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`1
`U.S. Patent and Trademark Office: U.S. DEPARTMENT OF COMMERCE
`‘.5 V
`Under the Paerwork Reduction Act of 1995, no ersons are re uired to resend to a collection of information unless it disla s a valid OMB control number.
` Mail No.
`71 DECLARATION FOR UTILITY, DESIGN, DIVISIONAL AND
`. 2 .. ..
`
`1 CONTINUATION-IN-PART PATENT APPLICATIONS (37 CFR 1.63)
`A“°""° D°°k°t Number
`~r4L345’32354
`
`First Named Inventor
`A MEESE, Claus
`‘I
`COMPLETE IF KNOWN
`IX] Declaration Submitted with lnItIal Filing
`
`
`
`
`A
`
`
`
`
`
`A E] Supplemental D Declaration
`Declaration
`Submitted for
`Submitted
`Continuation-ln-
`Part Filing
`
`
`
`El Declaration
`Submitted for
`Divisional Filing
`
`
`
`Filin Date
`GrouAItUnit
`Examiner Name
`
`
`
`As at below named inventor, I hereby declare that:
`
`residence, mailing address, and citizenship are as stated below next to my name.
`‘I believe I am the original, first and sole inventor (if only one name is listed below) or an original, first and joint inventor (if plural
`names are listed below of the sub'ect matter which is claimed and for which a atent is sou ht on the invention entitled:
`
`
`
`
`I
`
`STABLE SALTS OF NOVEL DERIVATIVES OF 3,3-PHENYLPROPYLAMINES
`
`
`
`
`
`the specification of which
`
`1:] is attached hereto
`OR
`
`(Title of the Invention)
`
`
`
`
`
`
`
`
`.
`
`51'
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`
`‘J
`
`
`
`
`
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`
`
`
`
`E was filed on (MM/DD/YYYY)
`
`11/15/2000
`
`as United States Application Number or PCT International
`
`
`
`Application Number
`
`PCT/EPOO/11309
`
`and was amended on (MM/DDIYYYY)
`
`(if applicable).
`
`I hereby state that l have reviewed and understand the contents of the above identified specification, including the claims, as
`amended by any amendment specifically referred to above.
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`I acknowledge the duty to disclose information which is material to patentability as defined in 37 CFR 1.56, including for continuation-
`in-part applications, material information which became available between the filing date of the prior application and the national or
`PCT international filin date of the continuation-in—art a Iication.
`
`
`I hereby claim foreign priority benefits under 35 U.S.C. 119(a)-(d) or (f), or 365(b) of any foreign application(s) for patent, inventor’s
`or plant breeder’s rights certificate(s), or 365(a) of any PCT international application which designated at least one country other
`than the United States of America,
`listed below and have also identified below, by checking the box, any foreign application for
`patent, inventor’s or plant breeder’s rights certificate(s), or any PCT international application having a filing date before that of the
`a Iication on which riorit
`is claimed.
`
`
`
`Prior Foreign Application
`Number s
`
`Country
`
`Foreign Filing Date
`MMIDDIYYYY
`
`Priority
`Not Claimed
`
`Certified Copy Attached?
`YES
`NO
`
`DE 199 55 190.1
`
`[:1
`El
`[3
`D
`Cl
`Cl
`El Additional forei n a - Iication numbers are listed on a su lemental riorit data sheet PTO/SB/02B attached hereto:
`[Page 1 of 2]
`
`Germany
`
`11/16/1999
`
`
`
`1887648
`
`
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 567
`
`

