BOARD OF PATENT
`APPEALS & ~ J5"
`INTERFERENCES . ::tr
`JUN I I 1992
`
`IN THE UNITED STATES PATENT AND TRADEMARK OFFICE
`BEFORE THE BOARD OF PATENT APPEALS AND INTERFERENCES
`
`WATTANASIN
`v.
`PICARD ET AL
`v.
`FUJIKAWA ET AL
`
`INTERFERENCE 102,648
`EXAMINER-IN-CHIEF:
`MICHAEL SOFOCLEOUS
`
`:
`.
`:
`•
`. . . .
`:
`. . . .
`. .
`
`FUJIKAWA ET AL MOTION TO ADD COUNTS 1
`37 CFR §1.633(c)
`
`HONORABLE COMMISSIONER OF PATENTS AND TRADEMARKS
`WASHINGTON, DC 20231
`.
`BOX INTERFERENCE
`
`SIR:
`
`Pursuant to the provisions of the above Motion, the Senior
`
`Party hereby moves that the subject matter of this Interference be
`
`redefined by the addition of Counts 3 and 4, set forth below. As
`
`required by 37 CFR §1.637(c)(1)(ii) and (vi), this Motion is
`
`accompanied by an Amendment in Fujikawa's application involved
`
`herein, and a Request for Benefit as to the proposed Counts, and
`
`claims added by Amendment.
`
`Fujikawa moves the following Counts be added to redefine the
`
`... ,,...;,.
`
`NCI Exhibit 2018
`Page 1 of 11
`
`
`APPEALS & ~ J5"
`INTERFERENCES . ::tr
`JUN I I 1992
`
`IN THE UNITED STATES PATENT AND TRADEMARK OFFICE
`BEFORE THE BOARD OF PATENT APPEALS AND INTERFERENCES
`
`WATTANASIN
`v.
`PICARD ET AL
`v.
`FUJIKAWA ET AL
`
`INTERFERENCE 102,648
`EXAMINER-IN-CHIEF:
`MICHAEL SOFOCLEOUS
`
`:
`.
`:
`•
`. . . .
`:
`. . . .
`. .
`
`FUJIKAWA ET AL MOTION TO ADD COUNTS 1
`37 CFR §1.633(c)
`
`HONORABLE COMMISSIONER OF PATENTS AND TRADEMARKS
`WASHINGTON, DC 20231
`.
`BOX INTERFERENCE
`
`SIR:
`
`Pursuant to the provisions of the above Motion, the Senior
`
`Party hereby moves that the subject matter of this Interference be
`
`redefined by the addition of Counts 3 and 4, set forth below. As
`
`required by 37 CFR §1.637(c)(1)(ii) and (vi), this Motion is
`
`accompanied by an Amendment in Fujikawa's application involved
`
`herein, and a Request for Benefit as to the proposed Counts, and
`
`claims added by Amendment.
`
`Fujikawa moves the following Counts be added to redefine the
`
`... ,,...;,.
`
`NCI Exhibit 2018
`Page 1 of 11
`
`
`
`Interference.
`
`2
`
`Count 3
`
`A compound of the formula:
`
`0
`
`z
`
`wherein R1 = H
`
`N
`
`. 5
`R
`
`R5 = cyclopropyl (c-Pr) and Z is selected from the group
`
`consisting of
`
`-CH(OH)-CH2-CH(OH)-CH2-COOH
`
`-CH(OH)-CH2-CH(OH)-CH2-COONa
`-CH(OH)-CH2-CH(OH)-CH2C001/2Ca
`-CH(OH)-CH2-CH(OH)-CH2-COOR, Wherein R is C1_31 alkyl and
`
`HO
`
`lactone.
`
`·-"--'·
`
`NCI Exhibit 2018
`Page 2 of 11
`
`
`
`Count 4
`
`3
`
`A method of inhibiting cholesterol biosynthesis in a
`
`patient
`
`in
`
`need
`
`of
`
`said
`
`treatment
`
`comprising
`
`administering thereto a cholesterol synthesis inhibiting
`
`amount of a compound as defined by Count 3 in combination
`
`with a pharmaceutically acceptable carrier.
