53 results about "Tryptase.beta" patented technology

Provided herein are novel and useful compounds having a tryptase inhibition activity, pharmaceutical compositions comprising such compounds, and methods treating subjects suffering from a condition, disease, or disorder that can be ameliorated by the administration of an inhibitor of tryptase, e.g., asthma and inflammatory diseases, to name only a few.

A sensitive bioluminescent assay to detect proteases including caspases, trypsin and tryptase is provided.

The present invention provides compositions and methods for detection, diagnosis, treatment and / or prevention of chronic pelvic pain syndrome. In particular, the present invention provides biomarkers of chronic pelvic pain syndrome (e.g., mast cell markers (e.g., tryptase)), and / or inhibition of mast cell function (e g inhibition of MCP-1 and / or MIP-1α) to treat or prevent chronic pelvic pain syndrome.

The invention is directed to synthetic polypeptide substrates for tryptase enzymes and assays for tryptase activity that utilize the synthetic polypeptide substrates. The preferred synthetic polypeptide substrates are tetramers of the formula P4-P3-P2-P1, wherein the substrate is selected from the group consisting of P-R-N-K (SEQ. ID. NO: 2), P-K-N-K (SEQ. ID. NO: 3), P-R-N-R (SEQ. ID. NO: 4), P-K-N-R (SEQ. ID. NO: 5), P-A-N-K (SEQ. ID. NO: 6), and P-R-T-K (SEQ. ID. NO: 7).

This invention is directed to processes for the preparation of a compound of the formula I or salt thereof,that is useful as a tryptase inhibitor, to intermediates useful in the preparation of such a compound, to processes for the preparation of such intermediates, and to the use of such intermediates for the preparation of such a compound.

The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.

A sensitive bioluminescent assay to detect proteases including caspases, trypsin and tryptase is provided.

The invention relates to a special nutrient liquid preparation for hatching penaeus vannamei and a preparation method of the special nutrient liquid preparation. The liquid preparation comprises bacillus pumilus of which the preservation number is CCTCC M 2013240, magnesium, zinc, copper, cobalt, vitamin A, vitamin D, vitamin E, vitamin B1, vitamin B2, vitamin C, stomach protease and tryptase. The invention further provides the preparation method of the special nutrient liquid preparation. The special nutrient liquid preparation has the advantages that the nutrients are comprehensive and balanced, the survival rate and the growth speed of penaeus vannamei are increased, and the disease is reduced. The preparation method of the special nutrient liquid preparation provided by the invention is simple in process and high in raw material utilization rate.

The present invention discloses and claims a series of substituted tropinone benzylamines of formula (I):The compounds of this invention are inhibitors of β-tryptase and are, therefore, useful as pharmaceutical agents. Additionally, this invention also discloses methods of preparation of substituted tropinone benzylamines.

The present invention provides a purified expressed δ tryptase polypeptide or fragment or analogue thereof, in particular, the human δ tryptase polypeptide or fragment or analogue thereof. The present invention also provides variants of such polypeptides. The invention further relates to methods of diagnosing disease states based on expression of these polypeptides and methods of screening for compounds that interact, bind and / or modulate the activity of the polypeptides.

Apparatus, implanted subcutaneously or in muscle, fat, joint spaces, or body cavities of any type, detects and responds to an allergic and / or anaphylactic reaction. Detection is carried out by monitoring the levels of biomarker molecules that indicate the occurrence of an allergic and / or anaphylactic reaction, such as: histamine, leukotrienes, prostaglandins, cytokines, tryptase, Fc-ε-RI complexes, anaphylatoxin C3a, chymase, carboxypeptidase A, platelet-activating factor8, other mast cell degranulation byproducts, or other basophil activation compounds. An appropriate dosage of medication (such as epinephrine, antihistamines, or steroids) is automatically dispensed to mitigate the allergic / anaphylactic response. The simplicity and ease of use of the invention has the potential to save many lives worldwide, while dramatically mitigating the risks of the current methods of handling severe allergic reactions using external auto-injectors. 8 Sala Cunill, A., Cardona, V. Biomarkers of anaphylaxis, beyond tryptase. Current Opinion in Allergy and Clinical Immunology. Vol 15(4), August 2015, p 329-336. Doi: 10.1097 / ACI.0000000000000184.