`
`’
`
`
`
`¥cgnefirai5pt.
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`
`PTO/SBl96 (08-00)
`Approved for use through 10/31/2002 OMB 0651-0031
`U.S Patent and Trademark Office, U.S. DEPARTMENT OF COMMERCE
`Under the Paenivork Reduction Act of 1995, no ersons are reuired to resend to a collection of information unless it disla s a valid OMB control number.
`
`
`
`
`
`STATEMENT UNDER 37 CFR 3.73]b[
`
`Applicant/Patent Owner: SCHWARZ PHARMA AG
`
`
`
`
`
`
`Application No./Patent No.:
`Filed/Issue Date:
`
`Entitled: STABLE SALTS OF NOVEL DERIVATIVES OF 3 3-DIPHENYLPROPYLAMINES
` SCHWARZ PHARMA AG
`, a CORPORATION
`.
`(Name of Assignee)
`(Type of Assignee, e g , corporation, partnership, university, government agency, etc )
`
`states that it is:
`
`
`
`1. E the assignee of the entire right, title, and interest; or
`2. [I an assignee of less than the entire right, title and interest.
`The extent (by. percentage) of its ownership interest is
`
` in the patent applicationlpatent identified above by virtue of either:
`A. [X] An assignment from the inventor(s) of the patent application/patent identified above. The assignment
`was recorded in the United States Patent and Trademark Office at Reel
`, Frame
`, or for
`which a copy thereof is attached.
`
`
`
`
`
`
`
` OR
`
`
`] A chain of title from the inventor(s), of the patent application/patent identified above, to the current
`B. [
`assignee as shown below:
`1. From
`To:
`
`The document was recorded in the United States Patent and Trademark Office at
`
`
`Reel
`. Frame
`, or for which a copy thereof is attached.
`
`
`2. From
`To:
`
`The document was recorded in the United States Patent and Trademark Office at
`
`Reel
`, Frame
`, or for which a copy thereof is attached.
`
`
`
`
`
`
`To:
`3. From
`The document was recorded in the United States Patent and Trademark Office at
`Reel
`, Frame
`, or for which a copy thereof is attached.
`
`
`
`[ ]Additiona| documents in the chain of title are listed on a supplemental sheet.
`
`[
`
`] Copies of assignments or other documents in the chain of title are attached.
`|NOTE: A separate copy (i.e., the original assignment document or a true copy of the original document)
`must be submitted to Assignment Division in accordance with 37 CFR Part 3, if the assignment is to be
`recorded in the records of the USPTO. fig MPEP 302.08]
`
`
`
`
`
`
`The undersigned (whose title is supplied below) is authorized to act on behalf of the assignee.
`
`2 May 2002
`Date
`
`
`i.V. D.w. Schacht
`p a. K.
`Hommerich
`
`
`Typed or printed name
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`Authorized Officer
`
`
`Signature
`
`Assistant Mana er
`Title
`
`
`
`Burden Hour Statement‘ This form is estimated to take 0 2 hours to complete. Time will vary depending upon the needs of the individual case Any comments on
`the amount of time you are required to complete this form should be sent to the Chief Information Officer, U S Patent and Trademark Office, Washington, DC
`20231. DO NOT SEND FEES OR COMPLETED FORMS TO THIS ADDRESS. SEND TO. Assistant Commissioner for Patents, Washington, DC 20231.
`
`1887451
`
`
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 568
`
`

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`Ap
`d for use through 10/31/2002. OMB 0651 0035
`U 8. Patent and Trademark Office; U 5 DEPARTMENT OF COMMERCE
`Under the Pa erwork Reduction Act of 1995, no
`ersons are reuired to resond to a collection of information unless it disla s a valid OMB control number.
`
`
`E
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`POWER OF ATTORNEY OR
`
`
`AUTHORIZATION OF AGENT
`
`
`
`
`
`—J
`— ——
`
`
`
`
`
`
`I hereby appoint:
` IX] Practitioners at Customer Number
`
`
`El Practitioner(s) named below:
`PATENT TRADEMARK OFFICE
`
`_,
`
`
`OR
`
`/ Re istration Number
`
` as my/our attorney(s) or agent(s) to prosecute the application identified above, and to transact all
`
`business in the United States Patent and Trademark Office connected therewith.
`Please change the correspondence address for the above-identified application to:
`D The above-mentioned Customer Number
`OR
`
`
`
`
`
`
`E] Practitioners at Customer Number
`021888
`OR
`
`F.
`
`,
`lr1i:lliT\1/igfial Name
`Paul A‘ Lesko
`Thomson cobum LLP
`one Us Bank Plaza
`
`m 63101
`
`
`
`
`
`314-552-6443
`
`
`
`
`
`
`Applicant/Inventor.
`
`
`Assignee of record of the entire interest. See 37 CFR 3.71.
`Statenient under 37 CFR 3. 73(b) is enclosed. (Form PTO/SB/96).
`r
`SIGNATERE ofA - licant or Assi o nee of Record
`
`
`D W. Schacht
` ppa. K.—D(/lHommeri~ch
`j_.V.
`
`
`
`
`
`
`NOTE: Signatures of all the inventors or assignees of record of the entire interest or their representative(s) are required. Submit multiple
`forms if more than one signature is required, see below‘.
`
`
`
`
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 569
`
`

