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1.发明授权Quinuclidine derivatives processes for preparing them and their uses as m2 and/or m3 muscarinic receptor inhibitors 失效奎宁环衍生物的制备方法及其作为m2和/或m3毒蕈碱受体抑制剂的用途公开(公告)号：US07361668B2
公开(公告)日：2008-04-22
申请号：US10490436
申请日：2002-09-23
申请人： Michel Guyaux , Chimmanamada U. Dinesh , Charles Mioskowski , Luc Quere , Jean-Philippe Starck , Patrice Talaga , Alain Wagner , Matteo Zanda
发明人： Michel Guyaux , Chimmanamada U. Dinesh , Charles Mioskowski , Luc Quere , Jean-Philippe Starck , Patrice Talaga , Alain Wagner , Matteo Zanda
IPC分类号： A61K31/45 , A61K43/96 , A61K43/40 , C07D453/02
CPC分类号： C07D453/02
摘要： The invention concerns quinuclidine derivatives of formula I or II wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention show high affinities for m3 and/or m2 muscarinic receptors and are particularly suited for treating urinary incontinence.
摘要翻译： 本发明涉及式I或II的奎宁环衍生物，其中取代基如说明书中所定义，以及它们作为药物的用途。 本发明化合物对于m 3和/或m 2毒蕈碱受体显示出高亲和力，特别适用于治疗尿失禁。
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2.发明申请Quinuclidine derivatives processes for preparing them and their uses as m2 and/or m3 muscarinic receptor inhibitors 失效奎宁环衍生物的制备方法及其作为m2和/或m3毒蕈碱受体抑制剂的用途公开(公告)号：US20050020660A1
公开(公告)日：2005-01-27
申请号：US10490436
申请日：2002-09-23
申请人： Michel Guyaux , Chimmanamada Dinesh , Charles Mioskowski , Luc Quere , Jean-Philippe Starck , Patrice Talaga , Alain Wagner , Mateo Zanda
发明人： Michel Guyaux , Chimmanamada Dinesh , Charles Mioskowski , Luc Quere , Jean-Philippe Starck , Patrice Talaga , Alain Wagner , Mateo Zanda
IPC分类号： A61K31/439 , A61K31/444 , A61P1/00 , A61P9/00 , A61P11/00 , A61P13/02 , A61P25/20 , A61P25/28 , C07D453/02 , C07F7/10 , C07D487/02 , A61K31/407
CPC分类号： C07D453/02
摘要： The invention concerns quinuclidine derivatives of formula I or II wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention_show high affinities for m3 and/or m2 muscarinic receptors and are particularly suited for treating urinary incontinence.
摘要翻译： 本发明涉及式I或II的奎宁环衍生物，其中取代基如说明书中所定义，以及它们作为药物的用途。 本发明的化合物对于m 3和/或m 2毒蕈碱受体具有高亲和力，并且特别适用于治疗尿失禁。
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3.发明授权2-oxo-1-pyrrolidine derivatives, processes for preparing them and their uses 有权2-氧代-1-吡咯烷衍生物，其制备方法及其用途公开(公告)号：US08034958B2
公开(公告)日：2011-10-11
申请号：US12656808
申请日：2010-02-17
申请人： Edmond Differding , Benoît Kenda , Bénédicte Lallemand , Alain Matagne , Philippe Michel , Patrick Pasau , Patrice Talaga
发明人： Edmond Differding , Benoît Kenda , Bénédicte Lallemand , Alain Matagne , Philippe Michel , Patrick Pasau , Patrice Talaga
IPC分类号： C07D207/00
CPC分类号： C07D207/26 , A61K31/4015 , C07C237/12 , C07D207/27 , C07D207/273 , C07D207/277 , C07D307/33 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07D495/04
摘要： The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.
