Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: The present invention provides a new kind of vinca alkaloid derivatives, new applications thereof and preparation methods therefor. The vinca alkaloid derivatives comprise hydrazinolyzed vinca alkaloids and vinca alkaloid dipeptide derivative. The hydrazinolyzed vinca alkaloids are the compounds obtained from the reaction of vinca alkaloids or salts thereof with hydrazinolyzed hydrate; and the vinca alkaloid dipeptide derivatives are the compounds obtained from the condensation of hydrazinolyzed vinca alkaloids with N-benzyloxycarbonylglycyl proline. The present invention provides the uses of the vinca alkaloids derivatives or the pharmaceutical compositions thereof in anti-tumor, preventing or treating diabetic retinopathy, rheumatoid arthritis and serving as angiogenesis inhibitors or vascular disrupting agents.

Abstract: To provide a compound which can demonstrate flame retardancy equal to or higher than V-1 of the UL94 standard by adding a flame retardant to resin containing aromatic polyester and styrene polymer. To provide a compound represented by General Formula (1) of Claim 1. In General Formula (1), R1 to R3 are alkyl groups having 1 to 4 carbon atoms and R1 to R3 may be the same or different from each other.

Abstract: Calcium phosphate particles are described comprising a surface treatment wherein the surface treatment comprises at least one sugar alcohol. Also described are various oral care compositions comprising surface treated calcium phosphate particles and methods of surface treating calcium phosphate particles.

Abstract: Generally, the present invention relates to improvements in metal utilization in supported, metal-containing catalysts. For example, the present invention relates to methods for directing and/or controlling metal deposition onto surfaces of porous substrates. The present invention also relates to methods for preparing catalysts in which a first metal is deposited onto a support (e.g., a porous carbon support) to provide one or more regions of a first metal at the surface of the support, and a second metal is deposited at the surface of the one or more regions of the first metal. Generally, the electropositivity of the first metal (e.g., copper or iron) is greater than the electropositivity of the second metal (e.g., a noble metal such as platinum) and the second metal is deposited at the surface of the one or more regions of the first metal by displacement of the first metal. The present invention further relates to treated substrates, catalyst precursor structures and catalysts prepared by these methods.

Abstract: A compound having a structure of:

Abstract: The present teachings relate to compounds and compositions for treatment of cancers. In some embodiments, the composition comprises a platinum (IV) complex having at least one reacting group for reacting with a functional group on a protein, engineered protein, antibody, antibody fragment, peptide, agonist, antagonist, aptamer or ligand which may be capable of recognizing a selected target cell population, and/or derivatives/analogs/mimics thereof.

Abstract: Anthracyclin compounds of the general structure: are disclosed. In these compounds R1 is methyl, acetyl or hydroxyacetyl; R2—R5 and R10—R13 are independently H or methyl; R6 R7 and R8 are independently H, OH or OCH3; and n is zero or one. The compounds are useful for treating cancer.

Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, and the uses of the compounds and compositions as modulators of histone methyltransferases, and for treating diseases influenced by modulation of histone methyltransferase activity.

Abstract: The invention relates to compositions, methods, kits, and assays related to the use and/or exploitation of isomers of cGAMP as well as the structure of the enzyme cGAS.

Abstract: A compound represented by the general formula (III) which serves as an intermediate of an oligonucleotide analog having stable and excellent antisense or antigene activity or having excellent activity as a detection reagent (probe) for a specific gene or as a primer for the initiation of amplification of a specific gene can be produced at high yields regardless of the type of nucleobase by a method comprising reacting a compound represented by the general formula (II) or a salt thereof with a trimethylsilylated compound obtained from a compound represented by the general formula (IVb), wherein X, Y, Z, A, R, and B are as defined in claim 1.

Abstract: The present invention provides novel Raman tags for exploring membrane interactions in cells. The tags comprise a phenyl diyne probe where in the dyine is capped with the phenyl group. Methods for using the tags are also provided.

Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, status epilepticus.

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

Abstract: The present invention provides a more productive method for culturing and a more productive method for harvesting culture product in cell culture wherein the cell produces the culture product.