`
`
`PTO/SB/01 (03-01)
`
`
`
`021888
`
`OR [3 Correspondence address below
`
`
`
`Direct all correspondence to: IE
`
`C t
`N
`oru§:rrg:rdeul::::[
`
`
`
`Paul A. Lesko, Esq.
`
`
`
`
`
`Address
`
`Thompson Coburn LLP
`One U.S. Bank Plaza, Suite 3500
`
`
`
` State MO
`ZIP
`
`
`
` 314-552- 6443
`Fax
`314-552-7443
`
`
`
`I hereby declare that all statements made herein of my own knowledge are true and that all statements made on information and belief
`are believed to be true; and further that these statements were made with the knowledge that willful false statements and the like so
`
`
`
`made are punishable by fine or imprisonment, or both, under 18 U.S.C. 1001 and that such willful false statements may jeopardize the
`
`validity of the application or any patent issued thereon.
`
`
`
`Family Name
`
`or Surname
`
`
`
`Given Name
`
`first and middle if an
`
`Inventor's
`Si nature
`
`
`
`
`
`Address
`
`Kreuzbererstrasse 50
`
`40789 Monheim
`
` COW"
`
`GERMANY
`
`
`
`
`
`
`El A petition has been filed for this unsigned inventor
`
` F
`
`Given Name
`
`amily Name
`or Surname
`
` Inventor's
`Si nature
`
`
`
`
`Citizenshi -
`
`
`
`1887648
`
`[Page 2 of 2]
`
`
`
`Approved for use through 10/31/2002. OMB 0651-0032
`U.S. Patent and Trademark Office; US. DEPARTMENT OF COMMERCE
`Under the Paenlvork Reduction Act of 1995. no ersons are re uired to resend to a collection of information unless it disla s a valid OMB control number.
`
`0
`
`DECLARATION — Utility or Design Patent Application
`
`
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 570
`
`

`
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`
`FORM PTO-1390
`U.S. DEPARTMENT OF
`(REV 11-2000)
`L
`TRANSMITTAL LETTER TO THE UNITED STATES
`
`41946732854
`
`CONCERNING A FILING UNDER 35 U.S.C. 371
`INTERNATIONAL FILING DATE
`15 NOVEMBER 2000
`
`U.S. APPLICATION NO. (If known, see 37 CFR 1.5)
`N” I O / 1 3 0 2 11,
`PRIORITY DATE CLAIMED
`16 NOVEMBER 1999
`
`TITLE OF INVENTION
`STABLE SALTS OF NOVEL DERIVATIVES OF 3,3,-DIPHENYLPROPYLAMINES
`
`Applicant herewith submits to the United States Designated/Elected Office (DO/EO/US) the following items and other infomiation:
`This is a FIRST submission of items concerning a filing under 35 U.S.C. 371.
`
`This is a SECOND or SUBSEQUENT submission of items concerning a filing under 35 U.S.C. 371.
`
`This is an express request to begin national examination procedures (35 U.S.C. 371(0). The submission must include
`items (5), (6), (9) and (21) indicated below.
`
`The US has been elected by the expiration of 19 months from the priority date (Article 31).
`A copy of the International Application as filed (35 U.S.C. 371(c)(2))
`
`a. D is attached hereto (required only if not communicated by the Intemational Bureau).
`b.
`has been communicated by the International Bureau.
`c. E]
`is not required, as the application was filed in the United States Receiving Office (RO/US).
`Afr English language translation of the International Application as filed (35 U.S.C. 371(c)(2)).
`
`a. _
`IE is attached hereto.
`b.- D has been previously submitted under 35 U.S.C. 154 (d)(4).
`Amendments to the claims of the International Application under PCT Article 19 (35 U.S.C. 371(c)(3))
`a.
`I___] are attached hereto (required only if not communicated by the International Bureau).
`b. D have been communicated by the International Bureau.
`c. D have not been made; however, the time limit for making such amendments has NOT expired.
`d. E have not been made and will not be made.
`
`An English language translation of the amendments to the claims under PCT Article 19 (35 U.S.C. 371 (c)(3)).
`
`An oath or declaration of the inventor(s) (35 U.S.C. 371(c)(4)).
`
`An English language translation of the annexes of the International Preliminary Examination Report under PCT
`Article 36 (35 U.S.C. 371(c)(5)).
`
`
`
`Items 11 to 20 below concern document(s) or information included:
`. E An Information Disclosure Statement under 37 CFR 1.97 and 1.98.
`
`. X An assignment document for recording. A separate cover sheet in compliance with 37 CFR 3.28 and 3.31 is included.
`. E A FIRST preliminary amendment.
`. D A SECOND or SUBSEQUENT preliminary amendment.
`. E] A substitute specification.
`. E A change of power of attorney and/or address letter.
`. I:] A computer-readable form of the sequence listing in accordance with PCT Rule 13ter.2 and 35 U.S.C. 1.821 — 1.825.
`. I:] A second copy of the published international application under 35 U.S.C. l54(d)(4).
`.
`A second copy of the English language translation of the international application under 35 U.S.C. l54(d)(4).
`.
`IX} Other items or information: Certificate of Express Mailing;
`’
`Postcard
`Statement Under 37 CFR 3.73(b)
`
`page 1 of2
`
`‘9°°°°3'9°°°°3
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 571
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 571
`
`

