Abstract: The present invention relates to novel identified polynucleotides, polypeptides encoded by them and to the use of such polynucleotides and polypeptides, and to their production. More particularly, the polynucleotides and polypeptides of the present invention relate to the G-protein coupled receptor family, referred to as IGS4-family. The invention also relates to inhibiting or activating the action of such polynucleotides and polypeptides, to a vector containing said polynucleotides, a host cell containing such vector and transgenic animals where the IGS4-gene is either overexpressed, misexpressed, underexposed or suppressed (knock-out animals).

Abstract: The present invention relates to a group of novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CB1 receptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I) wherein R and R1–R4 have the meanings given in the specification.

Abstract: This invention relates to newly identified polypeptides which have zinc metalloprotease activities and are referred to as IGS5, and polynucleotides encoding such polypeptides, to their use in therapy and in identifying compounds which may be stimulators and/or inhibitors which are useful in therapy, and to production of such polypeptides and polynucleotides.

Abstract: The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity.

Abstract: This invention relates to newly identified polypeptides which have zinc metalloprotease activities and are referred to as IGS5, and polynucleotides encoding such polypeptides, to their use in therapy and in identifying compounds which may be stimulators and/or inhibitors which are useful in therapy, and to production of such polypeptides and polynucleotides.

Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition, disturbances of memory, Parkinson's disease, schizophrenia, and psychotic disorders. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0–2; R5 and R6 are independently H or alkyl (1–3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3–5, and R7 is alkyl (1–3C), alkoxy (1–3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2–4, and salts thereof.

Abstract: The invention relates to the mesylates of a group of piperazine derivatives and to a process for the preparation of these mesylates in an economic way in the high yield and of high purity. According to the process of the invention the synthesis of the piperazine ring and the mesylate formation are combined in a single reaction step.

Abstract: A method for preparing an imidazolyl compound corresponding to the formula (I) by reacting a compound corresponding to formula (II) with a compound corresponding to formula (III) and then reacting the product with a compound corresponding to formula (IV)

Abstract: The present invention relates to 2-substituted-6-trifluoromethyl purine derivatives as selective adenosine antagonists, in particular adenosine-A3 receptor antagonists, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said purine derivatives. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.

Abstract: The present invention relates to novel identified polynucleotides, polypeptides encoded by them and to the use of such polynucleotides and polypeptides, and to their production. More particularly, the polynucleotides and polypeptides of the present invention relate to the G-protein coupled receptor family, referred to as IGS4-family. The invention also relates to inhibiting or activating the action of such polynucleotides and polypeptides, to a vector containing said polynucleotides, a host cell containing such vector and transgenic animals where the IGS4-gene is either overexpressed, misexpressed, underexpressed or suppressed (knock-out animals).

Abstract: The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (Ia) or (Ib) wherein the symbols have the meanings given in the specification.

Abstract: The present invention relates to novel identified polynucleotides, polypeptides encoded by them and to the use of such polynucleotides and polypeptides, and to their production. More particularly, the polynucleotides and polypeptides of the present invention relate to the G-protein coupled receptor family, referred to as IGS4-family. The invention also relates to inhibiting or activating the action of such polynucleotides and polypeptides, to a vector containing said polynucleotides, a host cell containing such vector and transgenic animals where the IGS4-gene is either overexpressed, misexpressed, underexpressed or suppressed (knock-out animals).

Abstract: The present invention relates to novel identified polynucleotides, polypeptides encoded by them and to the use of such polynucleotides and polypeptides, and to their production. More particularly, the polynucleotides and polypeptides of the present invention relate to the G-protein coupled receptor family, referred to as IGS4-family. The invention also relates to inhibiting or activating the action of such polynucleotides and polypeptides, to a vector containing said polynucleotides, a host cell containing such vector and transgenic animals where the IGS4-gene is either overexpressed, misexpressed, underexpressed or suppressed (knock-out animals).

Abstract: The present invention relates to novel identified polynucleotides, polypeptides encoded by them and to the use of such polynucleotides and polypeptides, and to their production. More particularly, the polynucleotides and polypeptides of the present invention relate to the G-protein coupled receptor family, referred to as IGS4-family. The invention also relates to inhibiting or activating the action of such polynucleotides and polypeptides, to a vector containing said polynucleotides, a host cell containing such vector and transgenic animals where the IGS4-gene is either overexpressed, misexpressed, underexpressed or suppressed (knock-out animals).

Abstract: The invention relates to the novel mesylate of a phenylpiperazine derivative of the formula (I). This salt has favorable properties as compared with the free base of this compound.

Abstract: Thiophenepyrimidinone compounds and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring inhibition of 17?-hydroxysteroid dehydrogenase enzymes.

Abstract: The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO2, ---Z represents —C, ?C or —N, R1 and R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- or 4-pyridylmethyl, wich groups may be substited with one or more more substituents from the group halogen, nitro, cyano, amino, mono- or di (1-3C)alkylamino, (1-3C) alkoxy, CF3, OCF3, SCF3, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy, and salts and prodrugs thereof.

Abstract: Thiophenepyrimidinone compounds and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring inhibition of 17?-hydroxysteroid dehydrogenase enzymes.

Abstract: Pharmaceutically acceptable metal salts of compounds of formula (I): in which R1 is selected from the group consisting of (C1-C6)alkoxy(C1-C6)alkyl which may be substituted with (C1-C6)alkoxy, phenyl-(C1-C6)-alkyl and/or phenyloxy-(C1-C6)-alkyl group in which any phenyl group may be substituted with (C1-C6)alkyl, (C1-C6)alkoxy or halogen, and naphtyl-(C1-C6)-alkyl; R2 and R3 are each independently hydrogen or halogen; R4 is a biolabile ester forming group; and in which the salt is selected from the lithium salt and salts of bivalent metal ions such as magnesium, calcium and zinc.

Abstract: This invention relates to newly identified polypeptides which have zinc metalloprotease activities and are referred to as IGS5, and polynucleotides encoding such polypeptides, to their use in therapy and in identifying compounds which may be stimulators and/or inhibitors which are useful in therapy, and to production of such polypeptides and polynucleotides.