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To treat desacomodamiento fundico Compounds, Pharmaceutical compositions containing Same, Process for preparing such compositions and Process for preparing such compounds

机译:为了治疗去甲二酰胺基化合物,含有该化合物的药物组合物,该组合物的制备方法和该化合物的制备方法

摘要

Formula compound (1),In the chemical isomerization isomer, N-oxide is an addictive salt or a salt of tetrabromodiphenyl ether acceptable for the same drug, where - A1 = A2-A3 = A4 - is a bivalent formula - n = CH-CH = ch -.-CH=N-CH=CH---CH=CH-N=CH---CH=CH-CH=N---N=N-CH=CH---N=CH-N=CH---N=CH-CH=N---CH=N-N=CH---CH = N-CH = N-,or ûCH = CH-N = N-;-Z1-z2 is a hybrid compounding laser CH (R4) - CH2-Y1-CH (R4) -O-,-Y1-CH (R4) -CH2-O-,-Y1-CH (R4) -CH2-S-,-Y1-CH (R4) -CH2-NH-,-Y1-CH (R4) -CH2-CH2-,-Y1-CH (R4) -CH2-CH2-CH2-,-Y1-CH (R4) 3DCH--Y1-CH (R4) 3DCH-CH2--Y1-CH (R4) -CH = CH-,-Y1-CH (R4) 3DCH-CH2-CH2-Or a ch2-ch (R4)wherein, when possible, optionally one or two hydrogen atoms of the same or different carbon or nitrogen atom may be replaced by hydroxyl, C1-4alkyloxyC1-4alkyl, C1-4alkylcarbonyl or C1-6 alkyl optionally substituted with halogen, hydroxyl, C3-6 cycloalkyl or phenyl; Y1 is oxygen or sulfur; Alk1 is C1-4alkylcarbonyl, C1-4alkylcarbonyl, C1-4C1-4alkylcarbonyl, C1-6alkylcarbonyl or optionally substituted with hydroxy, halogen, amino, C1-4alkyl, C1-4 hydroxycarbonyl, C1-alkyloxycarbonyl -4, aminocarbonyl, mono- or di (C1-4alkyl) aminocarbonyl, C1-4alkyloxyC1-4alkyl,C1-4alkylcarbonyloxy, C1-4alkylcarbonyloxyC1-4alkylcarbonyloxy, C1-4alkyloxyimino, phenylC1-4alkylamino, C1-4alkyloxycarbonylC4-6alkenyl, cyano C1-6 alkenyl or C1-6cycloalkylcarbonyloxyC1-4alkyloxycarbonyloxy; R1, R2 and R3 are each independently selected from hydrogen, C1-6 alkyl, C3-6 alkenyl, C1-6 hydroxycarbonyl, trihalomethyl, trihalomethoxy, halogen, hydroxy, cyano, nitro, amino, C1-6 alkylcarbonylamino, C1- 6alkyloxycarbonyl, C1-4alkyloxycarbonyloxy, aminocarbonyl, monoû or di (C1-6alkyl) aminocarbonyl, C1-6 aminoalkyl mono- or di (C1-6alkyl) aminoC1-6alkyl,C1-4alkylcarbonyloxyC1-4alkyloxycarbonyloxy or C3-6cycloalkylcarbonyloxyC1-4alkyloxycarbonyloxy; R4 is hydrogen, hydroxycarbonyl, phenyl, aminicarbonyl, mono- or di (C1-4alkyl) aminocarbonyl, C1-4alkyloxyC1-4alkyl, C1-4alkyloxycarbonyl, N-pyrrolidinecarbonyl, N-piperidinylcarbonyl, N-homopiperidinylcarbonyl, C1-4alkylcarbonyl, C1-4alkylcarbonyl, C1-4alkylcarbonyl -4C1-4alkyloxycarbonylC1-4alkyl, C3-6cycloalkylcarbonyloxyC1-4alkyloxycarbonyloxy or C1-6alkyl optionally substituted with hydroxyl, cyano, amino, phenyl, monoû