000			06520cam a2200853Ma 4500
001			ocn797858047
003			OCoLC
005			20170612141628.0
006			m o d
007			cr cn|||||||||
008			110927s2012 nju ob 001 0 eng d
040			_aE7B _beng _epn _cE7B _dOCLCF _dEBLCP _dIDEBK _dN$T _dDG1 _dYDXCP _dUIU _dEUX _dRECBK _dU3G _dOCLCQ _dDEBBG
019			_a792684096 _a795813847 _a860795540 _a898985666
020			_a1118219708 _q(electronic bk.)
020			_a9781118219706 _q(electronic bk.)
020			_a9781118219683 _q(electronic bk.)
020			_a1118219686 _q(electronic bk.)
020			_a9781118219676 _q(electronic bk.)
020			_a1118219678 _q(electronic bk.)
020			_a0470601817
020			_a9780470601815
020			_z9780470601815
020			_z9781118219706
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029	1		_aDEBBG _bBV042794919
029	1		_aDKDLA _b820120-katalog:000599605
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035			_a(OCoLC)797858047 _z(OCoLC)792684096 _z(OCoLC)795813847 _z(OCoLC)860795540 _z(OCoLC)898985666
037			_a10.1002/9781118219683 _bWiley InterScience _nhttp://www3.interscience.wiley.com
050		4	_aRS403 _b.C37 2012eb
072		7	_aMED _x023000 _2bisacsh
072		7	_aMED _x058170 _2bisacsh
072		7	_aMED _x071000 _2bisacsh
072		7	_aMED _x072000 _2bisacsh
082	0	4	_a615.19 _223
049			_aMAIN
245	0	0	_aCase studies in modern drug discovery and development / _cedited by Xianhai Huang, Robert G. Aslanian.
260			_aHoboken, NJ : _bJohn Wiley & Sons, _c©2012.
300			_a1 online resource (xviii, 451 pages)
336			_atext _btxt _2rdacontent
337			_acomputer _bc _2rdamedia
338			_aonline resource _bcr _2rdacarrier
504			_aIncludes bibliographical references and index.
505	0		_aCASE STUDIES IN MODERN DRUG DISCOVERY AND DEVELOPMENT; CONTENTS; PREFACE; CONTRIBUTORS; CHAPTER 1: INTRODUCTION: DRUG DISCOVERY IN DIFFICULT TIMES; CHAPTER 2: DISCOVERY AND DEVELOPMENT OF THE DPP-4 INHIBITOR JANUVIA; (SITA-GLIPTIN); 2.1 Introduction; 2.2 DPP-4 Inhibition as a Therapy for Type 2 Diabetes: Identification of Key Determinants for Efficacy and Safety; 2.2.1 Incretin-Based Therapy for T2DM; 2.2.2 Biological Rationale: DPP-4 is a Key Regulator of Incretin Activity; 2.2.3 Injectable GLP-1 Mimetics for the Treatment of T2DM.
505	8		_a2.2.11 DPP-4 Inhibitor Selectivity as a Key Parameter for Drug Development2.3 Medicinal Chemistry Program; 2.3.1 Lead Generation Approaches; 2.3.2 Cyclohexyl Glycine a-Amino Acid Series of DPP-4 Inhibitors; 2.3.3 Improving Selectivity of the a-Amino Acid Series; 2.3.4 Identification and Optimization of the ß-Amino Acid Series; 2.4 Synthetic and Manufacturing Routes to Sitagliptin; 2.4.1 Medicinal Chemistry Route to Sitagliptin and Early Modifications; 2.4.2 An Asymmetric Hydrogenation Manufacturing Route to Sitagliptin.
505	8		_a2.2.4 DPP-4 Inhibition as Oral Incretin-Based Therapy for T2DM2.2.5 Investigation of DPP-4 Biology: Identification of Candidate Substrates; 2.2.6 Preclinical Toxicities of In-Licensed DPP-4 Inhibitors; 2.2.7 Correlation of Preclinical Toxicity with Off-Target Inhibition of Pro-Specific Dipeptidase Activity; 2.2.8 Identification of Pro-Specific Dipeptidases Differentially Inhibited by the Probiodrug Compounds; 2.2.9 A Highly Selective DPP-4 Inhibitor is Safe and Well Tolerated in Preclinical Species; 2.2.10 A Highly Selective DPP-4 Inhibitor Does Not Inhibit T-Cell Proliferation in vitro.
505	8		_a2.4.3 A "Greener" Manufacturing Route to Sitagliptin Employing Biocatalytic Transamination2.5 Drug Product Development; 2.5.1 Overview; 2.5.2 Composition Development; 2.5.3 Manufacturing Process Development; 2.6 Clinical Studies; 2.6.1 Preclinical PD Studies and Early Clinical Development of Sitagliptin; 2.6.2 Summary of Phase II/III Clinical Trials; 2.7 Summary; References; CHAPTER 3: OLMESARTAN MEDOXOMIL: AN ANGIOTENSIN II RECEPTOR BLOCKER; 3.1 Background; 3.1.1 Introduction; 3.1.2 Prototype of Orally Active ARBs; 3.2 The Discovery of Olmesartan Medoxomil (Benicar); 3.2.1 Lead Generation.
505	8		_a3.2.2 Lead Optimization3.3 Characteristics of Olmesartan; 3.4 Binding Sites of Omlersartan to the AT1 Receptor and Its Inverse Agonoist Activity; 3.4.1 Binding Sites of Olmesartan to the AT1 Receptor; 3.4.2 Inverse Agonist Activity of Olmesartan; 3.4.3 Molecular Model of the Interaction between Olmesartan and the AT1 Receptor; 3.5 Practical Preparation of Olmesartan Medoxomil; 3.6 Preclinical Studies; 3.6.1 AT1 Receptor Blocking Action; 3.6.2 Inhibition of Ang II-Induced Vascular Contraction; 3.6.3 Inhibition of the Pressor Response to Ang II; 3.6.4 Blood Pressure Lowering Effects.
520			_aLearn why some drug discovery and development efforts succeed ... and others failWritten by international experts in drug discovery and development, this book sets forth carefully researched and analyzed case studies of both successful and failed drug discovery and development efforts, enabling medicinal chemists and pharmaceutical scientists to learn from actual examples. Each case study focuses on a particular drug and therapeutic target, guiding readers through the drug discovery and development process, including drug design rationale, structure-activity relationships, pharmacology, drug.
650		0	_aDrugs _xDesign.
650		0	_aPharmaceutical chemistry.
650		4	_aMedical.
650		7	_aMEDICAL _xDrug Guides. _2bisacsh
650		7	_aMEDICAL _xNursing _xPharmacology. _2bisacsh
650		7	_aMEDICAL _xPharmacology. _2bisacsh
650		7	_aMEDICAL _xPharmacy. _2bisacsh
650		7	_aDrugs _xDesign. _2fast _0(OCoLC)fst00898790
650		7	_aPharmaceutical chemistry. _2fast _0(OCoLC)fst01060115
655		4	_aElectronic books.
700	1		_aHuang, Xianhai.
700	1		_aAslanian, Robert G.
776	0	8	_iPrint version: _tCase studies in modern drug discovery and development _z9780470601815
856	4	0	_uhttp://onlinelibrary.wiley.com/book/10.1002/9781118219683 _zWiley Online Library
938			_aEBL - Ebook Library _bEBLB _nEBL822083
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938			_aRecorded Books, LLC _bRECE _nrbeEB00063040
938			_aYBP Library Services _bYANK _n7613837
938			_aYBP Library Services _bYANK _n12671182
994			_a92 _bDG1
999			_c206002 _d206002