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    Method of treating interferon non-responders using HCV protease inhibitor
    1.
    发明申请
    Method of treating interferon non-responders using HCV protease inhibitor 审中-公开
    使用HCV蛋白酶抑制剂治疗干扰素无应答者的方法

    公开(公告)号：US20070004635A1

    公开(公告)日：2007-01-04

    申请号：US11443868

    申请日：2006-05-31

    Applicant: Janice Albrecht ,  Mark Laughlin ,  Bruce Malcolm

    Inventor： Janice Albrecht ,  Mark Laughlin ,  Bruce Malcolm

    IPC: A61K38/08

    CPC classification number: A61K31/40 ,  A61K38/08 ,  C07K5/0802 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0812 ,  C07K5/1005 ,  C07K5/101 ,  C07K5/1016 ,  C07K7/06

    Abstract: A method of treating, preventing or ameliorating one or more symptoms associated with hepatitis C virus (HCV) in a patient in whom either the HCV is of Genotype 1 and/or the patient was previously treated with interferon and the previous interferon therapy was ineffective to treat the one or more symptoms associated with HCV, comprising administering to such a patient an effective amount of at least one compound of formulae I-XXVI of which the following structural formula is exemplary or a pharmaceutically acceptable salt, solvate or ester thereof. Optional combined administration of said at least one compound with an interferon or pegylated interferon and/or ribaviron is also contemplated.

    Abstract translation: 在丙型肝炎病毒（HCV）与丙型肝炎病毒（HCV）为基因型1和/或患者之前的治疗，预防或改善一种或多种与干扰素治疗有关的症状的方法，以前的干扰素治疗无效 治疗与HCV相关的一种或多种症状，其包括向所述患者施用有效量的至少一种下列结构式为其的式I-XXVI化合物或其药学上可接受的盐，溶剂合物或酯。 还考虑了所述至少一种化合物与干扰素或聚乙二醇化干扰素和/或ribaviron的任选组合给药。

    Immune regulating peptides and method of obtaining them
    3.
    发明授权
    Immune regulating peptides and method of obtaining them 有权
    免疫调节肽及其获得方法

    公开(公告)号：US6051683A

    公开(公告)日：2000-04-18

    申请号：US894963

    申请日：1998-08-17

    Applicant: Vladislav Isakovich Deigin ,  Andrei Marxovich Korotkov

    Inventor： Vladislav Isakovich Deigin ,  Andrei Marxovich Korotkov

    IPC: C07K5/08 ,  A61K38/00 ,  A61K38/08 ,  C07K5/02 ,  C07K5/065 ,  C07K5/072 ,  C07K5/083 ,  C07K5/087 ,  C07K5/09 ,  C07K5/093 ,  C07K5/097 ,  C07K5/10 ,  C07K5/103 ,  C07K5/107 ,  C07K5/113 ,  C07K5/117 ,  A61K38/04

    CPC classification number: C07K5/0821 ,  C07K5/0205 ,  C07K5/021 ,  C07K5/06104 ,  C07K5/0804 ,  C07K5/0812 ,  C07K5/0815 ,  C07K5/0819 ,  C07K5/0823 ,  C07K5/1005 ,  C07K5/1016 ,  C07K5/1021 ,  C07K5/1024 ,  A61K38/00

    Abstract: The invention relates to medicine, specifically, to methods of obtaining biologically active substances with immuno-regulating properties, and can be used in medicine and veterinary science and in experimental biochemistry. The fundamental problem addressed by the invention is that of producing a noval synthetic biologically active peptide with immuno-regulating properties and of the formula: X-Glu-Trp-Y, in which X is H or Gly, Ala, Leu, Ile, Val, NVal, Pro, Tyr, Phe, Trp, D-Ala, D-Leu, D-Ile, D-Val, D-NVal, D-Pro, D-Tyr, D-Phe, D-Trp, .gamma.-aminobutyric acid, .zeta.-aminocapronic acid; Y is Gla, Ala, Leu, Ile, Val, NVal, Pro, Tyr, Phe, Trp, D-Ala, D-Leu, D-Ile, D-Val, D-NVal, D-Pro, D-Tyr, D-Phe, D-Trp, .gamma.-aminobutyric acid .zeta.-aminocapronic acid, --OH, NH.sub.2,N.sub.2 H.sub.3, mono- or di-substituted amide (C.sub.1 -C.sub.3). Peptide synthesis takes place in a solution by successive growth of a chain from the C termination of the molecules, using a strategy of maximum blocking of functional groups, starting from amino acid alkyl ether, using the method of activating the ethers and the method of mixed anhydrides using tributyloxicarbonyl amino acid, with the proviso when X is H, Y is not OH.

