JP2019537557A5 - - Google Patents
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- JP2019537557A5 JP2019537557A5 JP2019517767A JP2019517767A JP2019537557A5 JP 2019537557 A5 JP2019537557 A5 JP 2019537557A5 JP 2019517767 A JP2019517767 A JP 2019517767A JP 2019517767 A JP2019517767 A JP 2019517767A JP 2019537557 A5 JP2019537557 A5 JP 2019537557A5
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- JP
- Japan
- Prior art keywords
- optionally substituted
- formula
- compound according
- pharmaceutically acceptable
- 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 69
- -1 substituted Chemical class 0.000 claims description 66
- 150000003839 salts Chemical class 0.000 claims description 27
- 229910052739 hydrogen Inorganic materials 0.000 claims description 22
- 239000001257 hydrogen Substances 0.000 claims description 22
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 20
- 201000010099 disease Diseases 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 18
- 125000000217 alkyl group Chemical group 0.000 claims description 15
- 125000001072 heteroaryl group Chemical group 0.000 claims description 14
- 125000003107 substituted aryl group Chemical group 0.000 claims description 13
- 150000002431 hydrogen Chemical class 0.000 claims description 12
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 11
- 125000000304 alkynyl group Chemical group 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 9
- 125000003342 alkenyl group Chemical group 0.000 claims description 9
- 239000008194 pharmaceutical composition Substances 0.000 claims description 9
- 229910052736 halogen Inorganic materials 0.000 claims description 8
- 150000002367 halogens Chemical class 0.000 claims description 8
- 230000001404 mediated effect Effects 0.000 claims description 8
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims description 6
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims description 6
- 206010008635 Cholestasis Diseases 0.000 claims description 6
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims description 6
- 230000007870 cholestasis Effects 0.000 claims description 6
- 231100000359 cholestasis Toxicity 0.000 claims description 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 6
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 6
- 210000004185 liver Anatomy 0.000 claims description 6
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 230000001684 chronic effect Effects 0.000 claims description 4
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 4
- 230000003176 fibrotic effect Effects 0.000 claims description 4
- 201000005206 focal segmental glomerulosclerosis Diseases 0.000 claims description 4
- 231100000854 focal segmental glomerulosclerosis Toxicity 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
- 208000017169 kidney disease Diseases 0.000 claims description 4
- 208000019423 liver disease Diseases 0.000 claims description 4
- 208000030159 metabolic disease Diseases 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims description 4
- 208000010157 sclerosing cholangitis Diseases 0.000 claims description 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 3
- 239000003814 drug Substances 0.000 claims description 3
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 2
- 208000022309 Alcoholic Liver disease Diseases 0.000 claims description 2
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims description 2
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims description 2
- 206010010356 Congenital anomaly Diseases 0.000 claims description 2
- 208000026292 Cystic Kidney disease Diseases 0.000 claims description 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 2
- 208000018522 Gastrointestinal disease Diseases 0.000 claims description 2
