6,7,8,9 - tetrahydro - 5H - benzocicloheptenil aciladas amines, method for their Synthesis, Pharmaceutical compositions and the use of said compounds for the manufacture of medicinal products

摘要

6.7, 8, 9-tetrahydro-5h-benzocyclohepenil-amine acilada, characterized by any proportion of the total formula (1) of any form of stereoisomer or a mixture thereof or one of the salts acceptable on its drugs, wherein: R1 and R4 are independently selected from the following h groups: C1-10, alquenilo C2-10 and C2-10 are unreplaced and at least single substituted C1-10 tars, and their substitutes are selected from the unreplaced group consisting of F, oh, Alcoy c1-8 mercato, CN, coor6, conr7r8, phenyl and isobutylene, and from at least one single substitution group, the substitutes are selected from the halogen and pseudo halogen groups,C1-3, alcox c1-3 and CF3, non substituted phenanthrene and non substitute, and at least one single substitute, selected from halogen, pseudo halogen, c1-3, alcox c1-3 and CF3, r9co, conr10r11, cour2, CF3, halogen, pseudo halogen, nr13r14, or15, s (o) MR16, so2n17r18 and NO2, R2 and R3, Independently, alternatives are selected from a group consisting of H, halogen, pseudo halogen, C1-10 asphalt, unsubstituted C1-10 asphalt, and at least one single alternative, including Oh, phenyl and isopropene, oh, alcox C1-10, phenyl, s (o) mr19, CF3, CN, NO2, C1-10 amine tar, -C1-10- amineC1-6-Conh--The unreplaced phenyl-conh and phenyl-so2-o are at least a single substitute, which is selected from the hydrocarbon groups of halogen, pseudo halogen, CH3 and metoxi, C1-6 so2-o -,1. C1-6 co type is not an alternative and at least a single alternative tar. Its alternatives are selected from group F, di codil c1-3 amino, pirrolidini and piperidinilo, and phenyl Co. its phenyl part can be replaced by one or more alternatives consisting of c1-3, halogen and thyroid; A selected from CH2, CHH and CH asphalt c1-3 groups; B selected from CH2 and ch1-3 groups; C independently, it has the same meaning as B; D independently, it has the same meaning as B; R5 is ar group or hetar group,both of which may be unsubstituted or carry one or more substituents selected from the group consisting of halogens, pseudohalogens, NH2, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy, C1-10 alkyl and unsubstituted and at least mono-substituted di-C 1-10 alkyl, whose substituents are selected from the group consisting of F, OH, C 1-8 alkoxy, aryloxy, C 1-8 mercapto alkyl, NH 2, C 1-8 amino alkyl and di- C1-8alkyl amino, C3-5 alkanediyl, phenyl, heteroaryl, C1-4alkyl substituted with aryl or heteroaryl, CF3, NO2, OH, phenoxy, benzyl-oxy, C1-10 alkyl COO, S (O) mR20, SH , phenylamino, benzylamino, C1-10 alkyl-CONH-,C1-10-has-c1-4, phenyl CONHPhenyl - containing - C1-4, heteromorphic - CONH,1. Pagan-c1-4, c1-10-co, c1-10-co, phenyl Co, pagan-co, cf3-co, och2o -,WaterOctabromodiphenyl ether-CH2CH2O...COOR21 CONR22R23 CNH (NCH2)SO2NR24R25, R26SO2NH-,R27so2n-c1-6, and different cycles of 5 to 7 mononuclear, liquefied, saturated or at least single unsaturated members, including 1 to 3 heterocyclic atoms selected from the N, O and s groups, which can be replaced by one or more substitutes selected from the halogen, c1-3 and alcox c1-3 groups, Oxo and CF3, where these heterocycles can selectively condense with this ar or hetar group, where all arilo, heterosexual, phenyl, arilo groups containing isomerization and phenyl are selectively present in alternatives to this ar or hetar group,they may be substituted with one or more substituents selected from the group consisting of halogens, pseudohalogens, C1-3 alkyl, OH, C1-3 alkoxy and CF3; R6 is selected from the group consisting of: H, C1-10 alkyl which may be substituted with one or more substituents