JP2018532698A5 - - Google Patents
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- JP2018532698A5 JP2018532698A5 JP2018510463A JP2018510463A JP2018532698A5 JP 2018532698 A5 JP2018532698 A5 JP 2018532698A5 JP 2018510463 A JP2018510463 A JP 2018510463A JP 2018510463 A JP2018510463 A JP 2018510463A JP 2018532698 A5 JP2018532698 A5 JP 2018532698A5
- Authority
- JP
- Japan
- Prior art keywords
- membered
- compound according
- independently
- haloalkyl
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims description 34
- 229910004013 NO 2 Inorganic materials 0.000 claims description 20
- 239000008194 pharmaceutical composition Substances 0.000 claims description 17
- 229910052805 deuterium Inorganic materials 0.000 claims description 16
- 229910052739 hydrogen Inorganic materials 0.000 claims description 16
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- 125000000217 alkyl group Chemical group 0.000 claims description 14
- 229910052736 halogen Inorganic materials 0.000 claims description 14
- 150000002367 halogens Chemical class 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
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 13
- 125000000623 heterocyclic group Chemical group 0.000 claims description 13
- 201000001431 Hyperuricemia Diseases 0.000 claims description 12
- -1 methoxy, ethoxy, i-propoxy, t-butoxy, n-butoxy, methylamino, ethylamino, difluoromethoxy, trifluoromethoxy, acetyl Chemical group 0.000 claims description 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 11
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 10
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 10
- LEHOTFFKMJEONL-UHFFFAOYSA-N Uric Acid Chemical compound N1C(=O)NC(=O)C2=C1NC(=O)N2 LEHOTFFKMJEONL-UHFFFAOYSA-N 0.000 claims description 10
- 125000004992 haloalkylamino group Chemical group 0.000 claims description 9
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 8
- UHOVQNZJYSORNB-UHFFFAOYSA-N monobenzene Natural products C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims description 8
- 201000005569 Gout Diseases 0.000 claims description 7
- 206010007027 Calculus urinary Diseases 0.000 claims description 6
- 206010018634 Gouty Arthritis Diseases 0.000 claims description 6
- 150000001204 N-oxides Chemical class 0.000 claims description 6
- TVWHNULVHGKJHS-UHFFFAOYSA-N Uric acid Natural products N1C(=O)NC(=O)C2NC(=O)NC21 TVWHNULVHGKJHS-UHFFFAOYSA-N 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims description 6
- 229940079593 drug Drugs 0.000 claims description 6
- 150000002148 esters Chemical class 0.000 claims description 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 6
- 208000017169 kidney disease Diseases 0.000 claims description 6
- 239000002207 metabolite Substances 0.000 claims description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 229940002612 prodrug Drugs 0.000 claims description 6
- 239000000651 prodrug Substances 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 239000012453 solvate Substances 0.000 claims description 6
- 125000001424 substituent group Chemical group 0.000 claims description 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 6
- 229940116269 uric acid Drugs 0.000 claims description 6
- 208000008281 urolithiasis Diseases 0.000 claims description 6
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims description 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 4
- IAKHMKGGTNLKSZ-INIZCTEOSA-N (S)-colchicine Chemical compound C1([C@@H](NC(C)=O)CC2)=CC(=O)C(OC)=CC=C1C1=C2C=C(OC)C(OC)=C1OC IAKHMKGGTNLKSZ-INIZCTEOSA-N 0.000 claims description 4
- 101000796092 Arabidopsis thaliana Sodium-dependent phosphate transport protein 1, chloroplastic Proteins 0.000 claims description 4
- 101001094043 Homo sapiens Solute carrier family 26 member 6 Proteins 0.000 claims description 4
- 102100035281 Solute carrier family 26 member 6 Human genes 0.000 claims description 4
- 108010093894 Xanthine oxidase Proteins 0.000 claims description 4
- 102100033220 Xanthine oxidase Human genes 0.000 claims description 4
- 150000001338 aliphatic hydrocarbons Chemical class 0.000 claims description 4
