Abstract: Disclosed herein are compounds of formula (I) and therapeutic methods of treatment with compounds of formula (I), wherein L1, L2, L4, R1, R4, R5, R6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, neuropathic pain, and related disorders.

Abstract: Disclosed herein are compounds of formula (I) and therapeutic methods of treatment with compounds of formula (I), wherein L1, L2, L4, R1, R4, R5, R6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, neuropathic pain, and related disorders.

Abstract: This invention is in the fields of immunology and autoimmunity. More particularly it concerns pharmaceutical compositions comprising compounds which are useful agents for inhibiting the functions of TIP60 and the use of such compounds in the treatment of an individual suffering, for example, from ulcerative colitis and other irritable bowel diseases.

Abstract: The invention provides compositions and methods for reducing healing wounds and reducing scars and blemishes. The compositions and methods of the invention include at least one EP4 agonist set forth herein. Wounds and or scars that can be treated by the compositions and methods of the invention can arise from events such as surgery, trauma, disease, mechanical injury, burn, radiation, poisoning, and the like.

Abstract: Disclosed herein are compounds of formula (I) and therapeutic methods of treatment with compounds of formula (I), wherein L1, L2, L4, R1, R4, R5, R6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, neuropathic pain, and related disorders.

Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.

Abstract: A method for producing N-vinyl-2-pyrrolidone by crystallization including: controlling a water content in a feed N-vinyl-2-pyrrolidone solution at an inlet of a crystallizer so as to be not lower than 0.7% by weight and not higher than 10% by weight based on the total weight of the N-vinyl-2-pyrrolidone solution; and supplying the feed N-vinyl-2-pyrrolidone solution to a crystallization process.

Abstract: The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a tautomer or salt thereof, where R1-R5, a, b, X and P2, are as defined in the specification.

Abstract: The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a g-amino-d-biphenyl-a-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.

Abstract: The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo,

Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.

Abstract: The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, —CH?N—, —CH?CH— or —N?CH—; A is CH2, O or S; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the physiologically tolerated acid addition salts

Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.

Abstract: The present invention relates to a method for preparing lactams using heterogeneous catalysis by hydrogenating at least one compound of the following formula (I), where A is a radical of the following formula (I?) or (II?): —CH(R1)—CH(R2)— (I?); or —CH(R1)—CH(R2)—CH(R3)— (II?); where R1, R2 and R3 are, independently from each other, H, OH, an alkyl radical, or a cycloalkyl radical; and R is H or a straight or branched alkyl radical having 1 to 20, preferably 1 to 10, and more preferably 1 to 4 carbon atoms. Said method is carried out at a pressure of less than 60 bars, preferably 10 to 50 bars, in the presence of a solid hydrogenation catalyst including at least two metals selected from the group of noble metals and transition metals, and an inert substance used as a support, wherein said compound of formula (I) can be used alone or as part of a mixture.

Abstract: The present invention relates to optically enriched or substantially optically pure 4-substituted-pyrrolidin-2-ones of formula (III), and their uses for the synthesis of 2-oxo-pyrrolidin-1-yl derivatives.

Abstract: The invention relates to compounds of formula (I): where A1, A2, A3, A4, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.

Abstract: Arylpyrrolidines of formula (I): wherein each substituent is as defined in the specification, and use thereof as pesticides and animal parasite-controlling agents.

Abstract: Methods and systems are provided for converting methane in a feed stream to acetylene. The method includes removing at least a portion of acids from a hydrocarbon stream. The hydrocarbon stream is introduced into a supersonic reactor and pyrolyzed to convert at least a portion of the methane to acetylene. The reactor effluent stream may be treated to convert acetylene to another hydrocarbon process. The method according to certain aspects includes controlling the level of acids in the hydrocarbon stream by use of adsorbents or basic solutions.

