메뉴 건너뛰기




Volumn 11, Issue 4, 2008, Pages 495-511

Recent advances in the discovery of 11β-HSD1 inhibitors

Author keywords

11 Hydroxysteroid dehydrogenase type 1; Glucocorticoids; Inhibitor; Metabolic syndrome; Obesity; Type 2 diabetes

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE; 11BETA HYDROXYSTEROID DEHYDROGENASE 1 INHIBITOR; 2 PYRROLIDONE DERIVATIVE; 3 CHLORO 2 METHYL N [4 [2 (4 METHYL 1 PIPERAZINYL) 2 OXOETHYL] 2 THIAZOLYL]BENZENESULFONAMIDE; ADAMANTANE DERIVATIVE; AMG 221; AMG 311; BICYCLO COMPOUND; BVT 14225; CARBENOXOLONE; CORTISONE; ENZYME INHIBITOR; FATTY ACID BINDING PROTEIN; GLYCYRRHETINIC ACID DERIVATIVE; HETEROCYCLIC COMPOUND; HYDROCORTISONE; INCB 13739; INCB 20817; METFORMIN; MIFEPRISTONE; NATURAL PRODUCT; PF 915275; PYRAZOLONE DERIVATIVE; PYRROLIDINE DERIVATIVE; QUINOLINE DERIVATIVE; SULFONAMIDE; THIAZOLE DERIVATIVE; TRIAZOLE DERIVATIVE; TROPANE DERIVATIVE; UNINDEXED DRUG;

EID: 46749139850     PISSN: 13676733     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review
Times cited : (39)

References (131)
  • 1
    • 84904153348 scopus 로고    scopus 로고
    • Obesity and overweight
    • World Health Organization, Geneva, Switzerland , www
    • Obesity and overweight. Fact sheet 311: World Health Organization, Geneva, Switzerland (2006). www.who.int/mediacentre/factsheets/fs311/en/ index.html
    • (2006) Fact sheet , vol.311
  • 2
    • 46749091003 scopus 로고    scopus 로고
    • Diabetes
    • World Health Organization, Geneva, Switzerland
    • Diabetes. Fact sheet 312: World Health Organization, Geneva, Switzerland (2006). www.who.int/mediacentre/factsheets/fs312/en/index.html
    • (2006) Fact sheet , vol.312
  • 3
    • 0037223174 scopus 로고    scopus 로고
    • Mokdad AH, Ford ES, Bowman BA, Dietz WH, Vinicor F, Bales VS, Marks JS: Prevalence of obesity, diabetes, and obesity-related health risk factors, 2001. J Am Med Assoc (2003) 289(1):76-79.
    • Mokdad AH, Ford ES, Bowman BA, Dietz WH, Vinicor F, Bales VS, Marks JS: Prevalence of obesity, diabetes, and obesity-related health risk factors, 2001. J Am Med Assoc (2003) 289(1):76-79.
  • 4
    • 17144380822 scopus 로고    scopus 로고
    • The metabolic syndrome
    • Eckel RH, Grundy SM, Zimmet PZ: The metabolic syndrome. Lancet (2005) 365(9468):1415-1428.
    • (2005) Lancet , vol.365 , Issue.9468 , pp. 1415-1428
    • Eckel, R.H.1    Grundy, S.M.2    Zimmet, P.Z.3
  • 5
    • 40749133016 scopus 로고    scopus 로고
    • Challenges in developing drugs for the metabolic syndrome
    • Matfin G: Challenges in developing drugs for the metabolic syndrome. Curr Diabetes Rep (2008) 8(1):31-36.
    • (2008) Curr Diabetes Rep , vol.8 , Issue.1 , pp. 31-36
    • Matfin, G.1
  • 6
    • 33751215200 scopus 로고    scopus 로고
    • Cortisol - cause and cure for metabolic syndrome?
    • Walker BR: Cortisol - cause and cure for metabolic syndrome? Diabetes Med (2006) 23(12):1281-1288.
    • (2006) Diabetes Med , vol.23 , Issue.12 , pp. 1281-1288
    • Walker, B.R.1
  • 7
    • 40349090041 scopus 로고    scopus 로고
    • Glucocorticoids and 11β-hydroxysteroid dehydrogenase type 1 in obesity and the metabolic syndrome
    • Stimson RH, Walker BR: Glucocorticoids and 11β-hydroxysteroid dehydrogenase type 1 in obesity and the metabolic syndrome. Minerva Endocrinol (2007) 32(3):141-159.
    • (2007) Minerva Endocrinol , vol.32 , Issue.3 , pp. 141-159
    • Stimson, R.H.1    Walker, B.R.2
  • 8
    • 42149162795 scopus 로고    scopus 로고
    • Hughes KA, Webster SP, Walker BR: 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors in type 2 diabetes mellitus and obesity. Expert Opin Invest Drugs (2008) 17(4):481-496. •• A recent review of 11β-HSD1 inhibitors that includes a summary of preclinical and clinical results of advanced structural classes and their implications for the treatment of various aspects of metabolic syndrome. Several primary references on the biology of 11β-HSD1 inhibition are also included.
    • Hughes KA, Webster SP, Walker BR: 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors in type 2 diabetes mellitus and obesity. Expert Opin Invest Drugs (2008) 17(4):481-496. •• A recent review of 11β-HSD1 inhibitors that includes a summary of preclinical and clinical results of advanced structural classes and their implications for the treatment of various aspects of metabolic syndrome. Several primary references on the biology of 11β-HSD1 inhibition are also included.
  • 9
    • 34447105433 scopus 로고    scopus 로고
    • Wamil M, Seckl JR: Inhibition of 11β-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target. Drug Disc Today (2007) 12(13-14):504-520. •• A recent review of 11β-HSD1 inhibitors that includes a detailed summary of human studies of 11β-HSD1 inhibition and several primary references on the biology of 11β-HSD1 inhibition.
    • Wamil M, Seckl JR: Inhibition of 11β-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target. Drug Disc Today (2007) 12(13-14):504-520. •• A recent review of 11β-HSD1 inhibitors that includes a detailed summary of human studies of 11β-HSD1 inhibition and several primary references on the biology of 11β-HSD1 inhibition.
  • 10
    • 33744935789 scopus 로고    scopus 로고
    • Recent progress in 11-β-hydroxysteroid dehydrogenase type 1 (11-β-HSD1) inhibitor development
    • Barf T, Williams M: Recent progress in 11-β-hydroxysteroid dehydrogenase type 1 (11-β-HSD1) inhibitor development. Drugs Future (2006) 31(3):231-243.
    • (2006) Drugs Future , vol.31 , Issue.3 , pp. 231-243
    • Barf, T.1    Williams, M.2
  • 11
    • 33645784827 scopus 로고    scopus 로고
    • Inhibitors of 11β-hydroxysteroid dehydrogenase type 1 for the treatment of metabolic syndrome
    • Wang M: Inhibitors of 11β-hydroxysteroid dehydrogenase type 1 for the treatment of metabolic syndrome. Curr Opin Invest Drugs (2006) 7(4):319-323.
    • (2006) Curr Opin Invest Drugs , vol.7 , Issue.4 , pp. 319-323
    • Wang, M.1
  • 12
    • 33748645318 scopus 로고    scopus 로고
    • Type 1 11β-hydroxysteroid dehydrogenase as universal drug target in metabolic diseases?
    • Oppermann U: Type 1 11β-hydroxysteroid dehydrogenase as universal drug target in metabolic diseases? Endocr Metab Immune Disord Drug Targets (2006) 6(3):259-269.
