338 results about "Activity inhibition" patented technology

The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formulae: wherein: J is independently —O— or —NR^N1−; R^N1, if present, is independently —H or a substituent; R^N2 is independently —H or a substituent; Y is independently —CH═ or —N═; Q is independently —(CH₂)_j-M-(CH₂)_k— wherein: j is independently 0, 1 or 2; k is independently 0, 1, or 2; j+k is 0, 1, or 2; M is independently O—, —S—, —NH—, —NMe-, or —CH₂—; each of R^P1, R^P2, R^P5, and R^P4 is independently —H or a substituent; and additionally R^P1 and R^P2 taken together may be CH═CH—CH═CH—; and additionally R^P1 and R^P5 taken together may be CH═CH—CH═CH—; L is independently: a linker group formed by a chain of 2, 3, or 4 linker moieties; each linker moiety is independently CH₂—, —NR^N—, —C(═X)—, or —S(═O)₂—; either: exactly one linker moiety is —NR^N—, or: exactly two linker moieties are —NR^N—; either: exactly one linker moiety is —C(═X)—, and no linker moiety is —S(═O)₂—, or: exactly one linker moiety is —S(═O)₂—, and no linker moiety is —C(═X)—; no two adjacent linker moieties are —NR^N—; X is independently ═O or ═S; each R^N is independently —H or a substituent; A is independently: C_6-14carboaryl, C_5-14heteroaryl, C_3-12carbocyclic, C_3-12heterocyclic; and is independently unsubstituted or substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.

This invention provides methods for the use of substituted indole compounds of the general formula:

and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A₂ enzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.

The invention discloses a Paenibacillus kribbensis, and a preparation method and an application thereof. The Paenibacillus kribbensis has a bacterial code name of TRCC82001, is preserved in China General Microbiological Culture Collection Center, and has a preservation number of CGMCCNo.7996. The above bacterial strain has the advantages of good production property, good metabolite antimicrobial effect, and strong activity against rice blast and sheath blight, and a solution obtained after diluting a broth subjected to antibiotic treatment to 100 times has an inhibition effect of above 80% on the rice blast and sheath blight. The bacterial strain and its metabolites have a broad antimicrobial spectrum, can be used for preparing biocontrol preparations for the broad spectrum activity inhibition of pathogenic fungi to control the fungal diseases of plants.

The invention provides a magnetic molecularly imprinted nano-particle as well as a preparation method and an application thereof. The nano-particle can perform specific recognition, trapping, separation and activity inhibition on target protein in a solution in vitro, more importantly, the nano-particle can enter a living cell rapidly under the action of a magnetic field and perform in-situ combination and activity inhibition on the target protein in the living cell, distribution of the nano-particles in the cell can be traced through a fluorescence microscope after fluorescence labeling, and quantitation can be performed through detection of fluorescence intensity.

The present invention provides an anti-PAC1 monoclonal antibody capable of recognizing a PAC1 having a native structure, a PAC1 activity regulator (in particular, activity inhibitor) containing the antibody, a prophylactic/therapeutic agent for a disease associated with accentuation of a bioactivity of PAC1, containing the antibody, a diagnostic reagent for a disease associated with an abnormality of PAC1 activity, containing the antibody, and a screening method for a substance that regulates the expression of PAC1, using the antibody and a PAC1-expressing cell.

The present invention relates to compounds which are inhibitors of the activity of Complex III of the mitochondrial electron transport chain and pharmaceutical compositions comprising said compounds alone or in combination with other active agents. The present invention further relates to use of the compounds of the invention as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit. More particularly the present invention relates to the use of the compounds of the invention in a method of treating and/or preventing cancers presenting tumor-initiating cells. (Formula I) (I)

The invention discloses a Chinese medicinal herb extract with the function of inhibiting the activity of lipase and the new application thereof. The Chinese medicinal herb extract refers to one of water extract and/or alcohol extract of 61 Chinese medicinal herbs.

The invention relates to the field of algae inhibitors, the invention specifically relates to a sesquiterpene alcohol compound derived from algal epiphytic fungus, a preparation method thereof and anapplication of the sesquiterpene alcohol compound in the aspect of inhibiting microalgae. The specific structural formula is shown in the formula (I). The preparation method comprises the following steps: inoculating a fungal culture medium with Trichoderma virens Y13-3 for fermentation culture, and subjecting a fermentation product to separating and purifying, and the product is namely a sesquiterpene alcohol compound as shown in the formula (I). The median inhibition concentration of the sesquiterpene alcohol compound to the microalga can be up to 1.2 microgram/ml through the microalga activity inhibition experiment.

