C07D215/42

SUBSTITUTED CONDENSED AZINES AS ANTHELMINTIC COMPOUNDS
20230174492 · 2023-06-08 ·

The present invention relates to novel anthelmintic compounds of general formula (I):


T-L-A   (I)

wherein A is A1 or A2

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#.sup.2 indicates the binding position between the group L and A, T is a group T.sup.1-T.sup.6, L is a group L.sup.1-L.sup.10, and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and Q are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.

Type 4 prepilin peptidase inhibitors and methods of use

Compounds for inhibiting Type 4 Prepilin Peptidases are provided as are methods of using the compounds as anti-bacterial agents.

Type 4 prepilin peptidase inhibitors and methods of use

Compounds for inhibiting Type 4 Prepilin Peptidases are provided as are methods of using the compounds as anti-bacterial agents.

Mechanism of resistance to bet bromodomain inhibitors

The present disclosure provides combination therapy comprising a BET inhibitor and a protein phosphatase 2A (PP2A) activator, a B-cell lymphoma-2 (Bcl-2) inhibitor, a B-cell lymphoma-extra large (Bcl-xl) inhibitor, a casein kinase 2 (CK2) inhibitor, and/or a mediator complex subunit 1 (MED1) for cancer. The combination therapy is expected to be synergistic in treating the cancer, compared to the monotherapy. Methods for identifying a subject having a cancer that is resistant to or at risk of developing resistance to bromodomain and extra terminal (BET) inhibitor therapy are also provided.

Quinoline derivatives and their applications

The invention relates to a series of quinoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs. Thereof M, R.sub.1, R.sub.2, X, Y and n are defined as claims. And the compounds of general formula I show potent inhibitory activity against c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer. ##STR00001##

Quinoline derivatives and their applications

The invention relates to a series of quinoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs. Thereof M, R.sub.1, R.sub.2, X, Y and n are defined as claims. And the compounds of general formula I show potent inhibitory activity against c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer. ##STR00001##

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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Histone deacetylase 6 inhibitors and use thereof

Disclosed is hydroxamic acid compounds of Formula (I) set forth herein. Also disclosed are a pharmaceutical composition containing such a compound and a method of using the compound for treating a condition associated with histone deacetylase 6.

Histone deacetylase 6 inhibitors and use thereof

Disclosed is hydroxamic acid compounds of Formula (I) set forth herein. Also disclosed are a pharmaceutical composition containing such a compound and a method of using the compound for treating a condition associated with histone deacetylase 6.

Quinazoline derivatives substituted by aniline, preparation method and use thereof
09730934 · 2017-08-15 · ·

The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof. ##STR00001##