37 results about "Phthalazines" patented technology

The present invention is directed to (phthalazin-3-yl)amine derivatives of formula (I) as BFL-1 inhibitors for use in methods of treatment of leukemias, lymphomas and other cancers.

The invention relates to compounds of formula (Ia) and to their use in treating or preventing an inflammatory disease, a disease associated with an undesirable immune response, cancer, obesity, a diabetic disease or a blood disorder:wherein RA, RB, RC and RD, X, Y1, Y2, Y3, Z1, Z2 and m are as defined herein.

The invention relates to a method for catalytically synthesizing 2, 4-disubstituted phthalazine 1-(2H)-ketone from 1, 5, 7-triazabicyclo [4.4. 0] dec-5-ene. According to the method, 3-alkenyl phthalide and hydrazine compounds are taken as initial raw materials, TBD which is low in price and easy to obtain is taken as a catalyst, sodium tert-butoxide is taken as alkali, reaction is carried out at room temperature, and the 2, 4-disubstituted phthalazine 1-(2H)-ketone is obtained at high yield. According to the method, the cheap TBD is adopted as the catalyst, the reaction is carried out under the room temperature condition, and compared with a traditional reaction strategy, the economic cost is greatly reduced, the steps are simple, heating and a transition metal catalyst are not needed, operation is convenient, the yield is high, the cost is low, and good economic benefits are achieved.

The invention relates to the field of preparation of drug intermediates, and particularly discloses a synthetic method of a drug intermediate pyrazolo [1, 2-b] phthalazine-5, 10-diketone derivative and a catalytic system for synthesis. According to the synthetic method, aromatic aldehyde, phthalylhydrazine and malononitrile are used as reaction raw materials; the pyrazolo [1, 2-b] phthalazine-5, 10-diketone derivative is synthesized under the catalytic action of a catalytic system consisting of an alkaline eutectic solvent and absolute ethyl alcohol. The content of each component and reaction process parameters are optimally designed, so that the utilization rate of the reaction raw materials and the yield of the pyrazolo [1, 2-b] phthalazine-5, 10-diketone derivative can be remarkably increased, and the economical efficiency is relatively good; the catalytic system is high in catalytic activity, the usage amount in the catalytic process and the loss amount of the catalyst during recycling are small, the number of times of recycling is large, the catalytic system does not need to be treated before recycling, and operation is easy.

A method for treating Ewing's sarcoma in a subject, comprising administering to a subject in need thereof a therapeutically effective amount of (E)-3-(2-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)pyrimidin-5-yl)-N-hydroxyacrylamide or a pharmaceutically acceptable salt thereof.

The present invention relates to the technical field of adhesives and discloses a flame-retardant polyurethane adhesive for reflective heat-resistant stickers. The adhesive comprises organophosphorus-modified polyethylene glycol, phthalazine-modified epoxy-terminated silicone oil, isophorone diisocyanate, a catalyst, a chain extender, triethylamine, distilled water, a stabilizer, and a filler. The organophosphorus-modified polyethylene glycol is prepared by introducing an organophosphorus flame retardant into the molecular chain of polyethylene glycol diglycidyl ether. The phthalazine-modified epoxy-terminated silicone oil is prepared by introducing a rigid phthalazine structure into the epoxy-terminated silicone oil structure, and the phthalazine-modified epoxy-terminated silicone oil participates in the synthesis process of the polyurethane as a soft segment of the polyurethane, thereby effectively improving the high-temperature resistance of the polyurethane adhesive. Moreover, since the structure contains the flame-retardant elements nitrogen and silicon, the adhesive can produce a synergistic flame-retardant effect with the organophosphorus flame retardant, thereby further enhancing the flame-retardant performance of the polyurethane adhesive.

