`
`Exhibit 1001
`
`U.S. Patent No. 8,865,688 (“the ‘688
`Patent”)
`
`

`
`(12) United States Patent
`(12) United States Patent
`Forbes
`Forbes
`
`(10) Patent N0.:
`(10) Patent N0.:
`(45) Date of Patent:
`(45) Date of Patent:
`
`US 8,865,688 B2
`US 8,865,688 B2
`Oct. 21, 2014
`Oct. 21, 2014
`
`US008865688B2
`USOO8865688B2
`
`2006/0223787 A1
`10/2006 Devane et al.
`(54) COMPOSITIONS AND METHODS FOR
`2006/02237 87 A1 10/2006 Devane et a1.
`(54) COMPOSITIONS AND METHODS FOR
`0
`SOII
`. . . . . . . . . . . . . . . . . . . . . . ..
`OFBOWEL 2323;312:212 :11 7:33:
`GRANULATED MESALAMINE
`2007/0243184 A1
`10/2007 Fischkoff et al.
`GRANULATED MESALAMINE
`2007/ 0243184 A1 10/2007 Fischkoff et al.
`.
`.
`.
`2008/0096849 A1
`4/2008 Johnson
`_
`2008/0096849 A1
`4/2008 Johnson
`1I1VeI1t0rI Wllllam Forbes, Ra1e1gh, NC (US)
`2010/0035850 A1 *
`2/2010 Karlstadt Meyeroff
`(75)
`(75) Inventori William Forbes, Ralelgh, NC (Us)
`2010/0035850 A1 *
`2/2010 Karlstadt Meyeroff
`et al.
`........................... .. 514/166
`et al. ........................... .. 514/166
`
`OFBOWEL
`
`222342122212 21* @4222; 0 Son . . . . . . . . . . . . . . . . . . . . . . ..
`
`(73) Assignee: Dr. Falk Pharma GmbH (DE)
`(73) Assignee: Dr. Falk Pharma GmbH (DE)
`
`( * ) Notice:
`( * ) Notice:
`
`Subject to any disclaimer, the term of this
`Subject to any disclaimer, the term of this
`patent is extended or adjusted under 35
`patent is extended or adjusted under 35
`U.S.C. 154(b) by 211 days.
`U.S.C.154(b)by211days.
`
`(21) APP1. N04 12/5731031
`
`(22)
`Filed:
`(22) Filed:
`
`Oct. 2, 2009
`Oct. 2, 2009
`
`(65)
`(65)
`
`Prior Publication Data
`Prior Publication Data
`
`US 2010/0086588 A1
`US 2010/0086588 A1
`
`Apr. 8, 2010
`Apr. 8, 2010
`
`Related U.S. Application Data
`Related US. Application Data
`.
`.
`.
`.
`(60) Provisional application No. 61/102,807, filed on Oct.
`
`(60) Provisional application No. 61/ 102,807, ?led on Oct. 3, 2008, provisional application No. 61/109,708, ?led
`3, 2008, provisional application No. 61/109,708, filed
`on Oct. 30, 2008.
`0n OCt. 30, 2008.
`
`(200601)
`(2006.01)
`(2006.01)
`(200601)
`(2006.01)
`
`(2006.01)
`
`(51)
`Int. Cl.
`(51) Int. Cl.
`A61]; 31/606
`A61K 31/606
`A61K 31/196
`A61K 31/136
`52 U 5 Cl
`(52) US’ Cl’
`A61K31/606 2013 01 _ A61K31/196
`(
`)
`'
`CPC ........... .. A61K31/606 (2013.01); A61K31/196
`"""""" "
`(2013 01)_(A61K31)}136 (2013 01)
`(201301), A61K31/136 (2013.01)
`'
`r
`'
`USPC ......... ... ...... ...................................... .. 514/166
`USPC ......... .... ...... ... .................................... .. 514/166
`(58) Fleld 0f Clasm?catlon searCh
`(58) Fleld of Classlficatmn Search
`NOD63
`None
`See application file for complete search history.
`See application ?le for complete search history.
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`7/2013 Otterbeck
`
`FOREIGN PATENT DOCUMENTS
`FOREIGN PATENT DOCUMENTS
`
`DE
`3
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`FR
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`WO
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`2004093883 A2
`2004093883 A2 11/2004
`
`.
`
`.
`
`.
`
`.
`
`.
`
`.
