JP2015503512A5 - - Google Patents

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JP2015503512A5
JP2015503512A5 JP2014549075A JP2014549075A JP2015503512A5 JP 2015503512 A5 JP2015503512 A5 JP 2015503512A5 JP 2014549075 A JP2014549075 A JP 2014549075A JP 2014549075 A JP2014549075 A JP 2014549075A JP 2015503512 A5 JP2015503512 A5 JP 2015503512A5
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growth
releasing
pat
peptide
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JP6375089B2 (ja
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本発明は、その好ましい実施形態に関して説明されているが、前記実施形態は、本発明者らが現在知っているベストモードを構築する。種々の変化および修飾が、本願明細書に添付の特許請求の範囲において説明される本発明の範囲から逸脱することなくなされ得ることは、当業者に明らかであろう。例えば、ペプチド鎖における修飾、特に前記ペプチドのカルボキシル末端から始まる欠失および29位付近への伸長は、前記ペプチドの生物学的活性の全部または非常に実質的な部分を保持するペプチドまたはぺプチドのフラグメントを生成するために、現在までに公知の実験的実務に基づいてなされ得る。このようなペプチドは、本発明の範囲内であると見なされる。さらに、本発明の範囲から逸脱することなく、特許請求されたポリペプチドの活性の少なくとも実質的な部分を有する他の類似体を生成するために、付加が、いずれかの末端または両末端になされてもよく、および/または、一般的に同等の残基は、ペプチド化学の全分野において周知のように、自然に発生する残基に置換され得る。さらに、修飾は、今日のこの分野の情勢に基づいて、C末端における好ましい−−NH基になされてもよい。例えば、前記C末端でのアミノ酸残基のカルボキシル部分は、基−−COOR、−−CRO、−−CONHNHR、−−CON(R)(R’)、または−−CH2−ORであり得る。RおよびR’は、低級アルキル、フルオロ低級アルキル、または水素である。本発明から逸脱することなく、このような修飾については、同等の合成ペプチドをもたらす(Rivier 米国特許第5262519号明細書)。
この出願の発明に関連する先行技術文献情報としては、以下のものがある(国際出願日以降国際段階で引用された文献及び他国に国内移行した際に引用された文献を含む)。
(先行技術文献)
(特許文献)
(特許文献1) 中国特許出願公開第1328570号明細書
(特許文献2) 中国特許出願公開第1871020号明細書
(特許文献3) 欧州特許出願公開第0413839号明細書
(特許文献4) 米国特許第4,622,312号明細書
(特許文献5) 米国特許第4,649,131号明細書
(特許文献6) 米国特許第4,689,318号明細書
(特許文献7) 米国特許第4,784,987号明細書
(特許文献8) 米国特許第4,914,189号明細書
(特許文献9) 米国特許第5,262,519号明細書
(特許文献10) 米国特許第5,792,747号明細書
(特許文献11) 米国特許第5,846,936号明細書
(特許文献12) 米国特許第7,241,744号明細書
(特許文献13) 米国特許第7,268,113号明細書
(特許文献14) 米国特許第7,928,063号明細書
(特許文献15) 米国特許出願公開第2005/0261201号明細書
(特許文献16) 米国特許出願公開第2007/0042950号明細書
(特許文献17) 米国特許出願公開第2009/0023646号明細書
(特許文献18) 米国特許出願公開第2010/0092539号明細書
(特許文献19) 国際公開第03/037928号
(特許文献20) 国際公開第90/12810号
(特許文献21) 国際公開第94/11396号
(特許文献22) 国際公開第94/11397号
(特許文献23) 国際公開第96/22782号
(特許文献24) 国際公開第97/42223号
(特許文献25) 国際公開第2009/009727号
(特許文献26) 国際公開第2011/034976号
(特許文献27) 国際公開第2011/153491号
(非特許文献)
(非特許文献1) European Search Report for 12860298.4 dated September 28,2015
(非特許文献2) Armann et al.,"Quantification of basal and stimulated ROS levels as predictors of islet potency and function,"Am J Transplant,(2007),7:38−47.
