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1.发明申请Tetrazole derivatives and methods of treatment of metabolic-related disorders thereof 失效四唑衍生物及其代谢相关病症的治疗方法公开(公告)号：US20060217562A1
公开(公告)日：2006-09-28
申请号：US10535345
申请日：2004-10-29
申请人： Graeme Semple , Thomas Schrader , Philip Skinner , Steven Colletti , Tawfik Gharbaoui , Jason Imbriglio , Jae-Kyu Jung , Rui Liang , Subharekha Raghavan , Darby Schmidt , James Tata
发明人： Graeme Semple , Thomas Schrader , Philip Skinner , Steven Colletti , Tawfik Gharbaoui , Jason Imbriglio , Jae-Kyu Jung , Rui Liang , Subharekha Raghavan , Darby Schmidt , James Tata
IPC分类号： A61K31/416 , C07D403/02
CPC分类号： C07D491/04 , C07D403/04 , C07D495/04
摘要： The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
摘要翻译： 本发明涉及式（I）的某些四唑衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为RUP25受体的激动剂。 本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病的方法 ，综合征-X等。 此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成 抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等。
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2.发明申请Tetrazole derivatives and methods of treatment of metabolic-related disorders thereof 审中-公开四唑衍生物及其代谢相关病症的治疗方法公开(公告)号：US20070072924A1
公开(公告)日：2007-03-29
申请号：US11601252
申请日：2006-11-17
申请人： Graeme Semple , Thomas Schrader , Philip Skinner , Steven Colletti , Tawfik Gharbaoui , Jason Imbriglio , Jae-Kyu Jung , Rui Liang , Subharekha Raghavan , Darby Schmidt , James Tata
发明人： Graeme Semple , Thomas Schrader , Philip Skinner , Steven Colletti , Tawfik Gharbaoui , Jason Imbriglio , Jae-Kyu Jung , Rui Liang , Subharekha Raghavan , Darby Schmidt , James Tata
IPC分类号： A61K31/416 , C07D403/04
CPC分类号： C07D491/04 , C07D403/04 , C07D495/04
摘要： The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
摘要翻译： 本发明涉及式（I）的某些四唑衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为RUP25受体的激动剂。 本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病 ，综合征-X等。 此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成 抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等。
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3.发明授权Tetrazole derivatives and methods of treatment of metabolic-related disorders thereof 失效四唑衍生物及其代谢相关病症的治疗方法公开(公告)号：US08637555B2
公开(公告)日：2014-01-28
申请号：US10535345
申请日：2004-10-29
申请人： Graeme Semple , Thomas Schrader , Philip J. Skinner , Steven L. Colletti , Tawfik Gharbaoui , Jason E. Imbriglio , Jae-Kyu Jung , Rui Liang , Subharekha Raghavan , Darby Schmidt , James R. Tata
发明人： Graeme Semple , Thomas Schrader , Philip J. Skinner , Steven L. Colletti , Tawfik Gharbaoui , Jason E. Imbriglio , Jae-Kyu Jung , Rui Liang , Subharekha Raghavan , Darby Schmidt , James R. Tata
IPC分类号： A61K31/407 , C07D231/54
CPC分类号： C07D491/04 , C07D403/04 , C07D495/04
摘要： The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
摘要翻译： 本发明涉及式（I）的某些四唑衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为RUP25受体的激动剂。 本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病 ，综合征-X等。 此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成 抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等。
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4.发明申请公开(公告)号：US20060205955A1
公开(公告)日：2006-09-14
申请号：US11315753
申请日：2005-12-22
申请人： P. Boatman , Thomas Schrader , Graeme Semple , Philip Skinner , Jae-Kyu Jung
发明人： P. Boatman , Thomas Schrader , Graeme Semple , Philip Skinner , Jae-Kyu Jung
IPC分类号： C07D231/54
CPC分类号： C07D403/04 , C07D209/80 , C07D209/88 , C07D231/54 , C07D265/36 , C07D471/04 , C07D471/14
摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.
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5.发明申请公开(公告)号：US20070073062A1
公开(公告)日：2007-03-29
申请号：US11601184
申请日：2006-11-17
申请人： P. Boatman , Thomas Schrader , Graeme Semple , Philip Skinner , Jae-Kyu Jung
发明人： P. Boatman , Thomas Schrader , Graeme Semple , Philip Skinner , Jae-Kyu Jung
IPC分类号： C07D231/54 , C07D403/02
CPC分类号： C07D403/04 , C07D209/80 , C07D209/88 , C07D231/54 , C07D265/36 , C07D471/04 , C07D471/14
摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.
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6.发明申请5-Substituted 2h-pyrazole-3-carboxylic acid derivatives as agonists for the acid receptor rup25 for the treatment of dyslipidemia and related diseases 审中-公开5-取代的2h-吡唑-3-羧酸衍生物作为用于治疗血脂异常和相关疾病的酸受体rup25的激动剂公开(公告)号：US20070032537A1
公开(公告)日：2007-02-08
申请号：US10560332
申请日：2004-06-10
申请人： Graeme Semple , Tawfik Gharbaoui , Young-Jun Shin , Marc Decaire , Claudia Averbuj , Philip Skinner
发明人： Graeme Semple , Tawfik Gharbaoui , Young-Jun Shin , Marc Decaire , Claudia Averbuj , Philip Skinner
IPC分类号： A61K31/4152 , C07D231/02
CPC分类号： C07D231/14 , A61K31/415 , A61K45/06 , A61K2300/00
摘要： The present invention relates to certain pyrazole carboxylic acid and ester derivatives, and pharmaceutically acceptable salts thereof, which exhibit useful pharmaceutical properties, for example as agonists for the RUP25 receptor. (I) Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the prophylaxis or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like the substituents are defined in claim 1.
