5-isoquinolinesulfonamide compounds

Details 5-isoquinolinesulfonamide compounds 5-isoquinolinesulfonamide compounds

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01) A61K 31/4725 (2006.01) A61P 27/06 (2006.01) A61P 43/00 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01)

Patent

CA 2621181

A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G1 represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G2 represents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, and the like; G3 represents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, and the like; G4 represents hydroxyl group, or - N(R1)(R2)(R1 and R2 represent hydrogen atom, an alkyl group, an aralkyl group, an alkenyl group, an alkynyl group, or a saturated heterocyclic group); G5 is a substituent on a ring-constituting carbon atom of A, and represents hydrogen atom, fluorine atom, or an alkyl group] or a salt thereof, or a derivative thereof that is a prodrug, which potently inhibits phosphorylation of the myosin regulatory light chain. (see formula 1)

Composé représenté par la formule (1) [dans laquelle A représente un cycle azoté saturé ; m est un nombre entier de 0-2 ; n est un nombre entier de 1-4 ; G1 représente un hydrogène, un chlore, un hydroxy, un alcoxy ou un amino ; G2 représente un halogéno, un hydroxy, un cyano, un carboxy, un alkyle, un alcényle, etc. ; G3 représente un hydrogène, un halogéno, un hydroxy, un cyano, un carboxy, un alkyle, un alcényle, etc. ; G4 représente un hydroxy ou -N(R1)(R2) (R1 et R2 représentent chacun un hydrogène, un alkyle, un aralkyle, un alcényle, un alcynyle ou un groupe hétérocyclique saturé) ; et G5, qui est un substituant lié à un atome de carbone constitutif du cycle dans A, représente un hydrogène, un fluor ou un alkyle], sel du composé ou dérivé de l'un ou l'autre qui est un promédicament. Le composé, le sel et le dérivé inhibent puissamment la phosphorylation des chaînes légères régulatrices de la myosine.

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