2-(substituted-amino)-benzothiazole sulfonamide HIV protease inhibitors
View Patent ↗The present invention relates to 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broad-spectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.
1. A compound having the formula (I)
a salt, stereoisomeric form or stereoisomeric form thereof wherein
R is a piperidine ring substituted on the N-atom in the ring by C 3-7 cycloalkyl.
2. A compound according to claim 1 wherein C 3-7 cycloalkyl is C 5 -cycloalkyl.
3. A compound according to claim 2 having the formula (II)
4. A pharmaceutical composition comprising an effective amount of at least one compound as claimed in claim 1 and a pharmaceutically tolerable excipient.
5. A composition comprising at least (a) a compound of formula (I) as claimed in claim 1 and, (b) a second antiretroviral agent for the simultaneous, separate or sequential use.
6. A composition according to claim 5 wherein the second agent is ritonavir.
7. A composition according to claim 6 wherein the compound of formula II is (1-benzyl-3-{[2-(1-cyclopentyl-piperidin-4-ylamino)-benzothiazole-6-sulfonyl]-isobutyl-amino}-2-hydroxy-propyl)-carbamic acid hexahydro-furo[2,3-b]furan-3-yl ester.
8. A method of inhibiting a protease of a multi-drug resistant retrovirus in a mammal infected with said retrovirus comprising administering a protease-inhibiting amount of a compound according to claim 1 to said mammal in need thereof.
9. A method of treating or combating infection or disease associated with multi-drug resistant retrovirus infection in a mammal comprising administering an effective amount of at least one compound according to claim 1 to said mammal.
10. A method of inhibiting multi-drug resistant retroviral replication comprising contacting a retrovirus with an effective amount of at least one compound according to claim 1 .