~h-· .
`. ~
`
`'
`
`PATENT APPUCATION SERIAL NO. 10 I 0 31116ll
`
`U.S. DEPARTMENT OF COMMERCE
`PATENT AND TRADEMARK OFFICE
`FEE RECORD SHEET
`
`~1/29/2002 SNAJARRO 00000015 :003:4&4
`690.0!) OP
`108.00 OP
`
`01 FC:970
`02 ~C:%&
`
`PT0-1556
`(5/87)
`
`'U.S. GPO: 2000-468-987139595
`
`INTELGENX 1027, pg. 1
`
`

`
`~
`PATENT APPLICATION FEE DETERMINATION RECORD
`10/0~.111611
`Effective October 1, 2001
`~
`~~~~~----~--~C-LA--IM_S __ A_S_F_I_l_E_D_·_P_A_R_T_I ______________ SM_A_L~L~E-N-T-ITY--~----0-T_H_E_R_T-HA-t
`TYPE c:J
`.l:l .. r.,.;t::..;;... ____ ___ _ ...,.....,_;.;;;.;.;;:.;.;.;.;.;...;.;..._
`OR SMALL ENTIT
`TOTAL CLAIMS
`
`RATE
`
`FEE
`
`RATE
`
`FEE
`
`Application or Docket Number
`
`FOR
`
`NUMBER FILED
`
`NUMBER EXTRA
`
`BASIC FEE
`
`TOTAL CHARGEABLE CLAIMS
`
`INDEPENDENT CLAIMS
`
`:l{p minus 20::: *
`I
`*
`minus 3 =
`MULTIPLE DEPENDENT CLAIM PRESENT
`
`D
`* If the difference in column 1 is less than zero, enter "0" in column 2
`
`X$9=
`
`X42:::::
`
`+140:::
`
`TOTAL
`
`OR
`
`OR
`
`OR
`
`-
`
`BASIC FEE <fR:
`I(Ji;
`
`X$18=
`
`X84=
`
`OR
`
`+280=
`
`OR
`
`TOTAL
`
`CLAIM_$ AS AMENDED • PART II
`
`**
`
`I CD i
`
`~
`~ :z::
`
`.::~':.
`
`A./
`
`OTHER THAN
`SMALL ENTITY OR SMALL ENTITY
`
`ADD!-
`RATE TIONAL
`FEE
`
`RATE
`
`ADD!-
`TIONAL
`
`X$9=
`
`X42:::::
`
`+140=
`
`TOTAL
`ADDIT. FEE
`
`OR X$18=
`
`OR X84=
`
`OR +280=
`
`PRESENT
`EXTRA
`
`ADDI-
`RATE TIONAL
`FEE
`
`RATE
`
`ADD I-
`TIONAL
`
`X$ 9=
`
`X42=
`
`+140=
`
`TOTAL
`ADDIT FEE
`
`OR X$18=
`
`OR X84=
`
`OR +280=
`
`PRESENT
`EXTRA
`
`ADDI-
`RATE TIONAL
`FEE
`
`ADDI-
`RATE· TIONAL
`
`• If the entry 1n column 1 is less than the entry 1n column 2. write ·o· 1n column 3
`" If the "Hig~1est Number Previously Paid For" IN THIS SPACE IS l·.:ss than 20. enter 20 "
`···11 the "Highest Number Previously Paid For" IN THIS SPACE is less than 3. enter ·3"
`The "Highest Number Previously Paid For" (Total 01 Independent) is the t11ghest number found in the appropriate box in column 1.
`
`X$ 9=
`
`X42=
`
`+140=
`
`TOTAL
`ADDIT FEE
`
`OR X$18::::
`
`OR X84=
`
`OR
`
`+280::::
`TOTAL
`OR ADD IT FEE'----....
`
`FORM PT0-875
`
`(Rev 8/01)
`
`INTELGENX 1027, pg. 2
`
`

