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    SIXTEEN AMINO ACID OF THE ANTINEOPLASTIC PROTEIN (ANUP) AS A PHARMACOLOGICALLY ACTIVE ANTI-TUMOR AGENT
    43.
    发明申请
    SIXTEEN AMINO ACID OF THE ANTINEOPLASTIC PROTEIN (ANUP) AS A PHARMACOLOGICALLY ACTIVE ANTI-TUMOR AGENT 失效

    公开(公告)号：US20020061851A1

    公开(公告)日：2002-05-23

    申请号：US08986606

    申请日：1997-12-08

    Inventor： NATHAN H. SLAONE

    IPC: A61K038/00 ,  C07K005/00 ,  C07K007/00 ,  C07K016/00 ,  C07K017/00 ,  A61K038/04 ,  A23J001/00 ,  C07K001/00 ,  C07K014/00

    CPC classification number: C07K14/47 ,  A61K38/10

    Abstract: The 16 amino acid peptide representing the partial N-terminal sequence of the Antineoplastic Protein (ANUP) is a highly active pharmacologically antitumor agent. The 16 amino acid peptide is about 50% as active as antitumor agent compared to the antitumor activity as the protein (ANUP) per se when tested as a tumor killer agent (in vitro) utilizing the human breast tumor cell line (MDA 231). The protein (ANUP) in the purified state also shows regression of both HeLa (human cervical tumor all line) and KB (human laryngeal cell line) implanted in nude mice (Sloane, Davis Tumor Targeting (1996) 2, pp 322-326. The nonapeptide is about 10% as active compared to the antineoplastic protein (ANUP) in the human breast tumor cell line in vitro assay system. Both peptides, the 9 amino acid peptide and the 16 amino acid peptide require presence of the detergent sodium dodecyl sulfate to activate the peptides for full pharmacological antitumor activity. The ANUP N-terminal 16 amino acid peptide contains the following sequence (as L-Amino Acids): 1 1.Pyroglu 2.LeuL 3.LysK 4.CysC 5.TyrY 6.ThrT 7.CysC 8.LysK 9.GluE 10.ProP 11.MetM 12.ThrT 13.SerS 14.AlaA 15.AlaA 16.CysC The use of the N-terminal Sixteen Amino Acid Peptide as a Pharmacologically Active Anti-tumor Agent

    Compounds with anti-KS and anti-HIV activity
    45.
    发明申请
    Compounds with anti-KS and anti-HIV activity 审中-公开
    具有抗KS和抗HIV活性的化合物

    公开(公告)号：US20040253608A1

    公开(公告)日：2004-12-16

    申请号：US10733323

    申请日：2003-12-12

    Applicant: Altachem Pharma Ltd.

    Inventor： Tony Antakly ,  Ram M. Sairam

    IPC: A61K038/00 ,  C12Q001/70 ,  A61K039/00 ,  C12Q001/68 ,  C07K017/00 ,  C07K014/00 ,  A01N037/18 ,  C07K016/00 ,  A61K039/21 ,  C07K005/00 ,  C07K007/00 ,  C07K001/00 ,  A61K038/04

    CPC classification number: A61K31/00 ,  A61K38/00 ,  C07K14/59 ,  Y10S530/834

    Abstract: The present invention relates to a compound having anti-KS and anti-HIV pharmaceutical activity which comprises an HCG-like inhibitory protein and fragments or derivatives thereof, said protein and fragments thereof are isolated from a biologically active fraction of APL-HCG, wherein said protein has a molecular weight of about 3,500 or of about 13,000 Dalton, and wherein said protein and fragments thereof are adsorbed polypropylene plastic supports. A pharmaceutical composition for the prevention and/or treatment of Kaposi's sarcoma (KS) and HIV which comprises an therapeutically effective amount of at least one compound of the present invention in association with a pharmaceutically acceptable carrier. A method for the prevention, treatment and/or reduction of Kaposi's sarcoma and HIV expression in AIDS patients, which consists in administering the composition to the patient.

