IL229944A - Fxr active modulator compounds and fxr (4h1nr) - Google Patents
Fxr active modulator compounds and fxr (4h1nr)Info
- Publication number
- IL229944A IL229944A IL229944A IL22994413A IL229944A IL 229944 A IL229944 A IL 229944A IL 229944 A IL229944 A IL 229944A IL 22994413 A IL22994413 A IL 22994413A IL 229944 A IL229944 A IL 229944A
- Authority
- IL
- Israel
- Prior art keywords
- group
- fxr
- compound
- liver
- compounds
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/435—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
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
-
- 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
- A61P1/16—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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Gastroenterology & Hepatology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161507153P | 2011-07-13 | 2011-07-13 | |
| EP11005722A EP2545964A1 (en) | 2011-07-13 | 2011-07-13 | Novel FXR (NR1H4) binding and activity modulating compounds |
| PCT/EP2012/002941 WO2013007387A1 (en) | 2011-07-13 | 2012-07-12 | Novel fxr (nr1h4) binding and activity modulating compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL229944A true IL229944A (en) | 2017-07-31 |
Family
ID=44513243
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL229944A IL229944A (en) | 2011-07-13 | 2013-12-17 | Fxr active modulator compounds and fxr (4h1nr) |
Country Status (31)
| Country | Link |
|---|---|
| US (5) | US9139539B2 (enExample) |
| EP (6) | EP2545964A1 (enExample) |
| JP (2) | JP5986633B2 (enExample) |
| KR (4) | KR101766323B1 (enExample) |
| CN (2) | CN107252424B (enExample) |
| AR (1) | AR087127A1 (enExample) |
| AU (4) | AU2012283387C1 (enExample) |
| BR (3) | BR122019026062B1 (enExample) |
| CA (1) | CA2839357C (enExample) |
| CY (1) | CY1117453T1 (enExample) |
| DK (2) | DK3246070T3 (enExample) |
| EA (1) | EA024843B1 (enExample) |
| ES (3) | ES2569718T3 (enExample) |
| FI (1) | FI3246070T3 (enExample) |
| HR (2) | HRP20160442T1 (enExample) |
| HU (2) | HUE066734T2 (enExample) |
| IL (1) | IL229944A (enExample) |
| LT (1) | LT3246070T (enExample) |
| ME (1) | ME02434B (enExample) |
| MX (2) | MX368371B (enExample) |
| MY (1) | MY161158A (enExample) |
| PH (1) | PH12014500124A1 (enExample) |
| PL (3) | PL3246070T3 (enExample) |
| PT (2) | PT2987532T (enExample) |
| RS (1) | RS54786B1 (enExample) |
| SI (3) | SI3246070T1 (enExample) |
| SM (1) | SMT201600169B (enExample) |
| TW (1) | TWI439455B (enExample) |
| UY (1) | UY34196A (enExample) |
| WO (1) | WO2013007387A1 (enExample) |
| ZA (1) | ZA201309521B (enExample) |
Families Citing this family (92)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI625121B (zh) | 2009-07-13 | 2018-06-01 | 基利科學股份有限公司 | 調節細胞凋亡信號之激酶的抑制劑 |
| IL253437A0 (en) * | 2011-07-13 | 2017-09-28 | Gilead Sciences Inc | New compounds modulate fxr (nr1h4) activity and bind |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| MX377523B (es) | 2013-09-11 | 2025-03-10 | Inst Nat Sante Rech Med | Metodos y composiciones farmaceuticas para el tratamiento de la infeccion por el virus de la hepatitis b. |
| US10238636B2 (en) | 2014-09-24 | 2019-03-26 | Gilead Sciences, Inc. | Methods of treating liver disease |
| EP3006939A1 (en) | 2014-10-06 | 2016-04-13 | Gilead Sciences, Inc. | Histidine-rich Glycoprotein as a marker for hepatic Farnesoid X receptor activation |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| EP3034499A1 (en) | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Novel FXR (NR1H4) modulating compounds |
| EP3034501A1 (en) | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Hydroxy containing FXR (NR1H4) modulating compounds |
| SG11201704340VA (en) * | 2014-12-18 | 2017-07-28 | Novartis Ag | Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases |
| MA41252A (fr) * | 2014-12-23 | 2017-10-31 | Gilead Sciences Inc | Formes solides d'un inhibiteur d'ask 1 |
| US9586933B2 (en) | 2014-12-23 | 2017-03-07 | Gilead Sciences, Inc. | Processes for preparing ASK1 inhibitors |
| TWI698430B (zh) | 2015-02-13 | 2020-07-11 | 南北兄弟藥業投資有限公司 | 三環化合物及其在藥物中的應用 |
| RU2712099C2 (ru) | 2015-03-31 | 2020-01-24 | Энанта Фармасьютикалс, Инк. | Производные желчных кислот в качестве агонистов fxr/tgr5 и способы их применения |
| ES2734713T3 (es) | 2015-07-06 | 2019-12-11 | Gilead Sciences Inc | Moduladores Cot y métodos de utilización de los mismos |
| CN106995416A (zh) * | 2016-01-26 | 2017-08-01 | 上海翰森生物医药科技有限公司 | Fxr激动剂及其制备方法和应用 |
| WO2017128896A1 (zh) * | 2016-01-26 | 2017-08-03 | 江苏豪森药业集团有限公司 | Fxr激动剂及其制备方法和应用 |
| TW201741307A (zh) * | 2016-02-22 | 2017-12-01 | 艾洛斯生物製藥公司 | Ｆｘｒ調節劑及其使用方法 |
| JP2019510752A (ja) | 2016-03-04 | 2019-04-18 | ギリアード サイエンシーズ， インコーポレイテッド | オートタキシン阻害剤の組成物及び合剤 |
| JP2019513737A (ja) | 2016-04-08 | 2019-05-30 | ギリアード サイエンシーズ， インコーポレイテッド | がん、炎症性疾患および自己免疫疾患を処置するための組成物および方法 |
| US10080742B2 (en) | 2016-04-26 | 2018-09-25 | 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 |
