A61K31/501

SUBSTITUTED HYDANTOINAMIDES AS ADAMTS7 ANTAGONISTS

The application relates to substituted hydantoinamides of formula (I) as ADAMTS7 antagonists, to processes for their preparation, their use alone or in combination for the treatment or prophylaxis of diseases, in particular of cardiovascular diseases, including atherosclerosis, coronary artery disease (CAD), peripheral vascular disease (PAD), arterial occlusive disease or restenosis after angioplasty. R.sup.1 is hydrogen, alkyl, cycloalkyl, heterocycloalkyl, heteroaryl or phenyl; R.sup.2 is hydrogen, cyano, halogen, alkylsulfonyl, alkyl, cycloalkyl or alkoxy; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen, halogen, alkyl or alkoxy; most groups being optionally substituted; with the proviso that at least one of R.sup.2, R.sup.3, R.sup.4 is H; X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5 and X.sup.6 are independently N or C; with the proviso that in each ring maximal one X is N.

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METHODS FOR MODULATING SPLICING
20230025130 · 2023-01-26 ·

Described herein are methods of use of small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of treating diseases and conditions associated with gene expression or activity of proteins encoded by genes.

METHODS FOR MODULATING SPLICING
20230025130 · 2023-01-26 ·

Described herein are methods of use of small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of treating diseases and conditions associated with gene expression or activity of proteins encoded by genes.

INHIBITORS OF ENL/AF9 YEATS

Methods and compositions for treating leukemia are disclosed. Acylated 6-aminoindoles, acylated 6-aminopyrrolopyridines and acylated 3-aminopyrrolo[3,2-c]pyridazines of the following formula

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inhibit ENL/AF9 YEATS and are therefore useful for treating leukemia.

INHIBITORS OF ENL/AF9 YEATS

Methods and compositions for treating leukemia are disclosed. Acylated 6-aminoindoles, acylated 6-aminopyrrolopyridines and acylated 3-aminopyrrolo[3,2-c]pyridazines of the following formula

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inhibit ENL/AF9 YEATS and are therefore useful for treating leukemia.

COMPOSITIONS AND METHODS FOR THE TREATMENT OF LIVER DISORDERS

The present disclosure is directed to FXR agonists, pharmaceutical compositions thereof, and methods of using the same for preventing, treating, or ameliorating fatty liver diseases such as steatosis, non-alcoholic fatty liver disease, and non-alcoholic steatohepatitis, either alone or in combination with thyroid receptor agonists.

COMPOSITIONS AND METHODS FOR THE TREATMENT OF LIVER DISORDERS

The present disclosure is directed to FXR agonists, pharmaceutical compositions thereof, and methods of using the same for preventing, treating, or ameliorating fatty liver diseases such as steatosis, non-alcoholic fatty liver disease, and non-alcoholic steatohepatitis, either alone or in combination with thyroid receptor agonists.

BENZAMIDE COMPOUND AND USE THEREOF

Provided are a novel compound that effectively antagonizes P2X3 receptor, a preparation method thereof, and use thereof in the preparation of drugs. The compound is a compound represented by Formula I, or a tautomer, a stereoisomer, a hydrate, a solvate, a pharmaceutically acceptable salt, or a prodrug thereof.

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Co-therapies including a metastasis inhibitor

Provided are methods of increasing a response to a chemotherapeutic agent or an immunotherapeutic agent in a patient in need thereof, and methods of treating cancer in a patient in need thereof, comprising administering to the patient a chemotherapeutic agent or an immunotherapeutic agent and a metastasis inhibiting compound, as described in this disclosure.

Co-therapies including a metastasis inhibitor

Provided are methods of increasing a response to a chemotherapeutic agent or an immunotherapeutic agent in a patient in need thereof, and methods of treating cancer in a patient in need thereof, comprising administering to the patient a chemotherapeutic agent or an immunotherapeutic agent and a metastasis inhibiting compound, as described in this disclosure.