selected from the group consisting of F, C1-8 alkoxy and di- C1-8 amino alkyl, aryl-C1-4 alkyl and heteroaryl-C1-4alkyl, which may be substituted with one or more substituents selected from the group consisting of halogens, C1-4alkoxy and di- C1-6alkyl amino; R7 is selected from the group consisting of: H, C1-10 alkyl which may be substituted with one or more substituents selected from the group consisting of F, C1-8 alkoxy,1. Di-c1-8 amine and fenilo, fenilo, indan Nile and heaterilo, each of which may not be replaced or carry one or more group substitutes consisting of halogen, pseudo halogen, c1-3 tar, alcoxi c1-3 and CF3; R8 is h or C1-10 tar; R9 is selected from the group consisting of the following: C1-10 may not be replaced or carry one or more substitutes, including F, alcoxi C1-4, di coil c1-3 amino, non substituted phenyl and isopropene, and at least one single substitute selected from the group of c1-3, alcoxi c1-3, halogen, pseudohalogen and CF3; R10, independent,R11 has the same meaning as R7; R11 has the same meaning as R8 independently; R12 has the same meaning as R6 independently; R13 is selected from the following components: H, C1-6 tar, phenyl, benzene, isopropene, c1-6-co tar, phenyl CO and isopropene Co, selected substitutes R14 has the same meaning as R13 in the group consisting of halogen, pseudo halogen, c1-3 tar, alcoxi c1-3 and CF3 and may have one or more substitutes; R15 is selected from the group consisting of H, C1-10 tar, alcox c1-3-c1-3 tar and bencilo,1. The substituted and non substituted phenyl and isopropene are selected from halogen, pseudo halogen, c1-3 tar, alcoxi c1-3 and CF3, and one or more of them can be found; R16 is selected from the following groups: C1-10 tar, which can be replaced by one or more substitutes of F, OH, alcox C1-8, Ariloxi, C1-8 Mercato, C1-8 tar, C1-8 Amino and Di-Acquil C1-8 Amino, CF3, phenyl and substitutes and non substitutes selected from the composition group. 2. Halogen, pseudo halogen, c1-3 tar, Alcoy c1-3 and CF3,and where one or more of these substituents may be present; R17, independently, has the same meaning as R7; R18, independently, has the same meaning as R8; R19 independently, has the same meaning as R16; R20, independently, has the same meaning as R16; R21, independently, has the same meaning as R6; R22, independently, has the same meaning as R7; R23, independently, has the same meaning as R8; R24, independently, has the same meaning as R7; R25, independently, has the same meaning as R8; R26, independently, has the same meaning as R16; R17, independently,It has the same meaning as R16; heteromorphism is a single or double cycle heteromorphism with 5 to 10 members, containing one or more heteroatoms selected from n, O and s groups; hetar group is a single or double cycle heteromorphism with 5 to 10 aromatic members, It contains one or more heteroatoms selected from n, O and s groups; arilo is phenyl, naft-1-ilo or naft-2-ilo; AR group is phenyl, naft-1-ilo or naft-2-ilo; m is 0, 1 or 2; its synthesis method, 1. Drug synthesis and use of these compounds to manufacture drugs for cardiovascular disease, stable and unstable thoracic vascular disease;Coronary artery disease, congenital vascular disease, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusion, endocrine disorder, arteriosclerosis, myocardial infarction, hypertension, essential hypertension Pulmonary hypertension, secondary hypertension, regenerative hypertension, chronic colonic ulcer, erectile dysfunction, ventricular spasm, diabetes, diabetic complications, nephropathy, retinopathy, vascular disease, bronchial asthma, chronic renal failure, cirrhosis, osteoporosis,O reduced cardiovascular risk in women with limited memory or learning ability, or menopause or contraceptive use.