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公开(公告)号：US20080255117A1
公开(公告)日：2008-10-16
申请号：US12040369
申请日：2008-02-29
申请人： Lars WORTMANN , Bernd Menzenbach , Marcus Koppitz , Dirk Kosemund , Hans Peter Muhn , Anna Schrey , Ronald Kuehne , Thomas Frenzel , Florian Peter Liesener
发明人： Lars WORTMANN , Bernd Menzenbach , Marcus Koppitz , Dirk Kosemund , Hans Peter Muhn , Anna Schrey , Ronald Kuehne , Thomas Frenzel , Florian Peter Liesener
IPC分类号： A61K31/4035 , C07D209/14 , A61K31/5377 , C07D413/02 , C07D403/12 , A61K31/454 , A61K31/4155 , C07D405/12 , A61K31/4709 , C07D215/36
CPC分类号： A61K31/4035 , A61K31/4155 , A61K31/454 , A61K31/4709 , A61K31/5377 , C07D209/14 , C07D215/36 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12
摘要： The present invention relates to sulfonyltryptophanols of the general formula I, in which Q, X, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description.The compounds according to the invention are effective FSH receptor antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译： 本发明涉及通式I的磺酰基色氨酸，其中Q，X，W，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8具有说明书中定义的含义。 根据本发明的化合物是有效的FSH受体拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。
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公开(公告)号：US20080207728A1
公开(公告)日：2008-08-28
申请号：US11956824
申请日：2007-12-14
申请人： Lars Wortmann , Bernd Menzenbach , Marcus Koppitz , Dirk Kosemund , Hans-Peter Muhn , Anna Schrey , Ronald Kuehne , Thomas Frenzel , Florian Peter Liesener
发明人： Lars Wortmann , Bernd Menzenbach , Marcus Koppitz , Dirk Kosemund , Hans-Peter Muhn , Anna Schrey , Ronald Kuehne , Thomas Frenzel , Florian Peter Liesener
IPC分类号： A61K31/404 , C07D405/12 , C07D311/02 , C07D307/77 , C07D209/14 , A61P15/18 , A61P15/16
CPC分类号： C07D417/14 , C07D405/12 , C07D405/14 , C07D409/14
摘要： The present invention relates to acyltryptophanols of the general formula I, in which Q, V, X, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description.The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译： 本发明涉及通式I的酰基色氨酸，其中Q，V，X，W，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8具有如说明书中所定义的含义。 根据本发明的化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。
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公开(公告)号：US20090082372A1
公开(公告)日：2009-03-26
申请号：US12179037
申请日：2008-07-24
申请人： Lars WORTMANN , Marcus Koppitz , Bernd Menzenbach , Dirk Kosemund , Norbert Schmees , Hans-Peter Muhn , Thomas Frenzel , Florian Peter Liesener , Anna Schrey , Ronald Kuehne
发明人： Lars WORTMANN , Marcus Koppitz , Bernd Menzenbach , Dirk Kosemund , Norbert Schmees , Hans-Peter Muhn , Thomas Frenzel , Florian Peter Liesener , Anna Schrey , Ronald Kuehne
IPC分类号： A61K31/437 , C07D471/04 , C07D409/12 , A61K31/416 , A61K31/4709 , A61P19/10 , A61P15/00 , A61K31/47 , C07D231/56 , A61K31/517
CPC分类号： C07D215/20 , C07D215/52 , C07D333/58 , C07D409/12 , C07D471/04
摘要： The present invention relates to arylmethylene substituted N-Acyl-β-amino alcohols of the formula I in which Y is selected from the aryl or heteroaryl groups: and R1, R2, R3, R4, R5, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译： 本发明涉及式I的芳基亚甲基取代的N-酰基-β-氨基醇，其中Y选自芳基或杂芳基：并且R 1，R 2，R 3，R 4，R 5，Q，X和W具有 如说明书中所定义。 根据本发明的化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。
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公开(公告)号：US20090075987A1
公开(公告)日：2009-03-19
申请号：US12178325
申请日：2008-07-23
申请人： Lars Wortmann , Marcus Koppitz , Hans Peter Muhn , Thomas Frenzel , Florian Peter Liesener , Anna Schrey , Ronald Kuehne
发明人： Lars Wortmann , Marcus Koppitz , Hans Peter Muhn , Thomas Frenzel , Florian Peter Liesener , Anna Schrey , Ronald Kuehne
IPC分类号： A61K31/541 , C07D209/18 , A61K31/404 , A61P15/08 , A61P19/10 , C07D417/02
CPC分类号： C07D209/14 , C07D405/12
摘要： The present invention relates to acyltryptophanols of the general formula I, in which R1, R2, R3, Q and X have the meaning as defined in the description.The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译： 本发明涉及通式Ⅰ的酰基色氨酸，其中R1，R2，R3，Q和X具有说明书中定义的含义。 根据本发明的化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。
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公开(公告)号：US20090069321A1
公开(公告)日：2009-03-12
申请号：US12181654
申请日：2008-07-29
申请人： Lars WORTMANN , Marcus Koppitz , Florian Peter Liesener , Thomas Frenzel , Hans-Peter Muhn , Anna Schrey , Ronald Kuehne
发明人： Lars WORTMANN , Marcus Koppitz , Florian Peter Liesener , Thomas Frenzel , Hans-Peter Muhn , Anna Schrey , Ronald Kuehne
IPC分类号： C07D209/18 , A61K31/404 , A61K31/5377 , C07D413/12 , C07D401/12 , A61K31/454 , A61K31/4709 , A61P19/10 , A61P15/16 , A61P15/18
