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1. 发明授权

US5506202A Insulin derivatives, a process for the preparation thereof, the use thereof, and a pharmaceutical formulation containing them 失效
标题翻译：胰岛素衍生物，其制备方法，其用途和含有它们的药物制剂
公开(公告)号：US5506202A
公开(公告)日：1996-04-09
申请号：US442296
申请日：1995-05-16
申请人： Laszlo Vertesy , Karl Geisen , Gunther J. Riess , Klaus Sauber
发明人： Laszlo Vertesy , Karl Geisen , Gunther J. Riess , Klaus Sauber
IPC分类号： C12P21/02 , A61K38/00 , A61K38/28 , A61P3/08 , A61P3/10 , C07H21/04 , C07K1/06 , C07K1/08 , C07K1/20 , C07K14/575 , C07K14/62 , C12N15/09 , C12R1/19 , C12R1/465
CPC分类号： C07K14/62 , A61K38/00
摘要： New insulin derivatives, a process for their preparation and use, and a pharmaceutical formulation containing them are disclosed. The derivatives contain the basic amino acid arginine at the amino-terminal position of the insulin A-chain, and various amino acid substitutions at the carboxyl terminus of the insulin B-chain. The compounds are suitable for the treatment of diabetes mellitus, have a delayed profile of action and are very well tolerated.
摘要翻译：公开了新的胰岛素衍生物，其制备和使用的方法以及含有它们的药物制剂。衍生物含有胰岛素A链氨基末端位置的碱性氨基酸精氨酸，胰岛素B链羧基末端的各种氨基酸取代。该化合物适用于治疗糖尿病，具有延迟的作用特征并且耐受性良好。

2. 发明授权

US4990500A Oxirane pseudooligosaccharides, a process for their preparation, their use and pharmaceutical preparations 失效
标题翻译：环氧乙烷假低聚糖，其制备方法，用途和药物制剂
公开(公告)号：US4990500A
公开(公告)日：1991-02-05
申请号：US83807
申请日：1987-08-11
申请人： Laszlo Vertesy , Joachim Betz , Hans-Wolfram Fehlhaber , Karl Geisen
发明人： Laszlo Vertesy , Joachim Betz , Hans-Wolfram Fehlhaber , Karl Geisen
IPC分类号： C08B37/00 , C07H15/26 , C07H17/04 , C12P19/00 , C12P19/26
CPC分类号： C07H15/26 , C07H17/04 , Y10S435/886 , Y10S514/835 , Y10S514/866
摘要： Oxirane-pseudooligosaccharides of the formula I ##STR1## in which z is zero or 1, their physiologically acceptable salts with acids, a process for their preparation, pharmaceutical preparations, and their use are described. The compounds have an .alpha.-glucosidase-inhibiting action.
摘要翻译：描述了其中z为零或1，其酸的生理学上可接受的盐，其制备方法，药物制剂及其用途的式I的视黄醛 - 假低聚糖。该化合物具有α-葡糖苷酶抑制作用。

3. 发明授权

US5149716A Insulin derivatives, process for their preparation, their use and a pharmaceutical preparation containing them 失效
标题翻译：胰岛素衍生物，其制备方法，其使用和含有它们的药物制剂
公开(公告)号：US5149716A
公开(公告)日：1992-09-22
申请号：US603835
申请日：1990-10-26
申请人： Laszlo Vertesy , Karl Geisen , Richard Bicker
发明人： Laszlo Vertesy , Karl Geisen , Richard Bicker
IPC分类号： C12P21/06 , A61K38/28 , A61P3/08 , A61P3/10 , C07K1/06 , C07K14/575 , C07K14/62 , C12P21/02
CPC分类号： C07K14/62
摘要： The invention relates to insulin derivatives of the formula III ##STR1## in which R.sup.30 and R.sup.31 together are OH, or R.sup.30 is a radical of a neutral, genetically encodable L-amino acid and R.sup.31 is OH or a physiologically acceptable organic group of basic character having up to 50 carbon atoms, whose synthesis involves 0 to 3 .alpha.-amino acids and whose optional terminal carboxyl function can be present free, as an ester function, as an amide function, as a lactone or reduced to CH.sub.2 OH, and R.sup.A-1 is a radical of a genetically encodable L-amino acid, and physiologically acceptable salts of said insulin derivative of the formula III.
摘要翻译：本发明涉及式III（III）的胰岛素衍生物，其中R30和R31一起是OH，或R30是中性的，可遗传编码的L-氨基酸的基团，R31是OH或生理上可接受的有机基团具有多至50个碳原子的基本特征，其合成涉及0至3个α-氨基酸，并且其任选的末端羧基官能团可作为酯官能团作为酰胺官能团作为内酯，作为内酯或还原成CH2OH，以及 RA-1是基因编码的L-氨基酸的基团，以及所述式III的胰岛素衍生物的生理上可接受的盐。

