Abstract: The present invention provides a compound of formula (1) and a pharmaceutical composition comprising the compound useful as a nerve regeneration promoter wherein R1-L- is R1—OC(O)—, or the like, R1 is hydrogen atom, optionally-substituted C1-6 alkyl group, optionally-substituted 3- to 8-membered cycloalkyl group, or the like, R2 is hydrogen atom or the like, Ring A is formula (2) or formula (3) wherein R3 is hydrogen atom, optionally-substituted C1-6 alkyl group, or the like, the part of X, Y, and Z is X?Y—Z, X—Y?Z, or X—Y—Z, X is nitrogen atom, NR4 (R4 is hydrogen atom, optionally-substituted C1-6 alkyl group, or the like), or the like, Y is carbon atom or the like, and Z is carbon atom, nitrogen atom or the like.

Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein X is O, S or NR5; or X is —C(R6)?C(R7)—, wherein the carbon atom bonded to R6 is also bonded to the carbon atom bonded to R4, and the carbon atom bonded to R7 is also bonded to the phenyl ring moiety in Formula 1; and R1, R2, R3, R4, R5, R6, R7, G and W are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.

Abstract: The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of ATR kinase for the treatment or prevention of cancer.

Abstract: There are provided, inter alia, compounds useful for binding to deoxycytidine kinase, and compounds and methods useful to modulate deoxycytidine kinase.

Abstract: Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.

Abstract: Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2?-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.

Abstract: Compounds having the following formula (I) and methods of their use and preparation are disclosed:

Abstract: The present invention provides novel pharmaceutically acceptable salts of a morpholine derivative, including a malate, a tartrate, a hydrochloride, an acetate, and a naphthalene disulfonate thereof, wherein the tartrate has 3 crystal salt forms: crystal form A, crystal form B and dihydrate; the malate, the hydrochloride, and the acetate each have one crystal salt form; the naphthalene disulfonate is amorphous. When compared to the known morpholine derivative free base, the present invention has one or more improved properties, e.g., a better crystalline state, greatly improved water solubility, light stability and thermal stability, etc. The present invention further provides preparation methods for the salts of morpholine derivative and the crystal forms thereof, pharmaceutical compositions and use thereof.

Abstract: The present invention is concerned with indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula I wherein Ar1, A2, R1, R2, R3, X and n are as described herein and pharmaceutically acceptable salts thereof for treatment of central nervous system disorders

Abstract: Compounds of Formula (I), their preparation, and use in preventing or treating a bacterial infection are disclosed.

Abstract: The present invention relates to pyrazole fused-ring derivatives, their preparation methods, and use thereof in medicine. In particular, the present invention relates to a novel derivative represented by formula (I), and a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising the same and a method for preparing the same. The present invention also relates to use of the derivatives and the pharmaceutically acceptable salt thereof or the pharmaceutical composition comprising the same in the preparation of therapeutic agents, in particular Bruton tyrosine kinase inhibitors, and preparing a medicament for treating and/or preventing tumors and inflammatory associated diseases. The substituents on formula (I) are defined same as in the specification.

Abstract: The present invention relates to substituted xanthine derivatives, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment of conditions having an association with TRPC5 containing ion channels.

Abstract: Provided herein are compounds of Formulae (RL), (I), (II), (III), (IV), and (V), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, prodrugs, and isotopically labeled derivatives thereof. Also provided are pharmaceutical compositions, kits, and methods involving the inventive compounds for the treatment of metabolic disorders (e.g., diabetes, hyperglycemia, impaired glucose tolerance, insulin resistance, obesity). The compound are useful as substrate selective inhibitors of insulin-degrading enzyme (IDE).

Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl) pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group —CH2—OR3, —CH2—NR4R5 or —C(?O)-NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group —CR8AR8B—OH, —CH2—NR9R10, —C(?O)—NR11R12 or —CH2—OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.