The invention relates to an establishment method of a zebra fish allergy detection model, and provides a method for evaluating injection (including adjuvant materials) allergenicity by the model simultaneously. The establishment method of the model mainly comprises the following steps: determining reaction concentration of Tryptase detection substrate BAPNA; determining a developmental stage of zebra fish; determining the quantity of the zebra fish for detection; determining concentration of positive control Compound 48 / 80, performing microwell plate analysis; and performing statistical analysis. The application of a living zebra fish model for evaluation of the injection (including the adjuvant materials) allergenicity has the advantages of reliability, fastness, efficiency, cheapness, high cost performance and the like, and high-throughput evaluation for the injection (including the adjuvant materials) allergenicity in vivo can be realized; and the establishment method and the application of the zebra fish allergy detection model has important significance on the injection (including the adjuvant materials) safety evaluation.

The present invention provides a biosensor preparation method based on ferritin-encapsulated Ir(ppy)3, and belongs to the technical field of novel nanomaterials and biosensing. According to the methodprovided by the present invention, a pH-guided protein depolymerization / recombination method is used to encapsulate a large number of tris(2-phenylpyridyl)firpic Ir(ppy)3 molecules in the apoferritinFt to obtain Ft-Ir(ppy)3 as an electrochemiluminescence ECL energy donor, the surface of the glassy carbon electrode modified with nanogold is taken as an ECL energy acceptor, and based on the excellent ECL performance of Ir(ppy)3 and the ECL resonance energy transfer principle with nanogold, a biosensor preparation method with a simple preparation, a low cost, low reaction energy consumption, green environmental protection and high sensitivity is proposed for the first time; the method is applied to the actual sample detection of tryptase, the detection limit is as low as 1.3 fg / mL, and thelinear range is as wide as 5 fg / mL-100 ng / mL; and the method has high sensitivity, good reproducibility, and large potential application value.

The present invention is to provide an imidazolidinedione derivative and oxazolidinedione derivative represented by the following general Formula (I) having the chymase and / or tryptase inhibition activity [wherein R1 and R2 are the same or different, and denote a lower alkyl group or a phenyl group, or R1 and R2 are taken together to form a ring, R3 denotes an optionally substituted naphthyl group or heterocyclic group, A denotes oxygen or NR4 (R4 is hydrogen or optionally substituted lower alkyl group), or NB2R5 (R5 is aryl group, and B2 is carbonyl group or sulfonyl group), and B1 denotes a carbonyl group or a sulfonyl group], or a pharmaceutically acceptable salt thereof.

The present invention relates to an improved process for obtaining a precursor of an insulin or insulin derivative having correctly bonded cystine bridges in the presence of cysteine or cysteine hydrochloride and chaotropic auxiliary.

The invention relates to a non-self-cutting trypsin and preparation method thereof. The invention provides a trypsin mutant, and compared with a wild type, the stability of the mutant is better. The present invention also provides a method of methylation modification of the trypsin mutant, so that the trypsin effectively avoids the generation of self-cutting.

The invention provides a farm-oriented insecticidal active compound having activating effect on insect trypsin, namely periplocoside P and belongs to the technical field of pesticides. A structural formula of the active compound is shown as follows: an IUPAC chemical name is delta5-pregnen-3beta,17alpha-dyhydroxy-,20(S)-oxygen-(2-O-acetyl-beta-D-digitalose(1-4)-beta-D-cymarose-(1-4)-beta-D-cymarose-(1-4)-beta-D-digitoxose-(1-4)-((1-5)-3,7-dideoxy-4-O-methyl-alpha-D-glucose-2-heptulose(2,4)-dyhydroxy-(1-3)-beta-D-cymarose). The compound selectively has strong stomach toxicity insecticidal activity on cabbage caterpillar, diamond back moths and beet armyworms, has activation on tryptase of insects to be tested and can be processed into a farm-oriented insecticidal preparation.

