Abstract: The present invention relates generally to glutaminase inhibitors of Formula I, Formula II, or Formula III, as well as pharmaceutical compounds containing them and methods of their use.

Abstract: Compounds, including those of the following formula: wherein the variables are defined herein, which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.

Abstract: Provided are crystals of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide which are stable and show excellent oral absorbability. The crystals are Form II crystals of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide showing an X-ray powder diffraction spectrum having at least three characteristic diffraction peaks at angles (2?±0.2°) selected from the group consisting of 7.7°, 8.0°, 11.1°, 12.5°, 12.9°, 15.2°, 15.8°, 17.2°, 19.0°, 22.5°, 26.1°, and 27.4°.

Abstract: Compounds of the formula Ia or of the formula Ib in which X, Y, R1 and R2 have the meanings indicated in claim 1, are inhibitors of pyruvate dehydrogenase kinase (PDHK), and can be employed, inter alia, for the treatment of diseases such as cancer.

Abstract: The present invention relates to an adduct of palbociclib, a method of preparing the preparing the same, and a pharmaceutical composition comprising the same. More particularly, the invention provides a crystalline form of palbociclib, a method of preparing the same, as well as a pharmaceutical composition comprising the same.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Abstract: Compounds represented by formula 1 can be potent and/or partially selective for the Kv7.2/7.3 heteromultimer. They may be useful in treating disorders related to seizures, pain, neurotransmitter release, etc.

Abstract: The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R7, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.

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: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.

Abstract: Compounds of formula (I), imidazopyrimidine ketones, as well as preparations and applications thereof. Compounds and pharmaceutically acceptable salts thereof which stimulate the body to produce tumor necrosis factor-related apoptosis-inducing ligands, while avoiding the drawbacks of existing cancer treatments based on recombinant proteins and antibodies. Thus, they can provide novel options for the treatment of related tumors.

Abstract: The present invention provides RUT analogs with various biological activities. In particular, the biological activities comprise anti-inflammatory activity, vasodilator effects, migration/invasion-suppressive activities, ability against damage due to remodeling between the epithelium and endothelium, collagen deposition and cardiac fibrosis suppress, Snail protein inhibitory effect, etc., which may improve cardiac, vasodilation, and lung functions. The RUT analogs disclosed herein also exhibit a lower cytotoxicity comparing to RUT.

Abstract: (?)-Jorumycin, ecteinascidin 743, saframycin A and related compounds, methods of preparing the same, formulations comprising the compounds, and methods of treating proliferative diseases with the same are provided.

Abstract: The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway [Formula should be inserted here] wherein R1, R2, R3, R4 and R5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.

Abstract: The present invention is directed to fused heteroaryl derivative compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract: The present invention relates to a heteroaryl derivative represented by Formula 1 wherein , A, R1, R2, R3, R4, and R5 are as defined herein, or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition for preventing or treating diseases associated with PI3 kinases, containing the same as an active ingredient. The heteroaryl derivative according to the present invention has an excellent effect of selectively inhibiting PI3 kinases, thereby being useful in preventing or treating PI3 kinase diseases such as cancers, autoimmune diseases, and respiratory diseases.

Abstract: The invention relates to compounds having the structure of formula (I) which can be used for the treatment of or against influenza infections.

Abstract: Glucosepane is a structurally complex protein post-translational modification (PTM) believed to exist in all living organisms. Glucosepane possesses a unique chemical structure that incorporates a surprising, never-before-prepared non-aromatic tautomer of imidazole, rendering it a challenging target for chemical synthesis. In this application, the inventors report the first total synthesis of glucosepane and related compounds according to the chemical structure: Methods of synthesis, compounds obtained therefrom, pharmaceutical compositions and methods of treatment provide embodiments of the present invention.

Abstract: A process for manufacturing crystals of 1,4:3,6-dianhydrohexitols, by manufacturing a solution of an internal dehydration product of at least one hexitol, distilling the solution, crystallizing, and wherein the crystallization mother liquors undergo a step of evaporative crystallization. Unlike the prior art processes that seek to recycle the crystallization mother liquors, evaporative crystallization economically and efficiently replaces the succession of steps consisting of at least one concentration, then at least one step of purification by distillation, chromatography, or crystallization.

