公开(公告)号：US4517183A

公开(公告)日：1985-05-14

申请号：US495548

申请日：1983-05-17

申请人： Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

发明人： Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

IPC分类号： A61K31/395 ,  A61K31/396 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/505 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  C07D203/22 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

CPC分类号： C07D203/22 ,  Y10S514/885

摘要： The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino or isothioureido radical, or R is a cycloalkyl or cycloalkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally bridged, or is an aryl or hetaryl radical which can be substituted one or more times by halogen, alkoxy, alkyl, hydroxyl, alkoxycarbonyl, carbamoyl, dialkylamino, cycloalkylamino, acylamino, nitro, cyano, acyl, alkylthio, alkylsulphinyl, alkylsulphonyl, sulphamoyl, phenyl, trifluoromethyl, aryloxy, acyloxy or methylenedioxy radicals and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds. Furthermore, the present invention is concerned with the use of the compounds of general formula (I') and of the pharmacologically acceptable salts thereof for combating diseases associated with a weakening of the immune system.

公开(公告)号：US4397848A

公开(公告)日：1983-08-09

申请号：US236375

申请日：1981-02-20

申请人： Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

发明人： Elmar Bosies ,  Wolfgang Kampe ,  Max Thiel ,  Uwe Bicker ,  Dietmar Boerner

IPC分类号： A61K31/395 ,  A61K31/396 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/505 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  C07D203/22 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

CPC分类号： C07D203/22 ,  Y10S514/885

摘要： The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, or an optionally substituted aliphatic hydrocarbon radical or cycloalkyl or cycloalkenyl radical, and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds. Furthermore, the present invention is concerned with the use of the compounds of general formula (I') and of the pharmacologically acceptable salts thereof for combating diseases associated with a weakening of the immune system.

摘要翻译： 本发明提供含有下列通式的N-取代的氮丙啶-2-羧酸衍生物的药物组合物：其中X是羧基，氰基，烷氧基羰基或任选取代的氨基甲酰基，R是 氢原子或任选取代的脂族烃基或环烷基或环烯基，R 1为氢原子或烷基或苯基; 和其药学上可接受的盐，与药物稀释剂或载体混合。 本发明还提供了作为新化合物的通式（I'）的N-取代的氮丙啶-2-羧酸衍生物，但条件是当X是氨基甲酰基或烷氧基羰基并且R 1是氢原子时，R不是 甲基，乙基，异丙基或苄基; 及其药理学上可接受的盐，也提供制备这些新化合物的方法。 此外，本发明涉及通式（I'）的化合物及其药理学上可接受的盐在与免疫系统的弱化相关的疾病中的用途。

公开(公告)号：US5369119A

公开(公告)日：1994-11-29

申请号：US26210

申请日：1993-03-02

申请人： Dieter Herrmann ,  Rainer Haag ,  Elmar Bosies ,  Uwe Bicker ,  Wolfgang Kampe

发明人： Dieter Herrmann ,  Rainer Haag ,  Elmar Bosies ,  Uwe Bicker ,  Wolfgang Kampe

IPC分类号： A61K31/505 ,  A61K31/415

CPC分类号： A61K31/505 ,  Y10S514/885

摘要： The subject of the present invention is the use of imexon for the production of pharmaceutical compositions with an immunosuppressive action. The present invention also provides pharmaceutical compositions containing imexon and further active materials.

摘要翻译： 本发明的主题是使用imexon生产具有免疫抑制作用的药物组合物。 本发明还提供含有imexon和其它活性物质的药物组合物。

公开(公告)号：US4409236A

公开(公告)日：1983-10-11

申请号：US268964

申请日：1981-06-01

申请人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

发明人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

IPC分类号： C07D203/08 ,  A61K31/395 ,  A61K31/396 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P37/04 ,  C07D203/06 ,  C07D401/04 ,  C07D403/06 ,  C07D405/04 ,  C07D409/04 ,  C07D333/30

CPC分类号： C07D203/06 ,  Y10S514/885

摘要： Aziridine-2-carboxylic acid derivatives of the formula ##STR1## wherein X is a carboxyl, nitrile, alkoxycarbonyl or carbamoyl group, andR and R.sup.1 are various organic radicals; or pharmacologically acceptable salts thereof, exhibit marked immunostimulant activity, especially in conjunction with added chemotherapeutic agents such as a penicillin, a cephalosporin, a nitrofuran or chloramphenicol. Those compounds are new where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, but R' is not an unsubstituted alkyl radical or an alkyl radical substituted by hydroxyl, alkoxy, dialkylamino, phenyl, 4-chlorophenyl or 4-methoxyphenyl or a vinyl radical substituted by a phenyl or methyl radical, or a cycloalkyl radical, a phenyl, a 4-chlorophenyl, a 4-methoxyphenyl, an s-triazinyl or a pyridinyl radical; or where X is a carbamoyl group and R.sub.1 is a hydrogen atom, R' is not an unsubstituted cyclohexyl, alkyl or benzyl radical; or where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a phenyl radical, R' is not an isopropyl, cyclohexyl, phenyl, benzyl or p-chlorobenzyl radical; or where R.sub.1 is a methyl radical, R.sup.1 is not a benzyl, p-chloro- or p- methoxybenzyl radical.