- 206010018367 Glomerulonephritis chronic Diseases 0.000 claims description 2
- 206010051920 Glomerulonephropathy Diseases 0.000 claims description 2
- 208000024815 Granulomatous liver disease Diseases 0.000 claims description 2
- 208000018565 Hemochromatosis Diseases 0.000 claims description 2
- 206010019799 Hepatitis viral Diseases 0.000 claims description 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims description 2
- 206010055171 Hypertensive nephropathy Diseases 0.000 claims description 2
- 206010022489 Insulin Resistance Diseases 0.000 claims description 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000008589 Obesity Diseases 0.000 claims description 2
- 208000012868 Overgrowth Diseases 0.000 claims description 2
- 206010040047 Sepsis Diseases 0.000 claims description 2
- 206010048302 Tubulointerstitial nephritis Diseases 0.000 claims description 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 2
- 230000001476 alcoholic effect Effects 0.000 claims description 2
- 208000006682 alpha 1-Antitrypsin Deficiency Diseases 0.000 claims description 2
- 208000011775 arteriosclerosis disease Diseases 0.000 claims description 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 2
- 230000001580 bacterial effect Effects 0.000 claims description 2
- 125000005841 biaryl group Chemical group 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 230000002490 cerebral effect Effects 0.000 claims description 2
- 230000001587 cholestatic effect Effects 0.000 claims description 2
- 231100000850 chronic interstitial nephritis Toxicity 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 2
- 208000010643 digestive system disease Diseases 0.000 claims description 2
- 208000016097 disease of metabolism Diseases 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 2
- 208000018685 gastrointestinal system disease Diseases 0.000 claims description 2
- 208000006454 hepatitis Diseases 0.000 claims description 2
- 231100000283 hepatitis Toxicity 0.000 claims description 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 2
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims description 2
- 208000006575 hypertriglyceridemia Diseases 0.000 claims description 2
- 208000001024 intrahepatic cholestasis Diseases 0.000 claims description 2
- 230000007872 intrahepatic cholestasis Effects 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 235000016236 parenteral nutrition Nutrition 0.000 claims description 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 2
- 229940127557 pharmaceutical product Drugs 0.000 claims description 2
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims description 2
- 208000005069 pulmonary fibrosis Diseases 0.000 claims description 2
- 230000008929 regeneration Effects 0.000 claims description 2
- 238000011069 regeneration method Methods 0.000 claims description 2
- 201000002793 renal fibrosis Diseases 0.000 claims description 2
- 201000000306 sarcoidosis Diseases 0.000 claims description 2
- 208000013223 septicemia Diseases 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 210000002435 tendon Anatomy 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
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 2
- 201000001862 viral hepatitis Diseases 0.000 claims description 2
- 125000002877 alkyl aryl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000000126 substance Substances 0.000 description 35
- 238000000034 method Methods 0.000 description 9
- 125000003545 alkoxy group Chemical group 0.000 description 4
- 206010003210 Arteriosclerosis Diseases 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 125000000000 cycloalkoxy group Chemical group 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662404059P | 2016-10-04 | 2016-10-04 | |
