JP2020505333A5 - - Google Patents
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- JP2020505333A5 JP2020505333A5 JP2019537134A JP2019537134A JP2020505333A5 JP 2020505333 A5 JP2020505333 A5 JP 2020505333A5 JP 2019537134 A JP2019537134 A JP 2019537134A JP 2019537134 A JP2019537134 A JP 2019537134A JP 2020505333 A5 JP2020505333 A5 JP 2020505333A5
- Authority
- JP
- Japan
- Prior art keywords
- bis
- diyl
- tetrahydroisoquinoline
- dioxo
- methyl
- 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.)
- Pending
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- 229910052757 nitrogen Inorganic materials 0.000 claims description 158
- -1 Dichloro-2-methyl-1,2,3,4-tetrahydroisoquinoline-4-yl Chemical group 0.000 claims description 103
- 150000001875 compounds Chemical class 0.000 claims description 58
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 52
- KHBQMWCZKVMBLN-UHFFFAOYSA-N Benzenesulfonamide Chemical compound NS(=O)(=O)C1=CC=CC=C1 KHBQMWCZKVMBLN-UHFFFAOYSA-N 0.000 claims description 32
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 32
- 125000000623 heterocyclic group Chemical group 0.000 claims description 25
- 125000001072 heteroaryl group Chemical group 0.000 claims description 24
- 125000000217 alkyl group Chemical group 0.000 claims description 23
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 20
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 20
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 16
- 239000004202 carbamide Substances 0.000 claims description 16
- 229910052799 carbon Inorganic materials 0.000 claims description 16
- 229910052760 oxygen Inorganic materials 0.000 claims description 16
- 125000003118 aryl group Chemical group 0.000 claims description 14
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 14
- 229910052736 halogen Inorganic materials 0.000 claims description 13
- 150000002367 halogens Chemical class 0.000 claims description 13
- 229910052717 sulfur Inorganic materials 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 11
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 10
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 10
- 125000005842 heteroatom Chemical group 0.000 claims description 10
- 229910052698 phosphorus Inorganic materials 0.000 claims description 10
- ZHNUHDYFZUAESO-UHFFFAOYSA-N Formamide Chemical compound NC=O ZHNUHDYFZUAESO-UHFFFAOYSA-N 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- XTFIVUDBNACUBN-UHFFFAOYSA-N 1,3,5-trinitro-1,3,5-triazinane Chemical compound [O-][N+](=O)N1CN([N+]([O-])=O)CN([N+]([O-])=O)C1 XTFIVUDBNACUBN-UHFFFAOYSA-N 0.000 claims description 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 6
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 5
- 239000012453 solvate Substances 0.000 claims description 5
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 3
- 125000004429 atom Chemical group 0.000 claims description 3
- CSTNAQPBOPARIZ-UHFFFAOYSA-N 1-[2-[2-[2-[[3-(6-chloro-2,8-dimethyl-3,4-dihydro-1H-isoquinolin-4-yl)-4-methylphenyl]sulfonylamino]ethoxy]ethoxy]ethyl]-3-[4-[2-[2-[2-[[3-(6-chloro-2,8-dimethyl-3,4-dihydro-1H-isoquinolin-4-yl)-4-methylphenyl]sulfonylamino]ethoxy]ethoxy]ethylcarbamoylamino]butyl]urea Chemical compound O=C(NCCOCCOCCNS(=O)(=O)C1=CC(=C(C=C1)C)C1CN(CC2=C(C=C(C=C12)Cl)C)C)NCCCCNC(NCCOCCOCCNS(=O)(=O)C1=CC(=C(C=C1)C)C1CN(CC2=C(C=C(C=C12)Cl)C)C)=O CSTNAQPBOPARIZ-UHFFFAOYSA-N 0.000 claims description 2
