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    Histone deacetylases (HDACs) inhibitors
    1.
    发明授权
    Histone deacetylases (HDACs) inhibitors 有权
    组蛋白脱乙酰酶（HDACs）抑制剂

    公开(公告)号：US09387209B2

    公开(公告)日：2016-07-12

    申请号：US13855525

    申请日：2013-04-02

    申请人： ANNJI PHARMACEUTICAL CO., LTD.

    发明人： Ji-Wang Chern ,  Chao-Wu Yu ,  Pei-Teh Chang

    IPC分类号： A61K31/517 ,  C07D239/91 ,  C07D403/06

    CPC分类号： A61K31/517 ,  C07D239/91 ,  C07D403/06

    摘要： Histone deacetylases inhibitors (HDACIs) and compositions comprising the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit are also disclosed. In one aspect, the invention relates to a compound having the structure or a pharmaceutically acceptable salt, a solvate or hydrate, a prodrug, or a metabolite thereof. In one embodiment of the invention, R1 is ethyl; R2 is 2-phenylethyl; R3 is hydrogen; R4 is fluoro; R5 is (2E)-3-N-hydroxyamino-3-oxo-propenyl; and R6 is hydrogen, or a salt thereof. In another embodiment of the invention, R1 is ethyl; R2 is 2-phenylethyl; R3 is hydrogen; R4 is (2E)-3-N-hydroxyamino-3-oxo-propenyl; R5 is chloro or fluoro; and R6 is hydrogen, or a salt thereof.

    摘要翻译： 组蛋白脱乙酰酶抑制剂（HDACI）和包含其的组合物被公开。 还公开了治疗HDAC的抑制提供益处的疾病和病症的方法。 一方面，本发明涉及具有结构或其药学上可接受的盐，溶剂化物或水合物，前药或代谢物的化合物。 在本发明的一个实施方案中，R 1是乙基; R2是2-苯基乙基; R3是氢; R4是氟; R5是（2E）-3-N-羟基氨基-3-氧代 - 丙烯基; R6为氢，或其盐。 在本发明的另一个实施方案中，R 1是乙基; R2是2-苯基乙基; R3是氢; R4是（2E）-3-N-羟基氨基-3-氧代 - 丙烯基; R5是氯或氟; R6为氢，或其盐。

    Histone deacetylases (HDACs) inhibitors
    2.
    发明授权
    Histone deacetylases (HDACs) inhibitors 有权

    公开(公告)号：US11535598B2

    公开(公告)日：2022-12-27

    申请号：US16494284

    申请日：2018-05-15

    申请人： ANNJI PHARMACEUTICAL CO., LTD.

    发明人： Ji-Wang Chern ,  Chao-Wu Yu ,  Jia-Rong Liu ,  Yi-Hsun Ho ,  Chia-Yu Wu ,  Chan-Hui Huang ,  Pei-Yun Hung

    IPC分类号： C07D239/96 ,  C07D401/04 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D471/04 ,  C07D495/04

    摘要： Histone deacetylases (HDACs) inhibitors are disclosed according to the following structural formula. The moiety A is a benzene ring, optionally substituted. The moiety B is a benzene ring attached at the 1,4 or 1,3 position, or a cyclohexane ring attached at the 1,4 position, optionally substituted. R and Z are further substituents. The HDACs inhibitors possess cytotoxicities to various cancer cell lines. They are useful for treating a tumor associated with deregulation of the activity of histone deacetylases in a subject in need thereof, in one embodiment, the HDACs inhibitors of the invention are useful for treating glioma, breast cancer, colon cancer, target cell lung cancer, adenocarcinoma of the lung, small cell lung cancer, stomach cancer, liver cancer, ovary adenocarcinoma, pancreas carcinoma, prostate carcinoma, promyiocytic leukemia, chronic myelocytic leukemia, or acute lymphocytic leukemia in a subject in need thereof.

    Indolin-2-one derivatives as protein kinase inhibitors
    3.
    发明授权
    Indolin-2-one derivatives as protein kinase inhibitors 有权

    公开(公告)号：US08946282B2

    公开(公告)日：2015-02-03

    申请号：US13855916

    申请日：2013-04-03

    申请人： Annji Pharmaceutical Co., Ltd.

    发明人： Ji-Wang Chern ,  Ajit Dhananjay Jagtap ,  Hsiao-Chun Wang ,  Grace Shiahuy Chen

    IPC分类号： C07D209/34 ,  C07D403/06 ,  C07D401/06 ,  A61K38/45 ,  C07D401/14 ,  C07D409/06 ,  C07D405/06 ,  C07D403/14 ,  A61K31/522 ,  C07D473/32 ,  C07D209/00

    CPC分类号： C07D209/34 ,  A61K31/522 ,  A61K38/45 ,  C07D209/00 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06 ,  C07D409/06 ,  C07D473/32

    摘要： A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer. In one aspect, the invention relates to a compound a compound of Formula A: or a pharmaceutically acceptable salt thereof, wherein: Ra is hydrogen, (C6-C18)aryl, halo(C6-C18)aryl, or (C1-C6)alkoxy(C6-C18)aryl; Rb is hydrogen, (C3-C18)heteroaryl, (C1-C6)alkoxy(C3-C18)heteroaryl; (C1-C6)alkyl(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)alkoxy(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)carboxyalkyl(C3-C18)heteroaryl; (C1-C6)alkyl(C1-C6)alkylamino(C1-C6)alkylcarbamoyl)(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C18)aryl(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)alkoxycarbonyl)(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)alkoxy(C1-C6)oxyalkyl(C3-C18)heteroaryl, (C1-C6)alkyl(C3-C6)heterocyclylcarbonyl(C3-C18)heteroaryl, (C1-C6)alkyl(C3-C6)heterocyclyl(C1-C6)oxyalkyl(C3-C18)heteroaryl, or (C1-C6)alkyl((C3-C6)heterocyclyl(C1-C6)alkylcarbamoyl)(C3-C18)heteroaryl; Rc is hydrogen, (C1-C6)alkoxybenzoylureido, or halo(C6-C18)aryl(C3-C18)heteroarylamido; Rd is hydrogen, halogen, (C1-C6)alkoxybenzoylureido, or halo(C6-C18)aryl(C3-C18)heteroarylamido; Re is-hydrogen, benzoylureido, halobenzoylureido, halo(C1-C6)alkoxybenzoylureido, (C1-C6)alkoxybenzoylureido, (C1-C6)alkylaminobenzoylureido, (C1-C6)alkylbenzoylureido, nitrobenzoylureido, (C1-C6)haloalkylbenzoylureido, (C1-C6)haloalkylhalobenzoylureido, halo(C6-C18)arylcarbomylacetamido, (C1-C6)alkoxy(C6-C18)arylcarbomylacetamido, (C1-C6)alkoxy(C6-C18)arylcarbamoyl(C3-C6)cycloalkylamido, halo(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, (C3-C6)cycloalkyl(C3-C18)heteroarylcarbonylamino, (C1-C6)alkylamino(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, halo(C1-C6)alkoxy(C6-C18)aryl(C3-C18) heteroarylcarbonylamino, (C1-C6)alkoxy(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, (C1-C6)alkyl(C3-C18)heteroarylcarbonylamino, aryl(C3-C18)heteroarylcarbonylamino, (C1-C6)haloalkylhalo(C6-C18)aryl(C3-C6)heterocyclylcarbonylamino, (C1-C6)haloalkyl(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, halo(C6-C18)aryl(C3-C18)heteroarylamido, (C1-C6)oxyalkyl(C3-C6)heterocyclylamido, (C1-C6)alkoxy(C1-C6)alkyl(C3-C18)heteroarylamido, (C6-C18)aryl(C3-C18)heteroarylamido, (C1-C6)alkyl(C1-C18)aryl(C3-C18)heteroarylamido, (C1-C6)haloalkyl(C6-C18)aryl(C3-C18)heteroarylamido, (C1-C6)alkyl(C3-C18)heteroarylamido, or (C1-C6)alkoxy(C6-C18)aryl(C3-C18)heteroarylamido; and Rf is hydrogen, (C1-C6)alkoxybenzoylureido, or halo(C6-C18)aryl(C3-C18)heteroarylamido.

