Duphar International Research Bv

Abbvie Bahamas Limited

Solvay Pharmaceuticals, B.v.

Eric Ronken

Cornelis G Kruse

Martinus T M Tulp

Gerben M Visser

Jacobus A J Den Hartog

Adrian Hobson

Wouter I Iwema Bakker

Hein K A C Coolen

Axel Stoit

Bartholomeus J Van Steen

Jurjen Frankena

Elizabeth Van Der Kam

Harmen Mons

Josephus H M Lange

Gustaaf J M Van Scharrenburg

Roelof W Feenstra

Andrew C McCreary

Gerrit P Toorop

Johannes W C M Jansen

Jan H Reinders

Hein Kac Coolen

Hein KAC Coolen

Van Der Elizabeth Kam

The present disclosure relates to (thio)morpholine derivatives of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof; with the proviso that the derivative of formula (I) is not 2-(4-ethylphenyl)-4-morpholinoethanol or 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.

(Thio)morpholine derivatives as S1P modulators

The present disclosure relates to (thio)morpholine derivatives of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof; with the proviso that the derivative of formula (I) is not 2-(4-ethylphenyl)-4-morpholinoethanol or 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the disclosure have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.

The invention relates to novel phenylpiperazine derivatives of the formula wherein: &mdash;R represents the group (a) or (b) as indicated in the description. These compounds are (partial) D2 receptor agonists and are usefull for treating CNS disorders, in particular Parkinson's disease.

Phenylpiperazines

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

Growing community of inventors

Weesp, Netherlands

Eric Ronken