Abstract: A [F-18]FEONM precursor is synthesized. 2-bromoethanol is added to further connect an atom of oxygen at an N terminal of the precursor. Four atoms of carbon can be further connected. Thus, better fat-solubility is obtained along with the increase in carbon. Positioning in brain imaging becomes better.

Abstract: This invention relates to novel precursors suitable for 18F radiolabeling of glutamate derivatives, methods for preparing such compounds and its intermediates, compositions comprising such compounds, kits comprising such compounds or compositions and methods for 18F radiolabeling of glutamate derivatives wherein the obtained 18F radiolabeled glutamate derivatives are suitable for diagnostic imaging by Positron Emission Tomography (PET) of proliferative diseases e.g. tumor in mammals.

Abstract: An actinic ray-sensitive or radiation-sensitive resin composition includes; a compound (A) which generates an acid by irradiation with actinic rays or radiation, wherein the acid is linked with a group represented by the following general formula (M) through covalent bonding. In the formula, Y1 and Y2 each independently represent a hydrogen atom, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aryl group, or an acyl group. Z represents a hydrogen atom or a substituent.

Abstract: This invention relates to novel precursors suitable for 18F radiolabeling of glutamate derivatives, methods for preparing such compounds and its intermediates, compositions comprising such compounds, kits comprising such compounds or compositions and methods for 18F radiolabeling of glutamate derivatives wherein the obtained 18F radiolabeled glutamate derivatives are suitable for diagnostic imaging by Positron Emission Tomography (PET) of proliferative diseases e.g. tumor in mammals.

Abstract: A catalytic process for the preparation of optically active compounds and their conversion thereafter to desired drug substances. In particular, the process relates to the preparation of (S)-3-(1-Dimethylamino-ethyl)-phenol using asymmetric catalytic reduction and transfer hydrogenation, thereby providing an improved route to forming drug substances such as rivastigimine and rivastigimine hydrogen tartrate.

Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.

Abstract: Methods for the synthesis and use of functionalized, substituted naphthalenes are described. The functionalized, substituted naphthalenes display useful properties including liquid crystals and fluorescence properties, such as solvatochromatic fluorescence, with high quantum yields, Stoke's shift, and show emission maxima that are significantly red-shifted.

Abstract: Embodiments of the invention provide methods and materials for chemical cross-coupling reactions that utilize unconventional phenol derivatives as cross-coupling partners. Embodiments of the invention can be used to synthesize a variety of useful organic compounds, for example the anti-inflammatory drug flurbiprofen.

Abstract: There are disclosed sulfonic acid precursor compositions, as are methods of using these compositions in, for example, photolithography. Other embodiments are also disclosed.

Abstract: Disclosed herein is an improved process for the preparation of 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol of Formula-I and its pharmaceutically acceptable salt which comprises the reaction of (S)-1-(dimethylamino)-2-methylpentan-3-one of formula VIII with 3-bromo anisole of formula II under Grignard conditions to get the compound (2S, 3R)-1-(dimethylamino)-3-(3-methoxyphenyl)-2-methyl pentan-3-ol of formula V followed by activation of the —OH group of the formula V to convert into sulfonate esters of formula IX, which are on reductive deoxygenation to yield (2R,3R)-3-(3-methoxyphenyl)-N,N,2-trimethylpentan-1-amine of formula VII and demethylation of formula VII to obtain the compound 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol of Formula-1.

Abstract: A sulfonic acid onium salt represented by the following formula (1) can be used as a superior radiosensitive acid generator for resist compositions. It is possible to form a good pattern by using a resist composition containing this sulfonic acid onium salt. In formula (1), R1 represents a monovalent organic group, and Q+ represents a sulfonium cation or iodonium cation.

Abstract: Disclosed herein are novel intermediates and process for large scale production of (S)-3-[(1-dimethylamino)ethyl]phenyl-N-ethyl-N-methyl-carbamate (rivastigmine) or its pharmaceutically acceptable salts employing the novel intermediates. Further provided are methods for producing the novel intermediates thereof.

Abstract: A catalytic process for the preparation of optically active compounds and their conversion thereafter to desired drug substances. In particular, the process relates to the preparation of (S)-3-(1-Dimethylamino-ethyl)-phenol using asymmetric catalytic reduction and transfer hydrogenation, thereby providing an improved route to forming drug substances such as rivastigimine and rivastigimine hydrogen tartrate.

