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Quinine Derivatives for Strengthening Transnational Radical Party Activities

机译:加强跨国激进党活动的奎宁衍生物

摘要

For example, compounds used to address potential defects in the processing of transnational Radical Party active cells. 1. Characteristic 1: A compound expressed in formula (1).Or a drug-acceptable, congenital or stale salt, in which A is a bicyclic heteromorphic organism consisting of 8 to 10 members, consisting of 1, 2 or 3 heteromorphic atoms selected from groups O, N and S, in which bicyclic heteromorphic organisms can be optionally replaced. N 1, 2 or 3 select replacement personnel between RA1;X1 was selected from group N and group C (RX1).X2 was selected from group N and group C (X2);X3 was selected from group N and group C (RX3);Comments more than a month agoX2 or X3 can be N; R1 is selected from a group consisting of - NR7491; R74955;C.C832183318326; asphalt, C832183318326; propoxy, C8383318326; phenylcyclopropylene, a single-ring heteromorphic, consisting of 5-6 members, each with one, two, three or four heteromorphic atoms, independently selected from O, N and S groups, plus a single-ring bicycle bridge heteromorphic; The periodic spiral of 4-10 members, each with one or two different atoms, is independently selected from groups O, N and S, in which the single-ring profiles of 5-6 members may be replaced by one or more substitutes. E. In R7497;]In this regard, alternatives between one, two, three or four independently selected R758484 can be chosen to replace single-ring, double-ring bridges and 4-10 spiral heterocyclic bicycles.If this isomer contains a part of NH, it can be selected to use EJOR from C83218C83326EJOR; - C (O) - C83318326; - aspha - C (O) - O - C8321838383226; - aspha - Y-S (O) 695 - C832183318332626Equi (W is 0, 1, 2 or 0);E. In C832183318326, asphalt, alcoxyl and cyclopentadiene, alternatives of one, two or three alternatives selected in R7501 and 7501 can be selected.Between R7510A, one or more substitutes can be used to replace phenyl.R2 can be replaced by one or more substitutes from hydrogen, halogen, cyanide, C83218331836263, tar, C832183313183266, Alcoxico and C832331836263; cyclopentadiene; among them, C83218331836262, C8321833283226, Alcoxilo and C83838383833183326263; 1. Swimming independently between groups consisting of halogen, hydroxyl and phenyl, where one or more substitutes can be selected between R7510 to replace phenyl.R3 unites from hydrogen, halogen, hydroxyl, C83218383263; tar, C83218383838383838326; - Acoxyl, - S (O) 695 - C83318326; - tar (W is 0, 1, or 2),- No. 749191-C83218331832626; asphalt, C8323833183263; cyclohexane, S(O) 695-C83833183266; cyclohexane (W 0, 1, or 2),- NR 74919-C83323-833183226; -cycloquilo, -o-phenyl, -S(O) 695e-phenyl (W 0, 1, or 2),- Nr.74919-Fenilo, C.83288331; 8322; - Benzocyclohexyl-NR7491; R7495;- OC (O) NR74919 - phenyl - NR7491A - C (O) - O - phenyl - NR7491A - C (O) - C (O) - C8321A - C (O) - C83318326; - alkyl - phenyl - C8321833126; - alkyl - NR7491A - phenyl - NR7491A - C833183226; - alkyl - phenyl, as well as a part of single, bicyclic, cyclic, cyclic, cyclic, cyclohexane - 914 - cyclohexane;A. O straight ring - S (O) 695 - (W is 0, 1, or 2), in which one or two heteroatoms are selected from each group consisting of O, N and S; in this group, if the heterocyclic ring - S, the straight ring - NR74919;O Heterosexual - S (o) 695 - Contains part - NH, optionally from C8321838326; - asphalt, - C (o) - C832138326; - C83318326; - asphalt, - C (o) - O - C832183318326; - asphalt, Y - S (o) 695C832183318326; - asphalt, including 2;There, isopropylene, isopropylene-NR749191,E. Isopropylene-S(o) 695 can be replaced by 1, 2, 3 or 4 alternatives selected between R758484 and R758484 respectively.Among them, this ratio of phenyl-O-phenyl-S(O) 695NR 7491; two or three substitutes Independent selection between R75100A;And C832183318326; - S (o) 695C832183326; (W is 0, 1, or 2),- No. 749191-C83218331832626; asphalt, C8323833183263; cyclohexane, S(O) 695-C83833183266; cyclohexane (W 0, 1, or 2),E.Y-NR74919-C8323183268 cyclo can be selected in R7501 and 7501;R8308 should be from hydrogen group and C8321838326; tar group, of which C83217C8331836262; one, two or three alternatives can be selected to replace each alternative, and the alternatives are from halogen group, hydroxyl group and C832183316326; alcoxyl; or R1; R830808,They combine with sulfur and nitrogen to form a selective one-cycle heteromorphic ring, which is replaced by 5-8 members who can choose an additional heteromorphic atom between O, N and S groups; R7497; 7497Se; A is conducted independently in each case between R7510A groups;Hydrogen, C832183318326; asphalt, C832383318326; cyclopentadiene, C832283318326; asphalt, C832283318326; asphalt, C832253318326; asphalt, C832183318326; Acoxyl, C83218326832683; - asphalt, S(o) 695-;(W is 0, 1 or 2)E.C8321C83318326; - N (R74919) - and C8321833126; - Alcoxiccarbonil-N (R7491) -;C.C832183318326; aspha C832383318326; cyclo; C832283318326; Alquenilo; C8322283318326; aspha Acoxyl; C8321838326838326; asphalt-S (O) 695-;C8321C8331836283; - N bitumen (R749191) -,E.C8321C83318326; - n (R749191) - Alternatives selected from R7510 may be substituted by one or more alternatives;R75484, 758484 were independently selected from halogen, hydroxyl, - NR7491, - R74955 groups in each case.Oxo, C832183318326, alkyl group and C832183318326; alcoxyl; R7501 and 7501 were separately selected from halogen, hydroxyl-NR7491; - R749595;C.C832183318326; asphalt, C8321833183326; Acoxyl, C832383318326; cyclo (optional by independent from halogen, hydroxyl, C832183318C83323; asphalt and C832183331) alcoxicol (alternative by one, two or three atoms); (S) FluorinePhenyl is a single-ring heteromorphic, consisting of 5-6 members, or 8-10 members, each with one, two or three heteromorphic