| US10080743B2 (en) | 2016-04-26 | 2018-09-25 | 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 |
| US10149835B2 (en) | 2016-05-18 | 2018-12-11 | Elmore Patent Law Group, P.C. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| NZ748641A (en) | 2016-06-13 | 2020-04-24 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| AR108711A1 (es) * | 2016-06-13 | 2018-09-19 | Gilead Sciences Inc | Compuestos moduladores de fxr (nr1h4) |
| CA2968836C (en) * | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (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 |
| CN106237332A (zh) * | 2016-08-11 | 2016-12-21 | 河南大学 | 核受体fxr在肝癌干细胞靶向治疗中的应用 |
| CA3039124A1 (en) | 2016-10-04 | 2018-04-12 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as fxr agonists and methods of use thereof |
| CN107973790A (zh) * | 2016-10-22 | 2018-05-01 | 合帕吉恩治疗公司 | 杂环fxr调节剂 |
| WO2018081285A1 (en) * | 2016-10-26 | 2018-05-03 | Enanta Pharmaceuticals, Inc. | Urea-containing isoxazole derivatives as fxr agonists and methods of use thereof |
| CA3042398A1 (en) * | 2016-11-11 | 2018-05-17 | Gilead Sciences, Inc. | Methods of treating liver disease |
| CN106588804B (zh) * | 2016-12-09 | 2018-11-09 | 都创(上海)医药科技有限公司 | 一种作为类法尼醇x受体(fxr)的化合物的制备方法 |
| CN108218852A (zh) * | 2016-12-15 | 2018-06-29 | 宁波百纳西药业有限公司 | 一种螺环化合物、其制备方法、组合物及用途 |
| CN109071468B (zh) * | 2017-01-20 | 2022-09-02 | 四川科伦博泰生物医药股份有限公司 | 一种杂环化合物及其制备方法和用途 |
| JP7618384B2 (ja) | 2017-02-21 | 2025-01-21 | ジェンフィ | Ｐｐａｒアゴニストとｆｘｒアゴニストとの組合せ |
| WO2018169742A1 (en) | 2017-03-14 | 2018-09-20 | Gilead Sciences, Inc. | Apoptosis signal-regulating kinase inhibtor |
| ES2982801T3 (es) * | 2017-03-28 | 2024-10-17 | Gilead Sciences Inc | Combinaciones terapéuticas para el tratamiento de las enfermedades hepáticas |
| JP2020515564A (ja) | 2017-03-30 | 2020-05-28 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | エピソーマルウイルスの持続性及び発現を低下させるための方法及び医薬組成物 |
| MX388300B (es) | 2017-04-07 | 2025-03-19 | Enanta Pharm Inc | Proceso para la preparación de derivados de ácidos biliares de sulfonil carbamato |
| RU2741306C1 (ru) | 2017-04-12 | 2021-01-25 | Ил Дон Фармасьютикал Ко., Лтд. | Производные изоксазола в качестве агонистов ядерных рецепторов и их применение |
| EP3609496A1 (en) * | 2017-04-12 | 2020-02-19 | Gilead Sciences, Inc. | Methods of treating liver disease |
| WO2018231851A1 (en) | 2017-06-13 | 2018-12-20 | Gilead Sciences, Inc. | Methods of treating liver fibrosis |
| CN111182904A (zh) | 2017-10-06 | 2020-05-19 | 吉利德科学公司 | 包含acc抑制剂的组合治疗 |
| KR102731925B1 (ko) | 2017-11-01 | 2024-11-18 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 멀티시클릭 화합물 |
| US11286252B2 (en) | 2017-11-01 | 2022-03-29 | Bristol-Myers Squibb Company | Alkene spirocyclic compounds as farnesoid X receptor modulators |
| CN111278821B (zh) | 2017-11-01 | 2023-10-03 | 百时美施贵宝公司 | 作为法尼醇x受体调节剂的螺环化合物 |
| US11168079B2 (en) | 2017-11-01 | 2021-11-09 | Bristol-Myers Squibb Company | Alkene compounds as farnesoid x receptor modulators |
| JP7212693B2 (ja) | 2017-11-01 | 2023-01-25 | ブリストル－マイヤーズ スクイブ カンパニー | ファルネソイドｘ受容体モジュレーターとしての架橋二環化合物 |
| US20200340060A1 (en) | 2017-11-13 | 2020-10-29 | Gilead Sciences, Inc. | Compositions and methods for identifying and treating liver diseases and monitoring treatment outcomes |
| 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 |
| WO2019160813A1 (en) | 2018-02-14 | 2019-08-22 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| WO2020029908A1 (zh) * | 2018-08-08 | 2020-02-13 | 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 |
| AU2019319750A1 (en) | 2018-08-08 | 2021-03-04 | Inorbit Therapeutics Ab | Compounds useful in modulating the farnesoid X receptor and methods of making and using the same |
| EP3852748B1 (en) | 2018-09-18 | 2025-09-03 | Eli Lilly and Company | Farnesoid x receptor agonists and uses thereof |
| HU231223B1 (hu) | 2018-09-28 | 2022-01-28 | Richter Gedeon Nyrt. | GABAA A5 receptor modulátor hatású biciklusos vegyületek |
| KR102692309B1 (ko) | 2019-01-15 | 2024-08-07 | 길리애드 사이언시즈, 인코포레이티드 | Fxr (nr1h4) 조정 화합물 |
| US12479816B2 (en) | 2019-02-08 | 2025-11-25 | University of Pittsburgh—of the Commonwealth System of Higher Education | 20-HETE formation inhibitors |
| JP7465883B2 (ja) | 2019-02-15 | 2024-04-11 | ブリストル－マイヤーズ スクイブ カンパニー | ファルネソイドｘ受容体モジュレータとしての置換二環式化合物 |
| US12319676B2 (en) | 2019-02-15 | 2025-06-03 | Bristol-Myers Squibb Company | 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 |
| JP7449300B2 (ja) | 2019-02-15 | 2024-03-13 | ブリストル－マイヤーズ スクイブ カンパニー | ファルネソイドｘ受容体モジュレータとして有用な置換アミド化合物 |
| WO2020172075A1 (en) | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| JP7697885B2 (ja) | 2019-03-11 | 2025-06-24 | ギリアード サイエンシーズ， インコーポレイテッド | 化合物の製剤およびそれらの使用 |
| WO2020231917A1 (en) | 2019-05-13 | 2020-11-19 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| TWI915558B (zh) | 2019-06-14 | 2026-02-21 | 美商基利科學股份有限公司 | Cot 調節劑及其使用方法 |
| WO2021009332A1 (en) | 2019-07-18 | 2021-01-21 | Enyo Pharma | Method for decreasing adverse-effects of interferon |
