Abstract: Analogues of cyclosporin-A are disclosed comprising modifications of the substituents as the positions of amino acids 1 and 3, according to the following Formula. The disclosed compounds include compounds having affinity for cyclophilin, including cyclophilin-A, and reduced immunosuppressivity in comparison with cyclosporin-A and analogs thereof modified solely at position 1.

Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, R5, and A-B are defined herein, which are non-immunosuppresive, cyclophilin-binding, mPTP blockers and are therefore useful for the prevention or treatment of diseases or disorders such as HCV infection, stroke, multiple sclerosis, HBV infection, HPV infection, asthma, cancer, muscular dystrophy, sepsis, ischemia/reperfusion injury, and heart failure.

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: The present invention comprises cyclic peptides bearing antitumor and antiangiogenic properties, as well as their corresponding pharmaceutically-suitable salts and also pharmaceutical compositions containing it. These cyclic peptides are used to prepare medicines for human and/or veterinary therapeutics, and additionally in diagnosis. These compounds can be used to detect, monitor and/or control a range of cellular proliferation-related disorders, such as oncological diseases and undesired angiogenesis. Moreover, they can be included as part of controlled release systems, and used more precisely in the field of nanobiotechnology, either because of their self-assembly capacity or as part of other systems.

Abstract: The current invention relates to the use of a peptide comprising an amino acid sequence in the preparation of a medicament for the regeneration of tissue, preferably for the treatment of a wound. Further the invention relates to compositions comprising such peptides, and use of said peptides in both medical and nonmedical (cosmetic) applications.

Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 4 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to agonize or to antagonize GPCR receptors such as CXCR3, urotensin and CCR10. They can be used as medicaments to treat or prevent diseases such as cardiovascular disorders, dermatological disorders, endocrine system and hormone disorders, metabolic diseases, inflammatory diseases, neurological diseases, respiratory diseases, haematological diseases and cancer. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

Abstract: A compound having formula (I) or formula (II): for use in anticancer or anti-obesity.

Abstract: Novel peptoids are disclosed that have a formula represented by the following formulae Ia and Ib: wherein X, Y, R, and n are as described herein. The peptoids demonstrate catalytic activity and are useful in substrate-selective catalytic transformations, including asymmetric catalytic transformations.

Abstract: Provided herein are compounds useful for diagnostic imaging and/or therapeutic purposes. Each compound comprises a ligand for the chemokine receptor CXCR4, which has a binding affinity for the CXCR4 receptor, measured as IC50 in the presence of 125I-CPCR4, of 250 nM or lower. The ligand is a cyclic oligopeptide moiety having a motif B-Arg or B-(Me)Arg within the cyclic moiety, wherein B is a basic amino acid, a derivative thereof, or phenylalanine, provided that the motif is B-Arg when B is a N?-methyl derivative of a basic amino acid, and provided that the cyclic oligopeptide moiety has a sequence other than cyclo[D-Tyr-Arg-Arg-NaI-Gly] or cyclo[D-Tyr-Orn-Arg-NaI-Gly].

Abstract: The present invention relates to a method for processing microbiologically produced, non-polar, cyclic oligopeptides comprising the step of a) extracting the entire fermentation broth incident to the microbiological production process using a liquid extractant that contains ether and is immiscible with water, wherein the amount of extractant is sufficient to form a two-phase system together with the total fermentation broth, and novel solvates of cyclosporin A and methyl-t-butyl ether.

Abstract: The present invention is related to new peptide antagonists of ?v?3 receptor, designed on the basis of the crystal structure of integrin ?v?3 in complex with c(RGDf[NMe]V) and the NMR structure of echistatin. These peptides are potent and selective antagonists of the ?v?3 receptor and can be used as novel anticancer drugs and/or new class of diagnostic non-invasive tracers as suitable tools for ?v?3-targeted therapy and imaging.

Abstract: The present invention relates to crystalline and crystal-like forms of lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention relates to methods of purifying lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention also relates to pharmaceutical compositions comprising the purified form of the lipopeptide and methods of using these compositions.

