JPWO2020131807A5 - - Google Patents
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- JPWO2020131807A5 JPWO2020131807A5 JP2021534284A JP2021534284A JPWO2020131807A5 JP WO2020131807 A5 JPWO2020131807 A5 JP WO2020131807A5 JP 2021534284 A JP2021534284 A JP 2021534284A JP 2021534284 A JP2021534284 A JP 2021534284A JP WO2020131807 A5 JPWO2020131807 A5 JP WO2020131807A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- ppm
- pharmaceutically acceptable
- solvate
- acceptable salt
- 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 75
- 239000012453 solvate Substances 0.000 claims description 69
- 150000003839 salts Chemical class 0.000 claims description 68
- 229940125782 compound 2 Drugs 0.000 claims description 66
- 125000004122 cyclic group Chemical group 0.000 claims description 60
- 239000000843 powder Substances 0.000 claims description 50
- 238000000034 method Methods 0.000 claims description 48
- QEBYEVQKHRUYPE-UHFFFAOYSA-N 2-(2-chlorophenyl)-5-[(1-methylpyrazol-3-yl)methyl]-4-[[methyl(pyridin-3-ylmethyl)amino]methyl]-1h-pyrazolo[4,3-c]pyridine-3,6-dione Chemical compound C1=CN(C)N=C1CN1C(=O)C=C2NN(C=3C(=CC=CC=3)Cl)C(=O)C2=C1CN(C)CC1=CC=CN=C1 QEBYEVQKHRUYPE-UHFFFAOYSA-N 0.000 claims description 36
- 125000006165 cyclic alkyl group Chemical group 0.000 claims description 34
- 125000001153 fluoro group Chemical group F* 0.000 claims description 32
- -1 cyano, methyl Chemical group 0.000 claims description 28
- 125000005843 halogen group Chemical group 0.000 claims description 28
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 28
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 25
- 239000002253 acid Substances 0.000 claims description 21
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 18
- 239000000203 mixture Substances 0.000 claims description 17
- 238000000655 nuclear magnetic resonance spectrum Methods 0.000 claims description 16
- 229910052739 hydrogen Inorganic materials 0.000 claims description 15
- 239000001257 hydrogen Substances 0.000 claims description 15
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 14
- 125000001188 haloalkyl group Chemical group 0.000 claims description 14
- 239000008194 pharmaceutical composition Substances 0.000 claims description 13
- 125000004055 thiomethyl group Chemical group [H]SC([H])([H])* 0.000 claims description 12
- 125000003545 alkoxy group Chemical group 0.000 claims description 11
- 125000004001 thioalkyl group Chemical group 0.000 claims description 11
- 230000003197 catalytic effect Effects 0.000 claims description 10
- 239000003638 chemical reducing agent Substances 0.000 claims description 10
- 125000000217 alkyl group Chemical group 0.000 claims description 9
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 9
- 150000002431 hydrogen Chemical class 0.000 claims description 9
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 9
- JMMWKPVZQRWMSS-UHFFFAOYSA-N isopropyl acetate Chemical compound CC(C)OC(C)=O JMMWKPVZQRWMSS-UHFFFAOYSA-N 0.000 claims description 9
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical group C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 8
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 8
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 8
