ES2529226T3 - Nuevos componentes que se unen a FXR (NR1H4) y modulan su actividad - Google Patents
Nuevos componentes que se unen a FXR (NR1H4) y modulan su actividad Download PDFInfo
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- ES2529226T3 ES2529226T3 ES10747171.6T ES10747171T ES2529226T3 ES 2529226 T3 ES2529226 T3 ES 2529226T3 ES 10747171 T ES10747171 T ES 10747171T ES 2529226 T3 ES2529226 T3 ES 2529226T3
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- 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
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- 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
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- 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
- A61K31/4192—1,2,3-Triazoles
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- 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
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- 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
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- 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
- A61K31/423—Oxazoles condensed with carbocyclic rings
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- 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
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- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
- C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
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- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
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- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
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- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Abstract
Un compuesto de acuerdo coo la siguiente fórmula (1), un enantiómero. dlastereómero, tautómero. o sal fannacéuticamente aceptable del mismo**Fórmula** en donde R es seleccionado del grupo que consiste de COORe" CONR7Ra. tetrazolllo o H. con Re independientemente seleccionado del grupo que consiste de H, o alquilo C1-6, y R7 y R8 Independientemente uno del otro seleccionado del grupo que consiste de H. alquilo C1-6, haloalquilo C1-6, alqulleno C1-6-R9. SO2 alquilo-C1-6 , donde R9 es seleccionado del grupo que consiste de COOH. OH. o SO3,H; A es seleccionado del grupo que consiste de lenilo, plrldilo, pirazolilo. Indolilo, tienllo. benzotlenilo. indazolllo, benzisoxazolilo, benzofuranllo, benzotriazolilo, furanllo, benzotiazolllo. tiazolilo. cada uno opcionalmente sustituido con uno o dos grupos independientemente seleccionados del grupo que consiste de OH, alquilo C1-6, ciCloalquilo C3-6, o halógeno; A es seleccionado del grupo que consiste de tenllo, pirldilo. tiazolllo, tiofenilo. plrlmidilo cada uno opcionalmente sustituido con uno o dos gnJpos independientemente seleccionados del gnJpo que consiste de alquilo C1-6. halógeno o CF3; o en donde R es seleccionado del grupo que consiste de COOA6. CONR7R8, tetrazolllo o H, con R6. R7 Y R8 independientemente seleccionados del grupo que consiste de H Y alquilo C1-6 ; A es seleccionado del grupo que consiste de fenilo, piridilo, indolilo. tienilo, benzotienilo, Indazolilo. benzisoxazolilo, benzofuranilo. benzotrlazolilo, furanilo. benzotlazolilo, tiazolilo. cada uno opcionalmente sustituido con uno o dos grupos independientemente seleccionados del grupo que consiste de OH. alquilo C1-6. cicloalquilo C3-6. Q es seleccionado del grupo que consiste de lenilo, piridilo. tiazolilo, tiofenilo, pirimidilo. cada uno opcionalmente sustituido con uno o dos grupos independientemente seleccionados del grupo que consiste de alquilo C1-6. halógeno y CF3;**Fórmula**
