- Discovery of highly potent and selective EGFRT790M/L858R TKIs against NSCLC based on molecular dynamic simulation
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Epidermal growth factor receptor (EGFR) is the most attractive target for drug research in non-small cell lung cancer (NSCLC). There have been three generation drugs developed to treat of NSCLC. The third-generation EGFR tyrosine kinase inhibitors (TKIs)
- Yang, Tingting,Zhang, Wenjuan,Cao, Shengjie,Sun, Shiyang,Cai, Xu,Xu, Lei,Li, Pengyun,Zheng, Zhibing,Li, Song
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- Design and synthesis of anti-tumor compounds containing ferulic acid-pyrazole skeleton
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The invention discloses design and a preparation method of an anti-tumor compound containing a ferulic acid-pyrazole skeleton. The structure of the anti-tumor compound is shown as a formula in the specification.
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Paragraph 0024-0025; 0027; 0031-0032; 0034
(2021/04/28)
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- FGFR Inhibitor compounds and uses thereof
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The invention relates to FGFR inhibitor compounds and uses thereof. , The application discloses a compound as shown in a formula (I). A compound, or an optical isomer, a geometric isomer, a tautomer or isomer mixture thereof, or a pharmaceutically acceptable salt thereof, or a prodrug thereof, or a metabolite thereof. The application further relates to the application of the compound in medicine.
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Paragraph 0474; 0477; 0479-0481
(2021/11/21)
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- Design and synthesis of novel pyrimidine analogs as highly selective, non-covalent BTK inhibitors
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BTK is a promising target for the treatment of multiple diseases such as B cell malignances, asthma, and rheumatoid arthritis. Here, we report the discovery of a series of novel pyrimidine analogs as potent, highly selective, non-covalent inhibitors of BTK. Compound 25d demonstrated higher affinity to an unactivated conformation of BTK that resulted in an excellent kinase selectivity. Compound 25d showed a good oral bioavailability in mice, and significantly inhibits the PCA reaction in mice.
- Kawahata, Wataru,Asami, Tokiko,Irie, Takayuki,Sawa, Masaaki
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p. 145 - 151
(2017/12/06)
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- FUSED RING PYRIMIDINE COMPOUND, INTERMEDIATE, AND PREPARATION METHOD, COMPOSITION AND USE THEREOF
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Disclosed area fused ring pyrimidine compound, and an intermediate, a preparation method, a composition and a use thereof. The fused ring pyrimidine compound is a compound as shown in formula I, a tautomer, an enantiomer, a diastereoisomer, a pharmaceutically acceptable salt, a metabolite, a metabolic precursor or a prodrug thereof, wherein the above-mentioned compound is used for the preparation of a medicine for preventing, remitting or treating one or more of immune system diseases, autoimmune diseases, cell proliferative diseases, allergic disorders and cardiovascular diseases, and the compound has a strong inhibitory effect on the Janues kinase, FGFR kinase, FLT3 kinase and Src family kinase.
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Paragraph 0243-0244
(2018/08/12)
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- Design, synthesis, and biological evaluation of pyrazole derivatives containing acetamide bond as potential BRAFV600E inhibitors
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With the increasingly acquired resistance, relapse and side effects of known marketed BRAFV600E inhibitors, it's significant to design the more effective and novel drugs. In this study, a series of novel pyrazole derivatives containing acetamid
- Wang, Chen-Ru,Wang, Ze-Feng,Shi, Lu,Wang, Zhong-Chang,Zhu, Hai-Liang
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supporting information
p. 2382 - 2390
(2018/06/25)
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- Identification and Biological Evaluation of Novel Type II B-RafV600E Inhibitors
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The mitogen-activated protein kinase (MAPK) pathway plays a vital role in signal transduction networks. Severe diseases may be triggered if it is disturbed by mutated components, especially the kinase B-RafV600E. New inhibitors of the kinase ar
- Wang, Peng-Fei,Wang, Ze-Feng,Qiu, Han-Yue,Huang, Yue,Hu, Hui-Min,Wang, Zhong-Chang,Zhu, Hai-Liang
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p. 2558 - 2566
(2018/11/23)
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- IRAK INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for inhibiting one or more interleukin-1 receptor-associated kinases ("IRAK").
