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公开(公告)号：US20050187263A1
公开(公告)日：2005-08-25
申请号：US11057263
申请日：2005-02-14
IPC分类号： A61K31/352 , C07D311/02 , A61K7/13
CPC分类号： A61K31/352 , C07D311/02
摘要： Host cells expressing HM74 were used to obtain oxydecalin-like molecules with agonist activity having the following structure:
摘要翻译： 使用表达HM74的宿主细胞获得具有以下结构的激动剂活性的氧六心肌样分子：
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公开(公告)号：US07264937B2
公开(公告)日：2007-09-04
申请号：US11057263
申请日：2005-02-14
IPC分类号： G01N33/53
CPC分类号： A61K31/352 , C07D311/02
摘要： Host cells expressing HM74 were used to obtain oxydecalin-like molecules with agonist activity having the following structure:
摘要翻译： 使用表达HM74的宿主细胞获得具有以下结构的激动剂活性的氧六心肌样分子：
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3.发明授权Pyridine-2,4-and -2,5-dicarboxylic acid amides and medicaments based on these compounds 失效基于这些化合物的吡啶-2,4和-2,5-二羧酸酰胺和药物
公开(公告)号：US5037839A
公开(公告)日：1991-08-06
申请号：US434402
申请日：1989-11-13
申请人： Martin Bickel , Dietrich Brocks , Harald Burghard , Volkmar Gunzler , Stephan Henke , Hartmut Hanauske-Abel , Jurgen Mohr , Georg Tschank
发明人： Martin Bickel , Dietrich Brocks , Harald Burghard , Volkmar Gunzler , Stephan Henke , Hartmut Hanauske-Abel , Jurgen Mohr , Georg Tschank
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/455 , A61P3/00 , A61P37/06 , A61P43/00 , C07D213/81 , C07D213/82 , C07D401/14 , C07D409/14 , C07D417/14
CPC分类号： C07D213/81 , C07D213/82 , C07D401/14 , C07D409/14 , C07D417/14
摘要： The invention relates to pyridine-2,4- and -2,5-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the meanings given, a process for the preparation of these compounds and their use, in particular in medicaments for influencing the metabolism of collagen and collagne-like substances or the biosynthesis of Cl.sub.q.
摘要翻译： 本发明涉及式Ⅰ（I）的吡啶-2,4-和二羧酸衍生物，其中R1，R2，R3，R4和X具有给定的含义，制备方法 的这些化合物及其用途，特别是用于影响胶原蛋白和类似物质的代谢的药物或Clq的生物合成。
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4.发明授权Substituted pyridine-2,4-dicarboxylic acid derivatives and medicaments based on these compounds 失效取代的吡啶-2,4-二羧酸衍生物和基于这些化合物的药物
公开(公告)号：US5004748A
公开(公告)日：1991-04-02
申请号：US164406
申请日：1988-03-04
申请人： Ekkehard Baader , Martin Bickel , Dietrich Brocks , Volkmar Gunzler , Stephan Henke , Hartmut Hanauske-Abel
发明人： Ekkehard Baader , Martin Bickel , Dietrich Brocks , Volkmar Gunzler , Stephan Henke , Hartmut Hanauske-Abel
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P37/06 , A61P43/00 , C07D213/79 , C07D213/81 , C07D401/04 , C07D405/04 , C07D409/04
CPC分类号： C07D213/79 , C07D213/81
摘要： The invention relates to substituted pyridine-2,4-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The invention also relates to a process for the preparation of the abovementioned compounds and to their use as medicaments, in particular as fibrosuppressants and immunosuppressants.
摘要翻译： 本发明涉及式I（I）的取代的吡啶-2,4-二羧酸衍生物，其中R 1和R 2具有给定的含义。 本发明还涉及制备上述化合物的方法及其作为药物的用途，特别是作为纤维抑制剂和免疫抑制剂。
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5.发明授权Peptide derivatives having an inhibitory action on hydroxylating enzymes, a process for their preparation, agents containing them, and their use 失效对羟化酶具有抑制作用的肽衍生物，其制备方法，含有它们的药剂及其用途
公开(公告)号：US4797471A
公开(公告)日：1989-01-10
申请号：US941066
申请日：1986-12-12
CPC分类号： C07K5/0815
摘要： The invention relates to peptide derivatives of the formula ##STR1## in which ##STR2## represents an acyl radical, B represents the radical of a dipeptide composed of a N.sup..omega. -acylated basic .alpha.-amino acid and another .alpha.-amino acid, and W represents hydroxyl or optionally substituted amino, to a process for their preparation, to agents containing them, and to their use.
