C07B59/002

METHODS OF MANUFACTURING BENZOQUINOLINE COMPOUNDS
20230060294 · 2023-03-02 ·

The present invention relates to new methods of manufacturing benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), and intermediates thereof.

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Crystal form of monomethanesulfonate of deuterated 3-(4,5-substituted aminopyrimidine)phenyl compound and preparation method therefor

Disclosed in the present invention are a crystal form of monomethanesulfonate of a deuterated 3-(4,5-substituted aminopyrimidine)phenyl compound as represented by formula I, and a preparation method therefor. The crystal form is highly stable, can be used for treatment or prevention of diseases or conditions by means of epidermal growth factor receptors (EGFRs) in some mutation forms, can effectively inhibit the growth of a variety of tumor cells, and have an inhibiting effect on other proteases of EGFR and Her families, and thus can be used for preparing antitumor drugs.

Tricyclic compounds as histone methyltransferase inhibitors

The present disclosure provides certain tricyclic compounds that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

DEUTERATED ANALOGS OF ELACRIDAR
20230158013 · 2023-05-25 · ·

The present invention relates to efflux inhibitor compounds, compositions, and methods of using the same. More specifically, the instant invention comprises deuterated analogs of elacridar with superior pharmacokinetic properties such that it is now possible to facilitate accumulation and distribution of therapeutic agents to effective levels in cells or compartments protected by efflux transporter proteins such as Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP). Such transporter protected compartments include brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, stem cells, and solid tumors. In other embodiments, the present invention comprises methods of using the instant deuterated analogs.

COMPOUND FOR ORGANIC ELECTRIC ELEMENT, ORGANIC ELECTRIC ELEMENT USING SAME, AND ELECTRONIC DEVICE THEREOF

Provided are a compound which can improve the luminous efficiency, stability, and service life of an element; an organic electric element using same; and an electronic device thereof.

AZEPINO-INDOLES FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
20230159544 · 2023-05-25 ·

Disclosed herein are compounds of Formulae I or II,

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or an isotopically enriched compound thereof, or a pharmaceutically acceptable salt thereof, methods for making the compounds, and methods for their use.

COMPOUND AND RADIOACTIVE LABELING COMPOUND

In a compound of the present invention, in a macroscopic view of a chemical structure thereof, a chelating moiety is located at the center of the structure, an atomic group containing an albumin binding moiety binds to one side of the chelating moiety, and an atomic group containing a target molecule binding moiety binds to the other side of the chelating moiety. The chelating moiety is also preferably DOTA or a derivative thereof. The target molecule binding moiety preferably has a structure to bind to a target molecule expressed in a cancer tissue. The present invention also provides a radioactive labeled compound in which the compound is coordinated to a radioactive metal ion.

Bicyclic compounds for diagnosis and therapy

The present invention relates to novel compounds that can be employed in the diagnosis, monitoring of disease progression or monitoring of drug activity, of a group of disorders and abnormalities associated with alpha-synuclein (α-synuclein, A-synuclein, aSynuclein, A-syn, α-syn, aSyn) aggregates including, but not limited to, Lewy bodies and/or Lewy neurites, such as Parkinson's disease. The instant compounds are particularly useful in determining a predisposition to such a disorder, monitoring residual disorder, or predicting the responsiveness of a patient who is suffering from such a disorder to the treatment with a certain medicament. The present compounds can also be used to treat, alleviate or prevent a disorder or abnormality associated with alpha-synuclein aggregates.

COMPOUND AND ORGANIC LIGHT EMITTING DEVICE COMPRISING SAME

A compound represented by Formula 1 and an organic light emitting device including the same, and the compound providing improved efficiency and service life characteristics when the compound is applied to an organic material layer of the organic light emitting device.

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FORMULATIONS OF PSMA IMAGING AGENTS

The present invention relates to formulations of radiolabeled compounds that are of use in radiotherapy and diagnostic imaging related to prostate specific membrane antigen (PSMA).