55 results about "2-Methoxyestradiol" 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 generally to methods and compositions of treating disease characterized by abnormal cell proliferation and/or abnormal or undesirable angiogenesis by administering antiangiogenic agents in combination with chemotherapeutic agents. More specifically, the present invention relates to a methods and compositions of treating diseases characterized by abnormal cell proliferation and/or abnormal or undesirable angiogenesis by administering 2-methoxyestradiol, in combination with chemotherapeutic agents.

The invention is of both a composition and method for inhibiting the proliferation of cancerous cells. The composition is, and the method is based on the use of a composition consisting (among active ingredients) substantially of 2-methoxyestradiol and/or one of a number of anaologues thereof. The present inventors have demonstrated beyond serious doubt that these compounds have a pronounced effect in inhibiting the proliferation of cancerous cells and, therefore, provide a desperately needed stepping stone for advancing toward meaningful treatment of cancer.

The invention relates to a 2-methoxyestradiol nanosuspension frozen powder and a preparation method thereof, which effectively solves the problems of poor solubility, short half-life period, low oral bioavailability, difficulty for common injection to achieve high drug loading and targeting effect existing in 2-methoxyestradiol. The 2-methoxyestradiol nanosuspension frozen powder prepared by the invention comprises the following components by weight ratio: 1 part of 2-methoxyestradiol, 1-50 parts of surface active agent and 3-30 parts of cryoprotector. The preparation of the 2-methoxyestradiol nanosuspension frozen powder can be realized by the following method: 1. preparing primary nanosuspension by using a precipitation method or a dispersion method; 2. preparing nanosuspension by using the method of reducing the particle diameter including a high pressure homogenizer method and an ultrasound comminution method; 3. preparing the frozen powder; and 4. re-dissolving the frozen powder by water for injection when in use. The frozen powder for intravenous injection prepared by the invention has fine stability and is favor of transporting and storing drugs.

The invention relates to hydrogel nanoparticles used as an injectable subcutaneous implant agent, which can effectively solves the problem of fulfilling an aim of realizing tumor treatment by locally injecting the hydrogel nanoparticles beside a subcutaneous tumor, changing the hydrogel nanoparticles into a gel and slowly releasing nanoparticles in vivo. The hydrogel nanoparticles are prepared from hydrogel solution and 2-methoxyl estradiol liposome nanoparticle powder or solid liposome nanoparticle powder by a method which comprises the following steps of: adding the 2-methoxyl estradiol liposome nanoparticle powder or the solid liposome nanoparticle powder into the hydrogel solution; and uniformly mixing to form the hydrogel nanoparticles which can be used as an injectable subcutaneous implant agent, wherein 100mg of the 2-methoxyl estradiol liposome nanoparticle powder is added into every 1ml of the hydrogel solution. The injectable hydrogel implant agent of the invention can be used for treating subcutaneous tumors such as breast cancer and the like, keep an effective medicament concentration in a local target site, can realize sustained release and controlled release, can avoid medicament resistance caused by long-term medication, simultaneously improve a curative effect and reduce dosage, reduce toxic and side effects on a whole body, and also can prevent lymphatic metastasis of the tumors such as the breast cancer and the like.

The invention relates to a 2-methoxy-estradiol analogue and a preparation method and application thereof, aiming to solve the problem of preparation of the 2-methoxy-estradiol analogue and realize the application of the 2-methoxy-estradiol analogue to preparation of anti-tumor medicaments. The method comprises the following steps: dissolving 2-methoxy-3-benzyloxy-estradiol-1,3,5-(10)-triene-17beta-alcohol or 17beta-amine serving as a raw material into an organic solvent; in the presence of Lewis alkali, carrying out an acylation reaction on the raw materials and a compound (1) to obtain a 2-methoxy-3-benzyloxy-estradiol-1,3,5-(10)-triene-17beta-ester or 17beta-amide compound (2); carrying out a catalytic hydrogenation to obtain a compound (3); carrying out an acylation reaction or a hydrocarbylation reaction to obtain a compound, namely, the 2-methoxy-estradiol analogue (4), wherein a reaction formula is shown in the specifications. The preparation method of the 2-methoxy-estradiol analogue has the advantages of easiness, mild conditions and high yield, and can be effectively applied to development of anti-tumor medicaments.