    • (2006) Endocr Metab Immune Disord Drug Targets , vol.6 , Issue.3 , pp. 259-269
    • Oppermann, U.1
  • 13
    • 33845221938 scopus 로고    scopus 로고
    • Tissue-specific glucocorticoid excess in the metabolic syndrome: 11β-HSD1 as a therapeutic target
    • Wang M: Tissue-specific glucocorticoid excess in the metabolic syndrome: 11β-HSD1 as a therapeutic target. Drug Dev Res (2006) 67(7):567-569.
    • (2006) Drug Dev Res , vol.67 , Issue.7 , pp. 567-569
    • Wang, M.1
  • 14
    • 33846391295 scopus 로고    scopus 로고
    • Boyle CD, Kowalski T, Zhang L: 11β-Hydroxysteroid dehydrogenase type 1 inhibitors. Annu Rep Med Chem (2006) 41:127-140. • Provides a summary of the background of 11β-HSD1 inhibition and the structural classes of 11β-HSD1 inhibitors that had been reported up to 2006. Several primary references on the biology of 11β-HSD1 inhibition are also included.
    • Boyle CD, Kowalski T, Zhang L: 11β-Hydroxysteroid dehydrogenase type 1 inhibitors. Annu Rep Med Chem (2006) 41:127-140. • Provides a summary of the background of 11β-HSD1 inhibition and the structural classes of 11β-HSD1 inhibitors that had been reported up to 2006. Several primary references on the biology of 11β-HSD1 inhibition are also included.
  • 15
    • 34250791225 scopus 로고    scopus 로고
    • Readjusting the glucocorticoid balance: An opportunity for modulators of 11β-hydroxysteroid dehydrogenase type 1 activity?
    • Atanasov AG, Odermatt A: Readjusting the glucocorticoid balance: An opportunity for modulators of 11β-hydroxysteroid dehydrogenase type 1 activity? Endocr Metab Immune Disord Drug Targets (2007) 7(2):125-140.
    • (2007) Endocr Metab Immune Disord Drug Targets , vol.7 , Issue.2 , pp. 125-140
    • Atanasov, A.G.1    Odermatt, A.2
  • 18
    • 0031572610 scopus 로고    scopus 로고
    • Function, gene organization and protein structures of 11β-hydroxysteroid dehydrogenase isoforms
    • Oppermann UC, Persson B, Jörnvall H: Function, gene organization and protein structures of 11β-hydroxysteroid dehydrogenase isoforms. Eur J Biochem (1997) 249(2):355-360.
    • (1997) Eur J Biochem , vol.249 , Issue.2 , pp. 355-360
    • Oppermann, U.C.1    Persson, B.2    Jörnvall, H.3
  • 20
    • 0024410541 scopus 로고
    • Licorice inhibits corticosteroid 11β-dehydrogenase of rat kidney and liver: In vivo and in vitro studies
    • Monder C, Stewart PM, Lakshmi V, Valentino R, Burt D, Edwards CR: Licorice inhibits corticosteroid 11β-dehydrogenase of rat kidney and liver: In vivo and in vitro studies. Endocrinology (1989) 125(2):1046-1053.
    • (1989) Endocrinology , vol.125 , Issue.2 , pp. 1046-1053
    • Monder, C.1    Stewart, P.M.2    Lakshmi, V.3    Valentino, R.4    Burt, D.5    Edwards, C.R.6
  • 21
    • 0028034209 scopus 로고
    • Cloning and tissue distribution of the human 11β-hydroxysteroid dehydrogenase type 2 enzyme
    • Albiston AL, Obeyesekere VR, Smith RE, Krozowski ZS: Cloning and tissue distribution of the human 11β-hydroxysteroid dehydrogenase type 2 enzyme. Mol Cell Endocrinol (1994) 105(2):R11-R17.
    • (1994) Mol Cell Endocrinol , vol.105 , Issue.2
    • Albiston, A.L.1    Obeyesekere, V.R.2    Smith, R.E.3    Krozowski, Z.S.4
  • 22
    • 0037194658 scopus 로고    scopus 로고
    • Barf T, Vallgårda J, Emond R, Häggström C, Kurz G, Nygren A, Larwood V, Mosialou E, Axelsson K, Olsson R, Engblom L et al: Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11β-hydroxysteroid dehydrogenase type 1. J Med Chem (2002) 45(18):3813-3815. • Describes the discovery of the first potent and selective small-molecule 11β-HSD1 inhibitors BVT-14225 and BVT-2733.
    • Barf T, Vallgårda J, Emond R, Häggström C, Kurz G, Nygren A, Larwood V, Mosialou E, Axelsson K, Olsson R, Engblom L et al: Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11β-hydroxysteroid dehydrogenase type 1. J Med Chem (2002) 45(18):3813-3815. • Describes the discovery of the first potent and selective small-molecule 11β-HSD1 inhibitors BVT-14225 and BVT-2733.
  • 23
    • 23944493717 scopus 로고    scopus 로고
    • Hermanowski-Vosatka A, Balkovec JM, Cheng K, Chen HY, Hernandez M, Koo GC, Le Grand CB, Li Z, Metzger JM, Mundt SS, Noonan H et al: 11β-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice. J Exp Med (2005) 202(4):517-527. • Describes several rodent studies with the selective triazole 11β-HSD1 inhibitor from Merck. The in vivo results were the first to demonstrate a positive effect on atherosclerosis with a small-molecule 11β-HSD1 inhibitor. Further experiments with the triazole also demonstrated positive effects on the other components of metabolic syndrome.
    • Hermanowski-Vosatka A, Balkovec JM, Cheng K, Chen HY, Hernandez M, Koo GC, Le Grand CB, Li Z, Metzger JM, Mundt SS, Noonan H et al: 11β-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice. J Exp Med (2005) 202(4):517-527. • Describes several rodent studies with the selective triazole 11β-HSD1 inhibitor from Merck. The in vivo results were the first to demonstrate a positive effect on atherosclerosis with a small-molecule 11β-HSD1 inhibitor. Further experiments with the triazole also demonstrated positive effects on the other components of metabolic syndrome.
  • 24
    • 0025815544 scopus 로고
    • The endocrine effects of long-term treatment with mifepristone (RU 486)
    • Lamberts SW, Koper JW, de Jong FH: The endocrine effects of long-term treatment with mifepristone (RU 486). J Clin Endocrinol Metab (1991) 73(1):187-191.
    • (1991) J Clin Endocrinol Metab , vol.73 , Issue.1 , pp. 187-191
    • Lamberts, S.W.1    Koper, J.W.2    de Jong, F.H.3
  • 25
    • 37849041637 scopus 로고    scopus 로고
    • Hale C, Véniant M, Wang Z, Chen M, McCormick J, Cupples R, Hickman D, Min X, Sudom A, Xu H, Matsumoto G et al: Structural characterization and pharmacodynamic effects of an orally active 11β-hydroxysteroid dehydrogenase type 1 inhibitor. Chem Biol Drug Des (2008) 71(1):36-44. • Describes the full characterization of the selective small-molecule 11β-HSD1 inhibitor compound 2922 from Amgen, including a mouse model that demonstrated a lack of hypothalamic- pituitary-adrenal axis activation by compound 2922.
