- SULFONYLUREA DERIVATIVES AND USES THEREOF
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The present disclosure relates to compounds of Formula (I) and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
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Paragraph 01277-01278
(2020/12/30)
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- 2-substituted parazoleamino-4-substituted amino-5-pyrimidine formamide compound, composition and application thereof
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The invention relates to a series of new compounds as a JAK inhibitor, as well as compositions and applications thereof, and particularly provides a series of compounds (I) that have a strong JAK inhibiting activity, or stereisomers, geometrical isomers, tautomers, pharmaceutically acceptable salts, prodrugs, metabolites, isotope derivatives, and solvates, as well as medicine compositions comprising such compounds. The invention also discloses applications of the compounds or the medicine compositions in preparation of a medicine, which is used for treatment of autoimmune diseases or cancer.
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Paragraph 0091; 0098; 0100
(2019/04/10)
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- SULPHONYL UREA DERIVATIVES AS NLRP3 INFLAMMASOME MODULATORS
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The present disclosure relates to compounds of Formula (I): (I) and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
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Paragraph 0964
(2019/07/13)
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- Pyrrolopyrimidine compound, pharmaceutical composition containing thereof, and preparation method and applications
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The invention relates to a pyrrolopyrimidine compound represented by formula I, a pharmaceutical composition containing thereof, and a preparation method and applications in preventing or treating Weel protein kinase related diseases.
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Paragraph 0303-0304; 0308-0310
(2019/11/29)
-
- Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines
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Computational and experimental studies were applied to the discovery of a series of novel vascular endothelial growth factor receptor 2 (VEGFR-2) inhibitors. Eight compounds exhibited nanomolar IC50 values against VEGFR-2, and compounds 6, 19,
- Zhang, Yanmin,Chen, Yadong,Zhang, Danfeng,Wang, Lu,Lu, Tao,Jiao, Yu
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p. 140 - 157
(2018/02/10)
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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 0255-0256
(2018/08/12)
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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 00293
(2017/01/23)
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- COMPOUND INHIBITING ACTIVITIES OF BTK AND/OR JAK3 KINASES
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The present invention relates to a compound inhibiting the activities of Bruton's tyrosine kinase (BTK) and/or Janus kinase 3 (JAK3), a pharmaceutical composition of the compound, pharmaceutical applications of same, a method for using the compound in inhibiting the activities of BTK and/or JAK3, and a method for using the compound in treatment and/or prevention of BTK- and/or JAK3-mediated diseases or disorders in mammals (especially human). The compound is as represented by structural formula (I).
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Paragraph 0298; 0299
(2016/08/29)
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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.
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Paragraph 00510; 00512
(2015/04/15)
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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 0301; 0303
(2015/12/07)
-
- Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives
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The c-jun N-terminal kinase 3 (JNK3) is expressed primarily in the brain. Numerous reports have shown that inhibition of JNK3 is a promising strategy for treatment of neurodegeneration. The optimization of aminopyrazole-based JNK3 inhibitors with improved potency, isoform selectivity, and pharmacological properties by structure-activity relationship (SAR) studies utilizing biochemical and cell-based assays, and structure-based drug design is reported. These inhibitors had high selectivity over JNK1 and p38α, minimal cytotoxicity, potent inhibition of 6-OHDA-induced mitochondrial membrane potential dissipation and ROS generation, and good drug metabolism and pharmacokinetic (DMPK) properties for iv dosing. 26n was profiled against 464 kinases and was found to be highly selective hitting only seven kinases with >80% inhibition at 10 μM. Moreover, 26n showed good solubility, good brain penetration, and good DMPK properties. Finally, the crystal structure of 26k in complex with JNK3 was solved at 1.8 ? to explore the binding mode of aminopyrazole based JNK3 inhibitors.
- Zheng, Ke,Iqbal, Sarah,Hernandez, Pamela,Park, Hajeung,Lograsso, Philip V.,Feng, Yangbo
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supporting information
p. 10013 - 10030
(2015/02/19)
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- RADIOLABELED COMPOUNDS AND THEIR USE AS RADIOTRACERS FOR QUANTITATIVE IMAGING OF PHOSPHODIESTERASE (PDE10A) IN MAMMALS
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The present invention provides radiolabeled compounds useful as radiotracers for quantitative imaging of PDE10A in mammals. The compound of the present invention is represented by the formula (I): wherein each symbols are as defined in the specification.
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Paragraph 0416
(2013/03/26)
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- HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS JAK INHIBITORS
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The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
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Page/Page column 70
(2011/05/06)
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- PYRIMIDINE INHIBITORS OF KINASES
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The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A1, A2, A3, A4, X and Y are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora and KDR.
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- IMIDAZOPYRAZINE SYK INHIBITORS
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Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
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Page/Page column 12; 13
(2010/06/22)
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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 42
(2009/04/24)
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- A practical, two-step synthesis of 1-alkyl-4-aminopyrazoles
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A novel synthesis of N1 alkyl-substituted pyrazoles with a free amino group at the C4 position is described. Commercially available 4-nitropyrazole was found to readily undergo Mitsunobu reactions with primary and secondary alcohols. Subsequent reduction of the nitro group via hydrogenation affords 1-alkyl-4-aminopyrazoles, which are valuable intermediates in the synthesis of pharmaceutically active compounds.
- Zabierek, Anna A.,Konrad, Kaleen M.,Haidle, Andrew M.
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p. 2996 - 2998
(2008/09/20)
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- QUINOLINE DERIVATIVES
-
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 112
(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 102
(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 99
(2008/06/13)
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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 115
(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 123-124
(2008/06/13)
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