54 results about "Atropisomer" patented technology

Disclosed in the present invention are a KRAS G12D degradation agent as well as a preparation method therefor and the use thereof. The present invention provides compounds as shown below, and / or stereoisomers, enantiomers, diastereoisomers, atropisomers, deuterated compounds, hydrates, solvates, prodrugs and / or pharmaceutically acceptable salts thereof. The compounds provided by the present invention can effectively degrade and / or inhibit KRAS G12D protein in cells, and can be used for preparing drugs for treating and / or preventing related diseases or disorders caused by KRAS G12D mediation. G-L-E I

The invention provides a pyrimidino heterocyclic compound as well as a pharmaceutical composition and application thereof. The invention provides a pyrimidino heterocyclic compound as shown in a formula I, and a stereoisomer, a tautomer, an atropisomer or a pharmaceutically acceptable salt of the pyrimidino heterocyclic compound. The compound disclosed by the invention has good proliferation inhibition activity on NCI-H358 cells, AsPC-1 cells and Capan-1 cells containing KRAS mutation, and has relatively weak proliferation inhibition activity on PC-9 cells wild in KRAS. # imgabs0 #

To provide an atropisomer of a 1,1'-binaphthyl derivative that exhibits a high HTP value even in small quantities.SOLUTION: The present invention provides an atropisomer represented by, for example, a following structural formula (2.1), a polymerizable liquid crystal composition comprising the atropisomer and a polymerizable liquid crystal compound, an optical film, an image display device and an eyewear.SELECTED DRAWING: None

Disclosed are compounds having the formula (I), or an enantiomer, diastereomer, or tautomer or atropisomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, wherein R1, R2, A and n are defined herein. Also disclosed are methods of preparing such compounds, as well as pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of inflammatory disorders, allergic disorders, skin disorders, mast cell disorders, pain disorders, and pruritus disorders. (I)

The present application provides compounds of Formula (I), or a stereoisomer thereof, or a atropisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of a stereoisomer thereof, or a pharmaceutically acceptable salt of a atropisomer thereof; methods of making the compounds and therapeutic uses thereof. The present application further provides combinations of pharmacologically active agents and pharmaceutical compositions comprising the compounds.

Provided are a bicyclic compound of formula I that achieves a degradative or inhibitory effect on NRF2 by means of activating KEAP1, an isotopically labeled form, an enantiomer, a diastereomer, an atropisomer, or a pharmaceutically acceptable salt thereof, a method for preparing the compound, and use thereof in treating cancers.

The present invention relates to novel heterocyclic compounds of formula (I) as inhibitors of PARG, their pharmaceutically acceptable salts, stereoisomers, solvates, polymorphs, tautomers, atropisomers, optical and geometric isomers, prodrugs, deuterated including other possible isotopes, combinations and use thereof in treating cancer. Formula (I) The present invention also relates to a process for the preparation of novel heterocyclic compounds of Formula (I), pharmaceutical compositions comprising them, and their use in the treatment of cancer.

The invention provides a purine compound as well as a preparation method and application thereof. Specifically, the invention provides a compound as shown in a formula I or pharmaceutically acceptable salts, enantiomers, diastereoisomers, atropisomers, polymorphs, solvates, isotope labeled compounds or racemes thereof. The definition of each substituent group is described in the specification and claims. The purine compound can be used for preparing a CDK12-cyclin K inhibitor and a CDK12-cyclin K degradation agent, and can be used for preparing medicines for treating diseases or symptoms caused by dysfunction of the CDK12-cyclin K. # imgabs0 #

The application belongs to the technical field of power equipment fault diagnosis, and particularly relates to a diagnostic agent suitable for overheat fault early warning of power oil-filled equipment. R The main body skeleton is in a configuration or S The main body skeleton is in a configuration or 1 R is hydrogen, aryl or alkyl; R 2 R is hydrogen, aryl or alkyl; R 2 R is alkyl. The application has the following beneficial effects: the diagnostic agent can be applied to the field of power equipment fault early warning; the early warning mechanism is based on low-energy barrier response, and early fault warning can be realized; the diagnostic principle is based on atropisomerism effect, the reaction path is clear, and a quantitative analysis model can be easily established; the diagnostic agent has good compatibility with insulating oil, insulating paper and metal materials, and does not affect normal operation of the equipment.

