Abstract: The present invention discloses organocatalytic process for asymmetric synthesis of highly enantioselective decanolide compounds in high yield with >99% ee. Further, the present invention disclose cost effective, improved organocatalytic process for asymmetric synthesis of highly enantioselective decanolides compounds from non-chiral, cheap, easily available raw materials.

Abstract: The present disclosure generally relates to methods of preparing nicotine and resolving R,S nicotine to enrich the (S)(?) enantiomer. The method may comprise combining N-methyl-2-pyrrolidone or a salt thereof with a nicotinate compound in the presence of a solvent and a strong base to form 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof; and reducing the 1-methyl-3-nicotinoyl-2-pyrrolidone or salt thereof in solution with Na2S2O4 to produce racemic nicotine or salt thereof. Resolving the racemic nicotine (or other enantiomeric mixture) may comprise combining the nicotine with (?)-O,O?-di-p-toluoyl-L-tartaric acid (L-PTTA).

Abstract: The present invention is directed to substituted indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

Abstract: The present invention provides a method of efficiently producing an optically active 6-(3-aminopiperidin-1-yl)-2,4-dioxo -1,2,3,4-tetrahydropyrimidine derivative. The optically active piperidine-3-carboxamide or a derivative thereof, which is obtained by subjecting 1,4,5,6-tetrahydropyridine -3-carboxamide or a derivative thereof to an asymmetric reduction in the presence of a catalyst, is used as an intermediate.

Abstract: 3-(3-chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine-•dihydrochloride with a dialkyl maleate to provide an alkyl 5-oxo-2-(pyridin-3-yl)pyrazolidine-3-carboxylate, by chlorinating to provide an alkyl 3-chloro-1-(pyridin-3-yl)-4,5-dihydro-1H-pyrazole-5-carboxylate, by oxidizing to provide an alkyl 3-chloro-1-(pyridin-3-yl)-1H-pyrazole-5-carboxylate, by converting the ester to the carboxylic acid by hydrolysis to provide 3-chloro-1-(pyridin-3-yl)-1H-pyrazole-5-carboxylic acid hydrochloride, and by removing the carboxylic acid by a decarboxylation reaction.

Abstract: Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

Abstract: Deuterated diaminopyrimidine compounds and pharmaceutical compositions containing such compounds are described. In particular, disclosed are deuterated diaminopyrimidine compounds of formula (I), and pharmaceutical compositions containing such compounds or crystal forms, pharmaceutically acceptable salt, hydrates or solvates thereof. The disclosed deuterated diaminopyrimidine compounds can be used for treating and/or preventing protein kinase-associated diseases, such as cell proliferative disease, cancer, immune disease and the like.

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.

Abstract: Compounds of formula (I): wherein Het, R3, R4, R5, R7, R8, R9, T, p, p?, q, and q? are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.

Abstract: Benzimidazoles of formula (I): wherein: A is 5- to 12-membered aryl or 5- to 12-membered heteroaryl, each of which is unsubstituted or substituted; Y is a single bond, —(CH2)p—, —X—, —CH2—X—, or —X—CH2—; X is —O—, —S—, —N(R2)—, >C?O, >S(?O), >S(?O)2, —O—C(?O)—, —C(?O)—O—, N(R2)—C(?O)—, or —C(?O)—N(R2)—; each L is independently a single bond, C1-3alkylene, C2-3alkenylene or C2-3alkynylene; R1 is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, each of which is unsubstituted or substituted; each Z is independently —N(R2)2, —OR2, —SR2, —S(?O)R2, —S(?O)2R2; each R2 is independently hydrogen, C1-6alkyl, C2-6alkenyl or C2-6 alkynyl, wherein said alkyl, alkenyl and alkynyl groups are unsubstituted or substituted; m is 0, 1, 2, or 3; n is 1, 2, or 3; and p is 1, 2, or 3; and the pharmaceutically acceptable salt thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.

Abstract: The invention provides methods of synthesizing a viral protease inhibitor in high yield, without using expensive catalysts or challenging reaction conditions.

Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.

Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.

Abstract: Provided herein are substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.

Abstract: The present invention relates to the technical field of medicine, and specifically relates to the carboxylic acid compound represented by the chemical formula I or chemical formula II, and a pharmaceutically acceptable salt, a prodrug, and a solvate thereof, and a method for preparation thereof, as well as a pharmaceutical composition containing the described substances, and a use thereof.

Abstract: Compounds are provided as inhibitors of CXCR2, having the structure:

Abstract: Compounds of formula (I) are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.

Abstract: Provided are novel selective androgen receptor agonists, a preparation method thereof, and a pharmaceutical composition including the same at a pharmaceutically effective amount. The selective androgen receptor agonists according to the present invention act on androgen receptors to increase androgen activity, thereby being usefully applied as a therapeutic and prophylactic agent for diseases or conditions, of which symptoms may be improved or may respond to treatment by increased activities of androgen receptors, namely, a variety of hormone-related diseases in male and female, muscle wasting disorders, osteoporosis, etc.

Abstract: A synthesis method of a sulfur-containing oxazine compound is provided. First, an oxazine compound as a precursor and an elemental sulfur as a feedstock are provided. Then, the elemental sulfur reacts with the oxazine compound directly to form a sulfur-containing oxazine compound.

Abstract: A fluorinated 2-arylbenzo heterocyclic compound with high affinity to A? plaques and containing a chiral side chain substituent, has a general formula (I) as follows: wherein X is N; Y is S or O; Z is N or CH; R1 is a 5 or 6-substituent and is F is 19F or 18F; R2 is NHCH3 or N(CH3)2. The compound of the present invention has high affinity to A? plaques and can be used to make appropriate radioactive nuclide labeling probes for early diagnosis of AD.

Abstract: Biheteroaryl dicarboxylates and esters, and salts thereof which are useful as modulators of CP4H activity and more particularly as inhibitors of CP4H. Compounds of formula: and salts thereof where: X is S, O, NH, or NR, where R is an alkyl group having 1-3 carbon atoms; R1 and R2 independently are —OR7, or —NHSO2R8, where R7 is selected from: hydrogen, alkyl, alkenyl, alkoxyalkyl, —R?—CO—R?, —R?—CO—O—R?, —CO—R?, —R?—O—CO—R?, —R?—CO—NR?, —CO—NR?, or —R?—O—CO—NR?, and R8 is selected from hydrogen, alkyl, aryl, arylalkyl; R3, R4 and R6 independently are hydrogen, alkyl, alkoxy, alkenyl, alkenoxy, haloalkyl, haloalkenyl, halogen, hydroxyl, hydroxyalkyl, hydroxyalkenyl, aryl, aryloxy, arylalkyl or arylalkyloxy; R5 is hydrogen, halogen, alkyl having 1-3 carbon atoms, or alkoxy having 1-3 carbon atoms; —R?— is a divalent straight chain or branched alkylene, and —R? is an alkyl, alkenyl, arylalkyl, or aryl group. Methods for inhibition of CP4H in vivo and in vitro.

Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.

Abstract: Disclosed herein are compounds and compositions useful in the treatment of GLS1 mediated diseases, such as cancer, having the structure of Formula I: Methods of inhibition GLS1 activity in a human or animal subject are also provided.

Abstract: The present invention belongs to the technical field of medicines, and relates to a crystal form of a compound used as a mineralocorticoid receptor antagonist and a preparation method therefor, and in particular, to a method for preparing a compound 2-chloro-4-[(3S,3aR)-3-cyclopentyl-7-(4-hydroxypiperidin-1-carbonyl)-3,3a,4,5-tetrahydro-2H-pyrazolo[3,4-f]quinolin-2-yl]benzonitrile of formula (1); a crystal form thereof, a preparation method for the crystal form, and the use of the crystal form in the preparation of drugs for the treatment and/or prevention of renal injury or cardiovascular diseases.

Abstract: Compounds useful in the treatment of fibrosis, bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, pain and burns in a mammal.

Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.