`
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`INTERNATIONAL APPLICATION NO.
`f
`‘_‘
`_
`__ V_
`PCT/EPO0/11309
`
`A'I'l'0RNEY'S DOCKET NUMBER
`41946/32854
`
`,
`
`'
`21. E The following fees are submitted:
`BASIC NATIONAL FEE (37 CFR 1.492 (a) (1) — (5)):
`Neither international preliminary examination fee (37 CFR 1.482)
`nor international search fee (37 CFR 1.445(a)(2)) paid to USPTO
`and International Search Report not prepared by the EPO or JPO .................... .. $1000.00
`International preliminary examination fee (37 CFR 1.482) not paid to
`USPTO but International Search Report prepared by the EPO or JPO ............... .. $860.00
`International preliminary examination fee (37 CFR 1.482) not paid to USPTO
`but international search fee (37 CFR l.445(a)(2)) paid to USPTO ..................... .. $710.00
`International preliminary examination fee (37 CFR 1.482) paid to USPTO
`but all claims did not satisfy provisions of PCT Article 33(1)-(4) ....................... .. $690.00
`International preliminary examination fee (37 CFR 1.482) paid to USPTO
`and all claims satisfied provisions of PCT Article 33(1)-(4) ............................... .. $100.00
`I
`
`ENTER APPROPRIATE BASIC FEE AMOUNT =
`
`Surcharge of $130.00 for furnishing the oath or declaration later than
`months from the earliest claimed priority date (37 CFR 1.492(e)).
`CLAIMS
`NUMBER FILED
`NUMBER EXTRA
`Total claims
`30- 20 =
`Indeendent claims
`10-
`3 =
`MULTIPLE DEPENDENT CLAIM S
`
`x $80.00
`+ $270.00
`ifa 0 licable
`TOTAL OF ABOVE CALCULATIONS =
`
`CALCULATIONS PTO USE ONLY
`
`$
`
`ll$
`
`$
`$
`$
`$
`
`D Applicant claims small entity status. See 37 CFR 1.27. The fees indicated above
`are reduced b 1/2.
`SUBTOTAL =
`I 30
`
`Processing fee of $130.00 for furnishing the English translation later than I 20
`months from the earliest claimed
`'
`'
`date 37 CFR 1.492
`TOTAL NATIONAL FEE =
`Fee for recording the enclosed assignment (37 CFR l.21(h)). The assignment must be
` 40.00
`accomanied b an a roriate cover sheet 37 CFR 3.28 3.31 .
`.
`TOTAL FEES ENCLOSED =
`1910.00
`Amount to be
`refunded:
`
`+
`
`char 1 ed:
`
`E A check in the amount of $
`
`1910.00
`
`to cover the above fees is enclosed.
`
`Please charge my Deposit Account No.
`A duplicate copy of this sheet is enclosed.
`
`in the amount of $
`
`to cover the above fees.
`
`The Commissioner is hereby authorized to charge any additional fees which may be required, or credit any
`overpayment to Deposit Account No.
`20-0823. A duplicate copy of this sheet is enclosed.
`
`Fees are to be charged to a credit card. WARNING: Information on this form may become public. Credit card
`information should not be included on this form. Provide credit card information and authorization on PTO-2038.
`
`Where an appropriate time limit under 37 CFR 1.494 or 1.495 has not been met, a petition to review (37 CFR
`1.137(a) or (b)) must be filed and granted to restore the application to pending st
`s.
`
`SENDALLCORRESPONDENCE TO:
`
`
`
`Signature
`
`Paul A. Lesko
`Name
`
`Paul A. Lesko, Esq.
`Thompson Coburn LLP
`One U.S. Bank Plaza
`St. L uis, MO 63101
`Telephone No.: 314.552.6443
`Facsi-mile No.: 314.552.7000
`'
`
`45,364
`‘ Re istration Number
`page 2 of 2
`
`
`
`19000031900003
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 572
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 572
`
`

