Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0601
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0601
`
`

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`tes oder unsubstituiertes Phenyl steht.
`
`15
`
`23. Verbindung der Formel
`
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`
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`24. Verbindung der Formel
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`GEAENDERTESBLATT
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0602
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0602
`
`

`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0603
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0603
`
`

`
`E O5-10-2001
`
`EPOO11309
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`
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`
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`
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`
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`
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`
`GEAENDERTES BLATT
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0604
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0604
`
`

`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0605
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0605
`
`

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`
`15
`
`als hochreines, kristallines, stabiles Zwischenprodukt
`
`bei der Herstellung Von pharmazeutisch nutzlichen Verbindungen
`der Formel 2 nach Patentanspruch 3.
`
`28. Verwendung einer Verbindung nach Anspruchen 23 bis 26 als
`
`20
`
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`.
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`
`GEAENDERTESBLATT
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0606
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0606
`
`

`
`...—
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0607
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0607
`
`

`
`P‘./" "-§NT COOPERATlON'TREA.T‘ fig,
`
`—\r1 as;
`
`PCT/E P00/1 1309
`
`From the INTERNATIONAL BUREAU
`
`
`
`PCT
`
`NOTIFICATION OF ELECTION
`
`(PCT Rule 61.2)
`
` 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'AMERlOUE
`
`'
`in its capacity as elected Office
`
`‘Applicant's or agent's file reference:
`
`11012/um
`PCT/EP00/11309
`V
`
`Priority date:
`
`_
`16 November 1999 (16.11.99)
`
`_
`
`
`
`_
` Applicant:
`MEESE, Claus
`
`
`
`
`
`
`
` 1. The designated Office is hereby notified of its election made:
`
`
`
`in the demand filed with the International preliminary Examining Authority on:.
`
`
`E in a notice effecting later election filed with the International Bureau on:
`
`2.
`The election
`was
`
` j.j:.
`17 January 2001 (17.01.01)
`
`.
`
`
`
`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).
`
`
`
` Authorized officer:
`The International Bureau of WIPO
`
`34, chemin des Colombettes
`
`1211 Geneva 20, Switzerland
`
`J. Zahra
`Facsimile No.: (41-22) 740.14.35
`
`(41-22) 1338.83.38
`Form PCT/IB/331 (July 1992)
`
`
`
`3 - 503
`
`Telephone No.:
`
`
`
`Patent Owner, UCB Pharma GmbH —
`
`
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0608
`
`

`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0609
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0609
`
`

