2 (en) | 1999-02-22 | 2000-09-08 | Orntoft Torben F | Gene expression in bladder tumors |
| WO2001062206A2 (en) | 2000-02-22 | 2001-08-30 | Mount Sinai School Of Medicine Of New York University | N-cadherin modulated migration, invasion, and metastasis |
| US6974667B2 (en) | 2000-06-14 | 2005-12-13 | Gene Logic, Inc. | Gene expression profiles in liver cancer |
| US6451828B1 (en) * | 2000-08-10 | 2002-09-17 | Elan Pharmaceuticals, Inc. | Selective inhibition of glutaminase by bis-thiadiazoles |
| DE60200248T2 (de) | 2002-08-01 | 2005-01-27 | Mtm Laboratories Ag | Verfahren für Lösung-basierte Diagnose |
| WO2006040569A1 (en) * | 2004-10-14 | 2006-04-20 | Astex Therapeutics Limited | Thiophene amide compounds for use in the treatment or prophylaxis of cancers |
| US20080182865A1 (en) | 2005-03-11 | 2008-07-31 | Witta Samir E | Histone deacetylase inhibitors sensitize cancer cells to epidermal growth factor inhibitors |
| CA2601157A1 (en) | 2005-03-16 | 2006-09-28 | Osi Pharmaceuticals, Inc. | Biological markers predictive of anti-cancer response to epidermal growth factor receptor kinase inhibitors |
| US8716472B2 (en) * | 2006-10-16 | 2014-05-06 | University Of Rochester | Tripodal cyclohexane derivatives and their use as carbohydrate receptors |
| AU2008326497B2 (en) | 2007-11-19 | 2014-02-13 | Genentech, Inc. | Compositions and methods for inhibiting tumor progression |
| EP2271941B1 (en) | 2008-03-07 | 2012-08-08 | OSI Pharmaceuticals, Inc. | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
| WO2010096574A1 (en) | 2009-02-20 | 2010-08-26 | Lisanti Michael P | 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 |
| US10532034B2 (en) | 2009-03-25 | 2020-01-14 | Cornell University | Inhibition of glutaminase C |
| EP2419177A1 (en) | 2009-04-17 | 2012-02-22 | OSI Pharmaceuticals, LLC | Biological markers predictive of anti-cancer response to epidermal growth factor receptor kinase inhibitors |
| WO2011143160A2 (en) | 2010-05-10 | 2011-11-17 | The Johns Hopkins University | Metabolic inhibitor against tumors having an idh mutation |
| EP3955004B1 (en) | 2010-06-23 | 2024-05-29 | University of Louisville Research Foundation, Inc. | Use of fatty acids in methods for detecting cancer |
| US10064885B2 (en) | 2010-07-09 | 2018-09-04 | Massachusetts Institute Of Technology | Metabolic gene, enzyme, and flux targets for cancer therapy |
| UY33930A (es) | 2011-03-04 | 2012-10-31 | Novartis Ag | Inhibidores novedosos de quinasas |
| 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 |
| HRP20192144T1 (hr) * | 2011-11-21 | 2020-02-21 | Calithera Biosciences Inc. | Heterociklični inhibitori glutaminaze |
| EP2844270A4 (en) | 2012-03-15 | 2016-01-27 | Univ New York State Res Found | COMBINATION THERAPIES WITH INHIBITORS OF THE EXTRACELLULAR DOMAIN OF E-CADHERINE |
| 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 |
| US20160008380A1 (en) | 2013-03-06 | 2016-01-14 | The Johns Hopkins University | Targeting glutamine metabolism in brain tumors |
| KR20160100408A (ko) * | 2014-01-06 | 2016-08-23 | 리젠 파마슈티컬스 소시에떼 아노님 | 신규한 글루타미나제 저해제 |
-
2015
- 2015-03-20 BR BR112016021620A patent/BR112016021620A2/pt not_active Application Discontinuation
- 2015-03-20 CA CA2943339A patent/CA2943339A1/en not_active Abandoned
- 2015-03-20 AU AU2015231053A patent/AU2015231053B2/en not_active Ceased
- 2015-03-20 KR KR1020167029269A patent/KR20160127149A/ko not_active Withdrawn
- 2015-03-20 EA EA201691896A patent/EA201691896A1/ru unknown
- 2015-03-20 JP JP2017501134A patent/JP6602364B2/ja not_active Expired - Fee Related
- 2015-03-20 US US15/127,742 patent/US10000479B2/en active Active
- 2015-03-20 EP EP15764391.7A patent/EP3119199B1/en active Active
- 2015-03-20 MX MX2016012244A patent/MX2016012244A/es unknown
- 2015-03-20 CN CN201580020934.4A patent/CN106231900B/zh not_active Expired - Fee Related
- 2015-03-20 WO PCT/US2015/021781 patent/WO2015143340A1/en not_active Ceased
-
2016
- 2016-09-19 ZA ZA2016/06450A patent/ZA201606450B/en unknown
- 2016-09-19 IL IL247921A patent/IL247921A0/en unknown
- 2016-09-20 PH PH12016501838A patent/PH12016501838A1/en unknown
-
2019
- 2019-10-08 JP JP2019184947A patent/JP2020019807A/ja not_active Withdrawn
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