Abstract: The present invention provides soluble single wall nanotube (SWNT) constructs functionalized with a plurality of a targeting moiety and a plurality of one or more payload molecules attached thereto. The targeting moiety and the payload molecules may be attached to the soluble SWNT via a DNA or other oligomer platform attached to the SWNT. These soluble SWNT constructs may comprise a radionuclide or contrast agent and as such are effective as diagnostic and therapeutic agents. Methods provided herein are to diagnosing or locating a cancer, treating a cancer, eliciting an immune response against a cancer or delivering an anticancer drug in situ via an enzymatic nanofactory using the soluble SWNT constructs.

Abstract: The instant invention relates to novel solid materials of {[(2S,5R,8S,11S)-5-benzyl-11-(3-guanidino-propyl)-8-isopropyl-7-methyl-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaaza-cyclopentadec-2-yl]-acetic acid}, methods for producing them, and the use of said solid materials in pharmaceuticals.

Abstract: Conjugates of a polymer having attached thereto an angiogenesis targeting moiety and a therapeutically active agent such as an anti-cancer agent or anti-angiogenesis agent, and processes of preparing same are disclosed. Pharmaceutical compositions containing these conjugates and uses thereof in the treatment of angiogenesis-related medical conditions such as cancer and cancer metastases are also disclosed.

Abstract: There is provided a novel process for preparing polyamides (in particular cyclic and hairpin polyamides) comprising the step of coupling an amine with a Boc-protected amino acid monomer in the presence of diphosgene and/or triphosgene. Such a process may be performed on a solid or solution phase.

Abstract: Described is a process for preparing platinum-carbene complexes.

Abstract: Methods and kits for binding and releasing biological targets, comprising, a binder having an environmentally reactive molecular switch that can switch between a high affinity state, to bind the target, to a low affinity state, to release the target. In one embodiment, the binder is a pre-existing chemical sequence, composition, or structural configuration but unknown or unspecified and still viable as a binder for attaching a molecular switch.

Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, comprises the structure: [(P1-S1j)p-L-(S2q-P2)r]t wherein: P1 and P2, which may be the same or different, are cyclic oligopeptide moieties, at least one of P1 and P2 having the motif B-Arg or B-(Me)Arg within the cyclic moiety, wherein B is a basic amino acid, a derivative thereof, or phenylalanine or a derivative thereof; S1 and S2 are spacer groups, which may be the same or different; L is a linker moiety containing at least two functional groups for attachment of the cyclic oligopeptides or spacer groups; n and q are independently 0 or 1; p and r are independently integers of 1 or more; and t is an integer of 1 or more, provided that, when t, p or r is greater than 1, the cyclic oligopeptide moiety, spacer group and/or the value of j or q may be the same or different between the multiple (P1-S1j) moieties or multiple (S2q-P2) moieties.

Abstract: The present invention relates to the field of molecular imaging, i.e. nuclear and fluorescent imaging using metal ion radionuclides in combination with chelates highly functionalized with peptidic, nonpeptidic or protein ligands or additional signalling moieties.

Abstract: Cyclic CRF antagonist peptides having improved properties of “drugability”. The peptides are 33 residues in length with a lactam bond between the residues in position 22 and 25; however, they may be N-terminally shortened by up to 3 residues.

Abstract: The disclosure concerns the use of cyclophilin inhibitors in the treatment of chronic Hepatitis C virus infection.

Abstract: The present invention features crystalline forms of Compound I. In one embodiment, a crystalline form of Compound I has characteristic peaks in the PXRD pattern at values of two theta (° 2?) of 10.7, 11.6, 12.7, 13.0, 13.2, 13.7, 14.5, 18.7, 19.0, and 19.9 after equilibration at 43% relative humidity.

Abstract: The invention concerns the use of cyclophilin inhibitors in the treatment of Hepatitis B and Hepatitis D virus infections.

Abstract: The present invention relates to compounds of the Formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, X1, X2, X3 and X4 have the meanings indicated in the claims, and which are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb), and are suitable, for example, for the therapy and prophylaxis of athero-thrombotic diseases. The invention furthermore relates to processes for the preparation of compounds of the Formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

Abstract: Chemically reactive dyes that are intramolecularly crosslinked with a water-soluble bridge, their bioconjugates and their uses are described. Reactive fluorescent dyes that have a water-soluble bridge are superior to those of conjugates of spectrally non-crosslinked dyes or the dyes that are crosslinked with a hydrophobic bridge. The invention includes reactive fluorescent dyes, their biological conjugates and uses.

