220464-68-6Relevant academic research and scientific papers
Piperidine compound and preparation method and medical application thereof
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Paragraph 0384-0395; 0400; 0384-0395; 0401, (2021/04/07)
The invention discloses a piperidine compound shown as a formula (I) and a preparation method and medical application thereof, and particularly relates to a piperidine USP7 inhibitor compound or pharmaceutically acceptable salt or ester or solvate thereof and a preparation method and application of the piperidine USP7 inhibitor compound or pharmaceutically acceptable salt or ester or solvate thereof. The compound provided by the invention can inhibit the activity of USP7 enzyme, has very good selectivity and druggability, and can be used for preparing medicines for preventing or treating tumor diseases or virus infectious diseases.
Identification and structure–activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus
Deng, Xiaoyan,Jiang, Neng,Jiang, Weizhe,Li, Qing,Meng, Liuwei,Xing, Junhao,Xu, Yanjun
, (2021/08/17)
Our previously reported carboxyl-containing DPP-4 inhibitors were highly potent but were poorly bioavailable. Esters of the carboxyl analogs exhibited a significant DPP-4 potency loss albeit with enhanced oral absorption. Herein, we described identificati
Optimization of the benzamide fragment targeting the S2′ site leads to potent dipeptidyl peptidase-IV inhibitors
Deng, Xiaoyan,Wang, Na,Meng, Liuwei,Zhou, Siru,Huang, Junli,Xing, Junhao,He, Linhong,Jiang, Weizhe,Li, Qing
, (2019/10/28)
Our recently successful identification of benzoic acid-based DPP-4 inhibitors spurs the further quest for in-depth structure-activity relationships (SAR) study in S2′ site DPP-4. Thus novel benzamide fragments were designed to target the S
COMPOUNDS TARGETING PROTEINS, COMPOSITIONS, METHODS, AND USES THEREOF
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Paragraph 0235, (2018/10/19)
The present invention provides modulators of protein function, to restore protein homeostasis, including GSPT1 activity. The invention provides methods of modulating protein-mediated diseases, such as GSPT1-mediated diseases, disorders, conditions, or responses. Compositions are also provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions, such as GSPT1-mediated diseases, disorders, and conditions, including cancer and astrogliosis.
HETEROARYL COMPOUNDS AND USES THEREOF
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Paragraph 00776, (2014/09/29)
The present invention relates to compounds useful as inhibitors of protein kinases, containing a cysteine residue in the ATP binding site. The invention further provides for pharmaceutically acceptable compositions comprising therapeutically effective amounts of one or more of the protein kinase inhibitor compounds and methods of using said compositions in the treatment of cancers and carcinomas.
5-ALKYLOXY-INDOLIN-2-ONE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPY
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Page/Page column 10, (2010/04/23)
The present invention relates to derivatives of 5-alkyloxy-indolin-2-one, their method of production and their therapeutic applications. These novel derivatives have affinity and selectivity for the V2 receptors of vasopressin (“V2 receptors”) and can therefore constitute active principles of pharmaceutical compositions.
Design, synthesis and identification of novel colchicine-derived immunosuppressant
Chang, Dong-Jo,Yoon, Eun-Young,Lee, Geon-Bong,Kim, Soon-Ok,Kim, Wan-Joo,Kim, Young-Myeong,Jung, Jong-Wha,An, Hongchan,Suh, Young-Ger
scheme or table, p. 4416 - 4420 (2010/04/05)
Synthesis and biological evaluation of various colchicine analogues through the mixed-lymphocyte reaction (MLR), lymphoproliferation, and inhibitory effects on the inflammatory genes are described. In addition, a new series of immunosuppressive agents developed on the structural basis of colchicine, as well as their structure-activity relationships is reported. The most potent analogue 20a exhibited an excellent immunosuppressive activity on in vivo skin-allograft model, which is comparable to that of cyclosporin A.
PYRROLIDINEANILINES
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Page/Page column 119, (2010/11/27)
The present invention relates to a compotind represented by the following formula I or a pharmaceutically acceptable salt thereof; wherein R1, R2, and y are defined herein. The present invention further relates to compositions that include the compound of the present invention as well as a method of treating a patient from endometreosis or uterine fibroids.
QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS
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Page/Page column 81, (2008/06/13)
The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
QUINOXALINES AS B RAF INHIBITORS
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Page/Page column 62, (2010/11/08)
The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
