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1. 发明授权

US4409236A N-Substituted aziridine-2-carboxylic acid derivatives and immuno-stimulation composition and method 失效
标题翻译： N-取代的氮丙啶-2-羧酸衍生物和免疫刺激组合物和方法
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。

2. 发明授权

US4321194A N-Substituted aziridine-2-carboxylic acid derivatives for immuno stimulation 失效
标题翻译： N-取代的氮丙啶-2-羧酸衍生物用于免疫刺激
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。

3. 发明授权

US4410532A N-Substituted aziridine-2-carboxylic acid derivatives and their immuno-stimulation compositions and methods 失效
标题翻译： N-取代的氮丙啶-2-羧酸衍生物及其免疫刺激组合物和方法
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。

4. 发明授权

US5369119A Use of imexon as an immune suppressive and pharmaceutical compositions containing imexon 失效
标题翻译：使用imexon作为免疫抑制剂和含有imexon的药物组合物
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。

5. 发明授权

US4397848A N-Substituted aziridine-2-carboxylic acid immunostimulant derivatives 失效
标题翻译： N-取代的氮丙啶-2-羧酸免疫刺激剂衍生物
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。

6. 发明授权

US4517183A N-Substituted aziridine-2-carboxylic acid derivatives 失效
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.

7. 发明授权

US4376731A 1-Aziridine carboxylic acid derivatives with immunostimulant activity 失效
标题翻译：具有免疫刺激活性的1-氮杂环丁烷羧酸衍生物
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。

8. 发明授权

US4444766A Sulfur-containing phospholipid compounds and therapeutic compositions 失效
标题翻译：含硫磷脂化合物和治疗组合物
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。

9. 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.

10. 发明授权

US5627170A Phosphonic acid compound containing heterocyclic substituents, pharmaceutical composition contains same and a method of treating calcium metabolism disturbance 失效
标题翻译：含有杂环取代基的膦酸化合物，药物组合物含有相同的治疗钙代谢紊乱的方法
公开(公告)号：US5627170A
公开(公告)日：1997-05-06
申请号：US465360
申请日：1995-06-05
申请人： Christos Tsaklakidis , Elmar Bosies , Angelika Esswein , Frieder Bauss
发明人： Christos Tsaklakidis , Elmar Bosies , Angelika Esswein , Frieder Bauss
IPC分类号： A61K31/66 , A61K31/662 , A61K31/675 , A61P3/00 , A61P3/14 , C07F9/38 , C07F9/40 , C07F9/553 , C07F9/572 , C07F9/58 , C07F9/6506 , C07F9/6509 , A61K31/40 , C07D203/08 , C07D205/04 , C07D207/06
CPC分类号： C07F9/65062 , C07F9/3808 , C07F9/4006 , C07F9/5532 , C07F9/5721 , C07F9/5722 , C07F9/582 , C07F9/65061
摘要： Compounds of the formula I ##STR1## in which R signifies a possibly substituted amino group of the general formula --NR.sup.1 R.sup.2, whereby, independently of one another, R.sup.1 and R.sup.2 each signify hydrogen, lower alkyl, lower alkenyl or lower alkynyl or R represents a saturated, unsaturated or aromatic heterocyclic ring which can possibly be substituted once or twice by lower alkyl or halogen, alk signifies a valency bond, a methylene, a saturated or unsaturated, straight-chained or branched alkylene chain with 2-6 carbon atoms and R.sup.3, R.sup.4 and R.sup.5, in each case independently of one another, signify hydrogen, lower alkyl or benzyl, as well as their pharmacologically acceptable salts and enantiomers, whereby, for the case that R.sup.3 =R.sup.4 =R.sup.5 =CH.sub.3 and alk signifies a valency bond, R cannot be the dimethylamino group, processes for their preparation and medicaments which contain these compounds for the treatment of calcium metabolism diseases.
摘要翻译：其中R表示通式-NR1R2的可能取代的氨基的式I化合物（I），其中R 1和R 2各自独立地表示氢，低级烷基，低级烯基或低级炔基或 R表示可以被低级烷基或卤素取代一次或两次的饱和，不饱和或芳族杂环，alk表示具有2-6碳的价键，亚甲基，饱和或不饱和的直链或支链亚烷基链原子和R 3，R 4和R 5在每种情况下彼此独立地表示氢，低级烷基或苄基，以及它们的药理学上可接受的盐和对映异构体，其中在R3 = R4 = R5 = CH3且alk表示化合键，R不能是二甲基氨基，其制备方法和含有这些化合物用于治疗钙代谢疾病的药物。

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