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54 results about "Aldosterone synthase" patented technology

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Aldosterone synthase is a steroid hydroxylase cytochrome P450 enzyme involved in the biosynthesis of the mineralocorticoid aldosterone. It is a protein which is only expressed in the zona glomerulosa of the adrenal cortex and is primarily regulated by the renin–angiotensin system. It is the sole enzyme capable of synthesizing aldosterone in humans and plays an important role in electrolyte balance and blood pressure.

Inhibitors of the Human Aldosterone Sythase CYP11B2

ActiveUS20110112067A1Promote degradationImprove survival rateBiocideOrganic chemistryDiseaseAldosterone Synthase Deficiency

The invention provides compounds of the general formula (I)

which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11β-hydroxylase (CYP11B1) with these compounds.

Inhibitors of the Human Aldosterone Sythase CYP11B2

Inhibitors of the Human Aldosterone Sythase CYP11B2

Inhibitors of the Human Aldosterone Sythase CYP11B2

Owner:ELEXOPHARM

Aryl pyridine as aldosterone synthase inhibitors

InactiveUS20100292225A1Improve adverse effectsSuppression problemBiocideSenses disorderArylAldosterone Synthase Deficiency

The present invention provides a compound of formula I;

a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Aryl pyridine as aldosterone synthase inhibitors

Aryl pyridine as aldosterone synthase inhibitors

Aryl pyridine as aldosterone synthase inhibitors

Owner:NOVARTIS AG

6-Pyridin-3-YL-3,4-Dihydro-1H-Quinolin-2-One Derivatives and Related Compounds as Inhibitors of the Human Aldosterone Synthase CYP11B2

ActiveUS20110118241A1Promote degradationImprove survival rateBiocideOrganic chemistryAldosterone Synthase DeficiencyIsrapafant

The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 β-hydroxylase (CYP11 B1).

6-Pyridin-3-YL-3,4-Dihydro-1H-Quinolin-2-One Derivatives and Related Compounds as Inhibitors of the Human Aldosterone Synthase CYP11B2

6-Pyridin-3-YL-3,4-Dihydro-1H-Quinolin-2-One Derivatives and Related Compounds as Inhibitors of the Human Aldosterone Synthase CYP11B2

6-Pyridin-3-YL-3,4-Dihydro-1H-Quinolin-2-One Derivatives and Related Compounds as Inhibitors of the Human Aldosterone Synthase CYP11B2

Owner:ELEXOPHARM

Dihydroquinoline-2-one derivatives

ActiveUS20130072679A1Good blood pressureImprove cardiac functionGroup 4/14 element organic compoundsUrinary disorderAldosterone Synthase DeficiencyPrimary aldosteronism

The invention provides novel compounds having the general formula (I)

wherein R¹, R², R³, R⁴, R⁵, R⁶, R⁷, A¹, A²and A³are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.

Dihydroquinoline-2-one derivatives

Dihydroquinoline-2-one derivatives

Dihydroquinoline-2-one derivatives

Owner:F HOFFMANN LA ROCHE INC

Pyrazolopyridyl compounds as aldosterone synthase inhibitors

ActiveUS20140288094A1BiocideOrganic chemistryAldosterone Synthase DeficiencyStructural formula

This invention relates to pyrazolopyridyl compounds of the structural formula:

or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

Pyrazolopyridyl compounds as aldosterone synthase inhibitors

Pyrazolopyridyl compounds as aldosterone synthase inhibitors

Pyrazolopyridyl compounds as aldosterone synthase inhibitors

Owner:MERCK SHARP & DOHME LLC

New bicyclic dihydroisoquinoline-1-one derivatives

ActiveUS20130143863A1Good blood pressureImprove cardiac functionBiocideOrganic chemistryAldosterone Synthase DeficiencyNephrosis

The invention provides novel compounds having the general formula (I)

wherein R¹, R², R³, R⁴, R⁵, R⁶, A¹, A², A³, A⁴, A⁵and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful, for example, as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.

