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公开(公告)号：US08759386B2
公开(公告)日：2014-06-24
申请号：US13353621
申请日：2012-01-19
IPC分类号： A61K31/4155 , C07D231/10 , C07D403/12 , C07D405/12 , C07D409/12
CPC分类号： C07D403/12 , C07D405/12 , C07D409/12
摘要： Pyrazole compounds of formula (Ia) or (Ib) and pharmaceutically acceptable salts thereof, wherein Ra, Rb, Rc, Rd, Y1, Y2, Y3, Y4, Y5, Z, R1, R2, n and R3 have one of the meanings as indicated in the specification and claims, to their use as medicaments, to pharmaceutical formulations containing the compounds and to pharmaceutical formulations containing the compounds in combination with one or more active substances.
摘要翻译： 式（Ia）或（Ib）的吡唑化合物及其药学上可接受的盐，其中Ra，Rb，Rc，Rd，Y1，Y2，Y3，Y4，Y5，Z，R1，R2，n和R3具有以下含义之一 如说明书和权利要求书中所指出的，它们作为药物的用途，含有该化合物的药物制剂和含有与一种或多种活性物质组合的化合物的药物制剂。
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公开(公告)号：US20130023576A1
公开(公告)日：2013-01-24
申请号：US13353621
申请日：2012-01-19
IPC分类号： A61K31/4155 , C07D405/12 , C07D409/12 , A61P29/00 , A61P31/00 , A61P27/14 , A61P11/00 , A61P1/00 , A61P19/02 , A61P37/08 , A61P11/06 , C07D403/12 , A61P37/02
CPC分类号： C07D403/12 , C07D405/12 , C07D409/12
摘要： Pyrazole compounds of formula (Ia) or (Ib) and pharmaceutically acceptable salts thereof, wherein Ra, Rb, Rc, Rd, Y1, Y2, Y3, Y4, Y5, Z, R1, R2, n and R3 have one of the meanings as indicated in the specification and claims, to their use as medicaments, to pharmaceutical formulations containing the compounds and to pharmaceutical formulations containing the compounds in combination with one or more active substances.
摘要翻译： 式（Ia）或（Ib）的吡唑化合物及其药学上可接受的盐，其中Ra，Rb，Rc，Rd，Y1，Y2，Y3，Y4，Y5，Z，R1，R2，n和R3具有以下含义之一 如说明书和权利要求书中所指出的，它们作为药物的用途，含有该化合物的药物制剂和含有与一种或多种活性物质组合的化合物的药物制剂。
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公开(公告)号：US09206164B2
公开(公告)日：2015-12-08
申请号：US14006170
申请日：2012-03-15
申请人： Domnic Martyres , Ralf Anderskewitz , Christoph Hoenke , Jan Kriegl , Thorsten Oost , Wolfgang Rist , Peter Seither
发明人： Domnic Martyres , Ralf Anderskewitz , Christoph Hoenke , Jan Kriegl , Thorsten Oost , Wolfgang Rist , Peter Seither
IPC分类号： A61K31/335 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/4164 , A61K31/421 , A61K31/426 , C07D403/10 , C07D471/04 , C07D487/04 , A61K31/4155 , A61K31/4184 , A61K31/437 , A61K31/52 , A61K45/06 , C07D473/00
CPC分类号： C07D403/10 , A61K31/335 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4184 , A61K31/421 , A61K31/437 , A61K31/52 , A61K45/06 , C07D471/04 , C07D473/00 , C07D487/04
摘要： The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2 antagonistic activity, wherein L, Y1, Y2, Y3, Y4, Y5, Z, R1, R2, R3 and n have one of the meanings as indicated in the specification and claims, to their use as medicaments, to pharmaceutical compositions containing said compounds and to pharmaceutical compositions containing said compounds in combination with one or more active substances.