Description
Claims (1)
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Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US23511709P | 2009-08-19 | 2009-08-19 | |
EP09010676 | 2009-08-19 | ||
EP09010676A EP2289883A1 (en) | 2009-08-19 | 2009-08-19 | Novel FXR (NR1H4) binding and activity modulating compounds |
US235117P | 2009-08-19 | ||
PCT/EP2010/005093 WO2011020615A1 (en) | 2009-08-19 | 2010-08-19 | Novel fxr (nr1h4 ) binding and activity modulating compounds |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2529226T3 true ES2529226T3 (es) | 2015-02-18 |
Family
ID=41137753
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES10747171.6T Active ES2529226T3 (es) | 2009-08-19 | 2010-08-19 | Nuevos componentes que se unen a FXR (NR1H4) y modulan su actividad |
Country Status (31)
Country | Link |
---|---|
US (1) | US8952042B2 (es) |
EP (2) | EP2289883A1 (es) |
JP (1) | JP5692934B2 (es) |
KR (1) | KR101712466B1 (es) |
CN (1) | CN102548974B (es) |
AU (1) | AU2010285175B2 (es) |
BR (1) | BR112012003554A2 (es) |
CA (1) | CA2771445C (es) |
CL (1) | CL2012000369A1 (es) |
DK (1) | DK2467366T3 (es) |
EA (1) | EA024083B1 (es) |
ES (1) | ES2529226T3 (es) |
GE (1) | GEP20146109B (es) |
HK (1) | HK1172325A1 (es) |
HR (1) | HRP20150159T1 (es) |
IL (1) | IL217676A (es) |
IN (1) | IN2012DN00790A (es) |
MA (1) | MA33575B1 (es) |
ME (1) | ME02047B (es) |
MX (1) | MX2012002119A (es) |
MY (1) | MY163109A (es) |
NZ (1) | NZ598328A (es) |
PL (1) | PL2467366T3 (es) |
PT (1) | PT2467366E (es) |
RS (1) | RS53812B1 (es) |
SG (1) | SG178336A1 (es) |
SI (1) | SI2467366T1 (es) |
SM (1) | SMT201500029B (es) |
UA (1) | UA108209C2 (es) |
WO (1) | WO2011020615A1 (es) |
ZA (1) | ZA201200730B (es) |
Families Citing this family (76)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
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 |
WO2013037482A1 (en) | 2011-09-15 | 2013-03-21 | Phenex Pharmaceuticals Ag | Farnesoid x receptor agonists for cancer treatment and prevention |
WO2014001278A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
WO2014001282A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
MX357504B (es) | 2012-06-26 | 2018-07-12 | Saniona Aps | Derivado de feniltriazol y su uso para modular complejo del receptor gabaa. |
WO2014001280A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
WO2014001279A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
JO3215B1 (ar) | 2012-08-09 | 2018-03-08 | Phenex Pharmaceuticals Ag | حلقات غير متجانسة بها 5 ذرات تحتوي على النيتروجين بها استبدال بكربوكساميد أو سلفوناميد كمعدلات لمستقبل نووي غير محمي RORy |
CN102976946A (zh) * | 2012-12-13 | 2013-03-20 | 烟台泰和新材料股份有限公司 | 合成间苯二甲酸二甲酯的方法 |
CN103232378B (zh) * | 2013-04-27 | 2015-11-18 | 国家海洋局第三海洋研究所 | 一种含6-溴吲哚满二酮的荔枝螺提取物及制备方法与其抗癌应用 |
HUE052856T2 (hu) | 2013-09-11 | 2021-05-28 | Inst Nat Sante Rech Med | Eljárások és gyógyászati készítmények Hepatitis B vírus fertõzés kezelésére |
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 |
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 |
EP3253382B1 (en) | 2015-02-06 | 2021-11-17 | Intercept Pharmaceuticals, Inc. | Pharmaceutical compositions for combination therapy |
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 |
WO2016161003A1 (en) | 2015-03-31 | 2016-10-06 | Enanta Phamraceuticals, Inc. | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
