JP2017537960A5 - - Google Patents
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- JP2017537960A5 JP2017537960A5 JP2017532168A JP2017532168A JP2017537960A5 JP 2017537960 A5 JP2017537960 A5 JP 2017537960A5 JP 2017532168 A JP2017532168 A JP 2017532168A JP 2017532168 A JP2017532168 A JP 2017532168A JP 2017537960 A5 JP2017537960 A5 JP 2017537960A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- compound
- acceptable salt
- methoxy
- formula
- 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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- 150000001875 compounds Chemical class 0.000 claims description 71
- 150000003839 salts Chemical class 0.000 claims description 34
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 102100038495 Bile acid receptor Human genes 0.000 claims description 8
- 101000603876 Homo sapiens Bile acid receptor Proteins 0.000 claims description 8
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims description 8
- 125000000217 alkyl group Chemical group 0.000 claims description 8
- 206010069703 Bile acid malabsorption Diseases 0.000 claims description 7
- 208000019423 liver disease Diseases 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 6
- 125000003545 alkoxy group Chemical group 0.000 claims description 4
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 229910052739 hydrogen Inorganic materials 0.000 claims description 4
- 239000001257 hydrogen Substances 0.000 claims description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 4
- 235000001968 nicotinic acid Nutrition 0.000 claims description 4
- 239000011664 nicotinic acid Substances 0.000 claims description 4
- NIPZZXUFJPQHNH-UHFFFAOYSA-N pyrazine-2-carboxylic acid Chemical compound OC(=O)C1=CN=CC=N1 NIPZZXUFJPQHNH-UHFFFAOYSA-N 0.000 claims description 4
- 125000003373 pyrazinyl 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
- 201000011374 Alagille syndrome Diseases 0.000 claims description 3
- 206010056979 Colitis microscopic Diseases 0.000 claims description 3
- 206010010317 Congenital absence of bile ducts Diseases 0.000 claims description 3
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 3
- 208000009329 Graft vs Host Disease Diseases 0.000 claims description 3
- 206010024715 Liver transplant rejection Diseases 0.000 claims description 3
- 206010057969 Reflux gastritis Diseases 0.000 claims description 3
- 201000005271 biliary atresia Diseases 0.000 claims description 3
- 210000002798 bone marrow cell Anatomy 0.000 claims description 3
- 206010009887 colitis Diseases 0.000 claims description 3
- 208000008609 collagenous colitis Diseases 0.000 claims description 3
- 208000024908 graft versus host disease Diseases 0.000 claims description 3
- 208000027138 indeterminate colitis Diseases 0.000 claims description 3
- 208000004341 lymphocytic colitis Diseases 0.000 claims description 3
- 210000000130 stem cell Anatomy 0.000 claims description 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 3
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical group C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims description 2
- 206010012735 Diarrhoea Diseases 0.000 claims description 2
- 239000003613 bile acid Substances 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 229910052736 halogen Inorganic materials 0.000 claims description 2
- 150000002367 halogens Chemical class 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- PVNIIMVLHYAWGP-UHFFFAOYSA-M nicotinate Chemical compound [O-]C(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-M 0.000 claims description 2
- NIPZZXUFJPQHNH-UHFFFAOYSA-M pyrazine-2-carboxylate Chemical compound [O-]C(=O)C1=CN=CC=N1 NIPZZXUFJPQHNH-UHFFFAOYSA-M 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 20
- 239000000203 mixture Substances 0.000 claims 1
- 235000016709 nutrition Nutrition 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 235000016236 parenteral nutrition Nutrition 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462093586P | 2014-12-18 | 2014-12-18 | |
| US62/093,586 | 2014-12-18 | ||
| PCT/IB2015/059450 WO2016097933A1 (en) | 2014-12-18 | 2015-12-08 | Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017537960A JP2017537960A (ja) | 2017-12-21 |
