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1. 发明授权

US07563903B2 Acylaminothiazole derivatives, their preparation and their therapeutic use 失效
标题翻译：酰氨基噻唑衍生物，其制备及其治疗用途
公开(公告)号：US07563903B2
公开(公告)日：2009-07-21
申请号：US11186507
申请日：2005-07-21
申请人： Pierre Despeyroux , Daniel Frehel , Bruno Schoentjes , Viviane Van Dorsselaer
发明人： Pierre Despeyroux , Daniel Frehel , Bruno Schoentjes , Viviane Van Dorsselaer
IPC分类号： A61K31/426 , C07D277/46
CPC分类号： C07D417/12 , C07D277/46
摘要： Compound corresponding to the general formula (I): in which, X represents an oxygen or sulphur atom; R1 represents a C1-10 alkyl group optionally substituted, a C3-7 cycloalkyl, thienyl, pyridinyl or pyrimidinyl group; the thienyl groups being optionally substituted; the phenyl group being optionally substituted; R2 represents a C1-6 alkyl group optionally substituted, a C3-7 cycloalkyl, piperidinyl, phenyl or pyridinyl group; the C3-7 cycloalkyl and piperidinyl groups being optionally substituted; the phenyl and pyridinyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-6 alkyl group optionally substituted with a C3-7 cycloalkyl group; R4 represents a hydrogen atom or a C1-6 alkyl group; R5 and R5′ represent, independently of each other, a hydrogen or halogen atom, a hydroxyl or C1-3 alkyl group; or R5 and R5′ form together an oxo or oxime group such as: where R7 represents a hydrogen atom or a C1-3 alkyl; n represents an integer ranging from 0 to 3; and R6 represents, independently of each other when n=2 or 3, a hydrogen or halogen atom, a hydroxyl, C1-3 alkyl, C1-3 alkoxy, C1-3 fluoroalkyl or C1-3 fluoroalkoxy group; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. therapeutic application.
摘要翻译：对应于通式（I）的化合物：其中X表示氧或硫原子; R 1表示任选取代的C 1-10烷基，C 3-7环烷基，噻吩基，吡啶基或嘧啶基; 噻吩基任选被取代; 苯基任选被取代; R 2表示任选取代的C 1-6烷基，C 3-7环烷基，哌啶基，苯基或吡啶基; C3-7环烷基和哌啶基任选被取代; 苯基和吡啶基任选被取代; R3表示氢原子或任选被C 3-7环烷基取代的C 1-6烷基; R4表示氢原子或C1-6烷基; R5和R5'彼此独立地表示氢或卤素原子，羟基或C1-3烷基; 或R 5和R 5'一起形成氧基或肟基，例如：其中R 7表示氢原子或C 1-3烷基; n表示0〜3的整数，当n = 2或3时，R 6表示独立地为氢或卤原子，羟基，C 1-3烷基，C 1-3烷氧基，C 1-3氟烷基或C 1-3氟烷氧基; 以碱的形式，与酸的加成盐，水合物或溶剂合物的治疗应用。

2. 发明申请

US20060052426A1 Acylaminothiazole derivatives, their preparation and their therapeutic use 失效
标题翻译：酰氨基噻唑衍生物，其制备及其治疗用途
公开(公告)号：US20060052426A1
公开(公告)日：2006-03-09
申请号：US11186507
申请日：2005-07-21
申请人： Pierre Despeyroux , Daniel Frehel , Bruno Schoentjes , Viviane Van Dorsselaer
发明人： Pierre Despeyroux , Daniel Frehel , Bruno Schoentjes , Viviane Van Dorsselaer
IPC分类号： C07D277/18 , A61K31/426
CPC分类号： C07D417/12 , C07D277/46
摘要： Compound corresponding to the general formula (I): in which, X represents an oxygen or sulphur atom; R1 represents a C1-10 alkyl group optionally substituted, a C3-7 cycloalkyl, thienyl, pyridinyl or pyrimidinyl group; the thienyl groups being optionally substituted; the phenyl group being optionally substituted; R2 represents a C1-6 alkyl group optionally substituted, a C3-7 cycloalkyl, piperidinyl, phenyl or pyridinyl group; the C3-7 cycloalkyl and piperidinyl groups being optionally substituted; the phenyl and pyridinyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-6 alkyl group optionally substituted with a C3-7 cycloalkyl group; R4 represents a hydrogen atom or a C1-6 alkyl group; R5 and R5′ represent, independently of each other, a hydrogen or halogen atom, a hydroxyl or C1-3 alkyl group; or R5 and R5′ form together an oxo or oxime group such as: where R7 represents a hydrogen atom or a C1-3 alkyl; n represents an integer ranging from 0 to 3; and R6 represents, independently of each other when n=2 or 3, a hydrogen or halogen atom, a hydroxyl, C1-3 alkyl, C1-3 alkoxy, C1-3 fluoroalkyl or C1-3 fluoroalkoxy group; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. therapeutic application.
摘要翻译：对应于通式（I）的化合物：

