- Oxidative Alkoxylation/Dehydrogenation of Unactivated Cyclic Ketones with Simple Alcohols: Direct Route to α-Alkoxy Cycloenones
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An oxidative functionalization of cyclopentanones or cyclohexanones with simple alcohols was first demonstrated, affording a series of 2-alkoxycyclopent-2-en-1-ones or 2-alkoxycyclohex-2-en-1-ones in moderate to excellent yields. The reaction was involved in tandem iodization, substitution, oxidation and addition-elimination processes in one pot. This method is highly atom-economical and operationally simple.
- Yan, Yizhe,Li, Shaoqing,Wang, Jianyong
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- ACYLSUFONAMIDE COMPOUNDS USEFUL AS EP3 RECEPTOR ANTAGONISTS
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The present invention is directed to acylsulfonamide derivatives of formula (I), pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of, for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
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Page/Page column 130
(2020/01/31)
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- HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF CYSTIC FIBROSIS
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The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses, in particular to modulate CFTR protein or ABC protein activities.
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Page/Page column 154
(2018/10/19)
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- INDAZOLONES AS MODULATORS OF TNF SIGNALING
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The disclosure provides indazolone compounds, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variables are defined herein. The compounds of the disclosure may be useful for treating immunological and oncological conditions.
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Page/Page column 200-201
(2016/11/02)
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- Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl] amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor
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The discovery of a novel class of inhibitors of cyclin dependent kinases (CDKs) is described. Starting from compound 1, showing good potency as inhibitor of CDKs but being poorly selective against a panel of serine-threonine and tyrosine kinases, new analogues were synthesized. Enhancement in selectivity, antiproliferative activity against A2780 human ovarian carcinoma cells, and optimization of the physical properties and pharmacokinetic profile led to the identification of highly potent and orally available compounds. Compound 28 (PHA-848125), which in the preclinical xenograft A2780 human ovarian carcinoma model showed good efficacy and was well tolerated upon repeated daily treatments, was identified as a drug candidate for further development. Compound 28 is currently undergoing phase I and phase II clinical trials.
- Brasca, Maria Gabriella,Amboldi, Nadia,Ballinari, Dario,Cameron, Alexander,Casale, Elena,Cervi, Giovanni,Colombo, Maristella,Colotta, Francesco,Croci, Valter,D'Alessio, Roberto,Fiorentini, Francesco,Isacchi, Antonella,Mercurio, Ciro,Moretti, Walter,Panzeri, Achille,Pastori, Wilma,Pevarello, Paolo,Quartieri, Francesca,Roletto, Fulvia,Traquandi, Gabriella,Vianello, Paola,Vulpetti, Anna,Ciomei, Marina
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experimental part
p. 5152 - 5163
(2010/03/04)
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- PYRAZOLO-QUINAZOLINE DERIVATIVES,PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
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Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
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- RADICAL CYCLIZATIONS OF DIOSPHENOL ω-HALOALKYL ETHERS TO OXABICYCLOALKANONES
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Radical cyclization of diosphenol ω-haloalkyl ethers gives spiro- and fused oxabicycloalkanones.
- Ponaras, Anthony A.,Zaim, Oemer
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p. 2879 - 2882
(2007/10/02)
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- 4-Ylidenebutenolide Syntheses, I. Simple Synthesis of Unsaturated Bicyclic Orthoesters and Their Acidic Hydrolysis to Fused 4-Alkylidene-2-buten-4-olides
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Reaction of (2,2-diethoxyvinylidene)triphenylphosphorane (4) with enolizing cyclic 1,2-diketones 5 via the (2,2-diethoxyvinyl)triphenylphosphonium enolates 8 yields the orthoester phosphoranes 11, which in an intramolecular Wittig reaction spontaneously give the fused orthoesters 7, whose acidic hydrolysis affords the 4-alkylidene-2-buten-4-olides 2.
- Saalfrank, Rolf W.,Schierling, Peter,Schaetzlein, Petra
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p. 1463 - 1467
(2007/10/02)
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