摘要翻译： 其中X是羧基，腈，烷氧基羰基或氨基甲酰基，R和R 1是各种有机基团; 或其药理学上可接受的盐具有显着的免疫刺激活性，特别是与添加的化学治疗剂如青霉素，头孢菌素，硝基呋喃或氯霉素结合使用。 那些化合物是新的，其中X是氰基或烷氧基羰基，R 1是氢原子，但R'不是未取代的烷基或被羟基，烷氧基，二烷基氨基，苯基，4-氯苯基或4- 甲氧基苯基或被苯基或甲基取代的乙烯基，或环烷基，苯基，4-氯苯基，4-甲氧基苯基，s-三嗪基或吡啶基; 或其中X为氨基甲酰基，R 1为氢原子，R'为未取代的环己基，烷基或苄基; 或其中X为氰基或烷氧基羰基，R 1为苯基，R'不为异丙基，环己基，苯基，苄基或对氯苄基; 或其中R 1是甲基，R 1不是苄基，对氯或对甲氧基苄基。

公开(公告)号：US4321194A

公开(公告)日：1982-03-23

申请号：US59863

申请日：1979-07-23

申请人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

发明人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

IPC分类号： C07D203/08 ,  A61K31/395 ,  A61K31/396 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P37/04 ,  C07D203/06 ,  C07D401/04 ,  C07D403/06 ,  C07D405/04 ,  C07D409/04 ,  C07D203/10 ,  C07D203/12 ,  C07D203/14

CPC分类号： C07D203/06 ,  Y10S514/885

摘要： Aziridine-2-carboxylic acid derivatives of the formula ##STR1## wherein X is a carboxyl, nitrile, alkoxycarbonyl or carbamoyl group, andR and R.sup.1 are various organic radicals, or pharmacologically acceptable salts thereof, exhibit marked immunostimulant activity, especially in conjunction with added chemotherapeutic agents such as a penicillin, a cephalosporin, a nitrofuran or chloramphenicol. Those compounds are new where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, but R' is not an unsubstituted alkyl radical or an alkyl radical substituted by hydroxyl, alkoxy, dialkylamino, phenyl, 4-chlorophenyl or 4-methoxyphenyl or a vinyl radical substituted by a phenyl or methyl radical, or a cycloalkyl radical, a phenyl a 4-chlorophenyl, a 4-methoxyphenyl, an s-triazinyl or a pyridinyl radical; or where X is a carbamoyl group and R.sub.1 is a hydrogen atom, R' is not an unsubstituted cyclohexyl, alkyl or benzyl radical; or where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a phenyl radical, R' is not an isopropyl, cyclohexyl, phenyl, benzyl or p-chlorobenzyl radical; or where R.sub.1 is a methyl radical, R.sup.1 is not a benzyl, p-chloro- or p- methoxybenzyl radical.

摘要翻译： 其中X是羧基，腈，烷氧基羰基或氨基甲酰基的氮杂环丁烷-2-羧酸衍生物，R和R 1是各种有机基团或其药理学上可接受的盐，具有显着的免疫刺激活性，特别是与 添加化学治疗剂如青霉素，头孢菌素，硝基呋喃或氯霉素。 那些化合物是新的，其中X是氰基或烷氧基羰基，R 1是氢原子，但R'不是未取代的烷基或被羟基，烷氧基，二烷基氨基，苯基，4-氯苯基或4- 甲氧基苯基或被苯基或甲基取代的乙烯基，或环烷基，苯基，4-氯苯基，4-甲氧基苯基，s-三嗪基或吡啶基; 或其中X为氨基甲酰基，R 1为氢原子，R'为未取代的环己基，烷基或苄基; 或其中X为氰基或烷氧基羰基，R 1为苯基，R'不为异丙基，环己基，苯基，苄基或对氯苄基; 或其中R 1是甲基，R 1不是苄基，对氯或对甲氧基苄基。

公开(公告)号：US4410532A

公开(公告)日：1983-10-18

申请号：US334614

申请日：1981-12-28

申请人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

发明人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

IPC分类号： C07D203/08 ,  A61K31/395 ,  A61K31/396 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P37/04 ,  C07D203/06 ,  C07D401/04 ,  C07D403/06 ,  C07D405/04 ,  C07D409/04 ,  C07D213/36

