109 results about "Spiro compound" patented technology

A spiro compound, and a preparation method therefor and a use thereof. Specifically, the present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, tautomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite, or prodrug thereof, a pharmaceutical composition comprising the compound, a preparation method therefor, and a use thereof in preparation of a drug for preventing or treating KRAS-mediated related diseases.

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, isotopic variant, tautomer or stereoisomer thereof as a KRAS mutant inhibitor. The present invention also provides a pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt, isotopic variant, tautomer or stereoisomer thereof, and a use in treating cancer.

Disclosed herein are compounds useful for the inhibition of KRAS G12D, G12V, G12A, G12S, G12R, G13D, Q61H, Q61L, Q61R or G12C. The compounds have a general Formula (I): (I) or pharmaceutically acceptable salts thereof, wherein the variables of Formula (I) are as defined herein. Also provided herein are pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a KRAS G12D, G12V, G12A, G12S, G12R, G13D, Q61H, Q61L, Q61R or G12C disorder.

Provided in the present invention is a compound of formula (X), or an isotopic variant, a tautomer or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as a KRAS mutant inhibitor. Further provided in the present invention are a pharmaceutical composition containing the compound, or the isotopic variant, the tautomer or the stereoisomer thereof, or the pharmaceutically acceptable salt thereof, and the use thereof in the treatment of cancers.

The present disclosure relates to spirocyclic compounds targeting KRAS, pharmaceutical compositions containing the compounds, and methods of using such compounds to treat disease, such as cancer.

The invention discloses a silicon spiro compound as well as a preparation method and application thereof. The silicon spiro compound has the following structural formula, the X group and the Y group are respectively and independently selected from any one of an oxygen atom, a carbonyl group, a sulfinyl group, a sulfuryl group, a substituted or unsubstituted C1-C6 alkylene group, a substituted or unsubstituted C2-C10 alkenyl group, a substituted or unsubstituted C2-C10 alkynyl group, a substituted or unsubstituted C2-C10 cyano group and an aryl group; the silicon spiro compound provided by the invention is suitable for being used as an additive of a lithium ion battery electrolyte, the stability and cycle life of a lithium ion battery can be obviously improved, the reaction condition is mild, and the product purity and yield are high.

This invention discloses a chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups, with the following structural formula: The preparation includes the following steps: 1. Sequentially adding a metal catalyst, a chiral ligand, a base, indigo-derived trifluoromethylimine ylide, and 3-methylene β-lactam, followed by the addition of an organic solvent to obtain a mixture. The mixture is stirred at a reaction temperature of 0℃ to 50℃. 2. After the reaction is complete, the chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups is obtained through post-processing. The chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups prepared in this application lays a material foundation for in-depth drug activity research based on new drug development.

The invention discloses a nitrogen-containing spiro compound crystal form and a preparation method and application thereof. The invention provides a crystal form I of a nitrogen-containing spiro compound as shown in a formula A. The crystal form I of the nitrogen-containing spiro compound is radiated by Cu-K alpha, and an X-ray powder diffraction pattern expressed by a 2 theta angle has diffraction peaks at 5.67 + / -0.20 degrees, 11.37 + / -0.20 degrees, 16.69 + / -0.20 degrees, 17.32 + / -0.20 degrees and 19.73 + / -0.20 degrees. The invention provides a crystal form II of a nitrogen-containing spiro compound as shown in a formula A. The crystal form II is radiated by Cu-K alpha, and an X-ray powder diffraction pattern expressed by a 20 angle has diffraction peaks at the positions of 11.32 + / -0.20 degrees, 11.70 + / -0.20 degrees, 11.93 + / -0.20 degrees, 18.03 + / -0.20 degrees, 18.81 + / -0.20 degrees and 19.17 + / -0.20 degrees. The crystal form of the nitrogen-containing spiro compound has good stability and complement factor D inhibitory activity, has a good inhibitory effect on rabbit red blood cell hemolysis, and has high in-vivo exposure and high oral bioavailability.

