ECSP003557A - Erythropoietin derivatives - Google Patents
Erythropoietin derivativesInfo
- Publication number
- ECSP003557A ECSP003557A ECSP003557A ECSP003557A EC SP003557 A ECSP003557 A EC SP003557A EC SP003557 A ECSP003557 A EC SP003557A EC SP003557 A ECSP003557 A EC SP003557A
- Authority
- EC
- Ecuador
- Prior art keywords
- erythropoietin
- poly
- ethylene glycol
- glycoprotein
- group
- Prior art date
Links
- OXCMYAYHXIHQOA-UHFFFAOYSA-N potassium;[2-butyl-5-chloro-3-[[4-[2-(1,2,4-triaza-3-azanidacyclopenta-1,4-dien-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanol Chemical class [K+].CCCCC1=NC(Cl)=C(CO)N1CC1=CC=C(C=2C(=CC=CC=2)C2=N[N-]N=N2)C=C1 OXCMYAYHXIHQOA-UHFFFAOYSA-N 0.000 title abstract 3
- 102000003951 Erythropoietin Human genes 0.000 abstract 3
- 108090000394 Erythropoietin Proteins 0.000 abstract 3
- 229920001223 polyethylene glycol Polymers 0.000 abstract 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical group OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 abstract 2
- 101000987586 Homo sapiens Eosinophil peroxidase Proteins 0.000 abstract 2
- 101000920686 Homo sapiens Erythropoietin Proteins 0.000 abstract 2
- 230000013595 glycosylation Effects 0.000 abstract 2
- 238000006206 glycosylation reaction Methods 0.000 abstract 2
- 102000044890 human EPO Human genes 0.000 abstract 2
- 102000003886 Glycoproteins Human genes 0.000 abstract 1
- 108090000288 Glycoproteins Proteins 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 230000004071 biological effect Effects 0.000 abstract 1
- 210000002798 bone marrow cell Anatomy 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 210000003743 erythrocyte Anatomy 0.000 abstract 1
- 229940105423 erythropoietin Drugs 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
Landscapes
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente invención se refiere a conjugados de eritropoyetina con poli (etilen glicol) comprendiendo una glucoproteína eritropoyetina que presenta al menos un grupo amino libre y que presenta la actividad biológica in vivo que hace que las células de la médula ósea incrementen la producción de reticulositos y glóbulos rojos y que es selccionada delo grupo que consiste en eritropoyetina humana y análogos de la misma que tienen la secuencia de la eritropoyetina humana modificada mediante la dición de entre 1 y 6 sitios de glicosiliación o mediante una nueva disposición de al menos un sitio de glicosiliación; dicha glucoproteina estando covalentemente unida a "n" grupos de poli (etlenglicol) de la fórmula -CO-(CH2)x -(OCH2 CH2)m-OR con el carbonilo de cada grupo de poli (etilenglicol) formando un enlace amida con uno de dichos amino; en donde R es alquilo inferior; x es 2 ó 3; m se encuentra entre alrededor de 450 y alrededor de 900; n se encuentra entre 1 y 3; y n y m son elegidosde forma que el peso melecular del conjugado menos la glucoproteina eritropoyetina se encuentre entre 20 Kilodaltons y 100 kilodaltons.The present invention relates to conjugates of erythropoietin with poly (ethylene glycol) comprising an erythropoietin glycoprotein that has at least one free amino group and that exhibits biological activity in vivo that causes bone marrow cells to increase the production of reticulosites and red blood cells and which is selected from the group consisting of human erythropoietin and analogs thereof that have the human erythropoietin sequence modified by the provision of between 1 and 6 glycosylation sites or by a new arrangement of at least one glycosylation site ; said glycoprotein being covalently bound to "n" poly (ethylene glycol) groups of the formula -CO- (CH2) x - (OCH2 CH2) m-OR with the carbonyl of each poly (ethylene glycol) group forming an amide bond with one of said amino; wherein R is lower alkyl; x is 2 or 3; m is between about 450 and about 900; n is between 1 and 3; and n and m are chosen so that the melecular weight of the conjugate minus the erythropoietin glycoprotein is between 20 Kilodaltons and 100 kilodaltons.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP003557 ECSP003557A (en) | 2000-06-30 | 2000-06-30 | Erythropoietin derivatives |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP003557 ECSP003557A (en) | 2000-06-30 | 2000-06-30 | Erythropoietin derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP003557A true ECSP003557A (en) | 2001-01-23 |
Family
ID=42041171
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP003557 ECSP003557A (en) | 2000-06-30 | 2000-06-30 | Erythropoietin derivatives |
Country Status (1)
| Country | Link |
|---|---|
| EC (1) | ECSP003557A (en) |
-
2000
- 2000-06-30 EC ECSP003557 patent/ECSP003557A/en unknown
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