    Histone deacetylases (HDACs) inhibitors
    5.
    发明授权
    Histone deacetylases (HDACs) inhibitors 有权
    组蛋白脱乙酰酶（HDACs）抑制剂

    公开(公告)号：US09155739B2

    公开(公告)日：2015-10-13

    申请号：US14666169

    申请日：2015-03-23

    申请人： ANNJI PHARMACEUTICAL CO., LTD.

    发明人： Ji-Wang Chern ,  Chao-Wu Yu ,  Pei-Teh Chang

    IPC分类号： A61K31/517 ,  C07D239/91 ,  C07D403/06

    CPC分类号： A61K31/517 ,  C07D239/91 ,  C07D403/06

    摘要： Histone deacetylases inhibitors (HDACIs) and methods for treating cancer in a subject in need thereof are disclosed. The HDACIs comprise a compound of Formula X. or a pharmaceutically acceptable salt thereof. In one embodiment of the invention, R1 is ethyl; R2 is 2-phenylethyl; R3 is hydrogen; R4 is fluoro; R5 is (2E)-3-N-hydroxyamino-3-oxo-propenyl; and R6 is hydrogen, or a salt thereof. In another embodiment of the invention, R1 is ethyl; R2 is 2-phenylethyl; R3 is hydrogen; R4 is (2E)-3-N-hydroxyamino-3-oxo-propenyl; R5 is chloro or fluoro; and R6 is hydrogen.

    摘要翻译： 公开组蛋白脱乙酰酶抑制剂（HDACI）和治疗有此需要的受试者的癌症的方法。 HDACIs包含式X化合物或其药学上可接受的盐。 在本发明的一个实施方案中，R 1是乙基; R2是2-苯基乙基; R3是氢; R4是氟; R5是（2E）-3-N-羟基氨基-3-氧代 - 丙烯基; R6为氢，或其盐。 在本发明的另一个实施方案中，R 1是乙基; R2是2-苯基乙基; R3是氢; R4是（2E）-3-N-羟基氨基-3-氧代 - 丙烯基; R5是氯或氟; R6是氢。

    HISTONE DEACETYLASES (HDACS) INHIBITORS
    6.
    发明申请
    HISTONE DEACETYLASES (HDACS) INHIBITORS 审中-公开
    HISTONE DEACETYLASES（HDACS）抑制剂

    公开(公告)号：US20150196563A1

    公开(公告)日：2015-07-16

    申请号：US14666169

    申请日：2015-03-23

    申请人： ANNJI PHARMACEUTICAL CO., LTD.

    发明人： Ji-Wang Chern ,  Chao-Wu Yu ,  Pei-Teh Chang

    IPC分类号： A61K31/517

    CPC分类号： A61K31/517 ,  C07D239/91 ,  C07D403/06

    摘要： Histone deacetylases inhibitors (HDACIs) and methods for treating cancer in a subject in need thereof are disclosed. The HDACIs comprise a compound of Formula X. or a pharmaceutically acceptable salt thereof. In one embodiment of the invention, R1 is ethyl; R2 is 2-phenylethyl; R3 is hydrogen; R4 is fluoro; R5 is (2E)-3-N-hydroxyamino-3-oxo-propenyl; and R6 is hydrogen, or a salt thereof. In another embodiment of the invention, R1 is ethyl: R2 is 2-phenylethyl; R3 is hydrogen; R4 is (2E)-3-N-hydroxyamino-3-oxo-propenyl; R5 is chloro or fluoro: and R6 is hydrogen.

    摘要翻译： 公开组蛋白脱乙酰酶抑制剂（HDACI）和治疗有此需要的受试者的癌症的方法。 HDACIs包含式X化合物或其药学上可接受的盐。 在本发明的一个实施方案中，R 1是乙基; R2是2-苯基乙基; R3是氢; R4是氟; R5是（2E）-3-N-羟基氨基-3-氧代 - 丙烯基; R6为氢，或其盐。 在本发明的另一个实施方案中，R 1是乙基：R 2是2-苯基乙基; R3是氢; R4是（2E）-3-N-羟基氨基-3-氧代 - 丙烯基; R5是氯或氟：R6是氢。

    Multifunctional quinoline derivatives as anti-neurodegenerative agents
    8.
    发明授权
    Multifunctional quinoline derivatives as anti-neurodegenerative agents 有权
    多功能喹啉衍生物作为抗神经变性剂

    公开(公告)号：US09302992B2

    公开(公告)日：2016-04-05

    申请号：US13855311

    申请日：2013-04-02

    申请人： ANNJI PHARMACEUTICAL CO., LTD.