Abstract: This invention relates to a process for preparing 2-pyrrolidone (also called 2-pyrrolidinone) and N-methylpyrrolidone (also called N-methylpyrrolidinone) from diammonium succinate in fermentation broth. In the first stage of this invention, renewable carbon resources are utilized to produce diammonium succinate through biological fermentation. In the second stage of this present invention, diammonium succinate is converted into 2-pyrrolidone and N-methylpyrrolidone through a two step reaction. Both the steps of the reaction leading to the production of 2-pyrrolidone and N-methylpyrrolidone are carried out in a solvent phase to prevent the loss of succinimide through hydrolysis.

Abstract: A method of eradicating weeds by applying to the weeds a compound derived from 3-acetyl-5-sec-butyl-4-hydroxy-3-pyrrolin-2-one.

Abstract: This invention relates to novel heterocyclic compounds that are useful for treating cancer and other cellular proliferative diseases and/or disorders associated with B-Raf activity. The compounds of the invention may be illustrated by the Formula (I).

Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.

Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.

Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.

Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.

Abstract: The present invention relates to a mixture comprising itaconic acid or an itaconic acid derivative and a primary amine of the formula (I) R—NH2??(I) where the molar ratio of primary amine to itaconic acid or the itaconic acid derivative is in the range from 0.5:1 to 20:1, wherein the mixture comprises 50 mole percent or less of 4-carboxypyrrolidones of the formula (II), derivatives of the 4-carboxypyrrolidones of the formula (II) and 4-carbamidopyrrolidones of the formula (III) based on the itaconic acid used or the itaconic acid derivative used and in which R is a linear or branched saturated aliphatic radical having 1 to 24 carbon atoms or a saturated cycloaliphatic radical having 3 to 24 carbon atoms. The invention further provides for the use of the inventive mixtures for preparing 1,3-alkylmethylpyrrolidones and/or 1,4-alkylmethylpyrrolidones, and also a process for preparing 1,3-alkylmethylpyrrolidones and/or 1,4-alkylmethylpyrrolidones.

Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.

Abstract: This application describes compounds useful as anti-microbial agents, including as antibacterial, disinfectant, antifungal, germicidal or antiviral agents.

Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.

Abstract: This application describes compounds useful as anti-microbial agents, including as antibacterial, disinfectant, antifungal, germicidal or antiviral agents.

Abstract: Methods and systems are provided for converting methane in a feed stream to acetylene. The method includes removing at least a portion of heavy hydrocarbon compounds including C2+ hydrocarbons from a hydrocarbon stream. The hydrocarbon stream is introduced into a supersonic reactor and pyrolyzed to convert at least a portion of the methane to acetylene. The reactor effluent stream may be treated to convert acetylene to another hydrocarbon process. The method according to certain aspects includes controlling the level heavy hydrocarbons in the hydrocarbon stream by use of adsorbents, physical separators or cryogenic separation.

Abstract: Methods and systems are provided for converting methane in a feed stream to acetylene. The method includes removing at least a portion of organic oxygenates from a hydrocarbon stream. The hydrocarbon stream is introduced into a supersonic reactor and pyrolyzed to convert at least a portion of the methane to acetylene. The reactor effluent stream may be treated to convert acetylene to another hydrocarbon process. The method according to certain aspects includes controlling the level of organic oxygenates in the hydrocarbon stream.

Abstract: Methods and systems are provided for converting methane in a feed stream to acetylene. The hydrocarbon stream is introduced into a supersonic reactor and pyrolyzed to convert at least a portion of the methane to acetylene. The reactor effluent stream may be treated to convert acetylene to another hydrocarbon process. The method according to certain aspects includes controlling the level of water, carbon dioxide and other condensable contaminants in the hydrocarbon stream by use of a fluid separation assembly such as a supersonic inertia separator. In addition, one or more adsorbent beds may be used to remove remaining trace amounts of condensable contaminants. The fluid separation assembly has a cyclonic fluid separator with a tubular throat portion arranged between a converging fluid inlet section and a diverging fluid outlet section and a swirl creating device.

