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    Ataxia Telengiectasia And Rad3-Related (ATR) Protein Kinase Inhibitors
    5.
    发明申请
    Ataxia Telengiectasia And Rad3-Related (ATR) Protein Kinase Inhibitors 有权

    公开(公告)号：US20160102104A1

    公开(公告)日：2016-04-14

    申请号：US14881680

    申请日：2015-10-13

    申请人： Atrin Pharmaceuticals LLC

    发明人： Henry Joseph Breslin ,  Oren Gilad

    IPC分类号： C07D498/08 ,  A61K31/4985 ,  A61N5/10 ,  C07D498/18 ,  A61K31/5377 ,  C07D515/08 ,  A61K45/06

    CPC分类号： C07D519/00 ,  A61K31/4985 ,  A61K31/5377 ,  A61K45/06 ,  C07D498/08 ,  C07D498/18 ,  C07D515/08 ,  C07D515/18

    摘要： 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.

    Methods for processing chemical compounds having reactive functional groups
    8.
    发明授权
    Methods for processing chemical compounds having reactive functional groups 失效
    处理具有反应性官能团的化合物的方法

    公开(公告)号：US06559303B1

    公开(公告)日：2003-05-06

    申请号：US09254219

    申请日：1999-04-09

    申请人： Phillip Dan Cook

    发明人： Phillip Dan Cook

    IPC分类号： C07D47108

    CPC分类号： C07D471/08 ,  B01J2219/0072 ,  C07D515/08

    摘要： Novel macrocyclic compounds are constructed to include large cyclic structures that are interrupted by at least one ring system. Each interrupting ring system includes two bridgehead atoms. Bridgehead atoms are bonded to one or more bridges that interconnect one or more ring systems thereby forming a large cyclic structure. Located in each bridge are two or more nitrogenous moieties that are derivatized with chemical functional groups. The ring systems can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring. These can also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the macrocyclic compounds. In accordance with certain embodiments of the invention, libraries of such macrocyclic compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the library.

    摘要翻译： 构建新的大环化合物以包括被至少一个环系统中断的大环状结构。 每个中断环系统包括两个桥头原子。 桥头原子键合到一个或多个互连一个或多个环系统的桥，从而形成大的环状结构。 位于每个桥中的是具有化学官能团衍生化的两个或多个含氮部分。 环系统可以包括作为环原子的另外的含氮部分或连接到环上的侧基上。 这些也可以用化学官能团衍生化。 化学官能团的总体对大环化合物赋予某些构象和其他性质。 根据本发明的某些实施方案，利用化学官能团和含氮部分的置换和组合来制备这种大环化合物的文库，从而构建文库的复杂性。

    Inhibitors of prenyl-protein transferase
    9.
    发明授权
    Inhibitors of prenyl-protein transferase 失效
    异戊烯基蛋白转移酶的抑制剂

    公开(公告)号：US06413964B1

    公开(公告)日：2002-07-02

    申请号：US09757213

    申请日：2001-01-09

    申请人： S. Jane deSolms ,  Suzanne C. MacTough ,  Anthony W. Shaw

    发明人： S. Jane deSolms ,  Suzanne C. MacTough ,  Anthony W. Shaw

    IPC分类号： A61K3155

    CPC分类号： C07D515/08

    摘要： The present invention is directed to peptidomimetic macrocyclic compounds of the formula A: wherein W is a heterocycle, V is a heterocycle or aryl moiety and Z1 is a suitably substituted aryl or heterocycle moiety. The instant compounds inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

    摘要翻译： 本发明涉及式A的拟肽大环化合物：其中W是杂环，V是杂环或芳基，Z1是适当取代的芳基或杂环部分。 本发明化合物抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化。 本发明还涉及含有本发明化合物的化疗组合物和抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化的方法。