`
`PATENT
`
`IN THE UNITED STATES PATENT AND TRADEMARK OFFICE
`
`Commissioner for Patents
`
`P.O. Box 1450
`
`Alexandria, VA 22313-1450
`
`Prior Application Art Unit: 1628 Prior Application Examiner: San Ming R. Hui
`
`Commissioner: This is a request for filing a
`
`[XI Continuation |:I Continuation-in-Part [:1 Divisional Application under 37 C.F.R.
`§ 1.53(b) of pending prior Application No. 12/285,887 filed October 15, 2008 of John R.
`EVANS and Rosalind U. GRUNDY for FORMULATION.
`
`1.
`
`IX
`
`Enclosed is a complete copy of the prior application including the oath or
`Declaration and 2 sheets of drawings, as filed as a Substitute
`Specification on March 3, 2010, which corresponds to the subject matter
`as originally filed. I hereby verify that the attached papers are a true copy
`of prior Application No. 12/285,887 as filed on March 3, 2010, which
`corresponds to the subject matter as originally filed on October 15, 2008,
`which is incorporated herein by reference.
`
`Enclosed is a Request for Non-Publication of Application and Certification
`Under 35 U.S.C. § 122(b)(2)(B)(i).
`
`A Preliminary Amendment is enclosed.
`
`Enclosed is a Certification and Request for Prioritized Examination Under
`35 U.S.C. § 1.102(e).
`
`|:|
`
`[Z
`
`IXI
`
`2.
`
`3
`
`4.
`
`5.
`
`E The filing fee is calculated on the basis of the claims existing in the prior
`application as amended in the Preliminary Amendment filed herewith.
`
`Search Fee
`
`Basic Utility Application Filing Fee
`
`Examination Fee
`
`|nnoPharma Exhibit 10870001
`
`
`
`
`
`Application No.: Unassigned
`Attorney Docket No.: 11285.0056-01000
`Page 2 of 3
`
`
`
`—I-_
`IT
`
`
`
`
`
`
`
`
`_-100+50=_*x$310
`
`
`
`Size Fee: Paper Filing
`Total Application Pages
`(specification, drawings, printed
`
`*Rounded up to next whole number
`sequence or computer listing,
`
`relimina
`amendment
`Additional Fee for Paper
`Filing New Application
`
`(DELETE if filing new application
`via EFS Web - fee not required for
`EFS new application
`
`submissions
`Size Fee: EFS-Web Filing
`Total Application Pages
`(specification, drawings, printed
`sequence or computer listing,
`reliminar amendment
`
`
`
`
`
`
`
`
`25X.75-100+50=O*x$31O
`
`‘Rounded up to next whole number
`
`$
`
`135°-0°
`
`
`
`
`
`
`T $
`
`
`
`
`Publication Fee under 35 U.S.C. § 1.18(d)
`
`TOTAL FEES DUE
`
`$
`
`$
`
`4-8°”-0°
`300.00
`
`6,480.00
`
`6.
`
`7.
`
`IX]
`
`IX]
`
`The fee of $ 6,480.00 is submitted herewith.
`
`The Commissioner is hereby authorized to charge any fees which may be
`required, including fees due under 37 C.F.R. § 1.16, and any other fees
`due under 37 C.F.R. § 1.17, or credit any overpayment during the
`pendency of this application to Deposit Account No. 06-0916.
`
`8.
`
`[I
`
`New acceptable drawings are enclosed.
`
`|nnoPharma Exhibit 10870002
`
`
`
`
`
`
`
`
`
`Application No.: Unassigned
`Attorney Docket No.: 11285.0056-01000
`Page 3 of 3
`
`9.
`
`X The prior application is assigned of record to: Astrazeneca AB as
`indicated by the assignments recorded at reel 011635, frame 0063 on
`March 27, 2001 and at reel 015906, frame 0402 on October 18, 2004.
`
`10.
`
`IX
`
`Priority of Application No. 0000313.7, filed on January 10, 2000 and
`Application No. 0008837.7, filed on April 12, 2000, both in Great Britain
`are claimed under 35 U.S.C. § 119. A certified copy
`
`11.
`
`12.
`
`I3
`
`XI
`
`CI is enclosed or
`
`IE is on file in the prior application.
`
`Small entity status is appropriate and applies to this application.
`
`The power of attorney in the prior application is to FINNEGAN,
`HENDERSON, FARABOW, GARRETT & DUNNER, L.L.P., Customer No.
`22,852.
`
`13.
`
`I:
`
`A Listing Under 37 C.F.R. § 1.32(c)(3) of Ten or Fewer Practitioners to
`be Recognized by the PTO as Being of Record is attached.
`
`14.
`
`|:|
`
`The power appears in the original declaration of the prior application.
`
`15. X Since the power does not appear in the original declaration, a copy of the
`power in the prior application is enclosed.
`
`16.
`
`X]
`
`Please address all correspondence to FINNEGAN, HENDERSON,
`FARABOW, GARRETT and DUNNER, L.L.P., Customer Number 22,852.
`
`If any extension of time is necessary for the filing of this
`PETITION FOR EXTENSION.
