发明名称 THERAPEUTIC COMPOUNDS AND METHODS
摘要 Biguanide compounds and salts thereof are disclosed. Also disclosed are pharmaceutical compositions and therapeutic methods for treating certain diseases including cancer such as breast cancer.
申请公布号 US2015342909(A1) 申请公布日期 2015.12.03
申请号 US201514641122 申请日期 2015.03.06
申请人 Regents of the University of Minnesota 发明人 Potter David A.;Guo Zhijun;Amin Elizabeth;Georg Gunda;Poulos Tom;Sevrioukova Irina
分类号 A61K31/155;A61K31/426;A61K31/417;A61K38/44;C07C279/26;C07D213/36;C07D277/28;C07D233/64;A61K31/4409;A61K45/06 主分类号 A61K31/155
代理机构 代理人
主权项 1. A method for treating or preventing breast cancer occurrence or recurrence in a patient in need thereof, comprising administering to the patient in need thereof an effective amount of a compound of formula I:wherein: R1 is H, (C1-C12)alkyl, (C2-C12)alkenyl, (C2-C12)alkynyl, —O(C1-C12)alkyl, —O(C2-C12)alkenyl, —O(C2-C12)alkynyl, —OH, (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl, wherein any (C1-C12)alkyl, (C2-C12)alkenyl, (C2-C12)alkynyl, —O(C1-C12)alkyl, —O(C2-C12)alkenyl or —O(C2-C12)alkynyl of R1 is optionally substituted with one or more Z1a groups and wherein any (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl of R1 is optionally substituted with one or more Z1b groups; R2 is H, (C1-C12)alkyl, (C2-C12)alkenyl, (C2-C12)alkynyl, —O(C1-C12)alkyl, —O(C2-C12)alkenyl, —O(C2-C12)alkynyl, —OH, (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl, wherein any (C1-C12)alkyl, (C2-C12)alkenyl, (C2-C12)alkynyl, —O(C1-C12)alkyl, —O(C2-C12)alkenyl, —O(C2-C12)alkynyl of R2 is optionally substituted with one or more Z2a groups and wherein any (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl of R1 is optionally substituted with one or more Z2b groups; R3 is H, (C1-C12)alkyl, (C2-C12)alkenyl, (C2-C12)alkynyl, —O(C1-C12)alkyl, —O(C2-C12)alkenyl, —O(C2-C12)alkynyl, —OH, (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl, wherein any (C1-C12)alkyl, (C2-C12)alkenyl, (C2-C12)alkynyl, —O(C1-C12)alkyl, —O(C2-C12)alkenyl or —O(C2-C12)alkynyl of R3 is optionally substituted with one or more Z3a groups and wherein any (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl of R3 is optionally substituted with one or more Z3b groups; R4 is H, (C1-C12)alkyl, (C2-C12)alkenyl, (C2-C12)alkynyl, —O(C1-C12)alkyl, —O(C2-C12)alkenyl, —O(C2-C12)alkynyl, —OH, (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl, wherein any (C1-C12)alkyl, (C2-C12)alkenyl, (C2-C12)alkynyl, —O(C1-C12)alkyl, —O(C2-C12)alkenyl, —O(C2-C12)alkynyl of R4 is optionally substituted with one or more Z4a groups and wherein any (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl of R4 is optionally substituted with one or more Z4b groups; Z1a is —OH, halogen, —O(C1-C6)alkyl, —C(═O)O(C1-C6)alkyl, (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl, wherein any (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl of Z1a is optionally substituted with one or more groups selected from (C1-C6)alkyl, —OH, halogen and —O(C1-C6)alkyl; Z1b is (C1-C6)alkyl, —OH, halogen or —O(C1-C6)alkyl; Z2a is —OH, halogen, —O(C1-C6)alkyl, —C(═O)O(C1-C6)alkyl, (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl, wherein any (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl of Z2a is optionally substituted with one or more groups selected from (C1-C6)alkyl, —OH, halogen and —O(C1-C6)alkyl; Z2b is (C1-C6)alkyl, —OH, halogen or —O(C1-C6)alkyl; Z3a is —OH, halogen, —O(C1-C6)alkyl, —C(═O)O(C1-C6)alkyl, (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl, wherein any (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl of Z3a is optionally substituted with one or more groups selected from (C1-C6)alkyl, —OH, halogen and —O(C1-C6)alkyl; Z3b is (C1-C6)alkyl, —OH, halogen or —O(C1-C6)alkyl; Z4a is —OH, halogen, —O(C1-C6)alkyl, —C(═O)O(C1-C6)alkyl, (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl, wherein any (C3-C8)carbocycle, 5-10 membered heteroaryl or aryl of Z4a is optionally substituted with one or more groups selected from (C1-C6)alkyl, —OH, halogen and —O(C1-C6)alkyl; and Z4b is (C1-C6)alkyl, —OH, halogen or —O(C1-C6)alkyl; or a pharmaceutically acceptable salt thereof.
地址 Minneapolis MN US