Branched polyalkylene glycols
First Claim
1. A branched polyalkylene glycol wherein two single-chain polyalkylene glycols are linked to a group having a cyclic structure other than a plane structure, and wherein a group having reactivity with an amino acid side chain, an N-terminal amino group or a C-terminal carboxyl group in a polypeptide or a group convertible into the group having reactivity is linked to the group having a structure other than a plane structure.
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Accused Products
Abstract
The present invention provides branched polyalkylene glycols useful as a chemically modifying agent for physiologically active polypeptides, wherein two single-chain polyalkylene glycols are linked to a group having a cyclic structure other than a plane structure, and wherein a group having reactivity with an amino acid side chain, an N-terminal amino group or a C-terminal carboxyl group in a polypeptide or a group convertible into the group having reactivity is linked to the group having a structure other than a plane structure.
29 Citations
16 Claims
- 1. A branched polyalkylene glycol wherein two single-chain polyalkylene glycols are linked to a group having a cyclic structure other than a plane structure, and wherein a group having reactivity with an amino acid side chain, an N-terminal amino group or a C-terminal carboxyl group in a polypeptide or a group convertible into the group having reactivity is linked to the group having a structure other than a plane structure.
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4. A branched polyalkylene glycol represented by formula (I):
(R1—
Mn—
X1)2L(X2—
X3—
R2)q
(I)wherein L represents a group having a cyclic structure other than a plane structure and being capable of having 3 to 5 branches, M represents OCH2CH2, OCH2CH2CH2, OCH(CH3)CH2, (OCH2CH2)r—
(OCH2CH2CH2)s in which r and s are the same or different and each represents any positive integer, or (OCH2CH2)ra—
(OCH(CH3)CH2)sa in which ra and sa have the same meanings as the above r and s, respectively,n represents any positive integer, q represents an integer of 1 to 3, R1 represents a hydrogen atom, lower alkyl or lower alkanoyl, R2 represents a group having reactivity with an amino acid side chain, an N-terminal amino group or a C-terminal carboxyl group in a polypeptide or a group convertible into the group having reactivity, X1 represents a bond;
O;
S;
alkylene;
O(CH2)ta in which ta represents an integer of 1 to 8;
(CH2)tbO in which tc has the same meaning as the above ta;
NR3 in which R3 represents a hydrogen atom or lower alkyl;
R4—
NH—
C(═
O)—
R5 wherein R4 represents a bond, alkylene or O(CH2)tc in which tb has the same meaning as the above ta, and R5 represents a bond, alkylene or OR5a in which R5a represents a bond or alkylene;
R6—
C(═
O)—
NH—
R7 wherein R6 represents a bond, alkylene or R6aO in which R6a has the same meaning as the above R5a, and R7 represents a bond, alkylene or (CH2)tdO in which td has the same meaning as the above ta;
R8—
C(═
O)—
O in which R8 has the same meaning as the above R5a;
or O—
C(═
O)—
R9 in which R9 has the same meaning as the above R5a,X2 represents a bond, O or (CH2)teO in which te has the same meaning as the above ta, X3 represents a bond or alkylene, and 2 R1—
Mn—
X1'"'"'s and 1 to 3 X2—
X3—
R2'"'"'s are independently the same or different.- View Dependent Claims (5, 6, 7, 8, 9)
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9. The branched polyalkylene glycol according to claim 8, wherein W is CH2 and u is 4.
Specification