(非特許文献3) Bajusz,et al.in Peptides,1982,Blaha and Melon,Eds.de Gruyter,Berlin−N.Y.,1983,pp.643−647.
(非特許文献4) Bonner−Weir,"In vitro cultivation of human islets from expanded ductal tissue,"Proc Natl Acad Sci USA,(July 5,2000),97(14):7999−8004.
(非特許文献5) Cai,et al.,"Synthesis of new potent agonistic analogs of growth hormone−releasing hormone(GHRH)and evaluation of their endocrine and cardiac activities,"Peptides(February 2014),52:104−112.Epub: December 25,2013.
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(非特許文献7) Campbell,et al.,"Rational Design,Synthesis,and Biological Evaluation of Novel Growth Hormone Releasing Factor Analogues,"Biopolymers(Peptide Science),(1995)Vol.37:67−88.
(非特許文献8) Corpas,et al.,"Growth Hormone (GH)−Releasing Hormone−(1−29) Twice Daily Reverses the Decreased GH and Insulin−Like Growth Factor−I Levels in Old Men,"J.Clin.Endacrin.Metabal.(1992),75,530−535.
(非特許文献9) Dor et al.,"Adult pancreatic B−cells are formed by self−duplication rather than stem−cell differentiation,"Nature,(May 6,2004),429:41−44.
(非特許文献10) Falutz,et al.,"Effects of Tesamorelin,a Growth Hormone−Releasing Factor,in HIV_Infected Patients with Abdominal Fat Accumulation: A Randomized Placebo−Controlled Trial With a Safety Extension,"Acquir Immune Defic Syndr.(2010),53: 311−322.
(非特許文献12) Felix,et al.,"Synthesis,biological activity and conformational analysis of cyclic GRF analogs,"Int.J.Peptide Protein Res.(December 1988),32(6): 441−454.
(非特許文献13) Ferninandi,et al.,"Non−Clinical Pharmacology and Safety Evaluation ofTH9507,a Human Growth Hormone−Releasing Factor Analogue,"Basic & Clin Pharmacol Toxicol.(2007),100: 49−58.
(非特許文献14) Fiaschi−Taesch et al.,"Hepatocyte Growth Factor Enhances Engraftment and Function of Nonhuman Primate Islets,"Diabetes,(October 2008),57:2745−2754.
(非特許文献15) Frohman,et al.,"Dipeptidylpeptidase IV and Trypsin−like Enzymatic Degradation of Human Growth Hormone−releasing Hormone in Plasma,"J.Clin.Invest.(1989),83,1533−1540.
(非特許文献16) Granata et al.,"Obestatin promotes survival of pancreatic beta−cells and human islets and induces expression of genes involved in the regulation of beta−cell mass and function,"Diabetes,(April 2008),57:967−979.
(非特許文献17) Granata et al.,"Growth hormone−releasing hormone promotes survival of cardiac myocytes in vitro and protects against ischaemia−reperfusion injury in rat heart,"Cardiovasc Res,(2009),83 :303−312.
(非特許文献18) Guarcello et al.,"Growth hormone releasing hormone receptors on thymocytes and splenocytes from rats,"Cell Immunol,(1991),136:291−902.
(非特許文献19) Havt et al.,"The expression of the pituitary growth hormone−releasing hormone receptor and its splice variants in normal and neoplastic human tissues,"Proc Natl Acad Sci USA(November 29,2005),102(48):17424−17429.
(非特許文献20) Houssay,"[Role of the hypophysis in carbohydrate metabolism and diabetes],"Folia Endoctrinol Mens Incretologia Incretoterapia,(1950) 3(2):127−136.
(非特許文献21) Huising et al.,"CRFRI is expressed on pancreatic B cells,promotes B cell proliferation,and potentiates insulin secretion in a glucose−dependent manner,"Proc Natl Acad Sci USA,(January 12,2010),107(2): 912−917.
