Abstract: There are provided compounds of formula I wherein k, m, n, p, R, R?, R?, R??, R3 and R4 are as defined in the application. Other embodiments are also disclosed.

Abstract: Provided herein are compositions and methods for the treatment of cancers. The compositions comprise at least one VEGF peptide mimic, HER-2 epitope, immunogenic VEGF peptides, and HER-2 immunogenic epitopes. The peptides and epitopes may be linear, cyclized, retro-inverso, or a combination of such forms. Also provided herein are antibodies raised to VEGF peptide mimics, HER-2 epitopes, immunogenic VEGF peptides, and HER-2 immunogenic epitopes.

Abstract: The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.

Abstract: A targeting lipid can have the formula (I) in which T4 is a targeting moiety. The targeting moiety can be chosen to favor the lipid being localized with a desired organ, tissue, cell, cell type or subtype, or organelle. The targeting moiety can include, for example, transferrin, anisamide, an RGD peptide, prostate specific membrane antigen (PSMA), fucose, an antibody, or an aptamer.

Abstract: A method has been developed for the formation of multivalent cyclic peptides. This procedure exploits on-resin peptide cyclization using a photoinitiated thiol-ene click reaction and subsequent clustering using thiol-yne photochemistry. Both reactions utilize the sulfhydrl group on natural cysteine amino acids to participate in the thiol-mediated reactions.

Abstract: The present invention concerns a method of detecting the antifungal cyclic hexapeptides Pneumocandin B0 and/or Pneumocandin C0 specific fragment is/are detected using MS in negative mode.

Abstract: The present invention relates to a method for isolating acyclohexapeptide and to a novel crystalline form of caspofungin diacetate thus obtained.

Abstract: The present invention relates to cyclosporin analogues having antiviral activity against HCV and useful in the treatment of HCV infections. More particularly, the invention relates to novel cyclosporin analogue compounds, compositions containing such compounds and methods for using the same, as well as processes for making such compounds.

Abstract: The invention provides methods for treating stroke and compositions for use in the same. The methods employ a chimeric peptide of an active peptide and an internalization peptide. The internalization peptide is a tat variant that promotes uptake of itself and a linked active peptide into a cell without substantial binding to N-type calcium channels. Use of the tat variant allows treating of stroke free of certain side effects associated with binding to N-type calcium channels. Tat variant peptides can also be linked to other active agent for use in treating other diseases.

Abstract: Cyclotetrapeptides of formula (I) or their pharmaceutically acceptable salts, cyclo[Arg-Asp-(beta-Lactam)] (I) wherein (beta-Lactam) is a biradical of the formula (II) wherein the terminal NH group of the (beta-Lactam) is attached to the ?-carbonyl group of the aspartic residue (Asp), and the terminal carbonyl group of the (beta-Lactam) is attached to the ?-amino group the arginine residue (Arg); processes for their preparation, and pharmaceutical compositions containing them, as well as their use in human and animal therapy.

Abstract: The invention relates to conjugates that bind to Her2/neu, methods of using conjugates that bind to Her2/neu and methods of treating undesirable or aberrant cell proliferation or hyperproliferative disorders, such as tumors, cancers, neoplasia and malignancies that express Her2/neu.

Abstract: Cyclic peptidomimetics that inhibit the interaction between MLL1 and WDR5 are disclosed. Methods of inhibiting MLL1 activity and methods of treating cancers also are disclosed.

Abstract: This invention discloses isolated short peptides comprising the amino acid sequence Cys-Glu-Phe-His (CEFH; SEQ ID NOS: 1 and 15) and analogs thereof as well as compositions comprising CEFH peptides and analogs thereof. The CEFH peptides disclosed herein are effective in mediating the denitration of 3-nitrotyrosines (3-NT) in cellular proteins thereby preventing tissue damage associated with excess nitric oxide (NO) and its reactive species. The CEFH peptides disclosed herein are useful in the treatment of ischemia/reperfusion (I/R) injury and other disorders.

Abstract: Improved methods of native chemical ligation are provided. The methods involve reacting a thioacid (e.g. a peptide thioacid) with an aziridinyl compound (e.g. an aziridinyl peptide) under mild conditions without the use of protecting groups, and without requiring that a cysteine residue be present in the ligation product. Initial coupling of the thioacid and the aziridinyl compound yields a ligation product which contains an aziridinyl ring. Subsequent opening of the aziridinyl ring (e.g. via a nucleophilic attack) produces a linearized and modified ligation product.