The invention provides a method for obtaining insulin or insulin derivatives correctly boned with cystine bond from the prosoma of the insulin or insulin derivatives. The prosoma undergoes a folding process from the presence of cysteine or cysteine hydrochloride and off-fluid additive, after the folding, the insulin or insulin derivatives are obtained from the prosoma by a method that: enzyme cleavage are carried on by selecting trypsinase or tryptase and optional selecting carboxypeptidase B, then purifications are carried out on polymeric adsorbent.

This invention is directed to processes for the preparation of compounds of the formula I and their salts, <CHEM> which are useful as tryptase inhibitors, to intermediates useful in the preparation of such compounds, to processes for the preparation of such intermediates, and to the use of such intermediates for the preparation of such compounds.

Compounds having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein A, A', B, X, Y, R2, R3, R4 and R5 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing such compounds, are tryptase antagonists.

The invention relates to the enzyme catalysis / enzyme inhibition biotechnological field, in particular to a test method for activity of a trypsin inhibitor. The particular test process is mainly that: a trypsin inhibitor extract and a trypsin action substrate are respectively added into a trypsin reaction system; after reaction for 10 to 15 minutes, reaction stopping solution is added, and then absorbance of the reaction stopping solution in the wavelength of 410 nautical miles is measured; a curve is drafted according to addition and the absorbance of the inhibitors; the activity of the trypsin inhibitor is determined; wherein, the trypsin action substrate is BAPNA solution and the addition is 0.5 to 1.0 milliliters per milliliter trypsin reaction system. The invention has the advantages of simple instruments used, convenient operation and high reaction sensitivity, and is suitable for testing activity of various trypsin inhibitors.

The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.

The invention relates to special nutrient powder for penaeus vannamei boone. The nutrient powder is prepared by mixing the following raw materials: magnesium, zinc, copper, cobalt, vitamin A, vitamin D, vitamin E, vitamin B1, vitamin B2, vitamin C, pepsase, tryptase, grease and the balance of wheat middling. Furthermore, the invention provides a preparation method of the nutrient powder. The nutrient powder disclosed by the invention can be used for improving the problems of penaeus vannamei boone feed currently sold on the market that the feed is incomprehensive in nutrition, and is deficient or unreasonable in the dosages of vitamin, mineral elements, enzyme and the like. If the nutrient powder disclosed by the invention is added to normal penaeus vannamei boone feed sold on the market, the survival rate and growth speed of the penaeus vannamei boone are improved, and diseases are reduced.

The invention is directed to synthetic polypeptide substrates for tryptase enzymes and assays for tryptase activity that utilize the synthetic polypeptide substrates. The preferred synthetic polypeptide substrates are tetramers of the formula P4-P3-P2-P1, wherein the substrate is selected from the group consisting of P-R-N-K (SEQ. ID. NO: 2), P-K-N-K (SEQ. ID. NO: 3), P-R-N-R (SEQ. ID. NO: 4), P-K-N-R (SEQ. ID. NO: 5), P-A-N-K (SEQ. ID. NO: 6), and P-R-T-K (SEQ. ID. NO: 7).

The present invention provides compositions and methods for detection, diagnosis, treatment and / or prevention of chronic pelvic pain syndrome. In particular, the present invention provides biomarkers of chronic pelvic pain syndrome (e.g., mast cell markers (e.g., tryptase)), and / or inhibition of mast cell function (e.g. inhibition of MCP-1 and / or MIP-1α) to treat or prevent chronic pelvic pain syndrome.

This invention relates to compounds of formulawhich inhibit Factor Xa or tryptase, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa or tryptase.

The present invention relates to novel protease inhibitor proteins that have been identified in ticks. These proteins may be used as components of vaccines, as inhibitors of mast cell tryptase, in detection of mast cells and in the isolation and purification of mast cell tryptase. The invention also relates to the control of diseases and injury caused by parasites in animals and humans and to the use of the proteins of the invention in the treatment of certain diseases and allergies.