Duphar International Research Bv

Bartholomeus J Van Steen

Cornelis G Kruse

Martinus T M Tulp

Gerben M Visser

Jacobus A J Den Hartog

Eric Ronken

Josephus H M Lange

Jan Hartog

Johannes Mos

Jacques Schipper

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

The present invention is concerned with compounds having 5-HT1A antagonistic activity useful in treating CNS disorders and having formula 2 ##STR1## wherein R.sub.1 is halogen, lower alkyl or alkoxy, hydroxy, trifluotomethyl or cyano,

2,3-dihydro-1,4-benzodioxin-5-yl-piperazine derivatives having 5-HT

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Weesp, Netherlands

Bartholomeus J Van Steen