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1. 发明申请

WO2008138939A1 PYRAZOLONE DERIVATIVES AS PDE4 INHIBITORS 审中-公开
标题翻译：吡唑啉酮衍生物作为PDE4抑制剂
公开(公告)号：WO2008138939A1
公开(公告)日：2008-11-20
申请号：PCT/EP2008/055867
申请日：2008-05-14
申请人： NYCOMED GMBH , SCHMIDT, Beate , SCHEUFLER, Christian , VOLZ, Jürgen , FETH, Martin P. , HUMMEL, Rolf-Peter , HATZELMANN, Armin , ZITT, Christof , WOHLSEN, Andrea , MARX, Degenhard , KLEY, Hans-Peter , OCKERT, Deborah , HEUSER, Anke , CHRISTIAANS, Johannes A. M. , STERK, Geert Jan , MENGE, Wiro M. P. B.
发明人： SCHMIDT, Beate , SCHEUFLER, Christian , VOLZ, Jürgen , FETH, Martin P. , HUMMEL, Rolf-Peter , HATZELMANN, Armin , ZITT, Christof , WOHLSEN, Andrea , MARX, Degenhard , KLEY, Hans-Peter , OCKERT, Deborah , HEUSER, Anke , CHRISTIAANS, Johannes A. M. , STERK, Geert Jan , MENGE, Wiro M. P. B.
IPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , A61K31/444 , A61K31/4155 , A61P1/00 , A61P11/00 , A61P17/00
CPC分类号： C07D401/14 , A61K31/4152
摘要： The compounds of a certain formula (1), in which R1, R7, R8, R9 and n have the meanings as given in the description, are novel effective inhibitors of the type 4 phosphodiesterase.
摘要翻译：其中R1，R7，R8，R9和n具有如说明书中给出的含义的某种式（1）的化合物是4型磷酸二酯酶的新型有效抑制剂。

2. 发明申请

WO2010055083A1 NOVEL PYRAZOLONE-DERIVATIVES AND THEIR USE AS PD4 INHIBITORS 审中-公开
标题翻译：新型吡咯烷酮衍生物及其作为PD4抑制剂的用途
公开(公告)号：WO2010055083A1
公开(公告)日：2010-05-20
申请号：PCT/EP2009/065031
申请日：2009-11-12
申请人： NYCOMED GMBH , SCHLEMMINGER, Imre , SCHMIDT, Beate , FLOCKERZI, Dieter , TENOR, Hermann , ZITT, Christof , HATZELMANN, Armin , MARX, Degenhard , BRAUN, Clemens , KÜLZER, Raimund , HEUSER, Anke , KLEY, Hans-Peter , STERK, Geert Jan
发明人： SCHLEMMINGER, Imre , SCHMIDT, Beate , FLOCKERZI, Dieter , TENOR, Hermann , ZITT, Christof , HATZELMANN, Armin , MARX, Degenhard , BRAUN, Clemens , KÜLZER, Raimund , HEUSER, Anke , KLEY, Hans-Peter , STERK, Geert Jan
IPC分类号： C07D401/04 , A61K31/454 , C07D401/14 , C07D405/14 , C07D471/04
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D471/04
摘要： The compounds of formula (1) wherein R1 represents a phenyl derivative of formulae (a), (b) or (c) R10 is 1-3C-alkyl and R11 is 1-3C-alkyl, or R10 and R11 together with the carbon atom, to which they are bonded, form a spiro-linked 3-, 4-, 5- or 6-membered hydrocarbon ring, A is C(O) or S(O) 2 , and R12 is phenyl, naphthalenyl, pyridinyl, quinolinyl, isoquinolinyl, quinoxalinyl, 1,6-naphthyridinyl, 1,8-naphthyridinyl, indolyl, phenyl substituted by R13, R14, R15 and R16, pyridinyl substituted by R17 and R18, naphthalenyl substituted by R19 and R20, quinolinyl substituted by R21 or indolyl substituted by R22, are novel effective inhibitors of the type 4 phosphodiesterase.
摘要翻译：其中R 1表示式（a），（b）或（c）R 10的苯基衍生物的式（1）化合物是1-3C-烷基，R11是1-3C-烷基，或R10和R11与碳原子与它们键合，形成螺连接的3-，4-，5-或6-元烃环，A是C（O）或S（O）2，R 12是苯基，萘基，吡啶基，喹啉基，异喹啉基，喹喔啉基，1,6-萘并吡嗪基，1,8-萘啶基，吲哚基，被R13，R14，R15和R16取代的苯基，被R17和R18取代的吡啶基，被R19和R20取代的萘基，被R21取代的喹啉基，由R22取代的吲哚基是4型磷酸二酯酶的新型有效抑制剂。

