首页> 外国专利> Derivatives of 6 - (6-o - triazolopiridazina - sulfanyl) benzotiazoles and benzimidazoles, method of preparing the same and intermediaries that Synthesis, medicines containing them and Use thereof in the treatment of cancer, arthritis, allergies, and other diseases.

Derivatives of 6 - (6-o - triazolopiridazina - sulfanyl) benzotiazoles and benzimidazoles, method of preparing the same and intermediaries that Synthesis, medicines containing them and Use thereof in the treatment of cancer, arthritis, allergies, and other diseases.

机译:6-(6-o-三唑并吡嗪并-硫烷基)苯并噻唑和苯并咪唑的衍生物,其合成方法和中间体,含有它们的药物及其在治疗癌症,关节炎,过敏和其他疾病中的用途。

摘要

1. Industrial property 1: Formula product (1), wherein - --- represents a simple or double bond; Rb represents a hydrogen atom or a fluorination atom; RA stands for a radical o-z-rc, Z stands for a simple link or linear tar or branch radical, consisting of 1 to 6 carbon atoms, which can be optionally replaced by a group of tar or a halogenated atom; RC stands for a cyclic electrolysis, heterocyclic electrolysis, arilo or alternative isomerization electrolysis; X represents s, so or SO2; a represents NH or s; W represents hydrogen atom; optional tar or cyclopentadiene atom is replaced by alcox, isocyclopentadiene or n3r4;Or a radical COR, in which R represents a cyclopentyl radical, or a radical tar, can choose to replace with a radical nr3r4, alcoxi, o-cycloquilo, o-co-r5, hydroxi, fenilo, isopropyl, or isopropyl propyl, which they choose; an optional alcoxi radical replaces nr3r4, alcoxi, Hydrogen or isocyclopentyl; an n-propyl or n-propyl radical or an n-propyl or n-propyl (CH2) radical with an optional phenyl substitute and N representing an integer of 1 to 4; or an nr1r2 radical with R1 and R2 representing a hydrogen atom, A cyclopentyl radical or a radical tar, and R1 and R2 represent a hydrogen atomA cyclopentyl radical or an optional tar, selected by one or more same or different radicals from hydroxyl, propoxy, isomer, isomerization, isomerization, isomerization, isomerization, nr3r4, alternative phenyl; or R1 and R2 form a cyclic radical with the attached nitrogen, with a strength of 3 to 3. The 10 bonds and the optional one or more different heteroatoms selected from O, s, N and NH may be the optional so or SO2 form; this radical, including its optional NH, is replaced; R3 and R4, the same or different, represent a hydrogen atom, a radical tar,1. Cyclopentyl, non cyclopentyl, heteromorphic or phenyl radicals are all replaced by one or more same or different radicals, which are selected from hydroxy, propyl, heteromorphic, isocyclopenyl, NH2, nhalk, n (ALK) 2, optional phenyl substitutes; Or R3 and R4 form a cyclic excimer with the nitrobenzene atom they are connected to, which is composed of 3 to 10 links, optionally composed of one or more different atoms selected from the O, s, N and NH, and may be in the form of so or SO2; and such excimer, including the optional NH contained therein, Alternative replacement;Tar, alcoxi-o-cycloquilo, cycloquilo, isomerization, isomerization, arilo and phenyl, and periodic radicals containing all of the above definitions, which can form R1 and R2, or R3 and R4, are linked to nitrobenzene atoms and can optionally be replaced by one or