`application, including any extension in parent Application No. 12/285,887, filed
`October 15, 2008, for the purpose of maintaining copendency between the parent
`application and this application, and such extension has not othen/vise been requested,
`such an extension is hereby requested, and the Commissioner is authorized to charge
`necessary fees for such an extension to Deposit Account No. 06-0916. A duplicate
`copy of this paper is enclosed for use in charging the deposit account.
`
`FINNEGAN, HENDERSON, FARABOW,
`GARRETT & DUNNER, L.L.P.
`
`Dated: September 4, 2012
`
`By:
`
`/
`
`3
`
`Carlos M. Tellez
`
`Reg. No. 48,638
`(202) 408-4123
`
`|nnoPharma Exhibit 1087.0003
`
`
`
`Attorney Docket No. 11285.0056-01000
`
`PATENT
`
`IN THE UNITED STATES PATENT AND TRADEMARK OFFICE
`
`Commissioner for Patents
`
`P.O. Box 1450
`
`Alexandria, VA 22313-1450
`
`Prior Application Art Unit: 1628 Prior Application Examiner: San Ming R. Hui
`
`Commissioner: This is a request for filing a
`
`[XI Continuation |:I Continuation-in-Part [:1 Divisional Application under 37 C.F.R.
`§ 1.53(b) of pending prior Application No. 12/285,887 filed October 15, 2008 of John R.
`EVANS and Rosalind U. GRUNDY for FORMULATION.
`
`1.
`
`IX
`
`Enclosed is a complete copy of the prior application including the oath or
`Declaration and 2 sheets of drawings, as filed as a Substitute
`Specification on March 3, 2010, which corresponds to the subject matter
`as originally filed. I hereby verify that the attached papers are a true copy
`of prior Application No. 12/285,887 as filed on March 3, 2010, which
`corresponds to the subject matter as originally filed on October 15, 2008,
`which is incorporated herein by reference.
`
`Enclosed is a Request for Non-Publication of Application and Certification
`Under 35 U.S.C. § 122(b)(2)(B)(i).
`
`A Preliminary Amendment is enclosed.
`
`Enclosed is a Certification and Request for Prioritized Examination Under
`35 U.S.C. § 1.102(e).
`
`|:|
`
`[Z
`
`IXI
`
`2.
`
`3
`
`4.
`
`5.
`
`E The filing fee is calculated on the basis of the claims existing in the prior
`application as amended in the Preliminary Amendment filed herewith.
`
`Search Fee
`
`Basic Utility Application Filing Fee
`
`Examination Fee
`
`|nnoPharma Exhibit 10870004
`
`
`
`
`
`Application No.: Unassigned
`Attorney Docket No.: 11285.0056-01000
`Page 2 of 3
`
`
`
`—I-_
`IT
`
`
`
`
`
`
`
`
`_-100+50=_*x$310
`
`
`
`Size Fee: Paper Filing
`Total Application Pages
`(specification, drawings, printed
`
`*Rounded up to next whole number
`sequence or computer listing,
`
`relimina
`amendment
`Additional Fee for Paper
`Filing New Application
`
`(DELETE if filing new application
`via EFS Web - fee not required for
`EFS new application
`
`submissions
`Size Fee: EFS-Web Filing
`Total Application Pages
`(specification, drawings, printed
`sequence or computer listing,
`reliminar amendment
`
`
`
`
`
`
`
`
`25X.75-100+50=O*x$31O
`
`‘Rounded up to next whole number
`
`$
`
`135°-0°
`
`
`
`
`
`
`T $
`
`
`
`
`Publication Fee under 35 U.S.C. § 1.18(d)
`
`TOTAL FEES DUE
`
`$
`
`$
`
`4-8°”-0°
`300.00
`
`6,480.00
`
`6.
`
`7.
`
`IX]
`
`IX]
`
`The fee of $ 6,480.00 is submitted herewith.
`
`The Commissioner is hereby authorized to charge any fees which may be
`required, including fees due under 37 C.F.R. § 1.16, and any other fees
`due under 37 C.F.R. § 1.17, or credit any overpayment during the
`pendency of this application to Deposit Account No. 06-0916.
`
`8.
`
`[I
`
`New acceptable drawings are enclosed.
`
`|nnoPharma Exhibit 1087.0005
`
`
`
`
`
`
`
`
`
`Application No.: Unassigned
`Attorney Docket No.: 11285.0056-01000
`Page 3 of 3
`
`9.
`
`X The prior application is assigned of record to: Astrazeneca AB as
`indicated by the assignments recorded at reel 011635, frame 0063 on
`March 27, 2001 and at reel 015906, frame 0402 on October 18, 2004.
`
`10.
`
`IX
`
`Priority of Application No. 0000313.7, filed on January 10, 2000 and
`Application No. 0008837.7, filed on April 12, 2000, both in Great Britain
`are claimed under 35 U.S.C. § 119. A certified copy
`
`11.
`
`12.
`
`I3
`
`XI
`
`CI is enclosed or
`
`IE is on file in the prior application.
