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1. 发明申请

US20070197601A1 Use of N-[Phenyl(piperidin-2-yl)methyl]benzamide derivatives in therapy 审中-公开
标题翻译： N- [苯基（哌啶-2-基）甲基]苯甲酰胺衍生物在治疗中的应用
公开(公告)号：US20070197601A1
公开(公告)日：2007-08-23
申请号：US11695912
申请日：2007-04-03
申请人： Gihad DARGAZANLI , Genevieve ESTENNE-BOUHTOU , Pascale MAGAT , Benoit MARABOUT , Florence MEDAISKO , Pierre ROGER , Mireille SEVRIN , Corinne VERONIQUE
发明人： Gihad DARGAZANLI , Genevieve ESTENNE-BOUHTOU , Pascale MAGAT , Benoit MARABOUT , Florence MEDAISKO , Pierre ROGER , Mireille SEVRIN , Corinne VERONIQUE
IPC分类号： A61K31/445
CPC分类号： C07D211/26
摘要： The present invention discloses and claims therapeutic use of a series of compounds of general formula (I) in which A, X and R2 are as described herein. Specifically, the compounds of formula (I) exhibit a particular activity as specific inhibitors of the glycine transporters glyt1 and/or glty2.
摘要翻译：本发明公开并要求治疗使用一系列通式（I）的化合物，其中A，X和R 2-2如本文所述。具体地，式（I）化合物作为甘氨酸转运蛋白glyt1和/或glty2的特异性抑制剂具有特定的活性。

2. 发明申请

US20060223885A1 Derivatives of N-phenyl (piperidine-2-yl) methyl benzamide, preparation method thereof and applications of same in therapeutics 失效
标题翻译： N-苯基（哌啶-2-基）甲基苯甲酰胺的衍生物及其制备方法及其在治疗中的应用
公开(公告)号：US20060223885A1
公开(公告)日：2006-10-05
申请号：US11405169
申请日：2006-04-17
申请人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Pascale Magat
发明人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Pascale Magat
IPC分类号： A61K31/27
CPC分类号： C07D403/12 , C07D401/12 , C07D409/12
摘要： Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine. Moreover, the compounds of the invention may be used for treating painful muscle contracture in rheumatology and in acute spinal pathology; for treating spastic contractures of medullary or cerebral origin; for the symptomatic treatment of acute and subacute pain of light to moderate intensity; for treating intense and/or chronic pain, neurogenic pain and intractable pain; for treating Parkinson's disease and Parkinson-like symptoms of neurodegenerative origin or induced by neuroleptics; for treating partial primary and secondary generalized epilepsy of simple or complex symptomology, mixed forms and other epileptic syndromes in addition to another antiepileptic treatment, or in monotherapy, for the treatment of sleep apnea, and for neuroprotection.
摘要翻译：本文定义的式（I）化合物可用于治疗与痴呆，精神病，特别是精神分裂症（缺陷形式和生产形式）和由精神安定药物诱发的急性或慢性锥体外系症状相关的行为障碍; 用于治疗各种形式的焦虑，恐慌发作，恐惧症和强迫性强迫症; 用于治疗各种形式的抑郁症，包括精神病性抑郁症; 用于治疗酒精滥用或酒精断奶引起的疾病，性行为障碍，进食障碍和用于治疗偏头痛。此外，本发明的化合物可用于治疗风湿病和急性脊髓病变中的疼痛性肌肉挛缩; 用于治疗髓质或脑源性痉挛性挛缩; 用于轻度至中度强度的急性和亚急性疼痛的对症治疗; 用于治疗强烈和/或慢性疼痛，神经源性疼痛和难治性疼痛; 用于治疗帕金森病和神经变性起源的帕金森样症状或由精神安定药诱导; 用于治疗单纯或复杂症状，混合形式和其他癫痫综合征的部分原发性和继发性全身性癫痫以及另一种抗癫痫治疗或单一疗法，用于治疗睡眠呼吸暂停和神经保护。

