Abstract: Disclosed in the present invention are a salt type and crystal type of 4H-pyrazolo[1, 5-alpha]benzimidazole compound and the preparation method and intermediate thereof.

Abstract: The invention relates to glucuronide prodrug compounds of the Janus kinase (JAK) inhibitor tofacitinib having formula I: where A1 and R1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, Y, A, W, R2, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of Formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.

Abstract: The invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS symptoms in a mammal using compounds of Formula I.

Abstract: Compounds of formula (I); wherein R1, R2, R3, R4, R5, R6, R7, R8, R14, W, A and n are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring a pro-apoptotic agent.

Abstract: The invention generally relates to novel fluorophore-labeled, bi- or multi-functional, chemically reactive and/or biologically active conjugates, and related compositions and methods thereof.

Abstract: In various embodiments novel rapamycin analogs are provides that show improved mTORC1 specificity.

Abstract: This disclosure provides methods of making certain 7-aminocephem derivatives useful in the manufacture of cephalosporin antibiotic compounds.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: Chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with P13 kinase activity are described herein.

Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.

Abstract: The present invention is related to crystalline forms of (S)-7-(1-(9H-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one which is a PI3K inhibitor useful in the treatment of cancer and other diseases.

Abstract: A method is disclosed for altering the redox equilibrium of a transmembrane receptor-like protein tyrosine phosphatase (RPTP), particularly a type IIa RPTP, by chemically modulating the activity through contact of such an enzyme with a diaryl boron compound that preferentially reacts with an RPTP in an oxidized state (CyS-OH). This redox modulation is most readily observed and put to use by assaying the inhibition of the phosphatase activity of the RPTP. Such an assay can be carried out on an enzyme in vitro or by contacting the enzyme in a living organism (in vivo). A useful diaryl boron compound corresponds in structure to Formula I in which Ar-1, Ar-2, R1, R2, R3 and R4 are defined within. A pharmaceutical composition containing a useful diaryl boron compound is also disclosed, as are particularly preferred diaryl boron compounds.

Abstract: The present invention provides processes for preparing silanylamines, such as disilanylamines and polysilanylamines, and compositions comprising the silanylamines. In one embodiment, the present invention provides processes for preparing a silanylamine compound, the processes comprising reacting a starting compound of general formula RR1N—(SixH2x+1) with an amine compound of general formula R2R3NH to produce the silanylamine compound of general formula R2mR3n-N(SixH2+1)3-m-n.

Abstract: Cyanoalkylfluorosilanes are prepared in exceptionally high yield by the reaction of the corresponding cyanoalkylchlorosilanes with specific metal fluorides. The products are useful in lithium ion battery electrolyte composition.

Abstract: The present invention relates to a process for preparing a tris[3-(alkoxysilyl)propyl] isocyanurate from the group of tris[3-(trialkoxysilyl)propyl] isocyanurate, tris[3-(alkyldialkoxysilyl)propyl] isocyanurate and tris[3-(dialkylalkoxysilyl)propyl] isocyanurate by hydrosilylation, by in step A initially charging a mixture comprising 1,3,5-triallyl-1,3,5-triazine-2,4,6(1H,3H,5H)-trione as olefin component, at least one carboxylic acid and a Pt catalyst, heating the mixture to a temperature of 50 to 140° C., in step B adding at least one hydroalkoxysilane from the group of hydrotrialkoxysilane, hydroalkyldialkoxysilane, hydrodialkylalkoxysilane [called H-silane(s) for short] to the mixture from step A while mixing, in step C leaving the mixture from step B to react while mixing, with addition of at least a defined amount of alcohol to the mixture as further cocatalyst, and in step D working up the product mixture thus obtained.

Abstract: The present invention relates to a process for preparing a tris[3-(alkoxysilyl)propyl] isocyanurate from the group of tris-[3-(trialkoxysilyl)propyl] isocyanurate, tris[3-(alkyldialkoxysilyl)propyl] isocyanurate and tris[3-(dialkylalkoxysilyl)propyl] isocyanurate by hydrosilylation, by in step A initially charging a mixture comprising at least one hydroalkoxysilane from the group of hydrotrialkoxysilane, hydroalkyldialkoxysilane, hydrodialkylalkoxysilane [called H-silane(s) for short], at least one carboxylic acid and a Pt catalyst, heating the mixture to a temperature of 50 to 140° C., in step B adding a mixture of 1,3,5-triallyl-1,3,5-triazine-2,4,6(1H,3H,5H)-trione and at least one alcohol to the mixture from step A while mixing, in step C leaving the mixture from step B to react while mixing and in step D working up the product mixture thus obtained.

Abstract: Provided herein are transmitter ligands that improve photon upconversion of near infrared light (NIR) to visible light. The presently provided ligands are complexed to semiconductor nanocrystals and improve triplet energy transfer from semiconductor nanocrystal to annihilator in triplet-triplet annihilation. Suitable applications include bio-imaging.