CPC分类号： C07D203/06 ,  Y10S514/885

摘要： A 2-cyanaziridine derivative of the formula ##STR1## wherein R' is a straight-chained or branched, saturated or mono- or polyunsaturated aliphatic hydrocarbon radical with up to 8 carbon atoms, which is substituted by an aromatic nitrogen-containing heterocyclic radical with 5 or 6 ring-members and 1, 2 or 3 nitrogen atoms optionally substituted by halogen, alkoxy with up to 8 carbon atoms, alkyl with up to 8 carbon atoms, hydroxyl, carbalkoxy with up to 9 carbon atoms, carbamoyl, dialkylamino the alkyl moieties of which having up to 8 carbon atoms, cycloalkylamino, the cycloalkyl moiety having 3-10 carbon atoms, acetylamino, nitro, cyano, acetyl, alkylthio with up to 8 carbon atoms, alkylsulphinyl with up to 8 carbon atoms, alkylsulphonyl with up to 8 carbon atoms, sulphamoyl, phenyl, trifluoromethyl, phenoxy, acetoxy or methylenedioxy;or a pharmacologically acceptable salt thereof, exhibits immune stimulating activity.

摘要翻译： 具有式“IMAGE”的2-氰基氮丙啶衍生物，其中R'是具有至多8个碳原子的直链或支链，饱和或单或多不饱和脂族烃基，其被含芳族含氮杂环基团取代， 5或6个环成员和1,2或3个任选被卤素取代的氮原子，具有至多8个碳原子的烷氧基，至多8个碳原子的烷基，羟基，至多9个碳原子的烷氧基，氨基甲酰基，二烷基氨基烷基 其具有至多8个碳原子的部分，环烷基氨基，具有3-10个碳原子的环烷基部分，乙酰氨基，硝基，氰基，乙酰基，具有至多8个碳原子的烷硫基，具有至多8个碳原子的烷基亚磺酰基，烷基磺酰基， 8个碳原子，氨磺酰基，苯基，三氟甲基，苯氧基，乙酰氧基或亚甲二氧基; 或其药理学上可接受的盐显示免疫刺激活性。

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。

公开(公告)号：US4376731A

公开(公告)日：1983-03-15

申请号：US859633

申请日：1978-01-31

申请人： Elmar Bosies ,  Ruth Heerdt ,  Rudi Gall ,  Uwe Bicker ,  Anna E. Ziegler

发明人： Elmar Bosies ,  Ruth Heerdt ,  Rudi Gall ,  Uwe Bicker ,  Anna E. Ziegler

IPC分类号： C07D203/20 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/395

CPC分类号： C07D403/12 ,  C07D203/20 ,  C07D405/12 ,  C07D409/12

摘要： 2-Substituted-1-aziridine-carboxylic acid esters exhibiting immuno-stimulant activity and of the formula ##STR1## wherein X is a carbamoyl or alkoxycarbonyl radical, andR.sup.1 is an aliphatic hydrocarbon radical optionally substituted by halogen, alkoxy, amino, carbamoyloxy, cycloalkyl, hydroxyl, an imido or heterocyclic radical, cycloalkyl; or aryl, aralkyl, aryloxyalkyl or arylthioalkyl wherein the aryl moiety is optionally substituted by halogen, alkyl, alkoxy, hydroxyl, amino, nitro, cyano, acyl, carbalkoxy, thioalkyl, alkylsulphonyl, phenyl or trifluoromethyl. Counterparts where X is --CN and R.sup.1 is as above, except for ethyl, are also new.

摘要翻译： 2-取代的1-氮丙啶 - 羧酸酯，其具有免疫刺激活性，并且具有下式：其中X是氨基甲酰基或烷氧基羰基，R1是任选被卤素，烷氧基，氨基，氨基甲酰氧基取代的脂族烃基， 环烷基，羟基，亚氨基或杂环基，环烷基; 芳基，芳烷基，芳氧基烷基或芳硫基烷基，其中芳基部分任选被卤素，烷基，烷氧基，羟基，氨基，硝基，氰基，酰基，烷氧基，硫代烷基，烷基磺酰基，苯基或三氟甲基取代。 对应物，其中X为-CN和R1如上所述，除乙基以外，也是新的。

公开(公告)号：US4444766A

公开(公告)日：1984-04-24

申请号：US311830

申请日：1981-10-16

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： A61K31/661 ,  C07F9/09 ,  C07F9/10 ,  C07F9/165 ,  A61K31/095 ,  A61K31/66

CPC分类号： C07F9/091 ,  C07F9/10 ,  C07F9/1651

摘要： Sulfur-containing phospholipid compounds of the formula ##STR1## pharmaceutical compositions having anti-tumor activity which include said phospholipid compounds, and the method of use for combating tumors, of said phospholipid compounds.

摘要翻译： 所述磷脂化合物的具有抗肿瘤活性的包含所述磷脂化合物的药物组合物和用于对抗肿瘤的方法的含硫磷脂化合物。

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.