-
公开(公告)号：EP1060171A2
公开(公告)日：2000-12-20
申请号：EP99907497.4
申请日：1999-02-04
申请人： Max-Planck-Gesellschaft zur Förderungder Wissenschaften e.V. , Byk Gulden Lomberg Chemische Fabrik GmbH
发明人： BODE, Wolfram , MORODER, Luis , PEREIRA, Pedro Jose Barbosa , BERGNER, Andreas , HUBER, Robert , SOMMERHOFF, Christian , SCHASCHKE, Norbert , BÄR, Thomas , MARTIN, Thomas , STADLWIESER, Josef , ULRICH, Wolf-Rüdiger , DOMINIK, Andreas , THIBAUT, Ulrich , BUNDSCHUH, Daniela , BEUME, Rolf , GOEBEL, Karl-Josef
IPC分类号： C07D295/20 , A61K31/485 , C07D211/58 , A61K31/445 , C07D279/18 , A61K31/155 , C07C237/10 , A61K31/16 , C07D213/44 , C07D213/82
CPC分类号： C07D213/81 , C07C237/22 , C07C279/16 , C07D211/58 , C07D213/82 , C07D295/185 , C07D295/215 , C07D401/14
摘要： The invention relates to bifunctional inhibitors of human tryptase of formula (I), to human tryptase in crystalline form, to a method for producing human tryptase in crystalline form, to pharmaceutical compositions comprising a bifunctional inhibitor of human tryptase, and to a method for developing and identifying tryptase inhibitors. The tryptase inhibitors are characterized in that both head groups K1 and K2 are the same or different and each comprises a group Q which can interact with a carboxylate group. The linker L can assume a conformation such that the groups Q of both head groups are situated at a distance ranging from 20 to 45 Å, such that the dimension of the head groups and of the linker permit the inhibitor to penetrate into a cavity with the dimensions 52 Å X 32 Å X 40 Å, and such that L represents formula (II) wherein A1 and A2 are the same or different, and represent -C(O)-, NH-, -O- (oxygen), -S- (sulfur), -S(O)2-, -S(O)2-NH-, -NH-S(O)2-, -C(O)-NH-, -NH-C(O)-, -O-C(O)-, -C(O)-O- or a bond. A3 and A4 are the same or different and represent -C(O)-, -C(S)-, -O-, -S-, -NH-, -O-C(O)-, -C(O)-O-, -C(O)-NH-, -NH-C(O)- or a bond, or are selected from the group A5, A6, M, B1-B6 as stated in the description.
-
公开(公告)号：EP1060175A2
公开(公告)日：2000-12-20
申请号：EP99910192.6
申请日：1999-02-04
申请人： Max-Planck-Gesellschaft zur Förderungder Wissenschaften e.V. , Byk Gulden Lomberg Chemische Fabrik GmbH
发明人： BODE, Wolfram , MORODER, Luis , PEREIRA, Pedro, Jose, Barbosa , BERGNER, Andreas , HUBER, Robert , SOMMERHOFF, Christian , SCHASCHKE, Norbert , BÄR, Thomas , MARTIN, Thomas , STADLWIESER, Josef , ULRICH, Wolf-Rüdiger , DOMINIK, Andreas , THIBAUT, Ulrich , BUNDSCHUH, Daniela , BEUME, Rolf , GOEBEL, Karl-Josef
IPC分类号： C07D401/12 , C07D295/192 , A61K31/44
CPC分类号： C07D213/81 , C07C279/16 , C07D211/58 , C07D213/82 , C07D295/185 , C07D295/215 , C07D401/14
摘要： The invention relates to compounds of formula (I), wherein M, A1, A2, A3, A4, A5, A6, B1, B2, B3, B4, B5, B6, K1 and K2 have the meanings given in the description. Said compounds are novel effective inhibitors of human tryptase.
摘要翻译： 本发明涉及式（I）的化合物，其中M，A1，A2，A3，A4，A5，A6，B1，B2，B3，B4，B5，B6，K1和K2具有在说明书中给出的含义。 所述化合物是人类类胰蛋白酶的新型有效抑制剂。
-
3.发明公开
公开(公告)号：EP0998487A2
公开(公告)日：2000-05-10
申请号：EP98936310.6
申请日：1998-06-05
发明人： BUDISA, Nediljko , HUBER, Robert , MINKS, Carolin , MORODER, Luis
CPC分类号： A61K47/62
摘要： The invention relates to a pharmaceutical compound containing as an active ingredient at least one pharmacologically active amino acid analogue incorporated into a peptide or polypeptide as carrier or vehicle. The invention also relates to methods for producing such pharmaceutical compounds.