4. 发明授权

US4632917A Pseudooligosaccharides with an .alpha.-glucosidase-inhibiting action, their use and pharmaceutical products 失效
标题翻译：具有α-葡糖苷酶抑制作用的伪低聚糖，其用途和药物产品
公开(公告)号：US4632917A
公开(公告)日：1986-12-30
申请号：US771610
申请日：1985-09-03
申请人： Laszlo Vertesy , Rudolf Bender , Hans-Wolfram Fehlhaber , Karl Geisen
发明人： Laszlo Vertesy , Rudolf Bender , Hans-Wolfram Fehlhaber , Karl Geisen
IPC分类号： G01N33/66 , A61K8/00 , A61K8/73 , A61K31/70 , A61K31/7028 , A61K31/715 , A61P1/02 , A61P3/00 , A61P3/06 , A61P43/00 , A61Q11/00 , C07H3/06 , C07H15/00 , C07H15/22 , C08B37/00 , C12P19/04 , C12P19/12 , C12P19/44 , C12R1/465 , A61K31/73
CPC分类号： C12R1/465 , C07H15/22 , C07H3/06 , C12P19/12 , C12P19/44 , Y10S514/835 , Y10S514/866
摘要： Pseudooligosaccharides of the formula I ##STR1## in which l, m and n have the meanings given, physiologically acceptable salts thereof with acids, a process for their preparation, pharmaceutical products and their use are described. The compounds have an .alpha.-glucosidase-inhibiting action.
摘要翻译：其中l，m和n具有给定的含义，式Ⅰ的假寡糖，其酸的生理上可接受的盐，其制备方法，药物产品及其用途。该化合物具有α-葡糖苷酶抑制作用。

5. 发明授权

US07148254B2 2-Phenylbenzofuran derivatives, a process for preparing them, and their use 有权
标题翻译： 2-苯基苯并呋喃衍生物，其制备方法及其应用
公开(公告)号：US07148254B2
公开(公告)日：2006-12-12
申请号：US10972546
申请日：2004-10-25
申请人： Laszlo Vertesy , Michael Kurz , Astrid Markus-Erb , Luigi Toti
发明人： Laszlo Vertesy , Michael Kurz , Astrid Markus-Erb , Luigi Toti
IPC分类号： A61K31/34 , C07D307/86 , C12P17/04 , C12N1/18
CPC分类号： C12R1/66 , C07D307/86 , C12P17/04
摘要： The present invention relates to 2-phenylbenzofurans of formula (I) which are formed, during fermentation, by the microorganism Aspergillus flavipes ST003878 (DSM 15290), to a process for preparing them and to their use as pharmaceuticals for the treatment and/or prophylaxis of bacterial infectious diseases or mycoses.
摘要翻译：本发明涉及式（I）的2-苯基苯并呋喃，其在发酵过程中由微生物黄曲霉ST003878（DSM15290）制成，涉及其制备方法及其作为药物用于治疗和/或预防的用途的细菌感染性疾病或真菌病。

