521300-01-6Relevant academic research and scientific papers
Synthesis and biological activity of 8-azapurine and pyrazolo[4,3-d]pyrimidine analogues of myoseverin
Krystof, Vladimir,Moravcova, Daniela,Paprskarova, Martina,Barbier, Pascale,Peyrot, Vincent,Hlobilkova, Alice,Havlicek, Libor,Strnad, Miroslav
, p. 1405 - 1411 (2006)
The trisubstituted purine myoseverin has been recently identified as a novel inhibitor of microtubule assembly. To analyze the effects of modifying its heterocyclic skeleton, we prepared 8-azapurine and pyrazolo[4,3-d]pyrimidine analogues of myoseverin an
INDOLE AHR INHIBITORS AND USES THEREOF
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Paragraph 00290; 00292, (2018/11/22)
The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.
The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents
DeNinno, Michael P.,Andrews, Melissa,Bell, Andrew S.,Chen, Yue,Eller-Zarbo, Cynthia,Eshelby, Nan,Etienne, John B.,Moore, Dianna E.,Palmer, Michael J.,Visser, Michael S.,Yu, Li J.,Zavadoski, William J.,Michael Gibbs
supporting information; experimental part, p. 2537 - 2541 (2009/12/25)
Starting from a non-selective pyrazolo-pyrimidone lead, the sequential use of parallel medicinal chemistry and directed synthesis led to the discovery of potent, highly selective, and orally bioavailable PDE9 inhibitors. The availability of these tools allowed for a thorough evaluation of the therapeutic potential of PDE9 inhibition.
5,7-DIAMINOPYRAZOLO`4,3-D!PYRIMIDINES USEFUL IN THE TREATMENT OF HYPERTENSION
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Page 169, (2008/06/13)
This invention relates to compounds of formula (I).
PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease
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Page 17, (2010/02/09)
The invention provides compounds of Formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs, wherein A, P, J, x, and R10 are as defined herein; pharmaceutical compositions thereof; and methods of using the pharmaceutical compositions for the treatment of diseases, including, diabetes, including type 1 and type 2 diabetes, hyperglycemia, dyslipidemia, impaired glucose tolerance, metabolic syndrome, and/or cardiovascular disease.
PDE9 inhibitors for treating cardiovascular disorders
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, (2008/06/13)
The invention relates to PDE9 inhibitors for treating cardiovascular disorders. Preferred PDE9 inhibitors are compounds of formula I wherein R1 is H or C1-6 alkyl, wherein R1 is attached to either N1 or N2; R2 is C1-6 alkyl optionally substituted by hydroxy or alkoxy; C3-7 cycloalkyl optionally substituted by alkyl, hydroxy or alkoxy; a saturated 5-6-membered heterocycle optionally substituted by alkyl, hydroxy or alkoxy; het1 or Ar1; R3 is C1-6 alkyl optionally substituted by 1 or 2 groups independently selected from: Ar2; C3-7cycloalkyl optionally substituted by C1-6alkyl; OAr2; SAr2; NHC(O)C1-6 alkyl; het2; xanthene; and naphthalene.
Pyrazolo[4,3-d]pyrimidines, processes for their preparation and methods for therapy
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Page/Page column 25, (2008/06/13)
The invention relates to 3-, 5-, 7-trisubstituted pyrazolo[4,3-d]pyrimidines represented by the general formula I and pharmaceutically acceptable salts thereof, wherein R3 is an optionally substituted alkyl, cycloalkyl, cycloheteroalkyl, cycloalkyl alkyl, aryl or alkylaryl group;R5 is halogen, -NHNH2, -NHOH, NHCONH2, guanylo (NH-C(NH)NH2) an optionally substituted C1-C6 alkyl, alkenyl, alkinyl, C3-C15 cycloalkyl, Rf (C3-C15 cycloalkyl), heterocycle, heteroalkyl, aryl, heteroaryl, arylalkyl, cycloheteroalkyl, cycloheteroalkyl alkyl, heteroarylalkyl group, the group -C(O)-Ra, -C(O)NRbRc, -SO3Rd, or -NHC(O)Re, wherein Ra and Rf are an optionally substituted C1-C6 alkyl, alkenyl, or alkinyl group, Rb, Rc and Rd are independently selected from the group consisting of H, optionally substituted C1-C6 alkyl, alkenyl, or alkinyl group, and Re is a hydroxy, amino, alkoxy, alkylamino, optionally substituted C1-C6 alkyl, alkenyl or alkinyl group; or the group -X-R5', wherein X is -NH-, -O-, -S- or -N(alkyl)- and R5' is hydrogen, an optionally substituted C1-C6 alkyl, alkenyl, alkinyl, C3-C15 cycloalkyl, , Rf(C3-C15 cycloalkyl), aryl, heterocycle, hetero C1-C6 alkyl, arylalkyl, heteroaryl, cycloheteroalkyl, cycloheteroalkyl alkyl, or heteroarylalkyl group, the group -C(O)-Ra, -C(O)NRbRc, -SO3Rd, or -NHC(O)Re, wherein Ra, Rb, Rc, Rd, Re and Rf have the above meaning, andR7 is halogen, -NHNH2, NHOH, NHCONH2, guanylo (NH-C(NH)NH2) or the group -X-R7', wherein X has the above meaning and the meaning of R7' is as defined for R5'.
