.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 8,969,330

« Back to Dashboard

Details for Patent: 8,969,330

Title:Steroids as agonists for FXR
Abstract: The invention relates to compounds of formula (I): ##STR00001## wherein R is ethyl, propyl or allyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
Inventor(s): Pellicciari; Roberto (Perugia, IT)
Assignee: Intercept Pharmaceuticals, Inc. (New York, NY)
Filing Date:Feb 07, 2013
Application Number:13/761,889
Claims:1. A process for preparing a compound of formula I: ##STR00007## or a pharmaceutically acceptable salt or amino acid conjugate thereof, comprising: a) reacting 3.alpha.-hydroxy-7-keto-5.beta.-cholan-24-oic acid with 3,4-dihydropyrane to prepare 3.alpha.-tetrahydropyranyloxy-7-keto-5.beta.-cholan-24-oic acid; b) reacting 3.alpha.-tetrahydropyranyloxy-7-keto-5.beta.-cholan-24-oic acid with an alkyl bromide of the formula R--Br, wherein R is ethyl, to prepare a compound of formula II: ##STR00008## c) reacting the compound of formula II with sodium borohydride to prepare a compound of formula III: ##STR00009## d) reacting the compound of formula II with sodium hydroxide to prepare the compound of formula I.

2. A method of increasing flow of bile acids from the liver to the intestine in a subject suffering from a cholestatic liver disease, comprising administering to the subject a therapeutically effective amount of a compound of formula I: ##STR00010## or a pharmaceutically acceptable salt or amino acid conjugate thereof.

3. The method of claim 2, wherein the compound is a glycine conjugate of the compound of formula I.

4. The method of claim 2, wherein the compound is a taurine conjugate of the compound of formula I.

5. The method of claim 2, wherein the compound is a pharmaceutically acceptable salt of the compound of formula I.

6. The method of claim 2, wherein the subject is a mammal.

7. The method of claim 6, wherein the mammal is a human.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc