Abstract: The present invention relates to methods of synthesizing long-chain polyunsaturated fatty acids, especially eicosapentaenoic acid, docosapentaenoic acid and docosahexaenoic acid, in recombinant cells such as yeast or plant cells. Also provided are recombinant cells or plants which produce long-chain polyunsaturated fatty acids. Furthermore, the present invention relates to a group of new enzymes which possess desaturase or elongase activity that can be used in methods of synthesizing long-chain polyunsaturated fatty acids.

Abstract: A heterobifunctional monodispersed polyethylene glycol represented by formula (1) which has two adjacent monodispersed polyethylene glycol side chains and does not have a chiral center in the molecular structure: wherein X1 and Y1 are each an atomic group containing a functional group capable of forming a covalent bond upon a reaction with a functional group present in a biofunctional molecule. R1 is a hydrocarbon group or the like. n is an integer of 3 to 72. A1 represents -L1-(CH2)m1— or the like, L1 and L2 represent each an ether bond or the like, and m1 and m2 each independently represent an integer of 1 to 5. B1 represents -L3-(CH2)m3— or the like, L3 and L4 represent an amide bond or the like, and m3 and m4 each independently represent an integer of 1 to 5. Also disclosed is an antibody-drug conjugate including the heterobifunctional monodispersed polyethylene glycol.

Abstract: A process for preparing isobutene homo- or copolymer derivatives by (i) polymerizing isobutene or an isobutene-comprising monomer mixture in the presence of an iron halide-donor complex, an aluminum trihalide-donor complex, or an alkylaluminum halide-donor complex, (ii) reacting a resulting high-reactivity isobutene polymer with a compound which introduces a low molecular weight polar group or a substructure thereof, and (iii) in the case of reaction with a substructure, further reacting to complete the formation of the low molecular weight polar group. The homo- or copolymer derivatives include a radical of a hydrophobic polyisobutene polymer having a number-average molecular weight of 110 to 250 000 and low molecular weight polar groups including amino functions, nitro groups, hydroxyl groups, mercaptan groups, carboxylic acid or carboxylic acid derivative functions, sulfonic acid or sulfonic acid derivative functions, aldehyde functions and/or silyl groups.

Abstract: A process for preparing isobutene homo- or copolymer derivatives by (i) polymerizing isobutene or an isobutene-comprising monomer mixture in the presence of an iron halide-donor complex, an aluminum trihalide-donor complex, or an alkylaluminum halide-donor complex, (ii) reacting a resulting high-reactivity isobutene polymer with a compound which introduces a low molecular weight polar group or a substructure thereof, and (iii) in the case of reaction with a substructure, further reacting to complete the formation of the low molecular weight polar group. The homo- or copolymer derivatives include a radical of a hydrophobic polyisobutene polymer having a number-average molecular weight of 110 to 250 000 and low molecular weight polar groups including amino functions, nitro groups, hydroxyl groups, mercaptan groups, carboxylic acid or carboxylic acid derivative functions, sulfonic acid or sulfonic acid derivative functions, aldehyde functions and/or silyl groups.

Abstract: A polysialic acid compound is reacted with a hetero-bifunctional reagent to introduce a pendant functional group for site-specific conjugation to sulfhydryl groups, for instance side chains of cysteine units in drugs, drug delivery systems, proteins or peptides. The functional group is, for instance, an N-maleimide group.

Abstract: A process for producing an isobutene copolymer derivative by: (I) free-radically copolymerizing (a) 10-90 mol % of a monoethylenically unsaturated C4- to C12-dicarboxylic acid, anhydride, or ester, (b) 10-90 mol % of a high-reactivity isobutene polymer having Mn=110-250000 and obtained by polymerizing isobutene in the presence of an iron-halide-, aluminum trihalide-, or alkylaluminum halide-donor complex, each donor being an ether or carboxylic ester function, or in the presence of a Lewis acid complex containing an organic sulfonic acid, and (c) 0-50 mol % of a monoethylenically unsaturated compound copolymerizable with (a) and (b), to obtain an intermediate isobutene copolymer; and (II) reacting the carboxylic acid functions in the intermediate with at least one of ammonia, an amine, and an alcohol, to form a moiety containing at least one of a hydroxyl, carboxylic ester, amino, quaternized amino, amido, and imido group.

