Abstract: The object is to prevent deterioration and loss of dicyanobenzene in producing dicyanobenzene by ammoxidation of xylene to thereby achieve industrial and economical advantage in producing of dicyanobenzene.

Abstract: The present invention refers to new solid forms of Enclomiphene citrate and Enclomiphene base, processes for preparing thereof and uses.

Abstract: Provided herein are methods of making the compound of Formula I: and certain intermediates involved in such process.

Abstract: This invention relates to novel benzazepine dicarboxamide compounds of the formula wherein R1 to R4 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, graft rejection, graft-versus-host disease, immunodeficiencies, and infectious diseases.

Abstract: New tranilast complexes and new tranilast cocrystals are disclosed. These include a 1:1 tranilast nicotinamide complex, a 1:1 tranilast nicotinamide cocrystal, a 1:1 tranilast saccharin complex, a 1:1 tranilast saccharin cocrystal, a 1:1 tranilast gentisic acid complex, a 1:1 tranilast gentisic acid cocrystal, a 1:1 tranilast salicylic acid complex, a 1:1 tranilast salicylic acid cocrystal, a 1:1 tranilast urea complex, a 1:1 tranilast urea cocrystal, a 1:1 tranilast 4-aminobenzoic acid complex, a 1:1 tranilast 4-aminobenzoic acid cocrystal, a 1:1 tranilast 2,4-dihydroxybenzoic acid complex and a 1:1 tranilast 2,4-dihydroxybenzoic acid cocrystal. Also disclosed are pharmaceutical compositions containing a tranilast complex or cocrystal of the invention and a pharmaceutically acceptable carrier. Methods of treatment using the tranilast complexes and cocrystals as well as the pharmaceutical compositions are disclosed.

Abstract: The present invention relates to a process for purifying adiponitrile (ADN), wherein crude ADN is introduced into a rectification apparatus (R1). The rectification apparatus (R1) comprises a first side draw and preferably also a second side draw, the first side draw being disposed below the crude ADN introduction point and the optional second side draw being disposed above the crude ADN introduction point. The first side draw is used to draw off a gaseous stream comprising ADN while the optional second side draw is used to draw off undesired by-products such as 1-amino-2-cyanocyclopentene (ACCP) which are often generated in ADN production and consequently may be present in the crude ADN. The gaseous stream from the first side draw of (R1) is introduced into a second rectification apparatus (R2). (R2) is used to separate off ADN from remaining high boilers and any other by-products present, pure ADN being drawn off from (D2) as overhead product.

Abstract: Described herein, inter alia, are compositions and methods useful for inhibiting fatty acid amide hydrolase.

Abstract: Provided is a compound having a formyl peptide receptor like 1 (FPRL1) agonist effect. The present invention relates to a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing the compound represented by the general formula (I) or a pharmacologically acceptable salt thereof.

Abstract: A method for the manufacture of a 2-hydrocarbyl-3,3-bis(hydroxyaryl)phthalimidine composition comprises: reacting a phthalimide with a phenol in the presence of a catalyst and optionally a solvent at an elevated temperature to form the 2-hydrocarbyl-3,3-bis(hydroxyaryl)phthalimidine composition.

Abstract: The present invention is in the field of pharmaceuticals and chemical industries. In particular, the present invention relates to new anticancer miliusane lactam compounds. The present invention also includes its preparation and application method for treating cancer.

Abstract: Disclosed are a variety of amphoteric compounds having a heterocyclic quaternary nitrogen group. The heterocycle includes pyridines, piperidines, and pyrrolidines, and is linked to the hydrophobe via either an amide or an ester linkage. These heterocyclic amphoteric compounds can be advantageously prepared in high yield and purity by a two-step chemoenzymatic process, and have excellent surfactant properties.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.

Abstract: Prodrugs of an NMDA antagonist, (S)-1-phenyl-2-(pyridin-2-yl)ethanamine, useful for the treatment of depression (particularly major depressive disorder) or pain; compositions comprising them, and methods of making them.

Abstract: There is provided a compound of formula VIIa, wherein Qx represents —C(O)O—C1-4 alkyl, or a salt or protected derivative thereof, and other compounds that are useful in the preparation of compounds that have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Abstract: 4-Amino-5-fluoro-3-chloro-6-(substituted)picolinates are prepared from trifluoroacetic acid, p-methoxyaniline, a 3,3-dialkoxyprop-1-yne and a substituted methylene amine by a series of steps.

Abstract: The present invention relates to quinoline compounds as defined by Formula I below. Such quinoline compounds have been shown to inhibit the formation of amyloid deposits (e.g., amyloid oligomers, fibrils or plaques). Consequently, these compounds are suitable for treating a range of diseases and disorders in which amyloid deposits are implicated, such as type-2 diabetes and Alzheimer's disease.

Abstract: The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.

Abstract: Provided herein are N?,N?,N?-trialkyl histidine derivative compounds and methods of their preparation. Also provided are methods of their use for preparing useful compounds such as ergothioneine.

