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106 results about "11-beta-Hydroxysteroid Dehydrogenases" patented technology
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Hydroxysteroid dehydrogenases that catalyzes the reversible conversion of CORTISOL to the inactive metabolite CORTISONE. Enzymes in this class can utilize either NAD or NADP as cofactors.
Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
ActiveUS20060149070A1Improve throughputLimit deliveryOrganic active ingredientsOrganic chemistryInsulin dependentEnzyme inhibitor
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
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
Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their therapeutic application
The present invention relates to the use of 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 or prophylactically treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions mediated by excessive glucocorticoid action.
Owner:ABBOTT LAB INC
Inhibitors of 11-beta hydroxysteroid dehydrogenase type I
InactiveUS20060235028A1Inhibitory activityBiocideNervous disorder11-beta-Hydroxysteroid DehydrogenasesCompound (substance)
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein G, L, Q, Z, R6, R7, and R8 are defined herein.
Owner:BRISTOL MYERS SQUIBB CO
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:ABBOTT LAB INC
Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
Owner:BRISTOL MYERS SQUIBB CO
Triazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
Owner:MERCK SHARP & DOHME LLC
Triazine 11-beta hydroxysteroid dehydrogenase type 1 inhibitors
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein.
Owner:BRISTOL MYERS SQUIBB CO
Metabolic stabilization of substituted adamantane
InactiveUS20060148871A1Good metabolic stabilityImprove stabilityBiocideAmide active ingredients11-beta-Hydroxysteroid DehydrogenasesHydroxysteroid
The present invention is directed to the method of increasing the metabolic stability of adamantane containing compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 (11-beta-HSD-1) enzyme. The stability is achieved by substitutions of the adamantane ring.
Owner:ABBOTT LAB INC
Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
ActiveUS20060281750A1Antibacterial agentsBiocide11-beta-Hydroxysteroid DehydrogenasesStereoisomerism
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: W-L-Z (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L and Z are defined herein.
Owner:BRISTOL MYERS SQUIBB CO
Inhibitors of the 11-beta-hydroxysteroid dehydrogenaseType 1 enzyme and their therapeutic application
The present invention relates to the use of 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 or prophylactically treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions mediated by excessive glucocorticoid action.
Owner:ABBOTT LAB INC
Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
ActiveUS20060281773A1Improve throughputLimit deliveryBiocideNervous disorderLipid formationInsulin dependent
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
Cyclic urea and carbamate inhibitors of 11 beta-hydroxysteroid dehydrogenase 1
InactiveUS20100197675A1Avoid conversionInhibit productionAntibacterial agentsBiocideDisease11-beta-Hydroxysteroid Dehydrogenases
This invention relates to novel compounds of the Formula (I), 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
Triazolopyridine 11-beta hydroxysteroid dehydrogenase type i inhibitors
Owner:BRISTOL MYERS SQUIBB CO
Cycloalkyl Lactame Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1
This invention relates to novel compounds of the Formula (I), any of the formulas I1-I26 Ia1-3-Ij1-3 or 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
Substituted [1,2,4]triazolo[4,3-A]pyrazine 11-beta-hydroxysteroid dehydrogenase inhibitors
Novel compounds are provided which are 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors. 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 1 1-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: W-L-Z or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L are defined herein and Z is selected from the following bicyclic heteroaryl groups: (a), (b), (c), (d).