Abstract: The present invention, among others, relates to a compound having a structure according to formula (I) or a pharmaceutically acceptable salt thereof, wherein Xaa1 to Xaa4 are independently of each other, an optionally N-alkylated natural or unnatural amino acid, R is H or methyl, L is a linker moiety, Ar is a spacer comprising an aromatic moiety, and D comprises, preferably is i) a combination of an organic complexation agent and a detectable label; or ii) a detectable label, an organic complexation agent or an active substance, said active substance particularly being selected from cytotoxic agents, lipids, sugars, sugar conjugates, sugar derivatives, proteins and combinations thereof, with the proviso that -L-Ar-D does not comprise a 18F-benzoyl residue.

Abstract: Disclosed herein are methods of making cyclosporin A Form 2.

Abstract: A peptide consisting of 7-17 amino acids and including the adjacent hexamer TX1EX2X3E, where X1, X2 and X3 can be any natural or non natural amino acid, wherein the peptide does not exhibit TNF-receptor-binding activity and is cyclic, for the treatment or prevention of vascular complications in diabetes patients.

Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer.

Abstract: The invention relates to the use of the Peptide of the formula Cyclo-(Arg-Gly-Asp-DPhe-NMe-Val) and/or the pharmaceutically acceptable dervatives, solvates and/or salts thereof, for the manufacture of a medicament for the treatment of breast cancer and/or bone metastases in humans, wherein the medicament is optionally to be used in combination with one or more cancer cotherapeutic agents, preferably selected from a) hormone modulating agents, b) osteoclast activity modulating agents, c) cancer chemotherapeutic agents, and/or d) radiotherapy, alone, concurrently or not in the dosage regime of the present invention.

Abstract: There are provided compounds of formula I: wherein k, m, n, p, R, R?, R?, R??, R3, R4, R7 and R8 are as defined in the application. Other embodiments are also disclosed.

Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer.

Abstract: The present invention relates to the identification of new peptides and peptidomimetics which bind the CXCR4 receptor, capable of forming complexes with receptors for chemokines, in particular with CXCR4. The invention also relates to the use of these peptides for the treatment, prevention and diagnosis of diseases which involve chemokine receptors (i.e. neoplasias, metastases, HIV-1 virus infections), and also the mobilization of stem cells of hemopoietic precursors in the case of autologous transplants. Finally, the invention comprises pharmaceutical compositions and diagnostic kits comprising said peptides.

Abstract: Disclosed are peptidomimetic macrocycles comprising a helix, such as an alpha helix, and methods of using such macrocycles for the treatment of disease such as cancer. In other aspects, the peptidomimetic macrocycle comprises an a,a-disubstituted amino acid, or may comprise a crosslinker linking the a-positions of at least two amino acids or at least one of said two amino acids may be an a,a-disubstituted amino acid. Further included is the targeting of components of the Wnt signaling pathway such as the Tcf4-/3-catenin complex.

Abstract: A process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S, or NR8, where R8 is C1-6 alkyl, C6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at —XC(O)— occurs without racemization, is provided. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerization.

Abstract: The present invention relates to tricarbonyl technetium-99m or rhenium-188 labeled cyclic RGD derivatives, a preparation method thereof, and a pharmaceutical composition containing the derivative as an active ingredient for use in the diagnosis or treatment (radiotherapy) of angiogenesis-related diseases. The tricarbonyl technetium-99m or rhenium-188 labeled cyclic RGD derivatives of the present invention has a high subnanomolar affinity to integrin ?v?3 (also called as a vitronectin receptor) that is activated in an angiogenic action induced by a tumor, reflects a high tumor image of the tricatvonyl technetium-99m labeled cyclic RGD derivative after initial intake in an animal in which cancer cells are transplanted, and acts exclusively upon cancer cells having selectively activated integrin ?v?3 because of a substantially low intake into the liver and intestines, compared to existing known radioactive isotope labeled cyclic RGD derivatives.

Abstract: The invention relates to compounds that are analogs of a cyclic peptide, cyclo[EKTOVNOGN], AFPep, that has anti-estrotrophic activity. The analogs of the invention include peptides and peptidomimetics that inhibit estrogen receptor-dependent cell proliferation. The compounds of the invention are useful for treating cell proliferative disorders or physiological conditions characterized by undesirable or unwanted estrogen induced cell proliferation, including breast cancer.

