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1. 发明申请

US20080300270A1 4-Phenyl-5-Oxo-1,4,5,6,7,8,- Hexahydroquinoline Derivatives as Medicaments for the Treatment of Infertility 有权
标题翻译： 4-苯基-5-氧代-1,4,5,6,7,8-六氢喹啉衍生物作为治疗不孕症的药物
公开(公告)号：US20080300270A1
公开(公告)日：2008-12-04
申请号：US11912746
申请日：2006-05-02
申请人： Cornelis Marius Timmers , Willem Frederik Karstens , Pedro Manuel Grima Poveda
发明人： Cornelis Marius Timmers , Willem Frederik Karstens , Pedro Manuel Grima Poveda
IPC分类号： A61K31/47 , C07D215/02 , A61P15/08
CPC分类号： C07D401/12 , C07D215/20 , C07D405/12 , C07D417/12
摘要： The invention relates to a 4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivative according to Formula (I), wherein the substituents are defined as in the description, or a pharmaceutically salt thereof. The compounds of this invention are potent FSH receptor activators and may be used for treating fertility disorders in e.g. controlled ovarian hyperstimulation and IVF procedures.
摘要翻译：本发明涉及根据式（I）的4-苯基-5-氧代-1,4,5,6,7,8-六氢喹啉衍生物，其中取代基如描述中所定义，或其药学上的盐。本发明的化合物是有效的FSH受体激活剂，并且可以用于治疗生殖障碍。控制卵巢过度刺激和IVF手术。

2. 发明授权

US07858794B2 Tetrahydroquinoline derivatives 有权
标题翻译：四氢喹啉衍生物
公开(公告)号：US07858794B2
公开(公告)日：2010-12-28
申请号：US10540336
申请日：2003-12-16
申请人： Cornelis Marius Timmers , Willem Frederik Karstens
发明人： Cornelis Marius Timmers , Willem Frederik Karstens
IPC分类号： C07D215/00 , A61K31/47 , A61K31/4709
CPC分类号： C07D215/38 , C07D215/44 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12
摘要： The present invention relates to tetrahydroquinoline derivatives having gene formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are H or Me; R3 is H, hydroxy, (1-4C)alkoxy, (di)(1-4C)alkylamino(2-4C)alkoxy or (2-6)heterocycloakl(2-4C)alkoxy; R4 is H, OH, (1-4C)alkoxy or R7; R5 is H, OH, (1-4C)alkoxy or R7, with the proviso that if R4 is H, R5 is not H, OH or (1-4C)alkoxy and that if R5 is H, R4 is not H, OH or (1-4C)alkoxy; R6 is (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2 6C)heterocycloalkyl or (1-6C)alkyl; R7 is amino, (di)(1-4C)alkylamino, (6C)arylcarbonylamino, (6C)arylcarbonyloxy, (2-5C) heteroarylcarbonylamino, (2-5C)heteroarylcarbonyloxy, R8-(2-4C)alkylamino, R8-(2-4C)alkoxy, R9-methylamino or R9-methoxy; R8 is hydroxy, amino, (-14C)alkoxy, (di)(1-4C)alkylamino, (2-6C)heterocycloalkyl, (2-6C) heterocycloalkylcarbonylamino, (di)(1-4C)alkylaminocarbonylamino, (1-4C)alkoxycarbonylamino and R9 is aminocarbonyl, (di)(1-4C)alkylaminocarbonyl, (2-5C)heteroaryl or (6C)aryl. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to regulate fertility.
摘要翻译：本发明涉及具有基因式（I）的四氢喹啉衍生物或其药学上可接受的盐，其中R1和R2是H或Me; R3是H，羟基，（1-4C）烷氧基，（二）（1-4C）烷基氨基（2-4C）烷氧基或（2-6）杂环基（2-4C）烷氧基; R4是H，OH，（1-4C）烷氧基或R7; R5是H，OH，（1-4C）烷氧基或R7，条件是如果R4是H，R5不是H，OH或（1-4C）烷氧基，如果R5是H，R4不是H，OH 或（1-4C）烷氧基; R 6是（2-5C）杂芳基，（6C）芳基，（3-8C）环烷基，（2 6C）杂环烷基或（1-6C）烷基; R7是氨基，（二）（1-4C）烷基氨基，（6C）芳基羰基氨基，（6C）芳基羰基氧基，（2-5C）杂芳基羰基氨基，（2-5C）杂芳基羰氧基，R8-（2-4C）烷基氨基，R8-（ 2-4C）烷氧基，R9-甲基氨基或R9-甲氧基; R8是羟基，氨基，（-14C）烷氧基，（二）（1-4C）烷基氨基，（2-6C）杂环烷基，（2-6C）杂环烷基羰基氨基，（二）（1-4C）烷基氨基羰基氨基，（1-4C ）烷氧基羰基氨基，R 9为氨基羰基，（二）（1-4C）烷基氨基羰基，（2-5C）杂芳基或（6C）芳基。本发明还涉及包含所述衍生物的药物组合物和这些衍生物用于调节生育力的用途。

