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1. 发明申请

US20060020012A1 Pyrazole derivatives 有权
标题翻译：吡唑衍生物
公开(公告)号：US20060020012A1
公开(公告)日：2006-01-26
申请号：US11157340
申请日：2005-06-20
申请人： Lyn Jones , Charles Mowbray , David Price , Matthew Selby , Paul Stupple
发明人： Lyn Jones , Charles Mowbray , David Price , Matthew Selby , Paul Stupple
IPC分类号： C07D403/02 , C07D231/04 , A61K31/4152
CPC分类号： C07D231/12 , C07D231/18 , C07D231/20 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/06 , C07D471/04
摘要： This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereofs, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
摘要翻译：本发明涉及式（I）的吡唑衍生物或其药学上可接受的盐，溶剂化物或衍生物，其中R1至R4在说明书中定义，其制备方法，用于制备含有它们的组合物的中间体和这种衍生物的用途。本发明的化合物与酶逆转录酶结合，是调节剂，特别是其抑制剂。因此，本发明的化合物可用于治疗各种病症，包括其中涉及逆转录酶的抑制的病症。感兴趣的疾病包括由人免疫缺陷病毒（HIV）引起的遗传相关逆转录病毒，如获得性免疫缺陷综合征（AIDS）。

2. 发明申请

US20050004129A1 Pyrazole derivatives 失效
标题翻译：吡唑衍生物
公开(公告)号：US20050004129A1
公开(公告)日：2005-01-06
申请号：US10669794
申请日：2003-09-23
申请人： Lyn Jones , Charles Mowbray , David Price , Matthew Selby , Paul Stupple
发明人： Lyn Jones , Charles Mowbray , David Price , Matthew Selby , Paul Stupple
IPC分类号： A61K31/4709 , A61K31/498 , A61P31/18 , C07D401/06 , C07D403/06 , C07D417/04 , C07D471/04 , C07D487/04 , C07
CPC分类号： C07D417/04 , C07D401/06 , C07D403/06 , C07D471/04 , C07D487/04
摘要： This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R4, n W, X and Y are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
摘要翻译：本发明涉及式（I）的吡唑衍生物或其药学上可接受的盐，溶剂化物或衍生物，其中R 1至R 4，n W，X和Y在说明书中定义，以及制备方法其制备中使用的含有它们的组合物和这些衍生物的用途。本发明的化合物与酶逆转录酶结合，是调节剂，特别是其抑制剂。因此，本发明的化合物可用于治疗各种病症，包括其中涉及逆转录酶的抑制的病症。感兴趣的疾病包括由人免疫缺陷病毒（HIV）引起的遗传相关逆转录病毒，如获得性免疫缺陷综合征（AIDS）。

3. 发明申请

US20050054707A1 Pyrazole derivatives 失效
标题翻译：吡唑衍生物
公开(公告)号：US20050054707A1
公开(公告)日：2005-03-10
申请号：US10657033
申请日：2003-09-05
申请人： Paul Edwards , Lyn Jones , Charles Mowbray , Paul Stupple , Isabelle Tran
发明人： Paul Edwards , Lyn Jones , Charles Mowbray , Paul Stupple , Isabelle Tran
IPC分类号： A61K31/4152 , A61K31/416 , A61K31/4439 , C07D43/02
CPC分类号： C07D231/18
摘要： This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
摘要翻译：本发明涉及式（I）的吡唑衍生物或其药学上可接受的盐，溶剂合物或衍生物，其中R 1至R 4在说明书中定义，及其制备方法，其制备中使用的中间体的含有它们的组合物和这种衍生物的用途。本发明的化合物与酶逆转录酶结合，是调节剂，特别是其抑制剂。因此，本发明的化合物可用于治疗各种病症，包括其中涉及逆转录酶的抑制的病症。感兴趣的疾病包括由人免疫缺陷病毒（HIV）引起的遗传相关逆转录病毒，如获得性免疫缺陷综合征（AIDS）。

4. 发明申请

US20050131011A1 Chemical compounds 有权
标题翻译：化合物
公开(公告)号：US20050131011A1
公开(公告)日：2005-06-16
申请号：US10953136
申请日：2004-09-28
申请人： Paul Stupple
发明人： Paul Stupple
IPC分类号： A61K31/4745 , A61P31/18 , C07D471/02 , C07D519/00
CPC分类号： C07D519/00 , A61K31/437 , Y02A50/406
摘要： The present invention provides compounds of formula (I) wherein R1 and R2 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.
摘要翻译：本发明提供式（I）化合物，其中R 1和R 2如上定义。本发明的化合物是趋化因子CCR5受体活性的调节剂，特别是拮抗剂。 CCR5受体的调节剂可用于治疗各种炎性疾病和病症，以及用于治疗HIV和遗传相关逆转录病毒的感染。

5. 发明申请

US20080085884A1 Melanin Concentrating Hormone Receptor-1 Antagonist Pyridinones 审中-公开
标题翻译：黑色素浓度激素受体-1拮抗剂吡啶酮
公开(公告)号：US20080085884A1
公开(公告)日：2008-04-10
申请号：US11862284
申请日：2007-09-27
申请人： Duncan Armour , Sebastian Galan , Charlotte Lane , Mark Lansdell , Paul Stupple
发明人： Duncan Armour , Sebastian Galan , Charlotte Lane , Mark Lansdell , Paul Stupple
IPC分类号： A61K31/397 , A61K31/4427 , A61K31/4523 , A61K31/496 , A61K31/501 , A61K31/55 , A61P1/00 , A61P15/00 , A61P25/00 , A61P29/00 , A61P3/04 , A61P9/00 , C07D205/02 , C07D213/02 , C07D221/00 , C07D223/02 , C07D237/02 , C07D295/00
CPC分类号： C07D213/74 , C07D487/04
摘要： The present invention provides for MCHR1 antagonist compounds of formula (I) and the pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein the substituents are as defined herein, and the pharmaceutically acceptable salts, solvates and prodrugs thereof, which are useful in treating diseases or conditions wherein antagonism of the MCHR1 receptor is beneficial.
摘要翻译：本发明提供式（I）的MCHR1拮抗剂化合物及其药学上可接受的盐，溶剂合物和前药，其中取代基如本文所定义，及其药学上可接受的盐，溶剂合物和前药，其可用于治疗疾病或其中MCHR1受体的拮抗作用是有益的。

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