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1. 发明申请

WO2006092417A1 6 -HETEROARYL-1, 2, 3,4,4A, 1OB-HEXAHYDRO-PHENANTHRIDINES AS PDE-4 INHIBITORS FOR THE TREATMENT OF INFLAMMATORY DISORDERS 审中-公开
标题翻译： 6 -HETEROARYL-1,2,4,4,4A，1-B-HEXAHYDRO-PHENANTHRIDINES作为治疗炎症性疾病的PDE-4抑制剂
公开(公告)号：WO2006092417A1
公开(公告)日：2006-09-08
申请号：PCT/EP2006/060370
申请日：2006-03-01
申请人： ALTANA PHARMA AG , KAUTZ, Ulrich , SCHMIDT, Beate , FLOCKERZI, Dieter , CHIESA, Maria Vittoria , HATZELMANN, Armin , ZITT, Christof , WOHLSEN, Andrea , MARX, Degenhard , KLEY, Hans-peter
发明人： KAUTZ, Ulrich , SCHMIDT, Beate , FLOCKERZI, Dieter , CHIESA, Maria Vittoria , HATZELMANN, Armin , ZITT, Christof , WOHLSEN, Andrea , MARX, Degenhard , KLEY, Hans-peter
IPC分类号： C07D401/04 , C07D401/14 , A61K31/473 , A61P29/00 , A61P11/00
CPC分类号： C07D401/04
摘要： Compounds of a certain formula (I), in which R1 , R2, R3, R31, R4, R5, R51 and Har have the meanings indicated in the description, are novel effective PDE4 inhibitors.
摘要翻译：其中R1，R2，R3，R31，R4，R5，R51和Har具有说明书中所示含义的某种式（I）的化合物是新的有效的PDE4抑制剂。

2. 发明申请

WO2005085225A1 NOVEL HYDROXY-6-HETEROARYLPHENANTHRIDINES AND THEIR USE AS PDE4 INHIBITORS 审中-公开
标题翻译：新型羟基-6-羟基噻嗪类及其作为PDE4抑制剂的用途
公开(公告)号：WO2005085225A1
公开(公告)日：2005-09-15
申请号：PCT/EP2005/050931
申请日：2005-03-02
申请人： ALTANA PHARMA AG , KAUTZ, Ulrich
发明人： KAUTZ, Ulrich , SCHMIDT, Beate , FLOCKERZI, Dieter , HATZELMANN, Armin , ZITT, Christof , BARSIG, Johannes , MARX, Degenhard , KLEY, Hans-Peter
IPC分类号： C07D401/04
CPC分类号： A61K31/473 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D401/04 , C07D401/14 , C07D405/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds of formula (I), in which R1 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, 2,2-difluoroethoxy, or completely or predominantly fluorine-substituted 1-4C-alkoxy, R2 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, 2,2-difluoroethoxy, or completely or predominantly fluorine-substituted 1-4C-alkoxy, or in which R1 and R2 together are a 1-2C-alkylenedioxy group, R3 is hydrogen or 1-4C-alkyl, R31 is hydrogen or 1-4C-alkyl, either, in a first embodiment (embodiment a) according to the present invention, R4 is -O-R41, in which R41 is hydrogen, 1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl, hydroxy-2-4C-alkyl, 1-7C-alkylcarbonyl, or completely or predominantly fluorine-substituted 1-4C-alkyl, and R5 is hydrogen or 1-4C-alkyl, or, in a second embodiment (embodiment b) according to the present invention, R4 is hydrogen or 1-4C-alkyl, and R5 is -O-R51, in which R51 is hydrogen, 1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl, hydroxy-2-4C-alkyl, 1-7C-alkylcarbonyl, or completely or predominantly fluorine-substituted 1-4C-alkyl, Har is optionally substituted by R6 and/or R7 and/or R8, and is a 5- to 10-membered monocylic or fused bicyclic unsaturated or partially saturated heteroaryl radical comprising 1 to 4 heteroatoms selected independently from the group consisting of oxygen, nitrogen and sulfur, are novel effective PDE4 inhibitors.
摘要翻译：式（I）化合物，其中R 1是羟基，1-4C-烷氧基，3-7C-环烷氧基，3-7C-环烷基甲氧基，2,2-二氟乙氧基或完全或主要是氟取代的1-4C-烷氧基， R2是羟基，1-4C-烷氧基，3-7C-环烷氧基，3-7C-环烷基甲氧基，2,2-二氟乙氧基或完全或主要是氟取代的1-4C-烷氧基，或其中R1和R2一起是 1-2C-亚烷基二氧基，R3是氢或1-4C-烷基，R31是氢或1-4C-烷基，在根据本发明的第一个实施方案（实施方案a）中，R 4是-O-R 41，其中R41是氢，1-4C-烷基，1-4C-烷氧基-1-4C-烷基，羟基-24C-烷基，1-7C-烷基羰基，或完全或主要是氟取代的1-4C-烷基或者R5为氢或1-4C-烷基，或在本发明的第二实施方案（实施方案b）中，R 4为氢或1-4C-烷基，R 5为-O-R 51，其中R 51为氢，1-4C-烷基，1-4C-烷氧基-1-4C-烷基，羟基-24C-烷基，1-7C-烷基羰基或com 完全或主要是氟取代的1-4C-烷基，Har任选被R 6和/或R 7和/或R 8取代，并且是5至10元单环或稠合双环不饱和或部分饱和的杂芳基，其包含1至4个独立选自氧，氮和硫的杂原子是新的有效的PDE4抑制剂。