`
`Small entity status is appropriate and applies to this application.
`
`The power of attorney in the prior application is to FINNEGAN,
`HENDERSON, FARABOW, GARRETT & DUNNER, L.L.P., Customer No.
`22,852.
`
`13.
`
`I:
`
`A Listing Under 37 C.F.R. § 1.32(c)(3) of Ten or Fewer Practitioners to
`be Recognized by the PTO as Being of Record is attached.
`
`14.
`
`|:|
`
`The power appears in the original declaration of the prior application.
`
`15. X Since the power does not appear in the original declaration, a copy of the
`power in the prior application is enclosed.
`
`16.
`
`X]
`
`Please address all correspondence to FINNEGAN, HENDERSON,
`FARABOW, GARRETT and DUNNER, L.L.P., Customer Number 22,852.
`
`If any extension of time is necessary for the filing of this
`PETITION FOR EXTENSION.
`application, including any extension in parent Application No. 12/285,887, filed
`October 15, 2008, for the purpose of maintaining copendency between the parent
`application and this application, and such extension has not othen/vise been requested,
`such an extension is hereby requested, and the Commissioner is authorized to charge
`necessary fees for such an extension to Deposit Account No. 06-0916. A duplicate
`copy of this paper is enclosed for use in charging the deposit account.
`
`FINNEGAN, HENDERSON, FARABOW,
`GARRETT & DUNNER, L.L.P.
`
`Dated: September 4, 2012
`
`By:
`
`/
`
`3
`
`Carlos M. Tellez
`
`Reg. No. 48,638
`(202) 408-4123
`
`|nnoPharma Exhibit 1087.0006
`
`
`
`
`_.____..__._,-_...-...__.....4
`...._....-a.‘,_______:_é.___,,-.__._fi_.
`
`1
`
`;70635/Us
`*
`FOR UTIUTYIDESIGN
`.)
`.
`CIPIPCT NATIONALIPLANT
`ORIGINALISUBSTITUTEISUPPLEMENTAL
`DECLARATIONS
`’
`
`“_
`
`C
`
`RULE ea (37 c.r=.n -
`.ORNEY
`DECLARATION mo POWEI
`,.
`.~-.,
`FOR PATENT APPLICATION
`IN THE utirreo STATES PATENT AND TRADEMARK ot=i_=Icrs
`
`_
`PM.& 5 .
`FORM
`
`\__
`
`As a below named inventor. I hereby declare that my residence. post office address and oitizenshtp are as stated below next to my name, an 1
`believe lam the orlglnal. first and sole Inventor (it only one name Ls listed below) or an original. firs! andjoint inventor (it plural names are listed
`below) at the subject matter which is claimed and lor which a patent is sought on the |NVENTlON ENTITLED
`FORMULATION
`
`the specification of which (gd_Eg_applicable &)$(_E_S.)_1
`A. CI is attached hereto.
`x
`'
`' as U.S. Application No.
`-)
`B. E] was filed on
`BOX(ES)
`
`“
`-) C. [3 was liled as PCT International Application No. PCTI
`I
`-)
`.
`.
`L& was amended on
`lherebystatathatlhave mvlewedartdmdorstartdttteconterttsotttteaboveldentified specificat£on.lndudng theelairnaasarnerxdedbyanyamendment reterredto
`above. Iadcnowtedgetnodutytodsdosoalllntonnationknowntomotobematerlaltopatentabu‘lityssdefinedln37c.F.R. 1.56. Eaaceptn.snotedbelow.llterebyclatm
`loreignpdoritybenclits under35U.s.c. 119(a)-(d)or3s5(b)olanylorei9n application(s)1or—palentorlnvento(s eertificate.or365(a)olanyPCTlntsmao'onal
`.
`AOp_flafia\whlch'deslgnatedatleastoneomercumuymanttwUnuedStat§. Bstadbelotvandhavealsolderttifiedbelowanyloreignapplkaflonlorpatemorhtveruofs -
`cemtlcato.orPC‘l'lntemationalAppl'ncation.lilodbymeormyasslgneedisclosinglies:biednunerdaknedhdtisappEea6onmdhavhgafitingdate(1)belommatd
`thoapplimtiononwhichprioritylsclalmed.or(2)ltnopr1oritydairnod.be1orethelilirtgdalaolthiaoppllcatiort:
`
`.
