CU20130082A7 - 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr - Google Patents

1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr

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Publication number
CU20130082A7
CU20130082A7 CUP2013000082A CU20130082A CU20130082A7 CU 20130082 A7 CU20130082 A7 CU 20130082A7 CU P2013000082 A CUP2013000082 A CU P2013000082A CU 20130082 A CU20130082 A CU 20130082A CU 20130082 A7 CU20130082 A7 CU 20130082A7
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CU
Cuba
Prior art keywords
azabiciclo
octano
oxazol
fxr modulators
fxr
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Application number
CUP2013000082A
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English (en)
Other versions
CU24152B1 (es
Inventor
David C Tully
Paul Vincent Rucker
Phillip B Alper
Daniel Mutnick
Donatella Chianelli
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Irm Llc
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Publication date
Application filed by Irm Llc filed Critical Irm Llc
Publication of CU20130082A7 publication Critical patent/CU20130082A7/es
Publication of CU24152B1 publication Critical patent/CU24152B1/es

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    • A61K31/435Heterocyclic 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
    • A61K31/468-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
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    • A61K31/47Quinolines; Isoquinolines
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    • A61K31/4965Non-condensed pyrazines
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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Abstract

La presente invención se refiere a compuestos de la fórmula (I), un estereisómero, enantiómero, una sal farmacéuticamente aceptable o un conjugado de aminoácidos del mismo; en donde las variables son como se definen en la presente, y sus composiciones farmacéuticas, que son útiles como moduladores de la actividad de los receptores X Fernesoides ( FXR).
CU20130082A 2010-12-20 2011-10-30 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr CU24152B1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201061425189P 2010-12-20 2010-12-20
US201161554297P 2011-11-01 2011-11-01
PCT/US2011/062724 WO2012087519A1 (en) 2010-12-20 2011-11-30 Compositions and methods for modulating fxr

Publications (2)

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CU20130082A7 true CU20130082A7 (es) 2013-10-29
CU24152B1 CU24152B1 (es) 2016-02-29

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US (2) US9150568B2 (es)
EP (1) EP2655370B1 (es)
JP (1) JP5740483B2 (es)
KR (1) KR101626046B1 (es)
CN (1) CN103443099B (es)
AP (1) AP3414A (es)
AR (1) AR084425A1 (es)
AU (1) AU2011345233B2 (es)
BR (1) BR112013015452B1 (es)
CA (1) CA2819825C (es)
CL (1) CL2013001677A1 (es)
CO (1) CO6801729A2 (es)
CR (1) CR20130307A (es)
CU (1) CU24152B1 (es)
CY (1) CY1119530T1 (es)
DK (1) DK2655370T3 (es)
EA (1) EA025569B1 (es)
ES (1) ES2645728T3 (es)
GT (1) GT201300159A (es)
HR (1) HRP20171615T1 (es)
HU (1) HUE034150T2 (es)
IL (1) IL226853A (es)
JO (1) JO3297B1 (es)
LT (1) LT2655370T (es)
MA (1) MA34767B1 (es)
MX (1) MX338845B (es)
MY (1) MY163216A (es)
NZ (1) NZ613234A (es)
PE (1) PE20140207A1 (es)
PL (1) PL2655370T3 (es)
PT (1) PT2655370T (es)
RS (1) RS56335B1 (es)
SG (1) SG191046A1 (es)
SI (1) SI2655370T1 (es)
TW (1) TWI427078B (es)
UY (1) UY33815A (es)
WO (1) WO2012087519A1 (es)
ZA (1) ZA201304044B (es)