The invention discloses a compound as shown in a formula (I-A) for treating cancer, and an isotope label, an enantiomer, a diastereoisomer, an atropisomer or a pharmaceutically acceptable salt thereof. The compound provided by the invention has better inhibitory activity on WRN and has a good application prospect.

The invention belongs to the technical field of organic chemical synthesis, and particularly discloses a pyrazole-pyrrole atropisomer and a synthesis method thereof.The structure of the pyrazole-pyrrole atropisomer is as shown in the formula I. The method comprises the steps that 1, 4-diketone derivatives, aminopyrazole and a chiral protonic acid catalyst are sequentially added into a dry reaction container, stirring is performed for 1-3 h, and a reaction solution is obtained; and then adding an organic solvent as a reaction medium, and stirring at a certain temperature until the reaction is finished to obtain the axially chiral pyrazole-pyrrole atropisomer. The synthesis method disclosed by the invention has the advantages of high target compound yield, easiness in purification, excellent enantioselectivity, wide substrate application range, simplicity and convenience in post-treatment and the like.

The present disclosure relates to novel compounds according to general Formula I or a pharmaceutically acceptable acid or base addition salts, hydrate, solvate, N-oxide, stereo chemically isomer forms, in particular diastereoisomer, enantiomer or atropisomers, or mixtures thereof, a polymorph or ester thereof. The present disclosure also relates to a pharmaceutical composition comprising a compound or prodrug thereof of Formula I for use in the treatment of conditions influenced by homologous recombination DNA repair pathway and wild-type, mutant and other BRCA1 and / or BRCA2 deficiencies, namely therapy or treatment of cancer.

The present application relates to an amide compound, a pharmaceutical composition thereof, and use thereof. The amide compound is selected from a compound of formula (I), a tautomer thereof, a mesomer thereof, a racemate thereof, an enantiomer thereof, a diastereomer thereof, an atropisomer thereof, and a pharmaceutically acceptable salt thereof. The present application develops a series of novel amide compounds. The amide compound has excellent anti-HIV activity and the ability to inhibit HIV capsid protein binding, and is suitable for intravenous administration, oral administration, and subcutaneous administration. The amide compound has a long half-life and high drug exposure in vivo, and thus possesses the potential to develop long-acting drugs. Also, the amide compound has good metabolic stability, low or medium penetrability and a high protein binding rate in cells, no significant inhibitory effects on various CYP enzymes, and high safety. The amide compound is promising for use against HIV infection.

The present application relates to an amide compound and its use, the amide compound is selected from the compound shown in formula (I), its tautomer, its endo racemate, its exo racemate, its enantiomer, its diastereoisomer, its atropisomer or its pharmaceutically acceptable salt. The present application develops a series of novel amide compounds, these amide compounds have excellent anti-HIV virus activity, and no obvious cytotoxicity, strong affinity to HIV-1 capsid protein, good specificity; suitable for intravenous administration, oral administration, subcutaneous administration, intramuscular administration mode, long half-life in vivo and high exposure; at the same time, the amide compound has no obvious inhibition to various CYP enzymes, shows high plasma protein binding, excellent safety and good metabolic stability in vivo, no potential off-target effect, high safety, and has the potential to develop into a clinical long-acting drug.

Solid-state forms of (S)-2-(3-(1-(5,5-dimethylpyrrolidine-2-carbonyl)-piperidine-4- carbonyl)-2-methyl-1H-pyrrolo[2,3-c]pyridin-1-yl)-5-fluoro-N,N-diisopropylbenzamide, Atropisomer A-2; corresponding pharmaceutical compositions; uses to treat and / or prevent Menin- mediated conditions; kits; and methods of preparation.

