首页> 外国专利> Adenosine A2A Receptor Antagonists of amino - 5 - 1,2,4 - triazole bicyclic, Pharmaceutical compositions containing the same, alone or in combination of the compounds and other agents for Preparation of Drugs useful in the treatment of Parkinson's disease and a

Adenosine A2A Receptor Antagonists of amino - 5 - 1,2,4 - triazole bicyclic, Pharmaceutical compositions containing the same, alone or in combination of the compounds and other agents for Preparation of Drugs useful in the treatment of Parkinson's disease and a

机译:氨基-5-[1,2,4]-三唑双环的腺苷A2A受体拮抗剂,药物组合物,单独或以化合物的形式或与化合物和其他药物组合使用,用于制备可用于治疗帕金森氏病和

摘要

1. A 5-amino-1, 2, 4-tricyclic compound represented by structural formula (1) or salt acceptable to the drug, wherein a is C (R1) or N; R1 and R1a are independently selected from group h-asphalt (C1-6),Halo, CN and CF3, this is - O,- yes.-So...-SO2...R5 isopropyl glycol, R5 arileno or some other formula (2);P and Q are independent 2-3; Q and Q1 are selected independently from the following groups: n, CH, CCN, COH and CC (o) CH3, provided that at least one Q and Q1 is n; R is R5 arilo, R5 direct arilo, R6 alquelino (c2-6) or R6 asphalt (c2-6);R2 is R5 arilo, R5 heterogeneous, R5 aril asphalt (C1-6) or R5 heterogeneous asphalt (C1-6);O r2-y as shown in the structure (3);U. V, and W are selected independently from group n and CR1, provided that at least one u, V and W is CR1; n is 1, 2 or 3; and (a) a is C (R1) and X is C (R3) (R3a).-C (O) -- that is...- yes.-So...-SO2...R4 arileno, R4 tremolite, o-n (R9) -,Or C (R1),This is a link, and X is - C (R3) (R3a)-C (O) -- that is...- yes.-So...-SO2...R4-arileno -N (R9) -e. Or R4 - tremolite, if x sea-n (R9) - or R4 - tremolite, R2 - non phenyl or phenyl - hydrocarbon (C1-6);Or (b) a is n, X is - n (R9) -,This is R5 arileno and R2 is a residual formula (4) or n is 2 or 3; and (c) a is n and X is - C (R3) (R3a).-C (O) -- that is...- yes.-So...-SO2...-N (R9) -R4 arileno or R4 tremolite; or a is n, is a link and X is - C (o) -,-N (R9) -R4 arileno R4 tremolite; or a is n, and a is n (r9a),-C (o) n (r9a) - O-O (CH2) 2-N (r9a) - and xes-n (R9) -;O a is n, X is n (R9) - E and R2, as a whole, structure (4) and N are 0; Y (d) is n, is a link, X is n (R9), R2 is selected from formula group (5);O (E) a is n, X is - n (R9) - E and R2 are added together, as shown in formula (6);Where Z is - C (o) - CH2,-C (o) - CH (C1-6 tar) -,-CH2CH (C1-6 tar) -,1. O-ch (C1-6 tar) - CH2 -;R3 and R3a are independently selected from the group consisting of H, -OH, C1-6 alkyl, hydroxy-C1-6 alkyl,2. Alcoxi (C1-6) - tar (C1-6),Carbamate (C1-6),1. Lease (C1-6) - Asphalt (C1-6) and diaklamine (C1-6) - Asphalt (C1-6);R4 is a 1-3 alternative selected from class H asphalt (C1-6),-Oh, alcoxi (C1-6),alcoxi (C1-6) -alcoxi (C1-6)Halo -, CF3 and CN; R5 are 1-3 alternatives selected from class H asphalt (C1-6),-Oh, alcoxi (C1-6),2. Alcoxi (C1-6) - tar (c1-9);alcoxi (C1-6) -alcoxi (C1-6)Halo, CF3, CN, NH2, rental (C1-6),dialquilamino (C1-6)1. Amino tar (C1-6),1. Lease (C1-6) - Bitumen (C1-6),1. Cumin (C1-6) - tar (C1-6),Alkane (C1-6) - ammonia, amine sulfite (C1-6),Bitumen (C1-6),Bitumen (C1-6) - Bitumen (C1-6),R6-alquenilo (C2-6)R6 asphalt (c2-6),Hydroxy asphalt (C1-6),2. Alcox (C1-6) - C (o) - amine, or isopropyl tar (C1-6);R6 is one to three alternatives