HUE029926T2 - Pegilált rekombináns humán növekedésihormon-vegyületek - Google Patents
Pegilált rekombináns humán növekedésihormon-vegyületek Download PDFInfo
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- HUE029926T2 HUE029926T2 HUE09738181A HUE09738181A HUE029926T2 HU E029926 T2 HUE029926 T2 HU E029926T2 HU E09738181 A HUE09738181 A HU E09738181A HU E09738181 A HUE09738181 A HU E09738181A HU E029926 T2 HUE029926 T2 HU E029926T2
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- hgh
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Claims (7)
- Pagtláfi rakorrtbináns humán növekedésibormon-vagyClletak SZABADALM* IGÉNYPONTOK1, Gyógyszerkészítmény, amely tartalmaz alkalmas kötőanyagokat, és tártál» mázzá egy rekombináns humán növekedésihormon (recombinant human growth hormone; rhGH}-PEGIIáli~prodrug~könjugatum ember szamara ín vivo klinikailag hatékony mennyiségét is, amelyben a REG az rhGH-hoz egy önhidroiizálható (önhasadé) tranziens kötőelemen keresztül kapcsolódik; a prodrug-kónjugátum azzal Jellem« m% hogy (1) : a konjugátum olyan GH-aktivitással rendelkezik, hogy ez a natív PEG-mentes növekedésihormon 5%-áná! kisebb; és (2) : a kötőelem autohktrollzis sebessége olyan mértékű, hogy az in viva felezési idő — amelyet a konjugátumnak patkányokba való intravénás injektálásával, és ezt követően idöintervallumonkénti vérminták vételével, plazma preparálásával és EÜSÄ alkalmazásával végzett hGH-analízissel mérünk.......10 érától 600 óráig terjed; és amelyben a PEGilálbprodmg-konjugátum kémiai szerkezete; aholHN-rhGH a tranziens kötőelemhez kapcsolt rhGH-maradékot jelenti; az R1, R2, R3, R4 és R5 csoportokat egymástól függetlenül a hidrogénatom, mell!-, etil-, propil», izopropii», buti!-, izobutik ferc-hutil-csoportok közül választjuk; REG a tranziens kötőelemhez kapcsolt pegiléiásí maradékot jelenti; n « 1 vagy 2; és az X csoportot az 1-8 szanatomos aikil- vagy az 1-12 szénatornos heteroaikil-csöportok közül választjuk ki; és aboi a PEG elágazó, és legalább 3 láncot, tartalmaz. 2„ Az 1. igénypont szerinti gyógyszerkészítmény, amelyben az autöhidrolízis sebessége olyan mértékű, bogy az ín vívó felezési idő legfeljebb ötször rövidebb, mint a megfelelő hGH-PEGílált-prodrug-konjugátum írt vitro felezési ideje. 3.A 2, igénypont szerinti gyógyszerkészítmény, ameiyben az in vivo felezési idő legfeljebb háromszor rövidebb, mint a megfelelő hGH-PEGilált-prGdryg-konjugá-tum in vitro felezési ideje. 4x A 2, vagy 3. igénypont szerinti gyógyszerkészítmény, amelyben min vivo felezés? Idő legfeljebb kétszer rövidebb, mint a megfelelő hGH-PEGiíált-prodrug-kon-jugátum in viiro felezési ideje, vagy ezzel majdnem megegyező.
- 8, Az 1-4. igénypontok egyike szerinti gyógyszerkészítmény, aböl a készítmény egy szuhkután beadásra, intramuszkuláris beadásra vagy intravénás injektálásra szolgáié készítmény. ff, Az 1-5. Igénypontok egyike szennti gyógyszerkészítmény, ahoi a PEGiiált--prodrugnak a növekedésihormon molekulára vonatkoztatott össz-PEG-terheíése legalább 25 köa-t tesz ki7, Az 1-6, igénypontok egyike szerinti gyógyszerkészítmény, aboí az 1 igénypont (A) szerkezeti képletében szereplő {1} rész-szerkezeti képletet, amelyazáíta! alkotott csoportból választjuk ki. B. Az 1-7. Igénypontok egyike szerinti gyógyszerkészítmény, ahol az 1 igénypont (A) szerkezeti képletében szereplő (II) rész-szerkezeti képletet, amelyazáltal alkotott csoportból választjuk ki. 9« Az 1 -8, igénypontok egyike szerinti gyógyszerkészítmény, ahol az 1, igénypont (A) kepietéhen szereplő PEG-X az egy (Ili) képietü PEG-W:ahol a PEG-W csoportot azáltal alkotott csoportból választjuk ki, 1ö. Az 1-6. igénypontok egyike szerinti gyógyszerkészítmény, ahol a prod rúg--konjugátum szerkezete:
- 11. Az előző igénypontok egyike szerinti gyógyszerkészítmény, amelyben a kötőelem önhasadási sebessége in vivo olyan mértékű, hogy az ín vivő felezési idő 20 órétói 3GÖ óráig terjed.