- LPOOAIYWJXCQLO-UHFFFAOYSA-N 1-[2-[2-[2-[[3-(6-chloro-2,8-dimethyl-3,4-dihydro-1H-isoquinolin-4-yl)phenyl]sulfonylamino]ethoxy]ethoxy]ethyl]-3-[4-[2-[2-[2-[[3-(6-chloro-2,8-dimethyl-3,4-dihydro-1H-isoquinolin-4-yl)phenyl]sulfonylamino]ethoxy]ethoxy]ethylcarbamoylamino]butyl]urea Chemical compound O=C(NCCOCCOCCNS(=O)(=O)C1=CC(=CC=C1)C1CN(CC2=C(C=C(C=C12)Cl)C)C)NCCCCNC(NCCOCCOCCNS(=O)(=O)C1=CC(=CC=C1)C1CN(CC2=C(C=C(C=C12)Cl)C)C)=O LPOOAIYWJXCQLO-UHFFFAOYSA-N 0.000 claims description 2
- JQJNCRYEIZDJMD-UHFFFAOYSA-N 1-[2-[2-[2-[[3-(6-chloro-8-cyano-2-methyl-3,4-dihydro-1H-isoquinolin-4-yl)-4-fluorophenyl]sulfonylamino]ethoxy]ethoxy]ethyl]-3-[4-[2-[2-[2-[[3-(6-chloro-8-cyano-2-methyl-3,4-dihydro-1H-isoquinolin-4-yl)-4-fluorophenyl]sulfonylamino]ethoxy]ethoxy]ethylcarbamoylamino]butyl]urea Chemical compound O=C(NCCOCCOCCNS(=O)(=O)C1=CC(=C(C=C1)F)C1CN(CC2=C(C=C(C=C12)Cl)C#N)C)NCCCCNC(NCCOCCOCCNS(=O)(=O)C1=CC(=C(C=C1)F)C1CN(CC2=C(C=C(C=C12)Cl)C#N)C)=O JQJNCRYEIZDJMD-UHFFFAOYSA-N 0.000 claims description 2
- FVAPOYPJYNUIPS-UHFFFAOYSA-N 1-[2-[2-[2-[[3-(6-chloro-8-cyano-2-methyl-3,4-dihydro-1H-isoquinolin-4-yl)-4-methylphenyl]sulfonylamino]ethoxy]ethoxy]ethyl]-3-[4-[2-[2-[2-[[3-(6-chloro-8-cyano-2-methyl-3,4-dihydro-1H-isoquinolin-4-yl)-4-methylphenyl]sulfonylamino]ethoxy]ethoxy]ethylcarbamoylamino]butyl]urea Chemical compound CN1CC(C2=C(C)C=CC(=C2)S(=O)(=O)NCCOCCOCCNC(=O)NCCCCNC(=O)NCCOCCOCCNS(=O)(=O)C2=CC(C3CN(C)CC4=C3C=C(Cl)C=C4C#N)=C(C)C=C2)C2=C(C1)C(=CC(Cl)=C2)C#N FVAPOYPJYNUIPS-UHFFFAOYSA-N 0.000 claims description 2
- RYXAQGKLQHUUBT-UHFFFAOYSA-N 1-[2-[2-[2-[[3-(6-chloro-8-cyano-2-methyl-3,4-dihydro-1H-isoquinolin-4-yl)phenyl]sulfonylamino]ethoxy]ethoxy]ethyl]-3-[4-[2-[2-[2-[[3-(6-chloro-8-cyano-2-methyl-3,4-dihydro-1H-isoquinolin-4-yl)phenyl]sulfonylamino]ethoxy]ethoxy]ethylcarbamoylamino]butyl]urea Chemical compound O=C(NCCOCCOCCNS(=O)(=O)C1=CC(=CC=C1)C1CN(CC2=C(C=C(C=C12)Cl)C#N)C)NCCCCNC(NCCOCCOCCNS(=O)(=O)C1=CC(=CC=C1)C1CN(CC2=C(C=C(C=C12)Cl)C#N)C)=O RYXAQGKLQHUUBT-UHFFFAOYSA-N 0.000 claims description 2
- INJBESAYBAGURN-UHFFFAOYSA-N 1-[2-[2-[2-[[5-(6,8-dichloro-2-methyl-3,4-dihydro-1H-isoquinolin-4-yl)-2-methylphenyl]sulfonylamino]ethoxy]ethoxy]ethyl]-3-[4-[2-[2-[2-[[5-(6,8-dichloro-2-methyl-3,4-dihydro-1H-isoquinolin-4-yl)-2-methylphenyl]sulfonylamino]ethoxy]ethoxy]ethylcarbamoylamino]butyl]urea Chemical compound CN1CC(C2=CC(=C(C)C=C2)S(=O)(=O)NCCOCCOCCNC(=O)NCCCCNC(=O)NCCOCCOCCNS(=O)(=O)C2=C(C)C=CC(=C2)C2CN(C)CC3=C2C=C(Cl)C=C3Cl)C2=C(C1)C(Cl)=CC(Cl)=C2 INJBESAYBAGURN-UHFFFAOYSA-N 0.000 claims description 2
- BUZIFTBLDVYRMI-UHFFFAOYSA-N 1-[2-[2-[2-[[5-(6-chloro-2,8-dimethyl-3,4-dihydro-1H-isoquinolin-4-yl)-2-methylphenyl]sulfonylamino]ethoxy]ethoxy]ethyl]-3-[4-[2-[2-[2-[[5-(6-chloro-2,8-dimethyl-3,4-dihydro-1H-isoquinolin-4-yl)-2-methylphenyl]sulfonylamino]ethoxy]ethoxy]ethylcarbamoylamino]butyl]urea Chemical compound O=C(NCCOCCOCCNS(=O)(=O)C1=C(C=CC(=C1)C1CN(CC2=C(C=C(C=C12)Cl)C)C)C)NCCCCNC(NCCOCCOCCNS(=O)(=O)C1=C(C=CC(=C1)C1CN(CC2=C(C=C(C=C12)Cl)C)C)C)=O BUZIFTBLDVYRMI-UHFFFAOYSA-N 0.000 claims description 2
- DPBWFNDFMCCGGJ-UHFFFAOYSA-N 4-Piperidine carboxamide Chemical compound NC(=O)C1CCNCC1 DPBWFNDFMCCGGJ-UHFFFAOYSA-N 0.000 claims description 2
