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公开(公告)号：US09644017B2
公开(公告)日：2017-05-09
申请号：US12820722
申请日：2010-06-22
申请人： Paul Habermann , Gerhard Seipke , Roland Kurrle , Gunter Muller , Mark Sommerfeld , Norbert Tennagels , Georg Tschank , Ulrich Werner
发明人： Paul Habermann , Gerhard Seipke , Roland Kurrle , Gunter Muller , Mark Sommerfeld , Norbert Tennagels , Georg Tschank , Ulrich Werner
摘要： The invention relates to novel insulin analogs having a basal time-action profile, which are characterized by the following features: a) the B chain end consists of an amidated basic amino acid residue such as lysine or arginine amide; b) the N-terminal amino acid residue of the insulin A chain is a lysine or arginine radical; c) the amino acid position A8 is occupied by a histidine radical; d) the amino acid position A21 is occupied by a glycine radical; and e) one or more substitutions and/or additions of negatively charged amino acid residues are carried out in the positions A5, A15, A18, B-1, B0, B1, B2, B3 and B4.
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公开(公告)号：US08603970B2
公开(公告)日：2013-12-10
申请号：US12820727
申请日：2010-06-22
申请人： Paul Habermann , Gerhard Seipke , Roland Kurrle , Gunter Muller , Mark Sommerfeld , Norbert Tennagels , Georg Tschank , Ulrich Werner
发明人： Paul Habermann , Gerhard Seipke , Roland Kurrle , Gunter Muller , Mark Sommerfeld , Norbert Tennagels , Georg Tschank , Ulrich Werner
摘要： The invention relates to novel insulin analogs having a basal time-action profile, which are characterized by the addition and/or substitution of negatively and positively charged amino acid residues and by an amidation of the C-terminal carboxy group of the B chain and histidine in position 8 of the insulin A chain. The invention also relates to the production and use thereof.
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公开(公告)号：US08633156B2
公开(公告)日：2014-01-21
申请号：US12820727
申请日：2010-06-22
申请人： Paul Habermann , Gerhard Seipke , Roland Kurrle , Gunter Muller , Mark Sommerfeld , Norbert Tennagels , Georg Tschank , Ulrich Werner
发明人： Paul Habermann , Gerhard Seipke , Roland Kurrle , Gunter Muller , Mark Sommerfeld , Norbert Tennagels , Georg Tschank , Ulrich Werner
CPC分类号： C07K14/62
摘要： The invention relates to novel insulin analogs having a basal time-action profile, which are characterized by the addition and/or substitution of negatively and positively charged amino acid residues and by an amidation of the C-terminal carboxy group of the B chain and histidine in position 8 of the insulin A chain. The invention also relates to the production and use thereof.
摘要翻译： 本发明涉及具有基础时间作用特征的新型胰岛素类似物，其特征在于负和带正电荷的氨基酸残基的添加和/或取代以及B链和组氨酸的C端羧基的酰胺化 在胰岛素A链的位置8。 本发明还涉及其生产和使用。
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4.发明申请公开(公告)号：US20050106653A1
公开(公告)日：2005-05-19
申请号：US10918015
申请日：2004-08-13
IPC分类号： A61K31/545 , A61K38/00 , C07K14/47 , C12Q1/48
CPC分类号： C07K14/47 , C12Q1/485 , G01N2500/00
摘要： The present invention relates to a method for the identification of an IRS protein kinase inhibitor, comprising the steps of a) bringing into contact PKC-ζ with at least one IRS peptide comprising at least one PKC-ζ-Ser-phosphorylation site in the presence of at least one possible inhibitor, and b) measuring the phosphorylation of the PKC-ζ-Ser-phosphorylation site.
摘要翻译： 本发明涉及一种鉴定IRS蛋白激酶抑制剂的方法，其包括以下步骤：a）在存在的情况下使PKC-ζ与至少一种包含至少一个PKC-ζ-Ser-磷酸化位点的IRS肽接触 的至少一种可能的抑制剂，和b）测量PKC-ζ-Ser-磷酸化位点的磷酸化。
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5.发明申请IMIDAZOPYRIDIN-2-ONE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES 有权作为药物和磷脂抑制剂的咪达唑啶-2-酮衍生物公开(公告)号：US20090076068A1
公开(公告)日：2009-03-19
申请号：US12235053
申请日：2008-09-22
IPC分类号： A61K31/4355 , C07D471/04 , A61K31/437 , A61P3/10 , A61P3/06 , A61P9/10
CPC分类号： C07D471/04
摘要： The present invention relates to imidazopyridin-2-one derivatives of the formula I with the definitions specified in the description, to their pharmaceutically usable salts and to their use as medicaments.
