218 results about "Isoindoline" patented technology

The invention belongs to the technical field of synthesis of organic compounds, and particularly relates to a chiral synthesis method of spiro [cyclopenta [c] carbazole-1, 1 '-isoindoline]-3'-ketone compounds. The compound synthesized by the invention has an isoindolinone skeleton and a carbazole active fragment at the same time. The carbazole compound and the isoindolinone compound are successfully combined in a cyclization mode for the first time, and the chiral compound can be prepared. The invention provides a synthesis method of a chiral spiro [cyclopenta [c] carbazole-1, 1 '-isoindoline]-3'-ketone compound, which has the advantages of mild reaction conditions, green and environment-friendly catalyst, easiness in operation, few synthesis steps, easiness in purification and separation of products, capability of obtaining higher yield and high stereoselectivity, easiness in amplification of reaction, high yield, high yield and high yield, and is suitable for large-scale production of the chiral spiro [cyclopenta [c] carbazole-1, 1 '-isoindoline]-3'-ketone compound. And the method has a wide application prospect.

The invention relates to the technical field of epoxy resin, in particular to an optical epoxy resin molding compound and a preparation method and application thereof. The coating comprises the following components: a colorant, epoxy resin, an antioxidant, a curing agent and an auxiliary agent, the color agent comprises an ultraviolet absorbent and a blue light absorbent; the epoxy resin comprises triazine skeleton epoxy resin. The toner comprises an ultraviolet absorbent and a blue light absorbent, and the epoxy resin comprises triazine skeleton epoxy resin, so that light rays below 460 nm can be effectively shielded, the transmittance of light rays above 500 nm reaches 85% or above, and meanwhile, excellent high-temperature resistance is achieved; the ultraviolet absorbent comprises a triazine ultraviolet absorbent, and the blue light absorbent comprises a triazine derivative structure of an isoindolinone heterocyclic skeleton, so that the numerical value of 460 nm light transmittance / 500 nm light transmittance can be reduced to 0.5 or below.

The invention provides compounds that degrade the epidermal growth factor receptor (EGFR) including mutant forms via the ubiquitination of the EGFR protein and subsequent proteasomal degradation. The compounds are useful for the treatment of various cancers.

The present disclosure relates to a compound represented by formula (I) or a salt, enantiomer, stereoisomer, solvate, polymorph thereof and a use thereof. The present disclosure also relates to pharmaceutical compositions comprising, as an active ingredient, the compound represented by formula (I) or the salt, enantiomer, stereoisomer, solvate, polymorph thereof, and a use thereof. In the present disclosure, the compounds designed and synthesized can effectively prevent or treat diseases or conditions related to celeblon protein, including tumors or cancers.

The invention belongs to the technical field of biological medicines, and particularly relates to a compound as shown in a formula (I), pharmaceutically acceptable salt, deuterated substance, stereoisomer, tautomer or a mixture of the pharmaceutically acceptable salt, the deuterated substance, the stereoisomer and the tautomer, and application of the compound as an IKZF1 and IKZF3 double-target immunomodulator.

The application relates to a preparation method of an arylmethoxy isoindoline derivative and belongs to the field of pharmaceutical chemical industry. Specifically, a compound of formula III and a compound of formula II are reacted in an organic solvent in the presence of a reducing agent to generate a compound of formula I. A new preparation route of the arylmethoxy isoindoline derivative is provided, and the preparation route has high yield and high product purity.

The present invention relates to an isoindolinone derivative, a preparation method, a pharmaceutical composition and an application. The derivative is a compound of formula I or a pharmaceutically acceptable salt of the compound of formula I, wherein Ra is one of a substituted or unsubstituted aryl, a substituted or unsubstituted C1-C6 alkyl; Rb and Rc are each one of a substituted or unsubstituted C1-C6 alkyl. Compared with the prior art, the isoindolinone derivative in the present invention has a novel structure, has significant anti-cancer cell proliferation activity, and the activities of multiple compounds are superior to those of doxorubicin.

