SG11201408501UA - Preparation, uses and solid forms of obeticholic acid - Google Patents

Preparation, uses and solid forms of obeticholic acid

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Publication number
SG11201408501UA
SG11201408501UA SG11201408501UA SG11201408501UA SG11201408501UA SG 11201408501U A SG11201408501U A SG 11201408501UA SG 11201408501U A SG11201408501U A SG 11201408501UA SG 11201408501U A SG11201408501U A SG 11201408501UA SG 11201408501U A SG11201408501U A SG 11201408501UA
Authority
SG
Singapore
Prior art keywords
cambridge
international
owe
obeticholic acid
science park
Prior art date
Application number
SG11201408501UA
Inventor
André Steiner
Poulsen Heidi Waenerlund
Emilie Jolibois
Melissa Rewolinski
Ralf Gross
Emma Sharp
Fiona Dubas-Fisher
Alex Eberlin
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48741553&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SG11201408501U(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Intercept Pharmaceuticals Inc filed Critical Intercept Pharmaceuticals Inc
Publication of SG11201408501UA publication Critical patent/SG11201408501UA/en

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Classifications

    • 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
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61P13/04—Drugs for disorders of the urinary system for urolithiasis
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • 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)

Abstract

(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 27 December 2013 (27.12.2013) WIPOIPCT (10) International Publication Number WO 2013/192097 A1 (51) International Patent Classification: C07J9/00 (2006.01) A61P1/16 (2006.01) A61K31/575 (2006.01) C07J51/00 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2013/046150 17 June 2013 (17.06.2013) English (30) Priority Data: 61/661,531 19 June 2012 (19.06.2012) English US (71) Applicant: INTERCEPT PHARMACEUTICALS, INC. [US/US]; 18 Desbrosses Street, New York, NY 10013 (US). (72) Inventors: STEINER, Andre; PharmaZell GmbH, Rosen- heimer Str. 43, 83064 Raubling (DE). WAENERLUND POULSEN, Heidi; FeF Chemicals A/S, Kobenhavnsvej 216, DK-4600 K0ge (DK). JOLIBOIS, Emilie; Phar- morphix Ltd., 250 Cambridge Science Park, Milton Road, Cambridge CB4 OWE (GB). REWOLINSKI, Melissa; 4350 La Jolla Village Drive, Suite 960, San Diego, CA 92122 (US). GROSS, Ralf; PharmaZell GmbH, Rosen- heimer Str. 43, 83064 Raubling (DE). SHARP, Emma; Pharmorphix Ltd., 250 Cambridge Science Park, Milton Road, Cambridge CB4 OWE (GB). DUBAS-FISHER, Fiona; Pharmorphix Ltd., 250 Cambridge Science Park, Milton Road, Cambridge CB4 OWE (GB). EBERLIN, Alex; Pharmorphix Ltd., 250 Cambridge Science Park, Milton Road, Cambridge CB4 OWE (GB). (74) Agents: ELRIFI, Ivor, R. et al.; Mintz Levin Cohn Ferris Glovsky and Popeo, P.C., One Financial Center, Boston, MA 02111 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available)'. AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, [Continued on next page] (54) Title: PREPARATION, USES AND SOLID FORMS OF OBETICHOLIC ACID l> 0\ © CJ 0\ FIG. 5 1600 1500 1400 1300 1200 1100- I\" 1000 o 900 O .S 800 • 700 600 500 400 300 200 100 0 I /^ir VVJVVH A*V. 20 2-Theta - Scale 30 40 (57) Abstract: The present invention relates to obeticholic acid: or a pharma- ceutically acceptable salt, solvate or amino acid conjugate thereof. Obetich­ olic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for redu­ cing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibi­ tion of fibrosis. The present invention also relates processes to for the synthes­ is of obeticholic acid. i-H o CJ o & WO 2013/192097 A1IIH SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, FT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3))
SG11201408501UA 2012-06-19 2013-06-17 Preparation, uses and solid forms of obeticholic acid SG11201408501UA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261661531P 2012-06-19 2012-06-19
PCT/US2013/046150 WO2013192097A1 (en) 2012-06-19 2013-06-17 Preparation, uses and solid forms of obeticholic acid

Publications (1)

Publication Number Publication Date
SG11201408501UA true SG11201408501UA (en) 2015-01-29

Family

ID=48741553

Family Applications (3)

Application Number Title Priority Date Filing Date
SG11201408501UA SG11201408501UA (en) 2012-06-19 2013-06-17 Preparation, uses and solid forms of obeticholic acid
SG10201610434YA SG10201610434YA (en) 2012-06-19 2013-06-17 Preparation, uses and solid forms of obeticholic acid
SG10201607230SA SG10201607230SA (en) 2012-06-19 2013-06-17 Preparation, Uses And Solid Forms Of Obeticholic Acid

Family Applications After (2)

Application Number Title Priority Date Filing Date
SG10201610434YA SG10201610434YA (en) 2012-06-19 2013-06-17 Preparation, uses and solid forms of obeticholic acid
SG10201607230SA SG10201607230SA (en) 2012-06-19 2013-06-17 Preparation, Uses And Solid Forms Of Obeticholic Acid

Country Status (25)

Country Link
US (8) US9238673B2 (en)
EP (4) EP3992201A1 (en)
JP (6) JP2015521621A (en)
KR (4) KR20190121871A (en)
CN (2) CN104781272A (en)
AU (5) AU2013277429B2 (en)
BR (2) BR112014031828B1 (en)
CA (3) CA2877122C (en)
CL (2) CL2014003475A1 (en)
CO (1) CO7240414A2 (en)
DK (1) DK3336097T3 (en)
EA (2) EA032347B1 (en)
ES (1) ES2822375T3 (en)
HK (1) HK1211296A1 (en)
IL (3) IL236231A0 (en)
IN (1) IN2014MN02561A (en)
MX (2) MX365059B (en)
NZ (3) NZ703072A (en)
PH (1) PH12014502835A1 (en)
PL (1) PL3336097T3 (en)
PT (1) PT3336097T (en)
SG (3) SG11201408501UA (en)
SI (1) SI3336097T1 (en)
TW (1) TWI673284B (en)
WO (1) WO2013192097A1 (en)

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