107 results about "Anti fibrosis" patented technology

Production of anti-fiberization medicine pyphenitone is carried out by taking 2-amino-5-picoline as initial materials, diazotizing, hydrolyzing to obtain 5-methyl-amino-2(1H)pyridone, nucleophilic substituting benzene halide with under existence of catalyst and purifying to obtain final product. It is cheap, has short reactive time and more yield. It can be used for industrial production.

The invention provides a compound for targeted ubiquitinated degradation of Smad3. The compound for targeted ubiquitinated degradation of Smad3 is formed by connecting a compound shown in a formula (I) and an ubiquitin ligase E3 identifying ligand shown in a formula (II) through a Linker shown in a formula (III) for connecting the two. The invention constructs a compound which can be specifically combined with Smad3 to degrade Smad3 proteins in a targeted manner through ubiquitination by jointly applying computer virtual screening and a technology of target ubiquitinated degradation of proteins, and the compound is verified to be capable of degrading Smad3 in a targeted ubiquitinated manner. As Smad3 is the major known fibrosis-inducing signaling protein, the Protac theoretically has an anti-fibrosis effect. Moreover, the molecular weight of the compound is small, so that the Protac can get into or out of cells freely, and therefore, the compound is likely to become a novel drug for treating fibrosis. The compound not only has scientific value, but also has important social value.

This invention relates to inhibition of αv integrins, especially αvβ3 and αvβ6 integrins, by specific antagonists, preferably non-peptidic antagonists, related compounds and compounds with comparable specificity, that downregulate fibrogenesis by inhibiting cell migration and production of pro-fibrogenic molecules (e.g., collagens, TIMP-1) and cytokines (e.g., CTGF) by activated hepatic stellate cells/myofibroblasts, activated epithelia and endothelia. These antagonists alone or in combination with other agents can effectively prevent, mitigate or even reverse development of advanced fibrosis, such as fibrosis/cirrhosis of the liver and fibrosis of other organs, such as lungs, kidneys, intestine, pancreas, skin and arteries.

Methods and compositions comprising an anti-ostepontin agent and/or a PDGF receptor blocker or antagonist, alone or in combination with one or more anti-connexin agents, for example, one or more anti-connexin polynucleotides and/or one or more anti-connexin peptides or peptidomimetics, are provided for the promotion and/or improvement of wound healing and/or tissue repair, and for anti-scarring, anti-inflammatory, anti-fibrosis and anti-adhesion indications.

The present invention relates to a composition for inhibiting fibrosis and more specifically, to a composition for inhibiting fibrosis, wherein the composition is effective in inhibiting fibrosis of tissue cells by containing a peptide derived from telomerase. The peptide according to the present invention exhibits an effect of inhibiting the progression of various kinds of fibrosis, including fibrosis due to occurrence of cancer, fibrosis due to the administration of chemotherapy anticancer drugs, fibrosis due to the exposure to radiation, or progressive fibrosis of tissues, including a TGF-β signaling procedure, and thus can provide a composition for anti-fibrosis or inhibiting fibrosis and a method for treating diseases due to fibrosis.

The present invention relates to a composition comprising Hovenia dulcis Thunb extract, Lindera obtusiloba extract or herbal mixture extract thereof as an effective ingredient.

Hovenia dulcis Thunb extract, Lindera obtusiloba extract or herbal mixture extract thereof of the present invention is highly effective for the improvement of liver functions since it can lower the level of GOT, GPT, ALP, BUN and total bilirubin, which are major liver function indices. ALP and BUN are also used as kidney function indices, so the decrease of the level of ALP and BUN by the extract of the present invention indicates that Hovenia dulcis Thunb extract, Lindera obtusiloba extract or herbal mixture extract thereof of the invention can improve kidney functions as well.

Hovenia dulcis Thunb extract, Lindera obtusiloba extract or herbal mixture extract thereof of the present invention also can lower the amount of hydroxyproline in liver but increase the amount of hydroxyproline in kidney, suggesting that the extract above has excellent anti-fibrosis and kidney protecting effects.

