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91.发明公开公开(公告)号：US20240261391A1
公开(公告)日：2024-08-08
申请号：US18565013
申请日：2022-05-30
Inventor： Xinxin ZHANG , Likun GONG , Jin REN , Guangyi JIN , Wei HUANG , Yong GAN , Jianhua SUN , Tingting LIU , Yiru LONG , Yunqiu MIAO , Qiuping QIN , Feng TANG , Pan YU , Linmiao GUO
IPC: A61K39/215 , A61K39/00 , A61K47/22 , C12N7/00
CPC classification number: A61K39/215 , A61K47/22 , C12N7/00 , A61K2039/55566 , C12N2770/20034
Abstract: The present invention relates to a novel coronavirus vaccine using a TLR7 agonist conjugated peptide as an antigen and an emulsion as an adjuvant. An antigen polypeptide of the conjugated peptide is a polypeptide derived from an S protein of SARS-COV-2, and the adjuvant is an oil-in-water nanoemulsion containing squalene. The conjugated peptide nanoemulsion vaccine preparation of the present invention is thermally stable, and can induce a high level of protective humoral immune response in a cynomolgus monkey, and the neutralizing antibody titer of antiserum after immunization of cynomolgus monkey is high, such that invasion of wild-type strain and mutant novel coronavirus can be blocked. The vaccine of the present invention has a nearly complete protection effect on the upper and lower respiratory tracts of the cynomolgus monkey in a cynomolgus monkey SARS-COV-2 challenge test. The nanoemulsion vaccine of the present invention is fast and convenient to prepare, and can realize large-scale production in a short term for coping with the novel coronavirus outbreak.
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公开(公告)号：US20240189443A1
公开(公告)日：2024-06-13
申请号：US18550346
申请日：2022-03-15
Inventor： Likun GONG , Xiaolu YU , Yiru LONG , Jianhua SUN , Yongliang TONG , Tingting LIU
CPC classification number: A61K47/6849 , A61J1/05 , A61K47/6803 , A61P35/00 , C07K16/2827 , C07K2317/24 , C07K2317/31 , C07K2317/569 , C07K2319/30
Abstract: Disclosed in the present invention are a use of a combination of an anti-PD-L1 nanobody and a TLR7 small molecule agonist in anti-tumor treatment, and a PD-L1 and TLR7 double-targeting nanobody coupling drug, a preparation method therefor, and a use thereof. Specifically, disclosed in the present invention are a use and solution of a combination of an anti-PD-L1 nanobody and a derived protein thereof as well as a TLR7 small molecule agonist and a derived compound thereof in anti-tumor treatment. Meanwhile, disclosed in the present invention are design, preparation, and identification solutions for a novel PD-L1 and TLR7 double-targeting-nanobody drug conjugate and a derived molecule thereof, and an effect of the novel PD-L1 and TLR7 double-targeting nanobody drug conjugate in anti-tumor treatment. The PD-L1 and TLR7 double-targeting nanobody drug conjugate of the present invention can yield a significant antineoplastic efficacy in various transplantation tumor models.
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公开(公告)号：US20240033244A1
公开(公告)日：2024-02-01
申请号：US18004623
申请日：2021-07-08
Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES , HANGZHOU LEADING EDGE PHARMACEUTICAL LTD. , SHANGHAI KANGQIAN BIOTECHNOLOGY LIMITED
Inventor： Cheng LUO , Meng XU , Shijie CHEN , Yilin LI , Yantao CHEN , Hualiang JIANG , Kaixian CHEN , Zhanpeng JIANG
IPC: A61K31/343 , A61K35/15 , A61K39/395 , A61K31/216 , A61P35/00
CPC classification number: A61K31/343 , A61K35/15 , A61K39/3955 , A61K31/216 , A61P35/00
Abstract: A YTH N6-Methyladenosine RNA Binding Protein 1 (YTHDF1) attenuating agent, with a compound, and when bound to YTHDF1, the compound binds to amino acid residues 372-392, 479-494 and 526-535 of SEQ ID NO: 1. A modified antigen presenting cell (mAPC), with the mAPC being treated with a YTHDF1 attenuating agent. A composition, with a YTHDF1 attenuating agent, a mAPC treated with the YTHDF1 attenuating agent, and optionally a pharmaceutically acceptable carrier. A method for attenuating an activity of YTHDF1, by administering an effective amount of a YTHDF1 attenuating agent. A method for determining whether or not a candidate agent is a YTHDF1 attenuating agent, by contacting the candidate agent with a YTHDF1 mutant. A method for treating a disease, disorder or condition associated with an expression of an antigen in a subject in need thereof.