3. 发明申请

WO2005087745A1 NOVEL AMIDO-SUBSTITUTED HYDROXY-6-PHENYLPHENANTHRIDINES AND THEIR USE AS PDE4 INHIBITORS 审中-公开
标题翻译：新型氨基取代的羟基-6-苯基噻吩并作为PDE4抑制剂使用
公开(公告)号：WO2005087745A1
公开(公告)日：2005-09-22
申请号：PCT/EP2005/051054
申请日：2005-03-09
申请人： ALTANA PHARMA AG , KAUTZ, Ulrich
发明人： KAUTZ, Ulrich , SCHMIDT, Beate , FLOCKERZI, Dieter , HATZELMANN, Armin , ZITT, Christof , BARSIG, Johannes , MARX, Degenhard , KLEY, Hans-Peter
IPC分类号： C07D221/12
CPC分类号： C07D221/12 , C07D401/12 , C07D471/04
摘要： Compounds of formula (I) in which R1 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, 2,2-difluoroethoxy, or com pletely or predominantly fluorine-substituted 1-4C-alkoxy, R2 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3 . 7C-cycloalkylmethoxy, 2,2-difluoroethoxy, or com pletely or predominantly fluorine-substituted 1-4C-alkoxy, or in which R1 and R2 together are a 1-2C-alkylenedioxy group, R3 is hydrogen or 1-4C-alkyl, R31 is hydrogen or 1-4C-alkyl, either, in a first embodiment (embodiment a) according to the present invention, R4 is -0-R41, in which R41 is hydrogen, 1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl, hydroxy-2-4C-alkyl, 1-7C-alkylcarbonyl, or com pletely or predominantly fluorine-substituted 1-4C-alkyl. and R5 is hydrogen or 1-4C-alkyl, or, in a second embodiment (embodiment b) according to the present invention, R4 is hydrogen or 1-4C-alkyl, and R5 is -0-R51, in which R51 is hydrogen, 1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl, hydroxy-2-4C-alkyl, 1-7C-alkylcarbonyt, or com pletely or predominantly fluorine-substituted 1-4C-alkyl, R6 is hydrogen, halogen, 1-4C-alkyl or 1-4C-alkoxy, either, in a first aspect (aspect 1) according to the present invention, R7 is -N(R8)R9, or, in a second aspect (aspect 2) according to the present invention, R7 is -NH-N(R18)R19, are novel effective PDE4 inhibitors.
摘要翻译：其中R1是羟基，1-4C-烷氧基，3-7C-环烷氧基，3-7C-环烷基甲氧基，2,2-二氟乙氧基或完全或主要是氟取代的1-4C-烷氧基的式（Ⅰ）化合物， R2是羟基，1-4C-烷氧基，3-7C-环烷氧基，3,7-环烷基甲氧基，2,2-二氟乙氧基或完全或主要是氟取代的1-4C-烷氧基，或其中R1和R2 在根据本发明的第一实施方案（实施方案a）中，R 1是亚烷基二氧基，R 3是氢或1-4C-烷基，R 31是氢或1-4C-烷基，R 4是-O -R41，其中R41是氢，1-4C-烷基，1-4C-烷氧基-1- 1-4C-烷基，羟基-24C-烷基，1-7C-烷基羰基，或完全或主要是氟取代的1 1-4C-烷基。或者R5是氢或1-4C-烷基，或者在根据本发明的第二个实施方案（实施方案b）中，R4是氢或1-4C-烷基，R5是-O-R51，其中R51是氢 1-4C-烷基，1-4C-烷氧基-14C-烷基，羟基-24C-烷基，1-7C-烷基羰基，或完全或主要是氟取代的1-4C-烷基，R6是氢，卤素，1-4C-烷基或1-4C-烷氧基，在根据本发明的第一方面（方面1）中，R7是-N（R8）R9，或在第二方面（方面2）中，根据本发明，R7是-NH-N（R18）R19，是新型有效的PDE4抑制剂。

