Abstract: Disclosed are a pyridopyrimidine derivative as shown in general formula (I), a preparation method therefor and a pharmaceutical composition containing the derivative, and the use thereof as a therapeutic agent, particularly as a TLR8 agonist, wherein each substituent of general formula (I) is the same as those defined in the description.

Abstract: The present disclosure is directed to methods of immunization and methods for generating antibodies using compositions comprising cationic lipids and polynucleotide molecules, such as polyribonucleotide molecules, e.g., mRNA, which code for immunogens (e.g., a target protein or a fragment thereof).

Abstract: Systems and methods for integrated glycerol carbonate and/or urea production. This disclosure pertains to development of a process for production of glycerol carbonate and/or urea from ammonia, carbon dioxide and glycerol. The process integrates glycerol carbonate production into a urea production process. The urea produced in the production facility may be used to produce glycerol carbonate by reacting urea with glycerol. The ammonia generated by glycerol carbonate production may be recycled back to urea production. Unreacted urea from the glycerol carbonate production may be separated and recycled to the urea product stream. The systems and methods can reduce the cost for urea production and increase product value of the excessive glycerol produced from other chemical plants.

Abstract: A method and system for membrane-assisted production of high purity concentrated dimethyl carbonate by the reaction of carbon dioxide and methanol is provided. Carbon dioxide is recovered from flue gas or other dilute streams from industrial processes by a membrane and subsequent conversion takes place to an intermediate methyl carbamate by reacting of carbon dioxide with ammonia and methanol. For high-purity carbon dioxide obtained by one of the carbon capture technologies or by a process (such as, for example, ethanol fermentation process) the membrane reactor is replaced with a catalytic reactor for direct conversion of carbon dioxide to methyl carbamate by reacting with ammonia and methanol. The methyl carbamate is further reacted with methanol for conversion to dimethyl carbonate. An integrated reactive distillation process using side reactors is used for facilitating the catalytic reaction in the subject method for producing high purity dimethyl carbonate.

Abstract: The present invention provides tools and methods for the systematic analysis of genetic interactions between cells. The present invention provides tools and methods for modulating cell phenotypes and compositions, combinatorial probing of cellular circuits, for dissecting cellular circuitry, for delineating molecular pathways, and/or for identifying relevant targets for therapeutics development.

Abstract: A process for preparing a diaryl carbonate from a dialkyl carbonate and an aryl alcohol is disclosed. The process takes place in apparatus comprising at least two distillation columns, and at least one of the distillation columns is operated at subatmospheric pressure which is achieved using vacuum equipment.

Abstract: The invention relates to a process for preparing (meth)acrylic esters by esterifying (meth)acrylic acid or transesterifying at least one (meth)acrylic ester with at least one compound comprising at least one OH group in the presence of a heterogeneous catalyst comprising at least one inorganic salt, wherein the esterification or transesterification is performed in the presence of 300 to 3000 ppm of water based on the total weight of the reaction mixture.

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

Abstract: The invention relates to the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. In another aspect, the invention relates to compounds of formula (II) processes for making these compounds, and the use thereof in the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. The invention also relates to methods of synthesis of oligomers, including but not limited to oligopeptides, oligosaccharides and oligonucleotides, particularly oligoribonucleotides and also oligodeoxyribonucleotides, in solution systems, and ionic tag linkers for use in methods provided herein.

Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.

Abstract: The present invention provides a compound having an excellent efficacy for controlling weeds. A cyclohexanone compound of the formula (I): wherein m is an integer of 1, 2 or 3; n is an integer of any one of 1 to 5; X represents CH2, O, S, S(O) or S(O)2; R1 represents a hydrogen atom or a methyl group; R2 and R3 represents a hydrogen atom, a C1-6 alkyl group and the like; R4 represents a C6-10 aryl group or a five- to six-membered heteroaryl group; G represents a hydrogen atom and the like; Z represents a halogen atom, a cyano group, a nitro group, a phenyl group, a C1-6 alkyl group and the like; is useful as an active ingredient for herbicides.

Abstract: The present disclosure relates to novel methanofullerene derivatives, negative-type photoresist compositions prepared therefrom and methods of using them. The derivatives, their photoresist compositions and the methods are ideal for fine pattern processing using, for example, ultraviolet radiation, beyond extreme ultraviolet radiation, extreme ultraviolet radiation, X-rays and charged particle rays.