Abstract: Chemical entities based on quinoxaline that are kinase inhibitors are described. Specifically quinoxaline derivatives of Formula I, containing a diarylamide or diarylurea substructure that inhibit Braf mutant kinase activity, pharmaceutical compositions containing the inhibitor compounds and methods of treatment of cancer comprising administering an effective amount of the Braf inhibitor compound are described.

Abstract: The present invention relates to diaminotriazine compounds of the formula (I) and to their use as herbicides. The present invention also relates to agrochemical compositions for crop protection and to a method for controlling unwanted vegetation. wherein A is phenyl, which is substituted by fluorine in the ortho-position and which may additionally carry 1, 2, 3 or 4 identical or different substituents RA; R1, R2 are inter alia H, OH, S(O)2NH2, CN, C1-C6-alkyl, C2-C6-alkenyl, etc.

Abstract: The invention relates to amphiphilic derivatives of a triazamacrocyclic compound, as well as to said derivatives as active molecule transporters. The invention also relates to a nanodrug including at least one amphiphilic derivative of a triazamacrocyclic compound and at least one active molecule of a protein such as an antibody, in particular for the treatment of autoimmune diseases or for the treatment of cancer.

Abstract: Disclosed is a novel method of preparing highly pure calcobutrol using an intermediate (butrol) of gadobutrol without using highly pure gadobutrol. This method is capable of obtaining calcobutrol at high purity and high yield through a simple and environmentally friendly process, and thus can be easily applied to mass production.

Abstract: A tetrazolinone compound represented by formula (1): [in the formula, R1 represents an alkyl group having 1-6 carbon atoms or the like] can be produced by reacting a compound represented by formula (2): [in the formula, X1 represents a bromine atom or the like, and R1 represents an alkyl group having 1-6 carbon atoms or the like] with a compound represented by formula (A): R—Mg—X??(A) [in the formula, R represents an alkyl group having 1-6 carbon atoms or the like, and X1 represents a bromine atom or the like] to provide a compound represented by formula (3): [in the formula, X2 represents a chlorine atom or the like] and reacting the compound represented by formula (3) with formaldehyde or a compound represented by formula (4): [in the formula, R6 represents an alkyl group having 1-6 carbon atoms or the like, and X3 represents a chlorine atom, bromine atom or iodine atom].

Abstract: The invention relates to an improved process for the preparation of pharmaceutical active ingredients and also to high purity salts and pharmaceutical compositions prepared by said process. More particularly the invention relates to an economical process for the preparation of the compound having the international non-proprietary name (INN) vortioxetine and the chemical nomenclature 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine. Vortioxetine corresponds to the following Formula Still more particularly the invention relates to the preparation of high purity vortioxetine L-(+)-mandelate salt of the Formula IX, the conversion of this salt into other highly pure salts and also to the formulation of said salts.

Abstract: There is provided a manufacturing assembly for the production of an alkylene oxide and a stream of glycol ethers. The manufacturing assembly produces the alkylene oxide and stream of glycol without the use of equipment for separating substantially all of the alkyl alcohol from the alkylene oxide product stream. Thus, the use of additional pieces of equipment can be avoided, or the equipment required to effectuate any required further separation and/or purification may be smaller and/or cheaper to purchase and/or operate.

Abstract: Copoly(imide oxetane) materials are disclosed that can exhibit a low surface energy while possessing the mechanical, thermal, chemical and optical properties associated with polyimides. The copoly(imide oxetane)s are prepared using a minor amount of fluorinated oxetane-derived oligomer with sufficient fluorine-containing segments of the copoly(imide oxetane)s that migrate to the exterior surface of the polymeric material to yield low surface energies. Thus the coatings and articles of manufacture made with the copoly(imide oxetane)s of this invention are characterized as having an anisotropic fluorine composition. The low surface energies can be achieved with very low content of fluorinated oxetane-derived oligomer. The copolymers of this invention can enhance the viability of polyimides for many applications and may be acceptable where homopolyimide materials have been unacceptable.

Abstract: The present invention relates to the field of natural pharmaceutical chemistry, and in particular, to a resveratrol dimer (7R,8R)-trans-?-viniferin (I), a preparation process therefor and a purpose thereof in lowering a blood sugar level. According to the present invention, an R type of resveratrol dimer is separated from the resveratrol dimer by using high-speed countercurrent chromatography. Pharmacodynamic tests proved that the R type of resveratrol dimer has a better effect in lowering a blood sugar level than a racemate.

Abstract: The invention relates to a process for producing Nebivolol hydrochloride, (formula I) comprising the steps of: provision of a protected Nebivolol hydrochloride of the general formula (II), with P being an amine protecting group, and hydrogenation of said protected Nebivolol hydrochloride yielding Nebivolol hydrochloride of the formula (I).

Abstract: Provided is a production method for an ellagic acid composition excellent in solubility in water. The production method for an ellagic acid composition includes the steps of: mixing an aqueous medium with a raw material which contains a guava leaf extract and which contains, in solids thereof, 1 to 5% by mass of free ellagic acid to prepare a material for heat treatment; and subjecting the material for heat treatment to heat treatment at from 100 to 180° C.

Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

Abstract: The present invention provides new processes for the preparation of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds which are useful, for example, for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-?. The invention can provide improved and/or efficient processes for the commercial production of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds, including, but not limited to, unsubstituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione.

Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

Abstract: A tetrazolinone compound represented by formula (1): wherein R1 and R2 each independently represents a hydrogen atom, a C1-C4 alkyl group optionally having one or more halogen atoms, etc.; R3 represents a hydrogen atom, a C1-C4 alkyl group optionally having one or more halogen atoms, etc.; R4 represents a halogen atom, a C1-C4 alkyl group optionally having one or more halogen atoms, etc.; h represents any one of integers of 0 to 4; X represents a nitrogen atom or CR5; and R5 represents a hydrogen atom, a halogen atom, etc.; has excellent control activity against pests.

Abstract: A compound of formula I wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), age-related cognitive decline, dementia, and Parkinson's disease.

Abstract: The present invention provides modulators of protein function, to restore protein homeostasis, including cytokine, aiolos, and/or ikaros activity, and cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions, including in combination with other cytokine and inflammatory mediators, are provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions, such as cytokine-mediated diseases, disorders, and conditions, including inflammation, fibromyalgia, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, inflammatory bowel diseases, Crohn's disease, ulcerative colitis, uveitis, inflammatory lung diseases, chronic obstructive pulmonary disease, Alzheimer's disease, and cancer, are provided.

Abstract: The present invention relates to novel triazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.

Abstract: The compounds of the invention are antagonists of MDM2 and MDMX, with excellent specificity for MDM2 and MDMX over other proteins, and with selective binding affinity to MDMX over MDM2. The compounds can therefore regulate p53 activity and treat a variety of cancers. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: This invention relates to pyrazole compounds or pharmaceutically acceptable salts thereof. Compounds of this invention are inhibitors of methionine aminopeptidase 2 (MetAP2) and dipeptidyl peptidase-4 (DPP-4). MetAP2 is a metalloproteinase that cleaves initiator methionine from nascent peptide emerging from the ribosomes. WO 2010/065879 reports small molecule MetAP2 inhibitors for obesity treatment. DPP-4 inhibitors are an established drug class to improve glycemic control in patients with type 2 diabetes mellitus. Compounds with dual inhibitory activity in both MetAP2 and DPP-4 are desired. The present invention provides novel compounds with dual MetAP2 and DPP-4 inhibitition. These dual inhibitor compounds can be useful in the treatment of a MetAP2 and DPP-4 mediated condition. The present invention provides a compound of the following Formula (I); or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

Abstract: There are disclosed compounds that are inhibitors of EZH2, pharmaceutical compositions containing said compounds and methods of treating hyperproliferative, inflammatory, infectious, and immunoregulatory disorders and diseases utilizing the compounds of the invention.

Abstract: Disclosed are taxifolin derivative with superior antioxidant effect, a method of synthesizing the same and a cosmetic composition containing the same. In accordance with the method, taxifolin derivatives having higher antioxidant activity than taxifolin can be synthesized using lipoic acid. As such, a novel taxifolin derivative synthesized according to the present invention can exhibit anti-aging effects when used for cosmetics and the like.

Abstract: The present invention relates to diaminotriazine compounds and to their use as herbicides. The present invention also relates to agrochemical compositions for crop protection and to a method for controlling unwanted vegetation. wherein A is a fused saturated or unsaturated, 5-, 6-membered carbocycle or a fused saturated or unsaturated, 5-, 6-membered heterocycle; P is 1 or 2 q is 0, 1, 2 or 3; Rb is inter alia halogen, OH, CN, amino, NO2, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C2-C6-alkenyloxy, C2-C6-alkynyloxy, etc.; R1 is inter alia H, OH, S(O)2NH2, CN, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, (C3-C6-cycloalkyl)-C1-C4-alkyl, C1-C6-alkoxy, etc.

Abstract: The present invention is directed to compounds encompassed by the Formula (I), pharmaceutical compositions thereof, methods for inhibiting LTA-4 hydrolase, and methods for the treatment of a disease and disorder which is ameliorated by the inhibition of LTA4-h activity. Non-limiting examples of such diseases and conditions include inflammatory and autoimmune diseases and disorders.

Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring B, and the subscript r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).

Abstract: The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a substituted bicyclic heteroaromatic ring compound of formula I: wherein two of X1 to X8 are N and the remaining of X1 to X8 are CH; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof.

Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.

Abstract: Provided is a sulfonamide derivative represented by the following general formula (1) and having an ?4 integrin inhibitory effect with high selectivity with a low effect on ?4?1 and a high effect on ?4?7, or a pharmaceutically acceptable salt thereof (in the general formula (1), A, B, D, E, R41, and a to h are as described in the description).

Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating ATM kinase mediated disease, including cancer, using such compounds and salts.

Abstract: Benzodiazepine dimers having a structure represented by wherein X comprises a heteroaromatic moiety and is as further defined in the application; R1 is and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).