4677-18-3Relevant academic research and scientific papers
Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors
Bamborough, Paul,Chung, Chun-Wa,Furze, Rebecca C.,Grandi, Paola,Michon, Anne-Marie,Watson, Robert J.,Mitchell, Darren J.,Barnett, Heather,Prinjha, Rab K.,Rau, Christina,Sheppard, Robert J.,Werner, Thilo,Demont, Emmanuel H.
, p. 8321 - 8336 (2018/09/27)
ATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of its class. In our recent disclosure of the first chemical probe against this bromodomain, GSK8814 (6), we described the use of a conformationally constrained methoxy piperidine to gain selectivity over the BET bromodomains. Here we describe an orthogonal conformational restriction strategy of the piperidine ring to give potent and selective tropane inhibitors and show structural insights into why this was more challenging than expected. Greater understanding of why different rational approaches succeeded or failed should help in the future design of selectivity in the bromodomain family.
DIHYDROPYRROLOPYRIDINE INHIBITORS OF ROR-GAMMA
-
, (2016/05/24)
Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions co
ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
-
, (2016/04/20)
Described herein are compounds of Formula (S-I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
Dihydropyrrolopyridine inhibitors of ROR-gamma
-
, (2016/11/21)
Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORγ. Also provided are pharmaceutical compositions co
EP1 RECEPTOR LIGANDS
-
, (2013/03/28)
The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
Compounds Which Selectively Modulate The CB2 Receptor
-
Page/Page column 17-18, (2011/04/18)
Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
TETRAZOLE COMPOUNDS WHICH SELECTIVELY MODULATE THE CB2 RECEPTOR
-
Page/Page column 28, (2011/10/03)
Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally usefu
AZAINDOLE GLUCOKINASE ACTIVATORS
-
, (2011/06/26)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
PURINE DERIVATIVES AS IMMUNOMODULATORS
-
Page/Page column 70, (2008/12/08)
The present invention includes novel compounds useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants
Synthesis of bicyclic tertiary α-amino acids
Strachan, Jon-Paul,Whitaker, Regina C.,Miller, Craig H.,Bhatti, Balwinder S.
, p. 9909 - 9911 (2007/10/03)
Novel bicyclic α-amino acids, exo and endo-1-azabicyclo-[2.2.1] heptane-2-carboxylic acid, 1-azabicyclo[2.2.1]heptane-7-carboxylic acid, and 1-azabicyclo[3.2.2]nonane-2-carboxylic acid have been readily synthesized for the generation of neuronal nicotinic receptor ligands. Alkylation of glycine-derived Schiff bases or nitroacetates with cyclic ether electrophiles, followed by acid-induced ring opening and cyclization in NH4OH, allowed for the preparation of substantial quantities of the three tertiary bicyclic α-amino acids.
