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    Analgesic polypeptide
    41.
    发明授权
    Analgesic polypeptide 失效
    止痛多肽

    公开(公告)号：US4196122A

    公开(公告)日：1980-04-01

    申请号：US812039

    申请日：1977-07-01

    Applicant: Dimitrios Sarantakis

    Inventor： Dimitrios Sarantakis

    IPC: A61K38/00 ,  C07K14/70 ,  C07C103/52 ,  A61K37/00

    CPC classification number: C07K14/702 ,  A61K38/00 ,  Y10S514/809

    Abstract: The polypeptides of the formula: ##STR1## in which X is hydrogen, Arg, Lys or Orn;X.sup.5 is a D-.alpha.-amino acid;R is hydrogen, methyl, allyl or cyclopropylmethyl;andR.sup.2 is --OH, --NH.sub.2 or --NHC.sub.n H.sub.2n+1 wheren is 1, 2, 3 or 4or a pharmaceutically acceptable salt thereof, exert an analgesic effect in warm-blooded animals when peripherally administered.

    Abstract translation: 下式的多肽：其中X是氢，Arg，Lys或Orn; X5是D-α-氨基酸; R是氢，甲基，烯丙基或环丙基甲基; R2为-OH，-NH2或-NHCnH2n + 1，其中n为1,2,3或4或其药学上可接受的盐，在外周施用时，在温血动物中发挥镇痛作用。

    Novel tricosapeptides, intermediates therefor and pharmaceutical compositions and methods employing said tricosapeptides
    42.
    发明授权
    Novel tricosapeptides, intermediates therefor and pharmaceutical compositions and methods employing said tricosapeptides 失效
    新型三环肽，其中间体以及使用所述三肽多肽的药物组合物和方法

    公开(公告)号：US4127536A

    公开(公告)日：1978-11-28

    申请号：US807211

    申请日：1977-06-16

    Applicant: David H. Coy ,  Abba J. Kastin

    Inventor： David H. Coy ,  Abba J. Kastin

    IPC: A61K38/00 ,  C07K14/675 ,  C08L37/00 ,  A61K37/00 ,  C07C103/52

    CPC classification number: C07K14/6755 ,  A61K38/00 ,  Y10S514/809 ,  Y10S930/12 ,  Y10S930/28

    Abstract: Novel tricosapeptides having the following amino acid sequenceH-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-Phe-Lys-Asn-Ala-Ile-Ile-Ywherein: X is a chiral residue of a D-amino acid selected from the group consisting of D-alanine, D-leucine, D-isoleucine, D-valine, D-phenylalanine, D-tyrosine, D-tryptophan, D-serine, D-threonine, D-methionine, D-glutamic acid, D-glutamine, D-proline D-aspartic acid, D-asparagine, D-lysine, D-arginine and D-histidine; and Y is selected from the group consisting of hydroxy, amino, loweralkylamino, diloweralkylamino and lower alkoxy; and the pharmaceutically acceptable salts thereof; intermediates useful in making the novel compounds; and pharmaceutical compositions and methods employing the novel compounds.

    Abstract translation: 具有以下氨基酸序列H-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-Ph e-Lys-Asn的新型三肽 -Ala-Ile-Ile-Y其中：X是D-氨基酸的手性残基，其选自D-丙氨酸，D-亮氨酸，D-异亮氨酸，D-缬氨酸，D-苯丙氨酸，D-酪氨酸 ，D-色氨酸，D-丝氨酸，D-苏氨酸，D-甲硫氨酸，D-谷氨酸，D-谷氨酰胺，D-脯氨酸D-天冬氨酸，D-天冬酰胺，D-赖氨酸，D-精氨酸和D-组氨酸; Y选自羟基，氨基，低级烷基氨基，二低级烷基氨基和低级烷氧基; 及其药学上可接受的盐; 用于制备新型化合物的中间体; 以及使用该新化合物的药物组合物和方法。