3. 发明申请

WO2005075456A1 2-(PIPERIDIN-4-YL) -4, 5-DIHYDRO-2H-PYRIDAZIN-3-ONE DERIVATIVES AS PDE4 INHIBITORS 审中-公开
标题翻译：作为PDE4抑制剂的2-（哌啶-4-基）-4,5-二氢-2H-吡啶-3-酮衍生物
公开(公告)号：WO2005075456A1
公开(公告)日：2005-08-18
申请号：PCT/EP2005/050415
申请日：2005-02-01
申请人： ALTANA PHARMA AG , MENGE, Wiro M. P. B. , STERK, Geert Jan
发明人： MENGE, Wiro M. P. B. , STERK, Geert Jan , HATZELMANN, Armin , BARSIG, Johannes , MARX, Degenhard , KLEY, Hans-Peter , CHRISTIAANS, Johannes A. M.
IPC分类号： C07D401/04
CPC分类号： C07D405/14 , C07D401/04
摘要： The compounds of a certain formula (1), in which R1, R2, R3 and R9 have the meanings as given in the description, are novel effective PDE4 inhibitors.
摘要翻译： R1，R2，R3和R9具有如说明书中给出的含义的某种式1的化合物是新的有效的PDE4抑制剂。

4. 发明申请

WO2005075437A1 PYRIDAZINONE DERIVATIVES AND THEIR USE AS PDE4 INHIBITORS 审中-公开
标题翻译：吡咯烷酮衍生物及其作为PDE4抑制剂的用途
公开(公告)号：WO2005075437A1
公开(公告)日：2005-08-18
申请号：PCT/EP2005/050412
申请日：2005-02-01
申请人： ALTANA PHARMA AG , MENGE, Wiro M. P. B. , STERK, Geert Jan
发明人： MENGE, Wiro M. P. B. , STERK, Geert Jan , HATZELMANN, Armin , BARSIG, Johannes , MARX, Degenhard , KLEY, Hans-Peter , CHRISTIAANS, Johannes A. M.
IPC分类号： C07D237/04
CPC分类号： C07D237/04 , C07D401/12 , C07D403/12
摘要： Compounds of formula (1) are effective PDE4 inhibitors in which R1 is 1-4C-alkyl and R2 is 1-4C-alkyl, R3 represents a phenyl dervative of formulae (a) or (b) wherein R4 is 1-4C-alkoxy or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R5 is 1-8C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R6 is 1-4C-alkoxy, 3-5C-cycloalkoxy, 3-5C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R7 is 1-4C-alkyl and R8 is hydrogen or 1-4C-alkyl, or wherein R7 and R8 together and with inclusion of the two carbon atoms, to which they are bonded, form a spiro-linked 5-, 6- or 7-membered hydrocarbon ring, optionally interrupted by an oxygen or sulphur atom and R9 is hydroxyl, halogen, nitro, cyano, 1-4C-alkyl, trifluoromethyl, 1-4C-alkoxy, 1-4C-alkoxy which is completely or predominantly substituted by fluorine, hydroxycarbonyl, hydroxycarbonyl-1-4C-alkyl, 1-4C-alkoxycarbonyl, 1-4C-alkylcarbonyl, 1-4C-alkylcarbonylamino, 1-4C-alkylcarbonyloxy, 1-4C-alkylsulfonyl, benzyloxy, -C(O)R10, -S(O) 2 -R11, -O(CH 2 ) n -C(O)-R12, -(CH 2 ), -C(O)-R26 or -N(R29)R30.
摘要翻译：式（1）化合物是有效的PDE4抑制剂，其中R1是1-4C-烷基，R2是1-4C-烷基，R3代表式（a）或（b）的苯基衍生物，其中R4是1-4C-烷氧基或完全或主要被氟取代的1-4C-烷氧基，R5是1-8个碳原子的烷氧基，3-7C-环烷氧基，3-7C-环烷基甲氧基或1-4C-烷氧基，其完全或主要被氟取代， R6是1-4C-烷氧基，3-5C-环烷氧基，3-5C-环烷基甲氧基或完全或主要被氟取代的1-4C-烷氧基，R7是1-4C-烷基，R8是氢或1-4C - 烷基，或其中R 7和R 8一起并且与它们所键合的两个碳原子一起形成螺键连接的5-，6-或7-元烃环，任选被氧或硫原子中断， R9是羟基，卤素，硝基，氰基，1-4C-烷基，三氟甲基，1-4C-烷氧基，完全或主要被氟取代的1-4C-烷氧基，羟基羰基，羟基羰基-1,4- C-alk 1-4C-烷氧基羰基，1-4C-烷基羰基氨基，1-4C-烷基羰基氧基，1-4C-烷基磺酰基，苄氧基，-C（O）R10，-S（O）2-R11， -O（CH 2）n C（O）-R 12， - （CH 2），-C（O）-R 26或-N（R 29）R 30。