Abstract: Sitagliptin intermediate compounds of formula (f) and methods of preparation and use thereof are disclosed. Compounds of formula (f) are prepared by the following steps: compounds of formula (a) are subjected to electrophilic reaction with benzyl halides to form compounds of formula (b), which then react with compounds of formula (i) to form novel compounds of formula (e). Gignard agents formed from 2,4,5-trifluoro bromobenzene and magnesium metal react with compounds of formula (e) to afford compounds of formula (f), which are novel intermediates for the preparation of Sitagliptin intermediates of formula (g). Compounds of formula (f) are subjected to reduction by Pd/C, debenzylation, substitution of protecting group to form compounds of formula (g). Compounds of formula (a), (b), (i), (e), (f), and (g) have the following structures, in which R is protecting group of carboxyl and R2 is (substituted) hydrocarbyl.

Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.

Abstract: The invention generally relates to functional polymers and hydrogels. More particularly, the invention provides versatile monomers and polymers with well-defined functionalities, e.g., polycarbonates and poly(ester-carbonates), compositions thereof, and methods for making and using the same. The invention also provides cytocompatible poly(ethylene glycol)-co-polycarobonate hydrogels (e.g., crosslinked by copper-free, strain-promoted “click” chemistry).

Abstract: Provided is a new photochemical process for preparing artemisinin. Also provided are certain dihydroartemisinic acid derivatives useful for preparing artemisinin.

Abstract: Processes for producing diaryl carbonates are disclosed, where such processes may provide for the production of diaryl carbonates from green house gases, such as carbon dioxide. The processes disclosed advantageously integrate diethyl carbonate and diaryl carbonate production, eliminating the need for solvent-based extractive distillation, as is commonly required when producing diaryl carbonates from dimethyl carbonate, providing for the integration of separation equipment and raw material usage, and reducing the operating and capital requirements for such processes. In some embodiments, processes disclosed herein may be operated essentially closed-loop with respect to ethanol usage, for example.

Abstract: A flame-retardant compound has a structure represented by formula (2): (Ar2—O—CO—O—)nA2-X-A1(—O—CO—O—Ar1)m??(2) wherein A1 and A2 each independently represents a substituted or unsubstituted aromatic group; X represents a divalent group represented by —S—, —O—, —CO—, —CN—, —CH2—, —C(CH3)2—, —CH(CH3)—, —NH—, —SO— or —SO2—; Ar1 and Ar2 each independently represents a substituted or unsubstituted phenyl group; and m and n each independently represents an integer of 1 to 3.

Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.

Abstract: Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract: Disclosed is a process for producing a phosphine derivative from a phosphine oxide derivative, which comprises the following steps: (I) mixing a phosphine oxide derivative represented by formula (1) with a chlorinating agent in a polar organic solvent to cause the reaction between these components; and (II-1) adding a salt of a metal having an ionization tendency equal to or lower than that of aluminum to the reaction mixture and carrying out the reductive reaction in the presence of aluminum or (II-2) subjecting the reaction mixture to electrolytic reduction, thereby producing a phosphine derivative represented by formula (2). ArnR3-nP?O (1) ArnR3-nP (2) In formulae (1) and (2), Ar represents an aryl group such as a phenyl group, a phenyl group having a substituent, a heteroaromatic ring group, and a heteroaromatic ring group having a substituent; R represents an aliphatic hydrocarbon group or an aliphatic hydrocarbon group having a substituent; and n represents an integer of 0 to 3.

Abstract: This invention is directed to a general catalyst of high activity and selectivity for the production of a variety of esters, particularly acrylate and methacrylate-based esters, by a transesterification reaction. This objective is achieved by reaction of an ester of a carboxylic or a carbonic acid, in particular of a saturated or unsaturated, typically, a 3 to 4 carbon atom carboxylic acid; with an alcohol in the presence of a catalyst comprising the combination of a metal 1,3-dicarbonyl complex (pref. Zn or Fe acetylacetonate) and a salt, in particular an inorganic salt, pref. ZnCl2, LiCI, NaCI, NH4CI or Lil. These catalysts are prepared from readily available starting materials within the reaction medium without the need for isolation (in-situ preparation).

