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1. 发明授权

US08227504B2 Substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides and therapeutic use thereof 有权
标题翻译：取代的N-苯基 - 吡咯烷基甲基吡咯烷酰胺及其治疗用途
公开(公告)号：US08227504B2
公开(公告)日：2012-07-24
申请号：US12724044
申请日：2010-03-15
申请人： Werngard Czechtizky , Zhongli Gao , William Joseph Hurst , Lothar Schwink , Siegfried Stengelin
发明人： Werngard Czechtizky , Zhongli Gao , William Joseph Hurst , Lothar Schwink , Siegfried Stengelin
IPC分类号： A61K31/5513 , A61K31/4725 , A61K31/4439 , A61K31/422 , A61K31/4184 , A61K31/4178 , A61K31/4155 , A61K31/404 , A61K31/4025 , C07D471/04 , C07D405/14 , C07D407/14 , C07D401/14 , C07D403/14 , C07D403/06
CPC分类号： C07D401/12 , C07D207/09 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.
摘要翻译：本发明公开并要求一系列取代的式（I）的N-苯基 - 吡咯烷基甲基吡咯烷酰胺。其中R，R 1，R 2，R 3和R 4如本文所述。更具体地，本发明的化合物是H3受体的调节剂，因此可用作药剂，特别是用于治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。此外，本发明还公开了制备取代的吡咯烷基甲基吡咯烷酰胺及其中间体的方法。

2. 发明授权

US08222290B2 Substituted N-phenyl-bipyrrolidine ureas and therapeutic use thereof 有权
标题翻译：取代的N-苯基 - 联吡咯烷脲及其治疗用途
公开(公告)号：US08222290B2
公开(公告)日：2012-07-17
申请号：US12724045
申请日：2010-03-15
申请人： Werngard Czechtizky , Zhongli Gao , William Joseph Hurst , Lothar Schwink , Siegfried Stengelin
发明人： Werngard Czechtizky , Zhongli Gao , William Joseph Hurst , Lothar Schwink , Siegfried Stengelin
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4035 , A61K31/4025 , C07D413/14 , C07D409/14 , C07D401/14 , C07D403/14 , C07D403/04
CPC分类号： C07D207/06 , C07D403/12 , C07D409/12
摘要： The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine ureas of formula (I). Wherein R, R1, R2, R3, R4 and R5 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine ureas and intermediates therefor.
摘要翻译：本发明公开并要求一系列式（I）的取代的N-苯基 - 联吡咯烷脲。其中R，R 1，R 2，R 3，R 4和R 5如本文所述。更具体地，本发明的化合物是H3受体的调节剂，因此可用作药剂，特别是用于治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。此外，本发明还公开了制备取代的N-苯基 - 联吡咯烷脲及其中间体的方法。

3. 发明授权

US08618159B2 Substituted N-phenyl-bipyrrolidine carboxamides and therapeutic use thereof 有权
标题翻译：取代的N-苯基 - 联吡咯烷甲酰胺及其治疗用途
公开(公告)号：US08618159B2
公开(公告)日：2013-12-31
申请号：US12724035
申请日：2010-03-15
申请人： Werngard Czechtizky , Zhongli Gao , William Joseph Hurst , Lothar Schwink , Siegfried Stengelin
发明人： Werngard Czechtizky , Zhongli Gao , William Joseph Hurst , Lothar Schwink , Siegfried Stengelin
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4035 , A61K31/4025 , C07D413/14 , C07D409/14 , C07D401/14 , C07D403/14 , C07D403/04
CPC分类号： C07D207/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D471/04
摘要： The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.
摘要翻译：本发明公开并要求一系列式（I）的取代的N-苯基 - 联吡咯烷甲酰胺。其中R，R 1，R 2，R 3和R 4如本文所述。更具体地，本发明的化合物是H3受体的调节剂，因此可用作药剂，特别是用于治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。此外，本发明还公开了制备取代的N-苯基 - 联吡咯烷甲酰胺及其中间体的方法。

4. 发明授权

US08252824B2 Substituted N-phenyl-bipyrrolidine carboxamides and therapeutic use thereof 有权
标题翻译：取代的N-苯基 - 联吡咯烷甲酰胺及其治疗用途
公开(公告)号：US08252824B2
公开(公告)日：2012-08-28
申请号：US13299574
申请日：2011-11-18
申请人： Werngard Czechtizky , Zhongli Gao , William Joseph Hurst , Lothar Schwink , Siegfried Stengelin
发明人： Werngard Czechtizky , Zhongli Gao , William Joseph Hurst , Lothar Schwink , Siegfried Stengelin
IPC分类号： A61K31/422 , A61K31/4025
CPC分类号： C07D413/12 , C07D207/06 , C07D401/14 , C07D403/12 , C07D405/12
摘要： The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.
摘要翻译：本发明公开并要求一系列式（I）的取代的N-苯基 - 联吡咯烷甲酰胺。其中R，R 1，R 2，R 3和R 4如本文所述。更具体地，本发明的化合物是H3受体的调节剂，因此可用作药剂，特别是用于治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。此外，本发明还公开了制备取代的N-苯基 - 联吡咯烷甲酰胺及其中间体的方法。

5. 发明授权

US08088808B2 Substituted N-phenyl-bipyrrolidine carboxamides and therapeutic use thereof 有权
标题翻译：取代的N-苯基 - 联吡咯烷甲酰胺及其治疗用途
公开(公告)号：US08088808B2
公开(公告)日：2012-01-03
申请号：US12724028
申请日：2010-03-15
申请人： Werngard Czechtizky , Zhongli Gao , William Joseph Hurst , Lothar Schwink , Siegfried Stengelin
发明人： Werngard Czechtizky , Zhongli Gao , William Joseph Hurst , Lothar Schwink , Siegfried Stengelin
IPC分类号： A61K31/422 , A61K31/4025 , C07D261/18 , C07D403/04 , C07D405/14
CPC分类号： C07D413/12 , C07D207/06 , C07D401/14 , C07D403/12 , C07D405/12
摘要： The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.
摘要翻译：本发明公开并要求一系列式（I）的取代的N-苯基 - 联吡咯烷甲酰胺。其中R，R 1，R 2，R 3和R 4如本文所述。更具体地，本发明的化合物是H3受体的调节剂，因此可用作药剂，特别是用于治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。此外，本发明还公开了制备取代的N-苯基 - 联吡咯烷甲酰胺及其中间体的方法。

6. 发明授权

US08846676B2 6-cycloamino-3-(pyrid-4-yl)imidazo[1,2-b]pyridazine derivatives, preparation thereof and therapeutic use thereof 有权
标题翻译： 6-环氨基-3-（吡啶-4-基）咪唑并[1,2-b]哒嗪衍生物及其治疗用途
公开(公告)号：US08846676B2
公开(公告)日：2014-09-30
申请号：US13617678
申请日：2012-09-14
申请人： Antonio Almario Garcia , Mathieu Barrague , Philippe Burnier , Cecile Enguehard-Gueiffier , Zhongli Gao , Pascal George , Alain Gueiffier , Adrien Tak Li , Frederic Peuch , Roy Vaz , Qiuxia Zhao
发明人： Antonio Almario Garcia , Mathieu Barrague , Philippe Burnier , Cecile Enguehard-Gueiffier , Zhongli Gao , Pascal George , Alain Gueiffier , Adrien Tak Li , Frederic Peuch , Roy Vaz , Qiuxia Zhao
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.
摘要翻译：本发明涉及对应于通式（I）的6-环氨基-3-（吡啶-4-基）咪唑并[ⅰ，2-b]哒嗪衍生物：其中R2，R3，R7，R8，A，L和B 如本文所定义。还公开了其制备方法及其治疗用途。

7. 发明授权

US08227481B2 Substituted piperidine spiro pyrrolidinone and piperidinone, preparation and therapeutic use thereof 有权
标题翻译：取代的哌啶螺吡咯烷酮和哌啶酮，其制备和治疗用途
公开(公告)号：US08227481B2
公开(公告)日：2012-07-24
申请号：US13151946
申请日：2011-06-02
申请人： Zhongli Gao , Daniel Hall , Ryan Hartung
发明人： Zhongli Gao , Daniel Hall , Ryan Hartung
IPC分类号： C07D401/04 , A61K31/438
CPC分类号： C07D471/10
摘要： The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). wherein R1, R2, R3, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor are disclosed.
摘要翻译：本公开涉及一系列式（I）的取代的N-苯基 - 联吡咯烷甲酰胺。其中R1，R2，R3，m，n和p如本文所述。更具体地，本发明的化合物是H3受体的调节剂，因此可用作药剂，特别是用于治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。另外，公开了制备取代的N-苯基 - 联吡咯烷甲酰胺及其中间体的方法。

