- CLASS OF HDAC INHIBITORS EXPANDS THE RENAL PROGENITOR CELLS POPULATION AND IMPROVES THE RATE OF RECOVERY FROM ACUTE KIDNEY INJURY
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Compounds and compositions are provided that inhibit histone deacylase activity and which expand renal progenitor cell populations and improve kidney function in a damaged kidney. Methods of use of the compounds and compositions are provided.
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- [3,3]-sigmatropic rearrangement versus carbene formation in gold-catalyzed transformations of alkynyl aryl sulfoxides: Mechanistic studies and expanded reaction scope
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Gold-catalyzed intramolecular oxidation of terminal alkynes with an arenesulfinyl group as the tethered oxidant is a reaction of high impact in gold chemistry, as it introduced to the field the highly valued concept of gold carbene generation via alkyne o
- Lu, Biao,Li, Yuxue,Wang, Youliang,Aue, Donald H.,Luo, Yingdong,Zhang, Liming
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p. 8512 - 8524
(2013/07/19)
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- Synthesis of a wide range of thioethers by indium triiodide catalyzed direct coupling between alkyl acetates and thiosilanes
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An indium triiodide-catalyzed substitution of the acetoxy group in alkyl acetates with thiosilanes provides access to a variety of thioethers. The method is efficient for a wide scope of acetates such as primary alkyl, secondary alkyl, tertiary alkyl, allylic, benzylic, and propargylic acetates.
- Nishimoto, Yoshihiro,Okita, Aya,Yasuda, Makoto,Baba, Akio
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supporting information; experimental part
p. 1846 - 1849
(2012/06/18)
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- CLASS OF HDAC INHIBITORS EXPANDS THE RENAL PROGENITOR CELLS POPULATION AND IMPROVES THE RATE OF RECOVERY FROM ACUTE KIDNEY INJURY
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Compounds and compositions are provided that inhibit histone deacylase activity and which expand renal progenitor cell populations and improve kidney function in a damaged kidney. Methods of use of the compounds and compositions are provided.
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- Discovery of Lu AA33810: A highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder
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The structure-activity relationship of a series of tricyclic-sulfonamide compounds 11-32 culminating in the discovery of N-[trans-4-(4,5-dihydro-3,6- dithia-1-aza-benzo[e]azulen-2-ylamino)-cyclohexylmethyl]-methanesulfonamide (15, Lu AA33810) is reported. Compound 15 was identified as a selective and high affinity NPY5 antagonist with good oral bioavailability in mice (42%) and rats (92%). Dose dependent inhibition of feeding was observed after i.c.v. injection of the selective NPY5 agonist ([cPP1-7,NPY19-23,Ala 31,Aib32,Gln34]-hPP). In addition, ip administration of Lu AA33810 (10 mg/kg) produced antidepressant-like effects in a rat model of chronic mild stress.
- Packiarajan, Mathivanan,Marzabadi, Mohammad R.,Desai, Mahesh,Lu, Yalei,Noble, Stewart A.,Wong, Wai C.,Jubian, Vrej,Chandrasena, Gamini,Wolinsky, Toni D.,Zhong, Hualing,Walker, Mary W.,Wiborg, Ove.,Andersen, Kim
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scheme or table
p. 5436 - 5441
(2011/10/12)
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- Design of potent inhibitors of human β-secretase. Part 1
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We describe a novel series of potent inhibitors of human β-secretase. These compounds possess the hydroxyethyl amine transition state isostere. A 2.5 A crystal structure of inhibitor 32 bound to BACE is provided.
- Freskos, John N.,Fobian, Yvette M.,Benson, Timothy E.,Bienkowski, Michael J.,Brown, David L.,Emmons, Thomas L.,Heintz, Robert,Laborde, Alice,McDonald, Joseph J.,Mischke, Brent V.,Molyneaux, John M.,Moon, Joseph B.,Mullins, Patrick B.,Bryan Prince,Paddock, Donna J.,Tomasselli, Alfredo G.,Winterrowd, Gregory
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- Substituted (aryl, heteroaryl, arylmethyl or heteroarylmethyl) hydroxamic acid compounds
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This invention is directed to compounds of formula I: wherein the variables are as described herein. Compounds within the scope of the present invention possess useful properties, more particularly pharmaceutical properties. They are especially useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. Compounds within the scope of the present invention may also inhibit an MMP, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting MMPs, such disease states involve tissue breakdown and those associated with a physiologically detrimental excess of TNF. The present invention is therefore also directed to the pharmaceutical use of the compounds, pharmaceutical compositions containing the compounds, intermediates leading thereto and methods for the preparation of the compounds and their intermediates.
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- CONVERSION OF LACTONE INTO LACTONE HEMITHIOACETAL AND SYNTHESIS OF ENOL LACTONE
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Lactone hemithioacetal was synthesized in good yield from ω-phenylthiocarboxylic acid derived from lactone, and it was converted into enol lactone via the corresponding sulfoxide.
- Ochiai, Masahito,Nishide, Kiyoharu,Node, Manabu,Fujita, Eiichi
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p. 283 - 284
(2007/10/02)
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- Hard Acid and Soft Nucleophile Systems. 5. Ring-Opening Reaction of Lactones to ω-Alkylthio or ω-Arylthio Carboxylic Acids with Aluminum Halide and Thiol
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Lactones were converted into ω-alkylthio carboxylic acids in high yields through ω-carbon-oxygen bond cleavage when they were treated with aluminun halide and alkanethiol.The aluminum halide and arenethiol system has also been found to be useful for the preparation of the synthetically valuable ω-arylthio carboxylic acids from lactones.
- Node, Manabu,Nishide, Kiyoharu,Ochiai, Masahito,Fuji, Kaoru,Fujita, Eiichi
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p. 5163 - 5166
(2007/10/02)
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