The application discloses a 3-(5-(aminomethyl)-1-oxoisoindoline-2-yl)piperidine-2,6-dione derivative and a synthesis method and application thereof, and relates to a 3-(5-(aminomethyl)-1-oxoisoindoline-2-yl)piperidine-2,6-dione derivative which is a compound with the following general formula (I): wherein R1 is selected from,,,,,,,,, and R2 is selected from,,, and. The compound can significantly inhibit the proliferation of leukemia, multiple myeloma, lymphoma, breast cancer, liver cancer and the like at a low dose (nanomole), can effectively degrade IKZF1, IKZF3, BRD4, GSPT1 and CK1 alpha, and has the prospect of being developed into an anti-tumor drug. The application solves the problem that the existing malignant hematological disease treatment drugs have a high safety risk.

The present disclosure provides a compound of Formula (I'): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein Rx, X1, X2, and Ri are as defined herein, and methods of making and using same.

Disclosed are compounds of Formula (I) or a salt thereof, wherein Ring A is a carbon-linked ring; and Ring A, R1, and n are defined herein. Also disclosed are methods of using such compounds to inhibit Helios protein, and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

The invention discloses a 1-oxo-isoindoline derivative with a structure as shown in a formula (I) and pharmaceutically acceptable salt, solvate, crystal form or stereoisomer thereof, the 1-oxo-isoindoline derivative can be used as a molecular glue degradation agent of GSPT1, has high degradation activity on GSPT1, and has good potential safety. The derivative can be used for degrading GSPTl, preparing drugs for treating diseases related to GSPTl activity and preparing antibody coupling degradation drugs. # imgabs0 #

The present invention belongs to the technical field of pharmaceutical intermediates, and specifically relates to a preparation method of 6-bromo-2-(2,6-dioxopiperidin-3-yl)-4-fluoroisoindoline-1,3-dione. The preparation of 6-bromo-2-(2,6-dioxopiperidin-3-yl)-4-fluoroisoindoline-1,3-dione uses 1-fluoronaphthalene as the starting material, and undergoes selective bromination, Oxone oxidation, and Ac2O dehydration and acid anhydride formation / amidation, a total of three steps of reactions to obtain the finished product. The preparation method provided by the present invention is scientifically and reasonably designed, and can achieve the safe preparation of 6-bromo-2-(2,6-dioxopiperidin-3-yl)-4-fluoroisoindoline-1,3-dione with the characteristics of environmental protection and low cost.

The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and / or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and / or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting or blocking NUAK kinase, such as cancers and fibrosis.

The present invention relates to an isoindoline compound containing a phenylethoxyalkyleneamine structure, a conjugate thereof, and use thereof. The isoindoline compound containing a phenylethoxyalkyleneamine structure has a structure represented by formula (I). The conjugate thereof has a structure represented by formula (B). The compound of the present invention exhibits increased proliferation inhibition activity for cancer cells and a degradation effect on proteins such as GSPT1, demonstrating practical values.

Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed.

Provided are compounds of the structural Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with ALK.

The present invention relates to pharmaceutical compounds and formulations comprising said compounds, wherein said compounds have the structure according to Formula I or II. The compounds and formulations are suitable for use as medicaments for the prevention or treatment of diseases or conditions characterized by percutaneous cell dysfunction, detachment and / or loss, for medical treatment for vascular stabilization, for treatment for promoting, restoring or maintaining attachment of percutaneous cells to blood vessels, and / or for the treatment of vascular-related diseases in patients. (I) (II)

Disclosed are compounds of Formula (1): Also disclosed are methods of using such compounds to decrease the levels of Ikaros protein, Helios protein, Aiolos protein, and Eos protein; and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

The present disclosure relates to compounds of formula (I) or salts, enantiomers, stereoisomers, solvates, polymorphs thereof, and uses thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds of formula (I) or salts, enantiomers, stereoisomers, solvates, polymorphs thereof as active ingredients and uses thereof. A series of compounds designed and synthesized by the invention can be used for effectively preventing or treating diseases or symptoms related to the cerebron protein, including tumors or cancers. # imgabs0 #

The invention discloses a method for preparing a furfural-based color-changing dye. The general structural formula of the furfural-based color-changing dye is: , wherein the group R is, ,. The method comprises the following steps: (1) generating three furan derivatives through a condensation reaction involving furfural; (2) subjecting 2‑(2‑(3,4,5‑trimethoxyphenylamino)ethyl)isoindoline‑1,3‑dione to a furan ring-opening reaction with the three products of step (1), respectively, to obtain three furfural-based color-changing dyes. The preparation method of the invention has the advantages of simple process, high dye yield and purity, and cheap and readily available raw materials; the obtained furfural-based dye has low toxicity, outstanding thermal stability and light fatigue resistance, can achieve reversible color change under visible light (600-700 nm) irradiation and heating conditions, and can be used for the manufacture of materials such as smart fabrics, temperature indicators, and artificial muscles.

