SG11201704340VA - Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases - Google Patents

Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases

Info

Publication number
SG11201704340VA
SG11201704340VA SG11201704340VA SG11201704340VA SG11201704340VA SG 11201704340V A SG11201704340V A SG 11201704340VA SG 11201704340V A SG11201704340V A SG 11201704340VA SG 11201704340V A SG11201704340V A SG 11201704340VA SG 11201704340V A SG11201704340V A SG 11201704340VA
Authority
SG
Singapore
Prior art keywords
liver
treatment
gastrointestinal diseases
fxr agonists
azabicyclooctane
Prior art date
Application number
SG11201704340VA
Other languages
English (en)
Inventor
Michael Badman
Lloyd B Klickstein
Bryan Laffitte
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=54979887&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SG11201704340V(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of SG11201704340VA publication Critical patent/SG11201704340VA/en

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
    • A61K31/435—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

Landscapes

  • 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)
SG11201704340VA 2014-12-18 2015-12-08 Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases SG11201704340VA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462093586P 2014-12-18 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)

Publication Number Publication Date
SG11201704340VA true SG11201704340VA (en) 2017-07-28

Family

ID=54979887

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201704340VA SG11201704340VA (en) 2014-12-18 2015-12-08 Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases

Country Status (17)

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

Families Citing this family (56)

