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Application US20200330602
Pharmacytics B.v.

METHOD FOR IMPROVING THE ORAL BIOAVAILABILITY OF A DRUG

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US20200330602

1. A method for increasing the oral bioavailability of a drug HX-DM. wherein HX represents an OH or SH functional group, comprising the step of linking a sugar-carbamoylalkylidene unit of formula (II) ##STR00030## wherein Sugar is selected from the group consisting of alpha- and beta-linked monosaccharides and disaccharides, wherein optionally one or more OH groups are replaced by a group R4 (1) (6)

4. The method according to any one of claims 1 to 3, wherein Sugar is an alpha- or beta-linked monosaccharide or dissacharide, wherein optionally one or more OH groups are replaced by a group R4. (1) (0)

8. The method according to any one of the preceding claims wherein R2 and R3 are both H. (0)

9. The method according to any one of the preceding claims, wherein the drug moiety is selected from the group consisting of quetiapine, montelukast, venlafaxine, mesalazine, desvenlafaxine, metoprolol, paliperidone, buprenorphine, morphine, ganciclovir, tapentadol, rotigotine, abiraterone, acetaminophen, saxagliptin, fulvestrant, afimoxifene, testosterone, simvastatin, tolterodine, tramadol, atenolol, naloxone, nabilone, metaraminol, dihydroartemisinin, orciprenaline, labetalol, kalydeco, azacitidine, niclosamide, tetrahydrocannabinol, raloxifene, propofol, gemcitabine, cannabidiol, carvedilol, edavarone, cytaribine, dasatinib, perrilyl alcohol, butorphanol and bazedoxifene. (0)

10. A compound obtainable by the method of any one of claims 1 to 9 having formula (I) ##STR00033## wherein Sugar is selected from the group consisting of alpha- and beta-linked monosaccharides and disaccharides, wherein optionally one or more OH groups are replaced by a group R4 (1) (7)

13. The compound according to any one of claims 10 to 12, wherein Sugar is an alpha- or beta-linked monosaccharide or dissacharide, wherein optionally one or more OH groups are replaced by a group R4. (1) (0)

17. The compound according to any one of the preceding claims wherein R2 and R3 are both H. (0)

18. The compound according to any one claims 10 to 17, wherein the drug moiety is selected from the group consisting of quetiapine, montelukast, venlafaxine, mesalazine, desvenlafaxine, metoprolol, paliperidone, buprenorphine, morphine, ganciclovir, tapentadol, rotigotine, abiraterone, acetaminophen, saxagliptin, fulvestrant, afimoxifene, testosterone, simvastatin, tolterodine, tramadol, atenolol, naloxone, nabilone, metaraminol, dihydroartemisinin, orciprenaline, labetalol, kalydeco, azacitidine, niclosamide, tetrahydrocannabinol, raloxifene, propofol, gemcitabine, cannabidiol, carvedilol, edavarone, cytaribine, dasatinib, perrilyl alcohol, butorphanol and bazedoxifene. (0)

19. Pharmaceutical composition comprising a compound according to any one of claims 10 to 18 and a pharmaceutically acceptable carrier. (0)
 

20. The compound according to any one of claims 10 to 17 for use as a medicament. (0)



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