Merck + Co., Inc.

Christine Stelmach

Andrew S Thompson

Steven D Young

Louis S Crocker

Joseph Kukura, Ii

Ashok V Katdare

Drazen Ostovic

Chung Y Lui

The instant invention describes a method for crystallizing (&#x2212;)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one from a solvent and anti-solvent solvent system and producing the crystalline product. The desired final crystal form, Form I, can be produced when using methanol or ethanol. Form II is isolated from 2-propanol and can be converted to the desired crystal form at low drying temperatures, such as between about a temperature of 40&#xb0; C. and 50&#xb0; C.

Crystal forms of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one

This invention relates to a dry granulation capsule formulation of the HIV protease inhibitor, indinavir sulfate, which is useful in the treatment of AIDS, ARC or HIV infection. Processes for making the oral formulation are also disclosed.

Dry granulation formulation for an HIV protease inhibitor

The instant invention describes a method for crystallizing (&minus;)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one from a solvent and anti-solvent system and producing the crystalline product. The desired final crystal form, Form I, can be produced when using methanol or ethanol. Form II is isolated from 2-propanol and can be converted to the desired crystal form at low drying temperatures, such as between about a temperature of 40&deg; C. and 50&deg; C.

Crystal Forms of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one

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Westfield, NJ, United States of America

Christine Stelmach