Abstract: The present invention relates to solid state forms of a p-toluenesulfonic acid salt (PTSA) of the selective PI3K delta inhibitor (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one (TGR-1202). The present invention also relates to methods of preparing the same, pharmaceutical compositions containing them, and methods of treating a PI3K kinase mediated disease or disorder, such as cancer, by administering the same.

Abstract: Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.

Abstract: The present invention relates to 1,3-disubstituted-1H-pyrazolo[3,4-d]pyrimidin-4-amine derivatives, 5,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives or 5,7-disubstituted-imidazo[5,1-f][1,2,4]triazine-4-amine derivatives, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compounds, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjögren's Syndrome, and other CFTR associated disorders.

Abstract: The present invention relates to 1,3-disubstituted-1H-pyrazolo[3,4-d]pyrimidin-4-amine derivatives, 5,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives or 5,7-disubstituted-imidazo[5,1-f][1,2,4]triazine-4-amine derivatives, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compounds, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjögren's Syndrome, and other CFTR associated disorders.

Abstract: The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.

Abstract: Methods of treating infections due to Helicobacter pylori (H. pylori), in particular in subjects having a peptic ulcer, are disclosed where the methods comprise administering inhibitors of H. pylori MTAN (5?-methylthioadenosine nucleosidase) to the subject.

Abstract: Provided are certain fused term or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof.

Abstract: The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.

Abstract: The present invention relates to crystalline forms of N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide, and pharmaceutical compositions containing the same. The crystalline forms can be easily used for the preparation of a pharmaceutical composition containing the same as an active ingredient.

Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiazine dioxide compounds bearing an ether linker, including compounds Formula (I) or a tautomer thereof and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, R3, RA, ring A, m, n, -L1-, ring B, RB, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

Abstract: Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are 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: Provided herein are mechanically interlocked air-stable persistent organic radicals. The radical compositions may access a multiplicity of radical, cationic redox states as well as a fully cationic redox state. A composition comprises a first ring mechanically interlocked with a second ring or a salt thereof, wherein the first ring comprises a 4,4?-bipyridinium subunit or a derivative thereof and a diazapyrenium subunit or a derivative thereof and the second ring comprises a 4,4?-bipyridinium subunit or a derivative thereof. In some embodiments, the second ring further comprises a diazapyrenium subunit or a derivative thereof. Methods of preparing the compositions are also provided.

Abstract: Provided herein are supramolecular assemblies, the supramolecular assemblies comprising a racemic mixture of rigid macrocycles capable of interacting through [C—H . . . O] hydrogen bonds. Also provided herein are methods for preparing supramolecular assemblies, the method comprising providing a mixture of rigid macrocycles capable of interacting through [C—H . . . O] hydrogen bonds, the mixture of rigid macrocycles comprising a first rigid macrocycle enantiomer and a second rigid macrocycle enantiomer, and providing a solvent.

Abstract: A phosphorescent compound of formula (I): wherein: M is a transition metal; C1 is a carbon atom forming a metal-carbene bond with M; A is a saturated bridged bicyclic or saturated bridged tricyclic group consisting of one nitrogen atom and 6-12 carbon atoms; either: (i) X1 is a bridgehead carbon atom of the bridged bicyclic or bridged tricyclic group and X2 is NR1 wherein R1 is a substituent, or (ii) X1 is N and X2 is a bridgehead group of formula CR6 wherein R6 is H or a substituent; Ar1 is a C6-20 aromatic group or a 5-20 membered heteroaromatic group; L in each occurrence is independently a mono- or poly-dentate ligand other than a ligand of formula A-Ar1; x is at least 1; and y is 0 or a positive integer. The compound of formula (I) may be used as a blue light-emitting material in a white organic light-emitting device.

Abstract: Cyclometallated Ir complex comprising three N,N diaryl substituted carbene ligands, bearing substituents in the 2 position of the non-cyclometallated aryl ring; an organic electronic device, preferably an organic light-emitting diode (OLED), comprising at least one cyclometallated Ir complex as described above, a light-emitting layer comprising said cyclometallated Ir complex preferably as emitter material, preferably in combination with at least one host material, use of said cyclometallated Ir complex in an OLED and an apparatus selected from the group consisting of stationary visual display units, mobile visual display units, illumination units, units in items of clothing, units in handbags, units in accessories, units in furniture and units in wallpaper comprising said organic electronic device, preferably said OLED, or said light-emitting layer. The present invention further relates to a process for the preparation of said cyclometallated Ir complex.