| JP2017537960A5 true JP2017537960A5 (enExample) | 2019-01-24 |
Family
ID=54979887
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017532168A Pending JP2017537960A (ja) | 2014-12-18 | 2015-12-08 | 肝疾患および胃腸疾患の治療に使用するためのｆｘｒアゴニストとしてのアザビシクロオクタン誘導体 |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US20170368038A1 (enExample) |
| EP (1) | EP3233083A1 (enExample) |
| JP (1) | JP2017537960A (enExample) |
| KR (1) | KR20170095965A (enExample) |
| CN (1) | CN107106555A (enExample) |
| AU (1) | AU2015365481B2 (enExample) |
| BR (1) | BR112017011972A2 (enExample) |
| CA (1) | CA2970866A1 (enExample) |
| CL (1) | CL2017001566A1 (enExample) |
| IL (1) | IL252596A0 (enExample) |
| MX (1) | MX2017008057A (enExample) |
| PH (1) | PH12017501046A1 (enExample) |
| RU (1) | RU2017125365A (enExample) |
| SG (1) | SG11201704340VA (enExample) |
| TN (1) | TN2017000243A1 (enExample) |
| TW (1) | TW201628615A (enExample) |
| WO (1) | WO2016097933A1 (enExample) |
Families Citing this family (56)
| 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 |
| WO2016161003A1 (en) | 2015-03-31 | 2016-10-06 | Enanta Phamraceuticals, Inc. | Bile acid derivatives as fxr/tgr5 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 |
| US10080742B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2017189652A1 (en) | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | 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 |
| WO2017201152A1 (en) | 2016-05-18 | 2017-11-23 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| WO2017201155A1 (en) | 2016-05-18 | 2017-11-23 | Enanta Pharmaceuticals, Inc. | lSOXAZOLE DERIVATIVES AS FXR AGONISTS AND METHODS OF USE THEREOF |
| 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. |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | Gilead Sciences, Inc. | Substituted tert-butyl-3-(2-chloro-phenyl)-3-hydroxyazetidine-1-carboxylate compounds |
| 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 |
| US11091482B2 (en) | 2016-08-23 | 2021-08-17 | Ardelyx, Inc. | Isoxazolyl-carbonyloxy azabicyclo[3.2.1]octanyl compounds as FXR activators |
| EP3504205B1 (en) * | 2016-08-23 | 2021-08-04 | Ardelyx, Inc. | Hormone receptor modulators for treating metabolic conditions and disorders |
| KR102218498B1 (ko) * | 2016-09-14 | 2021-02-22 | 노파르티스 아게 | Fxr 작용제들의 조합물 |
| WO2018067704A1 (en) | 2016-10-04 | 2018-04-12 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as fxr agonists and methods of use thereof |
| EP3522883A1 (en) * | 2016-10-05 | 2019-08-14 | Novartis AG | Combination compositions comprising fxr agonists for treating or preventing a fibrotic,cirrhotic disease or disorder |
| 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 |
| CN110461328A (zh) | 2017-03-28 | 2019-11-15 | 吉利德科学公司 | 治疗肝疾病的治疗组合 |
| JP6886074B2 (ja) | 2017-04-12 | 2021-06-16 | イルドン ファーマシューティカル カンパニー リミテッド | 核受容体の効能剤であるイソオキサゾール誘導体及びその用途 |
| US11352358B2 (en) * | 2017-07-06 | 2022-06-07 | Xuanzhu Biopharmaceutical Co., Ltd. | FXR agonist |
| MA50242A (fr) | 2017-09-14 | 2020-07-22 | Ardelyx Inc | Modulateurs du récepteur hormonal pour le traitement d'états et de troubles métaboliques mutagènes et fibrotiques |
| CN111511731B (zh) | 2017-11-01 | 2023-05-23 | 百时美施贵宝公司 | 作为法尼醇x受体调节剂的烯烃化合物 |
| WO2019089667A1 (en) * | 2017-11-01 | 2019-05-09 | Bristol-Myers Squibb Company | Bridged bicyclic compounds as farnesoid x receptor modulators |
| CA3081424A1 (en) | 2017-11-01 | 2019-05-09 | Bristol-Myers Squibb Company | Spirocyclic compounds as farnesoid x receptor modulators |
| WO2019089665A1 (en) | 2017-11-01 | 2019-05-09 | Bristol-Myers Squibb Company | Alkene spirocyclic compounds as farnesoid x receptor modulators |
| EP3704107B1 (en) | 2017-11-01 | 2023-04-12 | Bristol-Myers Squibb Company | Multicyclic compounds as farnesoid x receptor modulators |
| US10689391B2 (en) | 2017-12-12 | 2020-06-23 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
| JP7243959B2 (ja) | 2017-12-22 | 2023-03-22 | シチュアン ケルン－バイオテック バイオファーマシューティカル カンパニー リミテッド | イソオキサゾール誘導体、その製造方法、及びその使用 |
| 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 |
| CA3094167A1 (en) | 2018-03-22 | 2019-09-26 | Viking Therapeutics, Inc. | Crystalline forms and methods of producing crystalline forms of a compound |
