64407-57-4

This paper reports the studies on self-assembly and thermosensitive micellization phenomena of a supramolecular polymeric host-guest system consisting of star-shaped poly(N-isopropylacrylamide) (PNIPAAm) with a β-cyclodextrin (β-CD) core (the host polymer

Both thiols and hydrogen peroxide (H2O2) have great correlations with cancer and other diseases, and hence detection probes for sensing these agents may serve as early diagnostic tools. In this article, we report the development of a

The invention relates to a method for the immobilization of biomolecules containing at least one sulfhydryl group, which method comprises contacting a modified metal surface with the biomolecule irradiating the resulting surface with UV radiation in the presence of a photo-initiator, wherein said metal surface is modified with a cross-linker compound comprising a terminal thiol or dithiol group covalently linked to the metal surface, a spacer group, which at the other terminal end is carrying an isolated double or triple bond.

β-Substituted γ-amino acids, β-substituted γ-amino acid derivatives, and β-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.

The use of DCC, triethylamine and 4-dimethylaminopyridine in dichloromethane provides a general and standard one-pot procedure for the O-acylation of cyclic β-dicarbonyl compound derivatives (1) with palmitic and stearic acids which have long hydrocarbon tails, to synthesis of new type of fatty acid derivative in good to excellent yields. Structure elucidation was carried out by FT-IR, 1H NMR and 13C NMR spectroscopy techniques. The acyl migration was also found in results and the corresponding structure was characterized by X-ray crystallography. A proposed mechanism was discussed for the formation of products.

The invention provides novel antibodies which specifically bind to the methylphenidate metabolite ritalinic acid, enabling an immunoassay that can detect methyphenidate in biological samples for an extended period following its ingestion. The invention also describes novel conjugates and kits incorporating the antibodies.

The invention describes methods and kits for detecting and determining current and future synthetic cannabinoids from the JWH and CP families. Unique antibodies derived from immunogens enable said methods and kits.

The invention describes methods and kits for detecting and determining current and future synthetic cannabinoids from the JWH and RCS families. Unique antibodies derived from immunogens enable said methods and kits.

The invention relates to the detection and quantification of 1-benzylpiperazine and its metabolites. The invention is underpinned by novel polyclonal antibodies with unique binding properties which enable immunoassay methods and kits for various applications.

The invention relates to the detection and quantification of 1-benzylpiperazine and its metabolites. The invention is underpinned by novel polyclonal antibodies with unique binding properties which enable immunoassay methods and kits for various applications.

The present invention provides systems and methods for production of activatable diazo-derivatives for use in labeling nucleotides. Labeling nucleotides is accomplished by contacting a stable hydrazide derivative of a detectable moiety with an activating polymer reagent which is used to directly label the nucleotide sample. Labeling occurs on the phosphate backbone of the nucleotide which does not perturb hybridization of the labeled nucleotide with its anti-sense strand. Since the method involves direct labeling, all types of nucleotides can be labeled without prior amplification or alteration.

This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R1:-alkylenyl-C(O)NH-alkylenyl-R3, -alkylenyl-C(O)O—R4, R3:—COOH, —OH, —SH, —NH2, -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R4: H, succinimidyl group, R2: —H,-alkyl. In II: R1: -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R2: -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC═C(CN)2, —HC═CHNO2, -alkylenyl-NH2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine. These compounds are neutral, lipophilic and have low molecular weight and therefore they cross the blood brain barrier and attach to the amyloid sheets. The present invention provides procedures for obtaining naphthalene derivatives with good yields, which can be practical, economical and adapted to a larger-scale manufacturing. We are unaware whether the compounds presented in this invention have been previously reported.

The invention describes methods and kits for detecting and determining current and future synthetic cannabinoids from the JWH and CP families. Unique antibodies derived from novel immunogens enable said methods and kits.

The present invention relates to ε-polylysine conjugates, in particular conjugates of ε-polylysine with compounds carrying carboxyl groups, and to the preparation and use thereof for targeting of the kidney.

The use of opioid peptides of a novel structure is claimed which, in addition to a pharmacophore, additionally contain structural elements reactive with tachykinin receptors. Due to the synergistic reactivity of the opioid with an additional element, an i

The invention relates to an immunoassay method and kit for the detection and/or the determination of zolpidem. The invention is underpinned by a novel antibody, derived from a novel immunogen, that is highly sensitive and binds to zolpidem and its main ur

The invention is directed to novel synthetic C-glycolipids that selectively induce a ThI -type immune response characterized by enhanced IL- 12 secretion and increased activation of dendritic cells. The compounds of the invention are thereby useful in treating infections, cancers, cell proliferative disorders, and autoimmune diseases, both directly and as adjuvants.

Disclosed are huperzine A prodrugs and method of synthesis thereof. The invention further relates to methods of treating, preventing or reversing neurodegenerative diseases, such as, Alzheimer's Disease and neuronal dysfunctions, such as, memory impairment using a pharmaceutical composition comprising a huperzine A prodrug as disclosed herein.

