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14 条记录 (耗时 0.027 秒)

    HGH-RH(1-29)NH2 analogues having antagonistic activity
    1.
    发明授权
    HGH-RH(1-29)NH2 analogues having antagonistic activity 失效

    公开(公告)号：US5942489A

    公开(公告)日：1999-08-24

    申请号：US642472

    申请日：1996-05-03

    申请人： Andrew V. Schally ,  Marta Zarandi ,  Katalin Toth

    发明人： Andrew V. Schally ,  Marta Zarandi ,  Katalin Toth

    IPC分类号： A61K38/04 ,  A61K38/00 ,  A61P35/00 ,  C07K14/60 ,  A61K38/16 ,  A61K38/12 ,  C07K7/00 ,  C07K7/64

    CPC分类号： C07K14/60 ,  A61K38/00

    摘要： A peptide selected from the group having the formulae:.alpha.) X-R.sup.1 -R.sup.2 -R.sup.3 -R.sup.4 -R.sup.5 -R.sup.6 -Thr-R.sup.8 -R.sup.9 -R.sup.10 -R.sup.11 -R.sup.12 -Val-Leu-R.sup.15 -Gln-Leu-Ser-R.sup.19 -R.sup.20 -R.sup.21 -Leu-Leu-Gln-Asp-Ile-R.sup.27 -R.sup.28 -R.sup.29, wherein X is H, Ac, Aqc, IAc, BrProp, For, Ibu, Nac, 2-Nac, 1- or 2-Npt, 1- or 2-Npr, PhAc, Fpr, or any other aromatic or nonpolar acyl group, R.sup.1 is Tyr, His or Phe(Y), in which Y=H, F, Cl, Br, NO.sub.2, CH.sub.3 or OCH.sub.3, R.sup.2 is D-Arg, D-Cit, D-Har, D-Lys, D-Tic or D-Orn, R.sup.3 is Asp, D-Asp, Ala, D-Ala or Gly, R.sup.4 is Ala, Abu or Gly, R.sup.5 is Ile, Ala or Gly, R.sup.6 is Phe, Tic, Ala, Pro, Tpi, Nal or Phe(Y), in which Y=H, F, Cl, Br, NO.sub.2, NH.sub.2, CH.sub.3 or OCH.sub.3, R.sup.8 is Asn, Gln, Ser, Thr, Val, Leu, Ile, Ala, D-Ala, D-Asn, D-Gln, D-Thr, D-Leu, Abu, D-Abu, Nle, or Alb, R.sup.9 is Ser, R.sup.10 is Tyr or Phe(Y), in which Y=H, F, Cl, Br, NO.sub.2, CH.sub.3 or OCH.sub.3, R.sup.11 is Arg, D-Arg, or Cit, R.sup.12 is Lys, D-Lys, Cit, D-Cit, Orn, D-Orn, Nle or Ala, R.sup.15 is Gly, Ala, Abu or Gln, R.sup.19 is Ala or Abu, R.sup.20 is Arg, D-Arg or Cit, R.sup.21 is Lys, D-Lys, Orn or Cit, R.sup.27 is Met, Nle or Abu, R.sup.28 is Ser, Asn, Ala or Abu, R.sup.29 is Agm, Arg-NH.sub.2, Arg-OH, Cit-NH.sub.2, Cit-OH, Har-NH.sub.2 or Har-OH, and.beta.) X-A.sup.1 -B.sup.2 -A.sup.3 -R.sup.4 -R.sup.5 -R.sup.6 -Thr-A.sup.8 Ser-R.sup.10 -R.sup.11 -B.sup.12 -Val-Leu-R.sup.15 -A.sup.16 -A.sup.17 -Ser-R.sup.19 -B.sup.20 -B.sup.21 -Leu-Leu-Gln-A.sup.26 -Ile-R.sup.27 -R.sup.28 -R.sup.29, wherein a lactam bridge is formed between any one of the pairs of positions 1,2; 2,3; 8,12; 16,20; 17-21; 21,25; 25,29 or both 8,12 and 21,25 positions, and X is H, Ac, Aqc, IAc, BrProp, For, Ibu, Nac, 2-Nac, 1- or 2-Npt, 1- or 2-Npr, PhAc, Fpr, or any other aromatic or nonpolar acyl group, A is Glu, D-Glu, Gln, Asp, D-Asp, Asn, Abu, Leu, Tyr, His, Phe(Y), in which Y=H, F, cl, Br, NO.sub.2, NH.sub.2, CH.sub.3 or OCH.sub.3, Ser, Thr, Val, Ile, Ala, D-Ala, D-Asn, D-Gln, D-Thr, D-Leu, Abu, D-Abu, Nle, or Aib, B is Lys, D-Lys, Arg, D-Arg,Orn, D-Orn, or Agm; R.sup.4 is Ala, Abu or Gly, R.sup.5 is Ile, Ala or Gly, R.sup.6 is Phe, Tic, Tpi, Nal or Phe(Y), in which Y=H, F, Cl, Br, NO.sub.2, NH.sub.2 CH.sub.3 or OCH.sub.3, R.sup.10 is Tyr or Phe(Y), in which Y=H, F, Cl, Br, NO.sub.2, NH.sub.2 CH.sub.3 or OCH.sub.3, R.sup.15 is Gly, Ala, Abu or Gin, R.sup.27 is Met, Nle or Abu, R.sup.28 is Ser, Asn, Asp, Ala or Abu, and pharmaceutically acceptable salts thereof.