    Novel pentadecapeptides, intermediates therefor, and compositions and methods employing said pentadecapeptides
    43.
    发明授权
    Novel pentadecapeptides, intermediates therefor, and compositions and methods employing said pentadecapeptides 失效
    新的十五肽，其中间体，以及使用所述十五肽的组合物和方法

    公开(公告)号：US4127527A

    公开(公告)日：1978-11-28

    申请号：US807139

    申请日：1977-06-16

    Applicant: David H. Coy ,  Abba J. Kastin

    Inventor： David H. Coy ,  Abba J. Kastin

    IPC: A61K38/00 ,  C07K14/67 ,  C08L37/00 ,  A61K37/00 ,  C07C103/52

    CPC classification number: C07K14/672 ,  A61K38/00 ,  Y10S514/809

    Abstract: Novel pentadecapeptides having the following amino acid sequence.H-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Ywherein: X is a chiral residue of a D-amino acid selected from the group consisting of D-alanine, D-leucine, D-isoleucine, D-valine, D-phenylalanine, D-tyrosine, D-tryptophan, D-serine, D-threonine, D-methionine, D-glutamic acid, D-glutamine, D-proline D-aspartic acid, D-asparagine, D-lysine, D-arginine and D-histidine; and Y is selected from the group consisting of hydroxy, amino, loweralkylamino, diloweralkylamino and lower alkoxy; and the pharmaceutically acceptable salts thereof; intermediates useful in making the novel compounds; and pharmaceutical compositions and methods employing the novel compounds.

    Abstract translation: 具有以下氨基酸序列的新型十五肽。

    Novel triacontapeptides, intermediates therefor and pharmaceutical compositions and methods employing said triacontapeptides
    45.
    发明授权
    Novel triacontapeptides, intermediates therefor and pharmaceutical compositions and methods employing said triacontapeptides 失效
    新型三十肽，其中间体以及采用所述三烯肽的药物组合物和方法

    公开(公告)号：US4127522A

    公开(公告)日：1978-11-28

    申请号：US807128

    申请日：1977-06-16

    Applicant: David H. Coy ,  Abba J. Kastin

    Inventor： David H. Coy ,  Abba J. Kastin

    IPC: A61K38/00 ,  C07K14/675 ,  C08L37/00 ,  A61K37/00 ,  C07C103/52

    CPC classification number: C07K14/6755 ,  A61K38/00 ,  Y10S514/809 ,  Y10S930/12 ,  Y10S930/28

    Abstract: Novel triacontapeptides having the following amino acid sequenceH-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-Phe-Lys-Asn-Ala-Ile-Ile-Lys-Asn-Ala-Tyr-Lys-Lys-Gly-Ywherein: X is a chiral residue of a D-amino acid selected from the group consisting of D-alanine, D-leucine, D-isoleucine, D-valine, D-phenylalanine, D-tyrosine, D-tryptophan, D-serine, D-threonine, D-methionine, D-glutamic acid, D-glutamine, D-proline, D-aspartic acid, D-asparagine, D-lysine, D-arginine and D-histidine; and Y is selected from the group consisting of hydroxy, amino, loweralkylamino, diloweralkylamino and lower alkoxy; and the pharmaceutically acceptable salts thereof; intermediates useful in making the novel compounds; and pharmaceutical compositions and methods employing the novel compounds.

    Abstract translation: 具有以下氨基酸序列H-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-Ph e-Lys-Asn的新型三十多肽 -Ala-Ile-Ile-Lys-Asn-Ala-Tyr-Lys-Lys-Gly-Y其中：X是D-氨基酸的手性残基，其选自D-丙氨酸，D-亮氨酸，D - 异亮氨酸，D-缬氨酸，D-苯丙氨酸，D-酪氨酸，D-色氨酸，D-丝氨酸，D-苏氨酸，D-甲硫氨酸，D-谷氨酸，D-谷氨酰胺，D-脯氨酸，D-天冬氨酸，D 天冬氨酸，D-赖氨酸，D-精氨酸和D-组氨酸; Y选自羟基，氨基，低级烷基氨基，二低级烷基氨基和低级烷氧基; 及其药学上可接受的盐; 用于制备新型化合物的中间体; 以及使用该新化合物的药物组合物和方法。

