DTPA monoamides, pharmaceutical agents containing these compounds, their use and process for their production
申请人:Schering Aktiengesellschaft
公开号:US20030202943A1
公开(公告)日:2003-10-30
Compounds of general formula I
1
in which
Z
1
and Z
2
each stand for a hydrogen atom or the radical
—(CH
2
)
m
—(C
6
H
4
)
q
—(O)
k
—(CH
2
)
n
—(C
6
H
4
)
l
—(O)
r
—R,
in which
m and n independently mean numbers 0-20,
k, l, q and r independently mean numbers 0 and 1 and
R means a hydrogen atom, an optionally OR
1
-substituted C
1
-C
6
alkyl radical or a CH
2
COOR
1
group with R
1
meaning a hydrogen atom, a C
1
-C
6
alkyl radical or a benzyl group,
R
2
stands for a saturated, unsaturated, straight-chain or branched-chain or cyclic non-aromatic hydrocarbyl group with up to 20 C-atoms, an aryl group or aralkyl group, all substituted by a carboxyl group or a sulfone group, each optionally esterified with a C
1
-C
6
alkyl radical or benzyl radical,
R
3
stands for a hydrogen atom or for a saturated, unsaturated, straight-chain or branched-chain or cyclic non-aromatic hydrocarbyl group with up to 20 C-atoms, an aryl group or aralkyl group, in each case being optionally substituted by a carboxyl group or a sulfone group, each optionally esterified with a C
1
-C
6
alkyl radical or benzyl radical,
X stands for a hydrogen atom and/or a metal ion equivalent of an element of atomic numbers 21-29, 31, 32, 37-40, 42-44, 49 or 57-83, provided that at least one of substituents Z
1
and Z
2
stands for a hydrogen atom, that—if n and l each stand for the number 0—k and r are not the number 1 at the same time and that the radical of the acid groups is optionally present as an ester or amide as well as their salts with inorganic and/or organic bases, amino acids or amino acid amides, are valuable pharmaceutical agents.
通式I1的化合物中,其中Z1和Z2分别代表氢原子或基团—(CH2)m—(C6H4)q—(O)k—(CH2)n—(C6H4)l—(O)r—R,其中m和n分别独立地表示0-20的数字,k,l,q和r独立地表示0和1的数字,R表示氢原子,可选的OR1取代的C1-C6烷基基团或带有R1的CH2COOR1基团,其中R1表示氢原子,C1-C6烷基基团或苄基基团,R2表示饱和,不饱和,直链或支链或环状非芳香族碳氢基基团,具有多达20个C原子,芳基基团或芳基烷基基团,所有基团都被羧基或磺酰基取代,每个基团都可以用C1-C6烷基基团或苄基基团酯化,R3表示氢原子或饱和,不饱和,直链或支链或环状非芳香族碳氢基基团,具有多达20个C原子,芳基基团或芳基烷基基团,每种基团都可以用羧基或磺酰基取代,每个基团都可以用C1-C6烷基基团或苄基基团酯化,X表示氢原子和/或原子序数为21-29,31,32,37-40,42-44,49或57-83的元素的金属离子当中的等价物,前提是至少有一个取代基团Z1和Z2代表氢原子,如果n和l分别代表数字0,则k和r不同时为数字1,并且酸基团的基团可以作为酯或酰胺存在以及它们与无机和/或有机碱,氨基酸或氨基酸酰胺的盐是有价值的药物剂。