41 results about "Synthetic derivatives" patented technology

Methods are provided for the treatment of pulmonary hypertension and other conditions associated therewith. In particular, the methods include treatment of pulmonary hypertension with an estradiol metabolite or alkoxy analogue of an estradiol metabolite. The estradiol metabolite or alkoxy analogue thereof may be associated with biodegradable microparticles or nanoparticles alone or in combination with other therapeutic agents. Preferred estradiol metabolites include 2-methoxyestradiol, 4-methoxyestradiol, 2-hydroxyestradiol, and 4-hydroxyestradiol and preferred alkoxy analogues of estradiol metabolites include 2-ethoxyestradiol, and / or to synthetic derivatives and analogues thereof or prodrugs thereof. The compositions may also be in the form of a controlled release formulation.

The present invention relates to novel synthetic derivatives of betulin and the use of such derivatives as pharmaceuticals. The present invention is directed to novel compounds of Formula I: or a pharmaceutically acceptable salt or prodrug thereof.

A simple and effective stereocontrolled synthesis of salinosporamide A(1)has been developed which follows the pathway outlined in the FIGURE. The process, the first total synthesis of salinosporamide A, is capable of providing the compound in substantial quantities for further biological studies. In addition to the method of Scheme I, the present invention also includes several novel synthetic intermediate compounds, several intermediate steps of the preferred synthetic process; and the uses of these compounds in the preparation of synthetic derivatives of the compound Salinosporamide A. Salinosporamide A is of special interest as a synthetic target because of its protein in vitro cytotoxic activity against many tumor cell lines (IC50 values of 10 nM or less).

The invention relates to a combination of treatments, more particularly a combination treatment for HIV-1 infection. The present invention is directed to the use of bryostatin-1 and their natural and synthetic derivatives for AIDS therapy, in particular to the use of bryostatins in combination with other active drugs such as Histone Deacetylases (HDACs) inhibitors and anti-retrovirals, for the treatment of HIV-1 latency. According to the present invention, we provide a combination therapy for the treatment of HIV-1 latency which employs bryostatin-1 (and analogues) and one of the following HDAC inhibitors; valproic acid, butyrate derivatives, hydroxamic acids and benzamides. While HDACi can be used in continuous dosing protocol, bryostatins can be used following a cyclical dosing protocol. Bryostatins can be formulated in pharmaceutical acceptable carriers including nanoparticles, phospholipids nanosomes and / or biodegradable polymer nanospheres. This combination therapy needs to be used in patients treated with antiretroviral therapy (HIV-1 protease inhibitors, HIV-1 reverse transcriptase inhibitors, HIV-1 integrase inhibitors, CCR5 co-receptor inhibitors and fusion inhibitors).

The present invention is a chemical synthesis process of quinolone, which relates to the field of veterinary drug feed additives. The existing synthesis technology is to select from various quinoxaline compound substituted derivatives, but these compounds have relatively large toxic and side effects, and simply change The side chain can no longer meet the needs. The present invention uses heavy ion beams to modify the structure of quinoxaline to produce new compound molecules. Through pharmacodynamic research, the standard sample is separated for chemical synthesis. The present invention designs three synthetic routes. Corresponding to the three chemical synthesis processes, the new compound was identified by spectrum, and it was determined to be quinolone. After further growth-promoting and toxicity tests, it showed obvious improvement and improvement compared with the lead compound quinolone. The invention has the beneficial effects of greatly shortening the development cycle and greatly saving the development cost, and shows that quinolone is a very vital veterinary drug feed additive.

The present invention provides compositions comprising peptidyl inhibitors of CD40L-dependent signalling that are not derived from a natural binding partner of CD40L such as CD40, or from a native CD40-CD40L interface. More particularly, the peptidyl inhibitors of the present invention are derived from natural sources that do not express CD40-CD40L costimulatory pathways. The invention also provides synthetic derivatives and analogs of the peptidyl inhibitors having enhanced binding affinity for CD40L or enhanced inhibitory activity relative to their parent molecules.

