Kemin Pharma B.v.b.a.

Kemin Pharma Europe B.v.b.a.

Universiteit Gent

Johan Van Der Eycken

Benedikt J Sas

Jan Vandenkerckhove

Johan Van Hemel

Eric Peys

Bart Ruttens

Petra Blom

Steven Van Hoof

Jan Balzarini

Johan Neyts

Jelle Cornelus

Dries Van Den Bossche

Gert Smans

Nick Jacobs

Eric De Clercq

The present invention provides new therapeutic compounds for treatment of diseases caused or influenced by microtubule stability, such as proliferative diseases. The compounds are phenyl-analogs of the naturally occurring peloruside. The analogs are easier to synthesize, and hence open up the possibility to produce said compounds in large quantities for therapeutic use.

Peloruside analogs

Novel carbohydrate-based compounds with an attached ring system that have antimicrobial or cytostatic activity. The compounds are administered to humans and animals for the treatment or amelioration of bacterial, fungal, viral or protozoal infections or tumors. The compounds are of the general formula: 

Preparation and use of carbohydrate-based bicyclic ring structures with antimicrobial and cytostatic activity

The synthesis and study of biological activity of a series of new molecules with potential antimicrobial activity are described. The molecules are bicyclic carbohydrates, based on furanose sugars. Their antimicrobial activity against viruses is demonstrated, next to cytostatic effects. Significantly, a high and selective activity against Cytomegalovirus was observed.

Furanose-type bicyclic carbohydrates with biological activity

The use of bicyclic carbohydrates for the treatment of parasite infections is described. Different bicyclic carbohydrates have been tested in vitro against a number of protozoa. These compounds also have been screened against viruses, tumors, bacteria and fungi. Compound A1, a thiophenyl-containing bicyclic carbohydrate possessed significant activity against, a parasite that causes the lethal sleeping sickness. Compound A2 and Compound A3, bicyclic carbohydrates with halogen containing aryl groups, possessed significant activity against, a parasite that causes leishmaniasis. Bicyclic carbohydrates in general, and Compound A1, Compound A2 and Compound A3 more specifically, could be possible treatments for the sleeping sickness and leishmaniasis in the future.

Bicyclic carbohydrates as antiprotozoal bioactive for the treatment of infections caused by parasites

We describe the use of bicyclic carbohydrates for the treatment of hepatitis C virus infections. Different bicyclic carbohydrates were tested in vitro against DNA-viruses, retro-viruses andsp., an important family of human and animal RNA pathogens. Significant activity was observed against the bovine viral diarrhea virus (BVDV). As pestiviruses, such as BVDV, share many similarities with hepatitis C virus (HCV), the bicyclic carbohydrates in general and the preferred bicyclic carbohydrates more specifically are expected to be a treatment for hepatitis C viral infections.

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Bicyclic carbohydrates for the treatment of infections caused by herpseviridae, and in particular cytomegalovirus. The invention consists of the novel bicyclic carbohydrates the generic structure of which is: wherein Ris either -Bn or -Ph; Rand Rare either -alkyl, -aryl, -allyl, or &#x2014;H; Rand Rform a ring and are either &#x2014;CH(Ph)- or &#x2014;CH(aryl)- and X is either O, N or S.

Bicyclic carbohydrate compounds useful in the treatment of infections caused by herpesviridae

Novel bicyclic carbohydrate compounds are effective for the prophylaxis and treatment of diseases caused by infections of the alphaherpesvirinae HSV-1 and HSV-2. The invention includes the compound wherein X, X, and Xare selected from the group consisting of O, N, and S; wherein Yand Yare selected from the group consisting of O, N, and S; and wherein Z is selected from the group consisting of F, Cl, and Br, as well as analogs, prodrugs and pharmaceutically acceptable salts thereof, together with pharmaceutical compositions for the prophylaxis and treatment of diseases caused by infections of alphaherpesvirinae.

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Ninove, Belgium

Johan Van Der Eycken