66 results about "Estrogens catechol" patented technology

The present invention relates to a pH-responsive metal-catechol derivative nanoparticle for drug delivery based on a mussel adhesive protein, particularly Fe(III)-DOPA nanoparticle, and a method for preparing the same. A nanoparticle for drug delivery according to the present invention is prepared using a pH responsive substance, catechol derivative-metal complex, particularly Fe(III)-DOPA complex, based on a mussel adhesive protein. Thereby, the present invention has excellent biocompatibility, is capable of easily and quickly penetrating into a target cell, and releases a loaded drug under acidic conditions, which enables to selectively deliver a drug to a specific disease having an acidic environment.

The invention discloses a therapeutically active compositions of matter and member species thereof which comprise indazole-containing compounds, said compounds and their therapeutic activity resulting directly from an indazole-for-catechol bioisostere replacement of a catechol-containing compound having the same therapeutic activity, where non-catechol substituents are the same or homologous before and after said replacement, and wherein said compositions of matter comprise a compound of Formula (I<1>) or (I<2>), or a pharmaceutically acceptable salt thereof, wherein in a preferred embodiment R is hydrogen; R is cyclohexyl; and R is ethyl. Ra and Rb are each individually and independently hydrogen or non-catechol substituents of said compounds resulting directly from an indazole-for-catechol bioisotere replacement of said catechol-containing compound having said therapeutic activity, where said non-catechol substituents are the same or homologous before and after said replacement, provided that both of Ra and Rb cannot be hydrogen at the same time. The therapeutic activity involved may comprise cholinesterase inhibitory activity, adrenergic alpha 1-antagonist and beta 1-agonist activity, calcium channel inhibitory activity, antineoplastic activity, and phosphodiesterase type IV inhibitor activity.

The invention discloses a preparation method of thermosensitive hydrogel with adhesiveness and antibacterial activity. Firstly, natural chitosan is subjected to hydroxybutylation modification to havethermosensitivity (patent number: 201110214776.X); secondly, HBC (hydroxybutyl chitosan) is grafted with L-DOPA (levodopa) with the chemical name of 3-hydroxy-L-tyrosine, and L-DOPA contains catechingroups, so that the hydrogel has good adhesiveness; then, HBC is grafted with EPL (epsilon-poly-L-lysine), EPL is a polypeptide and has the antibacterial efficacy by use of protonated amino groups. The composite gel material has adhesiveness and antibacterial activity and possibly has wide application prospects in the aspects of tissue engineering and skin repairing.

The invention relates to the technical field of drug synthesis, and discloses a preparation method of norepinephrine bitartrate, which comprises the following steps of S1, taking chloroacetyl catecholas an initial raw material, carrying out a coupling reaction with dibenzylamine in a reaction solvent to obtain 2-(diphenylmethylamino)-3', 4' dihydroxyacetophenone hydrochloride, S2, carrying out hydrogenation catalysis on the 2-(diphenylmethylamino)-3', 4' dihydroxyacetophenone hydrochloride to reduce in the solvent to obtain racemic norepinephrine, S3, enabling racemic norepinephrine to be subjected to D-tartaric acid resolution in an alcohol-water solution, and acquiring L-norepinephrine D-tartrate, and S4, neutralizing the L-norepinephrine D-tartrate in water by alkali to obtain L-norepinephrine. Compared with the existing preparation method, the preparation method disclosed by the invention has the advantages that easily available starting materials are used, good reproducibility ofa synthetic route is ensured, unit operation is simple, economic accounting is realized, each step of reaction is easy to purify, the quality is controllable, and the reaction yield is greatly improved.

The invention provides compounds of formula I:

and salts thereof wherein R₁-R₄ have any of the meanings defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts, and methods for their use in therapy. The compounds have useful antiviral properties.

The invention discloses a method for quantitative determination of catechol-o-methyl transferase activity and a use thereof and belongs to the technical field of biological medicines. The method utilizes 4-acetoxy-7,8-dihydroxycoumarin as a COMT enzyme specific probe substrate. The substrate can be specifically catalyzed through the COMT enzyme to produce a 8-methoxy product, the 8-methoxy product can produce a fluorescence signal at wavelength of 520nm and through detection of fluorescence intensity change, COMT activity is detected quantificationally. The method can be used for quantitative evaluation of activity of COMT enzymes in biological samples with different sources and can also be used for external rapid screening of COMT inhibitors and assessment of an inhibition capability. The method can be used for quantitative assessment of real activity of COMT enzymes in various external biological samples, realizes inhibitor rapid screening and inhibition capability quantitative evaluation and can be used for evaluating catalytic activity of different types of COMTs and COMT mutants with different amino acid sequences and further evaluating a catechol drug metabolism capability. The method has the advantages of high selectivity, low price, acquisition easiness and high sensitivity.

An application of oroxylin A and a pro-drug thereof as a catechol-type medicine synergist belongs to the technical field of medicines. The compound is used as the catechol-type medicine synergist and has the following structure general formula (I), wherein R is hydrogen, carboxylic ester, glucuronic acid and the like substitutive groups. One or more compounds of the oroxylin A and the pro-drug thereof can be mixed with levodopa according to a certain ratio to prepare a drug composition for treatment of Parkinson's disease. The oroxylin A and the pro-drug prepared through modification thereof are improved in both solubility and transmembrane capability and are significantly prolonged in in-vivo metabolic half life period, which is longer than the in-vivo metabolic half life periods of majority of catechol-type medicines, so that the compounds have excellent medicine preparation prospect. In addition, the compounds also can be combined with a catechol-type medicine to form a compound medicine. The compound medicine can be prepared into an oral-taking slow-release preparation to further improve oral-taking bioavailability and treatment effects of the catechol-type medicines.

The present invention relates to a biocompatible, foldable, thin profile, low mass and high surface area, chitosan dressing, optionally modified with catechol, and suitable for treating bleeding in a physiological environment, e.g. bladder, and in particular in connection with the TURP procedure. The characteristics and structures of the chitosan dressing are provided. Methods of making and using the chitosan dressing are also provided.

The invention provides a catechol compound as well as a preparation method and application thereof. The catechol compound has a structure as shown in a formula (I) or a formula (III). The invention further discloses a preparation method of the catechol compound. The method is wide in raw material source, simple to operate, short in route, free of metal catalysis and low in cost, and has potential industrial value. The catechol compound disclosed by the invention has the activity of inhibiting the proliferation of PC3 human prostate cancer cells, so that the catechol compound can be used for preparing anti-prostate-cancer medicines.

The invention provides a chitosan arginine gel dressing for repairing dental tubules. The chitosan arginine gel dressing comprises 0.1-0.4 part by weight of a functional mixture, wherein the functional mixture is prepared by mixing modified beta-chitosan and arginine according to a mass ratio of (1-3): (6-8), and the modified beta-chitosan is obtained by compounding and modifying catechol and beta-chitosan under a weak acid condition. The chitosan arginine gel dressing prepared by the invention can better accelerate a sealing effect on dentin tubules, can quickly relieve dentin allergic aching pain, quickly resist allergy and strengthen teeth, has high sealing effect on the dentin tubules, and is beneficial to enhancing anti-inflammatory, tooth-strengthening and desensitization effects of the dentin.

The present invention provides a novel compound which has a wide antimicrobial spectrum, and in particular exhibits potent antimicrobial activity against beta-lactamase producing Gram negative bacteria. Specifically, the present invention provides a compound of the formula (I):

wherein each symbol is as defined in the specification, or an amino-protected compound when the amino group is present on the ring in the 7-side chain, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.