Solvay Pharmaceuticals, Gmbh

Duphar International Research Bv

Solvay Pharmaceuticals, B.v.

Johannes A M Van Der Heijden

Cornelis G Kruse

Gerben M Visser

Roelof Van Hes

Bernard J Van Vliet

Martinus T M Tulp

Jacobus Tipker

Gustaaf J M Van Scharrenburg

Roelof W Feenstra

Stephen K Long

Gerrit P Toorop

Johannes Mos

The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine Dreceptor 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 anxiety disorders, depression, Parkinson's disease, and schizophrenia. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein:

Phenylpiperazine

Phenylpiperazines

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, CF, OCF, SCF, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO, &#x2014;Z represents &#x2014;C, &#x2550;C or &#x2014;N, Rand Rindependently 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, CF, OCF, SCF, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy, and salts and prodrugs thereof. It has been found that these compounds have interesting pharmacological properties due to a combination of (partial) agonism towards the members of the dopamine D-receptor subfamily and affinity for relevant serotonin and/or noradrenergic receptors 

Piperazine and piperidine compounds

The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine Dreceptor 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:

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, CF, OCF, SCF, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO, ---Z represents &#x2014;C, &#x2550;C or &#x2014;N, Rand Rindependently 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, CF, OCF, SCF, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy, and salts and prodrugs thereof. It has been found that these compounds have interesting pharmacological properties due to a combination of (partial) agonism towards the members of the dopamine D-receptor subfamily and affinity for relevant serotonin and/or noradrenergic receptors

The invention relates to a group of novel piperazine and piperidine derivatives of formula (I), wherein: S is hydrogen, halogen, alkyl (1-3C), CN, CF , OCF , SCF , alkoxy (1-3C), amino or mono- or dialkyl (1-3C) substituted amino, or hydroxy; X represents NR , S, CH , O, SO or SO , wherein R is H or alkyl (1-3C); . . . Z represents &boxH;C or &mdash;N; &mdash;R independently represent H or alkyl (1-3C), or R and R together can form a bridge 2 or 3 C-atoms; R is hydrogen or alkyl (1-3C); Q is methyl, ethyl, ethyl substituted with one or more fluorine atoms, cyclopropyl&mdash;methyl, optionally substituted with one or more fluorine atoms, and salts and prodrugs thereof. It has been found that these compounds have both partial dopamine D -receptor agonism and partial serotonin 5-HT -receptor agonism mediated activities.

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Weesp, Netherlands

Johannes A M Van Der Heijden