By Janos Fischer, C. Robin Ganellin, David P. Rotella

ISBN-10: 3527312579

ISBN-13: 9783527312573

ISBN-10: 3527607498

ISBN-13: 9783527607495

The 1st authoritative review of previous and present ideas for profitable drug improvement through analog iteration, this detailed source spans all very important drug sessions and all significant healing fields, together with histamine antagonists, ACE inhibitors, beta blockers, opioids, quinolone antibiotics, steroids and anticancer platinum compounds.Of the nineteen analog sessions provided intimately, nine are defined through the scientists who discoverd them.The e-book encompasses a desk of the main winning drug analogs as in accordance with the IMS rating and compares them when it comes to chemical constitution, mode of motion and patentability.

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Design, synthesis and structure–activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors. J. Med. , 2001, 44, 2707–2718. Gully D, Roger P, Valette G, Wermuth CG, Courtemanche G, Gauthier C. Dérivés alkylamino ramifiés du thiazole, leurs procédés de préparation et les compositions pharmaceutiques qui les contiennent, Elf-Sanofi: French Demande No. 9207736, 24 June, 1992. 42 Gully D, Roger P, Wermuth CG. 4-Phe- 43 44 45 46 47 48 nyl-aminothiazole derivatives, method for preparing same and pharmaceutical compositions containing said derivatives, Sanofi: World Patent, 09 January, 1997.

3 Analogue Design as a Means of Discovering New Drugs . of well-known drug molecules. For these drugs, bioavailability and toxicity studies have already been performed, and they have proven usefulness in human therapy. Once a hit is observed with a given drug molecule, the task is then to prepare analogues of this molecule in order to transform the observed “side activity” into the main effect and to strongly reduce or abolish the initial pharmacological activity. 2 Rationale The rationale behind the SOSA approach lies in the fact that, in addition to their main activity, almost all drugs used in human therapy show one or several side effects.

35 Murugesan N, Gu Z, Spergel S, Young M, Chen P, Mathur A, Leith L, Hermsmeier M, Liu EC-K, Zhang R, Bird E, Waldron T, Marino A, Koplowitz B, Humphreys WG, Chong S, Morrison RA, Webb ML, Moreland S, Trippodo N, Barrish JC. Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[(4,5-dimethyl3-isoxazolyl)amino]sulfonyl]-4-(2-oxazo- References 36 37 38 39 40 41 lyl)[1,1′-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940, a highly potent and orally active ETA selective antagonist.

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Analogue-based Drug Discovery by Janos Fischer, C. Robin Ganellin, David P. Rotella

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