`
`APPU~(I)
`
`' ·~
`
`IND.
`
`DI!P,
`
`IND.
`
`DI!P.
`
`""'
`
`'•'
`
`. "'" .. ·~ . ' ,, "
`
`. '
`:
`
`. .· ..
`
`•
`...
`
`I
`FOP."' PT0.13SO(REV. ,_78)
`
`• ...
`
`- OEP.
`
`CLAIMS
`...._' _J~··~·-.,..r.'.....,..,~---=i'"l::-:" ~=~~==:'\'1·-:"!':··"r~,.,.···~··=· ::::":'":-..;:;.:;.;;:~--""''"l':-----...,..;r:---...... ...,.----~ 1
`!·; ···"'Aii!ii.a~r· ··;·~·;:;;· ·~~=~~
`I'"
`I'"
`'"
`r
`: j':" .. 'IIIIS:"'.:i •I'!P, -,mr.~· •DIR
`''IND •. ;"' DIP.
`'"t··-. ,-:-:;:;'<!!it~·--..
`·: 1i !':'·
`-
`;
`.lllllllili.~: '
`. . :~"."'"
`::"' .. "'
`2j·~··.
`3:
`~I .
`5' ,,
`8'.' ..
`7 .... , f-
`a.,
`9,·:;'.
`10
`11
`12
`'13
`14'
`11
`18
`17
`18
`19
`20
`21
`22
`23
`24
`25
`26
`27
`28
`29
`30
`31
`32
`33
`34
`35
`36
`37
`38
`39
`40
`41
`42
`43·
`44
`45
`46
`47
`48,.
`49'
`50
`TOiA~
`I NO,
`TOTAL
`OEP.
`Jfl,t~
`
`51
`52
`53
`54
`55
`56
`57
`58
`5~
`eo
`61
`62
`63
`64
`85
`66
`67
`68
`69
`70
`71
`72
`73
`74
`75
`76
`n
`78
`79
`80
`81
`82
`83
`84
`85
`86
`87
`88
`89
`90
`91
`92
`93
`94
`95
`96
`97
`98
`99
`100
`TOTAL
`IND •
`TOTAL
`
`·' ~· -
`
`._
`
`._
`
`~· f---- ... •
`dE},~'s "'lii&lm~~
`"-"==::....l.o---~~~
`Nalfollal8tapPJtii'/8111JfliO
`,. MAY BE USED FOR ADDmONAl. CLAIMS OR ADMENOMENTS
`~305-3831
`Barbara CamlibeD
`Nstfonsl Stage~lno
`u;S.OEPARThiENT OF COMMERCE
`Patent and Tnldelllll1t Offlc:e
`(70"3) 305-3631
`
`INTELGENX 1027, pg. 3
`
`

`
`PAT~NT COOPERATION TREATY.
`
`PCT
`
`To:
`
`From the INTERNATIONAL BUREAU
`
`PCT/US00/11130
`
`NOTIFICATION OF ELECTION
`
`(PCT Rule 61.2)
`
`Date of mailing (day/month/year)
`30 March 2001 (30.03.01)
`
`International application No.
`PCT/US00/11130
`
`International filing date (day/month/year)
`26 April 2000 (26.04.00)
`
`Applicant
`
`OREN, Peter, L. et al
`
`Commissioner
`US Department of Commerce
`United States Patent and Trademark
`Office, PCT
`2011 South Clark Place Room
`CP2/5C24
`Arlington, VA 22202
`ETATS-UNIS D'AMERIOUE
`in its capacity as elected Office
`
`Applicant's or agent's file reference
`29342/36230
`
`Priority date (day/month/year)
`03 August 1999 (03.08.99)
`
`1. The designated Office is hereby notified of its election made:
`
`0 in the demand filed with the International Preliminary Examining Authority on:
`
`D in a notice effecting later election filed with the International Bureau on:
`
`05 February 2001 (05.02.01)
`
`2. The election (8] was
`D was not
`
`made before the expiration of 19 months from the priority date or, where Rule 32 applies, within the time limit under
`Rule 32.2(b).
`
`The International Bureau of WIPO
`34, chemin des Colombettes
`121 1 Geneva 20, Switzerland
`
`Facsimile No.: (41-22) 740.14.35
`
`Form PCT/IB/331 (July 1992)
`
`Authorized officer
`
`Marie-Jose Devillard
`
`Telephone No.: (41-22) 338.83.38
`
`US0011130
`
`INTELGENX 1027, pg. 4
`
`

