发明名称 METHODS OF TREATING FIBROSIS
摘要 Disclosed are methods of treating fibrosis in a patient, comprising administering to a patient in need thereof a therapeutically effective amount of an ACK inhibitor (e.g., a BTK inhibitor, such as for example an irreversible BTK inhibitor, such as for example, ibrutinib).
申请公布号 US2016199376(A1) 申请公布日期 2016.07.14
申请号 US201514957294 申请日期 2015.12.02
申请人 Pharmacyclics LLC 发明人 GONZÁLEZ Toni Jauset;MASSÓ-VALLÉS Daniel;SOUCEK Laura
分类号 A61K31/519 主分类号 A61K31/519
代理机构 代理人
主权项 1. A method of treating fibrosis in a patient, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of Formula (A) having the structure: wherein: A is N; R1 is phenyl-O-phenyl or phenyl-S-phenyl; R2 and R3 are independently H; R4 is L3-X-L4-G, wherein, L3 is optional, and when present is a bond, optionally substituted or unsubstituted alkyl, optionally substituted or unsubstituted cycloalkyl, optionally substituted or unsubstituted alkenyl, optionally substituted or unsubstituted alkynyl; X is optional, and when present is a bond, —O—, —C(═O)—, —S—, —S(═O)—, —S(═O)2—, —NH—, —NR9—, —NHC(O)—, —C(O)NH—, —NR9C(O)—, —C(O)NR9—, —S(═O)2NH—, —NHS(═O)2—, —S(═O)2NR9—, —NR9S(═O)2—, —OC(O)NH—, —NHC(O)O—, —OC(O)NR9—, —NR9C(O)O—, —CH═NO—, —ON═CH—, —NR10C(O)NR10—, heteroaryl-, aryl-, —NR10C(═NR11)NR10—, —NR10C(═NR11)—, —C(═NR11)NR10—, —OC(═NR11)—, or —C(═NR11)O—; L4 is optional, and when present is a bond, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocycle; or L3, X and L4 taken together form a nitrogen containing heterocyclic ring; G iswherein, R6, R7 and R8 are independently selected from among H, halogen, CN, OH, substituted or unsubstituted alkyl or substituted or unsubstituted heteroalkyl or substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl; each R9 is independently selected from among H, substituted or unsubstituted lower alkyl, and substituted or unsubstituted lower cycloalkyl; each R10 is independently H, substituted or unsubstituted lower alkyl, or substituted or unsubstituted lower cycloalkyl; or two R10 groups can together form a 5-, 6-, 7-, or 8-membered heterocyclic ring; or R10 and R11 can together form a 5-, 6-, 7-, or 8-membered heterocyclic ring; or each R11 is independently selected from H or substituted or unsubstituted alkyl; or a pharmaceutically acceptable salt thereof, thereby treating the fibrosis.
地址 Sunnyvale CA US