Abstract: Methods and machinery are described for combining methane with sulfur trioxide to make MSA, in a system that sustains optimal concentrations of reactants in the main reactor for high yields, efficiency, and profitability. Rather than simply making MSA and then removing it, this design uses a “continuous loop system” with: (i) a “rich acid” stream containing a high concentration of MSA, mixed with sulfuric acid, which will emerge from the main reactor, and (ii) a “reduced acid” stream containing a low concentration of MSA (still mixed with sulfuric acid), from an extractor unit (such as a distillation unit) which removes some but not all of the MSA from the “rich acid”. Additional subassemblies are described which enable the main reactor to work efficiently, at a sustained high flow-through capacity. This system also can be scaled up or down, for any daily MSA production rate.

Abstract: The invention provides new processes for making and purifying amino acid compounds, which are useful in the preparation of AKT inhibitors used in the treatment of diseases such as cancer, including the compound (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.

Abstract: This invention relates to novel compounds suitable for labeling by 18F and to the corresponding 18F labeled compounds themselves, 19F-fluorinated analogues thereof and their use as reference standards, methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by Positron Emission Tomography (PET).

Abstract: The invention relates to the preparation of chiral compounds, in particular to the preparation of chiral compounds which may be used as intermediates for the preparation of anti-diabetic agents, preferably sitagliptin.

Abstract: The present invention relates to a compound of the following general formula (I): R1—NH—CH(R2)—P(?O)(OR3)—CH2—C(R4)(R5)—CONH—CH(R6)—COOR7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R1 represents a —C(?O)—O—C(R8)(R9)—OC(?O)—R10 group; R2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R3 represents a hydrogen atom or a —C(R12)(R13)—OC(?O)—R14 group; R4 and R5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R4 represents a hydrogen atom and R5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substi

Abstract: Crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid anhydrate and crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid hemihydrate, pharmaceutical compositions comprising such compounds, methods of making and methods of using the same are disclosed.

Abstract: The present invention relates to an improved method for manufacturing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention allows reduction of production costs by reacting low cost reagents, improves yield and is adaptable for mass production.

Abstract: Crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid anhydrate and crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid hemihydrate, pharmaceutical compositions comprising such compounds, methods of making and methods of using the same are disclosed.

Abstract: The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as oral anti-diabetic drug. Starting from L-aspartic acid derivate of formula IV the invention describes preparation of the chiral (R)-?-amino acid of formula II known as a precursor in the synthesis of Sitagliptin (formula I).

Abstract: There is provided a process for producing an amide compound having an excellent harmful arthropod-controlling activity and represented by the formula (3): wherein R1, R2 and R3 independently represent a C1-C6 alkyl group optionally substituted with at least one halogen atom etc., R4, R5, R6 and R7 independently represent a halogen atom etc.

Abstract: Crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid anhydrate and crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid hemihydrate, pharmaceutical compositions comprising such compounds, methods of making and methods of using the same are disclosed.

Abstract: The present invention relates to a process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine of formula I: where: A is aryl or heteroaryl, where the aryl is preferably a phenyl, optionally substituted, selected from benzyl and tolyl and the heteroaryl is preferably thiophenyl; Y is an aryl, preferably phenyl, a substituted phenyl or a naphthyl, where the substituted phenyl is preferably selected from tolyl, trihalomethyltolyl and alkoxytolyl, starting from a suitable amino alcohol of formula II:

Abstract: The present disclosure relates to methods of synthesizing 1-(acyloxy)-alkyl carbamate prodrugs and to intermediates used in the methods.

Abstract: The present invention is an improved method for the preparation of 4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester, compound of formula I. The invention is directed to a method of synthesis for the compound of formula I in three steps, comprising formation of 5-((tert-butoxycarbonyl)aminomethyl)-2-fluorobenzeneboronic acid (compound 11), reaction of compound 11 under Suzuki coupling conditions to yield (4-fluoro-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester and selective hydrogenation of the aforementioned product under hydrogenation conditions yields compound I. The invention is also directed to the intermediates 5-((tert-butoxycarbonyl)amino-methyl)-2-fluorobenzeneboronic acid (compound 11), and (4-fluoro-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester (compound 13).

