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1. 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。

2. 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.

3. 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。

4. 发明授权

US4136197A Hypoglycaemically and hypolipidaemically effective n-substituted carboxylic acid amides 失效
标题翻译：高效和高效的N-取代的羧酸酰胺
公开(公告)号：US4136197A
公开(公告)日：1979-01-23
申请号：US785255
申请日：1977-04-06
申请人： Manfred Hubner , Ruth Heerdt , Elmar Bosies , Hans Kuhnle , Felix H. Schmidt
发明人： Manfred Hubner , Ruth Heerdt , Elmar Bosies , Hans Kuhnle , Felix H. Schmidt
IPC分类号： A61K31/16 , A61K31/165 , A61K31/195 , A61K31/215 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/55 , A61P3/08 , C07C233/12 , C07C233/60 , C07C233/63 , C07D311/82 , C07D311/84 , C07D311/90 , C07D313/12 , C07D335/12 , C07D335/20 , C07D337/12 , C07C63/44
CPC分类号： C07D335/20 , A61K31/165 , C07C233/12 , C07D311/82 , C07D311/84 , C07D311/90 , C07D313/12 , C07D335/12 , C07D337/12 , C07C2103/18 , Y10S514/884
摘要： An N-substituted carboxylic acid amide of the formula ##STR1## wherein A is a valency bond or an oxygen or sulphur atom or a methylene, ethylene, vinylene, ethyleneoxa or ethylenethia radical,V is a trivalent hydrocarbon radical containing up to 4 carbon atoms,R.sub.1 and R.sub.2 each independently is hydrogen, a halogen atom, a hydroxyl group or an alkyl or alkoxy radical,R.sub.3 is hydrogen, a hydroxyl group or an alkoxy radical,Y is an alkylene radical containing up to 3 carbon atoms,X is a valency bond or a divalent aliphatic hydrocarbon radical containing up to 6 carbon atoms, andD is a hydroxymethyl, formyl, free or esterified carboxyl or an N-substituted carbamoyl radical, or a physiologically compatible salt thereof, characterized by hypoglycaemic and hypolipidaemic activity.

5. 发明授权

US4719203A Diphosphonic acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：二膦酸衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4719203A
公开(公告)日：1988-01-12
申请号：US930331
申请日：1986-11-12
申请人： Elmar Bosies , Rudi Gall
发明人： Elmar Bosies , Rudi Gall
IPC分类号： A61K31/665 , A61K31/66 , A61P3/00 , A61P3/02 , A61P3/14 , C07F9/38 , C07F9/40 , A61K31/045 , A61K31/13 , A61K31/185
CPC分类号： C07F9/405 , C07F9/3873
摘要： Diphosphonate compounds, processes for their preparation and pharmaceutical compositions containing them and being useful for treating calcium metabolism disorders. The diphosphonates are of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, acyl or alkyl which can be substituted by aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl or R.sub.3 and R.sub.4 together represent lower alkylene, R.sub.5 is a hydrogen atom or alkyl, X is a valency bond or alkylene, Y is a valency bond, alkylene or substituted alkylene, Z is hydrogen, hydroxyl or amino group optionally substituted by alkyl and n is 1, 2 or 3; and including the pharmacologically acceptable salts thereof.
摘要翻译：二膦酸酯化合物，其制备方法和含有它们的药物组合物，并且可用于治疗钙代谢紊乱。二膦酸酯具有下式（I）其中R 1和R 2是氢，可被芳基取代的酰基或烷基，R 3和R 4是氢或烷基或R 3和R 4一起代表低级亚烷基，R 5是氢原子或烷基，X是价键或亚烷基，Y是价键，亚烷基或取代的亚烷基，Z是氢，任选被烷基取代的羟基或氨基，n是1,2或3; 并包括其药理学上可接受的盐。

