Treatment of vasodilatory headache

Details Treatment of vasodilatory headache Treatment of vasodilatory headache

A - Human Necessities

61

K

A61K 31/00 (2006.01) A61K 31/403 (2006.01) A61P 25/06 (2006.01)

Patent

CA 2340117

A cerebral-selective anti-vasodilator e.g. of formula (I) for use in clinical conditions other than migraine resulting from undesired vasodilatation in the cerebral vasculature, wherein: R1 represents hydrogen, halogen, trifluoromethyl, nitro, hydroxy, C1-6alkyl, C1-6alkoxy, arylC1-6alkoxy, - CO2R4, -(CH2)nCN, -(CH2)nCONR5R6, -(CH2)nSO2NR5R6, C1-6alkanoylamino(CH2)n, or C1-6alkylsulphonyl-amino(CH2)n; R4 represents hydrogen, C1-6alkyl or arylC1- 6alkyl; R5 and R6 each independently represents hydrogen or C1-6alkyl, or R5 and R6 together with the nitrogen atom to which they are attached form a ring; n represents 0, 1 or 2; and R2 and R3 each independently represent hydrogen, C1-6alkyl or benzyl or together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or hexahydroazepino ring; and physiologically are acceptable salts thereof.

L'invention concerne un anti-vasodilatateur, cérébral, par exemple correspondant à la formule (I), utile dans des conditions cliniques autres que celles de la migraine et résultant d'une vasodilatation non souhaitée se produisant dans le système vasculaire cérébral. Dans cette formule R?1¿ représente hydrogène, halogène, trifluorométhyle, nitro, hydroxy, alkyle C¿1-6?, alcoxy C¿1-6?, aryl-alcoxy C¿1-6?, -CO¿2?R?4¿, -(CH¿2?)¿n?CN, -(CH¿2?)¿n?CONR?5¿R?6¿, -(CH¿2?)¿n?SO¿2?NR?5¿R?6¿, alcanoylamino C¿1-6?(CH¿2?)¿n?, ou alkylsulfonylamino C¿1-6?(CH¿2?)¿n?; R?4¿ représente hydrogène, alkyle C¿1-6?, ou aryl-alkyle C¿1-6?; R?5¿ et R?6¿ représentent chacun indépendamment hydrogène ou alkyle C¿1-6?, ou bien, ensemble, avec l'atome d'azote auquel ils sont liés, ils forment un noyau; n représente 0, 1 ou 2; et R?2¿ et R?3¿ représentent chacun indépendamment hydrogène, alkyle C¿1-6?, ou benzyle, ou bien, ensemble, avec l'atome d'azote auquel ils sont liés, ils forment un noyau pyrrolidino, pipéridino ou hexahydroazépino. L'invention concerne également des sels de ce composé, acceptables sur le plan physiologique.

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