107017-74-3Relevant articles and documents
Design, synthesis and pharmacological evaluation of new acyl sulfonamides as potent and selective Bcl-2 inhibitors
Liu, Xiaohua,Zhang, Yu,Huang, Wenjing,Tan, Wenfu,Zhang, Ao
, p. 443 - 454 (2018)
The antiapoptotic protein Bcl-2, overexpressed in many tumor cells, is an attractive target for potential small molecule anticancer drug discovery. Herein, we report a different structural modification approach on ABT-263 by merging the piperazinyl-phenyl fragment into a bicyclic framework leading to a series of novel analogues, among which tetrahydroisoquinoline 13 was nearly equally potent against Bcl-2 as ABT-263. Further SAR in the P4-interaction pocket affored the difluoroazetidine substituted analogue 55, which retained good Bcl-2 activity with improved Bcl-2/Bcl-xL selectivity.
SUBSTITUTED TRIAZINONES AS THYROID HORMONE RECEPTOR AGONISTS
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Paragraph 00421; 00424, (2021/07/24)
The application relates to a compound of Formula (I') or (I), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of thyroid hormone receptors, a pharmaceutical composition comprising a compound of Formula (I') or (I), and a method of treating or preventing a disease or disorder regulated by thyroid hormone.
ANTIVIRAL PYRIDOPYRAZINEDIONE COMPOUNDS
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Paragraph 0450; 0454; 0731; 0734, (2020/04/09)
The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.
PYRAZOLYL SUBSTITUTED TETRAHYDROPYRANYLSULFONES
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Page/Page column 40, (2017/08/01)
The invention relates to pyrazolyl substituted tetrahydropyranylsulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
METALLO-BETA-LACTAMASE INHIBITORS
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Page/Page column 186; 187, (2017/04/04)
The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORS
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Paragraph 0238; 0277; 0278, (2016/03/13)
The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R1, G, T, Y1, Y2, Y3, and Y4 are as defined herein.
IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORS
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Paragraph 0182-0183; 0218; 0221-0222, (2015/02/25)
The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R1, G, T, Y1, Y2, Y3, and Y4 are as defined herein.
Synthesis of spirocyclopropanated analogues of imidacloprid and thiacloprid
Brackmann, Farina,Yufit, Dmitrii S.,Howard, Judith A. K.,Es-Sayed, Mazen,De Meijere, Armin
, p. 600 - 609 (2007/10/03)
tert-Butyl N-[1-(hydroxymethyl)cyclopropyl]carbamate (8) was converted into spirocyclopropanated analogues 14-CP and 14-CT of the insecticide Thiacloprid (2) in six simple steps with overall yields of 24 % each, along with their regioisomers 13-CP and 13-CT in overall yields of 17 and 15 %, respectively. The spirocyclopropanated analogues 27-CP and 27-CT of the insecticide Imidacloprid (1) were prepared from 8 in five steps in an overall yield of 10 % each, along with their regioisomers 20-CP and 20-CT in an overall yield of 8 and 7 %, respectively. The key step in all preparations was a cocyclization of an appropiately protected (1-aminocyclopropyl)methyl derivative with S,S-dimethyl cyanodithioimino-carbonate (11) or nitroguanidine (22). The structures of several final products and by-products were verified by X-ray crystal structure analyses.