`
`I
`
`on
`
`j___.DatePatented
`
` %e_is_tL-a.44-
`“Mb
`@133: v eatflrglae £d_4x_orlN0.T...clalmed
`OO00313.7
`GB
`10 January 2000
`'
`,
`'
`_
`00O8837.7’
`ca
`12 April 2000
`
`_
`
`
`
`_
`_
`1-,. no--v
`-
`lu- »-
`-..L>' I
`--
`.lh'l'MA-".‘
`
`
`Eu-.-qatns noted below.l herebydaimdornestlcpriority
`t'¢under3SU.S.C. 119(e)or12oandor365(c)ottholndicat_edUnltodstates uppliatlons Istedbelowand
`PC‘Ti,IttematlonalapplicatiorutistedabovoorbelowInd.lllhBlsnoonfirwadon-h¢an(cW)applhadomhmlunmesubiednudufisdosoduwdaknedhmB
`appllca6onlsinadditiorttothattisdosedlr1su¢:ttprlorapp@tions.ladmofiedgethedmytoctisdosetfllnlonnafionknowntometobematorlaltopatentablltyas
`defined in 37 C.F.R. 1.56 which became available between the tiling data of eadt sud: prior appliationjand the national or PCT International filing date at this
`.__.___ .ant>licalion:___._.._._..______.__._..____.__
`-
`
`
`
`
`
`ERIORI U.S. PROVlSlON5l_., QONPBOVISIONAL AND/OR fig! APPLlCATlON(S|
`Aggllcatlon No. (series codelserlal no.)
`Da1IMONTHI'Year Fllg
`
`_
`Status
`‘
`gending, abandoned, patented
`
`Erlorlg NQT Claimed
`
`thereby declare that all staternerue madeherelnolmyownlmowledgo are wound tnatall statements madeonlnlorrnatlonandbelidare believedtobe true: and
`turmorthattnese statementswmumadewitttthelmowledgettmtwllllullalsestatementsusduuikesomadoamptmlmablebyfineorhtpdsunnermubodumder
`section 1001 ol‘l"nle laoltheunitedstatescodecndthatsuchwilllullalsestaternentsntayjeopardlze thevalldityottho iuaplicationorartypaterttlssuodttieraon.
`
`AndlherebyaapolntPillsburyMar£son&Stnm u.P.lntellec¢ual Propertyeroup. 1100NewYor1rAvenue. N.W.. Ninth Floor. EastTower.Washi09l0fl. D.c.2ooos<a91a.
`telephononurnber(202)8616000(wwhanaloormumlca6orsummbetfJreded).uIdmebelow«arMdpersors(dtlw sameaddressfincfividualtyartdcollectivelymy
`attorneystoprosecutethisappfiatiortartdtotransaetallbusinesslnttIePatentandTradanarkOlticeoonnededtl1ena-withutdwidndtorestfltirtgpatermutdlhereby
`authorlzotherntodeletenarneslnurnbersbdowotpersonsmbrtgawimmeirfimutdtonauurdymhstmdiunhunartdoamuniamémdtywitrdu
`puwdaxmadmmwymmvmganludonduhwidtflstsendskemflsasommanuuwmmmfldtlherebydeclarethatlltavooortsentedalterlulldkdowm
`lobomprasontedunlasluntillhstruadteaboiofinnandlorabdowananeyhwritingtomeoontrary.
`'
`Paul N. Kokulis
`16773
`Dale 8. Lazar
`28872
`Mark G. Paulson
`Raymond F. Uppitt
`17519
`Paul E. White, Jr.
`32011
`Stephen C. Glazier
`G. uoyd Knight
`17698
`Glenn J. Perry
`~
`_ 2868
`Pam F. Mccuade
`Carl G. Love
`18781
`Kendnewl-l. Cotton
`30368
`Ruth N. Morduch
`
`G. Paul Edgell
`
`Lynn F. Ecdeston
`Tu-no1hy.l. Klirna
`DavldA.
`
`24238
`
`35861
`34852
`$95
`
`Richard H. Zaillen
`
`Roger R. wise
`Jay M. Ftrkelstdn
`AnitaM.l<'itlq:ta1rid<
`
`30793 Michael R. Ozwonayk
`31361 W. Patrick Bengtsson
`31542
`Jacks. Barufka
`31044
`Adam R. Hess
`
`27248
`
`31204
`21082
`32617
`
`36787
`32456.
`37087
`41835
`
`_
`
`I_
`
`./
`
`Kevin F. Joyce
`
`20508
`
`18221
`George M. sirtlla
`25323
`Donald J. Bird
`25872
`PeterW.Gowdey‘
`lNVENTOR'S SIGNATURE:
`
`
` 1
`
`Vnitead. kindom
`
`-. .
`
`;
`
`.
`
`._
`
`=
`
`Post Office Address
`include 5 Code
`
`‘
`Zilatlllllij
`
`'
`
`- FOR ADDITIONAL INVENTORS. ‘X’ box D 3”’ proceed on the attached page to list each additional inventor-
`CI See additional foreign priorities on attached page (incorporated herein by reference).
`Atty. Dkt. No.
`
`PM
`
`___._..
`
`'
`
`(M#)
`
`'
`
`PAT-I16 nest‘
`
`|nnoPharma Exhibit 1087.000?
`
`
`
`IN THE UNITED STATES PATENT AND TRADEMARK OFFICE
`
`Attorney Docket No. 11285.0056-00000
`
`PATENT
`
`in re Application of:
`
`John R. Evans et al.
`
`Application No.: 12/285,887
`
`Filed: October 15, 2008
`
`For:
`
`FORMULATION
`
`Commissioner for Patents
`P.O. Box 1450
`Alexandria, VA 22313-1450
`
`Sir:
`
`Group Art Unit: 1628
`
`Examiner: HUI, San Ming R.