| US20230105984A1 (en) | 2019-12-23 | 2023-04-06 | Svetlana Marukian | Compositions and methods for the treatment of liver diseases and disorders |
| IL293892A (en) | 2020-01-15 | 2022-08-01 | Inserm Institut National De La Sant? Et De La Rech M?Dicale | Use of fxr agonists for treating an infection by hepatitis d virus |
| CN120227340A (zh) | 2020-03-18 | 2025-07-01 | 伊莱利利公司 | 法尼醇x受体激动剂的制剂 |
| KR20220154801A (ko) * | 2020-03-18 | 2022-11-22 | 메타크린, 인크. | 질환의 치료를 위한 파르네소이드 x 수용체 작용제 |
| JP7664278B2 (ja) | 2020-03-18 | 2025-04-17 | オルガノボ，インク． | ファルネソイドｘ受容体アゴニストの結晶質形態 |
| US12649738B2 (en) | 2020-03-26 | 2026-06-09 | Richter Gedeon Nyrt. | 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine derivatives as GABAA α5 receptor modulators |
| TWI901650B (zh) | 2020-03-26 | 2025-10-21 | 匈牙利商羅特格登公司 | 啶及吡啶并〔３，４－ｃ〕嗒衍生物 |
| CA3175541A1 (en) | 2020-03-30 | 2021-10-07 | Gilead Sciences, Inc. | Solid forms of (s)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1h-1,2,3-triazol-4-yl)2-methyl-1-oxo-1,2- dihydroisoquinolin-5-yl)methyl)))amino)8-chloro-(neopentylamino)quinoline-3-carb onitrile a cot inhibitor compound |
| EP4126862B1 (en) | 2020-04-02 | 2025-05-21 | Gilead Sciences, Inc. | Process for preparing a cot inhibitor compound |
| US11478533B2 (en) | 2020-04-27 | 2022-10-25 | Novo Nordisk A/S | Semaglutide for use in medicine |
| CN114656460B (zh) | 2020-12-22 | 2025-01-10 | 江苏天士力帝益药业有限公司 | 一种新型吡嗪结构fxr激动剂、制备方法及应用 |
| MX2023008365A (es) | 2021-01-14 | 2023-10-04 | Enyo Pharma | Efecto sinérgico de un agonista de fxr e ifn para el tratamiento de infección por hbv. |
| EP4304711A1 (en) | 2021-03-11 | 2024-01-17 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
| ES3061522T3 (en) | 2021-03-29 | 2026-04-06 | Gilead Sciences Inc | Khk inhibitors |
| TW202308629A (zh) | 2021-04-28 | 2023-03-01 | 法商Ｅｎｙｏ製藥公司 | 使用fxr激動劑作為組合治療以增強tlr3激動劑之療效 |
| TW202345826A (zh) | 2021-06-04 | 2023-12-01 | 美商基利科學股份有限公司 | 治療nash之方法 |
| KR20240021883A (ko) | 2021-06-16 | 2024-02-19 | 셀진 코포레이션 | 신경변성 질환의 치료를 위한 카르복실산 기를 포함하는 아제티디닐 화합물 |
| TW202311256A (zh) | 2021-06-18 | 2023-03-16 | 美商基利科學股份有限公司 | 用於治療ｆｘｒ誘發之搔癢之ｉｌ－３１調節劑 |
| WO2023125904A1 (zh) * | 2021-12-30 | 2023-07-06 | 苏州晶云药物科技股份有限公司 | 氮杂环丁基烟酸类化合物的晶型及其制备方法 |
| EP4608506A1 (en) | 2022-10-25 | 2025-09-03 | Assia Chemical Industries Ltd. | Solid state forms of cilofexor salts |
| US20260207538A1 (en) | 2024-12-20 | 2026-07-23 | Gilead Sciences, Inc. | Combinations for liver disease |
Family Cites Families (186)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ193011A (en) | 1979-03-19 | 1983-03-15 | Ici Australia Ltd | Diarylamine derivatives intermediates herbicidal compositions |
| ES2054725T3 (es) | 1987-04-21 | 1994-08-16 | Basf Ag | Heteroaromatos anulares de cinco miembros de p-fenoxi-fenoximetilo. |
| JP3121061B2 (ja) | 1991-10-04 | 2000-12-25 | 塩野義製薬株式会社 | アルコキシイミノアセトアミド類製造用中間体の製造法およびそれに用いる中間体 |
| DE4137940A1 (de) | 1991-11-18 | 1993-05-19 | Basf Ag | 3-isoxazolylphenylverbindungen, ihre herstellung und ihre verwendung |
| US5258551A (en) | 1991-12-18 | 1993-11-02 | Shionogi & Co., Ltd. | Process for producing α-ketoamide derivative |
| WO1994017059A1 (fr) | 1993-01-29 | 1994-08-04 | Nippon Soda Co., Ltd. | Derive heterocyclique |
| WO1994024095A1 (en) | 1993-04-16 | 1994-10-27 | Abbott Laboratories | Immunosuppressive agents |
| IL112721A0 (en) | 1994-03-10 | 1995-05-26 | Zeneca Ltd | Azole derivatives |
| EP0804434A1 (en) | 1994-08-02 | 1997-11-05 | MERCK SHARP & DOHME LTD. | Azetidine, pyrrolidine and piperidine derivatives |
| GB9501865D0 (en) | 1995-01-31 | 1995-03-22 | Merck Sharp & Dohme | Therapeutic agents |
| US5633272A (en) | 1995-02-13 | 1997-05-27 | Talley; John J. | Substituted isoxazoles for the treatment of inflammation |
| DE19536811A1 (de) | 1995-10-02 | 1997-04-03 | Basf Ag | Zwischenprodukte und Verfahren zur Herstellung von substituierten Salicylsäurederivaten als Pflanzenschutzmittel |
| AU1952597A (en) | 1996-02-13 | 1997-09-02 | G.D. Searle & Co. | Combinations, having immunosuppressive effects, containing cyclooxygenase-2 inhibitor and a leukotriene a4 hydrolase inhibitor |
| ES2326850T3 (es) | 1998-12-23 | 2009-10-20 | Glaxo Group Limited | Ensayos para ligandos de receptores nucleares. |
| ATE283860T1 (de) | 1999-06-11 | 2004-12-15 | Allergan Inc | Organosiliciumvebindungen mit der fähigkeit zur modulation von im zellkern lokalisierten hormonrezeptoren |
| US7022725B2 (en) | 2000-11-17 | 2006-04-04 | Takeda Pharmaceutical Company Limited | Isoxazole derivatives |
| US20040105885A1 (en) | 2001-04-17 | 2004-06-03 | Ping Gao | Gelatin capsule exhibiting reduced cross-linking |
| US20040105883A1 (en) | 2001-04-17 | 2004-06-03 | Ping Gao | Pharmaceutical dosage form capable of maintaining stable dissolution profile upon storage |
| US20040131670A1 (en) | 2001-04-17 | 2004-07-08 | Ping Gao | Pellicle-resistant gelatin capsule |