Abstract: The present invention concerns a compound of following formula (I): where: —R1 is H or OH, —R2 is a (C1-C6)alkyl, COOH, COO—((C1-C6)alkyl) or thiazolyl group, —R3 is H or a (C1-C6)alkyl group, and —R4 is: ? a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR5R6, ? —(CH2CH2X1)(CH2CH2X2)a2(CH2CH2X3)a3(CH2CH2X4)a4(CH2CH2X5)a5R7, ? an aryl-(C1-C8)alkyl group substituted by one or more groups chosen from among OH and NR9R10 groups, or ? a heterocycle-(C1-C8)alkyl group optionally substituted by one or more groups chosen from among (C1-C6)alkyl, OH and NR12R13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.

Abstract: The present invention concerns a compound of following formula (I) where: —R1 is H or OH, —R2 is a (C1-C6)alkyl, COOH, COO—((C1-C6)alkyl) or thiazolyl group, —R3 is H or a (C1-C6)alkyl group, and —R4 is an aryl-(C1-C8)alkyl group substituted by one or more groups chosen from among OH and NR9R10 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.

Abstract: The invention provides a molecule that modulates an activity of a Src family kinase for use in preventing or treating a metastatic cancer a subject. Preferably, the molecule comprises or consists of the structure: Bj-[(Pro)n-Xr-His-Pro-His-Ala-Arg-Ile-Lys]m-Rp, or Bj-[lys-ile-arg-ala-his-pro-his-xr-(pro)n]m-Rp, or a derivative or fragment thereof, wherein B is a first chemical moiety, j is 0 or 1, n is an integer from 1-10, X is any amino acid, r is an integer from 0 to 2, m is an integer from 1 to 3, R is a second chemical moiety, p is 0 or 1, and [lys-ile-arg-ala-his-pro-his-xr-(pro)n] is the retro-inverso peptide of [(Pro)n-Xr-His-Pro-His-Ala-Arg-Ile-Lys].

Abstract: This invention relates, e.g., to an inhibitory peptide or CPP inhibitor which specifically binds to p53 having an aberrant conformation (e.g., is aggregated or misfolded) and inhibits p53 amyloidogenic aggregation or restores proper folding of the misfolded protein. Methods of using the inhibitory peptide or CPP inhibitor (e.g. to treat subjects having tumors that comprise aggregated p53) are described.

Abstract: An anti-tumor polypeptide, having an amino acid sequence represented by FPGSDRF (SEQ ID NO. 15), X-FPGSDRF, FPGSDRF-Z, or X-FPGSDRF-Z, in which the various capital letters denote amino acids: F: phenylalanine; P: proline; G: glycine; S: serine; D: aspartic acid; R: arginine; S is a phosphorylated serine residue, X and Z are an amino acid residue or an amino acid sequence, respectively, X is one selected from the group consisting of F, (R)9, (R)9-F, 6-aminocaproic acid, 6-aminocaproic acid-F, 6-aminocaproic acid-(R)9, and 6-aminocaproic acid-(R)9-F, Z is one selected from the group consisting of A, (G)n-RGD, and A-(G)n-RGD; and n is an integer greater than or equal to 0.

Abstract: PROBLEM To provide a therapeutic agent for cardiac tamponade to suppress occurrence of complications accompanying cardiac tamponade by preventing and improving deterioration of macro- and micro-circulation caused by cardiac tamponade and also by suppressing local and systemic inflammation accompanying such deterioration of circulation. SOLUTION A pharmaceutical which contains a peptide of the present invention or a pharmaceutically acceptable salt of such peptide as an active ingredient is useful as a therapeutic agent for cardiac tamponade (pericardial tamponade) caused by myocardial infarction, malignant tumor metastasis, collagen disease, or the like.

Abstract: The present invention discloses new stable pentadecapeptide salts of formula (I): (I) SEQ?ID?NO?1 Gly?Glu?Pro?Pro?Pro?Gly?Lys?Pro?Ala?Asp?Asp?Ala 1???????????????5???????????????????10??????????? Gly?Leu?Val?· n?BAA ????????15 wherein n means 1, 2 or 3, and BAA means basic amino acid, a process for the preparation thereof, a process for the use thereof for the manufacture of pharmaceutical formulations in liquid and solid form and a use thereof for prevention, protection in treatment of diseases and disease conditions and for the preparation of formulations for use as food supplements.