`
`--
`
`PATENT COOPERATION TREATY
`
`•
`
`From the INTERNATIONAL SEARCHING AUTHORITY
`
`To:
`MARSHALL O'TOOLE GERSTEIN,'
`MURRAY & BORUN
`Attn. NAPOLI ,J
`6300 Sears Tower
`233 South Wacker Drive
`Chicago, I 11 i noi s 60606-6402
`UNITED STATES OF AMERICA
`
`Applicanfs or agent's file reference
`29342/36230
`International application No.
`PCT /US 00/11130
`Applicant
`
`LILLY ICOS LLC et al.
`
`•
`
`PCT
`
`NOTIFICATION OF TRANSMITTAL OF
`THE INTERNATIONAL SEARCH REPORT
`OR THE DECLARATION
`
`(PCI Rule 44.1)
`
`Date of mailing
`(day/month/year)
`
`07/09/2000
`
`FOR FURTHER ACTION
`
`See paragraphs 1 and 4 below
`
`International filing date
`(day/month/year)
`
`26/04/2000
`
`DOCKETED: 11 l-]tQo
`
`1 . [jJ The applicant is hereby notified that the International Search Report has been established and is transmitted herewith.
`Filing of amendments and statement under Article 19:
`The applicant is entitled. if he so wishes, to amend the claims of the International Application (see Rule 46):
`
`When? The time limit for filing such amendments is normally 2 months from the date of transmittal of the
`International Search Report: however, for more details. see the notes on the accompanying sheet.
`
`Where? Directly to the
`
`International Bureau of WIPO
`34. chemin des Colombettes
`1211 Geneva 20. Switzerland
`Fascimile No.: (41-22) 740.14.35
`
`For more detailed Instructions, see the notes on the accompanying sheet.
`
`The applicant is hereby notified that no International Search Report will be established and that the declaration under
`Article 17(2)(a) to that effect is transmitted herewith.
`
`3. D
`
`With regard to the protest against payment of (an) additional fee(s) under Rule 40.2, the applicant is notified that:
`
`D
`
`D
`
`the protest together with the decision thereon has been transmitted to the International Bureau together with the
`applicant's request to forward the texts of both the protest and the decision thereon to the designated Offices.
`
`no decision has been made yet on the protest: the applicant will be notified as soon as a decision is made.
`
`4. Further actlon(s):
`
`The applicant is reminded of the following:
`
`Shortly after 18 months from the priority date. the international application will be published by the International Bureau.
`If the applicant wishes to avoid or postpone publication. a notice of withdrawal of the international application. or of the
`priority claim. must reach the International Bureau as provided in Rules 90bis.1 and 90bis.3. respectively. before the
`completion of the technical preparations for international publication.
`
`Within 19 months from the pri~~.Qatft' r:Qefi:land for international preliminary examination must be filed if the applicant
`wishes to postpone the entrf-ih\dltle-'l\atienetlphase until 30 months from the priority date (in some Offices even later).
`
`Within 20 months from the priority d<!t!=!.....,ttl~.,.aPQiicant must perform the prescribed acts for entry into the national phase
`before all designated Offic~t}~IJ\dll.drb~en elected in the demand or in a later election within 19 months from the
`priority date or could not be elected because they are not bound by Chapter If.
`
`Name and mailing address of the International Searching Authority
`
`~ European Patent Office. P.B. 5818 Patentlaan 2
`
`Nl-2280 HV Rijswijk
`Tel. (+31-70) 340-2040. Tx. 31 651 epo nl,
`___::=-Fax: (+31-70) 340-3016
`
`Authorized officer
`Catherine Humbert
`
`Form PCTiiSA/220 (July 1998)
`
`INTELGENX 1027, pg. 5
`
`

`
`NO~. FORM PCT/ISA/220
`
`These Notes are intended to give the basic instructions concerning the filing of amendments und&f' article 19. The
`Notes are based on the requirements of the Patent Cooperation Treaty, the Regulations and the Administrative Instructions
`under that Treaty. In case of discrepancy between these Notes and those requirements, the latter are applicable. For more
`detailed information, see a~ the PqT Applicant's Guide, a publication of WI PO.
`
`•
`
`In these Notes, "Article", "Rule", and "Section" refer to the provisions of the PCT, the PCT Regulations and the PCT
`Administrative Instructions respectively.
`
`INSTRUCTIONS CONCERNING AMENDMENTS UNDER ARTICLE 19
`
`The applicant has, after having received the international search report, one opportunity to amend the claims of the
`international application. It should however be emphasized that, since all parts of the International application (claims,
`description and drawings) may be amended during the international preliminary examination procedure, there is usually
`no need to file amendments of the claims under Article 19 except where, e.g. the applicant wants the latter to be published
`for the purposes of provisional protectiOn or has another reason for amending the claims before international pbulication.
`Furthermore, it should be emphasized that provisional protection is available in some States only.
`
`What parts of the International application may be amended?
`
`Under Article 19, only the claims may be amended.
`
`During the international phase, the claims may also be amended (or further amended) under Article 34 before
`the International Preliminary Examining Authority. The description and drawings may only be amended under
`Article 34 before the International Examining Authority.
`
`Upon entry into the national phase, all parts ol the international application may be amended under Article 28
`or, where applicable, Article 41.
`
`When?
`
`Wrthin 2 months from the date of transmittal of the international aearch report or 16 months from the priority
`date, whichever time limit ex~ff:t!(.!Bfi~~be noted, however, that the amendments will be considered
`as having been received on bme d ifiey are received by the International Bureau after the expiration of the
`applicable time limit but before the completion of the technical preparations for international publication
`(Rule 46.1 ).
`
`Where not to file the amendments?
`
`The amendments may only be filed with the International Bureau and not with the receivtng Office or the
`International Searching Authority (Rule 46.2).
`
`Where a demand for international preliminary examination has been/is filed, see below.
`
`How?
`
`Either by cancelling one or more entire claims, by adding one or more n- claims or by amending the text of
`one or more of the c:taims as filed.
`
`A replacement sheet must be submitted for each sheet of the claims which, on account of an amendment or
`amendments, differs from the sheet originally liled.
`
`All the claims appearing on a replacement sheet must be numbered in Arabic numerals. Where a claim is
`cancelled, no renumbering of the other claims is required In all cases where claims are renumbered, they must
`be renumbered consecutively (Admintstrative Instructions, Section 205(b))
`
`The amendments must be made In the language In which the International application Is to be published.
`
`What documents must/may accompany the amendments?
`
`Letter (Section 205(b)):
`
`The amendments must be submitted with a letter.
`
`The letter will not be published with the international application and the amended claims. It should not be
`confused with the "Stalement under Article 19(1 )" (see below, under "Statement under Article 19(1 )").
`
`The letter must be In English or French, at the choice of the applicant. Howe vet", If the language of the
`International application Is English, the letter must be In English; If the language of the International application
`Is French, the letter must be In French.
`
`Notes to Form PCT/ISA/220 (first sheet) (January 1994)
`
`BNSOOCID: <XSISA220NOENP4_1_>
`
`INTELGENX 1027, pg. 6
`
`