Abstract: Embodiments of the present disclosure provide for RGD mimetic ?-AApeptide compounds, ?-AApeptide compounds capable of binding an RGD binding site on integrin ?v?3, linear ?-AApeptide compounds, cyclic ?-AApeptide compounds and multimeric RGD mimetic ?-AApeptide compounds, methods of making each, and methods of using each, and the like. In embodiments, the RGD mimetic ?-AApeptide compounds can be used in imaging, diagnostics, and treatment of angiogenesis related conditions.

Abstract: The present invention relates to a compound of the formula (I), (II), (III), (IV), (V), or (VI) or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing a viral infection using the same.

Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, comprises the structure: [(P1-S1j)p-L-(S2q-P2)r]t wherein: P1 and P2, which may be the same or different, are cyclic oligopeptide moieties, at least one of P1 and P2 having the motif B-Arg or B-(Me) Arg within the cyclic moiety, wherein B is a basic amino acid, a derivative thereof, or phenylalanine or a derivative thereof; S1 and S2 are spacer groups, which may be the same or different; L is a linker moiety containing at least two functional groups for attachment of the cyclic oligopeptides or spacer groups; n and q are independently 0 or 1; p and r are independently integers of 1 or more; and t is an integer of 1 or more, provided that, when t, p or r is greater than 1, the cyclic oligopeptide moiety, spacer group and/or the value of j or q may be the same or different between the multiple (P1-S1j) moieties or multiple (S2q-P2) moieties.

Abstract: A solid phase method for synthesizing a peptide containing three or more amino acid residues utilizing both Boc and Fmoc protected amino acids and a chloromethylated polystyrene resin.

Abstract: The present invention relates to a new cyclic peptide compound or a salt thereof, which has anti-hepatitis C virus activities based on inhibitory activity against the RNA replication of hepatitis C virus replicon, a process for preparation thereof, a pharmaceutical composition comprising the same, and a method for prophylactic and/or therapeutic treatment of hepatitis C in a human being or an animal.

Abstract: The present invention relates to novel cyclosporin analogs, processes for preparing them, pharmaceutical compositions containing them, and methods for using these analogs and the compositions containing them for the treatment of medical conditions, including but not limited to ocular conditions such as dry eye.

Abstract: The present invention relates to a triazanonane derivative indicated by the chemical formula 1 below, or a pharmaceutically acceptable salt thereof, and a method for preparing same, and the triazanonane derivative according to the present invention forms a complex with a metal-fluoride and displays an effect of increasing the labeling efficiency up to 78-90% when labeling F-18, thus enabling use in various radioactive medicine labeling (In the chemical formula 1, R1, R2, A. E. X, n and m are as defined in the present description.

Abstract: The instant invention relates to novel solid materials of {[(2S,5R,8S,11S)-5-Benzyl-11-(3-guanidino-propyl)-8-isopropyl-7-methyl-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaaza-cyclopentadec-2-yl]-acetic acid}, methods for producing them, and the use of said solid materials in pharmaceuticals.

Abstract: The present invention relates to a compound of the formula (I): or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing a viral infection using the same.

Abstract: The present invention relates to novel peptides and to topical and food compositions comprising them. The novel peptides have applications in skin lightening and immunomodulation when applied topically and to immunomodulation and modulation of body mass when consumed in food compositions.

Abstract: The current invention relates to the use of a peptide comprising an amino acid sequence in the preparation of a medicament for the regeneration of tissue, preferably for the treatment of a wound. Further the invention relates to compositions comprising such peptides, and use of said peptides in both medical and nonmedical (cosmetic) applications.

Abstract: The present invention describes immunosuppressant pharmaceutical formulations particularly formulations of mycophenolate salts with pulsatile release behaviour.

Abstract: Peptides useful in determining the presence of autoantibodies in patients suffering from rheumatoid arthritis are disclosed.

