- 1, 5-disubstituted indole derivative with leukotreines A4 hydrolase inhibiting effect and application
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The invention relates to a 1, 5-disubstituted indole derivative with leukotreines A4 hydrolase inhibiting effect. The 1, 5-disubstituted indole derivative has the function of inhibiting leukotreines A4 hydrolase. The 1, 5-disubstituted indole derivative i
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Paragraph 0059-0061
(2019/10/01)
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- Synthesis of Complex Phenols Enabled by a Rationally Designed Hydroxide Surrogate
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The conversion of aryl halides to phenols under mild reaction conditions is a longstanding and formidable challenge in organic chemistry. Herein, we report the rational design of a broadly applicable Pd-catalyzed method to prepare phenols with benzaldehyde oxime as a hydroxide surrogate. These reactions occur under mildly basic conditions and enable the late-stage hydroxylation of several functionally-dense drug-like aryl halides.
- Fier, Patrick S.,Maloney, Kevin M.
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supporting information
p. 4478 - 4482
(2017/04/13)
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- Reagent Design and Ligand Evolution for the Development of a Mild Copper-Catalyzed Hydroxylation Reaction
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Parallel synthesis and mass-directed purification of a modular ligand library, high-throughput experimentation, and rational ligand evolution have led to a novel copper catalyst for the synthesis of phenols with a traceless hydroxide surrogate. The mild reaction conditions reported here enable the late-stage synthesis of numerous complex, druglike phenols.
- Fier, Patrick S.,Maloney, Kevin M.
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supporting information
p. 3033 - 3036
(2017/06/07)
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- TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS
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The invention relates to a compound of formula I: (I) or a pharmaceutically acceptable salt thereof and/or stereoisomers thereof. The compounds of the invention are useful in therapy.
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Page/Page column 58
(2017/03/14)
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- Ligand compound of alpha7 nicotinic acetylcholine receptor and application of ligand compound
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The embodiment of the invention provides a ligand compound of an alpha7 nicotinic acetylcholine receptor, the ligand compound has one of the following general formulas: wherein (1) X and R1 are shown in the description, and R7 is halogen; (2) R2 is hydrogen, and R3 is halogen or amino; or R3 is hydrogen, and R2 is halogen or amino; (3) R6 is hydrogen, and R4 and R5 are synthesized into a compound shown in the description; or R4 is hydrogen, and R5 and R6 are synthesized into a compound shown in the description; R8 is halogen; and (4) Y is nitrogen or carbon, Z is shown in the description, and R9 and R10 are respectively halogens. The provided ligand compound is an excellent ligand compound of the alpha7 nicotinic acetylcholine receptor. After being chemically marked radioactively, the provided ligand compound of the alpha7 nicotinic acetylcholine receptor can serve as a PET photographic developer.
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Paragraph 0093; 0094; 0095
(2017/10/09)
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- Chemoselective N-acylation of indoles and oxazolidinones with carbonylazoles
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Unique reactivity: In the presence of more reactive amine and alcohol functional groups and of carboxylic acids, the chemoselective N-acylation of indoles (see scheme) and oxazolidinones is achieved by taking advantage of the unique reactivity of carbonylazole acylating agents with catalytic amounts of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU). Copyright
- Heller, Stephen T.,Schultz, Erica E.,Sarpong, Richmond
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supporting information; experimental part
p. 8304 - 8308
(2012/09/08)
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- Nucleoside Aryl Phosphoramidates for the Treatment of RNA-Dependent RNA Viral Infection
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The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are
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Page/Page column 21
(2010/09/18)
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- JAK INHIBITOR
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A JAK inhibitor comprising, as an active ingredient, a nitrogen-containing heterocyclic compound represented by formula (I) {wherein W represents a nitrogen atom or -CH-; X represents -C (=O) - or -CHR4- (wherein R4 represents a hydrogen atom, or the like); R1 represents the formula described below [wherein Q1 represents-CR8-(wherein R8 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like); Q2 represents -NR15- (wherein R15 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like); and R5 and R6 may be the same or different and each represents a hydrogen atom, halogen, carboxy, substituted or unsubstituted lower alkyl, or the like], or the like; and R2 and R3 may be the same or different and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like} or a pharmaceutically acceptable salt thereof.
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Page/Page column 87
(2009/10/21)
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- ANTI-VIRAL COMPOUNDS
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Compounds effective in inhibiting replication of Hepatitis C virus ("HCV") or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
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Page/Page column 127
(2010/11/27)
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- INDOLYL-THIENO`3,4-B!PYRAZIN-3-ONE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
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This invention relates to a compound of Formula (I): (I) and its use in treating hyper-proliferative disorders and diseases associated with angiogenesis.
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Page/Page column 57
(2010/02/11)
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- INDOLYL PYRAZINONE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
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This invention relates to a compound of Formula I (I)and its use in treating hyper-proliferative disorders and diseases associated with angiogenesis.
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