79418-73-8Relevant academic research and scientific papers
CEPHEM COMPOUND HAVING CATECHOL GROUP
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Paragraph 0343; 0345, (2013/03/26)
A compound of the formula: wherein X is -N=, -CH=, or the like; W is -CH2- or the like; U is -S- or the like; R1 and R2 are each independently hydrogen, halogen, optionally substituted lower alkyl, or the like; R3/su
Oxime derivatives for the treatment of dyslipidemia and hypercholesteremia
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, (2008/06/13)
The present invention relates to compounds of Formula (I) which may be useful in the treatment of diseases, such as, metabolic disorders, dyslipidemia and/or hyperchloesterolemia: 1
Heterocyclic derivatives for the treatment of diabetes and other diseases
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, (2008/06/13)
The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.
Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor.
Guay, Daniel,Hamel, Pierre,Blouin, Marc,Brideau, Christine,Chan, Chi Chung,Chauret, Nathalie,Ducharme, Yves,Huang, Zheng,Girard, Mario,Jones, Tom R,Laliberte, France,Masson, Paul,McAuliffe, Malia,Piechuta, Hanna,Silva, Jose,Young, Robert N,Girard, Yves
, p. 1457 - 1461 (2007/10/03)
Structure-activity relationship studies directed toward improving the potency and metabolic stability of CDP-840 (3) resulted in the discovery of L-791,943 (11n) as a potent (HWB TNF-alpha = 0.67 microM) and orally active phosphodiesterase type 4 (PDE4) inhibitor. This compound, which bears a stable bis-difluoromethoxy catechol and a pendant hexafluorocarbinol, exhibited a long half-life in rat and in squirrel monkey. It is well tolerated in ferret with an emetic threshold greater than 30 mg/kg (po) and was found to be active in the ovalbumin-induced bronchoconstriction model in guinea pig and in the ascaris-induced bronchoconstriction models in sheep and squirrel monkey.
