TH44628B - A new type of PEG derivative of interferon-alpha (IFN-alpha) conjugate. - Google Patents

Abstract

DC60 (03/12/56) PEG-IFN alpha m active alpha m conjugate is formulated as follows (Chemical formula) I The conjugate of this invention is used in the same way as IFN al. Alfalfa, for example, is used to inhibit Cell increase Specifically, PEG interferon-alpha conjugate invention. This is useful in the treatment of proper immune disorders such as neoplastic disease. For example, an increase in leukemia cells, CML, capocytes tumors. And infectious diseases Likewise, IFM alpha S (especially IFN alpha 2a) was used to treat these diseases. However, the capacity of the The invention has improved properties such as excellent stability, improved solubility, half life increase and plasma retention time. And this conjugate also has Excellent resistance to cell proliferation compared to IFN-alpha and found that this conjugate Provide resistance to virus And resistance to cell proliferation.This property is useful in increasing the agility in the desired area while reducing or discarding the agility of the unwanted PEG-IFN (alpha ) Active body has the following formula (chemical formula). The invention's conjugate is used in the same way as IFN alpha. Cell increase Specifically, the PEG interferon-alpha conjugate invention. This is useful in the treatment of proper immune disorders such as neoplastic disease. For example, an increase in leukemia cells, CML, capocytes tumors. And infectious diseases similarly to IFM alpha S (especially IFN alpha 2a) for these treatments. This invention has improved various features. These include excellent stability, improved solubility, increased half-life and plasma retention time. And the conjugate that is still Excellent resistance to cell proliferation compared to IFN-alpha and found that this conjugate Provide resistance to virus This property is useful in increasing agility in the desired area while reducing or discarding the agility in areas that do not require a drug patent.

Claims (3)

Disclaimer (all) which will not appear on the advertisement page: Amendment 12/6/2015 1. Pegylated Interferon (Formula)) conjugate chemical formula ) Where R and R \ 'are C1-C6, an independent alkyl, X is NH is O; n and n \' is a number with a sum of 600 to 1,500 and mean molecular weight. Of polyethylene units The tylene glycol in the said conjugate is 26,000 Dalton to 66,000 Dalton 2. Concentrate according to claim 1 where the molecular weight of the polyethylene glycol unit It is 35,000 Dalton to 45,000 Dalton 3. Concentrate according to claim 2 where the molecular weight of polyethylene glycol unit is 40,000 Dalton. Where R and R \ 'are methyl 5. Conjugate according to claim 1 where X is NH 6. Conjugate according to claim 1 where interferon (formula ) Is (Formula) 2a 7. Conjunction according to claim 1, where the mean sum of n and n \ 'is 850 to 1,000. 8. Concurrent according to claim 1, where R and R \ 'is methyl; X is NH; The interferon (formula) is an interferon (formula) 2f, and either or both of n and n \ 'is 420 9.Concentration according to claim 1, where R and R \ 'is methyl; X is NH; The interferon (formula) is an interferon (formula) 2a, and either or both of n and n \ 'is 520 1 0. The agile conjugate according to claim 1. In resistance to increase More cell counts than interferons (formulas) and less virility resistance. Interferon (Formula) 1 1. Method for manufacturing the piggyleted interferon concentrate (formula) With increasing agility In order to resist cell proliferation and decrease the agility of virus resistance compared to Interferon (formula), in which the method It consists of the covalent bond of a substance according to formula II (chemical formula), where R, R \ ', n and n \' are, as defined in claim 1, with interferon (formula) to produce. It is a conjugate of interferon (formula) that has been piggyed. 1 2. Pharmaceutical components Which contains the conjugate of the interferon (formula) that has been piggyed According to the claim 1-10, any one And a carrier that is inert to the treatment. According to any of the claims 1-10 for use in the manufacture of pharmaceuticals for the treatment of immunization disorders and infectious diseases ---------------- ------------------- 1. The conjugate of pegylated interferon alfa (chemical formula) where R and R \ 'Is C1-C6, an independent alkyl, X is NH is O; n and n \' is a number with a sums of 600 to 1,500 and the mean molecular weight of the polyethylene unit. The tylene glycol in the said conjugate is 26,000 Dalton to 66,000 Dalton 2. Concentrate according to claim 1 where the molecular weight of the polyethylene glycol unit It is 35,000 Dalton to 45,000 Dalton 3. Concentrate according to claim 2 where the molecular weight of polyethylene glycol unit is 40,000 Dalton. Where R and R \ 'are methyl 5. Conjugate according to claim 1 where X is NH 6. Conjugate according to claim 1 where interferon alpha is Alpha 2a 7. Conjugate according to claim 1, where the mean sum of n and n \ 'is 850 to 1,000 8. Consequently according to claim 1, where R and R \' are Methyl; X is NH; An alpha interferon is an alpha 2f interferon, and either or both of n and n \ 'is 420 9.Concentration according to claim 1, where R and R \' are Methyl; X is NH; An alpha interferon is an interferon alpha 2a, and either or both of n and n \ 'is 520 1 0. Which has the agility in resistance to increase More cell counts than interferon alpha and less virility resistance. Interferon Alpha 1 1.Production method of piggyated interferon alpha concentrates With increasing agility In order to resist cell proliferation and decrease the agility of virus resistance compared to Interferon alpha, which method It consists of the covalent bond of a substance according to formula II (chemical formula), where R, R \ ', n and n \' is as defined in claim 1 with interferon alpha to produce a con. Jugate of an alpha interferon that is pictured by a piggylet 1 2. Pharmaceutical components Which contains the conjugate of a piggyated alpha interferon According to the claim 1-10, any one And a carrier that is inert to treatment 1 3.Picky-lated alpha interferon alpha concentrates In accordance with any of the claims 1-10 for use in the manufacture of medical supplies for the treatment of immune deficiency disorders and infectious diseases.