Macrocyclic Compounds, which include esteroisomeros enantiomers, rotamers, and tautomeros, Salts and pharmaceutically acceptable solvates, Pharmaceutical composition, Preparation method thereof and the use of such compounds for the preparation of a Medicament, inhibitors of the serine protease

摘要

A macrocyclic compound, including dwarfs, rotorcraft stereoisomers, and the compound's golden eyed snapper,as well as pharmaceutically acceptable salts or solvates of said compound, which has the general structure set forth in formula (1) in which E, X and Y may be independently present or absent and, if present, are independently selected from Portions: alkyl, aryl, alkylaryl, heteroaryl, arylheteroaryl, alkylheteroaryl, cycloalkyl, alkyl ether, alkylaryl ether, aryl ether, alkylamino, arylamino, alkylaminolamino, alkylsulfide, alkylsulfide, arylsulfide, alkylsulfone, alkylsulfone, arylsulfone, alkylalkyl alkyloxylalkyl alkylalkyl alkylalkyl alkylsulphoxide arylamide, alkylsufonamide, alkylarylsulfonamide,arylsulfonamide, alkylurea, alquilarilurea, arylurea, alkyl carbamate, carbamate, alkyl aryl carbamate, alquilhidrazida, alquilarilhidrazida, alquilhidroxamida, alquilarilhidroxamida, alkylsulfonyl, arylsulfonyl, heteroalquilsulfonilo, hetroarilsulfonilo, alkylcarbonyl, arylcarbonyl, heteroarylalkylcarbonyl, heteroarylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, hetoroariloxicarbonilo, alkylaminocarbonyl, arylaminocarbonyl, heteroarylaminocarbonyl, or a combination thereof; with the proviso that optionally E, X, and Y may also be substituted with portions selected from the group consisting of aromatic, alkyl, alkylaryl,heteroalkyl, arylheteroaryl, alkylheteroaryl, cycloalkyl, alkyl ether, alkylaryl ether, alkylsulfide, alkylaryl sulphide, alkylsulfone, alkylarylsulfone, alkylamide, alkylarylamide, alkylsulfonamide, alkylamines, alkylarylsulfonamide, alkylaryl, alkylaryl, carbamate, alkoxycarbamate alkyl, aryl carbazate; R1 = COR5 or B (OR) 2, where R5 = H, OH, OR8NR9R10, CF3, C2F5, C3F7, CF2R6, R6, COR7 where R7 = H, OH, OR8, CHR9R10, where R6, R8, R9 and R10 are independently selected from the group consisting of H, alkyl, aryl, heteroalkyl, heteroaryl, cycloalkyl, cycloalkyl, arylalkyl,heteroarylalkyl, CH (R1 ') COOR11, CH (R1') CONR12R13, CH (R1 ') CONHCH (R2') COOR11, CH (R1 ') CONHCH (R2') CONR12R13, CH (R1 ') CONHCH (R2') CONHCH (R3 ') COOR11, CH (R1') CONHCH (R2 ') CONHCH (R3') CONR12R13, CH (R1 ') CONHCH (R2') CONHCH (R3 ') CONHCH (R4') COOR11, CH (R1 ' ) CONHCH (R2 ') CONHCH (R3') CONHCH (R4 ') CONR12R13, CH (R1') CONHCH (R2 ') CONHCH (R3') CONHCH (R4 ') CONHCH (R5') COOR11, CH (R1 ') CONHCH (R2 ') CONHCH (R3') CONHCHR4 ') CONHCH (R5') CONR12R13 where R1 ',R2',R3',R4, R5',R11, R12, R13 are independently selected from the group consisting of H, alkyl, aryl, heteroalkyl, heteroaryl, cycloalkyl, alkylaryl, alkylheteroaryl, arylalkyl, and heteroaralkyl; Z is selected from O, N or CH; W may be present or absent and, if present W is selected from C = O, C = S, SO2 or C = NR; Q is (NR) p, O, S, CH2, CHR, CRR 'or a double bond towards V; A is O, CH2, (CHR) p, (CHR-CHR ') p, (CRR') p, NR, S, SO2, C = O or a bond; G is (CH2) p, (CHR) p, (CRR ') p, NR, O, S, SO2, S (O) 2NH, C = O or a double bond to E or V; V is CH, CR or N; p is a number from 0 to 6 and R, R ',R2, R3, and R4 are from h, asphalt, C1-10, alquenilo C2-10, cyclopentanediol C3-8, isopentadiene C3-8, arilo, alcoxi, ariloxi, acultio, ariltio, amino, amido, ester, carboxylyl acid, carbamato, urea, cetona, aldehido, acuerdo, cineo, acquiro, nitro, isopropene, Rilo, rielhoarillo, 1. Tar and (heterocyclic) tar are composed of 3 to 8 carbon atoms and 0 to 6 oxygen, nitro, sulfur or phosphorus atoms. Tar is composed of 1 to 6 carbon atoms, including tar, isomerization, alquenilo, isomerization, isomerization and arilo,Alternative to isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl isopropyl Alcox, ariloxi, acultio, ariltio, amino, amido, ether, carboxyl acid, carbamato, urea, cetona, aldehido, Ciano, nitro, sulfonamida, sulfoxido, sulfonilurea, hydrazine, hydraxamato and tiourea; and the method for preparing these compounds. Previous pageThis report also introduces the pharmaceutical components including these macrocyclic substances, and their use in the treatment of hepatitis C virus protesa ns-3 queen bee inhibitor VHC protein disorder for the chlorination of drugs.