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1. 发明申请

WO2011005295A8 MODULATORS OF THE SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：用于治疗与相关疾病相关的SPHINGOSINE-1-PHOSPHATE（S1P）受体的调节剂
公开(公告)号：WO2011005295A8
公开(公告)日：2012-09-20
申请号：PCT/US2010001803
申请日：2010-06-23
申请人： ARENA PHARM INC , JONES ROBERT M , BUZARD DANIEL J , SCHRADER THOMAS O , KASEM MICHELLE , ZHU XIUWEN , JOHNSON BENJAMIN R , LEHMANN JUERG , HAN SANGDON , KAWASAKI ANDREW M
发明人： JONES ROBERT M , BUZARD DANIEL J , SCHRADER THOMAS O , KASEM MICHELLE , ZHU XIUWEN , JOHNSON BENJAMIN R , LEHMANN JUERG , HAN SANGDON , KAWASAKI ANDREW M
IPC分类号： C07D471/04 , A61K31/407 , A61K31/437 , A61P29/00 , A61P31/12 , A61P37/00 , C07D487/04 , C07D491/04 , C07D498/04
CPC分类号： C07D471/04 , C07D487/04 , C07D491/04 , C07D498/04
摘要： The present invention relates to certain compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 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 S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.
摘要翻译：本发明涉及某些表现出有用的药理学性质的式（Ia）化合物及其药学上可接受的盐，溶剂合物和水合物，例如作为S1P1受体的激动剂。本发明还提供了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S1P1受体相关疾病例如牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应，多发性硬化症，系统性红斑狼疮，溃疡性结肠炎，I型糖尿病，痤疮，心肌缺血再灌注损伤，高血压性肾病，肾小球硬化，胃炎，多发性肌炎，甲状腺炎，白癜风，肝炎，胆汁性肝硬化，微生物感染和相关疾病，由淋巴细胞介导的疾病，疾病和病症，自身免疫疾病，炎性疾病和癌症。

2. 发明申请

WO2011109471A1 PROCESSES FOR THE PREPARATION OF S1P1 RECEPTOR MODULATORS AND CRYSTALLINE FORMS THEREOF 审中-公开
标题翻译：制备S1P1受体调节剂的方法及其结晶形式
公开(公告)号：WO2011109471A1
公开(公告)日：2011-09-09
申请号：PCT/US2011/026806
申请日：2011-03-02
申请人： ARENA PHARMACEUTICALS, INC. , JONES, Robert M. , BUZARD, Daniel J. , GHARBAOUI, Tawfik , JOHNSON, Benjamin R. , KASEM, Michelle , SCHRADER, Thomas O. , STIRN, Scott
发明人： JONES, Robert M. , BUZARD, Daniel J. , GHARBAOUI, Tawfik , JOHNSON, Benjamin R. , KASEM, Michelle , SCHRADER, Thomas O. , STIRN, Scott
IPC分类号： C07D487/04 , A61K31/407 , A61P31/12 , A61P37/00
CPC分类号： C07D487/04
摘要： The present invention relates to salts, processes, and process intermediates useful in the preparation of (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid of Formula (Ia), salts, and crystalline forms thereof. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid has been identified as an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).
摘要翻译：本发明涉及可用于制备（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H- - 吡咯并[1,2-a]吲哚-1-基）乙酸，其盐和结晶形式。化合物（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H-吡咯并[1,2-a]吲哚-1-基）乙酸被鉴定为可用于治疗S1P1受体相关疾病的S1P1受体调节剂，例如由淋巴细胞介导的疾病和病症，移植排斥反应，自身免疫性疾病和病症，炎性疾病和病症（例如急性和慢性炎性病症），癌症和特征在于血管完整性的潜在缺陷或与血管发生相关的病症，例如可能是病理性的（例如，可能发生在炎症，肿瘤发展和动脉粥样硬化中）。

3. 发明申请

WO2005051937A3 4-OXO-4,5-DIHYDRO-FURAN-2-CARBOXYLIC AND ACID DERIVATIVES AND METHODS OF TREATMENT OF METABOLIC-RELATED DISORDERS THEREOF 审中-公开
标题翻译： 4-氧-4,5-二氢呋喃-2-羧酸和酸衍生物及其与代谢相关疾病的治疗方法
公开(公告)号：WO2005051937A3
公开(公告)日：2005-09-15
申请号：PCT/US2004038920
申请日：2004-11-18
申请人： ARENA PHARM INC , JUNG JAE-KYU , SEMPLE GRAEME , JOHNSON BENJAMIN R
发明人： JUNG JAE-KYU , SEMPLE GRAEME , JOHNSON BENJAMIN R
IPC分类号： C07D307/68 , C07D409/04 , C07D409/10 , A61K31/381 , A61P3/06
CPC分类号： C07D307/68 , C07D405/04 , C07D409/04 , C07D409/10
摘要： System for selecting a colour shade comprising a very small number of colour display cards with mixed shades of two or more colours. 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 colour tone.
摘要翻译：用于选择颜色阴影的系统，其包括具有两种或更多种颜色的混合阴影的非常少量的彩色显示卡。该系统包括用于在混合色调中选择一种色调的装置，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使油漆以期望色调的装置。

