发明申请
US20080261943A1 PYRROLOPYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE
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基本信息:
- 专利标题: PYRROLOPYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE
- 申请号:US10536119 申请日:2007-06-19
- 公开(公告)号:US20080261943A1 公开(公告)日:2008-10-23
- 发明人: Arlindo Castelhano , Bryan McKibben , Arno Steinig
- 申请人: Arlindo Castelhano , Bryan McKibben , Arno Steinig
- 申请人地址: US NY Melville
- 专利权人: OSI PHARMACEUTICALS, INC.
- 当前专利权人: OSI PHARMACEUTICALS, INC.
- 当前专利权人地址: US NY Melville
- 主分类号: A61K31/519
- IPC分类号: A61K31/519 ; C07D487/04
摘要:
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 —NH C(═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.
公开/授权文献:
IPC结构图谱:
A | 人类生活必需 |
--A61 | 医学或兽医学;卫生学 |
----A61K | 医用、牙科用或梳妆用的配制品 |
------A61K31/00 | 含有机有效成分的医药配制品 |
--------A61K31/33 | .杂环化合物 |
----------A61K31/335 | ..仅有氧作为环杂原子的,例如制霉色基素 |
------------A61K31/40 | ...有仅以1个氮作为环杂原子的五元环的,例如舒必利、琥珀酰亚胺、托尔米丁、甲氧吡丁苯 |
--------------A61K31/50 | ....哒嗪;氢化哒嗪 |
----------------A61K31/519 | .....与杂环系统邻位或迫位稠合的 |