`
`Confirmation No.2 1199
`
`‘ax/\/x/\/\/\.z\/\/\4
`
`REVOCATION OF POWER OF ATTORNEY
`
`STATEMENT UNDER 37 C.F.R. § 3.73(b)
`AND GRANT OF NEW POWER OF ATTORNEY
`
`The undersigned, a representative authorized to sign on behalf of the assignee
`
`owning all of the interest in this patent application, hereby revokes all previous powers
`
`of attorney or authorization of agent granted in this application before the date of
`
`execution hereof.
`
`As required by 37 C.F.R. § 3.73(b), the undersigned verifies that Astrazeneca AB
`
`is the assignee of the entire right, title, and interest in the patent application identified
`
`above by virtue of an assignment from the inventors recorded in parent Application
`
`No. 10/872,784 in the U.S. Patent and Trademark Office at Reel 015906, Frame 0402.
`
`The undersigned representative of the Assignee hereby grants its power of
`
`attorney to the patent practitioners associated with FINNEGAN, HENDERSON,
`
`FARABOW, GARRETT & DUNNER, L.L.P., Customer Number 22,852, to prosecute
`
`|nnoPharma Exhibit 1087.0008
`
`
`
`Application No.: 12/285,887
`Attorney Docket No.: 112850056-00000
`
`this application and to transact all business in the Patent and Trademark Office
`
`connected therewith, and to receive the Letters Patent.
`
`Please send all future correspondence concerning this application to Finnegan,
`
`Henderson, Farabow, Garrett & Dunner, L.L.P., Customer No. 22,852.
`
`Dated;
`
`27 May 2011
`
`By:
`
`~
`
`Name:
`
`DR ALLEN F GILES
`
`Title:
`
`AUTHORISED REPRESENTATIVE
`
`Astrazeneca AB
`
`|nnoPharma Exhibit 1087.0009
`
`
`
`i_
`
`CERTIFICATION AND REQUEST FOR PRIORITIZED EXAMINATION
`
`_l
`
`‘TFirst Named inventor
`
`John R. Evans
`
`FORMULATION
`
`UNDER 37 CFR1.102_(gL
`
`Title
`lg Invention
`APPLICANT HEREBY CERTIFIES THE FOLLOWING AND REQUEST PRIORITIZED EXAMINATION
`FOR THE ABOVE—IDENTIFIED APPLICATION.
`
`TNonprovisiona| Application l Unknown
`
`Number (if knowm:_
`
`'—i
`
`1.
`
`2.
`
`3.
`
`i.
`
`The processing fee set forth in 37 CFR 1.17(i), the prioritized examination fee set forth in 37 CFR
`1.17(c), and if not already paid, the publication fee set forth in 37 CFR 1.18(d) have been filed with
`the request. The basic filing fee, search fee, examination fee, and any required excess claims and
`application size fees are filed with the request or have already been paid.
`
`The application contains or is amended to contain no more than four independent claims and no
`more than thirty total claims, and no multiple dependent claims.
`
`The applicable box is checked below:
`
`I. ® Ori
`
`inal A lication Track One - Prioritized Examination under 1.102 e 1
`
`
`
`(a) The application is an original nonprovisional utility application filed under 35 U.S.C. 111(a).
`This certification and request is being filed with the utility application via EFS-Web.
`___oR___
`
`(b) The application is an original nonprovisional plant application filed under 35 U.S.C. 111(a).
`This certification and request is being filed with the plant application in paper.
`
`ii.
`
`An executed oath or declaration under 37 CFR 1.63 is filed with the application
`
`ll. El Re uest for Continued Examination - Prioritized Examination under 1.102 e 2
`
`A request for continued examination has been filed with, or prior to, this form.
`
`if the application is a utility application, this certification and request is being filed via EFS-Web.
`
`The application is an original nonprovisional utility application filed under 35 U.S.C. 111(a), or is a
`national stage entry under 35 U.S.C. 371.
`
`This certification and request is being filed priorto the mailing of a first Office Action responsive to
`the request for continued examination.
`
`No prior request for continued examination has been granted prioritized examination status under
`37 CFR 1.102(e)(2).
`
`i.
`
`ii.
`
`iii.
`
`iv.
`
`v.
`
`The Commissioner is hereby authorized to charge any additional filing fees, including any fees necessary
`to complete the Track 1 regu_irements, to Deposit Account No. 06-0916.
`_i
`/‘
`
`L1/\,\, M ‘_’ _L:/
`
`O‘i-$t=:(>-Z0l’Z-
`
`Carlos M.Tel|ez
`
`Reg No.2 48 638
`FINNEGAN, HENDERSON, FARABOW, GARRETT & DUNNER, LLP
`202-408-4000
`
`|nnoPharma Exhibit 1087.001O
`
`
`
`Attorney Docket No. 11285.0056-01000
`
`PATENT
`
`IN THE UNITED STATES PATENT AND TRADEMARK OFFICE
`
`In re Application of:
`
`John R. EVANS, et al.
