公开(公告)号：EP0906572B1

公开(公告)日：2002-04-03

申请号：EP97927032.9

申请日：1997-05-23

申请人： BAYER AG

发明人： KRAHN, Thomas ,  PAFFHAUSEN, Wolfgang ,  SCHADE, Andreas ,  BECHEM, Martin ,  SCHMIDT, Delf

IPC分类号： G01N33/543 ,  G01N33/53 ,  G01N33/50

CPC分类号： G01N33/542 ,  G01N33/5005 ,  G01N33/5306 ,  G01N33/54393 ,  Y10S436/80 ,  Y10S436/805 ,  Y10S436/823 ,  Y10T436/13

摘要： In a procedure for quantitative optical analysis of fluorescently-labelled biological cells (5) a cell layer is appplied to a transparent carrier at the base (2) of a reaction vessel (1) so that it is in contact with the solution (3) containing the fluorescent dye (4). The sensitivity of the determination may be significantly improved by adding to the solution (3) a masking dye (9), which absorbs the exciting light (6) for the fluorescent dye (4) already present in the solution (3) and/or its emitted light (7), and/or by applying an interlayer (10) that is permeable to the solution but absorbs and/or reflects the exciting light (6) or the emitted light (7) to the cell layer at the base (2). The same procedure may be used to improve sensitivity in quantitative optical analysis of a luminescent biological cell layer. In the latter case the interlayer (10) should be composed so that is possesses a high reflection factor with respect to luminescent light (11). Analogously, these procedural principles may also be applied in receptor studies to mask disturbing background radiation in quantitative optical analysis of fluorescently- or luminescently-labelled participants in a reaction. In this case a receptor layer (12) is placed at the base (2) of a reaction vessel (1) in contact with a solution (supernatant 3) in which a fluorescent or luminescent ligand (13) has been dissolved. The sensitivity and accuracy of the determination may be significantly improved if a masking dye (9) which absorbs the exciting light (6) for the fluorescent dye and/or its emitted light or (in case of luminescent ligands) the luminescent light is added to the supernatant (3). An interlayer (10) that is permeable to the solution (3) but absorbs and/or reflects the exciting light (6) and/or the emitted light or the luminescent light may be applied to the cell or receptor layer (12) at the base (2) instead of the masking dye in the solution (3) or possibly as a supplementary measure.

公开(公告)号：EP0970053A1

公开(公告)日：2000-01-12

申请号：EP98912383.1

申请日：1998-02-24

申请人： BAYER AG

发明人： MÜLLER-GLIEMANN, Matthias ,  ANGERBAUER, Rolf ,  BRANDES, Arndt ,  LÖGERS, Michael ,  SCHMECK, Carsten ,  SCHMIDT, Gunter ,  BREMM, Klaus-Dieter ,  BISCHOFF, Hilmar ,  SCHMIDT, Delf

IPC分类号： C07D215/20 ,  A61K31/47 ,  C07F7/18

CPC分类号： C07D215/20 ,  C07F7/1856

摘要： The invention relates to substituted chinolines of general formula (I) which are highly effective inhibitors of cholesterol ester transfer proteins (CTEP) and stimulate reverse cholesterol transfer. The inventive substances lower the LDL cholesterol level in the blood while at the same time increasing the HDL cholesterol level. Said substances can therefore be used in the treatment and prevention of hyperlipoproteinemia, hypolipoproteinimia, dyslipidiemia, hypertriglyceridemia, combined hyperlipidemia or arteriosclerosis.

公开(公告)号：EP0973744A1

公开(公告)日：2000-01-26

申请号：EP98904126.4

申请日：1998-01-23

申请人： BAYER AG

发明人： SCHMECK, Carsten ,  BRANDES, Arndt ,  LÖGERS, Michael ,  SCHMIDT, Gunter ,  BREMM, Klaus-Dieter ,  BISCHOFF, Hilmar ,  SCHMIDT, Delf ,  SCHUHMACHER, Joachim

IPC分类号： C07D213/74 ,  C07D401/04 ,  A61K31/44

CPC分类号： C07D213/74 ,  C07D401/04

摘要： The invention relates to novel 2-amino-substituted pyridines which are produced by first converting corresponding pyridine aldehydes into the corresponding hydroxides by means of metal-organic compounds such as Grignard compounds, and then reducing said hydroxides to a deshydroxy compound. The novel 2-amino-substituted pyridines are suitable for use as active ingredients in medicaments, particularly those used in the treatment of arteriosclerosis.

