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公开(公告)号：US20240158343A1
公开(公告)日：2024-05-16
申请号：US18417291
申请日：2024-01-19
发明人： Jiasheng LU , Jiamin GU , Xinyong LV , Guowei SONG , Dongdong WU , Daiqiang HU , Jun GU , Gang CHEN , Xiang JI , Xiuchun ZHANG , Jinchao AI , Xianqi KONG
IPC分类号： C07C309/14 , C07B59/00 , C07C309/15 , C07C309/59 , C07D233/61
CPC分类号： C07C309/14 , C07B59/001 , C07B59/002 , C07C309/15 , C07C309/59 , C07D233/61 , C07B2200/05
摘要： There are provided isotope-enriched compounds of Formula (I) and pharmaceutically acceptable salts or esters thereof, as well as pharmaceutical compositions thereof and methods of use thereof for prevention and treatment of amyloid-β related diseases, such as Alzheimer's disease.
R1R2X—CR2—CH2—CH2—SO3H (I)-
公开(公告)号：US20190185502A1
公开(公告)日：2019-06-20
申请号：US16222125
申请日：2018-12-17
发明人： Jiasheng LU , Jiamin GU , Xiang JI , Daiqiang HU , Xiuchun ZHANG , Xinyong LV , Jinchao AI , Dongdong WU , Xianqi KONG , Lin WANG , Dongqing ZHU , Xiaolin HE
CPC分类号： C07H5/06 , A61K9/0014 , A61K9/0053 , A61P19/02 , C07B2200/09 , C07H15/04 , C07H19/24
摘要： There are provided compounds of Formula (A) and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, used for the prevention or treatment in a mammal of joint and bone disorders such as arthritis and osteoporosis.
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公开(公告)号：US20240050577A1
公开(公告)日：2024-02-15
申请号：US18139692
申请日：2023-04-26
发明人： Jiasheng LV , Yao LIU , Xiangyang LI , Xianfeng LIN , Qisheng LIU , Yuanhong GU , Kang DU , Zhihong ZHANG , Mengchao SHI , Yuhua ZHANG , Jian GE , Tianlun ZHOU , Xiangsheng YE , Xianqi KONG , Dawei CHEN
CPC分类号： A61K47/55 , A61K47/60 , A61K47/545 , A61K45/06
摘要： The disclosure relates to bifunctional CDK-modulating compounds having the structure W-L-T, where W is a targeting group that binds specifically to a CDK protein, T is an E3-ligase binding group, and L is absent or is a bivalent linking group that connects W and T together via a covalent linkage. Compounds and pharmaceutical compositions thereof can promote degradation of one or more CDK protein in a cell and are thus useful for treating, inhibiting, and preventing CDK-associated diseases, disorders and conditions, including cancers.
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公开(公告)号：US20230321253A1
公开(公告)日：2023-10-12
申请号：US18119592
申请日：2023-03-09
发明人： Jiasheng LV , Xiangyang LI , Xiang JI , Yuhui CHEN , Yongyue CHEN , Chuanhao HUANG , Xingwu ZHU , Xiaolin HE , Jian GE , Tianlun ZHOU , Xianqi KONG , Dawei CHEN , Xiangsheng YE
CPC分类号： A61K47/545 , A61K45/06 , A61P35/00
摘要： The disclosure relates to bifunctional KRAS-G12D-modulating compounds having the structure W-L-T, where W is a targeting group that binds specifically to KRAS-G12D protein, T is an E3-ligase binding group, and L is absent or is a bivalent linking group that connects W and T together via a covalent linkage. Compounds and pharmaceutical compositions thereof can promote degradation of the KRAS-G12D protein in a cell and are thus useful for treating, inhibiting, and preventing KRAS-G12D-associated diseases, disorders and conditions, including cancers.
