Synthetic apelin mimetics for the treatment of heart failure
    41.
    发明授权
    Synthetic apelin mimetics for the treatment of heart failure 有权
    用于治疗心力衰竭的合成apelin模拟物

    公开(公告)号:US08673848B2

    公开(公告)日:2014-03-18

    申请号:US13747621

    申请日:2013-01-23

    IPC分类号: C07K7/08 C07K7/60 C07K7/56

    摘要: The invention provides a synthetic polypeptide of Formula I′: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

    摘要翻译: 本发明提供式I'的合成多肽:或其酰胺,酯或其盐,其中X1,X2,X3,X4,X5,X6,X7,X8,X9,X10,X11,X12和X13被定义 这里。 多肽是APJ受体的激动剂。 本发明还涉及制备本发明多肽的方法及其治疗用途,例如治疗或预防急性失代偿性心力衰竭(ADHF),慢性心力衰竭,肺动脉高压,心房颤动,Brugada综合征,室性心动过速,动脉粥样硬化 ,高血压,再狭窄,缺血性心血管疾病,心肌病,心脏纤维化,心律失常,保水,糖尿病(包括妊娠糖尿病),肥胖,外周动脉疾病,脑血管意外,短暂性脑缺血发作,创伤性脑损伤,肌萎缩性侧索硬化,烧伤( 包括晒伤)和先兆子痫。 本发明还提供药理活性剂和药物组合物的组合。

    Use of an adrenal hormone-modifying agent
    42.
    发明授权
    Use of an adrenal hormone-modifying agent 有权
    使用肾上腺激素调节剂

    公开(公告)号:US08609862B2

    公开(公告)日:2013-12-17

    申请号:US13521548

    申请日:2011-01-13

    IPC分类号: A61K31/4188 C07D235/02

    摘要: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4)alkyl, or —(C1-C4)alkyl-(C5-C7)aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4)alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10)aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明涉及治疗受试者特征为增加的应激激素水平和/或降低雄激素激素水平的疾病或病症的方法,包括向受试者施用治疗有效量的由式(I)表示的化合物:其中 n为1或3; 其中R a和R b独立地为 - (C 1 -C 4)烷基或 - (C 1 -C 4)烷基 - (C 5 -C 7)芳基),其中R a为 并且R b任选被 - (C 1 -C 4)烷氧基取代; R 1,R 2和R 3独立地是氢,卤素,氰基或 - (C 6 -C 10)芳基,其中所述 - (C 6 -C 10)芳基任选被卤素取代,条件是不大于1个, ,R3为氢; R4和R5是氢; 或其药学上可接受的盐。

    Organic compounds
    45.
    发明授权
    Organic compounds 失效
    有机化合物

    公开(公告)号:US08436035B2

    公开(公告)日:2013-05-07

    申请号:US12519697

    申请日:2007-12-14

    IPC分类号: A61K31/4174 C07D233/64

    摘要: The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase (CYP11B2), and/or 11 beta-hydroxylase (CYP11B1), and/or aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase, aromatase, or CYP11B1. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.

    摘要翻译: 本发明提供式I化合物:所述化合物是醛固酮合酶(CYP11B2)和/或11β-羟化酶(CYP11B1)和/或芳香酶的抑制剂,因此可用于治疗疾病或疾病 由醛固酮合酶,芳香酶或CYP11B1介导。 因此,式I化合物可用于治疗低钾血症,高血压,充血性心力衰竭,肾衰竭,特别是慢性肾功能衰竭,再狭窄,动脉粥样硬化,X综合症,肥胖症,肾病,心肌梗塞后,冠心病 增加胶原蛋白的形成,纤维化和高血压和内皮功能障碍后的重塑。 最后,本发明还提供药物组合物。

    Method of modelling an underground heterogeneous medium from multipoint statistics
    46.
    发明授权
    Method of modelling an underground heterogeneous medium from multipoint statistics 失效
    从多点统计学建模地下异质介质的方法

    公开(公告)号:US08422745B2

    公开(公告)日:2013-04-16

    申请号:US12767852

    申请日:2010-04-27

    IPC分类号: G06K9/00

    摘要: A method of constructing an image representing the distribution of a categorical physical property representative of an underground zone having applications for petroleum reservoir development. A first training image representative of a geometrical structure of the categorical property is constructed. Training images representative of the distributions of several auxiliary properties are then constructed from the first training image. A probability law of the categorical property and a probability law of each auxiliary property are determined, from each training image, for a given pixel according to the values of the neighboring pixels. A probability law of the categorical property is calculated from these laws and from the images representative of the distribution of the auxiliary physical properties in the zone, and for each pixel of the image to be constructed. Finally, the value of the categorical property is determined by carrying out a random selection for the calculated probability law.