8. 发明申请

US20070142435A1 [4-(5-Aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(4-bromo-3-methyl-5-propoxy-thiophen-2-yl)-methanone hydrochloride as an inhibitor of mast cell tryptase 审中-公开
标题翻译： [4-（5-氨基甲基-2-氟 - 苯基） - 哌啶-1-基] - （4-溴-3-甲基-5-丙氧基 - 噻吩-2-基） - 甲酮盐酸盐作为肥大细胞的抑制剂类胰蛋白酶
公开(公告)号：US20070142435A1
公开(公告)日：2007-06-21
申请号：US11520998
申请日：2006-09-14
申请人： Zhongli Gao , Larry Davis , Julian Levell , Mark Czekaj , Adam Sledeski
发明人： Zhongli Gao , Larry Davis , Julian Levell , Mark Czekaj , Adam Sledeski
IPC分类号： A61K31/453 , C07D409/02
CPC分类号： C07D409/06
摘要： The present invention extends to the compound of formula I: or a prodrug, pharmaceutically acceptable salt, or solvate of said compound. Furthermore, the present invention is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier. Furthermore, the present invention is directed to the use of a compound of formula I as an inhibitor of tryptase, comprising introducing the compound into a composition comprising tryptase. In addition, the present invention is directed to the use of a compound of formula I for treating a patient suffering from, or subject to, a physiological condition in need of amelioration of an inhibitor of tryptase comprising administering to the patient a therapeutically effective amount of the compound of claim 1 The present invention is directed also to the preparation of a compound of formula I.
摘要翻译：本发明延伸到式I化合物：或所述化合物的前药，药学上可接受的盐或溶剂合物。此外，本发明涉及包含药学有效量的式I化合物和药学上可接受的载体的药物组合物。此外，本发明涉及式I化合物作为类胰蛋白酶抑制剂的用途，其包括将化合物引入包含类胰蛋白酶的组合物中。此外，本发明涉及式I化合物用于治疗患有或受制于需要改善类胰蛋白酶抑制剂的生理条件的患者，包括向患者施用治疗有效量的权利要求1的化合物本发明还涉及式I化合物的制备。

9. 发明授权

US5734062A Method of preparation of physostigmine carbamate derivatives from eseretholes 失效
标题翻译：从eseretholes制备毒扁豆碱氨基甲酸酯衍生物的方法
公开(公告)号：US5734062A
公开(公告)日：1998-03-31
申请号：US858987
申请日：1997-05-20
申请人： Thomas B. K. Lee , Zhongli Gao
发明人： Thomas B. K. Lee , Zhongli Gao
IPC分类号： C07D487/04 , C07D471/02
CPC分类号： C07D487/04
摘要： This invention relates to a process for the preparation of a product of the formula ##STR1## wherein R is loweralkyl; R.sub.1 is hydrogen, loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl; Rs is loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl; or R.sub.1 and R.sub.2 taken together with the nitrogen atom to which they are attached form a group of the formula (Ia) ##STR2## wherein Y is hydrogen or loweralkyl and Z is hydrogen, loweralkyl, halogen, loweralkoxy or hydroxy; X is loweralkyl, loweralkoxy, halogen or trifluoromethyl; and m is 0, 1 or 2; or a pharmaceutically acceptable salt thereof; which process comprises(a) contacting a compound of formula (II) as defined herein with fortified hydrogen bromide to afford a compound of formula (III) as defined herein; contacting the reaction mixture containing a compound of formula (III) with either (1) an isocyanate of formula R.sub.1 NCO or (2) with a compound of formula (IV) as defined to afford a compound of formula (V) as defined herein and contacting the reaction mixture containing the compound of formula (V) with an amine of the formula R.sub.1 R.sub.2 NH herein in the presence of a carboxylic acid of the formula R.sub.5 COOH and forming and isolating the product of Formula (I).
摘要翻译：本发明涉及一种制备式（I）的产物的方法，其中R是低级烷基; R 1是氢，低级烷基，低级环烷基，低级环烷基低级烷基，低级双环烷基，芳基或芳基低级烷基; 低级烷基，低级环烷基，低级环烷基低级烷基，低级二环烷基，芳基或芳基低级烷基; 或者R 1和R 2与它们所连接的氮原子一起形成式（Ia）的基团，其中Y是氢或低级烷基，Z是氢，低级烷基，卤素，低级烷氧基或羟基; X是低级烷基，低级烷氧基，卤素或三氟甲基; m为0,1或2; 或其药学上可接受的盐; 该方法包括（a）使本文定义的式（II）化合物与强化溴化氢接触，得到本文定义的式（III）化合物; 使含有式（III）化合物的反应混合物与（1）式R1NCO或（2）的异氰酸酯与式（IV）化合物的定义相接触，得到如本文所定义的式（V）化合物和接触本文在式R 5 COOH的羧酸存在下将含有式（Ⅴ）化合物的反应混合物与式R 1 R 2 NH的胺反应，并形成并分离式（I）的产物。