This invention relates to compositions containing combinations of a balanced PC composition and one or more cannabinoids, a natural or synthetic derivative thereof, or a salt thereof, and kits containing such combinations and methods of using such combinations to treat subjects suffering from addiction to substances and related diseases or disorders. This invention also relates to the synergistic effect of such combination therapies in humans.

The present invention relates to novel synthetic derivatives of triterpenes and the use of such derivatives as pharmaceuticals. The present invention is directed to novel compounds of Formula I: or pharmaceutically acceptable salt or ester thereof, wherein R1 is a carboxyalkanoyl, where the alkanoyl chain can be interrupted by a nitrogen, sulfur or oxygen atom, or combinations thereof.

at least one aurone or a natural or synthetic derivative of aurone, or an analogue of aurone, in which the independent phenyl ring can be substituted by a heterocycle of pyrrole, imidazole, triazole, pyridine, furan, or thiophene type, is disclosed as a cosmetic agent, or as an active substance, for the manufacture either of a cosmetic composition, or of a pharmaceutical composition, notably a dermatological composition, having a melanogenesis-inhibiting activity or a depigmenting activity, or an anti-tyrosinase activity.

Agents and natural and synthetic formulations and extracts are useful in control of pathogen infection and infestation in humans, animals and plants, as well as pathogen contamination in environmental locales. A method inhibits growth or infection or infestation of a pathogen, including contacting the pathogen with an effective amount of a combination of a plant defensin or a functional natural or synthetic derivative or variant thereof and a non-defensin peptide, such as a cathelicidin peptide, a hairpin peptide, a hairpin peptide from which disulfide bridges have been removed, indolicidin, synthetic peptide CP-29, or a peptide derived from a cystatin. The combination of the defensin and peptide are synergistic compared to the use of each alone at the same individual dose as used in the combination.

The present invention relates to an improved mode of administration for cannabis and its natural and synthetic derivatives. A pharmaceutical composition suitable for sublingual aerosol or spray delivery of cannabis is provided. The formulation may be dispensed using a pump spray or the formulation may include a propellant, such as butane, 1,1,1,2-tetrafluoroethane (HFC-134a) or 1,1,1,2,3,3,3-heptafluoropropane (HFC-227). The term cannabis is used herein to refer to all physiologically active substances derived from the cannabis family of plants and synthetic cannabis analogues and derivatives, precursors, metabolites etc., or related substances having cannabis-like physiological effects.

The present invention relates to novel synthetic analogues of phosphatidyl-myo-inositol mannosides (hereinafter referred to as PIMs) of general formula (I): or a pharmaceutically acceptable salt thereof, to the method for preparing same and to the use thereof in the prevention or treatment of a disease associated with the overexpression of cytokines or of chemokines, in particular of TNF and / or of IL-12. The invention also relates to a pharmaceutical composition comprising at least one synthetic derivative of PIM.

This invention relates to compositions containing combinations of a balanced PC composition and one or more cannabinoids, a natural or synthetic derivative thereof, or a salt thereof, and kits containing such combinations and methods of using such combinations to treat subjects suffering from addiction to substances and related diseases or disorders. This invention also relates to the synergistic effect of such combination therapies in humans.

This invention relates to compositions containing combinations of a balanced phosphatidylcholine composition and one or more cannabinoids, a natural or synthetic derivative thereof, or a salt thereof, and kits containing such combinations and methods of using such combinations to treat subjects suffering from an imbalance of fatty acids and related diseases or disorders. This invention also relates to the synergistic effect of such combination therapies in humans.