`
`OTHER PUBLICATIONS
`OTHER PUBLICATIONS
`Kruis et al., “Once Daily Dosing of 3g mesalamine (Salofalk Gran-
`Kruis et al., “Once Daily Dosing of 3g mesalamine (Salofalk Gran
`.
`.
`.
`.
`.
`.
`ules) is Therapeutic Equivalent to a Three-Times Daily Dosing of 1 g
`ules) 1s Therapeutic Equivalent to a Three-Times Dally Dos1ng of 1g
`mesalamine for the Treatment of Active Ulcerative Colitis” Gastro-
`mesalamine for the Treatment ofActive Ulcerative Colitis”, Gastro
`emerolo
`Vol 127 Issue 4
`A_130_A_131 Abstract 8’98 (A I
`enterology, vol. 127, Issue 4, pp. A-130-A-131, Abstract 898 (Apr.
`2007)., gy’
`'
`’
`’pp'
`’
`P‘
`2007)*
`Salix Pharmaceuticals Announces Submisson of Granulated
`SaliX Pharmaceuticals Announces Submisson of Granulated
`Mesalamine new Drug Application: Application Seeks Once-a-Day
`Mesalamine new Drug Application: Application Seeks Once-a-Day
`Dosing for Maintenance of Remission of Ulcerative Colitis. New
`Dosing for Maintenance of Remission of Ulcerative Colitis. New
`Release [online]. Salix Pharmaceuticals, Apr. 20, 2008 [retrieved on
`Release [online]. SaliX Pharmaceuticals, Apr. 20, 2008 [retrieved on
`Nov. 18, 2009]. Retrieved from the Internet: <URL: http://web.
`Nov. 18, 2009]. Retrieved from the Internet: <URL: http://web.
`archive.org/web/20080420074304/http://salix.com/news/stories/
`archive.org/web/20080420074304/http://saliX.com/news/stories/
`20071231.aspx> p. 1, para. [0002]; ti.
`20071231.aspx> p. 1, para. [0002]; ti.
`Xifaxan Trials Initiated in C. difficile—Associated Diarrhea, Irri-
`Xifaxan Trials Initiated in C. dif?cileiAssociated Diarrhea, Irri
`table Bowel Syndrome and Hepatic Encelophalopathy. New Article
`table Bowel Syndrome and Hepatic Encelophalopathy. New Article
`[online]. EndoNurse, Jan. 12, 2006 [retrieved on Nov. 18, 2009].
`[online]. EndoNurse, Jan. 12, 2006 [retrieved on Nov. 18, 2009].
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`hotnews/61h1216383748345.htm1> p. 2, para [0001].
`hotnews/61h1216383748345.htm1> p. 2, para [0001].
`(Continued)
`(Continued)
`
`Primary Examiner — David J Blanchard
`Primary Examiner * David J Blanchard
`Assistant Examiner — Barbara Frazier
`Assistant Examiner * Barbara Frazier
`(74) Attorney, Agent, or Firm — McCarter & English LLP;
`(74) Attorney, Agent, or Firm * McCarter & English LLP;
`Jonathan M. Sparks; Michael J. DeGrazia
`Jonathan M. Sparks; Michael J. DeGraZia
`
`(57)
`(57)
`
`ABSTRACT
`ABSTRACT
`
`Disclosed are methods for treating gastrointestinal disorders,
`Disclosed are methods for treating gastrointestinal disorders,
`e.g., Crohn’s disease, ulcerative colitis, and diverticular dis-
`e.g., Crohn’s disease, ulcerative colitis, and diverticular dis
`ease, with a granulated mesalamine formulation. Some for-
`ease, with a granulated mesalamine formulation. Some for
`mulations use granulated mesalainine in capsule form. Also
`mulations use granulated mesalamine in capsule form. Also
`included are methods to extend remission ofulcerative colitis
`included are methods to extend remission of ulcerative colitis
`by administration of a once-daily dosage of granulated
`by administration of a once-daily dosage of granulated
`mesalamine.
`mesalamine.
`
`16 Claims, 3 Drawing Sheets
`16 Claims, 3 Drawing Sheets
`
`MycoNovo, Inc.
`Foxhill Opportunity
`Fund, L.P.
`
`EX 1001
`
`

`
`US 8,865,688 B2
`US 8,865,688 B2
`Page 2
`Page 2
`
`(56)
`(56)
`
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