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`‘XHIBIT 1005 — PART 2 83FOg
`
`

`
`NoticeOf
`
`Application No.
`09/788,173
`Examiner
`
`App|icant(s)
`
`Robl
`
`I I
`
`Art Unit
`
`IIIIIIIIIIIIIIIIIIIIIII
`
`--The MAILING DA TE of this communication appears on the cover sheet with the correspondence address--
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`If not included herewith
`All claims being allowable, PROSECUTION ON THE MERITS IS (OR REMAINS) CLOSED in this application.
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`THIS NOTICE OF ALLOWABILITY Is NOT A GRANT OF PATENT RIGHTS. This application is subject to withdrawal from issue at
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`1. IX} This communication is responsive to 8/37/01
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`2. [XI The allowed c|aim(s) is/are 1-24
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`3. II The drawings filed on
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`are acceptable as formal drawings.
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`4. CI Acknowledgement is made of a claim for foreign priority under 35 U.S.C. § 119lal-(dl.
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`b) D Some*
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`of the:
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`2. I:I Certified copies of the priority documents have been received in Application No.
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`application from the International Bureau (PCT Rule 17.2(a)).
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`*Certified copies not received:
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`Applicant has THREE MONTHS FROM THE "MAILING DATE" of this communication to file a reply complying with the requirements
`noted below. Failure to timely comply will result in ABANDONMENT of this application. THIS THREE-MONTH PERIOD IS NOT
`-
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`3
`3
`EXTENDAB_LE FOR SUBMITTING NEW FORMAL DRAWINGS. OR
`SUBSTITUTE OATH_ OR DECLARATION. Thiod
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`7. I: Applicant MUST submit NEW FORMAL DRAWINGS
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`including changes required by the Notice of Draftsperson's Patent Drawing Review (PTO—948) attached
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`2) D to Paper No.
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`(b) I:I
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`including changes required by the proposed drawing correction filed
`approved by the examiner.
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`, which has been
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`(c) CI
`
`including changes required by the attached Examiner's Amendment/Comment or in the Office action of
`Paper No.
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`Identifying indicia such as the application number (see 37 CFR 1.84(c)) should be written on the drawings. The
`drawings should be filed as a separate paper with a transmittal letter addressed to the Official Draftsperson.
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`Attachmentlsl
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`1 CI Notice of References Cited (PTO-892)
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`2 D Notice of Informal Patent Application (PTO-152)
`
`3 CI Notice of Draftsperson's Patent Drawing Review (PTO—948)
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`4 D Interview Summary (PTO-413), Paper No.
`
`.
`
`5 [XI
`
`Information Disclosure Statementls) (PTO-1449), Paper Nols).
`
`2
`
`6 I:I Examiner's Amendment/Comment
`
`Material
`
`7 E] Examiner's Comment Regarding Requirementfor Deposit of Biological
`
`SEI Other
`
`8 I: Examiner's Statement of Reasonsfir Allo
`
`I /
`' ERST
`,
`R9}
`PwMA YEXAM ER
`ART UNIT 162
`
`U. S. Patent and Trademark Office
`PTO-37 (Rev. 01-01)
`
`Notice of Allowability
`
`Part of Paper No. 5
`
`0306
`
`

`
`,
`
`Sheet1 of2
`
`,ai|ab|e Copy
`Be,
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`I-ORM PTO-1449 ,_
`-NT OF COMMERCE
`u.s. DEPAR,
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`PATENT AND TRADEMARK OFFICE
`INFORMATION DISCLOSURE CITATION
`-
`1 eets ifnecessary)
`‘
`'
`
`'
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`
`ATTY. DOC _,....«'J.
`LA0050 NP
`
`No-
`
`APPLICANT
`ROBL ET AL.
`FILING DATE
`FEBRUARY 16. 2001
`
`Group
`
`
`
`U.S. PATENT DOCUMENTS
`
`DOCUMENT NUMBER
`DATE
`FILING DATE
`A M. 5,462,928
`- 5,939,560
`- 6,011,155
`- 6,110,949
`[TlE
`
`8/17/99
`
`Jenkins et al
`
`1/4/00
`
`Villhauer, E.B.
`
`8/29/00
`
`Villhauer, E.G.
