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1.发明申请Substituted Oxadiazole Derivatives as Positive Allosteric Modulators of Metabotropic Glutamate Receptors 审中-公开取代的恶二唑衍生物作为代谢型谷氨酸受体的正变构调节剂公开(公告)号：US20090215822A1
公开(公告)日：2009-08-27
申请号：US11920603
申请日：2006-05-17
申请人： Marco Farina , Stefania Gagliardi , Emmanuel Le Poul , Vincent Mutel , Giovanni Palombi , Sonia-Maria Poli , Jean-Philippe Rocher
发明人： Marco Farina , Stefania Gagliardi , Emmanuel Le Poul , Vincent Mutel , Giovanni Palombi , Sonia-Maria Poli , Jean-Philippe Rocher
IPC分类号： A61K31/4545 , C07D413/04 , A61K31/454 , C07D413/14 , A61P25/18
CPC分类号： C07D413/04 , C07D413/14 , C07D417/14
摘要： The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q, W, R1 and R2 are defined in the description. Invention compounds are useful in the prevention or treatment of central or peripheral nervous system disorders as well as other disorders modulated by mGluR5 receptors.(I).
摘要翻译： 本发明涉及新的化合物，其是式（I）的恶二唑衍生物，其中B，P，Q，W，R 1和R 2在说明书中定义。 本发明化合物可用于预防或治疗中枢或周围神经系统疾病以及由mGluR5受体调节的其它障碍。（I）。
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2.发明申请Pyrrole Derivatives as Positive Allosteric Modulators of Metabotropic Receptors 审中-公开吡咯衍生物作为代谢型受体的正变构调节剂公开(公告)号：US20090203737A1
公开(公告)日：2009-08-13
申请号：US11920490
申请日：2006-05-17
申请人： Stefania Gagliardi , Emmanuel Le Poul , Iain Lingard , Giovanni Palombi , Sonia-Maria Poli , Jean-Philippe Rocher
发明人： Stefania Gagliardi , Emmanuel Le Poul , Iain Lingard , Giovanni Palombi , Sonia-Maria Poli , Jean-Philippe Rocher
IPC分类号： A61K31/4545 , C07D413/14 , A61K31/454 , A61P25/24
CPC分类号： C07D413/14
摘要： The present invention relates to new compounds which are Pyrrole derivatives of formula (I) wherein A, B, P, Q5W, R1 and R2 are defined in the description. Invention compounds are useful in the prevention or treatment of central or peripheral nervous system disorders as well as other disorders modulated by mGluR5 receptors.
摘要翻译： 本发明涉及新的化合物，其是式（I）的吡咯衍生物，其中A，B，P，Q5W，R 1和R 2在说明书中定义。 本发明化合物可用于预防或治疗中枢或周围神经系统疾病以及由mGluR5受体调节的其它病症。
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3.发明申请Novel Oxadiazole Derivatives and Their Use as Positive Allosteric Modulators of Metabotropic Glutamate Receptors 审中-公开新型恶二唑衍生物及其作为代谢型谷氨酸受体的正变构调节剂公开(公告)号：US20090197897A1
公开(公告)日：2009-08-06
申请号：US11920489
申请日：2006-05-17
申请人： Piergiuliano Bugada , Stefania Gagliardi , Emmanuel Le Poul , Vincent Mutel , Giovanni Palombi , Jean-Philippe Rocher
发明人： Piergiuliano Bugada , Stefania Gagliardi , Emmanuel Le Poul , Vincent Mutel , Giovanni Palombi , Jean-Philippe Rocher
IPC分类号： C07D413/14 , C07D413/02 , A61K31/4439 , A61K31/497 , A61P25/00
CPC分类号： C07D413/04 , C07D413/14 , C07D417/14
摘要： The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q, W, R1 and R2 are defined in the description. Invention compounds are useful in the prevention or treatment of central or peripheral nervous system disorders as well as other disorders modulated by mGluR5 receptors.
