Cholesteryl ester transfer protein inhibitors as high-density lipoprotein raising agents

Expert Opinion on Therapeutic Patents

Volumn 19, Issue 9, 2009, Pages 1229-1237

  Shinkai, Hisashi ^a  

^a JT Inc   (Japan)

Author keywords

Anacetrapib; Cholesteryl ester transfer protein; Coronary heart disease; Dalcetrapib; High density lipoprotein; Torcetrapib

Indexed keywords

2 METHYLPROPANETHIOIC ACID S [2 [1 (2 ETHYLBUTYL)CYCLOHEXYLCARBOXAMIDO]PHENYL] ESTER; ANACETRAPIB; ATORVASTATIN; CHOLESTEROL ESTER TRANSFER PROTEIN INHIBITOR; HIGH DENSITY LIPOPROTEIN; PLACEBO; PRAVASTATIN; TORCETRAPIB;

ATHEROSCLEROSIS; BICARBONATE BLOOD LEVEL; CARDIOVASCULAR DISEASE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; DOSE RESPONSE; DRUG ACTIVITY; DRUG EFFICACY; DRUG SAFETY; DRUG STRUCTURE; DRUG TOLERABILITY; HUMAN; IC 50; NONHUMAN; POTASSIUM BLOOD LEVEL; RANDOMIZED CONTROLLED TRIAL; REVIEW; SIDE EFFECT; SODIUM BLOOD LEVEL; SYSTOLIC BLOOD PRESSURE;

ANIMALS; ANTICHOLESTEREMIC AGENTS; ATHEROSCLEROSIS; CHOLESTEROL ESTER TRANSFER PROTEINS; CHOLESTEROL, HDL; CLINICAL TRIALS, PHASE III AS TOPIC; HUMANS; OXAZOLIDINONES; PATENTS AS TOPIC; QUINOLINES; SULFHYDRYL COMPOUNDS;

EID: 69949135636     PISSN: 13543776     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543770903198451     Document Type: Review

References (76)