According to the efficient synthesis method of the alpha-carbonyl spiro compound, aryl bromide is used as a substrate, benzene-1, 3, 5-triformic acid triester is used as a safe and green carbonyl source, palladium is used as a catalyst, organic phosphine is used as a ligand, and 1, 8-diazabicyclo [5.4. 0] undec-7-ene (DBU) is used as alkali, so that the amide-containing bis-heterocyclic compound is successfully synthesized. The method adopts a one-pot method, and has the characteristics of greenness, safety, simplicity in operation, wide substrate range, good functional group compatibility, high bonding efficiency and the like. The product alpha-carbonyl spiro compound is an important intermediate for synthesizing complex molecules such as drugs and natural products, and the method has important significance in the fields of medicines, pesticides, chemical engineering and the like.

The invention relates to a compound synthesis technology, in particular to a preparation method of 4-boron-L-phenylalanine. The reaction route of the preparation method is shown in the specification. According to the reaction route of the preparation method of the 4-boron-L-phenylalanine provided by the invention, the L-BPA is prepared by utilizing the boron spiro compound provided by the invention, so that the problems that the existing direct synthesis reaction route is relatively long, the reaction condition is harsh, a chiral catalyst is difficult to obtain and the like can be avoided. L-BPA with higher chemical yield is obtained through a shorter reaction route under mild reaction conditions.

Provided are a crystal form and an amorphous substance of an indoline spiro compound represented by formula (1), and a preparation method therefor and the use thereof. The X-ray powder diffraction pattern of the crystal form comprises characteristic peaks at 5.43±0.20°, 12.28±0.20° and 17.91±0.20° 2θ, as determined by using Cu-Kα radiation; and the XRPD spectrum of the amorphous substance has no obvious diffraction peak. The provided crystal form and the amorphous substance have high purity and good stability, and are beneficial to drug formation.

This invention discloses crystals of nitrogen-containing spiro compounds, methods for producing the same, and uses thereof. This invention provides a type I crystal of a nitrogen-containing spiro compound represented by formula A, in which the powder X-ray diffraction pattern displayed at a 2θ angle using Cu-Kα rays has diffraction peaks at positions 5.67±0.20°, 11.37±0.20°, 16.69±0.20°, 17.32±0.20°, and 19.73±0.20°. This invention also provides a type II crystal of a nitrogen-containing spiro compound represented by formula A, in which the powder X-ray diffraction pattern displayed at a 2θ angle using Cu-Kα rays has diffraction peaks at positions 11.32±0.20°, 11.70±0.20°, 11.93±0.20°, 18.03±0.20°, 18.81±0.20°, and 19.17±0.20°. The nitrogen-containing spiro compound crystals of the present invention exhibit good stability and complement factor D inhibitory activity, good inhibitory effect against rabbit erythrocyte hemolysis, high in vivo exposure levels, and high oral bioavailability. JPEG2026513298000037.jpg5469

The application discloses a chromone spiro compound, a preparation method and application thereof, and the chromone spiro compound is shown as formula I. The compound has selective CDK4 / 6 inhibitory activity, can relieve and / or treat myelosuppression caused by chemotherapy, improve weight loss caused by chemotherapy and improve survival rate, and has good drug safety. The compound has simple preparation method, is convenient for large-scale production, and has great application prospect.

The application discloses a preparation method and application of a spiro compound MOC material photocatalyst, which is a compound with a structural general formula (I). The compound is a photocatalyst capable of degrading dyes, tetracyclines and reduced hexavalent chromium under visible light, the catalyst is easy to separate from a solution, and has good structural stability and reusability.

The present disclosure relates to spirocyclic compounds targeting KRAS G12C, pharmaceutical compositions containing the compounds, and methods of using such compounds to treat disease, such as cancer.

The invention discloses a heterocyclic spiro compound and an organic light-emitting device, the heterocyclic spiro compound has a structural general formula as shown in formula (1): in the formula (1), ring A and ring B are independently selected from naphthalene rings or benzene rings; one of X and Y is S, and the other one is O or S; x1, X2 and X3 are respectively and independently selected from N or CR5, and at least one is N; and Ar1, Ar2 and Ar3 are independently selected from a substituted or unsubstituted C6-C30 aryl group, a substituted or unsubstituted C3-C16 cycloalkyl fused C6-C30 aryl group, and a substituted or unsubstituted C2-C30 heteroaryl group. The compound has the advantages of high optical and electrical stability, low driving voltage, high luminous efficiency, long device service life and the like, can be used as a hole blocking material and an electron transport layer material, and is used in OLED luminescent devices.

