30results about How to "Good immunosuppressive activity" patented technology

A compound having immunosuppressive activity with low toxicity or a pharmacological salt thereof. The compound has a general formula (I) shown below or a pharmacologically acceptable salt thereof, or a pharmacologically acceptable prodrug thereof

A pharmaceutical composition useful as a preventive or therapeutic agent for immune-related diseases. The pharmaceutical composition includes at least HMG-COA reductase inhibitor and at least one amino alcohol compound having the following formula (I), a pharmacologically acceptable salt thereof, or a pharmacologically acceptable ester thereof wherein R1 and R2 each represents hydrogen; R3 represents lower alkyl or hydroxymethyl; R4 represents hydrogen, alkyl, alkoxy or halogen; R5 represents hydrogen, halogeno, cyclohexyl or phenyl; X represents vinylene (CH═CH), oxygen, sulfur or methylated nitrogen; Y represents a single bond, oxygen, sulfur or carbonyl; Z represents a single bond or C1-C8 alkylene; n is 2 or 3.

Compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof, esters thereof or other derivatives: wherein R1 and R2 are a hydrogen atom, an amino protecting group; R3 is a hydrogen atom, a hydroxy protecting group; R4 is a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C1-C10 alkylene group, a C1-C10 alkylene group substituted with 1 to 3 substituents selected from substituent group a and b; R5 is an aryl group; R6 and R7 are a hydrogen atom, a group selected from substituent group a; with the proviso when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 alkylene group.

Antibody conjugates of immune-modulatory compounds and pharmaceutical compositions for use in the treatment of disease, such as fibrotic diseases, autoimmune, or autoinflammatory diseases, are disclosed herein. The disclosed conjugates are useful, among other things, in treating fibrotic diseases, autoimmune diseases, or autoinflammatory diseases, such as by modulating TGFβR1, TGFβR2, TNKS, TNIK, or mTOR.

The invention relates to cortex phellodendri polysaccharide extract and a preparation method and medical application thereof. The content of cortex phellodendri polysaccharide in the extract is counted by glucose, and the content of the polysaccharide accounts for above 65% of the cortex phellodendri extract in percentage by weight. Found by a large number of pharmacological experiments, the cortex phellodendri general polysaccharide extract has notable immunosuppressive activity, can be prepared into immunosuppressive medicaments or used as a medicinal material for preparing other immunosuppressive medicaments, and can be used for treating various immunoreaction-related diseases, including nephritis, pharyngitis, pneumonitis, upper respiratory tract infection, hepatitis, enteritis, gynecologic inflammation, rheumatoid arthritis, diabetes and other immune-related diseases.

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.

The invention discloses a preparation method and new application of artemisinin B. The extraction and separation method of artemisinin B comprises the following steps: drying sweet wormwood leaves, grinding, percolating / soaking with an organic solvent for extraction, recycling the solvent at 60 DEG C under reduced pressure, mixing with silica gel for column chromatography, airing, performing silica gel column chromatography to separate, performing gradient elution by use of a petroleum ether-ethyl acetate or petroleum ether-acetone mixed solvent, adopting the thin layer chromatography to detect the components of the eluent, collecting the component flow with artemisinin B, recycling the solvent to ensure that the solution has small volume, standing the solution to separate out coarse crystals, and repeatedly recrystallizing and purifying the coarse crystals by using an organic solvent such as acetone and ethanol to obtain artemisinin B. The artemisinin B is used for preparing immunosuppressive drugs, has obvious immunosuppressive activity, and can be used for preparing drugs for preventing and treating autoimmune diseases and inflammatory diseases and be used in clinic.

An amino alcohol derivative useful as an excellent immunosuppressive agent is provided.As a result of intensive research to create a highly safe compound which has an excellent immunosuppressive activity, it was discovered that an amino alcohol derivative represented by the general formula (1),has excellent immunosuppressive activity.

The invention discloses a preparation method of artemisinin B and an application in immune field. The extraction and separation method of artemisinin B comprises the following steps: drying sweet wormwood leaves, grinding, percolating / soaking with an organic solvent for extraction, recycling the solvent at 60 DEG C under reduced pressure, mixing with silica gel for column chromatography, airing, performing silica gel column chromatography to separate, performing gradient elution by use of a petroleum ether-ethyl acetate or petroleum ether-acetone mixed solvent, adopting the thin layer chromatography to detect the components of the eluent, collecting the component flow with artemisinin B, recycling the solvent to ensure that the solution has small volume, standing the solution to separate out coarse crystals, and repeatedly recrystallizing and purifying the coarse crystals by using an organic solvent such as acetone and ethanol to obtain artemisinin B. The artemisinin B is used for preparing immunosuppressive drugs, has obvious immunosuppressive activity, and can be used for preparing drugs for preventing and treating autoimmune diseases and inflammatory diseases and be used in clinic.