`
`.S TO FORM PCTIISA/220 (contlnu.
`
`The letter must indicate the differences between the claims as filed and the claims as amended. It must, in
`particular, indicate, in connection with each claim appearing in the international application (it being understood
`that identical indications concerning several claims may be grouped),whether
`
`(i}
`
`the claim is unchanged;
`
`(ii}
`
`the claim is cancelled;
`
`(iii)
`
`the claim is new;
`
`(iv)
`
`tne claim replaces one or more claims as filed;
`
`(v)
`
`the claim is the result of the division of a claim 88 filed.
`
`The following examples Illustrate the manner In which amendments must be expialned In the
`accompanying letter:
`
`(Where originally there were 48 claims and after amendment of some claims there are 51]:
`"Claims 1 to 29, 31, 32, 34, 35, 37 to 48 replaced by amended claims bearing the same numbera;
`claims 30, 33 and 36 unchanged; new claims 49 to 51 added"
`[Where originally there were 15 claims and after amendment of all claims there are 11 J:
`"Claims 1 to 15 replaced by amended claims 1 to 11. •
`(Where originally there were 14 claims and 1he amendments consist in cancelling some claims and in adding
`new claims]:
`"Claims 1 to 6 and 14 unchanged; claims 7 to 13 cancelled; new claims 15, 16 and 17 added." or
`"Claims 7 to 13 cancelled; new claims 15, 16 and 17 added; all other claims unchanged. •
`
`(Where various kinds of amendments are made):
`"Claims 1·1 0 unchanged; claims 11 to 13, 18 and 19 cancelled; claims 14, 15 and 16 replaced by amended
`claim 14; claim 17 subdivided into amended claims 15, 16 and 17; n- claims 20 and 21 added."
`
`2
`
`3.
`
`4.
`
`"Statement under article 19(1)• (Rule 46.4)
`
`The amendments may be accompanied by a statement explaining the amendments and indicating any impact
`that such amendments might have on the description and the dr-ings (which cannot be amended under
`Article 19(1)).
`
`The statement will be publtshed with the international application and the amended claims.
`
`It must be In the language In which the International apppllcatlon Is to be published.
`It must be btief, not exceeding 500 words if in English or if translated into English.
`
`It should not be confused with and does not replace the letter indicating the differences betw-n the claims
`as filed and as amended. It must ba filed on a separate sheet and must be identified as such by a heading,
`preferably by using the words "Statement under Article 19(1 ). •
`
`It may not contain any disparaging comments on the international search report or the relevance of citations
`contained in that report. Reference to citations, relevant to a given claim, contained in the international search
`report may be made only in connection with an amendment of that claim
`
`Consequence If a demand ffK International preliminary examination has already been flied
`
`If, at the time of filing any amendments under Article 1 9, a demand for international preliminary examination
`has already been submitted, the applicant must preferably, at the same lime of filing the amendments with the
`International Bureau, also file a copy of such amendments wrth the International Preliminary Examining
`Authority (s- Rule 62.2(a), first sentence)
`
`Consequence with regard to translation of the International application for entry Into the nation at phase
`
`The applicant's attention is dr-n to the fact that, where upon entry into the national phase, a translation of the
`claims as amended under Article 19 may have to be furnished to the designated/elected Offic-, instead of, or
`in addition to, the translation of the claims 88 filed.
`
`For further details on the requirements of each destgnatedlelected Office, see Volume II of the PCT Applicant's
`Guide
`
`Notes to Form PCTIISA/220 (second sheet) (January 1994)
`
`BNSOOCIO: <XS;SA220NOENP4_1_>
`
`INTELGENX 1027, pg. 7
`
`

