首页> 外国专利> Therapeutic agent for hepatitis C that includes a Condensed Ring Compound, Condensed Ring Compound, Pharmaceutical composition containing Same, thiazole and benzimidazole biphenyl Compounds, useful as Intermediates for producing Said Compounds, the use of compound Ring

Therapeutic agent for hepatitis C that includes a Condensed Ring Compound, Condensed Ring Compound, Pharmaceutical composition containing Same, thiazole and benzimidazole biphenyl Compounds, useful as Intermediates for producing Said Compounds, the use of compound Ring

机译:丙型肝炎治疗剂,包括稠环化合物,稠环化合物,含有相同化合物,噻唑和苯并咪唑联苯化合物的药物组合物,可用作制备所述化合物的中间体,化合物环的用途

摘要

Therapeutic agent for hepatitis C comprising a fused ring compound of the formula [1] where a dotted line is a single bond or a double bond; G1 is C (-R1) or a nitrogen atom; G2 is C (-R2) or a nitrogen atom; G3 is C (-R3) or a nitrogen atom; G4 is C (-R4) or a nitrogen atom; G5, G6, G8 and G9 are each independently a carbon atom or a nitrogen atom; G7 is C (-R7),An oxygen atom, a sulfur atom, or an optional nitrogen atom, is replaced by R8; wherein R1, R2, R3 and R4 are each hydrogen atoms, regardless of their (1) alkane C1-6, (3) hydrogen carbide, (4) cyanogen, (5) nitro, (6) C1-6 tar, they can be replaced by 1 to 3 substitutes in the next group. A. [group: halogen atom, one hydroxyl group, carboxilo, amino, alcoxi C1-6, alcoxi c1-6alcoxi C1-6, alcoxin C1-6 and rental C1-6],(7) - cora1, where ra1 is a C1-6 tar, optionally replaceable (as defined above) or aril C6-14 tar, optionally replaceable with 1 to 5 selected substitutes from group B, [group B: halogen, cyanogen, nitrogen, C1-6 tar, C1-6 halogenated tar, C1-6 alkane, C1-6, - (CH2) r-corb1, -(N2R and N2R are independent, A hydrogen atomC1-6 or alternative C1-6 tar (as described above),(9) - C (= nra4) NH2, where RA4 is a hydrogen atom or oxyhydrogen compound, (10) - nhr5, where ra5 is a hydrogen atom, C1-6 alkane or C1-6 alkylsulfonate (11) - RA6, where RA6 is a hydrogen atom or alternative C1-6 tar (as described above),(12) - so2ra7, where ra7 is a hydroxy, amino, C1-6 tar or hired C1-6, or (13) - P (= O) (ora31) 2, where ra31 is a hydrogen atom, C1-6 tar (as described above) or aril C6-14 tar (C1-6) is an optional alternative, replaced by 1 to 5 alternatives selected in the previous group B, Y (14) one to four heteromorphic atoms selected from the oxygen atom, one nitrogen atom and one sulfur atom; R7 and R8 are an alternative C1-6 hydrogen atom or tar, respectively (as described above);Propyl O (3) the remaining formulas [2], [3], [4] or [5], where u and V are independent,Integers 1 to 3; ring a is (1) arilo C6-14, (2) cycloquilo C3-8, (3) cycloquenio C3-8, or (4) a heteromorphic group consisting of 1 to 4 heteromorphic atoms selected from oxygen, nitrogen, and sulfur atoms; R5 and R6 are (1) a hydrogen atom, (2) a halogen atom, and (3) C1-6 tar, respectively. Options (as mentioned above),O (4) - or8, wherein ra8 is a hydrogen