摘要翻译： 本发明涉及式I的2-氧代-1-吡咯烷衍生物，其中取代基如说明书中所定义，以及它们作为药物的用途。 本发明的化合物特别适用于治疗诸如癫痫的神经障碍。
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公开(公告)号：US20060074068A1
公开(公告)日：2006-04-06
申请号：US10511660
申请日：2003-03-29
IPC分类号： A61K31/506 , A61K31/505 , C07D403/02
CPC分类号： C07D239/42 , C07D239/48 , C07D239/50 , C07D239/60 , C07D401/04 , C07D403/04 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04
摘要： The present invention concerns chemical compounds combining affinity and antagonism against the human m3 muscarinic receptor with activity as selective phosphodiesterase IV (PDE IV) inhibitors, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
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5.发明申请2-Oxo-1-pyrrolidine derivatives, processes for preparing them and their uses 审中-公开2-氧代-1-吡咯烷衍生物，其制备方法及其用途公开(公告)号：US20050171187A1
公开(公告)日：2005-08-04
申请号：US11043145
申请日：2005-01-27
申请人： Edmond Differding , Benoit Kenda , Benedicte Lallemand , Alain Matagne , Philippe Michel , Patrick Pasau , Patrice Talaga
发明人： Edmond Differding , Benoit Kenda , Benedicte Lallemand , Alain Matagne , Philippe Michel , Patrick Pasau , Patrice Talaga
IPC分类号： C07D401/04 , A61K31/4015 , A61K31/4025 , A61K31/41 , A61K31/4178 , A61K31/4188 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/541 , A61P9/00 , A61P9/06 , A61P9/10 , A61P11/00 , A61P11/06 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/16 , A61P37/08 , C07B61/00 , C07C237/06 , C07C237/12 , C07D207/26 , C07D207/27 , C07D207/273 , C07D207/277 , C07D307/33 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D495/04 , C07D207/12
CPC分类号： C07D207/26 , A61K31/4015 , C07C237/12 , C07D207/27 , C07D207/273 , C07D207/277 , C07D307/33 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07D495/04
摘要： The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.
摘要翻译： 本发明涉及式I的2-氧代-1-吡咯烷衍生物，其中取代基如说明书中所定义，以及它们作为药物的用途。 本发明的化合物特别适用于治疗诸如癫痫的神经障碍。
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6.发明申请2-Oxo-1-pyrrolidine derivatives, processes for preparing them and their uses 有权2-氧代-1-吡咯烷衍生物，其制备方法及其用途公开(公告)号：US20100222576A1
公开(公告)日：2010-09-02
申请号：US12656808
申请日：2010-02-17
申请人： Edmond Differding , Benoît Kenda , Bénédicte Lallemand , Alain Matagne , Philippe Michel , Patrick Pasau , Patrice Talaga
发明人： Edmond Differding , Benoît Kenda , Bénédicte Lallemand , Alain Matagne , Philippe Michel , Patrick Pasau , Patrice Talaga
IPC分类号： C07D417/06 , C07D207/267 , C07D403/06 , C07D403/04
CPC分类号： C07D207/26 , A61K31/4015 , C07C237/12 , C07D207/27 , C07D207/273 , C07D207/277 , C07D307/33 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07D495/04
摘要： The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals.The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.
摘要翻译： 本发明涉及式I的2-氧代-1-吡咯烷衍生物，其中取代基如说明书中所定义，以及它们作为药物的用途。 本发明的化合物特别适用于治疗诸如癫痫的神经障碍。
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7.发明授权2-oxo-1-pyrrolidine derivatives, processes for preparing them and their uses 有权2-氧代-1-吡咯烷衍生物，其制备方法及其用途公开(公告)号：US07692028B2
公开(公告)日：2010-04-06
申请号：US12000512
申请日：2007-12-13
申请人： Edmond Differding , Benoît Kenda , Bénédicte Lallemand , Alain Matagne , Philippe Michel , Patrick Pasau , Patrice Talaga
发明人： Edmond Differding , Benoît Kenda , Bénédicte Lallemand , Alain Matagne , Philippe Michel , Patrick Pasau , Patrice Talaga
IPC分类号： C07D207/00
CPC分类号： C07D207/26 , A61K31/4015 , C07C237/12 , C07D207/27 , C07D207/273 , C07D207/277 , C07D307/33 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07D495/04
摘要： The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.
摘要翻译： 本发明涉及式I的2-氧代-1-吡咯烷衍生物，其中取代基如说明书中所定义，以及它们作为药物的用途。 本发明的化合物特别适用于治疗诸如癫痫的神经障碍。
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8.发明授权Compounds comprising an oxazoline or thiazoline moiety, processes for making them, and their uses 失效包含恶唑啉或噻唑啉部分的化合物，其制备方法及其用途公开(公告)号：US07863450B2
公开(公告)日：2011-01-04
申请号：US11910153
申请日：2006-03-29
申请人： Sylvain Celanire , Patrice Talaga , Regorius Leurs , Frederic Denonne , Henkdrik Timmerman , Florence Lebon
发明人： Sylvain Celanire , Patrice Talaga , Regorius Leurs , Frederic Denonne , Henkdrik Timmerman , Florence Lebon
IPC分类号： C07D211/68 , C07D401/00 , A61K31/445
CPC分类号： C07D263/14 , C07D207/06 , C07D211/14 , C07D263/16 , C07D263/32 , C07D263/36 , C07D263/52 , C07D277/10 , C07D277/24 , C07D277/28 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to compounds comprising an oxazoline or thiazoline moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H3-receptor ligands, (I), wherein A1 is CH C(CH3) or N; R1 is hydrogen or halogen; R2 is (II); A2 is O or S; R3 is hydrogen, halogen, C1-4 alkyl or C1-4 alkoxy; R4 is hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or —O—(CH2)n-NR12aR each CH2 in —O—(CH2)n-NR12aR12b being optionally substituted by one or two C1-4 alkyl; R5 is hydrogen or —O—(CH2)m—NR13aR13b, each CH2 in —O—(CH2)m—NR13aR13b being optionally substituted by one or two C1-4 alkyl, and at least one of R4 and R5 should be a —O—(CH2)n-NR12/13aR12/13b group.
