- 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 1108-1113
(2019/12/02)
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- AURORA AND FLT3 KINASES MODULATORS
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The invention provides a compound having the formula (1): and salts thereof; wherein: R1 is hydrogen or C1-2 alkyl; and R2, R3 and R4 are the same or different and each is selected from hydrogen, C1-2 alkyl, fluorine, chlorine, C1-2 alkoxy and trifluoromethyl, provided that no more than two of R2, R3 and R4 are other than hydrogen. Also provided are pharmaceutical compositions containing the compounds and their use in medicine, and in particular in the treatment of cancer.
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Paragraph 0173; 0174
(2015/02/18)
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- AURORA AND FLT3 KINASES MODULATORS
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The invention provides a compound having the formula (1) useful as modulator of the activity of Aurora kinases and FLT3 kinases: and salts thereof; wherein: R1 is hydrogen or C1-2 alkyl; and R2, R3 and R4 are the same or different and each is selected from hydrogen, C1-2 alkyl, fluorine, chlorine, C1-2 alkoxy and trifluoromethyl, provided that no more than two of R2, R3 and R4 are other than hydrogen. Also provided are pharmaceutical compositions containing the compounds and their use in medicine, and in particular in the treatment of cancer
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Page/Page column 39
(2013/08/28)
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- Ep1 receptor ligands
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The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation,
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Paragraph 0151
(2013/03/28)
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- EP1 RECEPTOR LIGANDS
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The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
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Page/Page column 74
(2013/03/28)
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- SERINE/THREONINE PAK1 INHIBITORS
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Compounds having the formula I wherein A, Z, R1a, R1b, R2, R3, R4, R5, R6, R7, R9, R10, Ra, Rb and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
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Page/Page column 135
(2013/03/26)
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- SELECTIVE KINASE INHIBITORS
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Provided are pyrimidine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
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Paragraph 0526; 0527
(2013/06/06)
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- In search of simplicity and flexibility: A rational access to twelve fluoroindolecarboxylic acids
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All twelve indolecarboxylic acids 1-12 carrying both a fluorine substituent and a carboxy group at the benzo ring have been prepared either directly from the corresponding fluoroindoles 13-16 or from the chlorinated derivatives 22, 23 and 25 by hydrogen/metal permutation ("metalation"), or from the bromo- or iodofluoroindoles 17-20 and 26, 27, 29 and 30 by halogen/metal permutation, the organometallic intermediate being each time trapped with carbon dioxide. In most, though not all cases, the nitrogen atom in the five-membered ring had to be protected by a trialkylsilyl group. Some of the bromo- or iodofluoroindoles (26 and 27) were successfully subjected to a basicity gradient-driven selective migration of the heavy halogen. An unexpected finding on the way to the target compounds were the rigorously site-selective metalation of the 5-fluoro-N-(trialkylsilyl)indole (14b; exclusive deprotonation of the 4-position). The fluoroindoles 13-16, although previously known, were accessed more conveniently from suitably substituted nitrobenzenes using the Bartoli or the Leimgruber-Batcho method. A new and very attractive indole synthesis was elaborated consisting of the ortho-lithiation of an N-acyl-protected aniline followed by ortho-formylation, Wittig chloromethylenation and base-catalyzed cyclization accompanied by dehydrochlorination. These five consecutive steps can be contracted to a convenient one-pot protocol. Wiley-VCH Verlag GmbH & Co. KGaA, 2006.
- Schlosser, Manfred,Ginanneschi, Assunta,Leroux, Frederic
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p. 2956 - 2969
(2007/10/03)
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