`
`Application No.: To be Assigned
`
`Filed: Herewith
`
`For:
`
`FORMULATION
`
`Commissioner for Patents
`P.O. Box 1450
`
`Alexandria, VA 22313-1450
`
`Commissioner:
`
`\./\/\y\/\/\/\/\y¢
`
`Parent Group Art Unit: 1628
`
`Parent Examiner: San Ming R. Hui
`
`VIA EFS-WEB
`
`PRELIMINARY AMENDMENT
`
`Please amend the above-identified patent application as follows:
`
`Amendments to the Specification are included in this paper.
`
`Amendments to the Claims are reflected in the listing of claims in this paper.
`
`|nnoPharma Exhibit 1087.0011
`
`
`
`Application No.: Unassigned
`Attorney Docket No.: 11285.0056-01000
`
`AMENDMENTS TO THE SPECIFICATION
`
`Please amend this application, by replacing the paragraph on page 1, line 4-8
`
`with the following paragraph:
`
`This application is a Continuation Application of copending U.S. Patent
`
`Application No. 12/285 887 filed on October 15 2008 which claims benefit of U.S.
`
`Patent Application No. 10/872,784, filed June 22, 2004, now U.S. Patent No. 6 774 122
`
`which claims benefit of U.S. Patent Application No. 09fl56,291, filed January 9, 2001,
`
`now U.S. Patent No. 7,456,160 which claims the benefit of Great Britain Application No.
`
`0008837.7 filed April 12, 2000 and Great Britain Application No. 000313.7 filed January
`
`10, 2000, all ef—whieh five applications are incorporated herein by reference in their
`
`entireties.
`
`|nnoPharma Exhibit 1087.0012
`
`
`
`Application No.: Unassigned
`Attorney Docket No.: 11285.0056-01000
`
`AMENDMENTS TO‘ THE CLAIMS
`
`Please add new claims 24-43. Please also cancel claims 1-23 without prejudice
`
`or disclaimer. This listing of claims will replace all prior versions and listings of claims in
`
`the application.
`
`Claims 1-23 (Cancelled)
`
`24.
`
`(New) A method for treating a hormonal dependent benign or malignant disease
`
`of the breast or reproductive tract comprising administering intramuscularly to a
`
`human in need of such treatment a formulation comprising:
`
`about 50 mgml" of fulvestrant;
`
`a mixture of from 17 — 23% w/v of ethanol and benzyl alcohol;
`
`12 - 18% w/v of benzyl benzoate; and
`
`a sufficient amount of castor oil vehicle;
`
`wherein the method achieves a blood plasma fulvestrant concentration of at least
`
`2.5 ngml“ for at least two weeks.
`
`25.
`
`(New) The method of claim 24, wherein formulation comprises a mixture of
`
`from 19 — 21% w/v of ethanol and benzyl alcohol and 14 - 16% w/v of benzyl
`
`benzoate.
`
`26.
`
`(New) The method of claim 24, wherein formulation comprises:
`
`about 10% w/v of ethanol;
`
`|nnoPharma Exhibit 10870013
`
`
`
`Application No.: Unassigned
`Attorney Docket No.: 11285.0056-01000
`
`about 10% w/v of benzyl alcohol; and
`
`about 15% w/v of benzyl benzoate.
`
`27.
`
`28.
`
`29.
`
`30.
`
`31.
`
`32.
`
`33.
`
`(New) The method of claim 24, wherein the blood plasma fulvestrant
`
`concentration is at least 8.5 ngml“.
`
`(New) The method of claim 24, wherein the hormonal dependent benign or
`
`malignant disease of the breast or reproductive tract is breast cancer.
`
`(New) The method of claim 24, wherein the blood plasma fulvestrant
`
`concentration is attained for at least four weeks.
`
`(New) The method of claim 24, wherein the method comprises administering
`
`intramuscularly to a human in need of such treatment 5 ml of the formulation.
`
`(New) The method of claim 24, wherein the method further comprises once
`
`monthly administration of the formulation.
`
`(New) The method according to claim 24, wherein the formulation is
`
`administered in a divided dose.
`
`(New) The method of claim 26, wherein the hormonal dependent benign or
`
`malignant disease of the breast or reproductive tract is breast cancer and the
`
`blood plasma fulvestrant concentration is attained for at least 4 weeks.
`
`34.
`
`(New) A method fortreating a hormonal dependent benign or malignant disease
`
`of the breast or reproductive tract comprising administering intramuscularly to a
`
`human in need of such treatment a formulation consisting essentially of:
`
`-4-
`
`|nnoPharma Exhibit 1087.0014
`
`
`
`Application No.: Unassigned
`Attorney Docket No.: 11285.0056-01000
`
`about 50 mgml" of fulvestrant;
`
`a mixture of from 17 — 23% w/v of ethanol and benzyl alcohol;
`
`12 - 18% w/v of benzyl benzoate; and
`
`a sufficient amount of castor oil vehicle;
`
`wherein the method achieves a blood plasma fulvestrant concentration of at least
`
`2.5 ngml" for at least two weeks.
`
`35.
