Abstract: Compounds and compositions comprising synthetic analogs of Atrial Natriuretic Peptides are provided, together with methods for their production and use as natriuretics, diuretics and/or vasodilators, or as intermediates for or modulators of such useful compounds or of native Atrial Natriuretic Peptides.
Type:
Grant
Filed:
March 16, 1988
Date of Patent:
February 14, 1989
Assignee:
Biotechnology Research Associates, J.V.
Inventors:
John A. Lewicki, Robert M. Scarborough, Jr., Lorin K. Johnson
Abstract: This invention features a method for the solid phase synthesis of non-peptide bonds (CH.sub.2 --NH) in polypeptide chains. These polypeptides are synthesized by standard procedures and the non-peptide bond synthesized by reacting an amino aldehyde and an amino acid in the presence of NaCNBH.sub.3.This invention also features somatostatin analogs with non-peptide bonds.This invention further features a solid phase method of chemically modifying a peptide. The method involves synthesizing .alpha.-N-R and side group N-R analogs of peptides, where R is an alkyl or aryl group, by reacting a carbonyl-containing compound and an amino acid in the presence of NaCNBH.sub.3.
Type:
Grant
Filed:
June 27, 1986
Date of Patent:
February 7, 1989
Assignee:
The Administrators of the Tulane Educational Fund
Abstract: A process for the therapeutic treatment of cancer patients involving stimulation and promotion of the natural immune system (both T cell and NK cell activity) resisting and inhibiting tumorous growth (cancer) as well as resisting infections (viral, bacterial and fungal) by administering an effective dosage (e.g., 0.25 mg per kilogram of body weight to as low as about 10.sup.-14 mg/kg) of an endogenous endorphin (e.g., leucine-enkephalin and methionine-enkephalin).
Abstract: Human Growth Hormone-Releasing Factor (hGRF) analogs having the sequence [X.sup.3, Y.sup.8, Z.sup.25, Nle.sup.27 ]-hGRF(1-A)--B, wherein X, Y, and Z are selected from the group consisting of Asn and Asp, A has a value from 29-44, and B is NH.sub.2 or OH are synthesized and administered to animals to stimulate the release of Growth Hormone (GH).
Abstract: The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with an aromatic amino acid or the D-configuration converts bradykinin agonists into a bradykinin antagonist. The invention further includes additional modifications at other positions within the novel 7-position modified bradykinin antagonists which increase enzyme resistance, antagonist potency and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of the mammal and human body in which an excess of bradykinin or related kinins are produced or injected as by bites into the body.
Abstract: Many malignant neoplasias are treated by radiation therapy which can result in painful inflammation of the covering skin and/or mucosal membranes. Similarly, skin disorder patients receiving U.V. treatment may experience an inflammatory response.Certain neuropeptides have been discovered to have the unusual properties of preventing, or inhibiting, the edema and protein extravasation of skin and mucosal membrane injuries due to thermal or radiation assault or exposure to trauma or noxious agents. A method for inhibiting an inflammatory response in the skin or mucosal membranes of a patient is provided in which a therapeutically effective amount of a neuropeptide, such as Corticotropin Releasing Factor ("CRF") or its analogs, is administered.
Abstract: The invention relates to novel peptides, of pharmacological activity, of the formula: ##STR1## wherein R.sup.1 is hydrogen,R.sub.b.sup.1 is methyl,R.sup.2 is carboxy, carboxymethylcarbamoyl, 1-carboxyethylcarbamoyl or ethoxycarbonylmethylcarbamoyl,R.sup.q is carboxy or 3-t-butoxycarbonylcarbazoyl,R.sup.p is carboxy or methoxycarbonyl,R.sup.r is hydrogen, t-butoxycarbonyl or benzyloxycarbonyl,m is the integer 2, andn is the integer 1, or its pharmaceutically acceptable salt.
