85658-55-5Relevant academic research and scientific papers
Metal free C-H functionalization of diazines and related heteroarenes with organoboron species and its application in the synthesis of a CDK inhibitor, meriolin 1
Thatikonda, Thanusha,Singh, Umed,Ambala, Srinivas,Vishwakarma, Ram A.,Singh, Parvinder Pal
, p. 4312 - 4320 (2016/05/24)
Here, we report a metal-free cross-coupling reaction of diazines and related heteroarenes with organoboron species via C-H functionalization. The optimized conditions represent a metal-free method for the activation of aryl/heteroarylboronic acids, which undergo coupling with diazines and related heteroarenes. Optimized conditions also find application in the synthesis of a pyrimidine-based potent CDK inhibitor, meriolin1.
TRISUBSTITUTED HETEROCYCLIC DERIVATIVES AS ROR GAMMA MODULATORS
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Page/Page column 55; 56, (2014/09/03)
The present invention provides trisubstituted heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; (I) in which R1, R2, R3, Ra, X, L, m and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the trisubstituted heterocyclic derivatives of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
Administration of TLR7 ligands and prodrugs thereof for treatment of infection by hepatitis C virus
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Page/Page column 41, (2008/06/13)
This invention relates to methods for treating or preventing hepatitis C virus infections in mammals using Toll-Like Receptor (TLR)7 ligands and prodrugs thereof. More particularly, this invention relates to methods of orally administering a therapeutically effective amount of one or more prodrugs of TLR7 ligands for the treatment or prevention of hepatitis C viral infection. Oral administration of these TLR7 immunomodulating ligands and prodrugs thereof to a mammal provides therapeutically effective amounts and reduced undesirable side effects.
Adenosine receptor ligands and their use in the treatment of disease
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, (2008/06/13)
The invention relates to cyclic heteroaromatic compounds, containing at least one nitrogen atom, and to their use in the manufacture of medicaments for the treatment of diseases, related to adenosine receptor modulators, such as Alzheimer's disease, Parkinson's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, asthma, allergic responses, hypoxia, ischaemia, seizure, substance abuse, sedation and they may be active as muscle relaxants, antipsychotics, anti epileptics, anticonvulsants and cardiaprotective agents.
Transformations of 2-Aminopyrimidines and Their N-Oxides under Diazotation Conditions
Sedova, V. F.,Mustafina, T. Yu.,Krivopalov, V. P.,Mamaev, V. P.
, p. 91 - 94 (2007/10/02)
The diazotation of 2-aminopyrimidines and their N-oxides in solutions with various acidities was studied.It is shown that the amino group in pyrimidine N-oxides is not diazotized in strongly acidic media and that bromination in the 5 position of the pyrimidine ring is observed in concentrated hydrobromic acid.When the reaction was carried out in moderately acidic media, it was possible to synthesize the difficult-to-obtain 2-halopyrimidine N-oxides.