Abstract: The invention provides polyisocyanate prepolymers, characterised in that they contain polyether carbonate polyols as structural component, their preparation and their use as isocyanate component in 1- and 2-component systems for surface-coating compositions, adhesives and sealing materials.

Abstract: Sitagliptin intermediate compounds of formula (f) and methods of preparation and use thereof are disclosed. Compounds of formula (f) are prepared by the following steps: compounds of formula (a) are subjected to electrophilic reaction with benzyl halides to form compounds of formula (b), which then react with compounds of formula (i) to form novel compounds of formula (e). Gignard agents formed from 2,4,5-trifluoro brmobenzene and magnesium metal react with compounds of formula (e) to afford compounds of formula (f), which are novel intermediates for the preparation of Sitagliptin intermediates of formula (g). Compounds of formula (f) are subjected to reduction by Pd/C, debenzylation, substitution of protecting group to form compounds of formula (g). Compounds of formula (a), (b), (i), (e), (f), and (g) have the following structures, in which R is protecting group of carboxyl and R2 is (substituted) hydrocarbyl.

Abstract: The invention relates to a method for preparing a combretastatin derivative (I) or (II), said method including the following steps: triaryl(3,4,5-trimethoxybenzyl)phosphonium halide P3 (III), wherein Ar denotes an aryl group selected from among phenyl or thienyl, is reacted with P2 having formula (IV) or P?2 having formula (V) so as to respectively obtain the compound P4 or P?4, which have formulas (VI) and (VII), respectively; then, during a step for deprotection in the presence of an acid and/or a base, the compound having P4 or P?4 leads, after an optional purification step, to the compound having formula (I) or (II).

Abstract: A printing or coating composition has a non-volatile liquid vehicle carrying a conductive polymer to be deposited on a substrate and is cleavable by heat or acidification without decomposition of said material, cleavage of said vehicle producing decomposition products that are more volatile than said vehicle and which can be evaporated to dry the composition. Suitably, that vehicle is a carbonic acid diester or a malonic acid diester, e.g. of the formula: wherein R2 is an organic substituent such that R2—OH is a volatile alcohol; R1 is an aliphatic or aromatic substituent of more than three carbon atoms such that is volatile; and R3 is C1-3 alkyl.

Abstract: Bis-Phenol A (BPA) can now be replaced in industrial processes by BPA substitutes. The BPA substitutes can have structures that are derivatives of BPA. The BPA substitutes can be used in preparing epoxy composition, polycarbonate compositions, and polysulfonate compositions or for other uses in place of BPA.

Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.

Abstract: The present invention provides a process for the preparation of Efavirenz. A compound of Formula 1: may be prepared by a process comprising cyclizing, in the presence of a first base, a compound of Formula 5 with a haloformate of Formula 6. Other processes are also provided as well as novel compounds prepared by and used in such processes.

Abstract: The present invention relates to polyurethane, and specifically relates to a polyurethane microcellular elastomer, a method for preparing the same, and the use thereof. The polyurethane microcellular elastomer is the reaction product of (1) an isocyanate-terminated prepolymer obtained by reacting an isocyanate with a first polyol, (2) a second polyol, (3) a chain extender and (4) a catalyst, wherein the first polyol and/or second polyol comprise at least one polycarbonate polyol obtained by reacting carbon dioxide with an alkene oxide. This method of preparing polyurethane microcellular elastomer can not only reduce the demand for raw materials derived from petrochemicals, but also realize the utilization of the “greenhouse gas” carbon dioxide.

Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.

Abstract: A library of macrocyclic compounds of the formula (I) where part (A) is a bivalent radical, a —(CH2)y— bivalent radical or a covalent bond; where part (B) is a bivalent radical, a —(CH2)z— bivalent radical, or a covalent bond; where part (C) is a bivalent radical, a —(CH2)t— bivalent radical, or a covalent bond; and where part (T) is a —Y-L-Z— radical wherein Y is CH2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for the preparation of these compounds in a combinatorial manner, is also disclosed.

