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59 results about "11β hsd1" patented technology
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Selective testicular 11beta-HSD inhibitors and methods of use thereof
InactiveUS20050020550A1Improving male fertilityReduced male fertilityOrganic active ingredientsCompound (substance)11β hsd2
Methods for increasing and decreasing male fertility using selective 11β-HSD1-dehydrogenase, 11β-HSD1-reductase and 11β-HSD2 dehydrogenase modulating compounds are described.
Owner:MORRIS DAVID +2
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
Inhibitors Of 11beta-Hydroxysteroid Dehydrogenase Type 1
InactiveUS20110105504A1Increase insulin sensitivityAvoid conversionAntibacterial agentsBiocide11beta hydroxysteroid dehydrogenaseDisease
This invention relates to novel compounds of the Formula (I) and 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.
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, Io1, Io2, Io5, 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 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
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
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
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
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
Carbamate and urea inhibitors of 11ß-hydroxysteroid dehydrogenase 1
This invention relates to novel compounds of the invention 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 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
Cyclic urea inhibitors of 11 b-hydroxysteroid dehydrogenase 1
This invention relates to novel compounds of the Formula (I), (Ia) and (Ib), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, j 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 11beta-hydroxysteroid dehydrogenase type 1
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 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
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
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
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
Compound having 11beta-hsd1 inhibitory activity
InactiveUS20100179325A1Strong inhibitory activitySenses disorderNervous disorderHalogenHydrogen atom
The present invention provides compounds having excellent 11β-HSD1 inhibitory activity.A compound represented by the following formula (I):[whereinX1 represents an oxygen atom, or the formula —(CR11R12)p—, etc.,Y1 represents a hydrogen atom, a hydroxyl group, etc.,Z1 represents an oxygen atom or the formula —(NR14)—,R1 represents a hydrogen atom, a halogen atom, a cyano group, a C1-4 alkyl group, a C1-4 alkyl group substituted with 1 to 3 halogen atoms, a C1-4 alkoxy group, a C1-4 alkoxycarbonyl group, a carboxyl group, a carbamoyl group, or an amino group, and m represents an integer of 1 or 2, andR2 represents a hydrogen atom or a C1-4 alkyl group, and n represents an integer of 1 or 2].
Owner:TAISHO PHARMACEUTICAL CO LTD
11-beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof:are selective inhibitors of the 11β-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidernia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.
Owner:MERCK SHARP & DOHME LLC
Compound having 11β-HSD1 inhibitory activity
Owner:TAISHO PHARMACEUTICAL CO LTD
Picolinamide and pyrimidine-4-carboxamide compounds, process for preparing and phamaceutical composition comprising the same
ActiveUS20130210811A1Selective inhibitory activityImpaired glucose toleranceAntibacterial agentsBiocideDyslipidemiaGlucocorticoid
Provided are picolinamide and pyrimidine-4-carboxamide compounds, a method for preparing the same, a pharmaceutical composition containing the same, and a medical use using the compound as an agent for preventing, regulating, and treating diseases related to regulation of glucocorticoids by using selective inhibitory activity of the compound for an 11β-HSD1 enzyme. The picolinamide and pyrimidine-4-carboxamide compounds of the present invention are selective inhibitors of human-derived 11β-HSD1 enzymes, and are useful in an agent for preventing, regulating, and treating diseases related to glucocorticoid regulation in which human-derived 11β-HSD1 enzymes are involved, for example, metabolic syndromes such as, type 1 and type 2 diabetes, diabetes later complications, latent autoimmune diabetes adult (LADA), insulin tolerance syndromes, obesity, impaired glucose tolerance (IGT), impaired fasting glucose (IFG), damaged glucose tolerance, dyslipidemia, atherosclerosis, hypertension, etc.