Novel cyclohexylacetic acid compounds corresponding to formula I: processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.

Stimulant of hair growth based on a pantothenic acid derivative The invention relates to cosmetic industry and relates to application of new derivatives of pantothenic acid, namely, ammonium salts with peptides of the following formula (I) where X i s GIy, Ala , Leu , lie , VaI , Pro , Tyr , Phe , Trp , D- IIe , γ-aminobutyric acid ; Y is GIu , Z is OH, NH2, mono- or disubstituted amide (C1-C3) , alkyl ester (C1 - C3) , as well as conjugates of pantothenic acid with peptides of the following formula (II) where X is Gly, Ala , Leu, lie , VaI , Pro , Tyr , Phe , Trp ,D-Ile , γ-aminobutyric acid; Y i s Glu, Z is OH, NH2, mono- or disubstituted amide (C1-C3) , alkyl ester (C1- C3) as a hair growth stimulant, and also a method of preparation of these derivatives.

Polymers containing poly(hydroxyalkanoates) and agents for use with medical articles and methods of fabricating the same are disclosed. The medical article generally comprises an implantable substrate having a coating, and the coating contains a poly(hydroxyalkanoate).

The solution concerns reactive polymers and copolymers based on N-(2-hydroxypropyl)methacrylamide, which contain reactive thiazolidine-2-thione groups in side chains of the polymers or at the ends of polymer chains. The solution also includes a method of their preparation and their use for synthesis of polymer drugs and conjugates with proteins and preparation of gene delivery systems.

The present invention provides novel monofunctional polyethylene glycol aldehydes for the pegylation of therapeutically active proteins. The pegylated protein conjugates that are produced, retain a substantial portion of their therapeutic activity and are

The present invention provides novel monofunctional polyethylene glycol aldehydes for the pegylation of therapeutically active proteins. The pegylated protein conjugates that are produced, retain a substantial portion of their therapeutic activity and are

A process for preparation of crystalline perindopril erbumine of formula (II) which exhibits the X-ray (powder) diffraction pattern like that shown in the figure. The process comprises reacting a solution of perindopril of formula (I), in a solvent selected from N, N-dimethylformamide or dimethyl acetals of lower aliphatic aldehydes and ketones with tertiary butylamine and crystallization of the erbumine salt thus obtained by heating the reaction mixture to reflux, filtering hot, cooling gradually to 20 oC to 30 oC, and further cooling to 0o C to 15 oC for 30 minutes to 1 hour and finally filtering off and drying the crystals.

A linear poly-alpha-amino-acid derivative has at least glutamic or aspartic or serinic repeating units and additionally having a functional group at one or both ends of the polymer backbone and/or only a single functional group as a side group on the polymer backbone, the said functional end group and/or side group being other than alcohol. The said functional derivative is useful for the modification of biologically active materials.

The present invention provides compounds of formula (I), wherein X, Y, R1, R2, R3, and R4 are as defined in the description, and the preparation therof. The compounds of the formula bind to somatostatin receptiors and are useful as pharmaceuticals.

The present invention provides novel heterobifunctional and monobifunctional polyethylene glycol derivatives for the pegylation of therapeutically active proteins. The heterobifunctional PEGs which bear two different functional groups as well as the monobifunctional PEGs which contain two similar functional groups, may be used for cross-linking purposes. The cross-linking may be intramolecular between two areas within the same molecule or intermolecular between two separate molecules. The pegylated protein conjugates that are produced, retain a substantial portion of their therapeutic activity and are less immunogenic than the protein from which the conjugate is derived. New syntheses for preparing such bifunctional derivatives are described.

A composition having a negatively charged molecule and a cationic polyene macrolide compound having two to four positive charges that reacts with the negatively charged molecule is described. This compound can be used to vector molecules and especially nucleic acids into cells.

Group A streptogramin derivatives of general formula (I) in which:R1 represents a halogen atom or an azido or thiocyanato radical,R2 represents a hydrogen atom or a methyl or ethyl radical,R3 represents a hydrogen atom, or the residue of an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclylaliphatic ester which may be substituted, andthe bond - - -represents a single bond (stereochemistry 27R) or a double bond,as well as its salts when they exist.

The present invention relates to a novel use, in particular a novel pharmaceutical use for a series of quinoline derivatives.

Novel monofunctional polyethylene glycol aldehyde for pegylating therapeutically active proteins to produce pegylated protein conjugates which retain a substantial portion of their therapeutic activity and are less immunogenic than the protein from which

Tocopherol derivatives are provided. In one embodiment, the tocopherol derivative includes a tocopherol moiety covalently coupled to branched hydrophilic moiety. In another embodiment, the tocopherol derivative includes a first tocopherol moiety covalently coupled to a second tocopherol moiety through a hydrophilic moiety. In other embodiments, the derivative includes three or more tocopherol moieties.