    Antagonistic analogs of GH-RH inhibiting IGF-I and -II
    2.
    发明授权
    Antagonistic analogs of GH-RH inhibiting IGF-I and -II 失效
    GH-RH抑制IGF-I和-II的拮抗类似物

    公开(公告)号：US07026281B1

    公开(公告)日：2006-04-11

    申请号：US09547215

    申请日：2000-04-11

    申请人： Andrew V. Schally ,  Jozsef Varga ,  Marta Zarandi

    发明人： Andrew V. Schally ,  Jozsef Varga ,  Marta Zarandi

    IPC分类号： A61K38/00

    CPC分类号： C07K14/60 ,  A61K38/00

    摘要： There is provided a novel series of synthetic analogs of hGH-RH(1–29)NH2. These analogs inhibit the activity of endogenous hGH-RH, and therefore prevent the release of growth hormone. The stronger inhibitory potencies of the new analogs, as compared to previously described ones, results from replacement of various amino acids.

    摘要翻译： 提供了一系列hGH-RH（1-29）NH 2的合成类似物。 这些类似物抑制内源性hGH-RH的活性，从而阻止生长激素的释放。 与之前描述的相比，新类似物的更强的抑制效力来自各种氨基酸的置换。

    Novel GH-RH analogs with potent agonistic effects
    3.
    发明申请
    Novel GH-RH analogs with potent agonistic effects 有权
    新型GH-RH类似物具有强烈的激动作用

    公开(公告)号：US20140058068A1

    公开(公告)日：2014-02-27

    申请号：US13332624

    申请日：2011-12-21

    申请人： Andrew V. Schally ,  Ren Zhi Cai ,  Marta Zarandi

    发明人： Andrew V. Schally ,  Ren Zhi Cai ,  Marta Zarandi

    IPC分类号： C07K14/61

    CPC分类号： C07K14/60 ,  A61K38/00 ,  C07K14/61

    摘要： There are provided a novel series of peptide analogs of hGH-RH(1-29)NH2 and hGH-RH(1-30)NH2 which show high activities in stimulating the release of pituitary GH in animals. They retain their physiological activity in solution for extended periods of time and resist enzymic degradation in the body. These novel and useful properties appear to be due to novel substitution patterns ant at the 1, 15, 27 and 29 positions on the peptide.

