`
`Exhibit 1018
`
`‘688 Patent File History (“FH688”),
`Amendments to the Claims
`
`
`
`WHAT IS CLAIMED IS:
`
`Attorney Docket No. : 82741—2(473 81)
`
`A method of treating a subject having a gastrointestinal disorder comprising:
`
`selecting a patient that has failed treatment for a gastrointestinal disorder
`
`using mesalamine; and
`
`administering to the subject an effective amount of a granulated mesalamine
`
`formulation, thereby treating the subject.
`
`The method of claim 1, wherein the granulated mesalamine is in an extended release
`
`10
`
`formulation.
`
`The method of claim 1, wherein the gastrointestinal disorder is selected from the
`
`group consisting of: irritable bowel disease, gastrointestinal motility disorders,
`
`functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), Crohn's
`
`disease, ulcerative colitis (UC), active UC, UC in remission, diverticular disease,
`
`inflammatory bowel disease, and gastroparesis.
`
`The method of claim 1, wherein the effective amount of granulated mesalamine
`
`formulation comprises from between about 0.5 to about 4 g per day.
`
`The method of claim 1, wherein the effective amount of granulated mesalamine
`
`formulation comprises about 1.5 g per day.
`
`The method of claim 1, wherein the effective amount of granulated mesalamine
`
`formulation comprises about 3 g per day.
`
`The method of claim 5, wherein the 1.5 g of granulated mesalamine formulation is
`
`administered as four 375mg dosage units.
`
`The method of any one of claims 1-7, wherein the subject maintains remission of the
`
`gastrointestinal disease.
`
`The method of any one of claims 1-7, wherein the subject remains relapse free of the
`
`gastrointestinal disease.
`
`15
`
`20
`
`25
`
`30
`
`35
`
`BOS2 7588761
`
`42
`
`MycoNovo, Inc.
`Foxhill Opportunity Fund, L.P.
`
`EX1018
`
`
`
`Attorney Docket No. : 82741—2(473 81)
`
`10.
`
`11.
`
`12.
`
`The method of any one of claim 1-7, wherein the granulated mesalamine formulation
`
`is administered as a single daily dosage.
`
`The method of claim 1, wherein the subject’s rectal bleeding score improves over a
`
`baseline.
`
`The method of claim 1, wherein the physician’s rating of disease activity improves
`
`over a baseline.
`
`10
`
`13.
`
`The method of claim 1, wherein the subject’s stool frequency improves over baseline.
`
`15
`
`14.
`
`15.
`
`16.
`
`A method of treating a subject having ulcerative colitis comprising administering to
`
`the subject an effective amount of a granulated mesalamine formulation as a single
`
`daily dosage, wherein said single daily dosage results in treatment of the subject.
`
`The method of claim 14, wherein the subject maintains remission of ulcerative colitis.
`
`The method of claim 14, wherein the subject remains relapse free of ulcerative colitis.
`
`20
`
`17.
`
`The method of claim 1 or 14, wherein the granulated mesalamine formulation is a
`
`delayed and extended release formulation.
`
`18.
`
`The method of claim 14, wherein delayed and extended comprises first releasing
`
`mesalamine in ileum and continuing to release mesalamine throughout terminal ileum
`
`25
`
`and colon.
`
`19.
`
`20.
`
`30
`
`The method of claim 14, wherein the granulated mesalamine formulation is
`
`administered for the maintenance of remission of ulcerative colitis in subjects 18 years
`
`of age and older.
`
`The method of claim 14, wherein the granulated mesalamine formulation comprises
`
`four capsules administered once daily in the morning, afternoon or evening with or
`
`without food or without regard to meals.
`
`35
`
`21.
`
`The method of claim 14, the granulated mesalamine formulation comprises four
`
`capsules administered once daily in the morning, with or without food.
`
`BOS2 758876.1
`
`
`
`Attorney Docket No. : 82741—2(473 81)
`
`22.
`
`23.
`
`24.
`
`25.
`
`26.
`
`27.
`
`28.
`
`10
`
`15
`
`20
`
`The method of claim 14, wherein the granulated mesalamine formulation is not
`
`administered with antacids.
`
`The method of claim 14, further comprising advising the subject that hypersensitivity
`
`to salicylates, aminosalicylates, or any component of the granulated mesalamine
`
`formulation should not be administered the granulated mesalamine formulation.