4. 发明申请

WO2005051937A2 4-OXO-4,5-DIHYDRO-FURAN-2-CARBOXYLIC AND ACID DERIVATIVES AND METHODS OF TREATMENT OF METABOLIC-RELATED DISORDERS THEREOF 审中-公开
标题翻译： 4-氧代-4,5-二氢 - 呋喃-2-羧酸和酸衍生物及其代谢相关疾病的治疗方法
公开(公告)号：WO2005051937A2
公开(公告)日：2005-06-09
申请号：PCT/US2004/038920
申请日：2004-11-18
申请人： ARENA PHARMACEUTICALS, INC. , JUNG, Jae-Kyu , SEMPLE, Graeme , JOHNSON, Benjamin R.
发明人： JUNG, Jae-Kyu , SEMPLE, Graeme , JOHNSON, Benjamin R.
IPC分类号： C07D307/68
CPC分类号： C07D307/68 , C07D405/04 , C07D409/04 , C07D409/10
摘要： System for selecting a colour shade comprising a very small number of colour display cards with mixed shades of two or more colours. 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 colour 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。

5. 发明申请

WO2013028710A2 GENERATING BROADBAND SPECTRAL POWER IN MULTIPLE OPTICAL FIBERS 审中-公开
标题翻译：在多个光纤中产生宽带光谱功率
公开(公告)号：WO2013028710A2
公开(公告)日：2013-02-28
申请号：PCT/US2012/051775
申请日：2012-08-22
申请人： BAE SYSTEMS INTEGRATION AND ELECTRONIC SYSTEMS INTEGRATION INC. , CREEDEN, Daniel, J. , KELLY, David, P. , JOHNSON, Benjamin, R. , KETTERIDGE, Peter, A.
发明人： CREEDEN, Daniel, J. , KELLY, David, P. , JOHNSON, Benjamin, R. , KETTERIDGE, Peter, A.
IPC分类号： G02B26/00 , G02B6/00 , H01S3/02
CPC分类号： G02B6/268 , G02B6/14 , G02F1/383 , G02F2001/3528 , H01S3/06704 , H01S3/102 , H01S3/302
摘要： A broadband spectral power generator in a multimode optical fiber utilizes a standard multimode fiber that is coiled. A plate is placed on the coiled fiber and a force is applied to compresses the coiled fiber and thereby increase the interactions between the compressed windings and induce modal mixing and birefringence in the fiber. In addition, the compression causes additional non-linear processes to be excited and occur in the compressed fiber coil to generate more broadband light. This allows for better "mixing" of the spatial beam in the multimode fiber coil and allows for the various modes to overlap. The multimode fiber coil is made of silica, silicate, germinate, phosphate, fluoride, chalcogenide, or telluride. The compressed coiled fiber may be driven by a laser providing more than one wavelength output and this greatly increases the amount of nonlinear mixing in the fiber for a greatly enhanced spectral coverage.
摘要翻译：多模光纤中的宽带光谱发生器利用卷绕的标准多模光纤。将板放置在卷绕的纤维上并施加力以压缩卷绕的纤维，从而增加压缩绕组之间的相互作用，并引起纤维中的模态混合和双折射。此外，压缩使得额外的非线性处理被激发并发生在压缩的光纤线圈中以产生更多的宽带光。这允许在多模光纤线圈中更好地“混合”空间光束，并允许各种模式重叠。多模纤维线圈由二氧化硅，硅酸盐，发芽体，磷酸盐，氟化物，硫族化物或碲化物制成。压缩的盘绕的光纤可以由提供多于一个波长输出的激光器驱动，并且大大增加了光纤中的非线性混合量，从而大大增强了光谱覆盖。

