公开(公告)号：US20180208561A1

公开(公告)日：2018-07-26

申请号：US15326490

申请日：2015-06-15

Applicant: Development Center for Biotechnology ,  DCB-USA LLC

Inventor： Nan-Horng Lin ,  Chu-Bin Liao ,  Shao-Zheng Peng ,  Shih-Chieh Yen ,  Mann-Yan Kuo

IPC: C07D241/44 ,  A61P35/00 ,  A61P3/10 ,  A61P13/12 ,  A61P9/00 ,  A61P19/02 ,  C07D413/12 ,  C07D401/12 ,  C07D413/04

Abstract: A compound for treating a protein kinase-related disease or disorder having a structure of formula (I) wherein L is NR8 or O; R1, R2, R3, R4, R5, R6 and R7 are defined herein. Compounds of formula (I) are useful for inhibition of protein kinases. Methods of using compounds of formula (I), stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed

公开(公告)号：US10745360B2

公开(公告)日：2020-08-18

申请号：US15326490

申请日：2015-06-15

Applicant: Development Center for Biotechnology ,  DCB-USA LLC

Inventor： Nan-Horng Lin ,  Chu-Bin Liao ,  Shao-Zheng Peng ,  Shih-Chieh Yen ,  Mann-Yan Kuo

IPC: C07D241/44 ,  C07D401/12 ,  A61P35/00 ,  C07D413/04 ,  C07D413/12 ,  A61P9/00 ,  A61P19/02 ,  A61P3/10 ,  A61P13/12

Abstract: A compound for treating a protein kinase-related disease or disorder having a structure of formula (I) wherein L is NR8 or O; R1, R2, R3, R4, R5, R6 and R7 are defined herein. Compounds of formula (I) are useful for inhibition of protein kinases. Methods of using compounds of formula (I), stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

公开(公告)号：US09321762B2

公开(公告)日：2016-04-26

申请号：US14103662

申请日：2013-12-11

Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGY

Inventor： Mann-Yan Kuo ,  Chu-Bin Liao ,  Shao-Zheng Peng ,  Shih-Chieh Yen ,  Nan-Horng Lin

IPC: C07D417/14 ,  C07D239/94 ,  C07D401/04 ,  C07D403/04

CPC classification number: C07D417/14 ,  C07D239/94 ,  C07D401/04 ,  C07D403/04

Abstract: A compound for treating a protein kinase-related disease or disorder having a structure of formula (I) wherein G is a heteroaryl, heterocyclic or alkyne; X is N or CH; L1 is —N(R7)—, —O—, —C(S)—, —C(O)—, or —S—; L2 is —N(R8)— or —O—; R1 and R2 are independently hydrogen, halogen, hydroxyl, amino, cyano, nitro, carboxy, C1-C4 alkoxy, C1-C4 alkoxy C1-C4 alkoxy, N,N—(C1-C4 dialkyl)amino C1-C4 alkoxy, N—(C1-C4 alkyl)amino C1-C4 alkoxy, C1-C4 alkanoyl, C1-C4 alkanoyloxy, N—(C1-C4 alkyl)amino, N,N—(C1-C4 dialkyl)amino, C1-C4 alkanoyl amino, or heterocyclyl, wherein C1-C4 alkyl is optionally substituted with one or more substituents selected from fluorine and chlorine; R3, R4 and R5 are independently hydrogen, fluorine or chlorine; R6 is C1-C4 alkyl or aryl, which is optionally substituted with one or more substituents selected from halogen, hydroxyl, amino, cyano, nitro; or R6 and R8 form a 5-6 membered cyclyl or heterocyclyl.

Abstract translation: 一种用于治疗具有式（I）结构的蛋白激酶相关疾病或病症的化合物，其中G是杂芳基，杂环或炔基; X为N或CH; L 1是-N（R 7） - ， - O - ， - C（S） - ， - C（O） - 或-S-; L2是-N（R8） - 或-O-; R1和R2独立地是氢，卤素，羟基，氨基，氰基，硝基，羧基，C1-C4烷氧基，C1-C4烷氧基C1-C4烷氧基，N，N-（C1-C4二烷基）氨基C1-C4烷氧基，N - （C 1 -C 4烷基）氨基C 1 -C 4烷氧基，C 1 -C 4烷酰基，C 1 -C 4烷酰氧基，N-（C 1 -C 4烷基）氨基，N，N-（C 1 -C 4二烷基）氨基，C 1 -C 4烷酰基氨基 或杂环基，其中C 1 -C 4烷基任选被一个或多个选自氟和氯的取代基取代; R3，R4和R5独立地是氢，氟或氯; R6是C1-C4烷基或芳基，其任选被一个或多个选自卤素，羟基，氨基，氰基，硝基的取代基取代; 或R6和R8形成5-6元环基或杂环基。

