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IN THE UNITED STATES PATENT & TRADEMARK OFFICE
`
`IN RE APPLICATION OF:
`
`YOSHIHIRO FUJIKAWA ET AL
`
`:
`
`:
`
`GROUP ART UNIT:
`
`DIVISIONAL APPLICATION DIVIDED FROM
`
`EXAMINER:
`
`: :
`
`SERIAL NO.:
`
`07/631,092
`
`FOR:
`
`QUINOLINE TYPE MEVALONOLACTONES
`
`:
`
`DECLARATION UNDER 37 CFR 1.132
`
`HONORABLE COMMISSIONER OF PATENTS & TRADEMARKS
`
`WASHINGTON, D.C.
`
`20231
`
`SIR:
`
`I, Masaki Kitahara, do hereby declare and state
`
`that:
`
`l. I am a named co-inventor in the above-captioned
`
`patent application, an employee of Nissan Chemical
`
`Industries, Limited, and a citizen and resident of Japan.
`
`2.
`
`I am familiar with the above-captioned patent
`
`application, and Claims presented by Divisional
`
`Application.
`
`3. To demonstrate the unobvious superiority of the
`
`subject matter claimed therein, comparative tests were
`
`conducted, demonstrating the importance and unobvious
`
`superiority conferred on these compounds by the selection
`
`gwr.“
`
`Mylan Exhibit 1032, Page 1
`
`Mylan Exhibit 1032, Page 1
`
`

`
`-of the oyclopropyl
`
`(c—Pr) substituent. These are
`
`described as follows:
`
`Data was obtained with regard to the following
`
`compound having the formula:
`
`OH
`
`0}-{C00 - 1/2Ca F
`
`@ I
`@ ON
`
`R‘
`
`Comgound
`
`gfi
`
`Evaluation
`
`Evaluation
`
`TEST METHOD
`
`Test A
`
`Test B
`
`Compound
`
`of this
`Invention
`
`cyclopropyl
`
`4.4 x 10*9
`
`35.0 x 10—9
`
`(c—Pr)
`
`Reference
`
`isopropyl
`
`23.0 x 10-9
`
`105 x 10-9
`
`Compound
`
`(i-Pr)
`
`Test A:
`
`Inhibition of cholesterol
`
`biosynthesis from acetate in vitro
`
`This test was carried out as described on pages
`
`28-29 of the specification.
`
`The above numerical values
`
`indicate IC5o (molar concentration).
`
`Mylan Exhibit 1032, Page 2
`
`Mylan Exhibit 1032, Page 2
`
`

`
`O
`
`O
`
`Test B:
`
`inhibition of cholesterol
`
`bios nthesis in culture cells
`
`This test was carried out as described on pages 29
`
`to 30 of the specification.
`
`The above numerical values
`
`indicate IC5o (molar concentration).
`
`4. Based on the data reported above, it can be
`
`determined that the compound of this invention exhibits
`
`unobvious superiority, and in particular, sharply enhanced
`
`inhibition of cholesterol biosynthesis,
`
`in vitro, and
`
`culture cell, when compared with the referenced compound
`
`‘of the prior art, and compounds having an identical
`
`structure save for the selection of cyclopropyl, as
`
`opposed to isopropyl substituent, for R5. This enhanced
`
`activity could not be predicted on the basis of structure,
`
`or information available to those of ordinary skill in the
`
`art as of the effective filing date of this application.
`
`Mylan Exhibit 1032, Page 3
`
`Mylan Exhibit 1032, Page 3
`
`

`
`All statements made herein of my own knowledge are
`
`true, and all statements made on information and belief
`
`are believed true.
`
`I am aware that willful false
`
`statements and the like are punishable by fine,
`
`imprisonment or both, 18 U.S.C. §100l, and that such
`
`willful false statements may jeopardize the validity of
`
`the above-captioned patent application and any patent
`
`issuing thereon.
`
`FURTHER,
`
`I SAYETH NOT.
`
`May25, 1992
`D8“;
`
`{
`§:.!
`.
`l,{&a/
`Masaki Kitahara
`
`Mylan Exhibit 1032, Page 4
`
`Mylan Exhibit 1032, Page 4

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