4. 发明申请

WO2005085203A1 NOVEL DIFLUOROETHOXY-SUBSTITUTED HYDROXY-6-PHENYLPHENANTHRIDINES AND THEIR USE AS PDE4 INHIBITORS 审中-公开
标题翻译：新型二氟醚取代的羟基-6-苯基噻吩并作为PDE4抑制剂使用
公开(公告)号：WO2005085203A1
公开(公告)日：2005-09-15
申请号：PCT/EP2005/051022
申请日：2005-03-08
申请人： ALTANA PHARMA AG , KAUTZ, Ulrich
发明人： KAUTZ, Ulrich , SCHMIDT, Beate , FLOCKERZI, Dieter , HATZELMANN, Armin , ZITT, Christof , BARSIG, Johannes , MARX, Degenhard , KLEY, Hans-Peter
IPC分类号： C07D221/12
CPC分类号： C07D221/12
摘要： Compounds of a certain formula (I), in which R1, R2, R3, R31, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective PDE4 inhibitors.
摘要翻译：其中R 1，R 2，R 3，R 31，R 4，R 5，R 6和R 7具有说明书中所示含义的某种式（I）的化合物是新的有效的PDE4抑制剂。

5. 发明申请

WO2006082185A1 NOVEL 6-PYRIDYLPHENANTHRIDINES 审中-公开
标题翻译：新型6-吡啶基亚胺
公开(公告)号：WO2006082185A1
公开(公告)日：2006-08-10
申请号：PCT/EP2006/050557
申请日：2006-01-31
申请人： ALTANA Pharma AG , KAUTZ, Ulrich , SCHMIDT, Beate , FLOCKERZI, Dieter , CHIESA, Maria Vittoria , HATZELMANN, Armin , ZITT, Christof , BARSIG, Johannes , WOHLSEN, Andrea , MARX, Degenhard , KLEY, Hans-peter
发明人： KAUTZ, Ulrich , SCHMIDT, Beate , FLOCKERZI, Dieter , CHIESA, Maria Vittoria , HATZELMANN, Armin , ZITT, Christof , BARSIG, Johannes , WOHLSEN, Andrea , MARX, Degenhard , KLEY, Hans-peter
IPC分类号： C07D401/04 , A61K31/473 , A61P11/06
CPC分类号： C07D401/04
摘要： Compounds of a certain formula I, in which R1, R2, R3, R31, R4, R5, R51 and Har have the meanings indicated in the description, are novel effective PDE4 inhibitors.
摘要翻译：其中R1，R2，R3，R31，R4，R5，R51和Har具有说明书中所示含义的某种式I的化合物是新的有效的PDE4抑制剂。

