JP2020531443A5 - - Google Patents
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- JP2020531443A5 JP2020531443A5 JP2020508498A JP2020508498A JP2020531443A5 JP 2020531443 A5 JP2020531443 A5 JP 2020531443A5 JP 2020508498 A JP2020508498 A JP 2020508498A JP 2020508498 A JP2020508498 A JP 2020508498A JP 2020531443 A5 JP2020531443 A5 JP 2020531443A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- optionally substituted
- pharmaceutically acceptable
- acceptable salt
- alkyl
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 119
- 150000003839 salts Chemical class 0.000 claims description 76
- 229910052739 hydrogen Inorganic materials 0.000 claims description 51
- 239000001257 hydrogen Substances 0.000 claims description 51
- 150000002431 hydrogen Chemical class 0.000 claims description 45
- -1 substituted Chemical class 0.000 claims description 37
- 125000000217 alkyl group Chemical group 0.000 claims description 28
- 239000008194 pharmaceutical composition Substances 0.000 claims description 20
- 238000000034 method Methods 0.000 claims description 19
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 16
- 229910052736 halogen Inorganic materials 0.000 claims description 13
- 150000002367 halogens Chemical class 0.000 claims description 13
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 12
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 12
- 208000007502 anemia Diseases 0.000 claims description 10
- 125000004432 carbon atom Chemical group C* 0.000 claims description 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 8
- 208000007475 hemolytic anemia Diseases 0.000 claims description 8
- 125000000623 heterocyclic group Chemical group 0.000 claims description 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 6
- 229910052799 carbon Inorganic materials 0.000 claims description 6
- 150000001721 carbon Chemical group 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- 125000005017 substituted alkenyl group Chemical group 0.000 claims description 6
- 125000004426 substituted alkynyl group Chemical group 0.000 claims description 6
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 6
- 208000035185 Hemolytic Congenital Anemia Diseases 0.000 claims description 4
- 206010060893 Hereditary haemolytic anaemia Diseases 0.000 claims description 4
- 208000002903 Thalassemia Diseases 0.000 claims description 4
- 201000001516 congenital hemolytic anemia Diseases 0.000 claims description 4
- 208000024987 familial hemolytic anemia Diseases 0.000 claims description 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 4
- 208000007056 sickle cell anemia Diseases 0.000 claims description 4
- 125000003107 substituted aryl group Chemical group 0.000 claims description 4
- 108700014121 Pyruvate Kinase Deficiency of Red Cells Proteins 0.000 claims description 3
- 206010014490 Elliptocytosis hereditary Diseases 0.000 claims description 2
- 208000018565 Hemochromatosis Diseases 0.000 claims description 2
- 208000001825 Hereditary elliptocytosis Diseases 0.000 claims description 2
- 208000004622 abetalipoproteinemia Diseases 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 208000005980 beta thalassemia Diseases 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001188 haloalkyl group Chemical group 0.000 claims description 2