10. 发明授权

US5665880A Method of preparation of physostigmine carbamate derivatives from eseretholes 失效
标题翻译：从eseretholes制备毒扁豆碱氨基甲酸酯衍生物的方法
公开(公告)号：US5665880A
公开(公告)日：1997-09-09
申请号：US739402
申请日：1996-10-31
申请人： Thomas B. K. Lee , Zhongli Gao
发明人： Thomas B. K. Lee , Zhongli Gao
IPC分类号： C07D487/04 , C07D471/02
CPC分类号： C07D487/04
摘要： This invention relates to a process for the preparation of a product of the formula ##STR1## wherein R is loweralkyl; R.sub.1, is hydrogen, loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralyl; R.sub.2 is lower alkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl; or R.sub.1 and R.sub.2 taken together with the nitrogen atom to which they are attached form a group of the formula (Ia) ##STR2## wherein Y is hydrogen or loweralkyl and Z is hydrogen, loweralkyl, halogen, loweralkoxy or hydroxy; X is loweralkyl, loweralkoxy, halogen or trifluoromethyl; and m is 0, 1 or 2; or a pharmaceutically acceptable salt thereof; which process comprises(a) contacting a compound of formula (II) as defined herein with fortified hydrogen bromide to afford a compound of formula (III) as defined herein; contacting the reaction mixture containing a compound of formula (III) with either (1) an isocyanate of formula R.sub.1 NCO or (2) with a compound of formula (IV) as defined to afford a compound of formula (V) as defined herein and contacting the reaction mixture containing the compound of formula (V) with an amine of the formula R.sub.1 R.sub.2 NH herein in the presence of a carboxylic acid of the formula R.sub.5 COOH and forming and isolating the product of Formula (I).
摘要翻译：本发明涉及一种制备式（I）的产物的方法，其中R是低级烷基; R1，是氢，低级烷基，低级环烷基，低级环烷基低级烷基，低级双环烷基，芳基或芳基甲酰基; R2是低级烷基，低级环烷基，低级环烷基低级烷基，低级二环烷基，芳基或芳基低级烷基; 或者R 1和R 2与它们所连接的氮原子一起形成式（Ia）的基团，其中Y是氢或低级烷基，Z是氢，低级烷基，卤素，低级烷氧基或羟基; X是低级烷基，低级烷氧基，卤素或三氟甲基; m为0,1或2; 或其药学上可接受的盐; 该方法包括（a）使本文定义的式（II）化合物与强化溴化氢接触，得到本文定义的式（III）化合物; 使含有式（III）化合物的反应混合物与（1）式R1NCO或（2）的异氰酸酯与式（IV）化合物的定义相接触，得到如本文所定义的式（V）化合物和接触本文在式R 5 COOH的羧酸存在下将含有式（Ⅴ）化合物的反应混合物与式R 1 R 2 NH的胺反应，并形成并分离式（I）的产物。

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