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![Process for the preparation of 9-amino substituted 9,10-dihydropyrrolo[2,1-b][1,3]benzotiazepines](/abs-image/US/2006/07/18/US07078521B2/abs.jpg.150x150.jpg)
11.发明授权Process for the preparation of 9-amino substituted 9,10-dihydropyrrolo[2,1-b][1,3]benzotiazepines 失效制备9-氨基取代的9,10-二氢吡咯并[2,1-b] [1,3]苯并氮杂的方法公开(公告)号：US07078521B2
公开(公告)日：2006-07-18
申请号：US10343629
申请日：2001-07-20
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： A process is described for the preparation of compounds with the following formula where the groups are as defined below; in particular, R1 is a substituted amine; said process includes essentially the reaction of pyrrolobenzothiazepin-9-one with amine R1H to give the corresponding enamine, which is subsequently transformed into the final compound
摘要翻译： 描述了用于制备具有下式的化合物的方法，其中基团如下所定义; 特别地，R 1是取代的胺; 所述方法基本上包括吡咯并苯并硫氮杂-9-酮与胺R 1 H的反应，得到相应的烯胺，随后将其转化为最终化合物
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![Pyrrolo[2,1-B][3,1] benzothiazepines and their use for the preparation of medicaments with antipsychotic activity](/abs-image/US/2004/03/23/US06710041B2/abs.jpg.150x150.jpg)
12.发明授权Pyrrolo[2,1-B][3,1] benzothiazepines and their use for the preparation of medicaments with antipsychotic activity 失效吡咯并[2,1-B] [3,1]苯并硫氮杂和其用于制备具有抗精神病活性的药物公开(公告)号：US06710041B2
公开(公告)日：2004-03-23
申请号：US10343627
申请日：2003-02-03
IPC分类号： C07D51304
CPC分类号： C07D513/04
摘要： A compound of formula (I): where: R=H, Cl, Br, F, I, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, or C5-C6 cycloalkyl; R1 =C1-C4 dialkylamine, where the alkyl groups are the same or different from one another, 4-alkyl-1-piperazinyl, 4-hydroxyalkyl-1-piperazinyl, 1-imidazolyl, 4-alkyl-1-piperidinyl, or 4-alkyl-1-homopiperazinyl; R2 =H, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, CHO, or CH=NOH; R3 =H, CHO; or the pharmaceutically acceptable salts thereof.
摘要翻译： 式（I）化合物：其中：R = H，Cl，Br，F，I，C 1 -C 4烷氧基，C 1 -C 4烷硫基，C 1 -C 4烷基或C 5 -C 6环烷基; R1 = C1-C4二烷基胺，其中烷基彼此相同或不同，4-烷基-1-哌嗪基，4-羟基烷基-1-哌嗪基，1-咪唑基，4-烷基-1-哌啶基或4 - 烷基-1-高哌嗪基; R2 = H，C1-C4烷氧基，C1-C4烷硫基，C1-C4烷基，CHO或CH = NOH; R3 = H，CHO; 或其药学上可接受的盐。
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13.发明申请CARBAMATE DERIVATIVES IN PARTICULAR FOR THE TREATMENT OF NEUROLOGICAL DISORDERS 审中-公开特别用于治疗神经疾病的碳酸盐衍生物公开(公告)号：US20120252865A1
公开(公告)日：2012-10-04
申请号：US13202133
申请日：2010-03-08
IPC分类号： A61K31/40 , A61K31/341 , C07D207/34 , C07D333/22 , C07D307/68 , A61P25/00 , A61P3/00 , A61P9/00 , A61P11/00 , A61P1/16 , A61P1/00 , A61P35/00 , A61P21/00 , A61P25/22 , A61P25/16 , A61K31/38
CPC分类号： C07D207/34 , C07D307/56 , C07D333/26
摘要： The present invention relates to new carbamate derivatives of formula I, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders, such as neuropathic pain and anxiety.
摘要翻译： 本发明涉及式I的新型氨基甲酸酯衍生物，其制备方法，以及含有它们用于治疗神经性疾病如神经性疼痛和焦虑症的药物组合物。
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14.发明授权5-halo-tryptamine derivatives used as ligands on the 5-HT6 and/or 5-HT7 serotonin receptors 失效用作5-HT6和/或5-HT7血清素受体的配体的5-卤素 - 色胺衍生物公开(公告)号：US07098233B2
公开(公告)日：2006-08-29
申请号：US10481433
申请日：2002-06-17
IPC分类号： A61K31/405 , C07D209/196
CPC分类号： C07D209/16 , A61K31/405
摘要： Compounds of Formula (I): (I); wherein: R1 and R2 either the same or different, are H or linear or branched C1–C6 alkyl; R3=linear or branched C1–C6 alkyl; R4=halogen, and pharmaceutically acceptable salts thereof are useful as active ingredients in the preparation of medicaments used as ligands of the 5-HT6 and/or 5-HT7 serotoninergic receptors.
