Novel derivatives of arginine vasopressin antagonists
    91.
    发明授权
    Novel derivatives of arginine vasopressin antagonists 失效
    精氨酸加压素拮抗剂的新型衍生物

    公开(公告)号:US4714696A

    公开(公告)日:1987-12-22

    申请号:US574257

    申请日:1984-01-26

    摘要: Compounds acting as antagonists of the antidiuretic/and or vasopressor activity of arginine vasopressin are those of the formula ##STR1## wherein n is 4 or 5; X is (D- or L-)Tyr(R), D-Phe, D-Val, D-Leu, D-Ile, D-Nva, D-Nle, D-Cha, D-Abu, D-Thr, D-Asn, D-Met or D-Gln; Y is Val, Ile, Thr, Ala, Lys, Cha, Nva, Met, Nle, Orn, Ser, Asn, Gln, Phe, Tyr, Gly, Abu or Leu; Z is (D- or L-) Arg, Orn or Lys; Q is Arg(NH.sub.2), Ser(NH.sub.2), (D- or L-)Ala(NH.sub.2), Gly, OH or NH.sub.2 and R is methyl, ethyl, propyl or butyl; provided that, when Y is Gln or Val, R may also be H.

    摘要翻译: 作为精氨酸加压素的抗利尿和/或加压素活性的拮抗剂的化合物是下式的化合物,其中n为4或5; X是(D-或L-)Tyr(R),D-Phe,D-Val,D-Leu,D-Ile,D-Nva,D-Nle,D-Cha,D-Abu, D-Asn,D-Met或D-Gln; Y是Val,Ile,Thr,Ala,Lys,Cha,Nva,Met,Nle,Orn,Ser,Asn,Gln,Phe,Tyr,Gly,Abu或Leu; Z是(D-或L-)Arg,Orn或Lys; Q是Arg(NH2),Ser(NH2),(D或L)Ala(NH2),Gly,OH或NH2,R是甲基,乙基,丙基或丁基; 条件是当Y是Gln或Val时,R也可以是H.

    Oxytocin derivatives
    93.
    发明授权
    Oxytocin derivatives 失效
    催产素衍生物

    公开(公告)号:US4402942A

    公开(公告)日:1983-09-06

    申请号:US238715

    申请日:1981-02-27

    申请人: Per O. R. Melin

    发明人: Per O. R. Melin

    摘要: New oxytocin derivatives having an inhibitory effect on uterine contractions, pharmaceutical compositions containing the oxytocin derivatives, and use of the derivatives in the production of medicines are described. The derivatives are 1-deamino-(2-O-alkyltyrosine)-oxytocin of the formula ##STR1## wherein Mpa is a 3-mercaptopropionyl residue and X is an alkyl group having 2-4 carbon atoms, preferably an ethyl group. Apart from their inhibitory effect on vasopressin and oxytocin induced uterine contractions, the new oxytocin derivatives are capable of inhibiting the spontaneous contraction pattern of the uterus.

    摘要翻译: 描述了对子宫收缩具有抑制作用的新催产素衍生物,含有催产素衍生物的药物组合物及其衍生物在制备药物中的应用。 所述衍生物是式“IMAGE”的1-脱氨基 - (2-O-烷基酪氨酸) - 催产素,其中Mpa是3-巯基丙酰基残基,X是具有2-4个碳原子的烷基,优选乙基。 除了它们对加压素和催产素诱导的子宫收缩的抑制作用外,新的催产素衍生物能够抑制子宫的自发收缩模式。

    Antigen-protein complex for blocking allergic reactions
    94.
    发明授权
    Antigen-protein complex for blocking allergic reactions 失效
    用于阻断过敏反应的抗原蛋白复合物

    公开(公告)号:US4140679A

    公开(公告)日:1979-02-20

    申请号:US731414

    申请日:1976-10-12

    申请人: Arthur Malley

    发明人: Arthur Malley

    摘要: A multivalent complex suitable for blocking allergic reactions comprising (1) at least one Timothy antigen D fragment having the antigenic determinant structure: ##STR1## wherein: G represents glucose, andT represents threonine or a peptide linked to said structure through a threonine molecule;Covalently bonded through at least one glucose moiety to a peptide or protein, (2) a conjugate having the structure: ##STR2## OR (3) A CONJUGATE COMPRISING AT LEAST ONE CONJUGATE OF THE STRUCTURE: ##STR3## COVALENTLY BONDED TO A PROTEIN OR PEPTIDE BY A PEPTIDE LINKAGE THROUGH THE GLUTATHIONE MOIETY.A method of forming complex (1) by activating a glucose moiety of the Timothy antigen D fragment and reacting the thus activated intermediate with a peptide or protein.A method of treating allergies comprising injecting one of the above complexes into an individual to inhibit antigen-induced histamine release.An injectable composition for blocking allergic reactions containing the above complex.

    摘要翻译: 适用于阻断过敏反应的多价复合物,其包含(1)至少一种具有抗原决定簇结构的Timothy抗原D片段:其中:

    CARBETOCIN DRUG PRODUCT AND PROCESS FOR PREPARING SAME

    公开(公告)号:US20240091302A1

    公开(公告)日:2024-03-21

    申请号:US18511467

    申请日:2023-11-16

    摘要: The present disclosure includes a method of making an improved carbetocin drug product. The disclosed method for making an improved carbetocin drug product comprises agitating a carbetocin preparation containing an aqueous solution of carbetocin and one or more excipients for a period of to initiate the formation of aggregate-forming solids and filtering off the aggregates that form before further processing the remaining carbetocin into a final drug product. The present disclosure also relates to an improved carbetocin drug product, wherein the drug product is substantially free of aggregate-forming solids. The disclosed carbetocin drug product can be used for the treatment of a neurodevelopmental disorder, such as Präder-Willi syndrome. Additionally, the disclosed carbetocin drug product shows content uniformity of carbetocin over long periods of time before and after one or more free/thaw cycles, provides enhanced convenience and patient compliance, and/or are highly concentrated.