- JKTCBAGSMQIFNL-UHFFFAOYSA-N 2,3-dihydrofuran Chemical compound C1CC=CO1 JKTCBAGSMQIFNL-UHFFFAOYSA-N 0.000 claims description 6
- 102100030762 Apolipoprotein L1 Human genes 0.000 claims description 6
- 101100323521 Homo sapiens APOL1 gene Proteins 0.000 claims description 6
- 125000003342 alkenyl group Chemical group 0.000 claims description 6
- 125000001246 bromo group Chemical group Br* 0.000 claims description 6
- 239000003153 chemical reaction reagent Substances 0.000 claims description 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims description 5
- 201000005206 focal segmental glomerulosclerosis Diseases 0.000 claims description 5
- 231100000854 focal segmental glomerulosclerosis Toxicity 0.000 claims description 5
- 208000038001 non-diabetic kidney disease Diseases 0.000 claims description 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- SMCVPMKCDDNUCQ-UHFFFAOYSA-N methyl 3,3-dimethoxypropanoate Chemical compound COC(OC)CC(=O)OC SMCVPMKCDDNUCQ-UHFFFAOYSA-N 0.000 claims description 4
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 3
- 125000006164 6-membered heteroaryl group Chemical group 0.000 claims description 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims description 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 3
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 125000004852 dihydrofuranyl group Chemical group O1C(CC=C1)* 0.000 claims description 2
- VANNPISTIUFMLH-UHFFFAOYSA-N glutaric anhydride Chemical compound O=C1CCCC(=O)O1 VANNPISTIUFMLH-UHFFFAOYSA-N 0.000 claims description 2
- PYLWMHQQBFSUBP-UHFFFAOYSA-N monofluorobenzene Chemical compound FC1=CC=CC=C1 PYLWMHQQBFSUBP-UHFFFAOYSA-N 0.000 claims description 2
- HKOOXMFOFWEVGF-UHFFFAOYSA-N phenylhydrazine Chemical compound NNC1=CC=CC=C1 HKOOXMFOFWEVGF-UHFFFAOYSA-N 0.000 claims description 2
- 229940067157 phenylhydrazine Drugs 0.000 claims description 2
- 238000000806 fluorine-19 nuclear magnetic resonance spectrum Methods 0.000 claims 7
- 238000001460 carbon-13 nuclear magnetic resonance spectrum Methods 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000126 substance Substances 0.000 description 29
- 125000001072 heteroaryl group Chemical group 0.000 description 16
- 125000003118 aryl group Chemical group 0.000 description 14
- LMDZBCPBFSXMTL-UHFFFAOYSA-N 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide Chemical compound CCN=C=NCCCN(C)C LMDZBCPBFSXMTL-UHFFFAOYSA-N 0.000 description 8
- PAQZWJGSJMLPMG-UHFFFAOYSA-N 2,4,6-tripropyl-1,3,5,2$l^{5},4$l^{5},6$l^{5}-trioxatriphosphinane 2,4,6-trioxide Chemical compound CCCP1(=O)OP(=O)(CCC)OP(=O)(CCC)O1 PAQZWJGSJMLPMG-UHFFFAOYSA-N 0.000 description 8
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 6
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 6
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical group [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- 229910052500 inorganic mineral Inorganic materials 0.000 description 6
- 239000011707 mineral Substances 0.000 description 6
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 6
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 description 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 5
- YOETUEMZNOLGDB-UHFFFAOYSA-N 2-methylpropyl carbonochloridate Chemical compound CC(C)COC(Cl)=O YOETUEMZNOLGDB-UHFFFAOYSA-N 0.000 description 4