- 125000003342 alkenyl group Chemical group 0.000 claims description 4
- 125000003282 alkyl amino group Chemical group 0.000 claims description 4
- 125000000304 alkynyl group Chemical group 0.000 claims description 4
- 239000008280 blood Substances 0.000 claims description 4
- 210000004369 blood Anatomy 0.000 claims description 4
- 229910052794 bromium Inorganic materials 0.000 claims description 4
- 229910052801 chlorine Inorganic materials 0.000 claims description 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 229910052731 fluorine Inorganic materials 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 125000001624 naphthyl group Chemical group 0.000 claims description 4
- 125000002971 oxazolyl group Chemical group 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- 125000003363 1,3,5-triazinyl group Chemical group N1=C(N=CN=C1)* 0.000 claims description 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 2
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims description 2
- 206010054107 Nodule Diseases 0.000 claims description 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 230000003113 alkalizing effect Effects 0.000 claims description 2
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims description 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 2
- 229960001338 colchicine Drugs 0.000 claims description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 230000029142 excretion Effects 0.000 claims description 2
- IBRZMAIAORVEIM-UHFFFAOYSA-N formylcarbamic acid Chemical compound OC(=O)NC=O IBRZMAIAORVEIM-UHFFFAOYSA-N 0.000 claims description 2
- 125000002541 furyl group Chemical group 0.000 claims description 2
- 239000003862 glucocorticoid Substances 0.000 claims description 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 125000001041 indolyl group Chemical group 0.000 claims description 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 2
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims description 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 2
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims description 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 2
- 125000000466 oxiranyl group Chemical group 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 230000001737 promoting effect Effects 0.000 claims description 2
- DROIHSMGGKKIJT-UHFFFAOYSA-N propane-1-sulfonamide Chemical compound CCCS(N)(=O)=O DROIHSMGGKKIJT-UHFFFAOYSA-N 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 2
- 125000005493 quinolyl group Chemical group 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 2
- 210000002700 urine Anatomy 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 5
- 230000002401 inhibitory effect Effects 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 239000000203 mixture Substances 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510560190.7 | 2015-09-02 | ||
| CN201510560190 | 2015-09-02 | ||
| PCT/CN2016/097660 WO2017036404A1 (en) | 2015-09-02 | 2016-08-31 | Carboxy substituted (hetero) aromatic ring derivatives and preparation method and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018532698A JP2018532698A (ja) | 2018-11-08 |
| JP2018532698A5 true JP2018532698A5 (https=) | 2019-10-10 |
| JP6859323B2 JP6859323B2 (ja) | 2021-04-14 |
Family
ID=58186720
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018510463A Active JP6859323B2 (ja) | 2015-09-02 | 2016-08-31 | カルボキシ置換（ヘテロ）芳香環誘導体並びにその調製方法及び使用 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10266496B2 (https=) |
| EP (1) | EP3344604B1 (https=) |
| JP (1) | JP6859323B2 (https=) |
| KR (1) | KR102635986B1 (https=) |
| CN (1) | CN106478500B (https=) |
| AR (1) | AR105893A1 (https=) |
| AU (1) | AU2016316278B2 (https=) |
| CA (1) | CA2994336C (https=) |
| DK (1) | DK3344604T3 (https=) |
| ES (1) | ES2839201T3 (https=) |
| HU (1) | HUE052608T2 (https=) |
| MX (1) | MX2018002658A (https=) |
| RU (1) | RU2733750C2 (https=) |
| TW (1) | TWI733692B (https=) |
| WO (1) | WO2017036404A1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018157801A1 (zh) * | 2017-02-28 | 2018-09-07 | 广东东阳光药业有限公司 | 氰基取代的稠合双环衍生物及其制备方法和用途 |