(非特許文献22) Izdebski,et al.,"Synthesis and biological evaluation of superactive agonists of growth hormone releasing hormone,"Proc Natl Acad Sci USA,(May 1995),92:4872−4876.
(非特許文献23) Jabs et al.,"Reduced insulin secretion and content in VEGF−a deficient mouse pancreatic islets,"Exp Clin Endoctrinol Diabetes(2008),116 Suppl.1 :S45−49.
(非特許文献24) Kanashiro−Takeuchi et al.,"Cardioprotective effects of growth hormone−releasing hormone agonist after myocardial infarction,"Proc Natl Acad Sci USA,(February 9,2010),107(6):2604−2609.
(非特許文献25) Khorram et al.,"Effects of[Norleucine27]Growth Hormone−Releasing Hormone(GHRH)(1−29)−NH2 Administration on the Immune System of Aging Men and Women,"J Clin Endocrinol Metab,(1997),82(11):3590−3596.
(非特許文献26) Kirk,et al.,"Treatment with GHRH(1−29)NH2 in children with idiopathic short stature induces a sustained increase in growth velocity,"Clinical Endocrinol.(October 1994)41(4):487−493.
(非特許文献27) Kovacs,et al.,"An evaluation of intravenous,subcutaneous,and in vitro activity of new agmatine analogs of growth−hormone releasing hormone hGH−RW(1−29)NH2,"Life Science,(1988),42(1): 27−35.
(非特許文献28) Lehmann et al.,"Has time come for new goals in human islet transplantation?,"Am J Transplant,(2008),8: 1096−1100.
(非特許文献29) Letsch et al.,"Growth hormone−releasing hormone(GHRH)antagonists inhibit the proliferation of androgen−dependent and −independent prostate cancers,"Proc Natl Adac Sci USA,(February 4,2003),100(3):1250−1255.
(非特許文献30) Ling et al.,"Isolation,primary structure,and synthesis of human hypothalamic somatocrini: growth hormone−releasing factor,"Proc Natl Acad Sci USA,(1984),81 :4302−4306.
(非特許文献31) Merrifield,"Solid Phase Peptide Synthesis.I.The Synthesis of a Tetrapeptide,"J.Am.Chem.Soc.,(1963),85:2149.
(非特許文献32) Muranishi,et al.,"Lipophilic Peptides: Synthesis of Lauroyl Thyrotropin−Releasing Hormone and Its Biological Activity,"Pharm.Res.(May 1991),8(5)649−652.
(非特許文献33) Nielsen et al.,"Beta cell proliferation and growth factors,"J.Mol.Med.(1999),77:62−66.
(非特許文献34) Rekasi et al.,"Isolation and sequencing of cDNAs for splice variants of growth hormone releasing hormone receptors from human cancers,"Proc Natl Acad Sci USA,(September 12,2000),97(19):10561−10566.
(非特許文献35) Ross,et al.,"Treatment of Growth−Hormone Deficiency with Growth−Hormone−Releasing Hormone,"Lancet 1(January 3,1987),8523:5−8.
(非特許文献36) Schally et al.,"Agonistic Analogs of Growth Hormone−Releasing Hormone: Endocrine and Growth Studies,"Growth Hormone Secretagogues in Clinical Practice (1998),eds.Bercu and Walker,(Marcel Dekker,Inc.New York),131−143.
(非特許文献37) Shapiro et al.,"International trial of the Edmonton protocol for islet transplantation,"N Engl J Med,(2006),355:1318−1330.
(非特許文献38) Takano et al.,"Human growth hormone−releasing hormone(hGH−RH; hGRF)treatment of four patients with GH deficiency,"Endocrinol.Japan(1988)35(5); 775−781.
(非特許文献39) Thorner,et al.,"Acceleration of Growth in Two Children Treated with Human Growth Hormone−Releasing Factor,"N.Engl.J.Med.(January 3,1985),312(1):4−9.