`
`(New) The method of claim 34, wherein formulation consists essentially of a
`
`mixture of from 19 — 21% w/v of ethanol and benzyl alcohol and 14 - 16% w/v of
`
`benzyl benzoate.
`
`36.
`
`(New) The method of claim 34, wherein formulation consists essentially of:
`
`about 10% w/v of ethanol;
`
`about 10% w/v of benzyl alcohol; and
`
`about 15% w/v of benzyl benzoate.
`
`37.
`
`38.
`
`39.
`
`(New) The method of claim 34, wherein the blood plasma fulvestrant
`
`concentration is at least 8.5 ngml".
`
`(New) The method of claim 34, wherein the hormonal dependent benign or
`
`malignant disease of the breast or reproductive tract is breast cancer.
`
`(New) The method of claim 34, wherein the blood plasma fulvestrant
`
`concentration is attained for at least four weeks.
`
`|nnoPharma Exhibit 10870015
`
`
`
`Application No.: Unassigned
`Attorney Docket No.: 11285.0056-01000
`
`40.
`
`41.
`
`42.
`
`43.
`
`(New) The method of claim 34, wherein the method comprises administering
`
`intramuscularly to a human in need of such treatment 5 ml of the formulation.
`
`(New) The method of claim 34, wherein the method further comprises once
`
`monthly administration of the formulation.
`
`(New) The method according to claim 34, wherein the formulation is
`
`administered in a divided dose.
`
`(New) The method of claim 36, wherein the hormonal dependent benign or
`
`malignant disease of the breast or reproductive tract is breast cancer and the
`
`blood plasma fulvestrant concentration is attained for at least 4 weeks.
`
`|nnoPharma Exhibit 10870016
`
`
`
`Application No.: Unassigned
`Attorney Docket No.: 11285.0056-01000
`
`l. Amendments to the specification
`
`REMARKS
`
`Applicants amended the specification to insert the required reference to the
`
`priority applications, for which benefit is claimed.
`
`ll. Status of the claims and amendments
`
`Upon entry of the instant amendments, claims 24-43 will be pending in this
`
`application. Claims 1-23 are being cancelled in this Preliminary Amendment without
`
`prejudice or disclaimer. Claims 24-33 are directed to methods for treating a hormonal
`
`dependent benign or malignant disease of the breast or reproductive tract comprising
`
`administering intramuscularly to a human in need of such treatment a formulation
`
`comprising various components. Claims 34-43 are identical to claims 24-33 except that
`
`the phrase “formulation consisting essentially of’ replaces the phrase “formulation
`
`comprising” the various components.
`
`New claim 24 finds support, for example, in original claim 21. The recitation in
`
`claim 24 regarding “5O mg ml“ of fu|vestrant” finds support, for example, in the
`
`specification at p. 18, line 12. The recitation regarding “a mixture of from 17 — 23% w/v
`
`of ethanol and benzyl alcohol” finds support, for example, in the specification at p. 9.
`
`II. 18-26. The recitation regarding “12 - 18% w/v of benzyl benzoate” finds support, for
`
`example, in the specification at p. 10, I. 22 to p. 11, I. 9. The recitation regarding “a
`
`sufficient amount of castor oil vehic|e” finds support, for example, in the specification at
`
`_ 7 _
`
`|nnoPharma Exhibit 1087.001?
`
`
`
`Application No.: Unassigned
`Attorney Docket No.: 11285.0056-01000
`
`p. 8, II. 14-20. The recitation regarding “significant blood plasma fulvestrant
`
`concentration of at least 2.5 ngml'1 for at least two weeks” finds support, for example, in
`
`the specification at p. 8, II. 14-20 and p. 12, II. 20-23.
`
`New claim 25 finds support, for example, in the specification at p. 9, II. 13-26.
`
`New claim 26 finds support, for example, in the specification at p. 18, ll. 9-11. New
`
`claim 27 finds support, for example, in the specification at p. 12, II. 20-23. New claim
`
`28 finds support, for example, in the specification at p. 16, II. 20-27. New claim 29 finds
`
`support, for example, in the specification at p. 12, II. 24-28. New claim 30 finds suppolt,
`
`for example, in the specification at p. 12, II. 29-31. New claim 31 finds support, for
`
`example, in the specification at p. 7, II. 14-19. New claim 32 finds support, for example,
`
`in the specification at p. 12, II. 29-31. New claim 33 finds support, for example, in the
`
`specification at p. 16, II. 20-27 and p. 12, II. 24-28.
`
`Because claims 34-43 are identical to claims 24-33 except for the transitional
`
`phrase (“consisting essentially of” instead of “comprising”), the same disclosure from the
`
`instant specification cited above for claims 24-33 provides support for claims 34-43.
`
`The instant amendments do not add new matter.
`
`|nnoPharma Exhibit 10870018
`
`
`
`Application No.: Unassigned
`Attorney Docket No.: 11285.0056-01000
`
`Please grant any extensions of time required to enter this paper and charge any
`
`additional required fees to Deposit Account No. 06-0916.
`
`Respectfully submitted,
`
`FINNEGAN, HENDERSON, FARABOW,
`GARRETT & DUNNER, L.L.P.