- 208000009601 hereditary spherocytosis Diseases 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 230000000422 nocturnal effect Effects 0.000 claims description 2
- 230000001314 paroxysmal effect Effects 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 7
- 208000030760 Anaemia of chronic disease Diseases 0.000 claims 1
- 208000022400 anemia due to chronic disease Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 0 C*C(C1=O)=CC=NCC1(C)[Rn](C)C(C)N Chemical compound C*C(C1=O)=CC=NCC1(C)[Rn](C)C(C)N 0.000 description 10
- 210000003743 erythrocyte Anatomy 0.000 description 9
- 210000004369 blood Anatomy 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 108020005115 Pyruvate Kinase Proteins 0.000 description 2
- 102000013009 Pyruvate Kinase Human genes 0.000 description 2
- 230000003213 activating effect Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 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 description 1
- RTINBBNUUQZXQW-AATRIKPKSA-N CC(N)[Rn](C)/C(/C)=C/N=C Chemical compound CC(N)[Rn](C)/C(/C)=C/N=C RTINBBNUUQZXQW-AATRIKPKSA-N 0.000 description 1
- JCGZIBQMKYESAK-UHFFFAOYSA-N CCCN(C=CC(C)(C=N1)[Rn](C)C)C1=O Chemical compound CCCN(C=CC(C)(C=N1)[Rn](C)C)C1=O JCGZIBQMKYESAK-UHFFFAOYSA-N 0.000 description 1
- WHXNOIJKJFYUSM-UHFFFAOYSA-N C[n](c1c2C=NN(Cc(nc(cc3)N)c3F)C1=O)c1c2[s]c(Cc2n[nH]cc2)n1 Chemical compound C[n](c1c2C=NN(Cc(nc(cc3)N)c3F)C1=O)c1c2[s]c(Cc2n[nH]cc2)n1 WHXNOIJKJFYUSM-UHFFFAOYSA-N 0.000 description 1
- FXZBMEYGWLGHNX-UHFFFAOYSA-N C[n](c1c2C=NN(Cc3c[s]nc3)C1=O)c1c2[s]c(Cc2n[nH]cc2)n1 Chemical compound C[n](c1c2C=NN(Cc3c[s]nc3)C1=O)c1c2[s]c(Cc2n[nH]cc2)n1 FXZBMEYGWLGHNX-UHFFFAOYSA-N 0.000 description 1
- 208000017667 Chronic Disease Diseases 0.000 description 1
- 102000001554 Hemoglobins Human genes 0.000 description 1
- 108010054147 Hemoglobins Proteins 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 125000002950 monocyclic group Chemical group 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023005925A JP7530453B2 (ja) | 2017-08-15 | 2023-01-18 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
| JP2024121066A JP2024147805A (ja) | 2017-08-15 | 2024-07-26 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2017/097496 | 2017-08-15 | ||
| CN2017097496 | 2017-08-15 | ||
| US201862673526P | 2018-05-18 | 2018-05-18 | |
| US201862673533P | 2018-05-18 | 2018-05-18 | |
| US62/673,526 | 2018-05-18 | ||
| US62/673,533 | 2018-05-18 | ||
| PCT/US2018/000128 WO2019035864A1 (en) | 2017-08-15 | 2018-08-15 | PYRUVATE KINASE ACTIVATORS FOR USE IN THE TREATMENT OF BLOOD DISORDERS |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023005925A Division JP7530453B2 (ja) | 2017-08-15 | 2023-01-18 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020531443A JP2020531443A (ja) | 2020-11-05 |
| JP2020531443A5 true JP2020531443A5 (enExample) | 2021-09-30 |
| JP7275107B2 JP7275107B2 (ja) | 2023-05-17 |
Family
ID=63524352
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020508498A Active JP7275107B2 (ja) | 2017-08-15 | 2018-08-15 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
| JP2020508455A Active JP7301040B2 (ja) | 2017-08-15 | 2018-08-15 | ピルビン酸キナーゼ調節因子およびその使用 |
| JP2022199462A Pending JP2023027276A (ja) | 2017-08-15 | 2022-12-14 | ピルビン酸キナーゼ調節因子およびその使用 |
| JP2023005925A Active JP7530453B2 (ja) | 2017-08-15 | 2023-01-18 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