| US20040105884A1 (en) | 2001-04-17 | 2004-06-03 | Ping Gao | Pharmaceutical dosage form comprising a sulfite compound |
| EP1405636A4 (en) | 2001-06-26 | 2009-04-15 | Takeda Pharmaceutical | FUNCTIONAL REGULATOR FOR RETINOID RELATIVE RECEPTOR |
| US20070010562A1 (en) | 2001-08-13 | 2007-01-11 | Ulrike Bauer | Nr1h4 nuclear receptor binding compounds |
| DE60131967D1 (de) | 2001-08-13 | 2008-01-31 | Phenex Pharmaceuticals Ag | Nr1h4-kern-rezeptor-bindende verbindungen |
| WO2003015777A1 (en) | 2001-08-13 | 2003-02-27 | Lion Bioscience Ag | Nr1h4 nuclear receptor binding compounds |
| WO2003080803A2 (en) | 2002-03-21 | 2003-10-02 | Smithkline Beecham Corporation | Methods of using farnesoid x receptor (fxr) agonists |
| US7595311B2 (en) | 2002-05-24 | 2009-09-29 | Exelixis, Inc. | Azepinoindole derivatives as pharmaceutical agents |
| WO2004014881A2 (en) | 2002-08-09 | 2004-02-19 | Astra Zeneca Ab | '1,2,4'oxadiazoles as modulators of metabotropic glutamate receptor-5 |
| AU2003264018A1 (en) | 2002-08-09 | 2004-02-25 | Astrazeneca Ab | Compounds having an activity at metabotropic glutamate receptors |
| CN1691944A (zh) | 2002-08-09 | 2005-11-02 | 阿斯利康(瑞典)有限公司 | 作为代谢型谷氨酸受体－5调节剂的噁二唑 |
| EP1407774A1 (en) | 2002-09-10 | 2004-04-14 | LION Bioscience AG | 2-Amino-4-quinazolinones as LXR nuclear receptor binding compounds |
| AU2003290796A1 (en) | 2002-11-14 | 2004-06-15 | The Scripps Research Institute | Non-steroidal fxr agonists |
| US20050143449A1 (en) | 2002-11-15 | 2005-06-30 | The Salk Institute For Biological Studies | Non-steroidal farnesoid X receptor modulators and methods for the use thereof |
| JP2006515838A (ja) | 2002-11-22 | 2006-06-08 | スミスクライン ビーチャム コーポレーション | ファルネソイドｘ受容体アゴニスト |
| WO2004087076A2 (en) | 2003-03-31 | 2004-10-14 | The Rockefeller University | Methods for inhibiting adipogenesis and for treating type 2 diabetes |
| WO2005077373A2 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Treatment of gastro-esophageal reflux disease (gerd) |
| WO2005077345A1 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Compounds for the treatment of gastro-esophageal reflux disease |
| US7585881B2 (en) | 2004-02-18 | 2009-09-08 | Astrazeneca Ab | Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
| CA2564429A1 (en) | 2004-05-14 | 2005-12-01 | Irm Llc | Compounds and compositions as ppar modulators |
| MY144903A (en) | 2004-06-17 | 2011-11-30 | Novartis Ag | Pyrrolopyridine derivatives and their use as crth2 antagonists |
| JP2008515992A (ja) | 2004-10-13 | 2008-05-15 | ピーティーシー セラピューティクス，インコーポレーテッド | 体細胞変異に起因する疾患の阻止／治療用医薬を製造するための規定化合物の使用 |
| JP2008137894A (ja) | 2005-03-22 | 2008-06-19 | Nippon Kayaku Co Ltd | 新規なアセチレン誘導体 |
| TW200716576A (en) | 2005-06-07 | 2007-05-01 | Shionogi & Co | Heterocyclic derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| WO2007070796A1 (en) | 2005-12-15 | 2007-06-21 | Exelixis, Inc. | Azepinoindole derivatives as pharmaceutical agents |
| ATE526318T1 (de) | 2005-12-19 | 2011-10-15 | Glaxosmithkline Llc | Farnesoid-x-rezeptor-agonisten |
| US7560551B2 (en) | 2006-01-23 | 2009-07-14 | Amgen Inc. | Aurora kinase modulators and method of use |
| ES2452031T3 (es) | 2006-02-03 | 2014-03-31 | Eli Lilly & Company | Compuestos y procedimientos para modular receptores FX |
| CN101395170A (zh) * | 2006-02-14 | 2009-03-25 | 英特塞普特药品公司 | 用于预防或治疗fxr介导的疾病或状态的作为fxr配体的胆汁酸衍生物 |
| EP2007759A4 (en) | 2006-04-17 | 2010-12-22 | Neuromed Pharmaceuticals Ltd | ISOXAZOLE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS |
| CN101448798A (zh) * | 2006-05-24 | 2009-06-03 | 伊莱利利公司 | 用于调节fxr的化合物和方法 |
| WO2007135027A1 (de) | 2006-05-24 | 2007-11-29 | Boehringer Ingelheim International Gmbh | Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind |
| ES2340221T3 (es) * | 2006-05-24 | 2010-05-31 | Eli Lilly And Company | Compuestos y procedimientos para modular fxr. |
| DK2029547T3 (da) | 2006-05-24 | 2010-07-26 | Lilly Co Eli | FXR-agonister |
| DK2040713T3 (da) | 2006-06-27 | 2014-09-29 | Intercept Pharmaceuticals Inc | Galdesyrederivater som fxr-ligander til forebyggelsen eller behandlingen af fxr-medierede sygdomme eller tilstande |
| AU2007269540B2 (en) | 2006-07-05 | 2013-06-27 | Exelixis, Inc. | Methods of using IGF1R and Abl kinase modulators |
| PE20080401A1 (es) | 2006-07-07 | 2008-06-23 | Boehringer Ingelheim Int | DERIVADOS DE HETEROARIL-FENIL SUSTITUIDOS COMO INHIBIDORES DE B-Raf-QUINASAS |
| WO2008013660A2 (en) | 2006-07-07 | 2008-01-31 | Biostratum, Inc. | Inhibitors of advanced glycation end products |
| EP1894924A1 (en) * | 2006-08-29 | 2008-03-05 | Phenex Pharmaceuticals AG | Heterocyclic FXR binding compounds |
| EP1894928A1 (en) | 2006-08-29 | 2008-03-05 | PheneX Pharmaceuticals AG | Heterocyclic fxr binding compounds |
| US8193225B2 (en) | 2006-10-13 | 2012-06-05 | The Board Of Regents Of The University Of Texas System | Isoxazole amides, derivatives and methods of chemical induction of neurogenesis |
