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EP0154316A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Chemically modified lymphokine and production thereof

Assignee: Takeda Pharmaceutical Co Ltd
•
Filing: 1985-03-02
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Granted: —
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Expires: 2005-03-02
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Abstract

Abstract The invention provides chemically modified lymphokines having R-O-CH 2 CH 2n wherein R is a protective group for the terminal oxygen and n is an optional positive integer, bonded directly to at least one primary amino group of the lymphokine moiety, and a method of producing the same. The chemically modified lymphokines according to the invention can be produced by reacting a lymphokine with an aldehyde of the formula R-O-CH 2 CH 2n-1 O-CH 2 CHO wherein R and n are as defined above, in the presence of a reducing agent. The chemically modified lymphokines according to the invention are useful as drugs, among others.

Inventors

  • 👤 Osamu Nishimura
  • 👤 Masahiko Fujino

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-23 12:19
CPC Classifications
C; C07; C07K; C07K1/00; C07K1/107; C07K1/1072; C07K1/1077; C07K14/00; C07K14/435; C07K14/52; C07K14/54; C07K14/55; C07K14/555; C07K14/56; C07K14/57; A; A61; A61K; A61K38/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55

Claims Analysis

Total Claims: 19
Claim 1
Independent Claim 41 words
A chemically modified lymphokine having polyethylene glycol of the formula: wherein R is a protective group for the terminal oxygen atom and n is an optional positive integer, bonded directly to at least one primary amino group of the lymphokine moiety.
Claim 2
Dependent Claim 41 words
A chemically modified lymphokine having polyethylene glycol of the formula: wherein R is a protective group for the terminal oxygen atom and n is an optional positive integer, bonded directly to at least one primary amino group of the lymphokine moiety.
Claim 3
Dependent Claim 18 words
The modified lymphokine according to claim 1, wherein the lymphokine moiety has molecular weight from 5,000 to 50,000.
Claim 4
Dependent Claim 18 words
The modified lymphokine according to claim 2, wherein the lymphokine moiety has molecular weight from 10,000 to 30,000.
Claim 5
Dependent Claim 31 words
The modified lymphokine according to claim 1, wherein the lymphokine moiety is interferons, interleukin-2, macrophage differentiating factor, macrophage activating factor, or substances similar in structure and in physiological activity to these.
Claim 6
Dependent Claim 19 words
The modified lymphokine according to claim 1, wherein the lymphokine moiety is interferon-a, interferon-S, interferon-y, interferon-yd2, interferon-yd3 or interleukin-2.
Claim 7
Dependent Claim 13 words
The modified lymphokine according to claim 1, wherein the lymphokine moiety is inteferon-a.
Claim 8
Dependent Claim 13 words
The modified lymphokine according to claim 1, wherein the lymphokine moiety is interferon-y.
Claim 9
Dependent Claim 13 words
The modified lymphokine according to claim 1, wherein the lymphokine moiety is interleukin-2.
Claim 10
Dependent Claim 28 words
The modified lymphokine according to claim 1, wherein the polyethylene glycol has . molecular weight corresponding to 1 to 10% of the molecular weight of the lymphokine moiety.
Claim 11
Dependent Claim 18 words
The modified lymphokine according to claim 1, wherein the polyethylene glycol has molecular wieght from 350 to 6,000.
Claim 12
Dependent Claim 13 words
The modified lymphokine according to claim 1, wherein R is alkyl or alkanoyl.
Claim 13
Dependent Claim 17 words
The modified lymphokine according to claim 1, wherein n is a positive integer from 7 to 120.
Claim 14
Dependent Claim 26 words
The modified lymphokine according to claim 1, wherein the primary amino group is N-terminal a-amino group or e-amino group of lysine residue in the lymphokine moiety.
Claim 15
Dependent Claim 26 words
The modified lymphokine according to claim 1, which has polyethylene glycol bonded to 15 to 80% of ε-amino groups of lysine residue in the lymphokine moiety.
Claim 16
Independent Claim 71 words
A method of producing a chemically modified lymphokine having polyethylene glycol of the formula: wherein R is a protective group for the terminal oxygen atom and n is an optional positive integer, bonded directly to at least one primary amino group of the lymphokine moiety, which comprises reacting a lymphokine with an aldehyde of the formula: wherein R and n are as defined above, in the presence of a reducing agent.
Claim 17
Independent Claim 71 words
A method of producing a chemically modified lymphokine having polyethylene glycol of the formula: wherein R is a protective group for the terminal oxygen atom and n is an optional positive integer, bonded directly to at least one primary amino group of the lymphokine moiety, which comprises reacting a lymphokine with an aldehyde of the formula: wherein R and n are as defined above, in the presence of a reducing agent.
Claim 18
Dependent Claim 16 words
The method according to claim 15, wherein the reaction is conducted in the neighborhood of neutrality.
Claim 19
Dependent Claim 13 words
The method according to claim 15, wherein the reducing agent is sodium cyanoborohydride.

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