Appeal No. 2001-2646 Page 3
Application No. 08/463,951
released from nerves, and exert a variety of biological actions, which, in most
cases, depend upon activation of specific receptors expressed on the membrane
of target cells.” Id., page 2.
The specification discloses that the tachykinin known as substance P is
believed to be “involved in neurotransmission of pain sensations, including the
pain associated with migraine headaches and with arthritis.” Id. Tachykinins
“have also been implicated in gastrointestinal disorders and diseases of the
gastrointestinal tract such as inflammatory bowel disease.” Id. The specification
provides an extensive list of other disorders that are disclosed to be “associated
with an excess of tachykinins.” See pages 126-129.
Tachykinin receptor antagonists have been the subject of research as
potential therapeutic agents. See id., page 2. “The earliest tachykinin receptor
antagonists were peptide derivatives. These antagonists proved to be of limited
pharmaceutical utility because of their metabolic instability.” Id., pages 2-3. The
specification discloses “a class of potent non-peptide tachykinin receptor
antagonists.” Page 3. The specification provides 177 exemplary compounds
and shows that they have varying affinities for the NK-1 and NK-2 tachykinin
receptors when assayed in an in vitro test. See pages 44-110 (exemplary
compounds) and pages 111-126 (in vitro binding assays and results).
Discussion
The claims are directed to compounds corresponding to a subgenus of the
disclosed class of tachykinin receptor antagonists; specifically, those having a
piperidinyl or piperazinyl moiety in the R1 position. The claims also encompass
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