| ES2639863B1 (es) * | 2017-03-10 | 2018-09-20 | Universidad De Granada | Compuestos para el tratamiento de enfermedades causadas por la acumulación de oxalato |
| WO2019057946A1 (en) | 2017-09-25 | 2019-03-28 | F. Hoffmann-La Roche Ag | MULTI-CYCLIC AROMATIC COMPOUNDS AS D-FACTOR INHIBITORS |
| CN109503513B (zh) * | 2018-12-29 | 2020-09-25 | 嘉实（湖南）医药科技有限公司 | 一种非布司他中间体的“一锅法”合成方法 |
| CN111943957B (zh) * | 2019-05-17 | 2023-01-06 | 中国医学科学院药物研究所 | 喹啉甲酰胺类化合物及其制备方法和用途 |
| AU2020374919B9 (en) * | 2019-10-30 | 2024-02-29 | Tonghua Dongbao Pharmaceutical Co., Ltd. | Thiophene derivatives as xanthine oxidase inhibitors and application thereof |
| WO2021204884A1 (de) * | 2020-04-09 | 2021-10-14 | Bayer Aktiengesellschaft | 3-(4-alkenyl-phenyl)-3-pyrrolin-2-one und deren verwendung als herbizide |
| CN113105481A (zh) * | 2021-02-25 | 2021-07-13 | 浙江农林大学暨阳学院 | 一种双金属催化制备苯并-6，8-二氢异喹啉-1-亚硒砜基苯甲酰胺类化合物的方法 |
| AU2022265937B2 (en) * | 2021-04-29 | 2025-04-17 | Tonghua Dongbao Pharmaceutical Co., Ltd. | Crystal form of thiophene derivative and preparation method therefor |
| JP2025515359A (ja) * | 2022-04-27 | 2025-05-14 | 杭州新元素▲薬▼▲業▼有限公司 | 痛風に用いられる化合物 |
| CN116715633B (zh) * | 2022-04-27 | 2025-08-12 | 杭州新元素药业股份有限公司 | 可用于降尿酸的化合物 |
| CN115417804A (zh) * | 2022-09-16 | 2022-12-02 | 天津药明康德新药开发有限公司 | 一种7-甲基-1h-吲哚-5-羧酸的合成方法 |
| CN116375603A (zh) * | 2023-03-03 | 2023-07-04 | 大连理工大学 | 一种合成苯丙环丁烯衍生物的方法 |
| CN118063418A (zh) * | 2024-02-27 | 2024-05-24 | 无锡捷化医药科技有限公司 | 一种2-甲基-7-硝基苯并呋喃-4-甲酸的制备方法 |
| WO2025223330A1 (zh) * | 2024-04-23 | 2025-10-30 | 深壶制药(山东)有限公司 | 吲哚并饱和环类化合物或其衍生物及其应用 |
| CN119492694B (zh) * | 2024-11-12 | 2025-09-30 | 科顺防水科技股份有限公司 | 化学阻根剂手性分布的测量方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU642743B2 (en) | 1990-05-21 | 1993-10-28 | Smith Kline & French Laboratories Limited | Phenol and pyridinol derivatives as pharmaceuticals |
| DK0513379T3 (da) * | 1990-11-30 | 1996-09-30 | Teijin Ltd | 2-Arylthiazolderivater og farmaceutisk præparat indeholdende sådanne |
| US8003647B2 (en) | 2007-04-11 | 2011-08-23 | Kissei Pharmaceutical Co., Ltd. | (Aza)indole derivative and use thereof for medical purposes |
| AU2009304713B2 (en) * | 2008-10-15 | 2013-10-31 | Kissei Pharmaceutical Co., Ltd. | Fused-ring derivative and medical application of same |
| EP2338887A4 (en) * | 2008-10-15 | 2012-05-09 | Kissei Pharmaceutical | FUSIONED HETEROCYCLIC DERIVATIVE AND ITS USE FOR MEDICAL PURPOSES |
| WO2010093191A2 (en) * | 2009-02-13 | 2010-08-19 | Lg Life Sciences Ltd. | Novel compounds effective as xanthine oxidase inhibitors, method for preparing the same, and pharmaceutical composition containing the same |
| SI2415771T1 (sl) | 2009-03-31 | 2013-12-31 | Kissei Pharmaceutical Co., Ltd. | Derivat indolizina in njegova uporaba v medicinske namene |
| TWI423962B (zh) * | 2009-10-07 | 2014-01-21 | Lg Life Sciences Ltd | 有效作為黃嘌呤氧化酶抑制劑之新穎化合物、其製備方法及含該化合物之醫藥組成物 |
| ES2549926T3 (es) | 2010-09-29 | 2015-11-03 | Kissei Pharmaceutical Co., Ltd. | Derivados (aza)indolizínicos como inhibidores de la xantina-oxidasa |
| CN105308040B (zh) | 2013-06-21 | 2019-06-04 | 默克专利股份公司 | 1,3-二氨基环戊烷甲酰胺衍生物 |
| JP2015214527A (ja) * | 2014-05-13 | 2015-12-03 | 帝人ファーマ株式会社 | イミダゾール誘導体 |
-
2016
- 2016-08-31 HU HUE16840833A patent/HUE052608T2/hu unknown
- 2016-08-31 RU RU2018111106A patent/RU2733750C2/ru active
- 2016-08-31 EP EP16840833.4A patent/EP3344604B1/en active Active
- 2016-08-31 DK DK16840833.4T patent/DK3344604T3/da active
- 2016-08-31 KR KR1020187008513A patent/KR102635986B1/ko active Active
- 2016-08-31 WO PCT/CN2016/097660 patent/WO2017036404A1/en not_active Ceased
- 2016-08-31 CA CA2994336A patent/CA2994336C/en active Active
- 2016-08-31 US US15/750,205 patent/US10266496B2/en active Active
- 2016-08-31 ES ES16840833T patent/ES2839201T3/es active Active
- 2016-08-31 JP JP2018510463A patent/JP6859323B2/ja active Active
- 2016-08-31 CN CN201610786469.1A patent/CN106478500B/zh active Active
- 2016-08-31 MX MX2018002658A patent/MX2018002658A/es unknown
- 2016-08-31 AU AU2016316278A patent/AU2016316278B2/en active Active
- 2016-09-01 AR ARP160102677A patent/AR105893A1/es active IP Right Grant
- 2016-09-01 TW TW105128309A patent/TWI733692B/zh active
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