atoms, which are independently selected in a group consisting of O, N and S, and have a single-ring, double-ring bridge and 4-10 member helical rings. S chooses one or two heteroatoms in O, N and S groups, and if the heterocyclic ring contains a part of NH, a substitute can be selected in C8321A group to replace this nitrogen. - 1-1-0-0-0-0-0-0-0-0-0-0-0-0-0-0-0-0-0E.Y-S(o) 695-C83218331-832626 asphalt (W 0, 1, or 2);And where can we choose to replace phenyl with one, two or three alternatives selected between R688A and R688A respectively?At this point, one, two, three or four independently selected substitutes can be chosen to replace the single-ring, double-ring bridge and spiral rings of 4-10 members.R688, 6888 independently from halogen, cyanide, C8321833183326283; tar, C832183836263; - alcoxyl, S (o) 695 - C8321833183323; - tar, - S (o) 695 - NR7491; - R74955;- No. 74919-S (O) 695-C832183318333; Asphalt (W 0, 1, or 2),Each member has one, two or three different atoms, which are independently selected from the group composed of O, N and S, and a single ring composed of 4-7 members. Each member has one or two different atoms, and each member chooses independently. Siste en O, N, y S; C832183318326; - alcoxyl and S (o) 695e - C832183318383838323; - alternative tar with one, two or three halogens; R8305; - 8305 is selected independently from halogens, hydroxyl - NR7491; - R74955;OXO, C832121838331 degree-8326, tar and C8321838331 degree-8326, tar and C8321838383838383838326;alcoxicol; Ra1, independently selected from hydrogen, halogen, C83212183838383838383832326 tar, C8322838383838383832326, Alquenilo, C838383838383838383838383838326 asphalt, C832183838383838383838383833226; Alcoxiclo, Alcoxiclo, C832183838383838383838383838383838383838383838383832326;;;;;;;;;;;;;;;;;;;;;; CCCCCCCCCCCCCCCCCC8322222222222222222222222222222222222222222222222222222222222222222222222222222222222222228326;;; "R74955,- O-C(O) -NR7491-phenyl-phenyl-phenyl-phenyl-NR7491-phphphenyl-NR7491-C(O) -phenyl-phenyl, Y-NR7491-C83832183838383838331, S 8324 ribo-phenyl; CC8383832331-8326 tar, CC838383838383838331832326, AlQuenilo, C838383838331833183lalalalalalalalalo, C8383838383318326, Ginilo, C838383838383838391-phphphphphphphphphenyl, Y-NR7491-phenyl, Y-NR7491-C8383838383Replacement of members 4. Halogen, hydroxyl, phenyl and Y-NR7491; R74955;RX1 from hydrogen, halogen, cyanide, C832121; by one, or S or three substitutes selected from hydroxyl and halogen groups; among these substitutes, one or more substitutes selected from R7510 can be used to replace phenyl.Rx2 can replace phenyl with hydrogen, halogen, C83218331836263; tar, C83217C833183263; - alcoxyl, Y-C83216C83318326; - alcox-fenilo; among them, one or more substitutes selected from R7510 can be used.RX3 3 is from hydrogen, halogen, cyanide, C8321; by one, or S or three substitutes selected from hydroxyl and halogen groups; among these substitutes, one