2-甲基-2-丙基4-(3-氯苄基)-1-哌嗪羧酸酯 | 305860-09-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 中文名称: 2-甲基-2-丙基4-(3-氯苄基)-1-哌嗪羧酸酯
• 英文名称: 4-(3-chlorobenzyl)-piperazine-1-carboxylic acid tert-butyl ester
• 英文别名: Tert-butyl 4-[(3-chlorophenyl)methyl]piperazine-1-carboxylate
• CAS: 305860-09-7
• 化学式: C₁₆H₂₃ClN₂O₂
• mdl: MFCD01924370
• 分子量: 310.824
• InChiKey: RBHSRNNKRAPSFN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.562
• 拓扑面积：
  32.8
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 海关编码：
  2933599090

反应信息

• 作为反应物：
  描述：

  2-甲基-2-丙基4-(3-氯苄基)-1-哌嗪羧酸酯 在 三氟乙酸 作用下， 以 甲苯 为溶剂， 反应 1.33h， 生成 1-(3-氯苄基)哌嗪
  参考文献：
  名称：

  Synthesis and receptor binding studies of novel 4,4-disubstituted arylalkyl/arylalkylsulfonyl piperazine and piperidine-based derivatives as a new class of σ1 ligands

  摘要：

  This study presents the synthesis and biological evaluation of a new series of arylalkyliary/alkylsulfonyl piperazine and piperidine-based derivatives as sigma receptor ligands. It was found that a number of halogen substituted sulfonamides display relatively high and low affinities to sigma(1) and sigma(2) receptors, respectively. The sigma(1) affinities and subtype selectivities of four piperidine derivatives were also found to be generally comparable to those of piperazine analogues. Compared to sigma(1)-Rs compounds with n = 0 and 2, those with n = 1 proved to have optimal length of carbon chain by exhibiting higher affinities.Within this series, the 4-benzyl-1-(3-iodobenzylsulfonyl)piperidine sigma ligand was identified with 96-fold sigma(1)/sigma(2) selectivity ratio (K-i sigma(i) = 0.96 +/- 0.05 nM and K-i sigma(2) = 91.8 +/- 8.1 nM). (C) 2013 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2013.04.013
• 作为产物：
  描述：

  N-Boc-哌嗪 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 2-甲基-2-丙基4-(3-氯苄基)-1-哌嗪羧酸酯
  参考文献：
  名称：

  Synthesis and receptor binding studies of novel 4,4-disubstituted arylalkyl/arylalkylsulfonyl piperazine and piperidine-based derivatives as a new class of σ1 ligands

  摘要：

  This study presents the synthesis and biological evaluation of a new series of arylalkyliary/alkylsulfonyl piperazine and piperidine-based derivatives as sigma receptor ligands. It was found that a number of halogen substituted sulfonamides display relatively high and low affinities to sigma(1) and sigma(2) receptors, respectively. The sigma(1) affinities and subtype selectivities of four piperidine derivatives were also found to be generally comparable to those of piperazine analogues. Compared to sigma(1)-Rs compounds with n = 0 and 2, those with n = 1 proved to have optimal length of carbon chain by exhibiting higher affinities.Within this series, the 4-benzyl-1-(3-iodobenzylsulfonyl)piperidine sigma ligand was identified with 96-fold sigma(1)/sigma(2) selectivity ratio (K-i sigma(i) = 0.96 +/- 0.05 nM and K-i sigma(2) = 91.8 +/- 8.1 nM). (C) 2013 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2013.04.013

文献信息

• Pyrrolopyrimidine A2b selective antagonist compounds, their synthesis and use
  申请人：——

  公开号：US20030229067A1

  公开（公告）日：2003-12-11

  The subject invention provides compounds having the structure: 1 wherein, R 1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NR a R b , —NR a R b , —NR a C(═O)NR a R b , —NR a C(═O)OR a , —OC(═O)NR a R b , or —NHC(═O)R a ; R 2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NR a R b , —NR a R b , —NR a C(═O)NR a R b , —NR a C(═O)OR a , —OC(═O)NR a R b , or —NHC(═O)R a , or R 1 , R 2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH 2 ) 2 OH or —CH 2 C(═O)OH; R 3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C 1 -C 15 )alkyl, (C 1 -C 15 )alkoxy, or —NR a R b ; R 4 is hydrogen or substituted or unsubstituted (C 1 -C 15 )alkyl; R 5 is —(CH 2 ) m OR 6 , —CHNOR 7 , —C(═O)NR 8 R 9 , —(CH 2 ) m C(═O)OR 10 , —(CH 2 ) k C(═O)NR 11 R 12 ; wherein R 6 is a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R 7 is hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl; R 8 and R 9 are each independently hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl, (C 1 -C 30 )alkylamino, (C 1 -C 30 )alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R 8 , N, and R 9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R 10 is hydrogen or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R 11 , N and R 12 together form a 4-8 membered heterocyclic ring; R a and R b are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3, or a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A 2b adenosine receptor in a subject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.