公开(公告)号：EP0906572A1

公开(公告)日：1999-04-07

申请号：EP97927032.0

申请日：1997-05-23

申请人： BAYER AG

发明人： KRAHN, Thomas ,  PAFFHAUSEN, Wolfgang ,  SCHADE, Andreas ,  BECHEM, Martin ,  SCHMIDT, Delf

IPC分类号： G01N33

CPC分类号： G01N33/542 ,  G01N33/5005 ,  G01N33/5306 ,  G01N33/54393 ,  Y10S436/80 ,  Y10S436/805 ,  Y10S436/823 ,  Y10T436/13

摘要： In a procedure for quantitative optical analysis of fluorescently-labelled biological cells (5) a cell layer is appplied to a transparent carrier at the base (2) of a reaction vessel (1) so that it is in contact with the solution (3) containing the fluorescent dye (4). The sensitivity of the determination may be significantly improved by adding to the solution (3) a masking dye (9), which absorbs the exciting light (6) for the fluorescent dye (4) already present in the solution (3) and/or its emitted light (7), and/or by applying an interlayer (10) that is permeable to the solution but absorbs and/or reflects the exciting light (6) or the emitted light (7) to the cell layer at the base (2). The same procedure may be used to improve sensitivity in quantitative optical analysis of a luminescent biological cell layer. In the latter case the interlayer (10) should be composed so that is possesses a high reflection factor with respect to luminescent light (11). Analogously, these procedural principles may also be applied in receptor studies to mask disturbing background radiation in quantitative optical analysis of fluorescently- or luminescently-labelled participants in a reaction. In this case a receptor layer (12) is placed at the base (2) of a reaction vessel (1) in contact with a solution (supernatant 3) in which a fluorescent or luminescent ligand (13) has been dissolved. The sensitivity and accuracy of the determination may be significantly improved if a masking dye (9) which absorbs the exciting light (6) for the fluorescent dye and/or its emitted light or (in case of luminescent ligands) the luminescent light is added to the supernatant (3). An interlayer (10) that is permeable to the solution (3) but absorbs and/or reflects the exciting light (6) and/or the emitted light or the luminescent light may be applied to the cell or receptor layer (12) at the base (2) instead of the masking dye in the solution (3) or possibly as a supplementary measure.

公开(公告)号：EP0674638A1

公开(公告)日：1995-10-04

申请号：EP94902722.0

申请日：1993-12-08

申请人： BAYER AG

发明人： ANGERBAUER, Rolf ,  FEY, Peter ,  HÜBSCH, Walter ,  PHILIPPS, Thomas ,  BISCHOFF, Hilmar ,  KRAUSE, Hans-Peter ,  PETERSEN VON GEHR, Jörg ,  SCHMIDT, Delf

IPC分类号： C07D233 ,  A61K31 ,  A61P9 ,  A61P43 ,  C07C29 ,  C07C33 ,  C07C45 ,  C07C47 ,  C07C69 ,  C07D207 ,  C07D209 ,  C07D215 ,  C07D307 ,  C07D333 ,  C07D471 ,  C07F9

CPC分类号： C07F9/6561 ,  C07C33/28 ,  C07C33/36 ,  C07C33/38 ,  C07C69/013 ,  C07D209/12 ,  C07F9/3211

摘要： Substituted triols of Formula D-R wherein R represents the group of Formulae (a), (b), (c) or (d), can be used as active substances in drugs against hyperproteinemia.