    发明人： Ji-Wang Chern ,  Chen-Wei Huang ,  Pei-Teh Chang ,  Rahul Subhash Talekar

    IPC分类号： C07D215/26 ,  C07D215/28

    CPC分类号： C07D215/26 ,  C07D215/28

    摘要： Novel quinoline derivatives are disclosed. Also disclosed are synthesis and use thereof for treating neurodegenerative diseases. In one aspect, the invention relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R1 is hydrogen, (C1-C8)alkyl, (C1-C8)alkylene(C3-C8)cycloalkyl, (C1-C8)haloalkyl, or (C1-C8)alkylene(C6-C20)aryl; R2 is hydrogen or halogen; R3 is hydrogen, halogen, (C1-C8)alkyl, or (C1-C8)alkoxy; R4 is hydrogen, halogen, (C1-C8)alkyl, (C1-C8)alkoxy, or (C1-C8)haloalkyl; R5 is hydrogen or (C1-C20)alkanol; R6 is hydrogen; and R7 is (C1-C20)alkanol, (C1-C8)alkylene (C3-C8)heterocyclyl(C1-C20)alkanol, (C1-C8)alkylene (C3-C8)heterocyclyl(C1-C20)alkyl, (C1-C8)alkylene(C1-C6)alkylamino(C1-C6)alkynyl, (C1-C8)alkyleneamino(C1-C20)alkanol, or (C1-C8)alkyleneamino(C1-C20)alkanol(C1-C8)alkylene substituted (C3-C20)heteroaryl; (II) or wherein: R1, R2, R3, R4 and R6 are each defined in (I) above; R5 is (C1-C20)alkanol; and R7 is hydrogen, (C1-C20)alkanol, (C1-C8)alkylene (C3-C8)heterocyclyl(C1-C20)alkanol, (C1-C8)alkylene (C3-C8)heterocyclyl(C1-C20)alkyl, (C1-C8)alkylene(C1-C6)alkylamino(C1-C6)alkynyl, (C1-C8)alkyleneamino(C1-C20)alkanol, or (C1-C8)alkyleneamino(C1-C20)alkanol(C1-C8)alkylene substituted (C3-C20)heteroaryl.

    摘要翻译： 公开了新的喹啉衍生物。 还公开了其治疗神经变性疾病的合成及其用途。 一方面，本发明涉及式（I）化合物或其药学上可接受的盐：（I）其中R1是氢，（C1-C8）烷基，（C1-C8）亚烷基（C3-C8）环烷基， （C 1 -C 8）卤代烷基或（C 1 -C 8）亚烷基（C 6 -C 20）芳基; R2是氢或卤素; R3是氢，卤素，（C1-C8）烷基或（C1-C8）烷氧基; R4是氢，卤素，（C1-C8）烷基，（C1-C8）烷氧基或（C1-C8）卤代烷基; R5是氢或（C1-C20）链烷醇; R6是氢; 和（C1-C20）烷基，（C1-C20）链烷醇，（C1-C20）链烷醇，（C1-C20） -C 1 -C 8）亚烷基氨基（C 1 -C 8）亚烷基氨基（C 1 -C 8）亚烷基氨基（C 1 -C 8）亚烷基 （C 3 -C 20）杂芳基; （II）或其中：R 1，R 2，R 3，R 4和R 6各自定义在上述（I）中; R5是（C1-C20）烷醇; 并且R 7是氢，（C 1 -C 20）烷醇，（C 1 -C 8）亚烷基（C 3 -C 8）杂环基（C 1 -C 20）链烷醇，（C 1 -C 8）亚烷基（C 3 -C 8） （C1-C8）亚烷基（C1-C8）亚烷基（C1-C6）烷基氨基（C1-C6）炔基，（C1-C8）亚烷基氨基（C1-C20）链烷醇或（C1-C8） 亚烷基取代的（C 3 -C 20）杂芳基。