`
`
`
`
`Docket No.
`
`41946/32854
`
`- Ex - ress Mail No. EI.J94273160.L
`
`In Re Application Of:
`MEESE, Claus
`
`’
`
`
`
`Serial No.
`New
`
`I0/1302 I4
`
`Filing Date
`Herewith
`
`Examiner
`
`Not assigned
`
`Group Art Unit
`Not. assigned
`
`STABLE SALTS OF NOVEL DERIVATIVES OF 3,3-DIPHENYLPROPYLAMINES
`
`TO THE COMMISSIONER OF PATENTS AND TRADEMARKS
`
`_Transmitted herewith is:
`
`[X] Transmittal Letter to the United States Designated/Elected Office (DE/EO/US) Concerning a Filing under 35
`U.S.C. 371
`IE Declaration
`XI English Translation of the International Application as filed
`E Preliminary Amendment
`XI Information Disclosure Statement
`XI Assignment and Recordation Form Cover Sheet
`IX Statement Under 37 CFR 3.73(b)
`[X Power of Attorney
`E Check number 446161
`E Postcard
`
`
`
`Paul A. Lesko, Reg. No. 45,364
`Thompson Coburn LLP
`One U.S. Bank Plaza, Suite 3500
`St. Louis, Missouri 63101
`314-552-6443
`314-552-7000 FAX
`
`Customer No. 021888
`
`with the U.S. Postal Service as
`that the (IE: meimt and fee Is belng deposited on
`I cert
`Express
`ail u der 37 C.F.R. 1.10 and is addressed to the
`Commissioner for Patents, Box PCT, Washington, D.C. 20231.
`
`Express Mail No. EL942731601US ,
`
`signatureof Person Mailing Correspondence
`
`k
`L
`P3 I
`Typed or Printed Name of Person Malling Correspondence
`
`1895472
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 573
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 573
`
`

`
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`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 574
`
`

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`PATéN:T_ NUMBER and
`ISSUE DATE
`
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`
`PLISH 53 .
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`Foreign priority claimed
`35 USC 119 oonditions met
`Verified and Acknowledged Examinersis intials
`
`El yes Dno ‘
`D yes C! no
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 575
`
`

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`OR
`
`OR TOTAL _
`OTHER THAN
`
`
`
`
`
`CLAIMS AS FILED - PART I
`Column 1
`
`
`
`TOTAL CLAIMS
`
`
`..
`
`.36
`
`47 menus2o=
`/o
`
`7
`
`* If the difference in column 1 is less than zero, enter “0" in column 2
`CLAIMS AS AMENDED - PART II
`
`PATENT APPLICATION FEE DETERMINATION RECORD
`
`Effective October 1, 2001
`
`
`10/130215
`
`Application or Docket Number
`
`
`
`
`
`‘ Column 1
`CLAIMS
`REMAINING
`AFTEQ
`AMENDMENT
`
`HIGHEST
`NUMBER
`PREVIQUSLY
`PAID FOR
`
`Independent
`
`
`
`FIRST PRESENTATION OF MULTIPLE DEPENDENT CLAIM
`
`
`
`AMENDMENTA
`
`SMALL ENTITY OR SMALL ENTITY
`
`RATE
`
`ADD"
`TIONAL
`FEE
`
`RATE
`
`ADD"
`TIONAL
`
`0 VII
`
`+280:
`
`-I
`;‘n‘omi‘ITIF
`
`Independent
`
`AMENDMENTB
`
`U
`I-Z;
`1%;
`
`CLAIMS
`REMAINING
`AFTER
`AMENDMENT
`
`HIGHEST
`NUMBER
`PREVIOUSLY
`PAID FOR
`
`CLAIMS
`REMAINING
`AFTER
`AMENDMENT
`
`NUMBER
`PREVIOUSLY
`PAID FOR
`
`g Independent
`FIRST PRESENTATION OF MULTIPLE DEPENDENT CLAIM
`
`RATE
`
`ADD"
`TIONAL
`FEE
`
`RATE
`
`AUDI’
`TIONAL
`FEE
`
`OR X$18=
`
`OR
`
`X84:
`
`OR +280:
`-I
`0 13 >U 9
`
`RATE
`
`ADDI-
`TIONAL
`FEE
`
`RATE
`
`ADD"
`TIONAL
`FEE
`
`‘n rn O J) >U9
`:0mi‘IT|I_
`
`
`
`
`_
`ADD‘:-_<)g£E‘ OR ADDl;_OFT£é-
`
`HIGHEST
`
`
`
`
`
`5.
`
`
`— ' . o -
`. " 0 0
`A
`Petitioner M Ian Pharmaceu C n
`
`
`FORM PTO-B75 (Rev. 8/01)
`-u.s. Government Printing Office: 2001 -— 434.434/59253
`Patent and Trademark Office. U.S. DEPARTMENT OF COMMERCE
`
`" If the entry in column 1 is less than the enlry'in column 2. write "0" in column 3.
`*' If the “Highest Number Previously Paid For” IN THIS SPACE is less than 20, enter "20."
`"*‘If the “Highest Number Previously Paid For" IN THIS SPACE is less than 3. enter "3."
`The “Highest Number Previously Paid For" (Total or Independent) is the highest number found in the appropriate box in column 1.
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 577
`
`

