62458-96-2Relevant articles and documents
New P2X3 receptor antagonists. Part 2: Identification and SAR of quinazolinones
Szántó, Gábor,Makó, Attila,Vágó, István,Hergert, Tamás,Bata, Imre,Farkas, Bence,Kolok, Sándor,Vastag, Mónika
, p. 3905 - 3912 (2016/08/01)
Numerous potent P2X3 antagonists have been discovered and the therapeutic potential of P2X3 antagonism already comprises proof-of-concept data obtained in clinical trials with the most advanced compound. We have lately reported the discovery and optimization of thia-triaza-tricycle compounds with potent P2X3 antagonistic properties. This Letter describes the SAR of a back-up series containing a 4-oxo-quinazoline central ring. The discovery of the highly potent compounds 51 is presented.
ANTI-ANGIOGENESIS COMPOUND, INTERMEDIATE AND USE THEREOF
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, (2016/04/10)
Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like.
Inhibitors of HIV-1 attachment: The discovery and structure-activity relationships of tetrahydroisoquinolines as replacements for the piperazine benzamide in the 3-glyoxylyl 6-azaindole pharmacophore
Swidorski, Jacob J.,Liu, Zheng,Yin, Zhiwei,Wang, Tao,Carini, David J.,Rahematpura, Sandhya,Zheng, Ming,Johnson, Kim,Zhang, Sharon,Lin, Pin-Fang,Parker, Dawn D.,Li, Wenying,Meanwell, Nicholas A.,Hamann, Lawrence G.,Regueiro-Ren, Alicia
supporting information, p. 160 - 167 (2015/12/18)
6,6-Fused ring systems including tetrahydroisoquinolines and tetrahydropyrido[3,4-d]pyrimidines have been explored as possible replacements for the piperazine benzamide portion of the HIV-1 attachment inhibitor BMS-663068. In initial studies, the tetrahydroisoquinoline compounds demonstrate sub-nanomolar activity in a HIV-1 pseudotype viral infection assay used as the initial screen for inhibitory activity. Analysis of SARs and approaches to optimization for an improved drug-like profile are examined herein.
ANTI-ANGIOGENESIS COMPOUND, INTERMEDIATE AND USE THEREOF
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, (2016/11/02)
Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like.
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists
Hawryluk, Natalie A.,Merit, Jeffrey E.,Lebsack, Alec D.,Branstetter, Bryan J.,Hack, Michael D.,Swanson, Nadia,Ao, Hong,Maher, Michael P.,Bhattacharya, Anindya,Wang, Qi,Freedman, Jamie M.,Scott, Brian P.,Wickenden, Alan D.,Chaplan, Sandra R.,Breitenbucher, J. Guy
scheme or table, p. 7137 - 7141 (2010/12/25)
Utilization of a tetrahydro-pyrimdoazepine core as a bioisosteric replacement for a piperazine-urea resulted in the discovery a novel series of potent antagonists of TRPV1. The tetrahydro-pyrimdoazepines have been identified as having good in vitro and in
DIKETOPIPERIDINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS
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Page/Page column 67, (2010/01/30)
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketopiperidine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.
HETEROBICYCLIC COMPOUNDS USEFUL AS KINASE INHIBITORS
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Page/Page column 45, (2008/12/08)
A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p3
TETRAHYDROPYRIDO[3,4-D]PYRIMIDINES AND RELATED ANALOGUES
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Page/Page column 39, (2008/06/13)
Tetrahydropyrido[3,4-d]pyrimidines and related analogues are provided, of the formula (I) in which variables are as described herein, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamin
Synthesis and SAR of p38α MAP kinase inhibitors based on heterobicyclic scaffolds
Murali Dhar,Wrobleski, Stephen T.,Lin, Shuqun,Furch, Joseph A.,Nirschl, David S.,Fan, Yi,Todderud, Gordon,Pitt, Sidney,Doweyko, Arthur M.,Sack, John S.,Mathur, Arvind,McKinnon, Murray,Barrish, Joel C.,Dodd, John H.,Schieven, Gary L.,Leftheris, Katerina
, p. 5019 - 5024 (2008/03/11)
The synthesis and structure-activity relationships (SAR) of p38α MAP kinase inhibitors based on heterobicyclic scaffolds are described. This effort led to the identification of compound (21) as a potent inhibitor of p38α MAP kinase with good cellular potency toward the inhibition of TNF-α production. X-ray co-crystallography of an oxalamide analog (24) bound to unphosphorylated p38α is also disclosed.
BICYCLOHETEROARYLAMINE COMPOUNDS AS ION CHANNEL LIGANDS AND USES THEREOF
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Page/Page column 58-59, (2010/02/12)
Amine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, includin