申请人:Giardina Arnaldo Maria Giuseppe
公开号:US20070197546A1
公开(公告)日:2007-08-23
A compound, or a solvate or a salt thereof, of formula (I):
wherein, Ar is an optionally substituted aryl or a C
5-7
cycloalkdienyl group, or a C
5-7
cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group,;
R is C
1-6
alkyl, C
3-7
cycloalkyl, C
3-7
cycloalkylalkyl, optionally substituted phenyl or phenyl C
1-6
alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C
1-6
alkyl, amino C
1-6
alkyl, C
1-6
alkylaminoalkyl, di C
1-6
alkylaminoalkyl, C
1-6
acylaminoalkyl, C
1-6
alkoxyalkyl, C
1-6
alkylcarbonyl, carboxy, C
1-6
alkoxycarbonyl, C
1-6
alkoxycarbonyl C
1-6
alkyl, aminocarbonyl, C
1-6
alkylaminocarbonyl, di C
1-6
alkylaminocarbonyl, halogeno C
1-6
alkyl; or R is a group —(CH
2
)
p
— wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar;
R
1
represents hydrogen or up to four optional substituents selected from the list consisting of: C
1-6
alkyl, C
1-6
alkenyl, aryl, C
1-6
alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C
1-6
alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C
1-6
alkylamino;
R
2
represents a moiety —(CH
2
)
n
—NY
1
Y
2
wherein n is an integer in the range of from 1 to 9, Y
1
and Y
2
are independently selected from hydrogen; C
1-6
-alkyl; C
1-6
alkyl substituted with hydroxy, C
1-6
alkylamino or bis (C
1-6
alkyl) amino; C
1-6
-alkenyl; aryl or aryl-C
1-6
-alkyl or Y
1
and Y
2
together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group;
R
3
is branched or linear C
1-6
alkyl, C
3-7
cycloalkyl, C
4-7
cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and
R4 represents hydrogen or C
1-6
alkyl; a pharmaceutical composition comprising such a compound, process for preparing such a compound and the use of such a compound in medicine.
化合物,或其溶剂化合物或盐,其化学式为(I):其中,Ar是可选择取代的芳基或C5-7环烯基基团,或C5-7环烷基团或可选择取代的单环或融合环芳杂环基团;R是C1-6烷基,C3-7环烷基,C3-7环烷基烷基,可选择取代的苯基或苯基C1-6烷基,包含最多四个杂原子(O和N)的可选择取代的五元杂环芳香环,羟基C1-6烷基,氨基C1-6烷基,C1-6烷基氨基烷基,二C1-6烷基氨基烷基,C1-6酰胺基烷基,C1-6烷氧基烷基,C1-6烷基羰基,羧基,C1-6烷氧羰基,C1-6烷氧羰基C1-6烷基,氨基羰基,C1-6烷基氨基羰基,二C1-6烷基氨基羰基,卤代C1-6烷基;或R是一个基团-(CH2)p-,其中p为2或3,该基团与Ar的一个碳原子形成环;R1表示氢或最多四个可选择的取代基,选自以下列表:C1-6烷基,C1-6烯基,芳基,C1-6烷氧基,羟基,卤素,硝基,氰基,羧基,羧酰胺基,磺酰胺基,C1-6烷氧羰基,三氟甲基,酰氧基,邻苯二甲酰亚胺基,氨基或单-和二-C1-6烷基氨基;R2表示一个基团-(CH2)n-NY1Y2,其中n是1到9的整数,Y1和Y2独立选择自氢,C1-6烷基,C1-6烷基取代羟基,C1-6烷基氨基或双(C1-6烷基)氨基,C1-6烯基,芳基或芳基-C1-6烷基,或Y1和Y2与它们所连接的氮原子一起表示可选择取代的N-连接单环或融合环杂环基团;R3是支链或线性C1-6烷基,C3-7环烷基,C4-7环烷基烷基,可选择取代的芳基,或可选择取代的单环或融合环芳杂环基团;R4表示氢或C1-6烷基;包括这种化合物的药物组合物,制备这种化合物的方法以及在医学上使用这种化合物的用途。