`
`The method of claim 14, further comprising advising the subject that when being
`
`administered granulated mesalamine formulation renal impairment may occur.
`
`The method of claim 24, further comprising assessing the subject’s renal function one
`
`or more of at the beginning of treatment, before initiating therapy, or periodically
`
`during therapy.
`
`The method of claim 14, further comprising advising the subject that acute
`
`exacerbation of colitis symptoms can occur.
`
`The method of claim 14, further comprising advising the subject that the granulated
`
`mesalamine formulation should be used with caution in subjects with renal disease.
`
`The method of claim 14, further comprising monitoring the blood cell counts in
`
`geriatric subjects being administered the granulated mesalamine formulation.
`
`25
`
`29.
`
`The method of claim 14, further comprising advising the subject that there are adverse
`
`reactions associated with administration of the granulated mesalamine formulation.
`
`30.
`
`The method of claim 29, wherein the adverse reactions comprise one or more of
`
`headache, diarrhea, upper abdominal pain, nausea, nasopharyngitis, flu or flu—like
`
`30
`
`illness, sinusitis.
`
`31.
`
`32.
`
`35
`
`The method of claim 14, further comprising advising the subject that the granulated
`
`mesalamine formulation is not expected to inhibit the metabolism of drugs that are
`
`substrates of CYP1A2, CYPZC9, CYP2C19, CYPZD6, or CYP3A4.
`
`A method of treating a subject having a gastrointestinal disorder comprising:
`
`BOS2 7588761
`
`44
`
`
`
`Attorney Docket No.:82741—2(473 81)
`
`determining treatment failure from a non—granulated 5 —ASA mesalamine formulation;
`
`and
`
`administering to the subject an effective amount of a granulated mesalamine
`
`formulation to treat the subject.
`
`A method of treating a subject having a gastrointestinal disorder comprising:
`
`administering to the subject an effective amount of a granulated mesalamine
`
`formulation, wherein treatment of the subject with another formulation of mesalamine
`
`has failed;
`
`thereby treating the subject.
`
`A method of treating a subject having a gastrointestinal disorder comprising
`
`administering to the subject an effective amount of a granulated mesalamine
`
`formulation orally once daily in the morning.
`
`A method of treating or maintaining remission of ulcerative colitis, comprising:
`
`administering from between about 0.75 g and about 4 g of a granulated mesalamine
`
`formulation orally to the subject once daily in the morning.
`
`33.
`
`34.
`
`35.
`
`10
`
`15
`
`20
`
`36.
`
`The method of claim 35 , wherein about 1.5 g of the granulated mesalamine
`
`formulation is administered.
`
`25
`
`37.
`
`38.
`
`39.
`
`The method of claim 35 , wherein about 3 g of the granulated mesalamine formulation
`
`is administered.
`
`The method of claim 35 , wherein the granulated mesalamine formulation is taken
`
`without regard to meals.
`
`The method of claim 35, wherein the granulated mesalamine formulation is taken with
`
`30
`
`or without food.
`
`40.
`
`The method of claim 35 , wherein the granulated mesalamine formulation is not co-
`
`administered with antacids.
`
`35
`
`41.
`
`The method of claim 36, wherein the 1.5 g of granulated mesalamine formulation
`
`comprises four capsules.
`
`BOS2 758876.l
`
`
`
`Attorney Docket No.:82741—2(473 81)
`
`42.
`
`43.
`
`44.
`
`45.
`
`46.
`
`47.
`
`10
`
`15
`
`The method of claim 41, wherein the four capsules each comprise 0.375 g granulated
`
`mesalamine.
`
`The method of claim 41, wherein the four capsules each comprise from between about
`
`0.25 g to about 0.45 g mesalamine.
`
`The method of claim 35 , further comprising an evaluation of renal function prior to
`
`administration of the granulated mesalamine formulation.
`
`The method of claim 35 , wherein treatment is contraindicated if a subject has
`
`hypersensitivity to salicylates or aminosalicylates.
`
`The method of claim 35 , wherein the granulated mesalamine formulation is a locally-
`
`acting aminosalicylate.
`
`The method of claim 35, wherein the granulated mesalamine formulation is an
`
`extended release formulation.
`
`20
`
`48.
`
`The method of claim 35 , wherein the granulated mesalamine formulation is a delayed
`
`and an extended release formulation.
`
`49.
`
`50.