Abstract: Urethane acrylates of the general Formula (I), corresponding salts, solvates or solvates of a salt thereof: wherein R1, R2, R3, R4 and R5 each independently represent a substituent selected from the group consisting of hydrogen, halogens, C1-6-alkyls, trifluoromethyl, C1-6-alkylthios, C1-6-alkylselenos, C1-6-alkyltelluros, and nitro groups, with the proviso that at least one of R1, R2, R3, R4 and R5 is not hydrogen; R6 and R7 each independently represent a substituent selected from the group consisting of hydrogen and C1-6-alkyls; and A represents a saturated or unsaturated or linear or branched C1-6-alkyl radical or a polyalkylene oxide radical having 2-6 ethylene oxide or propylene oxide units; processes for producing and methods of using the same.

Abstract: Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.

Abstract: The present invention relates to Sitagliptin intermediate and preparation method and use thereof. The method comprises reacting compound of formula (II) and trifluorobromobenzene with a Grignard reagent by a Grignard reaction to obtain a compound of formula (I). Compound of formula (I) is a new intermediate compound for the synthesis of Sitagliptin. Compound of formula (I) can be easily used for preparing another important intermediate compound of formula (V) for the synthesis of Sitagliptin.

Abstract: The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as oral anti-diabetic drug. Starting from L-aspartic acid derivate of formula IV the invention describes preparation of the chiral (R)-?-amino acid of formula II known as a precursor in the synthesis of Sitagliptin (formula I).

Abstract: Disclosed is a method for preparing a compound of Formula 1 by contacting compound of Formula 2 with R1—NH2 in the presence of a carboxylic acid and a method for preparing a compound of Formula 2 by contacting a compound of Formula 4 with phosphorus tribromide. wherein R1 is H, C1-C4 alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R2 is CH3 or Cl; R3 is C1-C6 alkyl or C3-C6 alkenyl, each optionally substituted with up to 3 halogen and up to 1 phenyl; and X is Cl or Br. Also disclosed is a method for preparing a compound of Formula 5 wherein R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 that is characterized by preparing the compound of Formula 1 by the method above.

Abstract: The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield.

Abstract: The present invention relates to an improved method for manufacturing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention allows reduction of production costs by reacting low cost reagents, improves yield and is adaptable for mass production.

Abstract: Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

Abstract: The invention relates to the field of antibiotic compositions, both inside and outside the medical field. Presented is a new class of antibiotic compounds around the lead compound (3,4-dichloro-phenyl)-carbamic acid 2-isobutoxycarbonylamino-1-methyl-ethyl ester, which are especially useful for combating infections with gram-positive bacteria and especially MRSA.

Abstract: The present invention provides a method for producing an optically active N-(halopropyl)amino acid derivative, wherein the method comprises the steps of obtaining a compound represented by formula (III) by reacting an optically active alanine ester represented by formula (I) or a salt thereof (hereinafter sometimes simply referred to as an “alanine ester”) with a halogenated propane represented by formula (II); and obtaining an optically active N-(halopropyl)amino acid derivative represented by formula (IV) by introducing a protecting group onto the nitrogen atom of the compound represented by formula (III). The present invention provides a method for efficiently producing an optically active N-(halopropyl)amino acid derivative.

Abstract: What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.

Abstract: Compounds of Formula I are useful in the treatment of epilepsy, neuropathic pain, acute and chronic inflammatory pain, migraine, tardive dyskinesia and other related CNS disorders. wherein: A and R1 to R8 are defined in the specification.

Abstract: The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

Abstract: Disclosed herein is a novel functional diamine compound having a dendron structure, polyamic acid which is produced using functional diamine, aromatic cyclic diamine, aliphatic cyclic acid dianhydride, and aromatic cyclic acid dianhydride, polyimide which is produced by imidizing polyamic acid, and an LC alignment film produced using polyimide. Even if the diamine compound is used in a small amount, it is possible to realize a high pretilt angle, thus the pretilt angle is easily controlled. Therefore, it can be used to produce an LC alignment film using a twisted nematic (TN) mode, in which the pretilt angle of liquid crystal is low, and a vertically aligned (VA) mode, which requires a high pretilt angle of about 90°.

Abstract: The present invention relates to a process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine of formula I: where: A is aryl or heteroaryl, where the aryl is preferably a phenyl, optionally substituted, selected from benzyl and tolyl and the heteroaryl is preferably thiophenyl; Y is an aryl, preferably phenyl, a substituted phenyl or a naphthyl, where the substituted phenyl is preferably selected from tolyl, trihalomethyltolyl and alkoxytolyl, starting from a suitable amino alcohol of formula II:

Abstract: Disclosed are intermediates and processes for preparing epoxides of the formula: where R and PROT are defined herein. These epoxides are useful as intermediates in the production of biologically active compounds, i.e., in the production of pharmaceutical agents.

