71 results about "Atropisomer" patented technology

Provided herein are compounds of Formula (I) or tautomers, atropisomers, stereoisomers, or pharmaceutically acceptable salts thereof. These compounds are useful as KRAS mutant degraders and / or inhibitors.

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 #

Provided herein is a process 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 racemized compound A. Also provided is a process for isolating (P)-compound A from a composition comprising (P)-compound A and a tartrate, as described herein. Further provided herein, is a process for isolating a free acid of a tartrate or a hydrate thereof from a composition comprising a tartrate, (P)-compound A, and an organic solvent.

The invention relates to PRMT5 inhibitors of formula (I), a stereoisomer thereof, an atropisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of the stereoisomer thereof, a pharmaceutically acceptable salt of the atropisomer thereof, or a deuterated molecule thereof, and pharmaceutical compositions thereof, as well as the use thereof.

The invention discloses a heterocyclic aryl or heteroaryl-heteroaryl derivative and application of the heterocyclic aryl or heteroaryl-heteroaryl derivative. The heterocyclic aryl or heteroaryl-heteroaryl derivative of the present invention is a compound of formula (I), a stereoisomer thereof, an atropisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of a stereoisomer thereof, a pharmaceutically acceptable salt of an isomer thereof, a solvate thereof or a pharmaceutically acceptable salt of a solvate thereof. The compound disclosed by the invention has good inhibitory activity on a 20-hydroxyeicosatetraenoic acid (20-HETE) signal channel, and has a good medicinal prospect. # 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.

The present application relates to a compound of formula (I) for inhibiting Toll-like receptor 8 (TLR8) activity, 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 or a pharmaceutically acceptable salt of the deuterated derivative thereof, and a method for preparing the compound, a composition thereof and the use thereof.

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 invention relates to a continuous method for the production of a chemical compound A, comprising: – provision of a mixture comprising the chemical compound A and a chemical compound B which is an atropisomer of the chemical compound A; – chromatographic separation of the mixture so as to collect a fraction rich in chemical compound A and a fraction rich in chemical compound B; – a racemisation treatment of the fraction rich in chemical compound B, in which the chemical compound B is partially converted into chemical compound A, so as to obtain a racemised fraction; – recycling of the racemised fraction to the step of chromatographic separation of the mixture. The invention also relates to a plant for implementing this method.

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 invention provides a cyclobutyl dihydroquinoline sulfonamide compound of Formula (I),an enantiomer, diastereoisomer, atropisomer thereof, a mixture thereof, or a pharmaceutically acceptable salt thereof, that inhibits voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders, cough, and itch. Also provided arc pharmaceutical compositions containing the compounds of the present invention. Also further provided is an atropi-selective preparation of said compounds of Formula (I), and intermediate thereof.

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.

The present invention discloses a class of pyridazinone compounds, their preparation and applications, specifically a pyridazinone compound represented by general formula I, or a pharmaceutically acceptable salt thereof, or an enantiomer, diastereomer, tautomer, atropisomer, solvate, polymorph or prodrug thereof, a preparation method thereof and pharmaceutical applications thereof, wherein the definitions of each group are as described in the specification.

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.