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公开(公告)号：US20210347731A1
公开(公告)日：2021-11-11
申请号：US17140450
申请日：2021-01-04
发明人： Jiasheng LU , Jiamin GU , Xinyong LV , Guowei SONG , Dongdong WU , Daiqiang HU , Jun GU , Gang CHEN , Xiang JI , Xiuchun ZHANG , Jinchao AI , Xianqi KONG
IPC分类号： C07C309/14 , C07C309/15 , C07B59/00 , C07C309/59 , C07D233/61
摘要： There are provided isotope-enriched compounds of Formula (I) and pharmaceutically acceptable salts or esters thereof, as well as pharmaceutical compositions thereof and methods of use thereof for prevention and treatment of amyloid-β related diseases, such as Alzheimer's disease. R1R2X—CR2—CH2—CH2—SO3H (I)
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公开(公告)号：US20200339615A1
公开(公告)日：2020-10-29
申请号：US16856603
申请日：2020-04-23
发明人： Jiasheng LU , Jiamin GU , Gang CHEN , Xiaolin ZHANG , Feng ZHOU , Xianqi KONG
IPC分类号： C07F9/6574 , C07F9/22 , C07D401/14 , C07D401/12
摘要： There are provided compounds of Formula I, and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, used for inhibition or modulation of the activity of cyclin dependent kinases (CDK) and/or glycogen synthase kinase-3 (GSK-3), for the treatment of disease states or conditions mediated by cyclin dependent kinases and/or glycogen synthase kinase-3, including cancers.
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公开(公告)号：US20240051982A1
公开(公告)日：2024-02-15
申请号：US18211796
申请日：2023-06-20
发明人： Xianqi KONG , Jiasheng LU , Jiamin GU , Xiang JI , Daiqiang HU , Xiuchun ZHANG , Xinyong LV , Jinchao AI , Dongdong WU , Lin WANG , Dongqing ZHU , Xiaolin HE
IPC分类号： C07H15/12 , A61P19/02 , A61K9/00 , C07H15/14 , C07H15/18 , C07H15/203 , C07H15/26 , C07H19/01 , C07H19/02 , C07J9/00
CPC分类号： C07H15/12 , A61P19/02 , A61K9/0014 , A61K9/0053 , C07H15/14 , C07H15/18 , C07H15/203 , C07H15/26 , C07H19/01 , C07H19/02 , C07J9/00 , C07B2200/05
摘要： There are provided compounds of Formula (A) and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, used for the prevention or treatment in a manual of joint and bone disorders such as arthritis and osteoporosis.
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公开(公告)号：US20240024346A1
公开(公告)日：2024-01-25
申请号：US18021709
申请日：2021-11-25
申请人： RISEN (SUZHOU) PHARMA TECH CO., LTD. , Jiasheng LU , Gang CHEN , Qiguo ZHANG , Xianqi KONG , Dawei CHEN , Chuanhao HUANG , Xingwu ZHU , Yuhua ZHANG
发明人： Jiasheng LU , Gang CHEN , Qiguo ZHANG , Xianqi KONG , Dawei CHEN , Chuanhao HUANG , Xingwu ZHU , Yuhua ZHANG
IPC分类号： A61K31/7076 , C07H19/20 , A61K45/06
CPC分类号： A61K31/7076 , A61K45/06 , C07H19/20
摘要： CD73 (also known as ecto-5′-nucleotidase) inhibitor compounds are provided, as well as compositions and uses thereof for treating or preventing CD73-associated or related diseases, disorders and conditions, including cancer- and immune-related disorders. CD73 inhibitor compounds include compounds having the structure set forth in Formula I′ and pharmaceutically acceptable esters or salts thereof.
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公开(公告)号：US20230019098A1
公开(公告)日：2023-01-19
申请号：US17844407
申请日：2022-06-20
发明人： Jiasheng LV , Haixiao SIYANG , Yijie YIN , Wantao GUO , Haiming LI , Dawei CHEN , Jiamin GU , Xianqi KONG , Jun PAN , Xinxin MA , Peiming SONG , Chun WU , Hui FENG , Sheng YAO
IPC分类号： A61K47/54 , C07C275/16
摘要： There are provided bivalent compounds and conjugates thereof, the conjugates comprising a bivalent compound, a targeting moiety, and a bioactive agent, as well as pharmaceutical compositions and methods of use of the conjugate for the treatment, inhibition, or prevention of diseases and disorders which are therapeutic targets of the bioactive agent.
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10.发明申请公开(公告)号：US20220202778A1
公开(公告)日：2022-06-30
申请号：US17523160
申请日：2021-11-10
发明人： Jiasheng LU , Jiamin GU , Xianqi KONG
IPC分类号： A61K31/417 , A61P9/10 , A61K31/131 , A61K31/16 , A61K31/165
摘要： There are provided methods for treating or preventing a cerebrovascular disease in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an isotope-enriched compound or a pharmaceutical composition thereof, where the isotope-enriched compound has the general Formula (I) or is a pharmaceutically acceptable salt or ester thereof: R1R2X—CR2—CH2—CH2—SO3H (I).
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