| CL2007003035A1 (es) | 2006-10-24 | 2008-05-16 | Smithkline Beechman Corp | Compuestos derivados de isoxazol sustituidos, agonistas de receptores farnesoid x; procedimiento de preparacion; composicion farmaceutica que lo comprende; y uso del compuesto en el tratamiento de la obesidad, diabetes mellitus, fibrosis en organos, |
| US8501933B2 (en) | 2006-11-09 | 2013-08-06 | Roche Palo Alto Llc | Thiazole and oxazole-substituted arylamides as P2X3 and P2X2/3 antagonists |
| EP2121621B1 (en) | 2006-12-08 | 2014-05-07 | Exelixis Patent Company LLC | Lxr and fxr modulators |
| GB0625842D0 (en) | 2006-12-22 | 2007-02-07 | Argenta Discovery Ltd | Indolizine derivatives |
| US20090105251A1 (en) | 2007-01-25 | 2009-04-23 | Benjamin Jones | Renin inhibitors |
| CN101605760B (zh) | 2007-02-09 | 2012-06-20 | 陶氏益农公司 | 将某些取代的硫亚胺氧化为杀虫性磺基肟的方法 |
| US7511149B2 (en) | 2007-02-09 | 2009-03-31 | Dow Agrosciences Llc | Process for the oxidation of certain substituted sulfilimines to insecticidal sulfoximines |
| ZA200905012B (en) | 2007-02-26 | 2010-10-27 | Dow Agrosciences Llc | Process for the preparation of certain substituted sulfimines |
| BRPI0812521A2 (pt) | 2007-06-13 | 2015-06-23 | Glaxosmithkline Llc | Composto, composição farmacêutica, método para o tratamento de doença em um mamífero, processo para a preparação de um composto, e, uso de um composto |
| JP2008308448A (ja) | 2007-06-15 | 2008-12-25 | Sankyo Agro Kk | （３−硫黄原子置換フェニル）へテロアリール誘導体 |
| WO2008155054A1 (en) | 2007-06-20 | 2008-12-24 | F. Hoffmann-La Roche Ag | Farnesoid-x-receptor mutants, and crystallisation thereof |
| BRPI0812851A2 (pt) | 2007-07-02 | 2014-09-30 | Glaxosmithkline Llc | Composto, composição farmacêutica, métodos para o tratamento de uma doença e de uma condição em um indivíduo, processo para preparar um composto, e, uso de um composto |
| CA2692379A1 (en) | 2007-07-02 | 2009-01-08 | Boehringer Ingelheim International Gmbh | Antiproliferative compounds based on 5-membered heterocycles |
| US20090197880A1 (en) | 2007-07-13 | 2009-08-06 | Genelabs Technologies, Inc. | Anti-viral compounds, compositions, and methods of use |
| EA201000051A1 (ru) | 2007-07-13 | 2010-08-30 | ГЛАКСОСМИТКЛАЙН ЭлЭлСи | Противовирусные соединения, композиции и способы использования |
| TW200906823A (en) | 2007-07-16 | 2009-02-16 | Lilly Co Eli | Compounds and methods for modulating FXR |
| CN101790374A (zh) | 2007-08-01 | 2010-07-28 | H.隆德贝克有限公司 | Kcnq钾通道开放剂用于减轻多巴胺能系统受到干扰的障碍或病症的症状或治疗这种障碍或病症的用途 |
| US8188080B2 (en) | 2007-10-17 | 2012-05-29 | Sanford-Burnham Medical Research Institute | VHR protein tyrosine phosphatase inhibitors, compositions and methods of use |
| US20090143451A1 (en) | 2007-11-14 | 2009-06-04 | Andrews William H | Compounds that increase telomerase reverse transcriptase (tert) expression and methods for using the same |
| EP2110374A1 (en) | 2008-04-18 | 2009-10-21 | Merck Sante | Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators |
| US20120015988A1 (en) | 2008-05-13 | 2012-01-19 | Boehringer Ingelheim International Gmbh | Sulfone Compounds Which Modulate The CB2 Receptor |
| US8158636B2 (en) | 2008-05-19 | 2012-04-17 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| WO2009143150A2 (en) | 2008-05-19 | 2009-11-26 | Burnham Institute For Medical Research | Intestinal alkaline phosphatase modulators and uses thereof |
| EP2128158A1 (en) | 2008-05-26 | 2009-12-02 | Phenex Pharmaceuticals AG | Heterocyclic cyclopropyl-substituted FXR binding compounds |
| CN104530052A (zh) | 2008-06-10 | 2015-04-22 | 普莱希科公司 | 用于激酶调节的5h-吡咯[2,3-b]吡嗪衍生物和其适应症 |
| US8822513B2 (en) | 2010-03-01 | 2014-09-02 | Gtx, Inc. | Compounds for treatment of cancer |
| US8252939B2 (en) | 2008-06-23 | 2012-08-28 | Basf Se | Sulfoximinamide compounds for combating animal pests |
| WO2010006096A1 (en) | 2008-07-11 | 2010-01-14 | Smithkline Beecham Corporation | Processes for the preparation of anti-viral compounds and compositions containing them |
| JP2012500848A (ja) | 2008-08-25 | 2012-01-12 | ダウ グローバル テクノロジーズ エルエルシー | イソオキサゾール化合物の製造方法 |
| WO2010033906A2 (en) | 2008-09-19 | 2010-03-25 | President And Fellows Of Harvard College | Efficient induction of pluripotent stem cells using small molecule compounds |
| EP2344459B1 (en) | 2008-09-25 | 2013-12-25 | F. Hoffmann-La Roche AG | 2,3-substituted indazole or 4,5,6,7-tetrahydro-indazoles as fxr modulators against dyslipidemia and related diseases |
| MX2011002793A (es) | 2008-09-25 | 2011-04-05 | Hoffmann La Roche | Derivados de 3-amino-indazol o de 3-amino-4,5,6,7-tetrahidro-indaz ol. |
| JP2012503654A (ja) | 2008-09-26 | 2012-02-09 | ワイス・エルエルシー | １，２，３，６−テトラヒドロアゼピノ［４，５−ｂ］インドール−５−カルボキシレート核内受容体阻害剤 |
| EA022417B1 (ru) | 2008-10-21 | 2015-12-30 | Саймабэй Терапевтикс, Инк. | Арильные агонисты рецептора gpr120 и их применение |
| JP5679997B2 (ja) | 2009-02-04 | 2015-03-04 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤 |
| 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 |