- 12, Az előző igénypontok egyike szerinti gyógyszerkészitmény, amelyben a kötőelem önhasadásí sebessége in vívó olyan mértékű, hogy az in vivő felezési idő 20 órától 180 óráig terjed.
- 13, Az előző igénypontok egyike szerinti gyógyszerkészítmény, amelyben a kötőelem oohasadiSÍ sebessége ín vivő olyan mértékű, hogy az in vivo felezési idő 30 órától 100 őrig terjed.
- 14, Az előző igénypontok egyike szerinti gyógyszerkészítmény, amelyben a kötőelem önhasadási sebessége in vivő olyan mértékű, hegy az m vivő felezési idő 30 őrstől 75 óráig terjed,
- 15, Az 1-14. igénypontok bármelyike szerinti gyógyszerkészítmény kíiníkaiiag hafises mennyisége, egy GH-vii összefüggő betegségnek emberben való kezelésére szolgáló eljárásban való alkalmazásra, ahol a betegséget a növekedésibormon-híány, felnőttkorban jelentkező növekedésíhormon-hiány; 'furnér szindróma; Prader-áAfílli szindróma; röyidbéí szindróma; krónikus veseelégíelenség; éfeikofleli aía-csonynövés (small for gestational age, 86A); AIDS-wasting; öregedés elleni védelem; rheumatoid arthritis, idiopâtias alacsonynövés; short stature homeobox gén; somatöpause; Noonan szindróma; csontváz dysplasia; Down szindróma; huzamos sztéroîd alkalmazáshoz köthető alaosonynövés; Aarskog szindróma; krónikus vese-betegség; latiikofi rleumatöíd arthritis; cisztás fíbrózís; HAART kezelésben része-sitt gyerekbén fél lépő Hi\Afertôzès; nagyon kissúilyal születeti, SGA-ban nem szenvedő gyerekek alaesonynövése; csontváz dysplasie; hypochondroplasia; achondroplasia; Idiopátiás alacsonynövés; GHD felnőttekben; bosszú csontok tőrése vagy ezeken belüli tőrés; szivacsos csontok törése vagy ezeken belüli törés; in vagy ínszalag műtéten átesett betegek; distraction osteogenesis; csípő vagy porckorong pótlásból eredő rendellenességek, meni&zkusz javítás, gerincfúziók vagy protézis rögzítés; oszteoszíntézises anyagok rögzítéséből eredő rendellenességek; törések forradásának hiánya vagy forradás-hibák; osteoatomía-eredetü rendellenességek; impianfatumok beültetéséből származó betegségek; sérülés vagy arthritis okozta Izületi porc-degeneráöió a tirdben; osteoporosis Turner szindrómába szenvedő betegekben; osteoporosis férfiakban; felnőtt betegek krónikus dialízisben (adui patients in chromo dialysis, APÓD); alultápláltsághoz kötött szív-érrendszeri betegség APÓD esetén; sorvadás visszatérése APCD-beö; APCD-heli rák; krónikus obstruktiv tüdő-betegség APOD-beo; HÍV APCD-ben; idős emberik APCD-vei; krónikus májbefeg- ség APCD-ben; kimerülés szindróma APCD-ben: Crohn-betegség; májfunkcio-zavár; férfiak HÍV fertőzéssé!; rövidbe! szindróma; centrális el bizottság; HIV-asszocíált lipodisztrófia szindróma; féríimeddóség; nagy választott sebészeti beavatkozáson átesett betegek, alkohol vagy gyógyszer detoxtfikáiás; neurológiai sérülés; öregedés; törékeny idős emberek; osteoadhitis; traumaiikusan károsult poré; érékeié-díszfunkoló; fybromyeígla; memóriazavarok; depresszió; traumatikus agysérülés; subarachnoid vérzés; nagyon alacsony születési súly; metaboiikys szindróma; glucocorticoid myopathia; és glucocorticoid kezelésen átesett gyerekek alaesonynö-vése közül választjuk, 1.8» Prodrug, amelyet aahol m egy 200 és 250 közötti egész szám, és n egy 100 és 125 közötti egész szám;ahol n egy 400 és 500 közötti egész szám; î ahol n egy 400 és 500 közötti egész szám;és a ahol n egy 400 és 000 közötti egész szám,által alkotott csoportból választunk.
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| EP08155408A EP2113256A1 (en) | 2008-04-29 | 2008-04-29 | PEGylated rhGH compounds |
| EP08162865 | 2008-08-22 | ||
| EP08167289 | 2008-10-22 |
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| HUE09738181A HUE029926T2 (hu) | 2008-04-29 | 2009-04-29 | Pegilált rekombináns humán növekedésihormon-vegyületek |
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