In addition, Hovenia dulcis Thunb extract, Lindera obtusiloba extract or herbal mixture extract thereof of the present invention can lower the level of malondialdehyde, an index of lipid peroxidation in liver and kidney tissues, suggesting that the extract has excellent anti-oxidative effect.

Hovenia dulcis Thunb extract, Lindera obtusiloba extract or herbal mixture extract thereof of the present invention promotes cell viability in liver and kidney cell lines, indicating that the extract has excellent liver and kidney cell protective effects. Therefore, the composition of the present invention can be effectively used not only for anti-oxidation and anti-fibrosis but also for the protection and the improvement of liver and kidney functions.

The invention discloses a high-efficiency targeted type anti-fibrosis medicine nanometer preparation and a preparation method thereof, and relates to a collagenase and/or vitamin A-modified nanometerpreparation or a carrier thereof. The high-efficiency targeted type anti-fibrosis medicine nanometer preparation is characterized in that firstly, collagenase penetrates through a fibrosis collagen carrier; hepatic stellate cells are specifically targeted by the vitamin A, so that an anti-hepatic fibrosis medicine can be transferred in a targeted way at high efficiency, thereby reaching the purpose of high-efficiency hepatic fibrosis therapy. The high-efficiency targeted type anti-fibrosis medicine nanometer preparation has the advantage that the substance exchange barrier caused by accumulation of excessive collagen in the hepatic fibrosis process is overcome by the collagenase-modified nanometer preparation for the first time, so as to provide a novel way and strategy for the high-efficient transfer of the anti-hepatic fibrosis medicine.

Viral VEGF and viral anti-inflammatory cytokine compositions, methods of treatment using them, and kits containing them for use in the promotion and/or improvement of wound healing and/or tissue repair, and for anti-scarring, anti-inflammatory, anti-fibrosis and anti-adhesion indications.

The invention provides a polymer nano-carrier for folic acid specificity targeting of an active hepatic stellate cell and medicinal application thereof. In the transformation process from a resting state to a muscle fibrosis sample active state, expression of an alpha type folate receptor in the hepatic stellate cell is remarkably enhanced. A folic acid-coupled polymer nano-micelle carrier is further prepared, and specificity targeting on the active primary rat hepatic stellate cell and cell strains of the polymer nano-micelle carrier is successfully achieved. According to a medicine nano-carrier system, polyethylene glycol is adopted as a material of a hydrophilic section, and resisting to protein adsorption and cell adhesion in blood circulation of the medicine nano-carrier system is ensured; polycaprolactone serves as a material of a hydrophobic section for nucleation, and loading of a plurality of hydrophobic anti-fibrosis medicines and fluorescent dye is facilitated. Folic acid coupled to a PEG shell guarantees that the carrier system conducts specificity recognition on folate receptors on the surface of the active hepatic stellate cell, finally, the utilization rate of the medicine is effectively increased, and the toxic and side effect of the medicine is lowered.

The invention relates to protecting functions and applications of FSTL1 in anti-fibrosis steady-state regulation of tissues such as livers, and particularly relates to uses of FSTL1 protein or an FSTL1 regulating compound in preparation of medicines treating tissue fibrosis diseases. The invention also relates to a conditional FSTL1 gene knockout non-human animal model closely related to the degree of tissue fibrosis pathological changes, a preparing method thereof and uses of the model in tissue-fibrosis-preventing medicine screening. Treatment is performed by combining different tamoxifen dosages and different animal growth stages, the systemic or vascular endothelial cell FSTL1 gene knockout non-human animal model is obtained and the model is used for simulating different tissue fibrosis pathological changes.

