C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 243/08 (2006.01) A61K 49/00 (2006.01) A61K 49/08 (2006.01) A61K 49/10 (2006.01) C07C 229/16 (2006.01) C07C 229/76 (2006.01)
Patent
CA 2453845
Compounds of general formula (I):in which: R1 is hydrogen, C1-C2O alkyl, C3- C10 cycloalkyl, C4-C2O cycloalkylalkyl, aryl, arylalkyl, or two R1, taken together, form a straight or cyclic C2-C10 alkylene group or an ortho disubstituted arylene; R2 is hydrogen, C1-C2O alkyl, C3-C10 cycloalkyl, C4-C2O cycloalkylalkyl, aryl or aryl alkyl optionally substituted with functional groups which allow conjugation with a suitable molecule able to interact with physiological systems; R3, R4 and R5 are hydrogen, C1-C20 alkyl, C3-C10 cycloalkyl, C4-C2O cycloalkylalkyl, aryl, arylalkyl; and their chelates with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42,43,44,49, and between 57 and 83, and radioisotopes chosen among 203Pb 67Ga 68Ga 72As lllIn 113In 90Y 97Ru 62Cu 64Cu 52Fe 52mMn , 140La 175Yb 153Sm 166Ho 149Pm 177Lu 142Pr 159Gd 2l2Bi 47Sc 149Pm 67Cu, 111 Ag, 199 Au, 161Tb and 51Cr as well as the salts thereof with physiologically compatible bases or acids.
L'invention concerne les composés de la formule générale (1) dans laquelle R¿1? est hydrogène, C¿1?-C¿20? alkyl, C¿3?-C¿10? cycloalkyl, C¿4?-C¿20? cycloalkylalkyl, aryl, arylalkyl, ou deux R¿1? pris ensemble forment un groupe alkylène C¿2?-C¿10? linéaire ou cyclique ou un arylène ortho disubstitué ; R¿2? est hydrogène, C¿1?-C¿20? alkyl, C¿3?-C¿10? cycloalkyl, C¿4?-C¿20? cycloalkylalkyl, aryl ou arylalkyl éventuellement substitué avec des groupes fonctionnels permettant une conjugaison avec une molécule adaptée pouvant interagir avec des systèmes physiologiques ; R¿3?, R¿4? et R¿5? sont hydrogène, C¿1?-C¿20? alkyl, C¿3?-C¿10? cycloalkyl, C¿4?-C¿20? cycloalkylalkyl, aryl, arylalkyl ; et, FG sont des groupes carboxy, -PO¿3?H¿2? ou RP(O)OH, dans lesquels R est hydrogène, C¿1?-C¿20? alkyl, C¿3?-C¿10? cycloalkyl, C¿4?-C¿20? cycloalkylalkyl, aryl, arylalkyl. L'invention concerne également les chélates desdits composés contenant des ions bi/trivalents des éléments métalliques de numéro atomique valant entre 20 et 31, 39, 42, 43, 44, 49 et entre 57 et 83, ainsi que des radioisotopes choisis parmi ?203¿Pb, ?67¿Ga, ?68¿Ga, ?72¿As, ?111¿In, ?113¿In, ?90¿Y, ?97¿Ru, ?62¿Cu, ?64¿Cu, ?52¿Fe, ?52m¿Mn, ?140¿La, ?175¿Yb, ?153¿Sm, ?166¿Ho, ?149¿Pm, ?177¿Lu, ?142¿Pr, ?159¿Gd, ?2l2¿Bi, ?47¿Sc, ?149¿Pm, ?67¿Cu, ?111¿Ag, ?199¿ Au, ?161¿Tb, et ?51¿Cr ainsi que leurs sels contenant des bases et acides physiologiquement acceptables.
Aime Silvio
Calabi Luisella
Cavallotti Camilla
Giovenzana Giovanni Battista
Palmisano Giovanni
Bracco Imaging S.p.a.
Kirby Eades Gale Baker
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