30 results about "Atropisomer" patented technology

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 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 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.

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 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 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).

The disclosure is directed to novel ALPK1 inhibitors having the Formula (I), or a pharmaceutical acceptable salt, a stereoisomer, a tautomer, an atropisomer, a stable isotopic variant, a prodrug, or a crystal form thereof. The disclosure is also directed to pharmaceutical composition comprising the novel ALPK1 inhibitors, and use thereof in treating inflammation related diseases, such as ROSAH syndrome, inflammatory bowel disease (IBD), NASH, gout, diabetes, chronic kidney disease, pancreatitis, Kawasaki disease, inflammatory skin diseases and neurodegenerative diseases including the Alzheimer's disease.

Provided herein is a method comprising heating a composition comprising (P)-Compound A or a salt thereof and a solvent to a temperature of 250 °C to 350 °C to form racemic Compound A. Also provided is a method for isolating (P)-Compound A from a composition comprising (P)-Compound A and a tartrate salt as described herein. Further provided herein is a method for isolating a free acid of a tartrate salt or a hydrate thereof from a composition comprising a tartrate salt, (P)-Compound A, and an organic solvent. [INSERT STRUCTURE] (A).

Compounds of formula (I) represented by formula (Ia), or formula (Ib) wherein the substituents are as defined in claim 1, or agrochemically acceptable salts, stereoisomer, enantiomer, tautomer, atropisomer, and / or N-oxides of those compounds, can be used as insecticides.

This disclosure provides chemical entities (e.g., a compound, or a pharmaceutically acceptable salt thereof, or an atropisomer thereof; or a pharmaceutically acceptable salt of an atropisomer) that modulate (e.g., inhibit) the interaction between menin and mixed-lineage leukaemia ("MLL") proteins (e.g., MLL fusion proteins). The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a condition, disease or disorder in which aberrant (e.g., increased, e.g., excessive) menin-MLL interaction contribute to the pathology, symptoms and / or progression of the condition, disease or disorder (e.g., cancer, diabetes). This disclosure also provides compositions containing the chemical entities as well as methods of making and using the same....

The application discloses a kind of fused heterocyclic compounds, preparation method and purposes thereof.The specific, the application discloses a kind of compound shown in formula (I) for treating cardiovascular disease, its isotope marker, enantiomer, diastereoisomer, atropisomer or its pharmaceutically acceptable salt.The compound of the application can be used as NPR1 positive allosteric modulator, and has good application prospect.

Disclosed are compounds having the formula (I), or an enantiomer, diastereomer, tautomer or atropisomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, A, and n are defined herein. Also disclosed are methods of making 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)

To provide cyclobutyl dihydroquinoline sulfonamide compounds.SOLUTION: The present invention provides a cyclobutyl dihydroquinoline sulfonamide compound of formula (I) in the figure, an enantiomer, diastereoisomer, atropisomer thereof, a mixture thereof, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders, cough, and itch.SELECTED DRAWING: None

The application provides a diaryl N-oxide atropisomer and use thereof, and belongs to the technical field of chemical medicines.The diaryl N-oxide atropisomer is a compound shown in formula I, a salt or a stereoisomer thereof.A new strategy for synthesizing a diaryl heteroaromatic N-oxide is developed by constructing a novel heteroaromatic N-oxide ring.The copper-catalyzed novel heteroaromatic N-oxide ring synthesis can efficiently construct various novel N-oxide skeletons, and high yield and excellent enantioselectivity are achieved.The compound synthesized by the application can be used as an efficient and recyclable Lewis base organic catalyst for asymmetric allylation of aldehydes;meanwhile, the compound synthesized by the application also has excellent antitumor effect.The application promotes the synthesis of novel structure heteroaromatic N-oxide, and lays a foundation for developing excellent heteroaromatic N-oxide.