5618-01-9Relevant academic research and scientific papers
COMPLEMENT MODULATORS AND RELATED METHODS
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Paragraph 0750, (2020/10/20)
The present disclosure presents compounds and compositions that interact with complement components. Some compounds inhibit complement activity. Included are small molecule compounds and compositions that function as C5 inhibitor compounds. Methods for inhibiting complement activity and methods of treating complement-related indications with the C5 inhibitor compounds and compositions are provided.
Photochemical synthesis of highly functionalized cyclopropyl ketones
Wessig, Pablo,Muehling, Olaf
, p. 865 - 893 (2007/10/03)
A series of di- and trisubstituted cyclopropyl ketones 11 were prepared by irradiation of ketones 3 and 5, which bear a leaving group adjacent to the carbonyl C-atom. The required ketones 3 could be easily synthesized either by functionalization of ketones 1 with a hypervalent iodine reagent, 2, or by O-sulfonylation of α-hydroxy ketones 7. The nitrates 5 were obtained by treatment of the corresponding α-bromo ketones with AgNO3. The irradiation of 3 and 5 must be performed in the presence of an acid scavenger (1-methyl-1H-imidazole) to obtain the cyclopropanes 11 in good yields. The synthetic efficiency of the method was, among other things, demonstrated by the preparation of a highly strained bicyclo[2.1.0]pentane 11i in good yield. The mechanism of the photochemical cyclization was investigated by means of photokinetic measurements, as well as by quantum-chemical calculations. It was shown that the presence of the leaving group substantially influences all steps of the photochemical reaction cascade. The X-ray crystal structures of 11j and exo-11k were also determined.
METHOD FOR TREATING ANXIETY
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, (2008/06/13)
The present invention provides a method for treating anxiety in humans using azacyclic or azabicyclic compounds.
HETEROCYCLIC COMPOUNDS AND THEIR PREPARATION AND USE
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, (2008/06/13)
The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
Monoradical Rearrangements of the 1,4-Biradicals Involved in Norrish Type II Photoreactions
Wagner, Peter J.,Liu, Kou-Chang,Noguchi, Y.
, p. 3837 - 3841 (2007/10/02)
The photochemistry of α-allylbutyrophenone (α-AB) and that of γ-cyclopropylbutyrophenone (γ-CB) both reveal that the 1,4-biradicals generated by triplet-state γ-hydrogen abstraction undergo typical radical rearrangements in competition with their more normal type II reactions.From α-AB, 2-phenyl-2-norbornanol is formed in 1/24th the combined yield of 1-phenyl-4-penten-1-one and 1-phenyl-2-allylcyclobutanol.Its formation is explained by a 5-hexenyl-to-cyclopentylmethyl rearrangement of the 1,4-biradical, with a rate constant of 5 x 105 s-1.From γ-CB, 1-phenyl-4-hepten-1-one and 1-phenyl-4-cycloheptenol together are formed in double the yield of acetophenone.Their formation is explained by a cyclopropylcarbinyl-to-allylcarbinyl rearrangement of the 1,4-biradical, with a rate constant of 2 x 107 s-1.In both cases, the rearrangement percentages are what would be predicted if the biradicals have the same 35 - 50-ns lifetime measured for other ketones and if they rearrange with the same rate constants characteristic of monoradicals.Triplet γ-CB decays only 1.5 times faster than triplet γ-isopropylbutyrophenone, indicating that there is at most a small enhancement of the γ-hydrogen abstraction rate by cyclopropyl cojugation.Triplet α-AB decays 100 times faster than triplet butyrophenone, 99percent representing internal quenching by the β-vinyl group ( k = 8 x 108 s-1).Bicyclic oxetanes are formed in quantum yields of only 0.01.No oxetanes were isolated, only rearranged unsaturated alcohols and aldehydes.
Pyridine esters of cyclopropane-carboxylic acid
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, (2008/06/13)
Heterocyclic organic esters and thioesters characterized by the presence of one or two cyclopropane moieties, synthesis thereof, and compositions thereof for the control of mites and ticks.
Organic compositions
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, (2008/06/13)
Cyclopropyl substituted esters, syntheses thereof, compositions thereof, and use for the control of mites and ticks.
Control of Acarina by esters of cyclopropane acids
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, (2008/06/13)
Methods and compositions for the control of Acarina employing esters of cyclopropane carboxylic acids described herein.