Abstract: Described herein are thienopyrimidine compounds of Formula (I), and pharmaceutically acceptable salts, and pharmaceutical compositions thereof. Also provided are methods and kits involving the thienopyrimidine compounds or compositions for treating or preventing proliferative diseases such as cancers (e.g., brain tumors such as DIPGs) in a subject. The invention further provides an embryonic stem cell-based tumor cell model, which can be used for drug screening and disease target identification.

Abstract: The present invention relates to an organic light-emitting compound represented by Chemical Formula A and an organic light-emitting device. In Chemical Formula A, X, Y, Z, and the substituents R1 to R8, and R11 to R20 are as defined in the specification.

Abstract: Novel heterocyclic fused systems are disclosed herein which possess numerous biological activities, including but not limited to antibacterial activity, and usefulness to the treatment of many disease states, such as pathogenic infections. In particular, new imidazoles are disclosed along with related processes of preparation and methods of use as antibacterial agents. The disclosed compounds were found to be active against several Gram-positive bacteria, including Enterococcus faecalis and Bacillus subtilis, and were also found to be active against several species of multi-drug resistant Staphylococcus, such as S. aureus, S. saprophyticus, S. haemolyticus, and S. epidermidis.

Abstract: Provided herein are compounds useful for appending amino acids to nucleophiles.

Abstract: The present invention relates to novel compounds of formula (I) as GPR119 agonist, composition compositions containing such compounds and method of preparation thereof.

Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).

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: Provided is a compound which is bioapplicable and amyloid-selective, and is useful as an amyloid oxygenation catalyst applicable not only to A? peptides but also to other amyloids, and a preventive/therapeutic drug for an amyloid-related disease using the same.

Abstract: The disclosure includes high purity compounds having CCR5 and/or CCR2 antagonism, or a salt thereof, and processes for synthesizing the same.

Abstract: The present invention provides processes for the preparation of baricitinib of Formula I and an intermediate of Formula V. The present invention also provides the use of the intermediate of Formula V for the preparation of baricitinib.

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: Compounds of Formula II, wherein X is selected from chloro, fluoro, bromo and iodo, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, or —CH(CH3)2; compositions containing them, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.

Abstract: A silicone oil having a mean molecular weight average greater than about 20,000 Daltons, with no more than about 3% to about 4% of the total silicone oil by weight being comprised of components having a molecular weight less than about 15,000 Daltons. In some embodiments, the silicone oil is used in intraocular lens devices.

Abstract: The present invention discloses an ?-silane coupling agent and application thereof. The ?-silane coupling agent has a structure formula of formula (I): R1 is alkyl with 1 to 6 carbon atoms; R2 is alkyl with 1 to 6 carbon atoms; R3 is alkyl with 1 to 6 carbon atoms; R4 or R5 is selected from one of hydrogen, alkyl with 1 to 18 carbon atoms, aryl, benzyl, ester-containing group, carbamido-containing group or heterocyclic alkane; R4 and R5 are the same or different. The ?-silane coupling agent is applied to silicone rubber, which can be cured without adding a catalyst, and the curing speed is fast; the ?-silane coupling agent has strong reactivity, the surface curing time is less than 2 minutes; and the ?-silane coupling agent has good stability, which can be stored stably under conditions at room temperature for 6 months, and does not easily turn yellow.

Abstract: The present invention relates to novel hardeners for curing epoxy resins and to cure accelerants for the accelerated curing of epoxy resins comprising, in each case, at least one compound from the group of esters of phosphorus-containing acids according to Formula (I), wherein there applies to Formula (I): wherein there applies to the radicals R1, R2, R3, R6, X and indices m, n, p, simultaneously or independently of one another: R1, R2=simultaneously or independently of one another, hydrogen or alkyl, R3=alkyl, aryl, —O-alkyl, —O-aryl, —O-alkylaryl or —O-arylalkyl, R6=hydrogen, alkyl or —NHC(O)NR1R2, X=oxygen or sulphur, m=1, 2 or 3, n=0, 1 or 2, wherein there applies: m+n=3 p=0, 1 or 2.

Abstract: The invention relates to bisphosphites having 2,4-tert-butylphenyl units and a method for the preparation thereof. Furthermore, the invention relates to the use of the compounds as ligands in a ligand-metal complex. The compound, and also the complex, may be used as a catalytically active composition in hydroformylation reactions.

