Abstract: In production of a cationic lipid having at least one methylene group sandwiched between adjacent two cis form double bonds in the molecule, isomerization from a cis form to a trans form is suppressed. A compound represented by the following formula (I): R1—X??(I) (in Formula, R1 represents a hydrocarbon group having at least one methylene group sandwiched between adjacent two cis form double bonds in the molecule and having the carbon number of 8 to 24 and X represents a releasing group) is reacted with (B) a compound having at least one of each of tertiary amino group and hydroxyl group in the molecule in a saturated hydrocarbon solvent having the carbon number of 5 to 10 in the presence of an alkali catalyst.

Abstract: The invention relates to novel hemin derivatives of general formula (I), preparing and use thereof as antibacterial and/or antiviral agents, including, as a component in a pharmaceutical compositions. Advantages of the novel antibacterial and antiviral agents based on the hemin derivatives are in their biocompatibility, biodegradability, a high efficacy against resistant bacteria and widespread viruses which are dangerous to humans, and the lack of toxicity.

Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.

Abstract: The present invention relates to lipid compounds and uses thereof. In particular, the compounds include a class of cationic lipids having an amine moiety, such as an amino-amine or an amino-amide moiety. The lipid compounds are useful for in vivo or in vitro delivery of one or more agents (e.g., a polyanionic payload or an antisense payload, such as an RNAi agent).

Abstract: The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfonamido)propyl)benzyl)pyrrolidin-2-yl)oxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula wherein R1 is selected from the group consisting of CO2R7 and CON(R7)SO2R7 wherein R1, R2, R3, R4, and R7 are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, EP3, TP and/or EP4 receptor mediated diseases or conditions.

Abstract: Method of detecting Symmetrical dimethyl arginine (SDMA) in biological samples. SDMA analogs for generating anti-SDMA antibodies having little or no cross-reactivity with asymmetrical dimethyl arginine, arginine, and monomethylarginine. The analogs have a protected or free thiol (—SH) group or hydroxyl (—OH) group that allow them to be linked to a suitable conjugation target which can be, for example, a protein containing molecule of a label. The anti-SDMA antibodies can be used in diagnostic immunoassay for the diagnosis of SDMA associated disorders and/or diseases.

Abstract: A polishing composition of the present invention is used for polishing an object containing a phase-change alloy and is characterized by containing an ionic additive. Examples of the ionic additive include a cationic surfactant, an anionic surfactant, an amphoteric surfactant, and a cationic water-soluble polymer.

Abstract: The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted ? amino acid, each of the substituting groups in the ? amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.

Abstract: The present invention relates to novel polyamino polyketide antibiotics, methods of their production as well as methods of using these antibiotics, for example, for inhibition or removal of biofilm formation or for treating bacterial infection with these antibiotics.

Abstract: An oxygen absorber is provided that contains at least one of compounds each having a particular structure, and the oxygen absorber exhibits an oxygen absorbing capability without a metal contained, and is suitable for removing oxygen inside a packaging material packaging foods or the like.

Abstract: The present invention discloses novel cationic amphiphiles containing mannose-mimicking shikimic and quinic acid head-groups and a process for preparing cationic amphiphiles with mannose-mimicking polar head-groups such as, shikimic and quinic acids. The findings described herein also demonstrate that compounds of the present invention can target model DNA vaccines to antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs), via mannose receptors expressed on the cell surface of APCs. The cationic amphiphiles disclosed herein show enhanced cellular and humoral immune response compared to their mannosyl counterpart in dendritic cell (DC, the most professional APC) based genetic immunization in mice. Cationic amphiphiles with mannose-mimicking quinic and shikimic acid head-groups described in the present invention are likely to find future applications in the field of genetic immunization.

Abstract: Disclosed herein are corrosion inhibiting compounds and compositions useful in applications relating to the production, transportation, storage, and separation of crude oil and natural gas. Also disclosed herein are methods of using the compounds and compositions as corrosion inhibitors, particularly in applications relating to the production, transportation, storage, and separation of crude oil and natural gas.

Abstract: The present invention relates to fatty alkoxylated polyamine collectors for the beneficiation by flotation of aqueous suspensions of ores, the use of said fatty alkoxylated polyamine collectors in flotation processes for the beneficiation of ores, more particularly in reverse flotation processes for the beneficiation of silicates containing-ores.

