EP0510356A1
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EP
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Polyethylene glycol protein conjugates
Assignee: F Hoffmann La Roche AG
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Filing: 1992-03-18
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Granted: —
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Expires: 2012-03-18
Abstract
Abstract The present invention relates to physiologically active, substantially non-immunogenic water soluble polyethylene glycol protein conjugates having at least part of the biological activity of the protein which forms the conjugate, without exhibiting the same disadvantageous immunogenic responses thereof.
Inventors
- 👤 John Hakimi
- 👤 Patricia Kilian
- 👤 Perry Rosen
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-05 21:17
CPC Classifications
C; C07; C07K; C07K14/00; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/59; A61K47/60; A61P; A61P37/00; A61P37/02; A61P43/00; C08; C08G; C08G65/00; C08G65/02; C08G65/32; C08G65/329; C08G65/333; C08G65/3332; C08G65/33344; C08G65/33396; C08G65/334; C08G65/3344; C08G65/3348; C08L; C08L71/00; C08L71/02; Y; Y10; Y10S; Y10S435/00; Y10S435/964; Y10S530/00; Y10S530/81; Y10S530/812; Y10S530/815; Y10S530/816
Claims Analysis
Total Claims: 28
Claim 1
Independent Claim
113 words
A physiologically active conjugate of a protein of the formula wherein R¹ is lower alkyl; R² is -O- or -NH-; R³ is =N-R₄, =S or =o; R⁴ is lower alkyl or cycloalkyl; m and n are selected from integers ≧ 1 in a way that the conjugate has at least a portion of the biological activity of the non conjugated protein; with the proviso that when R² is -O-, R³ is other than =N-R⁴; that when R² is -O- and R³ is =O the protein is interferon-alpha, interleukin-1 or interleukin-1ra and that when R² is -O- and R³ is =S the protein is not antigen E from ragweed pollen or bovine plasma albumin.
Claim 2
Dependent Claim
32 words
A protein conjugate of claim 1 wherein m and n are selected in a way that the molecular weight of the pegylation residue(s) per protein molecule is from 300 to 30,000 daltons.
Claim 3
Dependent Claim
15 words
A protein conjugate of claim 1 or claim 2 wherein m is 1 or 2.
Claim 4
Dependent Claim
25 words
A protein conjugate of any one of claims 1-3 of the formula wherein R¹, R⁴, m, n and the protein are as in claim 1.
Claim 5
Dependent Claim
24 words
A protein conjugate of any one of claims 1-3 of the formula wherein R¹, m, n and the protein are as in claim 1.
Claim 6
Dependent Claim
24 words
A protein conjugate of any one of claims 1-3 of the formula wherein R¹, m, n and the protein are as in claim 1.
Claim 7
Dependent Claim
24 words
A protein conjugate of any one of claims 1-3 of the formula wherein R¹, m, n and the protein are as in claim 1.
Claim 8
Dependent Claim
24 words
A protein conjugate of any one of claims 1-3 of the formula wherein R¹, m, n and the protein are as in claim 1.
Claim 9
Dependent Claim
14 words
A protein conjugate according to any one of claims 1-8 wherein R¹ is CH₃.
Claim 10
Dependent Claim
15 words
A protein conjugate according to any one of claims 1-9 wherein the protein is interleukin-1.
Claim 11
Dependent Claim
15 words
A protein conjugate according to any one of claims 1-9 wherein the protein is interleukin-1ra.
Claim 12
Dependent Claim
15 words
A protein conjugate according to any one of claims 1-9 wherein the protein is interferon-alpha.
Claim 13
Dependent Claim
15 words
A protein conjugate according to any one of claims 1-9 wherein the protein is interleukin-2.
Claim 14
Dependent Claim
14 words
The protein conjugate of claim 1 of the formula wherein n is about 112.
Claim 15
Dependent Claim
14 words
The protein conjugate of claim 1 of the formula wherein n is about 112.
Claim 16
Dependent Claim
16 words
The protein conjugate according to claim 12 or claim 13 wherein the interferon-alpha is interferon-alpha A.
Claim 17
Dependent Claim
35 words
A compound selected from the group consisting of wherein R¹ is lower alkyl, R⁴ is lower alkyl or cycloalkyl, R⁵ is lower alkyl or H and n is any integer of from 1 to 1000.
Claim 18
Dependent Claim
9 words
A compound of claim 17 wherein R⁴ is cyclohexyl.
Claim 19
Dependent Claim
9 words
A compound of claim 17 wherein R⁵ is H.
Claim 20
Dependent Claim
9 words
A compound of claim 17 wherein R⁵ is CH₃.
Claim 21
Dependent Claim
13 words
A compound according to any one of claims 17-20 wherein R¹ is CH₃.
Claim 22
Dependent Claim
14 words
A compound with the formula wherein R¹ is CH₃ and n is about 112.
Claim 23
Dependent Claim
23 words
Protein conjugates in accordance with any one of claims 1-16 for use as therapeutically active compounds in the treatment or prophylaxis of illnesses.
Claim 24
Dependent Claim
46 words
Process for the preparation of a protein conjugate claimed in any one of claims 1-16, which process comprises reacting a compound claimed in claim 17 with a free amino group of a protein or a salt thereof and isolating the protein conjugate from the reaction mixture.
Claim 25
Dependent Claim
19 words
Pharmaceutical compositions comprising a protein conjugate as claimed in any one of claims 1-16 and a therapeutically inert carrier.
Claim 26
Dependent Claim
34 words
Pharmaceutical compositions for the treatment or prophylaxis of immunomodulatory disorders such as neoplastic diseases or infectious diseases comprising a protein conjugate as claimed in any one of claims 1-16 and a therapeutically inert carrier.
Claim 27
Dependent Claim
25 words
The use of the protein conjugates according to any one of claims 1-16 in the treatment or prophylaxis of illnesses of others than human beings.
Claim 28
Dependent Claim
27 words
The use of the protein conjugates according to any one of claims 1-16 for the manufacture of medicaments for use in the treatment or prophylaxis of illnesses.
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