Regulation of intracellular glucocorticoid concentrations

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C435S025000, C514S548000

Reexamination Certificate

active

07122531

ABSTRACT:
This invention relates to the interconversion of inactive 11-keto steroids with their active 11B-hydroxy equivalents, to methods by which the conversion of the inactive to the active form may be controlled, and to useful therapeutic effects which may be obtained as a result of such control. More specifically, but not exclusively, the invention is concerned with interconversion between cortisone and cortisol in humans.

REFERENCES:
patent: 5128150 (1992-07-01), Shanbrom
patent: 6368816 (2002-04-01), Walker et al.
patent: 97/07789 (1997-03-01), None
Gomez-Sanchez et al.; “Central hypertensionogenic effects of glycyrrhizic acid and carbenoxolone” American Jounal of Physiology; vol. 263, No. 6, E1125-1130. (1992).
Walker et al. Clinical Endocrinology 1993, pp. 221-227.
Stewart et al. J. Steroid Biochem. Molec. Bio. vol. 40, No. 4-6, pp. 501-509, 1991.
ACTH: Adrenocortical Steroids: Inhibitors Of Biosynthesis, Chapter 63, p. 1463-1473.
International Classification Of Diseases—10 (1992); pp. 332-337.
Endocrinology and Metabolism, Part Thirteen, Chapter 335, p. 1960-1965.
Anil K. Agarwalt, et al., Cloning And Expression Of Rat cDNA Encoding Corticosteroid 11β-Dehydrogenase, Journal of Biological Chemistry (1989), vol. 364, No. 32, p. 18939-18943.
Olusola A. Ajilore, et al., In Vivo Characterization Of 11β-Hydroxysteroid Dehydrogenase In Rat Hippocampus Using Glucocorticoid Neuroendangerment As an Endpoint, Neuroendocrinology (1999): 69, p. 138-144.
Robert C. Andrews, et al., Effects Of the 11β-Hydroxysteroid Dehydrogenase Inhibitor Carbenoxolone On Insulin Sensitivity In Men With Type 2 Diabetes, Journal of Clinical Endocrinology & Metabolism (2003): 88, (1), p. 285-291.
J.A. Atiea, et al., Early Morning Hyperglycaemia “Dawn Phenomenon” In Non-Insulin Dependent Diabetes Mellitus (NIDDM): Effects Of Cortisol Suppression By Metyrapone, Diabetes Research (1990): 14, p. 181-185.
C.G. Beardwell, et al., Prolonged Remission In Florid Cushing's Syndrome Following Metyrapone Treatment, Clinical Endocrinology (1981): 14, p. 485-492.
Andrew S. Brem, et al., Bidirectional Activity Of 11β-Hydroxysteroid Dehydrogenase In Vascular Smooth Muscle Cells, Steroids (1995): 60, p. 406-410.
C. Calle, et al., Decreased Insulin Binding And Antilipolytic Response In Adipocytes From Patients With Cushing's Syndrome, Bioscience Reports (1987) vol. 7, No. 9, p. 713-718.
C. Calle, et al., Binding And Antilopolytic Action Of Insulin In Isolated Adipocytes From Cortisol-Treated Rats, Revista Espanola De Fisiologia (1988) vol. 44, No. 3, p. 309-314.
S. Diederich, et al., In The Search For Specific Inhibitors Of Human 11β-Hydroxysteroid-Dehydrogenases (11β-HSDs): Chenodeoxycholic Acid Selectively Inhibits 11β-HSD-I, European Journal Of Endocrinology (2000) vol. 142, p. 200-207.
J. Donckier, et al., Successful control Of Cushing's disease In the Elderly With Long Term Metyrapone, Postgraduate Medical Journal (1986) vol. 62, p. 727-730.
D. Englehardt, et al., Therapy Of Cushing's Syndrome With Steroid Biosynthesis Inhibitors, J. Steroid Biochem. Molec. Biol. (1994) vol. 49, No. 4-6, p. 261-267.
J. Fain, et al., Effects Of Glucocorticoids On Metabolism Of Adipose Tissue In Vitro, The Journal Of Biological Chemsitry (1963) vol. 238, No. 1, p. 54-58.
Pietro Gareri, et al., Antiabsence Effects Of Carbenoxolone In Two Generic Animal Models Of Absence Epilepsy (WAG/Rij rats and lh/lh mice), Neuropharmacology (2005) vol. 49, p. 551-563.
A. Golay, et al., Evolution From Obesity To Diabetes, Diabete & Metabolisme (Paris) (1994): 20, p. 3-14.
J.A. Gomez-Capilla, et al., Effect Of Insulin And Carbenoxolone On Adrenaline Stimulated Lipolysis In Human Lipoma, Horm. Metab. Res. (1990): 22, p. 551-552.
J.A. Gomez-Capilla, et al., Effect Of Carbenoxolone On Glucose Metabolism In Rat Adipose Tissue (1988) vol. 37, No. 7, p. 1299-1301.
Elise P. Gomez-Sanchez, et al., Central Hypertensiogenic Effects Of Glycyrrhizic Acid And Carbenoxoloen, Am. J. Physiol (1992): 263, (Endocrinol. Metab. 26) p. E1125-E1130.
Paul Grinberg, et al., Effect Of Metyrapone On Insulin, Cortisol, And Glucose Tolerance Test Responses In Diabetes, New York State Journal Of Medicine (1970) p. 2341-2343.
