CGRP Receptor Antagonists, Pharmaceutical compositions containing Same, Preparation method and uses for the acute and Preventive Treatment of headaches, including migraines, and other diseases

摘要

The CGRP in general formula (1) is opposite to the cube, that is, R1 is a group selected from compound (2),(3) And (4),R1.1 represents h or h3c-o -;R2 refers to a set of general formulas (5), where R2.1 is ho -,H3CO...H-C (o) - or h3c-c (o) - or r2.2 is C1-2 - or h3co -;R3 is r4-1-2-8-nh-r4 is h, H2nA c1-3-nh(c1-3) 2-N - or 1-c1-6-o-c (o) - NH -;O R3 refers to a group of general preparations (6), where R3.2 is h or c1-3 -.R3.3 is a pair of free electrons or oxygen atoms, r3.4 is h or c1-3 tar, R4 is h, C1-6 tar.H2n-c1-6 tarC1-3-nh-c1-6-tar(c1-3 tar) 2-n-tar C1-6 -,C3-6-c1-6-tarNH2...1. C1-3-nh-o (c1-3) tar 2-N -,Or R4 is a group of radicals selected from the preparation group (7),O R4 the rest selected from the general formula (8), where x is C, r4.1 is h, Oh or c1-3 tar, or X is n and r4.1 is a pair of free electrons or an oxygen atom; orS (o) 2, when x = n, or Y is s, s (o),S (o) 2, when x = C; r4.2 is h or c1-3 -.R4.3 is h or c1-3-tarR4.4 is a pair of free electrons, or when r5.2 is not h or c1-3-c (or) tar,An oxygen atom, r5.1 is h, CN, oh, c1-3 tar,alquil C1-3-C (O) -O-C1-3-O--R5 1 1-O-C (O) -R5.1.1-O-C (O) -C2-4 alkylene or R5.1.1-O-C (O) -C1-3-O-alkylene;R5.1.1 is h, C1-6 tar,H2n-c (o) - c1-3 tar;1. C1-3-nh-c (o) - tar c1-3 -,(c1-3) 2-n-c (o) - c1-3 asphalt or c1-3-o-c (o) - or c1-3 asphaR5.2 is h, c1-3 tar,C3-6 bicycle.C3-6-c1-3-tar1. C1-3-c (o) tarR5.2.1-o-c (o) - c1-3 or r5.2.2-asphalt c2-4-o-c (o) - c1-3 -;R5.2.1 is h, C1-6 tar,1. C1-6-c (o) - or - c1-3 tar1. C1-3-o-c (o) - or - c1-3-tar;That's what it means, that's what it means, that's what it means.H2n-c (o) - c1-3 tar;1. C1-3-nh-c (o) - tar c1-3 -,(C1-3 alkyl) 2-NC (O) -C1-3 alkylene or R5.2.1.1-C (O) -C1-3 alkylene and R5.2.1.1 is a group selected from the radical group of the group of formulas (9) or R5.2.1 is a group selected from the radicals of the formula group (10);R5.2.2 is H2n, c1-3-nh-tar,(c1-3 tar) 2-N1. C1-3 - or c1-3 - or 1-3 - or 1-2-4 - orOr r5.2.2 is another radical selected from the preparation group (11),Provided that R3 and R4 are not combined simultaneously by atoms of N, its ceramic ware, its symmetrical isomer, its counterpart, hydrate, its mixture and salt, especially its physiologically compatible salt with inorganic or organic acids or bases.