61 results about "Piperidinedione" patented technology

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt thereof) that degrade and / or otherwise modulate (e.g., inhibit) NIMA Related Kinase 7 (NEK7). Said chemical entities are useful, e.g., for treating a subject (e.g., a human subject) having one or more disorders or diseases associated with NLRP3 inflammasome activation. Said disorders or diseases include but are not limited to, autoinflammatory and autoimmune disorders (e.g., gout, inflammatory bowel disease, rheumatoid arthritis, multiple sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease), cardiovascular and metabolic disorders (eg. pericarditis, atherosclerosis, Type 2 diabetes, obesity, and metabolic syndrome), fibrotic disorders (e.g. interstitial lung disease, chronic kidney disease), hematology (eg. anemia of inflammation) and eye disorders (eg. macular degeneration). In embodiments, and while not wishing to be bound by theory, it is believed that the chemical entities described herein directly target (e.g., directly bind to) NEK7, thereby altering (e.g., attenuating) the inflammatory response modulated by the NLRP3 inflammasome. This disclosure also features compositions containing the same as well as methods of using and making the same.

The invention provides a synthesis method of 6-(t-butyloxycarboryl)-3, 6-diazabicyclo [3.1. 1] heptane, which comprises the following steps: starting from N-benzyl-2, 6-piperidinedione, firstly forming a dibromide 1, then forming a bridge ring intermediate 2 under alkaline conditions, then removing benzyl to obtain an intermediate 3, then reducing dicarbonyl to form free amine 4, and finally synthesizing the 6-(t-butyloxycarboryl)-3, 6-diazabicyclo [3.1. 1] heptane. Then performing Boc protection on amino to obtain an intermediate 5, and performing debenzylation to form a target product. According to the synthesis method, few impurities are generated, and the product is easy to purify and high in purity, so that the total yield is increased, the unit cost is effectively reduced, and large-scale industrial production is facilitated.

The present disclosure relates to polymorphic forms of (S)-3-(5-(4-((1-(4-((1R,2S)-6-hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenyl)piperidin-4-yl)methyl)piperazin-1-yl)-1- oxoisoindolin-2-yl)piperidine-2,6-dione,methods of making these polymorphic forms, and compositions comprising these polymorphic forms. These polymorphic forms are useful in the treatment of various diseases, including, for example, breast cancer.

Provided are a 2,6-piperidinedione compound and an application thereof. Particularly provided are a compound represented by formula (II), a stereoisomer thereof, and a pharmaceutically acceptable salt thereof.

Disclosed herein are dosage forms comprising a VAV1 degrader. More specifically, disclosed herein are dosage forms comprising 3-(2-chloro-4'-(2-oxopyridin-1(2H)-yl)-[1,1'- biphenyl]-3-yl)piperidine-2,6-dione or a pharmaceutically acceptable salt thereof. These dosage forms are useful, e.g., for treating a subject (e.g., a human subject) having a disorder or disease that can be treated by reducing the level of VAV1, for example an inflammatory or autoimmune disorder, a transplantation setting disorder, or a cancer.

Provided herein are piperidine dione compounds having the following structure:wherein RN, R1, R2, R3, R4, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.

The invention relates to a piperidinedione compound as well as a pharmaceutical composition and application thereof, and particularly provides a piperidinedione compound shown in a formula (I) which can be used for preparing medicines, especially medicines for preventing and / or treating diseases or symptoms caused by or related to lymphocyte development or activity disorder. Each group in the formula (I) is as defined in the specification.

The present invention relates to a PROTAC compound which can increase the degradation effect of a protein of interest, and to a novel piperidinedione compound which can be used as an E3 enzyme ligand of the PROTAC compound. The piperazinedione derivative compound of the present invention acts on CRBN and thus may be used as a therapeutic agent (for example, an anticancer agent or an immunomodulator) for diseases associated with CRBN proteins.

The invention relates to the technical field of regulation and control of crop seed vigor, in particular to a 5-amino-2, 6-piperidinedione-containing AZD8055 derivative and application thereof.The 5-amino-2, 6-piperidinedione-containing AZD8055 derivative is of a chemical structure shown in a general formula (I): # imgabs0 #. The AZD8055 derivative can effectively improve the seed vigor and promote rapid germination of seeds, and then seedlings emerge robustly and consistently.

The invention relates to a preparation method of a 4-propyl-2, 6-piperidinedione compound, and belongs to the field of pharmaceutical chemicals. Specifically, a compound represented by a formula III or a salt thereof reacts with a compound represented by a formula V or a salt thereof in the presence of a reaction accelerator to generate a compound represented by a formula IV or a salt thereof, the invention provides a new preparation method of the 4-propyl-2, 6-piperidinedione compound, and the preparation method is high in yield and high in product purity, in the formula, R1 and R2 are independently selected from hydrogen or C1-C4 alkyl, and R2 is selected from hydrogen or C1-C4 alkyl. And R4 is selected from hydrogen or C1-C4 alkyl.

