Patent ID: 6492403
Filing Date: 2002-12-10
Classification: A61K,A61P,C07D

Abstract:
A method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein:X is S; Y is a direct covalent bond; Z is NR5R6; R1 is hydrogen, amino, hydroxy, halogen, cyano, C1-4 alkyl or â€”CH2R, where R is hydroxyamino or C1-3 alkoxy; R2 and R3 are independently: i. hydrogen, ii. halogen, iii. hydroxy, iv. nitro, v. cyano, vi. amino, monoalkylamino, dialkylamino, monoarylamino, diarylamino, monoalkylmonoarylamino, monoaralkylamino, diaralkylamino, alkylarylamino, alkoxycarbonylamino, aralkoxycarbonylamino, aryloxycarbonylamino, alkylsulfonylamino, aralkylsulfonylamino, arylsulfonylamino, formylamino, acylamino, H(S)CNHâ€”, or thioacylamino, vii. aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, acyl, aminoacyl, or arylaminocarbonyl, viii. aminothiocarbonyl, monoalkylaminothiocarbonyl, dialkylaminothiocarbonyl, thioacyl or aminothioacyl, ix. aminocarbonylamino, mono- and dialkylaminocarbonylamino, mono- and diarylaminocarbonylamino, or mono- and diaralkylaminocarbonylamino, x. aminocarbonyloxy, mono- and dialkylaminocarbonyloxy, mono- and diarylaminocarbonyloxy, mono- and dialkylaminocarbonyloxy, xi. aminosulfonyl, mono- and dialkylaminosulfonyl, mono- and diarylaminosulfonyl, or mono- and diaralkylaminosulfonyl, xii. alkoxy, or alkylthio, wherein the alkyl portion of each group may be optionally substituted, xiii. aralkoxy, aryloxy, aralkylthio, or arylthio, wherein the aryl portion of each group can be optionally substituted, xiv. alkylsulfonyl, wherein the alkyl portion can be optionally substituted, xv. aralkylsulfonyl, or arylsulfonyl, wherein the aryl portion of each group can be optionally substituted, xvi. alkenyl, or alkynyl, xvii. optionally substituted aryl, xviii. optionally substituted alkyl, xix. optionally substituted aralkyl, xx. optionally substituted heterocycle, or xxi. optionally substituted cycloalkyl; and R4, R5 and R6 are independently hydrogen, C1-4 alkyl, aryl, hydroxyalkyl, aminoalkyl, monoalkylamino(C2-10)alkyl, dialkylamino(C2-10)alkyl, carboxyalkyl, cyano, amino, alkoxy, or hydroxy, or â€”CO2Rw, where Rw is alkyl, cycloalkyl, phenyl, benzyl, â€ƒwhere Rd and Re are independently hydrogen, C1-6 alkyl, C2-6 alkenyl or phenyl, Rf is hydrogen, C1-6 alkyl, C2-6 alkenyl or phenyl, Rg is hydrogen, C1-6 alkyl, C2-6 alkenyl or phenyl, and Rh is aralkyl or C1-6 alkyl, provided that when R4 is hydrogen, neither R5 nor R6 is aryl.