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11β hydroxysteroid dehydrogenase patented technology retrieval search results - Eureka

Triazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1

ActiveUS6849636B2BiocideSenses disorderAcute hyperglycaemiaDyslipidemia

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.

Triazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1

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Owner:MERCK SHARP & DOHME LLC

Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1

ActiveUS8114868B2Antibacterial agentsOrganic active ingredientsMedicineEnantiomer

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.

Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1

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Owner:BOEHRINGER INGELHEIM INT GMBH

Indole- and benzimidazole amides as hydroxysteroid dehydrogenase inhibitors

InactiveUS20100076041A1Organic active ingredientsBiocideGlucocorticoidHydroxysteroid Dehydrogenases

The use of substituted amides of structure (I) for modulating the activity of 11 β-hydroxysteroid dehydrogenase type 1 (11 βHSD1) 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 11 βHSD1 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.

Indole- and benzimidazole amides as hydroxysteroid dehydrogenase inhibitors

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Owner:HIGH POINT PHARMA

Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1

InactiveUS7074788B2BiocideSenses disorderHydroxysteroidPhotochemistry

The present invention relates to compounds with the formula (I)and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1

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Owner:BIOVITRUM AB (PUBL)

1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11β-hydroxysteroid dehydrogenase 1

InactiveUS8202857B2BiocideSenses disorderDiseaseCortisone

This invention relates to novel compounds of the Formula (I), (I*), (I**), I, Ia, Ib, Ic, Id, Ie, If, Ig, Il1-3, Im1-3, In1-3, or Io1-2, 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.

1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11β-hydroxysteroid dehydrogenase 1

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Owner:VITAE PHARMA INC

Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1

InactiveUS20050009821A1BiocideOrganic chemistryHydroxysteroidPhotochemistry

The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

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Owner:BIOVITRUM AB (PUBL)

Inhibitors of 11-β-hydroxy steroid dehydrogenase type 1

InactiveUS7253196B2BiocideSenses disorderHydroxysteroidStereochemistry

The present invention relates to compounds with the formula (I), (II), (III) or (IV):wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

Inhibitors of 11-β-hydroxy steroid dehydrogenase type 1

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Owner:AMGEN INC +1

Process for making substituted 2-amino-thiazolones

InactiveUS20110160463A1High purityLarge scaleOrganic active ingredientsOrganic chemistryMedicinal chemistryHydroxysteroid

The present invention relates to methods of making compounds that inhibit 11-β-hydroxysteroid dehydrogenase type 1 enzyme (11-β HSD1). One method comprises (a) contacting a compound of formula (II) with a chiral base, deprotonating agent, and an alkylating agent R3-LG, (b) contacting the product of (a) with an acid to form a salt, and (c) reacting the salt with a base to form the compound of formula (I); wherein Z, R1, R2, and R3 are defined herein.

Process for making substituted 2-amino-thiazolones

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Owner:AMGEN INC

Novel amide and amidine derivatives and uses thereof

ActiveUS20100267738A1Decline of cognitive functionIncreases the potency of topically applied hydrocortisoneBiocideSenses disorderDiseaseGlucocorticoid

The present invention relates to inhibitors of 11-β-hydroxysteroid dehydrogenase type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.

Novel amide and amidine derivatives and uses thereof

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Owner:ABBVIE INC

Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1

InactiveUS7173030B2BiocideOrganic chemistryHydroxysteroidPhotochemistry

The present invention relates to compounds with the formula (I)and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

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Owner:BIOVITRUM AB (PUBL)

Methods and probes for diagnosing a gynaecological condition

InactiveUS20050142580A1Monitor progressSugar derivativesMicrobiological testing/measurementDiseaseDLX5

DNA sequences are identified that are useful in the diagnosis of gynaecological conditions such as endometriosis. Some of the sequences have a high identity with gene of known function such as Pim-2 oncogenes, IGFBP-5, ribosomal protein L41, propsaponin, fibulin-1, DLX5, 11β hydroxysteroid dehydrogenase type 2, SET, and RhoE. Methods for diagnosing or monitoring the progression of a gynaecological condition such as endometriosis may use primers directed to the DNA sequences identified herein.