Muhammad M. Hammami, et al., Regulation Of 11β-Hydroxysteroid Dehydrogenase Activity In Human Skin Fibroblasts: Enzymatic Modulation Of Glucocorticoid Action, Journal of Clinical Endocrinology and Metabolism (1991) vol. 73, No. 2, p. 326-334.
H. Hauner, et al., Glucocorticoids And Insulin Promote The Differentiation Of Human Adipocyte Precursor Cells Into Fat Cells, Journal of Clinical Endocrinology and Metabolism (1987), vol. 64, No. 4, p. 832-835.
A. Holmang, et al., The Effects Of Cortisol On Insulin Sensitivity In Muscle, Acta, Physiol Seand (1992): 144, p. 425-431.
B. Jeanrenaud, et al., Studies On Rat Adipose Tissue In Vitro, Journal of Biological Chemistry (1960) vol. 235, No. 8, p. 2217-2223.
W.J. Jeffcoate, et al., Metyrapone In Long-Term Management Of Cushing's Disease, British Medical Journal (1977): 2, p. 215-217.
P. H. Jellinck, et al., Differential Inhibition Of 11β-Hydroxysteroid Dehydrogenase By Carbenoxolone In Rat Brain Regions And Peripheral Tissues, J. Steroid Biochem. Molec. Biol. (1993) vol. 46, No. 2, p. 209-213.
H. J. Karl, et al., In Vitro Transformation Of Cortisol By Human Adipose Tissue, Horn. Metab. Res. (1969):1, p. 95.
V. Lakshimi, et al., Regional Distribution Of 11β-Hydroxysteroid Dehydrogenase In Rat Brain, Endocrinology (1991) vol. 128, No. 4, p. 1741-1748.
B. Lambert, et al., Effect of Carbenoxolone On Lipolysis In Rat Adipose Tissue, J. Pharm. Pharmac. (1977): 30, p. 301-303.
Joseph Levin, et al., Extraadrenal Effects Of Metyrapone In Man, Journal Of Clinical Endocrinology And Metabolism (1978) vol. 47, No. 4, p. 845-849.
D. E.W. Livingstone, et al., Is 11β-Hydroxysteroid Dehydrogenase Type 1 A Therapeutic Target? Effect Of Carbenoxolone In Lean And Obese Zucker Rats, Journal Of Pharmacology And Experimental Therapeutics (2003) vol. 305, No. 1, p. 167-172.
P. Loli, et al., Use of Ketoconazole In The Treatment Of Cushing's Syndrome, Journal Of Clinical Endocrinology And Metabolism (1986) vol. 63, No. 6, p. 1365-1371.
Susan C. Low, et al., Glucocorticoids Regulate Hippocampal 11β-Hydroxysteroid Dehydrogenase Activity And Gene Expression In Vivo In The Rat, Journal Of Neuroendocrinology (1994) vol. 6, p. 285-290.
Per Marin, et al., Cortisol Secretion in Relation To Body Fat Distribution In Obese Premenopausal Women, Metabolism (1992) vol. 41, No. 8, p. 882-886.
I. Mineu, et al., Insulinresistance: The Link Between Impaired Glucose Tolerance, Body Mass Index And Plasma Lipids, Rev. Roum. Med. Int. (1993) vol. 31, No. 4, p. 237-243.
M. Moisan, et al., 11β-Hydroxysteroid Dehydrogenase Bioactivity And Messenger RNA Expression In Rat Forebrain: Localization In Hypothalamus, Hippocampus, And Cortex, Endocrinology (1990) vol. 127, No. 3, p. 1450-1455.
C. Monder, et al., 11β-Hydroxysteroid Dehydrogenase, Vitamins and Hormones (1993) vol. 47, p. 187-271.
T. Ohno, et al., Metyrapone-Induced Thermogenesis In Cold And Heat Acclimated Rats, Japanese Journal Of Physiology (1986): 36, p. 821-825.
D. Orth, et al., Hyperfunction, The Adrenal Cortex, p. 536-562.
S. J. Quick, et al., Epithelial And Adipose Cells Isolated From mammary Glands Of Pregnant And Lactating Rats Differ in 11β-Hydroxysteroid Dehydrogenase Activity, J. Steroid Biochem. Molec. Biol. (1990) vol. 37, No. 4, p. 529-534.
S. J. Quick, et al., 11β-Hydroxysteroid Dehydrogenase Activity In The Mammary Gland, J. Steroid Biochem. (1990) vol. 35, No. 6, p. 623-625.
V. Rajan, et al., 11β-Hydroxysteroid Dehydrogenase In Cultured Hippocampal Cells Reactivates Inert 11-Dehydrocorticosterone, Potentiating Neurotoxicity, Journal Of Neuroscience (1996): 16, (1) p. 65-70.
V. Rajan, et al., Cloning, Sequencing And Tissue-Distribution Of Mouse 11β-Hydroxysteroid Dehydrogenase-1 cDNA, J. Steroid Biochem. Molec. Biol. (1995) vol. 52, No. 2, p. 141-1

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Regulation of intracellular glucocorticoid concentrations does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Regulation of intracellular glucocorticoid concentrations, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Regulation of intracellular glucocorticoid concentrations will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-3719139

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.