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Claims for Patent: 4,598,089

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Claims for Patent: 4,598,089

Title: Leucine derivatives
Abstract:Novel compounds of the formula ##STR1## wherein A signifies the group ##STR2## or --(CH.sub.2).sub.5 --, which inhibit pancreas lipase and can be used for the control or prevention of obesity and hyperlipaemia, are disclosed. The inventive compounds can be produced by the cultivation of microorganism Streptomyces toxytricini, identified as NRRL 15443.
Inventor(s): Hadvary; Paul (Biel-Benken, CH), Hochuli; Erich (Arisdorf, CH), Kupfer; Ernst (Basel, CH), Lengsfeld; Hans (Reinach, CH), Weibel; Ernst K. (Pratteln, CH)
Assignee: Hoffmann-La Roche Inc. (Nutley, NJ)
Application Number:06/621,827
Patent Claims: 1. A compound of the formula ##STR12## wherein A is the group ##STR13## or --(CH.sub.2).sub.5 --.

2. The compound of claim 1, (2S,3S,5S,7Z,10Z)-5-[(S)-2-formamido-4-methyl-valeryloxy]-2-hexyl-3-hydrox y-7,10-hexadecadienoic 1,3 acid lactone.

3. The compound of claim 1, (2S,3S,5S)-5-[(S)-2-formamido-4-methyl-valeryloxy]-2-hexyl-3-hydroxy-hexad ecanoic 1,3 acid lactone.

4. A pharmaceutical composition for administration to a patient comprising

(a) about 5% to about 95% of a compound of formula ##STR14## wherein A is the group ##STR15## or --(CH.sub.2).sub.5 -- said composition being present in a amount sufficient to supply about 0.1 to about 100 mg of compound I per kilogram of body weight of the patient per day; and

(b) 5% to 95% of a pharmaceutically acceptable inert carrier material, said composition being formulated in a unit dosage form.

5. The composition of claim 4 wherein said composition is formulated in an oral unit dosage form.

6. The composition of claim 5 wherein said oral unit dosage form is a tablet, dragee, capsule, solution, emulsion or suspension.

7. The composition of claim 4 wherein compound I is (2S,3S,5S,7Z,10Z)-5-[(S)-2-formamido-4-methyl-valeryloxy]-2-hexyl-3-hydrox y-7,10-hexadecadienoic 1,3 acid lactone.

8. The composition of claim 4 wherein compound I is (2S,3S,5S)-5-[(S)-2-formamido-4-methyl-valeryloxy]-2-hexyl-3-hydroxy-hexad ecanoic 1,3 acid lactone.

9. A method of treating obesity in an afflicted mammal comprising administering to the mammal a compound of the formula ##STR16## wherein A is the group ##STR17## or --(CH.sub.2).sub.5 -- in an amount which is effective in treating obesity.

10. The method of claim 9 wherein compound I is (2S,3S,5S,7Z,10Z)-5-[(S)-2-formamido-4-methyl-valeryloxy]-2-hexyl-3-hydrox y-7,10-hexadecadienoic 1,3 acid lactone.

11. The method of claim 9 wherein compound I is (2S,3S,5S)-5-[(S)-2-formamido-4-methyl-valeryloxy]-2-hexyl-3-hydroxy-hexad ecanoic 1,3 acid lactone.

12. The method of claim 9 wherein compound I is administered in a daily dose of about 0.1 mg to 100 mg/kg body weight of the mammal.

13. A method of treating hyperlipaemia in an afflicted mammal comprising adminstering to the mammal a compound of the formula ##STR18## wherein A is the group ##STR19## or --(CH.sub.2).sub.5 --, in an amount which is effective in treating hyperlipaemia.

14. The method of claim 13 wherein compound I is (2S,3S,5S,7Z,10Z)-5-[(S)-2-formamido-4-methyl-valeryloxy]-2-hexyl-3-hydrox y-7,10-hexadecadienoic 1,3 acid lactone.

15. The method of claim 13 wherein compound I is (2S,3S,5S)-5-[(S)-2-formamido-4-methyl-valeryloxy]-2-hexyl-3-hydroxy-hexad ecanoic 1,3 acid lactone.

16. The method of claim 13 wherein compound I is administered in a daily dose of about 0.1 mg to 100 mg/kg body weight of the mammal.

17. A method of preventing obesity in a mammal comprising administering to the mammal a compound of the formula ##STR20## wherein A is the group ##STR21## or --(CH.sub.2).sub.5 --, in an amount which is effective in preventing obesity by inhibiting pancrease lipase.

18. The method of claim 17 wherein compound I is (2S,3S,5S,7Z,10Z)-5-[(S)-2-Formamido-4-methyl-valeryloxy]-2-hexyl-3-hydrox y-7,10-hexadecadienoic 1,3 acid lactone.

19. The method of claim 17 wherein compound I is (2S,3S,5S)-5-[(S)-2-formamido-4-methyl-valeryloxy]-2-hexyl-3-hydroxy-hexad ecanoic 1,3 acid lactone.

20. The method of claim 17 wherein compound I is administered in a daily dose of about 0.1 mg to 100 mg/kg body weight of the mammal.
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