| CN110357876B (zh) * | 2018-04-10 | 2022-06-28 | 浙江海正药业股份有限公司 | 氮杂双环辛烷类衍生物及其制备方法和用途 |
| CN110357875B (zh) * | 2018-04-10 | 2022-06-21 | 浙江海正药业股份有限公司 | 氮杂双环辛烷类衍生物、其制备方法及其在医药上的用途 |
| CN112334467B (zh) * | 2018-06-26 | 2023-06-20 | 轩竹生物科技股份有限公司 | Fxr受体激动剂 |
| WO2020117962A1 (en) | 2018-12-05 | 2020-06-11 | Viking Therapeutics, Inc. | Compositions for the treatment of fibrosis and inflammation |
| EP4360632B1 (en) | 2019-01-15 | 2025-10-29 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
| EP3919489A4 (en) * | 2019-01-31 | 2022-10-12 | The National Institutes of Pharmaceutical R&D Co., Ltd | AROMATIC RING OR HETEROAROMATIC RING COMPOUNDS, PROCESS FOR THEIR PRODUCTION AND MEDICAL USE |
| BR112021015930A2 (pt) | 2019-02-15 | 2021-10-05 | Bristol-Myers Squibb Company | Compostos de amida substituídos úteis como moduladores de receptor farnesoide x |
| AR118050A1 (es) | 2019-02-15 | 2021-09-15 | Bristol Myers Squibb Co | Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x |
| KR102905880B1 (ko) | 2019-02-15 | 2025-12-29 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 치환된 비시클릭 화합물 |
| CN113727973B (zh) | 2019-02-15 | 2025-08-29 | 百时美施贵宝公司 | 可用作类法尼醇x受体调节剂的取代酰胺化合物 |
| US11524005B2 (en) | 2019-02-19 | 2022-12-13 | Gilead Sciences, Inc. | Solid forms of FXR agonists |
| CN111825701B (zh) * | 2019-04-19 | 2023-12-08 | 正大天晴药业集团股份有限公司 | 含苯并噻唑的三环类fxr调节剂化合物 |
| 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 |
| CN114728955A (zh) * | 2019-11-29 | 2022-07-08 | 广东东阳光药业有限公司 | Tropifexor的新晶型及其制备方法 |
| CN114728954B (zh) * | 2019-11-29 | 2023-10-17 | 广东东阳光药业股份有限公司 | Tropifexor的新晶型及其制备方法 |
| US20230060715A1 (en) | 2020-01-15 | 2023-03-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of fxr agonists for treating an infection by hepatitis d virus |
| WO2021252392A1 (en) * | 2020-06-09 | 2021-12-16 | Viking Therapeutics, Inc. | Compositions and methods for the treatment of liver disorders |
| JP7599014B2 (ja) * | 2020-06-30 | 2024-12-12 | オクヴィルク，ゼレン | グアニル酸シクラーゼｃ（ｇｕｃｙ２ｃ）アゴニストおよび短鎖脂肪酸またはそのプロドラッグの組み合わせを含む医薬組成物 |
| US20240100125A1 (en) | 2021-01-14 | 2024-03-28 | Enyo Pharma | Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection |
| CN113292555B (zh) * | 2021-04-28 | 2022-03-18 | 武汉纽瑞斯医药科技有限公司 | 一种Tropifexor的制备方法 |
| CN117320722A (zh) | 2021-04-28 | 2023-12-29 | 埃尼奥制药公司 | 使用fxr激动剂作为联合治疗强烈增强tlr3激动剂的作用 |
| CN116987062A (zh) * | 2023-08-03 | 2023-11-03 | 中国热带农业科学院分析测试中心 | 一种氨基酸键联槟榔碱衍生物的制备方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009511450A (ja) * | 2005-10-07 | 2009-03-19 | ノバルティス アクチエンゲゼルシャフト | ニロチニブとファルネシルトランスフェラーゼ阻害剤の組合せ |
| EP2655368A1 (en) * | 2010-12-20 | 2013-10-30 | Irm Llc | Compositions and methods for modulating farnesoid x receptors |
| CU24152B1 (es) * | 2010-12-20 | 2016-02-29 | Irm Llc | 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr |
| EP2545964A1 (en) * | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
-
2015
- 2015-12-08 KR KR1020177019415A patent/KR20170095965A/ko not_active Withdrawn
- 2015-12-08 CN CN201580068503.5A patent/CN107106555A/zh active Pending
- 2015-12-08 TN TN2017000243A patent/TN2017000243A1/en unknown
- 2015-12-08 RU RU2017125365A patent/RU2017125365A/ru not_active Application Discontinuation
- 2015-12-08 CA CA2970866A patent/CA2970866A1/en not_active Abandoned
- 2015-12-08 WO PCT/IB2015/059450 patent/WO2016097933A1/en not_active Ceased
- 2015-12-08 BR BR112017011972A patent/BR112017011972A2/pt not_active Application Discontinuation
- 2015-12-08 EP EP15813923.8A patent/EP3233083A1/en not_active Withdrawn
- 2015-12-08 US US15/534,324 patent/US20170368038A1/en not_active Abandoned
- 2015-12-08 AU AU2015365481A patent/AU2015365481B2/en not_active Ceased
- 2015-12-08 JP JP2017532168A patent/JP2017537960A/ja active Pending
- 2015-12-08 SG SG11201704340VA patent/SG11201704340VA/en unknown
- 2015-12-08 MX MX2017008057A patent/MX2017008057A/es unknown
- 2015-12-17 TW TW104142545A patent/TW201628615A/zh unknown
-
2017
- 2017-06-01 IL IL252596A patent/IL252596A0/en unknown
- 2017-06-06 PH PH12017501046A patent/PH12017501046A1/en unknown
- 2017-06-16 CL CL2017001566A patent/CL2017001566A1/es unknown
-
2018
- 2018-09-20 US US16/137,360 patent/US20190083473A1/en not_active Abandoned
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