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Paragraph 00289
(2017/01/23)
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- MACROCYCLIC FACTOR XIA INHIBITORS CONDENSED WITH HETEROCYCLES
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The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
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Page/Page column 82; 93; 94
(2015/09/23)
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- Five-And-Six-Membered Heterocyclic Compound, And Preparation Method, Pharmaceutical Composition And Use Thereof
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A five-and-six-membered heterocyclic compound as represented by general formula I, pharmaceutically acceptable salt, metabolite, metabolic precursors or drug precursors thereof, preparation method, pharmaceutical composition, and use thereof; the five-and-six-membered heterocyclic compound has activity as a Janus kinase (JAK) inhibitor, and can be used to prepare drugs for treating diseases caused by the abnormal activity of kinase, such as cell proliferation diseases like cancer.
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Paragraph 0296; 0297
(2015/12/07)
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- NOVEL PYRIMIDINE AND PYRIDINE COMPOUNDS AND USAGE THEREOF
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Provided are novel pyrimidine and pyridine compounds of formula (I) or a pharmaceutical acceptable salt thereof, pharmaceutical compositions containing them, a process for preparing them, and their use in therapy of a disease responsive to inhibition of F
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Page/Page column 31; 32
(2014/09/29)
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- NOVEL PYRIMIDINE AND PYRIDINE COMPOUNDS AND THEIR USAGE
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The present invention relates to novel pyrimidine and pyridine compounds of formula (I) or a pharmaceutical acceptable salt thereof, wherein R1, R2, R3, R4, R5, X, Y and G are as defined in the description, to pharmaceutical compositions containing them, a process for preparing them, and their use in therapy of a disease responsive to inhibition of FGFR, for example, cancer.
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Page/Page column 32; 33
(2014/09/29)
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- SUBSTITUTED PYRROLOPYRIMIDINE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
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Provided herein are Pyrrolopyrimidine Compounds having the following structure: wherein R1, R2, R3, and L are as defined herein, compositions comprising an effective amount of a Pyrrolopyrimidine Compound, and methods for treating or preventing breast cancer, more particularly triple negative breast cancer, comprising administering an effective amount of such Pyrrolopyrimidine Compounds to a subject in need thereof.
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Paragraph 0388
(2014/07/23)
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- 8-FLUOROPHTHALAZIN-1(2H)-ONE COMPOUNDS
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8-Fluorophthalazin-1(2h)-one compounds of Formula II where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula II for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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Paragraph 0354; 0355
(2013/05/21)
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- PYRIDINONES/PYRAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF
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Pyridone and pyrazinone compounds of Formula (I) including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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Page/Page column 84
(2012/03/26)
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- QUINOLINE DERIVATIVES
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The invention concerns quinoline derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
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Page/Page column 36
(2009/04/24)
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- QUINOLINE DERIVATIVES
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The invention concerns quinoline derivatives of Formula (I): or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
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Page/Page column 109
(2008/06/13)
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- QUINOLINE DERIVATIVES FOR TREATING CANCER
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The invention concerns quinoline derivatives of Formula (I) or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
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Page/Page column 95
(2008/06/13)
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- QUINAZOLINE DERIVATIVES
-
The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
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Page/Page column 104-105
(2008/06/13)
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- NAPHTHYRIDINE DERIVATIVES
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The invention concerns naphthyridine derivatives of Formula (Ia) or (Ib) or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, G1, G2, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders or disease states associated with angiogenesis and/or vascular permeability.
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Page/Page column 143
(2010/11/28)
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- NAPHTHYRIDINE DERIVATIVES AS ANTI-CANCER AGENTS
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The invention concerns naphthyridine derivatives of Formula (I): or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, G1, G2, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders or disease states associated with angiogenesis and/or vascular permeability.
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Page/Page column 94
(2010/11/28)
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- QUINAZOLINE DERIVATIVES
-
The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
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Page/Page column 123
(2008/06/13)
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- ARYL-AMINO SUBSTITUTED PYRROLOPYRIMIDINE MULTI-KINASE INHIBITING COMPOUNDS
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Compounds represented by Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mekl, PDK-1, GSK3?, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2
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Page/Page column 123
(2008/06/13)
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