Families Citing this family (103)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130261108A1 (en) * 2010-12-20 2013-10-03 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
EA026393B1 (ru) 2012-05-22 2017-04-28 Дженентек, Инк. N-замещенные бензамиды и их применение в лечении боли
CN103007081B (zh) * 2012-11-27 2013-12-04 鞠法红 一种治疗非酒精性脂肪肝的中药组合物
EP2964230A4 (en) 2013-03-07 2016-10-26 Califia Bio Inc KINASEHEMMER WITH MIXED ABSTRACT AND TREATMENT PROCESS THEREWITH
HUE039155T2 (hu) * 2013-11-05 2018-12-28 Novartis Ag Készítmények és eljárások farnezoid X receptorok modulálására
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
EP3233083A1 (en) * 2014-12-18 2017-10-25 Novartis AG Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases
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
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
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
CN108602811B (zh) * 2016-02-01 2021-11-16 轩竹生物科技有限公司 Fxr受体激动剂
BR112018016208A2 (pt) * 2016-02-08 2018-12-18 Redx Pharma Plc compostos heterocíclicos, em particular derivados 2-oxo-4,4,5,5,6,6,7,7-octahidrobenzoxazol, e seus usos como compostos antibacterianos
JP6986022B2 (ja) 2016-02-22 2021-12-22 ノバルティス アーゲー Fxrアゴニストを使用するための方法
CA3014733A1 (en) * 2016-02-22 2017-08-31 Novartis Ag Methods for using fxr agonists
JP7053478B2 (ja) 2016-02-22 2022-04-12 ノバルティス アーゲー Fxrアゴニストを使用するための方法
US10080743B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
WO2017189651A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
US10080741B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
WO2017201152A1 (en) * 2016-05-18 2017-11-23 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
US10149835B2 (en) 2016-05-18 2018-12-11 Elmore Patent Law Group, P.C. Isoxazole derivatives as FXR agonists and methods of use thereof
JP6678779B2 (ja) 2016-06-13 2020-04-08 ギリアード サイエンシーズ, インコーポレイテッド Fxr(nr1h4)調節化合物
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
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
JP7093341B2 (ja) * 2016-08-23 2022-06-29 アルデリックス, インコーポレイテッド 代謝異常状態及び代謝障害を治療するためのホルモン受容体調節薬
EP3486242B1 (en) 2016-08-31 2021-12-08 Jiangsu Hengrui Medicine Co., Ltd. Oxopicolinamide derivative, preparation method therefor and pharmaceutical use thereof
JOP20190040A1 (ar) * 2016-09-14 2019-03-10 Novartis Ag توليفة من ناهضات fxr
WO2018051229A1 (en) * 2016-09-14 2018-03-22 Novartis Ag Novel regimes of fxr agonists
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
US10450306B2 (en) 2016-10-04 2019-10-22 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
WO2018081285A1 (en) * 2016-10-26 2018-05-03 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
WO2018153933A1 (en) 2017-02-21 2018-08-30 Genfit Combination of a ppar agonist with a fxr agonist
EP4122464A1 (en) 2017-03-28 2023-01-25 Gilead Sciences, Inc. Therapeutic combinations for treating liver diseases
WO2018190643A1 (en) * 2017-04-12 2018-10-18 Il Dong Pharmaceutical Co., Ltd. An isoxazole derivatives as nuclear receptor agonists and used thereof
CA3059869C (en) 2017-04-12 2022-01-04 Il Dong Pharmaceutical Co., Ltd. Isoxazole derivatives as nuclear receptor agonists and uses thereof
CN109265471B (zh) * 2017-06-30 2021-06-04 轩竹生物科技有限公司 Fxr受体激动剂
CN112876467B (zh) * 2017-07-06 2023-06-16 轩竹生物科技股份有限公司 Fxr受体激动剂
CN109320517B (zh) * 2017-07-31 2021-08-17 轩竹生物科技有限公司 Fxr受体激动剂
AR114930A1 (es) * 2017-09-12 2020-11-11 Novartis Ag Composición farmacéutica
MA50242A (fr) * 2017-09-14 2020-07-22 Ardelyx Inc Modulateurs du récepteur hormonal pour le traitement d'états et de troubles métaboliques mutagènes et fibrotiques
KR20200081434A (ko) 2017-11-01 2020-07-07 브리스톨-마이어스 스큅 컴퍼니 파르네소이드 x 수용체 조정제로서의 가교된 비시클릭 화합물
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
KR20200081436A (ko) 2017-11-01 2020-07-07 브리스톨-마이어스 스큅 컴퍼니 파르네소이드 x 수용체 조정제로서의 알켄 화합물
US11078198B2 (en) * 2017-11-01 2021-08-03 Bristol-Myers Squibb Company Spirocyclic 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
WO2019106550A1 (en) * 2017-11-30 2019-06-06 Novartis Ag Fxr agonists for the treatment of liver diseases
US10689391B2 (en) 2017-12-12 2020-06-23 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
KR20200102415A (ko) 2017-12-22 2020-08-31 쓰촨 케룬-바이오테크 바이오파마수티컬 컴퍼니 리미티드 이소옥사졸 유도체, 그 제조 방법 및 그 용도
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
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
KR20210015849A (ko) 2018-05-31 2021-02-10 노파르티스 아게 트로피펙소르 및 세니크리비록을 포함하는 조합물