`
`Q
`
`VERTRAG I‘.-1% DIE INTERNATIONALE ZUSA
`PCT
`
`EM GEBIET DES PATENTWE
`
`A
`
`ENARBEIT
`
`INTERNATIONALEFI RECHERCHENBERICHT
`
`
`
`11012/um
`Internationales Aktenzeichen
`
`(Artikel 18 sowie Regeln 43 und 44 PCT)
`
`Aktenzeichen des Anmelders oder Anwalts
`
`siehe Mitteilung fiber die Ubermittlung des internationalen
`WEITERES
`Recherchenberichts (Formblatt PCT/ISN220) sowie, soweit
`VORGEHEN
`zutreffend, nachstehender Punkt 5
`
`Internationales Anmeldedatum
`(Frilhestes) Prioritatsdatum (Tag/Mona!/Jahr)
`(Tag/Mona I/Jahr)
`
`1 5/] 1/2000
`
`
`
`16/1]/1999
`
`
`
`
`
`PCT/EP 00/ 11309
`Anmelder
`
`
`
`SCHWARZ PHARMA AG et a1.
`
`Dieser intemationale Recherchenbericht wurde von der lnternationalen Recherchenbehcrde erstellt und wird dem Anmelder geméfi
`Artikel 18 flbermittelt. Eine Kopie wird dem Internationalen Biiro iibermittelt.
`
`Blétter.
`Dieser intemationale Recherchenbericht umfal3t insgesamt 2
`B]
`Darflber hinaus Iiegt ihm jeweils eine Kopie der in diesem Bericht genannten Unterlagen zum Stand der Technik bei.
`
`1. Grundlage cles Berichts
`
`a. Hinsichtlich der Sprache ist die internationale Recherche auf der Grundlage der internationalen Anmeldung in der Sprache
`durchgefflhrt worden, in der sie eingereicht wurde, sofern unter diesem Punkt nichts anderes angegeben ist.
`
`Die internationale Recherche ist auf der Grundlage einer bei der Behdrde eingereichten Ubersetzung der internationalen
`Anmeldung (Regel 23.1 b)) durchgefiihrt worden.
`
`b. Hinsichtlich der in der internationalen Anmeldung offenbarten Nucleotid- und/oder Aminoséuresequenz ist die internationale
`Recherche auf der Grundlage des Sequenzprotokolls durchgefiihrt worden, das
`In der Internationalen Anmeldung in Schriflicher Form enthalten ist.
`
`UCBElEIDEIDEI
`
`zusammen mit der internationalen Anmeldung in oomputerlesbarer Form eingerelcht worden ist.
`bei der Behdrde nachtragllch In schrlftlicher Form eingereicht worden ist.
`bei der Behérde nachtréglich in computerlesbarer Form eingereicht worden ist.
`
`Die Erklarung, dal3 das nachtraglich eingerelchte schrlftllche Sequenzprotokoll nicht fiber den Offenbarungsgehalt der
`internationalen Anmeldung im Anmeldezeitpunkt hinausgeht, wurde vorgelegt.
`
`Die Erklarung, daB die in computerlesbarer Form erfar3ten Inforrnationen dem schriftlichen Sequenzprotokoll entsprechen,
`wurde vorgelegt.
`
`Bestimmte Ansprfiche haben sich als nicht recherchierbar ewviesen (siehe Feld I).
`Mangelnde Einheitlichkeit der Erfindung (siehe Feld II).
`
`Hinsichtlich der Bezeichnung der Erfindung
`wird der vom Anmelder eingereichte wortlaut genehmigt.
`wurde der Wortlaut von der Behérde wie folgt festgesetzt:
`
`DB
`
`Hinsichtlich der Zusammenfassung
`
`[X]
`
`wird der vom Anmelder eingereichte Wortlaut genehmigt.
`wurde der Wortlaut nach Regel 38.2b) in der in Feld III angegebenen Fassung von der Behdrde festgesetzt. Der
`Anmelder kann der Behbrde Innerhalb eines Monats nach dem Datum der Absendung dieses international n
`Recherchenberichts
`ine Stellungnahme vorlegen.
`
`Folgende Abbildung der Zelchnungen Ist mit der Zusammenfassung zu verbffentlichen: Abb. Nr.
`El ' wie vom Anmelder vorgeschlagen
`D weil der Anmelder selbst kelne Abblldung vorgeschlagen hat.
`D w it diese Abbildung die Erfindung besser k nnzeichnet.
`
`m kelne der Abb.
`
`Formblatt PCT/ISA/210 (Blatt 1) (Juli 1998)
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0610
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0610
`
`

`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0611
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0611
`
`

