JP2020531432A5 - - Google Patents
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- JP2020531432A5 JP2020531432A5 JP2020508455A JP2020508455A JP2020531432A5 JP 2020531432 A5 JP2020531432 A5 JP 2020531432A5 JP 2020508455 A JP2020508455 A JP 2020508455A JP 2020508455 A JP2020508455 A JP 2020508455A JP 2020531432 A5 JP2020531432 A5 JP 2020531432A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- protecting group
- formula
- cycloalkyl
- 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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- 229910052739 hydrogen Inorganic materials 0.000 claims description 90
- 239000001257 hydrogen Substances 0.000 claims description 90
- 125000000217 alkyl group Chemical group 0.000 claims description 85
- -1 substituted Chemical class 0.000 claims description 79
- 150000002431 hydrogen Chemical group 0.000 claims description 72
- 150000001875 compounds Chemical class 0.000 claims description 56
- 238000000034 method Methods 0.000 claims description 53
- 125000000623 heterocyclic group Chemical group 0.000 claims description 46
- 125000001072 heteroaryl group Chemical group 0.000 claims description 34
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 34
- 150000003839 salts Chemical class 0.000 claims description 34
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 29
- 229910052736 halogen Inorganic materials 0.000 claims description 24
- 150000002367 halogens Chemical class 0.000 claims description 24
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 22
- 125000004432 carbon atom Chemical group C* 0.000 claims description 22
- 125000003118 aryl group Chemical group 0.000 claims description 20
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 20
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 18
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 18
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 16
- 125000005017 substituted alkenyl group Chemical group 0.000 claims description 14
- 125000004426 substituted alkynyl group Chemical group 0.000 claims description 14
- 125000003107 substituted aryl group Chemical group 0.000 claims description 14
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 12
- 125000005843 halogen group Chemical group 0.000 claims description 12
- 201000010099 disease Diseases 0.000 claims description 10
- 125000002947 alkylene group Chemical group 0.000 claims description 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 8
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 6
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 6
- 206010012601 diabetes mellitus Diseases 0.000 claims description 6
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 6
- 125000003342 alkenyl group Chemical group 0.000 claims description 5
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims description 4
- 208000005692 Bloom Syndrome Diseases 0.000 claims description 4
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims description 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 208000029078 coronary artery disease Diseases 0.000 claims description 4
- 230000008878 coupling Effects 0.000 claims description 4
- 238000010168 coupling process Methods 0.000 claims description 4
- 238000005859 coupling reaction Methods 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
- 125000002950 monocyclic group Chemical group 0.000 claims description 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 2
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 claims description 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000008589 Obesity Diseases 0.000 claims description 2
- 208000031481 Pathologic Constriction Diseases 0.000 claims description 2
- 102000013009 Pyruvate Kinase Human genes 0.000 claims description 2
- 108020005115 Pyruvate Kinase Proteins 0.000 claims description 2
- 230000002159 abnormal effect Effects 0.000 claims description 2
- 230000004913 activation Effects 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 230000008901 benefit Effects 0.000 claims description 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 150000001721 carbon Chemical group 0.000 claims description 2
- 230000004663 cell proliferation Effects 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 239000008103 glucose Substances 0.000 claims description 2
- 125000001188 haloalkyl group Chemical group 0.000 claims description 2