`
`10/31/95 Bachovchin et al
`
`-
`
`PCT
`
`PCT
`
`PCT
`
`DATE
`DOCUMENT NUMBER
`-—K
`WO 97/40832
`1 1/6/01
`--2
`WO 99/38501
`8/5/99
`—:
`WO 99/67279
`12/29/99
`—:
`WO 00/10549
`3/2/00
`--
`9/14/00
`WO 00/53171
`_—
`WO 00/56296
`9/28/00
`--
`AL WO 00/56297
`9/28/00
`——:
`AM WO 00/69868
`1 1/23/00
`——2
`AN
`EP 1050540A2
`1 1/8/00
`--
`AO WO 034241A1
`6/15/00
`-2
`-2'0
`OTHER DOCUMENTS (Including Author, Title, Date, Pertinent pages. Etc.)
`Lin, J. et al, Proc. Natl. Acad. Sci, USA, Vol. 95, pp. 14020-14024, Nov. 1998
`
`F G H I J K
`
`AQ
`
`AR
`
`Augustyns, KJL et al, Eur. J. Med. Chem. 32, 301-309, (1997)
`
`ASI Hughes, T.E. etal, Biochemistry,'28, 11597-11603, 1999
`
`/
`/
`
`t 7
`
`’
`
`I
`
`‘EXAMINER;
`conformance .
`
`.'
`
`itial of e e__rence considered, whether or not citation is in confonnan 3' “ ' 609: Draw a line through citation if not in
`I
`ot nsidred. Include a copy of this form with the next communicatio to plicant.
`
`/
`I
`
`/
`/
`
`0307
`
`0307
`
`

`
`Best Available Copy
`—
`' -v
`FORM PTO-1449
`U.S. DEPAR1
`T OF COMMERCE
`(REV. 7-85)
`PATENT AND TRADEMARK OFFICE
`INFORMATION DISCLOSURE CITATION
`(Use several
`-
`-
`-
`if necessary)
`O \ P 5
`
`
`
`Sheet 2 of 2
`
`A
`AT1'Y. DOCIIJ.
`LA0050 NP
`3;/§8L;°1»‘g'0N N0-
`APPL|E:AN1'
`ROBL ET AL.
`FILING DATE
`FEBRUARY 16, 2001
`
`Group
`
`Yamada, M. et al, Bioorganic & Medicinal Chemistry Letters 8, 1537-1540 (1998)
`
`Tanaka, S. et al, lmmunopharmacology 40, 21-26 (1998)
`
`Li, J. et al, Archives of Biochemistry and Biophysics, Vol. 323, No. 1, pp. 148-154, Oct. 20, 1995
`
`Ashworth, D.M. et al, Bioorganic & Medicinal Chemistry Letter, Vol. 6, No. 22, pp. 2745-2748, 1996
`
`Yamada, M. et al, Bioorganic & Medicinal Chemistry Letter 8, 1537-1540 (1998)
`
`Ashworth, D.M. et al, Bioorganic & Medicinal Chemistry Letter, Vol. 6, No. 10, pp. 1163-1166, 1996
`
`Lambeir, A.-M., et al, Biochimica et Biophysica Acts, 1290, pp. 76-82 (1996)
`
`Yoshimoto, T. et al, Agric. Biol. Chem., 55(4), pp. 1135-1136, 1991
`
`Belyaev, A. et al, J. Med. Chem., 42, 1041-1052, 1999
`
`Stockel, A. et al, Peptides: Chemistry, Structure and Biology, pp. 709-710, 1996
`
`Asai, Y. et al, The Journal of Antibiotics, Vol. 50, No. 8, pp. 653-657, Aug. 1997
`
`Demuth, H.-U. et al, FEBS LETTERS, Vol. 320, No. 1, pp. 23-27, March 1993
`
`A-I
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`W U3
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`WO
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`Ohnuki, T. et al, Drugs of the Future, 24(6): 665-670, 1999
`
`Demuth, H-U. et al, Diabetes, 2000, Vol.49, suppl. 1, A102
`
`Rotherberg, P. et al, Diabetes, 2000, Vol. 49, Suppl. 1, A39
`
`IIIU!H"
`
`7
`
`0308
`
`0308
`
`

`
`CERTIFICATE OF MAILING
`
`
`CASE LA0050 NP
`
`
`
`
`
`
`
`I hereby certify that this paper (along with any paper referred to as being attached or enclosed) is being deposited with the United
`States Postal Service on the date shown below with suff ient postag
`fir
`class mail in an envelope addressed to the: Assistant
`Commissioner for Patents, Washington, D.C. 20231.