`
`STATEMENT OF MATERIAL FACTS
`
`1.
`
`The compounds embraced by Count 1 of
`
`the current
`
`Interference and the claims of the Senior and Junior Party thereto
`
`(Judgment against Picard et .al having been rendered based on
`
`request for the same) designated as corresponding to the Count have
`
`utilities as
`
`inhibitors of biosynthesis of cholesterol
`
`(the
`
`synthesis, in vivo by animals, of cholestero·l).
`
`2. The method of inhibiting cholesterol biosynthesis in an
`
`animal in need of same by administration of the compounds of Count
`
`has been
`
`judged to be patentably distinct from Count 1, and
`
`constitutes separate Count 2 of this Interference.
`
`NCI Exhibit 2018
`Page 3 of 11
`
`
`
`4
`
`3.
`
`The compounds of proposed Count 3, characterized by a
`
`cyclopropyl substituent at R5
`
`, exhibit unusually high activity in
`
`the
`
`inhibition of cholesterol biosynthesis.
`
`Page 3 of
`
`the
`
`Declaration of Kitahara.
`
`4. In side-by-side comparisons with structural isomers of the
`
`proposed Count 3, varying only with respect to the identity of the
`
`R5 substituent,
`
`the n-propyl and
`
`isopropyl
`
`isomers exhibited
`
`dramatically reduced activity, whether measured in vivo or in
`
`vitro.
`
`The Declaration of Kitahara, see the tables attached
`
`thereto.
`
`5.
`
`The unusually high activity exhibited by compounds of
`
`proposed Count 3 is not a function of the molecular weight of the
`
`substituent at R5 • Analogous substituents, both lower and greater
`
`molecular weight, show lower activity, when the remainder of the
`
`molecule is the same.
`
`See the Kitahara · Declaration,
`
`tables
`
`attached thereto.
`
`6.
`
`There is nothing in the art that would suggest the
`
`enhanced activity conferred on the compounds of Count 1 when R5 is
`
`cyclopropyl and the remaining identities of Count 3 are observed •
`
`. :· ........
`
`NCI Exhibit 2018
`Page 4 of 11
`
`
`
`5
`
`One of ordinary skill in the art could not have predicted the
`
`differences between compounds of Count 3, and isomers thereof with
`
`respect
`
`to R5 ,
`
`on
`
`the basis of structure only.
`
`Kitahara
`
`Declaration, paragraph 5.
`
`7.
`
`The Fujikawa application describes, and enablingly
`
`discloses, compounds within the scope of proposed Count 3, as well
`
`as providing a generic description of that Count.
`
`B.
`
`The application of Wattanasin involved herein does not
`
`specifically identify cyclopropyl as a substituent at the R5
`
`position (R in the claims of Wattanasin). This substituent is
`
`suitably identified as cycloalkyl C3_71 however, and the application
`
`elsewhere identifies isopropyl and methyl as suitable substituents
`
`for this position.
`
`Thus, the identity of this substituent as
`
`cyclopropyl is reasonably conveyed to those of ordinary skill in
`
`the art by the application of Wattanasin.
`
`REASONS IN SUPPORT OF THE DESIRED RELIEF
`
`As set forth in MPP 2309.01, each Count must be drawn to a
`
`separate patentable invention. Separate counts to a species or
`
`NCI Exhibit 2018
`Page 5 of 11
`
`
`
`. '
`
`6
`
`sub-genus
`
`may
`
`be presented, if
`
`the specie or sub-genus
`
`is
`
`unobvious
`
`over
`
`the genus , even
`
`though the genus may not be
`
`patentable, given the specie. Thus, in this Interference, adoption
`
`of Counts 3 and 4 is appropriate if the sub-genus of Count 3 is
`
`patentable over the genus of Count 1, and the sub-genus of Count 4
`
`is patentable over the genus of Count 2. Fujikawa respectfully
`
`submits that the declaration of Kitahara clearly indicates that
`
`such is the situation here.
