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1. 发明申请

US20090226524A1 Stable active compound complex of salts of o-acetylsalicylic acid with basic amino acids and glycine 有权
标题翻译：邻乙酰水杨酸与碱性氨基酸和甘氨酸的稳定的活性复合物
公开(公告)号：US20090226524A1
公开(公告)日：2009-09-10
申请号：US11921339
申请日：2006-05-20
申请人： Gerhard Franckowiak , Wolfram Ledwoch , Eberhard Schweinheim , Yutaka Hayauchi
发明人： Gerhard Franckowiak , Wolfram Ledwoch , Eberhard Schweinheim , Yutaka Hayauchi
IPC分类号： A61K9/14 , A61K31/60 , A61P9/10
CPC分类号： A61K31/616 , A61K31/198 , C07C69/157 , C07C227/42 , C07C229/08 , C07C229/26
摘要： The present invention relates to stable active compound complexes of salts of o-acetylsalicylic acid with basic amino acids and glycine, to a process for their preparation and to their use as medicaments.
摘要翻译：本发明涉及邻乙酰水杨酸与碱性氨基酸和甘氨酸的稳定的活性化合物络合物，其制备方法和用作药物。

2. 发明授权

US08063243B2 Stable active compound complex of salts of o-acetylsalicylic acid with basic amino acids and glycine 有权
标题翻译：邻乙酰水杨酸与碱性氨基酸和甘氨酸的稳定的活性复合物
公开(公告)号：US08063243B2
公开(公告)日：2011-11-22
申请号：US11921339
申请日：2006-05-20
申请人： Gerhard Franckowiak , Wolfram Ledwoch , Eberhard Schweinheim , Yutaka Hayauchi
发明人： Gerhard Franckowiak , Wolfram Ledwoch , Eberhard Schweinheim , Yutaka Hayauchi
IPC分类号： C07C65/10
CPC分类号： A61K31/616 , A61K31/198 , C07C69/157 , C07C227/42 , C07C229/08 , C07C229/26
摘要： The present invention relates to stable active compound complexes of salts of o-acetylsalicylic acid with basic amino acids and glycine, to a process for their preparation and to their use as medicaments.
摘要翻译：本发明涉及邻乙酰水杨酸与碱性氨基酸和甘氨酸的稳定的活性化合物络合物，其制备方法和用作药物。

3. 发明申请

US20090306024A1 Combination preparations of o-acetylsalicylic acid salts 审中-公开
标题翻译：邻乙酰水杨酸盐的组合制剂
公开(公告)号：US20090306024A1
公开(公告)日：2009-12-10
申请号：US12090179
申请日：2006-10-04
申请人： Wolfram Ledwoch , Claus Gert Haase , Gerhard Franckowiak , Heike Wagner , Yutaka Hayauchi
发明人： Wolfram Ledwoch , Claus Gert Haase , Gerhard Franckowiak , Heike Wagner , Yutaka Hayauchi
IPC分类号： A61K31/60 , A61P9/00
CPC分类号： A61K9/2077 , A61K9/2054 , A61K9/4808 , A61K9/5084 , A61K31/366 , A61K31/40 , A61K31/44 , A61K31/60 , A61K47/542 , A61K2300/00
摘要： The present invention relates to a fixed combination comprising a salt of o-acetylsalicylic acid with a basic amino acid as component A and an HMG-CoA reductase inhibitor as component B, a medicament comprising this combination and a process for its production.
摘要翻译：本发明涉及包含邻乙酰水杨酸与碱性氨基酸作为组分A的盐和作为组分B的HMG-CoA还原酶抑制剂的固定组合物，包含该组合的药物及其生产方法。

4. 发明授权

US08613950B2 Pharmaceutical forms with improved pharmacokinetic properties 有权
标题翻译：具有改善的药代动力学性质的药物形式
公开(公告)号：US08613950B2
公开(公告)日：2013-12-24
申请号：US11885019
申请日：2006-02-16
申请人： Peter Serno , Roland Heinig , Kerstin Pauli , Yutaka Hayauchi
发明人： Peter Serno , Roland Heinig , Kerstin Pauli , Yutaka Hayauchi
IPC分类号： A61K31/53 , A61K9/20 , A61K9/00
CPC分类号： A61K9/2018 , A61K9/0056 , A61K9/006 , A61K31/53
摘要： The present application relates to novel drug formulations of vardenafil which dissolve rapidly in the mouth and lead to increased bioavailability and to a plateau-like plasma concentration profile, and to processes for their preparation.
摘要翻译：本申请涉及伐地那非的新型药物制剂，其在口中快速溶解并导致增加的生物利用度和平台状血浆浓度分布，以及其制备方法。

