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83 results about "11β-hydroxysteroid dehydrogenase type 1" patented technology
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11β-hydroxysteroid dehydrogenase type 1, or 'cortisone reductase' is an NADPH-dependent enzyme highly expressed in key metabolic tissues including liver, adipose tissue, and the central nervous system. In these tissues, HSD11B1 reduces cortisone to the active hormone cortisol that activates glucocorticoid receptors. It is inhibited by carbenoxolone, a drug typically used in the treatment of peptic ulcers. Moreover, 18alpha-glycyrrhizic acid from the root of Glycyrrhiza glabra was discovered as an inhibitor A study from 2014 found that Epigallocatechin gallate from Green tea can also potently inhibit this reaction, which might partly explain the anti-stress properties of Green tea consumption. The protein encoded by this gene is a microsomal enzyme that catalyzes the conversion of the stress hormone cortisol to the inactive metabolite cortisone. In addition, the encoded protein can catalyze the reverse reaction, the conversion of cortisone to cortisol. Too much cortisol can lead to central obesity, and a particular variation in this gene has been associated with obesity and insulin resistance in children.
Combination therapy using an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist to minimize the side effects associated with glucocorticoid receptor agonist therapy
InactiveUS20060094699A1Reduce adverse side effectsUndesirable side-effectBiocideAnimal repellants11beta hydroxysteroid dehydrogenaseSide effect
Combination therapy comprising the administration of an 11β-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist for treating some forms of cancer, diseases and disorders having inflammation as a component, and to minimize the side effects associated with glucorticoid receptor agonist therapy.
Owner:HIGH POINT PHARMA
Pharmaceutical use of substituted amides
The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and / or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Owner:HIGH POINT PHARMA
Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme
The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.
Owner:ABBVIE INC
11beta-hydroxysteroid dehydrogenase type 1 active compounds
A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.
Owner:HIGH POINT PHARMA
Combination therapy using an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent for the treatment of metabolic syndrome and related diseases and disorders
InactiveUS7501405B2Reduce development riskBiocideMetabolism disorderHypertension medicationsDyslipidemia
Combination therapy comprising the administration of an 11β-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent useful for treating, preventing and reducing the risk of developing insulin resistance, dyslipidemia, obesity, hypertension and other related diseases and disorders.
Owner:VTV THERAPEUTICS LLC
Cyclic Inhibitors Of 11Beta-Hydroxysteroid Dehydrogenase 1
This invention relates to novel compounds of the Formula (I), (II), 1u1-20, Iv1-20, Iv1-20, Iw1-20, Ix1-7, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 1β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
Owner:VITAE PHARMA INC
Cyclic Inhibitors Of 11Beta-Hydroxysteroid Dehydrogenase 1
This invention relates to novel compounds of the Formula Ik, Im1, Im2, Im5, In1, In2, In5, lo1, lo2, lo5, Ip1, Ip3, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
Owner:BOEHRINGER INGELHEIM INT GMBH
Amide Derivatives and Pharmaceutical Use Thereof
The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Owner:HIGH POINT PHARMA
Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
Disclosed is a compound represented by Formula (Im1)or a pharmaceutically acceptable salt, enantiomer or diastereomer thereof. Also disclosed are pharmaceutical compositions comprising the compound of Formula (Im1) or a pharmaceutically acceptable salt, enantiomer or diastereomer thereof and methods of inhibiting 11β-HSD1 activity comprising the step of administering to a mammal in need of such treatment an effective amount of a compound of Formulas (Im1), or a pharmaceutically acceptable salt, enantiomer or diastereomer thereof.
Owner:BOEHRINGER INGELHEIM INT GMBH
Urea derivatives of tropane, their preparation and their therapeutic application
The present invention is related to a compound of formula (I)
wherein R1a, R1b, R1c, R1d, R2a, R2b, R3, R4, p, r and are as defined herein, its preparation, pharmaceutical composition and use as a modulator of the activity of the 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1).
Owner:SANOFI SA
Cyclic Inhibitors Of 11Beta-Hydroxysteroid Dehydrogenase 1
This invention relates to novel compounds of the Formula I, Ik, Iq1-21, Ir1-21, Is1-21, It1-7, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
Owner:VITAE PHARMA INC +1
Pharmaceutical use of substituted 1,2,4-triazoles
The use of substituted 1,2,4-triazoles for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of substituted 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments has been described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Owner:NOVO NORDISK AS
Combination Therapy Using An 11beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitor And A Glucocorticoid Receptor Agonist To Minimize The Side Effects Associated With Glucocorticoid Receptor Agonist Therapy
InactiveUS20090264412A1Undesirable side-effectBiocideAnimal repellantsDisease11beta hydroxysteroid dehydrogenase
Combination therapy comprising the administration of an 11β-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist for treating some forms of cancer, diseases and disorders having inflammation as a component, and to minimize the side effects associated with glucorticoid receptor agonist therapy.
