[EN] SULFANYLAMIDE DERIVATIVES, USES THEREOF AND COMPOSITIONS COMPRISING THEM [FR] DÉRIVÉS DE SULFANYLAMIDE, LEURS UTILISATIONS ET COMPOSITIONS LES CONTENANT
Syntheses and Evaluation of Anticonvulsant Profile and Teratogenicity of Novel Amide Derivatives of Branched Aliphatic Carboxylic Acids with 4-Aminobenzensulfonamide
作者:Naama Hen、Meir Bialer、Bogdan Wlodarczyk、Richard H. Finnell、Boris Yagen
DOI:10.1021/jm100170w
日期:2010.5.27
Despite the availability of 14 new antiepileptic drugs (AEDs), about 30% of epileptic patients are not seizure-free. Consequently there is substantial need to develop new effective AEDs. A novel class of aromatic amides composed of phenylacetic acid or branched aliphatic carboxylic acids, with five to nine carbons in their carboxylic moiety, and aminobenzenesulfonamide were synthesized and evaluated in the anticonvulsant rat-maximal electroshock (MES) and subcutaneous metrazol seizure (scMet) tests. Fourteen of the synthesized amides had an anticonvulsant ED(50) of <50 mg/kg in the rat-MES test. The amides 2-methyl-N-(4-sulfamoylphenyl)butyramide (10), 2-ethyl-N-(4-sulfamoylphenyl)butyramide (11), and 3,3-dimethyl-N-(4-sulfamoylphenyl)butyramide (15) were the most potent compounds possessing MES-ED(50) values of 7.6, 9.9, and 9.4 mg/kg and remarkable protective index (PI = TD(50)/ ED(50)) values of 65.7, 50.5, and 53.2, respectively. These potent sulfanylamides caused neural tube defects only at doses markedly exceeding their effective dose. The anticonvulsant properties of these compounds make them potential candidates for further development as new, potent, and safe AEDs.
There is provided a lithographic printing plate precursor that enables image recording using a laser and that provides an excellent scumming resistance and an excellent developability while maintaining a satisfactory printing durability. Also provided are a platemaking method, and a novel polymerizable monomer. A lithographic printing plate precursor has a support, and an image recording layer disposed thereon and containing a radical polymerization initiator and a polymerizable monomer that has a sulfonamide group and at least two ethylenically unsaturated groups; a lithographic printing plate platemaking method uses this lithographic printing plate precursor; and a polymerizable monomer has a sulfonamide group and at least two ethylenically unsaturated groups.
RESIN COMPOSITION FOR LASER ENGRAVING, RELIEF PRINTING PLATE PRECURSOR FOR LASER ENGRAVING AND PROCESS FOR PRODUCING SAME, AND PROCESS FOR MAKING RELIEF PRINTING PLATE
申请人:KAWASHIMA Takashi
公开号:US20120146264A1
公开(公告)日:2012-06-14
A resin composition for laser engraving is provided that includes a low molecular weight compound containing at least one type of polymerizable group selected from the group consisting of an ethylenically unsaturated group, an epoxy group, an oxetanyl group, a hydrolyzable silyl group, and a silanol group and further containing a sulfonamide group, a low molecular weight compound containing a residue selected from the group consisting of a maleimide group, a succinimide group, and a phthalimide group, or a polymer compound containing a constituent unit derived from a compound containing a maleimide group or a constituent unit containing a sulfonamide group.
SULFANYLAMIDE DERIVATIVES, USES THEREOF AND COMPOSITIONS COMPRISING THEM
申请人:Bialer Meir
公开号:US20120264827A1
公开(公告)日:2012-10-18
The present invention concerns a family of sulfanilamide derivatives of formula (I) as anticonvulsant agents, where R is selected from optionally substituted C
4
-C
9
alkyl, optionally substituted C
6
-C
10
aryl, optionally substituted C
6
-C
10
alkylenearyl and optionally substituted C
5
-C
10
heteroaryl; R
2
is selected from —H and optionally substituted C
1
-C
6
alkyl; each of R
3
and R
4
, independently of each other, is selected from —H, optionally substituted C
1
-C
6
alkyl, optionally substituted C
6
-C
10
aryl and optionally substituted C
5
-C
10
heteroaryl; n is 0, 1, 2, 3 or 4. The derivatives have been prepared and their anticonvulsant profile was evaluated for the control of epileptic seizures.