18 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.

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.

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

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

This application relates to the use of one of 5-amino-2,3-dihydro-1,4-phthalazinediones or a pharmaceutically acceptable salt thereof in the prevention or treatment of RNA virus infection. In particular, the present invention relates to the use of sodium 5-amino-2,3-dihydro-1,4-phthalazinediones for said purpose. Pharmaceutical compositions, combinations, and advantageous formulation techniques are disclosed.

The present invention relates to compounds of formula (I) inhibiting P2X purinoceptor 3; particularly the invention relates to compounds that are phthalazine derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. The compounds of the invention may be useful in the treatment of many disorders associated with P2X3 receptors mechanisms, such as respiratory diseases including cough, asthma, idiopathic pulmonary fibrosis (IPF) and chronic obstructive pulmonary disease (COPD).

The present disclosure relates to 5-amino-2, 3-dihydro-1, 4-phthalazindiones and pharmaceutically acceptable salts thereof for use in the prevention or treatment of thrombotic disorders. In particular, the invention relates to the use of a sodium salt of 5-amino-2, 3-dihydro-1, 4-phthalazindione for this purpose. Pharmaceutical compositions, advantageous techniques of formulation, and methods of treatment are disclosed.