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1. 发明授权

US06900213B2 Bisaryl derivatives having FSH modulatory activity 失效
标题翻译：具有FSH调节活性的二芳基衍生物
公开(公告)号：US06900213B2
公开(公告)日：2005-05-31
申请号：US10623640
申请日：2003-07-21
申请人： Tao Guo , Koc-Kan Ho , Edward McDonald , Roland Ellwood Dolle , Kurt W. Saionz , Steven G. Kultgen , Ruiyan Liu , Guizhen Dong , Peng Geng , Anton Egbert Peter Adang , Nicole Corine Renee Van Straten
发明人： Tao Guo , Koc-Kan Ho , Edward McDonald , Roland Ellwood Dolle , Kurt W. Saionz , Steven G. Kultgen , Ruiyan Liu , Guizhen Dong , Peng Geng , Anton Egbert Peter Adang , Nicole Corine Renee Van Straten
IPC分类号： A61K38/00 , C07C237/22 , C07C271/22 , C07C275/14 , C07D207/26 , C07D207/273 , C07D223/10 , C07D233/76 , C07D241/08 , C07D243/08 , C07K5/06 , C07K5/065 , A61K31/495
CPC分类号： C07D207/273 , A61K38/00 , C07C237/22 , C07C271/22 , C07C275/14 , C07C2601/02 , C07D223/10 , C07D233/76 , C07D241/08 , C07D243/08 , C07K5/06078 , C07K5/06191
摘要： The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV or V: An example is (3S,6S)-1-N-(7-phenylheptyl)-3-(4-(3,4,5-trimethoxyphenyl)benzyl)-4-N-methyl-6-methyl-2,5-dioxo-1,4-piperazine: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.
摘要翻译：本发明涉及式I的二芳基衍生物，其中（R，R）选自（H，H），O，（H，CH 3），（H，OH）和（H ，CN）; Ar是取代的苯基，A是式II，III，IV或V的基团：实例是（3S，6S）-1-N-（7-苯基庚基）-3-（4-（3,4,5- 三甲氧基苯基）苄基）-4-N-甲基-6-甲基-2,5-二氧代-1,4-哌嗪本发明化合物具有FSH受体调节活性，可用于控制生育力，避孕或用于治疗激素依赖性疾病。

2. 发明申请

US20090215773A1 DIHYDROPYRIDINE DERIVATIVES 有权
标题翻译：二氢吡啶衍生物
公开(公告)号：US20090215773A1
公开(公告)日：2009-08-27
申请号：US11912719
申请日：2005-05-04
申请人： Nicole Corine Renee Van Straten , Gerritdina Geziena Gerritsma , Lars Anders Van Der Veen
发明人： Nicole Corine Renee Van Straten , Gerritdina Geziena Gerritsma , Lars Anders Van Der Veen
IPC分类号： A61K31/5377 , C07D215/00 , A61K31/47 , C07D409/02 , A61K31/4709 , C07D413/02 , A61P15/08
CPC分类号： C07D215/54
摘要： The present invention relates to dihydropyridine derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, phenyl, (1-5C)heteroaryl R2, R3 are independently (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkoxy, (24C)alkenyloxy, (2-4C)alkynyloxy, halogen X is SO2, CH2, C(O) or X is absent R4 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (3-6C)cycloalkyl, (3-6C)cycloalkenyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl, (2-6C)heterocycloalkyl(14C)alkyl, (6-1 OC)aryl, (6-10C)aryl(1-4C)alkyl, (1-9C)heteroaryl or (1-9C)heteroaryl(14C)alkyl. The compounds are useful for the treatment of fertility disorders.
摘要翻译：本发明涉及具有通式（I）的二氢吡啶衍生物或其药学上可接受的盐，其中R1为（1-6C）烷基，（2-6C）烯基，（2-6C）炔基，苯基，（1-5C ）杂芳基R2，R3独立地为（1-4C）烷基，（2-4C）烯基，（2-4C）炔基，（1-4C）烷氧基，（24C）烯氧基，（2-4C）炔氧基，卤素X SO 2，CH 2，C（O）或X不存在R 4是（1-6C）烷基，（2-6C）链烯基，（2-6C）炔基，（3-6C）环烷基，（3-6C）环烯基，（ 3-6C）环烷基（1-4C）烷基，（2-6C）杂环烷基，（2-6C）杂环烷基（14C）烷基，（6-1C）芳基，（6-10C）芳基（1-4C）烷基，（1-9C）杂芳基或（1-9C）杂芳基（14C）烷基。该化合物可用于治疗生育障碍。