  该主题发明提供具有以下结构的化合物： 1 其中， R 1 是取代或未取代的烷基，其中取代基是羟基、二羟基、羧基、—C(═O)NR a R b 、—NR a R b 、—NR a C(═O)NR a R b 、—NR a C(═O)OR a 、—OC(═O)NR a R b 或—NHC(═O)R a ； R 2 是氢或取代或未取代的烷基，其中取代基是羟基、二羟基、羧基、—C(═O)NR a R b 、—NR a R b 、—NR a C(═O)NR a R b 、—NR a C(═O)OR a 、—OC(═O)NR a R b 或—NHC(═O)R a ，或 R 1 、R 2 和N共同形成取代哌嗪、取代氮杂环丙烷环或取代的—(CH 2 ) 2 OH或—CH 2 C(═O)OH的吡咯烷环； R 3 是取代或未取代的苯基或5-6成员杂芳环，其中取代基是卤素、羟基、氰基、(C 1 -C 15 )烷基、(C 1 -C 15 )烷氧基或—NR a R b ； R 4 是氢或取代或未取代的(C 1 -C 15 )烷基； R 5 是—(CH 2 ) m OR 6 、—CHNOR 7 、—C(═O)NR 8 R 9 、—(CH 2 ) m C(═O)OR 10 、—(CH 2) k C(═O)NR 11 R 12 ； 其中R 6 是取代或未取代的(C 1 -C 30 )烷基、(C 3 -C 10 )环烷基或芳基、杂芳基或4-8成员杂环环； R 7 是氢或取代或未取代的(C 1 -C 30 )烷基、(C 1 -C 30 )烷基芳基； R 8 和R 9 各自独立地是氢或取代或未取代的(C 1 -C 30 )烷基、(C 1 -C 30 )烷基芳基、(C 1 -C 30 )烷基氨基、(C 1 -C 30 )烷氧基或饱和或不饱和的、单环或双环的、碳环或杂环环，或 R 8 、N和R 9 共同形成取代或未取代的4-8成员杂环环； R 10 是氢或取代或未取代的(C 1 -C 30 )烷基、(C 3 -C 10 )环烷基或芳基、杂芳基或杂环环； R 11 、N和R 12 共同形成4-8成员杂环环； R a 和R b 各自独立地是氢或烷基； m为0、1、2或3；和 k为1、2或3， 或其特定对映体，或其特定互变异构体，或其药学上可接受的盐，以及一种治疗与需要此类治疗的受试者相关的A 2b 腺苷受体相关疾病的方法，包括向受试者施用该发明化合物的治疗有效量。
• Pyrimidine A2b selective antagonist compounds, their synthesis and use
  申请人：——

  公开号：US20030162764A1

  公开（公告）日：2003-08-28

  The subject invention provides compounds having the structure: 1 wherein R 1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R 2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R 3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R 2 and R 3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R 3 is oxygen; R 4 and R 5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R 4 NR 5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; R 12 is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A 2b adenosine receptor by administering a therapeutically effective amount of the compounds of the invention.

  本发明提供具有以下结构的化合物： 1 其中R 1 是取代或未取代的苯基或含1至5个杂原子的5-6元杂环或杂芳环；R 2 是氢，或取代或未取代的烷基，—C(O)-烷基，—C(O)—O-烷基，烷氧基，环烷基，烯丙基，单环或双环芳基，杂芳基或杂环部分；R 3 是氢，或取代或未取代的烷基，—C(O)-烷基，—C(O)—O-烷基，烷氧基，环烷基，烯丙基，单环或双环芳基，杂芳基或杂环部分，或者R 2 和R 3 连接形成一个杂环；其中虚线代表可能存在或不存在第二键，当存在时R 3 是氧；R 4 和R 5 各自独立地是取代或未取代的烷基，—C(O)-烷基，—C(O)—O-烷基，烷氧基，环烷基，烯丙基，单环或双环芳基，杂芳基或杂环部分，或者R 4 和R 5 共同形成一个含1至6个杂原子的取代或未取代的单环或双环杂环或杂芳基部分；R 12 是氢，烷基，卤素或腈；且n是0，1，2，3或4，或其对应的手性体，或特定的互变异构体，或其药物可接受的盐，以及通过给药治疗与A 2b 腺苷受体相关疾病的方法。
• Pyrimidine A2B selective antagonist compounds, their synthesis and use
  申请人：Castelhano Arlindo

