申请人:Novartis Corporation
公开号:US05817822A1
公开(公告)日:1998-10-06
The present invention relates to the alpha-(N-substituted pyrrolidinyl and piperidinyl) alpha-(arysulfonamido)-aceto-hydroxamic acids of formula I ##STR1## wherein R represents acyl derived from a carboxylic acid, from a carbonic acid or from a carbamic acid; or R represents (lower alkyl, aryl-lower alkyl or aryl)-sulfonyl, di-(aryl-lower alkyl or alkyl)-aminosulfonyl, or aryl-lower alkyl; Ar represents carbocyclic aryl, heterocyclic aryl or biaryl; R.sub.1 and R.sub.2 represent independently hydrogen, lower alkyl, lower alkoxy, halogen, hydroxy, acyloxy, lower alkoxy-lower alkoxy, trifluoromethyl or cyano; or R.sub.1 and R.sub.2 together on adjacent carbon atoms represent lower alkylenedioxy; m represents zero or one; n represents an integer from 1 to 5; pharmaceutically acceptable prodrug derivatives thereof; and pharmaceutically acceptable salts thereof; further to a process for the preparation of these compounds, to pharmaceutical compositions comprising these compounds, to the use of these compounds for the therapeutic treatment of the human or animal body or for the manufacture of a pharmaceutical composition.
本发明涉及式I的α-(N-取代吡咯烷基和哌嗪基)α-(芳基磺酰胺基)-乙酰羟肟酸,其中R表示来自羧酸、碳酸或氨基甲酸的酰基; 或R表示(较低的烷基、芳基-较低的烷基或芳基)-磺酰基、二-(芳基-较低的烷基或烷基)-氨基磺酰基或芳基-较低的烷基; Ar表示碳环芳基、杂环芳基或双芳基; R1和R2独立地表示氢、较低的烷基、较低的烷氧基、卤素、羟基、酰氧基、较低的烷氧基-较低的烷氧基、三氟甲基或氰基; 或R1和R2在相邻的碳原子上共同表示较低的烷基二氧基; m表示零或一; n表示1到5的整数; 其药物学上可接受的前药衍生物; 以及其药物学上可接受的盐; 进一步涉及制备这些化合物的方法、包含这些化合物的制药组合物、使用这些化合物治疗人体或动物体或制造制药组合物的用途。