Abstract: A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R—NH—CX—NH—(CH2)n—Ar-Q-SO2—NH2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n=0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.

Abstract: The present invention relates to the novel compound classes of dendritic polyglycerol sulfates and sultanates as well as to their production and use for the treatment of diseases, particularly inflammatory diseases, and to their use as selectin inhibitors and selectin indicators. The dendritic polyglycerol sulfates and sulfonates are also suitable for imaging diagnostics, particularly with respect to inflammatory diseases.

Abstract: A radioisotope labeled reagent includes a compound having the general formula (I), L-(aCbH2)naC5bH3??(I) where a in each occurrence independently is a carbon mass number between 11 and 14 inclusive, b in each occurrence independently is a hydrogen mass number between 1 and 3 inclusive, such that a in each occurrence is not 12 simultaneously with b in each occurrence being 1; L is a leaving group R1SO2—O—, R1—S—, 12C1H3(12C1H2)n—S—R1C(O)O—, NC—, (R1)3P—, XMg— and Li—, where n is an integer between 0 and 3 inclusive, where X is chloro, bromo or iodine, where R1 is H, aryl, a substituent containing aryl, C1-C20 alkyl, a substituent containing C1-C20 alkyl, C2-C20 alkenyl, a substituent containing C2-C20 alkenyl, C2-C20 alkynyl, and a substitute containing C2-C20 alkynyl with the proviso that when n is 0, a is 13 and b is 2 and R1 in R1—S is not aryl.

Abstract: The present invention provides novel and advantageous processes for preparing and purifying pharmaceuticals The processes comprise a nucleophilic reaction wherein a modified leaving group LM, which has increased lipophilicity, of a vector in a nucleophilic reaction which offers a convenient and time-saving way to purify the product from non-reacted precursors vector-LM and by-products LM.

Abstract: Rinsable dyes with improved fugitivity are formulated by attaching dyestuff compounds with amine-capped sulfonic solubilizing groups to commercially available ethoxylated aniline, so that the surfactant effect of the ethoxylated aniline counteracts the substantivity of the dyestuff compound, while the neutralization of the sulfonic solubilizing groups reduces substantivity.

Abstract: An oxime compound represented by the formula (I): wherein Y represents an unsubstituted or substituted n-valent C6-C14 aromatic hydrocarbon group, n represents an integer of 1 to 6, R1 represents a C1-C30 aliphatic hydrocarbon group etc., R2 represents a linear or branched chain C1-C20 aliphatic hydrocarbon group etc., W represents —CO—O— etc., Q1 and Q2 each independently represent a fluorine atom etc., Z represents a C1-C20 halogenated aliphatic hydrocarbon group etc, and the resist composition containing the same.

Abstract: Pantoic acid ester neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed.

Abstract: This invention relates to compounds of Formula (I), (II), or (III) as shown in the specification, which contain a 1,5-diphenylpenta-1,4-dien-3-one backbone. These compounds can be used to treat cancer, inflammatory disease, or autoimmune disease.

Abstract: Disclosed herein are novel intermediates and process for large scale production of (S)-3-[(1-dimethylamino)ethyl]phenyl-N-ethyl-N-methyl-carbamate (rivastigmine) or its pharmaceutically acceptable salts employing the novel intermediates. Further provided are methods for producing the novel intermediates thereof.

Abstract: A radioisotope labeled reagent includes a compound having the general formula (I), L-(aCbH2)naC5bH3??(I) where a in each occurrence independently is a carbon mass number between 11 and 14 inclusive, b in each occurrence independently is a hydrogen mass number between 1 and 3 inclusive, such that a in each occurrence is not 12 simultaneously with b in each occurrence being 1; L is a leaving group R1SO2—O—, R1—S—, 12C1H3(12C1H2)n—S—R1C(O)O—, NC—, (R1)3P—, XMg— and Li—, where n is an integer between 0 and 3 inclusive, where X is chloro, bromo or iodine, where R1 is H, aryl, a substituent containing aryl, C1-C20 alkyl, a substituent containing C1-C20 alkyl, C2-C20 alkenyl, a substituent containing C2-C20 alkenyl, C2-C20 alkynyl, and a substitute containing C2-C20 alkynyl with the proviso that when n is 0, a is 13 and b is 2 and R1 in R1—S is not aryl.

