US4837305A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Derivatives of β-adrenergic antagonists
Assignee: University of California, San Diego
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Filing: 1987-08-13
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Granted: 1989-06-06
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Expires: 2007-08-13
Abstract
Abstract Molecular structures of β-adrenergic antagonists are modified to produce biologically active compounds. The β-antagonists are modified to form molecules of the general structure: ##STR1## wherein R is most generally R"--OCH 2 --, and in some instances is R"--, and R"=an aryl or substituted aryl moiety; R'=--H, --CH 3 , or a short chain alkyl moiety; and Y=--OH, or more usually, --OAX or --NHAX, where A=an alkyl, aryl, or aralkyl moiety, and X=a terminal grouping, such as --CH 3 , --CF 3 or --(CH 2 ) n COOH; or AX may be a carrier moiety consisting of a defined peptide or protein.
Inventors
- 👤 Murray Goodman
- 👤 Debra Marr-Leisy
- 👤 Roberto P. Rosenkranz
- 👤 Kenneth L. Melmon
- 👤 Michael S. Verlander
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 08:39
CPC Classifications
C; C07; C07D; C07D209/00; C07D209/02; C07D209/04; C07D209/08; C07C; C07C235/00; C07C235/70; C07C235/72; C07C235/74; C07D209/44; C07D209/48; C07D303/00; C07D303/02; C07D303/12; C07D303/18; C07D303/20; C07D303/22; C07D303/24; C07D405/00; C07D405/02; C07D405/12; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06078
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
94 words
β-adrenergic antagonist compounds having the formula: ##STR34## wherein R=an aryl or substituted aryl or heterocyclic or substituted heterocyclic moiety selected from the group consisting of: ##STR35## R'=H, --CH 3 , or short chain alkyl moiety; n is an integer between 1 and 15; and Y=--O--A--X, or --NH--A--X, where A--a linking functional grouping selected from alkyl, aryl or aralkyl, and X=carrier moiety selected from polypeptides, peptide hormones, proteins, or antibodies each having a molecular weight of between about 75 and 10,000 daltons wherein said carrier moiety in and of itself has essentially no biological activity.
Claim 2
Dependent Claim
94 words
β-adrenergic antagonist compounds having the formula: ##STR34## wherein R=an aryl or substituted aryl or heterocyclic or substituted heterocyclic moiety selected from the group consisting of: ##STR35## R'=H, --CH 3 , or short chain alkyl moiety; n is an integer between 1 and 15; and Y=--O--A--X, or --NH--A--X, where A--a linking functional grouping selected from alkyl, aryl or aralkyl, and X=carrier moiety selected from polypeptides, peptide hormones, proteins, or antibodies each having a molecular weight of between about 75 and 10,000 daltons wherein said carrier moiety in and of itself has essentially no biological activity.
Claim 3
Dependent Claim
19 words
The compound of claim 1 wherein X is selected from polypeptides wherein said polypeptides have essentially no biological activity.
Claim 4
Dependent Claim
13 words
The compound of claim 2 wherein the polypeptides are selected from homooligopeptide blocks.
Claim 5
Dependent Claim
13 words
The compounds of claim 1 wherein the carrier moiety is a defined peptide.
Claim 6
Dependent Claim
12 words
The compounds of claim 1 wherein the carrier moiety is a protein.
Claim 7
Dependent Claim
14 words
The compounds of claim 1 wherein the carrier moiety is a naturally occurring peptide.
Claim 8
Dependent Claim
9 words
The compound N.sup.α -acetyl-p-{6-(3-[4-acetamidophenoxy]-2-hydroxypropylamino)-heptanoylamino}-L-phenylalanyl-3-hydroxypropylamide and pharmaceutically acceptable salts thereof.
Claim 9
Dependent Claim
9 words
The compound N.sup.α -acetyl-p-{6-(3-[4-acetamidophenoxy]-2-hydroxypropylamino)-heptanoylamino}-L-phenylalanyl-3-hydroxypropylamide and pharmaceutically acceptable salts thereof.
Claim 10
Dependent Claim
189 words
A β-andrenergic antagonist compound of the formula: ##STR36## wherein R is selected from the group consisting of: ##STR37## R'=--H, --CH 3 , or short chain alkyl moiety; n is an integer between 1 and 15; and Y=--O--A--X, or --NH--A--X, where A=a linking functional grouping selected from alkyl, aryl or aralkyl and X=a carrier moiety having a molecular weight in the range of 75 to 10,000 daltons wherein said carrier itself has essentially no biological activity and wherein X is a peptide carrier of the formula: ##STR38## wherein A' and B' are oligopeptide blocks wherein the amino acid residues are the same or different with predesigned sequences; C' is an amino acid residue to which the congener is bound; X" is an amine blocking group or H; X' is a carboxyl blocking group, or H; Y" is a general amino acid residue side chain; Y"' is a general amino acide residue side chain; Y' is a side chain on the amino acid residue to which the congener is bound where a=b, a=b, a or b are each be 0 or any samll integer; and m is 1, 2 or 3.
Claim 11
Dependent Claim
189 words
A β-andrenergic antagonist compound of the formula: ##STR36## wherein R is selected from the group consisting of: ##STR37## R'=--H, --CH 3 , or short chain alkyl moiety; n is an integer between 1 and 15; and Y=--O--A--X, or --NH--A--X, where A=a linking functional grouping selected from alkyl, aryl or aralkyl and X=a carrier moiety having a molecular weight in the range of 75 to 10,000 daltons wherein said carrier itself has essentially no biological activity and wherein X is a peptide carrier of the formula: ##STR38## wherein A' and B' are oligopeptide blocks wherein the amino acid residues are the same or different with predesigned sequences; C' is an amino acid residue to which the congener is bound; X" is an amine blocking group or H; X' is a carboxyl blocking group, or H; Y" is a general amino acid residue side chain; Y"' is a general amino acide residue side chain; Y' is a side chain on the amino acid residue to which the congener is bound where a=b, a=b, a or b are each be 0 or any samll integer; and m is 1, 2 or 3.
Claim 12
Dependent Claim
18 words
The β-andrenergic antagonist compound of claim 8 wherein X is a carrier consisting essentially of identical amino acids.
Claim 13
Dependent Claim
23 words
The β-andrenergic antagonist compound of claim 8 wherein the a=b, and a or b are 0 or an integer from 1 to 9.
Claim 14
Dependent Claim
28 words
The β-andrenergic antagonist compound of claim 10 wherein A' and B' are selected from oligopeptide blocks wherein a and b are each selected from an integer from 1-3.
Claim 15
Dependent Claim
45 words
The β-andrenergic antagonist compound of claim 8 wherein X=a carrier moiety having a molecular weight in the range of 200 and 10,000 daltons, wherein said carrier moiety X is selected from synthetic peptides selected from polyserine, polyglysine, polytyrosine, polythreonine, polycysteine, polyaspartic acid or polyglutamic acid.
References Cited (Backward Citations)
US4687873A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-06-05 | 1992-12-05 | 1993-06-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-06-05 | 1996-12-05 | 1997-06-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-06-05 | 2000-12-05 | 2001-06-06 | $7700.00 | Window Closed / Lapsed |