公开(公告)号：US11407757B2

公开(公告)日：2022-08-09

申请号：US16958721

申请日：2018-12-26

Applicant: Development Center for Biotechnology

Inventor： Shih-Chieh Yen ,  Chu-Bin Liao ,  Hui-Chen Wang ,  Po-Ting Chen ,  Yu-Chih Pan ,  Tsung-Hui Li ,  Bo-Rong Chen ,  Shian-Yi Chiou

IPC: C07D487/04 ,  A61P35/00

Abstract: Disclosed are compounds of formula (I) below and tautomers, stereoisomers, isotopologues, or pharmaceutically acceptable salts thereof: in which each of variables R1, ring A, L, W, V, and G is defined herein. Also disclosed are a method for treating disease or disorder mediated by Tyro3, Axl, and/or Mer kinase with a compound of formula (I) or a tautomer, stereoisomer, isotopologue, or salt thereof and a pharmaceutical composition containing same.

公开(公告)号：US20150158854A1

公开(公告)日：2015-06-11

申请号：US14103662

申请日：2013-12-11

Applicant: Development Center For Biotechnology

Inventor： Mann-Yan Kuo ,  Chu-Bin Liao ,  Shao-Zheng Peng ,  Shih-Chieh Yen ,  Nan-Horng Lin

IPC: C07D417/14 ,  C07D403/04 ,  C07D239/94 ,  C07D401/04

CPC classification number: C07D417/14 ,  C07D239/94 ,  C07D401/04 ,  C07D403/04

Abstract: A compound for treating a protein kinase-related disease or disorder having a structure of formula (I) wherein G is a heteroaryl, heterocyclic or alkyne; X is N or CH; L1 is —N(R7)—, —O—, —C(S)—, —C(O)—, or —S—; L2 is —N(R8)— or —O—; R1 and R2 are independently hydrogen, halogen, hydroxyl, amino, cyano, nitro, carboxy, C1-C4 alkoxy, C1-C4 alkoxy C1-C4 alkoxy, N,N—(C1-C4 dialkyl)amino C1-C4 alkoxy, N—(C1-C4 alkyl)amino C1-C4 alkoxy, C1-C4 alkanoyl, C1-C4 alkanoyloxy, N—(C1-C4 alkyl)amino, N,N—(C1-C4 dialkyl)amino, C1-C4 alkanoyl amino, or heterocyclyl, wherein C1-C4 alkyl is optionally substituted with one or more substituents selected from fluorine and chlorine; R3, R4 and R5 are independently hydrogen, fluorine or chlorine; R6 is C1-C4 alkyl or aryl, which is optionally substituted with one or more substituents selected from halogen, hydroxyl, amino, cyano, nitro; or R6 and R8 form a 5-6 membered cyclyl or heterocyclyl.

Abstract translation: 一种用于治疗具有式（I）结构的蛋白激酶相关疾病或病症的化合物，其中G是杂芳基，杂环或炔基; X为N或CH; L 1是-N（R 7） - ， - O - ， - C（S） - ， - C（O） - 或-S-; L2是-N（R8） - 或-O-; R1和R2独立地是氢，卤素，羟基，氨基，氰基，硝基，羧基，C1-C4烷氧基，C1-C4烷氧基C1-C4烷氧基，N，N-（C1-C4二烷基）氨基C1-C4烷氧基，N - （C 1 -C 4烷基）氨基C 1 -C 4烷氧基，C 1 -C 4烷酰基，C 1 -C 4烷酰氧基，N-（C 1 -C 4烷基）氨基，N，N-（C 1 -C 4二烷基）氨基，C 1 -C 4烷酰基氨基 或杂环基，其中C 1 -C 4烷基任选被一个或多个选自氟和氯的取代基取代; R3，R4和R5独立地是氢，氟或氯; R6是C1-C4烷基或芳基，其任选被一个或多个选自卤素，羟基，氨基，氰基，硝基的取代基取代; 或R6和R8形成5-6元环基或杂环基。