Inhibitors of Serine proteases with lower molecular weight and polihidroxicicloalquilo polihidroxialquilo radical

摘要

A compound of amitriptyline or guardipine, having a general formula of a-b-d-e-g-k-l, wherein a is h, CH3, H - (ra1) ia, wherein ra1 is equal to formula (1) of a group,Among them, ra2 is h, NH2, nh-coch3, F, nhcho; RA3 is h, CH2OH; RA4 is h, CH3, COOH; IA = 1-20; JA = 0, 1, 2; Ka = 2, 3; La = 0, 1; Ma = 0, 1, 2; if ra1 excimer is greater than 1, it may be the same or different; B is a formula of this group (2);A-B is one of the group's formulas (3);Or a radical neuron acid of n-acetyl-n-acrylic acid, each of which is combined by anthrax function; RB1 is equivalent to h, CH2OH, C1-4 tar; Rb2 is equivalent to h, NH2, nh-coch3, F, nhcho; RB3 is equivalent to h, C1-4 tar, ch2-o-4, COOH, F, nh-coch3, CONH2; RB4 is equivalent to c1h, C14 tar, Ch2-o-tar C1-4, COOH, CHO, in the latter case, the intramolecular aceous may be formed; RB5 is equal to h, C1-4 tar, ch2-o-4, COH; KB = 0, 1; LB = 0, 1; LB = 0, 1, 2, 3 (Lb1 is different from 0, where a = RB1 = RB3 = h, MB = KB = 0, D is the link);MB = 0, 1, 2, 3, 4; Nb = 0, 1, 2, 3; rb6 equals C1-4 tar, phenyl, phenylethyl; BB7 equals h, C1-4 tar, benzene, phenylethyl; D equals o-n (RD1) - rd2-rd3-rd4.In the case of RD1 equal to h, C1-4 leased land; RD2 equal to C1-4 linked or leased land; RD3 equal to the formula of a group (4),LD = 1, 2, 3, 4, 5, 6 and rd5 are equal to h, C1-4 hydrocarbon, CL; rd6 is equal to h, CH3; in this case, additional aromatic or aromatic rings can be incorporated into the above RD3 ring system; RD4 is equal to link, C1-4 hydrocarbon, Co, SO2, ch2-co; E is a set of formulas (5),Among them, Ke = 0, 1, 2; E = 0, 1, 2; me = 0, 1, 2, 3; ne = 0, 1, 2; PE = 0, 1, 2; RE1 is h, C1-6 asphalt, cyclo-8, arilo (especially phenyl or naftil),Heteromorphic (especially pyridylene, butadiene, pyridylene, indolilo),e. Other RE1 as defined in the memory, in addition, re4oco-ch2 - (RE4 is equal to h, No. C1-12 asphalt, No. c1-3 lease);Re2 is h, C1-6 tar, cyclo-c3-8, arilo (especially phenyl or nafos),Isopropene (especially pyridine, furan, Tianjin, pyridine, indolilo),4. Tetrahydropyridine, tetrahydrazine and other substances defined in memory; RE3 is h, C1-6 tar, C3-8 cyclopentadiene, arilo (especially phenyl or endorphin),heteroaryl (in particular pyridyl, thienyl, imidazolyl, indolyl) and others as defined herein; the groups mentioned can be linked under RE1 and RE2 to each other by a link; the groups mentioned under RE2 and RE3 can also be linked together through a link; RE2 is also CORE5 (RE5 is equal to OH, O-C1-6 alkyl, O-C1-3 alkyl-aryl),Conre6re7 (where R6 or R7 equals h, C1-6, rental c0-3),Nre6re7; E may also be D-Asp, D-Glu, D-Lys, d-orn, d-su, d-dab, d-dap, D-Arg; G is a set of LG = 2, 3, 4 or 5 formulas, in which a set of CH2 in the ring can be replaced by O, s, NH, nalquilo c1-3, Choh, CHO acquilo c1-3, C (c1-3 Baibai reservoir) 2, ch-3,CHF, CHCl, CF2, etc. described in the report; in addition, G is a formula group (7),QG is 0, 1, 2; RG is 0, 1, 2; Rg3 is h, C1-6 tar, C3-8 cyclopentadiene, arilo; rg4 is h, C1-6 tar, C3-8 cyclopentadiene, arilo (especially phenyl, nafilo);K is NH - (CH2) nk-qk, where NK = 0, 1, 2, 3; QK is equal to c2-6 tar, where up to two sets of CH2 can be replaced by O or s as described in the report, others are C2 as described in the report; l represents a group formula (8),RL1 is equivalent to h, oh, o-asphalt C1-6, O - (CH2) 0-3-phenyl, co-6, co2-asphalt C1-6, co2-rental c1-3 or its tautometer, stereoisomer, salt and its products with tolerable acid or pharmacological basis. A pharmaceutical component containing a compound as an active component, and a pharmaceutical component for which the compound is used for preparation, used as a thrombus inhibitor, anticoagulant, supplement inhibitor, and anti-inflammatory agent. One of the characteristics of the new compounds is the binding of polyurethane protein inhibitors, which also has the function of amidina or guanidinia,1. An excimer with two or more hydroxyl functions, wherein the tar of the excimer is derived from a sugar derivative. Several sugar units or units extracted from sugar can be combined at present. This principle of docking of sugar derivatives leads to oral active compounds.