Triazaspiro[4.5]decan | 19540-00-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: Triazaspiro[4.5]decan
• 英文别名: 1,2,3-triazaspiro[4.5]decane
• CAS: 19540-00-2
• 化学式: C₇H₁₅N₃
• 分子量: 141.21
• InChiKey: AQKHWDFZPSQMCS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  36.1
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• Substituted Indole Compounds
  申请人：Schunk Stefan

  公开号：US20100222324A1

  公开（公告）日：2010-09-02

  Substituted indole compounds corresponding to the formula I: In which R 8 , R 9a , R 9b , R 10 , R 11 , R 200 , R 210 , A, D, T, q, s and t have defined meanings, processes for the preparation thereof, pharmaceutical compositions containing such compounds and the use of substituted indole compounds for the treatment or inhibition of pain and other conditions which are at least partly mediated by Bradykinin 1 receptors (B1R).

  将与下式I对应的吲哚化合物替代： 其中R8、R9a、R9b、R10、R11、R200、R210、A、D、T、q、s和t具有定义的含义，其制备方法，含有这种化合物的药物组合物以及用于治疗或抑制至少部分由Bradykinin 1受体（B1R）介导的疼痛和其他病症的替代吲哚化合物的用途。
• 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。
• 4,4-DISUBSTITUTED PIPERIDINE DERIVATIVES
  申请人：Christ Andreas D.

  公开号：US20080293756A1

  公开（公告）日：2008-11-27

  This invention relates to 4,4-disubstituted piperidine derivatives of the formula wherein A and R 1 to R 5 are as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

  这项发明涉及公式 的4,4-二取代哌啶衍生物，其中A和R1至R5如规范中所定义，并其药学上可接受的盐。该发明还涉及含有这种化合物的药物组合物，以及用于制备它们的方法和它们用于治疗和/或预防与调节SST受体亚型5相关的疾病的用途。
• [EN] 2-OXO-1,3,8-TRIAZASPIRO[4.5]DECAN-3-YL] CARBOXYLIC ACID DERIVATIVES<br/>[FR] DÉRIVÉS DE L'ACIDE 2-OXO-1,3,8-TRIAZASPIRO[4,5]DÉCAN-3-YL] CARBOXYLIQUE
  申请人：LILLY CO ELI

  公开号：WO2016205032A1

  公开（公告）日：2016-12-22

  The present invention provides compounds of Formula 1, where A is selected from (formula II), (formula III), and; (formula IV) and R1, R2 and R3 are defined in the specification, or a pharmaceutically acceptable salt thereof, methods of using the compounds to treat diabetes, and processes for the synthesis of the compounds.

  本发明提供了Formula 1的化合物，其中A从(formula II)，(formula III)和(formula IV)中选择；R1、R2和R3在规范中定义，或其药用可接受盐，使用这些化合物治疗糖尿病的方法，以及合成这些化合物的方法。