RU2017125365A - Производные азабициклооктана в качестве агонистов fxr для применения при лечении заболеваний печени и желудочно-кишечных заболеваний - Google Patents
Производные азабициклооктана в качестве агонистов fxr для применения при лечении заболеваний печени и желудочно-кишечных заболеваний Download PDFInfo
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- RU2017125365A RU2017125365A RU2017125365A RU2017125365A RU2017125365A RU 2017125365 A RU2017125365 A RU 2017125365A RU 2017125365 A RU2017125365 A RU 2017125365A RU 2017125365 A RU2017125365 A RU 2017125365A RU 2017125365 A RU2017125365 A RU 2017125365A
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- 208000019423 liver disease Diseases 0.000 title claims 3
- 208000018522 Gastrointestinal disease Diseases 0.000 title 1
- 229940121360 farnesoid X receptor (fxr) agonists Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 41
- -1 {5-cyclopropyl-3- [2- (trifluoromethoxy) phenyl] -1,2-oxazol-4-yl} methoxy Chemical group 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 9
- 102100038495 Bile acid receptor Human genes 0.000 claims 5
- 101000603876 Homo sapiens Bile acid receptor Proteins 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 230000001575 pathological effect Effects 0.000 claims 5
- 206010025476 Malabsorption Diseases 0.000 claims 4
- 208000004155 Malabsorption Syndromes Diseases 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 239000003613 bile acid Substances 0.000 claims 4
- 210000004185 liver Anatomy 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims 3
- 206010009887 colitis Diseases 0.000 claims 3
- NIPZZXUFJPQHNH-UHFFFAOYSA-N pyrazine-2-carboxylic acid Chemical compound OC(=O)C1=CN=CC=N1 NIPZZXUFJPQHNH-UHFFFAOYSA-N 0.000 claims 3
- 206010056979 Colitis microscopic Diseases 0.000 claims 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims 2
- 206010057969 Reflux gastritis Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 210000000013 bile duct Anatomy 0.000 claims 2
- 238000010322 bone marrow transplantation Methods 0.000 claims 2
- 208000008609 collagenous colitis Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 208000024908 graft versus host disease Diseases 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 208000004341 lymphocytic colitis Diseases 0.000 claims 2
- 235000016236 parenteral nutrition Nutrition 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 238000011476 stem cell transplantation Methods 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- VYLOOGHLKSNNEK-JWTNVVGKSA-N 2-[(1R,5S)-3-[[5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl]methoxy]-8-azabicyclo[3.2.1]octan-8-yl]-4-fluoro-1,3-benzothiazole-6-carboxylic acid Chemical compound C([C@]1(CC[C@@](C2)(N1C=1SC3=CC(=CC(F)=C3N=1)C(O)=O)[H])[H])C2OCC1=C(C2CC2)ON=C1C1=CC=CC=C1OC(F)(F)F VYLOOGHLKSNNEK-JWTNVVGKSA-N 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 208000025086 undetermined colitis Diseases 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4748—Quinolines; Isoquinolines forming part of bridged ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Transplantation (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Saccharide Compounds (AREA)
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 |
|---|---|
| RU2017125365A true RU2017125365A (ru) | 2019-01-21 |
| RU2017125365A3 RU2017125365A3 (enExample) | 2019-07-17 |
Family
ID=54979887
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2017125365A RU2017125365A (ru) | 2014-12-18 | 2015-12-08 | Производные азабициклооктана в качестве агонистов fxr для применения при лечении заболеваний печени и желудочно-кишечных заболеваний |