| US62/404,059 | 2016-10-04 | ||
| PCT/US2017/055147 WO2018067704A1 (en) | 2016-10-04 | 2017-10-04 | Isoxazole analogs as fxr agonists and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019537557A JP2019537557A (ja) | 2019-12-26 |
| JP2019537557A5 true JP2019537557A5 (enExample) | 2020-09-24 |
Family
ID=61830059
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019517767A Abandoned JP2019537557A (ja) | 2016-10-04 | 2017-10-04 | Ｆｘｒアゴニストとしてのイソキサゾール類似体およびその使用方法 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10450306B2 (enExample) |
| EP (1) | EP3523298A4 (enExample) |
| JP (1) | JP2019537557A (enExample) |
| KR (1) | KR20190056436A (enExample) |
| CN (1) | CN109906223A (enExample) |
| AU (1) | AU2017338853A1 (enExample) |
| BR (1) | BR112019006651A2 (enExample) |
| CA (1) | CA3039124A1 (enExample) |
| IL (1) | IL265803A (enExample) |
| MX (1) | MX2019003790A (enExample) |
| PH (1) | PH12019550050A1 (enExample) |
| RU (1) | RU2019113066A (enExample) |
| WO (1) | WO2018067704A1 (enExample) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| SMT202100593T1 (it) | 2015-03-31 | 2021-11-12 | Enanta Pharm Inc | Derivati degli acidi biliari come agonisti di fxr/tgr5 e metodi per il loro uso |
| US10080742B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2017189663A1 (en) | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| US10080741B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| US10149835B2 (en) | 2016-05-18 | 2018-12-11 | Elmore Patent Law Group, P.C. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| US10144729B2 (en) | 2016-05-18 | 2018-12-04 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
| US10138228B2 (en) | 2016-05-18 | 2018-11-27 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use therof |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
| BR112018075734A2 (pt) | 2016-06-13 | 2019-04-02 | Gilead Sciences, Inc. | composto, composição farmacêutica, método para tratar um paciente com uma doença ou condição mediada pelo menos em parte por fxr, e, uso de um composto. |
| TW201808283A (zh) | 2016-08-05 | 2018-03-16 | 廣東東陽光藥業有限公司 | 含氮三環化合物及其在藥物中的應用 |
| BR112019006651A2 (pt) | 2016-10-04 | 2019-07-02 | Enanta Pharm Inc | análogos de isoxazol como agonistas de fxr e métodos de uso do mesmo |
| US10597391B2 (en) | 2016-10-26 | 2020-03-24 | Enanta Pharmaceuticals, Inc. | Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof |
| CN108017636A (zh) * | 2016-11-04 | 2018-05-11 | 合帕吉恩治疗公司 | 作为fxr调节剂的含氮杂环化合物 |
| JP6906626B2 (ja) | 2017-03-28 | 2021-07-21 | ギリアード サイエンシーズ， インコーポレイテッド | 肝疾患を処置するための治療的組み合わせ |
| US10689391B2 (en) | 2017-12-12 | 2020-06-23 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
| CN110128432B (zh) | 2018-02-02 | 2021-03-02 | 广东东阳光药业有限公司 | 含氮三环化合物及其在药物中的应用 |
| US10829486B2 (en) * | 2018-02-14 | 2020-11-10 | Enanta Pharmacueticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2020011146A1 (zh) * | 2018-07-11 | 2020-01-16 | 中国医药研究开发中心有限公司 | 1,2,4-噁二唑类化合物及其制备方法和医药用途 |
| CN110818704B (zh) * | 2018-08-08 | 2023-08-01 | 广州市恒诺康医药科技有限公司 | 螺桥环化合物、其药物组合物及其用途 |
| WO2020114307A1 (zh) * | 2018-12-07 | 2020-06-11 | 四川科伦博泰生物医药股份有限公司 | 异噁唑衍生物及其制备方法和用途 |
| EA202191566A1 (ru) | 2019-01-15 | 2021-11-01 | Джилид Сайенсиз, Инк. | Соединения, модулирующие fxr (nr1h4) |
| US20220127258A1 (en) * | 2019-01-31 | 2022-04-28 | The National Institutes of Pharmaceutical R&D Co., Ltd. | Aromatic ring or heteroaromatic ring compounds, preparation method therefor and medical use thereof |
| CN118388473A (zh) | 2019-02-19 | 2024-07-26 | 吉利德科学公司 | Fxr激动剂的固体形式 |
| CN111825595A (zh) * | 2019-04-15 | 2020-10-27 | 山东轩竹医药科技有限公司 | 钠通道阻滞剂 |
| US12240841B2 (en) | 2019-04-19 | 2025-03-04 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | FXR small molecule agonist and preparation method therefor and use thereof |
