Abstract: Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

Abstract: Provided is a pharmaceutical composition for prevention and treatment of drug or alcohol addiction or bipolar disorder, comprising sodium phenylbutyrate (PBA). The pharmaceutical composition for prevention and treatment of drug or alcohol addiction or bipolar disorder in accordance with the present invention provides effects capable of inhibiting increases in locomotor activity which is a behavioral indicator of drug or alcohol addiction or bipolar disorder, by controlling a level of a neurotransmitter via regulation of expression of a neurotransmitter transporter.

Abstract: Benzodiazepine withdrawal induced anxiety is treated by administration of an enkephalinase inhibitor, and a gamma-aminobutyric acid (“GABA”) precursor, or an endorphin or enkephalin releaser. These components promote restoration of normal neurotransmitter function and are non-addictive. Use of the enkephalinase inhibitor D-phenylalanine, the GABA precursor glutamine, the serotonin precursor 5-HTP, glycine, and taurine, in combination with coenzymatic functionality of folic acid is preferred for activation of ligand-gated Cl? channel in the central nervous system. Food supplement embodiments provide the human body nutritional supplements to intake certain neurotransmitter precursor substrates, thereby enabling patients of all ages to self-regulate their ability to quell perturbations to equilibrium and simultaneously to adverse effects upon normal physiological and psychological functioning attributable to induced anxiety and panic associated with benzodiazepine withdrawal.

Abstract: A composition including a compound which binds to a receptor for glucagon-like peptide-1 and a pharmaceutical carrier. The amount of the compound present is effective to control appetite in a human. Also disclosed is a method for controlling appetite and for reducing food intake in a human by administering to the human a composition comprising a compound which binds to a receptor for glucagon-like peptide-1 and a pharmaceutical carrier.

Abstract: A method of spherifying a sustained release ionic conjugate which contains a free carboxyl group-containing polymer and a free amino group-containing drug which are ionically bonded to each other.

Abstract: An active &bgr;-endorphin fragment or an analog of such a fragment is provided to a patient for alleviating the effect of muscle-wasting disease and for inhibiting or reducing leakage of an enzyme from a living muscle. The &bgr;-endorphin fragment is selected from &bgr;-endorphin (30, 31), &bgr;-endorphin (29-31), &bgr;-endorphin (28-31) and stabilized analogs thereof.

Abstract: Disclosed is a sustained release pharmaceutical composition. The composition includes a polyester containing a free COOH group ionically conjugated with a bioactive polypeptide comprising at least one effective ionogenic amine, wherein at least 50% by weight of the polypeptide present in the composition is ionically conjugated to the polyester.

Abstract: This invention relates to novel salts composed of a cation derived from a peptide containing at least one basic group and an anion derived from a carboxy-terminated polyester, processes for the manufacture of such salts, and the use of such salts in the manufacture of extended release pharmaceutical compositions. The salts of the invention possess a variety of properties which are useful in the formulation of extended release pharmaceutical compositions, whether the salts are in pure form or are in admixture with either an excess of the peptide in its free, unbound form or an excess of the free polyester.

Abstract: This invention relates to novel salts composed of a cation derived from a peptide containing at least one basic group and an anion derived from a carboxy-terminated polyester, processes for the manufacture of such salts, and the use of such salts in the manufacture of extended release pharmaceutical compositions. The salts of the invention possess a variety of properties which are useful in the formulation of extended release pharmaceutical compositions, whether the salts are in pure form or are in admixture with either an excess of the peptide in its free, unbound form or an excess of the free polyester.

Abstract: Disclosed is a sustained release pharmaceutical composition. The composition includes a polyester containing a free COOH group ionically conjugated with a bioactive polypeptide comprising at least one effective ionogenic amine, wherein at least 50% by weight of the polypeptide present in the composition is ionically conjugated to the polyester.

Abstract: A composition including a polyester containing one or more free COOH groups ionically conjugated with a bioactive polypeptide comprising at least one effective ionogenic amine, wherein the polyester contains a member selected from the group of L-lactic acid, D-lactic acid, DL-lactic acid, .epsilon.-caprolactone, p-dioxanone, .epsilon.-caprolic acid, alkylene oxalate, cycloalkylene oxalate, alkylene succinate, .beta.-hydroxybutyrate, substituted or unsubstituted trimethylene carbonate, 1,5-dioxopan-2-one, 1,4-dioxepan-2-one, glycolide, glycolic acid, L-lactide, D-lactide, DL-lactide, meso-lactide, and any optically active isomers, racemates or copolymers thereof, and at least 50%, by weight, of the polypeptide present in the composition is ionically conjugated to said polyester.