Abstract: The present invention provides a lubricating oil composition for internal combustion engine exhibiting excellent fuel-saving performance for a long period of time. The lubricating oil composition for internal combustion engine is characterized by containing a base oil having a kinematic viscosity as measured at 100° C. of 2 to 10 mm2/s, an aromatic content (% CA) of 3 or less, and a sulfur content of 300 ppm by mass or less, and the following additives: (1) an alkaline earth metal salicylate-based detergent in an amount of 0.3 to 1.5 mass % as reduced to sulfated ash; (2) a zinc dihydrocarbyldithiophosphate in an amount of 0.03 to 0.10 mass % as reduced to phosphorus; (3) a succinimide-based ashless dispersant having a molecular weight of 500 to 4,000, and an alkenyl group or an alkyl group in an amount of 0.05 to 0.20 mass % as reduced to nitrogen; (4) a phenol-based ashless antioxidant in an amount of 0.05 to 3.0 mass %; (5) an amine-based ashless antioxidant in an amount of 0.05 to 3.

Abstract: A process for preparing isobutene homo- or copolymer derivatives by (i) polymerizing isobutene or an isobutene-comprising monomer mixture in the presence of an iron halide-donor complex, an aluminum trihalide-donor complex, or an alkylaluminum halide-donor complex, (ii) reacting a resulting high-reactivity isobutene polymer with a compound which introduces a low molecular weight polar group or a substructure thereof, and (iii) in the case of reaction with a substructure, further reacting to complete the formation of the low molecular weight polar group. The homo- or copolymer derivatives include a radical of a hydrophobic polyisobutene polymer having a number-average molecular weight of 110 to 250,000 and low molecular weight polar groups including amino functions, nitro groups, hydroxyl groups, mercaptan groups, carboxylic acid or carboxylic acid derivative functions, sulfonic acid or sulfonic acid derivative functions, aldehyde functions and/or silyl groups.

Abstract: The invention provides carriers that enhance the absorption, half-life or bioavailability of therapeutic compounds. The carriers comprise targeting groups that bind the Vitamin D Binding protein (DBP), conjugation groups for coupling the targeting groups to the therapeutic compounds, and optionally scaffolding moieties.

Abstract: The invention relates to compounds of formula (I), wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to LFA-1 integrin antagonists to target cells expressing LFA-1.

Abstract: The invention relates to compounds of formula (I): wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-integrin antagonists to target cells expressing alpha-V-beta-3.

Abstract: The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to VLA-4 integrin antagonists to target cells expressing VLA-4.

Abstract: A compound is disclosed. The compound has the general structure: wherein Y is selected from the group consisting of hydrocarbons, hydrocarbons including nitrogen in the carbon backbone, and hydrocarbons including oxygen in the carbon backbone; wherein R1 and R2 are each independently selected from the group consisting of hydrogen, linear hydrocarbons, branched hydrocarbons, and cyclic hydrocarbons and wherein R1 and R2 are not both hydrogen; wherein X is selected from the group consisting of CH2, O, N—R3, S, and nothing and wherein R3 is selected from the group consisting of hydrogen, branched hydrocarbons, linear hydrocarbons, and cyclic hydrocarbons; wherein m is an integer between 1 and 50, inclusive; wherein n is an integer between 1 and 10,000, inclusive; and wherein p, q, and z are each independently an integer greater than 0.

Abstract: The present disclosure provides a C-terminal tethered amino acid for modulating the thrombolytic, fibrinolytic and/or anticoagulant properties of a coagulation protein. The present disclosure also provides a coagulation protein having a catalytic site modified, either at the histidine or serine residue, with the C-terminal tethered amino acid as well as therapeutic applications of those modified coagulation proteins.

Abstract: The invention is directed to multi-functional N-maleimidyl polymer derivatives comprising a water soluble and non-peptidic polymer backbone having a terminal carbon, such as a poly(alkylene glycol), the terminal carbon of the polymer backbone being directly bonded to the nitrogen atom of a N-maleimidyl moiety without a linking group therebetween. The invention also provides two methods of preparing such linkerless N-maleimidyl polymer derivatives.

