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 Title: |
US4110322:
Peptide derivatives and pharmaceutical compositions containing same
[ Derwent Title ]
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| Country: |
US United States of America
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| Inventor: |
Greven, Hendrik M.; Heesch, Netherlands
DE Wied, David; Bilthoven, Netherlands
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| Assignee: |
Akzona Incorporated, Asheville, NC
other patents from AKZONA INCORPORATED (16025) (approx. 687)
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| Published / Filed: |
1978-08-29
/ 1977-06-27
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| Application Number: |
US1977000810277
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| IPC Code: |
Advanced:
A61K 38/22;
C07K 1/113;
C07K 5/068;
C07K 5/087;
C07K 7/06;
C07K 7/08;
C07K 14/695;
A61K 38/00;
Core:
C07K 1/00;
C07K 5/00;
C07K 7/00;
C07K 14/435;
more...
IPC-7:
A61K 37/00;
C07C 103/51;
C07G 7/00;
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| ECLA Code: |
C07K5/06B; C07K5/08A2; C07K14/695A; K61K38/00;
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| U.S. Class: |
Current:
530/326;
530/327;
930/010;
930/021;
930/070;
930/DIG.572;
930/DIG.782;
Original:
260/112.5R;
424/177;
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| Field of Search: |
260/112.5 R
424/177
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| Priority Number: |
| 1976-07-12 |
NL1976000007683 |
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| Abstract: |
Biologically active novel peptide compounds are disclosed of the formula A-L-B-D-Lys-L-Phe-Gly-(L or D)Lys-L-Pro-L-Val-Gly-L-Lys-L-Lys-X or a pharmaceutically acceptable non-toxic functional derivative thereof; A is a N-terminal chain prolongation selected from the group consisting of (1) hydrogen and (2) N-acyl radicals derived from (a) alkyl carboxylic acids having from one to about six carbons, (b) aralkyl carboxylic acids having from seven to about ten carbons, (c) amino acids, (d) peptides, (e) the N-alkylcarbonyl or N-aralkylcarbonyl derivatives of the amino acids, and (f) the N-alkylcarbonyl or N-aralkylcarbonyl derivatives of the peptides; B is an amino-acid residue selected from the group consisting of Phe, Trp, Tyr, and -NH-CHR1-CO-, wherein R1 is hydrogen or alkyl from one to about six carbons; and X is a member selected from the group consisting of hydroxy, esterified hydroxy radicals, unsubstituted amino radicals and substituted amino radicals. Pharmaceutical compositions containing these compounds are also disclosed to take advantage of the valuable psychopharmacological properties thereof, such as utilization for the treatment for senility or, more generally, for a stimulation of the mental performance.
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| Attorney, Agent or Firm: |
Falk, Robert H. ;
Wendel, Charles A. ;
Young, Francis W. ;
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| Primary / Asst. Examiners: |
Phillips, Delbert R.; Hazel, Blondel
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| INPADOC Legal Status: |
None
Family Legal Status Report
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| Family: |
Show 26 known family members
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First Claim:
Show all 34 claims |
We claim as our invention:
1. Compounds of the formula: A-L-B-D-Lys-L-Phe-Gly-(L or D)Lys-L-Pro-L-Val-Gly-L-Lys-L-Lys-X and their functional derivatives, wherein:
- A is an N-terminal chain prolongation selected from the group consisting of:
- (2) the N-acyl radicals derived from:
- (a) alkyl carboxylic acids having from one to about six carbon atoms,
- (b) aralkyl carboxylic acids having from seven to about ten carbon atoms,
- (c) amino acids selected from the group consisting of Met, Met(.fwdarw. O), Met (.fwdarw. O2), Glu, Ser, His, Phe, Arg, Lys, Trp, Gly, Val, Leu, Ala, Ileu, β-Ala, (α-Me) Ala, Pro, Tyr, and Thr,
- (d) peptides comprising two or three α-amino acids,
- (e) the N-alkylcarbonyl or N-aralkylcarbonyl derivatives of said amino acids, and
- (f) the N-alkylcarbonyl or N-aralkylcarbonyl derivatives of said peptides,
wherein the alkyl moiety in (e) and (f) has from one to about six carbon atoms, and wherein the aralkyl moiety in (e) and (f) has from seven to about ten carbon atoms;
- B is an amino acid residue selected from the group consisting of Phe, Trp, Tyr and --NH--CHR1 --CO--, wherein R1 is hydrogen or alkyl from one to about six carbon atoms; and
- X is a member selected from the group consisting of hydroxy, esterified hydroxy radicals of from one to eighteen carbon atoms, unsubstituted amino radicals, and substituted amino radicals selected from the group consisting of mono-alkyl (one to six carbons) amino, dialkyl-(one to six carbons) amino radicals, and radicals derived from amino acids or peptides having the sequence 17, 17-18, 17-19, up to and including 17-24 of the ACTH molcule, or a C-terminal ester o amide thereof, with the proviso that Arg may be replaced by Lys.
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| Background / Summary: |
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| Drawing Descriptions: |
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| Description: |
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| Forward References: |
Show 11 U.S. patent(s) that reference this one
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