公开(公告)号：EP1087950A1

公开(公告)日：2001-04-04

申请号：EP99929179.2

申请日：1999-06-11

申请人： BAYER AG

发明人： LENSKY, Stephan ,  RIEDL, Bernd ,  FÜRSTNER, Chantal ,  ERGÜDEN, Jens ,  BÖSS, Frank ,  SCHMIDT, Bernard ,  VAN DER STAAY, Franz-Josef ,  SCHRÖDER, Werner ,  SCHUHMACHER, Joachim ,  SCHMIDT, Delf

IPC分类号： C07D261/12 ,  C07D413/06 ,  A61K31/42

CPC分类号： C07D413/06 ,  C07D261/12

摘要： The invention relates to new 2-aminocarbonyl-5(2H)-isoxazolones used as selective ligands of a high-affinity binding site of diisopropyl-fluorophosphate (DFP) on brain membranes, for prophylaxis and treatment of diseases of the central nervous system, especially cognitive disorders, depression, schizophrenia and anxiety.

公开(公告)号：EP0934274A1

公开(公告)日：1999-08-11

申请号：EP97936259.0

申请日：1997-07-29

申请人： Bayer Corporation ,  BAYER AG

发明人： SCHMIDT, Gunter ,  ANGERBAUER, Rolf ,  BRANDES, Arndt ,  MULLER-GLIEMANN, Matthias ,  BISCHOFF, Hilmar ,  SCHMIDT, Delf ,  WOHLFEIL, Stefan ,  SCHOEN, William, R. ,  LADOUCEUR, Gaetan, H. ,  COOK, James, H., II ,  LEASE, Timothy, G. ,  WOLANIN, Donald, J. ,  KRAMSS, Richard, H. ,  HERTZOG, Donald, L. ,  OSTERHOUT, Martin, H.

IPC分类号： C07C33 ,  A61K31 ,  A61P3 ,  C07C39 ,  C07C43 ,  C07C323 ,  C07D213 ,  C07D215 ,  C07D221 ,  C07D275 ,  C07D277 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D407 ,  C07D409 ,  C07D411 ,  C07D413 ,  C07D417 ,  C07D419 ,  C07D487 ,  C07D521 ,  C07F7 ,  C07D211

CPC分类号： C07D213/30 ,  C07D213/32 ,  C07D213/34 ,  C07D213/38 ,  C07D213/50 ,  C07D213/55 ,  C07D213/64 ,  C07D213/70 ,  C07D213/74 ,  C07D213/80 ,  C07D215/14 ,  C07D221/04 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D411/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07F7/1856

摘要： Substituted pyridines of formula (IA) are produced by reaction of suitably substituted pyridylaldehydes with Grignard or Witting reagents, and the resulting products are appropriately reduced. The pyridines of formula (IA) are suitable as active compounds in pharmaceutical products, particularly in pharmaceutical products for the inhibition of cholesterol ester transfer proteins. 3-Heteroalkyl-aryl-substituted pyridines of formula (IB) are produced from pyridines which are correspondingly protected at the hydroxy group and correspondingly substituted. The compounds of formula (IB) according to the invention are suitable as active compounds in pharmaceutical products, particularly pharmaceutical products for the treatment of hyperlipoproteinemia. Substituted pyridines and benzenes of formula (IC) are produced by procedures disclosed herein, and are useful as active ingredients in pharmaceutical products, particularly pharmaceutical products for inhibition of the glucagon receptor, leading to treatment of glucagon-mediated conditions such as diabetes.

摘要翻译： 式（IA）的取代的吡啶通过适当取代的吡啶基醛与格氏试剂或Witting试剂反应而生成，并且所得产物被适当还原。 式（IA）的吡啶适于作为药物产品中的活性化合物，特别是用于抑制胆固醇酯转移蛋白的药物产品中。 式（IB）的3-杂烷基 - 芳基取代的吡啶由在羟基处相应保护并相应地被取代的吡啶制备。 根据本发明的式（IB）化合物适合作为药物产品中的活性化合物，特别是用于治疗高脂蛋白血症的药物产品。 式（IC）的取代的吡啶和苯是通过本文公开的方法制备的，并且可用作药物产品中的活性成分，特别是用于抑制胰高血糖素受体的药物产品，导致治疗胰高血糖素介导的病症例如糖尿病。

