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    ANDROGRAPHOLIDE DERIVATIVES AND USE THEREOF IN MANUFACTURE OF MEDICAMENTS
    2.
    发明申请
    ANDROGRAPHOLIDE DERIVATIVES AND USE THEREOF IN MANUFACTURE OF MEDICAMENTS 审中-公开
    异丙肾上腺素衍生物及其在药物制造中的应用

    公开(公告)号：WO2009018780A1

    公开(公告)日：2009-02-12

    申请号：PCT/CN2008/071919

    申请日：2008-08-07

    Applicant: PANORAMA RESEARCH INC. ,  WANG, Yuqiang ,  JIANG, Xiaojian ,  JIANG, Jie ,  ZHANG, Zaijun ,  YANG, Zhaoqi ,  YU, Pei

    Inventor： WANG, Yuqiang ,  JIANG, Xiaojian ,  JIANG, Jie ,  ZHANG, Zaijun ,  YANG, Zhaoqi ,  YU, Pei

    IPC: C07D409/12 ,  C07D307/60 ,  A61K31/365 ,  A61K31/385 ,  A61P35/00 ,  A61P29/00 ,  A61P3/10 ,  A61P31/00

    CPC classification number: C07D307/58 ,  C07D307/60 ,  C07D409/12

    Abstract: The present invention relates to an andrographolide derivative of the formula (I), wherein R 1 , R 2 and R 3 are same or different substituents selected from hydrogen, substituted or unsubstituted organic acid radicals, inorganic acid radicals, alkyl, aryl or heteroaryl, and at least one of R 1 , R 2 and R 3 is R-lipoic acid, S-lipoic acid or a mixture thereof, or corresponding dihydrolipoic acids thereof, or N-acetylcysteine radical. The derivative has good antitumor effect, can induce apoptosis of tumor cells, can directly kill Gram-positive bacteria (staphylococcus aureus) and drug resistance bacteria (MRSA5676 and MRSA5677), can inhibit the QS-system of Gram-negative bacteria (Pseudomonas aeruginosa), can inhibit and destroy the formation of biofilm of Pseudomonas aeruginosa; and exhibits significant hypoglycemic effect, so that it can be used in manufacture of medicaments for treatment of cancers, inflammation, diabetes, and bacterial and viral infections.

    Abstract translation: 本发明涉及式（I）的穿心莲内酯衍生物，其中R 1，R 2和R 3是相同或不同的选自氢，取代或未取代的有机酸基，无机酸基，烷基，芳基或杂芳基的取代基，至少 R1，R2和R3之一是R-硫辛酸，S-硫辛酸或其混合物，或其相应的二氢硫辛酸或N-乙酰半胱氨酸碱基。 该衍生物具有良好的抗肿瘤作用，可诱导肿瘤细胞凋亡，可直接杀死革兰氏阳性菌（金黄色葡萄球菌）和耐药细菌（MRSA5676和MRSA5677），可抑制革兰氏阴性菌（绿脓假单胞菌）的QS系统， ，可以抑制和破坏铜绿假单胞菌生物膜的形成; 并显示出显着的降血糖作用，因此可用于制造用于治疗癌症，炎症，糖尿病以及细菌和病毒感染的药物。

    CC-1065 ANALOGUES FOR USE AGAINST CANCERS
    5.
    发明申请
    CC-1065 ANALOGUES FOR USE AGAINST CANCERS 审中-公开
    CC-1065使用癌症的模拟物

    公开(公告)号：WO2005103040A1

    公开(公告)日：2005-11-03

    申请号：PCT/US2005/013284

    申请日：2005-04-19

    Applicant: PANORAMA RESEARCH INC. ,  WANG, Yuqiang

    Inventor： WANG, Yuqiang

    IPC: C07D405/14

    CPC classification number: C07D405/14 ,  C07D403/14

    Abstract: The present invention relates to novel CC-1065 derivatives that bind to albumin in vitro and in vivo forming albumin-drug conjugates, and their use as antitumor agents. The compounds disclosed have the following formula CC-1065 analogue-linker-maleimide (formula I), wherein the term "CC-1065 analogue" designates a moiety of formula (II) and "maleimide" is a moiety of formula (III).

    Abstract translation: 本发明涉及在体外和体内结合白蛋白的新型CC-1065衍生物，其形成白蛋白 - 药物偶联物，以及它们作为抗肿瘤剂的用途。 所公开的化合物具有下式CC-1065类似物 - 接头 - 马来酰亚胺（式I），其中术语“CC-1065类似物”表示式（II）的部分，“马来酰亚胺”是式（III）的部分。

    A 24 KILODALTON CYTOPLASMIC PROTEASE ACTIVATING DNA FRAGMENTATION APOPTOSIS
    7.
    发明申请
    A 24 KILODALTON CYTOPLASMIC PROTEASE ACTIVATING DNA FRAGMENTATION APOPTOSIS 审中-公开

    公开(公告)号：WO1995034576A1

    公开(公告)日：1995-12-21

    申请号：PCT/US1995007091

    申请日：1995-06-05

    Applicant: PANORAMA RESEARCH, INC.