    • Hale C, Véniant M, Wang Z, Chen M, McCormick J, Cupples R, Hickman D, Min X, Sudom A, Xu H, Matsumoto G et al: Structural characterization and pharmacodynamic effects of an orally active 11β-hydroxysteroid dehydrogenase type 1 inhibitor. Chem Biol Drug Des (2008) 71(1):36-44. • Describes the full characterization of the selective small-molecule 11β-HSD1 inhibitor compound 2922 from Amgen, including a mouse model that demonstrated a lack of hypothalamic- pituitary-adrenal axis activation by compound 2922.
  • 26
    • 36549001222 scopus 로고    scopus 로고
    • Glucocorticoids and cardiovascular disease
    • Walker BR: Glucocorticoids and cardiovascular disease. Eur J Endocrinol (2007) 157(5):545-559.
    • (2007) Eur J Endocrinol , vol.157 , Issue.5 , pp. 545-559
    • Walker, B.R.1
  • 27
    • 33644926098 scopus 로고    scopus 로고
    • The role of 11β-hydroxysteroid dehydrogenases in the brain
    • Holmes MC, Seckl JR: The role of 11β-hydroxysteroid dehydrogenases in the brain. Mol Cell Endocrinol (2006) 248 (1-2):9-14.
    • (2006) Mol Cell Endocrinol , vol.248 , Issue.1-2 , pp. 9-14
    • Holmes, M.C.1    Seckl, J.R.2
  • 28
    • 2342616297 scopus 로고    scopus 로고
    • 11β-Hydroxysteroid dehydrogenase inhibition improves cognitive function in healthy elderly men and type 2 diabetics
    • Sandeep TC, Yau JL, MacLullich AM, Noble J, Deary IJ, Walker BR, Seckl JR: 11β-Hydroxysteroid dehydrogenase inhibition improves cognitive function in healthy elderly men and type 2 diabetics. Proc Natl Acad Sci USA (2004) 101(17):6734-6739.
    • (2004) Proc Natl Acad Sci USA , vol.101 , Issue.17 , pp. 6734-6739
    • Sandeep, T.C.1    Yau, J.L.2    MacLullich, A.M.3    Noble, J.4    Deary, I.J.5    Walker, B.R.6    Seckl, J.R.7
  • 30
    • 38149133022 scopus 로고    scopus 로고
    • Webster SP, Pallin TD: 11β-Hydroxysteroid dehydrogenase type 1 inhibitors as therapeutic agents. Expert Opin Ther Pat (2007) 17(12):1407-1422. • A recent and extensive 11β-HSD1 patent review covering the literature from 2006 to August 2007.
    • Webster SP, Pallin TD: 11β-Hydroxysteroid dehydrogenase type 1 inhibitors as therapeutic agents. Expert Opin Ther Pat (2007) 17(12):1407-1422. • A recent and extensive 11β-HSD1 patent review covering the literature from 2006 to August 2007.
  • 31
    • 15544380476 scopus 로고    scopus 로고
    • Fotsch C, Askew BC, Chen JJ: 11β-Hydroxysteroid dehydrogenase-1 as a therapeutic target for metabolic diseases. Expert Opin Ther Pat (2005) 15(3):289-303. • The first extensive patent review of 11β-HSD1 inhibitors covering the literature up to 2005.
    • Fotsch C, Askew BC, Chen JJ: 11β-Hydroxysteroid dehydrogenase-1 as a therapeutic target for metabolic diseases. Expert Opin Ther Pat (2005) 15(3):289-303. • The first extensive patent review of 11β-HSD1 inhibitors covering the literature up to 2005.
  • 32
    • 34250173800 scopus 로고    scopus 로고
    • Inhibition of human and rat 11β-hydroxysteroid dehydrogenase type 1 by 18β-glycyrrhetinic acid derivatives
    • Su X, Vicker N, Lawrence H, Smith A, Purohit A, Reed MJ, Potter BV: Inhibition of human and rat 11β-hydroxysteroid dehydrogenase type 1 by 18β-glycyrrhetinic acid derivatives. J Steroid Biochem Mol Biol (2007) 104(3-5):312-320.
    • (2007) J Steroid Biochem Mol Biol , vol.104 , Issue.3-5 , pp. 312-320
    • Su, X.1    Vicker, N.2    Lawrence, H.3    Smith, A.4    Purohit, A.5    Reed, M.J.6    Potter, B.V.7
  • 33
    • 33745855823 scopus 로고    scopus 로고
    • Coffee inhibits the reactivation of glucocorticoids by 11β-hydroxysteroid dehydrogenase type 1: A glucocorticoid connection in the anti-diabetic action of coffee?
    • Atanasov AG, Dzyakanchuk AA, Schweizer RA, Nashev LG, Maurer EM, Odermatt A: Coffee inhibits the reactivation of glucocorticoids by 11β-hydroxysteroid dehydrogenase type 1: A glucocorticoid connection in the anti-diabetic action of coffee? FEBS Lett (2006) 580(17):4081-4085.
    • (2006) FEBS Lett , vol.580 , Issue.17 , pp. 4081-4085
    • Atanasov, A.G.1    Dzyakanchuk, A.A.2    Schweizer, R.A.3    Nashev, L.G.4    Maurer, E.M.5    Odermatt, A.6
  • 34
    • 34249996711 scopus 로고    scopus 로고
    • Endogenous inhibitors (GALFs) of 11β-hydroxysteroid dehydrogenase isoforms 1 and 2: Derivatives of adrenally produced corticosterone and cortisol
    • Morris DJ, Latif SA, Hardy MP, Brem AS: Endogenous inhibitors (GALFs) of 11β-hydroxysteroid dehydrogenase isoforms 1 and 2: Derivatives of adrenally produced corticosterone and cortisol. J Steroid Biochem Mol Biol (2007) 104(3-5):161-168.
    • (2007) J Steroid Biochem Mol Biol , vol.104 , Issue.3-5 , pp. 161-168
    • Morris, D.J.1    Latif, S.A.2    Hardy, M.P.3    Brem, A.S.4
  • 35
    • 46749119570 scopus 로고    scopus 로고
    • AMG-211. Thomson Pharma Drug Report, Thomson Reuters - Scientific, London, UK (2008).
    • AMG-211. Thomson Pharma Drug Report, Thomson Reuters - Scientific, London, UK (2008).
  • 37
    • 21144456678 scopus 로고    scopus 로고
    • Synthesis and biological evaluation of sulfonamidooxazoles and β-keto sulfones: Selective inhibitors of 11β-hydroxysteroid dehydrogenase type I
    • Xiang J, Ipek M, Suri V, Massefski W, Pan N, Ge T, Tam M, Xing Y, Tobin JF, Xu X, Tam S: Synthesis and biological evaluation of sulfonamidooxazoles and β-keto sulfones: Selective inhibitors of 11β-hydroxysteroid dehydrogenase type I. Bioorg Med Chem Lett (2005) 15(11):2865-2869.
    • (2005) Bioorg Med Chem Lett , vol.15 , Issue.11 , pp. 2865-2869
    • Xiang, J.1    Ipek, M.2    Suri, V.3    Massefski, W.4    Pan, N.5    Ge, T.6    Tam, M.7    Xing, Y.8    Tobin, J.F.9    Xu, X.10    Tam, S.11
  • 41
    • 33846228383 scopus 로고    scopus 로고
    • Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11β-hydroxysteroid dehydrogenase type 1 inhibitors
    • Rohde JJ, Pliushchev MA, Sorensen BK, Wodka D, Shuai Q, Wang J, Fung S, Monzon KM, Chiou WJ, Pan L, Deng X et al: Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11β-hydroxysteroid dehydrogenase type 1 inhibitors. J Med Chem (2007) 50(1):149-164.