The present invention relates to a bicyclic-type MAT2A inhibitor and use thereof. Specifically, the present invention discloses a bicyclic compound represented by formula (I) or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a racemate, an atropisomer, a polymorph, a solvate, or an isotope labeled compound thereof. The compound represented by formula (I) has MAT2A enzyme inhibitory activity, can be used as a good MAT2A inhibitor, and is further used for preparing drugs for treating and / or preventing MTAP-related diseases, especially tumors.

Disclosed in the present invention are a nitrogen-containing heteroaryl compound, a preparation method therefor and the use thereof. The present invention specifically relates to a compound represented by formula (I) for treating cancer, and an isotope-labelled substance, enantiomer, diastereomer, atropisomer, solvate, prodrug or pharmaceutically acceptable salt thereof. The compound of the present invention has good inhibitory activity against WRN, and has good application prospects.

To provide compounds for therapeutically and / or prophylactically treating cancers containing KrasG12D mutations.SOLUTION: Provided is a compound represented by the following formula (I) or a stereoisomer, an atropisomer, a tautomer or a pharmaceutically acceptable salt thereof: Wherein X is O or NR6, m and n are 1 or 2, and R5 is independently halogen, oxo, unsubstituted C1-3 alkyl or unsubstituted C1-3 haloalkyl; or two R5 taken together form a bridge between two carbons of ring A, the bridge comprising 1 to 3 carbons and optionally 1 heteroatom selected from O and N.SELECTED DRAWING: None

The present disclosure relates to a novel ALPK1 inhibitor of formula (I), or a pharmaceutically acceptable salt, stereoisomer, tautomer, atropisomer, stable isotope variant, prodrug, or crystalline form thereof. The disclosure also relates to pharmaceutical compositions comprising said novel ALPK1 inhibitors, and their use in the treatment of inflammatory related diseases, such as ROSAH syndrome, inflammatory bowel disease (IBD), NASH, gout, diabetes, chronic kidney disease, pancreatitis, Kawasaki disease, inflammatory skin disease, and neurodegenerative diseases including Alzheimer's disease.

To provide pyrazolyl derivative compounds; their use for inhibiting KRAS G12C, HRAS G12C, or NRAS G12C, particularly KRAS G12C; methods for treating or preventing diseases, especially cancer, by using the compounds; and methods and intermediates for producing the compounds.SOLUTION: The present application relates to a compound of formula (I), or a stereoisomer thereof, or an atropisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer, or a pharmaceutically acceptable salt of the atropisomer; a method for producing the compound; and its therapeutic use. The present application further provides a pharmaceutical composition comprising the compound and a combination of pharmacologically active substances.SELECTED DRAWING: None

The present invention relates to a heterocyclic compound, a pharmaceutical composition thereof, and a use thereof. Specifically, the present invention relates to a compound of formula (I), a stereoisomer thereof, an atropisomer thereof, a deuterated derivative thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of the stereoisomer thereof, a pharmaceutically acceptable salt of the atropisomer thereof, a pharmaceutically acceptable salt of the deuterated derivative thereof, or a solvate of any one of the foregoing. The compound exhibits significantly high inhibitory activity against KYSE70 cancer cells and has good pharmacokinetic properties.

The present disclosure provides atropisomers of pyridazinone derivatives of a compound of Formula 1a and Formula 1b, N-oxides or salts thereof, wherein R1, R2, R3, R4 and R5 are defined in the disclosure. Also disclosed is a composition containing a compound of Formula 1a or 1b, and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound of Formula 1a or 1b or a composition thereof. Also disclosed are methods for preparing a compound of Formula I.

This disclosure provides atropisomers of pyridazinone derivatives of a compound of formula 1a and formula 1b, N-oxides or salts thereof (see Formulas), wherein R1, R2, R3, R4, and R5 are defined herein. Also disclosed is a composition containing a compound of formula 1a or 1b and methods for controlling unwanted vegetation comprising contacting the unwanted vegetation or its surroundings with an effective amount of a compound of formula 1a or 1b, or a composition thereof. Methods for preparing a compound of formula I are also disclosed.