3. 发明授权

US07879889B2 Therapeutic use of acylaminothiazole derivatives 失效
标题翻译：酰氨基噻唑衍生物的治疗用途
公开(公告)号：US07879889B2
公开(公告)日：2011-02-01
申请号：US12488658
申请日：2009-06-22
申请人： Pierre Despey-Roux , Daniel Frehel , Bruno Schoentjes , Viviane Van Dorsselaer
发明人： Pierre Despey-Roux , Daniel Frehel , Bruno Schoentjes , Viviane Van Dorsselaer
IPC分类号： A61K31/426
CPC分类号： C07D417/12 , C07D277/46
摘要： The present invention discloses and claims therapeutic uses of a compound corresponding to the general formula (I): Wherein, X, R1, R2, R3, R4, R5, R5′, R6 and n are as described herein.
摘要翻译：本发明公开并要求对应于通式（I）的化合物的治疗用途：其中X，R 1，R 2，R 3，R 4，R 5，R 5'，R 6和n如本文所述。

4. 发明授权

US07795289B2 Use of acylaminothiazole derivatives as therapeutic agents 失效
标题翻译：酰基氨基噻唑衍生物作为治疗剂的用途
公开(公告)号：US07795289B2
公开(公告)日：2010-09-14
申请号：US11859443
申请日：2007-09-21
申请人： Sylvie Baltzer , Bruno Schoentjes , Viviane Van Dorsselaer
发明人： Sylvie Baltzer , Bruno Schoentjes , Viviane Van Dorsselaer
IPC分类号： A61K31/426
CPC分类号： C07D417/12 , C07D277/56
摘要： This invention discloses and claims a method of treatment of a disease as defined herein using a compound conforming to the general formula (I): Wherein R1, R2, R′2, R3, R4 and R5 are as described herein. Specifically, the compounds of the present invention exhibit an inhibitory effect on the production of β-amyloid peptide (β-A4) by inhibition of gamma protease. Therefore, the compounds of the present invention are useful in the treatment of pathologies such as senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy and/or cerebrovascular disorders.
摘要翻译：本发明公开并要求使用符合通式（I）的化合物治疗本文定义的疾病的方法：其中R 1，R 2，R'2，R 3，R 4和R 5如本文所述。具体地，本发明的化合物通过抑制γ蛋白酶表现出对β-淀粉样蛋白肽（＆bgr; -A4）的产生的抑制作用。因此，本发明的化合物可用于治疗老年性痴呆，阿尔茨海默氏病，唐氏综合征，帕金森病，淀粉样血管病和/或脑血管障碍等病态。

5. 发明授权

US07291636B2 Acylaminothiazole derivatives, preparation and therapeutic use thereof 失效
标题翻译：酰氨基噻唑衍生物，其制备和治疗用途
公开(公告)号：US07291636B2
公开(公告)日：2007-11-06
申请号：US11035803
申请日：2005-01-14
申请人： Sylvie Baltzer , Bruno Schoentjes , Viviane Van Dorsselaer
发明人： Sylvie Baltzer , Bruno Schoentjes , Viviane Van Dorsselaer
IPC分类号： A61K31/426 , C07D277/46
CPC分类号： C07D417/12 , C07D277/56
摘要： This invention discloses and claims a compound conforming to the general formula (I): Wherein R1, R2, R′2, R3, R4 and R5 are as described herein. The compounds of the present invention exhibit an inhibitory effect on the production of β-amyloid peptide (β-A4) by inhibition of gamma protease. Therefore, the compounds of the present invention are useful in the treatment of pathologies such as senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy and/or cerebrovascular disorders.
摘要翻译：本发明公开了一种符合通式（I）的化合物：其中R 1，R 2，R 2，R 2， R 3，R 4和R 5如本文所述。本发明的化合物通过抑制γ蛋白酶对β-淀粉样蛋白肽（β-A4）的产生具有抑制作用。因此，本发明的化合物可用于治疗老年性痴呆，阿尔茨海默氏病，唐氏综合征，帕金森病，淀粉样血管病和/或脑血管障碍等病态。