A cross-linkable monomer comprises a fumaric acid functional group having a first end and a second end, a first spacer group affixed to said first end and comprising at least repeating unit, a first terminal group affixed to said first spacer group, a second spacer group affixed to said second end and comprising at least one ethylene glycol repeating unit, and a second terminal group affixed to said second spacer group. A hydrogel formed by cross-linking the present monomer and a method for making the monomer. A method for forming a hydrogel, comprises the steps of a) synthesizing a copolymer of poly(propylene fumarate) (PPF) and poly(ethylene glycol (PEG) so as to produce P(PF-co-EG), b) synthesizing a PEG-tethered fumarate (PEGF), c) coupling agmatine sulfate to the PEGF to produce PEGF modified with agmatine (Agm-PEGF), and d) cross-linking the P(PF-co-EG) from step a) with Agm-PEGF from step c).

A compound which comprises a backbone having a plurality of chiral carbon atoms, the backbone bearing a plurality of ligands each being individually bound to a chiral carbon atom of the plurality of chiral carbon atoms, the ligands including one or more pair(s) of adjacent ligands each containing a moiety selected from the group consisting of a naturally occurring nucleobase and a nucleobase binding group, wherein moieties of the one or more pair(s) are directly linked to one another via a linker chain; building blocks for synthesizing the compound; and rises of the compound, particularly in antisense therapy.

The present invention provides oligomers which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligomer is modified to include an aminooxy linkage. These oligomers are useful for

Compounds of the formula: having two double bonds which are activated so that they will take part in a polymerization reaction, the double bonds being sufficiently close together to ensure that cyclopolymerization will preferentially occur. These compounds are used as monomers which preferentially are cyclopolymerized under the influence of ultraviolet or thermal radiation in the production of network polymers, for example coatings or binders.

Compositions and methods are described for preventing and treating sepsis in humans and other animals. Surgical patients, low birth weight infants, burn and trauma victims, as well as other individuals at risk can be treated prophylactically. Methods for treating acute infections with advantages over current therapeutic approaches are provided.

Compounds of formula (I): wherein Rxis cyano or bromo; R1is halo; R2is C1-C3alkyl, and pharmaceutically acceptable salts and prodrugs thereof have activity as antiretrovirals.

A composition comprising a polypeptide and an active agent covalently attached to the polypeptide. Also provided is a method for delivery of an active agent to a patient comprising administering to the patient a composition comprising a polypeptide and an active agent covalently attached to the polypeptide. Also provided is a method for protecting an active agent from degradation comprising covalently attaching the active agent to a polypeptide. Also provided is a method for controlling release of an active agent from a composition comprising covalently attaching the active agent to the polypeptide.

A family of compounds capable of inhibiting the activity of farnesyl transferase.

The invention provides compositions that include conjugates of a carrier molecule, preferably cis-docosahexaenoic acid, and 2′,3′-dideoxycytidine. The conjugates are useful in treating viral infections, especially retroviral infections, and particularly reservoirs of viral infection in peripheral T cells and central nervous system manifestations thereof.

Probe sets for the multiplexed detection of the binding of, or interaction between, one or more ligands and target antiligands are provided. Detection involves the release of identifying tags as a consequence of target recognition. The probe sets include

Electrophoretic probes comprising fluorescent compounds as detection groups and mobility modifiers are disclosed for the multiplexed detection of the binding of, or interaction between, one or more ligands and target antiligands are provided. In one embod

Selective cleavage of single stranded nucleic acids can be effected by contacting the nucleic acid with a zinc finger peptide in dimeric form. Dimerization results from diminution or elimination of zinc from the peptide, such that easily controllable and highly selective cleavage may be realized.

A chemical compound comprising an isotopically labeled analog of a standard taxane molecule, wherein said isotopically labeled analog is synthetically formed to have incorporated therein at a selected position a stable isotope of an element existing at said selected positon in said standard taxane molecule, said isotope having amass different form a mass of a mass of a most abundantly occurring isotope of said element in nature, such that said isotopically labeled analog has a molecular weight different form a molecular weight of said standard taxane molecule.

Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.

A polyamide having repeating units represented by formula (1), wherein R1represents a divalent hydrocarbon residue optionally having in the structure a heteroatom having no active hydrogen. The polyamide has a high refractive index, is biodegradable, and is useful as a material for fibers and plastics.

The invention concerns novel lipid compounds suitable for the transport of biologically active substances or molecules in cells. A preferred compound according to the invention is L-lysine-bis-(O,O′-cis-9-octadecenoyl-β-hydroxyethyl)-amide dihydrochloride or one of its optical isomers. In addition, the invention concerns complexes of the novel lipid compounds with polyanions such as DNA and RNA, and ternary complexes of the novel lipid compounds with polyanion and polycations. Finally, the invention concerns liposome formulations made from biologically active substances and the novel lipid compounds, as well as methods of transporting polyanions, polycations or biologically active substances through biological membranes by means fo the novel lipid compounds.

A compound of formula (I) below, which exhibits excellent macrophage activity inhibitory action, is useful for the treatment or prophylaxis of inflammatory disorders, autoimmune diseases or septicemia. In a preferred embodiment, R1 and R3