    • (2007) J Med Chem , vol.50 , Issue.1 , pp. 149-164
    • Rohde, J.J.1    Pliushchev, M.A.2    Sorensen, B.K.3    Wodka, D.4    Shuai, Q.5    Wang, J.6    Fung, S.7    Monzon, K.M.8    Chiou, W.J.9    Pan, L.10    Deng, X.11
  • 47
    • 33748937192 scopus 로고    scopus 로고
    • A highly efficient synthesis of potent and selective butyrolactam inhibitors of 11β-HSD1
    • Yeh VS, Kurukulasuriya R, Kerdesky FA: A highly efficient synthesis of potent and selective butyrolactam inhibitors of 11β-HSD1. Org Lett (2006) 8(18):3963-3966.
    • (2006) Org Lett , vol.8 , Issue.18 , pp. 3963-3966
    • Yeh, V.S.1    Kurukulasuriya, R.2    Kerdesky, F.A.3
  • 58
    • 37349004141 scopus 로고    scopus 로고
    • Bhat BG, Hosea N, Fanjul A, Herrera J, Chapman J, Thalacker F, Stewart PM, Rejto PA: Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic relationship with 4′-cyano-biphenyl-4-sulfonic acid (6-amino-pyridin-2-yl)-amide (PF-915275), an inhibitor of 11β- hydroxysteroid dehydrogenase type 1, in cynomolgus monkeys. J Pharmacol Exp Ther (2008) 324(1):299-305. • Describes the use of exogenous prednisone to prednisolone conversion as a biomarker for 11β-HSD1 inhibition.
    • Bhat BG, Hosea N, Fanjul A, Herrera J, Chapman J, Thalacker F, Stewart PM, Rejto PA: Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic relationship with 4′-cyano-biphenyl-4-sulfonic acid (6-amino-pyridin-2-yl)-amide (PF-915275), an inhibitor of 11β- hydroxysteroid dehydrogenase type 1, in cynomolgus monkeys. J Pharmacol Exp Ther (2008) 324(1):299-305. • Describes the use of exogenous prednisone to prednisolone conversion as a biomarker for 11β-HSD1 inhibition.
  • 59
    • 39049131253 scopus 로고    scopus 로고
    • Modulation of 11β-hydroxysteroid dehydrogenase (11βHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11βHSD1 inhibitor
    • Describes the application of the prednisone/prednisolone biomarker see reference [58•, in human clinical trials of the selective 11β-HSD1 inhibitor PF-915275, ••
    • Courtney R, Stewart PM, Toh M, Ndongo MN, Calle RA, Hirshberg B: Modulation of 11β-hydroxysteroid dehydrogenase (11βHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11βHSD1 inhibitor. J Clin Endocrinol Metab (2008) 93(2):550-556. •• Describes the application of the prednisone/prednisolone biomarker (see reference [58•]) in human clinical trials of the selective 11β-HSD1 inhibitor PF-915275.
    • (2008) J Clin Endocrinol Metab , vol.93 , Issue.2 , pp. 550-556
    • Courtney, R.1    Stewart, P.M.2    Toh, M.3    Ndongo, M.N.4    Calle, R.A.5    Hirshberg, B.6
  • 63
    • 46749139225 scopus 로고    scopus 로고
    • BVT-3498. Thomson Pharma Drug Report, Thomson Reuters - Scientific, London, UK (2008).
    • BVT-3498. Thomson Pharma Drug Report, Thomson Reuters - Scientific, London, UK (2008).
  • 64
    • 84862913174 scopus 로고    scopus 로고
    • Thousand Oaks, CA, USA
    • Pipeline: Amgen Inc, Thousand Oaks, CA, USA (2008). wwwext.amgen.com/science/pipe.jsp
    • (2008) Pipeline
  • 65
    • 46749125097 scopus 로고    scopus 로고
    • Incyte reports progress in multiple clinical programs; expands JAK inhibitor program; announces 2007 financial results and provides 2008 financial guidance
    • Incyte Corp:, February 14
    • Incyte Corp: Incyte reports progress in multiple clinical programs; expands JAK inhibitor program; announces 2007 financial results and provides 2008 financial guidance. Press Release (2008) February 14.
    • (2008) Press Release
  • 66
    • 46749122400 scopus 로고    scopus 로고
    • INCB-13739. Thomson Pharma Drug Report, Thomson Reuters - Scientific, London, UK (2008).
    • INCB-13739. Thomson Pharma Drug Report, Thomson Reuters - Scientific, London, UK (2008).
  • 67
    • 46749154807 scopus 로고    scopus 로고
    • Incyte Corp, Wilmington, DE, USA
    • Incyte's Product Pipeline: Incyte Corp, Wilmington, DE, USA (2008). www.incyte.com/drugs_product_pipeline.html
    • (2008) Incyte's Product Pipeline
  • 68
    • 33745312505 scopus 로고    scopus 로고
    • Lipid-lowering drugs
    • Pahan K: Lipid-lowering drugs. Cell Mol Life Sci (2006) 63(10):1165-1178.
    • (2006) Cell Mol Life Sci , vol.63 , Issue.10 , pp. 1165-1178
    • Pahan, K.1
  • 69
    • 34848892188 scopus 로고    scopus 로고
    • Non-insulin therapies for type 2 diabetes
    • Ashiya M, Smith RET: Non-insulin therapies for type 2 diabetes. Nat Rev Drug Discov (2007) 6(10):777-778.
    • (2007) Nat Rev Drug Discov , vol.6 , Issue.10 , pp. 777-778
    • Ashiya, M.1    Smith, R.E.T.2
  • 70
    • 46749084816 scopus 로고    scopus 로고
    • MIRIAM HOSPITAL/POPULATION COUNCIL (Morris DJ, Latif SA, Hardy MP, Ge R): Selective testicular 11β-HSD inhibitors for the treatment of hypergonadism associated disorders and modulation of fertility. US-20070219172 (2007).
    • MIRIAM HOSPITAL/POPULATION COUNCIL (Morris DJ, Latif SA, Hardy MP, Ge R): Selective testicular 11β-HSD inhibitors for the treatment of hypergonadism associated disorders and modulation of fertility. US-20070219172 (2007).
  • 71
    • 46749090610 scopus 로고    scopus 로고
    • TAISHO PHARMACEUTICAL CO LTD (Fukushima H, Takahashi M, Mikami A, Busujima T, Kawaguchi T, Hirano H): Thiazole derivative. WO-2006051662 (2006).
    • TAISHO PHARMACEUTICAL CO LTD (Fukushima H, Takahashi M, Mikami A, Busujima T, Kawaguchi T, Hirano H): Thiazole derivative. WO-2006051662 (2006).
  • 72
    • 46749096495 scopus 로고    scopus 로고
    • TAKEDA SAN DIEGO INC (Brennan NK, Chang E, Kaldor SW, Kiryanov AA, Jennings AJ, Stafford JA): Hydroxysteroid dehydrogenase inhibitors. WO-2006066109 (2006).
    • TAKEDA SAN DIEGO INC (Brennan NK, Chang E, Kaldor SW, Kiryanov AA, Jennings AJ, Stafford JA): Hydroxysteroid dehydrogenase inhibitors. WO-2006066109 (2006).
  • 73
    • 46749097693 scopus 로고    scopus 로고
    • HOFFMANN-LA ROCHE INC (Gillespie P, Goodnow RA, Kowalczyk A, Le K, Zhang Q): Thiazoles as inhibitors of 11β-hydroxysteroid dehydrogenase. US-20070167622 (2007).
