CN107106555A - 氮杂双环辛烷衍生物作为fxr激动剂在治疗肝脏和胃肠疾病中的应用 - Google Patents

氮杂双环辛烷衍生物作为fxr激动剂在治疗肝脏和胃肠疾病中的应用 Download PDF

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Publication number
CN107106555A
CN107106555A CN201580068503.5A CN201580068503A CN107106555A CN 107106555 A CN107106555 A CN 107106555A CN 201580068503 A CN201580068503 A CN 201580068503A CN 107106555 A CN107106555 A CN 107106555A
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compound
formula
azabicyclo
cyclopropyl
methoxy
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M·百德曼
L·B·克里克斯坦
B·拉斐特
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Novartis AG
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Novartis AG
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4748—Quinolines; Isoquinolines forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
CN201580068503.5A 2014-12-18 2015-12-08 氮杂双环辛烷衍生物作为fxr激动剂在治疗肝脏和胃肠疾病中的应用 Pending CN107106555A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462093586P 2014-12-18 2014-12-18
US62/093,586 2014-12-18
PCT/IB2015/059450 WO2016097933A1 (en) 2014-12-18 2015-12-08 Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases

Publications (1)

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CN107106555A true CN107106555A (zh) 2017-08-29

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Country Status (17)

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US (2) US20170368038A1 (https=)
EP (1) EP3233083A1 (https=)
JP (1) JP2017537960A (https=)
KR (1) KR20170095965A (https=)
CN (1) CN107106555A (https=)
AU (1) AU2015365481B2 (https=)
BR (1) BR112017011972A2 (https=)
CA (1) CA2970866A1 (https=)
CL (1) CL2017001566A1 (https=)
IL (1) IL252596A0 (https=)
MX (1) MX2017008057A (https=)
PH (1) PH12017501046A1 (https=)
RU (1) RU2017125365A (https=)
SG (1) SG11201704340VA (https=)
TN (1) TN2017000243A1 (https=)
TW (1) TW201628615A (https=)
WO (1) WO2016097933A1 (https=)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110357875A (zh) * 2018-04-10 2019-10-22 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
CN110357876A (zh) * 2018-04-10 2019-10-22 浙江海正药业股份有限公司 氮杂双环辛烷类衍生物及其制备方法和用途
WO2020001304A1 (zh) * 2018-06-26 2020-01-02 轩竹（海南）医药科技有限公司 Fxr受体激动剂
CN111655680A (zh) * 2017-09-14 2020-09-11 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
CN111825701A (zh) * 2019-04-19 2020-10-27 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
CN113292555A (zh) * 2021-04-28 2021-08-24 武汉纽瑞斯医药科技有限公司 一种Tropifexor的制备方法
CN114728954A (zh) * 2019-11-29 2022-07-08 广东东阳光药业有限公司 Tropifexor的新晶型及其制备方法
CN114728955A (zh) * 2019-11-29 2022-07-08 广东东阳光药业有限公司 Tropifexor的新晶型及其制备方法
CN116987062A (zh) * 2023-08-03 2023-11-03 中国热带农业科学院分析测试中心 一种氨基酸键联槟榔碱衍生物的制备方法