The invention provides compounds that degrade the epidermal growth factor receptor (EGFR) including mutant forms via the ubiquitination of the EGFR protein and subsequent proteasomal degradation. The compounds are useful for the treatment of various cancers.

Provided herein are methods of using 2-(2,6-dioxopiperidin-3yl)-4-(2-fluoro-4-(3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione, or an enantiometer, a mixture of enantiomers, a tautomer, an isotopolog, or a pharmaceutically acceptable salt thereof, alone or in combination with obinutuzumab, for treating, preventing or managing chronic lymphocytic leukemia / small lymphocytic lymphoma.

The invention provides a PD-L1 targeting small-molecule inhibitor, nanoparticles prepared by combining the PD-L1 targeting small-molecule inhibitor with a photodynamic therapy, a medicine and application, and belongs to the technical field of biological medicine. The invention provides a PD-L1 targeting small molecule inhibitor, which is an alanine substituted isoindoline bitoluene derivative C2 as shown in a formula I which is described in the specification. Tests show that the alanine substituted isoindoline bitoluene derivative C2 can effectively inhibit PD-1 / PD-L1 binding and has certain anti-tumor activity, and nanoparticles of a nano delivery system prepared from the inhibitor and a photosensitizer have better anti-tumor (colon cancer) activity. The technical scheme of the invention provides a new thought for tumor treatment.

The present disclosure provides a compound of Formula (I) or salts, enantiomers, stereoisomers, solvates, or polymorphs thereof and uses thereof. The present disclosure also provides pharmaceutical compositions comprising, as an active ingredient, the compound of Formula (I) or salts, enantiomers, stereoisomers, solvates, or polymorphs thereof and uses thereof. The series of compounds designed and synthesized in the present disclosure can effectively prevent and / or treat diseases or disorders associated with the cereblon protein.

Described are compounds, compositions, and methods for treating Tumor Necrosis Factor Receptor-Associated Protein 1 (TRAP 1) related diseases and / or disorders, such as cancer.

The present invention relates to the field of epoxy resin technology, and more specifically, to an optical epoxy resin molding compound, its preparation method, and application. The components include: a colorant, an epoxy resin, an antioxidant, a curing agent, and an auxiliary agent; the colorant includes a UV absorber and a blue light absorber; and the epoxy resin includes a triazine skeleton epoxy resin. The colorant includes a UV absorber and a blue light absorber, and the epoxy resin includes a triazine skeleton epoxy resin, which can effectively shield light below 460nm and increase the transmittance of light above 500nm to more than 85%, while achieving excellent high-temperature resistance. The UV absorber includes a triazine-type UV absorber, and the blue light absorber includes a triazine-derived structure with an isoindolinone heterocyclic skeleton, which can reduce the value of 460nm transmittance / 500nm transmittance to less than 0.5.

The invention relates to the technical field of pigment synthesis, in particular to a production process of pigment yellow 139, which comprises the following steps: 1) adding water into barbituric acid, fully dissolving at the temperature of 30-70 DEG C, adjusting the pH value to be less than or equal to 1.8 to form a supersaturated solution, keeping the temperature unchanged, adding 1, 3-diimino isoindoline solid or a mixed solution of the 1, 3-diimino isoindoline solid and the water for multiple times, and reacting the barbituric acid with the 1, 3-diimino isoindoline solid to obtain a mixture; the molar ratio of the 2, 3-diimino isoindoline to the 2, 3-diimino isoindoline is (2.5-4.5): 1, keeping the pH value of the system to be less than 7 in the adding process, and then keeping the temperature at 40-70 DEG 2) crude product separation: after the heat preservation reaction is finished, keeping the temperature of the mixed solution in the step 1) at 50 DEG C or above, and carrying out hot filtration to separate a pigment crude product; 3) pigmentation: adding water into the pigment crude product, preserving heat at 105-130 DEG C for pigmentation within 4-10 hours to obtain a pigment yellow 139 product; and 4) carrying out heating reduced pressure distillation treatment on the filtrate obtained by hot filtration separation in the step 2) to obtain a barbituric acid aqueous solution and ammonia water. The raw material utilization rate is improved.