    • HOFFMANN-LA ROCHE INC (Gillespie P, Goodnow RA, Kowalczyk A, Le K, Zhang Q): Thiazoles as inhibitors of 11β-hydroxysteroid dehydrogenase. US-20070167622 (2007).
  • 74
    • 46749158841 scopus 로고    scopus 로고
    • ONO PHARMACEUTICAL CO LTD (Egashira H, Nishiyama E): Sulfonamide compound and pharmaceutical thereof. WO-2006095822 (2006).
    • ONO PHARMACEUTICAL CO LTD (Egashira H, Nishiyama E): Sulfonamide compound and pharmaceutical thereof. WO-2006095822 (2006).
  • 75
    • 46749119947 scopus 로고    scopus 로고
    • Homan E, Johansson L, Vallgarda J, Williams M, Bercot EA, Fotsch
    • CH, Li A, Cai G, Hungate RW, Yuan CC et al, Inhibitors of 11-β-hydroxy steroid dehydrogenase type 1. WO-2007061661 2007
    • AMGEN INC/BIOVITRUM AB (Henriksson M, Homan E, Johansson L, Vallgarda J, Williams M, Bercot EA, Fotsch CH, Li A, Cai G, Hungate RW, Yuan CC et al): Inhibitors of 11-β-hydroxy steroid dehydrogenase type 1. WO-2007061661 (2007).
  • 76
    • 46749100716 scopus 로고    scopus 로고
    • AMGEN INC (Bunel E, Guram A, Liu Q): Catalyzed process of making C-5-substituted heterocyclic inhibitors of 11β-hydroxy steroid dehydrogenase type 1. US-20070117985 (2007).
    • AMGEN INC (Bunel E, Guram A, Liu Q): Catalyzed process of making C-5-substituted heterocyclic inhibitors of 11β-hydroxy steroid dehydrogenase type 1. US-20070117985 (2007).
  • 77
    • 46749111614 scopus 로고    scopus 로고
    • HOFFMANN-LA ROCHE INC (Banner BL, Bilotta JA, Fotouhi N, Gillespie P, Goodnow RA Jr, Hamilton MM, Haynes NE, Kowalczyk A, Mayweg A, Myers MP, Pietranico-Cole SL et al): Pyrazolones as inhibitors of 11β-hydroxysteroid dehydrogenase. US-20070049632 (2007).
    • HOFFMANN-LA ROCHE INC (Banner BL, Bilotta JA, Fotouhi N, Gillespie P, Goodnow RA Jr, Hamilton MM, Haynes NE, Kowalczyk A, Mayweg A, Myers MP, Pietranico-Cole SL et al): Pyrazolones as inhibitors of 11β-hydroxysteroid dehydrogenase. US-20070049632 (2007).
  • 78
    • 46749096913 scopus 로고    scopus 로고
    • HOFFMANN-LA ROCHE INC (Amrein K, Hunziker D, Kuhn B, Mayweg AV, Neidhart W): New pyrazolones as 11β-HSD1 inhibitors for diabetes. US-20070049574 (2007).
    • HOFFMANN-LA ROCHE INC (Amrein K, Hunziker D, Kuhn B, Mayweg AV, Neidhart W): New pyrazolones as 11β-HSD1 inhibitors for diabetes. US-20070049574 (2007).
  • 79
    • 46749098065 scopus 로고    scopus 로고
    • ASTELLAS PHARMA INC (Murakami T, Kawano T, Shiraki R, Ishii H, Yoshimura S, Ohkawa T, Hosaka M, Fukudome H, Inoki Y): Triazole derivative or salt thereof. WO-2006030805 (2006).
    • ASTELLAS PHARMA INC (Murakami T, Kawano T, Shiraki R, Ishii H, Yoshimura S, Ohkawa T, Hosaka M, Fukudome H, Inoki Y): Triazole derivative or salt thereof. WO-2006030805 (2006).
  • 80
    • 46749091419 scopus 로고    scopus 로고
    • ASTELLAS PHARMA INC (Yoshimura S, Shiraki R, Kawano T, Susuga D, Hosaka M, Fukudome H, Kurosawa K, Ishii H, Koike T): Triazole derivative or salt thereof. WO-2007105753 (2007).
    • ASTELLAS PHARMA INC (Yoshimura S, Shiraki R, Kawano T, Susuga D, Hosaka M, Fukudome H, Kurosawa K, Ishii H, Koike T): Triazole derivative or salt thereof. WO-2007105753 (2007).
  • 81
    • 46749123226 scopus 로고    scopus 로고
    • BRISTOL-MYERS SQUIBB CO (Li J, Hamann LG, Wang H): Heteroaryl 11-β-hydroxysteroid dehydrogenase type 1 inhibitors. US-20060281750 (2006).
    • BRISTOL-MYERS SQUIBB CO (Li J, Hamann LG, Wang H): Heteroaryl 11-β-hydroxysteroid dehydrogenase type 1 inhibitors. US-20060281750 (2006).
  • 82
    • 46749127509 scopus 로고    scopus 로고
    • BRISTOL-MYERS SQUIBB CO (Li J, Robl JA, Kennedy LJ): Triazine 11-β hydroxysteroid dehydrogenase type 1 inhibitors. US-20070207985 (2007).
    • BRISTOL-MYERS SQUIBB CO (Li J, Robl JA, Kennedy LJ): Triazine 11-β hydroxysteroid dehydrogenase type 1 inhibitors. US-20070207985 (2007).
  • 83
    • 46749136555 scopus 로고    scopus 로고
    • BRISTOL-MYERS SQUIBB CO (Robl JA, Wu SC, Yoon DS): Pyridone/ hydroxypyridine 11-β hydroxysteroid dehydrogenase type 1 inhibitors. WO-2008005910 (2008).
    • BRISTOL-MYERS SQUIBB CO (Robl JA, Wu SC, Yoon DS): Pyridone/ hydroxypyridine 11-β hydroxysteroid dehydrogenase type 1 inhibitors. WO-2008005910 (2008).
  • 84
    • 46749138831 scopus 로고    scopus 로고
    • F HOFFMANN-LA ROCHE AG (Amrein K, Hunziker D, Kuhn B, Mayweg AV, Neidhart W): Pyridazine derivatives. WO-2007003521 (2007).
    • F HOFFMANN-LA ROCHE AG (Amrein K, Hunziker D, Kuhn B, Mayweg AV, Neidhart W): Pyridazine derivatives. WO-2007003521 (2007).
  • 85
    • 46749151926 scopus 로고    scopus 로고
    • F HOFFMANN-LA ROCHE AG (Amrein K, Hunziker D, Kuhn B, Mayweg AV, Neidhart W): Alkyl-pyridazine derivatives as inhibitors of 11-β hydroxysteroid dehydrogenase type 1 (11β-HSD 1). WO-2008003611 (2008).
    • F HOFFMANN-LA ROCHE AG (Amrein K, Hunziker D, Kuhn B, Mayweg AV, Neidhart W): Alkyl-pyridazine derivatives as inhibitors of 11-β hydroxysteroid dehydrogenase type 1 (11β-HSD 1). WO-2008003611 (2008).
  • 86
    • 46749122801 scopus 로고    scopus 로고
    • ELI LILLY AND CO (Aicher TD, Chicarelli MJ, Hinklin RJ, Tian H, Wallace OB): Cycloalkyl lactam derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2006068991 (2006).
