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1. 发明授权

US4278683A Saccharase inhibiting 3,4,5-trihydroxypiperidine derivatives 失效
标题翻译：糖精酶抑制3,4,5-三羟基哌啶衍生物
公开(公告)号：US4278683A
公开(公告)日：1981-07-14
申请号：US71347
申请日：1979-08-30
申请人： Jurgen Stoltefuss , Lutz Muller , Walter Puls , Rudiger Sitt
发明人： Jurgen Stoltefuss , Lutz Muller , Walter Puls , Rudiger Sitt
IPC分类号： A23K1/16 , A23K1/18 , A61K31/445 , A61P1/00 , A61P3/06 , A61P3/08 , A61P3/10 , A61P9/10 , A61P9/12 , A61P31/04 , A61P43/00 , C07D211/46 , C07D211/60 , C07D211/98 , C07F9/59
CPC分类号： C07D211/98 , A23K20/132 , A23K50/30 , C07D211/46 , C07D211/60 , C07F9/598 , Y10S514/866
摘要： The invention relates to 3,4,5-trihydroxypiperidines, processes for their producion, compositions containing them and methods for the use of said 3,4,5-trihydroxypiperidines and compositions containing them. The compounds and compositions of the invention are useful, inter alia, for their saccharase inhibiting activity in warm-blooded animals as well as their ability to improve feed utilization in warm-blooded and cold-blooded animals.
摘要翻译：本发明涉及3,4,5-三羟基哌啶，其生产方法，含有它们的组合物和使用所述3,4,5-三羟基哌啶的方法和含有它们的组合物。本发明的化合物和组合物尤其可用于温血动物中的糖酶抑制活性，以及它们在温血动物和冷血动物中提高饲料利用能力。

2. 发明授权

US4407809A N-phenoxy(or thio)hydrocarbon 3,4,5-trihydroxypiperidine derivatives, their use in medicine and in animal nutrition 失效
标题翻译： N-苯氧基（或硫代）烃3,4,5-三羟基哌啶衍生物，它们在医药和动物营养中的应用
公开(公告)号：US4407809A
公开(公告)日：1983-10-04
申请号：US231695
申请日：1981-02-05
申请人： Bodo Junge , Jurgen Stoltefuss , Lutz Muller , Hans-Peter Krause , Rudiger Sitt
发明人： Bodo Junge , Jurgen Stoltefuss , Lutz Muller , Hans-Peter Krause , Rudiger Sitt
IPC分类号： C07D401/12 , A23K1/16 , A61K31/4427 , A61K31/445 , A61K31/452 , A61K31/4523 , A61P3/00 , A61P3/06 , A61P3/08 , A61P3/10 , A61P43/00 , C07D211/40 , C07D211/46 , C12N9/99
CPC分类号： C07C321/00 , A23K20/132 , C07D211/46
摘要： The invention relates to 3,4,5-trihydroxypiperidine compound of Formula (I) as methods for the preparation of said compounds. Also included in the invention are compositions containing said piperidine compounds and methods for the use of said piperidine compounds and compositions. The invention further includes veterinary compositions containing said piperidine compounds and their use in animal nutrition.The piperidine compounds of Formula (I) are useful as agents against prediabetes, gastritis, constipation, infections of the gastro-intestinal tract, meteorism, flatulence, caries, arteriosclerosis and hypertension and in particular against diabetes, hyperlipaemia and adiposity, and also in animal nutrition for influencing the meat/fat ratio in favor of the meat content.
摘要翻译：本发明涉及作为制备所述化合物的方法的式（I）的3,4,5-三羟基哌啶化合物。本发明还包括含有所述哌啶化合物的组合物和使用所述哌啶化合物和组合物的方法。本发明还包括含有所述哌啶化合物的兽药组合物及其在动物营养中的用途。

