Appeal No. 2001-2157 Page 2
Application No. 08/918,741
about 60% of the bone mass in the trabecular compartment of the bone within 3 to 6
years after the cessation of menses. This rapid loss is generally associated with an
increase of bone resorption and formation. However, the resorptive cycle is more
dominant and the result is a net loss of bone mass. Osteoporosis is a common and
serious disease among postmenopausal women. (Specification, page 1).
At the time applicants' invention was made, raloxifene was a known therapeutic
drug classified as a selective estrogen receptor modulator (SERM). As stated in the
background section of applicants' specification, page 3, line 34 through page 4, line 3:
Raloxifene, a second generation SERM, displays potentially useful
selectivity in uterine tissue with apparent advantages over
triphenylethylene-based estrogen receptor ligands. As such, raloxifene
appears to be well-suited at least for the treatment of postmenopausal
complications, including osteoporosis and cardiovascular disease.
Applicants note, however, that:
The advancement of raloxifene, in particular, has been somewhat
hampered by its physical characteristics, both as to bioavailabilitiy and
manufacturing. For example, raloxifene is generally insoluble, which may
affect bioavailability. Clearly, any improvement in the physical
characteristics of raloxifene and in closely related compounds would
potentially offer a more beneficial therapy and enhanced manufacturing
capabilities.
Thus, it would be a significant contribution to the art to provide
amorphous forms of raloxifene and related compounds which have
increased solubility, methods of preparation, pharmaceutical formulations,
and methods of use. [Specification, page 4, lines 9-20].
Applicants' invention is drawn to raloxifene "in an amorphous form;" to a process
for preparing same; to a pharmaceutical formulation comprising amorphous raloxifene
in combination with a pharmaceutically acceptable carrier, diluent, or excipient; and to a
method for inhibiting bone loss or bone resorption by administering to a patient in need
thereof amorphous raloxifene.
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