SV2018005662A - Moduladores del receptor x farnesoide - Google Patents

Moduladores del receptor x farnesoide

Info

Publication number
SV2018005662A
SV2018005662A SV2018005662A SV2018005662A SV2018005662A SV 2018005662 A SV2018005662 A SV 2018005662A SV 2018005662 A SV2018005662 A SV 2018005662A SV 2018005662 A SV2018005662 A SV 2018005662A SV 2018005662 A SV2018005662 A SV 2018005662A
Authority
SV
El Salvador
Prior art keywords
farnesoid
receiver modulators
modulators
receiver
solvate
Prior art date
Application number
SV2018005662A
Other languages
English (en)
Inventor
Roberto Pelliciari
Antimo Gioiello
Original Assignee
Intercept Pharmaceuticals Inc
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
Application filed by Intercept Pharmaceuticals Inc filed Critical Intercept Pharmaceuticals Inc
Publication of SV2018005662A publication Critical patent/SV2018005662A/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • 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
    • 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
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
    • C07J41/0061—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives one of the carbon atoms being part of an amide group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/001—Oxiranes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Toxicology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Liquid Crystal Substances (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

LA PRESENTE SOLICITUD PROPORCIONA UN COMPUESTO DE FÓRMULA I : O UNA SAL, SOLVATO O CONJUGADO CON AMINOÁCIDOS FARMACÉUTICAMENTE ACEPTABLE DEL MISMO EN DONDE R1-R10, M, N, P, Y (VER FORMULA) SON COMO SE DESCRIBEN EN EL PRESENTE DOCUMENTO. LA PRESENTE INVENCIÓN SE REFIERE, EN GENERAL, A MODULADORES DE FXR Y A MÉTODOS PARA PRODUCIR Y USAR DICHOS COMPUESTOS
SV2018005662A 2015-10-07 2018-04-05 Moduladores del receptor x farnesoide SV2018005662A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562238246P 2015-10-07 2015-10-07

Publications (1)

Publication Number Publication Date
SV2018005662A true SV2018005662A (es) 2018-12-14

Family

ID=58488545

Family Applications (1)

Application Number Title Priority Date Filing Date
SV2018005662A SV2018005662A (es) 2015-10-07 2018-04-05 Moduladores del receptor x farnesoide

Country Status (27)

Country Link
US (2) US11034717B2 (es)
EP (2) EP3359160B1 (es)
JP (2) JP7021080B2 (es)
KR (1) KR20180061351A (es)
CN (1) CN108348530B (es)
AR (1) AR106293A1 (es)
AU (1) AU2016335765B2 (es)
BR (1) BR112018006892B1 (es)
CA (1) CA3000881C (es)
CL (1) CL2018000883A1 (es)
CO (1) CO2018003728A2 (es)
CR (1) CR20180201A (es)
DK (1) DK3359160T3 (es)
EA (1) EA038665B1 (es)
EC (1) ECSP18030284A (es)
ES (1) ES2898705T3 (es)
HK (1) HK1253558A1 (es)
IL (1) IL258359B2 (es)
MA (2) MA45761A (es)
MX (1) MX2018004186A (es)
PH (1) PH12018500777A1 (es)
SV (1) SV2018005662A (es)
TN (1) TN2018000106A1 (es)
TW (1) TW201718621A (es)
UA (1) UA123948C2 (es)
WO (1) WO2017062763A1 (es)
ZA (1) ZA201802901B (es)