The invention relates to an inhibitor for preventing browning of a cut vegetable, comprising the following components: one of solvent water and ethanol or mixture thereof; one of sodium alginate, xanthan gum, carrageenan and chitosan, one or more of sodium tripolyphosphate, sodium pyrophosphate and 6-sodium metaphosphate, one or more of phytic acid, ascorbic acid, cinnamic acid, citric acid, kojicacid and edible acetic acid, and one or more of potassium sorbate, sodium dehydroacetate, sodium chloride and 4-hexylresorcinol. The inhibitor is used by soaking, and the soaking time varies with thetemperature and the air pressure of the processing environment. All the components used in the inhibitor are permitted in the GB2760-2007 (hygienic standards of food additives), and the inhibitor issulfite-free, safe and non-toxic, and can be used for fresh cut vegetables and can play the multiple roles of pH regulation, enzyme activity inhibition, oxygen removal and isolation and water retention to effectively prevent browning and play a role of anticorrosion and refreshment.

The present invention discloses a telomerase activity detection kit and a detection method thereof. According to the kit, a ternary linking structure probe is adopted to recognize a telomerase product, and a ternary linking structure triggered DNA molecule machine and a base stacking triggered DNA molecule machine are combined to achieve isothermal cascade nucleic acid amplification to convert a reverse transcription event of the telomerase in a tumor cell extract into a significantly-enlarged fluorescence detection signal so as to precisely determine telomerase activity in a trace amount of tumor cells and achieve detection on tumor cell telomerase activity inhibition by chemical drugs.

The present invention pertains to certain pyrazines and pyridines, and derivatives thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formulae: (I) wherein: Q is independently —N═ or —CH═; one of R^P2 and R^P3 is independently a group of the formula -J¹-L¹-Z; wherein: if Q is —N═, then -J¹-L¹-Z is independently: —NH-Z; —O-Z; or S-Z; if Q is —CH═, then -J¹-L¹-Z is independently: —NH—(CH₂)_n-Z, wherein n is independently 0 or 1; —O-Z; or —S-Z; Z is independently: C_6-14 carboaryl, C_5-14 heteroaryl, C_3-12carbocyclic, C_3-12 heterocyclic; and is independently unsubstituted or substituted; the other of R^P2 and R^P3 is independently —H, —NHR^N1, or —NHC(═O)R^N2; wherein: R^N1, if present, is independently —H or aliphatic saturated C_1-4alkyl; R^N2, if present, is independently —H or aliphatic saturated C_1-4alkyl; one of R^P5 and R^P6 is independently a group of the formula —W—Y; wherein: W is independently: a covalent bond; —NR^N4—, —O—, —S—, —C(═O)—, —CH₂—; —NR^N4—CH₂—, —O—CH₂—, —S—CH₂—, —C(═O)—CH₂—, —(CH₂)₂—; —CH₂—NR^N4—, —CH₂—O—, —CH₂—S—, or —CH₂—C(═O)—; wherein R^N4, if present, is independently —H or aliphatic saturated C_1-4alkyl; Y is independently: C_6-14carboaryl, C_5-14heteroaryl, C_3-12carbocyclic, C_3-12heterocyclic; and is independently unsubstituted or substituted; the other of R^P5 and R^P6 is independently —H; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, e.g., both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.

The invention belongs to the field of medicinal chemistry, and in particular relates to fluoroquinolone derivatives and an application thereof. The compounds shown in a formula (I) are obtained by structural modification of fluoroquinolone medicines. The compounds provided by the invention can not only treat the infection caused by mycobacterium tuberculosis and common bacteria, but also can has activity inhibition effects on bacterial persister, citrus pathogenic bacteria, nicotinamide N-methyltransferase (NNMT) and interleukin IL-17 PPI; and the compounds have a simple and easy preparation process and mild conditions, a plurality of the compounds with enhanced antibacterial activity, improved water solubility and reduced toxic and side effects are obtained, and the compounds are expectedto reduce the dosage, shorten the treatment cycle and improve patient compliance, thereby providing novel molecular types and research ideas for medicines of tuberculosis and other diseases.

The invention relates to a tyrosinase polypeptide inhibitor, which consists of a polypeptide. In the polypeptide, one or more amino acids are further subjected to acetylation, amidation, formylation, hydroxylation, lipolyzation, methylation or phosphorylation modification. The tyrosinase inhibitor provided by the invention can be taken as a medical composition, comprises the polypeptide, and further comprises a pharmaceutically-acceptable supporting agent. The medicinal composition provided by the invention can be used for inhibiting the generation of black pigments under the action of activity inhibition of tyrosinase, and can be widely applied to cosmetics such as a whitening agent.

This invention discloses a method of using gene recombination technology to prepare telomerase activation profiling. This invention can prepare telomerase activation profilin which is high purity and high biologic activity with high efficiency and large scale.

Provided are compositions and methods for modulating cardiac cell hypertrophy and hyperplasia using inhibitors of c-Kit activity.