3. 发明授权

US4312872A 1-Alka-2,4-dienyl-2-hydroxymethyl-3,4,5-trihydroxypiperidines as inhibitors of .alpha.-glucoside hydrolases 失效
标题翻译： 1-烷基-2,4-二烯基-2-羟甲基-3,4,5-三羟基哌啶作为α-葡糖苷水解酶的抑制剂
公开(公告)号：US4312872A
公开(公告)日：1982-01-26
申请号：US158541
申请日：1980-06-11
申请人： Bodo Junge , Lutz Muller , Rudiger Sitt , Gunter Thomas , Hans P. Krause , Walter Puls
发明人： Bodo Junge , Lutz Muller , Rudiger Sitt , Gunter Thomas , Hans P. Krause , Walter Puls
IPC分类号： A61K31/445 , A61P3/06 , A61P3/08 , A61P3/10 , A61P43/00 , C07D211/46
CPC分类号： C07D211/46 , Y10S514/866
摘要： The invention relates to 1-alka-2,4-dienyl-2-hydroxymethyl-3,4,5-trihydroxypiperidine compounds which are, inter alia, potent inhibitors for .alpha.- glucoside hydrolases and effect lipid absorption. Also included in the invention are methods for the manufacture of the said compounds, compositions containing said compounds and methods for the use of said compounds and compositions.
摘要翻译：本发明涉及1-烷基-2,4-二烯基-2-羟甲基-3,4,5-三羟基哌啶化合物，其特别是α-葡萄糖苷水解酶的有效抑制剂并影响脂质吸收。本发明还包括制备所述化合物的方法，含有所述化合物的组合物和使用所述化合物和组合物的方法。

4. 发明授权

US4293551A N-Amino-3,4,5-trihydroxypiperidines, their production and their medicinal use 失效
标题翻译： N-氨基-3,4,5-三羟基哌啶，其生产及其药用
公开(公告)号：US4293551A
公开(公告)日：1981-10-06
申请号：US58348
申请日：1979-07-17
申请人： Gunther Kinast , Lutz Muller , Walter Puls , Rudiger Sitt
发明人： Gunther Kinast , Lutz Muller , Walter Puls , Rudiger Sitt
IPC分类号： A23K1/16 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P3/06 , A61P3/08 , A61P3/10 , A61P9/10 , A61P9/12 , A61P43/00 , C07D211/98 , C07D333/00 , C07D401/12 , C07D405/12 , C07D409/12 , C07H5/06 , C12N9/99
CPC分类号： C07H5/06 , C07D211/98 , Y10S514/824 , Y10S514/835 , Y10S514/866 , Y10S514/872
摘要： The invention relates to N-amino-3,4,5-trihydroxypiperidines, methods for their production, compositions containing said compounds. Also included are methods for the use of said compounds and compositions.
摘要翻译：本发明涉及N-氨基-3,4,5-三羟基哌啶，其制备方法，含有所述化合物的组合物。还包括使用所述化合物和组合物的方法。

5. 发明授权

US4348402A 2-Hydroxyalkyl-3,4,5-trihydroxy-piperidine compounds, their production and their medicinal use 失效
标题翻译： 2-羟基烷基-3,4,5-三羟基 - 哌啶化合物，其生产及其药用
公开(公告)号：US4348402A
公开(公告)日：1982-09-07
申请号：US193498
申请日：1980-10-02
申请人： Gunther Kinast , Lutz Muller , Rudiger Sitt , Walter Puls
发明人： Gunther Kinast , Lutz Muller , Rudiger Sitt , Walter Puls
IPC分类号： A61K31/445 , A61K31/70 , A61K31/7028 , A61P1/00 , A61P3/06 , A61P3/08 , A61P3/10 , A61P9/12 , A61P43/00 , C07D211/46 , C07D498/04 , C07H7/02 , C07H9/04 , C07H13/08 , C07H15/12 , C07H15/18 , C07D211/42
CPC分类号： C07H9/04 , C07D211/46 , C07H7/02 , Y10S514/824 , Y10S514/835 , Y10S514/866
摘要： The invention relates to .alpha.-hydroxyalkyl-3,4,5-trihydroxypiperidines defined by Formula (I), infra, and pharmaceutical compositions and medicaments containing said compounds. Also included in the invention are methods for the use of said compounds, compositions and medicaments as inhibitors of .alpha.-glucoside hydrolases; and intermediates for the compounds of said Formula (I).
摘要翻译：本发明涉及由下式（I）定义的α-羟基烷基-3,4,5-三羟基哌啶以及含有所述化合物的药物组合物和药物。本发明还包括使用所述化合物，组合物和药物作为α-葡糖苷水解酶抑制剂的方法; 和所述式（I）的化合物的中间体。