| WO2020231917A1 (en) | 2019-05-13 | 2020-11-19 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| AU2020312735A1 (en) | 2019-07-18 | 2021-12-16 | Enyo Pharma | Method for decreasing adverse-effects of interferon |
| JP2022541307A (ja) | 2019-07-23 | 2022-09-22 | ノバルティス アーゲー | Ｆｘｒアゴニストを含む処置 |
| EP4003349A1 (en) | 2019-07-23 | 2022-06-01 | Novartis AG | Combination treatment of liver diseases using fxr agonists |
| BR112022003884A2 (pt) | 2019-09-03 | 2022-05-31 | Novartis Ag | Tratamento de doença ou distúrbio hepático compreendendo antagonistas do receptor de actrii |
| US20220347190A1 (en) | 2019-09-19 | 2022-11-03 | Novartis Ag | Treatment comprising fxr agonists |
| US20220331341A1 (en) | 2019-09-30 | 2022-10-20 | Novartis Ag | Treatment comprising the use of fxr agonists |
| CN110804025B (zh) * | 2019-11-29 | 2022-02-08 | 扬州工业职业技术学院 | 一种卤代苯异噁唑衍生物及其制备方法与应用 |
| CN114929218A (zh) | 2019-12-20 | 2022-08-19 | 诺华股份有限公司 | 使用整联蛋白抑制剂组合治疗肝脏疾病 |
| JP2023510274A (ja) | 2020-01-15 | 2023-03-13 | アンセルム（アンスティチュート・ナシオナル・ドゥ・ラ・サンテ・エ・ドゥ・ラ・ルシェルシュ・メディカル） | Ｄ型肝炎ウイルスによる感染を処置するためのｆｘｒアゴニストの使用 |
| BR112022022338A2 (pt) | 2020-05-04 | 2023-01-10 | Amgen Inc | Compostos heterocíclicos como receptor desencadeador expresso em agonistas de células mieloides 2 e métodos de uso |
| TW202208355A (zh) | 2020-05-04 | 2022-03-01 | 美商安進公司 | 作為骨髓細胞觸發受體2促效劑之雜環化合物及使用方法 |
| CN114195786B (zh) * | 2020-09-18 | 2023-08-22 | 凯思凯迪（上海）医药科技有限公司 | 新型fxr小分子激动剂制备及其用途 |
| CN114315830B (zh) * | 2020-09-30 | 2025-08-12 | 中国科学院上海药物研究所 | Fxr小分子激动剂及其制备方法和用途 |
| US12180220B2 (en) | 2020-10-14 | 2024-12-31 | Tosk, Inc. | Heteroaryl modulators of RAS GTPase |
| US20220112178A1 (en) * | 2020-10-14 | 2022-04-14 | Tosk, Inc. | Small Molecule Modulators of RAS GTPase |
| WO2022101853A1 (en) | 2020-11-16 | 2022-05-19 | Novartis Ag | Method of determining liver fibrosis |
| EP4247793A1 (en) * | 2020-11-17 | 2023-09-27 | H. Lundbeck A/S | New catecholamine prodrugs for use in the treatment of parkinson's disease |
| JP2024502673A (ja) | 2021-01-14 | 2024-01-22 | ウエヌイグレックオ・ファーマ | Ｈｂｖ感染の処置のためのｆｘｒアゴニストとｉｆｎの相乗効果 |
| CN113024552B (zh) * | 2021-03-26 | 2022-08-05 | 厦门市博瑞来医药科技有限公司 | 一类新型非甾体fxr激动剂的合成及其应用 |
| US20240216364A1 (en) | 2021-04-28 | 2024-07-04 | Enyo Pharma | Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment |
| CN115433175B (zh) * | 2021-06-02 | 2025-05-27 | 上海交通大学 | 一类含炔基取代的喹啉和喹唑啉类化合物及其制备和用途 |
| WO2023137135A1 (en) * | 2022-01-17 | 2023-07-20 | Hepagene Therapeutics (HK) Limited | Solid forms of a benzthiazole-piperazinyl-oxazole compound and methods of use thereof |
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2017
- 2017-10-04 BR BR112019006651A patent/BR112019006651A2/pt not_active Application Discontinuation
- 2017-10-04 JP JP2019517767A patent/JP2019537557A/ja not_active Abandoned
- 2017-10-04 EP EP17859120.2A patent/EP3523298A4/en not_active Withdrawn
- 2017-10-04 RU RU2019113066A patent/RU2019113066A/ru not_active Application Discontinuation
- 2017-10-04 KR KR1020197012682A patent/KR20190056436A/ko not_active Withdrawn
- 2017-10-04 AU AU2017338853A patent/AU2017338853A1/en not_active Abandoned
- 2017-10-04 CN CN201780068563.6A patent/CN109906223A/zh active Pending
- 2017-10-04 MX MX2019003790A patent/MX2019003790A/es unknown
- 2017-10-04 CA CA3039124A patent/CA3039124A1/en not_active Abandoned
- 2017-10-04 WO PCT/US2017/055147 patent/WO2018067704A1/en not_active Ceased
- 2017-10-04 US US15/724,919 patent/US10450306B2/en active Active
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2019
- 2019-03-28 PH PH12019550050A patent/PH12019550050A1/en unknown
- 2019-04-03 IL IL265803A patent/IL265803A/en unknown
- 2019-09-13 US US16/569,819 patent/US11034684B2/en active Active