or more substitutes selected from R7510 can be used to replace phenyl.R7510 in each case from halogen, hydroxyl, cyanide, C83218331833262; tar, C832383318326; cyclic chlorine, C832183316326; oxygen, phenyl, C8321833183226; cyclic methoxy group, S (o) 695C8321833183838383830; tar, including 230;- S (O) 695-7491; R74955;Y-NR 7491; R74955;E.R749191 and R747595 are independently selected from the hydrogen group, C832183836263; - tar, phenyl, - C(O) - phenyl, Y-C(O) - C832183318326; - tar; C8321838383226; - tar, phenyl, - C(O) - phenyl, Y-C(O) - C83218331832683; - one or more alternatives can be selected; 1. Titles selected from halogen, cyanide, Oxo and hydroxyl groups, or R7491 and R74955, form a heterocycle with the attached nitrogen.
机译:例如,用于解决跨国激进党活性细胞加工中潜在缺陷的化合物。 1.特征1:式(1)表示的化合物或药物可接受的先天或陈旧盐,其中A是由8至10个成员组成的双环异质生物,其由1、2或3个所选的异质原子组成选自O,N和S组,其中双环异型生物可以任选被替换。 N1、2或3个在RA1和X组之间选择的替换人员; X1从N组和C组(RX1)中选择X2从N组和C组(X2)中选择; X3从N组和C组(RX3)中选择;一个多月前的注释X2或X3可以为N; R1选自-NR7491; R74955; C.C832183318326;沥青,C832183318326;丙氧基,C8383318326;苯环丙烯,一种单环异晶,由5-6个成员组成,每个成员具有一个,两个,三个或四个独立地选自O,N和S组的原子,外加一个单环自行车桥异晶;每个有一个或两个不同原子的4-10个成员的周期性螺旋独立地选自O,N和S组,其中5-6个成员的单环轮廓可以被一个或多个取代基取代。 E.在R7497中;]在这方面,可以选择一个,两个,三个或四个独立选择的R758484之间的替代方案来代替单环,双环桥和4-10个螺旋杂环自行车。 NH,可以从C83218C83326EJOR中选择使用EJOR; -C(O)-C83318326; -沥青; -C(O)-O-C8321838383226; -沥青; -Y-S(O)695-C832183318332626Equi(W为0、1、2或0); E。在C832183318326中,可以选择R7501和7501中选择的沥青,烷氧基和环戊二烯的一种,两种或三种替代品。在R7510A之间,可以使用一种或多种替代品替代苯基。氢,卤素,氰化物,C83218331836263,焦油,C832183313183266,Alcoxico和C832331836263;环戊二烯其中,C83218331836262,C8321833283226,Alcoxilo和C83838383833183326263; 1.独立地在由卤素,羟基和苯基组成的基团之间游动,其中可以在R7510之间选择一个或多个取代基来取代苯基。焦油,C83218383838383838326; -乙酰氧基-S(O)695-C83318326; -焦油(W为0、1或2),-编号749191-C83218331832626;沥青,C8323833183263;环己烷,S(O)695-C83833183266;环己烷(W 0、1或2),-NR 74919-C83323-833183226; -环基,-o-苯基,-S(O)695e-苯基(W 0、1或2),-Nr.74919-Fenilo,C.83288331; 8322; -苯并环己基-NR7491; R7495;-OC(O)NR74919-苯基-NR7491A-C(O)-O-苯基-NR7491A-C(O)-C(O)-C8321A-C(O)-C83318326; -烷基-苯基-C8321833126; -烷基-NR7491A-苯基-NR7491A-C833183226; -烷基-苯基以及单,双环,环状,环状,环状,环己烷的一部分-914-环己烷; A. O直环-S(O)695-(W为0、1或2),其中一个或两个杂原子选自O,N和S;在这一组中,如果杂环-S,则直环-NR74919; O异性-S(o)695-包含-NH部分,可选地选自C8321838326; -沥青,-C(o)-C832138326; -C83318326; -沥青,-C(o)-O-C832183318326; -沥青,Y-S(o)695C832183318326; -沥青,包括2;那里是异丙烯,异丙烯-NR749191,E。异丙烯-S(o)695可以用分别在R758484和R758484之间选择的1、2、3或4个替代品代替。其中,该比例的苯基-O-苯基-S(O)695NR 7491;两个或三个替代品在R75100A和C832183318326之间独立选择; -S(o)695C832183326; (W为0、1或2),-编号749191-C83218331832626;沥青,C8323833183263;环己烷,S(O)695-C83833183266; R7501和7501中可以选择环己烷(W 0、1或2),E.Y-NR74919-C8323183268环; R8308应选自氢基团和C8321838326; tar组,其中C83217C8331836262;可以选择一个,两个或三个替代物替代每个替代物,并且所述替代物选自卤素基团,羟基和C832183316326;烷氧基或R1; R830808,它们与硫和氮结合形成一个选择性的单环杂环,被5-8个成员取代,这些成员可以在O,N和S基团之间选择一个额外的同构原子; R7497; 7497Se;在R7510A组之间分别独立进行A; Hydrogen,C832183318326;沥青,C832383318326;环戊二烯,C832283318326;沥青,C832283318326;沥青,C832253318326;沥青,C832183318326;乙酰氧基,C83218326832683; -沥青,S(o)695-;(W为0,1或2)E.C8321C83318326; -N(R74919)-和C8321833126; -Alcoxiccarbonil-N(R7491)-; C.C832183318326;沥青; C832383318326;环C832283318326;阿尔奎尼洛; C8322283318326;沥青;乙氧基; C8321838326838326;沥青-S(O)695-; C8321C8331836283; -N沥青(R749191)-,E.C8321C83318326; -n(R749191)-选自R7510的替代物可以被一个或多个替代物取代; R75484、758484分别独立地选自卤素,羟基,-NR7491,-R74955基团。