* 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
SG11201707263XA (en) 2015-03-31 2017-10-30 Enanta Pharm Inc Bile acid derivatives as fxr/tgr5 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
US10080742B2 (en) 2016-04-26 2018-09-25 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
US10144729B2 (en) 2016-05-18 2018-12-04 Enanta Pharmaceuticals, Inc. Isoxazole analogs 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
US10149835B2 (en) 2016-05-18 2018-12-11 Elmore Patent Law Group, P.C. Isoxazole derivatives as FXR agonists and methods of use thereof
KR102269305B1 (ko) 2016-06-13 2021-06-25 길리애드 사이언시즈, 인코포레이티드 Fxr (nr1h4) 조정 화합물
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
WO2018039386A1 (en) * 2016-08-23 2018-03-01 Ardelyx, Inc. Hormone receptor modulators for treating metabolic conditions and disorders
JOP20190040A1 (ar) * 2016-09-14 2019-03-10 Novartis Ag توليفة من ناهضات fxr
BR112019006651A2 (pt) 2016-10-04 2019-07-02 Enanta Pharm Inc análogos de isoxazol como agonistas de fxr e métodos de uso do mesmo
KR20190062501A (ko) * 2016-10-05 2019-06-05 노파르티스 아게 섬유증, 간경화 질환 또는 질병을 치료 또는 예방하기 위한 fxr 작용제를 포함하는 조합 조성물
US10597391B2 (en) 2016-10-26 2020-03-24 Enanta Pharmaceuticals, Inc. Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof
CN108017636A (zh) 2016-11-04 2018-05-11 合帕吉恩治疗公司 作为fxr调节剂的含氮杂环化合物
AU2018243719B2 (en) 2017-03-28 2021-01-21 Gilead Sciences, Inc. Therapeutic combinations for treating liver diseases
CN110678450B (zh) 2017-04-12 2023-06-20 日东制药株式会社 作为核受体激动剂的异噁唑衍生物及其用途
JP6997870B2 (ja) * 2017-07-06 2022-02-10 シュアンチュー バイオファーマシューティカル カンパニー，リミティド Ｆｘｒ受容体刺激薬
WO2019055808A1 (en) * 2017-09-14 2019-03-21 Ardelyx, Inc. HORMONE RECEPTOR MODULATORS FOR THE TREATMENT OF MUTAGENIC AND FIBROTIC METABOLIC CONDITIONS AND DISORDERS
MX2020004405A (es) 2017-11-01 2020-08-06 Bristol Myers Squibb Co Compuestos biciclicos en puente como moduladores del receptor farnesoide x.
ES2944657T3 (es) 2017-11-01 2023-06-23 Bristol Myers Squibb Co Compuestos de alqueno como moduladores del receptor farnesoide X
EA202091101A1 (ru) 2017-11-01 2020-08-06 Бристол-Маерс Сквибб Компани Спироциклические соединения в качестве модуляторов фарнезоидного x-рецептора
EP3704107B1 (en) 2017-11-01 2023-04-12 Bristol-Myers Squibb Company Multicyclic compounds as farnesoid x receptor modulators
WO2019089665A1 (en) 2017-11-01 2019-05-09 Bristol-Myers Squibb Company Alkene spirocyclic compounds as farnesoid x receptor modulators
US10689391B2 (en) 2017-12-12 2020-06-23 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
WO2019120088A1 (zh) 2017-12-22 2019-06-27 四川科伦博泰生物医药股份有限公司 异噁唑衍生物及其制备方法和用途
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
WO2019183004A1 (en) 2018-03-22 2019-09-26 Viking Therapeutics, Inc. Crystalline forms and methods of producing crystalline forms of a compound
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
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
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
JP2022510691A (ja) 2018-12-05 2022-01-27 バイキング・セラピューティクス・インコーポレイテッド 線維症及び炎症の処置のための組成物
SG11202107434PA (en) 2019-01-15 2021-08-30 Gilead Sciences Inc Fxr (nr1h4) modulating compounds
AU2020214889A1 (en) * 2019-01-31 2021-09-02 The National Institutes of Pharmaceutical R&D Co., Ltd. Aromatic ring or heteroaromatic ring compounds, preparation method therefor and medical use thereof
CA3129619A1 (en) 2019-02-15 2020-08-20 Bristol-Myers Squibb Company Substituted amide compounds useful as farnesoid x receptor modulators
BR112021015930A2 (pt) 2019-02-15 2021-10-05 Bristol-Myers Squibb Company Compostos de amida substituídos úteis como moduladores de receptor farnesoide x
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
KR102725082B1 (ko) 2019-02-19 2024-11-04 길리애드 사이언시즈, 인코포레이티드 Fxr 효능제의 고체 형태
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
WO2020231917A1 (en) 2019-05-13 2020-11-19 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
EP3999101A1 (en) 2019-07-18 2022-05-25 ENYO Pharma Method for decreasing adverse-effects of interferon
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
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
CA3159163A1 (en) 2020-01-15 2021-07-22 Raphael Darteil Use of fxr agonists for treating an infection by hepatitis d virus
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
EP4171600B1 (en) 2020-06-30 2024-11-27 Sören OCVIRK Pharmaceutical composition comprising a combination of a guanylate cyclase c (gucy2c) agonist and a short-chain fatty acid or prodrug thereof
US20240100125A1 (en) 2021-01-14 2024-03-28 Enyo Pharma Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
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
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
CN116987062A (zh) * 2023-08-03 2023-11-03 中国热带农业科学院分析测试中心 一种氨基酸键联槟榔碱衍生物的制备方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009511450A (ja) * 2005-10-07 2009-03-19 ノバルティス アクチエンゲゼルシャフト ニロチニブとファルネシルトランスフェラーゼ阻害剤の組合せ
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

Also Published As

Publication number Publication date
RU2017125365A3 (zh) 2019-07-17
RU2017125365A (ru) 2019-01-21
CA2970866A1 (en) 2016-06-23
WO2016097933A1 (en) 2016-06-23
IL252596A0 (en) 2017-07-31
AU2015365481B2 (en) 2018-08-09
TN2017000243A1 (en) 2018-10-19
EP3233083A1 (en) 2017-10-25
JP2017537960A (ja) 2017-12-21
CL2017001566A1 (es) 2018-03-23
CN107106555A (zh) 2017-08-29
US20170368038A1 (en) 2017-12-28
MX2017008057A (es) 2017-09-28
TW201628615A (zh) 2016-08-16
BR112017011972A2 (pt) 2017-12-26
KR20170095965A (ko) 2017-08-23
PH12017501046A1 (en) 2017-11-27
AU2015365481A1 (en) 2017-06-22
US20190083473A1 (en) 2019-03-21

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