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Ariltienopirimidinas replaced with azaciclilo, Process for their Preparation and their use as medicines

机译：杀鼠灵替代阿奇替尼，其制备方法及其作为药物的用途

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Item 1: a formula compound (1)This means, R1, R1 ',R1 ".R1 '' 'independently of each other H, F, CI, Br, I, OH, CF3, NO2, CN, OCF3, O-C1-6 alkyl, O-C1-4 alkoxy-C1-4 alkyl, S-C1 alkyl -6, C1-6 alkyl, C2-6 alkenyl, C3-8 cycloalkyl, O3-8 cycloalkyl, C3-8 cycloalkenyl, C2-6 alkynyl, C0-8-aryl alkylene, C0-8-aryl O-alkylene , S-aryl, N (R3) (R4),So2-ch3, COOH, COO asphalt C1-6, con (R5) (R6),N (R7) CO (R8)N (R9) SO2 (R10)CO (R11)(C (R12) (R13)) x-O (R14)R3, R4, R5, R6, R7, R9 independently of each other H, C1-8 alkyl; or R3 and R4, R5 and R6 form independently of each other optionally together with the nitrogen atom to which a 5-6 membered ring is attached which, apart from the nitrogen atom, can also comprise 0-1 additional heteroatoms of the NH group , N 1-8 alkyl, oxygen and sulfur; R8, R10, R11 independently of each other H, C1-8 alkyl; R12, R13 independently of each other H, C1-8 alkyl; R14 H, C1-6 alkyl, aryl; x is 0, 1, 2, 3, 4, 5 or 6; R2 H, F, CI, Br, I, OH, CF3, NO2, CN, OCF3, O-C1-6 alkyl, O-C1-4 alkoxy C1-4 alkyl, S-C1-6 alkyl, C1-6 alkyl, C2-6 alkenyl, C3-8 cycloalkyl,O-cycloquino C3-8, cycloquinoo C3-8, tar c2-6, c0-8-arilo, o-coquileno c0-8-arilo, s-arilo, n (R15) (R16),So2-ch3, COOH, COO asphalt C1-6, con (R17) (R18),N (R19) CO (R20)N (R21) SO2 (R22)CO (R23)(C (R24) (R25)) x -O (R26)R15, R16, R17, R18, R19, R21 independently of each other H, C1-8 alkyl; or R15 and R16, R17 and R18 independently form each other and optionally together with the nitrogen atom to which a 5-6 membered ring is attached which, apart from the nitrogen atom, can also comprise 0-1 additional heteroatoms of the group of NH, N 1-6 alkyl, oxygen and sulfur; R20, R22, R23 independently of each other H, C1-8 alkyl; R24, R25 independently of each other H, C1-6 alkyl; R26 H, C1-6 alkyl, aryl; preferably H or C1-6 alkyl; x 'is 0, 1, 2, 3, 4, 5 or 6; R27 H, C1-6 alkyl; X S, O, C (R30) = C (R30 ');R30, R30 'independently from each other H, F, CI, Br, I, OH, CF3, NO2, CN, OCF3, O-C1-6 alkyl, O-C1-4 alkoxy-C1-4 alkyl, S-C1 alkyl -6, C1-6 alkyl, C2-6 alkenyl, C3-8 cycloalkyl, C3-8 O-cycloalkyl, C3-8 cycloalkenyl, C2-6 alkynyl, or aryl optionally substituted with F, Cl, Br, O-C1 alkyl -6 or C1-6 alkyl; To a link or linker that has 1 to 8 members, where the members are selected from the group consisting of O, S, SO2, N (R31),CO C (R32) (R33)C (R34) 3DC (R34)cyclopropylene, CsC, resulting in a chemically reasonable radical; R31, R34, R34 'independently from each other H, C1-8 alkyl; R32, R33 independently of each other H, C1-6 alkyl, OH, or O-C1-6 alkyl; B H, N (R35) (R36),1. Hydroxy-c1-4 tar, c1-8 tar, Alcoy c1-4-c1-4-tar, C1-4 alquenilo C2-8, c12-8 tar, a monkey ring,Double...tri- o espiroc clico de 3 a 10 miembros que puede comprender de 0 a 4 hetero tomos seleccionados entre el grupo de ox geno nitrogeno y azufre donde el sistema de anillos puede estar sustituido adicionalmente con uno oms de los siguientes sustituyentes F CI Br CF3 NO2 CON (R38) (R39)hidroxi COO (R40)N (R41) COalquilo C1-6 N (R42) (R43)a. So2ch3, ScF3 or s-asphalt C1-6; or the ring system can be connected with a through = C (r43);R35, R36, R37, R38, R39, R40, R41, R42, R43 independently of each other H, C1-8 alkyl; or R38 and R39, R42 and R43 form independently of each other optionally together with the nitrogen atom to which a 5-6 membered ring is attached which, apart from the nitrogen atom, can also comprise 0-1 additional heteroatoms of the NH group , N 1-6 alkyl, oxygen and sulfur; Q mono-ring structure,Double...For a saturated or partially unsaturated three ring helix, select one nitrogen atom and 0-3 