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Diaryl 1,2,4 - Oxadiazoles Compounds, Pharmaceutical compositions containing Same, Preparation Process and use as immunosuppressive agents in the treatment of autoimmune diseases and / or chronic inflammatory.

机译:二芳基1,2,4-恶二唑化合物,含有该化合物的药物组合物,制备方法以及在自身免疫性疾病和/或慢性炎症中的免疫抑制剂用途。

摘要

For example, compounds are useful in the treatment of autoimmune disorders such as multiple sclerosis and other diseases. ILO Convention No. 1: from oxadiazol de formula (1), where R1, R2 refers to h, Hal, CF3, ocf3, CN, ONO2, oh, a, OA; s refers to cor3, so2n2, con (R3) 2, O Z; Q refers to X (CH2) m, (CH2) MX (CH2) m, O UN connection unique; X es-o -,- third...-Coo-o-conr3--2 2 2 2 2 2 2 2 (nnnnnnnnnnnn2 (R3) 2, or "CF3" or "R3" if R1 or R2 is "Hal"; a is a beam splitting or linear tar, and It has 1 to 12 carbon atoms, one or more of which can be replaced by Hal, or3, cour3, CN, n (R3) 2 or het, and one or more non adjacent CH2 groups can be replaced by O, NR3, Co or s and / or CH = ch-o-csc or cyclopentanediol group with 3 to 7 carbon atoms,O refers to cyclopentadienyl or cyclopentadienyl propenyl or cyclopentadienyl propenyl with 3-7 carbon atoms; Z is a discrete or linear tar chain with 1-12 carbon atoms, one or more of which are composed of or3, Coordination3, have (R3), 2, CN, so2a, n (R3) 2 or het and / or one or more CH2 non adjacent groups are - O -,- cool...- third...-NBC...-O-S---SO2- and / or by groups -CH = CH- or -CsC- or cycloalkylene groups having 3 to 7 carbon atoms, or denotes cycloalkyl or cycloalkylalkylene having 3-7 ring C atoms; Hal is F, Cl, Br or I; Ar denotes a monocyclic or bicyclic, saturated, unsaturated or aromatic carbocyclic ring having 6 to 14 carbon atoms, which may be monosubstituted, disubstituted or trisubstituted by Hal, A, OR3, N (R3) 2, NO2, CN, COOR3, CF3, OCF3, CON (R3) 2, NR3COA, NR3CON (R3) 2, NR3SO2A, COR3, SO2N (R3) 2, SOA or SO2A, phenyl, pyridyl- [C (R3) 2] n-COOR3 and / or - O [C (R3) 2] n-CON (R3) 2,Therefore, at least one atom is adjacent to the atom connecting the group with the rest of the molecules, and there is one such substitute; het represents a single or double ring, saturated or heterocyclic aromatic ring, containing 1 to 4 N atoms, or Y / or S atoms, which can be independently replaced, desulfurized or Tristan by Hal (a). -The atoms of the atomic group are combined with the atoms, the atoms, the atoms, the atoms, the atoms, the atoms of the atomic group are combined with the atoms, the atoms are combined with other molecules with one of the substitutes; R3 is h or a;Two sets of R3 gemstones can be added together to form a ring with atoms; n is 0, 1, 2, 3, 4, 5, 6, 7 or 8; m is 1, 2, 3, 4, 5, 6, 7 or 8; and their derivatives, solutions, ceramics, salts and stereoisomers with acceptable efficacy, including mixtures in all their relationships.
机译:例如,化合物可用于治疗自身免疫疾病,例如多发性硬化症和其他疾病。国际劳工组织第1号公约:式(1)中的恶二唑,其中R1,R2表示h,Hal,CF3,ocf3,CN,ONO2,oh,a,OA; s表示cor3,so2n2,con(R3)2,O Z; Q是指X(CH2)m,(CH2)MX(CH2)m,O UN连接唯一; X es-o-,-第三...- Coo-o-conr3--2 2 2 2 2 2 2 2(nnnnnnnnnnnn2(R3)2,如果R1或R2为“ Hal”,则为“ CF3”或“ R3” ; a是分束或线性焦油,它具有1至12个碳原子,其中一个或多个可以被Hal,or3,cour3,CN,n(R3)2或het取代,并且一个或多个不相邻CH 2基团可以被O,NR 3,Co或s取代和/或CH =具有3至7个碳原子的ch-o-csc或环戊二醇基,O是指具有3至7个碳原子的环戊二烯基或环戊二烯基丙烯基或环戊二烯基丙烯基; Z是具有1-12个碳原子的离散或线性tar链,其中一个或多个由or3,配位3,具有(R3),2,CN,so2a,n(R3)2或het和/或一个或一个或多个构成更多的CH2非相邻基团是-O-,-冷却...-第三...- NBC ...- OS--SO2-和/或基团-CH = CH-或-CsC-或具有3到7个碳原子,或表示具有3-7个环C原子的环烷基或环烷基亚烷基; Hal为F,Cl,Br或I; Ar表示单环或双环,饱和,具有6至14个碳原子的饱和或芳族碳环,可以被Hal,A,OR3,N(R3)2,NO2,CN,COOR3,CF3,OCF3,CON(R3)2,NR3COA单取代,二取代或三取代,NR3CON(R3)2,NR3SO2A,COR3,SO2N(R3)2,SOA或SO2A,苯基,吡啶基-[C(R3)2] n-COOR3和/或-O [C(R3)2] n-CON (R3)2,因此,至少一个原子与连接该基团和其余分子的原子相邻,并且存在一个这样的取代基; het表示单环或双环,饱和或杂环芳族环,含有1-4个N原子或Y /或S原子,可被Hal(a)独立取代,脱硫或Tristan。 -原子团的原子与原子结合,原子团的原子,原子,原子,原子,原子,原子与原子结合,原子与具有取代基之一的其他分子结合; R3是h或a;可以将两组R3宝石加在一起以与原子形成环; n为0、1、2、3、4、5、6、7或8; m为1、2、3、4、5、6、7或8;及其衍生物,溶液,陶瓷,盐和立体异构体,具有可接受的功效,包括所有关系的混合物。

著录项

  • 公开/公告号AR068731A1

    专利类型

  • 公开/公告日2009-12-02

    原文格式PDF

  • 申请/专利权人 LABORATOIRES SERONO S.A.;

    申请/专利号AR2008P104333

  • 发明设计人

    申请日2008-10-03

  • 分类号C07D271/06;C07D413/04;C07D413/10;A61K31/4245;A61P37/06;A61P19/02;A61P3/10;A61P1/04;A61P1/16;A61P1/18;A61P13/12;A61P27/02;A61P11/06;A61P25/28;A61P31/04;A61P31/18;A61P35/00;

  • 国家 AR

  • 入库时间 2022-08-21 18:47:32

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