Felder Ernst (Rive S. Vitale CHX) Musu Carlo (Milan ITX) Fumagalli Luciano (Milan ITX) Uggeri Fulvio (Milan ITX)
출원인 / 주소
Bracco Industria Chimica S.p.A. (Milan ITX 03)
인용정보
피인용 횟수 :
10인용 특허 :
0
초록▼
Macrocyclic derivatives of 1,4,7,10-tetraazacyclododecane of general formula (I) hereinbelow, wherein A is a group of formula (II) hereinbelow, in which R is H or alkyl or optionally substituted benzyl or a H(OCH2CH2)1-4-, Me(OCH2CH2)1-4-, or Et(OCH2CH2)1-4-group, X or O-R1, in which R1 is H or alky
Macrocyclic derivatives of 1,4,7,10-tetraazacyclododecane of general formula (I) hereinbelow, wherein A is a group of formula (II) hereinbelow, in which R is H or alkyl or optionally substituted benzyl or a H(OCH2CH2)1-4-, Me(OCH2CH2)1-4-, or Et(OCH2CH2)1-4-group, X or O-R1, in which R1 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group or X is -NR2R3, in which R2 and R3 are H or alkyl, hydroxyalkyl, alkoxyalkyl or alkoxyhydroxyalkyl, and B1, B2 and B3 have the same meanings as A or are H or a group of formula (III) hereinbelow, in which R4 is H or alkyl, Y is a O-R5 group, wherein R5 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group, or Y is a -NR6R7 group, wherein R6 and R7 are H or alkyl, hydroxyalkyl, alkoxyalkyl, or alkoxyhydroxyalkyl, said derivatives optionally being salified, and the complex salts thereof, are used as pharmaceuticals and/or diagnostic agents. [Figure] (I) [Figure] (II) [Figure] (III)
대표청구항▼
A 1, 4, 7, 10-tetraazacyclododecane compound of formula I [Figure] I wherein A is a group of formula [Figure] in which R is H or a C1-C5 straight or branched alkyl group, or a benzyl group which is unsubstituted or mono- or poly-substituted on the aromatic ring by halogen, hydroxy, carboxy, carbamoy
A 1, 4, 7, 10-tetraazacyclododecane compound of formula I [Figure] I wherein A is a group of formula [Figure] in which R is H or a C1-C5 straight or branched alkyl group, or a benzyl group which is unsubstituted or mono- or poly-substituted on the aromatic ring by halogen, hydroxy, carboxy, carbamoyl, alkoxycarbonyl, sulphamoyl, lower alkyl, lower hydroxyalkyl, amino, acylamino, acyl, hydroxyacyl groups, or a group of formula H(OCH2CH2)1-4-, Me(OCH2CH2)1-4-, X is a O-R1 group in which R1 is H or a C1-C5 alkyl, hydroxyalkyl alkoxyalkyl, alkoxyhydroxyalkyl group, or a polyoxaalkyl group having 1 to 15 oxygen atoms and 3 to 45 carbon atoms, or X is a -NR2R3 group in which R2 and R3, are the same or different, and are H, C1-C6 alkyl, hydroxyalkyl, alkoxyalkyl or alkoxyhydroxyalkyl groups having up to 5 hydroxy groups and B1, B2 and B3, are the same or different, and have the same meaning as A or they are H or a group of formula [Figure] in which R4 is H or a C1-C5 straight or branched alkyl group, Y is a O-R5 group in which R5 is H or a C1-C5 alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl group, or a polyoxyalkyl group having 1 to 15 oxygen atoms and 3 to 45 carbon atoms, or Y is a -NR6R7 group in which R6 and R7, are the same or different, and are H or C1-C6 alkyl, hydroxyalkyl, alkoxyalkyl or alkoxyhydroxyalkyl groups having up to 5 hydroxy groups, and a salt of said compound of formula I with an organic base which is a member selected from the group consisting of primary, secondary, tertiary amines or with a basic aminoacid or with an inorganic base having a cation which is sodium, potassium or lithium, and a chelate of said compound of formula I or of a salt thereof with a di- or trivalent ion of a metal element having atomic number ranging from 20 to 31,39,42 to 44,49, 57 to 83, wherein said chelate is neutral or acidic or salified with an organic base which is a member selected from the group consisting of primary, secondary, tertiary amines or with a basic aminoacid or with an inorganic base having a cation which is sodium, potassium or lithium.
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