`
`INTERNATIONALER RECHERCHENBERICHT
`
`lnternatlonales Aktenzelc hen
`
`'NSTANDES
`'
`A. KLASSIFIZIEHUNG DES ANMELDUNGS
`IPK 7
`C07C215 54
`CO7C219/28
`
`Nach der Internationalen Patenlklassifikalion (IPK) oder nach der nationalen Klassilikation und der IPK
`B. RECHERCHIERTE GEBIETE
`Recherchiener Mindestprflfstoff (Klassifikationssystem und Klassifikationssymbole )
`IPK 7
`CO7C
`
`Recherchierte aber nichl zum Mindesmrfifsloff gehtirende Veréffentllchungen, soweh diese umer die recherchienen Gebiele fallen
`
`Wi-ihrend der internationalen Recherche konsultierle elektronische Datenbank (Name der Datenbank und ev1I. verwendete Suchbegriffe)
`
`EPO-Interna1, WPI Data, BEILSTEIN Data, CHEM ABS Data
`
`C. ALS WESENTLICH ANGESEHENE UNTERLAGEN
`
`Bezeichnung der Veriiffentlichung, soweit erforderlich unter Angebe der in Belracht kommenden Teile
`
`Belr. Anspruch Nr.
`
`X
`
`X
`
`X
`
`W0 98 43942 A (HARALDSSON MARTIN
`‘”;PHARMACIA¥& UPJOHN AB (SE); RINGBERG ERIK
`(SE);) 8. Oktober 1998 (1998-10-08)
`Seite 76, Zeile 7,8
`Seite 36, Zeile 32,33
`
`'
`
`(«we 94 11337 A (KABI PHARMACIA AB
`;JOHANSSON ROLF ARNE (SE); MOSES PINCHAS
`(SE); N) 26. Mai 1994 (1994-05-26)
`Seite 12, Zei1e 15,16,29,30
`Seite 8, Zei1e 13-16
`
`PALMER, L. ET AL.:
`to1terodine and the
`
`"Determination of
`.:
`
`5—hydroxymety1metabo11te ..."
`J. PHARM. BIOMED. ANAL.,
`Bd. 16, 1997, Seiten 155-165, XP000995770
`Abbildung 1
`-
`
`E Siehe Anhang Patentfamilie
`Weitene Veréffenllichungen sind der Fonsetzung von Feld C zu
`enlnehmen
`'T' Spétere Veréffentlichung, die nach dem internationalen Anmeldedatum
`" Besondere Kategorien von angegebenen Veréffenllichungen
`:
`we’ dem P'i‘."'"a‘5d§“:'m "9"3"e"m°m “'°"de" is‘ .!‘"d W“ der
`‘A’ Veréffentlichung, die den allgemeinen Stand der Technik definiert,
`Anmeldung mcht kollndlerl. sondern nur zum Verstandnls des der
`aber mom als besonders bedeutsam anzusehen is‘
`'1.
`.
`d
`.
`.
`.
`.
`$n$'3:.’$"§nZ§'e9g;r33g§'5§t9en en Pmmps Oder der ‘hr zugmndehegenden
`‘E’ éineres Dokumenl, das jedoch ersl am oder nach dem internationalen
`'X' Veréffentlichung von besonderer Bedeulung; die beanspruchte Erfindung
`A"me'deda‘"'T' Vmfifienuicm w°'d°" is‘
`kann allein aufgrund clieser Veréffemlichung nicht als neu oder auf
`'L' Veréffentlichung, die geeignel ist, einen Prioritétsanspruch zweifelhaft er-
`erfinderischer Tatigkeit bemhend betrachtet werden
`scheinen zu Iassen, oder durch die das Veréffenuidnungsdatum elner
`-
`anderen im Hecherchenbericht genannten Veriiffemlichung belegi werden .Y. Verbfienmchun
`_
`-
`.
`.
`.
`g von besonderer Bedeutung, due beanspruchte Erfindung
`.
`5°" °de' d'e aus emem a"de'e" bes°"d°'°" G”-'"d 3"9°9ebe" '3‘ (“"9
`kann nicht als auf erfinderischer Tétigkeil beruhend betrachtel
`ausgefflhn)
`werden, wenn die Veréffentlichung mil einer oder mehreren anderen
`'0' V3_"5"e"""°h'-|"9- die 550'‘ 3”’ eine mflndliche 0ff8nb3"""9-
`.
`Verfiffentlichungen dieser Kalegorie in Verbindung gebrachl wind und
`elne Benutzung, eine Ausstellung oder andere Mafsnahmen beznehl
`diese ve.-b|.-mung ffir einen Fachmann nahenegend is;
`P V§;?,':§2‘a"§2gfl,%h‘flf,,‘Q’;51:12};2§L";‘:2§'}§;?;‘nt’f}2hT?A:gf:,'::,"i;'}' ‘be’ "ac"
`'5' veratrennicnung, die Milglied derselben Patentfamllie is!
`Datum des Abschlusses der internationalen Recherche
`Absendedatum des lntemationalen Recherchenbe richts
`
`24. Apri1 2001
`Name und Poslanschrifl der lntemationalen Recherchenbehérde
`Europalsches Patentami, P.B. 5818 Palentlaan 2
`NL — 2280 HV Riiswijk
`Tel. (+31-70) 340-2040, TX. 31 651 epo nl.
`Fax: (+31-70)3-10-3016
`Formblatt PCT/ISA/210 (Blafl 2) (Juli 1992)
`
`11/05/2001
`Bevollméichtigler Bediensteler
`
`Goetz 3
`
`(5
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0612
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0612
`
`