The present invention relates to a method for selecting high-efficacy mesenchymal stem cells for use in treating an immune disease, the method comprising a step of measuring a level of a particular immunosuppressive biomarker in mesenchymal stem cells in which the expression or activity of suppressor of cytokine signaling (SOCS) is downregulated, high-efficacy mesenchymal stem cells selected by the method, and a method for treating an immune disease by using the high-efficacy mesenchymal stem cells. Providing a method useful for acquiring functionally excellent mesenchymal stem cells having anability to control immune reactions for clinical treatment of various immune diseases including graft-versus-host diseases and autoimmune diseases, the present invention can find useful applicationsin the therapy of immune diseases.

According to the present invention, a Phomopsis asparagi DHS-48 fermentation product is further separated and purified to obtain a compound having a novel structure, and the evaluation on the cytotoxicity and the immunosuppressive activity of the compound proves that the compound has low cytotoxicity and significant immunosuppressive activity on mouse splenocytes. The study on the mechanism of action shows that the compound is a potential immunosuppressor capable of inhibiting the dephosphorylation of the intracellular phosphorylated NFAT protein, and can be used for preparing immunosuppressive drugs aiming at organ transplantation and autoimmune diseases.

The present disclosure relates to cellular therapy products comprising mesenchymal lineage precursor or stem cells and potency assay for these products. The present disclosure also relates to methods for treatment of immune or inflammatory disorders, and treatment or prevention of graft versus host disease (GVHD), or one or more symptoms associated with GVHD, by administration of mesenchymal lineage precursor or stem cells.

The invention discloses 12beta-hydroxy-androstane4,14-diene-16-ketone compounds or pharmaceutically acceptable salt thereof, and the application of the compounds to preparation of immunosuppressive medicines and anti-tumor medicines. The compounds are extracted and separated from epigynum plants, and the structural formula is as shown in the specification, wherein R is selected from hydrogen, methoxyl, ethyoxyl, halogen, aliphatic group and fat amino; and in the formula, the formula as shown in the description represents single bond or double bonds. The experiment proves that the compounds reported in the invention have high immunosuppressive activity and anti-tumor activity; and the compounds provided by the invention provide leading compounds for developing immunosuppressive preparationsand anti-tumor preparations, and are favorable for developing and utilizing plant medicinal resources.

A scopaisoester and a preparation method and application thereof relate to the technical field of drugs. The scopaisoester is novel in structure, has an inhibition effect on T and B lymphocyte proliferation, has selectivity on the inhibition effect on T lymphocytes and can be widely applied to preparation of immunosuppressive drugs. The preparation method of the scopaisoester is simple to operate, and the scopaisoester can be rapidly and efficiently extracted from isodon scoparius. The invention also discloses a pharmaceutical composition, which comprises the scopaisoester and pharmaceutically acceptable auxiliary materials. The pharmaceutical composition has good immunosuppressive activity and can be used as an immunosuppressive agent.

The invention discloses a four-membered ring-containing hetero-diterpenoid compound, and relates to the technical field of medicines and a preparation method and application thereof, the hetero-diterpenoid compound is novel in structure, has an inhibition effect on T and B lymphocyte proliferation, has selectivity on the inhibition effect on T cells, and can be widely applied to preparation of immunosuppressive medicines. The preparation method of the hetero-diterpenoid compound is easy to operate and mild in condition, and the hetero-diterpenoid compound can be rapidly and efficiently obtained. The invention also discloses a pharmaceutical composition which comprises the hetero-diterpenoid compound and pharmaceutically acceptable auxiliary materials. The compound has good immunosuppressive activity and can be used as an immunosuppressive agent.

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.

The invention discloses tuber melanosporum, cordyceps and rhizoma polygonati granules and a preparation method thereof, and relates to the technical field of health care products. The raw materials ofthe tuber melanosporum, cordyceps and rhizoma polygonati granules comprise main materials and auxiliary materials, wherein the main materials include the following ingredients in parts by weight: 3-6parts of tuber melanosporum extracts, 3-6 parts of cordyceps powders, 12-16 parts of stichopus japonicas extracts, 12-16 parts of cervus nippon penis et testis cervi extracts, 7-10 parts of Maca powders, 10-15 parts of radix morindae officinalis extracts, 10-15 parts of rhizoma polygonati extracts, 10-15 parts of prepared radix rehmanniae extracts and 18-25 parts of glycyrrhizae radix extracts. In the tuber melanosporum, cordyceps and rhizoma polygonati granules, the glycyrrhizae radix is put in an important position, rhizoma polygonati is taken as an auxiliary material, the efficacy of warming the middle and benefiting qi of the rhizoma polygonati is taken, the stichopus japonicas is assisted to nourish the blood, nourish yin and replenish yin fluid, then, ingredients, including the tuber melanosporum extracts, the cordyceps powders, the cervus nippon penis et testis cervi extracts, the Maca powders, the radix morindae officinalis extracts the prepared radix rehmanniae extracts and the like, are added to nourish yin, supplement the kidney and enhance a human body autoimmunity function, the internal environment of the human body is maintained, physical power is accelerated to recover, the own anti-fatigue ability of the human body is improved, and the tuber melanosporum, cordyceps and rhizoma polygonati granules can be used for health care and body nourishment.