| JP2024121066A Pending JP2024147805A (ja) | 2017-08-15 | 2024-07-26 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020508455A Active JP7301040B2 (ja) | 2017-08-15 | 2018-08-15 | ピルビン酸キナーゼ調節因子およびその使用 |
| JP2022199462A Pending JP2023027276A (ja) | 2017-08-15 | 2022-12-14 | ピルビン酸キナーゼ調節因子およびその使用 |
| JP2023005925A Active JP7530453B2 (ja) | 2017-08-15 | 2023-01-18 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
| JP2024121066A Pending JP2024147805A (ja) | 2017-08-15 | 2024-07-26 | 血液障害の治療に使用するためのピルビン酸キナーゼ活性化因子 |
Country Status (34)
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
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| JP6594570B2 (ja) | 2017-03-20 | 2019-10-23 | フォーマ セラピューティクス，インコーポレイテッド | ピルビン酸キナーゼ（ｐｋｒ）活性化剤としてのピロロピロール組成物 |
| US11464775B2 (en) * | 2017-08-15 | 2022-10-11 | Agios Pharmaceuticals, Inc. | Pyruvate kinase modulators and use thereof |
| US12233063B2 (en) | 2017-10-20 | 2025-02-25 | The Regents Of The University Of Michigan | Compositions and methods for treating eye disorders |
| WO2020061255A1 (en) | 2018-09-19 | 2020-03-26 | Forma Therapeutics, Inc. | Activating pyruvate kinase r |
| WO2020061378A1 (en) | 2018-09-19 | 2020-03-26 | Forma Therapeutics, Inc. | Treating sickle cell disease with a pyruvate kinase r activating compound |
| BR112021015996A2 (pt) * | 2019-02-13 | 2021-11-09 | Agios Pharmaceuticals Inc | Derivados de tieno[3,2-b]pirrol[3,2-d]piridazinona e seu uso como derivados de pkm2 para o tratamento de câncer, obesidade e distúrbios relacionados a diabetes |
| JP7517337B2 (ja) * | 2019-06-26 | 2024-07-17 | 日産化学株式会社 | 電荷輸送性ワニス |
| AU2020350763A1 (en) | 2019-09-19 | 2022-04-07 | Novo Nordisk Health Care Ag | Pyruvate kinase R (PKR) activating compositions |
| AU2021311597A1 (en) * | 2020-07-21 | 2023-02-02 | The Regents Of The University Of Michigan | Compositions and methods for activating pyruvate kinase |
| CN112490502B (zh) * | 2020-12-04 | 2022-01-21 | 广州天赐高新材料股份有限公司 | 一种电解液及锂二次电池 |
| 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 |
| WO2023052783A1 (en) * | 2021-09-30 | 2023-04-06 | Sitryx Therapeutics Limited | Novel compounds |
| TW202329935A (zh) * | 2021-11-16 | 2023-08-01 | 美商阿吉歐斯製藥公司 | 用於治療ｍｄｓ相關聯之貧血及其他病況之化合物 |
| CN116159061A (zh) * | 2023-03-09 | 2023-05-26 | 上海市第十人民医院 | 丙酮酸激酶m2激活剂在制备预防或治疗心力衰竭的药物中的应用 |
| WO2024204337A1 (ja) | 2023-03-28 | 2024-10-03 | 本田技研工業株式会社 | 情報提供方法、情報提供プログラム、記憶媒体、及び情報処理装置 |
| AU2024271856A1 (en) | 2023-05-15 | 2025-11-27 | Agios Pharmaceuticals, Inc. | Crystalline salts or amorphous forms of 2-((1h-pyrazol-3-yl)methyl)-6-((6-aminopyridin-2-yl)methyl)-4-methyl-4,6-dihydro -5h-thiazolo[5',4':4,5]pyrrolo[2,3-d]pyridazin-5-one |
| TW202517652A (zh) * | 2023-07-05 | 2025-05-01 | 美商阿吉歐斯製藥公司 | 丙酮酸激酶活化劑之合成 |
| WO2025207563A1 (en) | 2024-03-27 | 2025-10-02 | Agios Pharmaceuticals, Inc. | Use of a pk activator in the treatment of sickle cell disease |
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2018
- 2018-08-15 US US16/639,086 patent/US11464775B2/en active Active
- 2018-08-15 PT PT187790688T patent/PT3668513T/pt unknown
- 2018-08-15 EP EP18766400.8A patent/EP3668512B1/en active Active
- 2018-08-15 TW TW107128431A patent/TWI796353B/zh active
- 2018-08-15 SI SI201830558T patent/SI3668513T1/sl unknown
- 2018-08-15 PL PL18779068T patent/PL3668513T3/pl unknown
- 2018-08-15 HU HUE18779068A patent/HUE057178T2/hu unknown