TN2017000426A1 (en) | 2015-04-07 | 2019-04-12 | Intercept Pharmaceuticals Inc | Pharmaceutical compositions for combination therapy |
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 |
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 |
CN109152840A (zh) | 2016-03-28 | 2019-01-04 | 英特塞普特医药品公司 | 通过结合fxr激动剂和arb获得的药物 |
WO2017189663A1 (en) | 2016-04-26 | 2017-11-02 | 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 |
US10080742B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
US10149835B2 (en) | 2016-05-18 | 2018-12-11 | Elmore Patent Law Group, P.C. | Isoxazole derivatives as FXR agonists and methods of use thereof |
US10138228B2 (en) | 2016-05-18 | 2018-11-27 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use therof |
US10144729B2 (en) | 2016-05-18 | 2018-12-04 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
AR108711A1 (es) | 2016-06-13 | 2018-09-19 | Gilead Sciences Inc | Compuestos moduladores de fxr (nr1h4) |
CA2968836A1 (en) | 2016-06-13 | 2017-12-13 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
EP3730487B1 (en) * | 2016-06-13 | 2022-04-27 | Gilead Sciences, Inc. | Azetidine derivatives as fxr (nr1h4) modulators |
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 |
US11091482B2 (en) | 2016-08-23 | 2021-08-17 | Ardelyx, Inc. | Isoxazolyl-carbonyloxy azabicyclo[3.2.1]octanyl compounds as FXR activators |
JP6915050B2 (ja) * | 2016-09-14 | 2021-08-04 | ノバルティス アーゲー | Fxrアゴニストの新規のレジーム |
KR20180036522A (ko) * | 2016-09-30 | 2018-04-09 | (주)나노믹스 | 스틸벤 유도체 및 그 제조 방법 |
BR112019006651A2 (pt) | 2016-10-04 | 2019-07-02 | Enanta Pharm Inc | análogos de isoxazol como agonistas de fxr e métodos de uso do mesmo |
CN107973790A (zh) * | 2016-10-22 | 2018-05-01 | 合帕吉恩治疗公司 | 杂环fxr调节剂 |
US10597391B2 (en) | 2016-10-26 | 2020-03-24 | Enanta Pharmaceuticals, Inc. | Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof |
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 |
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 |
AU2018223146B2 (en) | 2017-02-21 | 2023-12-21 | Genfit | Combination of a PPAR agonist with a FXR agonist |
WO2018183193A1 (en) | 2017-03-28 | 2018-10-04 | Gilead Sciences, Inc. | Therapeutic combinations for treating liver diseases |
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 |
MX2019011844A (es) | 2017-04-07 | 2021-11-30 | Enanta Pharm Inc | Proceso para la preparación de derivados de ácidos biliares de sulfonil carbamato. |
WO2018190643A1 (en) * | 2017-04-12 | 2018-10-18 | Il Dong Pharmaceutical Co., Ltd. | An isoxazole derivatives as nuclear receptor agonists and used thereof |
RS62711B1 (sr) * | 2017-04-12 | 2022-01-31 | Il Dong Pharma | Derivati izoksazola kao agonisti nuklearnih receptora i njihova upotreba |
KR20200010483A (ko) | 2017-05-26 | 2020-01-30 | 메드샤인 디스커버리 아이엔씨. | Fxr 수용체 작용제로서 락탐 화합물 |
CA3068928C (en) | 2017-07-06 | 2022-05-31 | Xuanzhu (Hainan) Biopharmaceutical Co., Ltd. | Fxr agonist |
CN111655680B (zh) * | 2017-09-14 | 2024-03-05 | 阿德利克斯股份有限公司 | 用于治疗代谢突变和纤维化病状及病症的激素受体调节剂 |
JP7264905B2 (ja) | 2017-11-01 | 2023-04-25 | 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多環化合物 |
KR20200081436A (ko) | 2017-11-01 | 2020-07-07 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 알켄 화합물 |
MX2020004102A (es) | 2017-11-01 | 2020-07-24 | Bristol Myers Squibb Co | Compuestos espirociclicos de alquenos como moduladores del receptor farnesoide x. |
US10689391B2 (en) | 2017-12-12 | 2020-06-23 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