additional heteroatoms from group n or group s. The rings on the structure can be helix unity, capacitance or connection, The ring system can be combined with one or more of the following alternatives: F, oh, CF3, CN, ocf3, oxo, o-tar c1-8, Alcoy c1-4-c1-4-tar, C1-6 tar, alquenilo c2-6, c12-6 tar, CO (R44),(C (R45) (R46)) or -R47, CO (C (R45) (R46)) p-R48, where Q comprises at least two atoms of N; R44 H, C1-8 alkyl; R45, R46 independently of each other H, C1-8 alkyl, OH, C3-8 cycloalkyl, or C1-4 alkoxy-C1-4 alkyl; or, p independently from each other 0, 1, 2, 3, 4, 5 or 6; R47, R48 independently of each other OH, F, O-C1-8 alkyl, CON (R49) (R50),N (R51) CO (R52)N (R53) (R54)CO2 (R55)So2me, CN, a 3-10 ring system consisting of 0 to 3 heteroatoms selected from group n or group s, can be replaced by one or more of the following alternatives: F, CI, Br, CF3, c1-8 tar, c1-8 tar, alcoxi c1-4-c1-4 tar, CO (R56),oxo, OH; R49, R50, R51, R52, R55, R56 independently of each other H, C1-8 alkyl; or R49 and R50 optionally form together with the nitrogen atom to which a 5-6 membered ring is attached which, apart from the nitrogen atom, can also comprise 0-1 additional heteroatoms of the NH group, N-C1-6 alkyl , oxygen and sulfur; R53, R54 independently of each other H, C1-8 alkyl, C1-4 alkoxy-C1-4 alkyl, C3-8 alkenyl, C3-8 alkynyl, CO (R57),(C (R58) (R59)) q-R60 CO (C (R61) (R62)) r-R63 CO-O-alquilo C1-8 o R53 y R54 forman junto con el tomo de nitrogeno al que est n unidos un Double...O 4 to 10 member helical helices, in addition to nitration atoms, include 0 to 3 other heteroatoms selected from group n, O and s, and can be replaced by one or more of the following substitutes: F, CI, Br, CF3, c1-8 tar, C1-6 tar, CO (R64),Oxy, oh, alcoxi c1-4-c1-4-tar, c1-4-alkyl, with (R65) (R66),N (R67) CO (R68)N (R69) (R70)CO2 (R71)and SO2-C1-6 alkyl; R58, R59 independently of each other H, C1-6 alkyl, or OH; R57, R61, R62, R64, R65, R66, R67, R68, R69, R70, R71 independently of each other H, C1-6 alkyl; or R69 and R70 optionally form together with the nitrogen atom to which a 5-6 membered ring is attached which, apart from the nitrogen atom, can also comprise 0-1 additional heteroatoms of the NH group, N-C1-6 alkyl , oxygen and sulfur; q, r independently from each other 0, 1, 2, 3, 4, 5 or 6; R60, R63 independently of each other OH, F, O-C1-6 alkyl, CN, COO (R78),N (R74) COalquilo C1-6 N (R76) (R77)And (R72) (R73),So2-c1-6, a monkey ringThe helix of b1-o 3-12 members, which may include one or more N, O and s heteroatoms, and the ring of 3-12 members may include additional substitutes, such as F, CI, Br, oh, CF3, NO2, CN, ocf3, oxo, o-hc-6, alcox c1-4-tar, C1-4, C1-4 salicylic, C1-6, C1-6 tar, alquinio c2-6, Cycloquinolo C3-8, o-cycloquinolo C3-8, cycloquinolo C3-8, o-cycloquinoo C3-8, tar layer c2-6, n (R76) (r77),COO (R78)So2-c1-8 and COOH; R72, R73, r74, R76, r77, R78, regardless of whether h, c1-8, or R72 and R73, R76 and r77 form a ring of 5-6 members separately with the nitrogen atoms attached together, except for nitrogen atoms, It may also include additional 0-1 heteroatoms of the NH group, C1-6 normal tar, oxygen and sulfur. If q is a single ring structure consisting of 6 to 7 members, thenhaving a nitrogen atom and an additional nitrogen atom where group Q is attached to the radical of formula (2) by a nitrogen atom of the ring of group Q; B is a non-aromatic ring, where the additional meanings for B have the meanings mentioned above for B; and in case Q is a monocyclic ring structure, saturated with 5 to 7 members, which has a nitrogen atom and no additional heteroatom, where the ring structure is substituted with a substituent (C (R45) (R46)) o-R47, where R47 is N (R53) (R54) and group Q is attached to the radical of formula (2) by a nitrogen atom of the ring of group Q;B is not an unreplaced phenyl ring.