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.

Disclosed is a novel piperidinedione compound of Formula 1 or a pharmaceutically acceptable salt thereof. Uses of the novel piperidinedione compound of Formula 1 or a pharmaceutically acceptable salt thereof as an anti-tumor agent or an immunomodulatory for treatment of CRBN protein-mediated diseases are disclosed. Also the compound or salt thereof can be used an E3 ligase binder in a PROTAC compound comprising a protein of interest ligand, a linker and an E3 ligase binder. Therefore, a PROTAC compound or a pharmaceutically acceptable salt thereof wherein, as an E3 ligase binder, the compound or salt thereof 1 is connected to the linker is disclosed:

The present disclosure is concerned with piperidinedione compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders associated with the presence of a premature termination codon such as, for example, cystic fibrosis, Duchenne muscular dystrophy, aniridia, Becker muscular dystrophy, spinal muscular atrophy, Hurler syndrome, hemophilia, epidermolysis bullosa (e.g., dystrophic (DEB) form, junctional (JEB) form). Usher syndrome, and cancer, using the compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

The invention provides a preparation method of an IRAK4 targeted protein degradation agent key intermediate, and belongs to the field of drug synthesis. According to the invention, 2-pyrrolidone and a benzimidazolone compound are used as raw materials to prepare a key intermediate of the IRAK4 targeted protein degradation agent, a protecting group is introduced to 2-pyrrolidone, and a reaction route is optimized, so that generation of a by-product 3-bromo-1-(3-methyl-2-oxo-2, 3-dihydro-1H-benzo [D] imidazole-4-yl) piperidine-2, 6-diketone is avoided, and the yield of the IRAK4 targeted protein degradation agent is improved. The product yield is obviously improved, the product is easier to purify, and the method has a wide application prospect and is convenient for industrialization.

The invention discloses a crystal form of a 2, 6-piperidinedione compound and a preparation method of the crystal form, and further discloses application of the crystal form in preparation of drugs for treating related diseases. Specifically disclosed are a crystal form A of a compound of formula (I) and a preparation method thereof.

The present invention relates to a pharmaceutically acceptable salt and a crystal form of a tetrahydronaphthalene derivative, and a preparation method. Specifically, the present disclosure provides a pharmaceutically acceptable salt and a crystal form of (S)-3-(5-(4-((1-(4-((1R,2R)-6-hydroxy-2-isobutyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenyl)piperidin-4-yl)methyl)piperazin-1-yl)-1-oxoisoindolin-2-yl)piperidine- 2,6-dione, and a preparation method therefor. The corresponding salt has good stability and can be better used for clinical treatment.

The invention discloses a radionuclide-labeled isoindole-piperidinedione derivative and application thereof, and the structural formula of the radionuclide-labeled isoindole-piperidinedione derivative is shown in the specification. E3 ubiquitin ligase key protein CRBN is used as a new target for nuclear medicine molecular imaging research; dynamic expression of CRBN in a tumor microenvironment is accurately described by constructing a targeted molecular probe with an isoindole-piperidinedione parent nucleus structure, imaging guidance is provided for clinically and accurately screening benefited people and predicting the therapeutic effect of targeted CRBN, and imaging examples are also provided for researching dynamic expression of other key proteins in a ubiquitination system.

Provided herein are piperidinedione compounds having the following structure (I) wherein RN, R1, R2, R3, R4, L, V, m and n are as defined herein; a composition comprising an effective amount of a piperidinedione compound; and methods for treating or preventing androgen receptor mediated diseases. # imgabs0 #

The invention discloses a piperidinedione compound as well as a preparation method and application thereof. The invention provides compounds as shown in formulas (I) and (II), or pharmaceutically acceptable salts, esters, stereoisomers, tautomers, polymorphs, solvates, isotope labels, metabolites or prodrugs thereof. The compound provided by the invention can be used for degrading proteins such as GSPTl and the like, so that diseases related to protein imbalance are prevented, relieved or treated; meanwhile, the compound provided by the invention can also be used as an effective load of a ligand drug conjugate, so that the adaptation disease range of the compound provided by the invention is further expanded.