`
`25
`
`The method of claim 47 or 48, wherein extended release comprises release throughout
`
`the lumen of a colon.
`
`The method of claim 48, wherein delayed and extended comprises first releasing
`
`mesalamine in ileum and continuing to release mesalamine throughout terminal ileum
`
`and colon.
`
`30
`
`51.
`
`The method of claim 48, wherein delayed release comprises release at between about
`
`pH 5.7 to about pH 7.
`
`52.
`
`The method of claim 48, wherein delayed release comprises release at between about
`
`pH 6.
`
`35
`
`BOS2 758876.l
`
`
`
`Attorney Docket No. : 82741—2(473 81)
`
`53.
`
`The method of claim 35, wherein treatment of the subject with another formulation of
`
`mesalamine has failed.
`
`54.
`
`The method of claim 35, wherein the subject remains relapse free.
`
`55.
`
`A method of treating a subject for a gastrointestinal disorder comprising:
`
`administering to the subject corticosteroids followed by granulated mesalamine;
`
`thereby decreasing the incidence of adverse events in the subject after treatment with
`
`mesalamine.
`
`10
`
`56.
`
`57.
`
`The method of claim 55, wherein the gastrointestinal disorder is ulcerative colitis.
`
`The method of claim 56, wherein the adverse events are ulcerative colitis-related
`
`adverse events.
`
`58.
`
`A method of administering granulated mesalamine as a treatment for a
`
`gastrointestinal disorder, comprising:
`
`15
`
`advising a health care worker that subjects previously prescribed corticosteroids
`
`followed by granulated mesalamine have a decreased incidence of adverse events; and
`
`administering the granulated mesalamine to the patient in order to treat the gastrointestinal
`
`disorder.
`
`59.
`
`60.
`
`20
`
`The method of claim 58, wherein the gastrointestinal disorder is ulcerative colitis.
`
`The method of claim 59, wherein the adverse events are ulcerative colitis-related
`
`adverse events.
`
`61.
`
`A method of decreasing the incidence of adverse events in the subject having a
`
`gastrointestinal disorder after the subject has been treated with corticosteroids, comprising:
`
`administering granulated mesalamine to the subject,
`
`25
`
`thereby decreasing the incidence of adverse events.
`
`62.
`
`63.
`
`The method of claim 61, wherein the gastrointestinal disorder is ulcerative colitis.
`
`The method of claim 62, wherein the adverse events are ulcerative colitis-related
`
`adverse events.
`
`64.
`
`The method of claim 61, wherein the subject is administered a once daily dose of
`
`30
`
`granulated mesalamine.
`
`65.
`
`The method of claim 64, wherein the once daily dose is 1.5g of granulated mesalamine.
`
`BOS2 7588761
`
`47
`
`
`
`Attorney Docket No.:82741—2(473 81)
`
`66.
`
`The method of claim 65, wherein the once daily dose is administered as four capsules
`
`of 375mg granulated mesalamine.
`
`67.
`
`A method of treating a subject having a gastrointestinal disorder, comprising:
`
`advising a health care worker that subjects having a low mucosal score are most
`
`likely remain in remission from the gastrointestinal disorder; and
`
`administering the granulated mesalamine to the patient in order to treat the
`
`gastrointestinal disorder.
`
`68.
`
`69.
`
`10
`
`The method of claim 67, wherein the gastrointestinal disorder is ulcerative colitis.
`
`The method of claim 57, wherein the low mucosal score is 0.
`
`BOS2 7588761
`
`
`
`Application No.: 12/573,081
`
`Docket No.: 119557—02804
`
`AMENDMENTS TO THE CLAIMS
`
`This listing of claims will replace all prior versions of the claims and listing of the claims
`
`in the application:
`
`1. -13. (Cancelled)
`
`14.
`
`(Original) A method of treating a subject having ulcerative colitis comprising
`
`administering to the subject an effective amount of a granulated mesalamine formulation as a
`
`single daily dosage, wherein said single daily dosage results in treatment of the subject.
`
`15.
`
`(Original) The method of claim 14, wherein the subject maintains remission of ulcerative
`
`colitis.
`
`16.
`
`(Original) The method of claim 14, wherein the subject remains relapse free of ulcerative
`
`colitis.
`
`17.
`
`(Currently Amended) The method of claim -1—er—14, wherein the granulated mesalamine
`
`formulation is a delayed and extended release formulation.
`
`18.
