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    • 54. 发明申请
    • PYRIMIDINE COMPOUNDS AND USE THEREOF
    • 吡嗪化合物及其用途
    • US20110118232A1
    • 2011-05-19
    • US12842776
    • 2010-07-23
    • Hervè GenesteAndreas HauptWilfried BrajeWilfried LubischGerd Steiner
    • Hervè GenesteAndreas HauptWilfried BrajeWilfried LubischGerd Steiner
    • A61K31/554C07D403/14A61K31/496C07D413/14A61K31/538C07D417/14A61K31/5415A61K31/551A61K31/55A61P25/00A61P25/18A61P25/24
    • C07D417/12C07D401/12C07D413/12
    • The invention relates to novel pyrimidine compounds of general formula (I), in which: A represents a group C═W or CRfRg; B represents a chemical bond or a group CRhRi; X represents O, S, a group N—Rk or a group CRmRn; D represents C═O or a chemical bond; E represents a linear or branched 2- to 10-membered alkylene chain that, as members of a chain, can have 1 or 2 non-adjacent heteroatom group(s) K, which is selected among O, S, S(O), S(O)2 and N—Rp and which can comprise a carbonyl group and/or a cycloalkanediyl group and/or a double or triple bond; W represents oxygen or sulfur; Z, together with the carbon atoms, to which it is bound, represents a condensed, optionally substituted 5-, 6- or 7-membered carbocyclic compound or heterocyclic compound that has 1, 2, 3 or 4 heteroatoms, which are selected among N, O and S; J represents CH2, CH2—CH2 or CH2—CH2—CH2; M represents CH or N; Y represents CH2, CH2—CH2 or CH2—CH2—CH2 or M-X, together, represent CH═C or CH2—CH═C; n is 0 or 1, and; Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh, Ri, Rk, Rp, R1, R2, R3, R4, R5 and R6 have the meanings cited in the claims and in the description. The invention also relates to the physiologically compatible acid addition salts of the aforementioned compounds, and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.
    • 本发明涉及通式(I)的新型嘧啶化合物,其中:A代表基团C = W或CRfRg; B表示化学键或CRhRi基; X表示O,S,基团N-Rk或基团CRmRn; D表示C = O或化学键; E表示直链或支链的2-至10-元亚烷基链,其作为链的成员可以具有1或2个不相邻的杂原子K,其选自O,S,S(O), S(O)2和N-Rp,并且其可以包含羰基和/或环烷二基和/或双键或三键; W表示氧或硫; Z与其结合的碳原子一起代表具有1,2,3或4个杂原子的缩合的,任选取代的5-,6-或7-元碳环化合物或杂环化合物,其选自N ,O和S; J表示CH 2,CH 2 -CH 2或CH 2 -CH 2 -CH 2; M表示CH或N; Y表示CH 2,CH 2 -CH 2或CH 2 -CH 2 -CH 2或M-X,一起表示CH = C或CH 2 -CH = C; n为0或1, Ra,Rb,Rc,Rd,Re,Rf,Rg,Rh,Ri,Rk,Rp,R1,R2,R3,R4,R5和R6具有权利要求书和说明书中引用的含义。 本发明还涉及上述化合物的生理上相容的酸加成盐,以及这些化合物(I)的化合物和化合物(I)的生理上相容的酸加成盐在制备用于治疗疾病的药剂中的用途 ,其响应于多巴胺D3受体拮抗剂或激动剂的影响。