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    • 5. 发明申请
    • Ataxia Telengiectasia And Rad3-Related (ATR) Protein Kinase Inhibitors
    • US20160102104A1
    • 2016-04-14
    • US14881680
    • 2015-10-13
    • Atrin Pharmaceuticals LLC
    • Henry Joseph BreslinOren Gilad
    • C07D498/08A61K31/4985A61N5/10C07D498/18A61K31/5377C07D515/08A61K45/06
    • C07D519/00A61K31/4985A61K31/5377A61K45/06C07D498/08C07D498/18C07D515/08C07D515/18
    • A macrocyclic compound having the structure of Formula (A), wherein each of R1 and R2 is independently (i) a 5-6 membered monocyclic aromatic ring containing 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or (ii) an 8-10 membered bicyclic aromatic ring containing 0-6 heteroatoms independently selected from nitrogen, oxygen, or sulfur. Each R1 and R2 may independently be substituted by 0, 1, 2, 3, or 4 substituents. Z1 represents a covalent bond, an atom, or a functional group comprising a grouping of atoms, wherein the grouping of atoms includes at least one heteroatom selected from the group consisting of N, O, P, and S. Also, Z1 may represent (i) a 5-6 membered monocyclic aromatic ring containing 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or (ii) an 8-10 membered bicyclic aromatic ring containing 0-6 heteroatoms independently selected from nitrogen, oxygen, or sulfur. Z2 represents a covalent bond, an atom, or a functional group comprising a grouping of atoms, wherein the grouping of atoms includes at least one heteroatom selected from the group consisting of N, O, P, and S. Variable v is an integer having a value of 1 or 0. T is a carbon atom, a nitrogen atom, a sulfur atom, or an oxygen atom. L is a linking group covalently bonded to T when v has a value of 1 or L is covalently bonded to R1 when v has a value of 0. L is covalently bonded to Z2 when Z2 is an atom or a functional group comprising grouping of atoms and/or L is covalently bonded to R2 when Z2 is a covalent bond. Each of R3, R4 and R5 may be the same as or different from each other and each is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, aralkyl, and heteraralkyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, aralkyl, and heteraralkyl is optionally substituted by one or more suitable substituents.