Abstract: A two-part disinfecting systems, as well as disinfecting compositions and methods for making and using the same. The two-part disinfecting system contains a first part and a second part adapted to be mixed to yield an aqueous disinfecting composition, wherein the first part comprises a chlorite and the second part comprises an acid, and wherein the first part, the second part, or both the first and second parts comprise an olefin compound.

Abstract: Methods of detecting at least one analyte and at least one nucleic acid in a sample are provided. Reagents for carrying out the methods are also provided.

Abstract: The invention relates to a compound represented by the following formula (I): and pharmaceutically acceptable salts, stereoisomers, enantiomers, prodrugs and solvates thereof. The compounds are useful as an agent for enhancing the neurite outgrowth and preventing or treating of diseases associated with HDAC in particular, tumor or cell proliferative diseases. In particular, the compounds of the invention can be used as an agent for anti-cancer, anti-diabetic, and anti-neurodegenerative diseases such as Alzheimer's disease, Huntington's disease, Spinocerebellar Ataxias (SCA), and human spinal muscular atrophy (SMA).

Abstract: The present invention relates to novel perfluorinated precursors for the production of F-18 labeled radiotracers for Positron Emission Tomography (PET) and processes for radiolabeling and purification using these precursors. The invention also comprises radiopharmaceutical kits using these precursors and processes.

Abstract: Segmented water soluble polymers, containing a higher molecular weight segment linked to a lower molecular weight segment, are described. In one embodiment, the polymer segments are poly(ethylene glycol) segments. The segmented polymers are functionalized and are useful for conjugation to various moieties such as pharmacologically active substances. Also described are conjugates of such polymers and methods of their preparation.

Abstract: Compounds represented by the following structural formulas can be used as photoacid generators: Such compounds are useful, for example, in fabricating arrays of polymers.

Abstract: This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, 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 methods of preparing compounds of formula (II) wherein Z represents —OR1 or N(R2)R2a—, where R1 is lower alkylene (C1-C6), R2 is lower alkyl or H and R2a is lower alkylene (C1-C6) or H; Q is absent when R2a is H and is otherwise selected from the group consisting of H, —OH and protected forms of —OH; one of X and Y is halogen and the other is —OSO2R3, where R3 is selected from the group consisting of lower alkyl (C1-C6), phenyl and CH2phenyl. The method comprises the steps of: (a) reacting a compound of formula (I) with aziridineethanol or a 2-[(2-haloethyl)amino]ethanol in the presence of a metal halide, to form a compound of the formula (III) wherein one of X and E is halogen and the other is hydroxy, and (b) reacting the compound of formula (III) with an alkyl- or arylsulfonyl halide or alkyl- or arylsulfonyl anhydride to obtain a compound of the formula (II).

Abstract: An oxime compound represented by the formula (I): wherein Y represents an unsubstituted or substituted n-valent C6-C14 aromatic hydrocarbon group, n represents an integer of 1 to 6, R1) represents a C1-C30 aliphatic hydrocarbon group etc., R2 represents a linear or branched chain C1-C20 aliphatic hydrocarbon group etc., W represents —CO—O— etc., Q1 and Q2 each independently represent a fluorine atom etc., Z represents a C1-C20 halogenated aliphatic hydrocarbon group etc, and the resist composition containing the same.

Abstract: The present invention relates to the use of end groups Y, where Y stands for CF3(CH2)aS— or CF3CF2S— or [CF3—(CH2)a]2N—, where a stands for an integer selected from the range from 0 to 5, as end group in surface-active compounds, to corresponding novel compounds, and to processes for the preparation of these compounds.

Abstract: This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, 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 present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.

Abstract: This invention relates to a method for producing compounds of formula (I) wherein R1 is a straight- or branched-chain C1-C24 alkyl, C2-C24-alkenyl or C1-C24-alkyl ether group or CH2CN or a group of the formula R2 and R3 are each individually a C1-C8-alkyl or C1-C4-hydroxyalkyl group. The method according to the invention is characterized by reacting a tertiary amine of the formula NR1R2R3 with chloroacetonitrile in an organic solvent and then adding an alkylating substance R11-Z, being C1-C4 alky.