摘要翻译： 本发明涉及新的化合物，其是式（I）的恶二唑衍生物，其中B，P，Q，W，R 1和R 2在说明书中定义。 本发明化合物可用于预防或治疗中枢或周围神经系统疾病以及由mGluR5受体调节的其它病症。
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4.发明申请Novel Heterocyclic Compounds as Positive Allosteric Modulators of Metabotropic Glutamate Receptors 审中-公开新型杂环化合物作为代谢型谷氨酸受体的正变构调节剂公开(公告)号：US20100004284A1
公开(公告)日：2010-01-07
申请号：US11920597
申请日：2006-05-17
IPC分类号： A61K31/4545 , C07D401/04 , C07D211/84 , A61K31/454 , A61P25/18
CPC分类号： C07D401/04 , C07D413/04 , C07D413/14
摘要： The present invention relates to new compounds which are Heterocyclic derivatives of formula (I) wherein A, B, P, X, Y, Q, W, R1 and R2 are defined in the description. Invention compounds are useful for treating central or peripheral nervous system disorders and other disorders which are affected by the neuromodulatory effect of mGluR5 positive allosteric modulators such as cognitive decline and also to treat both positive and negative symptoms in schizophrenia.
摘要翻译： 本发明涉及作为其中A，B，P，X，Y，Q，W，R 1和R 2在本说明书中定义的式（I）的杂环衍生物的新化合物。 本发明化合物可用于治疗受到mGluR5阳性变构调节剂如认知衰退的神经调节作用影响的中枢性或周围神经系统疾病和其它疾病，并且还可用于治疗精神分裂症中的阳性和阴性症状。
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5.发明申请Carbamate derivatives as positive allosteric modulators of metabotropic glutamate receptors 审中-公开氨基甲酸酯衍生物作为代谢型谷氨酸受体的正变构调节剂公开(公告)号：US20090082399A1
公开(公告)日：2009-03-26
申请号：US11920616
申请日：2006-05-17
IPC分类号： A61K31/4545 , C07D211/42 , C07D401/12 , A61K31/40 , C07D207/12 , A61K31/445
CPC分类号： C07D295/192 , C07D207/12 , C07D211/42 , C07D211/56 , C07D401/12
摘要： The present invention relates to new compounds which are Carbamate derivatives of formula I wherein X, B, P, Q5W, R1 and R2 are defined in the description. Invention compounds are useful for treating CNS or PNS disorders which are affected by the neuromodulatory effect of mGluR5 positive allosteric modulators such as cognitive decline and also to treat both positive and negative symptoms in schizophrenia
摘要翻译： 本发明涉及新的化合物，它们是式I的氨基甲酸酯衍生物，其中X，B，P，Q5W，R 1和R 2在说明书中定义。 本发明化合物可用于治疗受到认知衰退的mGluR5阳性变构调节剂的神经调节作用影响的CNS或PNS病症，并且也用于治疗精神分裂症中的阳性和阴性症状
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6.发明申请Novel Tetrazole Derivatives as Positive Allosteric Modulators of Metabotropic Glutamate 审中-公开新型四唑衍生物作为代谢型谷氨酸的正变构调节剂公开(公告)号：US20070299110A1
公开(公告)日：2007-12-27
申请号：US11667096
申请日：2005-11-02
IPC分类号： A61K31/454 , A61K31/4545 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/34 , A61P25/36 , C07D211/06 , C07D401/04
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14
摘要： The present invention relates to new tetrazole compounds of formula I wherein B, P, Q, W, R1 and R2 are defined in the description: invention compounds are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
摘要翻译： 本发明涉及式I中的新的四唑化合物，其中B，P，Q，W，R 1和R 2是在说明书中定义的：本发明化合物可用于 治疗或预防中枢神经系统疾病以及由mGluR5受体调节的其他疾病。
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7.发明授权Secondary 8-hydroxyquinoline-7-carboxamide derivatives for use as antifungal agents 有权用作抗真菌剂的次级8-羟基喹啉-7-甲酰胺衍生物公开(公告)号：US08969380B2
公开(公告)日：2015-03-03
申请号：US13519439
申请日：2010-12-28
IPC分类号： C07D417/12 , C07D401/12 , C07D405/12 , C07D413/12 , C07D409/12 , C07D215/48
CPC分类号： C07D401/12 , C07D215/48 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention provides secondary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. These compounds are active against Candida species such as Candida Albicans and Candida Glabrata.