机译：第1项：式化合物（1）这是指R1，R1'，R1“ .R1”'彼此独立地为H，F，Cl，Br，I，OH，CF3，NO2，CN，OCF3，O- C1-6烷基，O-C1-4烷氧基-C1-4烷基，S-C1烷基-6，C1-6烷基，C2-6烯基，C3-8环烷基，O3-8环烷基，C3-8环烯基，C2 -6炔基，C0-8-芳基亚烷基，C0-8-芳基O-亚烷基，S-芳基，N（R3）（R4），So2-ch3，COOH，COO沥青C1-6，con（R5）（R6 ），N（R7）CO（R8）N（R9）SO2（R10）CO（R11）（C（R12）（R13））xO（R14）R3，R4，R5，R6，R7，R9彼此独立H，C 1-8烷基;或R 3和R 4，R 5和R 6任选彼此独立地与连接有5-6元环的氮原子一起形成，该氮原子除氮原子外还可包含0-1 NH基团的另外的杂原子，N 1-8烷基，氧和硫; R8，R10，R11彼此独立地为H，C1-8烷基; R12，R13彼此独立地为H，C1-8烷基; R14 H， C 1-6烷基，芳基; x为0、1、2、3、4、5或6; R2 H，F，Cl，Br，I，OH，CF3，NO2，CN，OCF3，OC 1-6烷基，O-C1-4烷氧基C1-4烷基，S-C1-6烷基，C1-6烷基，C2-6烯基，C3-8环烷基，O-环喹啉C3-8，环喹啉C3-8，焦油c2-6，c0-8-arilo，o-coquileno c0-8-arilo，s-arilo，n（R15）（R16），So2-ch3，COOH，COO沥青C1-6，con（R17）（R18 ），N（R19）CO（R20）N（R21）SO2（R22）CO（R23）（C（R24）（R25））x -O（R26）R15，R16，R17，R18，R19，R21独立于彼此为H，C1-8烷基;或R 15和R 16，R 17和R 18彼此独立地形成，并且任选地与连接有5-6元环的氮原子一起形成，除氮原子之外，该氮原子还可以包含NH基团的0-1个额外的杂原子，N 1-6烷基，氧和硫; R20，R22，R23彼此独立地为H，C1-8烷基; R24，R25彼此独立地为H，C1-6烷基; R 26 H，C 1-6烷基，芳基;优选H或C1-6烷基; x'是0、1、2、3、4、5或6; R 27 H，C 1-6烷基; XS，O，C（R30）= C（R30'）; R30，R30'彼此独立地为H，F，Cl，Br，I，OH，CF3，NO2，CN，OCF3，O-C1-6烷基， O-C1-4烷氧基-C1-4烷基，S-C1烷基-6，C1-6烷基，C2-6烯基，C3-8环烷基，C3-8 O-环烷基，C3-8环烯基，C2-6炔基;或任选地被F，Cl，Br，O-C1烷基-6或C1-6烷基取代的芳基;到具有1到8个成员的链接或链接者，其中成员选自O，S，SO2，N（R31），CO C（R32）（R33）C（R34）3DC（R34）环丙烯CsC，产生化学上合理的自由基; R31，R34，R34'彼此独立地为H，C1-8烷基; R32，R33彼此独立地为H，C1-6烷基，OH或O-C1-6烷基; B H，N（R35）（R36），1。羟基C1-4焦油，C1-8焦油，Alcoy C1-4-C1-4焦油，C1-4 Alquenilo C2-8，C12-8焦油，猴环，双... 3 a 10 miembros que puede comprender de 0 a 4异形seleccionados entre el grupo de ox genonitroo y azufre donde el sistema de anillos puede estar sustituido adicionalmente con uno oms de los siguients F39（2） hidroxi COO（R40）N（R41）COalquilo C1-6 N（R42）（R43）a。 So2ch3，ScF3或S-沥青C1-6;或环系统可以通过直通＝ C（r43）连接; R35，R36，R37，R38，R39，R40，R41，R42，R43彼此独立地为H，C1-8烷基。或R38和R39，R42和R43彼此独立地任选地与连接有5-6元环的氮原子一起形成，该氮原子除氮原子外还可包含0-1个NH基团的另外的杂原子， N 1-6烷基，氧和硫; Q单环结构，双...对于饱和或部分不饱和的三环螺旋，从n组或s组中选择一个氮原子和0-3个其他杂原子。结构上的环可以是螺旋单元，电容或连接。