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

Abstract: This invention is generally related to small proteins, such as miniature proteins, including avian pancreatic polypeptide (aPP), modified so that the small proteins reach the cytosol. In some embodiments, the modified protein molecules deliver an associated cargo molecule to the cytosol. Other embodiments of the invention relate to modified protein fusion molecules that reach the cytosol.

Abstract: Disclosed herein is a recombinant viral construct and its uses thereof. The recombinant viral construct is capable of simultaneously expressing three exogenous proteins, including a classical swine fever virus (CSFV) antigen, a porcine circovirus type 2 (PCV2) antigen, and an immunomodulatory protein. The recombinant viral construct is hence useful as a bio-tool for simultaneously producing multiple antigens of a bi-subunit vaccine.

Abstract: The invention relates to compositions of vault complexes containing recombinant membrane lytic proteins, such as an adenovirus protein VI lytic domain, and methods of using the vault complexes to facilitate delivery and entry of a biomolecule into a cell or subject.

Abstract: The present invention provides cytotoxic proteins comprising immunoglobulin-type binding regions for mediating cell-type specific targeting and Shiga toxin effector regions derived from A Subunits of members of the Shiga toxin family for effectuating cytotoxicity. The cytotoxic proteins have uses for selective killing of specific cell types and as therapeutics for the treatment of a variety of diseases, including cancers, immune disorders, and microbial infections.

Abstract: Provided are compositions and methods for making a variety of products. The methods involve mixing sucker ring teeth (SRT) protein and a plasticizer or a solvent to obtain a mixture of the SRT protein and the plasticizer. When the SRT is mixed with a plasticizer it is heated to between 32° C. and 195° C. to obtain an SRT protein melt. The melt is used to form a wide variety of products. When the SRT is mixed with a solvent, such as an organic solvent or an aqueous solvent, a solution of the SRT protein is formed, and is subsequently used to forming a product from the solution, wherein the product contains SRT protein.

Abstract: The present invention for the first time discloses a novel small molecular weight enamel matrix polypeptide which is at least 80%, such as 90% identical to the amino acid sequence as shown in SEQ ID NO: 1 (MPLPPHPGHP GYINFSYEVL TPLKWYQNMI RHPYTSYGYE PMGGWLHHQI IPWSQQTPQ SHA) (TRAP63), a homologue, analogue, or a pharmaceutically acceptable salt thereof. The present invention further discloses a pharmaceutical composition consisting of an enamel matrix polypeptide which is at least 80%, such as 90% identical to the amino acid sequence as shown in SEQ ID NO: 1, a homologue, analogue, or a pharmaceutically acceptable salt thereof, and a suitable pharmaceutical carrier, which further can consist of one or more enamel matrix polypeptides selected from the group of enamel matrix polypeptides which correspond to: a. SEQ ID NO: 2, b. SEQ ID NO: 3 and c. SEQ ID NO: 4.

Abstract: The present invention relates to a method for preparing a GM1 gangliosidosis human cell model based on induced pluripotent stem cells (iPSCs) and iPSCs originated neural progenitor cells, and a use of the GM1 model above for the development of a GM1 gangliosidosis treating agent. The iPSCs originated from GM1 patient fibroblasts can be differentiated into neural progenitor cells (NPCs) and neurosphere cells that can emulate the characteristics shown in GM1 patient, so that the said cells can be efficiently used for the investigation of intracellular GM1 symptoms such as the GM1 gangliosidosis and lysosome accumulation and the gene expression pattern change. So, the GM1 cell model of the present invention can be efficiently used for the study of GM1 development mechanism and the study for the development of a therapeutic agent for the disease.

Abstract: The present disclosure is directed to individual A? peptide immunogen constructs, peptide compositions comprising these A? peptide immunogen constructs and mixtures thereof, pharmaceutical compositions including vaccine formulations comprising these A? peptide immunogen constructs, with the individual A? peptide immunogen constructs having the N-terminus of the A? peptide as the B cell (B) epitopes linked through spacer residue(s) to heterologous T helper cell (Th) epitopes derived from pathogen proteins that act together to stimulate the generation of highly specific antibodies directed against the N-terminus of the A? peptide offering protective immune responses to patients at risk for, or with, Alzheimer's Disease.

Abstract: The P21 protein is used as a medicament in the treatment of cancer, conjugate comprises a first region comprising the P21 protein, or a homologue functional fragment thereof; and a second region comprising a translocation factor.

