Duphar International Research Bv

Solvay Pharmaceuticals, Gmbh

Solvay Pharmaceuticals, B.v.

Gerben M Visser

Cornelis G Kruse

Martinus T M Tulp

Johannes A M Van Der Heijden

Roelof Van Hes

Bernard J Van Vliet

Jacobus Tipker

Jacobus A J Den Hartog

Eric Ronken

Roelof W Feenstra

Stephen K Long

Bartholomeus J Van Steen

Gerrit P Toorop

Josephus H M Lange

Gustaaf J M Van Scharrenburg

Johannes Mos

Jan H Reinders

Johannes W C M Jansen

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 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 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.

Piperazine and piperidine compounds

3-Tetrahydropyridin-4-yl indoles for treatment of psychotic disorders

The present invention relates to novel compounds, to a method for the preparation of these novel compounds, to pharmaceutical compositions containing one or more of these compounds as an active component and to methods of using these in the treatment of stress-related disorders.

Quinoline and quinazoline derivatives having corticotropin releasing factor (CRF) antagonist activity

The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R ) represents 0, 1, or 2 substituents, which can be the same or different, from the group C -alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino mono- or dialkyl (C )-amino, sulfonyl-(C )alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C )-amino, X is O, S, NH or NCH , Y represents CH , or (CH ) , (R ) represents 0, 1, or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R ) is a methylene bridge or ethylene bridge, A is a group &mdash;CH &mdash;(CRH) &mdash; wherein R is hydrogen or methyl and p is 0 or 1, and B represents 2- or 3-indolyl or 2-benzimidazolyl, which groups may be substituted at carbon with 1 or 2 substituents from the group C- -alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, mono- or dialkyl (C )amino, sulfonyl-(C )alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C )-amino.

Benzisoxazole derivatives having d4-antagonistic activity

The present invention relates to a group of novel 2-aminoquinoline derivatives which are potent and selective agonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R,),represents 1 or 2 substituents, which can be the same or different, from the group C,-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C,)amino, or two groups R,at adjacent carbon atoms together with the benzene ring may form the benzdioxane group or benzofuran group, X represents nitrogen or carbon, and the dotted line may represent a double bond, (R,),represents 0, 1 or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R,),is a methylene bridge or ethylene bridge, R,is hydrogen or methyl, and (R),represents 0, 1, or 2 substituents, which can be the same or different and can be located at all available positions of the quinolyl group, from the group C,-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C,)amino, on the understanding that R,cannot represent o-OCH,when X is nitrogen, (R,),and R,are hydrogen, m is 0 and n is 1

2-aminoquinoline derivatives having d4-agonistic activity

Novel piperazine and piperidine derivative compounds having interesting and advantageous pharmacological properties. The disdosed compounds have the general formula (a)

Piperazine compounds, their preparation, and methods of using them

Growing community of inventors

Weesp, Netherlands

Gerben M Visser