The invention discloses asymmetric cyclobutane derivatives (synthetic derivatives G of rabdosia scoparia lactones), which are named as scopariusicide derivatives, a pharmaceutical composition taking the asymmetric cyclobutane derivatives as the active component, a preparation method of asymmetric cyclobutane derivatives, and an application of asymmetric cyclobutane derivatives in preparation of immuno-suppressive drugs. According to the preparation, scopariusicides, which is derived from pharmaceutical plants, is taken as the template; a precursor compound ent-clerodane diterpene A is taken as the initial raw material, a series of artificial analogues are obtained through six steps of chemical synthesis; the basic structure of the derivatives has a characteristic that ent-clerodane hetero-diterpene has an asymmetric cyclobutane segment, the side chain and aromatic ring of the derivatives may have different substituents, and thus there are many kinds of derivatives. The compounds are synthesized for the first time, the synthesis route is novel, and the derivatives have potential bioactivity, can be used as the lead compounds of immuno-suppressive drugs, and have a very important research value and application prospect.

Cancer is one of the major causes of death worldwide. Although many advances have been made in the treatment and management of the disease, the existence of chemotherapy-resistance means there is still a great need to develop new strategies and drugs for its treatment. Provided herein are synthetic derivatives of combretastatin A-4, in particular those in which the aromatic rings are locked into a non-isomerisable active conformation, thus resulting in improved, stable compounds. The novel compounds are structurally related to combretastatin A-4 (CA-4) and lock the rings into the known active conformation by means of a four membered nitrogen containing heterocyclic ring, such as a beta-lactam ring, incorporated into the standard CA-4 structure. The compounds exhibit potent anti-cancer activity.

The invention relates to an external preparation for treating seborrheic dermatitis, comprising at least one effective parasite-expelling medicament which is extracted from etreptomyces and used as an active component, i.e. large ring lactone, such as abamectin, or chemical modified or synthetic derivative ivermectin, one or more of bactericidal antibiotics in erythrocin, aureomycin, chloromycetin, lincomycin hydrochloride, tobramycin, natamycin, norfloxacin, rifampicin, cyclosporine, gentamicin and neomycin and at least another traditional Chinese medical herbal amylase which are contained in carriers for the surface administration and the cutaneous penetration of the active component, or suitable amounts of glucose, sodium chloride or potassium chloride can be also added to the external preparation. The invention has rapid constringency and demanded efficacy for the seborrheic dermatitis, little excitation irritation to the skin, extremely mild skin peeling without obvious toxic and side effects; and the preparation process can ensure the chemical stabilities of various contents in the production process. The invention can be also used for treating whelks.

The invention relates to a method for synthesizing phenoxyacetic acid derivatives. The salt compound of phenol or methylphenol and the salt compound of chloroacetic acid are mixed and placed in a solvent for heating reaction, and then acidified with an inorganic acid to obtain phenoxyacetic acid. Then dissolve it in a solvent and add a catalyst therein, then pass chlorine gas into it and carry out heating and chlorination reaction, and obtain chlorophenoxyacetic acid (or methylphenoxyacetic acid) derivatives after cooling and crystallization. Compared with the prior art, in the reaction process, the present invention recovers and recycles the solvent and waste water of the reaction system, satisfies its own production balance, and can realize the recycling of the closed system, with a yield greater than 95% and a content greater than 98% , The utilization rate of solvent recycling is greater than 95%, and the waste water discharge in the whole production process is reduced by more than 95%.

Voacamine and its natural and synthetic derivatives such as 16′-decarbometheoxyvoacamine, N6-demethylvoacamine, voacamidine, tabernamine, ervahamine A, vobasine and coronaridine are useful as anti-microbial, anti-parasitic and anti-viral agents. A basic extract of the tertiary alkaloids present in plants of the genus Peschiera or Voacanga, especially Peschiera fuchsiaefolia can be isolated and used directly as such an agent.

The invention relates to the use of benfotiamine (a synthetic derivative of vitamin B1) in preparing drugs for treating diabetic retinopathy, that is, a new clinical indication thereof. Benfotiamine can reduce the formation of 6-phosphofructose and 3-phosphoglyceraldehyde by activating the pentose phosphate pathway, thereby blocking abnormal metabolism pathways including DAG-PKC pathway, aminohexose pathway, polyalcohol pathway and AGEs formation pathway and preventing hyperglycemia-induced damage to retinal capillary endothelial cells. The compound is combined with pharmaceutically-acceptable adjuvant to prepare pharmaceutical preparations suitable for oral intake at a daily dose of 5-100mg, 1-3 times daily.