The invention relates to the field of organic synthesis, in particular to a synthetic method of olaparib. The synthetic method of the olaparib comprises the following steps: under the action of a Pd monatomic catalyst and an alkaline substance, 4-(4-fluoro-3-iodobenzyl) phthalazine-1 (2H)-ketone, carbon monoxide and 1-cyclopropyl formyl piperazine are subjected to a reaction, and the olaparib is generated, wherein the Pd monatomic catalyst comprises a carrier and Pd monatomic atoms loaded on the carrier. The invention provides a method for efficiently synthesizing olaparib directly from a simple phthalazine raw material, a Pd monatomic catalyst is used in the process, the yield and selectivity are high, the solid catalyst can be directly filtered after the reaction to avoid pollution of heavy metal Pd to the product, and complex column chromatography separation is not needed.

The present invention provides a preparation method for a phthalazinone PRMT5 inhibitor (formula (S)) and an intermediate thereof. The method involves a novel reaction route, mild reaction conditions, simple operation, high reaction yield, high product purity and convenient work-up, and is suitable for industrial production.

A phthalazine ketone compound or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound, and a medical use of the compound. The compound of the present application has a neuroprotective effect and can be used for treating / preventing cerebrovascular-related diseases.

The invention relates to a phthalazinone compound containing an aryl malonamide structure and application of the phthalazinone compound, and belongs to the technical field of medicines, the phthalazinone compound containing the aryl malonamide structure has a structure shown in a general formula (I), and the phthalazinone compound containing the aryl malonamide structure can be pharmaceutically added with acid to form salt. Pharmacological activity screening results show that the compound has significant inhibition effects on human breast cancer cells MDA-MB-453, human lung adenocarcinoma cells A549 and human colon cancer cells HCT116, and has good prospects in development and application of antitumor drugs.

Disclosed is a compound as shown in general formula I or a pharmaceutically acceptable salt, tautomer, mesomer, racemate, enantiomer, and diastereomer thereof. The compound of the present invention significantly improves the degradation effect of GSPT1 protein and the anti-proliferative inhibition activity of AML and solid tumor cells. Therefore, the compound of the present invention can be used in the preparation of a medicament for treating or preventing diseases related to GSPT1, IKZF1, IKZF2, IKZF3, CK1α, N-MYC or C-MYC protein mutation, expression imbalance, and allostery and functional abnormalities; in addition, said compound can be used to prepare a GSPT1 degrading agent.

The invention provides a one-dosage-form multilayer film structure etching solution and a preparation method and application thereof, and the one-dosage-form multilayer film structure etching solution comprises the following components by weight: 8-12 parts of hydrogen peroxide; 8-18 parts of organic acid; 4-10 parts of an organic base; 0.01 to 0.05 part of a functional agent; 0.2 to 0.6 part of a surfactant; 0.1-1 part of a hydrogen peroxide stabilizer; 60 to 76 parts of ultrapure water; the functional agent comprises a phthalazine compound and a piperidine compound. The phthalazine compound and the piperidine compound are used as functional agents, so that the stability of the etching liquid is improved, and good etching morphology can be obtained after etching.

The present invention relates to novel phthalazine derivative compounds as SOS1 inhibitors and uses thereof. More specifically, the present invention relates to a novel phthalazine derivative compound having inhibitory activity on the binding of SOS1 to RAS family proteins and / or RAC1, a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the compound.

Disclosed are phthalazinone compounds, methods for their preparation, and medical uses. In particular, disclosed are compounds of formula (I) and pharmacodynamically acceptable salts thereof, and the use of the compounds as androgen receptor (AR) inhibitors for degradation. TIFF2023531390000270.tif43170

The application discloses a phthalazine dione compound and a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. The phthalazine dione compound prepared by the application has extensive antibacterial activity and shows extremely low toxicity to normal cells, and has the characteristics of high efficiency and low toxicity. Functional groups in the structure of the phthalazine dione compound can be further derivatized, thereby expanding the structural diversity of the phthalazine dione compound. Therefore, the application provides an important strategy for structural modification and diversity synthesis of the phthalazine dione compound. In addition, the preparation method of the application is simple and easy to operate, avoids the cumbersome process of pre-installation of a guiding group in other synthesis methods of the phthalazine dione compound, does not need to add an additional external oxidant, significantly improves the synthesis efficiency and reduces the cost, and has the advantages of cheap and easily available raw materials, mild conditions, environmental friendliness and the like.