Abstract: Provided herein are a symmetrical pincer metal and bimetallic complexes. The symmetrical pincer metal complex includes a structure according to Formula I: wherein M is a metal; each N and N? is independently nitrogen or carbon; Z is selected from the group consisting of CH, C, and N; n is 0-3; each L is independently a neutral or charged ligand; and each R is independently an alkyl, Nx, CH2TMS. The symmetrical bimetallic complex includes a structure according to Formula II: wherein M is a metal; each N and N? is independently nitrogen or carbon; Z is selected from the group consisting of CH, C, and N; n is 0-3; each L is independently a neutral or charged ligand; and wherein each R is independently an alkyl, Nx, CH2TMS. Also provided herein is a method of catalyzing a reaction including administering one or more of the compounds disclosed herein.

Abstract: The present invention provides a complex of formula (1), wherein, M is palladium or nickel, R1 and R2 are independently organic groups having 1-20 carbon atoms, or R1 and R2 are linked to form a ring structure with the phosphorus atom, R3 is selected from the group consisting of substituted and unsubstituted aryl, substituted and unsubstituted heteroaryl, and substituted and unsubstituted metallocenyl, R4 is an organic group having 1-20 carbon atoms, n is 0, 1, 2, 3, 4 or 5, and X is an anionic ligand. The invention also provides a process for the preparation of the complex, and its use in carbon-carbon or carbon-nitrogen coupling reactions.

Abstract: The invention relates to compounds for inhibiting a cancer cell or a virus. Particularly, the invention provides compounds for inhibiting, treating and/or preventing cancer and Zika virus.

Abstract: The present invention provides a phenylpropanoid compound and a preparation method and use thereof. The phenylpropanoid compound has a structural formula shown as formula (I), and the pharmaceutically acceptable salt has a structural formula shown as formula (II), formula (III), formula (IV), or formula (V). The phenylpropanoid compound and the pharmaceutically acceptable salt thereof have an effect on inhibiting a content of an inflammatory cytokine NO and an expression of an inflammatory cytokine TNF-?, have an effect on inhibiting a hydroxyl radical (—OH), thereby have anti-inflammatory and antioxidant activities, and has a good application prospect in preparing of a medicine for treating an inflammatory disease related to the above factors, such as cervicitis, endometritis, pelvic inflammatory disease, mastitis, sphagitis and/or arthritis.

Abstract: Novel aminoglycosides, represented by Formulae Ia and Ib, as defined in the instant specification, are disclosed. Also disclosed are pharmaceutical compositions containing the same, and uses thereof in the treatment of medical conditions associated with a pathogenic microorganism.

Abstract: Novel aminoglycosides, represented by Formulae I, Ia, III and IIIa, as defined in the instant specification, designed to exhibit stop codon mutation readthrough activity, are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic diseases and disorders, such as diseases and disorders associated with stop codon mutations.

Abstract: The invention provides a high throughput, high purity, high yield system and method of isolating and purifying rebaudioside A (“Reb A”), with acceptable water solubility for all commercial uses, from commercially available Stevia rebaudiana starting material. The invention also provides a means of maximizing yields of 99+% purity Reb A based on the attributes of a given batch of Stevia starting material. The purity of the Reb A final product, up to 99+% purity, can be selected based on a starting material assay.

Abstract: Provided herein are methods, compounds, and compositions for reducing expression of an ANGPTL3 mRNA and protein in an animal. Also provided herein are methods, compounds, and compositions for reducing lipids and/or glucose in an animal. Such methods, compounds, and compositions are useful to treat, prevent, delay, or ameliorate any one or more of cardiovascular disease and/or metabolic disease, or a symptom thereof, in an individual in need thereof.

