BR122016011808B1 - Processos para preparar a forma 1 de ácido obeticólico e o ácido obeticólico cristalino - Google Patents

Processos para preparar a forma 1 de ácido obeticólico e o ácido obeticólico cristalino Download PDF

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Publication number
BR122016011808B1
BR122016011808B1 BR122016011808-8A BR122016011808A BR122016011808B1 BR 122016011808 B1 BR122016011808 B1 BR 122016011808B1 BR 122016011808 A BR122016011808 A BR 122016011808A BR 122016011808 B1 BR122016011808 B1 BR 122016011808B1
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BR
Brazil
Prior art keywords
acid
obeticic
hydroxy
keto
oic
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BR122016011808-8A
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English (en)
Portuguese (pt)
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BR122016011808A2 (pt
Inventor
André Steiner
Heidi Waenerlund Poulsen
Emilie Jolibois
Melissa Rewolinski
Ralf Gross
Emma Sharp
Fiona Dubas-Fisher
Alex Eberlin
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Intercept Pharmaceuticals, Inc
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Application filed by Intercept Pharmaceuticals, Inc filed Critical Intercept Pharmaceuticals, Inc
Publication of BR122016011808A2 publication Critical patent/BR122016011808A2/pt
Publication of BR122016011808B1 publication Critical patent/BR122016011808B1/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal 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
    • C07J9/005Normal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/04Drugs for disorders of the urinary system for urolithiasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
BR122016011808-8A 2012-06-19 2013-06-17 Processos para preparar a forma 1 de ácido obeticólico e o ácido obeticólico cristalino BR122016011808B1 (pt)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201261661531P 2012-06-19 2012-06-19
US61/661,531 2012-06-19
PCT/US2013/046150 WO2013192097A1 (en) 2012-06-19 2013-06-17 Preparation, uses and solid forms of obeticholic acid
BR112014031828-0A BR112014031828B1 (pt) 2012-06-19 2013-06-17 Composições farmacêuticas compreendendo a forma 1 de ácido obeticólico

Publications (2)

Publication Number Publication Date
BR122016011808A2 BR122016011808A2 (pt) 2018-12-11
BR122016011808B1 true BR122016011808B1 (pt) 2021-09-21

Family

ID=48741553

Family Applications (2)

Application Number Title Priority Date Filing Date
BR122016011808-8A BR122016011808B1 (pt) 2012-06-19 2013-06-17 Processos para preparar a forma 1 de ácido obeticólico e o ácido obeticólico cristalino
BR112014031828-0A BR112014031828B1 (pt) 2012-06-19 2013-06-17 Composições farmacêuticas compreendendo a forma 1 de ácido obeticólico

Family Applications After (1)

Application Number Title Priority Date Filing Date
BR112014031828-0A BR112014031828B1 (pt) 2012-06-19 2013-06-17 Composições farmacêuticas compreendendo a forma 1 de ácido obeticólico

Country Status (25)

Country Link
US (9) US9238673B2 (enExample)
EP (4) EP3789394A1 (enExample)
JP (6) JP2015521621A (enExample)
KR (4) KR20180083966A (enExample)
CN (2) CN104781272A (enExample)
AU (5) AU2013277429B2 (enExample)
BR (2) BR122016011808B1 (enExample)
CA (3) CA2877122C (enExample)
CL (2) CL2014003475A1 (enExample)
CO (1) CO7240414A2 (enExample)
DK (1) DK3336097T3 (enExample)
EA (2) EA201990211A1 (enExample)
ES (1) ES2822375T3 (enExample)
HK (1) HK1211296A1 (enExample)
IL (3) IL236231A0 (enExample)
IN (1) IN2014MN02561A (enExample)
MX (2) MX365059B (enExample)
NZ (3) NZ719360A (enExample)
PH (1) PH12014502835A1 (enExample)
PL (1) PL3336097T3 (enExample)
PT (1) PT3336097T (enExample)
SG (3) SG10201610434YA (enExample)
SI (1) SI3336097T1 (enExample)
TW (1) TWI673284B (enExample)
WO (1) WO2013192097A1 (enExample)

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