TWI707683B (zh) 2018-06-13 2020-10-21 美商輝瑞股份有限公司 Glp-1受體促效劑及其用途
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
WO2020011146A1 (zh) * 2018-07-11 2020-01-16 中国医药研究开发中心有限公司 1,2,4-噁二唑类化合物及其制备方法和医药用途
BR112021000964A2 (pt) 2018-07-25 2021-04-20 Novartis Ag inibidores do inflamassoma de nlrp3
US11339153B2 (en) * 2018-08-08 2022-05-24 Inorbit Therapeutics Ab Compounds useful in modulating the farnesoid X receptor and methods of making and using the same
WO2020044266A1 (en) 2018-08-31 2020-03-05 Pfizer Inc. Combinations for treatment of nash/nafld and related diseases
EA202191566A1 (ru) 2019-01-15 2021-11-01 Джилид Сайенсиз, Инк. Соединения, модулирующие fxr (nr1h4)
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
AR118050A1 (es) 2019-02-15 2021-09-15 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x
EP3927683A1 (en) 2019-02-19 2021-12-29 Gilead Sciences, Inc. Solid forms of fxr agonists
JP2022524820A (ja) 2019-03-13 2022-05-10 ノバルティス アーゲー 医薬組成物
KR20220003558A (ko) * 2019-04-19 2022-01-10 상하이 인스티튜트 오브 마테리아 메디카 차이니즈 아카데미 오브 싸이언시즈 Fxr 소분자 작용제 및 이의 제조 방법과 용도
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
CN111825667B (zh) * 2019-04-19 2023-07-25 中国科学院上海药物研究所 Fxr小分子激动剂及其制备方法和用途
WO2020231917A1 (en) 2019-05-13 2020-11-19 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
AR119731A1 (es) 2019-05-17 2022-01-05 Novartis Ag Inhibidores del inflamasoma nlrp3
CA3140972A1 (en) 2019-05-20 2020-11-26 Pfizer Inc. Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases
MX2022000742A (es) 2019-07-18 2022-02-14 Enyo Pharma Metodo para disminuir los efectos adversos del interferon.
TW202114671A (zh) 2019-07-23 2021-04-16 瑞士商諾華公司 包含fxr促效劑之治療
TW202114672A (zh) 2019-07-23 2021-04-16 瑞士商諾華公司 使用fxr促效劑的肝臟疾病之組合治療
WO2021044351A1 (en) 2019-09-06 2021-03-11 Novartis Ag Methods of treating liver disease using lta4h inhibitors
EP4031137A1 (en) 2019-09-19 2022-07-27 Novartis AG Treatment comprising fxr agonists
US20220331341A1 (en) 2019-09-30 2022-10-20 Novartis Ag Treatment comprising the use of fxr agonists
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
CN114728954B (zh) * 2019-11-29 2023-10-17 广东东阳光药业股份有限公司 Tropifexor的新晶型及其制备方法
AU2020402177A1 (en) 2019-12-10 2022-06-16 Pfizer Inc. Solid forms of 2-((4-((s)-2-(5-chloropyridin-2-yl)-2-methylbenzo(d) (1,3)dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-benzo(d) imidazole-6-carboxylic acid, 1,3-dihydroxy-2-(hydroxymethyl)propan-2-amine salt
US20230055657A1 (en) 2019-12-20 2023-02-23 Novartis Ag Combination treatment of liver diseases using integrin inhibitors
US20230105984A1 (en) 2019-12-23 2023-04-06 Svetlana Marukian Compositions and methods for the treatment of liver diseases and disorders
US20230060715A1 (en) 2020-01-15 2023-03-02 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of fxr agonists for treating an infection by hepatitis d virus
TWI823072B (zh) 2020-03-27 2023-11-21 美商輝瑞股份有限公司 以2-〔(4-{6-〔(4-氰基-2-氟苄基)氧基〕吡啶-2-基}哌啶-1-基)甲基〕-1-〔(2s)-氧雜環丁烷-2-基甲基〕-1h-苯並咪唑-6-甲酸或其藥學上的鹽治療第2型糖尿病或肥胖症或體重過重
WO2021233461A1 (zh) * 2020-05-22 2021-11-25 苏州晶云药物科技股份有限公司 苯并噻唑类化合物的新晶型及其制备方法
JP2023530645A (ja) * 2020-06-09 2023-07-19 バイキング・セラピューティクス・インコーポレイテッド 肝障害を処置するための組成物及び方法
EP4211171A2 (en) 2020-09-10 2023-07-19 Precirix N.V. Antibody fragment against fap
CN114315830A (zh) * 2020-09-30 2022-04-12 中国科学院上海药物研究所 Fxr小分子激动剂及其制备方法和用途
US20240100125A1 (en) 2021-01-14 2024-03-28 Enyo Pharma Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
CN113024552B (zh) * 2021-03-26 2022-08-05 厦门市博瑞来医药科技有限公司 一类新型非甾体fxr激动剂的合成及其应用
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
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
WO2023031741A1 (en) 2021-08-31 2023-03-09 Pfizer Inc. Solid forms of 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid, 1,3-dihydroxy-2-(hydroxymethyl)propan-2-amine salt
EP4245365A1 (en) * 2022-03-16 2023-09-20 Cascade Pharmaceuticals, Inc. A fxr small molecule agonist, the preparation and use thereof
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
WO2023213801A1 (en) 2022-05-02 2023-11-09 Precirix N.V. Pre-targeting
WO2023228023A1 (en) 2022-05-23 2023-11-30 Pfizer Inc. Treatment of type 2 diabetes or weight management control with 2-((4-((s)-2-(5-chloropyridin-2-yl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-benzo[d]imidazole-6-carboxylic acid or a pharmaceutically salt thereof
WO2024005586A1 (ko) * 2022-06-30 2024-01-04 일동제약(주) 아이속사졸 유도체 또는 이의 염의 신규한 결정형
US20240067627A1 (en) 2022-08-03 2024-02-29 Novartis Ag Nlrp3 inflammasome inhibitors