New bicyclic dihydroisoquinoline-1-one derivatives

New bicyclic dihydroisoquinoline-1-one derivatives

New bicyclic dihydroisoquinoline-1-one derivatives

Owner:F HOFFMANN LA ROCHE & CO AG

5-pyridin-3-yl-1, 3-dihydro-indol-2-on derivatives and their use as modulators of aldosterone synthase and/or cyp11b1

InactiveUS20120071512A1Improve adverse effectsSuppression problemBiocideSenses disorderAldosterone Synthase DeficiencyActive agent

The present invention provides a compound of formula I;

a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

5-pyridin-3-yl-1, 3-dihydro-indol-2-on derivatives and their use as modulators of aldosterone synthase and/or cyp11b1

5-pyridin-3-yl-1, 3-dihydro-indol-2-on derivatives and their use as modulators of aldosterone synthase and/or cyp11b1

5-pyridin-3-yl-1, 3-dihydro-indol-2-on derivatives and their use as modulators of aldosterone synthase and/or cyp11b1

Owner:NOVARTIS AG

Aldosterone synthase inhibitors

ActiveUS20140323468A1Useful in treatmentBiocideOrganic chemistryAldosterone Synthase DeficiencyDisease

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

and pharmaceutically acceptable salts thereof, wherein R¹, R². R³, R⁴, R⁵, R⁶, R⁷, W, Y, m and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Aldosterone synthase inhibitors

Aldosterone synthase inhibitors

Aldosterone synthase inhibitors

Owner:BOEHRINGER INGELHEIM INT GMBH

Spirodiamine derivatives as aldosterone synthase inhibitors

ActiveUS10035804B2Organic active ingredientsOrganic chemistryAldosterone Synthase DeficiencyBiochemistry

The invention provides novel compounds having the general formula (I)wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R5, A1, A2, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.

Spirodiamine derivatives as aldosterone synthase inhibitors

Spirodiamine derivatives as aldosterone synthase inhibitors

Spirodiamine derivatives as aldosterone synthase inhibitors

Owner:F HOFFMANN LA ROCHE & CO AG

Imidazole derivatives as aldosterone synthase inhibitors

InactiveUS8575160B2BiocideSenses disorderAldosterone Synthase DeficiencyMedicine

The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, R5, R7 and p are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Imidazole derivatives as aldosterone synthase inhibitors

Imidazole derivatives as aldosterone synthase inhibitors

Imidazole derivatives as aldosterone synthase inhibitors

Owner:NOVARTIS AG

Inhibitors of the human aldosterone synthase CYP11B2

ActiveUS8541404B2Improve survival rateReduce morbidityBiocideOrganic chemistryDiseaseAldosterone Synthase Deficiency

The invention provides compounds of the general formula (I)which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and / or disorders or diseases that are mediated by 11β-hydroxylase (CYP11B1) with these compounds.

Inhibitors of the human aldosterone synthase CYP11B2

Inhibitors of the human aldosterone synthase CYP11B2

Inhibitors of the human aldosterone synthase CYP11B2

Owner:ELEXOPHARM

Aldosterone synthase inhibitors

ActiveUS9181272B2Organic chemistryUrinary disorderAldosterone Synthase DeficiencyDisease

The present invention relates to compounds of formula (I):and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, W, Y, m and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Aldosterone synthase inhibitors

Aldosterone synthase inhibitors

Aldosterone synthase inhibitors

Owner:BOEHRINGER INGELHEIM INT GMBH

Benzoxazolone derivatives as aldosterone synthase inhibitors

InactiveUS20120071514A1Improve adverse effectsSuppression problemBiocideSenses disorderAldosterone Synthase DeficiencyBenzoxazole

The present invention provides a compound of formula I;

a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Benzoxazolone derivatives as aldosterone synthase inhibitors

Benzoxazolone derivatives as aldosterone synthase inhibitors

Benzoxazolone derivatives as aldosterone synthase inhibitors

Owner:NOVARTIS AG

Dihydroquinoline-2-one derivatives

ActiveUS9260408B2Group 4/14 element organic compoundsUrinary disorderAldosterone Synthase DeficiencyMedicine

The invention provides novel compounds having the general formula (I)wherein R1, R2, R3, R4, R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.