摘要翻译： 式（I）的化合物：（I）; 其中：R 1和R 2相同或不同，为H或直链或支链C 1 -C 6 - 烷基; R 3 =直链或支链C 1 -C 6烷基; R 4 =卤素及其药学上可接受的盐可用作制备用作5-HT 6和/或5-HT 6配体的药物的活性成分， 5-羟色胺能受体。
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15.发明授权Oxidated derivatives of triazolylpurines useful as ligands of the adenosine A2A receptor and their use as medicaments 有权可用作腺苷A2A受体的配体的三唑基嘌呤的氧化衍生物及其作为药物的用途公开(公告)号：US09133197B2
公开(公告)日：2015-09-15
申请号：US13257750
申请日：2010-03-18
IPC分类号： C07D473/34
CPC分类号： C07D473/34 , A61K31/198 , A61K31/52
摘要： The present invention relates to new triazolyl purine derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders or cerebral ischaemia for which inhibition of adenosine A2A receptor will result at improving the health state of a patient.
摘要翻译： 本发明涉及式（I）的新的三唑基嘌呤衍生物，其制备方法和含有它们的药物组合物，用于治疗神经障碍或脑缺血，其中腺苷A2A受体的抑制将导致改善健康状态 病人。
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16.发明申请OXIDATED DERIVATIVES OF TRIAZOLYLPURINES USEFUL AS LIGANDS OF THE ADENOSINE A2A RECEPTOR AND THEIR USE AS MEDICAMENTS 有权作为腺苷A2A受体的配体及其作为药物使用的三唑来膦的氧化衍生物有用公开(公告)号：US20120053191A1
公开(公告)日：2012-03-01
申请号：US13257750
申请日：2010-03-18
CPC分类号： C07D473/34 , A61K31/198 , A61K31/52
摘要： The present invention relates to new triazolyl purine derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders or cerebral ischaemia for which inhibition of adenosine A2A receptor will result at improving the health state of a patient.
摘要翻译： 本发明涉及式（I）的新的三唑基嘌呤衍生物，其制备方法和含有它们的药物组合物，用于治疗神经障碍或脑缺血，其中腺苷A2A受体的抑制将导致改善健康状态 病人。
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公开(公告)号：US20080293689A1
公开(公告)日：2008-11-27
申请号：US11578113
申请日：2005-04-05
IPC分类号： A61K31/554 , C07D513/04 , C07D487/04 , A61K31/55
CPC分类号： C07D487/04
摘要： Formula (I) compounds with atypical antipsychotic activity where the meanings of the various groups are as described here below, are endowed with activity characteristic of atypical antipsychotic agents, and therefore are useful as medicaments, particularly for the treatment of schizophrenia, paranoid states, manic-depressive states, affective disorders, social regression, personality regression and hallucinations.
摘要翻译： 具有非典型抗精神病活性的式（I）化合物，其中各组的含义如下所述，具有非典型抗精神病药物的活性特征，因此可用作药物，特别是用于治疗精神分裂症，偏执型，躁狂症 压抑状态，情感障碍，社会回归，人格回归和幻觉。
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公开(公告)号：US20080255232A1
公开(公告)日：2008-10-16
申请号：US12090033
申请日：2006-10-12
申请人： Patrizia Minetti , Roberto Di Santo
发明人： Patrizia Minetti , Roberto Di Santo
IPC分类号： A61K31/245 , C07C211/55 , A61K31/136 , A61K31/10 , C07C317/24 , C07C229/60
CPC分类号： A61K31/195 , A61K31/216 , C07C215/86 , C07C229/56 , C07C229/60 , C07C317/22 , C07C323/20 , C07C323/21
摘要： Compounds useful in the treatment of disorders characterized by deposits of amyloid aggregates are herein described together with pharmaceutical compounds containing the same. In particular the compounds of the present invention are those having the Formula (I) as reported below, where the radicals have the meaning indicated in the description.
摘要翻译： 本文中描述了用于治疗以淀粉样蛋白聚集体沉积物为特征的疾病的化合物以及含有它们的药物化合物。 特别地，本发明的化合物是具有如下所述的式（I）的化合物，其中基团具有说明书中指出的含义。
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![Pyrrolo [2,1-b][1,3]benzothiazepines with atypical antipsychotic activity](/abs-image/US/2002/05/21/US06391870B2/abs.jpg.150x150.jpg)
19.发明授权Pyrrolo [2,1-b][1,3]benzothiazepines with atypical antipsychotic activity 失效具有非典型抗精神病活性的吡咯并[2,1-b] [1,3]苯并硫氮杂公开(公告)号：US06391870B2
公开(公告)日：2002-05-21
申请号：US09769740
申请日：2001-01-26
IPC分类号： C07D51300
CPC分类号： C07D513/04
摘要： Polycondensated heterocycles with a pyrrole[2,1-b][1,3]benzothiazepine structure of the following formula (I) where the groups are defined as in the description are disclosed. As compared to known antipsychotic agents, these compounds present substantial activity associated with a simultaneous reduction in unwanted extrapyramidal symptoms. These compounds can be formulated in pharmaceutical compositions for the treatment of psychoses such as, for example, schizophrenia.
摘要翻译： 公开了具有如描述中定义的基团的下式（I）的吡咯[2,1-b] [1,3]苯并硫氮杂结构的缩聚杂环。 与已知的抗精神病药相比，这些化合物具有与同时减少不需要的锥体外系症状相关的显着活性。 这些化合物可以配制在用于治疗精神病例如精神分裂症的药物组合物中。
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