- COMPOUNDS FOR THE TREATMENT OF KINASE-DEPENDENT DISORDERS
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The present invention relates to compounds that modulate cellular activities such as proliferation, differentiation, programmed cell death, migration, and chemoinvasion, by modulating protein kinase enzymatic activity, and compositions thereof, and methods of using such compounds.
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Paragraph 00287; 00289
(2020/08/13)
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- Indole compound as well as preparation method, pharmaceutical composition and application thereof
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The invention discloses an indole compound as well as a preparation method, a pharmaceutical composition and an application thereof. Specifically, the invention relates to an indole derivative as shown in a general formula I and a medicinal salt thereof, a preparation method of the indole derivative, a composition containing one or more compounds, and applications of the compounds in preparation of medicines for preventing and/or treating diseases related to IDO1 and/or TDO.
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Paragraph 1635; 1641-1643
(2019/12/02)
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- COMPOUNDS FOR THE TREATMENT OF KINASE-DEPENDENT DISORDERS
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Disclosed herein are compounds of Formula I'. Compounds of Formula I' inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase- dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
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Paragraph 000498; 000500
(2019/08/12)
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- Aurora Kinase Modulators and Method of Use
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The present invention relates to chemical compounds having a general formula I wherein A1-8, D′, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
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Paragraph 0508
(2014/11/27)
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- Mild and highly selective palladium-catalyzed monoarylation of ammonia enabled by the use of bulky biarylphosphine ligands and palladacycle precatalysts
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A method for the Pd-catalyzed arylation of ammonia with a wide range of aryl and heteroaryl halides, including challenging five-membered heterocyclic substrates, is described. Excellent selectivity for monoarylation of ammonia to primary arylamines was achieved under mild conditions or at rt by the use of bulky biarylphosphine ligands (L6, L7, and L4) as well as their corresponding aminobiphenyl palladacycle precatalysts (3a, 3b, and 3c). As this process requires neither the use of a glovebox nor high pressures of ammonia, it should be widely applicable.
- Cheung, Chi Wai,Surry, David S.,Buchwald, Stephen L.
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supporting information
p. 3734 - 3737
(2013/08/23)
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- Synthetic Uses of the Sequential Ring Positional Reactivity in Pyridin-3-ol and Derivatives
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A series of ring-substituted pyridin-3-ols has been prepared.The key to the scheme is the introduction of a bromo group to a specific ring position as a temporary blocking agent.As well as hydrogenolysis of the bromo function, nucleophilic displacement has also been investigated.
- Clark, Gary J.,Deady, Leslie W.
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p. 927 - 932
(2007/10/02)
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