    Abstract translation: PCT No.PCT / RU96 / 00046 Sec。 371日期1998年8月17日第 102（e）日期1998年8月17日PCT提交1996年2月28日PCT公布。 出版物WO96 / 26955 日期1996年9月6日本发明涉及药物，具体涉及获得具有免疫调节性质的生物活性物质的方法，可用于医药，兽医学和实验生物化学。 本发明解决的根本问题是制备具有免疫调节性质和式X-Glu-Trp-Y的诺瓦合成生物活性肽，其中X是H或Gly，Ala，Leu，Ile，Val ，NVal，Pro，Tyr，Phe，Trp，D-Ala，D-Leu，D-Ile，D-Val，D-NVal，D-Pro，D-Tyr，D-Phe，D-Trp，γ-氨基丁酸 酸，β-氨基己酸; Y是Gla，Ala，Leu，Ile，Val，NVal，Pro，Tyr，Phe，Trp，D-Ala，D-Leu，D-Ile，D-Val，D-NVal，D-Pro， D-Phe，D-Trp，γ-氨基丁酸ζ-氨基己酸，-OH，NH2，N2H3，单取代或二取代酰胺（C1-C3）。 通过使用从氨基酸烷基醚开始的功能基团的最大阻断的策略，使用活化醚的方法和混合的方法，通过从分子的C端连续生长链，在溶液中进行肽合成 使用三硫代羰基氨基酸的酸酐，条件是当X是H时，Y不是OH。

    Synthesis of peptides
    5.
    发明授权
    Synthesis of peptides 失效
    肽的合成

    公开(公告)号：US4217268A

    公开(公告)日：1980-08-12

    申请号：US926573

    申请日：1978-07-20

    Applicant: John L. Hughes ,  Jay K. Seyler ,  Robert C. Liu

    Inventor： John L. Hughes ,  Jay K. Seyler ,  Robert C. Liu

    IPC: A61K38/00 ,  C07K5/103 ,  C07K14/585 ,  C07C103/52 ,  A61K37/00 ,  C08F37/00

    CPC classification number: C07K5/1005 ,  C07K14/585 ,  A61K38/00

    Abstract: A new peptide is disclosed which has biological activity of the same type as known calcitonins and which has a shorter amino acid chain than natural calcitonins. Also resin peptides are disclosed which may be converted to peptides having such biological activity; and processes for producing said resin peptides and said calcitonin peptides.

    Abstract translation: 公开了一种新的肽，其具有与已知降钙素相同类型的生物活性，并且其具有比天然降钙素更短的氨基酸链。 还公开了可以转化成具有这种生物活性的肽的树脂肽; 以及用于制备所述树脂肽和所述降钙素肽的方法。

    Decapeptide analogs of somatostatin
    7.
    发明授权
    Decapeptide analogs of somatostatin 失效
    生长抑素的十肽类似物

    公开(公告)号：US4118380A

    公开(公告)日：1978-10-03

    申请号：US818500

    申请日：1977-07-25

    Applicant: Hans U. Immer ,  Nedumparambil A. Abraham

    Inventor： Hans U. Immer ,  Nedumparambil A. Abraham

    IPC: A61K38/00 ,  C07K5/083 ,  C07K5/103 ,  C07K14/655 ,  C07C103/52

    CPC classification number: C07K5/1005 ,  C07K14/655 ,  C07K5/0806 ,  A61K38/00 ,  Y10S930/16

    Abstract: Compounds of the formula 1 or 1a ##STR1##HSCH.sub.2 CH.sub.2 CO-A-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-NHCH.sub.2 CH.sub.2 SH (1a)in which A is Gly-Asn or Lys-Gly, or therapeutically acceptable salts thereof are disclosed. The compounds of formulae 1 and 1a are useful for the management of diabetes and the treatment of acromegaly in mammals. Compositions and methods for their use also are disclosed.