The present invention relates to a crystal form of a multi-membered spiro compound, and a preparation method therefor and a medical use thereof, and in particular to a crystal form of a compound represented by general formula (I), a preparation method, and a pharmaceutical composition containing a therapeutically effective amount of the crystal form and a pharmaceutical use thereof for treating diseases or conditions related to alternative complement pathway activation.

The present application relates to a nitrogen-containing spirocyclic compound, a pharmaceutical composition and a use thereof. The nitrogen-containing spirocyclic compound has the structural formula represented by formula (I). The compound of the present invention has TRPV3 inhibitory activity and can be used as a TRPV3 antagonist or inhibitor

The application discloses a thiazole spiro compound and a preparation method and application thereof; the thiazole spiro compound has the structure shown in formula I: wherein, n is greater than or equal to 1; 1 is less than or equal to 5, R 1 is selected from H, halogen, C 1～6 alkyl; R 2 is independently selected from H, C 1～12 alkyl, C 1～12 haloalkyl, C 1～12 alkoxy; R 3 is selected from H, C 1～12 alkyl, phenyl. The application provides a series of novel thiazole spiro compounds, and the compounds have inhibitory effect on tumor cells.

This invention discloses a spiro compound and its applications, belonging to the field of display technology. The chemical structural formula of the compound is as follows: ; wherein, Ar1 to Ar4 are each independently one of a substituted or unsubstituted C6-C60 aryl group or a substituted or unsubstituted C3-C30 heteroaryl group; Ar5, Ar6, and R are each independently one of a substituted or unsubstituted C6-C60 aryl group or a substituted or unsubstituted C3-C30 heteroaryl group; at least one of Z1 to Z3 is N, and the rest are CH; L is one of the following groups: , , ; R1 to R 10 Each of these compounds is independently one of hydrogen, halogen, cyano, nitro, C1-C8 alkyl, C1-C12 alkoxy, substituted or unsubstituted C6-C30 aryl, or substituted or unsubstituted C3-C30 heteroaryl. This compound exhibits excellent electron transport properties, which is beneficial for improving the voltage, efficiency, and lifetime of devices.

This application discloses a synthetic method for azaspirocyclic compounds and their derivatives, comprising reacting an alkynylamine of Formula I, an activator, and an additive to obtain a compound of Formula II. The method described in this application employs a σ-rearrangement and spirocyclic strategy to construct an azaspirocyclic skeleton in one step, overcoming the limitations of traditional multi-step synthesis. Furthermore, this method is characterized by mild conditions, simple operation, and broad functional group compatibility, showing promising application prospects. This application also successfully developed a systematic and diverse derivatization pathway using the core spirocyclic skeleton as a key intermediate, overcoming subsequent modification bottlenecks and providing efficient tools for drug development, natural product simulation, and ligand design. It possesses both academic breakthrough and industrial application potential, promoting the green and precise development of synthetic methodology.

The application belongs to the field of electroluminescence, and particularly discloses a spiro compound, a preparation method thereof, a light-emitting layer, a light-emitting device and a display device, the spiro compound has a structural formula of formula (I) or formula (II): formula (I); formula (II); the structure of D is ; and the structure of A is. The spiro compound provided by the application can be used as a host material of a light-emitting layer, has excellent organic solvent solubility and good film-forming property, and an organic electroluminescent device prepared by using a solution processing technology has balanced carrier transport performance; the structure of the spiro compound can assist light-emitting materials to realize the advantage of relatively aggregated accumulation, and finally can effectively improve the maximum current efficiency of the device and reduce the efficiency roll-off.