Methods and probes for diagnosing a gynaecological condition

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Owner:TAY SUN +1

Biomarkers

InactiveUS20100047779A1Rapid and early detectionQuick checkMicrobiological testing/measurementBiomarker (petroleum)RETINOSCHISIN

The present invention provides circulating biomarkers for conditions associated with metabolic syndrome, including diabetes mellitus, hypertension and congestive heart failure. The biomarkers include plasma DNA, neuron-specific enolase, 11β-hydroxysteroid dehydrogenase, rhodopsin, retinoschisin, RPE65 and cardiac troponin T. Methods and kits for detecting these biomarkers in the prediction, monitoring and diagnosing of disease are provided, particularly for determining mRNA levels thereof in a subject's blood.

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Owner:KING'S COLLEGE LONDON

Inhibitors of 11-beta-hydroxy steriod dehydrogenase type 1

InactiveUS20050250776A1BiocideOrganic chemistryStereochemistryHydroxysteroid dehydrogenase

The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

Inhibitors of 11-beta-hydroxy steriod dehydrogenase type 1

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Owner:BIOVITRUM AB (PUBL)

Ihibitors of 11-beta-hydroxy steroid dehydrogenase type 1

InactiveUS20070066614A1BiocideOrganic chemistryGreek letter betaMedicine

The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

Ihibitors of 11-beta-hydroxy steroid dehydrogenase type 1

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Owner:BIOVITRUM AB (PUBL)

Use of leptin for infant with low birth weight for prevention of obesity

InactiveUS20050065078A1Avoid developmentEfficiently provideMilk preparationPeptide/protein ingredientsObesity preventionPediatrics

The invention discloses the therapeutic and prophylactic administration of leptin to (i) an infant of low birth weight for age; (ii) a nursing mother of an infant, the infant having low birth weight for age; or (iii) a pregnant female predisposed to giving birth to an infant of low birth weight for age; for the prevention or treatment, in later life of the infant, of a metabolic disorder or other condition associated with low birth weight, such as type 2 diabetes, obesity, cardiovascular disease, gestational diabetes, impaired glucose tolerance, insulin resistance, hypertension or syndrome X. It is thought that the beneficial properties of leptin may be due at least in part to an effect on glucocorticoid metabolism, in particular to an increase in type 2 11β-hydroxysteroid dehydrogenase activity.

Use of leptin for infant with low birth weight for prevention of obesity

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Owner:CAWTHORNE ANTHONY MICHAEL +1

11β-hydroxysteroid dehydrogenase inhibitors

InactiveUS7230020B2BiocideOrganic chemistryStereochemistry11β hydroxysteroid dehydrogenase

A compound having Formula IR1—Z—R2Formula Iwherein R1 is an optionally substituted phenyl ring; R2 is or comprises an optionally substituted aromatic ring; and Z is —X—Y—L— or —Y—X—L— wherein either X is selected from —S(═O)(═O)— and —C(═O)—; and Y is —NR3—; or X is selected from —S(═O)(═O)— and —S—, and Y is —C(R4)(R5)—; L is an optional linker; and R3, R4 and R5 are each independently selected from H and hydrocarbyl; and wherein when R2 comprises the following structural moietywherein Q is an atom selected from the group consisting of S, O, N and C; the compound is selected from compounds of the formulae R1—C(═O)—NR3—L—R2; R1—S(═O)(═O)—C(R4)(R5)—L—R2; R1—S—C(R4)(R5)—L—R2; R1—NR3—S(═O)(═O)—L—R2; R1—NR3—C(═O)—L—R2; R1—C(R4)(R5)—S(═O)(═O)—L—R2; and R1—C(R4)(R5)—S—L—R2.