Abstract: The present invention provides a compound of the Formula (I) below: Wherein R1 is selected from the group consisting of H, CH3, CN, CH2CN, C(CH3)2CN, and F; R2 is selected from the group consisting of H, O(C1-C3alkyl)R5, CH2CN, and CN; R3 is selected from the group consisting of H, OCH3, CN, C(CH3)2CN, and CH2CN; R4 is selected from the group consisting of H and CH3; R5 is selected from the group consisting of H, CN, C(CH3)2CN, OCH3, S(O)2CH3, and C(CH3)2OH; provided that at least one selected from the group consisting of R1, R2, R3 and R4 is H; or a pharmaceutically acceptable salt thereof, methods of treating diabetes using the compound and a process for preparing the compound.

Abstract: Use of a tetramic acid compound according to formula (I) or (I?) with a second nematicide as a treatment for crop plants to combat and control nematodes in the soil of said crop plants.

Abstract: Non-fullerene electron acceptors for highly efficient organic photovoltaic devices are described. The non-fullerene electron acceptors have an extended, rigid, ?-conjugated electron-deficient framework that can facilitate exciton and charge derealization. The non-fullerene electron acceptors can physically mix with a donor polymer and facilitate improved electron transport. The non-fullerene electron acceptors can be incorporated into organic electronic devices, such as photovoltaic cells.

Abstract: The present invention relates to a method for screening a compound that inhibits secretion of toxins into host-cell cytoplasm by virulent bacteria using a needle type III secretion system. The compound of the invention is selected by screening for a compound which interacts with a loop region of the cytoplasmic domain of the membrane protein FlhB from Salmonella typhimurium or a paralog thereof. Compositions including the compound of the invention, use of the compound, and methods of treating disorders caused by virulent bacteria are also provided.

Abstract: The invention discloses a method for preparations of fluoro, chloro and fluorochloro alkylated compounds by homogeneous Pd catalyzed fluoro, chloro and fluorochloro alkylation with fluoro, chloro and fluorochloroalkyl halides in the presence of di(1-adamantyl)-adamantyl-n-butylphosphine and in the presence of 2,2,6,6-tetramethylpiperdine 1-oxyl.

Abstract: Compositions and methods for modulating innate and adaptive immunity and for use in immunotherapy are disclosed. In particular, the invention relates to novel ganciclovir derivatives and methods of using them for the treatment of immune-related disorders, including inflammation, autoimmunity, and infections, and neurological disorders, and cancer.

Abstract: Compounds of the formula I in which W, X and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.

Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: The material for forming an underlayer film for lithography of the present invention contains a compound having a structure represented by the following general formula (1). (in formula (1), each X independently represents an oxygen atom or a sulfur atom, R1 represents a single bond or a 2n-valent hydrocarbon group having 1 to 30 carbon atoms, the hydrocarbon group may have a cyclic hydrocarbon group, a double bond, a hetero atom or an aromatic group having 6 to 30 carbon atoms, R2 represents a linear, branched or cyclic alkyl group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, an alkenyl group having 2 to 10 carbon atoms, or a hydroxyl group, m is an integer of 0 to 3, n is an integer of 1 to 4, p is 0 or 1, and q is an integer of 1 to 100.).

Abstract: The present invention relates to small molecule compounds and their use in the treatment of diseases, in particular viral diseases, in particular hepatitis C virus (HCV).

Abstract: The invention provides deuterium-enriched isoindolinonyl-piperidinonyl conjugates, deuterium-enriched oxoquinazolin-3(4H)-yl-piperidinonyl conjugates, pharmaceutical compositions, and methods of using such conjugates and pharmaceutical compositions to treat cancer, angiogenesis disorders, immune disorders, and other medical disorders.

Abstract: The present invention discloses a novel DGAT1 inhibitor, especially the compound of formula (I) or a pharmaceutically acceptable salt thereof, preparation and pharmaceutical composition thereof, as well as their uses in the preparation of a medicament for the prevention and treatment of Familial hyperchylomicronemia (FCS), obesity, hyperlipoproteinemia or hypertriglyceridemia.