or di (C1-4alkyl) amino or mono- or di (C1-4alkyl) aminocarbonyl; -A- is a bivalent radical of formulas (2) to (8) in which m is 0 or 1;Alk2 is a bivalent radical selected from C1-4alkylcarbonylC1-4alkyl; phenyl; C3-6cycloalkylcarbonyloxyC1-4alkyloxycarbonyloxy; C3-6cycloalkandiyl optionally substituted with one or more halogens, hydroxyl, hydroxycarbonyl, hydroxyC1-4alkyl, C1-4alkyloxy, C1-4alkyloxyC1-4alkyl, C1-4alkyloxycarbonyl, C1-4alkylcarbonyloxyC1-4alkyloxycarbonyloxy, C3-6alkylcarbonyloxycarbonylcarbonyloxycarbonylcarbonyloxycarbonylcarbonylcarbonyloxycarbonyl or C1-6 alkyl optionally substituted with one or more hydroxyls, halogen, amino, hydroxycarbonyl, hydroxyC1-4alkyl, C1-4 alkyloxy, C1-4alkyloxyC1-4alkyl, C1-4alkyloxycarbonyl, C1-4alkylcarbonyloxyC1-4alkyloxycarbonyloxy, C3- cycloalkyl 6,aminocarbonyl, mono- or di (C1-4alkyl) aminocarbonyl or C1-6 alkyl in which C1-6 alkyl together with the carbon atom to which it is attached can form a C3-6 cycloalkyl; R6 is hydrogen, C1-4 alkyl, halogen, hydroxyl, C1-4 hydroxyalkyl, C1-4 alkyloxy C1-4 aminoalkyl, C1-4 alkyloxycarbonyl, C1-4alkylcarbonyloxyC1-4alkyloxycarbonyl, amino, hydroxycarbonyl, aminocarbonyl, mono - or di (C1-4alkyl) aminocarbonyl or C3-6cycloalkylcarbonyloxyC1-4alkyloxycarbonyloxy; R5 is a radical of formulas (9) to (13) in which n is 1 or 2, p1 is 0 and p2 is 1 or 2; or p1 is 1 or 2 and p2 is 0; X is oxygen, sulfur, NR9 or CHNO2; Y2 is oxygen or sulfur;R7 is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, phenyl or phenylmethyl; R 8 is C 1-6 alkyl, C 3-6 cycloalkyl, phenyl or phenylmethyl; R9 is cyano, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6 alkyl; or R9 and R10 taken together with the nitrogen atom to which they are attached can form a pyrrolidinyl, piperidinyl, homopiperidinyl, piperazinyl or morpholinyl group, optionally substituted with C1-4 alkyl or C1-4 alkyloxy; and Q is a bivalent radical of formulas: -CH2-CH2-,-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH=CH---CH2-CO...-CO-CH2...- (CH2) 2-CO-,-CO- (CH2) 2-,-CO-CH2-CO-CH2-CO-CH2-,In this case, one or two hydrogen atoms of the same or different carbon atoms can be replaced by C1-4 tar, hydroxy or phenyl, or q is a bivalent formula (14) or (15). These compounds are used to repair the changed furnaces The pharmaceutical compounds containing these compounds, the process of preparing these compounds and the process of preparing these compounds are also disclosed.