atom, C1-6 tar or aril C6-14 tar C1-6; X is (1) hydrogen atom, (2) halogen atom, (3) cyanogen, (4) nitrogen, (5) amine, alkane C1-6, (6) C1-6 tar, C1-6 alternative (as described above),(8) Alquenilo c2-6 can optionally replace the original a (9) - cora9 with a 1-3 substitute, wherein ra9 is a hydrogen atom or C1-6 (10) - CONH - (CH2) l-ra10, and RA10 is an optional substitute for C1-6 (as described above),C1-6 or C1-6 alkanes and L are 0 or integers 1 to 6, (11) - ora11, where Ra11 is a hydrogen atom or alternative C1-6 hydrocarbon (as defined above).O (12) a formula compound in which the B ring is (1 ') arilo C6-14, (2') C3-8 cyclo, or (3 ') as described above, a heterocyclic group;Each Z is a D group (1 ') selected from the next D group (2'), arilo C6-14 is optionally replaced by 1 to 5, C3-8 cyclopropyl compound selected from the next D group (3 '), and optionally by 1 to 5 to replace the alternative selected from the next D group, 1.2.2 (4 ') aril c6-14c6-14oquile C1-6 is optionally replaced by 1-5 selected substitutes in group D below, or (5') by 1-5 selected substitutes in group D below. In group D, there are 1-4 non atoms selected from oxygen and nitrogen atoms in the heterocycle group. And sulphur.6. [(6 ') C1-6 selects an aperiodic tar to replace with 1-5 of the following alternatives selected in group D, in which case, C1-6 selects an aperiodic tar to replace with C1-6, a set of alternative alternatives to replace with 1-5 alternatives selected in group D; [as mentioned above, group D: (a) an atom Hydrogen, (b) halogen atom, (c) cyanogen, (d) nitrogen, (E) C1-6 tar alternative (as described above),(f) - (CH2) t-cor18 (from now on, each T represents an independent, 0 or 1 to 6 integer)Ra18 is an (1 ') C1-6 alternative (as described above),(2 ') arilo C6-14 is selectively replaced by 1-5, replacing the non periodic group selected in the previous group B or (3'), replacing the non periodic group selected in the previous group B, with 1-4 non normal atoms selected from oxygen, nitrogen and sulfur atoms, (g) - (CH2) t-coor19, wherein ra19 is a hydrogen atom, C1-6 tar can be replaced optionally (as defined above), or aril c6-14c1-6 can be replaced optionally by 1-5 instead of the original B (H) - (CH2) t-conra27ra28, wherein RA27 and RA28 are independent,(1 ') a hydrogen atom (2') C1-6 tar alternative (as described above),3 '(3') arilo C6-14 is selectively changed to 1-5, replacing (4 ') aril c6-14c6-14c6-14c6 selected in the original group B, optionally changing to 1-5, replacing (s) selected in the original group B, (5') an alternative non periodic group, changing to (s) selected in the previous group B, (6 '. " The alternative C1-6 aperiodic heterocyclic tar cycle is replaced by one to five selected substitutes from the former group B, wherein the C1-6 aperiodic hybrid tar cycle is C1-6 tar, replaced by one optional aperiodic group, replacing one to five selected substitutes from the former group B,1. As