From HTS to Market: the Discovery and Development of Maraviroc, a CCR5 Antagonist for the Treatment of HIV - Accounts in Drug Discovery Case Studies in Medicinal Chemistry - page 188

O

N

O

N

N N N

N

O

N

N

N

N

N

S

N

N Cl

N N

Cl

O

Ono
mw = 420 : clogP = 4.3

Novartis
mw = 463 : clogP = 5.1

1 Pfizer
mw = 411 : clogP = 4.6

2 Pfizer
mw = 576 : clogP = 6.0

O

O

O

S

S

N

O

H

N

N

F

S
OO

O

Cl

N

N +

Cl

O

Merck
mw = 592 : clogP = 5.2

Takeda
mw = 452 : clogP = 4.1

Schering
mw = 601 : clogP = 5.6

Figure 9.2 Leads reportedly used to initiate CCR5 antagonist programs.