Provided herein are piperidinedione compounds having the following structure: (I) wherein RN, R1, R2, R3, R4, RN, L, V, X, a, m, and n are as defined herein; a composition comprising an effective amount of a piperidinedione compound; and methods for treating or preventing androgen receptor mediated diseases. # imgabs0 #

Provided herein are piperidinedione compounds having the following structure: (I), wherein R 1 、R 2 、R 3 、R 4 , L, V, X, A, A', a and m are as defined herein; compositions comprising an effective amount of a piperidinedione compound; and methods for treating or preventing androgen receptor-mediated diseases. #imgabs0#

The invention provides 3-deuterium-enriched 3-(6-, 7-, or 8-substituted-4-oxoquinazolin-3(4H)-yl)-piperidine-2,6-diones, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.

The invention relates to a CDK drug intermediate 3-(3-bromophenyl) piperidine-2, 6-diketone as well as a synthesis method and application thereof, and belongs to the technical field of medicine synthesis. The synthetic method of the CDK drug intermediate 3-(3-bromophenyl) piperidine-2, 6-diketone provided by the invention comprises the following steps: (1) mixing 3-bromobenzyl cyanide and acrylonitrile, slowly dropwise adding benzyltrimethylammonium hydroxide, and refluxing to obtain an intermediate 2-(3-bromophenyl) glutaronitrile; and (2) dissolving the intermediate 2-(3-bromophenyl) glutaronitrile in an acetic acid-concentrated sulfuric acid solution, and carrying out hydrolysis cyclization to obtain the target compound 3-(3-bromophenyl) piperidine-2, 6-diketone. According to the invention, 3-bromophenylacetonitrile is used as an initial raw material, and a target product is prepared only through two simple steps. The method has the advantages of easily available raw materials, short reaction route, simple post-treatment and the like, and is suitable for industrial preparation and production.

Disclosed are compounds of Formula (I): or a stereoisomer, tautomer or salt thereof, wherein R is defined herein. The invention also discloses methods of using such compounds to reduce the levels of Ikaros protein, Helios protein, Ailos protein, and Eos protein, and methods of using such compounds to reduce the levels of Ikaros protein, Helios protein, Ailos protein, and Eos protein; and pharmaceutical compositions comprising such compounds. Such compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

The invention belongs to the field of biological medicine, and particularly relates to a piperidine-2, 6-diketone compound, a pharmaceutical composition and a preparation method and application of the piperidine-2, 6-diketone compound. The piperidine-2, 6-diketone compound provided by the invention can be used for preparing a glutamine cyclase (sQC / gQC) inhibitor and an IKZF1 / 3 or VAV1 targeted degradation agent, provides a new medication choice for clinical treatment of diseases (such as Alzheimer's disease, inflammation, immune related diseases and tumors) which are related to abnormal activity of glutamine cyclase and are abnormally expressed by IKZF1 / 3 or VAV1, and has a broad application prospect. The application prospect is good.

Provided herein in certain aspects are methods of treating lymphoma, the methods comprising administering a CD19 antibody, a CD3xCD20 multispecific antibody, and a 3-(4-amino-1-oxo-1, 3-dihydro-2H-isoindol-2-yl) piperidine-2, 6-dione (Compound A).

This invention provides a method for preparing a key intermediate of an IRAK4-targeting protein degrader, belonging to the field of pharmaceutical synthesis. This invention uses 2-pyrrolidone and benzimidazolone compounds as raw materials to prepare the key intermediate of an IRAK4-targeting protein degrader. By introducing a protecting group onto 2-pyrrolidone and optimizing the reaction route, the generation of the byproduct 3-bromo-1-(3-methyl-2-oxo-2,3-dihydro-1H-benzo[D]imidazol-4-yl)piperidine-2,6-dione is avoided, significantly improving the product yield, making the product easier to purify, and possessing broad application prospects and facilitating industrialization.

The present application relates to a kind of piperidinedione derivatives, its preparation method and the medical use of pharmaceutical composition containing the derivative. Specifically, the present application relates to a kind of piperidinedione derivatives shown in general formula (I), its preparation method and its pharmaceutically acceptable salt, and their purposes as therapeutic agent, especially as VAV1 degradation agent, wherein the definition of each substituent in general formula (I) is the same as the definition in the specification.

The application belongs to the field of biological medicine, and particularly relates to a piperidine-2,6-dione compound, a pharmaceutical composition, and a preparation method and application thereof. The application provides a piperidine-2,6-dione compound, which can be used for preparing a glutamine cyclase (sQC / gQC) inhibitor and an IKZF1 / 3 or VAV1 targeted degrader, and provides a new drug selection for clinically treating diseases (such as Alzheimer's disease, inflammation, immune-related diseases, tumors) related to abnormal glutamine cyclase activity and abnormal expression of IKZF1 / 3 or VAV1, and has a good application prospect.

The invention provides 3-deuterium-enriched 3-(5-substituted-4-oxoquinazolin-3(4H)-yl)-piperidine-2,6-diones, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same, such as in the treatment of cancer, an immune-related disease, or an inflammatory disease.