Salts of peptides with carboxy-terminated polyesters
    5.
    发明申请
    Salts of peptides with carboxy-terminated polyesters 审中-公开
    具有羧基封端的聚酯的肽的盐

    公开(公告)号:US20020198315A1

    公开(公告)日:2002-12-26

    申请号:US09988068

    申请日:2001-11-16

    Abstract: This invention relates to novel salts composed of a cation derived from a peptide containing at least one basic group and an anion derived from a carboxy-terminated polyester, processes for the manufacture of such salts, and the use of such salts in the manufacture of extended release pharmaceutical compositions. The salts of the invention possess a variety of properties which are useful in the formulation of extended release pharmaceutical compositions, whether the salts are in pure form or are in admixture with either an excess of the peptide in its free, unbound form or an excess of the free polyester.

    Abstract translation: 本发明涉及由衍生自含有至少一个碱性基团的肽和衍生自羧基封端的聚酯的阴离子的阳离子组成的新型盐,用于制备这种盐的方法,以及这些盐在制备延伸的 释放药物组合物。 本发明的盐具有多种性质,其可用于延长释放药物组合物的制剂中,无论该盐是纯形式还是与过量的肽以其游离,未结合形式或过量的 自由聚酯。

    Treatment of neuropsychiatric disorders
    7.
    发明授权
    Treatment of neuropsychiatric disorders 失效
    治疗神经精神障碍

    公开(公告)号:US5468726A

    公开(公告)日:1995-11-21

    申请号:US484146

    申请日:1990-02-23

    Inventor: Ramon Cacabelos

    Abstract: The administration of Somatostatin and growth hormone releasing factor at useful dosage levels alleviates the symptoms of various neuropsychiatric disorders.Growth hormone and neuropsychiatric responses to the administration of growth hormone releasing factor to mammals indicate its usefulness as an antemortem marker for senile dementia of the Alzheimer's type.

    Abstract translation: 在有用剂量水平下,生长抑素和生长激素释放因子的给药减轻了各种神经精神障碍的症状。 生长激素和向哺乳动物施用生长激素释放因子的神经精神反应表明其作为阿尔茨海默氏型老年性痴呆的抗衰老标记的有用性。

    Therapeutic somatostatin analogs
    8.
    发明授权
    Therapeutic somatostatin analogs 失效
    治疗性生长抑素类似物

    公开(公告)号:US4904642A

    公开(公告)日:1990-02-27

    申请号:US312138

    申请日:1989-02-17

    CPC classification number: C07K7/06 C07K14/6555 A61K38/00 Y10S514/806

    Abstract: An octapeptide of the formula: ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl), or R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H; A.sub.3 is CH.sub.2 -A.sub.6 (where A.sub.6 is pentafluorophenyl, naphthyl, pyridyl, or phenyl); A.sub.4 is o- m- or p-substituted X-Phe (where X is a halogen, H, NO.sub.2, OH, NH.sub.2, or C.sub.1-3 alkyl), pentafluoro-Phe, or .beta.-Nal; A.sub.5 is Thr, Ser, Phe, Val, .alpha.-aminobutyric acid, or Ile, provided that when A.sub.3 is phenyl, A.sub.1 is H, and A.sub.2 is H, A.sub.5 cannot be Val; and A.sub.7 is Thr, Trp, or .beta.-Nal; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 其中每个A1和A2独立地是H,C1-12烷基,C7-10苯基烷基,R1CO(其中R1是C1-20烷基,C3-20烯基,C3-20炔基,苯基 ,萘基或C7-10苯基烷基)或R2OCO(其中R2为C1-10烷基或C7-10苯基烷基),条件是当A1或A2之一为R1CO或R2OCO时,另一个必须为H; A3是CH2-A6(其中A6是五氟苯基,萘基,吡啶基或苯基); A4是间 - 或 - 对 - 取代的X-Phe(其中X是卤素,H,NO 2,OH,NH 2或C 1-3烷基),五氟-Phe或β-Nal; A5是Thr,Ser,Phe,Val,α-氨基丁酸或Ile,条件是当A3是苯基时,A1是H,A2是H,A5不能是Val; A7是Thr,Trp或β-Nal; 或其药学上可接受的盐。

    Bridged cyclic hexapeptide somatostatin analogs
    10.
    发明授权
    Bridged cyclic hexapeptide somatostatin analogs 失效
    桥连环六肽生长抑素类似物

    公开(公告)号:US4663435A

    公开(公告)日:1987-05-05

    申请号:US748069

    申请日:1985-06-24

    Inventor: Stephen F. Brady

    CPC classification number: C07K14/6555 A61K38/00 Y10S514/806 Y10S930/16

    Abstract: Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a bridged grouping which replaces eight of the ring amino acids of somatostatin. The bridged cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of selectively inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These bridged cyclic hexapeptides are prepared by the solid phase method.

    Abstract translation: 制备生长抑素类似物,其中环状六肽含有替代生长抑素的八个环氨基酸的桥连基团。 桥联的环六肽更容易合成,具有较长的活性持续时间,并且许多具有比生长抑素更高的活性水平。 该化合物具有选择性抑制胰高血糖素,生长激素和胰岛素释放的性质。 某些化合物还能够抑制胃酸分泌物的释放。 该化合物特别可用于治疗肢端肥大症,糖尿病,糖尿病性视网膜病变和消化性溃疡。 这些桥连环六肽通过固相法制备。

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