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
JPH0672123B2 (ja) 1986-08-21 1994-09-14 セントラル硝子株式会社 トリフルオロメチル基を有するシクロヘキサンカルボン酸の製造方法
US7319109B2 (en) 2002-11-22 2008-01-15 Smith Kline Beecham Corporation Farnesoid X receptor agonists
CA2514733A1 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
US7932248B2 (en) 2005-11-09 2011-04-26 Memory Pharmaceuticals Corporation 1H-indazoles, benzothiazoles, 1,2-benzoisoxazoles, 1,2-benzoisothiazoles, and chromones and preparation and uses thereof
AU2006321349A1 (en) 2005-12-02 2007-06-07 Pfizer Limited Spirocyclic quinazoline derivatives as PDE7 inhibitors
CN101374834B (zh) * 2006-02-03 2011-12-14 伊莱利利公司 用于调节fxr的化合物和方法
JP2007230909A (ja) * 2006-03-01 2007-09-13 Univ Of Tokyo 置換イソキサゾール誘導体
ATE460403T1 (de) 2006-05-24 2010-03-15 Lilly Co Eli Verbindungen und verfahren zur modulierung von fx-rezeptoren
EP1894924A1 (en) * 2006-08-29 2008-03-05 Phenex Pharmaceuticals AG Heterocyclic FXR binding compounds
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
TW200906823A (en) * 2007-07-16 2009-02-16 Lilly Co Eli Compounds and methods for modulating FXR
AU2008317057B8 (en) 2007-10-22 2014-02-13 Merck Sharp & Dohme Corp. Bicyclic Heterocycle Derivatives and their use as modulators of the activity of GPR119
EP2289883A1 (en) * 2009-08-19 2011-03-02 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
CA2778684A1 (en) 2009-10-29 2011-05-05 Schering Corporation Bridged bicyclic piperidine derivatives and methods of use thereof
US20130261108A1 (en) 2010-12-20 2013-10-03 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
US20140039007A1 (en) 2010-12-20 2014-02-06 David C. Tully Compositions and methods for modulating farnesoid x receptors

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