143151-03-5Relevant academic research and scientific papers
METHODS USING HDAC11 INHIBITORS
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Paragraph 0495-0496, (2018/05/16)
The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases.
FACTOR IXa INHIBITORS
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Page/Page column 96, (2014/07/08)
The present invention provides a compound of Formula (I) wherein A is a heterocycle ring system and B is a heterocycle ring system or aryl ring system, and pharmaceutical compositions comprising one or more of said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.
NOVEL PIPERAZINE ANALOGS AS BROAD-SPECTRUM INFLUENZA ANTIVIRALS
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Page/Page column 60, (2012/03/27)
A compound of Formula (I) is set forth, including pharmaceutically acceptable salts thereof, wherein Het is a 5 or 6-membered heterocycle with -N, -O, or -S adjacent to the -Ar substituent or adjacent to the point of attachment for the -Ar substituent; Ar
BENZIMIDAZOLE DERIVATIVES
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, (2008/06/13)
This invention relates to the compounds represented by a general formula [I]: ???[in which A1 and A2 represent optionally fluorine-substituted methine or the like; B represents halogen, cyano, lower alkyl or the like; D represents optionally substituted heterocyclic group or the like; and G represents C3-C20 aliphatic group such as alicyclic group]. These compounds inhibit nociceptin activities due to their high affinity to nociceptin receptor, and are useful as analgesic, antiobestic, corebral function improver, drugs for treatment of alzheimer's disease and dementia, remedies for schizophrenia and neurodegenerative diseases, antidepressant, remedies for diabetes insipidus, polyuria, hypotension and so on.
2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors
Mackman, Richard L.,Hui, Hon C.,Breitenbucher,Katz, Bradley A.,Luong, Christine,Martelli, Arnold,McGee, Danny,Radika, Kesavan,Sendzik, Martin,Spencer, Jeffrey R.,Sprengeler, Paul A.,Tario, James,Verner, Erik,Wang, Jing
, p. 2019 - 2022 (2007/10/03)
The development of potent and selective urokinase-type plasminogen activator (uPA) inhibitors based on the lead molecule 2-(2-hydroxy-3-ethoxyphenyl)-1H-benzimidazole-5-carboxamidine (3a) is described.
Compounds and compositions as anticoagulants
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, (2008/06/13)
The present invention relates to novel biheterocyclic derivatives which are factor Xa inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.
[1,2,4]triazolo[4,3-a]quinoxaline compounds
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, (2008/06/13)
The present invention relates to [1,2,4]triazolo[4,3-a quinoxaline derivatives of formula I STR1 wherein one of R 1 and R 2 is a 5- or 6-membered nitrogen-containing heterocyclic ring which is optionally substituted with one, two or three substituents, wherein each substituent is independently phenyl or C 1-6 -alkyl, or one of R 1 and R 2 is a fused ring system comprising a 5- or 6-membered nitrogen-containing heterocyclic ring and a benzene, pyridine, pyrimidine or pyrazine ring, wherein the fused ring system is optionally substituted with phenyl or C 1-6 -alkyl; and the other of R 1 and R 2 is hydrogen, C 1-6 -alkyl, C 1-6 -alkoxy, halogen, NO 2, NH 2, CN, CF 3, COC 1-6 -alkyl or SO 2 NR''R"", wherein R'' and R"" are independently hydrogen or C 1-6 -alkyl; and X is O or S; and pharmaceutically acceptable salts thereof. The compounds have affinity for the AMPA receptors and are antagonists in connection with this type of receptors which makes them useful in the treatment of CNS ailments, especially in the treatment of any of the numerous indications caused by hyperactivity of excitatory amino acids.
6-(1H-imidazol-1-yl)-7-nitro-2,3 (1H,4H)-quinoxalinedione hydrochloride (YM90K) and related compounds: Structure-activity relationships for the AMPA- type non-NMDA receptor
Ohmori,Sakamoto,Kubota,Shimizu-Sasamata,Okada,Kawasaki,Hidaka,Togami,Furuya,Murase
, p. 467 - 475 (2007/10/02)
A novel series of quinoxalinediones possessing imidazolyl and related heteroaromatic substituents was synthesized and evaluated for their activity to inhibit [3H]AMPA binding from rat whole brain. From the structure- activity relationships, it was found that the 1H-imidazol-1-yl moiety could function as a bioisostere for the cyano and nitro groups, and that 6-(1H- imidazol-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione (11) showed the most potent activity for the AMPA receptor. Compound 11 was evaluated for selectivity versus other excitatory amino acid receptors, and its action against AMPA at its receptor in the rat striatum was characterized. These data showed that compound 11 was a selective antagonist for the AMPA receptor with a K(i) value of 0.084 μM, being approximately equipotent with 2,3-dihydro-6-nitro- 7-sulfamoylbenzo(f)quinoxaline (3) (NBQX; K(i) = 0.060 μM). Compound 11 was also found to give protection against sound-induced seizure on DBA/2 mice at the minimum effective dose of 3 mg/kg ip (3; 10 mg/kg ip).