3. 发明授权

US08034945B2 4-phenyl-5-OXO-1,4,5,6,7,8-hexahydroquinoline derivatives as medicaments for the treatment of infertility 有权
标题翻译： 4-苯基-5-OXO-1,4,5,6,7,8-六氢喹啉衍生物作为治疗不孕症的药物
公开(公告)号：US08034945B2
公开(公告)日：2011-10-11
申请号：US11912746
申请日：2006-05-02
申请人： Cornelis Marius Timmers , Willem Frederik Karstens , Pedro Manuel Grima Poveda
发明人： Cornelis Marius Timmers , Willem Frederik Karstens , Pedro Manuel Grima Poveda
IPC分类号： C07D215/04 , C07D215/00 , C07D413/00
CPC分类号： C07D401/12 , C07D215/20 , C07D405/12 , C07D417/12
摘要： The invention relates to a 4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivative according to Formula (I), wherein the substituents are defined as in the description, or a pharmaceutically salt thereof. The compounds of this invention are potent FSH receptor activators and may be used for treating fertility disorders in e.g. controlled ovarian hyperstimulation and IVF procedures.
摘要翻译：本发明涉及根据式（I）的4-苯基-5-氧代-1,4,5,6,7,8-六氢喹啉衍生物，其中取代基如描述中所定义，或其药学上的盐。本发明的化合物是有效的FSH受体激活剂，并且可以用于治疗生殖障碍。控制卵巢过度刺激和IVF手术。

4. 发明授权

US07674909B2 Tetrahydroquinoline derivatives and their use as FSH receptor modulators 有权
标题翻译：四氢喹啉衍生物及其作为FSH受体调节剂的用途
公开(公告)号：US07674909B2
公开(公告)日：2010-03-09
申请号：US10540335
申请日：2003-12-16
申请人： Cornelis Marius Timmers , Willem Frederik Karstens
发明人： Cornelis Marius Timmers , Willem Frederik Karstens
IPC分类号： C07D215/12 , C07D215/14 , C07D413/00 , C07D241/00 , C07D241/02 , C07D307/02 , C07D315/00 , C07D407/00 , A01N37/18 , A61K31/16
CPC分类号： C07D215/38 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are H, Me; R3 is (2-6C)heterocycloalkyl(1-4C)alkyl, (2-5C)heteroaryl(1-4C)alkyl, (6C)aryl (1-4C)alkyl, (1-4C)(di)alkylaminocarbonylamino(2-4C)alkyl, (2-6C) heterocycloalkylcarbonylamino(2-4C)alkyl, R5-(2-4C)alkyl or R5-carbonyl(1-4C)alkyl; R4 is (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2-6C)heterocycloalkyl or (1-6C) alkyl and R5 is (di)(1-4C)alkylamino, (1-4C)alkoxy, amino, hydroxy, (6C)arylamino, (di)(3-4C)alkenylamino, (2-5C)heteroaryl(1-4C)alkylamino, (6C)aryl(1-4C) alkylamino, (di)[(1-4C)alkoxy(2-4C)alkyl]amino, (di)[(1-4C)alkylamino(2-4C) alkyl]amino, (di)[amino(2-4C)alkyl]amino or (di)[hydroxy(2-4C)alkyl]amino. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to regulate fertility.
摘要翻译：本发明涉及具有通式（I）的四氢喹啉衍生物或其药学上可接受的盐，其中R1和R2是H，Me; R3是（2-6C）杂环烷基（1-4C）烷基，（2-5C）杂芳基（1-4C）烷基，（6C）芳基（1-4C）烷基，（1-4C）（二）烷基氨基羰基氨基 -4C）烷基，（2-6C）杂环烷基羰基氨基（2-4C）烷基，R5-（2-4C）烷基或R5-羰基（1-4C）烷基; R4为（2-5C）杂芳基，（6C）芳基，（3-8C）环烷基，（2-6C）杂环烷基或（1-6C）烷基，R5为（二）（1-4C）烷基氨基，（1- （C 6）芳基氨基，（二）（3-4C）链烯基氨基，（2-5C）杂芳基（1-4C）烷基氨基，（6C）芳基（1-4C）烷基氨基，（二）氨基，（二）[氨基（2-4C）烷基]氨基或（（C 1 -C 4）烷基]氨基或（二）[羟基（2-4C）烷基]氨基。本发明还涉及包含所述衍生物的药物组合物和这些衍生物用于调节生育力的用途。

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