公开(公告)号：EP1017659A1

公开(公告)日：2000-07-12

申请号：EP98951408.8

申请日：1998-09-16

申请人： BAYER AG

发明人： BRANDES, Arndt ,  LÖGERS, Michael ,  STOLTEFUSS, Jürgen ,  SCHMIDT, Gunter ,  BREMM, Klaus-Dieter ,  BISCHOFF, Hilmar ,  SCHMIDT, Delf ,  ANTONS, Stefan ,  PAULSEN, Holger ,  MÜLLER, Stephan, Nicholas ,  NAAB, Paul ,  SCHMECK, Carsten

IPC分类号： C07C35/52 ,  C07C43/192 ,  C07C49/813 ,  C07C49/83 ,  C07F7/18

CPC分类号： C07C69/76 ,  C07C35/52 ,  C07C43/192 ,  C07C49/83 ,  C07C69/757 ,  C07C69/94 ,  C07F7/1856

摘要： The invention relates to substituted tetrahydronaphthaline and analogous compounds which are produced by reducing or condensing corresponding functional substituents to substituted tetrahydronaphthaline and analogous compounds according to usual methods. In addition, functional groups are converted to the desired groups in the same manner. The inventive compounds are suited for additives in medicaments especially in medicaments for treating arteriosclerosis and dyslipidaemia.

公开(公告)号：EP0968162A1

公开(公告)日：2000-01-05

申请号：EP98905338.4

申请日：1998-01-23

申请人： BAYER AG

发明人： MÜLLER-GLIEMANN, Matthias ,  ANGERBAUER, Rolf ,  BRANDES, Arndt ,  LÖGERS, Michael ,  SCHMECK, Carsten ,  SCHMIDT, Gunter ,  BREMM, Klaus-Dieter ,  BISCHOFF, Hilmar ,  SCHMIDT, Delf

IPC分类号： C07C33/50 ,  C07C43/178 ,  C07C49/83 ,  C07C33/46 ,  A61K31/045 ,  A61K31/075 ,  A61K31/12

CPC分类号： C07C33/26 ,  C07C33/34 ,  C07C43/1786 ,  C07C49/83 ,  C07C69/76 ,  C07C2601/08

摘要： The invention relates to novel 5-hydroxyalkyl substituted phenyls, which are produced either by reacting corresponding benzaldehydes with Grignard compounds and then reduces the remaining functional groups, or by reducing corresponding benzoic acid esters according to the usual methods to the corresponding hydroxy compounds. The 5-hydroxyalkyl substituted phenyls are suitable as active substances in medicaments, especially for the treatment of dyslipidaemia.

摘要翻译： PCT号 PCT / EP98 / 00361秒。 日期月371 2，1999秒。 102（e）中的日期九月 2，1999年PCT提起1998年1月23日的PCT公布。 号 WO98 / 34895的PCT公布。 8月13日的日期，一九九八年新颖5-羟基烷基苯substituiertem通过要么制备的格利雅化合物反应的相应的苯甲醛，并随后降低了其它官能团或通过减少通过常规方法相应的苯甲酸酯，得到相应的羟基化合物 ， 的5-羟基烷基苯substituiertem是适合用作用于血脂异常的治疗药物中的活性化合物，特别是。

公开(公告)号：EP0674638B1

公开(公告)日：1998-03-18

申请号：EP94902722.1

申请日：1993-12-08

申请人： BAYER AG

发明人： ANGERBAUER, Rolf ,  FEY, Peter ,  HÜBSCH, Walter ,  PHILIPPS, Thomas ,  BISCHOFF, Hilmar ,  KRAUSE, Hans-Peter ,  PETERSEN VON GEHR, Jörg ,  SCHMIDT, Delf

IPC分类号： C07D471/04 ,  A61K31/435 ,  A61K31/34 ,  A61K31/38 ,  A61K31/40 ,  A61K31/47 ,  A61K31/045 ,  A61K31/415 ,  A61K31/22 ,  A61K31/35 ,  A61K31/66

CPC分类号： C07F9/6561 ,  C07C33/28 ,  C07C33/36 ,  C07C33/38 ,  C07C69/013 ,  C07D209/12 ,  C07F9/3211