首页> 外国专利> USE OF aIL- AGONISTS FOR PREPARING PHARMACEUTICAL COMPOSITIONS FOR TREATING URINARY INCONTINENCE, SOME PHENYLIMINOIMIDAZOLIDINE DERIVATIVES AND A PROCESS FOR THEIR PREPARATION

USE OF aIL- AGONISTS FOR PREPARING PHARMACEUTICAL COMPOSITIONS FOR TREATING URINARY INCONTINENCE, SOME PHENYLIMINOIMIDAZOLIDINE DERIVATIVES AND A PROCESS FOR THEIR PREPARATION

机译:使用抗菌剂制备药物组合物治疗尿不宁,某些苯并亚氨基咪唑啉衍生物及其制备方法

摘要

Use of aIL-agonists for the preparation of pharmaceutical compositions for treating urinary incontinence, particularly stress incontinence substantially as described in the specification. Phenyliminoimidazolidines of the formula 2961 י' בכסלו התשס" ב - November 25, 2001 wherein R1 denotes hydrogen, C1-6-alkyl, C3-6-cycloalkyl, C1-6-alkoxy; halogen, -CF3 or OCF3; R2 denotes -NR6R7 wherein R6 is hydrogen, C1-6-cycloalkyl, C1-6-alkyl, C2-4-acyl, R7 is hydrogen, C3-6-cycloalkyl, C1-6-alkyl, C2-4-acyl, or R6 and R7 together with the nitrogen atom form a 5- or 6-membered saturated or unsaturated ring which may contain up to two further heteroatoms from the group comprising oxygen, sulphur or nitrogen, whilst each additional nitrogen atom may be substituted by C1-4-alkyl, preferably methyl; or R6 and R7 together with the nitrogen atom form phthalimido; R3 denotes hydrogen, halogen, C1-6-alkyl, C1-6-alkoxy, -CF3 or -OCF3; R4 denotes hydrogen, C1-6-alkyl or halogen; R5 denotes hydrogen, C1-6-alkyl, C1-6-alkoxy, halogen, -CF3 or -OCF3, and the pharmaceutically acceptable acid addition salts thereof, with the exception of 2-(3-Acetamido-2,6- dibromophenylimino)- imidazolidine, 2-(3-Acetamido-2,6-diethylphenylimino) -imidazolidine, 2-(3-Acetamido-2,6- dimethylphenylimino)-imidazolidine, 2-(3-Acetamido-2,6- dibromophenylimino)-imidazolidine, 2-(3-Amino-2,6- dichloro-4- methylphenylimino)- imidazolidine, 2-(3-Amino-2,6- dichloro-4- methylphenylimino)- imidazolidine- Dihydrochloride, 2-(3-Amino-2,6- dichlorophenylimino)- imidazolidine, 2-(3-Amino-2,6- dichlorophenylimino)- imidazolidine-Hydrochloride, 2-(3-Amino-2,6- diethylphenylimino)- imidazolidine, 2-(3-Amino-2,6- diethylphenylimino)- imidazolidine-Dihydrochloride, 2-(3-Amino-2,6- dimethylphenylimino)- imidazolidine, 2-(3-Amino-2,6- ditrifluoromethylphenylimino)- imidazolidine, 2-(3-Amino-4- fluorophenylimino)- imidazolidine, 2-(3-Amino-6-chloro-4- methylphenylimino)- imidazolidine, 2-(3-Amino-6-chloro- 4-methylphenylimino)- imidazolidine- Dihydrochloride, 2-(3-Diethylamino-2- methylphenylimino)- imidazolidine, 