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US 7,094,909 B2Granted
HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
AssigneeAgouron Pharmaceuticals, Inc.
InventorsDavid John Kucera, Robert William Scott
Life of this patent
Estimating the term…
Abstract
The present invention concerns processes for preparing compounds of formula (I-H), or a prodrug, pharmaceutically active metabolite, or pharmaceutically active salt or solvate thereof, which are useful as inhibitors of the HIV protease enzyme.
Claims16
A process for preparing a compound of formula (I-H), or a prodrug, or pharmaceutically active salt or solvate thereof,
- wherein:
- R1 is a 5- or 6-membered mono-cyclic carbocyclic or heterocyclic group, wherein said carbocyclic or heterocyclic group is saturated, partially unsaturated or fully unsaturated and is optionally substituted by at least one substituent chosen from C1-6 alkyl, hydroxyl, C1-6 alkylcarbonyloxy, C6-10 arylcarbonyloxy, and heteroarylcarbonyloxy;
- R2 is C1-6 alkyl substituted with at least one halogen;
- and
- R4, R5, R6 and R7 are independently chosen from H and C1–C6 alkyl;
- comprising:
- reacting a compound of formula (II), wherein Y1 is hydroxyl or a leaving group, with a compound of formula (III), or a salt or solvate thereof,
4 more elements
A process for preparing a compound of formula (I-J),
- comprising:
- reacting a compound of formula (II-A) with a compound of formula (III-A).
A process for preparing a compound of formula (I-K),
- comprising:
- (i) reacting a compound of formula (II-A) with a compound of formula (III-A),
- to afford a compound of formula (I-J);
- and
- (ii) deprotecting the compound of formula (I-J).
2 more elements
Dependencies are inferred from the claim text.