US4190646A
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US
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Polypeptide compositions and methods
Assignee: Memorial Sloan Kettering Cancer Center
•
Filing: 1979-01-26
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Granted: 1980-02-26
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Expires: 1999-01-26
Abstract
Abstract There are disclosed polypeptide compositions having the following amino acid sequence as the active site: ARG-LYS-ASP-VAL-TYR These polypeptides have the capability of inducing the differentiation of T-lymphocytes but not of complement receptor (CR+) B-lymphocytes and thus are useful in a number of therapeutic areas. Also provided are derivatives of the pentapeptide, novel intermediate polypeptides, methods of manufacture of the peptides, therapeutic compositions, and methods for use of the compositions.
Inventors
- 👤 Gideon Goldstein
- 👤 David H. Schlesinger
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 22:52
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/66; C07K5/00; C07K5/04; C07K5/10; C07K5/1019; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/18
Claims Analysis
Total Claims: 35
Claim 1
Independent Claim
154 words
A polypeptide having the biological capability of inducing the differentiation of T-lymphocytes but not of complement receptor (CR + ) B lymphocytes, said polypeptide having the following sequence: R-NH-ARG-LYS-ASP-VAL-TYR-COR' wherein R and R' are terminal groups on said polypeptide which do not substantially affect the biological capability thereof, and the pharmaceutically acceptable salts, and wherein R and R' are selected from the groups consisting of: ______________________________________
R R'
______________________________________
Hydrogen OH
C.sub.1 --C.sub.7 alkyl
NH.sub.2
C.sub.5 --C.sub.12 aryl
NHR.sub.7
C.sub.6 --C.sub.20 alkaryl
N(R.sub.7).sub.2
C.sub.6 --C.sub.20 aralkyl
OR.sub.7
C.sub.1 --C.sub.7 alkanoyl
VAL
C.sub.2 --C.sub.7 alkenyl
GLN
C.sub.2 --C.sub.7 alkynyl
LEU
GLN TYR
GLU VAL-GLN
GLY VAL-LEU
GLU-GLN
GLY-GLN VAL-TYR
GLY-GLU GLN-LEU
GLY-GLU-GLN GLN-TYR
GLN-VAL
LEU-TYR
LEU-LEU
TYR-LEU
VAL-GLN-LEU
VAL-GLN-LEU-TYR
______________________________________ wherein R 7 is C 1 -C 7 alkyl, C 2 -C 7 alkenyl, C 2 -C 7 alkynyl, C 6 -C 20 aryl, C 6 -C 20 aralkyl, or C 6 -C 20 alkaryl.
Claim 2
Dependent Claim
154 words
A polypeptide having the biological capability of inducing the differentiation of T-lymphocytes but not of complement receptor (CR + ) B lymphocytes, said polypeptide having the following sequence: R-NH-ARG-LYS-ASP-VAL-TYR-COR' wherein R and R' are terminal groups on said polypeptide which do not substantially affect the biological capability thereof, and the pharmaceutically acceptable salts, and wherein R and R' are selected from the groups consisting of: ______________________________________
R R'
______________________________________
Hydrogen OH
C.sub.1 --C.sub.7 alkyl
NH.sub.2
C.sub.5 --C.sub.12 aryl
NHR.sub.7
C.sub.6 --C.sub.20 alkaryl
N(R.sub.7).sub.2
C.sub.6 --C.sub.20 aralkyl
OR.sub.7
C.sub.1 --C.sub.7 alkanoyl
VAL
C.sub.2 --C.sub.7 alkenyl
GLN
C.sub.2 --C.sub.7 alkynyl
LEU
GLN TYR
GLU VAL-GLN
GLY VAL-LEU
GLU-GLN
GLY-GLN VAL-TYR
GLY-GLU GLN-LEU
GLY-GLU-GLN GLN-TYR
GLN-VAL
LEU-TYR
LEU-LEU
TYR-LEU
VAL-GLN-LEU
VAL-GLN-LEU-TYR
______________________________________ wherein R 7 is C 1 -C 7 alkyl, C 2 -C 7 alkenyl, C 2 -C 7 alkynyl, C 6 -C 20 aryl, C 6 -C 20 aralkyl, or C 6 -C 20 alkaryl.
Claim 3
Dependent Claim
48 words
A pentapeptide of the following sequence: R-NH-ARG-LYS-ASP-VAL-TYR-COR' wherein R is hydrogen, C 1 -C 7 alkyl, C 5 -C 12 aryl, or C 1 -C 7 alkanoyl and R' is OH, NH 2 , NHR 7 , or N(R 7 ) 2 , and the pharmaceutically acceptable salts.
