345 results about "Tricyclic" patented technology

The present application relates to a novel tricyclic derivative compound as a KRAS mutant protein inhibitor, and use thereof. The compound according to one embodiment of the present application inhibits the activity of a KRAS mutant protein and thus can be used in the prevention or treatment of diseases induced by KRAS mutation.

Disclosed are compounds of Formula I (shown below), methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.

Provided are a fused tricyclic compound, a preparation method therefor and a pharmaceutical use thereof. Specifically, provided are a compound as shown in general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof as a therapeutic agent, particularly a use as an RAS inhibitor and a use in the preparation of a drug for treating and / or preventing RAS-mediated or RAS-dependent diseases or disorders. The groups in general formula (I) are as defined in the description.

The present disclosure is directed to compounds of Formula I:and pharmaceutically acceptable salts thereof, and compositions thereof, as well as methods of treatment of cancers such as those involving WRN protein.

The present disclosure relates to tricyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR enzyme and are useful in the treatment of FGFR-associated diseases such as cancer.

The invention discloses a polyfunctional rosin-based reactive diluent. The structural formula of the polyfunctional rosin-based reactive diluent is shown as a formula (I) or a formula (II). The polyfunctional rosin-based reactive diluent has a rigid tricyclic diterpenoid structure of rosin, is small in molecular weight and low in viscosity, can be used for preparing an ultraviolet curing material, has excellent hardness and scratch resistance after light curing and film forming, and is simple in preparation method, low in cost and suitable for industrial production. And a polycarboxylic acid functional group is efficiently constructed under a mild condition.

The disclosure provides substituted nitrogen containing tricyclic compounds as PARP inhibitors and the use thereof. This disclosure provides compounds represented by Formula (I) as below, wherein, the ring Z, Z1, Z2, Z3, Z4, Z5, A1, A2, A3, L, m, n, ring B and Cy are defined herein. The compounds of Formula I of the present disclosure are PARP inhibitors and thus are useful in the treatment of diseases, disorders and conditions, such as cancer, responsive to the inhibition of PARP activity. The present disclosure also relates to a pharmaceutical composition comprising the compound of Formula I and the use of the compound of Formula I in the preparation of a medicament for the treatment or prevention of diseases or conditions responsive to the inhibition of PARP activity.

This invention provides an siRNA nucleic acid pesticide targeting the DICER2 gene to control rice blast fungus, belonging to the field of biotechnology. The siRNA molecule can delay and inhibit the formation of rice blast fungus appressoria, thereby reducing the pathogenicity of the fungus and providing a new method for controlling rice blast. When used in combination with tricyclazole or clotrimazole, it has a synergistic effect. The siRNA molecule targeting the DICER2 gene is prepared into a nucleic acid pesticide and sprayed on rice leaves, effectively reducing rice blast lesions and their area, thus enabling its use in rice blast control. Furthermore, it avoids the cumbersome process of cultivating genetically modified crops and addresses consumer concerns.

The invention relates to the technical field of medicines, in particular to fused tricyclic substituted isoxazolidinyl urea derivatives, pharmaceutically acceptable salts, stereoisomers, pharmaceutical compositions and application thereof. The structure of the fused tricyclic substituted isoxazolidinyl urea derivative is as shown in a formula (I). The fused tricyclic substituted isoxazolidinyl urea derivative disclosed by the invention has obvious TrkA kinase and cell inhibition activity and selective inhibition activity.

Disclosed are tricyclic fused heterocyclic compounds with PDE3 / 4 dual inhibition effect shown in formula (I), and stereoisomers, solvates, or pharmaceutically acceptable salts thereof, and use thereof in the preparation of drugs for treating / preventing PDE3 / 4 mediated diseases, wherein the groups in formula (I) are as defined in the specification.

The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

The application belongs to the field of genetic engineering and biosynthesis, and particularly relates to biosynthesis of a class of diterpenoids. The application provides genes having a key role in the formation of a 5-8-5 tricyclic mother nucleus and a five-membered heterocyclic ring in biosynthesis of the class of diterpenoids, which are respectively named as PrcA and PrcB and polypeptides encoded by the genes, expression of PrcA and PrcB is carried out through a heterologous expression system of Aspergillus oryzae, and five diterpenoids with novel structures and anti-metabolic related fatty liver disease activity are obtained. The application provides application of the polypeptides in biosynthesis of the class of diterpenoids, and enriches a diterpenoid library, thereby providing lead compound resources for discovering new anti-metabolic related fatty liver disease medicinal raw materials.

Disclosed in the present invention are a series of tricyclic compounds, and particularly disclosed are a compound shown in formula (I) or a pharmaceutically acceptable salt thereof.

