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1. 发明授权

US07960560B2 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione 失效
标题翻译： 1-（联苯-4-基甲基）咪唑烷-2,4-二酮
公开(公告)号：US07960560B2
公开(公告)日：2011-06-14
申请号：US12628523
申请日：2009-12-01
申请人： Marcelis van der Stelt , Joseph Maria Gerardus Barbara Cals
发明人： Marcelis van der Stelt , Joseph Maria Gerardus Barbara Cals
IPC分类号： C07D487/10 , C07D233/40 , C07D401/10 , C07D417/10 , C07D413/10 , A61K31/54 , A61K31/5377 , A61K31/4523 , A61K31/4166
CPC分类号： C07D233/74 , C07D401/10
摘要： The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2′ are independently H or (C1-3)alkyl; or R2 and R2′ form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y represents or NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.
摘要翻译：本发明涉及具有通式I的1-（联苯-4-基甲基）咪唑烷-2,4-二酮衍生物，其中R 1是H，（C 1-6）烷基（任选被氧代取代，OR 4，COOR 5，卤素或 CN），（C2-6）烯基，（C2-6）炔基，（C3-6）环烷基或（C3-6）环烷基（C1-3）烷基; R2和R2'独立地为H或（C1-3）烷基; 或R 2和R 2'与它们所连接的碳原子一起形成（C 3-5）环烷基; R 3表示H或1至4个F取代基; Y表示或NR8R9; X表示CHR6，CF2，O，S，SO或SO2; R4和R5是（C1-6）烷基; R6是H，OR7或CN; R7是（C1-3）烷基; R8是包含选自O，S，SO和SO 2的杂原子的（C5-7）环烷基; R 9为H或（C 1-4）烷基; o和m表示取代基Y-CH 2的邻位或间位; 或其药学上可接受的盐; 以及所述1-（联苯-4-基甲基）咪唑烷-2,4-二酮衍生物在治疗疼痛中的用途，例如手术前疼痛，慢性疼痛，神经性疼痛，癌症疼痛和疼痛，以及与多发性硬化有关的痉挛症。

2. 发明申请

US20100144724A1 1-(4-(PYRIDIN-2-YL)BENZYL)IMIDAZOLIDINE-2,4-DIONE DERIVATIVES 失效
标题翻译： 1-（4-（吡啶-2-基）苄基）咪唑烷-2,4-二酮衍生物
公开(公告)号：US20100144724A1
公开(公告)日：2010-06-10
申请号：US12628538
申请日：2010-02-15
申请人： Marcelis van der Stelt , Joseph Maria Gerardus Barbara Cals , Johannes Petrus Gerardus Klomp
发明人： Marcelis van der Stelt , Joseph Maria Gerardus Barbara Cals , Johannes Petrus Gerardus Klomp
IPC分类号： A61K31/541 , C07D401/14 , A61K31/4545 , C07D413/14 , A61K31/5377 , C07D417/14 , A61P43/00
CPC分类号： C07D401/10 , C07D401/14 , C07D405/14
摘要： The invention relates to 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, (C1-3)alkyloxy, (C1-3)alkyloxycarbonyl, halogen or CN), (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each cycloalkyl ring optionally comprising a heteroatom selected from O and S; R2 and R3 are independently H or (C1-3)alkyl; or R2 and R3 form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R4 is H or 1 to 3 F substituents; R5 is H or 1 to 4 F substituents; R6 and R7 are independently H or F; X represents R8, OR8, NR8R9, R8 is (C5-7)cycloalkyl optionally comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; R10 represents 1-3 substituents independently selected from H, (C1-3)alkyl, halogen, oxo, CN and CF3; Y is CF2, O, S, SO or SO2; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.
摘要翻译：本发明涉及具有通式I的1-（4-（吡啶-2-基）苄基）咪唑烷-2,4-二酮衍生物，其中R 1是H，（C 1-6）烷基（任选被氧代取代，（C 1 -3）烷氧基，（C1-3）烷氧基羰基，卤素或CN），（C3-6）环烷基或（C3-6）环烷基（C1-3）烷基，每个环烷基环任选地包含选自O和S的杂原子; R2和R3独立地是H或（C1-3）烷基; 或者R 2和R 3与它们所连接的碳原子一起形成（C 3-5）环烷基; R4为H或1〜3F取代基; R5为H或1〜4F取代基; R6和R7独立地为H或F; X代表R8，OR8，NR8R9，R8是任选地含有选自O，S，SO和SO 2的杂原子的（C5-7）环烷基; R 9为H或（C 1-4）烷基; R 10表示1-3个独立地选自H，（C 1-3）烷基，卤素，氧代，CN和CF 3的取代基; Y为CF 2，O，S，SO或SO 2; 或其药学上可接受的盐用于包含其的药物组合物，以及所述1-（4-（吡啶-2-基）苄基）咪唑烷-2,4-二酮衍生物在治疗疼痛中的用途，例如例如围手术期疼痛，慢性疼痛，神经性疼痛，癌症疼痛和与多发性硬化相关的疼痛和痉挛状态。