Abstract: This invention relates to a polyether-amido-amine corn-pound, obtainable by a two-step reaction of a poly-etheramine with an alkyl acrylate and a polyalkyle-neimine, whereas the polyetheramine and the polyalkyleneimine have at least one primary or secondary amine group, in which the first step comprises the reaction of the polyetheramine with the alkyl acrylate and the second step comprises the reaction of the polyalkyleneimine with the product of the first step. The invention also relates to a method for synthesising a polyether-amido-amine compound by a two-step-reaction. Another object of this invention is a curable composition containing at least one polyether-amido-amine-compound of this invention and a method for coating the surface of a substrate or for binding at least two substrates together using such a curable composition.

Abstract: The present invention provides a novel separation reagent capable of obtaining a high extraction % of rhodium in a chlorine-based acid solution, which has never existed heretofore, and a method for separating and recovering a platinum group metal using the same. An organic phase composed of an amide-containing tertiary amine separation reagent represented by the structural formula shown below is brought into contact with an acid solution containing a platinum group metal, thereby extracting rhodium, platinum and palladium with the organic phase.

Abstract: The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.

Abstract: The invention provides formulations that contain an immunogenic or immunostimulatory cargo, delivery moiety and/or lipid, and a lipid that functions to reduce or prevent induction in a subject of an immune response which would otherwise occur when the immunogenic or immunostimulatory cargo, delivery moiety and/or lipid is administered to a subject as a component of an appropriate control formulation lacking the immune response reducing lipid. Specific immune response reducing lipids and uses thereof are further provided.

Abstract: An embodiment of the invention comprises a ligand of Formula I wherein R1 and R2 are independently an alkyl or cycloalkyl; R3 is and alkyl; X is CO or SO2; Y is (CH2)n, C6H4, (OCH2CH2)n(NHCH2CH2)n and (OCH2CH2CH2)n, or a combination thereof; Z is linker group capable of conjugating to a vector; and n is an integer between 0 and 10. Also included are an imaging agent comprising a compound of Formula I complexed to 99mTc and their method of use to image a subject having a target site using single photon emission computed tomography (SPECT).

Abstract: A lipid particle can include a cationic lipid. Synthesis of the cationic lipid can include a ylide-based reaction, such as a Wittig reaction or sulfur ylide reaction. In some cases, the synthesis can also include a Michael addition or a related addition reaction.

Abstract: The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

Abstract: The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.

Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

Abstract: Provided herein are novel cationic lipids, compositions comprising the cationic lipids, and methods of using the cationic lipids. In some claims, the cationic lipids have cytotoxic activity and can be used alone or in combination with a cytotoxic bioactive compound to kill a cell. In some of these claims, the cationic lipid enhances the cytotoxic activity of the cytotoxic bioactive compound. Methods for treating a subject afflicted with a disease or unwanted condition are provided, wherein the method comprises administering a delivery system comprising a novel cationic lipid to the subject. The invention further provides methods for making delivery systems comprising the novel cationic lipids of the invention.

Abstract: The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted ? amino acid, each of the substituting groups in the ? amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.

Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.

Abstract: The present invention relates to novel polyamino polyketide antibiotics, methods of their production as well as methods of using these antibiotics, for example, for inhibition or removal of biofilm formation or for treating bacterial infection with these antibiotics.

Abstract: The present invention relates to method for the preparation of an ?-amino-alkane(thio)amide having the general formula (6) Furthermore, novel intermediates and partial reaction steps of the claimed method are disclosed.

Abstract: Disclosed and claimed is a composition and method of inhibiting the formation of hydrate agglomerates in a fluid comprising water, gas, and optionally liquid hydrocarbon. The composition comprises the following formula and the method comprises adding to the fluid an effective anti-agglomerant amount of any of the following formula and optionally salts thereof. R1, R2, and R3 are each independently CnH2n+1 or benzyl. R4 is C4-C20 alkyl or alkenyl. n is an integer from 0 to 10. X? is a counterion.

Abstract: There are provided for herein novel amine-containing transfection compounds and methods for making and using same. The compounds are generally obtained by reacting a primary amine with an unsaturated compound. Transfection complexes made using the amine-containing transfection compounds in combination with additional compounds to encapsulate biologically active agents such as nucleic acids are also provided for herein. Methods of using the transfection complexes for the in vivo or in vitro delivery of biologically active agents are also described. The transfection complexes of the present invention are highly potent, thereby allowing effective modulation of a biological activity at relatively low doses compared to analogous transfection compounds known in the art.

Abstract: The present invention encompasses novel intermediates of pregabalin, namely 3-cyano-5-methyl hexanamide (28) and 3-(amino methyl)-5 methyl hexanamide (29), and processes for their preparation. The invention also encompasses a process for converting the novel pregabalin intermediates into pregabalin, Formula (I): The present invention further provides a cost effective method for the synthesis of (S)-pregabalin, which involves the recovery of mandelic acid and tartaric acid used in the resolution process and recycling them, increasing the yields of the final product formed, which substantially reduced the cost of the production.