6. 发明申请

WO2005077906A1 NOVEL GUANIDINYL-SUBSTITUTED HYDROXY-6-PHENYLPHENENTHRIDINES AS EFFECTIVE PHOSPHODIESTERASE (PDE) 4 INHIBITORS 审中-公开
标题翻译：新型胍基取代的羟基-6-苯基噻吩作为有效的磷酸酯酶（PDE）4抑制剂
公开(公告)号：WO2005077906A1
公开(公告)日：2005-08-25
申请号：PCT/EP2005/050708
申请日：2005-02-17
申请人： ALTANA PHARMA AG , KAUTZ, Ulrich
发明人： KAUTZ, Ulrich , SCHMIDT, Beate , FLOCKERZI, Dieter , HATZELMANN, Armin , ZITT, Christof , BARSIG, Johannes , MARX, Degenhard , KLEY, Hans-Peter
IPC分类号： C07D221/12
CPC分类号： C07D221/12
摘要： Compounds of a certain formula (1), in which R1, R2, R3, R31, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective PDE4 inhibitors in which R7 is a radical of formulae (a), (b), (c) or (d).
摘要翻译：其中R 1，R 2，R 3，R 31，R 4，R 5，R 6和R 7具有说明书中所示含义的某种式（1）的化合物是新的有效的PDE4抑制剂，其中R 7是式（a），（b），（c）或（d）。

7. 发明申请

WO2006095009A1 AMIDO-SUBSTITUTED 6-PHENYLPHENANTHRIDINES 审中-公开
标题翻译：氨基取代的6-苯基苯胺
公开(公告)号：WO2006095009A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/060595
申请日：2006-03-09
申请人： ALTANA PHARMA AG , KAUTZ, Ulrich , SCHMIDT, Beate , FLOCKERZI, Dieter , CHIESA, Maria Vittoria , HATZELMANN, Armin , ZITT, Christof , BARSIG, Johannes , MARX, Degenhard , KLEY, Hans-Peter
发明人： KAUTZ, Ulrich , SCHMIDT, Beate , FLOCKERZI, Dieter , CHIESA, Maria Vittoria , HATZELMANN, Armin , ZITT, Christof , BARSIG, Johannes , MARX, Degenhard , KLEY, Hans-Peter
IPC分类号： C07D401/10 , C07D221/12 , A61K31/473 , A61P11/00
CPC分类号： C07D401/10 , C07D221/12
摘要： Compounds of a certain formula (I), in which R1, R2, R3, R31, R4, R5, R51, R6 and R7 have the meanings indicated in the description, are novel effective PDE4 inhibitors.
摘要翻译：其中R 1，R 2，R 3，R 31，R 4，R 5，R 51，R 6和R 7具有说明书中所示含义的某种式（I）的化合物是新的有效的PDE4抑制剂。

8. 发明申请

WO2006027345A3 NOVEL 3-THIA-10-AZA-PHENANTHRENE DERIVATIVES 审中-公开
公开(公告)号：WO2006027345A3
公开(公告)日：2006-03-16
申请号：PCT/EP2005/054365
申请日：2005-09-05
申请人： ALTANA PHARMA AG , FLOCKERZI, Dieter , KAUTZ, Ulrich , HATZELMANN, Armin , ZITT, Christof , WOHLSEN, Andrea , MARX, Degenhard , KLEY, Hans-Peter , CHRISTOFFERS, Jens , ROSIAK, Anna
发明人： FLOCKERZI, Dieter , KAUTZ, Ulrich , HATZELMANN, Armin , ZITT, Christof , WOHLSEN, Andrea , MARX, Degenhard , KLEY, Hans-Peter , CHRISTOFFERS, Jens , ROSIAK, Anna
IPC分类号： C07D495/06 , A61P11/00 , A61K31/4745
摘要： Compounds of a certain formula 1, in which A, R1, R2 and R3 have the meanings indicated in the de- scription, are novel effective PDE4 inhibitors.

9. 发明申请

WO2006027344A2 NOVEL 3-OXA-10-AZA-PHENANTHRENES 审中-公开
标题翻译：新型3-OXA-10-AZA-PHENANTHRENES
公开(公告)号：WO2006027344A2
公开(公告)日：2006-03-16
申请号：PCT/EP2005/054364
申请日：2005-09-05
申请人： ALTANA PHARMA AG , FLOCKERZI, Dieter , KAUTZ, Ulrich , HATZELMANN, Armin , ZITT, Christof , WOHLSEN, Andrea , MARX, Degenhard , KLEY, Hans-Peter , CHRISTOFFERS, Jens , ROSIAK, Anna
发明人： FLOCKERZI, Dieter , KAUTZ, Ulrich , HATZELMANN, Armin , ZITT, Christof , WOHLSEN, Andrea , MARX, Degenhard , KLEY, Hans-Peter , CHRISTOFFERS, Jens , ROSIAK, Anna
CPC分类号： C07D491/04
摘要： Compounds of a certain formula 1, in which R1, R2 and R3 have the meanings indicated in the description, are novel effective PDE4 inhibitors.
摘要翻译： R1，R2和R3具有说明书中所示含义的某种式1的化合物是新的有效的PDE4抑制剂。