3. 发明申请

US20050159450A1 Derivative of n-[phenyl(piperidin-2-yl)methyl]benzamide, the preparation method thereof and application of same in therapeutics 失效
标题翻译： n- [苯基（哌啶-2-基）甲基]苯甲酰胺的衍生物及其制备方法及其在治疗中的应用
公开(公告)号：US20050159450A1
公开(公告)日：2005-07-21
申请号：US10511886
申请日：2003-04-17
申请人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Pascale Magat , Benoit Marabout , Florence Medaisko , Pierre Roger , Mireille Sevrin , Corinne Veronique
发明人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Pascale Magat , Benoit Marabout , Florence Medaisko , Pierre Roger , Mireille Sevrin , Corinne Veronique
IPC分类号： A61K20060101 , A61K31/445 , A61K31/4458 , A61K31/452 , A61P20060101 , A61P1/00 , A61P11/16 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/26 , C07D211/32 , C07D211/94
CPC分类号： C07D211/26
摘要： Compound of general formula (I) in which A represents either a group of formula N—R1 in which R1 represents a hydrogen atom, an alkyl group, a cycloalkyl group, a phenylalkyl group, an alkenyl group or an alkynyl group, or a group of formula N+(O−)R1 in which R1 is as defined above, or alternatively a group of formula N+(R′)R1 in which R′ represents an alkyl group and R1 is as defined above, X represents a hydrogen atom or one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, R2 represents a hydrogen atom, one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, amino groups of formula NR3R4 in which R3 and R4 each represent a hydrogen atom or an alkyl group, or form with the nitrogen atom carrying them a pyrrolidine, piperidine or morpholine ring, or an optionally substituted phenyl group. Application in therapy.
摘要翻译：通式（I）的化合物，其中A表示式NR 1的基团，其中R 1表示氢原子，烷基，环烷基，苯基烷基，烯基或炔基，或其中R 1为低级烷基的基团，其中R 1为N（O） > 1 如上所定义，或者可选地，其中R'表示烷基的式N +，（R'）R 1' 如上定义，X表示氢原子或一个或多个选自卤素原子和三氟甲基，烷基和烷氧基的取代基，R 2表示氢原子，一个或多个选自卤素原子和三氟甲基，烷基和烷氧基的更多取代基，式NR 3 R 4的氨基，其中R 3和R“ 或者分别代表氢原子或烷基，或与氮原子一起带有吡咯烷，哌啶或吗啉环的形式，或 n任选取代的苯基。应用于治疗。

4. 发明申请

US20100022548A1 USE OF N-HETEROCYCLYLMETHYLBENZAMIDES IN THERAPEUTICS 有权
标题翻译： N-环己基甲基苯并噻唑在治疗中的应用
公开(公告)号：US20100022548A1
公开(公告)日：2010-01-28
申请号：US12573470
申请日：2009-10-05
申请人： Gihad DARGAZANLI , Genevieve ESTENNE-BOUHTOU , Pascale MAGAT , Benoit MARABOUT , Pierre ROGER
发明人： Gihad DARGAZANLI , Genevieve ESTENNE-BOUHTOU , Pascale MAGAT , Benoit MARABOUT , Pierre ROGER
IPC分类号： A61K31/4995 , A61K31/439 , A61P25/16 , A61P25/20 , A61P25/08 , A61P29/00
CPC分类号： C07D471/08 , C07D487/08
摘要： The invention relates to use of compositions in therapeutics containing a compound having general formula (I): Wherein R, R1, R2, X and n are as described herein.
摘要翻译：本发明涉及组合物在含有通式（I）的化合物的治疗剂中的用途：其中R，R 1，R 2，X和n如本文所述。

5. 发明申请

US20080070941A1 DERIVATIVES OF N-HETEROCYCLYLMETHYLBENZAMIDES, PREPARATION METHOD THEREOF AND APPLICATION OF SAME IN THERAPEUTICS 有权
标题翻译： N-环己基甲基苯并噻唑的衍生物，其制备方法及其在治疗中的应用
公开(公告)号：US20080070941A1
公开(公告)日：2008-03-20
申请号：US11858436
申请日：2007-09-20
申请人： Gihad DARGAZANLI , Genevieve ESTENNE-BOUHTOU , Pascale MAGAT , Benoit MARABOUT , Pierre ROGER
发明人： Gihad DARGAZANLI , Genevieve ESTENNE-BOUHTOU , Pascale MAGAT , Benoit MARABOUT , Pierre ROGER
IPC分类号： A61K31/439 , A61K31/4995 , A61P25/00
CPC分类号： C07D471/08 , C07D487/08
摘要： The invention relates to compositions comprising a compound having general formula (I): Wherein R, R1, R2, X and n are as described herein. Also disclosed and claimed in certain of the embodiments herein are the methods of preparation of compound of formula (I) and its use in therapeutics.
摘要翻译：本发明涉及包含具有通式（I）的化合物的组合物：其中R，R 1，R 2，X和n如本文所述。在本文的某些实施方案中还公开和要求保护的是制备式（I）化合物及其在治疗中的用途的方法。