Abstract: The present invention deals with LHRH antagonists which possess improved water solubility and while having the high antagonist potency of the basic peptides, are free of the edematogenic effects. These compounds are highly potent in inhibiting the release of gonadotropins from the pituitary gland in mammals, including humans.The compounds of this invention are represented by the formulaX-R.sup.1 -R.sup.2 -R.sup.3 -Ser-Tyr-R.sup.6 -Leu-Arg-Pro-R.sup.10 -NH.sub.2whereinX is an acyl group derived from straight or branched chain aliphatic or alicyclic carboxylic acids having from 1 to 7 carbon atoms,R.sup.1 is D- or L-Pro, D- or L- .DELTA. .sup.3 -Pro, D-Phe, D-Phe(4-H1), D-Ser, D-Thr, D-Ala, D-Nal (1) or D-Nal (2),R.sup.2 is D-Phe or D-Phe(4-H1)R.sup.3 is D-Trp, D-Phe, D-Pal, D-Nal(1) or D-Nal (2),R.sup.6 is D-Cit, D-Hci, D-Cit(Q) or D-Hci(Q) andR.sup.
Abstract: DNA encoding the prepro inhibin .alpha. and .beta. chains has been isolated. This DNA is ligated into expression vectors and used to transform host cells for the preparation of inhibin or activin. Also provided are prohormone domains and other inhibin .alpha. or .beta. chain derivatives having therapeutic or diagnostic interest. The compositions provided herein are useful in the manipulation of fertility in animals.
Abstract: Tripeptide derivatives, characterized by the general formula:R.sub.1 --X--D--Arg--A--Arg--NH--R.sub.2wherein R.sub.1 is hydrogen, .alpha.- or .beta.-naphtyl residue, lower alkyl residue which may be substituted with a carboxyl group, unsubstituted or substituted phenyl- or phenylalkyl residue. ##STR1## or a single bond with the proviso that when R.sub.1 is hydrogen then and only then X is a single bondA=Gly or SarR.sub.2 =an aromatic or heterocyclic residue which gives a compound R.sub.2 --NH.sub.2 by enzymatic hydrolysis, which can be determined quantitativelyor disalts and trisalts of inorganic or organic acids thereof, process for their preparation and method for determination of serine proteases, especially Factor X.sub.a,or components which can interact with serine proteases or zymogen forms thereof.
Abstract: The invention relates to peptide derivatives of the formula ##STR1## in which ##STR2## represents an acyl radical, B represents the radical of a dipeptide composed of a N.sup..omega. -acylated basic .alpha.-amino acid and another .alpha.-amino acid, and W represents hydroxyl or optionally substituted amino, to a process for their preparation, to agents containing them, and to their use.
Type:
Grant
Filed:
December 12, 1986
Date of Patent:
January 10, 1989
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Volker Teetz, Stephan Henke, Dietrich Brocks, Hartmut Hanauske-Abel, Volkmar Gunzler
Abstract: A process for the synthesis, in liquid phase and by fragments, of hGRF 1-44 and hGRF 1-40. This process consists in coupling, one after the other and in the order of the sequence of the GRF,(1) on the one hand, the following fragments:__________________________________________________________________________ H--Ala--Arg--Ala--Arg--Leu--NH.sub.2 called Fragment A hGRF (40-44) or alaninamide (40) H--Gln--Glu--Arg--Gly--OH called Fragment B'.sub.1 hGRF (36-39) H--Glu--Ser--Asn--OH called Fragment B'.sub.2 hGRF (33-35) H--Ser--Arg--Gln--Gln--Gly--OH called Fragment C hGRF (28-32) H--Leu--Gln--Asp--Ile--Met--OH called Fragment D' hGRF (23-27) H--Arg--Lys--Leu--OH called Fragment E'.sub.1 hGRF (20-22) __________________________________________________________________________to obtain the peptide K.sub.
