41 results about "Melanoma inhibitory activity" patented technology

The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.

The invention discloses lactobacillus plantarum with the inhibitory activity to alpha-glucosidase. The lactobacillus plantarum is classified and named as Lactobacillus plantarum, is preserved on August 29, 2017 in China General Microbiological Culture Collection Center and has a preservation number of CGMCC NO.14573. By screening, the lactobacillus plantarum has in-vitro inhibitory activity to alpha-glucosidase; the survival rate of the lactobacillus plantarum reaches up to 71.04% under an acid condition that the pH value is 2.0 and is 77.14% in 2.0% cholate deionized water, the tolerances of the lactobacillus plantarum to artificially simulated saliva and intestinal fluid are higher than 90%, the tolerance of the lactobacillus plantarum to gastric fluid reaches 52.49%, and after artificially simulated fluid is sequentially digested, the survival rate reaches 88.27%; the lactobacillus plantarum has good effects on the prevention and treatment of diabetes mellitus type 2; the lactobacillus plantarum is added with a protection agent so as to prepare freeze-drying battier powder with a high viable count, and the viable count reaches up to 87% of the viable count before freeze-drying; and besides, the lactobacillus plantarum further has a good fermentation effect.

The invention relates to a quinoline multi-target kinase inhibitor with antitumor activity and a preparation method thereof. A general structural formula of the compound is shown in a formula (I) described in the specification. In vitro cell experiments verify that the compound provided by the invention has strong in vitro inhibitory activity on five common tumor cell lines, namely human thyroid carcinoma SW579, human hepatic carcinoma HepG2, human lung adenocarcinoma A549, human colorectal adenocarcinoma HCT116 and human gastric carcinoma MKN45, antitumor activities of most of target compounds are better than or equivalent to that of a positive control drug Cabozantinib, and the in vitro cell experiments verify that the compound provided by the invention has strong inhibitory activity on two kinases KDR and MET, so that the compound provided by the invention has a broad application prospect in preparation of a new antitumor drug.

The invention provides an inhibitor of acetylcholine esterase and cholinesterase shown in the general formula (I), wherein R1, R2 and N form an aliphatic heterocyclic ring with 3-7 carbons containing 1-2 hetero atoms, and X is selected from a covalent bond, CH2, CH2CH2, CH2CH2CH2, CH2CH2CH2CH2, and C[(CH2)mCH3]2 (m=5). The compound shows inhibitory activities to acetylcholine esterase and cholinesterase, and can be used for treating and / or preventing cognitive diseases and neurodegeneration diseases.

The invention relates to a novel heterocyclic derivative having a formula (I) and salt. The novel heterocyclic derivative comprises pharmaceutical salt, wherein R1, R2, R3, R4, X, Z and L are defined in the text. Compounds of the novel heterocyclic derivative are a CDK (cyclin-dependent kinase) 4 / 6 inhibitor and an HDAC (histone deacetylase) inhibitor and can be used for treating diseases mediated by CDK4 / 6 and HDAC and disturbances, such as cancer including mantle cell lymphoma, liposarcomata, non-small cell lung cancer, melanomas, squamous cell esophagus cancer and breast cancer. The invention also relates to a pharmaceutical composition containing the compounds provided by the invention, and also relates to application of the compounds or pharmaceutical composition containing the compounds provided by the invention to treatment of related disturbances. <FORMULA I>.

This disclosure relates to agents that bind and neutralize the inhibitory activity of Siglec-10 in lymphocytes, notably by inhibiting the binding of Siglec-10 to its sialic acid ligands on target cells, notably tumor cells. Such agents can be used for the treatment of cancers.

The present invention relates to an LK8-Fc fusion protein, which has increased angiogenesis inhibitory activity and in vivo stability. More specifically, relates to an LK8-Fc fusion protein in which an LK8 protein having angiogenesis inhibitory activity is fused with the Fc region of human immunoglobulin IgG1, as well as a composition for treating cancer, which contains the fusion protein. The LK8-Fc fusion protein has not only angiogenesis inhibitory activity leading to anticancer and metastasis inhibitory activities, but also a very long in vivo half-life, and thus can be used as a more efficient and economic cancer therapeutic agent or cancer inhibitor.