Abstract: The invention provides novel aryl and aliphatic esters of fluorinated alkanesulfonic acids. The invention also provides novel fluorinated alkanesulfonamides and a process to make the same. The invention also provides a process for the arylation of an amine by contacting the amine with an aryl ester of a fluorinated alkanesulfonic acid.

Abstract: This invention relates to novel compounds F-18 radio-labeled amino-alcohols suitable for labeling or already labeled by 18F methods of preparing such a compound, 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: A sulfamate compound corresponding to Formula I wherein R1 to R3 and n have defined meanings, pharmaceutical compositions comprising these compounds; a process for preparing these compounds, and the use of such compounds or compositions to treat or inhibit various disorders or disease states in patients in need thereof by administering to such a patient a therapeutically effective amount of such a compound.

Abstract: The present application describes deuterium-enriched gabexate mesylate, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The invention provides surfactant compounds of formulas I-IX, which can be used in methods for aiding the solubilization, digestion, preparation, analysis, and/or characterization of biological material, for example, proteins or cell membranes. The compounds can also aid in the recovery of peptides generated during protein digestion, particularly for in-gel digestion protocol. Additionally, the compounds can improve enzymatic protein deglycosylation without interfering with downstream sample preparation steps and mass spectrometric analysis. The compounds can be specifically useful as digestion aids that can be decomposed by an acid, by heat, or a combination thereof. Decomposition of the surfactants allows for facile separation from isolated samples, and/or allows for analysis of the sample without interfering with the sensitivity of various analytical techniques.

Abstract: Compounds represented by the following structural formulas can be used as photoacid generators: Such compounds are useful, for example, in fabricating arrays of polymers.

Abstract: A method for sulfonating compounds having one or more free hydroxyl functional groups and/or one or more optionally substituted primary or secondary functional groups, including treating the compounds with a complex of SO3-DMF in the presence of an acid capture agent.

Abstract: Sulfonate salts have the formula: R1COOCH2CH2CF2CF2SO3?M+ wherein R1 is alkyl, aryl or hetero-aryl, M+ is a Li, Na, K, ammonium or tetramethylammonium ion. Onium salts, oxime sulfonates and sulfonyloxyimides derived from these salts are effective photoacid generators in chemically amplified resist compositions.

Abstract: The present invention provides a single pot process for the preparation of diazonaphthoquinonesulfonyl ester, a useful organic material for micro electronic and dye industry. This study pertains to the one pot preparation of diazonaphthoquinonesulfonyl esters using the corresponding diazonaphthoquinine sulfonic acid or its sodium salt, diphosgene or triphosgene, variety of hydroxy compounds and tertiary organic base in an organic solvent medium.

Abstract: This invention relates to 2-substituted D-homo-estra-1,3,5(10)-trien-3-yl sulfamates of general formula I (I), in which R3 means a C1-C5-alkyl or C1-C5-alkyloxy group as well as their use for the production of a pharmaceutical agent for treating tumor diseases, which can be influenced positively by the inhibition of tubulin polymerization. The compounds according to the invention are distinguished by a D-homosubstitution.

Abstract: The present invention is directed to a continuous process for the preparation of fructopyranose sulfamate derivatives of the general formula (I) wherein R1, R3, R4, R5, R6 and X are as herein defined. The present invention is further directed to a continuous process for the preparation of Topiramate.

Abstract: The present invention is directed to a one-step process for the preparation of fructopyranose sulfamate derivatives of the general formula (I) wherein X, R1, R3, R4, R5 and R6 are as described in the specification.

Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), or —OSO2(C2–C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), —OSO2(C2–C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is S— or —HC?CH—; and Y is O—, —S—, —NH—, —NMe—, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen

Abstract: This invention relates to 2-substituted D-homo-estra-1,3,5(10)-trien-3-yl sulfamates of general formula I (I), in which R3 means a C1-C5-alkyl or C1-C5-alkyloxy group as well as their use for the production of a pharmaceutical agent for treating tumor diseases, which can be influenced positively by the inhibition of tubulin polymerization. The compounds according to the invention are distinguished by a D-homo-substitution.