selected from class H asphalt (C1-6),Oh, alcoxi (C1-6) and halo; R7 and r7a are independently selected from class H asphalt (C1-6),2. Alcoxi (C1-6) - tar (C1-6),R8 arilo and R8 heterosexual, or R7 and r7a substitutes in the same carbon can form = O; R8 is a 1-3 substitute independently selected from h, hydrocarbon (C1-6),-Oh, alcoxi (C1-6),alcoxi (C1-6) -alcoxi (C1-6)Halo -, CF3 and CN; R9 and r9a were selected independently from the h-tar (C1-6) group,Hydroalkyl (c2-6),2. Alcoxi (C1-6) - Asphalt (c2-6),1. Amino asphalt (c2-6),1. Rental (C1-6) - Asphalt (c2-6),1. Cumin (C1-6) - tar (c2-6),halo-alquelino (C3-6)CF3 tar (C1-6),alquenilo (C3-6)Bicycle (C3-6),e. Cyclopentanediol (C3-6) - Asphalt (C1-6);R10 is H-C (o) - o-asphalt (C1-6),R5 arilo, C (o) - Bitumen (C1-6),-C (o) - (R5 arilo) or R5 aril acquilo (C1-6). Drugs used to treat Parkinson's disease, used alone or in combination with other drugs to treat Parkinson's disease, drug synthesis to understand Parkinson's disease, and toolkits including composite components.
机译:1.一种结构式(1)表示的5-氨基-1、2、4-三环化合物或药物可接受的盐,其中a为C(R1)或N; R1和R1a独立选自h-沥青(C1-6),卤素,CN和CF3,这是-O,-是。-So ...- SO2 ... R5异丙基丙二醇,R5阿列里诺或其他一些式(2); P和Q独立为2-3; Q和Q1独立地选自以下组:n,CH,CCN,COH和CC(o)CH3,条件是至少一个Q和Q1为n。 R是R5 arilo,R5直接arilo,R6 alquelino(c2-6)或R6沥青(c2-6); R2是R5 arilo,R5异质,R5假种皮沥青(C1-6)或R5异质沥青(C1-6)如结构(3)所示; O r2-y; U。 V和W独立地选自组n和CR1,条件是u,V和W中至少一个是CR1。 n为1、2或3; (a)a是C(R1)和X是C(R3)(R3a)。-C(O)-即...-是。-所以... -SO2 ... R4 arileno,R4透闪石,在(R9)-或C(R1)上,这是一个链接,而X是-C(R3)(R3a)-C(O)-即...-是.-所以... -SO2 ... R4-芳基-N(R9)-e。或R4-透闪石(如果x sea-n(R9)-或R4-透闪石,R2-非苯基或苯基-烃(C1-6);或(b)a为n,X为-n(R9)-,这是R5 arileno,R2是残基式(4)或n是2或3; (c)a是n并且X是-C(R3)(R3a)。-C(O)-即...-是.-所以...- SO2 ...- N(R9)- R4 arileno或R4透闪石;或a为n,为连接,且X为-C(o)-,-N(R9)-R4阿里瑞诺R4透闪石;或或a为n,并且a为n(r9a),-C(o)n(r9a)-OO(CH2)2-N(r9a)-和xes-n(R9)-; O a为n,X为n(R9)-E和R2整体上,结构(4)和N为0; Y(d)是n,是一个链接,X是n(R9),R2从公式组(5)中选择; O(E)a是n,X是-n(R9)-E和R2加在一起,如式(6)所示;其中Z为-C(o)-CH 2,-C(o)-CH(C 1-6焦油)-,-CH 2 CH(C 1-6焦油)-,1。 O-ch(C 1-6焦油)-CH 2-; R 3和R 3a独立地选自H,-OH,C 1-6烷基,羟基-C 1-6烷基,2。酒精(C1-6)-焦油(C1-6),氨基甲酸酯(C1-6),1。租约(C1-6)-沥青(C1-6)和重胺(C1-6)-沥青(C1-6); R4是1-3替代品,选自H级沥青(C1-6),-Oh,醇(C1-6),醇(C1-6)-醇(C1-6)卤素-,CF3和CN; R5是选自H级沥青(C1-6),-Oh,醇(C1-6),2的1-3个替代物。酒精(C1-6)-焦油(c1-9);酒精(C1-6)-酒精(C1-6)卤素,CF3,CN,NH2,租用(C1-6),二基氨基(C1-6)1。氨基焦油(C1-6),1。租赁(C1-6)-沥青(C1-6),1。小茴香(C1-6)-焦油(C1-6),烷烃(C1-6)-氨,亚硫酸胺(C1-6),比妥(C1-6),比妥(C1-6)-沥青(C1-6) ),R6-alquenilo(C2-6)R6沥青(c2-6),羟基沥青(C1-6),2。 Alcox(C1-6)-C(o)-胺或异丙基焦油(C1-6); R6是从H级沥青(C1-6),Oh,酒精(C1-6)和卤素中选择的一种或三种选择; R7和r7a分别选自H级沥青(C1-6),2。 Alcoxi(C1-6)-焦油(C1-6),R8 arilo和R8是异性的,或者同一碳原子上的R7和r7a取代基可以形成= O; R8是1-3个独立地选自h,烃(C1-6),-Oh,醇(C1-6),醇(C1-6)-醇(C1-6)-卤素,CF3和CN的取代基; R 9和r 9a独立选自h-tar(C 1-6)基,氢烷基(c 2-6)2。酒精(C1-6)-沥青(c2-6),1。氨基沥青(c2-6),1。出租(C1-6)-沥青(c2-6),1。小茴香(C1-6)-焦油(c2-6),卤代-alquelino(C3-6)CF3焦油(C1-6),alquenilo(C3-6)自行车(C3-6),e。环戊二醇(C3-6)-沥青(C1-6); R10为HC(o)-邻沥青(C1-6),R5 arilo,C(o)-沥青(C1-6),-C(o) -(R5 arilo)或R5 aril acquilo(C1-6)。用于治疗帕金森氏病的药物,可单独使用或与其他药物组合用于治疗帕金森氏病,用于了解帕金森氏病的药物合成,以及包括复合成分的工具包。

著录项

  • 公开/公告号AR037681A1

    专利类型

  • 公开/公告日2004-12-01

    原文格式PDF

  • 申请/专利权人 SCHERING CORPORATION;

    申请/专利号AR2002P104562

  • 发明设计人

    申请日2002-11-27

  • 分类号C07D487/14;A61K31/505;A61P25/00;A61P25/16;C07D487/14;C07D239/00;C07D249/00;

  • 国家 AR

  • 入库时间 2022-08-21 22:18:52

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号