摘要翻译： 本发明涉及具有CRTH2拮抗活性的式（I）的吡唑化合物及其药学上可接受的盐，其中L，Y1，Y2，Y3，Y4，Y5，Z，R1，R2，R3和n具有以下含义之一： 在说明书和权利要求书中指出其作为药物的用途，含有所述化合物的药物组合物和含有所述化合物与一种或多种活性物质组合的药物组合物。
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公开(公告)号：US08791272B2
公开(公告)日：2014-07-29
申请号：US13012244
申请日：2011-01-24
申请人： Thorsten Oost , Ralf Anderskewitz , Dieter Wolfgang Hamprecht , Christoph Hoenke , Domnic Martyres , Wolfgang Rist , Peter Seither
发明人： Thorsten Oost , Ralf Anderskewitz , Dieter Wolfgang Hamprecht , Christoph Hoenke , Domnic Martyres , Wolfgang Rist , Peter Seither
IPC分类号： C07D231/12 , A61K31/415 , C07D405/12 , C07D401/06
CPC分类号： C07D231/12 , C07D401/06 , C07D405/12
摘要： The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2-activity, wherein W, L1, L2, X, L3, Y, R1 and R2 are as defined in the specification and claims, to their use as medicaments and to pharmaceutical formulations, containing said compounds or containing a combination of said compounds with one or more active substances.
摘要翻译： 本发明涉及具有CRTH2-活性的式（I）的吡唑化合物及其药学上可接受的盐，其中W，L1，L2，X，L3，Y，R1和R2如说明书和权利要求中所定义， 作为药物和药物制剂，含有所述化合物或含有所述化合物与一种或多种活性物质的组合。
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5.发明申请Novel n-(heterobicycloalkanes)-substituted indoles-or heteroderivatives thereof 审中-公开新的n-（杂双环烷烃） - 取代的吲哚或其异构衍生物公开(公告)号：US20050014782A1
公开(公告)日：2005-01-20
申请号：US10886973
申请日：2004-07-08
申请人： Ralf Anderskewitz , Franz Birke , Thierry Bouyssou , Horst Dollinger , Domnic Martyres , Pascale Pouzet
发明人： Ralf Anderskewitz , Franz Birke , Thierry Bouyssou , Horst Dollinger , Domnic Martyres , Pascale Pouzet
IPC分类号： A61K31/46 , C07D451/04 , C07D453/04
CPC分类号： C07D451/04 , A61K31/46
摘要： Use of a compound of general formula 1 for manufacturing a medicament to provide agonists or antagonists of CCR-3, or pharmaceutically acceptable salts thereof, in particular compounds of formula 1: wherein R1, R5, R6, A, B, X, W, Z, i, j, k, l and m are defined as in the description and claims. It is another object of the present invention to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
摘要翻译： 通式1的化合物用于制备药物以提供CCR-3的激动剂或拮抗剂或其药学上可接受的盐，特别是式1化合物的用途：其中R 1，R 5，R 6， 在说明书和权利要求书中定义了A，B，X，W，Z，i，j，k，l和m。 本发明的另一个目的是提供包含药学上可接受的载体和治疗有效量的至少一种本发明化合物或其药学上可接受的盐的药物组合物。
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公开(公告)号：US09115142B2
公开(公告)日：2015-08-25
申请号：US14134367
申请日：2013-12-19
申请人： Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
发明人： Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
IPC分类号： C07D495/04 , A61K31/519 , C07D519/00
CPC分类号： C07D495/04 , A61K31/519 , A61K2300/00
摘要： Dihydrothienopyrimidinesulphoxides of formula 1 wherein X is SO or SO2, R1 is H or C1-6-alkyl, R2 is H or an organic group as disclosed herein, and R3 is an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl, and the pharmacologically acceptable salts thereof, as well as pharmaceutical compositions which contain these compounds. These dihydrothienopyrimidinesulphoxides are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system, or cancers.
摘要翻译： 式1的二氢噻吩并嘧啶亚砜，其中X是SO或SO 2，R 1是H或C 1-6 - 烷基，R 2是H或如本文所公开的有机基团，并且R 3是任选取代的单或双环不饱和的，部分饱和的或饱和的 杂环或任选取代的单环或双环杂芳基及其药理学上可接受的盐，以及含有这些化合物的药物组合物。 这些二氢噻吩并嘧啶亚砜适用于治疗呼吸道或胃肠道疾病，关节，皮肤或眼睛的炎性疾病，外周或中枢神经系统疾病或癌症。
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公开(公告)号：US08754073B2
公开(公告)日：2014-06-17
申请号：US12738344
申请日：2008-10-16
申请人： Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
发明人： Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
IPC分类号： C07D495/04 , A61K31/519 , A61P29/00 , A61P11/06 , A61P25/28
CPC分类号： C07D495/04 , C07D519/00
摘要： Piperidinodihydrothienopyrimidines of formula 1 wherein X is SO or SO2 (preferably SO), and R1, R2, R3, and R4 may have the meanings given in the disclosure and claims, pharmacologically acceptable salts thereof, and pharmaceutical compositions containing these compounds. These piperidinodihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system, or cancers.