`
`(Original) The method of claim 14, wherein delayed and extended comprises first
`
`releasing mesalamine in ileum and continuing to release mesalamine throughout terminal ileum
`
`and colon.
`
`19.
`
`(Original) The method of claim 14, wherein the granulated mesalamine formulation is
`
`administered for the maintenance of remission of ulcerative colitis in subjects 18 years of age
`
`and older.
`
`20.
`
`(Original) The method of claim 14, wherein the granulated mesalamine formulation
`
`comprises four capsules administered once daily in the morning, afternoon or evening with or
`
`without food or without regard to meals.
`
`ME1 12235108v.1
`
`
`
`Application No.: 12/573,081
`
`Docket No.: 119557—02804
`
`21.
`
`(Original) The method of claim 14, the granulated mesalamine formulation comprises
`
`four capsules administered once daily in the morning, with or without food.
`
`22.
`
`(Original) The method of claim 14, wherein the granulated mesalamine formulation is
`
`not administered with antacids.
`
`23.
`
`(Original) The method of claim 14, further comprising advising the subject that
`
`hypersensitivity to salicylates, aminosalicylates, or any component of the granulated mesalamine
`
`formulation should not be administered the granulated mesalamine formulation.
`
`24.
`
`(Original) The method of claim 14, further comprising advising the subject that when
`
`being administered granulated mesalamine formulation renal impairment may occur.
`
`25.
`
`(Original) The method of claim 24, further comprising assessing the subject’s renal
`
`function one or more of at the beginning of treatment, before initiating therapy, or periodically
`
`during therapy.
`
`26.
`
`(Original) The method of claim 14, further comprising advising the subject that acute
`
`exacerbation of colitis symptoms can occur.
`
`27.
`
`(Original) The method of claim 14, further comprising advising the subject that the
`
`granulated mesalamine formulation should be used with caution in subjects with renal disease.
`
`28.
`
`(Original) The method of claim 14, further comprising monitoring the blood cell counts
`
`in geriatric subjects being administered the granulated mesalamine formulation.
`
`29.
`
`(Original) The method of claim 14, further comprising advising the subject that there are
`
`adverse reactions associated with administration of the granulated mesalamine formulation.
`
`30.
`
`(Original) The method of claim 29, wherein the adverse reactions comprise one or more
`
`of headache, diarrhea, upper abdominal pain, nausea, nasopharyngitis, flu or flu—like illness,
`
`sinusitis.
`
`ME1 12235108v.1
`
`
`
`Application No.: 12/573,081
`
`Docket No.: 119557—02804
`
`31.
`
`(Original) The method of claim 14, further comprising advising the subject that the
`
`granulated mesalamine formulation is not expected to inhibit the metabolism of drugs that are
`
`substrates of CYP1A2, CYPZC9, CYPZC19, CYP2D6, or CYP3A4.
`
`32.—34. (Cancelled)
`
`35.
`
`(Original) A method of treating or maintaining remission of ulcerative colitis,
`
`comprising:
`
`administering from between about 0.75 g and about 4 g of a granulated mesalamine
`
`formulation orally to the subject once daily in the morning.
`
`36.
`
`(Original) The method of claim 35, wherein about 1.5 g of the granulated mesalamine
`
`formulation is administered.
`
`37.
`
`(Original) The method of claim 35, wherein about 3 g of the granulated mesalamine
`
`formulation is administered.
`
`38.
`
`(Original) The method of claim 35, wherein the granulated mesalamine formulation is
`
`taken without regard to meals.
`
`39.
`
`(Original) The method of claim 35, wherein the granulated mesalamine formulation is
`
`taken with or without food.
`
`40.
`
`(Original) The method of claim 35, wherein the granulated mesalamine formulation is
`
`not co—administered with antacids.
`
`41.
`
`(Original) The method of claim 36, wherein the 1.5 g of granulated mesalamine
`
`formulation comprises four capsules.
`
`42.
`
`(Original) The method of claim 41, wherein the four capsules each comprise 0.375 g
`
`granulated mesalamine.
`
`ME1 12235108v.1
`
`
`
`Application No.: 12/573,081
`
`Docket No.: 119557—02804
`
`43.
`
`(Original) The method of claim 41, wherein the four capsules each comprise from
`
`between about 0.25 g to about 0.45 g mesalamine.
`
`44.
`
`(Original) The method of claim 35, further comprising an evaluation of renal function
`
`prior to administration of the granulated mesalamine formulation.