- WMFOQBRAJBCJND-UHFFFAOYSA-M Lithium hydroxide Chemical compound [Li+].[OH-] WMFOQBRAJBCJND-UHFFFAOYSA-M 0.000 description 4
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 4
- HUCVOHYBFXVBRW-UHFFFAOYSA-M caesium hydroxide Chemical compound [OH-].[Cs+] HUCVOHYBFXVBRW-UHFFFAOYSA-M 0.000 description 4
- PFKFTWBEEFSNDU-UHFFFAOYSA-N carbonyldiimidazole Chemical compound C1=CN=CN1C(=O)N1C=CN=C1 PFKFTWBEEFSNDU-UHFFFAOYSA-N 0.000 description 4
- 229910000000 metal hydroxide Inorganic materials 0.000 description 4
- 150000004692 metal hydroxides Chemical group 0.000 description 4
- CTSLXHKWHWQRSH-UHFFFAOYSA-N oxalyl chloride Chemical compound ClC(=O)C(Cl)=O CTSLXHKWHWQRSH-UHFFFAOYSA-N 0.000 description 4
- 150000003573 thiols Chemical class 0.000 description 4
- FYSNRJHAOHDILO-UHFFFAOYSA-N thionyl chloride Chemical compound ClS(Cl)=O FYSNRJHAOHDILO-UHFFFAOYSA-N 0.000 description 4
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 description 3
- 229940092714 benzenesulfonic acid Drugs 0.000 description 3
- 150000001638 boron Chemical class 0.000 description 3
- 125000000753 cycloalkyl group Chemical group 0.000 description 3
- 229940098779 methanesulfonic acid Drugs 0.000 description 3
- 150000003017 phosphorus Chemical class 0.000 description 3
- MIOPJNTWMNEORI-GMSGAONNSA-N (S)-camphorsulfonic acid Chemical compound C1C[C@@]2(CS(O)(=O)=O)C(=O)C[C@@H]1C2(C)C MIOPJNTWMNEORI-GMSGAONNSA-N 0.000 description 2
- ASOKPJOREAFHNY-UHFFFAOYSA-N 1-Hydroxybenzotriazole Chemical compound C1=CC=C2N(O)N=NC2=C1 ASOKPJOREAFHNY-UHFFFAOYSA-N 0.000 description 2
- JVSFQJZRHXAUGT-UHFFFAOYSA-N 2,2-dimethylpropanoyl chloride Chemical compound CC(C)(C)C(Cl)=O JVSFQJZRHXAUGT-UHFFFAOYSA-N 0.000 description 2
- GPIQOFWTZXXOOV-UHFFFAOYSA-N 2-chloro-4,6-dimethoxy-1,3,5-triazine Chemical group COC1=NC(Cl)=NC(OC)=N1 GPIQOFWTZXXOOV-UHFFFAOYSA-N 0.000 description 2
- 239000007821 HATU Substances 0.000 description 2
- 239000002841 Lewis acid Substances 0.000 description 2
- 150000007513 acids Chemical class 0.000 description 2
- 125000004103 aminoalkyl group Chemical group 0.000 description 2
- 229910052799 carbon Inorganic materials 0.000 description 2
- 150000001721 carbon Chemical group 0.000 description 2
- 150000007517 lewis acids Chemical class 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 description 1
- 208000033679 diabetic kidney disease Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 150000003460 sulfonic acids Chemical class 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862780667P | 2018-12-17 | 2018-12-17 | |
| US62/780,667 | 2018-12-17 | ||
| PCT/US2019/066746 WO2020131807A1 (en) | 2018-12-17 | 2019-12-17 | Inhibitors of apol1 and methods of using same |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022515369A JP2022515369A (ja) | 2022-02-18 |
| JP2022515369A5 JP2022515369A5 (https=) | 2022-12-23 |
| JPWO2020131807A5 true JPWO2020131807A5 (https=) | 2022-12-23 |
| JP7573528B2 JP7573528B2 (ja) | 2024-10-25 |
Family
ID=69182627
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021534284A Active JP7573528B2 (ja) | 2018-12-17 | 2019-12-17 | Ａｐｏｌ１の阻害剤及びその使用方法 |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US11618746B2 (https=) |
| EP (1) | EP3897833B1 (https=) |
| JP (1) | JP7573528B2 (https=) |