    摘要翻译: 构建代表具有用于石油储层开发应用的地下区域的分类物理特性的分布的图像的方法。 构建代表分类属性的几何结构的第一训练图像。 然后从第一训练图像构建表示几个辅助属性分布的训练图像。 根据相邻像素的值,从每个训练图像确定给定像素的分类属性的概率定律和每个辅助属性的概率定律。 根据这些定律和表示区域中辅助物理特性分布的图像以及要构建的图像的每个像素计算分类属性的概率定律。 最后,通过对计算出的概率定律进行随机选择来确定分类属性的值。

    USE OF AN ADRENAL HORMONE-MODIFYING AGENT
    47.
    发明申请
    USE OF AN ADRENAL HORMONE-MODIFYING AGENT 有权
    使用ADRENAL HORMONE-MODIFYING AGENT

    公开(公告)号:US20120295888A1

    公开(公告)日:2012-11-22

    申请号:US13521548

    申请日:2011-01-13

    摘要: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4)alkyl, or —(C1-C4)alkyl-(C5-C7)aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4)alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10)aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明涉及治疗受试者特征为增加的应激激素水平和/或降低雄激素激素水平的疾病或病症的方法,包括向受试者施用治疗有效量的由式(I)表示的化合物:其中 n为1或3; 其中R a和R b独立地为 - (C 1 -C 4)烷基或 - (C 1 -C 4)烷基 - (C 5 -C 7)芳基),其中R a为 并且R b任选被 - (C 1 -C 4)烷氧基取代; R 1,R 2和R 3独立地是氢,卤素,氰基或 - (C 6 -C 10)芳基,其中所述 - (C 6 -C 10)芳基任选被卤素取代,条件是不大于1个, ,R3为氢; R4和R5是氢; 或其药学上可接受的盐。

    METHOD AND SYSTEM FOR IMPLEMENTING DOMAIN SELECTION DURING THE TERMINATED CALL
    48.
    发明申请
    METHOD AND SYSTEM FOR IMPLEMENTING DOMAIN SELECTION DURING THE TERMINATED CALL 有权
    终止呼叫期间实施域选择的方法和系统

    公开(公告)号:US20120269117A1

    公开(公告)日:2012-10-25

    申请号:US13259440

    申请日:2010-04-23

    IPC分类号: H04W40/02

    摘要: The present invention discloses a method and a system for implementing domain selection during a terminated call, wherein, the method comprises: an application server (AS) sending, according to a received call request message, a query request message to a home subscriber server (HSS); the HSS querying, according to the query request message, a packet switching (PS) domain mobility management network element to obtain information of a called terminal and/or a network accessed by the called terminal in the call request message; the HSS feeding back the obtained information of the called terminal and/or the network accessed by the called terminal to the AS; and the AS selecting a domain to which a call message is to be routed according to the information of the called terminal and/or the network accessed by the called terminal. The present invention can greatly reduce the number of the signalings between the PS domain mobility management element and the HSS, avoids various limitations of the signaling loads generated by the HSS on network deployment, is convenient for the network deployment, and ensures the implementation of services.

    摘要翻译: 本发明公开了一种在终止呼叫期间实现域选择的方法和系统,其中,所述方法包括:应用服务器(AS)根据所接收的呼叫请求消息向所述归属订户服务器发送查询请求消息( HSS); HSS根据查询请求消息查询分组交换(PS)域移动性管理网元,以在呼叫请求消息中获取被叫终端和/或由被叫终端接入的网络的信息; HSS将被叫终端获得的信息和/或由被叫终端接入的网络反馈给AS; AS根据被叫终端的信息和/或由被叫终端接入的网络,选择要路由呼叫消息的域。 本发明可以大大减少PS域移动性管理单元与HSS之间的信号数量,避免了HSS在网络部署中产生的信令负载的各种限制,方便网络部署,保证业务的实现 。

    METHOD FOR ESTABLISHING DATA CONNECTION ON MOBILE NETWORK, MOBILE NETWORK, AND POLICY CONTROL ENTITY
    50.
    发明申请
    METHOD FOR ESTABLISHING DATA CONNECTION ON MOBILE NETWORK, MOBILE NETWORK, AND POLICY CONTROL ENTITY 有权
    移动网络,移动网络和政策控制实体建立数据连接的方法

    公开(公告)号:US20100274878A1

    公开(公告)日:2010-10-28

    申请号:US12833732

    申请日:2010-07-09

    IPC分类号: G06F15/16 H04L29/06

    摘要: A method for establishing data connections on a mobile network, a mobile network, and a policy control entity are disclosed. The method includes: establishing a data channel between a user equipment (UE) and a gateway (GW), and allocating an Internet Protocol (IP) address to the UE according to an address allocation request or a data channel setup request sent from the UE; and triggering the policy control entity to establish or update a policy control session according to the IP address. By using the mobile network and the policy control entity under the present invention, after the data channel is established between the UE and the GW, the GW may trigger the policy control entity to establish or update a policy control session.

    摘要翻译: 公开了一种用于在移动网络,移动网络和策略控制实体上建立数据连接的方法。 该方法包括:在用户设备(UE)和网关(GW)之间建立数据信道,并根据从UE发送的地址分配请求或数据信道建立请求向UE分配因特网协议(IP)地址 ; 并触发策略控制实体根据IP地址建立或更新策略控制会话。 通过使用本发明的移动网络和策略控制实体,在UE与GW之间建立数据信道之后,GW可以触发策略控制实体建立或更新策略控制会话。