公开(公告)号：US4245100A

公开(公告)日：1981-01-13

申请号：US855246

申请日：1977-11-28

申请人： Leonid E. Kholodov ,  Vladimir G. Yashunsky ,  Roald A. Altshuler ,  Mikhail D. Mashkovsky ,  Valentina V. Ogorodnikova ,  Zoya A. Olovyanishnikova ,  Anna S. Vitvitskaya ,  Valery A. Parshin ,  Ekaterina A. Kelekhsaeva

发明人： Leonid E. Kholodov ,  Vladimir G. Yashunsky ,  Roald A. Altshuler ,  Mikhail D. Mashkovsky ,  Valentina V. Ogorodnikova ,  Zoya A. Olovyanishnikova ,  Anna S. Vitvitskaya ,  Valery A. Parshin ,  Ekaterina A. Kelekhsaeva

IPC分类号： C07D271/04 ,  A61K31/42

CPC分类号： C07D271/04

摘要： N-acyl sydnonimines of the formula: ##STR1## wherein R is phenyl, .beta.-phenylethyl, dl-.alpha.-methyl-.beta.-phenylethyl or l-.alpha.-methyl-.beta.-phenylethyl; R' is hydrogen, phenyl; X is a lower alkyl, phenyl, ##STR2## wherein R" is hydrogen, a halogen, a lower fluorinated alkyl; R'" is hydrogen, a halogen, a lower alkyl; when R is dl-.alpha.-methyl-.beta.-phenylethyl, R' is H, R" is Cl, R'" is only Cl, while when R' is H, X is NHC.sub.6 H.sub.5 R is only l-.alpha.-methyl-.beta.-phenylethyl; when X is phenyl, R and R' are each phenyl only.The method for preparing sydnonimine N-acylderivatives comprises reacting N-nitrosoderivatives of N-substituted nitriles of .alpha.-aminoacids of the formula: ##STR3## wherein R is phenyl, .beta.-phenylethyl, di-.alpha.-methyl-.beta.-phenylethyl or l-.alpha.-methyl-.beta.-phenylethyl; R' is H, phenyl; when R' is phenyl R is phenyl only, with an acylation agent in a solvent medium in the presence of a basic-character catalyst, followed by isolation of the desired product.

摘要翻译： 其中R为苯基，β-苯乙基，dl-α-甲基-β-苯乙基或1-α-甲基-β-苯基乙基的N-酰基次磺酰亚胺：其中R为苯基， R'是氢，苯基; X是低级烷基，苯基，其中R“是氢，卤素，低级氟化烷基; R“'是氢，卤素，低级烷基; 当R是dl-α-甲基-β-苯基乙基时，R'是H，R“是Cl，R”'仅为Cl，而当R'是H时，X是NHC 6 H 5 R只是1-α-甲基 β-苯乙基; 当X是苯基时，R和R'各自为苯基。 制备sydnonimine N-酰基衍生物的方法包括使下式的α-氨基酸的N-取代腈的N-亚硝基衍生物：其中R是苯基，β-苯乙基，二 - α-甲基-β-苯乙基或1- α-甲基-β-苯乙基; R'是H，苯基; 当R'是苯基时，R仅为苯基，与酰基化剂在溶剂介质中，在碱性字符催化剂存在下，然后分离所需产物。

公开(公告)号：US4088647A

公开(公告)日：1978-05-09

申请号：US746688

申请日：1976-12-02

申请人： Robert G. Glushkov ,  Mikhail D. Mashkovsky ,  Nataiia I. Andreeva ,  Serafima S. Liberman ,  Leonid N. Gerchikov ,  Vera A. Volskova ,  Antonida V. Zaitseva ,  Onisim J. Magidson, deceased ,  by Galina K. Magidson ,  by July O. Magidson, administrators

发明人： Robert G. Glushkov ,  Mikhail D. Mashkovsky ,  Nataiia I. Andreeva ,  Serafima S. Liberman ,  Leonid N. Gerchikov ,  Vera A. Volskova ,  Antonida V. Zaitseva ,  Onisim J. Magidson, deceased ,  by Galina K. Magidson ,  by July O. Magidson, administrators

IPC分类号： C07D471/04 ,  C07D471/16 ,  C07D487/04 ,  C07D487/16 ,  C07D471/14

CPC分类号： C07D471/04 ,  C07D487/04

摘要： New tetracyclic compounds, containing indole nucleus in their structure, having the general formula ##STR1## where R is hydrogen, alkyl, or alkoxyl, R' is an alkyl, and m and n are 2 or 3.The said compounds react with organic and mineral acids to form salts readily soluble in water.The method for preparing the said compounds consists in cyclization of lactams, having the general formula ##STR2## where R, R', m and n are as specified above, or of their hydrochlorides by phosphorus oxychloride.