机译:式(1)的化合物,在化学异构化异构体中,N-氧化物是同一药物可接受的成瘾性盐或四溴二苯醚盐,其中-A1 = A2-A3 = A4-是二价式-n = CH- CH = ch -.- CH = N-CH = CH --- CH = CH-N = CH --- CH = CH-CH = N --- N = N-CH = CH --- N = CH- N = CH --- N = CH-CH = N --- CH = NN = CH --- CH = N-CH = N-,或ûCH= CH-N = N-;-Z1-z2是一个杂种复合激光CH(R4)-CH2-Y1-CH(R4)-O-,-Y1-CH(R4)-CH2-O-,-Y1-CH(R4)-CH2-S-,-Y1-CH( R4)-CH2-NH-,-Y1-CH(R4)-CH2-CH2-,-Y1-CH(R4)-CH2-CH2-CH2-,-Y1-CH(R4)3DCH--Y1-CH( R4)3DCH-CH2--Y1-CH(R4)-CH = CH-,-Y1-CH(R4)3DCH-CH2-CH2-或ch2-ch(R4)其中,在可能的情况下,可选地一个或两个相同或不同碳或氮原子的原子可以被羟基,C 1-4烷氧基C 1-4烷基,C 1-4烷基羰基或任选地被卤素,羟基,C 3-6环烷基或苯基取代的C 1-6烷基取代; Y1是氧或硫; Alk1是C1-4烷基羰基,C1-4烷基羰基,C1-4C1-4烷基羰基,C1-6烷基羰基或任选地被羟基,卤素,氨基,C1-4烷基,C1-4羟基羰基,C1-烷氧基羰基-4,氨基羰基,单或二取代(C1-4烷基)氨基羰基,C1-4烷基氧基C1-4烷基,C1-4烷基羰基氧基,C1-4烷基羰基氧基C1-4烷基羰基氧基,C1-4烷基氧基亚氨基,苯基C1-4烷基氨基,C1-4烷基氧基羰基C4-6烯基,氰基C1-6烯基或C1-6环烷基羰基氧基C1-4烷氧基羰基氧基; R1,R2和R3各自独立地选自氢,C1-6烷基,C3-6链烯基,C1-6羟基羰基,三卤甲基,三卤甲氧基,卤素,羟基,氰基,硝基,氨基,C1-6烷基羰基氨基,C1-6烷基氧羰基, C 1-4烷氧基羰氧基,氨基羰基,单或二(C 1-6烷基)氨基羰基,C 1-6氨基烷基单或二(C 1-6烷基)氨基C 1-6烷基,C 1-4烷基羰氧基C 1-4烷氧基羰氧基或C 3-6环烷基羰氧基C 1-4烷氧基羰氧基; R4是氢,羟基羰基,苯基,小羰基,单或二(C1-4烷基)氨基羰基,C1-4烷氧基C1-4烷基,C1-4烷氧基羰基,N-吡咯烷羰基,N-哌啶基羰基,N-高哌啶基羰基,C1-4烷基羰基,C1-4烷基羰基,C 1-4烷基羰基-4 C 1-4烷氧基羰基C 1-4烷基,C 3-6环烷基羰基氧基C 1-4烷氧基羰基氧基或任选地被羟基,氰基,氨基,苯基,一元或二(C 1-4烷基)氨基或一元或二(C 1-4烷基)取代的C 1-6烷基氨基羰基-A-为式(2)至(8)的二价基团,其中m为0或1; Alk2为选自C1-4烷基羰基C1-4烷基的二价基团;苯基C3-6环烷基羰基氧基C1-4烷基氧基羰基氧基;任选地被一个或多个卤素,羟基,羟羰基,羟基C1-4烷基,C1-4烷氧基,C1-4烷氧基C1-4烷基,C1-4烷氧基羰基,C1-4烷基羰氧基C1-4烷基氧基羰氧基,C3-6烷基羰氧基羰基羰氧基羰基羰基氧基羰基羰基羰基羰基或C1-6烷基取代的C3-6环烷二烷基一个或多个羟基,卤素,氨基,羟基羰基,羟基C1-4烷基,C1-4烷氧基,C1-4烷氧基C1-4烷基,C1-4烷氧基羰基,C1-4烷基羰氧基C1-4烷氧基羰氧基,C3-环烷基6,氨基羰基,单或二(C1-碳原子数为4烷基的氨基羰基或碳原子数为1〜6的烷基,其中碳原子数为1〜6的烷基与所连接的碳原子一起可以形成碳原子数为3〜6的环烷基。 R 6是氢,C 1-4烷基,卤素,羟基,C 1-4羟烷基,C 1-4烷氧基C 1-4氨基烷基,C 1-4烷氧基羰基,C 1-4烷基羰氧基C 1-4烷氧基羰基,氨基,羟羰基,氨基羰基,单-或二(C1 -4烷基)氨基羰基或C3-6环烷基羰氧基C1-4烷氧基羰氧基; R5为式(9)〜(13)的基团,其中n为1或2,p1为0,p2为1或2;或p1为1或2且p2为0;或者X是氧,硫,NR 9或CHNO 2; Y 2是氧或硫; R 7是氢,C 1-6烷基,C 3-6环烷基,苯基或苯甲基; R 8为C 1-6烷基,C 3-6环烷基,苯基或苯甲基; R9是氰基,C1-6烷基,C3-6环烷基,C1-6烷氧羰基或氨基羰基; R10是氢或C1-6烷基;或者R9和R10与它们所连接的氮原子一起可以形成吡咯烷基,哌啶基,高哌啶基,哌嗪基或吗啉基,任选地被C1-4烷基或C1-4烷氧基取代;并且Q是下式的二价基团:-CH2-CH2-,-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH = CH --- CH2-CO ...- CO-CH2 ...- (CH2)2-CO-,-CO-(CH2)2-,-CO-CH2-CO-CH2-CO-CH2-,在这种情况下,可以取代一个或两个相同或不同碳原子的氢原子C 1-4中的焦油,羟基或苯基或q为二价式(14)或(15)。这些化合物用于修理更换的炉子。还公开了含有这些化合物的药物化合物,制备这些化合物的方法和制备这些化合物的方法。

著录项

  • 公开/公告号AR032158A1

    专利类型

  • 公开/公告日2003-10-29

    原文格式PDF

  • 申请/专利权人 JANSSEN PHARMACEUTICA N.V.;

    申请/专利号AR2001P102955

  • 发明设计人

    申请日2001-06-21

  • 分类号C07D491/056;C07D491/052;C07D497/04;C07D498/04;A61K31/436;A61K31/4741;A61K31/536;A61P9/14;

  • 国家 AR

  • 入库时间 2022-08-22 00:04:02

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