Appeal No. 1997-0100
Application 08/167,051
Bradykinin (BK) is a nonapeptide generated as a result of the activity of
kallikreins, a group of proteolytic enzymes present in most tissues and body
fluids, on kininogens.
Bradykinin, and its physiologically important related peptides . . . exhibit
physiological actions which qualify them as mediators of inflammatory
reactions, hypotensive states, and pain. Bradykinin is overproduced in
pathological conditions such as septic shock, anaphylaxis, rhinitis, asthma . .
.
In addition to its analgesic and proinflammatory effects, bradykinin is a
vasodilator. Because of its ability to lower blood pressure, bradykinin has
been implicated in the pathogenesis of several shock syndromes . . .
Bradykinin is also a potent bronchoconstrictor . . .
Thus a bradykinin inhibitor or bradykinin receptor antagonist is expected to
possess a number of desirable biological effects in the treatment, for
example, inflammation, septic shock, asthma, burn pain, rhinitis and allergy.
According to appellants, the present invention is directed to bradykinin antagonists
“that act as specific and competitive inhibitors of the biological activities of bradykinin,”
wherein the L-Pro at position seven of the native bradykinin is replaced by D-Phe or D-Tic,
and the L-Phe at position eight is replaced by a hydroxyproline ether or a thioether
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derivative (Brief, page 3).
DISCUSSION
All of the pending claims stand rejected as obvious over Henke I, Henke II, Stewart I,
Stewart II, Hock, Patchett and Krapcho.
3Tic is the abbreviation for 1,2,3,4-tetrahydroisoquinoline-3-ylcarbonyl.
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