- DIHYDROINDOLE DERIVATIVES USEFUL IN PARKINSON'S DISEASE
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The invention relates to novel heterocyclic compounds of the formula (I) in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
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Page/Page column 15
(2009/04/25)
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- Methods for treating diseases and disorders related to unregulated angiogenesis and/or vasculogenesis
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The present invention relates to methods for treating diseases and disorders related to unregulated angiogenesis and/or vasculogenesis. More specifically, this invention relates to methods for treating diseases and disorders, such as rheumatoid arthritis,
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- Syntheses and properties of benzodipyrrinones
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2,3-Benzannelated dipyrrinone analogs (1 and 2) of xanthobilirubic acid (3) are prepared by base-catalyzed condensation of isoindolinone (5) and indolin-2-one (6) respectively, with methyl 3-(2-formyl-3,5-dimethyl-1H-pyrrol-4-yl)propanoate (4). Nuclear Overhauser effect H-nmr studies indicate that both 1 and 2 adopt preferentially a syn-Z configuration. The former forms a hydrogen-bonded homodimer in nonpolar solvents; the latter is intramolecularly hydrogen bonded.
- Boiadjiev, Stefan E.,Lightner, David A.
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p. 181 - 185
(2007/10/03)
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- Pyrrole substituted 2-indolinone protein kinase inhibitors
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The present invention relates to novel pyrrole substituted 2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
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- Design, synthesis, and evaluations of substituted 3-[(3- or 4- carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases
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Receptor tyrosine kinases (RTKs) have been implicated as therapeutic targets for the treatment of human diseases including cancers, inflammatory diseases, cardiovascular diseases including arterial restenosis, and fibrotic diseases of the lung, liver, and kidney. Three classes of 3-substituted indolin-2-ones containing propionic acid functionality attached to the pyrrole ring at the C-3 position of the core have been identified as catalytic inhibitors of the vascular endothelial growth factor (VEGF), fibroblast growth factor (FGF), and platelet-derived growth factor (PDGF) RTKs. Some of the compounds were found to inhibit the tyrosine kinase activity associated with isolated vascular endothelial growth factor receptor 2 (VEGF-R2) [fetal liver tyrosine kinase 1 (Flk-1)/kinase insert domain- containing receptor (KDR)], fibroblast growth factor receptor (FGF-R), and platelet-derived growth factor receptor (PDGF-R) tyrosine kinase with IC50 values at nanomolar level. Thus, compound 1 showed inhibition against VEGF-R2 (Flk-1/KDR) and FGF-R1 tyrosine kinase activity with IC50 values of 20 and 30 nM, respectively, while compound 16f inhibited the PDGF-R tyrosine kinase activity with IC50 value of 10 nM. Structural models and structure-activity relationship analysis of these compounds for the target receptors are discussed. The cellular activities of these compounds were profiled using cellular proliferation assays as measured by bromodeoxyuridine (BrdU) incorporation. Specific and potent inhibition of cell growth was observed for some of these compounds. These data provide evidence that these compounds can be used to inhibit the function of these target receptors.
- Sun, Li,Tran, Ngoc,Liang, Congxin,Tang, Flora,Rice, Audie,Schreck, Randall,Waltz, Kara,Shawver, Laura K.,McMahon, Gerald,Tang, Cho
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p. 5120 - 5130
(2007/10/03)
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