C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 405/04 (2006.01) A61K 31/35 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07D 241/04 (2006.01) C07D 295/096 (2006.01) C07D 311/06 (2006.01) C07D 311/08 (2006.01) C07D 311/18 (2006.01) C07D 403/06 (2006.01) C07D 405/06 (2006.01) C07D 405/14 (2006.01) C07D 413/06 (2006.01) C07D 413/14 (2006.01)
Patent
CA 2134630
Abstract The invention relates to a group of new 1-[2H-1-benzopyran-2-one-8-yl]-piperazine derivatives having interesting pharmacological properties due to 5-HT1A agonism and 5-HT10-antagonism. The compounds have the general formula (1) (1) Image wherein - R1 is alkyl (1-4C), alkoxy (1-4C), hydroxy, alkoxy(1-4C)alkyl(1-4C), pyrrolidinyl, piperidinyl, morpholinyl, halogen, cyano, trifluoromethyl, amino, or mono- or disubstituted amino wherein the substituents are alkyl (1-4C), or alkyl(1- 4C)carbonyl, - m has the value 0, 1 or 2, - R2 is alkyl (1-4C), alkoxy (1-4C), halogen or trifluoromethyl, - n is 0 or 1, on the understanding that m + n is at least 1, - R3 is hydrogen, alkyl (1-3C) or alkenyl (2-3C), - R4 is alkyl (1-4C), and - p has the value 0, 1 or 2, and pharmaceutically acceptable acid addition salts thereof. The compounds can be used for the treatment of affections or diseases of the central nervous system caused by disturbances of the serotonergic transmission.
Hartog Jan
Schipper Jacques
Van Der Heyden Johannes Anthonius Maria
Van Steen Bartholomeus Johannes
Duphar International Research B.v.
Fetherstonhaugh & Co.
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