AR049149A1 - Analogos antagonistas de gh-rh - Google Patents
Analogos antagonistas de gh-rhInfo
- Publication number
- AR049149A1 AR049149A1 ARP040102755A ARP040102755A AR049149A1 AR 049149 A1 AR049149 A1 AR 049149A1 AR P040102755 A ARP040102755 A AR P040102755A AR P040102755 A ARP040102755 A AR P040102755A AR 049149 A1 AR049149 A1 AR 049149A1
- Authority
- AR
- Argentina
- Prior art keywords
- cit
- arg
- har
- hes
- ala
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title abstract 2
- ODKSFYDXXFIFQN-SCSAIBSYSA-N D-arginine Chemical compound OC(=O)[C@H](N)CCCNC(N)=N ODKSFYDXXFIFQN-SCSAIBSYSA-N 0.000 abstract 8
- -1 Arg Chemical compound 0.000 abstract 3
- AHLPHDHHMVZTML-SCSAIBSYSA-N D-Ornithine Chemical compound NCCC[C@@H](N)C(O)=O AHLPHDHHMVZTML-SCSAIBSYSA-N 0.000 abstract 2
- KDXKERNSBIXSRK-RXMQYKEDSA-N D-lysine Chemical compound NCCCC[C@@H](N)C(O)=O KDXKERNSBIXSRK-RXMQYKEDSA-N 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 abstract 1
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 1
- DCXYFEDJOCDNAF-UWTATZPHSA-N D-Asparagine Chemical compound OC(=O)[C@H](N)CC(N)=O DCXYFEDJOCDNAF-UWTATZPHSA-N 0.000 abstract 1
- MTCFGRXMJLQNBG-UWTATZPHSA-N D-Serine Chemical compound OC[C@@H](N)C(O)=O MTCFGRXMJLQNBG-UWTATZPHSA-N 0.000 abstract 1
- QNAYBMKLOCPYGJ-UWTATZPHSA-N D-alanine Chemical compound C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 abstract 1
- ZDXPYRJPNDTMRX-GSVOUGTGSA-N D-glutamine Chemical compound OC(=O)[C@H](N)CCC(N)=O ZDXPYRJPNDTMRX-GSVOUGTGSA-N 0.000 abstract 1
- COLNVLDHVKWLRT-MRVPVSSYSA-N D-phenylalanine Chemical compound OC(=O)[C@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-MRVPVSSYSA-N 0.000 abstract 1
- AYFVYJQAPQTCCC-STHAYSLISA-N D-threonine Chemical compound C[C@H](O)[C@@H](N)C(O)=O AYFVYJQAPQTCCC-STHAYSLISA-N 0.000 abstract 1
- 102000018997 Growth Hormone Human genes 0.000 abstract 1
- 108010051696 Growth Hormone Proteins 0.000 abstract 1
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 abstract 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 abstract 1
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- CKUAXEQHGKSLHN-UHFFFAOYSA-N [C].[N] Chemical compound [C].[N] CKUAXEQHGKSLHN-UHFFFAOYSA-N 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 230000000235 effect on cancer Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000000122 growth hormone Substances 0.000 abstract 1
- CSJDCSCTVDEHRN-UHFFFAOYSA-N methane;molecular oxygen Chemical compound C.O=O CSJDCSCTVDEHRN-UHFFFAOYSA-N 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000003884 phenylalkyl group Chemical group 0.000 abstract 1
- 230000001817 pituitary effect Effects 0.000 abstract 1
- 230000036515 potency Effects 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 230000035755 proliferation Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/60—Growth hormone-releasing factor [GH-RF], i.e. somatoliberin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Endocrinology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmacology & Pharmacy (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Genetics & Genomics (AREA)
- Animal Behavior & Ethology (AREA)
- Biophysics (AREA)
- Toxicology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Zoology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Gastroenterology & Hepatology (AREA)
- Diabetes (AREA)
- Analytical Chemistry (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
