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55 results about "11β hydroxysteroid dehydrogenase" patented technology
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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
Cyclic inhibitors of 11β-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
Indole- and benzimidazole amides as hydroxysteroid dehydrogenase inhibitors
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.
Owner:HIGH POINT PHARMA
Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
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.
Owner:BIOVITRUM AB (PUBL)
1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11β-hydroxysteroid dehydrogenase 1
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.
Owner:VITAE PHARMA INC
Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
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.
Owner:BIOVITRUM AB (PUBL)
Inhibitors of 11-β-hydroxy steroid dehydrogenase type 1
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.
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.
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.
Owner:ABBVIE INC
Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
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.
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.
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.
Owner:KING'S COLLEGE LONDON
Inhibitors of 11-beta-hydroxy steriod dehydrogenase type 1
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.
Owner:BIOVITRUM AB (PUBL)
Ihibitors of 11-beta-hydroxy steroid dehydrogenase type 1
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.
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.
Owner:CAWTHORNE ANTHONY MICHAEL +1
11β-hydroxysteroid dehydrogenase inhibitors
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.
Owner:STRIX LTD
Treatment of central nervous system disorders
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.
Owner:ABBOTT LAB INC
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
Treatment of central nervous system disorders
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.
Owner:ABBOTT LAB INC
Cyclic inhibitors of 11β-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
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.
Owner:MERCK SHARP & DOHME CORP
Biomarkers
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.
Owner:GUYS & ST THOMAS NHS FOUND TRUST +1
Inhibitors of 11-beta-hydroxysteroid dehydrogenase type 1
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.
Owner:AMGEN INC +1
Amide and amidine derivatives and uses thereof
ActiveUS8507493B2Increases the potency of topically applied hydrocortisoneReduce formationBiocideSenses disorderDiseaseGlucocorticoid
Owner:ABBVIE INC
Lactam inhibitors of 11-β-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. (I)
Owner:VITAE PHARMA INC
Indole- and benzimidazole amides as hydroxysteroid dehydrogenase inhibitors
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.
Owner:HIGH POINT PHARMA
Inhibitors of 11-β-hydroxy steroid dehydrogenase type 1
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.
Owner:AMGEN INC +1
N-adamantyl benzamides as inhibitors of 11-β-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:VTV THERAPEUTICS LLC
11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors and uses thereof
A method for treating a patient suffering from inflammation, chronic inflammation, pain, rheumatoid arthritis (RA), osteoarthritis and osteoporosis, comprising administering an effective amount of a selective inhibitor of the 11-β-hydroxysteroid dehydrogenase Type 1 enzyme.
Owner:ABBVIE INC
Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
ActiveUS20130244993A1Suitable and pharmacokinetic propertyAntibacterial agentsBiocideDyslipidemiaEnzyme
The present invention relates to compounds defined by formula I: wherein the variables A1, A2, Cy1 Cy2, Cy3, E, R1a, R1b, R2, R3, n, and Q are as defined herein, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
Owner:BOEHRINGER INGELHEIM INT GMBH +1
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