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- aryl oxime Piperazines Compounds, Pharmaceutical composition, the use of such compounds for the manufacture of Drugs useful as CCR5 antagonists and a Team

机译:-芳基肟哌嗪化合物,药物组合物,此类化合物在制备用作CCR5拮抗剂的药物中的用途和一个研究小组

摘要

1. Aril oxma piperazines compound, including Omer, stereoisomer, tumbler, tumbler and derivatives of the compound, as well as pharmaceutically acceptable salts or solutions of the compound or derivatives, with the General Pharmaceutical structure (1),Where x is selected from groups h, F, Cl, Br, I, CF3, cf3o, CN, ch3so2,And cf3so2 -;R1 is h, a C1-6 fluoro tar, C1-6 tar, rectal tar, or branched chain tar with c3-7 cyclopentadiene, such as cyclopentamethyl,-C1-6 SCCPs, C1-6, or C16, C16, or C16, or c15-6, or C16 (b) a. Hetero compounds of 6 members substituted by R4, R5 and R6; hetero oxides of 6 members substituted by R4, R5 and R6; hetero compounds of 5 members substituted by R7 and R8; Northwest fluorine; fluorodiphenyl; and other formulas (2);Or other formula (3);In which R4 and R5 may be the same or different, and are independently selected from a group containing C1-6, halogen, nr12r13, oh-cf3, OCH3, o-acilo, ocf3 and - Si (CH3) 3, R6 as R4, hydrogen, phenyl, NO2, CN, ch2f, chf2, CHO, ch = nor12, piridio, n (R12) and conr13r14, -Nhconh (chlorine - (C1-6) asphalt,-Nhonh (c3-10) cyclopentadiene (C1-6) tar,Nhco (C1-6) asphalt, - nhcof3, - nhso2n ((C1-6) asphalt) 2, - nhso2 (C1-6) asphalt, - n (so2cf3),-NHCO2 (C1-6) alkyl, C3-10 cycloalkyl, -SR15, -SOR15, SO2R15, -SO2NH (C1-6) alkyl, -OSO2 (C1-6) alkyl, -OSO2CF3, hydroxy (C1-6) alkyl , -CONR12R13, -CON (CH2CH2-O-CH3) 2, -OCONH (C1-6) alkyl, -CO2R2, -Si (CH3) 3 or -B (OC (CH3) 2);R7 is the tar of C1-6, NH2 or r9-phenyl; R9 is one to three substitutes, which can be the same or different, and is a group independent of hydrogen, C1-6, CF3, co2r12, CN, alcox C1-6 and halogenated substances; R10 and R11 may be the same or different and selected independently from the group consisting of C1-6 hydrogen and tar, or R10 and R11 together are a c2-5 tar group connected with carbon atoms to form a spiral of 3 to 6 carbon atoms; R12, R13 and R14 may be the same or different, separated from group H and C1-6 tar; R15 is C1-6 tar or phenyl;Pharmaceutical compounds containing one or more compounds used in the manufacture of drugs for the treatment, prevention and improvement of one or more diseases associated with CCR5 receivers, and devices containing a single package, A composite agent for the treatment of human immunodeficiency virus, including a drug ingredient in a container, which contains an effective amount of CCR5 antagonists, an acceptable drug carrier, and a separate package,1. One or more pharmaceutical ingredients, including an effective number of antiviral agents or other effective preparations for the treatment of human immunodeficiency virus with drug acceptable carriers.
机译:1.具有一般药物结构(1)的阿里莫克辛哌嗪化合物,包括该化合物的Omer,立体异构体,tumbler,tumbler和衍生物,以及该化合物或衍生物的可药用盐或溶液,其中x选自h,F,Cl,Br,I,CF3,cf3o,CN,ch3so2和cf3so2-; R1是h,C1-6氟焦油,C1-6焦油,直肠焦油或带有c3-7环戊二烯的支链焦油(b)a。由R4,R5和R6取代的6个成员的杂化合物;由R4,R5和R6取代的6个成员的杂氧化物;由R7和R8取代的5个成员的杂化合物;西北氟;氟二苯; R4和R5可以相同或不同,并且独立地选自C1-6,卤素,nr12r13,oh-cf3,OCH3,o- acilo,ocf3和-Si(CH3)3,R6为R4,氢,苯基,NO2,CN,ch2f,chf2,CHO,ch = nor12,piridio,n(R12)和conr13r14,-Nhconh(氯-(C1- 6)沥青,-Nhonh(c3-10)环戊二烯(C1-6)焦油,Nhco(C1-6)沥青,-nhcof3,-nhso2n((C1-6)沥青)2,-nhso2(C1-6)沥青-n(so2cf3),-NHCO2(C1-6)烷基,C3-10环烷基,-SR15,-SOR15,SO2R15,-SO2NH(C1-6)烷基,-OSO2(C1-6)烷基,-OSO2CF3,羟基(C1-6)烷基,-CONR12R13,-CON(CH2CH2-O-CH3)2,-OCONH(C1-6)烷基,-CO2R2,-Si(CH3)3或-B(OC(CH3)2) ; R7为C1-6,NH2或r9-苯基的焦油; R9为一至三个可相同或不同的取代基,且独立于氢,C1-6,CF3,co2r12,CN,醇C1-6和卤代物质; R10和R11可以相同或不同,可以独立选择选自C 1-6氢和焦油,或R 10和R 11一起是与碳原子连接形成3至6个碳原子的螺旋的c 2-5焦油基团。 R12,R13和R14可以相同或不同,与H和C1-6焦油分开。 R15是C1-6焦油或苯基;含有一种或多种化合物的药物化合物,用于制造用于治疗,预防和改善与CCR5接收器有关的一种或多种疾病的药物,以及装有单个包装的装置,治疗人类免疫缺陷病毒,包括装在容器中的药物成分,该容器中装有有效量的CCR5拮抗剂,可接受的药物载体和单独的包装,1。一种或多种药物成分,包括有效量的抗病毒药或其他有效制剂,用于用药物可接受的载体治疗人免疫缺陷病毒。

著录项

  • 公开/公告号AR033622A1

    专利类型

  • 公开/公告日2003-12-26

    原文格式PDF

  • 申请/专利权人 SCHERING CORPORATION;

    申请/专利号AR2002P101139

  • 发明设计人

    申请日2002-03-27

  • 分类号C07D211/58;C07D401/04;C07D401/14;C07D401/06;A61K31/506;A61K31/496;A61P31/18;

  • 国家 AR

  • 入库时间 2022-08-21 23:12:32

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