Abstract: The present invention provides a composition for external application to skin containing one type or two or more types of compounds selected from the group consisting of aminoacetoamide compounds represented by the following general formula (1) and salts thereof.

Abstract: Relative quantification of metabolites by Electrospray Ionization Mass Spectrometry (ESI-MS) requiring a mechanism for simultaneous analysis of multiple analytes in two or more samples. Labeling reagents that are reactive to particular compound classes and differ only in their isotopic compositions facilitate relative quantification. Heavy and light isotopic forms of methylacetimidate were synthesized and used as labeling reagents for quantification of amine-containing molecules. Heavy and light isotopic forms of formaldehyde and cholamine were also synthesized and used independently as labeling reagents for quantification of amine-containing and carboxylic acid-containing molecules, such as found in biological samples. The labeled end-products are positively charged under normal acidic conditions involving conventional Liquid Chromatography Mass Spectrometry (LC/MS) applications.

Abstract: The invention provides low molecular weight apoE mimetic agents suitable for preparing a medicament to treat autoimmune, inflammatory or neurodegenerative disease, (X)a-L-(X)b(Formula (I)) wherein each X is a (potentially different) chemical moiety bearing a positive charge at physiological pH a and b are, independently, numbers between 3 and 6; and L is a linker.

Abstract: Provided are methionine analogs which may be useful for inhibiting protein synthesis, inhibiting microbial growth and/or treating infectious diseases. In some instances, the analogs exhibit bactericidal, antibacterial, anti-infective, antimicrobial, sporicidal, disinfectant, antifungal and/or antiviral properties. Also provided are methods of treatment and methods of preparation, as well as kits and unit dosages.

Abstract: A hair growth regulating agent containing, as an active ingredient, a compound represented by the following formula (I): [wherein R1 represents a substituted or unsubstituted, linear or branched C2 to C25 alkyl group; a group represented by the following formula (II): (wherein R1? represents a substituted or unsubstituted, linear or branched C2 to C20 alkylene group, or —(CH2)n-{O—(CH2)m}o-O—(CH2)p- in which each of n, m, o, and p is an integer from 1 to 6; X? represents —CO—NH—, —O—CO—O—, —NH—CO—, —CO—O—, —O—CO—, or —O—; Y? represents a substituted or unsubstituted C1 to C4 alkylene group; R2? represents a hydrogen atom or a C1 to C4 alkyl group; R3? represents a C1 to C4 alkyl group; and when R2? and R3? each represent a C1 to C4 alkyl group, the two alkyl groups may be identical to or different from each other); or a group represented by the following formula (III): (wherein R1?, X?, and Y? have the same meanings as defined above; R4?, R5?, and R6?, which may be identical to or different from one another,

Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.

Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.

Abstract: Provided herein are novel cationic lipids, compositions comprising the cationic lipids, and methods of using the cationic lipids. In some claims, the cationic lipids have cytotoxic activity and can be used alone or in combination with a cytotoxic bioactive compound to kill a cell. In some of these claims, the cationic lipid enhances the cytotoxic activity of the cytotoxic bioactive compound. Methods for treating a subject afflicted with a disease or unwanted condition are provided, wherein the method comprises administering a delivery system comprising a novel cationic lipid to the subject. The invention further provides methods for making delivery systems comprising the novel cationic lipids of the invention.

Abstract: Polyamine, polyamine/guanidino, and polyamine/biguanide compounds bearing allene, propargyl, cyclopropyl, and other reactive moieties are disclosed. The compounds are useful as irreversible inhibitors of the enzyme lysine-specific demethylase-1 and for the treatment of cancer.

Abstract: H3LMN series compounds used as radioactive agents for treatment of liver cancer and a manufacturing method thereof are revealed. 2-thioethylamine hydrochloride is reacted with triphenylmethanol for protection of thiol to obtain 2-[(triphenylmethyl)thio]ethylamine. Then obtain N-[2-((triphenylmethyl)thio)ethyl]chloroacetamide by a transamidation reaction between 2-[(triphenylmethyl)thio]ethylamine and chloroactyl chloride. Next produce a amine-amide-thiol ligand-N-[2-((triphenylmethyl)thio)ethyl][2-((triphenylmethyl)thio)ethylamino]acetamide by a substitution reaction of N-[2-((triphenylmethyl)thio)ethyl]chloroacetamide and 2-[(triphenylmethyl)thio]ethylamine. After respective reaction with 1-bromotetradecane, 1-bromohexadecane and ethyl 16-bromohexadecanoate, H3LMN series compounds are obtained. These amine-amide-dithiols quadridentate ligands can react with MO3+ (M=Tc or Re) to produce electrically neutral complexes.

Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein -D is an amine containing biologically active moiety; and -L is a non-biologically active linker moiety -L1 represented by formula (I), wherein the dashed line indicates the attachment to the amine of the biologically active moiety and wherein R1, R1a, R2, R2a, R3, R3a, X, X1, X2, X3 have the meaning as indicated in the description and the claims and wherein L1 is substituted with one to four groups L2-Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L2 is a single chemical bond or a spacer; and Z is a carrier group. The invention also relates to A-L, wherein A is a leaving group, pharmaceutical composition comprising said prodrugs and their use as medicaments.

Abstract: Disclosed herein are a method for synthesizing one-dimensional helical mesoporous structure, in which a self-assembled structure of a glycine-derived surfactant is used as a template at room temperature to synthesize the one-dimensional helical mesoporous silica structures having a uniform pore size and a method for synthesizing a glycine-derived surfactant for synthesizing the helical nanoporous structures, in which relatively expensive surfactant can be easily recovered using an organic solvent and reused, which provides economical and environment friendly effects and the glycine-derived surfactant is synthesized by homogeneously heating a reaction product of glycine and phthalic anhydride by dielectric heating with irradiation of microwave, whereby it is possible to realize high yield of the glycine-derived surfactant, shortened synthesis time and increase in energy efficiency, leading to improvement in productivity and reduction in production cost.

Abstract: The present invention relates to the use of a preparation comprising a substance that is capable of binding acetaldehyde, and to the use of a filter that is attached to a tobacco product to reduce tobacco and/or alcohol dependence.

Abstract: A compound consists of a fractal-like, plain or organometallic array useful for energy storage devices. A dendrimer useful in the synthesis of the fractal-like compound includes a single ligating moiety bound to a surface of each quadrant of the dendrimer. A method of making metallo-based (macro) molecules includes the steps of combining monomers selected from the group consisting of bipyridal- and terpyridal-based ligands with connecting metals and self assembling macrocycles wherein the monomes are interconnected by the metals.

Abstract: The invention relates to compounds, which are suitable for coupling to pharmaceuticals, in particular biopharmaceuticals, in addition to conjugates from the compounds comprising biomolecules or pharmaceutically active substances. The inventive compounds are highly cross-linked and can be formed in a simple manner by using a central cross-linking module. The invention also relates to the use of conjugates as an improved formulation of pharmaceuticals and to the production thereof.

Abstract: The present invention provides a novel separation reagent capable of obtaining a high extraction % of rhodium in a chlorine-based acid solution, which has never existed heretofore, and a method for separating and recovering a platinum group metal using the same. An organic phase composed of an amide-containing tertiary amine separation reagent represented by the structural formula shown below is brought into contact with an acid solution containing a platinum group metal, thereby extracting rhodium, platinum and palladium with the organic phase.

Abstract: The present invention provides a composition for external application to skin containing one type or two or more types of compounds selected from the group consisting of aminoacetoamide compounds represented by the following general formula (1) and salts thereof.

Abstract: The invention relates to conjugates of formula (V) or (VI): wherein X is —CO—NH—, —NH—, —O—, —NHCONH—, or —NHCSNH—; their use as radiopharmaceuticals, processes for their preparation, and synthetic intermediates used in such processes.

Abstract: Method of detecting Symmetrical dimethyl arginine (SDMA) in biological samples. SDMA analogs for generating anti-SDMA antibodies having little or no cross-reactivity with asymmetrical dimethyl arginine, arginine, and monomethylarginine. The analogs have a protected or free thiol (—SH) group or hydroxyl (—OH) group that allow them to be linked to a suitable conjugation target which can be, for example, a protein containing molecule of a label. The anti-SDMA antibodies can be used in diagnostic immunoassay for the diagnosis of SDMA associated disorders and/or diseases.

Abstract: Provided is a process for production of a ?-amino-?-hydroxy carboxamide derivative that is important in production of drugs or the like. In the presence of a predetermined solvent, a ?-(N-protected)amino-?-hydroxycarboxylic acid is reacted with an amine to conversion to a ?-(N-protected)amino-?-hydroxy carboxamide derivative; then the derivative is deprotected for conversion to a ?-amino-?-hydroxy carboxamide derivative; and the derivative is crystallized using a protic solvent to obtain a crystal. The high-purity ?-amino-?-hydroxy carboxamide derivative can be stably produced on an industrial scale by the process.