The invention discloses a phthalazinone derivative with PARP1 / CDK4 / 6 double-target inhibitory activity as well as a preparation method and application of the phthalazinone derivative. The invention provides a phthalazinone derivative with PARP1 / CDK4 / 6 double-target inhibitory activity, a pharmaceutical composition containing the derivative shown in the formula (I), a hydrate, and isotope derivatives, chiral isomers, allosteric substances, different salts, prodrugs, preparations and the like of the compounds, wherein the phthalazinone derivative has the structure shown in the formula (I). The invention also provides a preparation method of the phthalazinone derivative with PARP1 / CDK4 / 6 double-target inhibitory activity and application of the compounds in treatment of solid tumors and hematoma.

Novel compounds of structural formula (I), and pharmaceutically acceptable salts thereof, are inhibitors of NLRP3 and are useful in the treatment, prevention, management, amelioration, control and inhibition of diseases mediated by NLPR3. The compounds of the invention are useful in the treatment, prevention or management of diseases, disorders and conditions mediated by NLRP3, such as, but not limited to, gout, pseudogout, CAPS, NASH fibrosis, heart failure, idiopathic pericarditis, atopic dermatitis, inflammatory bowel disease, Alzheimer's disease, Parkinson's disease, and traumatic brain injury. # imgabs0 #

This invention discloses a phthalazinone compound, its preparation method, and its uses. The structure of this compound is shown in formula (I), and it exhibits excellent PARP14 inhibitory activity, inhibiting IC50 in vitro. 50 The optimal concentration level is nanomolar, which has the potential to become a new drug for the prevention and / or treatment of tumors and inflammatory diseases. When used in combination with existing known antitumor and anti-inflammatory drugs, it can improve the therapeutic effect of existing known antitumor and anti-inflammatory drugs while reducing the side effects of the drugs.

To provide an NLRP3 inhibitor that is effective in treating and preventing diseases, disorders, and conditions mediated by the formation and proliferation of the NLRP3 inflammasome.SOLUTION: A compound of the formula (I) is provided, where T is independently selected from the group: 1) CR3, and 2) N; provided that zero, one or two of T, U, V and W are N; U is independently selected from the group: 1) CR4, and 2) N; V is independently selected from the group: 1) CR5, and 2) N; W is independently selected from the group: 1) CR6, and 2) N; R1 is selected from -C3-12 cycloalkyl, -C3-12 cycloalkenyl, and -C2-12 heterocyclic alkyl, and R2 is selected from aryl and heteroaryl.SELECTED DRAWING: None

This invention provides novel crystals of triazoline dione adducts and methods for producing them, methods for producing and analyzing ene compounds using the novel crystals, and derivatization reagents for mass spectrometry and derivatization reagent kits containing the novel crystals. [Solution] The novel crystal according to the present invention is a crystal of 5,10-dihydro-2-(4'-dimethylaminophenyl)-5-phenyl-5,10[1',2']-benzeno-1H-[1,2,4]triazolo[1,2-b]phthalazine-1,3(2H)-dione (DAPTAD-PA) represented by the following formula (1), and has a single exothermic peak in the range of 175 to 185°C in differential scanning calorimetry. TIFF2026064145000011.tif42134

The invention belongs to the technical field of medicines, and discloses 4-benzyl phthalazine-1 (2H)-ketone derivatives as well as a preparation method, a pharmaceutical composition and application of the 4-benzyl phthalazine-1 (2H)-ketone derivatives. Specifically, the invention relates to a 4-benzyl phthalazine-1 (2H)-ketone derivative shown in a general formula I, a pharmaceutically acceptable salt thereof, a stereoisomer thereof, a preparation method thereof, a composition containing one or more of the compounds, and application of the compounds in preparation of drugs for diseases related to P97 or PARP1.