The invention relates to a 2-methoxy estradiol injectable hydrogel implant which can effectively solve the problems of maintaining the effective concentration of the target part of 2-methoxy estradiol and enhancing the treatment effect. The invention has the technical scheme that a temperature sensitive type PLGA-PEG-PLGA segmented copolymer having temperature sensitive hydrogel properties is adopted to be mixed with water to prepare dissolution swelling solution; the solution is mixed with the 2-methoxy estradiol to prepare an injection; the temperature sensitive type PLGA-PEG-PLGA segmented copolymer is uniformly mixed with the water to be kept stewing at 0 to 25 DEG C; the temperature sensitive type PLGA-PEG-PLGA segmented copolymer is fully dissolved and swelled into the solution; and the 2-methoxy estradiol is added to be uniformly mixed with solution at 0 to 25 DEG C on the use day or one day before use. The invention has scientific formula, easy production, low cost and good injection effect, can effectively maintain the effective concentration of the target part of the 2-methoxy estradiol and enhance the treatment effect is enhanced and is the innovation on the path of cancer treatment drug forms and drug administration.

The invention relates to a sustained-release microsphere injection containing an antitumor drug (2-methoxyestradiol), and the sustained-release microsphere injection can be used for effectively solving the problems that a conventional drug delivery system for 2-methoxyestradiol is not ideal in tumor treatment effect and has side effects. The technical scheme adopted for solving the problems is as follows: the sustained-release microsphere injection consists of the following parts by weight percent: 5-50% of sustained-release microspheres and 50-95% of solvent system, or independent sustained-release microsphere. The sustained-release microsphere injection can be used for realizing the purpose that the effect of drug can be sustained for a long time by one-time drug delivery, and overcoming the defects and shortcomings of a conventional 2-methoxyestradiol delivery system; and according to the sustained-release microsphere injection, the effective blood concentration can be maintained in the body for a long time, the dosage amount is only 1/30 that of the conventional drug delivery, the tumor inhibiting efficiency is 62% and is higher than that of the intravenous injection drug delivery by about 45%. The sustained-release microsphere injection can be used for reducing the dosage of the drug (toxic and side effects) and has the obvious advantages of improving the drug therapeutic effect.

Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula:

wherein the variables are defined in the specification.

The invention relates to a preparation method and an application of a 2-methoxyestradiol albumin nano freeze-dried agent, and effectively solves the problems in preparation of the 2-methoxyestradiol albumin nano freeze-dried agent and application of the freeze-dried agent to preparation of medicines for treating tumors. The method comprises the following steps: dissolving 2-methoxyestradiol albumin in an organic solvent-absolute ethanol to prepare a solution A; dissolving bovine serum albumin in ultra-pure water to prepare a solution B, adding a surfactant, and adjusting the pH value to be 8-10 by an NaOH solution; adding the solution A into the solution B to prepare a mixed solution C; adding glutaraldehyde into the mixed solution C, stirring evenly, standing and solidifying; performing rotary evaporation to remove the organic solvent to prepare a nano solution D; adding a freeze-drying protective agent into the nano solution D, and performing freeze-drying to prepare the 2-methoxyestradiol albumin nano freeze-dried agent. The 2-methoxyestradiol albumin nano freeze-dried agent is simple in method, easy to produce and prepare, good in stability, long in medicine effect, high in targeting property, rapid in acting, small in negative effect, low in administration frequency, high in bioavailability and simple to prepare; the medicines can be protected from being affected by an environment.

The present invention relates generally to methods and compositions for treating diseases characterized by abnormal cell proliferation and/or abnormal or undesirable angiogenesis by administering antiangiogenic agents in combination with anti-cancer agents. More specifically, the present invention relates to methods and compositions for treating diseases characterized by abnormal cell proliferation and/or abnormal or undesirable angiogenesis by administering 2-methoxyestradiol analogs, in combination with anti-cancer agents.