A process for upgrading a pyrolysis oil comprising contacting a pyrolysis oil feed with hydrogen in a first fixed bed reactor in the presence of a mixed metal oxide catalyst wherein: the pyrolysis oil feed comprises a polycyclic aromatic hydrocarbon compound comprising greater than or equal to 16 carbon atoms; and contacting the pyrolytic oil feedstock with hydrogen in the presence of a mixed metal oxide catalyst in a first fixed bed reactor to convert at least a portion of the polycyclic aromatic hydrocarbon compounds in the pyrolytic oil feedstock into bicyclic aromatic hydrocarbon compounds, tricyclic aromatic hydrocarbon compounds, or both, passing the intermediate stream comprising the bicyclic aromatic compound, the tricyclic aromatic compound, or both to a second fixed bed reactor downstream of the first fixed bed reactor; and contacting the intermediate stream with hydrogen in the presence of a mesoporous supported metal catalyst in a second fixed bed reactor.

The present invention relates to pharmaceutical compounds of formula (I) and pharmaceutical compositions containing said compounds, processes for the preparation of said compounds, and the use of said compounds as inhibitors of cyclin-dependent kinase 7 (CDK7), and their use in the treatment of diseases, such as cancer. [Formula 1] TIFF2023554673000617.tif33128

Provided are novel chiral aromatic diazatricyclo-compounds and pharmaceutically acceptable salts thereof, that are smooth muscle myosin 2 specific inhibitors useful for the treatment of ischemic events and conditions associated with capillary no-reflow, or other smooth-muscle related symptoms.

The invention belongs to the technical field of pesticides, and relates to 11 bactericide compositions for mainly preventing and treating crop diseases caused by pyricularia oryzae and colletotrichum gloeosporioides. The compound YJY-22 provided by the invention is novel in structure and unique in action mode, and has no cross resistance with isoprothiolane, fenoxanil, pyraclostrobin, tricyclazole, azoxystrobin, mancozeb, captan, difenoconazole, prochloraz, chlorothalonil and tebuconazole. As the action mechanism of the compound YJY-22 is different from that of the medicament, and the compound YJY-22 and the medicament have no cross resistance, the compound YJY-22 and the medicament are compounded, so that the sterilization range can be expanded, the sterilization effect can be enhanced, the drug resistance of phytopathogen can be delayed, the safety to crops is good, the prevention and control spectrum is expanded, and the requirements of pesticide reduction and synergism are met.

The present invention relates to a process for stereoselective polyene cyclization to produce tricyclic compounds of formula (I), wherein X is CH2or C=O, comprising reacting a compound of formula (II), wherein X is CH2or C=O and wherein the curved line indicates the E- or Z-configuration, in the presence of a catalytic amount of a Bronsted acid having an acidic sulfonamide moiety.(I)(II)

A 2-[2-({12,12-dimethyl-4-oxo-6-phenyl-3,11-dioxatricyclo[8.4.0.0,2,7]tetradeca-1,5,7,9-tetraen-8-yl}oxy)acetamido]benzamide compound and related derivatives, as well as the use thereof in the preparation of a medicament for treatment and / or prevention of diseases or disorders associated with the circadian rhythm are provided. The compound of the invention is a CLOCK-binding small molecule and also an inhibitor of CLOCK:BMAL1 interaction, and is therefore useful, as pharmaceutical agent, especially in the treatment and / or prevention of disorders associated with the circadian rhythm.

The invention relates to a tricyclic heterocyclic compound as well as a preparation method and medical application thereof. Specifically, the invention relates to a compound shown in a general formula (I), a preparation method of the compound, a pharmaceutical composition containing the compound and application of the compound as an MAT2A inhibitor. The compound and the pharmaceutical composition containing the compound can be used for treating and / or preventing diseases related to MAT2A activity, such as mesothelioma, neuroblastoma, rectal cancer, colon cancer, esophageal cancer and the like. Wherein the definition of each group in the general formula (I) is the same as that in the specification.

The invention provides a preparation method of 1-chloromethyl silazane, and relates to the technical field of chemical synthesis. The method specifically comprises the following steps: (1) adding a first catalyst and chloromethyl trichlorosilane into a mixed material containing an auxiliary solvent and a reactive solvent, and reacting to obtain a first material; the reactive solvent is a C1-C6 alcohol solvent; (2) distilling to remove hydrogen chloride in the first material to obtain a second material; (3) adding a catalyst alkali and a surfactant into the second material, and then adding triethanolamine for reaction; and precipitating the reacted material through an anti-solvent to obtain the high-purity 1-chloromethyl silatrane. The 1-chloromethyl silazane can be prepared by a one-pot method, and the second-stage reaction is directly carried out without separation and purification after the first-stage reaction is completed, so that the intermediate loss is reduced, and the yield of the target product is increased. According to the whole preparation method, the technological process is greatly simplified, operability is high, industrial production is easy, and important economic value is achieved.