An anti-scale agent used for barium, strontium and iron and a preparation method thereof. The preparation method includes following steps: on the basis of the mass of the composition as 100%, filling a reaction kettle with 30-55% by mass of a synthetic derivative composed of dihexenyltriamine, nitilotriacetic acid, formaldehyde and phosphorus trichloride; adding 5-10% of EDTA, and 15-30% of a synthetic substance composed of acrylic acid and 2-acrylamide-2-methylpropanesulfonic acid; performing a stirring process uniformly and a heating process to 40-60 DEG C; slowly adding dropwisely ammonia water and stopping adding the ammonia water until the pH value of the solution is 7.3-7.7; continuously carrying out a reaction for 2 hours with stirring; adding a certain amount of clear water; and performing stirring uniformly to obtain the anti-scale agent specially used for barium, strontium and iron. By means of the anti-scale agent, generation of large amounts of barium strontium sulfate scale and ferric oxide precipitate due to mixing between injected water and oil layer water can be prevented. The anti-scale agent can satisfy a requirement of large different and continuous change of the injected water in a water injection system, has a good inhibiting effect on the barium strontium sulfate scale and the ferric oxide precipitate, is low in cost and is more than 90% in anti-scale rate when a medicine adding amount achieves 200 mg / L.

Methods are provided for the treatment of pulmonary hypertension and other conditions associated therewith. In particular, the methods include treatment of pulmonary hypertension with estradiol metabolite or estradiol metabolite associated with biodegradable microparticles or nanoparticles alone or in combination with another therapeutic agent. Preferred estradiol metabolites include 2-methoxyestradiol, 4-methoxyestradiol, 2-hydroxyestradiol, and 4-hydroxyestradiol, and / or to synthetic derivatives and analogues thereof or prodrugs thereof. The compositions may also be in the form of a controlled release formulation.

The present invention relates to novel synthetic analogs of phosphatidyl-myo-inositol mannosides (hereinafter referred to as PIMs) of general formula (I): or a pharmaceutically acceptable salt thereof, to the method for preparing same and to the use thereof in the prevention or treatment of a disease associated with the overexpression of cytokines or of chemokines, in particular of TNF and / or of IL-12. The invention also relates to a pharmaceutical composition comprising at least one synthetic derivative of PIM.

Agents and natural and synthetic formulations and extracts are useful in control of pathogen infection and infestation in humans, animals and plants, as well as pathogen contamination in environmental locales. A method inhibits growth or infection or infestation of a pathogen, including contacting the pathogen with an effective amount of a combination of a plant defensin or a functional natural or synthetic derivative or variant thereof and a non-defensin peptide, such as a cathelicidin peptide, a hairpin peptide, a hairpin peptide from which disulfide bridges have been removed, indolicidin, synthetic peptide CP-29, or a peptide derived from a cystatin. The combination of the defensin and peptide are synergistic compared to the use of each alone at the same individual dose as used in the combination.

An anti-fungal composition is disclosed and has enhanced microbiocidal activities for killing or inhibiting growth of live mold cells and spores. Further, the composition stops the production of mycotoxins associated with molds. Included among the molds vulnerable to the composition are black mold, Aspergillus fumigatus, Aspergillus flavus, Aspergillus niger, Stachybotrys chartarum, cladosporium species, fusarium species, and penicillium species In the composition, naturally-occurring compounds selected from the phenylpropanoid family and synthetic derivatives of compounds selected from the phenylpropanoid family are active against the live cells, spores, and mycotoxins. Further, the composition includes D-isomers of naturally-occurring aromatic amino acids and synthetic derivatives of D-isomers of naturally-occurring aromatic amino acids in order to kill and inhibit growth of the live cells, spores, and mycotoxins.