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1. 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.

2. 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。

3. 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。

4. 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.

5. 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。

6. 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。

7. 发明授权

US5578590A Pharmaceutical composition preparation for use in inhibiting protein kinase C 失效
标题翻译：用于抑制蛋白激酶C的药物组合物制剂
公开(公告)号：US5578590A
公开(公告)日：1996-11-26
申请号：US319478
申请日：1994-10-07
申请人： Hans H. Grunicke , Dieter Herrmann , Johann Hofmann , Elmar Bosies
发明人： Hans H. Grunicke , Dieter Herrmann , Johann Hofmann , Elmar Bosies
IPC分类号： A61K33/24 , A61K45/06 , A61P35/00 , A61K31/545 , A61K31/55 , A61K31/70 , A61K31/35
CPC分类号： A61K33/24 , A61K45/06
摘要： The present invention provides a method of inhibiting protein kinase C in a mammal having a tumor system which contains protein kinase C, which mammal is undergoing cytostatic therapy. The method comprises administering to the mammal a protein kinase C inhibitor.
摘要翻译：本发明提供了具有肿瘤系统的哺乳动物中抑制蛋白激酶C的方法，所述肿瘤系统含有哺乳动物进行细胞抑制治疗的蛋白激酶C。该方法包括向哺乳动物施用蛋白激酶C抑制剂。

8. 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。

9. 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。

10. 发明授权

US5543402A [3-(C.sub.16 -C.sub.18)-alkanesulphinyl and sulphonyl-2-methoxy-methylpropyl]-(2-trimethylammonioethyl) phosphates, processes for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译： [3-（C16-C18） - 烷基亚磺酰基和磺酰基-2-甲氧基 - 甲基丙基] - （2-三甲基氨基乙基）磷酸酯，其制备方法和含有它们的药物组合物
公开(公告)号：US5543402A
公开(公告)日：1996-08-06
申请号：US95478
申请日：1993-07-23
申请人： Elmar Bosies , Dieter Herrmann , Wulf Pahlke
发明人： Elmar Bosies , Dieter Herrmann , Wulf Pahlke
IPC分类号： A61K31/685 , A61P35/00 , C07F9/09 , C07F9/10 , A61K31/66
CPC分类号： C07F9/10
摘要： The present invention provides [3-(C.sub.16 -C.sub.18)-alkaesulphinyl- and -sulphonyl-2-methoxy-methylpropyl]-(2-trimethylammonioethyl) phosphates having superior anti-tumor activity.
摘要翻译：本发明提供具有优异抗肿瘤活性的[3-（C16-C18） - 亚硫酰基 - 和 - 磺酰基-2-甲氧基 - 甲基丙基] - （2-三甲基铵乙基）磷酸酯。

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