`
`7
`
`1’
`
`5
`
`‘
`
`PATENT A_PPLICATTON SERIAL NO.
`
`‘
`
`U.S. DEPARTMENT OF COMMERCE
`
`PATENT AND TRADEMARK OFFICE
`
`FEE RECORD SHEET
`
`05/22/2003 SFREY1
`
`00000027 10130310
`
`01 FC:970
`02 FC:965
`03 F0564
`
`090.00 OP
`100.00 UP
`508.00 09
`
`05/22/2002 GFREYI
`" -1’.-T-‘
`'—-
`.
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`
`00000027 10130214
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`
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`
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`93/32/2332 ncanpm aamaas eeaoes
`a1rc:9ss
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`V
`a1a.aaop
`e2rc:9ss
`some cu
`
`'U.S. Government Printing Offlce: 2001 — 481-697/59173
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 578
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 578
`
`

`
`V...
`
`WJULTMPLE IEIPENDENT CILAHM
`FEE CALCULAWON SHEET
`(FOR USE WITH FORM PTO-875)
`
`SERIAL NO
`
`FIUNG DATE
`
`mm/‘)1@2n
`[0
`
`m
`
`4I
`
`wW
`M
`
`
`
`W.=======_==_=_===_====_=====-
`
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`
`
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`
`o0.0.0.00,OYo_.5WKujttmIm..._.Imm....___fi.nn___.n.__.u..____________._.__._.
`._.t..____n____.____..._ia.=..__.___.._.__.._.__H.,.
`
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`..,a____n__§§a§gggégggggnngnuumnnnaa
`
`.a
`
`m
`
`‘MAY BE USED FOR ADDITIONAL CLAIMS OR ADMENDMENTS
`
`FORM PTO-1350 (REV. 3-78)
`
`U.$.DEPARTMENT OF COMMERCE
`Patent and Trademalk Offlce
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 579
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 579
`
`
`

`
`,
`g
`'
`-
`—~.i.3ec'a PCT/PTO 1 4 MAY 2002
`INTHE UNITED STATES PATENTAND TRADEMARKOFFICE
`
`3.,
`
`In re Application of: MEESE, Claus et
`al.
`
`Appiicatiun No.: To be assigned
`
`Filed: Herewith
`
`Title: STABLE SALTS OF NOVEL
`
`DERIVATIVES OF 3,3-
`DIPHENYLPROPYLAMINES
`
`\—l‘~4\-/\J\J‘_l%%€
`
`Examiner: To be assigned
`
`Group Art Unit: To be assigned
`
`Docket No.: 41946/32854
`
`Commissioner for Patents
`Box PCT
`
`Washington, DC 20231
`
`‘
`Sir:
`
`PRELINHNARY AMENDMENT
`
`Prior to calculation of the filing fee and examination on the merits, kindly amend the
`
`above-identified patent application per the following instructions.
`
`Kindly amend the specification at page one after the title and before the first line of
`text, b insertin at that point the following sentence --‘This patent application claims the
`
`I
`
`a,
`
`benefit ofpriority under 35 U.S.C. § 119 of German Patent Application No. 199 55 190.1,
`filed November 16, 1999. German Patent Application No. 199 55 190.1 is incorporated
`
`:- herein in its entirety by reference.--
`—___?___
`The amendments to claims 18721, 23-25, 27, and 28 are pursuant to an Article 34
`
`amendment made to the PCT application on October 5, 2001.
`
`IN THE CLAIMS
`
`At page 56, amend claims 18-21, 23-25, 27, and 28 as follows:
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 580
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 580
`
`

`
`.
`
`
`
`-E I: Vd"‘£: "““f33
`" nil
`IxF'9iI 5'“
`«.4 -:i.;n :2: ..;u.. "'1r"u..i1'n:;
`
`*-
`
`18. (once amended) Compound of formula III
`
`Formula III
`
`
`
`ure cin hi hl stalline and stable form.
`
`
`
`19. (once amended) Compound of formula V
`
`.
`OH
`
`Formula V
`
`
`
`ure cin hi hl stalline and stable form.
`
`
`
`2
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 581
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 581
`
`

`
`gig. 4 Q .iiiii
`
`20. (once amended) Compound of formula VI
`
`HO 1\
`/ OH
`
`J\ Formula VI
`L
`
`in highly pure, crystalline and stable form.
`
`21. (once amended) Use of a compound in accordance with claims 18 to 20 as a highly pure,
`
`crystalline, stable intermediate product in the manufacture of pharmaceutically useful
`
`compounds of formula 1 in accordance with claim 1.
`
`23. (once amended) Compound of formula 3
`
`Formula 3
`
`
`
`ure cin hi hl stalline and stable form.
`
`
`
`3
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 582
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 582
`
`