1. Bays H, Stein EA. Pharmacotheraphy for dyslipidemia-current therapies and future agents. Expert Opin Pharmacother 2003;4:1901-1938 (Pubitemid 37408104)
2. Gordon T, Castelli WP, Hjortland MC, et al. High density lipoprotein as a protective factor against coronary heart disease. The Framingham study. Am J Med 1977;62:707-714 (Pubitemid 8110784)
3. Gordon DJ, Rifkind BM. High-density lipoprotein - the clinical implications of recent studies. N Engl J Med 1989;321:1311-1316 (Pubitemid 19267219)
4. Gordon DJ, Probstfield JL, Garrison RL, et al. High density lipoprotein cholesterol and cardiovascular disease. Four prospective American studies. Circulation 1989;79:8-15
5. Boden WE. High-density lipoprotein cholesterol as an independent risk factor in cardiovascular disease: assessing the data from Framingham to the Veterans Affairs high-density lipoprotein intervention trial. Am J Cardiol 2000;86:19L-22L
6. Tall AR. Plasma cholesteryl ester transfer protein. J Lipid Res 1993;34:1255-1274
7. Barter PJ, Brewer HBJ, Chapman MJ, et al. Cholesteryl ester transfer protein: a novel target for raising HDL and inhibiting atherosclerosis. Thromb Vasc Biol 2003;23:160-167
8. De Grooth GJ, Kuivenhoven JA, Stalenhoef AF, et al. Efficacy and safety of a novel cholesteryl ester transfer protein inhibitor, JTT-705, in humans: a randomized phase II dose-response study. Circulation 2002;105:2159-2165
9. Kuivenhoven JA, De Grooth GJ, Kawamura H, et al. Effectiveness of inhibition of cholesteryl ester transfer protein by JTT-705 in combination with pravastatin in type II dyslipidemia. Am J Cardiol 2005;95:1085-1088 (Pubitemid 40544314)
10. Brousseau ME, Schaefer EJ, Wolfe ML, et al. Effects of an inhibitor of cholesteryl ester transfer protein on HDL cholesterol. N Engl J Med 2004;350:1505-1515 (Pubitemid 38477775)
11. Sikorski JA. Cholesteryl ester transfer protein inhibitors as potential new therapies for coronary artery disease. Expert Opin Ther Patents 2006;16:753-772 (Pubitemid 43958353)
12. Sikorski JA. Oral cholesteryl ester transfer inhibitors: a potential new approach for treating coronary artery disease. J Med Chem 2006;49:1-22 (Pubitemid 43077315)
13. Shinkai H, Maeda K, Yamasaki T, et al. Bis(2-(acylamino)phenyl) disufides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. J Med Chem 2000;43:3566-3572 (Pubitemid 30736710)
14. Okamoto H, Yonemori F, Wakitani K, et al. A cholesteryl ester transfer protein inhibitor attenuates atherosclerosis in rabbits. Nature 2000;406:203-207 (Pubitemid 30469005)
15. Japan Tobacco, Inc. CETP activity inhibitors for use in the treatment of hyperlipidemia and atherosclerosis. WO09835937; 1998
16. Qiu X, Mistry A, Ammirati MJ, et al. Crystal structure of cholestery ester transfer protein reveals a long tunnel and four bound lipid molecules. Nat Struct Mol Biol 2007;14:106-113 (Pubitemid 46245810)
17. Pfizer Products, Inc. Novel 4-carboxyamino-2-methyl- 1,2,3,4- tetrahydroquinolines as CETP inhibitors. EP00987251; 2000
18. Pfizer Products, Inc. Novel 4-carboxyamino-2-substituted- 1,2,3,4-tetrahydroquinolines as CETP inhibitors. WO00017164; 2000
19. Pfizer Products, Inc. Novel 4-amino-substituted-2-substituted- 1,2,3,4-tetrahydroquinolines as CETP inhibitors. WO00017165; 2000
20. Pfizer Products, Inc. Novel 4-carboxyamino-2-methyl- 1,2,3,4- tetrahydroquinolines as CETP inhibitors. WO00017166; 2000
21. Pfizer Products, Inc. Novel annulated 4-carboxyamino-2-methyl- 1,2,3,4-tetrahydroquinolines useful as CETP inhibitors. EP00992496; 2000
22. Pfizer Products, Inc. New N-(3,5-bis-trifluoromethyl-benzyl)- N-(6-trifluoromethyl-1,2,3,4-tetrahydroquinolin- 4-yl)-amine derivatives are CETP inhibitors - useful for the treatment of atherosclerosis. WO2005033082; 2005
23. Morehouse LA, Sugarman ED, Bourassa PA, et al. Inhibition of CETP activity by torcetrapib reduces susceptibility to diet-induced atherosclerosis in New Zealand Whikte rabbits. J Lipd Res 2007;48:1267-1272
24. Japan Tobacco, Inc. CETP inhibitors useful in the treatment of arteriosclerosis and hyperlipidemia. JP2003221376; 2003
25. Japan Tobacco, Inc. Dibenzylamine compound and medicinal use thereof. WO2004020393; 2004
26. Eli Lilly & Co. New fused hexahydro-1H-azepine and octahydroazocine derivatives are CETP modulators - useful for the treatment of lipid metabolism disorders. WO2005097805; 2005
27. Merck & Co, Inc. New N,N-dibenzylamine derivatives are inhibitors of cholesterol ester transfer protein - useful for the treatment of atherosclerosis. WO2005100298; 2005
28. Merck & Co, Inc. New substituted phenyl derivatives are CETP inhibitors - useful for the prevention and treatment of atherosclerosis. WO2007041494; 2007
29. Merck & Co, Inc. New substituted biphenyl compounds are CETP inhibitors - useful for the prevention and treatment of atherosclerosis. WO2007047591; 2007