6. 发明申请

US20050182104A1 Acylaminothiazole derivatives, preparation and therapeutic use thereof 失效
标题翻译：酰氨基噻唑衍生物，其制备和治疗用途
公开(公告)号：US20050182104A1
公开(公告)日：2005-08-18
申请号：US11035803
申请日：2005-01-14
申请人： Sylvie Balter , Bruno Schoentjes , Viviane Van Dorsselaer
发明人： Sylvie Balter , Bruno Schoentjes , Viviane Van Dorsselaer
IPC分类号： C07D277/20 , A61K31/426 , A61K31/454 , A61K31/5377 , A61P7/00 , A61P9/10 , A61P25/16 , A61P25/28 , C07D277/46 , C07D277/56 , C07D417/12 , A61K31/4439 , C07D417/02
CPC分类号： C07D417/12 , C07D277/56
摘要： This invention discloses and claims a compound conforming to the general formula (I): Wherein R1, R2, R′2, R3, R4 and R5 are as described herein. The compounds of the present invention exhibit an inhibitory effect on the production of β-amyloid peptide (β-A4) by inhibition of gamma protease. Therefore, the compounds of the present invention are useful in the treatment of pathologies such as senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy and/or cerebrovascular disorders.
摘要翻译：本发明公开了一种符合通式（I）的化合物：其中R 1，R 2，R 2，R 2， R 3，R 4和R 5如本文所述。本发明的化合物通过抑制γ蛋白酶对β-淀粉样蛋白肽（β-A4）的产生具有抑制作用。因此，本发明的化合物可用于治疗老年性痴呆，阿尔茨海默氏病，唐氏综合征，帕金森病，淀粉样血管病和/或脑血管障碍等病态。

7. 发明授权

US08703973B2 Benzocycloheptane and benzoxepine derivatives 有权
标题翻译：苯并环庚烷和苯并恶庚因衍生物
公开(公告)号：US08703973B2
公开(公告)日：2014-04-22
申请号：US13597293
申请日：2012-08-29
申请人： Bruno Schoentjes , Alain Philippe Poncelet , Julien Georges Pierre-Olivier Doyon , Joannes Theodorus Maria Linders , Lieven Meerpoel , Luc August Laurentius Ver Donck
发明人： Bruno Schoentjes , Alain Philippe Poncelet , Julien Georges Pierre-Olivier Doyon , Joannes Theodorus Maria Linders , Lieven Meerpoel , Luc August Laurentius Ver Donck
IPC分类号： C07D305/00 , C07C211/00
CPC分类号： C07C215/42 , C07C35/52 , C07C43/192 , C07C215/64 , C07C217/08 , C07C217/74 , C07C2602/12 , C07D207/06 , C07D213/53 , C07D213/65 , C07D215/14 , C07D239/26 , C07D295/092 , C07D295/096 , C07D295/16 , C07D313/08 , C07D317/58 , C07D405/04 , C07D407/04
摘要： The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.
摘要翻译：本发明涉及包括其任何立体化学异构体形式的式（I）化合物，其中取代基如说明书和权利要求中所定义; 其N-氧化物，其药学上可接受的盐或其溶剂合物; 条件是该化合物不是其或其药学上可接受的盐。要求保护的化合物可用于治疗通过激活GHS1A-r受体而影响，介导或促进的疾病的治疗。本发明还涉及其药物组合物及其制备方法。