`
`24. (once amended) Compound of formula 5
`
`Formula 5
`
`
`
`ure cin hi hl stalline and stable form.
`
`
`
`25. (once amended) Compound of formula 6
`
`Formula 6
`
`
`
`
`
`ure cin hi hl stalline and stable form.
`
`4
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 583
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 583
`
`

`
`27. (once amended) Use of a compound in accordance with claims 23 to 26 as a highly pure,
`
`crystalline, stable intermediate product in the manufacture of pharmaceutically useful
`
`compounds of formula 2 in accordance with claim 3.
`
`28. (once amended) Use of a compound in accordance with claims 23 to 26 as an
`
`intermediate product in the manufacture of phenolic monoesters of general formula 1
`
`Formula 1
`
`in which R denotes Cl;Q§—a1kyl, C3£1_o-c cloalk 1 or unsubstituted or substituted hen 1.
`
`5
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 584
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 584
`
`

`
`1 ant ‘wen
`
`‘u .11
`
`59-93::
`
`‘
`
`f.3..:{'.‘§«"~srz~ 1.15§._i
`
`axnnh
`.
`u p
`.
`_
`n 4:-=1:
`.."“.’<fl"1lB3l "Z
`
`Kindly consider this preliminary amendment and enter it into the record of this
`
`application. Attached is a clean copy of the claims. All correspondence should to be directed
`
`to Paul A. Leskc, Thompson Coburn LLP, One U.S. Bank Plaza, St. Louis, MO 63101,
`
`Telephone No.: 314.552.6443, Facsimile No.: 314.552.7000.
`
`Respectfully submitted,
`
`//
`
`Pa A. Lesko
`
`Registration No. 45,364
`Thompson Coburn LLP
`One U.S. Bank Plaza
`
`St. Louis, MO 63101
`
`Telephone: 314.552.6443
`Facsimile: 314.552.7000
`
`6
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 585
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 585
`
`

`
`-:!=‘h:
`
`.,:i'i;3$""“T.§;3—’i’:- 3.. E3 Ii - 1
`
`;::...n
`
`CLEAN COPY OF PARAGRAPH TO BE INSERTED 1NTO SPECIFICATION
`
`-- This patent application claims the benefit of priority under 35 U.S.C. § 1 19 of German
`
`Patent Application No. 199 55 190.1, filed November 16, 1999. German Patent Application
`
`No. 199 55 190.1 is incorporated herein in its entirety by reference.-—
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 586
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 586
`
`

`
`3.13 -
`
`i‘"’'“; ii
`
`as :i."$*i§ :31. '3-.§-i§i,‘;-3&3;
`
`
`Compound of formula III
`
`Claims
`
` Formula IH
`
`in highly pure, crystalline and stable form.
`
`19.
`
`Compound of formula V
`
`0
`
`.
`OH
`
`Formula V
`
`in highly pure, crystalline and stable form.
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 587
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 587
`
`

`
`20.
`
`Compound of formula VI
`
`Q
`
`Ho 0
`
`OH
`
`0 J\ Formula VI
`i
`
`in highly pure, crystalline and stable form.
`
`21. Use of a compound in accordance with claims 18 to 20 as a highly pure, crystalline,
`
`stable intermediate product in the manufacture of pharmaceutically useful compounds
`
`of formula 1 in accordance with claim 1.
`
`
`
`23. Compound of formula 3
`
`a5
`
`Formula 3 o/\[j
`
`Mk
`_.)\
`
`in highly pure, crystalline and stable form.
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 588
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 588
`
`

`
`:3“ M’ ""‘';ii,, "3 £63 "’"' :5. "’*i'i=-firfi
`
`24.
`
`Compound of formula 5
`
`Formula 5
`
`H3C\
`
`
`
`in highly pure, crystalline and stable form.
`
`25.
`
`Compound of formula 6
`
`Formula 6
`
`in highly pure, crystalline and stable form.
`
`g 27.
`
`Use of a compound in accordance with claims 23 to 26 as a highly pure, crystalline,
`
`Q
`
`stable intermediate product in the manufacture of pharmaceutically useful compounds
`
`of formula 2 in accordance with claim 3.
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 589
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 589
`
`

`
`28
`
`Use of a compound in accordance with claims 23 to 26 as an intermediate product in
`
`2; #_
`L}
`
`the manufacture ofphenolic monoesters ofgeneral formula 1
`
`
`
`in which R denotes C1-C5-alkyl, C3-C10-cycloalkyl or unsubstituted or substituted phenyl.
`
`
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 590
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 590
`
`