Abstract: Therapeutically-effective amounts of novel analogs or derivatives of alkyl fatty acids, such as but not limited to lipoic acid, and pharmaceutical formulations comprising such analogs or derivatives and pharmaceutically-acceptable carriers therefor, are useful for the treatment, prevention, imaging, and/or diagnosis of medical disorders.

Abstract: The invention relates to the preparation and characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid. The invention also relates to the use of the novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid in pharmaceutical compositions in drug delivery systems for humans. The invention further relates to the use of the novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid or the pharmaceutical compositions thereof to treat and/or prevent a disease state associated with osteoporosis, tumor induced hypercalcemia (TIH), cancer-induced bone metastasis, Paget's disease or for adjuvant or neoadjuvant therapies.

Abstract: There are provided, inter alia, methods for decreasing mucus elasticity or decreasing mucus viscosity in a subject in need thereof, the methods including administering to the subject an effective amount of a thiosaccharide mucolytic agent, and compounds and pharmaceutical compositions useful for the methods.

Abstract: An embodiment of the present invention relates to a compound of the general formula. The compound of formula is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Furthermore an embodiment of the present invention concerns a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.

Abstract: Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation.

Abstract: The present invention relates to methods and intermediates for synthesizing 2?-deoxy-2?,2?-difluorotetrahydrouridine compounds.

Abstract: The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.

Abstract: A class of phosphorus containing polycyclic compounds of general formula I, of general formula I? or of general formula I?, wherein B1, B2, R1, R2, R1?, X1, X2, Y1, Y2, BL1, BL2, Z1, and Z2 are defined herein, that may be useful as modulators of type I interferon production, specifically as STING modulating agents, are provided. Also, provided are use of such compounds.

Abstract: A method of making and a modified allergen having reduced allergenicity and preserved immunogenicity compared to corresponding native allergenic material. The preserved immunogenicity is elicited by a IgG-mediated antibody response, all or part of the primary amine groups of the lysine residues of the native allergenic material are functionalized with carbamoyl or thiocarbamoyl moieties, and all or part of the primary amine groups of the arginine residues of the carbamoyl- or thiocarbamoyl functionalized allergenic material are further functionalized with dialdehyde or diketal moieties. The raw allergenic material is selected from the group consisting of DP mites extract, Der p1, ovalbumin and Lipid Transfer Protein (LTP), the average percentage of modified primary amine groups of the lysine ranges between 75% and 100%; and the average percentage of the substituted arginine residues ranges between 25% and 10%.

Abstract: Ligand functionalized substrates, methods of making ligand functionalized substrates, and methods of using functionalized substrates are disclosed.

Abstract: The present invention is directed to affinity chromatography devices that separate a targeted protein or antibody from an aqueous mixture containing the targeted protein or antibody. The chromatography device may contain a stacked membrane assembly or a wound membrane assembly. The membrane assemblies include (1) at least one polymer membrane that contains therein inorganic particles and (2) at least one impermeable layer (e.g., a thermoplastic polymer in a solid state). The polymer membrane and/or the inorganic particles have an affinity ligand bonded thereto. The affinity ligand may be a protein, an antibody, or a polysaccharide that reversibly binds to the targeted protein or antibody. The chromatography device may be repeatedly used and may be cleaned with a caustic solution between uses. The chromatography devices has a dynamic binding capacity (DBC) of at least 30 mg/ml (or 0.07 micromol/ml) at 10% breakthrough at a residence time of 20 seconds or less.

Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

Abstract: The present invention provides a cell penetrating peptide dimer by oxidative modification, in which each monomer is connected with each other by the disulfide linkage. The drugability of the peptide dimer has been improved through enhancing stability, reducing proteolysis, retaining permeability and increasing heparan sulfate binding specificity. The modified peptide products can be used to deliver drug molecules as a suitable drug carrier for targeted therapy.

Abstract: A pentapeptide associated with integrin receptor ?v?3, which has a sequence of arginine-tryptophan-arginine-asparagine-methionine. The pentapeptide targets tumor cells highly expressing ?v?3, but not tumor cells lowly expressing ?v?3 and normal cells. Accordingly, the pentapeptide is useful in the diagnosis and treatment of cancers.

Abstract: Provided are hydrogel-forming peptides that comprise at least one dyad of hydrophobic amino acid residues in which one is a ?3- or ?2-homo amino acid residue. The hydrogels derived from these peptides can be loaded with biological materials and can be used in physiological conditions.