  公开号：US20050119271A1

  公开（公告）日：2005-06-02

  The subject invention provides compounds having the structure: wherein R 1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R 2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R 3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R 2 and R 3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R 3 is oxygen; R 4 and R 5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R 4 NR 5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; R 12 is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A 2b adenosine receptor by administering a therapeutically effective amount of the compounds of the invention.

  本发明提供具有以下结构的化合物： 其中，R1是取代或未取代的苯基或含有1至5个杂原子的5-6元杂环或杂芳基环；R2是氢，或取代或未取代的烷基，-C(O)-烷基，-C(O)-O-烷基，烷氧基，环烷基，烯基，单环或双环芳基，杂芳基或杂环基；R3是氢，或取代或未取代的烷基，-C(O)-烷基，-C(O)-O-烷基，烷氧基，环烷基，烯基，单环或双环芳基，杂芳基或杂环基；或R2和R3结合形成杂环环；其中虚线表示第二键可能存在或不存在，当存在时，R3是氧；R4和R5分别是取代或未取代的烷基，-C(O)-烷基，-C(O)-O-烷基，烷氧基，环烷基，烯基，单环或双环芳基，杂芳基或杂环基；或R4NR5一起形成含有1至6个杂原子的取代或未取代的单环或双环，杂环或杂芳基；R12是氢，烷基，卤素或氰基；n为0、1、2、3或4，或其对映异构体，或其特定互变异构体，或其药学上可接受的盐，并提供了一种通过给予本发明化合物的治疗有效量来治疗与A2b腺苷受体相关的疾病的方法。
• PYRROLOPYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE
  申请人：Castelhano Arlindo

  公开号：US20080261943A1

  公开（公告）日：2008-10-23

  The subject invention provides compounds having the structure: wherein, R 1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NR a R b , —NR a R b , —NR a C(═O)NR a R b , —NR a C(═O)OR a , —OC(═O)NR a R b , or —NH C(═O) R a ; R 2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NR a R b , —NR a R b , —NR a C(═O)NR a R b , —NR a C(═O)OR a , —OC(═O)NR a R b , or —NHC(═O)R a , or R 1 , R 2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH 2 ) 2 OH or —CH 2 C(═O)OH; R 3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C 1 -C 15 )alkyl, (C 1 -C 15 )alkoxy, or —NR a R b ; R 4 is hydrogen or substituted or unsubstituted (C 1 -C 15 )alkyl; R 5 is —(CH 2 ) m OR 6 , —CHNOR 7 , —C(═O)NR 8 R 9 , —(CH 2 ) m C(═O)OR 10 , —(CH 2 ) k C(═O)NR 11 R 12 ; wherein R 6 is a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R 7 is hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl; R 8 and R 9 are each independently hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl, (C 1 -C 30 )alkylamino, (C 1 -C 30 )alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R 8 , N, and R 9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R 10 is hydrogen or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R 11 , N and R 12 together form a 4-8 membered heterocyclic ring; R a and R b are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3, or a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A 2b adenosine receptor in a subject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.