6. 发明申请

WO2015051108A1 ZERO STRESS FIBER OPTIC FLUID CONNECTOR 审中-公开
标题翻译：零应力光纤流体连接器
公开(公告)号：WO2015051108A1
公开(公告)日：2015-04-09
申请号：PCT/US2014/058810
申请日：2014-10-02
申请人： BAE SYSTEMS INFORMATION AND ELECTRONIC SYSTEMS INTEGRATION INC. , JOHNSON, Benjamin R. , KELLY, David P. , SHAW, Michael J.
发明人： JOHNSON, Benjamin R. , KELLY, David P. , SHAW, Michael J.
IPC分类号： G02B6/42
CPC分类号： G02B6/4407 , G02B6/3814 , G02B6/4268 , G02B6/4296 , G02B6/4436 , G02B6/4477
摘要： A system and method for passing a fiber cable through a fiber connector is presented. A fiber connector includes an outer body and a series of flutes inside the outer body. The outer body forms an interior chamber that has a first opening and a second opening. The first opening allows a coolant to flow into the first opening and the first and second openings allow the fiber cable to pass through the first opening and the second opening and through the fiber connector. A series of flutes are attached to an inner surface of the outer body and extend into the interior chamber. The flutes are spaced apart from each other and extend from the inner surface toward the fiber cable but do not touch the fiber cable when no liquid is flowing in the fiber connector.
摘要翻译：提出了一种使光纤通过光纤连接器的系统和方法。光纤连接器包括外部主体和外部主体内的一系列凹槽。外部主体形成具有第一开口和第二开口的内部室。第一开口允许冷却剂流入第一开口，并且第一和第二开口允许光缆穿过第一开口和第二开口并穿过光纤连接器。一系列凹槽连接到外体的内表面并延伸到内腔中。凹槽彼此间隔开并从内表面向纤维缆线延伸，但是当光纤连接器中没有液体流动时，不会接触光缆。

7. 发明申请

WO2013028710A3 GENERATING BROADBAND SPECTRAL POWER IN MULTIPLE OPTICAL FIBERS 审中-公开
标题翻译：在多光纤中产生宽带光谱功率
公开(公告)号：WO2013028710A3
公开(公告)日：2013-06-27
申请号：PCT/US2012051775
申请日：2012-08-22
申请人： BAE SYSTEMS INTEGRATION AND ELECTRONIC SYSTEMS INTEGRATION INC , CREEDEN DANIEL J , KELLY DAVID P , JOHNSON BENJAMIN R , KETTERIDGE PETER A
发明人： CREEDEN DANIEL J , KELLY DAVID P , JOHNSON BENJAMIN R , KETTERIDGE PETER A
IPC分类号： G02B26/00 , G02B6/00 , H01S3/02
CPC分类号： G02B6/268 , G02B6/14 , G02F1/383 , G02F2001/3528 , H01S3/06704 , H01S3/102 , H01S3/302
摘要： A broadband spectral power generator in a multimode optical fiber utilizes a standard multimode fiber that is coiled. A plate is placed on the coiled fiber and a force is applied to compresses the coiled fiber and thereby increase the interactions between the compressed windings and induce modal mixing and birefringence in the fiber. In addition, the compression causes additional non-linear processes to be excited and occur in the compressed fiber coil to generate more broadband light. This allows for better "mixing" of the spatial beam in the multimode fiber coil and allows for the various modes to overlap. The multimode fiber coil is made of silica, silicate, germinate, phosphate, fluoride, chalcogenide, or telluride. The compressed coiled fiber may be driven by a laser providing more than one wavelength output and this greatly increases the amount of nonlinear mixing in the fiber for a greatly enhanced spectral coverage.
摘要翻译：多模光纤中的宽带光谱功率发生器利用卷绕的标准多模光纤。在盘绕的纤维上放置一个板并施加力以压缩卷曲的纤维，从而增加压缩绕组之间的相互作用并引起纤维中的模态混合和双折射。另外，压缩导致额外的非线性过程被激发并发生在压缩光纤线圈中以产生更多的宽带光。这允许在多模光纤线圈中更好地“混合”空间光束，并且允许各种模式重叠。多模光纤线圈由二氧化硅，硅酸盐，发芽剂，磷酸盐，氟化物，硫属元素化物或碲化物制成。压缩卷曲光纤可以由提供多于一个波长输出的激光器驱动，并且这极大地增加了光纤中的非线性混合量，从而大大增强了光谱覆盖范围。