摘要翻译： 本发明涉及式“IMAGE”的肽衍生物，其中“IMAGE”表示酰基，B表示由Nω-酰化的碱式α-氨基酸和另一种α-氨基酸组成的二肽的基团，W表示W 表示羟基或任选取代的氨基，其制备方法，含有它们的试剂及其用途。
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6.发明授权Use of peptidic bradykinin antagonists for the treatment and prevention of Alzheimer's disease 失效使用肽缓激肽拮抗剂治疗和预防阿尔茨海默病公开(公告)号：US06245736B1
公开(公告)日：2001-06-12
申请号：US08949496
申请日：1997-10-14
申请人： Holger Heitsch , Stephan Henke , Gerhard Breipohl , Jochen Knolle , Klaus Wirth , Gabriele Wiemer
发明人： Holger Heitsch , Stephan Henke , Gerhard Breipohl , Jochen Knolle , Klaus Wirth , Gabriele Wiemer
IPC分类号： A61K3800
CPC分类号： A61K38/043 , C07K7/18
摘要： The invention relates to the use of bradykinin antagonists for the production of pharmaceuticals for the treatment and prevention of Alzheimer's disease. Suitable bradykinin antagonists are peptides which inhibit the effects of the Alzheimer's protein amyloid (&bgr;/A4) on isolated endothelial cells. A particularly suitable peptide is H-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg-OH (HOE 140) and its physiologically tolerable salts.
摘要翻译： 本发明涉及缓激肽拮抗剂在制备用于治疗和预防阿尔茨海默病的药物中的用途。 合适的缓激肽拮抗剂是抑制阿尔茨海默氏蛋白淀粉样蛋白（β/ A4）对分离的内皮细胞的影响的肽。 特别合适的肽是H-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg-OH（HOE 140）及其生理上可耐受的盐。
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公开(公告)号：US5206343A
公开(公告)日：1993-04-27
申请号：US360177
申请日：1989-06-01
申请人： Stephan Henke , Dietrich Brocks , Volkmar Gunzlen-Pukall , Kari I. Kivirikko , Raili M. H. Myllyla
发明人： Stephan Henke , Dietrich Brocks , Volkmar Gunzlen-Pukall , Kari I. Kivirikko , Raili M. H. Myllyla
IPC分类号： C07D233/02 , A61K38/00 , A61K38/55 , A61P1/16 , A61P9/10 , A61P11/00 , A61P17/00 , A61P35/00 , A61P37/06 , C07D231/04 , C07D263/04 , C07D263/06 , C07D265/30 , C07D277/06 , C07K1/113 , C07K5/06 , C07K5/065 , C07K5/08 , C07K5/087
CPC分类号： C07K5/0812 , C07K5/06078 , A61K38/00
摘要： The invention relates to compounds of the formula I ##STR1## in which A denotes an optionally substituted radical from the series comprising alkyl, acyl, cycloalkyl, aryl and heteroaryl; Cyc represents an optionally substituted heterocyclic carbonyl compound; D represents NH, NCH.sub.3, O or CH.sub.2 ; E represents CHOH, CO, SO or optionally N-substituted C.dbd.NH; F represents O, NH, NCH.sub.3 or a bond; R.sup.4 denotes an optionally substituted radical from the series comprising alkyl, cycloalkyl, aryl and heteroaryl; and R.sup.8 denotes hydrogen or optionally substituted alkyl, to a process for the preparation thereof, and to the use thereof as inhibitors of prolyl hydroxylase.
摘要翻译： 本发明涉及式Ⅰ（I）的化合物，其中A表示包含烷基，酰基，环烷基，芳基和杂芳基的系列中任意取代的基团; Cyc表示任选取代的杂环羰基化合物; D表示NH，NCH 3，O或CH 2; E表示CHOH，CO，SO或任选的N-取代的C = NH; F表示O，NH，NCH 3或键; R4表示包含烷基，环烷基，芳基和杂芳基的任选取代的基团; R8表示氢或任意取代的烷基，用于其制备方法，以及作为脯氨酰羟化酶抑制剂的用途。
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8.发明授权Substituted pyridine-2,4-dicarboxylic acid compounds and methods of use thereof 失效取代的吡啶-2,4-二羧酸化合物及其使用方法
公开(公告)号：US5143926A
公开(公告)日：1992-09-01
申请号：US606451
申请日：1990-10-31
申请人： Ekkehard Baader , Martin Bickel , Dietrich Brocks , Volkmar Gunzler , Stephan Henke , Hartmut Hanauske-Abel
发明人： Ekkehard Baader , Martin Bickel , Dietrich Brocks , Volkmar Gunzler , Stephan Henke , Hartmut Hanauske-Abel
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P37/06 , A61P43/00 , C07D213/79 , C07D213/81 , C07D401/04 , C07D405/04 , C07D409/04
CPC分类号： C07D213/79 , C07D213/81
摘要： The invention relates to substituted pyridine-2,4-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The invention also relates to a process for the preparation of the abovementioned compounds and to their use as medicaments, in particular as fibrosuppressants and immunosuppressants.