`
`45.
`
`(Original) The method of claim 35, wherein treatment is contraindicated if a subject has
`
`hypersensitivity to salicylates or aminosalicylates.
`
`46.
`
`(Original) The method of claim 35, wherein the granulated mesalamine formulation is a
`
`locally—acting aminosalicylate.
`
`47.
`
`(Original) The method of claim 35, wherein the granulated mesalamine formulation is an
`
`extended release formulation.
`
`48.
`
`(Original) The method of claim 35, wherein the granulated mesalamine formulation is a
`
`delayed and an extended release formulation.
`
`49.
`
`(Original) The method of claim 47 or 48, wherein extended release comprises release
`
`throughout the lumen of a colon.
`
`50.
`
`(Original) The method of claim 48, wherein delayed and extended comprises first
`
`releasing mesalamine in ileum and continuing to release mesalamine throughout terminal ileum
`
`and colon.
`
`51.
`
`(Original) The method of claim 48, wherein delayed release comprises release at between
`
`about pH 5.7 to about pH 7.
`
`52.
`
`(Original) The method of claim 48, wherein delayed release comprises release at between
`
`about pH 6.
`
`ME1 12235108v.1
`
`
`
`Application No.: 12/573,081
`
`Docket No.: ll9557—02804
`
`53.
`
`(Original) The method of claim 35, wherein treatment of the subject with another
`
`formulation of mesalamine has failed.
`
`54.
`
`(Original) The method of claim 35, wherein the subject remains relapse free.
`
`55.—69. (Cancelled)
`
`MEI l2235lO8v.l
`
`
`
`Application No.: 12/573,081
`
`Docket No.: 122184—02804
`
`AMENDMENTS TO THE CLAIMS
`
`This listing of claims will replace all prior Versions, and listing of claims, in this
`
`application.
`
`Listing of Claims:
`
`1-13. (Canceled)
`
`14.
`
`(Currently Amended) A method of treating maintaining the remission of ulcerative colitis
`
`ina subject comprising administering to the subject @
`
`dose of a granulated mesalamine formulation
`
`once per day, wherein said method
`
`maintains remission of ulcerative colitis in the subject for a period of at least 6 months of
`treatment wherein remission is defined as a DAI score of 0 or 1.
`
`15.
`
`(Cancelled)
`
`16.
`
`(Cancelled)
`
`17.
`
`(Previously Presented) The method of claim 14, wherein the granulated mesalamine
`
`formulation is a delayed and extended release formulation.
`
`18.
`
`(Currently Amended) The method of claim [[14]]1_7, wherein delayed and extended
`
`comprises first releasing mesalamine in ileum and continuing to release mesalamine throughout
`
`terminal ileum and colon.
`
`19.
`
`(Original) The method of claim 14, wherein the granulated mesalamine formulation is
`
`administered for the maintenance of remission of ulcerative colitis in subjects 18 years of age
`
`and older.
`
`20.
`
`(Currently Amended) The method of claim 14, wherein the granulated mesalamine
`
`formulation comprises four capsules administered once d-ail-y per day in the morning, afternoon
`
`or evening with or without food or without regard to meals.
`
`ME1 14116338v.1
`
`
`
`Application No.: 12/573,081
`
`Docket No.: 122184—02804
`
`21.
`
`(Currently Amended) The method of claim 14, the granulated mesalamine formulation
`
`comprises four capsules administered d-aei-l-y per day in the morning, with or without food.
`
`22.
`
`(Original) The method of claim 14, wherein the granulated mesalamine formulation is
`
`not administered with antacids.
`
`23.
`
`(Currently Amended) The method of claim 14, further comprising advising the subject
`
`that subjects having hypersensitivity to salicylates, aminosalicylates, or any component of the
`
`granulated mesalamine formulation should not be administered the granulated mesalamine
`
`formulation.
`
`24.
`
`(Original) The method of claim 14, further comprising advising the subject that when
`
`being administered granulated mesalamine formulation renal impairment may occur.
`
`25.
`
`(Original) The method of claim 24, further comprising assessing the subject’s renal
`
`function one or more of at the beginning of treatment, before initiating therapy, or periodically
`
`during therapy.
`
`26.
`
`(Original) The method of claim 14, further comprising advising the subject that acute
`
`exacerbation of colitis symptoms can occur.
`
`27.
