Al-awar RS, Ray JE, Schultz RM, Andis SL, Kennedy JH, Moore RE, Golakoti T, Subbaraju GV Corbett TH. A Convergent Approach to Cryptophycin 52 Analogues: Synthesis and Biological Evaluation of a Novel Series of Fragment A Epoxides and Chlorohydrins. J Med Chem 2003; 46:2985 - 3007

Andersen HS, Olsen OH, Iversen LF, S rensen ALP, Mortensen SB, Christensen MS, Branner S, Hansen TK, Lau JF, Jeppesen L, Moran EJ, et al. Discovery and SAR of a Novel Selective and Orally Bioavailable Nonpeptide Classical Competitive Inhibitor Class of Protein-Tyrosine Phosphatase 1B. J Med Chem 2002; 45:4443 - 4459

Ashwood VA, Field MJ, Horwell DC, Julien-Larose C, Lewthwaite RA, McCleary S, Pritchard MC, Raphy J, Singh L. Utilization of an Intramolecular Hydrogen Bond To Increase the CNS Penetration of an NK1 Receptor Antagonist. J Med Chem 2001; 44:2276-2285

Aungst BJ, Nguyen NH, Taylor NJ, Bindra DS. Formulation and Food Effects on the Oral Absorption of a Poorly Water Soluble, Highly Permeable Antiretroviral Agent. J Pharm Sci 2002; 91:1390-1395

Avdeef A. Physicochemical Profiling (Solubility, Permeability and Charge state). Curr Topics Med Chem 2001; 1:277-351

Clark DE. In Silico Prediction of Blood-Brain Barrier Permeation. Drug Discovery Today 2001; 8:927-933

Curatolo W. Physical Chemical Properties of Oral Drug Candidates in the Discovery and Exploratory Development Settings. Pharm Sci Tech Today 1998; 1: 387-393

Di L, Kerns EH. Profiling Drug-like Properties in Discovery Research. Curr Opinion in Chem Biology 2003; 7: 402-408

Di L, Kerns EH, Fan K, McConnell OJ, Carter G: High Throughput Artificial Membrane Permeability Assay for Blood-Brain Barrier. Eur J Med Chem 2003; 38:223-232

Dressman JB, Amidon GL, Reppas C, Shah VP. Dissolution Testing as a Prognostic Tool for Oral Drug Absorption: Immediate Release Dosage Forms. Pharm Res 1998; 15:11-22

Ettmayer P, Amidon GL, Clemant B. Testa B. Lessons Learned from Marketed and Investigational Prodrugs. J Med Chem 2004; 47:2393-2404

Fichert T, Yazdanian M, Proudfoot JR. A Structure-Permeability Study of Small Drug-like Molecules. Bioorg Med Chem Lett 2003; 13:719-722

Fray MJ, Bull DJ, Carr CL, Gautier ECL, Mowbray CE, Stobie A. Structure-Activity Relationships of 1,4-Dihydro-(1H,4H)-quinoxaline-2,3-diones as N-Methyl-D-aspartate (Glycine Site) Receptor Antagonists. 1. Heterocyclic Substituted 5-Alkyl Derivatives. J Med Chem 2001; 44:1951 - 1962

Goodwin JT, Conradi RA, Ho MFH, Burton PS. Physicochemical Determinants of Passive Membrane Permeability: Role of Solute Hydrogen-Bonding Potential and Volume. J Med Chem 2001; 44:3721-3729

Hwang KK, Martin NE, Jiang L, Zhu C. Permeation Prediction of M100240 Using the Parallel Artificial Membrane Permeability Assay. J Pharmacy Pharmaceutical Sci 2003; 6:315-320

IMS Health. Drug Monitor. (Accessed Jan. 2005)

Johnson KC, Swindell AC. Guidance in the Setting of Drug Particle Size Specifications to Minimize Variability in Absorption. Pharm Res 1996; 13:17951798

Jorgensen WL, Duffy EM. Prediction of Drug Solubility from Structure. Adv Drug Del Rev 2002; 54:355-366

Kansy M, Senner F, Gubernator K. Physicochemical High Throughput Screening: Parallel Artificial Membrane Permeation Assay in the Description of Passive Absorption Processes. J Med Chem 1998; 41:1007-1010

Kerns EH. High Throughput Physicochemical Profiling for Drug Discovery. J Pharm Sci 2001; 90:1838-1858.

