145 results about "Chymase" patented technology

According to this invention, there is provided an indole derivative having the general formula (I) wherein A is an oxygen atom or a nitrogen atom which nitrogen atom is optionally substituted with an alkyl group, and (i) R1 and R2 each stand for a hydrogen atom or an alkyl group, independently, or (ii) R1 and R2 as taken together form a cycloalkyl group or an aromatic ring, or (iii) R1 and R2 as taken together form a heterocyclic ring, and R3 is a hydrogen atom, a (C1-C10)alkyl group or others, R4 is a substituted alkyl group and R5 is a hydrogen atom, a halogen atom, an alkyl group or an alkoxy group and so on, as novel compounds by a novel chemical synthetic process. The indole derivative of formula (I) exhibits a useful chymase inhibitory activity.

Apparatus, systems and methods for measurement of B22 values of proteins in aqueous solutions in flow-mode utilize a dual-detector cell are provided. Simultaneous measurement of protein concentration and scattered light intensity is facilitated as the protein elutes from a size-exclusion column. Each data point on the resulting chromatograms is converted to Rayleigh's ratio, Rθ, and to concentration c, respectively. The B22 value is calculated from the slope of the Debye plot (Kc / Rθ versus c) generated from a range of the concentrations obtained from these chromatograms for a single protein injection. Measurements may be analyzed using modeling data derived from a predetermined modeling equation to quantify self-association of molecules. The apparatus and method provide a reliable means for determining B22 values for such proteins as lysozyme, chymotrypsinogen, and chymotrypsin in various solution conditions.

The invention relates to a purifying process for chymotrypsin, which belongs to the field of chymotrypsin in a bio-pharmaceutical technology. The purifying process comprises the following steps of: pulping; salting out, and filtering; adding ammonium sulfate till the saturation degree is 0.4, and standing in a cold chamber over night; filtering and performing ultrafiltration by using an ultrafiltration film of 50kDa; performing ultrafiltration by using an ultrafiltration film of 50kDa; adding ammonium sulfate into a filtrate till the saturation degree is 0.7, and standing at a low temperature over night; filtering and crystallizing; activating; precipitating; performing ultrafiltration by using an ultrafiltration film of 10kDa; purifying with an SP ion exchange column; and performing ultrafiltration by using an ultrafiltration film of 10-30kDa, and sterilizing to obtain the chymotrypsin. In the process, the chymotrypsin is purified by combining the ultrafiltration film with the ion exchange column, so that a good purifying effect is achieved, and an obtained product has high purity; and the chymotrypsin obtained through the process has high activity which is more than 1500 U / mg, the dosage can be reduced, the medical expense of a patient is reduced, the administration safety of the chymotrypsin is improved.

A method of treating weight loss due to underlying disease in a patient, the method comprising administering to the patient an effective amount of an agent which reduces sympathetic nervous system activity. A method of treating weight loss due to underlying disease in a patient the method comprising administering to the patient an effective amount of any one or more of the following: a compound which inhibits the effect of aldosterone such as an aldosterone antagonist; a chymase inhibitor; a cathepsin B inhibitor; a β receptor blocker; an imidazoline receptor antagonist; a centrally acting α receptor antagonist; a peripherally acting α receptor antagonist; a ganglion blocking agent; a drug that has an effect on cardiovascular reflexes and thereby reduces SNS activity such as an opiate; scopolamine; an endothelin receptor antagonist; and a xanthine oxidase inhibitor. The methods are particularly useful in treating cardiac cachexia.

An agent for improving abnormal glucose tolerance or a preventive and / or a remedy for diseases caused by abnormal glucose tolerance containing a chymase inhibitor as the active ingredient. Examples of the diseases caused by abnormal glucose tolerance include diabetes and / or complications of diabetes. Examples of the complications of diabetes include diabetic nephropathy, diabetic retinopathy, diabetic peripheral neuropathy, hyperinsulinemia, insulin resistance syndrome, arteriosclerosis, acute coronary syndrome, arteriosclerosis obliterans, vasculitis, brain infarction, hypertension, renal insufficiency, neuropathy, nephritis, renal aneurysm, renal infarction, obesity and so on.

Disclosed herein is the use of HLM-008182, as well as its analogues formed via in-house synthesis, as a potent proteasome inhibitors. A new method was developed for HLM-008182 through a four-step protocol and the method was further optimized to a two step protocol. The synthesis in both protocols was regioselective with TiCl4. The reaction was highly efficient with microwave assisted heating and THF as solvent. The modification around the molecule HLM-008182 established primary SAR, indicating that the proteasome inhibition activity was a function of the 2-side chain.