`
`PATENT COOPERAllON TREAlY
`
`From the
`INTERNATIONAL PRELIMINARY EXAMINING AUTHORITY
`
`•
`
`•
`
`PCT
`
`To:
`
`NAPOLI, J., J.
`MARSHALL O'TOOLE GERSTEIN,
`MURRAY & BORUN
`6300 Sears Tower
`233 South Wacker Drive
`Chicago, Illinois 60606
`ETATS-UNIS D'AMERIQUE
`
`Applicant's or agent's file reference
`29342/36230
`
`International application No.
`PCT/US00/11130
`
`Applicant
`LILLY ICOS LLC et al.
`
`NOTIFICATION OF TRANSMITTAL OF
`THE INTERNATIONAL PRELIMINARY
`EXAMINATION REPORT
`(PCT Rule 71.1)
`
`Date of mailing
`(day/month/year)
`
`05.12.2001
`
`International filing date (day/month/year)
`26/04/2000
`
`Priority date (day/month/year)
`03/08/1999
`
`IMPORTANT NOTIFJCA110N
`
`1. The applicant is hereby notified that this International Preliminary Examining Authority transmits herewith the
`international preliminary examination report and its annexes, if any, established on the international application.
`
`2. A copy of the report and its annexes, if any, is being transmitted to the International Bureau for communication
`to all the elected Offices.
`
`3. Where required by any of the elected Offices, the International Bureau will prepare an English translation of the
`report (but not of any annexes) and will transmit such translation to those Offices.
`
`4. REMINDER
`
`The applicant must enter the national phase before each elected Office by performing certain acts (filing
`translations and paying national fees) within 30 months from the priority date (or later in some Offices) (Article
`39(1)) (see also the reminder sent by the International Bureau with Form PCT/IB/301 ).
`
`Where a translation of the international application must be furnished to an elected Office, that translation must
`contain a translation of any annexes to the international preliminary examination report. It is the applicant's
`responsibility to prepare and furnish such translation directly to each elected Office concerned.
`
`For further details on the applicable time limits and requirements of the elected Offices, see Volume II of the
`PCT Applicant's Guide.
`
`Name and mailing address of the I PEA/
`
`--~ European Patent Office
`"~ D-80298 Munich
`!/)J Tel. +49 89 2399 • 0 Tx: 523656 epmu d
`Fax: +49 89 2399 • 4465
`
`Form PCT/IPEA/416 (July 1992)
`
`Authorized officer
`
`Senkel, H
`
`Tel.+49 89 2399·8071
`
`INTELGENX 1027, pg. 8
`
`

`
`.ATENT COOPE~ATION T.TY
`PCT
`-------··· -·----
`.
`·,;::-.0
`;-......
`INTERNATIONAL PRELIMINARY EXAMINATIQ~rEnponaRrTT.__:_'-.:::..·-· .:_' -·
`
`I HLCJ 0 7 DEC 2001
`
`(PCT Article 36 and Rule 70)
`
`Applicant's or agent's file reference
`
`29342/36230
`
`International application No.
`PCT/US00/11130
`
`FOR FURTHER ACTION
`
`See Notification of Transmittal of International
`Preliminary Examination Report (Fonn PCT/IPEA/416)
`
`International filing date (day/month/year)
`26/04/2000
`
`Priority date (day/month/year)
`03/08/1999
`
`International Patent Classification (I PC) or national classification and IPC
`A61 K31/495
`
`Applicant
`
`LILLY ICOS LLC et al.
`
`1. This international preliminary examination report has been prepared by this International Preliminary Examining Authority
`and is transmitted to the applicant according to Article 36.
`
`2. This REPORT consists of a total of 7 sheets, including this cover sheet.
`
`D This report is also accompanied by ANNEXES, i.e. sheets of the description, claims and/or drawings which have
`been amended and are the basis for this report and/or sheets containing rectifications made before this Authority
`(see Rule 70.16 and Section 607 of the Administrative Instructions under the PCT).
`
`These annexes consist of a total of sheets.
`
`3. This report contains indications relating to the following items:
`
`!81 Basis of the report
`I
`II D Priority
`!81 Non-establishment of opinion with regard to novelty, inventive step and industrial applicability
`Ill
`IV D Lack of unity of invention
`!81 Reasoned statement under Article 35(2) with regard to novelty, inventive step or industrial applicability;
`V
`citations and explanations suporting such statement
`VI D Certain documents cited
`VII D Certain defects in the international application
`!81 Certain observations on the international application
`VIII
`
`Date of submission of the demand
`
`Date of completion of this report
`
`05/02/2001
`
`Name and mailing address of the international
`preliminary examining authority:
`~ European Patent Office
`~} D-80298 Munich
`--=Y.=-- Tel. +49 89 2399-0 Tx: 523656 epmu d
`Fax: +49 89 2399 - 4465
`
`Fonn PCT/IPEA/409 (cover sheet) (January 1994)
`
`05.12.2001
`
`Authorized officer
`
`Blott, C
`
`Telephone No. +49 89 2:399 7538
`
`INTELGENX 1027, pg. 9
`
`

