TECHNICAL PROGRAM - American Chemical Society Publications

MEDI TECHNICAL PROGRAM
2:00 281. Combination strategies to treat
obesity: Overview of peripheral and central
pathways modulating energy homeostasis.
M. A. Pelleymounter
2:30 282. Discovery of Lorcaserin: A selective
5-HT 2C receptor agonist for the treatment
of obesity. B. M. Smith
3:00 283. MCH R1 antagonists: Problems
and solutions. D. L. Hertzog,
K. A. Al-Barazanji, K. K. Barvian,
E. Bigham, M. J. Bishop, C. S. Britt,
D. L. Carlton, A. J. Carpenter,
J. P. Cooper, D. M. Garrido, A. S. Goetz,
G. M. Green, M. K. Grizzle, Y. C. Guo,
A. L. Handlon, C. E. Hyman, D. M. Ignar,
D. G. Lang, R. O. Morgan, A. J. Peat,
G. E. Peckham, A. J. Reisinger,
J. D. Speake, W. R. Swain, F. X. Tavares,
H. Zhou
3:30 284. Discovery of S-2367 (velneperit): A
potent and selective NPY Y5 antagonist
for the treatment of obesity. T. Okuno,
H. Takenaka, Y. Aoyama, Y. Kanda,
Y. Yoshida, T. Okada, H. Hashizume,
M. Sakagami, T. Nakatani, K. Hattori,
T. Ichihashi, T. Yoshikawa, H. Yukioka,
K. Hanasaki, Y. Kawanishi
4:00 285. Anti-obesity potential of SGLT2
inhibitors in development for treatment of
diabetes. W. N. Washburn
4:30 286. Discovery of pramilitide and peptide
approaches to treating obesity.
S. S. Ghosh
Section A
Boston Convention & Exhibition Center
Ballroom West
General Oral Session Financially supported
by Gilead Sciences, Inc.
J. Zablocki, Organizer, Presiding
2:05 287. Isoquinucline-based GlyT1 inhibitors
for schizophrenia: Discovery, optimization,
synthesis, and in vivo pharmacology.
J. S. Albert, C. Alhambra, D. Brott,
T. Brugel, M. Chopra, G. E. Ernst,
J. Forst, F. Gharahdaghi, D. Gryte,
A. Gupta, C. Holmquist, J. Jonak,
G. Koether, J. Liu, J. Milano, T. E. Norris,
W. M. Potts, G. Smaggin, D. Song,
S. Sydserff, M. Sylvester, G. Tian,
J. G. Varnes, C. A. Veale, X. Wang,
D. Widzowski, D. Wilkins, M. Wood,
H. Xiong, S. Zukin
2:35 288. From fragment-based lead generation
to 2-aminoquinolines as potent beta-secretase
inhibitors that are efficacious
in vivo. Y. Cheng, K. Ashton,
M. Bartberger, J. Brown, C. Bryan,
K. Chen, J. Esmay, R. T. Fremeau Jr.,
J. Golden, S. Harried, D. Hickman,
S. A. Hitchcock, M. Huang, B. Jordan,
T. Judd, P. Lopez, S. W. Louie, Y. Luo,
S. Mercede, K. Michelsen, T. Nixey,
N. A. Paras, S. Poon, T. S. Powers,
A. Sickmier, D. St. Jean, C. Tegley,
W. Zhong, P. Wen, R. C. Wahl, S. Wood,
M. Xue, B. Yang
3:05 289. From discovery to clinic:
GSK962040, the first oral, small molecule
motilin receptor agonist for treatment of
conditions associated with impaired gastric
motility. S. M. Westaway,
G. J. Sanger, G. Dukes
3:35 290. Discovery of BMS-582949, a clinical
p38a MAP kinase inhibitor for the
treatment of inflammatory diseases.