The invention provides a vinegar-processed tripterygium processing method. The vinegar-processed tripterygium processing method comprises the following steps of: (1) taking a tripterygium root, removing a non-medicinal part, slicing, adding 10-40% of rice vinegar counted by the mass of the tripterygium, storing the tripterygium into a proper container, and soaking the tripterygium for 4-24 hours in a sealed way; (2) storing the tripterygium in a proper container, steaming the tripterygium on water for 1-6 hours; and (3) putting the steamed tripterygium into proper drying equipment, and drying the tripterygium for 1-9 hours at 50-150 DEG C till the moisture content of the tripterygium is 5-15%, and taking out and cooling the tripterygium to obtain the vinegar-processed tripterygium. The vinegar-processed tripterygium processing method is simple and easy to operate, is applicable to mass production, and can effectively meet clinical needs; in-vitro cell experiments prove that the obtained vinegar-processed tripterygium (decoction tablet) can not only keep significant immunosuppressive activity of the tripterygium, but also reduce liver and kidney toxicity caused by the tripterygium.

The invention discloses 3,16-androstenedione compounds or pharmaceutically acceptable salts thereof and application of the 3,16-androstenedione compounds or pharmaceutically acceptable salts in preparation of immunosuppressive and anti-tumor drugs. The 3,16-androstenedione compounds are represented in a following formula, are obtained by performing extraction and separation from Epigynum, and havefollowing structural formula, wherein R1 is selected from hydrogen, hydroxyl groups, methyl groups, halogen, carbonyl groups, aliphatic hydrocarbon groups and fatty amino groups, and R2 is selected from hydrogen, hydroxyl groups, methyl groups, halogen, aliphatic hydrocarbon groups and fatty amino groups. It is proven through experiments that the compounds have strong immunosuppressive and anti-tumor activities, and lead compounds are provided for development of immunosuppressants and anti-tumor preparations by the compounds, so that development and utilization of plant medicinal resources are facilitated.

The invention discloses novel N-containing biheterocyclic acylamide compounds and a preparation method as well as application of the compounds in immunology and particularly relates to the N-containing biheterocyclic acylamide compounds shown in a general formula (I). The compounds have an obvious inhibiting effect on a cell strain Jurkat cell of acute T lymphocytic leukemia and can be applied to treatment of autoimmune diseases and graft rejection. The formula is shown in the specification.

The present invention relates to a monoclonal antibody having excellent immunosuppressive activity or an antigen binding fragment thereof. More specifically, the present invention relates to a monoclonal antibody or an antigen binding fragment thereof, which binds to a peptide consisting an amino acid sequence represented by SSVLYGGPPSAA (SEQ ID NO: 1) or a conjugate of the peptide and a pharmaceutically acceptable carrier, the monoclonal antibody or an antigen binding fragment thereof having a higher binding affinity for core histone than for histone H1.

The invention relates to the technical field of medical microbial chemistry, and particularly discloses a furan ring derivative separated from a liquid fermentation product of an Ophiocordyceps xuefengensis strain and an application of the furan ring derivative in preparation of an immunosuppressive drug, more particularly an application of the furan ring derivative in preparation of a drug with remarkable inhibitory activity on T cell proliferation. According to the invention, the immunosuppressive effect of the furan ring derivative is better than that of an immunosuppressive agent cyclosporin A which is widely used clinically, and the furan ring derivative is an efficient immunosuppressive agent and can be used for preparing immunosuppressive drugs for organ transplantation and autoimmune diseases.

The present invention discloses a rheumatoid arthritis treatment traditional Chinese medicine composition, which is prepared from the following bulk drugs by mass: 1-20 parts of tripterygium wilfordii hook f, and 10-600 parts of schisandra chinensis. According to the present invention, with the compatibility, liver toxicity caused by tripterygium wilfordii hook f can be effectively reduced, and the synergistic effect is provided for treatment of rheumatoid arthritis with tripterygium wilfordii hook f.

The invention discloses a bis-(10-deoxydihydroartemisinin)-phloroglucinol derivative, the structural formula of the bis-(10-deoxydihydroartemisinin)-phloroglucinol derivative is shown in the specification, and the invention also provides a preparation method of the bis-(10-deoxydihydroartemisinin)-phloroglucinol derivative shown in the general formula (I). The invention also provides an application of the bis-(10-deoxydihydroartemisinin)-phloroglucinol derivative of the general formula (I) in preparation of a medicine for treating autoimmune diseases. The compounds provided by the invention are novel compounds for treating autoimmune diseases, have low cytotoxicity, can significantly inhibit immune cell proliferation, effectively inhibit ear swelling induced by 2, 4-dinitrofluorobenzene and plantar swelling induced by sheep erythrocytes on an ear swelling model and a plantar swelling model of delayed hypersensitivity, and can be used for treating autoimmune diseases. The compound shows a good dose-effect relationship, and has a very wide application prospect as a medicine for treating autoimmune diseases.