    • ELI LILLY AND CO (Aicher TD, Chicarelli MJ, Hinklin RJ, Tian H, Wallace OB): Cycloalkyl lactam derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2006068991 (2006).
  • 87
    • 46749120364 scopus 로고    scopus 로고
    • ELI LILLY AND CO (Aicher TD, Chicarelli MJ, Gauthier CA, Hinklin RJ, Tian H, Wallace OB, Krasutsky AP, Allen JG): Cycloalkyl lactam derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2006068992 (2006).
    • ELI LILLY AND CO (Aicher TD, Chicarelli MJ, Gauthier CA, Hinklin RJ, Tian H, Wallace OB, Krasutsky AP, Allen JG): Cycloalkyl lactam derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2006068992 (2006).
  • 88
    • 46749150592 scopus 로고    scopus 로고
    • ELI LILLY AND CO (Aicher TD, Chen Z, Hinklin RJ, Hite GA, Krasutsky AP, Li R, McCowan JR, Saeed A, Snyder NJ, Toth JL, Wallace OB et al, Biphenyl amide lactam derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007124337 2007
    • ELI LILLY AND CO (Aicher TD, Chen Z, Hinklin RJ, Hite GA, Krasutsky AP, Li R, McCowan JR, Saeed A, Snyder NJ, Toth JL, Wallace OB et al): Biphenyl amide lactam derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007124337 (2007).
  • 89
    • 46749115271 scopus 로고    scopus 로고
    • ELI LILLY AND CO (Allen JG, Krasutsky AP, Wallace OB, Xu Y, York JS): Substituted pyrrolidinones as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007127693 (2007).
    • ELI LILLY AND CO (Allen JG, Krasutsky AP, Wallace OB, Xu Y, York JS): Substituted pyrrolidinones as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007127693 (2007).
  • 90
    • 46749111205 scopus 로고    scopus 로고
    • ELI LILLY AND CO (Li R, Wallace OB, Xu Y): Inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007127765 (2007).
    • ELI LILLY AND CO (Li R, Wallace OB, Xu Y): Inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007127765 (2007).
  • 91
    • 46749101846 scopus 로고    scopus 로고
    • ELI LILLY AND CO (Bush JK, Hansen MM, Li R, Mabry TE, Snyder NJ, Wallace OB, Xu Y): Inhibitors of 11-β- hydroxysteroid dehydrogenase 1. WO-2007127688 (2007).
    • ELI LILLY AND CO (Bush JK, Hansen MM, Li R, Mabry TE, Snyder NJ, Wallace OB, Xu Y): Inhibitors of 11-β- hydroxysteroid dehydrogenase 1. WO-2007127688 (2007).
  • 92
    • 46749083555 scopus 로고    scopus 로고
    • ELI LILLY AND CO (York JS, Wallace OB, Xu Y): Piperidinyl substituted pyrrolidinones as inhibitors of 11-β- hydroxysteroid dehydrogenase 1. WO-2007127901 (2007).
    • ELI LILLY AND CO (York JS, Wallace OB, Xu Y): Piperidinyl substituted pyrrolidinones as inhibitors of 11-β- hydroxysteroid dehydrogenase 1. WO-2007127901 (2007).
  • 93
    • 46749146661 scopus 로고    scopus 로고
    • ELI LILLY AND CO (Guenther RL, Mabry TE, Saeed A, Snyder NJ, Wallace OB, Xu Y): Cyclohexylimidazole lactam derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007124329 (2007).
    • ELI LILLY AND CO (Guenther RL, Mabry TE, Saeed A, Snyder NJ, Wallace OB, Xu Y): Cyclohexylimidazole lactam derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007124329 (2007).
  • 94
    • 46749119953 scopus 로고    scopus 로고
    • ELI LILLY AND CO (Aicher TD, Anzeveno PB, Li R, Krasutsky AP, Mabry TE, Saeed A, Snyder NJ, Stephenson GA, Tian H, Wallace OB, Winneroski LL Jr et al, Cyclohexylpyrazole lactam derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007124254 2007
    • ELI LILLY AND CO (Aicher TD, Anzeveno PB, Li R, Krasutsky AP, Mabry TE, Saeed A, Snyder NJ, Stephenson GA, Tian H, Wallace OB, Winneroski LL Jr et al): Cyclohexylpyrazole lactam derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007124254 (2007).
  • 95
    • 46749146918 scopus 로고    scopus 로고
    • ELI LILLY AND CO (Krasutsky AP, Snyder NJ, Wallace OB, Xu Y, York JS): Cyclohexyl substituted pyrrolidinones as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007127704 (2007).
    • ELI LILLY AND CO (Krasutsky AP, Snyder NJ, Wallace OB, Xu Y, York JS): Cyclohexyl substituted pyrrolidinones as inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007127704 (2007).
  • 96
    • 46749102639 scopus 로고    scopus 로고
    • ELI LILLY AND CO (Wallace OB, Li R, Mabry TE, Winneroski LL Jr, Xu Y): Inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007127726 (2007).
    • ELI LILLY AND CO (Wallace OB, Li R, Mabry TE, Winneroski LL Jr, Xu Y): Inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007127726 (2007).
  • 97
    • 46749137649 scopus 로고    scopus 로고
    • ELI LILLY AND CO (Winneroski LL Jr, Mabry TE, Snyder NJ, Wallace OB, Xu Y): Inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007127763 (2007).
    • ELI LILLY AND CO (Winneroski LL Jr, Mabry TE, Snyder NJ, Wallace OB, Xu Y): Inhibitors of 11-β-hydroxysteroid dehydrogenase 1. WO-2007127763 (2007).
  • 98
    • 46749155209 scopus 로고    scopus 로고
    • ABBOTT LABORATORIES (Yeh VS, Kurukulassuriya R, Madar DJ, Link JT): Inhibitors of the 11-β-hydroxysteroid dehydrogenase type 1 enzyme. WO-2007118185 (2007).
    • ABBOTT LABORATORIES (Yeh VS, Kurukulassuriya R, Madar DJ, Link JT): Inhibitors of the 11-β-hydroxysteroid dehydrogenase type 1 enzyme. WO-2007118185 (2007).
  • 99
    • 46749118536 scopus 로고    scopus 로고
    • TAKEDA PHARMACEUTICAL CO LTD (Cho N, Kasai S, Yamashita T): Prophylactic/therapeutic agent for diabetes. WO-2006104280 (2006).
    • TAKEDA PHARMACEUTICAL CO LTD (Cho N, Kasai S, Yamashita T): Prophylactic/therapeutic agent for diabetes. WO-2006104280 (2006).
  • 100
    • 46749085233 scopus 로고    scopus 로고
    • TAISHO PHARMACEUTICAL CO LTD (Fukushima H, Takahashi H, Mikami A, Tanaka H): Preparation of imidazolidinone derivatives as 11β-HSD1 inhibitors. JP-2007254409 (2007).
    • TAISHO PHARMACEUTICAL CO LTD (Fukushima H, Takahashi H, Mikami A, Tanaka H): Preparation of imidazolidinone derivatives as 11β-HSD1 inhibitors. JP-2007254409 (2007).
  • 101
    • 46749091815 scopus 로고    scopus 로고
    • SHIONOGI AND CO LTD (Ogawa T, Kurose N, Tanaka S, Nishi K): Heterocyclic compound having type I 11 β hydroxysteroid dehydrogenase inhibitory activity. WO-2006132197 (2006).
