Patent FR1283603A successfully refreshed from Google Patents.
EP0063109A2
Expired / Lapsed
EP
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Therapeutically active compound and pharmaceutical composition containing the same
Assignee: Pfizer Health AB
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Filing: 1982-04-05
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Granted: —
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Expires: 2002-04-05
Abstract
Abstract Therapeutically active organic compound exhibiting at least one radical comprising a structure -S'-S"-R, where S"-R is defined by R being an organic group comprised in a physiologically acceptable compound H-S"-R obtainable by the splitting of the disulfide bridge-S'-S"- in said structure, in which compound H-S"-R the sulfur atom S" is bound to a carbon atom in a heterocyclic aromatic ring in R having a configuration being such that the compound H-S"-R, while maintaining physiological acceptability, is stabilized, by tautomerism or resonance involving the sulfur atom S" bound to R, so as to be mainly excluded from further reaction involving thiol disulfide exchange; S' being bound to an aliphatic carbon atom; and said compound, in addition to the group or groups comprising the structure -S'-S"-R, also consisting of a residue of a therapeutically active organic base compound of polypeptide structure bound to S', for therapeutical use in mammals, including humans. The invention also relates to a pharmaceutical composition containing as an active substance the compound mentioned above.
Inventors
- 👤 Rolf Erik Axel Verner Axen
- 👤 Jan Per Erik Carlsson
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 14:02
CPC Classifications
C; C12; C12N; C12N9/00; C12N9/0004; C12N9/0089; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/62; C12N9/0065; C12N9/96
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
150 words
Therapeutically active organic compound exhibiting at least one group comprising a structure -S'-S''-R, where S"-R is defined by R being an organic group comprised in a physiologically acceptable compound H-S''-R obtainable by the splitting of the disulfide bridge -S'-S in said structure, in which compound H-S"-R the sulfur atom S" is bound to a carbon atom in a heterocyclic aromatic ring in R having a configuration being such that the compound H-S"-R, while maintaining physiological acceptability, is stabilized, by tautomerism or resonance involving the sulfur atom S" bound to R, so as to be mainly excluded from further reaction involving thiol disulfide exchange; S' being bound to an aliphatic carbon atom; and said compound, in addition to the group or groups comprising the structure -S'-S"-R, also consisting of a residue of a therapeutically active organic base compound of polypeptide structure bound to S', for therapeutical use in mammals, including humans.
Claim 2
Dependent Claim
150 words
Therapeutically active organic compound exhibiting at least one group comprising a structure -S'-S''-R, where S"-R is defined by R being an organic group comprised in a physiologically acceptable compound H-S''-R obtainable by the splitting of the disulfide bridge -S'-S in said structure, in which compound H-S"-R the sulfur atom S" is bound to a carbon atom in a heterocyclic aromatic ring in R having a configuration being such that the compound H-S"-R, while maintaining physiological acceptability, is stabilized, by tautomerism or resonance involving the sulfur atom S" bound to R, so as to be mainly excluded from further reaction involving thiol disulfide exchange; S' being bound to an aliphatic carbon atom; and said compound, in addition to the group or groups comprising the structure -S'-S"-R, also consisting of a residue of a therapeutically active organic base compound of polypeptide structure bound to S', for therapeutical use in mammals, including humans.
Claim 3
Dependent Claim
40 words
Therapeutically active organic compound according to claim 1., wherein at least one group comprising the structure -S'-S''-R is substituted on a primary amino or secondary amino group or carboxy group in the therapeutically active organic base compound of polypeptide structure.
Claim 4
Dependent Claim
122 words
Therapeutically active organic compound according to claim 2., wherein one or more of the amino groups being substituted with a group of the formula where R, S" and S' have the same meanings as above, A is a straight, branched or cyclic hydrocarbon chain of 1 - 10 carbon atoms which optionally is substituted with 1 - 3 hydroxyl groups and optionally is broken by 1 - 3 oxygen or sulfur atoms, preferably at most one atom other than carbon and hydrogen is bound to one and the same carbon atom in A, and X is 1) the function -CO- bound to the nitrogen atom in the amino group or 2) a direct bond to the nitrogen atom in the amino group.
Claim 5
Dependent Claim
62 words
Therapeutically active organic compound according to claim 2., wherein one or more carboxy groups -CO-OH being transformed to one or several groups of formula -CO-X 1 -A-S'-S "-R; where A, R, S" and S' have the meanings given above and X is -0- or -N(R 1 )-, where R 1 is hydrogen or a lower alkyl with 1 - 5 carbon atoms.
Claim 6
Dependent Claim
49 words
Therapeutically active organic compound according to claim 1., wherein the therapeutically active organic base compound of polypeptide structure contains one or more SH-groups and/or inner -S-S-bridges and having at least one of these groups or bridges transformed to said structure -S'-S"-R or to one or two such structures respectively.
Claim 7
Dependent Claim
30 words
Therapeutically active organic compound according to any of claims 1 - 5, wherein the therapeutically active base compound is a therapeutically active protein, preferably a therapeutically active enzyme or hormone.
Claim 8
Dependent Claim
16 words
Therapeutically active organic compound according to claim 6., wherein the enzyme is superoxide dismutase or catalase.
Claim 9
Dependent Claim
13 words
Therapeutically active organic compound according to claim 6., wherein the hormone is insulin.
Claim 10
Dependent Claim
36 words
Therapeutically active organic compound according to any of claims 1. - 8., wherein R in the structure -S'-S" -R is 2-benzothiazolyl, 2-pyridyl, 5-nitro-2-pyridyl, 4-pyridyl, 5-carboxy-2-pyridyl or the N-oxide of any of the four last mentioned groups.
Claim 11
Dependent Claim
19 words
Pharmaceutical composition, containing as an active substance a therapeutically active organic compound according to any of claims 1..- 10.
References Cited (Backward Citations)
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