    摘要翻译： 提供了一系列hGH-RH（1-29）NH2和hGH-RH（1-30）NH2的肽类似物，其在刺激动物中垂体GH的释放方面表现出高的活性。 它们在溶液中保持长时间的生理活性，并抵抗体内酶降解。 这些新颖有用的性质似乎是由于肽上的1,15,27和29位的新型取代模式蚂蚁。

    Antagonistic analogs of GH RH (2003)
    4.
    发明授权
    Antagonistic analogs of GH RH (2003) 失效
    GH RH的拮抗类似物（2003）

    公开(公告)号：US07452865B2

    公开(公告)日：2008-11-18

    申请号：US10566776

    申请日：2004-07-26

    申请人： Andrew V. Schally ,  Jozsef Varga ,  Marta Zarandi ,  Ren Zhi Cai

    发明人： Andrew V. Schally ,  Jozsef Varga ,  Marta Zarandi ,  Ren Zhi Cai

    IPC分类号： A61K38/00 ,  A61K38/16 ,  A61K38/25 ,  C07K14/00

    CPC分类号： C07K14/60 ,  A61K38/00

    摘要： There is provided a novel series of synthetic antagonistic analogs of hGH-RH(1-29)NH2. These analogs inhibit the activity of endogenous hGH-RH on the pituitary GH-RH receptors, and therefore prevent the release of growth hormone. The analogs also inhibit the proliferation of human cancers through a direct effect on the cancer cells. The higher inhibitory potencies of the new analogs, as compared to previously described ones, results from replacement of various amino acids.

    摘要翻译： 提供了一系列hGH-RH（1-29）NH 2的合成拮抗类似物。 这些类似物抑制内源性hGH-RH对垂体GH-RH受体的活性，因此防止生长激素的释放。 类似物还通过对癌细胞的直接作用来抑制人类癌症的增殖。 与之前描述的相比，新类似物的更高的抑制效力来自各种氨基酸的替换。

    Novel N- and C- terminal substituted antagonistic analogs of GH-RH
    6.
    发明申请
    Novel N- and C- terminal substituted antagonistic analogs of GH-RH 有权
    GH-RH的新型N-和C-末端取代拮抗类似物

    公开(公告)号：US20130261055A1

    公开(公告)日：2013-10-03

    申请号：US12890626

    申请日：2010-09-25

    申请人： Andrew V. Schally ,  Marta Zarandi ,  Jozsef L. Varga ,  Ren Zhi Cai

    发明人： Andrew V. Schally ,  Marta Zarandi ,  Jozsef L. Varga ,  Ren Zhi Cai

    IPC分类号： A61K38/25 ,  A61P35/00 ,  A61K38/22

    CPC分类号： A61K38/25 ,  A61K38/00 ,  C07K14/60 ,  C07K14/645

    摘要： There is provided a novel series of synthetic analogs of hGH-RH(1-29)NH2 (SEQ ID NO: 96) and hGH-RH(1-30)NH2. Of particular interest are those carrying PhAc, N-Me-Aib, Dca, Ac-Ada, Fer, Ac-Amc, Me-NH-Sub, PhAc-Ada, Ac-Ada-D-Phe, Ac-Ada-Phe, Dca-Ada, Dca-Amc, Nac-Ada, Ada-Ada, or CH3—(CH2)10—CO-Ada, at the N-Terminus and β-Ala, Amc, Apa, Ada, AE2A, AE4P, ε-Lys(α-NH2), Agm, Lys(Oct) or Ahx, at the C-terminus. These analogs inhibit the release of growth hormone from the pituitary in mammals as well as inhibit the proliferation of human cancers, and inhibit the hyperplastic and benign proliferative disorders of various organs, through a direct effect on the cancerous and non-malignant cells. The stronger inhibitory potencies of the new analogs, as compared to previously described ones, result from replacement of various amino acids.

