Abstract: New N-alkyl and N-acyl derivatives of A82846A, A82846B, A82846C and PA-42867-A are provided. The new glycopeptide derivatives are useful for the treatment of susceptible bacterial infections, especially infections due to Gram-positive microorganisms.

Abstract: The invention relates to fluorogenic compounds for the detection of hydrolyzing enzymes and the use of the fluorogenic compounds.

Abstract: Compounds which inhibit interleukin-1.beta. protease activity, pharmaceutical compositions containing the compounds and methods using the compounds are provided. The compounds have the formula ##STR1## wherein n is 0-2; each AA is independently L-valine or L-alanine; R.sub.1 is selected from the group consisting of N-[4-(N,N-dimethylaminomethyl)]benzoyl, N-benzyloxycarbonyl, N-methyl-N-[4-(pyridyl)methyl], N-[4-(pyridyl)methyl]carbonyl, N-3-(piperidinopropionyl), N-[4-(morpholinoethoxy)benzoyl, N-2-(quinuclidinyl)carbonyl, N-(3-pyridyl)methoxy carbonyl, N-(2-pyridyl)methoxy carbonyl, N-methyl-N-benzyl carbonyl, N-methyl-N-[2-(4-pyridyl)ethyl]carbonyl, and N-(N-phenylpiperazino)carbonyl; and R.sub.8, R.sub.9, R.sub.10 are each independently hydrogen, lower alkyl, halo substituted methyl, carbalkoxy, benzyl, phenyl, or phenyl mono or disubstituted with fluoro, nitro, methoxy, chloro, trifluoromethyl or methanesulfonyl.

Abstract: The invention provides substantially purified T-cadherin polypeptides and isolated nucleic acids which encode the T-cadherin polypeptides. Antibodies reactive with various forms of T-cadherin, but not reactive with N-, E- or P-cadherin are also provided. The invention provides methods for detecting the various forms of T-cadherin in a subject as well as a method of detecting tumor growth which consists of inhibiting the activity of T-cadherin in a tumor. A method of effecting traumatized neurons is provided. The method entails treating traumatized neurons with a therapeutically effective dose of T-cadherin.

Abstract: The present invention provides novel peptidylaldehyde inhibitors of proteolysis mediated by the multicatalytic proteinase complex (MPC) or proteasome. The inhibitors have the general formulaZ-P.sub.4 -P.sub.3 -P.sub.2 -P.sub.1 -CHO (I)whereinP.sub.1 is selected from among branched chain amino acids occurring naturally in proteins and norleucine;P.sub.2 is selected from among non-polar L-amino acids;P.sub.3 is proline or hydroxyproline;P.sub.4 is selected from among non-polar L-amino acids;CHO is an aldehyde replacement for the COOH group on the P.sub.1 amino acid; andZ is an amino blocking group attached to the NH.sub.2 group on the P.sub.4 amino acid.The amino blocking group Z may be chosen from among benzyloxycarbonyl, benzoylglycine, tertiary butoxycarbonyl, acetylbenzyloxycarbonyl, benzoylglycine, tertiary butoxycarbonyl, acetyl or other NH.sub.2 blocking groups known in protein and peptide chemistry.

Abstract: Compounds which inhibit amylin activity are provided. These compounds may be used in the treatment of conditions where it is of benefit to reduce amylin activity, including the treatment of Type 2 diabetes mellitus, impaired glucose tolerance, obesity and insulin resistance.

Abstract: Novel peptoids of .alpha.-substituted Trp derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further the compounds are antianxiety agents and antiulcer agents. They are agents useful for preventing the response to withdrawal from chronic treatment or use of nicotine, diazepam, alcohol, cocaine, caffeine, or opioids. The compounds are also useful in the treatment and/or prevention of panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the peptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare diagnostic compositions.

Abstract: Peptide-chelator conjugates are provided that when labelled with a traceable metal are useful for diagnostic imaging of sites of inflammation. The peptide component is an antagonist of the naturally occurring tetrapeptide tuftsin while the chelator component serves as a labelling site for metals, in particular radionuclide metals such as technetium-99m.

Abstract: The present invention relates to a family of peptides encoding antagonists of the vasoactive intestinal peptide (VIP) designed to distinguish multiple receptors that mediate VIP neurotransmission, neurotrophism and cell division. The invention also relates to methods of using these peptides to antagonize VIP-associated activity and function. The invention further relates to pharmaceutical compositions dsigned to inhibit VIP-associated activity.

Abstract: A method for the treatment of dehydration or nitrogen deficiency-based malnutrition is provided which involves administering to a patient in need thereof an effective amount of a compound selected from oligopeptides formed from the coupling of one or more amino acids with glutamine, the product of coupling glucose with glutamine, the product of coupling glucose and one or more amino acids with glutamine, or the product from acylating glutamine with a carboxylic acid having from 2 to 6 carbon atoms.

