发明名称 A<sub>1 </sub>adenosine receptor antagonists
摘要 This invention relates to compounds of formula (I), Wherein R1-R4 are defined in the Specification, their uses in the practice of medicine, their medicinal formulations, their use in medical diagnosis, and their preparation.;
申请公布号 US9522916(B2) 申请公布日期 2016.12.20
申请号 US200813883893 申请日期 2008.12.19
申请人 Wilson Constance Neely 发明人 Wilson Constance Neely
分类号 C07D473/04;C07D473/06 主分类号 C07D473/04
代理机构 Passé Intellectual Property, LLC 代理人 Passé James G.;Passé Intellectual Property, LLC
主权项 1. A compound of formula (I): wherein; R1 is C2-8 straight or branched, optionally unsaturated, hydrocarbon moiety optionally substituted with one or more OR5, NR5R6, SO3H, PO3H2, COOR7, NR8R9, NR10COR11, Alk1COOR12, SO2R13, Alk2NR14R15, Alk3OH, or halogen groups, wherein R5 to R15 are independently H or C1-8 straight or branched, optionally unsaturated, hydrocarbon chain, Alk1 through Alk3 are independently C1-8 straight or branched alkylene or alkenylene; R2 is L1G1, wherein; L1 is a C1-2 or C4-20 straight or branched, optionally unsaturated, hydrocarbon chain moiety; G1 is a H, OR16, NR17R18, PO3H2, CONR19R20, COOR21, NR22COAlk4NR23R24, NR25COAlk5NR26Alk6NR27R28, OCOC6H4SO2F, NHCOC6H4SO2F; or a C3-11 hydrocarbon, optionally bridged, optionally aromatic, optionally unsaturated, ring optionally substituted with one or more groups selected from SO3H, PO3H2, halogen, OR29, COOR30, NO2, NR31R32, NR33COR34, NR35COAlk7NR36R37, NR38COAlk8CONR39Alk9NR40R41, NR42COAlk10COORAlk11NR43R44, Alk12NR45COAlk13NR46R47, Alk14NR48COAlk15CONR40Alk16NR50R51, Alk17COOR52, Alk18COAlk19NR53R54, SO2R55, SO2F, Alk20OR56, Alk21NR57R58, Alk22COAlk23CONR59Alk24NR60R61 or Alk25COOR62; wherein; Alk4-Alk25 are independently C1-8 straight or branched alkylene or alkenylene; R16-R62 are independently H or C1-8 straight or branched alkyl; R3 is L2G2, wherein; L2 is a C1 or C3-8 straight optionally unsaturated, hydrocarbon moiety optionally substituted with one or more, water soluble, polar groups selected from OR63, NR64R65, SO3H, PO3H2, COOR66, NR67R68NR69COR70, Alk26COOR71, SO2R72, Alk27NR73R74, Alk28OH, or halogen; and when L2 is C3-8, L2 may be intraspersed with one or more hetero atoms; G2 is one or two C4-5 or C7-11 non-aromatic, non-bridged, cyclic hydrocarbons, which independently may have one or more carbon atoms substituted with a hetero atom, and which may be optionally substituted with one or more groups selected from SO3H, PO3H2, halogen, OR75, COOR76, NO2, NR77COR78, Alk29COOR79, SO2R80, Alk30NR81R82, H, Alk31OH, NR85CONR86R87, Alk34H, or NR88R89; wherein; Alk26-Alk34 are independently C1-8 straight or branched alkylene or alkenylene, R63-R89 are independently H or C1-8 straight or branched alkyl; R4 is Cm alkyl, Alk36COOR90, Alk37CONR91R92, Alk39SO3H, Alk40PO3H2, Alk41OR93, Alk43NR94R95, or Alk44NR96Alk45OH; and R4 may also be H or methyl when G2 is one C4-5 or two C10-11 non-aromatic, non-bridged, cyclic hydrocarbons, wherein; Alk35 through Alk45 are independently C1-8 straight or branched alkylene or alkenylene; R90 through R96 are independently H or C1-8 straight or branched alkyl; and when R4 is other than H, methyl, alkyl, Alk36COOR90, Alk39SO3H, or Alk41ORg3, G2 may include bridged cyclic hydrocarbons; and salts thereof.
地址 Raleigh NC US