USOO961 0321B2
`
`(12) United States Patent
`Comiskey et al.
`
`(10) Patent No.:
`(45) Date of Patent:
`
`US 9,610,321 B2
`*Apr. 4, 2017
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`FORMULATIONS OF GUANYLATE
`CYCLASE CAGONSTS AND METHODS OF
`USE
`
`Applicant: Synergy Pharmaceuticals Inc., New
`York, NY (US)
`Inventors: Stephen Comiskey, Doylestown, PA
`(US); Rong Feng, Langhorne, PA (US);
`John Foss, Doylestown, PA (US);
`Kunwar Shailubhai, Audubon, PA
`(US)
`Assignee: SYNERGY PHARMACEUTICALS,
`INC., New York, NY (US)
`Subject to any disclaimer, the term of this
`patent is extended or adjusted under 35
`U.S.C. 154(b) by 0 days.
`This patent is Subject to a terminal dis
`claimer.
`
`Notice:
`
`Appl. No.: 14/845,644
`Filed:
`Sep. 4, 2015
`
`Prior Publication Data
`US 2015/0366935 A1
`Dec. 24, 2015
`
`Related U.S. Application Data
`Continuation of application No. 14/661,299, filed on
`Mar. 18, 2015, now abandoned, which is a
`continuation of application No. 13/421,769, filed on
`Mar. 15, 2012, which is a continuation-in-part of
`application No. PCT/US2011/051805, filed on Sep.
`15, 2011.
`Provisional application No. 61/383,156, filed on Sep.
`15, 2010, provisional application No. 61/387,636,
`filed on Sep. 29, 2010, provisional application No.
`61/392,186, filed on Oct. 12, 2010.
`
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
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`
`Int. C.
`A6 IK 38/10
`A6 IK 9/48
`A6 IK 9/00
`A6 IK 38/12
`C07K 7/54
`A6 IK 9/16
`A6 IK 9/20
`A6 IK 45/06
`A6 IK3I/92
`A6 IK3I/50 I
`A 6LX 3/59
`A6 IK3I/53
`A6 IK3I/765
`A6 IK3I/78
`U.S. C.
`CPC ............ A61K 38/12 (2013.01); A61K 9/1623
`(2013.01); A61K 9/1652 (2013.01); A61 K
`9/1676 (2013.01); A61K 9/2054 (2013.01);
`A61K 9/4858 (2013.01); A61K 9/4866
`(2013.01); A61K 31/192 (2013.01); A61 K
`
`3 1/501 (2013.01); A61 K3I/519 (2013.01);
`A6 IK3I/53 (2013.01); A61 K3I/765
`(2013.01); A61 K3I/78 (2013.01); A61K 38/10
`(2013.01); A61K 45/06 (2013.01); C07K 7/54
`(2013.01); C12Y 406/0.1002 (2013.01)
`(58) Field of Classification Search
`None
`See application file for complete search history.
`
`(56)
`
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`(Guanilib) in Chronic Constipation and Irritable Bowel Syndrome.
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`(Continued)
`
`Primary Examiner — Satyanarayana R. Gudibande
`Assistant Examiner — Jia-Hai Lee
`(74) Attorney, Agent, or Firm — Cynthia Kozakiewicz;
`Ivor Elrifi
`
`(57)
`
`ABSTRACT
`
`The invention provides low-dose formulations of guanylate
`cyclase-C (“GCC) agonist peptides and methods for their
`use. The formulations of the invention can be administered
`either alone or in combination with one or more additional
`therapeutic agents, preferably an inhibitor of c(GMP-depen
`dent phosphodiesterase or a laxative.
`
`16 Claims, 6 Drawing Sheets
`
`MYLAN - EXHIBIT 1001
`
`

`

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`

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`US 9,610,321 B2
`
`1.
`FORMULATIONS OF GUANYLATE
`CYCLASE CAGONSTS AND METHODS OF
`USE
`
`RELATED APPLICATIONS
`
`This application is a continuation of U.S. patent applica
`tion Ser. No. 14/661,299, filed Mar. 18, 2015, which is a
`continuation of U.S. patent application Ser. No. 13/421,769,
`filed Mar. 15, 2012, which is a continuation-in-part of
`PCT/US2011/051805 filed on Sep. 15, 2011, which claims
`the benefit of priority to U.S. Provisional Application No.
`61/383,156 filed on Sep. 15, 2010, U.S. Provisional Appli
`cation No. 61/387,636 filed on Sep. 29, 2010, and U.S.
`Provisional Application No. 61/392,186 filed on Oct. 12,
`2010, the contents of which are incorporated by reference in
`their entireties.
`
`10
`
`15
`
`INCORPORATION-BY-REFERENCE OF
`SEQUENCE LISTING
`
`named
`file
`text
`the
`of
`COntents
`The
`“SYPA 009 CO2US Sequence Listing..txt”, which was
`created on Sep. 3, 2015 and is 113 KB in size, are hereby
`incorpor