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Genvoya tablet

IP.com Disclosure Number: IPCOM000248781D
Publication Date: 2017-Jan-10
Document File: 2 page(s) / 20K

Publishing Venue

The IP.com Prior Art Database

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1

Genvoya 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 Genvoya tablet (Lot No. -WPWK, Expiry date: June 2018, GILEAD, US

market):

One Genvoya tablet was weighed, grinded to a powder and dissolved by sonication for 10 min in 75 ml

of diluent (60% 0.01M Ammonium Acetate : 40%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-

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

diphenylhexan-2-yl]carbamate, %

Impurity Profile , RRT , % on area

1.00 0.86 0.98 1.07 1.16 1.18

99.0 0.06 0.61 0.07 0.14 0.08

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 the

Genvoya tablet (Lot No. -WPWK, Expiry date: June 2018, GILEAD, US market):

was determined to be less than 0.62 %;

N

S

N

O

N H O

H N

Ph

N H

O

O N S

Ph N

O

2

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

thiazol-4-yl]methyl}carbamoyl)amino]-4-(morpholin-4-yl)butanoyl]amino}-1,6-di...