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 |
| CNPCT/CN2013/000294 | 2013-03-15 | ||
| 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 |
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 (OSRAM) | 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 |
| JP6275153B2 (ja) | 2012-11-16 | 2018-02-07 | 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 | ヘテロ環式グルタミナーゼ阻害剤 |
| 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 |
| JP6437452B2 (ja) | 2013-01-14 | 2018-12-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物 |
| LT2945939T (lt) | 2013-01-15 | 2020-07-27 | Incyte Holdings Corporation | Triazolkarboksamidai ir piridinkarboksamido junginiai, naudotini kaip pim kinazės inhibitoriai |
| EP3036238A1 (en) | 2013-08-23 | 2016-06-29 | Incyte Corporation | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
| EP3092235A2 (en) | 2014-01-06 | 2016-11-16 | Rhizen Pharmaceuticals S.A. | Novel inhibitors of glutaminase |
| MX2016012244A (es) * | 2014-03-21 | 2017-05-08 | Agios Pharmaceuticals Inc | Compuestos y sus metodos de uso. |
| MX2016014143A (es) * | 2014-04-30 | 2017-02-15 | 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 |
| 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 |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic 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 |
| EA037738B1 (ru) | 2014-08-07 | 2021-05-17 | Калитера Байосайенсиз, Инк. | Кристаллические формы ингибиторов глутаминазы |
| WO2016054388A1 (en) * | 2014-10-03 | 2016-04-07 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Glutaminase inhibitors |
| US10441587B2 (en) | 2015-04-06 | 2019-10-15 | 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 |
| 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 |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| WO2017062354A1 (en) | 2015-10-05 | 2017-04-13 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors and immuno-oncology agents |
| US10040789B2 (en) * | 2015-11-30 | 2018-08-07 | Astrazeneca Ab | 1,3,4-thiadiazole compounds and their use in treating cancer |
| CN109503570B (zh) * | 2015-12-18 | 2020-08-25 | 诺言医药科技(上海)有限公司 | 一种含有索拉非尼的药物组合物及其应用 |
| US10150753B2 (en) | 2015-12-22 | 2018-12-11 | Board Of Regents, The University Of Texas System | Salt forms and polymorphs of (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyrdin-2-yl)acetamido) pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide |
| 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 |
| WO2018039544A1 (en) * | 2016-08-25 | 2018-03-01 | Calithera Biosciences, Inc. | Combination therapy with glutaminase inhibitors |
| 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 |
| TW201924683A (zh) | 2017-12-08 | 2019-07-01 | 美商英塞特公司 | 用於治療骨髓增生性贅瘤的低劑量組合療法 |
| EP3801069A4 (en) | 2018-06-01 | 2022-03-16 | Cornell University | MULTIPLE THERAPY FOR DISEASE OR DISORDER ASSOCIATED WITH PI3K |
| 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 |
| US20220400732A1 (en) * | 2019-03-21 | 2022-12-22 | Cornell University | 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 |
| 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 |
| SU1761672A1 (ru) * | 1990-05-22 | 1992-09-15 | Белгородский технологический институт строительных материалов им.И.А.Гришманова | Способ получени тонкодисперсного мела |
| DE69425882T2 (de) | 1993-03-29 | 2001-01-11 | Basf Ag | 1-amino-3-phenoxy-propan-derivate als modulatoren bei multi-drug resistenz |
| 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 |
| ES2237919T4 (es) * | 1998-06-18 | 2007-05-01 | Bristol-Myers Squibb Company | Inhibidores aminotiazol sustituidos con carbono de quinasas dependientes de ciclina. |
