wherein n is 0 to 4; m is 0 or 1 with the proviso that the sulphur atom and R3 are in vicinal position (if m=0 then R3 is in position 2′, and if m=1 then R3 is on position 1′); R is ethyl or vinyl; R1 is hydrogen or (C1-6)alkyl, R2 is hydrogen or
(C3-6)cycloalkyl, or unsubstituted (C1-6)alkyl, or (C1-6)alkyl substituted by one or more of
hydroxy; preferably one or two, methoxy, halogen, (C3-6)cycloalkyl, or
R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring containing at least 1 nitrogen atom or 1 nitrogen and 1 additional heteroatom e. g. selected from N or O, or
R1 is hydroxy and R2 is formyl; R3 is OH, OR4, a halogen atom, or R3 is bound to 2′ and represents —O—(CH2)p—O— with p is 2 or 3; R4 is unsubstituted (C1-6)alkyl or (C3-6)cycloalkyl, or a pharmaceutically acceptable salt, solvate, prodrug or metabolite thereof
for the specific use in the treatment or prevention of an inflammatory disease which is not mediated by bacteria.
摘要:
The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
摘要:
Disclosed is a method for the transition metal-mediated oxidation of C—H bonds to form C—O or C—S bonds. The methods are useful for the formation of ethers (R—OR′) from alcohols, R′OH, and sp3-hybridized C—H bonds in substrates, R—H. Aryl or heteroaryl acetates may also be used for C—H to C—OAr bond formation. The methods are also useful in the preparation of C—S bonds from acetyl-protected thiols, MeC(O)SR, and disulfides, RSSR. Advantageously, the methods minimize reaction steps, the handling of oxidized intermediates, and environmental impact.
摘要:
The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.
摘要:
Surfactants useful as dispersing aids in the preparation of compositions comprising a hydrophilic colloid having hydrophobic particles dispersed therein have the structure ##STR1## wherein M is a cation; X represents a group having the structure ##STR2## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen or alkyl; or R.sup.1 and R.sup.2 taken together represent cycloalkyl; or R.sup.3 and R.sup.4 taken together represent cycloalkyl; and, n represents 0 or 1; provided that the total number of carbon atoms in each X group is 3 or 4, and when R.sup.1 is hydrogen R.sup.2 is other than methyl. Such surfactants offer coating and photographic property advantages when incorporated in multilayer photographic materials comprising a support bearing a plurality of hydrophilic colloid layers.
摘要:
The present invention relates to 2-arylpropyl ether or thioether derivatives represented by the following general formula [I]: ##STR1## wherein Ar stands for an aryl group, R stands for a methyl or ethyl group, Y stands for an oxygen or sulfur atom, and B stands for a group represented by the following formula [II]: ##STR2## or the following general formula [III]: ##STR3## wherein Z stands for an oxygen or sulfur atom or a carbonyl or methylene group, R.sup.1 stands for a hydrogen or halogen atom or a lower alkyl group or a lower alkoxy group, and n is an integer of from 1 to 5 with the proviso that when n is 2 or more, the groups R.sup.1 may be the same or different, and also to processes for the preparation or these ethers of thioethers and a use of these ethers or thioethers.These compounds of the present invention have excellent insecticidal and acaricidal activities while the toxicity of these compounds are very low.
摘要:
The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
摘要:
The present invention discloses processes for producing a thiol compound or a sulfide compound from an olefin compound. Diphenylamine or a phenol compound can be used to increase the rate of conversion of the olefin compound to the thiol compound or the sulfide compound.
摘要:
Disclosed herein is a novel method for preparing cyclophanes, comprising forming a disulfide cyclophane by contacting a linker moiety which includes two or more thiol groups, with a metal salt and an oxidant. The disulfide cyclophane is then desulfurized to form a thiacyclophane comprising thioether bridges. This thiacyclophane optionally may be further desulfurized to form an unsaturated hydrocarbon cyclophane, which can then be reduced to form a saturated hydrocarbon cyclophane. The various cyclophanes can be synthesized in a ring form, such as a dimer, trimer or tetramer etc., or they can be synthesized in a tetrahedral or larger structure. Also disclosed are novel cyclophanes formed by the disclosed method.