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51. 发明授权

US07589089B2 Inhibitors for GlyT-1 失效
标题翻译： GlyT-1抑制剂
公开(公告)号：US07589089B2
公开(公告)日：2009-09-15
申请号：US11895097
申请日：2007-08-23
申请人： Synese Jolidon , Robert Narquizian , Emmanuel Pinard
发明人： Synese Jolidon , Robert Narquizian , Emmanuel Pinard
IPC分类号： C07D261/06 , C07D307/02 , C07D333/02 , C07D333/50 , C07D295/00 , C07D213/02 , C07D317/44 , A61K31/5375 , A61K31/164 , A61K31/341 , A61K31/357 , A61K31/381 , A61K31/42 , A61K31/44 , C07C233/00
CPC分类号： C07C237/12 , C07C255/57 , C07D213/81 , C07D213/82 , C07D317/52 , C07D333/20 , C07D333/70
摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, R4, and X are as defined herein or to pharmaceutically acceptable acid addition salts thereof, with the exception of 4-methoxy-N-[2-oxo-2-(phenylamino)ethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[5-chloro-2-methoxyphenyl)amino]-2-oxoethyl]-N-benzamide, 4-methyl-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide, N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-methyl-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide and N-[2-[(2,4-dimethoxyphenyl)amino]-2-oxoethyl]-N-[(2-fluorophenyl)methyl]-benzeneacetamide. The compounds are useful in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及式I化合物，其中R 1，R 2，R 3，R 4和X如本文所定义，或其药学上可接受的酸加成盐，除了4-甲氧基-N- [2-氧代-2- （苯基氨基）乙基] -N-苯基 - 苯甲酰胺，4-氯-N- [2 - [（4-甲基苯基）氨基] -2-氧代乙基] -N-苯基 - 苯甲酰胺，4-氯-N- [2- [5-氯-2-甲氧基苯基]氨基] -2-氧代乙基] -N-苯甲酰胺，4-甲基-N-（2-氧代-2 - [（2,4,6-三氯苯基）氨基]乙基] -N - 苯甲酰胺，N- [2 - [（4-甲基苯基）氨基] -2-氧代乙基] -N-苯基 - 苯甲酰胺，4-甲基-N- [2 - [（4-甲基苯基）氨基] -2-氧代乙基] -N-苯基 - 苯甲酰胺，4-氯-N-（2-氧代-2 - [（2,4,6-三氯苯基）氨基]乙基] -N-苯甲酰胺和N- [2 - [（2,4- 二甲氧基苯基）氨基] -2-氧代乙基] -N - [（2-氟苯基）甲基] - 苯乙酰胺。该化合物可用于治疗神经和神经精神障碍。

52. 发明授权

US07557114B2 Heterocyclic-substituted phenyl methanones 有权
标题翻译：杂环取代的苯基甲酮
公开(公告)号：US07557114B2
公开(公告)日：2009-07-07
申请号：US11343365
申请日：2006-01-31
申请人： Synese Jolidon , Robert Narquizian , Roger David Norcross , Emmanuel Pinard
发明人： Synese Jolidon , Robert Narquizian , Roger David Norcross , Emmanuel Pinard
IPC分类号： A01N43/90 , A01N43/42 , A61K31/519 , A61K31/44 , A01N43/52 , A01N43/56 , A61K31/40 , C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02
CPC分类号： C07D471/04 , C07D209/08 , C07D209/44 , C07D209/46 , C07D209/88 , C07D231/56 , C07D235/06 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07D487/04 , C07D491/08
摘要： The present invention relates to compounds of formula I wherein R1 and R2 are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. Compounds of the invention are GlyT-1 inhibitors and are useful for the treatment of CNS disorders such as psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders, or Alzheimer's disease.
摘要翻译：本发明涉及式I化合物，其中R 1和R 2在本说明书中定义及其药学上可接受的酸加成盐。本发明化合物是GlyT-1抑制剂，可用于治疗CNS疾病如精神病，记忆障碍和学习功能障碍，精神分裂症，痴呆，注意力缺陷障碍或阿尔茨海默病。

