- FGFR4 Inhibitor. Compositions and their use in pharmaceutical preparations
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The invention provides 3 inhibitor which takes 4 - 4 dihydropyrimidine [5 - d,2] pyrimidine - (1H) FGFR4 ketone as a mother nucleus and has a covalent structure. The examples give 9 specific compounds and kinase inhibitory activity testing of these 9 compounds, wherein LX08 for FGFR4 kinase inhibitory activity is only 7 nm, lower than FIIN - 2 of the active control, and potential application prospects. In addition, by subjecting the synthesized compound to MALDI-TOF mass spectrometry, we found that compounds of LX01, LX05, LX06, LX07, LX08 are covalently bound to FGFR4 of Cys552, cannot covalently bind FGFR4 of Cys477, and LX09 are FGFR4 inhibitors which can be covalently bound to the two cysteines Cys552 and Cys477 in FGFR4.
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- DEGRADERS OF FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2)
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The present invention relates to bispecific compounds, compositions, and methods for treating diseases or conditions characterized or mediated by aberrant fibroblast growth factor receptor 2 (FGFR2) activity.
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- Synthetic route of generic FGFR covalent inhibitor PRN1371
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The invention relates to a synthetic route of a generic FGFR covalent inhibitor PRN1371, and belongs to the field of medicinal chemistry. The synthetic route steps of the PRN1371 comprise 11 steps, purification of a product can be achieved through simple operation of various intermediates in the aftertreatment process, the problems that the product is difficult to separate, the purification operation yield is low and the like are solved, and industrial production is facilitated. The invention aims to provide a synthetic route of the FGFR irreversible covalent inhibitor PRN1371, and the methodhas the advantages of few synthesis steps, simple operation, high yield, reduction of the production cost, and provision of a new synthesis idea for the industrial production of PRN1371.
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- NEW ANTIBACTERIAL COMPOUNDS
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The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials.
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- ANTIBACTERIAL COMPOUNDS HAVING BROAD SPECTRUM OF ACTIVITY
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The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials.
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Page/Page column 44
(2016/07/05)
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- CINNAMIC ACID AMIDE DERIVATIVE
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The present invention provides a cinnamic acid amide derivative having an excellent analgesic action. The cinnamic acid amide derivative of the present invention is a compound showing excellent analgesic actions to not only a nociceptive pain model animal but also a neuropathic pain model animal, which is very useful as an agent for treating various pain diseases showing acute or chronic pains or neuropathic pains.
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Paragraph 0028; 0047
(2015/11/24)
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- [4-(Benzo[B]Thiophen-2-Yl) Pyrimidin-2-Yl]-Amine Derivatives As Ikk-Beta Inhibitors For The Treatment Of Cancer And Inflammatory Diseases
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The present invention provides compounds of Formula I: useful in the treatment of cancer and inflammatory diseases.
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Page/Page column 4-5
(2009/01/20)
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- MEDICINAL USE OF RECEPTOR LIGANDS
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Compounds of formula (I) are ligands of the melanin concentrating hormone-1 receptor (MCH-1 R), useful in the treatment of diseases responsive to modulation of melanin concentrating hormone (MCH) activity, for example feeding disorders and diseases for which obesity is a risk factor (I): wherein ring B is selected from specific substituted phenyl or benz-fused 5-membered N-containing heterocycles defined in the specification; R, is attached to a ring carbon of ring B, and represents hydrogen, F, Cl, or -OCH3; X is =CH- or =N-; L, is -CH2- or -CH2CH2- ; L2 is a bond, -CH2- or -CO-; R2 is H or C,-C3 alkyl, or -N(R2) L,- is selected from specific cyclic amino linker radicals as defined in the specification; ring A is selected from specific N- containing heterocyclic rings as defined in the specification.
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Page/Page column 46
(2008/06/13)
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- PYRIMIDINES WITH TIE2 (TEK) ACTIVITY
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The invention relates to a compound of the Formula (I). or salt thereof wherein R1, R2, R3, R4, R5, R6, A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm-blooded animal. The invention also relates to processes for the preparation of said compounds.
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Page/Page column 138
(2010/02/12)
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- Alkylamine derivatives of dihydropyridine NPY antagonists
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A series of non-peptidergic antagonists of NPY have been synthesized and are comprises of amino and piperazine derivatives of 4-phenyl-1,4-dihydropyridines of Formula 1. where X is CH or N As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
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