6. 发明申请

US20100234424A1 DERIVATIVES OF N-PHENYL(PIPERIDINE-2-YL) METHYL BENZAMIDE PREPARATION METHOD THEREOF AND APPLICATIONS OF SAME IN THERAPEUTICS 审中-公开
标题翻译：哌嗪（哌啶-2-基）甲基苯甲酰胺的制备方法及其在治疗中的应用
公开(公告)号：US20100234424A1
公开(公告)日：2010-09-16
申请号：US12784007
申请日：2010-05-20
申请人： Gihad DARGAZANLI , Genevieve ESTENNE-BOUHTOU , Pascale MAGAT
发明人： Gihad DARGAZANLI , Genevieve ESTENNE-BOUHTOU , Pascale MAGAT
IPC分类号： C07D401/12 , A61P25/32 , A61K31/4545 , A61P25/28 , A61P25/00 , A61K31/445 , C07D211/06 , A61K31/4535 , A61P25/08 , A61K31/454 , A61K31/47 , C07D215/14 , A61P25/24 , A61P25/06 , C07D409/12 , A61P25/18
CPC分类号： C07D403/12 , C07D401/12 , C07D409/12
摘要： Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine. Moreover, the compounds of the invention may be used for treating painful muscle contracture in rheumatology and in acute spinal pathology; for treating spastic contractures of medullary or cerebral origin; for the symptomatic treatment of acute and subacute pain of light to moderate intensity; for treating intense and/or chronic pain, neurogenic pain and intractable pain; for treating Parkinson's disease and Parkinson-like symptoms of neurodegenerative origin or induced by neuroleptics; for treating partial primary and secondary generalized epilepsy of simple or complex symptomology, mixed forms and other epileptic syndromes in addition to another antiepileptic treatment, or in monotherapy, for the treatment of sleep apnea, and for neuroprotection.
摘要翻译：本文定义的式（I）化合物可用于治疗与痴呆，精神病，特别是精神分裂症（缺陷形式和生产形式）和由精神安定药物诱发的急性或慢性锥体外系症状相关的行为障碍; 用于治疗各种形式的焦虑，恐慌发作，恐惧症和强迫性强迫症; 用于治疗各种形式的抑郁症，包括精神病性抑郁症; 用于治疗酒精滥用或酒精断奶引起的疾病，性行为障碍，进食障碍和用于治疗偏头痛。此外，本发明的化合物可用于治疗风湿病和急性脊髓病变中的疼痛性肌肉挛缩; 用于治疗髓质或脑源性痉挛性挛缩; 用于轻度至中度强度的急性和亚急性疼痛的对症治疗; 用于治疗强烈和/或慢性疼痛，神经源性疼痛和难治性疼痛; 用于治疗帕金森病和神经变性起源的帕金森样症状或由精神安定药诱导; 用于治疗单纯或复杂症状，混合形式和其他癫痫综合征的部分原发性和继发性全身性癫痫以及另一种抗癫痫治疗或单一疗法，用于治疗睡眠呼吸暂停和神经保护。

7. 发明授权

US07619089B2 Derivatives of N-heterocyclylmethylbenzamides, preparation method thereof and application of same in therapeutics 有权
标题翻译： N-杂环基甲基苯甲酰胺的衍生物，其制备方法及其在治疗中的应用
公开(公告)号：US07619089B2
公开(公告)日：2009-11-17
申请号：US11858436
申请日：2007-09-20
申请人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Pascale Magat , Benoit Marabout , Pierre Roger
发明人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Pascale Magat , Benoit Marabout , Pierre Roger
IPC分类号： C07D453/02 , A01N43/90
CPC分类号： C07D471/08 , C07D487/08
摘要： The invention relates to compositions comprising a compound having general formula (I): Wherein R, R1, R2, X and n are as described herein. Also disclosed and claimed in certain of the embodiments herein are the methods of preparation of compound of formula (I) and its use in therapeutics.
摘要翻译：本发明涉及包含具有通式（I）的化合物的组合物：其中R，R 1，R 2，X和n如本文所述。在本文的某些实施方案中还公开和要求保护的是制备式（I）化合物及其在治疗中的用途的方法。