摘要翻译： 本发明涉及式I的咪唑并吡啶-2-酮衍生物，其描述中定义的定义，其药学上可用的盐及其作为药物的用途。
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公开(公告)号：US08357698B2
公开(公告)日：2013-01-22
申请号：US12839863
申请日：2010-07-20
申请人： Gerhard Zoller , Stefan Petry , Gunter Muller , Hubert Heuer , Norbert Tennagels
发明人： Gerhard Zoller , Stefan Petry , Gunter Muller , Hubert Heuer , Norbert Tennagels
IPC分类号： C07D487/04 , A61K31/4375
CPC分类号： C07D231/56 , C07D401/14 , C07D471/04 , C07D495/04
摘要： The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds to treat diabetes mellitus, dyslipidemia and atherosclerotic disorders.
摘要翻译： 本发明涉及通式（I）或（II）的二酰基吲唑衍生物及其药学上可接受的盐：其中X，R 1和R 2如本文所定义。 本发明还涉及这些化合物用于治疗糖尿病，血脂异常和动脉粥样硬化性疾病的用途。
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公开(公告)号：US20080287448A1
公开(公告)日：2008-11-20
申请号：US12099337
申请日：2008-04-08
申请人： Gerhard Zoller , Stefan Petry , Gunter Muller , Hubert Heuer , Norbert Tennagels
发明人： Gerhard Zoller , Stefan Petry , Gunter Muller , Hubert Heuer , Norbert Tennagels
IPC分类号： A61K31/519 , C07D487/04 , C07D471/04 , A61K31/437 , A61P3/00 , A61K31/4985 , A61K31/5025
CPC分类号： C07D231/56 , C07D401/14 , C07D471/04 , C07D495/04
摘要： The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds as pharmaceutical products.
摘要翻译： 本发明涉及通式（I）或（II）的二酰基吲唑衍生物及其药学上可接受的盐：其中X，R 1和R 2如本文所定义。 本发明还涉及这些化合物作为药物产品的用途。
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公开(公告)号：US08921404B2
公开(公告)日：2014-12-30
申请号：US11873846
申请日：2007-10-17
申请人： Gerhard Zoller , Stefan Petry , Gunter Muller , Hubert Heuer , Norbert Tennagels
发明人： Gerhard Zoller , Stefan Petry , Gunter Muller , Hubert Heuer , Norbert Tennagels
IPC分类号： A61K31/4523 , A61K31/423 , A61K31/428 , C07D275/04 , C07D498/04 , C07D261/20 , C07D413/12 , C07D513/04
CPC分类号： C07D261/20 , C07D275/04 , C07D413/12 , C07D513/04
摘要： The invention relates to azole derivatives of the general formula I as defined in the present application as well as to their uses in treatment of conditions that would benefit from their inhibitory effect on hormone sensitive lipase, HSL, an allosteric enzyme in adipocytes which is inhibited by insulin and is responsible for the breakdown of fats in fat cells and thus for transferring fat constituents into the blood stream. Inhibition of this enzyme is therefore equivalent to an insulin-like effect of the compounds of the invention.
摘要翻译： 本发明涉及本申请中定义的通式I的唑衍生物，以及它们在治疗受益于其对激素敏感性脂肪酶HSL（对脂肪细胞中受抑制的脂肪细胞中的变构酶）的抑制作用的条件的用途 胰岛素，并且负责脂肪细胞中脂肪的分解，从而将脂肪成分转移到血液中。 因此，该酶的抑制等同于本发明化合物的胰岛素样效应。
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9.发明授权Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases 有权偶氮吡啶-3-酮衍生物作为脂肪酶和磷脂酶的抑制剂公开(公告)号：US08148395B2
公开(公告)日：2012-04-03
申请号：US12235047
申请日：2008-09-22
申请人： Gerhard Zoller , Stefan Petry , Gunter Muller , Norbert Tennagels
发明人： Gerhard Zoller , Stefan Petry , Gunter Muller , Norbert Tennagels
IPC分类号： A61K31/44 , C07D471/02 , C07D491/02 , C07D498/02
CPC分类号： C07D471/04
摘要： The present invention relates to azolopyridin-3-one derivatives of the general formula I with the meanings indicated in the description, their pharmaceutically usable salts and their use as medicinal substances.
摘要翻译： 本发明涉及通式I的苯并吡喃-3-酮衍生物，其具有说明书中所述的含义，其药学上可用的盐及其作为药用物质的用途。
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10.发明申请AZOLOPYRIDIN-3-ONE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES 有权作为脂蛋白和磷脂酰胺的抑制剂的AZOLOPYRIDIN-3-ONE衍生物公开(公告)号：US20090054478A1
公开(公告)日：2009-02-26
申请号：US12235047
申请日：2008-09-22
申请人： Gerhard Zoller , Stefan Petry , Gunter Muller , Norbert Tennagels
发明人： Gerhard Zoller , Stefan Petry , Gunter Muller , Norbert Tennagels
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to azolopyridin-3-one derivatives of the general formula I with the meanings indicated in the description, their pharmaceutically usable salts and their use as medicinal substances.
摘要翻译： 本发明涉及通式I的苯并吡喃-3-酮衍生物，其具有说明书中所述的含义，其药学上可用的盐及其作为药用物质的用途。
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