摘要翻译： 本发明提供通式（I）的第二8-羟基喹啉-7-甲酰胺衍生物及其药学上可接受的盐。 这些化合物可用作抗真菌剂。 具体地说，这些化合物被测试针对红纹枯菌（Tricophyton Rubrum），三孢球菌（Tricophyton Mentagrophytes），黑曲霉（Aspergillus Niger）和Scopulariopsis Brevicaulis（Scopulariopsis Brevicaulis）。 这些化合物对假丝酵母属（Candida albicans）和念珠菌（Candida Glabrata）有活性。
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8.发明申请SECONDARY 8-HYDROXYQUINOLINE-7-CARBOXAMIDE DERIVATIVES FOR USE AS ANTIFUNGAL AGENTS 有权用作抗真菌剂的二级8-羟基喹啉-7-羧酰胺衍生物公开(公告)号：US20120329797A1
公开(公告)日：2012-12-27
申请号：US13519439
申请日：2010-12-28
IPC分类号： A61K31/4709 , C07D401/12 , A61K31/497 , A61K31/47 , A61P31/10 , A61K31/5377
CPC分类号： C07D401/12 , C07D215/48 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention provides secondary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. These compounds are active against Candida species such as Candida Albicans and Candida Glabrata.
摘要翻译： 本发明提供通式（I）的第二8-羟基喹啉-7-甲酰胺衍生物及其药学上可接受的盐。 这些化合物可用作抗真菌剂。 具体地说，这些化合物被测试针对红纹枯菌（Tricophyton Rubrum），三孢球菌（Tricophyton Mentagrophytes），黑曲霉（Aspergillus Niger）和Scopulariopsis Brevicaulis（Scopulariopsis Brevicaulis）。 这些化合物对假丝酵母属（Candida albicans）和念珠菌（Candida Glabrata）有活性。
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9.发明申请QUINOLINE-4-CARBOXAMIDE DERIVATIVES AS NK-3 and NK-2 RECEPTOR ANTAGONISTS 审中-公开喹啉-4-羧酰胺衍生物作为NK-3和NK-2受体拮抗剂公开(公告)号：US20070161647A1
公开(公告)日：2007-07-12
申请号：US11685380
申请日：2007-03-13
IPC分类号： A61K31/496 , A61K31/4747 , C07D403/02 , C07D471/10
CPC分类号： C07D215/50 , C07D215/16 , C07D215/52 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/04 , C07D409/14 , C07D417/06 , C07D487/04
摘要： A compound of formula (I) as detailed in the specification or a pharmaceutically acceptable salt or solvate thereof, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.
摘要翻译： 说明书或其药学上可接受的盐或溶剂合物中详述的式（I）化合物，制备这些化合物的方法，包含这些化合物的药物组合物以及这些化合物在医药中的用途。
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10.发明授权Indole derivatives and their use for the treatment of osteoporosis amongst other applications 失效吲哚衍生物及其在其他应用中用于治疗骨质疏松症的用途公开(公告)号：US06787550B1
公开(公告)日：2004-09-07
申请号：US10018443
申请日：2001-12-12
IPC分类号： C07D40112
CPC分类号： C07D209/18 , C07D401/12 , C07D403/12
摘要： A compound of formula (1) or a salt thereof, or a solvate thereof, wherein; R1 and R2 each independently represents C1-6alkoxy or halo; R3 and R4 each independently represents hydrogen, C1-6alkoxy, arylC1-6alkoxy, hydroxy, carboxyC1-6alkoxy, hydroxyC1-6alkoxy, dihydroxyC1-6alkoxy, mono- and di-(C1-6alkyl)aminoC1-6alkoxy or aminoC1-6alkoxy, and; R5 represents —NRsRt wherein Rs and Rt each independently represent hydrogen, unsubstituted or substituted C1-6alkyl, or unsubstituted or substituted heterocyclyl, a process for the preparation of such a compound, a pharmaceutical composition containing such a compound and the use of the compound or composition in medicine.
摘要翻译： 式（1）的化合物或其盐或其溶剂合物，其中：R 1和R 2各自独立地表示C 1-6烷氧基或卤素; R 3和R 4各自独立地表示氢，C 1-6烷氧基，芳基C 1-6烷氧基，羟基，羧基C 1 1-6烷氧基，羟基C 1-6烷氧基，二羟基C 1-6烷氧基，单 - 和二 - （C 1-6烷基）氨基C 1-6烷氧基或氨基C 1-6烷氧基，和R 5表示-NR s R t，其中R 5和R t各自独立地表示氢，未取代或取代的C 1-6烷基 ，或未取代或取代的杂环基，制备这种化合物的方法，含有这种化合物的药物组合物和药物中化合物或组合物的用途。
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