Abstract: A method is provided for N-alkylation of acridine compounds by reduction of acridines to corresponding acridans to improve the reactivity of the acridine nitrogen, and subsequent N-alkylation of the acridans in ionic liquid solvents to provide the corresponding acridinium compounds in high yield. This inventive process improves chemical conversion, and does not require the use of highly toxic alkylating agents, such as 1,3-propane sultone.

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: formula (I): wherein A is selected from the group consisting of: formula (II) and wherein Z is selected from the group consisting of: formula (III): and. are useful as HIV attachment inhibitors.

Abstract: [Problem] to provide an aromatic imide compound wherein the sensitivity for visible light such as g-line, h-line etc. is increased and solubility is also improved. [Means for solving problem] The aromatic imide compound of the invention is a compound represented by the formula (1) below (in the formula, R1 represents a haloalkyl group having 1 to 7 carbon atoms or a haloaryl group, R2 represents a group containing a substituted or unsubstituted, aliphatic or aromatic group which may have a heteroatom, and adjacent R2s may form an imido group by connecting each other, R3 represent a halogen atom or a hydrocarbon group, m is zero or an integer of 1 or more, n is zero or an integer of 1 or more, and a sum of n and m is 1 to 6). These compounds are obtained by following processes. A halogenated naphtharic anhydride is reacted with an aromatic group-containing hydrocarbon such as ethynylbenzene to prepare a naphthalic anhydride substituted by an aromatic group-containing group.

Abstract: Described herein are methods of preparing 6-hydroxy N-alkyl morphinan-6-ols from morphinan-6-ones, as illustrated below: wherein the variables R1, R2, R3, R10, R11, R14, and are as defined herein and wherein the reactions occur in a one-pot procedure using a boron based reducing agent.

Abstract: The invention concerns a spiro-amino compound of Formula (I), wherein A is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring containing 1 to 3 nitrogen atom; X is a substituent selected from the group consisting of (C1-C3)alkyl and halogen, Y is a substituent selected from the group consisting of halogen and trifluoromethyl or a pharmaceutically acceptable salt thereof for use in the treatment of pathologies which require an antagonist of the NK1 receptor.

Abstract: The present invention relates to a compound of general formula (I) in which: —R1 and R2 are simultaneously or independently H, OH, OCH3 or a C1-C5 alkyl radical, —R3 and R4 are simultaneously CH3, —or R3 is H and R4 is CH3, CH2CH3 or an isopropyl radical or a phenyl radical, —R5 is a C4-C24 alkyl radical or a 3-phenylpropanyl or 2,2-diphenylethanyl radical.

Abstract: The present invention provides compounds of Formula (I): (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.

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

Abstract: The present invention relates to a compound represented by the following formula (1): wherein W, X, Y, R1, R2, R33, R34, m and n are as defined in the claims, or a pharmacologically acceptable salt thereof.

Abstract: The present invention provides novel imidazole analogs of Formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

Abstract: The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.

Abstract: Novel alpha-hydrogen substituted nitroxyl compounds and their corresponding oxidized (oxoammonium cations) and reduced (hydroxylamine) forms, and the use of such compounds, inter alia, for oxidation of primary and secondary alcohols to aldehydes and ketones, respectively; resolution of racemic alcohols; desymmetrization of meso-alcohol; as radicals and spin trapping reagents; and as polymerization agents. Processes for preparing the novel nitroxyl/oxoammonium/hydroxylamine compounds from the corresponding amines, and certain novel amine derivatives and their uses. The compounds and amine precursors are useful as ligands for transition metals and as organocatalysts in e.g., aldol reactions.

Abstract: A method for producing a high-purity nitrogen-containing heterocyclic compound includes: a process (a) and a process (b): (a) a process of mixing a mixture containing a compound and as an impurity compound with a solvent and a metal salt, and (b) a process of obtaining a mixture in a solution state in which the content of the compound has decreased compared to that in the mixture in the process (a) by filtering a mixed solution obtained in the process (a), or a process of obtaining a mixture in which the content of the compound has decreased compared to that in the mixture in the process (a) by further evaporating the solvent or crystallizing following the filtering; (where R1 and R2 are each independently a hydrogen atom, a C1-6 alkyl group, etc., R3 is a hydrogen atom, a C1-6 alkyl group, etc., X is a hydrogen atom, etc.).

Abstract: The present invention is directed to tricyclic compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5 and R6 are as described herein, compositions including the compounds and methods of using the compounds.

Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.

Abstract: Present invention relates to methods for preparing (1?, 2?, 4?, 5?, 7?)-7-[(hydroxidi-2-thienllacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane-bromide.

Abstract: It relates to spirocyclic compounds of formula (I), or pharmaceutically or veterinary acceptable salts thereof, or any stereoisomers either of the compounds of formula (I) or of their pharmaceutically or veterinary acceptable salts, wherein A and B form a spirocyclic ring system wherein the spiro atom connecting A and B is a carbon atom and wherein A is a known 3- to 8-membered carbocyclic or heterocyclic monocyclic ring or a known 6- to 18-membered carbocyclic or heterocyclic polycyclic ring system; B is a known 4- to 7-membered carbocyclic or heterocyclic monocyclic ring; C is phenyl or a known 5- to 6-membered heteroaromatic ring; and R1-R7 are as defined herein. It also relates to a process for their preparation, as well as to the intermediates used in this process; to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular as antifibrinolytic and antihemorragic agents.

Abstract: Present invention refers to new compounds of formula I or II, its synthesis and its use in the treatment of metabolic syndrome, particularly for the treatment of type I or type II diabetes and/or metabolic syndrome or metabolic disease or metabolic disorders.

Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.