6. 发明授权

US4927814A Diphosphonate derivatives, pharmaceutical compositions and methods of use 失效
标题翻译：二膦酸衍生物，药物组合物和使用方法
公开(公告)号：US4927814A
公开(公告)日：1990-05-22
申请号：US71471
申请日：1987-07-09
申请人： Rudi Gall , Elmar Bosies
发明人： Rudi Gall , Elmar Bosies
IPC分类号： A61K31/66 , A61P3/00 , A61P3/14 , A61P29/00 , A61P43/00 , C07F9/38 , C07F9/40
CPC分类号： C07F9/405 , C07F9/3873
摘要： The present invention provides disphosphonates of the general formula: ##STR1## wherein R.sub.1 is a straight-chain or branched, saturated or unsaturated aliphatic hydrocarbon radical of 1-9 carbon atoms which is optionally substituted by phenyl or cyclohexyl, R.sub.2 is cyclohexyl or cyclohexylmethyl, benzyl or a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon of 4 to 18 carbon atoms which is optionally substituted by phenyl or oxygen wherein the oxygen can be esterified or etherified, R.sub.3 is hydrogen or a straight-chain or branched alkyl of 1-4 carbon atoms, X is a straight-chain or branched alkylene chain of 1-6 carbon atoms and Y is hydrogen, hydroxyl or an amino group optionally substituted by alkyl radicals of 1-6 carbon atoms; as well as the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these diphosphonic acid derivatives and pharmaceutical compositions containing them for the prophyllaxis treatment of diseases or disturbances of calcium metabolism such as osteoporsis, Pagets disease, Bechterew's disease, bone metastases, urolithiasis, heterotropic ossifications, rheumatoid arthritis, osteoarthritis and degenerative arthrosis.
摘要翻译：本发明提供以下通式的分解膦酸盐：其中R 1是1-9个碳原子的直链或支链，饱和或不饱和脂族烃基，其任选被苯基或环己基取代，R 2是环己基或环己基甲基，苄基或具有4至18个碳原子的直链或支链，饱和或不饱和的脂族烃，其任选被苯基或氧取代，其中氧可被酯化或醚化，R 3是氢或直链或支链 1-4个碳原子的烷基，X是1-6个碳原子的直链或支链亚烷基链，Y是氢，羟基或任选被1-6个碳原子的烷基取代的氨基; 以及其药理学上可接受的盐。本发明还提供制备这些二膦酸衍生物的方法和含有它们的药物组合物，用于预防性治疗钙代谢疾病或紊乱，例如骨质疏松症，佩吉特氏病，贝克特尔病，骨转移，尿石症，异质性骨化，类风湿性关节炎，骨关节炎和退行性关节病。

7. 发明授权

US4238506A Hypoglycaemically and hypolipidaemically active derivatives of phenyl-alkane-carboxylic acids 失效
标题翻译：苯基 - 烷烃 - 羧酸的低血糖和降血糖活性衍生物
公开(公告)号：US4238506A
公开(公告)日：1980-12-09
申请号：US920508
申请日：1978-06-29
申请人： Kurt Stach, deceased , Elmar Bosies , Ruth Heerdt , Hans-Frieder Kuhnle , Felix H. Schmidt
发明人： Kurt Stach, deceased , Elmar Bosies , Ruth Heerdt , Hans-Frieder Kuhnle , Felix H. Schmidt
IPC分类号： C07D213/82 , C07D241/24 , C07D307/79 , C07D311/66 , C07D333/38 , C07C101/42
CPC分类号： C07D213/82 , C07D241/24 , C07D307/79 , C07D311/66 , C07D333/38 , C07C2103/18
摘要： Phenyl-alkane-carboxylic acids of the formula ##STR1## wherein A is an aryl, aralkyl or arylvinyl radical optionally substituted by hydroxy, halogen, trifluoromethyl, alkyl, alkylthio, alkoxy, alkenyloxy, alkoxyalkoxy, alkyl-substituted amino, aryloxy or alkoxy-substituted aryloxy, or is an aryloxyalkyl or arylthioalkyl radical, or a heterocyclic ring system optionally substituted by halogen, alkyl or alkoxy,Y is a valency bond or an unbranched or branched lower alkylene radical containing up to 3 carbon atoms,X is a straight or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing 2 to 8 carbon atoms, there being at least 2 carbon atoms between the benzene ring and the carboxyl group, andR is a hydrogen atom or a lower alkyl radical, as well as physiologically compatible salts, esters and amides thereof, exhibit hypoglycaemic and hypolipidaemic activity.
摘要翻译：式（I）的苯基 - 烷烃 - 羧酸其中A是任选被羟基，卤素，三氟甲基，烷基，烷硫基，烷氧基，烯氧基，烷氧基烷氧基，烷基取代的氨基，芳氧基或烷氧基取代的芳氧基，或是芳氧基烷基或芳硫基烷基，或任选被卤素，烷基或烷氧基取代的杂环体系，Y是价态键或含有至多3个碳原子的无支链或支链低级亚烷基，X是含有2至8个碳原子的直链或支链，饱和或不饱和的二价脂族烃基，苯环和羧基之间至少有2个碳原子，R是氢原子或低级烷基，以及其生理上相容的盐，酯和酰胺显示出低血糖和降血脂活性。

