EP0335423A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Modified human G-CSF
Assignee: KH Neochem Co Ltd
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Filing: 1989-03-31
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Granted: —
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Expires: 2009-03-31
Abstract
Abstract A modified polypeptide having human granulocyte colony stimulating factor (hG-CSF) activity comprising a polypeptide having hG-CSF activity with at least one amino group thereof substituted with a group of the formula wherein R 1 is an alkyl or alkanoyl group; n is an optionally variable positive integer; X is 0, NH or S; R 2 is [where R 3 is OH, Cl, O-(CH 2 CH 2 O) n -R 1 , where R 1 and n are as defined above, Y may not be present or represents Z-(CH 2 )pCO, where Z is 0, S or NH and p is an optionally variable positive interger], or (CO) m -(CH 2 )gCO, where m is 0 or 1; t is an optionally variable positive integer, which can provide an enhanced peripheral leukocyte (granulocyte) increasing effect with improved stability and residence time in the blood and, as such, can be used advantageously in clinical medicines.
Inventors
- 👤 Motoo Yamasaki
- 👤 Yoshiharu Yokoo
- 👤 Makoto Morimoto
- 👤 Masami Okabe
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 12:54
CPC Classifications
C; C07; C07K; C07K16/00; C07K16/18; C07K16/24; C07K16/243; C07K1/00; C07K1/107; C07K1/113; C07K14/00; C07K14/435; C07K14/52; C07K14/53; C07K14/535; C07K17/00; C07K17/02; C07K17/06; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
125 words
A modified polypeptide having human granulocyte colony stimulating factor (hG-CSF) activity comprising a polypeptide having hG-CSF activity with at least one amino group thereof substituted with a group of the formula wherein R, is an alkyl or alkanoyl group: n is an optionally variable positive integer; X is 0, NH or S; R 2 is [where R 3 is OH, Cl, O-(CH 2 CH 2 O) n -R 1 , where R 1 and n are as defined above, Y may not be present or represents Z-(CH 2 )pCO, where Z is 0, S or NH and p is an optionally variable positive interger], or (CO) m -(CH 2 ) ℓ CO, where m is 0 or 1; t is an optionally variable positive integer.
Claim 2
Dependent Claim
125 words
A modified polypeptide having human granulocyte colony stimulating factor (hG-CSF) activity comprising a polypeptide having hG-CSF activity with at least one amino group thereof substituted with a group of the formula wherein R, is an alkyl or alkanoyl group: n is an optionally variable positive integer; X is 0, NH or S; R 2 is [where R 3 is OH, Cl, O-(CH 2 CH 2 O) n -R 1 , where R 1 and n are as defined above, Y may not be present or represents Z-(CH 2 )pCO, where Z is 0, S or NH and p is an optionally variable positive interger], or (CO) m -(CH 2 ) ℓ CO, where m is 0 or 1; t is an optionally variable positive integer.
Claim 3
Dependent Claim
18 words
The modified polypeptide of claim 1, wherein R 1 is a C, - 18 alkyl or alkanoyl group.
Claim 4
Dependent Claim
17 words
The modified polypeptide of claim 1, wherein n is a positive integer of not more than 500.
Claim 5
Dependent Claim
17 words
The modified polypeptide of claim 1, wherein t is a positive integer of not more than 100.
Claim 6
Dependent Claim
21 words
The modified polypeptide of claim 1, wherein the group of formula (I) has a molecular weight of not more than 30,000.
Claim 7
Dependent Claim
14 words
A lyophilized preparation containing the modified polypeptide of anyone of claims 1 to 5.
Claim 8
Dependent Claim
16 words
A leukocyte growth promoting agent comprising the modified polypeptide of anyone of claims 1 to 5.
Claim 9
Dependent Claim
31 words
A carboxylic acid represented by formula wherein R 1 , n and X are as defined above, Z is 0, S or NH and p is an optionally variable positive integer.
Claim 10
Dependent Claim
31 words
A carboxylic acid represented by formula wherein R 1 , n and X are as defined above, Z is 0, S or NH and p is an optionally variable positive integer.
Claim 11
Dependent Claim
83 words
Process for preparing a chemically modified hG-CSF according to anyone of claims 1 to 5, comprising condensation of hG-CSF with a halide of formula (II) wherein R 1 , n, X and R 3 are as defined hereinbefore or condensation of hG-CSF with a carboxylic acid of formula (III) wherein Ri, n, X, m and ℓ are as defined hereinbefore or with a carboxylic acid of formula (IV) wherein R 1 , n, Z, X, R 3 and p are as defined hereinbefore.
Claim 12
Dependent Claim
40 words
Process according to claim 9, comprising condensation of hG-CSF with a carboxylic acid represented by formula (V) wherein Ri, n and X are as defined above, Z is 0, S or NH and p is an optionally variable positive integer.
Claim 13
Dependent Claim
87 words
Process according to claim 9 or 10, characterized in that the halide or active carboxylic acid compound is added to the polypeptide in a proportion (mole ratio) of 2 to 100 times the amount of amino groups present in the polypeptide molecule and the mixture is allowed to react at a temperature of 4 to 37 °C, preferably 4 to 10 C, and at pH 7 to 10 for 1 hour to 2 days, preferably 1 to 24 hours, whereby the desired chemically modified hG-CSF is produced.
References Cited (Backward Citations)
No citation records indexed.
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