Abstract: Processes for producing diaryl carbonates are disclosed, where such processes may provide for the production of diaryl carbonates from green house gases, such as carbon dioxide. The processes disclosed advantageously integrate diethyl carbonate and diaryl carbonate production, eliminating the need for solvent-based extractive distillation, as is commonly required when producing diaryl carbonates from dimethyl carbonate, providing for the integration of separation equipment and raw material usage, and reducing the operating and capital requirements for such processes. In some embodiments, processes disclosed herein may be operated essentially closed-loop with respect to ethanol usage, for example.

Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.

Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.

Abstract: The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula III, wherein R, R1, and R? are as defined in the specification, or a salt thereof, and a compound of formula IV wherein R, R1, R2 and R? are as defined in the specification, and processes of manufacturing these.

Abstract: A process for producing a carbonic ester, characterized in that an aromatic monohydroxy compound or an aliphatic monohydroxy compound is subjected to oxidative carbonylation with carbon monoxide and oxygen in the presence of a palladium catalyst using a compound having a carbonate bond as a reaction solvent. A process for producing a polycarbonate, characterized in that an aromatic dihydroxy compound or an aliphatic dihydroxy compound is subjected to oxidative carbonylation with carbon monoxide and oxygen in the presence of a palladium catalyst using a compound having a carbonate bond as a reaction solvent is also described. The carbonic ester can be produced with a higher yield and at a higher reaction rate and, also, a polycarbonate having a higher molecular weight as compared with the conventional method can be produced with a higher yield and at a higher reaction rate.

Abstract: The compounds of Formula I are pro-drugs of CETP inhibitors having a central oxazolidinone ring. The compounds cyclize by the elimination of HX to form an oxazolidinone ring after administration to a patient.

Abstract: The invention relates to novel compounds of the formula (I) in which X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates 33 and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.

Abstract: Novel compounds are provided, which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Y, wherein Y is a chemical structure as shown in FIG. 1. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.

Abstract: A salt represented by the formula (I-BB): wherein Q1 and Q2 each independently represent a fluorine atom etc., X1 represents a single bond etc., Y1 represents a C1-C36 aliphatic hydrocarbon group etc., A1 and A2 independently each represents a C1-C20 aliphatic hydrocarbon group etc., Ar1 represents a (m4+1)-valent C6-C20 aromatic hydrocarbon group which can have one or more substituents, B1 represents a single bond etc., B2 represents a C4-C36 alicyclic hydrocarbon group which has one or more —OXa groups and which is not capable of being eliminated by the action of an acid etc., and Xa represents a hydrogen atom or a group capable of being eliminated by the action of an acid, m1 and m2 independently each represents an integer of 0 to 2, m3 represents an integer of 1 to 3, with the proviso that m1 plus m2 plus m3 equals 3, and m4 represents an integer of 1 to 3.

Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.

Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.

Abstract: The present invention discloses novel and improved nucleosidic and nucleotidic compounds that are useful in the light-directed synthesis of oligonucleotides, as well as, methods and reagents for their preparation. These compounds are characterized by novel photolabile protective groups that are attached to either the 5?- or the 3?-hydroxyl group of a nucleoside moiety. The photolabile protective group is comprised of a 2-(2-nitrophenyl)-ethyoxycarbonyl skeleton with at least one substituent on the aromatic ring that is either an aryl, an aroyl, a heteroaryl or an alkoxycarbonyl group. The present invention includes the use of the aforementioned compounds in light-directed oligonucleotide synthesis, the respective assembly of nucleic acid microarrays and their application.

Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

Abstract: Provided are compounds of formula A and formula I: A compound of formula A: wherein n is an integer from 6 to 17 and a compound of formula I:

Abstract: A compound of formula I where the substituents have the meanings assigned to them in claim 1, compositions comprising a compound of formula (I) and the use of such compounds and/or compositions controlling insects, acarines, nematodes or molluscs.

Abstract: The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H)-furanones useful in the treatment of cyclooxygenase-2 mediated diseases, Formula (I). The invention also encompasses certain pharmaceutical compositions and methods for treating cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula 1. The above compounds may be used as a combination therapy with low-dose aspirin to treat chronic cyclooxygenase-2 mediated diseases or conditions while also reducing the risk of thrombotic cardiovascular events.