more radicals selected from the protons. Halogen, hydroxy, oxo, alcoxi, o-co-r5, or5-cooh, coor5, CONH2, conhr5, NH2, nhr5 ',-Nh-co-r5-nhcoor5 and alchemy, isopropyl Agave, cyclopentyl glycol, isopropyl isopropyl isopropyl ester, ch2-isopropyl, phenyl, phenylisopropyl, isopropyl and isopropyl allylidene, among these last radicals, represents an option. Alchemy radicals, allyl radicals, isopropyl radicals, isopropyl radicals, phenyl radicals, isopropyl radicals and isopropyl radicals all have their own choices It is replaced by one or more radicals selected from hydroxyl, oxo, tar and Alcoy radicals, NH2, nhalk and n (ALK) 2 of halogenated atoms and 1-4 carbon atoms; in addition, there are all the radicals defined above, namely cyclopentyl, isocyclopenyl, isobutylene and phenyl,Option 3; R5 and R5 ',The same or different tar or cyclopentyl radicals representing no more than six carbon atoms; ALK radical tar representing no more than four carbon atoms; it is understood that: (1) if RB represents a simple connection, then RC does not represent a cyclopentyl radical; (2) if RB represents a simple connection, then RC does not represent a cyclopentyl radical Hydrogen and Z represent a tar radical, so RC does not represent isomerization cyclopropyl radical, and these formula products (1) exist in various possible isomers, racemization, dwarfism and isomerization forms,And addictive salts (1) containing minerals and organic acids or minerals and organic bases of these formula products.
机译:1.工业性质1:配方产品(1),其中---代表单键或双键; Rb代表氢原子或氟化原子; RA代表基团o-z-rc,Z代表一个简单的连接或线性tar或支链基团,由1至6个碳原子组成,可以任选地被一组tar或卤代原子取代; RC代表循环电解,杂环电解,芳基或替代异构化电解; X代表s,所以代表SO2; a代表NH或s; W代表氢原子;可选的tar或环戊二烯原子被Alcox,异环戊二烯或n3r4取代;或COR基团(其中R代表环戊基基团)或基团tar可以选择被nr3r4基团取代,醇盐,邻环基,o-co他们选择的-r5,hydroxi,fenilo,异丙基或异丙​​基丙基;任选的醇氧基取代nr3r4,醇,氢或异环戊基; n-丙基或n-丙基或n-丙基或n-丙基(CH2)基团,其具有任选的苯基取代基,并且N表示1-4的整数;或nr1r2基团,其中R1和R2代表氢原子,环戊基或基团tar,而R1和R2代表氢原子环戊基或任选的tar,由一个或多个相同或不同的基团选自羟基,丙氧基,异构体,异构化,异构化,异构化,异构化,nr3r4,替代苯基; R 1和R 2与连接的氮形成环状自由基,强度为3至3。10个键和选自O,s,N和NH的任选的一个或多个不同的杂原子可以为任选的so或SO 2形式;或取代了该自由基,包括其可选的NH; R 3和R 4相同或不同,代表氢原子,自由基焦油,1。环戊基,非环戊基,杂晶或苯基均被一个或多个相同或不同的基团取代,所述基团选自羟基,丙基,杂晶,异环戊基,NH 2,nhalk,n(ALK)2,任选的苯基取代基;或R 3和R 4与它们连接的硝基苯原子形成环状准分子,其由3至10个链组成,任选地由一个或多个选自O,s,N和NH的不同原子组成,并且可以在二氧化硫或二氧化硫的形式;以及该准分子,包括其中包含的任选的NH,替代替换; Tar,alcoxi-o-cycloquilo,cycloquilo,异构化,异构化,arilo和苯基,以及含有所有上述定义的可形成R1和R2的周期基,或R 3和R 4连接至硝基苯原子,并且可以任选地被一个或多个选自质子的基团取代。卤素,羟基,羰基,羟基,邻-co-r5或or5-cooh,coor5,CONH2,conhr5,NH2,nhr5',-Nh-co-r5-nhcoor5和炼金术,异丙基龙舌兰,环戊二醇,异丙基异丙基异丙酯在这些最后的基团中,ch 2-异丙基,苯基,苯基异丙基,异丙基和异丙基亚烷基代表一种选择。炼金术基团,烯丙基基团,异丙基基团,异丙基基团,苯基基团,异丙基基团和异丙基基团都有自己的选择。它被一个或多个选自羟基,氧代,焦油和醇基的基团取代,这些基团包括NH2,nhalk和n( ALK)2个卤原子和1-4个碳原子;另外,存在以上定义的所有基团,即环戊基,异环戊基,异丁烯和苯基,选项3; R5和R5',代表不超过六个碳原子的相同或不同的焦油或环戊基;代表不超过四个碳原子的ALK自由基焦油;可以理解:(1)如果RB表示简单连接,则RC不表示环戊基; (2)如果RB代表简单连接,则RC不代表环戊基氢和Z代表焦油基,因此RC不代表环丙基的异构化,这些分子式(1)存在各种可能的异构体,消旋化,矮化和异构化形式,以及含有矿物质和有机酸或这些配方产品的矿物质和有机碱的成瘾盐(1)。

著录项

  • 公开/公告号AR075249A1

    专利类型

  • 公开/公告日2011-03-16

    原文格式PDF

  • 申请/专利权人 SANOFI-AVENTIS;

    申请/专利号AR2010P100317

  • 申请日2010-02-05

  • 分类号C07D487/04;C07D277/82;A61K31/5025;A61K31/4196;A61K31/428;A61P35/00;A61P3/10;A61P37/00;A61P19/02;A61P17/06;A61P11/06;

  • 国家 AR

  • 入库时间 2022-08-21 18:07:28

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