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。

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。

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.

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.

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。

公开(公告)号：US20060167270A1

公开(公告)日：2006-07-27

申请号：US10530902

申请日：2003-10-09

申请人： Graeme Semple ,  Claudia Averbuj ,  Philip Skinner ,  Tawfik Gharbaoui ,  Young-Jun Shin

发明人： Graeme Semple ,  Claudia Averbuj ,  Philip Skinner ,  Tawfik Gharbaoui ,  Young-Jun Shin

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。

公开(公告)号：US20060122240A1

公开(公告)日：2006-06-08

申请号：US10533799

申请日：2003-11-04

申请人： Graeme Semple ,  Philip Skinner ,  Martin Cherrier ,  Peter Webb ,  Susan Tamura

发明人： Graeme Semple ,  Philip Skinner ,  Martin Cherrier ,  Peter Webb ,  Susan Tamura

IPC分类号： C07D249/16 ,  A61K31/4192

CPC分类号： C07D405/06 ,  A61K31/4192 ,  C07D249/18

摘要： The present invention relates to certain benzotriazole carboxylic acid or ester derivatives of Formula (I), pharmaceutically acceptable salts and solvates thereof, which exhibit useful pharmaceutical properties, for example, as agonists for the GPCR referred to as hRUP38. 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 -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： 本发明涉及一些表现出有用的药物性质的式（I）的苯并三唑羧酸或酯衍生物，其药学上可接受的盐和溶剂化物，例如被称为hRUP38的GPCR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，胰岛素抵抗，类型 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。

公开(公告)号：US20120329692A1

公开(公告)日：2012-12-27

申请号：US13579638

申请日：2010-02-19

申请人： Joe R. Noles, JR. ,  Hirokazu Saito ,  Philip Skinner ,  Raymond F. Watts ,  Keiji Hayashi ,  Atsushi Suzuki ,  Koji Saito

发明人： Joe R. Noles, JR. ,  Hirokazu Saito ,  Philip Skinner ,  Raymond F. Watts ,  Keiji Hayashi ,  Atsushi Suzuki ,  Koji Saito

IPC分类号： C10M141/10 ,  F16D13/74

CPC分类号： C10M141/10 ,  C10M141/12 ,  C10M2207/042 ,  C10M2207/126 ,  C10M2207/144 ,  C10M2207/289 ,  C10M2215/04 ,  C10M2215/042 ,  C10M2215/08 ,  C10M2215/224 ,  C10M2215/28 ,  C10M2219/022 ,  C10M2219/046 ,  C10M2223/04 ,  C10M2223/041 ,  C10M2223/043 ,  C10M2223/045 ,  C10M2223/047 ,  C10M2223/049 ,  C10N2230/06 ,  C10N2230/42 ,  C10N2230/44 ,  C10N2230/45 ,  C10N2240/04 ,  C10N2240/042 ,  C10N2240/044 ,  C10N2240/045 ,  C10N2240/08 ,  C10N2260/14 ,  C10N2260/12 ,  C10N2210/01 ,  C10N2210/02

摘要： A wet friction clutch-lubricant system wherein a wet friction clutch having a cellulose-based friction lining, or a device including such a clutch, is lubricated with a lubricant composition a major amount of oil of lubricating viscosity and minor effective amounts of performance enhancing additives including (a) one or more ashless dispersant; (b) one or more organic phosphorus compound and (c) one or more sodium salt of an organic acid; and optionally, (d) an auxiliary friction modifier.

摘要翻译： 一种湿式摩擦离合器 - 润滑剂系统，其中具有纤维素基摩擦衬片的湿摩擦离合器或包括这种离合器的装置用润滑剂组合物润滑，润滑剂组合物具有大量润滑粘度的油和少量有效量的性能增强添加剂 包括（a）一种或多种无灰分散剂; （b）一种或多种有机磷化合物和（c）一种或多种有机酸的钠盐; 和（d）辅助摩擦改性剂。

公开(公告)号：US20080164732A1

公开(公告)日：2008-07-10

申请号：US11620213

申请日：2007-01-05

申请人： Anthony Valasin ,  Radesh Vangipuram ,  Richard Squires ,  Philip Skinner ,  Joseph Talamonti

发明人： Anthony Valasin ,  Radesh Vangipuram ,  Richard Squires ,  Philip Skinner ,  Joseph Talamonti

IPC分类号： B60N2/42

CPC分类号： B60N2/688 ,  B60N2/01583 ,  B60N2/7047 ,  B60R22/023 ,  B60R22/26

摘要： A structural member for a removable vehicle seat provides integrated attachment features for a flex-mat, risers, and restraint system.

摘要翻译： 用于可移动车辆座椅的结构构件提供用于柔性垫，立管和约束系统的集成附接特征。

公开(公告)号：US6103672A

公开(公告)日：2000-08-15

申请号：US70905

申请日：1998-05-01

申请人： Adrian Dunn ,  Alain Louis Pierre Lenack ,  Philip Skinner

发明人： Adrian Dunn ,  Alain Louis Pierre Lenack ,  Philip Skinner

IPC分类号： C10M139/00 ,  C10M159/20 ,  C10M163/00 ,  C10N10/04 ,  C10N40/25 ,  C10M105/32

CPC分类号： C10M163/00 ,  C10M2201/087 ,  C10M2201/10 ,  C10M2201/102 ,  C10M2201/105 ,  C10M2203/108 ,  C10M2207/028 ,  C10M2207/26 ,  C10M2207/262 ,  C10M2215/04 ,  C10M2215/24 ,  C10M2215/26 ,  C10M2217/042 ,  C10M2217/043 ,  C10M2217/046 ,  C10M2217/06 ,  C10M2219/046 ,  C10M2219/087 ,  C10M2219/088 ,  C10M2219/089 ,  C10M2227/00 ,  C10M2227/06 ,  C10M2227/061 ,  C10M2227/062 ,  C10M2227/063 ,  C10M2227/065 ,  C10M2227/066 ,  C10N2240/102 ,  C10N2240/103 ,  C10N2270/02

摘要： An improved polybutene-free lubricant composition for marine diesel engines, comprising a major amount of oil of lubricating viscosity and, provided by admixing therewith, minor amounts of a) at least one of a borated dispersant or oil-soluble or oil-dispersible boron compound; and b) one or more overbased metal compounds the or each compound having a TBN of at least 300, with the proviso that if an overbased metal salicylate is present then the TBN of said salicylate is at least 200; wherein the TBN of the composition is at least 10 and the viscosity index of the composition is at least 90.

摘要翻译： 一种用于船用柴油发动机的改进的无聚丁烯润滑剂组合物，其包含主要量的润滑粘度的油，并且通过与其混合提供少量的a）至少一种硼酸化分散剂或油溶性或油分散性硼化合物 ; 和b）一种或多种高碱性金属化合物，所述化合物或每种化合物的TBN为至少300，条件是如果存在高碱性金属水杨酸盐，则所述水杨酸盐的TBN为至少200; 其中所述组合物的TBN为至少10，并且所述组合物的粘度指数为至少90。