The invention discloses a pyrazolopyrimidine derivative, a preparation method, a pharmaceutical composition and application. The invention provides the pyrazolopyrimidine derivative as shown in a formula I and stereoisomer or solvate or pharmaceutically acceptable salts or active metabolite or prodrug thereof. The pyrazolopyrimidine derivative as shown in the formula I has good inhibitory activity on Bruton's tyrosine kinase (Btk) and particularly has good in vitro and in vivo inhibitory activity on growth of tumor cells, and a good marketization prospect is achieved. Please see the formula I in the description.

The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-H′ function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-H's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.

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.

The present application describes an ethyl acetate fraction of Melissa leaf having excellent angiogenesis and MMP inhibitory activities, and a composition comprising the same.

The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.

The invention discloses a xanthine derivative and its pharmaceutically acceptable salt. In vitro DPP-IV activity inhibition tests, influence tests of normal mouse's glucose tolerance, and influence tests of spontaneous diabetic mouse's blood glucose confirm that the compound and its pharmaceutically acceptable salt show significant DPP-IV inhibitory activity, and can be used in preparation of drugs for treating dipeptidyl peptidase IV associated diseases.

The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.

The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-H′ function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-H's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.

Peptides, modified peptides and antibody or antibody fragment, which inhibit the activity of MIA (Melanoma Inhibitory Activity), for detecting, preventing and curing vitiligo are disclosed.

The invention relates to the technical field of medicine, in particular to a series of rare diterpene compounds which contain four-membered rings merged with pimarane mother nucleuses and are obtainedby conducting extraction, separation and purification on Eutypella sp. D-1 in Arctic soil. The chemical structures of the compounds are shown in the description. It is proved through in-vitro activity tests that the compounds have certain inhibitory activity on various different tumor cells such as human cervical cancer cells Hela, human breast cancer cells MCF-7, human colon cancer cells HCT-116, human chronic leukemia cells K562 and human pancreatic cancer cells SW1990 and can be used for preparing antitumor drugs.

The invention provides mastic tetracyclic triterpenoid components with 11 beta-hydroxysteroid dehydrogenase 1 inhibitory activity, a composition of the mastic tetracyclic triterpenoid components and application, and novel application of mastic tetracyclic triterpenoid components with structures of the general formulas I-IV as 11 beta-HDS inhibitors. As a class of 11 beta-HSD inhibitors in novel structure types, the mastic tetracyclic triterpenoid components have certain selective inhibition effects on 11 beta-HSD1 and are expected to be developed into medicine for regulating lipid metabolism and treating diabetes, obesity, cardiovascular diseases and the like.

The present invention provides small peptide fragments derived from the NF-κB p65 subunit and a pharmaceutical or cosmetic composition comprising the same. The peptides have a NF-κB inhibitory activity, through controlling the transcription-activation of NF-κB. The peptides inhibit the expressions of pro-inflammatory mediators, which are induced by NF-κB, and also inhibit the transmigration of leukocytes, thereby exhibiting an anti-inflammatory activity. Especially, the peptides have excellent inhibitory activities against dermatitis and skin aging. And also, the peptides inhibit base membrane invasion of cancer cells, thereby exhibiting an inhibitory activity against the growth and / or metastasis of cancer cells.

Disclosed is a novel therapeutic agent for autoimmune diseases, particularly type-1 diabetes and rheumatoid arthritis. A novel anti-CD98 antibody can be produced, and a novel therapeutic agent for autoimmune diseases (type-1 diabetes and rheumatoid arthritis) which relies on a novel mechanism of action can be provided using the antibody. The novel anti-CD98 antibody does not inhibit the transport of an amino acid by CD98. Further, unlike conventional anti-CD98 antibodies, the novel anti-CD98 antibody has activities such as an inhibitory activity on the activation of T-lymphocytes, an inhibitory activity on fibronectin-mediated cell adhesion, and an inhibitory activity on the production of an OVA antibody in an OVA-sensitized model.

