EP0040506A2
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Reactive polymer and process for the preparation thereof
Assignee: Teijin Ltd
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Filing: 1981-05-13
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Granted: —
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Expires: 2001-05-13
Abstract
Abstract A reactive polymer having the degree of polymerization in the range of 5 to 3,000, with 60 mole % or more of the whole constituent units comprising the constituent units expressed by formula (I) wherein Z indicates a hydrogen atom or a univalent cation; m is an integer 1 to 4: and has an active group expressed by formula (II) at the carboxyl end of the main chain wherein X indicates a hydrogen atom or a group which can form an active disulfide linkage together with a neighboring sulfur atom; W is a divalent organic group; and R 1 represents a hydrogen atom or an alkyl group having 1 to4 carbon atoms. Since this reactive polymer can bind to cytotoxic substances, which contain an amino group or imino group in the molecule by way of the carboxyl group of the side chain and it also can bind to, for instance, antitumor immunoglobulins by way of an active group (thiol group or active disulfide group) atthe end of the main chain, it can be used as a polymercarrier in the preparation of target seeking antitumor drugs.
Inventors
- 👤 Yoshinori Kato
- 👤 Hisashi Fukushima
- 👤 Takeshi Hara
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-26 05:01
CPC Classifications
C; C08; C08G; C08G69/00; C08G69/48; A; A61; A61K; A61K39/00; A61K39/395; A61K39/44; A61K47/00; A61K47/50; A61K47/51; A61K47/62; A61K47/64; A61K47/645; A61K47/68; A61K47/6835; A61K47/6881; A61K47/6883; C08G69/42
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
113 words
A reactive polymer having the degree of polymerization in the range of 5 to 3,000, with 60 mole % or more of the whole constituent units comprising the constituent units expressed by formula (I) wherein Z indicates a hydrogen atom or a univalent cation; m is an integer 1 to 4: and has an active group expressed by formula (II) at the carboxyl end of the main chain wherein X indicates a hydrogen atom or a group which can form an active disulfide linkage together with a neighboring sulfur atom; W is a divalent organic group; and R 1 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms.
Claim 2
Dependent Claim
113 words
A reactive polymer having the degree of polymerization in the range of 5 to 3,000, with 60 mole % or more of the whole constituent units comprising the constituent units expressed by formula (I) wherein Z indicates a hydrogen atom or a univalent cation; m is an integer 1 to 4: and has an active group expressed by formula (II) at the carboxyl end of the main chain wherein X indicates a hydrogen atom or a group which can form an active disulfide linkage together with a neighboring sulfur atom; W is a divalent organic group; and R 1 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms.
Claim 3
Dependent Claim
23 words
A reactive polymer according to Claim 1, wherein W in the formula (II) is an alkylene group having 1 to 4 carbon atoms.
Claim 4
Dependent Claim
50 words
A reactive polymer according to Claim 1, wherein X in the formula (II) is a group, which can form an active disulfide linkage, selected from the group consisting of 2-pyridylthio group, 4-pyridylthio group, 3-carboxy-4-nitrophenylthio group, 4-carboxy-2-pyridylthio group, N-oxy-2-pyridylthio group, 2-nitrophenylthio group, 4-nitro-2-pyridylthio group, 2-benzothiazolylthio group, 2-benzoimidazolylthio group and N-phenylamino-N'-phenyliminomethylthio group.
Claim 5
Dependent Claim
251 words
A process for preparing a reactive polymer having the degree of polymerization in the.range of 5 to 3,000, with 60 mole % or more of the whole constituent units comprising the constituent units expressed by formula (I) wherein Z and m respectively have the meaning defined for formula (I) in Claim 1: and has a group containing a disulfide linkage expressed by the following formula (III) in the main chain or at the carboxyl terminal of the main chain wherein W and R 1 respectively have the meaning defined for formula. (II) in Claim 1; R 2 indicates an alkyl group, aralkyl group, or aryl group, when the group expressed by formula (III) is an end group of the main chain, and indicates a divalent group represented when the group expressed by formula (III) is in the main chain: in which W' is a divalent organic group identical with or different from W and is linked with S of formula (III); R 1 is identical with or different from R 1 and represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms: and is characterized by reductively cleaving the disulfide linkage contained in the hydrophilic polymer, with 60 mole % or more of the whole constituent units comprising the constituent units expressed by formula (I), having an active group expressed by formula (II-a) at the carboxyl terminal of the main chain wherein W and R 1 respectively have the meaning defined for formula (II) in Claim 1.