    • SHIONOGI AND CO LTD (Ogawa T, Kurose N, Tanaka S, Nishi K): Heterocyclic compound having type I 11 β hydroxysteroid dehydrogenase inhibitory activity. WO-2006132197 (2006).
  • 102
    • 46749098066 scopus 로고    scopus 로고
    • SHIONOGI AND CO LTD (Ogawa T, Chomei N, Masuda K, Tanaka S): Isoxazole derivative and isothiazole derivative having inhibitory activity on 11β-hydroxysteroid dehydrogenase type 1. WO-2007114124 (2007).
    • SHIONOGI AND CO LTD (Ogawa T, Chomei N, Masuda K, Tanaka S): Isoxazole derivative and isothiazole derivative having inhibitory activity on 11β-hydroxysteroid dehydrogenase type 1. WO-2007114124 (2007).
  • 103
    • 46749125898 scopus 로고    scopus 로고
    • SHIONOGI AND CO LTD (Kurose N, Hayashi M, Ogawa T, Masuda K, Kojima E): Heterocyclic compound having inhibitory activity on 11-β-hydroxysteroid dehydrogenase type 1. WO-2007058346 (2007).
    • SHIONOGI AND CO LTD (Kurose N, Hayashi M, Ogawa T, Masuda K, Kojima E): Heterocyclic compound having inhibitory activity on 11-β-hydroxysteroid dehydrogenase type 1. WO-2007058346 (2007).
  • 104
    • 46749141441 scopus 로고    scopus 로고
    • F HOFFMANN-LA ROCHE AG (Anderson KW, Fotouhi N, Gillespie P, Goodnow RA Jr, Guertin KR, Haynes NE, Myers MP, Pietranico-Cole SL, Qi L, Rossman PL, Scott NR et al, Pyrazoles as 11-β-HSD-1. WO-2007107470 2007
    • F HOFFMANN-LA ROCHE AG (Anderson KW, Fotouhi N, Gillespie P, Goodnow RA Jr, Guertin KR, Haynes NE, Myers MP, Pietranico-Cole SL, Qi L, Rossman PL, Scott NR et al): Pyrazoles as 11-β-HSD-1. WO-2007107470 (2007).
  • 105
    • 46749148130 scopus 로고    scopus 로고
    • PFIZER PRODUCTS INC (Cheng H, Cripps SJ, Lafontaine JA, Le PTQ, Matthews JJ, Nair SK): Sulfonyl derivatives. WO-2007057768 (2007).
    • PFIZER PRODUCTS INC (Cheng H, Cripps SJ, Lafontaine JA, Le PTQ, Matthews JJ, Nair SK): Sulfonyl derivatives. WO-2007057768 (2007).
  • 106
    • 46749121562 scopus 로고    scopus 로고
    • MERCK PATENT GMBH (Carniato D, Charon C, Gleitz J, Roche D, Hock B): 2-Adamantylurea derivatives as selective 11β-HSD1 inhibitors. WO-2007068330 (2007).
    • MERCK PATENT GMBH (Carniato D, Charon C, Gleitz J, Roche D, Hock B): 2-Adamantylurea derivatives as selective 11β-HSD1 inhibitors. WO-2007068330 (2007).
  • 107
    • 46749132438 scopus 로고    scopus 로고
    • VITAE PHARMACEUTICALS INC (Claremon DA, Singh SB, Tice CM, Ye Y, Cacatian S, He W, Simpson R, Xu Z, Zhao W): Inhibitors of 11β-hydroxysteroid dehydrogenase type 1. WO-2008024497 (2008).
    • VITAE PHARMACEUTICALS INC (Claremon DA, Singh SB, Tice CM, Ye Y, Cacatian S, He W, Simpson R, Xu Z, Zhao W): Inhibitors of 11β-hydroxysteroid dehydrogenase type 1. WO-2008024497 (2008).
  • 108
    • 46749122802 scopus 로고    scopus 로고
    • NOVO NORDISK A/S (Ebdrup S): Adamantane derivatives for the treatment of metabolic syndrome. WO-2007107550 (2007).
    • NOVO NORDISK A/S (Ebdrup S): Adamantane derivatives for the treatment of metabolic syndrome. WO-2007107550 (2007).
  • 109
    • 46749093084 scopus 로고    scopus 로고
    • BRISTOL-MYERS SQUIBB CO (Ye XY, Robl JA, Hanson RL, Guo Z, Patel RN): Cyclic 11-β hydroxysteroid dehydrogenase type 1 inhibitors. WO-2008024892 (2008).
    • BRISTOL-MYERS SQUIBB CO (Ye XY, Robl JA, Hanson RL, Guo Z, Patel RN): Cyclic 11-β hydroxysteroid dehydrogenase type 1 inhibitors. WO-2008024892 (2008).
  • 110
    • 46749104223 scopus 로고    scopus 로고
    • NOVO NORDISK A/S (Ebdrup S, Andersen HS): 4-Piperidylbenzamides as 11-β-hydroxysteroid dehydrogenase type 1 inhibitors. WO-2008006703 (2008).
    • NOVO NORDISK A/S (Ebdrup S, Andersen HS): 4-Piperidylbenzamides as 11-β-hydroxysteroid dehydrogenase type 1 inhibitors. WO-2008006703 (2008).
  • 111
    • 46749144693 scopus 로고    scopus 로고
    • NOVO NORDISK A/S (Ebdrup S, Andersen HS): 11β-hydroxysteroid dehydrogenase type 1 active compounds. WO-2008006702 (2008).
    • NOVO NORDISK A/S (Ebdrup S, Andersen HS): 11β-hydroxysteroid dehydrogenase type 1 active compounds. WO-2008006702 (2008).
  • 112
    • 46749124808 scopus 로고    scopus 로고
    • NOVO NORDISK A/S (Ebdrup S, Andersen HS): 11β-Hydroxysteroid dehydrogenase type 1 active compounds. WO-2007115935 (2007).
    • NOVO NORDISK A/S (Ebdrup S, Andersen HS): 11β-Hydroxysteroid dehydrogenase type 1 active compounds. WO-2007115935 (2007).
  • 113
    • 46749085634 scopus 로고    scopus 로고
    • HOFFMANN-LA ROCHE INC (Gillespie P, Goodnow RA Jr, Zhang Q): Pyrazoles. US-20060223852 (2006).
    • HOFFMANN-LA ROCHE INC (Gillespie P, Goodnow RA Jr, Zhang Q): Pyrazoles. US-20060223852 (2006).
  • 114
    • 46749107807 scopus 로고    scopus 로고
    • INCYTE CORP (Yao W, Xu M, Zhang C, Agrios K, Metcalf B, Zhuo J): Amido compounds and their use as pharmaceuticals. WO-2006002349 (2006).
    • INCYTE CORP (Yao W, Xu M, Zhang C, Agrios K, Metcalf B, Zhuo J): Amido compounds and their use as pharmaceuticals. WO-2006002349 (2006).
  • 115
    • 46749098730 scopus 로고    scopus 로고
    • INCYTE CORP (Zhuo J, Li YL, Xu M, He C, Yao W): Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same. US-20070208001 (2007).
    • INCYTE CORP (Zhuo J, Li YL, Xu M, He C, Yao W): Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same. US-20070208001 (2007).
  • 116
    • 46749150209 scopus 로고    scopus 로고
    • INCYTE CORP (Li YL, Yao W): Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same. WO-2007101270 (2007).
    • INCYTE CORP (Li YL, Yao W): Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same. WO-2007101270 (2007).