Abstract: Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.

Abstract: A non-hydroxylic-solvent soluble silver complex comprises a reducible silver ion complexed with an ?-oxy carboxylate and a 5- or 6-membered N-heteroaromatic compound. The non-hydroxylic-solvent soluble silver complex can be represented by the following formula (I): (Ag+)a(L)b(P)c?? (I) wherein L represents the ?-oxy carboxylate; P represents the 5- or 6-membered N-heteroaromatic compound; a is 1 or 2; b is 1 or 2; and c is 1, 2, 3, or 4, provided that when a is 1, b is 1, and when a is 2, b is 2. Such complexes can be incorporated into photosensitive compositions for thin films or patterns in various articles to provide electrically-conductive silver metal.

Abstract: The present invention describes chemical systems and methods for silylating aromatic organic substrates, said system or method comprising or consisting essentially of a mixture of (a) at least one organosilane and (b) at least one strong base, the definition of strong base now also including KOH, said system being preferably, but not necessarily substantially free of a transition-metal compound, and said methods comprising contacting a quantity of the organic substrate with a mixture of (a) at least one organosilane and (b) at least one strong base, under conditions sufficient to silylate the aromatic substrate.

Abstract: Provided are a novel cyclodisilazane derivative, a method for preparing the same, and a silicon-containing thin film using the same, wherein the cyclodisilazane derivative having thermal stability, high volatility, and high reactivity and being present in a liquid state at room temperature and under a pressure where handling is easy, may form a high purity silicon-containing thin film having excellent physical and electrical properties by various deposition methods.

Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.

Abstract: The present invention provides a compound of Formula I: wherein X, Y, Z, R1 and R2 are as described herein, and salts thereof and therapeutic uses of these compounds for treatment of disorders associated with RAF kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.

Abstract: Novel bidentate ligands of general formula (I) are described. In formula (I), A and B each independently represent a linking group; and R represents a hydrocarbyl aromatic structure. The substituent(s) Yi on the aromatic structure together have a total number ?ti of atoms other than hydrogen such that ?ti is greater than or equal to 4, wherein ti represents the number of atoms other than hydrogen on a particular substituent Yi. i ranges from 1 to n; and n is the total number of substituent(s) Yi. The groups X1, X2, X3 and X4 are joined via tertiary carbon atoms to the respective atom Q2 or Q1. Q1 and Q2 each independently represent phosphorus, arsenic, or antimony. A catalyst system and a process for the carbonylation of ethylenically unsaturated compounds utilizing the catalyst system are also described.

Abstract: The invention relates to a method and kits for isolating and/or purifying nucleic acids, in particular, short-chain nucleic acids, from a nucleic acid containing starting material, characterized by the following method steps: (a) bonding the nucleic acids to a nucleic acid bonding support material, wherein the starting material is brought into contact with the nucleic acid bonding support material in the presence of at least one chaotropic compound and preferably isopropanol, wherein the isopropanol is present in a concentration of ?15% (v/v) and ?35% (v/v), (b) optional elution of the bonded nucleic acids from the nucleic acid bonding support material. Said method is particularly suitable for the purification of foetal DNA from maternal blood.

Abstract: Methods and compositions for processing biomass using [Co(CN)5]3? are disclosed. The resulting products include monomeric carbohydrate units that can also be converted to basic alcohols, including ethanol, for a variety of uses including transportation fuels and the generation of electricity.

Abstract: Cells incorporating a synthetic molecule construct of the structure F—S1—S2-L where: F—S1 is an aminoalkylglycoside where F is a mono-, di-, tri- or oligo-saccharide and S1 is 2-aminoethyl, 3-aminopropyl, 4-aminobutyl, or 5-aminopentyl; S2 is —CO(CH2)2CO—, —CO(CH2)3CO—, —CO(CH2)4CO— or —CO(CH2)5CO—; and L is phosphatidylethanolamine.

Abstract: Compositions and methods related to anti-cancer terpenoid compounds isolated from plants in the Salviniaceae family, pharmaceutical compositions comprising the same, and methods of treating cancer.