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    • 4. 发明授权
    • Bioconjugates of synthetic apelin polypeptides
    • 合成apelin多肽的生物缀合物
    • US09340582B2
    • 2016-05-17
    • US14336290
    • 2014-07-21
    • Jun YuanFrederic ZecriPhilipp GroscheHongjuan ZhaoEric PetersShari Lynn CaplanChanggang Lou
    • Jun YuanFrederic ZecriPhilipp GroscheHongjuan ZhaoEric PetersShari Lynn CaplanChanggang Lou
    • C07K14/47C07K7/08A61K47/48A61K45/06A61K38/10C07K16/00A61K39/395
    • A61K38/10A61K38/00A61K45/06A61K47/542A61K47/643A61K47/68A61K47/6811C07K14/47C07K14/765C07K2319/30C07K2319/31
    • 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.
    • 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。
    • 8. 发明授权
    • Micro-controller, processing method and device for power line carrier signal reception
    • 微控制器,电源线载波信号接收的处理方法和装置
    • US08649468B2
    • 2014-02-11
    • US13609245
    • 2012-09-10
    • Rui WangSong PanJian CuiJun YuanYajun Hu
    • Rui WangSong PanJian CuiJun YuanYajun Hu
    • H04L27/06
    • H04B3/542
    • The present invention provides a micro-controller, a processing method and device for power line carrier signal reception, where the method includes: an analog mixer mixes received power line carrier signals, an analog filter filters the mixed power line carrier signals, an analog-to-digital converter converts the filtered signals, a digital mixer mixes converted signals, a digital filter filters the mixed signals and a digital demodulator demodulates the filtered signals to obtain base band data. The present invention also provides a corresponding device and a micro-controller including the device. The technical solution of the present invention can modulate the carrier signals of any frequency to a fixed frequency through two-stage frequency mixing, so that demodulation of power line carrier signals with any frequency is possible.
    • 本发明提供了一种用于电力线载波信号接收的微控制器,处理方法和装置,其中所述方法包括:模拟混频器混合接收到的电力线载波信号,模拟滤波器对混合电力线载波信号进行滤波, 数字转换器转换滤波后的信号,数字混频器混合转换的信号,数字滤波器对混合信号进行滤波,并且数字解调器解调滤波后的信号以获得基带数据。 本发明还提供了包括该装置的相应装置和微控制器。 本发明的技术方案可以通过两级混频将任何频率的载波信号调制到固定频率,从而可以对具有任何频率的电力线载波信号进行解调。
    • 9. 发明授权
    • Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
    • 吡咯并吡啶,吡咯并嘧啶和相关的杂环化合物
    • US08633193B2
    • 2014-01-21
    • US13014066
    • 2011-01-26
    • Jun YuanPeter HrnciarQin GuoGeorge D. Maynard
    • Jun YuanPeter HrnciarQin GuoGeorge D. Maynard
    • A61K31/519C07D487/04A61P37/00A61P37/06A61P11/06A61P17/06
    • C07D471/04
    • Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
    • 吡咯并 - 吡啶,吡咯并 - 嘧啶和相关的杂环化合物,其分子式如下:其中R,R 2,R 5,E,Z 1,Z 3,Z 4和Ar如本文所定义。 这些化合物是C5a受体的配体。 本发明优选的吡咯并 - 吡啶,吡咯并 - 嘧啶和相关杂环化合物以高亲和力结合C5a受体,并在C5a受体上表现出中性拮抗剂或反向激动剂活性。 本发明还涉及包含这些化合物的药物组合物,以及这些化合物在治疗各种炎性,心血管和免疫系统疾病中的用途。 此外,本发明提供了标记的吡咯并 - 吡啶,吡咯并 - 嘧啶和相关杂环化合物,其可用作C5a受体定位的探针。