SG11201805235XA - Polymorphic crystalline forms of obeticholic acid - Google Patents

Polymorphic crystalline forms of obeticholic acid

Info

Publication number
SG11201805235XA
SG11201805235XA SG11201805235XA SG11201805235XA SG11201805235XA SG 11201805235X A SG11201805235X A SG 11201805235XA SG 11201805235X A SG11201805235X A SG 11201805235XA SG 11201805235X A SG11201805235X A SG 11201805235XA SG 11201805235X A SG11201805235X A SG 11201805235XA
Authority
SG
Singapore
Prior art keywords
international
cambridge
owe
crystalline forms
obeticholic acid
Prior art date
Application number
SG11201805235XA
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=55650649&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SG11201805235X(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US14/979,005 external-priority patent/US9982008B2/en
Application filed by Intercept Pharmaceuticals Inc filed Critical Intercept Pharmaceuticals Inc
Publication of SG11201805235XA publication Critical patent/SG11201805235XA/en

Links

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
    • 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
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization MD 1111101110101011111 HO 11111 01E33 0111111011111011111011 III International Bureau ... .... ..Yjd (10) International Publication Number (43) International Publication Date ..... ...r .....1 WO 2017/111979 Al 29 June 2017(29.06.2017) WIPO I PCT (51) International Patent Classification: morphix Ltd., 250 Cambridge Science Park, Milton Road, C07J 9/00 (2006.01) A61K 31/575 (2006.01) Cambridge CB4 OWE (GB). C07J 17/00 (2006.01) A61P 1/16 (2006.01) (74) Agent: IWAMOTO-FAN, Michelle; Intercept Pharma- C07J 51/00 (2006.01) ceuticals, Inc., 450 W. 15th Suite 505, New York, NY (21) International Application Number: 10011 (US). PCT/US2016/012651 (81) Designated States (unless otherwise indicated, for every (22) International Filing Date: kind of national protection available): AE, AG, AL, AM, 8 January 2016 (08.01.2016) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, (25) Filing Language: English DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (26) Publication Language: English HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, (30) Priority Data: MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, 14/979,005 22 December 2015 (22.12.2015) US PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, (71) Applicant: INTERCEPT PHARMACEUTICALS, INC. SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, [US/US]; 450 W. 15th Suite 505, New York, NY 10011 TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (US). (84) Designated States (unless otherwise indicated, for every (72) Inventors: STEINER, Andre; PharmaZell GmbH, Rosen- kind of regional protection available): ARIPO (BW, GH, heimer Str. 43, 83064 Raubling (DE). WAENERLUND GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, POULSEN, Heidi; FeF Chemicals A/S, Kobenbavnsvej TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, 216, 4600 Koge (DK). JOLIBOIS, Emilie; Pharmorphix TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, Ltd., 250 Cambridge Science Park, Milton Road, Cam- DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, bridge CB4 OWE (GB). REWOLINSKI, Melissa; 4350 LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, La Jolla Village Drive, Suite 960, San Diego, CA 92122 SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, (US). GROSS, Ralf; PharmaZell GmbH, Rosenheimer Str. GW, KM, ML, MR, NE, SN, TD, TG). = 43, 83064 Raubling (DE). SHARP, Emma; Pharmorphix Published: Ltd., 250 Cambridge Science Park, Milton Road, Cam- bridge CB4 OWE (GB). DUBAS-FISHER, Fiona; Phar- with international search report (Art. 21(3)) morphix Ltd., 250 Cambridge Science Park, Milton Road, Cambridge CB4 OWE (GB). EBERLIN, Alex; Phar- (54) Title: POLYMORPHIC CRYSTALLINE FORMS OF OBETICHOLIC ACID CO2H 1-1 C:r IN o, ,-, ,-, ,-, H 0 ‘ / OH - _ IN 1-1 (57) : The present application relates to crystalline forms A, D, F, G and I of obeticholic acid. These crystalline forms are 0 useful in the production of Obeticholic acid (in particular its purification), which is a drug useful for the treatment or prevention of a \" FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lower - 0 ing triglycerides in a mammal, or for inhibition of fibrosis.
SG11201805235XA 2015-12-22 2016-01-08 Polymorphic crystalline forms of obeticholic acid SG11201805235XA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US14/979,005 US9982008B2 (en) 2012-06-19 2015-12-22 Preparation and uses of obeticholic acid
PCT/US2016/012651 WO2017111979A1 (en) 2015-12-22 2016-01-08 Polymorphic crystalline forms of obeticholic acid

Publications (1)

Publication Number Publication Date
SG11201805235XA true SG11201805235XA (en) 2018-07-30

Family

ID=55650649

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201805235XA SG11201805235XA (en) 2015-12-22 2016-01-08 Polymorphic crystalline forms of obeticholic acid

Country Status (15)