摘要翻译： 本发明涉及表现出有用的药物性质的某些吡唑羧酸和酯衍生物及其药学上可接受的盐，例如作为RUP25受体的激动剂。 （I）本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物预防或治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素 抗性，2型糖尿病，综合征等。 此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成 抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等，取代基如权利要求1中所定义。
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7.发明申请5-substituted 2h-pyrazone-3-carbixylic acid derivatives as antilipolytic agents for the treatment of metabolic-related disorders such as dyslipidemia 审中-公开5-取代的2h-吡嗪-3-肟基衍生物作为用于治疗代谢相关疾病如血脂异常的抗溶解剂公开(公告)号：US20060167270A1
公开(公告)日：2006-07-27
申请号：US10530902
申请日：2003-10-09
IPC分类号： C07D231/08
CPC分类号： C07D231/16 , C07D231/14
摘要： The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R2 is H, halogen, C1-12 alkyl or C1-12 haloalkyl; and R3 is C3-6 cycloalkyl, C1-12 alkyl, C1-12 haloalkyl, C3-6 cycloalkyl-C1-4-alkylene, aryl-C1-4-alkylene or heteroaryl-C1-4-alkylene, wherein said aryl-C1-4-alkylene and heteroaryl-C1-4-alkylene can be optionally substituted 1 to 5 substituents selected from the substituents listed in the claims. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for pharmaceutical compositions in combination with other active agents, for example, those agents belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, thiazolidinedione and the like.
摘要翻译： 本发明涉及式（Ia）的某些吡唑羧酸衍生物及其药学上可接受的盐作为抗脂解剂，并且针对受体RUP25，其中：R 2是H，卤素， C 1-12烷基或C 1-12卤代烷基; 且R 3是C 3-6环烷基，C 1-12烷基，C 1-12卤代烷基， C 3-6环烷基-C 1-4亚烷基，芳基-C 1-4 - 亚烷基或杂芳基-C 1 -4亚烷基，其中所述芳基-C 1-4 - 亚烷基和杂芳基-C 1-4 - 亚烷基可以是任选取代的1至5个取代基 选自权利要求中所列的取代基。 本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病的方法 ，综合征-X等。 此外，本发明还提供了与其它活性剂（例如属于α-葡糖苷酶抑制剂，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成抑制剂，贝特类）的那些试剂组合的药物组合物 ，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂，噻唑烷二酮等。
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8.发明授权4-oxo-4,5-dihydro-furan-2-carboxylic acid derivatives and methods of treatment of metabolic-related disorders thereof 失效4-氧代-4,5-二氢呋喃-2-羧酸衍生物及其代谢相关病症的治疗方法公开(公告)号：US07803837B2
公开(公告)日：2010-09-28
申请号：US11602551
申请日：2006-11-21
申请人： Jae-Kyu Jung , Graeme Semple , Benjamin R. Johnson
发明人： Jae-Kyu Jung , Graeme Semple , Benjamin R. Johnson
IPC分类号： A61K31/341 , A61K31/381 , C07D307/32 , C07D409/04
CPC分类号： C07D307/68 , C07D405/04 , C07D409/04 , C07D409/10
摘要： System for selecting a color shade comprising a very small number of color display cards with mixed shades of two or more colors. The system comprises means for selecting one shade among mixed shades, means for presenting the selected mixed shade as well as means for specifying the selected mixed shade for making paint in the desired color tone.
摘要翻译： 用于选择颜色的系统，其包括具有两种或更多种颜色的混合色调的非常少量的彩色显示卡。 该系统包括用于选择混合色调中的一个色调的装置，用于呈现所选择的混合色调的装置以及用于指定所选择的混合色调以用于制作所需色调的油漆的装置。
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9.发明申请FUSED PYRAZOLE DERIVATIVES AND METHODS OF TREATMENT OF METABOLIC-RELATED DISORDERS THEREOF 审中-公开熔化的吡唑衍生物及其代谢相关疾病的治疗方法公开(公告)号：US20090258892A1
公开(公告)日：2009-10-15
申请号：US12433704
申请日：2009-04-30
IPC分类号： A61K31/437 , C07D231/54 , C07D403/04 , A61K31/416 , A61K31/41 , A61K31/40
CPC分类号： C07D403/04 , C07D209/80 , C07D209/88 , C07D231/54 , C07D265/36 , C07D471/04 , C07D471/14
摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.
摘要翻译： 本发明涉及式（Ia）的某些稠合吡唑衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为RUP25受体的激动剂。 本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病的方法 ，综合征-X等。 此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成 抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂，DP受体拮抗剂等。
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10.发明授权Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof 有权融合的吡唑衍生物及其代谢相关病症的治疗方法公开(公告)号：US07241792B2
公开(公告)日：2007-07-10
申请号：US11315753
申请日：2005-12-22
IPC分类号： A61K31/407 , C07D231/54
CPC分类号： C07D403/04 , C07D209/80 , C07D209/88 , C07D231/54 , C07D265/36 , C07D471/04 , C07D471/14
摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.
摘要翻译： 本发明涉及式（Ia）的某些稠合吡唑衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为RUP25受体的激动剂。 本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病的方法 ，综合征-X等。 此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成 抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂，DP受体拮抗剂等。
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