`
`(Original) The method of claim 14, further comprising advising the subject that the
`
`granulated mesalamine formulation should be used with caution in subjects with renal disease.
`
`28.
`
`(Original) The method of claim 14, further comprising monitoring the blood cell counts
`
`in geriatric subjects being administered the granulated mesalamine formulation.
`
`29.
`
`(Original) The method of claim 14, further comprising advising the subject that there are
`
`adverse reactions associated with administration of the granulated mesalamine formulation.
`
`ME1 14116338v.1
`
`
`
`Application No.: 12/573,081
`
`Docket No.: 122184—02804
`
`30.
`
`(Original) The method of claim 29, wherein the adverse reactions comprise one or more
`
`of headache, diarrhea, upper abdominal pain, nausea, nasopharyngitis, flu or flu—like illness,
`
`sinusitis.
`
`31.
`
`(Original) The method of claim 14, further comprising advising the subject that the
`
`granulated mesalamine formulation is not expected to inhibit the metabolism of drugs that are
`
`substrates of CYP1A2, CYP2C9, CYP2C19, CYP2D6, or CYP3A4.
`
`32-34. (Canceled)
`
`35.
`
`(Currently Amended) A method of maintaining remission of ulcerative colitis
`
`in a sub'ect, comprising:
`
`administeringf to the subject a single 1.5 gram
`
`dose of a granulated mesalamine formulation once per day%MH+ in the
`
`morning, wherein the method maintains remission of ulcerative colitis in the sub'ect for a period
`of at least 6 months of treatment wherein remission is defined as a DAI score of 0 or 1.
`
`36.
`
`(Cancelled)
`
`37.
`
`(Cancelled)
`
`38.
`
`(Original) The method of claim 35, wherein the granulated mesalamine formulation is
`
`taken without regard to meals.
`
`39.
`
`(Original) The method of claim 35, wherein the granulated mesalamine formulation is
`
`taken with or without food.
`
`40.
`
`(Original) The method of claim 35, wherein the granulated mesalamine formulation is
`
`not co—administered with antacids.
`
`41.
`
`(Currently Amended) The method of claim fiéré, wherein the 1.5 g of granulated
`
`mesalamine formulation comprises four capsules.
`
`ME1 14116338v.1
`
`4
`
`
`
`Application No.: 12/573,081
`
`Docket No.: 122184—02804
`
`42.
`
`(Original) The method of claim 41, wherein the four capsules each comprise 0.375 g
`
`granulated mesalamine.
`
`43.
`
`(Cancelled)
`
`44.
`
`(Original) The method of claim 35, further comprising an evaluation of renal function
`
`prior to administration of the granulated mesalamine formulation.
`
`45.
`
`(Original) The method of claim 35, wherein treatment is contraindicated if a subject has
`
`hypersensitivity to salicylates or aminosalicylates.
`
`46.
`
`(Original) The method of claim 35, wherein the granulated mesalamine formulation is a
`
`locally—acting aminosalicylate.
`
`47.
`
`(Original) The method of claim 35, wherein the granulated mesalamine formulation is an
`
`extended release formulation.
`
`48.
`
`(Original) The method of claim 35, wherein the granulated mesalamine formulation is a
`
`delayed and an extended release formulation.
`
`49.
`
`(Original) The method of claim 47 or 48, wherein extended release comprises release
`
`throughout the lumen of a colon.
`
`50.
`
`(Original) The method of claim 48, wherein delayed and extended comprises first
`
`releasing mesalamine in ileum and continuing to release mesalamine throughout terminal ileum
`
`and colon.
`
`51.
`
`(Original) The method of claim 48, wherein delayed release comprises release at between
`
`about pH 5.7 to about pH 7.
`
`ME1 14116338v.1
`
`
`
`Application No.: 12/573,081
`
`Docket No.: 122184—02804
`
`52.
`
`(Original) The method of claim 48, wherein delayed release comprises release at between
`
`about pH 6.
`
`53.
`
`(Original) The method of claim 35, wherein treatment of the subject with another
`
`formulation of mesalamine has failed.
`
`54-69. (Canceled)
`
`70.
`
`(New) The method of claim 14, further comprising selecting a subject with a DAI score
`
`of 0 or 1 for maintaining remission of ulcerative colitis with granulated mesalamie.
`
`71.