Abstract: Compounds of formula (I), where: R0 is (C8-C11)-branched alkyl, CH3—(CH2)m—, CH3—O—(CH2CH2O)2CH2—, or phenyl-(CH2)x—; m=6-10; x=1-3; R1, R3, R4, R7, and R8 are independently selected from the formula GF-(CH2)n—; with n=1-4; and GF=—NH2 or —NH—C(?NH)—NH2; R2 is —CH(CH3)(OH), —CH(CH3)2, —CH2NH2 o —CH2OH; R5 and R6 are independently selected among H, —(C1-C4)— linear or branched alkyl, —(CH2)—R10, —CH2—CH2—S—CH3 and —CH—(CH3)—OH; R9 is CONH2, —CH(CH3)(OH) or CONHR11; R10 is phenyl, 3-indolyl, 4-imidazolyl, 4-hydroyiphenyl, ? o ?-naphtyl or 2-, 3- or 4-pyridyl; R11 is a specific peptide sequence; u is CH2 or S; v is NH o S; w is CH2 or CO; with the condition that when R9 is CONH2, then (a) R5 or R6 is —CH(CH3)(OH), or (b) R5 and R6 are H; or (c) the configuration of the C bound to R9 is S or (d) the configuration of the C bound to R5 is R; and with the condition that when R9 is —CH(CH3)OH, then R8 is GF(CH2)n where n is 3 and GF is —NH—C(?NH)—NH2, and R7 is GF(CH2)n where n is 2 and GF is NH2, have been found to

Abstract: The present invention includes methods for selective binding of inorganic materials and the compositions that made up of the selecting agent and the target materials. One form of the present invention is a method for selecting crystal-binding peptides with binding specificity including the steps of contacting one or more amino acid oligomers with one or more single-crystals of a semiconductor material so that the oligomers may bind to the crystal and eluting the bound amino acid oligomers from the single-crystals.

Abstract: A purification method of the compound represented by formula 1 is provided, which includes the following steps: (1) loading crude compound 1 on macroporous adsorbent resin, (2) washing the macroporous adsorbent resin with an aqueous solution, an organic solvent or a mixture solution of organic solvent and water, (3) eluting with an aqueous solution, an organic solvent or a mixture solution of organic solvent and water. The purified compound represented by formula 1 is obtained.

Abstract: The present invention relates generally to crystalline forms of cyclosporine A and particularly to a newly identified form of cyclosporine A. The invention further relates to methods for its preparation and to methods for treating certain ocular disorders.

Abstract: A compound of formula (I) is described, wherein Y represents a macrocycle, the ring of which has 9 to 36 atoms, and is functionalized by three amine or COOH functions; Rc represents a group of formula H—Xa—Xb—Xc—Xd—Xe—(Xf)i—, i represents 0 or 1, Xa is in particular lysine, arginine, or ornithine residues, Xb is in particular glycine, asparagine, L-proline or D-proline residues, Xc and Xd are in particular tyrosine, phenylalanine or 3-nitrotyrosine residues, Xe and Xf are in particular amino acid residues: NH2—(CH2)n—COOH, n ranging from 1 to 10, or NH2—(CH2—CH2—O)m—CH2CH2COOH, m ranging from 3 to 6, provided that at least one of the amino acid residues Xa, Xb, Xc and Xd is different from the corresponding amino acid in the sequence of the natural CD40 143Lys-Gly-Tyr-Tyr146 fragment(SEQ ID NO: 1).

Abstract: Methods for producing and obtaining natural products from microbial amplification chambers are described. This approach utilizes the concept of green chemistry to synthesize and extract the marine and terrestrial natural products. The method describes techniques to colonize and grow the selected bacteria and to continuously harvest the pharmaceutical agent from the broth without using any commercial solvents.

Abstract: According to the present invention, a novel polyazamacrocyclic compound which is used as a bifunctional chelating agent (BFC) can be synthesized selectively and in high yield. The novel polyazamacrocyclic compound synthesized by this method chelates with metals and thus can be conjugated with bioactive molecules such as peptides, and can be used in the diagnosis and treatment of medical conditions.

Abstract: The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic pentapeptide and hexapeptide analogs of endomorphin that have (i) a carboxy-terminal extension with an amidated hydrophilic amino acid and (ii) a substitution in amino acid position 2. These peptide analogs exhibit decreased tolerance relative to morphine, increased solubility compared to similar tetrapeptide analogs, while maintaining favorable or improved therapeutic ratios of analgesia to side effects.

Abstract: The present invention relates to cyclic cationic peptides and their use in the treatment of microbial infections.

Abstract: Antibodies and meditopes that bind to the antibodies are provided, as well as complexes, compositions and combinations containing the meditopes and antibodies, and methods of producing, using, testing, and screening the same, including therapeutic and diagnostic methods and uses.

Abstract: The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.

