Lead generation: Sowing the seeds for future success

被引：10

作者：

Bleicher, KH ^{[1
]}

Nettekoven, M ^{[1
]}

Peters, JU ^{[1
]}

Wyler, R ^{[1
]}

机构：

[1] F Hoffmann La Roche Ltd, Div Pharmaceut, Lead Generat, CH-4070 Basel, Switzerland

来源：

CHIMIA | 2004年 / 58卷 / 09期

关键词：

lead generation; lead series; parallel synthesis; privileged structures; targeted libraries;

D O I：

10.2533/000942904777677542

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Lead generation and the associated hit-to-lead process are key strategic elements in modern pharmaceutical research, and most companies have implemented this concept. Efficient lead generation is one of the main attempts to reduce the high attrition rates observed along the drug discovery process by focussing on the early developmental phases. The level of integration of the lead generation activities within the discovery organization, the flexibility in assessing and implementing new chemistries and new technologies, the high-quality standards set for the identification of the best possible chemical lead series will ultimately determine the future success in discovering new medicines.

引用

页码：588 / 600

页数：13

共 92 条

[1] REACTIONS WITH ALPHA-SUBSTITUTED CINNAMONITRILES - A NOVEL SYNTHESIS OF ARYLPYRIMIDINES
ABDELFATTAH, AM
HUSSAIN, SM
ELREEDY, AM
YOUSIF, NM
[J]. TETRAHEDRON, 1983, 39 (19) : 3197 - 3199
[2] The contribution of combinatorial chemistry to lead generation: An interim analysis
Adang, AEP
Hermkens, PHH
[J]. CURRENT MEDICINAL CHEMISTRY, 2001, 8 (09) : 985 - 998
[3] AGARWAL KC, 1999, PLATELET PHYSL PHARM, P102
[4] Alanine A, 2003, COMB CHEM HIGH T SCR, V6, P51
[5] ARNDT KE, 2002, Patent No. 0238572
[6] BAXTER A.D., 2001, Drug Discovery World, V2, P9
[7] Ligand identification for G-protein-coupled receptors: a lead generation perspective
Bleicher, KH
Green, LG
Martin, RE
Rogers-Evans, M
[J]. CURRENT OPINION IN CHEMICAL BIOLOGY, 2004, 8 (03) : 287 - 296
[8] Parallel solution- and solid-phase synthesis of spiropyrrolo-pyrroles as novel neurokinin receptor ligands
Bleicher, KH
Wüthrich, Y
Adam, G
Hoffmann, T
Sleight, AJ
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (21) : 3073 - 3076
[9] Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands
Bleicher, KH
Wüthrich, Y
De Boni, M
Kolczewski, S
Hoffmann, T
Sleight, AJ
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (18) : 2519 - 2522
[10] Chemogenomics: Bridging a drug discovery gap
Bleicher, KH
[J]. CURRENT MEDICINAL CHEMISTRY, 2002, 9 (23) : 2077 - 2084

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