30. Merck & Co, Inc. New azole derivatives are CETP inhibitors - useful for the treatment of atherosclerosis. WO2006014357; 2006
31. Merck & Co, Inc. New oxazolidinone and related heterocyclic derivatives are CETP inhibitors - useful for the treatment of atherosclerosis. WO2007079186; 2007
32. Merck & Co, Inc. New substituted heterocyclic compounds are CETP inhibitors - useful for raising HDL-C, lowering LDL-C and for the treatment of atherosclerosis. WO2007081570; 2007
33. Merck & Co, Inc. New substituted cyclic compounds are CETP inhibitors - useful for raising HDL-C, lowering LDL-C and the treatment of atherosclerosis. WO2007081571; 2007
34. Vergeer M, Kastelein JJP. Anacetrapib: new hope for cholesteryl ester transfer protein inhibitors in the treatment of dyslipidemia. Nat Clin Pract Cardiovasc Med 2008;5:302-303
35. Tanabe Seiyaku Co. Ltd. New tetrahydroquinoline derivatives are CETP inhibitors - useful for treating e.g. cardiovascular diseases, diabetes and obesity. WO2005095409; 2005
36. Tanabe Seiyaku Co. Ltd. New tetrahydronaphthyridine derivatives are CETP inhibitors - useful for treating e.g. cardiovascular diseases, diabetes and obesity. WO2005095395; 2005
37. Tanabe Seiyaku Co. Ltd. New trisubstituted amine derivatives are CETP inhibitors - useful for the treatment of arteriosclerotic diseases, hyperlipidemia or dyslipidemia. WO2007088996; 2007
38. Tanabe Seiyaku Co. Ltd. New trisubstituted amine derivatives are CETP inhibitors - useful for the treatment of arteriosclerotic diseases, hyperlipidemia or dyslipidemia. WO2007088999; 2007
39. Array BioPharma, Inc. New substituted dihydroquinoline compounds are cholesterol ester transfer protein inhibitors - useful for the treatment of e.g. atherosclerosis, coronary artery disease, hypertension, diabetes mellitus and inflammation. US20060270675; 2006
40. Reddy US Therapeutics, Inc. New benzylamine derivatives are CETP inhibitors - useful for the treatment of lipoprotein metabolism disorders. WO2006073973; 2006
41. Novartis AG. New pyridinyl amine derivatives are CETP inhibitors - useful for the treatment of eg hyperlipidemia, atherosclerosis, coronary heart disease, stroke and diabetes type II. WO2007073934; 2007
42. Novartis AG. New bicyclic derivatives are CETP inhibitors - useful for the treatment of eg hyperlipidemia and atherosclerosis. WO2007128568; 2007
43. Novartis AG. New benzylamine derivatives are CETP inhibitors - useful for the treatment of eg dyslipidemia, cardiovascular disease, stroke, diabetes and obesity. WO2007132906; 2007
44. Novartis AG. New amino-piperidine derivatives are CETP inhibitors - useful for the treatment of eg atherosclerosis, dyslipidemia, stroke, reperfusion injury, hypertension, diabetes type II and obesity. WO2008009435; 2008
45. Novartis AG. New pyridine and pyrazine derivatives are CETP inhibitors - useful for the treatment of eg lipid metabolism disorders, cardiovascular disease, stroke, diabetes and obesity. WO2008058961; 2008
46. Novartis AG. New pyridine and pyrazine derivatives are CETP inhibitors - useful for the treatment of eg lipid metabolism disorders, cardiovascular disease, stroke, diabetes and obesity. WO2008058967; 2008
47. Kowa Co. Ltd. New 2-(benzyl(pyridylmethyl)amino)pyrimidine compounds are cholesterol ester transfer protein inhibitors - for treating and preventing e.g. hyperlipidemia, arteriosclerois and peripheral vascular disease. WO2008018529; 2008
48. Kowa Co. Ltd. New pyrimidine compounds are cholesterol ester transfer protein inhibitors - useful for treating and preventing hyperlipidemia, arterosclerosis, peripheral vascular disease, cardiovascular disorders, angina pectoris, ischemia, myocardial ischemia, thrombosis, reperfusion disorders, and hypertension. WO2008111604; 2008
49. Kowa Co. Ltd. New pyrimidine compounds are cholesterol ester transfer protein inhibitors - useful for treating and preventing hyperlipidemia, arterosclerosis, peripheral vascular disease, cardiovascular disorders, angina pectoris, ischemia, myocardial ischemia, thrombosis, reperfusion disorders, and hypertension. WO2008129951; 2008
50. Davidson MH, McKenney JM, Shear CL, et al. Efficacy and safety of torcetrapib, a novel cholesterol ester transfer protein inhibitor, in individuals with below-average high-density lipoprotein cholesterol levels. J Am Coll Cardiol 2006;48:1774-1781 (Pubitemid 44648633)
51. McKenney JM, Davidson MH, Shear CL, et al. Efficacy and safety of torcetrapib, a novel cholesterol ester transfer protein inhibitor, in individuals with below-average high-density lipoprotein cholesterol levels on a background of atrovastatin. J AM Coll Cardiol 2006;48:1782-1790 (Pubitemid 44648632)
52. Barter PJ, Caulfield M, Eriksson M, et al. Effects of torcetrapib in patients at high risk for coronary events. N Engl J Med 2007;357:2109-2122 (Pubitemid 350146106)