The invention discloses anti-fibrosis drug pirfenidone crystal forms and a preparation method thereof, and belongs to the technical field of anti-fibrosis drug pirfenidone. The technical scheme includes that the anti-fibrosis drug pirfenidone crystal forms include a pirfenidone crystal form II and a pirfenidone crystal form III, and the preparation method for the pirfenidone crystal form II and the pirfenidone crystal form III is provided specifically. The prepared pirfenidone crystal form II and the prepared pirfenidone crystal form III have the advantages of stable chemical-physical property, uniform crystal grain, suitability for long-term storage, convenience in preparation manufacture and the like.

The invention discloses immunoliposome based on endostatin genes, a preparation method and the application thereof. The immunoliposome comprises Vasohibin gene recombination eukaryotic expression vector, liposome and anti-eighth factor-associated antigen monoclonal antibody; wherein the liposome internally wraps up the Vasohibin gene recombination eukaryotic expression vector; the surface of the liposome is connected with the anti-eighth factor-associated antigen monoclonal antibody; the preparation method thereof comprises three steps of: the construction of the Vasohibin gene recombination eukaryotic expression vector, the preparation of the liposome wrapping up the Vasohibin gene recombination eukaryotic expression vector, and the connection of the liposome wrapping up the Vasohibin gene recombination eukaryotic expression vector and the anti-eighth factor-associated antigen monoclonal antibody. The immunoliposome can particularly act on vascular endothelial cells of the lung to inhibit the vasculogenesis and pulmonary fibrosis formation, has strong targeting effect, little side effect and can be used for preparing anti-fibrosis drugs.

The invention provides application of a pirfenidone derivative to pharmacy and discloses application of a compound as shown in a formula (I) (the formula can be seen in specification) or medically acceptable salt, the crystal form, aquo-complex or solvent thereof to preparation of anti-fibrosis drugs and/or antineoplastic drugs; wherein R1, R2, R3, R4 and R5 are separately or simultaneously selected from H, halogen, hydroxyl, nitro, carbonyl or a C1 alkyl group, a C2 alkyl group, a C3 alkyl group, a C4 alkyl group, a C5 alkyl group, a C6 alkyl group, a C7 alkyl group or a C8 alkyl group. The invention provides application of the novel compound as shown in the formula (I) (the formula can be seen in specification) or medically acceptable salt, the crystal form, aquo-complex or solvent thereof to preparation of anti-fibrosis drugs and/or antineoplastic drugs, compared with pirfenidone, the novel compound has different ring structures, anti-fibrosis activity of the novel compound is remarkably better than that of pirfenidone, and the novel compound has good industrialized prospect.

The invention discloses an application of small interfering RNA of Fstl 1 in anti-pulmonary fibrosis. Pharmacology experiments confirm that the small interfering RNA of Fstl 1 can effectively reduce a mortality rate of bleomycin-instilled mice, and pulmonary damage and pulmonary fibrosis which are induced by bleomycin can be reduced significantly via decreasing expression of Fstl 1, thereby indicating that the small interfering RNA of Fstl 1 can be used for preparing drugs for preventing and/or treating pulmonary fibrosis.

The invention belongs to the field of biological materials. A medical implant material can generate a foreign body reaction when entering a human body, and a present, a drug coating for preventing andtreating the foreign body reaction is difficult to delay and control drug release in a drug release process. Aiming at the problems in the prior art, the invention discloses a preparation method of amultiple drug fiber membrane for reducing a foreign body reaction of an implant material. The preparation method comprises the following steps of: firstly, preparing a nano fiber membrane with a 'skin-core' layer structure through a coaxial electrostatic spinning technology; and then spraying polymer microspheres containing an anti-fibrosis drug on the surface of the fiber membrane through a high-voltage electrostatic spraying technology. The preparation method provided by the invention is simple; and the prepared multiple drug fiber membrane has a multiple drug release system, and can realize multiple controlled release of drugs and reduce the foreign body reaction of the implant material.

An article of manufacture is disclosed which comprises at least two active agents, wherein a first of the two active agents comprises an anti-cancer agent or an antifibrotic agent and a second of the at least two active agents downregulates the activity and/or expression of lysyl-oxidase like protein-2 (LOXL-2) and which is capable of altering the structure of the extracellular matrix.