- MGZVSYCVURJMKP-ACEFPKFPSA-N CN1C[C@H](C2=C(C1)C(=CC(=C2)Cl)Cl)C3=CC(=CC=C3)S(=O)(=O)N4CCC(CC4)C(CCNC(=O)NCCCCNC(=O)NCCCC(=O)N)C(=O)N Chemical compound CN1C[C@H](C2=C(C1)C(=CC(=C2)Cl)Cl)C3=CC(=CC=C3)S(=O)(=O)N4CCC(CC4)C(CCNC(=O)NCCCCNC(=O)NCCCC(=O)N)C(=O)N MGZVSYCVURJMKP-ACEFPKFPSA-N 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- BVOCPVIXARZNQN-UHFFFAOYSA-N nipecotamide Chemical compound NC(=O)C1CCCNC1 BVOCPVIXARZNQN-UHFFFAOYSA-N 0.000 claims description 2
- 229940124530 sulfonamide Drugs 0.000 claims description 2
- 150000003456 sulfonamides Chemical class 0.000 claims description 2
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- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 3
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762444338P | 2017-01-09 | 2017-01-09 | |
| US62/444,338 | 2017-01-09 | ||
| PCT/US2018/013027 WO2018129557A1 (en) | 2017-01-09 | 2018-01-09 | Inhibitors of nhe-mediated antiport |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020505333A JP2020505333A (ja) | 2020-02-20 |
| JP2020505333A5 true JP2020505333A5 (https=) | 2021-02-25 |
Family
ID=61074570
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019537134A Pending JP2020505333A (ja) | 2017-01-09 | 2018-01-09 | Ｎｈｅ媒介性アンチポートの阻害薬 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US11147884B2 (https=) |
| EP (1) | EP3565811A1 (https=) |
| JP (1) | JP2020505333A (https=) |
| KR (1) | KR20190128626A (https=) |
| CN (1) | CN110291082A (https=) |
| AU (1) | AU2018206479B2 (https=) |
| BR (1) | BR112019013963A2 (https=) |
| CA (1) | CA3049679A1 (https=) |
| EA (1) | EA201991676A1 (https=) |
| IL (1) | IL267821B2 (https=) |
| MA (1) | MA47203A (https=) |
| MX (1) | MX2019008171A (https=) |
| WO (1) | WO2018129557A1 (https=) |
| ZA (1) | ZA201904460B (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020181555A1 (zh) | 2019-03-14 | 2020-09-17 | 深圳仁泰医药科技有限公司 | Nhe3抑制剂的晶型a及其制备方法和应用 |
| CN112679427B (zh) * | 2019-10-17 | 2023-05-12 | 江苏恒瑞医药股份有限公司 | 四氢异喹啉类衍生物、其制备方法及其在医药上的应用 |
| WO2022127917A1 (zh) * | 2020-12-18 | 2022-06-23 | 上海济煜医药科技有限公司 | 苯并杂环取代四氢异喹啉类化合物 |
| CN114716458A (zh) * | 2021-01-04 | 2022-07-08 | 上海济煜医药科技有限公司 | 四氢异喹啉类化合物 |
| CN114805202A (zh) * | 2021-01-28 | 2022-07-29 | 江西济民可信集团有限公司 | 苯磺酰胺类化合物及其制备方法和应用 |
| CN113636960A (zh) * | 2021-08-24 | 2021-11-12 | 上海皓元医药股份有限公司 | 一种2-(氯磺酰基)环己烷-1-烯甲酸乙酯衍生物的制备方法 |
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- 2018-01-09 EA EA201991676A patent/EA201991676A1/ru unknown
- 2018-01-09 EP EP18701988.0A patent/EP3565811A1/en not_active Withdrawn
- 2018-01-09 MX MX2019008171A patent/MX2019008171A/es unknown
- 2018-01-09 BR BR112019013963A patent/BR112019013963A2/pt not_active Application Discontinuation
- 2018-01-09 JP JP2019537134A patent/JP2020505333A/ja active Pending
- 2018-01-09 AU AU2018206479A patent/AU2018206479B2/en active Active
- 2018-01-09 CA CA3049679A patent/CA3049679A1/en not_active Abandoned
- 2018-01-09 CN CN201880011759.6A patent/CN110291082A/zh active Pending
- 2018-01-09 KR KR1020197023351A patent/KR20190128626A/ko not_active Ceased
- 2018-01-09 US US16/476,835 patent/US11147884B2/en active Active
- 2018-01-09 MA MA047203A patent/MA47203A/fr unknown
- 2018-01-09 WO PCT/US2018/013027 patent/WO2018129557A1/en not_active Ceased
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2019
- 2019-07-03 IL IL267821A patent/IL267821B2/en unknown
- 2019-07-08 ZA ZA2019/04460A patent/ZA201904460B/en unknown
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