53. Vergeer M, Bots ML, van Leuven SI, et al. Cholesteryl ester transfer protein inhibitor torcetrapib and off-target toxicity. A pooled analysis of the rating atherosclerotic disease change by imaging with a new CETP inhibitor (RADIANCE) trials. Circulation 2008;118:2515-2522
54. Kastelein JJ, van Leuven SI, Burgess L, et al. RADIANCE 2 investigators. Effect of torcetrapib on carotid atherosclerosis in familial hypercholesterolemia. N Engl J Med 2007;356:1620-1630 (Pubitemid 46631671)
55. Bots ML, Visseren FL, Evans GW, et al. RADIANCE 2 investigators. Torcetrapib and carotid intima-media thickness in mixed dyslipidaemia (RADIANCE 2 study): a randomised, double-blind trial. Lancet 2007;370:153-160
56. Kastelein JJ, van Leuven SI, Evans GW, et al. Design of RADIANCE 1 and 2: carotid ultrasound studies comparing the effects of torcetrapib/atorvastatin with atorvastatin alone on atherosclerosis. Curr Med Res Opin 2007;23:885-894
57. Nicholls SJ, Tuzcu EM, Brennan DM, et al. Cholesteryl ester transfer protein inhibition, high-density lipoprotein raising, and progression of coronary atherosclerosis. Insight from ILLUSTRATE (investigation of lipid level management using coronary ultrasound to assess reduction of atherosclerosis by CETP inhibition and HDL elevation). Circulation 2008;118:2506-2514
58. Nissen SE, Tardif JC, Nicholls SJ, et al. Effect of torcetrapib on the progression of coronary atherosclerosis. N Engl J Med 2007;356:1304-1316 (Pubitemid 46513296)
59. Forrest MJ, Bloomfield D, Briscoe RJ, et al. Torcetrapib-induced blood pressure elevation is independent of CETP inhibition and is accompanied by increased circulating levels of aldosterone. Br J Pharmacol 2008;154:1465-1473
60. Monsanto Co. Substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamines useful for inhibiting cholesteryl ester transfer protein activity. WO00018721; 2000
61. Monsanto Co. Substituted N-aliphatic- N-aromatic tertiary- heteroalkylamines useful for inhibiting cholesteryl ester transfer protein activity. WO00018723; 2000
62. Takeda Pharmaceutical Co. Ltd. Novel aminoethanol derivatives useful for the treatment of hyperlipidemia. WO02059077; 2002
63. Pfizer Products, Inc. New substituted 1,1,1-trifluoro-3-[(benzyl) (pyrimidin-2-yl) amino]propan-2-ol derivatives - useful for the treatment of cardiovascular and lipid metabolism disorders. WO2006090250; 2006
64. Bristol-Myers Squibb Co. New tertiary amine and related derivatives are CETP inhibitors - useful for the treatment of eg atherosclerosis, obesity and lipid metabolism disorders. WO2007062342; 2007
65. Bristol-Myers Squibb Co. New tertiary amine and related derivatives are CETP inhibitors - useful for the treatment of eg atherosclerosis, obesity and lipid metabolism disorders. WO2007062314; 2007
66. Bristol-Myers Squibb Co. New 1,1-diphenyl-methylamine and related derivatives are CETP inhibitors - useful for the treatment of eg atherosclerosis, obesity and lipid metabolism disorders. WO2007062308; 2007
67. F Hoffmann-La Roche Ltd. New indole, indazole and indoline derivatives are cholesteryl ester transfer protein inhibitors - useful for the treatment of cardiovascular and lipid metabolism disorders. WO2006013048; 2006
68. F Hoffmann-La Roche Ltd. New anthranilamide and 2-aminoheteroarene carboxamide derivatives are cholesteryl ester transfer protein inhibitors - useful for the treatment of eg lipid metabolism disorders, atherosclerosis and cardiovascular disease. WO2007090752; 2007
69. Merck & Co, Inc. New heterocyclic derivatives are CETP inhibitors - useful for the treatment of atherosclerosis. WO2007070173; 2007
70. Merck & Co, Inc. Novel benzoxazole arylamide compounds are CETP inhibitors - useful for the treatment of atherosclerosis. WO2008156715; 2008
71. Merck & Co, Inc. Novel benzoxazole arylamide compounds are CETP inhibitors - useful for the treatment of atherosclerosis. WO2008156718; 2008
72. Merck & Co, Inc. Novel benzoxazole arylamide compounds are CETP inhibitors - useful for the treatment of atherosclerosis. WO2008156717; 2008
73. Bayer HealthCare AG. New chromanol derivatives are CETP inhibitors - useful for the treatment of eg coronary heart disease, dyslipidemia, arteriosclerosis, restenosis, obesity, diabetes, metabolic syndrome, stroke and Alzheimer's disease. WO2007107243; 2007
74. Joy TR, Hegele RA. Commentary. The failure of torcetrapib: what have we learned? Br J Pharmacol 2008;154:1379-1381
75. Farrell B, Godwin J, Richards S. The United Kingdom transient ischaemic attack (UK-TIA) aspirin trial: final results. J Neurol Neurosurg Psychiatry 1991;54:1044-1054
76. Lewington S, Clarke R, Qizilbash N. Age-specific relevance of usual blood pressure to vascular mortality: a meta-analysis of individual data for one million adults in 61 prospective studies. Lancet 2002;360:1903-1913 (Pubitemid 35472129)