The present invention discloses five kinds of active oligopeptides with inhibitory effect on tumor cells and their applications. drug. The amino acid sequences of these five oligopeptides are: 1) QAQGSNN; 2) GDLERW; 3) SLENNW; 4) GTYGDL; 5) DVTNAY. The five oligopeptides of the present invention can be obtained in large quantities by artificial synthesis, and have the advantages of short production cycle, large production scale and low production cost, so they have great practical significance and broad application in the research of tumor therapeutic drugs. Application prospect.

The present invention relates to an anti-inflammatory compound having inhibitory activity against tyrosine kinases, and a pharmaceutical composition containing the same as an active ingredient. The compound according to the present invention can inhibit the activity of multiple tyrosine kinases, and thus can be used for efficiently preventing or treating inflammatory diseases, autoimmune diseases or the like related to the tyrosine kinases.

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.

The present invention relates to novel fusarisetin compounds separated from Fusarium sp. FN080326 and having an anticancer activity, and to the use thereof. In detail, novel fusarisetin compounds separated and purified from Fusarium sp. FN080326, which is in turn separated from a soil sample, have an inhibitory activity on the proliferation and transfer of cancer cells such as breast cancer cells, liver cancer cells or myeloid leukemic cells. Therefore, the compounds can be effectively used for anticancer compositions containing the compounds as active ingredients.

The present invention is directed to peptides, antibodies and antibody fragments inhibiting activity of “Melanoma Inhibitory Activity” (MIA).

The present invention relates to the technical field of chemical medicine, and particularly relates to an antitumor compound or a pharmaceutically acceptable salt thereof, and uses of the antitumor compound or pharmaceutically acceptable salt thereof. According to the present invention, the provided compound has a structure represented by a formula I, and the pharmacological experiment results show that the compounds provide good inhibitory activity on a variety of tumor cell lines; and the compound provides selective inhibitory activity against colorectal cancer and breast cancer, further can inhibit the formation of the colorectal cancer cell HCT116 cell population, can block the SW620 cell cycle in the G0 / G1 phase, and can concurrently promote the apoptosis of the two colorectal cancer cells such as HCT116 cells and SW620 cells. The formula I is defined in the specification.

Drug candidates for inhibition of HIV-I replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-I viral replication in vitro.

The present invention provides peptides derived from mammalian serum amyloid A2.1 and their mimics and compounds that have been screened to enhance the activity of macrophage cholesterol esterase and / or inhibit the activity of acyl-CoA:cholesterol transferase or compositions, and methods of treating coronary heart disease, cardiovascular disease, and arteriosclerosis using these compositions are provided.

Disclosed in the present disclosure are substances having tyrosine kinase inhibitory activity and a preparation method and use thereof, wherein the substances are the compounds having the structure of general formula (I) or the geometric isomers or pharmaceutical salts thereof. Through evaluation on tyrosine kinase inhibitory activity and related experiments, the present disclosure demonstrates that these compounds have a good tyrosine kinase inhibitory activity, and may inhibit a variety of tumor cells, and thus may be developed into drugs for preventing and treating tumor diseases, especially liver cancer, lung cancer and neuroblastoma.

The invention provides a compound monomer extracted and separated from streptomycete IIR21 strain fermentation liquor. The monomer contains a 36-element ring polyhydroxy macrolides compound; three desoxy-sugars and 1,4-naphthoquinone are contained in a side chain; the compound monomer has excellent inhibitory activity for bacteria, plant pathogenic fungi and cancer cells. The invention also provides a preparation method for the compound. The compound can be used for preparing the drug for restraining bacteria, plant pathogenic fungi and cancer cells. The bacteria include micrococcus luteus; the fungi includes rhizoctonia solani, magnaporthe oryzae NO-1 strain, magnaporthe oryzae 168 strain, pythium germs, yellow fusarium wilt, Hegu fusarium wilt, brewer yeast and candida albicans; the cancer cells include human lung cancer cells, human breast cancer cells and colon cancer cells.