Modified amino acids for production of antibodies and labelled compounds suitable for RIA and ELISA assays

摘要

Modified amino acids of general formula (I). Wherein; R is unbranched C1-7alkyl group which may be substituted at the w-position, unbranched C1-6alkylamino group optionally substituted at the nitrogen atom by a C1-6alkyl group or by a phenylmethyl group, which may substituted in the w-position or R is as described in formula (II); Z is -NR1- or a methylene group, wherein R1 is H, C1-7alkyl or phenylC1-2alkyl group; m is 0 nor 1; n is 1 or 2; R2 is an aromatic or heteroaromatic group optionally mono-, di- or tri-substituted in the carbon skeleton by F, Cl or Br, by C1-6alkyl groups, C1-6alkoxy, trifluormethyl, C1-4alkoxycarbonyl, carboxy, OH, nitro or amino groups; R11 is H or C1-3alkyl group; X is oxygen or 2 hydrogen atoms; A is shown as Formula (III), wherein R8 and R9 together are n-propylene group, R8 is H, alkyl or phenyl group, R9 is H or branched and unbranched C1-5alkyl group substituted in the w-position; R3 is H, C1-7alkyl group substituted at the w-position, a phenyl or pyridinyl group; R4 is H or C1-3alkyl group optionally substituted by a phenyl or pyridinyl group; or R3 and R4 together form the compound shown in Formula (IV), wherein Y3 is carbon, if R12 is a free pair of electron, Y3 may also be nitrogen, r is 0-2, q is 0-2, R10 is H , amino, alkylamino, dialkylamino, alkyl, cycloalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkylaminocarbonylamino, cycloalkylaminocarbonylamino, phenylaminocarbonylamino, aminocarbonylalkyl, aminocarbonylaminoalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, carboxy group or 1,1-dioxido-3(4H)-oxo-1,2,4-benzothiadiazin-2-yl group, R12 is H, C1-4alkyl, alkoxycarbonyl, cyano or aminocarbonyl, R13 and R14 is H. The method and use for the production and purification of antibodies and as marked compounds in RIA and ELISA assays and as diagnostic or analytic auxiliary agents in neurotransmitter research are described. The pharmaceutical composition is suitable for acute and prophylactic treatment of headaches, for treating non-insulin dependent diabetes melitis, cardiovascular disorders, skin diseases, inflammatory disease, allergic rhinitis asthma, disease accompanied by excessive vasodilation and consequently reduced blood circulation, e.g. shock and sepsis, and morphine tolerance.