摘要翻译： 在其结构中含有吲哚核的新的四环化合物，具有通式“IMAGE”，其中R是氢，烷基或烷氧基，R'是烷基，m和n是2或3。

公开(公告)号：US4876360A

公开(公告)日：1989-10-24

申请号：US333349

申请日：1989-04-05

申请人： Vladimir G. Granik ,  Tatyana V. Stezhko ,  Robert G. Glushkov ,  Mikhail D. Mashkovsky ,  Lidia F. Roschina ,  Antonina I. Polezhaeva ,  Roza B. Parimbetova ,  Jury G. Bobkov ,  Alexandr S. Losev ,  Irina A. Ivanova

发明人： Vladimir G. Granik ,  Tatyana V. Stezhko ,  Robert G. Glushkov ,  Mikhail D. Mashkovsky ,  Lidia F. Roschina ,  Antonina I. Polezhaeva ,  Roza B. Parimbetova ,  Jury G. Bobkov ,  Alexandr S. Losev ,  Irina A. Ivanova

IPC分类号： C07D207/24

CPC分类号： C07D207/24

摘要： A novel compound, namely, 1-thiocarbamylmethylpyrrolidine-2-thione has the following formula: ##STR1## A process for preparing said compound comprises reacting a derivative of pyrrolidone-2 of the general formula: ##STR2## wherein R is nitrile or carbamoyl, with phosphorus pentasulphide in an inert non-polar solvent at a temperature above room temperature, followed by treatment of the resulting precipitate with water upon boiling and isolation of the desired product.The compound according to the present invention exhibits antihypoxic and nootropic activity.

摘要翻译： 一种新化合物，即1-硫代氨基甲酰基甲基吡咯烷-2-硫酮具有下列结构式：制备所述化合物的方法包括使下列通式的吡咯烷酮-2的衍生物：其中R是腈或氨基甲酰基， 在惰性非极性溶剂中，在高于室温的温度下加入五硫化二磷，然后在沸腾并分离所需产物后用水处理所得沉淀。 根据本发明的化合物显示出抗低氧和向异性活性。

公开(公告)号：US4839380A

公开(公告)日：1989-06-13

申请号：US198999

申请日：1988-04-04

申请人： Vladimir G. Granik ,  Tatyana V. Stezhko ,  Robert G. Glushkov ,  Mikhail D. Mashkovsky ,  Lidia F. Roschina ,  Antonina I. Polezhaeva ,  Roza B. Parimbetova ,  Jury G. Bobkov ,  Alexandr S. Losev ,  Irina A. Ivanova

发明人： Vladimir G. Granik ,  Tatyana V. Stezhko ,  Robert G. Glushkov ,  Mikhail D. Mashkovsky ,  Lidia F. Roschina ,  Antonina I. Polezhaeva ,  Roza B. Parimbetova ,  Jury G. Bobkov ,  Alexandr S. Losev ,  Irina A. Ivanova

IPC分类号： C07D207/00 ,  A61K31/40 ,  A61P21/00 ,  A61P25/28 ,  C07D207/24

CPC分类号： C07D207/24

摘要： A novel compound, namely, 1-thiocarbamylmethylpyrrolidine-2-thione has the following formula: ##STR1## A process for preparing said compound comprises reacting a derivative of pyrrolidone-2 of the general formula: ##STR2## wherein R is nitrile or carbamoyl, with phosphorus pentasulphide in an inert non-polar solvent at a temperature above room temperature, followed by treatment of the resulting precipitate with water upon boiling and isolation of the desired product.The compound according to the present invention exhibits antihypoxic and nootropic activity.

摘要翻译： PCT No.PCT / SU86 / 00080 Sec。 371日期：1988年4月4日 102（e）日期1988年4月4日PCT提交1986年8月25日PCT公布。 出版物WO88 / 01620 日期：1988年3月10日。一种新化合物，即1-硫代氨基甲酰基甲基吡咯烷-2-硫酮具有下式：其中制备所述化合物的方法包括使通式如下的吡咯烷酮-2的衍生物： 其中R是腈或氨基甲酰基，在惰性非极性溶剂中，在高于室温的温度下加入五硫化二磷，随后在沸腾和分离所需产物时用水处理所得沉淀。 根据本发明的化合物显示出抗低氧和向异性活性。