6. 发明授权

US4574124A Lipid absorption-inhibiting agents and their use 失效
标题翻译：脂质吸收抑制剂及其用途
公开(公告)号：US4574124A
公开(公告)日：1986-03-04
申请号：US573168
申请日：1984-01-23
申请人： Hans-Joachim Kabbe , Hans-Peter Krause , Rudiger Sitt
发明人： Hans-Joachim Kabbe , Hans-Peter Krause , Rudiger Sitt
IPC分类号： C07D209/08 , C07D215/08 , C07D215/18 , C07D215/20 , C07D279/16 , A61K31/535 , C07D265/28
CPC分类号： C07D279/16 , C07D209/08 , C07D215/08 , C07D215/18 , C07D215/20
摘要： The invention relates to alkylurea derivatives of Formula (I), as defined in the specification, which alkylurea derivatives are useful as hypolipaemic agents. Also included in the invention are methods for the manufacture of said alkylurea derivatives compositions and medicaments containing said alkylurea derivatives and methods for the use of said alkylurea derivatives.
摘要翻译：本发明涉及如说明书中定义的式（I）的烷基脲衍生物，其中烷基脲衍生物可用作降血糖剂。本发明还包括制备所述烷基脲衍生物组合物和含有所述烷基脲衍生物的药物的方法和使用所述烷基脲衍生物的方法。

7. 发明授权

US4328233A .alpha.-Glucosidase inhibiting 2-hydroxymethyl-3,4,5-trihydroxy-piperidines 失效
标题翻译： α-葡糖苷酶抑制2-羟甲基-3,4,5-三羟基 - 哌啶
公开(公告)号：US4328233A
公开(公告)日：1982-05-04
申请号：US88990
申请日：1979-10-29
申请人： Horst Boshagen , Rudiger Sitt , Ernst Truscheit
发明人： Horst Boshagen , Rudiger Sitt , Ernst Truscheit
IPC分类号： A23K1/16 , A23K1/18 , A61K31/445 , A61K31/451 , A61P3/06 , A61P3/08 , A61P3/10 , A61P43/00 , C07D211/46 , C07D211/60
CPC分类号： C07D211/46 , A23K20/132 , A23K50/30 , Y10S514/866
摘要： The invention relates to 2-hydroxymethyl-3,4,5-trihydroxy-6-substituted-piperidines and methods for their preparation. The invention also includes compositions containing said 2-hydroxymethyl-3,4,5-trihydroxy-6-substituted-piperidines and the use of said compounds and compositions for influencing carbohydrate metabolism and fat metabolism and for use in animal nutrition as feed additives.
摘要翻译：本发明涉及2-羟甲基-3,4,5-三羟基-6-取代哌啶及其制备方法。本发明还包括含有所述2-羟甲基-3,4,5-三羟基-6-取代哌啶的组合物，以及所述化合物和组合物用于影响碳水化合物代谢和脂肪代谢以及用作动物营养作为饲料添加剂的用途。

8. 发明授权

US4330677A Polyether compounds, their production and their medicinal use 失效
标题翻译：聚醚化合物，其生产及其药用
公开(公告)号：US4330677A
公开(公告)日：1982-05-18
申请号：US89839
申请日：1979-10-31
申请人： Siegfried Linke , Mithat Mardin , Hans P. Krause , Rudiger Sitt
发明人： Siegfried Linke , Mithat Mardin , Hans P. Krause , Rudiger Sitt
IPC分类号： A61K31/765 , A61K31/77 , A61P1/00 , A61P3/06 , C08G65/00 , C08G65/32 , C08G65/321 , C08G65/326 , C08G65/332 , C08G65/337 , C07C59/00
CPC分类号： C08G65/326 , A61K31/77 , C08G65/321 , C08G65/3326 , C08G65/337 , Y10S514/824
摘要： The invention relates to polyethers having an an average molecule weight of 3000 to 5000 and having a propylene oxide proportion of 60 to 80% and an ethylene oxide proportion of 20 to 40%. Also included in the invention are compositions containing said polyethers and methods for the use of said polyethers and compositions, particularly for their anti-lipidaemic effect.
摘要翻译：本发明涉及平均分子量为3000〜5000，环氧丙烷的比例为60〜80％，环氧乙烷的比例为20〜40％的聚醚。本发明还包括含有所述聚醚的组合物和使用所述聚醚和组合物的方法，特别是其抗脂质代谢作用。