2-(5-Amino-2,4- dibromo-6- fluorophenylimino)- imidazolidine, 2-(5-Amino-2,4- dibromophenylimino)- imidazolidine, 2-(5-Amino-2,4- dichloro-6- fluorophenylimino)- imidazolidine, 2-(5-Amino-2,4- dichlorophenylimino)- imidazolidine, 2-(5-Amino-2,4- dimethylphenylimino) -imidazolidine, 2-(5-Amino-2-bromo- 4-chloro-6- fluorophenylimino)- imidazolidine, 2-(5-Amino-2-bromo-4-fluorophenylimino)- imidazolidine, 2-(5-Amino-2-bromophenylimino)- imidazolidine, 2-(5-Amino-2- chloro- 4-fluorophenylimino)- imidazolidine, 2-(5-Amino-2- chlorophenylimino)- imidazolidine, 2-(5-Amino-2-chlorophenylimino)- imidazolidine-Hydrochloride, 2-(5-Amino-2- methylphenylimino)- imidazolidine, 2-(5-Amino-2- methylphenylimino)- imidazolidine- Dihydrochloride, 2-(5-Amino-4-bromo-2- chloro- 6-fluorophenylimino)- imidazolidine are claimed as novel.
机译:基本上如说明书中所述,aIL激动剂在制备用于治疗尿失禁,尤其是压力性尿失禁的药物组合物中的用途。式2961的苯基亚氨基亚咪唑烷-2001年11月25日,其中R1代表氢,C1-6-烷基,C3-6-环烷基,C1-6-烷氧基;卤素,-CF3或OCF3; R2代表-NR6R7其中R6是氢,C1-6-环烷基,C1-6-烷基,C2-4-酰基,R7是氢,C3-6-环烷基,C1-6-烷基,C2-4-酰基,或R6和R7一起与氮原子形成5或6元饱和或不饱和环,其可含有至多两个选自氧,硫或氮的杂原子,而每个另外的氮原子可被C 1-4烷基取代,优选甲基;或R 6和R 7与氮原子一起形成邻苯二甲酰亚胺基; R 3表示氢,卤素,C 1-6-烷基,C 1-6-烷氧基,-CF 3或-OCF 3; R 4表示氢,C 1-6-烷基或卤素; R 5表示氢,C 1-6-烷基,C 1-6-烷氧基,卤素,-CF 3或-OCF 3及其药学上可接受的酸加成盐,但2-(3-乙酰氨基-2,6-二溴苯基亚氨基)除外。 -咪唑吡啶,2-(3-乙酰氨基-2,6-二乙基苯基亚氨基)-咪唑烷,2-(3-乙酰氨基-2,6-二甲基苯基亚氨基)-咪唑烷,2-(3-乙酰氨基-2,6-二溴苯基亚氨基)-咪唑烷, 2-(3-氨基-2,6-二氯-4-甲基苯基亚氨基)-咪唑烷,2-(3-氨基-2,6-二氯-4-甲基苯基亚氨基)-咪唑烷-二盐酸盐,2-(3-氨基-2 ,6-二氯苯基亚氨基)-咪唑烷,2-(3-氨基-2,6-二氯苯基亚氨基)-咪唑烷-盐酸,2-(3-氨基-2,6-二乙基苯基亚氨基)-咪唑烷,2-(3-氨基-2 ,6-二乙基苯基亚氨基)-咪唑烷-二盐酸盐,2-(3-氨基-2,6-二甲基苯基亚氨基)-咪唑烷,2-(3-氨基-2,6-二三氟甲基苯基亚氨基)-咪唑烷,2-(3-氨基-4 -氟苯基亚氨基)-咪唑烷,2-(3-氨基-6-氯-4-甲基苯基亚氨基)-咪唑烷,2-(3-氨基-6-氯-4-甲基苯基亚氨基)-咪唑烷-二盐酸盐,2-(3-二乙基氨基-2-甲基苯基亚氨基)-咪唑烷2-(5-氨基-2,4-二溴-6-氟苯基亚氨基)-咪唑烷,2-(5-氨基-2,4-二溴苯ylimino)-咪唑烷,2-(5-Amino-2,4-dichloro-6-fluorophenylimino)-咪唑烷,2-(5-Amino-2,4-dichlorophenylimino)-咪唑烷,2-(5-Amino-2, 4-二甲基苯基亚氨基)-咪唑烷,2-(5-氨基-2-溴-4-氯-6-氟苯基亚氨基)-咪唑烷,2-(5-氨基-2-溴-4-氟苯基亚氨基)-咪唑烷,2-( 5-氨基-2-溴苯基亚氨基)-咪唑烷,2-(5-氨基-2-氯-4-氟苯基亚氨基)-咪唑烷,2-(5-氨基-2-氯苯基亚氨基)-咪唑烷,2-(5-氨基- 2-氯苯基亚氨基)-咪唑烷-盐酸,2-(5-氨基-2-甲基苯基亚氨基)-咪唑烷,2-(5-氨基-2-甲基苯基亚氨基)-咪唑烷-二盐酸盐,2-(5-氨基-4-溴- 2-氯-6-氟苯基亚氨基)-咪唑烷被认为是新的。

著录项

  • 公开/公告号IL117956B

    专利类型

  • 公开/公告日2001-11-25

    原文格式PDF

  • 申请/专利权人 BOEHRINGER INGELHEIM KG;

    申请/专利号IL117956

  • 发明设计人

    申请日1996-04-18

  • 分类号A61K31/395;A61P13/00;A61P43/00;C07D401/06;C07D403/06;C07D409/06;C07D417/06;

  • 国家 IL

  • 入库时间 2022-08-22 00:45:02

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