The invention discloses a groups of compounds with functions of anti-fibrosis and inhibition of gelatingase activity and their use, test results show that, the compounds can effectively inhibit the activity of gelatinase-2 (MMP-2) and gelatinase-9 (MMP-9), thus can be used for preparing medicament for preventing or treating fibrosis diseases, periodontitis, arthritis, combination fibrosis, tumor metastasis and related diseases.

The invention discloses a traditional Chinese medicine compound for preventing or treating hepatic fibrosis and cirrhosis, a preparation and a preparation method for the preparation. The active ingredients of the traditional Chinese medicine compound/preparation mainly include curcumin, silymarin and astragalus membranaceus. Salvia miltiorrhiza, poria cocos and radix bupleuri can be added for preparing into liquid or solid preparation. On the basis of the theory of traditional Chinese medicine and the modern pathological study, a clinical efficacy test proves that the traditional Chinese medicine compound/preparation has preventing and treating effects for hepatic fibrosis and cirrhosis caused by viral hepatitis, alcoholic fatty liver, non-alcoholic fatty liver disease, and the like, has strong anti-inflammatory, anti-fibrosis, antioxidant and immune-regulating effects and can comprehensively protect the liver.

The invention relates to a 3-vinyl indazole derivative as well as a preparation method and application thereof, and belongs to the field of chemical medicines. The invention provides a compound represented by a formula I, an optical isomer of the compound, and a pharmaceutically acceptable salt of the compound or the optical isomer of the compound. Biological experiments prove that the 3-vinyl indazole derivative provided by the invention has a remarkable inhibition effect on the activity of FGFR kinase, can effectively inhibit proliferation of various cancer cells such as breast cancer, lungcancer and gastric cancer, and has a broad-spectrum anti-cancer effect; besides, the 3-vinyl indazole derivative also has an obvious inhibiting effect on proliferation of fibroblasts, the effect of the 3-vinyl indazole derivative is equivalent to that of a drug Nintedanib for treating pulmonary fibrosis clinically at present, and the anti-fibrosis curative effect is remarkable. The 3-vinyl indazole derivative provides a new choice for development and application of anti-cancer and anti-fibrosis drugs.

The invention discloses a compound shown in the formula I or pharmaceutically acceptable salt or a pharmaceutically acceptable crystal form or pharmaceutically acceptable hydrate or pharmaceutically acceptable solvate thereof. R1, R2, R3, R4 and R5 are selected from H, halogen, hydroxyl, nitryl and carbonyl or C1-C8 alkyl respectively or simultaneously; R6 and R7 are selected from H or C1-C8 alkyl respectively or simultaneously, and R6 and R7 are connected to form a five-membered ring or a six-membered ring containing 3-17 carbon atoms. Compared with pirfenidone, the novel compound has different ring structures, the anti-fibrosis activity of the novel compound is remarkably superior to that of pirfenidone, and especially, the inhibition ratio of the novel compound for fibroblast proliferation is increased by at least 30% compared with pirfenidone; meanwhile, the inhibition effect of the novel compound on fibroblast secretory fibronectin is remarkably superior to that of pirfenidone, and good industrial prospects are achieved. The formula I is shown in the specification.

Novel and effective anti-fibrosis agents are obtained. An anti-fibrosis agent containing an antagonist for integrin α8β1 is used. In addition, used is an antagonist containing an anti-integrin α8β1 antibody that specifically binds to at least one amino acid in a cap subdomain of an integrin α8 chain and a periphery thereof. Also, used is an anti-fibrosis agent containing an anti-integrin α8β1 antibody that specifically binds to R120 of an integrin α8 chain and a periphery thereof or S132 and a periphery thereof. Note that the above antagonists may each be an anti-integrin α8β1 antibody capable of binding to any of integrins α8β1 derived from a human, mouse, and rat.