摘要翻译： 本发明涉及包含恶唑啉或噻唑啉部分的化合物，其制备方法，包含所述化合物的药物组合物及其作为H3-受体配体的用途，（I）其中A1为CHC（CH3）或N; R1是氢或卤素; R2是（II）; A2为O或S; R3是氢，卤素，C1-4烷基或C1-4烷氧基; R4是氢，卤素，C1-4烷基，C1-4烷氧基，三氟甲基或-O-（CH2）n-NR12aR，-O-（CH2）n-NR12aR12b中的每个CH2任选被一个或两个C 1-4烷基 ; R 5是氢或-O-（CH 2）m -NR 13 a R 13b，-O-（CH 2）m -NR 13 a R 13 b中的每个CH 2任选被一个或两个C 1-4烷基取代，并且R 4和R 5中的至少一个应为 - O-（CH 2）n -NR 12 / 13aR 12 / 13b基团。
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9.发明授权2-Oxo-1-pyrrolidine derivatives, processes for preparing them and their uses 有权2-氧代-1-吡咯烷衍生物，其制备方法及其用途公开(公告)号：US07358276B2
公开(公告)日：2008-04-15
申请号：US11043176
申请日：2005-01-27
申请人： Edmond Differding , Benoît Kenda , Bénédicte Lallemand , Alain Matagne , Philippe Michel , Patrick Pasau , Patrice Talaga
发明人： Edmond Differding , Benoît Kenda , Bénédicte Lallemand , Alain Matagne , Philippe Michel , Patrick Pasau , Patrice Talaga
IPC分类号： C07C205/00 , A61K31/21
CPC分类号： C07D207/26 , A61K31/4015 , C07C237/12 , C07D207/27 , C07D207/273 , C07D207/277 , C07D307/33 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07D495/04
摘要： The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.
摘要翻译： 本发明涉及式I的2-氧代-1-吡咯烷衍生物，其中取代基如说明书中所定义，以及它们作为药物的用途。 本发明的化合物特别适用于治疗诸如癫痫的神经障碍。
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10.发明授权2-oxo-1-pyrrolidine derivatives, processes for preparing them and their uses 有权2-氧代-1-吡咯烷衍生物，其制备方法及其用途公开(公告)号：US06911461B2
公开(公告)日：2005-06-28
申请号：US10693917
申请日：2003-10-28
申请人： Edmond Differding , Benoît Kenda , Bénédicte Lallemand , Alain Matagne , Philippe Michel , Patrick Pasau , Patrice Talaga
发明人： Edmond Differding , Benoît Kenda , Bénédicte Lallemand , Alain Matagne , Philippe Michel , Patrick Pasau , Patrice Talaga
IPC分类号： C07D401/04 , A61K31/4015 , A61K31/4025 , A61K31/41 , A61K31/4178 , A61K31/4188 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/541 , A61P9/00 , A61P9/06 , A61P9/10 , A61P11/00 , A61P11/06 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/16 , A61P37/08 , C07B61/00 , C07C237/06 , C07C237/12 , C07D207/26 , C07D207/27 , C07D207/273 , C07D207/277 , C07D307/33 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D495/04 , A61K31/426 , C07D277/20
CPC分类号： C07D207/26 , A61K31/4015 , C07C237/12 , C07D207/27 , C07D207/273 , C07D207/277 , C07D307/33 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07D495/04
摘要： The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.
摘要翻译： 本发明涉及式I的2-氧代-1-吡咯烷衍生物，其中取代基如说明书中所定义，以及它们作为药物的用途。 本发明的化合物特别适用于治疗诸如癫痫的神经障碍。
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