Heteroaryl amide derivatives
    3.
    发明授权
    Heteroaryl amide derivatives 失效
    杂芳酰胺衍生物

    公开(公告)号:US08431593B2

    公开(公告)日:2013-04-30

    申请号:US12516480

    申请日:2007-11-27

    摘要: Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

    摘要翻译: 提供了以下分子式的杂芳酰胺衍生物:其中变量如本文所述。 这些化合物是可用于在体内或体外调节特异性受体活性的配体,并且特别可用于治疗与人类,驯养伴侣动物和家畜中的病理受体激活相关的病症。 还提供了使用这些化合物治疗这种病症的药物组合物和方法,以及使用这些配体进行受体定位研究的方法。

    Heteroaryl amide analogues as P2X7 antagonists
    5.
    发明授权
    Heteroaryl amide analogues as P2X7 antagonists 失效
    杂芳基酰胺类似物作为P2X7拮抗剂

    公开(公告)号:US08580812B2

    公开(公告)日:2013-11-12

    申请号:US12595394

    申请日:2008-04-09

    摘要: Heteroaryl amide analogues are provided, of Formula (I), wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

    摘要翻译: 提供了式(I)的杂芳基酰胺类似物,其中变量如本文所述。 这些化合物是可用于在体内或体外调节特异性受体活性的配体,并且特别可用于治疗与人类,驯养伴侣动物和家畜中的病理受体激活相关的病症。 还提供了使用这些化合物治疗这种病症的药物组合物和方法,以及使用这些配体进行受体定位研究的方法。

    Bioconjugates of synthetic apelin polypeptides
    8.
    发明授权
    Bioconjugates of synthetic apelin polypeptides 有权
    合成apelin多肽的生物缀合物

    公开(公告)号:US09340582B2

    公开(公告)日:2016-05-17

    申请号:US14336290

    申请日:2014-07-21

    摘要: The invention provides a bioconjugates comprising a synthetic polypeptide of Formula I′ (SEQ ID NO: 1): 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 and a half-life extending moiety wherein the peptide and the half-life extending moiety are covalently linked or fuse, optionally via a linker. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the bioconjugates 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: 本发明提供包含式I'(SEQ ID NO:1)的合成多肽的生物缀合物或其酰胺,其酯或其盐,其中X 1,X 2,X 3,X 4,X 5,X 6,X 7,X 8,X 9 ,X10,X11,X12和X13在本文中定义并且半衰期延长部分,其中肽和半衰期延长部分任选地经由连接体共价连接或融合。 多肽是APJ受体的激动剂。 本发明还涉及本发明的生物缀合物的制备方法及其治疗用途,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,布鲁加达综合征,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。

    Method and system for providing an uplink structure and improved channelization scheme in a wireless communication network
    9.
    发明授权
    Method and system for providing an uplink structure and improved channelization scheme in a wireless communication network 有权
    在无线通信网络中提供上行链路结构和改进的信道化方案的方法和系统

    公开(公告)号:US09036570B2

    公开(公告)日:2015-05-19

    申请号:US13264936

    申请日:2010-04-16

    摘要: A method and system are provided to perform channelization in a wireless communication network, wherein the wireless communication network including at least one base station that is communicatively coupled to at least one mobile terminal. A bandwidth of the wireless communication network is divided into a plurality of zones at the base station. Resource blocks are provided at the base station to receive data symbols transmitted in the wireless communication network. A plurality of resource blocks are combined at the base station to form a physical basic channel unit which are allocated to one of the plurality of zones at the base station. A permutation is performed on the physical basic channel unit to form a logical basic channel unit. A channel is provided to communicatively couple the base station and the mobile terminal so that the mobile terminal may send an access grant message and a user identification to the base station to transmit data in the logical basic channel unit.

    摘要翻译: 提供了一种在无线通信网络中执行信道化的方法和系统,其中所述无线通信网络包括通信地耦合到至少一个移动终端的至少一个基站。 无线通信网络的带宽在基站被分成多个区域。 在基站处提供资源块以接收在无线通信网络中发送的数据符号。 在基站处组合多个资源块,以形成分配给基站的多个区域之一的物理基本信道单元。 在物理基本信道单元上执行置换以形成逻辑基本信道单元。 提供了一种通信来通信地耦合基站和移动终端,使得移动终端可以向基站发送接入许可消息和用户标识以在逻辑基本信道单元中发送数据。

    CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE
    10.
    发明申请
    CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE 有权
    治疗心力衰竭的循环多糖

    公开(公告)号:US20150031604A1

    公开(公告)日:2015-01-29

    申请号:US14336262

    申请日:2014-07-21

    摘要: The invention provides a cyclic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13  I or an amide, an ester or a salt thereof, or a bioconjugate thereof, wherein X1, X3, X4, 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 or bioconjugates thereof, and their 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(SEQ ID NO:1)的环状多肽:X1-R-X3-X4-LS-X7-X8-X9-X10-X11-X12-X13I或酰胺,酯或盐 或其生物缀合物,其中X1,X3,X4,X7,X8,X9,X10,X11,X12和X13在本文中定义。 多肽是APJ受体的激动剂。 本发明还涉及制备本发明多肽或其生物缀合物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,心室 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,潴留,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。