Oxo,C832183318326,烷基和C832183318326;烷氧基R7501和7501分别选自卤素,羟基-NR7491;和-R749595; C.C832183318326;沥青,C8321833183326;乙酰氧基,C832383318326;环烷醇(可选地,独立于卤素,羟基,C832183318C83323;沥青和C832183331);环烷醇(一个,两个或三个原子替代); (S)氟苯基是单环杂晶,由5-6个成员或8-10个成员组成,每个成员具有一个,两个或三个杂种原子,这些原子独立地选自O,N和S,并且有一个单环,双环桥和4-10个成员的螺旋环。 S在O,N和S基团中选择一个或两个杂原子,并且如果杂环包含一部分NH,则可以在C8321A基团中选择一个取代基来取代该氮。 -1-1-0-0-0-0-0-0-0-0-0-0-0-0-0-0-0-0-0E.YS(o)695-C83218331-832626沥青( W 0、1或2);在哪里可以选择分别用R688A和R688A之间选择的一个,两个或三个取代基取代苯基?此时,可以选择一个,两个,三个或四个独立选择的取代基来取代R688、6888独立于卤素,氰化物,C8321833183326283的4-10个成员的单环,双环桥和螺旋环;焦油,C832183836263; -烷氧基,S(o)695-C8321833183323; -焦油-S(o)695-NR7491; -R74955;-No.74919-S(O)695-C832183318333;沥青(W 0、1或2),每个成员具有一个,两个或三个不同的原子,它们独立地选自O,N和S,以及一个由4-7个成员组成的单环。每个成员具有一个或两个不同的原子,并且每个成员独立选择。 Siste en O,N,y S; C832183318326; -烷氧基和S(o)695e-C832183318383838323; -具有一,二或三个卤素的替代焦油; R8305; -8305独立地选自卤素,羟基-NR7491; -R74955; OXO,C832121838331度为8326,焦油和C8321838331度为8326,焦油和C8321838383838383838326; alcoxicol; Ra1,独立地选自氢,卤素,C83212183838383838383832326焦油,C8322838383838383832326,Alquenilo,C838383838383838383838383838326沥青,C832183838383838383838383833226; Alcoxiclo,Alcoxiclo,C832183838383838383838383838383838383838383838383832832 ;;;;;;;;;;;;; CCCCCCCCCCCCCCCCCCCC8322222222222222222222222222222222222222222222222222222222222222222222222222222222222228326 ;;; “ R74955,-OC(O)-NR7491-苯基-苯基-苯基-苯基-NR7491-phphphenyl-NR7491-C(O)-苯基-苯基,Y-NR7491-C83832183838383838331,S 8324核糖苯基; CC8383832331-8326焦油,CC838383838383838331832326,AlQuenilo,C838383838331833183Lalalalalalalalalallo,C8383838383318326,Ginilo,C838383838383838391-phphphphphphphphphenyl,Y-NR7491-苯基,Y-NR7491-C8383838383取代成员4。 Rx2可以用氢,卤素,C83218331836263;焦油,C83217C833183263;或R,或R或R;或R;或R;或R;或R;或R;或R;或R;或R。 RX3 3选自氢,卤素,氰化物,C8321;一个或多个S,或三个选自羟基的取代基; -Alcox,Y-C83216C83318326; -alcox-fenilo;其中,可以使用选自R7510的一种或多种取代基。卤素基团;在这些取代基中分子,选自R7510的一种或多种取代基可用于取代苯基。R7510在每种情况下均选自卤素,羟基,氰化物,C83218331833262;焦油,C832383318326;环氯,C832183316326;氧,苯基,C8321833183226;环甲氧基,S(o)695C8321833183838383830;焦油,包括230;-S(O)695-7491; R74955; Y-NR 7491; R74955; E.R749191和R747595独立地选自氢基团,C832183836263;和-焦油,苯基,-C(O)-苯基,Y-C(O)-C832183318326; - 柏油; C8321838383226; -焦油,苯基,-C(O)-苯基,Y-C(O)-C83218331832683; -可以选择一个或多个备选方案; 1.选自卤素,氰化物,氧代和羟基或R7491和R74955的标题与所连接的氮形成杂环。

著录项

  • 公开/公告号AR111496A1

    专利类型

  • 公开/公告日2019-07-17

    原文格式PDF

  • 申请/专利权人 PROTEOSTASIS THERAPEUTICS INC.;

    申请/专利号AR2018P101104

  • 发明设计人 PARKS DANIEL;MUNOZ BENITO;

    申请日2018-04-27

  • 分类号C07D405/04;A61K31/4709;A61P11;A61P25/28;C07D405/14;C07D409/04;C07D409/14;C07D417/14;

  • 国家 AR

  • 入库时间 2022-08-21 12:03:56

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