    Abstract translation: 式1或1a的化合物（1）HSCH2CH2CO-A-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-NHCH2CH2SH（1a）其中A是Gly-Asn或Lys-Gly，或 公开了其治疗上可接受的盐。 式1和1a的化合物可用于治疗糖尿病和哺乳动物肢端肥大症的治疗。 其使用的组合物和方法也被公开。

    Method for protecting guanidino group and restoring the same
    8.
    发明授权
    Method for protecting guanidino group and restoring the same 失效
    保护guanidino组和恢复相同的方法

    公开(公告)号：US3997516A

    公开(公告)日：1976-12-14

    申请号：US590948

    申请日：1975-06-27

    Applicant: Osamu Nishimura

    Inventor： Osamu Nishimura

    IPC: C07K1/02 ,  C07K1/06 ,  C07K5/103 ,  C07C103/52 ,  C07C63/00 ,  C07C149/40

    CPC classification number: C07K1/02 ,  C07K1/06 ,  C07K1/064 ,  C07K5/1005 ,  Y02P20/55

    Abstract: A guanidino group in an amino acid or a peptide can be protected with a specific protective group, i.e. lower alkoxybenzenesulfonyl group or tri-lower alkylbenzenesulfonyl group, and the protective group may easily be removed without affecting the amino acid or the peptide to be derived from the protected amino acid or peptide. Thus, the method is useful in the related chemical industries, especially in the peptide synthesis.

    Abstract translation: 氨基酸或肽中的胍基可以被特定的保护基保护，即低级烷氧基苯磺酰基或三低级烷基苯磺酰基，保护基可以容易地除去而不影响氨基酸或肽衍生的肽 被保护的氨基酸或肽。 因此，该方法在相关化学工业中尤其在肽合成中是有用的。

    Agonist analogues of luteinizing hormone releasing hormone
    9.
    发明授权
    Agonist analogues of luteinizing hormone releasing hormone 失效
    促黄体激素释放激素的激动剂类似物

    公开(公告)号：US3992365A

    公开(公告)日：1976-11-16

    申请号：US519667

    申请日：1974-10-31

    Applicant: Christopher Raymond Beddell ,  Lawrence Alfred Lowe ,  Samuel Wilkinson

    Inventor： Christopher Raymond Beddell ,  Lawrence Alfred Lowe ,  Samuel Wilkinson

    IPC: C07K14/575 ,  C07K1/113 ,  C07K5/103 ,  C07K7/23 ,  C07C103/52 ,  A61K37/00

    CPC classification number: C07K7/23 ,  C07K5/1005 ,  Y10S514/80 ,  Y10S930/13

    Abstract: Novel peptide compounds of the formulaGlu-His-X.sup.3 -X.sup.4 -X.sup.5 -X.sup.6 -X.sup.7 -X.sup.8 -Pro-Ware provided together with their acid addition salts and their complexes with pharmaceutically acceptable metals. The compounds are LH-RH analogues and together with their salts and complexes exhibit LH-RH agonist activity. In the formulaX.sup.3 and X.sup.5 are the same or different and each is phenylalanyl optionally substituted in the benzene ring;X.sup.4 and X.sup.6 are the same or different and each is selected from glycyl, alanyl (D- or L-) and asparaginyl;X.sup.7 is a radical of a neutral hydrophobic nonsulphur containing non-heterocyclic amino acid;X.sup.8 is a radical of a basic amino acid or is glycyl or phenylalanyl optionally substituted in the benzene ring; andW is selected from glycine amide and a group --NR.sup.1 R.sup.2.All references are to the L-amino acids and their radicals except in the case of glycine and unless otherwise stated.Also provided are methods for the preparation of the peptides, salts and complexes, pharmaceutical formulations containing them and methods for the preparation of such formulations, and methods for the use of the peptides, salts and complexes in human and in veterinary medicine.

