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199 条记录 (耗时 0.043 秒)

    FPR1 antagonist derivatives and use thereof
    4.
    发明授权
    FPR1 antagonist derivatives and use thereof 有权
    FPR1拮抗剂衍生物及其用途

    公开(公告)号：US09593144B2

    公开(公告)日：2017-03-14

    申请号：US14792147

    申请日：2015-07-06

    申请人： CHANG GUNG UNIVERSITY

    发明人： Tsong-Long Hwang ,  Pei-Wen Hsieh ,  Yin-Ting Huang ,  Chih-Hao Hung

    IPC分类号： C07K5/065 ,  C07D209/20 ,  C07K5/078 ,  A61K38/00

    CPC分类号： C07K5/06078 ,  A61K38/00 ,  C07D209/20 ,  C07K5/06156

    摘要： A dipeptide derivative as formyl peptide receptor 1 (FPR1) antagonist is provided. The dipeptide derivative is represented by formula (I), wherein: the chiral centers in formula (I) are S and R configurations respectively; each of RK and RT is selected from a group consisting of a hydrogen, a hydroxyl group, a C1-C4 alkyl-substituted hydroxyl group, a C1-C4 alkoxyl group, a carboxylic acid group, a C1-C4 alkyl nitrile-substituted, C1-C4 alkyl-substituted or C1-C4 alkoxyl-substituted amido group, a C1-C4 alkyl-substituted ester group and a benzoyl group having a C1-C4 alkyl-substituted benzene ring; and each of RM and RS is selected from a group consisting of a hydrogen, a hydroxyl group, a phenyl group, a pyridinyl group, a carboxylic acid group, a C1-C4 alkoxyl substituted ester group, and a benzoyl group having a hydroxyl-substituted, a halogen-substituted, a C1-C4 alkoxyl-substituted or a C1-C4 alkyl-substituted benzene ring.

    摘要翻译： 提供了作为甲酰肽受体1（FPR1）拮抗剂的二肽衍生物。 二肽衍生物由式（I）表示，其中：式（I）中的手性中心分别为S和R构型; RK和RT各自选自氢，羟基，C1-C4烷基取代的羟基，C1-C4烷氧基，羧酸基，C1-C4烷基腈取代的， C1-C4烷基取代或C1-C4烷氧基取代的酰胺基，C1-C4烷基取代的酯基和具有C1-C4烷基取代的苯环的苯甲酰基; RM和RS中的每一个选自氢，羟基，苯基，吡啶基，羧酸基，C 1 -C 4烷氧基取代的酯基和具有羟基的苯甲酰基， 取代的卤素取代的C 1 -C 4烷氧基取代的苯环或C 1 -C 4烷基取代的苯环。

    CHEMICAL SYNTHESIS AND SCREENING OF BICYCLIC PEPTIDE LIBRARIES
    7.
    发明申请
    CHEMICAL SYNTHESIS AND SCREENING OF BICYCLIC PEPTIDE LIBRARIES 有权
    化学合成和双相胶体图谱的筛选

    公开(公告)号：US20160115202A1

    公开(公告)日：2016-04-28

    申请号：US14893203

    申请日：2014-05-23

    申请人： OHIO STATE INNOVATION FOUNDATION

    发明人： Dehua Pei ,  Punit Upadhyaya ,  Wenlong Lian ,  Thi Trinh

    IPC分类号： C07K7/64

    CPC分类号： C07K7/64 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/06156 ,  C07K5/0817

    摘要： Disclosed herein are bicyclic peptide compounds, compositions comprising same, methods for making same, and libraries comprising same. The disclosed compounds, in various aspects, are useful for treating a variety of disorders, including inflammatory disorders, autoimmune disorders, and disorders of uncontrolled cellular proliferation. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

    摘要翻译： 本文公开了双环肽化合物，包含其的组合物，其制备方法和包含其的文库。 在各个方面，所公开的化合物可用于治疗各种疾病，包括炎性疾病，自身免疫性疾病和不受控制的细胞增殖紊乱。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

    DENDRIMERIC PEPTIDES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME
    8.
    发明申请
    DENDRIMERIC PEPTIDES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME 审中-公开
    滴定肽，药物组合物及其使用方法

    公开(公告)号：US20150337011A1

    公开(公告)日：2015-11-26

    申请号：US14814982

    申请日：2015-07-31

    申请人： Neville R. Kallenbach ,  Filbert Totsingan

    发明人： Neville R. Kallenbach ,  Filbert Totsingan

    IPC分类号： C07K7/02 ,  C07K5/078

    CPC分类号： C07K7/02 ,  A61K38/00 ,  C07K5/06156 ,  C07K14/001 ,  C07K19/00 ,  Y02A50/473 ,  Y02A50/475

    摘要： Novel peptide compounds and pharmaceutical compositions thereof are disclosed that have a formula represented by the following formula (I) wherein L1, L2, L3, Z, R1, R2, R4 and R5 are as described herein. The compounds demonstrate antimicrobial activity and may be prepared as pharmaceutical compositions and used for the prevention and treatment of a variety of conditions in mammals including humans where microbial invasion is involved. The present peptides are particularly valuable as their effect is rapid, broad in spectrum and mostly indifferent to resistance provided by standard antibiotics.

    摘要翻译： 公开了新的肽化合物及其药物组合物，其具有由下式（I）表示的式，其中L 1，L 2，L 3，Z，R 1，R 2，R 4和R 5如本文所述。 这些化合物表现出抗微生物活性，并且可以制备成药物组合物，并用于预防和治疗涉及微生物入侵的哺乳动物包括人的各种病症。 本发明的肽是特别有价值的，因为它们的作用是快速的，光谱广泛的，并且对标准抗生素提供的抗性几乎无关。

    Dipeptide analogs for treating conditions associated with amyloid fibril formation
    9.
    发明授权
    Dipeptide analogs for treating conditions associated with amyloid fibril formation 有权
    用于治疗与淀粉样蛋白原纤维形成相关的病症的二肽类似物

    公开(公告)号：US09096645B2

    公开(公告)日：2015-08-04

    申请号：US13884989

    申请日：2011-11-15

    申请人： Ehud Gazit ,  Yaniv Amir ,  Ludmila Buzhansky ,  Ulrich Abel ,  Anat Frydman-Marom

    发明人： Ehud Gazit ,  Yaniv Amir ,  Ludmila Buzhansky ,  Ulrich Abel ,  Anat Frydman-Marom

    IPC分类号： A61K38/05 ,  C07D209/20 ,  C07K5/078

    CPC分类号： C07K5/06156

    摘要： Dipeptide analogs comprising a tryptophan (Trp) moiety coupled to a beta-sheet breaker moiety derived from alpha-aminoisobutyric acid (Aib) are disclosed. The dipeptide analogs exhibit an improved performance in inhibiting amyloid fibril formation, as compared to previously described dipeptides. Compositions containing the dipeptide analogs and uses thereof in treating amyloid-associated diseases and disorders are also disclosed.

    摘要翻译： 公开了包含与衍生自α-氨基异丁酸（Aib）的β-折叠片断裂部分偶联的色氨酸（Trp）部分的二肽类似物。 与先前描述的二肽相比，二肽类似物在抑制淀粉样蛋白原纤维形成中表现出改进的性能。 还公开了含有二肽类似物的组合物及其在治疗淀粉样蛋白相关疾病和病症中的用途。