defined above, (7 ') cycloquilo C3-8 can be optionally replaced by 1 to 5, and (8') cycloquil c3-8c1-6 or (8 ') cycloquil c3-8c1-6 selected from the previous group B can be optionally replaced by 1 to 5, replacing (9') hydroxy or (10 '' alcox C1-6 selected from the previous group B, (i) - (CH2) T-C (= nra33) NH2, wherein RA33 is a hydrogen atom or C1-6 hydrocarbon group, a group of hydroxyl groups or alcoxi C1-6, (J) - (CH2) t-or20, wherein RA20 is (1) (` 1 ') a hydrogen atom, (2'), C1-6 optional alternative tar (as defined above),(3 "alquenilo c2-6 alternative, as described above),1. (4 ') to replace (5') arilo C6-14 selected in the original group A with 1 to 3, to replace (6 ') aril C6-14 selected in the original group B with 1 to 5, to replace (7') selected in the original group B. 1-5 is used to replace 1-6 aperiodic C1-6 asphalt selected in group B, 1-5 (9 ') cyclo-8 alternative selected in group B, and 1-5 (s) selected in group B,O (10 ') cycloquil c3-8c1-6 was voluntarily replaced with the selected substitute in the group B (k) - (CH2) t-o (CH2) p-cora21 before 1-5, wherein ra21 was ammonia water and C1-6 or optional non periodic group was rented instead of 1-5 substitute selected in group B, P was 0 or 1-6 integer, (l) - (CH2) t-nra2ra23, wherein ra22 and ra23 are independent hydrogen atoms respectively, (1 ') (2') C1-6 optional replacement tar (as defined above),(3 ') arilo C6-14 is replaced by alternatives 1 to 5, replacing the 1 to 5 selected in the original group B, (4') aril c6-14c6-14 tar, alternative 1 to 5 selected in the former group B, or (5 ') C1-6 aperiodic alternative to the 1 to 5 selected in the former group B, (6 ') the alternative aperiodic group is replaced by 1 to 5, replacing some C1-6 or C1-6 alkane atoms selected in the previous group B (m) - (CH2) t-ra29co-ra24, ra24 is hydrogen atom, C1-6 or C1-6 alkane atom, ra24 is ammonia water (1'), (2 ') lease C1-6, C1-6, 3',(4 ') arilo C6-14 is selectively changed to 1-5, replacing the (5') non periodic alternative selected in the previous group B, replacing the (s) or (6 ') non periodic condensate reservoir selected in the previous group B with 1-5.
机译:丙型肝炎治疗剂,其包含式[1]的稠环化合物,其中虚线为单键或双键; G1为C(-R1)或氮原子; G 2为C(-R 2)或氮原子; G3为C(-R3)或氮原子; G4为C(-R4)或氮原子; G5,G6,G8和G9各自独立地为碳原子或氮原子; G7为C(-R7),氧原子,硫原子或任选的氮原子被R8取代;其中R 1,R 2,R 3和R 4均为氢原子,而与它们的(1)烷烃C1-6,(3)碳化氢,(4)氰,(5)硝基,(6)C1-6焦油无关。在下一组中被1-3个替代品替代。 A. [组:卤素原子,一个羟基,羧酸根,氨基,alcoxi C1-6,alcoxi c1-6alcoxi C1-6,alcoxin C1-6和Rent C1-6],(7)-cora1,其中ra1是C1-6焦油,可选地可替换(如上定义)或假种C6-14焦油,可选地可被B组的1-5个所选替代物替换,[B组:卤素,氰,氮,C1-6焦油,C1-6卤化焦油,C1-6烷烃,C1-6,-(CH2)r-corb1,-(N2R和N2R是独立的,氢原子C1-6或替代的C1-6焦油(如上所述),(9)-C( = nra4)NH2,其中RA4是氢原子或氢氧化合物,(10)-nhr5,其中ra5是氢原子,C1-6烷烃或C1-6烷基磺酸盐(11)-RA6,其中RA6是氢原子或替代的C1-6焦油(如上所述),(12)-so2ra7,其中ra7是羟基,氨基,C1-6焦油或租用的C1-6,或(13)-P(= O)(ora31)2,其中ra31是氢原子,C1-6焦油(如上所述)或Aril C6-14焦油(C1-6)是可选的替代物,由t中选择的1-5个替代物替代他先前的B,Y族(14)是从氧原子,一个氮原子和一个硫原子中选出的1-4个异质原子; R 7和R 8分别是一个可选的C 1-6氢原子或焦油(如上所述);丙基O(3)其余的式[2],[3],[4]或[5],其中u和V为独立,整数1到3;环a是(1)芳基C6-14,(2)环基C3-8,(3)环奎基C3-8或(4)由1至4个选自氧,氮和硫原子的杂晶原子组成的杂晶基团; R 5和R 6分别为(1)氢原子,(2)卤原子和(3)C 1-6焦油。