77747-69-4Relevant academic research and scientific papers
The role of polycyclic frameworks in modulating P2X7 receptor function
Callis, Timothy B.,Reekie, Tristan A.,O'Brien-Brown, James,Wong, Erick C.N.,Werry, Eryn L.,Elias, Nabiha,Jorgensen, William T.,Tsanaktsidis, John,Rendina, Louis M.,Kassiou, Michael
, p. 1207 - 1219 (2017/11/24)
Herein we describe our recent attempts to target the P2X7 receptor for potential treatment of neurological disorders. This work focusses on different polycycles including carborane, adamantane or cubane, joined by either a cyanoguanidine or an amide linker to phenyl or isoquinoline moieties. We have demonstrated the superiority of the adamantyl moiety over other polycycles in terms of synthetic accessibility and biological (cellular) activity. We have also shown that an amide or cyanoguanidine linker can greatly alter the biological activity of compounds. This SAR study provides important insights into the types of functionality required to target the P2X7 receptor.
Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
-
Page/Page column 19; 22; 24-25, (2008/06/13)
Bicycloheteroaryl 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 huma
REARRANGED PENTANOLS, A METHOD FOR THE PRODUCTION THEREOF, AND THEIR USE AS ANTIPHLOGISTICS
-
Page/Page column 23, (2008/06/13)
The invention relates to compounds of formula (I), to a method for the production thereof, and to their use as antiphlogistics.
1-AMINO-2-OXY-SUBSTITUTED TETRAHYDRONAPHTALENE DERIVATIVES, METHODS FOR THE PRODUCTION THEREOF, AND THEIR USE AS ANTIPHLOGISTICS
-
Page/Page column 56, (2010/02/11)
The invention relates to polysubstituted tetrahydronaphtalene derivatives of formula (I), to methods for the production thereof, and to their use as antiphlogistics. The substituents are defined in Claim 1.
Rearranged pentanols, a process for their production and their use as anti-inflammatory agents
-
Page/Page column 8, (2010/02/12)
The invention relates to the compounds of formula I, a process for their production and their use as anti-inflammatory agents.
Multiply-substituted tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents
-
Page/Page column 15, (2010/02/14)
The invention relates to multiply-substituted tetrahydronaphthalene derivatives of formula (I) process for their production and their use as anti-inflammatory agents.
Substituted tetrahydroisoquinolines and uses thereof
-
Page/Page column 21, (2008/06/13)
The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein, n, X, Y, R1, R2, R3, R4 and R5 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.
A new synthesis of 'push-pull' naphthalenes by condensation of nitro-2-methylbenzoate esters with dimethylacetamide dimethyl acetal
Wong, See-Mun,Shah, Bhavini,Shah, Priyal,Butt, Ian C.,Woon, Esther C.Y.,Wright, James A.,Thompson, Andrew S.,Upton, Christopher,Threadgill, Michael D.
, p. 2299 - 2302 (2007/10/03)
Whereas condensation of 2-methyl-3-nitrobenzoate esters with dimethylformamide dimethyl acetal gives 5-nitroisocoumarin, analogous condensation with dimethylacetamide dimethyl acetal proceeds via a different route, affording 1-methoxy-3-dimethylamino-5-ni
Novel 5-HT3 antagonists. Isoquinolinones and 3-aryl-2-pyridones
Matsui,Sugiura,Nakai,Iguchi,Shigeoka,Takada,Odagaki,Nagao,Ushio,Ohmoto,Iwamura,Yamazaki,Arai,Kawamura
, p. 3307 - 3319 (2007/10/02)
Synthesis and pharmacological evaluation of a series of 1,2-dihydro-1-[(5- methyl-1-imidazol-4-yl)methyl]-2-oxopyridine 5-HT3 antagonists are described. The key pharmacophoric elements were defined as a basic nitrogen, a linking group capable o
A ONE POT SYNTHESIS OF 4-HYDROXYMETHYLINDOLE
Somei, Masanori,Shoda, Toshiya
, p. 417 - 423 (2007/10/02)
A practical one pot synthetic method of 4-hydroxymethylindole is developed.The method consists of three operations, in which a novel ring transformation reaction of isocoumarins into isochromans is included.Product analysis and distribution of each operat
