Abstract: Provided herein are cell penetrating compounds having the Formula I: where, generally, each T is a thiol reactive group (e.g., a phosphorothioate), each L is a linker (e.g., a linear alkyl), and Y is a biologic (e.g., an antibody). Also provided are pharmaceutical compositions including the cell penetrating compounds, and methods of delivering the compound into a cell.

Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to oxadiazaspiro compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular against drug abuse and addiction.

Abstract: An alternative and improved process for the preparation of Apremilast (Formula I) and Apremilast form B or a pharmaceutically acceptable salt thereof is provided. The novel process includes hydrogenation in acetone, Cyclization and acetylation followed by condensation in methyl isobutyl ketone (MIBK) and acetic acid mixture in specific volume ratios.

Abstract: Provided are benzotriazole derivative compounds of the general formula that are novel compounds capable of strongly absorbing light in the ultraviolet range, particularly 300-330 nm, while strongly absorbing light in the visible light short-wavelength range up to around 450 nm and being used suitably as a light absorber having high light fastness with a light-blocking function over an extended period of time. Preferably, R1 is a hydrogen atom or alkyl group, R2 is a C1-8 alkyl group, R3 is a hydrogen atom, alkyl group, acryloyloxyalkyl group, or methacryloyloxyalkyl group.

Abstract: The invention provides compounds of formula (I): wherein X is and the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.

Abstract: Provided herein are compounds that are able to bind metal ions (e.g., free metal ions or metal ions bound to low affinity ligands) in a sample or subject. Also provided herein are methods of using the compounds for chelating metal ions and for the treatment of diseases associated with abnormal levels of metal ions. Methods of preparing the compounds and pharmaceutical compositions are also provided.

Abstract: The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A/B (Rgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to compounds of formula (I) and to pharmaceutical compositions containing them: wherein meanings of the substituents are indicated in the description. Such compounds for use in the treatment of cancer and other diseases related to altered angiogenesis, such as arthritic pathology, diabetic retinopathy, psoriasis and chronic inflammatory disease, are also within the scope of the present invention.

Abstract: The present application relates to novel whitening agents for cellulosic substrates. The whitening agents are comprised of at least two constituents: at least one chromophore constituent and at least one polymeric constituent. Suitable chromophore components generally fluoresce blue, red, violet, or purple color when exposed to light, or they may absorb light to reflect these same shades. The whitening agents are further characterized by the polymeric component comprising at least two repeating glycerol units. This disclosure also relates to laundry care compositions including but not limited to liquid and/or powder laundry detergent formulations and rinse added fabric softening (RAFS) compositions that comprise such whitening agents.

Abstract: A fluidized-bed catalyst suitable for the production of halogenated aromatic nitriles includes an active component and a support. The active component is a complex having the following composition expressed in atomic ratio: VPaCrbAcMdOx, wherein A represents at least one metal selected from the group consisting of alkali metals and alkaline earth metals; M represents at least one element selected from the group consisting of Ti, Zr, Hf, La, Ce, Nb, Mo, W, Co, Zn, Fe, Ni, B, Sb, Bi, As, Ga, Ge, Sn, and In; in the XRD spectrum of the catalyst, diffraction peaks are present at 2?=27.8±0.5° and 2?=13.8±0.5°, and the ratio of the height (I1) of the diffraction peak at 2?=27.8±0.5° to the height (I2) of the diffraction peak at 2?=13.8±0.5° is 3.5-6, i.e. I1:I2=3.5-6.

Abstract: Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.

Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating non-alcoholic steatohepatitis are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.

Abstract: The present application is directed to excimer forming compounds of Formula I: W—V—[Y]n wherein W is an excimer forming fluorophore, V is a linker moiety, Y is a metal ion coordinating moiety and n is 1, 2 or 3. In particular, the application is directed to excimer forming compounds for the detection of proximally phosphorylated sites including those found on polypeptides, proteins, pyrophosphate and RNA, for example in aqueous solution, polyacrylamide gels blotting membranes, solid-support assays and in cell culture samples.

Abstract: The present invention relates to a crystalline metal organic framework which comprises repeating units of formula (RR)-(IA) or (SS)-(IA) or (RS)-(IA) or (SR)-(IA); or alternatively of formula (RR)-(IB) or (SS)-(IB) or (RS)-(IB) or (SR)-(IB) and a composition containing it. It also relates to processes for their preparation and their uses as a separation agent and as a catalyst.

Abstract: The present invention provides a photoelectric conversion element exhibiting excellent responsiveness, and excellent photoelectric conversion efficiency in a case where the photoelectric conversion film is a thin film, an optical sensor, an imaging element which include the photoelectric conversion element, and a compound. The photoelectric conversion element of the present invention includes a conductive film, a photoelectric conversion film, and a transparent conductive film, in this order, in which the photoelectric conversion film contains a compound represented by Formula (1) and having a structure represented by Formula (2).

Abstract: Disclosed are a class of URAT1 inhibitor compounds and the use of such compounds. These compounds are compounds represented by the structure of formula (I) or pharmaceutically acceptable salts thereof. Experiments show that the compounds provided by the present invention have a very good inhibitory effect on hURAT1-transported uric acid in HEK293 transfected cells, and show that such compounds have a good potential for application in the treatment of hyperuricemia or gout.

Abstract: A polymer consisting of small functional molecules can be integrated into solar thermal fuels in the solid-state for solar energy harvesting and storage. In certain embodiments, a solar energy storage device can include one or more layers of photoswitchable moieties associated with a polymer. Such solar thermal fuel polymers can be used to enable deposition from low concentration solutions, resulting in uniform and large-area thin-films. This approach enables conformal deposition on a variety of conducting substrates that can be either flat or structured and control over film growth via electrodeposition conditions and results in highly uniform and large-area thin films.

Abstract: A SIRT6 activating molecule as shown in Tables 1-3 or a compound according to a pharmacophore as described herein.

Abstract: Disclosed in the present specification is a method capable of preparing N-[4-[(1R)-1-[[(R)-(1,1-dimethylethyl)sulfinyl]amino]ethyl]-2,6-difluorophenyl]-methanesulfonamide (INT028-2) with high optical purity, through the selection of Ellman-chiral auxiliaries and the recrystallization and separation of optical isomers. According to the above method, high-purity N-[4-[(1R)-1-[[(R)-(1,1-dimethylethyl)sulfinyl]amino]ethyl]-2,6-difluorophenyl]-methanesulfonamide with excellent quality can be produced at room temperature by improving cryogenic process conditions necessary for realizing high optical purity, and thus the trimming due to the process failure rate can be remarkably reduced.

Abstract: The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.