Dihydroquinoline-2-one derivatives

Dihydroquinoline-2-one derivatives

Dihydroquinoline-2-one derivatives

Owner:F HOFFMANN LA ROCHE & CO AG

Aldosterone synthase inhibitors

ActiveUS9334285B2Lower Level RequirementsUseful in treatmentOrganic active ingredientsOrganic chemistryDiseaseAldosterone Synthase Deficiency

The present invention relates to compounds of formula I:and pharmaceutically acceptable salts thereof, wherein Cy, R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Owner:BOEHRINGER INGELHEIM INT GMBH

Imidazole derivatives as aldosterone synthase inhibitors

InactiveUS20130065893A1Increased collagen formationBiocideSenses disorderAldosterone synthaseActive agent

The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R¹, R², R³, R⁴, R⁵, R⁷and p are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Imidazole derivatives as aldosterone synthase inhibitors

Imidazole derivatives as aldosterone synthase inhibitors

Imidazole derivatives as aldosterone synthase inhibitors

Owner:NOVARTIS AG

6-pyridin-3-yl-3,4-dihydro-1h-quinolin-2-one derivatives and related compounds as inhibitors of the human aldosterone synthase CYP11B2

ActiveUS8685960B2Improve survival rateReduce morbidityBiocideOrganic chemistryAldosterone Synthase DeficiencyPyridine

The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and / or disorders or diseases that are mediated by 11 β-hydroxylase (CYP11 B1).

6-pyridin-3-yl-3,4-dihydro-1h-quinolin-2-one derivatives and related compounds as inhibitors of the human aldosterone synthase CYP11B2

6-pyridin-3-yl-3,4-dihydro-1h-quinolin-2-one derivatives and related compounds as inhibitors of the human aldosterone synthase CYP11B2

6-pyridin-3-yl-3,4-dihydro-1h-quinolin-2-one derivatives and related compounds as inhibitors of the human aldosterone synthase CYP11B2

Owner:ELEXOPHARM

Biomarkers of Mineralocorticoid Receptor Activation

ActiveUS20160362744A1Precision therapyMetabolism disorderMicrobiological testing/measurementGelatinasesAldosterone Synthase Deficiency

The present invention relates to the use of Neutrophil Gelatinase-Associated Lipocalin (NGAL) and / or SERPINA3 as biomarkers of the Mineralocorticoid Receptor (MR) activation in a patient. More particularly, the present invention relates to a method for predicting the responsiveness of a patient to a treatment with a MR antagonist or an aldosterone synthase inhibitor, said method comprising determining in a biological sample obtained from said patient the expression level of the NGAL gene and / or of the SERPINA3 gene.

Biomarkers of Mineralocorticoid Receptor Activation

Biomarkers of Mineralocorticoid Receptor Activation

Biomarkers of Mineralocorticoid Receptor Activation

Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM) +2

Aldosterone synthase inhibitors

ActiveUS20130317057A1BiocideOrganic chemistryAldosterone Synthase DeficiencyElevated aldosterone levels

The invention involves compounds of structural Formula (I) and the pharmaceutically acceptable salts thereof. The compounds of the invention are effective at selectively inhibiting CYP11B2, and are therefore useful for the treatment or prophylaxis of disorders that are associated with elevated aldosterone levels, including, but not limited to, hypertension and heart failure.

