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1. 发明授权

US08143419B2 Trisubstituted 1,2,4-triazoles 有权
标题翻译：三取代的1,2,4-三唑
公开(公告)号：US08143419B2
公开(公告)日：2012-03-27
申请号：US12297059
申请日：2007-04-19
申请人： Johannes Wilhelmus John F. Thuring , Gregor James MacDonald , Anne Simone Josephine Lesage , Wei Zhuang , Marcel Frans Leopold De Bruyn , Frans Alfons Maria Van Den Keybus , Yves Emiel Maria Van Roosbroeck , Theodorus Dinklo , James Edward Stewart Duffy
发明人： Johannes Wilhelmus John F. Thuring , Gregor James MacDonald , Anne Simone Josephine Lesage , Wei Zhuang , Marcel Frans Leopold De Bruyn , Frans Alfons Maria Van Den Keybus , Yves Emiel Maria Van Roosbroeck , Theodorus Dinklo , James Edward Stewart Duffy
IPC分类号： A61K31/41 , C07D249/08
CPC分类号： C07D249/08 , C07D249/14 , C07D401/04 , C07D405/04 , C07D405/14 , C07D413/14 , C07D491/044 , C07D491/048
摘要： The present invention relates to 3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.
摘要翻译：本发明涉及3-苯胺-5-芳基三唑衍生物及其类似物或药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途，根据式（I）。本发明特别涉及烟碱乙酰胆碱受体的正变构调节剂，这种正变构调节剂具有增加烟碱受体激动剂功效的能力。

2. 发明申请

US20090253691A1 TRISUBSTITUTED 1,2,4-TRIAZOLES 有权
标题翻译：分离的1,2,4-TRIAZOLES
公开(公告)号：US20090253691A1
公开(公告)日：2009-10-08
申请号：US12297059
申请日：2007-04-19
申请人： Johannes Wilhelmus John F. Thuring , Gregor James MacDonald , Anne Simone Josephine Lesage , Wei Zhuang , Marcel Frans Leopold De Bruyn , Frans Alfons Maria Van Den Keybus , Yves Emiel Maria Van Roosbroeck , Theodorus Dinklo
发明人： Johannes Wilhelmus John F. Thuring , Gregor James MacDonald , Anne Simone Josephine Lesage , Wei Zhuang , Marcel Frans Leopold De Bruyn , Frans Alfons Maria Van Den Keybus , Yves Emiel Maria Van Roosbroeck , Theodorus Dinklo
IPC分类号： A61K31/538 , C07D407/10 , A61K31/4196 , A61K31/4439 , C07D401/04 , C07D491/048 , A61K31/4355 , C07D413/10
CPC分类号： C07D249/08 , C07D249/14 , C07D401/04 , C07D405/04 , C07D405/14 , C07D413/14 , C07D491/044 , C07D491/048
摘要： The present invention relates to 3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.
摘要翻译：本发明涉及3-苯胺-5-芳基三唑衍生物及其类似物或药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途，根据式（I）。本发明特别涉及烟碱乙酰胆碱受体的正变构调节剂，这种正变构调节剂具有增加烟碱受体激动剂功效的能力。

3. 发明申请

US20080227791A1 Piperidin-4-Yl-Pyridazin-3-Ylamine Derivatives as Fast Dissociating Dopamine 2 Receptor Antagonists 有权
标题翻译：哌啶-4-Y1-哒嗪-3-胺衍生物作为快速分离多巴胺2受体拮抗剂
公开(公告)号：US20080227791A1
公开(公告)日：2008-09-18
申请号：US12091219
申请日：2006-10-24
申请人： Marcel Frans Leopold De Bruyn , Gregor James Macdonald , Ludo Edmond Josephine Kennis , Xavier Jean Michel Langlois , Frans Alfons Maria Van Den Keybus , Yves Emiel Maria Van Roosbroeck
发明人： Marcel Frans Leopold De Bruyn , Gregor James Macdonald , Ludo Edmond Josephine Kennis , Xavier Jean Michel Langlois , Frans Alfons Maria Van Den Keybus , Yves Emiel Maria Van Roosbroeck
IPC分类号： A61K31/501 , C07D401/12
CPC分类号： C07D401/12 , A61K31/501 , C07D409/14
摘要： The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
摘要翻译：本发明涉及快速解离多巴胺2受体拮抗剂，制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物。该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。

4. 发明授权

US08940743B2 Piperidin-4-yl-pyridazin-3-ylamine derivatives as fast dissociating dopamine 2 receptor antagonists 有权
标题翻译：哌啶-4-基 - 哒嗪-3-基胺衍生物作为快速解离的多巴胺2受体拮抗剂
公开(公告)号：US08940743B2
公开(公告)日：2015-01-27
申请号：US12091219
申请日：2006-10-24
申请人： Marcel Frans Leopold De Bruyn , Gregor James MacDonald , Ludo Edmond Josephine Kennis , Xavier Jean Michel Langlois , Frans Alfons Maria Van Den Keybus , Yves Emiel Maria Van Roosbroeck
发明人： Marcel Frans Leopold De Bruyn , Gregor James MacDonald , Ludo Edmond Josephine Kennis , Xavier Jean Michel Langlois , Frans Alfons Maria Van Den Keybus , Yves Emiel Maria Van Roosbroeck
IPC分类号： C07D401/12 , C07D401/14 , A61K31/501 , C07D409/14 , C07D491/113 , C07D211/44 , C07D211/58 , C07D237/20 , A61P25/18
CPC分类号： C07D401/12 , A61K31/501 , C07D409/14
摘要： The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
摘要翻译：本发明涉及快速解离多巴胺2受体拮抗剂，制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物。该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。

5. 发明授权

US08440701B2 Trisubstituted 1,2,4 triazoles 有权
标题翻译：三取代的1,2,4-三唑
公开(公告)号：US08440701B2
公开(公告)日：2013-05-14
申请号：US12738763
申请日：2008-10-15
申请人： Johannes Wilhelmus John F. Thuring , Theodorus Dinklo , Anne Simone Josephine Lesage , Marcel Frans Leopold De Bruyn , Wei Zhuang
发明人： Johannes Wilhelmus John F. Thuring , Theodorus Dinklo , Anne Simone Josephine Lesage , Marcel Frans Leopold De Bruyn , Wei Zhuang
IPC分类号： A61K31/4439 , C07D401/04
CPC分类号： C07D401/04
摘要： The present invention relates to substituted 1-(alkyl)-3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to potent positive allosteric modulators of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.
摘要翻译：本发明涉及取代的1-（烷基）-3-苯胺-5-芳基三唑衍生物及其类似物或药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途，根据式（I）。本发明特别涉及具有增加烟碱受体激动剂功效的烟碱型乙酰胆碱受体的有效的正变构调节剂。

6. 发明申请

US20100216846A1 TRISUBSTITUTED 1,2,4 TRIAZOLES 有权
标题翻译：检测1,2,4三唑
公开(公告)号：US20100216846A1
公开(公告)日：2010-08-26
申请号：US12738763
申请日：2008-10-15
申请人： Johannes Wilhelmus John F. Thuring , Theodorus Dinklo , Anne Simone Josephine Lesage , Marcel Frans Leopold De Bruyn , Wei Zhuang
发明人： Johannes Wilhelmus John F. Thuring , Theodorus Dinklo , Anne Simone Josephine Lesage , Marcel Frans Leopold De Bruyn , Wei Zhuang
IPC分类号： A61K31/4439 , C07D401/04 , A61P25/00
CPC分类号： C07D401/04
摘要： The present invention relates to substituted 1-(alkyl)-3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to potent positive allosteric modulators of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.
摘要翻译：本发明涉及取代的1-（烷基）-3-苯胺-5-芳基三唑衍生物及其类似物或药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途，根据式（I）。本发明特别涉及具有增加烟碱受体激动剂功效的烟碱型乙酰胆碱受体的有效的正变构调节剂。

7. 发明申请

US20170022181A1 FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：快速分解多巴胺2受体拮抗剂
公开(公告)号：US20170022181A1
公开(公告)日：2017-01-26
申请号：US15264185
申请日：2016-09-13
申请人： Marcel Frans Leopold De Bruyn , Gregor James Macdonald , Ludo Edmond Josephine Kennis , Xavier Jean Michel Langlois , Frans Alfons Maria Van den Keytus , Yves Emiel Maria Van Roosbroeck
发明人： Marcel Frans Leopold De Bruyn , Gregor James Macdonald , Ludo Edmond Josephine Kennis , Xavier Jean Michel Langlois , Frans Alfons Maria Van den Keytus , Yves Emiel Maria Van Roosbroeck
IPC分类号： C07D401/12 , C07D409/14
CPC分类号： C07D401/12 , A61K31/501 , C07D409/14
摘要： The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
摘要翻译：本发明涉及快速解离多巴胺2受体拮抗剂，制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物。该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。