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94.发明授权公开(公告)号：US11834432B2
公开(公告)日：2023-12-05
申请号：US15998927
申请日：2017-02-17
Inventor： Ao Zhang , Meiyu Geng , Li Xing , Jing Ai , Zilan Song , Xia Peng , Wangting Gu , Jian Ding
IPC: C07D213/75 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , A61P35/00 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4433 , A61K31/4409 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/5377 , A61K31/4545 , A61K31/44
CPC classification number: C07D401/12 , A61P35/00 , C07D213/75 , C07D403/12 , C07D405/12 , C07D413/14 , C07D417/14
Abstract: Provided in the present invention are a substituted amino six-membered nitric heterocyclic ring compound and a preparation and use thereof. In particular, provided in the present invention is a compound as shown by general formula (I) below, wherein the definition of each group is as described in the description. The compound of the present invention has an excellent tyrosine kinase inhibitory activity, and can thus be used to prepare a series of medicines for treating diseases related to tyrosine kinase inhibitory activity.
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公开(公告)号：US20230382871A1
公开(公告)日：2023-11-30
申请号：US18027759
申请日：2021-09-22
Inventor： Jian DING , Wenhu DUAN , Hua XIE , Meiyu GENG , Caixia WANG , Zhengsheng ZHAN , Na GAO , Yang ZHANG
IPC: C07D231/56 , A61P35/00 , C07K16/28
CPC classification number: C07D231/56 , A61P35/00 , C07K16/2818 , C07K16/2827 , A61K2039/505
Abstract: Provided is the use of a CSF1R kinase inhibitor compound or a pharmaceutically acceptable salt thereof in the preparation of drugs for treating diseases related to the CSF1R kinase signal transduction pathway or drugs for regulating immunization.
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Patent Agency Ranking
公开(公告)号：US20230357244A1
公开(公告)日：2023-11-09
申请号：US18029359
申请日：2021-09-28
Inventor： Huaqiang XU , Jia LI , Jingjing SHI , Yi ZANG , Dandan SUN , Mingliang LIU , Rongrong XIE , Erli YOU , Lixin GAO , Qian TAN
IPC: C07D471/08
CPC classification number: C07D471/08
Abstract: A strong FXR small-molecule agonist, and a preparation method therefor and use thereof, the structure of the agonist being represented by formula (I), are provided. In the formula, each substituent is as defined in the description and the claims. The compound provided has the advantages of high FXR agonist activity, simple synthesis, easily available raw materials and the like, and can be used for preparing medicines for treating FXR related diseases.
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公开(公告)号：US20230338510A1
公开(公告)日：2023-10-26
申请号：US18010522
申请日：2021-06-11
Inventor： Likun GONG , Jin REN , Qiuping QIN , Weiliang ZHU , Yiru LONG , Zhijian XU , Jianhua SUN , Tingting LIU , Guangyi JIN , Jianping ZUO , Wei HUANG
IPC: A61P31/14 , A61K39/215 , A61K39/00
CPC classification number: A61K39/215 , A61K39/4611 , A61K39/4613 , A61K39/4614 , A61K39/4615 , A61K39/464838 , A61P31/14 , A61K2039/575 , A61K2039/70
Abstract: Provided are a tandem epitope polypeptide vaccine for novel coronavirus and use thereof. Specifically, a vaccine polypeptide for novel coronavirus pneumonia is provided on the basis of analysis and study of the RBD sequence and structural information of the S protein of SARS-CoV-2. Said vaccine polypeptide comprises the following elements connected in series: a generic Th epitope sequence, a B cell epitope sequence and a T cell epitope sequence. The B cell epitope and the T cell epitope have an amino acid sequence from the RBM region of the S protein of SARS-CoV-2. Provided are a vaccine composition containing said vaccine polypeptide and use thereof. Experiments show that the vaccine polypeptide of the present invention can enable cynomolgus monkeys to initiate strong cellular and humoral immunity, and to generate neutralizing antibodies that block the binding of RBD and ACE2, and can be used for preventing and treating novel coronavirus pneumonia.