`
`INTERNATIONAL PREL-ARY
`EXAMINATION REPORT
`
`I. Basis of the report
`
`•
`
`International application No. PCT/US00/11130
`
`1 . With regard to the elements of the international application (Replacement sheets which have been furnished to
`the receiving Office in response to an invitation under Article 14 are referred to in this report as "originally filed"
`and are not annexed to this report since they do not contain amendments (Rules 70. 16 and 70. 17)):
`Description, pages:
`
`1-28
`
`as originally filed
`
`Claims, No.:
`
`1-27
`
`as originally filed
`
`2. With regard to the language, all the elements marked above were available or furnished to this Authority in the
`language in which the international application was filed, unless otherwise indicated under this item.
`
`These elements were available or furnished to this Authority in the following language:
`
`, which is:
`
`0
`0
`0
`
`the language of a translation furnished for the purposes of the international search (under Rule 23.1 (b)).
`the language of publication of the international application (under Rule 48.3(b)).
`
`the language of a translation furnished for the purposes of international preliminary examination (under Rule
`55.2 and/or 55.3).
`
`3. With regard to any nucleotide and/or amino acid sequence disclosed in the international application, the
`international preliminary examination was carried out on the basis of the sequence listing:
`
`contained in the international application in written form.
`
`filed together with the international application in computer readable form.
`
`0
`0
`0
`furnished subsequently to this Authority in written form.
`0
`furnished subsequently to this Authority in computer readable form.
`0 The statement that the subsequently furnished written sequence listing does not go beyond the disclosure in
`the international application as filed has been furnished.
`0 The statement that the information recorded in computer readable form is identical to the written sequence
`listing has been furnished.
`
`4. The amendments have resulted in the cancellation of:
`
`0
`0
`0
`
`the description,
`
`the claims,
`
`the drawings,
`
`pages:
`
`Nos.:
`
`sheets:
`
`5. 0
`
`This report has been established as if (some of) the amendments had not been rr.ade, since they have been
`considered to go beyond the disclosure as filed (Rule 70.2(c)):
`
`Form PCT/IPEN409 (Boxes I-VIII, Sheet 1) {July 1998)
`
`INTELGENX 1027, pg. 10
`
`

`
`INTERNATIONAL PREL-ARY
`EXAMINATION REPORT
`
`•
`
`International application No. PCT/US00/11130
`
`(Any replacement sheet containing such amendments must be referred to under item 1 and annexed to this
`report.)
`
`6. Additional observations, if necessary:
`
`Ill. Non-establishment of opinion with regard to novelty, inventive step and industrial applicability
`
`1. The questions whether the claimed invention appears to be novel, to involve an inventive step (to be non(cid:173)
`obvious), or to be industrially applicable have not been examined in respect of:
`0
`
`the entire international application.
`
`181
`
`claims Nos. 26,27.
`
`because:
`
`IZJ
`
`the said international application, or the said claims Nos. 26 (with regard to industrial applicability) relate to
`the following subject matter which does not require an international preliminary examination (specify):
`see separate sheet
`
`0
`
`the description, claims or drawings (indicate particular elements below) or said claims Nos. are so unclear
`that no meaningful opinion could be formed (specify):
`
`D
`
`the claims, or said claims Nos. are so inadequately supported by the description that no meaningful opinion
`could be formed.
`
`181 no international search report has been established for the said claims Nos. 27 (incomplete).
`
`2. A meaningful international preliminary examination cannot be carried out due to the failure of the nucleotide
`and/or amino acid sequence listing to comply with the standard provided for in Annex C of the Administrative
`Instructions:
`
`0
`
`0
`
`the written form has not been furnished or does not comply with the standard.
`
`the computer readable form has not been furnished or does not comply with the standard.
`
`V. Reasoned statement under Article 35(2) with regard to novelty, inventive step or industrial applicability;
`citations and explanations supporting such statement
`
`1. Statement
`
`Novelty (N)
`
`Yes: Claims 5,7,10-11 '13, 17-25
`Claims 1-4,6,8-9,12,14-16,26-27
`No:
`
`Inventive step (IS)
`
`Yes: Claims
`No:
`Claims 1-27
`
`Industrial applicability (lA)
`
`Yes: Claims 1-25,27
`
`Form PCT/IPEA/409 (Boxes I-VIII, Sheet 2) (July 1998)
`
`INTELGENX 1027, pg. 11
`
`