The application discloses 2-boronic acid pinacol ester-9,9'-spirobis(xanthene) and a synthesis method thereof, and belongs to the field of organic chemical synthesis. A structural formula of the 2-boronic acid pinacol ester-9,9'-spirobis(xanthene) is as follows: the 2-boronic acid pinacol ester-9,9'-spirobis(xanthene) is synthesized by the following method: 2-bromoxanthone is used as a starting material, reacts with phenol to synthesize 2-bromo-9,9'-spirobis(xanthene), and then is subjected to Suzuki-Miyaura reaction to synthesize. The synthesis method is simple in operation, low in production cost, and high in product content (greater than 99.9%); the synthesis method can meet the requirements of industrial production and application, is suitable for industrial production, and expands the application of spiro compounds as intermediates in the design and synthesis of organic optoelectronic functional materials.

This invention discloses an isoquinolinone dihydropyridine-[1,2-α]indole spirocyclic compound, its preparation method, and its applications, belonging to the field of organic compound synthesis technology. Using N-indole-linked o-alkynyl nitrone compounds as raw materials, this invention employs a two-step, one-pot method to provide a novel synthesis of isoquinolinone dihydropyridine-[1,2-α]indole spirocyclic compounds that are difficult to prepare using conventional methods. This method is based on a rhodium-catalyzed internal redox / dearomatization [3+2] cycloaddition reaction and a cerium ammonium nitrate-promoted oxidative debenzylation / spirocyclic tandem reaction strategy. The method of this invention has advantages such as simple operation, low catalyst loading, broad substrate range, single stereoselectivity, and high yield. The isoquinolinone dihydropyridine-[1,2-α]indole spirocyclic compound prepared by this invention has a certain inhibitory effect on plant pathogens and can be potentially applied to the control of tomato gray mold, wheat scab, and rice sheath blight.

This invention provides spirocyclic compounds as inhibitors of KRASG12D mutants, including compounds, pharmaceutically acceptable salts, isotopic variants, tautomers, or stereoisomers thereof. The invention also provides pharmaceutical compositions comprising said compounds and their use in the treatment of cancer.

The present invention relates to a spiro compound, a preparation method therefor and a use thereof. Specifically, the present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, tautomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof, a pharmaceutical composition comprising same, a preparation method therefor, and a use thereof in the preparation of drugs for preventing or treating KRAS-mediated related diseases.

The application provides a kind of spiro compound and its application, the structure of the spiro compound is as shown in formula I or formula II, the spiro compound is used for the preparation of spiro compound, and the preparation method comprises the following steps: (1) compound I is subjected to alkylation reaction to obtain compound II;(2) compound II is reacted with benzylamine compound to obtain compound III;(3) compound III is reduced to obtain compound IV;(4) compound IV is mixed with debenzyl reagent to obtain compound V, and then chiral resolution obtains the target spiro compound.The preparation method provided by the application is simple in process operation, raw materials are cheap and easy to obtain, the yield is high, and the process avoids the use of hydrogen and metal catalyst in the debenzyl process through specific process design, greatly reduces the safety and environmental problems, and also reduces the production cost.

The invention discloses a novel spiro compound as well as a pharmaceutical composition and application thereof, the novel spiro compound is shown as a formula (I), and the definition of each substituent is shown in the specification. The compound can be used for preparing medicines for preventing or treating head pain diseases.

The invention belongs to the technical field of medicines, and discloses a double-spiro compound IDO inhibitor as well as a preparation method, a pharmaceutical composition and application thereof. Specifically, the invention discloses a compound shown in a general formula (I) and pharmaceutically acceptable salts thereof, a preparation process of the compound, a pharmaceutical composition containing the compound shown in the general formula (I), and application of the compound and the pharmaceutical composition in the anti-tumor direction.

The application provides a chiral spiro compound and a preparation method and application thereof, and belongs to the technical field of organic synthesis. The chiral spiro compound is obtained by mixing spiro olefin, alkyl iodide, cobalt salt, a chiral ligand, an organic solvent, a reducing agent and an alkaline substance to perform a hydrogen alkylization reaction. A cobalt-catalyzed stereodivergent asymmetric synthesis method is disclosed, high-efficiency preparation of a spiro compound containing 1,3-non-adjacent stereogenic centers is realized by ligand regulation, and the product has excellent biological activity. The method has wide substrate compatibility and high selectivity, and provides a new way for drug development.