`
`(New) The method of claim 35, further comprising selecting a subject with a DAI score
`
`of 0 or 1 for maintaining remission of ulcerative colitis with granulated mesalamie.
`
`72.
`
`(New) The method of claim 21, wherein the four capsules each comprise 0.375 g
`
`granulated mesalamine.
`
`ME1 14116338v.1
`
`
`
`Docket No.: 122184—02804
`
`Application No.: 12/573,081
`
`AMENDMENTS TO THE CLAIMS
`
`This listing of claims will replace all prior Versions, and listing of claims, in this
`
`application.
`
`Listing of Claims:
`
`1-13. (Cancelled)
`
`14.
`
`(Currently Amended) A method of maintaining the remission of ulcerative colitis in a
`
`subject comprising administering to the subject a single 1.5 gram dose of a granulated
`
`mesalamine formulation once per day, wherein;
`
`said method maintains remission of ulcerative colitis in the subject for a period of at least
`
`6 months of treatment[[,]];whe1=eirn
`
`remission is defined as a DAI score of 0 or 1[[,]]; and
`
`the granulated mesalamine formulation is not administered with antacids.
`
`15.
`
`(Cancelled)
`
`16.
`
`(Cancelled)
`
`17.
`
`(Previously Presented) The method of claim 14, wherein the granulated mesalamine
`
`formulation is a delayed and extended release formulation.
`
`18.
`
`(Previously Presented) The method of claim 17, wherein delayed and extended comprises
`
`first releasing mesalamine in ileum and continuing to release mesalamine throughout terminal
`
`ileum and colon.
`
`19.
`
`(Original) The method of claim 14, wherein the granulated mesalamine formulation is
`
`administered for the maintenance of remission of ulcerative colitis in subjects 18 years of age
`
`and older.
`
`ME1 14492589v.1
`
`
`
`Docket No.: 122184—02804
`
`Application No.: 12/573,081
`
`20.
`
`(Previously Presented) The method of claim 14, wherein the granulated mesalamine
`
`formulation comprises four capsules administered once per day in the morning, afternoon or
`
`evening with or without food or without regard to meals.
`
`21.
`
`(Previously Presented) The method of claim 14, the granulated mesalamine formulation
`
`comprises four capsules administered per day in the morning, with or without food.
`
`22.
`
`(Cancelled)
`
`23.
`
`(Previously Presented) The method of claim 14, further comprising advising the subject
`
`that subjects having hypersensitivity to salicylates, aminosalicylates, or any component of the
`
`granulated mesalamine formulation should not be administered the granulated mesalamine
`
`formulation.
`
`24.
`
`(Original) The method of claim 14, further comprising advising the subject that when
`
`being administered granulated mesalamine formulation renal impairment may occur.
`
`25.
`
`(Original) The method of claim 24, further comprising assessing the subject’s renal
`
`function one or more of at the beginning of treatment, before initiating therapy, or periodically
`
`during therapy.
`
`26.
`
`(Original) The method of claim 14, further comprising advising the subject that acute
`
`exacerbation of colitis symptoms can occur.
`
`27.
`
`(Original) The method of claim 14, further comprising advising the subject that the
`
`granulated mesalamine formulation should be used with caution in subjects with renal disease.
`
`28.
`
`(Original) The method of claim 14, further comprising monitoring the blood cell counts
`
`in geriatric subjects being administered the granulated mesalamine formulation.
`
`ME1 14492589v.1
`
`
`
`Docket No.: 122184—02804
`
`Application No.: 12/573,081
`
`29.
`
`(Original) The method of claim 14, further comprising advising the subject that there are
`
`adverse reactions associated with administration of the granulated mesalamine formulation.
`
`30.
`
`(Original) The method of claim 29, wherein the adverse reactions comprise one or more
`
`of headache, diarrhea, upper abdominal pain, nausea, nasopharyngitis, flu or flu—like illness,
`
`sinusitis.
`
`31.
`
`(Original) The method of claim 14, further comprising advising the subject that the
`
`granulated mesalamine formulation is not expected to inhibit the metabolism of drugs that are
`
`substrates of CYP1A2, CYP2C9, CYP2C19, CYP2D6, or CYP3A4.
`
`32-69. (Cancelled)
`
`70.
`
`(Currently Amended) The method of claim 14, further comprising selecting a subject
`
`with a DAI score of 0 or 1 for maintaining remission of ulcerative colitis with granulated
`
` mesalamine.
`
`71.