`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0613
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0613
`
`

`
`
`
`iNTEFHWATKDNA¢.SEUU§CF|REFKJRT
`international Application No
`
`inform
`~ on patent famiiy members
`
`
`
`P V‘
`
`' 00/11 309
`
`
`
`cited in search report
`
`date
`
`member(s)
`
`date
`
`NO 9843942
`
`A
`
`08-10-1998
`
`AU
`BR
`CN
`EP
`NO
`ZA
`
`6755298 A
`9808069 A
`1251569 T
`1019358 A
`994438 A
`9802478 A
`
`22-10-1998
`08-03-2000
`26-04-2000
`19-07-2000
`26-11-1999
`08-10-1998
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`NO 9411337
`
`A
`
`26-05-1994
`
`164828 T
`15-04-1998
`AU
`672458 B
`03-10-1996
`AU
`5438094 A
`08-06-1994
`CA
`2148827 A
`26-05-1994
`DE
`69317898 0
`14-05-1998
`
`DE
`69317898 T
`15-10-1998
`
`DK
`667852 T
`11-01-1999
`EP
`0667852 A
`23-08-1995
`
`ES
`2117155 T
`01-08-1998
`FI
`952179 A
`05-05-1995
`
`HK
`1006349 A
`19-02-1999
`
`HU
`72742 A
`28-05-1996
`JP
`8503208 T
`09-04-1996
`
`NO
`951775 A
`05-05-1995
`US
`5559269 A
`24-09-1996
`
`11-11-1997 5686464 A
`
`
`
`Form PCTI|SAI210 (patent lamiiy annex) (Jury 1992)
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0614
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0614
`
`

`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0615
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0615
`
`

`
`i
`
`TRANSMITTAL or lNFORMATlON DISCLOSURE STATEMENT
`.(Under 37 CFR 1.97(b) or 1.97(c))
`
`D°°ke' N°'
`‘”945’32854
`
`In Re Application:
`
`Meese, Claus
`
`Serial No.
`
`Filing Date
`
`Examiner
`
`Group Art Unit
`
`10/130214
`
`5/14/2002
`
`El
`IX]
`
`"o¢9&& %
`Payment of Fee‘
`(Only complete if Applicant elects to pay the fee set forth in 37 CFR 1. g @
`Acheck in the amount of
`is attached.
`The Assistant Commissioner is hereby authorized to charge and credit Deposit Acotfigzt No.
`as described below. A duplicate copy of this sheet is enclosed.
`/3.
`3 3
`I]
`Charge the amount of
`IX
`Credit any overpayment.
`/
`IX]
`Charge any additional fee required.
`
`2002
`
`>
`
`Certificate of Transmission by Facsimile*
`
`1
`
`Certificate of Mailing by Express Mail
`
`
`
`I certify that this document and authorization to charge deposit
`account is being facsimile transmitted to the United States Patent
`
`
`
`and Trademark Office (Fax No.
`) on
`
`
`
`
`I certify that this document and fee is being deposited on
`August 14, 2002
`with the U.S. Postal Service as
`Express Mail under 37 C.F.R. 1.10 and addressed to
`the Assistant Commissioner for Patents, Washington,
`D.C. 20231.
`
`Express Mail No.: EL474 165 3 79UL /“
`
`Signature ofPerson Mailing Correspondence
`
`Paul A. Lesko
`
`Typed or Printed Name ofPerson Mailing Certificate
`
`
`
`
`
`
`
`
`
`
`
`
`(Date)
`
`
`
`Typed or Printed Name ofPerson Signing Certificate
`
`*This certificate may only be used if paying by
`deposit account.
`
` Dated:)44§q//_
`
`Paul A. Lesko, Reg. No. #45364
`Thompson Coburn LLP
`One US Bank Plaza
`St. Louis, Missouri 63101-9928
`314-552-6443
`
`ZLUX
`
`314-552-7443 FAX
`
`Customer No:
`
`021888
`
`mm-In
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0616
`
`P1 OC/REV02
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0616
`
`