`
`Burton Rodney
`Type or print name
`
`IN RE APPLICATION OF
`
`Art Unit: 1626
`
`ROBL ET AL.
`
`Examiner: R. Gerstl
`
`APPLICATION NO: 09/788,173
`
`Batch No.1 N53
`
`FILED: FEBRUARY 16, 2001
`
`FOR: CYCLOPROPYL-FUSED PYRROLIDINE-BASED INHIBITORS OF
`DIPEPTIDYL PEPTIDASE IV AND METHOD
`
`Assistant Commissioner for Patents
`
`Washington, D.C. 20231
`
`PETITION PURSUANT TO 37 CFR §1.97gd}
`
`Sir:
`
`Consideration of the Information Disclosure Statement submitted concurrently herewith is requested.
`
`Please charge Deposit Account No. 19-3880 in the name of Bristol-Myers Squibb Company in the amount of
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`An additional copy of this paper is here enclosed. The Commissioner is hereby authorized to charge
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`any additional fees which may be required, or credit any overpayment, to Account No. 19-3880 in the name of
`
`Bristol-Myers Squibb Company.
`
`Respectfully submitted,
`
`
`
`urton Rodney
`Attorney for Applicants
`Reg. No. 22,076
`
`
`
`Bristol-Myers Squibb Company
`Patent Department
`P.O. Box 4000
`Princeton, NJ 08543-4000
`(609)2 2-4336 \
`Date:
`/J 5 )‘;ao(
`
`_
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`0309
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`

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`Best Available Copy
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`_ 5
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`CASE LAOO50 NP
` /
`CERTIFICATE OF MAILING
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`l,hereby certify that this paper (along with any paper referred to as being attached -or enclosed) is being deposited with the United
`,States Postal Service on the date shown below with suffic' nt pos
`e as first class mail in an envelope addressed to the: Assistant
`
`
`
`
`
`N
`
`Date
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`6
`
`
`
`Commissionerfor Patents. Washington, D.C. 20231.
` Burton Rodney
`
`Type or print name
`
`
`
`RE APPLICATION OF
`
`Art Unit: 1626
`
`ROBL ET AL.
`
`Examiner: R. Gerstl
`
`APPLICATION‘ NO: 09/788,173
`
`Batch No.2 N53
`
`FILED: FEBRUARY 16, 2001
`
`FOR: CYCLOPROPYL-FUSED PYRROLIDINE-BASED INHIBITORS OF
`DIPEPTIDYL PEPTIDASE IV AND METHOD
`
`Assistant Commissioner for Patents
`
`Washington, D.C. 20231
`
`SUPPLEMENTAL INFORMATION DISCLOSURE STATEMENT
`
`Sir:
`
`In accordance with 37 C.F.R. §1.56, applicants wish to call the Examiner’s attention to the
`
`references cited on the attached form(s) PTO-1449.
`
`These references were cited in a search report in a corresponding PCT International
`
`application dated October 23, 2001 that is within 3 months of the filing of this information disclosure
`
`statement. Copies of these references and the search report are enclosed‘ herewith.
`I“
`\
`A petition pursuant\to 37 C.F.R. §1.97(d) is enclosed herewith.
`
`The Examiner is requested to consider the foregoing information in relation to this
`
`application and indicate that each reference was considered by returning a copy of the initialed PTO
`
`1449 form(s).
`
`I2/21/E001 CCIII-lI.I1
`
`00000059 193880
`
`09786173
`
`01 FC':1'c36
`
`180.00 CH
`
`0310
`
`0310
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`

`
`Best wable Copy
`
`.SE LA0050 NP
`
`Certificate under 37 C.F.R.
`
`1.97 e 1
`
`I, the undersigned attorney, hereby certify that each item of information contained in this
`
`Information Disclosure Statement was cited in a communication from a foreign patent office in a
`
`counterpart foreign application not more than three months prior to the filing of this Statement.