`
`(Cancelled)
`
`72.
`
`(Previously Presented) The method of claim 21, wherein the four capsules each comprise
`
`0.375 g granulated mesalamine.
`
`ME1 14492589v.1
`
`
`
`Docket No.: 122184—02804
`
`Application No.: 12/573,081
`
`AMENDMENTS TO THE CLAIMS
`
`This listing of claims will replace all prior versions, and listing of claims, in this
`
`application.
`
`Listing of Claims:
`
`1- 13. (Cancelled)
`
`14.
`
`(Previously Presented) A method of maintaining the remission of ulcerative colitis in a
`
`subject comprising administering to the subject a single 1.5 gram dose of a granulated
`
`mesalamine formulation once per day, wherein:
`
`said method maintains remission of ulcerative colitis in the subject for a period of at least
`
`6 months of treatment;
`
`remission is defined as a DAI score of 0 or 1; and
`
`the granulated mesalamine formulation is not administered with antacids.
`
`15.
`
`(Cancelled)
`
`16.
`
`(Cancelled)
`
`17.
`
`(Previously Presented) The method of claim 14, wherein the granulated mesalamine
`
`formulation is a delayed and extended release formulation.
`
`18.
`
`(Previously Presented) The method of claim 17, wherein delayed and extended comprises
`
`first releasing mesalamine in ileum and continuing to release mesalamine throughout terminal
`
`ileum and colon.
`
`19.
`
`(Original) The method of claim 14, wherein the granulated mesalamine formulation is
`
`administered for the maintenance of remission of ulcerative colitis in subjects 18 years of age
`
`and older.
`
`ME1 15162951v.1
`
`
`
`Docket No.: 122184—02804
`
`Application No.: 12/573,081
`
`20.
`
`(Previously Presented) The method of claim 14, wherein the granulated mesalamine
`
`formulation comprises four capsules administered once per day in the morning, afternoon or
`
`evening with or without food or without regard to meals.
`
`21.
`
`(Previously Presented) The method of claim 14, the granulated mesalamine formulation
`
`comprises four capsules administered per day in the morning, with or without food.
`
`22.
`
`(Cancelled)
`
`23.
`
`(Previously Presented) The method of claim 14, further comprising advising the subject
`
`that subjects having hypersensitivity to salicylates, aminosalicylates, or any component of the
`
`granulated mesalamine formulation should not be administered the granulated mesalamine
`
`formulation.
`
`24.
`
`(Original) The method of claim 14, further comprising advising the subject that when
`
`being administered granulated mesalamine formulation renal impairment may occur.
`
`25.
`
`(Original) The method of claim 24, further comprising assessing the subject’s renal
`
`function one or more of at the beginning of treatment, before initiating therapy, or periodically
`
`during therapy.
`
`26.
`
`(Original) The method of claim 14, further comprising advising the subject that acute
`
`exacerbation of colitis symptoms can occur.
`
`27.
`
`(Original) The method of claim 14, further comprising advising the subject that the
`
`granulated mesalamine formulation should be used with caution in subjects with renal disease.
`
`28.
`
`(Original) The method of claim 14, further comprising monitoring the blood cell counts
`
`in geriatric subjects being administered the granulated mesalamine formulation.
`
`ME1 15162951v.1
`
`
`
`Docket No.: 122184—02804
`
`Application No.: 12/573,081
`
`29.
`
`(Original) The method of claim 14, further comprising advising the subject that there are
`
`adverse reactions associated with administration of the granulated mesalamine formulation.
`
`30.
`
`(Original) The method of claim 29, wherein the adverse reactions comprise one or more
`
`of headache, diarrhea, upper abdominal pain, nausea, nasopharyngitis, flu or flu—like illness,
`
`sinusitis.
`
`31.
`
`(Original) The method of claim 14, further comprising advising the subject that the
`
`granulated mesalamine formulation is not expected to inhibit the metabolism of drugs that are
`
`substrates of CYP1A2, CYP2C9, CYP2C19, CYP2D6, or CYP3A4.
`
`32-69. (Cancelled)
`
`70.
`
`(Previously Presented) The method of claim 14, further comprising selecting a subject
`
`with a DAI score of 0 or 1 for maintaining remission of ulcerative colitis with granulated
`
`mesalamine.
`
`71.
`
`(Cancelled)
`
`72.
`
`(Previously Presented) The method of claim 21, wherein the four cap
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