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Methods of treating crohn's disease and ulcerative colitis

a technology of ulcerative colitis and crohn's disease, which is applied in the field of methods of treating crohn's disease and ulcerative colitis, can solve the problems of inability to respond to conventional treatment or experience intolerance of patients,

Pending Publication Date: 2021-11-25
ABBVIE INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0119]In one embodiment, the patient is unable to taper corticosteroid below a dose equivalent to prednisone 10 mg daily orally without recurrent active disease.
[0139]In one embodiment, the patient is unable to taper corticosteroid below a dose equivalent to prednisone 10 mg daily orally without recurrent active disease.
[0158]In one embodiment, the patient is unable to taper corticosteroid below a dose equivalent to prednisone 10 mg daily orally without recurrent active disease.

Problems solved by technology

The patient may have had an inadequate response to or experienced intolerance to conventional treatment, such as aminosalicylates, corticosteroids or immunosuppressants, or to a previous treatment with an anti-TNF therapy or another biologic agent.

Method used

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  • Methods of treating crohn's disease and ulcerative colitis
  • Methods of treating crohn's disease and ulcerative colitis
  • Methods of treating crohn's disease and ulcerative colitis

Examples

Experimental program
Comparison scheme
Effect test

example 1

on of Amorphous Freebase

[0728]A. Method A: Precipitation from Water

[0729]Upadacitinib (approximately 300 g) was dissolved in water (10 L) and 50% sodium hydroxide (160 g) was added drop-wise over a two hour period to adjust the pH to greater than 12. Solids formed immediately. The solids were filtered, washed with two 500 mL aliquots of water, and then dried in a vacuum oven. The solids were equilibrated for a short period of time at ambient temperature prior to characterization. Conversion to Amorphous Freebase of upadacitinib was confirmed by PXRD analysis.

[0730]B. Method B: Dehydration of Freebase Hydrate Form B

[0731]A sample of the Freebase Hydrate Form B form of upadacitinib (crystallized from ethanol / water at sub-ambient temperatures as described in Example 2, Method C below) was placed in a vacuum oven at 40° C. overnight. The solids removed from the vacuum oven were equilibrated for a short time at 23° C. prior to characterization. Conversion to Amorphous Freebase of upadaci...

example 2

on of Freebase Solvate Form a and Freebase Hydrate Form B

[0732]A. Method A: Freebase Solvate Form a (Isopropyl Acetate / Water Solvate)

[0733]A sample of the Amorphous Freebase of upadacitinib (25 mg) was added to a vial followed by isopropyl acetate (125 μL) and water (10 μL). All solids dissolved at ambient temperature. The solution was placed in a freezer at −16° C. for 4 days. The liquor was decanted and the crystallized solids were isolated. The isolated crystals were analyzed by PXRD while still wet. Conversion to Freebase Solvate Form A (isopropyl acetate / water solvate) of upadacitinib was confirmed by PXRD analysis.

[0734]B. Method B: Freebase Hydrate Form B from Methanol / Water

[0735]A sample of the Amorphous Freebase of upadacitinib (164 mg) and MeOH (621 mg) were added to a vial. The components were mixed at ambient temperature until the solids dissolved. Water (approximately 680 μL) was added to the vial and the vial was placed in an ice / sodium chloride bath at approximately −...

example 3

on of Freebase Hydrate Form C

[0741]A. Method A: Freebase Hydrate Form C from Ethanol / Water

[0742]A sample of the Amorphous Freebase of upadacitinib (2 g) was transferred to a 500 mL beaker equipped with a stirring bar. EtOH (50 g) was added to the beaker and stirred until all solids dissolved. The solution was transferred to a 250 mL jacketed flask equipped with a dispersing device. The solution was cooled to 6° C. Water (150 g) was added to the solution and the solution was subjected to high shear for two hours using the dispersing device. After solid formation was observed, an additional amount of water (50 g) was added to the resulting suspension. The suspension was held overnight at ambient temperature. Solids were isolated and examined on the following day. Conversion to upadacitinib Freebase Hydrate Form C was confirmed by PXRD analysis.

[0743]B. Method B: Freebase Hydrate Form C from Ethyl Acetate / Heptane / Water

[0744]A crude reaction mixture assaying for 11.1 g of upadacitinib w...

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Abstract

The present disclosure is directed to methods for treating Crohn's disease, and in particular, to methods for inducing clinical remission and / or endoscopic improvement of Crohn's disease, using a JAK1 inhibitor. In certain embodiments, the patient is administered an induction dose of the JAK1 inhibitor to induce clinical remission and / or endoscopic improvement of the Crohn's disease, followed by administration of at least one maintenance dose of the JAK1 inhibitor thereafter. In other embodiments, the present disclosure is directed to methods for treating ulcerative colitis using a JAK1 inhibitor.

Description

RELATED APPLICATIONS[0001]This application is a continuation of U.S. patent application Ser. No. 15 / 917,013, filed Mar. 9, 2018, and which claims priority to U.S. Provisional Application No. 62 / 469,337, filed Mar. 9, 2017, U.S. Provisional Application No. 62 / 470,565, filed Mar. 13, 2017, U.S. Provisional Application 62 / 483,289, filed Apr. 7, 2017 and U.S. Provisional Application No. 62 / 593,629, filed Dec. 1, 2017, each of which is incorporated by reference in its entirety.FIELD OF THE DISCLOSURE[0002]The present disclosure is directed to methods for treating inflammatory bowel diseases, such as Crohn's disease and ulcerative colitis, and in particular, to methods for inducing clinical remission and endoscopic improvement of Crohn's disease or a clinical remission and endoscopic improvement of ulcerative colitis, using a JAK1 inhibitor. In certain embodiments, the patient is administered an induction dose of the JAK1 inhibitor to induce clinical remission and / or endoscopic improvemen...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/4985A61K31/495A61P1/00A61K9/00A61K9/48
CPCA61K31/4985A61K31/495A61K9/48A61K9/0053A61P1/00
Inventor THAKKAR, ROOPAL B.JUNGERWIRTH, STEVENMACHADO DE LACERDA, ANA PAULAROBINSON, ANN M.ENEJOSA, JOSE JEFFREY V.PANGAN, AILEEN L.MOHAMED, MOHAMED-ESLAM F.OTHMAN, AHMED A.KLUNDER, BENALLIAN, AYMAN D.
Owner ABBVIE INC
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