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 |
| NZ735126A (en) | 2015-03-31 | 2022-10-28 | Enanta Pharm Inc | Bile acid derivatives as fxr/tgr5 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 |
| 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 |
| WO2017201150A1 (en) | 2016-05-18 | 2017-11-23 | 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 |
| US10149835B2 (en) | 2016-05-18 | 2018-12-11 | Elmore Patent Law Group, P.C. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| SI3730487T1 (sl) | 2016-06-13 | 2022-08-31 | Gilead Sciences, Inc. | Azetidinski derivati kot modulatorji FXR (NR1H4) |
| 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 |
| WO2018039384A1 (en) | 2016-08-23 | 2018-03-01 | Ardelyx, Inc. | Isoxazolyl-carbonyloxy azabicyclo[3.2.1]octanyl compounds as fxr activators |
| EP3954684A1 (en) | 2016-08-23 | 2022-02-16 | Ardelyx, Inc. | Process for the preparation of hormone receptor modulators for treating metabolic conditions and disorders |
| JOP20190040A1 (ar) * | 2016-09-14 | 2019-03-10 | Novartis Ag | توليفة من ناهضات fxr |
| CA3039124A1 (en) | 2016-10-04 | 2018-04-12 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as fxr agonists and methods of use thereof |
| JP2019530696A (ja) * | 2016-10-05 | 2019-10-24 | ノバルティス アーゲー | 線維性、硬変性の疾患もしくは障害を治療または予防するためのｆｘｒアゴニストを含む組合せ組成物 |
| 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 |
| RS62711B1 (sr) | 2017-04-12 | 2022-01-31 | Il Dong Pharma | Derivati izoksazola kao agonisti nuklearnih receptora i njihova upotreba |
| CN110944997B (zh) * | 2017-07-06 | 2021-04-09 | 轩竹生物科技有限公司 | Fxr受体激动剂 |
| EP3681881B1 (en) * | 2017-09-14 | 2022-11-02 | Ardelyx, Inc. | Hormone receptor modulators for treating metabolic mutagenic and fibrotic conditions and disorders |
| US10730863B2 (en) | 2017-11-01 | 2020-08-04 | Bristol-Myers Squibb Company | Bridged bicyclic compounds as farnesoid X receptor modulators |
| US11370785B2 (en) | 2017-11-01 | 2022-06-28 | Bristol-Myers Squibb Company | Multicyclic compounds as farnesoid X receptor modulators |
| KR102732404B1 (ko) | 2017-11-01 | 2024-11-19 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 알켄 화합물 |
| ES2933184T3 (es) | 2017-11-01 | 2023-02-02 | Bristol Myers Squibb Co | Compuestos espirocíclicos como moduladores del receptor farnesoide X |
| CN111630051B (zh) | 2017-11-01 | 2023-12-26 | 百时美施贵宝公司 | 作为法尼醇x受体调节剂的烯烃螺环化合物 |
| WO2019118571A1 (en) | 2017-12-12 | 2019-06-20 | 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 |
| EA202091979A1 (ru) | 2018-03-22 | 2021-06-22 | Вайкинг Терапьютикс, Инк. | Кристаллические формы и способы получения кристаллических форм соединения |
| 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 |
| 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 |
| 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 |
| US12102646B2 (en) | 2018-12-05 | 2024-10-01 | Viking Therapeutics, Inc. | Compositions for the treatment of fibrosis and inflammation |
| US11225473B2 (en) | 2019-01-15 | 2022-01-18 | Gilead Sciences, Inc. | FXR (NR1H4) modulating compounds |
| CA3128416A1 (en) * | 2019-01-31 | 2020-08-06 | The National Institutes of Pharmaceutical R&D Co., Ltd. | Aromatic ring or heteroaromatic ring compounds, preparation method therefor and medical use thereof |
| EP3924337A1 (en) | 2019-02-15 | 2021-12-22 | Bristol-Myers Squibb Company | Substituted bicyclic compounds as farnesoid x receptor modulators |
| SG11202108794RA (en) | 2019-02-15 | 2021-09-29 | Bristol Myers Squibb Co | Substituted amide compounds useful as farnesoid x receptor modulators |
