Patent classifications
C07D215/28
8-HYDROXYQUINOLINE DERIVATIVES AS DIAGNOSTIC AND THERAPEUTIC AGENTS
The present application provides compounds useful in methods of treating neurological disorders such as Alzheimer's disease, and cancer such as prostate cancer. Also provided herein are radiolabeled compounds useful for imaging techniques, and techniques for diagnosis and monitoring of treatment of neurological disorders and cancer. An exemplary radiolabeled compound provided herein is useful as a radiotracer for positron emission tomography or single-photon emission computed tomography. Methods for preparing radiolabeled compounds and methods for preparing unlabeled compounds are also provided.
8-HYDROXYQUINOLINE DERIVATIVES AS DIAGNOSTIC AND THERAPEUTIC AGENTS
The present application provides compounds useful in methods of treating neurological disorders such as Alzheimer's disease, and cancer such as prostate cancer. Also provided herein are radiolabeled compounds useful for imaging techniques, and techniques for diagnosis and monitoring of treatment of neurological disorders and cancer. An exemplary radiolabeled compound provided herein is useful as a radiotracer for positron emission tomography or single-photon emission computed tomography. Methods for preparing radiolabeled compounds and methods for preparing unlabeled compounds are also provided.
HALOGENATED QUINOLINE DERIVATIVES AS ANTIMICROBIAL AGENTS
The present invention provides halogenated quinoline derivatives, such as compounds of Formula (I) or (I), and pharmaceutically acceptable salts thereof, and methods of preparing the halogenated quinoline derivatives. The halogenated quinoline derivatives are expected to be antimicrobial agents and may act through an iron(II)-dependent mode of action. The present invention also provides pharmaceutical compositions, kits, uses, and methods that involve the halogenated quinoline derivatives and may be useful in preventing or treating a microbial infection (e.g., a bacterial infection) in a subject, inhibiting the growth and/or reproduction of a microorganism (e.g., a bacterium), killing a microorganism (e.g., a bacterium), inhibiting the formation and/or growth of a biofilm, reducing or removing a biofilm, and/or disinfecting a surface.
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Nitroxoline prodrug and use thereof
Provided are a nitroxoline prodrug and a use thereof. Specifically, provided are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, a composition containing the compound, and a use thereof in the preparation of anti-infective and antitumor drugs, and definitions of groups in formula (I) are as stated in the specification. The compound represented by formula (I) has better pharmacokinetic parameters such as solubility, blood medicine concentration, or half-life period than nitroxoline. The compound represented by formula (I) can reduce the frequency of drug administration, and has potential for application in other fields other than the field of urinary tracts. ##STR00001##
Thyromimetics with a biphenylmethane scaffold and their use
The invention concerns a compound of Formula (I) or a salt thereof, wherein R.sub.1 is H, (C.sub.1-C.sub.3)alkyl or CF.sub.3; R.sub.2 is H, (C.sub.1-C.sub.3)alkyl or CF.sub.3; A is CH.sub.2COOH, XCH.sub.2COOCH.sub.2CH.sub.3, XCH.sub.2COOH, XCH.sub.2CH.sub.2NH.sub.2, where X is nitrogen or oxygen atom; Ar is an aromatic fragment selected from the group consisting of (Ar1), (Ar2) and (Ar3); where R.sub.3 is H, CH.sub.3, CH.sub.2CH.sub.3 or CH.sub.3CO, R.sub.4 is H or CH.sub.3, R5 is H or CH.sub.3, and R.sub.6 is H or CH.sub.3. The compounds of Formula (I) can be used in the treatment of diseases modulated by thyroid hormone receptor-beta (TRb or TR).
Thyromimetics with a biphenylmethane scaffold and their use
The invention concerns a compound of Formula (I) or a salt thereof, wherein R.sub.1 is H, (C.sub.1-C.sub.3)alkyl or CF.sub.3; R.sub.2 is H, (C.sub.1-C.sub.3)alkyl or CF.sub.3; A is CH.sub.2COOH, XCH.sub.2COOCH.sub.2CH.sub.3, XCH.sub.2COOH, XCH.sub.2CH.sub.2NH.sub.2, where X is nitrogen or oxygen atom; Ar is an aromatic fragment selected from the group consisting of (Ar1), (Ar2) and (Ar3); where R.sub.3 is H, CH.sub.3, CH.sub.2CH.sub.3 or CH.sub.3CO, R.sub.4 is H or CH.sub.3, R5 is H or CH.sub.3, and R.sub.6 is H or CH.sub.3. The compounds of Formula (I) can be used in the treatment of diseases modulated by thyroid hormone receptor-beta (TRb or TR).
PREPARATION METHODS OF QUINOLONE COMPOUNDS AND INTERMEDIATES THEREOF
The present application relates to processes for the preparation of quinolone compounds and intermediates thereof, particularly to processes for the preparation of quinolones and pharmaceutical intermediates of the quinolones. In particular, the present application provides a process for the preparation of a compound of Formula I, and a process for the synthesis of quinolone compounds using the compound of Formula I as an intermediate. The process for the preparation of the compound of Formula I comprises the steps of: reacting a compound of Formula A with R.sup.5NH.sub.2 and R.sup.6Cl in the presence of a base to form the compound of Formula I,
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Methionine Aminopeptidase Inhibitors for Treating Infectious Diseases
The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivative thereof or a pharmaceutical salt thereof.
Methionine Aminopeptidase Inhibitors for Treating Infectious Diseases
The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivative thereof or a pharmaceutical salt thereof.
Methionine Aminopeptidase Inhibitors for Treating Infectious Diseases
The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivative thereof or a pharmaceutical salt thereof.