Abstract: The present invention provides peptides and peptide conjugates for treating inflammatory bowel diseases, including ulcerative colitis and Crohn's disease. The peptides are derived from annexin-1, can be acetylated or conjugated to fatty acids, may be linear or cyclic, and may comprise D amino acids. Pharmaceutical compositions and methods of use are also disclosed.

Abstract: The invention relates to tumour therapy. In one aspect, the present invention relates to conjugates of an amatoxin and a target-binding moiety, e.g. an antibody, connected by a linker comprising a urea moiety, which are useful in the treatment of cancer. In a further aspect the invention relates to pharmaceutical compositions comprising such conjugates.

Abstract: The present invention relates to the field of radiopharmaceuticals for in vivo imaging, in particular to a method of labelling a biological targeting molecule with a radioisotope. The method of the invention is particularly suitable for use with an automated synthesizer apparatus. Also provided are precursors in sterile form, as well as cassettes comprising such precursors useful in the method.

Abstract: The invention relates to novel cyclodecapeptide compounds having formula (I) for use as drugs and, more specifically, for use in the diagnosis, prevention and/or treatment of neurodegenerative diseases, such as Wilson's disease and Alzheimer's disease, and for use in the diagnosis, prevention and/or treatment of poisoning with metal ions, such as copper and mercury ions. The invention also relates to pharmaceutical compositions comprising at least one compound having formula (I) as an active principle.

Abstract: The invention concerns the use of cyclophilin inhibitors in the treatment of Hepatitis C virus infection.

Abstract: The present application is directed to rapid and efficient synthesis of radiometal-labeled probes, pharmaceutical compositions comprising radiometal-labeled probes, and methods of using the radiometal-labeled probes. Such radiometal-labeled probes can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT), and therapy studies.

Abstract: Disclosed is a preparation method for caspofungin, comprising the steps: (a) a compound as represented in Formula 2 and a strong leaving group 5 are mixed to obtain a compound as represented in Formula 3; (b) the compound as represented in Formula 3 and ethylenediamine are mixed to obtain a compound as represented in Formula 4; and, (c) the compound as represented in Formula 4 is mixed with a hydroxyl protection agent, and then a borane complex is mixed in to obtain a compound as represented in Formula 1.

Abstract: The invention concerns the use of cyclophilin inhibitors in the treatment of Hepatitis C virus genotype 2 or 3 infection.

Abstract: In one aspect, the present invention provides isolated novel peptides that can be used to modulate innate immunity in a subject and/or for the treatment of an immune-related disorder, including treating and preventing infection by modulating innate immunity. Also provided are an agent reactive with the peptide, a pharmaceutical composition that includes the peptide, an isolated nucleic acid molecule encoding the peptide, a recombinant nucleic acid construct that includes the nucleic acid molecule, at least one host cell comprising the recombinant nucleic acid construct, and a method of producing the peptide using the host cell. The present invention further provides a method for treating and/or preventing infection in a subject by administering the peptide of the invention to the subject, thereby modulating innate immunity in the subject. Additionally, the present invention provides a method for predicting whether a subject would be responsive to treatment with a peptide of the invention.

Abstract: A microreactor for preparing a radiolabeled complex or a biomolecule conjugate comprises a microchannel for fluid flow, where the microchannel comprises a mixing portion comprising one or more passive mixing elements, and a reservoir for incubating a mixed fluid. The reservoir is in fluid communication with the microchannel and is disposed downstream of the mixing portion. A method of preparing a radiolabeled complex includes flowing a radiometal solution comprising a metallic radionuclide through a downstream mixing portion of a microchannel, where the downstream mixing portion includes one or more passive mixing elements, and flowing a ligand solution comprising a bifunctional chelator through the downstream mixing portion. The ligand solution and the radiometal solution are passively mixed while in the downstream mixing portion to initiate a chelation reaction between the metallic radionuclide and the bifunctional chelator. The chelation reaction is completed to form a radiolabeled complex.

Abstract: Novel template-fixed ?-hairpin peptidomimetics of the general formula (I), wherein the single elements T or P are ?-amino acid residues connected from the carbonyl (C?O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these ?-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilisation of stem cells.