Chemistry Reference
In-Depth Information
Table 15.2
(Continued)
Exclusivity
expiration
date
(United
States)
Active
ingredient
name
Commercial
name(s)
Type of
coupling(s)
FDA approval
date
Structure
Ref.
Applicant
Indication
Abiraterone
acetate
Zytiga
Suzuki-
Miyaura
14
Jansenn Biotech Inhibitor of
human
cytochrome
P450 17a for the
treatment of
castration-
resistant
prostate cancer
April 28,
2011
February
2014
N
H
H
H
AcO
Crizotinib
Xalkori
Cl
Suzuki-
Miyaura
15
Pfizer
Treatment of
metastatic
non-small cell
lung cancer
August 26,
2011
March 2025
N
N
O
NH
F
Cl
N
H 2 N
Ruxolitinib
phosphate
Jakafi
Jakavi
Suzuki-
Miyaura
16
Incyte/Novartis
Tyrosine-protein
kinase JAK 1/2
inhibitor for
treatment of
myelofibrosis
November
16, 2011
December
2027
CN
N
N
￿H 3 PO 4
N
N
H
N
Vemurafenib Zelboraf
Suzuki-
Miyaura
17
Plexxikon/
Genentech/F.
Hoffmann La
Roche
B-Raf enzyme
inhibitor for
the treatment
of unresectable
or metastatic
melanoma
August 17,
2011
October
2026
F
O
O
Cl
O
S
N
H
n -Pr
F
H
N
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