Se provee una serie de análogos antagonistas sintéticos de hGH-RH(1-29)NH2. Estos análogos inhiben la actividad de hGH-RH endogena en los receptores de GH-RH de la pituitaria y, por lo tanto, previenen la liberacion de la hormona de crecimiento. También los análogos inhiben la proliferacion de cánceres humanos a través de un efecto directo sobre las células cancerosas. Las potencias más altas de los nuevos análogos, en comparacion con los anteriores descritos, resulta del reemplazo de varios amino ácidos. Reivindicacion 1: Un péptido seleccionado del grupo que tiene la formula: R1-A0-A1-A2-Asp-Ala-A5-A6-Thr-A8-A9-A10-A11-A12-Val-Leu-A15-A16-Leu-Ser-A19-A20-A21-A22-Leu-Gln-Asp-IIe-A27-A28-A29-A30-R2, en que R1 es un miembro del grupo que consiste de a) PhAc, Hca, Dat, IndAc, Ipa, 1-Nac, 2-Nac, 1-Npr, 2-Npr, Ibu; CH3(CH2)nCO, o HOOC(CH2)nCO, en que n es un entero desde 2 hasta 20 y b) es cualquier otro grupo carbocíclico o heterocíclico aromático, de cadena recta, o cadena ramificada, saturado, insaturado o poli-insaturado, con desde 3 hasta 8 átomos de carbono, conteniendo al menos un átomo del grupo de S, N y O en el anillo heterocíclico, A0 es Phe, D-Phe, Arg, D-Arg, o un enlace simple carbono-nitrogeno, A1 es Tyr o Hes, A2 es D-Arg o D-Cit, A5 es IIe o Val, A6 es Phe, Tyr, Nal, o Phe(Y), en que Y=F, Cl, Br, o I, A8 es Asn, D-Asn, Cit, D-Cit, Gln, D-Gln, Ser, D-ser, Thr, D-Thr, Ala, D-Ala, Abu, D-Abu, o Aib, A9 es Hes, D-Hes, Amp, D-Amp, Gup o D-Gup, A10 es Tyr, Tyr(Et), Tyr(Me); Phe(Y), en que Y=H; F, Cl, Br, o I; Amp, Hes, Cha, Chg, Bpa, Dip, Trp, Trp(For), Tpi, 1-Nal, 3-Pal , 4-Pal, Phe(NH2), o Phe(NO2), A11 es Hes, D-Hes, Arg, D-Arg, Cit, Har, D-Har, Amp, D-Amp, Gup, o D-Gup, A12 es Lys, D-Lys, Orn, D-Orn, Har, D-Har, Cit, D-Cit, Nle, o Ala; A15 es Gly, Ala, Abu, Aib, Nle, Gln, Cit, o Hes; A16 es Gln o Arg; A19 es Ala o Abu; A20 es Hes, D-Hes, Arg, D-Arg, o Cit; A21 es Lys, D-Lys, Orn, D-Orn, Cit, o D-Cit; A22 es Leu, Ala o Aib; A27 es Met, Leu, Nle, Abu, o D-Arg; A28 es Arg, D-Arg, Har, D-Har, Ser, Asn, Asp, Ala, Abu, o Cit; A29 es Arg, D-Arg, Har, D-Har, Cit, D-Cit, o Agm, A30 es Arg, D-Arg, Har, D-Har, Cit, D-Cit, Agm, o es un enlace simple carbono-nitrogeno o carbono-oxígeno; R2 es -NH2, -NH-NH2, -NH-OH, -NHR3, -NR3R4, -OH, u -O3, en que R3 y R4 son cualquiera de alquil C1-10, alquenil C2-10, alquinil C2-10, fenilalquil C7-16, -C6H5, o -CH(C6H5)2; con la salvedad que si A29 es Agm, entonces A30 y R2 están ausentes y, si A30 es Agm, entonces R2 está ausente, y la sales farmacéuticamente aceptables de los mismos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US49270603P | 2003-08-05 | 2003-08-05 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR049149A1 true AR049149A1 (es) | 2006-07-05 |
Family
ID=34193144
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP040102755A AR049149A1 (es) | 2003-08-05 | 2004-08-03 | Analogos antagonistas de gh-rh |
Country Status (19)
Country | Link |
---|---|
US (1) | US7452865B2 (es) |
EP (1) | EP1651662A4 (es) |
JP (1) | JP2007526900A (es) |
KR (1) | KR20060088875A (es) |
CN (1) | CN1871020A (es) |
AR (1) | AR049149A1 (es) |
AU (1) | AU2004265280A1 (es) |
BR (1) | BRPI0413257A (es) |
CA (1) | CA2534436A1 (es) |
IL (1) | IL173201A0 (es) |
MX (1) | MXPA06001369A (es) |
NO (1) | NO20061060L (es) |
PL (1) | PL380437A1 (es) |
RS (1) | RS20060086A (es) |
RU (1) | RU2335506C2 (es) |
SG (1) | SG136958A1 (es) |
TW (1) | TW200517400A (es) |
WO (1) | WO2005016953A2 (es) |
ZA (1) | ZA200600966B (es) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2009108364A2 (en) * | 2008-02-27 | 2009-09-03 | Ipsen Pharma S.A.S. | Antagonistic analogues of ghrh |
US8691942B2 (en) | 2008-03-28 | 2014-04-08 | University Of Miami | N- and C- terminal substituted antagonistic analogs of GH-RH |
CN101983068B (zh) * | 2008-03-28 | 2014-12-24 | 迈阿密大学 | N末端和c末端取代的人gh-rh拮抗类似物 |
US8796216B2 (en) | 2008-06-12 | 2014-08-05 | Syntaxin Limited | Suppression of neuroendocrine diseases |
JP5799397B2 (ja) * | 2008-06-12 | 2015-10-28 | イプセン・バイオイノベーション・リミテッドIpsen Bioinnovation Limited | 癌の抑制 |
EP2719392B1 (en) * | 2008-06-12 | 2019-07-24 | Ipsen Bioinnovation Limited | Fusion proteins for use in the treatment of acromegaly |
US8227421B2 (en) * | 2009-09-17 | 2012-07-24 | University Of Miami | Fluorinated GHRH antagonists |