3. 发明申请

US20100144723A1 1-(BIPHENYL-4-YLMETHYL)IMIDAZOLIDINE-2,4-DIONE 失效
标题翻译： 1-（联苯-4-基甲基）咪唑烷-2,4-二酮
公开(公告)号：US20100144723A1
公开(公告)日：2010-06-10
申请号：US12628523
申请日：2009-12-01
申请人： Marcelis van der Stelt , Joseph Maria Gerardus Barbara Cals
发明人： Marcelis van der Stelt , Joseph Maria Gerardus Barbara Cals
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/454 , A61K31/4178 , C07D417/10 , C07D413/10 , C07D401/10 , C07D405/10 , A61P29/02 , A61P25/02
CPC分类号： C07D233/74 , C07D401/10
摘要： The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2′ are independently H or (C1-3)alkyl; or R2 and R2′ form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y represents or NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.
摘要翻译：本发明涉及具有通式I的1-（联苯-4-基甲基）咪唑烷-2,4-二酮衍生物，其中R 1是H，（C 1-6）烷基（任选被氧代取代，OR 4，COOR 5，卤素或 CN），（C2-6）烯基，（C2-6）炔基，（C3-6）环烷基或（C3-6）环烷基（C1-3）烷基; R2和R2'独立地为H或（C1-3）烷基; 或R 2和R 2'与它们所连接的碳原子一起形成（C 3-5）环烷基; R 3表示H或1至4个F取代基; Y表示或NR8R9; X表示CHR6，CF2，O，S，SO或SO2; R4和R5是（C1-6）烷基; R6是H，OR7或CN; R7是（C1-3）烷基; R8是包含选自O，S，SO和SO 2的杂原子的（C5-7）环烷基; R 9为H或（C 1-4）烷基; o和m表示取代基Y-CH 2的邻位或间位; 或其药学上可接受的盐; 以及所述1-（联苯-4-基甲基）咪唑烷-2,4-二酮衍生物在治疗疼痛中的用途，例如手术前疼痛，慢性疼痛，神经性疼痛，癌症疼痛和疼痛，以及与多发性硬化有关的痉挛症。

4. 发明授权

US08993757B2 N-piperidin-4-yl derivatives 有权
标题翻译： N-哌啶-4-基衍生物
公开(公告)号：US08993757B2
公开(公告)日：2015-03-31
申请号：US14346241
申请日：2012-09-14
申请人： Ines Huisman , Marcelis Van Der Stelt , Wouter Wiedenhof , Charles Anthony Graham Baker-Glenn , Wesley Peter Blackaby , Naimisha Trivedi
发明人： Ines Huisman , Marcelis Van Der Stelt , Wouter Wiedenhof , Charles Anthony Graham Baker-Glenn , Wesley Peter Blackaby , Naimisha Trivedi
IPC分类号： C07D401/04 , C07D401/14 , A61K31/444 , C07D417/14 , C07D405/14 , C07D413/14
CPC分类号： C07D417/14 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The invention relates to a N-piperidin-4-yl derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said N-piperidin-4-yl derivatives for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, or for the treatment of uterine fibroids or other menstrual-related disorders.
摘要翻译：本发明涉及具有通式I的N-哌啶-4-基衍生物或其药学上可接受的盐，涉及含有该通式I的药物组合物和所述N-哌啶-4-基衍生物用于治疗和预防的用途的子宫内膜异位症，用于治疗和预防绝经前和绝经前激素依赖性乳腺癌，用于避孕，或用于治疗子宫肌瘤或其他月经相关疾病。

