Permucous preparation
    5.
    发明授权
    Permucous preparation 失效
    允许的准备

    公开(公告)号:US06228836B1

    公开(公告)日:2001-05-08

    申请号:US09402886

    申请日:1999-10-18

    IPC分类号: A61K4726

    摘要: A composition for permucosal administration characterized by containing Antago-3 or a physiologically acceptable salt thereof, and a sucrose fatty acid ester. With the composition for permucosal administration of the invention there is provided a long-term stable preparation having the high permucosal absorption of physiologically active peptide Antago-3 without irritation.

    摘要翻译: 一种用于粘膜给药的组合物,其特征在于含有Antago-3或其生理学上可接受的盐,以及蔗糖脂肪酸酯。本发明的用于粘膜给药的组合物提供了具有生理学上高粘膜吸收的长期稳定的制剂 活性肽Antago-3无刺激。

    Microemulsion preparation containing a slightly absorbable substance
    6.
    发明授权
    Microemulsion preparation containing a slightly absorbable substance 失效
    含微量吸收物质的微乳液制剂

    公开(公告)号:US5948825A

    公开(公告)日:1999-09-07

    申请号:US537676

    申请日:1995-10-19

    IPC分类号: A61K9/107

    摘要: Microemulsion preparation in which a plurality of specified surfactants are combined such that aqueous-phase droplets that contain a physiologically active substance of low absorption and which have an average size of 0.4-100 nm are dispersed in an oil-phase dispersion medium. In order to improve its low transdermic or transmucosal absorbability, the physiologically active substance is allowed to be present as dissolved in the aqueous-phase droplets in the W/O emulsion. The preparation is low in local irritation and uses neither malodorous substances such as higher alcohols nor conventional absorption enhancers.

    摘要翻译: PCT No.PCT / JP94 / 00645 Sec。 371 1995年10月19日日期 102(e)日期1995年10月19日PCT 1994年4月19日PCT PCT。 第WO94 / 23749号公报 日期:1994年10月27日微乳液制剂,其中组合了多种特定的表面活性剂,使得含有低吸收性生理活性物质并且平均粒径为0.4-100nm的水相液滴分散在油相分散体 中。 为了改善其低透皮质或经粘膜吸收性,允许生理活性物质溶解在W / O乳液中的水相液滴中。 该制剂的局部刺激性低,既不使用高级醇等恶臭物质也不常用吸收促进剂。

    Biologically active agent having antihypertensive activity in mammals
    7.
    发明授权
    Biologically active agent having antihypertensive activity in mammals 失效
    在哺乳动物中具有抗高血压活性的生物活性剂

    公开(公告)号:US5122371A

    公开(公告)日:1992-06-16

    申请号:US665269

    申请日:1991-03-06

    IPC分类号: A61K35/12

    CPC分类号: A61K35/12 Y10S514/807

    摘要: A biologically active agent extracted from female breast cyst fluids displays anti-hypertensive activity in mammals. The agent is also useful in the treatment of congestive heart disease, artial fibrillation and idiopathic edema in mammals.

    摘要翻译: 从雌性乳腺囊肿液中提取的生物活性剂在哺乳动物中显示抗高血压活性。 该药物还可用于治疗充血性心脏病,哺乳动物的原纤维性颤动和特发性水肿。

    Linear derivatives of arginine vasopressin antagonists
    9.
    发明授权
    Linear derivatives of arginine vasopressin antagonists 失效
    ARGININE VASOPRESSIN ANTAGONISTS的线性衍生物

    公开(公告)号:US5055448A

    公开(公告)日:1991-10-08

    申请号:US66949

    申请日:1987-06-25

    摘要: Compounds acting as antagonists of the antidiuretic/and or vasopressor activity of arginine vasopressin are those of the formulaA--CH.sub.2 CO--D--Tyr(R)--Phe--Y--Asn--T--U--Z--Qwherein A is a-adamantyl, cyclohexyl, cyclopentyl, 1-mercaptocyclohexyl, 1-mercaptocyclopentyl, 1-ethyl-1-mercaptopropyl, yclohexylmethyl, cyclopentylmethyl, methyl, isopropyl, tert-butyl or phenyl; R is alkyl of 1-4 carbon atoms; Y is Val, Ile, Thr, Ala, Lys, Cha, Nva, Met, Nle, Orn, Ser, Asn, Gln, Phe, Tyr, Gly, Abu or Leu; T is Pen, Abu, Orn, Oys, Arg, Ala, Cha or Thr; U is Pro, Arg, Lys or Orn or a single bond; Z is (d-or L-) Arg, Orn or Lys and Q is Gly(NH.sub.2), Arg (NH.sub.2), Orn(NH.sub.2), Lys (NH.sub.2), (D- or L-)Ala(NH.sub.2), Ser(NH.sub.2), Val(NH.sub.2), Phe(NH.sub.2), Ile(NH.sub.2), Thr(NH.sub.2), Pro(NH.sub.2), Tyr(NH.sub.2), NH.sub.2, OH, NHR, NGbzl, NH(CH.sub.2).sub.p NH.sub.2 or NH(CH.sub.2).sub.p OH, wherein R is as above and p is an integer from 2 to 6. Compounds wherein T is Cys have similar activity.

    Novel arginine vasopressin-binding peptides
    10.
    发明授权
    Novel arginine vasopressin-binding peptides 失效
    新型精氨酸加压素结合肽

    公开(公告)号:US4786631A

    公开(公告)日:1988-11-22

    申请号:US169713

    申请日:1988-03-18

    摘要: The invention concerns novel AVP-binding peptides having the formula:Thr-Met-X-Val-Leu-Thr-Gly-Ser-Pro-Bwherein X is selected from the group consisting of Lys, Arg, and Asp; B is OH, NH.sub.2, NHAlk, wherein Alk is lower alkyl of 1-4 carbons, inclusive. These peptides block AVP function, and, therefore, are useful in many areas among which is the control of hypertension.

    摘要翻译: 本发明涉及具有下式的新型AVP结合肽:Thr-Met-X-Val-Leu-Thr-Gly-Ser-Pro-B,其中X选自Lys,Arg和Asp; B是OH,NH 2,NHAlk,其中Alk是1-4个碳的低级烷基,包括端值。 这些肽阻断AVP功能,因此在许多领域中是有用的,其中控制高血压。