Abstract: Novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies and have the general formula I: wherein R1, R2, R3, R4, R5 and R6 are as described herein.

Abstract: A method of radiostabilizing an oxime ligation or imine formation reaction using aniline is described.

Abstract: Provided is a method for preparing eptifibatide, wherein the method comprises: obtaining an eptifibatide refined peptide solution; and obtaining and freeze-drying an eptifibatide refined peptide concentrate after rotary evaporation of the eptifibatide refined peptide solution, wherein the concentration of the eptifibatide refined peptide concentrate is 15-30 mg/ml and the temperature of rotary evaporation is 251° C.-35° C. The preparation method of the eptifibatide refined peptide solution is as follows: coupling Cys with a resin to obtain a Cys-resin; obtaining a polypeptide having a sequence as represented by SEQ ID NO: 1 by gradually coupling the Cys-resin with Pro, Trp, Asp, Gly, Har and Mpa; and obtaining the eptifibatide refined peptide solution through oxidation, cleavage, purification and transfer to salt.

Abstract: The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, and identify a TFPI-binding compound.

Abstract: A compound having the formula: wherein X is S, SO or SO2; one of R1, R2, and R3 is O and the others of R1, R2 and R3 are independently, the same or different, CH2, or CR13 wherein, R13 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)mOR15, wherein R15 is an alkyl group or an aryl group and m is an integer in the range of 1 to 10, and one of R5, R6, and R7 is O and the others of R5, R6 and R7 are independently, the same or different, CH2, or CR14 wherein, R14 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)nOR16, wherein R16 is an alkyl group or an aryl group and n is an integer in the range of 1 to 10; R4 and R8 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group, a C1-C3 alkoxy group, an aryloxy group, or —(CH2)qOR17, wherein R17 is an alkyl group or an aryl group and q is an integer in the range of 1 to 10, provided that R4 is not a C1-C3 alkoxy g

Abstract: The present disclosure provides pyrimidine diol amides of Formula (I), and the pharmaceutically acceptable solvates and prodrugs thereof, wherein A1, X, A2, W1, W2, W3, R1, R2, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.

Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aliphatic amine group is conjugated to one or more polymeric carriers via dipeptide-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.

Abstract: A problem to be solved by the present invention is to provide a peptide compound for producing a drug delivery carrier capable of releasing a target substance in a weakly acidic pH environment. The present invention provides a peptide compound comprising a hydrophilic amino acid block and a hydrophobic amino acid block; [1] the peptide compound containing 24 to 36 amino acids in total; [2] the hydrophilic amino acid block containing 4 to 10 amino acids in total and having an average hydropathy index of ?3.0 to ?1.0; and [3] the hydrophobic amino acid block containing 20 to 32 amino acids in total, containing one or more His residues, and having an average hydropathy index of 1.0 to 2.5.

Abstract: The present invention relates to methods for treating and/or preventing podocytes related disorders and/or nephrotic syndrome comprising the administration of an effective amount of a certain DPP-4 inhibitor, as well as to the use of a certain DPP-4 inhibitor for treating and/or preventing a metabolic disease in a patient with or at risk of podocytes related disorders and/or nephrotic syndrome.

Abstract: The invention relates to peptide dimer compounds and peptide monomer compounds that potently inhibit binding of ?4?7 to the mucosal addressin cell adhesion molecule (MAdCAM) in vivo, possess high selectivity against ?4?1 binding, and have high stability under gastrointestinal conditions.

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 provides a peptide-phospholipid conjugate of Formula 1: wherein: X is selected from the group consisting of —CR1R2—, —R3—, —O—, —S—, and S+(R3)—; Y is selected from the group consisting of a bond, alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, amino, ether, cycloamino, cycloether, aryl heteroaryl, arylalkyl, heteroarylalkyl, hydroxyaryl, arylether, cycloalkyl, heterocycloalkyl, hydroxycycloalkyl, halocycloalkyl, and aminocycloalkyl; Z is a peptide comprising 1 to 50 amino acids; R1 and R2 each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, amino, ether, cycloamino, cycloether, aryl, heteroaryl, arylalkyl, heteroarylalkyl, hydroxyaryl, arylether, cycloalkyl, heterocycloalkyl, hydroxycycloalkyl, halocycloalkyl, and aminocycloalkyl; and R3 is selected from the group consisting of alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, amino, ether, cycloamino, cycloether, ary

Abstract: Provided are compounds of Formula: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.

Abstract: The embodiments provide Compound KC-8, N-1-[3-(oxycodone-6-enol-carbonyl-methyl-amino)-2,2-dimethyl-propylamine]-arginine-glycine-malonic acid, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug, Compound KC-8, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

Abstract: The present invention relates to inhibitors of protein-protein interactions (PPI). Specifically, the present invention relates to a structural informatics approach to designing peptidomimetic macrocycles containing an amino acid “warhead” for ligand-directed covalent modification of cysteine and lysine-containing proteins for the treatment of diseases such as cancer. Further included is the targeting of components of the BCL2 signaling pathway, specifically BCL2-A1 and MCL-1.

Abstract: The invention relates to a method or process for solution phase chemical manufacture of depsipeptides of the formula I, wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.

Abstract: The present invention relates to pharmaceutically and/or diagnostically active compounds, in particular peptide analogs (peptidomimetics), which can be reversibly controlled between an active and an inactive state by irradiation with light of different wavelengths. The present invention further relates to an intermediate compound usable in the manufacture of such pharmaceutically and/or diagnostically active compounds, as well as a manufacturing method thereof.

Abstract: This invention relates to an isolated compound of Formula (1) or derivatives or pharmaceutically acceptable salts thereof. The invention also includes all isomeric and tautomeric forms of the compound of Formula (1) or the derivatives thereof. The present invention further relates to processes for the production of the compound of Formula (1) by fermentation of the fungal strain of Actinomycetes (PM0895172/MTCC 684), pharmaceutical compositions comprising the compound of Formula (1) as the active ingredient; and use of the compounds or composition containing them in the treatment of cancer.

Abstract: Conjugates of an immune response modifier, a linker, and an antigen are disclosed. The linker is represented by formula (I): wherein A is CH or N, p is in a range from 1 to 50, R? is a bond or -alkylene-O—, R? is alkylene that is optionally interrupted or terminated with one or more amide or ether groups, and E is an amine- or thiol-reactive group. Pharmaceutical compositions containing the compound or the conjugate, methods of making a conjugate, and methods of use of the compounds or conjugates as immunomodulators for inducing cytokine biosynthesis in an animal and for vaccinating an animal are also disclosed. An antigen modified by the linker is also disclosed.

Abstract: The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.