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Tybost tablet

IP.com Disclosure Number: IPCOM000244189D
Publication Date: 2015-Nov-22
Document File: 2 page(s) / 275K

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Page 01 of 2

Tybost tablet

1,3-thiazol-5-ylmethyl [(2R,5R)-5-{[(2S)-2-[(methyl{[2-(propan-2-yl)-1,3-thiazol-4- yl]methyl}carbamoyl)amino]-4-(morpholin-4-yl)butanoyl]amino}-1,6-diphenylhexan-2-yl]carbamate has the following chemical structure:

Chromatographic purity of Tybost tablet (Lot No. -61184901 KVXFD, Expiry date: February 2015,

Gilead Sciences Intl Ltd, EU market):

One Tybost tabletwas weighed, grinded to a powder and dissolved by sonication for 10 min in 100 ml of diluent (75% 0.15% TFA in Water: 25%Acetonitrile). The resulting solution was filtered and injected into the HPLC system.

The obtained purity results are as follows:

Purity of: 1,3-thiazol-5-ylmethyl [(2R,5R)-5-

{[(2S)-2-[(methyl{[2-(propan-2-yl)-1,3-

thiazol-4-yl]methyl}carbamoyl)amino]-4-

Impurity Profile , RRT , % on area

(morpholin-4-yl)butanoyl]amino}-1,6-

diphenylhexan-2-yl]carbamate, %


1.00


0.69 0.87 0.92 0.98 1.03 1.19 1.21


98.8


0.03 0.06 0.04 0.70 0.09 0.03 0.09

The content of the most prominent diasteriomer 1,3-thiazol-5-ylmethyl [(2R,5R)-5-{[(2R)-2- [(methyl{[2-(propan-2-yl)-1,3-thiazol-4-yl]methyl}carbamoyl)amino]-4-(morpholin-4- yl)butanoyl]amino}-1,6-diphenylhexan-2-yl]carbamate, as depicted in the picture below, in Tybost tablet (Lot No. -61184901 KVXFD, Expiry date: February 2015, Gilead Sciences Intl Ltd, EU market)

was determined to be less than 0.71 %;

N

S

O

N

Ph

N O

NH O

HN

Ph

NH O

O N S

1


Page 02 of 2

The content of enantiomer 1,3-thiazol-5-ylmethyl [(2S,5S)-5-{[(2R)-2-[(methyl{[2-(pro...