`
`Respectfully submitted,
`
`Burton Rodney
`Attorney for Applicants
`Reg. No. 22,076
`
`Bristol-Myers Squibb Company
`Patent Department
`P.O. Box 4000
`Princeton, NJ 08543-4000
`(609) 252-4336
`
`Date: /\/\\f' 3) ywq
`
`0311
`
`

`
`_ J
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`Best
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`"
`FORM PTO-1449
`U.S. DEPARTMI:.. OF COMMERCE
`(REV. 7-85)
`PATENT AND TRADEMARK OFFICE
`INFORMATION DISCLOSURE CITATION
`(Use several sheets if necessa
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`ROBL ET AL.
`FILING DATE
`FEBRUARY 16, 2001
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`DATE
`DOCUMENT NUMBER
`
`4,254,057
`
`4,379,785
`
`5,998,463
`
`3/3/81
`
`4/12/83
`
`Day et aI
`
`Weyer et al
`
`,
`
`12/7/99
`
`Hulin et al
`
`FOREIGN PATENT DOCUMENTS
`
`
`
`OTHER DOCUMENTS (Including Author, TitIe, Date, Pertinent pages, Etc.)
`
`
`» -w l~"—-—~§s‘.‘”s“‘..'8”
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`‘I Sagnard, I. etal, Tetrahedron Letters, Vol. 36, No. 18, pp. 3149-3152, 1995.
`Tverezovsky, V.V. etal, Tetrahedron, Vol. 53, No. 43, pp. 14773-14792, 1997.
`N Hanessian, S. et al, Bioorganic & Medicinal Chem. Letters, Vol. 8, No. 16, pp. 2123-2128, Aug. 18,
`_
`_
`‘ /
`4 A
`EXAM ER
`DATE CONSIDRED
`/
`Initial ofre
`‘EXAMINER:
`not itation is in
`-
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`zfll" M P6:’ Drawa line through citation ifnot in
`conformance and not consider.
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`TENT COOPERATION TREATY ‘
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`From the INTERNATIONAL SEARC ‘
`
`To-
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`PCT
`
`
`
`ATION OF TRANSMITTAL OF
`‘ RNATIONAL SEARCH REPORT
`OR THE DECLARATION
`
`
`
`BRISTOL—MYERS SQUIBB C0.
`Attn. Algieri, Aldo A.
`P.0. Box 4000
`Lawrenceville-Princeton
`
`(PCT Rule 44.1)
`PRINCETON, NJ 08543
`
`UNITED STATES OF AMERIC*
`
`
`
`
`
`
`
`
`‘day/m°"'“’Y9a” 23/10/2001
`
`Date of mailing
`
`
`
`FOR FURTHER ACTION
`See paragraphs 1 and 4 below
`
`International filing date
`International application No.
`l"""Y""°"""Y“')
`05/03/2001
`
`
`Applicant's or agents file reference
`
`LA0050
`
`PCT/US 01/ 07151
`
`Applicant
`
`BRISTOL-MYERS SQUIBB CO .
`
`
`1. [E 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.
`
`2. D 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 the protest together with the decision thereon has been transmitted to the lntemation‘al 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 action(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 priority date, a demand for international prellmlnary examination must be filed it the applicant
`wishes to postpone the entry into the national phase until 30 months from the priority date (in some Offices even later).
`
`within 20 months from the priority date, the applicant must perform the prescribed acts for entry into the national phase
`before all designated Offices which have not been 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 ll.
`
`
`
`
`
`
`
`
`Fax: (+31—7o) 340-3016
`
`Name and mailing address of the International Searching Authority
`_— European Patent Office, P.B. 5818 Patentlaan 2
`NL-2280 HV Rijswijk
`.0 Tel. (+31—7o) 340-2040. Tx. 31651 epo nl,
`
`Authorized officer
`
`Chantal Meyer
`
`Form PCT/ISA/220 (July 1998)
`
`0313
`
`0313
`
`

`
`
`
`
`
`
`These Notes are intended to give the basic instructions conceming the filing of amendments under article 19. The
`Notes are based on the requirements of the Patent Cooperation Treaty, the Regulations and the Adninistretive Instructions
`under that Treaty. In case of discrepancy between these Notes and those requirements, the latter are applicable. For more
`detailed information, see also the PCT Applicant's Guide, a publication of WIPO.
`
`
`
`
`
`in these Notes, ‘Article’, “Rule”, and 'Section' refer to the provisions of the PCT, the PCT Regulations and the PCT
`Administrative lnstmdions respectively.