    Abstract translation: 本发明涉及具有抗KS和抗HIV药物活性的化合物，其包含HCG样抑制蛋白及其片段或衍生物，所述蛋白质及其片段从APL-HCG的生物活性部分分离，其中所述 蛋白质具有约3,500或约13,000道尔顿的分子量，并且其中所述蛋白质及其片段吸附有聚丙烯塑料支持体。 一种用于预防和/或治疗卡波西氏肉瘤（KS）和HIV的药物组合物，其包含治疗有效量的至少一种本发明化合物与药学上可接受的载体。 一种预防，治疗和/或减少艾滋病患者卡波西氏肉瘤和艾滋病毒表达的方法，其中包括向患者施用组合物。

    Process for the preparation of perindopril, its analgous compounds and salts therof using 2,5 dioxo-oxazolidine intermediate compounds
    46.
    发明申请
    Process for the preparation of perindopril, its analgous compounds and salts therof using 2,5 dioxo-oxazolidine intermediate compounds 审中-公开
    使用2,5二氧代恶唑烷中间体化合物制备培哚普利，其化合物和盐的方法

    公开(公告)号：US20040248814A1

    公开(公告)日：2004-12-09

    申请号：US10484672

    申请日：2004-07-12

    Inventor： Pau Cid

    IPC: A61K038/04 ,  C07D209/12

    CPC classification number: C07D263/44 ,  C07C227/18 ,  C07K5/0222 ,  Y02P20/55 ,  C07C229/16

    Abstract: A process for the preparation of a compound of formula (IV), or an ester or a salt thereof comprising 1) reacting a compound of formula (I), (wherein Ra represents C1-4 alkyl, Rb represents C1-4 alkyl and Rc represents C1-6 alkyl) with a compound of formula X2Cnull0 (wherein each X independently represents a leaving group) to give a compound of formula (II), (wherein Ra, Rb and Rc are as hereinbefore defined); and 2) reacting said compound of formula (II) with a compound of formula (III) (wherein Rd represents hydrogen or a protecting group).

    Abstract translation: 一种制备式（IV）化合物或其酯或其盐的方法，其包括：1）使式（I）化合物（其中R a表示C 1-4烷基，R b表示C 1-4烷基和R c 代表C 1-6烷基）与式X2C = 0的化合物（其中每个X独立地表示离去基团），得到式（II）化合物，其中R a，R b和R c如上文所定义）; 和2）使式（II）化合物与式（III）化合物（其中Rd表示氢或保护基）反应。

    PREPARATION OF QUINAPRIL HYDROCHLORIDE
    50.
    发明申请
    PREPARATION OF QUINAPRIL HYDROCHLORIDE 失效
    喹啉盐酸盐的制备

    公开(公告)号：US20040192613A1

    公开(公告)日：2004-09-30

    申请号：US10806707

    申请日：2004-03-23

    Inventor： Sandra Marie Jennings

    IPC: A61K038/04 ,  C07D217/12

    CPC classification number: C07D217/26

    Abstract: Methods and materials for preparing quinapril, its pharmaceutically acceptable salts, including quinapril hydrochloride, are disclosed. The method includes reacting (2S,4S)-2-(4-methyl-2,5-dioxo-oxazolidin-3-yl)-4-phenyl-butyric acid ethyl ester with (3S)-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid tert-butyl ester to yield quinapril tert-butyl ester, which is subsequently reacted with an acid to yield quinapril or an acid addition salt of quinapril.

    Abstract translation: 公开了制备喹那普利及其药学上可接受的盐，包括盐酸喹那普的方法和材料。 该方法包括使（2S，4S）-2-（4-甲基-2,5-二氧代 - 恶唑烷-3-基）-4-苯基 - 丁酸乙酯与（3S）-1,2,3,4 - 四氢 - 异喹啉-3-甲酸叔丁酯，得到喹喔啉叔丁酯，随后与酸反应，得到喹那普利或喹那普利的酸加成盐。

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