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
WO2016161003A1 (en) 2015-03-31 2016-10-06 Enanta Phamraceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
WO2017189651A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
WO2017189663A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
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
WO2017201155A1 (en) 2016-05-18 2017-11-23 Enanta Pharmaceuticals, Inc. lSOXAZOLE DERIVATIVES AS FXR AGONISTS AND METHODS OF USE THEREOF
CA3252823A1 (en) 2016-06-13 2025-02-25 Gilead Sciences, Inc. Substituted tert-butyl-3-(2-chloro-phenyl)-3-hydroxyazetidine-1-carboxylate compounds
MX385718B (es) 2016-06-13 2025-03-18 Gilead Sciences Inc Compuestos moduladores de fxr (nr1h4).
TW201808283A (zh) 2016-08-05 2018-03-16 廣東東陽光藥業有限公司 含氮三環化合物及其在藥物中的應用
CN116854681A (zh) 2016-08-23 2023-10-10 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
WO2018039384A1 (en) 2016-08-23 2018-03-01 Ardelyx, Inc. Isoxazolyl-carbonyloxy azabicyclo[3.2.1]octanyl compounds as fxr activators
PE20190972A1 (es) * 2016-09-14 2019-07-09 Novartis Ag Combinacion de agonistas de fxr
US10450306B2 (en) 2016-10-04 2019-10-22 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
RU2019113150A (ru) * 2016-10-05 2020-11-06 Новартис Аг Комбинация композиций, содержащих агонисты fxr, предназначенная для лечения или предупреждения фиброзирующего, цирротического заболевания или нарушения
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
PT3600309T (pt) 2017-03-28 2022-10-03 Gilead Sciences Inc Combinações terapêuticas para o tratamento de doenças hepáticas
PL3612520T3 (pl) 2017-04-12 2022-03-21 Il Dong Pharmaceutical Co., Ltd. Pochodne izoksazolu jako agoniści receptora jądrowego i ich zastosowania
KR102400183B1 (ko) * 2017-07-06 2022-05-18 수안주 바이오파마슈티컬 컴퍼니 리미티드 Fxr 작용제
CN111511731B (zh) 2017-11-01 2023-05-23 百时美施贵宝公司 作为法尼醇x受体调节剂的烯烃化合物
CN111278817B (zh) 2017-11-01 2023-05-16 百时美施贵宝公司 作为法尼醇x受体调节剂的多环化合物
AU2018360575A1 (en) 2017-11-01 2020-06-18 Bristol-Myers Squibb Company Alkene spirocyclic compounds as farnesoid X receptor modulators
KR102731924B1 (ko) 2017-11-01 2024-11-19 브리스톨-마이어스 스큅 컴퍼니 파르네소이드 x 수용체 조정제로서의 스피로시클릭 화합물
PE20201170A1 (es) 2017-11-01 2020-10-28 Bristol Myers Squibb Co Compuestos biciclicos en puente como moduladores del receptor farnesoide x
WO2019118571A1 (en) 2017-12-12 2019-06-20 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
US10829486B2 (en) 2018-02-14 2020-11-10 Enanta Pharmacueticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
ES3053674T3 (en) 2018-03-22 2026-01-23 Viking Therapeutics Inc Crystalline forms and methods of producing crystalline forms of a compound
WO2020117962A1 (en) 2018-12-05 2020-06-11 Viking Therapeutics, Inc. Compositions for the treatment of fibrosis and inflammation
EP3911647B1 (en) 2019-01-15 2023-12-13 Gilead Sciences, Inc. Isoxazole compound as fxr agonist and pharmaceutical compositions comprising same
KR20210123337A (ko) * 2019-01-31 2021-10-13 더 내셔널 인스티튜츠 오브 파마슈티컬 알앤디 컴퍼니 리미티드 방향족 고리 또는 헤테로방향족 고리 화합물, 이의 제조 방법 및 이의 의학 용도
AU2020221371A1 (en) 2019-02-15 2021-10-07 Bristol-Myers Squibb Company Substituted amide compounds useful as farnesoid x receptor modulators
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
CN113727973B (zh) 2019-02-15 2025-08-29 百时美施贵宝公司 可用作类法尼醇x受体调节剂的取代酰胺化合物
AR118050A1 (es) 2019-02-15 2021-09-15 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x
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
KR20220035365A (ko) 2019-07-18 2022-03-22 엔요 파마 인터페론의 부작용을 감소시키는 방법
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
WO2021252392A1 (en) * 2020-06-09 2021-12-16 Viking Therapeutics, Inc. Compositions and methods for the treatment of liver disorders
JP7599014B2 (ja) * 2020-06-30 2024-12-12 オクヴィルク，ゼレン グアニル酸シクラーゼｃ（ｇｕｃｙ２ｃ）アゴニストおよび短鎖脂肪酸またはそのプロドラッグの組み合わせを含む医薬組成物
JP2024502673A (ja) 2021-01-14 2024-01-22 ウエヌイグレックオ・ファーマ Ｈｂｖ感染の処置のためのｆｘｒアゴニストとｉｆｎの相乗効果
JP2024517181A (ja) 2021-04-28 2024-04-19 ウエヌイグレックオ・ファーマ 組合せ治療としてｆｘｒアゴニストを使用するｔｌｒ３アゴニストの効果の強い増強

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103443099A (zh) * 2010-12-20 2013-12-11 Irm责任有限公司 调节fxr的组合物和方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080255171A1 (en) * 2005-10-07 2008-10-16 Manley Paul W Combination of Nilotinib with Farnesyl Transferase Inhibitors
EP2655368A1 (en) * 2010-12-20 2013-10-30 Irm Llc Compositions and methods for modulating farnesoid x receptors
EP2545964A1 (en) * 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103443099A (zh) * 2010-12-20 2013-12-11 Irm责任有限公司 调节fxr的组合物和方法

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DIANA JUNG等: "FXR agonists and FGF15 reduce fecal bile acid excretion in a mouse model of bile acid malabsorption", 《JOURNAL OF LIPID RESEARCH》 *
池肇春: "《胃肠及肝胆胰疾病鉴别诊断学》", 30 November 2003, 军事医学科学出版社 *
许国铭: "《胆汁反流相关性疾病》", 30 September 2002, 上海科学技术出版社 *

Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111655680A (zh) * 2017-09-14 2020-09-11 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
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
CN110357876A (zh) * 2018-04-10 2019-10-22 浙江海正药业股份有限公司 氮杂双环辛烷类衍生物及其制备方法和用途
CN110357875A (zh) * 2018-04-10 2019-10-22 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
CN110357875B (zh) * 2018-04-10 2022-06-21 浙江海正药业股份有限公司 氮杂双环辛烷类衍生物、其制备方法及其在医药上的用途
CN110357876B (zh) * 2018-04-10 2022-06-28 浙江海正药业股份有限公司 氮杂双环辛烷类衍生物及其制备方法和用途
CN112334467B (zh) * 2018-06-26 2023-06-20 轩竹生物科技股份有限公司 Fxr受体激动剂
WO2020001304A1 (zh) * 2018-06-26 2020-01-02 轩竹（海南）医药科技有限公司 Fxr受体激动剂
CN112334467A (zh) * 2018-06-26 2021-02-05 轩竹生物科技有限公司 Fxr受体激动剂
CN111825701A (zh) * 2019-04-19 2020-10-27 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
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
CN114728955A (zh) * 2019-11-29 2022-07-08 广东东阳光药业有限公司 Tropifexor的新晶型及其制备方法
CN114728954A (zh) * 2019-11-29 2022-07-08 广东东阳光药业有限公司 Tropifexor的新晶型及其制备方法
CN114728954B (zh) * 2019-11-29 2023-10-17 广东东阳光药业股份有限公司 Tropifexor的新晶型及其制备方法
CN113292555A (zh) * 2021-04-28 2021-08-24 武汉纽瑞斯医药科技有限公司 一种Tropifexor的制备方法
CN116987062A (zh) * 2023-08-03 2023-11-03 中国热带农业科学院分析测试中心 一种氨基酸键联槟榔碱衍生物的制备方法

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