  本发明提供了具有以下结构的化合物：其中，R1是取代或未取代的烷基，其中取代基是羟基，二羟基，羧基，—C（═O）NRaRb，—NRaRb，—NRaC（═O）NRaRb，—NRaC（═O）ORa，—OC（═O）NRaRb或—NH C（═O） Ra；R2是氢或取代或未取代的烷基，其中取代基是羟基，二羟基，羧基，—C（═O）NRaRb，—NRaRb，—NRaC（═O）NRaRb，—NRaC（═O）ORa，—OC（═O）NRaRb或—NHC（═O）Ra，或R1，R2和N共同形成取代的哌嗪，取代的氮杂环丙烷环或取代的吡咯烷环，取代基为—（CH2）2OH或—CH2C（═O）OH；R3是取代或未取代的苯基或5-6成员的杂芳基环，其中取代基为卤素，羟基，氰基，（C1-C15）烷基，（C1-C15）烷氧基或—NRaRb；R4是氢或取代或未取代的（C1-C15）烷基；R5是—（CH2）mOR6，—CHNOR7，—C（═O）NR8R9，—（CH2）mC（═O）OR10，—（CH2）kC（═O）NR11R12；其中，R6是取代或未取代的（C1-C30）烷基，（C3-C10）环烷基或芳基，杂芳基或4-8成员的杂环；R7是氢或取代或未取代的（C1-C30）烷基，（C1-C30）烷基芳基；R8和R9各自独立地是氢或取代或未取代的（C1-C30）烷基，（C1-C30）烷基芳基，（C1-C30）烷基氨基，（C1-C30）烷氧基或饱和或不饱和的单环或双环，碳环或杂环，或R8，N和R9共同形成取代或未取代的4-8成员的杂环；R10是氢或取代或未取代的（C1-C30）烷基，（C3-C10）环烷基，芳基，杂芳基或杂环；R11，N和R12共同形成4-8成员的杂环；Ra和Rb各自独立地是氢或烷基；m为0，1，2或3；k为1，2或3，或其特定对映体，或其特定互变异构体，或其药学上可接受的盐，以及一种用于治疗与A2b腺苷受体相关的疾病的方法，包括向需要这种治疗的受体中施用本发明化合物的治疗有效量。
• Pyrrolopyrimidine A2B selective antagonist compounds, their synthesis and use
  申请人：OSI Pharmaceuticals, Inc.

  公开号：US07645754B2

  公开（公告）日：2010-01-12

  The subject invention provides compounds having the structure: wherein, R1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NHC(═O) Ra; R2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NHC(═O)Ra, or R1, R2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH2)2OH or —CH2C(═O)OH; R3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C1-C15)alkyl, (C1-C15)alkoxy, or —NRaRb; R4 is hydrogen or substituted or unsubstituted (C1-C15)alkyl; R5 is —(CH2)mOR6, —CHNOR7, —C(═O)NR8R9, —(CH2)mC(═O)OR10, —(CH2)kC(═O)NR11R12; wherein R6 is a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R7 is hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl; R8 and R9 are each independently hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl, (C1-C30)alkylamino, (C1-C30)alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R8, N, and R9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R10 is hydrogen or a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R11, N and R12 together form a 4-8 membered heterocyclic ring; Ra and Rb are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3, or a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A2b adenosine receptor in a subject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.

  本发明提供具有以下结构的化合物：其中，R1是取代或未取代的烷基，其中取代基是羟基、二羟基、羧基、—C（═O）NRaRb、—NRaRb、—NRaC（═O）NRaRb、—NRaC（═O）ORa、—OC（═O）NRaRb或—NHC（═O）Ra；R2是氢或取代或未取代的烷基，其中取代基是羟基、二羟基、羧基、—C（═O）NRaRb、—NRaRb、—NRaC（═O）NRaRb、—NRaC（═O）ORa、—OC（═O）NRaRb或—NHC（═O）Ra，或R1、R2和N共同形成取代的哌嗪、取代的氮杂环丙烷环或取代的吡咯烷环，其被取代的基团为—（CH2）2OH或—CH2C（═O）OH；R3是取代或未取代的苯或5-6成员的杂芳环，其中取代基是卤素、羟基、氰基、（C1-C15）烷基、（C1-C15）烷氧基或—NRaRb；R4是氢或取代或未取代的（C1-C15）烷基；R5是—（CH2）mOR6、—CHNOR7、—C（═O）NR8R9、—（CH2）mC（═O）OR10、—（CH2）kC（═O）NR11R12；其中，R6是取代或未取代的（C1-C30）烷基、（C3-C10）环烷基或芳基、杂芳基或4-8成员的杂环；R7是氢或取代或未取代的（C1-C30）烷基、（C1-C30）烷基芳基；R8和R9分别独立地是氢或取代或未取代的（C1-C30）烷基、（C1-C30）烷基芳基、（C1-C30）烷基氨基、（C1-C30）烷氧基或饱和或不饱和的、单环或双环、碳环或杂环，或R8、N和R9共同形成取代或未取代的4-8成员的杂环；R10是氢或取代或未取代的（C1-C30）烷基、（C3-C10）环烷基或芳基、杂芳基或杂环；R11、N和R12共同形成4-8成员的杂环；Ra和Rb分别独立地是氢或烷基；m为0、1、2或3；k为1、2或3，或其特定对映体，或其特定互变异构体，或其药学上可接受的盐，以及一种用于治疗需要该治疗的受体A2b腺苷酸受体相关疾病的患者的方法，包括向患者投与本发明化合物的治疗有效量。