Abstract: The present invention relates to a metallocene compound, and preparation and use thereof, and the compound can be used as a catalyst for synthesis of poly-?-olefin as lubricating base oil. The metallocene compound includes a substituted aryl group, a bridged atom, an optionally unsubstituted, 3-mono-substituted or 3,6-disubstituted 5H-indeno [1,2-b] pyridyl group or optionally unsubstituted, 3-mono-substituted or 3,6-disubstituted 5H-indeno [1,2-b] thiopyranyl group, and a metal coordination group. As a catalyst, the metallocene compound is shown to be structurally stable and high in catalytic efficiency, and the preparation of the catalyst is relatively easy in operation, high in yield, low in cost, low in pollution and easy to scale up for industrial production.

Abstract: There is provided phospholipid-peptide or phospholipid-protein conjugates useful for identification of autoantibodies, and in particular autoantibodies directed towards phospholipids. There is further provided intermediates and methods for their preparation as well as synthesis of the phospholipid-peptide or phospholipid-protein conjugates.

Abstract: Described herein is an enzyme-mediated approach to bioconjugation at nanoparticle (NP) surfaces. This process is enabled by a new synthetic linker compatible with the covalent attachment of alkyne modified substrates, including dyes, peptides and nucleic acids. The methods described herein specifically allow for the linkage of molecules to a DNA-functionalized nanoparticle surface. Enzymatic ligation of molecules to the terminal hydroxyl group of DNA using T4 DNA ligase is achieved through incorporation of a single monophosphate on the approaching substrate. In contrast to previous strategies, the linkers disclosed herein are compatible with alkyne modified molecules of a variety of sizes and charges indicating that the ligase minimally requires the monophosphate and the incoming hydroxyl for conjugation to be successful.

Abstract: The invention relates to Brønsted-acidic fluoroalkyl phosphonates as bifunctional catalysts and to processes for the preparation thereof.

Abstract: Provided herein are optically active compounds of the formulae (ii); and (III) and pharmaceutical compositions thereof. Also provided herein are processes of making these compounds and resolving the racemic mixture or the enrichment of same with in one of its enantiomers to provide (R)- and (S)-1-(3-(3-N,N-dimethylaminocarbonyl)phenoxyl-4-nitrophenyl)-1-ethyl-N,N?-bis(ethylene)phosphoramidate, and methods of treating cancer comprising administering such compounds.

Abstract: The synthesis of 2D metal chalcogenide nanosheets and metal-ion or metalloid-ion doped 2D metal chalcogenide nanosheets by adding a metal complex to a hot dispersing medium. The mean lateral dimension of the nanosheets may be controlled by appropriate temperature selection.

Abstract: Metal complexes useful as emitters in OLEDs are disclosed.

Abstract: Provided herein are platinum complexes of Formula I: Also, provided are methods of making the platinum complexes of Formula I and apparatuses that include platinum complexes of Formula I. The apparatuses can include near infrared organic light emitting devices.

Abstract: A method of enhancing the growth of an animal is provided. The method includes causing the animal to ingest or absorb an effective amount of a preparation obtainable by a process including, bringing a tyrosinate moiety into contact with an Fe(III)-containing substance, optionally wherein the tyrosinate moiety is tyrosine and it is brought into contact with the Fe(III)-containing substance in the presence of a base, or wherein the tyrosinate moiety is a tyrosine salt and it is brought into contact with an Fe(III)-containing substance. Methods for inhibiting, reducing, or preventing biofilm formation or buildup on a surface; the treatment of, inhibition of growth of, and inhibition of colonization by, bacteria, both in biological and non-biological environments; disinfecting surfaces, potentiating the effects of antibiotics and other anti-microbial agents, and increasing the sensitivity of bacteria and other microorganisms, to anti-microbial agents are also provided.

Abstract: The present invention relates to highly efficient Nrf2 activators-CO-releasing molecules of formula (I) and (II) capable of increasing HO-1 protein expression and simultaneously releasing CO, their synthesis and their use in therapeutic applications, in particular their use in the treatment of inflammatory or cardiovascular diseases, wherein CORM represents a carbonyl metal complex chosen from among: Mn(CO)5, formula (III), (IV), (V), (VI), (VII), (VIII) and (IX).

Abstract: The invention comprises GalNAc phosphoramidite derivatives of the formula I wherein R1 is a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20 and its corresponding enantiomers and/or optical isomers thereof. The invention further comprises a process for the preparation of the GalNAc phosphoramidite derivatives of the formula I and its use in the preparation of therapeutically valuable GalNAc-cluster oligonucleotide conjugates.

Abstract: This invention discloses the use of aminoglycoside antibiotics such as gentamicin B1 to suppress premature termination codons during translation and promote the full length read-through of transcripts such as p53 that incorporate nonsense mutations and to treat disease conditions such as cancer caused by such genetic mutations.

Abstract: Disclosed are steviol glycosides referred to as rebaudioside V and rebaudioside W. Also disclosed are methods for producing rebaudioside M (Reb M), rebausoside G (Reb G), rebaudioside KA (Reb KA), rebaudioside V (Reb V) and rebaudioside (Reb W).

