Pharmaceutical combinations containing an inhibitor of platelet aggregation and a fibrate
    21.
    发明申请
    Pharmaceutical combinations containing an inhibitor of platelet aggregation and a fibrate 审中-公开
    含有血小板聚集抑制剂和贝特类药物的药物组合

    公开(公告)号:US20090062240A1

    公开(公告)日:2009-03-05

    申请号:US11658501

    申请日:2005-07-25

    IPC分类号: A61K31/60

    摘要: The present invention relates to a novel pharmaceutical combination, containing an inhibitor of platelet aggregation and a fÊbrate, where the inhibitor of platelet aggregation is preferably either aspirin or clopidogreL Such a pharmaceutical combination of an inhibitor of platelet aggregation and a fÊbrate is expected to be useful in the treatment and/or prevention of myocardial infarction (heart attack), cardiac arrest, peripheral vascular disease (including symptomatic carotid artery disease), congestive heart failure, ischemic heart disease, angina pectoris (including unstable angina), sudden cardiac death, unstable angina, as well as cerebrovascular events such as cerebral infarction, cerebral thrombosis, cerebral ischemia and transient ischemic attack, disorders related to bypass operations (angioplasty), fitting of endovascular prostheses and restenosis, and inflammatory disorders, including arthritic conditions such as rheumatoid arthritis and osteoarthritis, as well as asthma or related airway or respiratory inflammatory disorders.

    摘要翻译: 本发明涉及含有血小板聚集抑制剂和血小板聚集的抑制剂的新型药物组合,其中血小板聚集抑制剂优选为阿司匹林或氯吡格雷。预期血小板聚集抑制剂和磷脂酰胆碱的药物组合是有用的 在治疗和/或预防心肌梗塞(心脏病发作),心脏停搏,外周血管疾病(包括症状性颈动脉疾病),充血性心力衰竭,缺血性心脏病,心绞痛(包括不稳定型心绞痛),心源性猝死,不稳定 心脑血管事件以及脑血栓事件如脑梗死,脑血栓形成,脑缺血和短暂性脑缺血发作,与旁路手术相关的疾病(血管成形术),血管内修复术和再狭窄的适应性,以及炎性疾病,包括关节炎病症如类风湿性关节炎和 骨关节炎,以及哮喘 或相关的气道或呼吸道炎症性疾病。

    Serine protease genes related to DPPIV
    22.
    发明授权
    Serine protease genes related to DPPIV 有权
    与DPPIV相关的丝氨酸蛋白酶基因

    公开(公告)号:US07157241B2

    公开(公告)日:2007-01-02

    申请号:US10982512

    申请日:2004-11-05

    CPC分类号: C12N9/48 C12N2799/026

    摘要: Novel proteins or polypeptides having significant sequence homology to DPPIV, nucleic acids coding therefor, cells which have been modified with such nucleic acid so as to express these proteins, antibodies to these proteins, screening methods for the discovery of new therapeutic agents which are inhibitors of the activity of these proteins or of related proteins, and therapeutic agents discovered by such screening methods, as well as new therapeutic treatments, are all provided.

    摘要翻译: 与DPPIV具有显着序列同源性的新型蛋白质或多肽,其编码的核酸,已经用此类核酸修饰以表达这些蛋白质的细胞,对这些蛋白质的抗体,用于发现作为这些蛋白质的抑制剂的新治疗剂的筛选方法 这些蛋白质或相关蛋白质的活性以及通过这种筛选方法发现的治疗剂以及新的治疗方法都被提供。

    Kappa receptor opioid peptides
    23.
    发明授权
    Kappa receptor opioid peptides 失效
    卡帕受体阿片样肽

    公开(公告)号:US5965701A

    公开(公告)日:1999-10-12

    申请号:US997208

    申请日:1997-12-23

    摘要: Peptides which exhibit high selectivity for the kappa opioid receptor (KOR) and long duration of peripheral action without significant entry into the brain are created which are sequences of four D-isomer amino acid residues having a C-terminus which is a mono or di-substituted amide. Representative compounds, which have an affinity for the KOR at least 1,000 times their affinity for the mu opioid receptor and an ED.sub.50 of not greater than about 0.5 mg/kg, includeH-D-Phe-D-Phe-D-Nle-D-Arg-NHEt,H-D-Phe-D-Phe-D-Nle-D-Arg-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NHPr,H-D-Phe-D-Phe-D-Nle-D-Arg-thiomorpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NEt.sub.2,H-D-Phe-D-Phe-D-Nle-D-Arg-NHMe,H-D-Phe-D-Phe-D-Leu-D-Orn-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NHhEt,H-D-Phe-D-Phe-D-Nle-D-Arg-NH-cyclopropyl,H-D-Ala(2Thi)-D-4Cpa-D-Leu-D-Arg-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-piperidinyl,H-D-Phe-D-Phe-D-Leu-D-Orn-NHEt,H-D-Phe-D-Phe-D-Leu-D-Lys-morpholinyl,andH-D-Phe-D-Phe-D-Nle-D-Arg-piperazinyl.