| AR118050A1 (es) | 2019-02-15 | 2021-09-15 | Bristol Myers Squibb Co | Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x |
| CN113677659B (zh) | 2019-02-15 | 2024-09-06 | 百时美施贵宝公司 | 可用作类法尼醇x受体调节剂的经取代的酰胺化合物 |
| EP3927683A1 (en) | 2019-02-19 | 2021-12-29 | 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 |
| US11555032B2 (en) | 2019-05-13 | 2023-01-17 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2021009332A1 (en) | 2019-07-18 | 2021-01-21 | Enyo Pharma | Method for decreasing adverse-effects of interferon |
| WO2021104021A1 (zh) * | 2019-11-29 | 2021-06-03 | 广东东阳光药业有限公司 | Tropifexor的新晶型及其制备方法 |
| WO2021104022A1 (zh) * | 2019-11-29 | 2021-06-03 | 广东东阳光药业有限公司 | Tropifexor的新晶型及其制备方法 |
| CA3159163A1 (en) | 2020-01-15 | 2021-07-22 | Raphael Darteil | 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 |
| WO2022002369A1 (en) * | 2020-06-30 | 2022-01-06 | Ocvirk Soeren | Pharmaceutical composition comprising a combination of a guanylate cyclase c (gucy2c) agonist and a short-chain fatty acid or prodrug thereof |
| CA3204800A1 (en) | 2021-01-14 | 2022-07-21 | Raphael Darteil | 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 |
| US20240216364A1 (en) | 2021-04-28 | 2024-07-04 | Enyo Pharma | Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment |
| 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)
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|---|---|---|---|---|
| US20080255171A1 (en) * | 2005-10-07 | 2008-10-16 | Manley Paul W | Combination of Nilotinib with Farnesyl Transferase Inhibitors |
| 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 |
| WO2012087520A1 (en) * | 2010-12-20 | 2012-06-28 | Irm Llc | Compositions and methods for modulating farnesoid x receptors |
| EP2545964A1 (en) * | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
-
2015
- 2015-12-08 BR BR112017011972A patent/BR112017011972A2/pt not_active Application Discontinuation
- 2015-12-08 JP JP2017532168A patent/JP2017537960A/ja active Pending
- 2015-12-08 TN TN2017000243A patent/TN2017000243A1/en unknown
- 2015-12-08 CN CN201580068503.5A patent/CN107106555A/zh active Pending
- 2015-12-08 WO PCT/IB2015/059450 patent/WO2016097933A1/en not_active Ceased
- 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 RU RU2017125365A patent/RU2017125365A/ru not_active Application Discontinuation
- 2015-12-08 KR KR1020177019415A patent/KR20170095965A/ko not_active Withdrawn
- 2015-12-08 AU AU2015365481A patent/AU2015365481B2/en not_active Ceased
- 2015-12-08 SG SG11201704340VA patent/SG11201704340VA/en unknown
- 2015-12-08 MX MX2017008057A patent/MX2017008057A/es unknown
- 2015-12-08 CA CA2970866A patent/CA2970866A1/en not_active Abandoned
- 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
Also Published As
| Publication number | Publication date |
|---|---|
| PH12017501046A1 (en) | 2017-11-27 |
| CL2017001566A1 (es) | 2018-03-23 |
| CN107106555A (zh) | 2017-08-29 |
| BR112017011972A2 (pt) | 2017-12-26 |
| IL252596A0 (en) | 2017-07-31 |
| MX2017008057A (es) | 2017-09-28 |
| US20190083473A1 (en) | 2019-03-21 |
| SG11201704340VA (en) | 2017-07-28 |
| TN2017000243A1 (en) | 2018-10-19 |
| WO2016097933A1 (en) | 2016-06-23 |
| RU2017125365A3 (enExample) | 2019-07-17 |
| CA2970866A1 (en) | 2016-06-23 |
| AU2015365481A1 (en) | 2017-06-22 |
| US20170368038A1 (en) | 2017-12-28 |
| AU2015365481B2 (en) | 2018-08-09 |
| JP2017537960A (ja) | 2017-12-21 |
| EP3233083A1 (en) | 2017-10-25 |
| KR20170095965A (ko) | 2017-08-23 |
| TW201628615A (zh) | 2016-08-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20191211 |