- 2018-08-15 CN CN201880053325.2A patent/CN111032046B/zh active Active
- 2018-08-15 WO PCT/US2018/000127 patent/WO2019035863A1/en not_active Ceased
- 2018-08-15 CN CN202310962497.4A patent/CN117186119A/zh active Pending
- 2018-08-15 TW TW111135803A patent/TWI823580B/zh active
- 2018-08-15 TW TW107128429A patent/TWI790271B/zh active
- 2018-08-15 DK DK18779068.8T patent/DK3668513T3/da active
- 2018-08-15 WO PCT/US2018/000129 patent/WO2019035865A1/en not_active Ceased
- 2018-08-15 EP EP21207073.4A patent/EP4026838A1/en not_active Withdrawn
- 2018-08-15 HU HUE18766400A patent/HUE061910T2/hu unknown
- 2018-08-15 SG SG11202001262QA patent/SG11202001262QA/en unknown
- 2018-08-15 CR CR20200123A patent/CR20200123A/es unknown
- 2018-08-15 HR HRP20220039TT patent/HRP20220039T1/hr unknown
- 2018-08-15 CN CN201880053315.9A patent/CN111032045B/zh active Active
- 2018-08-15 WO PCT/US2018/000128 patent/WO2019035864A1/en not_active Ceased
- 2018-08-15 KR KR1020207007346A patent/KR102642408B1/ko active Active
- 2018-08-15 PH PH1/2020/500343A patent/PH12020500343B1/en unknown
- 2018-08-15 KR KR1020207007344A patent/KR102717594B1/ko active Active
- 2018-08-15 ES ES18766400T patent/ES2944545T3/es active Active
- 2018-08-15 AU AU2018316587A patent/AU2018316587B2/en active Active
- 2018-08-15 JP JP2020508498A patent/JP7275107B2/ja active Active
- 2018-08-15 UA UAA202001747A patent/UA126292C2/uk unknown
- 2018-08-15 RS RS20230354A patent/RS64221B1/sr unknown
- 2018-08-15 ES ES18766063T patent/ES2966825T3/es active Active
- 2018-08-15 IL IL272599A patent/IL272599B/en unknown
- 2018-08-15 JP JP2020508455A patent/JP7301040B2/ja active Active
- 2018-08-15 US US16/639,075 patent/US11364240B2/en active Active
- 2018-08-15 LT LTEPPCT/US2018/000128T patent/LT3668513T/lt unknown
- 2018-08-15 AU AU2018316588A patent/AU2018316588B2/en active Active
- 2018-08-15 US US16/639,081 patent/US11590132B2/en active Active
- 2018-08-15 SM SM20220023T patent/SMT202200023T1/it unknown
- 2018-08-15 KR KR1020237028222A patent/KR102764124B1/ko active Active
- 2018-08-15 BR BR112020003262-0A patent/BR112020003262A2/pt active Search and Examination
- 2018-08-15 PL PL18766400.8T patent/PL3668512T3/pl unknown
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- 2018-08-15 EP EP18766063.4A patent/EP3668881B1/en active Active
- 2018-08-15 CA CA3072455A patent/CA3072455A1/en active Pending
- 2018-08-15 RS RS20220003A patent/RS62871B1/sr unknown
- 2018-08-15 MD MDE20200663T patent/MD3668513T2/ro unknown
- 2018-08-15 MY MYPI2020000757A patent/MY204421A/en unknown
- 2018-08-15 ES ES18779068T patent/ES2905100T3/es active Active
- 2018-08-15 SI SI201830914T patent/SI3668512T1/sl unknown
- 2018-08-15 HR HRP20230452TT patent/HRP20230452T1/hr unknown
- 2018-08-15 PE PE2020000245A patent/PE20200724A1/es unknown
- 2018-08-15 BR BR112020003254-9A patent/BR112020003254A2/pt unknown
- 2018-08-15 EP EP18779068.8A patent/EP3668513B1/en active Active
- 2018-08-15 LT LTEPPCT/US2018/000129T patent/LT3668512T/lt unknown
- 2018-08-15 MX MX2020001833A patent/MX2020001833A/es unknown
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2020
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2022
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2023
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2024
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