Owner:HIGH POINT PHARMA
Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines
The use of substituted pyrazolo[1,5-a]pyrimidines for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions are described. Also a novel class of substituted pyrazolo[1,5-a]pyrimidines their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
![Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines](https://images-eureka.patsnap.com/patent_img/c6c614f0-88e6-4823-8b9c-a1dbec4cadc6/US20070270408A1-20071122-C00001.png "Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines")
![Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines](https://images-eureka.patsnap.com/patent_img/c6c614f0-88e6-4823-8b9c-a1dbec4cadc6/US20070270408A1-20071122-C00002.png "Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines")
![Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines](https://images-eureka.patsnap.com/patent_img/c6c614f0-88e6-4823-8b9c-a1dbec4cadc6/US20070270408A1-20071122-C00003.png "Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines")
Owner:HIGH POINT PHARMA
Pharmaceutical use of fused 1,2,4-triazoles
The use of fused 1,2,4-triazoles for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of fused 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments has been described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and / or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Owner:HIGH POINT PHARMA
Carbamate And Urea Inhibitors Of 11Beta-Hydroxysteroid Dehydrogenase 1
This invention relates to novel compounds of the Formula I, II, III, IHa, NIb, IV, IVa, IVb, IVc, IVd, IVe, V, Va, Vb1 V1, V1a, VIb, VII, Vi1a, VIIb, VIII, V111a, VIIIb, IX, IXa, X, and Xa, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
Owner:VITAE PHARMA INC
Pharmaceutical use of substituted amides
The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Owner:HIGH POINT PHARMA
Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
InactiveUS20110112082A1Inhibitory activityAntibacterial agentsOrganic active ingredientsDiseaseMammal
This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie),(If), (Ig), (Ih), (Ii), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
Owner:VITAE PHARMA INC
Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
ActiveUS7217838B2Improve throughputLimit deliveryOrganic active ingredientsOrganic chemistryDiseaseInsulin dependent
The present invention relates to compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
Owner:ABBVIE INC
Pharmaceutical use of fused 1,2,4-triazoles
The use of fused 1,2,4-triazoles for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of fused 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments has been described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Owner:HIGH POINT PHARMA
Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
This invention relates to novel compounds of the Formula (I), dependent compounds of Formula (II), (II-A), (II-B), (II-C), (II-D), (II-E), (II-F), (II-G), (II-H), (III), (III-A), (III-B), (III-C), (IV), (IV-A), (IV-B), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
Owner:BOEHRINGER INGELHEIM INT GMBH
Adamantane derivatives for the treatment of the metabolic syndrome
Novel substituted adamantane based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
Owner:HIGH POINT PHARMA
11beta-hsd1 active compounds
A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.
Owner:HIGH POINT PHARMA
N-adamantyl benzamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase
InactiveUS20110003856A1Decreased intracellular concentrationImpaired glucose toleranceBiocideSenses disorderDisease11-beta-Hydroxysteroid Dehydrogenases
Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
Owner:HIGH POINT PHARMA
N-adamantyl benzamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase
Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
Owner:HIGH POINT PHARMA
Pharmaceutical use of substituted amides
The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and / or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Owner:HIGH POINT PHARMA
N-adamantyl benzamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase
ActiveUS20110039853A1Decreased intracellular concentrationImpaired glucose toleranceBiocideNervous disorderDisease11-beta-Hydroxysteroid Dehydrogenases
Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
Owner:VTV THERAPEUTICS LLC
INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1
This invention relates to novel compounds of the Formula (I), (Ia1-10), (Ib1-10), (Ic1-10), (Id1-7), (Ie1-5) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
Owner:BOEHRINGER INGELHEIM INT GMBH +1
Pharmaceutical use of substituted piperidine carboxamides
A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.
Owner:HIGH POINT PHARMA
Cyclic urea inhibitors of 11beta-hydroxysteroid dehydrogenase 1
Disclosed is a compound represented by Formula (I):or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Also disclosed are pharmaceutical compositions comprising the compound of Formula (I) or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof and methods of inhibiting 11β-HSD1 activity comprising the step of administering to a mammal in need of such treatment an effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Values for the variables in Formula (I) are defined herein.
Owner:VITAE PHARMA INC
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