8. 发明申请

WO2011005295A1 MODULATORS OF THE SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：用于治疗与相关疾病相关的SPHINGOSINE-1-PHOSPHATE（S1P）受体的调节剂
公开(公告)号：WO2011005295A1
公开(公告)日：2011-01-13
申请号：PCT/US2010/001803
申请日：2010-06-23
申请人： ARENA PHARMACEUTICALS, INC. , JONES, Robert M. , BUZARD, Daniel J. , SCHRADER, Thomas O. , KASEM, Michelle , ZHU, Xiuwen , JOHNSON, Benjamin R. , LEHMANN, Juerg , HAN, Sangdon , KAWASAKI, Andrew M.
发明人： JONES, Robert M. , BUZARD, Daniel J. , SCHRADER, Thomas O. , KASEM, Michelle , ZHU, Xiuwen , JOHNSON, Benjamin R. , LEHMANN, Juerg , HAN, Sangdon , KAWASAKI, Andrew M.
IPC分类号： C07D471/04 , C07D487/04 , C07D491/04 , C07D498/04 , A61K31/407 , A61K31/437 , A61P29/00 , A61P31/12 , A61P37/00
CPC分类号： C07D471/04 , C07D487/04 , C07D491/04 , C07D498/04
摘要： The present invention relates to certain compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 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 S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.
摘要翻译：本发明涉及某些式（Ia）化合物及其药学上可接受的盐，溶剂化物和水合物，其表现出有用的药理学性质，例如作为S1P1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S1P1受体相关疾病例如牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应的方法，多发性硬化症，系统性红斑狼疮，溃疡性结肠炎，I型糖尿病，痤疮，心肌缺血再灌注损伤，高血压性肾病，肾小球硬化，胃炎，多发性肌炎，甲状腺炎，白癜风，肝炎，胆汁性肝硬化，微生物感染和相关疾病，由淋巴细胞介导的疾病，疾病和病症，自身免疫疾病，炎性疾病和癌症。

9. 发明申请

WO2010030360A1 3H-IMIDAZO[4,5-b]PYRIDIN-5-OL DERIVATIVES USEFUL IN THE TREATMENT OF GPR81 RECEPTOR DISORDERS 审中-公开
标题翻译：用于治疗GPR81受体疾病的3H-咪唑并[4,5-b]吡啶-5-OL衍生物
公开(公告)号：WO2010030360A1
公开(公告)日：2010-03-18
申请号：PCT/US2009/005083
申请日：2009-09-10
申请人： ARENA PHARMACEUTICALS, INC. , MERCK & CO., INC. , BOATMAN, P. Douglas , JOHNSON, Benjamin R. , JUNG, Jae-Kyu , KASEM, Michelle , SCHRADER, Thomas O. , SKINNER, Philip J. , COLLETTI, Steven L.
发明人： BOATMAN, P. Douglas , JOHNSON, Benjamin R. , JUNG, Jae-Kyu , KASEM, Michelle , SCHRADER, Thomas O. , SKINNER, Philip J. , COLLETTI, Steven L.
IPC分类号： C07D471/04 , A61K31/437 , A61P3/06
CPC分类号： C07D471/04
摘要： The present invention is directed to certain 3H-imidazo[4,5-b]pyridin-5-ol derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the GPR81 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 GPR81 associated disorders, for example, dyslipidemia, atherosclerosis, atheromatous disease, hypertension, coronary heart disease, stroke, insulin resistance, impaired glucose tolerance, type 2 diabetes, syndrome X, obesity, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type 1 diabetes and acne.
摘要翻译：本发明涉及式（Ia）的某些3H-咪唑并[4,5-b]吡啶-5-醇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GPR81受体的激动剂。本发明还提供了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GPR81相关疾病例如血脂异常，动脉粥样硬化，动脉粥样硬化疾病，高血压，冠心病，中风，胰岛素抵抗，葡萄糖耐量异常，2型糖尿病，X综合征，肥胖症，牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应，多发性硬化，系统性红斑狼疮，溃疡性结肠炎，1型糖尿病和痤疮。

10. 发明申请

WO2005051937A8 4-OXO-4,5-DIHYDRO-FURAN-2-CARBOXYLIC AND ACID DERIVATIVES AND METHODS OF TREATMENT OF METABOLIC-RELATED DISORDERS THEREOF 审中-公开
标题翻译： 4-氧代-4,5-二氢 - 呋喃-2-羧酸和酸衍生物及其代谢相关疾病的治疗方法
公开(公告)号：WO2005051937A8
公开(公告)日：2006-08-31
申请号：PCT/US2004038920
申请日：2004-11-18
申请人： ARENA PHARM INC , JUNG JAE-KYU , SEMPLE GRAEME , JOHNSON BENJAMIN R
发明人： JUNG JAE-KYU , SEMPLE GRAEME , JOHNSON BENJAMIN R
IPC分类号： C07D307/68 , C07D409/04 , C07D409/10
CPC分类号： C07D307/68 , C07D405/04 , C07D409/04 , C07D409/10
摘要： The present invention relates to certain 4-oxo-4,5-dihydro-furan-2-carboxylic acid and ester 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 a-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4-氧代-4,5-二氢呋喃-2-羧酸和酯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的激动剂受体。本发明还提供含有本发明化合物的药物组合物和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，本发明还提供了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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