发明名称 METHODS OF ADMINISTERING GLUTAMINASE INHIBITORS
摘要 In some aspects, the invention relates to a method of treating cancer, a myeloproliferative disease, an immunological disease, a neurological disease, or a viral infection, comprising orally administering a compound of formula I, formula II, formula III, formula IV, formula V, and/or formula VI, wherein the compound is administered with a meal (e.g., with food as defined herein) or in fed mode.
申请公布号 US2016287564(A1) 申请公布日期 2016.10.06
申请号 US201615085451 申请日期 2016.03.30
申请人 Calithera Biosciences, Inc. 发明人 Gross Matthew I.;Bennett Mark K.;Molineaux Christopher
分类号 A61K31/433;A61K45/06;A61K31/5377;A61K31/496;A61K31/4545;A61K31/506;A61K31/444;A61K31/501;A61K31/4439;A61K31/519;A61K31/4245;A61K31/4725;A61K9/00;A61K31/4709 主分类号 A61K31/433
代理机构 代理人
主权项 1. A method of treating cancer, a myeloproliferative disease, an immunological disease, a neurological disease, or a viral infection, comprising orally administering a compound of formula I, or a pharmaceutically acceptable salt thereof, wherein: L represents CH2SCH2, CH2CH2, CH2CH2CH2, CH2, CH2S, SCH2, CH2NHCH2, CH═CH, or  wherein any hydrogen atom of a CH or CH2 unit may be replaced by alkyl or alkoxy, any hydrogen of an NH unit may be replaced by alkyl, and any hydrogen atom of a CH2 unit of CH2CH2, CH2CH2CH2 or CH2 may be replaced by hydroxy; X, independently for each occurrence, represents S, O or CH═CH, wherein any hydrogen atom of a CH unit may be replaced by alkyl; Y, independently for each occurrence, represents H or CH2O(CO)R7, R7, independently for each occurrence, represents H or substituted or unsubstituted alkyl, alkoxy, aminoalkyl, alkylaminoalkyl, heterocyclylalkyl, or heterocyclylalkoxy; Z represents H or R3(CO); R1 and R2 each independently represent H, alkyl, alkoxy or hydroxy; R3, independently for each occurrence, represents substituted or unsubstituted alkyl, hydroxyalkyl, aminoalkyl, acylaminoalkyl, alkenyl, alkoxy, alkoxyalkyl, aryl, arylalkyl, aryloxy, aryloxyalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl, heteroaryloxy, heteroaryloxyalkyl or C(R8)(R9)(R10), N(R4)(R5) or OR6, wherein any free hydroxyl group may be acylated to form C(O)R7; R4 and R5 each independently represent H or substituted or unsubstituted alkyl, hydroxyalkyl, acyl, aminoalkyl, acylaminoalkyl, alkenyl, alkoxyalkyl, aryl, arylalkyl, aryloxy, aryloxyalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl, heteroaryloxy, or heteroaryloxyalkyl, wherein any free hydroxyl group may be acylated to form C(O)R7; R6, independently for each occurrence, represents substituted or unsubstituted alkyl, hydroxyalkyl, aminoalkyl, acylaminoalkyl, alkenyl, alkoxyalkyl, aryl, arylalkyl, aryloxy, aryloxyalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl, heteroaryloxy, or heteroaryloxyalkyl, wherein any free hydroxyl group may be acylated to form C(O)R7; R8, R9 and R10 each independently represent H or substituted or unsubstituted alkyl, hydroxy, hydroxyalkyl, amino, acylamino, aminoalkyl, acylaminoalkyl, alkoxycarbonyl, alkoxycarbonylamino, alkenyl, alkoxy, alkoxyalkyl, aryl, arylalkyl, aryloxy, aryloxyalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl, heteroaryloxy, or heteroaryloxyalkyl, or R8 and R9 together with the carbon to which they are attached, form a carbocyclic or heterocyclic ring system, wherein any free hydroxyl group may be acylated to form C(O)R7; and the compound is preferably administered with a meal.
地址 South San Francisco CA US