CN110128432B (zh) * | 2018-02-02 | 2021-03-02 | 广东东阳光药业有限公司 | 含氮三环化合物及其在药物中的应用 |
US10829486B2 (en) | 2018-02-14 | 2020-11-10 | Enanta Pharmacueticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
AU2019263176A1 (en) * | 2018-04-30 | 2020-10-08 | The Trustees Of Indiana University | Compounds for modulating DDAH and ADMA levels, as well as methods of using thereof to treat disease |
BR102019014802A2 (pt) | 2018-07-20 | 2020-02-04 | Boehringer Ingelheim Int | difluorometil-fenil triazóis |
MX2021001513A (es) | 2018-08-08 | 2021-06-15 | Inorbit Therapeutics Ab | Compuestos utiles en la modulacion del receptor x farnesoide y metodos de preparacion y utilizacion de los mismos. |
KR20210114457A (ko) | 2019-01-15 | 2021-09-23 | 길리애드 사이언시즈, 인코포레이티드 | Fxr (nr1h4) 조정 화합물 |
CN112955448B (zh) | 2019-01-31 | 2023-02-03 | 中国医药研究开发中心有限公司 | 芳环或芳杂环类化合物及其制备方法和医药用途 |
CA3233305A1 (en) | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
WO2020231917A1 (en) | 2019-05-13 | 2020-11-19 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
JP2022536060A (ja) | 2019-05-30 | 2022-08-12 | インターセプト ファーマシューティカルズ, インコーポレイテッド | 胆汁鬱滞性肝疾患の処置で使用するためのfxrアゴニストおよびフィブラートを含む医薬組成物 |
JP2022540699A (ja) | 2019-07-18 | 2022-09-16 | ウエヌイグレックオ・ファーマ | インターフェロンの有害作用を減少させる方法 |
MX2022008062A (es) | 2020-01-15 | 2022-07-27 | Inst Nat Sante Rech Med | Uso del agonista fxr para el tratamiento de una infeccion por el virus de la hepatitis d. |
US11478533B2 (en) | 2020-04-27 | 2022-10-25 | Novo Nordisk A/S | Semaglutide for use in medicine |
EP4277622A1 (en) | 2021-01-14 | 2023-11-22 | ENYO Pharma | Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection |
WO2022229302A1 (en) | 2021-04-28 | 2022-11-03 | Enyo Pharma | Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment |
WO2023090858A1 (ko) * | 2021-11-17 | 2023-05-25 | 일동제약(주) | 아이속사졸 유도체의 제조 방법 및 그의 중간체 |
WO2023090859A1 (ko) * | 2021-11-17 | 2023-05-25 | 일동제약(주) | 아이속사졸 유도체의 제조 방법 및 그의 신규한 중간체 |
WO2024005586A1 (ko) * | 2022-06-30 | 2024-01-04 | 일동제약(주) | 아이속사졸 유도체 또는 이의 염의 신규한 결정형 |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2326850T3 (es) | 1998-12-23 | 2009-10-20 | Glaxo Group Limited | Ensayos para ligandos de receptores nucleares. |
EP1285914B1 (en) | 2001-08-13 | 2007-12-19 | PheneX Pharmaceuticals AG | Nr1h4 nuclear receptor binding compounds |
US20050107475A1 (en) | 2002-03-21 | 2005-05-19 | Jones Stacey A. | Methods of using farnesoid x receptor (frx) agonists |
WO2004048349A1 (en) | 2002-11-22 | 2004-06-10 | Smithkline Beecham Corporation | Farnesoid x receptor agonists |
WO2004087076A2 (en) | 2003-03-31 | 2004-10-14 | The Rockefeller University | Methods for inhibiting adipogenesis and for treating type 2 diabetes |
US7705028B2 (en) | 2005-12-19 | 2010-04-27 | Glaxosmithkline Llc | Farnesoid X receptor agonists |
JP5301286B2 (ja) | 2006-02-03 | 2013-09-25 | イーライ リリー アンド カンパニー | Fx受容体を調節するための化合物及び方法 |
DK2029547T3 (da) | 2006-05-24 | 2010-07-26 | Lilly Co Eli | FXR-agonister |
WO2007140174A2 (en) | 2006-05-24 | 2007-12-06 | Eli Lilly And Company | Compounds and methods for modulating fxr |
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 |
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, |
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 |
AU2008270784A1 (en) | 2007-07-02 | 2009-01-08 | Glaxosmithkline Llc | Farnesoid X receptor agonists |
TW200906823A (en) | 2007-07-16 | 2009-02-16 | Lilly Co Eli | Compounds and methods for modulating FXR |
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