Abstract: Disclosed are steviol glycosides referred to as rebaudioside V and rebaudioside W. Also disclosed are methods for producing rebaudioside M (Reb M), rebausoside G (Reb G), rebaudioside KA (Reb KA), rebaudioside V (Reb V) and rebaudioside (Reb W).

Abstract: Disclosed are steviol glycosides referred to as rebaudioside V and rebaudioside W. Also disclosed are methods for producing rebaudioside M (Reb M), rebausoside G (Reb G), rebaudioside KA (Reb KA), rebaudioside V (Reb V) and rebaudioside (Reb W).

Abstract: The present disclosure provides nicotinate/nicotinamide riboside compounds or derivatives of formula (I): wherein X?, Z1, Z2, n, R1, R2, R3, R4, R5, R6, R7, and R8 are described herein, reduced analogs thereof, and synthetic processes for the preparation thereof.

Abstract: Antimicrobial compounds and compositions of Formula (I) and methods of use are disclosed.

Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent, and methods of using the compounds and compositions for treatment of viral infections, especially HRV.

Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disease and conditions, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.

Abstract: The invention provides a compound of formula I: wherein R1-R6 and X have any of the values described herein, as well as pharmaceutical compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.

Abstract: A compound of Formula (I) wherein Y1, Y2, X1, X2, R1, R2, R3, R4, R5, R6, R8, and R9 are as defined herein; and pharmaceutically acceptable salts and tautomers thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, in the treatment of diseases in which modulation of STING (Stimulator of Interferon Genes) is beneficial, for example inflammation, allergic and autoimmune diseases, infectious diseases, cancer, pre-cancerous syndromes and as vaccine adjuvants.

Abstract: Methods for modulating (inhibiting or stimulating) retinoid-related orphan receptor ? (ROR?) activity. This modulation has numerous effects, including inhibition of TH-17 cell function and/or TH-17 cell activity, and inhibition of re-stimulation of TH-17 cells, which are beneficial to treatment of inflammation and autoimmune disorders. Stimulation of ROR? results in stimulation of TH-17 cell function and/or activity which is beneficial for immune-enhancing compositions (e.g., vaccines).

Abstract: Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.

Abstract: Disclosed herein are novel HDAC inhibitors. The HDAC inhibitors may be used in methods of treating cancer. The HDAC inhibitors may be used in methods of treating a neurological disorder.

Abstract: The present invention relates to method for connecting a protein and a drug to a protein drug conjugate, wherein the drug is linked to the protein through a specific branched linker, said branched linker comprises a peptide chain and is derived from o-hydroxy p-amino benzylic alcohol, wherein the peptide chain is connected to the phenyl ring via the p-amino group, the drug is connected to the phenyl ring via the benzylic alcohol moiety, and the protein is connected to the phenyl ring via the o-hydroxy group; further to a process for the preparation of said protein-drug-conjugates via various intermediates, to the pharmaceutical use of such protein drug conjugates, such as methods of controlling the growth of undesirable cells, to pharmaceutical compositions comprising such protein drug conjugates, and to intermediates of the preparation of the protein drug conjugates.

Abstract: Methods of making copolymers are described.

Abstract: Tetrapeptide linkers for reversibly linking a first compound to a amine-containing second compound are described. Compounds containing the tetrapeptide linkers and methods of using the tetrapeptide linkers are also described.

Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorders, such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

Abstract: The present invention relates to targeted microcapsules comprising a skin aging compound to target fibroblast with a peptide, which is a FGF receptor agonist, wherein said peptide is coupled to the outer surface of the microcapsule. It also relates to the use of said microcapsules for the cosmetic prevention and/or cosmetic treatment of cutaneous effects of skin aging and to the cosmetic compositions comprising said microcapsules. The invention also relates to the FGF receptor agonist peptide coupled to the microcapsule.

Abstract: An object of the present invention is to conduct a search for a compound to be arranged at a terminal of a peptide nucleic acid effective in detecting a single nucleotide polymorphism. Provided is a tolan compound represented by the following formula (1): wherein R1 represents a phenyl group or a naphthyl group, the phenyl group may have 1 to 5 substituents that are identical to or different from each other, and the naphthyl group may have 1 to 7 substituents that are identical to or different from each other.

Abstract: The present invention describes unique means for reducing autoreactivity that sensitizes against sustained treatments, and toxicity associated with administration of biologicals, in order to develop safer cancer immunotherapeutics. Short functional sequences are identified in the biologic and matched to their most homologous human counterpart. The human homologs are swapped in to replace their foreign counterparts. Alternatively, variants are selected that have exhibit less toxicity in human or primate experiments from nature, and these sequences are swapped in to replace their counterparts in the biologic. Also, human sequences that mediate the same function as foreign sequences in the biologic, but lack any sequence homology, can be swapped in for their foreign sequence counterparts. These inventions are applied to derivatize the HIV/SIV Tat protein into humanized trimers (CATS) useful for the treatment of cancer.