Owner:SK CHEM CO LTD
Amido-Isothiazole Compounds and Their Use as Inhibitors of 11Beta-HSD1 for the Treatment of Metabolic Syndrome and Related Disorders
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-isothiazole compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
Owner:THE UNIV COURT OF THE UNIV OF EDINBURGH
Amido-Thiophene Compounds and Their Use as 11-Beta-HSD1 Inhibitors
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
Owner:THE UNIV OF EDINBURGH
Amido-thiophene compounds and their use
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
Owner:THE UNIV COURT OF THE UNIV OF EDINBURGH
Amido-Thiophene Compounds and Their Use
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
Owner:THE UNIV OF EDINBURGH
Substituted quinoxalines, their preparation and their therapeutical use as 11βHSD1 modulators
The present invention is related to a compound of formula (I):wherein i, j, n, o, p, q, r, R1a, R1b, R1c, R1d, R2a, R2b, R2c, R2d, R3a, R3b and R4 are as defined herein, or an addition salt with an acid thereof, or a hydrate or solvate thereof, its preparation, pharmaceutical composition, and uses for treating a disease in which the enzyme 11β-HSD1 is involved.
Owner:SANOFI AVENTIS SA
Lipid profile modulation
InactiveUS20050032761A1Altered cardiovascular risk profileLower Level RequirementsOrganic active ingredientsMetabolism disorderLipid regulation11β hsd1
The invention provides use of an agent which lowers levels of 11β-HSD1 in the manufacture of a composition for the promotion of an atheroprotective lipid profile.
Owner:THE UNIV OF EDINBURGH
N-cyclohexyl benzamides and benzeneacetamides as inhibitors of 11-beta-hydroxysteroid dehydrogenases
InactiveUS20080221175A1Relieve effectIncrease insulin sensitivityBiocideOrganic chemistryBenzeneacetamides11-beta-Hydroxysteroid Dehydrogenases
The present invention provides N-cyclohexyl benzamide and benzeneacetamide compounds according to formula (I):where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, m, n, p, and q are as defined in the description; as well as pharmaceutical compositions comprising the same, methods of use of the compounds and compositions of the invention for the treatment of conditions associated with hydroxysteroid dehydrogenases (e.g., 11β-HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.
Owner:AMGEN INC
3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanones as inhibitors of 11 (BETA)-hsd1
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, 3,3-disubstituted-(6-aza-bicyclo[3.1.1]hept-6-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, and 4,4-disubstituted piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds of the following formula that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
![3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanones as inhibitors of 11 (BETA)-hsd1](https://images-eureka.patsnap.com/patent_img/376f7422-66fb-420d-95c3-10472bb1ef39/US20130123268A1-20130516-C00001.png "3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanones as inhibitors of 11 (BETA)-hsd1")
![3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanones as inhibitors of 11 (BETA)-hsd1](https://images-eureka.patsnap.com/patent_img/376f7422-66fb-420d-95c3-10472bb1ef39/US20130123268A1-20130516-C00002.png "3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanones as inhibitors of 11 (BETA)-hsd1")
![3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanones as inhibitors of 11 (BETA)-hsd1](https://images-eureka.patsnap.com/patent_img/376f7422-66fb-420d-95c3-10472bb1ef39/US20130123268A1-20130516-C00003.png "3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanones as inhibitors of 11 (BETA)-hsd1")
Owner:THE UNIV COURT OF THE UNIV OF EDINBURGH
Amido-thiophene compounds and their use as 11-beta-HSD1 inhibitors
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
Owner:THE UNIV COURT OF THE UNIV OF EDINBURGH
Selective 11beta HSD inhibitors and methods of use thereof
InactiveUS20060148725A1Extended half-lifeBiocideOrganic active ingredientsCompound (substance)11β hsd2
Methods for treating glucocorticoid associated states using selective 11β-HSD1-dehydrogenase, 11β-HSD1-reductase and 11β-HSD2 dehydrogenase modulating compounds are described.
Owner:RHODE ISLAND HOSPITAL +1
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