To provide an atropisomer of a specific pyridazinone derivative, a method for preparing the same, and a herbicidal composition containing the specific compound.SOLUTION: There is provided an optically active compound selected from the atropisomers of Formula 1a and Formula 1b, their N-oxides or salts, wherein said atropisomers of Formula 1a or 1b, their N-oxides or salts have a plus (+) rotation value and exist over their corresponding enantiomers, or their N-oxides or salts.SELECTED DRAWING: None

The present invention relates to a compound for treating thrombotic diseases. Specifically, the present invention provides a compound represented by formula I, or a pharmaceutically acceptable salt, or an enantiomer, or a diastereoisomer, or an atropisomer, or a racemate, or a polymorph, or a solvate, or an isotopically labeled derivative thereof. The compound disclosed in the present invention can be specifically combined with SH3 domain protein of Src kinase and then interfere the combination of integrin αIIbβ3 and Src kinase, so that outside-to-inside signal transduction is selectively inhibited and inside-to-outside signal transduction is not influenced; thus, while resisting thrombus, the compound of the present invention does not affect the normal physiological hemostatic function, prevents the occurrence of hemorrhagic side effect, and can be used as a new generation of effective medicine for preventing and treating thrombosis-related cardiovascular and cerebrovascular diseases.

The present application provides an amide compound and a use thereof. The amide compound is selected from a compound represented by formula (I), a tautomer thereof, a mesomer thereof, a racemate thereof, an enantiomer thereof, a diastereomer thereof, an atropisomer thereof, or a pharmaceutically acceptable salt thereof. In the present application, a series of novel amide compounds is developed. These amide compounds have excellent anti-HIV activity, no significant cytotoxicity, relatively strong affinity for HIV-1 capsid protein, and good specificity, are suitable for intravenous administration, oral administration, subcutaneous administration, and intramuscular injection administration, and show relatively long half-life and relatively high exposure in vivo. In addition, the amide compounds have no significant inhibitory effect on various CYP enzymes, exhibit high plasma protein binding, and have excellent safety and good metabolic stability in vivo, no potential off-target effect, high safety, and the potential to be developed into clinical long-acting drugs.

The invention provides a multi-chiral-center non-biaryl organosilicone atropisomer and a preparation method and application thereof, and the structural formula of the multi-chiral-center non-biaryl organosilicone atropisomer is as shown in formula (I), the synthesis method of the multi-chiral-center non-biaryl organosilicone atropisomer specifically comprises the following steps: in the presence of a phosphine ligand, a nickel catalyst and a reaction medium, carrying out silicon-carbon bond activation on non-biaryl aldehyde and benzo silacyclobutane to carry out ring expansion reaction. According to the present invention, the reaction condition is mild, the operation is simple, the substrate universality is strong, the crude product is subjected to rapid column chromatography impurity removal, vacuum concentration is performed to obtain the pure product, the post-treatment is convenient, the finally obtained product has high stereoselectivity, and the non-biaryl organosilicon atropisomer contains a plurality of functional groups and a plurality of chiral centers, has potential biological activity, and can be used for the preparation of the non-biaryl organosilicon atropisomer. The compound can be used as a fine chemical intermediate to be widely applied to various organic reactions and drug synthesis, and has considerable application value.

The present invention relates to a compound or pharmaceutically acceptable salt, hydrate, solvate, N-oxide, stereoisomer, diastereoisomer, enantiomer, atropisomer, dimer or polymorph for use in medicine comprising the following chemical formula (I): wherein R 1 , R 2 and R 3 are selected independently of each other; R 1 is selected from aryl or heterocycle; R 2 is selected from H, alkyl, aryl, alkoxy, halogen, hydroxyl, amine, carbonyl or heterocycle; R 3 is selected from H or (II).