52 results about "Atropisomer" patented technology

Atropisomers of 3-substituted-4-arylquinolin-2-one derivatives having the general formula

wherein R, R¹, R², R³, R⁴ and R⁵, are as defined herein, or a non-toxic pharmaceutically acceptable salt, solvate or prodrug thereof. The atropisomers can modulate the large conductance calcium-activated K⁺ channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels. In addition, the atropisomers can be stable, i.e., do not interconvert, for periods of up to one month, or more.

The invention discloses synthesis for chiral polyester containing binaphthyl. A binaphthyl compound is a common atropisomer compound with a C3 chiral axis. The axis of a binaphthyl structure is in an asymmetrical, multifunctional and stable chiral form, so that molecules and copolymers constructed by binaphthyl have superior structures and properties and wide application prospects in the field of materials. The patent is developed mainly around the synthesis of novel chiral polyester containing binaphthyl. A method for preparing the chiral polyester comprises the following steps of: synthesizing binaphthol or dinaphthyline by taking 2-naphthol or 2-naphthylamine as a raw material, and splitting to obtain chiral binaphthol or dinaphthyline; making dinaphthyline react with halohydrinare to obtain diol containing dinaphthalene radial, and react with the diacid to obtain chiral polyester; and making naphthidine react with chloride acyl chloride, hydrolyzing to obtain diol containing binaphthyl, and reacting with diacid to obtain chiral polyester containing binaphthyl. In the preparation of the chiral polyester, diol or diacid containing binaphthyl is prepared firstly, and then the chiral polyester is prepared by reacting. At last, the prepared chiral polyester is applied to molecular recognition.

The invention relates to two novel substances, namely (1R,2S,3S,4R)-3-acetoxy-1,2,4,5-tetrahydroxy-7-methoxy-2-methyl-1,2,3,4-tetrahydroanthracene-9,10-dione (3-O-acetyl altersolanol M)

and 8-(4,5,6-trihydroxy-7-methyl-2-methoxy-9,10-dioxo-9H,10H-anthracen-1-yl)-(1S,2S,3R,4S)-1,2,3,4,5-pentahydroxy-7-methoxy-2-methyl-1,2,3,4-tetrahydro-9H,10H-anthracene-9,10-dione (the atropisomers alterporriol I and J)

to their use as anti-infectives and as anti-cancer agents, as well as to methods of producing the same.

Disclosed are compounds of Formula (I): or a salt thereof, wherein Q is: or; and X, R_1a, R_1b, R₃, R₄, and R₅ are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

The present invention relates to novel compounds that can act as antidotes for treating “Acute Cannabinoid Overdose” produced by classical cannabinoids such as Δ⁹-tetrahydrocannabinol (THC) and several synthetic psychoactive cannabinoids (SPCs). The cannabis constituent THC exerts its psychotropic effects via CB1 receptor activation and SPCs mimic the effects of THC with higher potency and severe neurotoxicity. Compounds disclosed in this invention, their enantiomers, diastereomers, geometric isomers, racemates, tautomers, rotamers, atropisomers, metabolites, N-oxides, salts, solvates, hydrates, isotopic variations and their polymorphic forms can be therapeutically useful in an emergency setting for counteracting the intoxicating effects of acute THC ingestion and SPC overdose. Also, aspects of the invention are concerned with pyrazoles, imidazoles, triazoles, thiazoles, oxazoles, dihydropyrazoles, pyrrolidinones, azetidines, oxyazetidines and azaspiro[3.3]heptanes with unique pharmacokinetic and pharmacodynamic properties for treating “Acute Cannabinoid Overdose”.

The invention relates to a compound for treating thrombotic diseases. Specifically, the invention provides a compound as shown in a formula I, or a pharmaceutically acceptable salt thereof, or an enantiomer thereof, or a diastereoisomer thereof, or an atropisomer thereof, or a raceme thereof, or a polymorphic substance thereof, or a solvate thereof, or an isotope labeled derivative thereof. After the compound disclosed by the invention is specifically combined with an SH3 structural domain protein of Src kinase, the interference integrin alpha IIb beta 3 is combined with the Src kinase, so that signal transduction from outside to inside is selectively inhibited, and the signal transduction from inside to outside is not influenced, so that the compound disclosed by the invention does not influence a normal physiological hemostasis function while resisting thrombus, and avoids side effects, and the compound can become a new generation of effective medicine for preventing and treating thrombus-related cardiovascular and cerebrovascular diseases.

The present invention relates to a bromodomain inhibitor. Provided are a compound represented by general formula I or a pharmaceutically acceptable salt, enantiomer, diastereomer, atropisomer, racemate, polymorph, solvate, or isotopically labeled compound (including deuterium substitution) thereof, a preparation method of the same, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof.