JP2016501189A5 - - Google Patents
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- Publication number
- JP2016501189A5 JP2016501189A5 JP2015541933A JP2015541933A JP2016501189A5 JP 2016501189 A5 JP2016501189 A5 JP 2016501189A5 JP 2015541933 A JP2015541933 A JP 2015541933A JP 2015541933 A JP2015541933 A JP 2015541933A JP 2016501189 A5 JP2016501189 A5 JP 2016501189A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- pharmaceutical composition
- optionally substituted
- 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 51
- 150000003839 salts Chemical class 0.000 claims description 26
- 239000008194 pharmaceutical composition Substances 0.000 claims description 20
- 239000000203 mixture Substances 0.000 claims description 17
- 125000000217 alkyl group Chemical group 0.000 claims description 14
- 210000004369 blood Anatomy 0.000 claims description 11
- 239000008280 blood Substances 0.000 claims description 11
- 101001091538 Homo sapiens Pyruvate kinase PKM Proteins 0.000 claims description 10
- 102100034911 Pyruvate kinase PKM Human genes 0.000 claims description 10
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 230000000694 effects Effects 0.000 claims description 10
- 125000001072 heteroaryl group Chemical group 0.000 claims description 10
- 210000003743 erythrocyte Anatomy 0.000 claims description 9
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 6
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 6
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 6
- -1 quinolin-8-yl Chemical group 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 5
- 201000011510 cancer Diseases 0.000 claims description 5
- 238000004519 manufacturing process Methods 0.000 claims description 5
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 125000001188 haloalkyl group Chemical group 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 208000007475 hemolytic anemia Diseases 0.000 claims description 3
- 238000000338 in vitro Methods 0.000 claims description 3
- 208000007056 sickle cell anemia Diseases 0.000 claims description 3
- XOHUEYCVLUUEJJ-UHFFFAOYSA-I 2,3-Diphosphoglycerate Chemical compound [O-]P(=O)([O-])OC(C(=O)[O-])COP([O-])([O-])=O XOHUEYCVLUUEJJ-UHFFFAOYSA-I 0.000 claims description 2
- 125000003545 alkoxy group Chemical group 0.000 claims description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001475 halogen functional group Chemical group 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 125000001424 substituent group Chemical group 0.000 claims description 2
- 230000001105 regulatory effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 8
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 235000014655 lactic acid Nutrition 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 230000010627 oxidative phosphorylation Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261724266P | 2012-11-08 | 2012-11-08 | |
| US61/724,266 | 2012-11-08 | ||
| PCT/US2013/069193 WO2014074848A1 (en) | 2012-11-08 | 2013-11-08 | Therapeutic compounds and compositions and their use as pkm2 modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016501189A JP2016501189A (ja) | 2016-01-18 |
| JP2016501189A5 true JP2016501189A5 (enExample) | 2016-12-22 |
| JP6362610B2 JP6362610B2 (ja) | 2018-07-25 |
Family
ID=49667584
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015541933A Expired - Fee Related JP6362610B2 (ja) | 2012-11-08 | 2013-11-08 | 治療用化合物及び組成物並びにｐｋｍ２調節剤としてのそれらの使用 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US9458132B2 (enExample) |
| EP (1) | EP2917207A1 (enExample) |
| JP (1) | JP6362610B2 (enExample) |
| KR (1) | KR20150080619A (enExample) |
| CN (1) | CN104822672B (enExample) |
| AU (1) | AU2013342203B2 (enExample) |
| CA (1) | CA2890664A1 (enExample) |
| EA (1) | EA032007B1 (enExample) |
| HK (1) | HK1213888A1 (enExample) |
| MX (1) | MX2015005841A (enExample) |
| NZ (1) | NZ707778A (enExample) |
| WO (1) | WO2014074848A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6243918B2 (ja) | 2012-10-16 | 2017-12-06 | トレロ ファーマシューティカルズ， インコーポレイテッド | Ｐｋｍ２調節因子およびそれらの使用方法 |
| AU2014216178B2 (en) | 2013-02-15 | 2018-06-28 | KALA BIO, Inc. | Therapeutic compounds and uses thereof |
| US9688688B2 (en) | 2013-02-20 | 2017-06-27 | Kala Pharmaceuticals, Inc. | Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof |
| EP2958895B1 (en) | 2013-02-20 | 2020-08-19 | Kala Pharmaceuticals, Inc. | Therapeutic compounds and uses thereof |
| US9890173B2 (en) | 2013-11-01 | 2018-02-13 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| CA2928658A1 (en) | 2013-11-01 | 2015-05-07 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| CN104817490B (zh) * | 2015-05-13 | 2017-10-13 | 北京大学 | 氨基二硫代甲酸酯类化合物及其制备方法与应用 |
| WO2017095751A1 (en) | 2015-12-02 | 2017-06-08 | Partikula Llc | Compositions and methods for modulating cancer cell metabolism |
