Abstract: The present invention provides a method for enhancing the specific uptake of a neurotoxin polypeptide into cells, the method comprising: incubating cells susceptible to neurotoxin intoxication with a neurotoxin polypeptide for a time and under conditions which allow for the neurotoxin polypeptide to exert its biological activity, the incubation comprising at least one of the following steps: (i) K+-mediated depolarization of the cells, (ii) a reduced neurotoxin polypeptide exposition time and/or (iii) agitation of the cells during neurotoxin polypeptide exposition, thereby enhancing the specific uptake of the neurotoxin polypeptide into said cells.

Abstract: The present invention provides a method for enhancing the specific uptake of a neurotoxin polypeptide into cells, the method comprising: incubating cells susceptible to neurotoxin intoxication with a neurotoxin polypeptide for a time and under conditions which allow for the neurotoxin polypeptide to exert its biological activity, the incubation comprising at least one of the following steps: (i) K+-mediated depolarization of the cells, (ii) a reduced neurotoxin polypeptide exposition time and/or (iii) agitation of the cells during neurotoxin polypeptide exposition, thereby enhancing the specific uptake of the neurotoxin polypeptide into said cells.

Abstract: Substituted pyrazolopyrimidine derivatives of formula (I) wherein Y1, Y2, Y3, Y4 represent N or C—, whereby at least two of the groups Y1 to Y4 represent a carbon atom, R1 represents chloro or bromo, R2 to R7 represent e.g. hydrogen, methyl or ethyl; and R10 and R11 independently represent e.g. hydrogen or C1-C6alkyl, are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.

Abstract: Substituted pyrazolopyrimidine derivatives of formula (I) wherein Y1, Y2, Y3, Y4 represent N or C—, whereby at least two of the groups Y1 to Y4 represent a carbon atom, R1 represents chloro or bromo, R2 to R7 represent e.g. hydrogen, methyl or ethyl; and R10 and R11 independently represent e.g. hydrogen or C1-C6alkyl, are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.

Abstract: The invention relates to pyrazolopyrimidine derivatives of formula (I) wherein Y1, Y2 and Y3 independently are e.g. CR10, NH, S or O, whereby at least one of Y1, Y2 and Y3 represents CR10; R1 represents chloro or bromo; R2, R3, R4, R5, R6 and R7 represent e.g. hydrogen or C1-C6-alkyl, and R10 represents e.g. hydrogen, halogen or phenyl; which are potent mGluR5 modulators and are e.g. useful for the treatment of various neurological disorders.

Abstract: The invention relates to ethynyl-substituted tetrahydroquinolinone derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are group I mGluR modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.

Abstract: The invention relates to ethynyl-substituted tetrahydroquinolinone derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are group I mGluR modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.

Abstract: The invention relates to pyrazolopyrimidine derivatives of formula (I) wherein Y1, Y2 and Y3 independently are e.g. CR10, NH, S or O, whereby at least one of Y1, Y2 and Y3 represents CR10; R1 represents chloro or bromo; R2, R3, R4, R5, R6 and R7 represent e.g. hydrogen or C1-C6-alkyl, and R10 represents e.g. hydrogen, halogen or phenyl; which are potent mGluR5 modulators and are e.g. useful for the treatment of various neurological disorders.

Abstract: Substituted pyrazolopyrimidine derivatives of formula (I) wherein Y1, Y2, Y3, Y4 represent N or C—, whereby at least two of the groups Y1 to Y4 represent a carbon atom, R1 represents chloro or bromo, R2 to R7 represent e.g. hydrogen, methyl or ethyl; and R10 and R11 independently represent e.g. hydrogen or C1-C6alkyl, are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.

Abstract: Substituted pyrazolopyrimidine derivatives of formula (I) wherein R1 represents chloro or bromo; R2, R3, R4, R5, R6 and R7 independently represent e.g. hydrogen or C1-6-alkyl; R8 represents a radical R9 or a radical R10, whereby one of the two radicals R8 represents R9 and the other radical R8 represents Ret; R9 represents e.g. a phenyl or thiophene group, and R10 represents e.g. hydrogen or methyl; are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.