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公开(公告)号：US20240122921A1
公开(公告)日：2024-04-18
申请号：US18473796
申请日：2023-09-25
发明人： Yifan ZHAI , Zi CHEN , Qian JIANG , Xiaojun HUANG , Wei LIU , Dajun YANG
IPC分类号： A61K31/496 , A61P35/00
CPC分类号： A61K31/496 , A61P35/00
摘要： The present invention relates to methods for treating patients with cancer, including patients with hematological malignancy, wherein the method comprises administering to the patient a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are as defined herein.
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2.发明公开公开(公告)号：US20240016747A1
公开(公告)日：2024-01-18
申请号：US18038628
申请日：2021-11-25
发明人： Yanqiong LIN , Hualiang XU , Feng XU , Chen WU , Hongtao GUO , Xiaoling HE
IPC分类号： A61K9/28 , A61K31/635 , A61K47/32 , A61K47/38 , A61K47/10 , A61K47/26 , A61K9/14 , A61K47/02
CPC分类号： A61K9/2866 , A61K31/635 , A61K47/32 , A61K47/38 , A61K47/10 , A61K47/26 , A61K9/146 , A61K47/02
摘要： The invention discloses a solid dispersion, a pharmaceutical preparation, a preparation method and an application thereof. The solid dispersion of the invention comprises carriers and active constituents, which is a compound as shown in formula (I) and/or a pharmaceutically acceptable salt thereof; The carrier is “homopolymer and copolymer of N-vinyl lactam” and/or pH-dependent cellulose derivatives. The preparation of the invention comprises the solid dispersion, fillers and disintegrating agents. The solid dispersion of the invention has good dissolution and significantly improves the solubility of effective constituents. The preparation can effectively improve the bioavailability of Bcl-2 inhibitor, has good dissolution and stability, and can improve the safety of a medication.
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3.发明公开公开(公告)号：US20230159524A1
公开(公告)日：2023-05-25
申请号：US17921257
申请日：2021-07-01
发明人： Jianfeng WEN , Jianyong CHEN , Yunlong ZHOU , Jianpeng FENG , Ming GUO , Tianzhu WU , Minmin CAI , Yu JING , Lingling JIAO
IPC分类号： C07D471/04 , C07D295/073 , C07D319/12 , C07C63/10 , C07C47/457 , B01J31/24
CPC分类号： C07D471/04 , C07D295/073 , C07D319/12 , C07C63/10 , C07C47/457 , B01J31/24 , C07C2602/50
摘要： Disclosed is a method for synthesizing N-(phenylsulfonyl)benzamide compound and intermediate thereof. The method comprises a method for synthesizing a compound 1, comprising conducting a Buchwald-Hartwig coupling reaction as shown below with compound A and compound B in a solvent and in the presence of a base and a palladium catalyst to obtain the compound 1; wherein R is C1-C8 alkyl. The present disclosure synthesizes three intermediate compounds required by the target compound and their preparation methods for the first time. Using the method disclosed in the present disclosure to synthesize the target compound 3 has the advantages of high yield, good purity, easy-to-obtain reaction raw materials, suitable for industrial production.
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4.发明申请公开(公告)号：US20230029259A1
公开(公告)日：2023-01-26
申请号：US17781699
申请日：2020-12-02
发明人： Yifan Zhai , Dajun Yang , Douglas Dong Fang , Qiang Li
IPC分类号： C07D519/00 , A61P35/00
摘要： A pharmaceutical composition comprising: a) an effective amount of an Inhibitors of Apoptosis Proteins (IAP) inhibitor, wherein the IAP inhibitor is represented by formula (I): or a pharmaceutically acceptable salt thereof, the definitions of each variable are provided herein; b) an effective amount of a second inhibitor, wherein the second inhibitor is a poly ADP ribose polymerase (PARP) inhibitor or a mitogen-activated protein kinase kinase (MEK) inhibitor; and a pharmaceutically acceptable carrier or diluent.
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公开(公告)号：US20220332701A1
公开(公告)日：2022-10-20
申请号：US17262533
申请日：2020-07-29
发明人： Yunlong Zhou , Guozhi TANG , Chao LI , Fang LIU , Yu JING , Renlin WANG , Lingling JIAO
IPC分类号： C07D403/04 , C07D413/04 , C07D401/04 , A61P35/00
摘要： The present disclosure provides compounds represented by Formula I: wherein R1, R2a, R2b, R2c, R2d, R3, R4a, R4b, A, L, X, Y, Z, and are as defined in the specification, and the pharmaceutically acceptable salts and solvates thereof. Compounds of Formula I are BCR-ABL inhibitors. BCR-ABL inhibitors are useful for the treatment of cancer and other diseases.