Abstract: Provided are compounds of Formula I, as well as pharmaceutical compositions containing compounds of Formula I and methods for treating Orthomyxoviridae virus infections by administering these compounds. The compounds, compositions, and methods provided are particularly useful for the treatment of Human Influenza virus infections.

Abstract: This disclosure features dinucleotide compounds that modulate Stimulator of Interferon Genes (STING) activity, for use for example in the treatment of cancer. This disclosure also features compositions as well as other methods of using and making the same (Formula (A)). A and B are each independently selected from the group consisting of Formulae (i), (ii), (iii), and (iv).

Abstract: The invention relates to double-stranded ribonucleic acid (dsRNA) compositions targeting the COL1A1, TGF-?, and SMAD2/3 genes, and methods of using such dsRNA compositions to inhibit expression of COL1A1, TGF-?, and SMAD2/3.

Abstract: The disclosure provides a protein-poly(amino acid) conjugate and a protein-poly(amino acid) cyclic conjugate, as well as a poly(amino acid) for preparing such conjugates. In addition, the disclosure provides a method for preparing such conjugates and such poly(amino acid).

Abstract: Charge variants of a recombinantly expressed antibody population may be separated both from the main antibody molecule and from each other. Separation and isolation of charge variants may proceed via a combined modulation of salt concentration and pH during charge variant elution from a cation exchange support. Isolated charge variants may be assessed for their contribution to the potency of the overall antibody preparation. The make-up of an antibody preparation, at least in terms of the proportion of charge variants and of the main antibody can thus be controlled, for example, for biosimilar matching or for improving potency of the preparation.

Abstract: The invention provides methods of producing and purifying fusion proteins containing a domain capable of binding one or more extracellular matrix components, such as heparin and chondroitin sulfate, by cation-exchange chromatography.

Abstract: A process for purifying fibrinogen from a fibrinogen containing source by precipitation of fibrinogen by a precipitating agent from a fibrinogen containing solution in the presence of one or more chelating agent(s) and removal of the supernatant from the fibrinogen paste, characterised in that fibrinogen is extracted from the paste forming a liquid fraction containing fibrinogen, and an undissolved residue, which is separated from the liquid.

Abstract: The invention relates to thioether monomer and dimer peptide molecules which inhibit binding of ?4?7 to the mucosal addressing cell adhesion molecule (MAdCAM) in vivo.

Abstract: Disclosed herein are novel antimicrobial peptides, pharmaceutical compositions containing the peptides, and methods of use of the peptides to inhibit the growth or proliferation of microbes. The antimicrobial peptides are particularly useful to treat infections of dangerous gram positive organisms such as MRSA and VRSA.

Abstract: Compounds comprising peptides and peptidomimetics capable of binding C3 protein and inhibiting complement activation are disclosed. These compounds display greatly improved complement activation-inhibitory activity as compared with currently available compounds. Methods of making and using the compounds are also disclosed.

Abstract: Disclosed are capsid-modified rAAV expression vectors, as well as infectious virions, compositions, and pharmaceutical formulations containing them. Also provided are methods of preparing and using the disclosed capsid-protein-mutated rAAV constructs in a variety of diagnostic and therapeutic modalities, including, inter alia, as mammalian cell-targeting delivery agents, and as human gene therapy vectors. Also disclosed are large-scale production methods for capsid-modified rAAV expression vectors, viral particles, and infectious virions having improved transduction efficiencies over those of the corresponding, un-modified, rAAV vectors, as well as use of the disclosed compositions in the manufacture of medicaments for a variety of in vitro and/or in vivo applications.

Abstract: The present invention relates to polymerized recombinant proteins, to recombinant nucleic acids coding for the polymerized recombinant proteins, to expression cassettes comprising the recombinant nucleic acids, to host cells transformed by the expression cassettes and to a method for multimerizing a recombinant protein. The polymerized proteins of the invention may be used in pharmaceutical or immunogenic compositions. In particular, the recombinant proteins may be antigens, antibodies or scaffolds. In particular, the polymerized recombinant protein may be an influenza haemagglutinin.