Claim 6
Dependent Claim
161 words
A process for preparing a reactive polymer having the degree of polymerization in the range of 5 to 3,000, with 60 mole % or more of the whole constituent units comprising the constituent units expressed by formula (I) wherein Z and m respectively have the meaning defined for formula (I) in Claim 1: characterized by making the hydrophilic polymer which has an active group expressed by formula (II-a) at the carboxyl terminal of the main chain wherein W and R 1 respectively have the meaning defined for formula (II) in Claim 1; with an active disulfide compound, and 60 mole % or more of the whole constituent units comprising the constituent units expressed by formula (I), having an active group expressed by formula (II-b) at the carboxyl terminal of the main chain wherein W and R l respectively have the meaning defined for formula (II); X' indicates a group capable of forming an active disulfide linkage with a neighboring sulfur atom.
Claim 7
Dependent Claim
91 words
A hydrophilic polymer having the degree of polymerization in the range of 5 to 3,000, with 60 mole % or more of the whole constituent units comprising the constituent units expressed by formula (I) wherein Z and m respectively have the meaning defined for formula (I) in Claim 1: and has a disulfide linkage-containing group expressed by formula (III) in the main chain or at the carboxyl terminal of the main chain wherein W, R l , and R 2 respectively have the meaning defined for formula (III) in Claim 4.
Claim 8
Dependent Claim
137 words
A reactive polymer, which is linked with a cytotoxic substance, having the degree of polymerization in the range of 5 to 3,000, with 60 mole % or more of the whole constituent units comprising the total of the constituent units expressed by formula (I) wherein Z and m respectively have the meaning defined for formula (I) in Claim 1: and the constituent units expressed by formula (IV) wherein Y indicates a reaction residue of the amino group or imino group of the cytotoxic substance which contains an amino group or imino group in its molecule; and m is an integer 1 to 4: and has an active group expressed by formula (II) at the carboxyl end of the main chain wherein X, W, and R 1 ,respectively have the meaning defined for formula (II) in Claim 1.
Claim 9
Dependent Claim
118 words
8 . A process for preparing a reactive polymer linked with a cytotoxic substance comprising (1) first making a cytotoxic substance, which contains an amino group or imino group in its molecule, react with a reactive polymer having the degree of polymerization in the range of 5 to 3,000, with 60 mole % or more of the whole constituent units consisting of the constituent units expressed by formula (I) wherein Z and m respectively have the meaning defined for formula (I) in Claim 1: and has an active group expressed by formula (II) at the carboxyl end of the main chain wherein X, W, and R 1 respectively have the meaning defined for formula (II) in Claim 1.
Claim 10
Dependent Claim
170 words
A process for preparing a reactive polymer, which is linked with a cytotoxic substance, having an active group expressed by formula (II-a) at the carboxyl end of the main chain wherein Wand R 1 respectively have the meaning defined for formula (II) in Claim 1: which process comprises making a cytotoxic substance which contains an amino group or imino group in its molecule react with a hydrophilic polymer having the degree of polymerization in the range of 5 to 3,000, with 60 mole % or more of the whole constituent units consisting of the constituent units expressed by formula (I) wherein Z and m respectively have the meaning defined for formula (I) in Claim 1; and has a disulfide linkage-containing group expressed by formula (III) in the main chain or at the carboxyl terminal of the main chain wherein W, R 1 , and R 2 respectively have the meaning defined for formula (III) in Claim 4: and (2) then reductively cleaving the disulfide linkage contained in the reactive product.
Claim 11
Dependent Claim
166 words
A process for preparing a reactive polymer, which is linked with a cytotoxic substance, having an active group expressed by formula (II-b) at the carboxyl end of the main chain wherein X', W, and R 1 respectively have the meaning defined for formula (II-b) in Claim 5: which process comprises making an active disulfide compound react with a polymer having the degree of polymerization in the range of 5 to 3,000, with 60 mole % or more of the whole constituent units consisting of the total of the constituent units expressed by formula (I) wherein Z and m respectively have the meaning defined for formula (I) in Claim 1: and the constituent units expressed by formula (IV) wherein Y and m respectively have the meaning defined for formula (IV) in Claim 7: and has an active group expressed by formula (II) at the carboxyl end of the main chain wherein S, W, and R 1 respectively have the meaning defined for formula (II) in Claim 1.
References Cited (Backward Citations)
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