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    • 3. 发明申请
    • DERIVATIVES OF 2-AMINO-1,2,3,4-TETRAHYDRONAPHTHALENE ACTIVE ON THE CARDIOVASCULAR SYSTEM
    • 2-氨基-1,2,3,4-四氢萘酮在心脏血管系统中的作用
    • WO1995007885A1
    • 1995-03-23
    • PCT/EP1994002981
    • 1994-09-07
    • ZAMBON GROUP S.P.A.MONTANARI, StefaniaCAVALLERI, PaoloSANTANGELO, Francesco
    • ZAMBON GROUP S.P.A.
    • C07C323/25
    • C07D213/69C07C225/16C07C323/25C07C2602/10C07D213/70C07D233/64C07D233/84C07D261/12C07D333/20
    • Compounds of formula (I), wherein R is a hydrogen atom or an OY group; R1 is a hydrogen atom or an OY' group; R2 is a hydrogen atom or an OY'' group; provided that at least one among R, R1 and R2 is hydrogen but R, R1 and R2 are not contemporaneously hydrogen atoms and R1 and R2 are not contemporaneously OY' or OY'' groups respectively; m &cir& _ is an integer selected between 1 and 2; n &cir& _ is an integer comprised among 3 and 8; p &cir& _ is an integer comprised among 2 and 4; R3 is a hydrogen atom or a C1-C4 alkyl; R4 is a phenyl optionally substituted by halogen atoms, C1-C3 alkyl or alkoxy groups or a 5- or 6-membered heteroaryl containing one or more heteroatoms selected among oxygen, nitrogen and sulphur, optionally substituted by halogen atoms, hydroxy groups, C1-C3 alkyl or alkoxy groups; X is CH2, NH, S, SO, SO2, CO, CF2, O and, when R4 is a 5- or 6-membered heteroaryl, X can be also a single bond; and their pharmaceutically acceptable salts are described. The compounds of formula (I) are useful in the treatment of arterial hypertension and heart failure, of renal insufficiency, of peripheral arteriopathies and of cerebrovascular insufficiencies.
    • 式(I)的化合物,其中R是氢原子或OY基团; R1是氢原子或OY'基团; R2是氢原子或OY“基团; 条件是R,R 1和R 2中的至少一个是氢,但R,R 1和R 2不是同时存在的氢原子,并且R 1和R 2不是分别同时是OY'或OY“基团; m&cir&_是从1到2之间选择的整数; n&cir&_是3和8之间的整数; p&cir&_是2和4之间的整数; R3是氢原子或C1-C4烷基; R4是任选被卤素原子,C 1 -C 3烷基或烷氧基取代的苯基或含有一个或多个选自氧,氮和硫的杂原子的5-或6-元杂芳基,任选被卤素原子取代,羟基,C1- C3烷基或烷氧基; X是CH 2,NH,S,SO,SO 2,CO,CF 2,O,当R 4是5-或6-元杂芳基时,X也可以是单键; 及其药学上可接受的盐。 式(I)化合物可用于治疗动脉高血压和心力衰竭,肾功能不全,外周动脉炎和脑血管功能不全的治疗。
    • 5. 发明申请
    • DERIVATIVES OF 2-AMINO-1,2,3,4-TETRAHYDRONAPHTHALENE ACTIVE ON THE CARDIOVASCULAR SYSTEM
    • 2-氨基-1,2,3,4-四氢萘酮在心脏血管系统中的作用
    • WO1996008463A1
    • 1996-03-21
    • PCT/EP1995003479
    • 1995-09-05
    • ZAMBON GROUP S.P.A.MONTANARI, StefaniaBOTTA, DanielaCAVALLERI, PaoloSANTANGELO, Francesco
    • ZAMBON GROUP S.P.A.
    • C07C215/44
    • C07D213/38C07C215/64
    • Compounds of formula (I), wherein m is an integer number selected among 4, 5, 6, 7 and 8; R, R' and R" are hydrogen atoms or OH groups, provided that at least one among R, R' and R" is a hydrogen atom but R, R' and R" are not all contemporaneously hydrogen atoms and R' and R" are not both contemporaneously OH groups; R1 is a hydrogen atom or a C1-C4 alkyl group; R2 is a -(CH2)n-Ar group, wherein n is an integer number selected among 2, 3, 4 and 5; Ar is a pyridyl or a phenyl or R2 is a group of formula (a), wherein one or two among R3, R4, R5 and R6 are OH groups and the remaining are hydrogen atoms; R7 and R8 are hydrogen atoms or together can form a -CH2-CH2-chain; and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful in the treatment of arterial hypertension and heart failure, of renal failure, of peripheral arteriopathies, of cerebrosvascular insufficiencies and of ischemic cardiopathy.
    • 式(I)化合物,其中m为选自4,5,6,7和8之间的整数; R,R'和R“是氢原子或OH基团,条件是R,R'和R”中的至少一个是氢原子,但R,R'和R“不全部同时为氢原子,R'和R “不是同时是OH组; R1是氢原子或C1-C4烷基; R2是 - (CH2)n-Ar基团,其中n是选自2,3,4和5中的整数; Ar是吡啶基或苯基或R2是式(a)的基团,其中R3,R4,R5和R6中的一个或两个是OH基团,其余是氢原子; R7和R8是氢原子或一起可以形成-CH 2 -CH 2 - 链; 及其药学上可接受的盐。 式(I)化合物可用于治疗动脉高血压和心力衰竭,肾衰竭,外周动脉病变,脑血管功能不全和缺血性心脏病的治疗。