Type:
Grant
Filed:
August 21, 1987
Date of Patent:
January 10, 1989
Assignee:
Sanofi
Inventors:
Joseph Diaz, Henri Demarne, Romeo Roncucci, Paul-Henry Schmelck
Abstract: This invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is ##STR2## where X is oxygen or sulfur, Y is oxygen or nitrogen, and R.sup.11 represents straight or branched chain lower alkenyl having 2-6 carbon atoms, or phenyl, benzyl, and their equivalents such as nitro, halogen, or lower alkyl or lower alkoxy substituted phenyl or benzyl; wherein R.sup.2 and R.sup.3 may be the same or different and represent straight or branched chain lower alkyl having 1-6 carbon atoms, wherein R.sup.4 -R.sup.9 may be the same or different and represent hydrogen, or straight or branched chain lower alkyl having 1-6 carbon atoms; wherein C.sub.w is an asymmetric carbon atom when R.sup.7 and R.sup.8 are not the same and may be racemic or have the D or L configuration; and wherein C.sup.v is an asymmetric carbon atom and may be racemic or may have the D or L configuration.
Type:
Grant
Filed:
February 13, 1987
Date of Patent:
January 10, 1989
Assignee:
G. D. Searle & Co.
Inventors:
Barnett S. Pitzele, Donald W. Hansen, Jr., Robert W. Hamilton, Daniel R. Pilipauskas, Michael Clare
Abstract: Disclosed herein are antiviral peptides of the formula A-R.sup.8 -R.sup.9 -R.sup.10 -R.sup.11 -R.sup.12 -R.sup.13 -R.sup.14 -R.sup.15 -B wherein A is from zero up to seven amino acid residues and includes a terminal hydrogen or a terminal N-acyl, or A is a phenylacetyl with optional substitution of the para position of the phenyl, R.sup.8, R.sup.9, R.sup.10, R.sup.13, R.sup.14 and R.sup.15 are various amino acid residues with the stipulation that one or more of the four amino acid residues immediately preceding R.sup.11 may optionally be deleted, R.sup.11 and R.sup.12 are independently Val, D-Val, Nva, D-Nva, Leu, D-Leu, Nle, D-Nle, Ile or D-Ile, and B is hydroxy, amino or lower alkylamino. The antiviral activity of the peptides can be enhanced by combining them with a protease inhibitor. The peptides and the combination are useful for the treatment of herpes viral infections in mammals.
Type:
Grant
Filed:
May 7, 1987
Date of Patent:
January 3, 1989
Inventors:
Eric A. Cohen, Pierrette Gaudreau, Jacques Michaud, Paul Brazeau, Yves Langelier
Abstract: Pharmaceutical compositions containing a polypeptide of the cholecystokinin-cerulein group are effective in the treatment of shock conditions and of respiratory and cardiocirculatory insufficiences.The compositions of the invention may be administered by parenteral or inhalatory route at a dosage ranging from 5 to 20 .mu.g of active principle per kg of body weight.
Abstract: The parenteral administration of 80-160 .mu.g per kg body weight of substituted or unsubstituted fragments of ACTH (1-39) having formula ACTH (X-Y) wherein X is an integer from 1 to 5 and Y is an integer from 10 to 39 (provided that, when X is 1, Y is not 24) restores the normal blood pressure and respiratory frequence in a patient in serious shock conditions, particularly in hypovolemic shock.
Abstract: The present invention relates to a leukemia-associated virus immunogens, vaccines, antibody combining sites and assays. The immunogens are relatively short polypeptides with peptide sequences corresponding to the antigenic determinant domains of a leukemia-associated virus envelope protein. The immunogens when introduced into a host stimulate the production of antibodies which immunoreact with the polypeptides and the leukemia-associated virus.
Abstract: New pentapeptide of the formula ##STR1## in which X.sup.1 and X.sup.2 are the same or different and are OH or NH.sub.2,Y is H or OH,X.sup.3 is CO or CH.sub.2,one of the groups Z.sup.1 and Z.sup.2 is H and the other is H or CH.sub.3,all the amino acid unit being in L-configuration, with the exception that the C-terminal amino acid unit is in D-configuration when Z.sup.2 is methyl,and the C-terminal carboxyl group may be reduced to --CH.sub.2 --OH or be in amide form, and cation complexes and salts thereof.The pentapeptide may be prepared by subjecting a protected derivative thereof to deprotection.The pentapeptide has cell growth regulatory activity.