    Abstract translation: 式Glu-His-X3-X4-X5-X6-X7-X8-Pro-W的新型肽化合物与它们的酸加成盐及其与药学上可接受的金属的络合物一起提供。 化合物是LH-RH类似物，并与它们的盐和配合物一起表现出LH-RH激动剂活性。 式X3和X5相同或不同，分别为在苯环中任意取代的苯丙氨酰基; X4和X6相同或不同，各自选自甘氨酰，丙氨酰（D-或L-）和天冬酰胺酰基; X7是含有非杂环氨基酸的中性疏水性非硫酸基团; X8是碱性氨基酸的基团，或在苯环中任选取代的甘氨酰或苯丙氨酰基; W选自甘氨酸酰胺和基团-NR1R2。

    Synthetic antigens of luteinizing hormone releasing hormone
    10.
    发明授权
    Synthetic antigens of luteinizing hormone releasing hormone 失效
    黄体激素释放激素的合成抗原

    公开(公告)号：US3963691A

    公开(公告)日：1976-06-15

    申请号：US512563

    申请日：1974-10-07

    Applicant: Carl H. Hoffman ,  Harvey Schwam ,  Stephen F. Brady ,  Martin Hichens ,  Ruth F. Nutt

    Inventor： Carl H. Hoffman ,  Harvey Schwam ,  Stephen F. Brady ,  Martin Hichens ,  Ruth F. Nutt

    IPC: A61K39/00 ,  C07K5/097 ,  C07K5/103 ,  C07K7/23 ,  C07C103/52 ,  C07G7/00

    CPC classification number: C07K5/0821 ,  C07K5/1005 ,  C07K7/23 ,  A61K39/00 ,  Y10S514/80 ,  Y10S530/812 ,  Y10S530/815 ,  Y10S930/13 ,  Y10S930/28

    Abstract: Synthetic antigens related to luteinizing hormone-releasing hormone (hereinafter designated LH-RH) having the amino acid composition, pyroglutamyl-histidyl-tryptophanylseryl-tyrosyl-glycyl-leucyl-arginyl-prolyl-glycyl-poly-L-lysine (hereinafter designated pyroglu-his-trp-ser-tyr-glyleu-arg-pro-gly-poly-L-lys) and poly-L-lysyl-glutarylhistidyl-tryptophanyl-seryl-tyrosyl-glycyl-leucyl-arginylprolyl-glycine amide (hereinafter designated poly-L-lysglutaryl-his-trp-ser-tyr-gly-leu-arg-pro-gly) are prepared by coupling the corresponding decapeptide with poly-L-lysine. The corresponding decapeptides are prepared by controlled stepwise procedures starting with individual amino acid components. These antigens have the property of inducing formation of antibodies to luteinizing hormone-releasing hormone (LH-RH) in animals.

    Abstract translation: 与具有氨基酸组成的促黄体激素释放激素（以下称为LH-RH）相关的合成抗原，焦谷氨酰 - 组氨酰基 - 色氨酰基 - 酰基 - 酪氨酰 - 甘氨酰 - 亮氨酰 - 精氨酰 - 脯氨酰 - 甘氨酰 - 聚-L-赖氨酸（以下称为pyroglu- his-trp-ser-tyr-glyleu-arg-pro-gly-poly-L-lys）和聚-L-赖氨酰 - 戊二酰基组氨酰基 - 色氨酸 - 丝氨酰 - 酪氨酰 - 甘氨酰 - 亮氨酰 - 炔丙基 - 甘氨酰胺（下文称为聚 - 通过将相应的十肽与聚-L-赖氨酸偶联来制备L-赖氨酰赖氨基-he-trp-ser-tyr-gly-leu-arg-pro-gly）。 相应的十肽通过从各个氨基酸组分开始的受控逐步方法制备。 这些抗原具有在动物体内诱导形成促黄体激素释放激素（LH-RH）的抗体的性质。

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