5. 发明申请

US20140329822A1 N-PIPERIDIN-4-YL DERIVATIVES 有权
标题翻译： N-PIPERIDIN-4-YL衍生物
公开(公告)号：US20140329822A1
公开(公告)日：2014-11-06
申请号：US14346241
申请日：2012-09-14
申请人： Ines Huisman , Marcelis Van Der Stelt , Wouter Wiedenhof , Charles Anthony Graham Baker-Glenn , Wesley Peter Blackaby , Naimisha Trivedi
发明人： Ines Huisman , Marcelis Van Der Stelt , Wouter Wiedenhof , Charles Anthony Graham Baker-Glenn , Wesley Peter Blackaby , Naimisha Trivedi
IPC分类号： C07D417/14 , C07D401/04 , C07D405/14 , C07D401/14 , C07D413/14
CPC分类号： C07D417/14 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The invention relates to a N-piperidin-4-yl derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said N-piperidin-4-yl derivatives for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, or for the treatment of uterine fibroids or other menstrual-related disorders.
摘要翻译：本发明涉及具有通式I的N-哌啶-4-基衍生物或其药学上可接受的盐，涉及含有该通式I的药物组合物和所述N-哌啶-4-基衍生物用于治疗和预防的用途的子宫内膜异位症，用于治疗和预防绝经前和绝经前激素依赖性乳腺癌，用于避孕，或用于治疗子宫肌瘤或其他月经相关疾病。

6. 发明授权

US08143246B2 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives 失效
标题翻译： 1-（4-（吡啶-2-基）苄基）咪唑烷-2,4-二酮衍生物
公开(公告)号：US08143246B2
公开(公告)日：2012-03-27
申请号：US12628538
申请日：2010-02-15
申请人： Marcelis van der Stelt , Joseph Maria Gerardus Barbara Cals , Johannes Petrus Gerardus Klomp
发明人： Marcelis van der Stelt , Joseph Maria Gerardus Barbara Cals , Johannes Petrus Gerardus Klomp
IPC分类号： C07D417/14 , C07D401/14 , C07D413/14 , C07D405/14 , A61K31/445 , A61K31/541
CPC分类号： C07D401/10 , C07D401/14 , C07D405/14
摘要： The invention relates to 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, (C1-3)alkyloxy, (C1-3)alkyloxycarbonyl, halogen or CN), (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each cycloalkyl ring optionally comprising a heteroatom selected from O and S; R2 and R3 are independently H or (C1-3)alkyl; or R2 and R3 form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R4 is H or 1 to 3 F substituents; R5 is H or 1 to 4 F substituents; R6 and R7 are independently H or F; X represents R8, OR8, NR8R9, R8 is (C5-7)cycloalkyl optionally comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; R10 represents 1-3 substituents independently selected from H, (C1-3)alkyl, halogen, oxo, CN and CF3; Y is CF2, O, S, SO or SO2; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.
摘要翻译：本发明涉及具有通式I的1-（4-（吡啶-2-基）苄基）咪唑烷-2,4-二酮衍生物，其中R 1是H，（C 1-6）烷基（任选被氧代取代，（C 1 -3）烷氧基，（C1-3）烷氧基羰基，卤素或CN），（C3-6）环烷基或（C3-6）环烷基（C1-3）烷基，每个环烷基环任选地包含选自O和S的杂原子; R2和R3独立地是H或（C1-3）烷基; 或者R 2和R 3与它们所连接的碳原子一起形成（C 3-5）环烷基; R4为H或1〜3F取代基; R5为H或1〜4F取代基; R6和R7独立地为H或F; X代表R8，OR8，NR8R9，R8是任选地含有选自O，S，SO和SO 2的杂原子的（C5-7）环烷基; R 9为H或（C 1-4）烷基; R 10表示1-3个独立地选自H，（C 1-3）烷基，卤素，氧代，CN和CF 3的取代基; Y为CF 2，O，S，SO或SO 2; 或其药学上可接受的盐用于包含其的药物组合物，以及所述1-（4-（吡啶-2-基）苄基）咪唑烷-2,4-二酮衍生物在治疗疼痛中的用途，例如例如围手术期疼痛，慢性疼痛，神经性疼痛，癌症疼痛和与多发性硬化相关的疼痛和痉挛状态。

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