32 results about "Aldosterone Synthase Deficiency" patented technology

Provided are compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders, or symptoms thereof mediated by such metalloenzymes. In some embodiments, a provided compound is a compound of Formula I,or a pharmaceutically acceptable salt thereof. In some embodiments, a provided method is a method of alleviating or abating a disorder or disease associated with aldosterone synthase (CYP11B2) or ameliorating a symptom thereof.

Disclosed are solid forms of an inhibitor of aldosterone synthase (ASi) having the formula The invention also relates to methods of making these solid forms, pharmaceutical compositions comprising these solid forms, and their use for medical conditions responsive to treatment with an inhibitor of aldosterone synthase.

The application discloses a pyrano pyridine compound, a preparation method, a pharmaceutical composition and application thereof. The application provides a compound as shown in formula (I), a pharmaceutically acceptable salt or a stereoisomer thereof, the compounds have a strong inhibitory effect on aldosterone synthase, have little influence on cortisol synthase, have high selectivity and high safety, and can be used for preventing and / or treating various diseases related to aldosterone.

Disclosed are methods of using an aldosterone synthase inhibitor of formula (1) for treating, reducing the risk of, or delaying the progression of heart failure related disorders. The invention further relates to methods of using Compound 1 in combination with sodium-glucose cotransporter-2 (SGLT2) inhibitors.

The present invention provides a salt of a triazine compound which has an inhibitory action against aldosterone synthase and is useful as a drug, and especially as a drug for preventing or treating primary aldosteronism and the like, a crystal thereof, and a method for producing the same. Specifically, the present invention provides a pharmaceutically acceptable salt of 3-[4-[[trans-4-(acetamino)cyclohexyl]carbamoylmethyl]piperazin-1-yl]-5-(p-tolyl)-1,2,4-triazine, wherein the salt is hydrobromide, sulfate, succinate, or tosylate, and the like.

Provided is a method for producing a triazine compound which has an inhibitory action against aldosterone synthetase and is useful as a drug, particularly a prophylactic or therapeutic drug for primary aldosterone hyperplasia and the like.

The present invention provides a salt of a triazine compound which has an inhibitory action against aldosterone synthase and is useful as a drug, and especially as a drug for preventing or treating primary aldosteronism and the like, a crystal thereof, and a method for producing the same. Specifically, the present invention provides a pharmaceutically acceptable salt of 3-[4-[[trans-4-(acetamino)cyclohexyl]carbamoylmethyl]piperazin-1-yl]-5-(p-tolyl)-1,2,4-triazine, wherein the salt is hydrobromide, sulfate, succinate, or tosylate, and the like.

The present application relates to a salt of a triazine compound, a crystal form thereof, and a method for producing the same. Provided are: a salt and a crystal of a triazine compound, which have an inhibitory effect on aldosterone synthetase and are useful as a drug, particularly a prophylactic or therapeutic drug for primary aldosterone hyperplasia and the like; and a method for producing the salt and the crystal of the triazine compound. Specifically, the present invention provides a pharmaceutically acceptable salt of 3-[4-[[trans-4-(acetamido) cyclohexyl] carbamoylmethyl] piperazin-1-yl]-5-(p-tolyl)-1, 2, 4-triazine (wherein the salt is a hydrobromide salt, a sulfate salt, a succinate salt, a p-toluenesulfonate salt, or the like), and a pharmaceutically acceptable salt of 3-[4-[[trans-4-(acetamido) cyclohexyl] carbamoylmethyl] piperazin-1-yl]-5-(p-tolyl)-1, 2, 4-triazine.

The present invention provides a salt of a triazine compound which has an inhibitory action against aldosterone synthase and is useful as a drug, and especially as a drug for preventing or treating primary aldosteronism and the like, a crystal thereof, and a method for producing the same. Specifically, the present invention provides a pharmaceutically acceptable salt of 3-[4-[[trans-4-(acetamino)cyclohexyl]carbamoylmethyl]piperazin-1-yl]-5-(p-tolyl)-1,2,4-triazine, wherein the salt is hydrobromide, sulfate, succinate, or tosilate, and the like.