5. 发明授权

US4699899A Substituted O-sulphonyl-glycosylamides, processes for their preparation and their use as medicaments 失效
标题翻译：取代的O-磺酰基 - 糖基酰胺，其制备方法及其作为药物的用途
公开(公告)号：US4699899A
公开(公告)日：1987-10-13
申请号：US832482
申请日：1986-02-21
申请人： Bernd-Wieland Kruger , Yutaka Hayauchi , Oswald Lockhoff , Peter Stadler , Karl G. Metzger , Klaus G. Stunkel , Hans-Joachim Zeiler
发明人： Bernd-Wieland Kruger , Yutaka Hayauchi , Oswald Lockhoff , Peter Stadler , Karl G. Metzger , Klaus G. Stunkel , Hans-Joachim Zeiler
IPC分类号： C07H13/00 , A61K31/70 , A61K31/7024 , A61K31/7028 , A61P31/00 , A61P37/04 , C07H1/00 , C07H13/12 , C07H15/04 , C07H15/12
CPC分类号： C07H13/12 , C07H15/04 , Y10S514/885
摘要： Novel compounds of the formula ##STR1## in which X is hydrogen or --CH.sub.2 --OR.sup.5,Z represents OR.sup.4, NH.sub.2 or ##STR2## R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently is hydrogen or ##STR3## at least one of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 being ##STR4## Y and W each independently is oxygen, sulphur, NH or CH.sub.2, and R.sup.1, R.sup.6, R.sup.7 and R.sup.8 each independently is an optionally substituted hydrocarbon radical with up to 50 C atoms,stimulate the immune system.
摘要翻译：式中，X为氢或-CH 2 OR 5的新颖化合物，Z为OR 4，NH 2或R 2，R 3，R 4和R 5各自独立地为氢或R 2，R 3，，R 4和R 5是Y，W各自独立地是氧，硫，NH或CH 2，R 1，R 6，R 7和R 8各自独立地是具有至多50个C原子的任选取代的烃基，刺激免疫系统。

6. 发明申请

US20080249096A1 Pharmaceutical Forms with Improved Pharmacokinetic Properties 有权
标题翻译：具有改善的药物动力学性质的药物形式
公开(公告)号：US20080249096A1
公开(公告)日：2008-10-09
申请号：US11885019
申请日：2006-02-16
申请人： Peter Serno , Roland Heinig , Kerstin Pauli , Yutaka Hayauchi
发明人： Peter Serno , Roland Heinig , Kerstin Pauli , Yutaka Hayauchi
IPC分类号： A61K31/53 , A61P15/10
CPC分类号： A61K9/2018 , A61K9/0056 , A61K9/006 , A61K31/53
摘要： The present application relates to novel drug formulations of vardenafil which dissolve rapidly in the mouth and lead to increased bioavailability and to a plateau-like plasma concentration profile, and to processes for their preparation.
摘要翻译：本申请涉及伐地那非的新型药物制剂，其在口腔中快速溶解并导致生物利用度增加和平台状血浆浓度分布，以及其制备方法。

