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Wai C. Wong

ImClone Systems

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Bioorganic & Medicinal Chemistry | 2009

Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2

Matthew Duncton; Eugene L. Piatnitski Chekler; Reeti Katoch-Rouse; Dan Sherman; Wai C. Wong; Leon M. Smith; Joel Kawakami; Alexander S. Kiselyov; Daniel L. Milligan; Chris Balagtas; Yaron R. Hadari; Ying Wang; Sheetal Patel; Robin L. Rolster; James R. Tonra; David Surguladze; Stan Mitelman; Paul Kussie; Peter Bohlen; Jacqueline F. Doody

A series of arylphthalazine derivatives were synthesized and evaluated as antagonists of VEGF receptor II (VEGFR-2). IM-094482 57, which was prepared in two steps from commercially available starting materials, was found to be a potent inhibitor of VEGFR-2 in enzymatic, cellular and mitogenic assays (comparable activity to ZD-6474). Additionally, 57 inhibited the related receptor, VEGF receptor I (VEGFR-1), and showed excellent exposure when dosed orally to female CD-1 mice.

Synthetic Communications | 2006

Efficient Preparation of ((3‐Chloro‐2‐fluoro‐phenyl)‐[7‐methoxy‐8‐(3‐morpholin‐4‐yl‐propoxy)‐10,11‐dihydro‐5‐oxa‐2,4,11‐triaza‐dibenzo(a,d)cyclohepten‐1‐yl]‐amine) for In‐Vivo Study

Hu Liu; Leon M. Smith; Yunyu Mao; Weitao Pan; Yong-Jiang Xu; Sabina Burdzovic-Wizeman; Matthew Duncton; Wai C. Wong

Abstract An improved route for the preparation of highly functionalized 5,6‐dihydro‐pyrimido[4,5‐b][1,4]oxazepine 1a in multigram quantities was developed. This new methodology was highlighted by the proper methoxy disposition via a regioselective methylation of 2,4,5‐trihydroxy‐benzaldehyde followed by a magnesium sulfate–promoted cyclization.

Bioorganic & Medicinal Chemistry Letters | 2005

Synthesis and structure–activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors

Xiaohu Ouyang; Xiaoling Chen; Evgueni Piatnitski; Alexander S. Kiselyov; Hai-Ying He; Yunyu Mao; Vatee Pattaropong; Yang Yu; Ki Kim; John Kincaid; Leon M. Smith; Wai C. Wong; Sui Ping Lee; Daniel L. Milligan; Asra Malikzay; James Fleming; Jason Gerlak; Dhanvanthri S. Deevi; Jacqueline F. Doody; Hui-Hsien Chiang; Sheetal Patel; Ying Wang; Robin L. Rolser; Paul Kussie; Marc Labelle; M. Carolina Tuma

Bioorganic & Medicinal Chemistry Letters | 2005

Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase.

Evgueni Piatnitski; Matthew Duncton; Alexander S. Kiselyov; Reeti Katoch-Rouse; Dan Sherman; Daniel L. Milligan; Chris Balagtas; Wai C. Wong; Joel Kawakami; Jacqueline F. Doody

Bioorganic & Medicinal Chemistry Letters | 2006

Arylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II.

Matthew Duncton; Evgueni Piatnitski; Reeti Katoch-Rouse; Leon M. Smith; Alexander S. Kiselyov; Daniel L. Milligan; Chris Balagtas; Wai C. Wong; Joel Kawakami; Jacqueline F. Doody

Bioorganic & Medicinal Chemistry Letters | 2006

1-[4-(1H-Benzoimidazol-2-yl)-phenyl]-3-[4-(1H-benzoimidazol-2-yl)-phenyl]-urea derivatives as small molecule heparanase inhibitors.

Weitao Pan; Hua-Quan Miao; Yong-Jiang Xu; Elizabeth Navarro; James R. Tonra; Erik Corcoran; Armin Lahiji; Paul Kussie; Alexander S. Kiselyov; Wai C. Wong; Hu Liu

Bioorganic & Medicinal Chemistry Letters | 2005

Pyrimido-oxazepine as a versatile template for the development of inhibitors of specific kinases.

Weitao Pan; Hu Liu; Yong-Jiang Xu; Xin Chen; Ki Kim; Daniel L. Milligan; John Columbus; Yaron R. Hadari; Paul Kussie; Wai C. Wong; Marc Labelle

Bioorganic & Medicinal Chemistry Letters | 2006

Novel tricyclic azepine derivatives: Biological evaluation of pyrimido[4,5-b]-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase

Leon M. Smith; Wai C. Wong; Alexander S. Kiselyov; Sabina Burdzovic-Wizemann; Yunyu Mao; Yong-Jiang Xu; Matthew Duncton; Ki Kim; Evgueni Piatnitski; Jacqueline F. Doody; Ying Wang; Robin L. Rosler; Daniel L. Milligan; John Columbus; Chris Balagtas; Sui Ping Lee; Andrey Konovalov; Yaron R. Hadari

Bioorganic & Medicinal Chemistry Letters | 2006

N-(4-{[4-(1H-Benzoimidazol-2-yl)-arylamino]-methyl}-phenyl)-benzamide derivatives as small molecule heparanase inhibitors.

Yong-Jiang Xu; Hua-Quan Miao; Weitao Pan; Elizabeth Navarro; James R. Tonra; Stan Mitelman; Margarita Camara; Dhanvanthri S. Deevi; Alexander S. Kiselyov; Paul Kussie; Wai C. Wong; Hu Liu

Bioorganic & Medicinal Chemistry Letters | 2006

Tricyclic azepine derivatives: Pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors

Leon M. Smith; Evgueni Piatnitski; Alexander S. Kiselyov; Xiaohu Ouyang; Xiaoling Chen; Sabina Burdzovic-Wizemann; Yong-Jiang Xu; Ying Wang; Robin L. Rosler; Sheetal Patel; Hui-Hsien Chiang; Daniel L. Milligan; John Columbus; Wai C. Wong; Jacqueline F. Doody; Yaron R. Hadari

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