`
`Dated: September 4, 2012
`
`By: C11»
`
`M /2 /
`
`Carlos M. Téllez
`
`Reg. No. 48,638
`(202) 408-4123
`
`|nnoPharma Exhibit 10870019
`
`
`
`Z70635
`
`FORMULATION
`
`CROSS-REFERENCE TO RELATED APPLICATIONS
`
`This application is a Continuation Application of copending U.S. Patent Application
`
`No. 10/872,784, filed June 22, 2004, which claims benefit of U.S. Patent Application No.
`
`09/756,291, filed January 9, 2001 which claims the benefit of Great Britain Application No.
`
`0008837.7 filed April 12, 2000 and Great Britain Application No. 0000313.7, filed January
`
`10, 2000, all of which are incorporated herein by reference in their entireties.
`
`BACKGROUND OF THE INVENTION
`
`V10
`
`Field of the Invention
`
`The invention relates to a novel sustained release pharmaceutical formulation adapted
`
`for administration by injection containing the compound
`
`70c-[9-(4,4,5,5,5-pentafluoropentylsulphiny1)nonyl]oestra-1,3 ,5(10)-triene-3, 17B-diol.
`
`15
`
`20
`
`25
`
`30
`
`Description of the Related Art
`
`Oestrogen deprivation is fundamental to the treatment of many benign and malignant
`
`diseases of the breast and reproductive tract. In premenopausal women, this is achieved by
`
`the ablation of ovarian function through surgical, radiotherapeutic, or medical means, and, in
`
`postmenopausal women, by the use of aromatase inhibitors.
`
`An alternative approach to oestrogen withdrawal is to antagonise oestrogens with
`
`antioestrogens. These are drugs that bind to and compete for oestrogen receptors (ER)
`
`present in the nuclei of oestrogen-responsive tissue. Conventional nonsteroidal
`
`» antioestrogens, such as tamoxifen, compete efficiently for ER binding but their effectiveness
`
`is often limited by the partial agonism they display, which results in an incomplete blockade
`
`of oestrogen-mediated activity (Furr and Jordan 1984, May and Westley 1987).
`
`The potential for nonsteroidal antioestrogens to display agonistic properties prompted
`
`the search for novel compounds that would bind ER with high affinity without activating any
`
`of the normal transcriptional honnone responses and consequent manifestations of oestrogens.
`
`Such molecules would be “pure” antioestrogens, clearly distinguished from tamoxifen-like
`
`ligands and capable of eliciting complete ablation of the trophic effects of oestrogens. Such
`
`compounds are referred to as Estrogen Receptor-Downregulators (E.R.D.). The rationale for
`
`|nnoPharma Exhibit 1087.002O
`
`
`
`Z70635
`
`the design and testing of novel, pure antioestrogens has been described in: Bowler et al 1989,
`
`Wakeling 1990a, 1990b, 1990c. Wakeling and Bowler 1987, 1988.
`
`Steroidal analogues of oestradiol, with an alkylsulphinyl side chain in the 7a position,
`
`provided the first examples of compounds devoid of oestrogenic activity (Bowler et al 1989).
`
`One of these, 7ot-[9-(4,4,5,5,5-pentafluoropentyl sulphinyl)nonyl]oestra-1,3,5-(10)triene-
`
`3,17B-diol was selected for intensive study on the basis of its pure oestrogen antagonist
`
`activity and significantly increased antioestrogenic potency over other available
`
`antioestrogens. In vitro findings and early clinical experience with
`7oL-[9—(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3-5(10)-triene-3 ,17B-diol have
`
`promoted interest in the development of the drug as a therapeutic agent for oestrogen-
`
`dependent indications such as breast cancer and certain benign gynaecological conditions.
`
`70c—[9—(4,4,5,5 ,5—Pentafluoropentylsulphinyl)nonyl]oestra— 1,3 —5(l0)—triene—3 ,17B—diol,
`
`or ICI 182,780, has been allocated the international non-proprietary name fulvestrant, which
`
`is used hereinafter. When referring to fulvestrant we include pharmaceutically-acceptable
`
`salts thereof and any possible solvates of either thereof.
`
`Fulvestrant binds to ER with an affinity similar to that of oestradiol and completely
`
`blocks the growth stimulatory action of oestradiol on human breast cancer cells in vitro; it is
`more potent and more effective than tamoxifen in this respect. Fulvestrant blocks completely
`
`the uterotrophic action of oestradiol in rats, mice and monkeys, and also blocks the
`
`uterotrophic activity of tamoxifen.
`
`10
`
`15
`
`20
`
`Because fulvestrant has none of the oestrogen-like stimulatory activity that is
`
`characteristic of clinically available antioestrogens such as tamoxifen or toremifene, it may
`
`offer improved therapeutic activity characterised by more rapid, complete, or longer-lasting
`
`tumour regression; a lower incidence or rate of development of resistance to treatment; and a
`
`25
`
`reduction of tumour invasiveness.
`
`In intact adult rats, fulvestrant achieves maximum regression of the uterus