`
`
`
`
`NOTES TO FORM PCTllSAI220
`
`
`
`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 dawings) 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 publhed
`tor 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 appllcatlon 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
`The description and dawings may only be amended under
`Article 34 before the lntemational Examining Authority.
`—
`
`
`
`Upon entry into the ndional phase, all parts of the international application may be amended under Article 28
`or, where applicable, Article 41.
`
`
`
`Within 2 months from the date of transmittal of the international search report or 16 months lrom the priority
`date, whichever time limit expires later. It should be noted, however, that the amendments will be considered
`as having been received on time if they are received by the lntemational Bureau after the expiration of the
`applicable time limit but before the completion ot the technical preparations for international publication
`(Rule 46.1).
`
`
`
`
`
`
`
`Where not to tile the amendments?
`
`
`The amendments may only be filed with the International Bureau and not with the receiving Office or the
`International Searching Authority (Rule 46.2).
`
`
`
`Where a demand for international preliminary examination has been/is filed, see below.
`
`
`
` Either by cancelling one or more entire claims, by adding one or more new claims or by amendng the text or
`one or more ofthe claims 3 filed.
`
`
`
`A replacement sheet must be submitted for each sheet of the claims which, on account of an amendment or
`arnencknerrts, differs trom the sheet originally tiled.
`
`
`
`
`All the claims appearing on a replacement sheet must be numbered in Arabic numerals. Where a claim is
`cancelled, no renumbering ol the other claims is required. In all cases where claims are renumbered, they must
`be renumbered consecutively (Administrative Instructions, Section 205(b)).
`
`The amendments must be made In the language In which thelntematlonal application la to be published.
`
`_
`
`What documents must/may accompany the amendments?
`
`Letter (sedlon 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
`conlused with the ‘Statement under Article 19(1)‘ (see below, under ‘Statement under Article 19(1)‘).
`
`The letter must be In English or French, at the cholce of the appllcant. However, If the language of the
`international application is Engllsh, the letter must be In English; it the language of the lnternatlonal qapllcatlon
`is French, the letter must be In French.
`
`Notes to Fonn F’CTIlSAl22O (first sheet) (January 1994)
`
`nnreno-win. -veicMnnur\:aiD.a I \
`
`4
`
`
`
`
`0314
`
`

`
`NOTES TO FORM PCTllSAl220 (contlnued)
`
`‘lhe letter must "indicate the differences between the claims as filed and the claims as amended. It must, in
`particular, indcate. in connection with each claim appearing in the international application Gt being understood
`that identical indications concerning several claims may be grouped),whether
`(i)
`the claim is unchanged;
`
`(Ii)
`
`(iii)
`
`(iv)
`
`(v)
`
`the claim is cancelled;
`
`the claim is new;
`
`the claim replaces one or more claims as filed;
`
`the claim is the result of the division of a claim as filed.
`
`The lollowlng examples Illustrate the manner In which amendments must be explained In the
`accompanying later:
`
`1. ' [Where originally there were 48 claims and alter amendmentol some claims there are 51]:
`‘Claims 1 to 29, 31, 32. 34, 35, 37 to 48 replaced by amended claims bearing the same numbers;
`claims 30. 33 and 36 unchanged; new claims 49 to 51 added.‘
`
`[Where originally there were 15 claims and alter amencknent of all claims there are 11]:
`‘Claims 1 to 15 replaced by amended claims 1 to 11 ."
`
`[Where originally there were 14 claims and the amendments consist in cancelling aorne claims and in addng
`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 ot amendments are made]:
`‘Claims 1-10 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; new claims 20 and 21 added.‘
`
`‘Statement under article 19(1)‘ (Flute 46.4)
`
`The amendments may be accompanied by a statement explaining the amendments and indcating any impact
`that such amendments might have on the description and the ckewings (which cannot be amended under
`Article 19(1 )).
`
`The statement will be published 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 briel, not exceeding 500 words it in English or it translated into English.
`
`It should not be confused with and does not replace the letter indicating the citferenoes between the claims
`as filed and as amended. it must be 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 dparaging 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 01 that claim.
`
`consequence it a demand tor International preliminary examination has dready been tiled
`ll, at the time of filing any amendments under Article 1 9, a demand for international preliminaiy examination
`has already been submitted, the applicant must prelerably, at the same time of filing the amendments with the
`lntemational Bureau, also file a copy ct such amendments with the lntematicnal Preliminary Examining
`Authority (see Rule 62.2(a), first sentence).