`
`To
`
`.
`
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`
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`
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`
`1 I. 2uu2'__ 3
`
`4
`14%!’
`
`
`
`AU§:;2 3 2002
`,
`U.S. PatentanI § EH'5T% ,
`rsons are reuired to resend to a collection of information untéss it disla
`V
`’
`
`TRANSMITTAL
`
`J‘
`
`3;
`“PT
`1
`
`I
`
`.
`
`,
`' ‘
`
`
`
`
`'
`
`-
`
`FORM
`
`
`(to be used for all correspondence after
`initial filing)
`
`check all that a - I
` ENCLOSURES
`After Allowance Communication
`Assignment Papers
`(for an Application)
`to Group
`'
`-
`Appeal Communication to Board
`
`
`
`Drawing(s)
`of Appeals and lnterferences
`Licensing-related Papers
`
`
`Appeal Communication to Group
`(Appea/Notice, 8n'ef_ Repfy Brief)
`Pr°prieta'y '"f°"“afi°"
`
` Status Letter
`
`
`
`
`
`
`
`D Charge Deposit Account -20-0823
`-
`A
`d
`E Fee “ache
`D A'l‘e"dme”t/ Rep”
`E] Affidavits/declarations(s)
`'3 Extension of Time Request
`
`[:1 Express Abandonment Request
`
`'
`
`to M5 in Parts
`it-Res ons
`— Incomplete Application
`
`I5 9
`e
`p
`D Response to Missing Parts
`under 37 CFR 1.52 or 1.53
`
`
`
`
`
`
`
`
`
`Petition
`Petition to Convert to a
`Provisional Application
`
`Power of Attorney, Revocation
`Request To Rescind Previous
`Change of Correspondence
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`Address
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`Commissioner is hereby authorized to charge fees in this
`application and any fees which may be required, or any
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`I have
`enclosed a duplicate copy of this sheet
`Amount:
`
`
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` El
`
`Petition For Revival of an Application for
`Patent Abandoned Unintentionally Under
`37 CFR 1.137(b))
`
`
`
`
`
`
`
`
`_
`
`'
`
`
`
`
`
`
`_
`
`Firm
`or
`individual Name
`
`
`_
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`Paul A. Lesko
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`August 14, 2002
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`37 C.F.R. 1.10 and addressed to: Assistant Commissioner for Patents, Washington, D.C. 20231.
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`Paum. Lesko
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` E Auust14,2002
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`
`date: August 14,
`2002 -
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`1722218
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`Patent Owner, UCB Pharma GmbH 4 Exhibit 2012 - 0617
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`In Re Application Of:
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`Title:
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`Address to:
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`37 CFR 1.97(b)
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`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0618
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`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0618
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`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0619
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`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0619
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`

`
`In Re Application Of: _
`Claus Meese
`
`10/130,214
`
`Title:
`
`,
`
`05/14/2002
`
`Stable Salts of Novel Derivatives of 3,3-Diphenylpropylamines
`
`Docket No.
`
`41 946/32854
`
`Group Art Unit
`
`Address to:
`Assistant Commissioner for Patents
`Washington, D.C. 20231
`
`37 cm 1.97(b)
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`1. E The Information Disclosure Statement submitted herewith is being filed within'three ‘months of the
`filing of a national application other than a continued prosecution application under. 37 CFR 1.53(d);
`within three months of the date of entry of the national stage as set forth in 37 CFR 1.491 in an
`international application; before the mailing of a first Office Action on the merits, or before the mailing
`of a first Office Action after the filing of a request for continued examination under 37 CFR 1.114.
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`37 CFR 1.97(c)
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`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0620
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`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0620
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`Mail in an envelope address d to: Assistant Commissioner for Patents, Washington, D.C. 20231.
`date: November
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`R
`Paul A. Lesio -
`r November13.2oo2
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`CERTIFICATE OF EXPRESS MAILING
`Exress Mail No. EL948415117US
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`1722218
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`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0621
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0621
`
`

