Dorogov Mikhail Vladimirovich,Дорогов Михаил Владимирович,Krasavin Mikhail Yurevich,Красавин Михаил Юрьевич
申请号：
RU2015138755
公开号：
RU0002607630C1
申请日:
2015.09.11
申请国别(地区):
RU
年份:
2017
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: present invention relates to novel aromatic sulphonamide derivatives, general formula 1 and pharmaceutically acceptable salts thereof, which are selective inhibitors of carbonic anhydrase II (CA II). Substituted sulphonamides correspond to general formula 1,where A is phenyl or thiophene R1 is C1-C5alkyl, C-3C6cycloalkyl, -C(O)R3 provided that R1 is not methyl, when A is phenyl, R2 represents hydrogen R3 is a 5-6 member heterocyclyl with one or two heteroatoms, selected from nitrogen or oxygen atoms R2 is C1-C3alkyl, C1-C3alkoxy. Invention also relates to a method of producing compounds of general formula 1. Method involves two stages: a) sulphochlorination of corresponding oxazole derivative of general formula 5 (a-o) or 6 (a-j) with a mixture chlorosulphonic acid and thionyl chloride to produce intermediate sulphochlorides of formula 7 (a-o) or 8 (a-j), respectively, and b) with subsequent conversion of obtained sulphochlorides into primary sulphamides of formula 9 (b-o) or 10 (a-j) by reacting with ammonia according to following scheme,where,where R1 is C1-C5alkyl, C3-C6cycloalkyl NRRʺ is a morpholine or pyrrolidine.EFFECT: compounds can be used for treating glaucoma, in particular, open-angle glaucoma, and other diseases caused by high intraocular pressure, age-related macular degeneration, diabetic macular edema, diabetic retinopathy, hypertensive retinopathy and retinal vasculopathy mediated by activity of carbonic anhydrase II.11 cl, 2 dwg, 2 tbl, 57 exНастоящее изобретение относится к новым ароматическим производным сульфаниламидов, общей формулы 1 и их фармацевтически приемлемым солям, которые являются селективными ингибиторами карбоангидразы II (СА II). Соединения смогут быть использованы для лечения глаукомы, в частности открытоугольной глаукомы, и др. заболеваний, вызванных повышенным внутриглазным давлением, возрастной макулярной дегенерации, диабетического макулярного отека, диабетической ретинопатии, гипертензивной ретинопа