| FR2943059A1 (fr) | 2009-03-16 | 2010-09-17 | Sanofi Aventis | Derives de n-°6-aza-bicyclo°3.2.1!oct-5-yl)-aryl-methyl!- heterobenzamide,leur preparation et leur application en therapeutique |
| US8883832B2 (en) | 2009-07-06 | 2014-11-11 | Aerpio Therapeutics Inc. | Compounds, compositions, and methods for preventing metastasis of cancer cells |
| ES2461618T3 (es) | 2009-07-06 | 2014-05-20 | Basf Se | Compuestos de piridacina para el control de plagas de invertebrados |
| JP2013500246A (ja) | 2009-07-24 | 2013-01-07 | ビーエーエスエフ ソシエタス・ヨーロピア | 無脊椎動物系害虫防除用ピリジン誘導体化合物 |
| US9212177B2 (en) | 2009-08-05 | 2015-12-15 | Versitech Limited | Antiviral compounds and methods of making and using thereof |
| EP2289883A1 (en) | 2009-08-19 | 2011-03-02 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| KR20120081119A (ko) | 2009-09-04 | 2012-07-18 | 잘리커스 파마슈티컬즈 리미티드 | 통증 및 간질 치료를 위한 치환된 헤테로고리 유도체 |
| WO2011047129A1 (en) | 2009-10-15 | 2011-04-21 | Southern Research Institute | Treatment of neurodegenerative diseases, causation of memory enhancement, and assay for screening compounds for such |
| CA2791738C (en) | 2010-03-01 | 2020-06-09 | Gtx, Inc. | Aryl imidazolyl compounds for the treatment of cancer |
| US20130231348A1 (en) | 2010-06-09 | 2013-09-05 | Afraxis, Inc. | 8-(HETEROARYLMETHYL)PYRIDO[2,3-d]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS |
| WO2012058531A2 (en) | 2010-10-29 | 2012-05-03 | North Carolina State University | Modulation of response regulators by imidazole derivatives |
| TWI408128B (zh) | 2010-12-03 | 2013-09-11 | Nat Univ Tsing Hua | 間-三聯苯衍生物及其在有機發光二極體之應用 |
| JP2014500319A (ja) | 2010-12-20 | 2014-01-09 | アイアールエム・リミテッド・ライアビリティ・カンパニー | ファルネソイドｘ受容体を調節するための組成物および方法 |
| WO2012087520A1 (en) | 2010-12-20 | 2012-06-28 | 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 |
| WO2013037482A1 (en) | 2011-09-15 | 2013-03-21 | Phenex Pharmaceuticals Ag | Farnesoid x receptor agonists for cancer treatment and prevention |
| ES2822375T3 (es) | 2012-06-19 | 2021-04-30 | Intercept Pharmaceuticals Inc | Preparación de la forma no cristalina del ácido obeticólico |
| TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代２－氮雜雙環類及其作為食慾素受體調控劑之用途 |
| WO2014181287A1 (en) | 2013-05-09 | 2014-11-13 | Piramal Enterprises Limited | Heterocyclyl compounds and uses thereof |
| CN105377870B (zh) | 2013-05-14 | 2018-04-03 | 英特塞普特医药品公司 | 作为法尼醇x受体调节剂的胆汁酸的11‑羟基衍生物及其氨基酸共轭物 |
| BR112016002268B1 (pt) | 2013-08-01 | 2022-11-01 | The Penn State Research Foundation | Uso de inibidores do receptor x farnesoide |
| MX377523B (es) | 2013-09-11 | 2025-03-10 | Inst Nat Sante Rech Med | Metodos y composiciones farmaceuticas para el tratamiento de la infeccion por el virus de la hepatitis b. |
| US20150082981A1 (en) | 2013-09-20 | 2015-03-26 | E I Du Pont De Nemours And Company | Capture of trifluoromethane using ionic liquids |
| CN104513213A (zh) | 2013-09-28 | 2015-04-15 | 山东亨利医药科技有限责任公司 | Fxr激动剂 |
| WO2015065983A1 (en) | 2013-10-29 | 2015-05-07 | Lumena Pharmaceuticals, Inc. | Bile acid recycling inhibitors for treatment of gastrointestinal infections |
| SG11201603026PA (en) | 2013-11-05 | 2016-05-30 | Novartis Ag | Compositions and methods for modulating farnesoid x receptors |
| WO2015116856A2 (en) | 2014-01-29 | 2015-08-06 | City Of Hope | Farnesoid x receptor antagonists |
| US10077268B2 (en) | 2014-03-13 | 2018-09-18 | Salk Institute For Biological Studies | FXR agonists and methods for making and using |
| JP2017511304A (ja) | 2014-03-13 | 2017-04-20 | ソーク インスティチュート フォー バイオロジカル スタディーズ | フェキサラミン類似体ならびに作製方法および使用方法 |
| CA2942403A1 (en) | 2014-03-13 | 2015-09-17 | Salk Institute For Biological Studies | Fxr agonists and methods for making and using |
| US9879000B2 (en) | 2014-04-14 | 2018-01-30 | Grünenthal GmbH | Heteroaryl substituted heterocyclyl sulfones |
| WO2015162538A1 (en) | 2014-04-21 | 2015-10-29 | Lupin Limited | Heterocyclic compounds as calcium sensing receptor modulators for the treatment of hyperparathyroidism, chronic renal failure and chronic kidney disease |
| WO2015162244A1 (en) | 2014-04-25 | 2015-10-29 | Basf Se | N-acylamidine compounds |
| WO2015165960A1 (en) | 2014-04-30 | 2015-11-05 | Basf Se | N-acylamidine compounds |
| SI3626725T1 (sl) | 2014-05-29 | 2023-04-28 | Bar Pharmaceuticals S.R.L. | Derivati holana za uporabo pri zdravljenju in/ali preprečevanju bolezni, posredovanih s FXR in TGR5/GPBAR1 |
| CN104045635A (zh) | 2014-06-23 | 2014-09-17 | 华东理工大学 | 3,4,5-三取代异恶唑类化合物及其用途 |
| WO2016054560A1 (en) | 2014-10-02 | 2016-04-07 | Flatley Discovery Lab | Isoxazole compounds and methods for the treatment of cystic fibrosis |
| EP3006939A1 (en) | 2014-10-06 | 2016-04-13 | Gilead Sciences, Inc. | Histidine-rich Glycoprotein as a marker for hepatic Farnesoid X receptor activation |
| TWI577070B (zh) | 2014-10-27 | 2017-04-01 | Lg 化學股份有限公司 | 有機電致發光元件 |
| BR112017009657A2 (pt) | 2014-11-06 | 2018-01-23 | Enanta Pharmaceuticals, Inc | análogos de ácidos biliares como agonistas de fxr/tgr5 e métodos de uso dos mesmos |