7. 发明授权

US4855283A Novel pharmaceutically active N-(2-aminoacylamido-2-deoxy-hexosyl)-amides, -carbamates and -ureas 失效
标题翻译：新型药物活性N-（2-氨基酰氨基-2-脱氧己糖基） - 酰胺， - 氨基甲酸酯和脲
公开(公告)号：US4855283A
公开(公告)日：1989-08-08
申请号：US874983
申请日：1986-06-16
申请人： Oswald Lockhoff , Yutaka Hayauchi , Peter Stadler , Klaus G. Stunkel , Gert Streissle , Arnold Paessens , Volker Klimetzek , Hans-Joachim Zeiler , Karl G. Metzger , Hein-Peter Kroll , Helmut Brunner , Klaus Schaller
发明人： Oswald Lockhoff , Yutaka Hayauchi , Peter Stadler , Klaus G. Stunkel , Gert Streissle , Arnold Paessens , Volker Klimetzek , Hans-Joachim Zeiler , Karl G. Metzger , Hein-Peter Kroll , Helmut Brunner , Klaus Schaller
IPC分类号： A61K31/70 , A61K31/7024 , A61K31/7028 , A61K39/39 , A61P1/16 , A61P11/00 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/12 , A61P37/00 , C07H13/04 , C07H13/06 , C07H13/12 , C07H15/04 , C07H15/12
CPC分类号： C07H13/04 , A61K39/39 , C07H13/12 , A61K2039/55511
摘要： Compounds of the formula ##STR1## in which R.sup.1 denotes hydrogen or a saturated or singly or multiply unsaturated alkyl radical having up to 50 carbon atoms,X represents --CH.sub.2 --, --O-- or --NH--,R.sup.2 denotes hydrogen or a saturated or singly or multiply unsaturated alkyl radical having up to 50 carbon atoms,R.sup.3, R.sup.4 and R.sup.5, independently of one another, denotes hydrogen or acyl--CO--R.sup.6, R.sup.6 being an alkyl radical having up to 10 carbon atoms,R.sup.7 denotes hydrogen, C.sub.1 -C.sub.7 -alkyl-, hydroxymethyl, 1-hydroxyethyl, mercaptomethyl, 2-(methylthio)-ethyl, 3-aminopropyl, 3-ureidopropyl, 3-guanidyl-propyl, 4-aminobutyl, carboxymethyl, carbamylmethyl, 2-carboxyethyl, 2-carbamoylethyl, benzyl, 4-hydroxybenzyl, 3-indolylmethyl or 4-imidazolylmethyl, andR.sup.8 represents hydrogen or methyl, andR.sup.9 represents hydrogen, acetyl, benzoyl, trichloroacetyl, trifluoroacetyl, methoxycarbonyl, t-butyloxycarbonyl or benzyloxycarbonyl andR.sup.7 and R.sup.8 together can denote --CH.sub.2 --CH.sub.2 --CH.sub.2, and pharmaceutically acceptable salts thereof stimulate the immune system and can be used in conjuction with antibiotics and vaccines. New intermediates are also shown.
摘要翻译：其中R 1表示氢或具有至多50个碳原子的饱和或单或多不饱和烷基的式“IMAGE”的化合物，X表示-CH 2 - ， - O-或-NH-，R 2表示氢或饱和或具有多达50个碳原子的单或多不饱和烷基，R 3，R 4和R 5彼此独立地表示氢或酰基-CO-R 6，R 6是具有至多10个碳原子的烷基，R 7表示氢，C 1 C 1-7 - 烷基 - ，羟甲基，1-羟乙基，巯基甲基，2-（甲硫基） - 乙基，3-氨丙基，3-脲基丙基，3-氨基丙基 - 丙基，4-氨基丁基，羧甲基，氨基甲酰甲基，2-羧乙基，乙酰基，苯甲酰基，三氯乙酰基，三氟乙酰基，甲氧基羰基，叔丁氧基羰基或苄氧基羰基，R7和R8一起可以表示（C 1 -C 6）烷基，苄基，4-羟基苄基，3-吲哚基甲基或4-咪唑基甲基，R 8表示氢或甲基， -CH 2 -CH 2 -CH 2，及其药学上可接受的盐模拟免疫系统，并可与抗生素和疫苗结合使用。还显示了新的中间体。

8. 发明授权

US4891425A N-glycosylamide derivatives, processes for their preparation and their use as medicaments 失效
标题翻译： N-糖酰胺衍生物，其制备方法及其作为药物的用途
公开(公告)号：US4891425A
公开(公告)日：1990-01-02
申请号：US7703
申请日：1987-01-28
申请人： Oswald Lockhoff , Yutaka Hayauchi , Peter Stadler , Helmut Brunner
发明人： Oswald Lockhoff , Yutaka Hayauchi , Peter Stadler , Helmut Brunner
IPC分类号： A01N57/16 , A61K31/70 , A61K31/7028 , A61P31/04 , A61P37/00 , C07H13/04 , C07H15/04 , C07H15/12 , C07H15/18
CPC分类号： C07H13/04 , C07H15/04
摘要： A N-glycosylamide derivative of the formula (I) ##STR1## in which R.sup.1 denotes hydrogen or a saturated or mono- or polyunsaturated alkyl radical with one to 50 carbon atoms,R.sup.2 denotes hydrogen or a saturated or mono- or polyunsaturated alkyl radical with one to 50 carbon atoms,R.sup.3 denotes hydrogen or an acyl radical with up to 20 carbon atoms,R.sup.4 denotes hydrogen or an alkyl radical with up to 4 carbon atoms andR.sup.5 and R.sup.6 independently of one another denote hydrogen or an acyl radical with up to 10 carbon atoms or a saturated or an unsaturated alkyl radical or an aralkyl radical with up to 10 carbon atoms, orR.sup.5 l and R.sup.6 together denote a grouping ##STR2## wherein R.sup.7 and R.sup.8 independently of one another denote hydrogen or lower alkyl with up to 5 carbon atoms or an unsubstituted or substituted aryl radical with up to 10 C atoms in the aromatic part. The N-glycosylamide derivatives exhibiting a broad defense-increasing action in the body.
摘要翻译：式（I）的N-糖酰胺衍生物其中R 1表示氢或具有1至50个碳原子的饱和或单或多不饱和烷基，R 2表示氢或饱和或单或多不饱和的具有1至50个碳原子的烷基，R 3表示氢或至多20个碳原子的酰基，R 4表示氢或具有至多4个碳原子的烷基，R 5和R 6彼此独立地表示氢或酰基具有至多10个碳原子或饱和或不饱和的烷基或具有至多10个碳原子的芳烷基，或者R 5和R 6一起表示分组，其中R 7和R 8彼此独立地表示氢或低级烷基具有多至5个碳原子的芳族部分或未被取代的或取代的芳基，其中芳族部分中具有至多10个C原子。 N-糖酰胺衍生物在体内表现出广泛的防御增加作用。

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