Abstract: Disclosed are novel crystalline salts of (S)-6-((1-acetylpiperidin-4-yl)amino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)pyrimidine-4-carboxamide and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.

Abstract: The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.

Abstract: Provided here in are compounds of Formula I having the structure: Also provided herein are compositions comprising compounds of Formula I and methods of using compounds of Formula I for the treatment of disorders, diseases or conditions mediated by GluN2B receptors.

Abstract: Disclosed are a novel crystalline form and an amorphous form of Olaparib, and the process for their preparation.

Abstract: Compounds that are agonists of the MCIR receptor and that exhibit reduced toxicity relative to other compounds of the same class are described. These compounds can have the general formula (I) wherein: R1 represents a cyclopropylmethyl or a 4-hydroxybutyl group; R2 represents a hydrogen atom or a methyl group; and also the salts and enantiomers of the corresponding compounds of general formula (I). Also described, are methods for treating hypopigmentary pathologies and photosensitive dermatoses.

Abstract: A contrast agent precursor is revealed. The contrast agent precursor includes a 1,4,7-Tris(carbonylmethyl)-1,4,7,10-tetraazacyclododecane that forms complexes with radioisotopes or connects to a peptide. The contrast agent precursor also includes a 2-nitroimidazole that allows the precursor to become retained in hypoxic tissues According to the features mentioned above, the contrast agent prepared by the precursor has a better binding specificity, labeling accuracy and detection sensitivity. Moreover, a method for preparing the contrast agent precursor not only solves the emulsion problem generated during conventional synthesis of intermediate products but also provides a solution to the problem of residual trifluoroacetic acid. Both the yield rate and the purity of the final product are also improved.

Abstract: The present invention relates to compounds of formula (I) or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R1, R2, R3, R4, X, and Z? have one of the meanings as defined in the specification, to the use of compounds of formula (I) as medicaments, to pharmaceutical compositions comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I). The compounds are ENaC inhibitors useful for the treatment of respiratory diseases and allergic diseases of the airways.

Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: Described herein are compounds and compositions for the treatment of a fibrotic disease.

Abstract: The present invention relates to a process for preparing substituted piperidine compounds and especially chiral substituted piperidine compounds. The process involves reacting a substituted pyridinium ion with an amine as defined herein, in the presence of a hydrogen donor, a catalysts and a suitable solvent.

Abstract: Oxazolidines, a process for producing the oxazolidines, and use as additives for fuels to prevent and control deposits in internal combustion engines are disclosed. The oxazolidines are derived from polyalkyl or polyalkenyl N-hydroxyalkyl succinimides and have the structural formula wherein: R is a polyakyl or polyalkenyl group having an average molecular weight ranging from 450 to 5000 daltons; m is an integer between 1 and 5; n is an integer between 0 and 1; and R1, R2, R3, and R4 are independent radicals, represented by the groups: —H, —CH2(CH2)AB, —C6H3DE or —C10H4FG; wherein: A is an integer between 0 and 8, B is a group selected among —H, —NH2, —OH, —COOH, and D, E, F, and G are independent radicals, selected among the groups: —H, —CH3, —CH2CH3, —CH2CH2CH3, —CH2(CH2)2CH3, —(CH3)3, C6H5, —NH2, —OH, —OCH3, OCH2CH2OH, OCH(CH3)CH2OH, OC6H5—COOH, and —SO3.

Abstract: Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.

Abstract: The present invention relates to a novel pyrrolidine compound having melanocortin receptor agonist activity or a pharmaceutically acceptable salt thereof, and to pharmaceutical applications thereof. The present invention relates to a pyrrolidine derivative represented by formula [I], wherein ring A represents an optionally substituted aryl group or the like; R1 represents an optionally substituted alkyl group or the like; R2 represents a halogen atom or the like; and R3 is an alkyl group substituted with an optionally substituted aryl group or the like, and R4 is a hydrogen atom or the like; or R3 and R4 are terminally attached to each other, and together with the nitrogen atom to which they are attached, form an optionally substituted nitrogen-containing aliphatic heterocyclic ring that may partially contain a double bond; or to a pharmaceutically acceptable salt thereof.

Abstract: Provided herein are compounds that bind to dCK and methods for treating cancer.

Abstract: The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-?B-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.

Abstract: The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-?B-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.

Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy); optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or -alkylaryl; R2 represents H; or alkyl; R3 represents H; or alkyl; U, V and W represent —(CH2)—; or U and V together represent —CH?CH— and W represents C?O; Y represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein opti

Abstract: The present invention relates to an improved process for preparing Idelalisib (1). In this process, acid addition salts of idelalisamine (2) are useful intermediates for purification purposes.

Abstract: The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.