| KR (2) | KR102912203B1 (https=) |
| CN (1) | CN113453760B (https=) |
| AR (1) | AR116913A1 (https=) |
| AU (1) | AU2019405477B2 (https=) |
| CA (1) | CA3121910A1 (https=) |
| CL (1) | CL2021001561A1 (https=) |
| CO (1) | CO2021009053A2 (https=) |
| CR (1) | CR20210383A (https=) |
| DK (1) | DK3897833T3 (https=) |
| DO (1) | DOP2021000116A (https=) |
| EC (1) | ECSP21052184A (https=) |
| FI (1) | FI3897833T3 (https=) |
| IL (2) | IL283592B2 (https=) |
| JO (3) | JOP20210131A1 (https=) |
| MA (1) | MA54538A (https=) |
| MX (1) | MX2021007152A (https=) |
| PE (1) | PE20212302A1 (https=) |
| SA (1) | SA521422270B1 (https=) |
| SG (1) | SG11202105769XA (https=) |
| TW (1) | TWI848031B (https=) |
| UA (1) | UA128375C2 (https=) |
| UY (1) | UY38514A (https=) |
| WO (1) | WO2020131807A1 (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI848031B (zh) | 2018-12-17 | 2024-07-11 | 美商維泰克斯製藥公司 | Apol1抑制劑及其使用方法 |
| WO2021154997A1 (en) * | 2020-01-29 | 2021-08-05 | Vertex Pharmaceuticals Incorporated | Inhibitors of apol1 and methods of using same |
| US20210246121A1 (en) * | 2020-02-04 | 2021-08-12 | Vertex Pharmaceuticals Incorporated | Solid forms of apol1 inhibitor and methods of using same |
| CA3173808A1 (en) | 2020-03-06 | 2021-09-10 | Vertex Pharmaceuticals Incorporated | Methods of treating apol-1 dependent focal segmental glomerulosclerosis |
| CA3185604A1 (en) * | 2020-06-12 | 2021-12-16 | Vertex Pharmaceuticals Incorporated | Inhibitors of apol1 and use of the same |
| WO2021252849A1 (en) * | 2020-06-12 | 2021-12-16 | Vertex Pharmaceuticals Incorporated | Inhibitors of apol1 and use of the same |
| WO2021252863A1 (en) * | 2020-06-12 | 2021-12-16 | Vertex Pharmaceuticals Incorporated | Solid forms of apol1 inhibitor and using the same |
| IL300298B2 (en) * | 2020-08-26 | 2025-06-01 | Vertex Pharma | Inhibitors of apol1 and methods of using same |
| CN116997546A (zh) * | 2021-02-19 | 2023-11-03 | 梅兹治疗公司 | Apol1抑制剂及使用方法 |
| MX2024002229A (es) * | 2021-08-26 | 2024-05-15 | Vertex Pharma | Formas solidas de inhibidores de apolipoproteina l1 (apol1) espirotriciclicos y metodos de uso de las mismas. |
| CA3240523A1 (en) * | 2021-11-30 | 2023-06-08 | Vertex Pharmaceuticals Incorporated | Spirocyclic inhibitors of apol1 and methods of using same |
| IL314330A (en) | 2022-01-18 | 2024-09-01 | Maze Therapeutics Inc | Apol1 inhibitors and methods of use |
| CN119343353A (zh) * | 2022-02-08 | 2025-01-21 | 弗特克斯药品有限公司 | 作为APOL1抑制剂的2-甲基-4',5'-二氢螺[哌啶-4,7'-噻吩并[2,3-c]吡喃]衍生物和其使用方法 |
| WO2023194895A1 (en) | 2022-04-06 | 2023-10-12 | Glaxosmithkline Intellectual Property Development Limited | Pyrrol derivatives as inhibitors of apolipoprotein l-1 |
| US20260055083A1 (en) * | 2022-08-19 | 2026-02-26 | Maze Therapeutics, Inc. | Apol1 inhibitors and methods of use |
| WO2025006262A1 (en) * | 2023-06-29 | 2025-01-02 | Omniab, Inc. | Tetracyclic compounds containing a fused indole for treating apol1-mediated chronic kidney disease |
| GB202401326D0 (en) * | 2024-02-01 | 2024-03-20 | Podium Bio Ltd | Novel compounds |
| KR20250122547A (ko) | 2024-02-05 | 2025-08-14 | 서주사이언티픽 주식회사 | AIoT 기반 방사성 동위원소 관리 시스템 |
| WO2026012338A1 (zh) * | 2024-07-09 | 2026-01-15 | 上海旭成医药科技有限公司 | 一种APOLs抑制剂 |
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