Abstract: The present invention provides a macromolecular dispersant and a synthesis method thereof, and the dispersant is synthesized by reacting polyisobutylene-g-succinic anhydride with amine compounds. In addition, the present invention also provides an oil-soluble dispersant composition with nano particle pigments and the manufacturing method thereof. The oil-soluble dispersant composition is manufactured by milling a macromolecular dispersant with a pigment and a grinding media. The oil-soluble dispersant composition is adequate for various pigments, shows the excellent immiscibility of oil/water interface, and owns the low viscosity of ?4 cps and the optical density of ink ?1.1. Therefore, the oil-soluble dispersant of the present invention for the nano particle pigment can be acted as the material of the electrowetting display.

Abstract: The present application discloses compositions and methods of synthesis and use of 18F- or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may then be directly or indirectly attached to the targeting molecule. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the bifunctional chelating agent bound to 18F- or 19F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.

Abstract: The invention provides a method for producing a curing agent having an acidic substituent and an unsaturated maleimido group, including reacting, in an organic solvent, a maleimide compound (a) having at least two N-substituted maleimido groups in a molecule thereof with an amine compound (b) having an acidic substituent (represented by formula (I)); a thermosetting resin composition containing the curing agent (A) produced through the method and a compound (B) which is cured with the curing agent, wherein a cured product of the composition has a glass transition temperature of 200° C. or higher; and a prepreg and a laminated sheet produced therefrom.

Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.

Abstract: Provided are a thiol-reactive polyoxyalkylene-modified lipid which can be used to chemically modify bioactive substances and which can be used for drug delivery systems such as liposomes and a method for producing the same. The polyoxyalkylene-modified lipid is represented by the following formula (1): (wherein, R1 and R2 are hydrocarbon groups which are the same as or different from each other and which contain 4 to 24 carbon atoms, R3 is a divalent hydrocarbon group containing 1 to 6 carbon atoms, OA is oxyalkylene groups containing 2 to 4 carbon atoms, n is the average addition mole number of the oxyalkylene groups and is 5 to 1,000, and Z is a group containing either maleimide or iodoacetamide.

Abstract: The present invention relates to compounds from Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) or human immunodeficiency virus (HIV) infection.

Abstract: An oil-soluble lubricating oil additive composition prepared by the process which comprises reacting (A) reacting a copolymer of an (i) an unsaturated acidic reagent; and (ii) a mono-olefin, with at least one linking hydrocarbyl di-primary amine, thereby producing a hybrid succinic anhydride copolymer having from about 10% to about 90% unreacted anhydride groups; and subsequently (B) reacting the hybrid succinic anhydride copolymer with a second amine compound, thereby producing the succinimide; and (C) reacting the succinimide with at least one post-treating agent selected from a cyclic carbonate, a linear mono-carbonate, a linear poly-carbonate, an aromatic polycarboxylic acid, an aromatic polycarboxylic anhydride, an aromatic polycarboxylic acid ester, or mixtures thereof.

Abstract: Surfactants are provided that have a hydrophobic tail portion and a hydrophilic head portion. The hydrophilic head portion includes a terminal dialkyl-substituted tertiary amine or a terminal cycloalkyl-substituted tertiary amine. Also provided are pigment-based inks employing the surfactant, a combination of an electronic display and the pigment-based inks, and a process for reducing conductivity in primary amine-based surfactants and improving reliability of electronic inks employing such surfactants.

Abstract: The present invention relates to the use of 3,4-disubstituted pyrrole 2,5-diones of the formula I as defined in the description for controlling phytopathogenic fungi. Further the invention relates to novel compounds of the formula I.

Abstract: A fuel composition for a fuel injected diesel engine, a method for improving performance of fuel injectors and a method for cleaning fuel injectors for a diesel engine. The fuel composition includes a major amount of fuel and a minor effective amount of a reaction product of (i) a hydrocarbyl substituted compound containing at least one tertiary amino group and (ii) a halogen substituted C2-C8 carboxylic acid, ester, amide, or salt thereof, wherein the reaction product as made is substantially devoid of free anion species.

Abstract: The present invention relates to method for connecting a protein and a drug to a protein drug conjugate, wherein the drug is linked to the protein through a specific branched linker, said branched linker comprises a peptide chain and is derived from o-hydroxy p-amino benzylic alcohol, wherein the peptide chain is connected to the phenyl ring via the p-amino group, the drug is connected to the phenyl ring via the benzylic alcohol moiety, and the protein is connected to the phenyl ring via the o-hydroxy group; further to a process for the preparation of said protein-drug-conjugates via various intermediates, to the pharmaceutical use of such protein drug conjugates, such as methods of controlling the growth of undesirable cells, to pharmaceutical compositions comprising such protein drug conjugates, and to intermediates of the preparation of the protein drug conjugates.