-
公开(公告)号：EP1135486A1
公开(公告)日：2001-09-26
申请号：EP99961054.6
申请日：1999-12-03
发明人： SONDERMANN, Peter , HUBER, Robert , JAKOB, Uwe
IPC分类号： C12N15/12 , C07K14/705 , C12N1/21 , C12N15/70 , G01N33/53 , G01N33/68 , A61K38/17 , C07K17/00
CPC分类号： C07K14/70535 , A61K38/00 , C07K2299/00
摘要： Recombinant soluble Fc receptors according to the present invention are characterized by the absence of transmembrane domains, signal peptides and glycosylation. Such Fc receptors can easily be obtained by expressing respective nucleic acids in prokaryotic host cells and renaturation of the obtained inclusion bodies, which procedure leads to a very homogenous and pure product. The products can be used for diagnostic as well as pharmaceutical applications and also for the generation of crystal structure data. Such crystal structure data can be used for the modelling of artificial molecules. A further embodiment comprises coupling the Fc receptors according to the invention to solid materials like chromatography materials that can be used to separate and/or enrich antibodies.
-
公开(公告)号：EP0968279A1
公开(公告)日：2000-01-05
申请号：EP98917038.6
申请日：1998-03-20
发明人： GROLL, Michael , HUBER, Robert , DITZEL, Lars , ENGH, Richard
IPC分类号： C12N9/60
CPC分类号： C12Y304/25001 , C12N9/60
摘要： The invention relates to a method for the production of a purified eucaryotic crystallizable proteasome preparation, and to the proteasome preparation obtained by this method. The invention also relates to a purified eucaryotic proteasome preparation in crystallized form. With the aid of crystal data from this proteasome preparation, new proteasome inhibitors can be identified and produced, in particular with the aid of computer assisted modelling programmes.
-
公开(公告)号：EP1267854A2
公开(公告)日：2003-01-02
申请号：EP01938022.9
申请日：2001-03-15
发明人： MAGDOLEN, Viktor , SPERL, Stefan , STÜRZEBECHER, Jörg , WILHELM, Olaf , ARROYO-DEPRADA, Nuria , MORODER, Luis , HUBER, Robert , JACOB, Uwe , BODE, Wolfram
IPC分类号： A61K31/00
CPC分类号： C07C279/18 , A61K31/155 , C07C2603/74
摘要： The invention relates to novel selective inhibitors of the urokinase plasminogen activator (uPA, EC 3.4.21.31), of the arylguanidine type.
摘要翻译： 由包含氢键供体和受体基团的侧链取代的芳基 - 胍衍生物（I）是新的。 是由包含氢键供体和受体基团的侧链取代的式（I）的芳基胍衍生物及其盐，是新的。 [图] Ar：芳族或杂芳族环系; X1-CR3R4-C（= X2）-CR6R7R8，-NH-C（O）-CR6R7R8或-CR3R4-C（= X2）-NHR8; R 1 H或（全部任选取代的）烷基，烯基，炔基，芳基和/或杂芳基; （R3）3，-C（R3）2C（R3）3，-OC（R3）3或-OC（R3）2C（R3）3; R3H或卤素（特别是F）; R4-R7H或（全部任选取代的）烷基，烯基或炔基，R4或R5任选地与R6或R7键合，条件是R4和R5中至少一个以及R6和R7中的至少一个含有氢键供体基团; R8H; 烷基，烯基，炔基，芳基和/或杂芳基（全部被取代）; 或SO2R9; 烷基，烯基，炔基，芳基和/或杂芳基; X2氢键受体基团，特别是NH，NR10，O或S; R10烷基，烯基或炔基（全部任意取代）; m：0-4。 - 活动：细胞抑制。 没有给出生物数据。 - 作用机制：尿激酶纤溶酶原激活物（uPA）抑制剂; 尿激酶（UK）抑制剂
-
-
-
-
-
搜索结果
6 条记录 (耗时 0.018 秒)