Kerns EH, Di L. Pharmaceutical Profiling in Drug Discovery. Drug Discovery Today 2003; 8:316-323

Kerns EH, Di L, Petusky S, Farris M, Ley R, Jupp P. Combined application of parallel artificial membrane permeability assay and Caco-2 permeability assays in drug discovery. J Pharm Sci 2004, 93:1440-1453

Lee YC, Zocharski PD, Samas B. An Intravenous Formulation Decision Tree for Discovery Compound Formulation Development. Int J Pharm 2003; 253:111119

Liljebris C, Larsen SD, Ogg D, Palazuk BJ, Bleasdale JE. Investigation of Potential Bioisosteric Replacements for the Carboxyl Groups of Peptidomimetic Inhibitors of Protein Tyrosine Phosphatase 1B: Identification of a Tetrazole-Containing Inhibitor with Cellular Activity. J Med Chem 2002; 45: 1785 - 1798

Lipinski CA. Drug-like Properties and the Causes of Poor Solubility and Poor Permeability. J Pharm Tox Methods 2000; 44:235-249

Lobell M, Molnar L, Keserü GM. Recent Advances in the Prediction of Blood-Brain Partitioning from Molecular Structure. J Pharm Sci 2003; 92:360-370

Milbank JBJ, Tercel M, Atwell GJ, Wilson WR, Hogg A, Denny WA. Synthesis of 1-Substituted 3-(Chloromethyl)-6-aminoindoline (6-Amino-seco-CI) DNA Minor Groove Alkylating Agents and Structure-Activity Relationships for Their Cytotoxicity. J Med Chem 1999; 42:649 - 658

Panchagnula R, Thomas NS. Biopharmaceutics and Pharmacokinetics in Drug Research. Int J Pharm 2000; 201:131-150

Pardridge WM. Transport of Small Molecules Through the Blood-Brain Barrier: Biology and Methodology. Adv Drug Del Rev 1995; 15:5-36

Pardridge WM. Crossing the blood-brain barrier: are we getting it right? Drug Discovery Today 2001; 6:1-2

Smith DA. High-throughput Screening - Brain Versus Brawn. Ernst Schering

Research Foundation Workshop 2002; 37:203-212

Quan ML, Lam PYS, Han Q, Pinto DJP, He MY, Li R, Ellis CD, Clark CG, Teleha CA, Sun JH, et al. Discovery of 1-(3'-Aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide Hydrochloride (Razaxaban), a Highly Potent, Selective, and Orally Bioavailable Factor Xa Inhibitor. J Med Chem 2004; ASAP Article

Stella VJ, A Case for Prodrugs: Fosphenytoin. Adv Drug Del Rev 1996; 19:311-330

Sugano K, Hamada H, Machida M, Ushio H, Saitoh K, Terada K. Optimized Conditions of Bio-mimetic Artificial Membrane Permeability Assay. Int J Pharm 2001; 228:181-188

van de Waterbeemd H. The Fundamental Variables of the Biopharmaceutics Classification System (BCS): a Commentary. Eur J Pharm Sci 1998; 7:1-3

van de Waterbeemd H, Smith DA, Beaumont K, Walker DK. Property-Based Design: Optimization of Drug Absorption and Pharmacokinetics. J Med Chem 2001; 44:1313 - 1333

Wan SH, Pentikainen PJ, Azarnoff DL. Bioavailability of Aminosalicylic Acid and its Various Salts in Humans. III. Absorption from Tablets. J Pharm Sci 1974; 63:708-11

Ward PD, Tippin TK, Thakker DR. Enhancing Paracellular Permeability by Modulating Epithelial Tight Junctions. Pharm Sci Tech Today 2000; 3: 346-358

Wohnsland F, Faller B. High-Throughput Permeability pH Profile and High-Throughput Alkane/Water Log P with Artificial Membranes. J Med Chem 2001; 44:923-930

Yalkowsky SH, Banerjee S. Aqueous Solubility: Methods of Estimation for Organic Compounds. New York, NY: Marcel Dekker, Inc; 1992.

Zhu C, Jiang L, Chen TM, Hwang KK. A Comparative Study of Artificial Membrane Permeability Assay for High Throughput Profiling of Drug Absorption Potential. Eur J Med Chem 2002; 37: 399-407

Zimmerman JJ, Ferron GM, Lim HK, Parker V The Effect of a High-Fat Meal on the Oral Bioavailability of the Immunosuppressant Sirolimus (Rapamycin). J

Clin Pharmacol 1999; 39:1155-1161

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