9. 发明授权

US4261988A Chromanone derivatives 失效
标题翻译：色酮衍生物
公开(公告)号：US4261988A
公开(公告)日：1981-04-14
申请号：US20119
申请日：1979-03-13
申请人： Arno Widdig , Hans-Joachim Kabbe , Martin Scheer , Rudiger Sitt
发明人： Arno Widdig , Hans-Joachim Kabbe , Martin Scheer , Rudiger Sitt
IPC分类号： A61K31/35 , A61K31/352 , A61P19/06 , C07D311/22 , C07D311/24 , C07D311/32 , C07D311/92 , C07D311/96 , C07D405/04 , C07D491/10 , C07D491/107
CPC分类号： C07D491/10 , C07D311/22 , C07D311/24 , C07D311/32 , C07D311/92 , C07D311/96
摘要： Compounds useful in the treatment of cholesterolaemia are of the general formula ##STR1## or salts thereof in which R.sup.1 and R.sup.2 independently denote radicals including hydrogen, alkyl, aryl and heterocyclic radical or together complete a carbocyclic or heterocylic ring, R.sup.3 denotes a radical ##STR2## in which R.sup.9, R.sup.10 and R.sup.11 include hydrogen, cyano, nitro, alkyl and aryl or, in pairs, complete carbocyclic rings, X denotes cyano, nitro or substituted carbonyl, sulphonyl or phosphonyl group, R.sup.4 is hydrogen or a radical defined for R.sup.1 or R.sup.3, and R.sup.5, R.sup.6, R.sup.7 and R.sup.8 include hydrogen, nitro, cyano, carboxyl, alkyl and aryl or, in pairs, complete carbocyclic rings, with the proviso that R.sup.1 and R.sup.9 are not both phenyl if X denotes CO--C.sub.6 H.sub.6. The compounds exhibit considerably higher hypocholesterolaemic activity than the known clofibrate and in addition exhibit a pronounced nutritive effect, e.g., in a medicated fodder or premix.
摘要翻译：用于治疗胆固醇血症的化合物具有通式（I）或其盐，其中R 1和R 2独立地表示包括氢，烷基，芳基和杂环基团的基团，或者一起完成碳环或杂环，R3表示其中R9，R10和R11包括氢，氰基，硝基，烷基和芳基，或成对地成为完全碳环，X表示氰基，硝基或取代的羰基，磺酰基或膦酰基，R4是氢或基团对于R 1或R 3而言，R 5，R 6，R 7和R 8包括氢，硝基，氰基，羧基，烷基和芳基，或成对地成为完全碳环，条件是如果X表示CO，则R 1和R 9不是苯基 -C6H6。化合物显示比已知的氯贝特明显更高的降血胆固醇血症活性，并且还显示出明显的营养作用，例如在药物饲料或预混物中。

10. 发明授权

US4510156A Bisindolyl alkylene ureas lipid absorption-inhibiting agents and their use thereas 失效
标题翻译：双吲哚基亚烷基脲类脂质吸收抑制剂及其用途
公开(公告)号：US4510156A
公开(公告)日：1985-04-09
申请号：US347599
申请日：1982-02-10
申请人： Hans-Joachim Kabbe , Hans-Peter Krause , Rudiger Sitt
发明人： Hans-Joachim Kabbe , Hans-Peter Krause , Rudiger Sitt
IPC分类号： C07D209/08 , C07D215/08 , C07D215/18 , C07D215/20 , C07D279/16 , A61K31/40 , C07D209/26 , C07D403/12
CPC分类号： C07D279/16 , C07D209/08 , C07D215/08 , C07D215/18 , C07D215/20
摘要： The invention relates to alkylurea derivatives of Formula (I), as defined in the specification, which alkylurea derivatives are useful as hypolipaemic agents. Also included in the invention are methods for the manufacture of said alkylurea derivatives compositions and medicaments containing said alkylurea derivatives and methods for the use of said alkylurea derivatives.
摘要翻译：本发明涉及如说明书中定义的式（I）的烷基脲衍生物，其中烷基脲衍生物可用作降血糖剂。本发明还包括制备所述烷基脲衍生物组合物和含有所述烷基脲衍生物的药物的方法和使用所述烷基脲衍生物的方法。

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