    摘要翻译: 产生对κ阿片样物质受体(KOR)具有高选择性且长期持续的外周作用而不显着进入脑的肽是具有C末端的四个D-异构体氨基酸残基的序列,其是单或二 - 取代的酰胺。 对KOR具有至少1,000次对μ阿片受体的亲和力和不大于约0.5mg / kg的ED 50的亲和力的代表性化合物包括H-D-Phe-D-Phe-D-Nle-D- Arg-NHEt,HD-Phe-D-Phe-D-Nle-D-Arg-吗啉基,HD-Phe-D-Phe-D-Nle-D-Arg-NH-4-吡啶甲基,HD-Phe- Phe-D-Nle-D-Arg-NHPr,HD-Phe-D-Phe-D-Nle-D-Arg-硫代吗啉基,HD-Phe-D-Phe-D-Nle-D-Arg-NEt2, Phe-D-Phe-D-Nle-D-Arg-NHMe,HD-Phe-D-Phe-D-Leu-D-Orn-吗啉基,HD-Phe-D-Phe-D-Nle-D-Arg- NHhEt,HD-Phe-D-Phe-D-Nle-D-Arg-NH-环丙基,HD-Ala(2Thi)-D-4Cpa-D-Leu-D-Arg-吗啉基,HD-Phe-D-Phe -D-Nle-D-Arg-哌啶基,HD-Phe-D-Phe-D-Leu-D-Orn-NHEt,HD-Phe-D-Phe-D-Leu-D-Lys-吗啉基和H-D -Phe-D-Phe-D-Nle-D-Arg-哌嗪基。

    Propanamines, their pharmacological properties and their application for
therapeutic in particular antidiarrheal, purposes
    25.
    发明授权
    Propanamines, their pharmacological properties and their application for therapeutic in particular antidiarrheal, purposes 失效
    丙氨酸,其药理学特性及其在特异性抗病毒治疗中的应用,目的

    公开(公告)号:US5143938A

    公开(公告)日:1992-09-01

    申请号:US660873

    申请日:1991-02-26

    摘要: A compound which is a propanamine of general formula (I) ##STR1## in which: R1 is a phenyl radical optionally mono-, di- or trisubstituted,or is a 5- or 6-membered monocyclic heteroaryl radical in which the single heteroatom is nitrogen, oxygen or sulfur,R2 is a lower alkyl radical,R3 and R4 are a hydrogen atom or a lower alkyl, lower alkenyl or lower cycloalkylalkyl radical,or, together with the nitrogen atom to which they are attached, form a saturated 5- to 6-membered heterocycle comprising only one heteroatom,R5 is a 5- to 7-membered cycloalkyl radical, a phenyl radical or a 5- or 6-membered monocyclic heteroaryl radical,and W representsa group .dbd.CH--QH,or a heterocycle .dbd.C[Q--(CH2)n--Q],or a group .dbd.C.dbd.Q, in which groupsQ is an oxygen or sulfur atom,n has the value 2 or 3,W being .dbd.C.dbd.Q only when R3 and R4 are not both hydrogen, and their additions salts with pharmaceutically acceptable acids.A pharmaceutical composition comprising a compound of general formula (I) with the above definitions for the treatment of diarrheal states.

    摘要翻译: 作为通式(I)的丙胺的化合物,其中:R 1是任选被一个,二或三取代的苯基,或是5或6元单环杂芳基,其中 单个杂原子是氮,氧或硫,R2是低级烷基,R3和R4是氢原子或低级烷基,低级烯基或低级环烷基烷基,或者与它们相连的氮原子一起形成 饱和的5至6元杂环,仅包含一个杂原子,R 5为5-至7-元环烷基,苯基或5-或6-元单环杂芳基,W表示基团= CH-QH, 或杂环= C [Q-(CH 2)nQ]或基团= C = Q,其中基团Q是氧或硫原子,n具有值2或3,W仅当R 3为 和R4不同时为氢,并且它们与药学上可接受的酸相加。 一种药物组合物,其包含具有上述定义用于治疗腹泻状态的通式(I)的化合物。