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 201000001421 hyperglycemia Diseases 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 125000006239 protecting group Chemical group 0.000 claims description 2
- 208000037804 stenosis Diseases 0.000 claims description 2
- 125000005415 substituted alkoxy group Chemical group 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 239000011593 sulfur Substances 0.000 claims description 2
- 0 *C(*=I)(N(C1=O)N=Cc2c1[n](*)c1c2[s]c(I*)n1)[Ru] Chemical compound *C(*=I)(N(C1=O)N=Cc2c1[n](*)c1c2[s]c(I*)n1)[Ru] 0.000 description 26
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 9
- 125000003545 alkoxy group Chemical group 0.000 description 5
- 239000011541 reaction mixture Substances 0.000 description 4
- 238000003556 assay Methods 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 239000012895 dilution Substances 0.000 description 2
- 238000010790 dilution Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 239000011535 reaction buffer Substances 0.000 description 2
- 230000001105 regulatory effect Effects 0.000 description 2
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- SCIOVXDURPOXPM-UTCJRWHESA-N CC(C(N(C)/C=N\N[RnH])=O)[RnH] Chemical compound CC(C(N(C)/C=N\N[RnH])=O)[RnH] SCIOVXDURPOXPM-UTCJRWHESA-N 0.000 description 1
- JQKCGRMCAXRDNC-GQCTYLIASA-N CCN/C=N\C=C(/C)\[Rn]=N Chemical compound CCN/C=N\C=C(/C)\[Rn]=N JQKCGRMCAXRDNC-GQCTYLIASA-N 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 239000007983 Tris buffer Substances 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 229930027945 nicotinamide-adenine dinucleotide Natural products 0.000 description 1
- BOPGDPNILDQYTO-NNYOXOHSSA-N nicotinamide-adenine dinucleotide Chemical compound C1=CCC(C(=O)N)=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](COP(O)(=O)OP(O)(=O)OC[C@@H]2[C@H]([C@@H](O)[C@@H](O2)N2C3=NC=NC(N)=C3N=C2)O)O1 BOPGDPNILDQYTO-NNYOXOHSSA-N 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 239000011550 stock solution Substances 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022199462A 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 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2017/097496 | 2017-08-15 | ||
| CN2017097496 | 2017-08-15 | ||
| US201862673533P | 2018-05-18 | 2018-05-18 | |
| US201862673526P | 2018-05-18 | 2018-05-18 | |
| US62/673,526 | 2018-05-18 | ||
| US62/673,533 | 2018-05-18 | ||
| PCT/US2018/000129 WO2019035865A1 (en) | 2017-08-15 | 2018-08-15 | MODULATORS OF PYRUVATE KINASE AND THEIR USE |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022199462A Division 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020531432A JP2020531432A (ja) | 2020-11-05 |
| JP2020531432A5 true JP2020531432A5 (https=) | 2021-09-30 |
| JP7301040B2 JP7301040B2 (ja) | 2023-06-30 |
Family
ID=63524352
Family Applications (5)
| 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 |
| 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 |
| 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 |
|---|---|---|---|
| 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 |
| 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)
| Country | Link |
|---|---|
| US (8) | US11464775B2 (https=) |
| EP (4) | EP3668881B1 (https=) |
| JP (5) | JP7301040B2 (https=) |
| KR (3) | KR102642408B1 (https=) |
| CN (3) | CN111032045B (https=) |
| AU (4) | AU2018316588B2 (https=) |
| BR (1) | BR112020003254A2 (https=) |
| CA (1) | CA3072455A1 (https=) |
| CL (1) | CL2020000375A1 (https=) |
| CO (2) | CO2020002959A2 (https=) |
| CR (1) | CR20200123A (https=) |
| CY (1) | CY1124953T1 (https=) |
| DK (2) | DK3668513T3 (https=) |
| EC (1) | ECSP20018487A (https=) |
| ES (3) | ES2905100T3 (https=) |
| FI (1) | FI3668512T3 (https=) |
| HR (2) | HRP20220039T1 (https=) |
| HU (2) | HUE061910T2 (https=) |
| IL (3) | IL272599B (https=) |
| LT (2) | LT3668513T (https=) |
| MD (1) | MD3668513T2 (https=) |
| MX (2) | MX2020001833A (https=) |
| MY (1) | MY204421A (https=) |
| PE (1) | PE20200724A1 (https=) |
| PH (1) | PH12020500343B1 (https=) |
| PL (2) | PL3668513T3 (https=) |
| PT (2) | PT3668513T (https=) |
| RS (2) | RS62871B1 (https=) |
| SG (2) | SG11202001262QA (https=) |
| SI (2) | SI3668512T1 (https=) |
| SM (2) | SMT202200023T1 (https=) |
| TW (3) | TWI796353B (https=) |
| UA (1) | UA126292C2 (https=) |