3. 发明授权

US08258293B2 Tetrahydroquinoline derivatives 有权
公开(公告)号：US08258293B2
公开(公告)日：2012-09-04
申请号：US13268214
申请日：2011-10-07
申请人： Nicole Corine Renee Van Straten , Rudolf Gijsbertus Van Someren , Jurgen Schulz
发明人： Nicole Corine Renee Van Straten , Rudolf Gijsbertus Van Someren , Jurgen Schulz
IPC分类号： C07D215/08 , C07D215/12 , C07D215/20 , C07D215/38 , C07D215/48 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D215/38 , A61K31/47 , A61K31/4709 , C07D215/08 , C07D215/20 , C07D215/48
摘要： The present invention relates to tetrahydroquinoline derivatives having general formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1-4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; Y—X is C(O)—O, S(O)2-O, NHC(O)—O, NHC(S)—O, OC(O)—O, bond-O, C(O)—NH, S(O)2-NH, NHC(O)—NH, NHC(S)—NH, OC(O)—NH, bond-NH, NH—C(O), O—C(O), NH—S(O)2, or O—S(O)2 or Y—X is a bond; R6 is H, trifluoromethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8,R9-aminocarbonyl(1-4C)alkyl, R8,R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro, hydroxyl; and R8 and/or R9 is H, (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (6-10C)aryl, (3-9C)heteroaryl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, (1-4C)(di)alkylamino(1-4C)alkyl, (1-4C)alkoxy(1-4C)alkyl, (1-4C)alkylthio(1-4C)alkyl, (1-4C)alkylcarbonylamino(1-4C)alkyl, (1-4C)alkoxycarbonyl(1-4C)alkyl, (1-4C)alkoxycarbonylamino(1-4C)alkyl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, or R8 and R9 may be joined in a (2-6C)heterocycloalkyl ring. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to control fertility.

4. 发明授权

US07994189B2 Dihydropyridine derivatives 有权
标题翻译：二氢吡啶衍生物
公开(公告)号：US07994189B2
公开(公告)日：2011-08-09
申请号：US11912719
申请日：2005-05-04
申请人： Nicole Corine Renee Van Straten , Gerritdina Geziena Gerritsma , Lars Anders Van Der Veen
发明人： Nicole Corine Renee Van Straten , Gerritdina Geziena Gerritsma , Lars Anders Van Der Veen
IPC分类号： A61K31/44 , A61K31/47
CPC分类号： C07D215/54
摘要： The present invention relates to dihydropyridine derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, phenyl, (1-5C)heteroaryl R2, R3 are independently (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkoxy, (24C)alkenyloxy, (2-4C)alkynyloxy, halogen X is SO2, CH2, C(O) or X is absent R4 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (3-6C)cycloalkyl, (3-6C)cycloalkenyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl, (2-6C)heterocycloalkyl(14C)alkyl, (6-1 OC)aryl, (6-10C)aryl(1-4C)alkyl, (1-9C)heteroaryl or (1-9C)heteroaryl(14C)alkyl. The compounds are useful for the treatment of fertility disorders.
摘要翻译：本发明涉及具有通式（I）的二氢吡啶衍生物或其药学上可接受的盐，其中R1为（1-6C）烷基，（2-6C）烯基，（2-6C）炔基，苯基，（1-5C ）杂芳基R2，R3独立地为（1-4C）烷基，（2-4C）烯基，（2-4C）炔基，（1-4C）烷氧基，（24C）烯氧基，（2-4C）炔氧基，卤素X SO 2，CH 2，C（O）或X不存在R 4是（1-6C）烷基，（2-6C）链烯基，（2-6C）炔基，（3-6C）环烷基，（3-6C）环烯基，（ 3-6C）环烷基（1-4C）烷基，（2-6C）杂环烷基，（2-6C）杂环烷基（14C）烷基，（6-1C）芳基，（6-10C）芳基（1-4C）烷基，（1-9C）杂芳基或（1-9C）杂芳基（14C）烷基。该化合物可用于治疗生育障碍。

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