C. Liu, J. Lin, S. T. Wrobleski, S. Lin,
J. Hynes, Jr., H. Wu, A. J. Dyckman, T. Li,
J. Wityak, K. M. Gillooly, S. Pitt, D. Shen,
R. F. Zhang, K. W. McIntyre,
L. Salter-Cid, D. J. Shuster, H. Zhang,
P. H. Marathe, A. M. Doweyko,
J. S. Sack, L. Gao, J. Wang, R. R. Latek,
U. Thienel, S. Kaul, M. McKinnon,
J. H. Dodd, J. C. Barrish, G. L. Schieven,
K. Leftheris
78–TECH
‡ Cooperative Cosponsorship
4:05 291. Development of an oxazolobenzimidazole
class of positive allosteric
modulators of mGluR2 for the treatment
of schizophrenia. R. M. Garbaccio,
E. J. Brnardic, M. E. Fraley, M. E. Layton,
G. D. Hartman, M. A. Jacobson,
B. C. Magliaro, P. H. Hutson,
J. A. O’Brien, S. L. Huszar, J. M. Uslaner,
K. L. Fillgrove, C. Tang, Y. Kuo, S. M. Sur
4:35 292. Substituted biaryl pyrazoles as sodium
channel blockers for the treatment
of neuropathic pain. S. Tyagarajan,
P. K. Chakravarty, B. Zhou, B. Taylor,
W. H. Parsons, M. H. Fisher,
M. J. Wyvratt, K. Lyons, T. Klatt, X. Li,
S. Kumar, B. Williams, J. Felix,
B. T. Priest, R. M. Brochu, V. Warren,
M. Smith, M. Garcia, G. J. Kaczorowski,
W. J. Martin, C. Abbadie, E. McGowan,
N. Jochnowitz, A. Weber, J. L. Duffy
Improving Drug Candidates by Design: A
Focus on Physical Properties to Improve
Disposition and Safety Sponsored by TOXI,
Cosponsored by MEDI
Natural Products Biosynthesis Sponsored
by BIOL, Cosponsored by MEDI and ORGN
Oligonucleotide Therapeutics Sponsored by
CARB, Cosponsored by ANYL, BIOL, MEDI,
and ORGN
Using Waters Explicitly in Drug Discovery
Hybrid Explicit/Implicit Methods Sponsored
by COMP, Cosponsored by CINF and MEDI
WEDNESDAY MORNING
Section A
Boston Convention & Exhibition Center
Ballroom West
JAK Kinase Inhibitors for Cancer and
Myeloproliferative Disease
S. Ioannidis, Organizer
M. Lamb, Organizer, Presiding
8:30 293. Molecular pathogenesis and therapy
of myeloproliferative neoplasms.
P. Koppikar, O. Abdel-Wahab,
S. Marubayashi, O. Kilpivaara, N. Kucine,
R. L. Levine
9:10 294. Identification of AZD1480 as a
novel JAK2 inhibitor. S. Ioannidis
9:50 295. Discovery of CYT387: A potent
and selective dual inhibitor of JAK1 and
JAK2. C. J. Burns
10:30 296. Discovery of polycyclic azaindoles
and deazapurines as potent JAK2
inhibitors. M. W. Ledeboer
11:10 297. Discovery of INCB018424: A potent
and selective JAK1/JAK2 inhibitor for
the treatment of myeloproliferative neoplasms.
J. D. Rodgers, J. S. Fridman,
S. Shepard, T. P. Maduskuie,
A. G. Arvanitis, H. Wang, L. Shao,
B. Folmer, N. Falahatpisheh, M. Rafalski,
L. Storace, R. K. Jalluri, K. Vaddi,
P. J. Haley, T. C. Burn, M. Rupar,
P. C. Liu, M. B. Covington, E. Caulder,
J. Li, P. Waeltz, A. Margulis, R. Wynn,
M. Becker-Pasha, Y. Li, Y. Lo,
B. Thomas, G. Hollis, M. F. Favata,
X. Wen, J. Kelly, K. Solomon,
P. A. Scherle, J. Shi, S. Yeleswaram,
R. C. Newton, S. M. Friedman, B. Metcalf
Section B
Boston Convention & Exhibition Center
Room 253A/B
Opioid Receptors as Targets for Drug
Discovery
M. Lamb, T. Prisinzano, Organizers
T. Brugel, Organizer, Presiding
8:30 Introductory Remarks
8:35 298. Opioid receptors: Past, present,
and future. T. E. Prisinzano
9:20 299. Strategies employed and outcomes
of the multiparameter optimization
of 4-piperidin-4-ylidenemethyl-benzamides
as potent and selective �-opioid
receptor agonists. C. L. Dantzman,
M. M. King, S. Wesolowski, G. E. Ernst,
X. Wang, J. McCauley, K. Brush,
W. E. Palmer, W. Frietze, V. Hoesch,
D. W. Andisik, T. J. Hudzik, K. H. Bui,
J. Liu, N. Spear
10:05 300. Discovery of carboxamide bioisosteres
of the phenolic-OH of opioids.
M. P. Wentland, J. M. Bidlack, Y. Bu,
C. L. Cioffi, D. J. Cohen,
C. M. Dehnhardt, W. Duan, R. Ganorkar,
J. Gargano, C. Guo, J. Jaber, J. Jin,
X. Jia, S. Jo, B. I. Knapp, R. Kucejko,
R. Lou, Q. Lu, A. L. Parkhill,
G. P. Richardson, X. Sun,
M. A. VanAlstine, G. Xu, Y. Ye, H. Zhang,
S. Zhang, Q. Zhou
10:50 301. Discovery and characterization
of a new kappa selective opioid receptor
antagonist. C. H. Mitch, S. Quimby,
J. Matt, N. Diaz, C. Pedregal,
M. De La Torre, Q. Shi, E. Canada,
D. McKinzie, M. Statnick
11:35 302. Potential of opioid receptor antagonists
to manage L-DOPA-induced
dyskinesia in Parkinson’s disease.