Abstract: Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.

Abstract: The invention relates to compounds of formula (I): The invention likewise relates to a cosmetic method for depigmenting, lightening and/or whitening keratin materials, more particularly the skin, that utilizes these compounds

Abstract: UV-absorbing compounds are disclosed that are derived from at least: (a) a UV absorber having at least one hydroxyl group, primary amine group, or secondary amine group, (b) a coupling agent having anhydride functionality, and (c) a graft host comprising an unsaturated fatty acid. These compounds absorb, scatter, deflect, or scatter ultraviolet radiation in a variety of personal care and performance chemical applications. R? and R?? are alkyl or alkenyl groups that naturally occur in oil.

Abstract: A Diels-Alder adduct of a trans-cyclooctene with a tetrazine is provided, wherein the adduct bears a substituent labeled with a radionuclide. A method of producing a PET or other image of an organ in an animal or human includes forming the Diels-Alder adduct in the animal or human. Trans-cyclooctenes and tetrazines suitable for preparing the adducts 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: The present invention relates to compounds from Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) or human immunodeficiency virus (HIV) infection.

Abstract: The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to LFA-1 integrin antagonists to target cells expressing LFA-1.

Abstract: A bis-type alkenyl-substituted succinimide which is prepared by reaction of succinic anhydride substituted with 2-alkenyl group having a branch structure in ?-position with alkylenepolyamine and its derivatives derived from the bis-type alkenyl-substituted succinimide by post-treatment are of value as friction modifiers, particularly for incorporation into lubricating oils for automatic transmissions.

Abstract: The present invention is a process for preparing (3R)-2?-(4-bromo-2-fluorobenzyl)spiro-[pyrrolidine-3,4?(1?H)-pyrrolo[1,2-a]pyrazine]-1?,2,3?,5(2H?)-tetraone, comprising, for example, the following steps: (1) reacting a compound of the formula (III) wherein R is a C1-6 alkyl group, with 2,5-dimethoxytetrahydrofuran to provide a compound of the formula (IV) wherein R is a C1-6 alkyl group; (2) reacting the compound of the formula (IV) wherein R is a C1-6 alkyl group, with trichloroacetyl chloride to provide a compound of the formula wherein R is a C1-6 group; and (3) reacting the compound provided in step (2) with 4-bromo-2-fluorobenzylamine to provide (3R)-2?-(4-bromo-2-fluorobenzyl)spiro-[pyrrolidine-3,4?(1?H)-pyrrolo[1,2-a]pyrazine]-1?,2,3?,5(2H?)-tetraone.

Abstract: Zwitterion-containing compounds for the modification of hydrophobic molecules to improve their solubility and/or to lower their non-specific binding as provided. The zwitterion-containing compounds may be suitable for modification of detectable labels such as biotin and fluorescein to improve their solubility. The zwitterion-containing compounds may also be useful for the preparation of conjugates of proteins, peptides and other macromolecules or for crosslinking molecules and/or macromolecules.

Abstract: Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.

Abstract: Novel polypeptide derivatives having protracted profile of action.

Abstract: The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.

Abstract: The present invention relates to biodegradable biocompatible polyketals, methods for their preparation, and methods for treating animals by administration of biodegradable biocompatible polyketals. In one aspect, a method for forming the biodegradable biocompatible polyketals comprises combining a glycol-specific oxidizing agent with a polysaccharide to form an aldehyde intermediate, which is combined with a reducing agent to form the biodegradable biocompatible polyketal. The resultant biodegradable biocompatible polyketals can be chemically modified to incorporate additional hydrophilic moieties. A method for treating animals includes the administration of the biodegradable biocompatible polyketal in which biologically active compounds or diagnostic labels can be disposed. The present invention also relates to chiral polyketals, methods for their preparation, and methods for use in chromatographic applications, specifically in chiral separations.