    摘要翻译： 提供了hGH-RH（1-29）NH2（SEQ ID NO：96）和hGH-RH（1-30）NH2的新一系列合成类似物。 特别感兴趣的是携带PhAc，N-Me-Aib，Dca，Ac-Ada，Fer，Ac-Amc，Me-NH-Sub，PhAc-Ada，Ac-Ada-D-Phe，Ac-Ada-Phe， Dca-Ada，Dca-Amc，Nac-Ada，Ada-Ada或CH 3 - （CH 2）10 -CO-Ada，在N-末端和β-Ala，Amc，Apa，Ada，AE2A，AE4P， Lys（α-NH2），Agm，Lys（Oct）或Ahx。 这些类似物通过对癌和非恶性细胞的直接作用，抑制哺乳动物垂体中生长激素的释放以及抑制人类癌症的增殖，并抑制各种器官的增生和良性增生性疾病。 与之前描述的相比，新类似物的更强的抑制效力是由于各种氨基酸的替换而产生的。

    N- and C- terminal substituted antagonistic analogs of GH-RH
    7.
    发明授权
    N- and C- terminal substituted antagonistic analogs of GH-RH 有权
    GH-RH的N-和C-末端取代的拮抗类似物

    公开(公告)号：US08691942B2

    公开(公告)日：2014-04-08

    申请号：US12890626

    申请日：2010-09-25

    申请人： Andrew V. Schally ,  Marta Zarandi ,  Jozsef L. Varga ,  Ren Zhi Cai

    发明人： Andrew V. Schally ,  Marta Zarandi ,  Jozsef L. Varga ,  Ren Zhi Cai

    IPC分类号： C07K14/60 ,  A61K38/25

    CPC分类号： A61K38/25 ,  A61K38/00 ,  C07K14/60 ,  C07K14/645

    摘要： There is provided a novel series of synthetic analogs of hGH-RH(1-29)NH2 (SEQ ID NO: 1) and hGH-RH(1-30)NH2. Of particular interest are those carrying PhAc, N-Me-Aib, Dca, Ac-Ada, Fer, Ac-Amc, Me-NH-Sub, PhAc-Ada, Ac-Ada-D-Phe, Ac-Ada-Phe, Dca-Ada, Dca-Amc, Nac-Ada, Ada-Ada, or CH3—(CH2)10—CO-Ada, at the N-Terminus and β-Ala, Amc, Apa, Ada, AE2A, AE4P, ε-Lys(α-NH2), Agm, Lys(Oct) or Ahx, at the C-terminus. These analogs inhibit the release of growth hormone from the pituitary in mammals as well as inhibit the proliferation of human cancers, and inhibit the hyperplastic and benign proliferative disorders of various organs, through a direct effect on the cancerous and non-malignant cells. The stronger inhibitory potencies of the new analogs, as compared to previously described ones, result from replacement of various amino acids.

    摘要翻译： 提供了一系列hGH-RH（1-29）NH2（SEQ ID NO：1）和hGH-RH（1-30）NH2的合成类似物。 特别感兴趣的是携带PhAc，N-Me-Aib，Dca，Ac-Ada，Fer，Ac-Amc，Me-NH-Sub，PhAc-Ada，Ac-Ada-D-Phe，Ac-Ada-Phe， Dca-Ada，Dca-Amc，Nac-Ada，Ada-Ada或CH 3 - （CH 2）10-CO-Ada，在N-Terminus和-Ab，-Ala，Amc，Apa，Ada，AE2A，AE4P， ; -Lys（α-NH2），Agm，Lys（Oct）或Ahx。 这些类似物通过对癌和非恶性细胞的直接作用，抑制哺乳动物垂体中生长激素的释放以及抑制人类癌症的增殖，并抑制各种器官的增生和良性增生性疾病。 与之前描述的相比，新类似物的更强的抑制效力是由于各种氨基酸的替换而产生的。

    Analogues of hGH-RH(1-29)NH.sub.2 having antagonistic activity
    9.
    发明授权
    Analogues of hGH-RH(1-29)NH.sub.2 having antagonistic activity 失效
    具有拮抗活性的hGH-RH（1-29）NH2的类似物