    Inventor： PANORAMA RESEARCH, INC. ,  WRIGHT, Susan, C. ,  LARRICK, James, W.

    IPC: C07K01/22

    CPC classification number: C12N9/6421 ,  A61K38/00 ,  Y10S514/01

    Abstract: A 24 kilodalton cytoplasmic protease which cleaves at proline-valine bonds is purified from UV-induced human U937 histiocytic lymphoma cells by affinity chromatography using the inhibitor DK120 as the ligand, followed by heparin-sepharose chromatography and reverse phase HPLC. Treating nuclei of uninduced U937 cells with the affinity-purified protease is sufficient to activate internucleosomal DNA fragmentation characteristic of apoptosis as demonstrated by gel electrophoresis in the figure.

    Abstract translation: 通过使用抑制剂DK120作为配体的亲和层析，然后用肝素 - 琼脂糖层析和反相HPLC，从UV诱导的人U937组织细胞淋巴瘤细胞中纯化从脯氨酸 - 缬氨酸键切割的24千道尔顿胞质蛋白酶。 用亲和纯化的蛋白酶处理未诱导的U937细胞的细胞核足以激活核糖体DNA断裂特征的细胞凋亡，如图中凝胶电泳所证实的。

    NOVEL ANTICANCER CONJUGATES OF CAMPTOTHECIN AND UNSATURATED FATTY ACIDS
    8.
    发明申请
    NOVEL ANTICANCER CONJUGATES OF CAMPTOTHECIN AND UNSATURATED FATTY ACIDS 审中-公开
    新西兰冠心病和不饱和脂肪酸的新药

    公开(公告)号：WO2004012661A2

    公开(公告)日：2004-02-12

    申请号：PCT/US2003/023983

    申请日：2003-07-31

    Applicant: PANORAMA RESEARCH, INC. ,  WANG, Yuqiang

    Inventor： WANG, Yuqiang

    IPC: A61K

    CPC classification number: C07D491/22

    Abstract: The present invention provides novel conjugates of camptothecin compounds and long-chain unsaturated fatty acid. The novel conjugates can be used to treat mammalian cell proliferative diseases such as cancer.

    Abstract translation: 本发明提供喜树碱化合物和长链不饱和脂肪酸的新型缀合物。 新型缀合物可用于治疗哺乳动物细胞增殖性疾病如癌症。

    MAMMALIAN CATIONIC PROTEINS HAVING LIPOPOLYSACCHARIDE BINDING AND ANTI-COAGULANT ACTIVITY
    9.
    发明申请
    MAMMALIAN CATIONIC PROTEINS HAVING LIPOPOLYSACCHARIDE BINDING AND ANTI-COAGULANT ACTIVITY 审中-公开
    具有脂多糖结合和抗癌活性的马马里兰阳离子蛋白

    公开(公告)号：WO1994002589A1

    公开(公告)日：1994-02-03

    申请号：PCT/US1993006731

    申请日：1993-07-15

    Applicant: PANORAMA RESEARCH, INC. ,  LARRICK, James, W. ,  WRIGHT, Susan, C. ,  HIRATA, Michimasa

    Inventor： PANORAMA RESEARCH, INC.

    IPC: C12N01/21

    CPC classification number: C07K14/4723 ,  A61K38/00

    Abstract: Compositions and methods for the treatment and diagnosis of lipopolysaccharide-related conditions and coagulant-related disease are provided. Compositions include polypeptides which are identical or homologous to a certain cationic protein (CAP18) obtained from mammalian granulocytes, particularly including a reactive nitrogen inhibiting peptide (RNIP) fragment found at the carboxy-terminus of CAP18. Polypeptides are capable of binding to LPS and inhibiting LPS-mediated activation of macrophage, as well as interfering with the clotting cascade to inhibit coagulation in conditions such as disseminated intravascular coagulation. Compositions comprising the polypeptides in a suitable pharmaceutical carrier are also provided.

    Abstract translation: 提供了用于治疗和诊断脂多糖相关病症和凝血剂相关疾病的组合物和方法。 组合物包括与从哺乳动物粒细胞获得的特定阳离子蛋白（CAP18）相同或同源的多肽，特别是包括在CAP18的羧基末端发现的活性氮抑制肽（RNIP）片段。 多肽能够结合LPS并抑制LPS介导的巨噬细胞活化，以及干扰凝血级联以在诸如弥散性血管内凝血的病症中抑制凝血。 还提供了在合适的药物载体中包含多肽的组合物。

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