Abstract: Interleukin-10 muteins and other interleukin-10-related molecules are described, as well as methods of identifying interleukin-10 muteins and other interleukin-10-related molecules. Also described herein are modifications of the foregoing, which modifications may enhance a property (e.g., half-life) of the muteins or other molecules compared to human interleukin-10. Particular interleukin-10 muteins and related molecules have comparable immunogenicity to human interleukin-10 and/or bioactivity at least comparable to human interleukin-10. Pharmaceutical compositions and methods of use are also described herein.

Abstract: The present invention relates to a pharmaceutical composition for treating a cancer or an infection in a subject by administrating an amount of an IL-15 derivative conjugate so as to induce a proliferation of natural killer cells (NK cells) which is the same or higher than the one obtained with high dose of interleukin-2 (HDIL-2); eventually associated with a pharmaceutically acceptable carrier.

Abstract: The present invention provides compositions and methods for treating insulin-dependent diabetes mellitus in a subject comprising administration of a self-vector encoding and expressing human proinsulin.

Abstract: A humanised agonistic antibody which binds human PD-1 comprising a heavy chain and a light chain wherein the variable domain of the heavy chain comprises the sequence given in SEQ ID NO:1 for CDR-H1, the sequence given in SEQ ID NO:2 for CDR-H2 and the sequence given in SEQ ID NO:3 for CDR-H3 and the variable domain of the light chain comprises the sequence given in SEQ ID NO:4 for CDR-L1, the sequence given in SEQ ID NO:5 for CDR-L2 and the sequence given in SEQ ID NO:7 for CDR-L3. The invention also extends to therapeutic uses of the antibody molecules, compositions and methods for producing said antibody molecules.

Abstract: The present invention relates to oligopeptide-free cell culture media comprising at least 0.5 mg/L of a polyamine and to methods for cultivating cells in said oligopeptide-free cell culture media comprising at least 0.5 mg/L of a polyamine. The invention also relates to methods for expressing at least one protein in a medium comprising at least 0.5 mg/L of a polyamine and to methods for producing at least one virus in a medium comprising at least 0.5 mg/L of a polyamine.

Abstract: The invention relates generally to compositions and methods for altering the isoelectric point of an antibody, and in some cases, resulting in improved plasma pharmacokinetics, e.g. increased serum half-life in vivo.

Abstract: Anti-SpA murine, chimeric and humanized monoclonal antibodies, and variant antibodies having a heavy chain with at least one amino acid substitution are provided. Such antibodies may be used to prevent or treat microbial infections.

Abstract: The present invention provides isolated polypeptides isolatable from a Staphylococcus spp. Also provided by the present invention are compositions that include one or more of the polypeptides, and methods for making and methods for using the polypeptides.

Abstract: Monoclonal antibodies or antigen-binding fragments thereof that bind to Clostridium difficile (C. difficile) toxin A or toxin B and methods of using the same to detect or treat C. difficile infections and/or C. difficile-associated disease. C. difficile is a gram positive, anaerobic bacterium that causes gastrointestinal disease in humans. The bacteria are transmitted through feces and spread to food and other surfaces when people who are infected do not thoroughly wash their hands.

Abstract: The present invention relates to an antibody against C5, and a method for preventing and treating complement-related diseases using the antibody, wherein the antibody against C5 is effectively usable in preventing and treating complement-related diseases by inhibiting complement activation.

Abstract: [PROBLEM] To provide a monoclonal antibody against a biomarker which shows high specificity and can be effectively used in detection and diagnosis of various lesions relevant to various kinds of carcinomas and foci of necrosis, and so forth. [MEANS] A monoclonal antibody against a necrosis marker consisting the following amino acid sequence: (1) the amino acid sequence of SEQ ID NO: 1, or (2) an amino acid sequence having substitution, deletion and/or insertion of one or several amino acid residues in the amino acid sequence of (1) or sharing a homology of 90% or more with the amino acid sequence of (1), and showing the same function, activity or property as that of the amino acid sequence of (1) as a protein.

Abstract: Hemoglobin, its variants, and glycated forms of each are determined individually in a multiplex assay that permits correction of the measured level of HbA1c to account for glycated variants and other factors related to the inclusion of the variants in the sample. New antibodies that are particularly well adapted to the multiplex assay are also provided.