选项(如上所述),O(4)-或8,其中ra 8是氢原子,C 1-6焦油或Aril C 6-14焦油C 1-6; X是(1)氢原子,(2)卤素原子,(3)氰,(4)氮,(5)胺,烷烃C1-6,(6)C1-6焦油,C1-6替代物(如上所述) ),(8)Alquenilo c2-6可以选择性地用1-3取代基代替原始的(9)-cora9,其中ra9是氢原子或C1-6(10)-CONH-(CH2)1-ra10, RA10是C1-6(如上所述)的可选替代物,C1-6或C1-6烷烃,L为0或1至6的整数,(11)-ora11,其中Ra11为氢原子或替代的C1- 6烃(如上定义)。O(12)式化合物,其中B环为(1')芳基C6-14,(2')C3-8环或(3')如上所述的杂环每个Z是选自下一个D组(2')的D基团(1'),arilo C6-14可选地被1-5个选自下一个D组(3')的C3-8环丙基化合物取代,并可选地用1到5替换从下一个D组中选择的替代物,1.2.2(4')假种皮c6-14c6-14oquile C1-6可选地用1-5个所选替代物替换在下面的D组中,或(5')被下面的D组中的1-5个选定的替代物取代。在组D中,在杂环基中有1-4个选自氧和氮原子的非原子。和硫6。 [(6')C1-6选择了一个非周期性焦油,以替换D组中所选的以下1-5个替代品,在这种情况下,C1-6选择一个非周期性焦油,以替换为C1-6,一组替代品用D组中选择的1-5种替代品替代; [如上所述,D组:(a)氢原子,(b)卤原子,(c)氰基,(d)氮,(E)C1-6焦油替代物(如上所述),(f)-( CH2)t-cor18(从现在开始,每个T代表一个独立的0或1至6整数)Ra18是(1')C1-6替代品(如上所述),(2')arilo C6-14被选择性地被1-5取代,替换先前的B组或(3')中选择的非周期性基团,替换先前的B组中选择的非周期性基团,并使用1-4个选自氧,氮和硫原子的非正态原子,(g)-(CH 2)t-coor 19,其中ra 19是氢原子,C 1-6焦油可以任选地被取代(如上所定义),或者C 6-14 c 1-6芳烃可以任选地被1-5代替原始的B(H)-(CH2)t-conra27ra28,其中RA27和RA28是独立的,(1')氢原子(2')C1-6焦油替代物(如上所述),3'(3')arilo C6-14选择性地更改为1-5,替换了(4')在原始B组中选择的假药c6-14c6-14c6-14c6,可选地更改为1-5,替换在原始组B中选择的(s),(5')替代非周期性组,更改为在先前组B中选择的(s),(6'。“替换的C1-6非周期性杂环tar循环被前B组中的1-5个选定的替代物取代,其中C1-6非周期性杂焦油循环为C1-6 tar,被一个可选的非周期性基团取代,从前一组B,1中替换一到五个选定的替代物。如上定义,(7')环基C3-8可以可选地被1-5取代,(8')环基c3-8c1-6或(8 ')从先前B组中选出的cycloquil c3-8c1-6可以任选地被1-5取代,取代(9')羟基或从先前B组中选出的(10''羟丙基C1-6,(i)-( CH2)TC(= nra33)NH2,其中RA33为氢原子或C1-6烃基,羟基或醇基C1-6,(J)-(CH2)t-or20,其中RA20为(1) ('1')氢原子,(2'),C1-6可选替代焦油(如上所述),(3“ alquenilo c2-6替代如上所述,),1。(4')代替(5 ')arilo C6-14在原始A组中选择为1至3,以替换(6')ar il用1至5在原始B组中选择的C6-14替换在原始B组中选择的(7')。1-5用于替换在B组中选择的1-6非周期性C1-6沥青,1-在B组中选择了5(9')个cyclo-8替代物,在B组中选择了1-5(s),O(10')将cycloquil c3-8c1-6自愿替换为B组中选择的替代物(k )-1-5之前的(CH2)至(CH2)p-cora21,其中ra21是氨水,租用了C1-6或可选的非周期性基团代替B组中选择的1-5个取代基,P为0或1- 6个整数,(l)-(CH2)t-nra2ra23,其中ra22和ra23分别是独立的氢原子,(1')(2')C1-6可选取代焦油(如上定义),(3')arilo C6 -14被替换为1-5,替换了原始B组中选择的1-5,(4')aril c6-14c6-14 tar,替代了先前B组中选择的1-5,或(5') C1-6非周期性替代方案,从前B组中选择1至5,(6')替代性替代方案ic基团被1到5取代,取代了先前基团B(m)-(CH2)t-ra29co-ra24中选择的一些C1-6或C1-6烷烃原子,ra24是氢原子,C1-6或C1- 6烷烃原子,ra24为氨水(1'),(2')租借C1-6,C1-6、3',(4')arilo C6-14选择性地更改为1-5,代替(5' )在上一组B中选择的非周期性替代物,用1-5替换在上一组B中选择的(s)或(6')非周期性凝析油藏。

著录项

  • 公开/公告号AR035543A1

    专利类型

  • 公开/公告日2004-06-16

    原文格式PDF

  • 申请/专利权人 JAPAN TOBACCO INC.;

    申请/专利号AR2002P102384

  • 发明设计人 HASHIMOTO SEIZO;MIZUTANI K.;YOSHIDA A.;

    申请日2002-06-25

  • 分类号C07D235/18;C07D417/12;C07D401/12;C07D409/12;C07D413/12;C07D235/30;C07D413/04;C07D401/04;C07D405/12;C07D401/14;C07D409/04;C07D405/04;C07D409/14;C07D417/14;C07D403/12;C07D209/12;C07D235/20;C07D495/04;C07D471/04;A61K31/4184;A61K31/427;A61K31/4439;A61K31/53;A61K31/496;A61K31/5377;A61K31/541;A61K31/4245;A61K31/433;A61K31/404;A61K31/4709;A61K31/551;A61K31/519;A61K31/437;A61K31/422;A61P31/12;A61P1/16;A61P43/00;

  • 国家 AR

  • 入库时间 2022-08-21 23:12:21

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