- RESPIRATORY SYNCYTIAL VIRUS INHIBITORS
-
Compounds of Formula (I): (Formula I), wherein Z1 is NR1A, CHR1A or CR1BR1B; one of Z2 and Z3 is CH or CR1A', the other is N, CH or CR1A'; n is 0, 1 or 2; q is 0, 1 or 2; R1A, R1A', R1B, R2 and R3 are as defined herein, their use as inhibitors of RSV and related aspects.
- -
-
Page/Page column 31; 32
(2017/02/24)
-
- Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: Optimization of the 4-substituted piperidine
-
In our continuing effort to identify CGRP receptor antagonists for the acute treatment of migraine, we have undertaken a study to evaluate alternative 4-substituted piperidines to the lead dihydroquinazolinone 1. In this regard, we have identified the piperidinyl-azabenzimidazolone and phenylimidazolinone structures which, when incorporated into the benzodiazepine core, afford potent CGRP receptor antagonists (e.g., 18 and 29). These studies produced a potent analog (18) which overcomes the instability issues associated with the lead structure 1. A general pharmacophore for the 4-substituted piperidine component of these CGRP receptor antagonists is also presented.
- Burgey, Christopher S.,Stump, Craig A.,Nguyen, Diem N.,Deng, James Z.,Quigley, Amy G.,Norton, Beth R.,Bell, Ian M.,Mosser, Scott D.,Salvatore, Christopher A.,Rutledge, Ruth Z.,Kane, Stefanie A.,Koblan, Kenneth S.,Vacca, Joseph P.,Graham, Samuel L.,Williams, Theresa M.
-
p. 5052 - 5056
(2007/10/03)
-
- Dipeptides which promote release of growth hormone
-
Compounds of formula (I) are growth hormone releasing peptide mimetics which are useful for the treatment and prevention of osteoporosis. STR1
- -
-
-