1036389-86-2Relevant articles and documents
IRAK DEGRADERS AND USES THEREOF
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, (2021/01/23)
The present invention provides compounds, compositions thereof, and methods of using the same. The compounds include an IRAK binding moiety capable of binding to IRAK4 and a degradation inducing moiety (DIM). The DIM could be DTM a ligase binding moiety (LBM) or lysine mimetic. The compounds could be useful as IRAK protein kinase inhibitors and applied to IRAK mediated disorders.
ASK1 INHIBITOR COMPOUNDS AND USES THEREOF
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, (2018/11/02)
Described herein are compounds, including pharmaceutically acceptable salts, solvates, metabolites, prodrugs thereof, methods of making such compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat non
Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors
Wurtz, Nicholas R.,Parkhurst, Brandon L.,Jiang, Wen,DeLucca, Indawati,Zhang, Xiaojun,Ladziata, Vladimir,Cheney, Daniel L.,Bozarth, Jeffrey R.,Rendina, Alan R.,Wei, Anzhi,Luettgen, Joseph M.,Wu, Yiming,Wong, Pancras C.,Seiffert, Dietmar A.,Wexler, Ruth R.,Priestley, E. Scott
, p. 1077 - 1081 (2016/12/18)
Inhibitors of Factor VIIa (FVIIa), a serine protease in the clotting cascade, have shown strong antithrombotic efficacy in preclinical thrombosis models with minimal bleeding liabilities. Discovery of potent, orally active FVIIa inhibitors has been largely unsuccessful because known chemotypes have required a highly basic group in the S1 binding pocket for high affinity. A recently reported fragment screening effort resulted in the discovery of a neutral heterocycle, 7-chloro-3,4-dihydroisoquinolin-1(2H)-one, that binds in the S1 pocket of FVIIa and can be incorporated into a phenylglycine FVIIa inhibitor. Optimization of this P1 binding group led to the first series of neutral, permeable FVIIa inhibitors with low nanomolar potency.
Sulfo-imidazole-diketone and imidazole-diketone compound and applications thereof
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, (2017/01/02)
The invention discloses a sulfo-imidazole-diketone and imidazole-diketone compound and applications thereof. The invention provides the formula (I) compound (please see the specification) or pharmaceutical salt, solvate, prodrug, stereoisomer, tautomer and metabolite thereof, wherein X, Y, Z, R1, R2, R3 and A are defined in the formula. The invention further provides a preparing method for the compound and applications of the compound serving as an androgen receptor antagonist to treating diseases related to an androgen receptor, such as prostatic cancer, prostatic hyperplasia, acne, feather-loss disorder, hair hyperplasia, breast cancer and poor male sexual function.
A kind of diaryl hydanto?n derivatives, its preparation method, pharmaceutical composition and application
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Paragraph 0187, (2016/10/20)
Provided are a compound as represented by formula I, or pharmaceutically acceptable salt, solvate, precursor drug, stereoisomer, tautomer, polymorph or metabolite thereof, pharmaceutical composition containing same, and uses thereof in the preparation of drugs for treating androgen receptor related diseases.
BICYCLIC LACTAM FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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Page/Page column 137, (2008/12/07)
The present invention provides novel bicyclic lactams derivatives, and analogues thereof, of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, B, C, W, Y, Z1, Z2, Z3, Z4, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
MACROCYCLIC FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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Page/Page column 92, (2008/12/07)
The present invention relates generally to novel macrocycles of Formula (I) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z1, Z2, Z3, Z4, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.