8. 发明申请

US20100292228A1 SUBSTITUTED OXA-DIAZA-SPIRO-[5.5]-UNDECANONE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 失效
标题翻译：取代的OXA-DIAZA-SPIRO- [5.5] - 泛醌衍生物及其作为神经营养因子拮抗剂的用途
公开(公告)号：US20100292228A1
公开(公告)日：2010-11-18
申请号：US11913890
申请日：2006-03-03
申请人： Frans Eduard Jenssens , Sophie Coupa , Alain Philippe Poncelet , Bruno Schoentjes
发明人： Frans Eduard Jenssens , Sophie Coupa , Alain Philippe Poncelet , Bruno Schoentjes
IPC分类号： A61K31/537 , C07D498/10 , A61P25/18 , A61P25/24
CPC分类号： C07D498/10 , B82Y5/00
摘要： This invention concerns substituted oxa-diaza-spiro-[5.5]-undecanone derivatives having neurokinin antagonistic activity, in particular an NK1 antagonistic activity, an NK3 antagonistic activity, a combined NK1/NK2 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.
摘要翻译：本发明涉及具有神经激肽拮抗活性的取代的氧杂 - 二氮杂螺 - [5.5] - 十一烷酮衍生物，特别是NK1拮抗活性，NK3拮抗活性，组合NK1 / NK2拮抗活性和组合NK1 / NK2 / NK3拮抗活性，它们的制剂，包含它们的组合物及其作为药物的用途，特别是用于治疗和/或预防精神分裂症，呕吐，焦虑和抑郁，肠易激综合征（IBS），昼夜节律紊乱，先兆子痫，伤害感受，疼痛，特别是内脏和神经性疼痛，胰腺炎，神经源性炎症，哮喘，慢性阻塞性肺病（COPD）和排尿障碍如尿失禁。根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其前药，其中所有取代基定义为在权利要求1中。

9. 发明申请

US20090149493A1 INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 有权
标题翻译： MDM2和P53之间相互作用的抑制剂
公开(公告)号：US20090149493A1
公开(公告)日：2009-06-11
申请号：US12293545
申请日：2007-03-19
申请人： Jean Fernand Armand Lacrampe , Christophe Meyer , Bruno Schoentjes , Delphine Yvonne Raymonde Lardeau , Alain Philippe Poncelet , Luc Van Hijfte
发明人： Jean Fernand Armand Lacrampe , Christophe Meyer , Bruno Schoentjes , Delphine Yvonne Raymonde Lardeau , Alain Philippe Poncelet , Luc Van Hijfte
IPC分类号： A61K31/4439 , C07D405/12 , C07D471/04 , C07D401/12 , A61P35/00 , C07D495/04 , A61K31/443 , A61K31/437
CPC分类号： C07D405/12 , C07D401/12 , C07D471/04
摘要： The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, A and Z have defined meanings.
摘要翻译：本发明提供式（I）化合物，其作为p53-MDM2相互作用的抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中n，m，p，s，t，R 1，R 2， A和Z定义含义。

10. 发明申请

US20070232636A1 Substituted Diaza-Spiro-[5.5]-Undecane Derivaties and Their Use as Neurokinin Antagonists 失效
标题翻译：取代的Diaza-Spiro- [5.5] - 十二烷衍生物及其作为神经激肽拮抗剂的用途
公开(公告)号：US20070232636A1
公开(公告)日：2007-10-04
申请号：US11547889
申请日：2005-04-04
申请人： Frans Janssens , Bruno Schoentjes , Sophie Coupa , Alain Poncelet , Yvan Simonnet
发明人： Frans Janssens , Bruno Schoentjes , Sophie Coupa , Alain Poncelet , Yvan Simonnet
IPC分类号： A61K31/438 , C07D215/00
CPC分类号： C07D471/10 , C07D519/00
摘要： This invention concerns substituted diaza-spiro-[5.5]-undecane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, COPD and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
摘要翻译：本发明涉及具有神经激肽拮抗活性，特别是NK 1拮抗活性的组合NK 1 / NK 2的取代的二氮 - 螺 - [5.5] - 十一烷衍生物组合的NK 1 / NK 3拮抗活性和组合的NK 1 / NK 2拮抗活性，拮抗活性，它们的制备，包含它们的组合物及其作为药物的用途，特别是用于治疗和/或预防精神分裂症，呕吐，焦虑和抑郁症，肠易激综合征（肠易激综合征 IBS），昼夜节律紊乱，先兆子痫，伤害感受，疼痛，特别是内脏和神经性疼痛，胰腺炎，神经源性炎症，哮喘，COPD和排尿障碍如尿失禁。根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其前药，其中所有取代基定义为在权利要求1中。

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