  • 117
    • 46749148543 scopus 로고    scopus 로고
    • INCYTE CORP (Li YL, Bostrom LL, Yao W): Tetrasubstituted ureas as modulators of 11-β hydroxyl steroid dehydrogenase type 1. WO-2007130898 (2007).
    • INCYTE CORP (Li YL, Bostrom LL, Yao W): Tetrasubstituted ureas as modulators of 11-β hydroxyl steroid dehydrogenase type 1. WO-2007130898 (2007).
  • 118
    • 46749084401 scopus 로고    scopus 로고
    • AMGEN INC/BIOVITRUM AB (Fotsch CH, Bartberger MD, Haraldsson M, St Jean D, Johansson L, Nilsson M, Sutin L): Substituted azole aromatic heterocycles as inhibitors of 11β-HSD-1. WO-2008011453 (2008).
    • AMGEN INC/BIOVITRUM AB (Fotsch CH, Bartberger MD, Haraldsson M, St Jean D, Johansson L, Nilsson M, Sutin L): Substituted azole aromatic heterocycles as inhibitors of 11β-HSD-1. WO-2008011453 (2008).
  • 119
    • 46749108596 scopus 로고    scopus 로고
    • SANOFI-AVENTIS (Braun A, Gussregen S, Mougenot P, Namane C, Nicolai E, Pacquet F, Philippo C, Venier O, Crespin O, Pascal C, Aletru M): Derivatives of ureas of piperidine or pyrrolidine, their preparation and their therapeutical use. WO-2008000950 (2008).
    • SANOFI-AVENTIS (Braun A, Gussregen S, Mougenot P, Namane C, Nicolai E, Pacquet F, Philippo C, Venier O, Crespin O, Pascal C, Aletru M): Derivatives of ureas of piperidine or pyrrolidine, their preparation and their therapeutical use. WO-2008000950 (2008).
  • 120
    • 46749127908 scopus 로고    scopus 로고
    • INCYTE CORP (Yao W, Xu M, Zhang C, Li Y, Zhuo J, Metcalf BW): N-Substituted piperidines and their use as pharmaceuticals. US-20060004049 (2006).
    • INCYTE CORP (Yao W, Xu M, Zhang C, Li Y, Zhuo J, Metcalf BW): N-Substituted piperidines and their use as pharmaceuticals. US-20060004049 (2006).
  • 121
    • 46749158033 scopus 로고    scopus 로고
    • HOFFMANN-LA ROCHE INC (Gillespie P, Goodnow RA Jr, Kowalczyk A, So SS, Zhang Q): Aryl sulfonyl piperidines. US-20060199816 (2006).
    • HOFFMANN-LA ROCHE INC (Gillespie P, Goodnow RA Jr, Kowalczyk A, So SS, Zhang Q): Aryl sulfonyl piperidines. US-20060199816 (2006).
  • 122
    • 46749108176 scopus 로고    scopus 로고
    • NOVO NORDISK A/S (Kilburn JP, Kampen GCT, Andersen HS): Pharmaceutical use of substituted piperidine carboxamides. WO-2007144394 (2007).
    • NOVO NORDISK A/S (Kilburn JP, Kampen GCT, Andersen HS): Pharmaceutical use of substituted piperidine carboxamides. WO-2007144394 (2007).
  • 123
    • 46749146266 scopus 로고    scopus 로고
    • ASTRAZENECA PLC (McCoull W, Packer M, Scott JS, Whittamore PRO): Chemical compounds 428. WO-2008012532 (2008).
    • ASTRAZENECA PLC (McCoull W, Packer M, Scott JS, Whittamore PRO): Chemical compounds 428. WO-2008012532 (2008).
  • 124
    • 46749143049 scopus 로고    scopus 로고
    • WYETH (Xiang JS, Saiah E, Tam SY, McKew JC, Chen L, Ipek M, Lee K, Li HQ, Li J, Li W, Mansour TS et al, 11-β HSD1 inhibitors. WO-2007092435 2007
    • WYETH (Xiang JS, Saiah E, Tam SY, McKew JC, Chen L, Ipek M, Lee K, Li HQ, Li J, Li W, Mansour TS et al): 11-β HSD1 inhibitors. WO-2007092435 (2007).
  • 125
    • 46749127510 scopus 로고    scopus 로고
    • TAKEDA SAN DIEGO INC (Aertgeerts K, Brennan NK, Cao SX, Chang E, Kiryanov AA, Liu Y): Hydroxysteroid dehydrogenase inhibitors. WO-2006105127 (2006).
    • TAKEDA SAN DIEGO INC (Aertgeerts K, Brennan NK, Cao SX, Chang E, Kiryanov AA, Liu Y): Hydroxysteroid dehydrogenase inhibitors. WO-2006105127 (2006).
  • 126
    • 46749150737 scopus 로고    scopus 로고
    • AMGEN INC (Powers JP, DeGraffenreid MR, He X, Julian L, McMinn DL, Sun D, Rew Y, Yan X): Benzamide derivatives and uses related thereto. WO-2006138508 (2006).
    • AMGEN INC (Powers JP, DeGraffenreid MR, He X, Julian L, McMinn DL, Sun D, Rew Y, Yan X): Benzamide derivatives and uses related thereto. WO-2006138508 (2006).
  • 127
    • 46749104629 scopus 로고    scopus 로고
    • AMGEN INC (Powers JP, Rew Y, Yan X): Benzamide derivatives and uses related thereto. WO-2007145834 (2007).
    • AMGEN INC (Powers JP, Rew Y, Yan X): Benzamide derivatives and uses related thereto. WO-2007145834 (2007).
  • 128
    • 46749114159 scopus 로고    scopus 로고
    • ASTRAZENECA AB (Caulkett PWR, McCoull W, Packer M, Whittamore PRO): 1,4-Disubstituted piperazine and 1,4-disubstituted azepane as 11-β-hydroxysteroid dehydrogenase 1 inhibitors. WO-2007135427 (2007).
    • ASTRAZENECA AB (Caulkett PWR, McCoull W, Packer M, Whittamore PRO): 1,4-Disubstituted piperazine and 1,4-disubstituted azepane as 11-β-hydroxysteroid dehydrogenase 1 inhibitors. WO-2007135427 (2007).
  • 129
    • 46749116569 scopus 로고    scopus 로고
    • ASTRAZENECA PLC (Caulkett PWR, McCoull W, Packer M, Whittamore PRO): Diazepan-1-yl-sulfonyl derivatives for the treatment of metabolic syndrome. WO-2007122411 (2007).
    • ASTRAZENECA PLC (Caulkett PWR, McCoull W, Packer M, Whittamore PRO): Diazepan-1-yl-sulfonyl derivatives for the treatment of metabolic syndrome. WO-2007122411 (2007).
  • 130
    • 46749101854 scopus 로고    scopus 로고
    • HOFFMANN-LA ROCHE INC (Amrein K, Hunziker D, Kuhn B, Mayweg A, Neidhart W): Pyridines. US-20060074237 (2006).
    • HOFFMANN-LA ROCHE INC (Amrein K, Hunziker D, Kuhn B, Mayweg A, Neidhart W): Pyridines. US-20060074237 (2006).
  • 131
    • 46749157076 scopus 로고    scopus 로고
    • AMGEN INC (Powers JP, He X, McMinn D, Rew Y): Aniline sulfonamide derivatives and their uses. US-20070021502 (2007).
    • AMGEN INC (Powers JP, He X, McMinn D, Rew Y): Aniline sulfonamide derivatives and their uses. US-20070021502 (2007).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.