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11. 发明授权

US4492659A Phospholipid compound 失效
公开(公告)号：US4492659A
公开(公告)日：1985-01-08
申请号：US395954
申请日：1982-07-07
申请人： Elmar Bosies , Rudi Gall , Gunter Weimann , Uwe Bicker , Wulf Pahlke
发明人： Elmar Bosies , Rudi Gall , Gunter Weimann , Uwe Bicker , Wulf Pahlke
IPC分类号： A61K31/66 , A61P35/00 , C07F9/09 , C07F9/10 , C07F9/02
CPC分类号： C07F9/10 , C07F9/091
摘要： The present invention provides phospholipids of the general formula: ##STR1## wherein X is a valency bond, an oxygen or sulphur atom or a sulfonyl, sulfinyl, phenylene, cycloaklylene, carbonylamino, aminocarbonyl, ureido or carbonyl group, R.sub.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon radical containing up to 18 carbon atoms, which is optionally substituted one or more times by halogen, alkoxy, alkylthio, alkanesulfinyl, alkanesulfonyl, carbalkoxy or phenyl, R.sub.2 is a straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing up to 18 carbon atoms, which is optionally substituted one or more times by halogen, alkoxy, alkylthio, alkanesulphinyl, alkanesulphonyl, carbalkoxy or phenyl, Y is an oxygen atom or a --O--CO--O--, --O--CO--NH-- or --O--CS--NH-- group, R.sub.3 is a straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing 2 to 8 carbon atoms, which can also be part of a cycloalkane ring system and is optionally substituted one or more times by hydroxyl, halogen, alkylthio, alkanesulphinyl, alkanesulfonyl, nitrile, alkoxycarbonyl, carboxamido optionally substituted by alkyl radicals, cycoalkyl, optionally substituted phenyl or alkoxy, which in turn is optionally substituted by phenyl, hydroxyl, alkoxy, alkylthio, alkanesulfinyl, alkanesulfonyl, optionally acylated amino, alkoxycarbonyl, nitrile or carboxamido optionally substituted by alkyl radicals, Z is an oxygen or sulfur atom, R.sub.4 is a straight-chained or branched alkylene radical containing 2 to 5 carbon atoms and R.sub.5 is a hydrogen atom or a lower alkyl radical, with the proviso that when X is a valency bond, R.sub.1 and R.sub.2 together represent an unsubstituted, straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon chain containing up to 18 carbon atoms, Y, R.sub.4 and R.sub.5 have the above-given meanings and Z is an oxygen atom, R.sub.3 cannot be a propylene or 2-methylpropylene chain optionally substituted by hydroxyl, alkoxy or benzyloxy and with the proviso that when X is a valency bond, R.sub.1 and R.sub.2 together signify an alkyl radical containing up to 18 carbon atoms and substituted by halogen or phenyl, Y and Z are oxygen atoms and R.sub.4 and R.sub.5 have the above-given meanings, R.sub.3 cannot be a propylene or 2-hydroxypropylene chain; and the pharmacologically acceptable salts thereof.The invention also provides pharmaceutical compositions containing such compounds, having cancerostatic action without inducing thrombocyte aggregation.

12. 发明授权

US4083987A 4-Imino-1,3-diazabicyclo-(3.1.0)-hexan-2-one as a cancerostat and immuno-stimulant 失效
标题翻译： 4-甲氧基-1,3-二氮杂双环 - （3.1.0） - 己烷-2-酮作为抑制剂和免疫兴奋剂
公开(公告)号：US4083987A
公开(公告)日：1978-04-11
申请号：US690340
申请日：1976-05-26
申请人： Uwe Bicker , Wolfgang Kampe , Wolfgang Steingross
发明人： Uwe Bicker , Wolfgang Kampe , Wolfgang Steingross
IPC分类号： A61K31/396 , A61K31/415 , A61P35/00 , A61P37/04 , C07D203/26 , C07D235/02 , C07D487/04
CPC分类号： C07D487/04 , Y10S514/885
摘要： 4-Imino-1,3-diazabicyclo[3.1.0]-hexan-2-one of one or more of the tautomeric formulas ##STR1## or a physiologically compatible salt thereof exhibits cancerostatic and immuno-stimulant activity. It is produced by cyclized 1-carboxamido-2-cyanoaziridine in an anhydrous polar organic solvent in the presence of a catalytic amount of an alkali.
摘要翻译：一种或多种互变异构体式“IMAGE”或其生理上相容的盐的4-亚氨基-1,3-二氮杂双环[3.1.0] - 己烷-2-酮显示出癌症和免疫刺激活性。在无水极性有机溶剂中，在催化量的碱存在下，通过环化的1-甲酰氨基-2-氰基氮丙啶生产。

