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Claims for Patent: 5,196,438

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Claims for Patent: 5,196,438

Title: Amino acid derivatives
Abstract:Compounds having the formula ##STR1## wherein R is benzyloxycarbonyl or 2-quinolylcarbonyl, and their pharmaceutically acceptable acid addition salts inhibit proteases of viral origin and can be used as medicaments for the treatment of prophylaxis of viral infections in mammals, humans or non-humans.
Inventor(s): Martin; Joseph A. (Harpenden, GB2), Redshaw; Sally (Stevenage, GB2)
Assignee: Hoffmann-La Roche Inc. (Nutley, NJ)
Application Number:07/615,534
Patent Claims: 1. A compound having the formula ##STR13## wherein R is benzyloxycarbonyl or 2-quinolylcarbonyl, and its pharmaceutically acceptable acid addition salts.

2. The compound of claim 1, N-tert.butyl-decahydro-2-[2(R)-hydroxy-4-phenyl-3(S)-[[N-(2-quinolylcarbon yl)-L-asparaginyl]amino]butyl]-(4aS,8aS)-isoquinoline-3(S)-carboxamide.

3. The compound of claim 1, N-tert.butyl-decahydro-2-[2(R)-hydroxy-4-phenyl-3(S)-[[N-benzyloxycarbonyl )-L-asparaginyl]amino]butyl]-(4aS,8aS)-isoquinoline-3(S)-carboxamide.

4. A compound having the formula ##STR14##

5. A compound having the formula ##STR15##

6. A pharmaceutical composition which comprises a therapeutically effective amount of a compound having the formula ##STR16## wherein R is benzyloxycarbonyl or 2-quinolylcarbonyl, or a pharmaceutically acceptable acid addition salt thereof, and a therapeutically inert carrier.

7. The pharmaceutical composition of claim 6 wherein in formula I, R is benzyloxycarbonyl.

8. The pharmaceutical composition of claim 6, wherein in formula I, R is 2-quinolylcarbonyl.

9. The pharmaceutical composition of claim 6, which is present in an amount effective to control viral infections.

10. The pharmaceutical composition of claim 6, wherein the amount of said compound of formula I is from about 3 mg to about 3000 mg.

11. The pharmaceutical composition of claim 10, wherein the amount of said compound of formula I is from about 10 mg to about 1000 mg.

12. The pharmaceutical composition of claim 6 which is in unit dosage form.

13. The pharmaceutical composition of claim 12 wherein the amount of compound of formula I is from about 10 mg to about 1000 mg.

14. The pharmaceutical composition of claim 12 wherein said unit dosage form is selected from the group consisting of tablets, coated tablets, dragees, hard gelatin capsules, soft gelatin capsules, solutions, emulsions, suspensions, syrups, sprays, and suppositories.

15. A method for treating a mammal having viral infections, which comprises administering to said mammal a compound having the formula ##STR17## wherein R is benzyloxycarbonyl or 2-quinolylcarbonyl, or a pharmaceutically acceptable acid addition salt thereof in an amount which is effective in treating viral infections.

16. The method of claim 15 wherein, in formula I R is benzyloxycarbonyl.

17. The method of claim 15 wherein, in formula I R is 2-quinolylcarbonyl.
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