53. 发明授权

US07553862B2 4-amino-1,5-substituted-1,5-dihydro-imidazol-2-ones 失效
标题翻译： 4-氨基-1,5-取代-1,5-二氢 - 咪唑-2-酮
公开(公告)号：US07553862B2
公开(公告)日：2009-06-30
申请号：US11712783
申请日：2007-03-01
申请人： Synese Jolidon , Robert Narquizian , Roger Norcross , Emmanuel Pinard
发明人： Synese Jolidon , Robert Narquizian , Roger Norcross , Emmanuel Pinard
IPC分类号： A61K31/4166 , C07D233/32
CPC分类号： C07D233/92
摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, and R4 are as defined herein and to pharmaceutically acceptable acid addition salts thereof. Compounds of formula I or their tautomeric forms are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. Such compounds are useful for the treatment of schizophrenia.
摘要翻译：本发明涉及其中R 1，R 2，R 3和R 4如本文所定义的式I化合物及其药学上可接受的酸加成盐。式I化合物或其互变异构体形式是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂，对甘氨酸转运蛋白2（GlyT-2）抑制剂具有良好的选择性。这些化合物可用于治疗精神分裂症。

54. 发明申请

US20080287455A1 SULFANYL SUBSTITUTED PHENYL METHANONES 审中-公开
标题翻译： SULFANYL替代苯甲醇
公开(公告)号：US20080287455A1
公开(公告)日：2008-11-20
申请号：US12173886
申请日：2008-07-16
申请人： Synese Jolidon , Robert Narquizian , Roger David Norcross , Emmanuel Pinard
发明人： Synese Jolidon , Robert Narquizian , Roger David Norcross , Emmanuel Pinard
IPC分类号： A61K31/496 , C07D295/00 , A61K31/495 , A61P25/18 , C07D403/02 , C07D401/02
CPC分类号： C07D213/74 , C07D239/42 , C07D295/192
摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, X, X1, and n are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. These compounds are good inhibitors of the glycine transporter 1 (GlyT-1) for the treatment CNS disorders, such as schizophrenia, cognitive impairment, and Alzheimer's disease.
摘要翻译：本发明涉及式I化合物，其中R 1，R 2，R 3，X，X 1， >，和n如说明书中所定义及其药学上可接受的酸加成盐。这些化合物是用于治疗CNS疾病如精神分裂症，认知障碍和阿尔茨海默病的甘氨酸转运蛋白1（GlyT-1）的良好抑制剂。

55. 发明授权

US07253318B2 Benzyloxy derivatives as MAOB inhibitors 失效
标题翻译：苄氧基衍生物作为MAOB抑制剂
公开(公告)号：US07253318B2
公开(公告)日：2007-08-07
申请号：US11156417
申请日：2005-06-20
申请人： Synese Jolidon , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Wolfgang Wostl , Rene Wyler
发明人： Synese Jolidon , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Wolfgang Wostl , Rene Wyler
IPC分类号： C07C233/65 , A61K31/165
CPC分类号： C07C255/54 , C07C235/20
摘要： The invention relates to compounds of the formula and their pharmaceutically acceptable salts wherein R1, R2, R3, R4, R5, n, m, and o are as defined in the specification. The compounds are selective monoamine oxidase β inhibitors and are useful for the treatment and prevention of Alzheimer's disease and senile dementia, as well as other CNS disorders. The invention also relates to processes for preparing such compounds and pharmaceutical compositions containing them.
摘要翻译：本发明涉及下式的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4， / SUP>，R 5，n，m和o如说明书中所定义。这些化合物是选择性单胺氧化酶β抑制剂，并且可用于治疗和预防阿尔茨海默氏病和老年痴呆以及其它CNS疾病。本发明还涉及制备这些化合物的方法和含有它们的药物组合物。

