C07D209/42

MODULATORS OF MAS-RELATED G-PROTEIN RECEPTOR X2 AND RELATED PRODUCTS AND METHODS

Methods are provided for modulating MRGPRX2 generally, or for treating a MRGPRX2 dependent condition more specifically, by contacting the MRGPRX2 or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I):

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or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein D, W, Z, R.sup.1, R.sup.2 and R.sup.3 are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

MODULATORS OF MAS-RELATED G-PROTEIN RECEPTOR X2 AND RELATED PRODUCTS AND METHODS

Methods are provided for modulating MRGPRX2 generally, or for treating a MRGPRX2 dependent condition more specifically, by contacting the MRGPRX2 or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I):

##STR00001##

or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein A, B, C, D, E, G, W, Y, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

G9a INHIBITOR

A compound represented by the general formula (I) given below or a pharmacologically acceptable salt thereof has been found to have a strong G9a inhibitory effect. The compound (I) or the pharmacologically acceptable salt thereof inhibits G9a and thereby has high usefulness for the treatment, prevention or suppression of various pathological conditions (proliferative disease such as cancer, β-globin abnormality, fibrosis, pain, neurodegenerative disease, Prader-Willi syndrome, malaria, viral infection, myopathy, autism, etc.).

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G9a INHIBITOR

A compound represented by the general formula (I) given below or a pharmacologically acceptable salt thereof has been found to have a strong G9a inhibitory effect. The compound (I) or the pharmacologically acceptable salt thereof inhibits G9a and thereby has high usefulness for the treatment, prevention or suppression of various pathological conditions (proliferative disease such as cancer, β-globin abnormality, fibrosis, pain, neurodegenerative disease, Prader-Willi syndrome, malaria, viral infection, myopathy, autism, etc.).

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Bicyclic carboxamides and methods of use thereof

Compounds, compositions and methods are provided for modulating the activity of EP.sub.2 and EP.sub.4 receptors, and for the treatment, prevention and amelioration of one or more symptoms of diseases or disorders related to the activity of EP.sub.2 and EP.sub.4 receptors. In certain embodiments, the compounds are antagonists of both the EP.sub.2 and EP.sub.4 receptors.

Bicyclic carboxamides and methods of use thereof

Compounds, compositions and methods are provided for modulating the activity of EP.sub.2 and EP.sub.4 receptors, and for the treatment, prevention and amelioration of one or more symptoms of diseases or disorders related to the activity of EP.sub.2 and EP.sub.4 receptors. In certain embodiments, the compounds are antagonists of both the EP.sub.2 and EP.sub.4 receptors.

Selective D.SUB.3 .dopamine receptor agonists and methods of their use

The disclosure of a compound of Formula (I) or a pharmaceutically acceptable salt thereof (I) The variables W, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined in the disclosure. The disclosure provides a compound or salt of Formula (I) together with a pharmaceutically acceptable carrier. The disclosure also provides methods of treating a patient for Parkinson's disease and related syndromes, dyskinesia, especially dyskinesias secondary to treating Parkinson's disease with L-DOPA, neurodegenerative disorders such as Alzheimer's disease and dementia, Huntington's disease, restless legs syndrome, bipolar disorder and depression, schizophrenia, cognitive dysfunction, or substance use disorders, the methods comprising administering a compound of Formula I or salt thereof to the patient. The disclosure provides combination methods of treatment in which the compound of Formula (I) is administered to the patient together with one or more additional active agents.

Selective D.SUB.3 .dopamine receptor agonists and methods of their use

The disclosure of a compound of Formula (I) or a pharmaceutically acceptable salt thereof (I) The variables W, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined in the disclosure. The disclosure provides a compound or salt of Formula (I) together with a pharmaceutically acceptable carrier. The disclosure also provides methods of treating a patient for Parkinson's disease and related syndromes, dyskinesia, especially dyskinesias secondary to treating Parkinson's disease with L-DOPA, neurodegenerative disorders such as Alzheimer's disease and dementia, Huntington's disease, restless legs syndrome, bipolar disorder and depression, schizophrenia, cognitive dysfunction, or substance use disorders, the methods comprising administering a compound of Formula I or salt thereof to the patient. The disclosure provides combination methods of treatment in which the compound of Formula (I) is administered to the patient together with one or more additional active agents.

NOVEL COMPOUNDS AS INHIBITORS OF PCSK9
20230122967 · 2023-04-20 ·

Disclosed are a compound of formula (I), wherein the variables are defined in the specification, a pharmaceutical composition containing the same, and a method and a use of the compound or composition in the treatment of a PCSK9-mediated disease such as cardiovascular disease.

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NOVEL COMPOUNDS AS INHIBITORS OF PCSK9
20230122967 · 2023-04-20 ·

Disclosed are a compound of formula (I), wherein the variables are defined in the specification, a pharmaceutical composition containing the same, and a method and a use of the compound or composition in the treatment of a PCSK9-mediated disease such as cardiovascular disease.

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