`
`-63..
`
`1/1
`
`Figure 1
`
`Reaction diagram 1
`
`(i),
`
`(ii), (iii),
`
`(iv),
`
`(v) stand for:
`
`(i), LiAlH4,
`
`(ii),
`
`Raney nickel/H2, (iii), Me2CH—CoCl, Et3N,
`
`(iv),
`
`fumaric acid,
`
`(v), hydrochloric acids; R stands for isopropyl
`
`(iPr)
`
`
`
`(iii)
`
`(iv or v)
`
`————+ 1
`
`——————> 2a or 2b
`
`R=i—Pr
`
`'
`
`R=i—Pr
`
`6
`
`'
`
`a:X=C4H3O4
`b:X=Cl
`
`'
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 591
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 591
`
`

`
`‘l E i
`«E
`.'£I
`.
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`ec’d PCT/PTO 14 MAY 2002
`
`‘/Pi“-1-
`
`SPECIFICATION
`
`Stable salts of novel derivatives of
`‘I
`3,3-di hen i ro lamines
`
`The present invention concerns highly pure, crystalline,
`
`stable compounds of novel derivatives of 3,3-
`
`diphenylpropylamines in the form of their salts, a method for
`
`manufacturing these and highly pure, stable,
`
`intermediate
`
`products.
`
`From document PCT/EP99/03212 novel derivatives of 3,3-
`
`diphenylproprylamines are known.
`
`These are valuable prodrugs for the treatment of urinary
`
`incontinence and other spasmodic complaints, which overcome
`
`the disadvantage of the active substances available to date,
`
`namely inadequate absorption of the active substance by
`
`biological membranes or the unfavourable metabolism of these.
`
`Furthermore these novel prodrugs have improved
`
`pharmacokinetic characteristics compared with Oxybutynin and
`
`Tolterodint
`
`Preferred compounds from the group of these novel derivatives
`
`of 3,3—diphenylpropylamines are esters of aliphatic or
`
`aromatic carboxylic acids with the general formula A referred
`
`_to below
`
`Formula A
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 592
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 592
`
`

`
`.31
`
`.-.‘5“‘.‘.: -..n ‘=35
`$1.511 .;.§L..""'
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`
`-us
`
`in which R denotes C1-C6-alkyl, C3-C1o—cycloalkyl or
`
`unsubstituted or substituted phenyl. These can occur in their
`
`optical isomers form as racemic mixtures and in the form of
`
`their individual enantiomers.
`
`Compounds with the structure of formula A do, however, have
`
`low solubility in water. This restricts their oral
`
`bioavailability.
`
`Finally, monoesters of the structure, as shown in formula A,
`
`have a tendency towards intermolecular transesterification.
`
`During long periods of storage,
`
`therefore, as the content of
`
`the compounds with the structure of general formula A drops
`
`an increase in diesters and free diol can be detected.
`
`Basically salts of the compounds of general formula A can be
`
`obtained if solutions of the compounds of formula A (base
`
`component) are purified with solutions of acids in suitable
`
`solvents, but the salts obtained in the form of solid matter
`
`can prove to be altogether amorphous and/or hygroscopic and
`
`cannot be directly crystallized from the normal solvents
`
`either. Such salts have inadequate chemical stability to be
`
`galenically processed as valuable pharmaceutically active
`
`substances.
`
`l|Il'K.';.—u2a—'T“JI¥.*
`
`Surprisingly, it has now been found that the abovementioned
`
`disadvantages can be avoided if compounds with the structure
`
`of general formula A, once they have been prepared under a
`
`special reaction process, are converted with a
`
`physiologically compatible inorganic or organic acid with
`
`general formula H—X,
`
`in which "X represents the respective
`
`Petitioner Mylan Pharmaceuticals Inc. — Exhibit 1002 — Page 593
`
`Petitioner Mylan Pharmaceuticals Inc. - Exhibit 1002 - Page 593
`
`

`
`Vu“‘u‘&fl:@ =wwtmE;
`
`:I“‘In1fi‘“"' ‘.4:
`J"
`
`33 :1 \a—‘Ah -'---:i
`
`acid residue,
`
`into their respective salt with general formula
`
`I.
`
`Formula I
`
`The problem for the present invention is therefore to provide
`
`highly pure, crystalline, stable compounds of novel
`
`derivatives of 3,3-diphenylpropylamines in the form of their
`
`salts,
`
`that avoid the stated disadvantages and are well
`
`suited to use in pharmaceutical-technical formulations and
`
`can be processed into these.
`
`A further problem for the present invention is to provide a
`
`method for manufacturing such highly pure, crystalline,
`
`stable compounds in the form of their salts, as well as
`
`highly pure, stable intermediate products.
`
`The final problem for the invention is to provide a method
`
`for manufacturing the abovementioned compounds with which a
`
`high yield of the products of the process and the respective
`
`intermediate products can be obtained chemo— or
`
`regioselectively.
`
`Petitione