`
`There is no question that the sub-genus of Counts 3 and 4 are
`
`herein embraced by Counts 1 and 2.. Demonstration of the unobvious
`
`nature, and patentability, of a sub-genus or a species over an
`
`embracing genus can be achieved by proof tending to show activity
`
`in the sub-genus or species that is unpredictably higher than that
`
`exhibited in the genus as a whole. Ex parte Ebata, 19 USPQ2d 1952
`
`(POBAI 1991).
`
`The Declaration of Kitahara submitted herewith
`
`clearly demonstrates such unpredicted superior bioactivity.
`
`As noted above, Count 1 embraces a wide number of compounds
`
`whose utility is identified by both parties as the inhibition of
`
`the biosynthesis of cholesterol. In other words, administration of
`
`these compounds to individuals can result in the reduction of
`
`NCI Exhibit 2018
`Page 6 of 11
`
`
`
`7
`
`biosynthesis of cholesterol by the individual so treated. This
`
`second invention is addressed by Count 2. As set forth in the
`
`Declaration of Kitahara submitted herewith, compounds within the
`
`limited sub-genus of Count 3, when R5 is cyclopropyl, exhibit
`
`unexpectedly superior cholesterol biosynthesis inhibition activity,
`
`when compare with isomeric forms of the compounds of Count 1. Not
`
`only the isomers, but analogous compounds, wherein R5 is an alkyl
`
`group of lower or higher carbon number, branched or unbranched,
`
`have also been demonstrated to be patentably distinct from the
`
`compounds of Count 3, in terms of bioactivity.
`
`Similar to the relation between Counts 1 and 3, administration
`
`of the compounds of Count 3 to an animal in need of inhibition of
`
`biosynthesis of cholesterol as called for in Count 4 is equally
`
`patentable over the broad genus of Count 2 .
`
`This can be most
`
`clearly seen by reference to the Declaration of Kitahara, and the
`
`Tables attached thereto. The unobviously superior bioactivity of
`
`Kitahara is evidenced in the dramatically reduced IC 50 values of the
`
`compounds of Count 3.
`
`Thus, administration will ·require
`
`dramatically reduced dosages, or reduced administration periods, to
`
`achieve the same results. Such is the stuff of unobviousness.
`
`NCI Exhibit 2018
`Page 7 of 11
`
`
`
`8
`
`Structural similarity would predict similar bioactivity.
`
`Certainly, there is nothing of record which would predict the
`
`unusual bioactivity keyed by the R5 substituent as cyclopropyl.
`
`See the Declaration of Kitahara.
`
`Indeed,
`
`it is respectfully
`
`submitted that one of ordinary
`
`skill in
`
`the art would not
`
`immediately recognize the substitution as a point on the molecule
`
`determining activity. Nonetheless, the same has been demonstrated
`
`to be true, by competent comparative experiment.
`
`Counts 3 and 4 having been demonstrated, by comparative
`
`experiment commensurate in scope with the Counts themselves, to be
`
`unobvious over the genus over Counts 1 and 2, addition of Counts 3
`
`and 4 to this Interference is respectfully requested.
`
`FUJIKAWA'S CLAIMS TO CORRESPOND TO THE COUNTER INTERFERENCE
`
`The original claim 10 of
`
`the Fujikawa application was
`
`cancelled, and pursued in a copending application which is the
`
`subject of a separate paper in this Interference, during ex parte
`
`prosecution, see the Amendment of December 19, 1990. Claim 10
`
`would have corresponded to proposed Count 3 .
`
`In a separate
`
`Amendment pursuant to 37 CFR 1.637(c)(1)(ii), Fujikawa submits an
`
`'
`
`NCI Exhibit 2018
`Page 8 of 11
`
`
`
`Amendment presenting claims 41-44, claims 41-43 corresponding to
`
`Count 3 and claim 44 corresponding to Count 4.
`
`9
`
`PROPOSED CLAIM FOR WATTANASIN
`
`Pursuant to the provisions of Rule 637(c)(l)(iii), Fujikawa
`
`notes that no claim currently presented by Wattanasin appears to
`
`correspond to either Count 3 or Count 4.
`
`Such claims can be
`
`presented by Wattanasin, and the same are suggested below.
`
`As a claim corresponding to Count 3 of the Interference,
`
`Fujikawa suggests Wattanasin adapt the following claim 11.
`
`Claim 11. The compound of claim 1, wherein R1 and R2 are
`
`hydrogen, R, is -@- F, X is -CH=CH-, R is
`
`-CH(cid:173)
`cyclopropyl, Q is I
`OH
`
`atoms and M is sodium.
`
`R6 is H, R8 is an alkyl of 1-3 carbon
`
`As a claim corresponding to Count 4, Fujikawa proposes Wattanasin
`
`adopt the following claim 12.
`
`NCI Exhibit 2018
`Page 9 of 11
`
`
`
`10
`
`Claim 12. A method of inhibiting cholesterol biosynthesis in
`
`a patient in need of said treatment comprising administering
`
`a cholesterol biosynthesis inhibiting amount of the compound
`
`of Claim 11 in combination with a pharmaceutically acceptable
`
`carrier.
`
`Save for the issue of a priority, these claims appear to be
`
`patentable to Wattanasin. Note in particular that in Claim 11, the
`
`identity of all substituents is selected
`
`from a disclosure
`
`appearing in Claim 2, save for the identifi:cation of M and R. With
`
`regard to the identity of M, Wattanasin identifies sodium as a
`
`pharmaceutically acceptable cation at page 5 of the specification.
`
`Indeed, this is the preferred cation. With regard to cyclopropyl,
`
`as the identity for R, note that Claim 1 specifies that this group
`
`may be cycloalkyl of 3-7 carbon atoms. Although cyclopropyl is not
`
`specified, the corresponding non-cyclocpropyl isomer, isopropyl is
`
`particularly identified.
`
`See, e.g. Cla~ 4 and with more
`
`particularity, the disclosure at page 4 of the specifications.
`
`Accordingly, substituent R as cyclocpropyl in the Application and
`
`Claim 1 of Wattanasin appears to be reasonably conveyed to those of
`
`ordinary skill in the art, and the claim appears to be patentable
`
`to Wattanasin, save for the issue of priority in this Interference.
`
`With regard to Claim 12, this appears to correspond exactly to
`
`Claim a·of Wattanasin, substituting Claim 11 for Claim 1.
`
`NCI Exhibit 2018
`Page 10 of 11
`
`
`
`11
`
`Accordingly, as Wattanasin appears able to contest this
`
`Interference with claims patentable
`
`thereto, entry of an
`
`appropriate Order is respectfully requested.
`
`Fujikawa, having demonstrated proposed Counts 3 and 4 to be
`
`directed to subject matter patentable over the current Counts of
`
`the Interference and directed to an invention separately patentable
`
`from every Count in the Interference, having added claims to its
`
`own Application that correspond to the Count and suggested Claims
`
`for Wattanasin that correspond to the Count, redefinition of the
`
`subject matter of the Interference by addition of Counts 3 and 4 is
`
`respectfully requested.
`
`A Motion for Benefit accompanies this
`
`Motion.
`
`Respectfully submitted,
`
`OBLON, SPIVAK, McCLELLAND,
`MAIER & NEUSTADT, P.C.
`
`Norman F. Oblon
`Registration No.: 24,618
`
`Steven B. Kelber
`Registration No.: 30,073
`Attorneys of Record
`
`Fourth Floor
`1755 South Jefferson
`Arlington, Virginia
`703-521-5940
`
`Davis Highway
`22202
`
`NCI Exhibit 2018
`Page 11 of 11
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