Abstract: The present invention embodiments relate to a compound with formula (V?) The invention also relates in certain embodiments to the synthesis method for compound (V?) and its use for the preparation of 1,4,7-triazacyclononane (tacn) and N- and/or C-functionalized derivatives thereof, particularly compounds with formula (I) The invention also relates in certain embodiments to metallic complexes comprising a ligand with formula (I) and a metal and their use for imaging.

Abstract: Disclosed are substituted pyrrolo[2,3-d]pyrimidine compounds.

Abstract: The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R1 and R2 are as defined herein. The present invention also relates to compositions comprising at least one Imidazole Derivative, and methods of using the Imidazole Derivatives for inhibiting CYP450 3A. Inhibition of CYP450 3A can be used to improve the pharmacokinetics of a drug that is metabolized by CYP450 3A4.

Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein X is —C(?O) or —S(O)2—, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.

Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to the Compound for formula 1: having the name 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and tautomers thereof.

Abstract: Provided herein are N-hydroxy bicyclic hydantoin carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of serine hydrolases. Furthermore, the subject compounds and compositions are useful for the treatment of one or more of cancer, pain, diabetes, obesity/metabolic syndrome, epilepsy, traumatic brain injury, and inflammation.

Abstract: Presently provided are inhibitors of IDO and TDO and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase and 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; treating tumor-specific immunosuppression associated with cancer; and treating immunosuppression associated with an infectious disease.

Abstract: A method for treating prostate cancer in a subject, comprising administering a therapeutically effective amount of at least one agent to the subject, wherein the agent is selected from: (a) a phenyl-substituted imidazole, or a pharmaceutically acceptable salt or ester thereof; or (b) a compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; R21 is an alkanediyl or a substituted alkanediyl; a is 0 or 1; c is 0 or 1; X is C or S; R22 is a moiety that includes at least one divalent amino radical; and R23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing

Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.

Abstract: The invention concerns novel substituted bicyclic pyrazolo pyrimidine compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.

Abstract: The discovery of distinct modes of asymmetric catalysis has the potential to rapidly advance chemists' ability to build enantioenriched molecules. As an example, the use of chiral cation salts as phase-transfer catalysts for anionic reagents has enabled a vast set of enantioselective transformations. A largely overlooked analogous mechanism wherein a chiral anionic catalyst brings a cationic species into solution is itself a powerful method. The concept is broadly applicable to a number of different reaction pathways, including to the enantioselective fluorocyclization of olefins, and dearomatization of aromatic systems with a cationic electrophile-transferring (e.g., fluorinating) agent and a chiral phosphate catalyst. The reactions proceed in high yield and stereoselectivity. The compounds and methods of the invention are of particular value, especially considering the scarcity of alternative approaches.

Abstract: There is provided a novel process for the preparation of a compound of formula I, wherein R1, R2 and R3 are as described in the description, by conversion of a corresponding allylic alcohol.

Abstract: There is provided a novel process for the preparation of a hydrocodone salt. In particular, there is provided a novel process for the preparation of a free-flowing slurry of a hydrocodone salt, for example, a free-flowing slurry of hydrocodone bitartrate hemipentahydrate.

Abstract: Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

Abstract: Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.

Abstract: The invention relates to a multilayer superoleophobic and/or superhydrophobic material comprising: ? on the one hand, a first constituent that is a conductive substrate or a substrate that has previously been rendered conductive (1): ? the surface of which is modified by chemical and/or physical treatment (2) and that incorporates a first adhesion-promoting conductive layer (3); ? or that incorporates a first adhesion-promoting conductive layer (3); ? and, on the other hand, at least one other constituent that is a superoleophobic and/or superhydrophobic polymer or copolymer layer (4, 5 or 6) composed of one or more monomers based on an aromatic or heteroaromatic ring substituted by one or more fluorocarbon and/or hydrocarbon chains. It is characterized in that the various constituents of said material comply with an increasing hydrophobicity gradient between the first layer deposited on the conductive substrate or substrate previously rendered conductive (1) and the last layer of said material.

Abstract: The invention relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as PI-3 kinase.

Abstract: The present invention aims to provide a method for purifying cis-5-hydroxy-2-piperidinecarboxylic acid with high purity, and a method for producing its derivative. The present invention provides a method for producing a cis-5-hydroxy-2-piperidinecarboxylic acid derivative, which method comprises a step of converting cis-5-hydroxy-2-piperidinecarboxylic acid into a compound(s) of Formula (1) and/or Formula (2) (wherein R1 represents a protective group for an amino group, and R2 represents a C1-C6 alkyl group), and a method for purifying cis-5-hydroxy-2-piperidinecarboxylic acid.