6. 发明授权

US07067112B2 Cephaibols: novel antiparasitics from Acremonium tubakii, process for their production, and use thereof 有权
标题翻译：头孢唑醇：来自Acremonium tubakii的新型抗寄生虫药，其生产方法及其用途
公开(公告)号：US07067112B2
公开(公告)日：2006-06-27
申请号：US10411144
申请日：2003-04-11
申请人： Laszlo Vertesy , Michael Kurz , Matthias Schiell , Joachim Hofmann
发明人： Laszlo Vertesy , Michael Kurz , Matthias Schiell , Joachim Hofmann
IPC分类号： A61K49/00 , A61K38/10 , C07K7/08
CPC分类号： C07K7/08 , A61K38/00
摘要： The invention relates to compounds of the formula I AcPhe-Aib-Aib-Aib-x-w-Leu-y-Aib-Hyp-Gln-z-Hyp-Aib-Pro-R (I) in which R is Phe-ol or Phe-al and w, x, y, and z have the following meanings: a) w is Gly or Ala; x is Aib and y and z are Iva; b) w is Gly; x, y and z are Iva; c) w is Gly; x and z are Aib and y is Iva; d) w is Gly; x, y and z are Aib; or e) w is Gly; x and y are Aib and z is Iva; or of the formula II AcPhe-Iva-Gln-Aib-lle-Thr-Aib-Leu-Aib-x-Gln-Aib-Hyp-Aib-Pro-Phe-Ser, (II) wherein x is Hyp or Pro, which are synthesized by Acremonium tubakii FH 1685 DSM 12774 during fermentation and released into the culture medium, a process for the isolation of the cephaibols from the culture medium, and their purification, and the use of the cephaibols as pharmacologically active compounds, in particular for the control of parasites.
摘要翻译：本发明涉及式I化合物<？in-line-formula description =“In-line Formulas”end =“lead”→AcPhe-Aib-Aib-Aib-xw-Leu-y-Aib-Hyp-Gln -z-Hyp-Aib-Pro-R（I）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中R是Phe-ol或Phe-al，w，x ，y和z具有以下含义：a）w是Gly或Ala; x是Aib，y和z是Iva; b）w是Gly; x，y和z是Iva; c）w是Gly; x和z是Aib，y是Iva; d）w是Gly; x，y和z是Aib; 或e）w是Gly; x和y是Aib，z是Iva; AcPhe-Iva-Gln-Aib-Lle-Thr-Aib-Leu-Aib-x-Gln-Aib，或者式II <？in-line-formula description =“In-line Formulas”end =“lead” -Hyp-Aib-Pro-Phe-Ser，（II）<？在线公式描述=“在线公式”end =“tail”？>其中x是Hyp或Pro，它们是由Acremonium tubakii FH 1685 DSM 12774在发酵过程中释放到培养基中，从培养基中分离头孢胆素的方法及其纯化，以及将头孢唑醇用作药物活性化合物，特别是用于控制寄生虫的方法。

7. 发明授权

US6022851A Lantibiotic related to actagardine, and processes for the preparation and use thereof 有权
标题翻译：与阿达加丁有关的蓝霉素，以及其制备和使用的方法
公开(公告)号：US6022851A
公开(公告)日：2000-02-08
申请号：US172042
申请日：1998-10-14
申请人： Laszlo Vertesy , Herbert Kogler , Matthias Schiell , Joachim Wink
发明人： Laszlo Vertesy , Herbert Kogler , Matthias Schiell , Joachim Wink
IPC分类号： C12P21/02 , A61K31/00 , A61K38/00 , A61P31/00 , A61P31/04 , C07K7/08 , C07K14/365 , C12R1/045 , A61K38/04 , A61K38/12 , C07K1/107 , C07K4/04
CPC分类号： C07K7/08 , A61K38/00
摘要： The present invention relates to a novel lantibiotic having the formula NH.sub.2 --R-actagardine, where NH.sub.2 --R is the radical of the amino acid alanine, which is formed by the microorganism Actinoplanes liguriae, DSM 11797 or Actinoplanes garbadiensis, DSM 11796 during fermentation, chemical derivatives of the lantibiotic, a process for its preparation and the use of the lantibiotics as pharmaceuticals.
摘要翻译：本发明涉及一种新型的具有式NH2-R-卡那加丁的羊毛硫抗生素，其中NH2-R是氨基酸丙氨酸的基团，其由微生物活性荧光素，DSM 11797或Actinoplanes garbadiensis，DSM 11796在发酵过程中形成，羊毛硫抗生素的化学衍生物，其制备方法以及作为药物使用的羊毛硫抗生素。