Abstract: Compounds of the formula: ##STR1## or the amides, esters or salts thereof, wherein: L is an electron withdrawing leaving group;S.sup.x is S.dbd.O, O.dbd.S.dbd.O, S.dbd.NH, HN.dbd.S.dbd.O, Se.dbd.O, O.dbd.Se.dbd.O, Se.dbd.NH, HN.dbd.Se.dbd.O, S.sup.+ R.sup.4 wherein R.sup.4 is alkyl (1-6C), or O--C.dbd.O or HN--C.dbd.O;each R of R.sup.1, R.sup.2 and R.sup.3 is independently H or a noninterfering substituent;n is 0, 1 or 2;Y is selected from the group consisting of ##STR2## wherein m is 1 or 2; and AA.sub.C is an amino acid linked through a peptide bond to the remainder of said compound of formula 1, are disclosed.These compounds are useful prodrugs for selective treatment of target tissues which contain compatible glutathione S-transferase (GST) isoenzymes, and simultaneously elevate the levels of GM progenitor cells in bone marrow.

Abstract: There is provided metal-peptide compositions for use as stimulating agents for hair growth in warm-blooded animals. Methods for stimulating the growth of hair in warm-blooded animals are also disclosed. The methods utilize a stimulating effective amount of the metal-peptide composition or a pharmaceutical preparation containing the metal-peptide composition.

Abstract: Disclosed herein are inbibitors of the multicatalytic protease enzyme which are represented by the general formula: ##STR1## Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.

Abstract: The present invention discloses various parenteral pharmaceutical formulations, which comprise a mixture of a monomeric insulin analog and insulin-NPH. The analog formulations provide a rapid onset and a prolonged duration of action.

Abstract: Compounds of the formula: ##STR1## or the amides, esters or salts thereof, wherein: L is an electron withdrawing leaving group;S.sup.x is S=O, O=S=O, S=NH, HN=S=O, Se=O, O=Se=O, Se=NH, HN=Se=O, S+R.sup.4 wherein R.sup.4 is alkyl (1-6 C), or O--C=O or HN--C=O;each R of R.sup.1, R.sup.2 and R.sup.3 is independently H or a noninterfering substituent;n is 0, 1 or 2;Y is selected from the group consisting of ##STR2## wherein m is 1 or 2; and AA.sub.C is an amino acid linked through a peptide bond to the remainder of said compound of formula 1, are dislosed.These compounds are useful prodrugs for selective treatment of target tissues which contain compatible glutathione S-transferase (GST) isoenzymes.

Abstract: The invention provides effective analogs of the active GLP-1 peptides, 7-34, 7-35, 7-36, and 7-37, which have improved characteristics for treatment of diabetes Type II. These analogs have amino acid substitutions at positions 7-10 and/or are truncated at the C-terminus and/or contain various other amino acid substitutions in the basic peptide. The analogs may either have an enhanced capacity to stimulate insulin production as compared to glucagon or may exhibit enhanced stability in plasma as compared to GLP-1 (7-37) or both. Either of these properties will enhance the potency of the analog as a therapeutic. Analogs having D-amino acid substitutions in the 7 and 8 positions and/or N-alkylated or N-acylated amino acids in the 7 position are particularly resistant to degradation in vivo.

Abstract: Optically pure .alpha.-ketoamide compounds, and use therefor in treating neurodegenerative pathologies having enhanced Calpain activity, are disclosed. These compounds comprise optically pure .alpha.-ketoamides, and physiologically acceptable salts thereof, wherein the .alpha.-ketoamide contains an amino acid isomer which has an L-configuration about the chiral center which is structurally located in the .alpha. position to the ketone of the .alpha.-ketoamide, and wherein the amide functionality of the .alpha.-ketoamide portion of the compound's molecule is derived from an amine of an amino acid or an amine substituted with a sulfone functionality. The method of treating a human neurodegenerative pathology, having enhanced Calpain activity, with a Calpain inhibitor composition while reducing undesirable inhibition of other cysteine proteases and other side effects associated with the racemic calpain inhibitor composition includes administering an optically pure L-isomer of an .alpha.

Abstract: Methods, compounds, compositions and kits that relate to pretargeted delivery of diagnostic and therapeutic agents are disclosed. In particular, methods for radiometal labeling of biotin, as well as related compounds, are described. Articles of manufacture useful in pretargeting methods are also discussed.

Abstract: Peptide-copper complexes are disclosed which stimulate the growth of hair on warm-blooded animals. In one aspect of this invention, the peptide-copper complexes are dipeptides or tripeptides chelated to copper at a molar ratio ranging from about 1:1 to 3:1, with the second position of the peptide from the amino terminus being histidine, arginine or a derivative thereof. The peptide-copper complexes may be formulated for administration by, for example, topical application or injection. Any affliction associate with hair loss, including hair loss associated with both androgenetic and secondary alopecia, may be treated with the peptide-copper complexes of this invention.

Abstract: A pharmaceutical preparation for the therapy of immune deficiency conditions comprising an active principle--a peptide of the structure: H-L-Glu-L-Trp-OH and a pharmaceutically acceptable vehicle.