8. 发明授权

US06864273B1 Aminoalkyl substituted (benzodioxan, benzofuran or benzopyran) derivatives 有权
标题翻译：氨基烷基取代的（苯并二恶烷，苯并呋喃或苯并吡喃）衍生物
公开(公告)号：US06864273B1
公开(公告)日：2005-03-08
申请号：US09980452
申请日：2000-05-23
申请人： Kristof Van Emelen , Marcel Frans Leopold De Bruyn
发明人： Kristof Van Emelen , Marcel Frans Leopold De Bruyn
IPC分类号： A61K31/4164 , A61K31/4178 , A61K31/513 , A61P1/14 , A61P9/00 , A61P9/08 , C07D405/12 , C07D417/12
CPC分类号： C07D405/12 , C07D417/12
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R6 is hydrogen or phenylmethyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.
摘要翻译：本发明涉及式（I）化合物，其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，其中-Z 1 -Z 2 - 是二价基团; R 1，R 2和R 3各自独立地选自氢，C 1-6烷基，羟基，卤素等; 或当R 1和R 2在相邻的碳原子上时，R 1和R 2一起可以形成式的二价基团; Alk 1和Alk 2是任选取代的C 1-6烷二基; R 6是氢或苯基甲基; R 5是脯氨酸的基团，n是1或2; p <1>为0，p <2为1或2; 或p <1>为1或2，p <2为0; X是氧，硫或= NR 9; Y是氧或硫; R 7是氢，C 1-6烷基，C 3-6环烷基，苯基或苯基甲基; R 8是C 1-6烷基，C 3-6环烷基苯基或苯基甲基; R 9是氰基，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基羰基或氨基羰基; R 10是氢或C 1-6烷基; 而Q是二价基团。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与减退的放松有关的病症。

9. 发明授权

US07423048B2 Compounds for treating fundic disaccomodation 有权
公开(公告)号：US07423048B2
公开(公告)日：2008-09-09
申请号：US11355402
申请日：2006-02-16
申请人： Kristol Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encamacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
发明人： Kristol Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encamacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
IPC分类号： C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D403/06 , C07D403/14 , A61K31/436 , A61P1/14
CPC分类号： C07D411/04 , C07D491/04
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a1═a2-a3═a4- is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH═; -Z1-Z2- is a bivalent radical; -A- is a bivalent radical of formula —N(R6)-Alk2- or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to disturbed fundic accomodation.

10. 发明授权

US06495547B1 (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties 有权
标题翻译：（苯并二恶烷，苯并呋喃或苯并吡喃）衍生物
公开(公告)号：US06495547B1
公开(公告)日：2002-12-17
申请号：US09641485
申请日：2000-08-18
申请人： Piet Tom Bert Paul Wigerinck , Wim Gaston Verschueren , Marc Francis Josephine Schroven , Marcel Frans Leopold De Bruyn
发明人： Piet Tom Bert Paul Wigerinck , Wim Gaston Verschueren , Marc Francis Josephine Schroven , Marcel Frans Leopold De Bruyn
IPC分类号： C07D40514
CPC分类号： C07D405/12 , C07D405/14
摘要： The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6—Alk2— (b-1), or —Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen. sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.
摘要翻译：式（I）化合物的本发明是其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，其中Alk1是任选被羟基，C 1-4烷氧基或C 1-4烷基羰基氧基取代的C 1-6烷二基; -Z1-Z2-是二价基团; R 1，R 2和R 3各自独立地选自氢，C 1-6烷基，羟基，卤素等; 或当R 1和R 2在相邻碳原子上时，R 1和R 2一起可以形成二价基; R4是氢或C1-6烷基; A是式-NR6-Alk2-（b-1）或-N-哌啶基 - （CH2）m（b-2）的二价基团，其中m是0或1; R5是一种基团，其中n是1或2; p1为0，p2为1或2; 或p1为1或2，p2为0; X是氧。硫或= NR9; Y是氧或硫; R7是氢，C1-6烷基，C3-6环烷基，苯基或苯基甲基; R8是C1-6烷基，C3-6环烷基苯基或苯基甲基; R9是氰基，C1-6烷基，C3-6环烷基，C1-6烷氧基羰基或氨基羰基; R 10是氢或C 1-6烷基; 而Q是二价基团。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与减退的放松有关的病症。

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