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RU2017118569A (ru) 2014-11-06 2018-12-06 Энанта Фармасьютикалс, Инк. Аналоги желчных кислот как агонисты fxr/tgr5 и способы их применения
WO2016086169A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
US11578097B2 (en) 2014-11-26 2023-02-14 Enanta Pharmaceuticals, Inc. Tetrazole derivatives of bile acids as FXR/TGR5 agonists and methods of use thereof
SG11201706089RA (en) 2015-02-11 2017-09-28 Enanta Pharm Inc Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
CN107427527B (zh) 2015-03-31 2021-01-26 英安塔制药有限公司 作为fxr/tgr5激动剂的胆汁酸衍生物及其使用方法
US11034717B2 (en) * 2015-10-07 2021-06-15 Intercept Pharmaceuticals, Inc. Farnesoid X receptor modulators
WO2017147174A1 (en) 2016-02-23 2017-08-31 Enanta Pharmaceuticals, Inc. Heteroaryl containing bile acid analogs as fxr/tgr5 agonists and methods of use thereof
US10323060B2 (en) 2016-02-23 2019-06-18 Enanta Pharmaceuticals, Inc. Benzoic acid derivatives of bile acid as FXR/TGR5 agonists and methods of use thereof
WO2017147159A1 (en) 2016-02-23 2017-08-31 Enanta Pharmaceuticals, Inc. Deuterated bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
WO2018102418A1 (en) 2016-11-29 2018-06-07 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonylurea bile acid derivatives
US10472386B2 (en) 2017-02-14 2019-11-12 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR agonists and methods of use thereof
EP3606533B1 (en) 2017-04-07 2023-11-15 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonyl carbamate bile acid derivatives
AU2018288883B2 (en) 2017-06-23 2022-06-02 Intercept Pharmaceuticals, Inc. Methods and intermediates for the preparation of bile acid derivatives
CN111050772A (zh) 2017-07-24 2020-04-21 英特塞普特医药品公司 同位素标记的胆汁酸衍生物
JP6948680B2 (ja) * 2017-12-19 2021-10-13 西安奥立泰医薬科技有限公司Ｘｉ’Ａｎ Ｂｉｏｃａｒｅ Ｐｈａｒｍａ Ｌｔｄ． 代謝性疾患治療用化合物及びその製造方法、並びに応用
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
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
WO2023288123A1 (en) 2021-07-16 2023-01-19 Interecept Pharmaceuticals, Inc. Methods and intermediates for the preparation of 3.alpha.,7.alpha.,11.beta.-trihydroxy-6.alpha.-ethyl-5.beta.-cholan-24-oic acid

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EP0101554B1 (en) * 1982-07-29 1986-10-15 Lehner A.G. New derivatives of biliary acids, process for the production thereof and pharmaceutical compositions containing the same
IT1223313B (it) 1987-10-20 1990-09-19 Gipharmex Spa Derivati di acidi biliari loro preparazione e composizioni farmaceutiche che li contengono
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SI2040713T1 (sl) * 2006-06-27 2014-11-28 Intercept Pharmaceuticals, Inc. Derivati žolčne kisline kot FXR ligandi za preprečevanje ali zdravljenje bolezni ali stanj, posredovanih s FXR
KR101789960B1 (ko) * 2008-11-19 2017-10-25 인터셉트 파마슈티컬즈, 인크. Tgr5 조절제 및 그의 사용 방법
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WO2016086169A1 (en) * 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
US11034717B2 (en) * 2015-10-07 2021-06-15 Intercept Pharmaceuticals, Inc. Farnesoid X receptor modulators
CN108347941B (zh) 2015-10-07 2021-06-01 斯托尔勒企业公司 使用含有二酰基脲或二芳基脲和至少一种金属配合物的具有协同作用的农业配方管理植物中的乙烯
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Also Published As

Publication number Publication date
EP3359160B1 (en) 2021-08-25
EP3981779A1 (en) 2022-04-13
CA3000881A1 (en) 2017-04-13
EA038665B1 (ru) 2021-09-30
AU2016335765A1 (en) 2018-04-19
WO2017062763A1 (en) 2017-04-13
DK3359160T3 (da) 2021-11-22
EP3359160A4 (en) 2019-06-05
IL258359A (en) 2018-06-28
PH12018500777A1 (en) 2018-10-29
KR20180061351A (ko) 2018-06-07
JP2019210297A (ja) 2019-12-12
AR106293A1 (es) 2018-01-03
IL258359B2 (en) 2023-11-01
ES2898705T3 (es) 2022-03-08
UA123948C2 (uk) 2021-06-30
CA3000881C (en) 2024-03-19
AU2016335765B2 (en) 2022-01-06
US20170101434A1 (en) 2017-04-13
BR112018006892A2 (pt) 2018-10-16
MA42339A1 (fr) 2019-01-31
HK1253558A1 (zh) 2019-06-21
CL2018000883A1 (es) 2018-06-29
ZA201802901B (en) 2019-07-31
JP7021080B2 (ja) 2022-02-16
MA45761A (fr) 2021-04-21
US20210269475A1 (en) 2021-09-02
ECSP18030284A (es) 2018-05-31
EA201890899A1 (ru) 2018-09-28
BR112018006892B1 (pt) 2023-04-11
US11034717B2 (en) 2021-06-15
TW201718621A (zh) 2017-06-01
IL258359B1 (en) 2023-07-01
CN108348530A (zh) 2018-07-31
CO2018003728A2 (es) 2018-07-31
CR20180201A (es) 2018-08-24
TN2018000106A1 (en) 2019-10-04
CN108348530B (zh) 2023-09-29
JP2018530559A (ja) 2018-10-18
EP3359160A1 (en) 2018-08-15
MX2018004186A (es) 2018-05-17

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