C07D215/46

ASYMMETRIC BISAMINOQUINOLINES AND BISAMINOQUINOLINES WITH VARIED LINKERS AS AUTOPHAGY INHIBITORS FOR CANCER AND OTHER THERAPY

The invention provides novel asymmetric and symmetric bisaminoquinolmes and related compounds, methods of treatment and syntheses. The novel compounds exhibit effective anticancer activity and are useful in the treatment of a variety of autophagy-related disorders.

Inhibitors of Low Molecular Weight Protein Tyrosine Phosphatase and Uses Thereof

Herein are provided, inter alia, compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and methods of using the same. In embodiments, the compound has a structure according to Formula (I-A).

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Inhibitors of Low Molecular Weight Protein Tyrosine Phosphatase and Uses Thereof

Herein are provided, inter alia, compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and methods of using the same. In embodiments, the compound has a structure according to Formula (I-A).

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COMPOUNDS FOR PREVENTING, INHIBITING, OR TREATING CANCER, AIDS AND/OR PREMATURE AGING

The manufacture and use of compounds of formula (Ia) or a pharmaceutically acceptable salt thereof for preventing, inhibiting or treating cancer, AIDS and/or premature aging. The compounds of formula (Ia) being:

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where: R independently represents a hydrogen atom, a halogen atom, a (C.sub.1-C.sub.3)alkyl group, a —CN group, a hydroxyl group, a —COOR.sub.1 group, a (C.sub.1-C.sub.3)fluoroalkyl group, a —NO.sub.2 group, a —NR.sub.1R.sub.2 group, or a (C.sub.1-C.sub.3)alkoxy group; R′ is a hydrogen atom, a halogen atom, a (C.sub.1-C.sub.3)alkyl group, a —NO.sub.2 group, a (C.sub.1-C.sub.3)alkoxy group, or a —NR.sub.1R.sub.2 group; and R.sub.1 and R.sub.2 are a hydrogen atom or a (C.sub.1-C.sub.3) alkyl group.

ANTIMALARIAL COMPOUNDS

Antimalarial compounds of the formula: in which n is 1 or 2; X is C or N; R.sub.1 is a moiety comprising a secondary amine and a tertiary amine joined by a C.sub.2 to C.sub.4 alkyl chain; and R.sub.2 is CF.sub.3, F, or H, or an analog, combination, derivative, prodrug, stereoisomer, or pharmaceutically acceptable salt thereof. Pharmaceutical compounds including the antimalarial compounds. Methods of treating or preventing malaria comprising administering an effective amount of the antimalarial compounds.

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ANTIMALARIAL COMPOUNDS

Antimalarial compounds of the formula: in which n is 1 or 2; X is C or N; R.sub.1 is a moiety comprising a secondary amine and a tertiary amine joined by a C.sub.2 to C.sub.4 alkyl chain; and R.sub.2 is CF.sub.3, F, or H, or an analog, combination, derivative, prodrug, stereoisomer, or pharmaceutically acceptable salt thereof. Pharmaceutical compounds including the antimalarial compounds. Methods of treating or preventing malaria comprising administering an effective amount of the antimalarial compounds.

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PROCESS FOR THE PREPARATION OF A SUBSTITUTED IMIDAZOQUINOLINE
20220144822 · 2022-05-12 ·

The present invention relates to a process for synthesizing N-(4-(4-amino-2-(2-methoxyethyl)-1H-imidazo[4,5-c]quinolin-1-yl)butyl)-N-(tetrahydro-2H-pyran-4-yl)acetamide, an imidazoquinoline derivative useful as toll-like receptor agonist, in particular as an agonist of TLR7, which promotes induction of certain cytokines. Furthermore, the present invention also provides intermediates useful in the synthesis of N-(4-(4-amino-2-(2-methoxyethyl)-1H-imidazo[4,5-c]quinolin-1-yl)butyl)-N-(tetrahydro-2H-pyran-4-yl)acetamide.

PROCESS FOR THE PREPARATION OF A SUBSTITUTED IMIDAZOQUINOLINE
20220144822 · 2022-05-12 ·

The present invention relates to a process for synthesizing N-(4-(4-amino-2-(2-methoxyethyl)-1H-imidazo[4,5-c]quinolin-1-yl)butyl)-N-(tetrahydro-2H-pyran-4-yl)acetamide, an imidazoquinoline derivative useful as toll-like receptor agonist, in particular as an agonist of TLR7, which promotes induction of certain cytokines. Furthermore, the present invention also provides intermediates useful in the synthesis of N-(4-(4-amino-2-(2-methoxyethyl)-1H-imidazo[4,5-c]quinolin-1-yl)butyl)-N-(tetrahydro-2H-pyran-4-yl)acetamide.