`
`consequence with regard to translation of the International application for entry Into the national phase
`
`The applicant's attention is drawn 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 lurnished to the designatedlelected Offices, instead ot, or
`in addition to. the translation of the claims as filed.
`
`For further details on the requirements of each designated/elected Office, see Volume ll 01 the PCT Applicant's
`Guide.
`
`Notes to Form PCT/ISA/220 (second sheet) (January 1994)
`
`nuervvwn» -va|enoonMr\:MDA I
`
`-.
`
`5
`
`0315
`
`

`
`I
`
`_
`
`H 9A+em ccsopisrmion TREAT
`
`INTERNATIONAL SEARCH REPCRT
`
`(PCT Article 18 and Rules 43 and 44)
`
`Applicants or agents file reference
`
`LA0050
`International application No.
`
`PCT/US 01/ 07151
`Applicant
`
`F R F RTHEE see Notification of Transmittal of International Search Report
`0
`U
`(Form PCT/ISA/220) as well as, where applicable, item 5 below.
`ACTION
`International filing date (day/month/year)
`
`(Earliest) Priority Date (day/month/year)
`
`I
`
`g
`
`05/03/2001
`
`10/03/2000
`
`BRISTOL-MYERS SQUIBB CO .
`
`This International Search Report has been prepared by this International Searching Authority and is transmitted to the applicant
`according to Article 18. A copy is being transmitted to the International Bureau.
`
`sheets.
`5
`This International Search Report consists of a total of
`El
`It is also accompanied by a copy of each prior art document cited in this report.
`
`1. Basis of the report
`
`a. with regard to the language, the international search was carried out on the basis of the international application in the
`language in which it was filed, unless otherwise indicated under this item.
`
`B the international search was carried out on the basis of a translation of the international application furnished to this
`Authority (Rule 23.1 (b)).
`
`With regard to any nucleotide andlor amino acid sequence disclosed in the international application, the international search
`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.
`
`furnished subsequently to this Authority in written form.
`
`furnished subsequently to this Authority in computer readble form.
`the statement that the subsequently furnished written sequence listing does not go beyond the disclosure in the
`international application as filed has been furnished.
`the statement that the information recorded in computer readable form is identical to the written sequence listing has been
`furnished
`
`Certain claims were found unsearchable (See Box I).
`
`Unity of invention is lacking (see Box II).
`
`4. With regard to the title,
`
`the text is approved as submitted by the applicant.
`E]
`m the text has been established by this Authority to read as follows:
`CYCLOPROPYL—FUSED PYRROLIDINE—BASED INHIBITORS OF DIPEPTIDYL IV, PROCESSES FOR
`THEIR PREPARATION, AND THEIR USE
`
`5. With regard to the abstract,
`
`the text is approved as submitted by the applicant.
`E]
`D the text has been established, according to Rule 38.2(b), by this Authority as it appears in Box III. The applicant may,
`within one month from the date of mailing of this international search report, submit comments to this Authority.
`
`6. The figure of the drawings to be published with the abstract is Figure No.
`D as suggested by the applicant.
`E]
`because the applicant failed to suggest a figure.
`|:]
`because this figure better characterizes the invention.
`
`Form PCT/ISA/210 (first sheet) (July 1998)
`
`E]
`
`None of the figures.
`
`0316
`
`0316
`
`

`
`
`
`
`
`2-
`
`-
`
`.
`
`.lNTER.TlONAL SEAFtCH_REF_’ORT : tlonal-Application No _
`
`
`A. CLASSIFICATION OF SU JECT MATTER
`IPC 7
`c070209 52
`A61K31/403
`
`PCT/US 01/07151
`
`A61P3/04
`
`A61P3/06
`
`A61P3/10
`
`
`
` According to International Patent Classification (IPC) or to both national classification and IPC
`B. FIELDS SEARCHED
`
`
`
`Minimum documentation searched (classification system followed by classification symbols)
`IPC 7
`C07D
`
`
`
`
`
`Documentation searched other than minimum documentation to the extent that such documents are included in the fields searched
`
`Electronic data base consulted during the international search (name of data base and. where practical. search terms used)
`
`EPO—Internal, CHEM ABS Data
`
`
`
`
`
`C. DOCUMENTS CONSIDEFIED TO BE RELEVANT
`
`Category ‘’
`
`Citation of document, with indication, where appropriate. of the relevant passages
`
`Relevant to claim No.