`
`
`
`9 W
`
`ORLD INTELLECTUAL PROPERTY ORGANIZATION
`International Bureau
`
`0.
`
` (
`
`43) International Publication Date:
`
`
`
`INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT)
` (11) International Publication Number:
`(51) International Patent Classification 6 :
`wo 99/53473
`7c 1/oo 217/62 217/48 219/23
`E109/22, co’71) 207/66, 295/66, co7’c
`13 N°V°mb°r '99?’ 03-’ 1-99)
`271/08, C0713‘ 7./18, cmc 307/02, A6132
`
`31/135, 31/325, 31/4o, 31/435
`
`
`
`(21) International Application Number:
`
`
`PCT/EP99/03212
`
`
`
`
`(81) Designated States: AE. AL. AM. AT, AU, AZ. BA. BB, BG.
`BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB,
`GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG,
`ll May 1999 (1105.99)
`(22) International Filing Date:
`
`
`KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV. MD, MG. MK.
`
`
`MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI,
`SK, SL, TJ, TM, TR, TI‘, UA, UG, US, UZ, VN, YU, ZA,
`(30) Priority Data:
`ZW, ARIPO patent (GH, GM, KE, LS, MW, SD, SL, SZ.
`981086085
`12 May 1998 (l2.05.98)
`EP
`UG, ZW), Eurasian patent (AM, AZ, BY, KG, KZ, MD,
`
`RU, TJ, TM), European patent (AT, BE, CH, CY, DE, DK,
`ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE), OAPI
`
`patent (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR,
`NE, SN, TD, TG).
`
`
`
`
`
`
`
`
`
`
`
`
`(71) Applicant (for all designated States except US): SCHWARZ
`PHARMA AG [DE/DE]; Alfred—Nobel—Strasse
`10,
`D-40789 Monheim (DE).
`
`(72) Inventors; and
`
`Published
`
`(75) Inventors/Applicants (for US only): MEESE, Claus [DFJDE];
`
`
`With international search report.
`
`
`Kreuzberger Strasse 50, D-40789 Monheim (DE). SPARF,
`Bengt [SE/SE]; Drottningstigen 6, S-142 65 Trangsund. _
`(SE).
`
`
`
`
`
`
`Kraus & Weisert,
`Thomas;
`ALBRECHT,
`(74) Agent:
`'I‘homas—Wimmer—Ring 15, D-80539 Munich (DE).
`
`
`
` (54) Title: NOVEL DERIVATIVES OF 3,3—DIPHENYLPROPYLAMINES
`(57) Abstract
`The invention concerns novel derivatives of 3,3—diphenylpropylamines, methods for their preparation, pharmaceutical compositions
`containing the novel compounds, and the use of the compounds for preparing drugs;~More particularly, the invention relates to novel
`prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine,
`methods for their preparation, pharmaceutical compositions containing them, a method of using said compouds and compositions for the
`treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.
`
`
`
`
`
` M puma M”
`
`5,4./(,{€' H spec.
`
`F130/V1
`
`09 700077 .
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0622
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0622
`
`