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98.发明公开公开(公告)号：US20230312584A1
公开(公告)日：2023-10-05
申请号：US18033673
申请日：2021-10-21
Applicant: VIGONVITA LIFE SCIENCES CO., LTD. , SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES , WUHAN INSTITUTE OF VIROLOGY, CHINESE ACADEMY OF SCIENCES
Inventor： Jingshan SHEN , Yuanchao XIE , Leike ZHANG , Gengfu XIAO , Zhen WANG , Hualiang JIANG , Huaqiang XU , Tianwen HU , Guanghui TIAN
IPC: C07D487/04
CPC classification number: C07D487/04 , C07B2200/13
Abstract: A salt of nucleoside analog, and crystal form, pharmaceutical composition and use thereof. The salt of nucleoside analog has a structure shown in formula I, wherein X is hydrogen or deuterium; Y is an acid, n is 0.5 to 2, or n is 1. When X is hydrogen or deuterium, Y is hydrogen bromide, and n is 1, the salt of the nucleoside analog exists in the form of a crystal with crystal form I or crystal form A or exists in an amorphous form.
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99.发明公开公开(公告)号：US20230295144A1
公开(公告)日：2023-09-21
申请号：US18100782
申请日：2023-01-24
Inventor： Tao Liu , Jia Li , Yongzhou Hu , Yubo Zhou , Xiaowu Dong , Anhui Gao , Pinrao Song , Peipei Wang , Lexian Tong , Xiaobei Hu , Mingbo Su
IPC: C07D413/14 , A61P35/02 , A61P35/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
CPC classification number: C07D413/14 , A61P35/00 , A61P35/02 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
Abstract: The present invention provides a 2-polysubstituted aromatic ring-pyrimidine derivative and an optical isomer thereof, or a pharmaceutically acceptable salt or solvate thereof, the compound, and an optical isomer thereof or a pharmaceutically thereof acceptable salts or solvates can be used in the preparation of anti-tumor drugs. The invention designs and synthesizes a series of novel small molecule Chk1 inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained by structure-based virtual screening as a lead compound, and carries out Chk1 kinase inhibitory activity test. The experiment confirmed that said compounds possess potent anticancer activity, Chk1 kinase inhibitory activity, and are promising Chk1 inhibitors, and can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal. The 2-polysubstituted aromatic ring-pyrimidine derivatives provided by the present invention has the structure of the formula I:
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公开(公告)号：US20230241204A1
公开(公告)日：2023-08-03
申请号：US18008826
申请日：2020-12-01
Inventor： Likun GONG , Jin REN , Guangyi JIN , Wei HUANG , Qiuping QIN , Yiru LONG , Jianhua SUN , Tingting LIU , Feng TANG , Peng ZHU
IPC: A61K39/215 , A61P31/14
CPC classification number: A61K39/215 , A61P31/14 , A61K2039/60
Abstract: Disclosed are a polypeptide vaccine coupled with a TLR7 agonist for novel coronavirus and the use thereof. Specifically, the present invention provides a vaccine polypeptide for novel coronavirus pneumonia based on the basis of the analytical study of the RBD sequence and structural information of the S protein of SARS-CoV-2, wherein the vaccine polypeptide has the following structural formula: Z-(J-U)n, where in the formula, Z, J, U, n, etc. are as defined in the description. Also provided in the present invention are a vaccine composition containing the vaccine polypeptide and the use thereof.
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