`
`
`
`
`
`
`
`
`
`
`
`
`US 6 011 155 A (VILLHAUER EDWIN BERNARD)
`4 January 2000 (2000-01-04)
`abstract; claims; examples
`
`W0 99 47545 A (NANNAMAKER MARION N; BEMIS
`GUY N (US); MURCKO MARK A (US); VERTEX)
`23 September 1999 (1999-09-23)
`page 9, formula 1; page 26, especially
`lines 18-22; page 97, compounds 23d, 23h
`claims 1,6,18,19,23
`
`
`
`
`
`
`
`
`
`
`
`
`N0 99 67279 A (SCHMIDT JOERN; GLUND KONRAD
`(DE); DEMUTH HANS ULRICH (DE); HOFFMAN)
`29 December 1999 (1999-12-29)
`page 11 —page 17; claims 1,2,8—13
`
`_/__
`
`
`
`
`
`
`
`
`
`23/10/2001
`Authorized officer
`
`16 October 2001
`
`Name and mailing address of the ISA
`
`European Patent Office, PB. 5818 Patentlaan 2
`
`NL - 2280 HV Flllswijk
`Tel. (+31 -70) 340-2040. Tx. 31 651 epo nl.
`Fax: (+31—7o) 340-3016
`
`
`
`
`
`Hass, C
`
`
`
`Form PCT/ISA/210 (second sheet) (July 1992)
`
`
`
`fig‘.,
`
`page 1 of 3
`
`0317
`
`E Further documents are listed in the continuation of box C.
`° Special categories of cited documents:
`
`'A' document defining the general state of the art which is not
`considered to be of particular relevance
`'E‘ earlier document but published on or after the international
`filing date
`'L' document which may throw doubts on priority claim(s) or
`which is cited to establish the publication date of another
`.
`.
`.
`.
`.
`°""‘“'°" °' °"‘e' 5pe°'a' 'ea5°" (35 Specmed)
`'0' document reterrlng to an oral disclosure, use. exhibition or
`other means
`‘P’ document published prior to the international filing date but
`
`later than the priority date claimed
`
`
`
`E Patent family members are listed in annex.
`A
`_
`.
`g
`'T'
`later document published after the Intematlonal filing date
`or priority date and not in conflict with the application but
`cited to understand the principle or theory undenying the
`invention
`'X' document of particular relevance: the claimed invention
`
`
`cannot be considered novel or cannot be considered to
`involve an inventive step when the document is taken alone
`
`
`'Y' document of particular relevance; the claimed invention
`cannot be considered to involve an inventive step when the
`
`
`document is combined with one or more other such docu-
`ments, such combination being obvious to a person skilled
`
`in ‘he an‘
`'8.‘ document member of the same patent family
`
`Date of mailing of the lntemational search report
`Date of the actual completion of the international search
`
`0317
`
`

`
`-
`
`—
`
`INTEI-'.TIoNAL SEABCHREPOBT _,
`
`‘
`
`' In
`
`atlonalltpplication No-
`
`,.
`
`.
`
`-_
`
`.
`
`
`C.(Contlnuat|on) DOCUMENTS CONSIDERED To BE FIELEVANT
`
`
`
`US 4 379 785 A (NEYER RUDI
`12 April 1983 (1983-04-12)
`cited in the application
`claims 1,5,6
`
`ET AL)
`
`
`
`Citation ofdocument. with indicatiomwhere appropriate, 0! the relevant passage
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`EP 0 219 782 A (HOECHST AG)
`29 April 1987 (1987-04-29)
`page 1, formula (I); page 3, substructure
`K; page 16,
`line 33 to page 17,
`line 6
`claims 1,2
`
`DE.33 24 263 A (HOECHST AG)
`_ 17 January 1985 (1985-01—17)_
`claims 1,19,20
`
`DE 39 26 606 A (HOECHST AG)
`14 February 1991 (1991-02-14)
`page 2, formula (I); page 3, substructure
`(K); page 6,
`lines 62-66
`
`US 4 254 057 A (DAY JANET A ET AL)
`3 March 1981 (1981-03-03)
`column 2,
`line 26 — line 38
`
`EP 0 007 652 A (SHELL INT RESEARCH)
`6 February 1980 (1980-