650628-19-6Relevant academic research and scientific papers
COMBINATION THERAPY FOR TREATING MPS1
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Paragraph 0311-0314; 0382-0385, (2021/08/14)
The application is directed to compounds of formula (I) and their salts and solvates, wherein B, R1, R2, R3, R3', R4, R4', and R5 are as set forth in the specification, as well as to methods for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of, e.g., MPS1, optionally in combination with α-L-iduronidase or an analog or variant thereof, e.g., laronidase.
Identification of novel GLUT inhibitors
Siebeneicher, Holger,Bauser, Marcus,Buchmann, Bernd,Heisler, Iring,Müller, Thomas,Neuhaus, Roland,Rehwinkel, Hartmut,Telser, Joachim,Zorn, Ludwig
, p. 1732 - 1737 (2016/07/27)
The compound class of 1H-pyrazolo[3,4-d]pyrimidines was identified using HTS as very potent inhibitors of facilitated glucose transporter 1 (GLUT1). Extensive structure–activity relationship studies (SAR) of each ring system of the molecular framework was established revealing essential structural motives (i.e., ortho-methoxy substituted benzene, piperazine and pyrimidine). The selectivity against GLUT2 was excellent and initial in vitro and in vivo pharmacokinetic (PK) studies are encouraging.
AMINO-HETEROCYCLIC COMPOUNDS
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Page/Page column 16-17, (2009/02/11)
The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3 are as defined herein. Pharmaceutical compositions containing the compounds of Formul
AMINO-HETEROCYCLIC COMPOUNDS
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Page/Page column 48-49, (2009/01/20)
The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3 are as defined herein. Pharmaceutical compositions containing the compounds of Formul
6-Arylmethyl-substituted pyrazolopyrimidines
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, (2008/06/13)
The invention relates to novel 6-arylmethyl-substituted pyrazolopyrimidines, process for their preparation and their use for producing medicaments for improving perception, concentration, learning and/or memory.
6-ARYLMETHYL-SUBSTITUTED PYRAZOLOPYRIMIDINES
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Page/Page column 30, (2008/06/13)
The invention relates to novel 6-arylmethyl-substituted pyrazolopyrimidines of formula (I) wherein R1 represents phenyl, pyridyl or thiophenyl, and R2 represents phenyl or heteroaryl. The invention also relates to the salts and solvates thereof, and/or solvates of the salts thereof, to methods for producing said pyrazolopyrimidines, and to the use of the same for producing pharmaceuticals for improving perception, power of concentration, learning capacity and/or memory retention.
6-CYCLYLMETHYL- AND 6-ALKYLMETHYL-SUBSTITUTED PYRAZOLOPYRIMIDINES
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Page/Page column 34-35, (2008/06/13)
The invention relates to novel 6-cyclylmethyl- and 6-alkylmethyl-substituted pyrazolopyrimidines, method for production and use thereof for the production of medicaments for the improvement of cognition, concentration, learning and/or memory capacity.
PYRAZOLOPYRIMIDINES AS KINASE INHIBITORS
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Page 28, (2010/02/06)
The present invention relates generally to inhibitors of the kinases and more particularly to novel pyrazolopyrimidine compounds.
Novel pyrazolopyrimidine derivatives as GSK-3 inhibitors
Peat, Andrew J.,Boucheron, Joyce A.,Dickerson, Scott H.,Garrido, Dulce,Mills, Wendy,Peckham, Jennifer,Preugschat, Frank,Smalley, Terrence,Schweiker, Stephanie L.,Wilson, Jayme R.,Wang, Tony Y.,Zhou, Huiqiang Q.,Thomson, Stephen A.
, p. 2121 - 2125 (2007/10/03)
A series of [1-aryl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]arylhydrazones were discovered as novel inhibitors glycogen synthase kinase-3 (GSK-3). Based on initial modeling a detailed SAR was constructed. Modification of the interior binding aryl ring (Ar1) determined this to be a tight binding region with little room for modification. As predicted from the model, a large variety of modifications could be incorporated into the hydrazone aryl ring. This work led to GSK-3 inhibitors in the low nano-molar range.