`
`FOR THE PURPOSES OF INFORMATION ONLY
`
`Codes used to identify States party to the PCT on the front pages of pamphlets publishing international applications under the PCT.
`Slovenia
`SI
`ES
`Lesotho
`Albania
`LS
`Slovakia
`SK
`LT
`Lithuania
`FI
`Armenia
`SN
`LU
`FR
`Senegal
`Austria
`Luxembourg
`SZ
`Swaziland
`Latvia
`LV
`Australia
`GA
`TD
`Chad
`Monaco
`MC
`GB
`Azerbaijan
`MD
`TG
`GE
`Togo
`Republic of Moldova
`Bosnia and Herzegovina
`TJ
`MG
`GH
`Barbados
`Tajikistan
`Madagascar
`TM
`Turkmenistan
`MK
`GN
`The former Yugoslav
`Belgium
`TR
`GR
`Burkina Faso
`'l'\1rkey
`Republic of Macedonia
`TT
`Mali
`HU
`Trinidad and Tobago
`Bulgaria
`UA
`Ukraine
`[E
`Benin
`Mongolia
`UG
`Mauritania
`[L
`Brazil
`Uganda
`United States of America
`US
`Malawi
`IS
`Belarus
`UZ
`Uzbekistan
`IT
`Mexico
`Canada
`VN
`Viel. Nam
`JP
`Niger
`Central African Republic
`YU
`KE
`Netherlands
`Yugoslavia
`Congo
`ZW
`Zimbabwe
`KG
`Switzerland
`Norway
`New Zealand
`KP
`Cbte d'lvoire
`Poland
`Cameroon
`China
`Portugal
`Romania
`Cuba
`Russian Federation
`Czech Republic
`Sudan
`Germany
`Sweden
`Denmark
`Estonia
`Singapore
`
`Spain
`Finland
`France
`Gabon
`United Kingdom
`Georgia
`Ghana
`Guinea
`Greece
`Hungary
`Ireland
`Israel
`Iceland
`Italy
`Japan
`Kenya
`Kyrgyzstan
`Democratic People's
`Republic of Korea
`Republic of Korea
`Kazakstan
`Saint Lucia
`Liechtenstein
`Sri Lanka
`Liberia
`
`ML
`MN
`MR
`MW
`MX
`NE
`NL
`NO
`NZ
`PL
`PT
`R0
`RU
`SD
`SE
`SG
`
`KR
`KZ
`LC
`Ll
`LK
`LR
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0623
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0623
`
`

`
`WO 99/58478
`
`PCT/EP99/032.12
`
`Description
`
`
`
`Novel derivatives of 3,3—diphenylpropylamines
`
`
`
`The present invention relates to novel derivatives of 3,3—
`
`diphenylpropylamines, methods for their preparation, phar-
`
`maceutical compositions containing the novel compounds, and
`
`the use of the compounds for preparing drugs.
`
`In man, normal urinary bladder contractions are mediated
`
`mainly through cholinergic muscarinic receptor stimulation.
`
`There is reason to believe that muscarinic receptors medi~
`
`ate not only normal bladder contractions, but also the main
`
`part of the contractions in the overactive bladder resulting
`
`in symptoms such as urinary frequency, urgency and urge in-
`
`continence. For this reason, antimuscarinic drugs have been
`
`proposed for the treatment of bladder overactivity.
`
`Among the antimuscarinic drugs available on the market,
`
`oxy—
`
`butynin is currently regarded as the gold standard for phar-
`
`macological treatment of urge incontinence and other symp-
`
`toms related to bladder overactivity. The effectiveness of
`
`oxybutynin has been demonstrated in several clinical studies,
`
`but the clinical usefulness of oxybutynin is limited due to
`
`antimuscarinic side effects. Dryness of the mouth is the most
`
`common experienced side effect which may be severe enough to
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0624 r
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0624
`
`

`
`WO 99/58478
`
`PCT/EP99/03212
`
`result in poor compliance or discontinuation of treatment
`
`(Andersson, K,-E,, 1988, Current concepts in the treatment
`
`of disorders of micturition, Drugs 35, 477-494; Kelleher et
`
`al. 1994).
`
`Tolterodine is a new, potent and competitive, muscarinic re-
`
`ceptor antagonist intended for the treatment of urinary urge
`
`incontinence and detrusor hyperactivity. Preclinical pharma-
`
`cological data show that tolterodine exhibits a favourable
`
`tissue selectivity in vivo for the urinary bladder over the
`
`effect on the salivation (Nilvebrant et al., 1997, Toltero—
`
`dine - a new bladder-selective antimuscarinic agent, Eur. J.
`
`Pharmacol. 327 (1997), 195-207), whereas oxybutynin exhibits
`
`the reversed selectivity. Tolterodine is equipotent to oxy-
`
`butynin at urinary bladder muscarinic receptors and the fa-
`
`vourable tissue selectivity of tolterodine demonstrated in
`
`the preclinical studies has been confirmed in clinical stud-
`
`ies. Thus a good clinical efficacy has been combined with a
`
`very low number of incidences of dry mouth and antimuscarinic
`
`side effects.
`
`A major metabolite of tolterodine,
`
`the 5—hydroxymethyl de-
`
`rivative is also a potent muscarinic receptor antagonist and
`
`the pharmacological in vitro and in vivo profiles of this
`
`metabolite are almost identical to those of tolterodine
`
`(Nilvebrant et al., 1997, Eur. J. Pharmacol. 327 (1997),
`
`195-207). Combined pharmacological and pharmacokinetic data
`
`indicate that it is most likely that the metabolite gives a
`
`major contribution to the clinical effect in most patients.
`
`WO 94/11337 proposes the active metabolite of tolterodine as
`
`a new drug for urge incontinence. Administration of the ac-
`
`tive metabolite directly to patients has the advantage com-
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0625
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0625
`
`