![Substituted [1,2,4]triazolo[4,3-A]pyrazine 11-beta-hydroxysteroid dehydrogenase inhibitors](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/14c918c5-545e-4a7a-9616-6cdcaf0b3f40/US08546394-20131001-C00001.png "Substituted [1,2,4]triazolo[4,3-A]pyrazine 11-beta-hydroxysteroid dehydrogenase inhibitors")
![Substituted [1,2,4]triazolo[4,3-A]pyrazine 11-beta-hydroxysteroid dehydrogenase inhibitors](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/14c918c5-545e-4a7a-9616-6cdcaf0b3f40/US08546394-20131001-C00002.png "Substituted [1,2,4]triazolo[4,3-A]pyrazine 11-beta-hydroxysteroid dehydrogenase inhibitors")
![Substituted [1,2,4]triazolo[4,3-A]pyrazine 11-beta-hydroxysteroid dehydrogenase inhibitors](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/14c918c5-545e-4a7a-9616-6cdcaf0b3f40/US08546394-20131001-C00003.png "Substituted [1,2,4]triazolo[4,3-A]pyrazine 11-beta-hydroxysteroid dehydrogenase inhibitors")
Owner:BRISTOL MYERS SQUIBB CO
Lactam Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1
This invention relates to novel compounds of the Formula (I), (I*), (Ia), (Ib), (Ic), (Id), (Ie), (If), (If*), (Ig), (Ih), (Ij), (Ik), (ll1-3), (Im1-3), (In1-3), (lo1-2), (Ip1-9), (Iq1-9), (Ir1-9) and (Is1-3) 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
Owner:ABBVIE INC
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
Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme
InactiveUS7435833B2Improve effectivenessAvoid flowBiocideNervous disorderDisease11-beta-Hydroxysteroid Dehydrogenases
Owner:ABBVIE INC
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
Cyclic Inhibitors of 11 beta-Hydroxysteroid Dehydrogenase 1
InactiveUS20120232050A1Organic active ingredientsBiocide11-beta-Hydroxysteroid DehydrogenasesCortisone
This invention relates to novel compounds of the Formula (I), (II), (II-A), (II-B), (II-C), (II-D), (III). (III-A). (IIII-B). (III-C). (III-D), (III-E) (IV), (IV-A), (IV-B). (IV-C), (IV-D). (V), (V-A), (V-B), (V-C), (V-D), 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
11-Beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
InactiveUS20050070720A1Inhibiting the reduction of cortisoneLower Level RequirementsBiocideSenses disorderDyslipidemiaAcute hyperglycaemia
Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof: are selective inhibitors of the 11β-HSD1 enzyme. They inhibit the 11β-HSD1-mediated conversion of cortisone and other 11-keto-glucocorticoids to cortisol and other 11β-hydroxy-glucocorticoids. The 11β-HSD1 inhibitors therefore decrease the amount of cortisol in target tissues, thereby modulating the effects of cortisol. Modulation of cortisol may be effective in controlling non-insulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM or with excess cortisol in the body.
Owner:MERCK SHARP & DOHME CORP
Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
InactiveCN101137616AImprove throughputOrganic active ingredientsOrganic chemistry11-beta-Hydroxysteroid DehydrogenasesChemistry
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
Cycloalkyl Lactam Derivatives as Inhibitors of 11-Beta-Hydroxysteroid Dehydrogenase 1
InactiveUS20080275043A1Function increaseInhibit apoptosisBiocideOrganic chemistryAcute hyperglycaemiaDisease
The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Fomula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.
Owner:ELI LILLY & CO
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:ABBOTT LAB INC
Triazolopyridine 11-beta hydroxysteroid dehydrogenase type i inhibitors
ActiveUS20090093516A1High purityFew process stepsBiocideSenses disorderDisease11-beta-Hydroxysteroid Dehydrogenases
Novel compounds are provided which are 11 -beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula I:or stereoisomers or pharmaceutically acceptable salts thereof, wherein G, Q, X, Y, R3, R3a, and R3b are defined herein.
Owner:BRISTOL MYERS SQUIBB CO
Cycloalkyl Lactam Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1
InactiveUS20080207691A1Function increaseInhibit apoptosisBiocideOrganic chemistry11-beta-Hydroxysteroid DehydrogenasesSelective inhibition
The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, Ru0 is (II), or (III) G1 is methylene or ethylene; L is a divalent linking group selected from —(C1-C4) alkylene-, —S—, —CH(OH)—, or —O—; A is methylene, —S—, —O—, or —NH—; and the other substituents are as defined in the claims.
Owner:ELI LILLY & CO
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