    公开(公告)号：US5550212A

    公开(公告)日：1996-08-27

    申请号：US168810

    申请日：1993-12-17

    申请人： Marta Zarandi ,  Andrew V. Schally

    发明人： Marta Zarandi ,  Andrew V. Schally

    IPC分类号： A61K38/04 ,  A61K38/00 ,  A61P3/00 ,  A61P3/08 ,  A61P3/10 ,  A61P5/00 ,  A61P13/02 ,  A61P15/00 ,  A61P27/02 ,  A61P35/00 ,  C07K14/60 ,  C07K7/00 ,  C07K7/10

    CPC分类号： C07K14/60 ,  A61K38/00

    摘要： Synthetic analogues of hGH-RH(1-29)NH.sub.2 having substitutions of various amino acids and acylated at the N-terminus, and exhibiting prolonged antagonistic duration. Embodiments include analogues of the formula: ##STR1## wherein X is nil, H, Ac, IAc, BrProp, Ibu, Nac, 2-Nac, 1- or 2-Npt, 1- or 2-Npr or Aqc; R.sup.1 is Tyr, His, Glu or Glt; R.sup.2 is D-Arg, D-Cit, D-Har, D-Lys or D-Orn; R.sup.3 is Asp, Ala or Gly; R.sup.4 is Ala or Gly; R.sup.5 is Ile, Ala or Gly; R.sup.6 is Phe, Ala, Pro, Tpi, Nal or Phe(Y), in which Y is F, Cl, Br, NO.sub.2, CH.sub.3 or OCH.sub.3 ; R.sup.8 is Asn, Ser, Val, Ile, Ala, Abu, Nle, or Aib; R.sup.11 is Arg, D-Arg or Cit; R.sup.12 is Lys, D-Lys, Cit or Ala; R.sup.15 is Gly, Ala, Abu or Gln; R.sup.19 is Ala or Abu; R.sup.20 is Arg, D-Arg or Cit; R.sup.21 is Lys, D-Lys or Cit; R.sup.27 is Met, Nle or Abu; R.sup.28 is Ser, Asn, Asp or Abu; R.sup.29 is Agm, Arg-NH.sub.2, Arg-OH, Cit-NH.sub.2, Cit-OH, Har-NH.sub.2 or Har-OH; provided that when R.sup.1 is Glt, X is nil and when X is H, R.sup.15 is other than Gly, and pharmaceutically acceptable acid addition salts thereof.

    摘要翻译： hGH-RH（1-29）NH2的合成类似物具有各种氨基酸的取代并且在N末端被酰化，并表现出延长的拮抗持续时间。 实施方案包括下式的类似物：X-R1-R2-R3-R4-R5-R6-Thr-R8-Ser-Tyr-R11-R12-Val-Leu-R15-Gln-Leu-Ser-R19-R20-R21 - Leu-Leu-Gln-Asp-Ile-R27-R28-R29，其中X为无，H，Ac，IAc，BrProp，Ibu，Nac，2-Nac，1或2-Npt，1或2-Npr 或Aqc; R1是Tyr，His，Glu或Glt; R2是D-Arg，D-Cit，D-Har，D-Lys或D-Orn; R3是Asp，Ala或Gly; R4是Ala或Gly; R5是Ile，Ala或Gly; R6是Phe，Ala，Pro，Tpi，Nal或Phe（Y），其中Y是F，Cl，Br，NO2，CH3或OCH3; R8是Asn，Ser，Val，Ile，Ala，Abu，Nle或Aib; R11为Arg，D-Arg或Cit; R12为Lys，D-Lys，Cit或Ala; R15是Gly，Ala，Abu或Gln; R19是Ala或Abu; R20是Arg，D-Arg或Cit; R21为Lys，D-Lys或Cit; R27是Met，Nle或Abu; R28为Ser，Asn，Asp或Abu; R29是Agm，Arg-NH2，Arg-OH，Cit-NH2，Cit-OH，Har-NH2或Har-OH; 条件是当R1为Glt时，X为零，当X为H时，R15为Gly以外的其药学上可接受的酸加成盐。