3528-58-3Relevant academic research and scientific papers
The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist
Rimland, Joseph,Dunne, Angela,Hunjan, Suchete S.,Sasse, Rosemary,Uings, Iain,Montanari, Dino,Caivano, Matilde,Shah, Poonam,Standing, David,Gray, David,Brown, David,Cairns, William,Trump, Ryan,Smith, Paul W.,Bertheleme, Nicolas,D'Alessandro, Pier,Gul, Sheraz,Vimal, Mythily,Smith, David N.,Watson, Stephen P.
scheme or table, p. 2340 - 2343 (2010/08/22)
The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A selective over PR is described. Associated structure-activity relationships and the process of optimisation of an initial HTS hit are also described.
PHOSPHODIESTARASE INHIBITORS
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Page/Page column 30-31, (2010/05/13)
The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4 /PDE type 7 inhibitors. Compounds disclosed herein can be useful in the treatment, prevention, inhibition or suppression of CNS diseases, f
Approach to the library of fused pyridine-4-carboxylic acids by combes-type reaction of acyl pyruvates and electron-rich amino heterocycles
Volochnyuk, Dmitriy M.,Ryabukhin, Sergey V.,Plaskon, Andrey S.,Dmytriv, Yuri V.,Grygorenko, Oleksandr O.,Mykhailiuk, Pavel K.,Krotko, Dmitriy G.,Pushechnikov, Alexei,Tolmachev, Andrey A.
scheme or table, p. 510 - 517 (2010/09/05)
A library of fused pyridine-4-carboxylic acids (including pyrazolo[3,4-b]pyridines, isoxazolo[5,4-b]pyridines, furo[2,3-b]pyridines, thieno[2,3-b]pyridines, and pyrido[2,3-d]pyrimidines) was generated by Combes-type reaction of acyl pyruvates and electron-rich amino heterocycles followed by hydrolysis of the ester. The library members were also demonstrated to undergo the standard combinatorial transformations including amide coupling and esterification, as well as less common heterocyclizations to 1,2,4-triazoles and 1,2,4-oxadiazoles.
PYRAZOLO (3, 4-B) PYRIDINE DERIVATIVES AS PDE4 INHIBITORS
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Page/Page column 110, (2008/06/13)
The present invention provides a compound of formula (I) or a salt thereof (in particular, a pharmaceutically acceptable salt thereof): The invention also provides the use of the compounds or salts as inhibitors of phosphodiesterase type IV (PDE4) and/or
PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS
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Page/Page column 168-169, (2010/11/30)
The invention provides a compound of formula (I) or a salt thereof: wherein Ar has the sub-formula (x): and wherein: Q1 is NH or NMe, in which case Q2 is -C(O)-, -S(O)2-, -C(O)NH- or -C(O)NMe-; or Q1 is a bond o
Heterocyclic compounds and their therapeutic use
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, (2008/06/13)
A compound of the formula wherein R1is C1-3alkyl optionally substituted with one or more fluorines; R2is C1-6alkyl, cycloalkyl or NR4R5; R3is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) NR4R5is a nitrogen-containing heterocyclic ring; R6is C1-3alkyl; and R7and R8, which are the same or different, each represents C1-3alkyl, halogen, CF3or CN; or a pharmaceutically-acceptable salt thereof.
Method for inhibiting neoplastic cells by exposure to substituted N-cycloalkylmethyl-1-H-pyrazolo (3,4-B) quinolone-4 amines
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, (2008/06/13)
A method for inhibiting neoplastic cells and related conditions by exposing them to substituted N-cycloalkylmethyl-1H-pyrazolo?3,4-b!quinolin-4-amines.
Substituted N-cycloalkylmethyl-1H-pyrazolo(3,4-b)quinolin-4 amines and compositions and methods of use thereof
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, (2008/06/13)
Substituted N-cycloalkylmethyl-1H-pyrazolo[3,4-b]quinolin-4-amines, pharmaceutical compositions containing them and methods for a) effecting c-GMP-phosphodiesterase inhibition, b) treating heart failure and/or hypertension, c) reversing or reducing nitrate-induced tolerance and d) treating angina pectoris, congestive heart disease and myocardial infarction utilizing them.
Rearrangement of N-(Alkylamino)azoles in Acid Media: A New Entry to C-Amino-N-substituted Azoles
Salazar, Loreto,Espada, Modesta,Avendano, Carmen,Claramunt, Rosa Maria,Sanz, Dionisia,Elguero, Jose
, p. 1563 - 1567 (2007/10/02)
A ring-opening / ring-closure mechanism for the thermal rearrangement of 1-(alkylamino)pyrazoles into 5-amino-1-alkylpyrazoles in acid medium has been established. 1-(Benzylamino)pyrazoles show a different reactivity, affording bis(5-amino-1-benzyl-4-pyrazolyl)phenylmethanes.The reaction was extended to 1-(alkylamino)indazoles but failed in the case of 1-(alkylamino)-1,2,4-triazoles.