8. 发明授权

US4113871A Hypoglycemically and hypolipidemically active derivatives of phenyl-alkane-carboxylic acids 失效
标题翻译：苯基 - 羧酸 - 羧酸的高分子和低分子活性衍生物
公开(公告)号：US4113871A
公开(公告)日：1978-09-12
申请号：US674993
申请日：1976-04-08
申请人： Kurt Stach, deceased , Elmar Bosies , Ruth Heerdt , Hans-Frieder Kuhnle , Felix Helmut Schmidt
发明人： Kurt Stach, deceased , Elmar Bosies , Ruth Heerdt , Hans-Frieder Kuhnle , Felix Helmut Schmidt
IPC分类号： C07D209/42 , A61K31/165 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/51 , C07C233/54 , C07C233/55 , C07C233/81 , C07C233/87 , C07C235/20 , C07C235/24 , C07C235/34 , C07C235/36 , C07C235/38 , C07C235/52 , C07C235/56 , C07C237/20 , C07C237/36 , C07C237/40 , C07C313/00 , C07C319/20 , C07C323/60 , C07D213/82 , C07D215/48 , C07D241/24 , C07D261/18 , C07D263/58 , C07D307/79 , C07D311/66 , C07D333/38 , A61K31/42 , A61K31/34
CPC分类号： C07D213/82 , C07D241/24 , C07D307/79 , C07D311/66 , C07D333/38 , C07C2103/18
摘要： Phenyl-alkane-carboxylic acids of the formula ##STR1## wherein A is an aryl, aralkyl or arylvinyl radical optionally substituted by hydroxy, halogen, trifluoromethyl, alkyl, alkylthio, alkoxy, alkenyloxy, alkoxyalkoxy, alkyl-substituted amino, aryloxy or alkoxy-substituted aryloxy, or is an aryloxyalkyl or arylthioalkyl radical, or a heterocyclic ring system optionally substituted by halogen, alkyl or alkoxy,Y is a valency bond or an unbranched or branched lower alkylene radical containing up to 3 carbon atoms,X is a straight or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing 2 to 8 carbon atoms, there being at least 2 carbon atoms between the benzene ring and the carboxyl group, andR is a hydrogen atom or a lower alkyl radical, as well as physiologically compatible salts, esters and amides thereof, exhibit hypoglycaemic and hypolipidaemic activity.

9. 发明授权

US4017539A Biguanide compounds and anti-diabetic compositions 失效
标题翻译：双胍化合物和抗糖尿病组合物
公开(公告)号：US4017539A
公开(公告)日：1977-04-12
申请号：US575098
申请日：1975-05-07
申请人： Elmar Bosies , Kurt Stach , Felix Helmut Schmidt , Ruth Heerdt , Helmut Weber
发明人： Elmar Bosies , Kurt Stach , Felix Helmut Schmidt , Ruth Heerdt , Helmut Weber
IPC分类号： C07C279/26 , A61K20060101 , A61K31/155 , C07C20060101 , C07C67/00 , C07C239/00 , C07C123/00
CPC分类号： C07C279/26
摘要： New biguanide compounds of the formula: ##STR1## wherein A is saturated or unsaturated cycloaliphatic hydrocarbyl, and the physiologically compatible salts thereof; display outstanding anti-diabetic effectiveness in the treatment of diabetes mellitus, without showing the typical side effects of biguanide treatment, viz., lactacidosis.
摘要翻译：新的具有下式的双胍化合物：其中A是饱和或不饱和脂环族烃基，及其生理上相容的盐; 在糖尿病治疗中显示出优异的抗糖尿病有效性，没有显示双胍治疗的典型副作用，即乳酸发生。

10. 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。

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