Claim 4
Dependent Claim
48 words
A pentapeptide of the following sequence: R-NH-ARG-LYS-ASP-VAL-TYR-COR' wherein R is hydrogen, C 1 -C 7 alkyl, C 5 -C 12 aryl, or C 1 -C 7 alkanoyl and R' is OH, NH 2 , NHR 7 , or N(R 7 ) 2 , and the pharmaceutically acceptable salts.
Claim 5
Dependent Claim
13 words
A polypeptide of the following sequence: H.sub.2 N-ARG-LYS-ASP-VAL-TYR-COOH and the pharmaceutically acceptable salts.
Claim 6
Dependent Claim
13 words
A polypeptide of the following sequence: H.sub.2 N-ARG-LYS-ASP-VAL-TYR-COOH and the pharmaceutically acceptable salts.
Claim 7
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R is hydrogen and R' is OH.
Claim 8
Dependent Claim
16 words
A polypeptide according to claim 1 wherein R is CH 3 CO-- and R' is OH.
Claim 9
Dependent Claim
15 words
A polypeptide according to claim 1 wherein R is CH 3 and R' is OH.
Claim 10
Dependent Claim
16 words
A polypeptide according to claim 1 wherein R is H and R' is --NH 2 .
Claim 11
Dependent Claim
16 words
A polypeptide according to claim 1 wherein R is H and R' is --NH(CH 3 ).
Claim 12
Dependent Claim
20 words
A polypeptide according to claim 1 wherein R is H and R' is --NH(C 2 H 5 ) 2 .
Claim 13
Dependent Claim
18 words
A polypeptide according to claim 1 wherein R is CH 3 CO-- and R' is NH 2 .
Claim 14
Dependent Claim
16 words
A polypeptide according to claim 1 wherein R is H and R' is --OCH 3 .
Claim 15
Dependent Claim
18 words
A polypeptide according to claim 1 wherein R is H and R' is OC 2 H 5 .
Claim 16
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R is phenyl and R' is --OH.
Claim 17
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R is benzyl and R' is --OH.
Claim 18
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R is tolyl- and R' is --OH.
Claim 19
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R is GLN and R' is --OH.
Claim 20
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R is GLU and R' is --OH.
Claim 21
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R is GLY and R' is --OH.
Claim 22
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R is H and R' is VAL.
Claim 23
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R is H and R' is GLN.
Claim 24
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R is H and R' is LEU.
Claim 25
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R is H and R' is TYR.
Claim 26
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R is H and R' is VAL-GLN.
Claim 27
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R in GLN and R' is VAL.
Claim 28
Dependent Claim
14 words
A polypeptide according to claim 1 wherein R is GLU-GLN and R' is VAL-GLN.
Claim 29
Dependent Claim
21 words
A therapeutic composition of matter comprising a therapeutically effective amount of a polypeptide of claim 1 in a pharmaceutically acceptable carrier.
Claim 30
Dependent Claim
27 words
A therapeutic composition of matter according to claim 26 wherein the therapeutically effective amount of the polypeptide ranges from about 0.1 to 10 mg/kg of body weight.
Claim 31
Dependent Claim
29 words
A method for the treatment of conditions resulting from relative or absolute T cell deficiencies which comprise administration of a pharmaceutically effective amount of the composition of claim 1.
Claim 32
Dependent Claim
28 words
A method for inducing bone marrow cells to develop the characteristics or thymus-derived lymphocytes which comprises administration of a therapeutically effective amount of the composition of claim 1.
Claim 33
Dependent Claim
37 words
A method for affecting the immune response in the body to assist in the correction of relative or absolute deficiencies of the thymus which comprises administration of a therapeutically effective amount of the composition of claim 1.
Claim 34
Dependent Claim
26 words
A method for the treatment of conditions resulting from excess neuromuscular activity which comprises administration of a therapeutically effective amount of the composition of claim 1.
Claim 35
Dependent Claim
24 words
A method for inhibiting the uncontrolled proliferation of Thymopoietin-responsive lymphocytes which comprises administration of a therapeutically effective amount of the composition of claim 1.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-02-25 | 1983-08-27 | 1984-02-26 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-02-25 | 1987-08-27 | 1988-02-26 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-02-25 | 1991-08-27 | 1992-02-26 | $7700.00 | Window Closed / Lapsed |