Abstract: Conjugates of porphyrin, chlorophyll and bacteriochlorophyll photosensitizers with RGD-containing peptides or RGD peptidomimetics are provided that are useful for photodynamic therapy (PDT), particularly vascular-targeted PDT (VTP), of tumors and nonneoplastic vascular diseases such as age-related macular degeneration, and for diagnosis of tumors by different techniques.

Abstract: The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.

Abstract: Embodiments of the present invention provide for novel peptides of use for detection and/or inhibition of anti-?1-adrenergic receptor antibodies. Certain embodiments concern uses of cyclic and/or linear peptides. In other embodiments, the present invention relates to novel peptides of use in diagnostic and/or pharmaceutical compositions. Some embodiments concern diagnosing and/or treating cardiac conditions. Cardiac conditions of the instant invention can concern infectious heart disease, non-infectious heart disease, ischemic heart disease, non-ischemic heart disease, inflammatory heart disease, myocarditis, cardiac dilatation, idiopathic cardiomyopathy, idiopathic dilated cardiomyopathy, immune-cardiomyopathy, heart failure, and any cardiac arrhythmia condition.

Abstract: ?-Hairpin peptidomimetics of the general formula Cyclo(-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-), and pharmaceutically acceptable salts thereof, with Xaa 1-Xaa 16 being amino acid residues of certain types which are defined in the description and the claims, have CXCR4 antagonizing properties and prolonged half-lives in vivo and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections eases of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid-and solution phase synthetic strategy.

Abstract: Novel template-fixed ?-hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are ?-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property to antagonize the receptor CCR10. They can be used as medicaments to treat or prevent diseases or conditions in the area of dermatological and cutaneous disorders, inflammation, allergic disorders, respiratory diseases, diseases of the gastro-intestinal tract, ophthalmic diseases, haematology and cancer. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

Abstract: The present invention relates to the field of polymer chemistry and more particularly to click-functionalized targeting compounds and methods for using the same.

Abstract: Compounds based around tetrapeptide, tripeptide and dipeptide moeties and corresponding peptiod moeties. Related methods and pharmaceutical compositions for use in treatment of cancer, inflammatory diseases, and other disorders.

Abstract: The present invention is concerned with a novel composition of matter—a cyclic peptide derived from computer modeling studies that modulates the structure and function of the HIV main envelope protein gp120. The compound is capable of binding to the CD4-binding region of gp120 (this defines it as a CD4 mimic), and can be used for the purposes of: (1) controlling and preventing HIV infections, (2) detecting, isolating and purifying gp120. Contrary to examples of prior art that involved CD4 mimics being either small molecules or macromolecules, the present invention is concerned with the class of “large small molecules” that may offer a satisfactory balance between the activity and drug-like properties. Modified variants of the prototype compound that can be reasonably considered its derivatives are also claimed.

Abstract: This invention relates to novel immunogens carrying conformationally discriminating epitopes (CDEs) and to immunization methods for producing antibodies that specifically recognize proteins with very closely related homologues. In particular, the invention relates to antibodies which are specific for either Fc?RIIb and Fc?RIIa.

Abstract: This invention relates to cyclosporin derivatives of general formula (I): wherein A, B, R1, R2 and X are as defined in the specification, and pharmaceutical compositions prepared from the same, for use in treatment of hepatitis C virus.

Abstract: A method of preparing purified cyclosporin H includes dissolving cyclosporin A in a first organic solvent and heating the first organic solvent in the presence of an acid catalyst; adding a base to the first organic solvent; recrystallizing cyclosporin H in a second solvent; and purifying the recrystallized cyclosporin H via chromatography to obtain purified cyclosporin H, while excluding recrystallizing the cyclosporin H in the presence of ether. In a further aspect, the method includes, after adding the base and before the recrystallizing, mixing the first organic solvent with a solvent more polar than the first organic solvent, separating the first organic solvent, and drying the first organic solvent. Cyclosporin H prepared as described herein was found to be biologically active, unlike that prepared using a previously-described method.

Abstract: The present invention is directed to modulators of eosinophilic and neutrophilic function and the use of such modulators for treatment of eosinophil-associated and neutrophil-associated diseases.

Abstract: Provided are a cross-bridged tetraaza macrocyclic compound of a novel structure that can be used, for example, as a contrast agent for diagnostic imaging or a radiopharmaceutical and a method for preparing the same. The disclosed tetraaza macrocyclic compound is able to form a stable metal complex at a lower temperature and allows easy conjugation with a bioactive substance or a chemically active substance, when compared to the existing cross-bridged tetraaza macrocyclic compounds.