- Sulfonyl fluoride inhibitors of fatty acid amide hydrolase
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Sulfonyl fluorides are known to inhibit esterases. Early work from our laboratory has identified hexadecyl sulfonylfluoride (AM374) as a potent in vitro and in vivo inhibitor of fatty acid amide hydrolase (FAAH). We now report on later generation sulfonyl
- Alapafuja, Shakiru O.,Nikas, Spyros P.,Bharathan, Indu T.,Shukla, Vidyanand G.,Nasr, Mahmoud L.,Bowman, Anna L.,Zvonok, Nikolai,Li, Jing,Shi, Xiaomeng,Engen, John R.,Makriyannis, Alexandros
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p. 10074 - 10089
(2013/01/16)
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- Dioxolane analogs for improved inter-cellular delivery
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Dioxolane analogs of the following formula: wherein R1 and R2 are defined herein, are useful in the treatment of cancer. For example, the compounds can be used to treat patients with cancer in which the cancer cells are deficient in nucleoside or nucleosi
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- Azetidinone derivatives for the treatment of atherosclerosis
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PCT No. PCT/EP95/04202 Sec. 371 Date Sep. 30, 1997 Sec. 102(e) Date Sep. 30, 1997 PCT Filed Oct. 25, 1995 PCT Pub. No. WO96/13484 PCT Pub. Date May 9, 1996Azetidinone derivatives of formula (I) in which R1 and R2, which may be the same or different, is each selected from hydrogen or C(1-8)alkyl; R3 is C(1-8)alkyl or C(3-8)cycloalkyl each of which may be optionally substituted; X is a linker group; Y is an aryl group; and n is 0, 1 or 2; and excluding benzyl (4-methylthio-2-oxo-azetidin-1-yl)acetate are inhibitors of the enzyme Lp PLA2 and are of use in therapy, in particular treating atherosclerosis.
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- Substituted azetidin-2-ones for treatment of atherosclerosis
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Compounds of formula (I) in which R1 and R2, which may be the same or different, is each selected from hydrogen, halogen or C(1-8) alkyl; R3 is aryl or aryl C(1-4) alkyl which may be optionally substituted; X is a linker group; Y is an optionally substituted aryl group; and n is 0, 1 or 2; are inhibitors of the enzyme Lp-PLA2 and thereof of use in treating atherosclerosis.
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- 2-amino-1,3-propanediol compound and immunosuppressant
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2-Amino-1,3-propanediol compounds of the formula (I) STR1 wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R2, R3, R4 and R5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients. The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.
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- ALIPHATIC AMINO BIS-ARYL SQUALENE SYNTHASE INHIBITORS
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This invention relates to a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
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- One-pot, one- and multi-carbon homologation of alkyl halides; reaction of Grignard reagents with chloroiodomethane
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Reaction of a Grignard reagent (RMgX) with chloroiodomethane affords the corresponding iodide (RI) and, depending on R, solvent and temperature, iodides which are one-carbon and multicarbon homologs of RX. Allyl iodide but not allyl bromide can be monohomologated by the combined action of chloroiodomethane and isopropyl Grignard.
- Hahn,Tompkins
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p. 937 - 940
(2007/10/02)
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- Aryl substituted diketones
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Aryl substituted diketones and keto-esters, useful as antiviral agents and insecticides, are prepared by reacting an arylalkyl or arylalkenyl iodide with a metal salt of the appropriate diketone or keto-ester.
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- Methylenedioxyphenyl substituted aliphatic diketones
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Aryl substituted diketones and keto-esters, useful as antiviral agents and insecticides, are prepared by reacting an arylalkyl or arylalkenyl iodide with a metal salt of the appropriate diketone or keto-ester.
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- Aryl substituted ketones
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Aryl substituted tertiary carbinols, useful as antiviral agents and insecticides, are prepared by reacting the Grignard reagent derived from an arylalkyl or arylalkenyl iodide with a dialkyl ketone or an alkyl alkenyl ketone; or by reacting an arylalkyl or arylalkenyl ketone with an alkyl- or alkenylmagnesium halide.
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