C07B59/002

COMPOUND USED AS RET KINASE INHIBITOR AND APPLICATION THEREOF

The present invention relates to the technical field of medicines. Specifically disclosed is a compound as represented by formula I′, or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, symbols therein being as defined in the claims. The compound of the present invention may be used as a drug for regulating RET kinase activity or treating RET-related diseases, and has good pharmacokinetic properties.

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ORGANIC LIGHT-EMITTING ELEMENT

Provided is an organic light emitting device including a light emitting layer comprising a compound of Chemical Formula 1 and a first organic material layer comprising a compound of Chemical Formula 2:

##STR00001## wherein: Cy1 to Cy5 are each independently one selected from among a substituted or unsubstituted: aromatic hydrocarbon ring, aliphatic hydrocarbon ring, and aromatic hetero ring, or a ring in which two or more rings selected from the above group are fused, one or more of Cy1 to Cy5 are a ring of Chemical Formula 1-A:

##STR00002## one to three of a* to d* are a position fused to or linked to Chemical Formula 1;

##STR00003## L1 to L3 are each independently a direct bond or a substituted or unsubstituted: arylene or divalent heterocyclic group; and Ar1 and Ar2 are each independently a substituted or unsubstituted: aryl or heterocyclic group.

INTERMEDIATE, PREPARING METHOD THEREOF, AND METHOD OF PREPARING DRUG

An intermediate is provided herein, and it has the structure shown in the formula (1) as follows:

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formula (1). In the formula (1), R.sub.1 is —Cl, —Br, —I, —OSO.sub.2CF.sub.3, —B(OH).sub.2, or

##STR00002##

R.sub.2 is —F, —.sup.18F, —Cl, —Br, —I, —SnMe.sub.3, —SnBu.sub.3, —B(OH).sub.2, or

##STR00003##

and A is a chiral auxiliary.

In vivo imaging of matrix metalloproteinases in lung disease

The present invention provides a method of imaging a subject's lung which comprises contacting the subject's lung with a matrix metalloproteinase inhibitor labeled with a radioisotope under conditions such that the inhibitor binds to matrix metalloproteinase in the lung, and then imaging the radiolabeled inhibitor bound to matrix metalloproteinase in the subject's lung. The invention also provides Ro 32-3555 labeled with a radioisotope.

Stabilized radiolabelling reaction

The present invention provides a method for the synthesis of an injectable composition comprising a [.sup.18F]-labelled pyridaben derivative that is advantageous over prior methods. In particular, the method of the present invention comprises a method of radiosynthesis that permits a more facile purification using solid phase extraction (SPE).

METHODS FOR PRACTICAL SYNTHESIS OF DEUTERATED AMINO ACIDS
20230023607 · 2023-01-26 ·

Disclosed are a deuterated compound of fomula (I), or a salt thereof, and methods for preparation thereof. The present disclosure may provide a mild, versatile organophotoredox method for the preparation of diverse, enantioenriched α-deuterated α-amino acids. In particular, the present disclosure may address the long-standing challenge of installing sterically demanding side chains into α-amino acids, including late-stage modifications on medicinal agents and natural products.

Organic compounds

This invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT.sub.2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D.sub.1/D.sub.2 receptor signaling systems, and/or the treatment of residual symptoms.

COMPOUNDS, COMPOSITIONS, AND METHODS

The present disclosure relates generally to LRRK2 inhibitors, or a pharmaceutically acceptable salt, deuterated analog, prodrug, tautomer, stereoisomer, or mixture of stereoisomers thereof, and methods of making and using thereof.

Quinazolinone derivative, preparation method therefor, pharmaceutical composition, and applications

Disclosed are a quinazolinone derivative, a preparation method therefor, a pharmaceutical composition, and applications. Provided are a compound represented by formula I, a pharmaceutically acceptable salt, a solvate, a crystal form, a eutectic crystal, a stereoisomer, an isotope compound, a metabolite, or a prodrug thereof. Generation or activity of a cell factor can be regulated, and accordingly, cancers and inflammatory diseases can be effectively treated. ##STR00001##

AMIDE-SUBSTITUTED HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF CONDITIONS RELATED TO THE MODULATION OF IL-12, IL-23 AND/OR IFN-ALPHA

Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.