Aldosterone synthase inhibitors

Aldosterone synthase inhibitors

Aldosterone synthase inhibitors

Owner:MERCK SHARP & DOHME LLC

Pet radiopharmaceuticals for differential diagnosis between bilateral and unilateral conditions of primary hyperaldosteronism

InactiveUS20130089502A1Organic chemistryRadioactive preparation carriersRadioactive tracerMammal

A functional PET imaging method is disclosed for differentiation between bilateral hyperplasia and unilateral adenoma comprising (1) introducing a radioactively labelled CYP11 B2 (aldosterone synthase) inhibitor which binds selectively to CYP11 B2 (aldosterone synthase) relative to CYP11 B1 (11β-hydroxylase) into a mammal with adrenal glands and (2) conducting positron emission tomography (PET) in the region of the adrenal glands to obtain a functional PET image of the adrenal glands. Also disclosed are radioactive tracer compounds suitable for use in this method, precursors for making the same, and a process for making the radioactive tracer compounds capable of being conducted as a rapid one-pot reaction.

Pet radiopharmaceuticals for differential diagnosis between bilateral and unilateral conditions of primary hyperaldosteronism

Pet radiopharmaceuticals for differential diagnosis between bilateral and unilateral conditions of primary hyperaldosteronism

Pet radiopharmaceuticals for differential diagnosis between bilateral and unilateral conditions of primary hyperaldosteronism

Owner:UNIV DES SAARLANDES +1

New forms and salts of a dihydropyrrolo[1,2c]imidazolyl aldosterone synthase or aromatase inhibitor

ActiveUS20140364470A1Organic active ingredientsBiocideDiseasePhosphate

The invention relates to a phosphate salt or a nitrate salt of 4-(R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl-3-fluoro-benzonitrile, especially in crystalline form, and specific forms of these salts, as well as related invention embodiments. The salts and salt forms allow for the prophylactic and / or therapeutic treatment of aldosterone synthase and / or aromatase mediated diseases or disorders.

New forms and salts of a dihydropyrrolo[1,2c]imidazolyl aldosterone synthase or aromatase inhibitor

New forms and salts of a dihydropyrrolo[1,2c]imidazolyl aldosterone synthase or aromatase inhibitor

New forms and salts of a dihydropyrrolo[1,2c]imidazolyl aldosterone synthase or aromatase inhibitor

Owner:RECORDATI AG

Biomarkers of Mineralocorticoid Receptor Activation

InactiveUS20110257140A1Precision therapyOrganic active ingredientsMetabolism disorderGelatinasesAldosterone Synthase Deficiency

The present invention relates to the use of Neutrophil Gelatinase-Associated Lipocalin (NGAL) and/or SERPINA3 as biomarkers of the Mineralocorticoid Receptor (MR) activation in a patient. More particularly, the present invention relates to a method for predicting the responsiveness of a patient to a treatment with a MR antagonist or an aldosterone synthase inhibitor, said method comprising determining in a biological sample obtained from said patient the expression level of the NGAL gene and/or of the SERPINA3 gene.

Biomarkers of Mineralocorticoid Receptor Activation

Biomarkers of Mineralocorticoid Receptor Activation

Biomarkers of Mineralocorticoid Receptor Activation

Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM) +2

Aldosterone synthase inhibitor

ActiveUS10822332B2Decreased and very low aromatase activityDegreeOrganic active ingredientsMetabolism disorderAldosterone Synthase DeficiencyPediatric patient

The present invention relates to a compound selected from (R)-(+)-5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine and a pharmaceutically acceptable salt thereof, and in particular to the phosphate salt of (R)-(+)-5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine, both having preferably an enantiomeric excess of the (R) form higher than or equal to 97%. Furthermore, the present invention relates to pharmaceutical compositions comprising the same, their use as a medicament and in methods of treatment of diseases and disorders in humans including women of child bearing potential and pediatric patients in which aldosterone over-exposure contributes to the deleterious effects of said diseases or disorders, as well as processes for preparing said inventive compounds.