The present application is concerned with tricyclic pyrimidinones as inhibitors of WRN, as well as pharmaceutical compositions and methods of use related thereto. The compounds are useful in treating, preventing, or ameliorating diseases or disorders such as cancer or infections.

This invention discloses a sophoridine tricyclic derivative or its pharmaceutical salt, with the following general structural formula: R1 is selected from hydrogen, C1-C20 straight-chain alkyl, and C1-C20 branched alkyl. In vitro experiments have verified that the sophoridine tricyclic derivative can inhibit TGF-β-induced activation of hepatic stellate cells, improve CCl4- and bile duct ligation-induced liver injury and liver fibrosis in mice, inhibit TGF-β / Smads signaling pathway activation, and also inhibit diethylnitrosamine-induced primary liver cancer in mice. Therefore, this invention provides new evidence for the treatment, alleviation, or improvement of liver fibrosis or primary liver cancer using sophoridine tricyclic derivatives.

A method for reducing or preventing corrosion or fouling in an apparatus for carrying out a chemical process, where corrosion or fouling is caused by acidic compounds present in the chemical process, which comprises the addition of at least one quaternary ammonium hydroxide of the formula (I) to the apparatus, wherein the chemical process is carried out: [Chem. 1] where R1, R2, R3 are each independently C1-C10 alkyl; R4 is inter alia C1-C18 alkyl, benzyl, monocycloalkyl having 5, 6, 7 or 8 carbon atoms, bicycloalkyl having 6 to 8 carbon atoms, tricycloalkyl having 7 to 10 carbon atoms, where monocycloalkyl, bicycloalkyl and tricycloalkyl are unsubstituted or substituted by 1 or 2 methyl groups, or tri-C1-C4 alkyl ammonium groups. R1 and R2 together with the nitrogen atom may also form a 5 or 6-membered, saturated nitrogen heterocycle, which is unsubstituted or carries 1 or 2 methyl groups; and / or R3 and R4 together with the nitrogen atom may also form a 5 or 6-membered, saturated nitrogen heterocycle, which is unsubstituted or carries 1 or 2 methyl groups.

This invention discloses a heterozygous sesquiterpene tricyclic epoxy compound derived from the strain *Arthrum oligosporum*, its preparation method, and its applications, belonging to the field of natural product chemistry. This invention provides a heterozygous sesquiterpene tricyclic epoxy compound derived from *Arthrum oligosporum* (… A.oligospora ) AOL_ s00210g57 Anthrobotrisin D, a novel heterozygous sesquiterpene tricyclic epoxy compound from a gene knockout strain, has been shown in vitro to possess excellent anti-inflammatory activity, significantly inhibiting lipopolysaccharide-induced inflammatory responses in mouse microglia. It exhibits a clear dose-dependent inhibitory trend at multiple levels, including NO release, protein and mRNA expression of inflammatory factors (TNF-α, IL-1β, IL-6), and iNOS protein and mRNA expression. Furthermore, at a concentration of 33 μM, its anti-inflammatory effect is comparable to that of the clinically proven positive drug dexamethasone, and in some aspects, it is even superior. This invention not only provides a new lead compound for the development of anti-inflammatory drugs but also opens up new directions for developing new drugs from the unique microbial resource of nematode-preying fungi.

An object of the present invention is to provide a solid-phase carrier for nucleic acid synthesis, in which a nucleic acid and an adduct can be easily separated by HPLC in a case where the nucleic acid is synthesized using the solid-phase carrier for nucleic acid synthesis and the nucleic acid is cut out, a compound which serves as a linker of the solid-phase carrier, a compound which serves as a precursor of the linker, and a method for producing a nucleic acid using the solid-phase carrier. The compound according to the embodiment of the present invention is a compound represented by the following general formula (1).In the general formula (1), Ar represents a tri- to tetracyclic aromatic ring which may have a substituent, Z represents a hydrogen atom or a protective group eliminable by an acid, and R1 to R4 each independently represent a hydrogen atom, an alkyl group, or an alkoxy group.

The present invention addresses the problem of providing a method for producing TCD-DA having less impurities generated as by-products, by depositing materials in a reactor in a batch and performing a hydroformylation rection at a low pressure.　The method for producing tricyclodecane dialdehyde is characterized by depositing a catalyst, dicyclopentadiene, and a solvent in a reactor in a batch, increasing the pressure to 2.0-4.0 MPaG by means of a gas mixture of hydrogen and carbon monoxide, and performing a hydroformylation reaction in the gas mixture in which the molar ratio of hydrogen : carbon monoxide is 90:10 to 100:99.

Provided are a series of substituted tricyclic derivatives and the use thereof. Specifically provided are compounds represented by formula (II), (I-1) or (I-2), stereoisomers thereof and pharmaceutically acceptable salts thereof.