5. 发明申请

WO2004108723A1 4,5-DIHYDRO-IMIDAZO[4,5,1-II]QUINOLIN-6-ONES AS PARP INHIBITORS 审中-公开
标题翻译： 4,5-二氢咪唑并[4,5,1-II]喹啉-6-酮作为PARP抑制剂
公开(公告)号：WO2004108723A1
公开(公告)日：2004-12-16
申请号：PCT/EP2004/051019
申请日：2004-06-03
申请人： ALTANA PHARMA AG , CHRISTIAANS, Johannes A. M.
发明人： CHRISTIAANS, Johannes A. M. , WEINBRENNER, Steffen , KLEIN, Thomas , FLOCKERZI, Dieter , STERK, Geert Jan , MENGE, Wiro M. P. B. , BRUNDEL, Paulus Johannes Gaurerius
IPC分类号： C07D471/06
CPC分类号： C07D471/06
摘要： Compounds of the formula 1, in which R1 and R2 have the meanings indicated in the description, are novel active PARP inhibitors.
摘要翻译：其中R1和R2具有说明书中所示含义的式1化合物是新的活性PARP抑制剂。

6. 发明申请

WO2005075457A1 PHTHALAZINONE-DERIVATIVES AS PDE4 INHIBITORS 审中-公开
标题翻译：苯乙烯酮衍生物作为PDE4抑制剂
公开(公告)号：WO2005075457A1
公开(公告)日：2005-08-18
申请号：PCT/EP2005/050417
申请日：2005-02-01
申请人： ALTANA PHARMA AG , STERK, Geert Jan
发明人： STERK, Geert Jan , HATZELMANN, Armin , BARSIG, Johannes , MARX, Degenhard , KLEY, Hans-Peter , CHRISTIAANS, Johannes A. M. , MENGE, Wiro M. P. B.
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/14
摘要： The compounds of a certain formula (1), in which R1, R2, R3, R9 and n have the meanings as given in the description, are novel effective PDE4 inhibitors.
摘要翻译：其中R1，R2，R3，R9和n具有如说明书中给出的含义的某种式（1）的化合物是新的有效的PDE4抑制剂。

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