56. 发明授权

US07173133B2 Diaza-spiropiperidine derivatives 失效
标题翻译：二氮杂 - 哌啶衍生物
公开(公告)号：US07173133B2
公开(公告)日：2007-02-06
申请号：US11028281
申请日：2005-01-03
申请人： Simona Maria Ceccarelli , Synese Jolidon , Emmanuel Pinard , Andrew William Thomas
发明人： Simona Maria Ceccarelli , Synese Jolidon , Emmanuel Pinard , Andrew William Thomas
IPC分类号： C07D471/10 , C07D405/14
CPC分类号： C07D471/10
摘要： The present invention relates to compounds of formula wherein A-B is —CH2—CH2—, —CH2—O— or —O—CH2—; X is hydrogen or hydroxy; R1 is aryl, optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, cyano, CF3, —OCF3, lower alkoxy, —SO2-lower alkyl and heteroaryl; R2 is aryl, optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, CF3, and lower alkoxy; R3 is hydrogen or lower alkyl; n is 0, 1 or 2; or a pharmaceutically active salt thereof. The compounds of the invention may be used in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及下式的化合物其中AB是-CH 2 -CH 2 - ， - CH 2 -O - 或-O- CH 2 - ; X是氢或羟基; R 1是芳基，任选被一个或两个选自卤素，低级烷基，氰基，CF 3，-OCF 3，低级烷氧基，-SO 2 - 低级烷基和杂芳基; R 2是任选被一个或两个选自卤素，低级烷基，CF 3 N 3和低级烷氧基的取代基取代的芳基; R 3是氢或低级烷基; n为0,1或2; 或其药物活性盐。本发明的化合物可用于治疗神经和神经精神障碍。

57. 发明申请

US20060167009A1 Monocyclic substituted phenyl methanones 有权
标题翻译：单环取代苯甲酮
公开(公告)号：US20060167009A1
公开(公告)日：2006-07-27
申请号：US11324990
申请日：2006-01-03
申请人： Synese Jolidon , Robert Narquizian , Roger Norcross , Emmanuel Pinard
发明人： Synese Jolidon , Robert Narquizian , Roger Norcross , Emmanuel Pinard
IPC分类号： A61K31/496 , C07D417/02
CPC分类号： C07D285/08 , C07D277/42 , C07D277/56 , C07D285/135 , C07D417/12
摘要： The present invention relates to compounds of formula I wherein R1, R2, X1, and X2 are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. Such compounds are inhibitors of the glycine transporter 1 (GlyT-1) and can be used in the treatment of schizophrenia, cognitive impairment, and Alzheimer's disease.
摘要翻译：本发明涉及式I化合物，其中R 1，R 2，X 1和X 2，如本说明书中所定义的及其药学上可接受的酸加成盐。这些化合物是甘氨酸转运蛋白1（GlyT-1）的抑制剂，可用于治疗精神分裂症，认知障碍和阿尔茨海默病。

58. 发明申请

US20050070539A1 Benzoyl-piperazine derivatives 有权
标题翻译：苯甲酰哌嗪衍生物
公开(公告)号：US20050070539A1
公开(公告)日：2005-03-31
申请号：US10933103
申请日：2004-09-02
申请人： Daniela Alberati-Giani , Synese Jolidon , Robert Narquizian , Matthias Nettekoven , Roger Norcross , Emmanuel Pinard , Henri Stadler
发明人： Daniela Alberati-Giani , Synese Jolidon , Robert Narquizian , Matthias Nettekoven , Roger Norcross , Emmanuel Pinard , Henri Stadler
IPC分类号： A61K31/495 , A61K31/496 , A61P25/28 , C07D207/08 , C07D207/12 , C07D207/20 , C07D211/42 , C07D231/12 , C07D233/54 , C07D237/20 , C07D249/08 , C07D257/04 , C07D295/192 , C07D307/14 , C07D309/14 , C07D43/02 , A61K31/501 , A61K31/506 , A61K31/53
CPC分类号： C07D295/192 , A61K31/495 , A61K31/496 , C07D207/08 , C07D207/12 , C07D207/20 , C07D211/42 , C07D231/12 , C07D233/54 , C07D237/20 , C07D249/08 , C07D257/04 , C07D307/14 , C07D309/14
摘要： A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译：式的化合物，其中取代基如治疗精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆和其他认知过程受损的其他疾病（如注意力缺陷障碍或阿尔茨海默病）的治疗方法所述。