Country Link
EP (1) EP3394081A1 (en)
JP (1) JP2018538331A (en)
KR (1) KR20180095070A (en)
CN (1) CN108495858A (en)
AU (1) AU2016375566A1 (en)
BR (1) BR112018012590A2 (en)
CA (1) CA3009149A1 (en)
CL (1) CL2018001720A1 (en)
CO (1) CO2018006701A2 (en)
EA (1) EA201891491A1 (en)
IL (1) IL259998A (en)
MX (1) MX2018007776A (en)
PH (1) PH12018501318A1 (en)
SG (1) SG11201805235XA (en)
WO (1) WO2017111979A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105801653B (en) * 2014-12-30 2018-04-17 苏州晶云药物科技有限公司 Crystal form A of shellfish cholic acid difficult to understand and preparation method thereof
WO2018211413A1 (en) * 2017-05-15 2018-11-22 Dr. Reddy’S Laboratories Limited Solid forms of obeticholic acid and process for preparation
CN109280071A (en) * 2017-07-19 2019-01-29 东莞东阳光药物研发有限公司 The crystal form and preparation method thereof of shellfish cholic acid difficult to understand
CN107383139A (en) * 2017-08-09 2017-11-24 杭州和泽医药科技有限公司 The method that a kind of β cholanic acid new derivatives of 7 oxo of 3 α hydroxyls 5 prepare shellfish cholic acid difficult to understand
CZ31099U1 (en) * 2017-09-05 2017-10-17 Zentiva, K.S. The crystalline forms of (3α,5β,6α,7α)-6-ethyl-3,7-dihydroxycholan-24-oic acid
CN109485687A (en) * 2017-09-12 2019-03-19 成都弘达药业有限公司 The crystal form J and preparation method thereof of shellfish cholic acid difficult to understand
WO2019106043A1 (en) 2017-11-29 2019-06-06 Hexal Ag Pharmaceutical composition comprising obeticholic acid
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
CN113264972A (en) * 2020-02-14 2021-08-17 四川科伦药物研究院有限公司 Method for preparing obeticholic acid

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ITMI20050912A1 (en) * 2005-05-19 2006-11-20 Erregierre Spa PROCESS OF PREPARATION OF ACIDS 3-A-YA (B) -DIDROSSI-6-A (B) -ALCHIL-5B-COLANICI
DK3336097T3 (en) * 2012-06-19 2020-09-28 Intercept Pharmaceuticals Inc Preparation of non-crystalline obeticholic acid
CN106459136B (en) * 2014-09-28 2018-06-26 江苏盛迪医药有限公司 A kind of preparation method of Austria's shellfish cholic acid
CN107108688B (en) * 2014-11-19 2019-10-29 Nzp英国有限公司 6 alpha-alkyl -3,7- diketone the steroids as the intermediate for preparing steroids FXR regulator
EP3221331B1 (en) * 2014-11-19 2019-09-18 Nzp Uk Limited 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators
EA033445B1 (en) * 2014-11-19 2019-10-31 Nzp Uk Ltd 5-beta-6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal fxr modulators
KR102527821B1 (en) * 2014-11-19 2023-05-02 엔제트피 유케이 리미티드 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators

Also Published As

Publication number Publication date
KR20180095070A (en) 2018-08-24
MX2018007776A (en) 2018-08-09
PH12018501318A1 (en) 2019-02-18
CN108495858A (en) 2018-09-04
CA3009149A1 (en) 2017-06-29
BR112018012590A2 (en) 2018-12-04
EP3394081A1 (en) 2018-10-31
JP2018538331A (en) 2018-12-27
EA201891491A1 (en) 2018-11-30
CO2018006701A2 (en) 2018-07-10
WO2017111979A1 (en) 2017-06-29
IL259998A (en) 2018-07-31
AU2016375566A1 (en) 2018-07-05
CL2018001720A1 (en) 2018-08-10

Similar Documents

Publication Publication Date Title
SG11201805235XA (en) Polymorphic crystalline forms of obeticholic acid
SG11201408501UA (en) Preparation, uses and solid forms of obeticholic acid
SG11201906209SA (en) Bicyclic compounds as allosteric shp2 inhibitors
SG11201906412SA (en) Pyridine compounds as allosteric shp2 inhibitors
SG11201408769QA (en) Methods of reducing the risk of a cardiovascular event in a subject on statin therapy
SG11201809344QA (en) Process for synthesizing 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)-pyridin-3-yl)methoxy)benzaldehyde
SG11201803686UA (en) Prodrugs of a jak inhibitor compound for treatment of gastrointestinal inflammatory disease
SG11201804170RA (en) Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders
SG11201809299QA (en) Formulations of an lsd1 inhibitor
SG11201407662WA (en) Process for the preparation of treprostinil and derivatives thereof
SG11201804647TA (en) Dosing regimens for 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde
SG11201807012QA (en) Acid addition salts of piperazine derivatives
SG11201807784SA (en) 3-desoxy derivative and pharmaceutical compositions thereof
SG11201804811WA (en) Fenfluramine compositions and methods of preparing the same
SG11201900349VA (en) Somatostatin modulators and uses thereof
SG11201900745VA (en) Substituted thiazolo-pyridine compounds as malt1 inhibitors
SG11201901140QA (en) Compounds and methods for reducing tau expression
SG11201809342YA (en) Pyrimidine compounds as jak kinase inhibitors
SG11201408251SA (en) A pharmaceutical composition containing nicotinic acid and/or nicotinamide and/or tryptophan for positively influencing the intestinal microbiota
SG11201804774YA (en) Diastereoselective synthesis of phosphate derivatives and of the gemcitabine prodrug nuc-1031
SG11201908512YA (en) Somatostatin modulators and uses thereof
SG11201810177VA (en) Pet-imaging immunomodulators
SG11201906436VA (en) Novel heterocyclic compound, its preparation method, and pharmaceutical composition comprising the same
SG11201407988UA (en) Process for improved opioid synthesis
SG11201804100UA (en) Pharmaceutical composition comprising a potent inhibitor of urat1