Abstract: The present invention provides substituted cyclic pentapeptide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable slats, esters and amides thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: Cyclic disulfide and linear dynorphin Dyn A.sub.1-11 and dynorphin Dyn A.sub.1-13 analogs which are highly specific for .kappa. opioid receptors. These analogs are useful in pharmaceutical compositions and for the analysis of opioid receptor/ligand interactions.

Abstract: Solid nasal inserts of calcitonin and other peptides have particularly interesting drug absorption profiles.

Abstract: Pharmaceutical compositions in the form of a buccal tablet comprising etorphine or a salt thereof, at least one monosaccharide, disaccharide or a mixture thereof, and a mixture of xanthan gum and locust bean gum in a weight ratio 3:1 to 1:1, wherein the total weight of the mono- and/or di-saccharides relative to the combined weight of the xanthan and locust bean gums is in the ratio of 20:1 to 3:1. The tablet affords improved bioavailability.

Abstract: A process for the therapeutic treatment of AIDS (acquired immune deficiency syndrome) 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.-4 mg/kg) of an endogenous endorphin (e.g., leucine-enkephalin and methionine-enkephalin).

Abstract: A novel polypeptide is defined by the below shown formula and is useful as an analgesic. ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each represents a hydrogen atom or a lower alkyl or lower alkenyl group, A represents a D-amino acid, Gly or Sar provided that when the D-amino acid is D-Cys, it is bonded with L-Cys or D-Cys in position 5 through a S--S bond to effect intramolecular ring closure, B represents L-Phe or D-Phe in which the benzene ring may be substituted or an .alpha.-N-alkyl derivative thereof, C represents an L-amino acid, D-Cys or an .alpha.-N-alkyl derivative thereof, D and E each represent an L- or D-basic amino acid or an .alpha.-N-alkyl derivative thereof, F represents a group of the formula --OR.sup.3 (in which R.sup.3 is H or a lower alkyl group), a group of the formula: ##STR2## (in which R.sup.4 and R.sup.5 are the same or different and each represents H or a lower alkyl group), a group of the formula: --G--OR.sup.

Abstract: A method of treatment for patients suffering from cerebral ischemia is provided by administering an opioid peptide. Particulary preferred is the administration of dynorphin, or dynorphin-related peptides, in the acid or amidated form. Practice of the invention is useful in prolonging survival.

Abstract: A pharmaceutical composition containing a hydrophilic drug which is poorly absorbable through the gastrointestinal tract, and cyclodextrin, increases the absorbability of the drug into the mammalian body when administered by a non-oral or non-injection route.

Abstract: Pharmacologically active peptides of the following formulas are described:L--Tyr--X--L--Phe--X--TL--Tyr--X--L--Phe--X--A--TL--Tyr--X--L--Phe--X--A--X--TL--Tyr--X--L--Phe--X--A--X--B--Tin which L--Tyr is the N-terminal amino acid residue L-tyrosine, X any amino acid residue of the D-form, L--Phe is the amino acid L-phenylalanine, A and B are any desired amino acid residues and T is the C-terminal carboxyl group, which is further disclosed in the description.The substances are suitable for the therapy of diseases.

Abstract: Therapeutically useful pseudopeptides characterized by the replacement of at least one peptide group, both in a naturally occurring peptide or protein by a thiomethylene group are useful in the treatment of various metabolic malfunctions.

Abstract: The invention relates to novel enkephalin analogs of the formula: ##STR1## which are useful as analgesic agents.

Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sub.1 represents straight or branched lower alkyl having 1 to 4 carbons;R.sub.2 represents hydrogen, hydroxy, --OCO.sub.2 R.sub.1 substituent or lower alkyl having 1 to 4 carbons;R.sub.3 represents a hydrogen or lower alkyl having 1 to 6 carbons;R.sub.4 and R.sub.5 may be the same or different and represent hydrogen or lower alkyl having 1 to 6 carbons;n is 1 to 6;X represents a hydrogen, hydroxy or OCO.sub.2 R.sub.1 substituent;A represents a cyclohexyl, phenyl or phenyl substituted with one or more lower alkyls containing 1 to 6 carbons, one or more amino, hydroxy, halogen, nitro or lower alkoxy substituent having 1 to 6 carbons;V represents the asymmetric carbon that may be racemic or have the D or L configuration;W represents the asymmetric carbon when R.sub.4 and R.sub.