CPC分类号： C07D209/16 , C07D209/14 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to cyanomethyl substituted N-acyl tryptamines of the formula I in whichR1, R2, R3, R4, R5, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译： 本发明涉及式I的氰基甲基取代的N-酰基色胺，其中R1，R2，R3，R4，R5，Q，X和W具有如说明书中所定义的含义。 根据本发明的化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。
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公开(公告)号：US20080275083A1
公开(公告)日：2008-11-06
申请号：US12055524
申请日：2008-03-26
申请人： Lars Wortmann , Marcus Koppitz , Hans Peter Muhn , Thomas Frenzel , Florian Peter Liesener , Anna Schrey , Ronald Kuehne
发明人： Lars Wortmann , Marcus Koppitz , Hans Peter Muhn , Thomas Frenzel , Florian Peter Liesener , Anna Schrey , Ronald Kuehne
IPC分类号： C07D209/82 , C07D401/12 , A61K31/4709 , A61K31/403 , A61P15/08
CPC分类号： C07D401/12 , C07D209/88 , C07D405/12
摘要： The present invention relates to 2,3,4,9-tetrahydro-1H-carbazoles of the general formula I, in which Q, X, W, R1, R2, R3, R4 and R5 have the meaning as defined in the description.The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译： 本发明涉及通式I的2,3,4,9-四氢-1H-咔唑，其中Q，X，W，R 1，R 2，R 3，R 4和R 5具有如说明书中所定义的含义。 根据本发明的化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。
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公开(公告)号：US20080221195A1
公开(公告)日：2008-09-11
申请号：US11955045
申请日：2007-12-12
申请人： Lars Wortmann , Hans-Peter Muhn , Bernd Menzenbach , Anna Schrey , Ronald Kuehne , Dirk Kosemund , Marcus Koppitz
发明人： Lars Wortmann , Hans-Peter Muhn , Bernd Menzenbach , Anna Schrey , Ronald Kuehne , Dirk Kosemund , Marcus Koppitz
IPC分类号： A61K31/404 , C07D209/20 , A61P15/00 , A61P19/10
CPC分类号： C07D209/20 , C07D209/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to acyltryptophanols of the general formula I, in which Q, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description.The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译： 本发明涉及通式I的酰基色氨酸，其中Q，W，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8具有如说明书中定义的含义。 根据本发明的化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。
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公开(公告)号：US20070060573A1
公开(公告)日：2007-03-15
申请号：US11501228
申请日：2006-08-09
申请人： Lars Wortmann , Arwed Cleve , Bernd Menzenbach , Hans-Peter Muhn , Gernot Langer , Anna Schrey , Ronald Kuehne , Marcu Koppitz , Dirk Kosemund
发明人： Lars Wortmann , Arwed Cleve , Bernd Menzenbach , Hans-Peter Muhn , Gernot Langer , Anna Schrey , Ronald Kuehne , Marcu Koppitz , Dirk Kosemund
IPC分类号： A61K31/551 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/405 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D209/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/14
摘要： The present patent application relates to acyltryptophanols of the general formula I, in which Q, X, Y, W, R1, R2, R3, R4, R5, R8 have the meanings stated in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译： 本发明涉及通式I的酰基色氨酸，其中Q，X，Y，W，R 1，R 2，R 3，R 4，R 5，R 8具有说明书中所述的含义。 根据本发明的化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。
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公开(公告)号：US20090069328A1
公开(公告)日：2009-03-12
申请号：US12191656
申请日：2008-08-14
申请人： Lars Wortmann , Marcus Koppitz , Hans Peter Muhn , Anna Schrey , Ronald Kuehne
发明人： Lars Wortmann , Marcus Koppitz , Hans Peter Muhn , Anna Schrey , Ronald Kuehne
IPC分类号： A61K31/404 , C07D209/18 , C07D413/14 , C07D403/14 , C07D409/12 , A61K31/5377 , A61K31/496 , A61K31/4725 , A61K31/4155 , A61K31/4178 , C07D403/12 , C07D401/12 , A61P15/00
CPC分类号： C07D209/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to α-alkyl substituted N-acyltryptophanols of the formula I in which R1, R2, R3, R4, R5, R6, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
摘要翻译： 本发明涉及式Ⅰ的α-烷基取代N-酰基色氨酸，其中R1，R2，R3，R4，R5，R6，Q，X和W具有说明书中定义的含义。 根据本发明的化合物是有效的FSH拮抗剂，可用于例如男性或女性的生育控制，或用于预防和/或治疗骨质疏松症。
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10.发明授权Structural mimetics of proline-rich peptides and the pharmaceutical use thereof 有权富含脯氨酸的肽的结构模拟物及其药物用途公开(公告)号：US08242105B2
公开(公告)日：2012-08-14
申请号：US12442681
申请日：2007-09-25
IPC分类号： A61K31/55 , C07D223/00
CPC分类号： C07D487/14
摘要： The invention relates to compounds of general formula (I), which can be used particularly as structural mimetics of proline-rich peptides and are therefore capable of binding PRM binding domains (proline-rich motif binding domains) of proteins. The invention also relates to the use of said compounds as pharmaceutical active agents and the use of these pharmaceutical active agents for treating bacterial diseases, neurodegenerative diseases and tumors.
摘要翻译： 本发明涉及通式（I）的化合物，其可特别用作富含脯氨酸的肽的结构模拟物，因此能够结合蛋白质的PRM结合结构域（富含脯氨酸的基序结合结构域）。 本发明还涉及所述化合物作为药物活性剂的用途以及这些药物活性剂用于治疗细菌性疾病，神经变性疾病和肿瘤的用途。
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