Abstract: The present disclosure relates to methods of synthesizing 1-(acyloxy)-alkyl carbamate prodrugs and to intermediates used in the methods.

Abstract: Urethane acrylates of the general Formula (I), corresponding salts, solvates or solvates of a salt thereof: wherein R1, R2, R3, R4 and R5 each independently represent a substituent selected from the group consisting of hydrogen, halogens, C1-6-alkyls, trifluoromethyl, C1-6-alkylthios, C1-6-alkylselenos, C1-6-alkyltelluros, and nitro groups, with the proviso that at least one of R1, R2, R3, R4 and R5 is not hydrogen; R6 and R7 each independently represent a substituent selected from the group consisting of hydrogen and C1-6-alkyls; and A represents a saturated or unsaturated or linear or branched C1-6-alkyl radical or a polyalkylene oxide radical having 2-6 ethylene oxide or propylene oxide units; processes for producing and methods of using the same.

Abstract: The present invention is directed to novel alkylated aromatic compositions, zeolite catalyst compositions and processes for making the same. The catalyst compositions comprise zeolite Y and mordenite zeolite having a controlled macropore structure. The present invention is also directed to the preparation of the catalyst compositions and their use in the preparation of novel alkylated aromatic compositions. The catalyst compositions of the present invention exhibit reduced deactivation rates during the alkylation process, thereby increasing the life of the catalysts.

Abstract: The present invention is directed to a zeolite Y catalyst having a controlled macropore structure. The present invention is also directed to a zeolite Y catalyst composite and a process for preparing the catalyst composite. The catalyst composite exhibits reduced deactivation rates during the alkylation process, thereby increasing the life of the catalyst. The present invention is also directed to processes for the preparation of carbonated, overbased aromatic sulfonates, which processes comprise alkylation, carbonation of aromatic hydrocarbons with one or more olefins.

Abstract: The present invention is directed to a zeolite Y catalyst having a controlled macropore structure. The present invention is also directed to a zeolite Y catalyst composite and a process for preparing the catalyst composite. The catalyst composite exhibits reduced deactivation rates during the alkylation process, thereby increasing the life of the catalyst. The present invention is also directed to processes for the preparation of carbonated, overbased aromatic sulfonates, which processes comprise alkylation, carbonation of aromatic hydrocarbons with one or more olefins.

Abstract: A readily available and inexpensive natural ?-amino acid is converted into a compound represented by formula (1), which is then reacted with an organometallic reagent represented by formula (2) to give an optically active 5-hydroxyoxazolidine represented by formula (3), which is then treated with an acid to provide an optically active aminoketone represented by formula (4). The product is then converted into an optically active aminoalcohol represented by formula (5) or (6) by, for example reduction.

Abstract: Compounds of formula (I) or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of disorders using the compounds are disclosed.

Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.

Abstract: Derivatives of C2-substituted indan-1-ol compounds of formula I: its physiologically acceptable salts, and its physiologically functional derivatives for the prophylaxis or treatment of obesity are disclosed herein. Compositions comprising the same, methods for preparing the instant compounds, and methods for reducing weight in mammals and for the prophylaxis or treatment of obesity are also described.

Abstract: A family of substituted chiral allosteric effectors of hemoglobin is useful for delivering more oxygen to hypoxic and ischemic tissues by reducing the oxygen affinity of hemoglobin in whole blood.

Abstract: New thyroid receptor ligands are provided which have the general formula I: wherein R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C3-7 cycloalkyl; R2 and R3 are each independently hydrogen, halogen, substituted or unsubstituted C1-4 alkyl, or substituted or unsubstituted C3-6 cycloalkyl, wherein at least one of R2 and R3 is other than hydrogen; R4 is a carboxylic acid selected from the group consisting of (CH2)nCOOH, (CH)2COOH, NHCO(CH2)nCOOH, CONH(CH2)nCOOH and NH(CH2)mCOOH; n is an integer from 0 to 4; and m is an integer from 1 to 4. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

Abstract: Polysubstituted indan-1-ol compounds of formula I, its physiologically acceptable salts and physiologically functional derivatives are disclosed Compositions comprising the same, methods of preparation and methods for the prophylaxis or treatment of obesity are also disclosed herein.

Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.

Abstract: The invention relates to the compounds of general formula (I), that are present with respect to R1 as racemates as well as L- or D-configured compounds and as E/Z mixtures as well as E or Z isomers and in which the various symbols are defined as in the description and the claims, as well as to the salts thereof, for use as therapeutic agents and for diagnostic purposes. The inventive compounds can be processed to medicaments or to diagnostic agents that are used for the diagnosis, therapy and prevention of urokinase- or urokinase-receptor associated diseases, for example for the treatment of tumors. The compounds are highly efficient in inhibiting growth and/or spread of malign tumors, for example tumor spread of pancreatic cancer, tumor growth of breast cancer and the formation of tumor metastases. The compounds of formula (I) and the salts thereof can be produced by conventional methods.

Abstract: The present invention relates to an uracil compound of the formula [I]: wherein W represents oxygen, sulfur, imino or C1 to C3 alkylimino; Y represents oxygen, sulfur, imino or C1 to C3 alkylimino; R1 represents C1 to C3 alkyl or C1 to C3 haloalkyl; R2 represents C1 to C3 alkyl; R4 represents hydrogen or methyl; R5 represents C1 to C6 alkyl, C1 to C6 haloalkyl, or the like; X1 represents halogen, cyano or nitro; X2 represents hydrogen or halogen; and each of X3 and X4 independently represents hydrogen, halogen, C1 to C6 alkyl, or the like. The present compound has an excellent herbicidal activity.

Abstract: Compounds and pharmaceutical compositions useful as plasminogen activator inhibitor (PAI) antagonists are provided. In particular, methods of antagonizing PAI with substituted and unsubstituted aryl and heteroaryl ethers and thioethers are provided.

Abstract: Biarylalkylenecarbamic acid derivative represented by general formula (I): [wherein Q is a phenyl group which may be substituted or the like, X is a halogen atom, a (C1-C6) alkyl group or the like, n is 0 or an integer of from 1 to 4, R1 is a (C1-C6) alkyl group or the like, R2 is a hydrogen atom, a (C1-C6) alkyl group or the like, A is a (C1-C7) alkylene group which may be branched, and G is an oxygen atom, a sulfur atom or a group —NR— (wherein R3 is a hydrogen atom or a (C1-C4) alkyl group)] and agricultural and horticultural fungicides. The agricultural and horticultural fungicides of the present invention are useful as agricultural and horticultural fungicides because they have high preventive effects on cucumber downy mildew, apple scab, wheat powdery mildew, rice blast, cucumber gray mold and rice sheath blight without damaging crops, and are excellent in residual effectiveness and rain-resistance.

Abstract: The present invention relates to a novel blocked phenylenediamine developer useful, in reactive association, for enabling, on development, a non-magenta color, for example a cyan color, from a dye-forming coupler. In one embodiment, the developer has the property that the dye color formed with the coupler is distinctly different from the color formed by the same coupler with an oxidized form of the conventional developer 4-(N-ethyl-N-2-hydroxyethyl)-2-methylphenylenediamine. The invention is also directed to a light-sensitive silver-halide color photographic element comprising the blocked developing agent according to the present invention.

Abstract: A family of substituted chiral allosteric effectors of hemoglobin is useful for delivering more oxygen to hypoxic and ischemic tissues by reducing the oxygen affinity of hemoglobin in whole blood.

Abstract: Compounds of formula (I) wherein R1 is C1-C4-alkyl or cyclopropyl; R2 is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkinyl; or C1-C6-alkyl substituted by 1 to 5 fluorine atoms; R3 is C1-C6-alkyl, C1-C6-alkoxy, C3-C6-cycloalkyl, C3-C6-cycloalkoxy, C2-C6-alkenyl, C2-C6-alkenyloxy, C2-C6-alkinyl, C2-C6-alkinyloxy, C1-C6-alkoxycarbonyl, CN, or aryl, heteroaryl, heterocyclyl, aryloxy, heteroaryloxy or heterocyclyloxy, whereby the above-mentioned groups may be substituted by identical of different substituents, R5 signifies hydrogen or methyl; R6 and R7 are C1-C4-alkyl; have microbicidal, insecticidal and acaricidal activity and may be used for the control of pests and plant-pathogenic fungi in agriculture, horticulture and in the field of hygiene.