10. 发明申请

WO2005090311A1 NOVEL HETEROCYCLYL-SUBSTITUTED HYDROXY-6-PHENYLPHENANTHRIDINES AND THEIR USE AS PDE4 INHIBITORS 审中-公开
标题翻译：新型环己基取代的羟基-6-苯基噻吩并作为PDE4抑制剂使用
公开(公告)号：WO2005090311A1
公开(公告)日：2005-09-29
申请号：PCT/EP2005/050946
申请日：2005-03-03
申请人： ALTANA PHARMA AG , KAUTZ, Ulrich
发明人： KAUTZ, Ulrich , SCHMIDT, Beate , FLOCKERZI, Dieter , HATZELMANN, Armin , ZITT, Christof , BARSIG, Johannes , MARX, Degenhard , KLEY, Hans-Peter
IPC分类号： C07D221/12
CPC分类号： C07D221/12 , C07D401/10 , C07D413/10 , C07D417/10
摘要： Compounds of formula (I) in which R1 is hydroxyl, 1-4C-alkoxy, 3-7C-cydoalkoxy, 3-7C-cydoalkylmethoxy, 2,2-difluoroethoxy, or completely or predominantly fluorine-substituted 1-4C-alkoxy, R2 is hydroxyl, 1-4C-aikoxy, 3-7C-cydoalkoxy, 3-7C-cydoalkylmethoxy, 2,2-difluoroethoxy, or completely or predominantly fluorine-substituted 1-4C-alkoxy, or in which R1 and R2 together are a 1-2C-alkylenedioxy group, R3 is hydrogen or 1-4C-alkyl, R31 is hydrogen or 1-4C-alkyl, either, in a first embodiment (embodiment a) according to the present invention, R4 is -O-R41, in which R41 is hydrogen, 1-4C-aikyl,1-4C-alkoxy-1-4C-alkyl, hydroxy-2-C-alkyl, 1-7C-alkylcarbonyl, or completely or predominantly fluorine-substituted 1-4C-alkyl, and R5 is hydrogen or 1-4C-alkyl, or, in a second embodiment (embodiment b) according to the present invention, R4 Is hydrogen or 1-4C-alkyl, and R5 is -O-R51, in which R51 Is hydrogen, 1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl, hydroxy-2-4C-alkyl. 1-7C-alkylcarbonyl, or completely or predominantly fluorine-substituted 1-4C-alkyl, R6 is hydrogen, halogen, 1-4C-alkyl or 1.4C-alkoxy, R7 is Het1, Het2, Hart, Het3 or Har2, In which.
摘要翻译：其中R1是羟基，1-4C-烷氧基，3-7C-环烷氧基，3-7C-环烷基甲氧基，2,2-二氟乙氧基或完全或主要是氟取代的1-4C-烷氧基的式（I）化合物，R2 是羟基，1-4C-烷氧基，3-7C-环烷氧基，3-7C-环烷基甲氧基，2,2-二氟乙氧基或完全或主要是氟取代的1-4C-烷氧基，或其中R1和R2一起为1 -2C-亚烷基二氧基，R3是氢或1-4C-烷基，R31是氢或1-4C-烷基，在根据本发明的第一个实施方案（实施方案a）中，R 4是-O-R 41，在其中R41是氢，1-4C-烷基，1-4C-烷氧基-1-4C-烷基，羟基-2- C-烷基，1-7C-烷基羰基，或完全或主要是氟取代的1-4C-烷基，或者R5是氢或1-4C-烷基，或者在根据本发明的第二个实施方案（实施方案b）中，R4是氢或1-4C-烷基，R5是-O-R51，其中R51是氢 1-4C-烷基，1-4C-烷氧基-14C-烷基，羟基-24C-烷基。 1-7C-烷基羰基，或完全或主要是氟取代的1-4C-烷基，R6是氢，卤素，1-4C-烷基或1-4C-烷氧基，R7是Het1，Het2，Hart，Het3或Har2，其中。

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