| US6335170B1 (en) | 1999-02-22 | 2002-01-01 | Torben F. Orntoft | Gene expression in bladder tumors |
| AU2001249064A1 (en) | 2000-02-22 | 2001-09-03 | Mount Sinai School Of Medicine Of New York University | N-cadherin modulated migration, invasion, and metastasis |
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| 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 |
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| WO2008048967A1 (en) | 2006-10-16 | 2008-04-24 | University Of Rochester | Tripodal cyclohexane derivatives and their use as carbohydrate receptors |
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| 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 |
| RS59705B1 (sr) * | 2011-11-21 | 2020-01-31 | Calithera Biosciences Inc | Heterociklični inhibitori glutaminaze |
| RU2014141114A (ru) | 2012-03-15 | 2016-05-10 | Дзе Рисерч Фаундейшн Фор Дзе Стейт Юниверсити Оф Нью Йорк | Комбинированные виды терапии с использованием ингибиторов внеклеточного домена е-кадгерина |
| 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 |
| EP3092235A2 (en) | 2014-01-06 | 2016-11-16 | Rhizen Pharmaceuticals S.A. | Novel inhibitors of glutaminase |
| MX2016012244A (es) | 2014-03-21 | 2017-05-08 | Agios Pharmaceuticals Inc | Compuestos y sus metodos de uso. |
-
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 WO PCT/CN2013/001428 patent/WO2014079150A1/en not_active Ceased
- 2013-11-21 BR BR112015011830A patent/BR112015011830A2/pt not_active Application Discontinuation
- 2013-11-21 SI SI201331140T patent/SI2922850T1/sl unknown
- 2013-11-21 DK DK13857585.7T patent/DK2922850T3/en active
- 2013-11-21 EP EP18183580.2A patent/EP3456719A1/en not_active Withdrawn
- 2013-11-21 RS RS20181133A patent/RS57859B1/sr unknown
- 2013-11-21 KR KR1020157016414A patent/KR20150085079A/ko 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 SG SG10201609940RA patent/SG10201609940RA/en unknown
- 2013-11-21 NZ NZ708382A patent/NZ708382A/en unknown
- 2013-11-21 UA UAA201506066A patent/UA117360C2/uk unknown
- 2013-11-21 HR HRP20181628TT patent/HRP20181628T1/hr unknown
- 2013-11-21 CN CN201810824418.2A patent/CN108727307A/zh active Pending
- 2013-11-21 US US14/646,634 patent/US10087172B2/en active Active
- 2013-11-21 LT LTEP13857585.7T patent/LT2922850T/lt unknown
- 2013-11-21 PL PL13857585T patent/PL2922850T3/pl unknown
- 2013-11-21 TR TR2018/12360T patent/TR201812360T4/tr unknown
- 2013-11-21 CN CN201380070365.5A patent/CN104936954B/zh not_active Expired - Fee Related
- 2013-11-21 MY MYPI2015001355A patent/MY177344A/en unknown
- 2013-11-21 SG SG11201504049VA patent/SG11201504049VA/en unknown
- 2013-11-21 SM SM20180504T patent/SMT201800504T1/it unknown
- 2013-11-21 JP JP2015543242A patent/JP6333277B2/ja not_active Expired - Fee Related
- 2013-11-21 HU HUE13857585A patent/HUE040111T2/hu 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 MX MX2015006493A patent/MX367389B/es active IP Right Grant
- 2013-11-21 EA EA201590987A patent/EA030646B1/ru not_active IP Right Cessation
- 2013-11-21 PT PT13857585T patent/PT2922850T/pt unknown
- 2013-11-21 EA EA201890754A patent/EA201890754A1/ru unknown
- 2013-11-21 PE PE2015000674A patent/PE20151072A1/es unknown
- 2013-11-22 AR ARP130104322A patent/AR093598A1/es unknown
- 2013-11-22 TW TW107111990A patent/TW201906825A/zh unknown
- 2013-11-22 TW TW102142566A patent/TWI629268B/zh not_active IP Right Cessation
-
2015
- 2015-05-21 IL IL238958A patent/IL238958B/en not_active IP Right Cessation
- 2015-05-22 PH PH12015501150A patent/PH12015501150B1/en unknown
- 2015-05-22 SA SA515360469A patent/SA515360469B1/ar 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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