| CA3252823A1 (en) * | 2016-06-13 | 2025-02-25 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| CA3036340A1 (en) | 2016-09-08 | 2018-03-15 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| CA3036065A1 (en) | 2016-09-08 | 2018-03-15 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| AU2017324713B2 (en) | 2016-09-08 | 2020-08-13 | KALA BIO, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| DK3448859T3 (da) | 2017-03-20 | 2019-09-23 | Forma Therapeutics Inc | Pyrrolopyrrolsammensætninger som pyruvatkinase- (pkr) aktivatorer |
| TWI796353B (zh) | 2017-08-15 | 2023-03-21 | 美商阿吉歐斯製藥公司 | 丙酮酸激酶調節劑及其用途 |
| WO2019075367A1 (en) | 2017-10-13 | 2019-04-18 | Tolero Pharmaceuticals, Inc. | PKM2 ACTIVATORS IN COMBINATION WITH OXYGEN REACTIVE SPECIES FOR THE TREATMENT OF CANCER |
| JP7450610B2 (ja) | 2018-09-19 | 2024-03-15 | ノヴォ・ノルディスク・ヘルス・ケア・アーゲー | ピルビン酸キナーゼｒの活性化 |
| WO2020061378A1 (en) | 2018-09-19 | 2020-03-26 | Forma Therapeutics, Inc. | Treating sickle cell disease with a pyruvate kinase r activating compound |
| EP3927683A1 (en) | 2019-02-19 | 2021-12-29 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| WO2020198077A1 (en) | 2019-03-22 | 2020-10-01 | Sumitomo Dainippon Pharma Oncology, Inc. | Compositions comprising pkm2 modulators and methods of treatment using the same |
| MX2022003254A (es) | 2019-09-19 | 2022-04-18 | Forma Therapeutics Inc | Composiciones activadoras de piruvato cinasa r (pkr). |
| WO2022170200A1 (en) | 2021-02-08 | 2022-08-11 | Global Blood Therapeutics, Inc. | 1-(2-sulfonyl-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4h)-yl]-ethanone derivatives as pyruvate kinase (pkr) and pkm2 activators for the treatment of sickle cell disease |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3545461B2 (ja) | 1993-09-10 | 2004-07-21 | エーザイ株式会社 | 二環式ヘテロ環含有スルホンアミド誘導体 |
| US6214879B1 (en) | 1998-03-24 | 2001-04-10 | Virginia Commonwealth University | Allosteric inhibitors of pyruvate kinase |
| DE60009319T2 (de) | 1999-09-04 | 2005-03-31 | Astrazeneca Ab | Substituierte n-phenyl-2-hydroxy-2-methyl-3,3,3-trifluorpropanamid-derivative zur erhöhung der pyruvatdehydrogenaseaktivität |
| JP2008514590A (ja) | 2004-09-24 | 2008-05-08 | アストラゼネカ・アクチエボラーグ | ベンゾイミダゾール誘導体、それを含む組成物、その製造方法及びその使用 |
| CA3041868C (en) * | 2008-10-09 | 2023-03-07 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Bis sulfonamide piperazinyl and piperidinyl activators of human pyruvatekinase |
| EP2406389B1 (en) | 2009-03-13 | 2019-05-08 | Agios Pharmaceuticals, Inc. | Methods and compositions for cell-proliferation-related disorders |
| EP2417123A2 (en) | 2009-04-06 | 2012-02-15 | Agios Pharmaceuticals, Inc. | Therapeutic compositions and related methods of use |
| WO2010124114A1 (en) | 2009-04-22 | 2010-10-28 | Janssen Pharmaceutica Nv | Azetidinyl diamides as monoacylglycerol lipase inhibitors |
| EP2448581B1 (en) * | 2009-06-29 | 2016-12-07 | Agios Pharmaceuticals, Inc. | Therapeutic compositions and related methods of use |
| CA2944788C (en) * | 2009-06-29 | 2023-08-22 | Agios Pharmaceuticals, Inc. | Compounds, and compositions thereof, which modulate pyruvate kinase m2, and methods of making same |
| US20130109672A1 (en) * | 2010-04-29 | 2013-05-02 | The United States Of America,As Represented By The Secretary, Department Of Health And Human Service | Activators of human pyruvate kinase |
| DE102010048800A1 (de) | 2010-10-20 | 2012-05-10 | Merck Patent Gmbh | Chinoxalinderivate |
| JP5837091B2 (ja) * | 2010-12-17 | 2015-12-24 | アジオス ファーマシューティカルズ， インコーポレイテッド | ピルビン酸キナーゼｍ２（ｐｋｍ２）調節剤としての新規ｎ−（４−（アゼチジン−１−カルボニル）フェニル）−（ヘテロ−）アリールスルホンアミド誘導体 |
| TWI549947B (zh) * | 2010-12-29 | 2016-09-21 | 阿吉歐斯製藥公司 | 治療化合物及組成物 |
| US9388164B2 (en) * | 2011-05-03 | 2016-07-12 | Agios Pharmaceuticals, Inc | Methods of using pyruvate kinase activators |
| KR101873543B1 (ko) * | 2011-05-03 | 2018-07-02 | 아지오스 파마슈티컬스 아이엔씨. | 치료에 사용하기 위한 피루베이트 키나아제 활성제 |
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2013
- 2013-11-08 US US14/441,746 patent/US9458132B2/en not_active Expired - Fee Related
- 2013-11-08 AU AU2013342203A patent/AU2013342203B2/en not_active Ceased
- 2013-11-08 EP EP13795929.2A patent/EP2917207A1/en not_active Withdrawn
- 2013-11-08 CN CN201380063407.2A patent/CN104822672B/zh not_active Expired - Fee Related
- 2013-11-08 MX MX2015005841A patent/MX2015005841A/es unknown
- 2013-11-08 EA EA201590881A patent/EA032007B1/ru not_active IP Right Cessation
- 2013-11-08 HK HK16101847.5A patent/HK1213888A1/zh unknown
- 2013-11-08 JP JP2015541933A patent/JP6362610B2/ja not_active Expired - Fee Related
- 2013-11-08 CA CA2890664A patent/CA2890664A1/en not_active Abandoned
- 2013-11-08 NZ NZ707778A patent/NZ707778A/en not_active IP Right Cessation
- 2013-11-08 WO PCT/US2013/069193 patent/WO2014074848A1/en not_active Ceased
- 2013-11-08 KR KR1020157014747A patent/KR20150080619A/ko not_active Withdrawn