    Octadecapeptides, intermediates therefor, and compositions and methods employing said octadecapeptides
    46.
    发明授权
    Octadecapeptides, intermediates therefor, and compositions and methods employing said octadecapeptides 失效
    十八肽，其中间体，以及使用所述十八肽的组合物和方法

    公开(公告)号：US4127519A

    公开(公告)日：1978-11-28

    申请号：US807121

    申请日：1977-06-16

    Applicant: David H. Coy ,  Abba J. Kastin

    Inventor： David H. Coy ,  Abba J. Kastin

    IPC: A61K38/00 ,  C07K14/675 ,  C08L37/00 ,  A61K37/00 ,  C07C103/52

    CPC classification number: C07K14/6755 ,  A61K38/00 ,  Y10S514/809 ,  Y10S930/12 ,  Y10S930/28

    Abstract: Novel octadecapeptides having the following amino acid sequenceH-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-Phe-Ywherein: X is a chiral residue of a D-amino acid selected from the group consisting of D-alanine, D-leucine, D-isoleucine, D-valine, D-phenylalanine, D-tyrosine, D-tryptophan, D-serine, D-threonine, D-methionine, D-glutamic acid, D-glutamine, D-proline D-aspartic acid, D-asparagine, D-lysine, D-arginine and D-histidine; and Y is selected from the group consisting of hydroxy, amino, loweralkylamino, diloweralkylamino and lower alkoxy; and the pharmaceutically acceptable salts thereof; intermediates useful in making the novel compounds; and pharmaceutical compositions and methods employing the novel compounds.

    Abstract translation: 具有以下氨基酸序列H-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-Phe-Y的新型十八肽其中：X 是D-氨基酸的手性残基，其选自D-丙氨酸，D-亮氨酸，D-异亮氨酸，D-缬氨酸，D-苯丙氨酸，D-酪氨酸，D-色氨酸，D-丝氨酸，D- 苏氨酸，D-甲硫氨酸，D-谷氨酸，D-谷氨酰胺，D-脯氨酸D-天冬氨酸，D-天冬酰胺，D-赖氨酸，D-精氨酸和D-组氨酸; Y选自羟基，氨基，低级烷基氨基，二低级烷基氨基和低级烷氧基; 及其药学上可接受的盐; 用于制备新型化合物的中间体; 以及使用该新化合物的药物组合物和方法。

    Purification of enkephalin, an endogenous composition in the human body and synthesis of same
    47.
    发明授权
    Purification of enkephalin, an endogenous composition in the human body and synthesis of same 失效
    人参皂甙，人体内源性组合物的纯化及其合成

    公开(公告)号：US4105651A

    公开(公告)日：1978-08-08

    申请号：US666647

    申请日：1976-03-15

    Applicant: John Hughes

    Inventor： John Hughes

    IPC: A61K38/00 ,  C07K14/70 ,  C07C103/52 ,  A61K37/00

    CPC classification number: C07K14/70 ,  A61K38/00 ,  Y10S514/809

    Abstract: The purification of an endogenous composition isolated from mammalian brain tissue and termed enkephalin ("in the head"). Enkephalin is recovered from brain tissue by acetone solution and purified by means of column and thin layer chromatography. The composition which is a mixture of two pentapeptides, namely, (a) H-Tyr-Gly-Gly-Phe-Met-OH and (b) H-Tyr-Gly-Gly-Phe-Leu-OH wherein the ratio of a:b is from 3:1 to 4:1 has been found to be a non-addictive narcotic and an opiate agonist.The synthesis of the pentapeptide composition from the known structure above is accomplished by conventional solution techniques of protection of the amino groups, such as t-butyloxycarbonyl, benzyloxycarbonyl, and t-amyloxycarbonyl, or the solid phase peptide synthesis of R. Bruce Merrifield using a polymeric support and the same or similar amine protecting groups.

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