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 (OSRAM) | 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 (OSRAM) |
| EP (1) | EP2917207A1 (OSRAM) |
| JP (1) | JP6362610B2 (OSRAM) |
| KR (1) | KR20150080619A (OSRAM) |
| CN (1) | CN104822672B (OSRAM) |
| AU (1) | AU2013342203B2 (OSRAM) |
| CA (1) | CA2890664A1 (OSRAM) |
| EA (1) | EA032007B1 (OSRAM) |
| HK (1) | HK1213888A1 (OSRAM) |
| MX (1) | MX2015005841A (OSRAM) |
| NZ (1) | NZ707778A (OSRAM) |
| WO (1) | WO2014074848A1 (OSRAM) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2909181T3 (da) | 2012-10-16 | 2017-11-20 | Tolero Pharmaceuticals Inc | PKM2-modulatorer og fremgangsmåder til anvendelse deraf |
| JP6669499B2 (ja) | 2013-02-15 | 2020-03-18 | カラ ファーマシューティカルズ インコーポレイテッド | 治療用化合物 |
| WO2014130612A1 (en) | 2013-02-20 | 2014-08-28 | Kala Pharmaceuticals, 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 |
| CN108530458A (zh) | 2013-11-01 | 2018-09-14 | 卡拉制药公司 | 治疗化合物的结晶形式及其用途 |
| US9890173B2 (en) | 2013-11-01 | 2018-02-13 | 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 |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (NR1H4) |
| EP3509423A4 (en) | 2016-09-08 | 2020-05-13 | 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 |
| EP3509421A4 (en) | 2016-09-08 | 2020-05-20 | Kala Pharmaceuticals, Inc. | CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF |
| US11014927B2 (en) * | 2017-03-20 | 2021-05-25 | Forma Therapeutics, Inc. | Pyrrolopyrrole compositions as pyruvate kinase (PKR) activators |
| MX2020001832A (es) | 2017-08-15 | 2020-07-22 | Agios Pharmaceuticals Inc | Activadores de piruvato quinasas para usar en el tratamiento de trastornos en la sangre. |
| US20200237766A1 (en) | 2017-10-13 | 2020-07-30 | Tolero Pharmaceuticals, Inc. | Pkm2 activators in combination with reactive oxygen species for treatment of cancer |
| US12053458B2 (en) | 2018-09-19 | 2024-08-06 | Novo Nordisk Health Care Ag | Treating sickle cell disease with a pyruvate kinase R activating compound |
| ES2989438T3 (es) | 2018-09-19 | 2024-11-26 | Novo Nordisk Healthcare Ag | Activación de la piruvato cinasa R |
| CN118388474A (zh) | 2019-02-19 | 2024-07-26 | 吉利德科学公司 | Fxr激动剂的固体形式 |
| CA3133460A1 (en) | 2019-03-22 | 2020-10-01 | Sumitomo Dainippon Pharma Oncology, Inc. | Compositions comprising pkm2 modulators and methods of treatment using the same |
| EP4031132A4 (en) | 2019-09-19 | 2023-09-13 | Forma Therapeutics, Inc. | Activating pyruvate kinase r |
| TW202245758A (zh) | 2021-02-08 | 2022-12-01 | 美商全球血液治療公司 | 作為丙酮酸激酶活化劑之吡咯啶-吡唑 |
| 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 |
| MXPA02002319A (es) | 1999-09-04 | 2002-07-30 | Astrazeneca Ab | Derivados 2-hidroxi-2-metil-3,3,3-trifluoropropanamida con n-fenilo susbtituido que elevan la actividad de la deshidrogenasa de piruvato. |
| WO2006033628A1 (en) | 2004-09-24 | 2006-03-30 | Astrazeneca Ab | Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof |
| EP2344453B1 (en) * | 2008-10-09 | 2016-12-28 | The U.S.A. As Represented By The Secretary, Department Of Health And Human Services | Activators of human pyruvate kinase |
| CN108524505A (zh) | 2009-03-13 | 2018-09-14 | 安吉奥斯医药品有限公司 | 用于细胞增殖相关病症的方法和组合物 |
| CN102448951B (zh) * | 2009-04-06 | 2017-05-10 | 安吉奥斯医药品有限公司 | 丙酮酸激酶m2调节剂、治疗组合物和相关使用方法 |
| CA2759604A1 (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 |
| PT2448582T (pt) * | 2009-06-29 | 2017-07-10 | Agios Pharmaceuticals Inc | Compostos e composições terapêuticas |
| 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 |
| WO2012151448A1 (en) * | 2011-05-03 | 2012-11-08 | Agios Pharmaceuticals, Inc. | Pyruvate kinase activators for use in therapy |
| CN108451955B (zh) * | 2011-05-03 | 2022-02-01 | 安吉奥斯医药品有限公司 | 用于治疗的丙酮酸激酶活化剂 |
-
2013
- 2013-11-08 US US14/441,746 patent/US9458132B2/en not_active Expired - Fee Related
- 2013-11-08 HK HK16101847.5A patent/HK1213888A1/zh unknown
- 2013-11-08 EA EA201590881A patent/EA032007B1/ru not_active IP Right Cessation
- 2013-11-08 CN CN201380063407.2A patent/CN104822672B/zh not_active Expired - Fee Related
- 2013-11-08 CA CA2890664A patent/CA2890664A1/en not_active Abandoned
- 2013-11-08 KR KR1020157014747A patent/KR20150080619A/ko not_active Withdrawn
- 2013-11-08 MX MX2015005841A patent/MX2015005841A/es unknown
- 2013-11-08 WO PCT/US2013/069193 patent/WO2014074848A1/en not_active Ceased
- 2013-11-08 EP EP13795929.2A patent/EP2917207A1/en not_active Withdrawn
- 2013-11-08 JP JP2015541933A patent/JP6362610B2/ja not_active Expired - Fee Related
- 2013-11-08 NZ NZ707778A patent/NZ707778A/en not_active IP Right Cessation
- 2013-11-08 AU AU2013342203A patent/AU2013342203B2/en not_active Ceased
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