环系统可以与以下一种或多种替代品组合：F，oh，CF3，CN，ocf3，oxo，o-tar c1-8，Alcoy c1 -4-c1-4-tar，C1-6 tar，alquenilo c2-6，c12-6 tar，CO（R44），（C（R45）（R46））或-R47，CO（C（R45）（R46 ））p-R48，其中Q包含至少两个N原子; R44 H，C1-8烷基; R45，R46彼此独立地为H，C1-8烷基，OH，C3-8环烷基或C1-4烷氧基-C1-4烷基;或者，p彼此独立地为0、1、2、3、4、5或6; R47，R48彼此独立OH，F，O-C1-8烷基，CON（R49）（R50），N（R51）CO（R52）N（R53）（R54）CO2（R55）So2me，CN，a由10个从n组或s组中选择的3至3个杂原子组成的3-10环系统可被以下一种或多种替代物取代：F，CI，Br，CF3，c1-8焦油，c1-8焦油，醇盐c1-4-c1-4焦油，CO（R56），氧代，OH; R49，R50，R51，R52，R55，R56彼此独立地为H，C1-8烷基;或R49和R50任选与连接有5-6元环的氮原子一起形成，除氮原子外，该氮原子还可包含0-1个NH基团的另外的杂原子，N-C1-6烷基，氧和硫; R53，R54彼此独立地H，C1-8烷基，C1-4烷氧基-C1-4烷基，C3-8烯基，C3-8炔基，CO（R57），（C（R58）（R59））q-R60 CO（C（R61）（R62））r-R63 CO-O-alquilo C1-8 o R53和R54 forman un Double ... O 4至10个成员螺旋螺旋，除了硝化原子外，还包括选自n，O和s组的0至3个其他杂原子，并且可以被以下一个或多个替代物取代：F，CI ，Br，CF3，c1-8焦油，C1-6焦油，CO（R64），Oxy，哦，醇类c1-4-c1-4-tar，c1-4-烷基，（R65）（R66），N （R67）CO（R68）N（R69）（R70）CO2（R71）和SO2-C1-6烷基; R58，R59彼此独立地为H，C1-6烷基或OH; R57，R61，R62，R64，R65，R66，R67，R68，R69，R70，R71彼此独立地为H，C1-6烷基;或R69和R70任选与连接有5-6元环的氮原子一起形成，除氮原子外，该氮原子还可包含0-1个NH基团的另外的杂原子，N-C1-6烷基，氧和硫; q，r彼此独立地为0、1、2、3、4、5或6; R60，R63彼此独立OH，F，O-C1-6烷基，CN，COO（R78），N（R74）COalquilo C1-6 N（R76）（R77）和（R72）（R73），So2- c1-6，猴环b1-o 3-12成员的螺旋，可包括一个或多个N，O和s杂原子，而3-12成员的环可包括其他取代基，例如F，CI，Br ，哦，CF3，NO2，CN，ocf3，氧代，o-hc-6，alcox c1-4-tar，C1-4，C1-4水杨酸，C1-6，C1-6 tar，alquinio c2-6，Cycloquinolo C3-8，邻环喹啉C3-8，环喹啉C3-8，邻环喹啉C3-8，焦油层c2-6，n（R76）（r77），COO（R78）So2-c1-8和COOH; R72，R73，r74，R76，r77，R78，无论h，c1-8或R72与R73，R76和r77是否分别形成5-6个成员的氮原子相连的环，除了氮原子，它还可能包括NH基团的额外0-1个杂原子，C1-6正构焦油，氧和硫。如果q是由6至7元组成的单环结构，则具有一个氮原子和一个额外的氮原子，其中Q基团通过Q基团的环的氮原子与式（2）的基团连接; B是非芳族环，其中B的附加含义具有以上针对B的含义;在Q是一个5到7个成员饱和的单环环结构中，它具有一个氮原子并且没有其他杂原子，其中该环结构被取代基（C（R45）（R46））o-R47取代，其中R47为N（R53）（R54），基团Q通过基团Q的环的氮原子连接于式（2）的基团; B不是未取代的苯环。

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公开/公告号AR059521A1

专利类型
公开/公告日2008-04-09

原文格式PDF
申请/专利权人 SANOFI-AVENTIS DEUTSCHLAND GMBH;
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申请/专利号AR2007P100660
发明设计人
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申请日2007-02-15
分类号C07D239/91;C07D403/10;C07D491/04;C07D495/04;C07D519/00;A61K31/4355;A61K31/4365;A61K31/506;A61K31/513;A61P3/00;
国家 AR
入库时间 2022-08-21 20:08:58

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