`
`W0 99/S8478
`
`PCT/EP99/03212
`
`pared to tolterodine that only one active principle (com-
`
`pound) has to be handled _y the patient which normally should
`
`result in a lower variation in efficacy and side effects be-
`
`tween patients and lower risk of interaction with other
`
`drugs.
`
`However,
`
`the introduction of an additional hydroxy group in
`
`the tolterodine results in an increased hydrophilic property
`
`of the new compounds
`
`(3,3—diphenylpropylamines) compared to
`
`the parent compounds which normally results in a lower ab-
`
`sorption/bioavailability,
`
`leading to pre-systemic side ef-
`
`fects or interactions due to non-absorbed antimuscarinic
`
`drug.
`
`In a method to circumvent this disadvantage, different
`
`prodrugs of the metabolite have been synthesized and tested
`
`for their antimuscarinic activity, potential absorption
`
`through biological membranes and enzymatic cleavage.
`
`It is an object of the present invention to provide novel
`
`derivatives of 3,3-diphenylpropylamines. It is a further ob-
`
`ject of the present invention to provide new derivatives of
`
`3,3—diphenylpropy1amines which will be more useful as pro-
`
`drugs for treatment of urinary incontinence and other spas—
`
`mogenic conditions that are caused by muscarinic mechanisms
`
`while avoiding the disadvantage of a too low absorption
`
`through biological membranes of the drugs or an unfavourable
`
`metabolism.
`
`A further object of the invention is to provide novel pro-
`
`drugs of antimuscarinic agents with superior pharmacokinetic
`
`properties compared to present drugs as oxybutynin and tol-
`
`terodine, methods for preparing thereof, pharmaceutical com-
`
`positions containing them, a method of using said compounds
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0626
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0626
`
`

`
`WO 99/58478
`
`PCI‘/EP99/03212
`
`and compositions for the treatment of urinary incontinence,
`
`gastrointestinal hyperactivity (irritable bowel syndrome)
`
`and other smooth muscle contractile conditions.
`
`According to the present invention, novel 3,3-diphenylpropyli
`
`amines are provided, which are represented by the general
`
`formulae I and VII‘
`
`
`
`Farrnula vu-
`
`wherein R and R‘ are independently selected from
`
`a)
`
`hydrogen, C1-C5 alkyl, C3-Cm cycloalkyl, substituted or
`
`unsubstituted benzyl, allyl or carbohydrate; or
`
`b)
`
`formyl, C1-Csalkylcarbonyl, cycloalkylcarbonyl. sub-
`
`stituted or unsubstituted arylcarbonyl, preferably benzoyl;
`OI‘
`
`c)
`
`C1-C5 alkoxycarbonyl, substituted or unsubstituted aryl—
`
`oxycarbonyl, benzoylacyl, benzoylglycyl. a Substituted °r
`
`unsubstituted amino acid residue; or
`
`Patent Owner, UCB Pharma GmbH — Exhibit 2012 - 0627
`
`Patent Owner, UCB Pharma GmbH – Exhibit 2012 - 0627
`
`

`
`WO 99/58478
`
`PCT/EP99/032 12
`
`_ 5 _
`
`C1)
`
`R4
`\N-co-
`R5
`
`wherein R‘ and R5 independently
`
`repre