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Solid dosage forms of (s)-ethyl 2-amino-3-(4-(2-amino-6-((r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate

a technology of ethyl amino-3 and phenyl phenyl, which is applied in the direction of biocide, drug composition, organic chemistry, etc., can solve the problems of difficult incorporation of ethyl amino-3 into a commercially viable dosage form, and complicate the manufacture of dosage forms containing ethyl amino-3

Inactive Publication Date: 2015-06-11
CHEN JINLING +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Benefits of technology

The resulting tablets exhibit rapid disintegration times, high stability, and effective drug release, maintaining chemical integrity even under typical storage conditions, thus addressing the challenges of telotristat's properties.

Problems solved by technology

Unfortunately, telotristat's physicochemical properties make its incorporation into a commercially viable dosage form difficult.
The poor flowability of telotristat's crystalline hippurate salt (telotristat etiprate) further complicates the manufacture of dosage forms comprising it.

Method used

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  • Solid dosage forms of (s)-ethyl 2-amino-3-(4-(2-amino-6-((r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate
  • Solid dosage forms of (s)-ethyl 2-amino-3-(4-(2-amino-6-((r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate
  • Solid dosage forms of (s)-ethyl 2-amino-3-(4-(2-amino-6-((r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate

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Embodiment Construction

[0018]This invention is directed to solid pharmaceutical dosage forms in which an active pharmaceutical ingredient (API) is (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate (telotristat):

or a pharmaceutically acceptable salt thereof. The compound, its salts and crystalline forms can be obtained by methods known in the art. See, e.g., U.S. Pat. No. 7,709,493.

[0019]Particular dosage forms comprise crystalline telotristat freebase. One form of this compound has a melting point of about 104° C. as determined by differential scanning calorimetry (DSC) (onset temperature). As used in connection with DSC temperatures, the term “about” means ±3° C. This form provides an X-ray powder diffraction (XRPD) pattern that contains peaks at about 10.7, 12.2, 12.8, 17.7 and / or 22.0 degrees 2θ. As used in connection with XPRD peaks, the term “about” means ±0.3 degrees 2θ. As those skilled in the art are well a...

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Abstract

Solid pharmaceutical dosage forms comprising (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4- yl)phenyl)propanoate (telotristat) are disclosed, as well as methods of making them and compositions useful in their manufacture.

Description

[0001]This application claims priority to U.S. patent application Ser. No. 13 / 652,527, filed Oct. 16, 2012, which claims priority to U.S. provisional patent application No. 61 / 547,894, filed Oct. 17, 2011, the entiries of which is incorporated herein by reference.1. FIELD OF THE INVENTION[0002]This invention relates to solid pharmaceutical dosage forms of (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate (telotristat).2. BACKGROUND OF THE INVENTION[0003]The compound (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate (telotristat) is an inhibitor of tryptophan hydroxylase, the enzyme responsible for the rate-limiting step in biosynthesis of 5-hydroxytryptamine (serotonin). See, e.g., U.S. Pat. No. 7,709,493. The compound is believed to be useful in the treatment of diseases and disorders associated with ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/506A61K9/28A61K9/20
CPCA61K31/506A61K9/2806A61K9/2893A61K9/2095A61K9/1623A61K9/1652A61K9/2018A61K9/2054A61P1/04A61P35/00A61P43/00C07D403/12A61K9/16A61K9/2077
Inventor CHEN, JINLINGDEAVER, MATTHEW S.HOLL, RICHARD J.NUGURU, KALYAN
Owner CHEN JINLING
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