170 results about "Spiro compound" patented technology

The present invention covers spirocyclic compounds of general formula (I), in which R1, R2, X, Y, and Z are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neoplastic disorders, respectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant KRAS signaling, as a sole agent or in combination with other active ingredients.

The present disclosure is directed to compounds of Formula I: wherein Z1, Z2, R1, R2, R3, and R4 are described herein, which are spirocyclic compounds for inhibiting Werner Syndrome dsDNA helicase (WRN) and methods of treating disease using these compounds. This disclosure further provides compounds and their use for the treatment of cancers characterized as microsatellite instability-high (MSI-H) or mismatch repair deficient (dMMR), including colorectal, gastric, endometrial and ovarian cancer.

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 invention discloses an isoquinolinone dihydropyridine-[1, 2-alpha] indole spiro compound as well as a preparation method and application thereof, and belongs to the technical field of synthesis of organic compounds. An N-indole connected o-alkynyl nitrone compound is used as a raw material, a two-step one-pot method is adopted, and the isoquinolinone dihydropyridine-[1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, the invention relates to a novel method for synthesizing a spiro [1, 2-alpha] indole. The method disclosed by the invention has the advantages of simplicity in operation, low catalyst loading capacity, wide reaction substrate range, single stereoselectivity, high yield and the like. The isoquinolinone dihydropyridine-[1, 2-alpha] indole spiro compound prepared by the invention has a certain inhibition effect on phytopathogen, and can be potentially applied to prevention and treatment of tomato gray mold, wheat scab and rhizoctonia solani.

The invention relates to a rigid spiro compound and a preparation method and application thereof.The preparation method comprises the steps that 6-methylene-androstane-4-ene-3, 17-diketone (V) is dissolved in a mixed solution of dichloromethane and trifluoroacetic acid, reaction and reduced pressure distillation are conducted at the temperature of 20-25 DEG C, then extraction washing and distillation are conducted, a rigid spiro compound crude product can be obtained, and the rigid spiro compound is obtained. The crude product can be subjected to column chromatography separation and purification to obtain a refined rigid spiro compound (I). By adopting the preparation method, the friction and wear properties of the base oil are remarkably improved, and the base oil has lower friction coefficient and wear scar diameter, and has good application prospect as an antifriction and wear-resistant additive.

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 relates to a preparation method for producing a polyketone compound by using a recombinant strain Streptomyces coelicola A3 (2) / p15A-KOspiH3 (the preservation number is CCTCC NO: M 20241470), and also relates to an application of the polyketone compound in tumor resistance, and the structural formula of the polyketone compound is # imgabs0 #, the structural formula of the polyketone compound is as shown in the specification, the structural formula of the polyketone compound is as shown in the specification, and the structural formula of the polyketone compound is as shown in the specification. A fermentation product containing the compound can be obtained through fermentation culture of Streptomyces coelicola A3 (2) / p15A-KOspiH3, and then the compound is obtained through separation and purification of methods such as VLC normal-phase column chromatography separation, C-18 ODS reversed-phase column chromatography separation and semi-preparative HPLC. The invention aims to obtain a novel compound with an anti-tumor effect in a gene cluster of a heterologous expression actinomycete source, and the novel compound has a good application prospect.

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.

The invention relates to the technical field of spiro compounds, in particular to an 8, 8-difluoro-2-oxaspiro [4, 5] decane-1, 3-diketone compound as well as a preparation method and application thereof. The invention provides the 8, 8-difluoro-2-oxaspiro [4, 5] decane-1, 3-diketone compound, the compound shows excellent biological activity, and through test comparison, when the mass concentration is 0.1 mu g / mL, the insecticidal effect of the compound is increased by nearly 10% compared with that of a common insecticide chlorantraniliprole. It means that the compound shows a more efficient insecticidal effect on lepidoptera pests such as plutella xylostella and the like under a lower dosage, and cost reduction and synergism are realized. Due to the characteristic, the compound or the agronomically acceptable salt thereof shows important potential application value in the field of insecticides, and a new thought is provided for upgrading and updating of insecticides in the future.

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.

A chimeric compound for targeted degradation of androgen receptor protein, a preparation method therefor, and a medical use thereof. Specifically, the present invention relates to a spiro compound represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the spiro compound, and uses thereof as a therapeutic agent, in particular a use as an androgen receptor degradation agent and a use in the preparation of a drug for treating and / or preventing androgen receptor mediated or dependent diseases or conditions.

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.

Spiro compound as detergent additive in lubricants for marine engines The present application relates to the use, as detergent additive in a lubricating composition intended for a marine engine, of at least one spiro compound of formula (I) in which M is an atom chosen from boron and aluminum; n1 and n2 are, independently of one another, 0, 1 or 2; and R represent, independently of one another, a hydrocarbon group comprising from 1 to 50 carbon atoms, in particular from 5 to 20 carbon atoms. It also relates to the use of said spiro compound as an additive in a lubricating composition intended for a marine engine, to improve the oxidation stability of said lubricating composition.Finally, it relates to a lubricating composition intended for the lubrication of a marine engine, comprising one or more base oils and at least one spiro compound of formula (I), as well as a method for lubricating a marine engine using such a composition.

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 an oral pharmaceutical composition comprising a spiro compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a preparation method of the oral pharmaceutical composition, and a combined product comprising the oral pharmaceutical composition and another antiviral drug, the invention also discloses application of the oral pharmaceutical composition and the combination product in resisting virus infection and treating or preventing related diseases caused by virus infection. # imgabs0 #

According to an embodiment, the organic electroluminescent device includes: a first electrode; a hole transport region disposed on the first electrode; a light-emitting layer disposed on the hole transport region; an electron transport region disposed on the light-emitting layer; and a second electrode disposed on the electron transport region, wherein the light-emitting layer includes a spiro compound containing an arylamine group and an indenoindole derivative, and can therefore exhibit high luminescence efficiency and emit green light.

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.

The invention provides a spiro compound which is shown in a formula I and has a binding effect with E3 ligase protein CRBN, and application of the spiro compound in preparation of a medicine for treating cell abnormal proliferation diseases. # imgabs0 #

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.

A Spiro compound serving as an ERK inhibitor, and an application thereof in preparing a drug for treating an ERK-related disease. The present invention specifically relates to a compound represented by formula (III) or a pharmaceutically acceptable salt thereof.

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.

A compound of the following formula:which is capable of binding to an E3 ubiquitin ligase cereblon (CRBN). An application of the compound, or a stereoisomer, a deuterated compound or a pharmaceutically acceptable salt thereof in the preparation of drugs for the treatment of diseases associated with abnormal cell proliferation and targeted protein degradation is also provided.

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.