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公开(公告)号：US20200297704A1
公开(公告)日：2020-09-24
申请号：US16896059
申请日：2020-06-08
发明人： Dajun Yang , Yifan Zhai , Douglas Dong Fang , Qiuqiong Tang
IPC分类号： A61K31/437 , A61K45/06 , A61K31/407 , A61K31/519 , A61P35/00
摘要： Disclosed is a pharmaceutical composition comprising (i) a compound of formula (I) or a pharmaceutically acceptable salt thereof; (ii) a CDK inhibitor or a pharmaceutically acceptable salt thereof, for the prevention and/or treatment of a disease mediated by MDM2 and/or CDK activity.
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公开(公告)号：US20200222366A1
公开(公告)日：2020-07-16
申请号：US16828558
申请日：2020-03-24
发明人： Dajun Yang , Yifan Zhai , Douglas Dong Fang , Saijie Zhu
IPC分类号： A61K31/407 , A61P19/02 , A61K9/00
摘要： The present invention relates to a compound for treating or preventing osteoarthritis. The compound relieves the joint pain, inhibits and attenuates the development of post-traumatic osteoarthritis in mouse model. The present invention also provides a pharmaceutical composition comprising the compound for treating or preventing osteoarthritis. The present invention further provides a method for treating or preventing osteoarthritis by administrating to the patient in need thereof with the pharmaceutical composition.
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公开(公告)号：US20240316051A1
公开(公告)日：2024-09-26
申请号：US18551910
申请日：2022-04-19
发明人： Yifan ZHAI , Dajun YANG , Douglas Dong FANG , Saijie ZHU , Hengrui ZHU , Ran TAO
IPC分类号： A61K31/519 , A61K31/404 , A61K31/496 , A61K31/506 , A61P35/00
CPC分类号： A61K31/519 , A61K31/404 , A61K31/496 , A61K31/506 , A61P35/00
摘要： Provided herein are the pharmaceutical combination comprising an embryonic ectoderm development (EED) inhibitor and one or more anticancer reagents, and the use of the combination in the treatment of a disease. Provided also is a pharmaceutical composition or a kit comprising the combination.
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公开(公告)号：US11872237B2
公开(公告)日：2024-01-16
申请号：US16758272
申请日：2019-12-12
发明人： Ming Guo , Yanqiong Lin , Zhenzhong Shao , Pengfei Cao
IPC分类号： A61K31/675 , A61K9/19 , A61K47/02 , A61K47/10 , A61K47/26
CPC分类号： A61K31/675 , A61K9/19 , A61K47/02 , A61K47/10 , A61K47/26
摘要： The present invention relates to a pharmaceutical composition comprising a sulfonamide as an inhibitor of Bcl-2/Bcl-xL, especially compound (3R)-1-(3-(4-(4-(4-(3-(2-(4-chlorophenyl)-1-isopropyl-4-methylsulfonyl-5-methyl-1H-pyrrol-3-yl)-5-fluorophenyl)piperazin-1-yl)-phenylaminosulfonyl)-2-trifluoromethyl sulfonyl-anilino)-4-phenylthio-butyl)-piperidine-4-carboxylic acid 3-phosphonopropyl ester or a pharmaceutically acceptable salt thereof and suitable excipients, preferably a pharmaceutical composition in the form of a lyophilized powder. The invention also relates to a method for preparing the pharmaceutical composition.
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公开(公告)号：US20230404998A1
公开(公告)日：2023-12-21
申请号：US18298800
申请日：2023-04-11
申请人： ASCENTAGE PHARMA (SUZHOU) CO., LTD. , ASCENTAGE PHARMA GROUP CORP LIMITED , GUANGZHOU HEALTHQUEST PHARMA CO., LTD.
发明人： Yifan ZHAI , Dajun YANG , Guangfeng WANG , Miaozhen QIU , Fan LUO
IPC分类号： A61K31/496 , A61K31/4439 , A61K39/395 , A61P35/02
CPC分类号： A61K31/496 , A61K31/4439 , A61K39/3955 , A61P35/02 , A61K2039/505
摘要： The present invention relates to one or more combination treatments of cancer patients with a compound of formula (I),
and an allosteric inhibitor or an immune checkpoint molecule, wherein R1 and R2 are as described herein.
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