59. 发明授权

US06846832B2 2,3-dihydro-isoindol-1-one derivatives 失效
标题翻译： 2,3-二氢 - 异吲哚-1-酮衍生物
公开(公告)号：US06846832B2
公开(公告)日：2005-01-25
申请号：US10625116
申请日：2003-07-22
申请人： Synese Jolidon , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Rene Wyler
发明人： Synese Jolidon , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Rene Wyler
IPC分类号： A61K31/4035 , A61K31/405 , A61P1/14 , A61P3/00 , A61P3/04 , A61P25/00 , A61P25/02 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/34 , A61P43/00 , C07D209/46 , C07D209/48 , C07D471/04 , A61K31/435 , C07D209/44 , C07D221/02
CPC分类号： C07D471/04 , C07D209/46
摘要： 2,3-Dihydro-isoindol-1-one derivatives, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them, for the prevention and treatment of diseases which are mediated by monoamine oxidase B.
摘要翻译： 2,3-二氢 - 异吲哚-1-酮衍生物，其制备方法，它们作为药物的用途和包含它们的药物组合物，用于预防和治疗由单胺氧化酶B介导的疾病。

60. 发明授权

US5239084A Substituted aminoalkyl biphenyl compounds 失效
标题翻译：取代的氨基烷基联苯化合物
公开(公告)号：US5239084A
公开(公告)日：1993-08-24
申请号：US943268
申请日：1992-09-10
申请人： Philippe Guerry , Synese Jolidon
发明人： Philippe Guerry , Synese Jolidon
IPC分类号： C07C215/30 , C07C225/16 , C07C255/58
CPC分类号： C07C225/16 , C07C215/30 , C07C255/58
摘要： Antimycotically-active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-7 -alkyl or C.sub.2-7 -alkenyl or together are a straight chain C.sub.2-4 -alkylene; R.sup.3 and R.sup.4 each independently are hydrogen or C.sub.1-7 -alkyl; R.sup.5 and R.sup.6 each independently are hydrogen, halogen, trifluoromethyl, nitro, cyano, C.sub.1-7 -alkoxy or C.sub.1-7 -alkyl; and Q is an unsubstituted or substituted phenyl or naphthyl group, wherein the substituents are at least one of halogen, trifluoromethyl, cyano, nitro, C.sub.1-7 -alkyl, C.sub.1-7 -alkoxy; C.sub.2-10 -alkenyl; or a substituted or unsubstituted C.sub.1-10 -alkyl group wherein said substituents are at least one hydroxy group; andpharmaceutically acceptable acid addition salts thereof.
摘要翻译：式IMA的抗真菌活性化合物，其中R 1和R 2各自独立地为氢，C 1-7 - 烷基或C 2-7 - 烯基或一起为直链C 2-4 - 亚烷基; R 3和R 4各自独立地为氢或C 1-7 - 烷基; R 5和R 6各自独立地为氢，卤素，三氟甲基，硝基，氰基，C 1-7 - 烷氧基或C 1-7 - 烷基; Q为未取代或取代的苯基或萘基，其中取代基为卤素，三氟甲基，氰基，硝基，C 1-7 - 烷基，C 1-7 - 烷氧基， C2-10-烯基; 或取代或未取代的C 1-10 - 烷基，其中所述取代基是至少一个羟基; 及其药学上可接受的酸加成盐。

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