Abstract: Methods and systems are provided for converting methane in a feed stream to acetylene. The method includes removing at least a portion of mercury from a hydrocarbon stream. The hydrocarbon stream is introduced into a supersonic reactor and pyrolyzed to convert at least a portion of the methane to acetylene. The reactor effluent stream may be treated to convert acetylene to another hydrocarbon process. The method according to certain aspects includes controlling the level of mercury and mercury containing compounds in the hydrocarbon stream.

Abstract: Methods and systems are provided for converting methane in a feed stream to acetylene. The method includes removing at least a portion of acids from a hydrocarbon stream. The hydrocarbon stream is introduced into a supersonic reactor and pyrolyzed to convert at least a portion of the methane to acetylene. The reactor effluent stream may be treated to convert acetylene to another hydrocarbon process. The method according to certain aspects includes controlling the level of acids in the hydrocarbon stream by use of adsorbents or basic solutions.

Abstract: Provided herein is a non-naturally occurring microbial organism having a methanol metabolic pathway that can enhance the availability of reducing equivalents in the presence of methanol. Such reducing equivalents can be used to increase the product yield of organic compounds produced by the microbial organism, such as 1,4-butanediol (BDO). Also provided herein are methods for using such an organism to produce BDO.

Abstract: Methods and systems are provided for converting methane in a feed stream to acetylene. The method includes removing at least a portion of solids from a hydrocarbon stream. The hydrocarbon stream is introduced into a supersonic reactor and pyrolyzed to convert at least a portion of the methane to acetylene. The reactor effluent stream may be treated to convert acetylene to another hydrocarbon process. The method according to certain aspects includes controlling the level of inorganic and organic solids in the hydrocarbon stream by use of adsorbent beds, filters, cyclone or gravity separators.

Abstract: Methods and systems are provided for converting methane in a feed stream to acetylene. The method includes removing at least a portion of heavy metals from a hydrocarbon stream. The hydrocarbon stream is introduced into a supersonic reactor and pyrolyzed to convert at least a portion of the methane to acetylene. The reactor effluent stream may be treated to convert acetylene to another hydrocarbon process. The method according to certain aspects includes controlling the level of heavy metals in the hydrocarbon stream.

Abstract: Arylpyrrolidines of Formula (I): wherein each substituent is as defined in the specification, and use thereof as pesticides and animal paracite-controlling agents.

Abstract: New compounds and pharmaceutical compositions comprising active ingredients having inhibition effects on osteoclast differentiation are provided. The pharmaceutical compositions comprising the new compounds can be used as medicines for treating metabolic bone diseases such as bone metastatic cancer, solid cancer bone metastasis, musculoskeletal complication by solid cancer bone metastasis, hypercalcemia by malignant tumor, multiple myeloma, primary bone tumor, osteoporosis, rheumatoid arthritis, osteoarthritis, periodontal disease, inflammatory resorption of alveolar bone, inflammatory resorption of bone, and Paget's disease.

Abstract: The present invention provides a process for preparing a bicyclic amine derivative of the formula (Ia) or (Ib), comprising the rhodium-catalyzed asymmetric hydrogenation of an enamine of the formula (II), in the presence of a chiral ligand, wherein the chiral ligand is a chiral phosphine ligand.

Abstract: The present invention is directed to a process for the production of high density polyethylene by polymerisation of ethylene in the presence of a supported chromium oxide based catalyst which is modified with an organic compound comprising oxygen and a nitrogen atom which is selected from the group consisting of saturated heterocyclic organic compounds with a five or six membered ring, amino esters and amino alcohols. Such organic compounds allow manufacturing of HDPE with increases molecular weight distribution and increased molecular weight.