`
`•
`
`International application No. PCT/US00/11130
`
`INTERNATIONAL PREL-NARY
`EXAMINATION REPORT
`
`No:
`
`Claims
`
`2. Citations and explanations
`see separate sheet
`
`VIII. Certain observations on the international application
`
`The following observations on the clarity of the claims, description, and drawings or on the question whether the
`claims are fully supported by the description, are made:
`see separate sheet
`
`Form PCT/IPEA/409 (Boxes I-VIII, Sheet 3) (July 1998)
`
`INTELGENX 1027, pg. 12
`
`

`
`••
`
`•
`
`INTERNATIONAL PRELIMINARY
`International application No. PCT/US00/11130
`EXAMINATION REPORT- SEPARATE SHEET
`
`SECTION Ill
`1.
`The IPEA will only formulate an assessment of novelty, inventive step and industrial
`applicability for the present claims for which an International Search Report has been
`drawn up, i.e. claims 1-26 (complete) and claim 27 (incomplete) (Rule 66.1 (e)
`PCT)(cf. form PCT/ISA/21 0, box 1.2).
`
`2.
`
`Claim 26 relates to a subject-matter considered by this authority to be covered by the
`provisions of Rule 67.1 (iv) PCT. Consequently, no opinion will be formulated with
`respect to the industrial applicability of the subject-matter of this claim (Art. 34(4)(a)(i)
`PCT).
`
`SECTION V
`3.
`a) The following documents, which were cited in the International Search Report, are
`referred to in this report; the numbering will be adhered to in the rest of the
`procedure:
`01: WO 97 03675 cited in the application
`02: WO 96 38131 cited in the application
`03: wo 98 23270
`
`b) 01 refers to the use of cGMP-phosphodiesterase inhibitors such as the compound
`mentioned in present claim 1 (=compound A), for the treatment of erectile dysfunction
`(cf. page 1, lines 1-6 and claims 1, 2). On page 13, 01 discloses tablets comprising:
`-compound A
`50 mg ( 1 Oo/o w/w)
`-polyvinyl pyrrolidone (PVP)
`150 mg (30°/o w/w)
`-polyethylene glycol (PEG)
`50 mg (1 Oo/o w/w)
`-polysorbate 80
`1 0 mg (2°/o w/w)
`-magnesium stearate
`2,5 mg (0,5°/o w/w)
`-croscarmellose sodium
`25 mg (5°/o w/w)
`-colloidal silicon dioxide
`2,5 mg (0,5% w/w)
`210 mg (42% w/w)
`-microcrystalline cellulose
`The compositions of 01 may also be administered in the form of capsules or ovules
`(cf. page 5, line 20 and pages 15-16).
`
`c) 02 is a patent application of the same applicant as 01. 02 discloses
`pharmaceutical formulations comprising a co-precipitate of compound A with
`
`Form PCT/Separate Sheet/409 (Sheet 1) (EPO-April1997)
`
`INTELGENX 1027, pg. 13
`
`

