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公开(公告)号：US20130203735A1
公开(公告)日：2013-08-08
申请号：US13880441
申请日：2011-10-24
IPC分类号： C07D413/04 , C07D413/14
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is directed to caprolactams which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译： 本发明涉及作为代谢型谷氨酸受体，特别是mGluR5受体的正性变构调节剂的己内酰胺，并且其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及涉及代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。
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公开(公告)号：US07410992B2
公开(公告)日：2008-08-12
申请号：US10569921
申请日：2004-08-31
IPC分类号： A61K31/416 , C07D231/54
CPC分类号： C07D401/06 , C07F9/65038 , C07F9/65583
摘要： This invention relates to potent potassium channel blocker compounds of Formula (I) or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans, or a pharmaceutically acceptable salt, in vivo hydrolysable ester, enantiomer, diastereomer or mixture thereof: formula (II) represents C6-10 aryl or C3-10 heterocyclyl, said aryl or heterocyclyl optionally substituted with 1-3 groups selected from Ra; Z represents (CH2)nPO(OR)(OR*).
摘要翻译： 本发明涉及式（I）的有效钾通道阻断剂化合物或其制剂用于治疗青光眼和导致患者眼睛中眼内压升高的其它病症。 本发明还涉及这些化合物对哺乳动物物种，特别是人类或其药学上可接受的盐，体内可水解的酯，对映异构体，非对映体或其混合物的眼睛的神经保护作用的用途：式（II） 所述芳基或杂环基任选被1-3个选自R a，R b，R 3，R 3，R 3， Z表示（CH 2）n PO（OR）（OR *）。
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公开(公告)号：US07196082B2
公开(公告)日：2007-03-27
申请号：US10684990
申请日：2003-10-14
IPC分类号： A61K31/5375 , A61K31/44 , A61K31/416 , C07D231/56 , C07D413/06
CPC分类号： C07F9/65038 , C07D231/56
摘要： This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
摘要翻译： 本发明涉及式I的有效钾通道阻断剂化合物或其制剂用于治疗青光眼和导致患者眼睛中眼内压升高的其它病症。 本发明还涉及这些化合物对哺乳动物物种尤其是人的眼睛的神经保护作用的用途。
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公开(公告)号：US07807684B2
公开(公告)日：2010-10-05
申请号：US11487885
申请日：2006-07-17
申请人： Sandeep A. Saggar , John T. Sisko , Thomas J. Tucker , Robert M. Tynebor , Dai-Shi Su , Neville J. Anthony
发明人： Sandeep A. Saggar , John T. Sisko , Thomas J. Tucker , Robert M. Tynebor , Dai-Shi Su , Neville J. Anthony
IPC分类号： C07D471/02 , A61K31/47
CPC分类号： C07C311/46 , C07C255/54 , C07C255/60 , C07C307/06 , C07C317/40 , C07C2601/14 , C07D209/08 , C07D213/65 , C07D213/75 , C07D231/56 , C07D235/06 , C07D249/04 , C07D249/06 , C07D263/56 , C07D271/06 , C07D271/10 , C07D271/107 , C07D277/64 , C07D333/48 , C07D471/04
摘要： Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译： 具有以下结构的化合物是HIV逆转录酶抑制剂，其中A，X，Y，Z，R 1和R 2在本文中定义。 化合物及其药学上可接受的盐可用于抑制HIV逆转录酶，预防和治疗HIV感染以及艾滋病的预防，延迟发作和治疗。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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公开(公告)号：US07528163B2
公开(公告)日：2009-05-05
申请号：US10530840
申请日：2003-11-04
申请人： James B. Doherty , Meng-Hsin Chen , Luping Liu , Swaminathan R. Natarajan , Dong-Ming Shen , Robert M. Tynebor
发明人： James B. Doherty , Meng-Hsin Chen , Luping Liu , Swaminathan R. Natarajan , Dong-Ming Shen , Robert M. Tynebor
IPC分类号： A61K31/415 , C07D231/56
CPC分类号： C07D417/14 , C07D231/56 , C07D401/06 , C07D403/06 , C07D417/12
摘要： This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
摘要翻译： 本发明涉及式I的有效钾通道阻断剂化合物或其制剂用于治疗青光眼和导致患者眼睛眼内压升高的其它病症。 本发明还涉及这些化合物对哺乳动物物种尤其是人的眼睛的神经保护作用的用途。
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公开(公告)号：US07547720B2
公开(公告)日：2009-06-16
申请号：US11641212
申请日：2006-12-19
IPC分类号： A61K31/416 , C07D231/56
CPC分类号： C07F9/65038 , C07D231/56
摘要： This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
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公开(公告)号：US07494983B2
公开(公告)日：2009-02-24
申请号：US10570231
申请日：2004-08-31
IPC分类号： A61K31/675 , A61K31/4439 , C07F9/06
CPC分类号： C07D401/06
摘要： This invention relates to potent potassium channel blocker compounds of structural Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
摘要翻译： 本发明涉及结构式I的有效钾通道阻断剂化合物或其制剂用于治疗青光眼和导致患者眼睛中眼内压升高的其它病症。 本发明还涉及这些化合物对哺乳动物物种尤其是人的眼睛的神经保护作用的用途。
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