Abstract: A class of dipeptide derivatives having opiate activity having the formulaTyrosyl--X--Ywherein X is a D- or L-amino acid radical and Y is an amide or substituted amide are disclosed.

Abstract: Novel peptides of formula (I) ##STR1## wherein R.sup.1 is hydrogen, alkyl of 1 or 2 carbon atoms or an amidino group,R.sup.2 is alkyl of 1 or 2 carbon atoms,R.sup.3 is hydrogen or carbamyl,X.sup.2 is a D-radical having the structure: ##STR2## Z.sup.1 and Z.sup.2 are the same or different and each is hydrogen, halo, nitro or trifluoromethyl and at least one is other than hydrogen,m is 2, 3 or 4 andn is 0, 1 or 2,provided that when R.sup.3 is carbamyl then n is always 1;and salts thereof.The compounds have a selectively peripheral analgesic effect when administered to mammals and also exhibit antidiarrhoeal and antitussive activity and may thus be used in human or veterinary medicine for the relief or prevention of pain, for the treatment of diarrhoea or dysentery and for the suppression of cough.

Abstract: A process of stimulating and promoting the natural immune system (T cells and NK cells) resisting and inhibiting the growth of tumorous cells as well as resisting infections (virus bacteria, and fungi) is disclosed. Endogenous endorphins are disclosed as the agent for stimulating the immune system.

Abstract: A genus of dipeptide amides including as the preferred subgenus the dipeptide amides having the structural formula R.sub.1 TyrR.sub.2 D-AlaNHR.sub.4 wherein R.sub.1 and R.sub.2 are each hydrogen or alkyl provided that at least one of them is other than hydrogen and R.sub.4 is phenylalkyl or substituted-phenylalkyl are prepared by condensing the dipeptide with the amine or the amino acid with the amino acid amide and are useful as analgesics.

Abstract: A genus of dipeptide amides including as the preferred subgenus the dipeptide amides having the structural formula HTyrD-AlaNR.sub.2 R.sub.3 wherein R.sub.2 is phenylalkyl or substituted-phenylalkyl and R.sub.3 is hydrogen, alkyl, phenylalkyl, substituted-phenylalkyl or X-alkyl wherein X is an electronegative moiety are prepared by condensing the dipeptide with the amine or the amino acid with the amino acid amide and are useful as analgesics.

Abstract: Novel compounds which are capable of binding with enhanced specificity to the delta receptor are disclosed. The compounds are a series of cyclic, conformationally constrained analogs of enkephalins which display exceptional delta receptor specificity. The compounds of the present invention are polypeptides of the formula: ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, methyl, or lower alkyl having 1 to 5 carbon atoms;R.sup.3 and R.sup.4, which may be the same or different, are hydrogen, methyl, or lower alkyl having 1 to 5 carbon atoms, provided, however that R.sup.1, R.sup.2, R.sup.3, and R.sup.4 may not all be hydrogen when both n and m are zero;R.sup.5 is hydrogen, L-tyrosine, D-tyrosine, or L-tyrosine or D-tyrosine substituted on the N.sup..alpha. -amino with 1 or 2 lower alkyl or alkenyl groups;R.sup.6 is a substituted or unsubstituted aromatic;R.sup.7 is hydrogen or methyl;R.sup.

Abstract: In one aspect, compounds capable of inhibiting an endopeptidase responsible for a degradation pathway of enkephalin and having the general formulaA--B--NHOHwherein A is one of the aromatic group-containing amino acid residues L-tryptophyl, D-tryptophyl, L-tyrosyl, D-tyrosyl, L-phenylalanyl, or D-phenylalanyl, and B is one of the amino acids glycine, L-alanine, D-alanine, L-leucine, D-leucine, L-isoleucine, or D-isoleucine; or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to novel enkephalin analogs of the formula: ##STR1## which are useful as analgesic agents.