| CA2968434A1 (en) | 2014-11-21 | 2016-05-26 | Akarna Therapeutics, Ltd. | Fused bicyclic compounds for the treatment of disease |
| WO2016086115A1 (en) | 2014-11-26 | 2016-06-02 | Enanta Pharmaceuticals, Inc. | Tetrazole derivatives of bile acids as fxr/tgr5 agonists and methods of use thereof |
| RU2017121457A (ru) | 2014-11-26 | 2018-12-26 | Энанта Фармасьютикалс, Инк. | Аналоги желчной кислоты в качестве агонистов fxr/tgr5 и способы их применения |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| WO2016086134A1 (en) | 2014-11-26 | 2016-06-02 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| EP3034501A1 (en) | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Hydroxy containing FXR (NR1H4) modulating compounds |
| EP3034499A1 (en) | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Novel FXR (NR1H4) modulating compounds |
| SG11201704340VA (en) | 2014-12-18 | 2017-07-28 | Novartis Ag | Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases |
| MX2017008844A (es) | 2015-01-09 | 2018-03-14 | Gilead Apollo Llc | Terapia de combinacion con inhibidor de acetil-coa carboxilasa (acc) para el tratamiento de enfermedad de higado graso no alcoholico. |
| ES2907461T3 (es) | 2015-01-20 | 2022-04-25 | Boehringer Ingelheim Animal Health Usa Inc | Compuestos antihelmínticos, composiciones y procedimientos de uso de los mismos |
| TWI698430B (zh) | 2015-02-13 | 2020-07-11 | 南北兄弟藥業投資有限公司 | 三環化合物及其在藥物中的應用 |
| US10100285B2 (en) | 2015-04-03 | 2018-10-16 | Propagenix Inc. | Ex vivo proliferation of epithelial cells |
| CN106146483A (zh) | 2015-04-23 | 2016-11-23 | 上海迪诺医药科技有限公司 | 杂环类法尼酯衍生物x受体调节剂 |
| GB201507340D0 (en) | 2015-04-29 | 2015-06-10 | Univ St Andrews | Light emitting devices and compounds |
| ES2550374B1 (es) * | 2015-06-30 | 2016-09-08 | Universidad De La Rioja | Compuestos fotoprotectores análogos de MAA, procedimiento de síntesis y composición que comprende los mismos |
| WO2017011466A1 (en) | 2015-07-13 | 2017-01-19 | Zwiebel Laurence J | Thermal volatilization of orco agonists |
| JP6869231B2 (ja) | 2015-09-11 | 2021-05-12 | プロパジェニクス インコーポレイテッド | ｅｘ ｖｉｖｏでの上皮細胞の増殖 |
| AR106948A1 (es) | 2015-12-04 | 2018-03-07 | Bristol Myers Squibb Co | Agonistas del receptor de apelina y método de uso |
| WO2017097870A1 (de) | 2015-12-11 | 2017-06-15 | Bayer Cropscience Aktiengesellschaft | Substituierte malonsäureamide als insektizide |
| CN106946867B (zh) | 2016-01-06 | 2019-11-12 | 广州市恒诺康医药科技有限公司 | Fxr受体调节剂及其制备方法和用途 |
| EP3190103A1 (en) | 2016-01-08 | 2017-07-12 | Rijksuniversiteit Groningen | Inhibitors of the pd-1/pd-l1 protein/protein interaction |
| EP3400229B1 (en) | 2016-01-10 | 2024-03-06 | Provincial Health Services Authority | 18/19f-labelled compounds which target the prostate specific membrane antigen |
| WO2017122209A2 (en) | 2016-01-12 | 2017-07-20 | Yeda Research And Development Co. Ltd. | NF-kappaB INHIBITORS |
| WO2017128896A1 (zh) | 2016-01-26 | 2017-08-03 | 江苏豪森药业集团有限公司 | Fxr激动剂及其制备方法和应用 |
| CN107021957A (zh) | 2016-02-01 | 2017-08-08 | 山东轩竹医药科技有限公司 | Fxr受体激动剂 |
| CN107021958A (zh) | 2016-02-01 | 2017-08-08 | 山东轩竹医药科技有限公司 | Fxr受体激动剂 |
| CN108602811B (zh) | 2016-02-01 | 2021-11-16 | 轩竹生物科技有限公司 | Fxr受体激动剂 |
| TW201741307A (zh) | 2016-02-22 | 2017-12-01 | 艾洛斯生物製藥公司 | Ｆｘｒ調節劑及其使用方法 |
| CN107224583A (zh) | 2016-03-24 | 2017-10-03 | 中美华世通生物医药科技（武汉）有限公司 | 药物组合物及其用途 |
| US10080743B2 (en) | 2016-04-26 | 2018-09-25 | 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 |
| US10080741B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives 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 |
| US10144729B2 (en) | 2016-05-18 | 2018-12-04 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
| KR102444366B1 (ko) | 2016-06-03 | 2022-09-19 | 케모센트릭스, 인크. | 간 섬유화 치료 방법 |
| NZ748641A (en) | 2016-06-13 | 2020-04-24 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (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 |
| CN116854681B (zh) | 2016-08-23 | 2026-05-26 | 阿德利克斯股份有限公司 | 用于治疗代谢病状和病症的激素受体调节剂 |
| CN108430998B (zh) | 2016-09-28 | 2021-07-09 | 四川科伦博泰生物医药股份有限公司 | 氮杂双环衍生物及其制备方法和用途 |
| WO2018060075A1 (en) | 2016-09-29 | 2018-04-05 | Bayer Cropscience Aktiengesellschaft | 1 -[2-(1 -chlorocyclopropyl)-2-hydroxy-3-(3-phenyl-1,2-oxazol-5-yl)propyl]-1h-imidazole-5-carbonitrile derivatives and related compounds as fungicides for crop protection |
| CA3039124A1 (en) | 2016-10-04 | 2018-04-12 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as fxr agonists and methods of use thereof |
| CN107973790A (zh) | 2016-10-22 | 2018-05-01 | 合帕吉恩治疗公司 | 杂环fxr调节剂 |
| CA3152584C (en) | 2016-11-10 | 2024-02-13 | Galmed Research And Development Ltd. | Treatment for fibrosis |
| CA3042398A1 (en) | 2016-11-11 | 2018-05-17 | Gilead Sciences, Inc. | Methods of treating liver disease |
| CN106588804B (zh) | 2016-12-09 | 2018-11-09 | 都创(上海)医药科技有限公司 | 一种作为类法尼醇x受体(fxr)的化合物的制备方法 |
| CN106632294A (zh) | 2016-12-15 | 2017-05-10 | 宁波百纳西药业有限公司 | 一种螺环化合物及其药物用途 |
| CN106748922B (zh) | 2017-01-12 | 2019-02-01 | 中国药科大学 | 一类新型砜酸衍生物、其制备方法及其作为药物的用途 |