摘要翻译： 本发明涉及式I（I）的取代的吡啶-2,4-二羧酸衍生物，其中R 1和R 2具有给定的含义。 本发明还涉及制备上述化合物的方法及其作为药物的用途，特别是作为纤维抑制剂和免疫抑制剂。
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9.发明授权Cyclohexapeptides and their mixtures, a process for preparing them, and their use 失效环己肽及其混合物，其制备方法及其用途
公开(公告)号：US6080719A
公开(公告)日：2000-06-27
申请号：US606711
申请日：1996-02-23
申请人： Stephan Henke , Birgit Jordan , Jochen Knolle , Leander Lauffer , Susanne Feiertag , Karl-Heinz Wiesmuller , Gunther Jung
发明人： Stephan Henke , Birgit Jordan , Jochen Knolle , Leander Lauffer , Susanne Feiertag , Karl-Heinz Wiesmuller , Gunther Jung
摘要： The invention relates to compounds of the formula Icyclo(A-B-C-E-F-(D)-Ala) (I)in which A, B, C, E and F are each independently the residue of a natural amino acid other than cysteine (Cys) and tryptophan (Trp), their mixtures and their physiologically tolerated salts; to a process for their preparation and to their use for preparing a diagnostic agent, a medicament for the treatment or prophylaxis of allergies and infections, or a scientific tool for inhibiting the binding of interleukin-4 (IL-4) to the IL-4 receptor.
摘要翻译： 本发明涉及式I环（ABCEF-（D）-Ala）（I）的化合物，其中A，B，C，E和F各自独立地是除半胱氨酸（Cys）和色氨酸之外的天然氨基酸的残基 （Trp），它们的混合物及其生理耐受盐; 其制备方法及其用于制备诊断剂的用途，用于治疗或预防过敏和感染的药物，或用于抑制白细胞介素-4（IL-4）与IL-4（IL-4）结合的科学工具 受体。
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10.发明授权2,3-disubstituted isoxazolidines, a process for their preparation, agents containing them, and their use 失效2,3-二取代的异恶唑烷，其制备方法，含有它们的试剂及其用途
公开(公告)号：US5610146A
公开(公告)日：1997-03-11
申请号：US393814
申请日：1995-02-24
申请人： Stephan Henke , Dietrich Brocks , Volkmar G unzler
发明人： Stephan Henke , Dietrich Brocks , Volkmar G unzler
IPC分类号： C07D261/02 , A61K31/42 , A61K38/00 , A61P1/16 , A61P9/10 , A61P11/00 , A61P17/00 , A61P43/00 , C07K5/08 , C07K5/083 , C07K5/087 , C07K5/09 , C07K5/093 , C07K5/097 , A61K38/05 , G07D261/02
CPC分类号： C07K5/0823 , C07K5/0806 , C07K5/0812 , C07K5/0815 , C07K5/0819
摘要： The invention relates to compounds of the formula ##STR1## in which A denotes an optionally substituted radical from the series comprising alkyl, acyl, cycloalkyl, aryl and heteroaryl; A.sup.1 represents CO, CS, C.dbd.NH, CN-alkyl, CN--O-alkyl, SO, optionally substituted CH.sub.2 or a bond; A.sup.2 represents NH, NCH.sub.3, O, CH.sub.2 or a bond; E represents CHOH, CO, SO or optionally N-substituted C.dbd.NH; A.sup.3 represents O, NH, NCH.sub.3 or a bond; R.sup.4 denotes an optionally substituted radical from the series comprising alkyl, cycloalkyl, aryl and heteroaryl; and R.sup.8 denotes hydrogen or optionally substituted alkyl, to a process for their preparation, and to their use as inhibitors of prolyl hydroxylase.
摘要翻译： 本发明涉及式（I）的化合物，其中A表示包含烷基，酰基，环烷基，芳基和杂芳基的任选取代的基团; A1表示CO，CS，C = NH，CN-烷基，CN-O-烷基，SO，任选取代的CH 2或键; A2表示NH，NCH 3，O，CH 2或键; E表示CHOH，CO，SO或任选的N-取代的C = NH; A3表示O，NH，NCH 3或键; R4表示包含烷基，环烷基，芳基和杂芳基的任选取代的基团; R8表示氢或任意取代的烷基，用于制备它们的方法，以及它们作为脯氨酰羟化酶抑制剂的用途。
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