R. E. Dolle, A. Goodman,
B. Le Bourdonnec, P. J. Little,
J. M. Brotchie, T. H. Johnston,
J. B. Koprich, S. H. Fox
Process Chemistry: Role of Organic
Chemistry in Early Clinical Drug
Development V Sponsored by ORGN,
Cosponsored by MEDI
Recognition of DNA: Recent Advances
Sponsored by CARB, Cosponsored by MEDI
The Emerging Concepts of Activity
Landscapes and Activity Cliffs and their
Role in Drug Research Sponsored by CINF,
Cosponsored by COMP and MEDI
WEDNESDAY AFTERNOON
Section B
Boston Convention & Exhibition Center
Room 253A/B
New Therapeutic Approaches for Major
Ocular Diseases
T. Bannister, R. Fecik, Organizers,
Presiding
1:30 303. Multifunctional antioxidants for
the treatment of age-related eye diseases.
P. F. Kador, J. Randazzo,
H. Kawada, H. Jin
1:55 304. Aldose reductase inhibitors for the
treatment of diabetic cataracts and retinopathy.
P. F. Kador, M. Wyman,
K. Blessing
2:15 305. KDR kinase inhibitors for retinal
disease: The design and investigation of
small molecules for topical and intravitreal
dosing. M. T. Bilodeau,
A. L. Webber, L. A. Hettrick,
A. C. Hughes, J. W. Maxwell, Y. Kim,
R. L. Peiffer, W. O. Cook, S. Mittal, B. Ma,
X. Mao, K. A. Thomas, C. J. Thut
2:45 306. Recent investigations of prostaglandin
receptor agonist analogs as novel
ocular hypotensive agents in glaucoma
management. R. M. Burk
3:15 307. Discovery and in vitro SAR of AR-
12286, a potent kinase inhibitor for the
treatment of glaucoma. M. A. deLong,
J. M. Sturdivant, S. M. Royalty,
G. R. Heintzelman, J. D. Yingling,
C. L. Laethem, B. W. Sherman,
C. C. Kopczynski
3:45 308. Development of Rho kinase inhibitors
for the treatment of glaucoma.
Y. Feng, P. LoGrasso, Y. Yin, Y. Chen,
X. Fang, S. Chowdhury, T. D. Bannister,
A. Weiser, J. Pocas, W. Grant,
T. Schroeter, M. D. Cameron, L. Lin,
C. Ruiz, S. Khan, A. Pachori, T. Inoue,
V. Rao
4:15 309. Palomid 529, a dual TORC1/
TORC2 inhibitor of the PI3K/Akt/mTOR
pathway as a therapeutic approach to ocular
diseases of retinal neovascularization.
D. Sherris
4:45 310. Activation of the serotonin 5-HT1A
receptor protects the retina from severe
photo-oxidative stress. R. J. Collier
5:15 311. Rho kinase inhibitors: A potential
new treatment for glaucoma. D. J. Slade,
N. Pelz, J. Lampe, P. Watson,
W. Peterson, A. Brown, E. Glaub,
C. Crean, R. Verhoeven, J. Vittitow
Section A
Boston Convention & Exhibition Center
Ballroom West
Drug Discovery for Epigenetic Targets
D. Hertzog, Organizer
R. Trump, Organizer, Presiding
2:00 312. Epigenetic reprogramming of cancer
cells by targeting DNA methylation
dynamics. D. J. Bearss,D.A.Jones,
B. R. Cairns, S. Sharma
2:30 313. Modulating the epigenetic code
readout in transcription. M. Zhou
3:00 314. Discovery of epigenetic chemical
probes. H. Ouyang, C. Arrowsmith,
P. J. Brown
3:30 315. Structure and mechanism guided
identification of histone demethylase inhibitors.
C. J. Schofield
4:00 316. Discovery of chemical probes for
protein lysine methyltransferase G9a.
F. Liu, X. Chen, A. Allali-Hassani,
A. M. Quinn, T. J. Wigle, D. Barsyte,
J. M. Yost, G. A. Wasney, A. Dong,
I. Kozieradzki, G. Senisterra, I. Chau,
A. Siarheyeva, A. Van Deusen,
D. B. Kireev, A. Jadhav, M. Herold,
S. V. Frye, C. H. Arrowsmith,
W. P. Janzen, P. J. Brown, A. Simeonov,
M. Vedadi, J. Jin
4:30 317. Identification of potent and selective
small molecule inhibitors of the BET
family bromodomains demonstrate the
tractability of a new class of epigenetic
targets for drug discovery. C. Chung
The Emerging Concepts of Activity
Landscapes and Activity Cliffs and their
Role in Drug Research Sponsored by CINF,
Cosponsored by COMP and MEDI
WEDNESDAY EVENING
Section A
Boston Convention & Exhibition Center
Room 153ABC
General Poster Session
J. Zablocki, Organizer
7:00–9:00
318. Asymmetric synthesis of the estrogen
receptor � ligand, S-2,3-bis(p-hydroxyphenyl)propionitrile
(S-DPN).
V. M. Carroll, J. A. Katzenellenbogen
319. Synthesis and structural optimization of
multiple H-bonding region of diarylalkyl
(thio)amides as novel TRPV1 antagonists.
F. Li, J. Jang, N. Kim, Y. Jeong, S. Kim,
Y. Park, Y. Suh
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