公开(公告)号：US4308278A

公开(公告)日：1981-12-29

申请号：US90450

申请日：1979-11-01

申请人： Geza Schneider ,  Ferenc Andrasi ,  Pal Berzsenyi ,  Arpad Lazar ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

发明人： Geza Schneider ,  Ferenc Andrasi ,  Pal Berzsenyi ,  Arpad Lazar ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

IPC分类号： A61K31/415 ,  A61K31/4166 ,  A61P1/00 ,  A61P3/04 ,  C07C45/71 ,  C07D233/32 ,  C07D233/34 ,  C07D233/38 ,  C07D233/78

CPC分类号： C07C255/00 ,  C07C45/71 ,  C07D233/32 ,  C07D233/38 ,  C07D233/78 ,  Y10S514/91

摘要： 4-[(3,4-Dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives having the formula I ##STR1## wherein R.sup.1 stands for a cycloalkyl group containing from 3 to 6 carbon atoms or benzyl group;R.sup.2 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.3 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.4 stands for hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms or an alkoxycarbonyl group containing from 1 to 4 carbon atoms; andR.sup.5 stands for hydrogen atom or an alkoxycarbonyl group containing from 1 to 4 carbon atoms,are prepared by(a) reducing a hydantoin derivative having the general formula II, wherein R.sup.1 and R.sup.2 are as defined above, with lithium aluminum hydride in a neutral organic solvent, or(b) hydrogenating catalytically an 1,3-dihydro-2H-imidazol-2-one derivative having the general formula III, wherein R.sup.1 and R.sup.3 are as defined above, while the meaning of R.sup.4 is hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, or(c) reacting a carbamate derivative having the general formula IV, wherein R.sup.1 is as defined above, while R.sup.6 stands for an alkyl group containing from 1 to 4 carbon atoms, with an organic or inorganic base.The compounds having the formula I possess valuable therapeutical properties, mainly anorexigenic activity.

摘要翻译： 4 - [（3,4-二烷氧基苯基）烷基] -2-咪唑啉酮衍生物，其具有式I其中R1代表含有3至6个碳原子的环烷基或苄基; R2代表氢原子或含有1至4个碳原子的烷基; R3代表氢原子或含有1至4个碳原子的烷基; R4表示氢原子或含有1至4个碳原子的烷基或含有1至4个碳原子的烷氧基羰基; 并且R5代表氢原子或含有1至4个碳原子的烷氧基羰基，是通过以下步骤制备的：（a）将具有通式II的乙内酰脲衍生物（其中R 1和R 2如上定义）与中性的氢化铝锂 有机溶剂，或（b）催化氢化具有通式III的1,3-二氢-2H-咪唑-2-酮衍生物，其中R 1和R 3如上所定义，而R 4的含义是氢原子或烷基 含有1至4个碳原子的基团，或（c）使具有通式IV的氨基甲酸酯衍生物与其中R 1如上定义，而R6代表含有1至4个碳原子的烷基，与有机或无机 基础。 具有式I的化合物具有有价值的治疗性质，主要是厌食症活性。

公开(公告)号：US4579954A

公开(公告)日：1986-04-01

申请号：US604385

申请日：1984-04-27

申请人： Kalman Harsanyi ,  Gyorgy Domany ,  Oszkar Fuchs ,  Lajos Toldy ,  Gyorgy Fekete ,  Endre Kasztreiner ,  Bela Hegedus ,  Ferenc Morasz ,  Andras Rado ,  Tibor Lang ,  Arpad Lazar ,  Eva Csongor ,  Tibor Balogh ,  Janos Borvendeg ,  Jozsef Reiter ,  Tibor Somogyi ,  Margit Bidlo nee Igloy

发明人： Kalman Harsanyi ,  Gyorgy Domany ,  Oszkar Fuchs ,  Lajos Toldy ,  Gyorgy Fekete ,  Endre Kasztreiner ,  Bela Hegedus ,  Ferenc Morasz ,  Andras Rado ,  Tibor Lang ,  Arpad Lazar ,  Eva Csongor ,  Tibor Balogh ,  Janos Borvendeg ,  Jozsef Reiter ,  Tibor Somogyi ,  Margit Bidlo nee Igloy

IPC分类号： A61K31/415 ,  A61P1/04 ,  C07D233/54 ,  C07D233/64

CPC分类号： C07D233/64

摘要： The invention relates to the new monohydrate of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine (cimetidine), a histamine-H.sub.2 receptor antagonist which is called N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine H (cimetidine H) as well as to a process for the preparation of same, which comprises pouring a hot, homogeneous aqueous solution of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine, optionally containing also methylamine, onto ice and separating the N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidine monohydrate.

摘要翻译： 本发明涉及N-甲基-N' - {2 - [（5-甲基咪唑-4-基） - 甲硫基] - 乙基} -N' - 氰基胍（西咪替丁），组胺-H 2受体 称为N-甲基-N' - {2 - [（5-甲基咪唑-4-基） - 甲硫基] - 乙基} -N'-氰基胍脒H（西咪替丁H）的方法以及 其包括将热的均匀的N-甲基-N' - {2 - [（5-甲基咪唑-4-基） - 甲硫基] - 乙基} -N“ - 氰基胍的水溶液，任选地含有 并将甲胺加到冰上并分离N-甲基-N' - {2 - [（5-甲基咪唑-4-基） - 甲硫基] - 乙基} -N'-氰基胍一水合物。