Aldosterone synthase inhibitor

Aldosterone synthase inhibitor

Aldosterone synthase inhibitor

Owner:DAMIAN PHARMA AG

Imidazole derivatives as aldosterone synthase inhibitors

InactiveCN102666535AOrganic active ingredientsSenses disorderAldosterone Synthase DeficiencyActive agent

The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, R5, R7 and p are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Imidazole derivatives as aldosterone synthase inhibitors

Imidazole derivatives as aldosterone synthase inhibitors

Imidazole derivatives as aldosterone synthase inhibitors

Owner:NOVARTIS AG

Benzoxazolone derivatives as aldosterone synthase inhibitors

InactiveUS8455522B2BiocideSenses disorderAldosterone Synthase DeficiencyBenzoxazole

The present invention provides a compound of formula I;a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Benzoxazolone derivatives as aldosterone synthase inhibitors

Benzoxazolone derivatives as aldosterone synthase inhibitors

Benzoxazolone derivatives as aldosterone synthase inhibitors

Owner:NOVARTIS AG

Aryl-pyridine derivatives as aldosterone synthase inhibitors

InactiveUS8519134B2BiocideNervous disorderArylAldosterone Synthase Deficiency

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Aryl-pyridine derivatives as aldosterone synthase inhibitors

Aryl-pyridine derivatives as aldosterone synthase inhibitors

Aryl-pyridine derivatives as aldosterone synthase inhibitors

Owner:NOVARTIS AG

Aryl-pyridine derivatives as aldosterone synthase inhibitors

InactiveUS20120316195A1Increased collagen formationEffective treatmentBiocideNervous disorderAldosterone Synthase DeficiencyAryl

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R¹, R², R³, R⁴, R⁵and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Aryl-pyridine derivatives as aldosterone synthase inhibitors

Aryl-pyridine derivatives as aldosterone synthase inhibitors

Aryl-pyridine derivatives as aldosterone synthase inhibitors

Owner:NOVARTIS AG

New bicyclic dihydroquinoline-2-one derivatives

ActiveUS20130079365A1Good blood pressureImprove cardiac functionBiocideOrganic chemistryAldosterone Synthase DeficiencyPrimary aldosteronism

The invention provides novel compounds having the general formula (I)

wherein R¹, R², R³, R⁴, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, R¹², A¹, A²A³and n are as described herein, compositions including the compounds and methods of using the compounds.

The compounds of the present invention are useful as inhibitors of aldosterone synthase. The compounds may be used, for example, in the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.

New bicyclic dihydroquinoline-2-one derivatives

New bicyclic dihydroquinoline-2-one derivatives

New bicyclic dihydroquinoline-2-one derivatives

Owner:F HOFFMANN LA ROCHE INC

Aryl pyridine as aldosterone synthase inhibitors

InactiveUS20130035354A1Increased collagen formationBiocideSenses disorderAldosterone Synthase DeficiencyAryl

The present invention provides a compound of formula I;a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Aryl pyridine as aldosterone synthase inhibitors

Aryl pyridine as aldosterone synthase inhibitors

Aryl pyridine as aldosterone synthase inhibitors

Owner:NOVARTIS AG

Non-invasive diagnostic imaging agent for heart disease

InactiveUS20190255199A1Pharmaceutical delivery mechanismRadioactive preparation carriersAldosterone Synthase DeficiencyImaging agent

The present invention addresses the problem of providing a technique for detecting a lesion of a heart disease in a non-invasive manner. The present invention provides a non-invasive diagnostic imaging agent for a heart disease, which contains a radioactively labeled compound capable of binding to an aldosterone synthase or a salt thereof as an active ingredient.

Non-invasive diagnostic imaging agent for heart disease

Non-invasive diagnostic imaging agent for heart disease

Non-invasive diagnostic imaging agent for heart disease

Owner:NIHON MEDI PHYSICS CO LTD

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