Abstract: The invention pertains to a compound generating an acid of the formula I or II, for instance corresponding sulfonium and iodonium salts, as well as corresponding sulfonyloximes wherein X is CH2 or CO; Y is O, NR4, S, O(CO), O(CO)O, O(CO)NR4, OSO2, O(CS), or O(CS)NR4; R1 is for example C1-C18alkyl, C1-C10haloalkyl, C2-C12alkenyl, C4-C30cycloalkenyl, phenyl-C1-C3-alkyl, C3-C30cycloalkyl, C3-C30cycloalkyl-C1-C18alkyl, interrupted C2-C18alkyl, interrupted C3-C30cycloalkyl, interrupted C3-C30cycloalkyl-C1-C18alkyl, interrupted C4-C30cycloalkenyl, phenyl, naphthyl, anthracyl, phenanthryl, biphenylyl, fluorenyl or heteroaryl, all unsubstituted or are substituted; or R1 is NR12R13; R2 and R3 are for example C3-C30cycloalkylene, C3-C30cycloalkyl-C1-C18alkylene, C1-C18alkylene, C1-C10haloalkylene, C2-C12alkenylene, C4-C30cycloalkenylene, phenylene, naphthylene, anthracylene, phenanthrylene, biphenylene or heteroarylene; all unsubstituted or substituted; R4 is for example C3-C30cycloalkyl, C3-C30cycloalkyl-C1-C18al

Abstract: The present invention relates to a preparation method of a high-stable non-ionic N-vinyl butyrolactam iodine, wherein non-ionic N-vinyl butyrolactam, iodine and at least one grinding aid are stirred at 150-800 r/min at a temperature of 50° C.-90° C. for 1 to 12 hours to prepare the high-stable non-ionic N-vinyl butyrolactam iodine, wherein the K value of the non-ionic N-vinyl butyrolactam is 32±1, the PD value of the main peak of the non-ionic N-vinyl butyrolactam is ?1.6, the moisture content of the non-ionic N-vinyl butyrolactam is ?2.5%, preferably, the grinding aid is selected one or several from sodium chloride, sodium citrate, sodium carbonate and sodium phosphate, the amount of the grinding aid added is 0.

Abstract: Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided.

Abstract: Natural and synthetic compounds having a lactone structure methods for alleviation of pain, especially pain associated with disorders such as melanoma, leukemia, breast cancer, lung cancer, ovarian cancer, colon cancer, esophagus cancer, liver cancer, and lymphatic cancer. Initial studies have shown that patients can be taken off of morphine when the preferred alpha-methylene-gamma-butyrolactone is administered in a dosage of between 60 and 120 mg/day intramuscularly.

Abstract: Provided is a complex of hydrogen peroxide and at least one compound represented by Formula I: wherein X is: —C(R3)3, —C?C(R3), —O(R3), —N(R3)2, or —S(R3); and R1, R2, and R3 are each independently selected from H, alkyl, alkenyl, alkynyl, aralkyl, aryl, heteroaryl heteroarylalkyl, heterocyclyl, and cycloalkyl, or R2 and an R3 are optionally taken together to form an alicyclic ring. Also provided are anaerobic cure systems and curable compositions employing the complexes described herein.

Abstract: The present invention provides a method for producing of ultra-clean and high-purity N-methyl pyrrolidone through using industrial grade N-methyl pyrrolidone as raw material. After the pretreatment, sorption and dehydration with 4A molecular sieve, twice membrane filtrations are carried out through using ?-cyclodextrin composite membrane for the first and 18-crown-6 composite membrane for the second. The filtrate is rectified under vacuum and filtered through using complexant composite microporous membrane to obtain the product. The ultra-clean and high-purity N-methyl pyrrolidone, produced by the method provided by the present invention, is up to the SEMI C8 standard. And the purity of the product is over 99.8%, the moisture content is less than 0.03%, and the content of single metal ion is less than 1 ppb. Comparing to the prior art, the present invention has the advantage such as the stable quality of the product, simple operation, and is suitable for industrial continuous production.

Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).

Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.