(非特許文献40) Vance,"Growth−Hormone−Releasing Hormone,"Clin Chem,(1990),36:415−420.
(非特許文献41) Vance,"Growth hormone for the elderly?,"N.Eng.J.Med(1990),323(1):52−54.
(非特許文献42) Vasavada et al.,"Growth factors and beta cell replication,"Int J.Biochem Cell Biol,Epub 31,(August 2005),38(5−6):931−950.
(非特許文献43) Witkowska,et al.,"Tryptic Hydrolysis of hGH−RH(1−29)−NH2 Analogues Containing Lys or Orn in Positions 12 and 21,"J.Peptide Sci.7:166−172(2001).
(非特許文献44) Zarandi,et al.,"Synthesis and in vitro and in vivo activity of analogs of growth hormone releasing hormone(GH−RH)with C−terminal agmatine,"Int.J.Peptide Protein Res.(December 1990),36(6):499−505.
(非特許文献45) Zarandi,et al.,"Potent agonists of growth hormone−releasing hormone,"Int.J.Peptide Protein Res.39,1992,211−217.
(非特許文献46) Ziegler et al.,"Dehydroepiandrosterone induces a neuroendocrine phenotype in nerve growth factor−stimulated chromaffin pheochromocytoma PC12 cells,"Endocrinology,(2008),149:320−328.
(非特許文献47) Ziegler et al.,"Expression of neuropeptide hormone receptors in human adrenal tumors and cell lines: Antiproliferative effects of peptide analogues,"Proc Natl Acad Sci USA,(September 15,2009),106(37): 15879−15884.
(非特許文献48) International Search Report for PCT/US2012/067690 dated March 28,2013.
JP2014549075A 2011-12-21 2012-12-04 強力なアゴニスト作用を有する新規なgh−rh類似体 Expired - Fee Related JP6375089B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13/332,624 US9079974B2 (en) 2011-12-21 2011-12-21 GH-RH analogs with potent agonistic effects
US13/332,624 2011-12-21
PCT/US2012/067690 WO2013095903A1 (en) 2011-12-21 2012-12-04 Novel gh-rh analogs with potent agonistic effects

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JP2015503512A JP2015503512A (ja) 2015-02-02
JP2015503512A5 true JP2015503512A5 (ja) 2016-01-28
JP6375089B2 JP6375089B2 (ja) 2018-08-15

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US (2) US9079974B2 (ja)
EP (1) EP2794647B1 (ja)
JP (1) JP6375089B2 (ja)
KR (1) KR102117216B1 (ja)
CN (1) CN104520314B (ja)
AU (1) AU2012355743B2 (ja)
CA (1) CA2859675C (ja)
IL (1) IL233186B (ja)
MX (1) MX353869B (ja)
WO (1) WO2013095903A1 (ja)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9079974B2 (en) * 2011-12-21 2015-07-14 The University Of Miami GH-RH analogs with potent agonistic effects
WO2014100816A2 (en) * 2012-12-21 2014-06-26 University Of Miami Ghrh agonists for islet cell transplantation and function and the treatment of diabetes
US9855312B2 (en) * 2012-12-21 2018-01-02 University Of Miami GHRH agonists for the treatment of ischemic disorders
FR3020810B1 (fr) * 2014-05-06 2016-05-06 Servier Lab Nouveau sel de l'ivabradine et son procede de preparation.
PT3445778T (pt) 2016-04-19 2020-10-15 Griffon Pharmaceuticals Int Sa C/O Biopole Sa Péptidos bioativos peguilados e suas utilizações
CN107320718B (zh) * 2017-05-23 2020-12-11 余红 促生长激素释放激素激动剂在制备抗血管钙化药物中的应用
CN111407884B (zh) * 2019-06-24 2021-12-07 浙江大学 促生长激素释放激素激动剂ghrh-a在制备抗衰老药物中的用途

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