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    Modified glycoprotein hormones having a CTP at the amino terminus
    2.
    发明授权
    Modified glycoprotein hormones having a CTP at the amino terminus 失效
    在氨基末端具有CTP的修饰的糖蛋白激素

    公开(公告)号：US5792460A

    公开(公告)日：1998-08-11

    申请号：US419519

    申请日：1995-04-10

    Applicant: Irving Boime

    Inventor： Irving Boime

    IPC: A61K38/00 ,  C07K14/59 ,  C07K16/26 ,  A61K38/24

    CPC classification number: C07K16/26 ,  C07K14/59 ,  A61K38/00 ,  C07K2319/00 ,  Y10S930/11

    Abstract: "Partial" and "complete" CTP units are used to modify biologically active proteins and peptides to alter their clearance patterns. "Complete" CTP units have the amino acid sequence found at positions 112-118 to position 145 of the .beta.-subunit of human chorionic gonadotropin; "partial" CTP units are missing at least one amino acid in the region of position 118-145 inclusive. Variants of these CTP units contain 1-5 conservative amino acid substitutions which do not destroy activity. Suitable peptides or proteins which may be modified in this manner include various hormones and cytokines.

    Abstract translation: “部分”和“完整”CTP单位用于修饰生物活性蛋白质和肽以改变其清除模式。 “完全”CTP单元具有在人绒毛膜促性腺激素的β亚基的位置112-118至位置145处发现的氨基酸序列; “部分”CTP单位在118-145位置区域中缺少至少一个氨基酸。 这些CTP单元的变体含有1-5个保守氨基酸取代，其不破坏活性。 可以以这种方式修饰的合适的肽或蛋白质包括各种激素和细胞因子。

    LHRH antagonists
    5.
    发明授权
    LHRH antagonists 失效
    LHRH拮抗剂

    公开(公告)号：US4800191A

    公开(公告)日：1989-01-24

    申请号：US74126

    申请日：1987-07-17

    Applicant: Andrew V. Schally ,  Sandor Bajusz

    Inventor： Andrew V. Schally ,  Sandor Bajusz

    IPC: A61K38/04 ,  A61K31/00 ,  A61K38/00 ,  A61P15/00 ,  A61P15/18 ,  C07K1/02 ,  C07K1/04 ,  C07K1/113 ,  C07K7/23 ,  C07K14/59 ,  A61K37/43 ,  C07K7/20 ,  C08F283/00

    CPC classification number: C07K7/23 ,  A61K38/00 ,  Y10S514/80 ,  Y10S930/11 ,  Y10S930/12 ,  Y10S930/13

    Abstract: The present invention deals with LHRH antagonists which possess improved water solubility and while having the high antagonist potency of the basic peptides, are free of the edematogenic effects. These compounds are highly potent in inhibiting the release of gonadotropins from the pituitary gland in mammals, including humans.The compounds of this invention are represented by the formulaX-R.sup.1 -R.sup.2 -R.sup.3 -Ser-Tyr-R.sup.6 -Leu-Arg-Pro-R.sup.10 -NH.sub.2whereinX is an acyl group derived from straight or branched chain aliphatic or alicyclic carboxylic acids having from 1 to 7 carbon atoms,R.sup.1 is D- or L-Pro, D- or L- .DELTA. .sup.3 -Pro, D-Phe, D-Phe(4-H1), D-Ser, D-Thr, D-Ala, D-Nal (1) or D-Nal (2),R.sup.2 is D-Phe or D-Phe(4-H1)R.sup.3 is D-Trp, D-Phe, D-Pal, D-Nal(1) or D-Nal (2),R.sup.6 is D-Cit, D-Hci, D-Cit(Q) or D-Hci(Q) andR.sup.10 is Gly or D-Alawhere Q is lower alkyl of 1-3 carbon atoms and H1 is fluoro, chloro or bromo,and the pharmaceutically acceptable acid addition salts thereof and methods of use pertaining to these compounds.

    Abstract translation: 本发明涉及具有改善的水溶性并且具有高的拮抗剂碱性肽的效力的LHRH拮抗剂，没有水肿作用。 这些化合物在抑制哺乳动物（包括人）垂体腺中释放促性腺激素方面是非常有效的。 本发明的化合物由式X-R1-R2-R3-Ser-Tyr-R6-Leu-Arg-Pro-R10-NH2表示，其中X是衍生自直链或支链脂族或脂环族羧酸的酰基 具有1至7个碳原子，R1是D-或L-Pro，D-或L- DELTA 3-Pro，D-Phe，D-Phe（4-H1），D-Ser，D-Thr， Ala，D-Nal（1）或D-Nal（2），R2是D-Phe或D-Phe（4-H1）R3是D-Trp，D-Phe，D-Pal，D-Nal（1） 或D-Nal（2），R6是D-Cit，D-Hci，D-Cit（Q）或D-Hci（Q），R10是Gly或D-Ala，其中Q是1-3个碳原子的低级烷基 和H1是氟，氯或溴，以及其药学上可接受的酸加成盐和这些化合物的使用方法。

    Method of reducing mammalian fertility and drugs therefor
    8.
    发明授权
    Method of reducing mammalian fertility and drugs therefor 失效
    降低哺乳动物生殖力的方法及其药物

    公开(公告)号：US4081533A

    公开(公告)日：1978-03-28

    申请号：US719659

    申请日：1976-09-01

    Applicant: Dean W. Cheesman

    Inventor： Dean W. Cheesman

    IPC: A61K38/00 ,  A61K38/095 ,  C07K5/097 ,  A61K37/00 ,  C07C103/52

    CPC classification number: C07K5/0823 ,  A61K38/11 ,  Y10S514/807 ,  Y10S930/11 ,  Y10S930/15 ,  Y10S930/26

    Abstract: The pre-ovulatory surge of luteinizing hormone from the pituitary gland is selectively suppressed or eliminated by introducing nonapeptide, 8-arginine vasotocin, or the tripeptide, propyl-arginyl-glycinamide, into the subject. Analogs and related peptides also exhibit a similar inhibitory effect. This anovulatory effect in the female, or reduction in spermatogenesis in the male, results in loss of fertility.

    Abstract translation: 通过将非肽，8-精氨酸血管生成素或三肽，丙基 - 精氨酰 - 甘氨酰胺引入受试者，选择性地抑制或消除垂体中促黄体生成激素的排卵。 类似物和相关肽也表现出相似的抑制作用。 这种在女性中的排卵效应或男性精子发生的减少导致生育力丧失。

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