Abstract: Compounds having the general structure: which are effective antimicrobial agents.

Abstract: As discussed above, there remains a need for the development of novel therapeutic agents useful for treating inflammatory or autoimmune and proliferative diseases. The present invention provides novel compounds of general formula (I), and pharmaceutical compositions thereof, as described generally and in classes and subclasses herein, as well as methods of making and using such compounds.

Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.

Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.

Abstract: The invention relates to compounds having general formula (I), wherein R is as defined herein. The invention also relates to acid addition salt, a hydrate or a solvate of compounds of formula (I). The invention further relates to the method of preparing said compounds and to the use of same in therapeutics.

Abstract: Disclosed are compounds based on lactone ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.

Abstract: The invention relates to compounds of the formula I having antithrombotic activity, which in particular inhibit the protease-activated receptor 1 (PAR1), processes for their preparation and use thereof as medicaments.

Abstract: The present invention relates to the novel compounds Methyl 2-[(3S)-[3-[(2E)(7-chloro quinolin-2-yl)ethenyl]phenyl]-3-halopropyl]benzoates (IV) wherein the halo is chloro, bromo, iodo, starting from the known compound Methyl 2-[(3S)-[3-[(2E)-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-hydroxypropyl]benzoate (1). Reaction of Methyl 2-[(3S)-[3-[(2E)-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-hydroxypropyl]benzoate (1) with thionyl chloride or with methane sulfonyl chloride-lithium bromide or with trimethyl chlorosilane-sodium iodide in presence or absence of base gives Methyl 2-[(3S)-[3-[(2E)-(7-chloro quinolin-2-yl)ethenyl]phenyl]-3-halopropyl]benzoates.

Abstract: The present disclosure relates to imidazopyridine derivatives of formula (I): The present disclosure also relates to a method for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A2B adenosine receptor.

Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: 1.

Abstract: Disclosed is a method of making (?)-cocaine efficient for use on a large scale. The cocaine is created by reacting an aqueous solution of (+)-2-carbomethoxytropinone (2-CMT) bitartrate, sodium amalgam and an acid that forms a highly soluble sodium salt to form (?)-methylecgonine. (?)-Methylecgonine is converted into (?)-cocaine. Sodium amalgam is continuously supplied from an electrolyzing unit to a reactor containing the aqueous solution of (+)-2-carbomethoxytropinone bitartrate and spent amalgam is continuously removed and regenerated. The aqueous solution is prepared by adding (rac)-2-CMT in chloroform to a solution of (+)-tartaric acid in water to create an aqueous phase having diastereomeric salts of 2-CMT with (+)-tartaric acid. An organic solvent is added to the aqueous phase and the crystals obtained from the combined aqueous phase and organic solvent are dried to obtain substantially pure crystalline (+)-2-carbomethoxytropinone bitartrate.

Abstract: A phosphodiesterase 10A inhibitor serving as an effective prophylactic or therapeutic agent for Parkinson's disease, Huntington's disease, Alzheimer's disease, and schizophrenia. The PDE10A inhibitor contains as an active ingredient a pyrazolo[1,5-a]pyridine derivative represented by the following general formula: wherein R1 and R2 are each independently a hydrogen atom or a lower alkyl group having 1 to 4 carbons; and R3 is a hydrogen atom, a lower alkyl group having 1 to 4 carbons, or a lower alkoxyl group having 1 to 3 carbons.

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, B, R1, R2, R3, R4 and R5 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

Abstract: The invention relates to substituted pyrazolopyridines according to the general formula (I): in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted pyrazolopyridine compounds, to methods of preparing said substituted pyrazolopyridines, as well as to uses thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.

Abstract: The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases. A compound of the general formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X1?X2—X3?X4— is a formula of —C(R1)?C(R2)—C(R3)?N— etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is optionally substituted C1-C6 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is optionally substituted C1-C6 alkyl etc.; R9 is carboxy etc.; M is sulfonyl etc.; Y is a single bond etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.

Abstract: A process performs solid phase synthesis of halogenated derivatives of fluorescein, and includes reacting fluorescein with a halide MX, wherein M is an alkali metal and X is a halogen, and Oxone® (2 KHSO5.KHSO4.K2SO4), at a temperature higher than or equal to 150° C. A structure uses a halogenated derivative of fluorescein selected from the group consisting of 2?,4?,5?-trichlorofluorescein, 2?,4?,5?,7?-tetrachlorofluorescein, 4?,5?-diiodofluorescein diacetate and 2?,4?,5?-triiodofluorescein as electro-bistable material in a non-volatile memory device.

Abstract: Quinuclidine derivative of the general formula (I) in the form of single enantiomers or mixtures thereof are useful in the manufacture of a medicament for the prevention and therapy of respiratory diseases such as asthma, chronic obstructive pulmonary disease (COPD), chronic bronchitis, cough and emphysema wherein: R1 is selected from H, F, Cl, Br, I and (C1-C4)-alkyl; R2 is optionally substituted 2- or 3-thienyl, or substituted phenyl; R3 is (CH2)1-4—COR4 or (CH2)1-4—S(O)nR4, wherein R4 is optionally substituted phenyl or optionally substituted 2- or 3-thienyl; n is 0, 1 or 2; X? is a pharmaceutically acceptable anion.

Abstract: A method for producing a phenolphthalein compound is disclosed, comprising: reacting a phenolic compound of the formula: wherein Ra is a hydrogen or a C1-C12 hydrocarbyl group, with a phthalic anhydride compound of the formula: wherein Rb is a hydrogen, a C1-C12 hydrocarbyl group, or a halogen, in the presence of an ionic liquid catalyst composition and a promoter to form a reaction mixture comprising a phenolphthalein compound of the formula: wherein each Ra is independently a hydrogen or a C1-C12 hydrocarbyl group, and Rb is a hydrogen, a C1-C12 hydrocarbyl group, or a halogen; wherein the ionic liquid catalyst composition comprises a combination of an ionic liquid and a metal halide wherein the metal is selected from the group consisting of a Group IIB, IIIA, VIII, or IVA metal, and a combination thereof.

Abstract: Organic compounds having Formulas I and II are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier can be prepared. Methods of preparing the compounds includes deprotecting protected precursor compounds. Methods of treating cancer or inhibiting ATPase include administering the organic compounds to a subject in need thereof.

Abstract: The present invention relates to 7-azaindole-based compounds, to processes for the preparation thereof, to pharmaceutical compositions comprising them, and to the use thereof in the preparation of medicaments that are useful as inhibitors of MTP and of ApoB secretion.