8. 发明授权

US4618602A Amine containing pseudooligosaccharide, pharmaceutical composition and method of use 失效
标题翻译：含有假低聚糖的胺，药物组合物和使用方法
公开(公告)号：US4618602A
公开(公告)日：1986-10-21
申请号：US771638
申请日：1985-09-03
申请人： Laszlo Vertesy , Rudolf Bender , Hans-Wolfram Fehlhaber
发明人： Laszlo Vertesy , Rudolf Bender , Hans-Wolfram Fehlhaber
IPC分类号： A61K49/00 , A61K8/00 , A61K8/73 , A61K31/715 , A61P1/02 , A61P3/00 , A61Q11/00 , C07H15/22 , C08B37/00 , C12P19/04 , C12P19/28 , C12R1/465 , A61K31/73
CPC分类号： C07H15/22 , C12P19/28 , Y10S514/835 , Y10S514/866
摘要： Pseudooligosaccharide of the formula I ##STR1## and physiologically acceptable salts thereof with acids, a process for the preparation, pharmaceutical products and the use are described. The compound has a .alpha.-glucosidase-inhibiting action.
摘要翻译：描述了式I的伪低聚糖和其与酸的生理上可接受的盐，制备方法，药物产品和用途。该化合物具有α-葡糖苷酶抑制作用。

9. 发明授权

US06599930B2 Coniosetin and derivatives thereof, process for the preparation and the use thereof 有权
标题翻译：洋葱素及其衍生物，其制备方法和用途
公开(公告)号：US06599930B2
公开(公告)日：2003-07-29
申请号：US10003413
申请日：2001-12-06
申请人： Laszlo Vertesy , Martin Knauf , Astrid Markus-Erb , Luigi Toti , Marie-Cecile Raynal-Wetzel , Florence Fassy
发明人： Laszlo Vertesy , Martin Knauf , Astrid Markus-Erb , Luigi Toti , Marie-Cecile Raynal-Wetzel , Florence Fassy
IPC分类号： A61K3142
CPC分类号： C07D207/44
摘要： The present invention relates to novel active substances (coniosetin and coniosetin derivatives) of the formula I which are produced by the microorganism Coniochaeta ellipsoidea Udagawa (DSM 13856) during fermentation, wherein R, R2, R3, R4, R5, X, X2, X3 and X4 have the meanings stated in the specification, to chemical derivatives of coniosetin, to a process for their preparation and to their use as pharmaceuticals.
摘要翻译：本发明涉及在发酵过程中由微生物Coniochaeta ellipsoidea Udagawa（DSM 13856）生产的式I的新型活性物质（coniosetin和conisonetin衍生物），其中R，R2，R3，R4，R5，X，X2，X3和 X4具有说明书中所述的含义，对于曲妥单抗的化学衍生物，其制备方法及其作为药物的用途。

10. 发明授权

US4451455A .alpha.-Amylase inactivator, a process for its preparation, an agent based on this inactivator and its use 失效
标题翻译： α-淀粉酶灭活剂，其制备方法，基于该灭活剂的药剂及其用途
公开(公告)号：US4451455A
公开(公告)日：1984-05-29
申请号：US309444
申请日：1981-10-07
申请人： Laszlo Vertesy , Miroslav Mracek , Gerhard Braunitzer , Heinz Aschauer
发明人： Laszlo Vertesy , Miroslav Mracek , Gerhard Braunitzer , Heinz Aschauer
IPC分类号： A61K38/00 , C07K14/36 , A61K37/02 , C07C103/52 , C12P21/00 , C12P21/02
CPC分类号： C12R1/465 , C07K14/36 , A61K38/00 , Y10S930/26
摘要： What are disclosed are two peptides having .alpha.-amylase inactivator activity, a method for making the inhibitors, in combination, by culturing Streptomyces tendae 4158 or Streptomyces tendae HAG 1226, methods for separating the combination into its two components, and methods and compositions for treating diabetes, pre-diabetes, or adiposity by administration of such peptide .alpha.-amylase inhibitors.
摘要翻译：所公开的是具有α-淀粉酶灭活剂活性的两种肽，组合制备抑制剂的方法，通过培养耻骨链霉菌4158或耻骨链球菌HAG 1226，将组合分离成其两种组分的方法，以及用于治疗的方法和组合物糖尿病，前期糖尿病或肥胖，通过施用这种肽α-淀粉酶抑制剂。

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