Abstract: This invention relates to polymerizable ultraviolet light absorbers and yellow colorants and their use in ophthalmic lenses. In particular, this invention relates to polymerizable ultraviolet light absorbing methane compounds and yellow compounds of the methine and anthraquinone classes that block ultraviolet light and/or violet-blue light transmission through ophthalmic lenses.

Abstract: The invention relates to the use of salts of compound of the formula (1) and amines of the formula (2), where R1 means C8- to C30-Alkyl or C8- to C30-Alkenyl, R2 means hydrogen or a group of the formula -(A-O)x—H, R3, R4 mean hydrogen, C1- to C4-Alkyl or a group of the formula -(A-O)x—H, A means C2- to C4-Alkylene, and x means a number from 1 to 10, as water-soluble or water-dispersible corrosion inhibitors.

Abstract: The present invention relates to a compound having formula (I): wherein: X is in particular 125I Or 211At; R1 and R?1 are independently from each other chosen preferably from the group consisting of electron-withdrawing groups and alkyl groups; R2 is chosen from the group consisting of: H, alkyl groups, functional groups being able to bind a vector, and functional groups having targeting properties which make the compound of the invention a vector itself; Z is a heteroatom, R5, R8 and R9 are preferably H; Y is preferably an electron withdrawing group.

Abstract: The present invention discloses antimicrobial water treatment membranes, comprising a water treatment membrane, covalently attached to one or more antimicrobial peptides or derivatives thereof, either directly or via one or more tether molecules. There are also provided a process for preparing these antimicrobial membranes, and uses thereof in water treatment applications.

Abstract: The invention relates to growth hormone compounds with a protracted profile. The effect is obtained by linking an albumin binding residue via a hydrophilic spacer to growth hormone variants. Further described are methods of preparing and using such compounds. These growth hormone compounds are based on there altered profile considered particular useful in therapy.

Abstract: A one-component, moisture curing composition that has a) at least one polyurethane polymer P1, being liquid at room temperature and having isocyanate groups and b) at least one polyurethane polymer A of the formula (Ia) or (Ib), being solid at room temperature and having aldimine groups with a melting point in the range from 40° C. to 80° C., the composition 1) being capable of being applied warm; 2) having adjustable cure times and a good initial strength with suitable application properties; 3) curing under the influence of humidity without bubbles; and 4) having a good elasticity and mechanical rigidity after curing.

Abstract: Disclosed are methods of preparing a macromolecular conjugated ligand and a metal complex thereof. The metal complex is targeted for use as a contrast agent, for example, in MRI. The method of preparing a macromolecular conjugated ligand comprises: (a) providing a compound of formula (I) wherein R, A, and Pg are as defined herein, (b) reacting the compound of formula (I) with a macromolecular compound (e.g., dendrimer) in an organic solvent medium which is substantially free of water to obtain a macromolecular conjugated compound, and (c) removing the carboxyl-protecting groups to obtain a carboxyl-deprotected macromolecular conjugated compound. The metal complex can be prepared by reacting the carboxyl-deprotected macromolecular conjugated compound with an ion (e.g., Gd(III)). Also disclosed are two carboxyl-protected 1B4M-DTPA intermediate compounds.

Abstract: Provided are a thiol-reactive polyoxyalkylene-modified lipid which can be used to chemically modify bioactive substances and which can be used for drug delivery systems such as liposomes and a method for producing the same. The polyoxyalkylene-modified lipid is represented by the following formula (1): (wherein, R1 and R2 are hydrocarbon groups which are the same as or different from each other and which contain 4 to 24 carbon atoms, R3 is a divalent hydrocarbon group containing 1 to 6 carbon atoms, OA is oxyalkylene groups containing 2 to 4 carbon atoms, n is the average addition mole number of the oxyalkylene groups and is 5 to 1,000, and Z is a group containing either maleimide or iodoacetamide.

Abstract: Compounds which specifically inhibit legumain, also known as asparaginyl endopeptidase are provided. The compounds have an epoxide or N-Michael acceptor warhead, and have an asparagine side chain attached to a nitrogen atom in the backbone adjacent the warhead. The compounds also preferably comprise a proline residue adjacent the asparagine, and the compound may also contain a third residue and/or a label for cellular or in vivo imaging of active legumain.

Abstract: The present invention is directed to conjugates of hydrolytically stabilized maleimide-functionalized water soluble polymers and to methods for making and utilizing such polymers and their precursors.