| WO (3) | WO2019035864A1 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT3483164T (lt) | 2017-03-20 | 2020-05-11 | Forma Therapeutics, Inc. | Pirolpirolo kompozicijos kaip piruvato kinazės (pkr) aktyvatoriai |
| 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 |
| EP3697354A4 (en) | 2017-10-20 | 2021-06-30 | The Regents of The University of Michigan | EYE DISEASE COMPOSITIONS AND METHODS |
| EP3852791B1 (en) | 2018-09-19 | 2024-07-03 | Novo Nordisk Health Care AG | Activating pyruvate kinase r |
| EP3853206B1 (en) | 2018-09-19 | 2024-04-10 | Novo Nordisk Health Care AG | 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 |
| WO2020262419A1 (ja) * | 2019-06-26 | 2020-12-30 | 日産化学株式会社 | 電荷輸送性ワニス |
| HRP20251148T1 (hr) | 2019-09-19 | 2025-11-21 | Novo Nordisk Health Care Ag | Pripravci koji aktiviraju piruvat-kinazu r (pkr) |
| EP4185293A4 (en) * | 2020-07-21 | 2025-01-15 | 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 |
| US11566030B2 (en) | 2021-02-08 | 2023-01-31 | Global Blood Therapeutics, Inc. | Substituted 2,6-dihydropyrrolo[3,4-c]pyrazoles as pyruvate kinase activators |
| 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 |
| IL312679A (en) * | 2021-11-16 | 2024-07-01 | Agios Pharmaceuticals Inc | Compounds for the treatment of anemia associated with MDS and other conditions |
| 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 |
| EP4671102A1 (en) | 2023-03-28 | 2025-12-31 | Honda Motor Co., Ltd. | METHOD FOR PROVIDING INFORMATION, PROGRAM FOR PROVIDING INFORMATION, STORAGE MEDIA AND INFORMATION PROCESSING APPARATUS |
| TW202509043A (zh) | 2023-05-15 | 2025-03-01 | 美商阿吉歐斯製藥公司 | ２－（（１ｈ－吡唑－３－基）甲基）－６－（（６－胺基吡啶－２－基）甲基）－４－甲基－４，６－二氫－５ｈ－噻唑基［５＇，４＇：４，５］吡咯并［２，３－ｄ］嗒𠯤－５－酮之結晶形式 |
| KR20260035223A (ko) * | 2023-07-05 | 2026-03-12 | 아지오스 파마슈티컬스 아이엔씨. | 피루브산 키나아제 활성화제의 합성 |
| TW202539675A (zh) | 2024-03-27 | 2025-10-16 | 美商阿吉歐斯製藥公司 | Ｐｋ活化劑在治療鐮狀細胞疾病中之用途 |
| WO2026076363A1 (en) | 2024-10-04 | 2026-04-09 | Agios Pharmaceuticals, Inc. | Compounds for treating mds-associated anemias and other conditions |
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| US4405635A (en) | 1979-06-18 | 1983-09-20 | Merrell Dow Pharmaceuticals Inc. | 4-Aroylimidazol-2-ones and their use as pharmaceuticals |
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| CA2380644A1 (en) | 1999-07-30 | 2001-02-08 | Basf Aktiengesellschaft | 2-pyrazolin-5-ones |
| CA2381581A1 (en) | 1999-09-04 | 2001-03-15 | Astrazeneca Ab | Substituted n-phenyl 2-hydroxy-2-methyl-3,3,3-trifluoropropanamide derivatives which elevate pyruvate dehydrogenase activity |
| EP1972629A1 (en) * | 2007-03-23 | 2008-09-24 | Mutabilis SA | New imidazolo-heteroaryl derivatives with antibacterial properties |
| FR2933983B1 (fr) * | 2008-07-15 | 2010-08-27 | Servier Lab | Nouveaux derives tricycliques,leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| MX2011000843A (es) * | 2008-07-23 | 2011-04-11 | Vertex Pharma | Inhibidores de pirazolopiridin cinasa triciclicos. |
| EP2334673A1 (en) * | 2008-08-29 | 2011-06-22 | Amgen Inc. | PYRIDO[3,2-d]PYRIDAZINE-2(1H)-ONE COMPOUNDS AS P38 MODULATORS AND METHODS OF USE THEREOF |
| WO2010042867A2 (en) | 2008-10-09 | 2010-04-15 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Activators of human pyruvate kinase |
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| 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 |
| KR101861883B1 (ko) | 2010-12-06 | 2018-05-28 | 글락소 그룹 리미티드 | Lp-PLA₂에 의해 매개되는 질환 또는 상태의 치료에 사용하기 위한 피리미디논 화합물 |
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| SMT202400081T1 (it) * | 2011-05-03 | 2024-03-13 | Agios Pharmaceuticals Inc | Attivatori della piruvato chinasi per uso in terapia |
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| 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 |
| 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 |
-
2018
- 2018-08-15 TW TW107128431A patent/TWI796353B/zh active
- 2018-08-15 MX MX2020001833A patent/MX2020001833A/es unknown
- 2018-08-15 RS RS20220003A patent/RS62871B1/sr unknown
- 2018-08-15 PL PL18779068T patent/PL3668513T3/pl unknown
- 2018-08-15 RS RS20230354A patent/RS64221B1/sr unknown
- 2018-08-15 SM SM20220023T patent/SMT202200023T1/it unknown
- 2018-08-15 PE PE2020000245A patent/PE20200724A1/es unknown
- 2018-08-15 CN CN201880053315.9A patent/CN111032045B/zh active Active
- 2018-08-15 EP EP18766063.4A patent/EP3668881B1/en active Active
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