-
2011
- 2011-07-13 EP EP11005722A patent/EP2545964A1/en not_active Withdrawn
-
2012
- 2012-07-02 TW TW101123785A patent/TWI439455B/zh active
- 2012-07-11 AR ARP120102511A patent/AR087127A1/es active IP Right Grant
- 2012-07-12 KR KR1020177000763A patent/KR101766323B1/ko active Active
- 2012-07-12 BR BR122019026062-1A patent/BR122019026062B1/pt active IP Right Grant
- 2012-07-12 BR BR122020008872-9A patent/BR122020008872B1/pt active IP Right Grant
- 2012-07-12 AU AU2012283387A patent/AU2012283387C1/en active Active
- 2012-07-12 EP EP15002478.4A patent/EP2987532B1/en active Active
- 2012-07-12 LT LTEP17000383.4T patent/LT3246070T/lt unknown
- 2012-07-12 WO PCT/EP2012/002941 patent/WO2013007387A1/en not_active Ceased
- 2012-07-12 CN CN201710308892.5A patent/CN107252424B/zh active Active
- 2012-07-12 ES ES12735100.5T patent/ES2569718T3/es active Active
- 2012-07-12 PL PL17000383.4T patent/PL3246070T3/pl unknown
- 2012-07-12 SI SI201232062T patent/SI3246070T1/sl unknown
- 2012-07-12 PH PH1/2014/500124A patent/PH12014500124A1/en unknown
- 2012-07-12 JP JP2014519453A patent/JP5986633B2/ja active Active
- 2012-07-12 KR KR1020187013304A patent/KR101934335B1/ko active Active
- 2012-07-12 HU HUE17000383A patent/HUE066734T2/hu unknown
- 2012-07-12 CA CA2839357A patent/CA2839357C/en active Active
- 2012-07-12 US US14/232,118 patent/US9139539B2/en active Active
- 2012-07-12 ES ES17000383T patent/ES2978166T3/es active Active
- 2012-07-12 HU HUE12735100A patent/HUE027931T2/en unknown
- 2012-07-12 DK DK17000383.4T patent/DK3246070T3/da active
- 2012-07-12 EP EP12735100.5A patent/EP2731676B1/en active Active
- 2012-07-12 RS RS20160266A patent/RS54786B1/sr unknown
- 2012-07-12 PL PL12735100T patent/PL2731676T3/pl unknown
- 2012-07-12 KR KR1020147002937A patent/KR101722410B1/ko active Active
- 2012-07-12 EP EP24164624.9A patent/EP4400503B1/en active Active
- 2012-07-12 EP EP26171268.1A patent/EP4793273A2/en active Pending
- 2012-07-12 DK DK12735100.5T patent/DK2731676T3/en active
- 2012-07-12 SI SI201230535A patent/SI2731676T1/sl unknown
- 2012-07-12 ES ES15002478.4T patent/ES2632492T3/es active Active
- 2012-07-12 CN CN201280033148.4A patent/CN103702719B/zh active Active
- 2012-07-12 PL PL15002478T patent/PL2987532T3/pl unknown
- 2012-07-12 EA EA201391674A patent/EA024843B1/ru unknown
- 2012-07-12 MX MX2014000534A patent/MX368371B/es active IP Right Grant
- 2012-07-12 KR KR1020177021651A patent/KR101859533B1/ko active Active
- 2012-07-12 PT PT150024784T patent/PT2987532T/pt unknown
- 2012-07-12 PT PT170003834T patent/PT3246070T/pt unknown
- 2012-07-12 UY UY0001034196A patent/UY34196A/es active IP Right Grant
- 2012-07-12 ME MEP-2016-81A patent/ME02434B/me unknown
- 2012-07-12 BR BR112014000260-6A patent/BR112014000260B1/pt active IP Right Grant
- 2012-07-12 HR HRP20160442TT patent/HRP20160442T1/hr unknown
- 2012-07-12 HR HRP20240422TT patent/HRP20240422T1/hr unknown
- 2012-07-12 MY MYPI2013004373A patent/MY161158A/en unknown
- 2012-07-12 FI FIEP17000383.4T patent/FI3246070T3/fi active
- 2012-07-12 EP EP17000383.4A patent/EP3246070B1/en active Active
- 2012-07-12 SI SI201230969A patent/SI2987532T1/sl unknown
-
2013
- 2013-12-17 ZA ZA2013/09521A patent/ZA201309521B/en unknown
- 2013-12-17 IL IL229944A patent/IL229944A/en active IP Right Grant
-
2014
- 2014-01-13 MX MX2019011629A patent/MX2019011629A/es unknown
-
2015
- 2015-08-12 US US14/824,971 patent/US9539244B2/en active Active
-
2016
- 2016-04-28 CY CY20161100369T patent/CY1117453T1/el unknown
- 2016-06-10 SM SM201600169T patent/SMT201600169B/it unknown
- 2016-08-05 JP JP2016154511A patent/JP6321097B2/ja active Active
- 2016-11-29 AU AU2016265993A patent/AU2016265993B2/en active Active
- 2016-12-05 US US15/369,521 patent/US9820979B2/en active Active
-
2017
- 2017-10-13 US US15/783,530 patent/US10220027B2/en active Active
-
2018
- 2018-05-22 AU AU2018203613A patent/AU2018203613B2/en active Active
-
2019
- 2019-01-15 US US16/248,178 patent/US10485795B2/en active Active
- 2019-11-04 AU AU2019261667A patent/AU2019261667B2/en active Active
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2018203613B2 (en) | Novel FXR (NR1H4) binding and activity modulating compounds | |
| HK40113314A (en) | Novel fxr (nr1h4) binding and activity modulating compounds | |
| HK1246716A1 (en) | Novel fxr (nr1h4) binding and activity modulating azoles | |
| HK1246716B (en) | Novel fxr (nr1h4) binding and activity modulating azoles | |
| NZ710770B2 (en) | Novel fxr (nr1h4) binding and activity modulating compounds | |
| HK1221680B (en) | Novel fxr (nr1h4) binding and activity modulating compounds | |
| HK1244682B (en) | Novel fxr (nr1h4) binding and activity modulating compounds | |
| HK1192181B (en) | Novel fxr (nr1h4) modulating compounds | |
| NZ620177B2 (en) | Novel fxr (nr1h4) binding and activity modulating compounds |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| KB | Patent renewed | ||
| KB | Patent renewed |