The present application provides a salt of a triazine compound having an inhibitory action against aldosterone synthase, which is useful as a medicine, particularly a prophylactic or therapeutic agent for primary aldosteronism and the like, a crystal thereof, and a production method thereof. Specifically, the present application provides a pharmaceutically acceptable salt of 3-[4-[[trans-4-(acetylamino)cyclohexyl]carbamoylmethyl]piperazin-1-yl]-5-(p-tolyl)-1,2,4-triazine, wherein the salt is a hydrobromide, a sulfate, a succinate, or a p-toluenesulfonate, or the like.

This invention provides a method of treating hypertension in a hypertensive subject, the method administering to the subject, an amount of a diuretic and an amount of a CYP 11β2 beta hydroxylase inhibitor once or twice per day, wherein the amounts taken together are sufficient to treat hypertension in the hypertensive subject when taken in combination with other antihypertensive agents. In particular, the method is sufficient to elicit a safe and robust reduction in hypertension (>10 mmHg reduction in systolic blood pressure) in the hypertensive subject.

The invention discloses a pyranopyridine compound as well as a preparation method, a pharmaceutical composition and application thereof. The invention provides a compound as shown in a formula (I), a pharmaceutically acceptable salt or a stereoisomer thereof, and the compound has a relatively strong inhibition effect on aldosterone synthetase, almost has no influence on cortisol synthetase, has high selectivity and relatively high safety, and can be used for preventing and / or treating various diseases related to aldosterone.

The present invention belongs to the technical field of chemical pharmaceuticals. Provided in the present invention are an aldosterone synthase inhibitor, and a preparation method therefor and the use thereof.  

Novel crystalline forms of baxdrostat, methods for producing the same, pharmaceutical compositions containing the crystalline form, and the production of aldosterone synthase inhibitors, as well as the use of the crystalline form in the production of pharmaceuticals for the treatment of hypertension, primary aldosteronism, and chronic kidney disease.

The disclosure provides methods of reducing the risk of cardiovascular events and heart failure events in patients at risk of heart failure, the methods comprising administering to the patient a combination comprising an aldosterone synthase inhibitor (ASi) and a sodium-glucose co-transporter 2 inhibitor (SGLT2i).

The invention discloses application of cinnamaldehyde to preparation of an aldosterone synthase inhibitor, and relates to the field of natural medicine.Firstly, an effective target of cinnamaldehyde playing a role in inhibiting aldosterone synthesis is screened through a network pharmacology analysis tool, and the result indicates that cinnamaldehyde may play a role by acting on aldosterone synthase (CYP11B2); subsequently, the influence of cinnamaldehyde on aldosterone and CYP11B2 is detected through an in-vitro experiment, and cinnamaldehyde is proved to have an inhibiting effect on CYP11B2; finally, human adrenal cortex adenocarcinoma cells (NCI-H295R) and cinnamaldehyde are incubated together, it is found that cinnamaldehyde can inhibit the activity of CYP11B2 of the NCI-H295R cells and reduce the aldosterone level, and it is proved that cinnamaldehyde can inhibit biosynthesis of aldosterone through CYP11B2.

The invention discloses a pyranopyridine compound, a preparation process, a pharmaceutical composition and use thereof. The present invention provides a compound of Formula (I), a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, which has a strong inhibitory effect on aldosterone synthase, but has little effect on cortisol synthase, is highly selective and has a higher safety, and can be used for preventing and / or treating various diseases associated with aldosterone.

The present invention pertains to the technical field of chemical pharmaceutical products. The present invention provides an aldosterone synthase inhibitor, a method for preparing and using the same.

The invention discloses a method for synthesizing a 2-(hetero) aryl-3-cyano indole skeleton through a one-step method based on photochemical reaction and application, and relates to the technical field of organic synthesis.The method is technically characterized by comprising the steps that an indole derivative, a (hetero) aryl derivative, alkali and a solvent are added into a reaction container, under the nitrogen atmosphere, visible light or ultraviolet light is adopted for irradiation, and the 2-(hetero) aryl-3-cyano indole skeleton is obtained; reacting at room temperature for 12 hours; and after the reaction is completed, concentrating the reaction liquid and purifying to obtain the 2-(hetero) aryl-3-cyano indole derivative. The 2-aryl-3-cyano indole skeleton synthesized by the method has significant drug research and development potential, especially in the development of HCV inhibitors and aldosterone synthetase inhibitors, the method has the advantages of being green and environment-friendly, efficient and simple, cheap and easily available in raw materials, strong in modification of molecular structures and the like, and the 2-aryl-3-cyano indole skeleton can be synthesized by adjusting reaction conditions or initial raw materials. Therefore, diversified construction of target molecules can be realized, and great flexibility is provided for optimization and research and development of drug molecules.

The present invention relates to a composition for use in the treatment of a disease or disorder, wherein said disease or disorder is preferably a disease or disorder in which aldosterone overexposure contributes to the symptoms of said disease or disorder, said composition comprises a compound which is (R)-(+)-5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine or a pharmaceutically acceptable salt thereof, wherein preferably said compound is (R)-(+)-5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazolium[1,5-a]pyridine dihydrogen phosphate, and wherein said compound has an enantiomeric excess (ee) of the (R) form higher than or equal to 99%, and wherein said composition is administered once daily for at least eight weeks to a patient in need thereof.

This invention relates to a method of treating heart failure with preserved ejection fraction (HFpEF) in a subject afflicted with HFpEF, the method comprising administering to the subject an aldosterone synthase inhibitor once per day in an amount effective to treat HFpEF in the subject. This invention also relates to a method of treating left ventricular diastolic dysfunction (LVDD) in a subject afflicted with LVDD, the method comprising administering to the subject an aldosterone synthase inhibitor once per day in an amount effective to treat LVDD in the subject.

The present invention provides a method of treating hypertension in a hypertensive subject by administering to the subject an amount of a diuretic agent and an amount of a CYP 11 [beta] 2 [beta] hydroxylase inhibitor once or twice per day, where when taken in combination with other antihypertensive agents, the amount of the CYP 11 [beta] 2 [beta] hydroxylase inhibitor is less than the amount of the diuretic agent and the amount of the CYP 11 [beta] 2 [beta] hydroxylase inhibitor. The co-administration amount is sufficient to treat hypertension in the hypertensive subject. In particular, the methods are sufficient to safely and reliably reduce hypertension in the hypertensive subject (systolic pressure reduction > 10 mmHg).

The invention discloses a pyranopyridine compound, a preparation process, a pharmaceutical composition and use thereof. The present invention provides a compound of Formula (I), a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, which has a strong inhibitory effect on aldosterone synthase, but has little effect on cortisol synthase, is highly selective and has a higher safety, and can be used for preventing and / or treating various diseases associated with aldosterone.

The invention discloses a pyranopyridine compound as well as a preparation method, a pharmaceutical composition and application thereof. The invention provides a compound as shown in a formula (I), a pharmaceutically acceptable salt or a stereoisomer thereof, and the compound has a relatively strong inhibition effect on aldosterone synthetase, almost has no influence on cortisol synthetase, has high selectivity and relatively high safety, and can be used for preventing and / or treating various diseases related to aldosterone.

The present invention provides a salt of a triazine compound which has an inhibitory action against aldosterone synthase and is useful as a drug, and especially as a drug for preventing or treating primary aldosteronism and the like, a crystal thereof, and a method for producing the same. Specifically, the present invention provides a pharmaceutically acceptable salt of 3-[4-[[trans-4-(acetamino)cyclohexyl]carbamoylmethyl]piperazin-1-yl]-5-(p-tolyl)-1,2,4-triazine, wherein the salt is hydrobromide, sulfate, succinate, or tosylate, and the like.

The present invention relates to organic chemistry, pharmacology, medicine, in particular to compounds for inhibiting human cytochrome 11B2 (CYP11B2) activity and their use in the treatment and / or prevention of various diseases and conditions mediated or maintained by aldosterone hormone activity. The compound has a structure as shown in a general formula (I), wherein R1, R2, R3, R4 and R5 are defined in the specification. The invention also relates to a pharmaceutical composition containing the compound and a preparation method thereof. # imgabs0 #

Disclosed are solid forms of an inhibitor of aldosterone synthase (ASi) having the formula (1)The invention also relates to methods of making these solid forms, pharmaceutical compositions comprising these solid forms, and their use for medical conditions responsive to treatment with an inhibitor of aldosterone synthase.

Disclosed are solid forms of an inhibitor of aldosterone synthase (ASi) having the formula The invention also relates to methods of making these solid forms, pharmaceutical compositions comprising these solid forms, and their use for medical conditions responsive to treatment with an inhibitor of aldosterone synthase.

A new crystal form of Baxdrostat, and a preparation method therefor, a pharmaceutical composition containing the crystal form, and the use of the crystal form in the preparation of an aldosterone synthase inhibitor drug and a drug for treating hypertension, primary aldosteronism, and chronic kidney disease.