`
`••
`
`•
`
`INTERNATIONAL PRELIMINARY
`International application No. PCT/US00/11130
`EXAMINATION REPORT- SEPARATE SHEET
`
`hydroxypropyl methyl cellulose phthalate (ct. examples). 02 does not disclose
`formulations comprising compound A as a free drug, provided that compounds
`comprised in a co-precipitate do not fall within the definition of the term "free drug"
`(cf. description page 5, lines 24-27 and section VIII 7.).
`
`d) 03 refers to pharmaceutical formulations for oral administration of certain 3,4-
`diarylchromans in combinations with a hydrophilic binder and a water-soluble diluent
`(ct. page 1, lines 1-12). 03 does not refer to pharmaceutical formulations comprising
`compound A.
`
`4.
`
`Novelty
`a) 01 anticipates the subject-matter of present claim 1, since it discloses (ct. item
`3.b)) pharmaceutical formulations comprising the active compound of claim 1 as a
`free drug, PEG, which may be considered a water-soluble diluent, magnesium
`stearate and colloidal silicon dioxide, which are lubricants, PVP=povidone, which is
`a hydrophilic binder, croscarmellose sodium, which is a disintegrant, polysorbate 80,
`which is a wetting agent and microcrystalline cellulose.
`
`The subject-matter of claim 1 therefore lacks novelty over 01 (Art. 33(2) PCT).
`
`b) Item a) also applies to dependent claims 2-4, 6, 8-9, 12, 14-16 as well as to claims
`26-27.
`
`c) None of the above-cited documents discloses nor anticipates the subject-matter
`of claims 5, 7, 10-11, 13, 17-25. The subject-matter of said claims therefore is new
`over the cited prior art documents (Art. 33(2) PCT).
`
`5.
`
`Inventive step
`Dependent claims 5, 7, 10-11, 13, 17-25 do not seem to contain any technical
`feature which is not easily derivable from 01, the closest prior art document, or which
`is not a matter of routine for the skilled person. The subject-matter of said claims
`therefore appears to lack an inventive step, especially since the Applicant did not
`provide evidence for the claimed effect, i.e. enhanced dosage uniformity, stability and
`bioavailability (cf. description page 7, lines 21-28) (Art. 33(3) PCT).
`
`Fonn PCT/Separate Sheet/409 (Sheet 2) (EPO-April 1997)
`
`INTELGENX 1027, pg. 14
`
`

`
`•
`
`•
`
`INTERNATIONAL PRELiMINARY
`International application No. PCT/US00/11130
`EXAMINATION REPORT- SEPARATE SHEET
`
`6.
`
`Industrial applicability
`For the assessment of the present claim 26 on the question whether it is industrially
`applicable, no unified criteria exist in the PCT Contracting States. The patentability
`can also be dependent upon the formulation of the claims. The EPO, for example,
`does not recognize as industrially applicable the subject-matter of claims to the use
`of a compound in medical treatment, but may allow claims to a known compound for
`first use in medical treatment and the use of such a compound for the manufacture
`of a medicament for a new medical treatment.
`
`SECTION VIII
`7.
`The term " .. .free drug ... " used in claim 1 and in the description is unclear, especially
`since salts and solvates of the active compound also seem to fall within said
`definition (ct. page 4, lines 1-3 and page 5, lines 24-27) (Art. 6 PCT).
`
`8.
`
`9.
`
`The term "about" in relation to a range used in claims 4-5, 8, 10, 12-14, 19-25 and
`in the description is vague and unclear (Art. 6 PCT).
`
`Claim 16 erroneously refers back to claim 1. Claim 16 is dependent on claim 3 and
`should therefore contain, if possible at the beginning, a reference to this claim (Rule
`6.4(a) PCT).
`
`10. Claims 23 and 24 comprise all the features of claim 22 and are therefore not
`appropriately formulated as claims dependent on the latter (Rule 6.4(a) PCT).
`
`11.
`
`It seems that the following features are not referred to in the description. The claims
`are therefore not supported by the description as required by Art. 6 PCT:
`-claims 7, 9, 11, 15, 16: " ... mixtures ... "
`-claims 13, 20: " ... 5°/o ... "
`-claim 19: " ... formulation comprising: (a) ... (b) ... (e) ... 10% by weight croscarmellose
`sodium ... "
`-claims 22-24: " ... a tablet comprising ... 1 to about 20 mg (5 to about 15 mg) (5mg or
`about 10 mg) ... "
`-claim 25: " ... about 1 to about 20 mg per capsule ... "
`
`Fonn PCT/Separate Sheet/409 (Sheet 3) (EPQ.April 1997)
`
`INTELGENX 1027, pg. 15
`
`

`
`••
`
`•
`
`Page 1 of2
`
`IF3
`
`Conmtisoioncr lot Patents. IJO>< PC'I
`Umu;,d Stat~ Patent and Traoornark Offi<:e
`Washingwn. D.C. 202:!1
`w~.uepl-:1.&""
`
`U.S. APPLICATION NUMBER NO.
`10/031,464
`
`FIRST NAMED APPLICANT
`Peter L. Oren
`
`04743
`MARSHALL, GERSTEIN & BORUN
`6300 SEARS TOWER
`233 SOUTH WACKER
`CHICAGO, IL 60606-6357
`
`Date Mailed: 04/08/2002
`
`ATTY. DOCKET NO.
`29342/36230A
`INTERNATIONAL APPLICATION NO,
`PCT/US00/1 1130
`I PRIORITY DATE
`lA FILING DATE
`04/26/2000
`08/03/1999
`
`CONFIRMATION NO. 6930
`371 FORMALITIES LEITER
`111111111111111~ II~ Ill~ Ill~ II~ Ill~ Ill~ Ul~ Ul~ IIIII II~ IIIII ~Ill m1111