WO2011153491A2 (en) | 2010-06-03 | 2011-12-08 | University Of Miami | Agonists of growth hormone releasing hormone as effectors for survival and proliferation of pancreatic islets |
KR20140027284A (ko) | 2011-04-21 | 2014-03-06 | 쎄러테크놀로지스 인코포레이티드 | 성장 호르몬 방출 인자(grf) 유사체 및 이의 용도 |
US9079974B2 (en) * | 2011-12-21 | 2015-07-14 | The University Of Miami | GH-RH analogs with potent agonistic effects |
EP2866894A4 (en) * | 2012-06-27 | 2016-03-16 | Univ Miami | COMPOSITION AND METHOD FOR THE TREATMENT OF MORBUS ALZHEIMER |
EP2934565B1 (en) | 2012-12-21 | 2019-03-13 | University of Miami | Ghrh agonists for the treatment of ischemic disorders |
WO2014100816A2 (en) | 2012-12-21 | 2014-06-26 | University Of Miami | Ghrh agonists for islet cell transplantation and function and the treatment of diabetes |
WO2020163833A2 (en) | 2019-02-08 | 2020-08-13 | United States Government As Represented By The Department Of Veterans Affairs | Growth hormone-releasing hormone antagonists and uses thereof |
WO2021222129A1 (en) | 2020-04-27 | 2021-11-04 | The University Of Miami | Method of treating an inflammatory disorder |
CN114195881B (zh) * | 2021-12-16 | 2022-09-16 | 浙江湃肽生物股份有限公司 | 一种制备醋酸舍莫瑞林的方法 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5942489A (en) * | 1996-05-03 | 1999-08-24 | The Administrators Of The Tulane Educational Fund | HGH-RH(1-29)NH2 analogues having antagonistic activity |
US6057422A (en) * | 1998-11-25 | 2000-05-02 | The Administrators Of The Tulane Educational Fund | Antagonistic analogs of GH-RH inhibiting IGF-I and -II |
-
2004
- 2004-07-23 TW TW093121985A patent/TW200517400A/zh unknown
- 2004-07-26 SG SG200716961-8A patent/SG136958A1/en unknown
- 2004-07-26 MX MXPA06001369A patent/MXPA06001369A/es unknown
- 2004-07-26 WO PCT/US2004/024183 patent/WO2005016953A2/en active Application Filing
- 2004-07-26 CA CA002534436A patent/CA2534436A1/en not_active Abandoned
- 2004-07-26 CN CNA2004800222868A patent/CN1871020A/zh active Pending
- 2004-07-26 PL PL380437A patent/PL380437A1/pl unknown
- 2004-07-26 JP JP2006522602A patent/JP2007526900A/ja active Pending
- 2004-07-26 US US10/566,776 patent/US7452865B2/en not_active Expired - Fee Related
- 2004-07-26 RS YUP-2006/0086A patent/RS20060086A/sr unknown
- 2004-07-26 AU AU2004265280A patent/AU2004265280A1/en not_active Abandoned
- 2004-07-26 KR KR1020067002465A patent/KR20060088875A/ko active IP Right Grant
- 2004-07-26 RU RU2006106701/04A patent/RU2335506C2/ru not_active IP Right Cessation
- 2004-07-26 EP EP04757325A patent/EP1651662A4/en not_active Withdrawn
- 2004-07-26 BR BRPI0413257-2A patent/BRPI0413257A/pt not_active IP Right Cessation
- 2004-08-03 AR ARP040102755A patent/AR049149A1/es unknown
-
2006
- 2006-01-17 IL IL173201A patent/IL173201A0/en unknown
- 2006-02-02 ZA ZA200600966A patent/ZA200600966B/en unknown
- 2006-03-03 NO NO20061060A patent/NO20061060L/no not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
RS20060086A (en) | 2008-08-07 |
PL380437A1 (pl) | 2007-01-22 |
WO2005016953A2 (en) | 2005-02-24 |
CN1871020A (zh) | 2006-11-29 |
BRPI0413257A (pt) | 2006-10-03 |
ZA200600966B (en) | 2007-05-30 |
RU2335506C2 (ru) | 2008-10-10 |
NO20061060L (no) | 2006-05-03 |
EP1651662A2 (en) | 2006-05-03 |
IL173201A0 (en) | 2006-06-11 |
US7452865B2 (en) | 2008-11-18 |
JP2007526900A (ja) | 2007-09-20 |
AU2004265280A1 (en) | 2005-02-24 |
MXPA06001369A (es) | 2007-02-19 |
EP1651662A4 (en) | 2009-07-01 |
KR20060088875A (ko) | 2006-08-07 |
US20070042950A1 (en) | 2007-02-22 |
RU2006106701A (ru) | 2007-09-20 |
SG136958A1 (en) | 2007-11-29 |
WO2005016953A3 (en) | 2006-02-09 |
TW200517400A (en) | 2005-06-01 |
CA2534436A1 (en) | 2005-02-24 |
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Legal Events
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FB | Suspension of granting procedure |