Abstract: The present invention related to a process of preparation of pharmaceutically acceptable formulations containing as active substance 3-(4-cinnamy-1-piperazinyl)-amino derivatives of 3-formylrifamycine SV and 3-formylrifamycine S, which possess high activity against Gram-positive and Gram-negative microorganisms, as well as against tuberculous micobacteria (including atypical and rifamycin resistant), and to a method for the preparation of 3-(4-cinnamyl-1-piperazinyl)-amino derivatives of 3-formylrifamycine SV and 3-formylrifamycine S. The method for the preparation of pharmaceutical compositions is readily feasible, and does not require special equipment for its implementation. The process for preparing the compounds is characterized by high yield and purity, using an environmental clean solvent—ethanol and water in the preparation and isolation of substances, and the absence of residual organic solvents in the final product.

Abstract: The present invention relates to certain tetramic acid derivatives and, in particular, bicyclic tetramic acid derivatives that are suitable for use in the preparation and development of antimicrobial (e.g. antibacterial or antifungal) compositions. The present invention also relates to the use of such compounds as antimicrobial (e.g. antibacterial or antifungal agents) and, in particular, as topical antibacterial or antifungal agents.

Abstract: A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C1-C10 alkyl) or S; each X is independently CH or N; R1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R2 is LY; each L is a direct bond, C1-C10 alkylene, C2-C10 alkenylene or C2-C10 alkynylene; Y is an optionally substituted fused, bridged or spirocyclic non-aromatic 5-12 membered heterocycle containing up to 4 heteroatoms selected from N or O; and each R3 is independently H, C1-C10 alkyl, halogen, fluoro C1-C10 alkyl, O—C1-C10 alkyl, NH—C1-C10 alkyl, S—C1-C10 alkyl, O-fluoro C1-C10 alkyl, NH-acyl, NH—C(O)—NH—C1-C10 alkyl, C(O)—NH—C1-C10 alkyl, aryl or heteroaryl, are useful as inhibitors of the class IA phosphoinositide 3-kinase enzyme, PI3K-p110?, and therefore have potential utility in the therapy of cancer, immune and inflammatory diseases.

Abstract: Provided herein are novel polymorphic forms and co-crystals of a compound useful in the treatment, prevention, or amelioration of cancer. In particular, the invention provides polymorphs and co-crystals of 6-{(1R)-1-[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl}-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one, which is an inhibitor of c-Met.

Abstract: Macrocyclic compounds having the structure of Formula (A), or pharmaceutically acceptable salts thereof, are provided, wherein R1, R2, R3, R4 and R5 are defined herein. Also provided are pharmaceutical compositions comprising the macrocyclic compound and methods for treating cancer in a patient comprising administering to the patient the macrocyclic compound.

Abstract: The present disclosure provides dimers of melampomagnolide B (MMB), including carbamate, carbonate, succinic amide, ester and carboxamide dimers of MMB. These derivatives are useful for treating cancer in humans, in particular in treating leukemia, including acute myelogenous leukemia (AML). A compound comprising Formula (1) wherein: Z is independently selected from the group consisting of CH2, O, C(O), and CH, wherein when Z is CH, Z is connected to Y via a double bond and Y is N.

Abstract: Certain embodiments are directed to a composition comprising a complex of the general formula [M(crown ether)(solvent)n][arene??], wherein M is an alkali metal and method of making the same.

Abstract: A method of producing an alcohol, comprises reducing an aldehyde or a ketone with a hydridosilatrane. The reducing is carried out with an activator.

Abstract: Disclosed herein are a manufacturing method of a carbon-silicon composite, including: (a) preparing a slurry solution including silicon (Si)-block copolymer core-shell particles; (b) mixing the slurry solution with a carbon raw material to manufacture a mixed solution; (c) performing a primary carbonization process on the mixed solution, followed by pulverization, to manufacture a primary carbon-silicon composite; and (d) performing a secondary carbonization process on the primary carbon-silicon composite, followed by pulverization, to manufacture a secondary carbon-silicon composite, the carbon-silicon composite, an anode for a secondary battery manufactured by applying the carbon-silicon composite, and a secondary battery including the anode for a secondary battery.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.

Abstract: Azocarbonyl-functionalized silanes of formula I (R1)3-a(R2)aSi—R1—NH—C(O)—N?N—R4??(I) and methods for their production are provided. The silanes of formula (I) are useful in rubber mixtures to provide moldings having improved tear-resistance.

Abstract: Chemical linkage reagents, methods of making and method of using the same are provided. Chemical linkage reagents according to at least some of the embodiments of the present disclosure may be incorporated into or operatively-linked with affinity molecules for attachment to silicon oxide surfaces to, for example, measure interactions between an affinity molecule and its targeting biomolecules.

Abstract: The present invention provides water-soluble acetaminophen prodrugs and formulations which may be suitable for parenteral administration. Methods of treating a disease or condition responsive to acetaminophen (such as fever and/or pain) using the acetaminophen prodrugs, as well as kits, unit dosages, and combinations with additional pharmaceutical agent(s) are also provided.