- METHODS OF TREATING CANCER
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The present disclosure relates to methods of treating cancer in a patient using a combination of an inhibitor of an immune checkpoint protein and an indole compound or its phosphate derivative.
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Paragraph 00206
(2020/06/10)
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- INDOLE COMPOUNDS AND THEIR USE
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The present disclosure relates to indole compounds and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer.
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Paragraph 00191; 00194
(2019/06/05)
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- Novel indole derivative and medicine containing the same (by machine translation)
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[A] formation of Amyloid fibrils can be compounds, including therapeutic or prophylactic agent for neurodegenerative disease Amyloid fibrils formation inhibitor compound and of. (I) or its pharmaceutically acceptable compound represented by the formula [a] or a salt or solvate thereof includes the, Amyloid fibrils formation inhibitor. [R1 And R2 Each independently is H, an alkyl group, a cyano group or the like; R3 And R4 Each independently is H, or an alkyl group; R3 And R4 The, joint may form a ring; Ar1 And Ar2 The substituted or unsubstituted heteroaryl group are independently substituted/unsubstituted aryl groups /; X and Y are each independently a single bond, - (=O) - C etc., Z is O or CH2 ; N is an integer of 1 - 3][Drawing] no (by machine translation)
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Paragraph 0168; 0170
(2018/06/30)
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- Lithium tert-butoxide-mediated carboxylation reactions of unprotected indoles and pyrroles with carbon dioxide
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Unprotected indoles and pyrroles were found to undergo base-mediated carboxylation reactions under ambient pressure of carbon dioxide. It was found that this transition metal-free carboxylation reaction proceeded smoothly with the use of a large excess of LiOtBu.
- Yoo, Woo-Jin,Nguyen, Thanh V. Q.,Guiteras Capdevila, Montse,Kobayashi, Shu
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p. 1196 - 1204
(2015/04/21)
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- N -[6-(4-Butanoyl-5-methyl-1 H -pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1 H -indole-3-carboxamide (SAR216471), a Novel Intravenous and Oral, Reversible, and Directly Acting P2Y12 Antagonist
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In the search of a potential backup for clopidogrel, we have initiated a HTS campaign designed to identify novel reversible P2Y12 antagonists. Starting from a hit with low micromolar binding activity, we report here the main steps of the optimization process leading to the identification of the preclinical candidate SAR216471. It is a potent, highly selective, and reversible P2Y12 receptor antagonist and by far the most potent inhibitor of ADP-induced platelet aggregation among the P2Y12 antagonists described in the literature. SAR216471 displays potent in vivo antiplatelet and antithrombotic activities and has the potential to differentiate from other antiplatelet agents.
- Boldron, Christophe,Besse, Angélina,Bordes, Marie-Fran?oise,Tissandié, Stéphanie,Yvon, Xavier,Gau, Benjamin,Badorc, Alain,Rousseaux, Tristan,Barré, Guillaume,Meneyrol, Jér?me,Zech, Gernot,Nazare, Marc,Fossey, Valérie,Pflieger, Anne-Marie,Bonnet-Lignon, Sandrine,Millet, Laurence,Briot, Christophe,Dol, Frédérique,Hérault, Jean-Pascal,Savi, Pierre,Lassalle, Gilbert,Delesque, Nathalie,Herbert, Jean-Marc,Bono, Fran?oise
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supporting information
p. 7293 - 7316
(2015/01/08)
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- An investigation into the substituent effect of halogen atoms on the crystal structures of indole-3-carboxylic acid (ICA)
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An investigation into the substituent effect of halogen atoms (F, Cl, Br) on the crystal structure of indole-3-carboxylic acid (ICA) was prepared in this work. The investigation was done through the aspect of crystal structure, intermolecular interactions and π...π stacking motifs with the assistance of infrared spectra, elemental analyses, NMR spectra, differential scanning calorimetry (DSC), thermogravimetric analyses (TGA) and hot stage microscopy (HSM) measurements. The results revealed that the different kinds of halogen atoms and the different substituted positions have a significant effect on the crystal structures, molecular π...π stacking motifs and the kinds of intermolecular interactions. We further correlated the melting points of the ICAs with the H-H, O-H and X-H (X = F, Cl, Br) interactions, and found a positive correlation between them.
- Luo, Yang-Hui,Sun, Bai-Wang
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p. 7490 - 7497
(2013/09/24)
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- NOVEL BIS-INDOLIC DERIVATIVES, A PROCESS FOR PREPARING THE SAME AND THEIR USES AS A DRUG
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The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.
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Paragraph 0178; 0179
(2013/03/26)
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- BIS-INDOLIC DERIVATIVES, A PROCESS FOR PREPARING THE SAME AND THEIR USES AS A DRUG
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The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.
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Page/Page column 26; 32; 33
(2013/03/26)
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- Base-mediated carboxylation of unprotected indole derivatives with carbon dioxide
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A simple and straightforward method for the preparation of indole-3-carboxylic acids was discovered through the direct carboxylation of indoles with atmospheric pressure of carbon dioxide (CO2) under basic conditions. The key for the reaction was found to be the use of a large excess of LiOtBu as a base to suppress the undesired decarboxylation side reaction.
- Yoo, Woo-Jin,Capdevila, Montse Guiteras,Du, Xiangwei,Kobayashi, Shu
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supporting information
p. 5326 - 5329,4
(2020/09/02)
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- PYRIMIDINE DERIVATIVES AS PI3K INHIBITORS
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Thienopyrimidines of formula (Ia) or (Ib): wherein R1, R2, R3, are as defined in the claims.
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Page/Page column 73-74
(2008/06/13)
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