摘要翻译： 其中X为SO或SO 2（优选为SO）的R1为吡啶并二氢噻吩并嘧啶，R1，R2，R3和R4可具有本公开和权利要求书中给出的含义，其药理学上可接受的盐，以及含有这些化合物的药物组合物。 这些哌啶二氢噻吩并嘧啶适用于治疗呼吸道或胃肠道疾病，关节，皮肤或眼睛的炎性疾病，外周或中枢神经系统疾病或癌症。
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公开(公告)号：US20060030590A1
公开(公告)日：2006-02-09
申请号：US11191539
申请日：2005-07-28
IPC分类号： A61K31/454 , C07D403/02
CPC分类号： C07D401/06
摘要： A compound of general formula 1a wherein R1, R5, R6, A, B, Y, i, j and m are defined as in the description and claims. It is another object of the present invention to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
摘要翻译： 定义了通式1a的化合物，其中R 1，R 5，R 6，A，B，Y，i，j和m定义 如在说明书和权利要求中所述。 本发明的另一个目的是提供包含药学上可接受的载体和治疗有效量的至少一种本发明化合物或其药学上可接受的盐的药物组合物。
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公开(公告)号：US08637519B2
公开(公告)日：2014-01-28
申请号：US12738429
申请日：2008-10-16
申请人： Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
发明人： Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
IPC分类号： C07D495/04 , A61K31/519 , A61P11/06 , A61P25/28 , A61P25/24 , A61P25/22 , A61P25/18 , A61P35/00
CPC分类号： C07D495/04 , A61K31/519 , A61K2300/00
摘要： Dihydrothienopyrimidinesulphoxides of formula 1 wherein X is SO or SO2, R1 is H or C1-6-alkyl, R2 is H or an organic group as disclosed herein, and R3 is an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl, and the pharmacologically acceptable salts thereof, as well as pharmaceutical compositions which contain these compounds. These dihydrothienopyrimidinesulphoxides are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system, or cancers.
摘要翻译： 式1的二氢噻吩并嘧啶亚砜，其中X是SO或SO 2，R 1是H或C 1-6 - 烷基，R 2是H或如本文所公开的有机基团，并且R 3是任选取代的单或双环不饱和的，部分饱和的或饱和的 杂环或任选取代的单环或双环杂芳基及其药理学上可接受的盐，以及含有这些化合物的药物组合物。 这些二氢噻吩并嘧啶亚砜适用于治疗呼吸道或胃肠道疾病，关节，皮肤或眼睛的炎性疾病，外周或中枢神经系统疾病或癌症。
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公开(公告)号：US20110021501A1
公开(公告)日：2011-01-27
申请号：US12738344
申请日：2008-10-16
申请人： Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
发明人： Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
IPC分类号： A61K31/519 , C07D495/04 , A61K31/527 , A61K31/55 , A61K31/5377 , C07D498/10 , A61K31/5386 , A61P29/00 , A61P25/28 , A61P25/18 , A61P25/00
CPC分类号： C07D495/04 , C07D519/00
摘要： The invention relates to new piperidino-dihydrothienopyrimidines of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 may have the meanings given in claim 1, as well as pharmaceutical compositions which contain these compounds.These new piperidino-dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.
摘要翻译： 本发明涉及式1的新的哌啶子基 - 二氢噻吩并嘧啶，以及其药学上可接受的盐，其中X是SO或SO 2，但优选为SO，其中R 1，R 2，R 3和R 4可以具有权利要求1中给出的含义， 以及含有这些化合物的药物组合物。 这些新的哌啶子基 - 二氢噻吩并嘧啶适用于治疗呼吸道或胃肠道疾病，关节，皮肤或眼睛的炎性疾病，外周或中枢神经系统或癌症的疾病。
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