13. 发明授权

US4370323A 2-Cyanoaziridinyl-(1)-2-substituted-aziridinyl-(1)-methanes 失效
标题翻译： 2-氰基氮丙啶基 - （1）-2-取代的吖丙啶基 - （1） - 甲烷
公开(公告)号：US4370323A
公开(公告)日：1983-01-25
申请号：US776068
申请日：1977-03-09
申请人： Wolfgang Kampe , Max Thiel , Erich Fauland , Uwe Bicker , Gottfried Hebold
发明人： Wolfgang Kampe , Max Thiel , Erich Fauland , Uwe Bicker , Gottfried Hebold
IPC分类号： C07D203/06 , A61K31/395 , A61K31/396 , A61K31/435 , A61P35/00 , A61P37/04 , C07D203/08 , C07D203/12 , C07D203/14 , C07D333/00 , C07D335/00 , C07D403/14 , C07D405/14 , C07D409/14 , C07D451/14 , C07D403/06 , C07D401/14
CPC分类号： C07D203/08 , C07D451/14 , Y10S514/885
摘要： A 2-cyanoaziridinyl-(1)-2-substituted-aziridinyl-(1)-methane ##STR1## wherein R is a nitrile or carbamoyl group, andR.sub.1 and R.sub.2 each independently is a hydrogen atom, an aliphatic hydrocarbon radical containing up to 10 carbon atoms optionally substituted by hydroxyl, alkoxy, amino, alkylamino, dialkylamino, alkoxycarbonyl, cyano, 1, 2 or 3 halogens, cycloalkyl, phenyl or phenoxy; nitrile, carboxyl, alkoxycarbonyl or optionally hydrogenated monocyclic heteroaryl or phenyl optionally substituted by alkyl, alkoxy, hydroxy, alkoxcarbonyl, dialkylamino, alkylthio, trifluoromethyl, nitro, carbamoyl, nitrile, sulphonamido, hydroxyalkyl, methylenedioxy, or halogen; or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a ring containing up to 8 ring members of which at least one may be oxygen, sulphur, SO, SO.sub.2 NH, N-alkyl, N-acyl or N-alkoxycarbonylalkyl, and which can be substituted by alkyl, alkoxy, hydroxyl, alkylenedioxy, alkoxycarbonyl, hydroxyalkyl, alkoxycarbonylalkyl, dialkylamino, oxo or 2-cyanoaziridino groups, or can be fused to 1 or 2 benzene rings or can be bridged by alkylene radicals containing up to 3 carbon atoms.The compounds are characterized by cytostatic and immune response-stimulating activity.
摘要翻译： 2-氰基氮丙啶基 - （1）-2-取代的吖丙啶基 - （1） - 甲烷，其中R是腈或氨基甲酰基，R 1和R 2各自独立地为氢原子，含有至多任选被羟基，烷氧基，氨基，烷基氨基，二烷基氨基，烷氧基羰基，氰基，1,2或3卤素，环烷基，苯基或苯氧基取代的10个碳原子; 腈，羧基，烷氧基羰基或任选氢化的单环杂芳基或任选被烷基，烷氧基，羟基，烷氧基羰基，二烷基氨基，烷硫基，三氟甲基，硝基，氨基甲酰基，腈，磺酰胺基，羟烷基，亚甲二氧基或卤素取代的苯基。或R 1和R 2与它们所连接的碳原子一起形成含有至多8个环成员的环，其中至少一个可以是氧，硫，SO，SO 2 + L，NH，N-烷基，酰基或N-烷氧基羰基烷基，其可以被烷基，烷氧基，羟基，亚烷基二氧基，烷氧基羰基，羟基烷基，烷氧基羰基烷基，二烷基氨基，氧代或2-氰基氮丙啶基取代，或者可以与1或2个苯环稠合，或可以被含有至多3个碳原子的亚烷基。该化合物的特征在于细胞抑制和免疫应答刺激活性。

14. 发明授权

US5055290A Ciamexone as a selective immunosuppressant 失效
标题翻译：作为选择性免疫抑制剂的Ciamexone
公开(公告)号：US5055290A
公开(公告)日：1991-10-08
申请号：US198790
申请日：1988-05-25
申请人： Uwe Bicker , Wulf Pahlke
发明人： Uwe Bicker , Wulf Pahlke
IPC分类号： A61K31/44
CPC分类号： A61K31/44 , Y10S514/825 , Y10S514/866 , Y10S514/903
摘要： A method of selectively suppressing the excess immune reaction produced iatrogenically or autochthonously by administering 0.1 to 100 mg of ciamexone per kg of body weight.
摘要翻译：通过每kg体重施用0.1至100mg的赛米酮，选择性地抑制由医源性或自身产生的过量免疫反应的方法。

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