US4215112A
Expired / Lapsed
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Tripeptides and methods
Assignee: Ortho Pharmaceutical Corp
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Filing: 1979-03-14
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Granted: 1980-07-29
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Expires: 1999-03-14
Abstract
Abstract There are disclosed new biological active polypeptides: A--X--B wherein A is deamino-LYS or LYS; X is a suitable neutral aliphatic amino acid residue; e.g., one selected from the group consisting of SER, ALA, 2-Me-ALA, GLY, LEU, THR, D-SER, D-ALA, D-THR, allo-THR, D-LEU, and SAR; B is GLN-R', decarboxy-GLN, or ##STR1## and R' is a substituent which does not substantially affect the biological activity of the tripeptide. These polypeptides have the capability of inducing the differentiation of T-lymphocytes as measured by the acquisition of the thymic differentiation antigen Th-1, as well as B-lymphocytes as measured by the acquisition of the differentiation antigen Bu-1. The polypeptides are thus useful in thymic function and immunity areas such as in treatment for congenital absence of thymus. Also provided are therapeutic compositions and methods for use of the polypeptides.
Inventors
- 👤 Gideon Goldstein
- 👤 George Heavner
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 00:54
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/08; C07K5/0815; A; A61; A61P; A61P37/00; A61P37/02; A61P37/04; A61P43/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/18
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
136 words
A polypeptide having the capability of inducing the differentiation of both Th-1 + T-lymphocytes and Bu-1 + B-lymphocytes, said polypeptide having the formula: A--X--B wherein A is deamino-LYS or LYS; X is a suitable neutral aliphatic amino acid residue selected from the group consisting of SER, ALA, 2-Me-ALA, GLY, LEU, THR, D-SER, D-ALA, D-THR, allo-THR, D-LEU, and SAR; B is GLN-R', decarboxy-GLN, or ##STR7## R' is a member selected from the group consisting of OH, NH 2 , NHR", N(R") 2 , OR", GLY, GLY--GLY, GLY--GLY--SER, and GLY--GLY--SER--ASN; and R" is a member selected from the group consisting of C 1 -C 7 alkyl, C 6 -C 12 aryl, C 6 -C 20 alkaryl, C 6 -C 20 aralkyl, C 2 -C 7 alkenyl, and C 2 -C 7 alkynyl; and the pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
136 words
A polypeptide having the capability of inducing the differentiation of both Th-1 + T-lymphocytes and Bu-1 + B-lymphocytes, said polypeptide having the formula: A--X--B wherein A is deamino-LYS or LYS; X is a suitable neutral aliphatic amino acid residue selected from the group consisting of SER, ALA, 2-Me-ALA, GLY, LEU, THR, D-SER, D-ALA, D-THR, allo-THR, D-LEU, and SAR; B is GLN-R', decarboxy-GLN, or ##STR7## R' is a member selected from the group consisting of OH, NH 2 , NHR", N(R") 2 , OR", GLY, GLY--GLY, GLY--GLY--SER, and GLY--GLY--SER--ASN; and R" is a member selected from the group consisting of C 1 -C 7 alkyl, C 6 -C 12 aryl, C 6 -C 20 alkaryl, C 6 -C 20 aralkyl, C 2 -C 7 alkenyl, and C 2 -C 7 alkynyl; and the pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
70 words
A polypeptide according to claim 1, having the formula: A--SAR--B wherein A is deamino-LYS or LYS; B is GLN-R', decarboxy-GLN, or ##STR8## R' is a member selected from the group consisting of OH, NH 2 , NHR", N(R") 2 , and OR"; and R" is a member selected from the group consisting of C 1 -C 7 alkyl and C 6 -C 12 aryl; and the pharmaceutically acceptable salts thereof.
Claim 4
Dependent Claim
44 words
A polypeptide according to claim 1, having the formula: A--SAR--B wherein A is deamino-LYS or LYS; B is GLN-R', decarboxy-GLN, or ##STR9## and R' is a member selected from the group consisting of OH and NH 2 ; and the pharmaceutically acceptable salts thereof.
Claim 5
Dependent Claim
13 words
A polypeptide of the following sequence: H--LYS--SAR--GLN--NH.sub.2 and the pharmaceutically acceptable salts thereof.
Claim 6
Dependent Claim
13 words
A polypeptide of the following sequence: H--LYS--SAR--GLN--NH.sub.2 and the pharmaceutically acceptable salts thereof.
Claim 7
Dependent Claim
13 words
A polypeptide of the following sequence: Deamino-LYS--SAR--GLN--NH.sub.2 and the pharmaceutically acceptable salts thereof.
Claim 8
Dependent Claim
13 words
A polypeptide of the following sequence: Deamino-LYS--SAR--GLN--NH.sub.2 and the pharmaceutically acceptable salts thereof.
Claim 9
Dependent Claim
13 words
A polypeptide of the following sequence: H--LYS--SAR--GLN--OH and the pharmaceutically acceptable salts thereof.
Claim 10
Dependent Claim
13 words
A polypeptide of the following sequence: H--LYS--SAR--GLN--OH and the pharmaceutically acceptable salts thereof.
Claim 11
Dependent Claim
13 words
A polypeptide of the following sequence: Deamino--LYS--SAR--GLN--OH and the pharmaceutically acceptable salts thereof.
Claim 12
Dependent Claim
13 words
A polypeptide of the following sequence: Deamino--LYS--SAR--GLN--OH and the pharmaceutically acceptable salts thereof.
Claim 13
Dependent Claim
21 words
A therapeutic composition of matter comprising a therapeutically effective amount of the polypeptide of claim 1 in a pharmaceutically acceptable carrier.
Claim 14
Dependent Claim
30 words
A therapeutic composition of matter for parenteral administration according to claim 8, wherein the therapeutically effective amount of the polypeptide ranges from about 1 to about 100 μg/kg body weight.
Claim 15
Dependent Claim
31 words
A therapeutic composition of matter for oral administration according to claim 8, wherein the therapeutically effective amount of the polypeptide ranges from about 100 μg/kg to about 10 mg/kg body weight.
Claim 16
Dependent Claim
29 words
A method for the treatment of conditions resulting from relative or absolute T cell deficiencies which comprises administration of a therapeutically effective amount of the polypeptide of claim 1.
Claim 17
Dependent Claim
29 words
A method for the treatment of conditions resulting from relative or absolute B cell deficiencies which comprises administration of a therapeutically effective amount of the polypeptide of claim 1.
Claim 18
Dependent Claim
28 words
A method for inducing bone marrow cells to develop the characteristics of thymus-derived lymphocytes which comprises administration of a therapeutically effective amount of the polypeptide of claim 1.
Claim 19
Dependent Claim
29 words
A method for inducing bone marrow cells to develop the characteristics of immunocompetent B cells which comprises administration of a therapeutically effective amount of the polypeptide of claim 1.
Claim 20
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 polypeptide of claim 1.
Claim 21
Dependent Claim
42 words
A method for affecting the immune response in the body to assist in the correction of relative or absolute deficiencies of the body tissues which differentiate B cells which comprises administration of a therapeutically effective amount of the polypeptide of claim 1.
References Cited (Backward Citations)
US4098777A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-07-29 | 1984-01-28 | 1984-07-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-07-29 | 1988-01-28 | 1988-07-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-07-29 | 1992-01-28 | 1992-07-29 | $7700.00 | Window Closed / Lapsed |