11β-hydroxysteroid dehydrogenase inhibitors

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Owner:STRIX LTD

Treatment of central nervous system disorders

InactiveUS20090054426A1BiocideNervous disorderAIDS dementiaAttention deficits

A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-β-hydroxysteroid dehydrogenase Type 1 enzyme activity.

Treatment of central nervous system disorders

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Owner:ABBOTT LAB INC

Triazole derivatives as inhibitors of 11-beta hydroxysteroid dehydrogenase-1

ActiveUS20060258695A1BiocideOrganic chemistryAcute hyperglycaemiaDyslipidemia

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.

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Owner:MERCK SHARP & DOHME LLC

Treatment of central nervous system disorders

InactiveUS20100152179A9BiocideNervous disorderAIDS dementiaAttention deficits

A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-β-hydroxysteroid dehydrogenase Type 1 enzyme activity.

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Owner:ABBOTT LAB INC

Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1

ActiveUS8569292B2Organic active ingredientsSenses disorderDiseaseCortisone

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.

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Owner:VITAE PHARMA INC +1

Pyrazole Carboxamides as Inhibitors of 11-Beta-Hydroxysteroid Dehydrogenase-1

InactiveUS20080153893A1Improves glucose stimulated insulin secretionReduce insulin secretionOrganic active ingredientsBiocideAcute hyperglycaemiaDyslipidemia

Pyrazole carboxamides 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.

Pyrazole Carboxamides as Inhibitors of 11-Beta-Hydroxysteroid Dehydrogenase-1

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Owner:MERCK SHARP & DOHME CORP

Biomarkers

InactiveUS7888030B2Quick checkMicrobiological testing/measurementDiseaseRETINOSCHISIN

The present invention provides circulating biomarkers for conditions associated with metabolic syndrome, including diabetes mellitus, hypertension and congestive heart failure. The biomarkers include plasma DNA, neuron-specific enolase, 11β-hydroxysteroid dehydrogenase, rhodopsin, retinoschisin, RPE65 and cardiac troponin T. Methods and kits for detecting these biomarkers in the prediction, monitoring and diagnosing of disease are provided, particularly for determining mRNA levels thereof in a subject's blood.

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Owner:GUYS & ST THOMAS NHS FOUND TRUST +1

Inhibitors of 11-beta-hydroxysteroid dehydrogenase type 1

InactiveUS8541592B2BiocideSenses disorder11-beta-Hydroxysteroid DehydrogenasesMedicine

The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

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Owner:AMGEN INC +1

Amide and amidine derivatives and uses thereof

ActiveUS8507493B2Increases the potency of topically applied hydrocortisoneReduce formationBiocideSenses disorderDiseaseGlucocorticoid

The present invention relates to inhibitors of 11-β-hydroxysteroid dehydrogenase type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.

Amide and amidine derivatives and uses thereof

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Owner:ABBVIE INC

Lactam inhibitors of 11-β-hydroxysteroid dehydrogenase 1

InactiveUS8680281B2BiocideSenses disorderCortisoneHydrocortisone

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. (I)

Lactam inhibitors of 11-β-hydroxysteroid dehydrogenase 1

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Owner:VITAE PHARMA INC

Indole- and benzimidazole amides as hydroxysteroid dehydrogenase inhibitors

InactiveUS8153798B2BiocideNervous disorderMedical disorderGlucocorticoid

The use of substituted amides of structure (I) for modulating the activity of 11 β-hydroxysteroid dehydrogenase type 1 (11 βHSD1) 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 11 βHSD1 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.

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Owner:HIGH POINT PHARMA

Inhibitors of 11-β-hydroxy steroid dehydrogenase type 1

InactiveUS8686011B2BiocideOrganic active ingredientsHydroxysteroidStereochemistry

The present invention relates to compounds with the formula (I), (II), (III) or (IV):wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

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Owner:AMGEN INC +1

N-adamantyl benzamides as inhibitors of 11-β-hydroxysteroid dehydrogenase

ActiveUS8383820B2BiocideNervous disorderDiseaseBiochemistry

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.