397 results about "Antagonism" patented technology

An antibody of the invention interacts with human DR5 to produce agonistic or antagonistic effects downstream of the receptor including inhibition of cell proliferation and apoptosis. Nucleic acid sequences and amino acid sequences of anti-DR5 antibodies have been elucidated and vectors and cells containing and expressing these sequences have been generated. Methods and uses for the antibodies are detailed including treatment of apoptosis-related disease and treatment of dysregulated cell growth.

Disclosed are compounds that are bradykinin B₁ receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B₁ receptor.

The invention discloses a compound microbial fertilizer for antagonism of soil-borne fungal diseases, and a preparation method and an application thereof; the fertilizer takes humic acid as a compound carrier, includes bacillus amyloliquefaciens HFJ-7 with the bacteria content of 1.8*10<8>-2.1*10<8> CFU/g, and also includes bacillus megatherium B3. The bacillus amyloliquefaciens HFJ-7 in the compound microbial fertilizer has the preservation number of CGMCC No.10011. The bacillus amyloliquefaciens HFJ-7 strain can be antagonistic to rhizoctonia solani, fusarium oxysporum, root rot pathogen, cucumber fusarium wilt pathogen, phytophthora capsici leon pathogen and other soil-borne disease pathogenic fungi. After the bacillus amyloliquefaciens HFJ-7 is compounded with the bacillus megatherium B3, the resistance to rhizoctonia solani and pepper root rot pathogen can be significantly improved, a disease state index of pepper seedling root rot disease can be significantly reduced, and the occurrence and spreading of pepper root rot can be effectively prevented and controlled.

The present invention provides methods and compositions for drug screens to identify and characterize agents that are agonistic or antagonistic to activation of the promoter region of the NAG-1 gene. Activation of the NAG-1 gene is associated with the apoptotic elimination of cancer cells both in vitro and in vivo. The invention also provides novel promoter region sequences of the NAG-1 gene.

The invention discloses a dihydropyrimidine compound as well as a preparation method and an application thereof, and belongs to the technical field of medicinal chemistry. The structure of the dihydropyrimidine compound provided by the invention is as shown in a formula I in the specification. The preparation method provided by the invention comprises the following steps: carrying out substitution reaction on a compound a and a compound k under the catalysis of alkali to generate a compound b; performing substitution reaction on the compound c and the compound d under an alkaline condition to obtain a compound e; carrying out Mitsunobu reaction on the compound e and f to obtain an intermediate g, and carrying out coupling reaction on the compound g and b to generate a compound h. The invention provides the application of the compound shown in the formula I or salt, solvate, allomer, metabolite, nitric oxide and prodrug thereof in preparation of drugs for treating or preventing P2X3 and/or/P2X2/3 receptor related diseases. The dihydropyrimidine compound disclosed by the invention has a good P2X3 receptor antagonism effect and better safety.

Tetrahydroquinoline derivatives of general formula (I) or salts thereof, having a specific and strong binding affinity for AR and exhibiting AR agonism or antagonism; and pharmaceutical compositions containing the derivatives or the salts.

Disclosed is a novel compound that acts as an antagonist for P2X3 and/or P2X2/3 receptors. Also disclosed is a pharmaceutical composition that acts as an antagonist for P2X3 and/or P2X2/3 receptors, said composition containing: a compound represented by formula (I), a pharmacologically permitted salt thereof, or a solvate of either. In the formula, ring A represents a substituted or unsubstituted five-to-seven-membered cycloalkane, a substituted or unsubstituted five-to-seven-membered cycloalkene, or the like; C represents a carbon atom; -X- represents -N(R16)- or the like; R16 represents hydrogen, a substituted or unsubstituted alkyl, or the like; R7 represents a substituted or unsubstituted five- or six-membered heteroaryl or a substituted or unsubstituted six-to-ten-membered aryl; each of Q1 and Q2 independently represents a carbon atom or a nitrogen atom; -L- represents -O-, -S-, or the like; R6 represents a substituted or unsubstituted cycloalkyl, a substituted or unsubstituted cycloalkenyl, or the like; and R2 represents hydrogen, hydroxyl, or the like.

[Problems] Provided is a compound which has an antagonistic action on a muscarinic M₃ receptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.

[Means for Solving Problems] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic M₃ receptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic M₃ receptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic M₃ receptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.

This disclosure relates to binding agents with specificity for programmed cell death 1 (PD-1) and to methods for using the same to treat, prevent and/or ameliorate an infectious disease (e.g., human immunodeficiency virus (HIV)), cancer and/or autoimmunity. In addition, this disclosure identifies a novel binding patch (“P2”) on PD-1 that is linked with a previously unidentified functional activity of PD-1 that is distinct from the interaction site involved with either the PD-L1 or PD-L2 ligands. Furthermore, we demonstrate that antibodies that interact with this region of PD-1 are able to act as antagonists of PD-1 and that this antagonism is further enhanced with the addition of antibodies that act through the blockade of the PD-1/PD-L1/L2 interaction.

The invention provides an antagonistic peptide which can simulate the key sequence for bonding MD2 and LPS and competitively antagonize the specific bonding which is generated by LPS and MD2, thus achieving the mitigation of the excessive activation of the immune inflammatory cells of LPS and further easing the caused excessive septic damages to the body. The amino acid sequence of the antagonist peptide includes: a sequence 1 of Lys Thr Val Pro Asp Asn His; and the sequence 2 of Ile Gly Lys Phe Leu Tyr Arg. The peptide can effectively mitigate the septic inflammation damage which is induced by the intracellular toxin LPS, thus significantly improving the survival rate of mouses which are infected by the intracellular toxin and maintaining the body immune defense function at the same time of specifically inhibiting the excessive stimulation of the LPS on the inflammatory cells. The antagonistic peptide can be used for preparing the treatment drugs of the inflammatory diseases which are caused by gram-negative bacteria and are related to a toll-like receptor protein.

The invention provides a Korean pseudomonas and application thereof. The Korean pseudomonas is identified as Korean pseudomonas CJ-361, and the preservation number is CGMCC NO.12122. The Korean pseudomonas CJ-361 is obtained through separation from radix pseudostellariae rhizosphere soil by adopting a pseudomonas selectivity culture medium, an antagonistic experiment is performed on fusarium oxysporum and fusarium moniliforme separated to the radix pseudostellariae root lesion portion through an agar plate opposite culture method, and it is found that the Korean pseudomonas has the strong antagonism on the fusarium oxysporum and the fusarium moniliforme. Meanwhile, the invention provides the optimum culture medium for antagonistic bacterium growth, the optimum formula is 1/4LB+1/20MS (containing no ferric salt)+0.1 wt% brown sugar, and the fermented liquor has the obvious antagonistic effect. The antagonistic strain and the microbial agent thereof can effectively prevent and treat radix pseudostellariae root rot diseases, and the environment-friendly, ecological and safe biological prevention and control potential strain is provided for overcoming or relieving replantation diseases of radix pseudostellariae.

In a method comprising comparing a solid phase carrier extract 1 obtained by pre-treating a sample with a ligand-immobilized solid phase carrier and a solid phase carrier extract 2 obtained by treating the pretreated sample again with a ligand-immobilized solid phase carrier in terms of the proteins contained therein, and identifying a protein whose content is remarkably decreased in the extract 2 compared to the extract 1, 1) the problem of the solubility of subject ligand, 2) the problem of the non-specific protein-denaturing effect of the subject ligand added, and the like, which have been problematic in antagonism experiments in target search using an affinity resin, have been solved.

The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.