755752-82-0Relevant articles and documents
Indazole ester compound and pharmaceutical application thereof
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Paragraph 0088-0091, (2021/10/20)
The invention provides an indazole ester compound and a pharmaceutical application thereof. Specifically provided is a compound represented by a formula I, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, or an optical isomer thereof, or an isotope substitution form thereof. The compound can be used for effectively inhibiting the activity of SARS-CoV-2Mpro, and can be used for preparing an SARS-CoV-2Mpro inhibitor. The compound provided by the invention has a good application prospect in preparation of drugs for resisting novel coronavirus and drugs for preventing and/or treating novel coronavirus pneumonia.
Azacycle diketone compound and preparation method thereof (by machine translation)
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Paragraph 0673-0678, (2020/09/12)
The invention provides a azacyclodiketone compound which is characterized by being a compound represented by the following structure. The compound has inhibitory activity on cap-dependent endonuclease. (by machine translation)
Preparation method of niraparib tosilate monohydrate
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Paragraph 0050; 0051, (2017/07/21)
The invention discloses a preparation method of a compound 2-[4-((3S)-3-piperidyl)phenyl]-2H-indazole-7-formamide tosilate monohydrate. The method includes: carrying out Ulman reaction on 1H-indazole-7-methyl formate and (S)-3-(4-halogenophenyl)piperidine-1-tert-butyl formate to prepare 2-[4-((3S)-3-piperidyl)phenyl]-2H-indazole-7-methyl formate, then under the conditions of ammonia gas and p-toluenesulfonic acid, preparing 2-[4-((3S)-3-piperidyl)phenyl]-2H-indazole-7-formamide tosilate monohydrate. The invention aims to avoid the disadvantages of existing methods, shortens the preparation route, and provides the preparation method of the 2-[4-((3S)-3-piperidyl)phenyl]-2H-indazole-7-formamide tosilate monohydrate with high chiral purity, and the method has the characteristics of mild reaction and easy operation.
A novel synthetic method for preparing an anticancer medicine Niraparib
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Page/Page column 9, (2017/08/02)
A novel synthetic method for preparing an anticancer medicine Niraparib is disclosed. The method includes subjecting an initial raw material that is 3-formyl-2-nitrobenzoic acid to 2-site nitro reduction, diazotization, reduction, cyclization, substitution, isomer resolution, amidation, and BOC removing to obtain the optically pure Niraparib the purity of which is 97.51% or above. The method is simple, convenient, high in yield, low in loss, easy to operate, low in equipment requirement and suitable for industrial production.
Asymmetric Synthesis of Fused Polycyclic Indazoles through Aminocatalyzed Aza-Michael Addition/Intramolecular Cyclization
Giardinetti, Maxime,Marrot, Jér?me,Moreau, Xavier,Coeffard, Vincent,Greck, Christine
, p. 6855 - 6861 (2016/08/16)
The first example of an asymmetric aminocatalyzed aza-Michael addition of 1H-indazole derivatives to α,β-unsaturated aldehydes is described. The iminium/enamine cascade process lies at the heart of our strategy, leading to enantioenriched fused polycyclic indazole architectures. Variations on both the α,β-unsaturated aldehydes and the indazole-7-carbaldehyde heterocycles were studied in order to broaden the scope of the transformation in synthetically interesting directions. The fused polycyclic indazoles exhibit fluorescence properties and can undergo synthetic transformations.
Synthesis and pharmacological evaluation of N-benzyl substituted 4-bromo-2,5-dimethoxyphenethylamines as 5-HT2A/2C partial agonists
Hansen, Martin,Jacobsen, Stine Engesgaard,Plunkett, Shane,Liebscher, Gudrun Eckhard,McCorvy, John D.,Br?uner-Osborne, Hans,Kristensen, Jesper Langgaard
supporting information, p. 3933 - 3937 (2015/01/30)
N-Benzyl substitution of phenethylamine 5-HT2A receptor agonists has dramatic effects on binding affinity, receptor selectivity and agonist activity. In this paper we examine how affinity for the 5-HT2A/2C receptors are influenced by N-benzyl substitution of 4-bromo-2,5-dimethoxyphenethylamine derivatives. Special attention is given to the 2′ and 3′-position of the N-benzyl as such compounds are known to be very potent. We found that substitutions in these positions are generally well tolerated. The 2′-position was further examined using a range of substituents to probe the hydrogen bonding requirements for optimal affinity and selectivity, and it was found that small changes in the ligands in this area had a profound effect on their affinities. Furthermore, two ligands that lack a 2′-benzyl substituent were also found to have high affinity contradicting previous held notions. Several high-affinity ligands were identified and assayed for functional activity at the 5-HT2A and 5-HT2C receptor, and they were generally found to be less efficacious agonists than previously reported N-benzyl phenethylamines.
SPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS
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Page/Page column 27-28, (2008/12/06)
The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating mammals suffering from the condition of being overweight.
INDOLE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
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Page/Page column 29, (2008/06/13)
The invention is directed to indole amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.
INDAZOLES, BENZOTHIAZOLES, AND BENZOISOTHIAZOLES, AND PREPARATION AND USES THEREOF
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Page 64, (2008/06/13)
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.