8. 发明授权

US07326722B2 N-[Phenyl(piperidin-2-yl)methyl]benzamide derivatives, their preparation and their application in therapy 失效
标题翻译： N- [苯基（哌啶-2-基）甲基]苯甲酰胺衍生物，其制备及其在治疗中的应用
公开(公告)号：US07326722B2
公开(公告)日：2008-02-05
申请号：US10511886
申请日：2003-04-17
申请人： Gihad Dargazanli , Geneviève Estenne-Bouhtou , Pascale Magat , Benoît Marabout , Florence Medaisko , Pierre Roger , Mireille Sevrin , Corinne Veronique
发明人： Gihad Dargazanli , Geneviève Estenne-Bouhtou , Pascale Magat , Benoît Marabout , Florence Medaisko , Pierre Roger , Mireille Sevrin , Corinne Veronique
IPC分类号： A61K31/445 , C07D413/02
CPC分类号： C07D211/26
摘要： The present invention discloses and claims a compound of general formula (I) wherein A, X and R2 are as described herein. Also disclosed and claimed is application of this compound in a variety of therapeutic applications.
摘要翻译：本发明公开并要求其中A，X和R 2 2如本文所述的通式（I）的化合物。还公开并要求保护的是这种化合物在各种治疗应用中的应用。

9. 发明授权

US08513246B2 Use of N-heterocyclylmethylbenzamides in therapeutics 有权
标题翻译：在治疗中使用N-杂环基甲基苯甲酰胺
公开(公告)号：US08513246B2
公开(公告)日：2013-08-20
申请号：US12573470
申请日：2009-10-05
申请人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Pascale Magat , Benoit Marabout , Pierre Roger
发明人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Pascale Magat , Benoit Marabout , Pierre Roger
IPC分类号： A01N43/58 , A01N43/90
CPC分类号： C07D471/08 , C07D487/08
摘要： The invention relates to use of compositions in therapeutics containing a compound having general formula (I): Wherein R, R1, R2, X and n are as described herein.
摘要翻译：本发明涉及组合物在含有通式（I）的化合物的治疗剂中的用途：其中R，R 1，R 2，X和n如本文所述。

10. 发明授权

US07750025B2 Derivatives of N-phenyl (piperidine-2-yl) methyl benzamide, preparation method thereof and applications of same in therapeutics 失效
标题翻译： N-苯基（哌啶-2-基）甲基苯甲酰胺的衍生物及其制备方法及其在治疗中的应用
公开(公告)号：US07750025B2
公开(公告)日：2010-07-06
申请号：US11405169
申请日：2006-04-17
申请人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Pascale Magat
发明人： Gihad Dargazanli , Genevieve Estenne-Bouhtou , Pascale Magat
IPC分类号： A61K31/445 , C07D409/12
CPC分类号： C07D403/12 , C07D401/12 , C07D409/12
摘要： Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine. Moreover, the compounds of the invention may be used for treating painful muscle contracture in rheumatology and in acute spinal pathology; for treating spastic contractures of medullary or cerebral origin; for the symptomatic treatment of acute and subacute pain of light to moderate intensity; for treating intense and/or chronic pain, neurogenic pain and intractable pain; for treating Parkinson's disease and Parkinson-like symptoms of neurodegenerative origin or induced by neuroleptics; for treating partial primary and secondary generalized epilepsy of simple or complex symptomology, mixed forms and other epileptic syndromes in addition to another antiepileptic treatment, or in monotherapy, for the treatment of sleep apnea, and for neuroprotection.
摘要翻译：本文定义的式（I）化合物可用于治疗与痴呆，精神病，特别是精神分裂症（缺陷形式和生产形式）和由精神安定药物诱发的急性或慢性锥体外系症状相关的行为障碍; 用于治疗各种形式的焦虑，恐慌发作，恐惧症和强迫性强迫症; 用于治疗各种形式的抑郁症，包括精神病性抑郁症; 用于治疗酒精滥用或酒精断奶引起的疾病，性行为障碍，进食障碍和用于治疗偏头痛。此外，本发明的化合物可用于治疗风湿病和急性脊髓病变中的疼痛性肌肉挛缩; 用于治疗髓质或脑源性痉挛性挛缩; 用于轻度至中度强度的急性和亚急性疼痛的对症治疗; 用于治疗强烈和/或慢性疼痛，神经源性疼痛和难治性疼痛; 用于治疗帕金森病和神经变性起源的帕金森样症状或由精神安定药诱导; 用于治疗单纯或复杂症状，混合形式和其他癫痫综合征的部分原发性和继发性全身性癫痫以及另一种抗癫痫治疗或单一疗法，用于治疗睡眠呼吸暂停和神经保护。

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